CN1878777A

CN1878777A - 2,3-dihydro-6-nitroimidazo (2,1-b) oxazole compounds for the treatment of tuberculosis

Info

Publication number: CN1878777A
Application number: CN 200480032244
Authority: CN
Inventors: 壶内英继; 佐佐木博文; 丝谷元宏; 原口佳和; 宫村伸; 松本真; 桥诘博之; 富重辰夫; 川崎昌则; 大黑绢枝; 住田卓美; 长谷川武司; 田中一穗; 竹村勋
Original assignee: Otsuka Pharmaceutical Co Ltd
Current assignee: Otsuka Pharmaceutical Co Ltd
Priority date: 2003-10-31
Filing date: 2004-10-29
Publication date: 2006-12-13
Anticipated expiration: 2024-10-29
Also published as: UA91822C2; CN100497345C; ZA200602184B

Abstract

The present invention provides a 2,3-dihydro-6-nitroimidazo[2,1-b]oxazole compound represented by the following general formula: (1)in the above formula (1), R1 represents a hydrogen atom or C1-C6 alkyl group, n represents an integer of 0 to 6, R1 and -(CH2)nR2 may form a spiro ring represented by the formula (30) below, together with the adjacent carbon atom (in the formula below, RRR represents a piperidyl group which may have substituents on the piperidine ring), (30)and R2 represents a benzothiazolyloxy group, quinolyloxy group, pyridyloxy group or the like. The present compound has an excellent bactericidal action against Mycobacterium tuberculosis, multi-drug-resistant Mycobacterium tuberculosis, and atypical acid-fast bacteria.

Description

Treat lungyly 2,3-dihydro-6-nitroimidazole is [2,1-b] _ azole compounds also

Technical field

The present invention relates to 2, the 3-glyoxalidine is [2,1-b] _ azole compounds also.

Background technology

In aciduric bacteria, the people Mycobacterium tuberculosisBe known.It is said that 1/3rd population infection has this bacterium.Except the people Mycobacterium tuberculosisIn addition, Mycobacterium africanumWith The ox branch BacillusKnownly also belong to Mycobacterium tuberculosisClass.These bacteriums are known to be that the mankind are had powerful pathogenic mycobacterium.

Resist these treatments lungy and utilize three kinds of medicines to carry out, i.e. Rimactazid and Tibutol (or Streptomycin sulphate), they are regarded as a line medicine, perhaps utilize four kinds of medicines to carry out, for example above-mentioned three kinds and pyrazinoic acid amide.

But, because treatment lungy requires very secular drug administration, this may cause poor compliance, and treatment often ends in failure.

And about said medicine, reported: Rifampin causes hepatopathy, influenza syndrome, drug allergy, and because the inducing action of P450-relevant enzyme, and the concomitant dosing of itself and other drug is incompatibility; The vazadrine causes the peripheral nervous system obstacle when uniting use with Rifampin, bring out serious hepatopathy; Tibutol is because optic nerve disorder causes visual deterioration; Streptomycin sulphate reduces owing to the 8th cranial nerve obstacle causes hearing; Pyrazinoic acid amide causes untoward reaction, and for example hepatopathy, the gout relevant with the uric acid level increase are shown effect, vomiting (A Clinician ' s Guide ToTuberculosis, Michael D.Iseman 2000 by Lippincott Williams ﹠amp; Wilkins, printed in the USA, ISBN 0-7817-1749-3, Tuberculosis, 2ndedition, Fumiyuki Kuze and Takahide Izumi, Igaku-Shoin Ltd., 1992).

In fact, reported owing to can not carry out 70% (about 23%, 52 example) (Kekkaku, the Vol.74 that the case of standard chemical therapy accounts for whole cases of interrupting drug administration (amounts to 228 and accept the inpatients studied) to the untoward reaction of these medicines, 77-82,1999).

Especially, by the liver toxicity that Rimactazid and Tibutol brought out of uniting 5 kinds of medicines that are used for above-mentioned first-line treatment, known is the untoward reaction of frequent formation.Meanwhile, tolerance antitubercular agent Mycobacterium tuberculosis, be multidrug-resisting Mycobacterium tuberculosisDeng increasing always, these Mycobacterium tuberculosisThe existence of type makes treatment difficulty more.

According to the research (1996 to 1999) that WHO did, tolerate any existing antitubercular agent in the world Mycobacterium tuberculosisAccount for separated all Mycobacterium tuberculosisThe ratio of type reaches 19%, and has announced the multiple medicines tolerance Mycobacterium tuberculosisRatio be 5.1%.By this class multidrug-resisting Mycobacterium tuberculosisThe amount vector that infects is 60,000,000 according to estimates, for multidrug-resisting Mycobacterium tuberculosisThe following worry that will increase rise (April calendar year 2001, tuberculosis supplementary issue, the " Scientific Blueprint for TB Drug Development. ")

In addition, AIDS patient's major causes of death is a tuberculosis.Reported that the number of suffering from tuberculosis and HIV simultaneously reached 10,700,000 (Global Alliance for TBdrug development) in 1997.And, it is believed that the polyinfection of tuberculosis and HIV develops into danger lungy than at least 30 times of general case height.

In view of above-mentioned current situation, the profile of required antitubercular agent is as follows: (1) is even to multidrug-resisting Mycobacterium tuberculosisAlso be that effectively (2) make short-course chemotherapy become possibility, (3) have untoward reaction still less, and (4) are to latent infection Mycobacterium tuberculosis(latent just Tuberculosis branch bar Bacterium) demonstration effect and (5) Orally-administrable.

Known have the intruding into property bacterium that pathogenic bacterium example comprises the MAC infection (mycobacterium tuberculosis multiplicity of infection in bird type-cell) that increases day by day to the mankind, for example Mycobacterium aviumWith Cell Mycobacterium intracellulareAnd the atypia acid-fast bacterium, for example Mycobacterium kansasii, Mycobacterium scrofulaceum( Mycobacterium Marinum), Mycobacterium habana, Mycobacterium scrofulaceum( Mycobacterium Scrofulaceum), The Si Shi mycobacterium, Mycobacterium littorale, The Ma Ermo mycobacterium, Bloodthirsty branch The branch bacillus, Mycobacterium buruli, The Shi Shi mycobacterium, Mycobacterium fortutitum, Mycobacterium chelonei, M. smegmaticsWith Golden mycobacterium

Nowadays, seldom there is therapeutical agent that these atypia acid-fast bacteriums are infected effectively.Can unite use antitubercular agent, macrolide antibiotic, aminoglycoside antibiotics and tetracycline antibiotic under the environment at present, described antitubercular agent is Rimactazid, Tibutol, Streptomycin sulphate and kantlex for example, and the latter is a kind of new quinolones common bacteria treatment of infection agent.

But, compare with the common bacteria treatment of infection, the treatment that the atypia acid-fast bacterium infects requires long-term drug administration, and has reported that infection hardened the neck, finally causes death cases.In order to break through above-mentioned current situation, the medicine that needs exploitation to have stronger effect.

For example, the country of international patent application announces that No.11-508270 (WO97/01562) discloses 6-nitro-1,2,3, and 4-tetrahydrochysene [2,1-b] imidazo pyrylium compound is right Mycobacterium tuberculosis(H37Rv bacterial strain) and multidrug-resisting Mycobacterium tuberculosisHave the extracorporeal disinfecting effect, and above-claimed cpd has result of treatment to infecting animal model lungy when oral administration, thereby can be used as antitubercular agent.

But, the compound described in the above-mentioned publication is different from The compounds of this invention on basic framework, is considered to and the The compounds of this invention dissmilarity.

People such as Kuppsuwamy Nagara jan are at European Journal of MedicinalChemistry, and 1989, Vol.24, reported the compound by following general formula (I) representative among the pp.631-633:

R wherein ¹Represent hydrogen atom or methyl ,-(CH ₂) _nR ²Represent chloromethyl, C1-C7 alkyl, isopropoxy methyl, 3-propenyloxy group methyl or unsubstituted phenoxy methyl,

With the compound by above-mentioned same general formula (I) representative, wherein R ¹With-(CH ₂) _nR ²Being bonded to each other constitutes pentamethylene or cyclohexane ring (amounting to 16 kinds of types of compounds),

Right Mycobacterium tuberculosis(H37Rv bacterial strain) has germicidal action.

But, above-mentioned publication has been described above-claimed cpd to have only 4 kinds of types of compounds when oral administration has been effective.It also described have the most highly active compound, just by the compound (CGI-17341) of above-mentioned general formula (I) representative (R wherein ¹Represent hydrogen atom ,-(CH ₂) _nR ²Represent ethyl) be found and have mutagenicity, therefore abandoned of the exploitation of these series of compounds as medicine.

In addition, people such as Dilip R.Astekar are at Antimicrobial Agents andChemotherapy, and Feb.1993 reported the antimicrobial behavior of above-claimed cpd CGI-17341 among the pp.183-186.According to this report, Compound C GI-17341 is when in 250 μ g/ml or following use, and is right Mycobacterium tuberculosis(H37Rv bacterial strain) and multidrug-resisting Mycobacterium tuberculosisHave germicidal action, but atypia acid-fast bacterium mycobacterium avium, mycobacterium intracellulare and mycobacterium fortutitum are not had activity.

And, Journal of Medicinal Chemistry, 1981, Vol.24, pp.601-604 disclose 6-nitro-2, and 3-glyoxalidine also [2,1-b] _ azole compounds has the radiation sensitizability to the hypoxemia mammalian cell.

Disclosure of an invention

It is right to the purpose of this invention is to provide Mycobacterium tuberculosisWith multidrug-resisting Mycobacterium tuberculosisCompound with excellent germicidal action.

Another object of the present invention provides the compound that the atypia acid-fast bacterium is had excellent germicidal action.

As the result of further investigation, the inventor has successfully synthesized 2 of novelty, and the 3-glyoxalidine is [2,1-b] _ azole compounds also, and it is right Mycobacterium tuberculosis, multidrug-resisting Tuberculosis branch bar BacteriumHas excellent germicidal action with the atypia acid-fast bacterium.Based on such discovery, finished the present invention.

The invention provides by 2 of following general formula (I) representative, 3-dihydro-6-nitroimidazole is [2,1-b] _ azole compounds, its optically active form or its pharmacy acceptable salt also:

R wherein ¹Represent hydrogen atom or C1-C6 alkyl,

N represents the integer between 0 and 6,

R ¹With-(CH ₂) _nR ²Can be each other with they adjacent carbon atom combination, constitute volution by general formula (30) representative:

Wherein RRR represents piperidyl [wherein on this piperidine ring, can be substituted with at least one phenoxy group (wherein on this benzyl ring, can be substituted with at least one and be selected from following group: halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed)]

R ²Represent any one described group in following (a) to (y):

(a) phenyl is (wherein on this benzyl ring, can be substituted with at least one piperidyl [wherein on this piperidine ring, can be substituted with at least one phenoxy group (wherein on this benzyl ring, can be substituted with at least one and be selected from the group that following group halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and halogen replacement or unsubstituted C1-C6 alkoxyl group are formed)]);

(b) benzothiazole oxygen base (wherein on this benzothiazole ring, can be substituted with the group that at least one is selected from the group of being made up of following (b-1) to (b-5):

(b-1) phenyl [wherein on this benzyl ring, can be substituted with at least one and be selected from following group: halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed],

(b-2) piperazinyl is [wherein on this piperazine ring, can be substituted with at least one group, it is selected from by phenyl C1-C6 alkyl (wherein on this phenyl, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed), phenyl C2-C6 thiazolinyl is (wherein on this phenyl, can be substituted with at least one group, it is selected from by halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group) and phenyl (wherein on this phenyl, can be substituted with at least one group, it is selected from by halogen atom, the group that halogen replacement or unsubstituted C1-C6 alkyl and halogen replacement or unsubstituted C1-C6 alkoxyl group are formed) group of forming]

(b-3) piperidyl is [wherein on this piperidine ring, can be substituted with at least one group, it is selected from by amino (wherein on this amino, can be substituted with at least one group, it is selected from by phenyl [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group] and the group of C1-C6 alkyl composition), phenoxy group is (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group) and phenyl C1-C6 alkyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, the group that halogen replacement or unsubstituted C1-C6 alkyl and halogen replacement or unsubstituted C1-C6 alkoxyl group are formed) group of forming]

(b-4) pyrryl is [wherein on this pyrrole ring, can be substituted with at least one group, it is selected from by C1-C6 alkyl and phenyl C1-C6 alkyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group) group formed]

(b-5) thiophenyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group));

(c) quinoline oxy (wherein on this quinoline ring, can be substituted with the group that at least one is selected from the group of being made up of following (c-1) to (c-4):

(c-1) halogen atom,

(c-2) phenoxy group [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group],

(c-3) piperazinyl is [wherein on this piperazine ring, can be substituted with at least one group, it is selected from by phenyl C1-C6 alkyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed), phenyl is [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by phenoxy group (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed), halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group] and phenyl C2-C6 thiazolinyl [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group] group formed]

(c-4) piperidyl is [wherein on this piperidine ring, can be substituted with the group that at least one is selected from following groups: amino (wherein on this amino, can be substituted with at least one group, it is selected from by phenyl [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group] and the group formed of C1-C6 alkyl); Phenoxy group (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group); Phenyl C1-C6 alkyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by C1-C4 alkylene dioxo base, halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group); Phenyl C1-C6 alkoxyl group (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group); Phenyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group); Naphthyl C1-C6 alkyl; With phenyl C1-C6 alkylidene group (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group)]);

(d) pyridyloxy (wherein on this pyridine ring, can be substituted with at least one and be selected from group by following (d-1) and the group (d-2) formed:

(d-1) piperidyl is [wherein on this piperidine ring, can be substituted with at least one group, it is selected from by phenoxy group (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed), the C1-C6 alkyl that phenyl C1-C6 alkoxyl group replaces is (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed), phenoxy group C1-C6 alkyl is (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group) and phenyl C1-C6 alkyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, the group that halogen replacement or unsubstituted C1-C6 alkyl and halogen replacement or unsubstituted C1-C6 alkoxyl group are formed) group of forming];

(d-2) piperazinyl is [wherein on this piperazine ring, can be substituted with at least one group, it is selected from the alkoxy carbonyl by C1-C6, furyl C1-C6 alkyl is [wherein on this furan nucleus, can be substituted with at least one phenyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed)], pyridyl C1-C6 alkyl is [wherein on this pyridine ring, can be substituted with at least one group, it is selected from the group be made up of furyl and phenyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed)], benzothienyl C1-C6 alkyl is (wherein on this thionaphthene ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed), phenyl C2-C6 thiazolinyl is (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed), benzofuryl C1-C6 alkyl is [wherein on this cumarone ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed], benzofuryl C2-C6 thiazolinyl is [wherein on this cumarone ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed], thiazolyl C1-C6 alkyl is [wherein on this thiazole ring, can be substituted with at least one phenyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed)], phenoxy group C1-C6 alkyl is (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed), indyl C1-C6 alkyl is (wherein on this indole ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group) and phenyl C1-C6 alkyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by benzofuryl, halogen atom, the group that halogen replacement or unsubstituted C1-C6 alkyl and halogen replacement or unsubstituted C1-C6 alkoxyl group are formed) group of forming]);

(e) 1,2,3,4-tetrahydroquinoline oxygen base (wherein this 1,2,3, on the 4-tetrahydroquinoline ring, can be substituted with at least one group, it is selected from by the oxo base, [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom phenyl, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group] and phenyl C1-C6 alkyl [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group] group formed);

(f) 1,2,3,4-tetrahydrochysene naphthyloxy (wherein this 1,2,3, on the 4-tetrahydric naphthalene ring, can be substituted with at least one oxo base);

(g) 2H-chromene oxygen base (wherein on this 2H-chromene ring, can be substituted with at least one oxo base);

(h) naphthyloxy is (wherein on this naphthalene nucleus, can be substituted with at least one piperidyl [wherein on this piperidine ring, can be substituted with at least one phenoxy group (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group)]);

(i) 1,2,3,4-tetrahydroisoquinoline oxygen base (wherein this 1,2,3, on the 4-tetrahydroisoquinoline ring, can be substituted with at least one group, it is selected from the alkoxy carbonyl by C1-C6, [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom phenyl C1-C6 alkyl, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group] and phenyl [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group] group formed);

(j) group-NR ²²R ²³(R wherein ²²Represent hydrogen atom or C1-C6 alkyl, R ²³Represent at least one to be selected from following (j-1) group to (j-5):

(j-1) phenyl is [wherein on this benzyl ring, be substituted with at least one piperidyl (wherein on this piperidine ring, can be substituted with at least one phenoxy group [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group])]

(j-2) phenyl C1-C6 alkyl is [wherein on this benzyl ring, be substituted with at least one group, it is selected from by piperidyl (wherein on this piperidine ring, be substituted with phenoxy group [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group]) and group-NR ²⁴R ²⁵(R wherein ²⁴Represent hydrogen atom or C1-C6 alkyl, R ²⁵Represent phenyl C2-C6 thiazolinyl [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group]) group formed],

(j-3) piperidyl C1-C6 alkyl is [wherein on this piperidine ring, be substituted with at least one phenyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group)]

(j-4) thiazolyl is [wherein on this thiazole ring, can be substituted with at least one group, it is selected from by phenyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed), piperazinyl C1-C6 alkyl is (wherein on this piperazine ring, can be substituted with at least one phenyl [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group]) and piperidyl C1-C6 alkyl (wherein on this piperidine ring, can be substituted with at least one phenoxy group [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group]) group formed]

(j-5) phenyl C2-C6 thiazolinyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group));

(k) benzo _ azoles oxygen base is (wherein on this benzo _ azoles ring, can be substituted with at least one group, it is selected from by piperazinyl [wherein on this piperazine ring, can be substituted with at least one group, it is selected from by phenyl C1-C6 alkyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group) and phenyl C2-C6 thiazolinyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, the group that halogen replacement or unsubstituted C1-C6 alkyl and halogen replacement or unsubstituted C1-C6 alkoxyl group are formed) group of forming], piperidyl is (wherein on this piperidine ring, can be substituted with at least one group, it is selected from by phenyl C1-C6 alkyl [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed] and amino [wherein on this amino, can be substituted with at least one group, it is selected from by C1-C6 alkyl and phenyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group) group formed] group formed) and phenyl [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group] group formed);

(l) benzoglyoxaline oxygen base is (wherein on this benzoglyoxaline ring, can be substituted with at least one group, it is selected from the alkyl by C1-C6, phenyl is [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed], piperidyl is [wherein on this piperidine ring, can be substituted with at least one phenoxy group (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, the group that halogen replacement or unsubstituted C1-C6 alkyl and halogen replacement or unsubstituted C1-C6 alkoxyl group are formed) group of forming], piperazinyl is [wherein on this piperazine ring, can be substituted with at least one phenyl C1-C6 alkyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group) group formed] and phenyl C1-C6 alkyl [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group] group formed);

(m) 1,2,3, the 4-tetrahydro isoquinolyl (wherein this 1,2,3, on the 4-tetrahydroisoquinoline ring, can be substituted with at least one and be selected from group by following (m-1) and the group (m-2) formed:

(m-1) amino [wherein on this amino, can be substituted with at least one group, it is selected from the alkyl by C1-C6, phenyl is (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group) and phenyl C1-C6 alkyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, the group that halogen replacement or unsubstituted C1-C6 alkyl and halogen replacement or unsubstituted C1-C6 alkoxyl group are formed) group of forming]

(m-2) phenoxy group [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group]);

(n) piperidyl (wherein on this piperidine ring, can be substituted with the group that at least one is selected from the group of being made up of following (n-1) to (n-4):

(n-1) phenyl [wherein on this benzyl ring, is substituted with at least one group-NR ²⁶R ²⁷(R wherein ²⁶Represent hydrogen atom or C1-C6 alkyl, R ²⁷Represent phenyl [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group])],

(n-2) group-W ₁NR ²⁸R ²⁹[W wherein ₁Represent the C1-C6 alkylidene group, R ²⁸Represent hydrogen atom or C1-C6 alkyl, R ²⁹Represent phenyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group)],

(n-3) C1-C6 alkoxyl group, wherein be substituted with two phenyl [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group]

(n-4) phenyl C1-C6 alkyl is [wherein on this benzyl ring, be substituted with at least one phenyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group)]);

(o) piperazinyl is (wherein on this piperazine ring, be substituted with the group that at least one is selected from following groups: the C1-C6 alkyl that wherein is substituted with two phenyl is [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed], phenyl C1-C6 alkyl is [wherein on this benzyl ring, be substituted with at least one phenoxy group (wherein on this benzyl ring, be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed)], thiazolyl is (wherein on this thiazole ring, can be substituted with at least one phenyl), phenoxy group C1-C6 alkyl is (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by phenyl (wherein on this benzyl ring, can be substituted with halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replacement or unsubstituted C1-C6 alkoxyl group), halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed), phenyl C2-C6 thiazolinyl is [wherein on this benzyl ring, be substituted with at least one group, it is selected from by halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group] and imidazolyl [wherein on this imidazole ring, can be substituted with at least one phenyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed)]);

(p) thiazolyl C1-C6 alkoxyl group (wherein on this thiazole ring, can be substituted with at least a types of radicals that is selected from the group of forming by following (p-1) to (p-5):

(p-1) phenoxy group C1-C6 alkyl [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group],

(p-2) phenylamino C1-C6 alkyl [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group],

(p-3) phenyl C1-C6 alkyl [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group],

(p-4) piperazinyl C1-C6 alkyl is [wherein on this piperazine ring, can be substituted with at least one phenyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group)]

(p-5) piperidyl C1-C6 alkyl is [wherein on this piperidine ring, can be substituted with at least one phenoxy group (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group)]);

(q) 8-azabicyclic [3.2.1] octyl group is (wherein on this 8-azabicyclic [3.2.1] octane ring, can be substituted with at least one phenoxy group [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group]);

(r) group of representing by following chemical formula (31):

[wherein X represents halogen atom, the perhaps amino C1-C6 alkyl that replaces, and it can have the C1-C6 alkyl as substituting group, and m represents the integer between 0 and 3, R ³Represent any one described group in following (i) to (xxii):

(i) o-NR of group-(W) ⁴R ⁵

(wherein W representative-CO-or C1-C6 alkylidene group, o represents 0 or 1, R ⁴Represent hydrogen atom, C1-C6 alkyl or phenyl carbamyl [wherein on this benzyl ring; can be substituted with at least one group; it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group], R ⁵Representative: phenyl C1-C6 alkoxy carbonyl [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group]; Phenyl C2-C6 alkenyl carbonyl [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group]; Phenyl C2-C6 thiazolinyl [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group]; Piperidyl C1-C6 alkyl is [wherein on this piperidine ring, can be substituted with at least one phenyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group)]; Phenyl C1-C6 alkyl is (wherein on this benzyl ring, be substituted with at least one phenyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group)); Benzofuryl C1-C6 alkyl (wherein on this cumarone ring, can be substituted with at least one halogen and replace or unsubstituted C1-C6 alkyl); Piperidino carbonyl C1-C6 alkyl is [wherein on this piperidine ring, can be substituted with at least one phenoxy group (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group); Perhaps by the group of following chemical formula (32) representative:

R wherein ⁶Representative: C1-C6 alkyl; Phenyl is (wherein on this benzyl ring, can be substituted with the group that at least one is selected from following groups: the C1-C4 alkylene dioxo base, cyano group, nitro, can have the C1-C6 alkyl as substituent amino, can have the C1-C6 alkyl as the substituent amino alkylsulfonyl that replaces, the C1-C6 alkoxy carbonyl, the C1-C6 alkylthio, phenoxy group, phenyl C1-C6 alkoxyl group, pyrrolidyl [wherein on this pyrrolidine ring, can be substituted with at least one oxo base], imidazolyl, different _ the azoles base, _ azoles base, phenyl C1-C6 alkyl, phenyl, can have the C1-C6 alkyl as substituent amino C1-C6 alkyl, pyrrolidyl C1-C6 alkoxyl group, halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replacement or unsubstituted C1-C6 alkoxyl group); Phenyl C1-C6 alkoxy carbonyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group); Benzofuryl C1-C6 alkyl (wherein on this cumarone ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group); Benzofuryl C2-C6 thiazolinyl (wherein on this cumarone ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group); Phenoxy group C1-C6 alkyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group); Thiazolyl C1-C6 alkyl is (wherein on this thiazole ring, can be substituted with at least one phenyl [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group]); Phenyl C1-C6 alkyl is [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by phenyl (wherein on this benzyl ring, can be substituted with halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and halogen and replace or unsubstituted C1-C6 alkoxyl group), halogen atom, halogen replaces or the group of unsubstituted C1-C6 alkyl and halogen replacement or unsubstituted C1-C6 alkoxyl group composition]; Pyridyl C1-C6 alkyl is [wherein on this pyridine ring, can be substituted with at least one phenyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group)]; The C1-C6 alkoxy carbonyl; Benzoyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group); Phenylamino formyl radical (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group); Benzothienyl C1-C6 alkyl (wherein on this thionaphthene ring, can be substituted with at least one halogen atom); Indyl C1-C6 alkyl (wherein on this indole ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group); 4H-1,3-benzo two _ Ying Ji (, on 3-benzo two _ English (benzodioxine) ring, can be substituted with at least one halogen atom) wherein at this 4H-1; Benzothienyl; Naphthyl; Quinolyl; Benzothiazolyl (wherein on this benzothiazole ring, can be substituted with at least one C1-C6 alkyl); 2,3-dihydro-1H-indenyl (wherein this 2, on 3-dihydro-1H-indenes ring, can be substituted with at least one oxo base); Perhaps 9H-fluorenyl or phenyl C2-C6 thiazolinyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group));

(ii) by the group of following chemical formula (33) representative:

(wherein W and o are same as described above, and it can be two keys that dotted line is represented this key, when the two key of dotted line representative, this means and have only R ⁸Be substituted; R ⁷Represent hydrogen atom, hydroxyl, C1-C6 alkoxyl group or phenyl [wherein on this benzyl ring, can be substituted with halogen]; R ⁸Represent any one described group in following (1) to (63):

(1) the C1-C6 alkyl of phenyl C1-C6 alkoxyl group replacement is (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by C1-C4 alkylene dioxo base, halogen atom, cyano group, phenyl, phenyl C1-C6 alkoxyl group, phenyl C2-C6 thiazolinyl, phenoxy group, C1-C6 alkylthio, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group);

(2) phenyl C1-C6 alkoxyl group is (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by cyano group, phenyl, C1-C6 alkoxy carbonyl, phenoxy group, C1-C6 alkylthio, halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group);

(3) phenyl C2-C6 alkene oxygen base (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group);

(4) o-NR of group-(W) ⁹R ¹⁰

(wherein W and o are same as described above, and

R ⁹And R ¹⁰Represent: hydrogen atom separately identical or differently; Can have hydroxyl as substituent C1-C6 alkyl; The C1-C6 alkyloyl; The C1-C6 alkoxy carbonyl; Phenyl C1-C6 alkoxy carbonyl [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group]; Phenyl is [on this benzyl ring; can be substituted with at least one and be selected from down group in the group as substituting group: halogen atom; halogen replaces or unsubstituted C1-C6 alkyl; halogen replaces or unsubstituted C1-C6 alkoxyl group; can have the group that is selected from C1-C6 alkyloyl and the C1-C6 alkyl as substituent amino; the C1-C6 alkoxy carbonyl; phenyl; phenoxy group is (wherein on this benzyl ring; can be substituted with at least one group; it is selected from by halogen atom; halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed); amino-sulfonyl; 1; 2; 3; the 4-tetrahydric quinoline group (wherein this 1; 2; 3; on the 4-tetrahydroquinoline ring; can be substituted with at least one oxo base as substituting group); the C1-C6 alkyl sulphonyl; the C3-C8 cycloalkyl; nitro; cyano group; the C1-C6 alkylthio; benzenesulfonyl is (wherein on this benzyl ring; can be substituted with at least one group, it is selected from by halogen atom; halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed); C1-C6 alkyl that hydroxyl replaces and the group of representing by following chemical formula (34):

(W wherein ₁Represent the C1-C6 alkylidene group, R ¹¹And R ¹²Represent the C1-C6 alkoxyl group separately identical or differently)]; Phenyl C1-C6 alkyl is [wherein on this benzyl ring, can be substituted with at least one and be selected from following group as substituting group: C1-C4 alkylene dioxo base, phenyl are (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group), group-N (R ^11A) R ^12A(R wherein ^11AAnd R ^12ARepresent hydrogen atom, C1-C6 alkyl or phenyl, R separately identical or differently ^11AAnd R ^12ACan be each other with their direct neighbors or pass through nitrogen, the nitrogen-atoms combination together that oxygen or sulphur atom are adjacent, constitute 5-7 unit saturated heterocyclic), phenoxy group is (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed), phenyl C1-C6 alkoxyl group, can have the C1-C6 alkyl as the substituent amino C1-C6 alkoxyl group that replaces, halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C10 alkoxyl group is formed]; Benzofuryl C1-C6 alkyl [wherein on this cumarone ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group]; Benzenesulfonyl [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replacement or unsubstituted C1-C6 alkoxyl group, and the group of C1-C4 alkylene dioxo base composition]; Phenyloxycarbonyl [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group]; Phenyl C2-C6 thiazolinyl [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group]; The C1-C6 alkyl that the C1-C6 alkoxyl group replaces; The C2-C6 thiazolinyl; The C2-C6 alkyloyl that the C1-C6 alkoxyl group replaces; The C1-C6 alkyl of C3-C8 cycloalkyl substituted; Phenoxy group C1-C6 alkyl [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group]; Benzoyl [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group]; Phenylamino formyl radical [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group]; Pyridyl; Pyridyl C1-C6 alkyl; Imidazolyl C1-C6 alkyl; 1,2,3, the 4-tetrahydric quinoline group [wherein this 1,2,3, on the 4-tetrahydroquinoline ring, can be substituted with at least one group as substituting group, it is selected from the group of being made up of oxo base and C1-C6 alkyl]; Quinolyl; Indyl; Can have the C1-C6 alkyl as substituent amino; Indazolyl; Naphthyl; The C3-C8 cycloalkyl; Can have the C1-C6 alkyl as the substituent amino C1-C6 alkyl that replaces; The C1-C6 alkyl that cyano group replaces; The C1-C6 alkyl that furyl replaces; Formula (35) group

(wherein RR represents phenyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group)); Perhaps the C1-C6 alkyl of piperazinyl replacement is [wherein on this piperazine ring, can be substituted with at least one phenyl as substituting group (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group)]

And then, R ⁹And R ¹⁰Can be each other with their direct neighbors or pass through nitrogen, the nitrogen-atoms combination together that oxygen or sulphur atom are adjacent, constitute 1,2,3, the 4-tetrahydro isoquinolyl, pseudoindoyl or 5-7 unit saturated heterocyclic, wherein on this heterocycle, can be substituted with at least one and be selected from group in the following groups: halogen atom, halogen replaces or unsubstituted C1-C6 alkyl, halogen replaces or unsubstituted C1-C6 alkoxyl group, phenyl is [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by phenyl, halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed], benzoyl is [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed], pyridyl C1-C6 alkyl, the C3-C8 cycloalkyl, phenyl C1-C6 alkyl is [wherein on this benzyl ring, can be substituted with at least one group, it is selected from the alkylene dioxo base by C1-C4, halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed], piperidyl C1-C6 alkyl, piperidyl, phenyl C1-C6 alkoxyl group is [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed], phenoxy group is [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed], amino (wherein can be substituted with at least one group as substituting group, it is selected from by phenyl [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed], C1-C6 alkyl and phenyl C1-C6 alkyl are [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group] group formed), benzo _ azoles base, phenyl C2-C6 thiazolinyl is (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed) and benzimidazolyl-);

(5) phenyl C1-C6 alkyl is (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, phenyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group), halogen replaces or unsubstituted C1-C6 alkyl and halogen replacement or unsubstituted C1-C6 alkoxyl group are formed group);

(6) carbamoyloxy group is (wherein on this amino, can be substituted with at least one group, it is selected from by C1-C6 alkyl and phenyl [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group] group formed);

(7) the C1-C6 alkyl of carbamoyloxy group replacement is (wherein on this amino, can be substituted with at least one group, it is selected from the alkyl by C1-C6, phenyl C1-C6 alkyl, the C3-C8 cycloalkyl, naphthyl, 2,3-dihydro-1H-indenyl, 2,3-dihydro benzo furyl and phenyl are [wherein on this benzyl ring, can be substituted with at least one group, it is selected from the alkylene dioxo base by C1-C4, cyano group, phenoxy group, the C1-C6 alkylthio, the C1-C6 alkyloyl, phenyl, phenyl C1-C6 alkyl, halogen atom, halogen replaces or unsubstituted C1-C10 alkyl and halogen replaces or unsubstituted C1-C10 alkoxyl group is formed group] group formed);

(8) phenoxy group C1-C6 alkyl (wherein on this benzyl ring, can be substituted with the group that at least one is selected from following groups: halogen atom; The C1-C4 alkylene dioxo base; The C1-C6 alkoxy carbonyl; Phenyl; Phenoxy group; Pyrryl; Benzothiazolyl; 1,2, the 4-triazolyl; Imidazolyl; Different _ the azoles base; Benzo _ azoles base; The benzotriazole base; Cyano group; Nitro; The C2-C6 thiazolinyl; The C1-C6 alkyloyl; The C1-C6 alkyl that the C1-C6 alkoxy carbonyl replaces; The C1-C6 alkyl that the C1-C6 alkyloyl replaces; Group-N (R ^11B) R ^12B(R wherein ^11BAnd R ^12BRepresent hydrogen atom, C1-C6 alkyl, C1-C6 alkyloyl or phenyl, R separately identical or differently ^11BAnd R ^12BCan be each other with their direct neighbors or pass through nitrogen, the nitrogen-atoms combination together that oxygen or sulphur atom are adjacent, constitute 5-7 unit saturated heterocyclic, wherein on this heterocycle, can be substituted with at least one group, it is selected from by C1-C6 alkoxy carbonyl and amino [wherein on this amino, can be substituted with at least one and be selected from phenyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group) and the group of C1-C6 alkyl] group of composition); Phenyl C1-C6 alkoxyl group; Phenyl C1-C6 alkyl; The C1-C6 alkylthio; The C3-C8 cycloalkyl; Halogen replaces or unsubstituted C1-C6 alkyl; Replace or unsubstituted C1-C10 alkoxyl group with halogen);

(9) tetrahydro-pyran oxy C1-C6 alkyl;

(10) the C1-C6 alkyl of hydroxyl replacement;

(11) the C1-C6 alkyl (wherein on this furan nucleus, can be substituted with at least one C1-C6 alkoxy carbonyl) of furyl C1-C6 alkoxyl group replacement;

(12) the C1-C6 alkyl of tetrazyl C1-C6 alkoxyl group replacement is (wherein on this tetrazole ring, can be substituted with at least one group, it is selected from by phenyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group), the group formed of phenyl C1-C6 alkyl and C3-C8 cycloalkyl C1-C6 alkyl);

(13) the C1-C6 alkyl (wherein on this different _ azoles ring, can be substituted with at least one C1-C6 alkyl) of different _ azoles base C1-C6 alkoxyl group replacement;

(14) the C1-C6 alkyl of benzothienyl C1-C6 alkoxyl group replacement is (wherein on this thionaphthene ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group);

(15) 1,3, the C1-C6 alkyl that 4-_ di azoly C1-C6 alkoxyl group replaces (wherein this 1,3, on the 4-_ diazole ring, can be substituted with phenyl [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group]);

(16) the C1-C6 alkyl of C2-C6 alkynyloxy group replacement;

(17) the C1-C6 alkyl of naphthyl C1-C6 alkoxyl group replacement;

(18) 1,2, the C1-C6 alkyl that 4-_ di azoly C1-C6 alkoxyl group replaces [wherein this 1,2, on the 4-_ diazole ring, can be substituted with phenyl];

(19) the C1-C6 alkyl of pyridyl C1-C6 alkoxyl group replacement is [wherein on this pyridine ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group];

(20) the C1-C6 alkyl of thiazolyl C1-C6 alkoxyl group replacement is [wherein on this thiazole ring, can be substituted with at least one group, it is selected from by phenyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group) and the group formed of C1-C6 alkyl];

(21) 1,2,3, the C1-C6 alkyl that 4-tetralyl C1-C6 alkoxyl group replaces [wherein this 1,2,3, on the 4-tetrahydric naphthalene ring, can be substituted with at least one C1-C6 alkyl];

(22) the C1-C6 alkyl of carbamyl C1-C6 alkoxyl group replacement is [wherein on this amino, can be substituted with at least one group, it is selected from by C3-C8 cycloalkyl and phenyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group) group formed];

(23) the C1-C6 alkyl [wherein on this cumarone ring, can be substituted with at least one cyano group] of benzofuryl C1-C6 alkoxyl group replacement;

(24) benzofuryl C1-C6 alkyl [wherein on this cumarone ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group];

(25) phenoxy group [wherein on this benzyl ring, be substituted with at least one group, it is selected from the group of being made up of phenyl C1-C6 alkoxyl group, C3-C8 cycloalkyl, C7-C10 alkoxyl group and phenoxy group];

(26) naphthyloxy;

(27) 2,3-Dihydrobenzofuranes oxygen bases [wherein this 2, on the 3-Dihydrobenzofuranes ring, can be substituted with at least one oxo base];

(28) benzothiazolyl oxygen base [wherein on this benzothiazole ring, can be substituted with at least one C1-C6 alkyl];

(29) 1,2,3,4-tetrahydrochysene naphthyloxy [wherein this 1,2,3, on the 4-tetrahydric naphthalene ring, can be substituted with at least one oxo base];

(30) diphenylene-oxide oxygen base;

(31) quinoline oxy;

(32) furyl C1-C6 alkoxyl group [wherein on this furan nucleus, can be substituted with at least one C1-C6 alkoxy carbonyl];

(33) tetrazyl C1-C6 alkoxyl group [wherein on this tetrazole ring, can be substituted with at least one group, it is selected from the group of being made up of phenyl C1-C6 alkyl and C3-C8 cycloalkyl C1-C6 alkyl];

(34) 1,2,4-_ di azoly C1-C6 alkoxyl group [wherein this 1,2, on the 4-_ diazole ring, can be substituted with phenyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group)];

(35) benzothienyl C1-C6 alkoxyl group [wherein on this thionaphthene ring, can be substituted with at least one halogen atom];

(36) different _ azoles base C1-C6 alkoxyl group [wherein on this different _ azoles ring, can be substituted with at least one C1-C6 alkyl];

(37) 1,3,4-_ di azoly C1-C6 alkoxyl group [wherein this 1,3, on the 4-_ diazole ring, can be substituted with at least one phenyl (wherein on this benzyl ring, can be substituted with at least one C1-C6 alkyl)];

(38) naphthyl C1-C6 alkoxyl group;

(39) pyridyl C1-C6 alkoxyl group (wherein on this pyridine ring, can be substituted with at least one halogen and replace or unsubstituted C1-C6 alkyl);

(40) thiazolyl C1-C6 alkoxyl group is [wherein on this thiazole ring, can be substituted with at least one phenyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group)];

(41) 1,2,3,4-tetralyl C1-C6 alkoxyl group (wherein this 1,2,3, on the 4-tetrahydric naphthalene ring, can be substituted with at least one C1-C6 alkyl);

(42) phenoxy group C1-C6 alkoxyl group (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group);

(43) carbamyl C1-C6 alkoxyl group is [wherein on this amino, can be substituted with at least one group, it is selected from by C3-C8 cycloalkyl and phenyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group) group formed];

(44) benzofuryl C1-C6 alkoxyl group (wherein on this cumarone ring, can be substituted with at least one cyano group);

(45) naphthyloxy C1-C6 alkyl (wherein on this naphthalene nucleus, can be substituted with at least one C1-C6 alkoxyl group);

(46) benzothiazole oxygen base C1-C6 alkyl (wherein on this benzothiazole ring, can be substituted with at least one C1-C6 alkyl);

(47) quinoline oxy C1-C6 alkyl (wherein on this quinoline ring, can be substituted with at least one C1-C6 alkyl);

(48) 2,3-Dihydrobenzofuranes oxygen base C1-C6 alkyl (wherein this 2, on the 3-Dihydrobenzofuranes ring, can be substituted with at least one group, it is selected from the group of being made up of C1-C6 alkyl and oxo base);

(49) 1,2,3,4-tetrahydrochysene naphthyloxy C1-C6 alkyl (wherein this 1,2,3, on the 4-tetrahydric naphthalene ring, can be substituted with at least one oxo base);

(50) 2,3-dihydro-1H-indenes oxygen base C1-C6 alkyl (wherein this 2, on 3-dihydro-1H-indenes ring, can be substituted with at least one oxo base);

(51) benzo oxathiolane oxygen base C1-C6 alkyl (wherein on this benzo oxathiolane (benzoxathiolane) ring, can be substituted with at least one oxo base);

(52) isoquinoline 99.9 oxygen base C1-C6 alkyl;

(53) pyridyloxy C1-C6 alkyl;

(54) diphenylene-oxide oxygen base C1-C6 alkyl;

(55) 2H-1-chromene oxygen base C1-C6 alkyl (wherein on this 2H-1-chromene ring, can be substituted with at least one oxo base);

(56) benzisoxa _ azoles oxygen base C1-C6 alkyl;

(57) benzo furazan oxygen base (benzofurazanyloxy) C1-C6 alkyl;

(58) quinoxaline oxygen base C1-C6 alkyl;

(59) the C1-C6 alkyl of C1-C6 alkoxy C 1-C6 alkoxyl group replacement;

(60) the C1-C6 alkyl (wherein on this thiphene ring, can be substituted with at least one halogen atom) of thienyl C1-C6 alkoxyl group replacement;

(61) the C1-C6 alkyl of phenyl C2-C6 alkene oxygen base replacement is (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group);

(62) the C1-C6 alkyl of quinolyl C1-C6 alkoxyl group replacement;

(63) the C1-C6 alkyl of piperidino carbonyl C1-C6 alkoxyl group replacement,

And then, R ⁷And R ⁸Can constitute group=C (R together ²⁹) (R ³⁰), R wherein ²⁹And R ³⁰Represent hydrogen atom, C1-C6 alkyl or phenyl [wherein on this benzyl ring separately identical or differently, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group]);

(iii) by the group of following chemical formula (36) representative:

(W wherein ₁Same as described above with o, R ¹³Representative: 2,3-dihydro-1H-indenyl; Benzothienyl; Phenyl C2-C10 thiazolinyl is [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, C1-C4 alkylene dioxo base, C1-C6 alkylthio, benzoyl, cyano group, nitro, C2-C6 alkanoyloxy, can have that the C1-C6 alkyl replaces as substituent amino, hydroxyl, phenyl C1-C6 alkoxyl group, phenoxy group, halogen or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group]; Naphthyl C2-C6 thiazolinyl; Benzofuryl C1-C6 alkyl [wherein on this cumarone ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group]; Benzothienyl C2-C6 thiazolinyl; Benzothiazolyl C2-C6 thiazolinyl [wherein on this benzothiazole ring, can be substituted with at least one C1-C6 alkyl]; Phenyl C1-C6 alkyl is [wherein on this benzyl ring, be substituted with the group that at least one is selected from down group: piperidyl is (on this piperidine ring, can be substituted with at least one phenoxy group [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed]), phenyl is (wherein on this benzyl ring, be substituted with at least one group, it is selected from by halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group) and phenoxy group (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed)]; Phenylbenzene C1-C6 alkyl [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group]; Benzoyl C1-C6 alkyl [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group]; Amino, wherein can be substituted with the group that at least one is selected from following groups: C1-C6 alkyl, C1-C6 alkoxy carbonyl and phenyl C1-C6 alkyl are [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by phenyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group), halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replacement or unsubstituted C1-C6 alkoxyl group are formed group]; Amino C1-C6 alkyl, wherein can be substituted with at least one group, it is selected from by C1-C6 alkyl and phenyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group) group formed; Benzofuryl C2-C6 thiazolinyl [wherein on this cumarone ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group]; Piperidyl is [wherein on this piperidine ring, can be substituted with at least one phenyl C2-C6 thiazolinyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group)]; The C1-C6 alkyl that ferrocene replaces; Indyl C1-C6 alkyl (wherein on this indole ring, can be substituted with at least one halogen atom); Phenyl C2-C6 alkynyl; Phenyl is [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by C1-C4 alkylene dioxo base, phenyl, C1-C6 alkoxy carbonyl, hydroxyl and phenoxy group (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group) group formed]; Benzofuryl [wherein on this cumarone ring, can be substituted with at least one group, it is selected from the group of being made up of halogen atom and C1-C6 alkyl]; Benzothiazole quinoline base [wherein on this benzothiazole quinoline ring, can be substituted with at least one oxo base]; Benzothienyl [wherein on this thionaphthene ring, can be substituted with at least one halogen atom]; Naphthyl; 1,2,3, the 4-tetrahydric quinoline group [wherein this 1,2,3, on the 4-tetrahydroquinoline ring, can be substituted with at least one group, it is selected from the group of being made up of oxo base and C1-C6 alkyl]; Benzisoxa _ azoles base; 2, the 3-dihydro benzo furyl; 1,2-dihydroquinoline base [wherein this 1, on the 2-dihydroquinoline ring, can be substituted with at least one oxo base]; 1,2,3,4-tetrahydro quinazoline base [wherein this 1,2,3, on the 4-tetrahydro quinazoline ring, can be substituted with at least one group, it is selected from the group of being made up of oxo base and C1-C6 alkyl]; The benzocyclohepta base; Phenoxy group C1-C6 alkyl [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group]; The C1-C6 alkyl [wherein on this thionaphthene ring, can be substituted with at least one halogen atom] that benzothienyl replaces; The C1-C6 alkyl of naphthyl substituted (wherein on this naphthalene nucleus, can be substituted with at least one C1-C6 alkoxyl group); The C1-C6 alkyl [wherein on this pyridine ring, can be substituted with at least one halogen atom] that pyridyl replaces; The C1-C6 alkyl [wherein on this furan nucleus, can be substituted with at least one nitro] that furyl replaces; The C1-C6 alkyl [wherein on this thiphene ring, can be substituted with at least one halogen atom] that thienyl replaces; The C1-C6 alkyl that thiazolyl replaces is [wherein on this thiazole ring, can be substituted with at least one group, it is selected from by C1-C6 alkyl and phenyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from the group by halogen atom and halogen replace or unsubstituted C1-C6 alkyl is formed) group formed]; The C1-C6 alkyl [wherein on this tetrazole ring, can be substituted with at least one C1-C6 alkyl] that tetrazyl replaces; The C1-C6 alkyl [wherein on this different _ azoles ring, can be substituted with at least one C1-C6 alkyl] that different _ azoles base replaces; 1,2, the C1-C6 alkyl that the 4-_ di azoly replaces [wherein this 1,2, on the 4-_ diazole ring, can be substituted with at least one phenyl (wherein on this benzyl ring, can be substituted with the C1-C6 alkyl)]; The perhaps C1-C6 alkyl that replaces of benzo furazan base);

(iv) by the group of following chemical formula (37) representative:

(R wherein ¹⁴Representative: phenylamino [wherein on the N-position of this phenylamino, can be substituted with the C1-C6 alkyl, on the benzyl ring of this phenylamino, can be substituted with at least one halogen and replace or unsubstituted C1-C6 alkoxyl group]; Piperidyl is [wherein on this piperidine ring, can be substituted with at least one group, it is selected from by phenoxy group (wherein on this benzyl ring, can be substituted with halogen replaces or unsubstituted C1-C6 alkoxyl group) and amino (wherein on this amino, can be substituted with at least one and be selected from following group as substituting group: C1-C6 alkyl and phenyl are [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group] group formed) group formed]; Piperazinyl is [wherein on this piperazine ring, can be substituted with the group that at least one is selected from down group: the C1-C6 alkoxy carbonyl, phenyl C1-C6 alkyl is (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed), phenyl C2-C6 thiazolinyl is (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group) and benzoyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed)]; Phenyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group); High piperazinyl is [wherein on this high piperazine ring, can be substituted with at least one group, it is selected from by C1-C6 alkoxy carbonyl and phenyl C1-C6 alkyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group) group formed]; Perhaps phenoxy group is [wherein on this benzyl ring, can be substituted with at least one group, it is selected from the group of being made up of the phenyl of halogen replacement or unsubstituted C1-C6 alkoxyl group and phenoxy group replacement (wherein on this benzyl ring, can be substituted with at least one halogen and replace or unsubstituted C1-C6 alkoxyl group)]);

(v) by the group of following chemical formula (38) representative:

(R wherein ¹³Same as described above, it can be two keys that dotted line is represented this key);

(vi) high piperazinyl (wherein on this high piperazine ring, can be substituted with the group that at least one is selected from down group: the C1-C6 alkoxy carbonyl; Phenyl C1-C6 alkyl [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group]; Phenyl [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group]; Phenyl C1-C6 alkoxy carbonyl [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group]; Phenylamino formyl radical [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group]; Phenyl C2-C6 thiazolinyl [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group]; And benzoyl [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group]);

(vii) by the group of following chemical formula (39) representative:

(R wherein ¹⁹Represent the C1-C6 alkoxyl group, R ²⁰Represent phenyl [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group]);

(viii) group-CHR ²⁰R ²¹

(R wherein ²⁰Same as described above, R ²¹Representative can have the C1-C6 alkyl as substituent amino);

(ix) 1,2,3, the 4-tetrahydro isoquinolyl (wherein this 1,2,3, on the 4-tetrahydroisoquinoline ring, can be substituted with at least one amino [wherein on this amino, can be substituted with at least one group, it is selected from the group of being made up of phenyl C1-C6 alkyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group) and C1-C6 alkyl]);

(x) _ the azoles base (wherein this _ the azoles ring on, can be substituted with the group that at least one is selected from down group: phenyl is [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed], C1-C6 alkyl and piperidyl are [wherein on this piperidine ring, can be substituted with at least one phenoxy group (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed)]);

(xi) iso-dihydro-indole-group (wherein on this isoindoline ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group);

(xii) thiazolyl is (wherein on this thiazole ring, can be substituted with the group that at least one is selected from down group: phenoxy group C1-C6 alkyl is [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group]; Phenyl [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group]; Phenyl C1-C6 alkyl [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group]; Group-(W ₁) oNR ³¹R ³²[W wherein ₁Same as described above with o, R ³¹And R ³²Represent hydrogen atom, C1-C6 alkyl, phenyl (wherein on this benzyl ring separately identical or differently, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group) or phenyl C1-C6 alkyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group)]; Piperazinyl is [wherein on this piperazine ring, can be substituted with at least one phenyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group)]; Piperidyl is [wherein on this piperidine ring, can be substituted with at least one group, it is selected from by phenoxy group (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group) and the group formed of phenyl C1-C6 alkyl]; And phenoxy group [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group]);

(xiii) the C1-C6 alkyl of hydroxyl replacement;

(xiv) _ azoles base C1-C6 alkyl [wherein this _ the azoles ring on, can be substituted with at least one phenyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group)];

(xv) different _ azoles base is [wherein on this different _ azoles ring, can be substituted with at least one benzyl ring (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group)];

(xvi) benzo _ azoles base (wherein on this benzo _ azoles ring, can be substituted with at least one halogen atom);

(xvii) thiophenyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group);

(xviii) benzimidazolyl-is [wherein on this benzoglyoxaline ring, can be substituted with at least one group, it is selected from by halogen atom and phenyl C1-C6 alkyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group) group formed];

(xiv) pyrrolidyl is [wherein on this pyrrolidine ring, can be substituted with at least one amino (wherein on this amino, can be substituted with at least one group, it is selected from by C1-C6 alkyl and phenyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group) group formed)];

(xx) benzenesulfonyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group);

(xxi) imidazolyl is [wherein on this imidazole ring, be substituted with at least one phenyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group)];

(xxii) phenyl sulfinyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group)];

(s) imidazolyl (wherein on this imidazole ring, can be substituted with at least one group, it is selected from the group of being made up of halogen atom and nitro);

(t) isoindoline oxygen base is [wherein on this isoindoline ring, can be substituted with the group that at least one is selected from down group: the C1-C6 alkoxy carbonyl, phenyl C1-C6 alkyl is (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by benzofuryl, halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed), phenyl C2-C6 thiazolinyl is (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed), furyl C1-C6 alkyl is [wherein on this furan nucleus, can be substituted with at least one phenyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed)], pyridyl C1-C6 alkyl is [wherein on this pyridine ring, can be substituted with at least one group, it is selected from by furyl and phenyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, the group that halogen replacement or unsubstituted C1-C6 alkyl and halogen replacement or unsubstituted C1-C6 alkoxyl group are formed) group of forming], benzofuryl C1-C6 alkyl is (wherein on this cumarone ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed), benzothienyl C1-C6 alkyl is (wherein on this thionaphthene ring, can be substituted with at least one halogen atom), benzofuryl C2-C6 thiazolinyl is (wherein on this cumarone ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed), thiazolyl is [wherein on this thiazole ring, can be substituted with at least one phenyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed)], phenoxy group C1-C6 alkyl is (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed)];

(u) the benzothiazole alkoxyl group is [wherein on this benzothiazole alkane ring, can be substituted with at least one group, it is selected from by oxo base and phenyl C1-C6 alkyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group) group formed];

(v) indoxyl is [wherein on this indole ring, can be substituted with at least one phenyl C1-C6 alkyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group)];

(w) pyrrolidyl is [wherein on this pyrrolidine ring, be substituted with at least one amino (wherein on this amino, can be substituted with at least one group, it is selected from by C1-C6 alkyl and phenyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group) group formed)];

(x) indolinyl (wherein on this indoline ring, can be substituted with at least one halogen atom);

(y) indoline oxygen base is [wherein on this indoline ring, can be substituted with at least one group, it is selected from by phenyl C1-C6 alkyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group) and the group formed of oxo base].

The invention provides according to 2 of above-mentioned general formula (1), 3-dihydro-6-nitroimidazole is acceptable salt, wherein R on [2,1-b] _ azole compounds, its optically active form or its pharmacology also ²Representative (a) to (c), (e) to (h), (j) to (q) and (s) to (y) any one described group.

The present invention also provides according to 2 of above-mentioned general formula (1), and 3-dihydro-6-nitroimidazole is acceptable salt, wherein R on [2,1-b] _ azole compounds, its optically active form or its pharmacology also ²Representative (d) described group.

The invention provides according to 2 of above-mentioned general formula (1), 3-dihydro-6-nitroimidazole is acceptable salt, wherein R on [2,1-b] _ azole compounds, its optically active form or its pharmacology also ²Representative (i) described group.

The invention provides according to 2 of above-mentioned general formula (1), 3-dihydro-6-nitroimidazole is acceptable salt, wherein R on [2,1-b] _ azole compounds, its optically active form or its pharmacology also ²Representative (r) described group.

The invention provides according to 2 of above-mentioned general formula (1), 3-dihydro-6-nitroimidazole is acceptable salt, wherein R on [2,1-b] _ azole compounds, its optically active form or its pharmacology also ¹Represent hydrogen atom.

The invention provides according to 2 of above-mentioned general formula (1), 3-dihydro-6-nitroimidazole is acceptable salt, wherein R on [2,1-b] _ azole compounds, its optically active form or its pharmacology also ¹Represent the C1-C6 alkyl.

The invention provides according to 2 of above-mentioned general formula (1), 3-dihydro-6-nitroimidazole is acceptable salt, wherein R on [2,1-b] _ azole compounds, its optically active form or its pharmacology also ¹With-(CH ₂) _nR ²Can be bonded to each other, constitute the volution of representing by following formula (30) with their adjacent carbon atoms:

Wherein RRR represents piperidyl [wherein on this piperidine ring, can be substituted with at least one phenoxy group (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group)].

The invention provides according to 2 of above-mentioned general formula (1), 3-dihydro-6-nitroimidazole is acceptable salt, wherein R on [2,1-b] _ azole compounds, its optically active form or its pharmacology also ¹Represent hydrogen atom or C1-C6 alkyl, R ³Representative (i) described group.

The invention provides according to 2 of above-mentioned general formula (1), 3-dihydro-6-nitroimidazole is acceptable salt, wherein R on [2,1-b] _ azole compounds, its optically active form or its pharmacology also ¹Represent hydrogen atom or C1-C6 alkyl, R ³Represent (ii) described group.

The invention provides according to 2 of above-mentioned general formula (1), 3-dihydro-6-nitroimidazole is acceptable salt, wherein R on [2,1-b] _ azole compounds, its optically active form or its pharmacology also ¹Represent hydrogen atom or C1-C6 alkyl, R ³Represent (iii) described group.

The invention provides according to 2 of above-mentioned general formula (1), 3-dihydro-6-nitroimidazole is acceptable salt, wherein R on [2,1-b] _ azole compounds, its optically active form or its pharmacology also ¹Represent hydrogen atom or C1-C6 alkyl, R ³Represent (iv) described group.

The invention provides according to 2 of above-mentioned general formula (1), 3-dihydro-6-nitroimidazole is acceptable salt, wherein R on [2,1-b] _ azole compounds, its optically active form or its pharmacology also ¹Represent hydrogen atom or C1-C6 alkyl, R ³Representative (v) described group.

The invention provides according to 2 of above-mentioned general formula (1), 3-dihydro-6-nitroimidazole is acceptable salt, wherein R on [2,1-b] _ azole compounds, its optically active form or its pharmacology also ¹Represent hydrogen atom or C1-C6 alkyl, R ³Representative (vi) described group.

The invention provides according to 2 of above-mentioned general formula (1), 3-dihydro-6-nitroimidazole is acceptable salt, wherein R on [2,1-b] _ azole compounds, its optically active form or its pharmacology also ¹Represent hydrogen atom or C1-C6 alkyl, R ³Representative (vii) described group.

The invention provides according to 2 of above-mentioned general formula (1), 3-dihydro-6-nitroimidazole is acceptable salt, wherein R on [2,1-b] _ azole compounds, its optically active form or its pharmacology also ¹Represent hydrogen atom or C1-C6 alkyl, R ³Representative (viii) described group.

The invention provides according to 2 of above-mentioned general formula (1), 3-dihydro-6-nitroimidazole is acceptable salt, wherein R on [2,1-b] _ azole compounds, its optically active form or its pharmacology also ¹Represent hydrogen atom or C1-C6 alkyl, R ³Representative (ix) described group.

The invention provides according to 2 of above-mentioned general formula (1), 3-dihydro-6-nitroimidazole is acceptable salt, wherein R on [2,1-b] _ azole compounds, its optically active form or its pharmacology also ¹Represent hydrogen atom or C1-C6 alkyl, R ³Representative (x) described group.

The invention provides according to 2 of above-mentioned general formula (1), 3-dihydro-6-nitroimidazole is acceptable salt, wherein R on [2,1-b] _ azole compounds, its optically active form or its pharmacology also ¹Represent hydrogen atom or C1-C6 alkyl, R ³Representative (xi) described group.

The invention provides according to 2 of above-mentioned general formula (1), 3-dihydro-6-nitroimidazole is acceptable salt, wherein R on [2,1-b] _ azole compounds, its optically active form or its pharmacology also ¹Represent hydrogen atom or C1-C6 alkyl, R ³Representative (xii) described group.

The invention provides according to 2 of above-mentioned general formula (1), 3-dihydro-6-nitroimidazole is acceptable salt, wherein R on [2,1-b] _ azole compounds, its optically active form or its pharmacology also ¹Represent hydrogen atom or C1-C6 alkyl, R ³Representative (xiii) described group.

The invention provides according to 2 of above-mentioned general formula (1), 3-dihydro-6-nitroimidazole is acceptable salt, wherein R on [2,1-b] _ azole compounds, its optically active form or its pharmacology also ¹Represent hydrogen atom or C1-C6 alkyl, R ³Representative (xiv) described group.

The invention provides according to 2 of above-mentioned general formula (1), 3-dihydro-6-nitroimidazole is acceptable salt, wherein R on [2,1-b] _ azole compounds, its optically active form or its pharmacology also ¹Represent hydrogen atom or C1-C6 alkyl, R ³Representative (xv) described group.

The invention provides according to 2 of above-mentioned general formula (1), 3-dihydro-6-nitroimidazole is acceptable salt, wherein R on [2,1-b] _ azole compounds, its optically active form or its pharmacology also ¹Represent hydrogen atom or C1-C6 alkyl, R ³Representative (xvi) described group.

The invention provides according to 2 of above-mentioned general formula (1), 3-dihydro-6-nitroimidazole is acceptable salt, wherein R on [2,1-b] _ azole compounds, its optically active form or its pharmacology also ¹Represent hydrogen atom or C1-C6 alkyl, R ³Representative (xvii) described group.

The invention provides according to 2 of above-mentioned general formula (1), 3-dihydro-6-nitroimidazole is acceptable salt, wherein R on [2,1-b] _ azole compounds, its optically active form or its pharmacology also ¹Represent hydrogen atom or C1-C6 alkyl, R ³Representative (xviii) described group.

The invention provides according to 2 of above-mentioned general formula (1), 3-dihydro-6-nitroimidazole is acceptable salt, wherein R on [2,1-b] _ azole compounds, its optically active form or its pharmacology also ¹Represent hydrogen atom or C1-C6 alkyl, R ³Representative (xix) described group.

The invention provides according to 2 of above-mentioned general formula (1), 3-dihydro-6-nitroimidazole is acceptable salt, wherein R on [2,1-b] _ azole compounds, its optically active form or its pharmacology also ¹Represent hydrogen atom or C1-C6 alkyl, R ³Representative (xx) described group.

The invention provides according to 2 of above-mentioned general formula (1), 3-dihydro-6-nitroimidazole is acceptable salt, wherein R on [2,1-b] _ azole compounds, its optically active form or its pharmacology also ¹Represent hydrogen atom or C1-C6 alkyl, R ³Representative (xxi) described group.

The invention provides according to 2 of above-mentioned general formula (1), 3-dihydro-6-nitroimidazole is acceptable salt, wherein R on [2,1-b] _ azole compounds, its optically active form or its pharmacology also ¹Represent hydrogen atom or C1-C6 alkyl, R ³Representative (xxii) described group.

In The compounds of this invention, particularly preferred as follows by formula (1) representative:

2-methyl-6-nitro-2-{4-[4-(4-trifluoromethyl benzyloxy methyl) piperidines-1-yl] phenoxymethyl }-2, the 3-glyoxalidine is [2,1-b] _ azoles also,

(R)-and 2-methyl-6-nitro-2-{4-[4-(4-trifluoromethyl benzyloxy methyl) piperidines-1-yl] phenoxymethyl }-2, the 3-glyoxalidine is [2,1-b] _ azoles also,

(S)-and 2-methyl-6-nitro-2-{4-[4-(4-trifluoromethyl benzyloxy methyl) piperidines-1-yl] phenoxymethyl }-2, the 3-glyoxalidine is [2,1-b] _ azoles also,

2-methyl-6-nitro-2-{4-[4-(4-chlorophenoxy methyl) piperidines-1-yl] phenoxymethyl }-2, the 3-glyoxalidine is [2,1-b] _ azoles also,

(R)-and 2-methyl-6-nitro-2-{4-[4-(4-chlorophenoxy methyl) piperidines-1-yl] phenoxymethyl }-2, the 3-glyoxalidine is [2,1-b] _ azoles also,

(S)-and 2-methyl-6-nitro-2-{4-[4-(4-chlorophenoxy methyl) piperidines-1-yl] phenoxymethyl }-2, the 3-glyoxalidine is [2,1-b] _ azoles also,

2-methyl-6-nitro-2-{4-[4-(4-trifluoromethyl cinnamyl) piperazine-1-yl] phenoxymethyl }-2, the 3-glyoxalidine is [2,1-b] _ azoles also,

(R)-and 2-methyl-6-nitro-2-{4-[4-(4-trifluoromethyl cinnamyl) piperazine-1-yl] phenoxymethyl }-2, the 3-glyoxalidine is [2,1-b] _ azoles also,

(S)-and 2-methyl-6-nitro-2-{4-[4-(4-trifluoromethyl cinnamyl) piperazine-1-yl] phenoxymethyl }-2, the 3-glyoxalidine is [2,1-b] _ azoles also,

2-methyl-6-nitro-2-{4-[4-(4-trifluoromethoxy cinnamyl) piperazine-1-yl] phenoxymethyl }-2, the 3-glyoxalidine is [2,1-b] _ azoles also,

(R)-and 2-methyl-6-nitro-2-{4-[4-(4-trifluoromethoxy cinnamyl) piperazine-1-yl] phenoxymethyl }-2, the 3-glyoxalidine is [2,1-b] _ azoles also,

(S)-and 2-methyl-6-nitro-2-{4-[4-(4-trifluoromethoxy cinnamyl) piperazine-1-yl] phenoxymethyl }-2, the 3-glyoxalidine is [2,1-b] _ azoles also,

2-methyl-6-nitro-2-{4-[4-(4-4-trifluoromethylphenopendant methyl) piperidines-1-yl] phenoxymethyl)-2, the 3-glyoxalidine is [2,1-b] _ azoles also,

(R)-and 2-methyl-6-nitro-2-{4-[4-(4-4-trifluoromethylphenopendant methyl) piperidines-1-yl] phenoxymethyl }-2, the 3-glyoxalidine is [2,1-b] _ azoles also,

(S)-and 2-methyl-6-nitro-2-{4-[4-(4-4-trifluoromethylphenopendant methyl) piperidines-1-yl] phenoxymethyl }-2, the 3-glyoxalidine is [2,1-b] _ azoles also,

6-nitro-2-{4-[4-(4-trifluoromethoxy benzyloxy) piperidines-1-yl] phenoxymethyl }-2, the 3-glyoxalidine is [2,1-b] _ azoles also,

(R)-and 6-nitro-2-{4-[4-(4-trifluoromethoxy benzyloxy) piperidines-1-yl] phenoxymethyl }-2, the 3-glyoxalidine is [2,1-b] _ azoles also,

(S)-and 6-nitro-2-{4-[4-(4-trifluoromethoxy benzyloxy) piperidines-1-yl] phenoxymethyl }-2, the 3-glyoxalidine is [2,1-b] _ azoles also,

6-nitro-2-{4-[4-(4-Trifluoromethyl phenyl ether oxygen ylmethyl) piperidines-1-yl] phenoxymethyl }-2, the 3-glyoxalidine is [2,1-b] _ azoles also,

(R)-and 6-nitro-2-{4-[4-(4-Trifluoromethyl phenyl ether oxygen ylmethyl) piperidines-1-yl] phenoxymethyl }-2, the 3-glyoxalidine is [2,1-b] _ azoles also,

(S)-and 6-nitro-2-{4-[4-(4-Trifluoromethyl phenyl ether oxygen ylmethyl) piperidines-1-yl] phenoxymethyl }-2, the 3-glyoxalidine is [2,1-b] _ azoles also,

6-nitro-2-{4-[4-(4-trifluoro-methoxybenzyl) piperidines-1-yl] phenoxymethyl }-2, the 3-glyoxalidine is [2,1-b] _ azoles also,

(R)-and 6-nitro-2-{4-[4-(4-trifluoro-methoxybenzyl) piperidines-1-yl] phenoxymethyl }-2, the 3-glyoxalidine is [2,1-b] _ azoles also,

(S)-and 6-nitro-2-{4-[4-(4-trifluoro-methoxybenzyl) piperidines-1-yl] phenoxymethyl }-2, the 3-glyoxalidine is [2,1-b] _ azoles also,

2-methyl-6-nitro-2-{4-[4-(4-trifluoro-methoxybenzyl) piperidines-1-yl] phenoxymethyl }-2, the 3-glyoxalidine is [2,1-b] _ azoles also,

(R)-and 2-methyl-6-nitro-2-{4-[4-(4-trifluoro-methoxybenzyl) piperidines-1-yl] phenoxymethyl }-2, the 3-glyoxalidine is [2,1-b] _ azoles also,

(S)-and 2-methyl-6-nitro-2-{4-[4-(4-trifluoro-methoxybenzyl) piperidines-1-yl] phenoxymethyl }-2, the 3-glyoxalidine is [2,1-b] _ azoles also,

2-methyl-6-nitro-2-[4-{4-[4-(4-trifluoromethyl) piperazine-1-yl] piperidines-1-yl } phenoxymethyl]-2, the 3-glyoxalidine is [2,1-b] _ azoles also,

(R)-and 2-methyl-6-nitro-2-[4-{4-[4-(4-trifluoromethyl) piperazine-1-yl] piperidines-1-yl } phenoxymethyl]-2, the 3-glyoxalidine is [2,1-b] _ azoles also,

(S)-and 2-methyl-6-nitro-2-[4-{4-[4-(4-trifluoromethyl) piperazine-1-yl] piperidines-1-yl } phenoxymethyl]-2, the 3-glyoxalidine is [2,1-b] _ azoles also,

2-methyl-6-nitro-2-[4-{4-[4-(4-Trifluoromethyl phenyl ether oxygen base) benzyl] piperazine-1-yl } phenoxymethyl]-2, the 3-glyoxalidine is [2,1-b] _ azoles also,

(R)-and 2-methyl-6-nitro-2-[4-{4-[4-(4-Trifluoromethyl phenyl ether oxygen base) benzyl] piperazine-1-yl } phenoxymethyl]-2, the 3-glyoxalidine is [2,1-b] _ azoles also,

(S)-and 2-methyl-6-nitro-2-[4-{4-[4-(4-Trifluoromethyl phenyl ether oxygen base) benzyl] piperazine-1-yl } phenoxymethyl]-2, the 3-glyoxalidine is [2,1-b] _ azoles also,

6-nitro-2-[4-{4-[3-(4-Trifluoromethoxyphen-l) propyl group] piperidines-1-yl } phenoxymethyl]-2, the 3-glyoxalidine is [2,1-b] _ azoles also,

(R)-and 6-nitro-2-[4-{4-[3-(4-Trifluoromethoxyphen-l) propyl group] piperidines-1-yl } phenoxymethyl]-2, the 3-glyoxalidine is [2,1-b] _ azoles also,

(S)-and 6-nitro-2-[4-{4-[3-(4-Trifluoromethoxyphen-l) propyl group] piperidines-1-yl } phenoxymethyl]-2, the 3-glyoxalidine is [2,1-b] _ azoles also,

2-methyl-6-nitro-2-{4-[2-(4-Trifluoromethoxyphen-l) _ azoles-4-yl] phenoxymethyl }-2, the 3-glyoxalidine is [2,1-b] _ azoles also,

(R)-and 2-methyl-6-nitro-2-{4-[2-(4-Trifluoromethoxyphen-l) _ azoles-4-yl] phenoxymethyl }-2, the 3-glyoxalidine is [2,1-b] _ azoles also,

(S)-and 2-methyl-6-nitro-2-{4-[2-(4-Trifluoromethoxyphen-l) _ azoles-4-yl] phenoxymethyl }-2, the 3-glyoxalidine is [2,1-b] _ azoles also,

6-nitro-2-{4-[4-(4-chlorophenoxy methyl) piperidines-1-yl] phenoxymethyl }-2, the 3-glyoxalidine is [2,1-b] _ azoles also,

(R)-and 6-nitro-2-{4-[4-(4-chlorophenoxy methyl) piperidines-1-yl] phenoxymethyl }-2, the 3-glyoxalidine is [2,1-b] _ azoles also,

(S)-and 6-nitro-2-{4-[4-(4-chlorophenoxy methyl) piperidines-1-yl] phenoxymethyl }-2, the 3-glyoxalidine is [2,1-b] _ azoles also,

2-methyl-6-nitro-2-{4-[4-(5-trifluoromethyl benzo furans-2-yl) methyl piperidine-1-yl] phenoxymethyl }-2, the 3-glyoxalidine is [2,1-b] _ azoles also,

(R)-and 2-methyl-6-nitro-2-{4-[4-(5-trifluoromethyl benzo furans-2-yl) methyl piperidine-1-yl] phenoxymethyl }-2, the 3-glyoxalidine is [2,1-b] _ azoles also,

(S)-and 2-methyl-6-nitro-2-{4-[4-(5-trifluoromethyl benzo furans-2-yl) methyl piperidine-1-yl] phenoxymethyl }-2, the 3-glyoxalidine is [2,1-b] _ azoles also,

2-methyl-6-nitro-2-{4-[2-(4-chloro-phenyl-) _ azoles-4-yl] phenoxymethyl }-2, the 3-glyoxalidine is [2,1-b] _ azoles also,

(R)-and 2-methyl-6-nitro-2-{4-[2-(4-chloro-phenyl-) _ azoles-4-yl] phenoxymethyl]-2, the 3-glyoxalidine is [2,1-b] _ azoles also,

(S)-and 2-methyl-6-nitro-2-{4-[2-(4-chloro-phenyl-) _ azoles-4-yl] phenoxymethyl }-2, the 3-glyoxalidine is [2,1-b] _ azoles also,

6-nitro-2-{4-[4-(4-4-trifluoromethylphenopendant methyl) piperidines-1-yl] phenoxymethyl }-2, the 3-glyoxalidine is [2,1-b] _ azoles also,

(R)-and 6-nitro-2-{4-[4-(4-4-trifluoromethylphenopendant methyl) piperidines-1-yl] phenoxymethyl }-2, the 3-glyoxalidine is [2,1-b] _ azoles also,

(S)-and 6-nitro-2-{4-[4-(4-4-trifluoromethylphenopendant methyl) piperidines-1-yl] phenoxymethyl }-2, the 3-glyoxalidine is [2,1-b] _ azoles also,

2-methyl-6-nitro-2-{4-[4-(4-cinnamyl bromide base) piperazine-1-yl] phenoxymethyl }-2, the 3-glyoxalidine is [2,1-b] _ azoles also,

(R)-and 2-methyl-6-nitro-2-{4-[4-(4-cinnamyl bromide base) piperazine-1-yl] phenoxymethyl }-2, the 3-glyoxalidine is [2,1-b] _ azoles also,

(S)-and 2-methyl-6-nitro-2-{4-[4-(4-cinnamyl bromide base) piperazine-1-yl] phenoxymethyl }-2, the 3-glyoxalidine is [2,1-b] _ azoles also,

2-methyl-6-nitro-2-[2-(4-Trifluoromethoxyphen-l)-1,2,3,4-tetrahydroisoquinoline-6-base oxygen ylmethyl]-2, the 3-glyoxalidine is [2,1-b] _ azoles also,

(R)-2-methyl-6-nitro-2-[2-(4-Trifluoromethoxyphen-l)-1,2,3,4-tetrahydroisoquinoline-6-base oxygen ylmethyl]-2, the 3-glyoxalidine also [2,1-b] _ azoles and

(S)-and 2-methyl-6-nitro-2-[2-(4-Trifluoromethoxyphen-l)-1,2,3,4-tetrahydroisoquinoline-6-base oxygen ylmethyl]-2, the 3-glyoxalidine is [2,1-b] _ azoles also.

The invention provides pharmaceutical composition, it is an antitubercular agent, wherein comprise by 2 of general formula (1) representative, 3-dihydro-6-nitroimidazole also on [2,1-b] _ azole compounds, its optically active form or its pharmacology acceptable salt as activeconstituents.

Definite, the invention provides pharmaceutical composition, it is an antitubercular agent, wherein comprise to be selected from as 2 of listed preferred compound above, 3-dihydro-6-nitroimidazole also at least a compound of [2,1-b] _ azole compounds as activeconstituents.

The invention provides the method for production by the compound of general formula (1) representative:

(R wherein ¹, R ²Have above-mentioned identical definition with n),

Described method comprises:

Will be by the 4-nitroimidazole compound of following general formula (2) representative:

(X wherein ₁Represent halogen atom or nitro),

React with epoxy compounds by following general formula (3a) representative:

(R wherein ¹, R ²Have above-mentioned identical definition with n), obtain compound by following general formula (4a) representative:

(R wherein ¹, R ²Have above-mentioned identical definition, X with n ¹Represent halogen atom or nitro); The compound that gained is represented by above-mentioned general formula (4a) encircles closure subsequently.

The invention provides the method for production by the compound of following general formula (1w) representative:

(R wherein ^1ARepresent hydrogen atom or C1-C6 alkyl, R ^2ARepresentative is any one described group in (a) to (y) as defined above, and n represents the integer between 0 and 6),

Described method comprises:

Will be by the compound of following general formula (3b) representative:

(R wherein ^1ASame as described above, X ¹Represent halogen atom or nitro),

With compound R ^2AH (5) or its reactant salt (R wherein ^2ARepresentative is (a) to (y) any one described group as defined above), obtain compound by following general formula (4c) representative:

(R wherein ¹Has above-mentioned identical definition, R ^2ARepresentative is (a) to (y) any one described group as defined above, X ¹Represent halogen atom or nitro); The compound that gained is represented by above-mentioned general formula (4c) encircles closure subsequently.

(R wherein ^1A, R ^2AHave above-mentioned identical definition with n),

Described method comprises:

Will be by the compound of following general formula (6) representative:

(R wherein ^1AHave above-mentioned identical definition, R with n ¹⁵Represent C1-C6 alkyl sulphonyl or benzenesulfonyl, wherein can be substituted with the C1-C6 alkyl),

With compound R ^2AH (5) or its reactant salt (R wherein ^2ARepresentative is (a) to (y) any one described group as defined above).

The best mode that carries out an invention

In the The compounds of this invention, particularly preferred R ¹, R ², R ³Group is as follows.R ¹Preferably hydrogen atom or C1-C6 alkyl.R ²Preferably group (d), (i) or (r) as defined above.R ³Preferably group is (ii), (iii) or (x) as defined above.R ⁸Preferably group (1), (2), (4), (5), (8), (24) or (25) as defined above.R ¹³Preferably phenyl C2-C10 thiazolinyl is [wherein on this benzyl ring; can be substituted with at least one group; it is selected from by halogen atom; the C1-C4 alkylene dioxo base; the C1-C6 alkylthio; benzoyl; cyano group; nitro; the C2-C6 alkanoyloxy; can have the C1-C6 alkyl as substituent amino; hydroxyl; phenyl C1-C6 alkoxyl group; phenoxy group; halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group] or phenyl C1-C6 alkyl [wherein on this benzyl ring; can be substituted with at least one group; it is selected from by piperidyl (wherein on this piperidine ring; can be substituted with at least one phenoxy group [wherein on this benzyl ring; can be substituted with at least one group; it is selected from by halogen atom; halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed]); phenyl is (wherein on this benzyl ring; can be substituted with at least one group; it is selected from by halogen atom; halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group) and phenoxy group (wherein on this benzyl ring; can be substituted with at least one group, it is selected from by halogen atom; the group that halogen replacement or unsubstituted C1-C6 alkyl and halogen replacement or unsubstituted C1-C6 alkoxyl group are formed) group of forming].

In this specification sheets, each is by R ¹, R ², R ³Group Deng representative is specific as follows:

The example of halogen atom has fluorine atom, chlorine atom, bromine atoms and iodine atom.

The C1-C6 alkyl is the straight or branched alkyl that contains 1 to 6 carbon atom, and the example comprises methyl, ethyl, n-propyl, sec.-propyl, normal-butyl, isobutyl-, the tertiary butyl, sec-butyl, n-pentyl, neo-pentyl, n-hexyl, isohexyl, 3-methyl amyl etc.

The C1-C6 alkoxyl group is to contain the group of C1-C6 alkyl and Sauerstoffatom as defined above, and the example comprises methoxyl group, oxyethyl group, positive propoxy, isopropoxy, n-butoxy, isobutoxy, tert.-butoxy, sec-butoxy, n-pentyloxy, neopentyl oxygen, positive hexyloxy, different hexyloxy, 3-methyl pentyloxy etc.

Halogen replaces or unsubstituted C1-C6 alkyl is the straight or branched alkyl that contains 1 to 6 carbon atom as defined above, it is replaced by 1 to 7 halogen atom alternatively, the example comprises methyl, ethyl, n-propyl, sec.-propyl, normal-butyl, isobutyl-, the tertiary butyl, sec-butyl, n-pentyl, neo-pentyl, n-hexyl, isohexyl, the 3-methyl amyl, methyl fluoride, difluoromethyl, trifluoromethyl, chloromethyl, dichloromethyl, trichloromethyl, brooethyl, two brooethyls, dichlorofluoromethyl, 2,2, the 2-trifluoroethyl, pentafluoroethyl group, the 2-chloroethyl, 3,3, the 3-trifluoro propyl, seven fluoropropyls, seven fluorine sec.-propyls, the 3-chloropropyl, the 2-chloropropyl, the 3-bromopropyl, 4,4,4-trifluoro butyl, 4,4,4,3,3-five fluorine butyl, the 4-chlorobutyl, the 4-brombutyl, the 2-chlorobutyl, 5,5,5-trifluoro amyl group, 5-chlorine amyl group, 6,6,6-trifluoro hexyl, 6-chlorine hexyl etc.

Halogen replaces or unsubstituted C1-C6 alkoxyl group is a C1-C6 alkoxyl group as defined above, it is replaced by 1 to 7 halogen atom alternatively, the example comprises methoxyl group, oxyethyl group, positive propoxy, isopropoxy, n-butoxy, isobutoxy, tert.-butoxy, sec-butoxy, n-pentyloxy, neopentyl oxygen, positive hexyloxy, different hexyloxy, 3-methyl pentyloxy, the fluorine methoxyl group, difluoro-methoxy, trifluoromethoxy, the chlorine methoxyl group, the dichloro methoxyl group, the trichlorine methoxyl group, the bromine methoxyl group, the dibromo methoxyl group, dichloro fluorine methoxyl group, 2,2, the 2-trifluoro ethoxy, five fluorine oxyethyl groups, the 2-chloroethoxy, 3,3,3-trifluoro propoxy-, seven fluorine propoxy-, seven fluorine isopropoxies, 3-chlorine propoxy-, 2-chlorine propoxy-, 3-bromine propoxy-, 4,4,4-trifluoro butoxy, 4,4,4,3,3-five fluorine butoxy, 4-chlorine butoxy, 4-bromine butoxy, 2-chlorine butoxy, 5,5,5-trifluoro pentyloxy, 5-chlorine pentyloxy, 6,6,6-trifluoro hexyloxy, 6-chlorine hexyloxy etc.

Phenoxy group is (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed) comprise that phenoxy group is (wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed), phenoxy group for example, the 2-fluorophenoxy, the 3-fluorophenoxy, the 4-fluorophenoxy, the 2-chlorophenoxy, the 3-chlorophenoxy, the 4-chlorophenoxy, 2-bromine phenoxy group, 3-bromine phenoxy group, 4-bromine phenoxy group, 2, the 3-dichlorophenoxy, 3, the 4-dichlorophenoxy, 2, the 4-dichlorophenoxy, 3,4, the 5-Trichlorophenoxy, 2,4, the 6-Trichlorophenoxy, 2,3,4,5,6-penta fluoro benzene oxygen base, the 2-methylphenoxy, the 3-methylphenoxy, the 4-methylphenoxy, 2-ethyl phenoxy group, 3-ethyl phenoxy group, 4-ethyl phenoxy group, 4-n-propyl phenoxy group, 4-tertiary butyl phenoxy group, 4-normal-butyl phenoxy group, the 2-4-trifluoromethylphenopendant, the 3-4-trifluoromethylphenopendant, the 4-4-trifluoromethylphenopendant, 2-pentafluoroethyl group phenoxy group, 3-pentafluoroethyl group phenoxy group, 2, the 3-dimethyl phenoxy, 3,4,5-trimethylammonium phenoxy group, 4-n-pentyl phenoxy group, 4-n-hexyl phenoxy group, 2-methoxyl group phenoxy group, 3-methoxyl group phenoxy group, 4-methoxyl group phenoxy group, the 2-ethoxy phenoxy, the 3-ethoxy phenoxy, the 4-ethoxy phenoxy, 4-positive propoxy phenoxy group, 4-tert.-butoxy phenoxy group, 4-n-butoxy phenoxy group, 2-Trifluoromethyl phenyl ether oxygen base, 3-Trifluoromethyl phenyl ether oxygen base, 4-Trifluoromethyl phenyl ether oxygen base, 2-five fluorine ethoxy phenoxies, 3-five fluorine ethoxy phenoxies, 2,3-dimethoxy phenoxy group, 3,4,5-trimethoxy phenoxy group, 4-n-pentyloxy phenoxy group, the positive hexyloxy phenoxy group of 4-etc.

Piperidyl is [wherein on this piperidine ring, can be substituted with at least one phenoxy group (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed)] comprise that piperidyl is [wherein on this piperidine ring, can be substituted with 1 to 3 phenoxy group (wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed)], piperidino for example, the 2-piperidyl, the 3-piperidyl, the 4-piperidyl, 4-phenoxy group-piperidino, 2,4-hexichol Oxy-1-piperidyl, 2,4,6-triple phenoxyl-piperidino, 2-(2-fluorophenoxy)-piperidino, 3-(3-fluorophenoxy)-2-piperidyl, 4-(4-fluorophenoxy)-3-piperidyl, 2-(2-chlorophenoxy)-4-piperidyl, 3-(3-chlorophenoxy)-5-piperidyl, 4-(4-chlorophenoxy)-2-piperidyl, 5-(2-bromine phenoxy group)-2-piperidyl, 6-(3-bromine phenoxy group)-3-piperidyl, 4-(4-bromine phenoxy group)-piperidino, 3-(2, the 3-dichlorophenoxy)-the 2-piperidyl, 4-(3, the 4-dichlorophenoxy)-the 3-piperidyl, 3-(2, the 4-dichlorophenoxy)-the 4-piperidyl, 2-(3,4, the 5-Trichlorophenoxy)-the 3-piperidyl, 6-(2,4, the 6-Trichlorophenoxy)-the 2-piperidyl, 3-(2,3,4,5,6-penta fluoro benzene oxygen base)-piperidino, 4-(2-methylphenoxy)-piperidino, 5-(3-methylphenoxy)-2-piperidyl, 6-(4-methylphenoxy)-3-piperidyl, 1-(2-ethyl phenoxy group)-4-piperidyl, 2-(3-ethyl phenoxy group)-piperidino, 3-(4-ethyl phenoxy group)-2-piperidyl, 4-(4-n-propyl phenoxy group)-3-piperidyl, 3-(4-tertiary butyl phenoxy group)-4-piperidyl, 2-(4-normal-butyl phenoxy group)-3-piperidyl, 1-(2-4-trifluoromethylphenopendant)-2-piperidyl, 2-(3-4-trifluoromethylphenopendant)-piperidino, 3-(4-4-trifluoromethylphenopendant)-piperidino, 1-(2-pentafluoroethyl group phenoxy group)-4-piperidyl, 1-(3-pentafluoroethyl group phenoxy group)-4-piperidyl, 4-(2, the 3-dimethyl phenoxy)-piperidino, 1-(3,4,5-trimethylammonium phenoxy group)-the 4-piperidyl, 1-(4-n-pentyl phenoxy group)-4-piperidyl, 4-(4-n-hexyl phenoxy group)-piperidino, 4-(2-methoxyl group phenoxy group)-piperidino, 1-(3-methoxyl group phenoxy group)-4-piperidyl, 1-(4-methoxyl group phenoxy group)-4-piperidyl, 2-(2-ethoxy phenoxy)-3-piperidyl, 3-(3-ethoxy phenoxy)-4-piperidyl, 4-(4-ethoxy phenoxy)-3-piperidyl, 3-(4-positive propoxy phenoxy group)-2-piperidyl, 2-(4-tert.-butoxy phenoxy group)-piperidino, 1-(4-n-butoxy phenoxy group)-2-piperidyl, 2-(2-Trifluoromethyl phenyl ether oxygen base)-3-piperidyl, 3-(3-Trifluoromethyl phenyl ether oxygen base)-4-piperidyl, 4-(4-Trifluoromethyl phenyl ether oxygen base)-3-piperidyl, 3-(2-five fluorine ethoxy phenoxies)-2-piperidyl, 2-(4-five fluorine ethoxy phenoxies)-piperidino, 1-(2,3-dimethoxy phenoxy group)-the 4-piperidyl, 4-(3,4,5-trimethoxy phenoxy group)-piperidino, 4-(4-n-pentyloxy phenoxy group)-piperidino, 4-(the positive hexyloxy phenoxy group of 4-)-piperidino etc.

Phenyl is (wherein on this benzyl ring, can be substituted with at least one piperidyl [wherein on this piperidine ring, can be substituted with at least one phenoxy group (wherein on this phenyl, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed)]) comprise that phenyl is (wherein on this benzyl ring, can be substituted with 1 to 3 piperidyl [wherein on this piperidine ring, can be substituted with 1 to 3 phenoxy group (wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed)]), phenyl for example, 4-(piperidino) phenyl, 2,4-two (piperidino) phenyl, 2,4,6-three (piperidino) phenyl, 3-(4-piperidyl) phenyl, 2-(2-piperidyl) phenyl, 4-(3-piperidyl) phenyl, 3-(4-phenoxy group-piperidino) phenyl, 2-(2,4-hexichol Oxy-1-piperidyl) phenyl, 4-(2,4,6-triple phenoxyl-piperidino) phenyl, 3-[2-(2-fluorophenoxy)-piperidino] phenyl, 2-[3-(3-fluorophenoxy)-2-piperidyl] phenyl, 4-[4-(4-fluorophenoxy)-3-piperidyl] phenyl, 3-[2-(2-chlorophenoxy)-4-piperidyl] phenyl, 2-[3-(3-chlorophenoxy)-5-piperidyl] phenyl, 4-[4-(4-chlorophenoxy)-2-piperidyl] phenyl, 3-[5-(2-bromine phenoxy group)-2-piperidyl] phenyl, 2-[6-(3-bromine phenoxy group)-3-piperidyl] phenyl, 4-[4-(4-bromine phenoxy group)-piperidino] phenyl, 3-[3-(2, the 3-dichlorophenoxy)-and the 2-piperidyl] phenyl, 2-[4-(3, the 4-dichlorophenoxy)-and the 3-piperidyl] phenyl, 4-[3-(2, the 4-dichlorophenoxy)-and the 4-piperidyl] phenyl, 3-[2-(3,4, the 5-Trichlorophenoxy)-and the 3-piperidyl] phenyl, 2-[6-(2,4, the 6-Trichlorophenoxy)-and the 2-piperidyl] phenyl, 4-[3-(2,3,4,5,6-penta fluoro benzene oxygen base)-and piperidino] phenyl, 3-[4-(2-methylphenoxy)-piperidino] phenyl, 2-[5-(3-methylphenoxy)-2-piperidyl] phenyl, 4-[6-(4-methylphenoxy)-3-piperidyl] phenyl, 3-[1-(2-ethyl phenoxy group)-4-piperidyl] phenyl, 2-[2-(3-ethyl phenoxy group)-piperidino] phenyl, 4-[3-(4-ethyl phenoxy group)-2-piperidyl] phenyl, 3-[4-(4-n-propyl phenoxy group)-3-piperidyl] phenyl, 2-[3-(4-tertiary butyl phenoxy group)-4-piperidyl] phenyl, 4-[2-(4-normal-butyl phenoxy group)-3-piperidyl] phenyl, 3-[1-(2-4-trifluoromethylphenopendant)-2-piperidyl] phenyl, 2-[2-(3-4-trifluoromethylphenopendant)-piperidino] phenyl, 4-[3-(4-4-trifluoromethylphenopendant)-piperidino] phenyl, 3-[1-(2-pentafluoroethyl group phenoxy group)-4-piperidyl] phenyl, 2-[1-(3-pentafluoroethyl group phenoxy group)-4-piperidyl] phenyl, 4-[4-(2, the 3-dimethyl phenoxy)-and piperidino] phenyl, 3-[1-(3,4,5-trimethylammonium phenoxy group)-and the 4-piperidyl] phenyl, 2-[1-(4-n-pentyl phenoxy group)-4-piperidyl] phenyl, 4-[4-(4-n-hexyl phenoxy group)-piperidino] phenyl, 3-[4-(2-methoxyl group phenoxy group)-piperidino] phenyl, 2-[1-(3-methoxyl group phenoxy group)-4-piperidyl] phenyl, 4-[1-(4-methoxyl group phenoxy group)-4-piperidyl] phenyl, 3-[2-(2-ethoxy phenoxy)-3-piperidyl] phenyl, 2-[3-(3-ethoxy phenoxy)-4-piperidyl] phenyl, 4-[4-(4-ethoxy phenoxy)-3-piperidyl] phenyl, 3-[3-(4-positive propoxy phenoxy group)-2-piperidyl] phenyl, 2-[2-(4-tert.-butoxy phenoxy group)-piperidino] phenyl, 4-[1-(4-n-butoxy phenoxy group)-2-piperidyl] phenyl, 3-[2-(2-Trifluoromethyl phenyl ether oxygen base)-3-piperidyl] phenyl, 2-[3-(3-Trifluoromethyl phenyl ether oxygen base)-4-piperidyl] phenyl, 4-[4-(4-Trifluoromethyl phenyl ether oxygen base)-piperidino] phenyl, 3-[3-(2-five fluorine ethoxy phenoxies)-2-piperidyl] phenyl, 2-[2-(4-five fluorine ethoxy phenoxies)-piperidino] phenyl, 4-[1-(2,3-dimethoxy phenoxy group)-and the 4-piperidyl] phenyl, 3-[4-(3,4,5-trimethoxy phenoxy group)-piperidino] phenyl, 2-[4-(4-n-pentyloxy phenoxy group)-piperidino] phenyl, 4-[4-(the positive hexyloxy phenoxy group of 4-)-piperidino] phenyl etc.

Phenyl is [wherein on this benzyl ring, can be substituted with at least-individual group, it is selected from by halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group] comprise unsubstituted or by 1 to 5, the phenyl that preferred 1 to 3 substituting group replaces, described substituting group is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed, as defined above, the example comprises phenyl, the 2-fluorophenyl, the 3-fluorophenyl, the 4-fluorophenyl, the 2-chloro-phenyl-, the 3-chloro-phenyl-, the 4-chloro-phenyl-, the 2-bromophenyl, the 3-bromophenyl, the 4-bromophenyl, the 2-iodophenyl, the 3-iodophenyl, the 4-iodophenyl, 2, the 3-difluorophenyl, 3, the 4-difluorophenyl, 3, the 5-difluorophenyl, 2, the 4-difluorophenyl, 2, the 6-difluorophenyl, 2, the 3-dichlorophenyl, 3, the 4-dichlorophenyl, 3, the 5-dichlorophenyl, 2, the 4-dichlorophenyl, 2, the 6-dichlorophenyl, 3,4, the 5-trifluorophenyl, 3,4, the 5-trichlorophenyl, 2,4, the 6-trifluorophenyl, 2,4, the 6-trichlorophenyl, 2-fluoro-4-bromophenyl, 4-chloro-3-fluorophenyl, 2,3, the 4-trichlorophenyl, 2,3,4,5, the 6-pentafluorophenyl group, 2,4, the 6-trimethylphenyl, the 4-n-butylphenyl, 2, the 4-3,5-dimethylphenyl, 2, the 3-3,5-dimethylphenyl, 2, the 6-3,5-dimethylphenyl, 3, the 5-3,5-dimethylphenyl, 2, the 5-3,5-dimethylphenyl, 3,5-two trifluoromethyls, 4-n-butoxy phenyl, 2, the 4-Dimethoxyphenyl, 2, the 3-Dimethoxyphenyl, 2, the 6-Dimethoxyphenyl, 3, the 5-Dimethoxyphenyl, 2, the 5-Dimethoxyphenyl, 2,4, the 6-trimethoxyphenyl, 3,5-two Trifluoromethoxyphen-ls, 3-chloro-4-p-methoxy-phenyl, 2-chloro-4-Trifluoromethoxyphen-l, 3-methyl-4-fluorophenyl, 4-bromo-3-trifluoromethyl, the 2-aminomethyl phenyl, the 3-aminomethyl phenyl, the 4-aminomethyl phenyl, 2-methyl-3-chloro-phenyl-, 3-methyl-4-chloro-phenyl-, 2-chloro-4-aminomethyl phenyl, 2-methyl-3-fluorophenyl, the 2-trifluoromethyl, the 3-trifluoromethyl, the 4-trifluoromethyl, 2-pentafluoroethyl group phenyl, 3-pentafluoroethyl group phenyl, 4-pentafluoroethyl group phenyl, the 2-isopropyl phenyl, the 3-isopropyl phenyl, the 4-isopropyl phenyl, the 2-tert-butyl-phenyl, the 3-tert-butyl-phenyl, the 4-tert-butyl-phenyl, the 2-secondary butyl phenenyl, the 3-secondary butyl phenenyl, the 4-secondary butyl phenenyl, 2-is the fluoropropyl phenyl just-seven, 3-is the fluoropropyl phenyl just-seven, 4-is the fluoropropyl phenyl just-seven, 4-amyl group phenyl, 4-hexyl phenyl, the 2-p-methoxy-phenyl, the 3-p-methoxy-phenyl, the 4-p-methoxy-phenyl, 3-chloro-2-p-methoxy-phenyl, 2-fluoro-3-p-methoxy-phenyl, 2-fluoro-4-p-methoxy-phenyl, 2,3, the 4-trifluorophenyl, the 2-Trifluoromethoxyphen-l, the 3-Trifluoromethoxyphen-l, the 4-Trifluoromethoxyphen-l, 3-fluoro-2-Trifluoromethoxyphen-l, 2-fluoro-3-Trifluoromethoxyphen-l, 3-fluoro-4-Trifluoromethoxyphen-l, 3-chloro-2-Trifluoromethoxyphen-l, 2-chloro-3-Trifluoromethoxyphen-l, 3-chloro-4-Trifluoromethoxyphen-l, 2-five fluorine ethoxyl phenenyls, 3-five fluorine ethoxyl phenenyls, 4-five fluorine ethoxyl phenenyls, 3-chloro-2-five fluorine ethoxyl phenenyls, 2-chloro-3-five fluorine ethoxyl phenenyls, 3-chloro-4-five fluorine ethoxyl phenenyls, the 2-isopropyl phenyl, the 3-isopropyl phenyl, the 4-isopropyl phenyl, 2-tert.-butoxy phenyl, 3-tert.-butoxy phenyl, 4-tert.-butoxy phenyl, 2-sec-butoxy phenyl, 3-sec-butoxy phenyl, 4-sec-butoxy phenyl, 2-is fluorine propoxy-phenyl just-seven, 3-is fluorine propoxy-phenyl just-seven, 4-is fluorine propoxy-phenyl just-seven, 4-n-pentyloxy phenyl, the positive hexyloxy phenyl of 4-etc.

The example of phenyl C1-C6 alkyl comprises benzyl, 1-styroyl, 2-styroyl, 3-phenyl propyl, 2-phenyl propyl, 4-phenyl butyl, 5-phenylpentyl, 4-phenylpentyl, 6-phenyl hexyl, 2-methyl-3-phenyl propyl, 1,1-dimethyl-2-phenylethyl etc.

Phenyl C1-C6 alkyl is (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, the group that halogen replacement or unsubstituted C1-C6 alkyl and halogen replacement or unsubstituted C1-C6 alkoxyl group are formed) comprises phenyl C1-C6 alkyl, this benzyl ring is unsubstituted or by 1 to 5, preferred 1 to 3 substituting group replaces, described substituting group is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed, the example comprises benzyl, the 1-styroyl, the 2-styroyl, the 3-phenyl propyl, the 2-phenyl propyl, the 4-phenyl butyl, the 5-phenylpentyl, the 4-phenylpentyl, 6-phenyl hexyl, the 2-luorobenzyl, the 3-luorobenzyl, the 4-luorobenzyl, 2-benzyl chloride base, 3-benzyl chloride base, 4-benzyl chloride base, the 2-bromobenzyl, the 3-bromobenzyl, the 4-bromobenzyl, 2-iodine benzyl, 3-iodine benzyl, 4-iodine benzyl, 2, the 3-difluorobenzyl, 3, the 4-difluorobenzyl, 3, the 5-difluorobenzyl, 2, the 4-difluorobenzyl, 2, the 6-difluorobenzyl, 2, the 3-dichloro benzyl, 3, the 4-dichloro benzyl, 3, the 5-dichloro benzyl, 2, the 4-dichloro benzyl, 2, the 6-dichloro benzyl, 2-fluoro-4-bromobenzyl, 4-chloro-3-luorobenzyl, 2,3,4-trichlorine benzyl, 3,4, the 5-trifluoro-benzyl, 2,4,6-trichlorine benzyl, the 4-isopropyl benzyl, 4-normal-butyl benzyl, the 4-methyl-benzyl, the 2-methyl-benzyl, the 3-methyl-benzyl, 2, the 4-dimethyl benzyl, 2, the 3-dimethyl benzyl, 2, the 6-dimethyl benzyl, 3, the 5-dimethyl benzyl, 2, the 5-dimethyl benzyl, 2,4, the 6-trimethyl benzyl, 3,5-two trifluoromethyl benzyls, 2,3,4,5, the 6-PFBBR, the 4-isopropoxide benzyl, 4-n-butoxy benzyl, the 4-methoxy-benzyl, the 2-methoxy-benzyl, the 3-methoxy-benzyl, 2, the 4-dimethoxy-benzyl, 2, the 3-dimethoxy-benzyl, 2, the 6-dimethoxy-benzyl, 3, the 5-dimethoxy-benzyl, 2, the 5-dimethoxy-benzyl, 2,4,6-trimethoxy benzyl, 3,5-two trifluoro-methoxybenzyls, the 2-isopropoxide benzyl, 3-chloro-4-methoxy-benzyl, 2-chloro-4-trifluoro-methoxybenzyl, 3-methyl-4-luorobenzyl, 4-bromo-3-trifluoromethyl benzyl, the 2-trifluoromethyl benzyl, the 3-trifluoromethyl benzyl, the 4-trifluoromethyl benzyl, 2-pentafluoroethyl group benzyl, 3-pentafluoroethyl group benzyl, 4-pentafluoroethyl group benzyl, the 2-trifluoro-methoxybenzyl, the 3-trifluoro-methoxybenzyl, the 4-trifluoro-methoxybenzyl, 2-five fluorine ethoxy benzyls, 3-five fluorine ethoxy benzyls, 4-five fluorine ethoxy benzyls, 2-(2-trifluoromethyl) ethyl, 2-(3-trifluoromethyl) ethyl, 2-(4-trifluoromethyl) ethyl, 2-(2-Trifluoromethoxyphen-l)-ethyl, 2-(3-(Trifluoromethoxyphen-l) ethyl, 2-(4-Trifluoromethoxyphen-l) ethyl, 2-(2-five fluorine ethoxyl phenenyls) ethyl, 2-(3-five fluorine ethoxyl phenenyls) ethyl, 2-(4-five fluorine ethoxyl phenenyls) ethyl, 3-(2-trifluoromethyl) propyl group, 3-(3-trifluoromethyl) propyl group, 3-(4-trifluoromethyl) propyl group, 3-(2-Trifluoromethoxyphen-l) propyl group, 3-(3-Trifluoromethoxyphen-l) propyl group, 3-(4-Trifluoromethoxyphen-l) propyl group, 3-(3-five fluorine ethoxyl phenenyls) propyl group, 3-(4-five fluorine ethoxyl phenenyls) propyl group, 4-(3-five fluorine ethoxyl phenenyls) butyl, 5-(4-trifluoromethyl) amyl group, 4-(4-trifluoromethyl) amyl group, 4-(4-Trifluoromethoxyphen-l) amyl group, 6-(3-trifluoromethyl) hexyl, 6-(4-trifluoromethyl) hexyl, 6-(4-trifluoromethoxy-phenyl) hexyl etc.

Phenyl C1-C6 alkyl is [wherein on this phenyl, can be substituted with at least one group, it is selected from by halogen atom, phenyl is (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed), halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group] comprise phenylalkyl, wherein this moieties be contain 1 to 6 carbon atom the straight or branched alkyl [wherein on this phenyl, can be substituted with 1 to 5, preferred 1 to 3 group, it is selected from by halogen atom, phenyl is (wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed), halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed], the example comprises 4-(4-trifluoromethyl) benzyl, 4-(4-Trifluoromethoxyphen-l) benzyl, 4-(4-chloro-phenyl-) benzyl, 4-(4-trifluoromethyl)-benzyl, the 4-phenylbenzyl, the 3-phenylbenzyl, 3,4-phenylbenzene benzyl, 3,4,5-triphenyl benzyl, 4-nitro-3-trifluoromethyl benzyl, 4-trifluoromethoxy-3-phenylbenzyl etc., also has above-mentioned phenyl C1-C6 alkyl in addition (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed).

Piperazinyl is [wherein on this piperazine ring, can be substituted with at least one phenyl C1-C6 alkyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed)] comprise that piperazinyl is [wherein on this piperazine ring, can be substituted with 1 to 3 phenyl C1-C6 alkyl (wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed)], 1-piperazinyl for example, the 2-piperazinyl, 3,4-dibenzyl-1-piperazinyl, 2,3,4-tribenzyl-1-piperazinyl, 4-benzyl-1-piperazinyl, 4-(2-styroyl (phenetyl))-1-piperazinyl, 4-(3-phenyl propyl)-1-piperazinyl, 4-(4-phenyl butyl)-1-piperazinyl, 4-(5-phenylpentyl)-1-piperazinyl, 4-(6-phenyl hexyl)-1-piperazinyl, 4-(2-luorobenzyl)-1-piperazinyl, 4-(3-luorobenzyl)-1-piperazinyl, 4-(4-luorobenzyl)-1-piperazinyl, 4-(2-benzyl chloride base)-1-piperazinyl, 4-(3-benzyl chloride base)-1-piperazinyl, 4-(4-benzyl chloride base)-1-piperazinyl, 4-(2, the 3-dichloro benzyl)-the 1-piperazinyl, 4-(2, the 4-dichloro benzyl)-the 1-piperazinyl, 4-(3, the 4-dichloro benzyl)-the 1-piperazinyl, 4-(3, the 5-dichloro benzyl)-the 1-piperazinyl, 4-(3,4,5-trichlorine benzyl)-the 1-piperazinyl, 4-(2,3,4,5, the 6-PFBBR)-the 1-piperazinyl, 4-(2-trifluoromethyl benzyl)-1-piperazinyl, 4-(3-trifluoromethyl benzyl)-1-piperazinyl, 4-(4-trifluoromethyl benzyl)-1-piperazinyl, 4-(4-methyl-benzyl)-1-piperazinyl, 4-(3, the 4-dimethyl benzyl)-the 1-piperazinyl, 4-(2,4, the 6-trimethyl benzyl)-the 1-piperazinyl, 4-(2-pentafluoroethyl group benzyl)-1-piperazinyl, 4-(3-pentafluoroethyl group benzyl)-1-piperazinyl, 4-(4-pentafluoroethyl group benzyl)-1-piperazinyl, 4-(2-trifluoro-methoxybenzyl)-1-piperazinyl, 4-(3-trifluoro-methoxybenzyl)-1-piperazinyl, 4-(4-trifluoro-methoxybenzyl)-1-piperazinyl, 4-(4-methoxy-benzyl)-1-piperazinyl, 4-(3, the 4-dimethoxy-benzyl)-the 1-piperazinyl, 4-(2,4,6-trimethoxy benzyl)-the 1-piperazinyl, 4-(2-five fluorine ethoxy benzyls)-1-piperazinyl, 4-(3-five fluorine ethoxy benzyls)-1-piperazinyl, 4-(4-five fluorine ethoxy benzyls)-1-piperazinyl, 4-[2-(4-Trifluoromethoxyphen-l) ethyl]-the 1-piperazinyl, 4-[3-(4-Trifluoromethoxyphen-l) propyl group]-the 1-piperazinyl, 4-[4-(4-Trifluoromethoxyphen-l) butyl]-the 1-piperazinyl, 4-[5-(4-Trifluoromethoxyphen-l)-amyl group]-the 1-piperazinyl, 4-[6-(4-Trifluoromethoxyphen-l) hexyl]-the 1-piperazinyl, 4-[2-(4-trifluoromethyl) ethyl]-the 1-piperazinyl, 4-[3-(4-trifluoromethyl) propyl group]-the 1-piperazinyl, 4-[4-(4-Trifluoromethoxyphen-l) butyl]-the 1-piperazinyl, 4-[5-(4-trifluoromethyl)-amyl group]-the 1-piperazinyl, 4-[6-(4-trifluoromethyl) hexyl]-the 1-piperazinyl etc.

Piperidyl is [wherein on this piperidine ring, can be substituted with at least one group, it is selected from by amino (wherein on this amino, can be substituted with at least one group, it is selected from by phenyl [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group] and the group of C1-C6 alkyl composition), phenoxy group is (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group) and phenyl C1-C6 alkyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, the group that halogen replacement or unsubstituted C1-C6 alkyl and halogen replacement or unsubstituted C1-C6 alkoxyl group are formed) group of forming] comprise that piperidyl is [wherein on this piperidine ring, can be substituted with 1 to 3 substituting group, it is selected from by amino (wherein on this amino, can be substituted with 1 or 2 and be selected from following substituting group: phenyl is [wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 group, it is selected from by halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group] and the group of C1-C6 alkyl composition), phenoxy group is (wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 group, it is selected from by halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group) and phenyl C1-C6 alkyl (wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 group, it is selected from by halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group) group formed], piperidino for example, the 2-piperidyl, the 3-piperidyl, the 4-piperidyl, 2,4-diaminostilbene-piperidyl, 2,4,6-triamino-piperidino, 2-amino-piperidino, 3-amino-piperidino, 4-amino-piperidino, 4-methylamino-piperidino, 4-ethylamino-piperidino, 4-n-propyl amino-piperidino, 4-dimethylamino-piperidino, 4-diethylamino-piperidino, 4-two-n-propyl amino-piperidino, 4-phenyl amino-piperidino, 4-(N-phenyl-N-methylamino)-piperidino, 4-(2-fluorophenyl amino)-piperidino, 4-(3-fluorophenyl amino)-piperidino, 4-(4-fluorophenyl amino)-piperidino, 4-(2-chloro-phenyl-amino)-piperidino, 4-(3-chloro-phenyl-amino)-piperidino, 4-(4-chloro-phenyl-amino)-piperidino, 4-(2,3-dichlorophenyl amino)-piperidino, 4-(2,4,6-trifluorophenyl amino)-piperidino, 4-(2,4 dichloro benzene base amino)-piperidino, 4-(3,4-dichlorophenyl amino)-piperidino, 4-(3,5-dichlorophenyl amino)-piperidino, 4-(2,3,4,5,6-pentafluorophenyl group amino)-piperidino, 4-(2-trifluoromethyl amino)-piperidino, 4-(2-aminomethyl phenyl amino)-piperidino, 4-(2,3-3,5-dimethylphenyl amino)-piperidino, 4-(2-trifluoromethyl amino)-piperidino, 4-(2,4,6-trimethylphenyl amino)-piperidino, 4-(4-trifluoromethyl amino)-piperidino, 4-(2-pentafluoroethyl group phenyl amino)-piperidino, 4-(3-pentafluoroethyl group phenyl amino)-piperidino, 4-(4-pentafluoroethyl group phenyl amino)-piperidino, 4-(2-Trifluoromethoxyphen-l amino)-piperidino, 4-(2-p-methoxy-phenyl amino)-piperidino, 4-(2,3-Dimethoxyphenyl amino)-piperidino, 4-(2,4,6-trimethoxyphenyl amino)-piperidino, 4-[N-methyl-N-(2,4,6-trimethoxyphenyl amino)]-piperidino, 4-[N-methyl-N-(3,4-3,5-dimethylphenyl amino)]-piperidino, 4-(3-Trifluoromethoxyphen-l amino)-piperidino, 4-(4-Trifluoromethoxyphen-l amino)-piperidino, 4-(2-five fluorine ethoxyl phenenyl amino)-piperidino, 4-(3-five fluorine ethoxyl phenenyl amino)-piperidino, 4-(4-five fluorine ethoxyl phenenyl amino)-piperidino, 4-phenoxy group-piperidino, 2,4-hexichol Oxy-1-piperidyl, 2,4,6-triple phenoxyl-piperidino, 2-(2-fluorophenoxy)-piperidino, 3-(3-fluorophenoxy)-2-piperidyl, 4-(4-fluorophenoxy)-3-piperidyl, 2-(2-chlorophenoxy)-4-piperidyl, 3-(3-chlorophenoxy)-5-piperidyl, 4-(4-chlorophenoxy)-2-piperidyl, 5-(2-bromine phenoxy group)-2-piperidyl, 6-(3-bromine phenoxy group)-3-piperidyl, 4-(4-bromine phenoxy group)-piperidino, 3-(2, the 3-dichlorophenoxy)-the 2-piperidyl, 4-(3, the 4-dichlorophenoxy)-3-piperidyl, 3-(2,4 dichloro benzene oxygen base)-4-piperidyl, 2-(3,4, the 5-Trichlorophenoxy)-the 3-piperidyl, 6-(2,4, the 6-Trichlorophenoxy)-2-piperidyl, 3-(2,3,4,5,6-penta fluoro benzene oxygen base)-piperidino, 4-(2-methylphenoxy)-piperidino, 5-(3-methylphenoxy)-2-piperidyl, 6-(4-methylphenoxy)-3-piperidyl, 1-(2-ethyl phenoxy group)-4-piperidyl, 2-(3-ethyl phenoxy group)-piperidino, 3-(4-ethyl phenoxy group)-2-piperidyl, 4-(4-n-propyl phenoxy group)-3-piperidyl, 3-(4-tertiary butyl phenoxy group)-4-piperidyl, 2-(4-normal-butyl phenoxy group)-3-piperidyl, 1-(2-4-trifluoromethylphenopendant)-2-piperidyl, 2-(3-4-trifluoromethylphenopendant)-piperidino, 3-(4-4-trifluoromethylphenopendant)-piperidino, 1-(2-pentafluoroethyl group phenoxy group)-4-piperidyl, 1-(3-pentafluoroethyl group phenoxy group)-4-piperidyl, 4-(2, the 3-dimethyl phenoxy)-piperidino, 1-(3,4,5-trimethylammonium phenoxy group)-the 4-piperidyl, 1-(4-n-pentyl phenoxy group)-4-piperidyl, 4-(4-n-hexyl phenoxy group)-piperidino, 4-(2-methoxyl group phenoxy group)-piperidino, 1-(3-methoxyl group phenoxy group)-4-piperidyl, 1-(4-methoxyl group phenoxy group)-4-piperidyl, 2-(2-ethoxy phenoxy)-3-piperidyl, 3-(3-ethoxy phenoxy)-4-piperidyl, 4-(4-ethoxy phenoxy)-3-piperidyl, 3-(4-positive propoxy phenoxy group)-2-piperidyl, 2-(4-tert.-butoxy phenoxy group)-piperidino, 1-(4-n-butoxy phenoxy group)-2-piperidyl, 2-(2-Trifluoromethyl phenyl ether oxygen base)-3-piperidyl, 3-(3-Trifluoromethyl phenyl ether oxygen base)-4-piperidyl, 4-(4-Trifluoromethyl phenyl ether oxygen base)-3-piperidyl, 3-(2-five fluorine ethoxy phenoxies)-2-piperidyl, 2-(4-five fluorine ethoxy phenoxies)-piperidino, 1-(2,3-dimethoxy phenoxy group)-4-piperidyl, 4-(3,4,5-trimethoxy phenoxy group)-piperidino, 4-(4-n-pentyloxy phenoxy group)-piperidino, 4-(the positive hexyloxy phenoxy group of 4-)-piperidino, 4-benzyl-piperidino, 2,4-dibenzyl-piperidino, 2,4,6-tribenzyl-piperidino, 2-(2-luorobenzyl)-piperidino, 3-[2-(3-fluorophenyl) ethyl]-the 2-piperidyl, 4-[1-(4-fluorophenyl) ethyl]-the 3-piperidyl, 2-[3-(2-chloro-phenyl-) propyl group]-the 4-piperidyl, 3-[4-(3-chloro-phenyl-) butyl]-the 5-piperidyl, 4-[5-(4-chloro-phenyl-) amyl group]-the 2-piperidyl, 5-[6-(2-bromophenyl) hexyl]-the 2-piperidyl, 6-(3-bromobenzyl)-3-piperidyl, 4-(4-bromobenzyl)-piperidino, 3-(2, the 3-dichloro benzyl)-the 2-piperidyl, 4-(3, the 4-dichloro benzyl)-3-piperidyl, 3-(2, the 4-dichloro benzyl)-4-piperidyl, 2-(3,4,5-trichlorine benzyl)-the 3-piperidyl, 6-(2,4,6-trichlorine benzyl)-2-piperidyl, 3-(2,3,4,5, the 6-PFBBR)-piperidino, 4-(2-methyl-benzyl)-piperidino, 5-[2-(3-aminomethyl phenyl) ethyl]-the 2-piperidyl, 6-[3-(4-aminomethyl phenyl) propyl group]-the 3-piperidyl, 1-[4-(2-ethylphenyl) butyl]-the 4-piperidyl, 2-[5-(3-ethylphenyl) amyl group]-piperidino, 3-[6-(4-ethylphenyl) hexyl]-the 2-piperidyl, 4-(4-n-propyl benzyl)-3-piperidyl, 3-(4-tertiary butyl benzyl)-4-piperidyl, 2-(4-normal-butyl benzyl)-3-piperidyl, 1-(2-trifluoromethyl benzyl)-2-piperidyl, 2-(3-trifluoromethyl benzyl)-piperidino, 3-(4-trifluoromethyl benzyl)-piperidino, 1-(2-pentafluoroethyl group benzyl)-4-piperidyl, 1-(3-pentafluoroethyl group benzyl)-4-piperidyl, 4-(2, the 3-dimethyl benzyl)-piperidino, 1-(3,4, the 5-trimethyl benzyl)-the 4-piperidyl, 1-(4-n-pentyl benzyl)-4-piperidyl, 4-(4-n-hexyl benzyl)-piperidino, 4-(2-methoxy-benzyl)-piperidino, 1-[2-(3-p-methoxy-phenyl) ethyl]-the 4-piperidyl, 1-[1-(4-p-methoxy-phenyl) ethyl]-the 4-piperidyl, 2-[3-(2-ethoxyl phenenyl) propyl group]-the 3-piperidyl, 3-[4-(3-ethoxyl phenenyl) butyl]-the 4-piperidyl, 4-[5-(4-ethoxyl phenenyl) amyl group]-the 3-piperidyl, 3-[6-(4-positive propoxy phenyl) hexyl]-the 2-piperidyl, 2-(4-tert.-butoxy benzyl)-piperidino, 1-(4-n-butoxy benzyl)-2-piperidyl, 2-(2-trifluoro-methoxybenzyl)-3-piperidyl, 3-(3-trifluoro-methoxybenzyl)-4-piperidyl, 4-(4-trifluoro-methoxybenzyl)-3-piperidyl, 3-(2-five fluorine ethoxy benzyls)-2-piperidyl, 2-(4-five fluorine ethoxy benzyls)-piperidino, 1-(2, the 3-dimethoxy-benzyl)-4-piperidyl, 4-(3,4,5-trimethoxy benzyl)-piperidino, 4-(4-n-pentyloxy benzyl)-piperidino, 4-(the positive hexyloxy benzyl of 4-)-piperidino, 4-benzyl-3-phenoxy group-piperidino, 4-phenoxy group-2-methylamino-piperidino etc.

The C1-C6 alkyl that C1-C6 alkoxy C 1-C6 alkoxyl group replaces comprises alkoxy alkoxy alkyl, on this alkoxyl group part, has the straight or branched alkoxyl group that contains 1 to 6 carbon atom, on this moieties, has the straight or branched alkyl that contains 1 to 6 carbon atom, methoxymethoxy methyl for example, 2-(methoxymethoxy) ethyl, 1-(2-methoxy ethoxy) ethyl, 1-(methoxymethoxy) ethyl, 2-(3-propoxy-) propoxy-ethyl, 3-(2-oxyethyl group isopropoxy) propyl group, 4-(4-butoxy butoxy) butyl, 5-(5-pentyloxy pentyloxy) amyl group, 6-(6-hexyloxy hexyloxy) hexyl, 1,1-dimethyl-2-(oxyethyl group methoxy base) ethyl, 2-methyl-3-(methoxy ethoxy) propyl group or 3-(propoxy-methoxyl group) propyl group etc.

The C1-C6 alkyl that thienyl C1-C6 alkoxyl group replaces is (wherein on this thiphene ring, can be substituted with at least one halogen atom) comprise the thienyl alkoxyalkyl, on this alkoxyl group part, has the straight or branched alkoxyl group that contains 1 to 6 carbon atom, have on this moieties contain 1 to 6 carbon atom the straight or branched alkyl (wherein on this thiphene ring, can be substituted with 1 to 3 halogen atom as substituting group), 2-thienyl methoxymethyl for example, 3-thienyl methoxymethyl, 2-(2-(2-thienyl) oxyethyl group) ethyl, 3-(3-(2-thienyl) propoxy-) propyl group, 4-(4-(2-thienyl) butoxy) butyl, 4-(4-(3-thienyl) butoxy) butyl, 5-(5-(2-thienyl) pentyloxy) amyl group, 5-(5-(3-thienyl) pentyloxy) amyl group, 6-(6-(2-thienyl) hexyloxy) hexyl, 6-(6-(3-thienyl) hexyloxy) hexyl, (5-chloro-2-thienyl methoxyl group) methyl, (5-chloro-3-thienyl methoxyl group) methyl, 2-(2-(4-bromo-2-thienyl) oxyethyl group) ethyl, 3-(3-(3-fluoro-2-thienyl) propoxy-) propyl group, 4-(4-(5-iodo-2-thienyl) butoxy) butyl, 4-(4-(4-chloro-3-thienyl) butoxy) butyl, 5-(5-(3-chloro-2-thienyl) pentyloxy) amyl group, 5-((2-chloro-3-thienyl) methoxyl group) amyl group, 6-(2-(3-chloro-2-thienyl) oxyethyl group) hexyl, 6-(6-(5-chloro-3-thienyl) hexyloxy) hexyl, (2-(4,5-two chloro-2-thienyls) methyl oxyethyl group), ((2,4,5-three chloro-3-thienyls) methoxyl group) methyl etc.

The C1-C6 alkyl that phenyl C2-C6 alkene oxygen base replaces is (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group) be the group of following composition: unsubstituted or by 1 to 5, the phenyl that preferred 1 to 3 substituting group replaces, described substituting group is selected from by halogen atom, halogen replaces or unsubstituted straight or branched alkyl and the halogen that contains 1 to 6 carbon atom replaces or the unsubstituted group that contains the straight or branched alkoxyl group composition of 1 to 6 carbon atom; And thiazolinyl, wherein contain 2 to 6 carbon atoms, have at least 1 to 3 two key.Phenyl C2-C6 alkene oxygen base comprises trans and the cis form.This class phenyl C2-C6 alkene oxygen base C1-C6 alkyl comprises (2-phenyl vinyloxy group) methyl, (3-phenyl-2-propenyloxy group) methyl, 2-(4-phenyl-2-butylene oxygen base) ethyl, 1-(4-phenyl-3-butenyloxy) ethyl, 3-(4-phenyl-1,3-divinyl oxygen base) propyl group, 4-(5-phenyl-1,3,5-hexatriene oxygen base) butyl, 5-(3-(2-fluorophenyl)-2-propenyloxy group) amyl group, 6-(3-(3-fluorophenyl)-2-propenyloxy group) hexyl, (3-(4-fluorophenyl)-2-propenyloxy group) methyl, (3-(2 for 2-, the 3-difluorophenyl)-and the 2-propenyloxy group) ethyl, (3-(2 for 3-, 3,4,5, the 6-pentafluorophenyl group)-and the 2-propenyloxy group) propyl group, (3-(2 for 4-, the 4-difluorophenyl)-and the 2-propenyloxy group) butyl, (3-(3 for 5-, the 4-difluorophenyl)-and the 2-propenyloxy group) amyl group, (3-(3 for 6-, the 5-difluorophenyl)-and the 2-propenyloxy group) hexyl, (3-(2-chloro-phenyl-)-2-propenyloxy group) methyl, 2-(3-(3-chloro-phenyl-)-2-propenyloxy group) ethyl, 3-(3-(4-chloro-phenyl-)-2-propenyloxy group) propyl group, (3-(2 for 4-, the 3-dichlorophenyl)-and the 2-propenyloxy group) butyl, (3-(2 for 5-, the 4-dichlorophenyl)-and the 2-propenyloxy group) amyl group, (3-(3 for 6-, the 4-dichlorophenyl)-and the 2-propenyloxy group) hexyl, (3-(3, the 5-dichlorophenyl)-and the 2-propenyloxy group) methyl, 2-(3-(2-bromophenyl)-2-propenyloxy group) ethyl, 3-(3-(3-bromophenyl)-2-propenyloxy group) propyl group, 4-(3-(4-bromophenyl)-2-propenyloxy group) butyl, 5-(3-(2-aminomethyl phenyl)-2-propenyloxy group) amyl group, 6-(3-(3-aminomethyl phenyl)-2-propenyloxy group) hexyl, (3-(4-aminomethyl phenyl)-2-propenyloxy group) methyl, 2-(3-(2-trifluoromethyl)-2-propenyloxy group) ethyl, 3-(3-(2-fluoro-4-bromophenyl)-2-propenyloxy group) propyl group, 4-(3-(4-chloro-3-fluorophenyl)-2-propenyloxy group) butyl, (3-(2 for 5-, 3, the 4-trichlorophenyl)-and the 2-propenyloxy group) amyl group, (3-(2 for 6-, 4, the 6-trichlorophenyl)-and the 2-propenyloxy group) hexyl, (3-(4-isopropyl phenyl)-2-propenyloxy group) methyl, 2-(3 ((4-n-butylphenyl)-2-propenyloxy group) ethyl, (3-(2 for 1-, the 4-3,5-dimethylphenyl)-and the 2-propenyloxy group) ethyl, 3-(3 ((2, the 3-3,5-dimethylphenyl)-and the 2-propenyloxy group) propyl group, ((2, the 6-3,5-dimethylphenyl)-and the 2-propenyloxy group) methyl, (3-(3 for 5-, the 5-3,5-dimethylphenyl)-and the 2-propenyloxy group) amyl group, (3-(2 for 6-, the 5-3,5-dimethylphenyl)-and the 2-propenyloxy group) hexyl, (3-(2,4, the 6-trimethylphenyl)-and the 2-propenyloxy group) methyl, (3-(3,5-two trifluoromethyls)-and the 2-propenyloxy group) methyl, (3-(4-n-butoxy phenyl)-2-propenyloxy group) methyl, (3-(2, the 4-Dimethoxyphenyl)-and the 2-propenyloxy group) methyl, (3-(2, the 3-Dimethoxyphenyl)-and the 2-propenyloxy group) methyl, (3-(2, the 6-Dimethoxyphenyl)-and the 2-propenyloxy group) methyl, (3-(3, the 5-Dimethoxyphenyl)-and the 2-propenyloxy group) methyl, (3-(2, the 5-Dimethoxyphenyl)-and the 2-propenyloxy group) methyl, (3-(3,5-two Trifluoromethoxyphen-ls)-and the 2-propenyloxy group) methyl, (3-(3-chloro-4-p-methoxy-phenyl)-2-propenyloxy group) methyl, (3-(2-chloro-4-Trifluoromethoxyphen-l)-2-propenyloxy group) methyl, (3-(3-methyl-4-fluorophenyl)-2-propenyloxy group) methyl, (3-(4-bromo-3-trifluoromethyl)-2-propenyloxy group) methyl, (3-(3-trifluoromethyl)-2-propenyloxy group) methyl, (3-(4-trifluoromethyl)-2-propenyloxy group) methyl, (3-(2-Trifluoromethoxyphen-l)-2-propenyloxy group) methyl, (3-(3-Trifluoromethoxyphen-l)-2-propenyloxy group) methyl, (3-(4-Trifluoromethoxyphen-l)-2-propenyloxy group) methyl, (3-(2-p-methoxy-phenyl)-2-propenyloxy group) methyl, (3-(3-p-methoxy-phenyl)-2-propenyloxy group) methyl, (3-(4-p-methoxy-phenyl)-2-propenyloxy group) methyl, (3-(3, the 4-Dimethoxyphenyl)-and the 2-propenyloxy group) methyl, (3-(3, the 5-Dimethoxyphenyl)-2-propenyloxy group) methyl, (4-(4-chloro-phenyl-)-2-butylene oxygen base) methyl, (4-(4-chloro-phenyl-)-3-butenyloxy) methyl, (5-(4-chloro-phenyl-)-2-amylene oxygen base) methyl, (5-(4-chloro-phenyl-)-4-amylene oxygen base) methyl, (5-(4-chloro-phenyl-)-3-amylene oxygen base) methyl, (6-(4-chloro-phenyl-)-5-hexene oxygen base) methyl, (6-(4-chloro-phenyl-)-4-hexene oxygen base) methyl, (6-(4-chloro-phenyl-)-3-hexene oxygen base) methyl, (6-(4-chloro-phenyl-)-3-hexene oxygen base) methyl etc.

The C1-C6 alkyl that quinolyl C1-C6 alkoxyl group replaces comprises the quinolyl alkoxyalkyl, has the straight or branched alkoxyl group that contains 1 to 6 carbon atom on this alkoxyl group part, has the straight or branched alkyl that contains 1 to 6 carbon atom on this moieties, for example (2-, 3-, 4-, 5-, 6-, 7-or 8-) the quinolyl methoxymethyl, 2-(2-((2-, 3-, 4-, 5-, 6-, 7-or 8-) quinolyl) oxyethyl group) ethyl, 3-(3-((2-, 3-, 4-, 5-, 6-, 7-or 8-) quinolyl) propoxy-) propyl group, 4-(4-((2-, 3-, 4-, 5-, 6-, 7-or 8-) quinolyl) butoxy) butyl, 5-(5-((2-, 3-, 4-, 5-, 6-, 7-or 8-) quinolyl) pentyloxy) amyl group, 6-(6-((2-, 3-, 4-, 5-, 6-, 7-or 8-) quinolyl) hexyloxy) hexyl etc.

The C1-C6 alkyl that piperidinyl carbonyl C1-C6 alkoxyl group replaces comprises the piperidinyl carbonyl alkoxyalkyl, on this alkoxyl group part, has the straight or branched alkoxyl group that contains 1 to 6 carbon atom, on this moieties, has the straight or branched alkyl that contains 1 to 6 carbon atom, (1-for example, 2-or 3-) the piperidinyl carbonyl methoxymethyl, 2-(2-((1-, 2-or 3-) piperidinyl carbonyl) oxyethyl group) ethyl, 3-(3-((1-, 2-or 3-) piperidinyl carbonyl) propoxy-) propyl group, 4-(4-((1-, 2-or 3-) piperidinyl carbonyl) butoxy) butyl, 5-(5-((1-, 2-or 3-) piperidinyl carbonyl) pentyloxy) amyl group, 6-(6-((1-, 2-or 3-) piperidinyl carbonyl) hexyloxy) hexyl etc.

Phenyl C1-C6 alkyl is [wherein on this benzyl ring, be substituted with at least one phenyl (wherein on this benzyl ring, be substituted with at least one group, it is selected from by halogen atom, the group that halogen replacement or unsubstituted C1-C6 alkyl and halogen replacement or unsubstituted C1-C6 alkoxyl group are formed)] comprise such phenylalkyl, wherein have on this moieties contain 1 to 6 carbon atom the straight or branched alkyl [wherein on this benzyl ring, be substituted with 1 to 3 phenyl (wherein on this benzyl ring, be substituted with 1 to 5, preferred 1 to 3 substituting group, it is selected from by halogen atom, halogen replacement or unsubstituted straight or branched C1-C6 alkyl and the group that halogen replaces or unsubstituted straight or branched C1-C6 alkoxyl group is formed)], 2-(2-fluorophenyl) benzyl for example, 3-(3-fluorophenyl) benzyl, 4-(4-fluorophenyl) benzyl, 2-(2-chloro-phenyl-) benzyl, 3-(3-chloro-phenyl-) benzyl, 4-(4-chloro-phenyl-) benzyl, 2-(2-bromophenyl) benzyl, 3-(3-bromophenyl) benzyl, 4-(4-bromophenyl) benzyl, 2-(2-iodophenyl) benzyl, 3-(3-iodophenyl) benzyl, 4-(4-iodophenyl) benzyl, 4-(2, the 3-difluorophenyl) benzyl, 3-(3, the 4-difluorophenyl) benzyl, 2-(3, the 5-difluorophenyl) benzyl, 4-(2, the 4-difluorophenyl) benzyl, 3-(2, the 6-difluorophenyl) benzyl, 2-(2, the 3-dichlorophenyl) benzyl, 4-(3, the 4-dichlorophenyl) benzyl, 3-(3, the 5-dichlorophenyl) benzyl, 2-(2, the 4-dichlorophenyl) benzyl, 4-(2, the 6-dichlorophenyl) benzyl, 3-(2-fluoro-4-bromophenyl) benzyl, 2-(4-chloro-3-fluorophenyl) benzyl, 4-(2,3, the 4-trichlorophenyl) benzyl, 3-(3,4, the 5-trifluorophenyl) benzyl, 2-(2,4, the 6-trichlorophenyl) benzyl, 4-(4-isopropyl phenyl) benzyl, 3-(4-n-butylphenyl) benzyl, 2-(4-aminomethyl phenyl) benzyl, 4-(2-aminomethyl phenyl) benzyl, 3-(3-aminomethyl phenyl) benzyl, 2-(2, the 4-3,5-dimethylphenyl) benzyl, 4-(2,3-3,5-dimethylphenyl benzyl, 3-(2, the 6-3,5-dimethylphenyl) benzyl, 2-(3, the 5-3,5-dimethylphenyl) benzyl, 4-(2, the 5-3,5-dimethylphenyl) benzyl, 3-(2,4, the 6-trimethylphenyl) benzyl, 2-(3,5-two trifluoromethyls) benzyl, 4-(2,3,4,5, the 6-pentafluorophenyl group) benzyl, 3-(4-isopropyl phenyl) benzyl, 2-(4-n-butoxy phenyl) benzyl, 4-(4-p-methoxy-phenyl) benzyl, 3-(2-p-methoxy-phenyl) benzyl, 2-(3-p-methoxy-phenyl) benzyl, 4-(2, the 4-Dimethoxyphenyl) benzyl, 3-(2, the 3-Dimethoxyphenyl) benzyl, 2-(2, the 6-Dimethoxyphenyl) benzyl, 2-(3, the 5-Dimethoxyphenyl) benzyl, 4-(2, the 5-Dimethoxyphenyl) benzyl, 3-(2,4, the 6-trimethoxyphenyl) benzyl, 2-(3,5-two Trifluoromethoxyphen-ls) benzyl, 4-(2-isopropyl phenyl) benzyl, 3-(3-chloro-4-p-methoxy-phenyl) benzyl, 2-(2-chloro-4-Trifluoromethoxyphen-l) benzyl, 4-(3-methyl-4-fluorophenyl) benzyl, 3-(4-bromo-3-trifluoromethyl) benzyl, 4-(2-trifluoromethyl) benzyl, 3-(3-trifluoromethyl) benzyl, 4-(4-trifluoromethyl) benzyl, 2-(2-pentafluoroethyl group phenyl) benzyl, 3-(3-pentafluoroethyl group phenyl) benzyl, 2-(4-pentafluoroethyl group phenyl) benzyl, 4-(2-Trifluoromethoxyphen-l) benzyl, 3-(3-Trifluoromethoxyphen-l) benzyl, 4-(4-Trifluoromethoxyphen-l) benzyl, 4-(2-five fluorine ethoxyl phenenyls) benzyl, 3-(3-five fluorine ethoxyl phenenyls) benzyl, 2-(4-five fluorine ethoxyl phenenyls) benzyl, 2-(4-(2-trifluoromethyl) phenyl) ethyl, 2-(3-(3-trifluoromethyl) phenyl) ethyl, 2-(2-(4-trifluoromethyl) phenyl) ethyl, 2-(4-(2-Trifluoromethoxyphen-l) phenyl) ethyl, 2-(3-(3-Trifluoromethoxyphen-l) phenyl) ethyl, 2-(2-(4-Trifluoromethoxyphen-l) phenyl) ethyl, 2-(4-(2-five fluorine ethoxyl phenenyls) phenyl) ethyl, 2-(3-(3-five fluorine ethoxyl phenenyls) phenyl) ethyl, 2-(2-(4-five fluorine ethoxyl phenenyls) phenyl) ethyl, 3-(4-(2-trifluoromethyl) phenyl) propyl group, 3-(3-(3-trifluoromethyl) phenyl) propyl group, 3-(2-(4-trifluoromethyl) phenyl) propyl group, 3-(4-(2-Trifluoromethoxyphen-l) phenyl) propyl group, 3-(3-(3-Trifluoromethoxyphen-l) phenyl) propyl group, 3-(2-(4-Trifluoromethoxyphen-l) phenyl) propyl group, 3-(4-(3-five fluorine ethoxyl phenenyls) phenyl) propyl group, 3-(3-(4-five fluorine ethoxyl phenenyls) phenyl) propyl group, 4-(2-(3-five fluorine ethoxyl phenenyls) phenyl) butyl, 5-(4-(4-trifluoromethyl) phenyl) amyl group, 4-(3-(4-trifluoromethyl) phenyl) amyl group, 4-(2-(4-Trifluoromethoxyphen-l) phenyl) amyl group, 6-(4-(3-trifluoromethyl) phenyl) hexyl, 6-(3-(4-trifluoromethyl) phenyl) hexyl, 6-(2-(4-trifluoromethyl) phenyl) hexyl, 2,4-two (4-trifluoromethyl) benzyl, 2,4,6-three (4-Trifluoromethoxyphen-l) benzyl etc.

Benzoyl C1-C6 alkyl is (wherein on this benzyl ring; can be substituted with at least one group; it is selected from by halogen atom; halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed) be benzoyl C1-C6 alkyl; wherein be unsubstituted or on this benzyl ring by 1 to 5; preferred 1 to 3 substituting group replaces; described substituting group is selected from by halogen atom; the group of halogen replacement or unsubstituted straight or branched C1-C6 alkyl and halogen replacement or unsubstituted straight or branched C1-C6 alkoxyl group composition; the example comprises the benzoyl methyl; 1-benzoyl ethyl; 2-benzoyl ethyl; 3-benzoyl propyl group; 2-benzoyl propyl group; 4-benzoyl butyl; 5-benzoyl amyl group; 4-benzoyl amyl group; 6-benzoyl hexyl; 2-fluorobenzoyl ylmethyl; 3-fluorobenzoyl ylmethyl; 4-fluorobenzoyl ylmethyl; 2-chlorobenzoyl ylmethyl; 3-chlorobenzoyl ylmethyl; 4-chlorobenzoyl ylmethyl; 2-benzoyl bromide methyl; 3-benzoyl bromide methyl; 4-benzoyl bromide methyl; 2-iodobenzene formyl radical methyl; 3-iodobenzene formyl radical methyl; 4-iodobenzene formyl radical methyl; 2; 3-difluoro benzoyl methyl; 3; 4-difluoro benzoyl methyl; 3; 5-difluoro benzoyl methyl; 2; 4-difluoro benzoyl methyl; 2; 6-difluoro benzoyl methyl; 2; 3-dichloro-benzoyl ylmethyl; 3; 4-dichloro-benzoyl ylmethyl; 3; 5-dichloro-benzoyl ylmethyl; 2; 4-dichloro-benzoyl ylmethyl; 2; 6-dichloro-benzoyl ylmethyl; 2-fluoro-4-benzoyl bromide methyl; 4-chloro-3-fluorobenzoyl ylmethyl; 2; 3; 4-trichlorobenzene formyl radical methyl; 3; 4; 5-trifluoromethyl benzonitrile acyl group methyl; 2; 4; 6-trichlorobenzene formyl radical methyl; 4-isopropyl benzene formyl radical methyl; 4-n-butylbenzene formyl radical methyl; 4-toluyl ylmethyl; 2-toluyl ylmethyl; 3-toluyl ylmethyl; 2; 4-dimethylbenzoyl methyl; 2; 3-dimethylbenzoyl methyl; 2; 6-dimethylbenzoyl methyl; 3; 5-dimethylbenzoyl methyl; 2; 5-dimethylbenzoyl methyl; 2; 4; 6-trimethylbenzoyl methyl; 3; 5-two trifluoromethyl benzoyl methyl; 2; 3; 4; 5; 6-penta fluoro benzene formyl radical methyl; 4-isopropoxy benzoyl methyl; 4-n-butoxy benzoyl methyl; 4-anisoyl methyl; 2-anisoyl methyl; 3-anisoyl methyl; 2; 4-dimethoxy benzoyl methyl; 2; 3-dimethoxy benzoyl methyl; 2; 6-dimethoxy benzoyl methyl; 3; 5-dimethoxy benzoyl methyl; 2; 5-dimethoxy benzoyl methyl; 2; 4; 6-trimethoxy benzoyl methyl; 3,5-two trifluoromethoxy benzoyl methyl; 2-isopropoxy benzoyl methyl; 3-chloro-4-anisoyl methyl; 2-chloro-4-trifluoromethoxy benzoyl methyl; 3-methyl-4-fluorobenzoyl ylmethyl; 4-bromo-3-trifluoromethyl benzoyl methyl; 2-trifluoromethyl benzoyl methyl; 3-trifluoromethyl benzoyl methyl; 4-trifluoromethyl benzoyl methyl; 2-pentafluoroethyl group benzoyl methyl; 3-pentafluoroethyl group benzoyl methyl; 4-pentafluoroethyl group benzoyl methyl; 2-trifluoromethoxy benzoyl methyl; 3-trifluoromethoxy benzoyl methyl; 4-trifluoromethoxy benzoyl methyl; 2-five fluorine phenetole formyl radical methyl; 3-five fluorine phenetole formyl radical methyl; 4-five fluorine phenetole formyl radical methyl; 2-(2-trifluoromethyl benzoyl) ethyl; 2-(3-trifluoromethyl benzoyl) ethyl; 2-(4-trifluoromethyl benzoyl) ethyl; 2-(2-trifluoromethoxy benzoyl) ethyl; 2-(3-trifluoromethoxy benzoyl) ethyl; 2-(4-trifluoromethoxy benzoyl) ethyl; 2-(2-five fluorine phenetole formyl radicals) ethyl; 2-(3-five fluorine phenetole formyl radicals) ethyl; 2-(4-five fluorine phenetole formyl radicals) ethyl; 3-(2-trifluoromethyl benzoyl) propyl group; 3-(3-trifluoromethyl benzoyl) propyl group; 3-(4-trifluoromethyl benzoyl) propyl group; 3-(2-trifluoromethoxy benzoyl) propyl group; 3-(3-trifluoromethoxy benzoyl) propyl group; 3-(4-trifluoromethoxy benzoyl) propyl group; 3-(3-five fluorine phenetole formyl radicals) propyl group; 3-(4-five fluorine phenetole formyl radicals) propyl group; 4-(3-five fluorine phenetole formyl radicals) butyl; 5-(4-trifluoromethyl benzoyl) amyl group; 4-(4-trifluoromethyl benzoyl) amyl group; 4-(4-trifluoromethoxy benzoyl) amyl group; 6-(3-trifluoromethyl benzoyl) hexyl; 6-(4-trifluoromethyl benzoyl) hexyl; 6-(4-trifluoromethoxy benzoyl) hexyl etc.

(described substituting group is selected from the alkyl by C1-C6 to the amino that can be replaced by at least one group, C1-C6 alkoxy carbonyl and phenyl C1-C6 alkyl are [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by phenyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed), halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group] group formed) comprise the amino that can be replaced by 1 or 2 substituting group, described substituting group is selected from by as above or the described straight or branched alkyl that contains 1 to 6 carbon atom in back, contain the straight or branched alkoxy carbonyl of 1 to 6 carbon atom and at the phenylalkyl that has the straight or branched alkyl that contains 1 to 6 carbon atom on the alkyl [wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 substituting group, it is selected from by phenyl (wherein on this phenyl, can be substituted with 1 to 5, preferred 1 to 3 substituting group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 straight or branched alkyl and the group that halogen replaces or unsubstituted C1-C6 straight or branched alkoxyl group is formed), halogen atom, halogen replaces or unsubstituted C1-C6 straight or branched alkyl and halogen replaces or unsubstituted C1-C6 straight or branched alkoxyl group is formed group] group formed, for example amino, tert-butoxycarbonyl amino, methylamino, benzylamino, (4-trifluoro-methoxybenzyl) amino, (4-trifluoromethyl benzyl) amino, (4-benzyl chloride base) amino, (4-(4-Trifluoromethoxyphen-l) benzyl) amino, (4-(4-trifluoromethyl) benzyl) amino, (4-(4-chloro-phenyl-) benzyl) amino, N-methyl-N-benzylamino, N-methyl-N-(4-trifluoro-methoxybenzyl) amino, N-methyl-N-(4-trifluoromethyl benzyl) amino, N-methyl-N-(4-benzyl chloride base) amino, N-methyl-N-(4-(4-Trifluoromethoxyphen-l) benzyl) amino, N-methyl-N-(4-(4-trifluoromethyl) benzyl) amino, N-methyl-N-(4-(4-chloro-phenyl-) benzyl) amino, N-methoxycarbonyl-N-benzylamino, N-ethoxy carbonyl-N-(4-trifluoro-methoxybenzyl) amino, N-propoxycarbonyl-N-(4-trifluoromethyl benzyl) amino, N-n-butoxy carbonyl-N-(4-benzyl chloride base) amino, N-n-pentyloxy carbonyl-N-(4-(4-Trifluoromethoxyphen-l) benzyl) amino, positive hexyloxy carbonyl-the N-of N-(4-(4-trifluoromethyl) benzyl) amino, N-ethoxy carbonyl-N-(4-(4-chloro-phenyl-) benzyl) amino, N, the N-dimethylamino, N-methyl-N-ethylamino etc.

[described substituting group is selected from by C1-C6 alkyl and phenyl (wherein on this benzyl ring the amino C1-C6 alkyl that can be replaced by at least one group, can be substituted with at least one group, it is selected from by halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group) group formed] comprise aminoalkyl group, on this moieties, has the straight or branched alkyl that contains 1 to 6 carbon atom, it can be replaced by 1 or 2 substituting group, described substituting group is selected from by the straight or branched alkyl that contains 1 to 6 carbon atom and phenyl (wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 substituting group, it is selected from by halogen atom, halogen replaces or unsubstituted C1-C6 straight or branched alkyl and halogen replaces or unsubstituted C1-C6 straight or branched alkoxyl group is formed group) group formed] comprise for example amino methyl, the 2-amino-ethyl, the 1-amino-ethyl, the 3-aminopropyl, the amino butyl of 4-, the amino amyl group of 5-, the amino hexyl of 6-, 2-methyl-3-aminopropyl, 1,1-dimethyl-2-amino-ethyl, the ethylamino methyl, 1-(propyl group amino) ethyl, 2-(methylamino) ethyl, 3-(sec.-propyl amino) propyl group, 4-(normal-butyl amino) butyl, 5-(n-pentyl amino) amyl group, 6-(n-hexyl amino) hexyl, dimethylaminomethyl, (N-ethyl-N-propyl group amino) methyl, 2-(N-methyl-N-n-hexyl amino) ethyl, the phenyl amino methyl, 1-(phenyl amino) ethyl, 2-(4-chlorobenzene amino) ethyl, 2-(4-trifluoromethoxy phenylamino) ethyl, 2-(4-trifluoromethyl phenylamino) ethyl, 3-(4-fluoroanilino) propyl group, 4-(3,4-two fluoroanilino) butyl, 5-(3,4,6-trifluoro-benzene amino) amyl group, 6-(4-methylbenzene amino) hexyl, (3-anisole amino) methyl, (2,3,4-trimethoxy phenylamino) methyl, (3, the 4-xylidino) methyl, (2,4, the 6-trimethylanilino) methyl, (N-ethyl-N-(3,4-dimethoxy phenylamino)) methyl, 2-(N-methyl-N-(4-chlorobenzene amino)) ethyl, 2-(N-methyl-N-(4-trifluoromethoxy phenylamino)) ethyl, 2-(N-methyl-N-(4-trifluoromethyl phenylamino)) ethyl etc.

Benzofuryl C2-C6 thiazolinyl is [wherein on this cumarone ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group] comprise the benzofuryl thiazolinyl, on this alkenyl part, has the straight or branched thiazolinyl that contains 2 to 6 carbon atoms, and has 1 to 3 two key, comprise that trans and cis form is [wherein on this cumarone ring, can be substituted with 1 to 3 substituting group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 straight or branched alkyl and the group that halogen replaces or unsubstituted C1-C6 straight or branched alkoxyl group is formed], 2-((2-for example, 3-, 4-, 5-, 6-or 7-) benzofuryl) vinyl, 3-((2-, 3-, 4-, 5-, 6-or 7-) benzofuryl)-the 2-2-propenyl, 3-((2-, 3-, 4-, 5-, 6-or 7-) benzofuryl)-2-methyl-2-propenyl, 4-((2-, 3-, 4-, 5-, 6-or 7-) benzofuryl)-crotyl, 4-((2-, 3-, 4-, 5-, 6-or 7-) benzofuryl-3-butenyl, 4-((2-, 3-, 4-, 5-, 6-or 7-) benzofuryl)-1, the 3-butadienyl, 5-((2-, 3-, 4-, 5-, 6-or 7-) benzofuryl)-1,3,5-hexatriene base, 5-((2-, 3-, 4-, 5-, 6-or 7-) benzofuryl)-2, the 4-hexadienyl, 5-((2-, 3-, 4-, 5-, 6-or 7-) benzofuryl)-the 3-pentenyl, 3-(5-trifluoromethyl-(2-, 3-, 4-, 6-or 7-) benzofuryl)-the 2-propenyl, 3-(6-trifluoromethoxy-(2-, 3-, 4-, 5-or 7-) benzofuryl) the 2-propenyl, 3-(6-trifluoromethyl-(2-, 3-, 4-, 5-or 7-) benzofuryl)-the 2-propenyl, 3-(4-chloro-(2-, 3-, 5-, 6-or 7-) benzofuryl)-the 2-propenyl, 3-(4,5-dimethoxy-(2-, 3-, 6-or 7-) benzofuryl)-the 2-propenyl, 3-(3,4,5-trimethylammonium-(2-, 6-or 7-) benzofuryl)-the 2-propenyl, 3-(3-methyl-5-methoxyl group-(2-, 4-, 6-or 7-) benzofuryl)-the 2-propenyl etc., comprise that the benzofuryl thiazolinyl is (wherein on this cumarone ring, can be substituted with 1 to 3 and be selected from following substituting group: halogen atom, halogen replacement or unsubstituted C1-C6 straight or branched alkyl and the group that halogen replaces or unsubstituted C1-C6 straight or branched alkoxyl group is formed), comprise trans or the cis form.

Piperidyl is [wherein on this piperidine ring, can be substituted with at least one phenyl C2-C6 thiazolinyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed)] comprise that piperidyl is [wherein on this piperidine ring, can be substituted with 1 to 3 aforesaid phenyl thiazolinyl, it has the straight or branched thiazolinyl that contains 2 to 6 carbon atoms on this alkenyl part, and has 1 to 3 two key, comprise that trans and cis form is (wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 substituting group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 straight or branched alkyl and the group that halogen replaces or unsubstituted C1-C6 straight or branched alkoxyl group is formed)], (1-for example, 2-, 3-or 4-) piperidyl, 1-(3-phenyl-2-propenyl)-(2-, 3-or 4-) piperidyl, 1,3-two (3-phenyl-2-propenyl)-(2-, 4-, 5-or 6-) piperidyl, 1,2,4-three (3-phenyl-2-propenyl)-(3-, 5-or 6-) piperidyl, 1-(3-(4-Trifluoromethoxyphen-l)-2-propenyl)-(2-, 3-or 4-) piperidyl, 1-(3-(4-trifluoromethyl)-2-propenyl)-(2-, 3-or 4-) piperidyl, 1-(3-(4-chloro-phenyl-)-2-propenyl)-(2-, 3-or 4-) piperidyl, (3-(3 for 1-, the 4-Dimethoxyphenyl)-the 2-propenyl)-(2-, 3-or 4-) piperidyl, (3-(2 for 1-, 4, the 6-trimethylphenyl)-the 2-propenyl)-2 (2-, 3-or 4-) piperidyl etc.

The C1-C6 alkyl that ferrocene replaces comprises the ferrocene alkyl, it has the straight or branched alkyl that contains 1 to 6 carbon atom on this moieties, for example ferrocene methyl, 1-ferrocene ethyl, 2-ferrocene ethyl, 3-ferrocene propyl group, 2-ferrocene propyl group, 4-ferrocene butyl, 5-ferrocene amyl group, 4-ferrocene amyl group, 6-ferrocene hexyl, 1,1-dimethyl-2-ferrocene ethyl, 2-methyl-3-ferrocene propyl group etc.

Indyl C1-C6 alkyl (wherein on this indole ring, can be substituted with at least one halogen atom) comprises indolyl alkyl, has the straight or branched alkyl (wherein on this indole ring, can be substituted with 1 to 3 halogen atom) that contains 1 to 6 carbon atom on this moieties, for example ((1-, 2-, 3-, 4-, 5-, 6-or 7-) indyl) methyl, 1-((1-, 2-, 3-, 4-, 5-, 6-or 7-) indyl) ethyl, 2-((1-, 2-, 3-, 4-, 5-, 6-or 7-) indyl) ethyl, 3-((1-, 2-, 3-, 4-, 5-, 6-or 7-) indyl) propyl group, 2-((1-, 2-, 3-, 4-, 5-, 6-or 7-) indyl) propyl group, 4-((1-, 2-, 3-, 4-, 5-, 6-or 7-) indyl) butyl, 5-((1-, 2-, 3-, 4-, 5-, 6-or 7-) indyl) amyl group, 4-((1-, 2-, 3-, 4-, 5-, 6-or 7-) indyl) amyl group, 6-((1-, 2-, 3-, 4-, 5-, 6-or 7-) indyl) hexyl, 1,1-dimethyl-2-((1-, 2-, 3-, 4-, 5-, 6-or 7-) indyl) ethyl, 2-methyl-3-((1-, 2-, 3-, 4-, 5-, 6-or 7-) indyl) propyl group, (5-chloro-(1-, 2-, 3-, 4-, 6-or 7-) indyl) methyl, (5,6-two fluoro-(1-, 2-, 3-, 4-or 7-) indyl) methyl, (3,5,6-three bromo-(1-, 2-, 4-or 7-) indyl) methyl etc.

Phenyl C2-C6 alkynyl comprises the phenyl alkynyl, on this alkynyl part, has the straight or branched alkynyl that contains 2 to 6 carbon atoms, for example 2-phenylacetylene base, 3-phenyl-2-propynyl, 3-phenyl-1-methyl-2-propynyl, 4-phenyl-2-butyne base, 4-phenyl-3-butynyl, 4-phenyl-ethyl acetylene base, 5-phenyl-valerylene base, 6-phenyl-2-hexin base etc.

The C1-C6 alkyl of naphthyl substituted is (wherein on this naphthalene nucleus, can be substituted with at least one C1-C6 alkoxyl group) comprise the alkyl of naphthyl substituted, have on this moieties contain 1 to 6 carbon atom the straight or branched alkyl (wherein on this naphthalene nucleus, can be substituted with 1 to 3 above-mentioned straight or branched alkoxyl group that contains 1 to 6 carbon atom), (1-or 2-) naphthyl for example) methyl, 1-((1-or 2-) naphthyl) ethyl, 2-((1-or 2-) naphthyl) ethyl, 3-((1-or 2-) naphthyl) propyl group, 2-((1-or 2-) naphthyl) propyl group, 4-((1-or 2-) naphthyl) butyl, 5-((1-or 2-) naphthyl) amyl group, 4-((1-or 2-) naphthyl) amyl group, 6-((1-or 2-) naphthyl) hexyl, 1,1-dimethyl-2-((1-or 2-) naphthyl) ethyl, 2-methyl-3-((1-or 2-) naphthyl) propyl group, (6-methoxyl group-(1-, 2-, 3-, 4-, 5-, 7-or 8-) naphthyl) methyl, (5,6-dimethoxy-(1-, 2-, 3-, 4-, 7-or 8-) naphthyl) methyl, (5,6,7-trimethoxy-(1-, 2-, 3-, 4-or 8-) naphthyl) methyl etc.

Benzothiazolyl group (wherein the benzothiazole ring, may be substituted with at least one group, The selected (b-1) phenyl [wherein the phenyl ring may be substituted with at least one group which is Selected from a halogen atom, a halogen substituted or unsubstituted C1-C6 alkyl group and a halogen-substituted or unsubstituted C1-C6 alkoxy group], (b-2) piperazinyl (piperadinyl group) [wherein in the Piperazine ring, may be substituted with at least one group which is selected from phenyl C1-C6 alkyl (wherein the The phenyl ring may be substituted with at least one group selected from the group consisting of a halogen atom, a halogen substituted or Unsubstituted C1-C6 alkyl group and a halogen-substituted or unsubstituted C1-C6 alkoxy group), benzene C2-C6 alkenyl group (wherein the phenyl ring may be substituted with at least one group which is selected from A halogen atom, a halogen substituted or unsubstituted C1-C6 alkyl group and a halogen-substituted or unsubstituted C1-C6 alkoxy The group consisting of alkoxy), and phenyl (wherein the phenyl ring may be substituted with at least one group, Selected from the group consisting of a halogen atom, a halogen substituted or unsubstituted C1-C6 alkyl group and a halogen-substituted or unsubstituted C1-C6 alkoxy group) from the group consisting], (b-3) piperidyl group [wherein the piperidine ring, May be substituted with at least one group selected from the free amino group (wherein the amino group, may be substituted With at least one group which is selected from phenyl group [wherein the phenyl ring may be substituted with at least one A group selected from the group consisting of a halogen atom, a halogen substituted or unsubstituted C1-C6 alkyl group and a halogen substituted or Unsubstituted C1-C6 alkoxy group] and a C1-C6 alkyl groups), a phenoxy group (wherein In the phenyl ring may be substituted with at least one group selected from the group consisting of a halogen atom, a halogen-substituted Unsubstituted C1-C6 alkyl and halogen-substituted or unsubstituted C1-C6 alkoxy group), and Phenyl C1-C6 alkyl group (wherein the phenyl ring may be substituted with at least one group selected from A halogen atom, a halogen substituted or unsubstituted C1-C6 alkyl group and a halogen-substituted or unsubstituted C1-C6 Alkoxy group) from the group consisting], (b-4) pyrrolyl group [wherein the pyrrole ring, can be taken Generation of at least one group which is selected from C1-C6 alkyl and phenyl C1-C6 alkyl group (wherein the phenyl Base ring may be substituted with at least one group selected from the group consisting of a halogen atom, a halogen substituted or unsubstituted Substituted C1-C6 alkyl group and a halogen-substituted or unsubstituted C1-C6 alkoxy group) consisting of Group] And (b-5) phenylthio group (wherein the phenyl ring may be substituted with at least one group selected from A halogen atom, a halogen substituted or unsubstituted C1-C6 alkyl group and a halogen-substituted or unsubstituted C1-C6 Alkoxy group) consisting of group) include benzothiazole group (wherein the benzothiazole ring , It can be substituted with 1 to 3 substituents selected from the following: (b-1) phenyl group (wherein the phenyl ring , It can be substituted with 1 to 5, preferably 1 to 3 substituents selected from: a halogen atom, a halogen Substituted or unsubstituted C1-C6 alkyl group and a halogen-substituted or unsubstituted C1-C6 alkoxy group consisting of Group), (b-2) piperazinyl group [wherein the piperazine ring may be substituted with 1 to 3 substituents Selected from C1-C6 alkyl phenyl (wherein the phenyl ring may be substituted with 1 to 5, preferably 1 To 3 substituents selected from the group consisting of a halogen atom, a halogen substituted or unsubstituted C1-C6 alkyl and halo Substituted or unsubstituted C1-C6 alkoxy group), as described later, phenyl C2-C6 alkenyl group (In which the alkenyl moiety having from 2 to 6 containing carbon atoms, a straight-chain or branched alkenyl group having from 1 to 3 Of the double bond, including trans-and cis-form) (wherein the phenyl ring may be substituted with 1 to 5 , Preferably 1 to 3 substituents selected from the group consisting of a halogen atom, a halogen substituted or unsubstituted C1-C6 Alkyl and halogen-substituted or unsubstituted C1-C6 alkoxy group) and a phenyl group as described above, (Wherein the phenyl ring may be substituted with 1 to 5, preferably 1 to 3 substituents, selected from A halogen atom, a halogen substituted or unsubstituted C1-C6 alkyl group and a halogen-substituted or unsubstituted C1-C6 Alkoxy group) from the group consisting], (b-3) piperidyl group [wherein the piperidine ring, and can be taken Generation of from 1 to 3 substituents, selected from the free amino group (wherein the amino group may be substituted with 1 or 2 A group selected from a phenyl group [wherein the phenyl ring may be substituted with 1 to 5, preferably 1 to 3 Substituents selected from the group consisting of a halogen atom, a halogen substituted or unsubstituted C1-C6 alkyl and halo-substituted Unsubstituted C1-C6 alkoxy group consisting of], and 1 or 2 groups selected from C1-C6 alkyl group), benzene Group (wherein the phenyl ring may be substituted with 1 to 5, preferably 1 to 3 substituents, which Selected from a halogen atom, a halogen substituted or unsubstituted C1-C6 alkyl group and a halogen-substituted or unsubstituted C1-C6 alkoxy group) and a phenyl C1-C6 alkyl group (wherein the phenyl ring, can be taken Generation of from 1 to 5, preferably 1 to 3 substituents selected from a halogen atom, a halogen substituted or unsubstituted A C1-C6 alkyl group and a halogen-substituted or unsubstituted C1-C6 alkoxy group) consisting of Group] (B-4) pyrrolyl group as described later [wherein the pyrrole ring may be substituted with 1 to 3 substituents Group, which is selected from C1-C6 alkyl and phenyl C1-C6 alkyl group (wherein the phenyl ring, can be taken Generation of from 1 to 5, preferably 1 to 3 substituents selected from a halogen atom, a halogen substituted or unsubstituted A C1-C6 alkyl group and a halogen-substituted or unsubstituted C1-C6 alkoxy group) consisting of Group] And (b-5) as described later phenyl group (wherein the phenyl ring may be substituted with 1 to 5, Preferably 1 to 3 substituents selected from the group consisting of a halogen atom, a halogen substituted or unsubstituted C1-C6 alkyl and Halogen-substituted or unsubstituted C1-C6 alkoxy group) consisting of the group), e.g., 2 - benzothiazolyl Yl group, a 4 - benzothiazolyl group, a 5 - benzothiazolyl group, a 6 - benzothiazolyl group 7 - benzo Thiazolyl group, a 2 - (1 - piperazinyl) -4 - benzothiazole group, a 2 - (4 - benzyl-1 - piperazinyl) -4 - Benzothiazolyl group, a 2 - (3,4 - dibenzyl-1 - piperazinyl) -4 - benzothiazole group, a 5 - (2,3,4 - Tribenzyl-1 - piperazinyl) -2 - benzothiazolyl group, a 4 - (4 - (2 - phenylethyl) -1 - piperazinyl) -2 - Benzothiazolyl group, a 4 - (4 - (3 - phenyl-propyl) -1 - piperazinyl) -5 - benzothiazole group, 4 - (4 - (4 - phenylbutyl) -1 - piperazinyl) -6 - benzothiazole group, a 4 - (4 - (5 - phenyl-pentyl Yl) -1 - piperazinyl) -7 - benzothiazole group, a 2 - (4 - (6 - phenyl-hexyl)-1 - piperazinyl) -4 - phenyl Benzothiazole group, a 4 - (4 - (2 - fluorobenzyl)-1 - piperazinyl) -2 - benzothiazolyl group, a 2 - (4 - (3 - Fluorobenzyl)-1 - piperazinyl) -4 - benzothiazole group, a 2 - (4 - (4 - fluorobenzyl)-1 - piperazinyl) -5 - Benzothiazolyl group, a 2 - (4 - (2 - chloro-benzyl) -1 - piperazinyl) -6 - benzothiazole group, a 2 - (4 - (3 - Chlorobenzyl) -1 - piperazinyl) -7 - benzothiazole group, a 5 - (4 - (4 - chlorobenzyl) -1 - piperazinyl) -4 - Benzothiazolyl group, a 6 - (4 - (2,3 - dichloro-benzyl) -1 - piperazinyl) -4 - benzothiazole group, 7 - (4 - (2,4 - dichloro-benzyl) -1 - piperazinyl) -4 - benzothiazole group, a 2 - (4 - (3,4 - dichloro-benzyl Yl)-1 - piperazinyl) -4 - benzothiazole group, a 4 - (4 - (3,5 - dichloro-benzyl) -1 - piperazinyl) -2 - Benzothiazolyl group, a 4 - (4 - (3,4,5 - trichloro-benzyl)-1 - piperazinyl) -5 - benzothiazole group, 4 - (4 - (2,3,4,5,6 - pentafluoro-benzyl)-1 - piperazinyl) -2 - benzothiazolyl group, a 4 - (4 - (2 - Three Fluorine-methylbenzyl)-1 - piperazinyl) -6 - benzothiazole group, a 4 - (4 - (3 - (trifluoromethyl) benzyl) -1 - -Piperazinyl) -7 - benzothiazole group, a 2 - (4 - (4 - (trifluoromethyl) benzyl)-1 - piperazinyl) -4 - benzo Thiazolyl group, a 5 - (4 - (4 - methylbenzyl)-1 - piperazinyl) -4 - benzothiazole group, a 6 - (4 - (3,4 - Dimethylbenzyl)-1 - piperazinyl) -4 - benzothiazolyl group, 7 - (4 - (2,4,6 - trimethyl-benzyl Yl)-1 - piperazinyl) -4 - benzothiazole group, a 4 - (4 - (2 - pentafluoroethyl-benzyl) - 1-piperazinyl Yl) -2 - benzothiazolyl group, a 4 - (4 - (3 - pentafluoroethyl-benzyl) - 1-piperazinyl)-5 - benzothiazole Group, a 4 - (4 - (4 - benzyl-pentafluoroethyl)-1 - piperazinyl) -6 - benzothiazole group, a 4 - (4 - (2 - Trifluoromethoxy-benzyl) - 1-piperazinyl)-7 - benzothiazole group, a 5 - (4 - (3 - (Trifluoromethoxy) benzyl Yl)-1 - piperazinyl) -4 - benzothiazole group, a 6 - (4 - (4 - trifluoromethoxy-benzyl) - 1-piperazinyl Yl) -5 - benzothiazolyl group, 7 - (4 - (4 - methoxybenzyl)-1 - piperazinyl) -5 - benzothiazole oxygen Group, 6 - (4 - (3,4 - dimethoxy-benzyl) -1 - piperazinyl) -4 - benzothiazole group, 7 - (4 - (2,4,6 - trimethoxybenzyl)-1 - piperazinyl) -4 - benzothiazole group, a 5 - (4 - (2 - Five Fluoro-ethoxy-benzyl) - 1-piperazinyl)-4 - benzothiazole group, a 4 - (4 - (3 - benzyloxy pentafluoroethoxy Yl)-1 - piperazinyl) -2 - benzothiazolyl group, a 6 - (4 - (4 - pentafluoro-ethoxy-benzyl) - 1-piperazinyl Yl) -4 - benzothiazole group, a 4 - (4 - (2 - (4 - trifluoromethoxy-phenyl)-ethyl) - 1-piperazinyl Yl) -2 - benzothiazolyl group, a 4 - (4 - (3 - (4 - trifluoromethoxy-phenyl) propyl) - 1-piperazinyl Yl) -2 - benzothiazolyl group, a 4 - (4 - (4 - (4 - trifluoromethoxy-phenyl) butyl) - 1-piperazinyl Yl) -2 - benzothiazolyl group, a 4 - (4 - (5 - (4 - trifluoromethoxyphenyl) pentyl) - 1-piperazinyl Yl) -2 - benzothiazolyl group, a 4 - (4 - (6 - (4 - trifluoromethoxyphenyl) hexyl) - 1-piperazinyl Yl) -2 - benzothiazolyl group, a 4 - (4 - (2 - (4 - (trifluoromethyl) phenyl) ethyl)-1 - piperazinyl) -2 - Benzothiazolyl group, a 5 - (4 - (3 - (4 - (trifluoromethyl) phenyl) propyl) -1 - piperazinyl) -2 - benzothiazol Yl group, a 6 - (4 - (4 - (4 - (trifluoromethyl) phenyl) butyl) - 1-piperazinyl)-2 - benzothiazolyl group, 7 - (4 - (5 - (4 - (trifluoromethyl) phenyl) pentyl)-1 - piperazinyl) -2 - benzothiazolyl group, 5 - (4 - (6 - (4 - (trifluoromethyl) phenyl) hexyl)-1 - piperazinyl) -2 - benzothiazolyl group, 2 - (4 - (trifluoro-methoxy-1 - piperidinyl)) -6 - benzothiazole group, a 2 - (4 - (trifluoromethyl Alkoxy benzyl-1 - piperidinyl)) -6 - benzothiazole group, 2 - (4 - (N-ethyl-N-(4 - chlorophenyl) Amino) -1 - piperidinyl) -6 - benzothiazole group, a 2 - phenyl-5 - benzothiazolyl group, a 2 - (4 - chloro- Phenyl) -5 - benzothiazole group, a 2 - (4 - trifluoromethoxy-phenyl) -6 - benzothiazole group, a 2 - (3 - Trifluoromethyl-phenyl) -5 - benzothiazole group, a 2 - (1 - piperidinyl) -4 - benzothiazole group, a 2 - (4 - Benzyl-1 - piperidinyl) -4 - benzothiazole group, a 2 - (3,4 - dibenzyl-1 - piperidinyl) -4 - benzothiazol Yl group, a 5 - (2,3,4 - tribenzyl-1 - piperidinyl)-2 - benzothiazolyl group, a 4 - (4 - (2 - phenylethyl Yl) -1 - piperidinyl)-2 - benzothiazolyl group, a 4 - (4 - (3 - phenyl-propyl) -1 - piperidinyl) -5 - phenyl Benzothiazole group, a 4 - (4 - (4 - phenylbutyl)-1 - piperidinyl) -6 - benzothiazole group, a 4 - (4 - (5 - Phenyl-pentyl)-1 - piperidinyl) -7 - benzothiazole group, a 2 - (4 - (6 - phenylhexyl) -1 - piperidine Yl) -4 - benzothiazole group, a 4 - (4 - (2 - fluorobenzyl)-1 - piperidinyl)-2 - benzothiazolyl group, 2 - (4 - (3 - fluorobenzyl)-1 - piperidinyl) -4 - benzothiazole group, a 2 - (4 - (4 - fluorobenzyl) -1 - piperazine Piperidyl) -5 - benzothiazole group, a 2 - (4 - (2 - chloro-benzyl) -1 - piperidinyl) -6 - benzothiazole group, 2 - (4 - (3 - chloro-benzyl) -1 - piperidinyl) -7 - benzothiazole group, a 5 - (4 - (4 - chlorobenzyl) - piperazine Piperidinyl) -4 - benzothiazole group, a 6 - (4 - (2,3 - dichloro-benzyl-1 - piperidinyl) -4 - benzothiazole oxygen Group, 7 - (4 - (2,4 - dichloro-benzyl) -1 - piperidinyl) -4 - benzothiazole group, a 2 - (4 - (3,4 - Chlorobenzyl) -1 - piperidinyl) -4 - benzothiazole group, a 4 - (4 - (3,5 - dichloro-benzyl) -1 - piperidine Yl) -2 - benzothiazolyl group, a 4 - (4 - (3,4,5 - trichloro-benzyl)-1 - piperidinyl) -5 - benzothiazole Group, a 4 - (4 - (2,3,4,5,6 - pentafluoro-benzyl)-1 - piperidinyl)-2 - benzothiazolyl group, 4 - (4 - (2 - (trifluoromethyl) benzyl) -1 - piperidinyl) -6 - benzothiazole group, a 4 - (4 - (3 - trifluoromethyl Benzyl) -1 - piperidinyl) -7 - benzothiazole group, a 2 - (4 - (4 - (trifluoromethyl) benzyl) -1 - piperidine Yl) -4 - benzothiazole group, a 5 - (4 - (4 - methylbenzyl)-1 - piperidinyl) -4 - benzothiazole group, 6 - (4 - (3,4 - dimethylbenzyl)-1 - piperidinyl) -4 - benzothiazolyl group, 7 - (4 - (2,4,6 - Methylbenzyl)-1 - piperidinyl) -4 - benzothiazole group, a 4 - (4 - (2 - benzyl-pentafluoroethyl) -1 - piperazine Piperidinyl)-2 - benzothiazolyl group, a 4 - (4 - (3 - pentafluoroethyl benzyl) -1 - piperidinyl) -5 - benzothiazol Yl group, a 4 - (4 - (4 - benzyl-pentafluoroethyl)-1 - piperidinyl) -6 - benzothiazole group, a 4 - (4 - (2 - Trifluoromethoxy-benzyl)-1 - piperidinyl) -7 - benzothiazole group, a 5 - (4 - (3 - (Trifluoromethoxy) benzyl Yl) -1 - piperidinyl) -4 - benzothiazole group, a 6 - (4 - (4 - (Trifluoromethoxy) benzyl) -1 - piperidine Yl) -5 - benzothiazolyl group, 7 - (4 - (4 - methoxybenzyl)-1 - piperidinyl) -5 - benzothiazole oxygen Group, 6 - (4 - (3,4 - dimethoxy-benzyl) -1 - piperidinyl) -4 - benzothiazole group, 7 - (4 - (2,4,6 - trimethoxybenzyl) -1 - piperidinyl) -4 - benzothiazole group, a 5 - (4 - (2 - Five Fluoro-ethoxy benzyl)-1 - piperidinyl) -4 - benzothiazole group, a 4 - (4 - (3 - benzyloxy pentafluoroethoxy Yl) -1 - piperidinyl)-2 - benzothiazolyl group, a 6 - (4 - (4 - benzyl-1 pentafluoroethoxy - piperidine Yl) -4 - benzothiazole group, a 4 - (4 - (2 - (4 - trifluoromethoxy-phenyl)-ethyl) -1 - piperidine Yl) -2 - benzothiazolyl group, a 4 - (4 - (3 - (4 - trifluoromethoxy-phenyl) propyl) -1 - piperidine Yl) -2 - benzothiazolyl group, a 4 - (4 - (4 - (4 - trifluoromethoxy-phenyl)-butyl) -1 - piperidine Yl) -2 - benzothiazolyl group, a 4 - (4 - (5 - (4 - trifluoromethoxyphenyl) pentyl)-1 - piperidine Yl) -2 - benzothiazolyl group, a 4 - (4 - (6 - (4 - trifluoromethoxyphenyl) hexyl)-1 - piperidine Yl) -2 - benzothiazolyl group, a 4 - (4 - (2 - (4 - (trifluoromethyl) phenyl) ethyl) -1 - piperidinyl) -2 - Benzothiazolyl group, a 5 - (4 - (3 - (4 - (trifluoromethyl) phenyl) propyl) -1 - piperidinyl) -2 - benzothiazol Yl group, a 6 - (4 - (4 - (4 - (trifluoromethyl) phenyl) butyl)-1 - piperidinyl)-2 - benzothiazolyl group, 7 - (4 - (5 - (4 - (trifluoromethyl) phenyl) pentyl)-1 - piperidinyl)-2 - benzothiazolyl group, 5 - (4 - (6 - (4 - (trifluoromethyl) phenyl) hexyl)-1 - piperidinyl)-2 - benzothiazolyl group, a 2 - (4 - Phenoxy-1 - piperidinyl) -4 - benzothiazole group, a 2 - (3,4 - diphenyl-1 - piperidinyl) -4 - Benzothiazolyl group, a 5 - (2,3,4 - triphenyl-1 - piperidinyl)-2 - benzothiazolyl group, 4 - (4 - (2 - fluorophenoxy)-1 - piperidinyl)-2 - benzothiazolyl group, a 2 - (4 - (3 - fluorophenoxy Yl) -1 - piperidinyl) -4 - benzothiazole group, a 2 - (4 - (4 - fluorophenoxy)-1 - piperidinyl) -5 - phenyl Benzothiazole group, a 2 - (4 - (2 - chlorophenoxy) -1 - piperidinyl) -6 - benzothiazole group, a 2 - (4 - (3 - Chlorophenoxy) -1 - piperidinyl) -7 - benzothiazole group, a 5 - (4 - (4 - chlorophenoxy) -1 - piperidine Yl) -4 - benzothiazole group, a 6 - (4 - (2,3 - dichlorophenoxy)-1 - piperidinyl) -4 - benzothiazole Group, 7 - (4 - (2,4 - dichlorophenoxy)-1 - piperidinyl) -4 - benzothiazole group, a 2 - (4 - (3,4 - Dichlorophenoxy) -1 - piperidinyl) -4 - benzothiazole group, a 4 - (4 - (3,5 - dichlorophenoxy) -1 - Piperidinyl)-2 - benzothiazolyl group, a 4 - (4 - (3,4,5 - trichlorophenyl)-1 - piperidinyl) -5 - phenyl Benzothiazole group, a 4 - (4 - (2,3,4,5,6 - pentafluorophenoxy) -1 - piperidinyl) -2 - benzothiazole oxygen Yl, 4 - (4 - (2 - (trifluoromethyl) phenoxy) -1 - piperidinyl) -6 - benzothiazole group, a 4 - (4 - (3 - Trifluoromethylphenoxy)-1 - piperidinyl) -7 - benzothiazole group, a 2 - (4 - (4 - (trifluoromethyl) phenoxy Yl) -1 - piperidinyl) -4 - benzothiazole group, a 5 - (4 - (4 - methylphenoxy)-1 - piperidinyl) -4 - Benzothiazolyl group, a 6 - (4 - (3,4 - dimethoxy-phenoxy)-1 - piperidinyl) -4 - benzothiazole group, 7 - (4 - (2,4,6 - trimethoxy-phenoxy)-1 - piperidinyl) -4 - benzothiazole group, a 4 - (4 - (2 - Five Fluoro-phenoxy-ethyl)-1 - piperidinyl)-2 - benzothiazolyl group, a 4 - (4 - (3 - phenoxy pentafluoroethyl Yl) -1 - piperidinyl) -5 - benzothiazole group, a 4 - (4 - (4 - pentafluoroethyl-phenoxy) -1 - piperidine Yl) -6 - benzothiazole group, a 4 - (4 - (2 - (trifluoromethoxy) phenoxy) -1 - piperidinyl) -7 - benzo Thiazolyl group, a 5 - (4 - (3 - trifluoromethyl-methoxyphenoxy)-1 - piperidinyl) -4 - benzothiazole group, 6 - (4 - (4 - (trifluoromethoxy) phenoxy) -1 - piperidinyl) -5 - benzothiazolyl group, 7 - (4 - (4 - methyl Phenoxy)-1 - piperidinyl) -5 - benzothiazole group, a 6 - (4 - (3,4 - dimethoxy-phenoxy Yl) -1 - piperidinyl) -4 - benzothiazolyl group, 7 - (4 - (2,4,6 - trimethoxy-phenyl)-1 - piperazine Piperidinyl) -4 - benzothiazole group, a 5 - (4 - (2 - pentafluoroethoxy phenoxy)-1 - piperidinyl) -4 - phenyl Benzothiazole group, a 4 - (4 - (3 - pentafluoro-phenoxy-ethoxy)-1 - piperidinyl)-2 - benzothiazolyl group, 6 - (4 - (4 - pentafluoro-ethoxy-phenoxy)-1 - piperidinyl) -4 - benzothiazole group, 2,5,6 - triphenyl -7 - benzothiazolyl group, a 2 - (4 - amino-1 - piperidinyl) -6 - benzothiazole group, a 4 - (2,4 - Diamino-1 - piperidinyl)-2 - benzothiazolyl group, a 5 - (2,4,6 - triamino-1 - piperidinyl) -4 - Benzothiazolyl group, a 6 - (2 - amino-1 - piperidinyl) -5 - benzothiazolyl group, 7 - (3 - amino-1 - Piperidinyl) -6 - benzothiazole group, a 2 - (4 - methyl-1 - piperidinyl) -4 - benzothiazole group, 2 - (4 - ethyl-amino-1 - piperidinyl) -5 - benzothiazole group, a 2 - (4 - n-propyl-amino-1 - piperidinyl Yl) -6 - benzothiazole group, a 2 - (4 - dimethylamino-1 - piperidinyl) -7 - benzothiazole group, 2 - (4 - diethylamino-1 - piperidinyl) -4 - benzothiazole group, a 2 - (4 - II - n-propyl-amino-1 - Piperidyl) -5 - benzothiazole group, a 2 - (4 - phenyl-1 - piperidinyl) -6 - benzothiazole group, 2 - (4 - (N-phenyl-N-methyl-amino) -1 - piperidinyl) -7 - benzothiazole group, a 2 - (4 - (2 - fluorophenyl Ylamino)-1 - piperidinyl) -4 - benzothiazole group, a 2 - (4 - (3 - fluorophenyl)-1 - piperidine Yl) -5 - benzothiazole group, a 2 - (4 - (4 - fluorophenyl)-1 - piperidinyl) -6 - benzothiazole oxygen Group, 2 - (4 - (2 - chlorophenyl)-1 - piperidinyl) -7 - benzothiazole group, a 2 - (4 - (3 - chlorophenyl Ylamino)-1 - piperidinyl) -4 - benzothiazole group, a 2 - (4 - (4 - chlorophenyl)-1 - piperidine Yl) -5 - benzothiazole group, a 2 - (4 - (2,3 - dichlorophenyl)-1 - piperidinyl) -6 - benzothiazol Yl group, a 2 - (4 - (2,4,6 - trifluoro-phenylamino)-1 - piperidinyl) -7 - benzothiazole group, 2 - (4 - (2,4 - dichlorophenyl)-1 - piperidinyl) -4 - benzothiazole group, a 2 - (4 - (3,4 - Chlorophenyl)-1 - piperidinyl) -6 - benzothiazole group, a 4 - (3,5 - dichlorophenyl)-1 - Piperidyl) -5 - benzothiazole group, a 2 - (4 - (2,3,4,5,6 - pentafluorophenyl)-1 - piperidine Yl) -6 - benzothiazole group, a 2 - (4 - (2 - (trifluoromethyl) phenylamino)-1 - piperidinyl) -7 - benzo Thiazolyl group, a 2 - (4 - (2 - methyl-phenylamino)-1 - piperidinyl) -4 - benzothiazole group, 2 - (4 - (2,3 - dimethylphenyl)-1 - piperidinyl) -5 - benzothiazole group, a 2 - (4 - (2 - Three Trifluoromethylphenyl)-1 - piperidinyl) -6 - benzothiazole group, a 2 - (4 - (2,4,6 - trimethylbenzene Ylamino)-1 - piperidinyl) -7 - benzothiazole group, a 2 - (4 - (4 - (trifluoromethyl) phenylamino) -1 - Piperidinyl) -4 - benzothiazole group, a 2 - (4 - (2 - pentafluoroethyl phenylamino) -1 - piperidinyl) -5 - Benzothiazolyl group, a 2 - (4 - (3 - pentafluoroethyl phenylamino)-1 - piperidinyl) -5 - benzothiazole oxygen Group, 2 - (4 - (4 - pentafluoroethyl phenylamino)-1 - piperidinyl) -6 - benzothiazole group, a 2 - (4 - (2 - Trifluoromethoxy-phenylamino)-1 - piperidinyl) -7 - benzothiazole group, a 2 - (4 - (2 - methoxyphenyl Ylamino)-1 - piperidinyl) -4 - benzothiazole group, a 2 - (4 - (2,3 - dimethoxyphenyl ammonia Yl) -1 - piperidinyl) -5 - benzothiazole group, a 2 - (4 - (2,4,6 - trimethoxyphenyl)-1 - Piperidinyl) -6 - benzothiazole group, 2 - (4 - (N-methyl-N-(2,4,6 - trimethoxyphenyl ammonia Yl)) -1 - piperidinyl) -7 - benzothiazole group, 2 - (4 - (N-methyl-N-(3,4 - dimethylphenyl ammonium Yl)) -1 - piperidinyl) -4 - benzothiazole group, a 2 - (4 - (3 - (Trifluoromethoxy) phenylamino) -1 - Piperidyl) -5 - benzothiazole group, a 2 - (4 - (4 - trifluoromethoxy-phenylamino)-1 - piperidine Yl) -6 - benzothiazole group, a 2 - (4 - (2 - pentafluoroethoxy phenylamino)-1 - piperidinyl) -7 - benzene Benzothiazole group, a 2 - (4 - (3 - pentafluoro-ethoxyphenyl)-1 - piperidinyl) -4 - benzothiazole oxygen Group, 2 - (4 - (4 - pentafluoroethoxy phenylamino)-1 - piperidinyl) -5 - benzothiazole group, 2 - (4 - (2 - fluorophenyl)-1 - piperidinyl) -5 - benzothiazole group, a 4 - (3 - fluorophenyl ammonia Yl) -1 - piperidinyl) -6 - benzothiazole group, a 2 - (4 - (4 - fluorophenyl)-1 - piperidinyl) -7 - Benzothiazolyl group, a 2 - phenyl-5 - (4 - phenoxy-1 - piperidinyl) -7 - benzothiazole group, 2 - (1 - (4 - trifluoromethoxy-phenyl) - (2 - or 3 -) pyrrolyl) - (4 -, 5 -, 6 - or 7 -) benzothiazolyl Yl group, a 2 - (1 - methyl - (2 - or 3 -) pyrrolyl) - (4 -, 5 -, 6 - or 7 -) benzothiazolyl group, 2 - (4 - (3 - (4 - (trifluoromethyl) phenyl) -2 - propenyl) - (1 -, 2 - or 3 -) piperidyl) - (4 -, 5 -, 6 - or 7 -) benzothiazolyl group, 2 - (4 - (4 - trifluoromethoxyphenyl)) - (1 -, 2 - or 3 -)-piperidine Yl) - (4 -, 5 -, 6 - or 7 -) benzothiazolyl group, 2 - (4 - (4 - (trifluoromethyl) phenyl)) - (1 -, 2 - Or 3 -) piperidyl) - (4 -, 5 -, 6 - or 7 -) benzothiazolyl group, 2 - (4 - chlorophenyl thio) - (4 -, 5 -, 6 - or 7 -) benzothiazolyl group. ...

Phenyl C1-C6 alkylidene group is (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed) comprise that phenyl C1-C6 alkylidene group is (on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 substituting group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed), benzylidene for example, 1-phenyl ethylidene, 2-phenyl ethylidene, 3-phenyl propylidene, 2-phenyl propylidene, 4-phenyl butylidene, 5-phenyl pentylidene, 4-phenyl pentylidene, 6-phenyl hexylidene, 2-fluorine benzylidene, 3-fluorine benzylidene, 4-fluorine benzylidene, 2-chlorine benzylidene, 3-chlorine benzylidene, 4-chlorine benzylidene, 2-bromine benzylidene, 3-bromine benzylidene, 4-bromine benzylidene, 2-iodine benzylidene, 3-iodine benzylidene, 4-iodine benzylidene, 2,3-difluoro benzylidene, 3,4-difluoro benzylidene, 3,5-difluoro benzylidene, 2,4-difluoro benzylidene, 2,6-difluoro benzylidene, 2, the 3-dichlorin benzylidene, 3, the 4-dichlorin benzylidene, 3, the 5-dichlorin benzylidene, 2, the 4-dichlorin benzylidene, 2, the 6-dichlorin benzylidene, 2-fluoro-4-bromine benzylidene, 4-chloro-3-fluorine benzylidene, 2,3,4-trichlorine benzylidene, 3,4,5-trifluoro benzylidene, 2,4,6-trichlorine benzylidene, 4-sec.-propyl benzylidene, 4-normal-butyl benzylidene, 4-methyl benzylidene, 2-methyl benzylidene, 3-methyl benzylidene, 2, the 4-dimethyl benzylidene, 2, the 3-dimethyl benzylidene, 2, the 6-dimethyl benzylidene, 3, the 5-dimethyl benzylidene, 2, the 5-dimethyl benzylidene, 2,4,6-trimethylammonium benzylidene, 3,5-two trifluoromethyl benzylidenes, 2,3,4,5,6-five fluorine benzylidenes, 4-isopropoxy benzylidene, 4-n-butoxy benzylidene, 4-methoxyl group benzylidene, 2-methoxyl group benzylidene, 3-methoxyl group benzylidene, 2, the 4-dimethoxybenzylidenegroup group, 2, the 3-dimethoxybenzylidenegroup group, 2, the 6-dimethoxybenzylidenegroup group, 3, the 5-dimethoxybenzylidenegroup group, 2, the 5-dimethoxybenzylidenegroup group, 2,4,6-trimethoxy benzylidene, 3,5-two trifluoromethoxy benzylidenes, 2-isopropoxy benzylidene, 3-chloro-4-methoxyl group benzylidene, 2-chloro-4-trifluoromethoxy benzylidene, 3-methyl-4-fluorine benzylidene, 4-bromo-3-trifluoromethyl benzylidene, 2-trifluoromethyl benzylidene, 3-trifluoromethyl benzylidene, 4-trifluoromethyl benzylidene, 2-pentafluoroethyl group benzylidene, 3-pentafluoroethyl group benzylidene, 4-pentafluoroethyl group benzylidene, 2-trifluoromethoxy benzylidene, 3-trifluoromethoxy benzylidene, 4-trifluoromethoxy benzylidene, 2-five fluorine oxyethyl group benzylidenes, 3-five fluorine oxyethyl group benzylidenes, 4-five fluorine oxyethyl group benzylidenes, 2-(2-trifluoromethyl) ethylidene, 2-(3-trifluoromethyl) ethylidene, 2-(4-trifluoromethyl) ethylidene, 2-(2-Trifluoromethoxyphen-l) ethylidene, 2-(3-Trifluoromethoxyphen-l) ethylidene, 2-(4-Trifluoromethoxyphen-l) ethylidene, 2-(2-five fluorine ethoxyl phenenyls) ethylidene, 2-(3-five fluorine ethoxyl phenenyls) ethylidene, 2-(4-five fluorine ethoxyl phenenyls) ethylidene, 3-(2-trifluoromethyl) propylidene, 3-(3-trifluoromethyl) propylidene, 3-(4-trifluoromethyl) propylidene, 3-(2-Trifluoromethoxyphen-l) propylidene, 3-(3-Trifluoromethoxyphen-l) propylidene, 3-(4-Trifluoromethoxyphen-l) propylidene, 3-(3-five fluorine ethoxyl phenenyls) propylidene, 3-(4-five fluorine ethoxyl phenenyls) propylidene, 4-(3-five fluorine ethoxyl phenenyls) butylidene, 5-(4-trifluoromethyl) pentylidene, 4-(4-trifluoromethyl) pentylidene, 4-(4-Trifluoromethoxyphen-l) pentylidene, 6-(3-trifluoromethyl) hexylidene, 6-(4-trifluoromethyl) hexylidene, 6-(4-Trifluoromethoxyphen-l) hexylidene etc.

Piperidyl group [wherein the piperidine ring may be substituted with at least one group which is selected from Amino group (wherein the amino group may be substituted with at least one group which is selected from phenyl group [wherein On the phenyl may be substituted with at least one group selected from the group consisting of a halogen atom, a halogen substituted or Unsubstituted C1-C6 alkyl group and a halogen-substituted or unsubstituted C1-C6 alkoxy group], and C1-C6 alkyl groups); phenoxy group (wherein the phenyl ring may be substituted with at least one A group selected from the group consisting of a halogen atom, a halogen substituted or unsubstituted C1-C6 alkyl group and a halogen substituted or Unsubstituted C1-C6 alkoxy group); phenyl C1-C6 alkyl group (wherein the phenyl ring, May be substituted with at least one group which is selected from C1-C4 alkylenedioxy group, a halogen atom, a halogen- Substituted or unsubstituted C1-C6 alkyl group and a halogen-substituted or unsubstituted C1-C6 alkoxy group); Phenyl C1-C6 alkoxy group (wherein the phenyl ring may be substituted with at least one group selected from the Consisting of a halogen atom, a halogen substituted or unsubstituted C1-C6 alkyl group and a halogen-substituted or unsubstituted C1-C6 alkoxy group); phenyl (wherein the phenyl ring may be substituted with at least one A group selected from the group consisting of a halogen atom, a halogen substituted or unsubstituted C1-C6 alkyl group and a halogen substituted or Unsubstituted C1-C6 alkoxy group); naphthyl C1-C6 alkyl group; and a phenyl C1-C6 alkylene group (Wherein the phenyl ring may be substituted with at least one group selected from the group consisting of a halogen atom, a halogen Su substituted or unsubstituted C1-C6 alkyl group and a halogen-substituted or unsubstituted C1-C6 alkoxy group consisting of Group) from the group consisting] include piperidinyl, [wherein the piperidine ring may be substituted with 1 to 3 substituents Group, selected from the free amino group (wherein the amino group may be substituted with 1 or 2 groups selected from The phenyl group [wherein the phenyl ring may be substituted with 1 to 5, preferably 1 to 3 substituents, which Selected from a halogen atom, a halogen substituted or unsubstituted C1-C6 alkyl group and a halogen-substituted or unsubstituted C1-C6 alkoxy group] and a C1-C6 alkyl groups); phenoxy group (wherein the phenyl group The ring may be substituted with 1 to 5, preferably 1 to 3 substituents, selected from the group consisting of a halogen atom, a halogen Substituted or unsubstituted C1-C6 alkyl group and a halogen-substituted or unsubstituted C1-C6 alkoxy group consisting of Group); phenyl C1-C6 alkyl group (wherein the phenyl ring may be substituted with 1 to 5, preferably 1 To 3 substituents selected from 1 to 4 carbon atoms, straight-chain or branched-chain C1-C4 alkylenedioxy Group, a halogen atom, a halogen substituted or unsubstituted C1-C6 alkyl group and a halogen-substituted or unsubstituted C1-C6 Alkoxy group); as described later phenyl C1-C6 alkoxy group (wherein the phenyl ring, May be substituted with 1 to 5, preferably 1 to 3 substituents, selected from the group consisting of a halogen atom, a halogen substituted or Unsubstituted C1-C6 alkyl group and a halogen-substituted or unsubstituted C1-C6 alkoxy group); if The said phenyl (wherein the phenyl ring may be substituted with 1 to 5, preferably 1 to 3, taken Substituent selected from the group consisting of a halogen atom, a halogen substituted or unsubstituted C1-C6 alkyl group and a halogen substituted or unsubstituted Substituted C1-C6 alkoxy group); as described later naphthyl C1-C6 alkyl, the alkyl Moiety having from 1 to 6 carbon atoms, a straight-chain or branched-chain alkyl group; and a phenyl C1-C6 alkylene group (Wherein the phenyl ring may be substituted with 1 to 5, preferably 1 to 3 substituents, selected from A halogen atom, a halogen substituted or unsubstituted C1-C6 alkyl group and a halogen-substituted or unsubstituted C1-C6 Alkoxy group) consisting of Group], such as 1 - piperidinyl group, a 2 - piperidyl group, 3 - piperidyl group, 4 - Piperidinyl, 2,4 - diamino-1 - piperidinyl, 2,4,6 - triamino-1 - piperidinyl group, a 2 - amino-1 - Piperidyl group, a 3 - amino-1 - piperidinyl group, 4 - amino-1 - piperidinyl group, 4 - dimethylamino-1 - piperidinyl, 4 - ethyl-1 - piperidinyl group, 4 - n-propyl-1 - piperidinyl group, 4 - dimethylamino-1 - piperidinyl Group, 4 - diethylamino-1 - piperidinyl group, 4 - II - n-propyl-1 - piperidinyl group, 4 - phenylamino -1 - Piperidinyl, 4 - (N-phenyl-N-methyl-amino) -1 - piperidinyl, 4 - (2 - fluorophenyl)-1 - Piperidinyl, 4 - (3 - fluorophenyl)-1 - piperidinyl, 4 - (4 - fluorophenyl)-1 - piperidinyl, 4 - (2 - chlorophenyl)-1 - piperidinyl, 4 - (3 - chlorophenyl-amino) -1 - piperidinyl, 4 - (4 - chlorophenyl Ylamino) -1 - piperidinyl, 4 - (2,3 - dichlorophenyl)-1 - piperidinyl, 4 - (2,4,6 - trifluoro- Phenylamino) -1 - piperidinyl, 4 - (2,4 - dichlorophenyl)-1 - piperidinyl, 4 - (3,4 - dichloro- Phenylamino) -1 - piperidinyl, 4 - (3,5 - dichlorophenyl)-1 - piperidinyl, 4 - (2,3,4,5,6 - Pentafluorophenyl amino) -1 - piperidinyl, 4 - (2 - (trifluoromethyl) phenylamino) -1 - piperidinyl, 4 - (2 - Methyl-phenylamino)-1 - piperidinyl, 4 - (2,3 - dimethylphenyl)-1 - piperidinyl, 4 - (3 - Trifluoromethyl-phenylamino) -1 - piperidinyl, 4 - (2,4,6 - trimethylphenyl)-1 - piperidinyl, 4 - (4 - (trifluoromethyl) phenylamino) -1 - piperidinyl, 4 - (2 - amino-pentafluoroethyl-phenyl) -1 - piperidine Yl, 4 - (3 - pentafluoroethyl phenylamino) -1 - piperidinyl, 4 - (4 - pentafluoroethyl phenylamino) -1 - Piperidinyl, 4 - (2 - (trifluoromethoxy) phenyl amino) -1 - piperidinyl, 4 - (2 - methoxy-phenyl-amino Yl) -1 - piperidinyl, 4 - (2,3 - dimethoxyphenyl)-1 - piperidinyl, 4 - (2,4,6 - trimethoxy Amino-phenyl) -1 - piperidinyl, 4 - (N-methyl-N-(2,4,6 - trimethoxyphenyl ammonia Yl)) -1 - piperidinyl, 4 - (N-methyl-N-(3,4 - dimethyl-phenylamino)) -1 - piperidinyl, 4 - (N- Ethyl-N-(4 - chlorophenyl group)) -1 - piperidinyl, 4 - (3 - trifluoromethoxyphenyl)-1 - piperazine Piperidinyl, 4 - (4 - trifluoromethoxy-phenylamino)-1 - piperidinyl, 4 - (2 - Phenyl pentafluoroethoxy Yl) -1 - piperidinyl, 4 - (3 - pentafluoro-ethoxyphenyl)-1 - piperidinyl, 4 - (4 - pentafluoro-ethoxyethyl Amino-phenyl) -1 - piperidinyl, 4 - (N-methyl-N-(2 - fluorophenyl) amino) -1 - piperidinyl, 4 - (N-methyl-N-(3 - fluorophenyl) amino) -1 - piperidinyl, 4 - (N-methyl-N-(4 - fluorophenyl) amino Yl) -1 - piperidinyl group, 4 - phenoxy-1 - piperidinyl, 2,4 - diphenyl-1 - piperidinyl, 2,4,6 - Triphenyl-1 - piperidinyl, 2 - (2 - fluorophenoxy)-1 - piperidinyl, 3 - (3 - fluorophenoxy) -2 - Piperidinyl, 4 - (4 - fluorophenyl) -3 - piperidinyl, 2 - (2 - chlorophenoxy)-4 - piperidinyl, 3 - (3 - Chlorophenoxy) -5 - piperidinyl, 4 - (4 - chlorophenoxy) -5 - piperidyl group, 5 - (2 - bromophenyl) -2 - Piperidinyl, 6 - (3 - bromophenyl) -3 - piperidyl group, 4 - (4 - bromophenyl)-1 - piperidinyl, 3 - (2,3 - Dichlorophenoxy) -2 - piperidyl group, 4 - (3,4 - dichlorophenoxy) -3 - piperidyl group, 3 - (2,4 - dichloro- Phenoxy)-4 - piperidinyl, 2 - (3,4,5 - trichlorophenyl) -3 - piperidyl group, 6 - (2,4,6 - trichloro- Phenoxy) -2 - piperidyl group, 3 - (2,3,4,5,6 - pentafluorophenoxy) -1 - piperidinyl, 4 - (2 - methyl- Phenoxy)-1 - piperidinyl, 5 - (3 - methyl-phenoxy) -2 - piperidyl group, 6 - (4 - methyl-phenoxy) -3 - Piperidinyl, 4 - (2 - phenoxy-ethyl) -1 - piperidinyl, 2 - (3 - phenoxy-ethyl) -1 - piperidinyl, 3 - (4 - ethyl-phenoxy) -2 - piperidyl group, 4 - (4 - n-propyl-phenoxy) -3 - piperidyl group, 3 - (4 - Tert-butyl-phenoxy)-4 - piperidinyl, 2 - (4 - n-butyl-phenoxy) -3 - piperidyl group, 1 - (2 - trifluoro- Methylphenoxy) -2 - piperidyl group, 2 - (3 - (trifluoromethyl) phenoxy) -1 - piperidinyl, 4 - (4 - trifluoromethyl Methylphenoxy) -1 - piperidinyl, 1 - (2 - phenoxy-pentafluoroethyl) -4 - piperidinyl, 4 - (3 - pentafluoro- Phenoxy-ethyl) -1 - piperidinyl, 4 - (2,3 - dimethyl-phenoxy) -1 - piperidinyl, 4 - (3,4,5 - Trimethylphenoxy) -1 - piperidinyl, 4 - (4 - n-pentyloxy-phenoxy) -1 - piperidinyl, 4 - (4 - n-hexyl Phenoxy) -1 - piperidinyl, 4 - (2 - methoxyphenoxy) -1 - piperidinyl, 4 - (3 - Methoxyphenyl Oxy)-1 - piperidinyl, 4 - (4 - methoxyphenoxy)-1 - piperidinyl, 2 - (2 - ethoxy-phenoxy Yl) -3 - piperidyl group, 3 - (3 - phenoxy-ethoxy) -4 - piperidinyl, 4 - (4 - ethoxy-phenoxy) -3 - Piperidinyl, 3 - (4 - n-propoxy-phenoxy) -2 - piperidyl group, 2 - (4 - tert-butoxy-phenoxy) -1 - Piperidinyl, 4 - (4 - n-butyl phenoxy) -2 - piperidyl group, 2 - (2 - (trifluoromethoxy) phenoxy) -3 - Piperidinyl, 3 - (3 - trifluoromethyl-methoxyphenoxy) -4 - piperidinyl, 4 - (4 - (Trifluoromethoxy) phenoxy Yl) -3 - piperidyl group, 3 - (2 - pentafluoroethoxy phenoxy) -2 - piperidyl group, 2 - (4 - pentafluoroethoxy Phenoxy) -1 - piperidinyl, 4 - (2,3 - dimethoxyphenoxy) -14 - piperidinyl, 4 - (3,4,5 - Trimethoxyphenoxy) -1 - piperidinyl, 4 - (4 - n-pentyloxy-phenoxy) -1 - piperidinyl, 4 - (4 - N-hexyloxy-phenoxy) -1 - piperidyl group, 4 - benzyl-1 - piperidinyl, 2,4 - dibenzyl-1 - piperidinyl, 2,4,6 - benzyl-1 - piperidinyl, 2 - (2 - fluoro-benzyl) -1 - piperidinyl, 3 - (2 - (3 - fluorophenyl) Ethyl) -2 - piperidyl group, 4 - (1 - (4 - fluorophenyl) ethyl) -3 - piperidinyl, 2 - (3 - (2 - chlorophenyl) Propyl) -4 - piperidinyl, 3 - (4 - (3 - chlorophenyl) butyl) -5 - piperidinyl, 4 - (5 - (4 - chlorophenyl) Pentyl) -2 - piperidyl group, 5 - (6 - (2 - bromophenyl) hexyl) -2 - piperidyl group, 6 - (3 - bromo-benzyl) -3 - Piperidinyl, 4 - (4 - bromobenzyl)-1 - piperidinyl, 3 - (2,3 - dichloro-benzyl) -2 - piperidyl group, 4 - (3,4 - Dichloro-benzyl) -3 - piperidyl group, 3 - (2,4 - dichloro-benzyl)-4 - piperidinyl, 2 - (3,4,5 - trichloro-benzyl Yl) -3 - piperidyl group, 6 - (2,4,6 - trichloro-benzyl) -2 - piperidyl group, 3 - (2,3,4,5,6 - pentafluorobenzyl Yl) -1 - piperidinyl, 4 - (2 - methyl-benzyl) -1 - piperidinyl, 5 - (2 - (3 - methylphenyl) ethyl) -2 - Piperidinyl, 6 - (3 - (4 - methylphenyl) propyl) -3 - piperidyl group, 1 - (4 - (2 - ethyl-phenyl) butyl Yl) -4 - piperidinyl, 2 - (5 - (3 - ethylphenyl) pentyl)-1 - piperidinyl, 3 - (6 - (4 - ethyl-phenyl) Hexyl) -2 - piperidyl group, 4 - (4 - benzyl n-propyl) -3 - piperidyl group, 3 - (4 - tert-butylbenzyl) -4 - Piperidinyl, 2 - (4 - n-butyl benzyl) -3 - piperidyl group, 1 - (2 - (trifluoromethyl) benzyl) -2 - piperidyl group, 2 - (3 - (trifluoromethyl) benzyl) -1 - piperidinyl, 4 - (4 - (trifluoromethyl) benzyl) -1 - piperidinyl, 1 - (2 - Pentafluoroethyl-benzyl)-4 - piperidinyl, 1 - (3 - pentafluoroethyl benzyl)-4 - piperidinyl, 4 - (2,3 - Methylbenzyl)-1 - piperidinyl, 1 - (3,4,5 - trimethyl-benzyl)-4 - piperidinyl, 1 - (4 - n-pentyl Benzyl)-4 - piperidinyl, 4 - (4 - n-hexyl benzyl) -1 - piperidinyl, 4 - (2 - methoxy-benzyl) -1 - Piperidinyl, 1 - (2 - (3 - methoxyphenyl) ethyl) -4 - piperidinyl, 1 - (1 - (4 - methoxyphenyl) Ethyl)-4 - piperidinyl, 2 - (3 - (2 - ethoxy-phenyl) propyl) -3 - piperidyl group, 3 - (4 - (3 - ethoxy Yl-phenyl) butyl) -4 - piperidinyl, 4 - (5 - (4 - ethoxyphenyl) pentyl) -3 - piperidyl group, 3 - (6 - (4 - n-propoxy-phenyl) hexyl) -2 - piperidyl group, 2 - (4 - tert-butyl-benzyl) -1 - piperidine Group, 1 - (4 - n-butoxy-benzyl) -2 - piperidyl group, 2 - (2 - (Trifluoromethoxy) benzyl) -3 - piperidyl group, 3 - (3 - (Trifluoromethoxy) benzyl)-4 - piperidinyl, 4 - (4 - (Trifluoromethoxy) benzyl) -1 - piperidinyl, 3 - (2 - pentafluoroethoxy benzyl) -2 - piperidyl group, 2 - (4 - pentafluoroethoxy benzyl) -1 - piperidinyl, 1 - (2,3 - dimethoxy-benzyl) -4 - piperidinyl, 4 - (3,4,5 - trimethoxybenzyl) -1 - piperidinyl, 4 - (4 - n-pentyl-benzyl) -1 - piperidinyl, 4 - (4 - n-hexyl-benzyl) -1 - piperidyl group, 4 - benzyl -3 - phenoxy-1 - piperidinyl group, 4 - phenoxy-2 - methyl-1 - piperidinyl, 4 - (4 - trifluoromethyl Oxygen-benzylidene) -1 - piperidinyl, 4 - (4 - chloro-benzylidene) -1 - piperidinyl, 4 - (4 - trifluoromethylsulfinyl Benzyl) -1 - piperidinyl, 4 - (3,4 - dichloro-benzyloxy) - (1 -, 2 - or 3 -) piperidinyl, 4 - (4 - methyl Benzyloxy) - (1 -, 2 - or 3 -) piperidinyl, 4 - (4 - (Trifluoromethoxy) benzyloxy) - (1 -, 2 -, or 3 -) piperidyl group, 4 - (4 - methoxyphenyl) - (1 -, 2 - or 3 -) piperidyl group, 4 - (3,4 - dichlorophenyl Yl) - (1 -, 2 - or 3 -) piperidyl group, 4 - ((1 - or 2 -) naphthylmethyl) - (1 -, 2 - or 3 -) piperidinyl, 4 - (3,4 - methylenedioxy-phenyl) - (1 -, 2 - or 3 -) piperidinyl, 4 - (4 - chloro-benzyloxy) - (1 -, 2 - or 3 -) piperidyl group and the like. ...

Quinoline group (wherein the quinoline ring, may be substituted with at least one group selected from The (c-1) a halogen atom, (c-2) phenoxy group [wherein the phenyl ring may be substituted with at least one Group selected from the group consisting of a halogen atom, a halogen substituted or unsubstituted C1-C6 alkyl group and a halogen substituted or unsubstituted Substituted C1-C6 alkoxy group], (c-3) piperazinyl group [wherein the piperazine ring, can be Substituted with at least one group which is selected from phenyl C1-C6 alkyl group (wherein the phenyl ring may be To replace at least one group selected from the group consisting of a halogen atom, a halogen substituted or unsubstituted C1-C6 Alkyl and halogen-substituted or unsubstituted C1-C6 alkoxy group), a phenyl group [wherein the phenyl Base ring may be substituted with at least one group which is selected from a phenoxy group (wherein the phenyl ring , It can be substituted with at least one group selected from the group consisting of a halogen atom, a halogen substituted or unsubstituted C1-C6 alkyl group and a halogen-substituted or unsubstituted C1-C6 alkoxy group), a halogen atom, a halogen Su substituted or unsubstituted C1-C6 alkyl group and a halogen-substituted or unsubstituted C1-C6 alkoxy group consisting of Group] and a phenyl C2-C6 alkenyl group [wherein the phenyl ring may be substituted with at least one group which is Selected from a halogen atom, a halogen substituted or unsubstituted C1-C6 alkyl group and a halogen-substituted or unsubstituted C1-C6 alkoxy group] from the group consisting], and (c-4) piperidyl group [wherein the piperidine ring, it can be To replace at least one group selected from the free amino group (wherein the amino group may be substituted At least one group which is selected from phenyl group [wherein the phenyl ring may be substituted with at least one Group selected from the group consisting of a halogen atom, a halogen substituted or unsubstituted C1-C6 alkyl group and a halogen substituted or unsubstituted Substituted C1-C6 alkoxy group] and a C1-C6 alkyl groups); phenoxy group (wherein the The phenyl ring may be substituted with at least one group selected from the group consisting of a halogen atom, a halogen substituted or Unsubstituted C1-C6 alkyl group and a halogen-substituted or unsubstituted C1-C6 alkoxy group); benzene C1-C6 alkyl group (wherein the phenyl ring may be substituted with at least one group which is selected from C1-C4 alkylenedioxy group, a halogen atom, a halogen substituted or unsubstituted C1-C6 alkyl and halo-substituted Unsubstituted C1-C6 alkoxy group consisting of); phenyl C1-C6 alkoxy group (wherein the phenyl group The ring may be substituted with at least one group selected from the group consisting of a halogen atom, a halogen substituted or unsubstituted A C1-C6 alkyl group and a halogen-substituted or unsubstituted C1-C6 alkoxy group); phenyl (which At the phenyl ring may be substituted with at least one group selected from the group consisting of a halogen atom, a halogen- Substituted or unsubstituted C1-C6 alkyl group and a halogen-substituted or unsubstituted C1-C6 alkoxy group); Naphthyl C1-C6 alkyl; and phenyl C1-C6 alkylene group (wherein the phenyl ring may be substituted At least one group selected from the group consisting of a halogen atom, a halogen substituted or unsubstituted C1-C6 alkyl and halo Substituted or unsubstituted C1-C6 alkoxy group) the group consisting of] the group consisting of) include quinoline Group (wherein the quinoline ring, may be substituted with 1 to 3 substituents selected from (c-1) A halogen atom, (c-2) phenoxy group (wherein the phenyl ring may be substituted with 1 to 5, preferably 1 To 3 substituents selected from the group consisting of a halogen atom, a halogen substituted or unsubstituted C1-C6 alkyl and halo Substituted or unsubstituted C1-C6 alkoxy group), (c-3) piperazinyl group [wherein the piperazine ring , It can be substituted with 1 to 5, preferably 1 to 3 groups, which is selected from phenyl C1-C6 alkyl group (which At the phenyl ring may be substituted with 1 to 5, preferably 1 to 3 substituents, selected from the group consisting of halogen Atom, a halogen substituted or unsubstituted C1-C6 alkyl group and a halogen-substituted or unsubstituted C1-C6 alkoxy Group consisting of), a phenyl group [wherein the phenyl ring may be substituted with 1 to 5, preferably 1 to 3 A group which is selected from a phenoxy group (wherein the phenyl ring may be substituted with 1 to 5, preferably Select 1 to 3 groups selected from the group consisting of a halogen atom, a halogen substituted or unsubstituted C1-C6 alkyl and halo Substituted or unsubstituted C1-C6 alkoxy group), a halogen atom, a halogen substituted or unsubstituted C1-C6 alkyl group and a halogen-substituted or unsubstituted C1-C6 alkoxy group] and a phenyl alkenyl group (which Containing at least 1 to 3 double bonds, C2-C6 alkenyl group, wherein each double bond is trans form and Cis-form) (wherein the phenyl ring may be substituted with at least one group which is selected from A halogen atom, a halogen substituted or unsubstituted C1-C6 alkyl group and a halogen-substituted or unsubstituted C1-C6 alkoxy The group consisting of alkoxy) group consisting of], and (C-4) piperidyl group [wherein the piperidine ring can be substituted From 1 to 3 substituents, selected from the free amino group (wherein the amino group may be substituted with 1 or 2 Group, which is selected from phenyl group [wherein the phenyl ring may be substituted with 1 to 5, preferably 1 to 3 Substituents selected from the group consisting of a halogen atom, a halogen substituted or unsubstituted C1-C6 alkyl and halo-substituted Unsubstituted C1-C6 alkoxy group consisting of], and C1-C6 alkyl groups); phenoxy group (which At the phenyl ring may be substituted with 1 to 5, preferably 1 to 3 substituents, selected from the group consisting of halogen Atom, a halogen substituted or unsubstituted C1-C6 alkyl group and a halogen-substituted or unsubstituted C1-C6 alkoxy Group consisting of); phenyl C1-C6 alkyl group (wherein the phenyl ring may be substituted with 1 to 5 , Preferably 1 to 3 substituents selected from straight-chain or branched-chain C1-C4 alkylenedioxy group, a halogen atom, Halogen-substituted or unsubstituted C1-C6 alkyl group and a halogen-substituted or unsubstituted C1-C6 alkoxy Group); phenyl alkoxy, wherein the alkoxy moiety is a straight chain or branched chain C1-C6 alkoxy group (which At the phenyl ring may be substituted with 1 to 5, preferably 1 to 3 groups selected from the group consisting of halogen original Son, halogen-substituted or unsubstituted C1-C6 alkyl and halogen-substituted or unsubstituted C1-C6 alkoxy group The group consisting of); phenyl (wherein the phenyl ring may be substituted with 1 to 5, preferably 1 to 3 A group selected from the group consisting of a halogen atom, a halogen substituted or unsubstituted C1-C6 alkyl group and a halogen substituted or Unsubstituted C1-C6 alkoxy group); naphthyl alkyl wherein the alkyl moiety is a straight chain or Branched-chain C1-C6 alkyl; and phenyl C1-C6 alkylene group (wherein the phenyl ring may be substituted with 1 To 5, preferably 1 to 3 substituents, selected from the group consisting of a halogen atom, a halogen substituted or unsubstituted C1-C6 Alkyl and halogen-substituted or unsubstituted C1-C6 alkoxy group) the group consisting of] the composition of Group), for example, 2 - quinolyl group, a 3 - quinolyl group, a 4 - quinolyl group, a 5 - quinolyl group, a 6 - quinoline Yloxy 7 - quinolinoxy 8 - quinolyl group, a 4 - (1 - piperazinyl) -2 - quinoline group, a 3 - (2 - Piperidinyl) -4 - quinoline group, a 4 - (1 - piperazinyl) -3 - quinoline group, a 5 - (1 - piperazinyl) -4 - quinoline Morpholino group, a 6 - (3,4 - dibenzyl-1 - piperazinyl) -5 - quinoline group, 7 - (2,3,4 - tribenzyl-1 - Piperazinyl)-6 - quinolyl group, a 4 - (4 - benzyl-1 - piperazinyl) -2 - quinoline group, a 3 - (4 - (2 - phenyl Ethyl)-1 - piperazinyl) -2 - quinolyl group, a 4 - (4 - (3 - phenylpropyl) - 1-piperazinyl)-3 - quinoline Group, a 5 - (4 - (4 - phenylbutyl) -1 - piperazinyl)-4 - quinolyl group, a 6 - (4 - (5 - phenyl-pentyl Yl) -1 - piperazinyl) -5 - quinoline group, 7 - (4 - (6 - phenyl-hexyl)-1 - piperazinyl) -6 - quinolinoxy Group, 8-( 4 - (2 - fluorobenzyl)-1 - piperazinyl)-7 - quinoline group, a 2 - (4 - (3 - fluorobenzyl)-1 - piperazine Piperazinyl)-8 - quinolyl group, a 3 - (4 - (4 - fluorobenzyl)-1 - piperazinyl) -2 - quinolyl group, a 4 - (4 - (2 - Chlorobenzyl) -1 - piperazinyl) -3 - quinoline group, a 5 - (4 - (3 - chloro-benzyl)-1 - piperazinyl) -4 - quinoline Group, a 2 - (4 - (4 - chlorobenzyl) -1 - piperazinyl)-6 - quinolyl group, 7 - (4 - (2,3 - dichloro-benzyl Yl)-1 - piperazinyl)-6 - quinolyl group, 8-( 4 - (2,4 - dichloro-benzyl) -1 - piperazinyl)-7 - quinoline Group, a 2 - (4 - (3,4 - dichloro-benzyl) -1 - piperazinyl)-8 - quinolyl group, a 3 - (4 - (3,5 - dichloro- Benzyl)-1 - piperazinyl) -2 - quinoline group, a 4 - (4 - (3,4,5 - trichloro-benzyl)-1 - piperazinyl) -3 - Quinoline group, a 5 - (4 - (2,3,4,5,6 - pentafluoro-benzyl)-1 - piperazinyl) -4 - quinolinyl group, 6 - (4 - (2 - (trifluoromethyl) benzyl) -1 - piperazinyl) -5 - quinoline group, 7 - (4 - (3 - (trifluoromethyl) benzyl Yl)-1 - piperazinyl)-6 - quinolyl group, a 2 - (4 - (4 - (trifluoromethyl) benzyl) -1 - piperazinyl) -6 - quinoline Morpholino group, a 2 - (4 - (4 - methylbenzyl)-1 - piperazinyl)-8 - quinolyl group, a 3 - (4 - (3,4 - dimethoxyphenyl Benzyl)-1 - piperazinyl) -2 - quinoline group, a 4 - (4 - (2,4,6 - trimethyl-benzyl) - 1-piperazinyl Yl) -3 - quinolyl group, a 5 - (4 - (2 - benzyl-pentafluoroethyl)-1 - piperazinyl)-4 - quinolyl group, 6 - (4 - (3 - pentafluoroethyl-benzyl) - 1-piperazinyl)-5 - quinolyl group, 7 - (4 - (4 - benzyloxy pentafluoroethyl Yl)-1 - piperazinyl)-6 - quinolyl group, a 2 - (4 - (4 - (Trifluoromethoxy) benzyl) -1 - piperazinyl) -6 - Quinoline group, a 2 - (4 - (3 - (Trifluoromethoxy) benzyl) -1 - piperazinyl)-8 - quinolyl group, a 3 - (4 - (4 - Trifluoromethoxy-benzyl) - 1-piperazinyl)-2 - quinolyl group, a 4 - (4 - (4 - methoxybenzyl)-1 - piperazine Piperazinyl) -3 - quinolyl group, a 5 - (4 - (3,4 - dimethoxy-benzyl) -1 - piperazinyl)-4 - quinolyl group, 6 - (4 - (2,4,6 - trimethoxybenzyl) -1 - piperazinyl) -5 - quinoline group, 7 - (4 - (2 - pentafluoroethyl Benzyl) -1 - piperazinyl)-6 - quinolyl group, 8-( 4 - (3 - pentafluoro-ethoxy-benzyl) - 1-piperazinyl Yl) -2 - quinoline group, a 3 - (4 - (4 - pentafluoro-ethoxy-benzyl) - 1-piperazinyl)-2 - quinolyl group, 4 - (4 - (2 - (4 - trifluoromethoxy-phenyl) ethyl)-1 - piperazinyl) -3 - quinolyl group, 5 - (4 - (3 - (4 - trifluoromethoxy-phenyl) propyl) -1 - piperazinyl)-4 - quinolyl group, 6 - (4 - (4 - (4 - trifluoromethoxy-phenyl) butyl) - 1-piperazinyl)-5 - quinolyl group, 7 - (4 - (5 - (4 - trifluoromethoxyphenyl) pentyl)-1 - piperazinyl)-6 - quinolyl group, 8-( 4 - (6 - (4 - trifluoromethoxyphenyl) hexyl)-1 - piperazinyl)-7 - quinoline group, 2 - (4 - (2 - (4 - (trifluoromethyl) phenyl) ethyl) -1 - piperazinyl)-8 - quinolyl group, a 3 - (4 - (3 - (4 - Trifluoromethyl-phenyl)-propyl) -1 - piperazinyl) -2 - quinoline group, a 4 - (4 - (4 - (4 - (trifluoromethyl) phenyl Yl) butyl)-1 - piperazinyl) -2 - quinoline group, a 5 - (4 - (5 - (4 - (trifluoromethyl) phenyl) pentyl) -1 - Piperazinyl) -2 - quinolinyl group, a 6 - (4 - (6 - (4 - (trifluoromethyl) phenyl) hexyl)-1 - piperazinyl) -2 - Quinoline group, a 3 - (2 - piperidinyl) -2 - quinoline group, a 4 - (3 - piperidin-yl) -3 - quinolyl group, a 5 - (4 - Piperidinyl) -4 - quinolinyl group, a 6 - (2,4 - diamino-1 - piperidinyl) -5 - quinoline group, 7 - (2,4,6 - triamino-1 - piperidinyl)-6 - quinolyl group, 8-( 4 - amino-1 - piperidinyl) -7 - quinoline Morpholino group, a 2 - (4 - amino-1 - piperidinyl)-8 - quinolyl group, a 3 - (4 - amino-1 - piperidinyl) -2 - Quinolyl group, a 4 - (4 - methyl-1 - piperidinyl)-3 - quinoline group, a 5 - (4 - ethyl-amino-1 - Piperidinyl) -4 - quinolinyl group, a 6 - (4 - n-propyl-amino-1 - piperidinyl) -5 - quinoline group, 7 - (4 - Dimethylamino-1 - piperidinyl)-6 - quinolyl group, 8-( 4 - diethylamino-1 - piperidinyl) -7 - Quinoline group, a 2 - (4 - II - n-propyl-1 - piperidinyl)-8 - quinolyl group, a 3 - (4 - Phenyl -1 - piperidinyl)-2 - quinolyl group, 4 - (4 - (N-phenyl-N-methyl-amino) -1 - piperidinyl) -3 - Quinoline group, a 5 - (4 - (2 - fluorophenyl)-1 - piperidinyl) -4 - quinolinyl group, a 6 - (4 - (3 - fluoro- Phenylamino)-1 - piperidinyl) -5 - quinoline group, 7 - (4 - (4 - fluorophenyl)-1 - piperidine Yl) -6 - quinolyl group, 8-( 4 - (2 - chlorophenyl)-1 - piperidinyl) -7 - quinoline group, 2 - (4 - (3 - chlorophenyl)-1 - piperidinyl)-8 - quinolyl group, a 3 - (4 - (4 - chlorophenyl ammonia Yl) -1 - piperidinyl) -2 - quinoline group, a 4 - (4 - (2,3 - dichlorophenyl)-1 - piperidinyl) -3 - Quinoline group, a 5 - (4 - (2,4,6 - trifluoro-phenylamino)-1 - piperidinyl) -4 - quinoline group, 6 - (4 - (2,4 - dichlorophenyl)-1 - piperidinyl) -5 - quinolyl group, 7 - (4 - (3,4 - dichlorophenyl Ylamino)-1 - piperidinyl)-6 - quinolyl group, 8-( 4 - (3,5 - dichlorophenyl)-1 - piperidine Yl) -7 - quinoline group, a 2 - (4 - (2,3,4,5,6 - pentafluorophenyl)-1 - piperidinyl)-8 - quinoline Group, a 3 - (4 - (2 - (trifluoromethyl) phenylamino)-1 - piperidinyl) -2 - quinoline group, a 4 - (4 - (2 - Methyl-phenylamino)-1 - piperidinyl)-3 - quinoline group, a 5 - (4 - (2,3 - dimethyl-phenylamino Yl) -1 - piperidinyl) -4 - quinolinyl group, a 6 - (4 - (2 - (trifluoromethyl) phenylamino) -1 - piperidine Yl) -5 - quinolyl group, 7 - (4 - (2,4,6 - trimethylphenyl)-1 - piperidinyl)-6 - quinolyl oxide Group, 8-( 4 - (4 - (trifluoromethyl) phenylamino)-1 - piperidinyl) -7 - quinoline group, a 2 - (4 - (2 - Five Fluoroethyl phenylamino)-1 - piperidinyl)-8 - quinolyl group, a 3 - (4 - (3 - amino phenyl pentafluoroethyl Yl) -1 - piperidinyl) -2 - quinoline group, a 4 - (4 - (4 - pentafluoroethyl phenylamino) -1 - piperidine Yl) -3 - quinolyl group, a 5 - (4 - (2 - (Trifluoromethoxy) phenylamino)-1 - piperidinyl) -4 - quinolinoxy Group, 6 - (4 - (2 - methoxyphenyl)-1 - piperidinyl) -5 - quinoline group, 7 - (4 - (2,3 - Methoxyphenyl)-1 - piperidinyl)-6 - quinolyl group, 8-( 4 - (2,4,6 - trimethoxyphenyl Amino) -1 - piperidinyl) -7 - quinoline group, 2 - (4 - (N-methyl-N-(2,4,6 - trimethoxyphenyl Amino)) -1 - piperidinyl)-8 - quinolyl group, 3 - (4 - (N-methyl-N-(3,4 - dimethylphenyl ammonium Yl)) -1 - piperidinyl)-2 - quinolyl group, a 4 - (4 - (3 - (Trifluoromethoxy) phenylamino)-1 - piperidine Yl) -2 - quinoline group, a 5 - (4 - (4 - trifluoromethoxy-phenylamino)-1 - piperidinyl) -2 - quinolinoxy Group, 6 - (4 - (2 - pentafluoroethoxy phenylamino)-1 - piperidinyl)-2 - quinolyl group, 7 - (4 - (3 - Pentafluoro-ethoxyphenyl)-1 - piperidinyl) -2 - quinoline group, 8-( 4 - (4 - phenyl pentafluoroethoxy Ylamino)-1 - piperidinyl) -2 - quinoline group, a 2 - (4 - (2 - fluorophenyl)-1 - piperidinyl) -3 - Quinoline group, a 3 - (4 - (3 - fluorophenyl)-1 - piperidinyl)-2 - quinolyl group, a 4 - (4 - (4 - fluoro- Phenylamino)-1 - piperidinyl) -2 - quinolyloxy, 2 - (4 - (N-ethyl-N-(4 - chlorophenyl ammonia Yl)) -1 - piperidinyl)-6 - quinolyl group, a 2,4 - bis (1 - piperazinyl (piperadinyl)) -6 - Quinoline group, a 3 - (1 - piperidinyl) -4 - (1 - piperazinyl (piperadinyl)) -2 - quinoline group, 2,4,6 - tris (1 - piperidinyl)-3 - quinoline group, a 5 - chloro-8 - quinolyl group, a 2 - (4 - (Trifluoromethoxy) Phenoxy) -6 - quinoline group, a 2 - (4 - (4 - (trifluoromethoxy) benzylidene)-1 - piperidinyl) -6 - quinoline Group, a 2 - (4 - (4 - chloro-benzylidene)-1 - piperidinyl)-6 - quinolyl group, a 2 - (4 - (4 - (trifluoromethyl) Benzylidene)-1 - piperidinyl)-6 - quinolyl group, a 2 - (4 - benzyl-1 - piperidinyl) -4 - quinoline group, 2 - (3,4 - dibenzyl-1 - piperidinyl) -4 - quinoline group, a 5 - (2,3,4 - tribenzyl-1 - piperidine Yl) -2 - quinolyl group, a 4 - (4 - (2 - phenylethyl) -1 - piperidinyl)-2 - quinolyl group, a 4 - (4 - (3 - Phenyl-propyl)-1 - piperidinyl) -5 - quinoline group, a 4 - (4 - (4 - phenyl-butyl) -1 - piperidinyl) -6 - Quinolyl group, a 4 - (4 - (5 - phenyl-pentyl)-1 - piperidinyl) -7 - quinoline group, a 2 - (4 - (6 - phenyl- Hexyl)-1 - piperidinyl) -4 - quinolyl group, a 4 - (4 - (2 - fluorobenzyl)-1 - piperidinyl) -2 - quinolinoxy Group, 2 - (4 - (3 - fluorobenzyl)-1 - piperidinyl) -4 - quinoline group, a 2 - (4 - (4 - fluorobenzyl) -1 - piperazine Piperidyl) -5 - quinoline group, a 2 - (4 - (2 - chloro-benzyl) -1 - piperidinyl)-6 - quinolyl group, a 2 - (4 - (3 - Chlorobenzyl) -1 - piperidinyl) -7 - quinoline group, a 5 - (4 - (4 - chlorobenzyl) -1 - piperidinyl) -4 - quinoline Oxy, 6 - (4 - (2,3 - dichloro-benzyl) -1 - piperidinyl) -4 - quinolyl group, 7 - (4 - (2,4 - dichloro- Benzyl) -1 - piperidinyl)-8 - quinolyl group, a 2 - (4 - (3,4 - dichloro-benzyl) -1 - piperidinyl) -8 - quinoline Morpholino group, a 4 - (4 - (3,5 - dichloro-benzyl) -1 - piperidinyl)-2 - quinolyl group, a 4 - (4 - (3,4,5 - Trichloro-benzyl)-1 - piperidinyl) -5 - quinolyl group, a 4 - (4 - (2,3,4,5,6 - pentafluoro-benzyl) -1 - piperazine Piperidinyl)-2 - quinolyl group, a 4 - (4 - (2 - (trifluoromethyl) benzyl) -1 - piperidinyl)-6 - quinolyl group, 4 - (4 - (3 - (trifluoromethyl) benzyl) -1 - piperidinyl) -7 - quinoline group, a 2 - (4 - (4 - (trifluoromethyl) benzyl Yl) -1 - piperidinyl)-8 - quinolyl group, a 5 - (4 - (4 - methylbenzyl)-1 - piperidinyl) -4 - quinolinoxy Group, 6 - (4 - (3,4 - dimethylbenzyl)-1 - piperidinyl) -4 - quinoline group, 8-( 4 - (2,4,6 - Methylbenzyl)-1 - piperidinyl) -4 - quinoline group, a 3 - (4 - (2 - benzyl-pentafluoroethyl) -1 - piperidine Yl) -2 - quinoline group, 8-( 4 - (3 - pentafluoroethyl benzyl) -1 - piperidinyl) -5 - quinoline group, 4 - (4 - (4 - benzyl-pentafluoroethyl)-1 - piperidinyl)-6 - quinolyl group, a 4 - (4 - (2 - (Trifluoromethoxy) Benzyl) -1 - piperidinyl) -7 - quinoline group, a 5 - (4 - (3 - (Trifluoromethoxy) benzyl) -1 - piperidine Yl) -4 - quinolyl group, a 6 - (4 - (4 - (Trifluoromethoxy) benzyl) -1 - piperidinyl) -5 - quinoline group, 7 - (4 - (4 - methoxybenzyl)-1 - piperidinyl) -5 - quinolyl group, a 6 - (4 - (3,4 - dimethoxybenzyl Yl) -1 - piperidinyl) -4 - quinoline group, 7 - (4 - (2,4,6 - trimethoxybenzyl) -1 - piperidine Yl) -4 - quinolyl group, a 5 - (4 - (2 - pentafluoroethoxy benzyl) -1 - piperidinyl) -4 - quinolyl group, 4 - (4 - (3 - pentafluoroethoxy benzyl) -1 - piperidinyl)-2 - quinolyl group, a 6 - (4 - (4 - pentafluoro-ethoxyethyl Benzyl)-1 - piperidinyl) -4 - quinolyl group, a 4 - (4 - (2 - (4 - trifluoromethoxy-phenyl) ethyl Yl) -1 - piperidinyl) -2 - quinoline group, a 4 - (4 - (3 - (4 - trifluoromethoxy-phenyl) propyl) -1 - piperazine Piperidinyl)-2 - quinolyl group, a 4 - (4 - (4 - (4 - trifluoromethoxy-phenyl)-butyl) -1 - piperidinyl) -2 - Quinolyl group, a 4 - (4 - (5 - (4 - trifluoromethoxyphenyl) pentyl)-1 - piperidinyl)-3 - quinoline group, 4 - (4 - (6 - (4 - trifluoromethoxyphenyl) hexyl)-1 - piperidinyl)-3 - quinoline group, 4 - (4 - (2 - (4 - (trifluoromethyl) phenyl) ethyl)-1 - piperidinyl)-2 - quinolyl group, a 5 - (4 - (3 - (4 - Trifluoromethyl-phenyl)-propyl) -1 - piperidinyl) -2 - quinolinyl group, a 6 - (4 - (4 - (4 - (trifluoromethyl) phenyl Yl) butyl) -1 - piperidinyl)-2 - quinolyl group, 7 - (4 - (5 - (4 - (trifluoromethyl) phenyl) pentyl) -2 - Piperidinyl) -2 - quinoline group, a 5 - (4 - (6 - (4 - (trifluoromethyl) phenyl) hexyl)-1 - piperidinyl) -2 - Quinoline group, a 2 - (4 - phenoxy-1 - piperidinyl) -4 - quinoline group, a 2 - (3,4 - diphenyl-1 - Piperidinyl) -4 - quinoline group, a 5 - (2,3,4 - triphenyl-1 - piperidinyl) -2 - quinoline group, 4 - (4 - (2 - fluorophenoxy)-1 - piperidinyl)-2 - quinolyl group, a 2 - (4 - (3 - fluorophenoxy)-1 - piperazine Piperidinyl) -4 - quinoline group, a 2 - (4 - (4 - fluorophenoxy)-1 - piperidinyl) -5 - quinoline group, 2 - (4 - (2 - chlorophenoxy) -1 - piperidinyl)-6 - quinolyl group, a 2 - (4 - (3 - chlorophenoxy) -1 - piperazine Piperidinyl) -7 - quinoline group, a 5 - (4 - (4 - chlorophenoxy)-1 - piperidinyl) -4 - quinoline group, 6 - (4 - (2,3 - dichlorophenoxy)-1 - piperidinyl) -4 - quinolyl group, 7 - (4 - (2,4 - dichloro-phenoxy Yl) -1 - piperidinyl) -4 - quinoline group, a 2 - (4 - (3,4 - dichlorophenoxy) -1 - piperidinyl) -8 - quinoline Morpholino group, a 4 - (4 - (3,5 - dichlorophenoxy)-1 - piperidinyl)-2 - quinolyl group, a 4 - (4 - (3,4,5 - Trichlorophenoxy) -1 - piperidinyl) -5 - quinoline group, a 4 - (4 - (2,3,4,5,6 - pentafluorophenyl oxygen Yl) -1 - piperidinyl) -2 - quinoline group, a 4 - (4 - (2 - (trifluoromethyl) phenoxy) -1 - piperidinyl) -6 - Quinolyl group, a 4 - (4 - (3 - (trifluoromethyl) phenoxy) -1 - piperidinyl) -7 - quinoline group, a 2 - (4 - (4 - Trifluoromethylphenoxy)-1 - piperidinyl) -4 - quinoline group, a 5 - (4 - (4 - methyl-phenoxy) -1 - piperazine Piperidinyl) -4 - quinolyl group, a 6 - (4 - (3,4 - dimethoxy-phenoxy)-1 - piperidinyl) -4 - quinolyl group, 7 - (4 - (2,4,6 - trimethoxy-phenoxy)-1 - piperidinyl) -4 - quinolyl group, a 4 - (4 - (2 - pentafluoroethyl Phenoxy)-1 - piperidinyl)-2 - quinolyl group, a 4 - (4 - (3 - pentafluoroethyl-phenoxy) -1 - piperidine Yl) -5 - quinolyl group, a 4 - (4 - (4 - pentafluoroethyl-phenoxy)-1 - piperidinyl)-6 - quinolyl group, 4 - (4 - (2 - (trifluoromethoxy) phenoxy) -1 - piperidinyl) -7 - quinolyl group, a 5 - (4 - (3 - trifluoromethyl Phenoxy)-1 - piperidinyl) -4 - quinolyl group, a 6 - (4 - (4 - (trifluoromethoxy) phenoxy) -1 - Piperidyl) -5 - quinolyloxy, 7 - (4 - (4 - methoxyphenoxy)-1 - piperidinyl) -5 - quinoline group, 6 - (4 - (3,4 - dimethoxyphenyl)-1 - piperidinyl) -4 - quinolyl group, 8-( 4 - (2,4,6 - Methoxyphenoxy)-1 - piperidinyl) -4 - quinoline group, a 5 - (4 - (2 - phenoxy pentafluoroethoxy Yl) -1 - piperidinyl) -4 - quinolyl group, a 4 - (4 - (3 - pentafluoro-ethoxy-phenoxy) -1 - piperidine Yl) -2 - quinolyl group, a 6 - (4 - (4 - pentafluoro-ethoxy-phenoxy)-1 - piperidinyl) -4 - quinolyl group, 2,5,6 - triphenyl-7 - quinoline group, 4,5,6 - trichloro-2 - quinolyl group, 2 - phenoxy-6 - Bromo-5 - quinoline group, a 2 - (2,3 - dimethoxy-phenoxy) -5 - quinoline group, a 2 - (3,4,5 - trimethyl- Phenoxy) -6 - quinoline group, a 2 - (2,3 - dimethoxyphenyl)-7 - quinoline group, a 2 - (3,4,5 - Trimethoxyphenoxy)-8 - quinolyl group, a 2 - (2,3,4,5,6 - pentafluorophenoxy) -6 - quinolinoxy Group, 2 - (2 - methylphenoxy) -4 - quinoline group, a 2 - (3 - methyl-phenoxy) -3 - quinoline group, 3 - (4 - methylphenoxy)-2 - quinolyl group, a 4 - (2 - methoxyphenoxy)-3 - quinoline group, 5 - (3 - methoxyphenoxy) -4 - quinolyl group, a 6 - (4 - methoxyphenoxy) -5 - quinoline group, 7 - (2 - fluorophenoxy)-6 - quinolyl group, 8-( 3 - fluorophenoxy) -7 - quinoline group, a 2 - (4 - fluorophenyl Oxy) -5 - quinoline group, a 3 - (2 - chlorophenoxy)-2 - quinolyl group, a 4 - (3 - chlorophenoxy) -6 - Quinoline group, a 5 - (4 - chlorophenoxy)-2 - quinolyl group, a 6 - (2 - bromophenyl) -3 - quinolyl group, 7 - (3 - bromophenyl)-4 - quinolyl group, 8-( 4 - bromophenyl) -2 - quinoline group, a 2 - (2,3 - Dichlorophenoxy)-6 - quinolyl group, a 3 - (3,4 - dichlorophenoxy) -7 - quinolyl group, a 4 - (2,4 - Dichlorophenoxy) -5 - quinoline group, a 2 - (3,4,5 - trichlorophenyl)-6 - quinolyl group, 2 - (2,4,6 - trichlorophenyl)-5 - quinolyl group, a 2 - (3 - (trifluoromethyl) phenoxy) -7 - O quinoline Group, 2 - (4 - (3 - (4 - (trifluoromethyl) phenyl) -2 - propenyl) - (1 -, 2 - or 3 -) piperazinyl) - (3 -, 4 -, 5 -, 6 -, 7 - or 8-) quinolyloxy, 2 - (4 - (4 - methoxyphenyl) - (1 -, 2 - or 3 -) piperazine Piperazinyl) - (3 -, 4 -, 5 -, 6 -, 7 - or 8-) quinolyloxy, 2 - (4 - (3,4 - dimethylphenyl Yl) - (1 -, 2 - or 3 -) piperazinyl) - (3 -, 4 -, 5 -, 6 -, 7 - or 8-) quinolyloxy, 2 - (4 - (4 - fluorophenyl) - (1 -, 2 - or 3 -) piperazinyl) - (3 -, 4 -, 5 -, 6 -, 7 - or 8-) quinolyl Morpholino group, a 2 - (4 - (4 - trifluoromethyl-phenyl) - (1 -, 2 - or 3 -) piperazinyl) - (3 -, 4 -, 5 -, 6 -, 7 - or 8-) quinolyloxy, 2 - (4 - (4 - methylphenyl) - (1 -, 2 - or 3 -) piperazinyl) - (3 -, 4 -, 5 -, 6 -, 7 - or 8-) quinolyloxy, 2 - (4 - (3,4 - dichlorophenyl) - (1 -, 2 - or 3 -) piperazine Piperazinyl) - (3 -, 4 -, 5 -, 6 -, 7 - or 8-) quinolyloxy, 2 - (4 - (4 - (trifluoromethoxy) benzene Yl) - (1 -, 2 - or 3 -) piperazinyl) - (3 -, 4 -, 5 -, 6 -, 7 - or 8-) quinolyloxy, 2 - (4 - (4 - (4 - chlorophenoxy) phenyl) - (1 -, 2 - or 3 -) piperazinyl) - (3 -, 4 -, 5 -, 6 -, 7 - or 8-) quinolyloxy, 2 - (4 - (3,4 - dichloro-benzyloxy) - (1 -, 2 - or 3 -) piperazinyl) - (3 -, 4 -, 5 -, 6 -, 7 - or 8-) quinolyloxy, 2 - (4 - (4 - methyl-benzyloxy) - (1 -, 2 - or 3 -) piperazine Piperazinyl) - (3 -, 4 -, 5 -, 6 -, 7 - or 8-) quinolyloxy, 2 - (4 - (4 - (Trifluoromethoxy) benzyloxy Yl) - (1 -, 2 - or 3 -) piperazinyl) - (3 -, 4 -, 5 -, 6 -, 7 - or 8-) quinolyloxy, 2 - (4 - (4 - methoxyphenyl) - (1 -, 2 - or 3 -) piperazinyl) - (3 -, 4 -, 5 -, 6 -, 7 - or 8-) Quinoline group, a 2 - (4 - (3,4 - dichlorophenyl) - (1 -, 2 - or 3 -) piperazinyl) - (3 -, 4 -, 5 -, 6 -, 7 - or 8-) quinolyloxy, 2 - (4 - ((1 - or 2 -) naphthylmethyl) - (1 -, 2 - or 3 -)-piperazine Yl) - (3 -, 4 -, 5 -, 6 -, 7 - or 8-) quinoline group, 2 - (4 - (3,4 - methylenedioxybenzene Yl) - (1 -, 2 - or 3 -) piperazinyl) - (3 -, 4 -, 5 -, 6 -, 7 - or 8-) quinolyloxy, 2 - (4 - (4 - chloro-benzyloxy) - (1 -, 2 - or 3 -) piperazinyl) - (3 -, 4 -, 5 -, 6 -, 7 - or 8-) Quinoline group. ...

The C1-C6 alkyl that phenyl C1-C6 alkoxyl group replaces is (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, the group that halogen replacement or unsubstituted C1-C6 alkyl and halogen replacement or unsubstituted C1-C6 alkoxyl group are formed) group of forming by phenyl C1-C6 alkoxyl group and C1-C6 alkyl, it can be by 1 to 5, preferred 1 to 3 substituting group replaces, described substituting group is selected from by halogen atom as defined above, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed, the example comprises benzyloxymethyl, 2-phenyl ethoxy methyl, 3-phenyl propoxy-methyl, 2-phenyl propoxy-methyl, 4-phenyl butoxymethyl, 5-phenyl pentyloxy methyl, 4-phenyl pentyloxy methyl, 6-phenyl hexyloxy methyl, 2-fluorine benzyloxymethyl, 4-fluorine benzyloxymethyl, 4-benzyl chloride oxygen ylmethyl, 3-benzyl chloride oxygen ylmethyl, 2-benzyl chloride oxygen ylmethyl, 3,5-dichloro-benzyloxy methyl, 3,4-dichloro-benzyloxy methyl, 2-(3-fluorine benzyloxy) ethyl, 1-(4-fluorine benzyloxy) ethyl, 3-(2-(2-fluorophenyl) oxyethyl group) propyl group, 4-(2-(3-fluorophenyl) oxyethyl group) butyl, 5-(2-(4-fluorophenyl) oxyethyl group) amyl group, 6-(2-chlorine benzyloxy) hexyl, 3-benzyl chloride oxygen ylmethyl, 2-(4-chlorine benzyloxy) ethyl, 1-(2-fluoro-4-bromo-benzyloxy-) ethyl, 3-(4-chloro-3-fluorine benzyloxy) propyl group, 4-(2,3,4-trichlorine benzyloxy) butyl, 5-(3,4,5-trifluoromethyl benzyl oxy base) amyl group, 6-(2,3,4,5,6-five fluorine benzyloxies) hexyl, 2,4,6-trichlorine benzyloxymethyl, 2-(4-isopropyl benzyloxy) ethyl, 1-(4-normal-butyl benzyloxy) ethyl, 3-(4-methyl benzyloxy) propyl group, 4-(2-methyl benzyloxy) butyl, 5-(3-methyl benzyloxy) amyl group, 6-(2, the 4-benzyloxy-dimethyl) hexyl, 2,3-benzyloxy-dimethyl methyl, 4-methyl benzyloxymethyl, 4-ethyl benzyloxymethyl, 3,5-benzyloxy-dimethyl methyl, 4-isopropyl benzyloxy methyl, 3-trifluoromethyl benzyloxy methyl, 4-trifluoromethyl benzyloxy methyl, 2-trifluoromethyl benzyloxy methyl, 2-(2, the 6-benzyloxy-dimethyl) ethyl, 1-(3, the 5-benzyloxy-dimethyl) ethyl, 3-(2, the 5-benzyloxy-dimethyl) propyl group, 4-(2,4,6-trimethylammonium benzyloxy) butyl, 5-(3,5-two trifluoromethyl benzyloxies) amyl group, 6-(4-isopropoxy benzyloxy) hexyl, 4-n-butoxy benzyloxymethyl, 4-trifluoromethoxy benzyloxymethyl, 2-trifluoromethoxy benzyloxymethyl, 3-trifluoromethoxy benzyloxymethyl, 3-methoxyl group benzyloxy ylmethyl, 2-(4-methoxyl group benzyloxy base) ethyl, 1-(2-methoxyl group benzyloxy base) ethyl, 3-(3-methoxyl group benzyloxy base) propyl group, 4-(2,4-dimethoxy benzyloxy) butyl, 5-(2,3-dimethoxy benzyloxy) amyl group, 6-(2,6-dimethoxy benzyloxy) hexyl, 3,5-dimethoxy benzyloxymethyl, 2-(2,5-dimethoxy benzyloxy) ethyl, 1-(2,4,6-trimethoxy benzyloxy) ethyl, 3-(3,5-two trifluoromethoxy benzyloxies) propyl group, 4-(2-isopropoxy benzyloxy) butyl, 5-(3-chloro-4-methoxyl group benzyloxy base) amyl group, 6-(2-chloro-4-trifluoromethoxy benzyloxy) hexyl, 3-methyl-4-fluorine benzyloxymethyl, 2-(4-bromo-3-trifluoromethyl benzyloxy) ethyl, 1-(2-(2-chloro-phenyl-) oxyethyl group) methyl, 3-(2-(3-chloro-phenyl-) oxyethyl group) propyl group, 4-(2-(4-chloro-phenyl-) oxyethyl group) butyl, 5-(2-trifluoromethyl benzyloxy) amyl group, 6-(3-trifluoromethyl benzyloxy) hexyl, 4-trifluoromethyl benzyloxy methyl, 2-(2-trifluoromethoxy benzyloxy) ethyl, 1-(3-trifluoromethoxy benzyloxy) ethyl, 3-(4-trifluoromethoxy benzyloxy) propyl group, 4-(2-(2-trifluoromethyl) oxyethyl group) butyl, 5-(2-(3-trifluoromethyl) oxyethyl group) amyl group, 6-(2-(4-trifluoromethyl) oxyethyl group) hexyl, (2-(2-Trifluoromethoxyphen-l) oxyethyl group) methyl, 2-(2-(3-Trifluoromethoxyphen-l) oxyethyl group) ethyl, 1-(2-(4-Trifluoromethoxyphen-l) oxyethyl group) ethyl, 3-(3-(2-trifluoromethyl) propoxy-) propyl group, 4-(3-(3-trifluoromethyl) propoxy-) butyl, 5-(3-(4-trifluoromethyl) propoxy-) amyl group, 6-(3-(2-trifluoromethyl) propoxy-) amyl group, (3-(3-Trifluoromethoxyphen-l) propoxy-) methyl, 2-(3-(4-Trifluoromethoxyphen-l) propoxy-) ethyl, 1-(4-(3-trifluoromethyl) butoxy) ethyl, 3-(5-(4-trifluoromethyl) pentyloxy) butyl, 4-(4-(4-trifluoromethyl) pentyloxy) butyl, 5-(4-(4-Trifluoromethoxyphen-l) pentyloxy) amyl group, 6-(6-(3-trifluoromethyl) hexyloxy) hexyl, (6-(4-trifluoromethyl) hexyloxy) methyl, 2-(6-(4-Trifluoromethoxyphen-l) hexyloxy) ethyl etc.

Piperidyl group [wherein the piperidine ring may be substituted with at least one group which is selected from A phenoxy group (wherein the phenyl ring may be substituted with at least one group which is selected from a halogen atom Son, halogen-substituted or unsubstituted C1-C6 alkyl and halogen-substituted or unsubstituted C1-C6 alkoxy group The group consisting of), a phenyl C1-C6 alkoxy-substituted C1-C6 alkyl group (wherein the phenyl ring, May be substituted with at least one group selected from the group consisting of a halogen atom, a halogen substituted or unsubstituted C1-C6 Alkyl and halogen-substituted or unsubstituted C1-C6 alkoxy group), a phenoxy C1-C6 alkyl group (Wherein the phenyl ring may be substituted with at least one group selected from the group consisting of a halogen atom, a halogen Su substituted or unsubstituted C1-C6 alkyl group and a halogen-substituted or unsubstituted C1-C6 alkoxy group consisting of Group) and a phenyl C1-C6 alkyl group (wherein the phenyl ring may be substituted with at least one group, Selected from the group consisting of a halogen atom, a halogen substituted or unsubstituted C1-C6 alkyl group and a halogen-substituted or unsubstituted C1-C6 alkoxy group) from the group consisting] include piperidinyl group [wherein the piperidine ring can be Substituted with 1 to 3 substituents selected from a phenoxy group (wherein the phenyl ring may be substituted From 1 to 5, preferably 1 to 3 substituents selected from the group consisting of a halogen atom, a halogen substituted or unsubstituted C1-C6 alkyl group and a halogen-substituted or unsubstituted C1-C6 alkoxy group), a phenyl C1-C6 Alkoxy-substituted C1-C6 alkyl group (wherein the phenyl ring may be substituted with 1 to 5, preferably 1 to 3 substituents selected from the group consisting of a halogen atom, a halogen substituted or unsubstituted C1-C6 alkyl and halo Substituted or unsubstituted C1-C6 alkoxy group), as described later in the alkyl portion Having from 1 to 6 carbon atoms, a straight-chain or branched-chain alkyl phenoxy C1-C6 alkyl (wherein the On the phenyl ring, may be substituted with 1 to 5, preferably 1 to 3 substituents, selected from the group consisting of a halogen atom, Halogen-substituted or unsubstituted C1-C6 alkyl group and a halogen-substituted or unsubstituted C1-C6 alkoxy Group) and a phenyl C1-C6 alkyl group (wherein the phenyl ring may be substituted with 1 to 5, preferably 1 to 3 substituents selected from the group consisting of a halogen atom, a halogen substituted or unsubstituted C1-C6 alkyl and halo Substituted or unsubstituted C1-C6 alkoxy group) consisting of Group], such as 1 - piperidinyl group, 4 - Piperidinyl 2 - piperidyl group, 3 - piperidyl group, 4 - phenoxy-1 - piperidinyl, 2,4 - diphenyl-1 - Piperidinyl, 2,4,6 - triphenyl-1 - piperidinyl, 2 - (2 - fluorophenoxy)-1 - piperidinyl, 3 - (3 - Fluorophenoxy) -2 - piperidyl group, 4 - (4 - fluorophenyl) -3 - piperidinyl, 2 - (2 - chlorophenoxy) -4 - Piperidinyl, 3 - (3 - chlorophenoxy) -5 - piperidinyl, 4 - (4 - chlorophenoxy) -2 - piperidyl group, 5 - (2 - Bromophenyl) -2 - piperidyl group, 6 - (3 - bromophenyl) -3 - piperidyl group, 4 - (4 - bromophenyl)-1 - Piperidinyl, 3 - (2,3 - dichlorophenoxy) -2 - piperidyl group, 4 - (3,4 - dichlorophenoxy) -3 - piperidine Group, a 3 - (2,4 - dichlorophenoxy)-4 - piperidinyl, 2 - (3,4,5 - trichlorophenyl) -3 - piperidyl group, 6 - (2,4,6 - trichlorophenyl) -2 - piperidyl group, 3 - (2,3,4,5,6 - pentafluorophenoxy) -1 - piperidine Yl, 4 - (2 - methylphenoxy)-1 - piperidinyl, 5 - (3 - methyl-phenoxy) -2 - piperidyl group, 6 - (4 - Methylphenoxy) -3 - piperidyl group, 3 - (2 - phenoxy-ethyl) -4 - piperidinyl, 2 - (3 - ethyl-phenoxy Yl) -1 - piperidinyl, 3 - (4 - ethyl-phenoxy) -2 - piperidyl group, 4 - (4 - n-propyl-phenoxy) -3 - Piperidinyl, 3 - (4 - tert-butyl-phenoxy)-4 - piperidinyl, 2 - (4 - n-butyl-phenoxy) -3 - piperidine Yl, 4 - (2 - (trifluoromethyl) phenoxy) -2 - piperidyl group, 2 - (3 - (trifluoromethyl) phenoxy) -1 - piperidine Group, 3 - (4 - (trifluoromethyl) phenoxy) -1 - piperidinyl, 1 - (2 - pentafluoroethyl-phenoxy)-4 - piperidine Group, 1 - (3 - pentafluoroethyl phenoxy) -4 - piperidinyl, 4 - (2,3 - dimethyl-phenoxy) -1 - piperidine Group, a 3 - (3,4,5 - trimethyl-phenoxy)-4 - piperidinyl, 1 - (4 - n-pentyloxy-phenoxy)-4 - piperidine Yl, 4 - (4 - n-hexyl-phenoxy) -1 - piperidinyl, 4 - (2 - methoxyphenoxy) -1 - piperidinyl, 1 - (3 - methoxyphenoxy) -4 - piperidinyl, 3 - (4 - methoxyphenoxy) -4 - piperidinyl, 2 - (2 - Phenoxy-ethoxy) -3 - piperidyl group, 3 - (3 - phenoxy-ethoxy) -4 - piperidinyl, 4 - (4 - ethoxy- Phenyl) -3 - piperidyl group, 3 - (4 - n-propoxy-phenoxy) -2 - piperidyl group, 2 - (4 - tert-Butoxy- Phenoxy) -2 - piperidyl group, 4 - (4 - n-butoxy-phenoxy) -2 - piperidyl group, 2 - (2 - trifluoromethyl Phenoxy) -3 - piperidyl group, 3 - (3 - trifluoromethyl-methoxyphenoxy) -4 - piperidinyl, 4 - (4 - Three Fluoro-methoxyphenoxy) -3 - piperidyl group, 3 - (2 - pentafluoroethoxy phenoxy) -2 - piperidyl group, 2 - (4 - Pentafluoro-ethoxy-phenoxy) -1 - piperidinyl, 3 - (2,3 - dimethoxyphenyl)-4 - piperidinyl, 4 - (3,4,5 - trimethoxy-phenyl)-1 - piperidinyl, 4 - (4 - n-pentyloxy-phenoxy) -1 - piperidine Yl, 4 - (4 - n-hexyloxy-phenoxy) -1 - piperidyl group, 4 - benzyl-1 - piperidinyl, 2,4 - dibenzyl -1 - Piperidinyl, 2,4,6 - benzyl-1 - piperidinyl, 2 - (2 - fluoro-benzyl) -1 - piperidinyl, 3 - (2 - (3 - Fluorophenyl) ethyl] -2 - piperidyl group, 4 - (1 - (4 - fluorophenyl) ethyl] -3 - piperidinyl, 2 - (3 - (2 - Chlorophenyl) propyl] -4 - piperidinyl, 3 - (4 - (3 - chlorophenyl) butyl] -5 - piperidinyl, 4 - (5 - (4 - Chlorophenyl) pentyl] -2 - piperidyl group, 5 - ((6 - (2 - bromophenyl) hexyl] -2 - piperidyl group, 6 - (3 - bromo- Benzyl) -3 - piperidyl group, 4 - (4 - bromobenzyl)-1 - piperidinyl, 3 - (2,3 - dichloro-benzyl) -2 - piperidine Yl, 4 - (3,4 - dichloro-benzyl) -3 - piperidyl group, 3 - (2,4 - dichloro-benzyl)-4 - piperidinyl, 2 - (3,4,5 - trichloro-benzyl) -3 - piperidyl group, 6 - (2,4,6 - trichloro-benzyl) -2 - piperidyl group, 3 - (2,3,4,5,6 - pentafluoro-benzyl) -1 - piperidinyl, 4 - (2 - methyl-benzyl) -1 - piperidinyl, 5 - (2 - (3 - methylphenyl) ethyl] -2 - piperidyl group, 6 - (3 - (4 - methylphenyl) propyl]-3 - piperidine Group, 1 - (4 - (2 - ethyl-phenyl) butyl] -4 - piperidinyl, 2 - (5 - (3 - ethylphenyl) pentyl] -1 - Piperidinyl, 3 - (6 - (4 - ethyl-phenyl) hexyl] -2 - piperidyl group, 4 - (4 - n-propyl-benzyl) -3 - piperazine Piperidinyl, 3 - (4 - tert-butylbenzyl)-4 - piperidinyl, 2 - (4 - n-butyl-benzyl) -3 - piperidyl group, 1 - (2 - Trifluoromethyl-benzyl) -2 - piperidyl group, 2 - (3 - (trifluoromethyl) benzyl) -1 - piperidinyl, 4 - (4 - trifluoromethyl Methylbenzyl)-1 - piperidinyl, 1 - (2 - pentafluoroethyl benzyl)-4 - piperidinyl, 1 - (3 - pentafluoroethyl Benzyl)-4 - piperidinyl, 4 - (2,3 - dimethylbenzyl)-1 - piperidinyl, 1 - (3,4,5 - trimethyl-benzyl Yl) -4 - piperidinyl, 1 - (4 - n-pentyl benzyl) -4 - piperidinyl, 4 - (4 - n-hexyl benzyl) -1 - piperazine Piperidinyl, 4 - (2 - methoxy-benzyl) -1 - piperidinyl, 1 - (2 - (3 - methoxyphenyl) ethyl] -4 - piperidine Piperidinyl, 1 - (1 - (4 - methoxyphenyl) ethyl] -4 - piperidinyl, 2 - (3 - (2 - ethoxyphenyl) Yl] -3 - piperidyl group, 3 - (4 - (3 - ethoxy-phenyl) butyl] -4 - piperidinyl, 3 - (4 - (3 - ethoxy- Phenyl) butyl] -4 - piperidinyl, 4 - (5 - (4 - ethoxyphenyl) pentyl] -3 - piperidinyl, 3 - (6 - (4 - N-propoxy-phenyl) hexyl] -2 - piperidinyl, 2 - (4 - tert-butyl-benzyl) -1 - piperidinyl, 1 - (4 - N-butyl-benzyl) -2 - piperidyl group, 2 - (2 - (Trifluoromethoxy) benzyl) -3 - piperidyl group, 3 - (3 - Triple Fluorine-methoxybenzyl) -4 - piperidinyl, 4 - (4 - (Trifluoromethoxy) benzyl) -1 - piperidinyl, 3 - (2 - Five Fluoro-ethoxy benzyl) -2 - piperidyl group, 2 - (4 - pentafluoroethoxy benzyl) -1 - piperidinyl, 1 - (2,3 - Dimethoxy-benzyl)-4 - piperidinyl, 4 - (3,4,5 - trimethoxybenzyl) -1 - piperidinyl, 4 - (4 - N-pentyl-benzyl) -1 - piperidinyl, 4 - (4 - n-hexyl-benzyl) -1 - piperidyl group, 4 - benzyl-3 - Phenoxy-1 - piperidinyl group, 4 - benzyloxy-1 - piperidinyl, 2,4 - benzyloxy-1 - piperidine , 2,4,6 - tris-benzyloxy-1 - piperidinyl group, 2 - ((2 - fluoro-benzyloxy) methyl] -1 - piperidinyl, 3 - (2 - (2 - (3 - fluorophenyl) ethoxy] ethyl) -2 - piperidyl group, 4 - (1 - (1 - (4 - fluorophenyl) ethyl Yl] ethoxy) -3 - piperidinyl, 2 - (3 - (3 - (2 - chlorophenyl) propoxy] propyl) -4 - piperidinyl, 3 - (4 - (4 - (3 - chlorophenyl) butoxy] butyl) -5 - piperidinyl, 4 - (5 - (5 - (4 - chlorophenyl) pentyloxy Yl]-pentyl) -2 - piperidyl group, 5 - (6 - (6 - (2 - bromophenyl) hexyloxy] -2 - piperidyl group, 6 - (3 - bromo- Benzyloxymethyl) -3 - piperidyl group, 4 - (4 - bromo-benzyloxymethyl) -1 - piperidinyl, 3 - (2,3 - dichloro- Benzyloxymethyl) -2 - piperidyl group, 4 - (3,4 - dichloro-benzyloxy)-3 - piperidinyl, 3 - (2,4 - Dichloro-benzyloxymethyl) -4 - piperidinyl, 2 - (3,4,5 - trichloro-methyl-benzyloxy) -3 - piperidyl group, 6 - (2,4,6 - trichloro-methyl-benzyloxy) -2 - piperidyl group, 3 - (2,3,4,5,6 - pentafluoro-benzyloxy methyl Yl) -1 - piperidinyl, 4 - (2 - methyl-benzyloxy)-1 - piperidinyl group, a 5 - (2 - (2 - (3 - methyl-phenyl Yl) ethoxy] ethyl) -2 - piperidyl group, 6 - (3 - (3 - (4 - methylphenyl) propoxy] propyl) -3 - Piperidinyl, 1 - (4 - (4 - (2 - ethylphenyl) butoxy] butyl)-4 - piperidinyl, 2 - (5 - (5 - (3 - Ethylphenyl) pentyloxy] pentyl)-1 - piperidinyl, 3 - (6 - (6 - (4 - ethylphenyl) hexyloxy] hexyl Yl) -2 - piperidyl group, 4 - (4 - n-propyl-methyl-benzyloxy) -3 - piperidyl group, 3 - (4 - tert-butyl-benzyloxy Ylmethyl) -4 - piperidinyl, 2 - (4 - n-butyl methyl-benzyloxy) -3 - piperidyl group, 1 - (2 - trifluoromethyl Methyl-benzyloxy) -2 - piperidyl group, 2 - (3 - (trifluoromethyl) benzyloxy)-1 - piperidinyl, 4 - (4 - (Trifluoromethyl) benzyloxy)-1 - piperidinyl, 1 - (2 - pentafluoroethyl benzyloxymethyl) -4 - piperidine Group, 1 - (3 - pentafluoroethyl benzyloxymethyl) -4 - piperidinyl, 4 - (2,3 - dimethyl-benzyloxy methyl Yl) -1 - piperidinyl, 1 - (3,4,5 - trimethyl-benzyloxy)-4 - piperidinyl, 1 - (4 - n-pentyl Benzyloxymethyl) -4 - piperidinyl, 4 - (4 - n-hexyl-benzyloxymethyl) -1 - piperidinyl, 4 - (2 - methyl Group benzyloxymethyl)-1 - piperidinyl, 1 - (2 - (2 - (3 - methoxyphenyl) ethoxy] ethyl) -4 - Piperidinyl, 1 - (1 - (1 - (4 - methoxyphenyl) ethoxy] ethyl)-4 - piperidinyl, 2 - (3 - (3 - (2 - Ethoxyphenyl) propoxy] propyl) -3 - piperidyl group, 3 - (4 - (4 - (3 - ethoxy-phenyl)-butoxy] Butyl)-4 - piperidinyl, 4 - (5 - (5 - (4 - ethoxyphenyl) pentyloxy] pentyl) -3 - piperidyl group, 3 - (6 - (6 - (4 - n-propoxy-phenyl) hexyloxy] hexyl) -2 - piperidyl group, 2 - (4 - tert-butoxy-benzyl Oxymethyl)-1 - piperidinyl, 1 - (4 - n-butoxy methyl-benzyloxy) -2 - piperidyl group, 2 - (2 - Three Difluoromethoxy-benzyloxymethyl) -3 - piperidyl group, 3 - (3 - trifluoromethoxy-benzyloxy)-4 - piperidine Yl, 4 - (4 - trifluoromethoxy-benzyloxy)-1 - piperidinyl, 3 - (2 - benzyloxy pentafluoroethoxy Methyl) -2 - piperidyl group, 2 - (4 - pentafluoroethoxy benzyloxymethyl)-1 - piperidinyl, 1 - (2,3 - Methoxy-benzyloxy)-4 - piperidinyl, 4 - (3,4,5 - trimethoxy-benzyloxymethyl) -1 - piperidine Yl, 4 - (4 - n-pentyloxy benzyloxymethyl) -1 - piperidinyl, 4 - (4 - n-hexyloxy a benzyloxy Yl) -1 - piperidinyl group, 4 - benzyloxy-3 - phenoxy-1 - piperidinyl group, 4 - benzyl-3 - phenoxy-1 - Piperidinyl, 4 - (4 - chlorophenoxymethyl) - (1 -, 2 - or 3 -) piperidyl group and the like. ...

Pyridyl group (wherein the pyridine ring, may be substituted with at least one group selected from By the (d-1) piperidyl [wherein the piperidine ring can be substituted with at least one group selected from By a phenoxy group (wherein the phenyl ring may be substituted with at least one group selected from the group consisting of halogen Atom, a halogen substituted or unsubstituted C1-C6 alkyl group and a halogen-substituted or unsubstituted C1-C6 alkoxy Group consisting of), a phenyl C1-C6 alkoxy-substituted C1-C6 alkyl group (wherein the phenyl ring, May be substituted with at least one group selected from the group consisting of a halogen atom, a halogen substituted or unsubstituted C1-C6 Alkyl and halogen-substituted or unsubstituted C1-C6 alkoxy group), a phenoxy C1-C6 alkyl group (Wherein the phenyl ring may be substituted with at least one group selected from the group consisting of a halogen atom, a halogen Su substituted or unsubstituted C1-C6 alkyl group and a halogen-substituted or unsubstituted C1-C6 alkoxy group consisting of Group) and a phenyl C1-C6 alkyl group (wherein the phenyl ring may be substituted with at least one group, Selected from the group consisting of a halogen atom, a halogen substituted or unsubstituted C1-C6 alkyl group and a halogen-substituted or unsubstituted C1-C6 alkoxy group) consisting of Group], and (d-2) piperazinyl group [wherein the piperazine ring, May be substituted with at least one group which is selected from C1-C6 alkoxycarbonyl group, a furyl C1-C6 alkoxy group Group [wherein the furan ring, at least one phenyl group may be substituted (wherein the phenyl ring, May be substituted with at least one group selected from the group consisting of a halogen atom, a halogen substituted or unsubstituted C1-C6 Alkyl and halogen-substituted or unsubstituted C1-C6 alkoxy group)], a pyridyl C1-C6 alkyl group [Wherein the pyridine ring, may be substituted with at least one group which is selected from furyl and phenyl (Wherein the phenyl ring may be substituted with at least one group selected from the group consisting of a halogen atom, a halogen Su substituted or unsubstituted C1-C6 alkyl group and a halogen-substituted or unsubstituted C1-C6 alkoxy group consisting of Group) consisting of Group], benzothienyl C1-C6 alkyl group (wherein the benzothiophene ring, can Substituted with at least one group selected from the group consisting of a halogen atom, a halogen substituted or unsubstituted C1-C6 alkyl And a halogen substituted or unsubstituted C1-C6 alkoxy group), a phenyl C2-C6 alkenyl group (wherein In the phenyl ring may be substituted with at least one group selected from the group consisting of a halogen atom, a halogen-substituted Unsubstituted C1-C6 alkyl and halogen-substituted or unsubstituted C1-C6 alkoxy group), Benzofuryl C1-C6 alkyl group [wherein the benzofuran ring can be substituted with at least one group Group, which is selected from a halogen atom, a halogen substituted or unsubstituted C1-C6 alkyl and halogen substituted or unsubstituted Substituted C1-C6 alkoxy group], benzofuryl C2-C6 alkenyl group [wherein the benzofuran The ring may be substituted with at least one group selected from the group consisting of a halogen atom, a halogen substituted or unsubstituted A C1-C6 alkyl group and a halogen-substituted or unsubstituted C1-C6 alkoxy group], a thiazolyl group C1-C6 alkyl group [wherein the thiazole ring, may be substituted with at least one phenyl (wherein the phenyl Base ring may be substituted with at least one group selected from the group consisting of a halogen atom, a halogen substituted or unsubstituted Substituted C1-C6 alkyl group and a halogen-substituted or unsubstituted C1-C6 alkoxy group)], a phenoxy group C1-C6 alkyl group (wherein the phenyl ring may be substituted with at least one group selected from the group consisting of halogen Atom, a halogen substituted or unsubstituted C1-C6 alkyl group and a halogen-substituted or unsubstituted C1-C6 alkoxy Group consisting of), indolyl C1-C6 alkyl group (wherein the indole ring, may be substituted with at least A group selected from the group consisting of a halogen atom, a halogen substituted or unsubstituted C1-C6 alkyl and halo-substituted Unsubstituted C1-C6 alkoxy group) and a phenyl C1-C6 alkyl group (wherein the phenyl ring , It can be substituted with at least one group which is selected from benzofuranyl, a halogen atom, a halogen- Substituted or unsubstituted C1-C6 alkyl group and a halogen-substituted or unsubstituted C1-C6 alkoxy group) The group consisting of] the group consisting of) include pyridine group (wherein the pyridine ring can be substituted with 1 To 3 substituents selected from (d-1) a pyridyl group [wherein the piperidine ring may be substituted with 1 To 5, preferably 1 to 3 substituents selected from a phenoxy group (wherein the phenyl ring may be Substituted with 1 to 5, preferably 1 to 3 substituents, selected from the group consisting of a halogen atom, a halogen substituted or unsubstituted Substituted C1-C6 alkyl group and a halogen-substituted or unsubstituted C1-C6 alkoxy group), a phenyl group C1-C6 alkoxy-substituted C1-C6 alkyl group (wherein the phenyl ring may be substituted with 1 to 5, Preferably 1 to 3 substituents selected from the group consisting of a halogen atom, a halogen substituted or unsubstituted C1-C6 alkyl and Halogen-substituted or unsubstituted C1-C6 alkoxy group), as described later in the alkyl portion Stars having from 1 to 6 carbon atoms, a straight-chain or branched-chain alkyl phenoxy C1-C6 alkyl group (wherein In the phenyl ring may be substituted with 1 to 5, preferably 1 to 3 substituents selected from halogen atoms Son, halogen-substituted or unsubstituted C1-C6 alkyl and halogen-substituted or unsubstituted C1-C6 alkoxy group The group consisting of) and the above C1-C6 alkyl phenyl (wherein the phenyl ring may be substituted From 1 to 5, preferably 1 to 3 substituents selected from the group consisting of a halogen atom, a halogen substituted or unsubstituted C1-C6 alkyl group and a halogen-substituted or unsubstituted C1-C6 alkoxy group) from the group consisting] and (D-2) piperazinyl group [wherein the piperazine ring may be substituted with 1 to 3 substituents selected from As described above, a C1-C6 alkoxycarbonyl group, as described later in the alkyl portion contains 1 having To 6 carbon atoms, a straight-chain or branched-chain alkyl C1-C6 alkyl furyl [wherein the furan ring, May be substituted with 1 to 3 phenyl group (wherein the phenyl ring may be substituted with 1 to 5, preferably 1 To 3 substituents selected from the group consisting of a halogen atom, a halogen substituted or unsubstituted C1-C6 alkyl and halo Substituted or unsubstituted C1-C6 alkoxy group)], as described later in the alkyl portion Having from 1 to 6 carbon atoms, a straight-chain or branched-chain alkyl C1-C6 alkyl pyridyl group [wherein the The pyridine ring may be substituted with 1 to 3 substituents selected from furyl group, and a phenyl group (wherein In the phenyl ring may be substituted with 1 to 5, preferably 1 to 3 substituents selected from halogen atoms Son, halogen-substituted or unsubstituted C1-C6 alkyl and halogen-substituted or unsubstituted C1-C6 alkoxy group The group consisting of) the group consisting of], as described later in the alkyl part has from 1 to 6 carbon Atoms, straight-chain or branched-chain alkyl group benzothienyl C1-C6 alkyl group (wherein the benzothiophene ring , It can be substituted with 1 to 3 substituents selected from the group consisting of a halogen atom, a halogen substituted or unsubstituted C1-C6 alkyl group and a halogen-substituted or unsubstituted C1-C6 alkoxy group), as described later Phenyl C2-C6 alkenyl group (which has having 2 to 6 carbon atoms, a straight-chain or branched alkenyl group having from 1 To 3 double bonds, including the trans-and cis-form) (wherein the phenyl ring may be substituted with 1 To 5, preferably 1 to 3 substituents, selected from the group consisting of a halogen atom, a halogen substituted or unsubstituted C1-C6 Alkyl and halogen-substituted or unsubstituted C1-C6 alkoxy group), as described later in this An alkyl group having from 1 to 6 carbon atoms, a straight-chain or branched-chain alkyl group benzofuryl C1-C6 alkoxy Group [wherein the benzofuran ring can be substituted with 1 to 3 substituents selected from a halogen atom, Halogen-substituted or unsubstituted C1-C6 alkyl group and a halogen-substituted or unsubstituted C1-C6 alkoxy Group], as described later benzofuryl C2-C6 alkenyl group (the alkenyl moiety containing 2 having To 6 carbon atoms, a straight-chain or branched alkenyl group having 1-3 double bonds, including the trans-and cis-form) (Wherein the benzofuran ring can be substituted with 1 to 3 substituents selected from a halogen atom, Halogen-substituted or unsubstituted C1-C6 alkyl group and a halogen-substituted or unsubstituted C1-C6 alkoxy Group), as described later in the alkyl portion has from 1 to 6 carbon atoms, a straight-chain or Thiazolyl branched alkyl C1-C6 alkyl group [wherein the thiazole ring, may be substituted with 1 or 2 benzene Group (wherein the phenyl ring may be substituted with 1 to 5, preferably 1 to 3 substituents selected from the Consisting of a halogen atom, a halogen substituted or unsubstituted C1-C6 alkyl group and a halogen-substituted or unsubstituted C1-C6 alkoxy group)], as described later in the alkyl part has from 1 to 6 Carbon atoms, straight-chain or branched-chain alkyl phenoxy C1-C6 alkyl group (wherein the indole ring, it can be With substituted with 1 to 3 substituents selected from the group consisting of a halogen atom, a halogen substituted or unsubstituted C1-C6 Alkyl and halogen-substituted or unsubstituted C1-C6 alkoxy group), as described later in this The alkyl part has from 1 to 6 carbon atoms, a straight-chain or branched-chain alkyl indolyl C1-C6 alkoxy Group (wherein the phenyl ring may be substituted with 1 to 5, preferably 1 to 3 substituents selected from the Consisting of a halogen atom, a halogen substituted or unsubstituted C1-C6 alkyl group and a halogen-substituted or unsubstituted C1-C6 alkoxy group) and a phenyl C1-C6 alkyl group (wherein the phenyl ring may be With substituted with 1 to 5, preferably 1 to 3 substituents, selected from the free-benzofuranyl group, a halogen atom, Halogen-substituted or unsubstituted C1-C6 alkyl group and a halogen-substituted or unsubstituted C1-C6 alkoxy Groups) the group consisting of] the group consisting of), such as 2 - pyridyl group, a 3 - pyridyl group, a 4 - pyridyloxy Group, 3 - (1 - piperidinyl) - 2 - pyridyl group, a 2 - (4 - piperidinyl) -3 - pyridyloxy group, 4 - (2 - piperidine Yl) -3 - pyridyloxy group, 5 - (3 - piperidinyl) - 2 - pyridyl group, a 2,4 - bis (1 - piperidinyl) -3 - pyridine Piperidinyloxy, 2 - (1 - piperidinyl) -4 - (2 - (2 - fluorophenoxy)-1 - piperidinyl] -3 - pyridyloxy group, 2,4,6 - tris (1 - piperidinyl) -, methyl group, 2 - (4 - phenoxy-1 - piperidinyl) -3 - pyridyloxy Group, 2 - (2,4 - diphenyl-1 - piperidinyl) -3 - pyridyl group, a 3 - (2,4,6 - triphenyl-1 - Piperidyl)-4 - pyridyl group, a 4 - (2 - (2 - fluorophenoxy)-1 - piperidinyl] -2 - pyridinyl group, 5 - (3 - (3 - fluorophenoxy) -2 - piperidyl] -3 - pyridyloxy group, 6 - (4 - (4 - fluorophenyl) -3 - piperazine Piperidinyl]-4 - pyridyl group, a 2 - (2 - (2 - chlorophenoxy) -4 - piperidinyl] -3 - pyridyloxy group, 3 - (3 - (3 - chlorophenoxy) -5 - piperidinyl]-4 - pyridyl group, a 4 - (4 - (4 - chlorophenoxy) -5 - piperazine Piperidinyl]-4 - pyridyl group, a 5 - (5 - (2 - bromophenyl) -2 - piperidyl] -3 - pyridyloxy group, 2 - (6 - (3 - bromophenyl) -3 - piperidinyl]-4 - pyridyl group, a 2 - (4 - (4 - bromophenyl)-1 - piperazine Piperidinyl]-2 - pyridyloxy group, 3 - (3 - (2,3 - dichlorophenoxy) -2 - piperidyl] -4 - pyridyloxy, 3 - (4 - (3,4 - dichlorophenoxy) -3 - piperidinyl]-4 - pyridyl group, a 4 - (3 - (2,4 - dichloro-phenoxy Yl) -4 - piperidinyl]-2 - pyridyloxy group, 5 - (2 - (3,4,5 - trichlorophenyl) -3 - piperidinyl] -2 - Pyridyloxy group, 6 - (6 - (2,4,6 - trichlorophenyl) -2 - piperidyl] -3 - pyridyloxy group, 2 - (3 - (2,3,4,5,6 - pentafluorophenoxy)-1 - piperidinyl] -3 - pyridyloxy group, 4 - (4 - (2 - methyl- Phenoxy)-1 - piperidinyl] - 2 - pyridyl group, a 3 - (5 - (3 - methyl-phenoxy) -2 - piperidinyl] -2 - Pyridyloxy group, 5 - (6 - (4 - methyl-phenoxy) -3 - piperidinyl] -3 - pyridyloxy group, 2 - (1 - (2 - ethyl Phenoxy) -4 - piperidinyl]-4 - pyridyl group, a 2 - (2 - (3 - phenoxy-ethyl) -1 - piperidine Yl] -3 - pyridyloxy group, 3 - (3 - (4 - ethyl-phenoxy) -2 - piperidyl] -4 - pyridyloxy, 4 - (4 - (4 - n-propyl-phenoxy) -3 - piperidinyl]-2 - pyridyl group, a 5 - (5 - (4 - tert-butyl-phenoxy Yl) -4 - piperidinyl] -3 - pyridyloxy group, 6 - (2 - (4 - n-butyl-phenoxy) -3 - piperidinyl] -2 - pyridine Piperidinyloxy, 2 - (1 - (2 - (trifluoromethyl) phenoxy) -2 - piperidyl]-4 - pyridyl group, a 3 - (2 - (3 - Trifluoromethylphenoxy)-1 - piperidinyl]-4 - pyridyl group, a 4 - (3 - (4 - (trifluoromethyl) phenoxy Yl) -1 - piperidinyl]-2 - pyridyl group, a 5 - (1 - (2 - phenoxy-pentafluoroethyl) -4 - piperidinyl] -3 - Pyridyloxy group, 6 - (1 - (3 - pentafluoroethyl-phenoxy)-4 - piperidinyl] - 2 - pyridyl group, 2 - (4 - (2,3 - dimethoxy-phenoxy)-1 - piperidinyl] -3 - pyridyloxy group, 3 - (1 - (3,4,5 - Phenoxy) -4 - piperidinyl]-2 - pyridyl group, a 4 - (1 - (4 - n-pentyloxy-phenoxy)-4 - piperidine Yl] -3 - pyridyloxy group, 5 - (4 - (4 - n-hexyl-phenoxy) -1 - piperidinyl] - 2 - pyridyl group, 6 - (4 - (2 - methoxyphenoxy) -1 - piperidinyl]-2 - pyridyl group, a 2 - (1 - (3 - methoxy-phenoxy Yl) -4 - piperidinyl]-4 - pyridyl group, a 3 - (1 - (4 - methoxyphenoxy) -4 - piperidinyl] -2 - pyridine Oxyl, 4 - (2 - (2 - phenoxy-ethoxy) -3 - piperidinyl]-2 - pyridyl group, a 5 - (3 - (3 - B Phenoxy) -4 - piperidinyl] -3 - pyridyloxy group, 2 - (4 - (4 - ethoxy-phenoxy) -5 - piperidine Yl] -4 - pyridyloxy, 2 - (3 - (4 - n-propoxy-phenoxy) -2 - piperidyl] -4 - pyridyloxy, 3 - (2 - (4 - tert-butoxy-phenoxy)-1 - piperidinyl]-4 - pyridyl group, a 4 - (1 - (4 - n-butoxy- Phenoxy) -2 - piperidinyl] - 2 - pyridyl group, a 5 - (2 - (2 - trifluoromethoxyphenoxy) -3 - piperidine Yl] -2 - pyridinyl group, a 6 - (3 - (3 - trifluoromethyl-methoxyphenoxy) -4 - piperidinyl] - 2 - pyridyl group, 6 - (4 - (4 - (Trifluoromethoxy) phenoxy) -3 - piperidinyl]-2 - pyridyl group, a 2 - (3 - (2 - pentafluoroethyl Phenoxy) -2 - piperidyl] -3 - pyridyloxy group, 3 - (4 - (4 - pentafluoro-ethoxy-phenoxy) -1 - Piperidinyl]-2 - pyridyl group, a 4 - (1 - (2,3 - dimethoxyphenyl)-4 - piperidinyl] -2 - pyridinyl Group, a 5 - (4 - (3,4,5 - trimethoxy-phenyl)-1 - piperidinyl] -3 - pyridyloxy group, 6 - (4 - (4 - N-pentyl phenoxy)-1 - piperidinyl] -3 - pyridyloxy group, 5 - (4 - (4 - n-hexyloxyphenoxy Yl) -1 - piperidinyl] -3 - pyridyloxy group, 2 - (4 - (4 - (trifluoromethyl) benzyloxy)-1 - piperidine Yl] -5 - pyridyloxy group, 2 - (4 - trifluoromethoxy-benzyl-1 - piperidinyl) -5 - pyridyloxy, 2 - (4 - (4 - chlorobenzyl) -1 - piperazinyl] -5 - pyridyloxy group, 2 - (4 - (4 - (trifluoromethyl) benzyl) -1 - Piperidinyl] -5 - pyridyloxy group, 2 - (4 - (4 - chloro-benzyloxy)-1 - piperazinyl] -5 - pyridyloxy group, 4 - (4 - fluoro-benzyl-1 - piperazinyl)-6 - pyridyl group, a 4 - phenoxy-3 - (4 - (4 - (trifluoromethoxy) benzyl Oxymethyl)-1 - piperidinyl] - 2 - pyridyl group, a 2 - (4 - tert-butoxycarbonyl group - (1 -, 2 - or 3 -) -Piperazinyl] - (3 -, 4 -, 5 - or 6 -) pyridyloxy group, 2 - (4 - (4 - ((2 -, 3 -, 4 -, 5 -, 6 - Or 7 -) benzofuryl] benzyl) - (1 -, 2 - or 3 -) piperazinyl] - (3 -, 4 -, 5 - or 6 -) pyridine Group, a 2 - (4 - (3 - ((2 - or 3 -) furyl] pyridylmethyl) - (1 -, 2 - or 3 -)-piperazine Yl] - (3 -, 4 -, 5 - or 6 -) pyridyloxy group, 2 - (4 - (2 - (4 - trifluoromethoxyphenyl) pyridyl Methyl] - (1 -, 2 - or 3 -) piperazinyl) - (3 -, 4 -, 5 - or 6 -) pyridyloxy group, 2 - (4 - (2 - (3 - Chloro-4 - fluorophenyl) pyridylmethyl] - (1 -, 2 - or 3 -) piperazinyl) - (3 -, 4 -, 5 - or 6 -) pyridine Piperidinyloxy, 2 - (4 - (5 - (trifluoromethyl) - (2 -, 3 -, 4 -, 6 - or 7 -) methyl-benzofuranyl Yl] - (1 -, 2 - or 3 -) piperazinyl) - (3 -, 4 -, 5 - or 6 -) pyridyloxy group, 2 - (4 - (6 - trifluoromethyl Methyl - (2 -, 3 -, 4 -, 5 - or 7 -) benzofuran-ylmethyl] - (1 -, 2 - or 3 -)-piperazine Yl) - (3 -, 4 -, 5 - or 6 -) pyridyloxy group, 2 - (4 - (5 - chloro - (2 -, 3 -, 4 -, 6 - or 7 -) Benzothienyl methyl] - (1 -, 2 - or 3 -) piperazinyl) - (3 -, 4 -, 5 - or 6 -) pyridyloxy group, 2 - (4 - (6 - chloro - (2 -, 3 -, 4 -, 5 - or 7 -) benzofuran-ylmethyl] - (1 -, 2 - or 3 -)-piperazine Yl) - (3 -, 4 -, 5 - or 6 -) pyridyloxy group, 2 - (4 - (5 - (Trifluoromethoxy) - (2 -, 3 -, 4 -, 6 - Or 7 -) benzofuran-ylmethyl] - (1 -, 2 - or 3 -) piperazinyl) - (3 -, 4 -, 5 - or 6 -) pyridyloxy Group, 2 - (4 - (3 - (4 - (trifluoromethyl) phenyl) -2 - propenyl] - (1 -, 2 - or 3 -) piperazinyl) pyridine Group, a 2 - (4 - (3 - (3,4 - dichlorophenyl) -2 - propenyl] - (1 -, 2 - or 3 -) piperazinyl) pyridine Group, a 2 - (4 - (3 - (4 - chlorophenyl) -2 - propenyl] - (1 -, 2 - or 3 -) piperazinyl) pyridine group, 2 - (4 - (3 - (6 - (trifluoromethyl) - (2 -, 3 -, 4 -, 5 - or 7 -) benzofuryl] -2 - propenyl Yl) - (1 -, 2 - or 3 -) piperazinyl] pyridyloxy group, 2 - (4 - (3 - (5 - chloro - (2 -, 3 -, 4 -, 5 - Or 7 -) benzofuryl] -2 - propenyl) - (1 -, 2 - or 3 -) piperazinyl] pyridine group, 2 - (4 - (5 - chloro - (2 -, 3 -, 4 -, 6 - or 7 -) benzofuran-ylmethyl] - (1 -, 2 - or 3 -)-piperazine Yl) - (3 -, 4 -, 5 - or 6 -) pyridyloxy group, 2 - (4 - (2 - (4 - trifluoromethyl-phenyl) - (4 - or 5 -) - Thiazolyl methyl] - (1 -, 2 - or 3 -) piperazinyl) pyridine group, a 2 - (4 - (2 - (4 - (Trifluoromethoxy) Phenoxy) ethyl] - (1 -, 2 - or 3 -) piperazinyl) pyridine group, a 2 - (4 - (3 - (4 - (Trifluoromethoxy) Phenyl) -2 - propenyl] - (1 -, 2 - or 3 -) piperazinyl) pyridine group, a 2 - (4 - (5 - (Trifluoromethoxy) - (1 -, 2 -, 3 -, 4 -, 6 - or 7 -) indolylmethyl] - (1 -, 2 - or 3 -) piperazinyl) pyridine oxide Group, 2 - (4 - (4 - chlorophenoxymethyl) - (1 -, 2 - or 3 -) piperidyl] - (3 -, 4 -, 5 - or 6 -) Pyridyloxy group, 2 - (4 - (2 - (4 - chlorophenyl) - (3 -, 4 - or 5 -) furylmethyl] - (1 -, 2 -, or 3 -) piperazinyl) pyridine group, a 2 - (4 - (2 - (2 - chloro-5 - trifluoromethyl-phenyl) - (3 -, 4 - or 5 -) Furyl methyl] - (1 -, 2 - or 3 -) piperazinyl) pyridine group. ...

1,2,3,4-tetrahydroquinoline oxygen base (wherein this 1,2,3, on the 4-tetrahydroquinoline ring, can be substituted with at least one group, it is selected from by the oxo base, phenyl is [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group] and phenyl C1-C6 alkyl [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group] group formed) comprise 1,2,3,4-tetrahydroquinoline oxygen base [wherein this 1,2,3, on the 4-tetrahydroquinoline ring, can be substituted with 1 to 3 substituting group, it is selected from by the oxo base, aforesaid phenyl is (wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 substituting group, it is selected from by halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group) and aforesaid phenyl C1-C6 alkyl (wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 substituting group, it is selected from by halogen atom, the group that halogen replacement or unsubstituted C1-C6 alkyl and halogen replacement or unsubstituted C1-C6 alkoxyl group are formed) group of forming], for example 1,2,3,4-tetrahydrochysene-(1-, 2-, 3-, 4-, 5-, 6-, 7-or 8-) quinoline oxy, 1-(4-trifluoromethyl benzyl)-2-oxo-1,2,3,4-tetrahydrochysene-6-quinoline oxy, 1-(4-trifluoro-methoxybenzyl)-2-oxo-1,2,3,4-tetrahydrochysene-6-quinoline oxy, 1-(4-benzyl chloride base)-2-oxo-1,2,3,4-tetrahydrochysene-6-quinoline oxy, 1-(4-trifluoromethyl benzyl)-1,2,3,4-tetrahydrochysene-6-quinoline oxy, 1-(4-trifluoro-methoxybenzyl)-1,2,3,4-tetrahydrochysene-6-quinoline oxy, 1-(4-benzyl chloride base)-1,2,3,4-tetrahydrochysene-6-quinoline oxy, 1-(4-chloro-phenyl-)-1,2,3,4-tetrahydrochysene-6-quinoline oxy, 1-(4-Trifluoromethoxyphen-l)-1,2,3,4-tetrahydrochysene-6-quinoline oxy, 1-(4-trifluoromethyl)-1,2,3,4-tetrahydrochysene-6-quinoline oxy, 1-(3, the 4-dichloro benzyl)-1,2,3,4-tetrahydrochysene-6-quinoline oxy, 1-(3,4-two (trifluoromethoxy) benzyl]-1,2,3,4-tetrahydrochysene-6-quinoline oxy, 1-(4-chloro-phenyl-)-1,2,3,4-tetrahydrochysene-5-quinoline oxy, 1-(4-Trifluoromethoxyphen-l)-1,2,3,4-tetrahydrochysene-5-quinoline oxy, 1-(4-trifluoromethyl)-1,2,3,4-tetrahydrochysene-5-quinoline oxy, 1-(4-benzyl chloride base)-1,2,3,4-tetrahydrochysene-5-quinoline oxy, 1-(4-trifluoro-methoxybenzyl)-1,2,3,4-tetrahydrochysene-5-quinoline oxy, 1-(4-trifluoromethyl benzyl)-1,2,3,4-tetrahydrochysene-5-quinoline oxy, 1-(3,4,5-three (trifluoromethyl) benzyl]-1,2,3,4-tetrahydrochysene-6-quinoline oxy, 1-benzyl-4-phenyl-1,2,3,4-tetrahydrochysene-6-quinoline oxy, 1-phenyl-4,6-dibenzyl-1,2,3,4-tetrahydrochysene-5-quinoline oxy, 4-phenyl-2-oxo-1,2,3,4-tetrahydrochysene-1-quinoline oxy etc.

1,2,3,4-tetrahydrochysene naphthyloxy (wherein this 1,2,3, on the 4-tetrahydric naphthalene ring, can be substituted with at least one oxo base) comprise 1,2,3,4-tetrahydrochysene naphthyloxy (wherein this 1,2,3, on the 4-tetrahydric naphthalene ring, can be substituted with 1 to 3 oxo base), (1-, 2-, 5-or 6-) 1 for example, 2,3,4-tetrahydrochysene naphthyloxy, 4-oxo-7-1,2,3,4-tetrahydrochysene naphthyloxy, 1,4-dioxo-6-1,2,3,4-tetrahydrochysene naphthyloxy, 1,2,4-trioxy--5-1,2,3,4-tetrahydrochysene naphthyloxy etc.

2H-chromene oxygen base is (wherein on this 2H-chromene ring, can be substituted with at least one oxo base) comprise that 2H-chromene oxygen base is (wherein on this 2H-chromene ring, can be substituted with at least one oxo base), for example 2H-chromene oxygen base, 2-oxo-2H-chromene oxygen base etc.

Naphthyloxy is (wherein on this naphthalene nucleus, can be substituted with at least one piperidyl [wherein on this piperidines basic ring, can be substituted with at least one phenoxy group (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed)]) comprise that naphthyloxy is (wherein on this naphthalene nucleus, can be substituted with 1 to 3 aforesaid piperidyl [wherein on this piperidine ring, can be substituted with 1 to 3 phenoxy group (wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 substituting group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed)]), (1-or 2-) naphthyloxy for example, 6-(4-(4-Trifluoromethyl phenyl ether oxygen base)-piperidino]-the 2-naphthyloxy, 5-(piperidino)-2-naphthyloxy, 2-(4-piperidyl)-3-naphthyloxy, 4-(2-piperidyl)-1-naphthyloxy, 5-(3-piperidyl)-2-naphthyloxy, 5,6-two (piperidino)-1-naphthyloxy, 7-(piperidino)-6-(2-(2-fluorophenoxy)-piperidino]-the 1-naphthyloxy, 5,6,7-three (piperidino)-2-naphthyloxy, 6-(4-phenoxy group-piperidino)-3-naphthyloxy, 2-(2,4-hexichol Oxy-1-piperidyl)-the 4-naphthyloxy, 3-(2,4,6-triple phenoxyl-piperidino)-the 5-naphthyloxy, 4-(2-(2-fluorophenoxy)-piperidino]-the 6-naphthyloxy, 4-(3-(3-fluorophenoxy)-2-piperidyl]-the 2-naphthyloxy, 3-(4-(4-fluorophenoxy)-3-piperidyl]-the 1-naphthyloxy, 5-(2-(2-chlorophenoxy)-4-piperidyl]-the 2-naphthyloxy, 6-(3-(3-chlorophenoxy)-5-piperidyl]-the 1-naphthyloxy, 4-(4-(4-chlorophenoxy)-2-piperidyl]-the 2-naphthyloxy, 5-(5-(2-bromine phenoxy group)-2-piperidyl]-the 3-naphthyloxy, 6-(6-(3-bromine phenoxy group)-3-piperidyl]-the 4-naphthyloxy, 6-(4-(4-bromine phenoxy group)-piperidino]-the 2-naphthyloxy, (3-(2 for 3-, the 3-dichlorophenoxy)-the 2-piperidyl]-the 4-naphthyloxy, (4-(3 for 6-, the 4-dichlorophenoxy)-the 3-piperidyl]-the 1-naphthyloxy, (3-(2 for 4-, the 4-dichlorophenoxy)-the 4-piperidyl]-the 2-naphthyloxy, (2-(3 for 5-, 4, the 5-Trichlorophenoxy)-the 3-piperidyl]-the 2-naphthyloxy, (6-(2 for 6-, 4, the 6-Trichlorophenoxy)-the 2-piperidyl]-the 3-naphthyloxy, (3-(2 for 2-, 3,4,5,6-penta fluoro benzene oxygen base)-piperidino]-the 3-naphthyloxy, 4-(4-(2-methylphenoxy)-piperidino]-the 2-naphthyloxy, 3-(5-(3-methylphenoxy)-2-piperidyl]-the 2-naphthyloxy, 5-(6-(4-methylphenoxy)-3-piperidyl]-the 3-naphthyloxy, 6-(1-(2-ethyl phenoxy group)-4-piperidyl]-the 4-naphthyloxy, 2-(2-(3-ethyl phenoxy group)-piperidino]-the 3-naphthyloxy, 3-(3-(4-ethyl phenoxy group)-2-piperidyl]-the 4-naphthyloxy, 4-(4-(4-n-propyl phenoxy group)-3-piperidyl]-the 2-naphthyloxy, 5-(5-(4-tertiary butyl phenoxy group)-4-piperidyl]-the 1-naphthyloxy, 6-(2-(4-normal-butyl phenoxy group)-3-piperidyl]-the 2-naphthyloxy, 2-(1-(2-4-trifluoromethylphenopendant)-2-piperidyl]-the 4-naphthyloxy, 3-(2-(3-4-trifluoromethylphenopendant)-piperidino]-the 4-naphthyloxy, 4-(3-(4-4-trifluoromethylphenopendant)-piperidino]-the 2-naphthyloxy, 5-(1-(2-pentafluoroethyl group phenoxy group)-4-piperidyl]-the 3-naphthyloxy, 6-(1-(3-pentafluoroethyl group phenoxy group)-4-piperidyl]-the 2-naphthyloxy, (4-(2 for 2-, the 3-dimethyl phenoxy)-piperidino]-the 1-naphthyloxy, (1-(3 for 3-, 4,5-trimethylammonium phenoxy group)-the 4-piperidyl]-the 2-naphthyloxy, 4-(1-(4-n-pentyl phenoxy group)-4-piperidyl]-the 1-naphthyloxy, 5-(4-(4-n-hexyl phenoxy group)-piperidino]-the 2-naphthyloxy, 6-(4-(2-methoxyl group phenoxy group)-piperidino]-the 2-naphthyloxy, 2-(1-(3-methoxyl group phenoxy group)-4-piperidyl]-the 4-naphthyloxy, 3-(1-(4-methoxyl group phenoxy group)-4-piperidyl]-the 2-naphthyloxy, 4-(2-(2-ethoxy phenoxy)-3-piperidyl]-the 2-naphthyloxy, 5-(3-(3-ethoxy phenoxy)-4-piperidyl]-the 1-naphthyloxy, 6-(4-(4-ethoxy phenoxy)-5-piperidyl]-the 4-naphthyloxy, 2-(3-(4-positive propoxy phenoxy group)-2-piperidyl]-the 4-naphthyloxy, 3-(2-(4-tert.-butoxy phenoxy group)-piperidino]-the 4-naphthyloxy, 4-(1-(4-n-butoxy phenoxy group)-2-piperidyl]-the 2-naphthyloxy, 5-(2-(2-Trifluoromethyl phenyl ether oxygen base)-3-piperidyl]-the 2-naphthyloxy, 6-(3-(3-Trifluoromethyl phenyl ether oxygen base)-4-piperidyl]-the 2-naphthyloxy, 6-(4-(4-Trifluoromethyl phenyl ether oxygen base)-3-piperidyl]-the 2-naphthyloxy, 2-(3-(2-five fluorine ethoxy phenoxies)-2-piperidyl]-the 3-naphthyloxy, 3-(4-(4-five fluorine ethoxy phenoxies)-piperidino]-the 2-naphthyloxy, (1-(2 for 4-, 3-dimethoxy phenoxy group)-the 4-piperidyl]-the 2-naphthyloxy, (4-(3 for 5-, 4,5-trimethoxy phenoxy group)-piperidino]-the 1-naphthyloxy, 6-(4-(4-n-pentyloxy phenoxy group)-piperidino]-the 3-naphthyloxy, 5-(4-(the positive hexyloxy phenoxy group of 4-)-piperidino]-the 1-naphthyloxy etc.

1,2,3,4-tetrahydroisoquinoline oxygen base (wherein this 1,2,3, on the 4-tetrahydroisoquinoline ring, can be substituted with at least one group, it is selected from the alkoxy carbonyl by C1-C6, phenyl C1-C6 alkyl is [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group] and phenyl [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group] group formed) comprise 1,2,3,4-tetrahydroisoquinoline oxygen base (wherein this 1,2,3, on the 4-tetrahydroisoquinoline ring, can be substituted with 1 to 3 substituting group, it is selected from the alkoxy carbonyl by C1-C6, phenyl C1-C6 alkyl is (wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 substituting group, it is selected from by halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group) and aforesaid phenyl [wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 substituting group, it is selected from by halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group] group formed), for example 1,2,3,4-tetrahydro isoquinolyl (1-, 2-, 3-, 4-, 5-, 6-, 7-or 8-) quinoline oxy, 2-tert-butoxycarbonyl-1,2,3,4-tetrahydrochysene-6-isoquinoline 99.9 oxygen base, 2-(4-benzyl chloride base)-1,2,3,4-tetrahydrochysene-6-isoquinoline 99.9 oxygen base, 2-(4-trifluoro-methoxybenzyl)-1,2,3,4-tetrahydrochysene-6-isoquinoline 99.9 oxygen base, 2-(4-trifluoromethyl benzyl)-1,2,3,4-tetrahydrochysene-6-isoquinoline 99.9 oxygen base, 2-ethoxy carbonyl-4-benzyl-1,2,3,4-tetrahydrochysene-7-isoquinoline 99.9 oxygen base, 1,4,6-tribenzyl-1,2,3,4-tetrahydrochysene-8-isoquinoline 99.9 oxygen base, 1-(3,4-two (trifluoromethoxy) benzyl]-1,2,3,4-tetrahydrochysene-6-isoquinoline 99.9 oxygen base, 1-(3,4,5-three (trifluoromethyl) benzyl]-1,2,3,4-tetrahydrochysene-6-isoquinoline 99.9 oxygen base, 2-(4-Trifluoromethoxyphen-l)-(1-, 3-, 4-, 5-, 6-, 7-or 8-) isoquinoline 99.9 oxygen base etc.

Phenyl is [wherein on this benzyl ring, be substituted with at least one piperidyl (wherein on this piperidine ring, can be substituted with at least one phenoxy group [wherein on this phenyl, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed])] comprise that phenyl is [wherein on this benzyl ring, be substituted with 1 to 3 aforesaid piperidyl (wherein on this piperidine ring, can be substituted with 1 to 3 phenoxy group [wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 substituting group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed])], 4-(piperidino) phenyl for example, 3-(2-piperidyl) phenyl, 4-(4-(4-Trifluoromethyl phenyl ether oxygen base)-piperidino] phenyl, 4-(4-(4-4-trifluoromethylphenopendant)-piperidino] phenyl, 4-(4-(4-chlorophenoxy)-piperidino] phenyl, (4-(3 for 4-, 4-two (trifluoromethoxy) phenoxy group-piperidino]) phenyl, (4-(3 for 4-, 4,5-three (trifluoromethyl) phenoxy group-piperidino]) phenyl, (4-(2 for 4-, the 4-dichlorophenoxy)-and piperidino] phenyl, (4-(2 for 4-, 4,6-trifluoromethoxy phenoxy base)-and piperidino] phenyl, 2-(2,4,5-triple phenoxyl-piperidino) phenyl, 3-(1,2-two phenoxy groups-4-piperidyl) phenyl, 2,4-two (4-piperidyl) phenyl, 2,4,6-three (3-piperidyl) phenyl etc.

Phenyl C1-C6 alkyl is [wherein on this benzyl ring, be substituted with at least one group, it is selected from by at least one piperidyl (wherein on this piperidine ring, be substituted with phenoxy group [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group]) and group-NR ²⁴R ²⁵(R ²⁴Represent halogen atom or C1-C6 alkyl, R ²⁵Represent phenyl C2-C6 thiazolinyl [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group]) group formed] comprise that aforesaid phenyl C1-C6 alkyl is [wherein on this benzyl ring, be substituted with 1 to 3 substituting group, it is selected from by 1 to 3 aforesaid piperidyl (wherein on this piperidine ring, be substituted with 1 to 3 phenoxy group [wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 substituting group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed]) and group-NR ²⁴R ²⁵(R ²⁴Represent halogen atom or C1-C6 alkyl, R ²⁵The representative phenyl C2-C6 thiazolinyl [group of forming by 1 or 2 phenyl and thiazolinyl as hereinafter described, described phenyl is unsubstituted or by 1 to 5, preferred 1 to 3 substituting group replaces, described substituting group is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed, described thiazolinyl contains 2 to 6 carbon atoms, have 1 to 3 two key]) group formed], 4-(piperidino) benzyl for example, 2,4-two (4-piperidyl) benzyl, 2,4,6-three (2-piperidyl) benzyl, 4-(4-(4-Trifluoromethyl phenyl ether oxygen base)-piperidino] benzyl, 4-(N-methyl-N-(4-trifluoromethoxy cinnamyl) amino] benzyl, 4-(N-(4-trifluoromethoxy cinnamyl) amino] benzyl, 4-(4-(4-4-trifluoromethylphenopendant)-piperidino] benzyl, 4-(4-(4-chlorophenoxy)-piperidino] benzyl, (4-(3 for 4-, 4-two (trifluoromethoxy) phenoxy group]-piperidino) benzyl, (4-(2 for 4-, 4,6-three (trifluoromethyl) phenoxy group]-piperidino) benzyl, (4-(2 for 4-, the 4-dichlorophenoxy)-and piperidino] benzyl, (4-(2 for 4-, 4,6-trifluoromethoxy phenoxy base)-and piperidino] benzyl, 3-(2,4-two phenoxy groups-3-piperidyl] benzyl, 2-(1,2,3-triple phenoxyl-4-piperidyl] benzyl, 4-(N-methyl-N-(4-trifluoromethoxy cinnamyl) amino]-3-(4-(4-Trifluoromethyl phenyl ether oxygen base)-piperidino] benzyl etc.

Piperidyl C1-C6 alkyl is (wherein on this piperidine ring, be substituted with at least one phenyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed)) comprise that piperidyl C1-C6 alkyl is (wherein on this piperidine ring, be substituted with 1 to 3 aforesaid phenyl (wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 substituting group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed)), (4-phenyl-piperidino) methyl for example, 2-(3-phenyl-2-piperidyl) ethyl, 3-(2-phenyl-3-piperidyl) propyl group, 4-(1-phenyl-4-piperidyl) butyl, 5-(4-phenyl-piperidino) amyl group, 6-(1-phenyl-2-piperidyl) hexyl, 1-(4-Trifluoromethoxyphen-l)-4-piperidino methyl, 1-(4-trifluoromethyl)-4-piperidino methyl, 1-(3-p-methoxy-phenyl)-4-piperidino methyl, 1-(2-aminomethyl phenyl)-4-piperidino methyl, 1-(4-chloro-phenyl-)-4-piperidino methyl, 1-(3,4-two (trifluoromethoxy) phenyl]-the 4-piperidino methyl, 1-(2,4,6-three (trifluoromethyl) phenyl]-the 4-piperidino methyl, 1-(3, the 4-3,5-dimethylphenyl)-the 4-piperidino methyl, 1-(2,4, the 6-trimethoxyphenyl)-the 4-piperidino methyl, 1-(3, the 4-dichlorophenyl)-the 4-piperidino methyl, 1-(2,4,6-tribromo phenyl)-the 4-piperidino methyl, (1,2,6-triphenyl-4-piperidyl) methyl, (2,4-phenylbenzene-piperidino) methyl etc.

Piperazinyl C1-C6 alkyl is (wherein on this piperazine ring, can be substituted with at least one phenyl [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed]) comprise that piperazinyl C1-C6 alkyl is (wherein on this piperazine ring, can be substituted with 1 to 3 aforesaid phenyl [wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 substituting group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed]), 1-piperazinyl methyl for example, 1-(2-piperazinyl) ethyl, 2-(1-piperazinyl) ethyl, 3-(1-piperazinyl) propyl group, 2-(1-piperazinyl) propyl group, 4-(2-piperazinyl) butyl, 5-(2-piperazinyl) amyl group, 4-(1-piperazinyl) amyl group, 6-(1-piperazinyl) hexyl, 2-methyl-3-(1-piperazinyl) propyl group, 1,1-dimethyl-2-(1-piperazinyl) ethyl, (4-phenyl-peiperazinyl) methyl, (2,4-phenylbenzene-1-piperazinyl) methyl, (2,4,5-triphenyl-1-piperazinyl) methyl, (4-(4-Trifluoromethoxyphen-l)-1-piperazinyl] methyl, (4-(4-trifluoromethyl)-1-piperazinyl] methyl, (4-(4-chloro-phenyl-)-1-piperazinyl] methyl, (4-(2, the 4-dichlorophenyl)-and the 1-piperazinyl] methyl, (4-(2,4, the 6-trifluorophenyl)-and the 1-piperazinyl] methyl, (2,4-two (trifluoromethyl) phenyl-peiperazinyl] methyl, (2,4,6-three (trifluoromethoxy) phenyl-peiperazinyl] methyl etc.

Piperidyl C1-C6 alkyl is (wherein on this piperidine ring, can be substituted with at least one phenoxy group [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed]) comprise that piperidyl C1-C6 alkyl is (wherein on this piperidine ring, can be substituted with 1 to 3 aforesaid phenoxy group [wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 substituting group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed]), piperidino methyl for example, 2-(2-piperidyl) ethyl, 3-(3-piperidyl) propyl group, 4-(4-piperidyl) butyl, 5-(piperidino) amyl group, 6-(2-piperidyl) hexyl, 1-(4-Trifluoromethyl phenyl ether oxygen base)-4-piperidino methyl, 1-(4-4-trifluoromethylphenopendant)-4-piperidino methyl, 2-methyl-3-(piperidines-1-yl) propyl group, 1,1-dimethyl-2-(piperidines-1-yl) ethyl, 1-(4-chlorophenoxy)-4-piperidino methyl, 1-(3,4-two (trifluoromethoxy) phenoxy group]-the 4-piperidino methyl, 1-(2,4,6-three (trifluoromethoxy) phenoxy group]-the 4-piperidino methyl, 1-(3, the 4-dichlorophenoxy)-the 4-piperidino methyl, 1-(2,4, the 6-tribromophenoxy)-the 4-piperidino methyl, (1,2,6-triple phenoxyl-4-piperidyl) methyl, (2,4-hexichol Oxy-1-piperidyl) methyl etc.

Thiazolyl is [wherein on this thiazole ring, can be substituted with at least one group, it is selected from by phenyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed), piperazinyl C1-C6 alkyl is (wherein on this piperazine ring, can be substituted with at least one phenyl [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group]) and piperidyl C1-C6 alkyl (wherein on this piperidine ring, can be substituted with at least one phenoxy group [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group]) group formed] comprise that thiazolyl is [wherein on this thiazole ring, can be substituted with 1 or 2 substituting group, it is selected from by aforesaid phenyl (wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 substituting group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed), aforesaid piperazinyl C1-C6 alkyl is (wherein on this piperazine ring, can be substituted with 1 to 3 phenyl [wherein on this phenyl, can be substituted with 1 to 5, preferred 1 to 3 substituting group, it is selected from by halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group]) and aforesaid piperidyl C1-C6 alkyl (wherein on this piperidine ring, can be substituted with 1 to 3 phenoxy group [wherein on this phenyl, can be substituted with 1 to 5, preferred 1 to 3 substituting group, it is selected from by halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group]) group formed], (2-for example, 4-or 5-) thiazolyl, 2-(4-Trifluoromethoxyphen-l)-5-thiazolyl, 2-(4-(4-Trifluoromethoxyphen-l)-1-piperazinyl] the methyl-5-thiazole base, 2-(4-(4-Trifluoromethyl phenyl ether oxygen base)-piperidino] the methyl-5-thiazole base, 2-(2,4-two (trifluoromethoxy) phenyl)-the 5-thiazolyl, (4-(2 for 2-, 4-two (trifluoromethoxy) phenyl)-and the 1-piperazinyl) the methyl-5-thiazole base, (4-(2 for 2-, 4-two (trifluoromethoxy) phenoxy group)-and the 1-piperazinyl) the methyl-5-thiazole base, 2-(4-trifluoromethyl)-5-thiazolyl, 2-(4-(4-4-trifluoromethylphenopendant)-piperidino) methyl-5-thiazole base, 2-(4-(4-trifluoromethyl)-piperidino) methyl-5-thiazole base, 2-(2,4,6-three (trifluoromethyl) phenyl))-the 5-thiazolyl, (4-(2 for 2-, 4,6-three (trifluoromethyl) phenyl)-and the 1-piperazinyl) the methyl-5-thiazole base, (2-(2 for 2-, 4,6-three (trifluoromethyl) phenoxy group]-piperidino) methyl-t-thiazolyl, (4-(2 for 2-, 4,6-three (trifluoromethyl) phenoxy group)-and piperidino) the methyl-5-thiazole base, 2-(4-chloro-phenyl-)-5-thiazolyl, 2-(4-(4-chloro-phenyl-)-1-piperazinyl] the methyl-5-thiazole base, 2-(4-(2-chlorophenoxy)-piperidino] the methyl-5-thiazole base, 2-(2, the 4-dichlorophenyl)-the 5-thiazolyl, (4-(2 for 2-, the 4-dichlorophenyl)-and the 1-piperazinyl) the methyl-5-thiazole base, (2-(2 for 2-, the 4-dichlorophenyl)-and the 1-piperazinyl] methyl-t-thiazolyl, (4-(2 for 2-, the 4-dichlorophenoxy)-and piperidino] the methyl-5-thiazole base, 2-(2,4, the 6-trifluorophenyl)-the 5-thiazolyl, (4-(2 for 2-, 4, the 6-trifluorophenyl)-and the 1-piperazinyl] the methyl-5-thiazole base, (4-(2 for 2-, 4,6-trifluoromethoxy phenoxy base)-and piperidino] the methyl-5-thiazole base, 2-(2,4-hexichol Oxy-1-piperidyl) methyl-5-thiazole base, 5-(2,4,5-triple phenoxyl-piperidino) methyl-2-thiazolyl, 5-(2,4-phenylbenzene-1-piperazinyl) methyl-2-thiazolyl, 2-(2,4,5-triphenyl-1-piperazinyl) methyl-4-thiazolyl, 4-(piperidino)-2-(1-piperazinyl)-5-thiazolyl etc.

Benzo _ azoles oxygen base is (wherein on this benzo _ azoles ring, be substituted with at least one group, it is selected from by piperazinyl [wherein on this piperazine ring, can be substituted with 1 to 3 group, it is selected from by phenyl C1-C6 alkyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group) and phenyl C2-C6 thiazolinyl as hereinafter described (on this alkenyl part, have the straight or branched thiazolinyl that contains 2 to 6 carbon atoms, has 1 to 3 two key, comprise trans and the cis form) (wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 substituting group, it is selected from by halogen atom, the group that halogen replacement or unsubstituted C1-C6 alkyl and halogen replacement or unsubstituted C1-C6 alkoxyl group are formed) group of forming], piperidyl is (wherein on this piperidine ring, can be substituted with 1 to 3 substituting group, it is selected from by aforesaid phenyl C1-C6 alkyl [wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 substituting group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed] and amino [wherein on this amino, can be substituted with 1 or 2 substituting group, it is selected from by aforesaid C1-C6 alkyl and aforesaid phenyl (wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 substituting group, it is selected from by halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group) group formed] group formed) and phenyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, the group that halogen replacement or unsubstituted C1-C6 alkyl and halogen replacement or unsubstituted C1-C6 alkoxyl group are formed) group of forming) comprises that benzo _ azoles oxygen base is (wherein on this benzo _ azoles ring, be substituted with 1 to 3 substituting group, it is selected from by aforesaid piperazinyl [wherein on this piperazine ring, can be substituted with at least one group, it is selected from by phenyl C1-C6 alkyl (wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 substituting group, it is selected from by halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group) and phenyl C2-C6 thiazolinyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, the group that halogen replacement or unsubstituted C1-C6 alkyl and halogen replacement or unsubstituted C1-C6 alkoxyl group are formed) group of forming], piperidyl is (wherein on this piperidine ring, can be substituted with at least one group, it is selected from by phenyl C1-C6 alkyl [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group] and amino [wherein on this amino, can be substituted with at least one group, it is selected from by C1-C6 alkyl and phenyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group) group formed] group formed) and aforesaid phenyl (wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 substituting group, it is selected from by halogen atom, the group that halogen replacement or unsubstituted C1-C6 alkyl and halogen replacement or unsubstituted C1-C6 alkoxyl group are formed) group of forming), for example 2-(4-(4-trifluoro-methoxybenzyl)-1-piperazinyl]-6-benzo _ azoles oxygen base, 2-phenyl-5-benzo _ azoles oxygen base, 2-(4-chloro-phenyl-)-5-benzo _ azoles oxygen base, 2-(4-(4-trifluoromethyl benzyl)-1-piperazinyl]-6-benzo _ azoles oxygen base, 2-(4-(4-benzyl chloride base)-1-piperazinyl]-6-benzo _ azoles oxygen base, (4-(2 for 2-, 4,6-three (trifluoromethoxy) benzyl]-the 1-piperazinyl)-6-benzo _ azoles oxygen base, 2-(4-(2,4-two (trifluoromethyl) benzyl]-the 1-piperazinyl)-6-benzo _ azoles oxygen base, (4-(2 for 2-, the 4-dichloro benzyl)-the 1-piperazinyl]-6-benzo _ azoles oxygen base, (4-(2 for 2-, 4, the 6-trifluoro-benzyl)-the 1-piperazinyl]-6-benzo _ azoles oxygen base, 2-(4-benzyl-1-piperazinyl)-4-benzo _ azoles oxygen base, 2-(2,4-dibenzyl-1-piperazinyl)-7-benzo _ azoles oxygen base, 2-(2,4,6-tribenzyl-1-piperazinyl)-6-benzo _ azoles oxygen base, 2-(4-Trifluoromethoxyphen-l)-5-benzo _ azoles oxygen base, 2-(4-trifluoromethyl)-5-benzo _ azoles oxygen base, 2-(2, the 4-dibromo phenyl)-5-benzo _ azoles oxygen base, 2-(2,4, the 6-trichlorophenyl)-5-benzo _ azoles oxygen base, 2-(2,4,6-three (trifluoromethoxy) phenyl]-5-benzo _ azoles oxygen base, 2-(2,4-two (trifluoromethyl) phenyl]-5-benzo _ azoles oxygen base, 4-phenyl-5-(1-piperazinyl)-2-benzo _ azoles oxygen base, 2,4,5-triphenyl-7-benzo _ azoles oxygen base, 2-(4-(4-trifluoro-methoxybenzyl)-(1-, 2-or 3-) piperidyl]-(2-, 4-, 5-, 6-or 7-) benzo _ azoles oxygen base, 2-(4-(3-(4-trifluoromethyl)-2-propenyl]-(1-, 2-or 3-) piperazinyl)-(2-, 4-, 5-, 6-or 7-) benzo _ azoles oxygen base, 4-(N-methyl-N-(4-chloro-phenyl-) amino]-(1-, 2-or 3-) piperidyl]-(2-, 4-, 5-, 6-or 7-) benzo _ azoles oxygen base etc.

Benzoglyoxaline oxygen base is (wherein on this benzoglyoxaline ring, can be substituted with at least one group, it is selected from the alkyl by C1-C6, phenyl is [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed], piperidyl is [wherein on this piperidine ring, can be substituted with at least one phenoxy group (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, the group that halogen replacement or unsubstituted C1-C6 alkyl and halogen replacement or unsubstituted C1-C6 alkoxyl group are formed) group of forming], piperazinyl is [wherein on this piperazine ring, can be substituted with at least one phenyl C1-C6 alkyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group) group formed] and phenyl C1-C6 alkyl [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group] group formed) comprise that benzoglyoxaline oxygen base is (wherein on this benzoglyoxaline ring, can be substituted with 1 to 3 substituting group, it is selected from the alkyl by C1-C6, phenyl is [wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 substituting group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed], aforesaid piperidyl is [wherein on this piperidine ring, can be substituted with 1 to 3 phenoxy group (wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 substituting group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed)], aforesaid piperazinyl is [wherein on this piperazine ring, can be substituted with 1 to 3 phenyl C1-C6 alkyl (wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 substituting group, it is selected from by halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group)] and aforesaid phenyl C1-C6 alkyl [wherein on this benzyl ring, can be substituted with 1 to 3 substituting group, it is selected from by halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group] group formed), (1-for example, 2-, 4-, 5-, 6-or 7-) benzoglyoxaline oxygen base, 2-phenyl-5-benzoglyoxaline oxygen base, 1-methyl-5-benzoglyoxaline oxygen base, 1-methyl-2-phenyl-5-benzoglyoxaline oxygen base, 2-(4-chloro-phenyl-)-5-benzoglyoxaline oxygen base, 1-methyl-2-(4-chloro-phenyl-)-5-benzoglyoxaline oxygen base, 1,2-phenylbenzene-5-benzoglyoxaline oxygen base, 1,4-dimethyl-5-benzoglyoxaline oxygen base, 1-methyl-2,6-phenylbenzene-5-benzoglyoxaline oxygen base, 2-(4-trifluoromethyl)-5-benzoglyoxaline oxygen base, 1-methyl-2-(4-Trifluoromethoxyphen-l)-5-benzoglyoxaline oxygen base, 1,2,7-triphenyl-5-benzoglyoxaline oxygen base, 1,2,4-trimethylammonium-5-benzoglyoxaline oxygen base, 1-ethyl-2,6-phenylbenzene-5-benzoglyoxaline oxygen base, 2-(2,4-two (trifluoromethyl) phenyl]-5-benzoglyoxaline oxygen base, 1-methyl-2-(2,4,6-three (trifluoromethoxy) phenyl]-5-benzoglyoxaline oxygen base, 2-(2, the 4-dichlorophenyl)-5-benzoglyoxaline oxygen base, 2-(2,4, the 6-trifluorophenyl)-5-benzoglyoxaline oxygen base, 2-(3-bromophenyl)-5-benzoglyoxaline oxygen base, 2-(2-iodophenyl)-5-benzoglyoxaline oxygen base, 2-(4-Trifluoromethyl phenyl ether oxygen base-(1-, 2-or 3-) piperidyl-(1-, 4-, 5-, 6-or 7-) imidazoles oxygen base, 1-benzyl-2-(4-trifluoro-methoxybenzyl-(1-, 2-or 3-) piperazinyl]-(4-, 5-, 6-or-7) imidazoles oxygen base, 1-(4-trifluoro-methoxybenzyl)-(2-, 4-, 5-, 6-or 7-) imidazoles oxygen base etc.

1,2,3, the 4-tetrahydro isoquinolyl (wherein this 1,2,3, on the 4-tetrahydroisoquinoline ring, can be substituted with at least one group, it is selected from by (m-1) amino [wherein on this amino, can be substituted with at least one group, it is selected from the alkyl by C1-C6, phenyl is (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group) and phenyl C1-C6 alkyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group) group formed] and (m-2) phenoxy group [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group] group formed) comprise 1,2,3, the 4-tetrahydro isoquinolyl (wherein this 1,2,3, on the 4-tetrahydroisoquinoline ring, can be substituted with 1 to 3 substituting group, it is selected from by as hereinafter described amino [wherein on this amino, can be substituted with 1 or 2 substituting group, it is selected from the alkyl by C1-C6, phenyl (wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 substituting group, it is selected from by halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group) and phenyl C1-C6 alkyl (wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 substituting group, it is selected from by halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group) group formed] and aforesaid phenoxy group [wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 substituting group, it is selected from by halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group] group formed), for example (1-, 2-, 3-, 4-, 5-, 6-, 7-or 8-) 1,2,3, the 4-tetrahydro isoquinolyl, 7-(N-methyl-N-(4-Trifluoromethoxyphen-l) amino]-1,2,3,4-tetrahydrochysene-2-isoquinolyl, 7-(N-methyl-N-(4-trifluoro-methoxybenzyl) amino]-1,2,3,4-tetrahydrochysene-2-isoquinolyl, 6-(4-Trifluoromethyl phenyl ether oxygen base)-1,2,3,4-tetrahydrochysene-2-isoquinolyl, 7-(N-methyl-N-(4-trifluoromethyl) amino]-1,2,3,4-tetrahydrochysene-2-isoquinolyl, 7-(N-methyl-N-(4-trifluoromethyl benzyl) amino]-1,2,3,4-tetrahydrochysene-2-isoquinolyl, 6-(4-4-trifluoromethylphenopendant)-1,2,3,4-tetrahydrochysene-2-isoquinolyl, 7-(N-methyl-N-(4-chloro-phenyl-) amino]-1,2,3,4-tetrahydrochysene-2-isoquinolyl, 7-(N-(4-chloro-phenyl-) amino]-1,2,3,4-tetrahydrochysene-2-isoquinolyl, 7-(N-methyl-N-(4-benzyl chloride base) amino]-1,2,3,4-tetrahydrochysene-2-isoquinolyl, 7-(N-(4-benzyl chloride base) amino]-1,2,3,4-tetrahydrochysene-2-isoquinolyl, 6-(4-chlorophenoxy)-1,2,3,4-tetrahydrochysene-2-isoquinolyl, 7-(N-methyl-N-(2,4-two (trifluoromethoxy) phenyl] amino)-1,2,3,4-tetrahydrochysene-2-isoquinolyl, 7-(N-methyl-N-(2,4,6-three (trifluoromethoxy) benzyl] amino)-1,2,3,4-tetrahydrochysene-2-isoquinolyl, 6-(2,4-two (trifluoromethoxy) phenoxy group]-1,2,3,4-tetrahydrochysene-2-isoquinolyl, 7-(N-methyl-N-(2,4,6-three (trifluoromethyl) phenyl] amino)-1,2,3,4-tetrahydrochysene-2-isoquinolyl, 7-(N-methyl-N-(2,4-two (trifluoromethyl) benzyl] amino)-1,2,3,4-tetrahydrochysene-2-isoquinolyl, 6-(2,4,6-three (trifluoromethyl)-phenoxy group]-1,2,3,4-tetrahydrochysene-2-isoquinolyl, 7-(N-methyl-N-(2, the 4-dibromo phenyl) amino]-1,2,3,4-tetrahydrochysene-2-isoquinolyl, 7-(N-methyl-N-(2,3-diiodo-benzyl) amino]-1,2,3,4-tetrahydrochysene-2-isoquinolyl, 6-(2,4,6-trifluoromethoxy phenoxy base)-1,2,3,4-tetrahydrochysene-2-isoquinolyl, 7-amino-6-phenoxy group-1,2,3,4-tetrahydrochysene-2-isoquinolyl, 4,5,6-triple phenoxyl-1,2,3,4-tetrahydrochysene-7-isoquinolyl etc.

The C1-C6 alkoxyl group that is replaced by 2 phenyl is [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed] comprise that the C1-C6 alkoxyl group that is replaced by 2 phenyl is (wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 substituting group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed), for example 1,1-phenylbenzene methoxy base, 1,2-phenylbenzene oxyethyl group, 3,3-phenylbenzene propoxy-, 3,4-phenylbenzene butoxy, 3,5-phenylbenzene pentyloxy, 4,6-phenylbenzene hexyloxy, 1,1-two (4-Trifluoromethoxyphen-l) methoxyl group, 1-(2-fluorophenyl)-1-(3-fluorophenyl) methoxyl group, 1-(4-fluorophenyl)-1-(2-chloro-phenyl-) methoxyl group, 1-(3-chloro-phenyl-)-1-(4-chloro-phenyl-) methoxyl group, 1-(2-bromophenyl)-1-(3-bromophenyl) methoxyl group, 1-(4-bromophenyl)-2-(2-iodophenyl) oxyethyl group, 3-(3-iodophenyl)-3-(4-iodophenyl) propoxy-, 1-(2, the 3-difluorophenyl)-1-(3, the 4-difluorophenyl) methoxyl group, 4-(3, the 5-difluorophenyl)-4-(2, the 4-difluorophenyl) butoxy, 5-(2, the 6-difluorophenyl)-5-(2, the 3-dichlorophenyl) pentyloxy, 6-(3, the 4-dichlorophenyl)-6-(3, the 5-dichlorophenyl) hexyloxy, 1-(2, the 4-dichlorophenyl)-1-(2, the 6-dichlorophenyl) methoxyl group, 1-(3,4, the 5-trifluorophenyl)-1-(3,4, the 5-trichlorophenyl) methoxyl group, 1-(2,3,4,5, the 6-pentafluorophenyl group)-1-(2,4, the 6-trimethylphenyl) methoxyl group, 1-(4-n-butylphenyl)-1-(2, the 4-3,5-dimethylphenyl) methoxyl group, 1-(3,5-two trifluoromethyls)-1-(4-n-butoxy phenyl) methoxyl group, 1-(2, the 4-Dimethoxyphenyl)-1-(2, the 3-Dimethoxyphenyl) methoxyl group, 1-(2,4, the 6-trimethoxyphenyl)-1-(3,5-two Trifluoromethoxyphen-ls)-methoxyl group, 1-(3-chloro-4-p-methoxy-phenyl)-1-(2-chloro-4-Trifluoromethoxyphen-l) methoxyl group, 1-(3-methyl-4-fluorophenyl)-1-(2-bromo-3-trifluoromethyl) methoxyl group, 1-(2-aminomethyl phenyl)-1-(3-aminomethyl phenyl) methoxyl group, 1-(2-pentafluoroethyl group phenyl)-1-(3-pentafluoroethyl group phenyl)-methoxyl group, 1-(2-isopropyl phenyl)-1-(2-tert-butyl-phenyl) methoxyl group, 1-(2-secondary butyl phenenyl)-1-(2-is the fluoropropyl phenyl just-seven) methoxyl group, 1-(4-amyl group phenyl)-1-(4-hexyl phenyl) methoxyl group, 1-(2-p-methoxy-phenyl)-1-(2, the 6-Dimethoxyphenyl) methoxyl group, 1-(2-five fluorine ethoxyl phenenyls)-1-(isopropyl phenyl) methoxyl group, 1-(2-tert.-butoxy phenyl)-1-(2-sec-butoxy phenyl) methoxyl group, 1-(2-is fluoro-propoxy-phenyl just-seven)-1-(4-n-pentyloxy phenyl) methoxyl group, 1,1-two (the positive hexyloxy phenyl of 4-) methoxyl group etc.

(wherein on this piperidine ring, can be substituted with at least one group, it is selected from by (n-1) phenyl and [wherein on this benzyl ring, is substituted with at least one group-NR piperidyl ²⁶R ²⁷(R ²⁶Represent hydrogen atom or C1-C6 alkyl, R ²⁷Represent phenyl [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group])], (n-2) group-W ₁NR ²⁸R ²⁹[W ₁Represent the C1-C6 alkylidene group, R ²⁸Represent hydrogen atom or C1-C6 alkyl, R ²⁹Represent phenyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed)], (n-3) the C1-C6 alkoxyl group that is replaced by 2 phenyl is [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group] and (n-4) phenyl C1-C6 alkyl [wherein on this benzyl ring, be substituted with at least one phenyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, the group that halogen replacement or unsubstituted C1-C6 alkyl and halogen replacement or unsubstituted C1-C6 alkoxyl group are formed)] group of forming) comprise that piperidyl is (wherein on this piperidine ring, can be substituted with 1 to 3 substituting group, it is selected from by (n-1) phenyl and [wherein on this benzyl ring, is substituted with 1 to 3 group-NRNR ²⁶R ²⁷(R ²⁶Represent hydrogen atom or C1-C6 alkyl, R ²⁷Represent aforesaid phenyl [wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 substituting group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group])], (n-2) group-W ₁NR ²⁸R ²⁹[W ₁Represent the C1-C6 alkylidene group, R ²⁸Represent hydrogen atom or aforesaid C1-C6 alkyl, R ²⁹Represent aforesaid phenyl (wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 substituting group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed)], (n-3) the aforesaid C1-C6 alkoxyl group that is replaced by 2 phenyl is [wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 substituting group, it is selected from by halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group] and (n-4) as hereinafter described phenyl C1-C6 alkyl [wherein on this benzyl ring, be substituted with 1 to 3 phenyl (wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 substituting group, it is selected from by halogen atom, the group that halogen replacement or unsubstituted C1-C6 alkyl and halogen replacement or unsubstituted C1-C6 alkoxyl group are formed)] group of forming), (1-for example, 2-, 3-or 4-) piperidyl, 4-(N-methyl-N-(4-Trifluoromethoxyphen-l) amino] phenyl-piperidino, 4-(N-(4-Trifluoromethoxyphen-l)-amino methyl]-piperidino, 4-(N-methyl-N-(4-Trifluoromethoxyphen-l) amino methyl]-piperidino, 4-(N-ethyl-N-(4-Trifluoromethoxyphen-l) amino methyl]-piperidino, 4-(1,1-two (4-Trifluoromethoxyphen-l)-methoxyl group]-piperidino, 4-(N-methyl-N-(4-trifluoromethyl) amino] phenyl-piperidino, 4-(N-(4-trifluoromethyl) amino methyl]-piperidino, 4-(N-methyl-N-(2,4-two (trifluoromethyl) phenyl]-amino methyl)-piperidino, 4-(N-ethyl-N-(2,4,6-three (trifluoromethoxy) phenyl] amino methyl)-piperidino, 4-(1,1-two (4-trifluoromethyl) methoxyl group-piperidino, 4-(N-methyl-N-(4-chloro-phenyl-) amino]-phenyl-piperidino, (N-(2 for 4-, the 4-dibromo phenyl)-amino methyl]-piperidino, 4-(N-methyl-N-(2,4, the 6-trifluorophenyl) amino methyl]-piperidino, 4-(N-ethyl-N-(4-chloro-phenyl-) amino methyl]-piperidino, 4-(1,1-two (4-chloro-phenyl-) methoxyl group]-piperidino, 4-(N-methyl-N-(2, the 4-dibromo phenyl) amino] phenyl-piperidino, 4-(1,1-two (2, the 4-dibromo phenyl) methoxyl group]-piperidino, 4-(N-methyl-N-(2,4, the 6-trifluorophenyl)-and amino] phenyl-piperidino, 4-(1,1-two (2,4, the 6-trifluorophenyl) methoxyl group]-piperidino, 4-(N-methyl-N-(2,4-two (trifluoromethyl) phenyl] amino) phenyl-piperidino, 4-(N-methyl-N-(2,4,6-three (trifluoromethoxy) phenyl] amino) phenyl-piperidino, (1-(2 for 4-, 4-two (trifluoromethyl) phenyl]-1-(2,4,6-three (trifluoromethoxy) phenyl] methoxyl group)-piperidino, 4-(N-(4-Trifluoromethoxyphen-l) amino methyl]-3-(N-(4-trifluoromethyl) amino methyl]-piperidino, 3,4,6-three (1,1-phenylbenzene methoxy base)-piperidino, 4-(4-phenylbenzyl)-(1-, 2-or 3-) piperidyl etc.

The C1-C6 alkyl that is replaced by 2 phenyl is [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed] comprise that the C1-C6 alkyl that is replaced by 2 phenyl is [wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 substituting group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed], for example 1, the 1-diphenyl methyl, 1, the 2-diphenyl-ethyl, 3, the 3-diphenyl propyl, 3, the 4-diphenyl-ethyl, 3,5-phenylbenzene amyl group, 4,6-phenylbenzene hexyl, 1,1-two (4-Trifluoromethoxyphen-l) methyl, 1,1-two (4-chloro-phenyl-) methyl, 1-(2-fluorophenyl)-1-(3-fluorophenyl) methyl, 1-(4-fluorophenyl)-1-(2-chloro-phenyl-) methyl, 1-(3-chloro-phenyl-)-1-(4-chloro-phenyl-) methyl, 1-(2-bromophenyl)-1-(3-bromophenyl) methyl, 1-(4-bromophenyl)-2-(2-iodophenyl) ethyl, 3-(3-iodophenyl)-3-(4-iodophenyl) propyl group, 1-(2, the 3-difluorophenyl)-1-(3, the 4-difluorophenyl) methyl, 4-(3, the 5-difluorophenyl)-4-(2, the 4-difluorophenyl) butyl, 5-(2, the 6-difluorophenyl)-5-(2, the 3-dichlorophenyl) amyl group, 6-(3, the 4-dichlorophenyl)-6-(3, the 5-dichlorophenyl) hexyl, 1-(2, the 4-dichlorophenyl)-1-(2, the 6-dichlorophenyl) methyl, 1-(3,4, the 5-trifluorophenyl)-1-(3,4, the 5-trichlorophenyl) methyl, 1-(2,3,4,5, the 6-pentafluorophenyl group)-1-(2,4, the 6-trimethylphenyl) methyl, 1-(4-n-butylphenyl)-1-(2, the 4-3,5-dimethylphenyl) methyl, 1-(3,5-two trifluoromethyls)-1-(4-n-butoxy phenyl) methyl, 1-(2, the 4-Dimethoxyphenyl)-1-(2, the 3-Dimethoxyphenyl) methyl, 1-(2,4, the 6-trimethoxyphenyl)-1-(3,5-two Trifluoromethoxyphen-ls)-methyl, 1-(3-chloro-4-p-methoxy-phenyl)-1-(2-chloro-4-Trifluoromethoxyphen-l) methyl, 1-(3-methyl-4-fluorophenyl)-1-(4-bromo-3-trifluoromethyl) methyl, 1-(2-aminomethyl phenyl)-1-(3-aminomethyl phenyl) methyl, 1-(2-pentafluoroethyl group phenyl)-1-(3-pentafluoroethyl group phenyl) methyl, 1-(2-isopropyl phenyl)-1-(2-tert-butyl-phenyl) methyl, 1-(2-secondary butyl phenenyl)-1-(2-is the fluoropropyl phenyl just-seven)-methyl, 1-(4-n-pentyl phenyl)-1-(4-n-hexyl phenyl) methyl, 1-(2-p-methoxy-phenyl)-1-(2, the 6-Dimethoxyphenyl) methyl, 1-(2-five fluoro-ethoxyl phenenyls)-1-(isopropyl phenyl) methyl, 1-(2-tert.-butoxy phenyl)-1-(2-sec-butoxy phenyl) methyl, 1-(2-is fluorine propoxy-phenyl just-seven)-1-(4-n-pentyloxy phenyl) methyl, 1,1-two (the positive hexyloxy phenyl of 4-) methyl etc.

Phenyl C2-C6 thiazolinyl is [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group] group formed by 1 or 2 phenyl and thiazolinyl, described phenyl can be by 1 to 5, preferred 1 to 3 substituting group replacement, it is selected from by the group that halogen atom, halogen C1-C6 alkyl and halogen replace or unsubstituted C1-C6 alkoxyl group is formed, and described thiazolinyl contains 2 to 6 carbon atoms and 1 to 3 two key.Phenyl C2-C6 thiazolinyl comprises trans and the cis form.This class phenyl C2-C6 thiazolinyl comprises 3-(2-fluorophenyl)-2-propenyl, 3,3-two (2-fluorophenyl)-2-propenyl, 3-(3-fluorophenyl)-2-propenyl, 3-(4-fluorophenyl)-2-propenyl, 3-(2, the 3-difluorophenyl)-the 2-propenyl, 3-(2,3,4,5, the 6-pentafluorophenyl group)-the 2-propenyl, 3-(2, the 4-difluorophenyl)-the 2-propenyl, 3-(3, the 4-difluorophenyl)-the 2-propenyl, 3-(3, the 5-difluorophenyl)-the 2-propenyl, 3-(2-chloro-phenyl-)-2-propenyl, 3-(3-chloro-phenyl-)-2-propenyl, 3-(4-chloro-phenyl-)-2-propenyl, 3-(2, the 3-dichlorophenyl)-the 2-propenyl, 3-(2, the 4-dichlorophenyl)-the 2-propenyl, 3-(3, the 4-dichlorophenyl)-the 2-propenyl, 3-(3, the 5-dichlorophenyl)-the 2-propenyl, 3-(2-bromophenyl)-2-propenyl, 3-(3-bromophenyl)-2-propenyl, 3-(4-bromophenyl)-2-propenyl, 3-(2-aminomethyl phenyl)-2-propenyl, 3-(3-aminomethyl phenyl)-2-propenyl, 3-(4-aminomethyl phenyl)-2-propenyl, 3-(2-trifluoromethyl)-2-propenyl, 3-(2-fluoro-4-bromophenyl)-2-propenyl, 3-(4-chloro-3-fluorophenyl)-2-propenyl, 3-(2,3, the 4-trichlorophenyl)-the 2-propenyl, 3-(2,4, the 6-trichlorophenyl)-the 2-propenyl, 3-(4-isopropyl phenyl)-2-propenyl, 3-(4-n-butylphenyl)-2-propenyl, 3-(2, the 4-3,5-dimethylphenyl)-the 2-propenyl, 3-(2, the 3-3,5-dimethylphenyl)-the 2-propenyl, 3-(2, the 6-3,5-dimethylphenyl)-the 2-propenyl, 3-(3, the 5-3,5-dimethylphenyl)-the 2-propenyl, 3-(2, the 5-3,5-dimethylphenyl)-the 2-propenyl, 3-(2,4, the 6-trimethylphenyl)-the 2-propenyl, 3-(3,5-two trifluoromethyls)-the 2-propenyl, 3-(4-n-butoxy phenyl)-2-propenyl, 3-(2, the 4-Dimethoxyphenyl)-the 2-propenyl, 3-(2, the 3-Dimethoxyphenyl)-the 2-propenyl, 3-(2, the 6-Dimethoxyphenyl)-the 2-propenyl, 3-(3, the 5-Dimethoxyphenyl)-the 2-propenyl, 3-(2, the 5-Dimethoxyphenyl)-the 2-propenyl, 3-(3,5-two Trifluoromethoxyphen-ls)-the 2-propenyl, 3-(3-chloro-4-p-methoxy-phenyl-2-propenyl, 3-(2-chloro-4-Trifluoromethoxyphen-l-2-propenyl, 3-(3-methyl-4-fluorophenyl)-2-propenyl, 3-(4-bromo-3-trifluoromethyl)-2-propenyl, 3-(3-trifluoromethyl)-2-propenyl, 3-(4-trifluoromethyl)-2-propenyl, 3-(2-Trifluoromethoxyphen-l)-2-propenyl, 3-(3-Trifluoromethoxyphen-l)-2-propenyl, 3-(4-Trifluoromethoxyphen-l)-2-propenyl, 3-(2-p-methoxy-phenyl)-2-propenyl, 3-(3-p-methoxy-phenyl)-2-propenyl, 3-(4-p-methoxy-phenyl)-2-propenyl, 3-(3, the 4-Dimethoxyphenyl)-the 2-propenyl, 3-(3, the 5-Dimethoxyphenyl)-2-propenyl, 4-(4-chloro-phenyl-)-crotyl, 4-(4-chloro-phenyl-)-3-butenyl, 5-(4-chloro-phenyl-)-pentenyl, 5-(4-chloro-phenyl-)-4-pentenyl, 5-(4-chloro-phenyl-)-3-pentenyl, 6-(4-chloro-phenyl-)-5-hexenyl, 6-(4-chloro-phenyl-)-4-hexenyl, 6-(4-chloro-phenyl-)-3-hexenyl, 6-(4-chloro-phenyl-)-3-hexenyl etc.

Imidazolyl is [wherein on this imidazole ring, can be substituted with at least one phenyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed)] comprise that imidazolyl is [wherein on this imidazole ring, can be substituted with 1 to 3 phenyl (wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 substituting group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed)], (1-for example, 2-, 4-or 5-) imidazolyl, 1-phenyl-2-imidazolyl, 2-(2-fluorophenyl)-1-imidazolyl, 4-(3-fluorophenyl)-2-imidazolyl, 5-(4-fluorophenyl)-3-imidazolyl, 1-(2-chloro-phenyl-)-3-imidazolyl, 2-(3-chloro-phenyl-)-5-imidazolyl, 1-(4-chloro-phenyl-)-2-imidazolyl, 4-(2-bromophenyl)-5-imidazolyl, 5-(3-bromophenyl)-2-imidazolyl, 1-(4-bromophenyl)-3-imidazolyl, 2-(2-iodophenyl)-r-imidazolyl, 4-(3-iodophenyl)-5-imidazolyl, 5-(4-iodophenyl)-1-imidazolyl, 1-(2, the 3-difluorophenyl)-the 2-imidazolyl, 1-(3, the 4-difluorophenyl)-the 2-imidazolyl, 1-(3, the 5-difluorophenyl)-the 2-imidazolyl, 1-(2, the 4-difluorophenyl)-the 4-imidazolyl, 1-(2, the 6-difluorophenyl)-the 5-imidazolyl, 1-(2, the 3-dichlorophenyl)-the 2-imidazolyl, 1-(3, the 4-dichlorophenyl)-the 4-imidazolyl, 1-(3, the 5-dichlorophenyl)-the 5-imidazolyl, 1-(2, the 4-dichlorophenyl)-the 2-imidazolyl, 1-(2, the 6-dichlorophenyl)-the 4-imidazolyl, 1-(3,4, the 5-trifluorophenyl)-the 5-imidazolyl, 1-(3,4, the 5-trichlorophenyl)-the 2-imidazolyl, 1-(2,4, the 6-trifluorophenyl)-the 4-imidazolyl, 1-(2,4, the 6-trichlorophenyl)-the 5-imidazolyl, 1-(2-fluoro-4-bromophenyl)-2-imidazolyl, 1-(4-chloro-3-fluorophenyl)-4-imidazolyl, 1-(2,3, the 4-trichlorophenyl)-the 5-imidazolyl, 1-(2,3,4,5, the 6-pentafluorophenyl group)-the 2-imidazolyl, 1-(2,4, the 6-trimethylphenyl)-the 2-imidazolyl, 2-(4-n-butylphenyl)-4-imidazolyl, 4-(2, the 4-3,5-dimethylphenyl)-the 1-imidazolyl, 5-(2, the 3-3,5-dimethylphenyl)-the 2-imidazolyl, 1-(2, the 6-3,5-dimethylphenyl)-the 4-imidazolyl, 2-(3, the 5-3,5-dimethylphenyl)-the 5-imidazolyl, 4-(2, the 5-3,5-dimethylphenyl)-the 1-imidazolyl, 5-(3,5-di-trifluoromethyl phenyl)-the 2-imidazolyl, 1-(4-n-butoxy phenyl)-2-imidazolyl, 1-(2, the 4-Dimethoxyphenyl)-the 2-imidazolyl, 1-(2, the 3-Dimethoxyphenyl)-the 2-imidazolyl, 1-(2, the 6-Dimethoxyphenyl)-the 2-imidazolyl, 2-(3, the 5-Dimethoxyphenyl)-the 4-imidazolyl, 4-(2, the 5-Dimethoxyphenyl)-the 1-imidazolyl, 5-(2,4,6-triethoxy phenyl)-the 2-imidazolyl, 1-(3,5-two Trifluoromethoxyphen-ls)-the 2-imidazolyl, 1-(3-chloro-4-p-methoxy-phenyl)-2-imidazolyl, 1-(2-chloro-4-Trifluoromethoxyphen-l)-2-imidazolyl, 1-(4-bromo-3-trifluoromethyl)-2-imidazolyl, 1-(2-aminomethyl phenyl)-2-imidazolyl, 2-(3-aminomethyl phenyl)-4-imidazolyl, 4-(4-aminomethyl phenyl)-5-imidazolyl, 5-(2-methyl-3-chloro-phenyl-)-1-imidazolyl, 1-(3-methyl-4-chloro-phenyl-)-2-imidazolyl, 2-(2-chloro-4-aminomethyl phenyl)-4-imidazolyl, 4-(2-methyl-3-fluorophenyl)-5-imidazolyl, 5-(2-trifluoromethyl)-1-imidazolyl, 1-(3-trifluoromethyl)-2-imidazolyl, 2-(4-trifluoromethyl)-4-imidazolyl, 4-(2-pentafluoroethyl group phenyl)-5-imidazolyl, 5-(3-pentafluoroethyl group phenyl)-1-imidazolyl, 1-(4-pentafluoroethyl group phenyl)-2-imidazolyl, 2-(2-isopropyl phenyl)-4-imidazolyl, 4-(3-isopropyl phenyl)-5-imidazolyl, 5-(4-isopropyl phenyl)-1-imidazolyl, 1-(2-tert-butyl-phenyl)-2-imidazolyl, 2-(3-tert-butyl-phenyl)-4-imidazolyl, 4-(4-tert-butyl-phenyl)-5-imidazolyl, 5-(2-secondary butyl phenenyl)-1-imidazolyl, 1-(3-secondary butyl phenenyl)-2-imidazolyl, 2-(4-secondary butyl phenenyl)-4-imidazolyl, 4-(2-is the fluoropropyl phenyl just-seven)-5-imidazolyl, 5-(3-is the fluoropropyl phenyl just-seven)-1-imidazolyl, 1-(4-is the fluoropropyl phenyl just-seven)-2-imidazolyl, 2-(4-amyl group phenyl)-4-imidazolyl, 4-(4-hexyl phenyl)-5-imidazolyl, 1-(2-p-methoxy-phenyl)-2-imidazolyl, 5-(3-p-methoxy-phenyl)-1-imidazolyl, 1-(4-p-methoxy-phenyl)-2-imidazolyl, 2-(3-chloro-2-p-methoxy-phenyl)-4-imidazolyl, 4-(2-fluoro-3-p-methoxy-phenyl)-5-imidazolyl, 5-(2-fluoro-4-p-methoxy-phenyl)-1-imidazolyl, 1-(2, the 6-Dimethoxyphenyl)-the 2-imidazolyl, 1-(2,3, the 4-trifluorophenyl)-the 2-imidazolyl, 1-(2-Trifluoromethoxyphen-l)-2-imidazolyl, 2-(3-Trifluoromethoxyphen-l)-4-imidazolyl, 1-(4-Trifluoromethoxyphen-l)-2-imidazolyl, 1-(3-fluoro-2-Trifluoromethoxyphen-l)-2-imidazolyl, 1-(2-fluoro-3-Trifluoromethoxyphen-l)-2-imidazolyl, 1-(3-fluoro-4-Trifluoromethoxyphen-l)-2-imidazolyl, 1-(3-chloro-2-Trifluoromethoxyphen-l)-2-imidazolyl, 1-(2-chloro-3-Trifluoromethoxyphen-l)-2-imidazolyl, 1-(3-chloro-4-Trifluoromethoxyphen-l)-2-imidazolyl, 1-(2-five fluorine ethoxyl phenenyls)-2-imidazolyl, 1-(3-five fluorine ethoxyl phenenyls)-2-imidazolyl, 1-(4-five fluorine ethoxyl phenenyls)-2-imidazolyl, 1-(3-chloro-2-five fluorine ethoxyl phenenyls)-2-imidazolyl, 1-(2-chloro-3-five fluorine ethoxyl phenenyls)-2-imidazolyl, 1-(3-chloro-4-five fluorine ethoxyl phenenyls)-2-imidazolyl, 1-(2-isopropyl phenyl)-2-imidazolyl, 1-(3-isopropyl phenyl)-2-imidazolyl, 1-(4-isopropyl phenyl)-2-imidazolyl, 1-(2-tert.-butoxy phenyl)-2-imidazolyl, 1-(3-tert.-butoxy phenyl)-2-imidazolyl, 1-(4-tert.-butoxy phenyl)-2-imidazolyl, 1-(2-sec-butoxy phenyl)-2-imidazolyl, 1-(3-sec-butoxy phenyl)-2-imidazolyl, 1-(4-sec-butoxy phenyl)-2-imidazolyl, 1-(2-is fluorine propoxy-phenyl just-seven)-2-imidazolyl, 1-(3-is fluorine propoxy-phenyl just-seven)-2-imidazolyl, 1-(4-is fluorine propoxy-phenyl just-seven)-2-imidazolyl, 1-(4-n-pentyloxy phenyl)-2-imidazolyl, 1-(the positive hexyloxy phenyl of 4-)-2-imidazolyl, 1,4-phenylbenzene-2-imidazolyl, 1,4,5-triphenyl-2-imidazolyl etc.

Piperazinyl (piperadinyl) is (wherein on this piperazine (piperadine) ring, be substituted with at least one group, it is selected from by the C1-C6 alkyl that is replaced by 2 phenyl [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed], phenyl C1-C6 alkyl is [wherein on this benzyl ring, can be substituted with at least one phenoxy group (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed)], thiazolyl is (wherein on this thiazole ring, can be substituted with at least one phenyl), phenoxy group C1-C6 alkyl is (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by phenyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed), halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed), phenyl C2-C6 thiazolinyl is [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group] and imidazolyl [wherein on this imidazole ring, can be substituted with at least one phenyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, the group that halogen replacement or unsubstituted C1-C6 alkyl and halogen replacement or unsubstituted C1-C6 alkoxyl group are formed)] group of forming) comprise that piperazinyl is (wherein on this piperazine ring, be substituted with 1 to 3 substituting group, it is selected from by the aforesaid C1-C6 alkyl that is replaced by 2 phenyl [wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 substituting group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed], phenyl C1-C6 alkyl is [wherein on this benzyl ring, be substituted with 1 to 3 phenoxy group (wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 substituting group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed)], thiazolyl as hereinafter described is (wherein on this thiazole ring, can be substituted with 1 or 2 phenyl), phenoxy group C1-C6 alkyl as hereinafter described is (wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 substituting group, it is selected from by aforesaid phenyl (wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 substituting group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed), halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed), the phenyl C2-C6 thiazolinyl [group of forming by 1 or 2 phenyl and thiazolinyl, described phenyl is by 1 to 5, preferred 1 to 3 substituting group replaces, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed, described thiazolinyl contains 2 to 6 carbon atoms, have 1 to 3 two key] and imidazolyl [wherein on this imidazole ring, can be substituted with 1 to 3 phenyl (wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 substituting group, it is selected from by halogen atom, the group that halogen replacement or unsubstituted C1-C6 alkyl and halogen replacement or unsubstituted C1-C6 alkoxyl group are formed)] group of forming), for example 4-(1,1-two (4-chloro-phenyl-) methyl]-the 1-piperazinyl, 4-(1,1-two (4-Trifluoromethoxyphen-l) methyl)-the 1-piperazinyl, 4-(4-chlorine cinnamyl)-piperidino, 4-(4-trifluoromethoxy cinnamyl)-1-piperazinyl, 4-(1-(4-chloro-phenyl-)-2-imidazolyl]-the 1-piperazinyl, 4-(1,1-two (2, the 4-dibromo phenyl) methyl]-the 1-piperazinyl, 4-(1,1-two (4-trifluoromethyl) methyl]-the 1-piperazinyl, 4-(2,4-dichloro cinnamyl)-the 1-piperazinyl, 4-(4-trifluoromethyl cinnamyl)-1-piperazinyl, 4-(1-(2,4-two (trifluoromethoxy) phenyl]-the 2-imidazolyl)-the 1-piperazinyl, (1,1-two (2 for 4-, 4, the 6-trifluorophenyl) methyl]-the 1-piperazinyl, 4-(1,1-two (2,4-two (trifluoromethoxy) phenyl] methyl)-the 1-piperazinyl, 4-(2,4,6-three (trifluoromethoxy) cinnamyl]-the 1-piperazinyl, 4-(2,4-two (trifluoromethoxy)-cinnamyl]-the 1-piperazinyl, 4-(1-(4-trifluoromethyl)-2-imidazolyl]-the 1-piperazinyl, 4-(2,4,6-trifluoro cinnamyl)-the 1-piperazinyl, (1-(2 for 4-, the 4-dibromo phenyl)-the 2-imidazolyl]-the 1-piperazinyl, 4-(1,1-two (4-chloro-phenyl-) methyl]-3-(4-chlorine cinnamyl)-1-1-piperazinyl, 4-(4-trifluoromethoxy cinnamyl)-2-(1-(4-chloro-phenyl-)-2-imidazolyl]-the 1-piperazinyl, 4-(4-trifluoromethoxy cinnamyl)-2-(1-(4-chloro-phenyl-)-2-imidazolyl]-6-(1-imidazolyl)-1-piperazinyl, 4-(4-(4-Trifluoromethyl phenyl ether oxygen base) benzyl]-(1-, 2-or 3-) piperazinyl, 4-(4-phenyl-(2-or 5-) thiazolyl]-(1-, 2-or 3-) piperazinyl, 4-(2-(4-Trifluoromethyl phenyl ether oxygen base) ethyl]-(1-, 2-or 3-) piperazinyl, 4-(2-(4-phenyl phenoxy group) ethyl]-(1-, 2-or 3-) piperazinyl, 4-(2-(4-chlorophenoxy) ethyl]-(1-, 2-or 3-) piperazinyl, (2-(3 for 4-, the 4-dichlorophenoxy) ethyl]-(1-, 2-or 3-) piperazinyl, 4-(2-(4-4-trifluoromethylphenopendant)-ethyl]-(1-, 2-or 3-) piperazinyl, 4-(2-(4-Trifluoromethyl phenyl ether oxygen base) ethyl]-(1-, 2-or 3-) piperazinyl etc.

Phenylamino C1-C6 alkyl is [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group] comprise the group of forming by phenylamino and C1-C6 alkyl, described phenylamino can be replaced by the C1-C6 alkyl on the N-position of this phenylamino, and be unsubstituted or by 1 to 5, preferred 1 to 3 substituting group replaces, it is selected from by halogen as defined above and replaces or unsubstituted C1-C6 alkyl, the group that halogen replacement or unsubstituted C1-C6 alkoxyl group and halogen are formed, the example comprises the phenylamino methyl, N-methyl-N-phenylamino methyl, N-ethyl-N-phenylamino methyl, N-n-propyl-N-phenylamino methyl, N-normal-butyl-N-phenylamino methyl, N-n-pentyl-N-phenylamino methyl, N-n-hexyl-N-phenylamino methyl, 2-phenylamino ethyl, 3-phenylamino propyl group, 4-phenylamino butyl, 5-phenylamino amyl group, 6-phenylamino hexyl, 4-fluoroanilino methyl, 2-fluoro-4-bromobenzene amino methyl, 4-chloro-3-fluoroanilino methyl, 2,3,4-trichlorobenzene amino methyl, 3,4,5-trichlorobenzene amino methyl, 2,4,6-trichlorobenzene amino methyl, N-methyl-N-2,4,6-trichlorobenzene amino methyl, 4-isopropyl benzene amino methyl, 4-n-butylbenzene amino methyl, 4-methylbenzene amino methyl, 2-methylbenzene amino methyl, 3-methylbenzene amino methyl, 2,4-xylidino methyl, 2,3-xylidino methyl, 2,6-xylidino methyl, 3,5-xylidino methyl, 2,5-xylidino methyl, N-methyl-N-2,5-dimethoxy benzene amino methyl, 2,4,6-trimethylanilino methyl, 3,5-two trifluoromethylbenzene amino methyls, 2,3,4,5,6-penta fluoro benzene amino methyl, 4-isopropoxy benzene amino methyl, 4-n-butoxy phenylamino methyl, 4-anisole amino methyl, 2-anisole amino methyl, 3-anisole amino methyl, N-methyl-N-3-anisole amino methyl, 2,4-dimethoxy benzene amino methyl, 2,3-dimethoxy benzene amino methyl, 2,6-dimethoxy benzene amino methyl, 3,5-dimethoxy benzene amino methyl, 2,5-dimethoxy benzene amino methyl, 2,4,6-trimethoxy-benzene amino methyl, 3,5-two Trifluoromethyl phenyl ether amino methyls, 2-isopropoxy benzene amino methyl, 3-chloro-4-anisole amino methyl, 2-chloro-4-Trifluoromethyl phenyl ether amino methyl, 3-methyl-4-fluoroanilino methyl, 4-bromo-3-trifluoromethylbenzene amino methyl, 2-(4-fluoroanilino) ethyl, 3-(4-fluoroanilino) propyl group, 4-(4-fluoroanilino) butyl, 5-(4-fluoroanilino) amyl group, 6-(4-fluoroanilino) hexyl, 4-chlorobenzene amino methyl, 2-(4-chlorobenzene amino) ethyl, 3-(4-chlorobenzene amino) propyl group, 4-(4-chlorobenzene amino) butyl, 5-(4-chlorobenzene amino) amyl group, 6-(4-chlorobenzene amino) hexyl, 4-methylbenzene amino methyl, 2-(4-methylbenzene amino) ethyl, 3-(4-methylbenzene amino) propyl group, 4-(4-methylbenzene amino) butyl, 5-(4-methylbenzene amino) amyl group, 6-(4-methylbenzene amino) hexyl, 4-trifluoromethylbenzene amino methyl, 2-(4-trifluoromethyl phenylamino) ethyl, 3-(4-trifluoromethyl phenylamino) propyl group, 4-(4-trifluoromethyl phenylamino) butyl, N-methyl-N-(4-(4-trifluoromethyl phenylamino)] butyl, 5-(4-trifluoromethyl phenylamino) amyl group, 6-(4-trifluoromethyl phenylamino) hexyl, 4-Trifluoromethyl phenyl ether amino methyl, N-methyl-N-4 Trifluoromethyl phenyl ether amino methyl, 2-(4-trifluoromethoxy phenylamino) ethyl, 3-(4-trifluoromethoxy phenylamino) propyl group, 4-(4-trifluoromethoxy phenylamino) butyl, 5-(4-trifluoromethoxy phenylamino) amyl group, 6-(4-trifluoromethoxy phenylamino) hexyl, 4-anisole amino methyl, 2-(4-anisole amino) ethyl, 3-(4-anisole amino) propyl group, 4-(4-anisole amino) butyl, 5-(4-anisole amino) amyl group, 6-(4-anisole amino) hexyl etc.

Thiazolyl C1-C6 alkoxyl group is (wherein on this thiazole ring, can be substituted with at least one group, it is selected from by (p-1) phenoxy group C1-C6 alkyl [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed], (p-2) phenylamino C1-C6 alkyl is [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed], (p-3) phenyl C1-C6 alkyl is [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed], (p-4) piperazinyl C1-C6 alkyl is [wherein on this piperazine ring, can be substituted with at least one phenyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group)] and (p-5) piperidyl C1-C6 alkyl [wherein on this piperidine ring, can be substituted with at least one phenoxy group (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, the group that halogen replacement or unsubstituted C1-C6 alkyl and halogen replacement or unsubstituted C1-C6 alkoxyl group are formed)] group of forming) comprise that thiazolyl C1-C6 alkoxyl group is (wherein on this thiazole ring, can be substituted with 1 to 3 substituting group, it is selected from by as hereinafter described phenoxy group C1-C6 alkyl [wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 substituting group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed], aforesaid phenylamino C1-C6 alkyl is [wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 substituting group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed], aforesaid phenyl C1-C6 alkyl is [wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 substituting group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed], aforesaid piperazinyl C1-C6 alkyl is [wherein on this piperazine ring, can be substituted with 1 to 3 phenyl (wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 substituting group, it is selected from by halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group)] and aforesaid piperidyl C1-C6 alkyl [wherein on this piperidine ring, can be substituted with 1 to 3 phenoxy group (wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 substituting group, it is selected from by halogen atom, the group that halogen replacement or unsubstituted C1-C6 alkyl and halogen replacement or unsubstituted C1-C6 alkoxyl group are formed)] group of forming), (2-thiazolyl) methoxyl group for example, 2-(4-thiazolyl) oxyethyl group, 3-(5-thiazolyl) propoxy-, 4-(2-thiazolyl) butoxy, 5-(4-thiazolyl) pentyloxy, 6-(5-thiazolyl) hexyloxy, (4-(4-(4-chlorophenoxy)-piperidino methyl]-the 2-thiazolyl) methoxyl group, (4-(4-(4-4-trifluoromethylphenopendant)-piperidino methyl]-the 2-thiazolyl) methoxyl group, 2-methyl-3-(2-thiazolyl) propoxy-, 1,1-dimethyl-2-(2-thiazolyl) oxyethyl group, (4-(4-(4-Trifluoromethyl phenyl ether oxygen base)-piperidino methyl]-the 2-thiazolyl) methoxyl group, ((4-(2 for 4-, 4-two (trifluoromethoxy) phenoxy group]-the piperidino methyl)-the 2-thiazolyl] methoxyl group, ((4-(2 for 4-, 4,6-three (trifluoromethyl) phenoxy group]-the piperidino methyl)-the 2-thiazolyl] methoxyl group, ((4-(2 for 4-, 4-dibromo-phenoxy base)-the piperidino methyl]-the 2-thiazolyl) methoxyl group, ((4-(2 for 4-, 4,6-trifluoromethoxy phenoxy base)-the piperidino methyl]-the 2-thiazolyl) methoxyl group, ((4-(2 for 4-, 4-dibromo-phenoxy base)-the piperidino methyl]-the 2-thiazolyl) methoxyl group, (4-(4-(4-Trifluoromethoxyphen-l)-1-piperazinyl methyl]-the 2-thiazolyl) methoxyl group, (4-(4-(4-chloro-phenyl-)-1-piperazinyl methyl]-the 2-thiazolyl) methoxyl group, (4-(4-(2,4-two (trifluoromethyl) phenyl]-1-piperazinyl methyl)-the 2-thiazolyl] methoxyl group, ((4-(2,4 for 4-, 6-three (trifluoromethoxy) phenyl]-1-piperazinyl methyl)-the 2-thiazolyl] methoxyl group, ((4-(2 for 4-, the 4-dibromo phenyl)-1-piperazinyl methyl]-the 2-thiazolyl) methoxyl group, (4-(4-(2,4, the 6-trifluorophenyl)-1-piperazinyl methyl]-the 2-thiazolyl) methoxyl group, 4-(4-4-trifluoromethylphenopendant methyl)-2-thiazolyl, (4-(4-Trifluoromethyl phenyl ether Oxymethoxy)-2-thiazolyl] methoxyl group, (4-(4-chlorophenoxy methyl)-2-thiazolyl] methoxyl group, (4-(2,4-two (trifluoromethoxy) phenoxymethyl]-the 2-thiazolyl) methoxyl group, (4-(2,4,6-three (trifluoromethyl) phenoxymethyl]-the 2-thiazolyl) methoxyl group, (4-(2,4-dibromo-phenoxy ylmethyl)-2-thiazolyl] methoxyl group, (4-(2,4,6-trifluoromethoxy phenoxy ylmethyl)-and the 2-thiazolyl] methoxyl group, (4-(4-trifluoromethylbenzene amino methyl)-2-thiazolyl] methoxyl group, (4-(4-trifluoromethoxy phenylamino methoxyl group)-2-thiazolyl] methoxyl group, (4-(4-chlorobenzene amino methyl)-2-thiazolyl] methoxyl group, (4-(2,4-two (trifluoromethoxy) phenylamino methyl]-the 2-thiazolyl) methoxyl group, (4-(2,4,6-three (trifluoromethyl) phenylamino methyl]-the 2-thiazolyl) methoxyl group, (4-(2,4-dibromobenzene amino methyl]-the 2-thiazolyl] methoxyl group, (4-(2,4,6-trifluoro-benzene amino methyl)-2-thiazolyl] methoxyl group, (4-(3-(4-Trifluoromethoxyphen-l) propyl group]-the 2-thiazolyl) methoxyl group, (4-(3-(4-trifluoromethyl) propyl group]-the 2-thiazolyl) methoxyl group, (4-(3-(4-chloro-phenyl-) propyl group]-the 2-thiazolyl) methoxyl group, (4-(2,4-diiodo-benzyl)-and the 2-thiazolyl] methoxyl group, (4-(2,4,6-three bromobenzyls)-the 2-thiazolyl] methoxyl group, (4-(2,4-two (trifluoromethoxy) benzyl]-the 2-thiazolyl) methoxyl group, (4-(2,4,6-three (trifluoromethyl) benzyl]-the 2-thiazolyl) methoxyl group, (4,5-dibenzyl-2-thiazolyl) methoxyl group, (2-phenoxymethyl-4-benzyl-5-thiazolyl) methoxyl group, (2,5-diphenylamino methyl-4-thiazolyl) methoxyl group etc.

8-azabicyclic [3.2.1] octyl group is (wherein on this 8-azabicyclic [3.2.1] octane ring, can be substituted with at least one phenoxy group [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed]) comprise that 8-azabicyclic [3.2.1] octyl group is (wherein on this 8-azabicyclic [3.2.1] octane ring, can be substituted with 1 to 3 aforesaid phenoxy group [wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 substituting group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed]), 8-azabicyclic [3.2.1] octyl group for example, 3-(4-Trifluoromethyl phenyl ether oxygen base)-8-azabicyclic [3.2.1] octyl group, 3-(4-4-trifluoromethylphenopendant)-8-azabicyclic [3.2.1] octyl group, 3-(4-chlorophenoxy)-8-azabicyclic [3.2.1] octyl group, 3-(2, the 4-dichlorophenoxy)-8-azabicyclic [3.2.1] octyl group, 3-(2,4, the 6-Trichlorophenoxy)-8-azabicyclic [3.2.1] octyl group, 3-(2-bromine phenoxy group)-8-azabicyclic [3.2.1] octyl group, 3-(3-fluorophenoxy)-8-azabicyclic [3.2.1] octyl group, 3-(2,4-two (trifluoromethoxy) phenoxy group]-8-azabicyclic [3.2.1] octyl group, 3-(2,4,6-three (trifluoromethoxy) phenoxy group]-8-azabicyclic [3.2.1] octyl group, 3-(2,4-two (trifluoromethyl) phenoxy group]-8-azabicyclic [3.2.1] octyl group, 3-(2,4,6-three (trifluoromethyl) phenoxy group]-8-azabicyclic [3.2.1] octyl group, 3,6-two phenoxy groups-8-azabicyclic [3.2.1] octyl group, 3,7,6-triple phenoxyl-8-azabicyclic [3.2.1] octyl group, 3-(4-methoxyl group phenoxy group)-8-azabicyclic [3.2.1] octyl group, 3-(4-methylphenoxy)-8-azabicyclic [3.2.1] octyl group, 3-(2,4-dimethoxy phenoxy group)-8-azabicyclic [3.2.1] octyl group, 3-(2,4,6-trimethoxy phenoxy group)-8-azabicyclic [3.2.1] octyl group, 3-(2, the 4-dimethyl phenoxy)-8-azabicyclic [3.2.1] octyl group, 3-(2,4,6-trimethylammonium phenoxy group)-8-azabicyclic [3.2.1] octyl group etc.

Can have the C1-C6 alkyl and be comprised to have 1 or 2 C1-C6 alkyl by the amino C1-C6 alkyl that replaces as substituent amino-C1-C6 alkyl as substituent, amino methyl for example, the 2-amino-ethyl, the 1-amino-ethyl, the 3-aminopropyl, the amino butyl of 4-, the amino amyl group of 5-, the amino hexyl of 6-, 2-methyl-3-aminopropyl, 1,1-dimethyl-2-amino-ethyl, the ethylamino methyl, 1-(propyl group amino) ethyl, 2-(methylamino) ethyl, 3-(sec.-propyl amino) propyl group, 4-(normal-butyl amino) butyl, 5-(n-pentyl amino) amyl group, 6-(n-hexyl amino) hexyl, dimethylaminomethyl, (N-ethyl-N-propyl group amino) methyl, 2-(N-methyl-N-hexyl amino) ethyl etc.

The C1-C6 alkylidene group comprises methylene radical, ethylidene, propylidene, 2-methyl propylidene, 2,2-dimethyl propylidene, 1-methyl propylidene, methyl methylene radical, ethyl methylene radical, butylidene, pentylidene, hexylidene etc.

Phenyl C1-C6 alkoxy carbonyl is [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group] comprise the group of forming by phenyl C1-C6 alkoxyl group and carbonyl, described phenyl C1-C6 alkoxyl group can be by 1 to 5, preferred 1 to 3 substituting group replaces, it is selected from by halogen atom as defined above, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed, the example comprises benzyloxycarbonyl, 2-phenyl ethoxy carbonyl, 3-phenyl propoxycarbonyl, 2-phenyl propoxycarbonyl, 4-phenyl butoxy carbonyl, 5-phenyl pentyloxy carbonyl, 4-phenyl pentyloxy carbonyl, 6-phenyl hexyloxy carbonyl, 2-fluorine benzyloxycarbonyl, 3-fluorine benzyloxycarbonyl, 4-fluorine benzyloxycarbonyl, 2-(2-fluorophenyl) ethoxy carbonyl, 2-(3-fluorophenyl) ethoxy carbonyl, 2-(4-fluorophenyl) ethoxy carbonyl, 2-chlorine benzyloxycarbonyl, 3-chlorine benzyloxycarbonyl, 4-chlorine benzyloxycarbonyl, 2-fluoro-4-bromo-benzyloxy-carbonyl, 4-chloro-3-fluorine benzyloxycarbonyl, 2,3,4-trichlorine benzyloxycarbonyl, 3,4,5-trifluoromethyl benzyl oxy base carbonyl, 2,3,4,5,6-five fluorine benzyloxycarbonyl, 2,4,6-trichlorine benzyloxycarbonyl, 4-isopropyl benzyloxy carbonyl, 4-normal-butyl benzyloxycarbonyl, 4-methyl benzyloxycarbonyl, 2-methyl benzyloxycarbonyl, 3-methyl benzyloxycarbonyl, 2,4-benzyloxy-dimethyl carbonyl, 2,3-benzyloxy-dimethyl carbonyl, 2,6-benzyloxy-dimethyl carbonyl, 3,5-benzyloxy-dimethyl carbonyl, 2,5-benzyloxy-dimethyl carbonyl, 2,4,6-trimethylammonium benzyloxycarbonyl, 3,5-two trifluoromethyl benzyloxy carbonyls, 4-isopropoxy benzyloxycarbonyl, 4-n-butoxy benzyloxycarbonyl, 4-methoxyl group benzyloxy base carbonyl, 2-methoxyl group benzyloxy base carbonyl, 3-methoxyl group benzyloxy base carbonyl, 2,4-dimethoxy benzyloxycarbonyl, 2,3-dimethoxy benzyloxycarbonyl, 2,6-dimethoxy benzyloxycarbonyl, 3,5-dimethoxy benzyloxycarbonyl, 2,5-dimethoxy benzyloxycarbonyl, 2,4,6-trimethoxy benzyloxycarbonyl, 3,5-two trifluoromethoxy benzyloxycarbonyl, 2-isopropoxy benzyloxycarbonyl, 3-chloro-4-methoxyl group benzyloxy base carbonyl, 2-chloro-4-trifluoromethoxy benzyloxycarbonyl, 3-methyl-4-fluorine benzyloxycarbonyl, 4-bromo-3-trifluoromethyl benzyloxy carbonyl, 2-(2-chloro-phenyl-) ethoxy carbonyl, 2-(3-chloro-phenyl-) ethoxy carbonyl, 2-(4-chloro-phenyl-) ethoxy carbonyl, 2-trifluoromethyl benzyloxy carbonyl, 3-trifluoromethyl benzyloxy carbonyl, 4-trifluoromethyl benzyloxy carbonyl, 2-trifluoromethoxy benzyloxycarbonyl, 3-trifluoromethoxy benzyloxycarbonyl, 4-trifluoromethoxy benzyloxycarbonyl, 2-(2-trifluoromethyl) ethoxy carbonyl, 2-(3-trifluoromethyl) ethoxy carbonyl, 2-(4-trifluoromethyl) ethoxy carbonyl, 2-(2-Trifluoromethoxyphen-l) ethoxy carbonyl, 2-(3-Trifluoromethoxyphen-l) ethoxy carbonyl, 2-(4-Trifluoromethoxyphen-l) ethoxy carbonyl, 3-(2-trifluoromethyl) propoxycarbonyl, 3-(3-trifluoromethyl) propoxycarbonyl, 3-(4-trifluoromethyl) propoxycarbonyl, 3-(2-trifluoromethyl) propoxycarbonyl, 3-(3-Trifluoromethoxyphen-l) propoxycarbonyl, 3-(4-Trifluoromethoxyphen-l) propoxycarbonyl, 4-(3-trifluoromethyl) butoxy carbonyl, 5-(4-trifluoromethyl) pentyloxy carbonyl, 4-(4-trifluoromethyl) pentyloxy carbonyl, 4-(4-Trifluoromethoxyphen-l) pentyloxy carbonyl, 6-(3-trifluoromethyl) hexyloxy carbonyl, 6-(4-trifluoromethyl) hexyloxy carbonyl, 6-(4-Trifluoromethoxyphen-l) hexyloxy carbonyl etc.

Phenyl C2-C6 alkenyl carbonyl is [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group] comprise the group of forming by phenyl and alkenyl carbonyl, described phenyl can be by 1 to 5, preferred 1 to 3 substituting group replacement, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group, described alkenyl carbonyl contains 2 to 6 carbon atoms, has 1 to 3 two key.Phenyl C2-C6 alkenyl carbonyl comprises trans and the cis form.This class phenyl C2-C6 alkenyl carbonyl comprises 2-phenyl vinyl carbonyl; 3-phenyl-2-propenyl carbonyl (common name: cinnamoyl); 4-phenyl-crotyl carbonyl; 4-phenyl-3-butenyl carbonyl; 4-phenyl-1; 3-butadienyl carbonyl; 5-phenyl-1; 3; 5-hexatriene base carbonyl; 3-(2-fluorophenyl)-2-propenyl carbonyl; 3-(3-fluorophenyl)-2-propenyl carbonyl; 3-(4-fluorophenyl)-2-propenyl carbonyl; 3-(2; the 3-difluorophenyl)-2-propenyl carbonyl; 3-(2; 3; 4; 5; the 6-pentafluorophenyl group)-2-propenyl carbonyl; 3-(2; the 4-difluorophenyl)-2-propenyl carbonyl; 3-(3; the 4-difluorophenyl)-2-propenyl carbonyl; 3-(3; the 5-difluorophenyl)-2-propenyl carbonyl; 3-(2-chloro-phenyl-)-2-propenyl carbonyl; 3-(3-chloro-phenyl-)-2-propenyl carbonyl; 3-(4-chloro-phenyl-)-2-propenyl carbonyl; 3-(2; the 3-dichlorophenyl)-2-propenyl carbonyl; 3-(2; the 4-dichlorophenyl)-2-propenyl carbonyl; 3-(3; the 4-dichlorophenyl)-2-propenyl carbonyl; 3-(3; the 5-dichlorophenyl)-2-propenyl carbonyl; 3-(2-bromophenyl)-2-propenyl carbonyl; 3-(3-bromophenyl)-2-propenyl carbonyl; 3-(4-bromophenyl)-2-propenyl carbonyl; 3-(2-aminomethyl phenyl)-2-propenyl carbonyl; 3-(3-aminomethyl phenyl)-2-propenyl carbonyl; 3-(4-aminomethyl phenyl)-2-propenyl carbonyl; 3-(4-trifluoromethyl)-2-propenyl carbonyl; 3-(2-fluoro-4-bromophenyl)-2-propenyl carbonyl; 3-(4-chloro-3-fluorophenyl)-2-propenyl carbonyl; 3-(2; 3; the 4-trichlorophenyl)-2-propenyl carbonyl; 3-(2; 4; the 6-trichlorophenyl)-2-propenyl carbonyl; 3-(4-isopropyl phenyl)-2-propenyl carbonyl; 3-(4-n-butylphenyl)-2-propenyl carbonyl; 3-(2; the 4-3,5-dimethylphenyl)-2-propenyl carbonyl; 3-(2; the 3-3,5-dimethylphenyl)-2-propenyl carbonyl; 3-(2; the 6-3,5-dimethylphenyl)-2-propenyl carbonyl; 3-(3; 5-3,5-dimethylphenyl-2-propenyl carbonyl; 3-(2; the 5-3,5-dimethylphenyl)-2-propenyl carbonyl; 3-(2; 4; the 6-trimethylphenyl)-2-propenyl carbonyl; 3-(3; 5-two trifluoromethyls)-2-propenyl carbonyl; 3-(4-n-butoxy phenyl)-2-propenyl carbonyl; 3-(2; the 4-Dimethoxyphenyl)-2-propenyl carbonyl; 3-(2; the 3-Dimethoxyphenyl)-2-propenyl carbonyl; 3-(2; the 6-Dimethoxyphenyl)-2-propenyl carbonyl; 3-(3; the 5-Dimethoxyphenyl)-2-propenyl carbonyl; 3-(2; the 5-Dimethoxyphenyl)-2-propenyl carbonyl; 3-(3; 5-two Trifluoromethoxyphen-ls)-2-propenyl carbonyl; 3-(3-chloro-4-p-methoxy-phenyl)-2-propenyl carbonyl; 3-(2-chloro-4-Trifluoromethoxyphen-l)-2-propenyl carbonyl; 3-(3-methyl-4-fluorophenyl)-2-propenyl carbonyl; 3-(4-bromo-3-trifluoromethyl)-2-propenyl carbonyl; 3-(3-trifluoromethyl)-2-propenyl carbonyl; 3-(4-trifluoromethyl)-2-propenyl carbonyl; 3-(2-Trifluoromethoxyphen-l)-2-propenyl carbonyl; 3-(3-Trifluoromethoxyphen-l)-2-propenyl carbonyl; 3-(4-Trifluoromethoxyphen-l)-2-propenyl carbonyl; 3-(2-p-methoxy-phenyl)-2-propenyl carbonyl; 3-(3-p-methoxy-phenyl)-2-propenyl carbonyl; 3-(4-p-methoxy-phenyl)-2-propenyl carbonyl; 3-(3; the 4-Dimethoxyphenyl)-2-propenyl carbonyl; 3-(3, the 5-Dimethoxyphenyl)-2-propenyl carbonyl; 4-(4-chloro-phenyl-)-crotyl carbonyl; 4-(4-chloro-phenyl-)-3-butenyl carbonyl; 5-(4-chloro-phenyl-)-pentenyl carbonyl; 5-(4-chloro-phenyl-)-4-pentenyl carbonyl; 5-(4-chloro-phenyl-)-3-pentenyl carbonyl; 6-(4-chloro-phenyl-)-5-hexenyl carbonyl; 6-(4-chloro-phenyl-)-4-hexenyl carbonyl; 6-(4-chloro-phenyl-)-3-hexenyl carbonyl; 6-(4-chloro-phenyl-)-3-hexenyl carbonyl etc.

The C1-C4 alkylene dioxo base comprises methylene-dioxy, ethylenedioxy, the inferior third dioxy base, Aden's dioxy base etc.

Can have the C1-C6 alkyl and be comprised to have 1 to 2 C1-C6 alkyl by the amino alkylsulfonyl that replaces as substituent amino-sulfonyl, for example amino-sulfonyl as substituent; the methylamino alkylsulfonyl; the ethylamino alkylsulfonyl; the propyl group amino-sulfonyl; the sec.-propyl amino-sulfonyl; the butyl amino-sulfonyl; tertiary butyl amino-sulfonyl; the amyl group amino-sulfonyl; the hexyl amino-sulfonyl; the dimethylamino alkylsulfonyl; the diethylamino alkylsulfonyl; the dipropyl amino-sulfonyl; the dibutylamino alkylsulfonyl; the diamyl amino-sulfonyl; the dihexyl amino-sulfonyl; N-methyl-N-ethylamino alkylsulfonyl; N-ethyl-N-propyl group amino-sulfonyl; N-methyl-N-butyl amino-sulfonyl; N-methyl-N-hexyl amino-sulfonyl etc.

Phenyl C1-C6 alkoxyl group comprises benzyloxy, 2-phenyl ethoxy, 1-phenyl ethoxy, 3-phenyl propoxy-, 2-phenyl propoxy-, 4-phenyl butoxy, 5-phenyl pentyloxy, 4-phenyl pentyloxy, 6-phenyl hexyloxy, 2-methyl-3-phenyl propoxy-, 1,1-dimethyl-2-phenyl ethoxy etc.

Pyrrolidyl is [wherein on this pyrrolidine ring, can be substituted with at least one oxo base] comprise that pyrrolidyl is (wherein on this pyrrolidine ring, can be substituted with 1 or 2 oxo base), for example pyrrolidyl, 2-oxo-pyrrolidine base, 2,5-dioxo pyrrolidyl etc.

Pyrrolidyl C1-C6 alkoxyl group comprises (1-pyrrolidyl) methoxyl group, 2-(1-pyrrolidyl)-oxyethyl group, 1-(2-pyrrolidyl) oxyethyl group, 3-(1-pyrrolidyl) propoxy-, 2-(3-pyrrolidyl) propoxy-, 4-(1-pyrrolidyl) butoxy, 5-(2-pyrrolidyl) pentyloxy, 4-(3-pyrrolidyl) pentyloxy, 6-(1-pyrrolidyl) hexyloxy, 2-methyl-3-(1-pyrrolidyl) propoxy-, 1,1-dimethyl-2-(1-pyrrolidyl) oxyethyl group etc.

Benzofuryl C1-C6 alkyl is (wherein on this cumarone ring, can be substituted with at least-individual halogen atom is as substituting group) comprise the C1-C6 alkyl that benzofuryl replaces, it can be replaced by 1 to 3 halogen atom on this cumarone ring, 2-cumarone ylmethyl for example, 1-(2-benzofuryl) ethyl, 2-(4-benzofuryl) ethyl, 3-(5-benzofuryl) propyl group, 4-(6-benzofuryl) butyl, 5-(7-benzofuryl) amyl group, 6-(2-benzofuryl) hexyl, 4-fluoro-2-cumarone ylmethyl, 5-fluoro-2-cumarone ylmethyl, 6-fluoro-2-cumarone ylmethyl, 7-fluoro-2-cumarone ylmethyl, 4-chloro-2-cumarone ylmethyl, 5-chloro-2-cumarone ylmethyl, 6-chloro-2-cumarone ylmethyl, 7-chloro-2-cumarone ylmethyl, 4-bromo-2-cumarone ylmethyl, 5-bromo-2-cumarone ylmethyl, 6-bromo-2-cumarone ylmethyl, 7-bromo-2-cumarone ylmethyl, 4-iodo-2-cumarone ylmethyl, 5-iodo-2-cumarone ylmethyl, 6-iodo-2-cumarone ylmethyl, 7-iodo-2-cumarone ylmethyl, 4-fluoro-3-cumarone ylmethyl, 5-fluoro-3-cumarone ylmethyl, 6-fluoro-3-cumarone ylmethyl, 7-fluoro-3-cumarone ylmethyl, 4-chloro-3-cumarone ylmethyl, 5-chloro-3-cumarone ylmethyl, 6-chloro-3-cumarone ylmethyl, 7-chloro-3-cumarone ylmethyl, 4-bromo-3-cumarone ylmethyl, 5-bromo-3-cumarone ylmethyl, 6-bromo-3-cumarone ylmethyl, 7-bromo-3-cumarone ylmethyl, 4-iodo-3-cumarone ylmethyl, 5-iodo-3-cumarone ylmethyl, 6-iodo-3-cumarone ylmethyl, 7-iodo-3-cumarone ylmethyl, 2-(4-fluoro-2-benzofuryl) ethyl, 2-(5-fluoro-2-benzofuryl) ethyl, 2-(6-fluoro-2-benzofuryl) ethyl, 2-(7-fluoro-2-benzofuryl) ethyl, 2-(4-chloro-2-benzofuryl) ethyl, 2-(5-chloro-2-benzofuryl) ethyl, 2-(6-chloro-2-benzofuryl) ethyl, 2-(7-chloro-2-benzofuryl) ethyl, 2-(4-fluoro-3-benzofuryl) methyl, 2-(5-fluoro-3-benzofuryl) methyl, 2-(6-fluoro-3-benzofuryl) ethyl, 2-(7-fluoro-3-benzofuryl) ethyl, 2-(4-chloro-3-benzofuryl) ethyl, 2-(5-chloro-3-benzofuryl) ethyl, 2-(6-chloro-3-benzofuryl) ethyl, 2-(7-chloro-3-benzofuryl) ethyl, 2-(4-fluoro-2-benzofuryl) ethyl, 6-(5-fluoro-2-benzofuryl) hexyl, 6-(6-fluoro-2-benzofuryl) hexyl, 6-(7-fluoro-2-benzofuryl) hexyl, 6-(4-chloro-2-benzofuryl) hexyl, 6-(5-chloro-2-benzofuryl) hexyl, 6-(6-chloro-2-benzofuryl) hexyl, 6-(7-chloro-2-benzofuryl) hexyl, 6-(4-fluoro-3-benzofuryl) methyl, 6-(5-fluoro-3-benzofuryl) hexyl, 6-(6-fluoro-3-benzofuryl) hexyl, 6-(7-fluoro-3-benzofuryl) hexyl, 6-(4-chloro-3-benzofuryl) hexyl, 6-(5-chloro-3-benzofuryl) hexyl, 6-(6-chloro-3-benzofuryl) hexyl, 6-(7-chloro-3-benzofuryl) hexyl, (2,4-two bromo-3-benzofuryls) methyl, (4,5,6-three chloro-3-benzofuryls) methyl etc.

Phenoxy group C1-C6 alkyl is (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, the group that halogen replacement or unsubstituted C1-C6 alkyl and halogen replacement or unsubstituted C1-C6 alkoxyl group are formed) group of forming by phenoxy group and C1-C6 alkyl, described phenoxy group is unsubstituted or by 1 to 5, preferred 1 to 3 substituting group replaces, substituting group is selected from as defined above, and halogen replaces or unsubstituted C1-C6 alkyl, halogen replaces or unsubstituted C1-C6 alkoxyl group and halogen, the example comprises phenoxymethyl, 2-phenoxy group ethyl, the 3-phenoxy propyl, 4-phenoxy group butyl, 5-phenoxy group amyl group, 6-phenoxy group hexyl, 4-fluoro-6-methylenedioxy phenoxy ylmethyl, 2-fluoro-4-bromobenzene oxygen ylmethyl, 2-fluoro-4-bromobenzene oxygen ylmethyl, 4-chloro-3-fluorophenoxy methyl, 2-chlorophenoxy methyl, 3-chlorophenoxy methyl, 4-chlorophenoxy methyl, 3,4-Dichlorophenoxy ylmethyl, 2,3,4-Trichlorophenoxy methyl, 3,4,5-Trichlorophenoxy methyl, 2,4,6-Trichlorophenoxy methyl, 2 (2-chlorophenoxy) ethyl, 2-(3-chlorophenoxy) ethyl, 2-(4-chlorophenoxy) ethyl, 2-(3, the 4-dichlorophenoxy) ethyl, 2 (4-fluorophenoxy) ethyl, 4-sec.-propyl phenoxymethyl, 4-normal-butyl phenoxymethyl, 4-methylenedioxy phenoxy ylmethyl, 2-methylenedioxy phenoxy ylmethyl, 3-methylenedioxy phenoxy ylmethyl, 4-n-propyl phenoxymethyl, 4-sec.-propyl phenoxymethyl, 2,4-dimethyl phenoxy methyl, 2,3-dimethyl phenoxy methyl, 2,6-dimethyl phenoxy methyl, 3,5-dimethyl phenoxy methyl, 2,5-dimethyl phenoxy methyl, 2,4,6-trimethylammonium phenoxymethyl, 2,4,6-trimethylammonium phenoxymethyl, 4-hexyl phenoxymethyl, 2-(3-methylphenoxy) ethyl, 2-(3, the 4-dimethyl phenoxy) ethyl, 3,5-two 4-trifluoromethylphenopendant methyl, 2,3,4,5,6-penta fluoro benzene oxygen ylmethyl, 4-isopropoxy phenoxymethyl, 4-n-butoxy phenoxymethyl, 4-methoxyl group phenoxymethyl, 2-methoxyl group phenoxymethyl, 3-methoxyl group phenoxymethyl, 2-(3-methoxyl group phenoxy group) ethyl, 2-(4-methoxyl group phenoxy group) ethyl, 2-(3,4-dimethoxy phenoxy group) ethyl, 2,4-dimethoxy phenoxymethyl, 2,3-dimethoxy phenoxymethyl, 3,4-dimethoxy phenoxymethyl, 2,6-dimethoxy phenoxymethyl, 3,5-dimethoxy phenoxymethyl, 2,5-dimethoxy phenoxymethyl, 2,4,6-trimethoxy phenoxymethyl, 3,4,5-trimethoxy phenoxymethyl, 3,5-two Trifluoromethyl phenyl ether oxygen ylmethyls, 2-isopropoxy phenoxymethyl, 3-chloro-4-methoxyl group phenoxymethyl, 2-chloro-4-methoxyl group phenoxymethyl, 2-chloro-4-Trifluoromethyl phenyl ether oxygen ylmethyl, 3-methyl-4-fluorophenoxy methyl, 4-bromo-3-4-trifluoromethylphenopendant methyl, 2-(4-fluorophenoxy) ethyl, 3-(4-fluorophenoxy) propyl group, 4-(4-fluorophenoxy) butyl, 5-(4-fluorophenoxy) amyl group, 6-(4-fluorophenoxy) hexyl, 4-chlorophenoxy methyl, 3-(4-chlorophenoxy) propyl group, 4-(4-chlorophenoxy) butyl, 5-(4-chlorophenoxy) amyl group, 6-(4-chlorophenoxy) hexyl, 4-methylenedioxy phenoxy ylmethyl, 2-(4-methylphenoxy) ethyl, 2-(2-sec.-propyl phenoxy group) ethyl, 2-(4-sec.-propyl phenoxy group) ethyl, 2-(4-hexyl phenoxy group) ethyl, 2-(2-fluoro-5-methylphenoxy) ethyl, 2-(2-chloro-4-methoxyl group phenoxy group) ethyl, 2-(3-fluoro-4-chlorophenoxy) ethyl, 2-(3,4,5-trimethylammonium phenoxy group) ethyl, 3-(4-methylphenoxy) propyl group, 4-(4-methylphenoxy) butyl, 5-(4-methylphenoxy) amyl group, 6-(4-methylphenoxy) hexyl, 4-4-trifluoromethylphenopendant methyl, 2-4-trifluoromethylphenopendant methyl, 3-4-trifluoromethylphenopendant methyl, 2-(4-4-trifluoromethylphenopendant) ethyl, 2-(2-4-trifluoromethylphenopendant) ethyl, 2-(3-4-trifluoromethylphenopendant) ethyl, 3-(4-4-trifluoromethylphenopendant) propyl group, 4-(4-4-trifluoromethylphenopendant) butyl, 5-(4-4-trifluoromethylphenopendant) amyl group, 6-(4-4-trifluoromethylphenopendant) hexyl, 4-Trifluoromethyl phenyl ether oxygen ylmethyl, 2-(4-Trifluoromethyl phenyl ether oxygen base) ethyl, 2-(3-Trifluoromethyl phenyl ether oxygen base) ethyl, 2-(2-Trifluoromethyl phenyl ether oxygen base) ethyl, 3-(4-Trifluoromethyl phenyl ether oxygen base) propyl group, 4-(4-Trifluoromethyl phenyl ether oxygen base) butyl, 5-(4-Trifluoromethyl phenyl ether oxygen base) amyl group, 6-(4-Trifluoromethyl phenyl ether oxygen base) hexyl, 4-methoxyl group phenoxymethyl, 2-isopropoxy phenoxymethyl, 2-(4-methoxyl group phenoxy group) ethyl, 3-(4-methoxyl group phenoxy group) propyl group, 4-(4-methoxyl group phenoxy group) butyl, 5-(4-methoxyl group phenoxy group) amyl group, 6-(4-methoxyl group phenoxy group) hexyl etc.

Thiazolyl C1-C6 alkyl is (wherein on this thiazole ring, can be substituted with at least one phenyl [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed]) comprise that thiazolyl C1-C6 alkyl is (wherein on this thiazole ring, can be substituted with 1 or 2 phenyl [wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 substituting group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed]), 2-thiazolyl methyl for example, 4-thiazolyl methyl, 5-thiazolyl methyl, 5-phenyl-4-thiazolyl methyl, 4-phenyl-5-thiazolyl methyl, 2-phenyl-4-thiazolyl methyl, 2-phenyl-5-thiazolyl methyl, 2,5-phenylbenzene-4-thiazolyl methyl, 2,4-phenylbenzene-5-thiazolyl methyl, 5-(2-fluorophenyl)-4-thiazolyl methyl, 4-(2-fluorophenyl)-5-thiazolyl methyl, 2-(2-chloro-phenyl-)-4-thiazolyl methyl, 2-(2-bromophenyl)-5-thiazolyl methyl, 2-(2,3,4,5, the 6-pentafluorophenyl group)-4-thiazolyl methyl, 2-(2-bromophenyl)-5-thiazolyl methyl, 5-(3-iodophenyl)-4-thiazolyl methyl, 4-(3-fluorophenyl)-5-thiazolyl methyl, 2-(2, the 3-difluorophenyl)-4-thiazolyl methyl, 2-(3-bromophenyl)-5-thiazolyl methyl, 2-(3,4, the 5-trifluorophenyl)-4-thiazolyl methyl, 2-(3-fluorophenyl)-5-thiazolyl methyl, 5-(2,4, the 6-trichlorophenyl)-4-thiazolyl methyl, 4-(2,3,4,5, the 6-pentafluorophenyl group)-5-thiazolyl methyl, 2-(4-fluorophenyl)-4-thiazolyl methyl, 4-(2-fluorophenyl)-5-thiazolyl methyl, 2-(4-fluorophenyl)-5-thiazolyl methyl, 5-(2-chloro-phenyl-)-4-thiazolyl methyl, 4-(2-chloro-phenyl-)-5-thiazolyl methyl, 2-(2-chloro-phenyl-)-5-thiazolyl methyl, 5-(3-aminomethyl phenyl)-4-thiazolyl methyl, 4-(3-ethylphenyl)-5-thiazolyl methyl, 2-(3-propyl group phenyl)-4-thiazolyl methyl, 2-(2-n-butylphenyl)-5-thiazolyl methyl, 2-(3-n-pentyl phenyl)-4-thiazolyl methyl, 2-(3-n-hexyl phenyl)-5-thiazolyl methyl, 5-(3, the 4-3,5-dimethylphenyl)-4-thiazolyl methyl, 4-(2,4, the 6-trimethylphenyl)-5-thiazolyl methyl, 2-(4-p-methoxy-phenyl)-4-thiazolyl methyl, 2-(4-ethoxyl phenenyl)-5-thiazolyl methyl, 2-(4-propoxy-phenyl)-4-thiazolyl methyl, 2-(4-n-butoxy phenyl)-5-thiazolyl methyl, 2-(2-thiazolyl) ethyl, 2-(4-thiazolyl) ethyl, 2-(5-thiazolyl) ethyl, 2-(5-(2-n-pentyloxy phenyl)-4-thiazolyl] ethyl, 2-(2-(the positive hexyloxy phenyl of 2-)-5-thiazolyl] ethyl, (2-(2 for 2-, the 5-Dimethoxyphenyl)-and the 4-thiazolyl] ethyl, (2-(2 for 2-, 4, the 6-trimethoxyphenyl)-and the 5-thiazolyl] ethyl, 2-(2-trifluoromethyl)-4-thiazolyl methyl, 2,4-two (trifluoromethyl) phenyl-5-thiazolyl methyl, 2-Trifluoromethoxyphen-l-4-thiazolyl methyl, 2,3-two (trifluoromethoxy) phenyl-5-thiazolyl methyl, 2-(2-methyl-5-Trifluoromethoxyphen-l-4-thiazolyl) ethyl, 3-(2-thiazolyl) propyl group, 2-(4-thiazolyl) propyl group, 3-(5-thiazolyl) propyl group, 3-((2-methoxyl group-4-trifluoromethyl)-4-thiazolyl]] propyl group, 4-(2-thiazolyl) butyl, 4-(4-thiazolyl) butyl, 3-(5-thiazolyl) butyl, 4-(4-(2-chloro-4-aminomethyl phenyl)-2-thiazolyl] butyl, 5-(2-thiazolyl) amyl group, 5-(5-(2-fluoro-3-p-methoxy-phenyl)-2-thiazolyl] amyl group, 5-(4-thiazolyl) amyl group, 5-(5-thiazolyl) amyl group, 5-(2-thiazolyl) hexyl, 5-(4-thiazolyl) hexyl, 5-(5-thiazolyl) hexyl etc.

The group that the C1-C6 alkoxy carbonyl is made up of C1-C6 alkoxyl group and carbonyl as defined above, the example comprise methoxycarbonyl, ethoxy carbonyl, propoxycarbonyl, isopropoxy carbonyl, n-butoxy carbonyl, isobutoxy carbonyl, tert-butoxycarbonyl, sec-butoxy carbonyl, n-pentyloxy carbonyl, neopentyl oxygen carbonyl, positive hexyloxy carbonyl, different hexyloxy carbonyl, 3-methyl pentyloxy carbonyl etc.

Benzoyl is (wherein on this benzyl ring; can be substituted with at least one group; it is selected from by halogen atom; halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed) comprise that benzoyl is (wherein on this benzyl ring; can be substituted with 1 to 5; preferred 1 to 3 substituting group; it is selected from by halogen atom; halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed); benzoyl for example; the 2-fluoro benzoyl; the 3-fluoro benzoyl; the 4-fluoro benzoyl; 2; the 3-difluoro benzoyl; 3; the 4-difluoro benzoyl; the 2-chlorobenzene formacyl; the 3-chlorobenzene formacyl; the 4-chlorobenzene formacyl; 2; 3-dichloro-benzoyl base; 3; 4-dichloro-benzoyl base; 2; 4; 6-trichlorobenzene formyl radical; 4-iodobenzene formyl radical; 2; 3; 4; 5; 6-penta fluoro benzene formyl radical; the 2-benzoyl bromide; the 3-benzoyl bromide; the 4-benzoyl bromide; 2; 3-dibromobenzene formyl radical; 3; 4-dibromobenzene formyl radical; the 2-methyl benzoyl; the 3-methyl benzoyl; the 4-methyl benzoyl; 2; the 3-dimethylbenzoyl; 3; the 4-dimethylbenzoyl; 3; 4; the 5-trimethylbenzoyl; 2-trifluoromethyl benzoyl; 3-trifluoromethyl benzoyl; 4-trifluoromethyl benzoyl; 2; 3-two trifluoromethyl benzoyls; 3; 4-two trifluoromethyl benzoyls; the 2-anisoyl; the 3-anisoyl; the 4-anisoyl; 3; 4-dimethoxy benzoyl; 2; 4,6-trimethoxy benzoyl; 2-trifluoromethoxy benzoyl; 3-trifluoromethoxy benzoyl; 4-trifluoromethoxy benzoyl; 2-methoxyl group-3-fluoro benzoyl; 3-methyl-4-chlorobenzene formacyl; 3-trifluoromethoxy-4-methyl benzoyl; 2-methoxyl group-4-trifluoromethyl benzoyl etc.

The phenylamino formyl radical is (wherein on this benzyl ring; can be substituted with at least one group; it is selected from by halogen atom; the group that halogen replacement or unsubstituted C1-C6 alkyl and halogen replacement or unsubstituted C1-C6 alkoxyl group are formed) group of forming by aniline and carbonyl; described aniline can be by 1 to 5 on this benzyl ring; preferred 1 to 3 substituting group replaces; it is selected from by halogen atom; halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed; or the group of forming by N-C1-C6 alkyl benzene amine or N-phenyl C1-C6 alkyl benzene amine and carbonyl; the example comprises the phenylamino formyl radical; 2-fluorophenyl carbamyl; 3-fluorophenyl carbamyl; 4-fluorophenyl carbamyl; 2-chloro-phenyl-carbamyl; 3-chloro-phenyl-carbamyl; 4-chloro-phenyl-carbamyl; 2-bromophenyl carbamyl; 3-bromophenyl carbamyl; 4-bromophenyl carbamyl; 2-iodophenyl carbamyl; 3-iodophenyl carbamyl; 4-iodophenyl carbamyl; 2; 3-difluorophenyl carbamyl; 3; 4-difluorophenyl carbamyl; 3; 5-difluorophenyl carbamyl; 2; 4-difluorophenyl carbamyl; 2; 6-difluorophenyl carbamyl; 2; 3-dichlorophenyl carbamyl; 3; 4-dichlorophenyl carbamyl; 3; 5-dichlorophenyl carbamyl; 2; 4-dichlorophenyl carbamyl; 2; 6-dichlorophenyl carbamyl; 3; 4; 5-trifluorophenyl carbamyl; 2; 3; 4; 5; 6-pentafluorophenyl group carbamyl; 3; 4; 5-trichlorophenyl carbamyl; 2; 4,6-trifluorophenyl carbamyl; 2,4; 6-trichlorophenyl carbamyl; 2-aminomethyl phenyl carbamyl; 3-aminomethyl phenyl carbamyl; 4-aminomethyl phenyl carbamyl; 2-methyl-3-chloro-phenyl-carbamyl; 3-methyl-4-chloro-phenyl-carbamyl; 2-chloro-4-aminomethyl phenyl carbamyl; 2-methyl-3-fluorophenyl carbamyl; 2-trifluoromethyl carbamyl; 3-trifluoromethyl carbamyl; N-methyl-N-phenylamino formyl radical; N-(2-fluorophenyl)-N-methyl carbamyl; N-(3-fluorophenyl)-N-methyl carbamyl; N-(4-fluorophenyl)-N-methyl carbamyl; N-(2-chloro-phenyl-)-N-methyl carbamyl; N-(3-chloro-phenyl-)-N-methyl carbamyl; N-(4-chloro-phenyl-)-N-methyl carbamyl; N-(4-bromophenyl)-N-methyl carbamyl; N-(2-iodophenyl)-N-methyl carbamyl; N-(3-iodophenyl)-N-methyl carbamyl; N-(4-iodophenyl)-N-methyl carbamyl; N-(2; the 3-difluorophenyl)-N-methyl carbamyl; N-(3, the 4-difluorophenyl)-N-methyl carbamyl; N-(3, the 5-difluorophenyl)-N-methyl carbamyl; N-(2; the 4-difluorophenyl)-N-methyl carbamyl; N-(2; the 6-difluorophenyl)-N-methyl carbamyl; N-(2, the 3-dichlorophenyl)-N-methyl carbamyl; N-(3, the 4-dichlorophenyl)-N-methyl carbamyl; N-(3; the 5-dichlorophenyl)-N-methyl carbamyl; N-(2; the 4-dichlorophenyl)-N-methyl carbamyl; N-(2, the 6-dichlorophenyl)-N-methyl carbamyl; N-(3,4; the 5-trifluorophenyl)-N-methyl carbamyl; N-(3; 4, the 5-trichlorophenyl)-N-methyl carbamyl; N-(2,4; the 6-trifluorophenyl)-N-methyl carbamyl; N-(2; 4, the 6-trichlorophenyl)-N-methyl carbamyl; N-(2-aminomethyl phenyl)-N-methyl carbamyl; N-(3-aminomethyl phenyl)-N-methyl carbamyl; N-(4-aminomethyl phenyl)-N-methyl carbamyl; N-(2-methyl-3-chloro-phenyl-)-N-methyl carbamyl; N-(3-methyl-4-chloro-phenyl-)-N-methyl carbamyl; N-(2-chloro-4-aminomethyl phenyl)-N-methyl carbamyl; N-(2-methyl-3-fluorophenyl)-N-methyl carbamyl; N-(2-trifluoromethyl)-N-methyl carbamyl; N-(4-trifluoromethyl)-N-methyl carbamyl; N-benzyl-N-phenylamino formyl radical; N-benzyl-N-(2-fluorophenyl) carbamyl; N-benzyl-N-(3-fluorophenyl) carbamyl; N-benzyl-N-(4-fluorophenyl) carbamyl; N-benzyl-N-(2-chloro-phenyl-) carbamyl; N-benzyl-N-(3-chloro-phenyl-) carbamyl; N-benzyl-N-(4-chloro-phenyl-) carbamyl; N-benzyl-N-(2-bromophenyl) carbamyl; N-benzyl-N-(3-bromophenyl) carbamyl; N-benzyl-N-(4-bromophenyl) carbamyl; N-benzyl-N-(2-iodophenyl) carbamyl; N-benzyl-N-(3-iodophenyl) carbamyl; N-benzyl-N-(4-iodophenyl) carbamyl; N-benzyl-N-(2, the 3-difluorophenyl) carbamyl; N-benzyl-N-(3; the 4-difluorophenyl) carbamyl; N-benzyl-N-(3; the 5-difluorophenyl) carbamyl; N-benzyl-N-(2,4 difluorobenzene base) carbamyl; N-benzyl-N-(2, the 6-difluorophenyl) carbamyl; N-benzyl-N-(2; the 3-dichlorophenyl) carbamyl; N-benzyl-N-(3; the 4-dichlorophenyl) carbamyl; N-benzyl-N-(3, the 5-dichlorophenyl) carbamyl; N-benzyl-N-(2,4 dichloro benzene base) carbamyl; N-benzyl-N-(2; the 6-dichlorophenyl) carbamyl; N-benzyl-N-(3; 4, the 5-trifluorophenyl) carbamyl; N-benzyl-N-(3,4; the 5-trichlorophenyl) carbamyl; N-benzyl-N-(2; 4, the 6-trifluorophenyl) carbamyl; N-benzyl-N-(2,4; the 6-trichlorophenyl) carbamyl; N-benzyl-N-(2-aminomethyl phenyl) carbamyl; N-benzyl-N-(3-aminomethyl phenyl) carbamyl; N-benzyl-N-(4-aminomethyl phenyl) carbamyl; N-benzyl-N-(2-methyl-3-chloro-phenyl-) carbamyl; N-benzyl-N-(3-methyl-4-chloro-phenyl-) carbamyl; N-benzyl-N-(2-chloro-4-aminomethyl phenyl) carbamyl; N-benzyl-N-(2-methyl-3-fluorophenyl) carbamyl; N-benzyl-N-(2-trifluoromethyl) carbamyl; N-benzyl-N-(3-trifluoromethyl) carbamyl; N-benzyl-N-(4-trifluoromethyl) carbamyl; 2-pentafluoroethyl group phenylamino formyl radical; 3-pentafluoroethyl group phenylamino formyl radical; 4-pentafluoroethyl group phenylamino formyl radical; 2-isopropyl phenyl carbamyl; 3-isopropyl phenyl carbamyl; 4-isopropyl phenyl carbamyl; 2-tert-butyl-phenyl carbamyl; 3-tert-butyl-phenyl carbamyl; 4-tert-butyl-phenyl carbamyl; 2-secondary butyl phenenyl carbamyl; 3-secondary butyl phenenyl carbamyl; 4-secondary butyl phenenyl carbamyl; 2-is fluoropropyl phenylamino formyl radical just-seven; 3-is fluoropropyl phenylamino formyl radical just-seven; 4-is fluoropropyl phenylamino formyl radical just-seven; 4-amyl group phenyl carbamyl; 4-hexyl phenyl carbamyl; 2; 4-3,5-dimethylphenyl carbamyl; 2,4,6-trimethylphenyl carbamyl; 3; 4-Dimethoxyphenyl carbamyl; 3; 4,5-trimethoxyphenyl carbamyl; 2-p-methoxy-phenyl carbamyl; 3-p-methoxy-phenyl carbamyl; 4-p-methoxy-phenyl carbamyl; 2-methoxyl group-3-chloro-phenyl-carbamyl; 2-fluoro-3-p-methoxy-phenyl carbamyl; 2-fluoro-4-p-methoxy-phenyl carbamyl; 2,6-Dimethoxyphenyl carbamyl; 2; 3; 4-trifluorophenyl carbamyl; 3,4,5-trifluorophenyl carbamyl; 2-Trifluoromethoxyphen-l carbamyl; 3-Trifluoromethoxyphen-l carbamyl; 4-Trifluoromethoxyphen-l carbamyl; 2-five fluorine ethoxyl phenenyl carbamyls; 3-five fluorine ethoxyl phenenyl carbamyls; 4-five fluorine ethoxyl phenenyl carbamyls; 2-isopropyl phenyl carbamyl; 3-isopropyl phenyl carbamyl; 4-isopropyl phenyl carbamyl; 2-tert.-butoxy phenylamino formyl radical; 3-tert.-butoxy phenylamino formyl radical; 4-tert.-butoxy phenylamino formyl radical; 2-sec-butoxy phenylamino formyl radical; 3-sec-butoxy phenylamino formyl radical; 4-sec-butoxy phenylamino formyl radical; 2-is fluorine propoxy-phenylamino formyl radical just-seven; 3-is fluorine propoxy-phenylamino formyl radical just-seven; 4-is fluorine propoxy-phenylamino formyl radical just-seven; 4-n-pentyloxy phenylamino formyl radical; the positive hexyloxy phenylamino of 4-formyl radical etc.

Benzothiazolyl is (wherein on this benzothiazole ring, can be substituted with 1 to 3 C1-C6 alkyl) comprise that benzothiazolyl is (wherein on this benzothiazole ring, can be substituted with at least one C1-C6 alkyl), (2-for example, 4-, 5-, 6-or 7-) benzothiazolyl, 2-methyl-5-benzothiazolyl, 4-ethyl-6-benzothiazolyl, 5-propyl group-7-benzothiazolyl, the 6-tertiary butyl-2-[4-morpholinodithio base, 7-amyl group-4-benzothiazolyl, 2-hexyl-5-benzothiazolyl, 2,4-dimethyl-5-benzothiazolyl, 2,4,6-trimethylammonium-7-benzothiazolyl etc.

2,3-dihydro-1H-indenyl (wherein this 2, on 3-dihydro-1H-indenes ring, can be substituted with at least one oxo base) comprise 2,3-dihydro-1H-indenyl (wherein this 2, on 3-dihydro-1H-indenes ring, can be substituted with 1 or 2 oxo base), for example 2,3-dihydro-1H-indenyl, 1-oxo-2,3-dihydro-1H-indenyl, 1,3-dioxo-2,3-dihydro-1H-indenyl etc.

Phenyl C2-C6 thiazolinyl is (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, the group that halogen replacement or unsubstituted C1-C6 alkyl and halogen replacement or unsubstituted C1-C6 alkoxyl group are formed) group of forming by 1 or 2 phenyl and thiazolinyl, described phenyl is unsubstituted or by 1 to 5, preferred 1 to 3 substituting group replaces, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed, described thiazolinyl contains 2 to 6 carbon atoms, has 1 to 3 two key.Phenyl C2-C6 thiazolinyl comprises trans and the cis form.This class phenyl C2-C6 thiazolinyl comprises the 2-phenyl vinyl, 3-phenyl-2-propenyl (common name: cinnamyl), 3,3-phenylbenzene-2-propenyl, 3-phenyl-2-methyl-2-propenyl, 4-phenyl-crotyl, 4,4-phenylbenzene-crotyl, 4-phenyl-3-butenyl, 4-phenyl-1, the 3-butadienyl, 5-phenyl-1,3,5-hexatriene base, 5,5-phenylbenzene-3-pentenyl, 6,6-phenylbenzene-2-hexenyl, 6-phenyl-1, the 3-hexadienyl, 3-(2-fluorophenyl)-2-propenyl, 3-(3-fluorophenyl)-2-propenyl, 3-(4-fluorophenyl)-2-propenyl, 3-(2, the 3-difluorophenyl)-the 2-propenyl, 3-(2,3,4,5, the 6-pentafluorophenyl group)-the 2-propenyl, 3-(2, the 4-difluorophenyl)-the 2-propenyl, 3-(3, the 4-difluorophenyl)-the 2-propenyl, 3-(3, the 5-difluorophenyl)-the 2-propenyl, 3-(2-chloro-phenyl-)-2-propenyl, 3-(3-chloro-phenyl-)-2-propenyl, 3-(4-chloro-phenyl-)-2-propenyl, 3-(2, the 3-dichlorophenyl)-the 2-propenyl, 3-(2, the 4-dichlorophenyl)-the 2-propenyl, 3-(3, the 4-dichlorophenyl)-the 2-propenyl, 3-(3, the 5-dichlorophenyl)-the 2-propenyl, 3-(2, the 6-dichlorophenyl)-the 2-propenyl, 3-(3, the 6-dichlorophenyl)-the 2-propenyl, 3-(3,5, the 6-trichlorophenyl)-the 2-propenyl, 3-(2,4, the 5-trichlorophenyl)-the 2-propenyl, 3-(2-bromophenyl)-2-propenyl, 3-(3-bromophenyl)-2-propenyl, 3-(4-bromophenyl)-2-propenyl, 3-(2-aminomethyl phenyl)-2-propenyl, 3-(3-aminomethyl phenyl)-2-propenyl, 3-(4-aminomethyl phenyl)-2-propenyl, 3-(2-trifluoromethyl)-2-propenyl, 3-(2-fluoro-4-bromophenyl)-2-propenyl, 3-(4-chloro-3-fluorophenyl)-2-propenyl, 3-(2,3, the 4-trichlorophenyl)-the 2-propenyl, 3-(2,4, the 6-trichlorophenyl)-the 2-propenyl, 3-(4-ethylphenyl)-2-propenyl, 3-(4-n-hexyl phenyl)-2-propenyl, 3-(4-isopropyl phenyl)-2-propenyl, 3-(4-n-butylphenyl)-2-propenyl, 3-(2, the 4-3,5-dimethylphenyl)-the 2-propenyl, 3-(2, the 3-3,5-dimethylphenyl)-the 2-propenyl, 3-(2, the 6-3,5-dimethylphenyl)-the 2-propenyl, 3-(3, the 5-3,5-dimethylphenyl)-the 2-propenyl, 3-(2, the 5-3,5-dimethylphenyl)-the 2-propenyl, 3-(2,4, the 6-trimethylphenyl)-the 2-propenyl, 3-(3,5-two trifluoromethyls)-the 2-propenyl, 3-(4-n-butoxy phenyl)-2-propenyl, 3-(2, the 4-Dimethoxyphenyl)-the 2-propenyl, 3-(2, the 3-Dimethoxyphenyl)-the 2-propenyl, 3-(2, the 6-Dimethoxyphenyl)-the 2-propenyl, 3-(3, the 5-Dimethoxyphenyl)-the 2-propenyl, 3-(2, the 5-Dimethoxyphenyl)-the 2-propenyl, 3-(3,5-two Trifluoromethoxyphen-ls)-the 2-propenyl, 3-(3-chloro-4-p-methoxy-phenyl)-2-propenyl, 3-(2-chloro-4-Trifluoromethoxyphen-l)-2-propenyl, 3-(3-methyl-4-fluorophenyl)-2-propenyl, 3-(2-methyl-4-fluorophenyl)-2-propenyl, 3-(3-trifluoromethyl-4-fluorophenyl)-2-propenyl, 3-(3-trifluoromethyl-2-fluorophenyl)-2-propenyl, 3-(4-bromo-3-trifluoromethyl)-2-propenyl, 3-(4-chloro-3-trifluoromethyl)-2-propenyl, 3-(3-trifluoromethyl)-2-propenyl, 3-(2-trifluoromethyl)-2-propenyl, 3-(4-trifluoromethyl)-2-propenyl, 3-(2-Trifluoromethoxyphen-l)-2-propenyl, 3-(3-Trifluoromethoxyphen-l)-2-propenyl, 3-(4-Trifluoromethoxyphen-l)-2-propenyl, 3-(2-p-methoxy-phenyl)-2-propenyl, 3-(3-p-methoxy-phenyl)-2-propenyl, 3-(4-p-methoxy-phenyl)-2-propenyl, 3-(the positive hexyloxy phenyl of 4-)-2-propenyl, 3-(3, the 4-Dimethoxyphenyl)-the 2-propenyl, 3-(3, the 5-Dimethoxyphenyl)-2-propenyl, 4-(4-chloro-phenyl-)-crotyl, 4-(4-chloro-phenyl-)-3-butenyl, 5-(4-chloro-phenyl-)-pentenyl, 5-(4-chloro-phenyl-)-4-pentenyl, 5-(4-chloro-phenyl-)-3-pentenyl, 6-(4-chloro-phenyl-)-5-hexenyl, 6-(4-chloro-phenyl-)-4-hexenyl, 6-(4-chloro-phenyl-)-3-hexenyl, 6-(4-chloro-phenyl-)-3-hexenyl etc.

Phenyl is (wherein on this benzyl ring; can be substituted with at least one group; it is selected from the alkylene dioxo base by C1-C4; cyano group; nitro; can have the C1-C6 alkyl as substituent amino; can have the C1-C6 alkyl as the substituent alkylsulfonyl that is replaced by amino; the C1-C6 alkoxy carbonyl; the C1-C6 alkylthio; phenoxy group; phenyl C1-C6 alkoxyl group; pyrrolidyl is (wherein on this pyrrolidine ring; can be substituted with at least one oxo base); imidazolyl; different _ the azoles base; _ azoles base; phenyl C1-C6 alkyl; phenyl; can have the C1-C6 alkyl as substituent amino C1-C6 alkyl; pyrrolidyl C1-C6 alkoxyl group; halogen atom; halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group) except aforesaid phenyl (wherein on this benzyl ring; can be substituted with at least one group; it is selected from by halogen atom; halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed) in addition; comprise that also phenyl is (wherein on this benzyl ring; can be substituted with 1 to 5; preferred 1 to 3 substituting group; it is selected from by aforesaid C1-C4 alkylene dioxo base; cyano group; nitro; as hereinafter described can have 1 or 2 C1-C6 alkyl as substituent amino; aforesaid can have 1 or 2 C1-C6 alkyl as the substituent alkylsulfonyl that is replaced by amino; C1-C6 alkoxy carbonyl as hereinafter described; C1-C6 alkylthio as hereinafter described; phenoxy group; aforesaid phenyl C1-C6 alkoxyl group; aforesaid pyrrolidyl is (wherein on this pyrrolidine ring; can be substituted with at least one oxo base); imidazolyl; different _ the azoles base; _ azoles base; aforesaid phenyl C1-C6 alkyl; phenyl; as hereinafter described can have the C1-C6 alkyl as substituent amino C1-C6 alkyl; aforesaid pyrrolidyl C1-C6 alkoxyl group; halogen atom; halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed); 4-cyano-phenyl for example; the 3-cyano-phenyl; the 2-cyano-phenyl; 3; 4-dicyano phenyl; 2; 4; 6-tricyano phenyl; the 4-nitrophenyl; the 3-nitrophenyl; the 2-nitrophenyl; 3; the 4-dinitrophenyl; 2; 4; the 6-trinitrophenyl; the 4-dimethylaminophenyl; 3-methylamino phenyl; 2-N-ethyl-N-methylamino phenyl; 2; 4-two (methylamino) phenyl; 2; 4; 6-three (methylamino) phenyl; 4-dimethylamino alkylsulfonyl phenyl; 3-methylamino alkylsulfonyl phenyl; 2-N-ethyl-N-methylamino alkylsulfonyl phenyl; 2; 4-two (methylamino alkylsulfonyl) phenyl; 2; 4; 6-three (methylamino alkylsulfonyl) phenyl; 4-ethoxy carbonyl phenyl; 4-ethoxy carbonyl phenyl; 3-methoxycarbonyl phenyl; 2-propoxycarbonyl phenyl; 2; 4-di ethoxy carbonyl phenyl; 2; 4; 6-triethoxy carbonyl phenyl; 4-methylthio group phenyl; 3-ethylmercapto group phenyl; 2-methylthio group phenyl; 3; 4-diformazan sulfenyl phenyl; 2; 4; 6-three methylthio group phenyl; 3; 4-ethylenedioxy phenyl; 3; the 4-methylenedioxyphenyl; 4-diisopropylaminoethyl aminomethyl phenyl; 3-methylamino aminomethyl phenyl; 2-ethylamino aminomethyl phenyl; 2; 4-dimethylaminomethyl phenyl; 2; 4; 6-triethyl aminomethyl phenyl; the 4-Phenoxyphenyl; the 3-Phenoxyphenyl; the 2-Phenoxyphenyl; 2; 4-two Phenoxyphenyls; 3; 4; 5-triple phenoxyl phenyl; 4-benzyloxy phenyl; 3-benzyloxy phenyl; 2-benzyloxy phenyl; 2; the 4-benzyloxy phenenyl; 2; 4; 6-three benzyloxy phenyl; 4-(2-OXo-1-pyrrolidine base) phenyl; 4-(5-_ azoles base) phenyl; 4-(5-different _ azoles base) phenyl; 4-(1-imidazolyl) phenyl; the 4-benzyl phenyl; the 3-benzyl phenyl; the 2-benzyl phenyl; 3; 4-dibenzyl phenyl; 2; 4; 6-triphenyl phenyl; the 4-xenyl; the 3-xenyl; the 2-xenyl; 2; 4-phenylbenzene phenyl; 2; 4,6-triphenyl phenyl; 2-(2-imidazolyl)-4-Phenoxyphenyl; 3-(2-_ azoles base)-4-benzyloxy phenyl; 4-(3-different _ azoles base)-2-benzyl phenyl etc.

Phenyl [wherein on this benzyl ring, can be substituted with halogen] is included in can be by the phenyl of 1 to 5 halogen atom replacement, for example phenyl on this benzyl ring, the 2-fluorophenyl, the 3-fluorophenyl, the 4-fluorophenyl, the 2-chloro-phenyl-, the 3-chloro-phenyl-, the 4-chloro-phenyl-, the 2-bromophenyl, the 3-bromophenyl, the 4-bromophenyl, the 2-iodophenyl, the 3-iodophenyl, the 4-iodophenyl, 2, the 3-difluorophenyl, 3, the 4-difluorophenyl, 3, the 5-difluorophenyl, 2, the 4-difluorophenyl, 2, the 6-difluorophenyl, 2, the 3-dichlorophenyl, 3, the 4-dichlorophenyl, 3, the 5-dichlorophenyl, the 2,4 dichloro benzene base, 2, the 6-dichlorophenyl, 3,4, the 5-trifluorophenyl, 3,4, the 5-trichlorophenyl, 2,4, the 6-trifluorophenyl, 2,4, the 6-trichlorophenyl, 2-fluoro-4-bromophenyl, 4-chloro-3-fluorophenyl, 2,3, the 4-trichlorophenyl, 3,4, the 5-trifluorophenyl, 2,4,6-tribromo phenyl, 2,3,4,5,6-pentafluorophenyl group etc.

The C1-C6 alkyl that phenyl C1-C6 alkoxyl group replaces is (wherein on this benzyl ring, can be substituted with at least one group, it is selected from the alkylene dioxo base by C1-C4, halogen atom, cyano group, phenyl, phenyl C1-C6 alkoxyl group, phenyl C2-C6 thiazolinyl, phenoxy group, the C1-C6 alkylthio, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed) comprise that the C1-C6 alkyl of aforesaid phenyl C1-C6 alkoxyl group replacement is (wherein on this phenyl, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed), in addition the C1-C6 alkyl that also comprises the replacement of phenyl C1-C6 alkoxyl group is (wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 substituting group is (if substituting group is the C1-C4 alkylene dioxo base, preferred 1 or 2 substituting group), it is selected from by as above or the described straight or branched alkylene dioxo base that contains 1 to 4 carbon atom on this moieties in back, halogen atom, cyano group, phenyl, the phenyl alkoxyl group that on this alkoxyl group part, has the straight or branched alkoxyl group that contains 1 to 6 carbon atom, (this thiazolinyl contains 2 to 6 carbon atoms to the phenylene thiazolinyl, has at least 1 to 3 two key, comprise trans and the cis form), phenoxy group, the straight or branched C1-C6 alkylthio that contains 1 to 6 carbon atom, contain the halogen replacement or the unsubstituted straight or branched C1-C6 alkyl of 1 to 6 carbon atom and contain the halogen replacement of 1 to 6 carbon atom or the group that unsubstituted straight or branched C1-C6 alkoxyl group is formed), 4-cyano-phenyl methoxymethyl for example, 3-cyano-phenyl methoxymethyl, 2-cyano-phenyl methoxymethyl, 2,4-dicyanobenzenes ylmethoxy methyl, 2,4,6-tricyano phenyl methoxymethyl, 4-biphenyl methoxymethyl, 3-biphenyl methoxymethyl, 2-biphenyl methoxymethyl, 2,4-diphenyl benzene ylmethoxy methyl, 2,4,6-triphenylbenzene ylmethoxy methyl, 4-Phenoxyphenyl methoxymethyl, 3-Phenoxyphenyl methoxymethyl, 2-Phenoxyphenyl methoxymethyl, 3,4-two Phenoxyphenyl methoxymethyies, 3,4,5-triple phenoxyl phenyl methoxymethyl, 4-methylthio phenyl ylmethoxy methyl, 3-ethyl phenyl sulfide ylmethoxy methyl, 2-methylthio phenyl ylmethoxy methyl, 2,4-diformazan sulfenyl phenyl methoxymethyl, 2,4,6-three methylthio group phenyl methoxymethyies, 4-cyano group-2-phenyl methoxymethyl, 3-phenoxy group-4-methylthio phenyl ylmethoxy methyl, 3-trifluoromethyl-4-methylthio phenyl ylmethoxy methyl, 3-trifluoromethoxy-2-Phenoxyphenyl methoxymethyl, 3,4-methylenedioxyphenyl methoxymethyl, 4-benzyloxy phenyl methoxymethyl, 3,4-benzyloxy phenenyl methoxymethyl, 2,4,6-three benzyloxy phenyl methoxymethyies, 3-benzyloxy phenyl methoxymethyl, 2-benzyloxy phenyl methoxymethyl, 4-styryl phenyl methoxymethyl, 3-styryl phenyl methoxymethyl, 2-styryl phenyl methoxymethyl, 2,4-diphenylethyllene benzene ylmethoxy methyl, 2,4,6-triphenylethylene base phenyl methoxymethyl etc.

Phenyl C1-C6 alkoxyl group is (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by cyano group, phenyl, the C1-C6 alkoxy carbonyl, phenoxy group, the C1-C6 alkylthio, halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed) comprise that aforesaid phenyl C1-C6 alkoxyl group is (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed), in addition comprise also that the C1-C6 alkoxyl group that is replaced by 1 or 2 phenyl is (wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 substituting group, it is selected from by cyano group, phenyl, aforesaid C1-C6 alkoxy carbonyl, phenoxy group, aforesaid C1-C6 alkylthio, halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed), 4-cyano-phenyl methoxyl group for example, the 3-cyano benzyloxy, the 2-cyano benzyloxy, 2,4-dicyano benzyloxy, 2,3,4-tricyano benzyloxy, 4-biphenyl methoxyl group, 3-biphenyl methoxyl group, 2-biphenyl methoxyl group, 2,4-phenylbenzene benzyloxy, 2,4,6-triphenyl benzyloxy, 4-methoxycarbonyl benzyloxy, 3-ethoxy carbonyl benzyloxy, 2-methoxycarbonyl benzyloxy, 3,4-di ethoxy carbonyl benzyloxy, 3,4,5-trimethoxy carbonyl benzyloxy, 3-phenoxy group benzyloxy, 2-phenoxy group benzyloxy, 4-phenoxy group benzyloxy, 2,4-two phenoxy group benzyloxies, 2,4,6-triple phenoxyl benzyloxy, 4-methylthio group benzyloxy, 3-methylthio group benzyloxy, 2-methylthio group benzyloxy, 3,4-diformazan sulfenyl benzyloxy, 2,5,6-three methylthio group benzyloxies, 3-cyano group-4-joins benzyloxy (bibenzyloxy), 4-ethoxy carbonyl-3-phenoxy group benzyloxy, 3-methylthio group-4-ethyl benzyloxy, two (4-Trifluoromethoxyphen-l) methoxyl group, two (4-trifluoromethyl) methoxyl group, two (4-chloro-phenyl-) methoxyl group, two (3-p-methoxy-phenyl) methoxyl group, two (2-aminomethyl phenyl) methoxyl group, two (2, the 4-Dimethoxyphenyl) methoxyl group, two (3, the 4-3,5-dimethylphenyl) methoxyl group, two (2,4, the 6-trimethoxyphenyl) methoxyl group, two (3,4, the 5-trifluoromethyl) methoxyl group, two (2,4, the 6-trifluorophenyl) methoxyl group, 1-(4-Trifluoromethoxyphen-l)-1-(2,4 dichloro benzene base) methoxyl group etc.

Phenyl C2-C6 alkene oxygen base is (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group) comprise the group of forming by phenyl and thiazolinyl, described phenyl is unsubstituted or is replaced by 1 to 5, preferred 1 to 3 substituting group, be selected from group by halogen atom, halogen C1-C6 alkyl and halogen replace or unsubstituted C1-C6 alkoxyl group is formed, described thiazolinyl contains 2 to 6 carbon atoms, has at least 1 to 3 two key.Phenyl C2-C6 alkene oxygen base comprises trans and the cis form.This class phenyl C2-C6 alkene oxygen base comprises 2-phenyl vinyloxy group, 3-phenyl-2-propenyloxy group (common name: Chinese cassia tree oxygen base), 4-phenyl-2-butylene oxygen base, 4-phenyl-3-butenyloxy, 4-phenyl-1,3-divinyl oxygen base, 5-phenyl-1,3,5-hexatriene oxygen base, 3-(2-fluorophenyl)-2-propenyloxy group, 3-(3-fluorophenyl)-2-propenyloxy group, 3-(4-fluorophenyl)-2-propenyloxy group, 3-(2, the 3-difluorophenyl)-the 2-propenyloxy group, 3-(2,3,4,5, the 6-pentafluorophenyl group)-the 2-propenyloxy group, 3-(2, the 4-difluorophenyl)-the 2-propenyloxy group, 3-(3, the 4-difluorophenyl)-the 2-propenyloxy group, 3-(3, the 5-difluorophenyl)-the 2-propenyloxy group, 3-(2-chloro-phenyl-)-2-propenyloxy group, 3-(3-chloro-phenyl-)-2-propenyloxy group, 3-(4-chloro-phenyl-)-2-propenyloxy group, 3-(2, the 3-dichlorophenyl)-the 2-propenyloxy group, 3-(2, the 4-dichlorophenyl)-the 2-propenyloxy group, 3-(3, the 4-dichlorophenyl)-the 2-propenyloxy group, 3-(3, the 5-dichlorophenyl)-the 2-propenyloxy group, 3-(2-bromophenyl)-2-propenyloxy group, 3-(3-bromophenyl)-2-propenyloxy group, 3-(4-bromophenyl)-2-propenyloxy group, 3-(2-aminomethyl phenyl)-2-propenyloxy group, 3-(3-aminomethyl phenyl)-2-propenyloxy group, 3-(4-aminomethyl phenyl)-2-propenyloxy group, 3-(2-trifluoromethyl)-2-propenyloxy group, 3-(2-fluoro-4-bromophenyl)-2-propenyloxy group, 3-(4-chloro-3-fluorophenyl)-2-propenyloxy group, 3-(2,3, the 4-trichlorophenyl)-the 2-propenyloxy group, 3-(2,4, the 6-trichlorophenyl)-the 2-propenyloxy group, 3-(4-isopropyl phenyl)-2-propenyloxy group, 3-(4-n-butylphenyl)-2-propenyloxy group, 3-(2, the 4-3,5-dimethylphenyl)-the 2-propenyloxy group, 3-(2, the 3-3,5-dimethylphenyl)-the 2-propenyloxy group, 3-(2, the 6-3,5-dimethylphenyl)-the 2-propenyloxy group, 3-(3, the 5-3,5-dimethylphenyl)-the 2-propenyloxy group, 3-(2, the 5-3,5-dimethylphenyl)-the 2-propenyloxy group, 3-(2,4, the 6-trimethylphenyl)-the 2-propenyloxy group, 3-(3,5-two trifluoromethyls)-the 2-propenyloxy group, 3-(4-n-butoxy phenyl)-2-propenyloxy group, 3-(2, the 4-Dimethoxyphenyl)-the 2-propenyloxy group, 3-(2, the 3-Dimethoxyphenyl)-the 2-propenyloxy group, 3-(2, the 6-Dimethoxyphenyl)-the 2-propenyloxy group, 3-(3, the 5-Dimethoxyphenyl)-the 2-propenyloxy group, 3-(2, the 5-Dimethoxyphenyl)-the 2-propenyloxy group, 3-(3,5-two Trifluoromethoxyphen-ls)-the 2-propenyloxy group, 3-(3-chloro-4-p-methoxy-phenyl)-2-propenyloxy group, 3-(2-chloro-4-Trifluoromethoxyphen-l)-2-propenyloxy group, 3-(3-methyl-4-fluorophenyl)-2-propenyloxy group, 3-(4-bromo-3-trifluoromethyl)-2-propenyloxy group, 3-(3-trifluoromethyl)-2-propenyloxy group, 3-(4-trifluoromethyl)-2-propenyloxy group, 3-(2-Trifluoromethoxyphen-l)-2-propenyloxy group, 3-(3-Trifluoromethoxyphen-l)-2-propenyloxy group, 3-(4-Trifluoromethoxyphen-l)-2-propenyloxy group, 3-(2-p-methoxy-phenyl)-2-propenyloxy group, 3-(3-p-methoxy-phenyl)-2-propenyloxy group, 3-(4-p-methoxy-phenyl)-2-propenyloxy group, 3-(3, the 4-Dimethoxyphenyl)-the 2-propenyloxy group, 3-(3, the 5-Dimethoxyphenyl)-2-propenyloxy group, 4-(4-chloro-phenyl-)-2-butylene oxygen base, 5-(4-chloro-phenyl-)-2-amylene oxygen base, 4-(4-chloro-phenyl-)-3-butenyloxy, 5-(4-chloro-phenyl-)-4-amylene oxygen base, 5-(4-chloro-phenyl-)-3-amylene oxygen base, 6-(4-chloro-phenyl-)-5-hexene oxygen base, 6-(4-chloro-phenyl-)-4-hexene oxygen base, 6-(4-chloro-phenyl-)-3-hexene oxygen base, 6-(4-chloro-phenyl-)-3-hexene oxygen base etc.

Can have oxyhydroxide (hydroxide) group comprises beyond the aforesaid C1-C6 alkyl as substituent C1-C6 alkyl, also comprise the C1-C6 straight or branched alkyl that can have 1 to 3 hydroxide radicals, for example hydroxymethyl, 2-hydroxyethyl, 1-hydroxyethyl, 3-hydroxypropyl, 2,3-dihydroxypropyl, 4-hydroxybutyl, 3,4-dihydroxyl butyl, 1,1-dimethyl-2-hydroxyethyl, 5-hydroxyl amyl group, 6-hydroxyl hexyl, 2-methyl-3-hydroxypropyl, 2,3,4-trihydroxy-butyl etc.

The C1-C6 alkyloyl comprises that the example comprises formyl radical, ethanoyl, propionyl, butyryl radicals, pentanoyl, caproyl etc. from containing the aliphatic carboxylic acid deutero-group of 1 to 6 carbon atom.

Phenyl C1-C6 alkoxy carbonyl is [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group] group formed by phenyl C1-C6 alkoxyl group and carbonyl, described phenyl C1-C6 alkoxyl group can be by 1 to 5, preferred 1 to 3 substituting group replaces, it is selected from by halogen atom as defined above, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed, the example comprises benzyloxycarbonyl, 2-phenyl ethoxy carbonyl, 3-phenyl propoxycarbonyl, 2-phenyl propoxycarbonyl, 4-phenyl butoxy carbonyl, 5-phenyl pentyloxy carbonyl, 4-phenyl pentyloxy carbonyl, 6-phenyl hexyloxy carbonyl, 2-fluorine benzyloxycarbonyl, 3-fluorine benzyloxycarbonyl, 4-fluorine benzyloxycarbonyl, 2-(2-fluorophenyl) ethoxy carbonyl, 2-(3-fluorophenyl) ethoxy carbonyl, 2-(4-fluorophenyl) ethoxy carbonyl, 2-chlorine benzyloxycarbonyl, 3-chlorine benzyloxycarbonyl, 4-chlorine benzyloxycarbonyl, 2-fluoro-4-bromo-benzyloxy-carbonyl, 4-chloro-3-fluorine benzyloxycarbonyl, 2,3,4-trichlorine benzyloxycarbonyl, 3,4,5-trifluoromethyl benzyl oxy base carbonyl, 2,3,4,5,6-five fluorine benzyloxycarbonyl, 2,4,6-trichlorine benzyloxycarbonyl, 4-isopropyl benzyloxy carbonyl, 4-normal-butyl benzyloxycarbonyl, 4-methyl benzyloxycarbonyl, 2-methyl benzyloxycarbonyl, 3-methyl benzyloxycarbonyl, 2,4-benzyloxy-dimethyl carbonyl, 2,3-benzyloxy-dimethyl carbonyl, 2,6-benzyloxy-dimethyl carbonyl, 3,5-benzyloxy-dimethyl carbonyl, 2,5-benzyloxy-dimethyl carbonyl, 2,4,6-trimethylammonium benzyloxycarbonyl, 3,5-two trifluoromethyl benzyloxy carbonyls, 4-isopropoxy benzyloxycarbonyl, 4-n-butoxy benzyloxycarbonyl, 4-methoxyl group benzyloxy base carbonyl, 2-methoxyl group benzyloxy base carbonyl, 3-methoxyl group benzyloxy base carbonyl, 2,4-dimethoxy benzyloxycarbonyl, 2,3-dimethoxy benzyloxycarbonyl, 2,6-dimethoxy benzyloxycarbonyl, 3,5-dimethoxy benzyloxycarbonyl, 2,5-dimethoxy benzyloxycarbonyl, 2,4,6-trimethoxy benzyloxycarbonyl, 3,5-two trifluoromethoxy benzyloxycarbonyl, 2-isopropoxy benzyloxycarbonyl, 3-chloro-4-methoxyl group benzyloxy base carbonyl, 2-chloro-4-trifluoromethoxy benzyloxycarbonyl, 3-methyl-4-fluorine benzyloxycarbonyl, 4-bromo-3-trifluoromethyl benzyloxy carbonyl, 2-(2-chloro-phenyl-) ethoxy carbonyl, 2-(3-chloro-phenyl-) ethoxy carbonyl, 2-(4-chloro-phenyl-) ethoxy carbonyl, 2-trifluoromethyl benzyloxy carbonyl, 3-trifluoromethyl benzyloxy carbonyl, 4-trifluoromethyl benzyloxy carbonyl, 2-trifluoromethoxy benzyloxycarbonyl, 3-trifluoromethoxy benzyloxycarbonyl, 4-trifluoromethoxy benzyloxycarbonyl, 2-(2-trifluoromethyl) ethoxy carbonyl, 2-(3-trifluoromethyl) ethoxy carbonyl, 2-(4-trifluoromethyl) ethoxy carbonyl, 2-(2-Trifluoromethoxyphen-l) ethoxy carbonyl, 2-(3-Trifluoromethoxyphen-l) ethoxy carbonyl, 2-(4-Trifluoromethoxyphen-l) ethoxy carbonyl, 3-(2-trifluoromethyl) propoxycarbonyl, 3-(3-trifluoromethyl) propoxycarbonyl, 3-(4-trifluoromethyl) propoxycarbonyl, 3-(2-trifluoromethyl) propoxycarbonyl, 3-(3-Trifluoromethoxyphen-l) propoxycarbonyl, 3-(4-Trifluoromethoxyphen-l) propoxycarbonyl, 4-(3-trifluoromethyl) butoxy carbonyl, 5-(4-trifluoromethyl) pentyloxy carbonyl, 4-(4-Trifluoromethoxyphen-l) pentyloxy carbonyl, 6-(3-trifluoromethyl hexyloxy carbonyl, 6-(4-trifluoromethyl) hexyloxy carbonyl, 6-(4-Trifluoromethoxyphen-l) hexyloxy carbonyl etc.

Can have the group that is selected from C1-C6 alkyloyl and C1-C6 alkyl and comprise can having 1 or 2 group that is selected from C1-C6 alkyloyl and C1-C6 alkyl as substituent amino as substituent amino, for example amino; methylamino; ethylamino; n-propyl amino; sec.-propyl amino; normal-butyl amino; tertiary butyl amino; n-pentyl amino; n-hexyl amino; dimethylamino; diethylamino; two-n-propyl amino; di-n-butyl amino; two-n-pentyl amino; two-n-hexyl amino; N-methyl-N-ethylamino; N-ethyl-N-n-propyl amino; N-methyl-N-normal-butyl amino; N-methyl-N-n-hexyl amino; N-methyl-N-acetylamino; acetylamino; formyl radical amino; positive propionyl amino; positive butyryl radicals amino; isobutyryl amino; positive pentanoyl amino; positive caproyl amino; N-ethyl-N-acetylamino etc.

1,2,3, the 4-tetrahydric quinoline group (wherein this 1,2,3, on the 4-tetrahydroquinoline ring, can be substituted with at least one oxo base as substituting group) comprise 1,2,3, the 4-tetrahydric quinoline group (wherein this 1,2,3, on the 4-tetrahydroquinoline ring, can be substituted with 1 or 2 oxo base as substituting group), for example 1,2,3,4-tetrahydrochysene-1-quinolyl, 1,2,3,4-tetrahydrochysene-2-quinolyl, 1,2,3,4-tetrahydrochysene-3-quinolyl, 1,2,3,4-tetrahydrochysene-4-quinolyl, 1,2,3,4-tetrahydrochysene-5-quinolyl, 1,2,3,4-tetrahydrochysene-6-quinolyl, 1,2,3,4-tetrahydrochysene-7-quinolyl, 1,2,3,4-tetrahydrochysene-8-quinolyl, 2-oxo-1,2,3,4-tetrahydrochysene-1-quinolyl, 4-oxo-1,2,3,4-tetrahydrochysene-1-quinolyl, 2,4-dioxo-1,2,3,4-tetrahydrochysene-1-quinolyl, 2-oxo-1,2,3,4-tetrahydrochysene-6-quinolyl, 2-oxo-1,2,3,4-tetrahydrochysene-4-quinolyl, 2-oxo-1,2,3,4-tetrahydrochysene-7-quinolyl, 2-oxo-1,2,3,4-tetrahydrochysene-8-quinolyl, 2-oxo-1,2,3,4-tetrahydrochysene-5-quinolyl, 2-oxo-1,2,3,4-tetrahydrochysene-3-quinolyl etc.

The C1-C6 alkyl sulphonyl is by alkyl that contains 1 to 6 carbon atom and group that alkylsulfonyl is formed, and the example comprises methylsulfonyl, ethylsulfonyl, positive third alkylsulfonyl, positive fourth alkylsulfonyl, positive penta alkylsulfonyl, own alkylsulfonyl etc. just.

The C3-C8 cycloalkyl is ternary, quaternary, five yuan, hexa-atomic, seven yuan or the octatomic ring shape alkyl that contains 3 to 8 carbon atoms, the example comprises cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, suberyl, ring octyl group, 3,4-dimethylcyclopentyl, 3,3-Dimethylcyclohexyl etc.

The C1-C6 alkylthio is the straight or branched alkylthio that contains 1 to 6 carbon atom, and the example comprises methylthio group, ethylmercapto group, positive rosickyite base, iprotiazem base, positive butylthio, isobutyl sulfenyl, uncle's butylthio, secondary butylthio, positive penta sulfenyl, new penta sulfenyl, just own sulfenyl, dissident's sulfenyl, 3-methylpent sulfenyl etc.

Benzenesulfonyl is (wherein on this benzyl ring; can be substituted with at least one group; it is selected from by halogen atom; halogen replaces or unsubstituted C1-C6 alkyl; the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed) is unsubstituted or has 1 to 5; preferred 1 to 3 substituent benzenesulfonyl; described substituting group is selected from by halogen atom as defined above; halogen replaces or unsubstituted C1-C6 alkyl; the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed; the example comprises benzenesulfonyl; 2-fluorophenyl alkylsulfonyl; 3-fluorophenyl alkylsulfonyl; 4-fluorophenyl alkylsulfonyl; 2-chloro-phenyl-alkylsulfonyl; 3-chloro-phenyl-alkylsulfonyl; 4-chloro-phenyl-alkylsulfonyl; 2-bromophenyl alkylsulfonyl; 3-bromophenyl alkylsulfonyl; 4-bromophenyl alkylsulfonyl; 2-iodophenyl alkylsulfonyl; 3-iodophenyl alkylsulfonyl; 4-iodophenyl alkylsulfonyl; 2; 3-difluorophenyl alkylsulfonyl; 3; 4-difluorophenyl alkylsulfonyl; 3; 5-difluorophenyl alkylsulfonyl; 2; 4-difluorophenyl alkylsulfonyl; 2; 6-difluorophenyl alkylsulfonyl; 2; 3-dichlorophenyl alkylsulfonyl; 3; 4-dichlorophenyl alkylsulfonyl; 3; 5-dichlorophenyl alkylsulfonyl; 2; 4-dichlorophenyl alkylsulfonyl; 2; 6-dichlorophenyl alkylsulfonyl; 3; 4; 5-trifluorophenyl alkylsulfonyl; 3; 4; 5-trichlorophenyl alkylsulfonyl; 2; 4; 6-trifluorophenyl alkylsulfonyl; 2; 4; 6-trichlorophenyl alkylsulfonyl; 2-fluoro-4-bromophenyl alkylsulfonyl; 4-chloro-3-fluorophenyl alkylsulfonyl; 2; 3; 4-trichlorophenyl alkylsulfonyl; 3; 4; 5-trifluorophenyl alkylsulfonyl; 2; 3; 4; 5; 6-pentafluorophenyl group alkylsulfonyl; 2; 4; 6-trimethylphenyl alkylsulfonyl; 4-n-butylphenyl alkylsulfonyl; 2; 4-3,5-dimethylphenyl alkylsulfonyl; 2; 3-3,5-dimethylphenyl alkylsulfonyl; 2; 6-3,5-dimethylphenyl alkylsulfonyl; 3; 5-3,5-dimethylphenyl alkylsulfonyl; 2; 5-3,5-dimethylphenyl alkylsulfonyl; 3; 5-two trifluoromethyl alkylsulfonyls; 4-n-butoxy phenyl sulfonyl; 2; 4-Dimethoxyphenyl alkylsulfonyl; 2; 3-Dimethoxyphenyl alkylsulfonyl; 2; 6-Dimethoxyphenyl alkylsulfonyl; 3; 5-Dimethoxyphenyl alkylsulfonyl; 2; 5-Dimethoxyphenyl alkylsulfonyl; 2; 4; 6-trimethoxyphenyl alkylsulfonyl; 3; 5-two Trifluoromethoxyphen-l alkylsulfonyls; 3-chloro-4-p-methoxy-phenyl alkylsulfonyl; 2-chloro-4-Trifluoromethoxyphen-l alkylsulfonyl; 3-methyl-4-fluorophenyl alkylsulfonyl; 4-bromo-3-trifluoromethyl alkylsulfonyl; 2-aminomethyl phenyl alkylsulfonyl; 3-aminomethyl phenyl alkylsulfonyl; 4-aminomethyl phenyl alkylsulfonyl; 2-methyl-3-chloro-phenyl-alkylsulfonyl; 3-methyl-4-chloro-phenyl-alkylsulfonyl; 2-chloro-4-aminomethyl phenyl alkylsulfonyl; 2-methyl-3-fluorophenyl alkylsulfonyl; 2-trifluoromethyl alkylsulfonyl; 3-trifluoromethyl alkylsulfonyl; 4-trifluoromethyl alkylsulfonyl; 2-pentafluoroethyl group phenyl sulfonyl; 3-pentafluoroethyl group phenyl sulfonyl; 4-pentafluoroethyl group phenyl sulfonyl; 2-isopropyl phenyl alkylsulfonyl; 3-isopropyl phenyl alkylsulfonyl; 4-isopropyl phenyl alkylsulfonyl; 2-tert-butyl-phenyl alkylsulfonyl; 3-tert-butyl-phenyl alkylsulfonyl; 4-tert-butyl-phenyl alkylsulfonyl; 2-secondary butyl phenenyl alkylsulfonyl; 3-secondary butyl phenenyl alkylsulfonyl; 4-secondary butyl phenenyl alkylsulfonyl; 2-is the fluoropropyl phenyl sulfonyl just-seven; 3-is the fluoropropyl phenyl sulfonyl just-seven; 4-is the fluoropropyl phenyl sulfonyl just-seven; 4-n-pentyl phenyl alkylsulfonyl; 4-n-hexyl phenyl alkylsulfonyl; 2-p-methoxy-phenyl alkylsulfonyl; 3-p-methoxy-phenyl alkylsulfonyl; 4-p-methoxy-phenyl alkylsulfonyl; 3-chloro-2-p-methoxy-phenyl alkylsulfonyl; 2-fluoro-3-p-methoxy-phenyl alkylsulfonyl; 2-fluoro-4-p-methoxy-phenyl alkylsulfonyl; 2; 6-Dimethoxyphenyl alkylsulfonyl; 2; 3; 4-trifluorophenyl alkylsulfonyl; 2; 4,6-trifluorophenyl alkylsulfonyl; 2-Trifluoromethoxyphen-l alkylsulfonyl; 3-Trifluoromethoxyphen-l alkylsulfonyl; 4-Trifluoromethoxyphen-l alkylsulfonyl; 3-fluoro-2-Trifluoromethoxyphen-l alkylsulfonyl; 2-fluoro-3-Trifluoromethoxyphen-l alkylsulfonyl; 3-fluoro-4-Trifluoromethoxyphen-l alkylsulfonyl; 3-chloro-2-Trifluoromethoxyphen-l alkylsulfonyl; 2-chloro-3-Trifluoromethoxyphen-l alkylsulfonyl; 3-chloro-4-Trifluoromethoxyphen-l alkylsulfonyl; 2-five fluorine ethoxyl phenenyl alkylsulfonyls; 3-five fluorine ethoxyl phenenyl alkylsulfonyls; 4-five fluorine ethoxyl phenenyl alkylsulfonyls; 3-chloro-2-five fluorine ethoxyl phenenyl alkylsulfonyls; 2-chloro-3-five fluorine ethoxyl phenenyl alkylsulfonyls; 3-chloro-4-five fluorine ethoxyl phenenyl alkylsulfonyls; 2-isopropyl phenyl alkylsulfonyl; 3-isopropyl phenyl alkylsulfonyl; 4-isopropyl phenyl alkylsulfonyl; 2-tert.-butoxy phenyl sulfonyl; 3-tert.-butoxy phenyl sulfonyl; 4-tert.-butoxy phenyl sulfonyl; 2-sec-butoxy phenyl sulfonyl; 3-sec-butoxy phenyl sulfonyl; 4-sec-butoxy phenyl sulfonyl; 2-is fluorine propoxy-phenyl sulfonyl just-seven; 3-is fluorine propoxy-phenyl sulfonyl just-seven; 4-is fluorine propoxy-phenyl sulfonyl just-seven; 4-n-pentyloxy phenyl sulfonyl; the positive hexyloxy phenyl sulfonyl of 4-etc.

Can have the C1-C6 alkyl and be comprised to have 1 or 2 C1-C6 alkyl by the amino C1-C6 alkoxyl group that replaces as substituent amino-C1-C6 alkoxyl group as substituent, for example amino methoxyl group, the 2-amino ethoxy, the 1-amino ethoxy, the amino propoxy-of 3-, the amino butoxy of 4-, the amino pentyloxy of 5-, the amino hexyloxy of 6-, the amino propoxy-of 2-methyl-3-, 1,1-dimethyl-2-amino ethoxy, the ethylamino oxyethyl group, 1-(propyl group amino) oxyethyl group, 2-(methylamino) oxyethyl group, 3-(sec.-propyl amino) propoxy-, 4-(normal-butyl amino) butoxy, 5-(n-pentyl amino) pentyloxy, 6-(n-hexyl amino) hexyloxy, the dimethylamino ylmethoxy, the 3-dimethylamino propoxy, (N-ethyl-N-propyl group amino) methoxyl group, 2-(N-methyl-N-hexyl amino) oxyethyl group etc.

Phenyl is [wherein on this benzyl ring; can be substituted with at least one group as substituting group; it is selected from by halogen atom; halogen replaces or unsubstituted C1-C6 alkyl; halogen replaces or unsubstituted C1-C6 alkoxyl group; can have be selected from C1-C6 alkyloyl and C1-C6 alkyl group as substituent amino; the C1-C6 alkoxy carbonyl; phenyl; phenoxy group is (wherein on this benzyl ring; can be substituted with at least one group; it is selected from by halogen atom; halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed); amino-sulfonyl; 1; 2; 3; the 4-tetrahydric quinoline group (wherein this 1; 2; 3; on the 4-tetrahydroquinoline ring; can be substituted with at least one oxo base as substituting group); the C1-C6 alkyl sulphonyl; the C3-C8 cycloalkyl; nitro; cyano group; the C1-C6 alkylthio; benzenesulfonyl is (wherein on this benzyl ring; can be substituted with at least one group, it is selected from by halogen atom; halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed); C1-C6 alkyl and following groups that hydroxyl replaces:

(W wherein ₁Represent the C1-C6 alkylidene group, R ¹¹And R ¹²Be identical or different; represent the C1-C6 alkoxyl group separately) group formed] comprising can be 2 to 6 of this benzyl ring by 1 to 5; the phenyl that preferred 1 to 3 substituting group replaces; described substituting group is selected from by aforesaid halogen atom; halogen replaces or unsubstituted C1-C6 alkyl; halogen replaces or unsubstituted C1-C6 alkoxyl group; can have 1 or 2 group that is selected from C1-C6 alkyloyl and C1-C6 alkyl as substituent amino; the C1-C6 alkoxy carbonyl; phenyl; phenoxy group is (wherein on this benzyl ring; can be substituted with 1 to 5; preferred 1 to 3 substituting group; it is selected from by halogen atom; halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed); amino-sulfonyl; 1; 2; 3; the 4-tetrahydric quinoline group (wherein this 1; 2; 3; on the 4-tetrahydroquinoline ring; can be substituted with 1 to 2 oxo base as substituting group); the C1-C6 alkyl sulphonyl; the C3-C8 cycloalkyl; nitro; cyano group; the C1-C6 alkylthio; benzenesulfonyl is (wherein on this benzyl ring; can be substituted with 1 to 5; preferred 1 to 3 substituting group, it is selected from by halogen atom; halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed); C1-C6 alkyl and following groups that hydroxyl replaces:

(W wherein ₁Represent the C1-C6 alkylidene group, R ¹¹And R ¹²Be identical or different, represent the C1-C6 alkoxyl group separately) group formed.

Hydroxyl with 1 to 3 hydroxyl replaces C1-C6 straight or branched alkyl and comprises for example hydroxymethyl, 2-hydroxyethyl, 1-hydroxyethyl, 3-hydroxypropyl, 2,3-dihydroxypropyl, 4-hydroxybutyl, 3,4-dihydroxyl butyl, 1,1-dimethyl-2-hydroxyethyl, 5-hydroxyl amyl group, 6-hydroxyl hexyl, 2-methyl-3-hydroxypropyl, 2,3,4-trihydroxy-butyl etc.

Halogen replaces or unsubstituted C1-C10 alkoxyl group comprises that aforesaid halogen replaces or unsubstituted C1-C6 alkoxyl group beyond, also comprise the C1-C10 alkoxyl group that is replaced by 1 to 7 C1-C10 alkoxyl group and halogen atom, for example heptan the oxygen base, octyloxy, the ninth of the ten Heavenly Stems oxygen base, the last of the ten Heavenly stems oxygen base, 7-fluorine oxygen in heptan base, 7,7,6-trifluoro oxygen in heptan base, 7,7,7,6,6,5,5-seven fluorine oxygen in heptan bases, 8-chlorine octyloxy, 8,8-dibromo octyloxy, 6,7,8-trifluoro octyloxy, 8,8,8,7,7,6,6-seven fluorine octyloxies, 8,8,8,7,7-pentachloro-octyloxy, 9-iodine oxygen in ninth of the ten Heavenly Stems base, 9,9-dibromo oxygen in ninth of the ten Heavenly Stems base, 9,9,9,8,8-pentachloro-oxygen in ninth of the ten Heavenly Stems base, 9,9,9,8,8,7,7-seven fluorine oxygen in ninth of the ten Heavenly Stems bases, 10-chlorine oxygen in last of the ten Heavenly stems base, 10,10-dibromo oxygen in last of the ten Heavenly stems base, 10,10,10,9-tetrachloro oxygen in last of the ten Heavenly stems base, 10,10,10,9,9,9,8,8-seven fluorine oxygen in last of the ten Heavenly stems bases etc.

Phenyl C1-C6 alkyl is (wherein on this benzyl ring, can be substituted with at least one group as substituting group, it is selected from the alkylene dioxo base by C1-C4, phenyl, halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed) be phenyl C1-C6 alkyl, it is unsubstituted or is constituting on this benzyl ring of this alkyl by 1 to 5, preferred 1 to 3 substituting group replaces (if substituting group is the C1-C4 alkylene dioxo base, then preferred 1 or 2 substituting group), it is selected from the alkylene dioxo base by C1-C4, phenyl, halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed, the example comprises benzyl, the 1-styroyl, the 2-styroyl, the 3-phenyl propyl, the 2-phenyl propyl, the 4-phenyl butyl, the 5-phenylpentyl, the 4-phenylpentyl, 6-phenyl hexyl, 2, the 3-methylenedioxy benzyl, 3, the 4-methylenedioxy benzyl, the 3-phenylbenzyl, the 2-phenylbenzyl, the 4-phenylbenzyl, 3,4-phenylbenzene benzyl, 2,4,6-triphenyl benzyl, the 2-luorobenzyl, the 3-luorobenzyl, the 4-luorobenzyl, 2-benzyl chloride base, 3-benzyl chloride base, 4-benzyl chloride base, the 2-bromobenzyl, the 3-bromobenzyl, the 4-bromobenzyl, 2-iodine benzyl, 3-iodine benzyl, 4-iodine benzyl, 2, the 3-difluorobenzyl, 3, the 4-difluorobenzyl, 3, the 5-difluorobenzyl, 2, the 4-difluorobenzyl, 2, the 6-difluorobenzyl, 2, the 3-dichloro benzyl, 3, the 4-dichloro benzyl, 3, the 5-dichloro benzyl, 2, the 4-dichloro benzyl, 2, the 6-dichloro benzyl, 2-fluoro-4-bromobenzyl, 4-chloro-3-luorobenzyl, 2,3,4-trichlorine benzyl, 3,4, the 5-trifluoro-benzyl, 2,4,6-trichlorine benzyl, the 4-Ethylbenzyl, 4-sec-butyl benzyl, the 4-isopropyl benzyl, 4-normal-butyl benzyl, the 4-methyl-benzyl, the 2-methyl-benzyl, the 3-methyl-benzyl, 2, the 4-dimethyl benzyl, 2, the 3-dimethyl benzyl, 2, the 6-dimethyl benzyl, 3, the 5-dimethyl benzyl, 2, the 5-dimethyl benzyl, 2,4, the 6-trimethyl benzyl, 3,5-two trifluoromethyl benzyls, 2,3,4,5, the 6-PFBBR, the 4-isopropoxide benzyl, 4-n-butoxy benzyl, 4-tert.-butoxy benzyl, the 4-methoxy-benzyl, the 2-methoxy-benzyl, the 3-methoxy-benzyl, 2, the 4-dimethoxy-benzyl, 2, the 3-dimethoxy-benzyl, 2, the 6-dimethoxy-benzyl, 3, the 5-dimethoxy-benzyl, 2, the 5-dimethoxy-benzyl, 2,4,6-trimethoxy benzyl, 3,5-two trifluoro-methoxybenzyls, the 2-isopropoxide benzyl, 3-chloro-4-methoxy-benzyl, 2-chloro-4-trifluoro-methoxybenzyl, 3-methyl-4-luorobenzyl, 4-bromo-3-trifluoromethyl benzyl, the 2-trifluoromethyl benzyl, the 3-trifluoromethyl benzyl, the 4-trifluoromethyl benzyl, 2-pentafluoroethyl group benzyl, 3-pentafluoroethyl group benzyl, 4-pentafluoroethyl group benzyl, the 2-trifluoro-methoxybenzyl, the 3-trifluoro-methoxybenzyl, the 4-trifluoro-methoxybenzyl, 2-five fluorine ethoxy benzyls, 3-five fluorine ethoxy benzyls, 4-five fluorine ethoxy benzyls, 2-(2-trifluoromethyl) ethyl, 2-(3-trifluoromethyl) ethyl, 2-(4-trifluoromethyl) ethyl, 2-(2-Trifluoromethoxyphen-l) ethyl, 1-(3-Trifluoromethoxyphen-l) ethyl, 2-(4-Trifluoromethoxyphen-l) ethyl, 2-(2-five fluorine ethoxyl phenenyls) ethyl, 2-(3-five fluorine ethoxyl phenenyls) ethyl, 2-(4-five fluorine ethoxyl phenenyls) ethyl, 3-(2-trifluoromethyl) propyl group, 3-(3-trifluoromethyl) propyl group, 3-(4-trifluoromethyl) propyl group, 3-(2-Trifluoromethoxyphen-l) propyl group, 3-(3-Trifluoromethoxyphen-l) propyl group, 3-(4-Trifluoromethoxyphen-l) propyl group, 3-(3-five fluorine ethoxyl phenenyls) propyl group, 3-(4-five fluorine ethoxyl phenenyls) propyl group, 4-(3-five fluorine ethoxyl phenenyls) butyl, 5-(4-trifluoromethyl) amyl group, 4-(4-trifluoromethyl) amyl group, 4-(4-Trifluoromethoxyphen-l) amyl group, 6-(3-trifluoromethyl) hexyl, 6-(4-trifluoromethyl) hexyl, 6-(4-Trifluoromethoxyphen-l) hexyl, 4-(4-chloro-phenyl-) butyl etc.

Phenyl C1-C6 alkyl is [wherein on this benzyl ring, can be substituted with at least one and be selected from following group as substituting group: C1-C4 alkylene dioxo base, phenyl are (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group), group-N (R ^11A) R ^12A(R wherein ^11AAnd R ^12ABe identical or different, represent hydrogen atom, C1-C6 alkyl or phenyl separately, R ^11AAnd R ^12ACan by or do not pass through nitrogen, oxygen or sulphur atom be bonding each other, constitute five to seven yuan of saturated heterocyclics with their adjacent nitrogen-atoms), phenoxy group is (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed), phenyl C1-C6 alkoxyl group, can have the C1-C6 alkyl as the substituent C1-C6 alkoxyl group that is replaced by amino, halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C10 alkoxyl group is formed] comprise that aforesaid phenyl C1-C6 alkyl is (wherein on this benzyl ring, can be substituted with at least one group as substituting group, it is selected from the alkylene dioxo base by C1-C4, phenyl, halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed) in addition, comprise that also phenyl C1-C6 alkyl is [wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 substituting group is (if substituting group is the C1-C4 alkylene dioxo base, then preferred 1 or 2 substituting group), it is selected from the alkylene dioxo base by C1-C4, aforesaid phenyl is (wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 substituting group, it is selected from by halogen atom, halogen replaces or the unsubstituted straight or branched alkyl that contains 1 to 6 carbon atom, the group that halogen replaces or the unsubstituted straight or branched alkoxyl group that contains 1 to 6 carbon atom is formed), group-N (R ^11A) R ^12A(R wherein ^11AAnd R ^12ABe identical or different, represent hydrogen atom, aforesaid C1-C6 alkyl or phenyl separately, R ^11AAnd R ^12AAs hereinafter described, can by or do not pass through nitrogen, oxygen or sulphur atom and bonding each other, constitute five to seven yuan of saturated heterocyclics with their adjacent nitrogen-atoms), aforesaid phenoxy group is (wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 substituting group, it is selected from by halogen atom, halogen replaces or the unsubstituted straight or branched alkyl that contains 1 to 6 carbon atom, the group that halogen replaces or the unsubstituted straight or branched alkoxyl group that contains 1 to 6 carbon atom is formed), aforesaid phenyl C1-C6 alkoxyl group, can have the C1-C6 alkyl as mentioned above as the substituent C1-C6 alkoxyl group that is replaced by amino, aforesaid halogen atom, aforesaid halogen replacement or unsubstituted C1-C6 alkyl and the group that aforesaid halogen replaces or unsubstituted C1-C10 alkoxyl group is formed], 4-(4-trifluoromethyl) benzyl for example, 4-(4-Trifluoromethoxyphen-l) benzyl, 4-(4-chloro-phenyl-) benzyl, 4-(4-4-trifluoromethylphenopendant) benzyl, 4-(4-Trifluoromethyl phenyl ether oxygen base) benzyl, 4-(4-chlorophenoxy) benzyl, the 4-phenoxy benzyl, the 3-phenoxy benzyl, the 2-phenoxy benzyl, 2-4-two phenoxy benzyls, 2,4,6-triple phenoxyl benzyl, 4-benzyloxy benzyl, 3-benzyloxy benzyl, 2-benzyloxy benzyl, 3,4-benzyloxy benzyl, 3,4,5-three benzyloxy benzyls, 4-octyloxy benzyl, 3-oxy-benzyl in the ninth of the ten Heavenly Stems, 2-oxy-benzyl in the last of the ten Heavenly stems, 4-oxy-benzyl in heptan, 2,4-two octyloxy benzyls, 3,4,6-three octyloxy benzyls, 4-(8,8,8-trifluoro octyloxy) benzyl, 4-dimethylamino benzyl, 4-diphenyl amino benzyl, 4-(3-dimethylamino propoxy) benzyl, 4-di-n-butyl aminobenzyl, 3-(N-methyl-N-ethylamino) benzyl, 2-(N-methyl-N-phenyl amino) benzyl, 2,4,6-methylamino benzyl, 3-(3-dimethylamino propoxy) benzyl, 2,4-di-n-butyl aminobenzyl, 4-(2-methyl amino ethoxy) benzyl, 2-(4-methylamino butoxy) benzyl, 4-(2-dimethylamino ethoxy) benzyl, 2,3-diethylamino methoxy-benzyl, 2,4,6-three (2-dimethylamino ethoxy) benzyl, 2-phenoxy group-3-phenylbenzyl, 4-octyloxy-3-trifluoro-methoxybenzyl, 4-benzyloxy-2-dimethylamino benzyl, 4-(1-pyrrolidyl) benzyl, 4-(piperidino) benzyl etc.

Benzofuryl C1-C6 alkyl is [wherein on this cumarone ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed] comprise that benzofuryl C1-C6 alkyl is [wherein on this cumarone ring, can be substituted with 1 to 3 substituting group, it is selected from by aforesaid halogen atom, aforesaid halogen replacement or unsubstituted C1-C6 alkyl and the group that aforesaid halogen replaces or unsubstituted C1-C6 alkoxyl group is formed], (2-for example, 3-, 4-, 5-, 6-or 7-) the cumarone ylmethyl, 1-(2-benzofuryl) ethyl, 2-(3-benzofuryl) ethyl, 3-(4-benzofuryl) propyl group, 2-(5-benzofuryl) propyl group, 2-(6-benzofuryl) propyl group, 4-(7-benzofuryl) butyl, 5-(2-benzofuryl) amyl group, 4-(3-benzofuryl) amyl group, 6-(4-benzofuryl) hexyl, 2-methyl-3-(5-benzofuryl) propyl group, 1,1-dimethyl-2-(6-benzofuryl) ethyl, (5-chloro-2-benzofuryl) methyl, 2-(5-trifluoromethoxy benzo furyl) methyl, 2-(5-trifluoromethyl benzo furyl) methyl, (6-trifluoromethyl benzo furyl) methyl, 2-(5-methyl benzofuryl) methyl, 2-(5-methoxyl group benzo furyl) methyl, (5,6-two bromo-2-benzofuryls) methyl, (3,5,6-three fluoro-2-benzofuryls) methyl, 2-(5,6-dimethyl benzofuran base) methyl, 2-(5,7-dimethoxy benzo furyl) methyl, 2-(5,6,7-trimethylammonium benzo furyl) methyl, 2-(3,5,6-trimethoxy benzo furyl) methyl, 2-(5-trifluoromethyl-6-chlorobenzene and furyl) methyl, 2-(5-trifluoromethoxy-6-methoxyl group benzo furyl) methyl etc.

Benzenesulfonyl is [wherein on this benzyl ring; can be substituted with at least one group; it is selected from by halogen atom; halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group] be unsubstituted or have 1 to 5; preferred 1 to 3 substituting group is (if substituting group is the C1-C4 alkylene dioxo base; then preferred 1 or 2 substituting group) benzenesulfonyl; described substituting group is selected from by halogen atom; halogen replaces or unsubstituted C1-C6 alkyl; halogen replaces or the unsubstituted C1-C6 alkoxyl group and the group of C1-C4 alkylene dioxo base composition as defined above; benzenesulfonyl for example; 2-fluorophenyl alkylsulfonyl; 3-fluorophenyl alkylsulfonyl; 4-fluorophenyl alkylsulfonyl; 2-chloro-phenyl-alkylsulfonyl; 3-chloro-phenyl-alkylsulfonyl; 4-chloro-phenyl-alkylsulfonyl; 2-bromophenyl alkylsulfonyl; 3-bromophenyl alkylsulfonyl; 4-bromophenyl alkylsulfonyl; 2-iodophenyl alkylsulfonyl; 3-iodophenyl alkylsulfonyl; 4-iodophenyl alkylsulfonyl; 2; 3-difluorophenyl alkylsulfonyl; 3; 4-difluorophenyl alkylsulfonyl; 3; 5-difluorophenyl alkylsulfonyl; 2; 4-difluorophenyl alkylsulfonyl; 2; 6-difluorophenyl alkylsulfonyl; 2; 3-dichlorophenyl alkylsulfonyl; 3; 4-dichlorophenyl alkylsulfonyl; 3; 5-dichlorophenyl alkylsulfonyl; 2; 4-dichlorophenyl alkylsulfonyl; 2; 6-dichlorophenyl alkylsulfonyl; 3; 4; 5-trifluorophenyl alkylsulfonyl; 3; 4; 5-trichlorophenyl alkylsulfonyl; 2; 4; 6-trifluorophenyl alkylsulfonyl; 2; 4; 6-trichlorophenyl alkylsulfonyl; 2-fluoro-4-bromophenyl alkylsulfonyl; 4-chloro-3-fluorophenyl alkylsulfonyl; 2; 3; 4-trichlorophenyl alkylsulfonyl; 3; 4; 5-trifluorophenyl alkylsulfonyl; 2; 3; 4; 5; 6-pentafluorophenyl group alkylsulfonyl; 2; 4; 6-trimethylphenyl alkylsulfonyl; 4-n-butylphenyl alkylsulfonyl; 2; 4-3,5-dimethylphenyl alkylsulfonyl; 2; 3-3,5-dimethylphenyl alkylsulfonyl; 2; 6-3,5-dimethylphenyl alkylsulfonyl; 3; 5-3,5-dimethylphenyl alkylsulfonyl; 2; 5-3,5-dimethylphenyl alkylsulfonyl; 3; 5-two trifluoromethyl alkylsulfonyls; 4-n-butoxy phenyl sulfonyl; 2; 4-Dimethoxyphenyl alkylsulfonyl; 2; 3-Dimethoxyphenyl alkylsulfonyl; 2; 6-Dimethoxyphenyl alkylsulfonyl; 3; 5-Dimethoxyphenyl alkylsulfonyl; 2; 5-Dimethoxyphenyl alkylsulfonyl; 2; 4; 6-trimethoxyphenyl alkylsulfonyl; 3; 5-two Trifluoromethoxyphen-l alkylsulfonyls; 3-chloro-4-p-methoxy-phenyl alkylsulfonyl; 2-chloro-4-Trifluoromethoxyphen-l alkylsulfonyl; 3-methyl-4-fluorophenyl alkylsulfonyl; 4-bromo-3-trifluoromethyl alkylsulfonyl; 2-aminomethyl phenyl alkylsulfonyl; 3-aminomethyl phenyl alkylsulfonyl; 4-aminomethyl phenyl alkylsulfonyl; 2-methyl-3-chloro-phenyl-alkylsulfonyl; 3-methyl-4-chloro-phenyl-alkylsulfonyl; 2-chloro-4-aminomethyl phenyl alkylsulfonyl; 2-methyl-3-fluorophenyl alkylsulfonyl; 2-trifluoromethyl alkylsulfonyl; 3-trifluoromethyl alkylsulfonyl; 4-trifluoromethyl alkylsulfonyl; 2-pentafluoroethyl group phenyl sulfonyl; 3-pentafluoroethyl group phenyl sulfonyl; 4-pentafluoroethyl group phenyl sulfonyl; 2-isopropyl phenyl alkylsulfonyl; 3-isopropyl phenyl alkylsulfonyl; 4-isopropyl phenyl alkylsulfonyl; 2-tert-butyl-phenyl alkylsulfonyl; 3-tert-butyl-phenyl alkylsulfonyl; 4-tert-butyl-phenyl alkylsulfonyl; 2-secondary butyl phenenyl alkylsulfonyl; 3-secondary butyl phenenyl alkylsulfonyl; 4-secondary butyl phenenyl alkylsulfonyl; 2-is the fluoropropyl phenyl sulfonyl just-seven; 3-is the fluoropropyl phenyl sulfonyl just-seven; 4-is the fluoropropyl phenyl sulfonyl just-seven; 4-n-pentyl phenyl alkylsulfonyl; 4-n-hexyl phenyl alkylsulfonyl; 2-p-methoxy-phenyl alkylsulfonyl; 3-p-methoxy-phenyl alkylsulfonyl; 4-p-methoxy-phenyl alkylsulfonyl; 3-chloro-2-p-methoxy-phenyl alkylsulfonyl; 2-fluoro-3-p-methoxy-phenyl alkylsulfonyl; 2-fluoro-4-p-methoxy-phenyl alkylsulfonyl; 2; 6-Dimethoxyphenyl alkylsulfonyl; 2; 3; 4-trifluorophenyl alkylsulfonyl; 2; 4; 6-trifluorophenyl alkylsulfonyl; 2-Trifluoromethoxyphen-l alkylsulfonyl; 3-Trifluoromethoxyphen-l alkylsulfonyl; 4-Trifluoromethoxyphen-l alkylsulfonyl; 3-fluoro-2-Trifluoromethoxyphen-l alkylsulfonyl; 2-fluoro-3-Trifluoromethoxyphen-l alkylsulfonyl; 3-fluoro-4-Trifluoromethoxyphen-l alkylsulfonyl; 3-chloro-2-Trifluoromethoxyphen-l alkylsulfonyl; 2-chloro-3-Trifluoromethoxyphen-l alkylsulfonyl; 3-chloro-4-Trifluoromethoxyphen-l alkylsulfonyl; 2-five fluorine ethoxyl phenenyl alkylsulfonyls; 3-five fluorine ethoxyl phenenyl alkylsulfonyls; 4-five fluorine ethoxyl phenenyl alkylsulfonyls; 3-chloro-2-five fluorine ethoxyl phenenyl alkylsulfonyls; 2-chloro-3-five fluorine ethoxyl phenenyl alkylsulfonyls; 3-chloro-4-five fluorine ethoxyl phenenyl alkylsulfonyls; 2-isopropyl phenyl alkylsulfonyl; 3-isopropyl phenyl alkylsulfonyl; 4-isopropyl phenyl alkylsulfonyl; 2-tert.-butoxy phenyl sulfonyl; 3-tert.-butoxy phenyl sulfonyl; 4-tert.-butoxy phenyl sulfonyl; 2-sec-butoxy phenyl sulfonyl; 3-sec-butoxy phenyl sulfonyl; 4-sec-butoxy phenyl sulfonyl; 2-is fluorine propoxy-phenyl sulfonyl just-seven; 3-is fluorine propoxy-phenyl sulfonyl just-seven; 4-is fluorine propoxy-phenyl sulfonyl just-seven; 4-n-pentyloxy phenyl sulfonyl; the positive hexyloxy phenyl sulfonyl of 4-; 2; 3-methylenedioxyphenyl alkylsulfonyl; 3,4-methylenedioxyphenyl alkylsulfonyl etc.

Phenyloxycarbonyl is [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed] comprise that phenyloxycarbonyl is (wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 substituting group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed), phenyloxycarbonyl for example, 2-fluorophenoxy carbonyl, 3-fluorophenoxy carbonyl, 2,3,4,5,6-penta fluoro benzene oxygen base carbonyl, 4-fluorophenoxy carbonyl, 2-chlorophenoxy carbonyl, 3-chlorophenoxy carbonyl, 4-chlorophenoxy carbonyl, 2,3-dichlorophenoxy carbonyl, 3,4-dichlorophenoxy carbonyl, 3,5-dichlorophenoxy carbonyl, 2-bromine phenyloxycarbonyl, 3-bromine phenyloxycarbonyl, 4-bromine phenyloxycarbonyl, 2-methylphenoxy carbonyl, 3-methylphenoxy carbonyl, 4-methylphenoxy carbonyl, 2-ethyl phenyloxycarbonyl, 3-ethyl phenyloxycarbonyl, 4-ethyl phenyloxycarbonyl, 4-n-propyl phenyloxycarbonyl, 4-tertiary butyl phenyloxycarbonyl, 4-normal-butyl phenyloxycarbonyl, 2,3-dimethyl phenoxy carbonyl, 3,4,5-trimethylammonium phenyloxycarbonyl, 4-n-pentyl phenyloxycarbonyl, 4-n-hexyl phenyloxycarbonyl, 2-fluoro-4-bromine phenyloxycarbonyl, 4-chloro-3-fluorophenoxy carbonyl, 2,3,4-Trichlorophenoxy carbonyl, 2,4,6-Trichlorophenoxy carbonyl, 4-sec.-propyl phenyloxycarbonyl, 4-normal-butyl phenyloxycarbonyl, 2,4-dimethyl phenoxy carbonyl, 2,3-dimethyl phenoxy carbonyl, 2,6-dimethyl phenoxy carbonyl, 3,5-dimethyl phenoxy carbonyl, 2,5-dimethyl phenoxy carbonyl, 2,4,6-trimethylammonium phenyloxycarbonyl, 3,5-two 4-trifluoromethylphenopendant carbonyls, 4-n-butoxy phenyloxycarbonyl, 2,4-dimethoxy phenyloxycarbonyl, 2,3-dimethoxy phenyloxycarbonyl, 2,6-dimethoxy phenyloxycarbonyl, 3,5-dimethoxy phenyloxycarbonyl, 2,5-dimethoxy phenyloxycarbonyl, 3,5-two Trifluoromethyl phenyl ether oxygen base carbonyls, 3-chloro-4-methoxyl group phenyloxycarbonyl, 2-chloro-4-Trifluoromethyl phenyl ether oxygen base carbonyl, 3-methyl-4-fluorophenoxy carbonyl, 4-bromo-3-4-trifluoromethylphenopendant carbonyl, 2-4-trifluoromethylphenopendant carbonyl, 3-4-trifluoromethylphenopendant carbonyl, 4-4-trifluoromethylphenopendant carbonyl, 2-pentafluoroethyl group phenyloxycarbonyl, 3-pentafluoroethyl group phenyloxycarbonyl, 4-pentafluoroethyl group phenyloxycarbonyl, 2-methoxyl group phenyloxycarbonyl, 3-methoxyl group phenyloxycarbonyl, 4-methoxyl group phenyloxycarbonyl, 2-ethoxy phenoxy carbonyl, 3-ethoxy phenoxy carbonyl, 4-ethoxy phenoxy carbonyl, 4-positive propoxy phenyloxycarbonyl, 4-tert.-butoxy phenyloxycarbonyl, 4-n-butoxy phenyloxycarbonyl, 2,3-dimethoxy phenyloxycarbonyl, 3,4,5-trimethoxy phenyloxycarbonyl, 4-n-pentyloxy phenyloxycarbonyl, the positive hexyloxy phenyloxycarbonyl of 4-, 2-Trifluoromethyl phenyl ether oxygen base carbonyl, 3-Trifluoromethyl phenyl ether oxygen base carbonyl, 4-Trifluoromethyl phenyl ether oxygen base carbonyl, 2-five fluorine ethoxy phenoxy carbonyls, 3-five fluorine ethoxy phenoxy carbonyls, 4-five fluorine ethoxy phenoxy carbonyls etc.

The C1-C6 alkyl that the C1-C6 alkoxyl group replaces is by being the group that aforesaid C1-C6 alkyl and C1-C6 alkoxyl group are formed, and the example comprises methoxymethyl, 2-methoxy ethyl, 3-methoxy-propyl, 4-methoxyl group butyl, 5-methoxyl group amyl group, 6-methoxyl group hexyl, ethoxyl methyl, 2-ethoxyethyl group, 3-ethoxycarbonyl propyl, 2-isopropoxy ethyl, tert.-butoxy methyl, pentyloxy methyl, hexyloxy methyl, 2-(tert.-butoxy) ethyl, 3-(tert.-butoxy) propyl group, 6-(tert.-butoxy) hexyl, 4-(tert.-butoxy) butyl etc.

The C2-C6 thiazolinyl comprises vinyl, 2-propenyl, 3-butenyl, crotyl, 4-pentenyl, 3-pentenyl, 5-hexenyl, 4-hexenyl, 3-hexenyl etc.

The C2-C6 alkyloyl that the C1-C6 alkoxyl group replaces is by being the group that aforesaid C1-C6 alkyl and C2-C6 alkyloyl are formed, and the example comprises 2-methoxyl group ethanoyl; 2-methoxy propyl acyl group; 3-methoxy propyl acyl group; 4-methoxyl group butyryl radicals; 5-methoxyl group pentanoyl; 6-methoxyl group caproyl; 2-oxyethyl group ethanoyl; 2-ethoxy-c acyl group; 3-ethoxy-c acyl group; 2-isopropoxy propionyl; 2-(tert.-butoxy) ethanoyl; 2-pentyloxy ethanoyl; 2-hexyloxy ethanoyl; 2-(tert.-butoxy) propionyl; 3-(tert.-butoxy) propionyl; 6-(tert.-butoxy) caproyl; 4-(tert.-butoxy) butyryl radicals etc.

The group that the C1-C6 alkyl of C3-C8 cycloalkyl substituted is made up of cyclic alkyl that contains 3 to 8 carbon atoms and the alkyl that contains 1 to 6 carbon atom, the example comprises the cyclopropyl methyl, 2-cyclopropyl ethyl, 3-cyclopropyl propyl group, 4-cyclopropyl butyl, 5-cyclopropyl amyl group, 6-cyclopropyl hexyl, cyclobutylmethyl, 2-cyclobutyl ethyl, 3-cyclobutyl propyl group, 4-cyclobutyl butyl, 5-cyclobutyl amyl group, 6-cyclobutyl hexyl, cyclopentyl-methyl, 2-cyclopentyl ethyl, 3-cyclopentyl propyl group, 4-cyclopentyl butyl, 5-cyclopentyl amyl group, 6-cyclopentyl hexyl, cyclohexyl methyl, 2-cyclohexyl ethyl, 3-cyclohexyl propyl group, 4-cyclohexyl butyl, 5-cyclohexyl amyl group, 6-cyclohexyl hexyl, the suberyl methyl, 2-suberyl ethyl, 3-suberyl propyl group, 4-suberyl butyl, 5-suberyl amyl group, 6-suberyl hexyl, ring octyl group methyl, 2-ring octyl group ethyl, 3-ring octyl group propyl group, 4-ring octyl group butyl, 5-ring octyl group amyl group, 6-ring octyl group hexyl etc.

Pyridyl C1-C6 alkyl comprises 2-pyridylmethyl, 2-(3-pyridyl) ethyl, 1-(4-pyridyl) ethyl, 3-(2-pyridyl) propyl group, 4-(3-pyridyl) butyl, 5-(4-pyridyl) amyl group, 6-(2-pyridyl) hexyl, 2-methyl-3-(3-pyridyl) propyl group, 1,1-dimethyl-2-(2-pyridyl) ethyl etc.

Imidazolyl C1-C6 alkyl is (wherein on this imidazole ring, can be substituted with phenyl) comprise that imidazolyl C1-C6 alkyl is (wherein on this imidazole ring, can be substituted with 1 to 2 phenyl), 4-imidazolyl methyl for example, 2-(4-imidazolyl) ethyl, 3-(2-imidazolyl) propyl group, 4-(1-imidazolyl) butyl, 5-(5-imidazolyl) amyl group, 6-(4-imidazolyl) hexyl, 2,5-phenylbenzene-1-imidazolyl methyl, 2-phenyl-4-imidazolyl methyl, 2-(2-phenyl-4-imidazolyl) ethyl, 3-(2-phenyl-4-imidazolyl) propyl group, 4-(2-phenyl-5-imidazolyl) butyl, 5-(2-phenyl-4-imidazolyl) amyl group, 6-(2-phenyl-4-imidazolyl) hexyl etc.

1,2,3, the 4-tetrahydric quinoline group (wherein this 1,2,3, on the 4-tetrahydroquinoline ring, can be substituted with at least one group as substituting group, it is selected from the group of being made up of oxo base and C1-C6 alkyl) comprise 1,2,3, the 4-tetrahydric quinoline group (wherein this 1,2,3, on the 4-tetrahydroquinoline ring, can be substituted with 1 to 5 substituting group, it is selected from the group of being made up of oxo base and C1-C6 alkyl), for example 1,2,3,4-tetrahydrochysene-1-quinolyl, 1,2,3,4-tetrahydrochysene-2-quinolyl, 1,2,3,4-tetrahydrochysene-3-quinolyl, 1,2,3,4-tetrahydrochysene-4-quinolyl, 1,2,3,4-tetrahydrochysene-5-quinolyl, 1,2,3,4-tetrahydrochysene-6-quinolyl, 1,2,3,4-tetrahydrochysene-7-quinolyl, 1,2,3,4-tetrahydrochysene-8-quinolyl, 2-oxo-1,2,3,4-tetrahydrochysene-1-quinolyl, 4-oxo-1,2,3,4-tetrahydrochysene-1-quinolyl, 2,4-dioxo-1,2,3,4-tetrahydrochysene-1-quinolyl, 2-oxo-1,2,3,4-tetrahydrochysene-6-quinolyl, 2-oxo-1,2,3,4-tetrahydrochysene-4-quinolyl, 2-oxo-1,2,3,4-tetrahydrochysene-7-quinolyl, 2-oxo-1,2,3,4-tetrahydrochysene-8-quinolyl, 2-oxo-1,2,3,4-tetrahydrochysene-5-quinolyl, 2-oxo-1,2,3,4-tetrahydrochysene-3-quinolyl, the 2-methyl isophthalic acid, 2,3,4-tetrahydrochysene-1-quinolyl, 4-ethyl-1,2,3,4-tetrahydrochysene-1-quinolyl, 2,4-dimethyl-1,2,3,4-tetrahydrochysene-1-quinolyl, 1,5,6-trimethylammonium-1,2,3,4-tetrahydrochysene-1-quinolyl, 1,4,5,6-tetramethyl--2-oxo-1,2,3,4-tetrahydrochysene-1-quinolyl, 1-propyl group-1,2,3,4-tetrahydrochysene-6-quinolyl, 5-n-pentyl-1,2,3,4-tetrahydrochysene-4-quinolyl, 6-n-hexyl-1,2,3,4-tetrahydrochysene-7-quinolyl, the 7-tertiary butyl-1,2,3,4-tetrahydrochysene-8-quinolyl, 8-n-pentyl-1,2,3,4-tetrahydrochysene-8-quinolyl, 1-n-hexyl-2-oxo-1,2,3,4-tetrahydrochysene-8-quinolyl, 1-methyl-2-oxo-1,2,3,4-tetrahydrochysene-5-quinolyl, 3-ethyl-2-oxo-1,2,3,4-tetrahydrochysene-3-quinolyl etc.

Can have the C1-C6 alkyl and comprise to have 1 to 2 C1-C6 alkyl, for example amino, methylamino, ethylamino, n-propyl amino, sec.-propyl amino, normal-butyl amino, tertiary butyl amino, n-pentyl amino, n-hexyl amino, dimethylamino, diethylamino, two-n-propyl amino, di-n-butyl amino, two-n-pentyl amino, two-n-hexyl amino, N-methyl-N-ethylamino, N-ethyl-N-n-propyl amino, N-methyl-N-normal-butyl amino, N-methyl-N-n-hexyl amino etc. as substituent amino as substituent amino.

The C1-C6 alkyl that cyano group replaces comprises cyano methyl, 2-cyano ethyl, 1-cyano ethyl, 3-cyano group propyl group, 4-cyano group butyl, 5-cyano group amyl group, 6-cyano group hexyl, 2-methyl-3-cyano group propyl group, 1,1-dimethyl-2-cyano ethyl etc.

The C1-C6 alkyl that furyl replaces comprises 2-furyl methyl, 3-furyl methyl, 2-(2-furyl) ethyl, 1-(3-furyl) ethyl, 3-(2-furyl) propyl group, 3-(3-furyl) propyl group, 4-(2-furyl) butyl, 4-(3-furyl) butyl, 5-(2-furyl) amyl group, 5-(3-furyl) amyl group, 6-(2-furyl) hexyl, 6-(3-furyl) hexyl etc.

The C1-C6 alkyl that piperazinyl replaces is [wherein on this piperazine ring, can be substituted with at least one phenyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed)] comprise that the C1-C6 alkyl of piperazinyl replacement is [wherein on this piperazine ring, can be substituted with 1 to 3 phenyl as substituting group (wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 substituting group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed)], 1-piperazinyl methyl for example, 2-(2-piperazinyl) ethyl, 1-(1-piperazinyl) ethyl, 3-(1-piperazinyl) propyl group, 4-(1-piperazinyl) butyl, 5-(2-piperazinyl) amyl group, 6-(1-piperazinyl) hexyl, 2-(4-phenyl-peiperazinyl) ethyl, 3-(4-phenyl-peiperazinyl) propyl group, 4-(4-phenyl-peiperazinyl) butyl, 5-(4-phenyl-peiperazinyl) amyl group, 6-(4-phenyl-peiperazinyl) hexyl, 2-(4-(2-fluorophenyl)-1-piperazinyl) ethyl, 3-(4-(2-fluorophenyl)-1-piperazinyl) propyl group, (4-(2 for 4-, the 3-difluorophenyl)-and the 1-piperazinyl) butyl, 5-(4-(2-fluorophenyl)-1-piperazinyl) amyl group, 6-(4-(4-fluorophenyl)-1-piperazinyl) hexyl, 3-(4-(3-fluorophenyl)-1-piperazinyl) propyl group, 4-(4-(3-fluorophenyl)-1-piperazinyl) butyl, 5-(4-(3-fluorophenyl)-1-piperazinyl) amyl group, 3-(4-(4-fluorophenyl)-1-piperazinyl) propyl group, 4-(4-(fluorophenyl)-1-piperazinyl) butyl, 5-(4-(4-fluorophenyl)-1-piperazinyl) amyl group, 6-(4-(fluorophenyl)-1-piperazinyl) hexyl, (4-(2 for 2-, the 3-dichlorophenyl)-and the 1-piperazinyl) ethyl, 3-(4-(2-chloro-phenyl-)-1-piperazinyl) propyl group, 4-(4-(2-chloro-phenyl-)-1-piperazinyl) butyl, (4-(2 for 5-, 4, the 6-trichlorophenyl)-and the 1-piperazinyl) amyl group, 6-(4-(2-chloro-phenyl-)-1-piperazinyl) hexyl, 2-(4-(3-chloro-phenyl-)-1-piperazinyl) ethyl, 3-(4-(3-chloro-phenyl-)-1-piperazinyl) propyl group, 4-(4-(3-chloro-phenyl-)-1-piperazinyl) butyl, (4-(2 for 5-, 3,4,5, the 6-pentafluorophenyl group)-and the 1-piperazinyl) amyl group, 6-(4-(3-chloro-4-aminomethyl phenyl)-1-piperazinyl) hexyl, 2-(4-(4-chloro-phenyl-)-1-piperazinyl) ethyl, 3-(4-(4-chloro-phenyl-)-1-piperazinyl) propyl group, 4-(4-(4-chloro-3-p-methoxy-phenyl)-1-piperazinyl) butyl, 5-(4-(4-chloro-phenyl-)-1-piperazinyl) amyl group, 6-(4-(4-chloro-phenyl-)-1-piperazinyl) hexyl, 2-(4-(2-aminomethyl phenyl)-1-piperazinyl) methyl, (4-(2 for 2-, the 4-3,5-dimethylphenyl)-and the 1-piperazinyl) methyl, (4-(2 for 2-, 4, the 6-trimethylphenyl)-and the 1-piperazinyl) methyl, 2-(4-(2-trifluoromethyl)-1-piperazinyl) ethyl, (4-(3 for 3-, 5-two trifluoromethyls)-and the 1-piperazinyl) propyl group, 4-(4-(2-trifluoromethyl)-1-piperazinyl) butyl, 5-(4-(2-trifluoromethyl)-1-piperazinyl) amyl group, 6-(4-(2-trifluoromethyl)-1-piperazinyl) hexyl, 3-(4-(3-trifluoromethyl)-1-piperazinyl) propyl group, 4-(4-(3-trifluoromethyl)-1-piperazinyl) butyl, 5-(4-(3-trifluoromethyl)-1-piperazinyl) amyl group, 3-(4-(4-trifluoromethyl)-1-piperazinyl) propyl group, 4-(4-(4-trifluoromethyl)-1-piperazinyl) butyl, 5-(4-(4-trifluoromethyl)-1-piperazinyl) amyl group, 6-(4-(4-trifluoromethyl)-1-piperazinyl) hexyl, (4-(3 for 2-, 5-two Trifluoromethoxyphen-ls)-and the 1-piperazinyl) ethyl, 2-(4-(2-p-methoxy-phenyl)-1-piperazinyl) methyl, (4-(2 for 2-, the 4-Dimethoxyphenyl)-and the 1-piperazinyl) methyl, (4-(2 for 2-, 4, the 6-trimethoxyphenyl)-and the 1-piperazinyl) methyl, 3-(4-(2-Trifluoromethoxyphen-l)-1-piperazinyl) propyl group, 4-(4-(2-Trifluoromethoxyphen-l)-1-piperazinyl) butyl, 5-(4-(2-Trifluoromethoxyphen-l)-1-piperazinyl) amyl group, 6-(4-(2-Trifluoromethoxyphen-l)-1-piperazinyl) hexyl, 3-(4-(3-Trifluoromethoxyphen-l)-1-piperazinyl) propyl group, 4-(4-(3-Trifluoromethoxyphen-l)-1-piperazinyl) butyl, 5-(4-(3-Trifluoromethoxyphen-l)-1-piperazinyl) amyl group, 3-(4-(4-Trifluoromethoxyphen-l)-1-piperazinyl) propyl group, 4-(4-(4-Trifluoromethoxyphen-l)-1-piperazinyl) butyl, 5-(4-(4-Trifluoromethoxyphen-l)-1-piperazinyl) amyl group, 6-(4-(4-Trifluoromethoxyphen-l)-1-piperazinyl) hexyl, 2,4-phenylbenzene-1-piperazinyl methyl, (2,4,5-triphenyl-1-piperazinyl) methyl etc.

R ⁹And R ¹⁰, R ^11AAnd R ^12APerhaps R ^11BAnd R ^12BCan directly or by nitrogen, oxygen or sulphur atom be bonded to each other, constitute 5-7 unit saturated heterocyclic group with their adjacent nitrogen-atoms.The example of 5-7 unit saturated heterocyclic group can comprise that pyrrolidyl, piperazinyl, piperidyl, morpholino base, parathiazan are for base and high piperazinyl.

R ⁹And R ¹⁰Can directly or by nitrogen, oxygen or sulphur atom be bonded to each other, constitute 1,2,3,4-tetrahydro isoquinolyl, pseudoindoyl or above-mentioned 5-7 unit saturated heterocyclic with their adjacent nitrogen-atoms.On this group or ring; can be substituted with the group that at least one is selected from down group: halogen atom; halogen replaces or unsubstituted C1-C6 alkyl; halogen replaces or unsubstituted C1-C6 alkoxyl group; phenyl is [wherein on this benzyl ring; can be substituted with at least one group; it is selected from by phenyl; halogen atom; halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed]; benzoyl is [wherein on this benzyl ring; can be substituted with at least one group; it is selected from by halogen atom; halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed]; pyridyl C1-C6 alkyl; the C3-C8 cycloalkyl; phenyl C1-C6 alkyl is [wherein on this benzyl ring; can be substituted with at least one group; it is selected from the alkylene dioxo base by C1-C4; halogen atom; halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed]; piperidyl C1-C6 alkyl; piperidyl; phenyl C1-C6 alkoxyl group is [wherein on this benzyl ring; can be substituted with at least one group; it is selected from by halogen atom; halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed]; phenoxy group is [wherein on this benzyl ring; can be substituted with at least one group; it is selected from by halogen atom; halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed]; amino (wherein can be substituted with at least one group as substituting group; it is selected from by phenyl [wherein on this benzyl ring; can be substituted with at least one group; it is selected from by halogen atom; halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed]; C1-C6 alkyl and phenyl C1-C6 alkyl are [wherein on this benzyl ring; can be substituted with at least one group; it is selected from by halogen atom; halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group] group formed); benzo _ azoles base; phenyl C2-C6 thiazolinyl is (wherein on this benzyl ring; can be substituted with at least one group, it is selected from by halogen atom; halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed) and benzimidazolyl-.As this class substituting group; can be substituted with 1 to 3 group that is selected from following groups; they each naturally as mentioned or hereinafter described: halogen atom; halogen replaces or unsubstituted C1-C6 alkyl; halogen replaces or unsubstituted C1-C6 alkoxyl group; phenyl is [wherein on this benzyl ring; can be substituted with 1 to 5; preferred 1 to 3 group; it is selected from by phenyl; halogen atom; halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed]; benzoyl is [wherein on this benzyl ring; can be substituted with 1 to 5; preferred 1 to 3 group; it is selected from by halogen atom; halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed]; pyridyl C1-C6 alkyl; the C3-C8 cycloalkyl; phenyl C1-C6 alkyl is [wherein on this benzyl ring; can be substituted with 1 to 5; preferred 1 to 3 group; it is selected from the alkylene dioxo base by C1-C4; halogen atom; halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed; substituting group is under the situation of C1-C4 alkylene dioxo base therein; preferably be substituted with 1 or 2 group]; piperidyl C1-C6 alkyl; piperidyl; phenyl C1-C6 alkoxyl group is [wherein on this benzyl ring; can be substituted with 1 to 5; preferred 1 to 3 group; it is selected from by halogen atom; halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed]; phenoxy group is [wherein on this benzyl ring; can be substituted with 1 to 5; preferred 1 to 3 group; it is selected from by halogen atom; halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed]; it is amino that (wherein can be substituted with 1 or 2 and be selected from following group as substituting group: phenyl is [wherein on this benzyl ring; can be substituted with 1 to 5; preferred 1 to 3 group; it is selected from by halogen atom; halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed]; C1-C6 alkyl and phenyl C1-C6 alkyl are [wherein on this benzyl ring; can be substituted with 1 to 5; preferred 1 to 3 group; it is selected from by halogen atom; halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group] group formed); benzo _ azoles base; phenyl C2-C6 thiazolinyl is (wherein on this benzyl ring; can be substituted with 1 to 5; preferred 1 to 3 group, it is selected from by halogen atom; halogen replaces or the unsubstituted straight or branched alkyl of 1 to 6 carbon atom and the group that halogen replaces or the unsubstituted straight or branched alkoxyl group that contains 1 to 6 carbon atom is formed of containing) and benzimidazolyl-.

R ^11BAnd R ^12BCan directly or by nitrogen, oxygen or sulphur atom be bonded to each other, constitute the first saturated heterocyclic of above-mentioned 5-7 with their adjacent nitrogen-atoms.On this 5-7 unit saturated heterocyclic, can be substituted with at least one group, it is selected from by C1-C6 alkoxy carbonyl and amino [wherein on this amino, can be substituted with at least one group, it is selected from by phenyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group) and the group formed of C1-C6 alkyl] group formed.Substituent example can be to be selected from by C1-C6 alkoxy carbonyl and amino [wherein on this amino, can be substituted with 1 or 2 group, it is selected from by phenyl (wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group) and the group formed of C1-C6 alkyl] group of the group formed, they are as mentioned or hereinafter described.On this heterocycle, can be substituted with 1 to 3 such substituting group.

The term phenyl is [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by phenyl, halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group] be used to represent unsubstituted phenyl or phenyl as defined above in this article, it comprises 1 to 5 substituting group, preferred 1 to 3 substituting group, described substituting group are selected from by phenyl, halogen atom, halogen and replace or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group.The example of phenyl can comprise phenyl, the 2-phenyl, the 3-phenyl, the 4-phenyl, 2,3-phenylbenzene phenyl, 2,4,6-triphenyl phenyl, the 2-fluorophenyl, the 3-fluorophenyl, the 4-fluorophenyl, the 2-chloro-phenyl-, the 3-chloro-phenyl-, the 4-chloro-phenyl-, the 2-bromophenyl, the 3-bromophenyl, the 4-bromophenyl, the 2-iodophenyl, the 3-iodophenyl, the 4-iodophenyl, 2, the 3-difluorophenyl, 3, the 4-difluorophenyl, 3, the 5-difluorophenyl, 2, the 4-difluorophenyl, 2, the 6-difluorophenyl, 2, the 3-dichlorophenyl, 3, the 4-dichlorophenyl, 3, the 5-dichlorophenyl, 2, the 4-dichlorophenyl, 2, the 6-dichlorophenyl, 3,4, the 5-trifluorophenyl, 3,4, the 5-trichlorophenyl, 2,4, the 6-trifluorophenyl, 2,4, the 6-trichlorophenyl, 2-fluoro-4-bromophenyl, 4-chloro-3-fluorophenyl, 2,3, the 4-trichlorophenyl, 3,4, the 5-trifluorophenyl, 2,3,4,5, the 6-pentafluorophenyl group, 2,4, the 6-trimethylphenyl, the 4-n-butylphenyl, 2, the 4-3,5-dimethylphenyl, 2, the 3-3,5-dimethylphenyl, 2, the 6-3,5-dimethylphenyl, 3, the 5-3,5-dimethylphenyl, 2, the 5-3,5-dimethylphenyl, 3,5-two trifluoromethyls, 4-n-butoxy phenyl, 2, the 4-Dimethoxyphenyl, 2, the 3-Dimethoxyphenyl, 2, the 6-Dimethoxyphenyl, 3, the 5-Dimethoxyphenyl, 2, the 5-Dimethoxyphenyl, 2,4, the 6-trimethoxyphenyl, 3,5-two Trifluoromethoxyphen-ls, 3-chloro-4-p-methoxy-phenyl, 2-chloro-4-Trifluoromethoxyphen-l, 3-methyl-4-fluorophenyl, 4-bromo-3-trifluoromethyl, the 2-aminomethyl phenyl, the 3-aminomethyl phenyl, the 4-aminomethyl phenyl, 2-methyl-3-chloro-phenyl-, 3-methyl-4-chloro-phenyl-, 2-chloro-4-aminomethyl phenyl, 2-methyl-3-fluorophenyl, the 2-trifluoromethyl, the 3-trifluoromethyl, the 4-trifluoromethyl, 2-pentafluoroethyl group phenyl, 3-pentafluoroethyl group phenyl, 4-pentafluoroethyl group phenyl, the 2-isopropyl phenyl, the 3-isopropyl phenyl, the 4-isopropyl phenyl, the 2-tert-butyl-phenyl, the 3-tert-butyl-phenyl, the 4-tert-butyl-phenyl, the 2-secondary butyl phenenyl, the 3-secondary butyl phenenyl, the 4-secondary butyl phenenyl, 2-is the fluoropropyl phenyl just-seven, 3-is the fluoropropyl phenyl just-seven, 4-is the fluoropropyl phenyl just-seven, 4-n-pentyl phenyl, 4-n-hexyl phenyl, the 2-p-methoxy-phenyl, the 3-p-methoxy-phenyl, the 4-p-methoxy-phenyl, 3-chloro-2-p-methoxy-phenyl, 2-fluoro-3-p-methoxy-phenyl, 2-fluoro-4-p-methoxy-phenyl, 2, the 6-Dimethoxyphenyl, 2,3, the 4-trifluorophenyl, 2,4, the 6-trifluorophenyl, the 2-Trifluoromethoxyphen-l, the 3-Trifluoromethoxyphen-l, the 4-Trifluoromethoxyphen-l, 3-fluoro-2-Trifluoromethoxyphen-l, 2-fluoro-3-Trifluoromethoxyphen-l, 3-fluoro-4-Trifluoromethoxyphen-l, 3-chloro-2-Trifluoromethoxyphen-l, 2-chloro-3-Trifluoromethoxyphen-l, 3-chloro-4-Trifluoromethoxyphen-l, 2-five fluorine ethoxyl phenenyls, 3-five fluorine ethoxyl phenenyls, 4-five fluorine ethoxyl phenenyls, 3-chloro-2-five fluorine ethoxyl phenenyls, 2-chloro-3-five fluorine ethoxyl phenenyls, 3-chloro-4-five fluorine ethoxyl phenenyls, the 2-isopropyl phenyl, the 3-isopropyl phenyl, the 4-isopropyl phenyl, 2-tert.-butoxy phenyl, 3-tert.-butoxy phenyl, 4-tert.-butoxy phenyl, 2-sec-butoxy phenyl, 3-sec-butoxy phenyl, 4-sec-butoxy phenyl, 2-is fluorine propoxy-phenyl just-seven, 3-is fluorine propoxy-phenyl just-seven, 4-is fluorine propoxy-phenyl just-seven, the positive hexyloxy phenyl of 4-n-pentyloxy phenyl and 4-.

Term phenyl C1-C6 alkoxyl group is [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group] be used to represent phenyl C1-C6 alkoxyl group as defined above in this article, wherein can be substituted with 1 to 5, preferred 1 to 3 group, described group is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group.The example of phenyl C1-C6 alkoxyl group can comprise benzyloxy, the 2-phenyl ethoxy, 3-phenyl propoxy-, 2-phenyl propoxy-, 4-phenyl butoxy, 5-phenyl pentyloxy, 4-phenyl pentyloxy, 6-phenyl hexyloxy, 2-fluorine benzyloxy, 3-fluorine benzyloxy, 4-fluorine benzyloxy, 2-(2-fluorophenyl) oxyethyl group, 2-(3-fluorophenyl) oxyethyl group, 2-(4-fluorophenyl) oxyethyl group, 2-chlorine benzyloxy, 3-chlorine benzyloxy, 4-chlorine benzyloxy, 2-fluoro-4-bromo-benzyloxy-, 4-chloro-3-fluorine benzyloxy, 2-chloro-4-fluorine benzyloxy, 3, the 4-dichloro-benzyloxy, 3, the 5-dichloro-benzyloxy, 2, the 3-dichloro-benzyloxy, 2, the 5-dichloro-benzyloxy, 2,3,4-trichlorine benzyloxy, 3,4,5-trifluoromethyl benzyl oxy base, 2,3,4,5,6-five fluorine benzyloxies, 2,4,6-trichlorine benzyloxy, the 4-isopropyl benzyloxy, 4-normal-butyl benzyloxy, 4-methyl benzyloxy, 2-methyl benzyloxy, 3-methyl benzyloxy, 2, the 4-benzyloxy-dimethyl, 2, the 3-benzyloxy-dimethyl, 2, the 6-benzyloxy-dimethyl, 3, the 5-benzyloxy-dimethyl, 2, the 5-benzyloxy-dimethyl, 2,4,6-trimethylammonium benzyloxy, 4-ethyl benzyloxy, the 4-isopropyl benzyloxy, 3,5-two trifluoromethyl benzyloxies, 4-isopropoxy benzyloxy, 4-n-butoxy benzyloxy, 4-methoxyl group benzyloxy base, 2-methoxyl group benzyloxy base, 3-methoxyl group benzyloxy base, 2,4-dimethoxy benzyloxy, 2,3-dimethoxy benzyloxy, 2,6-dimethoxy benzyloxy, 3,5-dimethoxy benzyloxy, 2,5-dimethoxy benzyloxy, 2,4,6-trimethoxy benzyloxy, 3,5-two trifluoromethoxy benzyloxies, 2-isopropoxy benzyloxy, 3-chloro-4-methoxyl group benzyloxy base, 2-chloro-4-trifluoromethoxy benzyloxy, 3-methyl-4-fluorine benzyloxy, 4-bromo-3-trifluoromethyl benzyloxy, 2-(2-chloro-phenyl-) oxyethyl group, 2-(3-chloro-phenyl-) oxyethyl group, 2-(4-chloro-phenyl-) oxyethyl group, the 2-trifluoromethyl benzyloxy, the 3-trifluoromethyl benzyloxy, the 4-trifluoromethyl benzyloxy, 2-trifluoromethoxy benzyloxy, 3-trifluoromethoxy benzyloxy, 4-trifluoromethoxy benzyloxy, 2-(2-trifluoromethyl) oxyethyl group, 2-(3-trifluoromethyl) oxyethyl group, 2-(4-trifluoromethyl) oxyethyl group, 2-(2-Trifluoromethoxyphen-l) oxyethyl group, 2-(3-Trifluoromethoxyphen-l) oxyethyl group, 2-(4-Trifluoromethoxyphen-l) oxyethyl group, 3-(2-trifluoromethyl) propoxy-, 3-(3-trifluoromethyl) propoxy-, 3-(4-trifluoromethyl) propoxy-, 3-(2-trifluoromethyl) propoxy-, 3-(3-Trifluoromethoxyphen-l) propoxy-, 3-(4-Trifluoromethoxyphen-l) propoxy-, 4-(3-trifluoromethyl) butoxy, 5-(4-trifluoromethyl) pentyloxy, 4-(4-trifluoromethyl) pentyloxy, 4-(4-Trifluoromethoxyphen-l) pentyloxy, 6-(3-trifluoromethyl) hexyloxy, 6-(4-trifluoromethyl) hexyloxy and 6-(4-Trifluoromethoxyphen-l) hexyloxy.

The term phenoxy group is [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group] be used to represent unsubstituted phenoxy or phenoxy group as defined above in this article, it comprises 1 to 5 substituting group, preferred 1 to 3 substituting group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group.The example of phenoxy group can comprise phenoxy group, the 2-fluorophenoxy, the 3-fluorophenoxy, the 4-fluorophenoxy, the 2-chlorophenoxy, the 3-chlorophenoxy, the 4-chlorophenoxy, 2-bromine phenoxy group, 3-bromine phenoxy group, 4-bromine phenoxy group, 2-iodine phenoxy group, 3-iodine phenoxy group, 4-iodine phenoxy group, 2,3-two fluorophenoxies, 3,4-two fluorophenoxies, 3,5-two fluorophenoxies, 2,4-two fluorophenoxies, 2,6-two fluorophenoxies, 2, the 3-dichlorophenoxy, 3, the 4-dichlorophenoxy, 3, the 5-dichlorophenoxy, 2, the 4-dichlorophenoxy, 2, the 6-dichlorophenoxy, 3,4,5-trifluoromethoxy phenoxy base, 3,4, the 5-Trichlorophenoxy, 2,4,6-trifluoromethoxy phenoxy base, 2,4, the 6-Trichlorophenoxy, 2-fluoro-4-bromine phenoxy group, 4-chloro-3-fluorophenoxy, 2,3, the 4-Trichlorophenoxy, 3,4,5-trifluoromethoxy phenoxy base, 2,3,4,5,6-penta fluoro benzene oxygen base, 2,4,6-trimethylammonium phenoxy group, 4-normal-butyl phenoxy group, 2, the 4-dimethyl phenoxy, 2, the 3-dimethyl phenoxy, 2, the 6-dimethyl phenoxy, 3, the 5-dimethyl phenoxy, 2, the 5-dimethyl phenoxy, 3,5-two 4-trifluoromethylphenopendants, 4-n-butoxy phenoxy group, 2,4-dimethoxy phenoxy group, 2,3-dimethoxy phenoxy group, 2,6-dimethoxy phenoxy group, 3,5-dimethoxy phenoxy group, 2,5-dimethoxy phenoxy group, 2,4,6-trimethoxy phenoxy group, 3,5-two Trifluoromethyl phenyl ether oxygen bases, 3-chloro-4-methoxyl group phenoxy group, 2-chloro-4-Trifluoromethyl phenyl ether oxygen base, 3-methyl-4-fluorophenoxy, 4-bromo-3-4-trifluoromethylphenopendant, the 2-methylphenoxy, the 3-methylphenoxy, the 4-methylphenoxy, 2-methyl-3-chlorophenoxy, 3-methyl-4-chlorophenoxy, 2-chloro-4-methylphenoxy, 2-methyl-3-fluorophenoxy, the 2-4-trifluoromethylphenopendant, the 3-4-trifluoromethylphenopendant, the 4-4-trifluoromethylphenopendant, 2-pentafluoroethyl group phenoxy group, 3-pentafluoroethyl group phenoxy group, 4-pentafluoroethyl group phenoxy group, 2-sec.-propyl phenoxy group, 3-sec.-propyl phenoxy group, 4-sec.-propyl phenoxy group, 2-tertiary butyl phenoxy group, 3-tertiary butyl phenoxy group, 4-tertiary butyl phenoxy group, 2-sec-butyl phenoxy group, 3-sec-butyl phenoxy group, 4-sec-butyl phenoxy group, 2-is the fluoropropyl phenoxy group just-seven, 3-is the fluoropropyl phenoxy group just-seven, 4-is the fluoropropyl phenoxy group just-seven, 4-n-pentyl phenoxy group, 4-n-hexyl phenoxy group, 2-methoxyl group phenoxy group, 3-methoxyl group phenoxy group, 4-methoxyl group phenoxy group, 3-chloro-2-methoxyl group phenoxy group, 2-fluoro-3-methoxyl group phenoxy group, 2-fluoro-4-methoxyl group phenoxy group, 2,6-dimethoxy phenoxy group, 2,3,4-trifluoromethoxy phenoxy base, 2,4,6-trifluoromethoxy phenoxy base, 2-Trifluoromethyl phenyl ether oxygen base, 3-Trifluoromethyl phenyl ether oxygen base, 4-Trifluoromethyl phenyl ether oxygen base, 3-fluoro-2-Trifluoromethyl phenyl ether oxygen base, 2-fluoro-3-Trifluoromethyl phenyl ether oxygen base, 3-fluoro-4-Trifluoromethyl phenyl ether oxygen base, 3-chloro-2-Trifluoromethyl phenyl ether oxygen base, 2-chloro-3-Trifluoromethyl phenyl ether oxygen base, 3-chloro-4-Trifluoromethyl phenyl ether oxygen base, 2-five fluorine ethoxy phenoxies, 3-five fluorine ethoxy phenoxies, 4-five fluorine ethoxy phenoxies, 3-chloro-2-five fluorine ethoxy phenoxies, 2-chloro-3-five fluorine ethoxy phenoxies, 3-chloro-4-five fluorine ethoxy phenoxies, 2-isopropoxy phenoxy group, 3-isopropoxy phenoxy group, 4-isopropoxy phenoxy group, 2-tert.-butoxy phenoxy group, 3-tert.-butoxy phenoxy group, 4-tert.-butoxy phenoxy group, 2-sec-butoxy phenoxy group, 3-sec-butoxy phenoxy group, 4-sec-butoxy phenoxy group, 2-is fluorine propoxy-phenoxy group just-seven, 3-is fluorine propoxy-phenoxy group just-seven, 4-is fluorine propoxy-phenoxy group just-seven, the positive hexyloxy phenoxy group of 4-n-pentyloxy phenoxy group and 4-.

Term phenyl C1-C6 alkyl is [wherein on this benzyl ring, can be substituted with at least one group, it is selected from the alkylene dioxo base by C1-C4, halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group] be used to represent unsubstituted phenyl C1-C6 alkyl or such group in this article, wherein on the benzyl ring that constitutes this group, can be substituted with 1 to 5, preferred 1 to 3 is selected from following group: the C1-C4 alkylene dioxo base, halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed, its condition is when substituting group is the C1-C4 alkylene dioxo base, preferably is substituted with 1 to 2 substituting group.The example of phenyl C1-C6 alkyl can comprise benzyl, the 1-styroyl, the 2-styroyl, the 3-phenyl propyl, the 2-phenyl propyl, the 4-phenyl butyl, the 5-phenylpentyl, the 4-phenylpentyl, 6-phenyl hexyl, 2, the 3-methylenedioxy benzyl, 3, the 4-methylenedioxy benzyl, the 2-luorobenzyl, the 3-luorobenzyl, the 4-luorobenzyl, 2-benzyl chloride base, 3-benzyl chloride base, 4-benzyl chloride base, the 2-bromobenzyl, the 3-bromobenzyl, the 4-bromobenzyl, 2-iodine benzyl, 3-iodine benzyl, 4-iodine benzyl, 2, the 3-difluorobenzyl, 3, the 4-difluorobenzyl, 3, the 5-difluorobenzyl, 2, the 4-difluorobenzyl, 2, the 6-difluorobenzyl, 2, the 3-dichloro benzyl, 3, the 4-dichloro benzyl, 3, the 5-dichloro benzyl, 2, the 4-dichloro benzyl, 2, the 6-dichloro benzyl, 2-fluoro-4-bromobenzyl, 4-chloro-3-luorobenzyl, 2,3,4-trichlorine benzyl, 3,4, the 5-trifluoro-benzyl, 2,4,6-trichlorine benzyl, the 4-isopropyl benzyl, 4-normal-butyl benzyl, the 4-methyl-benzyl, the 2-methyl-benzyl, the 3-methyl-benzyl, 2, the 4-dimethyl benzyl, 2, the 3-dimethyl benzyl, 2, the 6-dimethyl benzyl, 3, the 5-dimethyl benzyl, 2, the 5-dimethyl benzyl, 2,4, the 6-trimethyl benzyl, 3,5-two trifluoromethyl benzyls, 2,3,4,5, the 6-PFBBR, the 4-isopropoxide benzyl, 4-n-butoxy benzyl, the 4-methoxy-benzyl, the 2-methoxy-benzyl, the 3-methoxy-benzyl, 2, the 4-dimethoxy-benzyl, 2, the 3-dimethoxy-benzyl, 2, the 6-dimethoxy-benzyl, 3, the 5-dimethoxy-benzyl, 2, the 5-dimethoxy-benzyl, 2,4,6-trimethoxy benzyl, 3,5-two trifluoro-methoxybenzyls, the 2-isopropoxide benzyl, 3-chloro-4-methoxy-benzyl, 2-chloro-4-trifluoro-methoxybenzyl, 3-methyl-4-luorobenzyl, 4-bromo-3-trifluoromethyl benzyl, the 2-trifluoromethyl benzyl, the 3-trifluoromethyl benzyl, the 4-trifluoromethyl benzyl, 2-pentafluoroethyl group benzyl, 3-pentafluoroethyl group benzyl, 4-pentafluoroethyl group benzyl, the 2-trifluoro-methoxybenzyl, the 3-trifluoro-methoxybenzyl, the 4-trifluoro-methoxybenzyl, 2-five fluorine ethoxy benzyls, 3-five fluorine ethoxy benzyls, 4-five fluorine ethoxy benzyls, 2-(2-trifluoromethyl) ethyl, 2-(3-trifluoromethyl) ethyl, 2-(4-trifluoromethyl) ethyl, 2-(2-Trifluoromethoxyphen-l) ethyl, 2-(3-Trifluoromethoxyphen-l) ethyl, 2-(4-Trifluoromethoxyphen-l) ethyl, 2-(2-five fluorine ethoxyl phenenyls) ethyl, 2-(3-five fluorine ethoxyl phenenyls) ethyl, 2-(4-five fluorine ethoxyl phenenyls) ethyl, 3-(2-trifluoromethyl) propyl group, 3-(3-trifluoromethyl) propyl group, 3-(4-trifluoromethyl) propyl group, 3-(2-Trifluoromethoxyphen-l) propyl group, 3-(3-Trifluoromethoxyphen-l) propyl group, 3-(4-trifluoromethyl) propyl group, 3-(3-five fluorine ethoxyl phenenyls) propyl group, 3-(4-five fluorine ethoxyl phenenyls) propyl group, 4-(3-five fluorine ethoxyl phenenyls) butyl, 5-(4-trifluoromethyl) amyl group, 4-(4-trifluoromethyl) amyl group, 4-(4-Trifluoromethoxyphen-l) amyl group, 6-(3-trifluoromethyl) hexyl, 6-(4-trifluoromethyl) hexyl and 6-(4-Trifluoromethoxyphen-l) hexyl.

The example of piperidyl C1-C6 alkyl can comprise piperidines-1-ylmethyl, piperidines-2-base ethyl, piperidines-3-base propyl group, piperidin-4-yl butyl, piperidines-1-base amyl group and piperidines-2-base hexyl.

It is amino that (wherein can be substituted with at least one and be selected from down group of organizing as substituting group: phenyl is [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed], C1-C6 alkyl and phenyl C1-C6 alkyl are [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group] group formed) can be that amino (wherein can be substituted with 1 or 2 and be selected from following group as substituting group: phenyl is [wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed], C1-C6 alkyl and phenyl C1-C6 alkyl are [wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 group, it is selected from by halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group] group formed).Amino example can comprise amino, methylamino, dimethylamino, ethylamino, diethylamino, n-propyl amino, normal-butyl amino, n-pentyl amino, n-hexyl amino, phenyl amino, (4-chloro-phenyl-) amino, (4-bromophenyl) amino, (2, the 4-dichlorophenyl) amino, (2,4, the 6-trichlorophenyl) amino, (2,3,4,5, the 6-pentafluorophenyl group) amino, (4-fluorophenyl) amino, (4-iodophenyl) amino, (4-chloro-phenyl-) amino, (3-aminomethyl phenyl) amino, (2-trifluoromethyl) amino, (3-trifluoromethyl) amino, (4-trifluoromethyl) amino, (3, the 4-3,5-dimethylphenyl) amino, (3,4, the 5-trimethylphenyl) amino, (2-p-methoxy-phenyl) amino, (4-Trifluoromethoxyphen-l) amino, (3-Trifluoromethoxyphen-l) amino, (3, the 5-Dimethoxyphenyl) amino, (2, the 5-Dimethoxyphenyl) amino, (2,4, the 6-trimethoxyphenyl) amino, N-methyl-N-(4-trifluoromethyl) amino, N-ethyl-N-(4-Trifluoromethoxyphen-l) amino, 1-styroyl amino, 2-styroyl amino, 3-phenyl propyl amino, 2-phenyl propyl amino, 4-phenyl butyl amino, 5-phenylpentyl amino, 4-phenylpentyl amino, 6-phenyl hexyl amino, 2-luorobenzyl amino, 3-luorobenzyl amino, N-phenyl-N-(4-luorobenzyl) amino, 2-benzyl chloride base amino, 3-benzyl chloride base amino, 4-benzyl chloride base amino, 2-bromobenzyl amino, N-methyl-N-(3-bromobenzyl) amino, 4-bromobenzyl amino, 2-iodine benzylamino, 3-iodine benzylamino, 4-iodine benzylamino, 2,3-difluorobenzyl amino, 3,4-difluorobenzyl amino, 3,5-difluorobenzyl amino, 2,4-difluorobenzyl amino, 2,6-difluorobenzyl amino, 2,3-dichloro benzyl amino, 3,4-dichloro benzyl amino, 3,5-dichloro benzyl amino, 2,4-dichloro benzyl amino, 2,6-dichloro benzyl amino, 2-fluoro-4-bromobenzyl amino, 4-chloro-3-luorobenzyl amino, 2,3,4-trichlorine benzylamino, 3,4,5-trifluoro-benzyl amino, 2,4,6-trichlorine benzylamino, 4-isopropyl benzyl amino, 4-normal-butyl benzylamino, 4-methyl-benzyl amino, 2-methyl-benzyl amino, 3-methyl-benzyl amino, 2,4-dimethyl benzyl amino, 2,3-dimethyl benzyl amino, 2,6-dimethyl benzyl amino, 3,5-dimethyl benzyl amino, 2,5-dimethyl benzyl amino, 2,4,6-trimethyl benzyl amino, 3,5-two trifluoromethyl benzyl amino, 2,3,4,5,6-PFBBR amino, 4-isopropoxide benzyl amino, 4-n-butoxy benzylamino, 4-methoxy-benzyl amino, 2-methoxy-benzyl amino, 3-methoxy-benzyl amino, 2,4-dimethoxy-benzyl amino, 2, the 3-dimethoxy-benzyl, 2,6-dimethoxy-benzyl amino, 3,5-dimethoxy-benzyl amino, 2,5-dimethoxy-benzyl amino, 2,4,6-trimethoxy benzylamino, 3,5-two trifluoro-methoxybenzyl amino, 2-isopropoxide benzyl amino, 3-chloro-4-methoxy-benzyl amino, 2-chloro-4-trifluoro-methoxybenzyl amino, 3-methyl-4-luorobenzyl amino, 4-bromo-3-trifluoromethyl benzyl amino, 2-trifluoromethyl benzyl amino, 3-trifluoromethyl benzyl amino, 4-trifluoromethyl benzyl amino, 2-pentafluoroethyl group benzylamino, 3-pentafluoroethyl group benzylamino, 4-pentafluoroethyl group benzylamino, 2-trifluoro-methoxybenzyl amino, 3-trifluoro-methoxybenzyl amino, 4-trifluoro-methoxybenzyl amino, 2-five fluorine ethoxy benzyl amino, 3-five fluorine ethoxy benzyl amino, 4-five fluorine ethoxy benzyl amino, 2-(2-trifluoromethyl) ethylamino, 2-(3-trifluoromethyl) ethylamino, 2-(4-trifluoromethyl) ethylamino, 2-(2-Trifluoromethoxyphen-l) ethylamino, 2-(3-Trifluoromethoxyphen-l) ethylamino, 2-(4-Trifluoromethoxyphen-l) ethylamino, 2-(2-five fluorine ethoxyl phenenyls) ethylamino, 2-(3-five fluorine ethoxyl phenenyls) ethylamino, 2-(4-five fluorine ethoxyl phenenyls) ethylamino, 3-(2-trifluoromethyl) propyl group amino, 3-(3-trifluoromethyl) propyl group amino, 3-(4-trifluoromethyl) propyl group amino, 3-(2-Trifluoromethoxyphen-l) propyl group amino, 3-(3-Trifluoromethoxyphen-l) propyl group amino, 3-(4-Trifluoromethoxyphen-l) propyl group amino, 3-(3-five fluorine ethoxyl phenenyls) propyl group amino, 3-(4-five fluorine ethoxyl phenenyls) propyl group amino, 4-(3-five fluorine ethoxyl phenenyls) butyl amino, 5-(4-trifluoromethyl) amyl group amino, 4-(4-trifluoromethyl) amyl group amino, 4-(4-Trifluoromethoxyphen-l) amyl group amino, 6-(3-trifluoromethyl) hexyl amino, 6-(4-trifluoromethyl) hexyl amino, 6-(4-Trifluoromethoxyphen-l) hexyl amino, N-methyl-N-phenyl amino, N-methyl-N-benzylamino and N-phenyl-N-benzylamino.

Carbamoyloxy group is (wherein on this amino, can be substituted with at least one is selected from by C1-C6 alkyl and phenyl [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group] group of the group of composition) example can comprise carbamoyloxy group, carbamoyloxy group for example, the phenylamino methanoyl, 2-fluorophenyl carbamoyloxy group, 3-fluorophenyl carbamoyloxy group, 4-fluorophenyl carbamoyloxy group, 2-chloro-phenyl-carbamoyloxy group, 3-chloro-phenyl-carbamoyloxy group, 4-chloro-phenyl-carbamoyloxy group, 2-bromophenyl carbamoyloxy group, 3-bromophenyl carbamoyloxy group, 4-bromophenyl carbamoyloxy group, 2-iodophenyl carbamoyloxy group, 3-iodophenyl carbamoyloxy group, 4-iodophenyl carbamoyloxy group, 2,3-difluorophenyl carbamoyloxy group, 3,4-difluorophenyl carbamoyloxy group, 3,5-difluorophenyl carbamoyloxy group, 2,4-difluorophenyl carbamoyloxy group, 2,6-difluorophenyl carbamoyloxy group, 2,3-dichlorophenyl carbamoyloxy group, 3,4-dichlorophenyl carbamoyloxy group, 3,5-dichlorophenyl carbamoyloxy group, 2,4-dichlorophenyl carbamoyloxy group, 2,6-dichlorophenyl carbamoyloxy group, 3,4,5-trifluorophenyl carbamoyloxy group, 2,3,4,5,6-pentafluorophenyl group carbamoyloxy group, 3,4,5-trichlorophenyl carbamoyloxy group, 2,4,6-trifluorophenyl carbamoyloxy group, 2,4,6-trichlorophenyl carbamoyloxy group, 2-aminomethyl phenyl carbamoyloxy group, 3-aminomethyl phenyl carbamoyloxy group, 4-aminomethyl phenyl carbamoyloxy group, 2-methyl-3-chloro-phenyl-carbamoyloxy group, 3-methyl-4-chloro-phenyl-carbamoyloxy group, 2-chloro-4-aminomethyl phenyl carbamoyloxy group, 2-methyl-3-fluorophenyl carbamoyloxy group, 2-trifluoromethyl carbamoyloxy group, 3-trifluoromethyl carbamoyloxy group, the methyl carbamoyloxy group, the ethyl carbamoyloxy group, the n-propyl carbamoyloxy group, the normal-butyl carbamoyloxy group, the n-hexyl carbamoyloxy group, the n-pentyl carbamoyloxy group, N-methyl-N-phenylamino methanoyl, N, N-dimethylamino methanoyl, N-methyl-N-ethyl carbamoyloxy group, N-(2-fluorophenyl)-N-methyl carbamoyloxy group, N-(3-fluorophenyl)-N-methyl carbamoyloxy group, N-(4-fluorophenyl)-N-methyl carbamoyloxy group, N-(2-chloro-phenyl-)-N-methyl carbamoyloxy group, N-(3-chloro-phenyl-)-N-methyl carbamoyloxy group, N-(4-chloro-phenyl-)-N-methyl carbamoyloxy group, N-(4-bromophenyl)-N-methyl carbamoyloxy group, N-(2-iodophenyl)-N-methyl carbamoyloxy group, N-(3-iodophenyl)-N-methyl carbamoyloxy group, N-(4-iodophenyl)-N-methyl carbamoyloxy group, N-(2, the 3-difluorophenyl)-N-methyl carbamoyloxy group, N-(3, the 4-difluorophenyl)-N-methyl carbamoyloxy group, N-(3, the 5-difluorophenyl)-N-methyl carbamoyloxy group, N-(2, the 4-difluorophenyl)-N-methyl carbamoyloxy group, N-(2, the 6-difluorophenyl)-N-methyl carbamoyloxy group, N-(2, the 3-dichlorophenyl)-N-methyl carbamoyloxy group, N-(3, the 4-dichlorophenyl)-N-methyl carbamoyloxy group, N-(3, the 5-dichlorophenyl)-N-methyl carbamoyloxy group, N-(2,4 dichloro benzene base)-N-methyl carbamoyloxy group, N-(2, the 6-dichlorophenyl)-N-methyl carbamoyloxy group, N-(3,4, the 5-trifluorophenyl)-N-methyl carbamoyloxy group, N-(3,4, the 5-trichlorophenyl)-N-methyl carbamoyloxy group, N-(2,4, the 6-trifluorophenyl)-N-methyl carbamoyloxy group, N-(2,4, the 6-trichlorophenyl)-N-methyl carbamoyloxy group, N-(2-aminomethyl phenyl)-N-methyl carbamoyloxy group, N-(3-aminomethyl phenyl)-N-methyl carbamoyloxy group, N-(4-aminomethyl phenyl)-N-methyl carbamoyloxy group, N-(2-methyl-3-chloro-phenyl-)-N-methyl carbamoyloxy group, N-(3-methyl-4-chloro-phenyl-)-N-methyl carbamoyloxy group, N-(2-chloro-4-aminomethyl phenyl)-N-methyl carbamoyloxy group, N-(2-methyl-3-fluorophenyl)-N-methyl carbamoyloxy group, N-(2-trifluoromethyl)-N-methyl carbamoyloxy group, N-(4-trifluoromethyl)-N-methyl carbamoyloxy group, N-phenyl-N-phenylamino methanoyl, N-phenyl-N-(2-fluorophenyl) carbamoyloxy group, N-phenyl-N-(3-fluorophenyl) carbamoyloxy group, N-phenyl-N-(4-fluorophenyl) carbamoyloxy group, N-phenyl-N-(2-chloro-phenyl-) carbamoyloxy group, N-phenyl-N-(3-chloro-phenyl-) carbamoyloxy group, N-phenyl-N-(4-chloro-phenyl-) carbamoyloxy group, N-phenyl-N-(2-bromophenyl) carbamoyloxy group, N-phenyl-N-(3-bromophenyl) carbamoyloxy group, N-phenyl-N-(4-bromophenyl) carbamoyloxy group, N-phenyl-N-(2-iodophenyl) carbamoyloxy group, N-phenyl-N-(3-iodophenyl) carbamoyloxy group, N-phenyl-N-(4-iodophenyl) carbamoyloxy group, N-phenyl-N-(2, the 3-difluorophenyl) carbamoyloxy group, N-phenyl-N-(3, the 4-difluorophenyl) carbamoyloxy group, N-phenyl-N-(3, the 5-difluorophenyl) carbamoyloxy group, N-phenyl-N-(2,4 difluorobenzene base) carbamoyloxy group, N-phenyl-N-(2, the 6-difluorophenyl) carbamoyloxy group, N-phenyl-N-(2, the 3-dichlorophenyl) carbamoyloxy group, N-phenyl-N-(3, the 4-dichlorophenyl) carbamoyloxy group, N-phenyl-N-(3, the 5-dichlorophenyl) carbamoyloxy group, N-phenyl-N-(2, the 4-dichlorophenyl) carbamoyloxy group, N-phenyl-N-(2, the 6-dichlorophenyl) carbamoyloxy group, N-phenyl-N-(3,4, the 5-trifluorophenyl) carbamoyloxy group, N-phenyl-N-(3,4, the 5-trichlorophenyl) carbamoyloxy group, N-phenyl-N-(2,4, the 6-trifluorophenyl) carbamoyloxy group, N-phenyl-N-(2,4, the 6-trichlorophenyl) carbamoyloxy group, N-phenyl-N-(2-aminomethyl phenyl) carbamoyloxy group, N-phenyl-N-(3-aminomethyl phenyl) carbamoyloxy group, N-phenyl-N-(4-aminomethyl phenyl) carbamoyloxy group, N-phenyl-N-(2-methyl-3-chloro-phenyl-) carbamoyloxy group, N-phenyl-N-(3-methyl-4-chloro-phenyl-) carbamoyloxy group, N-phenyl-N-(2-chloro-4-aminomethyl phenyl)-carbamoyloxy group, N-phenyl-N-(2-methyl-3-fluorophenyl) carbamoyloxy group, N-phenyl-N-(2-trifluoromethyl) carbamoyloxy group, N-phenyl-N-(3-trifluoromethyl) carbamoyloxy group, N-phenyl-N-(4-trifluoromethyl) carbamoyloxy group, 2-pentafluoroethyl group phenylamino methanoyl, 3-pentafluoroethyl group phenylamino methanoyl, 4-pentafluoroethyl group phenylamino methanoyl, 2-isopropyl phenyl carbamoyloxy group, 3-isopropyl phenyl carbamoyloxy group, 4-isopropyl phenyl carbamoyloxy group, 2-tert-butyl-phenyl carbamoyloxy group, 3-tert-butyl-phenyl carbamoyloxy group, 4-tert-butyl-phenyl carbamoyloxy group, 2-secondary butyl phenenyl carbamoyloxy group, 3-secondary butyl phenenyl carbamoyloxy group, 4-secondary butyl phenenyl carbamoyloxy group, 2-is fluoropropyl phenylamino methanoyl just-seven, 3-is fluoropropyl phenylamino methanoyl just-seven, 4-is fluoropropyl phenylamino methanoyl just-seven, 4-n-pentyl phenyl carbamoyloxy group, 4-n-hexyl phenyl carbamoyloxy group, 2,4-3,5-dimethylphenyl carbamoyloxy group, 2,4,6-trimethylphenyl carbamoyloxy group, 3,4-Dimethoxyphenyl carbamoyloxy group, 3,4,5-trimethoxyphenyl carbamoyloxy group, 2-p-methoxy-phenyl carbamoyloxy group, 3-p-methoxy-phenyl carbamoyloxy group, 4-p-methoxy-phenyl carbamoyloxy group, 2-methoxyl group-3-chloro-phenyl-carbamoyloxy group, 2-fluoro-3-p-methoxy-phenyl carbamoyloxy group, 2-fluoro-4-p-methoxy-phenyl carbamoyloxy group, 2,6-Dimethoxyphenyl carbamoyloxy group, 2,3,4-trifluorophenyl carbamoyloxy group, 3,4,5-trifluorophenyl carbamoyloxy group, 2-Trifluoromethoxyphen-l carbamoyloxy group, 3-Trifluoromethoxyphen-l carbamoyloxy group, 4-Trifluoromethoxyphen-l carbamoyloxy group, 2-five fluorine ethoxyl phenenyl carbamoyloxy groups, 3-five fluorine ethoxyl phenenyl carbamoyloxy groups, 4-five fluorine ethoxyl phenenyl carbamoyloxy groups, 2-isopropyl phenyl carbamoyloxy group, 3-isopropyl phenyl carbamoyloxy group, 4-isopropyl phenyl carbamoyloxy group, 2-tert.-butoxy phenylamino methanoyl, 3-tert.-butoxy phenylamino methanoyl, 4-tert.-butoxy phenylamino methanoyl, 2-sec-butoxy phenylamino methanoyl, 3-sec-butoxy phenylamino methanoyl, 4-sec-butoxy phenylamino methanoyl, 2-is fluorine propoxy-phenylamino methanoyl just-seven, 3-is fluorine propoxy-phenylamino methanoyl just-seven, 4-is fluorine propoxy-phenylamino methanoyl just-seven, (wherein on this amino, can be substituted with 1 or 2 and be selected from following group: C1-C6 alkyl and phenyl [wherein on this benzyl ring, can be substituted with 1 to 5 for 4-n-pentyloxy phenylamino methanoyl and the positive hexyloxy phenylamino of 4-methanoyl, preferred 1 to 3 is selected from following group: halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group] group formed).

Halogen replaces or the example of unsubstituted C1-C10 alkyl can comprise: above-mentioned halogen replaces or unsubstituted C1-C6 alkyl; The C1-C10 alkyl, for example heptyl, octyl group, nonyl, decyl, 7-fluorine heptyl, 7,7,6-trifluoro heptyl, 7,7,7,6,6,5,5-seven fluorine heptyl, 8-chlorine octyl group, 8,8-dibromo octyl group, 6,7,8-trifluoro octyl group, 8,8,8,7,7,6,6-seven fluorine octyl groups, 8,8,8,7,7-pentachloro-octyl group, 9-iodine nonyl, 9,9-dibromo nonyl, 9,9,9,8,8-pentachloro-nonyl, 9,9,9,8,8,7,7-seven fluorine nonyls, 10-chlorine decyl, 10,10-dibromo decyl, 10,10,10,9-tetrachloro decyl and 10,10,10,9,9,9,8,8-seven fluorine decyls; Wherein be substituted with the C1-C10 alkyl of 1 to 7 halogen atom.

Except above-mentioned phenyl (wherein on this benzyl ring; can be substituted with at least one group; it is selected from by halogen atom; halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed) in addition; phenyl is [wherein on this benzyl ring; can be substituted with at least one group; it is selected from the alkylene dioxo base by C1-C4; cyano group; phenoxy group; the C1-C6 alkylthio; the C1-C6 alkyloyl; phenyl; phenyl C1-C6 alkyl; halogen atom; halogen replaces or unsubstituted C1-C10 alkyl and halogen replaces or unsubstituted C1-C10 alkoxyl group is formed group] example may further include phenyl; 4-cyano-phenyl for example; the 3-cyano-phenyl; the 2-cyano-phenyl; 3; 4-dicyano phenyl; 3; 4; 5-tricyano phenyl; the 4-Phenoxyphenyl; the 3-Phenoxyphenyl; the 2-Phenoxyphenyl; 3; 4-two Phenoxyphenyls; 2; 4; 6-triple phenoxyl phenyl; 4-methylthio group phenyl; 3-methylthio group phenyl; 2-methylthio group phenyl; 3; 4-diformazan sulfenyl phenyl; 2; 4; 6-three methylthio group phenyl; the 4-acetylphenyl; the 3-acetylphenyl; the 2-acetylphenyl; 3; 4-diacetyl phenyl; 2; 4; 6-triacetyl phenyl; 4-biphenyl; 3-biphenyl; 2-biphenyl; 3; 4-phenylbenzene phenyl; 2; 4; 6-triphenyl phenyl; 4-oxygen in heptan base phenyl; the 3-octyloxyphenyl; 2-oxygen in ninth of the ten Heavenly Stems base phenyl; 4-oxygen in last of the ten Heavenly stems base phenyl; 2; 4-oxygen base in two heptan phenyl; 2; 4; 6-oxygen base in three heptan phenyl; 4-(7; 7-dichloro oxygen in heptan base) phenyl; the 4-benzyl phenyl; the 3-benzyl phenyl; the 2-benzyl phenyl; 2; 4-dibenzyl phenyl; 2; 4; 6-tribenzyl phenyl; the 4-octyl phenyl; 4-heptyl phenyl; the 3-octyl phenyl; 3-(8; 8; 8-trifluoro octyl group) phenyl; 2-nonyl phenyl; the 4-decyl phenyl; 2; 4-dioctyl phenyl; 2; 4; 6-trioctylphosphine phenylbenzene; 4-phenyl-3-chloro-phenyl-; 4-phenoxy group-3-methylthio group phenyl; 4-oxygen in heptan base-3-Trifluoromethoxyphen-l; 4-octyl group-2-trifluoromethyl; 4-benzyl-2-aminomethyl phenyl; 3; 4-ethylenedioxy phenyl and 3; the 4-methylenedioxyphenyl is [wherein on this benzyl ring; can be substituted with 1 to 5; preferred 1 to 3 group; it is selected from by above-mentioned C1-C4 alkylene dioxo base; cyano group; phenoxy group; above-mentioned C1-C6 alkylthio; above-mentioned C1-C6 alkyloyl; phenyl; above-mentioned phenyl C1-C6 alkyl; above-mentioned halogen atom; group (substituting group is under the situation of C1-C4 alkylenedioxy group therein, preferably is substituted with 1 or 2 group) that above-mentioned halogen replaces or unsubstituted C1-C6 alkyl and the replacement of above-mentioned halogen or that unsubstituted C1-C6 alkoxyl group is formed].

Carbamoyloxy substituted C1-C6 alkyl group (wherein the amino group can be substituted to At least one group which is selected from C1-C6 alkyl, phenyl C1-C6 alkyl, C3-C8 cycloalkyl group, Naphthyl group, a 2,3 - dihydro-1H-indenyl, 2,3 - dihydro-benzofuranyl, and phenyl [wherein the phenyl group The ring may be substituted with at least one group which is selected from C1-C4 alkylenedioxy group, a cyano group, Phenoxy, C1-C6 alkylthio, C1-C6 alkyl group, a phenyl group, a phenyl C1-C6 alkyl group, a halogen atom Son, halogen-substituted or unsubstituted C1-C10 alkyl and halogen-substituted or unsubstituted C1-C10 alkyl Group group consisting of] the group consisting of) may include a carbamoyloxy substituted C1-C6 alkoxy Group, for example, carbamoyloxy group, a 2 - carbamoyloxy group, 1 - carbamoyloxy group, a 3 - Carbamoyloxy propyl 4 - carbamoyl oxy group, a 5 - carbamoyloxy pentyl group, a 6 - carbamoyl oxygen Hexyl, phenyl carbamoyloxy group, a 2 - methyl-phenyl-carbamoyloxy methyl 3 - methyl-phenyl Carbamoyloxy group methyl 4 - methyl-phenyl carbamoyloxy group, 2,3 - dimethylphenyl carbamoyl Acyloxy group, 2,4 - dimethyl-phenyl carbamoyloxy group, 2,6 - dimethylphenyl carbamoyl Oxy methyl, 2,4,6 - trimethylphenyl bamoyloxy methyl 2 - (trifluoromethyl) phenyl carbamoyl Oxymethyl 3 - trifluoromethylphenyl carbamoyloxy methyl 4 - (trifluoromethyl) phenyl-carbamoyl oxygen Group, a 2,3 - bis (trifluoromethyl)-phenyl carbamoyloxy group, 2,4 - bis (trifluoromethyl) phenylamino Formyloxy group, 2,6 - bis (trifluoromethyl)-phenyl carbamoyloxy group, a 2 - phenyl pentafluoroethyl Carbamoyloxy methyl 3 - pentafluoroethyl carbamoyloxy phenyl methyl 4 - phenylcarbamoyl pentafluoroethyl Formyloxy group, 2 - (n-propyl-phenyl) carbamoyloxy group, 3 - (n-propyl-phenyl) carbamoyl Acyloxy group, 4 - (n-propyl-phenyl) carbamoyloxy group, 2 - (phenyl-carbamoyloxy) ethyl Group, 2 - (3 - (trifluoromethyl) phenyl carbamoyloxy) ethyl, 2 - (4 - trifluoromethyl-phenyl carbamoyl Oxy) ethyl, 2 - (2,3 - Bis (trifluoromethyl)-phenyl carbamoyloxy) ethyl, 2 - (2,4 - Bis (trifluoromethyl) Carbamoyloxy-methylphenyl) ethyl, 2 - (2,6 - Bis (trifluoromethyl)-phenyl carbamoyloxy) ethyl, 2 - (2 - pentafluoroethyl phenyl carbamoyloxy) ethyl, 2 - (3 - pentafluoroethyl phenyl carbamoyloxy) Ethyl, 2 - (4 - pentafluoroethyl phenyl carbamoyloxy) ethyl, 3 - (phenyl-carbamoyloxy) propyl, 3 - (3 - (trifluoromethyl) phenyl-carbamoyloxy) propyl, 3 - (4 - (trifluoromethyl) phenyl-carbamoyloxy) Propyl, 3 - (2,3 - Bis (trifluoromethyl)-phenyl carbamoyloxy) propyl, 3 - (2,4 - bis (trifluoromethyl) Phenyl-carbamoyloxy) propyl, 3 - (2,6 - Bis (trifluoromethyl)-phenyl carbamoyloxy) - propyl, 3 - (2 - phenyl-pentafluoroethyl - carbamoyloxy) propyl, 3 - (3 - pentafluoroethyl phenyl carbamoyloxy) Propyl, 3 - (4 - pentafluoroethyl phenyl carbamoyloxy) propyl, 4 - (4 - (trifluoromethyl) phenyl-carbamoyl Acyloxy)-butyl, 5 - (4 - trifluoromethyl-phenyl carbamoyloxy) pentyl, 6 - (4 - (trifluoromethyl) phenyl Carbamoyloxy yl) hexyl group, (2 - fluorophenyl carbamoyloxy) methyl, 2 - (3 - fluorophenyl carbamoyl Oxy) ethyl, 1 - (4 - fluorophenyl carbamoyloxy) ethyl, 3 - (2 - chlorophenyl carbamoyloxy) Propyl, 4 - (3 - chlorophenyl carbamoyloxy) butyl, 5 - (4 - chlorophenyl carbamoyloxy) pentyl group, 6 - (2 - bromophenyl carbamoyloxy) hexyl group, (3 - bromophenyl carbamoyloxy) methyl, 2 - (4 - bromo- Phenyl-carbamoyloxy) ethyl, 1 - (2 - iodo-phenyl-carbamoyloxy) ethyl, 3 - (3 - iodo-phenylamino Formyloxy) propyl, 4 - (4 - iodo-phenyl-carbamoyloxy) butyl group, 5 - (2,3 - difluorophenyl carbamoyl Acyloxy)-pentyl group, a 6 - (3,4 - difluorophenyl carbamoyloxy) hexyl group, (3,5 - difluorophenyl carbamoyl Acyloxy) methyl, 2 - (2,4 - difluorophenyl carbamoyloxy) ethyl, 1 - (2,6 - difluorophenyl ammonia Formyloxy) ethyl, 3 - (2,3 - dichlorophenyl carbamoyloxy) propyl, 4 - (3,4 - dichlorophenyl Carbamoyloxy) butyl, 5 - (3,5 - dichlorophenyl carbamoyloxy) pentyl, 6 - (2,4 - dichlorobenzene Carbamoyloxy yl) hexyl group, (2,6 - dichlorophenyl carbamoyloxy) methyl 2 - (3,4,5 - trifluoro- Phenyl-carbamoyloxy) ethyl, 1 - (2,3,4,5,6 - pentafluorophenyl carbamoyloxy) ethyl, 3 - (3,4,5 - trichloro-phenyl-carbamoyloxy) propyl group, 4 - (2,4,6 - trifluoro-phenyl-carbamoyloxy) Butyl group, 5 - (2,4,6 - trichlorophenyl carbamoyloxy) pentyl group, (2 - methyl - 3 - chlorophenyl carbamoyl Oxy) methyl, (3 - methyl - 4 - chlorophenyl carbamoyloxy) methyl, (2 - chloro-4 - methyl-phenyl-amino Formyloxy) methyl, (2 - methyl -3 - carbamoyloxy-fluorophenyl) methyl, ethyl carbamoyloxy Methyl, n-butyl carbamoyloxy group, n-hexyl carbamoyloxy group, n-pentyl carbamoyl Alkoxy methyl, N-methyl-N-phenyl-methyl carbamoyloxy, N, N-dimethyl-carbamoyloxy group A Group, N-methyl-N-ethyl-carbamoyloxy methyl, 2 - (N-(2 - fluorophenyl)-N-methyl-carbamoyl Oxy) ethyl, 1 - (N-(3 - fluorophenyl)-N-methyl-carbamoyloxy) ethyl, 3 - (N-(4 - fluorophenyl Yl)-N-methyl-carbamoyloxy) propyl group, 4 - (N-(2 - chlorophenyl)-N-methyl-carbamoyloxy) D Yl, 5 - (N-(3 - chlorophenyl)-N-methyl-carbamoyloxy) pentyl, 6 - (N-(4 - chlorophenyl)-N- Methyl-carbamoyloxy) hexyl group, (N-(4 - bromophenyl)-N-methyl-carbamoyloxy) methyl, 2 - (N-(2 - iodo-phenyl)-N-methyl-carbamoyloxy) ethyl, 1 - (N-(3 - iodo-phenyl)-N-methyl- Carbamoyloxy) ethyl, 3 - (N-(4 - iodo-phenyl)-N-methyl-carbamoyloxy) propyl, 4 - (N-(2,3 - difluorophenyl)-N-methyl-carbamoyloxy) butyl group, 5 - (N-(3,4 - difluorophenyl Yl)-N-methyl-carbamoyloxy) pentyl, 6 - (N-(3,5 - difluorophenyl)-N-methyl-carbamoyl oxygen Yl) hexyl group, (N-(2,4 - difluorophenyl)-N-methyl-carbamoyloxy) methyl, 2 - (N-(2,6 - two Fluorophenyl)-N-methyl-carbamoyloxy) ethyl, 1 - (N-(2,3 - dichlorophenyl)-N-methyl-carbamoyl Acyloxy) ethyl, 3 - (N-(3,4 - dichlorophenyl)-N-methyl-carbamoyloxy) propyl, (N-(3,5 - dichlorophenyl)-N-methyl-carbamoyloxy) methyl, 4 - (N-(2,4 - dichlorobenzene Yl)-N-methyl-carbamoyloxy) butyl group, 5 - (N-(2,6 - dichlorophenyl)-N-methyl-carbamoyl oxygen Yl) pentyl, 6 - (N-(3,4,5 - trifluoro-phenyl)-N-methyl-carbamoyloxy) hexyl group, (N-(3,4,5 - trichloro-phenyl)-N-methyl-carbamoyloxy) methyl, 2 - (N-(2,4,6 - trifluorobenzene Yl)-N-methyl-carbamoyloxy) ethyl, 1 - (N-(2,4,6 - trichloro-phenyl)-N-methyl-carbamoyl Oxy) ethyl, 3 - (N-(2 - methyl-phenyl)-N-methyl-carbamoyloxy) propyl group, 4 - (N-(3 - methyl Yl-phenyl)-N-methyl-carbamoyloxy) butyl group, 5 - (N-(4 - methylphenyl)-N-methyl-carbamoyl Oxy) hexyl, 6 - (N-(2 - methyl-3 - chlorophenyl)-N-methyl-carbamoyloxy) hexyl group, (N-(3 - Methyl-4 - chlorophenyl)-N-methyl-carbamoyloxy) methyl, 2 - (N-(2 - chloro-4 - methyl-phenyl Yl)-N-methyl-carbamoyloxy) ethyl, 1 - (N-(2 - methyl-3 - fluorophenyl)-N-methyl-carbamoyl Oxy) ethyl, 3 - (N-(2 - trifluoromethyl-phenyl)-N-methyl-carbamoyloxy) propyl, 4 - (N-(4 - trifluoromethyl-phenyl)-N-methyl-carbamoyloxy) butyl group, 2 - (N-(4 - trifluoromethyl- Phenyl)-N-methyl-carbamoyloxy) ethyl, 5 - (N-phenyl-N-phenyl-carbamoyloxy) pentyl group, 6 - (N-phenyl-N-(2 - fluorophenyl) carbamoyloxy) hexyl group, (N-phenyl-N-(3 - fluorophenyl) amino Formyloxy) methyl, 2 - (N-phenyl-N-(4 - fluorophenyl) - carbamoyloxy) ethyl, 1 - (N-phenyl Yl-N-(2 - chlorophenyl) carbamoyloxy) ethyl, 1 - (N-phenyl-N-(3 - chlorophenyl) carbamoyl oxygen Yl) ethyl, 3 - (N-phenyl-N-(4 - chlorophenyl) carbamoyloxy) propyl group, 4 - (N-phenyl-N-(2 - Bromophenyl) carbamoyloxy) butyl group, 5 - (N-phenyl-N-(3 - bromophenyl) carbamoyloxy) pentyl group, 6 - (N-phenyl-N-(4 - bromophenyl) - carbamoyloxy) hexyl group, (N-phenyl-N-(2 - iodo-phenyl) amino Formyloxy) methyl, 1 - (N-phenyl-N-(3 - iodophenyl) carbamoyloxy) ethyl, 2 - (N-phenyl Yl-N-(4 - iodophenyl) carbamoyloxy) ethyl, 1 - (N-phenyl-N-(2,3 - difluorophenyl) carbamoyl Acyloxy) ethyl, 3 - (N-phenyl-N-(3,4 - difluorophenyl) carbamoyloxy) propyl group, 4 - (N- Phenyl-N-(3,5 - difluorophenyl) - carbamoyloxy) butyl group, 5 - (N-phenyl-N-(2,4 - difluorophenyl Yl) carbamoyloxy) pentyl, 6 - (N-phenyl-N-(2,6 - difluorophenyl) carbamoyloxy) hexyl group, (N-phenyl-N-(2,3 - dichlorophenyl) carbamoyloxy) methyl, 2 - (N-phenyl-N-(3,4 - dichloro- Phenyl) - carbamoyloxy) ethyl, 1 - (N-phenyl-N-(3,5 - dichlorophenyl) carbamoyloxy) ethyl Group, 3 - (N-phenyl-N-(2,4 - dichlorophenyl) carbamoyloxy) propyl group, 4 - (N-phenyl- -N-(2,6 - dichlorophenyl) carbamoyloxy) butyl group, 5 - (N-phenyl-N-(3,4,5 - trifluorophenoxy Yl) - carbamoyloxy) pentyl, 6 - (N-phenyl-N-(3,4,5 - trichlorophenyl) carbamoyloxy) hexyl Group, (N-phenyl-N-(2,4,6 - trifluoro-phenyl) carbamoyloxy) methyl, 2 - (N-phenyl- -N-(2,4,6 - trichlorophenyl) carbamoyloxy) ethyl, 1 - (N-phenyl-N-(2 - methylphenyl) - Carbamoyloxy) ethyl, 3 - (N-phenyl-N-(3 - methylphenyl) carbamoyloxy) propyl group, 4 - (N- Phenyl-N-(4 - methylphenyl) carbamoyloxy) butyl group, 5 - (N-phenyl-N-(2 - methyl-3 - chlorophenyl Yl) carbamoyloxy) pentyl, 6 - (N-phenyl-N-(3 - methyl - 4 - chlorophenyl) - carbamoyloxy) Hexyl, (N-phenyl-N-(2 - chloro-4 - methylphenyl) carbamoyloxy) methyl, (N-phenyl-N-(2 - Methyl-3 - fluorophenyl) carbamoyloxy) methyl, 2 - (N-phenyl-N-(2 - trifluoromethyl-phenyl) - amino Formyloxy) ethyl, 1 - (N-phenyl-N-(3 - trifluoromethyl-phenyl) carbamoyloxy) ethyl, 3 - (N-phenyl-N-(4 - trifluoromethyl-phenyl) carbamoyloxy) propyl, 2 - isopropyl-phenyl-carbamoyl Acyloxymethyl 3 - isopropyl-phenyl carbamoyloxy group, 4 - iso-phenyl carbamoyloxy Methyl 2 - t-butylphenyl carbamoyloxy methyl 4 - n-butylphenyl carbamoyloxy group, 2 - methyl -4 - chlorophenyl carbamoyloxy methyl 3 - tert-butyl-phenyl-carbamoyloxy methyl 4 - Carbamoyloxy-tert-butylphenyl group, a 2 - sec-butylphenyl carbamoyloxy methyl 3 - sec Carbamoyloxy phenyl methyl 4 - sec-butylphenyl carbamoyloxy methyl 4 - phenylcarbamoyl pentyl Acyloxymethyl 4 - hexyl-phenyl carbamoyloxy group, 3,4 - dimethoxyphenyl carbamoyl oxygen Group, a 3,4,5 - trimethoxyphenyl carbamoyloxy group, 2 - methoxyphenyl carbamoyl oxygen Methyl 3 - methoxy-phenyl carbamoyloxy methyl 4 - methoxy-phenyl carbamoyloxy group, 2 - methoxy-3 - chlorophenyl carbamoyloxy group, 2 - (2 - fluoro-3 - methoxy-phenyl-carbamoyl oxygen Yl) ethyl, 1 - (2 - fluoro-4 - methoxy-phenyl-carbamoyloxy) ethyl, 3 - (2,6 - dimethoxy- Carbamoyloxy-phenyl) propyl, 4 - (2,3,4 - trifluoro-phenyl-carbamoyloxy) butyl group, 5 - (3,4,5 - trifluoro-phenyl-carbamoyloxy) pentyl group, a 6 - (2 - trifluoromethoxy-phenyl carbamoyl oxygen Yl) hexyl 3 - Trifluoromethoxyphenyl bamoyloxy methyl 4 - (trifluoromethoxy) phenyl carbamoyl Acyloxy group, 2 - (4 - trifluoromethoxy-phenyl carbamoyloxy) ethyl, 2 - (N-methyl-N-(4 - Trifluoromethoxyphenyl) carbamoyloxy) ethyl, 3 - (trifluoromethyl) phenyl-carbamoyloxy group, 4 - trifluoromethylphenyl carbamoyloxy methyl 3 - trifluoromethyl-4 - chlorophenyl methyl carbamoyloxy Yl, 3,5 - trifluoromethoxyphenyl carbamoyloxy group, 2,4 - dichlorophenyl carbamoyloxy Methyl 2 - chlorophenyl carbamoyloxy methyl 3 - chlorophenyl carbamoyloxy methyl 4 - chlorophenyl Carbamoyloxy group, 3,5 - dichlorophenyl carbamoyloxy group, 3,4 - dichlorophenyl carbamoyl Alkoxy group, a 2 - fluorophenyl carbamoyloxy methyl 3 - fluorophenyl carbamoyloxy methyl 4 - fluoro- Phenyl carbamoyloxy group, a 2 - phenyl pentafluoroethoxy carbamoyloxy methyl 3 - pentafluoro-ethoxyethyl Carbamoyloxy-phenyl methyl 4 - phenyl pentafluoroethoxy carbamoyloxy group, a 2 - isopropoxy Carbamoyloxy methyl-phenyl 3 - isopropoxy-phenyl-carbamoyloxy methyl 4 - isopropoxy Phenyl carbamoyloxy group, a 2 - tert-butoxy-phenyl-carbamoyloxy methyl 4 - n-butoxy-phenyl Carbamoyloxy group methyl 3 - methoxy-phenyl carbamoyloxy methyl 4 - methoxy-phenylcarbamoyl Acyloxymethyl 4 - ethoxyphenyl carbamoyloxy methyl 3 - tert-butoxy-phenyl carbamoyl oxygen Methyl 4 - tert-butoxy-phenyl carbamoyloxy group, a 2 - sec-butoxy-phenyl carbamoyloxy Methyl 3 - sec-butoxy-phenyl carbamoyloxy methyl 4 - sec-butoxy methyl-phenyl carbamoyloxy Group, 2 - n - heptafluoropropoxy bamoyloxy methyl phenyl 3 - n - heptafluoropropoxy phenylcarbamoyl Acyloxymethyl 4 - n - heptafluoropropoxy carbamoyloxy methyl phenyl 4 - n-pentyloxy-phenyl Carbamoyloxy methyl 4 - n-hexyloxy-phenyl carbamoyloxy methyl 4 - cyanophenyl carbamoyl Oxymethyl, (N-methyl-N-(3 - cyanophenyl) carbamoyloxy) methyl 2 - cyano-phenylamino Formyloxy group, 3,4 - dicyano-phenyl carbamoyloxy group, 3,4,5 - tricyanophenyl ammonia Formyloxy methyl 4 - phenoxy-phenyl-carbamoyloxy methyl, (N-methyl-N-(3 - phenoxy- Phenyl) carbamoyloxy) methyl 2 - phenoxy-phenyl carbamoyloxy group, 3,4 - diphenyl group Phenyl carbamoyloxy group, 2,4,6 - triphenyl methyl-phenyl carbamoyloxy 4 - (methylthio) Carbamoyloxy methyl phenyl, (N-methyl-N-(4 - methylthio-phenyl) carbamoyloxy) methyl, 3 - (methylthio) phenyl-carbamoyloxy group, a 2 - (methylthio) phenyl carbamoyloxy group, 3,4 - Methylthio-phenyl carbamoyloxy group, 2,4,6 - trimethoxyphenyl group phenyl-carbamoyloxy methyl 4 - Acetyl-phenyl carbamoyloxy methyl 3 - acetyl-phenyl carbamoyloxy group, a 2 - acetyl- Phenyl carbamoyloxy group, 3,4 - diacetyl-phenyl-carbamoyloxy methyl, (N-methyl- -N-(3,4 - diacetyl-phenyl) carbamoyloxy) methyl, 2,4,6 - triacetyl phenylcarbamoyloxy Oxy methyl 4 - biphenyl bamoyloxy methyl 3 - biphenyl bamoyloxy methyl 2 - benzidine Formyloxy methyl, (N-methyl-N-(2 - biphenyl) carbamoyloxy) methyl, 3,4 - diphenyl amino Formyloxy group, 2,4,6 - carbamoyloxy methyl phenyl 4 - n-heptyloxy-phenylcarbamoyl Formyloxy methyl, (N-methyl-N-4-(n-heptyloxyphenyl) carbamoyloxy) methyl, 3 - Regular Octyl-phenyl carbamoyloxy group, a 2 - n-nonyl phenyl methyl carbamoyloxy 4 - n-decyl Carbamoyloxy methyl-phenyl, 2,4 - II - n-heptyl-phenyl carbamoyloxy group, 2,4,6 - III - n-heptyl-phenyl carbamoyloxy group, 4 - (7,7 - dichloro-heptyl) phenyl amino Formyloxy methyl 4 - benzyloxy-phenyl carbamoyloxy methyl, (N-methyl-N-(4 - benzyloxy-phenyl) Carbamoyloxy) methyl 3 - benzyl-phenyl carbamoyloxy group, a 2 - benzyl-phenyl carbamoyl oxygen Ylmethyl, 2,4 - dibenzyl-phenyl carbamoyloxy group, 2,4,6 - tris-benzyloxy-phenyl carbamoyl oxygen Ylmethyl 4 - n-octylphenyl carbamoyloxy methyl, (N-methyl-N-(4 - n-octyl-phenyl) amino Formyloxy) methyl 3 - n-heptyl-phenyl carbamoyloxy group, a 2 - n-octyl-phenyl-carbamoyl Methyl group, 3 - (8,8,8 - trifluoro-octyl) phenyl carbamoyloxy methyl 4 - n-nonyl phenyl amino Formyloxy methyl 3 - n-decyl-phenyl carbamoyloxy group, 2,4 - II - n-octylphenyl ammonia Formyloxy group, 2,4,6 - III - octyl diphenyl-carbamoyloxy methyl 4 - phenyl - 3 - chloro- Bamoyloxy methyl phenyl 4 - phenoxy-3 - methylthiophenyl bamoyloxy methyl 4 - Positive Hept-3 - trifluoromethoxyphenyl carbamoyloxy methyl 4 - n-octyl-2 - (trifluoromethyl) phenyl - Carbamoyloxy methyl 4 - benzyl-2 - methyl-phenyl-carbamoyloxy group, 3,4 - ethylenedioxythiophene Carbamoyloxy methyl-phenyl, 3,4 - methylenedioxy-phenyl carbamoyloxy group, a benzyl group ammonia Formyloxy group, 2 - phenylethyl carbamoyloxy group, cyclohexyl carbamoyloxy group, 1 - naphthyl-carbamoyloxy group, a 2 - naphthyl carbamoyloxy group, 5 - (2,3 - dihydro-1H-indene Yl) carbamoyloxy group, 5 - (2,3 - dihydro-benzofuranyl) carbamoyloxy methyl, (N-methyl Yl-N-(3,4 - methylenedioxy-phenyl) carbamoyloxy) methyl, (N-methyl-N-benzyl-carbamoyl Oxy) methyl, (N-methyl-N-(2 - phenylethyl) carbamoyloxy) methyl, (N-methyl-N-Ring Hexyl carbamoyloxy) methyl, (N-methyl-N-(1 - naphthyl) carbamoyloxy) methyl, (N-methyl Yl-N-(2 - naphthyl) carbamoyloxy) methyl, (N-methyl-N-(5 - (2,3 - dihydro-1H-indene Yl)) - carbamoyloxy) methyl and (N-methyl-N-(2,3 - dihydro-5 - benzofuranyl) carbamoyl Oxy) methyl (wherein the amino group may be substituted with 1 or 2 groups selected from the following group Group: C1-C6 alkyl, C1-C6 alkyl where the phenyl group, the C3-C8 cycloalkyl, naphthyl, 2,3 - Dihydro-1H-indenyl group, a 2,3 - dihydro-benzofuran group and the phenyl group [wherein the phenyl ring, May be substituted with 1 to 5, preferably 1 to 3 groups, which is selected from C1-C4 alkylenedioxy, A cyano group, a phenoxy group, C1-C6 alkylthio, C1-C6 alkyl group, a phenyl group, a phenyl C1-C6 alkyl, A halogen atom, a halogen substituted or unsubstituted C1-C10 alkyl and halogen-substituted or unsubstituted C1-C10 alkoxy group (wherein the substituent is C1-C4 alkylenedioxy case Is preferably substituted with 1 or 2 groups)]). ...

The example of the C1-C6 alkyl that the C1-C6 alkyloyl replaces can comprise ethanoyl methyl, 2-propionyl ethyl, 1-butyryl radicals ethyl, 2-ethanoyl ethyl, 3-ethanoyl propyl group, 4-ethanoyl butyl, 4-isobutyryl butyl, 5-pentanoyl amyl group, 6-ethanoyl hexyl, 6-tertiary butyl carbonyl hexyl, 1,1-dimethyl-2-caproyl ethyl and 2-methyl-3-ethanoyl propyl group.

Except above-mentioned phenoxy group C1-C6 alkyl (wherein on this benzyl ring, can replace at least one group is arranged, it selects free halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and halogen replaces or the group of unsubstituted C1-C6 alkoxyl composition) in addition, phenoxy group C1-C6 alkyl (wherein on this benzyl ring, can replace and have at least one to be selected from the group of following group: halogen atom; The C1-C4 alkylene dioxo base; C1-C6 alkoxyl carbonyl; Phenyl; Phenoxy group; Pyrrole radicals; Benzothiazolyl; 1,2,4-triazolyl; Imidazole radicals; Different _ azoles base; Benzo _ azoles base; The BTA base; Cyano group; Nitro; The C2-C6 thiazolinyl; The C1-C6 alkanoyl; The C1-C6 alkyl that C1-C6 alkoxyl carbonyl replaces; The C1-C6 alkyl that the C1-C6 alkanoyl replaces; Group-N (R^11B)R ^12B(R wherein^11BAnd R^12BCan be identical or different, represent separately hydrogen atom, C1-C6 alkyl, C1-C6 alkanoyl or phenyl, R^11BAnd R^12Bcan directly or pass through nitrogen, oxygen or sulphur atom are bonded to each other, form 5-7 unit saturated heterocyclic together with the nitrogen-atoms adjacent with them, wherein on this heterocycle, can replace at least one group is arranged, it selects free C1-C6 alkoxyl carbonyl and amino [wherein on this amino, can replace and have at least one to be selected from phenyl (wherein on this benzyl ring, can replace at least one group is arranged, it selects free halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl forms group) and the group of C1-C6 alkyl] group of composition), phenyl C1-C6 alkoxyl, phenyl C1-C6 alkyl, the C1-C6 alkylthio group, the C3-C8 cycloalkyl, halogen replaces or unsubstituted C1-C6 alkyl, replace or unsubstituted C1-C6 alkoxyl with halogen) may further include phenoxy group C1-C6 alkyl, for example 3,4-methylenedioxybenzenes oxygen ylmethyl, 3,4-ethylenedioxybenzenes oxygen ylmethyl, 4-ethyoxyl carbonyl phenoxymethyl, 3-methoxycarbonyl phenoxymethyl, 2-ethyoxyl carbonyl phenoxymethyl, 2,4-di ethoxy carbonyl phenoxymethyl, 2,4,6-triethoxy carbonyl phenoxymethyl, 2-ethyoxyl carbonyl-4-methylenedioxy phenoxy ylmethyl, 2-methoxycarbonyl-4-methoxyphenoxy methyl, 2-methoxycarbonyl-3-methoxyphenoxy methyl, 2-(4-ethyoxyl carbonyl phenoxy group) ethyl, 4-cyano group phenoxymethyl, 3-cyano group phenoxymethyl, 2-cyano group phenoxymethyl, 2,4-dicyano phenoxymethyl, 2,4,6-tricyano phenoxymethyl, 2-(4-cyano group phenoxy group) ethyl, the 4-nitrophenoxy methyl, 3-nitro phenoxymethyl, 2-nitro phenoxymethyl, 2,4-2,4-dinitrophenoxy ylmethyl, 2,4,6-trinitro-phenoxymethyl, 2-(4-nitrophenoxy) ethyl, 4-pi-allyl phenoxymethyl, 3-pi-allyl phenoxymethyl, 2-pi-allyl phenoxymethyl, 3,4-diallyl phenoxymethyl, 3,4,5-triallyl phenoxymethyl, 2-(4-pi-allyl phenoxy group) ethyl, 2-(3-pi-allyl phenoxy group) ethyl, 3-diethylamino phenoxymethyl, 3-phenylamino phenoxymethyl, 4-acetyl-amino phenoxymethyl, 2,4,6-three (diethylamino) phenoxymethyl, 2-phenylamino phenoxymethyl, 2,4-diacetyl amino-benzene oxygen methyl, 2-(3-diethyl amino phenoxyl) ethyl, 2-(3-phenylamino phenoxy group) ethyl, 2-(4-(2-acetyl group ethyl) phenoxy group) ethyl, 4-(2-acetyl group ethyl) phenoxymethyl, 3-acetyl group methylenedioxy phenoxy ylmethyl, 2-(3-acetyl group propyl group) phenoxymethyl, 2,4-two (2-acetyl group ethyl) phenoxymethyl, 2,4,6-three (2-acetyl group ethyl) phenoxymethyl, 4-methoxycarbonyl methylenedioxy phenoxy ylmethyl, 3-ethyoxyl carbonyl methylenedioxy phenoxy ylmethyl, 2-methoxycarbonyl methylenedioxy phenoxy ylmethyl, 2,4-dimethoxy carbonyl methylenedioxy phenoxy ylmethyl, 2,4,6-trimethoxy carbonyl methylenedioxy phenoxy ylmethyl, 2-(4-methoxycarbonyl methylphenoxy) ethyl, 4-propiono phenoxymethyl, 4-acetyl group phenoxymethyl, 3-propiono phenoxymethyl, 2-acetyl group phenoxymethyl, 2,4-, two propiono phenoxymethyls, 2,4,6-triacetyl phenoxymethyl, 2-(4-propiono phenoxy group) ethyl, 2-benzyl phenoxymethyl, 3-benzyl phenoxymethyl, 4-benzyl phenoxymethyl, 2,3-dibenzyl phenoxymethyl, 3,4,5-tribenzyl phenoxymethyl, 4-methyl mercapto phenoxymethyl, 3-methyl mercapto phenoxymethyl, 2-methyl mercapto phenoxymethyl, 2,4-dimethyl sulphur-based phenoxymethyl, 2,4,6-, three methyl mercapto phenoxymethyls, 2-(4-methyl mercapto phenoxy group) ethyl, 4-cyclopenta phenoxymethyl, 3-cyclohexyl phenoxymethyl, 4-cyclohexyl phenoxymethyl, 2-suberyl phenoxymethyl, 2,4-, two cyclopenta phenoxymethyls, 2,4-cyclopenta-6-ring Octylphenoxy methyl, 2-(4-cyclohexyl phenoxy group) ethyl, 2-(4-cyclopenta phenoxy group) ethyl, 4-n-octyloxy phenoxymethyl, 2-(4-n-octyloxy phenoxy group) ethyl, 4-phenyl phenoxymethyl, 3-phenyl phenoxymethyl, 2-phenyl phenoxymethyl, 2,4-diphenyl phenoxymethyl, 2,4,6-triphenyl phenoxymethyl, 2-(4-phenyl phenoxy group) ethyl, 4-phenoxy-phenoxy methyl, 3-phenoxy-phenoxy methyl, 2-phenoxy-phenoxy methyl, 2,4-hexichol oxygen phenoxyl methyl, 2,4,6-triphen oxygen phenoxyl methyl, 2-(3-phenoxy-phenoxy) ethyl, 4-benzyloxy phenoxymethyl, 3-benzyloxy phenoxymethyl, 2-benzyloxy phenoxymethyl, 2,4-benzyloxy phenoxymethyl, 2,4,6-, three benzyloxy phenoxymethyls, 2-(4-benzyloxy phenoxy group) ethyl, 2,4-dibenzyl phenoxymethyl, 2,4,6-tribenzyl phenoxymethyl, 2-(4-benzyl phenoxy group) ethyl, 4-(1-pyrrole radicals) phenoxymethyl, 3-(1-pyrrole radicals) phenoxymethyl, 2-(1-pyrrole radicals) phenoxymethyl, 2,4-two (1-pyrrole radicals) phenoxymethyl, 2,4,6-three (1-pyrrole radicals) phenoxymethyl, 2-(2-[4-morpholinodithio base) phenoxymethyl, 2-(2-benzothiazolyl) phenoxymethyl, 3-(2-[4-morpholinodithio base) phenoxymethyl, 2,4,6-three (5-benzothiazolyl) phenoxymethyl, 2,4-two (6-benzothiazolyl) phenoxymethyl, 4-(1-1,2,4-triazolyl) phenoxymethyl, 3-(1-1,2,4-triazolyl) phenoxymethyl, 2-(1-1,2,4-triazolyl) phenoxymethyl, 4-(3-1,2,4-triazolyl) phenoxymethyl, 2,4-two (5-1,2,4-triazolyl) phenoxymethyl, 2,4,6-three (1-1,2,4-triazolyl) phenoxymethyl, 4-(5-different _ azoles base) phenoxymethyl, 3-(3-different _ azoles base) phenoxymethyl, 2-(4-different _ azoles base) phenoxymethyl, 2-(5-different _ azoles base) phenoxymethyl, 2,4-two (5-different _ azoles base) phenoxymethyl, 2,4,6-three (5-different _ azoles base) phenoxymethyl, 4-(1-imidazole radicals) phenoxymethyl, 3-(2-imidazole radicals) phenoxymethyl, 2-(4-imidazole radicals) phenoxymethyl, 2,4-two (1-imidazole radicals) phenoxymethyl, 2,4,6-three (1-imidazole radicals) phenoxymethyl, 4-(1-BTA base) phenoxymethyl, 3-(1-BTA base) phenoxymethyl, 2-(1-BTA base) phenoxymethyl, 2-(1-BTA base) phenoxymethyl, 2,4-two (1-BTA base) phenoxymethyl, 2,4,6-three (1-BTA base) phenoxymethyl, 4-(6-benzimidazolyl) phenoxymethyl, 3-(5-benzimidazolyl) phenoxymethyl, 2-(2-benzimidazolyl) phenoxymethyl, 2-(1-BTA base) phenoxymethyl, 2,4-two (2-benzimidazolyl) phenoxymethyl, 2,4,6-three (2-benzimidazolyl) phenoxymethyl, 4-(4-tert-butoxycarbonyl-1-piperazinyl) phenoxymethyl, 2-(4-(4-(4-(N-(4-chlorphenyl)-N-methylamino))-1-piperidyl) phenoxy group) ethyl, 2-(4-(1-1,2,4-triazolyl) phenoxy group) ethyl, 2-(2-(5-different _ azoles base) phenoxy group) ethyl, 2-(2-methoxyl group-4-pi-allyl phenoxy group) ethyl, 2-(2-fluoro-4-nitro phenoxy group) ethyl, 2-(2-ethyoxyl-5-pi-allyl phenoxy group) ethyl, 2-fluoro-4-nitrophenoxy methyl, 2-methoxyl group-4-pi-allyl phenoxymethyl, 2-ethyoxyl-5-pi-allyl phenoxymethyl and 2-methyl-4-acetyl group phenoxymethyl (wherein on this benzyl ring, can replace and have 1 to 5, preferred 1 to 3 group that is selected from following group: halogen atom, above-mentioned C1-C4 alkylene dioxo base, above-mentioned C1-C6 alkoxyl carbonyl, phenyl, phenoxy group, pyrrole radicals, benzothiazolyl, 1,2,4-triazolyl, imidazole radicals, different _ azoles base, benzo _ azoles base, the BTA base, cyano group, nitro, above-mentioned C2-C6 thiazolinyl, above-mentioned C1-C6 alkanoyl, the C1-C6 alkyl that above-mentioned C1-C6 alkoxyl carbonyl replaces, the C1-C6 alkyl that above-mentioned C1-C6 alkanoyl replaces, group-N (R^11B)R ^12B(R wherein^11BAnd R^12BCan be identical or different, represent separately hydrogen atom, above-mentioned C1-C6 alkyl, above-mentioned C1-C6 alkanoyl or phenyl, above-mentioned R^11BAnd R^12Bcan directly or pass through nitrogen, oxygen or sulphur atom are bonded to each other, form 5-7 unit saturated heterocyclic together with the nitrogen-atoms adjacent with them, wherein on this heterocycle, can replace 1 to 3 group is arranged, it selects free C1-C6 alkoxyl carbonyl and amino [wherein on this amino, can replace and have 1 or 2 to be selected from phenyl (wherein on this benzyl ring, can replace and have 1 to 5, preferred 1 to 3 is selected from following group: halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl forms group) and the group of C1-C6 alkyl] group of composition), above-mentioned phenyl C1-C6 alkoxyl, above-mentioned phenyl C1-C6 alkyl, above-mentioned C1-C6 alkylthio group, above-mentioned C3-C8 cycloalkyl, that replace or the unsubstituted C1-C6 alkyl of above-mentioned halogen, that replace with above-mentioned halogen or unsubstituted C1-C10 alkoxyl (substituting group is in the situation of C1-C4 alkylene dioxo base therein, can replace 1 or 2 group is arranged)).

The example of tetrahydro-pyran oxy C1-C6 alkyl can comprise (2-tetrahydro-pyran oxy) methyl, 2-(3-tetrahydro-pyran oxy) ethyl, 1-(4-tetrahydro-pyran oxy) ethyl, 2-(2-tetrahydro-pyran oxy) ethyl, 3-(2-tetrahydro-pyran oxy) propyl group, 4-(2-tetrahydro-pyran oxy) butyl, 4-(3-tetrahydro-pyran oxy) butyl, 5-(2-tetrahydro-pyran oxy) amyl group, 6-(2-tetrahydro-pyran oxy) hexyl, 6-(2-tetrahydro-pyran oxy) hexyl, 1,1-dimethyl-2-(4-tetrahydro-pyran oxy) ethyl and 2-methyl-3-(3-tetrahydro-pyran oxy) propyl group.

The C1-C6 alkyl that furyl C1-C6 alkoxyl group replaces is (wherein on this furan nucleus, can be substituted with at least one C1-C6 alkoxy carbonyl) example can comprise the C1-C6 alkyl that furyl C1-C6 alkoxyl group replaces, ((2-furyl) methoxyl group) methyl for example, (2-(3-furyl) oxyethyl group) methyl, (3-(2-furyl) propoxy-) methyl, (2-(3-furyl) propoxy-) methyl, (4-(2-furyl) butoxy) methyl, (5-(3-furyl) pentyloxy) methyl, (4-(2-furyl) pentyloxy) methyl, (6-(3-furyl) hexyloxy) methyl, 2-((2-furyl) methoxyl group) ethyl, 1-(2-(3-furyl) oxyethyl group) ethyl, 3-(3-(2-furyl) propoxy-) propyl group, 4-(2-(3-furyl) propoxy-) butyl, 5-(4-(2-furyl) butoxy) hexyl, 1,1-dimethyl-2-(5-(3-furyl) pentyloxy) ethyl, 2-methyl-3-(4-(2-furyl) pentyloxy) propyl group, 2-(6-(3-furyl) hexyloxy) ethyl, ((5-ethoxy carbonyl-2-furyl) methoxyl group) methyl, ((4-methoxycarbonyl-2-furyl) methoxyl group) methyl, ((3-propoxycarbonyl-2-furyl) methoxyl group) methyl, ((5-butoxy carbonyl-2-furyl) methoxyl group) methyl, ((4-pentyloxy carbonyl-2-furyl) methoxyl group) methyl, ((3-hexyloxy carbonyl-2-furyl) methoxyl group) methyl, ((3,5-di ethoxy carbonyl-2-furyl) methyl and ((3 methoxyl group), 4,5-triethoxy carbonyl-2-furyl) methyl (wherein on this furan nucleus, can be substituted with 1 to 3 C1-C6 alkoxy carbonyl) methoxyl group).

The example of C3-C8 cycloalkyl C1-C6 alkyl can comprise cyclohexyl methyl, 2-cyclopropyl ethyl, 1-cyclopentyl ethyl, 3-cyclobutyl propyl group, 4-cyclohexyl butyl, 5-suberyl amyl group, 6-ring octyl group hexyl, 1,1-dimethyl-2-cyclohexyl ethyl and 2-methyl-3-cyclohexyl propyl group.

The C1-C6 alkyl that tetrazyl C1-C6 alkoxyl group replaces is (wherein on this tetrazole ring, can be substituted with the group that is selected from following groups: phenyl is (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed), phenyl C1-C6 alkyl and C3-C8 cycloalkyl C1-C6 alkyl) example can comprise the C1-C6 alkyl that tetrazyl C1-C6 alkoxyl group replaces, ((5-tetrazyl) methoxyl group) methyl for example, (2-(5-tetrazyl) oxyethyl group) methyl, (3-(5-tetrazyl) propoxy-) methyl, (2-(5-tetrazyl) propoxy-) methyl, (4-(5-tetrazyl) butoxy) methyl, (5-(5-tetrazyl) pentyloxy) methyl, (4-(1-tetrazyl) pentyloxy) methyl, (6-(5-tetrazyl) hexyloxy) methyl, (2-(1-tetrazyl) methoxyl group) ethyl, 1-(2-(5-tetrazyl) oxyethyl group) ethyl, 3-(3-(1-tetrazyl) propoxy-) propyl group, 4-(2-(5-tetrazyl) propoxy-) butyl, 5-(4-(1-tetrazyl) butoxy) hexyl, 1,1-dimethyl-2-(5-(5-tetrazyl) pentyloxy) ethyl, 2-methyl-3-(4-(1-tetrazyl) pentyloxy) propyl group, 2-(6-(5-tetrazyl) hexyloxy) ethyl, ((1-(2-phenylethyl)-5-tetrazyl) methoxyl group) methyl, ((1-cyclohexyl methyl-5-tetrazyl) methoxyl group) methyl, ((5-benzyl-1-tetrazyl) methoxyl group) methyl, ((1-cyclopentyl-methyl-5-tetrazyl) methoxyl group) methyl, ((5-(2-cyclohexyl ethyl)-1-tetrazyl) methoxyl group) methyl, ((1-benzyl-5-tetrazyl) methoxyl group) methyl, ((1-suberyl methyl-5-tetrazyl) methoxyl group) methyl, ((1-(3-phenyl propyl)-5-tetrazyl) methoxyl group) methyl, (1-phenyl-5-tetrazyl) methoxymethyl, ((1-(4-Trifluoromethoxyphen-l)-5-tetrazyl) methoxymethyl, ((1-(4-trifluoromethyl)-5-tetrazyl) methoxyl group) methyl, ((1-(4-chloro-phenyl-)-5-tetrazyl) methoxyl group) methyl is (wherein on this tetrazole ring, can be substituted with the group that is selected from following groups: phenyl is (wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 group, it is selected from by halogen atom, halogen replaces or the unsubstituted straight or branched alkyl of 1 to 6 carbon atom and the group that halogen replaces or the unsubstituted straight or branched alkoxyl group that contains 1 to 6 carbon atom is formed of containing), above-mentioned phenyl C1-C6 alkyl and above-mentioned C3-C8 cycloalkyl C1-C6 alkyl).

The C1-C6 alkyl that different _ azoles base C1-C6 alkoxyl group replaces is (wherein on this different _ azoles ring, can be substituted with at least one C1-C6 alkyl) example can comprise the C1-C6 alkyl that different _ azoles base C1-C6 alkoxyl group replaces, ((3-different _ azoles base) methoxyl group for example) methyl, (2-(4-different _ azoles base) oxyethyl group) methyl, (3-(5-different _ azoles base) propoxy-) methyl, (2-(3-different _ azoles base) propoxy-) methyl, (4-(4-different _ azoles base) butoxy) methyl, (5-(5-different _ azoles base) pentyloxy) methyl, (4-(3-different _ azoles base) pentyloxy) methyl, (6-(4-different _ azoles base) hexyloxy) methyl, (2-(5-different _ azoles base) methoxyl group) ethyl, 1-(2-(3-different _ azoles base) oxyethyl group) ethyl, 3-(3-(4-different _ azoles base) propoxy-) propyl group, 4-(2-(5-different _ azoles base) propoxy-) butyl, 5-(4-(3-different _ azoles base) butoxy) hexyl, 1,1-dimethyl-2-(5-(4-different _ azoles base) pentyloxy) ethyl, 2-methyl-3-(4-(5-different _ azoles base) pentyloxy) propyl group, 2-(6-(3-different _ azoles base) hexyloxy) ethyl, ((5-methyl-3-different _ azoles base) methoxyl group) methyl, ((4-ethyl-3-different _ azoles base) methoxyl group) methyl, ((3-n-propyl-4-different _ azoles base) methoxyl group) methyl, ((5-normal-butyl-3-different _ azoles base) methoxyl group) methyl, ((4-n-pentyl-3-different _ azoles base) methoxyl group) methyl, ((3-n-hexyl-5-different _ azoles base) methoxyl group) methyl and ((4,5-dimethyl-3-is different _ the azoles base) and methoxyl group) methyl (wherein on this different _ azoles ring, can be substituted with above-mentioned 1 to 2 C1-C6 alkyl).

The C1-C6 alkyl that benzothienyl C1-C6 alkoxyl group replaces is (wherein on this thionaphthene ring, can be substituted with at least one and be selected from following group: halogen atom, the group that halogen replacement or unsubstituted C1-C6 alkyl and halogen replacement or unsubstituted C1-C6 alkoxyl group are formed) example can comprise the C1-C6 alkyl that benzothienyl C1-C6 alkoxyl group replaces, ((3-benzothienyl) methoxyl group) methyl for example, ((2-benzothienyl) oxyethyl group) methyl, (3-(4-benzothienyl) propoxy-) methyl, (2-(5-benzothienyl) propoxy-) methyl, (4-(6-benzothienyl) butoxy) methyl, (5-(7-benzothienyl) pentyloxy) methyl, (4-(3-benzothienyl) pentyloxy) methyl, (6-(2-benzothienyl) hexyloxy) methyl, 2-((4-benzothienyl) methoxyl group) ethyl, 1-(2-(5-benzothienyl) oxyethyl group) ethyl, 3-(3-(6-benzothienyl) propoxy-) propyl group, 4-(2-(7-benzothienyl) propoxy-) butyl, 5-(4-(3-benzothienyl) butoxy) hexyl, 1,1-dimethyl-2-(5-(3-benzothienyl) pentyloxy) ethyl, 2-methyl-3-(4-(5-benzothienyl) pentyloxy) propyl group, 2-(6-(3-benzothienyl) hexyloxy) ethyl, ((5-methyl-3-benzothienyl) methoxyl group) methyl, ((4-ethyl-3-benzothienyl) methoxyl group) methyl, ((5-chloro-3-benzothienyl) methoxyl group) methyl, ((6-methyl-3-benzothienyl) methoxyl group) methyl, ((4-trifluoromethyl-3-benzothienyl) methoxyl group) methyl, ((3-methoxyl group-5-benzothienyl) methoxyl group) methyl, ((5-trifluoromethoxy-3-benzothienyl) methoxyl group) methyl, ((4,5-two chloro-3-benzothienyls) methyl methoxyl group), ((2,4,5-three fluoro-3-benzothienyls) methyl methoxyl group), ((4,5-two chloro-2-methyl-3-benzothienyls) methyl and ((4 methoxyl group), 5-two chloro-2-methoxyl group-3-benzothienyls) methoxyl group) methyl (wherein on this thionaphthene ring, can be substituted with 1 to 3 and be selected from following group: above-mentioned halogen atom, group that above-mentioned halogen replaces or unsubstituted C1-C6 alkyl and the replacement of above-mentioned halogen or that unsubstituted C1-C6 alkoxyl group is formed).

1,3, the C1-C6 alkyl that 4-_ di azoly C1-C6 alkoxyl group replaces (wherein this 1,3, on the 4-_ diazole ring, can be substituted with phenyl [wherein on this benzyl ring, can be substituted with at least one and be selected from following group: halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group]) example can comprise 1,3, the C1-C6 alkyl that 4-_ di azoly C1-C6 alkoxyl group replaces, ((2-1 for example, 3, the 4-_ di azoly) methyl methoxyl group), (2-(2-1,3, the 4-_ di azoly) methyl oxyethyl group), (3-(2-1,3, the 4-_ di azoly) methyl propoxy-), (2-(2-1,3, the 4-_ di azoly) methyl propoxy-), (4-(2-1,3, the 4-_ di azoly) methyl butoxy), (5-(2-1,3, the 4-_ di azoly) methyl pentyloxy), (4-(2-1,3, the 4-_ di azoly) methyl pentyloxy), (6-(2-1,3, the 4-_ di azoly) methyl hexyloxy), 2-((2-1,3, the 4-_ di azoly) ethyl methoxyl group), 1-(2-(2-1,3, the 4-_ di azoly) ethyl oxyethyl group), 3-(3-(2-1,3, the 4-_ di azoly) propyl group propoxy-), 4-(2-(2-1,3, the 4-_ di azoly) butyl propoxy-), 5-((2-1,3, the 4-_ di azoly) amyl group methoxyl group), 6-(4-(2-1,3, the 4-_ di azoly) hexyl butoxy), 1,1-dimethyl-2-(5-(2-1,3, the 4-_ di azoly) ethyl pentyloxy), 2-methyl-3-(4-(2-1,3, the 4-_ di azoly) pentyloxy) propyl group, 2-(6-(2-1,3, the 4-_ di azoly) ethyl hexyloxy), (5-(4-aminomethyl phenyl)-2-1,3, the 4-_ di azoly) methoxymethyl, (5-(4-chloro-phenyl-)-2-1,3, the 4-_ di azoly) methoxymethyl, (5-(4-trifluoromethyl)-2-1,3, the 4-_ di azoly) methoxymethyl, (5-(4-p-methoxy-phenyl)-2-1,3, the 4-_ di azoly) methoxymethyl, (5-(4-Trifluoromethoxyphen-l)-2-1,3, the 4-_ di azoly) methoxymethyl, (5-(2,4 dichloro benzene base)-2-1,3, the 4-_ di azoly) methoxymethyl, (5-(2,4, the 6-trimethylphenyl)-2-1,3, the 4-_ di azoly) methoxymethyl and (5-(2, the 4-Dimethoxyphenyl)-2-1,3, the 4-_ di azoly) methoxymethyl (wherein this 1,3, on the 4-_ diazole ring, can be substituted with above-mentioned phenyl [wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed]).

The example of the C1-C6 alkyl that the C2-C6 alkynyloxy group replaces can comprise acetylene oxygen ylmethyl, 2-acetylene oxygen ylmethyl, 2-(2-second alkynyloxy group) ethyl, 1-(2-butyne oxygen base) ethyl, 2-(3-fourth alkynyloxy group) ethyl, 3-(1-methyl-2-third alkynyloxy group) propyl group, 4-(valerylene oxygen base) butyl, 4-(the own alkynyloxy group of 2-) butyl, 5-(2-third alkynyloxy group) amyl group, 6-(2-third alkynyloxy group) hexyl, 6-(2-butyne oxygen base) hexyl, 1,1-dimethyl-2-(2-third alkynyloxy group) ethyl and 2-methyl-3-(2-third alkynyloxy group) propyl group.

The example of the C1-C6 alkyl that naphthyl C1-C6 alkoxyl group replaces can comprise (1-naphthyl) methoxymethyl, (2-(2-naphthyl) oxyethyl group) methyl, (3-(1-naphthyl) propoxy-) methyl, (2-(2-naphthyl) propoxy-) methyl, (4-(1-naphthyl) butoxy) methyl, (5-(2-naphthyl) pentyloxy) methyl, (4-(1-naphthyl) pentyloxy) methyl, (6-(1-naphthyl) hexyloxy) methyl, 2-((1-naphthyl) methoxyl group) ethyl, 1-(2-(2-naphthyl) oxyethyl group) ethyl, 3-(3-(1-naphthyl) propoxy-) propyl group, 4-(2-(2-naphthyl) propoxy-) butyl, 5-(4-(1-naphthyl) butoxy) amyl group, 6-(5-(2-naphthyl) pentyloxy) hexyl, 1,1-dimethyl-2-(4-(1-naphthyl) pentyloxy) ethyl and 2-methyl-3-(6-(1-naphthyl) hexyloxy) propyl group.

1,2, the C1-C6 alkyl that 4-_ di azoly C1-C6 alkoxyl group replaces [wherein this 1,2, on the 4-_ diazole ring, can be substituted with phenyl] example can comprise 1,2, the C1-C6 alkyl that 4-_ di azoly C1-C6 alkoxyl group replaces, for example ((3-1,2, the 4-_ di azoly) methyl methoxyl group), (2-(5-1,2,4-_ di azoly) oxyethyl group) methyl, (3-(3-1,2, the 4-_ di azoly) methyl propoxy-), (2-(5-1,2,4-_ di azoly) propoxy-) methyl, (4-(3-1,2, the 4-_ di azoly) methyl butoxy), (5-(5-1,2,4-_ di azoly) pentyloxy) methyl, (4-(3-1,2, the 4-_ di azoly) methyl pentyloxy), (6-(3-1,2,4-_ di azoly) hexyloxy) methyl, 2-((5-1,2, the 4-_ di azoly) ethyl methoxyl group), 1-(2-(3-1,2,4-_ di azoly) oxyethyl group) ethyl, 3-(3-(5-1,2, the 4-_ di azoly) propyl group propoxy-), 4-(2-(3-1,2,4-_ di azoly) propoxy-) butyl, 5-((3-1,2, the 4-_ di azoly) amyl group methoxyl group), 6-(4-(5-1,2,4-_ di azoly) butoxy) hexyl, 1,1-dimethyl-2-(5-(3-1,2, the 4-_ di azoly) pentyloxy) ethyl, 2-methyl-3-(4-(5-1,2, the 4-_ di azoly) propyl group pentyloxy), 2-(6-(3-1,2, the 4-_ di azoly) hexyloxy) ethyl, (5-phenyl-3-1,2, the 4-_ di azoly) methoxymethyl and (3-phenyl-5-1,2,4-_ di azoly) methoxymethyl [wherein this 1,2, on the 4-_ diazole ring, can be substituted with phenyl].

The C1-C6 alkyl that pyridyl C1-C6 alkoxyl group replaces is [wherein on this pyridine ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group] example can comprise the C1-C6 alkyl that pyridyl C1-C6 alkoxyl group replaces, (2-pyridyl) methoxymethyl for example, (2-(3-pyridyl) oxyethyl group) methyl, (3-(4-pyridyl) propoxy-) methyl, (2-(2-pyridyl) propoxy-) methyl, (4-(3-pyridyl) butoxy) methyl, (5-(4-pyridyl) pentyloxy) methyl, (4-(2-pyridyl) pentyloxy) methyl, (6-(3-pyridyl) hexyloxy) methyl, (2-(4-pyridyl) methoxyl group) ethyl, 1-(2-(2-pyridyl) oxyethyl group) ethyl, 3-(3-(3-pyridyl) propoxy-) propyl group, 4-(2-(4-pyridyl) propoxy-) butyl, 5-((2-pyridyl) methoxyl group) amyl group, 6-(4-(2-pyridyl) butoxy) hexyl, 1,1-dimethyl-2-(5-(3-pyridyl) pentyloxy) ethyl, 2-methyl-3-(4-(4-pyridyl) pentyloxy) propyl group, 2-(6-(2-pyridyl) hexyloxy) ethyl, (2-trifluoromethyl-5-pyridyl) methoxymethyl, (4-chloro-2-pyridyl) methoxymethyl, (3-trifluoromethyl-2-pyridyl) methoxymethyl, (2-methoxyl group-4-pyridyl) methoxymethyl, (2-trifluoromethoxy-5-pyridyl) methoxymethyl, (2,4-two bromo-3-pyridyl) methoxymethyl, (2,4,6-trimethylammonium-5-pyridyl) methoxymethyl, (2,4-dimethoxy-5-pyridyl) methoxymethyl and (2,4,6-three fluoro-3-pyridyl) methoxymethyl is [wherein on this pyridine ring, can be substituted with 1 to 3 group, it is selected from by above-mentioned halogen atom, group that above-mentioned halogen replaces or unsubstituted C1-C6 alkyl and the replacement of above-mentioned halogen or that unsubstituted C1-C6 alkoxyl group is formed].

The C1-C6 alkyl that thiazolyl C1-C6 alkoxyl group replaces is [wherein on this thiazole ring, can be substituted with at least one group, it is selected from by phenyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group) and the group formed of low alkyl group] example can comprise the C1-C6 alkyl of thiazolyl C1-C6 alkoxyl group replacement, (4-thiazolyl) methoxymethyl for example, (2-(2-thiazolyl) oxyethyl group) methyl, (3-(5-thiazolyl) propoxy-) methyl, (2-(4-thiazolyl) propoxy-) methyl, (4-(2-thiazolyl) butoxy) methyl, (5-(4-thiazolyl) pentyloxy) methyl, (4-(5-thiazolyl) pentyloxy) methyl, (6-(4-thiazolyl) hexyloxy) methyl, (2-(2-thiazolyl) methoxyl group) ethyl, 1-(2-(5-thiazolyl) oxyethyl group) ethyl, 3-(3-(4-thiazolyl) propoxy-) propyl group, 4-(2-(2-thiazolyl) propoxy-) butyl, 5-((4-thiazolyl) methoxyl group) amyl group, 6-(4-(5-thiazolyl) butoxy) hexyl, 1,1-dimethyl-2-(5-(4-thiazolyl) pentyloxy) ethyl, 2-methyl-3-(4-(2-thiazolyl) pentyloxy) propyl group, 2-(6-(5-thiazolyl) hexyloxy) ethyl, (2-(4-aminomethyl phenyl)-4-thiazolyl) methoxymethyl, (2-(4-chloro-phenyl-)-4-thiazolyl) methoxymethyl, (2-(4-trifluoromethyl)-4-thiazolyl) methoxymethyl, (5-(4-p-methoxy-phenyl)-4-thiazolyl) methoxymethyl, (2-(4-Trifluoromethoxyphen-l)-4-thiazolyl) methoxymethyl, (5-(2, the 4-dichlorophenyl)-and the 2-thiazolyl) methoxymethyl, (4-(2,4, the 6-trimethylphenyl)-and the 2-thiazolyl) methoxymethyl, (4-(2, the 4-Dimethoxyphenyl)-and the 2-thiazolyl) methoxymethyl, (2-methyl-4-thiazolyl) methoxymethyl, (2,5-dimethyl-5-thiazolyl) methoxymethyl and (2-phenyl-4-methyl-5-thiazole base) methoxymethyl are [wherein on this thiazole ring, can be substituted with 1 or 2 group, it is selected from by above-mentioned phenyl (wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 is selected from following group: halogen atom, halogen replaces or the unsubstituted straight or branched C1-C6 alkyl of 1 to 6 carbon atom and the group that halogen replaces or the unsubstituted straight or branched C1-C6 alkoxyl group that contains 1 to 6 carbon atom is formed of containing) and contain the group of the straight or branched alkyl composition of 1 to 6 carbon atom].

1,2,3, the C1-C6 alkyl that 4-tetralyl C1-C6 alkoxyl group replaces [wherein this 1,2,3, on the 4-tetrahydric naphthalene ring, can be substituted with at least one C1-C6 alkyl] example can comprise 1,2,3, the C1-C6 alkyl that 4-tetralyl C1-C6 alkoxyl group replaces, for example (6-1,2,3, the 4-tetralyl) methoxymethyl, (2-(2-1,2,3, the 4-tetralyl) oxyethyl group) methyl, (3-(3-1,2,3, the 4-tetralyl) propoxy-) methyl, (2-(4-1,2,3, the 4-tetralyl) propoxy-) methyl, (4-(5-1,2,3, the 4-tetralyl) butoxy) methyl, (5-(6-1,2,3, the 4-tetralyl) pentyloxy) methyl, (4-(6-1,2,3, the 4-tetralyl) methyl pentyloxy), (6-(5-1,2,3, the 4-tetralyl) methyl hexyloxy), 2-((6-1,2,3, the 4-tetralyl) methoxyl group) ethyl, 1-(2-(6-1,2,3, the 4-tetralyl) oxyethyl group) ethyl, 3-(3-(5-1,2,3, the 4-tetralyl) propyl group propoxy-), 4-(2-(5-1,2,3, the 4-tetralyl) butyl propoxy-), 5-(4-(6-1,2,3, the 4-tetralyl) butoxy) amyl group, 6-(5-(5-1,2,3, the 4-tetralyl) pentyloxy) hexyl, 1,1-dimethyl-2-(4-(6-1,2,3, the 4-tetralyl) pentyloxy) ethyl, 2-methyl-3-(6-(6-1,2,3, the 4-tetralyl) propyl group hexyloxy), (1,1,4,4-tetramethyl--6-1,2,3, the 4-tetralyl) methoxymethyl, (1,1,4-trimethylammonium-6-1,2,3, the 4-tetralyl) methoxymethyl, (1,1-dimethyl-6-1,2,3, the 4-tetralyl) methoxymethyl, (1,1-dimethyl-7-1,2,3, the 4-tetralyl) methoxymethyl, (1-methyl-6-1,2,3, the 4-tetralyl) methoxymethyl, (1,4-dimethyl-6-1,2,3, the 4-tetralyl) methoxymethyl, (1,1,4,4-tetraethyl--6-1,2,3, the 4-tetralyl) methoxymethyl, (1,1-dimethyl-4-ethyl-6-1,2,3, the 4-tetralyl) methoxymethyl, (1,1-two-n-propyl-6-1,2,3, the 4-tetralyl) methoxymethyl, (4,4-di-n-butyl-6-1,2,3, the 4-tetralyl) methoxymethyl, (1-n-pentyl-6-1,2,3, the 4-tetralyl) methoxymethyl, (1,4-two-n-hexyl-6-1,2,3, the 4-tetralyl) methoxymethyl and (1-methyl-5-n-propyl-4-ethyl-6-1,2,3,4-tetralyl) methoxymethyl [wherein this 1,2,3, on the 4-tetrahydric naphthalene ring, can be substituted with above-mentioned 1 to 4 C1-C6 alkyl].

The C1-C6 alkyl that carbamyl C1-C6 alkoxyl group replaces is [wherein on this amino; can be substituted with at least one group; it is selected from by C3-C8 cycloalkyl and phenyl (wherein on this benzyl ring; can be substituted with at least one group; it is selected from by halogen atom; halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group) group formed] example can comprise the C1-C6 alkyl that carbamyl C1-C6 alkoxyl group replaces; carbamyl methoxymethyl for example; 2-(carbamyl oxyethyl group) methyl; (3-carbamyl propoxy-) methyl; (2-carbamyl propoxy-) methyl; (4-carbamyl butoxy) methyl; (5-carbamyl pentyloxy) methyl; (4-carbamyl pentyloxy) methyl; (6-carbamyl hexyloxy) methyl; (2-carbamyl methoxyl group) ethyl; 1-(2-carbamyl oxyethyl group) ethyl; 3-(3-carbamyl propoxy-) propyl group; 4-(2-carbamyl propoxy-) butyl; 5-(carbamyl methoxyl group) amyl group; 4-(2-carbamyl propoxy-) butyl; 6-(4-carbamyl butoxy) hexyl; 1; 1-dimethyl-2-(5-carbamyl pentyloxy) ethyl; 2-methyl-3-(4-carbamyl pentyloxy) propyl group; 2-(6-carbamyl hexyloxy) ethyl; (N-(4-aminomethyl phenyl) carbamyl) methoxymethyl; (N-(4-chloro-phenyl-) carbamyl) methoxymethyl; (N-(4-trifluoromethyl) carbamyl) methoxymethyl; (N-(4-p-methoxy-phenyl) carbamyl) methoxymethyl; (N-(4-Trifluoromethoxyphen-l) carbamyl) methoxymethyl; (N-(2; the 4-dichlorophenyl)-and carbamyl) methoxymethyl; (N-(2; 4; the 6-trimethylphenyl) methoxymethyl carbamyl); (N-(2; the 4-Dimethoxyphenyl) methoxymethyl carbamyl); (N-cyclohexyl carbamyl) methoxymethyl; (N-cyclopentyl carbamyl) methoxymethyl; (N-suberyl carbamyl) methoxymethyl; (N-ring octyl group carbamyl) methoxymethyl; (N-cyclobutyl carbamyl) methoxymethyl; (N-cyclopropyl carbamyl) methoxymethyl; (N-cyclopropyl-N-cyclohexyl carbamyl) methoxymethyl; (N; N-dicyclohexyl carbamyl) methoxymethyl; (N-cyclopropyl-N-(4-methyl fluoride phenyl) carbamyl)-methoxymethyl and (N-cyclohexyl-N-(4-methyl fluoride phenyl) carbamyl) methoxymethyl are (wherein on this amino; can be substituted with 1 or 2 group; it is selected from by above-mentioned C3-C8 cycloalkyl and above-mentioned phenyl [wherein on this benzyl ring; can be substituted with 1 to 5; preferred 1 to 3 group, it is selected from by halogen atom; halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group] group formed).

The C1-C6 alkyl that benzofuryl C1-C6 alkoxyl group replaces is [wherein on this cumarone ring, can be substituted with at least one cyano group] example can comprise the C1-C6 alkyl that benzofuryl C1-C6 alkoxyl group replaces, (2-benzofuryl) methoxymethyl for example, (2-(3-benzofuryl) oxyethyl group) methyl, (3-(4-benzofuryl) propoxy-) methyl, (2-(5-benzofuryl) propoxy-) methyl, (4-(6-benzofuryl) butoxy) methyl, (5-(7-benzofuryl) pentyloxy) methyl, (4-(2-benzofuryl) pentyloxy) methyl, (6-(3-benzofuryl) hexyloxy) methyl, (2-(2-benzofuryl) methoxyl group) ethyl, 1-(2-(3-benzofuryl) oxyethyl group) ethyl, 3-(3-(4-benzofuryl) propoxy-) propyl group, 4-(2-(5-benzofuryl) propoxy-) butyl, 5-(4-(6-benzofuryl) butoxy) amyl group, 6-(5-(7-benzofuryl) pentyloxy) hexyl, 1,1-dimethyl-2-(4-(2-benzofuryl) pentyloxy) ethyl, 2-methyl-3-(6-(3-benzofuryl) hexyloxy) propyl group, (7-cyano group-2-benzofuryl) methoxymethyl, (6-cyano group-2-benzofuryl) methoxymethyl, (5-cyano group-2-benzofuryl) methoxymethyl, (4-cyano group-2-benzofuryl) methoxymethyl, (3-cyano group-2-benzofuryl) methoxymethyl, (2-cyano group-5-benzofuryl) methoxymethyl, (6,7-dicyano-2-benzofuryl) methoxymethyl and (3,4,5-tricyano-2-benzofuryl) methoxymethyl [wherein on this cumarone ring, can be substituted with 1 to 3 cyano group].

The example of C7-C10 alkoxyl group can comprise oxygen base in positive heptan, n-octyloxy, positive ninth of the ten Heavenly Stems oxygen base, n-decyloxy, 5-methyl hexyloxy, 4,4-dimethyl pentyloxy, 6-methyl oxygen in heptan base and 5,5,5-trimethylpentyloxy.

Phenoxy group is [wherein on this benzyl ring, be substituted with at least one and be selected from following group: phenyl C1-C6 alkoxyl group, the C3-C8 cycloalkyl, the group that C7-C10 alkoxyl group and phenoxy group are formed] example can comprise phenoxy group, 4-benzyloxy phenoxy group for example, 4-cyclohexyl phenoxy group, 4-n-octyloxy phenoxy group, 4-cyclopentyl phenoxy group, 3-phenoxy group phenoxy group, 3-benzyloxy phenoxy group, 3-cyclohexyl phenoxy group, 3-n-octyloxy phenoxy group, 3-cyclopentyl phenoxy group, 4-phenoxy group phenoxy group, 2-benzyloxy phenoxy group, 2-cyclohexyl phenoxy group, 2-oxygen phenoxyl in positive heptan, 2-cyclopentyl phenoxy group, 2-phenoxy group phenoxy group, 4-(2-phenyl ethoxy) phenoxy group, 4-encircles Octylphenoxy, 4-oxygen phenoxyl in the positive ninth of the ten Heavenly Stems, 4-cyclopropyl phenoxy group, 2,3-hexichol oxygen phenoxyl, 4-(3-phenyl propoxy-) phenoxy group, 4-suberyl phenoxy group, 4-n-decyloxy phenoxy group, 4-cyclobutyl phenoxy group, 2,4,6-triple phenoxyl phenoxy group, 4-(4-phenyl butoxy) phenoxy group, 2,4-dicyclohexyl phenoxy group, 2,4-two-n-octyloxy phenoxy group, 2,4,6-three cyclopentyl phenoxy groups, 3-phenoxy group-4-benzyloxy phenoxy group, 4-(5-phenyl pentyloxy) phenoxy group, 4-cyclohexyl-3-phenoxy group phenoxy group, 2,4,6-three-n-octyloxy phenoxy group, 4-cyclopentyl-2-benzyloxy phenoxy group, 3-phenoxy group-2-cyclohexyl phenoxy group, 4-(6-phenyl hexyloxy) phenoxy group, 3,4,5-three benzyloxy phenoxy groups and 2,4-benzyloxy phenoxy group, its condition is on this benzyl ring, be substituted with 1 to 3 group, it is selected from by above-mentioned phenyl C1-C6 alkoxyl group, above-mentioned C3-C8 cycloalkyl, the group that above-mentioned C7-C10 alkoxyl group and above-mentioned phenoxy group are formed.

2,3-Dihydrobenzofuranes oxygen base [wherein this 2, on the 3-Dihydrobenzofuranes ring, can be substituted with at least one oxo base] example can comprise 2,3-Dihydrobenzofuranes oxygen base, for example (2-, 3-, 4-, 5-, 6-or 7-) 2,3-Dihydrobenzofuranes oxygen base, 3-oxo-6-2,3-Dihydrobenzofuranes oxygen base and 2-oxo-5-2,3-Dihydrobenzofuranes oxygen base, its condition be this 2, on the 3-Dihydrobenzofuranes ring, can be substituted with 1 or 2 oxo base.

Benzothiazole oxygen base is [wherein on this benzothiazole ring, can be substituted with at least one C1-C6 alkyl] example can comprise benzothiazole oxygen base, (2-for example, 4-, 5-, 6-or 7-) benzothiazole oxygen base, 2-methyl-5-benzothiazole oxygen base, 2-ethyl-5-benzothiazole oxygen base, 2-n-propyl-5-benzothiazole oxygen base, the 2-tertiary butyl-5-benzothiazole oxygen base, 2-n-pentyl-5-benzothiazole oxygen base, 2-n-hexyl-5-benzothiazole oxygen base, 2,5-dimethyl-6-benzothiazole oxygen base and 4,5,6-trimethylammonium-2-[4-morpholinodithio oxygen base, its condition is on this benzothiazole ring, can be substituted with above-mentioned 1 to 3 C1-C6 alkyl.

Furyl C1-C6 alkoxyl group is [wherein on this furan nucleus, can be substituted with at least one C1-C6 alkoxy carbonyl] example can comprise furyl C1-C6 alkoxyl group, (2-or 3-) furyl methoxyl group for example, 2-((2-or 3-) furyl) oxyethyl group, 1-((2-or 3-) furyl) oxyethyl group, 3-((2-or 3-) furyl) propoxy-, 2-((2-or 3-) furyl) propoxy-, 4-((2-or 3-) furyl) butoxy, 5-((2-or 3-) furyl) pentyloxy, 4-((2-or 3-) furyl) pentyloxy, 6-((2-or 3-) furyl) hexyloxy, 2-methyl-3-((2-or 3-) furyl) propoxy-, 1,1-dimethyl-2-((2-or 3-) furyl) oxyethyl group, 2-ethoxy carbonyl-5-furyl methoxyl group, 2-ethoxy carbonyl-5-furyl methoxyl group, 2-methoxycarbonyl-4-furyl methoxyl group, 2-propoxycarbonyl-3-furyl methoxyl group, 2-butoxy carbonyl-5-furyl methoxyl group, 2-pentyloxy carbonyl-5-furyl methoxyl group, 2-hexyloxy carbonyl-5-furyl methoxyl group, 2,3-di ethoxy carbonyl-5-furyl methoxyl group and 2,3,4-trimethoxy carbonyl-5-furyl methoxyl group, its condition is on this furan nucleus, can be substituted with above-mentioned 1 to 3 C1-C6 alkoxy carbonyl.

Tetrazyl C1-C6 alkoxyl group is [wherein on this tetrazole ring, can be substituted with at least one group, it is selected from the group of being made up of phenyl C1-C6 alkyl and C3-C8 cycloalkyl C1-C6 alkyl] example can comprise tetrazyl C1-C6 alkoxyl group, (1-for example, 2-or 5-) the tetrazyl methoxyl group, 2-((1-, 2-or 5-) tetrazyl) oxyethyl group, 1-((1-, 2-or 5-) tetrazyl) oxyethyl group, 3-((1-, 2-or 5-) tetrazyl) propoxy-, 2-((1-, 2-or 5-) tetrazyl) propoxy-, 4-((1-, 2-or 5-) tetrazyl) butoxy, 5-((1-, 2-or 5-) tetrazyl) pentyloxy, 4-((1-, 2-or 5-) tetrazyl) pentyloxy, 6-((1-, 2-or 5-) tetrazyl) hexyloxy, 2-methyl-3-((1-, 2-or 5-) tetrazyl) propoxy-, 1,1-dimethyl-2-((1-, 2-or 5-) tetrazyl) oxyethyl group, 1-(2-phenylethyl)-5-tetrazyl methoxyl group, 1-cyclohexyl methyl-5-tetrazyl methoxyl group, 5-benzyl-1-tetrazyl methoxyl group, 5-(2-cyclopentyl ethyl)-1-tetrazyl methoxyl group, 1-benzyl-5-tetrazyl methoxyl group, 1-(3-phenyl propyl)-5-tetrazyl methoxyl group, 1-(4-phenyl butyl)-5-tetrazyl methoxyl group, 1-(5-phenylpentyl)-5-tetrazyl methoxyl group, 1-(6-phenyl hexyl)-5-tetrazyl methoxyl group, 1-cyclobutylmethyl-5-tetrazyl methoxyl group, 1-(3-cyclopropyl propyl group)-5-tetrazyl methoxyl group, 1-(4-suberyl butyl)-5-tetrazyl methoxyl group, 1-(5-ring octyl group amyl group)-5-tetrazyl methoxyl group and 1-(6-cyclohexyl hexyl)-5-tetrazyl methoxyl group, its condition is on this tetrazole ring, can be substituted with a group that is selected from above-mentioned phenyl C1-C6 alkyl and the above-mentioned C3-C8 cycloalkyl C1-C6 alkyl.

1,2,4-_ di azoly C1-C6 alkoxyl group [wherein this 1,2, on the 4-_ diazole ring, can be substituted with phenyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, the group that halogen replacement or unsubstituted C1-C6 alkyl and halogen replacement or unsubstituted C1-C6 alkoxyl group are formed)] example can comprise 1,2,4-_ di azoly C1-C6 alkoxyl group, (3-or 5-) 1 for example, 2,4-_ di azoly methoxyl group, 2-((3-or 5-) 1,2, the 4-_ di azoly) oxyethyl group, 1-((3-or 5-) 1,2, the 4-_ di azoly) oxyethyl group, 3-((3-or 5-) 1,2, the 4-_ di azoly) propoxy-, 2-((3-or 5-) 1,2, the 4-_ di azoly) propoxy-, 4-((3-or 5-) 1,2, the 4-_ di azoly) butoxy, 5-((3-or 5-) 1,2, the 4-_ di azoly) pentyloxy, 4-((3-or 5-) 1,2, the 4-_ di azoly) pentyloxy, 6-((3-or 5-) 1,2, the 4-_ di azoly) hexyloxy, 2-methyl-3-((3-or 5-) 1,2, the 4-_ di azoly) propoxy-, 1,1-dimethyl-2-((3-or 5-) 1,2, the 4-_ di azoly) oxyethyl group, 3-(4-tert-butyl-phenyl)-5-1,2,4-_ di azoly methoxyl group, 3-phenyl-5-1,2,4-_ di azoly methoxyl group, 3-(4-chloro-phenyl-)-5-1,2,4-_ di azoly methoxyl group, 3-(4-trifluoromethyl)-5-1,2,4-_ di azoly methoxyl group, 5-(4-Trifluoromethoxyphen-l)-3-1,2,4-_ di azoly methoxyl group, 5-(4-p-methoxy-phenyl)-3-1,2,4-_ di azoly methoxyl group, 5-(2, the 4-3,5-dimethylphenyl)-3-1,2,4-_ di azoly methoxyl group, 3-(2,4, the 6-trimethylphenyl)-5-1,2,4-_ di azoly methoxyl group, 3-(2, the 4-3,5-dimethylphenyl)-and 5-1,2,4-_ di azoly methoxyl group, 5-(2,4, the 6-trimethoxyphenyl)-and 3-1,2,4-_ di azoly methoxyl group, 3-(2, the 4-dibromo phenyl)-5-1,2,4-_ di azoly methoxyl group, 3-(2,4, the 6-trifluorophenyl)-5-1,2,4-_ di azoly methoxyl group, 3-(3, the 5-dichlorophenyl)-5-1,2,4-_ di azoly methoxyl group, 3-(2-methyl-5-chloro phenyl)-5-1,2,4-_ di azoly methoxyl group, 3-(3-methoxyl group-5-chloro-phenyl-)-5-1,2,4-_ di azoly methoxyl group and 3-(2,3,4,5, the 6-pentafluorophenyl group)-and 5-1,2,4-_ di azoly methoxyl group, its condition be this 1,2, on the 4-_ diazole ring, can be substituted with above-mentioned phenyl (wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed).

The example of benzothienyl C1-C6 alkoxyl group [wherein on this thionaphthene ring, can be substituted with at least one halogen atom] can comprise benzothienyl C1-C6 alkoxyl group, for example (2-, 3-, 4-, 5-, 6-or 7-) the thionaphthene ylmethoxy, 2-((2-, 3-, 4-, 5-, 6-or 7-) benzothienyl) oxyethyl group, 1-((2-, 3-, 4-, 5-, 6-or 7-) benzothienyl) oxyethyl group, 3-((2-, 3-, 4-, 5-, 6-or 7-) benzothienyl) propoxy-, 2-((2-, 3-, 4-, 5-, 6-or 7-) benzothienyl) propoxy-, 4-((2-, 3-, 4-, 5-, 6-or 7-) benzothienyl)-butoxy, 5-((2-, 3-, 4-, 5-, 6-or 7-) benzothienyl) pentyloxy, 4-((2-, 3-, 4-, 5-, 6-or 7-) benzothienyl) pentyloxy, 6-((2-, 3-, 4-, 5-, 6-or 7-) benzothienyl) hexyloxy, 2-methyl-3-((2-, 3-, 4-, 5-, 6-or 7-) benzothienyl) propoxy-, 1,1-dimethyl-2-((2-, 3-, 4-, 5-, 6-or 7-) benzothienyl) oxyethyl group, 5-chloro-3-thionaphthene ylmethoxy, 4-bromo-2-thionaphthene ylmethoxy, 6-fluoro-5-thionaphthene ylmethoxy, 7-iodo-4-1,2,4-_ di azoly methoxyl group, 4,5-two chloro-3-thionaphthene ylmethoxies and 3,4,5-three fluoro-2-thionaphthene ylmethoxies, its condition is on this thionaphthene ring, can be substituted with 1 to 3 halogen atom.

Different _ azoles base C1-C6 alkoxyl group [wherein on this different _ azoles ring, can be substituted with at least one C1-C6 alkyl] example can comprise different _ azoles base C1-C6 alkoxyl group, (3-for example, 4-or 5-) different _ the azoles ylmethoxy, 2-((3-, 4-or 5-) different _ the azoles base) oxyethyl group, 1-((3-, 4-or 5-) different _ the azoles base) oxyethyl group, 3-((3-, 4-or 5-) different _ the azoles base) propoxy-, 2-((3-, 4-or 5-) different _ the azoles base) propoxy-, 4-((3-, 4-or 5-) different _ the azoles base) butoxy, 5-((3-, 4-or 5-) different _ the azoles base) pentyloxy, 4-((3-, 4-or 5-) different _ the azoles base) pentyloxy, 6-((3-, 4-or 5-) different _ the azoles base) hexyloxy, 2-methyl-3-((3-, 4-or 5-) different _ the azoles base) propoxy-, 1,1-dimethyl-2-((3-, 4-or 5-) different _ the azoles base) oxyethyl group, (3,5-dimethyl-4-is different _ the azoles base) and methoxyl group, (3-methyl-5-different _ azoles base) methoxyl group, (4-ethyl-5-different _ azoles base) methoxyl group, (5-n-propyl-4-different _ azoles base) methoxyl group, (the 3-tertiary butyl-4-different _ azoles base) methoxyl group, (4-n-pentyl-5-different _ azoles base) methoxyl group and (5-n-hexyl-5-different _ azoles base) methoxyl group, its condition is on this different _ azoles ring, can be substituted with above-mentioned 1 or 2 C1-C6 alkyl.

1,3,4-_ di azoly C1-C6 alkoxyl group [wherein this 1,3, on the 4-_ diazole ring, can be substituted with at least one phenyl (wherein on this benzyl ring, can be substituted with at least one C1-C6 alkyl)] example can comprise 1,3,4-_ di azoly C1-C6 alkoxyl group, 2-1 for example, 3,4-_ di azoly methoxyl group, 2-(2-1,3, the 4-_ di azoly) oxyethyl group, 1-(2-1,3, the 4-_ di azoly) oxyethyl group, 3-(2-1,3, the 4-_ di azoly) propoxy-, 2-(2-1,3, the 4-_ di azoly) propoxy-, 4-(2-1,3, the 4-_ di azoly) butoxy, 5-(2-1,3, the 4-_ di azoly) pentyloxy, 4-(2-1,3, the 4-_ di azoly) pentyloxy, 6-(2-1,3, the 4-_ di azoly) hexyloxy, 2-methyl-3-(2-1,3,4-is different _ the azoles base) and propoxy-, 1,1-dimethyl-2-(2-1,3,4-_ di azoly) oxyethyl group, 2-(4-aminomethyl phenyl)-5-1,3,4-_ di azoly methoxyl group, 3-phenyl-5-1,3,4-_ di azoly methoxyl group, 2-(4-ethylphenyl)-5-1,3,4-_ di azoly methoxyl group, 3-(4-n-propyl phenyl)-5-1,3,4-_ di azoly methoxyl group, 3-(4-secondary butyl phenenyl)-5-1,3,4-_ di azoly methoxyl group, 3-(4-n-pentyl phenyl)-5-1,3,4-_ di azoly methoxyl group, 3-(2, the 4-3,5-dimethylphenyl)-5-1,3,4-_ di azoly methoxyl group, 3-(2,4, the 6-trimethylphenyl)-5-1,3,4-_ di azoly methoxyl group, 3-(3-n-hexyl phenyl)-5-1,3,4-_ di azoly methoxyl group, 3-(2-aminomethyl phenyl)-5-1,3,4-_ di azoly methoxyl group and 3-(3-aminomethyl phenyl)-5-1,3,4-_ di azoly methoxyl group, its condition be this 1,3, on the 4-_ diazole ring, can be substituted with a phenyl (wherein on this benzyl ring, can be substituted with above-mentioned 1 to 3 C1-C6 alkyl).

The example of naphthyl C1-C6 alkoxyl group can comprise (2-or 3-) naphthyl methoxyl group, 2-((2-or 3-) naphthyl) oxyethyl group, 1-((2-or 3-) naphthyl) oxyethyl group, 3-((2-or 3-) naphthyl)-propoxy-, 2-((2-or 3-) naphthyl) propoxy-, 4-((2-or 3-) naphthyl) butoxy, 5-((2-or 3-) naphthyl) pentyloxy, 4-((1-or 2-) naphthyl) pentyloxy, 6-((2-or 3-) naphthyl) hexyloxy, 2-methyl-3-((2-or 3-) naphthyl) propoxy-and 1,1-dimethyl-2-((2-or 3-) naphthyl) oxyethyl group.

Pyridyl C1-C6 alkoxyl group is (wherein on this pyridine ring, can be substituted with at least one halogen replaces or unsubstituted C1-C6 alkyl) example can comprise pyridyl C1-C6 alkoxyl group, (1-for example, 2-, 3-or 4-) the pyridyl methoxyl group, 2-((1-, 2-, 3-or 4-) pyridyl) oxyethyl group, 1-((1-, 2-, 3-or 4-) pyridyl) oxyethyl group, 3-((1-, 2-, 3-or 4-) pyridyl) propoxy-, 2-((1-, 2-, 3-or 4-) pyridyl) propoxy-, 4-((1-, 2-, 3-or 4-) pyridyl) butoxy, 5-((1-, 2-, 3-or 4-) pyridyl) pentyloxy, 4-((1-, 2-, 3-or 4-) pyridyl) pentyloxy, 6-((1-, 2-, 3-or 4-) pyridyl) hexyloxy, 2-methyl-3-((1-, 2-, 3-or 4-) pyridyl) propoxy-, 1,1-dimethyl-2-((1-, 2-, 3-or 4-) pyridyl) oxyethyl group, 2-trifluoromethyl-5-pyridyl methoxyl group, 2-methyl-5-pyridyl methoxyl group, 2-ethyl-6-pyridyl methoxyl group, 3-n-propyl-2-pyridyl methoxyl group, 4-normal-butyl-5-pyridyl methoxyl group, 3-n-pentyl-4-pyridyl methoxyl group, 2-n-hexyl-6-pyridyl methoxyl group, 2,3-two trifluoromethyls-5-pyridyl methoxyl group, 3,4,5-three trifluoromethyls-2-pyridyl methoxyl group, 2,4-dimethyl-5-pyridyl methoxyl group and 3,4,5-trimethylammonium-2-pyridyl methoxyl group, its condition is on this pyridine ring, can be substituted with replace or the unsubstituted C1-C6 alkyl of 1 to 3 halogen.

Thiazolyl C1-C6 alkoxyl group is [wherein on this thiazole ring, can be substituted with at least one phenyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, the group that halogen replacement or unsubstituted C1-C6 alkyl and halogen replacement or unsubstituted C1-C6 alkoxyl group are formed)) example can comprise thiazolyl C1-C6 alkoxyl group, (2-for example, 4-or 5-) the thiazolyl methoxyl group, 2-((2-, 4-or 5-) thiazolyl) oxyethyl group, 1-((2-, 4-or 5-) thiazolyl) oxyethyl group, 3-((2-, 4-or 5-) thiazolyl) propoxy-, 2-((2-, 4-or 5-) thiazolyl) propoxy-, 4-((2-, 4-or 5-) thiazolyl) butoxy, 5-((2-, 4-or 5-) thiazolyl) pentyloxy, 4-((2-, 4-or 5-) thiazolyl) pentyloxy, 6-((2-, 4-or 5-) thiazolyl) hexyloxy, 2-methyl-3-((2-, 4-or 5-) thiazolyl) propoxy-, 1,1-dimethyl-2-((2-, 4-or 5-) thiazolyl) oxyethyl group, 2-(4-trifluoromethyl)-4-thiazolyl methoxyl group, 2-phenyl-4-thiazolyl methoxyl group, 2-(4-chloro-phenyl-)-4-thiazolyl methoxyl group, 2-(4-trifluoromethyl)-5-thiazolyl methoxyl group, 2-(4-Trifluoromethoxyphen-l)-4-thiazolyl methoxyl group, 5-(4-p-methoxy-phenyl)-3-thiazolyl methoxyl group, 5-(2, the 4-3,5-dimethylphenyl)-2-thiazolyl methoxyl group, 4-(2,4, the 6-trimethylphenyl)-2-thiazolyl methoxyl group, 2-(2, the 4-3,5-dimethylphenyl)-5-thiazolyl methoxyl group, 2-(2,4, the 6-trimethoxyphenyl)-4-thiazolyl methoxyl group, 2-(2, the 4-dibromo phenyl)-4-thiazolyl methoxyl group, 2-(2,4, the 6-trifluorophenyl)-5-thiazolyl methoxyl group, 2-(3, the 5-dichlorophenyl)-4-thiazolyl methoxyl group, 2-(2-methyl-5-chloro phenyl)-4-thiazolyl methoxyl group, 2-(3-methoxyl group-5-chloro-phenyl-)-4-thiazolyl methoxyl group, 2-(2,3,4,5, the 6-pentafluorophenyl group)-4-thiazolyl methoxyl group and 2,5-phenylbenzene-4-thiazolyl methoxyl group, its condition is on this thiazole ring, can be substituted with above-mentioned 1 or 2 phenyl (wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed).

1,2,3,4-tetralyl C1-C6 alkoxyl group (wherein this 1,2,3, on the 4-tetrahydric naphthalene ring, can be substituted with at least one C1-C6 alkyl) example can comprise 1,2,3,4-tetralyl C1-C6 alkoxyl group, for example (1-, 2-, 5-or 6-) 1,2,3,4-tetralyl methoxyl group, 2-((1-, 2-, 5-or 6-) 1,2,3, the 4-tetralyl) oxyethyl group, 1-((1-, 2-, 5-or 6-) 1,2,3, the 4-tetralyl) oxyethyl group, 3-((1-, 2-, 5-or 6-) 1,2,3, the 4-tetralyl) propoxy-, 2-((1-, 2-, 5-or 6-) 1,2,3, the 4-tetralyl) propoxy-, 4-((1-or 2-) 1,2,3, the 4-tetralyl) butoxy, 5-((1-or 2-) 1,2,3, the 4-tetralyl) pentyloxy, 4-((1-, 2-, 5-or 6-) 1,2,3, the 4-tetralyl) pentyloxy, 6-((1-, 2-, 5-or 6-) 1,2,3, the 4-tetralyl) hexyloxy, 2-methyl-3-((1-, 2-, 5-or 6-) 1,2,3, the 4-tetralyl) propoxy-, 1,1-dimethyl-2-((1-, 2-, 5-or 6-) 1,2,3, the 4-tetralyl) oxyethyl group, (1,1,4,4-tetramethyl--6-1,2,3, the 4-tetralyl) methoxyl group, (1,1,4-trimethylammonium-6-1,2,3, the 4-tetralyl) methoxyl group, (1,1-dimethyl-6-1,2,3, the 4-tetralyl) methoxyl group, (4,4-dimethyl-6-1,2,3, the 4-tetralyl) methoxyl group, (1-methyl-6-1,2,3, the 4-tetralyl) methoxyl group, (1,4-dimethyl-6-1,2,3, the 4-tetralyl) methoxyl group, (1,1,4,4-tetraethyl--6-1,2,3, the 4-tetralyl) methoxyl group, (1,1-dimethyl-4-ethyl-6-1,2,3, the 4-tetralyl) methoxyl group, (1,1-two-n-propyl-6-1,2,3, the 4-tetralyl) methoxyl group, (4,4-di-n-butyl-6-1,2,3, the 4-tetralyl) methoxyl group, (1-n-pentyl-6-1,2,3, the 4-tetralyl) methoxyl group, (1,4-two-n-hexyl-6-1,2,3, the 4-tetralyl) methoxyl group and (1-methyl-5-n-propyl-4-ethyl-6-1,2,3,4-tetralyl) methoxyl group, its condition be this 1,2,3, on the 4-tetrahydric naphthalene ring, can be substituted with above-mentioned 1 to 4 C1-C6 alkyl.

Phenoxy group C1-C6 alkoxyl group is (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, the group that halogen replacement or unsubstituted C1-C6 alkyl and halogen replacement or unsubstituted C1-C6 alkoxyl group are formed) example can comprise phenoxy group C1-C6 alkoxyl group, phenoxy group methoxyl group for example, 2-phenoxy group oxyethyl group, 1-phenoxy group oxyethyl group, 3-phenoxy group propoxy-, 2-phenoxy group propoxy-, 4-phenoxy group butoxy, 5-phenoxy group pentyloxy, 4-phenoxy group pentyloxy, 6-phenoxy group hexyloxy, 2-methyl-3-phenoxy group propoxy-, 1,1-dimethyl-2-phenoxy group oxyethyl group, 2-fluorophenoxy methoxyl group, 3-fluorophenoxy methoxyl group, 4-fluorophenoxy methoxyl group, 2-(2-fluorophenoxy) oxyethyl group, 2-(3-fluorophenoxy) oxyethyl group, 2-(4-fluorophenoxy) oxyethyl group, 2-chlorophenoxy methoxyl group, 3-chlorophenoxy methoxyl group, 4-chlorophenoxy methoxyl group, 2-fluoro-4-bromobenzene Oxymethoxy, 4-chloro-3-fluorophenoxy methoxyl group, 2-chloro-4-fluorophenoxy methoxyl group, 3,4-Dichlorophenoxy ylmethoxy, 3,5-Dichlorophenoxy ylmethoxy, 2,3-Dichlorophenoxy ylmethoxy, 2,5-Dichlorophenoxy ylmethoxy, 2,3,4-Trichlorophenoxy methoxyl group, 3,4,5-trifluoromethoxy phenoxy ylmethoxy, 2,3,4,5,6-penta fluoro benzene Oxymethoxy, 2,4,6-Trichlorophenoxy methoxyl group, 4-isopropyl benzene Oxymethoxy, 4-n-butylbenzene Oxymethoxy, 4-methylenedioxy phenoxy ylmethoxy, 2-methylenedioxy phenoxy ylmethoxy, 3-methylenedioxy phenoxy ylmethoxy, 2,4-dimethyl phenoxy methoxyl group, 2,3-dimethyl phenoxy methoxyl group, 2,6-dimethyl phenoxy methoxyl group, 3,5-dimethyl phenoxy methoxyl group, 2,5-dimethyl phenoxy methoxyl group, 2,4,6-Three methyl Benzene Oxymethoxy, 4-ethylbenzene Oxymethoxy, 4-isopropyl benzene Oxymethoxy, 3,5-two 4-trifluoromethylphenopendant methoxyl groups, 4-isopropoxy benzene Oxymethoxy, 4-n-butoxy phenoxy group methoxyl group, 4-anisole Oxymethoxy, 2-anisole Oxymethoxy, 3-anisole Oxymethoxy, 2,4-dimethoxy benzene Oxymethoxy, 2,3-dimethoxy benzene Oxymethoxy, 2,6-dimethoxy benzene Oxymethoxy, 3,5-dimethoxy benzene Oxymethoxy, 2,5-dimethoxy benzene Oxymethoxy, 2,4,6-trimethoxy-benzene Oxymethoxy, 3,5-two Trifluoromethyl phenyl ether Oxymethoxies, 2-isopropoxy benzene Oxymethoxy, 3-chloro-4-anisole Oxymethoxy, 2-chloro-4-Trifluoromethyl phenyl ether Oxymethoxy, 3-methyl-4-fluorophenoxy methoxyl group, 4-bromo-3-4-trifluoromethylphenopendant methoxyl group, 2-(2-chlorophenoxy) oxyethyl group, 2-(3-chlorophenoxy) oxyethyl group, 2-(4-chlorophenoxy) oxyethyl group, 2-4-trifluoromethylphenopendant methoxyl group, 3-4-trifluoromethylphenopendant methoxyl group, 4-4-trifluoromethylphenopendant methoxyl group, 2-Trifluoromethyl phenyl ether Oxymethoxy, 3-Trifluoromethyl phenyl ether Oxymethoxy, 4-Trifluoromethyl phenyl ether Oxymethoxy, 2-(2-4-trifluoromethylphenopendant) oxyethyl group, 2-(3-4-trifluoromethylphenopendant) oxyethyl group, 2-(4-4-trifluoromethylphenopendant) oxyethyl group, 2-(2-Trifluoromethyl phenyl ether oxygen base) oxyethyl group, 2-(3-Trifluoromethyl phenyl ether oxygen base) oxyethyl group, 2-(4-Trifluoromethyl phenyl ether oxygen base) oxyethyl group, 3-(2-4-trifluoromethylphenopendant) propoxy-, 3-(3-4-trifluoromethylphenopendant) propoxy-, 3-(4-4-trifluoromethylphenopendant) propoxy-, 3-(2-4-trifluoromethylphenopendant) propoxy-, 3-(3-Trifluoromethyl phenyl ether oxygen base) propoxy-, 3-(4-Trifluoromethyl phenyl ether oxygen base) propoxy-, 4-(3-4-trifluoromethylphenopendant) butoxy, 5-(4-4-trifluoromethylphenopendant) pentyloxy, 4-(4-4-trifluoromethylphenopendant) pentyloxy, 4-(4-Trifluoromethyl phenyl ether oxygen base) pentyloxy, 6-(3-4-trifluoromethylphenopendant) hexyloxy, 6-(4-4-trifluoromethylphenopendant) hexyloxy and 6-(4-Trifluoromethyl phenyl ether oxygen base) hexyloxy, its condition is on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 group, it is selected from by above-mentioned halogen atom, group that above-mentioned halogen replaces or unsubstituted C1-C6 alkyl and the replacement of above-mentioned halogen or that unsubstituted C1-C6 alkoxyl group is formed.

Carbamyl C1-C6 alkoxyl group is [wherein on this amino; can be substituted with at least one group; it is selected from by C3-C8 cycloalkyl and phenyl (wherein on this benzyl ring; can be substituted with at least one group; it is selected from by halogen atom; halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group) group formed] example can comprise carbamyl C1-C6 alkoxyl group; carbamyl methoxyl group for example; 2-carbamyl oxyethyl group; 3-carbamyl propoxy-; 2-carbamyl propoxy-; 4-carbamyl butoxy; 5-carbamyl pentyloxy; 4-carbamyl pentyloxy; 6-carbamyl hexyloxy; 2-methyl-3-carbamyl propoxy-; 1; 1-dimethyl-2-carbamyl oxyethyl group; (N-(4-aminomethyl phenyl) carbamyl) methoxyl group; (N-(4-chloro-phenyl-) carbamyl) methoxyl group; (N-(4-trifluoromethyl) carbamyl) methoxyl group; (N-(4-p-methoxy-phenyl) carbamyl) methoxyl group; (N-(4-Trifluoromethoxyphen-l) carbamyl) methoxyl group; (N-(2; the 4-dichlorophenyl) methoxyl group carbamyl); (N-(2; 4; the 6-trimethylphenyl) methoxyl group carbamyl); (N-(2; the 4-Dimethoxyphenyl) methoxyl group carbamyl); (N-cyclohexyl carbamyl) methoxyl group; (N-cyclopentyl carbamyl) methoxyl group; (N-suberyl carbamyl) methoxyl group; (N-ring octyl group carbamyl) methoxyl group; (N-cyclobutyl carbamyl) methoxyl group; (N-cyclopropyl carbamyl) methoxyl group; (N-cyclopropyl-N-cyclohexyl carbamyl) methoxyl group; (N; N-dicyclohexyl carbamyl) methoxyl group; (N-cyclopropyl-N-(4-methyl fluoride phenyl) carbamyl) methoxyl group and (N-cyclohexyl-N-(4-methyl fluoride phenyl) carbamyl) methoxyl group; its condition is on this amino; can be substituted with 1 or 2 group; it is selected from by above-mentioned C3-C8 cycloalkyl and above-mentioned phenyl (wherein on this benzyl ring; can be substituted with 1 to 5; preferred 1 to 3 group, it is selected from by halogen atom; the group that halogen replacement or unsubstituted C1-C6 alkyl and halogen replacement or unsubstituted C1-C6 alkoxyl group are formed) group of forming.

Benzofuryl C1-C6 alkoxyl group is (wherein on this cumarone ring, can be substituted with at least one cyano group) example can comprise benzofuryl C1-C6 alkyl, (2-benzofuryl) methoxyl group for example, 2-(3-benzofuryl) oxyethyl group, 3-(4-benzofuryl) propoxy-, 2-(5-benzofuryl) propoxy-, 4-(6-benzofuryl) butoxy, 5-(7-benzofuryl) pentyloxy, 4-(2-benzofuryl) pentyloxy, 6-(3-benzofuryl) hexyloxy, 2-(2-benzofuryl) methoxyl group, 1,1-dimethyl-2-(2-benzofuryl) oxyethyl group, 2-methyl-3-(3-benzofuryl) propoxy-, (7-cyano group-2-benzofuryl) methoxyl group, (6-cyano group-2-benzofuryl) methoxyl group, (5-cyano group-2-benzofuryl) methoxyl group, (4-cyano group-2-benzofuryl) methoxyl group, (3-cyano group-2-benzofuryl) methoxyl group, (2-cyano group-5-benzofuryl) methoxyl group and (6,7-dicyano-2-benzofuryl) methoxyl group, (3,4,5-tricyano-2-benzofuryl) methoxyl group, its condition is on this cumarone ring, can be substituted with 1 to 3 cyano group.

Naphthyloxy C1-C6 alkyl is (wherein on this naphthalene nucleus, can be substituted with at least one C1-C6 alkoxyl group) example can comprise naphthyloxy C1-C6 alkyl, (1-or 2-) naphthyloxy methyl for example, 2-((1-or 2-) naphthyloxy) ethyl, 1-((1-or 2-) naphthyloxy) ethyl, 3-((1-or 2-) naphthyloxy) propyl group, 2-((1-or 2-) naphthyloxy) butyl, 5-((1-or 2-) naphthyloxy) amyl group, 4-((1-or 2-) naphthyloxy) amyl group, 6-((1-or 2-) naphthyloxy) hexyl, 2-methyl-3-((1-or 2-) naphthyloxy) propyl group, 1,1-dimethyl-2-((1-or 2-) naphthyloxy) ethyl, 2-(4-methoxyl group-1-naphthyloxy) ethyl, (4-methoxyl group-1-naphthyloxy) methyl, 2-(3-oxyethyl group-1-naphthyloxy) ethyl, 2-positive propoxy-1-naphthyloxy methyl, 5-tert.-butoxy-2-naphthyloxy methyl, 6-n-pentyloxy-3-naphthyloxy methyl, the positive hexyloxy of 7--4-naphthyloxy methyl, 2-(2,4-dimethoxy-1-naphthyloxy) ethyl and 2-(1,2,3,4-tetramethoxy-5-naphthyloxy) ethyl, its condition is on this naphthalene nucleus, can be substituted with above-mentioned 1 to 4 C1-C6 alkoxyl group.

Benzothiazole oxygen base C1-C6 alkyl is (wherein on this benzothiazole ring, can be substituted with at least one C1-C6 alkyl) example can comprise benzothiazole oxygen base C1-C6 alkyl, (2-for example, 4-, 5-, 6-or 7-) benzothiazole oxygen ylmethyl, 2-((2-, 4-, 5-, 6-or 7-) benzothiazole oxygen base) ethyl, 1-((2-, 4-, 5-, 6-or 7-) benzothiazole oxygen base) ethyl, 3-((2-, 4-, 5-, 6-or 7-) benzothiazole oxygen base) propyl group, 2-((2-, 4-, 5-, 6-or 7-) benzothiazole oxygen base) propyl group, 4-((2-, 4-, 5-, 6-or 7-) benzothiazole oxygen base)-butyl, 5-((2-, 4-, 5-, 6-or 7-) benzothiazole oxygen base) amyl group, 4-((2-, 4-, 5-, 6-or 7-) benzothiazole oxygen base) amyl group, 6-((2-, 4-, 5-, 6-or 7-) benzothiazole oxygen base) hexyl, 2-methyl-3-((2-, 4-, 5-, 6-or 7-) benzothiazole oxygen base) propyl group, 1,1-dimethyl-2-((2-, 4-, 5-, 6-or 7-) benzothiazole oxygen base) ethyl, 2-(2-methyl-5-benzothiazole oxygen base) ethyl, (2-methyl-5-benzothiazole oxygen base) methyl, 2-(4-ethyl-6-benzothiazole oxygen base) ethyl, (2-n-propyl-4-benzothiazole oxygen base) methyl, (the 5-tertiary butyl-6-benzothiazole oxygen base) methyl, (6-n-pentyl-7-benzothiazole oxygen base) methyl, (7-n-hexyl-5-benzothiazole oxygen base) methyl, 2-(2,4-dimethyl-5-benzothiazole oxygen base) ethyl and 2-(2,4,5-trimethylammonium-7-benzothiazole oxygen base) ethyl, its condition is on this benzothiazole ring, can be substituted with above-mentioned 1 to 3 C1-C6 alkyl.

The example of quinoline oxy C1-C6 alkyl (wherein on this quinoline ring, can be substituted with at least one C1-C6 alkyl) can comprise quinoline oxy C1-C6 alkyl, for example (2-, 3-, 4-, 5-, 6-, 7-or 8-) the quinoline oxy methyl, 2-((2-, 3-, 4-, 5-, 6-, 7-or 8-) quinoline oxy) ethyl, 1-((2-, 3-, 4-, 5-, 6-, 7-or 8-) quinoline oxy) ethyl, 3-((2-, 3-, 4-, 5-, 6-, 7-or 8-) quinoline oxy) propyl group, 2-((2-, 3-, 4-, 5-, 6-, 7-or 8-) quinoline oxy) propyl group, 4-((2-, 3-, 4-, 5-, 6-, 7-or 8-) quinoline oxy) butyl, 5-((2-, 3-, 4-, 5-, 6-, 7-or 8-) quinoline oxy) amyl group, 4-((2-, 3-, 4-, 5-, 6-, 7-or 8-) quinoline oxy) amyl group, 6-((2-, 3-, 4-, 5-, 6-, 7-or 8-) quinoline oxy) hexyl, 2-methyl-3-((2-, 3-, 4-, 5-, 6-, 7-or 8-) quinoline oxy) propyl group, 1,1-dimethyl-2-((2-, 3-, 4-, 5-, 6-, 7-or 8-) quinoline oxy) ethyl, 2-methyl-8-quinoline oxy methyl, (3-ethyl-7-quinoline oxy) methyl, (4-n-propyl-6-quinoline oxy) methyl, (5-normal-butyl-4-quinoline oxy) methyl, (6-n-hexyl-5-quinoline oxy) methyl, (2-methyl-7-quinoline oxy) methyl, (7-n-pentyl-6-quinoline oxy) methyl, (8-methyl-2-quinoline oxy methyl), (2,4-dimethyl-8-quinoline oxy) methyl and (5,6,7-trimethylammonium-2-quinoline oxy) methyl, its condition are on this quinoline ring, can be substituted with above-mentioned 1 to 3 C1-C6 alkyl.

2,3-Dihydrobenzofuranes oxygen base C1-C6 alkyl (wherein this 2, on the 3-Dihydrobenzofuranes ring, can be substituted with at least one group, it is selected from the group of being made up of C1-C6 alkyl and oxo base) example can comprise 2,3-Dihydrobenzofuranes oxygen base C1-C6 alkyl, (2-for example, 3-, 4-, 5-, 6-or 7-) 2,3-Dihydrobenzofuranes oxygen ylmethyl, 2-((2-, 3-, 4-, 5-, 6-or 7-) 2,3-Dihydrobenzofuranes oxygen base) ethyl, 1-((2-, 3-, 4-, 5-, 6-or 7-) 2,3-Dihydrobenzofuranes oxygen base) ethyl, 3-((2-, 3-, 4-, 5-, 6-or 7-) 2,3-Dihydrobenzofuranes oxygen base) propyl group, 2-((2-, 3-, 4-, 5-, 6-or 7-) 2,3-Dihydrobenzofuranes oxygen base) propyl group, 4-((2-, 3-, 4-, 5-, 6-or 7-) 2,3-Dihydrobenzofuranes oxygen base) butyl, 5-((2-, 3-, 4-, 5-, 6-or 7-) 2,3-Dihydrobenzofuranes oxygen base) amyl group, 4-((2-, 3-, 4-, 5-, 6-or 7-) 2,3-Dihydrobenzofuranes oxygen base) amyl group, 6-((2-, 3-, 4-, 5-, 6-or 7-) 2,3-Dihydrobenzofuranes oxygen base) hexyl, 2-methyl-3-((2-, 3-, 4-, 5-, 6-or 7-) 2,3-Dihydrobenzofuranes oxygen base) propyl group, 1,1-dimethyl-2-((2-, 3-, 4-, 5-, 6-or 7-) 2,3-Dihydrobenzofuranes oxygen base) ethyl, 2-(2,2-dimethyl-7-2,3-Dihydrobenzofuranes oxygen base) ethyl, (2,2-dimethyl-7-2,3-Dihydrobenzofuranes oxygen base) methyl, 2-(3-ethyl-6-2,3-Dihydrobenzofuranes oxygen base) ethyl, (4-n-propyl-5-2,3-Dihydrobenzofuranes oxygen base) methyl, (the 5-tertiary butyl-6-2,3-Dihydrobenzofuranes oxygen base) methyl, (6-n-pentyl-7-2,3-Dihydrobenzofuranes oxygen base) methyl, (7-n-hexyl-5-2,3-Dihydrobenzofuranes oxygen base) methyl, 2-(2,4-dimethyl-5-2,3-Dihydrobenzofuranes oxygen base) ethyl, 2-(2,2,3-trimethylammonium-7-2,3-Dihydrobenzofuranes oxygen base) ethyl, (2-oxo-5-2,3-Dihydrobenzofuranes oxygen base) methyl, (3-oxo-6-2,3-Dihydrobenzofuranes oxygen base) methyl and (2-oxo-3-methyl-5-2,3-Dihydrobenzofuranes oxygen base) methyl, its condition be this 2, on the 3-Dihydrobenzofuranes ring, can be substituted with 1 to 3 group, it is selected from the group of being made up of above-mentioned C1-C6 alkyl and oxo base.

1,2,3,4-tetrahydrochysene naphthyloxy C1-C6 alkyl (wherein this 1,2,3, on the 4-tetrahydric naphthalene ring, can be substituted with at least one oxo base) example can comprise 1,2,3,4-tetrahydrochysene naphthyloxy C1-C6 alkyl, for example (1-, 2-, 5-or 6-) 1,2,3,4-naphthane oxygen ylmethyl, 2-((1-, 2-, 5-or 6-) 1,2,3,4-tetrahydrochysene naphthyloxy) ethyl, 1-((1-, 2-, 5-or 6-) 1,2,3,4-tetrahydrochysene naphthyloxy) ethyl, 3-((1-, 2-, 5-or 6-) 1,2,3,4-tetrahydrochysene naphthyloxy) propyl group, 2-((1-, 2-, 5-or 6-) 1,2,3,4-tetrahydrochysene naphthyloxy) propyl group, 4-((1-, 2-, 5-or 6-) 1,2,3,4-tetrahydrochysene naphthyloxy) butyl, 5-((1-, 2-, 5-or 6-) 1,2,3,4-tetrahydrochysene naphthyloxy) amyl group, 4-((1-or 2-) 1,2,3,4-tetrahydrochysene naphthyloxy) amyl group, 6-((1-or 2-) 1,2,3,4-tetrahydrochysene naphthyloxy) hexyl, 2-methyl-3-((1-, 2-, 5-or 6-) 1,2,3,4-tetrahydrochysene naphthyloxy) propyl group, 1,1-dimethyl-2-((1-, 2-, 5-or 6-) 1,2,3,4-tetrahydrochysene naphthyloxy) ethyl, (1-oxo-(2-, 5-or 6-) 1,2,3,4-tetrahydrochysene naphthyloxy) methyl, (1,4-dioxo-(2-, 5-or 6-) 1,2,3,4-tetrahydrochysene naphthyloxy) methyl and 1,2,4-trioxy--(3-, 5-, 6-, 7-or 8-) 1,2,3,4-tetrahydrochysene naphthyloxy) methyl, its condition be this 1,2,3, on the 4-tetrahydric naphthalene ring, can be substituted with 1 to 3 oxo base.

2,3-dihydro-1H-indenes oxygen base C1-C6 alkyl (wherein this 2, on 3-dihydro-1H-indenes ring, can be substituted with at least one oxo base) example can comprise 2,3-dihydro-1H-indenes oxygen base C1-C6 alkyl, for example (1-, 2-, 4-or 5-) 2,3-dihydro-1H-indenes oxygen ylmethyl, 2-((1-, 2-, 4-or 5-) 2,3-dihydro-1H-indenes oxygen base) ethyl, 1-((1-, 2-, 4-or 5-) 2,3-dihydro-1H-indenes oxygen base) ethyl, 3-((1-, 2-, 4-or 5-) 2,3-dihydro-1H-indenes oxygen base) propyl group, 2-((1-, 2-, 4-or 5-) 2,3-dihydro-1H-indenes oxygen base) propyl group, 4-((1-, 2-, 4-or 5-) 2,3-dihydro-1H-indenes oxygen base) butyl, 5-((1-, 2-, 4-or 5-) 2,3-dihydro-1H-indenes oxygen base) amyl group, 4-((1-, 2-, 4-or 5-) 2,3-dihydro-1H-indenes oxygen base) amyl group, 6-((1-, 2-, 4-or 5-) 2,3-dihydro-1H-indenes oxygen base) hexyl, 2-methyl-3-((1-, 2-, 4-or 5-) 2,3-dihydro-1H-indenes oxygen base) propyl group, 1,1-dimethyl-2-((1-, 2-, 4-or 5-) 2,3-dihydro-1H-indenes oxygen base) ethyl, (1-oxo-(2-, 3-, 4-, 5-, 6-or 7-) 2,3-dihydro-1H-indenes oxygen base) methyl and (1,3-dioxo-(2-, 4-or 5-) 2,3-dihydro-1H-indenes oxygen base) methyl, its condition be this 2, on 3-dihydro-1H-indenes ring, can be substituted with 1 or 2 oxo base.

Benzo oxathiolane oxygen base (benzoxathiolanyloxy) C1-C6 alkyl is (wherein on this benzo oxathiolane (benzoxathiolane) ring, can be substituted with at least one oxo base) example can comprise benzo oxathiolane oxygen base C1-C6 alkyl, (2-for example, 4-, 5-, 6-or 7-) benzo oxathiolane oxygen ylmethyl, 2-((2-, 4-, 5-, 6-or 7-) benzo oxathiolane oxygen base) ethyl, 1-((2-, 4-, 5-, 6-or 7-) benzo oxathiolane oxygen base) ethyl, 3-((2-, 4-, 5-, 6-or 7-) benzo oxathiolane oxygen base)-propyl group, 2-((2-, 4-, 5-, 6-or 7-) benzo oxathiolane oxygen base) propyl group, 4-((2-, 4-, 5-, 6-or 7-) benzo oxathiolane oxygen base) butyl, 5-((2-, 4-, 5-, 6-or 7-) benzo oxathiolane oxygen base) amyl group, 4-((2-, 4-, 5-, 6-or 7-) benzo oxathiolane oxygen base) amyl group, 6-((2-, 4-, 5-, 6-or 7-) benzo oxathiolane oxygen base) hexyl, 2-methyl-3-((2-, 4-, 5-, 6-or 7-) benzo oxathiolane oxygen base)-propyl group, 1,1-dimethyl-2-((2-, 4-, 5-, 6-or 7-) benzo oxathiolane oxygen base) ethyl and (2-oxo-(4-, 5-, 6-or 7-) benzo oxathiolane oxygen base)-methyl, its condition is on this benzo oxathiolane ring, can be substituted with an oxo base.

The example of isoquinoline 99.9 oxygen base C1-C6 alkyl can comprise (1-, 3-, 4-, 5-, 6-, 7-or 8-) isoquinoline 99.9 oxygen ylmethyl, 2-((1-, 3-, 4-, 5-, 6-, 7-or 8-) isoquinoline 99.9 oxygen base) ethyl, 1-((1-, 3-, 4-, 5-, 6-, 7-or 8-) isoquinoline 99.9 oxygen base) ethyl, 3-((1-, 3-, 4-, 5-, 6-, 7-or 8-) isoquinoline 99.9 oxygen base) propyl group, 2-((1-, 3-, 4-, 5-, 6-, 7-or 8-) isoquinoline 99.9 oxygen base) propyl group, 4-((1-, 3-, 4-, 5-, 6-, 7-or 8-) isoquinoline 99.9 oxygen base) butyl, 5-((1-, 3-, 4-, 5-, 6-, 7-or 8-) isoquinoline 99.9 oxygen base) amyl group, 4-((1-, 3-, 4-, 5-, 6-, 7-or 8-) isoquinoline 99.9 oxygen base) amyl group, 6-((1-, 3-, 4-, 5-, 6-, 7-or 8-) isoquinoline 99.9 oxygen base) hexyl, 2-methyl-3-((1-, 3-, 4-, 5-, 6-, 7-or 8-) isoquinoline 99.9 oxygen base) propyl group and 1,1-dimethyl-2-((1-, 3-, 4-, 5-, 6-, 7-or 8-) isoquinoline 99.9 oxygen base) ethyl.

The example of pyridyloxy C1-C6 alkyl can comprise (2-, 3-or 4-) the pyridyloxy methyl, 2-((2-, 3-or 4-) pyridyloxy) ethyl, 1-((2-, 3-or 4-) pyridyloxy) ethyl, 3-((2-, 3-or 4-) pyridyloxy) propyl group, 2-((2-, 3-or 4-) pyridyloxy) propyl group, 4-((2-, 3-or 4-) pyridyloxy) butyl, 5-((2-, 3-or 4-) pyridyloxy) amyl group, 4-((2-, 3-or 4-) pyridyloxy) amyl group, 6-((2-, 3-or 4-) pyridyloxy) hexyl, 2-methyl-3-((2-, 3-or 4-) pyridyloxy) propyl group and 1,1-dimethyl-2-((2-, 3-or 4-) pyridyloxy) ethyl.

The example of diphenylene-oxide oxygen base C1-C6 alkyl can comprise (1-, 2-, 3-or 4-) diphenylene-oxide oxygen base-methyl, 2-((1-, 2-, 3-, 4-, 5-, 6-, 7-or 8-) diphenylene-oxide oxygen base) ethyl, 1-((1-, 2-, 3-or 4-) diphenylene-oxide oxygen base) ethyl, 3-((1-, 2-, 3-or 4-) diphenylene-oxide oxygen base) propyl group, 2-((1-, 2-, 3-or 4-) diphenylene-oxide oxygen base) propyl group, 4-((1-, 2-, 3-or 4-) diphenylene-oxide oxygen base) butyl, 5-((1-, 2-, 3-or 4-) diphenylene-oxide oxygen base) amyl group, 4-((1-, 2-, 3-or 4-) diphenylene-oxide oxygen base) amyl group, 6-((1-, 2-, 3-or 4-) diphenylene-oxide oxygen base) hexyl, 2-methyl-3-((1-, 2-, 3-or 4-) diphenylene-oxide oxygen base) propyl group and 1,1-dimethyl-2-((1-, 2-, 3-or 4-) diphenylene-oxide oxygen base) ethyl.

The example of 2H-1-chromene oxygen base C1-C6 alkyl (wherein on this 2H-1-chromene ring, can be substituted with at least one oxo base) can comprise 2H-1-chromene oxygen base C1-C6 alkyl, for example (2-, 3-, 4-, 5-, 6-, 7-or 8-) 2H-1-chromene oxygen ylmethyl, 2-((2-, 3-, 4-, 5-, 6-, 7-or 8-) 2H-1-chromene oxygen base) ethyl, 1-((2-, 3-, 4-, 5-, 6-, 7-or 8-) 2H-1-chromene oxygen base) ethyl, 3-((2-, 3-, 4-, 5-, 6-, 7-or 8-) 2H-1-chromene oxygen base) propyl group, 2-((2-, 3-, 4-, 5-, 6-, 7-or 8-) 2H-1-chromene oxygen base) propyl group, 4-((2-, 3-, 4-, 5-, 6-, 7-or 8-) 2H-1-chromene oxygen base) butyl, 5-((2-, 3-, 4-, 5-, 6-, 7-or 8-) 2H-1-chromene oxygen base) amyl group, 4-((2-, 3-, 4-, 5-, 6-, 7-or 8-) 2H-1-chromene oxygen base) amyl group, 6-((2-, 3-, 4-, 5-, 6-, 7-or 8-) 2H-1-chromene oxygen base) hexyl, 2-methyl-3-((2-, 3-, 4-, 5-, 6-, 7-or 8-) 2H-1-chromene oxygen base) propyl group, 1,1-dimethyl-2-((2-, 3-, 4-, 5-, 6-, 7-or 8-) 2H-1-chromene oxygen base) ethyl and (2-oxo-(3-, 4-, 5-, 6-, 7-or 8-) 2H-1-chromene oxygen base) methyl, its condition is on this 2H-1-chromene ring, can be substituted with an oxo base.

The example of benzisoxa _ azoles oxygen base C1-C6 alkyl can comprise (3-, 4-, 5-, 6-or 7-) benzisoxa _ azoles oxygen ylmethyl, 2-((3-, 4-, 5-, 6-or 7-) benzisoxa _ azoles oxygen base) ethyl, 1-((3-, 4-, 5-, 6-or 7-) benzisoxa _ azoles oxygen base) ethyl, 3-((3-, 4-, 5-, 6-or 7-) benzisoxa _ azoles oxygen base) propyl group, 2-((3-, 4-, 5-, 6-or 7-) benzisoxa _ azoles oxygen base) propyl group, 4-((3-, 4-, 5-, 6-or 7-) benzisoxa _ azoles oxygen base) butyl, 5-((3-, 4-, 5-, 6-or 7-) benzisoxa _ azoles oxygen base) amyl group, 4-((3-, 4-, 5-, 6-or 7-) benzisoxa _ azoles oxygen base)-amyl group, 6-((3-, 4-, 5-, 6-or 7-) benzisoxa _ azoles oxygen base) hexyl, 2-methyl-3-((3-, 4-, 5-, 6-or 7-) benzisoxa _ azoles oxygen base) propyl group and 1,1-dimethyl-2-((3-, 4-, 5-, 6-or 7-) benzisoxa _ azoles oxygen base) ethyl.

The example of benzo furazan oxygen base (benzofurazanyloxy) C1-C6 alkyl can comprise (4-or 5-) benzo furazan oxygen ylmethyl, 2-((4-or 5-) benzo furazan oxygen base) ethyl, 1-((4-or 5-) benzo furazan oxygen base) ethyl, 3-((4-or 5-) benzo furazan oxygen base) propyl group, 2-((4-or 5-) benzo furazan oxygen base) propyl group, 4-((4-or 5-) benzo furazan oxygen base) butyl, 5-((4-or 5-) benzo furazan oxygen base) amyl group, 4-((4-or 5-) benzo furazan oxygen base) amyl group, 6-((4-or 5-) benzo furazan oxygen base) hexyl, 2-methyl-3-((4-or 5-) benzo furazan oxygen base) propyl group and 1,1-dimethyl-2-((4-or 5-) benzo furazan oxygen base) ethyl.

The example of quinoxaline oxygen base C1-C6 alkyl can comprise (2-, 5-or 6-) quinoxaline oxygen ylmethyl, 2-((2-, 5-or 6-) quinoxaline oxygen base) ethyl, 1-((2-, 5-or 6-) quinoxaline oxygen base) ethyl, 3-((2-, 5-or 6-) quinoxaline oxygen base) propyl group, 2-((2-, 5-or 6-) quinoxaline oxygen base) propyl group, 4-((2-, 5-or 6-) quinoxaline oxygen base) butyl, 5-((2-, 5-or 6-) quinoxaline oxygen base) amyl group, 4-((2-, 5-or 6-) quinoxaline oxygen base) amyl group, 6-((2-, 5-or 6-) quinoxaline oxygen base) hexyl, 2-methyl-3-((2-, 5-or 6-) quinoxaline oxygen base) propyl group and 1,1-dimethyl-2-((2-, 5-or 6-) quinoxaline oxygen base) ethyl.

Phenyl C2-C10 thiazolinyl is [wherein on this benzyl ring; can be substituted with the group that at least one is selected from following groups: halogen atom; the C1-C4 alkylene dioxo base; the C1-C6 alkylthio; benzoyl; cyano group; nitro; the C2-C6 alkanoyloxy; can have the C1-C6 alkyl as substituent amino; hydroxyl; phenyl C1-C6 alkoxyl group; phenoxy group; halogen replaces or unsubstituted C1-C6 alkyl and halogen replace or unsubstituted C1-C6 alkoxyl group] example can comprise that above-mentioned phenyl C2-C6 thiazolinyl is (wherein on this benzyl ring; can be substituted with at least one group; it is selected from by halogen atom; halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed); and contain 2 to 10 carbon atoms and have the thiazolinyl of 1 to 3 two key; wherein on this C2-C10 thiazolinyl; can be substituted with 1 or 2 phenyl; 2-n-pentyl-3-phenyl-2-propenyl for example; 9-phenyl-2-nonene base; 10-phenyl-2-decene base; 8-phenyl-1; the 3-octadienyl; 9-phenyl-1; 3; 5-trialkenyl in the ninth of the ten Heavenly Stems; 10-2; 4; 6-trialkenyl in the last of the ten Heavenly stems; 3-(4-methylthio group phenyl)-2-propenyl; 3-(3-methylthio group phenyl)-2-propenyl; 3-(2-methylthio group phenyl)-2-propenyl; 3-(3; 4-diformazan sulfenyl phenyl)-the 2-propenyl; 3-(3; 4; 5-three methylthio group phenyl)-the 2-propenyl; 3-(4-benzoyl)-2-propenyl; 3-(3-benzoyl)-2-propenyl; 3-(2-benzoyl)-2-propenyl; 3-(3; the 4-dibenzoyl)-the 2-propenyl; 3-(2; 4; the 6-tri-benzoyl)-the 2-propenyl; 3-(4-cyano-phenyl)-2-propenyl; 3-(3-cyano-phenyl)-2-propenyl; 3-(2-cyano-phenyl)-2-propenyl; 3-(3; 4-dicyano phenyl)-the 2-propenyl; 3-(2; 4; 6-tricyano phenyl)-the 2-propenyl; 3-(4-acetoxyl group phenyl)-2-propenyl; 3-(4-acetoxy-3-p-methoxy-phenyl)-2-propenyl; 3-(3-acetoxyl group phenyl)-2-propenyl; 3-(2-acetoxyl group phenyl)-2-propenyl; 3-(3; 4-diacetoxy phenyl)-the 2-propenyl; 3-(2; 4; 6-triacetyl oxygen base phenyl)-the 2-propenyl; 3-(4-dimethylaminophenyl)-2-propenyl; 3-(4-dimethylaminophenyl)-2-propenyl; 3-(3-methylamino phenyl)-2-propenyl; 3-(2-(N-methyl-N-ethylamino) phenyl)-2-propenyl; 3-(2; the 4-dimethylaminophenyl)-the 2-propenyl; 3-(2; 4; 6-three (dimethylamino) phenyl)-the 2-propenyl; 3-(2-hydroxy phenyl)-2-propenyl; 3-(3-hydroxy phenyl)-2-propenyl; 3-(4-hydroxy phenyl)-2-propenyl; 3-(3; 5-dimethyl-4-hydroxy phenyl)-the 2-propenyl; 3-(3-methoxyl group-4-hydroxy phenyl)-2-propenyl; 3-(2-hydroxy phenyl)-2-propenyl; 3-(4-benzyloxy phenyl)-2-propenyl; 3-(4-benzyloxy phenyl)-2-propenyl; 3-(2-benzyloxy phenyl)-2-propenyl; 3-(2; 4; 6-three benzyloxy phenyl)-the 2-propenyl; 3-(3; the 4-benzyloxy phenenyl)-the 2-propenyl; 3-(4-Phenoxyphenyl)-2-propenyl; 3-(3-Phenoxyphenyl)-2-propenyl; 3-(2-Phenoxyphenyl)-2-propenyl; 3-(2; 4-two Phenoxyphenyls)-the 2-propenyl; 3-(2; 4; 6-triple phenoxyl phenyl)-the 2-propenyl; 3-(3; the 4-methylenedioxyphenyl)-the 2-propenyl; 3-(2; 3-ethylenedioxy phenyl)-2-propenyl and 3-(3,4-ethylenedioxy phenyl)-2-propenyl.Above-mentioned phenyl C2-C10 thiazolinyl comprises trans forms and cis form.On this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 group that is selected from following groups: halogen atom, above-mentioned C1-C4 alkylene dioxo base, above-mentioned C1-C6 alkylthio, benzoyl, cyano group, nitro, above-mentioned C2-C6 alkanoyloxy, above-mentionedly can have that the C1-C6 alkyl replaces as substituent amino, hydroxyl, above-mentioned phenyl C1-C6 alkoxyl group, phenoxy group, above-mentioned halogen or unsubstituted C1-C6 alkyl and above-mentioned halogen is that replace or unsubstituted C1-C6 alkoxyl group.Substituting group is under the situation of C1-C4 alkylene dioxo base therein, preferably is substituted with 1 or 2 group on this benzyl ring.

The example of naphthyl C2-C6 thiazolinyl can comprise the thiazolinyl that contains 2 to 6 carbon atoms and have 1 to 3 two key, wherein be substituted with naphthyl, 2-(1-or 2-) naphthyl vinyl for example, 3-(1-or 2-) naphthyl-2-propenyl, 3-(1-or 2-) naphthyl-2-methyl-2-propenyl, 4-(1-or 2-) naphthyl-crotyl, 4-(1-or 2-) naphthyl-3-butenyl, 4-(1-or 2-) naphthyl-1, the 3-butadienyl, 5-(1-or 2-) naphthyl-1, the 3-pentadienyl, 6-(1-or 2-) naphthyl-3-hexadienyl, 6-(1-or 2-) naphthyl-2-hexenyl, 5-(1-or 2-) naphthyl-pentenyl and 6-(1-or 2-) naphthyl-1,3, the 5-hexadienyl.Above-mentioned naphthyl C2-C6 thiazolinyl comprises trans forms and cis form.

The example of benzothienyl C2-C6 thiazolinyl can comprise the thiazolinyl that contains 2 to 6 carbon atoms and have 1 to 3 two key, wherein is substituted with benzothienyl, for example 2-(2-, 3-, 4-, 5-, 6-or 7-) the benzothienyl vinyl, 3-(2-, 3-, 4-, 5-, 6-or 7-) benzothienyl-2-propenyl, 3-(2-, 3-, 4-, 5-, 6-or 7-) benzothienyl-2-methyl-2-propenyl, 4-(2-, 3-, 4-, 5-, 6-or 7-) benzothienyl-crotyl, 4-(2-, 3-, 4-, 5-, 6-or 7-) benzothienyl-3-butenyl, 4-(2-, 3-, 4-, 5-, 6-or 7-) benzothienyl-1, the 3-butadienyl, 5-(2-, 3-, 4-, 5-, 6-or 7-) benzothienyl-1,3-pentadiene base, 6-(2-, 3-, 4-, 5-, 6-or 7-) benzothienyl-1, the 3-hexadienyl, 6-(2-, 3-, 4-, 5-, 6-or 7-) benzothienyl-2-hexenyl, 5-(2-, 3-, 4-, 5-, 6-or 7-) benzothienyl-pentenyl and 6-(2-, 3-, 4-, 5-, 6-or 7-) benzothienyl-1,3,5-hexatriene base.Above-mentioned benzothienyl C2-C6 thiazolinyl comprises trans forms and cis form.

Benzothiazolyl C2-C6 thiazolinyl is [wherein on this benzothiazole ring, can be substituted with at least one C1-C6 alkyl] example can comprise the thiazolinyl that contains 2 to 6 carbon atoms and have 1 to 3 two key, wherein be substituted with benzothiazolyl, 2-(2-for example, 4-, 5-, 6-or 7-) the benzothiazolyl vinyl, 3-(2-, 4-, 5-, 6-or 7-) benzothiazolyl-2-propenyl, 3-(2-, 4-, 5-, 6-or 7-) benzothiazolyl-2-methyl-2-propenyl, 4-(2-, 4-, 5-, 6-or 7-) benzothiazolyl-crotyl, 4-(2-, 4-, 5-, 6-or 7-) benzothiazolyl-3-butenyl, 4-(2-, 4-, 5-, 6-or 7-) benzothiazolyl-1,3-butadiene base, 5-(2-, 4-, 5-, 6-or 7-) benzothiazolyl-1,3-pentadiene base, 6-(2-, 4-, 5-, 6-or 7-) benzothiazolyl-1, the 3-hexadienyl, 6-(2-, 4-, 5-, 6-or 7-) benzothiazolyl-2-hexenyl, 5-(2-, 4-, 5-, 6-or 7-) benzothiazolyl-pentenyl, 6-(2-, 4-, 5-, 6-or 7-) benzothiazolyl-1,3, the 5-hexadienyl, 3-(2-methyl-5-benzothiazolyl)-2-propenyl, 3-(2-ethyl-4-benzothiazolyl)-2-propenyl, 3-(2-n-propyl-6-benzothiazolyl)-2-propenyl, 3-(2-normal-butyl-7-benzothiazolyl)-2-propenyl, 3-(4-n-pentyl-5-benzothiazolyl)-2-propenyl, 3-(5-n-hexyl-2-[4-morpholinodithio base)-2-propenyl, 3-(2,4-dimethyl-5-benzothiazolyl)-2-propenyl and 3-(2,4,5-trimethylammonium-7-benzothiazolyl)-the 2-propenyl.Above-mentioned benzothiazolyl C2-C6 thiazolinyl comprises trans forms and cis form.

Phenyl C1-C6 alkyl is [wherein on this benzyl ring, be substituted with at least one and be selected from following group: piperidyl is (wherein on this piperidine ring, can be substituted with at least one phenoxy group [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group]) and phenoxy group (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group) group formed] example can comprise phenyl C1-C6 alkyl, 4-(piperidino) benzyl for example, 2,4-two (4-piperidyl) benzyl, 2,4,6-three (2-piperidyl) benzyl, 4-(4-(4-Trifluoromethyl phenyl ether oxygen base)-piperidino) benzyl, 4-(4-(4-4-trifluoromethylphenopendant)-piperidino) benzyl, 4-(4-(4-chlorophenoxy)-piperidino) benzyl, (4-(3 for 4-, 4-two (trifluoromethoxy) phenoxy group)-and piperidino) benzyl, (4-(2 for 4-, 4,6-three (trifluoromethyl) phenoxy group)-and piperidino) benzyl, (4-(2 for 4-, the 4-dichlorophenoxy)-and piperidino) benzyl, (4-(2 for 4-, 4,6-trifluoromethoxy phenoxy base)-and piperidino) benzyl, 3-(2,4-two phenoxy groups-3-piperidyl) benzyl, 2-(1,2,3-triple phenoxyl-4-piperidyl) benzyl, 4-(4-Trifluoromethyl phenyl ether oxygen base) benzyl, 4-(4-4-trifluoromethylphenopendant) benzyl, 4-(4-chlorophenoxy) benzyl, 4-(2, the 4-dichlorophenoxy) benzyl, 4-(3,4,5-trifluoromethoxy phenoxy base) benzyl, 4-(3-methylphenoxy) benzyl, 4-(2-methoxyl group phenoxy group) benzyl, 4-(2, the 4-dimethyl phenoxy) benzyl, 4-(3,4-dimethoxy phenoxy group) benzyl, 4-(2,4,6-trimethylammonium phenoxy group) benzyl, 4-(3,4,5-trimethoxy phenoxy group) benzyl, 2,4-two phenoxy benzyls, 2,4,6-triple phenoxyl benzyl and 2-phenoxy group-4-(piperidino) benzyl are [wherein on this benzyl ring, be substituted with 1 to 3 and be selected from following group: above-mentioned piperidyl is (wherein on this piperidine ring, can be substituted with 1 to 3 phenoxy group [wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 group, it is selected from by halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group]) and above-mentioned phenoxy group (wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 group, it is selected from by halogen atom, the group that halogen replacement or unsubstituted C1-C6 alkyl and halogen replacement or unsubstituted C1-C6 alkoxyl group are formed) group of forming].

Phenylbenzene C1-C6 alkyl is [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group] example can comprise the C1-C6 alkyl, wherein be substituted with 2 phenyl [wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed], diphenyl methyl for example, 2, the 2-diphenyl-ethyl, 1, the 1-diphenyl-ethyl, 3, the 3-diphenyl propyl, 2, the 3-diphenyl propyl, 4,4-phenylbenzene butyl, 5,5-phenylbenzene amyl group, 4,5-phenylbenzene amyl group, 6,6-phenylbenzene hexyl, 2-methyl-3, the 3-diphenyl propyl, 1,1-dimethyl-2, the 2-diphenyl-ethyl, two (4-chloro-phenyl-) methyl, two (4-Trifluoromethoxyphen-l) methyl, two (4-trifluoromethyl) methyl, two (3-p-methoxy-phenyl) methyl, two (2, the 4-dichlorophenyl) methyl, two (2-aminomethyl phenyl) methyl, two (2,4, the 6-trifluorophenyl) methyl, two (3, the 4-Dimethoxyphenyl) methyl, two (2,4, the 6-trimethoxyphenyl) methyl, two (3, the 4-3,5-dimethylphenyl) methyl, two (2,4, the 6-trimethylphenyl) methyl and 1-(4-Trifluoromethoxyphen-l)-1-(4-chloro-phenyl-) methyl.

Phenyl is [wherein on this benzyl ring, be substituted with at least one group, it is selected from the alkylene dioxo base by C1-C4, phenyl, the C1-C6 alkoxy carbonyl, hydroxyl and phenoxy group are (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group) group formed] example can comprise phenyl, 4-xenyl for example, 4-tert-butoxycarbonyl phenyl, 4-ethoxy carbonyl phenyl, the 2-xenyl, the 4-hydroxy phenyl, 4-(4-chlorophenoxy) phenyl, 2,3-ethylenedioxy phenyl, the 3-xenyl, 3-tert-butoxycarbonyl phenyl, 3-methoxycarbonyl phenyl, 2,4-phenylbenzene phenyl, the 3-hydroxy phenyl, 4-(4-Trifluoromethyl phenyl ether oxygen base) phenyl, 2, the 3-methylenedioxyphenyl, 2,4, the 6-triphenyl, 2-tert-butoxycarbonyl phenyl, 2-propoxycarbonyl phenyl, 2-n-pentyloxy phenyl, the 2-hydroxy phenyl, 4-(4-4-trifluoromethylphenopendant) phenyl, 3,4-ethylenedioxy phenyl, 2,4,6-trihydroxy-phenyl, the positive hexyloxy carbonyl phenyl of 4-, 2,4-di ethoxy carbonyl phenyl, the 2-xenyl, 3, the 4-dihydroxy phenyl, 4-(2, the 4-dichlorophenoxy) phenyl, 3-(2,4,6-trifluoromethoxy phenoxy base) phenyl, 2,4,6-triethoxy carbonyl phenyl, 3-(2-methylphenoxy) phenyl, 4-(3-methylphenoxy) phenyl, 2-(4-methylphenoxy) phenyl, 3-(2, the 3-dimethyl phenoxy) phenyl, 4-(2,4,5-trimethylammonium phenoxy group) phenyl, 3-(2-methoxyl group phenoxy group) phenyl, 4-(3-methoxyl group phenoxy group) phenyl, 2-(4-methoxyl group phenoxy group) phenyl, 3-(3,4-dimethoxy phenoxy group) phenyl, 4-(2,4,6-trimethoxy phenoxy group) phenyl, 2-phenoxy group-4-ethoxy carbonyl phenyl and 2-phenyl-3-Phenoxyphenyl are [wherein on this benzyl ring, be substituted with 1 to 3 group, it is selected from by above-mentioned C1-C4 alkylene dioxo base, above-mentioned phenyl, above-mentioned C1-C6 alkoxy carbonyl, hydroxyl and above-mentioned phenoxy group are (wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 group, it is selected from by halogen atom, the group that halogen replacement or unsubstituted C1-C6 alkyl and halogen replacement or unsubstituted C1-C6 alkoxyl group are formed) group of forming].

Benzofuryl is [wherein on this cumarone ring, can be substituted with at least one group, it is selected from the group of being made up of halogen atom and C1-C6 alkyl] example can comprise benzofuryl, (2-for example, 3-, 4-, 5-, 6-or 7-) benzofuryl, 5-chloro-7-benzofuryl, 5-methyl-7-benzofuryl, 4-iodo-6-benzofuryl, 6-ethyl-7-benzofuryl, 6-bromo-5-benzofuryl, 7-n-propyl-4-benzofuryl, 7-fluoro-2-benzofuryl, 4-normal-butyl-2-benzofuryl, 2,5-two chloro-7-benzofuryls, 5,6-dimethyl-7-benzofuryl, 3,5,6-three fluoro-2-benzofuryls, 3,4,5-trimethylammonium-3-benzofuryl, 5-chloro-4-methyl-7-benzofuryl and 5-methyl-3-fluoro-8-benzofuryl, its condition is on this cumarone ring, can be substituted with 1 to 3 and be selected from following group: the group that above-mentioned halogen atom and above-mentioned C1-C6 alkyl are formed.

Benzothiazole quinoline base is [wherein on this benzothiazole quinoline ring, can be substituted with at least one oxo base] example can comprise benzothiazole quinoline base, (2-for example, 4-, 5-, 6-or 7-) benzothiazolyl and 2-oxo-6-benzothiazolyl, its condition is on this benzothiazole quinoline ring, can be substituted with an oxo base.

Benzothienyl is [wherein on this thionaphthene ring, can be substituted with at least one halogen atom] example can comprise benzothienyl, (2-for example, 3-, 4-, 5-, 6-or 7-) benzothienyl, 5-fluoro-4-benzothienyl, 6-fluoro-2-benzothienyl, 2-chloro-3-benzothienyl, 3-bromo-6-benzothienyl, 4-iodo-5-benzothienyl, 2,4,6-three chloro-7-benzothienyls and 4,5-two fluoro-2-benzothienyls, its condition is on this thionaphthene ring, can be substituted with 1 to 3 halogen atom.

1,2,3, the 4-tetrahydric quinoline group (wherein this 1,2,3, on the 4-tetrahydroquinoline ring, can be substituted with at least one and be selected from following group: the example group that oxo base and C1-C6 alkyl are formed) can comprise 1,2,3,4-tetrahydric quinoline group, for example (1-, 2-, 3-, 4-, 5-, 6-, 7-or 8-) 1,2,3, the 4-tetrahydric quinoline group, 2-oxo-(1-, 3-, 4-, 5-, 6-, 7-or 8-) 1,2,3, the 4-tetrahydric quinoline group, 2,4-dioxo-(1-, 3-, 5-, 6-, 7-or 8-) 1,2,3, the 4-tetrahydric quinoline group, 3-oxo-(1-, 2-, 4-, 5-, 6-, 7-or 8-) 1,2,3, the 4-tetrahydric quinoline group, 1-methyl-2-oxo-5-1,2,3, the 4-tetrahydric quinoline group, 2-methyl isophthalic acid-1,2,3, the 4-tetrahydric quinoline group, 3-ethyl-2-1,2,3, the 4-tetrahydric quinoline group, 4-n-propyl-3-1,2,3, the 4-tetrahydric quinoline group, 5-normal-butyl-4-1,2,3, the 4-tetrahydric quinoline group, 6-n-pentyl-5-1,2,3, the 4-tetrahydric quinoline group, 7-n-hexyl-6-1,2,3, the 4-tetrahydric quinoline group, 8-methyl-7-1,2,3, the 4-tetrahydric quinoline group, 4,6-dimethyl-5-1,2,3,4-tetrahydric quinoline group and 5,6,7-trimethylammonium-4-1,2,3,4-tetrahydric quinoline group, its condition be this 1,2,3, on the 4-tetrahydroquinoline ring, can be substituted with 1 to 3 group that is selected from the group of forming by oxo base and above-mentioned C1-C6 alkyl.

1,2-dihydroquinoline base (dihydrohydroquinolyl) (wherein this 1, on the 2-dihydroquinoline ring, can be substituted with at least one oxo base) example can comprise 1,2-dihydroquinoline base, for example (1-, 2-, 3-, 4-, 5-, 6-, 7-or 8-) 1,2-dihydroquinoline base and 2-oxo-(1-, 3-, 4-, 5-, 6-, 7-or 8-) 1,2-dihydroquinoline base, its condition be this 1, on the 2-dihydroquinoline ring, can be substituted with an oxo base.

1,2,3,4-tetrahydrochysene-quinazolyl [wherein this 1,2,3, on the 4-tetrahydro quinazoline ring, can be substituted with at least one group, it is selected from the group of being made up of oxo base and C1-C6 alkyl] example can comprise 1,2,3,4-tetrahydro quinazoline base, for example (1-, 2-, 3-, 4-, 5-, 6-, 7-or 8-) 1,2,3,4-tetrahydro quinazoline base, 2-oxo-(1-, 3-, 4-, 5-, 6-, 7-or 8-) 1,2,3,4-tetrahydro quinazoline base, 4-oxo-(1-, 2-, 3-, 5-, 6-, 7-or 8-) 1,2,3,4-tetrahydro quinazoline base, 2,4-dioxo-(1-, 3-, 5-, 6-, 7-or 8-) 1,2,3,4-tetrahydro quinazoline base, 1-methyl-2,4-dioxo-(3-, 5-, 6-, 7-or 8-) 1,2,3,4-tetrahydro quinazoline base, 3-ethyl-2,4-dioxo-(1-, 5-, 6-, 7-or 8-) 1,2,3,4-tetrahydro quinazoline base, 1,3-dimethyl-2,4-dioxo-(5-, 6-, 7-or 8-) 1,2,3,4-tetrahydro quinazoline base, 1-n-propyl-5-methyl-2-oxo-(3-, 4-, 6-, 7-or 8-) 1,2,3,4-tetrahydro quinazoline base, 1-normal-butyl-6-methyl-4-oxo-(2-, 3-, 5-, 7-or 8-) 1,2,3,4-tetrahydro quinazoline base, 1-n-pentyl-7-methyl-2-oxo-(3-, 4-, 5-, 6-or 8-) 1,2,3,4-tetrahydro quinazoline base and 1-n-hexyl-8-methyl-2,4-dioxo-(3-, 5-, 6-or 7-) 1,2,3,4-tetrahydro quinazoline base, its condition be this 1,2,3, on the 4-tetrahydro quinazoline ring, can be substituted with 1 to 4 group that is selected from the group of forming by oxo base and above-mentioned C1-C6 alkyl.

The C1-C6 alkyl that benzothienyl replaces is [wherein on this thionaphthene ring, can be substituted with at least one halogen atom] example can comprise the C1-C6 alkyl that benzothienyl replaces, 2-thionaphthene ylmethyl for example, 3-thionaphthene ylmethyl, 4-thionaphthene ylmethyl, 5-thionaphthene ylmethyl, 6-thionaphthene ylmethyl, 7-thionaphthene ylmethyl, 2-(2-benzothienyl) ethyl, 3-(2-benzothienyl) propyl group, 4-(2-benzothienyl) butyl, 5-(2-benzothienyl) amyl group, 6-(2-benzothienyl) hexyl, 5-chloro-3-thionaphthene ylmethyl, 3,4-two bromo-2-thionaphthene ylmethyls and 4,5,6-three chloro-2-thionaphthene ylmethyls, its condition is on this thionaphthene ring, can be substituted with 1 to 3 halogen atom.

The example of the C1-C6 alkyl of naphthyl substituted can comprise 1-naphthyl methyl, 2-naphthyl methyl, 2-(1-naphthyl) ethyl, 1-(2-naphthyl) ethyl, 3-(1-naphthyl) propyl group, 3-(2-naphthyl) propyl group, 4-(1-naphthyl) butyl, 4-(2-naphthyl) butyl, 5-(1-naphthyl) amyl group, 5-(2-naphthyl) amyl group, 6-(1-naphthyl) hexyl and 6-(2-naphthyl) hexyl.

The C1-C6 alkyl that pyridyl replaces is [wherein on this pyridine ring, can be substituted with at least one halogen atom] example can comprise the C1-C6 alkyl that pyridyl replaces, 2-pyridylmethyl for example, the 3-pyridylmethyl, the 4-pyridylmethyl, 2-(2-pyridyl) ethyl, 2-(3-pyridyl) ethyl, 2-(4-pyridyl) ethyl, 3-(2-pyridyl) propyl group, 3-(3-pyridyl) propyl group, 3-(4-pyridyl) propyl group, 4-(2-pyridyl) butyl, 4-(3-pyridyl) butyl, 4-(4-pyridyl) butyl, 5-(2-pyridyl) amyl group, 5-(3-pyridyl) amyl group, 5-(4-pyridyl) amyl group, 6-(2-pyridyl) hexyl, 6-(3-pyridyl) hexyl, 6-(4-pyridyl) hexyl, 2-chloro-3-pyridylmethyl, 3-bromo-2-pyridylmethyl, 4-fluoro-2-pyridylmethyl, 2-(2-chloro-4-pyridyl) ethyl, 2-(3-chloro-5-pyridyl) ethyl, 2-(4-iodo-3-pyridyl) ethyl, 3-(2-bromo-5-pyridyl) propyl group, 3-(3-fluoro-4-pyridyl) propyl group, 3-(4-chloro-2-pyridyl) propyl group, 4-(2-iodo-5-pyridyl) butyl, 4-(3-bromo-5-pyridyl) butyl, 4-(4-chloro-3-pyridyl) butyl, 5-(2-chloro-5-pyridyl) amyl group, 5-(3-fluoro-2-pyridyl) amyl group, 5-(4-bromo-2-pyridyl) amyl group, 6-(2-chloro-5-pyridyl) hexyl, 6-(3-fluoro-4-pyridyl) hexyl, 6-(4-bromo-2-pyridyl) hexyl, (2,6-two chloro-4-pyridyl) methyl and (2,3,4-three chloro-6-pyridyl) methyl, its condition is on this pyridine ring, can be substituted with 1 to 3 halogen atom as substituting group.

The C1-C6 alkyl that furyl replaces is [wherein on this furan nucleus, can be substituted with at least one nitro] example can comprise the C1-C6 alkyl that furyl replaces, 2-furyl methyl for example, the 3-furyl methyl, 2-(2-furyl) ethyl, 3-(2-furyl) propyl group, 3-(3-furyl) propyl group, 4-(2-furyl) butyl, 4-(3-furyl) butyl, 5-(2-furyl) amyl group, 5-(3-furyl) amyl group, 6-(2-furyl) hexyl, 6-(3-furyl) hexyl, 5-nitro-2-furyl methyl, 5-nitro-3-furyl methyl, 2-(5-nitro-2-furyl) ethyl, 3-(5-nitro-2-furyl) propyl group, 4-(5-nitro-2-furyl) butyl, 4-(5-nitro-3-furyl) butyl, 5-(5-nitro-2-furyl) amyl group, 5-(5-nitro-3-furyl) amyl group, 6-(5-nitro-2-furyl) hexyl, 6-(5-nitro-3-furyl) hexyl, (4,5-dinitrobenzene-2-furyl) methyl and (2,4,5-trinitro--3-furyl) methyl, its condition is on this furan nucleus, can be substituted with 1 to 3 nitro as substituting group.

The C1 one C6 alkyl that thienyl replaces is [wherein on this thiphene ring, can be substituted with at least one halogen atom] example can comprise the C1-C6 alkyl that thienyl replaces, 2-thienyl methyl for example, the 3-thienyl methyl, 2-(2-thienyl) ethyl, 3-(2-thienyl) propyl group, 3-(3-thienyl) propyl group, 4-(2-thienyl) butyl, 4-(3-thienyl) butyl, 5-(2-thienyl) amyl group, 5-(3-thienyl) amyl group, 6-(2-thienyl) hexyl, 6-(3-thienyl) hexyl, 5-chloro-2-thienyl methyl, 5-chloro-3-thienyl methyl, 2-(4-bromo-2-thienyl) ethyl, 3-(3-fluoro-2-thienyl) propyl group, 4-(5-iodo-2-thienyl) butyl, 4-(4-chloro-3-thienyl) butyl, 5-(3-chloro-2-thienyl) amyl group, 5-(2-chloro-3-thienyl) amyl group, 6-(3-chloro-2-thienyl) hexyl, 6-(5-chloro-3-thienyl) hexyl, (4,5-two chloro-2-thienyls) methyl and (2,4,5-three chloro-3-thienyls) methyl, its condition is on this thiphene ring, can be substituted with 1 to 3 halogen atom as substituting group.

Phenyl is (wherein on this benzyl ring, can be substituted with at least one is selected from by the group in the group that halogen atom and halogen replace or unsubstituted C1-C6 alkyl is formed) example can comprise phenyl, the 2-fluorophenyl, the 3-fluorophenyl, the 4-fluorophenyl, the 2-chloro-phenyl-, the 3-chloro-phenyl-, the 4-chloro-phenyl-, the 2-bromophenyl, the 3-bromophenyl, the 4-bromophenyl, the 2-iodophenyl, the 3-iodophenyl, the 4-iodophenyl, 2, the 3-difluorophenyl, 3, the 4-difluorophenyl, 3, the 5-difluorophenyl, 2, the 4-difluorophenyl, 2, the 6-difluorophenyl, 2, the 3-dichlorophenyl, 3, the 4-dichlorophenyl, 3, the 5-dichlorophenyl, 2, the 4-dichlorophenyl, 2, the 6-dichlorophenyl, 3,4, the 5-trifluorophenyl, 3,4, the 5-trichlorophenyl, 2,4, the 6-trifluorophenyl, 2,4, the 6-trichlorophenyl, 2-fluoro-4-bromophenyl, 4-chloro-3-fluorophenyl, 2,3, the 4-trichlorophenyl, 3,4, the 5-trifluorophenyl, 2,3,4,5, the 6-pentafluorophenyl group, 2,4, the 6-trimethylphenyl, the 4-n-butylphenyl, 2, the 4-3,5-dimethylphenyl, 2, the 3-3,5-dimethylphenyl, 2, the 6-3,5-dimethylphenyl, 3, the 5-3,5-dimethylphenyl, 2, the 5-3,5-dimethylphenyl, 3,5-two trifluoromethyls, 3-methyl-4-fluorophenyl, 4-bromo-3-trifluoromethyl, the 2-aminomethyl phenyl, the 3-aminomethyl phenyl, the 4-aminomethyl phenyl, 2-methyl-3-chloro-phenyl-, 3-methyl-4-chloro-phenyl-, 2-chloro-4-aminomethyl phenyl, 2-methyl-3-fluorophenyl, the 2-trifluoromethyl, the 3-trifluoromethyl, the 4-trifluoromethyl, 2-pentafluoroethyl group phenyl, 3-pentafluoroethyl group phenyl, 4-pentafluoroethyl group phenyl, the 2-isopropyl phenyl, the 3-isopropyl phenyl, the 4-isopropyl phenyl, the 2-tert-butyl-phenyl, the 3-tert-butyl-phenyl, the 4-tert-butyl-phenyl, the 2-secondary butyl phenenyl, the 3-secondary butyl phenenyl, the 4-secondary butyl phenenyl, 2-is the fluoropropyl phenyl just-seven, 3-is the fluoropropyl phenyl just-seven, 4-is the fluoropropyl phenyl just-seven, 4-n-pentyl phenyl, 4-n-hexyl phenyl, 2,3,4-trifluorophenyl and 2,4, the 6-trifluorophenyl.

The C1-C6 alkyl that thiazolyl replaces is [wherein on this thiazole ring, can be substituted with at least one is selected from by C1-C6 alkyl and phenyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from the group by halogen atom and halogen replace or unsubstituted C1-C6 alkyl is formed) group in the group formed] example can comprise the C1-C6 alkyl of thiazolyl replacement, 4-thiazolyl methyl for example, 5-thiazolyl methyl, 2-methyl-4-thiazolyl methyl, 2-methyl-5-thiazole ylmethyl, 2,5-dimethyl-4-thiazolyl methyl, 2,4-dimethyl-5-thiazolyl methyl, 2-methyl-5-phenyl-4-thiazolyl methyl, 2-methyl-4-phenyl-5-thiazolyl methyl, 2-phenyl-4-thiazolyl methyl, 2-phenyl-5-thiazolyl methyl, 2-phenyl-5-methyl-4-thiazolyl methyl, 2-phenyl-4-methyl-5-thiazole ylmethyl, 2-methyl-5-(2-fluorophenyl)-4-thiazolyl methyl, 2-methyl-4-(2-fluorophenyl)-5-thiazolyl methyl, 2-(2-chloro-phenyl-)-4-thiazolyl methyl, 2-(2-bromophenyl)-5-thiazolyl methyl, 2-(2-fluorophenyl)-5-methyl-4-thiazolyl methyl, 2-(2-fluorophenyl)-4-methyl-5-thiazole ylmethyl, 2-methyl-5-(3-iodophenyl)-4-thiazolyl methyl, 2-methyl-4-(3-fluorophenyl)-5-thiazolyl methyl, 2-(2, the 3-difluorophenyl)-4-thiazolyl methyl, 2-(3-fluorophenyl)-5-thiazolyl methyl, 2-(3-fluorophenyl)-5-methyl-4-thiazolyl methyl, 2-(3-fluorophenyl)-4-methyl-5-thiazole ylmethyl, 2-methyl-5-(2,4, the 6-trichlorophenyl)-4-thiazolyl methyl, 2-methyl-4-(2,3,4,5, the 6-pentafluorophenyl group)-5-thiazolyl methyl, 2-(4-fluorophenyl)-4-thiazolyl methyl, 4-(2-fluorophenyl)-5-thiazolyl methyl, 2-(4-fluorophenyl)-5-methyl-4-thiazolyl methyl, 2-(4-fluorophenyl)-4-methyl-5-thiazole ylmethyl, 2-methyl-5-(2-chloro-phenyl-)-4-thiazolyl methyl, 2-methyl-4-(2-chloro-phenyl-)-5-thiazolyl methyl, 2-(2-chloro-phenyl-)-4-thiazolyl methyl, 2-(2-chloro-phenyl-)-5-thiazolyl methyl, 2-(2-chloro-phenyl-)-5-methyl-4-thiazolyl methyl, 2-(2-chloro-phenyl-)-4-methyl-5-thiazole ylmethyl, 2-methyl-5-(3-chloro-phenyl-)-4-thiazolyl methyl, 2-methyl-4-(3-chloro-phenyl-)-5-thiazolyl methyl, 2-(3-chloro-phenyl-)-4-thiazolyl methyl, 2-(2-fluorophenyl)-5-thiazolyl methyl, 2-(3-chloro-phenyl-)-5-methyl-4-thiazolyl methyl, 2-(3-chloro-phenyl-)-4-methyl-5-thiazole ylmethyl, 2-methyl-5-(4-chloro-phenyl-)-4-thiazolyl methyl, 2-methyl-4-(4-chloro-phenyl-)-5-thiazolyl methyl, 2-(4-chloro-phenyl-)-4-thiazolyl methyl, 2-(4-chloro-phenyl-)-5-thiazolyl methyl, 2-(4-chloro-phenyl-)-5-methyl-4-thiazolyl methyl, 2-(4-chloro-phenyl-)-4-methyl-5-thiazole ylmethyl, 2-(2-thiazolyl) ethyl, 2-(4-thiazolyl) ethyl, 2-(5-thiazolyl) ethyl, 2-(2-methyl-4-thiazolyl) ethyl, 2-(2-methyl-5-thiazole base) ethyl, 2-(2,5-dimethyl-4-thiazolyl) ethyl, 2-(2,4-dimethyl-5-thiazolyl) ethyl, 2-(2-methyl-5-phenyl-4-thiazolyl) ethyl, 2-(2-methyl-4-phenyl-5-thiazolyl) ethyl, 2-(2-phenyl-4-thiazolyl) ethyl, 2-(2-phenyl-5-thiazolyl) ethyl, 2-(2-phenyl-5-methyl-4-thiazolyl) ethyl, 3-(2-thiazolyl) propyl group, 2-(4-thiazolyl) propyl group, 3-(5-thiazolyl) propyl group, 3-(2-methyl-4-thiazolyl) propyl group, 2-(2-methyl-5-thiazole base) propyl group, 3-(2,5-dimethyl-4-thiazolyl) propyl group, 3-(2,4-dimethyl-5-thiazolyl) propyl group, 3-(2-methyl-5-phenyl-4-thiazolyl) propyl group, 3-(2-methyl-4-phenyl-5-thiazolyl) propyl group, 2-(2-phenyl-4-thiazolyl) propyl group, 3-(3-phenyl-5-thiazolyl) propyl group, 3-(2-phenyl-5-methyl-4-thiazolyl) propyl group, 4-(2-thiazolyl) butyl, 4-(4-thiazolyl) butyl, 3-(5-thiazolyl) butyl, 4-(2-methyl-4-thiazolyl) butyl, 4-(2-methyl-5-thiazole base) butyl, 4-(2,5-dimethyl-4-thiazolyl) butyl, 4-(2,4-dimethyl-5-thiazolyl) butyl, 4-(2-methyl-5-phenyl-4-thiazolyl) butyl, 4-(2-methyl-4-phenyl-5-thiazolyl) butyl, 4-(2-phenyl-4-thiazolyl) butyl, 4-(4-phenyl-5-thiazolyl) butyl, 4-(2-phenyl-5-methyl-4-thiazolyl) butyl, 5-(2-thiazolyl) amyl group, 5-(4-thiazolyl) amyl group, 5-(5-thiazolyl) amyl group, 5-(2-methyl-4-thiazolyl) amyl group, 5-(2-methyl-5-thiazole base) amyl group, 5-(2,5-dimethyl-4-thiazolyl) amyl group, 5-(2,4-dimethyl-5-thiazolyl) amyl group, 5-(2-methyl-5-phenyl-4-thiazolyl) amyl group, 5-(2-methyl-4-phenyl-5-thiazolyl) amyl group, 5-(2-phenyl-4-thiazolyl) amyl group, 5-(4-phenyl-5-thiazolyl) amyl group, 5-(2-phenyl-5-methyl-4-thiazolyl) amyl group, 6-(2-thiazolyl) hexyl, 6-(4-thiazolyl) hexyl, 6-(5-thiazolyl) hexyl, 6-(2-methyl-4-thiazolyl) hexyl, 6-(2-methyl-5-thiazole base) hexyl, 6-(2,5-dimethyl-4-thiazolyl) hexyl, 6-(2,4-dimethyl-5-thiazolyl) hexyl, 6-(2-methyl-5-phenyl-4-thiazolyl) hexyl, 6-(2-methyl-4-phenyl-5-thiazolyl) hexyl, 6-(2-phenyl-4-thiazolyl) hexyl, 6-(4-phenyl-5-thiazolyl) hexyl, 6-(2-phenyl-5-methyl-4-thiazolyl) hexyl, 2-(2, the 3-3,5-dimethylphenyl)-4-thiazolyl methyl, 2-(3-aminomethyl phenyl)-5-thiazolyl methyl, 2-(3-trifluoromethyl)-5-methyl-4-thiazolyl methyl, 2-(3-ethylphenyl)-4-methyl-5-thiazole ylmethyl, 2-(2-trifluoroethyl phenyl)-4-methyl-5-thiazole ylmethyl and 2-methyl-5-(2,4, the 6-trimethylphenyl)-4-thiazolyl methyl, its condition is on this thiazole ring, can be substituted with 1 or 2 is selected from by C1-C6 alkyl and phenyl (wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 group, it is selected from the group by halogen atom and halogen replace or unsubstituted C1-C6 alkyl is formed) group in the group formed.

The C1-C6 alkyl that tetrazyl replaces is [wherein on this tetrazole ring, can be substituted with at least one C1-C6 alkyl] example can comprise the C1-C6 alkyl that tetrazyl replaces, 5-(1H)-tetrazyl methyl for example, 2-(5-(1H)-tetrazyl) ethyl, 1-(5-(1H)-tetrazyl) ethyl, 3-(5-(1H)-tetrazyl) propyl group, 4-(5-(1H)-tetrazyl) butyl, 5-(5-(1H)-tetrazyl) amyl group, 6-(5-(1H)-tetrazyl) hexyl, 2-methyl-3-(5-(1H)-tetrazyl) propyl group, 1,1-dimethyl-2-(5-(1H)-tetrazyl) ethyl, 1-methyl-5-(1H)-tetrazyl methyl, 1-ethyl-5-(1H)-tetrazyl methyl, 1-n-propyl-5-(1H)-tetrazyl methyl, 1-normal-butyl-5-(1H)-tetrazyl methyl, 1-n-pentyl-5-(1H)-tetrazyl methyl, 1-n-hexyl-5-(1H)-tetrazyl methyl, 2-(1-methyl-5-(1H)-tetrazyl) ethyl, 2-(1-ethyl-5-(1H)-tetrazyl) ethyl, 2-(1-n-propyl-5-(1H)-tetrazyl) ethyl, 2-(1-normal-butyl-5-(1H)-tetrazyl) ethyl, 2-(1-n-pentyl-5-(1H)-tetrazyl) ethyl and 2-(1-n-hexyl-5-(1H)-tetrazyl) ethyl, its condition is on this tetrazole ring, can be substituted with a C1-C6 alkyl.

The C1-C6 alkyl that different _ azoles base replaces is [wherein on this different _ azoles ring, can be substituted with at least one C1-C6 alkyl] example can comprise the C1-C6 alkyl that different _ azoles base replaces, (3-for example, 4-or 5-be different _ the azoles base) and methyl, 2-(3-, 4-or 5-be different _ the azoles base) and ethyl, 1-(3-, 4-or 5-be different _ the azoles base) and ethyl, 3-(3-, 4-or 5-be different _ the azoles base) and propyl group, 4-(3-, 4-or 5-be different _ the azoles base) and butyl, 5-(3-, 4-or 5-be different _ the azoles base) and amyl group, 6-(3-, 4-or 5-be different _ the azoles base) and hexyl, 3-methyl-2-(3-, 4-or 5-be different _ the azoles base) and propyl group, 1,1-dimethyl-2-(3-, 4-or 5-be different _ the azoles base) and ethyl, (3-methyl-4-different _ azoles base) methyl, (4-ethyl-3-different _ azoles base) methyl, (5-n-propyl-3-different _ azoles base) methyl, (4-normal-butyl-5-different _ azoles base) methyl, (5-n-pentyl-3-different _ azoles base) methyl, (3-n-hexyl-4-different _ azoles base) methyl, (3,4-dimethyl-5-is different _ the azoles base) and methyl, 2-(3-methyl-4-different _ azoles base) ethyl, 1-(4-ethyl-3-different _ azoles base) ethyl, 3-(5-n-propyl-3-different _ azoles base) propyl group, 4-(4-normal-butyl-5-different _ azoles base) butyl, 5-(5-n-pentyl-3-different _ azoles base) amyl group, 6-(3-n-hexyl-4-different _ azoles base) hexyl and 2-(3,4-dimethyl-5-is different _ the azoles base) and ethyl, its condition is on this different _ azoles ring, can be substituted with 1 or 2 C1-C6 alkyl.

1,2, the C1-C6 alkyl that the 4-_ di azoly replaces [wherein this 1,2, on the 4-_ diazole ring, can be substituted with at least one phenyl (wherein on this benzyl ring, can be substituted with the C1-C6 alkyl)] example can comprise 1,2, the C1-C6 alkyl that the 4-_ di azoly replaces, (3-or 5-) 1 for example, 2,4-_ di azoly methyl, 2-((3-or 5-) 1,2, the 4-_ di azoly) ethyl, 1-((3-or 5-) 1,2, the 4-_ di azoly) ethyl, 3-((3-or 5-) 1,2, the 4-_ di azoly) propyl group, 4-((3-or 5-) 1,2, the 4-_ di azoly) butyl, 5-((3-or 5-) 1,2, the 4-_ di azoly) amyl group, 6-((3-or 5-) 1,2, the 4-_ di azoly) hexyl, 3-methyl-2-((3-or 5-) 1,2, the 4-_ di azoly) propyl group, 1,1-dimethyl-2-((3-or 5-) 1,2, the 4-_ di azoly) ethyl, (3-phenyl-5-1,2,4-_ di azoly) methyl, (5-phenyl-3-1,2, the 4-_ di azoly) methyl, (3-(3-aminomethyl phenyl)-5-1,2,4-_ di azoly) methyl, (5-(3, the 4-3,5-dimethylphenyl)-3-1,2, the 4-_ di azoly) methyl, (3-(2,4, the 6-trimethylphenyl)-5-1,2, the 4-_ di azoly) methyl, (5-(2-ethylphenyl)-3-1,2, the 4-_ di azoly) methyl, 2-((3-n-propyl phenyl)-5-1,2, the 4-_ di azoly) ethyl, 1-(5-(4-n-butylphenyl)-3-1,2, the 4-_ di azoly) ethyl, 3-(3-(3-n-pentyl phenyl)-5-1,2, the 4-_ di azoly) propyl group, 4-(5-(5-n-hexyl phenyl)-3-1,2, the 4-_ di azoly) butyl, 5-(3-(3-ethyl-4-aminomethyl phenyl)-5-1,2, the 4-_ di azoly) amyl group and 6-(5-(2-aminomethyl phenyl)-3-1,2, the 4-_ di azoly) hexyl, its condition be this 1,2, on the 4-_ diazole ring, can be substituted with a phenyl (wherein on this benzyl ring, can be substituted with 1 to 3 C1-C6 alkyl).

The example of the C1-C6 alkyl that benzo furazan base replaces can comprise 4-benzo furazan ylmethyl, 5-benzo furazan ylmethyl, 6-benzo furazan ylmethyl, 7-benzo furazan ylmethyl, 1-(4-benzo furazan base) ethyl, 2-(5-benzo furazan base) ethyl, 3-(6-benzo furazan base) propyl group, 4-(7-benzo furazan base) butyl, 5-(4-benzo furazan base) amyl group, 6-(5-benzo furazan base) hexyl, 2-methyl-3-(6-benzo furazan base) propyl group and 1,1-dimethyl-2-(7-benzo furazan base) ethyl.

Phenyl amino [wherein can be substituted with the C1-C6 alkyl on the N-position of this phenyl amino, wherein can be substituted with at least one halogen and replace or unsubstituted C1-C6 alkoxyl group on the benzyl ring of this phenyl amino] can be a unsubstituted phenyl amino (another name: phenylamino) or wherein be substituted with 1 to 3 halogen phenylamino that replace or unsubstituted C1-C6 alkoxyl group as defined above.The example of phenyl amino can comprise phenyl amino, 2-p-methoxy-phenyl amino, 3-p-methoxy-phenyl amino, 4-p-methoxy-phenyl amino, 2-ethoxyl phenenyl amino, 3-ethoxyl phenenyl amino, 4-ethoxyl phenenyl amino, 4-positive propoxy phenyl amino, 4-tert.-butoxy phenyl amino, 4-n-butoxy phenyl amino, 2-Trifluoromethoxyphen-l amino, 3-Trifluoromethoxyphen-l amino, 4-Trifluoromethoxyphen-l amino, 2-five fluorine ethoxyl phenenyl amino, 3-five fluorine ethoxyl phenenyl amino, 2,3-Dimethoxyphenyl amino, 3,4,5-trimethoxyphenyl amino, 4-n-pentyloxy phenyl amino, the positive hexyloxy phenyl amino of 4-, 3,5-two Trifluoromethoxyphen-l amino, N-phenyl-N-methylamino, N-(2-p-methoxy-phenyl)-N-ethylamino, N-(3-p-methoxy-phenyl)-N-n-propyl amino, N-(4-p-methoxy-phenyl)-N-normal-butyl amino, N-(2-ethoxyl phenenyl)-N-n-pentyl amino, N-(3-ethoxyl phenenyl)-N-n-hexyl amino, N-(4-ethoxyl phenenyl)-N-methylamino, N-(4-positive propoxy phenyl)-N-ethylamino, N-(4-tert.-butoxy phenyl)-N-n-propyl amino, N-(4-n-butoxy phenyl)-N-normal-butyl amino, N-(2-Trifluoromethoxyphen-l)-N-n-pentyl amino, N-(3-Trifluoromethoxyphen-l)-N-n-hexyl amino, N-(4-Trifluoromethoxyphen-l)-N-methylamino, N-(2-five fluorine ethoxyl phenenyls)-N-ethylamino, N-(3-five fluorine ethoxyl phenenyls)-N-n-propyl amino, N-(2, the 3-Dimethoxyphenyl)-the N-methylamino, N-(3,4, the 5-trimethoxyphenyl)-the N-methylamino, N-(4-n-pentyloxy phenyl)-N-methylamino, N-(the positive hexyloxy phenyl of 4-)-N-methylamino and N-(3,5-two Trifluoromethoxyphen-ls)-N-methylamino.

Phenoxy group is (wherein on this benzyl ring, can be substituted with that halogen replaces or unsubstituted C1-C6 alkoxyl group) example can comprise phenoxy group, phenoxy group for example, 2-methoxyl group phenoxy group, 3-methoxyl group phenoxy group, 4-methoxyl group phenoxy group, 4-isopropoxy phenoxy group, 4-n-butoxy phenoxy group, 2,4-dimethoxy phenoxy group, 2,3-dimethoxy phenoxy group, 2,3,4,5,6-pentamethoxyl phenoxy group, 3,5-dimethoxy phenoxy group, 2,5-dimethoxy phenoxy group, 2,4,6-trimethoxy phenoxy group, 3,5-two (trifluoromethoxy) phenoxy group, 4-methoxyl group-3-Trifluoromethyl phenyl ether oxygen base, 2,6-dimethoxy phenoxy group, 2-Trifluoromethyl phenyl ether oxygen base, 3-Trifluoromethyl phenyl ether oxygen base, 4-Trifluoromethyl phenyl ether oxygen base, 2,3-two (trifluoromethoxy) phenoxy group, 2,4-two (trifluoromethoxy) phenoxy group, 2-five fluorine ethoxy phenoxies, 3-five fluorine ethoxy phenoxies, 4-five fluorine ethoxy phenoxies, 2-isopropoxy phenoxy group, 3-isopropoxy phenoxy group, 4-isopropoxy phenoxy group, 2-tert.-butoxy phenoxy group, 3-tert.-butoxy phenoxy group, 4-tert.-butoxy phenoxy group, 2-sec-butoxy phenoxy group, 3-sec-butoxy phenoxy group, 4-sec-butoxy phenoxy group, the positive hexyloxy phenoxy group of 4-, 2-is fluorine propoxy-phenoxy group just-seven, 3-is fluorine propoxy-phenoxy group and 4-fluorine propoxy-phenoxy group just-seven just-seven, its condition is on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 group, it is selected from by halogen group that replace or that unsubstituted C1-C6 alkoxyl group is formed.

Amino (wherein on this amino, can be substituted with at least one is selected from by C1-C6 alkyl and phenyl [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group] group in the group of composition is as substituting group) example can comprise amino, for example amino, methylamino, dimethylamino, ethylamino, diethylamino, n-propyl amino, normal-butyl amino, n-pentyl amino, 3-n-hexyl amino, phenyl amino, (4-chloro-phenyl-) amino, (4-bromophenyl) amino, (2, the 4-dichlorophenyl) amino, (2,4, the 6-trichlorophenyl) amino, (2,3,4,5, the 6-pentafluorophenyl group) amino, (4-fluorophenyl) amino, (4-iodophenyl) amino, (4-chloro-phenyl-) amino, (3-aminomethyl phenyl) amino, (4-trifluoromethyl) amino, (4-trifluoromethyl) amino, 3-(4-trifluoromethyl) amino, (3, the 4-3,5-dimethylphenyl) amino, (3,4, the 5-trimethylphenyl) amino, (2-p-methoxy-phenyl) amino, (4-Trifluoromethoxyphen-l) amino, 3-(4-Trifluoromethoxyphen-l) amino, (3, the 5-Dimethoxyphenyl) amino, (2, the 5-Dimethoxyphenyl) amino, (2,4, the 6-trimethoxyphenyl) amino, amino and N-ethyl-N-(4-Trifluoromethoxyphen-l) amino of N-methyl-N-(4-trifluoromethyl), its condition is on this amino, can be substituted with 1 or 2 group as substituting group, described group is selected from by C1-C6 alkyl and phenyl [wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 group, it is selected from by halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group] group formed.

Piperidyl is [wherein on this piperidine ring, can be substituted with at least one group, this group is selected from by phenoxy group (wherein on this benzyl ring, can be substituted with halogen replacement or unsubstituted C1-C6 alkoxyl group as substituting group) and amino (wherein on this amino, can be substituted with at least one group as substituting group, it is selected from by C1-C6 alkyl and phenyl [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group] group formed) group formed] and example can comprise piperidyl, 2-piperidyl for example, the 3-piperidyl, the 4-piperidyl, 2,4-diaminostilbene-piperidyl, 2,4,6-triamino-piperidino, 4-amino-3-phenoxy group-piperidino, 4-phenoxy group-2-amino-piperidino, 2-amino-piperidino, 3-amino-piperidino, 4-amino-piperidino, 4-methylamino-piperidino, 4-ethylamino-piperidino, 4-n-propyl amino-piperidino, 4-dimethylamino-piperidino, 4-diethylamino-piperidino, 4-two-n-propyl amino-piperidino, 4-phenyl amino-piperidino, 4-(N-phenyl-N-methylamino)-piperidino, 4-(2-fluorophenyl amino)-piperidino, 4-(3-fluorophenyl amino)-piperidino, 4-(4-fluorophenyl amino)-piperidino, 4-(2-chloro-phenyl-amino)-piperidino, 4-(2,3-chloro-phenyl-amino)-piperidino, 4-(4-chloro-phenyl-amino)-piperidino, 4-(2,3-dichlorophenyl amino)-piperidino, 4-(2,4,6-trifluorophenyl amino)-piperidino, 4-(2,4-dichlorophenyl amino)-piperidino, 4-(3,4-dichlorophenyl amino)-piperidino, 4-(3,5-dichlorophenyl amino)-piperidino, 4-(2,3,4,5,6-pentafluorophenyl group amino)-piperidino, 4-(2-trifluoromethyl amino)-piperidino, 4-(2-aminomethyl phenyl amino)-piperidino, 4-(2,3-3,5-dimethylphenyl amino)-piperidino, 4-(2-trifluoromethyl amino)-piperidino, 4-(2,4,6-trimethylphenyl amino)-piperidino, 4-(4-trifluoromethyl amino)-piperidino, 4-(2-pentafluoroethyl group phenyl amino)-piperidino, 4-(3-pentafluoroethyl group phenyl amino)-piperidino, 4-(4-pentafluoroethyl group phenyl amino)-piperidino, 4-(2-Trifluoromethoxyphen-l amino)-piperidino, 4-(2-p-methoxy-phenyl amino)-piperidino, 4-(2,3-Dimethoxyphenyl amino)-piperidino, 4-(2,4,6-trimethoxyphenyl amino)-piperidino, 4-(N-methyl-N-(2,4,6-trimethoxyphenyl amino))-piperidino, 4-(N-methyl-N-(3,4-3,5-dimethylphenyl amino))-piperidino, 4-(3-Trifluoromethoxyphen-l amino)-piperidino, 4-(4-Trifluoromethoxyphen-l amino)-piperidino, 4-(2-five fluorine ethoxyl phenenyl amino)-piperidino, 4-(3-five fluorine ethoxyl phenenyl amino)-piperidino, 4-(4-five fluorine ethoxyl phenenyl amino)-piperidino, 4-(2-fluorophenyl amino)-piperidino, 4-(3-fluorophenyl amino)-piperidino, 4-(4-fluorophenyl amino)-piperidino, 4-phenoxy group-piperidino, 2,4-hexichol Oxy-1-piperidyl, 2,4,6-triple phenoxyl-piperidino, 4-(2-methoxyl group phenoxy group)-piperidino, 1-(3-methoxyl group phenoxy group)-4-piperidyl, 1-(4-methoxyl group phenoxy group)-4-piperidyl, 2-(2-ethoxy phenoxy)-3-piperidyl, 3-(3-ethoxy phenoxy)-4-piperidyl, 4-(4-ethoxy phenoxy)-5-piperidyl, 3-(4-positive propoxy phenoxy group)-2-piperidyl, 2-(4-tert.-butoxy phenoxy group)-piperidino, 1-(4-n-butoxy phenoxy group)-2-piperidyl, 2-(2-Trifluoromethyl phenyl ether oxygen base)-3-piperidyl, 3-(3-Trifluoromethyl phenyl ether oxygen base)-4-piperidyl, 4-(4-Trifluoromethyl phenyl ether oxygen base)-3-piperidyl, 3-(2-five fluorine ethoxy phenoxies)-2-piperidyl, 6-(3-five fluorine ethoxy phenoxies)-piperidino, 1-(2,3-dimethoxy phenoxy group)-the 4-piperidyl, 4-(3,4,5-trimethoxy phenoxy group)-piperidino, 4-(4-n-pentyloxy phenoxy group)-piperidino and 4-(the positive hexyloxy phenoxy group of 4-)-piperidino, its condition is on this piperidine ring, can be substituted with 1 to 3 group, it is selected from by phenoxy group (wherein on this benzyl ring, can be substituted with 1 to 5, that preferred 1 to 3 halogen replaces or unsubstituted C1-C6 alkoxyl group is as substituting group) and amino (wherein on this amino, can be substituted with 1 or 2 group as substituting group, it is selected from by C1-C6 alkyl and phenyl [wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 group, it is selected from by halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group] group formed) group formed.

Piperazinyl is [wherein on this piperazine ring; can be substituted with the group that at least one is selected from following groups: the C1-C6 alkoxy carbonyl; phenyl C1-C6 alkyl is (wherein on this benzyl ring; can be substituted with at least one group; it is selected from by halogen atom; halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed); phenyl C2-C6 thiazolinyl is (wherein on this benzyl ring; can be substituted with at least one group; it is selected from by halogen atom; halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group) and benzoyl (wherein on this benzyl ring; can be substituted with at least one group; it is selected from by halogen atom; the group that halogen replacement or unsubstituted C1-C6 alkyl and halogen replacement or unsubstituted C1-C6 alkoxyl group are formed)] example can comprise piperazinyl; (1-for example; 2-or 3-) piperazinyl; 4-tert-butoxycarbonyl-1-piperazinyl; 4-ethoxy carbonyl-1-piperazinyl; 4-methoxycarbonyl-1-piperazinyl; 2; 4-dimethoxy carbonyl-1-piperazinyl; 2; 4; 6-triethoxy carbonyl-1-piperazinyl; 4-(4-trifluoro-methoxybenzyl)-1-piperazinyl; 4-(4-benzyl chloride base)-1-piperazinyl; 4-(4-methoxy-benzyl)-1-piperazinyl; 4-(4-bromobenzyl)-1-piperazinyl; 4-(4-methyl-benzyl)-1-piperazinyl; 4-(2; the 4-dichloro benzyl)-the 1-piperazinyl; 4-(3; the 4-dimethoxy-benzyl)-the 1-piperazinyl; 4-(2; 4; the 6-trifluoro-benzyl)-the 1-piperazinyl; 4-(3; the 4-dimethyl benzyl)-the 1-piperazinyl; 4-(2; 4; 6-trimethoxy benzyl)-the 1-piperazinyl; 4-(2; 4; the 6-trimethyl benzyl)-the 1-piperazinyl; 4-(4-iodine benzyl)-1-piperazinyl; 4-(4-trifluoromethyl benzyl)-1-piperazinyl; 4-(3; the 4-dichloro benzyl)-the 1-piperazinyl; 4-(3-(4-trifluoromethyl)-2-propenyl)-1-piperazinyl; 4-(3-(4-trifluoromethyl)-2-propenyl)-1-piperazinyl; 4-(4-trifluoromethyl benzoyl)-1-piperazinyl; 4-(3-(4-chloro-phenyl-)-2-propenyl)-1-piperazinyl; 4-(3-(4-aminomethyl phenyl)-2-propenyl)-1-piperazinyl; 4-(3-(4-p-methoxy-phenyl)-2-propenyl)-1-piperazinyl; (3-(3 for 4-; the 4-3,5-dimethylphenyl)-the 2-propenyl)-the 1-piperazinyl; (3-(3 for 4-; the 4-Dimethoxyphenyl)-the 2-propenyl)-the 1-piperazinyl; (3-(3 for 4-; 4; the 5-trimethylphenyl)-the 2-propenyl)-the 1-piperazinyl; (3-(3 for 4-; 4; the 5-trimethoxyphenyl)-the 2-propenyl)-the 1-piperazinyl; (3-(3 for 4-; the 4-dichlorophenyl)-the 2-propenyl)-the 1-piperazinyl; (3-(2 for 4-; 4; the 6-trifluorophenyl)-the 2-propenyl)-the 1-piperazinyl; 4-(3-(4-iodophenyl)-2-propenyl)-1-piperazinyl; 4-(3-(3-bromophenyl)-2-propenyl)-1-piperazinyl; 4-(4-luorobenzyl)-1-piperazinyl; 4-(4-methyl benzoyl)-1-piperazinyl; 4-(4-anisoyl)-1-piperazinyl; 4-(3; 4-dimethylbenzoyl-1-piperazinyl; 4-(2; 4-dimethylbenzoyl-1-piperazinyl; 4-(3; 4; 5-trimethylbenzoyl-1-piperazinyl; 4-(2; 4; 6-trimethoxy benzoyl-1-piperazinyl; 4-(4-chlorobenzene formacyl)-1-piperazinyl; 4-(2; 4; 6-trifluoromethyl benzonitrile acyl group)-the 1-piperazinyl; 4-(4-benzoyl bromide)-1-piperazinyl; 4-(4-iodobenzene formyl radical)-1-piperazinyl; 4-(3; 4-dichloro-benzoyl base)-the 1-piperazinyl; 4-(4-fluoro benzoyl)-1-piperazinyl; 4-benzyl-3-(3-phenyl-2-propenyl)-1-piperazinyl and 4-benzoyl-3; 5-dibenzyl-1-piperazinyl; its condition is on this piperazine ring; can be substituted with 1 to 3 group that is selected from following groups: above-mentioned C1-C6 alkoxy carbonyl; above-mentioned phenyl C1-C6 alkyl is (wherein on this benzyl ring; can be substituted with 1 to 5; preferred 1 to 3 group; it is selected from by halogen atom; halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed); (it is unsubstituted to above-mentioned phenyl C2-C6 thiazolinyl; perhaps it is made up of 1 or 2 phenyl and thiazolinyl; described phenyl can be substituted with 1 to 5; preferred 1 to 3 is selected from following group: halogen atom; halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed; described thiazolinyl contains 2 to 6 carbon atoms; and have 1 to 3 two key) and above-mentioned benzoyl (wherein on this benzyl ring; can be substituted with 1 to 5; preferred 1 to 3 group, it is selected from by halogen atom; halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed).

High piperazinyl is [wherein on this high piperazine ring, can be substituted with at least one group, it is selected from by C1-C6 alkoxy carbonyl and phenyl C1-C6 alkyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group) group formed] example can comprise high piperazinyl, (1-for example, 2-, 3-, 4-, 5-, 6-or 7-) high piperazinyl, 3, the high piperazinyl of 4-dibenzyl-1-, 2, the high piperazinyl of 7-dibenzyl-1-, 2,3, the high piperazinyl of 4-tribenzyl-1-, 2,4, the high piperazinyl of 6-tribenzyl-1-, the high piperazinyl of 4-benzyl-1-, 4-(2-the styroyl)-high piperazinyl of 1-, 4-(3-the phenyl propyl)-high piperazinyl of 1-, 4-(4-the phenyl butyl)-high piperazinyl of 1-, 4-(5-the phenylpentyl)-high piperazinyl of 1-, 4-(6-phenyl the hexyl)-high piperazinyl of 1-, 4-(2-the luorobenzyl)-high piperazinyl of 1-, 4-(3-the luorobenzyl)-high piperazinyl of 1-, 4-(4-the luorobenzyl)-high piperazinyl of 1-, 4-(2-benzyl chloride the base)-high piperazinyl of 1-, 4-(3-benzyl chloride the base)-high piperazinyl of 1-, 4-(4-benzyl chloride the base)-high piperazinyl of 1-, 4-(2, the 3-dichloro benzyl)-the high piperazinyl of 1-, 4-(2, the 4-dichloro benzyl)-the high piperazinyl of 1-, 4-(3, the 4-dichloro benzyl)-the high piperazinyl of 1-, 4-(3, the 5-dichloro benzyl)-the high piperazinyl of 1-, 4-(3,4,5-trichlorine benzyl)-the high piperazinyl of 1-, 4-(2,3,4,5, the 6-PFBBR)-the high piperazinyl of 1-, 4-(2-the trifluoromethyl benzyl)-high piperazinyl of 1-, 4-(3-the trifluoromethyl benzyl)-high piperazinyl of 1-, 4-(4-the trifluoromethyl benzyl)-high piperazinyl of 1-, 4-(4-the methyl-benzyl)-high piperazinyl of 1-, 4-(3, the 4-dimethyl benzyl)-the high piperazinyl of 1-, 4-(2,4, the 6-trimethyl benzyl)-the high piperazinyl of 1-, 4-(2-pentafluoroethyl group the benzyl)-high piperazinyl of 1-, 4-(3-pentafluoroethyl group the benzyl)-high piperazinyl of 1-, 4-(4-pentafluoroethyl group the benzyl)-high piperazinyl of 1-, 4-(2-the trifluoro-methoxybenzyl)-high piperazinyl of 1-, 4-(3-the trifluoro-methoxybenzyl)-high piperazinyl of 1-, 4-(4-the trifluoro-methoxybenzyl)-high piperazinyl of 1-, 4-(4-the methoxy-benzyl)-high piperazinyl of 1-, 4-(3, the 4-dimethoxy-benzyl)-the high piperazinyl of 1-, 4-(2,4,6-trimethoxy benzyl)-the high piperazinyl of 1-, 4-(2-five fluorine the ethoxy benzyls)-high piperazinyl of 1-, 4-(3-five fluorine the ethoxy benzyls)-high piperazinyl of 1-, 4-(4-five fluorine the ethoxy benzyls)-high piperazinyl of 1-, 4-(2-(4-Trifluoromethoxyphen-l) the ethyl)-high piperazinyl of 1-, 4-(3-(4-Trifluoromethoxyphen-l) the propyl group)-high piperazinyl of 1-, 4-(4-(4-Trifluoromethoxyphen-l) the butyl)-high piperazinyl of 1-, 4-(5-(4-Trifluoromethoxyphen-l) the amyl group)-high piperazinyl of 1-, 4-(6-(4-Trifluoromethoxyphen-l) the hexyl)-high piperazinyl of 1-, 4-(2-(4-trifluoromethyl) the ethyl)-high piperazinyl of 1-, 4-(3-(4-trifluoromethyl) the propyl group)-high piperazinyl of 1-, 4-(4-(4-trifluoromethyl) the butyl)-high piperazinyl of 1-, 4-(5-(4-trifluoromethyl) the amyl group)-high piperazinyl of 1-, 4-(6-(4-trifluoromethyl) the hexyl)-high piperazinyl of 1-, 4-tert-butoxycarbonyl-(1-, 2-, 3-, 5-, 6-or 7-) high piperazinyl, 4-methoxycarbonyl (1-, 2-, 3-, 5-, 6-or 7-) high piperazinyl and 4-ethoxy carbonyl carbonyl (1-, 2-, 3-, 5-, 6-or 7-) high piperazinyl, its condition is on this high piperazine ring, can be substituted with 1 to 3 group, it is selected from by above-mentioned C1-C6 alkoxy carbonyl and phenyl C1-C6 alkyl (wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 group, it is selected from by halogen atom, the group that halogen replacement or unsubstituted C1-C6 alkyl and halogen replacement or unsubstituted C1-C6 alkoxyl group are formed) group of forming.

The phenyl that phenoxy group replaces is (wherein on this benzyl ring, can be substituted with at least one halogen replaces or unsubstituted C1-C6 alkoxyl group) example can comprise the phenyl that phenoxy group replaces, 2-Phenoxyphenyl for example, 2,3-two Phenoxyphenyls, 2,4,6-triple phenoxyl phenyl, 3-(2-methoxyl group phenoxy group) phenyl, 4-(3-methoxyl group phenoxy group) phenyl, 2-(4-methoxyl group phenoxy group) phenyl, 3-(4-isopropoxy phenoxy group) phenyl, 4-(4-n-butoxy phenoxy group) phenyl, 2-(2,4-dimethoxy phenoxy group) phenyl, 3-(2,3-dimethoxy phenoxy group) phenyl, 4-(2,3,4,5,6-pentamethoxyl phenoxy group) phenyl, 2-(3,5-dimethoxy phenoxy group) phenyl, 3-(2,5-dimethoxy phenoxy group) phenyl, 4-(2,4,6-trimethoxy phenoxy group) phenyl, 2-(3,5-two (trifluoromethoxy) phenoxy group) phenyl, 3-(4-methoxyl group-3-Trifluoromethyl phenyl ether oxygen base) phenyl, 4-(2,6-dimethoxy phenoxy group) phenyl, 2-(2-Trifluoromethyl phenyl ether oxygen base) phenyl, 3-(3-Trifluoromethyl phenyl ether oxygen base) phenyl, 4-(4-Trifluoromethyl phenyl ether oxygen base) phenyl, 2-(2,3-two (trifluoromethoxy) phenoxy group) phenyl, 3-(2,4-two (trifluoromethoxy) phenoxy group) phenyl, 4-(2-five fluorine ethoxy phenoxies) phenyl, 2-(3-five fluorine ethoxy phenoxies) phenyl, 3-(4-five fluorine ethoxy phenoxies) phenyl, 4-(2-isopropoxy phenoxy group) phenyl, 2-(3-isopropoxy phenoxy group) phenyl, 3-(4-isopropoxy phenoxy group) phenyl, 4-(2-tert.-butoxy phenoxy group) phenyl, 2-(3-tert.-butoxy phenoxy group) phenyl, 3-(4-tert.-butoxy phenoxy group) phenyl, 4-(2-sec-butoxy phenoxy group) phenyl, 3-(3-sec-butoxy phenoxy group) phenyl, 4-(4-sec-butoxy phenoxy group) phenyl, 2-(the positive hexyloxy phenoxy group of 4-) phenyl, 3-(2-is fluorine propoxy-phenoxy group just-seven) phenyl, 4-(3-is fluorine propoxy-phenoxy group just-seven) phenyl and 2-(4-is fluorine propoxy-phenoxy group just-seven) phenyl, its condition is on this benzyl ring, can be substituted with 1 to 5, replace or the unsubstituted C1-C6 alkoxyl group of preferred 1 to 3 halogen.

Phenoxy group is [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen replaces or unsubstituted C1-C6 alkoxyl group and phenoxy group replace phenyl (wherein on this benzyl ring, can be substituted with the group that C1-C6 alkoxyl group that at least one halogen replaces or unsubstituted is formed) group formed] example can comprise phenoxy group, phenoxy group for example, 2-methoxyl group phenoxy group, 3-methoxyl group phenoxy group, 4-methoxyl group phenoxy group, 4-isopropoxy phenoxy group, 4-n-butoxy phenoxy group, 2,4-dimethoxy phenoxy group, 2,3-dimethoxy phenoxy group, 2,3,4,5,6-pentamethoxyl phenoxy group, 3,5-dimethoxy phenoxy group, 2,5-dimethoxy phenoxy group, 2,4,6-trimethoxy phenoxy group, 3,5-two (trifluoromethoxy) phenoxy group, 4-methoxyl group-3-Trifluoromethyl phenyl ether oxygen base, 2,6-dimethoxy phenoxy group, 2-Trifluoromethyl phenyl ether oxygen base, 3-Trifluoromethyl phenyl ether oxygen base, 4-Trifluoromethyl phenyl ether oxygen base, 2,3-two (trifluoromethoxy) phenoxy group, 2,4-two (trifluoromethoxy) phenoxy group, 2-five fluorine ethoxy phenoxies, 3-five fluorine ethoxy phenoxies, 4-five fluorine ethoxy phenoxies, 2-isopropoxy phenoxy group, 3-isopropoxy phenoxy group, 4-isopropoxy phenoxy group, 2-tert.-butoxy phenoxy group, 3-tert.-butoxy phenoxy group, 4-tert.-butoxy phenoxy group, 2-sec-butoxy phenoxy group, 3-sec-butoxy phenoxy group, 4-sec-butoxy phenoxy group, the positive hexyloxy phenoxy group of 4-, 2-is fluorine propoxy-phenoxy group just-seven, 3-is fluorine propoxy-phenoxy group just-seven, 4-is fluorine propoxy-phenoxy group just-seven, 2-(2-Phenoxyphenyl) phenoxy group, 2,3-two (2-Phenoxyphenyl) phenoxy group, 2,3-two (2-Phenoxyphenyl)-4-methoxyl group phenoxy group, 2,4-dimethoxy-3-(3-Phenoxyphenyl) phenoxy group, 3-(2,3-two Phenoxyphenyls) phenoxy group, 4-(2,4,6-triple phenoxyl phenyl) phenoxy group, 2-(3-(2-methoxyl group phenoxy group) phenyl) phenoxy group, 3-(4-(3-methoxyl group phenoxy group) phenyl) phenoxy group, 4-(2-(4-methoxyl group phenoxy group) phenyl) phenoxy group, 2-(3-(4-isopropoxy phenoxy group) phenyl) phenoxy group, 3-(4-(4-n-butoxy phenoxy group) phenyl) phenoxy group, (2-(2 for 4-, 4-dimethoxy phenoxy group) phenoxy group phenyl), (3-(2 for 2-, 3-dimethoxy phenoxy group) phenoxy group phenyl), (4-(2 for 3-, 3,4,5,6-pentamethoxyl phenoxy group) phenoxy group phenyl), (2-(3 for 4-, 5-dimethoxy phenoxy group) phenoxy group phenyl), (3-(2 for 2-, 5-dimethoxy phenoxy group) phenoxy group phenyl), (4-(2 for 3-, 4,6-trimethoxy phenoxy group) phenoxy group phenyl), (2-(3 for 4-, 5-two (trifluoromethoxy) phenoxy group) phenoxy group phenyl), 2-(3-(4-methoxyl group-3-Trifluoromethyl phenyl ether oxygen base) phenyl) phenoxy group, (4-(2 for 3-, 6-dimethoxy phenoxy group) phenoxy group phenyl), 4-(2-(2-Trifluoromethyl phenyl ether oxygen base) phenyl) phenoxy group, 2-(3-(3-Trifluoromethyl phenyl ether oxygen base) phenyl) phenoxy group, 3-(4-(4-Trifluoromethyl phenyl ether oxygen base) phenyl) phenoxy group, (2-(2 for 4-, 3-two (trifluoromethoxy) phenoxy group) phenoxy group phenyl), (3-(2 for 2-, 4-two (trifluoromethoxy) phenoxy group) phenoxy group phenyl), 3-(4-(2-five fluorine ethoxy phenoxies) phenyl) phenoxy group, 4-(2-(3-five fluorine ethoxy phenoxies) phenyl) phenoxy group, 2-(3-(4-five fluorine ethoxy phenoxies) phenyl) phenoxy group, 3-(4-(2-isopropoxy phenoxy group) phenyl) phenoxy group, 4-(2-(3-isopropoxy phenoxy group) phenyl) phenoxy group, 2-(3-(4-isopropoxy phenoxy group) phenyl) phenoxy group, 3-(2-(2-tert.-butoxy phenoxy group) phenyl) phenoxy group, 4-(2-(3-tert.-butoxy phenoxy group) phenyl) phenoxy group, 2-(3-(4-tert.-butoxy phenoxy group) phenyl) phenoxy group, 3-(4-(2-sec-butoxy phenoxy group) phenyl) phenoxy group, 2-(2-(3-sec-butoxy phenoxy group) phenyl) phenoxy group, 2-(3-(4-sec-butoxy phenoxy group) phenyl) phenoxy group, 4-(2-(the positive hexyloxy phenoxy group of 4-) phenyl) phenoxy group, 2-(3-(2-is fluorine propoxy-phenoxy group just-seven) phenyl) phenoxy group, 3-(4-(3-is fluorine propoxy-phenoxy group just-seven) phenyl) phenoxy group and 4-(2-(4-is fluorine propoxy-phenoxy group just-seven) phenyl) phenoxy group, its condition is on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 group, its phenyl that is selected from by halogen replacement or unsubstituted C1-C6 alkoxyl group and phenoxy group replacement (wherein on this benzyl ring, can be substituted with 1 to 5, replace or the unsubstituted C1-C6 alkoxyl group of preferred 1 to 3 halogen) group of forming.

High piperazinyl is (wherein on this high piperazine ring; can be substituted with the group that at least one is selected from following groups: the C1-C6 alkoxy carbonyl; phenyl C1-C6 alkyl is [wherein on this benzyl ring; can be substituted with at least one group; it is selected from by halogen atom; halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed]; [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom phenyl; halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed]; phenyl C1-C6 alkoxy carbonyl is [wherein on this benzyl ring; can be substituted with at least one group; it is selected from by halogen atom; halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed]; [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom the phenylamino formyl radical; halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed]; phenyl C2-C6 thiazolinyl is [wherein on this benzyl ring; can be substituted with at least one group; it is selected from by halogen atom; halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group] and benzoyl [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom; halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group]) example can comprise high piperazinyl; (1-for example; 2-, 3-, 4-; 5-; 6-or 7-) high piperazinyl; the high piperazinyl of 4-tert-butoxycarbonyl-1-; the high piperazinyl of 4-ethoxy carbonyl-1-; the high piperazinyl of 4-methoxycarbonyl-1-; 2, the high piperazinyl of 4-dimethoxy carbonyl-1-; 2,4; the high piperazinyl of 6-triethoxy carbonyl-1-; 4-(4-the trifluoro-methoxybenzyl)-high piperazinyl of 1-; 4-(4-benzyl chloride the base)-high piperazinyl of 1-; 4-(4-the methoxy-benzyl)-high piperazinyl of 1-; 4-(4-the bromobenzyl)-high piperazinyl of 1-; 4-(4-the methyl-benzyl)-high piperazinyl of 1-; 4-(2; the 4-dichloro benzyl)-the high piperazinyl of 1-; 4-(3, the 4-the dimethoxy-benzyl)-high piperazinyl of 1-; 4-(2,4; the 6-trifluoro-benzyl)-the high piperazinyl of 1-; 4-(3; the 4-dimethyl benzyl)-the high piperazinyl of 1-; 4-(2,4,6-trimethoxy the benzyl)-high piperazinyl of 1-; 4-(2; 4; the 6-trimethyl benzyl)-the high piperazinyl of 1-; 4-(4-iodine the benzyl)-high piperazinyl of 1-; 4-(4-the trifluoromethyl benzyl)-high piperazinyl of 1-; 4-(3, the 4-the dichloro benzyl)-high piperazinyl of 1-; 4-(3-(4-trifluoromethyl)-2-the propenyl)-high piperazinyl of 1-; 4-(3-(4-trifluoromethyl)-2-the propenyl)-high piperazinyl of 1-; 4-(4-trifluoromethyl the benzoyl)-high piperazinyl of 1-; 4-(3-(4-chloro-phenyl-)-2-the propenyl)-high piperazinyl of 1-; 4-(3-(4-aminomethyl phenyl)-2-the propenyl)-high piperazinyl of 1-; 4-(3-(4-p-methoxy-phenyl)-2-the propenyl)-high piperazinyl of 1-; 4-(3-(3, the 4-3,5-dimethylphenyl)-2-the propenyl)-high piperazinyl of 1-; (3-(3 for 4-; the 4-Dimethoxyphenyl)-the 2-propenyl)-the high piperazinyl of 1-; (3-(3 for 4-; 4, the 5-trimethylphenyl)-the 2-propenyl)-the high piperazinyl of 1-; (3-(3,4 for 4-; the 5-trimethoxyphenyl)-the 2-propenyl)-the high piperazinyl of 1-; (3-(3 for 4-; the 4-dichlorophenyl)-the 2-propenyl)-the high piperazinyl of 1-; 4-(3-(2,4, the 6-trifluorophenyl)-2-the propenyl)-high piperazinyl of 1-; 4-(3-(4-iodophenyl)-2-the propenyl)-high piperazinyl of 1-; 4-(3-(3-bromophenyl)-2-the propenyl)-high piperazinyl of 1-; 4-(4-the luorobenzyl)-high piperazinyl of 1-; 4-(4-the methyl benzoyl)-high piperazinyl of 1-; 4-(4-the anisoyl)-high piperazinyl of 1-; 4-(3; the 4-dimethylbenzoyl)-the high piperazinyl of 1-; 4-(2; 4-dimethoxy benzoyl)-the high piperazinyl of 1-; 4-(3,4, the 5-the trimethylbenzoyl)-high piperazinyl of 1-; 4-(2; 4; 6-trimethoxy benzoyl)-the high piperazinyl of 1-; 4-(4-the chlorobenzene formacyl)-high piperazinyl of 1-; 4-(2,4,6-trifluoromethyl benzonitrile the acyl group)-high piperazinyl of 1-; 4-(4-the benzoyl bromide)-high piperazinyl of 1-; 4-(4-iodobenzene the formyl radical)-high piperazinyl of 1-; 4-(3; 4-dichloro-benzoyl base)-the high piperazinyl of 1-; 4-(4-the fluoro benzoyl)-high piperazinyl of 1-; 4-benzyl-3-(3-phenyl-2-the propenyl)-high piperazinyl of 1-; 4-benzoyl-3; the high piperazinyl of 5-dibenzyl-1-; 2,7-dibenzyl-4-phenyl-Gao piperazinyl; 4-(4-the trifluoromethyl)-high piperazinyl of 1-; 4-(4-the Trifluoromethoxyphen-l)-high piperazinyl of 1-; 4-(4-the chloro-phenyl-)-high piperazinyl of 1-; 4-(4-the p-methoxy-phenyl)-high piperazinyl of 1-; 4-(4-the aminomethyl phenyl)-high piperazinyl of 1-; 4-(2, the 4-the Dimethoxyphenyl)-high piperazinyl of 1-; 4-(2; the 4-3,5-dimethylphenyl)-the high piperazinyl of 1-; 4-(2; 4, the 6-trimethoxyphenyl)-the high piperazinyl of 1-; 4-(2,4; the 6-trimethylphenyl)-the high piperazinyl of 1-; 4-(3; the 4-dichlorophenyl)-the high piperazinyl of 1-; 4-(2,4, the 6-the trifluorophenyl)-high piperazinyl of 1-; 4-(4-the bromophenyl)-high piperazinyl of 1-; 4-(4-the iodophenyl)-high piperazinyl of 1-; 4-(4-the fluorophenyl)-high piperazinyl of 1-; 4-(4-trifluoromethoxy the benzyloxycarbonyl)-high piperazinyl of 1-; 4-(4-chlorine the benzyloxycarbonyl)-high piperazinyl of 1-; 4-(4-methoxyl group benzyloxy base the carbonyl)-high piperazinyl of 1-; 4-(4-bromo-benzyloxy-the carbonyl)-high piperazinyl of 1-; 4-(4-methyl the benzyloxycarbonyl)-high piperazinyl of 1-; 4-(2; 4-dichloro-benzyloxy carbonyl)-the high piperazinyl of 1-; 4-(3; 4-dimethoxy benzyloxycarbonyl)-the high piperazinyl of 1-; 4-(2,4,6-trifluoromethyl benzyl oxy base the carbonyl)-high piperazinyl of 1-; 4-(3; 4-benzyloxy-dimethyl carbonyl)-the high piperazinyl of 1-; 4-(2; 4,6-trimethoxy benzyloxycarbonyl)-the high piperazinyl of 1-; 4-(2,4; 6-trimethylammonium benzyloxycarbonyl)-the high piperazinyl of 1-; 4-(4-iodine the benzyloxycarbonyl)-high piperazinyl of 1-; 4-(4-trifluoromethyl benzyloxy the carbonyl)-high piperazinyl of 1-; 4-(3; 4-dichloro-benzyloxy carbonyl)-the high piperazinyl of 1-; 4-(4-Trifluoromethoxyphen-l the carbamyl)-high piperazinyl of 1-; 4-(4-chloro-phenyl-the carbamyl)-high piperazinyl of 1-; 4-(4-p-methoxy-phenyl the carbamyl)-high piperazinyl of 1-; 4-(4-bromophenyl the carbamyl)-high piperazinyl of 1-; 4-(4-aminomethyl phenyl the carbamyl)-high piperazinyl of 1-; 4-(2,4 dichloro benzene base the carbamyl)-high piperazinyl of 1-; 4-(3,4-Dimethoxyphenyl the carbamyl)-high piperazinyl of 1-; 4-(2; 4; 6-trifluorophenyl carbamyl)-the high piperazinyl of 1-; 4-(3,4-3,5-dimethylphenyl the carbamyl)-high piperazinyl of 1-; 4-(2,4; 6-trimethoxyphenyl carbamyl)-the high piperazinyl of 1-; 4-(2; 4,6-trimethylphenyl carbamyl)-the high piperazinyl of 1-; 4-(4-iodophenyl the carbamyl)-high piperazinyl of 1-; 4-(4-trifluoromethyl the carbamyl)-high piperazinyl of 1-; 3,4-two (phenylamino the formyl radical)-high piperazinyl of 1-; 4-(2-(4-trifluoromethyl) ethyl)-high piperazinyl of 1-and 4-(3-(4-trifluoromethyl) propyl group)-high piperazinyl of 1-; its condition is on this high piperazine ring; can be substituted with 1 to 3 group that is selected from following groups: above-mentioned C1-C6 alkoxy carbonyl; above-mentioned phenyl C1-C6 alkyl [wherein on this benzyl ring, can be substituted with 1 to 5; preferred 1 to 3 group, it is selected from by halogen atom; halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed]; above-mentioned phenyl is [wherein on this benzyl ring; can be substituted with 1 to 5; preferred 1 to 3 group; it is selected from by halogen atom; halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed]; above-mentioned phenyl C1-C6 alkoxy carbonyl [wherein on this benzyl ring, can be substituted with 1 to 5; preferred 1 to 3 group, it is selected from by halogen atom; halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed]; above-mentioned phenylamino formyl radical is [wherein on this benzyl ring; can be substituted with 1 to 5; preferred 1 to 3 group; it is selected from by halogen atom; halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed]; [it is unsubstituted to above-mentioned phenyl C2-C6 thiazolinyl, and perhaps it is made up of 1 or 2 phenyl and thiazolinyl, and described phenyl can be substituted with 1 to 5; preferred 1 to 3 is selected from by halogen atom; group in the group of halogen replacement or unsubstituted C1-C6 alkyl and halogen replacement or unsubstituted C1-C6 alkoxyl group composition; described thiazolinyl contains 2 to 6 carbon atoms; and have 1 to 3 two key] and above-mentioned benzoyl [wherein on this benzyl ring, can be substituted with 1 to 5; preferred 1 to 3 group, it is selected from by halogen atom; halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed].

1,2,3, the 4-tetrahydro isoquinolyl (wherein this 1,2,3, on the 4-tetrahydroisoquinoline ring, can be substituted with at least one amino [wherein on this amino, can be substituted with at least one group, it is selected from by phenyl C1-C6 alkyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group) and the group of C1-C6 alkyl composition]) example can comprise 1,2,3, the 4-tetrahydro isoquinolyl, for example 1,2,3,4-tetrahydrochysene (1-, 2-, 3-, 4-, 5-, 6-, 7-or 8-) isoquinolyl, 4,6-diaminostilbene, 2,3,4-tetrahydrochysene-2-isoquinolyl, 4,6,7-triamino-1,2,3,4-tetrahydrochysene-2-isoquinolyl, 7-(N-methyl-N-(4-trifluoro-methoxybenzyl) amino)-1,2,3,4-tetrahydrochysene-2-isoquinolyl, 6-(4-Trifluoromethyl phenyl ether oxygen base)-1,2,3,4-tetrahydrochysene-2-isoquinolyl, 7-(N-methyl-N-(4-trifluoromethyl benzyl) amino)-1,2,3,4-tetrahydrochysene-2-isoquinolyl, 7-(N-methyl-N-(4-benzyl chloride base) amino)-1,2,3,4-tetrahydrochysene-2-isoquinolyl, 7-(N-(4-benzyl chloride base) amino)-1,2,3,4-tetrahydrochysene-2-isoquinolyl, 7-(N-methyl-N-(2,4,6-three (trifluoromethoxy) benzyl) amino)-1,2,3,4-tetrahydrochysene-2-isoquinolyl, 7-(N-methyl-N-(2,4-two (trifluoromethyl) benzyl) amino)-1,2,3,4-tetrahydrochysene-2-isoquinolyl and 7-(N-methyl-N-(2,3-diiodo-benzyl) amino)-1,2,3,4-tetrahydrochysene-2-isoquinolyl, its condition be this 1,2,3, on the 4-tetrahydroisoquinoline ring, can be substituted with 1 to 3 amino [wherein on this amino, can be substituted with 1 or 2 group, it is selected from by above-mentioned phenyl C1-C6 alkyl (wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 group, it is selected from by halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group) and the group of above-mentioned C1-C6 alkyl composition].

_ azoles base (wherein this _ the azoles ring on, can be substituted with the group that at least one is selected from following groups: phenyl is [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed], C1-C6 alkyl and piperidyl are [wherein on this piperidine ring, can be substituted with at least one phenoxy group (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, the group that halogen replacement or unsubstituted C1-C6 alkyl and halogen replacement or unsubstituted C1-C6 alkoxyl group are formed)] example) can comprise _ the azoles base, (2-for example, 4-or 5-) _ the azoles base, 4-(4-chloro-phenyl-)-2-_ azoles base, 4-(4-Trifluoromethoxyphen-l)-2-_ azoles base, 2-(4-trifluoromethyl)-4-_ azoles base, 4-(4-trifluoromethyl)-2-_ azoles base, 2-(4-Trifluoromethoxyphen-l)-4-_ azoles base, 4-(3, the 4-dichlorophenyl)-2-_ azoles base, 5-(4-bromophenyl)-2-_ azoles base, 4-(4-fluorophenyl)-2-_ azoles base, 5-(4-iodophenyl)-2-_ azoles base, 2-(2,4, the 6-trifluorophenyl)-4-_ azoles base, 4-(4-aminomethyl phenyl)-2-_ azoles base, 4-(3-p-methoxy-phenyl)-2-_ azoles base, 2-(3, the 4-3,5-dimethylphenyl)-5-_ azoles base, 4-(2, the 4-Dimethoxyphenyl)-2-_ azoles base, 4-(2,4, the 6-trimethylphenyl)-2-_ azoles base, 4-(3,4, the 5-trimethoxyphenyl)-2-_ azoles base, 4,5-phenylbenzene-2-_ azoles base, 2,4-phenylbenzene-5-_ azoles base and 4-methyl-5-(4-(4-Trifluoromethyl phenyl ether oxygen base)-(1-, 2-or 3-) piperidyl)-2-_ azoles base, its condition be this _ the azoles ring on, can be substituted with 1 or 2 group that is selected from following groups: phenyl is [wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed], above-mentioned C1-C6 alkyl and following piperidyl are [wherein on this piperidine ring, can be substituted with 1 to 3 phenoxy group (wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed)].

(wherein on this isoindoline ring, can be substituted with at least one group, it is selected from by halogen atom iso-dihydro-indole-group, the group that halogen replacement or unsubstituted C1-C6 alkyl and halogen replacement or unsubstituted C1-C6 alkoxyl group are formed) example can comprise iso-dihydro-indole-group, (1-, 2-, 4-or 5-) iso-dihydro-indole-group for example, 4-chloro-(1-, 2-, 3-, 5-, 6-or 7-)-iso-dihydro-indole-group, 4-trifluoromethyl-(1-, 2-, 3-, 5-, 6-or 7-)-iso-dihydro-indole-group, 4-trifluoromethoxy-(1-, 2-, 3-, 5-, 6-or 7-)-iso-dihydro-indole-group, 5-methyl-(1-, 2-, 3-, 4-, 6-or 7-)-iso-dihydro-indole-group, 4-methoxyl group-(1-, 2-, 3-, 5-, 6-or 7-) iso-dihydro-indole-group, 3,4-two fluoro-(1-, 2-, 5-, 6-or 7-) iso-dihydro-indole-group, 4,5,6-trichlorine (1-, 2-, 3-or 7-) iso-dihydro-indole-group, 4,5-dimethyl (1-, 2-, 3-, 6-or 7-) iso-dihydro-indole-group, 4,5,6-trimethylammonium (1-, 2-, 3-or 7-) iso-dihydro-indole-group, 4,5-dimethoxy (1-, 2-, 3-, 6-or 7-) iso-dihydro-indole-group, 4,5,6-trimethoxy (1-, 2-, 3-or 7-) iso-dihydro-indole-group and 1,1-dimethyl-5-bromo-(2-, 3-, 4-, 6-or 7-) iso-dihydro-indole-group, its condition is on this isoindoline ring, can be substituted with 1 to 3 machine choosing, it is selected from by above-mentioned halogen atom, group that above-mentioned halogen replaces or unsubstituted C1-C6 alkyl and the replacement of above-mentioned halogen or that unsubstituted C1-C6 alkoxyl group is formed.

Piperazinyl is [wherein on this piperazine ring, can be substituted with at least one phenyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, the group that halogen replacement or unsubstituted C1-C6 alkyl and halogen replacement or unsubstituted C1-C6 alkoxyl group are formed)] example can comprise piperazinyl, (1-for example, 2-or 3-) piperazinyl, the 4-phenyl-peiperazinyl, 2,4-phenylbenzene-1-piperazinyl, 2,4,5-triphenyl-1-piperazinyl, 4-(4-Trifluoromethoxyphen-l)-1-piperazinyl, 4-(4-trifluoromethyl)-1-piperazinyl, (4-chloro-phenyl--1-piperazinyl) methyl, 4-(2, the 4-dichlorophenyl)-the 1-piperazinyl, 4-(2,4, the 6-trifluorophenyl)-the 1-piperazinyl, 2,4-two (trifluoromethyl) phenyl-peiperazinyl and 2,4,6-three (trifluoromethoxy) phenyl-peiperazinyl, its condition is on this piperazine ring, can be substituted with above-mentioned 1 to 3 phenyl (wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed).

Thiazolyl is (wherein on this thiazole ring, can replace and have at least one to be selected from the group of following group: phenoxy group C1-C6 alkyl is [wherein on this benzyl ring, can replace at least one group is arranged, it selects free halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and halogen replaces or the group of unsubstituted C1-C6 alkoxyl composition]; Phenyl [wherein on this benzyl ring, can replace at least one group is arranged, it selects free halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and halogen replaces or the group of unsubstituted C1-C6 alkoxyl composition]; Phenyl C1-C6 alkyl [wherein on this benzyl ring, can replace at least one group is arranged, it selects free halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and halogen replaces or the group of unsubstituted C1-C6 alkoxyl composition]; Group-(W₁)oNR ³¹R ³²[W wherein₁Same as described above with o, R³¹And R³²May be the same or different, each represents a hydrogen atom, C1-C6 alkyl, phenyl (wherein the phenyl ring may be substituted with at least one group selected from the Consisting of a halogen atom, a halogen substituted or unsubstituted C1-C6 alkyl group and a halogen-substituted or unsubstituted C1-C6 alkoxy group) or a phenyl C1-C6 alkyl group (wherein the phenyl ring, can be taken Generation of at least one group selected from the group consisting of a halogen atom, a halogen substituted or unsubstituted C1-C6 alkyl and Halogen-substituted or unsubstituted C1-C6 alkoxy group)]; piperazinyl group [wherein the piperazine ring , It can be substituted with at least one phenyl (wherein the phenyl ring may be substituted with at least one A group selected from the group consisting of a halogen atom, a halogen substituted or unsubstituted C1-C6 alkyl group and a halogen substituted or Unsubstituted C1-C6 alkoxy group)]; piperidyl group [wherein the piperidine ring, and can be taken Generation of at least one group which is selected from a phenoxy group (wherein the phenyl ring may be substituted At least one group selected from the group consisting of a halogen atom, a halogen substituted or unsubstituted C1-C6 alkyl and halo Substituted or unsubstituted C1-C6 alkoxy group) and a phenyl C1-C6 alkyl groups]; and A phenoxy group [wherein the phenyl ring may be substituted with at least one group selected from the group consisting of a halogen atom, Halogen-substituted or unsubstituted C1-C6 alkyl group and a halogen-substituted or unsubstituted C1-C6 alkoxy Group]) may include a thiazolyl group, such as (2 -, 4 - or 5 -) thiazolyl group, 2 - ((4 - fluoro-methyl Phenoxy) methyl) -4 - thiazolyl group, a 4 - ((4 - fluoro-methoxyphenoxy) methyl) -2 - thiazolyl group, 2 - ((4 - fluoro-phenoxy) methyl) -4 - thiazolyl group, 2 - ((4 - chlorophenoxy) methyl) -4 - thiazole Group, 2 - ((3 - methoxyphenoxy) methyl) -4 - thiazolyl group, 2 - ((2 - methylphenoxy) methyl) -5 - Thiazolyl group, 2 - ((2,4 - dimethoxyphenyl) methyl) -5 - thiazolyl group, 2 - ((3,4 - dimethylphenyl Oxy) methyl)-4 - thiazolyl, 5 - ((2,4,6 - methoxyphenoxy) methyl) -2 - thiazolyl group, 2 - ((3,4,5 - trimethoxy-phenoxy) methyl) -4 - thiazolyl, 2 - ((2,4,6 - trifluorophenoxy) methyl Yl) -4 - thiazolyl, 4 - ((3,4 - dichlorophenoxy) methyl) -2 - thiazolyl group, 2 - ((4 - bromophenoxy) Methyl) -4 - thiazolyl group, 2 - ((4 - iodo-phenoxy) methyl) -4 - thiazolyl group, a 4 - ((4 - fluorophenoxy) Methyl) -2 - thiazolyl group, a 2,5 - diphenoxy-4 - thiazolyl, 4,5 - diphenoxy-2 - Thiazolyl, 2 - (4 - fluorophenyl) -4 - thiazolyl, 4 - (4 - fluorophenyl) -2 - thiazolyl, 2 - (4 - chlorophenyl Yl) -4 - thiazolyl, 4 - (4 - chlorophenyl)-2 - thiazolyl, 2 - (4 - trifluoromethyl-phenyl)-4 - thiazolyl Group, 2 - (4 - trifluoromethoxy-phenyl)-4 - thiazolyl, 4 - (4 - (trifluoromethyl) phenyl) -2 - thiazolyl group, 4 - (4 - trifluoromethoxy-phenyl) -2 - thiazolyl group, 2 - (3,4 - dichlorophenyl)-4 - thiazolyl, 4 - (3,4 - dichlorophenyl) -2 - thiazolyl group, a 4 - (2,4,6 - trifluoro-phenyl) -2 - thiazolyl, 5 - (4 - Bromophenyl)-2 - thiazolyl, 5 - (4 - fluorophenyl)-4 - thiazolyl, 2 - (4 - iodo-phenyl) -5 - thiazolyl group, 2 - (4 - methylphenyl)-4 - thiazolyl, 2 - (4 - methoxyphenyl) -4 - thiazolyl, 2 - (2,4 - dimethoxyphenyl Yl-phenyl) -5 - thiazolyl group, a 4 - (3,4 - dimethoxyphenyl)-2 - thiazolyl, 4 - (2,4,6 - trimethoxy Yl-phenyl) -5 - thiazolyl, 5 - (3,4,5 - trimethoxyphenyl) - 4 - thiazolyl group, 2,4 - diphenyl-5 - Thiazolyl, 4,5 - diphenyl - 2 - thiazolyl group, a 2 - phenyl-5 - phenoxy-methyl - 4 - thiazolyl, 2 - (4 - Fluorobenzyl)-4 - thiazolyl, 2 - (4 - chlorobenzyl) -4 - thiazolyl, 2 - (4 - (trifluoromethyl) benzyl) -4 - Thiazolyl, 2 - (4 - (Trifluoromethoxy) benzyl)-4 - thiazolyl, 2 - (3,4 - dichloro-benzyl)-4 - thiazolyl Yl, 4 - (2,4,6 - trifluoro-benzyl)-2 - thiazolyl, 5 - (4 - bromo-benzyl)-2 - thiazolyl, 5 - (4 - Fluorobenzyl)-4 - thiazolyl, 2 - (4 - iodo-benzyl)-5 - thiazolyl, 2 - (4 - methyl-benzyl)-4 - thiazolyl Group, 2 - (4 - methoxybenzyl) -4 - thiazolyl, 2 - (2,4 - dimethylbenzyl) -5 - thiazolyl group, 4 - (3,4 - dimethoxy-benzyl)-2 - thiazolyl, 4 - (2,4,6 - trimethyl-benzyl)-5 - thiazolyl, 5 - (3,4,5 - trimethoxy-benzyl)-4 - thiazolyl, 2,4 - dibenzyl-5 - thiazolyl, 4,5 - dibenzyl -2 - thiazolyl group, a 2 - benzyl-5 - phenoxy-methyl-4 - thiazolyl, 4 - (4 - chlorobenzyl) amino-2 - Thiazolyl, 4 - (4 - (Trifluoromethoxy) benzyl) amino-2 - thiazolyl, 4 - (4 - trifluoromethyl-benzyl) Amino-2 - thiazolyl, 4 - (N-methyl-N-(4 - chlorobenzyl) amino) -2 - thiazolyl, 4 - (N-methyl- -N-(4 - trifluoromethoxy-benzyl) amino) -2 - thiazolyl, 4 - (N-methyl-N-(4 - trifluoromethyl-benzyl Yl) amino) -2 - thiazolyl, 4 - (4 - chlorophenyl)-2 - thiazolyl, 4 - (4 - (trifluoromethoxy) benzene Yl) amino-2 - thiazolyl, 4 - (4 - trifluoromethyl-phenyl)-2 - thiazolyl, 4 - (N-methyl- -N-(4 - chlorophenyl) amino) -2 - thiazolyl, 4 - (N-methyl-N-(4 - trifluoromethoxy-phenyl) amino Yl) -2 - thiazolyl, 4 - (N-methyl-N-(4 - trifluoromethyl-phenyl) amino) -2 - thiazolyl, 4 - (4 - Chlorobenzyl) amino-2 - thiazolyl, 4 - (4 - (Trifluoromethoxy) benzyl) amino-2 - thiazolyl Yl, 4 - (4 - (trifluoromethyl) benzyl) amino-2 - thiazolyl, 4 - (N-methyl-N-(4 - chlorobenzyl) Aminomethyl) -2 - thiazolyl, 4 - (N-methyl-N-(4 - (trifluoromethoxy) benzyl) aminomethyl) -2 - Thiazolyl, 4 - (N-methyl-N-(4 - trifluoromethyl-benzyl) aminomethyl)-2 - thiazolyl, 4 - (4 - Chlorophenyl) amino-2 - thiazolyl, 4 - (4 - trifluoromethoxyphenyl) aminomethyl-2 - thiazolyl Yl, 4 - (4 - (trifluoromethyl) phenyl) amino-2 - thiazolyl, 4 - (N-methyl-N-(4 - chlorophenyl) Aminomethyl) -2 - thiazolyl, 4 - (N-methyl-N-(4 - trifluoromethoxyphenyl) aminomethyl) -2 - Thiazolyl, 4 - (N-methyl-N-(4 - trifluoromethyl-phenyl) aminomethyl) -2 - thiazolyl, 4 - (4 - Bromobenzyl)-2 - thiazolyl, 4 - (4 - methoxybenzyl) amino-2 - thiazolyl, 4 - (4 - methyl- Benzyl) amino-2 - thiazolyl, 4 - (N-methyl-N-(3,4 - dichlorobenzyl) amino) -2 - thiazolyl group, 4 - (N-methyl-N-(2,4 - dimethoxybenzyl) amino) -2 - thiazolyl, 4 - (N-methyl-N-(3,4 - Dimethylbenzyl) amino) -2 - thiazolyl, 4 - (4 - bromophenyl)-2 - thiazolyl, 4 - (4 - methoxy- Yl-phenyl)-2 - thiazolyl, 4 - (4 - methylphenyl)-2 - thiazolyl, 4 - (N-methyl- -N-(3,4 - dichlorophenyl) amino) -2 - thiazolyl, 4 - (N-methyl-N-(3,4 - dimethoxyphenyl) Amino) -2 - thiazolyl, 4 - (N-methyl-N-(2,4 - dimethylphenyl) amino) -2 - thiazolyl group, 4 - (4 - bromobenzyl) aminomethyl-2 - thiazolyl, 4 - (4 - methoxybenzyl) amino-2 - thiazolyl Yl, 4 - (4 - methylbenzyl) amino-2 - thiazolyl, 4 - (N-methyl-N-(3,4 - dichloro-benzyl) Aminomethyl) -2 - thiazolyl, 4 - (N-methyl-N-(4 - methoxybenzyl) aminomethyl) -2 - thiazolyl Yl, 4 - (N-methyl-N-(3,4 - dimethylbenzyl) aminomethyl)-2 - thiazolyl, 4 - (4 - bromophenyl) Aminomethyl-2 - thiazolyl, 4 - (4 - methoxyphenyl) aminomethyl-2 - thiazolyl, 4 - (4 - methyl- Phenyl)-aminomethyl-2 - thiazolyl, 4 - (N-methyl-N-(3,4 - dichlorophenyl) aminomethyl) -2 - Thiazolyl, 4 - (N-methyl-N-(2,4 - dimethoxyphenyl) aminomethyl)-2 - thiazolyl, 4 - (N- Methyl-N-(3,4 - dimethylphenyl) aminomethyl)-2 - thiazolyl, 4 - (4 - fluorobenzyl) amino-2 - Thiazolyl, 4 - (2,4,6 - trimethoxy-benzyl)-2 - thiazolyl, 4 - (3,4,5 - trimethyl-benzyl Yl) amino-2 - thiazolyl, 4 - (N-methyl-N-(4 - iodo-benzyl) amino) -2 - thiazolyl, 4 - (N- Methyl-N-(2,4,6 - trifluoro-benzyl)-amino) -2 - thiazolyl, 4 - (N-methyl-N-(4 - iodo-benzyl) Amino) -2 - thiazolyl, 4 - (4 - fluorophenyl)-2 - thiazolyl, 4 - (2,4,6 - trimethoxy Yl) amino-2 - thiazolyl, 4 - (3,4,5 - trimethylphenyl)-2 - thiazolyl, 4 - (N-methyl- -N-(4 - iodo-phenyl) amino) -2 - thiazolyl, 4 - (N-methyl-N-(2,4,6 - trifluoro-phenyl) amino Yl) -2 - thiazolyl, 4 - (4 - fluorobenzyl) amino-2 - thiazolyl, 4 - (3,4,6 - trimethoxy- Benzyl) amino-2 - thiazolyl, 4 - (2,4,6 - trimethyl-benzyl) amino-2 - thiazolyl, 4 - (N-methyl-N-(4 - iodo-benzyl) aminomethyl)-2 - thiazolyl, 4 - (N-methyl-N-(2,4,6 - Trifluoro-benzyl) aminomethyl)-2 - thiazolyl, 4 - (4 - fluorophenyl) amino-2 - thiazolyl, 4 - (2,4,6 - trimethoxyphenyl) aminomethyl-2 - thiazolyl, 4 - (3,4,5 - trimethylphenyl) Aminomethyl-2 - thiazolyl, 4 - (N-methyl-N-(4 - iodo-phenyl) aminomethyl) -2 - thiazolyl group, 4 - (N-methyl-N-(2,4,6 - trifluoro-phenyl) aminomethyl) -2 - thiazolyl, 4 - (N-methyl-N-(4 - Trifluoromethylphenyl) aminomethyl)-2 - thiazolyl, 4 - (4 - trifluoromethyl-methoxyphenoxy) -2 - thiazolyl Yl, 4 - (4 - trifluoromethyl-phenoxy)-2 - thiazolyl, 4 - (4 - chlorophenoxy)-2 - thiazolyl, 4 - (3,4 - dichlorophenoxy)-2 - thiazolyl, 4 - (4 - methoxyphenoxy)-2 - thiazolyl, 4 - (4 - Methylphenoxy)-2 - thiazolyl, 4 - (3,4 - dimethoxyphenyl)-2 - thiazolyl, 5 - (2,4 - Dimethylphenoxy) -4 - thiazolyl, 4 - (2,4,6 - trimethoxy)-5 - thiazolyl, 4 - (3,4,5 - trimethyl-phenoxy)-2 - thiazolyl, 4 - (4 - fluorophenoxy)-2 - thiazolyl, 2 - (4 - Bromophenyl)-5 - thiazolyl, 2 - (4 - iodo-phenoxy)-4 - thiazolyl, 5 - (2,4,6 - trifluoro-phenoxy Yl) -2 - thiazolyl, 4 - (4 - (4 - trifluoromethyl-phenyl) -1 - piperazinyl)-2 - thiazolyl, 4 - (4 - (4 - Trifluoromethoxy-phenyl) -1 - piperazinyl)-2 - thiazolyl, 4 - (4 - (4 - chlorophenyl) - 1-piperazinyl Yl) -2 - thiazolyl, 4 - (4 - (4 - (trifluoromethyl) phenoxy)-1 - piperazinyl) -2 - thiazolyl group, 4 - (4 - (4 - (trifluoromethoxy) phenoxy) - 1-piperazinyl)-2 - thiazolyl, 4 - (4 - (4 - chlorophenoxy Yl) - 1-piperazinyl)-2 - thiazolyl, 5 - (3,4 - diphenyl - 1-piperazinyl)-2 - thiazolyl, 2 - (3,4,5 - triphenyl - 1-piperazinyl)-4 - thiazolyl, 5 - (3,4,5 - triphenyl-1 - piperazinyl Yl) -4 - thiazolyl, 4 - (3,4 - diphenyl-1 - piperazinyl)-5 - thiazolyl, 4 - (4 - (4 - trifluoromethyl Methoxyphenyl) -1 - piperazinyl) -5 - phenoxy-2 - thiazolyl, 4 - (4 - (4 - (Trifluoromethoxy) phenoxy Yl) -1 - piperazinyl) -5 - phenoxy-2 - thiazolyl group, a 4 - phenyl - 2 - thiazolyl group, 2 - phenyl - 4 - thiazolyl Group, and 2 - (4 - benzyl - (1 -, 2 - or 3 -) piperidyl) - (4 - or 5 -) thiazolyl group, provided that the Thiazole ring, may be substituted with 1 or 2 groups selected from the following group: the phenoxy C1-C6 Alkyl group [wherein the phenyl ring may be substituted with 1 to 5, preferably 1 to 3 groups selected from the group A halogen atom, a halogen substituted or unsubstituted C1-C6 alkyl group and a halogen-substituted or unsubstituted C1-C6 Alkoxy group]; where the phenyl group [wherein the phenyl ring may be substituted with 1 to 5, Preferably from 1 to 3 groups selected from the group consisting of a halogen atom, a halogen substituted or unsubstituted C1-C6 alkyl and halo Su substituted or unsubstituted C1-C6 alkoxy group]; said phenyl C1-C6 alkyl group [wherein The phenyl ring may be substituted with 1 to 5, preferably 1 to 3 groups selected from the group consisting of a halogen atom, Halogen-substituted or unsubstituted C1-C6 alkyl group and a halogen-substituted or unsubstituted C1-C6 alkoxy Group]; groups - (W ...₁)oNR ³¹R ³²[W wherein₁Same as described above with o, R³¹And R³²can be identical or different, represent separately hydrogen atom, above-mentioned C1-C6 alkyl, above-mentioned phenyl is (wherein on this benzyl ring, can replace and have 1 to 5, preferred 1 to 3 group, it selects free halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl forms group) or above-mentioned phenyl C1-C6 alkyl (wherein on this benzyl ring, can replace and have 1 to 5, preferred 1 to 3 group, it selects free halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl forms)], above-mentioned piperazinyl is [wherein on this piperazine ring, can replace and at least 1 to 3 phenyl be arranged (wherein on this benzyl ring, can replace have 1 to 5, preferred 1 to 3 group, it selects free halogen atom, halogen to replace or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl forms group)], above-mentioned piperidyl is [wherein on this piperidines ring, can replace 1 to 3 group is arranged, it selects free phenoxy group (wherein on this benzyl ring, can replace have 1 to 5, preferred 1 to 3 group, it selects free halogen atom, halogen to replace or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl forms group) and the group of above-mentioned phenyl C1-C6 alkyl composition], and phenoxy group [wherein on this benzyl ring, can replace have 1 to 5, preferred 1 to 3 group, it selects free halogen atom, halogen to replace or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl forms group].

The C1-C6 alkyl of naphthyl substituted is (wherein on this naphthalene nucleus, can be substituted with at least one C1-C6 alkoxyl group) comprise beyond the C1-C6 alkyl of aforesaid naphthyl substituted, comprise that also naphthyl C1-C6 alkyl is (wherein on this naphthalene nucleus, can be substituted with 1 to 4 C1-C6 alkoxyl group), 2-(6-methoxyl group-2-naphthyl) methyl for example, (4-methoxyl group-1-naphthyl) methyl, 2-(4-methoxyl group-1-naphthyl) ethyl, (4-methoxyl group-1-naphthyl) methyl, 2-(3-oxyethyl group-1-naphthyl) ethyl, 2-positive propoxy-1-naphthyl methyl, 5-tert.-butoxy-2-naphthyl methyl, 6-n-pentyloxy-3-naphthyl methyl, the positive hexyloxy of 7--4-naphthyl methyl, 2-(2,4-dimethoxy-1-naphthyloxy) ethyl, 2-(1,1,4,4-tetramethoxy-5-naphthyloxy) ethyl etc.

Imidazolyl is (wherein on this imidazole ring, can be substituted with at least one group, it is selected from the group of being made up of halogen atom and nitro) comprise that imidazolyl is (wherein on this imidazole ring, can be substituted with 1 to 3 substituting group, it is selected from the group of being made up of halogen atom and nitro), (1-for example, 2-, 4-or 5-) imidazolyl, 2-chloro-4-nitro-(1-or 5-) imidazolyl, 2-bromo-(1-, 4-or 5-) imidazolyl, 4-fluoro-(1-, 2-or 5-) imidazolyl, 2,5-dichloro (1-or 4-) imidazolyl, 2,4,5-three chloro-1-imidazolyl, 2-nitro-(1-, 4-or 5-) imidazolyl, 4-nitro-(1-, 2-or 5-) imidazolyl, 2,5-dinitrobenzene-(1-or 4-) imidazolyl, 2,4,5-trinitro--1-imidazolyl etc.

Phenyl C1-C6 alkyl is (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by benzofuryl, halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed) comprise that aforesaid phenyl C1-C6 alkyl is (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed) in addition, also comprise phenyl C1-C6 alkyl, have on this moieties contain 1 to 6 carbon atom the straight or branched alkyl (wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 substituting group, it is selected from by benzofuryl, halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed), 4-((2-for example, 3-, 4-, 5-, 6-or 7-) benzofuryl) benzyl, 2-((2-, 3-, 4-, 5-, 6-or 7-) benzofuryl) benzyl, 3-((2-, 3-, 4-, 5-, 6-or 7-) benzofuryl) benzyl, 2,4-two ((2-, 3-, 4-, 5-, 6-or 7-) benzofuryl) benzyl, 2,4,6-three ((2-, 3-, 4-, 5-, 6-or 7-) benzofuryl) benzyl, 2-trifluoromethyl-4-(2-, 3-, 4-, 5-, 6-or 7-) benzofuryl) benzyl, 3-trifluoromethoxy-4-(2-, 3-, 4-, 5-, 6-or 7-) benzofuryl) benzyl, 4-chloro-3-(2-, 3-, 4-, 5-, 6-or 7-) benzofuryl) benzyl etc.

Furyl C1-C6 alkyl is [wherein on this furan nucleus, can be substituted with at least one phenyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, the group that halogen replacement or unsubstituted C1-C6 alkyl and halogen replacement or unsubstituted C1-C6 alkoxyl group are formed)] comprise furyl C1-C6 alkyl, have on this moieties contain 1 to 6 carbon atom the straight or branched alkyl [wherein on this furan nucleus, can be substituted with 1 to 3 aforesaid phenyl (wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 substituting group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed)], (2-or 3-) furyl methyl for example, 1-((2-or 3-) furyl) ethyl, 2-((2-or 3-) furyl) ethyl, 3-((2-or 3-) furyl) propyl group, 2-((2-or 3-) furyl) propyl group, 4-((2-or 3-) furyl) butyl, 5-((2-or 3-) furyl) amyl group, 4-((2-or 3-) furyl) amyl group, 6-((2-or 3-) furyl) hexyl, 1,1-dimethyl-2-((2-or 3-) furyl) ethyl, 2-methyl-3-((2-or 3-) furyl) propyl group, 2-(4-chloro-phenyl-)-(3-, 4-or 5-) furyl methyl, 2-(2-chloro-5-trifluoromethyl)-(3-, 4-or 5-) furyl methyl, 2-(4-Trifluoromethoxyphen-l)-(3-, 4-or 5-) furyl methyl, 2-(2, the 4-dichlorophenyl)-(3-, 4-or 5-) furyl methyl, 2-(2,4, the 6-trifluorophenyl)-(3-, 4-or 5-) furyl methyl, 2-(4-aminomethyl phenyl)-(3-, 4-or 5-) furyl methyl, 2-(4-p-methoxy-phenyl)-(3-, 4-or 5-) furyl methyl, 2-(2, the 4-3,5-dimethylphenyl)-(3-, 4-or 5-) furyl methyl, 2-(3, the 4-Dimethoxyphenyl)-(3-, 4-or 5-) furyl methyl, 2-(2,4, the 6-trimethylphenyl)-(3-, 4-or 5-) furyl methyl, 2-(3,4, the 5-trimethoxyphenyl)-(3-, 4-or 5-) furyl methyl, 2,4-phenylbenzene (3-or 5-) furyl methyl, 2,4,5-triphenyl-3-furyl methyl etc.

Pyridyl C1-C6 alkyl is [wherein on this pyridine ring, can be substituted with at least one group, it is selected from by furyl and phenyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, the group that halogen replacement or unsubstituted C1-C6 alkyl and halogen replacement or unsubstituted C1-C6 alkoxyl group are formed) group of forming] comprise beyond the aforesaid pyridyl C1-C6 alkyl, also comprise pyridyl C1-C6 alkyl, have on this moieties contain 1 to 6 carbon atom the straight or branched alkyl [wherein on this pyridine ring, can be substituted with 1 to 3 substituting group, it is selected from by furyl and aforesaid phenyl (wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 substituting group, it is selected from by benzofuryl, halogen atom, the group that halogen replacement or unsubstituted C1-C6 alkyl and halogen replacement or unsubstituted C1-C6 alkoxyl group are formed) group of forming], 3-(2-or 3-) furyl-(2-for example, 4-, 5-or 6-) pyridylmethyl, 2-(4-Trifluoromethoxyphen-l)-(3-, 4-, 5-or 6-) pyridylmethyl, 2-(4-trifluoromethyl)-(3-, 4-, 5-or 6-) pyridylmethyl, 2-(4-p-methoxy-phenyl)-(3-, 4-, 5-or 6-) pyridylmethyl, 2-(4-aminomethyl phenyl)-(3-, 4-, 5-or 6-) pyridylmethyl, 2-(3-chloro-4-fluorophenyl)-(3-, 4-, 5-or 6-) pyridylmethyl, 2-(2, the 4-Dimethoxyphenyl)-(3-, 4-, 5-or 6-) pyridylmethyl, 2-(3,4, the 5-trimethoxyphenyl)-(3-, 4-, 5-or 6-) pyridylmethyl, 2-(2, the 4-3,5-dimethylphenyl)-(3-, 4-, 5-or 6-) pyridylmethyl, 2-(2,4, the 6-trimethylphenyl)-(3-, 4-, 5-or 6-) pyridylmethyl, 2-(2,4, the 6-trichlorophenyl)-(3-, 4-, 5-or 6-) pyridylmethyl, 2-(3-chloro-4-Trifluoromethoxyphen-l)-(3-, 4-, 5-or 6-) pyridylmethyl, 2,4-two (2-or 3-) furyl (5-or 6-) pyridylmethyl, 2,4,6-triphenyl (3-or 5-) pyridylmethyl, 2-furyl-5-phenyl (3-, 4-or 6-) pyridylmethyl etc.

Benzothienyl C1-C6 alkyl is (wherein on this thionaphthene ring, can be substituted with at least one halogen atom) comprise the C1-C6 alkyl (it can be replaced by 1 to 3 halogen atom) that benzothienyl replaces on this cumarone ring, 2-thionaphthene ylmethyl for example, 1-(2-benzothienyl) ethyl, 2-(4-benzothienyl) ethyl, 3-(5-benzothienyl) propyl group, 4-(6-benzothienyl) butyl, 5-(7-benzothienyl) amyl group, 6-(2-benzothienyl) hexyl, 4-fluoro-2-thionaphthene ylmethyl, 5-fluoro-2-thionaphthene ylmethyl, 6-fluoro-2-thionaphthene ylmethyl, 7-fluoro-2-thionaphthene ylmethyl, 4-chloro-2-thionaphthene ylmethyl, 5-chloro-2-thionaphthene ylmethyl, 6-chloro-2-thionaphthene ylmethyl, 7-chloro-2-thionaphthene ylmethyl, 4-bromo-2-thionaphthene ylmethyl, 5-bromo-2-thionaphthene ylmethyl, 6-bromo-2-thionaphthene ylmethyl, 7-bromo-2-thionaphthene ylmethyl, 4-iodo-2-thionaphthene ylmethyl, 5-iodo-2-thionaphthene ylmethyl, 6-iodo-2-thionaphthene ylmethyl, 7-iodo-2-thionaphthene ylmethyl, 4-fluoro-3-thionaphthene ylmethyl, 5-fluoro-3-thionaphthene ylmethyl, 6-fluoro-3-thionaphthene ylmethyl, 7-fluoro-3-thionaphthene ylmethyl, 4-chloro-3-thionaphthene ylmethyl, 5-chloro-3-thionaphthene ylmethyl, 6-chloro-3-thionaphthene ylmethyl, 7-chloro-3-thionaphthene ylmethyl, 4-bromo-3-thionaphthene ylmethyl, 5-bromo-3-thionaphthene ylmethyl, 6-bromo-3-thionaphthene ylmethyl, 7-bromo-3-thionaphthene ylmethyl, 4-iodo-3-thionaphthene ylmethyl, 5-iodo-3-thionaphthene ylmethyl, 6-iodo-3-thionaphthene ylmethyl, 7-iodo-3-thionaphthene ylmethyl, 2-(4-fluoro-2-benzothienyl) ethyl, 2-(5-fluoro-2-benzothienyl) ethyl, 2-(6-fluoro-2-benzothienyl) ethyl, 2-(7-fluoro-2-benzothienyl) ethyl, 2-(4-chloro-2-benzothienyl) ethyl, 2-(5-chloro-2-benzothienyl) ethyl, 2-(6-chloro-2-benzothienyl) ethyl, 2-(7-chloro-2-benzothienyl) ethyl, 2-(4-fluoro-3-benzothienyl) methyl, 2-(5-fluoro-3-benzothienyl) methyl, 2-(6-fluoro-3-benzothienyl) ethyl, 2-(7-fluoro-3-benzothienyl) ethyl, 2-(4-chloro-3-benzothienyl) ethyl, 2-(5-chloro-3-benzothienyl) ethyl, 2-(6-chloro-3-benzothienyl) ethyl, 2-(7-chloro-3-benzothienyl) ethyl, 2-(4-fluoro-2-benzothienyl) ethyl, 6-(5-fluoro-2-benzothienyl) hexyl, 6-(6-fluoro-2-benzothienyl) hexyl, 6-(7-fluoro-2-benzothienyl) hexyl, 6-(4-chloro-2-benzothienyl) hexyl, 6-(5-chloro-2-benzothienyl) hexyl, 6-(6-chloro-2-benzothienyl) hexyl, 6-(7-chloro-2-benzothienyl) hexyl, 6-(4-fluoro-3-benzothienyl) methyl, 6-(5-fluoro-3-benzothienyl) hexyl, 6-(6-fluoro-3-benzothienyl) hexyl, 6-(7-fluoro-3-benzothienyl) hexyl, 6-(4-chloro-3-benzothienyl) hexyl, 6-(5-chloro-3-benzothienyl) hexyl, 6-(6-chloro-3-benzothienyl) hexyl, 6-(7-chloro-3-benzothienyl) hexyl, (2,4-two bromo-3-benzothienyls) methyl, (4,5,6-three chloro-3-benzothienyls) methyl etc.

Benzofuryl C2-C6 thiazolinyl is (wherein on this cumarone ring, can be substituted with at least one group, it is selected from by halogen atom, the group that halogen replacement or unsubstituted C1-C6 alkyl and halogen replacement or unsubstituted C1-C6 alkoxyl group are formed) comprises benzofuryl, the group that it is made up of benzofuryl and straight or branched thiazolinyl, described benzofuryl is unsubstituted or is selected from following substituting group by 1 to 3 and replaces: halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed, described thiazolinyl contains 2 to 6 carbon atoms, and has 1 to 3 two key.Benzofuryl C2-C6 thiazolinyl comprises trans and the cis form.Benzofuryl C2-C6 thiazolinyl comprises 2-((2-, 3-, 4-, 5-, 6-or 7-) benzofuryl) vinyl, 3-((2-, 3-, 4-, 5-, 6-or 7-) benzofuryl)-the 2-propenyl, 3-((2-, 3-, 4-, 5-, 6-or 7-) benzofuryl)-2-methyl-2-propenyl, 4-((2-, 3-, 4-, 5-, 6-or 7-) benzofuryl)-crotyl, 4-((2-, 3-, 4-, 5-, 6-or 7-) benzofuryl)-the 3-butenyl, 4-((2-, 3-, 4-, 5-, 6-or 7-) benzofuryl)-the 1,3-butadiene base, 5-((2-, 3-, 4-, 5-, 6-or 7-) benzofuryl)-1,3,5-hexatriene base, 6-((2-, 3-, 4-, 5-, 6-or 7-) benzofuryl)-1, the 3-hexadienyl, 3-(6-trifluoromethyl (2-(2-, 3-, 4-, 5-or 7-) benzofuryl)-the 2-propenyl, 3-(5-trifluoromethoxy (2-, 3-, 4-, 5-or 7-) benzofuryl)-the 2-propenyl, 3-(7-chloro-(2-, 3-, 4-, 5-or 7-) benzofuryl)-the 2-propenyl, 3-(2,6-dimethyl-(3-, 4-, 5-or 7-) benzofuryl)-the 2-propenyl, 3-(3,6-dimethoxy (2-, 3-, 4-, 5-or 7-) benzofuryl)-the 2-propenyl, 3-(4,5,6-trimethylammonium (2-, 3-or 7-) benzofuryl)-the 2-propenyl, 3-(3,5,6-trimethoxy (2-, 4-or 7-) benzofuryl)-the 2-propenyl, 3-(3-chloro-6-trifluoromethyl (2-, 3-, 4-, 5-or 7-) benzofuryl)-the 2-propenyl etc.

Thiazolyl is [wherein on this thiazole ring, can be substituted with at least one phenyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, the group that halogen replacement or unsubstituted C1-C6 alkyl and halogen replacement or unsubstituted C1-C6 alkoxyl group are formed) group of forming] comprise that thiazolyl is [wherein on this thiazole ring, can be substituted with 1 to 2 aforesaid phenyl (wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 substituting group, it is selected from by halogen atom, the group that halogen replacement or unsubstituted C1-C6 alkyl and halogen replacement or unsubstituted C1-C6 alkoxyl group are formed) group of forming], (2-for example, 4-or 5-) thiazolyl, 4-phenyl-(2-or 5-) thiazolyl, 2-phenyl-(4-or 5-) thiazolyl, 5-phenyl-(2-or 4-) thiazolyl, 2,5-phenylbenzene-4-thiazolyl, 2,4-phenylbenzene-5-thiazolyl, 2-(4-trifluoromethyl)-(4-or 5-) thiazolyl, 2-(4-Trifluoromethoxyphen-l)-(4-or 5-) thiazolyl, 2-(4-chloro-phenyl-)-(4-or 5-) thiazolyl, 2-(3-chloro-4-trifluoromethyl)-(4-or 5-) thiazolyl, 2-(4-aminomethyl phenyl)-(4-or 5-) thiazolyl, 2-(2, the 4-3,5-dimethylphenyl)-(4-or 5-) thiazolyl, 2-(3,4, the 6-trimethylphenyl)-(4-or 5-) thiazolyl, 2-(4-p-methoxy-phenyl)-(4-or 5-) thiazolyl, 2-(2, the 4-Dimethoxyphenyl)-(4-or 5-) thiazolyl, 2-(3,4, the 6-trimethoxyphenyl)-(4-or 5-) thiazolyl, 2-(2, the 4-dichlorophenyl)-(4-or 5-) thiazolyl, 2-(3,4, the 6-trifluorophenyl)-(4-or 5-) thiazolyl etc.

Isoindoline oxygen base [wherein on this isoindoline ring, can be substituted with at least one and be selected from following group: the C1-C6 alkoxy carbonyl, phenyl C1-C6 alkyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by benzofuryl, halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed), (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom phenyl C2-C6 thiazolinyl, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed), furyl C1-C6 alkyl is [wherein on this furan nucleus, (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom can be substituted with at least one phenyl, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed)], pyridyl C1-C6 alkyl is [wherein on this pyridine ring, can be substituted with at least one group, it is selected from by furyl and phenyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by benzofuryl, halogen atom, the group that halogen replacement or unsubstituted C1-C6 alkyl and halogen replacement or unsubstituted C1-C6 alkoxyl group are formed) group of forming], (wherein on this cumarone ring, can be substituted with at least one group, it is selected from by halogen atom benzofuryl C1-C6 alkyl, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed), benzothienyl C1-C6 alkyl is (wherein on this thionaphthene ring, can be substituted with at least one halogen atom), (wherein on this cumarone basic ring, can be substituted with at least one group, it is selected from by halogen atom benzofuryl C2-C6 thiazolinyl, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed), thiazolyl is [wherein on this thiazole ring, (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom can be substituted with at least one phenyl, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group)] and phenoxy group C1-C6 alkyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, the group that halogen replacement or unsubstituted C1-C6 alkyl and halogen replacement or unsubstituted C1-C6 alkoxyl group are formed) group of forming] comprise that isoindoline oxygen base [wherein on this isoindoline ring, can be substituted with 1 to 3 substituting group, it is selected from the straight or branched C1-C6 alkoxy carbonyl that contains 1 to 6 carbon atom by aforesaid, aforesaid phenyl C1-C6 alkyl (having the straight or branched alkyl on this moieties) is (wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 substituting group, it is selected from by benzofuryl, halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed), aforesaid phenyl C2-C6 thiazolinyl (have the straight or branched thiazolinyl that contains 2 to 6 carbon atoms and have 1 to 3 two key on this alkenyl part, comprise trans and the cis form) is (wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 substituting group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed), aforesaid furyl C1-C6 alkyl (having the straight or branched alkyl that contains 1 to 6 carbon atom on this moieties) [wherein on this furan nucleus, can be substituted with 1 to 3 phenyl and (wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 substituting group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed)], aforesaid pyridyl C1-C6 alkyl (having the straight or branched alkyl that contains 1 to 6 carbon atom on this moieties) is [wherein on this pyridine ring, can be substituted with 1 to 3 substituting group, it is selected from by furyl and phenyl (wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 substituting group, it is selected from by benzofuryl, halogen atom, the group that halogen replacement or unsubstituted C1-C6 alkyl and halogen replacement or unsubstituted C1-C6 alkoxyl group are formed) group of forming], aforesaid benzofuryl C1-C6 alkyl (having the straight or branched alkyl that contains 1 to 6 carbon atom on this moieties) is (wherein on this cumarone ring, can be substituted with 1 to 3 substituting group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed), aforesaid benzothienyl C1-C6 alkyl (having the straight or branched alkyl that contains 1 to 6 carbon atom on this moieties) (wherein on this thionaphthene ring, can be substituted with 1 to 3 halogen atom), aforesaid benzofuryl C2-C6 thiazolinyl (has the straight or branched thiazolinyl that contains 2 to 6 carbon atoms and have 1 to 3 two key on this alkenyl part, comprise trans and the cis form) (wherein on this cumarone ring, can be substituted with 1 to 3 substituting group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed), aforesaid thiazolyl [wherein on this thiazole ring, can be substituted with 1 to 2 phenyl (wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 substituting group, it is selected from by halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group)] and aforesaid phenoxy group C1-C6 alkyl (having the straight or branched alkyl that contains 1 to 6 carbon atom on this moieties) (wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 substituting group, it is selected from by halogen atom, the group that halogen replacement or unsubstituted C1-C6 alkyl and halogen replacement or unsubstituted C1-C6 alkoxyl group are formed) group of forming], (1-for example, 2-, 3-or 4-) isoindoline oxygen base, 1-tert-butoxycarbonyl-(2-, 3-or 4-) isoindoline oxygen base, 1-(2-(4-chloro-phenyl-)-(3-, 4-or 5-) furyl methyl)-(2-, 3-or 4-) isoindoline oxygen base, 1-(2-(2-chloro-5-trifluoromethyl)-(3-, 4-or 5-) furyl methyl)-(2-, 3-or 4-) isoindoline oxygen base, 1-(3-trifluoromethyl-4-benzyl chloride base)-(2-, 3-or 4-) isoindoline oxygen base, 1-(4-((2-, 3-, 4-, 5-, 6-or 7-) benzofuryl) benzyl)-(2-, 3-or 4-) isoindoline oxygen base, 1-(3-((2-or 3-) furyl)-(2-, 4-, 5-or 6-) pyridylmethyl)-(2-, 3-or 4-) isoindoline oxygen base, 1-(2-(4-Trifluoromethoxyphen-l)-(3-, 4-, 5-or 6-) pyridylmethyl)-(2-, 3-or 4-) isoindoline oxygen base, 1-(2-(3-chloro-4-fluorophenyl)-(3-, 4-, 5-or 6-) pyridylmethyl)-(2-, 3-or 4-) isoindoline oxygen base, 1-(6-trifluoromethyl (2-, 3-, 4-, 5-or 7-) the cumarone ylmethyl)-(2-, 3-or 4-) isoindoline oxygen base, 1-(5-chloro-(2-, 3-, 4-, 6-or 7-) the thionaphthene ylmethyl)-(2-, 3-or 4-) isoindoline oxygen base, 1-(6-chlorine (2-, 3-, 4-, 5-or 7-) the cumarone ylmethyl)-(2-, 3-or 4-) isoindoline oxygen base, 1-(5-trifluoromethoxy (2-, 3-, 4-, 6-or 7-) the cumarone ylmethyl)-(2-, 3-or 4-) isoindoline oxygen base, 1-(3-(6-trifluoromethyl (2-, 3-, 4-, 5-or 7-) benzofuryl)-the 2-propenyl)-(2-, 3-or 4-) isoindoline oxygen base, 1-(5-chloro-(2-, 3-, 4-, 6-or 7-) the cumarone ylmethyl)-(2-, 3-or 4-) isoindoline oxygen base, 1-(2-(4-trifluoromethyl)-(4-or 5-) thiazolyl methyl)-(2-, 3-or 4-) isoindoline oxygen base, 1-(2-(4-Trifluoromethyl phenyl ether oxygen base) ethyl)-(2-, 3-or 4-) isoindoline oxygen base, 1,3-di ethoxy carbonyl-(2-or 4-) isoindoline oxygen base, 2-phenoxymethyl-4-((2-, 3-, 4-, 5-, 6-or 7-) the cumarone ylmethyl)-(1-, 3-, 5-, 6-or 7-) isoindoline oxygen base, 2-((2-or 3-) furyl methyl)-4,5-dimethoxy carbonyl-(1-, 3-, 6-or 7-) isoindoline oxygen base etc.

The benzothiazole alkoxyl group is [wherein on this benzothiazole alkane (benzothiazolydine) ring, can be substituted with at least one group, it is selected from by oxo base and phenyl C1-C6 alkyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, the group that halogen replacement or unsubstituted C1-C6 alkyl and halogen replacement or unsubstituted C1-C6 alkoxyl group are formed) group of forming] comprise that the benzothiazole alkoxyl group is [wherein on this benzothiazole alkane ring, can be substituted with 1 to 3 substituting group, it is selected from by oxo base and aforesaid phenyl C1-C6 alkyl (having the straight or branched alkyl that contains 1 to 6 carbon atom on this moieties) (wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 substituting group, it is selected from by halogen atom, the group that halogen replacement or unsubstituted C1-C6 alkyl and halogen replacement or unsubstituted C1-C6 alkoxyl group are formed) group of forming], (2-for example, 3-, 4-, 5-, 6-or 7-) the benzothiazole alkoxyl group, 3-(4-trifluoro-methoxybenzyl)-2-oxo-(4-, 5-, 6-or 7-) the benzothiazole alkoxyl group, 3-(4-trifluoromethyl benzyl)-(2-, 4-, 5-, 6-or 7-) the benzothiazole alkoxyl group, 3-(4-benzyl chloride base)-(2-, 4-, 5-, 6-or 7-) the benzothiazole alkoxyl group, 3-(4-methyl-benzyl)-(2-, 4-, 5-, 6-or 7-) the benzothiazole alkoxyl group, 3-(3, the 4-dimethyl benzyl)-(2-, 4-, 5-, 6-or 7-) the benzothiazole alkoxyl group, 3-(2,4, the 6-trimethyl benzyl)-(2-, 4-, 5-, 6-or 7-) the benzothiazole alkoxyl group, 3-(4-methoxy-benzyl)-(2-, 4-, 5-, 6-or 7-) the benzothiazole alkoxyl group, 3-(3, the 4-dimethoxy-benzyl)-(2-, 4-, 5-, 6-or 7-) the benzothiazole alkoxyl group, 3-(3,4,5-trimethoxy benzyl)-(2-, 4-, 5-, 6-or 7-) the benzothiazole alkoxyl group, 3-(4-luorobenzyl)-(2-, 4-, 5-6-or 7-) the benzothiazole alkoxyl group, 3-(3, the 4-dichloro benzyl)-(2-, 4-, 5-, 6-or 7-) the benzothiazole alkoxyl group, 3-(2,4, the 6-trifluoro-benzyl)-(2-, 4-, 5-, 6-or 7-) the benzothiazole alkoxyl group, 2-oxo-(2-, 4-, 5-, 6-or 7-) the benzothiazole alkoxyl group, 2,3-dibenzyl (4-, 5-, 6-or 7-) the benzothiazole alkoxyl group, 2,3,5-tribenzyl (4-, 5-, 6-or 7-) the benzothiazole alkoxyl group etc.

Indoxyl is [wherein on this indole ring, can be substituted with at least one phenyl C1-C6 alkyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed)] comprise that indoxyl is [wherein on this indole ring, can be substituted with 1 to 3 aforesaid phenyl C1-C6 alkyl, have on this moieties contain 1 to 6 carbon atom the straight or branched alkyl (wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 substituting group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed)], for example (1-, 2-, 3-, 4-, 5-, 6-or 7-) indoxyl, 1-(4-trifluoro-methoxybenzyl)-(2-, 3-, 4-, 5-, 6-or 7-) indoxyl, 1-(4-trifluoromethyl benzyl)-(2-, 3-, 4-, 5-, 6-or 7-) indoxyl, 1-(4-benzyl chloride base)-(2-, 3-, 4-, 5-, 6-or 7-) indoxyl, 2-(4-methyl-benzyl)-(1-, 3-, 4-, 5-, 6-or 7-) indoxyl, 3-(3, the 4-dimethyl benzyl)-(1-, 2-, 4-, 5-, 6-or 7-) indoxyl, 4-(2,4, the 6-trimethyl benzyl)-(1-, 2-, 3-, 5-, 6-or 7-) indoxyl, 5-(4-methoxy-benzyl)-(1-, 2-, 3-, 4-, 6-or 7-) indoxyl, 6-(3, the 4-dimethoxy-benzyl)-(1-, 2-, 3-, 4-, 5-or 7-) indoxyl, 7-(3,4,5-trimethoxy benzyl)-(1-, 2-, 3-, 4-, 5-or 6-) indoxyl, 1-(4-luorobenzyl)-(2-, 3-, 4-, 5-, 6-or 7-) indoxyl, 1-(3, the 4-dichloro benzyl)-(2-, 3-, 4-, 5-, 6-or 7-) indoxyl, 1-(2,4, the 6-trifluoro-benzyl)-(2-, 3-, 4-, 5-, 6-or 7-) indoxyl, 1,3-dibenzyl (2-, 4-, 5-, 6-or 7-) indoxyl, 1,3,5-tribenzyl (2-, 4-, 6-or 7-) indoxyl etc.

Pyrrolidyl is [wherein on this pyrrolidine ring, be substituted with at least one amino (wherein on this amino, can be substituted with at least one group, it is selected from by C1-C6 alkyl and phenyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, the group that halogen replacement or unsubstituted C1-C6 alkyl and halogen replacement or unsubstituted C1-C6 alkoxyl group are formed) group of forming)] comprises that pyrrolidyl is [wherein on this pyrrolidine ring, be substituted with 1 to 3 (wherein on this amino, can be substituted with 1 to 5, preferred 1 to 3 substituting group, it is selected from by aforesaid C1-C6 alkyl and aforesaid phenyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, the group that halogen replacement or unsubstituted C1-C6 alkyl and halogen replacement or unsubstituted C1-C6 alkoxyl group are formed) group of forming)], 3-(N-methyl-N-(3 for example, the 4-dichlorophenyl) amino)-(1-, 2-, 4-or 5-) pyrrolidyl, 3-amino-(1-, 2-, 4-or 5-) pyrrolidyl, 2,3-diamino-(1-, 4-or 5-) pyrrolidyl, 2,3,5-triamino-(1-or 4-) pyrrolidyl, 3-(N-methyl-N-(4-aminomethyl phenyl) amino)-(1-, 2-, 4-or 5-) pyrrolidyl, 3-(N-ethyl-N-(3-p-methoxy-phenyl) amino)-(1-, 2-, 4-or 5-) pyrrolidyl, 3-(N-(4-trifluoromethyl) amino)-(1-, 2-, 4-or 5-) pyrrolidyl, 3-(N-(4-Trifluoromethoxyphen-l) amino)-(1-, 2-, 4-or 5-) pyrrolidyl, 3-(N-methyl-N-(3,4, the 5-trifluorophenyl) amino)-(1-, 2-, 4-or 5-) pyrrolidyl, 3-(N-methyl-N-(3-chloro-4-trifluoromethyl) amino)-(1-, 2-, 4-or 5-) pyrrolidyl, 3-(N-phenyl amino)-(1-, 2-, 4-or 5-) pyrrolidyl, 3-methylamino-(1-, 2-, 4-or 5-) pyrrolidyl, 3-methylamino (1-, 2-, 4-or 5-) pyrrolidyl etc.

Indolinyl (wherein on this indoline ring, can be substituted with at least one halogen atom) comprises indolinyl (wherein on this indoline ring, can be substituted with 1 to 3 halogen atom), for example (1-, 2-, 3-, 4-, 5-, 6-or 7-) indolinyl, 5-bromo-(1-, 2-, 3-, 4-, 6-or 7-) indolinyl, 4-chloro-(1-, 2-, 3-, 5-, 6-or 7-) indolinyl, 6-fluoro-(1-, 2-, 3-, 4-, 5-or 7-) indolinyl, 5,7-two chloro-(1-, 2-, 3-, 4-or 6-) indolinyl, 3,5,6-three fluoro-(1-, 2-, 4-or 7-) indolinyl etc.

Indoline oxygen base is [wherein on this indoline ring, can be substituted with at least one group, it is selected from by phenyl C1-C6 alkyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group) and the group of oxo base composition] comprise that indoline oxygen base is [wherein on this indoline ring, can be substituted with 1 to 3 substituting group, it is selected from by aforesaid phenyl C1-C6 alkyl (having the straight or branched alkyl that contains 1 to 6 carbon atom on this moieties) (wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 substituting group, it is selected from by halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group) and the group of oxo base composition], (1-for example, 2-, 3-, 4-, 5-, 6-or 7-) indoline oxygen base, 1-(4-trifluoro-methoxybenzyl)-2,3-dioxo (1-, 2-, 3-, 4-, 5-, 6-or 7-) indoline oxygen base, 1-(4-trifluoro-methoxybenzyl)-2-oxo (3-, 4-, 5-, 6-or 7-) indoline oxygen base, 1-(4-trifluoromethyl benzyl)-(2-, 3-, 4-, 5-, 6-or 7-) indoline oxygen base, 1-(4-benzyl chloride base)-(2-, 3-, 4-, 5-, 6-or 7-) indoline oxygen base, 3-(4-methyl-benzyl)-(1-, 2-, 4-, 5-, 6-or 7-) indoline oxygen base, 4-(3, the 4-dimethyl benzyl)-(1-, 2-, 3-, 5-, 6-or 7-) indoline oxygen base, 2-(2,4, the 6-trimethyl benzyl)-(1-, 3-, 4-, 5-, 6-or 7-) indoline oxygen base, 5-(4-methoxy-benzyl)-(1-, 2-, 3-, 4-, 6-or 7-) indoline oxygen base, 6-(3, the 4-dimethoxy-benzyl)-(1-, 2-, 3-, 4-, 5-or 7-) indoline oxygen base, 7-(3,4,5-trimethoxy benzyl)-(1-, 2-, 3-, 4,5-or 6-) indoline oxygen base, 1-(4-luorobenzyl)-(2-, 3-, 4-, 5-, 6-or 7-) indoline oxygen base, 1-(3, the 4-dichloro benzyl)-(2-, 3-, 4-, 5-, 6-or 7-) indoline oxygen base, 1-(2,4, the 6-trifluoro-benzyl)-(2-, 3-, 4-, 5-, 6-or 7-) indoline oxygen base, 2-oxo-(1-, 3-, 4-, 5-, 6-or 7-) indoline oxygen base, 1,3-dibenzyl (2-, 4-, 5-, 6-or 7-) indoline oxygen base, 1,5,6-tribenzyl (1-, 2-, 3-, 4-or 7-) indoline oxygen base, 2,3-dioxo (1-, 4-, 5-, 6-or 7-) indoline oxygen base etc.

Pyrryl is [wherein on this pyrrole ring, can be substituted with at least one group, it is selected from by C1-C6 alkyl and phenyl C1-C6 alkyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and halogen group that replace or that unsubstituted C1-C6 alkoxyl group is formed) group of forming] comprise that pyrryl is [wherein on this pyrrole ring, can be substituted with 1 to 3 substituting group, it is selected from by aforesaid C1-C6 alkyl and aforesaid phenyl C1-C6 alkyl (having the straight or branched alkyl that contains 1 to 6 carbon atom on this moieties) (wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 substituting group, it is selected from by halogen atom, the group that halogen replacement or unsubstituted C1-C6 alkyl and halogen replacement or unsubstituted C1-C6 alkoxyl group are formed) group of forming], (1-for example, 2-or 3-) pyrryl, 1-(4-trifluoro-methoxybenzyl)-(2-or 3-) pyrryl, 1-(4-trifluoromethyl benzyl)-(2-or 3-) pyrryl, 1-(4-benzyl chloride base)-(2-or 3-) pyrryl, 1-(4-methoxy-benzyl)-(2-or 3-) pyrryl, 1-(4-methyl-benzyl)-(2-or 3-) pyrryl, 1-(3, the 4-dimethoxy-benzyl)-(2-or 3-) pyrryl, 1-(2,4,6-trimethoxy benzyl)-(2-or 3-) pyrryl, 1-(3, the 4-dimethyl benzyl)-(2-or 3-) pyrryl, 1-(2,4, the 6-trimethyl benzyl)-(2-or 3-) pyrryl, 1-(2,4, the 6-trifluoro-benzyl)-(2-or 3-) pyrryl, 1-(2, the 6-dichloro benzyl)-(2-or 3-) pyrryl, 1-benzyl-(2-or 3-) pyrryl, 1,2-dibenzyl-(3-, 4-or 5-) pyrryl, 1,2,4-tribenzyl-(3-or 5-) pyrryl, 2-(3-chloro-4-trifluoro-methoxybenzyl)-(1-, 3-, 4-or 5-) pyrryl, 1-methyl-(2-or 3-) pyrryl, 1-ethyl-(2-or 3-) pyrryl, 1-n-propyl-(2-or 3-) pyrryl, 1-normal-butyl-(2-or 3-) pyrryl, 1-n-pentyl-(2-or 3-) pyrryl, 1-hexyl-(2-or 3-) pyrryl, 1,3-dimethyl-(2-, 4-or 5-) pyrryl, 1,3,4-trimethylammonium-(2-or 5-) pyrryl, 1-benzyl-3-methyl-(2-, 4-or 5-) pyrryl etc.

Thiophenyl is (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, the group that halogen replacement or unsubstituted C1-C6 alkyl and halogen replacement or unsubstituted C1-C6 alkoxyl group are formed) comprises thiophenyl, it is unsubstituted or has 1 to 5, preferred 1 to 3 is selected from following substituting group: halogen atom as defined above, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed, the example comprises thiophenyl, 2-fluorobenzene sulfenyl, 3-fluorobenzene sulfenyl, 4-fluorobenzene sulfenyl, 2-chlorobenzene sulfenyl, 3-chlorobenzene sulfenyl, 4-chlorobenzene sulfenyl, 2-bromobenzene sulfenyl, 3-bromobenzene sulfenyl, the 4-bromophenyl, 2-iodobenzene sulfenyl, 3-iodobenzene sulfenyl, 4-iodobenzene sulfenyl, 2,3-difluoro thiophenyl, 3, the 4-difluorophenyl, 3,5-difluoro thiophenyl, 2,4-difluoro thiophenyl, 2,6-difluoro thiophenyl, 2,3-dichlorobenzene sulfenyl, 3,4-dichlorobenzene sulfenyl, 3,5-dichlorobenzene sulfenyl, 2,4-dichlorobenzene sulfenyl, 2,6-dichlorobenzene sulfenyl, 3,4,5-trifluoro-benzene sulfenyl, 3,4,5-trichlorobenzene sulfenyl, 2,4,6-trifluoro-benzene sulfenyl, 2,4,6-trichlorobenzene sulfenyl, 2-fluoro-4-bromobenzene sulfenyl, 4-chloro-3-fluorobenzene sulfenyl, 2,3,4-trichlorobenzene sulfenyl, 2,3,4,5,6-penta fluoro benzene sulfenyl, 2,4,6-Three methyl Benzene sulfenyl, 4-n-butylbenzene sulfenyl, 2,4-dimethyl benzene sulfenyl, 2,3-dimethyl benzene sulfenyl, 2,6-dimethyl benzene sulfenyl, 3,5-dimethyl benzene sulfenyl, 2,5-dimethyl benzene sulfenyl, 3,5-two trifluoromethyl thiophenyls, 4-n-butoxy thiophenyl, 2,4-dimethoxy thiophenyl, 2,3-dimethoxy thiophenyl, 2,6-dimethoxy thiophenyl, 3,5-dimethoxy thiophenyl, 2,5-dimethoxy thiophenyl, 2,4,6-trimethoxy thiophenyl, 3,5-two trifluoromethoxy thiophenyls, 3-chloro-4-anisole sulfenyl, 2-chloro-4-trifluoromethoxy thiophenyl, 3-methyl-4-fluorobenzene sulfenyl, 4-bromo-3-trifluoromethyl thiophenyl, 2-methylbenzene sulfenyl, 3-methylbenzene sulfenyl, 4-methylbenzene sulfenyl, 2-methyl-3-chlorobenzene sulfenyl, 3-methyl-4-chlorobenzene sulfenyl, 2-chloro-4-methylbenzene sulfenyl, 2-methyl-3-fluorobenzene sulfenyl, 2-trifluoromethyl thiophenyl, 3-trifluoromethyl thiophenyl, 4-trifluoromethyl thiophenyl, 2-pentafluoroethyl group thiophenyl, 3-pentafluoroethyl group thiophenyl, 4-pentafluoroethyl group thiophenyl, 2-isopropyl benzene sulfenyl, 3-isopropyl benzene sulfenyl, 4-isopropyl benzene sulfenyl, 2-tert.-butylbenzene sulfenyl, 3-tert.-butylbenzene sulfenyl, 4-tert.-butylbenzene sulfenyl, 2-sec-butylbenzene sulfenyl, 3-sec-butylbenzene sulfenyl, 4-sec-butylbenzene sulfenyl, 2-is the fluoropropyl thiophenyl just-seven, 3-is the fluoropropyl thiophenyl just-seven, 4-is the fluoropropyl thiophenyl just-seven, 4-amylbenzene sulfenyl, 4-hexyl benzene sulfenyl, 2-anisole sulfenyl, 3-anisole sulfenyl, 4-anisole sulfenyl, 3-chloro-2-anisole sulfenyl, 2-fluoro-3-anisole sulfenyl, 2-fluoro-4-anisole sulfenyl, 2,3,4-trifluoro-benzene sulfenyl, 2-trifluoromethoxy thiophenyl, 3-trifluoromethoxy thiophenyl, 4-trifluoromethoxy thiophenyl, 3-fluoro-2-trifluoromethoxy thiophenyl, 2-fluoro-3-trifluoromethoxy thiophenyl, 3-fluoro-4-trifluoromethoxy thiophenyl, 3-chloro-2-trifluoromethoxy thiophenyl, 2-chloro-3-trifluoromethoxy thiophenyl, 3-chloro-4-trifluoromethoxy thiophenyl, 2-five fluorine phenetole sulfenyls, 3-five fluorine phenetole sulfenyls, 4-five fluorine phenetole sulfenyls, 3-chloro-2-five fluorine phenetole sulfenyls, 2-chloro-3-five fluorine phenetole sulfenyls, 3-chloro-4-five fluorine phenetole sulfenyls, 2-isopropoxy thiophenyl, 3-isopropoxy thiophenyl, 4-isopropoxy thiophenyl, 2-tert.-butoxy thiophenyl, 3-tert.-butoxy thiophenyl, 4-tert.-butoxy thiophenyl, 2-sec-butoxy thiophenyl, 3-sec-butoxy thiophenyl, 4-sec-butoxy thiophenyl, 2-is fluorine propoxy-thiophenyl just-seven, 3-is fluorine propoxy-thiophenyl just-seven, 4-is fluorine propoxy-thiophenyl just-seven, 4-n-pentyloxy thiophenyl, the positive hexyloxy thiophenyl of 4-etc.

Piperazinyl is [wherein on this piperazine ring, can be substituted with at least one group, it is selected from by phenyl C1-C6 alkyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed), phenyl is [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by phenoxy group (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed), halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group] and phenyl C2-C6 thiazolinyl [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group] group formed] comprise that aforesaid piperazinyl is [wherein on this piperazinyl ring, can be substituted with at least one phenyl C1-C6 alkyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed)] in addition, comprise that also piperazinyl is [wherein on this piperazine ring, can be substituted with 1 to 3 substituting group, it is selected from by phenyl C1-C6 alkyl (wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 substituting group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed), phenyl is [wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 substituting group, it is selected from by aforesaid phenoxy group (wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 substituting group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed), halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group] and phenyl C2-C6 thiazolinyl as hereinafter described (on this alkenyl part, have the straight or branched thiazolinyl that contains 2 to 6 carbon atoms and have 1 to 3 pair of keys, comprise trans and the cis form) [wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 substituting group, it is selected from by halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group] group formed], 4-(3-(4-trifluoromethyl)-2-propenyl)-(1-for example, 2-or 3-) piperazinyl, 4-(4-p-methoxy-phenyl)-(1-, 2-or 3-) piperazinyl, 4-(3, the 4-3,5-dimethylphenyl)-(1-, 2-or 3-) piperazinyl, 4-(4-fluorophenyl)-(1-, 2-or 3-) piperazinyl, 4-(4-trifluoromethyl)-(1-, 2-or 3-) piperazinyl, 4-(4-aminomethyl phenyl)-(1-, 2-or 3-) piperazinyl, 4-(3, the 4-dichlorophenyl)-(1-, 2-or 3-) piperazinyl, 4-(4-Trifluoromethoxyphen-l)-(1-, 2-or 3-) piperazinyl, 4-(4-(4-chlorophenoxy) phenyl)-(1-, 2-or 3-) piperazinyl etc.

Naphthyl C1-C6 alkyl comprises the naphthyl alkyl, it has the straight or branched alkyl that contains 1 to 6 carbon atom on this moieties, ((1-or 2-) naphthyl) methyl for example, 1-((1-or 2-) naphthyl) ethyl, 2-((1-or 2-) naphthyl) ethyl, 3-((1-or 2-) naphthyl) propyl group, 2-((1-or 2-) naphthyl) propyl group, 4-((1-or 2-) naphthyl) butyl, 5-((1-or 2-) naphthyl) amyl group, 4-((1-or 2-) naphthyl) amyl group, 6-((1-or 2-) naphthyl) hexyl, 2-methyl-3-((1-or 2-) naphthyl) propyl group, 1,1-dimethyl-2-((1-or 2-) naphthyl) ethyl etc.

[wherein on this piperazine ring, can be substituted with at least one group, it is selected from the alkoxy carbonyl by C1-C6 to piperazinyl, furyl C1-C6 alkyl is [wherein on this furan nucleus, (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom can be substituted with at least one phenyl, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed)], pyridyl C1-C6 alkyl is [wherein on this pyridine ring, can be substituted with at least one group, it is selected from by furyl and phenyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, the group that halogen replacement or unsubstituted C1-C6 alkyl and halogen replacement or unsubstituted C1-C6 alkoxyl group are formed) group of forming], (wherein on this thionaphthene ring, can be substituted with at least one group, it is selected from by halogen atom benzothienyl C1-C6 alkyl, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed), phenyl C2-C6 thiazolinyl is (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed), benzofuryl C1-C6 alkyl [wherein on this cumarone ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed], [wherein on this cumarone ring, can be substituted with at least one group, it is selected from by halogen atom benzofuryl C2-C6 thiazolinyl, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed], thiazolyl C1-C6 alkyl is [wherein on this thiazole ring, (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom can be substituted with at least one phenyl, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed)], phenoxy group C1-C6 alkyl is (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed), indyl C1-C6 alkyl (wherein on this indole ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group) and phenyl C1-C6 alkyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by benzofuryl, halogen atom, the group that halogen replacement or unsubstituted C1-C6 alkyl and halogen replacement or unsubstituted C1-C6 alkoxyl group are formed) group of forming] comprise that aforesaid piperazinyl is [wherein on this piperazine ring, (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by benzofuryl can be substituted with at least one phenyl C1-C6 alkyl, halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed)] in addition, also comprise such piperazinyl, it can be on this piperazine ring be replaced by 1 to 3 substituting group, and described substituting group is selected from the C1-C6 alkoxy carbonyl by as hereinafter described, furyl C1-C6 alkyl as hereinafter described (having the straight or branched alkyl that contains 1 to 6 carbon atom on this moieties) is [wherein on this furan nucleus, 1 to 3 phenyl can be substituted with and (wherein on this benzyl ring, 1 to 5 can be substituted with, preferred 1 to 3 substituting group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkyl is formed)], pyridyl C1-C6 alkyl as hereinafter described (having the straight or branched alkyl that contains 1 to 6 carbon atom on this moieties) is [wherein on this pyridine ring, can be substituted with 1 to 3 substituting group, it is selected from by furyl and phenyl (wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 substituting group, it is selected from by halogen atom, the group that halogen replacement or unsubstituted C1-C6 alkyl and halogen replacement or unsubstituted C1-C6 alkoxyl group are formed) group of forming], (wherein on this thionaphthene ring, can be substituted with 1 to 3 substituting group, it is selected from by halogen atom benzothienyl C1-C6 alkyl as hereinafter described (having the straight or branched alkyl that contains 1 to 6 carbon atom on this moieties), halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed), phenyl C2-C6 thiazolinyl as hereinafter described (has the straight or branched thiazolinyl that contains 2 to 6 carbon atoms and have 1 to 3 two key on this alkenyl part, comprise trans and the cis form) (wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 substituting group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed), benzofuryl C1-C6 alkyl as hereinafter described (having the straight or branched alkyl that contains 1 to 6 carbon atom on this moieties) is [wherein on this cumarone ring, can be substituted with 1 to 3 substituting group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed], benzofuryl C2-C6 thiazolinyl as hereinafter described (have the straight or branched thiazolinyl that contains 2 to 6 carbon atoms and have 1 to 3 two key on this alkenyl part, comprise trans and the cis form) is [wherein on this cumarone ring, can be substituted with 1 to 3 substituting group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed], thiazolyl C1-C6 alkyl as hereinafter described (having the straight or branched alkyl that contains 1 to 6 carbon atom on this moieties) [wherein on this thiazole ring, can be substituted with 1 or 2 phenyl (wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 substituting group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed)], phenoxy group C1-C6 alkyl as hereinafter described (having the straight or branched alkyl that contains 1 to 6 carbon atom on this moieties) (wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 substituting group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed), indyl C1-C6 alkyl as hereinafter described (having the straight or branched alkyl that contains 1 to 6 carbon atom on this moieties) is (wherein on this indole ring, can be substituted with 1 to 3 substituting group, it is selected from by halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group) and phenyl C1-C6 alkyl as hereinafter described (wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 substituting group, it is selected from by the cumarone basic ring, halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed), 4-tert-butoxycarbonyl-(1-for example, 2-or 3-) piperazinyl, 4-(4-((2-, 3-, 4-, 5-, 6-or 7-) benzofuryl) benzyl)-(1-, 2-or 3-) piperazinyl, 4-(3-((2-or 3-) furyl) pyridyl) methyl)-(1-, 2-or 3-) piperazinyl, 4-(2-(4-Trifluoromethoxyphen-l) pyridylmethyl)-(1-, 2-or 3-) piperazinyl, 4-(2-(3-chloro-4-fluorophenyl) pyridylmethyl)-(1-, 2-or 3-) piperazinyl, 4-(5-trifluoromethyl (2-, 3-, 4-, 6-or 7-) the cumarone ylmethyl)-(1-, 2-or 3-) piperazinyl, 4-(6-trifluoromethyl-(2-, 3-, 4-, 5-or 7-) the cumarone ylmethyl)-(1-, 2-or 3-) piperazinyl, 4-(5-chlorine (2-, 3-, 4-, 6-or 7-) the thionaphthene ylmethyl)-(1-, 2-or 3-) piperazinyl, 4-(6-chlorine (2-, 3-, 4-, 5-or 7-) the cumarone ylmethyl)-(1-, 2-or 3-) piperazinyl, 4-(5-trifluoromethoxy (2-, 3-, 4-, 6-or 7-) the cumarone ylmethyl)-(1-, 2-or 3-) piperazinyl, 4-(3-(4-trifluoromethyl)-2-propenyl)-(1-, 2-or 3-) piperazinyl, 4-(3-(3, the 4-dichlorophenyl)-2-propenyl)-(1-, 2-or 3-) piperazinyl, 4-(3-(4-chloro-phenyl-)-2-propenyl)-(1-, 2-or 3-) piperazinyl, 4-(3-(6-trifluoromethyl (2-, 3-, 4-, 5-or 7-) benzofuryl)-the 2-propenyl)-(1-, 2-or 3-) piperazinyl, 4-(3-(5-chlorine (2-, 3-, 4-, 5-or 7-) benzofuryl))-the 2-propenyl)-(1-, 2-or 3-) piperazinyl, 4-(5-chlorine (2-, 3-, 4-, 6-or 7-) the cumarone ylmethyl)-(1-, 2-or 3-) piperazinyl, 4-(2-(4-trifluoromethyl)-(4-or 5-) thiazolyl methyl)-(1-, 2-or 3-) piperazinyl, 4-(2-(4-Trifluoromethyl phenyl ether oxygen base) ethyl)-(1-, 2-or 3-) piperazinyl, 4-(3-(4-Trifluoromethoxyphen-l)-2-propenyl)-(1-, 2-or 3-) piperazinyl, 4-(5-trifluoromethoxy (1-, 2-, 3-, 4-, 6-or 7-) the indyl methyl)-(1-, 2-or 3-) piperazinyl, 4-(2-(4-chloro-phenyl-)-(3-, 4-or 5-) furyl methyl)-(1-, 2-or 3-) piperazinyl, 4-(2-(2-chloro-5-trifluoromethyl)-(3-, 4-or 5-) furyl methyl)-(1-, 2-or 3-) piperazinyl etc.

Benzothienyl C1-C6 alkyl is (wherein on this thionaphthene ring, can be substituted with at least one group, it is selected from by halogen atom, the group that halogen replacement or unsubstituted C1-C6 alkoxyl group and halogen replacement or unsubstituted C1-C6 alkyl are formed) comprises benzothienyl C1-C6 alkyl, have on this moieties contain 1 to 6 carbon atom the straight or branched alkyl (wherein on this thionaphthene ring, can be substituted with 1 to 3 substituting group, it is selected from by halogen and replaces or unsubstituted C1-C6 alkoxyl group and halogen replaces or unsubstituted C1-C6 alkyl is formed group), ((2-for example, 3-, 4-, 5-, 6-or 7-) benzothienyl) methyl, 1-((2-, 3-, 4-, 5-, 6-or 7-) benzothienyl) ethyl, 2-((2-, 3-, 4-, 5-, 6-or 7-) benzothienyl) ethyl, 3-((2-, 3-, 4-, 5-, 6-or 7-) benzothienyl) propyl group, 2-((2-, 3-, 4-, 5-, 6-or 7-) benzothienyl) propyl group, 4-((2-, 3-, 4-, 5-, 6-or 7-) benzothienyl) butyl, 5-((2-, 3-, 4-, 5-, 6-or 7-) benzothienyl) amyl group, 4-((2-, 3-, 4-, 5-, 6-or 7-) benzothienyl) amyl group, 6-((2-, 3-, 4-, 5-, 6-or 7-) benzothienyl) hexyl, 2-methyl-3-((2-, 3-, 4-, 5-6-or 7-) benzothienyl) propyl group, 1,1-dimethyl-2-((2-, 3-, 4-, 5-, 6-or 7-) benzothienyl) ethyl, 5-chloro-(2-, 3-, 4-, 6-or 7-) the thionaphthene ylmethyl, 5-methyl-(2-, 3-, 4-, 6-or 7-) the thionaphthene ylmethyl, 5-methoxyl group-(2-, 3-, 4-, 6-or 7-) the thionaphthene ylmethyl, 5-trifluoromethyl-(2-, 3-, 4-, 6-or 7-) the thionaphthene ylmethyl, 5-trifluoromethoxy-(2-, 3-, 4-, 6-or 7-) the thionaphthene ylmethyl, 5,6-two chloro-(2-, 3-, 4-or 7-) thionaphthene ylmethyl, 4,5,6-three fluoro-(2-, 3-or 7-) thionaphthene ylmethyl, 5-chloro-6-trifluoromethoxy-(2-, 3-, 4-or 7-) the thionaphthene ylmethyl, 2,5-dimethyl-(3-, 4-, 6-or 7-) thionaphthene ylmethyl, 2,5,6-trimethylammonium-(3-, 4-, 6-or 7-) thionaphthene ylmethyl etc.

Thiazolyl C1-C6 alkyl is [wherein on this thiazole ring, can be substituted with at least one phenyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, the group that halogen replacement or unsubstituted C1-C6 alkyl and halogen replacement or unsubstituted C1-C6 alkoxyl group are formed)] comprise thiazolyl C1-C6 alkyl, have on this moieties contain 1 to 6 carbon atom the straight or branched alkyl [wherein on this thiazole ring, can be substituted with 1 to 2 aforesaid phenyl (wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 substituting group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed)], ((2-for example, 4-or 5-) thiazolyl) methyl, 1-((2-, 4-or 5-) thiazolyl) ethyl, 2-((2-, 4-or 5-) thiazolyl) ethyl, 3-((2-, 4-or 5-) thiazolyl) propyl group, 2-((2-, 4-or 5-) thiazolyl) propyl group, 4-((2-, 4-or 5-) thiazolyl) butyl, 5-((2-, 4-or 5-) thiazolyl) amyl group, 4-((2-, 4-or 5-) thiazolyl) amyl group, 6-((2-, 4-or 5-) thiazolyl) hexyl, 2-methyl-3-((2-, 4-or 5-) thiazolyl) propyl group, 1,1-dimethyl-2-((2-, 4-or 5-) thiazolyl) ethyl, 2-(4-trifluoromethyl)-(4-or 5-) thiazolyl methyl, 2-(4-trifluoromethyl)-(4-or 5-) thiazolyl methyl, 2-(4-Trifluoromethoxyphen-l)-(4-or 5-) thiazolyl methyl, 4-(3-aminomethyl phenyl)-(2-or 5-) thiazolyl methyl, 5-(2-p-methoxy-phenyl)-(2-or 5-) thiazolyl methyl, 4-(4-chloro-phenyl-)-(2-or 5-) thiazolyl methyl, 2-(2-, the 4-3,5-dimethylphenyl)-(4-or 5-) thiazolyl methyl, 2-(2,4, the 6-trimethylphenyl)-(4-or 5-) thiazolyl methyl, 2-(3, the 4-Dimethoxyphenyl)-(4-or 5-) thiazolyl methyl, 2-(3,4, the 5-trimethoxyphenyl)-(4-or 5-) thiazolyl methyl, 2-(3-chloro-4-trifluoromethyl)-(4-or 5-) thiazolyl methyl, 4-(3, the 4-dichlorophenyl)-(2-or 5-) thiazolyl methyl, 2-(3,4, the 6-trifluorophenyl)-(4-or 5-) thiazolyl methyl, 2,4-phenylbenzene (4-or 5-) thiazolyl methyl etc.

(wherein on this indole ring, can be substituted with at least one group, it is selected from by halogen atom indyl C1-C6 alkyl, the group that halogen replacement or unsubstituted C1-C6 alkyl and halogen replacement or unsubstituted C1-C6 alkoxyl group are formed) comprises indyl C1-C6 alkyl, (wherein on this indole ring, can be substituted with 1 to 3 substituting group, it is selected from by halogen atom having the straight or branched alkyl that contains 1 to 6 carbon atom on this moieties, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed), for example ((1-, 2-, 3-, 4-, 5-, 6-or 7-) indyl) methyl, 1-((1-, 2-, 3-, 4-, 5-, 6-or 7-) indyl) ethyl, 2-((1-, 2-, 3-, 4-, 5-, 6-or 7-) indyl) ethyl, 3-((1-, 2-, 3-, 4-, 5-, 6-or 7-) indyl) propyl group, 2-((1-, 2-, 3-, 4-, 5-, 6-or 7-) indyl) propyl group, 4-((1-, 2-, 3-, 4-, 5-, 6-or 7-) indyl) butyl, 5-((1-, 2-, 3-, 4-, 5-, 6-or 7-) indyl) amyl group, 4-(1-, 2-, 3-, 4-, 5-, 6-or 7-) indyl) amyl group, 6-((1-, 2-, 3-, 4-, 5-, 6-or 7-) indyl) hexyl, 2-methyl-3-((1-, 2-, 3-, 4-, 5-, 6-or 7-) indyl) propyl group, 1,1-dimethyl-2-((1-, 2-, 3-, 4-, 5-, 6-or 7-) indyl) ethyl, 2-trifluoromethyl-(1-, 3-, 4-, 5-, 6-or 7-) the indyl methyl, 5-trifluoromethyl-(1-, 2-, 3-, 4-, 6-or 7-) the indyl methyl, 2-trifluoromethoxy-(1-, 3-, 4-, 5-, 6-or 7-) the indyl methyl, 4-methyl-(1-, 2-, 3-, 5-, 6-or 7-) the indyl methyl, 5-methoxyl group-(1-, 2-, 3-, 4-, 6-or 7-) the indyl methyl, 4-chloro-(1-, 2-, 3-, 5-, 6-or 7-) the indyl methyl, 2,4-dimethyl-(1-, 3-, 5-, 6-or 7-) the indyl methyl, 2,4,6-trimethylammonium-(1-, 3-, 5-or 7-) the indyl methyl, 3,4-dimethoxy-(1-, 2-, 5-, 6-or 7-) the indyl methyl, 3,4,5-trimethoxy-(1-, 2-, 6-or 7-) the indyl methyl, 3-chloro-4-trifluoromethyl-(1-, 2-, 5-, 6-or 7-) the indyl methyl, 3,4-two chloro-(1-, 2-, 5-, 6-or 7-) the indyl methyl, 3,4,6-three fluoro-(1-, 2-, 5-or 7-) indyl methyl, 5-trifluoromethoxy-(1-, 2-, 3-, 4-, 6-or 7-) the indyl methyl, 5-trifluoromethoxy-6-chloro-(1-, 2-, 3-, 4-or 7-) the indyl methyl, 1,3-dimethyl-5-fluoro-(2-, 4-, 6-or 7-) the indyl methyl etc.

Phenyl C1-C6 alkyl is (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by benzofuryl, halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed) comprise that aforesaid phenyl C1-C6 alkyl is (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed) in addition, also comprise such phenyl C1-C6 alkyl, have on this moieties contain 1 to 6 carbon atom the straight or branched alkyl (wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 substituting group, it is selected from by benzofuryl, halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed), 4-((2-for example, 3-, 4-, 5-, 6-or 7-) benzofuryl) benzyl, 2-((2-, 3-, 4-, 5-, 6-or 7-) benzofuryl) benzyl, 3-((2-, 3-, 4-, 5-, 6-or 7-) benzofuryl) benzyl, 3,4-two ((2-, 3-, 4-, 5-, 6-or 7-) benzofuryl) benzyl, 2,4,6-three ((2-, 3-, 4-, 5-, 6-or 7-) benzofuryl) benzyl, 3-chloro-4-((2-, 3-, 4-, 5-, 6-or 7-) benzofuryl) benzyl etc.

Phenyl C1-C6 alkyl is [wherein on this phenyl, can be substituted with at least one phenyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, the group that halogen replacement or unsubstituted C1-C6 alkyl and halogen replacement or unsubstituted C1-C6 alkoxyl group are formed)] comprise phenyl C1-C6 alkyl, have on this moieties contain 1 to 6 carbon atom the straight or branched alkyl [wherein on this benzyl ring, can be substituted with 1 to 3 aforesaid phenyl (wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 substituting group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed)], 4-phenylbenzyl for example, the 3-phenylbenzyl, the 2-phenylbenzyl, 2,4-phenylbenzene benzyl, 2,4,6-triphenyl benzyl, 4-(4-Trifluoromethoxyphen-l) benzyl, 2-(3-trifluoromethyl) benzyl, 4-(2-fluorophenyl) benzyl, 3-(4-chloro-phenyl-) benzyl, 4-(4-p-methoxy-phenyl) benzyl, 3-(4-aminomethyl phenyl) benzyl, 2-(3, the 4-Dimethoxyphenyl) benzyl, 4-(3, the 4-3,5-dimethylphenyl) benzyl, 3-(3,4, the 6-trimethoxyphenyl) benzyl, 2-(2,4, the 5-trimethylphenyl) benzyl, 4-(3, the 4-dichlorophenyl) benzyl, 2-(2,4, the 6-trifluorophenyl) benzyl, 4-(3-chloro-4-Trifluoromethoxyphen-l) benzyl, 2-(4-(2-fluorophenyl) phenyl) ethyl, (2-(3 for 3-, the 4-Dimethoxyphenyl) propyl group phenyl), (2-(2 for 4-, 4, the 5-trimethylphenyl) phenyl) butyl, 5-(4-(3-chloro-4-Trifluoromethoxyphen-l) phenyl) amyl group, 6-(2-(3-trifluoromethyl) phenyl) hexyl, 1-(4-(4-Trifluoromethoxyphen-l) phenyl) ethyl etc.

Phenoxy group is (wherein on this benzyl ring, be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed) be to have 1 to 5, preferred 1 to 3 substituent phenoxy group, described substituting group is selected from by halogen atom as defined above, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed, the example comprises the 2-fluorophenoxy, the 3-fluorophenoxy, the 4-fluorophenoxy, the 2-chlorophenoxy, the 3-chlorophenoxy, the 4-chlorophenoxy, 2-bromine phenoxy group, 3-bromine phenoxy group, 4-bromine phenoxy group, 2-iodine phenoxy group, 3-iodine phenoxy group, 4-iodine phenoxy group, 2,3-two fluorophenoxies, 3,4-two fluorophenoxies, 3,5-two fluorophenoxies, 2,4-two fluorophenoxies, 2,6-two fluorophenoxies, 2, the 3-dichlorophenoxy, 3, the 4-dichlorophenoxy, 3, the 5-dichlorophenoxy, 2, the 4-dichlorophenoxy, 2, the 6-dichlorophenoxy, 3,4,5-trifluoromethoxy phenoxy base, 3,4, the 5-Trichlorophenoxy, 2,4,6-trifluoromethoxy phenoxy base, 2,4, the 6-Trichlorophenoxy, 2-fluoro-4-bromine phenoxy group, 4-chloro-3-fluorophenoxy, 2,3, the 4-Trichlorophenoxy, 3,4,5-trifluoromethoxy phenoxy base, 2,3,4,5,6-penta fluoro benzene oxygen base, 2,4,6-trimethylammonium phenoxy group, 4-normal-butyl phenoxy group, 2, the 4-dimethyl phenoxy, 2, the 3-dimethyl phenoxy, 2, the 6-dimethyl phenoxy, 3, the 5-dimethyl phenoxy, 2, the 5-dimethyl phenoxy, 3,5-two 4-trifluoromethylphenopendants, 4-n-butoxy phenoxy group, 2,4-dimethoxy phenoxy group, 2,3-dimethoxy phenoxy group, 2,6-dimethoxy phenoxy group, 3,5-dimethoxy phenoxy group, 2,5-dimethoxy phenoxy group, 2,4,6-trimethoxy phenoxy group, 3,5-two Trifluoromethyl phenyl ether oxygen bases, 3-chloro-4-methoxyl group phenoxy group, 2-chloro-4-Trifluoromethyl phenyl ether oxygen base, 3-methyl-4-fluorophenoxy, 4-bromo-3-4-trifluoromethylphenopendant, the 2-methylphenoxy, the 3-methylphenoxy, the 4-methylphenoxy, 2-methyl-3-chlorophenoxy, 3-methyl-4-chlorophenoxy, 2-chloro-4-methylphenoxy, 2-methyl-3-fluorophenoxy, the 2-4-trifluoromethylphenopendant, the 3-4-trifluoromethylphenopendant, the 4-4-trifluoromethylphenopendant, 2-pentafluoroethyl group phenoxy group, 3-pentafluoroethyl group phenoxy group, 4-pentafluoroethyl group phenoxy group, 2-sec.-propyl phenoxy group, 3-sec.-propyl phenoxy group, 4-sec.-propyl phenoxy group, 2-tertiary butyl phenoxy group, 3-tertiary butyl phenoxy group, 4-tertiary butyl phenoxy group, 2-sec-butyl phenoxy group, 3-sec-butyl phenoxy group, 4-sec-butyl phenoxy group, 2-is the fluoropropyl phenoxy group just-seven, 3-is the fluoropropyl phenoxy group just-seven, 4-is the fluoropropyl phenoxy group just-seven, 4-n-pentyl phenoxy group, 4-n-hexyl phenoxy group, 2-methoxyl group phenoxy group, 3-methoxyl group phenoxy group, 4-methoxyl group phenoxy group, 3-chloro-2-methoxyl group phenoxy group, 2-fluoro-3-methoxyl group phenoxy group, 2-fluoro-4-methoxyl group phenoxy group, 2,6-dimethoxy phenoxy group, 2,3,4-trifluoromethoxy phenoxy base, 2,4,6-trifluoromethoxy phenoxy base, 2-Trifluoromethyl phenyl ether oxygen base, 3-Trifluoromethyl phenyl ether oxygen base, 4-Trifluoromethyl phenyl ether oxygen base, 3-fluoro-2-Trifluoromethyl phenyl ether oxygen base, 2-fluoro-3-Trifluoromethyl phenyl ether oxygen base, 3-fluoro-4-Trifluoromethyl phenyl ether oxygen base, 3-chloro-2-Trifluoromethyl phenyl ether oxygen base, 2-chloro-3-Trifluoromethyl phenyl ether oxygen base, 3-chloro-4-Trifluoromethyl phenyl ether oxygen base, 2-five fluorine ethoxy phenoxies, 3-five fluorine ethoxy phenoxies, 4-five fluorine ethoxy phenoxies, 3-chloro-2-five fluorine ethoxy phenoxies, 2-chloro-3-five fluorine ethoxy phenoxies, 3-chloro-4-five fluorine ethoxy phenoxies, 2-isopropoxy phenoxy group, 3-isopropoxy phenoxy group, 4-isopropoxy phenoxy group, 2-tert.-butoxy phenoxy group, 3-tert.-butoxy phenoxy group, 4-tert.-butoxy phenoxy group, 2-sec-butoxy phenoxy group, 3-sec-butoxy phenoxy group, 4-sec-butoxy phenoxy group, 2-is fluorine propoxy-phenoxy group just-seven, 3-is fluorine propoxy-phenoxy group just-seven, 4-is fluorine propoxy-phenoxy group just-seven, 4-n-pentyloxy phenoxy group, the positive hexyloxy phenoxy group of 4-etc.

Phenyl C1-C6 alkyl is [wherein on this benzyl ring, be substituted with at least one phenoxy group (wherein on this benzyl ring, be substituted with at least one group, it is selected from by halogen atom, the group that halogen replacement or unsubstituted C1-C6 alkyl and halogen replacement or unsubstituted C1-C6 alkoxyl group are formed)] comprise phenyl C1-C6 alkyl, have on this moieties contain 1 to 6 carbon atom the straight or branched alkyl [wherein on this benzyl ring, be substituted with 1 to 3 aforesaid phenoxy group (wherein on this benzyl ring, be substituted with 1 to 3 substituting group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed)], 4-(4-Trifluoromethoxyphen-l) benzyl for example, 2,4-two (4-Trifluoromethoxyphen-l) benzyl, 2-(3-4-trifluoromethylphenopendant) benzyl, 4-(2-fluorophenoxy) benzyl, 2,4,6-three (2-fluorophenoxy) benzyl, 3-(4-chlorophenoxy) benzyl, 4-(4-methoxyl group phenoxy group) benzyl, 3-(4-methylphenoxy) benzyl, 2-(3,4-dimethoxy phenoxy group) benzyl, 4-(3, the 4-dimethyl phenoxy) benzyl, 3-(3,4,6-trimethoxy phenoxy group) benzyl, 2-(2,4,5-trimethylammonium phenoxy group) benzyl, 4-(3, the 4-dichlorophenoxy) benzyl, 2-(2,4,6-trifluoromethoxy phenoxy base) benzyl, 4-(3-chloro-4-Trifluoromethyl phenyl ether oxygen base) benzyl, 2-(4-(2-fluorophenoxy) phenyl) ethyl, (2-(3 for 3-, 4-dimethoxy phenoxy group) propyl group phenyl), (2-(2 for 4-, 4,5-trimethylammonium phenoxy group) phenyl) butyl, 5-(4-(3-chloro-4-Trifluoromethyl phenyl ether oxygen base) phenyl) amyl group, 6-(2-(3-4-trifluoromethylphenopendant) phenyl) hexyl, 1-(4-(4-Trifluoromethyl phenyl ether oxygen base) phenyl) ethyl etc.

Thiazolyl is (wherein on this thiazole ring, can be substituted with at least one phenyl) comprise that thiazolyl is (wherein on this thiazole ring, can be substituted with 1 or 2 phenyl), (2-for example, 4-or 5-) thiazolyl, 2-phenyl-(4-or 5-) thiazolyl, 4-phenyl-(2-or 5-) thiazolyl, 5-phenyl-(2-or 4-) thiazolyl, 2,5-phenylbenzene-4-thiazolyl, 2,4-phenylbenzene-5-thiazolyl, 4,5-phenylbenzene-2-thiazolyl.

Phenoxy group C1-C6 alkyl is (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by phenyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed), halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed) comprise that (it can be replaced by at least one group aforesaid phenoxy group C1-C6 alkyl, described substituting group is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed) in addition, also comprise such phenoxy group C1-C6 alkyl, its have on this moieties contain 1 to 6 carbon atom the straight or branched alkyl (wherein on this benzyl ring, can be substituted with 1 to 3 substituting group, it is selected from by aforesaid phenyl (wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 substituting group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed), halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed), 4-phenyl phenoxymethyl for example, 3-phenyl phenoxymethyl, 2-phenyl phenoxymethyl, 2,4-phenylbenzene phenoxymethyl, 2,4,6-triphenyl phenoxymethyl, 4-(4-Trifluoromethoxyphen-l) phenoxymethyl, 2-(3-trifluoromethyl) phenoxymethyl, 4-(2-fluorophenyl) phenoxymethyl, 3-(4-chloro-phenyl-) phenoxymethyl, 4-(4-p-methoxy-phenyl) phenoxymethyl, 3-(4-aminomethyl phenyl) phenoxymethyl, 2-(3, the 4-p-methoxy-phenyl) phenoxymethyl, 4-(3, the 4-3,5-dimethylphenyl) phenoxymethyl, 3-(3,4, the 6-trimethoxyphenyl) phenoxymethyl, 2-(2,4, the 5-trimethylphenyl) phenoxymethyl, 4-(3, the 4-dichlorophenyl) phenoxymethyl, 2-(2,4, the 6-trifluorophenyl) phenoxymethyl, 4-(3-chloro-4-Trifluoromethoxyphen-l) phenoxymethyl, 2-(4-phenyl phenoxy group) ethyl, 2-(4-(2-fluorophenyl) phenoxy group) ethyl, (2-(3 for 3-, the 4-Dimethoxyphenyl) propyl group phenoxy group), (2-(2 for 4-, 4, the 5-trimethylphenyl) phenoxy group) butyl, 5-(4-(3-chloro-4-Trifluoromethoxyphen-l) phenoxy group) amyl group, 6-(2-(3-trifluoromethyl) phenoxy group) hexyl, 2-(4-(4-trifluoromethyl) phenoxy group) ethyl, 2-(4-(4-Trifluoromethoxyphen-l) phenoxy group) ethyl etc.

Piperidyl is [wherein on this piperidine ring, can be substituted with at least one group, it is selected from by phenoxy group (on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group) and the group of phenyl C1-C6 alkyl composition] comprise beyond the above-mentioned piperidyl, comprise that also such piperidyl is [wherein on this piperidine ring, can be substituted with at least one phenoxy group (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed)], piperidyl is [wherein on this piperidine ring, can be substituted with 1 to 3 substituting group, it is selected from by aforesaid phenoxy group (wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 substituting group, it is selected from by halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group) and the group of phenyl C1-C6 alkyl composition], 4-benzyl-(1-for example, 2-or 3-) piperidyl, 3-benzyl-(1-, 2-, 4-, 5-or 6-) piperidyl, 2-benzyl-(1-, 3-, 4-, 5-or 6-) piperidyl, 2,4-dibenzyl-(1-, 3-, 5-or 6-) piperidyl, 2,3,4-tribenzyl-(1-, 5-or 6-) piperidyl, 4-phenoxy group-3-benzyl-(1-, 2-, 5-or 6-) piperidyl etc.

Benzofuryl C1-C6 alkyl is (wherein on this cumarone ring, can be substituted with at least one halogen replaces or unsubstituted C1-C6 alkyl) comprise benzofuryl C1-C6 alkyl, it has the straight or branched alkyl (wherein on this cumarone ring, can be substituted with replace or the unsubstituted C1-C6 alkyl of 1 to 3 halogen) that contains 1 to 6 carbon atom, for example ((2-on this moieties, 3-, 4-, 5-, 6-or 7-) benzofuryl) methyl, 1-((2-, 3-, 4-, 5-, 6-or 7-) benzofuryl) ethyl, 2-((2-, 3-, 4-, 5-, 6-or 7-) benzofuryl) ethyl, 3-((2-, 3-, 4-, 5-, 6-or 7-) benzofuryl) propyl group, 2-((2-, 3-, 4-, 5-, 6-or 7-) benzofuryl) propyl group, 4-((2-, 3-, 4-, 5-, 6-or 7-) benzofuryl) butyl, 5-((2-, 3-, 4-, 5-, 6-or 7-) benzofuryl) amyl group, 4-((2-, 3-, 4-, 5-, 6-or 7-) benzofuryl) amyl group, 6-((2-, 3-, 4-, 5-, 6-or 7-) benzofuryl) hexyl, 2-methyl-3-((2-, 3-, 4-, 5-, 6-or 7-) benzofuryl) propyl group, 1,1-dimethyl-2-((2-, 3-, 4-, 5-, 6-or 7-) benzofuryl) ethyl, 2-trifluoromethyl-(3-, 4-, 5-, 6-or 7-) the cumarone ylmethyl, 5-trifluoromethyl-(2-, 3-, 4-, 6-or 7-) the cumarone ylmethyl, 4-methyl-(2-, 3-, 5-, 6-or 7-) the cumarone ylmethyl, 2,4-dimethyl-(3-, 5-, 6-or 7-) the cumarone ylmethyl, 2,4,6-trimethylammonium-(3-, 5-or 7-) cumarone ylmethyl, 4-trifluoromethyl-(2-, 3-, 5-, 6-or 7-) the cumarone ylmethyl, 6-trifluoromethyl-(2-, 3-, 4-, 5-or 7-) the cumarone ylmethyl etc.

Piperidinyl carbonyl C1-C6 alkyl is [wherein on this piperidine ring, can be substituted with at least one phenoxy group (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, the group that halogen replacement or unsubstituted C1-C6 alkyl and halogen replacement or unsubstituted C1-C6 alkoxyl group are formed)] comprise piperidinyl carbonyl C1-C6 alkyl, have on this moieties contain 1 to 6 carbon atom the straight or branched alkyl (wherein on this piperidine ring, be substituted with 1 to 3 aforesaid phenoxy group (wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 substituting group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed), (4-phenoxy group-1-piperidinyl carbonyl) methyl for example, 2-(3-phenoxy group-2-piperidinyl carbonyl) ethyl, 3-(2-phenoxy group-3-piperidinyl carbonyl) propyl group, 4-(1-phenoxy group-4-piperidinyl carbonyl) butyl, 5-(4-phenoxy group-1-piperidinyl carbonyl) amyl group, 6-(1-phenoxy group-2-piperidinyl carbonyl) hexyl, 1-(4-Trifluoromethyl phenyl ether oxygen base)-4-piperidinyl carbonyl methyl, 4-(4-Trifluoromethyl phenyl ether oxygen base)-1-piperidinyl carbonyl methyl, 4-(4-4-trifluoromethylphenopendant)-1-piperidinyl carbonyl methyl, 4-(3-methoxyl group phenoxy group)-1-piperidinyl carbonyl methyl, 1-(2-methylphenoxy)-4-piperidinyl carbonyl methyl, 4-(4-chlorophenoxy)-1-piperidinyl carbonyl methyl, 4-(3,4-two (trifluoromethoxy) phenoxy group)-1-piperidinyl carbonyl methyl, 4-(2,4,6-three (trifluoromethyl) phenoxy group)-1-piperidinyl carbonyl methyl, 4-(3, the 4-dimethyl phenoxy)-1-piperidinyl carbonyl methyl, 4-(2,4,6-trimethoxy phenoxy group)-4-piperidinyl carbonyl methyl, 2-(3, the 4-dichlorophenoxy)-1-piperidinyl carbonyl methyl, 3-(2,4, the 6-tribromophenoxy)-1-piperidinyl carbonyl methyl, (1,2,6-triple phenoxyl-4-piperidinyl carbonyl) methyl, (2,4-hexichol Oxy-1-piperidinyl carbonyl) methyl etc.

_ azoles base C1-C6 alkyl [wherein this _ the azoles ring on, can be substituted with at least one phenyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed)] comprise _ azoles base C1-C6 alkyl, have on this moieties the straight or branched alkyl that contains 1 to 6 carbon atom [wherein this _ the azoles ring on, can be substituted with 1 or 2 aforesaid phenyl (wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 substituting group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed)], ((2-for example, 4-or 5-) _ the azoles base) methyl, 1-((2-, 4-or 5-) _ the azoles base) ethyl, 2-((2-, 4-or 5-) _ the azoles base) ethyl, 3-((2-, 4-or 5-) _ the azoles base) propyl group, 2-((2-, 4-or 5-) _ the azoles base) propyl group, 4-((2-, 4-or 5-) _ the azoles base) butyl, 5-((2-, 4-or 5-) _ the azoles base) amyl group, 4-((2-, 4-or 5-) _ the azoles base) amyl group, 6-((2-, 4-or 5-) _ the azoles base) hexyl, 2-methyl-3-((2-, 4-or 5-) _ the azoles base) propyl group, 1,1-dimethyl-2-((2-, 4-or 5-) _ the azoles base) ethyl, 4-(4-Trifluoromethoxyphen-l)-(2-or 5-) _ azoles ylmethyl, 4-(4-chloro-phenyl-)-(2-or 5-) _ azoles ylmethyl, 4-(4-trifluoromethyl)-(2-or 5-) _ azoles ylmethyl, 4-(4-aminomethyl phenyl)-(2-or 5-) _ azoles ylmethyl, 4-(4-p-methoxy-phenyl)-(2-or 5-) _ azoles ylmethyl, 4-(2, the 4-dichlorophenyl)-(2-or 5-) _ azoles ylmethyl, 4-(2,4, the 6-trifluorophenyl)-(2-or 5-) _ azoles ylmethyl, 2-(3, the 4-3,5-dimethylphenyl)-(4-or 5-) _ azoles ylmethyl, 5-(3,4, the 6-trimethylphenyl)-(2-or 4-) _ azoles ylmethyl, 2-(3, the 4-Dimethoxyphenyl)-(4-or 5-) _ azoles ylmethyl, 4-(2,4, the 6-trimethoxyphenyl)-(2-or 5-) _ azoles ylmethyl, 4-(3-chloro-4-Trifluoromethoxyphen-l)-(2-or 5-) _ azoles ylmethyl, 2,4-phenylbenzene-5-_ azoles ylmethyl, 4,5-phenylbenzene-2-_ azoles ylmethyl, 2,5-phenylbenzene-5-_ azoles ylmethyl etc.

Different _ the azoles base [wherein on this different _ oxazoline ring, can be substituted with at least one phenyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed)] comprise that different _ azoles base is [wherein on this different _ oxazoline ring, can be substituted with 1 or 2 aforesaid phenyl (wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 substituting group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed)], (3-for example, 4-or 5-) different _ the azoles base, 3-phenyl-(4-or 5-) be different _ the azoles base, 4-phenyl-(3-or 5-) be different _ the azoles base, 5-phenyl-(3-or 4-) be different _ the azoles base, 3,4-phenylbenzene-5-is different _ the azoles base, 3,5-phenylbenzene-4-is different _ the azoles base, 4,5-phenylbenzene-3-is different _ the azoles base, 3-(4-trifluorophenyl)-(4-or 5-) be different _ the azoles base, 4-(4-chloro-phenyl-)-(3-or 5-) be different _ the azoles base, 3-(4-trifluoromethyl)-(4-or 5-) be different _ the azoles base, 4-(4-aminomethyl phenyl)-(3-or 5-) be different _ the azoles base, 3-(4-p-methoxy-phenyl)-(4-or 5-) be different _ the azoles base, 4-(2, the 4-dichlorophenyl)-(3-or 5-) different _ azoles base, 3-(2,4, the 6-trifluorophenyl)-(4-or 5-) different _ azoles base, 3-(3, the 4-diphenyl methyl)-(4-or 5-) different _ azoles base, 5-(3,4, the 6-trimethylphenyl)-(3-or 4-) different _ azoles base, 3-(3, the 4-Dimethoxyphenyl)-(4-or 5-) different _ azoles base, 4-(2,4,6-trimethoxyphenyl)-(3-or 5-) different _ azoles base, 3-(3-chloro-4-Trifluoromethoxyphen-l)-(4-or 5-) is different _ the azoles base etc.

Benzo _ azoles base is (wherein on this benzo _ azoles ring, can be substituted with at least one halogen atom) comprise that benzo _ azoles base is (wherein on this benzo _ azoles ring, can be substituted with 1 to 3 halogen atom), for example (2-, 4-, 5-, 6-or 7-) benzo _ azoles base, 5-chloro-(2-, 4-, 6-or 7-) benzo _ azoles base, 6-chloro-(2-, 4-, 5-or 7-) benzo _ azoles base, 5-fluorine (2-, 4-, 6-or 7-) benzo _ azoles base, 6-bromo-(2-, 4-, 5-or 7-) benzo _ azoles base, 5-iodo-(2-, 4-, 6-or 7-) benzo _ azoles base, 5,6-two chloro-(2-, 4-or 7-) benzo _ azoles base, 4,5,6-three fluoro-(2-or 7-) benzo _ azoles base, 5-fluoro-6-chloro-(2-, 4-or 7-) benzo _ azoles base etc.

Benzimidazolyl-is [wherein on this benzoglyoxaline ring, can be substituted with at least one group, it is selected from by halogen atom and phenyl C1-C6 alkyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, the group that halogen replacement or unsubstituted C1-C6 alkyl and halogen replacement or unsubstituted C1-C6 alkoxyl group are formed) group of forming] comprise that benzimidazolyl-is [wherein on this benzoglyoxaline ring, can be substituted with 1 to 3 substituting group, it is selected from by halogen atom and aforesaid phenyl C1-C6 alkyl (wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 substituting group, it is selected from by halogen atom, the group that halogen replacement or unsubstituted C1-C6 alkyl and halogen replacement or unsubstituted C1-C6 alkoxyl group are formed) group of forming], (2-for example, 4-, 5-, 6-or 7-) benzimidazolyl-, 1-(4-trifluoro-methoxybenzyl)-5,6-two chloro-(2-, 4-or 7-) benzimidazolyl-, 5-chloro-(1-, 2-, 4-, 6-or 7-) benzimidazolyl-, 6-chloro-(1-, 2-, 4-, 5-or 7-) benzimidazolyl-, 5-fluoro-(1-, 2-, 4-, 6-or 7-) benzimidazolyl-, 6-bromo-(1-, 2-, 4-, 5-or 7-) benzimidazolyl-, 5-iodo-(1-, 2-, 4-, 6-or 7-) benzimidazolyl-, 5,6-two chloro-(1-, 2-, 4-or 7-) benzimidazolyl-, 4,5,6-three fluoro-(1-, 2-or 7-) benzimidazolyl-, 5-fluoro-6-chloro-(1-, 2-, 4-or 7-) benzimidazolyl-, 1-benzyl-(2-, 4-, 5-, 6-or 7-) benzimidazolyl-, 1-(4-trifluoromethyl benzyl)-(2-, 4-, 5-, 6-or 7-) benzimidazolyl-, 1-(4-benzyl chloride base)-(2-, 4-, 5-, 6-or 7-) benzimidazolyl-, 1-(3-methyl-benzyl)-(2-, 4-, 5-, 6-or 7-) benzimidazolyl-, 1-(2-methoxy-benzyl)-(2-, 4-, 5-, 6-or 7-) benzimidazolyl-, 1-(3, the 4-dimethyl benzyl)-(2-, 4-, 5-, 6-or 7-) benzimidazolyl-, 1-(2,4, the 6-trimethyl benzyl)-(2-, 4-, 5-, 6-or 7-) benzimidazolyl-, 1-(3, the 4-dimethoxy-benzyl)-(2-, 4-, 5-, 6-or 7-) benzimidazolyl-, 1-(2,4,5-trimethoxy benzyl)-(2-, 4-, 5-, 6-or 7-) benzimidazolyl-, 1-(3, the 4-dichloro benzyl)-(2-, 4-, 5-, 6-or 7-) benzimidazolyl-, 1-(2,4, the 6-trifluoro-benzyl)-(2-, 4-, 5-, 6-or 7-) benzimidazolyl-, 1-(3-chloro-4-trifluoromethyl benzyl)-(2-, 4-, 5-, 6-or 7-) benzimidazolyl-, (1,5-benzyl-(2-, 4-, 6-or 7-) benzimidazolyl-, 1,5,6-tribenzyl-(2-, 4-or 7-) benzimidazolyl-etc.

Imidazolyl is [wherein on this imidazole ring, be substituted with at least one phenyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed)] comprise that imidazolyl is [wherein on this imidazole ring, be substituted with 1 or 2 aforesaid phenyl (wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 substituting group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed)], 2-phenyl-(4-or 5-) imidazolyl for example, 4-phenyl-(2-or 5-) imidazolyl, 2,4-phenylbenzene-5-imidazolyl, 2,4-phenylbenzene-5-imidazolyl, 4,5-phenylbenzene-2-imidazolyl, 2-(4-Trifluoromethoxyphen-l)-(4-or 5-) imidazolyl, 2-(4-trifluorophenyl)-(4-or 5-) imidazolyl, 4-(4-chloro-phenyl-)-(2-or 5-) imidazolyl, 4-(4-trifluoromethyl)-(2-or 5-) imidazolyl, 4-(4-aminomethyl phenyl)-2-imidazolyl, 2-(4-p-methoxy-phenyl)-(4-or 5-) imidazolyl, 4-(2, the 4-dichlorophenyl)-(2-or 5-) imidazolyl, 2-(2,4, the 6-trifluorophenyl)-(4-or 5-) imidazolyl, 2-(3, the 4-diphenyl methyl)-(4-or 5-) imidazolyl, 5-(3,4, the 6-trimethylphenyl)-(2-or 4-) imidazolyl, 2-(3, the 4-Dimethoxyphenyl)-(4-or 5-) imidazolyl, 4-(2,4, the 6-trimethoxyphenyl)-(2-or 5-) imidazolyl, 5-(3-chloro-4-Trifluoromethoxyphen-l)-(2-or 4-) imidazolyl etc.

Benzenesulfinyl (phenylsulfinyl) is (wherein on this benzyl ring; can be substituted with at least one group; it is selected from by halogen atom; halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group) be unsubstituted or have 1 to 5; preferred 1 to 3 substituent benzenesulfinyl; described substituting group is selected from by halogen atom as defined above; halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed; the example comprises benzenesulfinyl; 2-fluorobenzene sulfinyl; 3-fluorobenzene sulfinyl; 4-fluorobenzene sulfinyl; 2-chlorobenzene sulfinyl; 3-chlorobenzene sulfinyl; 4-chlorobenzene sulfinyl; 2-bromobenzene sulfinyl; 3-bromobenzene sulfinyl; 4-bromobenzene sulfinyl; 2-iodobenzene sulfinyl; 3-iodobenzene sulfinyl; 4-iodobenzene sulfinyl; 2; 3-difluoro benzenesulfinyl; 3; 4-difluoro benzenesulfinyl; 3; 5-difluoro benzenesulfinyl; 2; 4-difluoro benzenesulfinyl; 2; 6-difluoro benzenesulfinyl; 2; 3-dichlorobenzene sulfinyl; 3; 4-dichlorobenzene sulfinyl; 3; 5-dichlorobenzene sulfinyl; 2; 4-dichlorobenzene sulfinyl; 2; 6-dichlorobenzene sulfinyl; 3; 4; 5-trifluoro-benzene sulfinyl; 3; 4; 5-trichlorobenzene sulfinyl; 2; 4; 6-trifluoro-benzene sulfinyl; 2; 4; 6-trichlorobenzene sulfinyl; 2-fluoro-4-bromobenzene sulfinyl; 4-chloro-3-fluorobenzene sulfinyl; 2; 3; 4-trichlorobenzene sulfinyl; 2; 3; 4; 5; 6-penta fluoro benzene sulfinyl; 2; 4; 6-Three methyl Benzene sulfinyl; 4-n-butylbenzene sulfinyl; 2; 4-dimethyl benzene sulfinyl; 2; 3-dimethyl benzene sulfinyl; 2; 6-dimethyl benzene sulfinyl; 3; 5-dimethyl benzene sulfinyl; 2; 5-dimethyl benzene sulfinyl; 3; 5-two trifluoromethyl benzenesulfinyl; 4-n-butoxy benzenesulfinyl; 2; 4-dimethoxy benzenesulfinyl; 2; 3-dimethoxy benzenesulfinyl; 2; 6-dimethoxy benzenesulfinyl; 3; 5-dimethoxy benzenesulfinyl; 2; 5-dimethoxy benzenesulfinyl; 2; 4; 6-trimethoxy benzenesulfinyl; 3; 5-two trifluoromethoxy benzenesulfinyl; 3-chloro-4-anisole sulfinyl; 2-chloro-4-trifluoromethoxy benzenesulfinyl; 3-methyl-4-fluorobenzene sulfinyl; 4-bromo-3-trifluoromethyl benzenesulfinyl; 2-methylbenzene sulfinyl; 3-methylbenzene sulfinyl; 4-methylbenzene sulfinyl; 2-methyl-3-chlorobenzene sulfinyl; 3-methyl-4-chlorobenzene sulfinyl; 2-chloro-4-methylbenzene sulfinyl; 2-methyl-3-fluorobenzene sulfinyl; 2-trifluoromethyl benzenesulfinyl; 3-trifluoromethyl benzenesulfinyl; 4-trifluoromethyl benzenesulfinyl; 2-pentafluoroethyl group benzenesulfinyl; 3-pentafluoroethyl group benzenesulfinyl; 4-pentafluoroethyl group benzenesulfinyl; 2-isopropyl benzene sulfinyl; 3-isopropyl benzene sulfinyl; 4-isopropyl benzene sulfinyl; 2-tert.-butylbenzene sulfinyl; 3-tert.-butylbenzene sulfinyl; 4-tert.-butylbenzene sulfinyl; 2-sec-butylbenzene sulfinyl; 3-sec-butylbenzene sulfinyl; 4-sec-butylbenzene sulfinyl; 2-is the fluoropropyl benzenesulfinyl just-seven; 3-is the fluoropropyl benzenesulfinyl just-seven; 4-is the fluoropropyl benzenesulfinyl just-seven; 4-n-amylbenzene sulfinyl; 4-positive hexyl phenenyl sulfinyl; 2-anisole sulfinyl; 3-anisole sulfinyl; 4-anisole sulfinyl; 3-chloro-2-anisole sulfinyl; 2-fluoro-3-anisole sulfinyl; 2-fluoro-4-anisole sulfinyl; 2; 3,4-trifluoro-benzene sulfinyl; 2-trifluoromethoxy benzenesulfinyl; 3-trifluoromethoxy benzenesulfinyl; 4-trifluoromethoxy benzenesulfinyl; 3-fluoro-2-trifluoromethoxy benzenesulfinyl; 2-fluoro-3-trifluoromethoxy benzenesulfinyl; 3-fluoro-4-trifluoromethoxy benzenesulfinyl; 3-chloro-2-trifluoromethoxy benzenesulfinyl; 2-chloro-3-trifluoromethoxy benzenesulfinyl; 3-chloro-4-trifluoromethoxy benzenesulfinyl; 2-five fluorine phenetole sulfinyls; 3-five fluorine phenetole sulfinyls; 4-five fluorine phenetole sulfinyls; 3-chloro-2-five fluorine phenetole sulfinyls; 2-chloro-3-five fluorine phenetole sulfinyls; 3-chloro-4-five fluorine phenetole sulfinyls; 2-isopropoxy benzenesulfinyl; 3-isopropoxy benzenesulfinyl; 4-isopropoxy benzenesulfinyl; 2-tert.-butoxy benzenesulfinyl; 3-tert.-butoxy benzenesulfinyl; 4-tert.-butoxy benzenesulfinyl; 2-sec-butoxy benzenesulfinyl; 3-sec-butoxy benzenesulfinyl; 4-sec-butoxy benzenesulfinyl; 2-is fluorine propoxy-benzenesulfinyl just-seven; 3-is fluorine propoxy-benzenesulfinyl just-seven; 4-is fluorine propoxy-benzenesulfinyl just-seven; 4-n-pentyloxy benzenesulfinyl; the positive hexyloxy benzenesulfinyl of 4-etc.

Pyridyl C1-C6 alkyl is [wherein on this pyridyl ring, can be substituted with at least one phenyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed)] comprise beyond the aforesaid pyridyl C1-C6 alkyl, also comprise such pyridyl C1-C6 alkyl, its have on this moieties contain 1 to 6 carbon atom the straight or branched alkyl [wherein on this pyridine ring, can be substituted with 1 to 3 aforesaid phenyl (wherein on this benzyl ring, can be substituted with 1 to 5, preferred 1 to 3 substituting group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed)], 2-(4-Trifluoromethoxyphen-l)-(3-for example, 4-, 5-or 6-) pyridylmethyl, 2-(4-trifluoromethyl)-(3-, 4-, 5-or 6-) pyridylmethyl, 2-(4-p-methoxy-phenyl)-(3-, 4-, 5-or 6-) pyridylmethyl, 2-(4-aminomethyl phenyl)-(3-, 4-, 5-or 6-) pyridylmethyl, 2-(3-chloro-4-fluorophenyl)-(3-, 4-, 5-or 6-) pyridylmethyl, 2-(2, the 4-Dimethoxyphenyl)-(3-, 4-, 5-or 6-) pyridylmethyl, 2-(3,4, the 5-trimethoxyphenyl)-(3-, 4-, 5-or 6-) pyridylmethyl, 2-(2, the 4-3,5-dimethylphenyl)-(3-, 4-, 5-or 6-) pyridylmethyl, 2-(2,4, the 6-trimethylphenyl)-(3-, 4-, 5-or 6-) pyridylmethyl, 2-(2,4, the 6-trichlorophenyl)-(3-, 4-, 5-or 6-) pyridylmethyl, 2-(3-chloro-4-Trifluoromethoxyphen-l)-(3-, 4-, 5-or 6-) pyridylmethyl, 2,4,6-triphenyl-(3-or 5-) pyridylmethyl, 2,5-phenylbenzene-(3-, 4-or 6-) pyridylmethyl etc.

4H-1,3-benzo two _ Ying Ji (wherein at this 4H-1, on 3-benzo two _ English (benzodioxine) ring, can be substituted with at least one halogen atom) comprises 4H-1,3-benzo two _ Ying Ji (wherein at this 4H-1,3-benzo two _ Ying Huanshang can be substituted with 1 to 4 halogen atom), for example (2-, 4-, 5-, 6-, 7-or 8-) 4H-1,3-benzo two _ Ying Ji, 2,2,4,4-tetrafluoro-(5-, 6-, 7-or 8-) 4H-1,3-benzo two _ Ying Ji, 2-chloro-(2-, 4-, 5-, 6-, 7-or 8-) 4H-1,3-benzo two _ Ying Ji, 4-bromo-(2-, 4-, 5-, 6-, 7-or 8-) 4H-1,3-benzo two _ Ying Ji, 2,4-two chloro-(2-, 4-, 5-, 6-, 7-or 8-) 4H-1,3-benzo two _ Ying Ji, 2,4,6-three fluoro-(2-, 4-, 5-, 7-or 8-) 4H-1,3-benzo two _ Ying Ji etc.

Below explain in detail the method for preparing The compounds of this invention.

Reaction process 1

R wherein ¹, R ²Same as described above with n, X ¹Represent halogen atom or nitro.

According to reaction process 1, The compounds of this invention by general formula (1) representative is to produce like this, promptly be with or without basic cpd in the presence of, make by the 4-nitroimidazole compound of general formula (2) representative and the epoxy compounds reaction of representing by general formula (3a), obtain compound, then the gained compound is encircled closed reaction by general formula (4a) representative.

The mol ratio of general formula (2) compound and general formula (3a) compound generally can be between 1: 0.5 and 1: 5, preferably between 1: 0.5 and 1: 3.

Can be extensive use of compound known conduct the basic cpd here.A kind of like this example of basic cpd comprises inorganic alkaline compound, for example metal hydride, metal alcoholate, oxyhydroxide, carbonate or supercarbonate, and organic basic compound, for example acetate.

The specific examples of metal hydride comprises sodium hydride and potassium hydride KH.The specific examples of metal alcoholate comprises sodium methylate, sodium ethylate and potassium tert.-butoxide.The specific examples of oxyhydroxide comprises sodium hydroxide and potassium hydroxide.The specific examples of carbonate comprises yellow soda ash and salt of wormwood.The specific examples of supercarbonate comprises sodium bicarbonate and saleratus.Except above-claimed cpd, in inorganic alkaline compound, also can comprise sodium amide etc.

The specific examples of acetate comprises sodium acetate and potassium acetate.Except these compounds, the specific examples of organic basic compound comprises triethylamine, Trimethylamine 99, diisopropylethylamine, pyridine, xylidine, 1-crassitude, N-methylmorpholine, 1,5-diazabicylo [4.3.0] nonene-5 (DBN), 1,8-diazabicylo [5.4.0] undecylene-7 (DBU) and 1,4-diazabicylo [2.2.2] octane (DABCO).

The mol ratio of above-mentioned basic cpd and general formula (2) compound generally can be between 0.1: 1 and 2: 1, preferably between 0.1: 1 and 1: 1, more preferably between 0.1: 1 and 0.5: 1.

The reaction of general formula (2) compound and general formula (3a) compound is generally carried out in appropriate solvent.

Can be extensive use of common solvent as above-mentioned solvent, need only its not inhibited reaction.A kind of like this example of solvent comprises non-proton property polar solvent, for example dimethyl formamide (DMF), dimethyl sulfoxide (DMSO) (DMSO) or acetonitrile, ketone solvent, for example acetone or methylethylketone, hydrocarbon solvent, for example benzene,toluene,xylene, naphthane or whiteruss, alcoholic solvent, for example methyl alcohol, ethanol, Virahol, propyl carbinol or the trimethyl carbinol, ether solvents, for example tetrahydrofuran (THF) (THF), dioxan, dipropyl ether, diethyl ether or diglyme, ester solvent, for example ethyl acetate or methyl acetate and their mixed solvent.In these solvents, can contain water.

For example following the carrying out of reaction of general formula (2) compound and general formula (3a) compound: general formula (2) compound is dissolved in reaction solvent, when stirring, to adding basic cpd in cooled on ice or up to the mixture under the temperature of room temperature (30 ℃).Then, mixture was stirred 30 minutes to 1 hour down in room temperature to 80 ℃, then to wherein adding general formula (3a) compound.Then, further stir the mixture, temperature is generally room temperature to 100 ℃, and preferred 50 ℃ to 80 ℃, the time was generally 30 minutes to 60 hours, preferred 1 to 50 hour.

Compound (2) as raw material is known.Compound (3a) comprises novel compound, and the method for producing this compound will be explained in the back.

The compounds of this invention by general formula (1) representative is to produce like this, promptly the compound by general formula (4a) representative is encircled closed reaction.The ring closed reaction is performed such, and is about to as above gained and is dissolved in reaction solvent by the compound of general formula (4a) representative, then to wherein adding basic cpd, succeeded by stirring.

Here, as reaction solvent and basic cpd, can use and above-mentioned general formula (2) compound and the used identical reaction solvent of reaction of general formula (3a) compound and identical basic cpd.

The mol ratio of basic cpd and general formula (4a) compound generally equaled 1: 1 or is higher, preferably between 1: 1 and 5: 1, more preferably between 1: 1 and 2: 1.

The temperature of reaction of ring closed reaction is generally 0 ℃ to 150 ℃, preferred room temperature to 120 ℃, more preferably 50 ℃ to 100 ℃.Reaction times was generally 30 minutes to 48 hours, and preferred 1 to 24 hour, more preferably 1 to 12 hour.

Among the present invention, can directly carry out following ring closed reaction, and need not to separate general formula (4a) compound that is generated as general formula (2) compound and general formula (3a) compound reaction result reaction mixture.For example, make general formula (2) compound and general formula (3a) compound, then, add basic cpd, succeeded by stirring down at 50 ℃ to 100 ℃ to the gained reaction mixture in room temperature to 80 ℃ reaction down.Perhaps,, concentrate the gained reaction mixture, resistates is dissolved in high boiling solvent making general formula (2) compound and general formula (3a) compound after room temperature to 80 ℃ following reaction.Then, add basic cpd, succeeded by stirring down, so that generate the allied compound of representing by general formula (1) at 50 ℃ to 100 ℃ to gained solution.

Select as an alternative, in the reaction of general formula (2) compound and general formula (3a) compound, the mol ratio of used basic cpd and compound (2) is between 0.9: 1 and 2: 1.Stir under 100 ℃ at 50 ℃,, generate allied compound by general formula (1) representative so that in single process, carry out the reaction of general formula (2) compound and general formula (3a) compound.

Reaction process 2

X wherein ¹Same as described above, R ^1ARepresent hydrogen atom or C1-C6 alkyl, R ^2ARepresentative is (a) to (y) group as defined above.

According to reaction process 2, The compounds of this invention by general formula (1w) representative is to produce like this, promptly in the presence of basic cpd, make by the compound of general formula (3b) representative and the compound or its salt reaction of representing by general formula (5), so that obtain the compound by general formula (4c) representative, the compound that gained is represented by general formula (4c) encircles closed reaction then.

Compound (3b) is novel, and the method (reaction process 6) of producing this compound will be explained in the back.And then compound (5) comprises novel compound.Back reference example 2 will be described the method example of producing above-claimed cpd.

The mol ratio of general formula (3b) compound and general formula (5) compound generally can be between 1: 0.5 and 1: 5, preferably between 1: 0.5 and 1: 2.

The reaction of general formula (3b) compound and general formula (5) compound is to carry out in the presence of basic cpd, in appropriate solvent.

As basic cpd and reaction solvent, can use and above-mentioned general formula (2) compound and the used identical reaction solvent of reaction of general formula (3a) compound and identical basic cpd.The mol ratio of basic cpd and general formula (3b) compound is generally catalytic amount, preferably between 0.1: 1 and 3: 1, more preferably between 0.1: 1 and 2: 1.

Can use the salt of compound (5) to replace using compound (5) and basic cpd.A kind of like this example of salt comprises an alkali metal salt of compound (5), for example sodium salt or sylvite.

The reaction of general formula (3b) compound and general formula (5) compound is generally carried out under room temperature to 150 ℃, is preferably room temperature to 120 ℃, more preferably room temperature to 80 ℃.Reaction times was generally 10 minutes to 48 hours, and preferred 10 minutes to 24 hours, more preferably 10 minutes to 2 hours.

The compounds of this invention by general formula (1w) representative is to produce like this, promptly the compound by general formula (4c) representative is encircled closed reaction.The ring closed reaction is performed such, and is about to as above gained and is dissolved in reaction solvent by the compound of general formula (4c) representative, then to wherein adding basic cpd, succeeded by stirring under a certain temperature.

Here, as reaction solvent and basic cpd, can use and above-mentioned general formula (3b) compound and the used identical reaction solvent of reaction of general formula (5) compound and identical basic cpd.

The mol ratio of basic cpd and general formula (4c) compound generally equaled 1: 1 or is higher, preferably between 1: 1 and 5: 1, more preferably between 1: 1 and 2: 1.

The temperature of reaction of ring closed reaction is generally 0 ℃ to 150 ℃, preferred room temperature to 120 ℃, more preferably 50 ℃ to 100 ℃.Reaction times was generally 10 minutes to 48 hours, and preferred 10 minutes to 24 hours, more preferably 20 minutes to 4 hours.

Among the present invention, can directly carry out following ring closed reaction to reaction mixture, and need not to separate general formula (4c) compound that is generated as general formula (3b) compound and general formula (5) compound reaction result, and so that generate allied compound, i.e. the The compounds of this invention of representing by general formula (1w).

If the mol ratio of used basic cpd and compound (5) equaled 1: 1 or be higher, and under 100 ℃, react, then can in single process, generate The compounds of this invention, need not separation of intermediates (4c) by general formula (1w) representative at 50 ℃.Under the situation of an alkali metal salt (for example sodium salt or sylvite) that uses compound (5), also be like this.

Reaction process 3

R wherein ^1A, R ^2ASame as described above with n, R ¹⁵Represent C1-C6 alkyl sulphonyl or benzenesulfonyl, it can be replaced by the C1-C6 alkyl on this phenyl ring.

Here, the C1-C6 alkyl sulphonyl is by alkyl with 1 to 6 carbon atom and group that alkylsulfonyl is formed, and the example of C1-C6 alkyl sulphonyl comprises methylsulfonyl, ethylsulfonyl, third alkylsulfonyl, fourth alkylsulfonyl, penta alkylsulfonyl, own alkylsulfonyl etc.

Can comprise the benzenesulfonyl that can on phenyl ring, have 1 to 3 C1-C6 alkyl at the example of the benzenesulfonyl that is replaced by the C1-C6 alkyl on the phenyl ring; for example benzenesulfonyl, neighbour-tosyl group ,-tosyl group, ptoluene-sulfonyl, 2-ethylbenzene alkylsulfonyl, 3-ethylbenzene alkylsulfonyl, 4-ethylbenzene alkylsulfonyl, 2-propyl group-benzenesulfonyl, 3-propylbenzene alkylsulfonyl, 4-propylbenzene alkylsulfonyl, 2; 3-dimethyl-benzenesulfonyl, 2; 4-dimethyl benzene alkylsulfonyl, 2; 4,6-Three methyl Benzene alkylsulfonyl etc.

Compound (6) is in appropriate solvent, carries out in the presence of basic cpd with the reaction of the compound of being represented by general formula (5).

Here can use any known solvent, as long as it does not suppress this reaction.A kind of like this example of solvent comprises water, non-proton property polar solvent, for example DMF, DMSO or acetonitrile, hydrocarbon solvent, for example benzene,toluene,xylene, naphthane, whiteruss or hexanaphthene, alcoholic solvent, for example ethanol, Virahol, propyl carbinol or the trimethyl carbinol, ether solvents, for example THF, dioxan, dipropyl ether, diethyl ether or diglyme, ethyl acetate, acetone and their mixed solvent.

As basic cpd, can use the used identical basic cpd of reaction with above-mentioned general formula (2) compound and general formula (3a) compound.

The mol ratio of basic cpd and compound (6) generally equaled 1: 1 or is higher, preferably between 1: 1 and 5: 1, more preferably between 1: 1 and 2: 1.

Generally can equal 1: 1 or higher by the mol ratio of the compound of general formula (5) representative and compound (6), preferably between 0.9: 1 and 2: 1, more preferably between 0.9: 1 and 1.5: 1.

Temperature of reaction is generally room temperature to 150 ℃, preferred room temperature to 100 ℃, more preferably 60 ℃ to 100 ℃.Reaction times was generally 10 minutes to 24 hours, and preferred 10 minutes to 12 hours, more preferably 20 minutes to 7 hours.

Below, explanation prepares the method for the raw material and the intermediate of The compounds of this invention.

Reaction process 4

R wherein ^1A, R ¹⁵Same as described above with n, R ¹⁶Represent C1-C6 alkoxy-C 1-C6 alkoxyl group or C1-C6 alkanoyloxy, X ²Represent halogen atom.

By the hydrolytic action of general formula (7) compound, generate general formula (8) compound.

The hydrolytic action of compound (7) is carried out under acidic conditions.Hydrolytic action is for example carried out like this, compound (7) is suspended or is dissolved in the appropriate solvent, adds acid to gained solution, succeeded by stirring down at 0 ℃ to 120 ℃.The example of solvent for use can comprise water, alcoholic solvent, for example methyl alcohol, ethanol, Virahol or ethylene glycol, acetonitrile, acetone, toluene, DMF, DMSO, acetate, trifluoroacetic acid and their mixed solvent.The example of used acid can comprise organic acid, for example trifluoroacetic acid or acetate, and mineral acid, for example hydrochloric acid, bromic acid, Hydrogen bromide or sulfuric acid.Organic acid, for example trifluoroacetic acid or acetate also can be used as reaction solvent.Temperature of reaction is generally 0 ℃ to 120 ℃, preferred room temperature to 100 ℃, more preferably room temperature to 80 ℃.Reaction times was generally 30 minutes to 24 hours, and preferred 30 minutes to 12 hours, more preferably 1 to 8 hour.

The hydrolytic action of compound (7) can be carried out under alkaline condition.Hydrolytic action for example is performed such, and compound (7) is suspended or is dissolved in the appropriate solvent, adds alkali to gained solution, succeeded by stirring down at 0 ℃ to 120 ℃.The example of solvent for use can comprise water, alcoholic solvent, for example methyl alcohol, ethanol, Virahol or ethylene glycol and their mixed solvent.The example of used alkali can comprise alkali metal hydroxide, for example sodium hydroxide or potassium hydroxide, alkaline carbonate, for example yellow soda ash or salt of wormwood, and acetate, for example sodium acetate.Temperature of reaction is generally 0 ℃ to 120 ℃, preferred room temperature to 100 ℃, more preferably room temperature to 80 ℃.Reaction times was generally 30 minutes to 24 hours, and preferred 30 minutes to 12 hours, more preferably 1 to 8 hour.

With regard to the reaction of compound (8) and compound (9), the reaction conditions of common sulfonylation that can widespread use alcohol.For example, compound (8) is dissolved in appropriate solvent, in the presence of basic cpd, adds compound (9), succeeded by stirring down, so that can obtain compound (6) at 0 ℃ to 150 ℃ to gained solution.

Here can use any known solvent, as long as it does not suppress sulfonylation.A kind of like this example of solvent comprises halogenated hydrocarbon solvent, for example methylene dichloride or chloroform, non-proton property polar solvent, for example DMF, DMSO or acetonitrile, aromatic hydrocarbon solvent, for example benzene, toluene or dimethylbenzene, hydrocarbon solvent, for example naphthane, whiteruss or hexanaphthene, ether solvents, for example THF, dioxan, dipropyl ether, diethyl ether or diglyme, ethyl acetate, acetone and their mixed solvent.

The mol ratio of compound used therefor (9) and compound (8) generally equaled 1: 1 or is higher, preferably between 1: 1 and 2: 1, more preferably between 1: 1 and 1.1: 1.

The mol ratio of basic cpd and compound (8) generally equaled 1: 1 or is higher, preferably between 1: 1 and 5: 1, more preferably between 1: 1 and 2: 1.

In this sulfonylation, can use 4-Dimethylamino pyridine, 4-(1-pyrrolidyl) pyridine etc. as catalyzer.

Temperature of reaction is generally 0 ℃ to 150 ℃, and preferred 0 ℃ to 100 ℃, more preferably 0 ℃ to 60 ℃.Reaction times was generally 30 minutes to 48 hours, and preferred 1 to 24 hour, more preferably 1 to 4 hour.

Reaction process 5

R wherein ^1A, R ^2A, R ¹⁵, X ¹Same as described above with n.

Reaction from compound (4b) to compound (10) for example be with reacting phase shown in reaction process 4 from compound (8) to compound (6) with reaction conditions under carry out.

Reaction from compound (10) to compound (4c) for example be with reacting phase shown in reaction process 3 from compound (6) to compound (1w) with reaction conditions under carry out.

Reaction process 6

R wherein ^1A, R ¹⁵And X ¹Same as described above.

Reaction from compound (10a) to compound (3b) is appropriate solvent, carries out in the presence of basic cpd.

Here can be extensive use of any solvent, need only its not inhibited reaction.A kind of like this example of solvent can comprise non-proton property polar solvent, for example DMSO or acetonitrile, hydrocarbon solvent, for example benzene,toluene,xylene, naphthane or whiteruss, halogenated hydrocarbon solvent, for example methylene dichloride, chloroform or ethylene dichloride, ether solvents, for example THF, dioxan, dipropyl ether, diethyl ether or diglyme, acetone, ethyl acetate and their mixed solvent.

Here can use and the used identical basic cpd of reaction of the compound of representing by above-mentioned general formula (2) with the compound of representing by above-mentioned general formula (3a).

The mol ratio of a kind of like this basic cpd and compound (10a) generally can equal 1: 1 or be higher, preferably between 1: 1 and 5: 1, more preferably between 1: 1 and 2: 1.

The temperature of reaction of this reaction is generally 0 ℃ to 150 ℃, and preferred 0 ℃ to 100 ℃, more preferably 0 ℃ to 60 ℃.Reaction times was generally 30 minutes to 48 hours, and preferred 1 to 24 hour, more preferably 1 to 4 hour.

Reaction process 7

R wherein ¹, R ²Same as described above with n.

Reaction from compound (11) to compound (3a) for example is performed such, and promptly in appropriate solvent, in the presence of basic cpd, compound (11) is handled with iodate trimethylsulfonium _ (trimethylsulfoxonium iodide).

Here can be extensive use of any solvent, need only its not inhibited reaction.A kind of like this example of solvent can comprise non-proton property polar solvent, for example DMSO or acetonitrile, hydrocarbon solvent, for example benzene,toluene,xylene, naphthane or whiteruss, ether solvents, for example THF, dioxan, dipropyl ether, diethyl ether or diglyme and their mixed solvent.

The example of basic cpd can comprise sodium hydride, sodium amide, metal alcoholate, for example sodium methylate, sodium ethylate or potassium tert.-butoxide.

The mol ratio of a kind of like this basic cpd and compound (11) generally can equal 1: 1 or be higher, preferably between 1: 1 and 3: 1, more preferably between 1: 1 and 1.5: 1.

And iodate trimethylsulfonium _ with the mol ratio of compound (11) generally can equal 1: 1 or be higher, preferably between 1: 1 and 3: 1, more preferably between 1: 1 and 1.5: 1.

The temperature of reaction of this reaction is generally 0 ℃ to 80 ℃, and preferred 10 ℃ to 50 ℃, more preferably 20 ℃ to 35 ℃.Reaction times was generally 1 to 24 hour, and preferred 1 to 12 hour, more preferably 1 to 4 hour.

Reaction from compound (12) to compound (3a) for example is performed such, and promptly in appropriate solvent, compound (12) is used peroxide treatment.

Here can be extensive use of any reaction solvent, need only its not inhibited reaction.A kind of like this example of solvent can comprise water, alcoholic solvent, for example methyl alcohol or ethanol, non-proton property polar solvent, for example DMF, DMSO or acetonitrile, hydrocarbon solvent, for example benzene,toluene,xylene, naphthane, whiteruss or hexanaphthene, halogenated hydrocarbon solvent, for example methylene dichloride, chloroform or ethylene dichloride, ether solvents, for example THF, dioxan, dipropyl ether, diethyl ether or diglyme and their mixed solvent.

The example of superoxide comprises metachloroperbenzoic acid (mCPBA), peroxybenzoic acid, peracetic acid and hydrogen peroxide.

The mol ratio of this class superoxide and compound (12) generally can be between 1: 1 and 2: 1, preferably between 1: 1 and 1.5: 1, more preferably between 1: 1 and 1.3: 1.

The temperature of reaction of this reaction is generally 0 ℃ to 80 ℃, and preferred 0 ℃ to 50 ℃, more preferably 20 ℃ to 35 ℃.Reaction times was generally 10 minutes to 24 hours, and preferred 1 to 12 hour, more preferably 1 to 8 hour.

For example, the following compound (3a) that generates a kind of optically active type from compound (12).

A kind of like this activity of optically active compounds (3a) can generate by the Sharpless epoxidation.That is to say that this compound can generate by the epoxidation with cumene hydroperoxide or tertbutyl peroxide, has Ti (O-iso-C jointly ₃H ₇) ₄With optically active C1-C6 alkyl tartrate, for example diethyl tartrate (D-or L-type) as catalyzer, replace the superoxide in the above-mentioned reaction to use, to obtain compound (3a) from compound (12).

Here can be extensive use of any solvent, need only its not inhibited reaction.A kind of like this example of solvent can comprise non-proton property polar solvent, acetonitrile for example, hydrocarbon solvent, for example benzene,toluene,xylene, naphthane, whiteruss or hexanaphthene, halogenated hydrocarbon solvent, for example methylene dichloride, chloroform or ethylene dichloride, ether solvents, for example THF, dioxan, dipropyl ether, diethyl ether or diglyme and their mixed solvent.

The mol ratio of cumene hydroperoxide or tertbutyl peroxide and compound (6) generally can be between 0.1: 1 and 2: 1, preferably between 0.1: 1 and 1.5: 1, more preferably between 0.1: 1 and 1: 1.

Ti (O-iso-C ₃H ₇) ₄And the mol ratio of compound (12) generally can be between 0.1: 1 and 2: 1, preferably between 0.1: 1 and 1.5: 1, more preferably between 0.1: 1 and 1: 1.

The mol ratio of optically active C1-C6 tartrate (D-or L-type) and compound (12) generally can be between 1: 1 and 2: 1, preferably between 1: 1 and 1.5: 1, more preferably between 1: 1 and 1.3: 1.

The temperature of reaction of this reaction is generally-50 ℃ to 30 ℃, and preferred-20 ℃ to 20 ℃, more preferably-20 ℃ to 5 ℃.Reaction times was generally 1 to 48 hour, and preferred 4 to 24 hours, more preferably 4 to 12 hours.

Reaction process 8

R wherein ^1A, R ^2A, R ¹⁵Same as described above with n.

Reaction from compound (13) to compound (3c) for example be with reacting phase shown in reaction process 3 from compound (6) to compound (1w) with reaction conditions under carry out.

Reaction process 9

(R wherein ^1A, X, n, m, W and o be same as described above.R ^7aRepresent hydrogen atom, hydroxyl, C1-C6 alkoxyl group or phenyl (it can be replaced by halogen atom) on benzyl ring.Dotted line representative on the piperidine ring can be the key of two keys.When dotted line is two key, should on piperidine ring, be substituted with hydroxyl.R ^6aRepresent THP trtrahydropyranyl.R ¹⁷Represent C1-C6 alkyl or phenyl (it can be replaced by at least one group, and described substituting group is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group) on benzyl ring.M represents basic metal, for example sodium, potassium etc.).

Reaction from compound (14) to compound (15) be with or without appropriate solvent in the presence of, in the presence of acid, carry out.

Here can be extensive use of any solvent, as long as it does not influence reaction.A kind of like this example of solvent can comprise water, halohydrocarbon, for example methylene dichloride, chloroform or tetracol phenixin, lower alcohol, for example methyl alcohol, ethanol or Virahol, ketone, for example acetone or methylethylketone, ether, for example dioxan, tetrahydrofuran (THF), methyl glycol or glycol dimethyl ether, aliphatic acid, for example formic acid or acetate and their mixed solvent.

A kind of like this example of acid can comprise for example mineral acid, for example hydrochloric acid, sulfuric acid or Hydrogen bromide, organic acid, for example formic acid, trifluoroacetic acid or acetate, or aromatic sulfonic acid, for example right-the toluenesulphonic acids pyridine _, right-toluenesulphonic acids etc.Although the amount of used a kind of like this acid can suit to be selected from wide in range scope and not have any special restriction, but,, generally can be about 0.1-10 mole, preferably about 0.1-2 mole for per 1 mole of common compounds (14).

Reaction generally suits to carry out under about 0-200 ℃, and preferred room temperature was generally finished in about 0.5-50 hour to about 150 ℃.

The reaction of compound (15) and compound (16) or (17) can be with or without basic cpd in the presence of, preferably do not having in the presence of it, in suitable inert solvent or do not have any solvent and carry out.

Here the example of used basic cpd for example comprises organic bases, triethylamine for example, Trimethylamine 99, pyridine, xylidine, the N-ethyl diisopropylamine, Dimethylamino pyridine, N-methylmorpholine, 1,5-diazabicylo [4.3.0] nonene-5 (DBN), 1,8-diazabicylo [5.4.0] undecylene-7 (DBU) or 1,4-diazabicylo [2.2.2] octane (DABCO), and mineral alkali comprise carbonate, yellow soda ash for example, salt of wormwood, sodium bicarbonate or saleratus, metal hydroxides, for example sodium hydroxide, potassium hydroxide or calcium hydroxide, potassium hydride KH, sodium hydride, potassium, sodium, sodium amide, metal alcoholate, for example sodium methylate or sodium ethylate etc.

The example of solvent for use for example comprises halohydrocarbon, chloroform for example, methylene dichloride, ethylene dichloride or tetracol phenixin, aromatic hydrocarbon, benzene for example, toluene or dimethylbenzene, ether, diethyl ether for example, diisopropyl ether, tetrahydrofuran (THF) or glycol dimethyl ether, ester, for example methyl acetate, ethyl acetate or isopropyl acetate, alcohol, methyl alcohol for example, ethanol, Virahol, propyl alcohol, butanols, 3-methoxyl group-1-butanols, ethyl cellosolve or methylcyclohexane, with non-proton property polar solvent, for example acetonitrile, pyridine, acetone, water, N,N-dimethylacetamide, N, dinethylformamide, dimethyl sulfoxide (DMSO) or HMPA, or their mixed solvent.

The mol ratio of compound (16) or (17) and compound (15) separately generally can be between about 1: 1 and 5: 1, preferably between about 1: 1 and 3: 1.

Reaction generally is carried out under about 0-200 ℃ temperature, preferably about room temperature to 150 ℃, generally needs about 5 minutes to 30 hours.

Can in reactive system, add boron compound, for example boron trifluoride etherate and halo copper compound, for example cupric chloride (I).

In the reaction of compound (15) and compound (17), when adding organic acid, for example trifluoroacetic acid in reactive system, reaction can advantageously be carried out.

Reaction process 10

(R wherein ^1A, X, n, m, W, R ^7a, X ²Same as described above with o.Two W in the general formula (1c) to (1g) can be identical or different.R ^9aRepresent hydrogen atom.)

R ^10aRepresent hydrogen atom; Can have hydroxyl as substituent C1-C6 alkyl; The C1-C6 alkyloyl; The C1-C6 alkoxy carbonyl; Phenyl C1-C6 alkoxy carbonyl (it can be replaced as substituting group by at least one group on benzyl ring, and described substituting group is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group); Phenyl is (wherein on this benzyl ring; can be substituted with at least one group; it is selected from by halogen atom; halogen replaces or unsubstituted C1-C6 alkyl; halogen replaces or unsubstituted C1-C6 alkoxyl group; can have be selected from C1-C6 alkyloyl and C1-C6 alkyl group as substituent amino; the C1-C6 alkoxy carbonyl; phenyl; phenoxy group is (wherein on this benzyl ring; can be substituted with at least one group; it is selected from by halogen atom; halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed); amino-sulfonyl; 1; 2; 3; the 4-tetrahydric quinoline group (it can this 1; 2; 3; replaced as substituting group by at least one oxo base on the 4-tetrahydroquinoline ring); the C1-C6 alkyl sulphonyl; the C3-C8 cycloalkyl; nitro; cyano group; the C1-C6 alkylthio; (it can be replaced by at least one group on this benzyl ring phenyl sulfonyl, and described substituting group is selected from by halogen atom; halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed); the C1-C6 alkyl and the following groups of hydroxyl-replacement:

(W wherein ₁Represent the C1-C6 alkylidene group.R ¹¹And R ¹²Represent the C1-C6 alkoxyl group, they can be identical or different) group of composition); Phenyl C1-C6 alkyl is (wherein on this benzyl ring, can be substituted with at least one group as substituting group, it is selected from by C1-C4 alkylene dioxo base, phenyl (it can be replaced by at least one group on this benzyl ring, and described substituting group is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group), group-N (R ^11A) R ^12A(R ^11AAnd R ^12ARepresent hydrogen atom, C1-C6 alkyl or phenyl, they can be identical or different, R ^11AAnd R ^12ACan pass through nitrogen-atoms, Sauerstoffatom or sulphur atom or do not combine with one another by them, constitute 5-to 7-unit saturated heterocyclic with adjacent nitrogen-atoms), (it can be replaced by at least one group on this benzyl ring phenoxy group, and described substituting group is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed), phenyl C1-C6 alkoxyl group, can be had the C1-C6 alkyl as the substituent amino C1-C6 alkoxyl group that replaces, halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C10 alkoxyl group is formed); Benzofuryl C1-C6 alkyl (it can be replaced by at least one group on this cumarone ring, and described substituting group is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group); Phenyl sulfonyl (it can be replaced by at least one group on this benzyl ring, and described substituting group is selected from the group of being made up of halogen atom, halogen replacement or unsubstituted C1-C6 alkyl, halogen replacement or unsubstituted C1-C6 alkoxyl group and C1-C4 alkylene dioxo base); Phenoxy group dicarbapentaborane (it can be on this benzyl ring be replaced as substituting group by at least one group, and described substituting group is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group); Phenyl C2-C6 thiazolinyl (it can be replaced by at least one group on this benzyl ring, and described substituting group is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group); The C1-C6 alkyl of C1-C6 alkoxyl group-replacement; The C2-C6 thiazolinyl; The C2-C6 alkyloyl of C1-C6 alkoxyl group-replacement; The C1-C6 alkyl of C3-C8 cycloalkyl-replacement; Phenoxy group C1-C6 alkyl (it can be replaced by at least one group on this benzyl ring, and described substituting group is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group); Benzoyl (it can be replaced by at least one group on this benzyl ring, and described substituting group is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group); Phenylamino formyl radical (it can be replaced by at least one group on this benzyl ring, and described substituting group is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group); Pyridyl; Pyridyl C1-C6 alkyl; Imidazolyl C1-C6 alkyl; 1,2,3, the 4-tetrahydric quinoline group (it can this 1,2,3, replaced as substituting group by at least one group on the 4-tetrahydroquinoline ring, described substituting group is selected from the group of being made up of oxo base and C1-C6 alkyl); Quinolyl; Indyl; Can have the C1-C6 alkyl as substituent amino; Indazolyl; Naphthyl; The C3-C8 cycloalkyl; Can have the C1-C6 alkyl of C1-C6 alkyl as substituent amino-replacement; The C1-C6 alkyl of cyano group-replacement; Furyl C1-C6 alkyl; Following groups:

(wherein RR represents phenyl (it can be replaced as substituting group by at least one group, and described substituting group is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group) on this benzyl ring); Or the C1-C6 alkyl of piperazinyl-replacement (it can on this piperazine ring by at least one phenyl (it can be replaced by at least one group on this benzyl ring, and described substituting group is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group) as the substituting group replacement).

R ^9bRepresent hydrogen atom; Can have hydroxyl as substituent C1-C6 alkyl; (it can be replaced as substituting group by at least one group on this benzyl ring phenyl, described substituting group is selected from by C1-C4 alkylene dioxo base, phenyl (it can be replaced by at least one group on this benzyl ring, and described substituting group is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group), group-N (R ^11A) R ^12A(R ^11AAnd R ^12ARepresent hydrogen atom, C1-C6 alkyl or phenyl, they can be identical or different, R ^11AAnd R ^12ACan pass through nitrogen-atoms, Sauerstoffatom or sulphur atom or do not combine with one another by them, constitute 5-to 7-unit saturated heterocyclic with adjacent nitrogen-atoms), (it can be replaced by at least one group on this benzyl ring phenoxy group, and described substituting group is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed), phenyl C1-C6 alkoxyl group, can be had the C1-C6 alkyl as the substituent amino C1-C6 alkoxyl group that replaces, halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C10 alkoxyl group is formed); (it can be replaced as substituting group by at least one group on this benzyl ring phenyl C1-C6 alkyl, described substituting group is selected from by C1-C4 alkylene dioxo base, phenyl (it can be replaced by at least one group on this benzyl ring, and described substituting group is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group), group-N (R ^11A) R ^12A(R ^11AAnd R ^12ARepresent hydrogen atom, C1-C6 alkyl or phenyl, they can be identical or different, R ^11AAnd R ^12ACan pass through nitrogen-atoms, Sauerstoffatom or sulphur atom or do not combine with one another by them, constitute 5-to 7-unit saturated heterocyclic with adjacent nitrogen-atoms), (it can be replaced by at least one group on this benzyl ring phenoxy group, and described substituting group is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed), phenyl C1-C6 alkoxyl group, can have the C1-C6 alkyl as the substituent C1-C6 alkoxyl group that is replaced by amino, halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C10 alkoxyl group is formed); Benzofuryl (it can be replaced by at least one group on this cumarone ring, and described substituting group is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group); Benzofuryl C1-C6 alkyl (it can be replaced by at least one group on this cumarone ring, and described substituting group is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group); The C1-C6 alkyl of C1-C6 alkoxyl group-replacement; The C1-C6 alkyl of C3-C8 cycloalkyl-replacement; The C3-C8 cycloalkyl; Phenoxy group C1-C6 alkyl (it can be replaced by at least one group on this benzyl ring, and described substituting group is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group); Pyridyl; Pyridyl C1-C6 alkyl; Imidazolyl; Imidazolyl C1-C6 alkyl; Can have the C1-C6 alkyl as the substituent quilt C1-C6 alkyl of amino-replacement; The C1-C6 alkyl of cyano group-replacement; The C1-C6 alkyl of furyl-replacement; Furyl; Piperazinyl (it can on this piperazine ring by at least one phenyl (it can be replaced by at least one group on this benzyl ring, and described substituting group is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group) as the substituting group replacement); Or the C1-C6 alkyl of piperazinyl-replacement (it can on this piperazine ring by at least one phenyl (it can be replaced by at least one group on this benzyl ring, and described substituting group is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group) as the substituting group replacement).

R ^9cRepresentative can have hydroxyl as substituent C1-C6 alkyl; The C1-C6 alkoxy carbonyl; Phenyl C1-C6 alkoxy carbonyl (it can be replaced as substituting group by at least one group on benzyl ring, and described substituting group is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group); Phenyl is (wherein on this benzyl ring; can be substituted with at least one group; it is selected from by halogen atom; halogen replaces or unsubstituted C1-C6 alkyl; halogen replaces or unsubstituted C1-C6 alkoxyl group; can have be selected from C1-C6 alkyloyl and C1-C6 alkyl group as substituent amino; the C1-C6 alkoxy carbonyl; phenyl; phenoxy group is (wherein on this benzyl ring; can be substituted with at least one group as substituting group; it is selected from by halogen atom; halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed); amino-sulfonyl; 1; 2; 3; the 4-tetrahydric quinoline group (it can this 1; 2; 3; replaced as substituting group by at least one oxo base on the 4-tetrahydroquinoline ring); the C1-C6 alkyl sulphonyl; the C3-C8 cycloalkyl; nitro; cyano group; the C1-C6 alkylthio; (it can be replaced as substituting group by at least one group on this benzyl ring phenyl sulfonyl, and described substituting group is selected from by halogen atom; halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed); the C1-C6 alkyl and the following groups of hydroxyl-replacement:

(W wherein ₁Represent the C1-C6 alkylidene group, R ¹¹And R ¹²Represent the C1-C6 alkoxyl group, they can be identical or different) group of composition); Phenyl C1-C6 alkyl is (wherein on this benzyl ring, can be substituted with at least one group as substituting group, it is selected from by C1-C4 alkylene dioxo base, phenyl (it can be replaced by at least one group on this benzyl ring, and described substituting group is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group), group-N (R ^11A) R ^12A(R ^11AAnd R ^12ARepresent hydrogen atom, C1-C6 alkyl or phenyl, they can be identical or different, R ^11AAnd R ^12ACan pass through nitrogen-atoms, Sauerstoffatom or sulphur atom or do not combine with one another by them, constitute 5-to 7-unit saturated heterocyclic with adjacent nitrogen-atoms), (it can be replaced by at least one group on this benzyl ring phenoxy group, and described substituting group is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed), phenyl C1-C6 alkoxyl group, can have the C1-C6 alkyl as the substituent C1-C6 alkoxyl group that is replaced by amino, halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C10 alkoxyl group is formed); Benzofuryl C1-C6 alkyl (it can be replaced by at least one group on this cumarone ring, and described substituting group is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group); Phenyl sulfonyl (it can be replaced by at least one group on this benzyl ring, and described substituting group is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl, halogen replaces or unsubstituted C1-C6 alkoxyl group and halogen replaces or unsubstituted C1-C4 alkylene dioxo base is formed group); Phenyl C2-C6 thiazolinyl (it can be replaced by at least one group on this benzyl ring, and described substituting group is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group); The C1-C6 alkyl of C1-C6 alkoxyl group-replacement; The C2-C6 thiazolinyl; The C1-C6 alkyl of C3-C8 cycloalkyl-replacement; Phenoxy group C1-C6 alkyl (it can be replaced by at least one group on this benzyl ring, and described substituting group is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group); Pyridyl; Pyridyl C1-C6 alkyl; Imidazolyl C1-C6 alkyl; 1,2,3, the 4-tetrahydric quinoline group (it can this 1,2,3, replaced as substituting group by at least one group on the 4-tetrahydroquinoline ring, described substituting group is selected from the group of being made up of oxo base and C1-C6 alkyl); Quinolyl; Indyl; Indazolyl; Naphthyl; The C3-C8 cycloalkyl; Can have the C1-C6 alkyl as the substituent quilt C1-C6 alkyl of amino-replacement; The C1-C6 alkyl of cyano group-replacement; The C1-C6 alkyl of furyl-replacement; Following groups:

R ^9dRepresent the C1-C6 alkyloyl; Phenoxy group dicarbapentaborane (it can be replaced by at least one group on this phenyl, and described substituting group is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group); The C2-C6 alkyloyl of C1-C6 alkoxyl group-replacement or benzoyl (it can be replaced by at least one group on this benzyl ring, and described substituting group is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group).

R ^9eRepresent phenyl (it can be replaced by at least one group, and described substituting group is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group) on this phenyl.

R ¹⁸Represent hydrogen atom or C1-C6 alkyl.

Dotted line representative on the piperidine ring can be the key of two keys.When dotted line is two key, should be substituted with the oNR of group-(W) ^9aR ^10a, the oN (CHR of group-(W) ¹⁸R ^9b) R ^10a, the oNR of group-(W) ^9cR ^10a, the oNR of group-(W) ^9dR ^10aOr the oN (CONHR of group-(W) ^9e) R ^10a

In general formula (1d), constitute group-N (R ^10a) CHR ¹⁸R ^9bCHR ¹⁸R ^9bTotal carbon number should be no more than 6.

The reaction of compound (1c) and compound (16) is in the presence of reductive agent, need not solvent or carry out in appropriate solvent.

Compound (16) generally can be at least 1: 1 with the mol ratio of compound (1c), and preferred 1: 1 to greatly excessive.

The example of reaction solvent for use can comprise water, lower alcohol, for example methyl alcohol, ethanol, Virahol, butanols, the trimethyl carbinol or ethylene glycol, acetonitrile, aliphatic acid, for example formic acid, acetate or trifluoroacetic acid, ether, for example diethyl ether, tetrahydrofuran (THF), dioxan, diethylene glycol monomethyl ether (monoglyme) or diglyme, aromatic hydrocarbon, for example benzene, toluene or dimethylbenzene, halohydrocarbon, for example methylene dichloride, ethylene dichloride, chloroform, tetracol phenixin, or their mixed solvent etc.

The example of reductive agent can comprise formic acid, alkali metal formate, sodium formiate for example, reductive agent, for example sodium borohydride, sodium cyanoborohydride, sodium triacetoxy borohydride, lithium aluminum hydride or its mix reductive agent, catalytic hydrogen-reductive agent, for example palladium-Hei, palladium-carbon, platinum oxide, platinum-Hei or Raney nickel etc.

When using formic acid and alkali metal formate as reductive agent, temperature of reaction generally suitably is about room temperature to 200 ℃, preferably about about 50-150 ℃, is reflected in about 10 minutes to 10 hours and finishes.The mol ratio of formic acid and compound (1c) can be greatly excessive.

When using reductive agent, temperature of reaction is general suitable be-80-100 ℃, preferably-80-70 ℃, be reflected in about 30 minutes to 100 hours and finish.The mol ratio of reductive agent and compound (1c) generally can be between about 1: 1 and 20: 1, preferably between about 1: 1 and 6: 1.Definite, when using lithium aluminum hydride, preferably use ether, for example diethyl ether, tetrahydrofuran (THF), dioxan, diethylene glycol monomethyl ether or diglyme, and aromatic hydrocarbon, for example benzene, toluene or dimethylbenzene as reductive agent.Can in reactive system, add amine, for example Trimethylamine 99, triethylamine or N-ethyl diisopropylamine, and molecular sieve, for example molecular sieve 3a (MS-3A), molecular sieve 4A (MS-4A) etc.

And then, when using catalytic hydrogen-reductive agent, reaction generally can be carried out to the nitrogen atmosphere of 20atm at about normal pressure, preferred about normal pressure is to 10atm, perhaps in the presence of (for example formic acid, ammonium formiate, tetrahydrobenzene or the hydrazine hydrate) of hydrogen-provide agent, carry out, temperature is generally pact-30-100 ℃, and preferably about 0-60 ℃, reaction was generally finished in about 1-12 hour.The consumption of catalytic hydrogen-reductive agent generally can be about 0.1-40wt% (based on compound (1c)), preferably about 1-20wt%.

The reaction of compound (1c) and compound (17) generally be in appropriate solvent, be with or without basic cpd in the presence of carry out.

The example of inert solvent can comprise aromatic hydrocarbon, for example benzene, toluene or dimethylbenzene, ether, diethyl ether for example, tetrahydrofuran (THF), dioxan, diethylene glycol monomethyl ether or diglyme, halohydrocarbon, for example methylene dichloride, ethylene dichloride, chloroform or tetracol phenixin, lower alcohol, methyl alcohol for example, ethanol, Virahol, butanols, the trimethyl carbinol or ethylene glycol, aliphatic acid, acetate for example, ester, for example ethyl acetate or methyl acetate, ketone, for example acetone or methylethylketone, acetonitrile, pyridine, dimethyl sulfoxide (DMSO), N, dinethylformamide, HMPA, or their mixed solvent.

The example of basic cpd can comprise carbonate, yellow soda ash for example, salt of wormwood, sodium bicarbonate, saleratus or cesium carbonate, metal hydroxides, sodium hydroxide for example, potassium hydroxide or calcium hydroxide, sodium hydride, potassium hydride KH, potassium, sodium, sodium amide, metal alcoholate, for example sodium methylate, sodium ethylate or propyl carbinol sodium, organic bases, pyridine for example, imidazoles, the N-ethyl diisopropylamine, Dimethylamino pyridine, triethylamine, Trimethylamine 99, xylidine, N-methylmorpholine, 1,5-diazabicylo [4.3.0] nonene-5 (DBN), 1,8-diazabicylo [5.4.0] undecylene-7 (DBU) or 1,4-diazabicylo [2.2.2] octane (DABCO), perhaps their mixture.

The mol ratio of used basic cpd and compound (1c) can be at least 1: 1, preferably between 1: 1 and 10: 1.

Compound used therefor (17) can be at least 1: 1 with the mol ratio of compound (1c), preferably between 1: 1 and 10: 1.

Reaction is generally carried out under 0-200 ℃, preferably about 0-150 ℃, generally finishes in about 5 minutes to 80 hours.

Can add alkali metal halide in reactive system, for example sodium iodide or potassiumiodide perhaps add phase-transfer catalyst.

Here, the example of phase-transfer catalyst can comprise catalyzer, tetrabutylammonium chloride for example, Tetrabutyl amonium bromide, tetrabutyl ammonium fluoride, tetrabutylammonium iodide, TBAH, tetrabutyl ammonium bisulfite, tributyl-methyl phosphonium ammonium chloride, the tributyl benzyl ammonium chloride, four pentyl ammonium chloride, the four pentyl brometo de amonio, four hexyl ammonium chlorides, benzyl dimethyl octyl group ammonium chloride, methyl three hexyl ammonium chlorides, benzyl dimethyl octadecyl ammonium chloride, methyl tridecyl ammonium chloride, benzyl tripropyl ammonium chloride, benzyltriethylammoinium chloride, the phenyl triethyl ammonium chloride, etamon chloride or tetramethyl ammonium chloride, be selected from down the quaternary ammonium salt of the group replacement of group: C1-C18 straight or branched alkyl, phenyl C1-C6 alkyl and phenyl, by (_) salt of C1-C18 straight or branched alkyl replacement, for example tetrabutyl chlorination (_), perhaps pyridine _ the salt that is replaced by C1-C18 straight or branched alkyl, for example 1-dodecyl chlorination pyridine _.

The mol ratio of used phase-transfer catalyst and compound (1c) generally can be between 0.1: 1 and 1: 1, preferably between 0.1: 1 and 0.5: 1.

Compound (1c) is undertaken by a kind of like this method with the reaction of compound (18), wherein utilizes common acid amides-coupling formation reaction to make the carboxylic acid reaction of compound (1c) and compound (18).

Here condition that can the known amido linkage formation reaction of widespread use.A kind of like this example of amido linkage formation reaction comprises (a) mixed anhydride method, just make carboxylic acid (18) and the reaction of halo alkyl formate obtain mixed acid anhydride and the method that makes the reaction of this mixed acid anhydride and amine (1c), (b) active ester method, just transform carboxylic acid (18) and be active ester, for example right-the nitrophenyl ester, N-hydroxy-succinamide ester or I-hydroxybenzotriazole ester, perhaps active amide, benzo _ azoles quinoline-2-thioketones for example, the method that itself and amine (1c) are reacted, (c) carbodlimide method, just in activator (dicyclohexylcarbodiimide for example, 1-(3-dimethylamino-propyl)-3-ethyl carbodiimide (WSC) or carbonyl dimidazoles) under the existence, carry out the method for the condensation reaction of carboxylic acid (18) and amine (1c), (d) additive method, comprise that using dewatering agent (for example diacetyl oxide) to transform carboxylic acid (18) is carboxylic acid anhydride and the method that makes the reaction of this carboxylic acid anhydride and amine (1c), make ester and the method that amine (1c) reacts and the carboxylic acid halides that makes carboxylic acid (18) of carboxylic acid (18) and lower alcohol under high pressure and high temperature, it is the method for carboxylic acid halides and amine (1c) reaction.

The mixed acid anhydride that is used in (a) mixed anhydride method as mentioned above is to obtain by common Schotten-Baumann reaction.Make mixed acid anhydride and amine (1c) reaction, generally need not to separate, so that generate the The compounds of this invention of representing by general formula (1f).

Above-mentioned Schotten-Baumann reaction is what to carry out in the presence of basic cpd.

Here can use the compound that is usually used in the Schotten-Baumann reaction as basic cpd.A kind of like this example of basic cpd comprises: organic bases, for example triethylamine, Trimethylamine 99, pyridine, xylidine, N-ethyl diisopropylamine, Dimethylamino pyridine, N-methylmorpholine, 1,5-diazabicylo [4.3.0] nonene-5 (DBN), 1,8-diazabicylo [5.4.0] undecylene-7 (DBU) or 1,4-diazabicylo [2.2.2] octane (DABCO); Mineral alkali comprises carbonate, for example yellow soda ash, salt of wormwood, sodium bicarbonate or saleratus, metal hydroxides, for example sodium hydroxide, potassium hydroxide or calcium hydroxide, potassium hydride KH, sodium hydride, potassium, sodium, sodium amide, and metal alcoholate, for example sodium methylate or sodium ethylate.

Reaction is generally carried out preferred 0 ℃ to 50 ℃ under-20 ℃ to 100 ℃.Reaction times was generally 5 minutes to 10 hours, preferred 5 minutes to 2 hours.

The reaction of gained mixed acid anhydride and amine (1c) is generally carried out under-20 ℃ to 150 ℃, preferred 10 ℃ to 50 ℃.Reaction times was generally 5 minutes to 10 hours, preferred 5 minutes to 5 hours.Mixed anhydride method is generally carried out in solvent.

Here can use any solvent that is usually used in mixed anhydride method.A kind of like this example of solvent comprises halohydrocarbon, for example chloroform, methylene dichloride, ethylene dichloride or tetracol phenixin, aromatic hydrocarbon, for example benzene, toluene or dimethylbenzene, ether, for example diethyl ether, diisopropyl ether, tetrahydrofuran (THF) or glycol dimethyl ether, ester, for example methyl acetate, ethyl acetate or isopropyl acetate, non-proton property polar solvent, for example N,N-dimethylacetamide, N, dinethylformamide, dimethyl sulfoxide (DMSO) or HMPA and their mixed solvent.

The example that is used for the halo alkyl formate of mixed anhydride method comprises methyl-chloroformate, bromine methyl-formiate, Vinyl chloroformate, bromine ethyl formate and isobutyl chlorocarbonate.The mol ratio of carboxylic acid (18), halo alkyl formate and amine (1c) generally can equal 1: 1.The mol ratio of used each halo alkyl formate and carboxylic acid (18) and amine (1c) also can be between 1: 1 and 1.5: 1.

The above-mentioned method (c) that is involved in the condensation reaction under existing of above-mentioned activator be in appropriate solvent, be with or without basic cpd in the presence of carry out.

As used here solvent and basic cpd, can use as above in (d) additive method described in the reaction of carboxylic acid halides and amine (1c) used any solvent.

The mol ratio of activator and compound (1c) can equal 1: 1 at least, preferably between 1: 1 and 5: 1.When using WSC, if add I-hydroxybenzotriazole to reactive system then react advantageously and carry out as activator.

Reaction is generally carried out preferred 0 ℃ to 150 ℃ under-20 ℃ to 180 ℃.Reaction times was generally 5 minutes to 90 hours.

When taking to make the method for carboxylic acid halides and amine (1c) reaction from above-mentioned (d) additive method, reaction is to carry out in the presence of basic cpd, in appropriate solvent.

Here can be extensive use of known basic cpd.For example, can use any basic cpd that in above-mentioned Schotten-Baumann reaction, uses.

The example of solvent for use can comprise alcohol, for example methyl alcohol, ethanol, Virahol, propyl alcohol, butanols, 3-methoxyl group-1-butanols, ethyl cellosolve or methylcyclohexane, acetonitrile, pyridine, acetone, water, and the solvent that is used for above-mentioned mixed anhydride method.

Amine (1c) is not particularly limited with the mol ratio of carboxylic acid halides, but can suitably be selected from wide in range scope.The mol ratio of these compounds generally can equal 1: 1 at least, preferably between 1: 1 and 1: 5.

Reaction is generally carried out preferred 0 ℃ to 150 ℃ under-20 ℃ to 180 ℃.Reaction times was generally 5 minutes to 50 hours.

Above-mentioned amido linkage formation reaction also can be carried out like this, even carboxylic acid (18) reacts in the presence of the phosphorus condensing agent with amine (1c), for example diphenyl phosphinyl chloride, phenyl-N-phenyl phosphamide muriate, diethyl chloro-phosphate, diethyl phosphorocyanidate, diphenyl phosphate trinitride or two (2-oxo-3-_ oxazolidinyl) inferior phosphonyl chloride.

This reaction is to carry out in the presence of solvent that is used for the above-mentioned method that makes the reaction of carboxylic acid halides and amine (1c) and basic cpd, and temperature is generally-20 ℃ to 150 ℃, preferred 0 ℃ to 100 ℃.Reaction times was generally 5 minutes to 30 hours.The mol ratio of each and amine (1c) equals 1: 1 at least in used condensing agent and the carboxylic acid (18), preferably between 1: 1 and 2: 1.

The reaction of compound (1c) and compound (19) can with by the reacting phase of the compound (15) of above-mentioned reaction process 9 representatives and compound (16) or (17) with condition under carry out.

Reaction process 11

(R wherein ^1A, X, n, m, W, R ^7a, R ⁹, R ¹⁰Same as described above with o.R ^6bRepresent the C1-C6 alkoxy carbonyl.Dotted line representative on the piperidine ring can be the key of two keys.When dotted line is two key, should be substituted with radicals R ^6b, COOH or-CONR ⁹R ¹⁰)

By hydrolysis compound (20), generate compound (21).

Hydrolysis reaction is in appropriate solvent or need not solvent, carries out in the presence of acid or basic cpd.

The example of solvent for use can comprise for example water, lower alcohol, for example methyl alcohol, ethanol, Virahol or the trimethyl carbinol, ketone, for example acetone or methylethylketone, ether, for example diethyl ether, dioxan, tetrahydrofuran (THF), diethylene glycol monomethyl ether or diglyme, aliphatic acid, for example acetate or formic acid, ester, for example ethyl acetate or methyl acetate, halohydrocarbon, for example chloroform, methylene dichloride, ethylene dichloride or tetracol phenixin, dimethyl sulfoxide (DMSO), N, dinethylformamide, HMPA, or their mixed solvent.

The example of acid can comprise for example mineral acid, for example hydrochloric acid, sulfuric acid or Hydrogen bromide, and organic acid, for example formic acid, acetate, trifluoroacetic acid or sulfonic acid are for example right-toluenesulphonic acids.

The example of basic cpd can comprise for example carbonate, for example yellow soda ash, salt of wormwood, sodium bicarbonate or saleratus, metal hydroxides, for example sodium hydroxide, potassium hydroxide, calcium hydroxide or lithium hydroxide etc.

The mol ratio of used acid or basic cpd and compound (20) is at least 1: 1, preferably between 1: 1 and 10: 1, perhaps can greatly excessively be used as reaction solvent.

Reaction is generally carried out under about 0-200 ℃, preferred 0-150 ℃, generally finishes in about 10 minutes to 30 hours.

After said hydrolyzed is handled, can further handle, about 1-30 of time minute, temperature was generally 0-100 ℃, preferably about room temperature to 70 ℃, in appropriate solvent, in the presence of basic cpd, to finish reaction.Here solvent for use and basic cpd can use and be used in solvent and the basic cpd that makes in the compound (1c) and compound (18) reaction method (d) in the above-mentioned reaction process 10 in the method that carboxylic acid halides and amine (1c) reacts arbitrarily.

The reaction of compound (21) and compound (22) with above-mentioned reaction process 10 in carry out under compound (1c) and the reaction conditions like compound (18) reacting phase.The amount of carboxylic acid (18) is based on amine (1c) in above-mentioned reaction process 10, and the amount of amine (22) is based on carboxylic acid (18) in this reaction.

Reaction process 12

(R wherein ^1A, n, X, m, W, o, X ², R ⁴And R ⁵Same as described above.)

The reaction of compound (1i) and compound (23) be with above-mentioned reaction process 10 in carry out under the reaction conditions like the reacting phase of compound (1c) and compound (17).

Reaction process 13

(R wherein ^1A, n, R ¹⁸, X, m, W, o, R ⁴And X ²Same as described above.)

R ^6aaRepresent the C1-C6 alkoxy carbonyl.

R ^6bbRepresent the C1-C6 alkyl; (it can be replaced by at least one group on this benzyl ring phenyl, and described substituting group is selected from the alkylene dioxo base by C1-C4, cyano group, nitro, can have the C1-C6 alkyl as substituent amino, can have the C1-C6 alkyl as the substituent quilt alkylsulfonyl of amino-replacement, the C1-C6 alkoxy carbonyl, the C1-C6 alkylthio, phenoxy group, phenyl C1-C6 alkoxyl group, pyrrolidyl (it can be replaced by at least one oxo base on this pyrrolidine ring), imidazolyl, different _ the azoles base, _ azoles base, phenyl C1-C6 alkyl, phenyl, can have the C1-C6 alkyl as substituent amino C1-C6 alkyl, pyrrolidyl C1-C6 alkoxyl group, halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed); Phenyl C1-C6 alkoxy carbonyl (it can be replaced by at least one group on this benzyl ring, and described substituting group is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group); Benzofuryl C1-C6 alkyl (it can be replaced by at least one group on this cumarone ring, and described substituting group is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group); Benzofuryl C2-C6 thiazolinyl (it can be replaced by at least one group on this cumarone ring, and described substituting group is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group); Phenoxy group C1-C6 alkyl (it can be replaced by at least one group on this benzyl ring, and described substituting group is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group); Thiazolyl C1-C6 alkyl (it can on this thiazole ring by at least one phenyl (it can be replaced by at least one group on this benzyl ring, and described substituting group is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group) replacement); Phenyl C1-C6 alkyl (it can on this benzyl ring by at least one phenyl (it can be replaced by at least one group on this benzyl ring, and described substituting group is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group), halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or the replacement of unsubstituted C1-C6 alkoxyl group); Pyridyl C1-C6 alkyl (it can on this pyridine ring by at least one phenyl (it can be replaced by at least one group on this benzyl ring, and described substituting group is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group) replacement); The C1-C6 alkoxy carbonyl; Benzothienyl; Benzothienyl C1-C6 alkyl (it can be replaced by at least one halogen atom on this thionaphthene ring); Indyl C1-C6 alkyl (it can be replaced by at least one group on this indole ring, and described substituting group is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group); 4H-1,3-benzo two _ Ying Ji (wherein at this 4H-1,3-benzo two _ Ying Huanshang can be substituted with at least one halogen atom); Naphthyl; Quinolyl; Benzothiazolyl (it can be replaced by at least one C1-C6 alkyl on this benzothiazole ring); 2,3-dihydro-1H-indenyl (it can this 2, replaced by at least one oxo base on 3-dihydro-1H-indenes ring); The 9H-fluorenyl; Or phenyl C2-C6 thiazolinyl (it can be replaced by at least one group on this benzyl ring, and described substituting group is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group).

R ^6cRepresent benzoyl (it can be replaced by at least one group, and described substituting group is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group), halogen atom on this benzyl ring, halogen replaces or unsubstituted C1-C6 alkyl and halogen replacement or unsubstituted C1-C6 alkoxyl group.

R ^6dRepresentative: hydrogen atom; (it can be replaced by at least one group on this benzyl ring phenyl, described substituting group is selected from by phenyl (it can be replaced by at least one group on this benzyl ring, and described substituting group is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group), halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replacement or unsubstituted C1-C6 alkoxyl group are formed group); Benzofuryl C1-C6 alkyl (it can be replaced by at least one group on this cumarone ring, and described substituting group is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group); Benzofuryl (it can be replaced by at least one group on this cumarone ring, and described substituting group is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group); Phenoxy group C1-C6 alkyl (it can be replaced by at least one group on this benzyl ring, and described substituting group is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group); Thiazolyl C1-C6 alkyl (it can on this thiazole ring by at least one phenyl (it can be replaced by at least one group on this benzyl ring, and described substituting group is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group) replacement); Thiazolyl (it can on this thiazole ring by at least one phenyl (it can be replaced by at least one group on this benzyl ring, and described substituting group is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group) replacement); (it can be replaced by at least one group on this benzyl ring phenyl C1-C6 alkyl, described substituting group is selected from by phenyl (it can be replaced by at least one group on this benzyl ring, and described substituting group is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group), halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replacement or unsubstituted C1-C6 alkoxyl group are formed group); Pyridyl C1-C6 alkyl (it can on this pyridine ring by at least one phenyl (it can be replaced by at least one group on this benzyl ring, and described substituting group is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group) replacement); Benzothienyl C1-C6 alkyl (can at least one halogen atom be arranged) at this thionaphthene substitution in ring; Indyl C1-C6 alkyl (it can be replaced by at least one group on this indole ring, and described substituting group is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group); Pyridyl (it can on this pyridine ring by at least one phenyl (it can be replaced by at least one group on this benzyl ring, and described substituting group is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group) replacement); Benzothienyl (can at least one halogen atom be arranged) at this thionaphthene substitution in ring; Or indyl (it can be replaced by at least one group on this indole ring, and described substituting group is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group).

R ^6eRepresent phenyl (it can be replaced by at least one group, and described substituting group is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group) on this benzyl ring.

Group-CHR in the general formula (1o) ¹⁸R ^6dTotal carbon number should be no more than 6.Reaction from compound (1k) to compound (1l) be with above-mentioned reaction process 11 carry out under the reaction conditions like from compound (20) to the reacting phase of compound (21).

The reaction of compound (1l) and compound (24) be with above-mentioned reaction process 10 in carry out under the reaction conditions like the reacting phase of compound (1c) and compound (17).

The reaction of compound (1l) and compound (25) be with above-mentioned reaction process 10 in carry out under the reaction conditions like the reacting phase of compound (1c) and compound (18).

The reaction of compound (1l) and compound (26) be with above-mentioned reaction process 10 in carry out under the reaction conditions like the reacting phase of compound (1c) and compound (16).

The reaction of compound (1l) and compound (27) be with above-mentioned reaction process 10 in carry out under the reaction conditions like the reacting phase of compound (1c) and compound (19).

Reaction process 14

(R wherein ^1A, n, X, m, W, o and R ⁴Same as described above.R ^6fRepresent C1-C6 alkyl or phenyl C1-C6 alkyl (it can be replaced by at least one group, and described substituting group is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group) on this benzyl ring.)

Compound (1q) is in appropriate solvent, carries out in the presence of condensing agent with the reaction of compound (26).

Here solvent for use can use and make employed any solvent in the method that carboxylic acid halides and amine (1c) reacts in other method (d) of compound (1c) and compound (18) reaction in above-mentioned reaction process 10.

The example of condensing agent can comprise for example N, N '-carbonyl dimidazoles etc.The mol ratio of compound used therefor (26) and condensing agent and compound (1q) can be at least, preferably between about 1: 1 and 2: 1.Reaction is generally carried out under 0-150 ℃, preferred about 0-100 ℃, finishes in about 1-30 hour.

Reaction process 15

(R wherein ^1A, n, X, m, W, o, R ⁹And R ¹⁰Same as described above.)

The reaction of compound (27) and compound (28) be with above-mentioned reaction process 10 in carry out under the reaction conditions like the reacting phase of compound (1c) and compound (16).

Reaction process 16

(R wherein ^1A, n, X, m, W, o, R ^7aAnd R ^10aSame as described above.Two W in the general formula (1t)-(1v) can be identical or different.R ^9fRepresent the C1-C6 alkoxy carbonyl.Dotted line representative on the piperidine ring can be the key of two keys.When dotted line is two key, should be substituted with the oNR of group-(W) ^9fR ^10a, the oNHR of group-(W) ^10aOr the oNR of group-(W) ^10a(COOR ^9g).R ^9gRepresent C1-C6 alkyl or phenyl C1-C6 alkyl (it can be replaced by at least one group, and described substituting group is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group) on this benzyl ring.)

Reaction from compound (1t) to compound (1u) be with above-mentioned reaction process 11 carry out under the reaction conditions like from compound (20) to the reacting phase of compound (21).

The reaction of compound (1u) and compound (29) be with above-mentioned reaction process 14 in carry out under the reaction conditions like the reacting phase of compound (1q) and compound (26).

Initial compounds (20) in initial compounds in the reaction process 9 (14) and the reaction process 11 is new compound.These compounds are to make easily, for example according to above-mentioned reaction process 1 to 3, use corresponding raw material to get final product.

The present invention is contained steric isomer and optically active isomer by compound (final compound) and above-mentioned each reaction process gained intermediate of general formula (1) representative.

Above-mentioned each each target compound of reaction process gained can separate and purifying from reaction mixture, for example separate crude reaction product by lock out operation, the for example filtration after the cooling, concentrate and extraction, succeeded by common purification process, for example column chromatography and recrystallization.

The compounds of this invention comprises the pharmacy acceptable salt of formula (1) compound.A kind of like this example of salt comprises inorganic salt, for example hydrochloride, hydrobromate, nitrate, vitriol or phosphoric acid salt, and organic salt, for example mesylate, right-tosylate, acetate, Citrate trianion, tartrate, maleate, fumarate, malate or lactic acid salt.

Below, explanation is contained the medical prepared product of The compounds of this invention as activeconstituents.

Above-mentioned medical prepared product is to prepare The compounds of this invention by the form with common medical prepared product to obtain.Use thinner commonly used or vehicle to prepare it, for example weighting agent, swelling agent, tackiness agent, wetting agent, disintegrating agent, tensio-active agent or lubricant.

A kind of so medical prepared product can be selected from various forms, and this depends on therapeutic purpose.The representative instance of prepared product form comprises tablet, pill, pulvis, liquid, suspension, emulsion, granule, capsule, suppository and injection (liquid, suspension etc.).

When the medical prepared product of preparation tablet form, can be extensive use of known carrier.A kind of like this example of carrier comprises vehicle, for example lactose, sucrose, sodium-chlor, glucose, urea, starch, lime carbonate, kaolin or crystalline cellulose; Tackiness agent, for example water, ethanol, propyl alcohol, simple syrup, glucose solution, starch solution, gelatin solution, carboxymethyl cellulose, shellac, methylcellulose gum, potassiumphosphate or polyvinylpyrrolidone; Disintegrating agent, for example dry starch, sodiun alginate, agar powder, kelp Icing Sugar, sodium bicarbonate, lime carbonate, Vykamol Sorbitol 8B, Sodium Lauryl Sulphate BP/USP, glyceryl monostearate, starch or lactose; Disintegration control agent, for example sucrose, tristearin, theobroma oil or winterized stearin; Absorption enhancer, for example quaternary ammonium hydroxide or Sodium Lauryl Sulphate BP/USP; Wetting agent, for example glycerine or starch; Sorbent material, for example starch, lactose, kaolin, wilkinite or colloid silica; And lubricant, for example purified talcum, stearate, boric acid powder or polyoxyethylene glycol.

And this class tablet can be made into to have the tablet of conventional tablet dressing, for example coated tablet, gelatine glaze sheet, casing sheet, film garment piece, double-contracting garment piece or many coating tablets.

When the medical prepared product of preparation pill, can be extensive use of known carrier.A kind of like this example of carrier comprises vehicle, for example glucose, lactose, starch, theobroma oil, hydrogenated vegetable oil, kaolin or talcum; Tackiness agent, for example gummi arabicum pulveratum, tragacanth gum powder, gelatin or ethanol; And disintegrating agent, for example laminariose (laminaran) or agar.

When the medical prepared product of preparation suppository form, can be extensive use of known carrier.A kind of like this example of carrier comprises polyoxyethylene glycol, theobroma oil, higher alcohols, high alcohol ester, gelatin and semisynthetic glyceryl ester.

Be made at medical prepared product under the situation of injection, for example liquid, emulsion or suspension preferably with these solution sterilizations, and are made with blood isoosmotic.When the medical prepared product of preparation a kind of like this liquid, emulsion or suspensions, can be extensive use of known thinner.A kind of like this example of thinner comprises water, ethanol, propylene glycol, ethoxylation isooctadecanol, polyoxyethylene isooctadecanol (polyoxylated isostearyl alcohol) and Vykamol Sorbitol 8B.And, using under the situation of medical prepared product as injection, can add a certain amount of salt, glucose or glycerine to medical prepared product, be enough to prepare isotonic solution.Perhaps, also can add common solubilizing agent, buffer reagent, negative catalyst etc. to medical prepared product.And then, if necessary, also can be to wherein adding tinting material, sanitas, spices, correctives, sweeting agent or other drug.

The content of The compounds of this invention in medical prepared product is not particularly limited, but can suitably be selected from wide in range scope.Generally speaking, the The compounds of this invention that in medical prepared product, preferably contains 1 to 70 weight %.

The method that gives the present invention's medicine prepared product is not particularly limited.Can carry out administration according to various prepared product forms, patient's age, sex, disease condition or other conditions.For example, if medical prepared product is taked tablet, pill, liquid, suspension, emulsion, granule or Capsule form, then oral administration.Under the situation of injection, can intravenous administration, separately or with common complementary combination of fluids, for example glucose or amino acid.And, if necessary, intramuscular, intradermal, subcutaneous or intraperitoneal administration individually.Under the situation of suppository, can drop rectum with drug.

Depend on usage, patient's age, sex, disease levels or other conditions, can suitably select the dosage of above-mentioned medical prepared product.Generally speaking, every kg body weight gives 0.01 to 100mg, preferred 0.1 to 50mg medical prepared product, once a day or be divided into several times.

Because above-mentioned dosage is different because of various conditions, may be enough in some cases less than the dosage of above-mentioned scope, perhaps in other cases may be greater than the dosage of above-mentioned scope.

The compounds of this invention has the specificity effect to mycobacterium tuberculosis, for example acid-fast bacterium (Mycobacterium, atypical acid-fast bacterium).The compounds of this invention has excellent effect to the multidrug-resisting mycobacterium tuberculosis.The compounds of this invention has anti-microbial effect to anaerobic bacterium.

The above-mentioned activity of the not only external demonstration of The compounds of this invention, and when oral administration, also show above-mentioned activity.

The compounds of this invention can not bring out diarrhoea, and the broad-spectrum antimicrobial agent of common bacteria (for example gram positive bacterium or gram negative bacterium) can be brought out diarrhoea.In addition, its untoward reaction is less than existing medicine.Therefore, it can be can long term administration medical prepared product.

The compounds of this invention can distribute in lung tissue good (major organs that lung is infected by acid-fast bacterium), and has such as character such as persistence effect or excellent securities.Therefore, expect the result of treatment height of described compound.

With existing antitubercular agent relatively the time, the show strong germicidal action of The compounds of this invention even also be so at the cytozoicus bacterium, for example is present in the mycobacterium tuberculosis in the human macrophage.Therefore, it can reduce recurrence rate lungy, realizes the short-term chemotherapy.Therefore expect that The compounds of this invention also can be used as main prophylactic agent and uses, for the HIV and the tuberculosis polyinfection administration that are regarded as serious problems.

Embodiment

Formulation example, test example, reference example and embodiment will be described below.

Formulation example 1

100g The compounds of this invention, 40g Avicel (trade mark is made by Asahi KaseiCorporation), 30g W-Gum and 2g Magnesium Stearate are mixed, grind, make tablet with sugar-coat R10mm pestle then.

Use film Drug coating dressing gained tablet, wherein contain 10g TC-5 (trade mark, Vltra tears is by Shin-Etsu Chemical Co., Ltd. make), 3g polyethylene glycol 6000,40g Viscotrol C and an amount of ethanol, form film garment piece with above-mentioned composition.

Reference example 1

The preparation of 1-(4-(tetrahydropyrans-2-base oxygen base) phenyl)-4-(N-(4-chloro-phenyl-)-N-methylamino) piperidines

Under nitrogen atmosphere, with 4-(N-(4-chloro-phenyl-)-N-methylamino)-piperidines (2.52g, 11.22mmol), 2-(4-bromine phenoxy group) tetrahydropyrans (2.89g, 11.22mmol), acid chloride (50mg, 0.22mmol), (S)-(-)-2, two (diphenyl phosphine)-1,1 of 2-'-dinaphthalene (BINAP) (212mg, 0.34mmol) and tert.-butoxy sodium (1.51g, 15.71mmol) reflux 3 hours in toluene (30ml).Add ethyl acetate and water to reaction soln, stir, remove by filter the gained precipitation by C salt then, use ethyl acetate extraction filtrate then.Organic phase is washed with saturated brine,, filter then through dried over mgso.After under reduced pressure concentrating gained filtrate, resistates is through silica gel chromatography (n-hexane/ethyl acetate=20/1), obtain 1-(4-(tetrahydropyrans-2-base oxygen base) phenyl)-4-(N-(4-chloro-phenyl-)-N-methylamino) piperidines (1.33g, yield 30%), be buff powder.

¹H-NMR(CDCl ₃)δppm：

1.50-2.04(10H，m)，2.68-2.80(2H，m)，2.78(3H，s)，3.50-3.70(4H，m)，3.85-4.03(1H，m)，5.31(1H，t，J＝5.7Hz)，6.72(2H，d，J＝9.1Hz)，6.90(2H，d，J＝9.2Hz)，6.98(2H，d，J＝9.2Hz)，7.17(2H，d，J＝9.1Hz).

Reference example 2

The preparation of 4-(4-(N-(4-chloro-phenyl-)-N-methylamino) piperidines-1-yl) phenol

(4-(tetrahydropyrans-2-base oxygen base) phenyl)-(1.33g 3.32mmol) is suspended in the ethanol (80ml) 4-(N-(4-chloro-phenyl-)-N-methylamino) piperidines with 1-.To the right-toluenesulphonic acids pyridine of this mixture adding _ (0.25g 1mmol), stirred 8 hours down at 70 ℃ then.Under reduced pressure remove ethanol, add methylene dichloride and saturated sodium bicarbonate aqueous solution to this resistates then, stir.Use dichloromethane extraction,, filter then through dried over mgso.After under reduced pressure concentrating gained filtrate, add methylene dichloride and normal hexane, filter the gained precipitation, obtain 4-(4-(N-(4-chloro-phenyl-)-N-methylamino) piperidines-1-yl) phenol (922.5mg, yield 88%), be the baby pink powder to resistates.

¹H-NMR(CDCl ₃)δppm：

1.79-2.04(4H，m)，2.67-2.79(2H，m)，2.79(3H，s)，3.56-3.68(2H，m)，4.48(1H，s)，6.69-6.80(4H，m)，6.85-6.92(2H，m)，7.14-7.21(2H，m).

Be similar to reference example 1 and 2 preparation following compounds.In the following table, Ph represents phenyl or phenylene.

Reference example 3

(4-chloro-phenyl-)-(4-hydroxy phenyl) ketone O-methyloxime

Ms：261(M ⁺).

Reference example 4

(4-hydroxy phenyl)-(4-trifluoromethyl) ketone O-methyloxime

Ms：295(M ⁺).

[table 1]

Reference example	R1	¹HNMR or MS
Reference example	R1	¹HNMR or MS	5 6 7 8 9 10 11 12	-CH ₂C ₆H ₅ 4-CF ₃OPhCH ₂- 4-CF ₃PhCH ₂- 4-ClPhCH ₂- 3，4-Cl ₂PhCH ₂- 4-CF ₃OPh(CH ₂) ₂- 4-CF ₃OPhCH＝CHCH ₂- 4-CF ₃OPh(CH ₂) ₃-	¹H NMR(CDCl ₃)δ1.79-1.89(2H，m)，2.01-2.08(2H，m)， 2.77-2.87(2H，m)，3.33-3.41(2H，m)，3.53-3.56(2H，m)，4.59(2H，s)， 4.63(1H，brs)，6.74(2H，d，J＝9.0Hz)，6.87(2H，d，J＝9.0Hz)， 7.27-7.36(5H，m). ¹H NMR(CDCl ₃)δ1.76-1.90(2H，m)，2.00-2.10(2H，m)，2.84(2H，m)， 3.33-3.42(2H，m)，3.51-3.60(1H，m)，4.53(1H，brs)，4.63(2H，s)，6.74(2H， d，J＝9.0Hz)，6.87(2H，d，J＝9.0Hz)，7.48(2H，d，J＝8.1Hz)，7.60(2H，d， J＝8.2Hz). ¹H NMR(CDCl ₃)δ1.71-1.93(2H，m)，1.95-2.15(2H，m)，2.71-2.93(2H， m)，3.26-3.46(2H，m)，3.46-3.63(1H，m)，4.50(1H，s).4.57(2H，s)，6.74(2H， d，J＝9.0Hz)，6.87(2H，d，J＝8.9Hz)，7.19(2H，d，J＝8.5Hz)，7.39(2H，d， J＝8.4Hz). ¹H NMR(CDCl ₃)δ1.69-1.91(2H，m)，1.95-2.14(2H，m). 2.72-2.90(2H，m)，3.26-3.44(2H，m)，3.44-3.63(1H，m)，4.46(1H，broad s)， 4.54(2H，s)，6.74(2H，d，J＝9.0Hz)，6.87(2H，d，J＝9.0Hz)，7.20-7.33(4H， m). ¹H NMR(CDCl ₃)δ1.71-1.93(2H，m)，1.93-2.18(2H，m)， 2.70-2.93(2H，m)，3.22-3.45(2H，m)，3.45-3.65(1H，m)，4.52(2H，s)， 4.85(1H，brs)，6.73(2H，d，J＝9.0Hz)，6.82(2H，d，J＝9.0Hz)，7.19(1H，dd， J＝8.2Hz.2.0Hz)，7.41(1H，d，J＝8.2Hz)，7.46(1H，d，J＝1.9Hz). Ms：381(M+) Ms：393(M+) Ms：395(M+)

[table 2]

Reference example	R1	R2	NMR or MS
Reference example	R1	R2	NMR or MS	13 14 15 16 17 18 19 20 21 22 23 24 25 26 27	4-ClPh- 4-CF ₃Ph- -CH ₂C ₆H ₅ 4-ClPhCH ₂- 3，4-Cl ₂PhCH ₂- 4-CF ₃PhCH ₂- 4-CF ₃OPhCH ₂- 4-CH ₃OPh- 4-ClPh- -CH ₂C ₆H ₅4-CH ₃OPh- 4-CF ₃Ph- 4-CF ₃PhCH ₂- (CH ₃) ₃COCO- (CH ₃) ₃COCO-	-CH ₃ -H -H -H -H -H -H -H -H -CH ₃ -CH ₃ -CH ₂CH ₂OCH ₃ -C ₆H ₅ -H -C ₂H ₅	¹H NMR(CDCl ₃)δ1.79-2.04(4H.m)，2.67-2.79(2H，m)， 2.79(3H，s)，3.56-3.68(2H，m)，4.48(1H，s)，6.69-6.80(4H，m)， 6.85-6.92(2H，m)，7.14-7.21(2H，m). ¹H NMR(CDCl ₃)δ1.56-1.72(2H，m)，2.13-2.20(2H，m)， 2.77-2.88(2H，m)，3.44-3.51(3H，m)，3.92(1H，d，J＝7.94Hz)， 4.86(1H，s)，6.59-6.63(2H，m)，6.72-6.79(2H，m)， 6.85-6.92(2H，m)，7.38-7.42(2H，m). ¹H NMR(CDCl ₃)δ1.26-2.46(3H，m)，2.51-2.80(3H，m)， 3.36-3.56(2H，m)，3.86(2H，s)，6.65-6.79(2H，m)，6.79-6.91(2H， m)，7.15-7.43(5H，m). ¹H NMR(CDCl ₃)δ1.34-1.87(2H，m)，1.88-2.11(2H，m)， 2.51-2.74(3H，m)，3.26-3.57(m，2H)，3.82(2H，s)，6.66-6.79(2H， m)，6.79-6.92(2H，m)，7.09-7.41(4H，m). ¹H NMR(CDCl ₃)δ1.34-1.80(2H，m)，1.89-2.10(2H，m)， 2.50-2.80(3H，m)，3.31-3.54(2H，m)，3.81(2H，s)，6.65-6.79(2H， m).6.80-6.90(2H，m)，7.11-7.23(1H，d，J＝8.0Hz)，7.33-7.42(1H. d，J＝8.2Hz)，7.43-7.50(1H，d，J＝2.0Hz). ¹H NMR(CDCl ₃)δ1.40-1.86(2H，m)，1.87-2.12(2H，m)， 2.50-2.80(3H，m)，3.38-3.56(2H，m)，3.92(2H，s)，6.66-6.80(2H， m)，6.80-6.93(2H，m)，7.47(2H，d，J＝8.2Hz)，7.58(2H，d， J＝8.1Hz). ¹H NMR(CDCl ₃)δ1.45-1.70(2H，m)，1.88-2.16(2H，m)， 2.48-2.83(3H，m)，3.33-3.57(2H，m)，3.85(2H，s)，6.62-6.78(2H， m)，6.80-6.93(2H，m)，7.17(2H，d，J＝8.4Hz)，7.37(2H，d， J＝8.5Hz). ¹H NMR(CDCl ₃)δ1.53-1.69(2H，m)，2.13-2.19(2H，m)， 2.75-2.86(2H，m)，3.37-3.51(3H，m)，3.63(1H，d，J＝7.86Hz)， 4.48(1H，s)，6.53-6.61(2H，m)，6.72-6.80(2H，m). 6.85-6.92(2H，m)，7.01-7.05(2H，m). ¹H NMR(CDCl ₃)δ1.52-1.68(2H，m)，2.13-2.18(2H，m)， 2.75-2.86(2H，m)，3.35-3.56(4H，m)，4.59(1H，brs)， 6.51-6.58(2H，m)，6.70-6.79(2H，m)，6.85-6.93(2H，m)， 7.10-7.15(2H，m). Ms：296(M+) Ms：366(M+) Ms：366(M+) Ms：426(M+) Ms：292(M+) Ms：320(M+)

[table 3]

Reference example	R1	NMR or MS
Reference example	R1	NMR or MS	28 29 30 31 32 33 34 35 36 37 38 39 40 41	-C ₆H ₅ 4-CF ₃OPhO- 4-CF ₃OPhCH ₂O- 4-CF ₃OPh- 4-CF ₃Ph- 4-ClPh- 3，4-Cl ₂Ph- 4-ClPhCH ₂O- 4-CF ₃PhCH ₂O- 4-ClPhO- 4-CF ₃PhNH- 4-ClPhNH- 4-CF ₃OPhNH- 4-ClPhNHCO ₂-	Ms；267(M+) ¹H NMR(CDCl ₃)δ1.48-1.63(2H，m)，1.87-1.98(3H，m)， 2.62-2.72(2H，m)，3.51-3.57(2H，m)，3.83(2H，d，J＝5.88Hz)， 4.50(1H，brs)，6.73-6.78(2H，m)，6.84-6.91(4H，m)，7.12- 7.16(2H，m). ¹H NMR(CDCl ₃)δ1.36-1.90(5H，m)，2.56-2.68(2H，m)， 3.38(2H，d，J＝6.31Hz)，3.44-3.53(2H，m)，4.51(2H，s)， 4.66(1H，brs)，6.70-6.77(2H，m)，6.83-6.89(2H，m)，7.17- 7.21(2H，m)，7.34-7.39(2H，m). Ms；351(M+) ¹H NMR(CDCl ₃)δ1.31-1.86(5H，m)，2.43-2.77(4H，m)， 3.34-3.58(2H，m)，4.57(1H，brs)，6.66-6.80(2H，m)，6.80- 6.92(2H，m)，7.28(2H，d，J＝7.7Hz)，7.55(2H，d，J＝8.1Hz). Ms；301(M+) Ms：335(M+) ¹H NMR(CDCl ₃)δ1.34-1.51(2H，m)，1.68-1.90(3H，m)， 2.56-2.67(2H，m)，3.36(2H，d，J＝6.36Hz)，3.46-3.52(2H，m)， 4.43(1H，s)，4.48(2H，s)，6.71-6.78(2H，m)，6.83-6.89(2H，m)， 7.27-7.34(4H，m). ¹H NMR(CDCl ₃)δ1.37-1.54(2H，m)，1.68-1.90(3H，m)， 2.57-2.68(2H，m)，3.39(2H，d，J＝6.29Hz)，3.46-3.52(2H，m)， 4.57(2H，s)，5.28(1H，s)，6.67-6.74(2H，m)，6.83-6.89(2H，m)， 7.43-7.47(2H，m)，7.58-7.62(2H，m). ¹H NMR(CDCl ₃)δ1.48-1.63(2H，m)，1.86-1.98(3H，m)， 2.61-2.71(2H，m)，3.51-3.56(2H，m)，3.82(2H，d，J＝5.95Hz)， 4.49(1H，s)，6.73-6.91(6H，m)，7.19-7.25(2H，m). ¹H NMR(CDCl ₃)δ1.38-1.54(2H，m)，1.64-1.79(1H，m)， 1.89(2H，d，J＝12.9Hz)，2.62(2H，dt，J＝1.99，11.98Hz)， 3.11(2H，t，J＝6.27Hz)，3.52(2H，d，J＝11.98Hz)，4.00- 4.18(1H，brm)，4.46(1H，brs)，4.39-4.55(1H，brs)，6.60(2H，d， J＝8.56Hz)，6.75(2H，d，J＝8.89Hz)，6.87(2H，d，J＝8.89Hz)， 7.40(2H，d，J＝8.56Hz) ¹H NMR(CDCl ₃)δ1.37-1.57(2H，m)，1.61-1.77(1H，m)， 1.79-1.97(2H，m)，2.52-2.70(2H，m)，3.04(2H，d，J＝6.70Hz)， 3.51(2H，d，J＝11.98Hz)，3.76-4.76(2H，br)，6.48-6.58(2H， m)，6.71-6.81(2H，m)，6.83-6.92(2H，m)，7.08-7.17(2H，m) ¹H NMR(CDCl ₃)δ1.37-1.81(4H，m)，1.90(2H，d，J＝6.20Hz)， 2.63(2H，t，J＝11.68Hz)，3.05(2H，d，J＝6.66Hz)，3.52(2H，d， J＝11.99Hz)，3.69-4.07(1H，br)，4.18-4.74(1H，br)，6.49- 6.63(2H，m)，6.67-6.82(2H，m)，6.87(2H，d，J＝8.64Hz)， 7.03(2H，d，J＝8.64Hz) ¹H NMR(DMSO)δ1.35-1.45(2H，m)，1.68-1.80(3H，m)， 2.46-2.56(2H，m)，3.40-3.46(2H，m)，4.00(2H，d，J＝5.90Hz)， 6.61-6.65(2H，m)，6.67-6.81(2H，m)，7.31-7.35(2H，m)，7.45- 7.51(2H，m)，8.78(1H，s)，9.79(1H，s).

[table 4]

Reference example	R1	R2	NMR
Reference example	R1	R2	NMR	42	-H	4-CF ₃OPhCH＝CHCH ₂-	¹H NMR(CDCl ₃)δ3.58(1H，brs)，3.89(2H，d，J＝5.7Hz)，4.24(1H， brs)，6.31(1H，dt，J＝15.9，5.7Hz)，6.57-6.62(3H，m)，6.69-6.73(2H，m)， 7.13-7.16(2H，m)，7.36-7.38(2H，m).

[table 5]

[table 6]

Reference example	R1	NMR
Reference example	R1	NMR	52 53	4-CF ₃Ph- 4-ClPh-	¹H NMR(CDCl ₃)δ3.96(2H，s)，4.66(1H，s)， 6.75-6.79(2H，m)，7.01-7.06(2H，m)，7.26-7.29(2H，m)， 7.51-7.54(2H，m). ¹H NMR(CDCl ₃)δ3.87(3H，brs)，6.74-6.78(2H，m)， 7.01-7.04(2H，m)，7.07-7.10(2H，m)，7.22-7.26(2H，m).

[table 7]

[table 8]

Reference example	R1	MS
Reference example	R1	MS	61 62 63	4-CF ₃OPhCH ₂- 4-CF ₃OPhN(CH ₃)- 4-ClPhN(CH ₃)-	260(M+1) ⁺ 224(M ⁺) 224(M ⁺)

[table 9]

[table 10]

Reference example	R1	R2	NMR
Reference example	R1	R2	NMR	65 66 67 68 69 70 71 72	-H -H -H -H -H -H -H -H	4-CF ₃PhCH ₂O(CH ₂) ₂- 4-CF ₃OPhCH ₂OCH ₂- 4-CF ₃OPhCH ₂O(CH ₂) ₂- 4-FPhNH- 4-CF ₃OPhNHCH ₂- 4-ClPhNHCH ₂- 3，5-Cl ₂PhNH- 4-n-C ₃H ₇-PhNH-	CDCl3；1.35-1.67(5H，m)，1.76-1.82(2H，m)，2.55-2.66 (2H，m)，3.44-3.50(2H，m)，3.57(2H，t，J＝6.3Hz)，4.38 (1H，s)，4.57(2H，s)，6.72-6.78(2H，m)，6.84-6.89 (2H，m)，7.43-7.48(2H，m)，7.59-7.62(2H，m) CDCl3；1.36-1.53(2H，m)，1.65-1.82(1H，m)，1.84-1.90 (2H，m)，2.56-2.67(2H，m)，3.38(2H，d，J＝6.3Hz)， 3.44-3.53(2H，m)，4.51(2H，s)，4.66(1H，bs)，6.70-6.77 (2H，m)，6.83-6.89(2H，m)，7.17-7.21(2H，m)，7.34-7.39 (2H，m) CDCl3；1.37-1.66(5H，m)，1.75-1.81(2H，m)，2.55-2.65 (2H，m)，3.44-3.50(2H，m)，3.55(2H，t，J＝6.3Hz)，4.44 (1H，s)，4.50(2H，s)，6.72-6.78(2H，m)，6.83-6.89 (2H，m)，7.18-7.22(2H，m)，7.35-7.39(2H，m) CDCl3；1.51-1.66(2H，m)，2.13-2.18(2H，m)，2.74- 2.85(2H，m)，3.30-3.50(4H，m)，4.50(1H，s)，6.53- 6.61(2H，m)，6.73-6.78(2H，m)，6.85-6.94(4H，m) CDCl3；7.03(2H，d，J＝8.6Hz)，6.87(2H，d，J＝8.6Hz)， 6.82-6.67(2H，m)，6.63-6.49(2H，m)，4.74-4.18(1H，br)， 4.07-3.69(1H，br)，3.53(2H，d，J＝12.0Hz)，3.05(2H，d， J＝6.7Hz)，2.63(2H，t，J＝6.7Hz)，1.90(2H，d，J＝12.4Hz)， 1.81-1.37(3H，m) CDCl3；7.17-7.08(2H，m)，6.92-6.83(2H，m)，6.81- 6.71(2H，m)，6.58-6.48(2H，m)，4.76-3.76(2H，br)， 3.51(2H，d，J＝12.0Hz)，3.04(2H，d，J＝6.7Hz)，2.70- 2.52(2H，m)，1.88(2H，d，J＝12.3Hz)，1.77-1.61(1H，m)， 1.57-1.37(2H，m) CDCl3； 1.48-1.64(2H，m)，2.05-2.19(2H，m)，2.71-2.88(2H， m)，3.21-3.48(3H，m)，3.75(1H，d，J＝8.0Hz)，4.71 (1H，bs)，6.46(2H，d，J＝1.8Hz)... CDCl3； 0.94(3H，t，J＝7.3Hz)，1.45-1.71(4H，m)，2.05-2.21 (2H，m)，2.47(2H，t，J＝7.3Hz)，2.64-2.83(2H，m)， 3.29-3.52(3H，m)，4.83(1H，br)，6...

[table 11]

[table 12]

Reference example	R1	R2	MS
Reference example	R1	R2	MS	77 78 79 80 81 82 83 84 85 86	-H -H -OH -H -H -H -H -H -H -H	4-CF ₃OPhCH ₂- 4-CF ₃OPh(CH ₂) ₃O- 4-ClPH- 4-CF ₃PhCH ₂OCH ₂- 4-ClPhCH ₂O ₂(CH ₂) ₂- 4-ClPhNHCO(CH ₂) ₂- 4-CF ₃OPh(CH ₂) ₂- 3，4-Cl ₂PhNH- 3-CF ₃OPhCH ₂- 2-CF ₃OPhCH ₂-	351(M ⁺) 395(M ⁺) 303(M ⁺) 364(M-1) ⁺ 345(M ⁺) 374(M ⁺) 365(M ⁺) 336(M-1) ⁺ 351(M ⁺) 351(M ⁺)

[table 13]

[table 14]

[table 15]

[table 16]

Reference example	R1	MS
Reference example	R1	MS	100 101 102	4-CF ₃PhCH ₂- 4-CF ₃OPhCH ₂- 4-ClPhCH ₂-	307 (M ⁺) 323 (M ⁺) 273 (M ⁺)

[table 17]

Reference example	R1	MS
Reference example	R1	MS	103 104	4-CF ₃OPhCH ₂- 4-ClPhCH ₂-	337 (M ⁺) 287 (M ⁺)

[table 18]

Reference example	R1	MS
Reference example	R1	MS	105 106	-Cl -H	245(M ⁺) 211(M ⁺)

[table 19]

[table 20]

[table 21]

Embodiment 1

(R)-and 2-methyl-6-nitro-2-(2-(4-(4-trifluoro-methoxybenzyl)-piperazine-1-yl) benzothiazole-6-base oxygen ylmethyl)-2, the 3-glyoxalidine is the preparation of [2,1-b] _ azoles also

With (R)-2-chloro-1-(2-methyl-2-Oxyranyle (oxyranyl) methyl)-4-nitro-1H-imidazoles (51mg, 0.23mmol) and 6-hydroxyl-2-(4-(4-trifluoro-methoxybenzyl)-piperazine-1-yl)-benzothiazole (80mg 0.20mmol) is dissolved in DMF (5ml).(10mg 0.25mmol), stirred 1.5 hours down at 60 ℃ to add sodium hydride to this mixture.After at room temperature placing, add entry, use ethyl acetate extraction to reaction soln.Merge organic layer, water and saturated brine washing are then through dried over mgso.Filter, then concentrated filtrate under reduced pressure.Resistates is through silica gel chromatography (normal hexane: ethyl acetate=1: 3 → ethyl acetate), recrystallization from ethanol, obtain (R)-2-methyl-6-nitro-2-(2-(4-(4-trifluoro-methoxybenzyl)-piperazine-1-yl) benzothiazole-6-base oxygen ylmethyl)-2,3-glyoxalidine also [2,1-b] _ azoles (40mg, yield 33%), be the crystal of colourless pulverizing.

Fusing point: 205.6-207.4 ℃.

Embodiment 2

(R)-and 2-methyl-6-nitro-2-(2-(4-(4-Trifluoromethyl phenyl ether oxygen base) piperidines-1-yl) pyridine-5-oxygen base) methyl-2, the 3-dihydro-imidazol-is the preparation of [2,1-b] _ azoles also

With 5-hydroxyl-2-(4-(4-trifluoromethoxy)-phenoxy group) piperidines-1-yl) and pyridine (0.67g, 1.9mmol) and (R)-(0.51g 2.4mmol) is dissolved in DMF (6.7ml) to 2-chloro-1-(2-methyl-2-oxiranylmethyl radical)-4-nitro-1H-imidazoles.(91mg 2.3mmol), stirred 1 hour down at 50-55 ℃ to add sodium hydride to this mixture.Add entry to reaction soln, use dichloromethane extraction.Organic layer is washed with saturated brine,, under suction, filter then through dried over mgso.Under reduced pressure concentrate gained filtrate.Resistates is through silica gel chromatography (dichloromethane/ethyl acetate=10/0,9/1,8/2), further crystallization from methylene dichloride/diisopropyl ether/ethyl acetate, obtain (R)-2-methyl-6-nitro-2-(2-(4-(4-Trifluoromethyl phenyl ether oxygen base) piperidines-1-yl) pyridine-5-oxygen base) methyl-2, the 3-dihydro-imidazol-is [2,1-b] _ azoles (0.30g also, yield 29%), be buff powder.

¹H-NMR(CDCl ₃)δppm：

1.77(3H，s)，1.80-1.94(2H，m)，1.94-2.17(2H，m)，3.21-3.44(2H，m)，3.67-3.89(2H，m)，3.96-4.11(2H，m)，4.19(1H，d，J＝10.4Hz)，4.36-4.59(2H，m)，6.65(1H，d，J＝9.2Hz)，6.83-6.97(2H，m)，7.02-7.20(3H，m)，7.56(1H，s)，7.87(1H，d，J＝3.0Hz).

Be similar to the foregoing description 2 preparation following compounds.In the following table, Ph represents phenyl or phenylene.

Embodiment 3

(R)-and 2-(4-(4-(N-(4-chloro-phenyl-)-N-methylamino) piperidines-1-yl) phenoxymethyl)-2-methyl-6-nitro-2, the 3-dihydro-imidazol-is [2,1-b] _ azoles also

Fusing point: 173.7-175.1 ℃.

Embodiment 4

(R)-and 2-methyl-6-nitro-2-(4-(4-(4-trifluoro-methoxybenzyl) piperidines-1-yl) phenoxymethyl)-2, the 3-glyoxalidine is [2,1-b] _ azoles also

¹H-NMR(CDCl ₃)δppm：

1.23-1.52(2H，m)，1.52-1.66(3H，m)，1.66-1.89(3H，m)，2.43-2.70(4H，m)，3.50(2H，d，J＝12.1Hz)，3.91-4.09(2H，m)，4.16(1H，d，J＝10.1Hz)，4.48(1H，d，J＝10.2Hz)，6.66-6.81(2H，m)，6.81-6.95(2H，m)，7.05-7.23(4H，m)，7.54(1H，s).

Fusing point: 210.9-212.4 ℃.

[α] _D=-9.0 ° (concentration: 1.0, CHCl ₃).

Embodiment 5

(R)-and 2-(4-(4-(3, the 4-dichloro benzyl) piperidines-1-yl) phenoxymethyl)-2-methyl-6-nitro-2, the 3-glyoxalidine is [2,1-b] _ azoles also

¹H-NMR(CDCl ₃)δppm：

1.24-1.52(2H，m)，1.52-1.64(4H，m)，1.64-1.73(1H，m)，1.73-1.87(4H，m)，2.38-2.68(4H，m)，3.49(2H，d，J＝12.1Hz)，3.91-4.09(2H，m)，4.16(1H，d，J＝10.2Hz)，4.49(1H，d，J＝10.2Hz)，6.67-6.81(2H，m)，6.81-6.92(2H，m)，6.94-7.07(1H，m)，7.25(1H，s)，7.35(1H，d，J＝8.2Hz)，7.55(1H，s).

Fusing point: 180.0-181.2 ℃.

[α] _D=-8.5 ° (concentration: 1.0, CHCl ₃).

Embodiment 6

(R)-and 6-nitro-2-(4-(4-(4-trifluoromethoxy benzyloxymethyl) piperidines-1-yl) phenoxymethyl)-2, the 3-glyoxalidine is [2,1-b] _ azoles also

Fusing point: 140.4-141.7 ℃.

Embodiment 7

(R)-and 2-methyl-6-nitro-2-(4-(4-(4-trifluoromethyl benzyloxy methyl)-piperidines-1-yl) phenoxymethyl)-2, the 3-glyoxalidine is [2,1-b] _ azoles also

Fusing point: 172.3-172.9 ℃.

Embodiment 8

(R)-and 2-methyl-6-nitro-2-(4-(4-(3-(4-trifluoromethyl)-2-propenyl) piperidines-1-yl) phenoxymethyl)-2, the 3-glyoxalidine is [2,1-b] _ azoles also

Fusing point: 199.7-202 ℃.

Embodiment 9

(R)-and 2-methyl-6-nitro-2-(4-(4-(2-(4-Trifluoromethyl phenyl ether oxygen base) ethyl) piperazine-1-yl) phenoxymethyl)-2, the 3-glyoxalidine is [2,1-b] _ azoles also

Fusing point: 194.8-195.6 ℃.

Embodiment 10

(R)-and 2-(4-(4-(N-(4-chloro-phenyl-)-N-ethylamino) piperidines-1-yl) phenoxymethyl)-2-methyl-6-nitro-2, the 3-glyoxalidine is [2,1-b] _ azoles also

Fusing point: 121.4-125 ℃.

Embodiment 11

(R)-and 2-(4-(4-(N-ethyl-N-(4-Trifluoromethoxyphen-l) amino) piperidines-1-yl) phenoxymethyl)-2-methyl-6-nitro-2, the 3-glyoxalidine is [2,1-b] _ azoles also

Fusing point: 122.5-122.8 ℃.

Embodiment 12

(R)-and 2-(4-(4-(N-ethyl-N-(4-trifluoromethyl)-amino) piperidines-1-yl) phenoxymethyl)-2-methyl-6-nitro-2, the 3-glyoxalidine is [2,1-b] _ azoles also

Fusing point: 105-108.5 ℃.

Embodiment 13

(R)-and 2-(4-(4-(5-chlorobenzene and furans-2-ylmethyl) piperidines-1-yl) phenoxymethyl)-2-methyl-6-nitro-2, the 3-glyoxalidine is [2,1-b] _ azoles also

Fusing point: 210.6-211.6 ℃.

Embodiment 14

(R)-and 2-methyl-6-nitro-2-(2-(4-(4-trifluoro-methoxybenzyl) piperidines-1-yl) benzothiazole-6-base oxygen ylmethyl)-2, the 3-glyoxalidine is [2,1-b] _ azoles also

Fusing point: 203.9-205.2 ℃.

Embodiment 15

2-methyl-6-nitro-2-(4-(4-(4-trifluoro-methoxybenzyl)-piperidines-1-yl) phenoxymethyl)-2, the 3-glyoxalidine is [2,1-b] _ azoles also

Fusing point: 180.9-182.7 ℃.

Embodiment 16

2-(4-(4-(3, the 4-dichloro benzyl) piperidines-1-yl) phenoxymethyl)-2-methyl-6-nitro-2, the 3-glyoxalidine is [2,1-b] _ azoles also

Fusing point: 191.4-192.1 ℃.

Embodiment 17

2-(4-(4-(N-(4-chloro-phenyl-)-N-methylamino) piperidines-1-yl) phenoxymethyl)-2-methyl-6-nitro-2, the 3-glyoxalidine is [2,1-b] _ azoles also

Fusing point: 137.6-141.5 ℃.

Embodiment 18

(R)-and 2-(4-(4-(N-(4-chloro-phenyl-)-N-methylamino) piperidines-1-yl) phenoxymethyl)-2-methyl-6-nitro-2, the 3-glyoxalidine is [2,1-b] _ azoles also, the 4-tosylate.

Fusing point: 212.6-214.1 ℃.

Embodiment 19

(R)-and 2-(4-(4-(N-(4-chloro-phenyl-)-N-methylamino)-piperidines-1-yl) phenoxymethyl)-2-methyl-6-nitro-2, the 3-glyoxalidine is [2,1-b] _ azoles also, mesylate.

Fusing point: 171.2-172.8 ℃.

Embodiment 20

(R)-and 2-(4-(4-(N-(4-chloro-phenyl-)-N-methylamino)-piperidines-1-yl) phenoxymethyl)-2-methyl-6-nitro-2, the 3-glyoxalidine is [2,1-b] _ azoles also, hydrochloride.

Fusing point: 170.0-173.7 ℃.

Embodiment 21

2-methyl-6-nitro-2-(4-(4-(4-trifluoromethoxy benzyloxy-methyl) piperidines-1-yl) phenoxymethyl)-2, the 3-glyoxalidine is [2,1-b] _ azoles also

Fusing point: 153.1-153.7 ℃.

Embodiment 22

(R)-(4-chloro-phenyl-) carboxylamine 1-(4-(2-methyl-6-nitro-2,3-glyoxalidine be [2,1-b] _ azoles-2-ylmethoxy also) phenyl) piperidin-4-yl methyl ester

Fusing point: 211.6-212.3 ℃ (decomposition).

Embodiment 23

2-methyl-6-nitro-2-(4-(4-(4-trifluoromethyl benzyloxy-methyl) piperidines-1-yl) phenoxymethyl)-2, the 3-glyoxalidine is [2,1-b] _ azoles also

Fusing point: 138.7-139.5 ℃.

[table 22]

[table 23]

Embodiment	R1	R2	mp(℃)
Embodiment	R1	R2	mp(℃)	29 30 31 32 33	-H -H -H -H -Cl	-H -OCF ₃ -CF ₃ -Cl -Cl	210.9-213.8 214.3-217.7 217.4-219.7 208.7-211.6 198.9-202.0

[table 24]

Embodiment	R1	R2	R3	mp(℃)
Embodiment	R1	R2	R3	mp(℃)	34 35 36 37 38 39 40 41 42 43 44 45 46 47 48 49 50 51 52 53 54 55	-CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -H -H -H -H -H	-CH ₃ -H -CH ₃ -H -CH ₃ -H -CH ₂CH ₃ -CH ₂CH ₃ 4-CF ₃PhCH ₂- -CH ₂CH ₂OH -CH ₂CH ₂OCH ₃ -C ₃H ₇ -C ₄H ₉ CH ₃OCH ₂CO- -CH ₂-cyclo-C ₃H ₅ -C ₄H ₉ -C ₂H ₅ -CH ₃ -C ₂H ₅ -CH ₃ -H -CH ₃	-Cl -CF ₃ -CF ₃ -OCF ₃ -OCF ₃ -Cl -Cl -CF ₃ -H -CF ₃ -CF ₃ -CF ₃ -Cl -CF ₃ -CF ₃ -CF ₃ -OCF ₃ -OCF ₃ -CF ₃ -CF ₃ -CF ₃ -Cl	173.7-175.1 178.4-181.1dec 135.0-137.5 195.4-197.8dec 158.1-158.8 187.0-189.5 121.4-125.0 105.0-108.5 192.5-195.3 147.3-148.6 89.5-93.4 103.4-107.9 122.1-124.0 124.7-127.0 157.6-160.4 117.8-120.2 122.5-122.8 154.0-157.3dec 172.0-174.2 189.4-190.8 179.2-180.7 203.6-204.5dec

[table 25]

Embodiment	R1	R2	R3	Mp (℃) or ¹H NMR
Embodiment	R1	R2	R3	Mp (℃) or ¹H NMR	56 57 58 59 60 61 62 63 64 65 66 67 68 69 70 71	-H -H -H -H -H -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -COCH ₃ 4-CF ₃OPhCH ₂- -COCH ₃ -CO ₂C ₆H ₅ -CO ₂C ₂H ₅ -C ₂H ₅	-H -H -Cl -H -H -H -H -H -Cl -H -H -H -Cl -H -H -H	-H -Cl -Cl -CF ₃ -OCF ₃ -Cl -OCF ₃ -H -Cl -CF ₃ -Cl -OCF ₃ -Cl -CF ₃ -CF ₃ -CF ₃	215.9-217.2 211.7-213.1 199.5-204.0 213.5-216.5 217.6-218.4 195.4-199.1 204.8-207.0 206.1-208.9 182.1-185.7 199.6-202.0 169.9-117.4 115.4-117.4 ¹H NMR(DMSO)δ1.42-1.87(8H，m)，2.11(3H，brs)， 2.53-2.77(2H，m)，3.52(2H.d，J＝12.4Hz)，4.15(1H，d， J＝11.9Hz)，4.17(2H，s)，4.35(1H，d，J＝10.9Hz)，4.51(2H， brs)，6.63-6.91(4H，m)，7.11-7.28(1H，m)，7.35-7.61(3H， m)，8.01(1H，s). 137.0-140.0 159.9-162.8 132.5-136.7

[table 26]

Embodiment	R1	R2	R3	mp(℃)
Embodiment	R1	R2	R3	mp(℃)	72 73 74 75 76 77 78 79 80 81 82 83 84	-CH ₃-CH ₃-CH ₃-CH ₃-CH ₃-CH ₃-CH ₃-CH ₃-CH ₃-CH ₃-CH ₃-CH ₃-CH ₃	-H -H -C ₂H ₅ -H -H -H -CH ₃ -CH ₃ -CH ₃ -CH ₃ -H -CH ₃ -CH ₃	(CH ₃) ₃COCO- 4-ClPhCH ₂OCO- (CH ₃) ₃COCO- 4-CF ₃Ph(CH ₂) ₂- 4-CF ₃Ph(CH ₂) ₃- 4-CF ₃PhCH＝CHCH ₂- 4-CF ₃Ph(CH ₂) ₂- 4-CF ₃Ph(CH ₂) ₃- 4-CF ₃PhCH＝CHCH ₂- 4-CF ₃OPhCH ₂CH ₂OCO- 4-ClPhCH ₂OCO- 4-ClPhCH ₂OCO- 4-CF ₃PhCH ₂OCO-	250.7-254.0 232.0-237.5 165.0-167.2 161.2-163.5 194.9-196.7 212.3-214.7dec 144.0 172.2-173.0 212.4-214.5dec 205.5-208.0 232.0-237.5dec 201.0-203.7 201.0-203.5

[table 27]

Embodiment	R1	R2	R3	mp(℃)
Embodiment	R1	R2	R3	mp(℃)	85 86 87 88 89	-CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃	-H -H -H -H -Cl	-H -OCF ₃ -CF ₃ -Cl -Cl	209.7-212.4 210.9-212.4 199.5-203.1 207.1-211.2 180.0-181.2

[table 28]

Embodiment	R1	R2	R3	R4	Mp (℃) or ¹H NMR
Embodiment	R1	R2	R3	R4	Mp (℃) or ¹H NMR	90 91 92 93 94 95 96 97 98 99 100 101 102 103 104 105 106 107 108 109 110 111 112 113 114 115 116 117 118 119 120	-CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -H -H -CH ₃ -H -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃	-H -H -H -H -H -H -H -H -H -H -H -H -H -H -CH ₂N(CH ₃) ₂ -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H	-H -H -H -H -OH -H -H -H -H -H -OC ₂H ₅ 4-ClPh- -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H	-OH (CH ₃) ₃COCO- -CO ₂H 4-CF ₃OPhNHCO- -C ₆H ₅ 4-CF ₃OPhCH ₂OCH ₂- 4-CF ₃OPhOCH ₂- -C ₆H ₅ 4-CF ₃OPh(CH ₂) ₂O- 4-CF ₃OPhCH＝CHCH ₂O- -OC ₂H ₅ -OH 4-CF ₃OPhOCH ₂- 4-CF ₃Ph(CH ₂) ₃O- 4-CF ₃OPhO- cyclo-C ₆H ₁₁CH ₂O- 4-ClPhCH ₂OCH ₂- 4-CF ₃PhCH ₂OCH ₂- 4-CF ₃OPhCH ₂OCH ₂- 4-CF ₃OPhCH ₂O- 4-ClPhOCH ₂- 4-CF ₃PhOCH ₂- NH ₂COO- 3，4-Cl2PhNHCOO- 4-CF ₃PhNHCOO- 4-ClPhNHCOO- 4-CF ₃OPhNHCOO- 4-CF ₃OPh(CH ₂) ₂- 4-CF ₃OPh(CH ₂) ₃- 4-ClPhN(CH ₃)COO- 4-ClPhN(C ₂H ₅)COO-	228.0-229.5dec 218.5-219.0dec ¹H NMR(DMSO)δ1.69(3H， s)，2.11(4H，brs)，2.64(1H， brs)，3.48(4H，brs)，4.20(1H， d，J＝11.0Hz)，4.34(2H，s)， 4.37(1H，d，J＝11.0Hz)， 7.03-7.08(2H，m)，7.69(2H， br)，8.16(1H，s)，12.44(1H， br). 251.0-254.7dec 242.7-243.5 185.0-186.1 226.2-226.9dec 263.0-265.1 171.8-174.2 213.7-217.4 153.0-156.8 231.3-231.9 223.2-225.2dec 196.8-200.0 186.6-190.5 238.7-241.0 175.3-175.5 172.3-172.9 140.4-141.7 188.3-189.4 220.2-223.1 175.0-180 208.7-209.9dec 218.5-222.2dec 224.0-226.6dec 236.0-238.7dec 223.0-225.5 239.4-241.3 191.4-193.2 224.6-224.9 181.1-182.6

[table 29]

Embodiment	R1	R2	R3	Mp (℃) or ¹H NMR
Embodiment	R1	R2	R3	Mp (℃) or ¹H NMR	121 122 123 124 125 126	-H -CH ₃ -H -CH ₃ -H -CH ₃	4-ClPh- 4-ClPh- 4-CF ₃OPh- 4-CF ₃OPh- 4-CF ₃Ph- 4-CF ₃Ph-	-C ₂H ₅ -C ₂H ₅ -C ₂H ₅ -C ₂H ₅ -C ₂H ₅ -C ₂H ₅	217.6-219.4dec 229.3-233.0dec 221.8-223.8dec 245.1-247.3dec ¹H NMR(CDCl ₃)δ1.21(3H，t，J＝7.01Hz)， 191-1.98(4H，m)，2.82-2.94(2H，m)，3.37(2H，q， J＝7.01Hz)，3.74-3.89(3H，m)，4.30-4.51(4H，m)， 5.58-5.69(1H，m)，6.74-6.79(2H，m)， 6.90-6.95(2H，m)，6.99-7.04(2H，m)， 7.42-7.52(6H，m). 251.8-253.5dec

[table 30]

[table 31]

[table 32]

Embodiment	R1	R2	R3	Mp (℃) or ¹H NMR
Embodiment	R1	R2	R3	Mp (℃) or ¹H NMR	136 137 138 139 140 141 142 143 144 145 146 147 148 149 150 151 152 153 154 155 156 157 158 159 160	-CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃	-CH ₃-CH ₃-CH ₃-CH ₃-CH ₃-CH ₃-CH ₃-H -C ₂H ₅-CH ₃-CH ₃-H -H -H -CH ₃-H -H -H -H -H -H -H -H -CH ₃-CH ₃	4-CF ₃Ph- 4-CF ₃OPhCH ₂- 4-ClPhCH ₂- 4-CF ₃PhCH ₂- 4-CF ₃OPhCH ₂OCO- 4-ClPhCH ₂OCO- 4-CF ₃PhCH ₂OCO- 4-CF ₃PhCH＝CHCH ₂- 4-CF ₃OPh- 4-CF ₃OPh- 4-ClPh- 4-CF ₃OPh- 4-ClPh- 4-CF ₃OPhO(CH ₂) ₂- (CH ₃) ₃COCO- 4-CF ₃OPhCH ₂- 4-ClPhCH ₂- 4-CF ₃PhCH ₂- 4-ClPhCH ₂OCO- 4-CF ₃OPhCH ₂OCO- 4-CF ₃PhCH ₂OCO- 4-CF ₃Ph- (CH ₃) ₃COCO- 4-CF ₃OPhCO- 4-CF ₃OPhNHCO-	167.8-168.7 154.8-155.9 149.6-153.4 145.0-146.9 141.8-144.3 132.4-135.0 152.2-155.6 160.5-163.7 125.2-128.1 137.9-139.2 190.8-193.8 145.6-149.3 163.3-167.3 140.9-143.1 153.6-154.7 181.7-183.6 183.7-186.6 173.0-176.3 125.2-127.6 120.5-124.9 103.5-107.3 ¹H NMR(CDCl ₃)δ1.46-1.62(2H，m)，1.76(3H，s)， 2.08-2.21(2H，m)，2.90-3.05(2H，m)，3.35-3.47(1H，m)， 3.70-3.83(2H，m)，3.98-4.06(2H，m)，4.16(1H，d， J＝10.20Hz)，4.50(1H，d，J＝10.20Hz)，6.53-6.65(2H，m)， 6.69-6.77(2H，m)，6.89-6.98(2H，m)，7.43-7.51(2H，m)， 7.55(1H，s) ¹H NMR(CDCl ₃)δ1.20-1.37(2H，m)，1.46(9H，s)， 1.76(3H，s)，1.94-2.07(2H，brm)，2.77-3.01(2H，brm)， 3.23-3.41(2H，brm)，3.94--4.11(4H，m)，4.14(1H，d， J＝10.19Hz)，4.49(1H，d，J＝10.15Hz)，6.50-6.59(2H，m)， 6.67-6.76(2H，m)，7.55(1H，s) 129.2-132.0 179.0-182.5

[table 33]

[table 34]

Embodiment	R1	R2	R3	Mp (℃) or ¹H NMR
Embodiment	R1	R2	R3	Mp (℃) or ¹H NMR	166 167 168 169 170	-CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃	4-CF ₃OPh- 4-CF ₃OPhCH ₂OCO- 4-CF ₃OPhCH ₂- 4-CF ₃OPhCO- 4-CF ₃OPhNHCO-	-CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃	¹H NMR(CDCl ₃)δ1.62-1.73(2H，m)，1.73-1.87(5H，m)， 1.96-2.12(2H，m)，2.77(3H，s)，2.88-3.03(2H，m)， 3.38-3.60(3H，m)，4.00-4.13(2H，m)，4.23(1H，d，J＝10.1Hz)， 4.50(1H，d，J＝10.2Hz)，6.67-6.74(2H，m)，6.76-6.84(2H，m)， 7.02-7.10(2H，m)，7.18-7.25(2H，m)，7.56(1H，s) 190.9-192.2 143.1-145.7 178.8-183.7 ¹H NMR(CDCl ₃)δ1.74-1.87(5H，m)，2.50-2.68(2H，m)， 2.68-2.83(2H，m)，2.97(3H，s)，3.42-3.56(2H，m)， 3.97-4.17(4H，m)，4.29(1H，d，J＝10.3Hz)，4.50(1H，d， J＝10.2Hz)，4.55-4.66(1H，m)，6.46-6.55(1H，br)， 6.84-6.93(2H，m)，7.10-7.18(2H，m)，7.37-7.44(2H，m)， 7.49-7.57(2H，m)，7.58(1H，s)

[table 35]

[table 36]

[table 37]

[table 38]

[table 39]

Embodiment	R1	R2	R3	R4	R5	R6	R7	MS(M+1)
Embodiment	R1	R2	R3	R4	R5	R6	R7	MS(M+1)	202 203 204 205 206 207 208 209 210 211 212 213 214 215 216 217 218 219 220 221 222 223 224 225 226 227 228 229 230 231 232 233 234 235 236 237 238	-CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃	-H -CH ₃ -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -CH ₃ -CH ₃ -CH ₃ -CH ₃	-H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -CH ₃ -H -H -F -H -H -H -H -H -H -H	-H -H -H -H -CF ₃ -H -H -H -H -H -H -OCH ₃ -H -H -H -H -H -H -H -H -H -H -H -H -Cl -H -H -H -H -F -H -H -H -H -H -H -H	-Cl -Cl -Cl -OCF ₃ -H -C ₄H ₉ -H -OCH ₃ -H -H -CH ₃ -OCH ₃ -H -F -N(CH ₃) ₂ -OC ₂H ₅ -C ₂H ₅ -H -H -H -Cl -OC ₆H ₅ -H -Cl -H -Cl -CH ₃ -OCH ₃ -CF ₃ -F -NO ₂ -CN -SCH ₃ -Cl -OCF ₃ -C ₄H ₉ -H	-H -H -Cl -H -CF ₃ -H -H -H -H -Cl -H -OCH ₃ -OCF ₃ -H -H -H -H -CO ₂C ₂H ₅ -H -H -H -H -Cl -H -Cl -Cl -H -Cl -H -F -H -H -H -Cl -H -H -H	-H -H -H -H -H -H -H -H -Cl -H -H -H -H -H -H -H -H -H -OCF ₃ -OCHF ₂ -OCF ₃ -H -Cl -Cl -H -Cl -CH ₃ -H -Cl -F -H -H -H -H -H -H -H	484 498 518 534 586 506 450 480 484 484 464 540 534 468 493 494 478 522 534 516 568 542 518 518 518 552 492 514 552 540 495 475 496 532 548 520 464

[table 40]

Embodiment	R1	R2	R3	R4	R5	R6	R7	MS(M+1)
Embodiment	R1	R2	R3	R4	R5	R6	R7	MS(M+1)	239 240 241 242 243 244 245 246 247 248 249 250 251 252 253 254 255 256 257 258 259	-CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃	-CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃	-H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H	-H -H -H -OCH ₃ -H -H -H -H -H -H -H -H -H -H -H -H -H -Cl -H -H -H	-H -H -CH ₃ -OCH ₃ -H -F -N(CH ₃) ₂ -OC ₂H ₅ -C ₂H ₅ -NHCOCH ₃ -H -H -H -Cl -OC ₆H ₅ -H -Cl -H -Cl -OCH ₃ -SCH ₃	-H -Cl -H -OCH ₃ -OCF ₃ -H -H -H -H -H -CO ₂C ₂H ₅ -H -H -H -H -Cl -H -Cl -Cl -Cl -H	-Cl -H -H -H -H -H -H -H -H -H -H -OCF ₃ -OCHF ₂ -OCF ₃ -H -Cl -Cl -H -Cl -H -H	498 498 478 554 548 482 507 508 492 521 536 548 530 582 556 532 532 532 566 528 510

[table 41]

Embodiment	R1	R2	R3	MS(M+1)
Embodiment	R1	R2	R3	MS(M+1)	260 261 262 263 264 265 266 267 268 269 270 271 272 273 274 275	-CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃	4-ClPhCH ₂- -CH ₂C ₆H ₅ 2-ClPhCH ₂- 3-ClPhCH ₂- 4-CH ₃PhCH ₂- 3，4，5-(CH ₃O) ₃PhCH ₂- -CH ₂C ₆H ₅ 4-CH ₃OPhCH ₂- 4-ClPhCH ₂- 4-FPhCH ₂- 3，4-(CH ₃O) ₂PhCH ₂- -CH ₂CH ₂OCH ₃ (C ₂H ₅) ₂N(CH ₂) ₂- -cyclo-C ₈H ₁₅ 4-ClPh(CH ₂) ₂- -CH ₂-cyclo-C ₆H ₁₁	-H -H -H -H -CH ₃ -CH ₃ -CH ₂CH ₂N(CH ₃) ₂ -H -CH ₃ -H -H -CH ₂CH ₂OCH ₃ -C ₂H ₅ -H -H -H	498 464 498 498 492 568 535 494 512 482 524 490 501 484 512 470

[table 42]

[table 43]

[table 44]

[table 45]

[table 46]

[table 47]

[table 48]

Embodiment	R1	R2	R3	Mp (℃) or ¹H NMR
Embodiment	R1	R2	R3	Mp (℃) or ¹H NMR	303 304 305 306 307 308 309 310 311 312 313 314 315 316 317 318 319 320 321	-CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃	4-CF ₃OPh- 4-CF ₃OPh- 4-CF ₃OPh- 4-ClPh- 4-CF ₃Ph- 4-CF ₃OPhCH ₂- 4-CF ₃OPh- 4-ClPh- 4-CF ₃Ph- 4-CF ₃OPhCH ₂- 4-CF ₃OPhCH ₂- 4-ClPhCH ₂- 4-CF ₃PhCH ₂- 4-CF ₃OPhCH ₂- 4-ClPhCH ₂- 4-CF ₃PhCH ₂- 4-CF ₃OPhCH ₂- 4-ClPhCH ₂- 4-CF ₃PhCH ₂-	-COCH ₃ -C ₂H ₅ -CH ₃ -CH ₃ -CH ₃ -COCH ₃ -H -H -H -C ₂H ₅ -CH ₃ -CH ₃ -CH ₃ -H -H -H (CH ₃) ₃COCO- (CH ₃) ₃COCO- (CH ₃) ₃COCO-	148.6-149.1 116.8-119.2 135.6-140.9 141.6-146.1 151.4-155.0 ¹H NMR(CDCl ₃)δ1.29-1.51(2H.brm)， 1.67-1.89(6H，brm)，2.13(1.5H，s)，2.20(1.5H，s)， 2.46-2.72(2H，brm)，3.12-3.23(1H，brm)， 3.27-3.36(1H，brm)，3.44-3.63(2H，brm)， 3.96-4.10(2H，brm)，4.10-4.26(1H，brm)，4.49(1H.d， J＝10.15Hz)，4.58(1H，s)，4.63(1H，s)，6.63-6.99(4H， brm)，7.12-7.30(4H，m)，7.56(1H，s) 181.9-182.5 177.6-179.1 164.7-165.8 163.9-165.2 180.5-180.8 169.5-170.6 166.7-167.5 163.9-167.6 163.8-166.3 157.0-160.8 ¹H NMR(CDCl ₃)δ1.29-1.56(11H，brm)， 1.60-1.84(6H，m)，2.46-2.66(2H，brm)，3.00-3.24(2H， brm)，3.44-3.57(2H，brm)，3.97-4.08(2H，m)，4.17(1H， d，.J＝10.12Hz)，4.35-4.55(3H，m)，6.70-6.80(2H，m)， 6.81-6.95(2H，m)，7.12-7.20(2H，m)，7.20-7.32(2H，m)， 7.50(1H，s) ¹H NMR(CDCl ₃)δ1.29-1.54(11H，brm)， 1.60-1.84(6H，m)，2.48-2.66(2H，brm)，3.00-3.22(2H， brm)，3.51(2H，d，J＝12.07Hz)，3.96-4.08(2H， m)4.17(1H，d，J＝10.10Hz)，4.34-4.46(2H，brm)， 4.49(1H，d，J＝10.10Hz)，6.76(2H，d，J＝8.97Hz)， 6.81-6.93(2H，brm)，7.07-7.21(2H，brm)，7.29(2H，d， J＝8.29Hz)，7.55(1H，s) ¹H NMR(CDCl ₃)δ1.31-1.57(11H，brm)， 1.61-1.88(6H，m)，2.45-2.72(2H，brm)，3.03-3.28(2H， brm)，3.52(2H，d，J＝12.05Hz)，3.96-4.08(2H，m)， 4.17(1H，d，J＝10.15Hz)，4.41-4.51(3H，m)，6.76(2H，d， J＝8.95Hz)，6.83-6.96(2H，brm)，7.26-7.42(2H，brm)， 7.55(1H，s)，7.59(2H，d，J＝7.95Hz)

[table 49]

Embodiment	R1	R2	R3	R4	R5	R6	MS(M+1)
Embodiment	R1	R2	R3	R4	R5	R6	MS(M+1)	322 323 324 325 326 327 328 329 330 331 332 333 334 335 336 337 338 339 340 341 342 343 344 345 346 347 348 349 350 351 352 353	-CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃	-H -H -H -H -H -H -H -H -H -Cl -H -H -H -H -H -H -H -H -Cl -Cl -H -H -H -H -H -H -H -H -H -H -H -H	-H -H -H -H -H -H -H -H -H -H -Cl -H -H -H -H -H -Cl -Cl -H -H -H -H -H -H -H -H -H -H -H -H -H -H	-H -H -H -H -F -Cl -CH ₃ -C(CH ₃) ₃ -H -H -H -SCH ₃ -COC ₆H ₅ -F -H -Cl -H -H -Cl -Cl -OCH ₃ -H -Cl -Cl -H -CN -H -H -OCOCH ₃ -NO ₂ -N(CH ₃) ₂ -H	-H -CH ₃ -H -OCF ₃ -H -CF ₃ -H -H -H -H -Cl -H -H -CF ₃ -CF ₃ -H -H -Cl -Cl -H -H -H -Cl -H -Cl -H -CN -Cl -OCH ₃ -H -H -H	-CH ₃ -H -OCF ₃ -H -CH ₃ -H -H -H -CF ₃ -Cl -H -H -H -H -F -Cl -Cl -Cl -H -Cl -H -NO ₂ -H -H -H -H -H -Cl -H -H -H -OH	490 490 560 560 508 578 490 532 544 544 544 522 580 562 562 544 544 578 578 578 506 521 544 510 510 501 501 544 564 521 519 492

[table 50]

Embodiment	R1	R2	R3	R4	R5	R6	MS(M+1)
Embodiment	R1	R2	R3	R4	R5	R6	MS(M+1)	354 355 356 357 358 359 360 361 362	-CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃	-H -H -H -H -H -H -H -H -H	-OCH ₃ -H -H -H -H -H -H -H -H	-OH -OH -C ₂H ₅ -C ₆H ₁₃ -OCH ₂C ₆H ₅ -OC ₆H ₅ -CH(CH ₃) ₂ -OC ₆H ₁₃ -OCF ₃	-OCH ₃ -OCH ₃ -H -H -H -H -H -H -H	-H -H -H -H -H -H -H -H -H	552 522 504 560 582 568 518 576 560

[table 51]

[table 52]

[table 53]

[table 54]

Embodiment	R1	R2	R3	R4	R5	R6	R7	mp(℃)
Embodiment	R1	R2	R3	R4	R5	R6	R7	mp(℃)	382 383 384 385 386 387 388 389 390	-CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃	-H -CH ₃ -H -CH ₃ -H -CH ₃ -H -CH ₃ -H	-H -H -H -H -H -H -H -H -H	-Cl -Cl -H -H -H -H -H -H -Cl	-H -H -C ₃H ₇ -C ₃H ₇ -F -F 4-CF ₃OPhO- 4-CF ₃OPhO- -Cl	-Cl -Cl -H -H -H -H -H -H -H	-H -H -H -H -H -H -H -H -H	122-124 166.5-167 222-223 198-199 180.2-182.8 175.7-177.4 167.4-170.2 167.4-170.2

[table 55]

Embodiment	R1	R2	R3	R4	R5	R6	R7	mp(℃)
Embodiment	R1	R2	R3	R4	R5	R6	R7	mp(℃)	391 392 393 394 395 396 397	-CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -H	-CH ₂CH ₂OH -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃	-H -F -CF ₃ -Cl -Cl -H -H	-H -H -H -Cl -H -CF ₃ -H	-CF ₃ -CF ₃ -H -H -Cl -H -CF ₃	-H -H -H -H -H -CF ₃ -H	-H -H -H -H -H -H -H	114.5-117.3 197.5-199.2 189.6-190.2 176.9-178.2 181.6-182.4 193.8-195.3 167.7-169.0

[table 56]

Embodiment	R1	R2	R3	R4	R5	R6	R7	MS(M+1)
Embodiment	R1	R2	R3	R4	R5	R6	R7	MS(M+1)	398 399 400 401 402 403 404 405 406 407 408 409 410 411 412 413	-CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃	-CH ₂CH ₂CN -C ₂H ₅ -C ₂H ₅ -C ₂H ₅ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃	-H -Cl -H -H -H -H -H -H -H -H -H -H -H -H -H -H	-H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H	-H -H -CH(CH ₃) ₂ -C ₆H ₅ -C ₂H ₅ -OC ₆H ₅ -OCH ₂C ₆H ₅ -OC ₈H ₁₇ -N(CH ₃) ₂ -C ₄H ₉ -CH ₂CH(CH ₃) ₂ -N(C _eH ₅) ₂ -OCH(CH ₃) ₂ -OC(CH ₃) ₃ -O(CH ₂) ₃N(CH ₃) ₂ N(C ₄H ₉) ₂	-H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H	-H -Cl -H -H -H -H -H -H -H -H -H -H -H -H -H -H	517 560 534 568 506 570 584 606 521 534 534 645 536 550 579 605

[table 57]

[table 58]

[table 59]

[table 60]

Embodiment	R1	R2	R3	R4	R5	R6	mp(℃)
Embodiment	R1	R2	R3	R4	R5	R6	mp(℃)	439 440 441 442 443	-H -CH ₃ -H -CH ₃ -H	-H -H -H -OCF ₃ -H	-H -OCF ₃ -OCF ₃ -H -H	-OCF ₃ -H -H -H -H	-H -H -H -H -H	-H -H -H -H -OCF ₃	160.5-164.0 187.4-189.8 153.7-156.3 205.8-208.5 155.9-159.0

[table 61]

Embodiment	R1	R2	R3	mp(℃)
Embodiment	R1	R2	R3	mp(℃)	444 445 446 447 448 449 450 451 452 453 454 455 456 457 458 459 460 461 462 463 464 465	-CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃	4-CF ₃OPh- 4-CF ₃OPh- 4-CF ₃OPh- 4-ClPh- 4-CF ₃Ph- 4-CF ₃OPhCH ₂- 4-CF ₃OPh- 4-ClPh- 4-CF ₃Ph- 4-CF ₃OPhCH ₂- 4-CF ₃OPhCH ₂- 4-ClPhCH ₂- 4-CF ₃PhCH ₂- 4-CF ₃OPhCH ₂- 4-ClPhCH ₂- 4-CF ₃PhCH ₂- 4-CF ₃OPhCH ₂- 4-ClPhCH ₂- 4-CF ₃PhCH ₂- 4-CF ₃OPhCH ₂OCO 4-CF ₃OPhCO- 4-CF ₃OPhNHCO-	-COCH ₃ -C ₂H ₅ -CH ₃ -CH ₃ -CH ₃ -COCH ₃ -H -H -H -C ₂H ₅ -CH ₃ -CH ₃ -CH ₃ -H -H -H (CH ₃) ₃COCO- (CH ₃) ₃COCO- (CH ₃) ₃COCO- -CH ₃ -CH ₃ -CH ₃	148.6-149.1 116.8-119.2 135.6-140.9 141.6-146.1 151.4-155.0 181.9-182.5 177.6-179.1 164.7-165.8 163.9-165.2 180.5-180.8 169.5-170.6 166.7-167.5 163.9-167.6 163.8-166.3 157.0-160.8

[table 62]

Embodiment	R1	R2	R3	mp(℃)
Embodiment	R1	R2	R3	mp(℃)	466 467 468 469 470	-CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃	-CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃	(CH ₃) ₃COCO- 4-CF ₃OPhCO- 4-CF ₃OPhNHCO- 4-CF ₃OPhCH ₂OCO- 4-CF ₃OPhCH ₂-	159.8-161.0 154.3-155.6 146.7-149.3 139.7-140.6 154.7-157.0

[table 63]

Embodiment	R1	R2	R3	R4	R5	R6	MS(M+1)
Embodiment	R1	R2	R3	R4	R5	R6	MS(M+1)	471 472 473 474 475 476 477 478 479 480 481 482 483 484 485 486 487 488 489 490 491 492 493 494 495 496 497	-CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃	-Cl -H -H -H -H -H -OCF ₃ -H -H -H -H -H -H -CF ₃ -H -H -H -Cl -H -Cl -H -Cl -H -H -H -H -H	-H -H -CF ₃ -H -H -H -H -CH ₃-H -Cl -H -OCH ₃-Cl -H -OC ₆H ₅-H -OCF ₃-H -Cl -Cl -CH ₃ -H -H -H -H -H -H	-H -CH(CH ₃) ₂ -H -C(CH ₃) ₃ -CN -C ₆H ₅ -H -H -OCF ₃ -H -F -H -Cl -H -H -SCH ₃ -H -F -H -H -H -H -C ₂H ₅ -Cl -CF ₃ -CH ₃ -H	-H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -Cl -H -CH ₃ -Cl -H -H -H -H -H	-H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H	513 521 547 535 504 555 563 493 563 513 497 509 547 547 571 525 563 531 547 547 507 547 507 513 547 493 479

[table 64]

Embodiment	R1	R2	R3	R4	R5	R6	mp(℃)
Embodiment	R1	R2	R3	R4	R5	R6	mp(℃)	498	-H	-H	-H	-CF ₃	-H	-H	126.8-129.0

[table 65]

Embodiment	R1	R2	R3	R4	R5	R6	MS(M+1)
Embodiment	R1	R2	R3	R4	R5	R6	MS(M+1)	499 500 501 502 503 504 505 506 507 508 509 510 511 512 513 514 515 516 517 518 519 520 521 522 523 524 525 526 527 528 529 530	-CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃	-H -H -H -H -H -H -H -H -CH ₃ -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H	-H -H -H -H -H -H -Cl -H -H -H -H -H -H -H -H -H -H -H -H -H -CH ₃ -H -H -H -H -H -CH＝CHCH ₃(cis) -H -H -H -H -H	-OCH ₃ -OCH ₃ -H -H -H -Cl -Cl -CH ₃ -CH ₃ -F -CO ₂C ₂H ₅ -CN -H -H -CF ₃ -OCF ₃ -H -CH ₃ -OCH ₃ -Br -H -C ₃H ₇ -Cl -NO ₂ -CH ₂CH＝CH ₂ -H -H -CH(CH ₃) ₂ -CH ₂CH ₂COCH ₃ -H -CH ₂CO ₂CH ₃ -OCH ₃	-H -OCH ₃ -H -H -Cl -H -H -H -H -H -H -H -H -CF ₃ -H -H -H -H -H -H -H -H -F -H -H -N(C ₂H ₅) ₂ -H -H -H -NHC ₆H ₅ -H -H	-H -H -H -Cl -H -H -H -H -H -H -H -H -CF ₃ -H -H -H -OCH(CH ₃) ₂ -CO ₂C ₂H ₅ -CO ₂CH ₃ -F -F -H -H -F -OCH ₃ -H -OC ₂H ₅ -H -H -H -H -Cl	495 525 465 499 499 499 533 479 493 483 537 490 533 533 533 549 523 551 553 561 497 507 517 528 535 536 549 507 535 556 537 529

[table 66]

Embodiment	R1	R2	R3	R4	R5	R6	MS(M+1)
Embodiment	R1	R2	R3	R4	R5	R6	MS(M+1)	531 532 533 534 535 536 537 538 539 540 541 542 543 544 545 546 547 548	-CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃	-H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H	-H -H -H -H -CH ₃ -H -OCH ₃ -H -H -H -H -H -H -H -H -H -H -H	-H -COC ₂H ₅ -COCH ₃ -NHCOCH ₃ -CH ₃ -H -H -SCH ₃ -H -1-PYRRYL -C ₆H ₅ -OCH ₂C ₆H ₅ -CH ₂C ₆H ₅ -cyclo-C ₆H ₁₁ -OC ₈H ₁₇ -cyclo-C ₅H ₉ -H -C ₆H ₁₃	-CO ₂CH ₃ -H -H -H -CH ₃ -H -H -H -H -H -H -H -H -H -H -H -OC ₆H ₅ -H	-H -H -CH ₃ -H -H -CH ₂C ₆H ₅ -CO ₂CH ₃ -H -2-BENZTHIAZOLYL -H -H -H -H -H -H -H -H -H	523 521 521 522 507 555 553 511 598 530 541 571 555 547 593 533 557 549

[table 67]

Embodiment	R1	R2	R3	R4	R5	R6	mp(℃)
Embodiment	R1	R2	R3	R4	R5	R6	mp(℃)	549 550	-H -H	-H -H	-H -H	-Cl -CF ₃	-H -H	-H -H	198.6-202.5 197.0-200.9

[table 68]

[table 69]

Embodiment	R1	R2	R3	R4	R5	R6	R7	MS(M+1)
Embodiment	R1	R2	R3	R4	R5	R6	R7	MS(M+1)	557 558 559 560 561 562 563 564 565 566 567 568 569 570 571 572 573 574 575 576 577 578 579 580 581 582 583 584 585 586 587 588 589 590 591	-CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃	-H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H	-H -Cl -H -H -OCH ₃ -H -H -H -H -H -H -CH ₃ -H -H -F -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H	-H -H -H -H -H -H -H -Cl -CF ₃-H -H -H -CH ₃-H -H -F -H -H -H -CF ₃-H -H -H -H -H -H -H -H -H -H -H -H -H -H -H	-H -H -H -Cl -H -H -Cl -H -H -CF ₃ -OCF ₃ -H -H -CH ₃ -H -H -F -Cl -CN -H -Cl -OC ₆H ₅ -OC ₂H ₅ -SCH ₃ -COCH ₃ -CH(CH ₃) ₂ -C ₄H ₉ -Cl -OC ₄H ₉ -C ₆H ₅ -C(CH ₃) ₃ -OC ₇H ₁₅ -OCHF ₂ -CH ₂C ₆H ₅ -C ₈H ₁₇	-H -H -Cl -H -H -OCH ₃ -Cl -Cl -H -H -H -H -H -H -H -H -H -H -H -CF ₃ -CF ₃ -H -H -H -H -H -H -H -H -H -H -H -H -H -H	-H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -Cl -H -H -H -H -H -H -H -H -H -CH ₃ -H -H -H -H -H -H -H	508 542 542 542 538 538 576 576 576 576 592 522 522 522 526 526 526 576 533 644 610 600 552 554 550 550 564 556 580 584 564 622 574 598 620

[table 70]

[table 71]

[table 72]

[table 73]

[table 74]

[table 75]

[table 76]

Embodiment	R1	R2	mp(℃)
Embodiment	R1	R2	mp(℃)	646 647 648 649 650 651 652 653 654 655 656 657 658 659	-CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -H -H -CH ₃ -CH ₃ -H -H	4-CF ₃OPhCH ₂- 4-CF ₃PhCH ₂- 4-ClPhCH ₂- 4-ClPhNHCO- 4-ClPhN(CH ₃)CO- 4-ClPhN(C ₂H ₅)CO- 4-CF ₃PhNHCO- 4-CF ₃OPhNHCO- 4-CF ₃PhNHCO- 4-CF ₃OPhNHCO- 4-CF ₃PhN(CH ₃)CO- 4-CF ₃OPhN(CH ₃)CO- 4-CF ₃PhN(CH ₃)CO- 4-CF ₃OPhN(CH ₃)CO-	204.8-206.7 198.0-199.2 197.6-198.2 212.7-213.3 189.4-191.6 168.6-171.6 216.2-217.1dec 218.3-218.5dec 179.9-180.7 187.6-189.8 195.8-199.1 181.0-184.2 148.7-151.8 150.1-152.6

[table 77]

[table 78]

[table 79]

[table 80]

[table 81]

Embodiment	R1	R2	mp(℃)
Embodiment	R1	R2	mp(℃)	691 692 693 694 695 696 697 698 699 700 701 702 703	-CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -H -H -H -H	(CH ₃) ₃COCO- -H 4-CF ₃OPhCH ₂- 4-ClPhCH ₂- 4-CF ₃PhCH ₂- 4-CF ₃PhCH＝CHCH ₂- 4-CF ₃OPhCO- 3，4-Cl ₂PhCH ₂- 4-FPhCH ₂- (CH ₃) ₃COCO- 4-CF ₃OPhCH ₂- 4-CF ₃PhCH ₂- 4-ClPhCH ₂-	261.0-266.3dec 238.2～240.3dec. 247.8～248.5dec. 247.7-248.4dec 221.0-226.0 248.0-252.0 222.6-225.1dec. 247.7-249.5 250dec 200dec 200dec 200dec

[table 82]

[table 83]

Embodiment	R1	R2	mp(℃)
Embodiment	R1	R2	mp(℃)	716 717 718 719 720 721 722 723 724 725 726 727 728 729 730 731 732 733 734	-CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃	(CH ₃) ₃COCO- 4-ClPhCH ₂- 4-CF ₃PhCH ₂- 4-CF ₃OPhCH ₂- 4-CF ₃Ph- 4-CF ₃OPh- 4-ClPh- 4-CF ₃OPhCH ₂OCO- 4-CF ₃PhCH ₂OCO- 4-ClPhCH ₂OCO- 4-ClPhNHCO- 4-CF ₃OPhNHCO- 4-CF ₃PhNHCO- 4-CF ₃PhCH＝CHCH ₂- 4-CF ₃Ph(CH ₂) ₂- 4-CF ₃Ph(CH ₂) ₃- 4-ClPhCO- 4-CF ₃PhCO- 4-CF ₃OPhCO-	150.3-153.9 136.5-138.4 150.6-153.5 156.6-158.1 134.0-137.9 149.7-151.2 90.2-93.0 86.7-89.0 109.0-112.3 199.0-203.6 208.5-212.0 149.5-154.0 (dihydrochloride)

[table 84]

[table 85]

[table 86]

[table 87]

[table 88]

[table 89]

[table 90]

[table 91]

[table 92]

[table 93]

[table 94]

Embodiment	R1	R2	R3	mp(℃)
Embodiment	R1	R2	R3	mp(℃)	809 810	-CH ₃ -H	-H -H	4-CF ₃OPh- 4-CF ₃OPh-	182.0-184.2 143.9-146.7

[table 95]

Embodiment	R1	R2	mp(℃)
Embodiment	R1	R2	mp(℃)	811	-CH ₃	4-CF ₃Ph-	226.0-227.6

[table 96]

Embodiment	R1	R2	mp(℃)
Embodiment	R1	R2	mp(℃)	812 813	-CH ₃ -H	4-CF ₃OPh- 4-CF ₃OPh-	209.0-212.0 208.0-210.9

[table 97]

Embodiment	R1	R2	mp(℃)
Embodiment	R1	R2	mp(℃)	814 815 816 817 818 819 820 821 822 823 824 825 826 827 828 829 830 831	-CH ₃-H -CH ₃-H -CH ₃-H -CH ₃-H -CH ₃-H -CH ₃-H -CH ₃-H -CH ₃-H -CH ₃-H	-C ₆H ₅ -C ₆H ₅ 4-FPh- 4-FPh- 4-ClPh- 4-ClPh- 4-CF ₃Ph- 4-CF ₃Ph- 4-CF ₃OPh- 4-CF ₃OPh- 3，4-Cl ₂Ph- 3，4-Cl ₂Ph- -NHC6H5 -NHC6H5 4-ClPhCH ₂- 4-ClPhCH ₂- 4-CF ₃OPhCH ₂- 4-CF ₃OPhCH ₂-	195.0-196.5 232dec 209.0-209.5 228.0-231.0 213.0-216.0 243.0-246.0dec 208.0-209.0 208.0-211.0 203.0-204.9 218.0-219.4 220.0-221.0 210.5-212.0 196-197.5

[table 98]

[table 99]

[table 100]

Embodiment	R1	R2	mp(℃)
Embodiment	R1	R2	mp(℃)	852 853 854 855 856 857 858 859 860 861 862 863 864 865	-CH ₃ -H -CH ₃ -H -CH ₃ -H -CH ₃ -H -CH ₃ -H -CH ₃ -H -CH ₃ -H	-C ₆H ₅ -C ₆H ₅ 4-ClPh- 4-ClPh- 4-FPh- 4-FPh- 4-CF ₃Ph- 4-Cf ₃Ph- 4-CF ₃OPh- 4-CF ₃OPh- 3，4-Cl ₂Ph- 3，4-Cl ₂Ph- 4-CF ₃OPhOCH ₂- 4-CF ₃OPhOCH ₂-	182.0-183.0 257.0-259.0 202.3-205.2 231.0-233.5dec 230.5-233.0 215.0-217.5 229.0-232.0 179.0-182.0 274.0-176.0 185-188 206-208.5 190-193 201.3-202.2 191.5-194.5

[table 101]

[table 102]

[table 103]

Embodiment	R1	R2	mp(℃)
Embodiment	R1	R2	mp(℃)	871 872 873 874	-CH ₃ -CH ₃ -H -H	-C ₆H ₅ 4-ClPh- -C ₆H ₅ 4-ClPh-	249.3-250.0 257.8-258.2 249.2-252.1dec

[table 104]

[table 105]

Embodiment	R1	R2	mp(℃)
Embodiment	R1	R2	mp(℃)	876 877 878 879	-CH ₃ -CH ₃ -H -H	-C ₆H ₅ 4-ClPh- -C ₆H ₅ 4-ClPh-	221.2-222.1 229.8-232.1 246.2-247.0 260.4-260.9

[table 106]

Embodiment	R1	R2	R3	mp(℃)
Embodiment	R1	R2	R3	mp(℃)	880 881 882 883 884 885 886 887	-CH ₃ -CH ₃ -H -H -CH ₃ -CH ₃ -H -H	-H -H -H -H -CH ₃ -CH ₃ -CH ₃ -CH ₃	-C ₆H ₅ 4-ClPh- -C ₆H ₅ 4-ClPh- -C ₆H ₅ 4-ClPh- -C ₆H ₅ 4-ClPh-	144.0-146.3 191.0-193.9dec 161.0-165.0dec 121.0-126.1dec 215.0-217.5dec 218.0-219.1dec 183.0-186.6dec

[table 107]

Embodiment	R1	R2	mp(℃)
Embodiment	R1	R2	mp(℃)	888 889	-CH ₃-CH ₃	4-ClPhCH ₂- 4-CF ₃OphCH ₂-	180.9-183.1 151.1-154.1

[table 108]

[table 109]

Embodiment	R1	R2	mp(℃)
Embodiment	R1	R2	mp(℃)	900 901 902 903	-CH ₃ -CH ₃ -CH ₃ -CH ₃	4-ClPh- 4-CF ₃OPh- 4-ClPhCH ₂- 4-CF ₃OPhCH ₂-	238-239 199-200 199-200 172-173

[table 110]

Embodiment	R1	R2	mp(℃)
Embodiment	R1	R2	mp(℃)	904 905	-CH ₃-CH ₃	4-ClPh- 4-CF ₃OPh-	175.5-176.5 122.5-124dec

[table 111]

[table 112]

Embodiment	R1	R2	R3	R4	R5	R6	MS(M+1)
Embodiment	R1	R2	R3	R4	R5	R6	MS(M+1)	918 919 920 921 922 923	-CH ₃-CH ₃-CH ₃-CH ₃-CH ₃-CH ₃	-H -H -H -C ₆H ₅-H -H	-H -H -H -H -H -H	-C ₆H ₅ (CH ₃) ₃COCO- -CO ₂C ₂H ₅ -H -OH 4-ClPhO-	-H -H -H -H	-H -H -H -H	526 522 526 576

[table 113]

[table 114]

[table 115]

Embodiment	R1	R2	R3	R4	R5	R6	MS(M+1)
Embodiment	R1	R2	R3	R4	R5	R6	MS(M+1)	942 943 944 945 946	-CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃	-H -H -H -H -H	-H -H -H -H -H	-OCH ₂C ₆H ₅ -cyclo-C ₆H ₁₁ -OC ₈H ₁₇ -cyclo-C ₅H ₉ -H	-H -H -H -H -OC ₆H ₅	-H -H -H -H -H	571 547 593 533 557

[table 116]

Embodiment	R1	R2	R3	R4	R5	R6	MS(M+1)
Embodiment	R1	R2	R3	R4	R5	R6	MS(M+1)	947 948 949 950 951 952 953 954 955 956 957 958 959 960 961 962 963 964 965 966 967 968 969 970 971 972 973 974	-CH ₃-CH ₃-CH ₃-CH ₃-CH ₃-CH ₃ -CH ₃-CH ₃-CH ₃-CH ₃-CH ₃-CH ₃-CH ₃-CH ₃-CH ₃-CH ₃-CH ₃-CH ₃-CH ₃ -CH ₃-CH ₃-CH ₃-CH ₃-CH ₃-CH ₃-CH ₃-CH ₃-CH ₃	-H -Cl -H -H -H -H -H -H -H -OCF ₃ -H -H -H -H -H -H -CF ₃ -H -H -H -H -H -Cl -H -Cl -H -Cl -H	-H -H -H -CF ₃-H -H -H -H -H -H -CH ₃-H -Cl -H -OCH ₃-Cl -H -H -OC ₆H ₅ -H -H -OCF ₃-H -Cl -Cl -CH ₃-H -H	-Cl -H -CH(CH ₃) ₂ -H -C(CH ₃) ₃ -CF ₃ -CH ₃ -CN -C ₆H ₅ -H -H -OCF ₃ -H -F -H -Cl -H -CO ₂CH ₃ -H -SCH ₃ -H -H -F -H -H -H -H -C ₂H ₅	-H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -Cl -H -CH ₃ -Cl -H	-H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H	513 513 521 547 535 547 493 504 555 563 493 563 513 497 509 547 547 537 571 525 479 563 531 547 547 507 547 507

[table 117]

[table 118]

[table 119]

[table 120]

[table 121]

[table 122]

[table 123]

[table 124]

[table 125]

Embodiment 1098

(R)-and 2-methyl-2-(4-(N-methyl-N-(1-methyl piperidine-4-yl) amino) phenoxymethyl)-6-nitro-2, the 3-glyoxalidine is [2,1-b] _ azoles also

Embodiment 1099

(R)-4-(1-(4-(2-methyl-6-nitro-2,3-dihydro-imidazol-be [2,1-b] _ azoles-2-ylmethoxy also) phenyl)-3-(4-Trifluoromethoxyphen-l) urea groups)-piperidines-1-carboxylic acid (4-Trifluoromethoxyphen-l) acid amides

Embodiment 1100

6-nitro-2-(4-(4-(4-trifluoromethyl benzyloxy methyl) piperidines-1-yl) phenoxymethyl)-2, the 3-glyoxalidine is [2,1-b] _ azoles also

Fusing point: 140.2-141.7 ℃.

Embodiment 1101

(R)-and 2-methyl-6-nitro-2-(4-(4-(tetrahydropyrans-2-base oxygen ylmethyl) piperidines-1-yl) phenoxymethyl)-2, the 3-glyoxalidine is [2,1-b] _ azoles also

Fusing point: 217.6-218.6 ℃.

Embodiment 1102

(R)-and 2-methyl-6-nitro-2-(4-(4-(hydroxymethyl) piperidines-1-yl) phenoxymethyl)-2, the 3-glyoxalidine is [2,1-b] _ azoles also

Embodiment 1103

2-methyl-6-nitro-2-(4-(4-(4-Trifluoromethyl phenyl ether oxygen base) piperidines-1-yl) benzyl)-2, the 3-glyoxalidine is [2,1-b] _ azoles also

Fusing point: 184.9-186.8 ℃.

Embodiment 1104

(R)-and 2-methyl-6-nitro-2-(4-(4-(4-Trifluoromethoxyphen-l) carbamoyloxy group methyl piperidine-1-yl) phenoxymethyl)-2, the 3-glyoxalidine is [2,1-b] _ azoles also

Fusing point: 211.6 ℃-212.0 ℃ (decomposition)

Embodiment 1105

(R)-and 2-(4-(4-(biphenyl-4-base oxygen ylmethyl) piperidines-1-yl) phenoxymethyl)-2-methyl-6-nitro-2, the 3-glyoxalidine is [2,1-b] _ azoles also

Fusing point: 245 ℃ (decomposition)

Embodiment 1106

(R)-and 2-(1-benzyl-2-(4-(4-trifluoro-methoxybenzyl) piperazine-1-yl)-1H-benzoglyoxaline-5-base oxygen ylmethyl)-2-methyl-6-nitro-2, the 3-glyoxalidine is [2,1-b] _ azoles also

Fusing point: 101.3 ℃-104.0 ℃

Embodiment 1107

(R)-and 2-methyl-6-nitro-2-(4-(4-(4-trifluoro-methoxybenzyl) piperidines-1-ylmethyl) phenoxymethyl)-2, the 3-glyoxalidine is [2,1-b] _ azoles also

Fusing point: 172.5 ℃-174.1 ℃

Embodiment 1108

2-(4-(4-(N-methyl-tert-butoxycarbonyl amino) piperidines-1-ylmethyl) phenoxymethyl)-2-methyl-6-nitro-2, the 3-glyoxalidine is [2,1-b] _ azoles also

Fusing point: 138.5 ℃-141.9 ℃

Embodiment 1109

(R)-2-(4 '-(4-tert-butoxycarbonyl-1,4-Diazesuberane-1-base [diazepan-1-yl]) biphenyl-4-base oxygen ylmethyl)-2-methyl-6-nitro-2, the 3-glyoxalidine is [2,1-b] _ azoles also

Fusing point: 213.8 ℃-215.7 ℃

Embodiment 1110

(R)-2-(4 '-(4-tert-butoxycarbonyl-1,4-Diazesuberane-1-yl) biphenyl-4-base oxygen ylmethyl)-6-nitro-2, the 3-glyoxalidine is [2,1-b] _ azoles also

Fusing point: 235.5 ℃-237.5 ℃

Embodiment 1111

(S)-and 2-methyl-2-(N-methyl-N-(4-(N-methyl-N-(4-trifluoromethyl cinnamyl) amino) benzyl) amino methyl)-6-nitro-2, the 3-glyoxalidine is [2,1-b] _ azoles also

Fusing point: 153.5 ℃-154.5 ℃

Embodiment 1112

(R)-and 2-methyl-6-nitro-2-(4-(2-oxo-2-(4-(4-Trifluoromethyl phenyl ether oxygen base) piperidines-1-yl) ethylamino carbonyl) phenoxymethyl)-2, the 3-glyoxalidine is [2,1-b] _ azoles also

Fusing point: 186.9 ℃-189.5 ℃

Embodiment 1113

2-methyl-6-nitro-2-(2-(4-(4-trifluoro-methoxybenzyl) piperazine-1-yl) benzothiazole-6-base oxygen ylmethyl)-2, the 3-glyoxalidine is [2,1-b] _ azoles also

Fusing point: 172.6 ℃-174.6 ℃

Embodiment 1114

2-(4-(4-(4-chlorophenoxy methyl) piperidines-1-yl) phenoxymethyl)-2-methyl-6-nitro-2, the 3-glyoxalidine is [2,1-b] _ azoles also

Fusing point: 190.0 ℃-190.4 ℃

Embodiment 1115

2-(4-(4-(4-chlorophenoxy methyl) piperidines-1-yl) phenoxymethyl)-6-nitro-2, the 3-glyoxalidine is [2,1-b] _ azoles also

Fusing point: 191.2 ℃-192.5 ℃

Embodiment 1116

6-nitro-2-(4-(4-(4-trifluoro-methoxybenzyl) piperidines-1-yl) phenoxymethyl)-2, the 3-glyoxalidine is [2,1-b] _ azoles also

Fusing point: 132.7 ℃-135.0 ℃

Embodiment 1117

2-methyl-6-nitro-2-(4-(4-(4-trifluoromethoxy cinnamyl) piperazine-1-yl) phenoxymethyl)-2, the 3-glyoxalidine is [2,1-b] _ azoles also

Fusing point: 181.1 ℃-182.2 ℃

[table 126]

Embodiment	R1	R2	R3	R4	R5	R6	mp(℃)
Embodiment	R1	R2	R3	R4	R5	R6	mp(℃)	1118 1119 1120 1121 1122 1123 1124 1125 1126 1127 1128 1129 1130 1131 1132 1133	-CH3 -CH3 -CH3 -CH3 -CH3 -H -H -H -H -CH3 -H -CH3 -CH3 -CH3 -CH3 -CH3	-H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -Cl	-H -H -H -H -H -H -H -Cl -H -H -H -Cl -CF3 -CF3 -CF3 -Cl	-Br -Cl -CH3 -OCF3 -Cl -CF3 -Cl -Cl -Br -OCH3 -OCF3 -H -H -Cl -F -H	-H -Cl -H -H -H -H -H -H -H -H -H -H -CF3 -H -H -H	-H -H -H -H -H -H -H -H -H -H -H -H -H -H -H -H	207.1-208.9 204.7-206.4 210.4-211.9 213.0-214.9 198.6-201.2 172.1-174.7 179.6-181.5 189.1-190.7 202.6-204.4 218.5-220.6 181.1-182.7 195dec 183dec 196.1-197.4 210.5dec 212dec

[table 127]

Embodiment	R1	R2	R3	R4	R5	R6	mp(℃)
Embodiment	R1	R2	R3	R4	R5	R6	mp(℃)	1134 1135 1136 1137 1138 1139	-H -CH ₃ -CH ₃ -H -CH ₃ -H	-H -H -H -H -H -H	-H -H -H -H -H -H	4-ClPh- 4-ClPh- -C ₆H ₅ 4-ClPhO- 4-ClPhO- -C ₆H ₅	-H -H -H -H -H -H	-H -H -H -H -H -H	245-248 241.7-243.5 254.6-258.0 184.7-187.9 179.2-181.8 256.0-258.2

[table 128]

Embodiment	R1	R2	R3	R4	R5	R6	¹H NMR
Embodiment	R1	R2	R3	R4	R5	R6	¹H NMR	1140 1141 1142 1143	-CH ₃ -CH ₃ -H -H	-H -H -H -H	-H -H -H -H	4-CF ₃Ph- 4-CF ₃OPh- 4-CF ₃Ph- 4-CF ₃OPh-	-H -H -H -H	-H -H -H -H	¹H NMR(CDCl ₃)δ1.75(3H，s)，2.52- 2.74(4H，m)，2.99-3.22(4H，m)，3.62(2H， s)，3.92-4.09(2H， m)，4.17(1H，d，J＝10.2Hz)，4.48(1H，d，J＝10 .2Hz)，6.66-6.82(2H，m)，6.82-6.94(2H， m)，7.43(2H，d，J＝8.2Hz)，7.50-7.61(3H， m)，7.69(4H，s). ¹H NMR(CDCl ₃)δ1.76(3H，s)，2.49- 2.74(4H，m)，2.97-3.22(4H，m)，3.61(2H， s)，3.89-4.10(2H，m)，4.17(1H，d， J＝10.2Hz)，4.49(1H，d，J＝10.2Hz)，6.68- 6.81(2H，m)，6.81-6.95(2H，m)，7.28(2H， d，J＝8.6Hz)，7.43(2H，d，J＝8.2Hz)，7.48- 7.67(5H，m). ¹H NMR(CDCl ₃)δ2.51-2.76(4H，m)， 3.00-3.24(4H，m)，3.62(2H，s)，4.14- 4.53(4H，m)，5.47-5.68(1H，m)，6.68- 6.97(4H，m)，7.44(2H，d，J＝8.2Hz)， 7.51-7.62(3H，m)，7.62-7.80(4H，m). ¹H NMR(CDCl ₃)δ2.53-2.73(4H，m)， 3.02-3.21(4H，m)，3.57(2H，s)，4.15- 4.50(4H，m)，5.49-5.66(1H，m)，6.72- 6.95(4H，m)，7.28(2H，d，J＝20.1Hz)， 7.43(2H，d，J＝8.2Hz)，7.52(2H，d， J＝8.3Hz)，7.56-7.67(3H，m).

[table 129]

Embodiment	R1	R2	mp(℃)
Embodiment	R1	R2	mp(℃)	1144 1145 1146 1147 1148 1149 1150 1151 1152 1153 1154 1155 1156 1157	-CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃	4-ClPhCOCH ₂- 4-CF ₃PhCOCH ₂- (CH ₃) ₃COCONH- 4-CF ₃OPhCOCH ₂- 4-CF ₃PhCH ₂N(CH ₃)- 4-CF ₃OPhCH ₂N(CH ₃)- 4-ClPhNHCH ₂CH ₂- 4-CF ₃OPhNHCH ₂CH ₂- 4-ClPhN(CH ₃)CH ₂CH ₂- 4-ClPhCH ₂N(CH ₃)- 4-CF ₃OPhN(CH ₃)CH ₂CH ₂- 4-CF ₃PhNHCH ₂CH ₂- 4-CF ₃PhN(CH ₃)CH ₂CH ₂- PhC≡CCH ₂-	211-212 197-198 254.1-255.9 200-202 201.1-203.7 208.9-210.3 172-173 161-162 179-180 204.8-205.5 141-142.5 159-160 177-178 186.0-189.0

[table 130]

[table 131]

[table 132]

Embodiment	R1	R2	R3	R4	R5	R6	R7	mp(℃)
Embodiment	R1	R2	R3	R4	R5	R6	R7	mp(℃)	1175 1176 1177 1178 1179 1180 1181 1182 1183 1184 1185 1186 1187	-CH ₃ -H -CH ₃ -CH ₃ -CH ₃ -CH ₃ -H -H -H -CH ₃ -CH ₃ -H -H	-CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -H -H -CH ₃ -CH ₃ -H	-CF ₃ -CF ₃ -H -H -H -H -H -H -H -H -H -H -H	-H -H -H -H -H -H -H -H -H -H -H -H -H	-CF ₃ -CF ₃ 4-CF ₃Ph- 4-ClPh- 4-ClPhO- 4-CF ₃OPhO- 4-ClPh- 4-CF ₃OPh- 4-CF ₃OPh- -C ₆H ₅ -C ₆H ₅ -C ₆H ₅ -C ₆H ₅	-H -H -H -H -H -H -H -H -H -H -H -H -H	-H -H -H -H -H -H -H -H -H -H -H -H -H	176.7-178.3 135.7-137.6 226.0-229.3 244.2-246.9 189.5-194.1 200.0-203.5 237.4-239.0 215.8-218.7 233.7-235.8 241.2-243.7 227.2-229.5 229.8-231.7 248.4-253.6

[table 133]

Embodiment	R1	R2	R3	R4	R5	R6	R7	¹H NMR
Embodiment	R1	R2	R3	R4	R5	R6	R7	¹H NMR	1188 1189	-CH ₃ -H	-CH ₃ -CH ₃	-H -H	-H -H	4-CF ₃OPh- 4-CF ₃Ph-	-H -H	-H -H	1H NMR(CDCl3)δ1.65-2.06(7H， m)，2.26(3H，s)，2.47-2.77(3H，m)， 3.51-3.72(4H，m)，3.92-4.09(2H， m)，4.17(1H，d，J＝10.2Hz)， 4.49(1H，d，J＝10.2Hz)，6.66- 6.82(2H，m)，6.82-6.97(2H，m)， 7.27(2H，d，J＝6.9Hz)，7.40(2H，d， J＝8.2Hz)，7.46-7.66(5H，m). 1H NMR(CDCl3)δ1.70-2.06(4H， m)，2.30(3H，s)，2.44-2.78(3H，s)， 3.48-3.75(4H，m)，4.17-4.53(4H， m)，5.48-5.70(1H，m)，6.71- 6.85(2H，m)，6.85-6.98(2H，m)， 7.42(2H，d，J＝8.2Hz)，7.51- 7.61(3H，m)，7.72(4H，s).

[table 134]

[table 135]

Embodiment	R1	R2	mp(℃)
Embodiment	R1	R2	mp(℃)	1192 1193 1194 1195	-CH ₃ -CH ₃ -CH ₃ -CH ₃	-CH ₃ 4-CF ₃PhCH＝CHCH ₂- 4-ClPhCH＝CHCH ₂- 4-CF ₃OPhCH＝CHCH ₂-	252-255dec. 232-234 231-232 228-230

[table 136]

Embodiment	R1	R2	R3	mp(℃)
Embodiment	R1	R2	R3	mp(℃)	1196 1197 1198 1199 1200	-CH ₃ -H -CH ₃ -CH ₃ -CH ₃	4-CF ₃Ph- 4-CF ₃Ph- 4-CF ₃OPh- 4-ClPh- -CH ₃	-CH ₃-CH ₃-C ₂H ₅-C ₂H ₅-CH ₃	188-195dec. 172-174 196.5-198 184.5-186.5 250-252

[table 137]

Embodiment	R1	R2	R3	R4	R5	R6	mp(℃)
Embodiment	R1	R2	R3	R4	R5	R6	mp(℃)	1201 1202 1203 1204 1205 1206 1207	-H -CH ₃ -H -CH ₃ -H -CH ₃ -H	-H -H -H -H -H -H -H	-H -H -H -H -H -H -H	4-CF ₃Ph- 4-CF ₃OPh- 4-CF ₃OPh- 4-ClPh- 4-ClPh- -C ₆H ₅ -C ₆H ₅	-H -H -H -H -H -H -H	-H -H -H -H -H -H -H	196.0-198.2 229.4-230.1 185.7-187.2 248.9-250.0 236.2-238.8 224.2-227.4 235.8-237.4

[table 138]

Embodiment	R1	R2	R3	R4	R5	R6	¹H NMR
Embodiment	R1	R2	R3	R4	R5	R6	¹H NMR	1208	-CH ₃	-H	-H	4-CF ₃Ph-	-H	-H	1H NMR(CDCl3)δ1.30-1.54(2H，m)， 1.58-1.98(6H，m)，2.44-2.72(4H，m)，3.36- 3.62(2H，m)，3.91-4.08(2H，m)，4.16(1H， d，J＝10.2Hz)，4.48(1H，d，J＝10.3Hz)， 6.66-6.81(2H，m)，6.81-6.94(2H，m)，7.18- 7.32(2H，m)，7.44-7.59(3H，m)，7.61- 7.75(4H，m).

[table 139]

Embodiment	R1	R2	mp(℃)
Embodiment	R1	R2	mp(℃)	1209 1210 1211	-CH ₃ -CH ₃ -H	-CH ₂OCH ₃ -H -CH ₂OCH ₃	194.0-195.6 216.8-218.4dec. 150.0-151.2

[table 140]

[table 141]

[table 142]

[table 143]

[table 144]

Embodiment	R1	R2	mp(℃)
Embodiment	R1	R2	mp(℃)	1231 1232	-CH ₃ -CH ₃	4-CF ₃OPhCH ₂- 4-CF ₃OPhCH＝CHCH ₂-	164.6-167.5 155.8-158.5

[table 145]

Embodiment	R1	R2	mp(℃)
Embodiment	R1	R2	mp(℃)	1233 1234 1235 1236 1237	-CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃	4-ClPhS- 4-CF ₃OPhS- 4-ClPhSO ₂- 4-CF ₃OPhSO- 4-CF ₃OPhSO ₂-	182.8-184.6 147.2-150.0 223.5-224.9 128.0-130.7 171.2-174.1

[table 146]

[table 147]

[table 148]

[table 149]

[table 150]

[table 151]

[table 152]

[table 153]

[table 154]

[table 155]

Embodiment	R1	R2	mp(℃)
Embodiment	R1	R2	mp(℃)	1280 1281 1282 1283 1284 1285 1286	-CH ₃ -CH ₃ -CH ₃ -CH ₃ -H -CH ₃ -H	4-CF ₃PhCH ₂- 4-ClPhCH ₂- 4-CF ₃PhCH＝CHCH ₂- 4-CF ₃OPh- 4-CF ₃OPh- 4-CF ₃Ph- 4-CF ₃Ph-	201.2-202.0 194.4-195.7 184.2-186.7 256.1-258.7 254.6-255.6 270.6-271.6 256.8-259.5

[table 156]

Embodiment	R1	R2	mp(℃)
Embodiment	R1	R2	mp(℃)	1287 1288 1289 1290 1291 1292	-CH ₃ -CH ₃ -CH ₃ -H -CH ₃ -H	4-CF ₃OPhO- 4-CF ₃OPhCH ₂- 4-ClPhN(C ₂H ₅)- 4-CF ₃PhO- 4-ClPhN(CH ₃)- 4-ClPhN(CH ₃)-	223.8-225.6 168.3-171.2 119.9-122.0 199.7-202.0 147.8-150.7 128.4-130.9

[table 157]

[table 158]

[table 159]

Embodiment	R1	R2	mp(℃)
Embodiment	R1	R2	mp(℃)	1306 1307 1308	-CH ₃ -CH ₃ -CH ₃	4-CF ₃OPhCH ₂- 4-ClPhCH ₂- 4-CF ₃OPh-	151.1-154.1 180.9-183.1 190.4-192.8

[table 160]

[table 161]

[table 162]

[table 163]

[table 164]

[table 165]

Embodiment	R1	R2	R3	R4	R5	R6	MS(M+1)
Embodiment	R1	R2	R3	R4	R5	R6	MS(M+1)	1328 1329 1330 1331 1332 1333	-CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃	-H -H -H -CH ₃ -CH ₃ -H	-H -H -H -H -H -H	-OCH ₃-CH ₃-OCH ₂C ₆H ₅-CH ₃-CH ₃-CH＝CHC ₆H ₅(trans)	-Cl -CH ₃ -H -H -CH ₃ -H	-H -H -H -CH ₃ -H -H	543 507 585 521 521 581

[table 166]

[table 167]

[table 168]

Embodiment	R1	R2	MS(M+1)
Embodiment	R1	R2	MS(M+1)	1345 1346 1347 1348 1349 1350 1351 1352 1353 1354 1355	-CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃	4-CH ₃OPh- 4-ClPh- 3，4-Cl ₂Ph- 4-CF ₃Ph- 4-CF ₃OPh- 4-ClPhCH ₂- 4-CF ₃PhCH ₂- 4-CH ₃PhCH ₂- 4-CF ₃OPhCH ₂- 3-CH ₃OPhCH ₂- 3，4-Cl ₂PhCH ₂-	578 582 616 616 632 596 630 576 646 592 630

[table 169]

Embodiment	R1	R2	MS(M+1)
Embodiment	R1	R2	MS(M+1)	1356 1357 1358 1359 1360 1361	-CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃	4-ClPh- 4-CH ₃OPh- 4-CF ₃Ph- 4-CH ₃Ph- 3，4-Cl ₂Ph- 4-CF ₃OPh-	567 563 601 547 601 617

[table 170]

Embodiment	R1	R2	MS(M+1)
Embodiment	R1	R2	MS(M+1)	1362 1363 1364 1365 1366 1367 1368 1369 1370 1371	-CH ₃-CH ₃-CH ₃-CH ₃-CH ₃-CH ₃-CH ₃-CH ₃-CH ₃-CH ₃	4-CH ₃OPh- 4-ClPh- 3，4-Cl ₂Ph- 4-CH ₃Ph- 4-CF ₃Ph- 4-ClPhCH ₂- 4-CF ₃PhCH ₂- 4-CF ₃OPhCH ₂- 3-CH ₃OPhCH ₂- 3，4-Cl ₂PhCH ₂-	592 596 630 576 630 610 644 660 606 644

[table 171]

Embodiment	R1	R2	MS(M+1)
Embodiment	R1	R2	MS(M+1)	1372 1373 1374 1375 1376	-CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃	4-ClPh- 4-CF ₃Ph- 4-CH ₃Ph- 3，4-Cl ₂Ph- 4-CF ₃OPh-	581 615 561 615 631

[table 172]

Embodiment	R1	R2	R3	MS(M+1)
Embodiment	R1	R2	R3	MS(M+1)	1377 1378 1379 1380	-CH ₃ -CH ₃ -CH ₃ -CH ₃	-CH ₃ -CH ₃ -CH ₃ -CH ₃	4-CF ₃OPh- 4-CF ₃Ph- 4-CH ₃Ph- 3，4-Cl ₂Ph-	645 629 575 629

[table 173]

[table 174]

[table 175]

[table 176]

[table 177]

[table 178]

[table 179]

[table 180]

Embodiment	R1	R2	R3	R4	R5	R6	MS(M+1)
Embodiment	R1	R2	R3	R4	R5	R6	MS(M+1)	1441 1442 1443 1444 1445 1446 1447 1448	-CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃ -CH ₃	-H -H -H -H -H -H -H -H	-H -H -H -H -H -H -H -H	-OCH ₃ -CH ₃ -F -CF ₃ -CH ₃ -Cl -OCF ₃ 4-ClPhO-	-H -CH ₃ -H -H -H -Cl -H -H	-H -H -H -H -H -H -H -H	517 515 505 555 501 555 571 613

[table 181]

[table 182]

Embodiment 1463

(R)-and 2-(4-(4-(4-chloro-phenyl-) _ azoles-2-yl) phenoxymethyl)-2-methyl-6-nitro-2, the 3-glyoxalidine is [2,1-b] _ azoles also

With 1.73g (7.9mmol) (R)-2-chloro-1-(2-methyl-2-Oxyranyle (oxyranyl) methyl)-4-nitro-1H-imidazoles, 1.80g (6.6mmol) 4-(4-(4-chloro-phenyl-) _ azoles-2-yl) phenol and 0.42g (2.0mmol) potassiumphosphate be suspended in the 15ml ethanol, in argon atmospher, mixture was heated 3 hours under refluxing, stir simultaneously.Concentrated reaction solution adds methylene dichloride to resistates then, to be settled out insoluble product, leaches then.Concentrated filtrate is dissolved in 20ml DMF with resistates, obtains solution.Add 0.29g (7.3mmol) 60% sodium hydride to this solution, use ice-cooledly simultaneously, the gained mixture was stirred 6 hours.Then, under reduced pressure remove and desolvate, add 100ml acetone and 10ml silica gel, succeeded by concentrating to resistates.Resistates is through silica gel chromatography (methylene dichloride: methyl alcohol=50: 1 to 30: 1), make products therefrom crystallization from the mixed solvent of being made up of methylene dichloride and ethanol.Make products therefrom recrystallization from the mixed solvent of forming by acetone and water then, obtain 1.15g (yield: light brown powder 38%), (R)-and 2-(4-(4-(4-chloro-phenyl-) _ azoles-2-yl) phenoxymethyl)-2-methyl-6-nitro-2, the 3-glyoxalidine is [2,1-b] _ azoles also.

Fusing point: 248.8 ℃-251.5 ℃

Embodiment 1464

6-((R)-2-methyl-6-nitro-2,3-glyoxalidine be [2,1-b] _ azoles-2-ylmethoxy also)-2-(4-(4-trifluoro-methoxybenzyl) piperidines-1-yl) quinoline

0.65g (R)-2-chloro-1-(2-methyl-2-oxiranylmethyl radical)-4-nitro-1H-imidazoles, 1.00g 6-hydroxyl-2-(4-(4-trifluoro-methoxybenzyl) piperidines-1-yl) quinoline and 0.16g potassiumphosphate are suspended in the 10ml ethanol, in argon atmospher, mixture was heated 4 hours under refluxing, stir simultaneously.Concentrated reaction solution, resistates is through silica gel chromatography (from hexane: ethyl acetate=1: 3 is to ethyl acetate).Concentrate products therefrom, then resistates is dissolved in DMF (10ml), then to wherein adding the 99mg sodium hydride.Mixture was at room temperature stirred 1 hour.Then, add entry, extract repeatedly with ethyl acetate then to reaction soln.Merge organic layer, water, then with the saturated sodium-chloride water solution washing, then through dried over sodium sulfate.Leach sodium sulfate, under reduced pressure concentrated filtrate.Resistates is through silica gel chromatography (hexane: ethyl acetate was from 1: 1 to 1: 3).Make products therefrom recrystallization from ethanol, obtain 0.57g (yield: yellow powder powder crystal 36%), 6-((R)-2-methyl-6-nitro-2,3-glyoxalidine be [2,1-b] _ azoles-2-ylmethoxy also)-2-(4-(4-trifluoro-methoxybenzyl) piperidines-1-yl) quinoline.

Fusing point: 184.9 ℃-185.9 ℃

Embodiment 1465

6-((R)-2-methyl-6-nitro-2,3-glyoxalidine be [2,1-b] _ azoles-2-ylmethoxy also)-2-(4-(4-trifluoromethoxy benzylidene) piperidines-1-yl) quinoline

0.66g (R)-2-chloro-1-(2-methyl-2-oxiranylmethyl radical)-4-nitro-1H-imidazoles, 0.94g 6-hydroxyl-2-(4-(4-trifluoromethoxy benzylidene)-piperidines-1-yl) quinoline and 0.15g potassiumphosphate are suspended in the 10ml ethanol, in argon atmospher, mixture was heated 6 hours under refluxing, stir simultaneously.Concentrated reaction solution, resistates is through silica gel chromatography (from hexane: ethyl acetate=1: 3 is to ethyl acetate).Concentrate products therefrom, then resistates is dissolved in DMF (10ml), then to wherein adding the 99mg sodium hydride.Mixture was at room temperature stirred 3 hours.Then, add ethyl acetate, then enriched mixture under reduced pressure to reaction soln.Resistates is through silica gel chromatography (methylene dichloride: methyl alcohol=50: 1).Make products therefrom recrystallization from ethanol, obtain 1.37g (yield: yellow powder shape crystal 51%), 6-((R)-2-methyl-6-nitro-2,3-glyoxalidine be [2,1-b] _ azoles-2-ylmethoxy also)-2-(4-(4-trifluoromethoxy benzylidene) piperidines-1-yl) quinoline.

Fusing point: 193.9 ℃-195.9 ℃

Embodiment 1466

(R)-and 2-methyl-6-nitro-2-(6-(4-(4-Trifluoromethyl phenyl ether oxygen base) piperidines-1-yl) naphthalene-2-base oxygen ylmethyl)-2, the 3-glyoxalidine is [2,1-b] _ azoles also

2.12g (R)-2-chloro-1-(2-methyl-2-oxiranylmethyl radical)-4-nitro-1H-imidazoles, 3.02g 6-(4-(4-Trifluoromethyl phenyl ether oxygen base) piperidines-1-yl) Betanaphthol and 0.48g potassiumphosphate are suspended in the 30ml ethanol, in nitrogen atmosphere, mixture was heated 6 hours under refluxing, stir simultaneously.Then, add entry, extract repeatedly with methylene dichloride to reaction soln.Merge organic layer, with the saturated sodium-chloride water solution washing, then through anhydrous magnesium sulfate drying, succeeded by concentrating.Resistates is through silica gel chromatography (from hexane: ethyl acetate=1: 3 is to ethyl acetate).Concentrate products therefrom, obtain the 2.73g yellow powder.The gained powder is dissolved in DMF (27ml), then to wherein adding the 0.21g sodium hydride, succeeded by at room temperature stirring 2.5 hours.Then, add saturated sodium-chloride water solution, extract repeatedly with methylene dichloride then to reaction soln.Merge organic layer, water, then with the saturated sodium-chloride water solution washing, then through anhydrous magnesium sulfate drying.Filter sal epsom, under reduced pressure concentrated filtrate.Resistates is through silica gel chromatography (methylene dichloride: ethyl acetate=4: 1).Make products therefrom recrystallization from the mixed solvent of forming by methylene dichloride, ethyl acetate and diisopropyl ether, obtain 1.05g (yield: yellow powder powder crystal 24%), (R)-2-methyl-6-nitro-2-(6-(4-(4-Trifluoromethyl phenyl ether oxygen base) piperidines-1-yl) naphthalene-2-base oxygen ylmethyl)-2, the 3-glyoxalidine is [2,1-b] _ azoles also.

Fusing point: 204.8 ℃-207.9 ℃

Embodiment 1467

(R)-and 2-methyl-6-nitro-2-(4-(4-(4-trifluoromethoxy benzyloxy) piperidines-1-yl) phenoxymethyl)-2, the 3-glyoxalidine is [2,1-b] _ azoles also

0.305g 4-(4-(4-trifluoromethoxy benzyloxy) piperidines-1-yl) phenol is dissolved in DMF (5ml), to wherein adding the 10mg sodium hydride, succeeded by stirring 20 minutes down at 70 ℃ to 80 ℃.Then, add 0.252g (R)-2-chloro-1-(2-methyl-2-oxiranylmethyl radical)-4-nitro-1H-imidazoles to reaction soln, use simultaneously ice-cooled, succeeded by stirring 20 minutes down at 70 ℃ to 80 ℃.Then, reaction soln is cooled to room temperature.Add entry to reaction soln, extract repeatedly with ethyl acetate.Merge organic layer, water, then with the saturated sodium-chloride water solution washing, then through dried over sodium sulfate.Leach sodium sulfate, under reduced pressure concentrated filtrate.Resistates is through silica gel chromatography (from hexane: ethyl acetate=1: 3 is to ethyl acetate).Make products therefrom recrystallization from the mixed solvent of forming by methylene dichloride and ethyl acetate, obtain 88mg (26.7%) colourless powder shape crystal, (R)-2-methyl-6-nitro-2-(4-(4-(4-trifluoromethoxy benzyloxy) piperidines-1-yl) phenoxymethyl)-2, the 3-glyoxalidine is [2,1-b] _ azoles also.

Fusing point: 214.3 ℃-217.7 ℃

Embodiment 1468

(R)-and 2-methyl-6-nitro-2-(4-(4-(4-trifluoromethyl benzyloxy) piperidines-1-yl) phenoxymethyl)-2, the 3-glyoxalidine is [2,1-b] _ azoles also

0.217g 4-(4-(4-trifluoromethyl benzyloxy) piperidines-1-yl) phenol is dissolved in DMF (5ml), to wherein adding the 27mg sodium hydride, succeeded by stirring 20 minutes down at 70 ℃ to 80 ℃.Then, add 0.188g (R)-2-chloro-1-(2-methyl-2-oxiranylmethyl radical)-4-nitro-1H-imidazoles to reaction soln, use simultaneously ice-cooled, succeeded by stirring 20 minutes down at 70 ℃ to 80 ℃.Then, reaction soln is cooled to room temperature.Add entry to reaction soln, extract repeatedly with ethyl acetate.Merge organic layer, water, then with the saturated sodium-chloride water solution washing, then through dried over sodium sulfate.Leach sodium sulfate, under reduced pressure concentrated filtrate.Resistates is through silica gel chromatography (from hexane: ethyl acetate=1: 3 is to ethyl acetate).Make products therefrom recrystallization from the mixed solvent of forming by methylene dichloride and ethyl acetate, obtain 88mg (26.7%) buff powder, (R)-and 2-methyl-6-nitro-2-(4-(4-(4-trifluoromethyl benzyloxy) piperidines-1-yl) phenoxymethyl)-2, the 3-glyoxalidine is [2,1-b] _ azoles also.

Fusing point: 217.4 ℃-219.7 ℃

Embodiment 1469

8.41g 4-(4-(4-trifluoro-methoxybenzyl) piperidines-1-yl) phenol is dissolved in DMF (84ml), to wherein adding the 1.05g sodium hydride, succeeded by stirring 20 minutes down at 70 ℃ to 80 ℃.Then, add 7.29g (R)-2-chloro-1-(2-methyl-2-oxiranylmethyl radical)-4-nitro-1H-imidazoles to reaction soln, use simultaneously ice-cooled, succeeded by stirring 20 minutes down at 70 ℃ to 80 ℃.Then, reaction soln is cooled to room temperature.Add entry to reaction soln, extract repeatedly with ethyl acetate.Merge organic layer, water, then with the saturated sodium-chloride water solution washing, then through dried over sodium sulfate.Leach sodium sulfate, under reduced pressure concentrated filtrate.Resistates is through silica gel chromatography (methylene dichloride: ethyl acetate=9: 1).Make products therefrom recrystallization from the mixed solvent of forming by methylene dichloride and ethyl acetate, obtain 4.65g (36.5%) buff powder, (R)-2-methyl-6-nitro-2-(4-(4-(4-trifluoro-methoxybenzyl) piperidines-1-yl) phenoxymethyl)-2, the 3-glyoxalidine is [2,1-b] _ azoles also.

¹H-NMR(CDCl ₃)δppm

1.23-1.52(2H，m)，1.52-1.66(3H，m)，1.66-1.89(3H，m)，2.43-2.70(4H，m)，3.50(2H，d，J＝12.1Hz)，3.91-4.09(2H，m)，4.16(1H，d，J＝10.1Hz)，4.48(1H，d，J＝10.2Hz)，6.66-6.81(2H，m)，6.81-6.95(2H，m)，7.05-7.23(4H，m)，7.54(1H，s)

Fusing point: 210.9 ℃-212.4 ℃

(α) _D＝-9.0deg.(c＝1.0，CHCl ₃)

Embodiment 1470

(R)-and 2-(4-(4-(4-benzyl chloride base) piperidines-1-yl) phenoxymethyl)-2-methyl-6-nitro-2, the 3-glyoxalidine is [2,1-b] _ azoles also

1.036g 4-(4-(4-benzyl chloride base) piperidines-1-yl) phenol is dissolved in DMF (5ml), to wherein adding the 151mg sodium hydride, succeeded by stirring 20 minutes down at 70 ℃ to 80 ℃.Then, add 1.04g (R)-2-chloro-1-(2-methyl-2-oxiranylmethyl radical)-4-nitro-1H-imidazoles to reaction soln, use simultaneously ice-cooled, succeeded by stirring 20 minutes down at 70 ℃ to 80 ℃.Then, reaction soln is cooled to room temperature.Add entry to reaction soln, extract repeatedly with ethyl acetate.Merge organic layer, water, then with the saturated sodium-chloride water solution washing, then through dried over sodium sulfate.Leach sodium sulfate, under reduced pressure concentrated filtrate.Resistates is through silica gel chromatography (from hexane: ethyl acetate=1: 3 is to ethyl acetate).Make products therefrom recrystallization from the mixed solvent of forming by methylene dichloride and ethyl acetate, obtain 0.286g (17.3%) yellow powder powder crystal, (R)-and 2-(4-(4-(4-benzyl chloride base) piperidines-1-yl) phenoxymethyl)-2-methyl-6-nitro-2, the 3-glyoxalidine is [2,1-b] _ azoles also.

Fusing point: 207.1 ℃-211.2 ℃

Embodiment 1471

(R)-and 2-methyl-6-nitro-2-(4-(4-(4-trifluoromethoxy Chinese cassia tree oxygen base) piperidines-1-yl) phenoxymethyl)-2, the 3-glyoxalidine is [2,1-b] _ azoles also

2.21g 4-(4-(4-trifluoromethoxy Chinese cassia tree oxygen base) piperidines-1-yl) phenol is dissolved in DMF (22ml), to wherein adding the 0.247g sodium hydride, succeeded by stirring 20 minutes down at 70 ℃ to 80 ℃.Then, add 1.71g (R)-2-chloro-1-(2-methyl-2-oxiranylmethyl radical)-4-nitro-1H-imidazoles to reaction soln, use simultaneously ice-cooled, succeeded by stirring 20 minutes down at 70 ℃ to 80 ℃.Then, reaction soln is cooled to room temperature.Add entry to reaction soln, extract repeatedly with ethyl acetate.Merge organic layer, water, then with the saturated sodium-chloride water solution washing, then through anhydrous magnesium sulfate drying.Leach sal epsom, under reduced pressure concentrated filtrate.Resistates is through silica gel chromatography (methylene dichloride: ethyl acetate=9: 1).Make products therefrom recrystallization from the mixed solvent of forming by methylene dichloride and ethyl acetate, obtain 0.70g (21.7%) yellow powder powder crystal, (R)-2-methyl-6-nitro-2-(4-(4-(4-trifluoromethoxy Chinese cassia tree oxygen base) piperidines-1-yl) phenoxymethyl)-2, the 3-glyoxalidine is [2,1-b] _ azoles also.

Fusing point: 213.7 ℃-217.4 ℃

Embodiment 1472

(R)-and 6-nitro-2-(4-(4-(4-trifluoromethoxy benzyloxy) piperidines-1-yl) phenoxymethyl)-2, the 3-glyoxalidine is [2,1-b] _ azoles also

4.60g 4-(4-(4-trifluoromethoxy benzyloxy) piperidines-1-yl) phenol is dissolved in DMF (46ml), to wherein adding the 0.55g sodium hydride, succeeded by stirring 20 minutes down at 70 ℃ to 80 ℃.Then, add 3.57g (R)-2-chloro-1-oxiranylmethyl radical-4-nitro-1H-imidazoles to reaction soln, use simultaneously ice-cooled, succeeded by stirring 20 minutes down at 70 ℃ to 80 ℃.Then, reaction soln is cooled to room temperature.Add entry to reaction soln, extract repeatedly with ethyl acetate.Merge organic layer, water, then with the saturated sodium-chloride water solution washing, then through dried over sodium sulfate.Leach sodium sulfate, under reduced pressure concentrated filtrate.Resistates is through silica gel chromatography (methylene dichloride: ethyl acetate was from 9: 1 to 6: 4).Make products therefrom recrystallization from the mixed solvent of forming by methylene dichloride and ethyl acetate, obtain 0.99g (14.8%) yellow powder powder crystal, (R)-6-nitro-2-(4-(4-(4-trifluoromethoxy benzyloxy) piperidines-1-yl) phenoxymethyl)-2, the 3-glyoxalidine is [2,1-b] _ azoles also.

Fusing point: 188.3 ℃-189.4 ℃

Embodiment 1473

(R)-and 2-methyl-6-nitro-2-(4-(4-(2-(4-Trifluoromethoxyphen-l) ethyl) piperidines-1-yl) phenoxymethyl)-2, the 3-glyoxalidine is [2,1-b] _ azoles also

1.01g (R)-2-chloro-1-(2-methyl-2-oxiranylmethyl radical)-4-nitro-1H-imidazoles and 1.36g 4-(4-(2-(4-Trifluoromethoxyphen-l) ethyl) piperidines-1-yl) phenol are dissolved in DMF (14ml), to wherein adding the 0.18g sodium hydride, succeeded by stirring 1 hour down at 50 ℃.Then, reaction soln is cooled to room temperature.Add entry to reaction soln, extract repeatedly with ethyl acetate.Merge organic layer, water, then with the saturated sodium-chloride water solution washing, then through dried over sodium sulfate.Leach sodium sulfate, under reduced pressure concentrated filtrate.Resistates is through silica gel chromatography (methylene dichloride: ethyl acetate was from 9: 1 to 8: 2).Make products therefrom recrystallization from the mixed solvent of forming by methylene dichloride, ethyl acetate and diisopropyl ether, obtain 0.70g (34.4%) yellow powder powder crystal, (R)-2-methyl-6-nitro-2-(4-(4-(2-(4-Trifluoromethoxyphen-l) ethyl) piperidines-1-yl) phenoxymethyl)-2, the 3-glyoxalidine is [2,1-b] _ azoles also.

Fusing point: 239.4 ℃-241.3 ℃

Embodiment 1474

(R)-and 2-methyl-6-nitro-2-(6-(4-(4-Trifluoromethyl phenyl ether oxygen base) piperidines-1-yl) pyridin-3-yl oxygen ylmethyl)-2, the 3-glyoxalidine is [2,1-b] _ azoles also

0.51g (R)-2-chloro-1-(2-methyl-2-oxiranylmethyl radical)-4-nitro-1H-imidazoles and 0.67g 3-hydroxyl-6-(4-(4-Trifluoromethyl phenyl ether oxygen base) piperidines-1-yl) pyridine are dissolved in DMF (6.7ml), to wherein adding the 91mg sodium hydride, succeeded by stirring 1 hour down at 50 ℃.Then, reaction soln is cooled to room temperature.Add entry to reaction soln, extract repeatedly with ethyl acetate.Merge organic layer, water, then with the saturated sodium-chloride water solution washing, then through anhydrous magnesium sulfate drying.Filter sal epsom, under reduced pressure concentrated filtrate.Resistates is through silica gel chromatography (methylene dichloride: ethyl acetate was from 9: 1 to 8: 2).Make products therefrom recrystallization from the mixed solvent of forming by methylene dichloride, ethyl acetate and diisopropyl ether, obtain 296mg (29.1%) yellow powder powder crystal, (R)-2-methyl-6-nitro-2-(6-(4-(4-Trifluoromethyl phenyl ether oxygen base) piperidines-1-yl) pyridin-3-yl oxygen ylmethyl)-2, the 3-glyoxalidine is [2,1-b] _ azoles also.

Fusing point: 185.9 ℃-186.7 ℃

Embodiment 1475

(R)-and 6-nitro-2-(4-(4-(4-trifluoro-methoxybenzyl) piperidines-1-yl) phenoxymethyl)-2, the 3-glyoxalidine is [2,1-b] _ azoles also

0.72g (R)-2-chloro-1-oxiranylmethyl radical-4-nitro-1H-imidazoles and 1.00g4-(4-(4-trifluoro-methoxybenzyl) piperidines-1-yl) phenol are dissolved in DMF (10ml), to wherein adding the 0.14g sodium hydride, succeeded by stirring 1 hour down at 50 ℃.Then, reaction soln is cooled to room temperature.Add entry to reaction soln, extract repeatedly with ethyl acetate.Merge organic layer, water, then with the saturated sodium-chloride water solution washing, then through anhydrous magnesium sulfate drying.Filter sal epsom, under reduced pressure concentrated filtrate.Resistates is through silica gel chromatography (methylene dichloride: ethyl acetate was from 9: 1 to 7: 3).Make products therefrom recrystallization from the mixed solvent of forming by methylene dichloride, ethyl acetate and diisopropyl ether, obtain 0.20g (13.7%) yellow powder powder crystal, (R)-6-nitro-2-(4-(4-(4-trifluoro-methoxybenzyl) piperidines-1-yl) phenoxymethyl)-2, the 3-glyoxalidine is [2,1-b] _ azoles also.

Fusing point: 160.5 ℃-164.0 ℃

Embodiment 1476

(R)-and 2-methyl-6-nitro-2-(4-(4-(4-Trifluoromethoxyphen-l)-1,4-Diazesuberane-1-yl) phenoxymethyl)-2, the 3-glyoxalidine is [2,1-b] _ azoles also

With 2.21g (R)-2-chloro-1-(2-methyl-2-oxiranylmethyl radical)-4-nitro-1H-imidazoles and 2.86g 4-(4-(4-Trifluoromethoxyphen-l)-1,4-Diazesuberane-1-yl) phenol is dissolved in DMF (29ml), to wherein adding the 0.39g sodium hydride, succeeded by stirring 1 hour down at 50 ℃.Then, reaction soln is cooled to room temperature.Add entry to reaction soln, extract repeatedly with methylene dichloride.Merge organic layer, water, then with the saturated sodium-chloride water solution washing concentrates then.Resistates is through silica gel chromatography (from hexane: ethyl acetate=1: 3 is to ethyl acetate).Make products therefrom recrystallization from Virahol then, obtain 720mg (16.6%) red powder, (R)-2-methyl-6-nitro-2-(4-(4-(4-Trifluoromethoxyphen-l)-1,4-Diazesuberane-1-yl) phenoxymethyl)-2, the 3-glyoxalidine is [2,1-b] _ azoles also.

Fusing point: 134.0 ℃-137.9 ℃

Embodiment 1477

(R)-and 2-methyl-2-(4-(4-(N-methyl-N-(2-fluoro-4-trifluoromethyl benzyl) amino) piperidines-1-yl) phenoxymethyl)-6-nitro-2, the 3-glyoxalidine is [2,1-b] _ azoles also

With 0.80g (R)-2-methyl-2-(4-(4-(N-methyl-N-tert-butoxycarbonyl amino) piperidines-1-yl) phenoxymethyl)-6-nitro-2,3-glyoxalidine also [2,1-b] _ azoles is dissolved in 2ml trifluoroacetic acid and 2ml methylene dichloride, succeeded by at room temperature stirring 15 hours.Then, concentrated reaction solution under reduced pressure, then, to wherein adding 2ml methylene dichloride and 2ml triethylamine.Mixture was at room temperature stirred 5 minutes, under reduced pressure concentrate then.Resistates is dissolved in the 8ml ethylene dichloride, then,, uses ice-cooled simultaneously to wherein adding 0.63g 2-fluoro-4-trifluoromethylated benzaldehyde and 0.70g sodium triacetoxy borohydride.Make mixture be warming up to room temperature, then mixture was stirred 24 hours.Then, add wet chemical and methylene dichloride to reaction soln.Stir the mixture, use dichloromethane extraction then.Organic layer through dried over mgso, is filtered then.Under reduced pressure concentrate gained filtrate.Resistates is through silica gel chromatography (methylene dichloride: methyl alcohol=9: 1).Make products therefrom crystallization from ethyl acetate, obtain 0.48g (yield: buff powder 51.8%), (R)-and 2-methyl-2-(4-(4-(N-methyl-N-(2-fluoro-4-trifluoromethyl benzyl) amino) piperidines-1-yl) phenoxymethyl)-6-nitro-2, the 3-glyoxalidine is [2,1-b] _ azoles also.

Fusing point: 197.5 ℃-199.2 ℃

Embodiment 1478

(R)-and 2-methyl-2-(4-(4-(N-methyl-N-(2-trifluoromethyl benzyl) amino) piperidines-1-yl) phenoxymethyl)-6-nitro-2, the 3-glyoxalidine is [2,1-b] _ azoles also

With 0.80g (R)-2-methyl-2-(4-(4-(N-methyl-N-tert-butoxycarbonyl amino) piperidines-1-yl) phenoxymethyl)-6-nitro-2,3-glyoxalidine also [2,1-b] _ azoles is dissolved in 2ml trifluoroacetic acid and 2ml methylene dichloride, succeeded by at room temperature stirring 15 hours.Then, concentrated reaction solution under reduced pressure, then, to wherein adding 2ml methylene dichloride and 2ml triethylamine.Mixture was at room temperature stirred 5 minutes, under reduced pressure concentrate then.Resistates is dissolved in the 8ml ethylene dichloride, then,, uses ice-cooled simultaneously to wherein adding 0.57g 2-trifluoromethylated benzaldehyde and 0.70g sodium triacetoxy borohydride.Make mixture be warming up to room temperature, then mixture was stirred 24 hours.Then, add wet chemical and methylene dichloride to reaction soln.Stir the mixture, use dichloromethane extraction then.Organic layer through dried over mgso, is filtered then.Under reduced pressure concentrate gained filtrate.Resistates is through silica gel chromatography (methylene dichloride: methyl alcohol=9: 1).Make products therefrom crystallization from ethyl acetate, obtain 0.47g (yield: buff powder 52.4%), (R)-and 2-methyl-2-(4-(4-(N-methyl-N-(2-trifluoromethyl benzyl) amino) piperidines-1-yl) phenoxymethyl)-6-nitro-2, the 3-glyoxalidine is [2,1-b] _ azoles also.

Fusing point: 189.6 ℃-190.2 ℃

Embodiment 1479

(R)-and 2-methyl-2-(4-(4-(N-methyl-N-(3,5-two trifluoromethyl benzyls) amino) piperidines-1-yl) phenoxymethyl)-6-nitro-2, the 3-glyoxalidine is [2,1-b] _ azoles also

With 0.80g (R)-2-methyl-2-(4-(4-(N-methyl-N-tert-butoxycarbonyl amino) piperidines-1-yl) phenoxymethyl)-6-nitro-2,3-glyoxalidine also [2,1-b] _ azoles is dissolved in 2ml trifluoroacetic acid and 2ml methylene dichloride, succeeded by at room temperature stirring 15 hours.Then, concentrated reaction solution under reduced pressure, then, to wherein adding 2ml methylene dichloride and 2ml triethylamine.Mixture was at room temperature stirred 5 minutes, under reduced pressure concentrate then.Resistates is dissolved in the 8ml ethylene dichloride, and then, to wherein adding 0.79g 3,5-two trifluoromethylated benzaldehydes and 0.70g sodium triacetoxy borohydride are used ice-cooled simultaneously.Make mixture be warming up to room temperature, then mixture was stirred 19 hours.Then, add wet chemical and methylene dichloride to reaction soln.Stir the mixture, use dichloromethane extraction then.Organic layer through dried over mgso, is filtered then.Under reduced pressure concentrate gained filtrate.Resistates is through silica gel chromatography (methylene dichloride: methyl alcohol=9: 1).Make products therefrom crystallization from ethyl acetate, obtain 0.55g (yield: buff powder 54.9%), (R)-2-methyl-2-(4-(4-(N-methyl-N-(3,5-two trifluoromethyl benzyls) amino) piperidines-1-yl) phenoxymethyl)-6-nitro-2, the 3-glyoxalidine is [2,1-b] _ azoles also.

Fusing point: 193.8 ℃-195.3 ℃

Embodiment 1480

(R)-and 2-methyl-6-nitro-2-(4-(4-(3-trifluoro-methoxybenzyl) piperidines-1-yl) phenoxymethyl)-2, the 3-glyoxalidine is [2,1-b] _ azoles also

1.21g (R)-2-chloro-1-(2-methyl-2-oxiranylmethyl radical)-4-nitro-1H-imidazoles and 1.56g 4-(4-(3-trifluoro-methoxybenzyl) piperidines-1-yl) phenol are dissolved in DMF (16ml), then to wherein adding the 0.21g sodium hydride, succeeded by stirring 1 hour down at 50 ℃.Then, reaction soln is cooled to room temperature.Add entry to reaction soln, extract mixture repeatedly with methylene dichloride then.Merge organic layer, water, then with the saturated sodium-chloride water solution washing, then through anhydrous sodium sulfate drying.Leach sodium sulfate, under reduced pressure concentrated filtrate.Resistates is through silica gel chromatography (methylene dichloride: ethyl acetate was from 9: 1 to 8: 2).Make products therefrom recrystallization from the mixed solvent of forming by methylene dichloride, ethyl acetate and diisopropyl ether, obtain 0.80g (33.8%) yellow powder powder crystal, (R)-2-methyl-6-nitro-2-(4-(4-(3-trifluoro-methoxybenzyl) piperidines-1-yl) phenoxymethyl)-2, the 3-glyoxalidine is [2,1-b] _ azoles also.

Fusing point: 187.4 ℃-189.8 ℃

Embodiment 1481

(R)-and 2-methyl-2-(4-(4-(N-methyl-N-(5-chlorobenzene and furans-2-ylmethyl) amino) piperidines-1-yl) phenoxymethyl)-6-nitro-2, the 3-glyoxalidine is [2,1-b] _ azoles also

With 0.80g (R)-2-methyl-2-(4-(4-(N-methyl-N-tert-butoxycarbonyl amino) piperidines-1-yl) phenoxymethyl)-6-nitro-2,3-glyoxalidine also [2,1-b] _ azoles is dissolved in 2ml trifluoroacetic acid and 2ml methylene dichloride, succeeded by at room temperature stirring 15 hours.Then, concentrated reaction solution under reduced pressure, then, to wherein adding 2ml methylene dichloride and 2ml triethylamine.Mixture was at room temperature stirred 5 minutes, under reduced pressure concentrate then.Resistates is dissolved in the 8ml ethylene dichloride, then,, uses ice-cooled simultaneously to wherein adding 0.59g 5-chlorobenzene and furans-2-formaldehyde and 0.70g sodium triacetoxy borohydride.Make mixture be warming up to room temperature, then mixture was stirred 22 hours.Then, add wet chemical and methylene dichloride to reaction soln.Stir the mixture, use dichloromethane extraction then.Organic layer through dried over mgso, is filtered then.Under reduced pressure concentrate gained filtrate.Resistates is through silica gel chromatography (methylene dichloride: methyl alcohol=9: 1).Make products therefrom crystallization from acetone then, obtain 0.65g (yield: yellow powder 66.5%), (R)-and 2-methyl-2-(4-(4-(N-methyl-N-(5-chlorobenzene and furans-2-ylmethyl) amino) piperidines-1-yl) phenoxymethyl)-6-nitro-2, the 3-glyoxalidine is [2,1-b] _ azoles also.

Fusing point: 207.4 ℃-210.0 ℃

Embodiment 1482

(R)-and 2-methyl-6-nitro-2-(6-(4-(4-trifluoro-methoxybenzyl) piperidines-1-yl) pyridin-3-yl oxygen ylmethyl)-2, the 3-glyoxalidine is [2,1-b] _ azoles also

2.63g (R)-2-chloro-1-(2-methyl-2-oxiranylmethyl radical)-4-nitro-1H-imidazoles and 3.41g 3-hydroxyl-6-(4-(4-trifluoro-methoxybenzyl) piperidines-1-yl) pyridine are dissolved in DMF (6.7ml), then to wherein adding the 0.46g sodium hydride, succeeded by stirring 1.5 hours down at 50 ℃.Then, reaction soln is cooled to room temperature.Add entry to reaction soln, extract mixture repeatedly with methylene dichloride then.Merge organic layer, water, then with the saturated sodium-chloride water solution washing, then through anhydrous magnesium sulfate drying.Filter sal epsom, under reduced pressure concentrated filtrate.Resistates is through silica gel chromatography (methylene dichloride: ethyl acetate was from 9: 1 to 6: 4).Make products therefrom recrystallization from the mixed solvent of forming by ethyl acetate and diisopropyl ether, obtain 1.46g (28.3%) yellow powder powder crystal, (R)-2-methyl-6-nitro-2-(6-(4-(4-trifluoro-methoxybenzyl) piperidines-1-yl) pyridin-3-yl oxygen ylmethyl)-2, the 3-glyoxalidine is [2,1-b] _ azoles also.

Fusing point: 200.1 ℃-202.9 ℃

Embodiment 1483

(R)-and 6-nitro-2-(4-(4-(2-(4-Trifluoromethoxyphen-l) ethyl) piperidines-1-yl) phenoxymethyl)-2, the 3-glyoxalidine is [2,1-b] _ azoles also

0.75g (R)-2-chloro-1-oxiranylmethyl radical-4-nitro-1H-imidazoles and 1.07g4-(4-(2-(4-Trifluoromethoxyphen-l) ethyl) piperidines-1-yl) phenol are dissolved in DMF (11ml), then to wherein adding the 0.14g sodium hydride, succeeded by stirring 1 hour down at 50 ℃.Then, reaction soln is cooled to room temperature.Add entry to reaction soln, extract mixture repeatedly with methylene dichloride then.Merge organic layer, water, then with the saturated sodium-chloride water solution washing, then through dried over mgso.Leach sal epsom, under reduced pressure concentrated filtrate.Resistates is through silica gel chromatography (methylene dichloride: ethyl acetate was from 9: 1 to 6: 4).Make products therefrom recrystallization from the mixed solvent of forming by methylene dichloride and diisopropyl ether, obtain 0.31g (19.8%) yellow powder powder crystal, (R)-6-nitro-2-(4-(4-(2-(4-Trifluoromethoxyphen-l) ethyl) piperidines-1-yl) phenoxymethyl)-2, the 3-glyoxalidine is [2,1-b] _ azoles also.

Fusing point: 208.9 ℃-211.7 ℃

Embodiment 1484

(R)-and 2-methyl-2-(4-(4-(N-methyl-N-(4-trifluoromethoxy cinnamyl) amino) piperidines-1-yl) phenoxymethyl)-6-nitro-2, the 3-glyoxalidine is [2,1-b] _ azoles also

With 2.76g (R)-2-methyl-2-(4-(4-(N-methyl-N-tert-butoxycarbonyl amino) piperidines-1-yl) phenoxymethyl)-6-nitro-2,3-glyoxalidine also [2,1-b] _ azoles is dissolved in 5ml trifluoroacetic acid and 10ml methylene dichloride, succeeded by at room temperature stirring 0.5 hour.Then, concentrated reaction solution under reduced pressure, then, to wherein adding 10ml methylene dichloride and 10ml N, N-dimethyl amine.Mixture was at room temperature stirred 10 minutes, under reduced pressure concentrate then.Resistates is dissolved in the 30ml ethylene dichloride, to wherein adding 1.43g 4-trifluoromethoxy phenylacrolein and 1.78g sodium triacetoxy borohydride, uses ice-cooled simultaneously then.Make mixture be warming up to room temperature, spend the night succeeded by stirring.Then, add wet chemical and methylene dichloride to reaction soln.Stir the mixture, use dichloromethane extraction then.Organic layer through dried over mgso, is filtered then.Under reduced pressure concentrate gained filtrate.Resistates is through silica gel chromatography (methylene dichloride: acetone was from 5: 1 to 1: 1).Make products therefrom recrystallization from aqueous acetone then, obtain 1.976g (yield: buff powder 58.9%), (R)-2-methyl-2-(4-(4-(N-methyl-N-(4-trifluoromethoxy cinnamyl) amino) piperidines-1-yl) phenoxymethyl)-6-nitro-2, the 3-glyoxalidine is [2,1-b] _ azoles also.

Fusing point: 213.0 ℃-214.9 ℃

Embodiment 1485

(R)-and 2-(4-(4-(3,4-dichloro cinnamyl) piperazine-1-yl) phenoxymethyl)-2-methyl-6-nitro-2, the 3-glyoxalidine is [2,1-b] _ azoles also

With 2.76g (R)-2-methyl-2-(4-(4-tert-butoxycarbonyl piperazine-1-yl) phenoxymethyl)-6-nitro-2,3-glyoxalidine also [2,1-b] _ azoles is dissolved in 5ml trifluoroacetic acid and 10ml methylene dichloride, succeeded by at room temperature stirring 0.5 hour.Then, concentrated reaction solution under reduced pressure, then, to wherein adding 10ml methylene dichloride and 10ml N, N-dimethyl amine.Mixture was at room temperature stirred 5 minutes, under reduced pressure concentrate then.Resistates is dissolved in the 30ml ethylene dichloride, then to wherein adding 1.33g 3,4-two chlorocinnamaldehydes and 1.78g sodium triacetoxy borohydride.Mixture at room temperature stirred spend the night.Then, add wet chemical and methylene dichloride to reaction soln.Stir the mixture, use dichloromethane extraction then.Organic layer through dried over mgso, is filtered then.Under reduced pressure concentrate gained filtrate.Resistates is through silica gel chromatography (methylene dichloride: acetone was from 5: 1 to 1: 1).Make products therefrom crystallization from the mixed solvent of forming by methylene dichloride and ethyl acetate then, obtain 2.243g (yield: buff powder 68.7%), (R)-((4-(3 for 4-for 2-, 4-dichloro cinnamyl) phenoxymethyl piperazine-1-yl))-2-methyl-6-nitro-2, the 3-glyoxalidine is [2,1-b] _ azoles also.

Fusing point: 204.7 ℃-206.4 ℃

Embodiment 1486

(R)-and 2-methyl-2-(4-(N-methyl-N-(1-(4-Trifluoromethoxyphen-l) piperidin-4-yl methyl) amino) phenoxymethyl)-6-nitro-2, the 3-glyoxalidine is [2,1-b] _ azoles also

0.408g (R)-2-chloro-1-(2-methyl-2-oxiranylmethyl radical)-4-nitro-1H-imidazoles and 0.57g 4-(N-methyl-N-(1-(4-Trifluoromethoxyphen-l) piperidin-4-yl methyl) amino) phenol are dissolved in 6ml DMF, then to wherein adding the 72mg sodium hydride, succeeded by stirring 2 hours down at 50 to 60 ℃.Then, reaction soln is cooled to room temperature.Add entry to reaction soln, extract mixture repeatedly with ethyl acetate then.Merge organic layer, water, then with the saturated sodium-chloride water solution washing, then through dried over mgso.Leach sal epsom, under reduced pressure concentrated filtrate.(from hexane: ethyl acetate=1: 3 is to methylene dichloride: ethyl acetate=1: 1) through silica gel chromatography for resistates.Make products therefrom recrystallization from aqueous acetone, obtain 0.130g (yield: orange powder shape crystal 15.4%), (R)-2-methyl-2-(4-(N-methyl-N-(1-(4-Trifluoromethoxyphen-l) piperidin-4-yl methyl) amino) phenoxymethyl)-6-nitro-2, the 3-glyoxalidine is [2,1-b] _ azoles also.

Fusing point: 172.5 ℃-175.2 ℃

Embodiment 1487

0.131g (R)-2-chloro-1-(2-methyl-2-oxiranylmethyl radical)-4-nitro-1H-imidazoles and 0.177g 4-(N-methyl-N-(1-(4-Trifluoromethoxyphen-l) piperidin-4-yl) amino) phenol are dissolved in 4ml DMF, then to wherein adding the 23mg sodium hydride, succeeded by stirring 2 hours down at 50 ℃ to 60 ℃.Then, reaction soln is cooled to room temperature.Add entry to reaction soln, extract mixture repeatedly with ethyl acetate then.Merge organic layer, water, then with the saturated sodium-chloride water solution washing, then through dried over mgso.Leach sal epsom, under reduced pressure concentrated filtrate.(from hexane: ethyl acetate=1: 3 is to methylene dichloride: ethyl acetate=1: 1) through silica gel chromatography for resistates.Make products therefrom recrystallization from aqueous acetone, obtain 93mg (yield: yellow powder powder crystal 35%), (R)-and 2-methyl-2-(4-(N-methyl-N-(1-(4-Trifluoromethoxyphen-l) piperidin-4-yl) amino) phenoxymethyl)-6-nitro-2, the 3-glyoxalidine is [2,1-b] _ azoles also.

Fusing point: 137.9 ℃-139.2 ℃

Embodiment 1488

(R)-and 2-methyl-6-nitro-2-(4-(1-(2-(4-trifluoromethyl) thiazole-4-ylmethyl) piperidin-4-yl) phenoxymethyl)-2, the 3-glyoxalidine is [2,1-b] _ azoles also

With 0.300g (R)-2-methyl-6-nitro-2-(4-(1-tert-butoxycarbonyl piperidin-4-yl) phenoxymethyl)-2,3-glyoxalidine also [2,1-b] _ azoles joins in 1ml trifluoroacetic acid and the 1ml methylene dichloride, succeeded by at room temperature stirring 1 hour.Then, under reduced pressure concentrated reaction solution is dissolved in resistates the 1ml methylene dichloride then, then to wherein adding the 1ml triethylamine.Mixture was at room temperature stirred 5 minutes, under reduced pressure concentrate then.Resistates is dissolved in 5ml methyl alcohol, then,, uses ice-cooled simultaneously to wherein adding 0.219g 2-(4-trifluoromethyl) thiazole-4-formaldehyde, 82mg sodium cyanoborohydride and 0.5ml acetate.The gained mixture was at room temperature stirred 3 days.Then, to wherein adding saturated sodium bicarbonate aqueous solution.Stir the mixture, use ethyl acetate extraction, wash with saturated sodium-chloride water solution then.Organic layer through dried over mgso, is under reduced pressure concentrated then.(from methylene dichloride: acetone=3: 1 is to methylene dichloride: methyl alcohol=20: 1) through silica gel chromatography for resistates.Make products therefrom recrystallization from aqueous acetone then, obtain 65mg (yield: white powder 16.6%), (R)-and 2-methyl-6-nitro-2-(4-(1-(2-(4-trifluoromethyl) thiazole-4-ylmethyl) piperidin-4-yl) phenoxymethyl)-2, the 3-glyoxalidine is [2,1-b] _ azoles also.

Fusing point: 194.6 ℃-196.4 ℃

Embodiment 1489

OPC-77094

(R)-and 2-methyl-6-nitro-2-(4-(1-(4-trifluoromethyl cinnamyl) piperidin-4-yl) phenoxymethyl)-2, the 3-glyoxalidine is [2,1-b] _ azoles also

With 0.300g (R)-2-methyl-6-nitro-2-(4-(1-tert-butoxycarbonyl piperidin-4-yl) phenoxymethyl)-2,3-glyoxalidine also [2,1-b] _ azoles joins in 1ml trifluoroacetic acid and the 1ml methylene dichloride, succeeded by at room temperature stirring 1 hour.Then, under reduced pressure concentrated reaction solution is dissolved in resistates the 1ml methylene dichloride then, then to wherein adding the 1ml triethylamine.Mixture was at room temperature stirred 5 minutes, under reduced pressure concentrate then.Resistates is dissolved in 5ml methyl alcohol, then,, uses ice-cooled simultaneously to wherein adding 0.170g 4-trifluoromethyl phenylacrolein, 82mg sodium cyanoborohydride and 0.5ml acetate.Then, the gained mixture was at room temperature stirred 3 days.To wherein adding saturated sodium bicarbonate aqueous solution.Stir the mixture, use ethyl acetate extraction, wash with saturated sodium-chloride water solution then.Organic layer through dried over mgso, is under reduced pressure concentrated then.(from methylene dichloride: acetone=3: 1 is to methylene dichloride: methyl alcohol=20: 1) through silica gel chromatography for resistates.Make products therefrom recrystallization from aqueous acetone then, obtain 66mg (yield: white powder 18.6%), (R)-and 2-methyl-6-nitro-2-(4-(1-(4-trifluoromethyl cinnamyl) piperidin-4-yl) phenoxymethyl)-2, the 3-glyoxalidine is [2,1-b] _ azoles also.

Fusing point: 185.9 ℃-187.1 ℃

Embodiment 1490

With 0.300g (R)-2-methyl-6-nitro-2-(4-(4-tert-butoxycarbonyl piperazine-1-yl) phenoxymethyl)-2,3-glyoxalidine also [2,1-b] _ azoles joins in 3ml trifluoroacetic acid and the 3ml methylene dichloride, succeeded by at room temperature stirring 2 hours.Then, under reduced pressure concentrated reaction solution is dissolved in resistates the 3ml methylene dichloride then, then to wherein adding the 3ml triethylamine.Mixture was at room temperature stirred 10 minutes, under reduced pressure concentrate then.Resistates is dissolved in 5ml methyl alcohol, then,, uses ice-cooled simultaneously to wherein adding 0.170g 4-trifluoromethoxy phenoxy acetaldehyde, 82mg sodium cyanoborohydride and 0.1ml acetate.Then, the gained mixture is at room temperature stirred spend the night.To wherein adding saturated sodium bicarbonate aqueous solution.Stir the mixture, use ethyl acetate extraction, wash with saturated sodium-chloride water solution then.Organic layer through dried over mgso, is under reduced pressure concentrated then.(from methylene dichloride: acetone=3: 1 is to methylene dichloride: methyl alcohol=20: 1) through silica gel chromatography for resistates.Make products therefrom recrystallization from aqueous acetone then, obtain 157mg (yield: white powder 42.7%), (R)-and 2-methyl-6-nitro-2-(4-(4-(2-(4-Trifluoromethyl phenyl ether oxygen base) ethyl) piperazine-1-yl) phenoxymethyl)-2, the 3-glyoxalidine is [2,1-b] _ azoles also.

Fusing point: 194.8 ℃-195.6 ℃

Embodiment 1491

(R)-and 2-methyl-6-nitro-2-(4-(4-(4-trifluoromethyl cinnamyl) piperazine-1-yl) phenoxymethyl)-2, the 3-glyoxalidine is [2,1-b] _ azoles also

With 0.300g (R)-2-methyl-6-nitro-2-(4-(4-tert-butoxycarbonyl piperazine-1-yl) phenoxymethyl)-2,3-glyoxalidine also [2,1-b] _ azoles joins in 3ml trifluoroacetic acid and the 3ml methylene dichloride, succeeded by at room temperature stirring 1 hour.Then, under reduced pressure concentrated reaction solution is dissolved in resistates the 3ml methylene dichloride then, then to wherein adding the 3ml triethylamine.Mixture was at room temperature stirred 5 minutes, under reduced pressure concentrate then.Resistates is dissolved in 5ml methyl alcohol, then,, uses ice-cooled simultaneously to wherein adding 0.170g 4-trifluoromethyl phenylacrolein, 82mg sodium cyanoborohydride and 0.1ml acetate.The gained mixture was at room temperature stirred 3 days.Then, to wherein adding saturated sodium bicarbonate aqueous solution.Stir the mixture, use ethyl acetate extraction, wash with saturated sodium-chloride water solution then.Organic layer through dried over mgso, is under reduced pressure concentrated then.(from methylene dichloride: acetone=3: 1 is to methylene dichloride: methyl alcohol=20: 1) through silica gel chromatography for resistates.Make products therefrom recrystallization from aqueous acetone then, obtain 66mg (yield: buff powder 18.6%), (R)-and 2-methyl-6-nitro-2-(4-(4-(4-trifluoromethyl cinnamyl) piperazine-1-yl) phenoxymethyl)-2, the 3-glyoxalidine is [2,1-b] _ azoles also.

Fusing point: 199.7 ℃-202.0 ℃

Embodiment 1492

(R)-and 2-methyl-6-nitro-2-(4-(4-(2-(4-trifluoromethyl) thiazole-4-ylmethyl) piperazine-1-yl) phenoxymethyl)-2, the 3-glyoxalidine is [2,1-b] _ azoles also

With 0.300g (R)-2-methyl-6-nitro-2-(4-(4-tert-butoxycarbonyl piperazine-1-yl) phenoxymethyl)-2,3-glyoxalidine also [2,1-b] _ azoles joins in 3ml trifluoroacetic acid and the 3ml methylene dichloride, succeeded by at room temperature stirring 2 hours.Then, concentrated reaction solution under reduced pressure.Resistates is dissolved in the 3ml methylene dichloride, then to wherein adding the 3ml triethylamine.Mixture was at room temperature stirred 10 minutes, under reduced pressure concentrate then.Resistates is dissolved in 5ml methyl alcohol, then,, uses ice-cooled simultaneously to wherein adding 0.218g 2-(4-trifluoromethyl) thiazole-4-formaldehyde, 82mg sodium cyanoborohydride and 0.5ml acetate.Mixture at room temperature stirred spend the night.Then, to wherein adding saturated sodium bicarbonate aqueous solution.Stir the mixture, use ethyl acetate extraction then, wash with saturated sodium-chloride water solution then.Organic layer through dried over mgso, is under reduced pressure concentrated then.(from methylene dichloride: acetone=3: 1 is to methylene dichloride: methyl alcohol=20: 1) through silica gel chromatography for resistates.Make products therefrom crystallization from aqueous acetone then, obtain 0.167g (yield: white powder 42.6%), (R)-and 2-methyl-6-nitro-2-(4-(4-(2-(4-trifluoromethyl) thiazole-4-ylmethyl) piperazine-1-yl) phenoxymethyl)-2, the 3-glyoxalidine is [2,1-b] _ azoles also.

Fusing point: 210.0 ℃-212.1 ℃

Embodiment 1493

(R)-and 2-(4-(4-(N-(4-chloro-phenyl-)-N-methylamino) piperidines-1-yl) phenoxymethyl)-2-methyl-6-nitro-2, the 3-glyoxalidine is [2,1-b] _ azoles also

776mg 4-(4-(N-(4-chloro-phenyl-)-N-methylamino) piperidines-1-yl) phenol is dissolved in 10ml DMF, then to wherein adding the 108mg sodium hydride, succeeded by stirring 10 minutes down at 70 ℃ to 80 ℃.Then, with reaction soln with ice-cooled, then to wherein adding 746mg (R)-2-chloro-1-(2-methyl-2-oxiranylmethyl radical)-4-nitro-1H-imidazoles, succeeded by stirring 20 minutes down at 70 ℃ to 80 ℃.Then, reaction soln is cooled to room temperature.Add frozen water to reaction soln, stir the mixture then, remove by filter infusible precipitate then.Filtrate is dissolved in methylene dichloride, with the saturated sodium-chloride water solution washing, then through dried over mgso.Leach sal epsom, under reduced pressure concentrated filtrate.Resistates is through silica gel chromatography (methylene dichloride: ethyl acetate=10: 1).Make products therefrom recrystallization from the mixed solvent of forming by methylene dichloride and ethyl acetate, obtain 485mg (yield: white powder crystal 39.8%), (R)-2-(4-(4-(N-(4-chloro-phenyl-)-N-methylamino) piperidines-1-yl) phenoxymethyl)-2-methyl-6-nitro-2, the 3-glyoxalidine is [2,1-b] _ azoles also.

Fusing point: 173.7 ℃-175.1 ℃

Embodiment 1494

(R)-and 2-methyl-6-nitro-2-(4-(4-(4-4-trifluoromethylphenopendant methyl) piperidines-1-yl) phenoxymethyl)-2, the 3-glyoxalidine is [2,1-b] _ azoles also

574mg (R)-2-chloro-1-(2-methyl-2-oxiranylmethyl radical)-4-nitro-1H-imidazoles and 844mg 4-(4-(4-4-trifluoromethylphenopendant methyl) piperidines-1-yl) phenol are heated to 140 ℃, succeeded by stirring 4 hours.Then, mixture is cooled to room temperature, mixture passes through silica gel chromatography (hexane: ethyl acetate=1: 3) then.After concentrated the finishing, resistates is dissolved in 10ml DMF.To wherein adding the 174mg sodium tert-butoxide, use ice-cooledly simultaneously, then mixture was at room temperature stirred 2 hours.Then, under reduced pressure remove and desolvate, then, add 100ml acetone and 10ml silica gel, succeeded by concentrating to resistates.Resistates is through silica gel chromatography (methylene dichloride: ethyl acetate was from 10: 1 to 1: 1).Make products therefrom recrystallization from the mixed solvent of forming by methylene dichloride and ethyl acetate, obtain 1.15g (yield: white powder 38%), (R)-2-methyl-6-nitro-2-(4-(4-(4-4-trifluoromethylphenopendant methyl) piperidines-1-yl) phenoxymethyl)-2, the 3-glyoxalidine is [2,1-b] _ azoles also.

Fusing point: 223.2 ℃-225.2 ℃ (decomposition)

Embodiment 1495

(R)-and 2-methyl-6-nitro-2-(4-(4-(4-trifluoromethyl benzyloxy methyl) piperidines-1-yl) phenoxymethyl)-2, the 3-glyoxalidine is [2,1-b] _ azoles also

2.48g 4-(4-(4-trifluoromethyl benzyloxy methyl) piperidines-1-yl) phenol is dissolved in 30mlDMF, then to wherein adding the 312mg sodium hydride, succeeded by stirring 10 minutes down at 70 ℃ to 80 ℃., then, with reaction soln with ice-cooled, then to wherein adding 2.07g (R)-2-chloro-1-(2-methyl-2-oxiranylmethyl radical)-4-nitro-1H-imidazoles, succeeded by stirring 20 minutes down at 70 ℃ to 80 ℃.Then, reaction soln is cooled to room temperature.Add frozen water to reaction soln, stir the mixture then, remove by filter infusible precipitate then.Filtrate is dissolved in methylene dichloride, with the saturated sodium-chloride water solution washing, then through dried over mgso.Leach sal epsom, under reduced pressure concentrated filtrate.Resistates is through silica gel chromatography (methylene dichloride: ethyl acetate=10: 1).Make products therefrom recrystallization from ethyl acetate then, obtain 1.66g (yield: white powder crystal 44.7%), (R)-and 2-methyl-6-nitro-2-(4-(4-(4-trifluoromethyl benzyloxy methyl) piperidines-1-yl) phenoxymethyl)-2, the 3-glyoxalidine is [2,1-b] _ azoles also.

Fusing point: 172.3 ℃-172.9 ℃

Embodiment 1496

(R)-and 2-methyl-6-nitro-2-(4-(4-(4-chloromethyl phenoxymethyl) piperidines-1-yl) phenoxymethyl)-2, the 3-glyoxalidine is [2,1-b] _ azoles also

1.09g 4-(4-(4-chloromethyl phenoxymethyl) piperidines-1-yl) phenol is dissolved in 20mlDMF, then to wherein adding the 158mg sodium hydride, succeeded by stirring 20 minutes down at 70 ℃ to 80 ℃.Then, with reaction soln with ice-cooled, then to wherein adding 1.04g (R)-2-chloro-1-(2-methyl-2-oxiranylmethyl radical)-4-nitro-1H-imidazoles, succeeded by stirring 30 minutes down at 60 ℃.Then, reaction soln is cooled to room temperature.Add frozen water to reaction soln, stir the mixture then, remove by filter infusible precipitate then.Filtrate is dissolved in methylene dichloride, with the saturated sodium-chloride water solution washing, then through dried over mgso.Leach sal epsom, under reduced pressure concentrated filtrate.Resistates is through silica gel chromatography (methylene dichloride: methyl alcohol=20: 1).Make products therefrom recrystallization from ethyl acetate then, obtain 744mg (yield: yellow powder powder crystal 43.5%), (R)-and 2-methyl-6-nitro-2-(4-(4-(4-chloromethyl phenoxymethyl) piperidines-1-yl) phenoxymethyl)-2, the 3-glyoxalidine is [2,1-b] _ azoles also.

Fusing point: 140.4 ℃-141.7 ℃

Embodiment 1497

(R)-and 6-nitro-2-(4-(4-(4-4-trifluoromethylphenopendant methyl) piperidines-1-yl) phenoxymethyl)-2, the 3-glyoxalidine is [2,1-b] _ azoles also

1.22g 4-(4-(4-4-trifluoromethylphenopendant methyl) piperidines-1-yl) phenol is dissolved in 15mlDMF, then to wherein adding the 196mg sodium hydride, succeeded by stirring 30 minutes down at 70 ℃ to 80 ℃.Then, with reaction soln with ice-cooled, then to wherein adding 1.57g (R)-2-chloro-1-oxiranylmethyl radical-4-nitro-1H-imidazoles, succeeded by stirring 20 minutes down at 80 ℃.Then, reaction soln is cooled to room temperature.Add frozen water to reaction soln, stir the mixture then, remove by filter infusible precipitate then.Filtrate is dissolved in methylene dichloride, with the saturated sodium-chloride water solution washing, then through dried over mgso.Filter sal epsom, under reduced pressure concentrated filtrate.Resistates is through silica gel chromatography (methylene dichloride: methyl alcohol=20: 1).Make products therefrom recrystallization from ethyl acetate then, obtain 505mg (yield: white powder crystal 22.1%), (R)-and 6-nitro-2-(4-(4-(4-4-trifluoromethylphenopendant methyl) piperidines-1-yl) phenoxymethyl)-2, the 3-glyoxalidine is [2,1-b] _ azoles also.

Fusing point: 175.0 ℃-180 ℃

Embodiment 1498

(R)-2-(4 '-(4-(4-benzyl chloride base) piperazine-1-yl) biphenyl-4-base oxygen ylmethyl)-2-methyl-6-nitro-2, the 3-glyoxalidine is [2,1-b] _ azoles also

With 850mg (R)-2-methyl-2-(4 '-(4-tert-butoxycarbonyl piperazine-1-yl) biphenyl-4-base oxygen ylmethyl)-6-nitro-2,3-glyoxalidine also [2,1-b] _ azoles is dissolved in 10ml trifluoroacetic acid and 5ml methylene dichloride, spends the night succeeded by at room temperature stirring.Then, concentrated reaction solution under reduced pressure, then, to wherein adding 6ml methylene dichloride and 6ml triethylamine.Mixture was at room temperature stirred 5 minutes, under reduced pressure concentrate then.Resistates is dissolved in 10ml DMF, then,, uses ice-cooledly simultaneously, spend the night succeeded by at room temperature stirring to wherein adding 444.2mg 4-chlorobenzaldehyde and 672mg sodium triacetoxy borohydride.Then, add sodium bicarbonate aqueous solution and ethyl acetate, stir the mixture, remove by filter infusible precipitate to reaction soln.With filtrate water and ethyl acetate washing, dry then, obtain 730mg (yield: buff powder 51.8%), (R)-2-(4 '-(4-(4-benzyl chloride base) piperazine-1-yl) biphenyl-4-base oxygen ylmethyl)-2-methyl-6-nitro-2, the 3-glyoxalidine is [2,1-b] _ azoles also.

Fusing point: 247.8 ℃-248.5 ℃ (decomposition)

Embodiment 1499

(R)-2-methyl-6-nitro-2-(4 '-(4-(4-trifluoromethyl benzyl) piperazine-1-yl) biphenyl-4-base oxygen ylmethyl)-2, the 3-glyoxalidine is [2,1-b] _ azoles also

With 790mg (R)-2-methyl-2-(4 '-(4-tert-butoxycarbonyl piperazine-1-yl) biphenyl-4-base oxygen ylmethyl)-6-nitro-2,3-glyoxalidine also [2,1-b] _ azoles is dissolved in 10ml trifluoroacetic acid and 5ml methylene dichloride, spends the night succeeded by at room temperature stirring.Then, concentrated reaction solution under reduced pressure, then, to wherein adding 6ml methylene dichloride and 6ml triethylamine.Mixture was at room temperature stirred 5 minutes, under reduced pressure concentrate then.Resistates is dissolved in 15ml DMF, then,, uses ice-cooledly simultaneously, spend the night succeeded by at room temperature stirring to wherein adding 0.4ml 4-trifluoromethylated benzaldehyde and 625mg sodium triacetoxy borohydride.Then, add entry, stir the mixture, remove by filter infusible precipitate to reaction soln.With the filtrate water washing, be dissolved in methylene dichloride then.Gained solution is washed with saturated sodium-chloride water solution, then through dried over sodium sulfate.Filter sodium sulfate, under reduced pressure concentrated filtrate.Resistates is through silica gel chromatography (methylene dichloride: methyl alcohol=20: 1).Make products therefrom recrystallization from the mixed solvent of forming by methylene dichloride and ethyl acetate, obtain 585mg (yield: buff powder 60.5%), (R)-2-methyl-6-nitro-2-(4 '-(4-(4-trifluoromethyl benzyl) piperazine-1-yl) biphenyl-4-base oxygen ylmethyl)-2, the 3-glyoxalidine is [2,1-b] _ azoles also.

Fusing point: 247.7 ℃-248.4 ℃ (decomposition)

Embodiment 1500

(R)-and 2-methyl-6-nitro-2-(4-(4-(2-(4-trifluoromethoxy benzyloxy) ethyl) piperidines-1-yl) phenoxymethyl)-2, the 3-glyoxalidine is [2,1-b] _ azoles also

959mg (R)-2-chloro-1-(2-methyl-2-oxiranylmethyl radical)-4-nitro-1H-imidazoles and 1.24g 4-(4-(2-(4-trifluoromethoxy benzyloxy) ethyl) piperidines-1-yl) phenol are dissolved in 20ml DMF, then to wherein adding the 176mg sodium hydride, succeeded by stirring 1 hour down at 55 ℃.Then, the temperature with reaction soln is cooled to room temperature.Add frozen water to reaction soln, stir the mixture then, remove by filter infusible precipitate then.Filtrate is dissolved in methylene dichloride, with the saturated sodium-chloride water solution washing, then through dried over mgso.Leach sal epsom, under reduced pressure concentrated filtrate.Resistates is through silica gel chromatography (methylene dichloride: ethyl acetate=10: 1).Make products therefrom recrystallization from the mixed solvent of forming by methylene dichloride and ethyl acetate, obtain 562mg (yield: white powder crystal 28.8%), (R)-2-methyl-6-nitro-2-(4-(4-(2-(4-trifluoromethoxy benzyloxy) ethyl) piperidines-1-yl) phenoxymethyl)-2, the 3-glyoxalidine is [2,1-b] _ azoles also.

Fusing point: 204.8 ℃-206.7 ℃

Embodiment 1501

(R)-and 2-methyl-6-nitro-2-(4-(4-(2-(4-trifluoromethyl benzyloxy) ethyl) piperidines-1-yl) phenoxymethyl)-2, the 3-glyoxalidine is [2,1-b] _ azoles also

741mg (R)-2-chloro-1-(2-methyl-2-oxiranylmethyl radical)-4-nitro-1H-imidazoles and 1.00g 4-(4-(2-(4-trifluoromethyl benzyloxy) ethyl) piperidines-1-yl) phenol are dissolved in 10ml DMF, then to wherein adding the 136mg sodium hydride, succeeded by stirring 1 hour down at 55 ℃.Then, reaction soln is cooled to room temperature.Add frozen water to reaction soln, stir the mixture then, remove by filter infusible precipitate then.Filtrate is dissolved in methylene dichloride, with the saturated sodium-chloride water solution washing, then through dried over mgso.Filter sal epsom, under reduced pressure concentrated filtrate.Resistates is through silica gel chromatography (methylene dichloride: ethyl acetate=10: 1).Make products therefrom recrystallization from the mixed solvent of forming by methylene dichloride and ethyl acetate, obtain 548mg (yield: white powder crystal 37.3%), (R)-2-methyl-6-nitro-2-(4-(4-(2-(4-trifluoromethyl benzyloxy) ethyl) piperidines-1-yl) phenoxymethyl)-2, the 3-glyoxalidine is [2,1-b] _ azoles also.

Fusing point: 198.0 ℃-199.2 ℃

Embodiment 1502

(R)-and 2-(4-(4-(2-(4-chlorine benzyloxy) ethyl) piperidines-1-yl) phenoxymethyl)-2-methyl-6-nitro-2, the 3-glyoxalidine is [2,1-b] _ azoles also

900mg (R)-2-chloro-1-(2-methyl-2-oxiranylmethyl radical)-4-nitro-1H-imidazoles and 1.10g 4-(4-(2-(4-chlorine benzyloxy) ethyl) piperidines-1-yl) phenol are dissolved in 10ml DMF, then to wherein adding the 165mg sodium hydride, succeeded by stirring 1 hour down at 55 ℃.Then, reaction soln is cooled to room temperature.Add frozen water to reaction soln, stir the mixture then, remove by filter infusible precipitate then.Filtrate is dissolved in methylene dichloride, with the saturated sodium-chloride water solution washing, then through dried over mgso.Leach sal epsom, under reduced pressure concentrated filtrate.Resistates is through silica gel chromatography (methylene dichloride: ethyl acetate=10: 1).Make products therefrom recrystallization from the mixed solvent of forming by methylene dichloride and ethyl acetate, obtain 548mg (yield: white powder crystal 37.3%), (R)-2-(4-(4-(2-(4-chlorine benzyloxy) ethyl) piperidines-1-yl) phenoxymethyl)-2-methyl-6-nitro-2, the 3-glyoxalidine is [2,1-b] _ azoles also.

Fusing point: 197.6 ℃-198.2 ℃

Embodiment 1503

(R)-and 2-methyl-6-nitro-2-(4-(4-(4-(4-(4-Trifluoromethyl phenyl ether oxygen base) piperidines-1-yl) benzyl) piperazine-1-yl) phenoxymethyl)-2, the 3-glyoxalidine is [2,1-b] _ azoles also

With 350mg (R)-2-methyl-2-(4-(4-tert-butoxycarbonyl piperazine-1-yl) phenoxymethyl)-6-nitro-2,3-glyoxalidine also [2,1-b] _ azoles is dissolved in the 10ml trifluoroacetic acid, succeeded by at room temperature stirring 5 hours.Then, concentrated reaction solution under reduced pressure, then, to wherein adding 2ml methylene dichloride and 2ml triethylamine.Mixture was at room temperature stirred 5 minutes, under reduced pressure concentrate then.Resistates is dissolved in the 10ml ethylene dichloride, then,, uses ice-cooledly simultaneously, spend the night succeeded by at room temperature stirring to wherein adding 278mg 4-(4-(4-Trifluoromethyl phenyl ether oxygen base) piperidines-1-yl) phenyl aldehyde and 242mg sodium triacetoxy borohydride.Then, add sodium bicarbonate aqueous solution, use dichloromethane extraction then to reaction soln.Extraction liquid is washed with saturated sodium-chloride water solution, then through dried over mgso.Leach sal epsom, under reduced pressure concentrated filtrate.Resistates is through silica gel chromatography (methylene dichloride: ethyl acetate=10: 1).Make products therefrom recrystallization from the mixed solvent of forming by methylene dichloride and diisopropyl ether then, obtain 295mg (yield: buff powder 55%), (R)-2-methyl-6-nitro-2-(4-(4-(4-(4-(4-Trifluoromethyl phenyl ether oxygen base) piperidines-1-yl) benzyl) piperazine-1-yl) phenoxymethyl)-2, the 3-glyoxalidine is [2,1-b] _ azoles also.

Fusing point: 198.2 ℃-201.4 ℃

Embodiment 1504

(R)-2-(4 '-(4-(3, the 4-dichloro benzyl) piperazine-1-yl) biphenyl-4-base oxygen ylmethyl)-2-methyl-6-nitro-2, the 3-glyoxalidine is [2,1-b] _ azoles also

With 350mg (R)-2-methyl-2-(4 '-(4-tert-butoxycarbonyl piperazine-1-yl) biphenyl-4-base oxygen ylmethyl)-6-nitro-2,3-glyoxalidine also [2,1-b] _ azoles is dissolved in the 10ml trifluoroacetic acid, succeeded by at room temperature stirring 5 hours.Then, concentrated reaction solution under reduced pressure, then, to wherein adding 2ml methylene dichloride and 2ml triethylamine.Mixture was at room temperature stirred 5 minutes, under reduced pressure concentrate then.Resistates is dissolved in the 10ml ethylene dichloride, and then, to wherein adding 278mg 3,4-dichlorobenzaldehyde and 242mg sodium triacetoxy borohydride are used ice-cooledly simultaneously, spend the night succeeded by at room temperature stirring.Then, add entry, stir the mixture, remove by filter infusible precipitate to reaction soln.Filtrate is dissolved in methylene dichloride.Solution is washed with saturated sodium-chloride water solution, then through dried over mgso.Leach sal epsom, under reduced pressure concentrated filtrate.Resistates is through silica gel chromatography (methylene dichloride: methyl alcohol=20: 1) obtain 252mg (yield: buff powder 41.1%), (R)-2-(4 '-(4-(3, the 4-dichloro benzyl) biphenyl-4-base oxygen ylmethyl piperazine-1-yl))-2-methyl-6-nitro-2, the 3-glyoxalidine is [2,1-b] _ azoles also.

Fusing point: 222.6 ℃-225.1 ℃ (decomposition)

Embodiment 1505

(R)-and 2-methyl-6-nitro-2-(4-(4-(4-(4-Trifluoromethyl phenyl ether oxygen base) phenyl amino) piperidines-1-yl) phenoxymethyl)-2, the 3-glyoxalidine is [2,1-b] _ azoles also

376mg 4-(4-Trifluoromethyl phenyl ether oxygen base) aniline and 453mg sodium triacetoxy borohydride joined contain 400mg (R)-2-methyl-6-nitro-2-(4-(4-oxo-piperidine-1-yl) phenoxymethyl)-2, the 3-glyoxalidine is also in the dichloroethane solution (10ml) of [2,1-b] _ azoles.Mixture at room temperature stirred spend the night.Then, add saturated sodium bicarbonate aqueous solution to reaction soln, succeeded by extracting repeatedly with methylene dichloride.Organic layer through dried over mgso, is filtered then.Concentrated filtrate under reduced pressure, resistates is through silica gel chromatography (methylene dichloride: methyl alcohol=20: 1).Make products therefrom recrystallization from the mixed solvent of forming by methylene dichloride and diisopropyl ether, obtain 650mg (yield: white powder 83.2%), (R)-2-methyl-6-nitro-2-(4-(4-(4-(4-Trifluoromethyl phenyl ether oxygen base) phenyl amino) piperidines-1-yl) phenoxymethyl)-2, the 3-glyoxalidine is [2,1-b] _ azoles also.

Fusing point: 198.6 ℃-201.1 ℃ (decomposition)

Embodiment 1506

(R)-and 2-methyl-6-nitro-2-(4-(4-(N-methyl-N-(3-(4-Trifluoromethyl phenyl ether oxygen base) propyl group) amino) piperidines-1-yl) phenoxymethyl)-2, the 3-glyoxalidine is [2,1-b] _ azoles also

With 237mg (R)-2-methyl-6-nitro-2-(4-(4-(3-(4-Trifluoromethyl phenyl ether oxygen base) propyl group amino) piperidines-1-yl) phenoxymethyl)-2,3-glyoxalidine also [2,1-b] _ azoles is dissolved in the mixed solvent of being made up of 10ml methylene dichloride and 10ml methyl alcohol.Then, add 0.15ml30% formalin, 71.4mg sodium cyanoborohydride and 0.01ml acetate, spend the night succeeded by at room temperature stirring to mixture.Then, add saturated sodium bicarbonate aqueous solution to reaction soln, succeeded by extracting repeatedly with methylene dichloride.Organic layer through dried over mgso, is filtered then.Concentrated filtrate under reduced pressure, resistates is through silica gel chromatography (methylene dichloride: methyl alcohol=20: 1).Make products therefrom recrystallization from the mixed solvent of forming by methylene dichloride and diisopropyl ether, obtain 215mg (yield: fine yellow powder 88.7%), (R)-2-methyl-6-nitro-2-(4-(4-(N-methyl-N-(3-(4-Trifluoromethyl phenyl ether oxygen base) propyl group) amino) piperidines-1-yl) phenoxymethyl)-2, the 3-glyoxalidine is [2,1-b] _ azoles also.

Fusing point: 167.4 ℃-170.2 ℃

Embodiment 1507

(R)-and 2-(4-(4-(3,4-dichlorophenyl amino) piperidines-1-yl) phenoxymethyl)-2-methyl-6-nitro-2, the 3-glyoxalidine is [2,1-b] _ azoles also

(4-(3 with 628mg (R)-2-chloro-1-(2-methyl-2-oxiranylmethyl radical)-4-nitro-1H-imidazoles and 750mg 4-, 4-dichlorophenyl amino) piperidines-1-yl) phenol is dissolved in 10ml DMF, then, to wherein adding the 117mg sodium hydride, succeeded by stirring 20 minutes down at 60 ℃.Then, reaction soln is cooled to room temperature.Add entry to reaction soln, remove by filter infusible precipitate then.Filtrate is dissolved in methylene dichloride, with the saturated sodium-chloride water solution washing, then through dried over mgso.Leach sal epsom, under reduced pressure concentrated filtrate.Resistates through silica gel chromatography (from methylene dichloride: ethyl acetate=9: 1 to 8: 2).Make products therefrom recrystallization from the mixed solvent of forming by methylene dichloride and diisopropyl ether then, obtain 441mg (yield: yellow powder powder crystal 39%), (R)-((4-(3 for 4-for 2-, 4-dichlorophenyl amino) phenoxymethyl piperidines-1-yl))-2-methyl-6-nitro-2, the 3-glyoxalidine is [2,1-b] _ azoles also.

Fusing point: 146 ℃-147.4 ℃

Embodiment 1508

(R)-and 2-methyl-6-nitro-2-(4-(4-(N-methyl-N-(2-(4-Trifluoromethyl phenyl ether oxygen base) ethyl) amino) piperidines-1-yl) phenoxymethyl)-2, the 3-glyoxalidine is [2,1-b] _ azoles also

With 200mg (R)-2-methyl-6-nitro-2-(4-(4-(2-(4-Trifluoromethyl phenyl ether oxygen base) ethylamino) piperidines-1-yl) phenoxymethyl)-2,3-glyoxalidine also [2,1-b] _ azoles is dissolved in the mixed solvent of being made up of 2ml methylene dichloride and 2ml methyl alcohol.Then, add 0.13ml 30% formalin, 65mg sodium cyanoborohydride and 0.07ml acetate, spend the night succeeded by at room temperature stirring to mixture.Then, add saturated sodium bicarbonate aqueous solution to reaction soln, succeeded by extracting repeatedly with methylene dichloride.Organic layer through dried over mgso, is filtered then.Concentrated filtrate under reduced pressure, resistates is through silica gel chromatography (methylene dichloride: methyl alcohol=20: 1).Make products therefrom recrystallization from the mixed solvent of forming by methylene dichloride and diisopropyl ether, obtain 155mg (yield: white powder 75.7%), (R)-2-methyl-6-nitro-2-(4-(4-(N-methyl-N-(2-(4-Trifluoromethyl phenyl ether oxygen base) ethyl) amino) piperidines-1-yl) phenoxymethyl)-2, the 3-glyoxalidine is [2,1-b] _ azoles also.

Fusing point: 185.7 ℃-187.7 ℃

Embodiment 1509

(R)-and 2-methyl-6-nitro-2-(4-(4-(4-(4-Trifluoromethoxyphen-l) piperazine-1-yl) piperidines-1-yl) phenoxymethyl)-2, the 3-glyoxalidine is [2,1-b] _ azoles also

145mg 1-Trifluoromethoxyphen-l piperazine, 273mg sodium triacetoxy borohydride and 0.061ml acetate joined contain 200mg (R)-2-methyl-6-nitro-2-(4-(4-oxo-piperidine-1-yl) phenoxymethyl)-2,3-glyoxalidine also [2,1-b] _ acetonitrile solution (15ml) of azoles in, succeeded by at room temperature stirring 11 days.Then, add saturated sodium bicarbonate aqueous solution to reaction soln, succeeded by extracting repeatedly with methylene dichloride.Organic layer through dried over mgso, is filtered then.Concentrated filtrate under reduced pressure, resistates is through silica gel chromatography (methylene dichloride: methyl alcohol=20: 1).Make products therefrom recrystallization from Virahol, obtain 143mg (yield: white powder 44.2%), (R)-and 2-methyl-6-nitro-2-(4-(4-(4-(4-Trifluoromethoxyphen-l) piperazine-1-yl) piperidines-1-yl) phenoxymethyl)-2, the 3-glyoxalidine is [2,1-b] _ azoles also.

Fusing point: 279 ℃-281 ℃

Embodiment 1510

(R)-and 2-(4-(4-(3,5-dichlorophenyl amino) piperidines-1-yl) phenoxymethyl)-2-methyl-6-nitro-2, the 3-glyoxalidine is [2,1-b] _ azoles also

(4-(3 with 1.82g (R)-2-chloro-1-(2-methyl-2-oxiranylmethyl radical)-4-nitro-1H-imidazoles and 2.02g 4-, 5-dichlorophenyl amino) piperidines-1-yl) phenol is dissolved in 20ml DMF, then, to wherein adding the 264mg sodium hydride, succeeded by stirring 20 minutes down at 60 ℃.Then, reaction soln is cooled to room temperature.Add entry and ethyl acetate to reaction soln, stir the mixture, remove by filter infusible precipitate then.Filtrate is dissolved in methylene dichloride, with the saturated sodium-chloride water solution washing, then through dried over mgso.Leach sal epsom, under reduced pressure concentrated filtrate.(from methylene dichloride: ethyl acetate=9: 1 is to methylene dichloride: methyl alcohol=20: 1) through silica gel chromatography for resistates.Make products therefrom recrystallization from the mixed solvent of forming by ethyl acetate and diethyl ether then, obtain 1.19g (yield: yellow powder powder crystal 38%), (R)-((4-(3 for 4-for 2-, 5-dichlorophenyl amino) phenoxymethyl piperidines-1-yl))-2-methyl-6-nitro-2, the 3-glyoxalidine is [2,1-b] _ azoles also.

Fusing point: 122 ℃-124 ℃

Embodiment 1511

(R)-and 2-(4-(4-(4-(4-chloro-phenyl-) piperazine-1-yl) piperidines-1-yl) phenoxymethyl)-2-methyl-6-nitro-2, the 3-glyoxalidine is [2,1-b] _ azoles also

10ml 20% aqueous sodium carbonate is joined in the aqueous solution (10ml) that contains 290mg 1-(4-chloro-phenyl-) piperazine dihydrochloride, then, to mixture using ultrasound ripple.With the products therefrom dichloromethane extraction, through dried over sodium sulfate.Then, under reduced pressure except that desolvating.Resistates is dissolved in the 15ml ethylene dichloride.Then, add 200mg (R)-2-methyl-6-nitro-2-(4-(4-oxo-piperidine-1-yl) phenoxymethyl)-2 to mixture, the 3-glyoxalidine is [2,1-b] _ azoles, 341ml sodium triacetoxy borohydride and 0.092ml acetate also, succeeded by at room temperature stirring 24 hours.Then, add 20% aqueous sodium carbonate, then enriched mixture under reduced pressure to reaction soln.Add entry to resistates, filter and collect infusible precipitate.Precipitation is washed with water, dry then.Make products therefrom recrystallization from Virahol then, obtain 232mg (yield: buff powder 78.1%), (R)-and 2-(4-(4-(4-(4-chloro-phenyl-) piperazine-1-yl) piperidines-1-yl) phenoxymethyl)-2-methyl-6-nitro-2, the 3-glyoxalidine is [2,1-b] _ azoles also.

Fusing point: 247 ℃-249 ℃

Embodiment 1512

(R)-and 2-methyl-2-(4-(4-(4-(N-methyl-N-(4-chloro-phenyl-) amino) piperidines-1-yl) piperidines-1-yl) phenoxymethyl)-6-nitro-2, the 3-glyoxalidine is [2,1-b] _ azoles also

241mg 4-(N-methyl-N-(4-chloro-phenyl-) amino) piperidines, 341mg sodium triacetoxy borohydride and 0.092ml acetate joined contain 200mg (R)-2-methyl-6-nitro-2-(4-(4-oxo-piperidine-1-yl) phenoxymethyl)-2, the 3-glyoxalidine is also in the dichloroethane solution (15ml) of [2,1-b] _ azoles.Mixture was at room temperature stirred 20 hours.Then, add 20% aqueous sodium carbonate, succeeded by extracting repeatedly with methylene dichloride to reaction soln.Organic layer through dried over sodium sulfate, is filtered then.Concentrated filtrate under reduced pressure, resistates is through silica gel chromatography (methylene dichloride: methyl alcohol=20: 1).Make products therefrom recrystallization from the mixed solvent of forming by methylene dichloride and diethyl ether then, obtain 105mg (yield: white powder 33.6%), (R)-2-methyl-2-(4-(4-(4-(N-methyl-N-(4-chloro-phenyl-) amino) piperidines-1-yl) piperidines-1-yl) phenoxymethyl)-6-nitro-2, the 3-glyoxalidine is [2,1-b] _ azoles also.

Fusing point: 230.8 ℃-232 ℃

Embodiment 1513

(R)-and 2-methyl-2-(4-(4-(4-(N-methyl-N-(4-Trifluoromethoxyphen-l) amino) piperidines-1-yl) piperidines-1-yl) phenoxymethyl)-6-nitro-2, the 3-glyoxalidine is [2,1-b] _ azoles also

283mg 4-(N-methyl-N-(4-Trifluoromethoxyphen-l) amino) piperidines, 328mg sodium triacetoxy borohydride and 0.089ml acetate joined contain 192mg (R)-2-methyl-6-nitro-2-(4-(4-oxo-piperidine-1-yl) phenoxymethyl)-2,3-glyoxalidine also [2,1-b] _ dichloroethane solution (15ml) of azoles in, succeeded by at room temperature stirring 14 hours.Then, add 20% aqueous sodium carbonate, succeeded by extracting repeatedly with methylene dichloride to reaction soln.Organic layer through dried over sodium sulfate, is filtered then.Concentrated filtrate under reduced pressure, resistates is through silica gel chromatography (methylene dichloride: methyl alcohol=20: 1).Make products therefrom recrystallization from the mixed solvent of forming by methylene dichloride and diethyl ether, obtain 153mg (yield: yellow powder 47.1%), (R)-2-methyl-2-(4-(4-(4-(N-methyl-N-(4-Trifluoromethoxyphen-l) amino) piperidines-1-yl) piperidines-1-yl) phenoxymethyl)-6-nitro-2, the 3-glyoxalidine is [2,1-b] _ azoles also.

Fusing point: 196 ℃-197 ℃

Embodiment 1514

(R)-and 2-(4-(4-(4-propyl group phenyl amino) piperidines-1-yl) phenoxymethyl)-2-methyl-6-nitro-2, the 3-glyoxalidine is [2,1-b] _ azoles also

1.86g (R)-2-chloro-1-(2-methyl-2-oxiranylmethyl radical)-4-nitro-1H-imidazoles and 1.9g 4-(4-(4-propyl group phenyl amino) piperidines-1-yl) phenol are dissolved in 20ml DMF, then, to wherein adding the 269mg sodium hydride, succeeded by stirring 2 hours down at 50 ℃.Then, reaction soln is cooled to room temperature.To wherein adding entry and ethyl acetate, stir the mixture, remove by filter infusible precipitate then.Filtrate is dissolved in methylene dichloride, with the saturated sodium-chloride water solution washing, then through dried over mgso.Leach sal epsom, under reduced pressure concentrated filtrate.(from methylene dichloride: ethyl acetate=9: 1 is to methylene dichloride: methyl alcohol=20: 1) through silica gel chromatography for resistates.Make products therefrom recrystallization from the mixed solvent of forming by ethyl acetate and diisopropyl ether then, obtain 660mg (yield: yellow powder powder crystal 21.9%), (R)-2-(4-(4-(4-propyl group phenyl amino) piperidines-1-yl) phenoxymethyl)-2-methyl-6-nitro-2, the 3-glyoxalidine is [2,1-b] _ azoles also.

Fusing point: 222 ℃-223 ℃

Embodiment 1515

(R)-and 2-(4-(4-(N-methyl-N-(4-propyl group phenyl) amino) piperidines-1-yl) phenoxymethyl)-2-methyl-6-nitro-2, the 3-glyoxalidine is [2,1-b] _ azoles also

With 300mg (R)-2-(4-(4-(4-propyl group phenyl amino) piperidines-1-yl) phenoxymethyl)-2-methyl-6-nitro-2,3-glyoxalidine also [2,1-b] _ azoles is dissolved in the mixed solvent of being made up of 4ml methylene dichloride and 4ml methyl alcohol.Then, add 0.14ml 30% formalin, 115mg sodium cyanoborohydride and 0.1ml acetate, spend the night succeeded by at room temperature stirring to mixture.Then, add 20% aqueous sodium carbonate, succeeded by extracting repeatedly with methylene dichloride to reaction soln.Organic layer through dried over mgso, is filtered then.Concentrated filtrate under reduced pressure, resistates is through silica gel chromatography (methylene dichloride: methyl alcohol=40: 1).Make products therefrom recrystallization from the mixed solvent of forming by ethyl acetate and diisopropyl ether, obtain 258mg (yield: fine yellow powder 83.6%), (R)-2-(4-(4-(N-methyl-N-(4-propyl group phenyl) amino) piperidines-1-yl) phenoxymethyl)-2-methyl-6-nitro-2, the 3-glyoxalidine is [2,1-b] _ azoles also.

Fusing point: 198 ℃-199 ℃

Test example 1

Antibacterial tests (agar-plate dilution method)

Be determined at sample 129 gained 2 in the 7H11 substratum (BBL Co.), also [2,1-b] _ azoles is right for 3-dihydro-6-nitroimidazole Mycobacterium tuberculosis H37RvMinimum inhibition concentration.Bacterial suspension by this microbial culture is prepared bacterial strain uses therefor in 7H9 substratum (BBL Co.) in advance is succeeded by calculating viable count and-80 ℃ of following cryopreservations.The final viable count of prepared product is approximately 10 ⁶CFU/ml.5-μ L bacterial suspension is joined in the 7H11 nutrient agar that contains test compound, cultivated 14 days down, measure minimum inhibition concentration then at 37 ℃.

Right Mycobacterium tuberculosis H37RvMinimum inhibition concentration be 0.0015 μ g/mL.

Test example 2

Antibacterial tests (agar-plate dilution method)

With regard to test compound as shown in the table, it is right to be determined in the 7H11 substratum (BBL Co.) Mycobacterium tuberculosis KuronoMinimum inhibition concentration.Bacterial suspension by this microbial culture is prepared bacterial strain uses therefor in 7H9 substratum (BBL Co.) in advance is succeeded by calculating viable count and-80 ℃ of following cryopreservations.The final viable count of prepared product is approximately 10 ⁶CFU/ml.5-μ L bacterial suspension is joined in the 7H11 nutrient agar that contains test compound, cultivated 14 days down, measure minimum inhibition concentration then at 37 ℃.

The result is shown in following table 183.

[table 183]

Test compound	Minimum inhibition concentration (μ g/ml)
Test compound	Minimum inhibition concentration (μ g/ml)	Compound of Example 1 Compound of Example 8 Example 9 Example 30 Compound Compound Compound of Example 31 Example 34 Example 86 Compound Compound Compound Example 88 Example 99 Compound of Example 102 Compound 105 Compound Example Example Example 107 Compound Compound Example 108 Example 115 Compound 109 Compound 132 Compound Example Example Example 134 Compound 178 Compound 145 Compound Example Example Example 211 Compound 185 Compound 214 Compound Example Example Example 225 Compound 222 Compound 230 Compound Example Example 240 Compound 324 Compound Example Example Example 325 Compound 326 Compound 327 Compound Example Example Example 330 Compound 335 Compound 331 Compound Example Example Example 337 Compound 336 Compound 338 Compound Example...	0.2 0.006 0.012 0.003 0.003 0.024 0.006 0.024 0.0015 0.0015 0.012 0.024 0.0015 0.024 0.003 0.003 0.006 0.024 0.024 0.024 0.024 0.024 0.024 0.024 0.012 0.024 0.024 0.012 ＜0.012 0.012 0.012 0.024 0.012 0.024 ＜0.12 0.024

Example Example 339 Compound 341 Compound 340 Compound Example Example Example 345 Compound 344 Compound 346 Compound Example Example Example 349 Compound 359 Compound 349 Compound Example Example Example 368 Compound 362 Compound 369 Compound Example Example Example 371 Compound 370 Compound 373 Compound Example Example Example 382 Compound 377 Compound 384 Compound Example Example Example 385 Compound 388 Compound 389 Compound Example Example Example 390 Compound 392 Compound 393 Compound Example compound of Example 396 Example 408 Compound 422 Compound Example Example Example 439 Compound 426 Compound 440 Compound Example Example Example 473 Compound 471 Compound 480 Compound Example Example Example 487 Compound 483 Compound 488 Compound Example...

0.006 0.024 0.006 0.006 0.012 0.024 ＜0.012 0.012 0.012 0.012 0.024 0.006 0.012 0.006 0.012 0.024 0.024 0.024 0.024 0.012 0.012 0.012 ＜0.008 0.024 0.012 0.024 0.024 0.024 0.39 0.05 0.024 0.024 0.024 0.024 0.024 0.024

Embodiment 508 compound embodiment 519 compound embodiment 530 compound embodiment 602 compound embodiment 612 compound embodiment 614 compound embodiment 646 compound embodiment 647 compound embodiment 648 compound embodiment 660 compound embodiment 663 compound embodiment 664 compound embodiment 665 compound embodiment 679 compound embodiment 694 compound embodiment 695 compound embodiment 698 compound embodiment 721 compound embodiment 738 compound embodiment 739 compound embodiment 756 compound embodiment 761 compound embodiment 768 compound embodiment 753 compound embodiment 780 compounds

0.05 0.024 0.012 0.024 0.024 0.024 0.012 0.024 0.024 0.024 0.05 0.024 0.024 0.024 0.1 0.024 0.012 0.024 0.003 0.012 0.05 0.78 0.012 0.024 0.006

Claims

1. by 2 of following general formula (I) representative, 3-dihydro-6-nitroimidazole is acceptable salt on [2,1-b] _ azole compounds, its optically active form or its pharmacology also:

R wherein ¹Represent hydrogen atom or C1-C6 alkyl,

N represents the integer between 0 and 6,

R ¹With-(CH ₂) _nR ²Can constitute volution each other with they adjacent carbon atom combinations by general formula (30) representative:

Wherein RRR represents piperidyl [wherein on this piperidine ring, can be substituted with at least one phenoxy group (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group)]

R ²Represent following (a) to (y) any described group:

(a) phenyl is (wherein on this benzyl ring, can be substituted with at least one piperidyl [wherein on this piperidine ring, can be substituted with at least one phenoxy group (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group)]);

(b) benzothiazole oxygen base (wherein on this benzothiazole ring, can be substituted with at least one group, it is selected from the group of being made up of to (b-5) following (b-1):

(b-1) phenyl [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group],

(c) quinoline oxy (wherein on this quinoline ring, can be substituted with at least one group, it is selected from the group of being made up of to (c-4) following (c-1):

(c-1) halogen atom,

(d) pyridyloxy (wherein on this pyridine ring, can be substituted with at least one group, it is selected from by following (d-1) and the group (d-2) formed:

(m) 1,2,3, the 4-tetrahydro isoquinolyl (wherein this 1,2,3, on the 4-tetrahydroisoquinoline ring, can be substituted with at least one group, it is selected from by following (m-1) and the group (m-2) formed:

(n) piperidyl (wherein on this piperidine ring, can be substituted with at least one group, it is selected from the group of being made up of to (n-4) following (n-1):

(p) thiazolyl C1-C6 alkoxyl group (wherein on this thiazole ring, can be substituted with the group of at least a type, it is selected from the group of being made up of to (p-5) following (p-1):

(r) group of representing by following chemical formula (31):

[wherein X represents halogen atom, perhaps can have the C1-C6 alkyl as the substituent C1-C6 alkyl that is replaced by amino, and m represents the integer between 0 and 3, R ³Represent any one described group in following (i) to (xxii):

(i) o-NR of group-(W) ⁴R ⁵(wherein W representative-CO-or C1-C6 alkylidene group, o represents 0 or 1, R ⁴Represent hydrogen atom, C1-C6 alkyl or phenyl carbamyl [wherein on this benzyl ring; can be substituted with at least one group; it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group], R ⁵Representative: phenyl C1-C6 alkoxy carbonyl [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group]; Phenyl C2-C6 alkenyl carbonyl [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group]; Phenyl C2-C6 thiazolinyl [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group]; Piperidyl C1-C6 alkyl is [wherein on this piperidine ring, can be substituted with at least one phenyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group)]; Phenyl C1-C6 alkyl is (wherein on this benzyl ring, be substituted with at least one phenyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group)); Benzofuryl C1-C6 alkyl (wherein on this cumarone ring, can be substituted with at least one halogen and replace or unsubstituted C1-C6 alkyl); Piperidinyl carbonyl C1-C6 alkyl is [wherein on this piperidine ring, can be substituted with at least one phenoxy group (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group); Perhaps by the group of following chemical formula (32) representative:

R wherein ⁶Representative: C1-C6 alkyl; Phenyl is (wherein on this benzyl ring, can be substituted with the group that at least one is selected from following groups: the C1-C4 alkylene dioxo base, cyano group, nitro, can have the C1-C6 alkyl as substituent amino, can have the C1-C6 alkyl as the substituent alkylsulfonyl that is replaced by amino, the C1-C6 alkoxy carbonyl, the C1-C6 alkylthio, phenoxy group, phenyl C1-C6 alkoxyl group, pyrrolidyl [wherein on this pyrrolidine ring, can be substituted with at least one oxo base], imidazolyl, different _ the azoles base, _ azoles base, phenyl C1-C6 alkyl, phenyl, can have the C1-C6 alkyl as substituent amino C1-C6 alkyl, pyrrolidyl C1-C6 alkoxyl group, halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replacement or unsubstituted C1-C6 alkoxyl group); Phenyl C1-C6 alkoxy carbonyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group); Benzofuryl C1-C6 alkyl (wherein on this cumarone ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group); Benzofuryl C2-C6 thiazolinyl (wherein on this cumarone ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group); Phenoxy group C1-C6 alkyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group); Thiazolyl C1-C6 alkyl is (wherein on this thiazole ring, can be substituted with at least one phenyl [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group]); Phenyl C1-C6 alkyl is [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by phenyl (wherein on this benzyl ring, can be substituted with halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and halogen and replace or unsubstituted C1-C6 alkoxyl group), halogen atom, halogen replaces or the group of unsubstituted C1-C6 alkyl and halogen replacement or unsubstituted C1-C6 alkoxyl group composition]; Pyridyl C1-C6 alkyl is [wherein on this pyridine ring, can be substituted with at least one phenyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group)]; The C1-C6 alkoxy carbonyl; Benzoyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group); Phenylamino formyl radical (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group); Benzothienyl C1-C6 alkyl (wherein on this thionaphthene ring, can be substituted with at least one halogen atom); Indyl C1-C6 alkyl (wherein on this indole ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group); 4H-1,3-benzo two _ Ying Ji (wherein at this 4H-1,3-benzo two _ Ying Huanshang can be substituted with at least one halogen atom); Benzothienyl; Naphthyl; Quinolyl; Benzothiazolyl (wherein on this benzothiazole oxygen base, can be substituted with at least one C1-C6 alkyl); 2,3-dihydro-1H-indenyl (wherein this 2, on 3-dihydro-1H-indenes ring, can be substituted with at least one oxo base); Perhaps 9H-fluorenyl or phenyl C2-C6 thiazolinyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group));

(ii) by the group of following chemical formula (33) representative:

(4) o-NR of group-(W) ⁹R ¹⁰

(wherein W and o are same as described above,

R ⁹And R ¹⁰Represent: hydrogen atom separately identical or differently; Can have hydroxyl as substituent C1-C6 alkyl; The C1-C6 alkyloyl; The C1-C6 alkoxy carbonyl; Phenyl C1-C6 alkoxy carbonyl [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group]; Phenyl is [on this benzyl ring; can be substituted with at least one group that is selected from following groups as substituting group: halogen atom; halogen replaces or unsubstituted C1-C6 alkyl; halogen replaces or unsubstituted C1-C6 alkoxyl group; can have be selected from C1-C6 alkyloyl and C1-C6 alkyl group as substituent amino; the C1-C6 alkoxy carbonyl; phenyl; phenoxy group is (wherein on this benzyl ring; can be substituted with at least one group; it is selected from by halogen atom; halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed); amino-sulfonyl; 1; 2; 3; the 4-tetrahydric quinoline group (wherein this 1; 2; 3; on the 4-tetrahydroquinoline ring; can be substituted with at least one oxo base as substituting group); the C1-C6 alkyl sulphonyl; the C3-C8 cycloalkyl; nitro; cyano group; the C1-C6 alkylthio; benzenesulfonyl is (wherein on this benzyl ring; can be substituted with at least one group, it is selected from by halogen atom; halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed); C1-C6 alkyl that hydroxyl replaces and the group of representing by following chemical formula (34):

(W wherein ₁Represent the C1-C6 alkylidene group, R ¹¹And R ¹²Represent the C1-C6 alkoxyl group separately identical or differently)]; Phenyl C1-C6 alkyl is [wherein on this benzyl ring, can be substituted with at least one group as substituting group, it is selected from by C1-C4 alkylene dioxo base, phenyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group), group-N (R ¹¹A) R ^12A(R wherein ^11AAnd R ^12ARepresent hydrogen atom, C1-C6 alkyl or phenyl, R separately identical or differently ^11AAnd R ^12ACan be each other with their direct neighbors or pass through nitrogen, the nitrogen-atoms combination together that oxygen or sulphur atom are adjacent, constitute 5-7 unit saturated heterocyclic), phenoxy group is (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed), phenyl C1-C6 alkoxyl group, can have the C1-C6 alkyl as the substituent C1-C6 alkoxyl group that is replaced by amino, halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C10 alkoxyl group is formed]; Benzofuryl C1-C6 alkyl [wherein on this cumarone ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group]; Benzenesulfonyl [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group and C1-C4 alkylene dioxo base are formed group]; Phenyloxycarbonyl [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group]; Phenyl C2-C6 thiazolinyl [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group]; The C1-C6 alkyl that the C1-C6 alkoxyl group replaces; The C2-C6 thiazolinyl; The C2-C6 alkyloyl that the C1-C6 alkoxyl group replaces; The C1-C6 alkyl of C3-C8 cycloalkyl substituted; Phenoxy group C1-C6 alkyl [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group]; Benzoyl [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group]; Phenylamino formyl radical [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group]; Pyridyl; Pyridyl C1-C6 alkyl; Imidazolyl C1-C6 alkyl; 1,2,3, the 4-tetrahydric quinoline group [wherein this 1,2,3, on the 4-tetrahydroquinoline ring, can be substituted with at least one group as substituting group, it is selected from the group of being made up of oxo base and C1-C6 alkyl]; Quinolyl; Indyl; Can have the C1-C6 alkyl as substituent amino; Indazolyl; Naphthyl; The C3-C8 cycloalkyl; Can have the C1-C6 alkyl as the substituent C1-C6 alkyl that is replaced by amino; The C1-C6 alkyl that cyano group replaces; The C1-C6 alkyl that furyl replaces; Formula (35) group

And then, R ⁹And R ¹⁰Can be each other with their direct neighbors or pass through nitrogen, the nitrogen-atoms combination together that oxygen or sulphur atom are adjacent, constitute 1,2,3, the 4-tetrahydro isoquinolyl, pseudoindoyl or 5-7 unit saturated heterocyclic, wherein on this heterocycle, can be substituted with the group that at least one is selected from following groups: halogen atom, halogen replaces or unsubstituted C1-C6 alkyl, halogen replaces or unsubstituted C1-C6 alkoxyl group, phenyl is [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by phenyl, halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed], benzoyl is [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed], pyridyl C1-C6 alkyl, the C3-C8 cycloalkyl, phenyl C1-C6 alkyl is [wherein on this benzyl ring, can be substituted with at least one group, it is selected from the alkylene dioxo base by C1-C4, halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed], piperidyl C1-C6 alkyl, piperidyl, phenyl C1-C6 alkoxyl group is [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed], phenoxy group is [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed], amino (wherein can be substituted with at least one group as substituting group, it is selected from by phenyl [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed], C1-C6 alkyl and phenyl C1-C6 alkyl are [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group] group formed), benzo _ azoles base, phenyl C2-C6 thiazolinyl is (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed) and benzimidazolyl-);

(9) tetrahydro-pyran oxy C1-C6 alkyl;

(10) the C1-C6 alkyl of hydroxyl replacement;

(16) the C1-C6 alkyl of C2-C6 alkynyloxy group replacement;

(17) the C1-C6 alkyl of naphthyl C1-C6 alkoxyl group replacement;

(26) naphthyloxy;

(28) benzothiazole oxygen base [wherein on this benzothiazole oxygen base, can be substituted with at least one C1-C6 alkyl];

(30) diphenylene-oxide oxygen base;

(31) quinoline oxy;

(38) naphthyl C1-C6 alkoxyl group;

(51) benzo oxathiolane oxygen base C1-C6 alkyl (wherein on this benzo oxathiolane ring, can be substituted with at least one oxo base);

(52) isoquinoline 99.9 oxygen base C1-C6 alkyl;

(53) pyridyloxy C1-C6 alkyl;

(54) diphenylene-oxide oxygen base C1-C6 alkyl;

(56) benzisoxa _ azoles oxygen base C1-C6 alkyl;

(57) benzo furazan oxygen base C1-C6 alkyl;

(58) quinoxaline oxygen base C1-C6 alkyl;

(59) the C1-C6 alkyl of C1-C6 alkoxy C 1-C6 alkoxyl group replacement;

(62) the C1-C6 alkyl of quinolyl C1-C6 alkoxyl group replacement;

(63) the C1-C6 alkyl of piperidinyl carbonyl C1-C6 alkoxyl group replacement,

(iii) by the group of following chemical formula (36) representative:

(W wherein ₁Same as described above with o, R ¹³Representative: 2,3-dihydro-1H-indenyl; Benzothienyl; Phenyl C2-C10 thiazolinyl is [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, C1-C4 alkylene dioxo base, C1-C6 alkylthio, benzoyl, cyano group, nitro, C2-C6 alkanoyloxy, can have that the C1-C6 alkyl replaces as substituent amino, hydroxyl, phenyl C1-C6 alkoxyl group, phenoxy group, halogen or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group]; Naphthyl C2-C6 thiazolinyl; Benzofuryl C1-C6 alkyl [wherein on this cumarone ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group]; Benzothienyl C2-C6 thiazolinyl; Benzothiazolyl C2-C6 thiazolinyl [wherein on this benzothiazole ring, can be substituted with at least one C1-C6 alkyl]; Phenyl C1-C6 alkyl is [wherein on this benzyl ring, be substituted with the group that at least one is selected from following groups: piperidyl is (on this piperidine ring, can be substituted with at least one phenoxy group [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed]), phenyl is (wherein on this benzyl ring, be substituted with at least one group, it is selected from by halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group) and phenoxy group (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed)]; Phenylbenzene C1-C6 alkyl [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group]; Benzoyl C1-C6 alkyl [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group]; Amino, wherein can be substituted with the group that at least one is selected from following groups: C1-C6 alkyl, C1-C6 alkoxy carbonyl and phenyl C1-C6 alkyl are [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by phenyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group), halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replacement or unsubstituted C1-C6 alkoxyl group are formed group]; Amino C1-C6 alkyl, wherein can be substituted with at least one group, described group is selected from by C1-C6 alkyl and phenyl (wherein on this benzyl ring, can be substituted with at least one group, described group is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group) group formed; Benzofuryl C2-C6 thiazolinyl [wherein on this cumarone ring, can be substituted with at least one group, described group is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group]; Piperidyl is [wherein on this piperidine ring, can be substituted with at least one phenyl C2-C6 thiazolinyl (wherein on this benzyl ring, can be substituted with at least one group, described group is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group)]; The C1-C6 alkyl that ferrocene replaces; Indyl C1-C6 alkyl (wherein on this indole ring, can be substituted with at least one halogen atom); Phenyl C2-C6 alkynyl; Phenyl is [wherein on this benzyl ring, be substituted with at least one group, described group is selected from by C1-C4 alkylene dioxo base, phenyl, C1-C6 alkoxy carbonyl, hydroxyl and phenoxy group (wherein on this benzyl ring, can be substituted with at least one group, described group is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group) group formed]; Benzofuryl [wherein on this cumarone ring, can be substituted with at least one group, described group is selected from the group of being made up of halogen atom and C1-C6 alkyl]; Benzothiazole quinoline base [wherein on this benzothiazole quinoline ring, can be substituted with at least one oxo base]; Benzothienyl [wherein on this thionaphthene ring, can be substituted with at least one halogen atom]; Naphthyl; 1,2,3, the 4-tetrahydric quinoline group [wherein this 1,2,3, on the 4-tetrahydroquinoline ring, can be substituted with at least one group, described group is selected from the group of being made up of oxo base and C1-C6 alkyl]; Benzisoxa _ azoles base; 2, the 3-dihydro benzo furyl; 1,2-dihydroquinoline base [wherein this 1, on the 2-dihydroquinoline ring, can be substituted with at least one oxo base]; 1,2,3,4-tetrahydro quinazoline base [wherein this 1,2,3, on the 4-tetrahydro quinazoline ring, can be substituted with at least one group, described group is selected from the group of being made up of oxo base and C1-C6 alkyl]; The benzocyclohepta base; Phenoxy group C1-C6 alkyl [wherein on this benzyl ring, can be substituted with at least one group, described group is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group]; The C1-C6 alkyl [wherein on this thionaphthene ring, can be substituted with at least one halogen atom] that benzothienyl replaces; The C1-C6 alkyl of naphthyl substituted (wherein on this naphthalene nucleus, can be substituted with at least one C1-C6 alkoxyl group); The C1-C6 alkyl [wherein on this pyridine ring, can be substituted with at least one halogen atom] that pyridyl replaces; The C1-C6 alkyl [wherein on this furan nucleus, can be substituted with at least one nitro] that furyl replaces; The C1-C6 alkyl [wherein on this thiphene ring, can be substituted with at least one halogen atom] that thienyl replaces; The C1-C6 alkyl that thiazolyl replaces is [wherein on this thiazole ring, can be substituted with at least one group, described group is selected from by C1-C6 alkyl and phenyl (wherein on this benzyl ring, can be substituted with at least one group, described group is selected from the group by halogen atom and halogen replace or unsubstituted C1-C6 alkyl is formed) group formed]; The C1-C6 alkyl [wherein on this tetrazole ring, can be substituted with at least one C1-C6 alkyl] that tetrazyl replaces; The C1-C6 alkyl [wherein on this different _ azoles ring, can be substituted with at least one C1-C6 alkyl] that different _ azoles base replaces; 1,2, the C1-C6 alkyl that the 4-_ di azoly replaces [wherein this 1,2, on the 4-_ diazole ring, can be substituted with at least one phenyl (wherein on this benzyl ring, can be substituted with the C1-C6 alkyl)]; The perhaps C1-C6 alkyl that replaces of benzo furazan base);

(iv) by the group of following chemical formula (37) representative:

(R wherein ¹⁴Representative: phenylamino [wherein on the N-position of this phenylamino, can be substituted with the C1-C6 alkyl, on the benzyl ring of this phenylamino, can be substituted with at least one halogen and replace or unsubstituted C1-C6 alkoxyl group]; Piperidyl is [wherein on this piperidine ring, can be substituted with at least one group, described group is selected from by phenoxy group (wherein on this benzyl ring, can be substituted with halogen replaces or unsubstituted C1-C6 alkoxyl group) and amino (wherein on this amino, can be substituted with at least one group as substituting group, described group is selected from by C1-C6 alkyl and phenyl [wherein on this benzyl ring, can be substituted with at least one group, described group is selected from by halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group] group formed) group formed]; Piperazinyl is [wherein on this piperazine ring, can be substituted with the group that at least one is selected from following groups: the C1-C6 alkoxy carbonyl, phenyl C1-C6 alkyl is (wherein on this benzyl ring, can be substituted with at least one group, described group is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed), phenyl C2-C6 thiazolinyl is (wherein on this benzyl ring, can be substituted with at least one group, described group is selected from by halogen atom, halogen replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group) and benzoyl (wherein on this benzyl ring, can be substituted with at least one group, described group is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed)]; Phenyl (wherein on this benzyl ring, can be substituted with at least one group, described group is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group); High piperazinyl is [wherein on this high piperazine ring, can be substituted with at least one group, described group is selected from by C1-C6 alkoxy carbonyl and phenyl C1-C6 alkyl (wherein on this benzyl ring, can be substituted with at least one group, described group is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group) group formed]; Perhaps phenoxy group is [wherein on this benzyl ring, can be substituted with at least one group, described group is selected from the group of being made up of the phenyl of halogen replacement or unsubstituted C1-C6 alkoxyl group and phenoxy group replacement (wherein on this benzyl ring, can be substituted with at least one halogen and replace or unsubstituted C1-C6 alkoxyl group)]);

(v) by the group of following chemical formula (38) representative:

(vi) high piperazinyl (wherein on this high piperazine ring, can be substituted with the group that at least one is selected from following groups: the C1-C6 alkoxy carbonyl; Phenyl C1-C6 alkyl [wherein on this benzyl ring, can be substituted with at least one group, described group is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group]; Phenyl [wherein on this benzyl ring, can be substituted with at least one group, described group is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group]; Phenyl C1-C6 alkoxy carbonyl [wherein on this benzyl ring, can be substituted with at least one group, described group is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group]; Phenylamino formyl radical [wherein on this benzyl ring, can be substituted with at least one group, described group is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group]; Phenyl C2-C6 thiazolinyl [wherein on this benzyl ring, can be substituted with at least one group, described group is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group]; And benzoyl [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group]);

(vii) by the group of following chemical formula (39) representative:

(R wherein ¹⁹Represent the C1-C6 alkoxyl group, R ²⁰Represent phenyl [wherein on this benzyl ring, can be substituted with at least one group, described group is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group]);

(viii) group-CHR ²⁰R ²¹

(ix) 1,2,3, the 4-tetrahydro isoquinolyl (wherein this 1,2,3, on the 4-tetrahydroisoquinoline ring, can be substituted with at least one amino [wherein on this amino, can be substituted with at least one group, described group is selected from the group of being made up of phenyl C1-C6 alkyl (wherein on this benzyl ring, can be substituted with at least one group, described group is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group) and C1-C6 alkyl]);

(x) _ the azoles base (wherein this _ the azoles ring on, can be substituted with the group that at least one is selected from following groups: phenyl is [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed], C1-C6 alkyl and piperidyl are [wherein on this piperidine ring, can be substituted with at least one phenoxy group (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed)]);

(xii) thiazolyl is (wherein on this thiazole ring, can be substituted with the group that at least one is selected from following groups: phenoxy group C1-C6 alkyl is [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group]; Phenyl [wherein on this benzyl ring, can be substituted with at least one group, described group is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group]; Phenyl C1-C6 alkyl [wherein on this benzyl ring, can be substituted with at least one group, described group is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group]; Group-(W ₁) oNR ³¹R ³²[W wherein ₁Same as described above with o, R ³¹And R ³²Represent hydrogen atom, C1-C6 alkyl, phenyl (wherein on this benzyl ring separately identical or differently, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group) or phenyl C1-C6 alkyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group)]; Piperazinyl is [wherein on this piperazine ring, can be substituted with at least one phenyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group)]; Piperidyl is [wherein on this piperidine ring, can be substituted with at least one group, it is selected from by phenoxy group (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group) and the group formed of phenyl C1-C6 alkyl]; And phenoxy group [wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group]);

(xiii) the C1-C6 alkyl of hydroxyl replacement;

(xiv) pyrrolidyl is [wherein on this pyrrolidine ring, be substituted with at least one amino (wherein on this amino, can be substituted with at least one group, it is selected from by C1-C6 alkyl and phenyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group) group formed)];

(xxii) benzenesulfinyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group)];

(t) isoindoline oxygen base is [wherein on this isoindoline ring, can be substituted with the group that at least one is selected from following groups: the C1-C6 alkoxy carbonyl, phenyl C1-C6 alkyl is (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by benzofuryl, halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed), phenyl C2-C6 thiazolinyl is (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed), furyl C1-C6 alkyl is [wherein on this furan nucleus, can be substituted with at least one phenyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed)], pyridyl C1-C6 alkyl is [wherein on this pyridine ring, can be substituted with at least one group, it is selected from by furyl and phenyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, the group that halogen replacement or unsubstituted C1-C6 alkyl and halogen replacement or unsubstituted C1-C6 alkoxyl group are formed) group of forming], benzofuryl C1-C6 alkyl is (wherein on this cumarone ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed), benzothienyl C1-C6 alkyl is (wherein on this thionaphthene ring, can be substituted with at least one halogen atom), benzofuryl C2-C6 thiazolinyl is (wherein on this cumarone ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed), thiazolyl is [wherein on this thiazole ring, can be substituted with at least one phenyl (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed)], phenoxy group C1-C6 alkyl is (wherein on this benzyl ring, can be substituted with at least one group, it is selected from by halogen atom, halogen replacement or unsubstituted C1-C6 alkyl and the group that halogen replaces or unsubstituted C1-C6 alkoxyl group is formed)];

2. according to 2 of claim 1,3-dihydro-6-nitroimidazole is acceptable salt, wherein R on [2,1-b] _ azole compounds, its optically active form or its pharmacology also ²Representative (a) to (c), (e) to (h), (j) to (q) and (s) any described group in (y).

3. according to 2 of claim 1,3-dihydro-6-nitroimidazole is acceptable salt, wherein R on [2,1-b] _ azole compounds, its optically active form or its pharmacology also ²Representative (d) described group.

4. according to 2 of claim 1,3-dihydro-6-nitroimidazole is acceptable salt, wherein R on [2,1-b] _ azole compounds, its optically active form or its pharmacology also ²Representative (i) described group.

5. according to 2 of claim 1,3-dihydro-6-nitroimidazole is acceptable salt, wherein R on [2,1-b] _ azole compounds, its optically active form or its pharmacology also ²Representative (r) described group.

6. according to 2 of claim 1,3-dihydro-6-nitroimidazole is acceptable salt, wherein R on [2,1-b] _ azole compounds, its optically active form or its pharmacology also ¹Represent hydrogen atom.

7. according to 2 of claim 1,3-dihydro-6-nitroimidazole is acceptable salt, wherein R on [2,1-b] _ azole compounds, its optically active form or its pharmacology also ¹Represent the C1-C6 alkyl.

8. according to 2 of claim 1,3-dihydro-6-nitroimidazole is acceptable salt, wherein R on [2,1-b] _ azole compounds, its optically active form or its pharmacology also ¹With-(CH ₂) _nR ²Can be bonded to each other, constitute the volution of representing by following formula (30) with their adjacent carbon atoms:

Wherein RRR represents piperidyl [wherein on this piperidine ring, can be substituted with at least one phenoxy group (wherein on this benzyl ring, can be substituted with at least one group, described group is selected from by halogen atom, halogen and replaces or unsubstituted C1-C6 alkyl and halogen replaces or unsubstituted C1-C6 alkoxyl group is formed group)].

9. according to 2 of claim 6 or 7,3-dihydro-6-nitroimidazole is acceptable salt, wherein R on [2,1-b] _ azole compounds, its optically active form or its pharmacology also ³Representative (i) described group.

10. according to 2 of claim 6 or 7,3-dihydro-6-nitroimidazole is acceptable salt, wherein R on [2,1-b] _ azole compounds, its optically active form or its pharmacology also ³Represent (ii) described group.

11. according to 2 of claim 6 or 7,3-dihydro-6-nitroimidazole is acceptable salt, wherein R on [2,1-b] _ azole compounds, its optically active form or its pharmacology also ³Represent (iii) described group.

12. according to 2 of claim 6 or 7,3-dihydro-6-nitroimidazole is acceptable salt, wherein R on [2,1-b] _ azole compounds, its optically active form or its pharmacology also ³Represent (iv) described group.

13. according to 2 of claim 6 or 7,3-dihydro-6-nitroimidazole is acceptable salt, wherein R on [2,1-b] _ azole compounds, its optically active form or its pharmacology also ³Representative (v) described group.

14. according to 2 of claim 6 or 7,3-dihydro-6-nitroimidazole is acceptable salt, wherein R on [2,1-b] _ azole compounds, its optically active form or its pharmacology also ³Representative (vi) described group.

15. according to 2 of claim 6 or 7,3-dihydro-6-nitroimidazole is acceptable salt, wherein R on [2,1-b] _ azole compounds, its optically active form or its pharmacology also ³Representative (vii) described group.

16. according to 2 of claim 6 or 7,3-dihydro-6-nitroimidazole is acceptable salt, wherein R on [2,1-b] _ azole compounds, its optically active form or its pharmacology also ³Representative (viii) described group.

17. according to 2 of claim 6 or 7,3-dihydro-6-nitroimidazole is acceptable salt, wherein R on [2,1-b] _ azole compounds, its optically active form or its pharmacology also ³Representative (ix) described group.

18. according to 2 of claim 6 or 7,3-dihydro-6-nitroimidazole is acceptable salt, wherein R on [2,1-b] _ azole compounds, its optically active form or its pharmacology also ³Representative (x) described group.

19. according to 2 of claim 6 or 7,3-dihydro-6-nitroimidazole is acceptable salt, wherein R on [2,1-b] _ azole compounds, its optically active form or its pharmacology also ³Representative (xi) described group.

20. according to 2 of claim 6 or 7,3-dihydro-6-nitroimidazole is acceptable salt, wherein R on [2,1-b] _ azole compounds, its optically active form or its pharmacology also ³Representative (xii) described group.

21. according to 2 of claim 6 or 7,3-dihydro-6-nitroimidazole is acceptable salt, wherein R on [2,1-b] _ azole compounds, its optically active form or its pharmacology also ³Representative (xiii) described group.

22. according to 2 of claim 6 or 7,3-dihydro-6-nitroimidazole is acceptable salt, wherein R on [2,1-b] _ azole compounds, its optically active form or its pharmacology also ³Representative (xiv) described group.

23. according to 2 of claim 6 or 7,3-dihydro-6-nitroimidazole is acceptable salt, wherein R on [2,1-b] _ azole compounds, its optically active form or its pharmacology also ³Representative (xv) described group.

24. according to 2 of claim 6 or 7,3-dihydro-6-nitroimidazole is acceptable salt, wherein R on [2,1-b] _ azole compounds, its optically active form or its pharmacology also ³Representative (xvi) described group.

25. according to 2 of claim 6 or 7,3-dihydro-6-nitroimidazole is acceptable salt, wherein R on [2,1-b] _ azole compounds, its optically active form or its pharmacology also ³Representative (xvii) described group.

26. according to 2 of claim 6 or 7,3-dihydro-6-nitroimidazole is acceptable salt, wherein R on [2,1-b] _ azole compounds, its optically active form or its pharmacology also ³Representative (xviii) described group.

27. according to 2 of claim 6 or 7,3-dihydro-6-nitroimidazole is acceptable salt, wherein R on [2,1-b] _ azole compounds, its optically active form or its pharmacology also ³Representative (xix) described group.

28. according to 2 of claim 6 or 7,3-dihydro-6-nitroimidazole is acceptable salt, wherein R on [2,1-b] _ azole compounds, its optically active form or its pharmacology also ³Representative (xx) described group.

29. according to 2 of claim 6 or 7,3-dihydro-6-nitroimidazole is acceptable salt, wherein R on [2,1-b] _ azole compounds, its optically active form or its pharmacology also ³Representative (XX1) described group.

30. according to 2 of claim 6 or 7,3-dihydro-6-nitroimidazole is acceptable salt, wherein R on [2,1-b] _ azole compounds, its optically active form or its pharmacology also ³Representative (xxii) described group.

31. according to 2 of claim 1,3-dihydro-6-nitroimidazole is acceptable salt on [2,1-b] _ azole compounds or its pharmacology also, it is selected from the group of being made up of following compounds:

2-methyl-6-nitro-2-{4-[4-(4-phenalgin oxygen ylmethyl) piperidines-1-yl] phenoxymethyl }-2, the 3-glyoxalidine is [2,1-b] _ azoles also,

2-methyl-6-nitro-2-{4-[4-(4-4-trifluoromethylphenopendant methyl) piperidines-1-yl] phenoxymethyl }-2, the 3-glyoxalidine is [2,1-b] _ azoles also,

(S)-and 2-methyl-6-nitro-2-{4-[4-(4-bromine cedductor base) piperazine-1-yl] phenoxymethyl }-2, the 3-glyoxalidine is [2,1-b] _ azoles also,

32. antitubercular agent is characterized in that described medicine comprises according to 2 of claim 1,3-dihydro-6-nitroimidazole is acceptable salt on [2,1-b] _ azole compounds, its optically active form or its pharmacology also.

33. produce method by the compound of general formula (1) representative:

(R wherein ¹, R ²Have and the described identical definition of claim 1 with n),

Described method comprises:

Make 4-nitroimidazole compound by following general formula (2) representative:

(X wherein ₁Represent halogen atom or nitro),

React with epoxy compounds by following general formula (3a) representative:

(R wherein ¹, R ²Have and the described identical definition of claim 1 with n), obtain compound by following general formula (4a) representative:

(R wherein ¹, R ²Have and the described identical definition of claim 1, X with n ¹Represent halogen atom or nitro); The compound that gained is represented by above-mentioned general formula (4a) encircles closure subsequently.

34. produce method by the compound of following general formula (1w) representative:

(R wherein ^1ARepresent hydrogen atom or C1-C6 alkyl, R ^2AAny described group among (a) to (y) of representative according to claim 1, n represents the integer between 0 and 6),

Described method comprises:

Make compound by following general formula (3b) representative:

(R wherein ^1ASame as described above, X ¹Represent halogen atom or nitro),

With compound R ^2AH (5) or its reactant salt (R wherein ^2AAny described group among (a) to (y) of representative according to claim 1), obtain compound by following general formula (4c) representative:

(R wherein ¹Have and the described identical definition of claim 1, R ^2AAny described group among (a) to (y) of representative according to claim 1, X ¹Represent halogen atom or nitro); The compound that gained is represented by above-mentioned general formula (4c) encircles closure subsequently.

35. produce method by the compound of following general formula (1w) representative:

(R wherein ^1A, R ^2AHave and the described identical definition of claim 34 with n),

Described method comprises:

Make compound by following general formula (6) representative:

(R wherein ^1AHave and the described identical definition of claim 34, R with n ¹⁵Represent C1-C6 alkyl sulphonyl or benzenesulfonyl, wherein can be substituted with the C1-C6 alkyl),

With compound R ^2AH (5) or its reactant salt (R wherein ^2AAny described group among (a) to (y) of representative according to claim 1).