CN101356173B

CN101356173B - Novel pyridopyrazines and their use as kinase modulators

Info

Publication number: CN101356173B
Application number: CN2006800507541A
Authority: CN
Inventors: E·克劳斯; I·塞佩尔特; E·京特; E·波利莫罗普洛斯; M·切霍; T·舒斯特
Original assignee: Zentaris AG
Current assignee: Aeterna Zentaris GmbH
Priority date: 2005-11-11
Filing date: 2006-11-10
Publication date: 2012-10-31
Anticipated expiration: 2026-11-10
Also published as: CN101356173A; ZA200803864B

Abstract

The invention relates to novel pyrido[2,3-b]pyrazine derivatives of the general formulae (I) and (II), their preparation and use as medicaments, in particular for the treatment of malignant and other disorders involving pathological cell proliferations.

Description

New pyrido-pyrazine and they purposes as kinase modulator

Technical field

The present invention relates to pyrido [2,3-b] pyrazine type kinase regulator, its preparation; With purposes as medicine; Said medicine be used to regulate misdirection the cell signalling process, be particularly useful for influencing the function of Tyrosylprotein kinase, serine/threonine kinase and lipid kinase and be used to treat pernicious or innocent tumour and other illness based on pathologic cell propagation, for example restenosis; Psoriatic, arteriosclerosis and liver cirrhosis.

Background technology

The activation of protein kinase is the central event of cell signalling process.In multiple pathological state, observe unusual kinase activator.It is a basic therapeutic destination that therefore kinase whose target suppresses.

Proteic phosphorylation is started by extracellular signal usually, is representing the general mechanism of controlling the various kinds of cell incident, and said cell incident is metabolic process for example, cell growth, cell migration, cytodifferentiation, film transhipment and apoptosis.Kinase protein family load protein phosphorylation.These enzymes meeting catalysis phosphoric acid salt are to the proteic transfer of specific substrates.Based on substrate specificity, kinases is divided into 3 big types: Tyrosylprotein kinase, serine/threonine kinase and lipid kinase.Receptor tyrosine kinase and kytoplasm tyrosine, serine/threonine and lipid kinase are the important albumen of cell signalling.These proteic expression excessively or degraded play an important role in the illness based on pathologic cell propagation.They comprise metabolic disease, the illness of reticular tissue and blood vessel and pernicious and innocent tumour.In the tumour initial sum was grown, they often occurred as carcinogens, promptly as unusual, form active kinase protein.The result of this excessive kinase activator is, for example, and cell growth out of control and the necrocytosis that reduces.The stimulation of the growth factor of tumor promotion also possibly be the reason of kinases overstimulation.Therefore, for all pathogenic courses that influenced by kinases, the exploitation of kinase modulator is to make us interested especially.

Ras-Raf-Mek-Erk and the cascade of PI3K-Akt signal transduction play central role in cell growth, cell proliferation, apoptosis, adhesion, migration and glucose metabolism.Thereby, verified ras-Raf-Mek-Erk and the basic participation of PI3K-Akt signal pathway in the pathogeny of diseases such as cancer, neurodegeneration and inflammatory conditions.Therefore, the single component of these signal cascades constitutes the critical treatment sexual assault point of intervening the various diseases process (people 2000 such as Weinstein-Oppenheimer C.R., people 2003 such as Chang F., people 2003 such as people such as Katso R. 2001 and Lu Y.).

The molecule and the biochemical property of 2 signal pathways will be described at first respectively below.

Many growth factors, cytokine and carcinogens are through the activation of G-albumen-link coupled ras; Transduce their growth-promotion signal; The activation of said G-albumen-link coupled ras can cause the activation of serine-threonine kinase Raf and the activation of mitogen-activated protein kinase kinase 1 and 2 (MAPKK1/2 or Mek1/2); And cause the phosphorylation and the activation of MAPK 1 and 2, said MAPK 1 and 2 to be also referred to as the kinases (Erk1 and 2) of extracellular signal-adjusting.Compare with other single approach, the ras-Raf-Mek-Erk signal pathway made up a large amount of former-carcinogens, comprise part, tyrosine kinase receptor, G albumen, kinases and nuclear factor.Tyrosine-kinases, for example EGFR people such as (, 2000) Mendelsohn J. cross express and neoplastic process that sudden change causes in, to downstream ras-Raf-Mek-Erk signal pathway mediation to the frequent activated signal of composing type.Ras sudden change sudden change in 30% everyone tumour (people such as Khleif S.N., 1999, Marshall C., 1999), high incidence is 90% (Friess h in carcinoma of the pancreas.Deng the people, 1996, people such as Sirivatanauksorn V., 1998).For c-Raf, the expression and/or the activation (people such as Hoshino R., 1999, people such as McPhillips F., 2001) of the imbalance in different tumours have been described.At everyone malignant melanoma of 66%, 14% ovarian cancer and 12% colorectal carcinoma (Daviesh.Deng the people, 2002) detect B-Raf point mutation body in.Therefore, no wonder is that Erk1/2 participates in the starting stage of many cell processes, for example cell growth, cell proliferation and cytodifferentiation (people such as LewisT.S., 1998, people such as Chang F., 2003).

In addition, the kinase whose member of Raf also has and is independent of function Mek-Erk, anti-apoptotic, its minute substep fully describe as yet.For the active possible interacting partner of describing of the Raf that is independent of Mek-Erk has been Ask1, Bc1-2, Akt and Bag1 (people such as Chen J, 2001, people such as Troppmaier J., 2003, people such as Rapp U.R., 2004, people such as Gotz R., 2005).Supposition now, the signal transduction mechanism with being independent of Mek-Erk that depends on Mek-Erk is being controlled the activation of upper reaches ras and Raf stimulation.

The isozyme of phosphatidyl inositol 3-kinase (PI3K) mainly plays the function of lipid kinase, and catalysis second messenger lipid PtdIns (phosphatidyl inositol) D3 phosphoric acid changes into PtdIns (3) P, PtdIns (3,4) P ₂, PtdIns (3,4,5) P ₃The phosphatidyl myo-inositol phosphates.I class PI3K structurally (δ) form with adjusting subunit (p85 α, β or p101 γ) by catalytic subunit by p110 α, beta, gamma.In addition, II class (PI3K-C2 α, PI3K-C2 β) and III class (Vps34p) enzyme belong to PI3 kinases family (people such as Wymann M.P., 1998, people such as VanHaesebroeck B., 2001).The PIP that is brought out by PI3K raises through the coupling of ras, at first activationa and proliferation property ras-Raf-Mek-Erk signal pathway people such as (, 1994) Rodriguez-Viciana P.; Secondly through raising Akt to cytolemma and too drastic subsequently it serves somebody right kinases, the signal pathway of stimulation anti-apoptotic (people such as Alessi D.R., 1996; People such as Chang h.W.; 1997, people such as Moore S.M., 1998).Thereby 2 important mechanism that tumour is grown are carried out in the activation of PI3K at least, specifically are the activation and the apoptotic inhibition of cell growth and cytodifferentiation.In addition, PI3K also has albumen-phosphorylation character (people such as Dhand, 1994, people such as Bondeva T.; 1998, people such as Bondev A., 1999, people such as VanHaesebroeck B.; 1999), for example, it can induce the Serine autophosphorylation, and it really regulates PI3K.Also known PI3K has and is independent of kinase whose adjusting effector character, for example in systaltic control (people such as Crackower M.A., 2002, people such as Patrucco, 2004).Also verified; PI3K δ and PI3K γ are specific expressed on hematopoietic cell, thereby are potential attack point (people such as Okkenhaug K., 2003 that are used to treat inflammatory conditions such as rheumatism, asthma and transformation reactions and treatment B and t cell lymphoma isozyme-specific PI3K δ and PI3K gamma inhibitors; AliK. wait the people; 2004, people such as Sujobert P., 2005).(people such as Shayesteh L., 1999, people such as Ma Y.Y., 2000 have been differentiated recently for former-carcinogenic PI3K α; People such as Samuels Y., 2004, people such as Campbell I.G.; 2004, Levine D.A., 2005) be a kind of important target thing of treatment tumour illness.Therefore, be (Chang F.& LeeJ.T.et al, 2003) very widely as the importance of the PI3K species of the target thing of activeconstituents exploitation.

Equally very interested is the relevant kinases (PIKK) of PI3K-, and they comprise serine/threonine kinase mTOR, ATM, ATR, h-SMG-1 and DNA-PK people 2004 such as () Chiang G.G..The catalytic domain of their catalytic domain and PI3K has high sequence homology.

In addition; Rise to reverse disappearance (people such as Li J., 1997, the people such as Steck P.A. of tumor suppressor protein PTEN of the function of the phosphorylation that PI3K starts; 1997) help excessive activation Akt and its downstream stage joint group branch, thereby stress the origin cause of formation importance of PI3K as the target thing molecule of oncotherapy.

The multiple suppressor factor of the single component of ras-Raf-Mek-Erk and PI3K-Akt signal pathway has been disclosed and patent protection.

People such as J.S.Sebolt-Leopold, 2004, and people such as R.Wetzker, in 2004 the summary, kinases-suppressor factor, the exploitation present situation in ras-Raf-Mek-Erk and PI3K-Akt approach field especially have been detailed.Said publication contains a large amount of tabulations of disclosed patent, and they have been described the synthetic of lower molecular weight ras-Raf-Mek-Erk and PI3K suppressor factor and have used.

(WO 99/32111, WO03/068223) shows serine/threonine kinase and Tyrosylprotein kinase for example Raf, VEGFR2/3, Flt-3, PDGFR, c-Kit and other kinase whose nonspecific relatively suppression mode for the SU11752 Bay 43-9006 in clinical trial.This suppressor factor is (for example under the situation in renal cell carcinoma) in the late tumor illness that blood vessel brings out, but also has very big importance having under the melanomatous situation of high B-Raf mutation rate.Also in patient, measure now and the for example clinical effect of the Bay 43-9006 of docetaxel associating with refractory solid tumor.Up to now, gentle spinoff and promising antitumor action have been described.Description or open Bay 43-9006 be not to the kinase whose inhibition in the PI3K-Akt signal pathway.

Mek1/2 suppressor factor PD0325901 (WO 02/06213) is at present in the I clinical trial phase.Precursor substance CI-1040 (WO 00/35435, and WO 00/37141) is noticeable because of its high Mek specificity and target thing avidity.But, find in studying in the I/II phase that this compound is that metabolism is unsettled.The clinical data of current follow-up Substance P D0325901 remains to be obtained.But, the function of adjusting when not having to announce or disclose interaction or inhibition PI3K-Akt signal pathway or they of this Mek suppressor factor and Erk1 or Erk2.

Disclosed up to now PI3K suppressor factor is still in preclinical test.ICOS discloses a kind of high PI3K δ isozyme specific PI3K suppressor factor IC87114 (WO01/81346) that has.For PI103 (WO 04/017950), Yamanouchi/Piramed has described the relation of selectivity and PI3K α isotype.In addition, in the early development of PI3K suppressor factor, there is very famous research field (referring to people such as R.Wetzker, 2004 summary).

The suppressor factor of the SAPK signal pathway of in document, describing, the i.e. suppressor factor of Jnk or p38 (Gum R.J., 1998, people 2001 such as Bennett B.L., people 2000 such as Davies S.P.).But, do not have to disclose the function of the inhibition PI3K of these SAPK suppressor factor, or any specificity of Erk1 or Erk2 suppressed, or any specificity of SAPK, Erk1, Erk2 or PI3K is suppressed.

The substituted pyrido of 6-or 7-[2,3-b] pyrazines derivatives can be widely used in the pharmaceutical chemistry field, as the compound of pharmacological activity with as synthesis unit.

For example, patent WO 04/104002 and WO 04/104003 have described pyrido [2,3-b] pyrazine, and it can be replaced by urea, thiocarbamide, amidine or the guanidine radicals 6-of group or 7-.These compounds have as kinase whose suppressor factor or regulator, especially tyrosine and the suppressor factor of serine/threonine kinase or the character of regulator, and have reported the purposes as medicine.On the contrary, do not describe these compounds as independent or with the purposes of the regulator of the lipid kinase of tyrosine and serine/threonine kinase combination.

In addition, patent WO 99/17759 has described pyrido [2,3-b] pyrazine, its have in the 6-position especially alkyl-, aryl-and heteroaryl-substituted carbamate.The target purposes of these compounds is the functions of regulating the serine-threonine protein kinase enzyme.

Patent WO 05/007099 (people such as Kawakami) has described, especially, urea-substituted pyrido [2,3-b] pyrazine, it is as the suppressor factor of serine/threonine kinase PKB.But this patent does not further define the R group, and this R group is used to describe the replacement scope of urea, thereby does not clearly disclose the replacement scope on the urea.For these compounds, reported the purposes in the treatment cancer.But, do not provide the specific examples of urea-substituted pyrido-pyrazine with these biological properties.In addition, pyrido-pyrazine described here structurally significantly is different from creative pyrido [2, the 3-b] pyrazine of describing in the present invention.

In patent WO 05/056547 (people such as Bemis), reported other instance of 6-and 7-urea-substituted pyrido [2,3-b] pyrazine.But the compound in this patent has extra carbonyl, sulfoxide, sulfone or imines replacement at 2-or 3-position, this means that this compound structurally significantly is different from creative pyrido [2, the 3-b] pyrazine of describing in the present invention.The pyrido-pyrazine of in WO05/056547, reporting is described to protein kinase, the suppressor factor of GSK-3, Syk and JAK-3 especially.For these compounds, the purposes of report is included in the purposes in the treatment proliferative disorders.Do not describe these compounds as independent or with the purposes of the regulator of the lipid kinase of serine/threonine kinase combination.

People's such as White patent WO 04/005472 has described, especially, 6-carbamate-substituted pyrido [2,3-b] pyrazine, it can suppress the growth of bacterium as antimicrobial substance.Antitumor action is not described.

In patent WO 03/084473 (people such as Barnett), WO 03/086394 (people such as Bilodeau) and WO 03/086403 (people such as Lindsley); To on phenyl ring, have specific alkyl pyrrolidine, Alkylpiperidine or alkyl sulfonamide group and its can also be in 6-or 7-position extra have urea or substituted some the phenylbenzene quinoxaline of carbamate and-pyrido [2,3-b] pyrazine is described as the active suppressor factor of serine/threonine kinase Akt.For these compounds, reported the purposes in the treatment cancer.For wherein said pyrido [2,3-b] pyrazine embodiment compound, do not specify the definite indication of biological action.In addition, structurally significantly be different from creative pyrido [2, the 3-b] pyrazine of describing in the present invention.

In addition; People's such as Delorme patent WO 03/024448 has described acid amides-and acrylic amide-substituted pyrido [2; 3-b] pyrazine, it also contains carbamate as extra substituting group, and can be with the histone deacetylase inhibitors that acts on treatment cell proliferation illness.

Another piece publication (C.Temple, Jr.; J.Med.Chem.1990 3044-3050) has used a case description synthesizing of 6-ethyl carbamate-substituted pyrido [2,3-b] pyrazines derivatives.Antitumor action is not disclosed, neither be conspicuous.

(J.Org.Chem.1968 in publication 2393-2397), has described other verivate synthetic of 6-ethyl carbamate-substituted pyrido [2,3-b] pyrazine at R.D.Elliott.The biological action of these compounds is not described, neither be conspicuous.

C.Temple, Jr.J.Med.Chem.1968, the publication of 1216-1218 have described the synthetic and inspection of 6-ethyl carbamate-substituted pyrido [2, the 3-b] pyrazine as potential activated antimalarial composition.Antitumor action is not disclosed, neither be conspicuous.

Summary of the invention

Therefore the present invention relates to the providing of new compound of the regulator that is suitable as receptor tyrosine kinase, cytoplasmic tyrosine kinase, serine/threonine kinase and lipid kinase.Owing to be not that all kinases that are present in a series of wrong signal transduction cascades of regulating (for example under the situation of Raf-Mek-Erk or PI3K-Akt) all need occur as carcinogenic kinases or as forming active enzyme; The present invention also regards the kinases of non-activity as curative target protein; Be that said new compound can be combined with active and kinases non-activity, thereby influence signal transduction.

The present invention also relates to as the providing of the new compound of the regulator of receptor tyrosine kinase, cytoplasmic tyrosine kinase, serine/threonine kinase and lipid kinase, said new compound has influence from a signal transduction cascade or unlike signal transductory cascade, especially ras-Raf-Mek-Erk and PI3K-Akt single plants kinases or 2 kinds or multiple kinases, the character of Erk1/2 and PI3K especially.Only attack a signal transduction pathway with therapeutic and compare, double mechanism (promptly suppressing 2 or a plurality of signal transduction cascade simultaneously) is because additive effect can cause receiving the increase of the result of treatment of all pathogenic courses that kinases influences.

It has surprisingly been found that now; From 6-or 7-position by for example urea or the substituted pyrido [2 of thiocarbamide part; 3-b] new compound of pyrazine group is applicable to the production medicine; Said medicine is used to regulate the cell signalling process of misdirection, is particularly useful for influencing the function of receptor tyrosine kinase, cytoplasmic tyrosine kinase, serine/threonine kinase and lipid kinase and is used to treat pernicious or the innocent tumour illness; For example the tumour illness of breast, prostate gland, lung, skin, ovary and other are based on the illness of pathologic cell propagation.

The new compound of pyrido [2,3-b] the pyrazine group of coming self-drifting (I) has been described in first aspect of the application

Wherein:

(A) one of Z3, Z4 group or Z3, Z4 group the two be " substituted aryl " independently, wherein " substituted aryl " is by at least one identical ground or different are selected from following substituting group and replace:

(a) " alkyl, naphthenic base, heterocyclic radical, aryl, heteroaryl ,-NH-X1 ,-N (alkyl) ₂,-NHC (O)-alkyl ,-NHC (O)-naphthenic base ,-NHC (O)-heterocyclic radical ,-NHC (O)-aryl ,-NHC (O)-heteroaryl ,-NHC (O)-arylalkyl ,-NHC (O)-heteroarylalkyl ,-NHS (O ₂)-alkyl ,-NHS (O ₂)-naphthenic base ,-NHS (O ₂)-heterocyclic radical ,-NHS (O ₂)-aryl ,-NHS (O ₂)-heteroaryl ,-NHS (O ₂)-arylalkyl ,-NHS (O ₂)-heteroarylalkyl ,-S-alkyl ,-S-aryl ,-S-heteroaryl ,-O-X2 ,-OC (O)-alkyl ,-OC (O)-naphthenic base ,-OC (O)-heterocyclic radical ,-OC (O)-aryl ,-OC (O)-heteroaryl ,-OC (O)-arylalkyl ,-OC (O)-heteroarylalkyl ,-OS (O ₂)-alkyl ,-OS (O ₂)-naphthenic base ,-OS (O ₂)-heterocyclic radical ,-OS (O ₂)-aryl ,-OS (O ₂)-heteroaryl ,-OS (O ₂)-arylalkyl ,-OS (O ₂)-heteroarylalkyl ,-C (O)-alkyl ,-C (O)-aryl ,-C (O)-heteroaryl ,-C (O) O-X3 ,-C (O) NH-X4 ,-C (O) N (alkyl) ₂,-C (O) N (naphthenic base) ₂,-C (O) N (aryl) ₂,-C (O) N (heteroaryl) ₂,-S (O)-alkyl ,-S (O)-aryl ,-S (O ₂)-alkyl ,-S (O ₂)-aryl ,-S (O ₂) the NH-alkyl ,-S (O ₂) the NH-aryl ,-S (O ₂) the NH-heteroaryl ,-S (O ₂) the NH-arylalkyl, S (O ₂) the O-alkyl ,-S (O ₂) the O-aryl ,-S (O ₂) the O-arylalkyl ";

X1 wherein, X2, X3, X4 is selected from independently of one another: " alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl ";

Condition is, the above-mentioned substituting group of substituting group group (a) is independently of one another by at least one identical ground or different are selected from following substituting group and further replace:

(i) " (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, N ₃,-NH-naphthenic base ,-NH-cycloalkylalkyl ,-NH-heteroaryl ,-NH-heteroarylalkyl ,-NH-arylalkyl ,-NH-heterocyclic radical;-NH-heterocyclic radical alkyl ,-NX5X6 ,-S-naphthenic base ,-S-cycloalkylalkyl ,-S-aryl ,-S-arylalkyl;-S-heteroaryl ,-S-heteroarylalkyl ,-S-heterocyclic radical ,-S-heterocyclic radical alkyl ,-O-naphthenic base ,-O-cycloalkylalkyl;-O-arylalkyl ,-O-heteroaryl ,-O-heteroarylalkyl ,-O-heterocyclic radical ,-O-heterocyclic radical alkyl ,-O is (X7-O) _p-X8 (p=1,2,3,4,5) ,-OP (O) is (OX10) (OX9) ,-C (O) O-X11 ,-C (O) NH ₂,-C (O) NH-X12 ,-C (O) NX13X14 ,-S (O ₂)-X15 ,-P (O) (OH) ₂,-P (O) is (OX17) (OX16), and-Si (X18) is (X20) (X19), and-O-Si (X21) is (X23) (X22);-O-C (O)-O-X24 ,-O-C (O)-NH-X25 ,-O-C (O)-NX26X27 ,-NH-C (O)-O-X28;-NH-C (O)-NH-X29 ,-NH-C (O)-NX30X31 ,-NX 32-C (O)-O-X33;-NX34-C (O)-NH-X35 ,-NX36-C (O)-NX37X38 ,-O-S (O ₂)-X39 ,-NH-C (O)-X40 ,-NX41-C (O)-X42 ,-C (O)-X43 ,-OC (O)-X44 ,-S (O)-X45 ,-S (O ₂)-NHX46 ,-S (O ₂)-NX47X48 ,-S (O ₂)-OX49 ,-O are (X50-O) _p-H (p=1,2,3,4,5) ";

Other condition is " N (alkyl) ₂" further replaced by at least one substituting group that is selected from following substituting group group (b);

X5 wherein, X6, X7, X8, X9, X10, X11, X12, X13, X14, X15, X16; X17, X18, X19, X20, X21, X22, X23, X24, X25, X26, X27, X28; X29, X30, X31, X32, X33, X34, X35, X36, X37, X38, X39, X40; X41, X42, X43, X44, X45, X46, X47, X48, X49, X50 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl; Arylalkyl, heteroaryl, heteroarylalkyl " and wherein, perhaps, X13; X14 and/or X26, X27 and/or X30, X31 and/or X37, X38 and/or X47, X48 also can form " heterocyclic radical " together;

And other condition is, when one of Z3 or Z4 group during by " heterocyclic radical alkyl " substituted " substituted aryl ", other Z3 or Z4 group are not " substituted or unsubstituted aryl " in each case;

Wherein randomly, extraly one of Z3, Z4 group or extraly Z3, Z4 group the two can be independently of one another by at least one identical ground or different are selected from following substituting group and further replace:

(b) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHX51 ,-NX52X53 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-X54 ,-C (O) O-X55 ,-C (O) NH-X56 ,-C (O) NX57X58 ,-O-X59 ,-O are (X60-O) _r-H (r=1,2,3,4,5) ,-O (X61-O) _r-X62 (r=1,2,3,4,5) ,-OC (O)-X63 ,-OC (O)-O-X64 ,-OC (O)-NHX65 ,-O-C (O)-NX66X67 ,-OP (O) is (OX69) (OX68), and-OSi (X70) is (X72) (X71) ,-OS (O ₂)-X73 ,-NHC (O)-X74 ,-NX75C (O)-X76 ,-NH-C (O)-O-X77 ,-NH-C (O)-NH-X78 ,-NH-C (O)-NX 79X80 ,-NX81-C (O)-O-X82 ,-NX83-C (O)-NH-X84 ,-NX85-C (O)-NX86X87 ,-NHS (O ₂)-X88 ,-NX89S (O ₂)-X90 ,-S-X91 ,-S (O)-X92 ,-S (O ₂)-X93 ,-S (O ₂) NH-X94 ,-S (O ₂) NX95X96 ,-S (O ₂) O-X97 ,-P (O) is (OX99) (OX98), and-Si (X100) is (X102) (X101) ";

X51 wherein, X52, X53, X54, X55, X56, X57, X58, X59, X60, X61, X62, X63, X64; X65, X66, X67, X68, X69, X70, X71, X72, X73, X74, X75, X76, X77; X78, X79, X80, X81, X82, X83, X84, X85, X86, X87, X88, X89, X90; X91, X92, X93, X94, X95, X96, X97, X98, X99, X100, X101, X102 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl; Arylalkyl, heteroaryl, heteroarylalkyl " and wherein, perhaps, X57; X58 and/or X66, X67 and/or X79, X80 and/or X86, X87 and/or X95, X96 also can form " heterocyclic radical " together;

Wherein randomly, the above-mentioned substituting group of substituting group group (b) can be selected from following substituting group replacement independently of one another and then by at least one identically or differently:

(ii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHX103 ,-NX104X105 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-X106 ,-C (O) O-X107 ,-C (O) NH-X108 ,-C (O) NX109X110 ,-O-X111 ,-O are (X112-O) _s-H (s=1,2,3,4,5) ,-O (X113-O) _s-X114 (s=1,2,3,4,5) ,-OC (O)-X115 ,-OC (O)-O-X116 ,-OC (O)-NHX117 ,-O-C (O)-NX118X119 ,-OP (O) is (OX121) (OX120), and-OSi (X122) is (X124) (X123) ,-OS (O ₂)-X125 ,-NHC (O)-X126 ,-NX127C (O)-X128 ,-NH-C (O)-O-X129 ,-NH-C (O)-NH-X130 ,-NH-C (O)-NX131X132 ,-NX133-C (O)-O-X134 ,-NX135-C (O)-NH-X136 ,-NX137-C (O)-NX138X139 ,-NHS (O ₂)-X140 ,-NX141S (O ₂)-X142 ,-S-X143 ,-S (O)-X144 ,-S (O ₂)-X145 ,-S (O ₂) NH-X146 ,-S (O ₂) NX147X148 ,-S (O ₂) O-X149 ,-P (O) is (OX151) (OX150), and-Si (X152) is (X154) (X153) ";

X103 wherein, X104, X105, X106, X107, X108, X109, X110, X111, X112, X113, X114, X115, X116; X117, X118, X119, X120, X121, X122, X123, X124, X125, X126, X127, X128, X129; X130, X131, X132, X133, X134, X135, X136, X137, X138, X139, X140, X141, X142; X143, X144, X145, X146, X147, X148, X149, X150, X151, X152, X153, X154 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl; Arylalkyl, heteroaryl, heteroarylalkyl " and wherein, perhaps, X109; X110 and/or X118, X119 and/or X131, X132 and/or X138, X139 and/or X147, X148 also can form " heterocyclic radical " together;

Wherein randomly, substituting group group (i) and/or substituting group group above-mentioned substituting group (ii) can be selected from following substituting group replacement independently of one another and then by at least one identically or differently:

(iii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHX155 ,-NX156X157 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-X158 ,-C (O) O-X159 ,-C (O) NH-X160 ,-C (O) NX161X162 ,-O-X163 ,-O are (X164-O) _t-H (t=1,2,3,4,5) ,-O (X165-O) _t-X166 (t=1,2,3,4,5) ,-OC (O)-X167 ,-OC (O)-O-X168 ,-OC (O)-NHX169 ,-O-C (O)-NX170X171 ,-OP (O) is (OX173) (OX172), and-OSi (X174) is (X176) (X175) ,-OS (O ₂)-X177 ,-NHC (O)-X178 ,-NX179C (O)-X180 ,-NH-C (O)-O-X181 ,-NH-C (O)-NH-X182 ,-NH-C (O)-NX183X184 ,-NX185-C (O)-O-X186 ,-NX187-C (O)-NH-X188 ,-NX189-C (O)-NX190X191 ,-NHS (O ₂)-X192 ,-NX193S (O ₂)-X194 ,-S-X195 ,-S (O)-X196 ,-S (O ₂)-X197 ,-S (O ₂) NH-X198 ,-S (O ₂) NX199X200 ,-S (O ₂) O-X201 ,-P (O) is (OX203) (OX202), and-Si (X204) is (X206) (X205) ";

X155 wherein, X156, X157, X158, X159, X160, X161, X162, X163, X164, X165, X166, X167, X168; X169, X170, X171, X172, X173, X174, X175, X176, X177, X178, X179, X180, X181; X182, X183, X184, X185, X186, X187, X188, X189, X190, X191, X192, X193, X194; X195, X196, X197, X198, X199, X200, X201, X202, X203, X204, X205, X206 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl; Arylalkyl, heteroaryl, heteroarylalkyl " and wherein, perhaps, X161; X162 and/or X170, X171 and/or X183, X184 and/or X190, X191 and/or X199, X200 also can form " heterocyclic radical " together;

Or one of Z3, Z4 group or Z3, Z4 group the two be " substituted aryl " independently, wherein " substituted aryl " is by at least one identical ground or different are selected from following substituting group and replace:

(c) " (C ₉-C ₃₀) alkyl ,-NX207X208 ,-NH-(C ₉-C ₃₀) alkyl ,-NHC (O)-cycloalkylalkyl ,-NHC (O)-heterocyclic radical alkyl ,-NHC (O)-(C ₉-C ₃₀) alkyl ,-NX209C (O)-X210 ,-NX211C (O)-(C ₉-C ₃₀) alkyl ,-NHC (O)-OX212 ,-NX213C (O)-OX214 ,-NHC (O)-NHX215 ,-NHC (O)-NX216X217 ,-NX218C (O)-NHX219 ,-NX220C (O)-NX221X222 ,-NHS (O ₂)-cycloalkylalkyl ,-NHS (O ₂)-heterocyclic radical alkyl ,-NX223S (O ₂)-X224 ,-O-(C ₉-C ₃₀) alkyl ,-S-naphthenic base ,-S-heterocyclic radical ,-S-arylalkyl ,-S-heteroarylalkyl ,-S-cycloalkylalkyl ,-S-heterocyclic radical alkyl ,-S-(C ₉-C ₃₀) alkyl ,-OC (O)-cycloalkylalkyl ,-OC (O)-heterocyclic radical alkyl ,-OC (O)-(C ₉-C ₃₀) alkyl ,-OS (O ₂)-cycloalkylalkyl ,-OS (O ₂)-heterocyclic radical alkyl ,-OS (O ₂)-(C ₉-C ₃₀) alkyl ,-OC (O)-OX225 ,-OC (O)-NHX226 ,-OC (O)-NX227X228;-OP (O) is (OX230) (OX229) ,-C (O)-naphthenic base ,-C (O)-heterocyclic radical ,-C (O)-arylalkyl;-C (O)-heteroarylalkyl ,-C (O)-cycloalkylalkyl ,-C (O)-heterocyclic radical alkyl ,-C (O)-(C ₉-C ₃₀) alkyl ,-C (O) O-(C ₉-C ₃₀) alkyl ,-C (O) NH-(C ₉-C ₃₀) alkyl ,-C (O) NX231X232 ,-C (O) NH-OX233 ,-C (O) NX234-OX235;-C (O) NH-NX236X237 ,-C (O) NX238-NX239X240 ,-S (O)-naphthenic base ,-S (O)-heterocyclic radical;-S (O)-heteroaryl ,-S (O)-arylalkyl ,-S (O)-heteroarylalkyl;-S (O)-cycloalkylalkyl ,-S (O)-heterocyclic radical alkyl ,-S (O)-(C ₉-C ₃₀) alkyl ,-S (O ₂)-naphthenic base ,-S (O ₂)-heterocyclic radical ,-S (O ₂)-heteroaryl ,-S (O ₂)-arylalkyl ,-S (O ₂)-heteroarylalkyl ,-S (O ₂)-cycloalkylalkyl ,-S (O ₂)-heterocyclic radical alkyl ,-S (O ₂)-(C ₉-C ₃₀) alkyl ,-S (O ₂) the NH-naphthenic base ,-S (O ₂) the NH-heterocyclic radical ,-S (O ₂) the NH-heteroarylalkyl ,-S (O ₂) the NH-cycloalkylalkyl ,-S (O ₂) NH-heterocyclic radical alkyl ,-S (O ₂) NH-(C ₉-C ₃₀) alkyl ,-S (O ₂) the O-naphthenic base ,-S (O ₂) the O-heterocyclic radical ,-S (O ₂) the O-heteroaryl ,-S (O ₂) the O-heteroarylalkyl ,-S (O ₂) the O-cycloalkylalkyl ,-S (O ₂) O-heterocyclic radical alkyl ,-S (O ₂) O-(C ₉-C ₃₀) alkyl ,-P (O) is (OH) ₂,-P (O) is (OX242) (OX241), and-Si (X243) is (X245) (X244) ,-O-Si (X246) is (X248) (X247) ";

X207 wherein, X208, X209, X210, X211, X212, X213, X214, X215, X216, X217; X218, X219, X220, X221, X222, X223, X224, X225, X226, X227, X228; X229, X230, X231, X232, X233, X234, X235, X236, X237, X238, X239; X240, X241, X242, X243, X244, X245, X246, X247, X248 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl; Aryl, arylalkyl, heteroaryl, heteroarylalkyl " and wherein; perhaps, X216, X217 and/or X221, X222 and/or X227; X228 and/or X231, X232 and/or X236, X237 and/or X239, X240 also can form " heterocyclic radical " in each case together;

Condition is substituting group " N (alkyl) ₂", " C (O) N (alkyl) ₂", " C (O) N (naphthenic base) ₂", " C (O) N (aryl) ₂", " C (O) N (heteroaryl) ₂" further replaced by at least one substituting group that is selected from following substituting group group (i);

Other condition is, when one of Z3 or Z4 group during by " heterocyclic radical alkyl " substituted " substituted aryl ", other Z3 or Z4 group are not " unsubstituted or substituted aryl " in each case;

Wherein randomly, the above-mentioned substituting group of substituting group group (c) can be selected from following substituting group replacement independently of one another and then by at least one identically or differently:

(i) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHX249 ,-NX250X251 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-X252 ,-C (O) O-X253 ,-C (O) NH-X254 ,-C (O) NX255X256 ,-O-X257 ,-O are (X258-O) _u-H (u=1,2,3,4,5) ,-O (X259-O) _u-X260 (u=1,2,3,4,5) ,-OC (O)-X261 ,-OC (O)-O-X262 ,-OC (O)-NHX263 ,-O-C (O)-NX264X265 ,-OP (O) is (OX267) (OX266), and-OSi (X268) is (X270) (X269) ,-OS (O ₂)-X271 ,-NHC (O)-X272 ,-NX273C (O)-X274 ,-NH-C (O)-O-X275 ,-NH-C (O)-NH-X276 ,-NH-C (O)-NX277X278 ,-NX279-C (O)-O-X280 ,-NX281-C (O)-NH-X282 ,-NX283-C (O)-NX284X285 ,-NHS (O ₂)-X286 ,-NX287S (O ₂)-X288 ,-S-X289 ,-S (O)-X290 ,-S (O ₂)-X291 ,-S (O ₂) NH-X292 ,-S (O ₂) NX293X294 ,-S (O ₂) O-X295 ,-P (O) is (OX297) (OX296), and-Si (X298) is (X300) (X299) ";

X249 wherein, X250, X251, X252, X253, X254, X255, X256, X257, X258, X259, X260, X261, X262; X263, X264, X265, X266, X267, X268, X269, X270, X271, X272, X273, X274, X275; X276, X277, X278, X279, X280, X281, X282, X283, X284, X285, X286, X287, X288; X289, X290, X291, X292, X293, X294, X295, X296, X297, X298, X299, X300 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, X255, X256 and/or X264; X265 and/or X277, X278 and/or X284, X285 and/or X293, X294 also can form " heterocyclic radical " in each case together;

(d) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHX 301 ,-NX302X303 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-X304 ,-C (O) O-X305 ,-C (O) NH-X306 ,-C (O) NX307X308 ,-O-X309 ,-O are (X310-O) _Uu-H (uu=1,2,3,4,5) ,-O (X311-O) _Uu-X312 (uu=1,2,3,4,5) ,-OC (O)-X313 ,-OC (O)-O-X314 ,-OC (O)-NHX315 ,-O-C (O)-NX316X317 ,-OP (O) is (OX319) (OX318), and-OSi (X320) is (X322) (X321) ,-OS (O ₂)-X323 ,-NHC (O)-X324 ,-NX325C (O)-X326 ,-NH-C (O)-O-X327 ,-NH-C (O)-NH-X328 ,-NH-C (O)-NX329X330 ,-NX331-C (O)-O-X332 ,-NX333-C (O)-NH-X334 ,-NX335-C (O)-NX336X337 ,-NHS (O ₂)-X338 ,-NX339S (O ₂)-X340 ,-S-X341 ,-S (O)-X342 ,-S (O ₂)-X343 ,-S (O ₂) NH-X344 ,-S (O ₂) NX345X346 ,-S (O ₂) O-X347 ,-P (O) is (OX349) (OX348), and-Si (X350) is (X352) (X351) ";

X301 wherein, X302, X303, X304, X305, X306, X307, X308, X309, X310, X311, X312, X313, X314; X315, X316, X317, X318, X319, X320, X321, X322, X323, X324, X325, X326, X327; X328, X329, X330, X331, X332, X333, X334, X335, X336, X337, X338, X339, X340; X341, X342, X343, X344, X345, X346, X347, X348, X349, X350, X351, X352 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, X307, X308 and/or X316; X317 and/or X329, X330 and/or X336, X337 and/or X345, X346 also can form " heterocyclic radical " in each case together;

Wherein randomly, the above-mentioned substituting group of substituting group group (d) can be selected from following substituting group replacement independently of one another and then by at least one identically or differently:

(ii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHX353 ,-NX354X355 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-X356 ,-C (O) O-X357 ,-C (O) NH-X358 ,-C (O) NX359X360 ,-O-X361 ,-O are (X362-O) _v-H (v=1,2,3,4,5) ,-O (X363-O) _v-X364 (v=1,2,3,4,5) ,-OC (O)-X365 ,-OC (O)-O-X366 ,-OC (O)-NHX367 ,-O-C (O)-NX368X369 ,-OP (O) is (OX371) (OX370), and-OSi (X372) is (X374) (X373) ,-OS (O ₂)-X375 ,-NHC (O)-X376 ,-NX377C (O)-X378 ,-NH-C (O)-O-X379 ,-NH-C (O)-NH-X380 ,-NH-C (O)-NX381X382 ,-NX383-C (O)-O-X384 ,-NX385-C (O)-NH-X386 ,-NX387-C (O)-NX388X389 ,-NHS (O ₂)-X390 ,-NX391S (O ₂)-X392 ,-S-X393 ,-S (O)-X394 ,-S (O ₂)-X395 ,-S (O ₂) NH-X396 ,-S (O ₂) NX397X398 ,-S (O ₂) O-X399 ,-P (O) is (OX401) (OX400), and-Si (X402) is (X404) (X403) ";

X353 wherein, X354, X355, X356, X357, X358, X359, X360, X361, X362, X363, X364, X365, X366; X367, X368, X369, X370, X371, X372, X373, X374, X375, X376, X377, X378, X379; X380, X381, X382, X383, X384, X385, X386, X387, X388, X389, X390, X391, X392; X393, X394, X395, X396, X397, X398, X399, X400, X401, X402, X403, X404 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, X359, X360 and/or X368; X369 and/or X381, X382 and/or X388, X389 and/or X397, X398 also can form " heterocyclic radical " in each case together;

(iii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHX405 ,-NX406X407 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-X408 ,-C (O) O-X409 ,-C (O) NH-X410 ,-C (O) NX411X412 ,-O-X413 ,-O are (X414-O) _w-H (w=1,2,3,4,5) ,-O (X415-O) _w-X416 (w=1,2,3,4,5) ,-OC (O)-X417 ,-OC (O)-O-X418 ,-OC (O)-NHX419 ,-O-C (O)-NX420X421 ,-OP (O) is (OX423) (OX422), and-OSi (X424) is (X426) (X425) ,-OS (O ₂)-X427 ,-NHC (O)-X428 ,-NX429C (O)-X430 ,-NH-C (O)-O-X431 ,-NH-C (O)-NH-X432 ,-NH-C (O)-NX433X434 ,-NX435-C (O)-O-X436 ,-NX437-C (O)-NH-X438 ,-NX439-C (O)-NX440X441 ,-NHS (O ₂)-X442 ,-NX443S (O ₂)-X444 ,-S-X445 ,-S (O)-X446 ,-S (O ₂)-X447 ,-S (O ₂) NH-X448 ,-S (O ₂) NX449X450 ,-S (O ₂) O-X451 ,-P (O) is (OX453) (OX452), and-Si (X454) is (X456) (X455) ";

X405 wherein, X406, X407, X408, X409, X410, X411, X412, X413, X414, X415, X416, X417, X418; X419, X420, X421, X422, X423, X424, X425, X426, X427, X428, X429, X430, X431; X432, X433, X434, X435, X436, X437, X438, X439, X440, X441, X442, X443, X444; X445, X446, X447, X448, X449, X450, X451, X452, X453, X454, X455, X456 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, X411, X412 and/or X420; X421 and/or X433, X434 and/or X440, X441 and/or X449, X450 also can form " heterocyclic radical " in each case together;

AndOne of Z3, Z4 group or Z3, Z4 group none are independently selected from:

(e) hydrogen;

(f) halogen, F, Cl, Br, I;

(g) unsubstituted or substituted alkyl or (C ₉-C ₃₀) alkyl, wherein randomly, said alkyl or (C ₉-C ₃₀) alkyl can or different are selected from following substituting group and replace by at least one identical ground:

(i) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHX457 ,-NX458X459 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-X460 ,-C (O) O-X461 ,-C (O) NH-X462 ,-C (O) NX463X464 ,-O-X465 ,-O are (X466-O) _x-H (x=1,2,3,4,5) ,-O (X467-O) _x-X468 (x=1,2,3,4,5) ,-OC (O)-X469 ,-OC (O)-O-X470 ,-OC (O)-NHX471 ,-O-C (O)-NX472X473 ,-OP (O) is (OX475) (OX474), and-OSi (X476) is (X478) (X477) ,-OS (O ₂)-X479 ,-NHC (O)-X480 ,-NX481C (O)-X482 ,-NH-C (O)-O-X483 ,-NH-C (O)-NH-X484 ,-NH-C (O)-NX485X486 ,-NX487-C (O)-O-X488 ,-NX489-C (O)-NH-X490 ,-NX491-C (O)-NX492X493 ,-NHS (O ₂)-X494 ,-NX495S (O ₂)-X496 ,-S-X497 ,-S (O)-X498 ,-S (O ₂)-X499 ,-S (O ₂) NH-X500 ,-S (O ₂) NX501X502 ,-S (O ₂) O-X503 ,-P (O) is (OX505) (OX504), and-Si (X506) is (X508) (X507) ";

X457 wherein, X458, X459, X460, X461, X462, X463, X464, X465, X466, X467, X468, X469, X470; X471, X472, X473, X474, X475, X476, X477, X478, X479, X480, X481, X482, X483; X484, X485, X486, X487, X488, X489, X490, X491, X492, X493, X494, X495, X496; X497, X498, X499, X500, X501, X502, X503, X504, X505, X506, X507, X508 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, X463, X464 and/or X472; X473 and/or X485, X486 and/or X492, X493 and/or X501, X502 also can form " heterocyclic radical " in each case together;

Wherein randomly, the above-mentioned substituting group of substituting group group (i) can and then be selected from following substituting group replacement by at least one independently of one another identically or differently:

(ii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHX509 ,-NX510X511 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-X512 ,-C (O) O-X513 ,-C (O) NH-X514 ,-C (O) NX515X516 ,-O-X517 ,-O are (X518-O) _y-H (y=1,2,3,4,5) ,-O (X519-O) _y-X520 (y=1,2,3,4,5) ,-OC (O)-X521 ,-OC (O)-O-X522 ,-OC (O)-NHX523 ,-O-C (O)-NX524X525 ,-OP (O) is (OX527) (OX526), and-OSi (X528) is (X530) (X529) ,-OS (O ₂)-X531 ,-NHC (O)-X532 ,-NX533C (O)-X534 ,-NH-C (O)-O-X535 ,-NH-C (O)-NH-X536 ,-NH-C (O)-NX537X538 ,-NX539-C (O)-O-X540 ,-NX541-C (O)-NH-X542 ,-NX543-C (O)-NX544X545 ,-NHS (O ₂)-X546 ,-NX547S (O ₂)-X548 ,-S-X549 ,-S (O)-X550 ,-S (O ₂)-X551 ,-S (O ₂) NH-X552 ,-S (O ₂) NX553X554 ,-S (O ₂) O-X555 ,-P (O) is (OX557) (OX556), and-Si (X558) is (X560) (X559) ";

X509 wherein, X510, X511, X512, X513, X514, X515, X516, X517, X518, X519, X520, X521, X522; X523, X524, X525, X526, X527, X528, X529, X530, X531, X532, X533, X534, X535; X536, X537, X538, X539, X540, X541, X542, X543, X544, X545, X546, X547, X548; X549, X550, X551, X552, X553, X554, X555, X556, X557, X558, X559, X560 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, X515, X516 and/or X524; X525 and/or X537, X538 and/or X544, X545 and/or X553, X554 also can form " heterocyclic radical " in each case together;

Wherein randomly, substituting group group above-mentioned substituting group (ii) can and then be selected from following substituting group replacement by at least one independently of one another identically or differently:

(iii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF3, N ₃, NH ₂,-NHX561 ,-NX562X563 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-X564 ,-C (O) O-X565 ,-C (O) NH-X566 ,-C (O) NX567X568 ,-O-X569 ,-O are (X570-O) _z-H (z=1,2,3,4,5) ,-O (X571-O) _z-X572 (z=1,2,3,4,5) ,-OC (O)-X573 ,-OC (O)-O-X574 ,-OC (O)-NHX575 ,-O-C (O)-NX576X577 ,-OP (O) is (OX579) (OX578), and-OSi (X580) is (X582) (X581) ,-OS (O ₂)-X583 ,-NHC (O)-X584 ,-NX585C (O)-X586 ,-NH-C (O)-O-X587 ,-NH-C (O)-NH-X588 ,-NH-C (O)-NX589X590 ,-NX591-C (O)-O-X592 ,-NX593-C (O)-NH-X594 ,-NX595-C (O)-NX596X597 ,-NHS (O ₂)-X598 ,-NX599S (O ₂)-X600 ,-S-X601 ,-S (O)-X602 ,-S (O ₂)-X603 ,-S (O ₂) NH-X604 ,-S (O ₂) NX605X606 ,-S (O ₂) O-X607 ,-P (O) is (OX609) (OX608), and-Si (X610) is (X612) (X611) ";

X561 wherein, X562, X563, X564, X565, X566, X567, X568, X569, X570, X571, X572, X573, X574; X575, X576, X577, X578, X579, X580, X581, X582, X583, X584, X585, X586, X587; X588, X589, X590, X591, X592, X593, X594, X595, X596, X597, X598, X599, X600; X601, X602, X603, X604, X605, X606, X607, X608, X609, X610, X611, X612 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, X567, X568 and/or X576; X577 and/or X589, X590 and/or X596, X597 and/or X605, X606 also can form " heterocyclic radical " in each case together;

(h) unsubstituted or substituted aryl, wherein randomly, said aryl can be selected from following substituting group by at least one identically or differently and replace:

(i) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHX613 ,-NX614X615 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-X616 ,-C (O) O-X617 ,-C (O) NH-X618 ,-C (O) NX619X620 ,-O-X621 ,-O are (X622-O) _a-H (a=1,2,3,4,5) ,-O (X623-O) _a-X624 (a=1,2,3,4,5) ,-OC (O)-X625 ,-OC (O)-O-X626 ,-OC (O)-NHX627 ,-O-C (O)-NX628X629 ,-OP (O) is (OX631) (OX630), and-OSi (X632) is (X634) (X633) ,-OS (O ₂)-X635 ,-NHC (O)-X636 ,-NX637C (O)-X638 ,-NH-C (O)-O-X639 ,-NH-C (O)-NH-X64O ,-NH-C (O)-NX641X642 ,-NX643-C (O)-O-X644 ,-NX645-C (O)-NH-X646 ,-NX647-C (O)-NX648X649 ,-NHS (O ₂)-X650 ,-NX651S (O ₂)-X652 ,-S-X653 ,-S (O)-X654 ,-S (O ₂)-X655 ,-S (O ₂) NH-X656 ,-S (O ₂) NX657X658 ,-S (O ₂) O-X659 ,-P (O) is (OX661) (OX660), and-Si (X662) is (X664) (X663) ";

X613 wherein, X614, X615, X616, X617, X618, X619, X620, X621, X622, X623, X624, X625, X626; X627, X628, X629, X630, X631, X632, X633, X634, X635, X636, X637, X638, X639; X640, X641, X642, X643, X644, X645, X646, X647, X648, X649, X650, X651, X652; X653, X654, X655, X656, X657, X658, X659, X660, X661, X662, X663, X664 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, X619, X620 and/or X628; X629 and/or X641, X642 and/or X648, X649 and/or X657, X658 also can form " heterocyclic radical " in each case together;

(ii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHX665 ,-NX666X667 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-X668 ,-C (O) O-X669 ,-C (O) NH-X670 ,-C (O) NX671X672 ,-O-X673 ,-O are (X674-O) _b-H (b=1,2,3,4,5) ,-O (X675-O) _b-X676 (b=1,2,3,4,5) ,-OC (O)-X677 ,-OC (O)-O-X678 ,-OC (O)-NHX679 ,-O-C (O)-NX680X681 ,-OP (O) is (OX683) (OX682), and-OSi (X684) is (X686) (X685) ,-OS (O ₂)-X687 ,-NHC (O)-X688 ,-NX689C (O)-X690 ,-NH-C (O)-O-X691 ,-NH-C (O)-NH-X692 ,-NH-C (O)-NX693X694 ,-NX695-C (O)-O-X696 ,-NX697-C (O)-NH-X698 ,-NX699-C (O)-NX700X701 ,-NHS (O ₂)-X702 ,-NX703S (O ₂)-X704 ,-S-X705 ,-S (O)-X706 ,-S (O ₂)-X707 ,-S (O ₂) NH-X708 ,-S (O ₂) NX709X710 ,-S (O ₂) O-X711 ,-P (O) is (OX713) (OX712), and-Si (X714) is (X716) (X715) ";

X665 wherein, X666, X667, X668, X669, X670, X671, X672, X673, X674, X675, X676, X677, X678; X679, X680, X681, X682, X683, X684, X685, X686, X687, X688, X689, X690, X691; X692, X693, X694, X695, X696, X697, X698, X699, X700, X701, X702, X703, X704; X705, X706, X707, X708, X709, X710, X711, X712, X713, X714, X715, X716 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, X671, X672 and/or X680; X681 and/or X693, X694 and/or X700, X701 and/or X709, X710 also can form " heterocyclic radical " in each case together;

(iii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHX717 ,-NX718X719 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-X720 ,-C (O) O-X721 ,-C (O) NH-X722 ,-C (O) NX723X724 ,-O-X725 ,-O are (X726-O) _c-H (c=1,2,3,4,5) ,-O (X727-O) _c-X728 (c=1,2,3,4,5) ,-OC (O)-X729 ,-OC (O)-O-X730 ,-OC (O)-NHX731 ,-O-C (O)-NX732X733 ,-OP (O) is (OX735) (OX734), and-OSi (X736) is (X738) (X737) ,-OS (O ₂)-X739 ,-NHC (O)-X740 ,-NX741C (O)-X742 ,-NH-C (O)-O-X743 ,-NH-C (O)-NH-X744 ,-NH-C (O)-NX745X746 ,-NX747-C (O)-O-X748 ,-NX749-C (O)-NH-X750 ,-NX751-C (O)-NX752X753 ,-NHS (O ₂)-X754 ,-NX755S (O ₂)-X756 ,-S-X757 ,-S (O)-X758 ,-S (O ₂)-X759 ,-S (O ₂) NH-X760 ,-S (O ₂) NX761X762 ,-S (O ₂) O-X763 ,-P (O) is (OX765) (OX764), and-Si (X766) is (X768) (X767) ";

X717 wherein, X718, X719, X720, X721, X722, X723, X724, X725, X726, X727, X728, X729, X730; X731, X732, X733, X734, X735, X736, X737, X738, X739, X740, X741, X742, X743; X744, X745, X746, X747, X748, X749, X750, X751, X752, X753, X754, X755, X756; X757, X758, X759, X760, X761, X762, X763, X764, X765, X766, X767, X768 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, X723, X724 and/or X732; X733 and/or X745, X746 and/or X752, X753 and/or X761, X762 also can form " heterocyclic radical " in each case together;

(j) unsubstituted or substituted heteroaryl, wherein randomly, said heteroaryl can be selected from following substituting group by at least one identically or differently and replace:

(i) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHX769 ,-NX770X771 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-X772 ,-C (O) O-X773 ,-C (O) NH-X774 ,-C (O) NX775X776 ,-O-X777 ,-O are (X778-O) _d-H (d=1,2,3,4,5) ,-O (X779-O) _d-X780 (d=1,2,3,4,5) ,-OC (O)-X781 ,-OC (O)-O-X782 ,-OC (O)-NHX783 ,-O-C (O)-NX784X785 ,-OP (O) is (OX787) (OX786), and-OSi (X788) is (X790) (X789) ,-OS (O ₂)-X791 ,-NHC (O)-X792 ,-NX793C (O)-X794 ,-NH-C (O)-O-X795 ,-NH-C (O)-NH-X796 ,-NH-C (O)-NX797X798 ,-NX799-C (O)-O-X800 ,-NX801-C (O)-NH-X802 ,-NX803-C (O)-NX804X805 ,-NHS (O ₂)-X806 ,-NX807S (O ₂)-X808 ,-S-X809 ,-S (O)-X810 ,-S (O ₂)-X811 ,-S (O ₂) NH-X812 ,-S (O ₂) NX813X814 ,-S (O ₂) O-X815 ,-P (O) is (OX817) (OX816), and-Si (X818) is (X820) (X819) ";

X769 wherein, X770, X771, X772, X773, X774, X775, X776, X777, X778, X779, X780, X781, X782; X783, X784, X785, X786, X787, X788, X789, X790, X791, X792, X793, X794, X795; X796, X797, X798, X799, X800, X801, X802, X803, X804, X805, X806, X807, X808; X809, X810, X811, X812, X813, X814, X815, X816, X817, X818, X819, X820 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, X775, X776 and/or X784; X785 and/or X797, X798 and/or X804, X805 and/or X813, X814 also can form " heterocyclic radical " in each case together;

(ii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHX821 ,-NX822X823 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-X824 ,-C (O) O-X825 ,-C (O) NH-X826 ,-C (O) NX827X828 ,-O-X829 ,-O are (X830-O) _e-H (e=1,2,3,4,5) ,-O (X831-O) _e-X832 (e=1,2,3,4,5) ,-OC (O)-X833 ,-OC (O)-O-X834 ,-OC (O)-NHX835 ,-O-C (O)-NX836X837 ,-OP (O) is (OX839) (OX838), and-OSi (X840) is (X842) (X841) ,-OS (O ₂)-X843 ,-NHC (O)-X844 ,-NX845C (O)-X846 ,-NH-C (O)-O-X847 ,-NH-C (O)-NH-X848 ,-NH-C (O)-NX849X850 ,-NX851-C (O)-O-X852 ,-NX853-C (O)-NH-X854 ,-NX855-C (O)-NX856X857 ,-NHS (O ₂)-X858 ,-NX859S (O ₂)-X860 ,-S-X861 ,-S (O)-X862 ,-S (O ₂)-X863 ,-S (O ₂) NH-X864 ,-S (O ₂) NX865X866 ,-S (O ₂) O-X867 ,-P (O) is (OX869) (OX868), and-Si (X870) is (X872) (X871) ";

X821 wherein, X822, X823, X824, X825, X826, X827, X828, X829, X830, X831, X832, X833, X834; X835, X836, X837, X838, X839, X840, X841, X842, X843, X844, X845, X846, X847; X848, X849, X850, X851, X852, X853, X854, X855, X856, X857, X858, X859, X860; X861, X862, X863, X864, X865, X866, X867, X868, X869, X870, X871, X872 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, X827, X828 and/or X836; X837 and/or X849, X850 and/or X856, X857 and/or X865, X866 also can form " heterocyclic radical " in each case together;

(iii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHX873 ,-NX874X875 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-X876 ,-C (O) O-X877 ,-C (O) NH-X878 ,-C (O) NX879X880 ,-O-X881 ,-O are (X882-O) _f-H (f=1,2,3,4,5) ,-O (X883-O) _f-X884 (f=1,2,3,4,5) ,-OC (O)-X885 ,-OC (O)-O-X886 ,-OC (O)-NHX887 ,-O-C (O)-NX888X889 ,-OP (O) is (OX891) (OX890), and-OSi (X892) is (X894) (X893) ,-OS (O ₂)-X895 ,-NHC (O)-X896 ,-NX897C (O)-X898 ,-NH-C (O)-O-X899 ,-NH-C (O)-NH-X900 ,-NH-C (O)-NX901X902 ,-NX903-C (O)-O-X904 ,-NX905-C (O)-NH-X906 ,-NX907-C (O)-NX908X909 ,-NHS (O ₂)-X910 ,-NX911S (O ₂)-X912 ,-S-X913 ,-S (O)-X914 ,-S (O ₂)-X915 ,-S (O ₂) NH-X916 ,-S (O ₂) NX917X918 ,-S (O ₂) O-X919 ,-P (O) is (OX921) (OX920), and-Si (X922) is (X924) (X923) ";

X873 wherein, X874, X875, X876, X877, X878, X879, X880, X881, X882, X883, X884, X885, X886; X887, X888, X889, X890, X891, X892, X893, X894, X895, X896, X897, X898, X899; X900, X901, X902, X903, X904, X905, X906, X907, X908, X909, X910, X911, X912; X913, X914, X915, X916, X917, X918, X919, X920, X921, X922, X923, X924 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, X879, X880 and/or X888; X889 and/or X901, X902 and/or X908, X909 and/or X917, X918 also can form " heterocyclic radical " in each case together;

(k) OZ6, wherein Z6 is independently selected from:

(i) " hydrogen, alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl ";

(ii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHX925 ,-NX926X927 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-X928 ,-C (O) O-X929 ,-C (O) NH-X930 ,-C (O) NX931X932 ,-O-X933 ,-O are (X934-O) _g-H (g=1,2,3,4,5) ,-O (X935-O) _g-X936 (g=1,2,3,4,5) ,-OC (O)-X937 ,-OC (O)-O-X938 ,-OC (O)-NHX939 ,-O-C (O)-NX940X941 ,-OP (O) is (OX943) (OX942), and-OSi (X944) is (X946) (X945) ,-OS (O ₂)-X947 ,-NHC (O)-X948 ,-NX949C (O)-X950 ,-NH-C (O)-O-X951 ,-NH-C (O)-NH-X952 ,-NH-C (O)-NX953X954 ,-NX955-C (O)-O-X956 ,-NX957-C (O)-NH-X958 ,-NX959-C (O)-NX960X961 ,-NHS (O ₂)-X962 ,-NX963S (O ₂)-X964 ,-S-X965 ,-S (O)-X966 ,-S (O ₂)-X967 ,-S (O ₂) NH-X968 ,-S (O ₂) NX969X970 ,-S (O ₂) O-X971 ,-P (O) is (OX973) (OX972), and-Si (X974) is (X976) (X975) ";

X925 wherein, X926, X927, X928, X929, X930, X931, X932, X933, X934, X935, X936, X937, X938; X939, X940, X941, X942, X943, X944, X945, X946, X947, X948, X949, X950, X951; X952, X953, X954, X955, X956, X957, X958, X959, X960, X961, X962, X963, X964; X965, X966, X967, X968, X969, X970, X971, X972, X973, X974, X975, X976 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, X931, X932 and/or X940; X941 and/or X953, X954 and/or X960, X961 and/or X969, X970 also can form " heterocyclic radical " in each case together;

(iii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHX977 ,-NX978X979 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-X980 ,-C (O) O-X981 ,-C (O) NH-X982 ,-C (O) NX983X984 ,-O-X985 ,-O are (X986-O) _h-H (h=1,2,3,4,5) ,-O (X987-O) _h-X988 (h=1,2,3,4,5) ,-OC (O)-X989 ,-OC (O)-O-X990 ,-OC (O)-NHX991 ,-O-C (O)-NX992X993 ,-OP (O) is (OX995) (OX994), and-OSi (X996) is (X998) (X997) ,-OS (O ₂)-X999 ,-NHC (O)-X1000 ,-NX1001C (O)-X1002 ,-NH-C (O)-O-X1003;-NH-C (O)-NH-X1004 ,-NH-C (O)-NX1005X1006 ,-NX1007-C (O)-O-X1008;-NX1009-C (O)-NH-X1010 ,-NX1011-C (O)-NX1012X1013 ,-NHS (O ₂)-X1014 ,-NX1015S (O ₂)-X1016 ,-S-X1017 ,-S (O)-X1018 ,-S (O ₂)-X1019 ,-S (O ₂) NH-X1020 ,-S (O ₂) NX1021X1022 ,-S (O ₂) O-X1023 ,-P (O) is (OX1025) (OX1024), and-Si (X1026) is (X1028) (X1027) ";

X977 wherein, X978, X979, X980, X981, X982, X983, X984, X985, X986, X987; X988, X989, X990, X991, X992, X993, X994, X995, X996, X997, X998; X999, X1000, X1001, X1002, X1003, X1004, X1005, X1006, X1007, X1008, X1009; X1010, X1011, X1012, X1013, X1014, X1015, X1016, X1017, X1018, X1019; X1020, X1021, X1022, X1023, X1024, X1025, X1026, X1027, X1028 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, X983, X984 and/or X992; X993 and/or X1005, X1006 and/or X1012, X1013 and/or X1021, X1022 also can form " heterocyclic radical " in each case together;

(1) SZ7, wherein Z7 is independently selected from:

(ii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHX1029 ,-NX1030X1031 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-X1032 ,-C (O) O-X1033 ,-C (O) NH-X1034 ,-C (O) NX1035X1036 ,-O-X1037 ,-O are (X1038-O) _i-H (i=1,2,3,4,5) ,-O (X1039-O) _i-X1040 (i=1,2,3,4,5) ,-OC (O)-X1041 ,-OC (O)-O-X1042 ,-OC (O)-NHX1043 ,-O-C (O)-NX1044X1045 ,-OP (O) is (OX1047) (OX1046), and-OSi (X1048) is (X1050) (X1049) ,-OS (O ₂)-X1051 ,-NHC (O)-X1052 ,-NX1053C (O)-X1054 ,-NH-C (O)-O-X1055;-NH-C (O)-NH-X1056 ,-NH-C (O)-NX1057X1058 ,-NX1059-C (O)-O-X1060;-NX1061-C (O)-NH-X1062 ,-NX1063-C (O)-NX1064X1065 ,-NHS (O ₂)-X1066 ,-NX1067S (O ₂)-X1068 ,-S-X1069 ,-S (O)-X1070 ,-S (O ₂)-X1071 ,-S (O ₂) NH-X1072 ,-S (O ₂) NX1073X1074 ,-S (O ₂) O-X1075 ,-P (O) is (OX1077) (OX1076), and-Si (X1078) is (X1080) (X1079) ";

X1029 wherein, X1030, X1031, X1032, X1033, X1034, X1035, X1036, X1037, X1038, X1039; X1040, X1041, X1042, X1043, X1044, X1045, X1046, X1047, X1048, X1049, X1050; X1051, X1052, X1053, X1054, X1055, X1056, X1057, X1058, X1059, X1060, X1061; X1062, X1063, X1064, X1065, X1066, X1067, X1068, X1069, X1070, X1071; X1072, X1073, X1074, X1075, X1076, X1077, X1078, X1079, X1080 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, X1035, X1036 and/or X1044; X1045 and/or X1057, X1058 and/or X1064, X1065 and/or X1073, X1074 also can form " heterocyclic radical " in each case together;

(iii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHX1081 ,-NX1082X1083 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-X1084 ,-C (O) O-X1085 ,-C (O) NH-X1086 ,-C (O) NX1087X1088 ,-O-X1089 ,-O are (X1090-O) _j-H (j=1,2,3,4,5) ,-O (X1091-O) _j-X1092 (j=1,2,3,4,5) ,-OC (O)-X1093 ,-OC (O)-O-X1094 ,-OC (O)-NHX1095 ,-O-C (O)-NX1096X1097 ,-OP (O) is (OX1099) (OX1098), and-OSi (X1100) is (X1102) (X1101) ,-OS (O ₂)-X1103 ,-NHC (O)-X1104 ,-NX1105C (O)-X1106 ,-NH-C (O)-O-X1107;-NH-C (O)-NH-X1108 ,-NH-C (O)-NX1109X1110 ,-NX1111-C (O)-O-X1112;-NX1113-C (O)-NH-X1114 ,-NX1115-C (O)-NX1116X1117 ,-NHS (O ₂)-X1118 ,-NX1119S (O ₂)-X1120 ,-S-X1121 ,-S (O)-X1122 ,-S (O ₂)-X1123 ,-S (O ₂) NH-X1124 ,-S (O ₂) NX1125X1126 ,-S (O ₂) O-X1127 ,-P (O) is (OX1129) (OX1128), and-Si (X1130) is (X1132) (X1131) ";

X1081 wherein, X1082, X1083, X1084, X1085, X1086, X1087, X1088, X1089, X1090, X1091; X1092, X1093, X1094, X1095, X1096, X1097, X1098, X1099, X1100, X1101, X1102; X1103, X1104, X1105, X1106, X1107, X1108, X1109, X1110, X1111, X1112, X1113; X1114, X1115, X1116, X1117, X1118, X1119, X1120, X1121, X1122, X1123; X1124, X1125, X1126, X1127, X1128, X1129, X1130, X1131, X1132 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, X1087, X1088 and/or X1096; X1097 and/or X1109, X1110 and/or X1116, X1117 and/or X1125, X1126 also can form " heterocyclic radical " in each case together;

(m) NZ8Z9, Z8 wherein, Z9 is selected from independently of one another:

(i) " hydrogen, alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl ,-C (O)-X1133 ,-C (O) O-X1134 ,-C (O)-NX1135X1136 ,-S (O ₂)-X1137 ,-S (O ₂) O-X1138 ";

X1133 wherein, X1134, X1135, X1136, X1137, X1138 is selected from independently of one another: hydrogen, alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl " and wherein, perhaps, X1135, X1136 also can form " heterocyclic radical " together;

(ii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHX1139 ,-NX1140X1141 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-X1142 ,-C (O) O-X1143 ,-C (O) NH-X1144 ,-C (O) NX1145X1146 ,-O-X1147 ,-O are (X1148-O) _k-H (k=1,2,3,4,5) ,-O (X1149-O) _k-X1150 (k=1,2,3,4,5) ,-OC (O)-X1151 ,-OC (O)-O-X1152 ,-OC (O)-NHX1153 ,-O-C (O)-NX1154X1155 ,-OP (O) is (OX1157) (OX1156), and-OSi (X1158) is (X1160) (X1159) ,-OS (O ₂)-X1161 ,-NHC (O)-X1162 ,-NX1163C (O)-X1164 ,-NH-C (O)-O-X1165;-NH-C (O)-NH-X1166 ,-NH-C (O)-NX1167X1168 ,-NX1169-C (O)-O-X1170;-NX1171-C (O)-NH-X1172 ,-NX1173-C (O)-NX1174X1175 ,-NHS (O ₂)-X1176 ,-NX1177S (O ₂)-X1178 ,-S-X1179 ,-S (O)-X1180 ,-S (O ₂)-X1181 ,-S (O ₂) NH-X1182 ,-S (O ₂) NX1183X1184 ,-S (O ₂) O-X1185 ,-P (O) is (OX1187) (OX1186), and-Si (X1188) is (X1190) (X1189) ";

X1139 wherein, X1140, X1141, X1142, X1143, X1144, X1145, X1146, X1147, X1148, X1149; X1150, X1151, X1152, X1153, X1154, X1155, X1156, X1157, X1158, X1159, X1160; X1161, X1162, X1163, X1164, X1165, X1166, X1167, X1168, X1169, X1170, X1171; X1172, X1173, X1174, X1175, X1176, X1177, X1178, X1179, X1180, X1181; X1182, X1183, X1184, X1185, X1186, X1187, X1188, X1189, X1190 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, X1145, X1146 and/or X1154; X1155 and/or X1167, X1168 and/or X1174, X1175 and/or X1183, X1184 also can form " heterocyclic radical " in each case together;

(iii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHX1191 ,-NX1192X1193 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-X1194 ,-C (O) O-X1195 ,-C (O) NH-X1196 ,-C (O) NX1197X1198 ,-O-X1199 ,-O are (X1200-O) _l-H (1=1,2,3,4,5) ,-O (X1201-O) _l-X1202 (1=1,2,3,4,5) ,-OC (O)-X1203 ,-OC (O)-O-X1204 ,-OC (O)-NHX1205 ,-O-C (O)-NX1206X1207 ,-OP (O) is (OX1209) (OX1208), and-OSi (X1210) is (X1212) (X1211) ,-OS (O ₂)-X1213 ,-NHC (O)-X1214 ,-NX1215C (O)-X1216 ,-NH-C (O)-O-X1217;-NH-C (O)-NH-X1218 ,-NH-C (O)-NX1219X1220 ,-NX1221-C (O)-O-X1222;-NX1223-C (O)-NH-X1224 ,-NX1225-C (O)-NX1226X1227 ,-NHS (O ₂)-X1228 ,-NX1229S (O ₂)-X1230 ,-S-X1231 ,-S (O)-X1232 ,-S (O ₂)-X1233 ,-S (O ₂) NH-X1234 ,-S (O ₂) NX1235X1236 ,-S (O ₂) O-X1237 ,-P (O) is (OX1239) (OX1238), and-Si (X1240) is (X1242) (X1241) ";

X1191 wherein, X1192, X1193, X1194, X1195, X1196, X1197, X1198, X1199, X1200, X1201; X1202, X1203, X1204, X1205, X1206, X1207, X1208, X1209, X1210, X1211, X1212; X1213, X1214, X1215, X1216, X1217, X1218, X1219, X1220, X1221, X1222, X1223; X1224, X1225, X1226, X1227, X1228, X1229, X1230, X1231, X1232, X1233; X1234, X1235, X1236, X1237, X1238, X1239, X1240, X1241, X1242 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, X1197, X1198 and/or X1206; X1207 and/or X1219, X1220 and/or X1226, X1227 and/or X1235, X1236 also can form " heterocyclic radical " in each case together;

Or

(B) one of Z3, Z4 group or Z3, Z4 group the two be " substituted heteroaryl " independently, wherein " substituted heteroaryl " is selected from following substituting group by at least one and replaces:

(a) " alkyl, naphthenic base, heterocyclic radical, aryl, heteroaryl ,-NH-V1 ,-N (alkyl) ₂,-NHC (O)-alkyl ,-NHC (O)-naphthenic base ,-NHC (O)-heterocyclic radical ,-NHC (O)-aryl ,-NHC (O)-heteroaryl ,-NHC (O)-arylalkyl ,-NHC (O)-heteroarylalkyl ,-NHS (O ₂)-alkyl ,-NHS (O ₂)-naphthenic base ,-NHS (O ₂)-heterocyclic radical ,-NHS (O ₂)-aryl ,-NHS (O ₂)-heteroaryl ,-NHS (O ₂)-arylalkyl ,-NHS (O ₂)-heteroarylalkyl ,-S-alkyl ,-S-aryl ,-S-heteroaryl ,-O-alkyl;-O-naphthenic base ,-O-cycloalkylalkyl ,-O-aryl ,-O-arylalkyl ,-O-heteroaryl;-O-heteroarylalkyl ,-O-heterocyclic radical alkyl ,-OC (O)-alkyl ,-OC (O)-naphthenic base ,-OC (O)-heterocyclic radical;-OC (O)-aryl ,-OC (O)-heteroaryl ,-OC (O)-arylalkyl ,-OC (O)-heteroarylalkyl ,-OS (O ₂)-alkyl ,-OS (O ₂)-naphthenic base ,-OS (O ₂)-heterocyclic radical ,-OS (O ₂)-aryl ,-OS (O ₂)-heteroaryl ,-OS (O ₂)-arylalkyl ,-OS (O ₂)-heteroarylalkyl ,-C (O)-alkyl ,-C (O)-aryl ,-C (O)-heteroaryl ,-C (O) O-V2 ,-C (O) NH-V3 ,-C (O) N (alkyl) ₂,-C (O) N (naphthenic base) ₂,-C (O) N (aryl) ₂,-C (O) N (heteroaryl) ₂,-S (O ₂) the NH-alkyl ,-S (O ₂) the NH-aryl ,-S (O ₂) the NH-heteroaryl ,-S (O ₂) the NH-arylalkyl ,-S (O ₂) the O-alkyl ,-S (O ₂) the O-aryl ,-S (O ₂) the O-arylalkyl ";

V1 wherein, V2, V3 is selected from independently of one another: " alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl ";

(i) " (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, N ₃,-NH-naphthenic base ,-NH-cycloalkylalkyl ,-NH-heteroaryl ,-NH-heteroarylalkyl ,-NH-arylalkyl ,-NH-heterocyclic radical;-NH-heterocyclic radical alkyl ,-NV4V5 ,-S-naphthenic base ,-S-cycloalkylalkyl ,-S-aryl ,-S-arylalkyl;-S-heteroaryl ,-S-heteroarylalkyl ,-S-heterocyclic radical ,-S-heterocyclic radical alkyl ,-O-naphthenic base ,-O-cycloalkylalkyl;-O-arylalkyl ,-O-heteroaryl ,-O-heteroarylalkyl ,-O-heterocyclic radical ,-O-heterocyclic radical alkyl ,-O is (V6-O) _p-H (p=1,2,3,4,5) ,-O (V7-O) _p-V8 (p=1,2,3,4,5) ,-OP (O) is (OV 10) (OV9) ,-C (O) O-V11 ,-C (O) NH ₂,-C (O) NH-V12 ,-C (O) NV13V14 ,-S (O ₂)-V15 ,-P (O) (OH) ₂,-P (O) is (OV17) (OV16), and-Si (V18) is (V20) (V19), and-O-Si (V21) is (V23) (V22);-O-C (O)-O-V24 ,-O-C (O)-NH-V25 ,-O-C (O)-NV26V27 ,-NH-C (O)-O-V28;-NH-C (O)-NH-V29 ,-NH-C (O)-NV30V31 ,-NV32-C (O)-O-V33;-NV34-C (O)-NH-V35 ,-NV36-C (O)-NV37V38 ,-NV39-S (O ₂)-V40 ,-NH-S (O ₂)-V41 ,-O-S (O ₂)-V42 ,-NH-C (O)-V43 ,-NV44-C (O)-V45 ,-C (O)-V46 ,-OC (O)-V47 ,-S (O)-V48 ,-S (O ₂)-NHV49 ,-S (O ₂)-NV50V51 ,-S (O ₂)-OV52 ";

V4 wherein, V5, V6, V7, V8, V9, V10, V11, V12, V13, V14, V15, V16; V17, V18, V19, V20, V21, V22, V23, V24, V25, V26, V27, V28, V29; V30, V31, V32, V33, V34, V35, V36, V37, V38, V39, V40, V41; V42, V43, V44, V45, V46, V47, V48, V49, V50, V51, V52 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl; Arylalkyl, heteroaryl, heteroarylalkyl " and wherein, perhaps, V13; V14 and/or V26, V27 and/or V30, V31 and/or V37, V38 and/or V50, V51 also can form " heterocyclic radical " together;

(b) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHV53 ,-NV54V55 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-V56 ,-C (O) O-V57 ,-C (O) NH-V58 ,-C (O) NV59V60 ,-O-V61 ,-O are (V62-O) _r-H (r=1,2,3,4,5) ,-O (V63-O) _r-V64 (r=1,2,3,4,5) ,-OC (O)-V65 ,-OC (O)-O-V66 ,-OC (O)-NHV67 ,-O-C (O)-NV68V69 ,-OP (O) is (OV71) (OV70), and-OSi (V72) is (V74) (V73) ,-OS (O ₂)-V75 ,-NHC (O)-V76 ,-NV77C (O)-V78 ,-NH-C (O)-O-V79 ,-NH-C (O)-NH-V80 ,-NH-C (O)-NV81V82 ,-NV83-C (O)-O-V84 ,-NV85-C (O)-NH-V86 ,-NV87-C (O)-NV88V89 ,-NHS (O ₂)-V90 ,-NV91S (O ₂)-V92 ,-S-V93 ,-S (O)-V94 ,-S (O ₂)-V95 ,-S (O ₂) NH-V96 ,-S (O ₂) NV97V98 ,-S (O ₂) O-V99 ,-P (O) is (OV101) (OV100), and-Si (V102) is (V104) (V103) ";

V53 wherein, V54, V55, V56, V57, V58, V59, V60, V61, V62, V63, V64, V65, V66; V67, V68, V69, V70, V71, V72, V73, V74, V75, V76, V77, V78, V79; V80, V81, V82, V83, V84, V85, V86, V87, V88, V89, V90, V91, V92; V93, V94, V95, V96, V97, V98, V99, V100, V101, V102, V103, V104 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl; Arylalkyl, heteroaryl, heteroarylalkyl " and wherein, perhaps, V59; V60 and/or V68, V69 and/or V81, V82 and/or V88, V89 and/or V97, V98 also can form " heterocyclic radical " together;

(ii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHV105 ,-NV106V107 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-V108 ,-C (O) O-V109 ,-C (O) NH-V110 ,-C (O) NV111V112 ,-O-V113 ,-O are (V114-O) _s-H (s=1,2,3,4,5) ,-O (V115-O) _s-V116 (s=1,2,3,4,5) ,-OC (O)-V117 ,-OC (O)-O-V118 ,-OC (O)-NHV119 ,-O-C (O)-NV120V121 ,-OP (O) is (OV123) (OV122), and-OSi (V124) is (V126) (V125) ,-OS (O ₂)-V127 ,-NHC (O)-V128 ,-NV129C (O)-V130 ,-NH-C (O)-O-V131 ,-NH-C (O)-NH-V132 ,-NH-C (O)-NV133V134 ,-NV135-C (O)-O-V136 ,-NV137-C (O)-NH-V138 ,-NV139-C (O)-NV140V141 ,-NHS (O ₂)-V142 ,-NV143S (O ₂)-V144 ,-S-V145 ,-S (O)-V146 ,-S (O ₂)-V147 ,-S (O ₂) NH-V148 ,-S (O ₂) NV149V150 ,-S (O ₂) O-V151 ,-P (O) is (OV153) (OV152), and-Si (V154) is (V156) (V155) ";

V105 wherein, V106, V107, V108, V109, V110, V111, V112, V113, V114, V115, V116, V117, V118; V119, V120, V121, V122, V123, V124, V125, V126, V127, V128, V129, V130, V131; V132, V133, V134, V135, V136, V137, V138, V139, V140, V141, V142, V143, V144; V145, V146, V147, V148, V149, V150, V151, V152, V153, V154, V155, V156 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl; Arylalkyl, heteroaryl, heteroarylalkyl " and wherein, perhaps, V111; V112 and/or V120, V121 and/or V133, V134 and/or V140, V141 and/or V149, V150 also can form " heterocyclic radical " together;

(iii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHV157 ,-NV158V159 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-V160 ,-C (O) O-V161 ,-C (O) NH-V162 ,-C (O) NV163V164 ,-O-V165 ,-O are (V166-O) _t-H (t=1,2,3,4,5) ,-O (V167-O) _t-V168 (t=1,2,3,4,5) ,-OC (O)-V169 ,-OC (O)-O-V170 ,-OC (O)-NHV171 ,-O-C (O)-NV172V173 ,-OP (O) is (OV175) (OV174), and-OSi (V176) is (V178) (V177) ,-OS (O ₂)-V179 ,-NHC (O)-V180 ,-NV181C (O)-V182 ,-NH-C (O)-O-V183 ,-NH-C (O)-NH-V184 ,-NH-C (O)-NV185V186 ,-NV187-C (O)-O-V188 ,-NV189-C (O)-NH-V190 ,-NV191-C (O)-NV192V193 ,-NHS (O ₂)-V194 ,-NV195S (O ₂)-V196 ,-S-V197 ,-S (O)-V198 ,-S (O ₂)-V199 ,-S (O ₂) NH-V200 ,-S (O ₂) NV201V202 ,-S (O ₂) O-V203 ,-P (O) is (OV205) (OV204), and-Si (V206) is (V208) (V207) ";

V157 wherein, V158, V159, V160, V161, V162, V163, V164, V165, V166, V167, V168, V169, V170; V171, V172, V173, V174, V175, V176, V177, V178, V179, V180, V181, V182, V183; V184, V185, V186, V187, V188, V189, V190, V191, V192, V193, V194, V195, V196; V197, V198, V199, V200, V201, V202, V203, V204, V205, V206, V207, V208 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl; Arylalkyl, heteroaryl, heteroarylalkyl " and wherein, perhaps, V163; V164 and/or V172, V173 and/or V185, V186 and/or V192, V193 and/or V201, V202 also can form " heterocyclic radical " together;

OrThe two is " substituted heteroaryl " independently for one of Z3, Z4 group or Z3, Z4 group, and wherein " substituted heteroaryl " is by at least one identical ground or different are selected from following substituting group and replace:

(c) " (C ₉-C ₃₀) alkyl ,-NV209V210 ,-NH-(C ₉-C ₃₀) alkyl ,-NHC (O)-cycloalkylalkyl ,-NHC (O)-heterocyclic radical alkyl ,-NHC (O)-(C ₉-C ₃₀) alkyl ,-NV211C (O)-V212 ,-NV213C (O)-(C ₉-C ₃₀) alkyl ,-NHC (O)-OV214 ,-NV215C (O)-OV216 ,-NHC (O)-NHV217 ,-NHC (O)-NV218V219 ,-NV220C (O)-NHV221 ,-NV222C (O)-NV223V224 ,-NHS (O ₂)-cycloalkylalkyl ,-NHS (O ₂)-heterocyclic radical alkyl ,-NV225S (O ₂)-V226 ,-O-heterocyclic radical ,-O-(C ₉-C ₃₀) alkyl ,-S-naphthenic base ,-S-heterocyclic radical ,-S-arylalkyl ,-S-heteroarylalkyl ,-S-cycloalkylalkyl ,-S-heterocyclic radical alkyl ,-S-(C ₉-C ₃₀) alkyl ,-OC (O)-cycloalkylalkyl ,-OC (O)-heterocyclic radical alkyl ,-OC (O)-(C ₉-C ₃₀) alkyl ,-OC (O)-OV227 ,-OC (O)-NHV228 ,-OC (O)-NV229V230 ,-OP (O) is (OV232) (OV231) ,-OS (O ₂)-cycloalkylalkyl ,-OS (O ₂)-heterocyclic radical alkyl ,-OS (O ₂)-(C ₉-C ₃₀) alkyl ,-C (O)-naphthenic base ,-C (O)-heterocyclic radical ,-C (O)-arylalkyl ,-C (O)-heteroarylalkyl ,-C (O)-cycloalkylalkyl ,-C (O)-heterocyclic radical alkyl ,-C (O)-(C ₉-C ₃₀) alkyl ,-C (O) O-(C ₉-C ₃₀) alkyl ,-C (O) NH-(C ₉-C ₃₀) alkyl ,-C (O) NV233V234 ,-C (O) NH-OV235 ,-C (O) NV236-OV237 ,-C (O) NH-NV238V239 ,-C (O) NV240-NV241V242 ,-S (O)-V243 ,-S (O ₂)-V244 ,-S (O ₂) the NH-naphthenic base ,-S (O ₂) the NH-heterocyclic radical ,-S (O ₂) the NH-heteroarylalkyl ,-S (O ₂) the NH-cycloalkylalkyl ,-S (O ₂) NH-heterocyclic radical alkyl ,-S (O ₂) NH-(C ₉-C ₃₀) alkyl ,-S (O ₂) the O-naphthenic base ,-S (O ₂) the O-heterocyclic radical ,-S (O ₂) the O-heteroaryl ,-S (O ₂) the O-heteroarylalkyl ,-S (O ₂) the O-cycloalkylalkyl ,-S (O ₂) O-heterocyclic radical alkyl ,-S (O ₂) O-(C ₉-C ₃₀) alkyl ,-P (O) is (OH) ₂,-P (O) is (OV246) (OV245), and-Si (V247) is (V249) (V248) ,-O-Si (V250) is (V252) (V251) ";

V209 wherein, V210, V211, V212, V213, V214, V215, V216, V217, V218, V219, V220; V221, V222, V223, V224, V225, V226, V227, V228, V229, V230, V231; V232, V233, V234, V235, V236, V237, V238, V239, V240, V241, V242; V243, V244, V245, V246, V247, V248, V249, V250, V251, V252 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl; Aryl, arylalkyl, heteroaryl, heteroarylalkyl " and wherein; perhaps, V218, V219 and/or V223, V224 and/or V229; V230 and/or V233, V234 and/or V238, V239 and/or V241, V242 also can form " heterocyclic radical " together;

(i) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHV253 ,-NV254V255 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-V256 ,-C (O) O-V257 ,-C (O) NH-V258 ,-C (O) NV259V260 ,-O-V261 ,-O are (V262-O) _u-H (u=1,2,3,4,5) ,-O (V263-O) _u-V264 (u=1,2,3,4,5) ,-OC (O)-V265 ,-OC (O)-O-V266 ,-OC (O)-NHV267 ,-O-C (O)-NV268V269 ,-OP (O) is (OV271) (OV270), and-OSi (V272) is (V274) (V273) ,-OS (O ₂)-V275 ,-NHC (O)-V276 ,-NV277C (O)-V278 ,-NH-C (O)-O-V279 ,-NH-C (O)-NH-V280 ,-NH-C (O)-NV281V282 ,-NV283-C (O)-O-V284 ,-NV285-C (O)-NH-V286 ,-NV287-C (O)-NV288V289 ,-NHS (O ₂)-V290 ,-NV291S (O ₂)-V292 ,-S-V293 ,-S (O)-V294 ,-S (O ₂)-V295 ,-S (O ₂) NH-V296 ,-S (O ₂) NV297V298 ,-S (O ₂) O-V299 ,-P (O) is (OV301) (OV300), and-Si (V302) is (V304) (V303) ";

V253 wherein, V254, V255, V256, V257, V258, V259, V260, V261, V262, V263, V264, V265, V266; V267, V268, V269, V270, V271, V272, V273, V274, V275, V276, V277, V278, V279; V280, V281, V282, V283, V284, V285, V286, V287, V288, V289, V290, V291, V292; V293, V294, V295, V296, V297, V298, V299, V300, V301, V302, V303, V304 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl; Arylalkyl, heteroaryl, heteroarylalkyl " and wherein, perhaps, V259; V260 and/or V268, V269 and/or V281, V282 and/or V288, V289 and/or V297, V298 also can form " heterocyclic radical " together;

(d) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHV305 ,-NV306V307 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-V308 ,-C (O) O-V309 ,-C (O) NH-V310 ,-C (O) NV311V312 ,-O-V313 ,-O are (V314-O) _v-H (v=1,2,3,4,5) ,-O (V315-O) _v-V316 (v=1,2,3,4,5) ,-OC (O)-V317 ,-OC (O)-O-V318 ,-OC (O)-NHV319 ,-O-C (O)-NV320V321 ,-OP (O) is (OV323) (OV322), and-OSi (V324) is (V326) (V325) ,-OS (O ₂)-V327 ,-NHC (O)-V328 ,-NV329C (O)-V330 ,-NH-C (O)-O-V331 ,-NH-C (O)-NH-V332 ,-NH-C (O)-NV333V334 ,-NV335-C (O)-O-V336 ,-NV337-C (O)-NH-V338 ,-NV339-C (O)-NV340V341 ,-NHS (O ₂)-V342 ,-NV343S (O ₂)-V344 ,-S-V345 ,-S (O)-V346 ,-S (O ₂)-V347 ,-S (O ₂) NH-V348 ,-S (O ₂) NV349V350 ,-S (O ₂) O-V351 ,-P (O) is (OV353) (OV352), and-Si (V354) is (V356) (V355) ";

V305 wherein, V306, V307, V308, V309, V310, V311, V312, V313, V314, V315, V316, V317, V318; V319, V320, V321, V322, V323, V324, V325, V326, V327, V328, V329, V330, V331; V332, V333, V334, V335, V336, V337, V338, V339, V340, V341, V342, V343, V344; V345, V346, V347, V348, V349, V350, V351, V352, V353, V354, V355, V356 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl; Arylalkyl, heteroaryl, heteroarylalkyl " and wherein, perhaps, V311; V312 and/or V320, V321 and/or V333, V334 and/or V340, V341 and/or V349, V350 also can form " heterocyclic radical " together;

(ii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHV357 ,-NV358V359 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-V360 ,-C (O) O-V361 ,-C (O) NH-V362 ,-C (O) NV363V364 ,-O-V365 ,-O are (V366-O) _w-H (w=1,2,3,4,5) ,-O (V367-O) _w-V368 (w=1,2,3,4,5) ,-OC (O)-V369 ,-OC (O)-O-V370 ,-OC (O)-NHV371 ,-O-C (O)-NV372V373 ,-OP (O) is (OV375) (OV374), and-OSi (V376) is (V378) (V377) ,-OS (O ₂)-V379 ,-NHC (O)-V380 ,-NV381C (O)-V382 ,-NH-C (O)-O-V383 ,-NH-C (O)-NH-V384 ,-NH-C (O)-NV385V386 ,-NV387-C (O)-O-V388 ,-NV389-C (O)-NH-V390 ,-NV391-C (O)-NV392V393 ,-NHS (O ₂)-V394 ,-NV395S (O ₂)-V396 ,-S-V397 ,-S (O)-V398 ,-S (O ₂)-V399 ,-S (O ₂) NH-V400 ,-S (O ₂) NV401V402 ,-S (O ₂) O-V403 ,-P (O) is (OV405) (OV404), and-Si (V406) is (V408) (V407) ";

V357 wherein, V358, V359, V360, V361, V362, V363, V364, V365, V366, V367, V368, V369, V370; V371, V372, V373, V374, V375, V376, V377, V378, V379, V380, V381, V382, V383; V384, V385, V386, V387, V388, V389, V390, V391, V392, V393, V394, V395, V396; V397, V398, V399, V400, V401, V402, V403, V404, V405, V406, V407, V408 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl; Arylalkyl, heteroaryl, heteroarylalkyl " and wherein, perhaps, V363; V364 and/or V372, V373 and/or V385, V386 and/or V392, V393 and/or V401, V402 also can form " heterocyclic radical " together;

(iii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHV409 ,-NV410V411 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-V412 ,-C (O) O-V413 ,-C (O) NH-V414 ,-C (O) NV415V416 ,-O-V417 ,-O are (V418-O) _x-H (x=1,2,3,4,5) ,-O (V419-O) _x-V420 (x=1,2,3,4,5) ,-OC (O)-V421 ,-OC (O)-O-V422 ,-OC (O)-NHV423 ,-O-C (O)-NV424V425 ,-OP (O) is (OV427) (OV426), and-OSi (V428) is (V430) (V429) ,-OS (O ₂)-V431 ,-NHC (O)-V432 ,-NV433C (O)-V434 ,-NH-C (O)-O-V435 ,-NH-C (O)-NH-V436 ,-NH-C (O)-NV437V438 ,-NV439-C (O)-O-V440 ,-NV441-C (O)-NH-V442 ,-NV443-C (O)-NV444V445 ,-NHS (O ₂)-V446 ,-NV447S (O ₂)-V448 ,-S-V449 ,-S (O)-V450 ,-S (O ₂)-V451 ,-S (O ₂) NH-V452 ,-S (O ₂) NV453V454 ,-S (O ₂) O-V455 ,-P (O) is (OV456b) (OV456a), and-Si (V456c) is (V456e) (V456d) ";

V409 wherein, V410, V411, V412, V413, V414, V415, V416, V417, V418, V419, V420, V421, V422; V423, V424, V425, V426, V427, V428, V429, V430, V431, V432, V433, V434, V435; V436, V437, V438, V439, V440, V441, V442, V443, V444, V445, V446, V447, V448; V449, V450, V451, V452, V453, V454, V455, V456a, V456b, V456c, V456d, V456e is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl; Arylalkyl, heteroaryl, heteroarylalkyl " and wherein, perhaps, V415; V416 and/or V424, V425 and/or V437, V438 and/or V444, V445 and/or V453, V454 also can form " heterocyclic radical " together;

AndOne of Z3, Z4 group or Z3, Z4 group none are independently selected from:

(e) hydrogen;

(f) halogen, F, Cl, Br, I;

(i) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHV457 ,-NV458V459 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-V460 ,-C (O) O-V461 ,-C (O) NH-V462 ,-C (O) NV463V464 ,-O-V465 ,-O are (V466-O) _y-H (y=1,2,3,4,5) ,-O (V467-O) _y-V468 (y=1,2,3,4,5) ,-OC (O)-V469 ,-OC (O)-O-V470 ,-OC (O)-NHV471 ,-O-C (O)-NV472V473 ,-OP (O) is (OV475) (OV474), and-OSi (V476) is (V478) (V477) ,-OS (O ₂)-V479 ,-NHC (O)-V480 ,-NV481C (O)-V482 ,-NH-C (O)-O-V483 ,-NH-C (O)-NH-V484 ,-NH-C (O)-NV485V486 ,-NV487-C (O)-O-V488 ,-NV489-C (O)-NH-V490 ,-NV491-C (O)-NV492V493 ,-NHS (O ₂)-V494 ,-NV495S (O ₂)-V496 ,-S-V497 ,-S (O)-V498 ,-S (O ₂)-V499 ,-S (O ₂) NH-V500 ,-S (O ₂) NV501V502 ,-S (O ₂) O-V503 ,-P (O) is (OV505) (OV504), and-Si (V506) is (V508) (V507) ";

V457 wherein, V458, V459, V460, V461, V462, V463, V464, V465, V466, V467, V468, V469, V470; V471, V472, V473, V474, V475, V476, V477, V478, V479, V480, V481, V482, V483; V484, V485, V486, V487, V488, V489, V490, V491, V492, V493, V494, V495, V496; V497, V498, V499, V500, V501, V502, V503, V504, V505, V506, V507, V508 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, V463, V464 and/or V472; V473 and/or V485, V486 and/or V492, V493 and/or V501, V502 also can form " heterocyclic radical " in each case together;

(ii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHV509 ,-NV510V511 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-V512 ,-C (O) O-V513 ,-C (O) NH-V514 ,-C (O) NV515V516 ,-O-V517 ,-O are (V518-O) _z-H (z=1,2,3,4,5) ,-O (V519-O) _z-V520 (z=1,2,3,4,5) ,-OC (O)-V521 ,-OC (O)-O-V522 ,-OC (O)-NHV523 ,-O-C (O)-NV524V525 ,-OP (O) is (OV527) (OV526), and-OSi (V528) is (V530) (V529) ,-OS (O ₂)-V531 ,-NHC (O)-V532 ,-NV533C (O)-V534 ,-NH-C (O)-O-V535 ,-NH-C (O)-NH-V536 ,-NH-C (O)-NV537V538 ,-NV539-C (O)-O-V 540 ,-NV541-C (O)-NH-V542 ,-NV543-C (O)-NV544V545 ,-NHS (O ₂)-V546 ,-NV547S (O ₂)-V548 ,-S-V549 ,-S (O)-V550 ,-S (O ₂)-V551 ,-S (O ₂) NH-V552 ,-S (O ₂) NV553V554 ,-S (O ₂) O-V555 ,-P (O) is (OV557) (OV556), and-Si (V558) is (V560) (V559) ";

V509 wherein, V510, V511, V512, V513, V514, V515, V516, V517, V518, V519, V520, V521, V522; V523, V524, V525, V526, V527, V528, V529, V530, V531, V532, V533, V534, V535; V536, V537, V538, V539, V540, V541, V542, V543, V544, V545, V546, V547, V548; V549, V550, V551, V552, V553, V554, V555, V556, V557, V558, V559, V560 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, V515, V516 and/or V524; V525 and/or V537, V538 and/or V544, V545 and/or V553, V554 also can form " heterocyclic radical " in each case together;

(iii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF3, N ₃, NH ₂,-NHV561 ,-NV562V563 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-V564 ,-C (O) O-V565 ,-C (O) NH-V566 ,-C (O) NV567V568 ,-O-V569 ,-O are (V570-O) _a-H (a=1,2,3,4,5) ,-O (V571-O) _a-V572 (a=1,2,3,4,5) ,-OC (O)-V573 ,-OC (O)-O-V574 ,-OC (O)-NHV575 ,-O-C (O)-NV576V577 ,-OP (O) is (OV579) (OV578), and-OSi (V580) is (V582) (V581) ,-OS (O ₂)-V583 ,-NHC (O)-V584 ,-NV585C (O)-V586 ,-NH-C (O)-O-V587 ,-NH-C (O)-NH-V588 ,-NH-C (O)-NV589V590 ,-NV591-C (O)-O-V592 ,-NV593-C (O)-NH-V594 ,-NV595-C (O)-NV596V597 ,-NHS (O ₂)-V598 ,-NV599S (O ₂)-V600 ,-S-V601 ,-S (O)-V602 ,-S (O ₂)-V603 ,-S (O ₂) NH-V604 ,-S (O ₂) NV605V606 ,-S (O ₂) O-V607 ,-P (O) is (OV609) (OV608), and-Si (V610) is (V612) (V611) ";

V561 wherein, V562, V563, V564, V565, V566, V567, V568, V569, V570, V571, V572, V573, V574; V575, V576, V577, V578, V579, V580, V581, V582, V583, V584, V585, V586, V587; V588, V589, V590, V591, V592, V593, V594, V595, V596, V597, V598, V599, V600; V601, V602, V603, V604, V605, V606, V607, V608, V609, V610, V611, V612 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, V567, V568 and/or V576; V577 and/or V589, V590 and/or V596, V597 and/or V605, V606 also can form " heterocyclic radical " in each case together;

(i) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHV613 ,-NV614V615 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-V616 ,-C (O) O-V617 ,-C (O) NH-V618 ,-C (O) NV619V620 ,-O-V621 ,-O are (V622-O) _b-H (b=1,2,3,4,5) ,-O (V623-O) _b-V624 (b=1,2,3,4,5) ,-OC (O)-V625 ,-OC (O)-O-V626 ,-OC (O)-NHV627 ,-O-C (O)-NV628V629 ,-OP (O) is (OV631) (OV630), and-OSi (V632) is (V634) (V633) ,-OS (O ₂)-V635 ,-NHC (O)-V636 ,-NV637C (O)-V638 ,-NH-C (O)-O-V639 ,-NH-C (O)-NH-V640 ,-NH-C (O)-NV641V642 ,-NV643-C (O)-O-V644 ,-NV645-C (O)-NH-V646 ,-NV647-C (O)-NV648V649 ,-NHS (O ₂)-V650 ,-NV651S (O ₂)-V652 ,-S-V653 ,-S (O)-V654 ,-S (O ₂)-V655 ,-S (O ₂) NH-V656 ,-S (O ₂) NV657V658 ,-S (O ₂) O-V659 ,-P (O) is (OV661) (OV660), and-Si (V662) is (V664) (V663) ";

V613 wherein, V614, V615, V616, V617, V618, V619, V620, V621, V622, V623, V624, V625, V626; V627, V628, V629, V630, V631, V632, V633, V634, V635, V636, V637, V638, V639; V640, V641, V642, V643, V644, V645, V646, V647, V648, V649, V650, V651, V652; V653, V654, V655, V656, V657, V658, V659, V660, V661, V662, V663, V664 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, V619, V620 and/or V628; V629 and/or V641, V642 and/or V648, V649 and/or V657, V658 also can form " heterocyclic radical " in each case together;

(ii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHV665 ,-NV666V667 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-V668 ,-C (O) O-V669 ,-C (O) NH-V670 ,-C (O) NV671V672 ,-O-V673 ,-O are (V674-O) _c-H (c=1,2,3,4,5) ,-O (V675-O) _c-V676 (c=1,2,3,4,5) ,-OC (O)-V677 ,-OC (O)-O-V678 ,-OC (O)-NHV679 ,-O-C (O)-NV680V681 ,-OP (O) is (OV683) (OV682), and-OSi (V684) is (V686) (V685) ,-OS (O ₂)-V687 ,-NHC (O)-V688 ,-NV689C (O)-V690 ,-NH-C (O)-O-V691 ,-NH-C (O)-NH-V692 ,-NH-C (O)-NV693V694 ,-NV695-C (O)-O-V696 ,-NV697-C (O)-NH-V698 ,-NV699-C (O)-NV700V701 ,-NHS (O ₂)-V702 ,-NV703S (O ₂)-V704 ,-S-V705 ,-S (O)-V706 ,-S (O ₂)-V707 ,-S (O ₂) NH-V708 ,-S (O ₂) NV709V710 ,-S (O ₂) O-V711 ,-P (O) is (OV713) (OV712), and-Si (V714) is (V716) (V715) ";

V665 wherein, V666, V667, V668, V669, V670, V671, V672, V673, V674, V675, V676, V677, V678; V679, V680, V681, V682, V683, V684, V685, V686, V687, V688, V689, V690, V691; V692, V693, V694, V695, V696, V697, V698, V699, V700, V701, V702, V703, V704; V705, V706, V707, V708, V709, V710, V711, V712, V713, V714, V715, V716 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, V671, V672 and/or V680; V681 and/or V693, V694 and/or V700, V701 and/or V709, V710 also can form " heterocyclic radical " in each case together;

(iii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHV717 ,-NV718V719 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-V720 ,-C (O) O-V721 ,-C (O) NH-V722 ,-C (O) NV723V724 ,-O-V725 ,-O are (V726-O) _d-H (d=1,2,3,4,5) ,-O (V727-O) _d-V728 (d=1,2,3,4,5) ,-OC (O)-V729 ,-OC (O)-O-V730 ,-OC (O)-NHV731 ,-O-C (O)-NV732V733 ,-OP (O) is (OV735) (OV734), and-OSi (V736) is (V738) (V737) ,-OS (O ₂)-V739 ,-NHC (O)-V740 ,-NV741C (O)-V742 ,-NH-C (O)-O-V743 ,-NH-C (O)-NH-V744 ,-NH-C (O)-NV745V746 ,-NV747-C (O)-O-V748 ,-NV749-C (O)-NH-V750 ,-NV751-C (O)-NV752V753 ,-NHS (O ₂)-V754 ,-NV755S (O ₂)-V756 ,-S-V757 ,-S (O)-V758 ,-S (O ₂)-V759 ,-S (O ₂) NH-V76O ,-S (O ₂) NV761V762 ,-S (O ₂) O-V763 ,-P (O) is (OV765) (OV764), and-Si (V766) is (V768) (V767) ";

V717 wherein, V718, V719, V720, V721, V722, V723, V724, V725, V726, V727, V728, V729, V730; V731, V732, V733, V734, V735, V736, V737, V738, V739, V740, V741, V742, V743; V744, V745, V746, V747, V748, V749, V750, V751, V752, V753, V754, V755, V756; V757, V758, V759, V760, V761, V762, V763, V764, V765, V766, V767, V768 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, V723, V724 and/or V732; V733 and/or V745, V746 and/or V752, V753 and/or V761, V762 also can form " heterocyclic radical " in each case together;

(i) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHV769 ,-NV770V771 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-V772 ,-C (O) O-V773 ,-C (O) NH-V774 ,-C (O) NV775V776 ,-O-V777 ,-O are (V778-O) _e-H (e=1,2,3,4,5) ,-O (V779-O) _e-V780 (e=1,2,3,4,5) ,-OC (O)-V781 ,-OC (O)-O-V782 ,-OC (O)-NHV783 ,-O-C (O)-NV784V785 ,-OP (O) is (OV787) (OV786), and-OSi (V788) is (V790) (V789) ,-OS (O ₂)-V791 ,-NHC (O)-V792 ,-NV793C (O)-V794 ,-NH-C (O)-O-V795 ,-NH-C (O)-NH-V796 ,-NH-C (O)-NV797V798 ,-NV799-C (O)-O-V800 ,-NV801-C (O)-NH-V802 ,-NV803-C (O)-NV804V805 ,-NHS (O ₂)-V806 ,-NV807S (O ₂)-V808 ,-S-V809 ,-S (O)-V810 ,-S (O ₂)-V811 ,-S (O ₂) NH-V812 ,-S (O ₂) NV813V814 ,-S (O ₂) O-V815 ,-P (O) is (OV817) (OV816), and-Si (V818) is (V820) (V819) ";

V769 wherein, V770, V771, V772, V773, V774, V775, V776, V777, V778, V779, V780, V781, V782; V783, V784, V785, V786, V787, V788, V789, V790, V791, V792, V793, V794, V795; V796, V797, V798, V799, V800, V801, V802, V803, V804, V805, V806, V807, V808; V809, V810, V811, V812, V813, V814, V815, V816, V817, V818, V819, V820 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, V775, V776 and/or V784; V785 and/or V797, V798 and/or V804, V805 and/or V813, V814 also can form " heterocyclic radical " in each case together;

(ii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHV821 ,-NV822V823 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-V824 ,-C (O) O-V825 ,-C (O) NH-V826 ,-C (O) NV827V828 ,-O-V829 ,-O are (V830-O) _f-H (f=1,2,3,4,5) ,-O (V831-O) _f-V832 (f=1,2,3,4,5) ,-OC (O)-V833 ,-OC (O)-O-V834 ,-OC (O)-NHV835 ,-O-C (O)-NV836V837 ,-OP (O) is (OV839) (OV838), and-OSi (V840) is (V842) (V841) ,-OS (O ₂)-V843 ,-NHC (O)-V844 ,-NV845C (O)-V846 ,-NH-C (O)-O-V847 ,-NH-C (O)-NH-V848 ,-NH-C (O)-NV849V850 ,-NV851-C (O)-O-V852 ,-NV853-C (O)-NH-V854 ,-NV855-C (O)-NV856V857 ,-NHS (O ₂)-V858 ,-NV859S (O ₂)-V860 ,-S-V861 ,-S (O)-V862 ,-S (O ₂)-V863 ,-S (O ₂) NH-V864 ,-S (O ₂) NV865V866 ,-S (O ₂) O-V867 ,-P (O) is (OV869) (OV868), and-Si (V870) is (V872) (V871) ";

V821 wherein, V822, V823, V824, V825, V826, V827, V828, V829, V830, V831, V832, V833, V834; V835, V836, V837, V838, V839, V840, V841, V842, V843, V844, V845, V846, V847; V848, V849, V850, V851, V852, V853, V854, V855, V856, V857, V858, V859, V860; V861, V862, V863, V864, V865, V866, V867, V868, V869, V870, V871, V872 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, V827, V828 and/or V836; V837 and/or V849, V850 and/or V856, V857 and/or V865, V866 also can form " heterocyclic radical " in each case together;

(iii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHV873 ,-NV874V875 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-V876 ,-C (O) O-V877 ,-C (O) NH-V878 ,-C (O) NV879V880 ,-O-V881 ,-O are (V882-O) _g-H (g=1,2,3,4,5) ,-O (V883-O) _g-V884 (g=1,2,3,4,5) ,-OC (O)-V885 ,-OC (O)-O-V886 ,-OC (O)-NHV887 ,-O-C (O)-NV888V889 ,-OP (O) is (OV891) (OV890), and-OSi (V892) is (V894) (V893) ,-OS (O ₂)-V895 ,-NHC (O)-V896 ,-NV897C (O)-V898 ,-NH-C (O)-O-V899 ,-NH-C (O)-NH-V900 ,-NH-C (O)-NV901V902 ,-NV903-C (O)-O-V904 ,-NV905-C (O)-NH-V906 ,-NV907-C (O)-NV908V909 ,-NHS (O ₂)-V910 ,-NV911S (O ₂)-V912 ,-S-V913 ,-S (O)-V914 ,-S (O ₂)-V915 ,-S (O ₂) NH-V916 ,-S (O ₂) NV917V918 ,-S (O ₂) O-V919 ,-P (O) is (OV921) (OV920), and-Si (V922) is (V924) (V923) ";

V873 wherein, V874, V875, V876, V877, V878, V879, V880, V881, V882, V883, V884, V885, V886; V887, V888, V889, V890, V891, V892, V893, V894, V895, V896, V897, V898, V899; V900, V901, V902, V903, V904, V905, V906, V907, V908, V909, V910, V911, V912; V913, V914, V915, V916, V917, V918, V919, V920, V921, V922, V923, V924 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, V879, V880 and/or V888; V889 and/or V901, V902 and/or V908, V909 and/or V917, V918 also can form " heterocyclic radical " in each case together;

(k) OZ6, wherein Z6 is independently selected from:

(ii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHV925 ,-NV926V927 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-V928 ,-C (O) O-V929 ,-C (O) NH-V930 ,-C (O) NV931V932 ,-O-V933 ,-O are (V934-O) _h-H (h=1,2,3,4,5) ,-O (V935-O) _h-V936 (h=1,2,3,4,5) ,-OC (O)-V937 ,-OC (O)-O-V938 ,-OC (O)-NHV939 ,-O-C (O)-NV940V941 ,-OP (O) is (OV943) (OV942), and-OSi (V944) is (V946) (V945) ,-OS (O ₂)-V947 ,-NHC (O)-V948 ,-NV949C (O)-V950 ,-NH-C (O)-O-V951 ,-NH-C (O)-NH-V952 ,-NH-C (O)-NV953V954 ,-NV955-C (O)-O-V956 ,-NV957-C (O)-NH-V958 ,-NV959-C (O)-NV960V961 ,-NHS (O ₂)-V962 ,-NV963S (O ₂)-V964 ,-S-V965 ,-S (O)-V966 ,-S (O ₂)-V967 ,-S (O ₂) NH-V968 ,-S (O ₂) NV969V970 ,-S (O ₂) O-V971 ,-P (O) is (OV973) (OV972), and-Si (V974) is (V976) (V975) ";

V925 wherein, V926, V927, V928, V929, V930, V931, V932, V933, V934, V935, V936, V937, V938; V939, V940, V941, V942, V943, V944, V945, V946, V947, V948, V949, V950, V951; V952, V953, V954, V955, V956, V957, V958, V959, V960, V961, V962, V963, V964; V965, V966, V967, V968, V969, V970, V971, V972, V973, V974, V975, V976 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, V931, V932 and/or V940; V941 and/or V953, V954 and/or V960, V961 and/or V969, V970 also can form " heterocyclic radical " in each case together;

(iii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHV977 ,-NV978V979 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-V980 ,-C (O) O-V981 ,-C (O) NH-V982 ,-C (O) NV983V984 ,-O-V985 ,-O are (V986-O) _i-H (i=1,2,3,4,5) ,-O (V987-O) _i-V988 (i=1,2,3,4,5) ,-OC (O)-V989 ,-OC (O)-O-V990 ,-OC (O)-NHV991 ,-O-C (O)-NV992V993 ,-OP (O) is (OV995) (OV994), and-OSi (V996) is (V998) (V997) ,-OS (O ₂)-V999 ,-NHC (O)-V1000 ,-NV1001C (O)-V1002 ,-NH-C (O)-O-V1003;-NH-C (O)-NH-V1004 ,-NH-C (O)-NV1005V1006 ,-NV1007-C (O)-O-V1008;-NV1009-C (O)-NH-V1010 ,-NV1011-C (O)-NV1012V1013 ,-NHS (O ₂)-V1014 ,-NV1015S (O ₂)-V1016 ,-S-V1017 ,-S (O)-V1018 ,-S (O ₂)-V1019 ,-S (O ₂) NH-V1020 ,-S (O ₂) NV1021V1022 ,-S (O ₂) O-V1023 ,-P (O) is (OV1025) (OV1024), and-Si (V1026) is (V1028) (V1027) ";

V977 wherein, V978, V979, V980, V981, V982, V983, V984, V985, V986, V987; V988, V989, V990, V991, V992, V993, V994, V995, V996, V997, V998; V999, V1000, V1001, V1002, V1003, V1004, V1005, V1006, V1007, V1008, V1009; V1010, V1011, V1012, V1013, V1014, V1015, V1016, V1017, V1018, V1019; V1020, V1021, V1022, V1023, V1024, V1025, V1026, V1027, V1028 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, V983, V984 and/or V992; V993 and/or V1005, V1006 and/or V1012, V1013 and/or V1021, V1022 also can form " heterocyclic radical " in each case together;

(1) SZ7, wherein Z7 is independently selected from:

(ii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHV1029 ,-NV1030V1031 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-V1032 ,-C (O) O-V1033 ,-C (O) NH-V1034 ,-C (O) NV1035V1036 ,-O-V1037 ,-O are (V1038-O) _j-H (j=1,2,3,4,5) ,-O (V1039-O) _j-V1040 (j=1,2,3,4,5) ,-OC (O)-V1041 ,-OC (O)-O-V1042 ,-OC (O)-NHV1043 ,-O-C (O)-NV1044V1045 ,-OP (O) is (OV1047) (OV1046), and-OSi (V1048) is (V1050) (V1049) ,-OS (O ₂)-V1051 ,-NHC (O)-V1052 ,-NV1053C (O)-V1054 ,-NH-C (O)-O-V1055;-NH-C (O)-NH-V1056 ,-NH-C (O)-NV1057V1058 ,-NV1059-C (O)-O-V1060;-NV1061-C (O)-NH-V1062 ,-NV1063-C (O)-NV1064V1065 ,-NHS (O ₂)-V1066 ,-NV1067S (O ₂)-V1068 ,-S-V1069 ,-S (O)-V1070 ,-S (O ₂)-V1071 ,-S (O ₂) NH-V1072 ,-S (O ₂) NV1073V1074 ,-S (O ₂) O-V1075 ,-P (O) is (OV1077) (OV1076), and-Si (V1078) is (V1080) (V1079) ";

V1029 wherein, V1030, V1031, V1032, V1033, V1034, V1035, V1036, V1037, V1038, V1039; V1040, V1041, V1042, V1043, V1044, V1045, V1046, V1047, V1048, V1049, V1050; V1051, V1052, V1053, V1054, V1055, V1056, V1057, V1058, V1059, V1060, V1061; V1062, V1063, V1064, V1065, V1066, V1067, V1068, V1069, V1070, V1071; V1072, V1073, V1074, V1075, V1076, V1077, V1078, V1079, V1080 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, V1035, V1036 and/or V1044; V1045 and/or V1057, V1058 and/or V1064, V1065 and/or V1073, V1074 also can form " heterocyclic radical " in each case together;

(iii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHV1081 ,-NV1082V1083 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-V1084 ,-C (O) O-V1085 ,-C (O) NH-V1086 ,-C (O) NV1087V1088 ,-O-V1089 ,-O are (V1090-O) _k-H (k=1,2,3,4,5) ,-O (V1091-O) _k-V1092 (k=1,2,3,4,5) ,-OC (O)-V1093 ,-OC (O)-O-V1094 ,-OC (O)-NHV1095 ,-O-C (O)-NV1096V1097 ,-OP (O) is (OV1099) (OV1098), and-OSi (V1100) is (V1102) (V1101) ,-OS (O ₂)-V1103 ,-NHC (O)-V11O4 ,-NV1105C (O)-V1106 ,-NH-C (O)-O-V1107;-NH-C (O)-NH-V1108 ,-NH-C (O)-NV1109V1110 ,-NV1111-C (O)-O-V1112;-NV1113-C (O)-NH-V1114 ,-NV1115-C (O)-NV1116V1117 ,-NHS (O ₂)-V1118 ,-NV1119S (O ₂)-V1120 ,-S-V1121 ,-S (O)-V1122 ,-S (O ₂)-V1123 ,-S (O ₂) NH-V1124 ,-S (O ₂) NV1125V1126 ,-S (O ₂) O-V1127 ,-P (O) is (OV1129) (OV1128), and-Si (V1130) is (V1132) (V1131) ";

V1081 wherein, V1082, V1083, V1084, V1085, V1086, V1087, V1088, V1089, V1090, V1091; V1092, V1093, V1094, V1095, V1096, V1097, V1098, V1099, V1100, V1101, V1102; V1103, V1104, V1105, V1106, V1107, V1108, V1109, V1110, V1111, V1112, V1113; V1114, V1115, V1116, V1117, V1118, V1119, V1120, V1121, V1122, V1123; V1124, V1125, V1126, V1127, V1128, V1129, V1130, V1131, V1132 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, V1087, V1088 and/or V1096; V1097 and/or V1109, V1110 and/or V1116, V1117 and/or V1125, V1126 also can form " heterocyclic radical " in each case together;

(m) NZ8Z9, Z8 wherein, Z9 is selected from independently of one another:

(i) " hydrogen, alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl ,-C (O)-V1133 ,-C (O) O-V1134 ,-C (O)-NV1135V1136 ,-S (O ₂)-V1137 ,-S (O ₂) O-V1138 ";

V1133 wherein, V1134, V1135, V1136, V1137, V1138 is selected from independently of one another: hydrogen, alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl " and wherein, perhaps, V1135, V1136 also can form " heterocyclic radical " together;

(ii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHV1139 ,-NV1140V1141 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-V1142 ,-C (O) O-V1143 ,-C (O) NH-V1144 ,-C (O) NV1145V1146 ,-O-V1147 ,-O are (V1148-O) _l-H (1=1,2,3,4,5) ,-O (V1149-O) _l-V1150 (l=1,2,3,4,5) ,-OC (O)-V1151 ,-OC (O)-O-V1152 ,-OC (O)-NHV1153 ,-O-C (O)-NV1154V1155 ,-OP (O) is (OV1157) (OV1156), and-OSi (V1158) is (V1160) (V1159) ,-OS (O ₂)-V1161 ,-NHC (O)-V1162 ,-NV1163C (O)-V1164 ,-NH-C (O)-O-V1165;-NH-C (O)-NH-V1166 ,-NH-C (O)-NV1167V1168 ,-NV1169-C (O)-O-V1170;-NV1171-C (O)-NH-V1172 ,-NV1173-C (O)-NV1174V1175 ,-NHS (O ₂)-V1176 ,-NV1177S (O ₂)-V1178 ,-S-V1179 ,-S (O)-V1180 ,-S (O ₂)-V1181 ,-S (O ₂) NH-V1182 ,-S (O ₂) NV1183V1184 ,-S (O ₂) O-V1185 ,-P (O) is (OV1187) (OV1186), and-Si (V1188) is (V1190) (V1189) ";

V1139 wherein, V1140, V1141, V1142, V1143, V1144, V1145, V1146, V1147, V1148, V1149; V1150, V1151, V1152, V1153, V1154, V1155, V1156, V1157, V1158, V1159, V1160; V1161, V1162, V1163, V1164, V1165, V1166, V1167, V1168, V1169, V1170, V1171; V1172, V1173, V1174, V1175, V1176, V1177, V1178, V1179, V1180, V1181; V1182, V1183, V1184, V1185, V1186, V1187, V1188, V1189, V1190 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, V1145, V1146 and/or V1154; V1155 and/or V1167, V1168 and/or V1174, V1175 and/or V1183, V1184 also can form " heterocyclic radical " in each case together;

(iii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHV1191 ,-NV1192V1193 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-V1194 ,-C (O) O-V1195 ,-C (O) NH-V1196 ,-C (O) NV1197V1198 ,-O-V1199 ,-O are (V1200-O) _m-H (m=1,2,3,4,5) ,-O (V1201-O) _m-V1202 (m=1,2,3,4,5) ,-OC (O)-V1203 ,-OC (O)-O-V1204 ,-OC (O)-NHV1205 ,-O-C (O)-NV1206V1207 ,-OP (O) is (OV1209) (OV1208), and-OSi (V1210) is (V1212) (V1211) ,-OS (O ₂)-V1213 ,-NHC (O)-V1214 ,-NV1215C (O)-V1216 ,-NH-C (O)-O-V1217;-NH-C (O)-NH-V1218 ,-NH-C (O)-NV1219V1220 ,-NV1221-C (O)-O-V1222;-NV1223-C (O)-NH-V1224 ,-NV1225-C (O)-NV1226V1227 ,-NHS (O ₂)-V1228 ,-NV1229S (O ₂)-V1230 ,-S-V1231 ,-S (O)-V1232 ,-S (O ₂)-V1233 ,-S (O ₂) NH-V1234 ,-S (O ₂) NV1235V1236 ,-S (O ₂) O-V1237 ,-P (O) is (OV1239) (OV1238), and-Si (V1240) is (V1242) (V1241) ";

V1191 wherein, V1192, V1193, V1194, V1195, V1196, V1197, V1198, V1199, V1200, V1201; V1202, V1203, V1204, V12O5, V1206, V1207, V1208, V1209, V1210, V1211, V1212; V1213, V1214, V1215, V1216, V1217, V1218, V1219, V1220, V1221, V1222, V1223; V1224, V1225, V1226, V1227, V1228, V1229, V1230, V1231, V1232, V1233; V1234, V1235, V1236, V1237, V1238, V1239, V1240, V1241, V1242 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, V1197, V1198 and/or V1206; V1207 and/or V1219, V1220 and/or V1226, V1227 and/or V1235, V1236 also can form " heterocyclic radical " in each case together;

Or

(C) one of Z3, Z4 group or Z3, Z4 group the two be " substituted alkyl " independently, wherein " substituted alkyl " is selected from following substituting group by at least one and replaces:

(a) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHW1 ,-NW2W3 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-W4 ,-C (O) O-W5 ,-C (O) NH-W6 ,-C (O) NW7W8 ,-O-W9 ,-O are (W10-O) _r-H (r=1,2,3,4,5) ,-O (W11-O) _r-W12 (r=1,2,3,4,5) ,-OC (O)-W13 ,-OC (O)-O-W14 ,-OC (O)-NHW15 ,-O-C (O)-NW16W17 ,-OP (O) is (OW19) (OW18), and-OSi (W20) is (W22) (W21) ,-OS (O ₂)-W23 ,-NHC (O)-W24 ,-NW25C (O)-W26 ,-NH-C (O)-O-W27 ,-NH-C (O)-NH-W28 ,-NH-C (O)-NW29W30 ,-NW31-C (O)-O-W32 ,-NW33-C (O)-NH-W34 ,-NW35-C (O)-NW36W37 ,-NHS (O ₂)-W38 ,-NW39S (O ₂)-W40 ,-S-W41 ,-S (O)-W42 ,-S (O ₂)-W43 ,-S (O ₂) NH-W44 ,-S (O ₂) NW45W46 ,-S (O ₂) O-W47 ,-P (O) is (OW49) (OW48), and-Si (W50) is (W52) (W51) ";

W1 wherein, W2, W3, W4, W5, W6, W7, W8, W9, W10, W11, W12, W13, W14; W15, W16, W17, W18, W19, W20, W21, W22, W23, W24, W25, W26, W27; W28, W29, W30, W31, W32, W33, W34, W35, W36, W37, W38, W39, W40; W41, W42, W43, W44, W45, W46, W47, W48, W49, W50, W51, W52 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl; Arylalkyl, heteroaryl, heteroarylalkyl " and wherein, perhaps, W7; W8 and/or W16, W17 and/or W29, W30 and/or W36, W37 and/or W45, W46 also can form " heterocyclic radical " in each case together;

Condition is, " C (O) NH-aryl ", and " C (O) NH-heteroaryl ", " C (O) NH-naphthenic base ", " C (O) NH-heterocyclic radical " further replaced by at least one substituting group that is selected from following substituting group group (i);

Wherein randomly, the above-mentioned substituting group of substituting group group (a) can and then be selected from following substituting group replacement by at least one independently of one another identically or differently:

(i) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHW53 ,-NW54W55 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-W56 ,-C (O) O-W57 ,-C (O) NH-W58 ,-C (O) NW59W60 ,-O-W61 ,-O are (W62-O) _s-H (s=1,2,3,4,5) ,-O (W63-O) _t-W64 (t=1,2,3,4,5) ,-OC (O)-W65 ,-OC (O)-O-W66 ,-OC (O)-NHW67 ,-O-C (O)-NW68W69 ,-OP (O) is (OW71) (OW70), and-OSi (W72) is (W74) (W73) ,-OS (O ₂)-W75 ,-NHC (O)-W76 ,-NW77C (O)-W78 ,-NH-C (O)-O-W79 ,-NH-C (O)-NH-W80 ,-NH-C (O)-NW81W82 ,-NW83-C (O)-O-W84 ,-NW85-C (O)-NH-W86 ,-NW87-C (O)-NW88W89 ,-NHS (O ₂)-W90 ,-NW91S (O ₂)-W92 ,-S-W93 ,-S (O)-W94 ,-S (O ₂)-W95 ,-S (O ₂) NH-W96 ,-S (O ₂) NW97W98 ,-S (O ₂) O-W99 ,-P (O) is (OW101) (OW100), and-Si (W102) is (W104) (W103) ";

W53 wherein, W54, W55, W56, W57, W58, W59, W60, W61, W62, W63, W64, W65, W66; W67, W68, W69, W70, W71, W72, W73, W74, W75, W76, W77, W78, W79; W80, W81, W82, W83, W84, W85, W86, W87, W88, W89, W90, W91, W92; W93, W94, W95, W96, W97, W98, W99, W100, W101, W102, W103, W104 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, W59, W60 and/or W68; W69 and/or W81, W82 and/or W88, W89 and/or W97, W98 also can form " heterocyclic radical " in each case together;

(ii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHW105 ,-NW106W107 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-W108 ,-C (O) O-W109 ,-C (O) NH-W110 ,-C (O) NW111W112 ,-O-W113 ,-O are (W114-O) _t-H (t=1,2,3,4,5) ,-O (W115-O) _t-W116 (t=1,2,3,4,5) ,-OC (O)-W117 ,-OC (O)-O-W118 ,-OC (O)-NHW119 ,-O-C (O)-NW120W121 ,-OP (O) is (OW123) (OW122), and-OSi (W124) is (W126) (W125) ,-OS (O ₂)-W127 ,-NHC (O)-W128 ,-NW129C (O)-W130 ,-NH-C (O)-O-W131 ,-NH-C (O)-NH-W132 ,-NH-C (O)-NW133W134 ,-NW135-C (O)-O-W136 ,-NW137-C (O)-NH-W138 ,-NW139-C (O)-NW140W141 ,-NHS (O ₂)-W142 ,-NW143S (O ₂)-W144 ,-S-W145 ,-S (O)-W146 ,-S (O ₂)-W147 ,-S (O ₂) NH-W148 ,-S (O ₂) NW149W150 ,-S (O ₂) O-W151 ,-P (O) is (OW153) (OW152), and-Si (W154) is (W156) (W155) ";

W105 wherein, W106, W107, W108, W109, W110, W111, W112, W113, W114, W115, W116, W117, W118; W119, W120, W121, W122, W123, W124, W125, W126, W127, W128, W129, W130, W131; W132, W133, W134, W135, W136, W137, W138, W139, W140, W141, W142, W143, W144; W145, W146, W147, W148, W149, W150, W151, W152, W153, W154, W155, W156 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, W111, W112 and/or W120; W121 and/or W133, W134 and/or W140, W141 and/or W149, W150 also can form " heterocyclic radical " in each case together;

OrThe two is " (C independently for one of Z3, Z4 group or Z3, Z4 group ₉-C ₃₀) alkyl ";

" (C wherein ₉-C ₃₀) alkyl " can be independently, randomly by at least one identical ground or different are selected from following substituting group and replace:

(i) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHW157 ,-NW158W159 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-W160 ,-C (O) O-W161 ,-C (O) NH-W162 ,-C (O) NW163W164 ,-O-W165 ,-O are (W166-O) _u-H (u=1,2,3,4,5) ,-O (W167-O) _u-W168 (u=1,2,3,4,5) ,-OC (O)-W169 ,-OC (O)-O-W170 ,-OC (O)-NHW171 ,-O-C (O)-NW172W173 ,-OP (O) is (OW175) (OW174), and-OSi (W176) is (W178) (W177) ,-OS (O ₂)-W179 ,-NHC (O)-W180 ,-NW181C (O)-W182 ,-NH-C (O)-O-W183 ,-NH-C (O)-NH-W184 ,-NH-C (O)-NW185W186 ,-NW187-C (O)-O-W188 ,-NW189-C (O)-NH-W190 ,-NW191-C (O)-NW192W193 ,-NHS (O ₂)-W194 ,-NW195S (O ₂)-W196 ,-S-W197 ,-S (O)-W198 ,-S (O ₂)-W199 ,-S (O ₂) NH-W200 ,-S (O ₂) NW201W202 ,-S (O ₂) O-W203 ,-P (O) is (OW205) (OW204), and-Si (W206) is (W208) (W207) ";

W157 wherein, W158, W159, W160, W161, W162, W163, W164, W165, W166, W167, W168, W169, W170; W171, W172, W173, W174, W175, W176, W177, W178, W179, W180, W181, W182, W183; W184, W185, W186, W187, W188, W189, W190, W191, W192, W193, W194, W195, W196; W197, W198, W199, W200, W201, W202, W203, W204, W205, W206, W207, W208 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, W163, W164 and/or W172; W173 and/or W185, W186 and/or W192, W193 and/or W201, W202 also can form " heterocyclic radical " in each case together;

(ii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHW209 ,-NW210W211 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-W212 ,-C (O) O-W213 ,-C (O) NH-W214 ,-C (O) NW215W216 ,-O-W217 ,-O are (W218-O) _v-H (v=1,2,3,4,5) ,-O (W219-O) _v-W220 (v=1,2,3,4,5) ,-OC (O)-W221 ,-OC (O)-O-W222 ,-OC (O)-NHW223 ,-O-C (O)-NW224W225 ,-OP (O) is (OW227) (OW226), and-OSi (W228) is (W230) (W229) ,-OS (O ₂)-W231 ,-NHC (O)-W232 ,-NW233C (O)-W234 ,-NH-C (O)-O-W235 ,-NH-C (O)-NH-W236 ,-NH-C (O)-NW237W238 ,-NW239-C (O)-O-W240 ,-NW241-C (O)-NH-W242 ,-NW243-C (O)-NW244W245 ,-NHS (O ₂)-W246 ,-NW247S (O ₂)-W248 ,-S-W249 ,-S (O)-W250 ,-S (O ₂)-W251 ,-S (O ₂) NH-W252 ,-S (O ₂) NW253W254 ,-S (O ₂) O-W255 ,-P (O) is (OW257) (OW256), and-Si (W258) is (W260) (W259) ";

W209 wherein, W210, W211, W212, W213, W214, W215, W216, W217, W218, W219, W220, W221, W222; W223, W224, W225, W226, W227, W228, W229, W230, W231, W232, W233, W234, W235; W236, W237, W238, W239, W240, W241, W242, W243, W244, W245, W246, W247, W248; W249, W250, W251, W252, W253, W254, W255, W256, W257, W258, W259, W260 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, W215, W216 and/or W224; W225 and/or W237, W238 and/or W244, W245 and/or W253, W254 also can form " heterocyclic radical " in each case together;

AndOne of Z3, Z4 group or Z3, Z4 group none are independently selected from:

(b) hydrogen;

(c) halogen, F, Cl, Br, I;

(d) unsubstituted or substituted alkyl or (C ₉-C ₃₀) alkyl, wherein randomly, said alkyl or (C ₉-C ₃₀) alkyl can or different are selected from following substituting group and replace by at least one identical ground:

(i) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHW457 ,-NW458W459 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-W460 ,-C (O) O-W461 ,-C (O) NH-W462 ,-C (O) NW463W464 ,-O-W465 ,-O are (W466-O) _x-H (x=1,2,3,4,5) ,-O (W467-O) _x-W468 (x=1,2,3,4,5) ,-OC (O)-W469 ,-OC (O)-O-W470 ,-OC (O)-NHW471 ,-O-C (O)-NW472W473 ,-OP (O) is (OW475) (OW474), and-OSi (W476) is (W478) (W477) ,-OS (O ₂)-W479 ,-NHC (O)-W480 ,-NW481C (O)-W482 ,-NH-C (O)-O-W483 ,-NH-C (O)-NH-W484 ,-NH-C (O)-NW485W486 ,-NW487-C (O)-O-W488 ,-NW489-C (O)-NH-W490 ,-NW491-C (O)-NW492W493 ,-NHS (O ₂)-W494 ,-NW495S (O ₂)-W496 ,-S-W497 ,-S (O)-W498 ,-S (O ₂)-W499 ,-S (O ₂) NH-W500 ,-S (O ₂) NW501W502 ,-S (O ₂) O-W503 ,-P (O) is (OW505) (OW504), and-Si (W506) is (W508) (W507) ";

W457 wherein, W458, W459, W460, W461, W462, W463, W464, W465, W466, W467, W468, W469, W470; W471, W472, W473, W474, W475, W476, W477, W478, W479, W480, W481, W482, W483; W484, W485, W486, W487, W488, W489, W490, W491, W492, W493, W494, W495, W496; W497, W498, W499, W500, W501, W502, W503, W504, W505, W506, W507, W508 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, W463, W464 and/or W472; W473 and/or W485, W486 and/or W492, W493 and/or W501, W502 also can form " heterocyclic radical " in each case together;

(ii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHW509 ,-NW510W511 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-W512 ,-C (O) O-W513 ,-C (O) NH-W514 ,-C (O) NW515W516 ,-O-W517 ,-O are (W518-O) _y-H (y=1,2,3,4,5) ,-O (W519-O) _y-W520 (y=1,2,3,4,5) ,-OC (O)-W521 ,-OC (O)-O-W522 ,-OC (O)-NHW523 ,-O-C (O)-NW524W525 ,-OP (O) is (OW527) (OW526), and-OSi (W528) is (W530) (W529) ,-OS (O ₂)-W531 ,-NHC (O)-W532 ,-NW533C (O)-W534 ,-NH-C (O)-O-W535 ,-NH-C (O)-NH-W536 ,-NH-C (O)-NW537W538 ,-NW539-C (O)-O-W540 ,-NW541-C (O)-NH-W542 ,-NW543-C (O)-NW544W545 ,-NHS (O ₂)-W546 ,-NW547S (O ₂)-W548 ,-S-W549 ,-S (O)-W550 ,-S (O ₂)-W551 ,-S (O ₂) NH-W552 ,-S (O ₂) NW553W554 ,-S (O ₂) O-W555 ,-P (O) is (OW557) (OW556), and-Si (W558) is (W560) (W559) ";

W509 wherein, W51O, W511, W512, W513, W514, W515, W516, W517, W518, W519, W520, W521, W522; W523, W524, W525, W526, W527, W528, W529, W530, W531, W532, W533, W534, W535; W536, W537, W538, W539, W540, W541, W542, W543, W544, W545, W546, W547, W548; W549, W550, W551, W552, W553, W554, W555, W556, W557, W558, W559, W560 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, W515, W516 and/or W524; W525 and/or W537, W538 and/or W544, W545 and/or W553, W554 also can form " heterocyclic radical " in each case together;

(iii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF3, N ₃, NH ₂,-NHW561 ,-NW562W563 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-W564 ,-C (O) O-W565 ,-C (O) NH-W566 ,-C (O) NW567W568 ,-O-W569 ,-O are (W570-O) _z-H (z=1,2,3,4,5) ,-O (W571-O) _z-W572 (z=1,2,3,4,5) ,-OC (O)-W573 ,-OC (O)-O-W574 ,-OC (O)-NHW575 ,-O-C (O)-NW576W577 ,-OP (O) is (OW579) (OW578), and-OSi (W580) is (W582) (W581) ,-OS (O ₂)-W583 ,-NHC (O)-W584 ,-NW585C (O)-W586 ,-NH-C (O)-O-W587 ,-NH-C (O)-NH-W588 ,-NH-C (O)-NW589W590 ,-NW591-C (O)-O-W592 ,-NW593-C (O)-NH-W594 ,-NW595-C (O)-NW596W597 ,-NHS (O ₂)-W598 ,-NW599S (O ₂)-W600 ,-S-W601 ,-S (O)-W602 ,-S (O ₂)-W603 ,-S (O ₂) NH-W604 ,-S (O ₂) NW605W606 ,-S (O ₂) O-W607 ,-P (O) is (OW609) (OW608), and-Si (W610) is (W612) (W611) ";

W561 wherein, W562, W563, W564, W565, W566, W567, W568, W569, W570, W571, W572, W573, W574; W575, W576, W577, W578, W579, W580, W581, W582, W583, W584, W585, W586, W587; W588, W589, W590, W591, W592, W593, W594, W595, W596, W597, W598, W599, W600; W601, W602, W603, W604, W605, W606, W607, W608, W609, W610, W611, W612 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, W567, W568 and/or W576; W577 and/or W589, W590 and/or W596, W597 and/or W605, W606 also can form " heterocyclic radical " in each case together;

(e) unsubstituted or substituted aryl, wherein randomly, said aryl can be selected from following substituting group by at least one identically or differently and replace:

(i) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHW613 ,-NW614W615 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-W616 ,-C (O) O-W617 ,-C (O) NH-W618 ,-C (O) NW619W620 ,-O-W621 ,-O are (W622-O) _a-H (a=1,2,3,4,5) ,-O (W623-O) _a-W624 (a=1,2,3,4,5) ,-OC (O)-W625 ,-OC (O)-O-W626 ,-OC (O)-NHW627 ,-O-C (O)-NW628W629 ,-OP (O) is (OW631) (OW630), and-OSi (W632) is (W634) (W633) ,-OS (O ₂)-W635 ,-NHC (O)-W636 ,-NW637C (O)-W638 ,-NH-C (O)-O-W639 ,-NH-C (O)-NH-W640 ,-NH-C (O)-NW641W642 ,-NW643-C (O)-O-W644 ,-NW645-C (O)-NH-W646 ,-NW647-C (O)-NW648W649 ,-NHS (O ₂)-W650 ,-NW651S (O ₂)-W652 ,-S-W653 ,-S (O)-W654 ,-S (O ₂)-W655 ,-S (O ₂) NH-W656 ,-S (O ₂) NW657W658 ,-S (O ₂) O-W659 ,-P (O) is (OW661) (OW660), and-Si (W662) is (W664) (W663) ";

W613 wherein, W614, W615, W616, W617, W618, W619, W620, W621, W622, W623, W624, W625, W626; W627, W628, W629, W630, W631, W632, W633, W634, W635, W636, W637, W638, W639; W640, W641, W642, W643, W644, W645, W646, W647, W648, W649, W650, W651, W652; W653, W654, W655, W656, W657, W658, W659, W660, W661, W662, W663, W664 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, W619, W620 and/or W628; W629 and/or W641, W642 and/or W648, W649 and/or W657, W658 also can form " heterocyclic radical " in each case together;

(ii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHW665 ,-NW666W667 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-W668 ,-C (O) O-W669 ,-C (O) NH-W670 ,-C (O) NW671W672 ,-O-W673 ,-O are (W674-O) _b-H (b=1,2,3,4,5) ,-O (W675-O) _b-W676 (b=1,2,3,4,5) ,-OC (O)-W677 ,-OC (O)-O-W678 ,-OC (O)-NHW679 ,-O-C (O)-NW680W681 ,-OP (O) is (OW683) (OW682), and-OSi (W684) is (W686) (W685) ,-OS (O ₂)-W687 ,-NHC (O)-W688 ,-NW689C (O)-W690 ,-NH-C (O)-O-W691 ,-NH-C (O)-NH-W692 ,-NH-C (O)-NW693W694 ,-NW695-C (O)-O-W696 ,-NW697-C (O)-NH-W698 ,-NW699-C (O)-NW700W701 ,-NHS (O ₂)-W702 ,-NW703S (O ₂)-W704 ,-S-W705 ,-S (O)-W706 ,-S (O ₂)-W707 ,-S (O ₂) NH-W708 ,-S (O ₂) NW709W710 ,-S (O ₂) O-W711 ,-P (O) is (OW713) (OW712), and-Si (W714) is (W716) (W715) ";

W665 wherein, W666, W667, W668, W669, W670, W671, W672, W673, W674, W675, W676, W677, W678; W679, W680, W681, W682, W683, W684, W685, W686, W687, W688, W689, W690, W691; W692, W693, W694, W695, W696, W697, W698, W699, W700, W701, W702, W703, W704; W705, W706, W707, W708, W709, W710, W711, W712, W713, W714, W715, W716 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, W671, W672 and/or W680; W681 and/or W693, W694 and/or W700, W701 and/or W709, W710 also can form " heterocyclic radical " in each case together;

(iii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHW717 ,-NW718W719 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-W720 ,-C (O) O-W721 ,-C (O) NH-W722 ,-C (O) NW723W724 ,-O-W725 ,-O are (W726-O) _c-H (c=1,2,3,4,5) ,-O (W727-O) _c-W728 (c=1,2,3,4,5) ,-OC (O)-W729 ,-OC (O)-O-W730 ,-OC (O)-NHW731 ,-O-C (O)-NW732W733 ,-OP (O) is (OW735) (OW734), and-OSi (W736) is (W738) (W737) ,-OS (O ₂)-W739 ,-NHC (O)-W740 ,-NW741C (O)-W742 ,-NH-C (O)-O-W743 ,-NH-C (O)-NH-W744 ,-NH-C (O)-NW745W746 ,-NW747-C (O)-O-W748 ,-NW749-C (O)-NH-W750 ,-NW751-C (O)-NW752W753 ,-NHS (O ₂)-W754 ,-NW755S (O ₂)-W756 ,-S-W757 ,-S (O)-W758 ,-S (O ₂)-W759 ,-S (O ₂) NH-W760 ,-S (O ₂) NW761W762 ,-S (O ₂) O-W763 ,-P (O) is (OW765) (OW764), and-Si (W766) is (W768) (W767) ";

W717 wherein, W718, W719, W720, W721, W722, W723, W724, W725, W726, W727, W728, W729, W730; W731, W732, W733, W734, W735, W736, W737, W738, W739, W740, W741, W742, W743; W744, W745, W746, W747, W748, W749, W750, W751, W752, W753, W754, W755, W756; W757, W758, W759, W760, W761, W762, W763, W764, W765, W766, W767, W768 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, W723, W724 and/or W732; W733 and/or W745, W746 and/or W752, W753 and/or W761, W762 also can form " heterocyclic radical " in each case together;

(f) unsubstituted or substituted heteroaryl, wherein randomly, said heteroaryl can be selected from following substituting group by at least one identically or differently and replace:

(i) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHW769 ,-NW770W771 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-W772 ,-C (O) O-W773 ,-C (O) NH-W774 ,-C (O) NW775W776 ,-O-W777 ,-O are (W778-O) _d-H (d=1,2,3,4,5) ,-O (W779-O) _d-W780 (d=1,2,3,4,5) ,-OC (O)-W781 ,-OC (O)-O-W782 ,-OC (O)-NHW783 ,-O-C (O)-NW784W785 ,-OP (O) is (OW787) (OW786), and-OSi (W788) is (W790) (W789) ,-OS (O ₂)-W791 ,-NHC (O)-W792 ,-NW793C (O)-W794 ,-NH-C (O)-O-W795 ,-NH-C (O)-NH-W796 ,-NH-C (O)-NW797W798 ,-NW799-C (O)-O-W800 ,-NW801-C (O)-NH-W802 ,-NW803-C (O)-NW804W805 ,-NHS (O ₂)-W806 ,-NW807S (O ₂)-W808 ,-S-W809 ,-S (O)-W810 ,-S (O ₂)-W811 ,-S (O ₂) NH-W812 ,-S (O ₂) NW813W814 ,-S (O ₂) O-W815 ,-P (O) is (OW817) (OW816), and-Si (W818) is (W820) (W819) ";

W769 wherein, W770, W771, W772, W773, W774, W775, W776, W777, W778, W779, W780, W781, W782; W783, W784, W785, W786, W787, W788, W789, W790, W791, W792, W793, W794, W795; W796, W797, W798, W799, W800, W801, W802, W803, W804, W805, W806, W807, W808; W809, W810, W811, W812, W813, W814, W815, W816, W817, W818, W819, W820 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, W775, W776 and/or W784; W785 and/or W797, W798 and/or W804, W805 and/or W813, W814 also can form " heterocyclic radical " in each case together;

(ii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHW821 ,-NW822W823 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-W824 ,-C (O) O-W825 ,-C (O) NH-W826 ,-C (O) NW827W828 ,-O-W829 ,-O are (W830-O) _e-H (e=1,2,3,4,5) ,-O (W831-O) _e-W832 (e=1,2,3,4,5) ,-OC (O)-W833 ,-OC (O)-O-W834 ,-OC (O)-NHW835 ,-O-C (O)-NW836W837 ,-OP (O) is (OW839) (OW838), and-OSi (W840) is (W842) (W841) ,-OS (O ₂)-W843 ,-NHC (O)-W844 ,-NW845C (O)-W846 ,-NH-C (O)-O-W847 ,-NH-C (O)-NH-W848 ,-NH-C (O)-NW849W850 ,-NW851-C (O)-O-W852 ,-NW853-C (O)-NH-W854 ,-NW855-C (O)-NW856W857 ,-NHS (O ₂)-W858 ,-NW859S (O ₂)-W860 ,-S-W861 ,-S (O)-W862 ,-S (O ₂)-W863 ,-S (O ₂) NH-W864 ,-S (O ₂) NW865W866 ,-S (O ₂) O-W867 ,-P (O) is (OW869) (OW868), and-Si (W870) is (W872) (W871) ";

W821 wherein, W822, W823, W824, W825, W826, W827, W828, W829, W830, W831, W832, W833, W834; W835, W836, W837, W838, W839, W840, W841, W842, W843, W844, W845, W846, W847; W848, W849, W850, W851, W852, W853, W854, W855, W856, W857, W858, W859, W860; W861, W862, W863, W864, W865, W866, W867, W868, W869, W870, W871, W872 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, W827, W828 and/or W836; W837 and/or W849, W850 and/or W856, W857 and/or W865, W866 also can form " heterocyclic radical " in each case together;

(iii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHW873 ,-NW874W875 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-W876 ,-C (O) O-W877 ,-C (O) NH-W878 ,-C (O) NW879W880 ,-O-W881 ,-O are (W882-O) _f-H (f=1,2,3,4,5) ,-O (W883-O) _f-W884 (f=1,2,3,4,5) ,-OC (O)-W885 ,-OC (O)-O-W886 ,-OC (O)-NHW887 ,-O-C (O)-NW888W889 ,-OP (O) is (OW891) (OW890), and-OSi (W892) is (W894) (W893) ,-OS (O ₂)-W895 ,-NHC (O)-W896 ,-NW897C (O)-W898 ,-NH-C (O)-O-W899 ,-NH-C (O)-NH-W900 ,-NH-C (O)-NW901W902 ,-NW903-C (O)-O-W904 ,-NW905-C (O)-NH-W906 ,-NW907-C (O)-NW908W909 ,-NHS (O ₂)-W910 ,-NW911S (O ₂)-W912 ,-S-W913 ,-S (O)-W914 ,-S (O ₂)-W915 ,-S (O ₂) NH-W916 ,-S (O ₂) NW917W918 ,-S (O ₂) O-W919 ,-P (O) is (OW921) (OW920), and-Si (W922) is (W924) (W923) ";

W873 wherein, W874, W875, W876, W877, W878, W879, W880, W881, W882, W883, W884, W885, W886; W887, W888, W889, W890, W891, W892, W893, W894, W895, W896, W897, W898, W899; W900, W901, W902, W903, W904, W905, W906, W907, W908, W909, W910, W911, W912; W913, W914, W915, W916, W917, W918, W919, W920, W921, W922, W923, W924 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, W879, W880 and/or W888; W889 and/or W901, W902 and/or W908, W909 and/or W917, W918 also can form " heterocyclic radical " in each case together;

(g) OZ6, wherein Z6 is independently selected from:

(ii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHW925 ,-NW926W927 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-W928 ,-C (O) O-W929 ,-C (O) NH-W930 ,-C (O) NW931W932 ,-O-W933 ,-O are (W934-O) _g-H (g=1,2,3,4,5) ,-O (W935-O) _g-W936 (g=1,2,3,4,5) ,-OC (O)-W937 ,-OC (O)-O-W938 ,-OC (O)-NHW939 ,-O-C (O)-NW940W941 ,-OP (O) is (OW943) (OW942), and-OSi (W944) is (W946) (W945) ,-OS (O ₂)-W947 ,-NHC (O)-W948 ,-NW949C (O)-W950 ,-NH-C (O)-O-W951 ,-NH-C (O)-NH-W952 ,-NH-C (O)-NW953W954 ,-NW955-C (O)-O-W956 ,-NW957-C (O)-NH-W958 ,-NW959-C (O)-NW960W961 ,-NHS (O ₂)-W962 ,-NW963S (O ₂)-W964 ,-S-W965 ,-S (O)-W966 ,-S (O ₂)-W967 ,-S (O ₂) NH-W968 ,-S (O ₂) NW969W970 ,-S (O ₂) O-W971 ,-P (O) is (OW973) (OW972), and-Si (W974) is (W976) (W975) ";

W925 wherein, W926, W927, W928, W929, W930, W931, W932, W933, W934, W935, W936, W937, W938; W939, W940, W941, W942, W943, W944, W945, W946, W947, W948, W949, W950, W951; W952, W953, W954, W955, W956, W957, W958, W959, W960, W961, W962, W963, W964; W965, W966, W967, W968, W969, W970, W971, W972, W973, W974, W975, W976 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, W931, W932 and/or W940; W941 and/or W953, W954 and/or W960, W961 and/or W969, W970 also can form " heterocyclic radical " in each case together;

(iii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHW977 ,-NW978W979 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-W980 ,-C (O) O-W981 ,-C (O) NH-W982 ,-C (O) NW983W984 ,-O-W985 ,-O are (W986-O) _h-H (h=1,2,3,4,5) ,-O (W987-O) _h-W988 (h=1,2,3,4,5) ,-OC (O)-W989 ,-OC (O)-O-W990 ,-OC (O)-NHW991 ,-O-C (O)-NW992W993 ,-OP (O) is (OW995) (OW994), and-OSi (W996) is (W998) (W997) ,-OS (O ₂)-W999 ,-NHC (O)-W1000 ,-NW1001C (O)-W1002 ,-NH-C (O)-O-W1003;-NH-C (O)-NH-W1004 ,-NH-C (O)-NW1005W1006 ,-NW1007-C (O)-O-W1008;-NW1009-C (O)-NH-W1010 ,-NW1011-C (O)-NW1012W1013 ,-NHS (O ₂)-W1014 ,-NW1015S (O ₂)-W1016 ,-S-W1017 ,-S (O)-W1018 ,-S (O ₂)-W1019 ,-S (O ₂) NH-W1020 ,-S (O ₂) NW1021W1022 ,-S (O ₂) O-W1023 ,-P (O) is (OW1025) (OW1024), and-Si (W1026) is (W1028) (W1027) ";

W977 wherein, W978, W979, W980, W981, W982, W983, W984, W985, W986, W987; W988, W989, W990, W991, W992, W993, W994, W995, W996, W997, W998; W999, W1000, W1001, W1002, W1003, W1004, W1005, W1006, W1007, W1008, W1009; W1010, W1011, W1012, W1013, W1014, W1015, W1016, W1017, W1018, W1019; W1020, W1021, W1022, W1023, W1024, W1025, W1026, W1027, W1028 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, W983, W984 and/or W992; W993 and/or W1005, W1006 and/or W1012, W1013 and/or W1021, W1022 also can form " heterocyclic radical " in each case together;

(h) S27, wherein Z7 is independently selected from:

(ii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHW1029 ,-NW1030W1031 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-W1032 ,-C (O) O-W1033 ,-C (O) NH-W1034 ,-C (O) NW1035W1036 ,-O-W1037 ,-O are (W1038-O) _i-H (i=1,2,3,4,5) ,-O (W1039-O) _i-W1040 (i=1,2,3,4,5) ,-OC (O)-W1041 ,-OC (O)-O-W1042 ,-OC (O)-NHW1043 ,-O-C (O)-NW1044W1045 ,-OP (O) is (OW1047) (OW1046), and-OSi (W1048) is (W1050) (W1049) ,-OS (O ₂)-W1051 ,-NHC (O)-W1052 ,-NW1053C (O)-W1054 ,-NH-C (O)-O-W1055;-NH-C (O)-NH-W1056 ,-NH-C (O)-NW1057W1058 ,-NW1059-C (O)-O-W1060;-NW1061-C (O)-NH-W1062 ,-NW1063-C (O)-NW1064W1065 ,-NHS (O ₂)-W1066 ,-NW1067S (O ₂)-W1068 ,-S-W1069 ,-S (O)-W1070 ,-S (O ₂)-W1071 ,-S (O ₂) NH-W1072 ,-S (O ₂) NW1073W1074 ,-S (O ₂) O-W1075 ,-P (O) is (OW1077) (OW1076), and-Si (W1078) is (W1080) (W1079) ";

W1029 wherein, W1030, W1031, W1032, W1033, W1034, W1035, W1036, W1037, W1038, W1039; W1040, W1041, W1042, W1043, W1044, W1045, W1046, W1047, W1048, W1049, W1050; W1051, W1052, W1053, W1054, W1055, W1056, W1057, W1058, W1059, W1060, W1061; W1062, W1063, W1064, W1065, W1066, W1067, W1068, W1069, W1070, W1071; W1072, W1073, W1074, W1075, W1076, W1077, W1078, W1079, W1080 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, W1035, W1036 and/or W1044; W1045 and/or W1057, W1058 and/or W1064, W1065 and/or W1073, W1074 also can form " heterocyclic radical " in each case together;

(iii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHW1081 ,-NW1082W1083 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-W1084 ,-C (O) O-W1085 ,-C (O) NH-W1086 ,-C (O) NW1087W1088 ,-O-W1089 ,-O are (W1090-O) _j-H (j=1,2,3,4,5) ,-O (W1091-O) _j-W1092 (j=1,2,3,4,5) ,-OC (O)-W1093 ,-OC (O)-O-W1094 ,-OC (O)-NHW1095 ,-O-C (O)-NW1096W1097 ,-OP (O) is (OW1099) (OW1098), and-OSi (W1100) is (W1102) (W1101) ,-OS (O ₂)-W1103 ,-NHC (O)-W1104 ,-NW1105C (O)-W1106 ,-NH-C (O)-O-W1107;-NH-C (O)-NH-W1108 ,-NH-C (O)-NW1109W1110 ,-NW1111-C (O)-O-W1112;-NW1113-C (O)-NH-W1114 ,-NW1115-C (O)-NW1116W1117 ,-NHS (O ₂)-W1118 ,-NW1119S (O ₂)-W1120 ,-S-W1121 ,-S (O)-W1122 ,-S (O ₂)-W1123 ,-S (O ₂) NH-W1124 ,-S (O ₂) NW1125W1126 ,-S (O ₂) O-W1127 ,-P (O) is (OW1129) (OW1128), and-Si (W1130) is (W1132) (W1131) ";

W1081 wherein, W1082, W1083, W1084, W1085, W1086, W1087, W1088, W1089, W1090, W1091; W1092, W1093, W1094, W1095, W1096, W1097, W1098, W1099, W1100, W1101, W1102; W1103, W1104, W1105, W1106, W1107, W1108, W1109, W1110, W1111, W1112, W1113; W1114, W1115, W1116, W1117, W1118, W1119, W1120, W1121, W1122, W1123; W1124, W1125, W1126, W1127, W1128, W1129, W1130, W1131, W1132 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, W1087, W1088 and/or W1096; W1097 and/or W1109, W1110 and/or W1116, W1117 and/or W1125, W1126 also can form " heterocyclic radical " in each case together;

(j) NZ8Z9, Z8 wherein, Z9 is selected from independently of one another:

(i) " hydrogen, alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl ,-C (O)-W1133 ,-C (O) O-W1134 ,-C (O)-NW1135W1136 ,-S (O ₂)-W1137 ,-S (O ₂) O-W1138 ";

W1133 wherein, W1134, W1135, W1136, W1137, W1138 is selected from independently of one another: hydrogen, alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl " and wherein, perhaps, W1135, W1136 also can form " heterocyclic radical " together;

(ii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHW1139 ,-NW1140W1141 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-W1142 ,-C (O) O-W1143 ,-C (O) NH-W1144 ,-C (O) NW1145W1146 ,-O-W1147 ,-O are (W1148-O) _k-H (k=1,2,3,4,5) ,-O (W1149-O) _k-W1150 (k=1,2,3,4,5) ,-OC (O)-W1151 ,-OC (O)-O-W1152 ,-OC (O)-NHW1153 ,-O-C (O)-NW1154W1155 ,-OP (O) is (OW1157) (OW1156), and-OSi (W1158) is (W1160) (W1159) ,-OS (O ₂)-W1161 ,-NHC (O)-W1162 ,-NW1163C (O)-W1164 ,-NH-C (O)-O-W1165;-NH-C (O)-NH-W1166 ,-NH-C (O)-NW1167W1168 ,-NW1169-C (O)-O-W1170;-NW1171-C (O)-NH-W1172 ,-NW1173-C (O)-NW1174W1175 ,-NHS (O ₂)-W1176 ,-NW1177S (O ₂)-W1178 ,-S-W1179 ,-S (O)-W1180 ,-S (O ₂)-W1181 ,-S (O ₂) NH-W1182 ,-S (O ₂) NW1183W1184 ,-S (O ₂) O-W1185 ,-P (O) is (OW1187) (OW1186), and-Si (W1188) is (W1190) (W1189) ";

W1139 wherein, W1140, W1141, W1142, W1143, W1144, W1145, W1146, W1147, W1148, W1149; W1150, W1151, W1152, W1153, W1154, W1155, W1156, W1157, W1158, W1159, W1160; W1161, W1162, W1163, W1164, W1165, W1166, W1167, W1168, W1169, W1170, W1171; W1172, W1173, W1174, W1175, W1176, W1177, W1178, W1179, W1180, W1181; W1182, W1183, W1184, W1185, W1186, W1187, W1188, W1189, W1190 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, W1145, W1146 and/or W1154; W1155 and/or W1167, W1168 and/or W1174, W1175 and/or W1183, W1184 also can form " heterocyclic radical " in each case together;

(iii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHW1191 ,-NW1192W1193 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-W1194 ,-C (O) O-W1195 ,-C (O) NH-W1196 ,-C (O) NW1197W1198 ,-O-W1199 ,-O are (W1200-O) _l-H (1=1,2,3,4,5) ,-O (W1201-O) _l-W1202 (1=1,2,3,4,5) ,-OC (O)-W1203 ,-OC (O)-O-W1204 ,-OC (O)-NHW1205 ,-O-C (O)-NW1206W1207 ,-OP (O) is (OW1209) (OW1208), and-OSi (W1210) is (W1212) (W1211) ,-OS (O ₂)-W1213 ,-NHC (O)-W1214 ,-NW1215C (O)-W1216 ,-NH-C (O)-O-W1217;-NH-C (O)-NH-W1218 ,-NH-C (O)-NW1219W1220 ,-NW1221-C (O)-O-W1222;-NW1223-C (O)-NH-W1224 ,-NW1225-C (O)-NW1226W1227 ,-NHS (O ₂)-W1228 ,-NW1229S (O ₂)-W1230 ,-S-W1231 ,-S (O)-W1232 ,-S (O ₂)-W1233 ,-S (O ₂) NH-W1234 ,-S (O ₂) NW1235W1236 ,-S (O ₂) O-W1237 ,-P (O) is (OW1239) (OW1238), and-Si (W1240) is (W1242) (W1241) ";

W1191 wherein, W1192, W1193, W1194, W1195, W1196, W1197, W1198, W1199, W1200, W1201; W1202, W1203, W1204, W1205, W1206, W1207, W1208, W1209, W1210, W1211, W1212; W1213, W1214, W1215, W1216, W1217, W1218, W1219, W1220, W1221, W1222, W1223; W1224, W1225, W1226, W1227, W1228, W1229, W1230, W1231, W1232, W1233; W1234, W1235, W1236, W1237, W1238, W1239, W1240, W1241, W1242 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, W1197, W1198 and/or W1206; W1207 and/or W1219, W1220 and/or W1226, W1227 and/or W1235, W1236 also can form " heterocyclic radical " in each case together;

Or

(D) one of Z3, Z4 group or Z3, Z4 group the two be selected from independently of one another:

(1)“-NZ10Z11，-OZ12，-SZ13”；

Wherein one of Z10, Z11 group or Z10, Z11 group and Z12, Z13 group the two be selected from independently of one another:

(a) " hydrogen, alkyl, naphthenic base, cycloalkylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, heterocyclic radical, heterocyclic radical alkyl ";

Condition is, the two is not hydrogen simultaneously for Z10, Z11 group;

Other condition is that the Z12 group is not a hydrogen;

Other condition is, the above-mentioned substituting group of substituting group group (a) is when being not hydrogen, independently of one another by at least one identical ground or different are selected from following substituting group and further replace:

(i) " (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, N ₃,-NH-naphthenic base ,-NH-cycloalkylalkyl ,-NH-heteroaryl ,-NH-heteroarylalkyl ,-NH-arylalkyl ,-NH-heterocyclic radical;-NH-heterocyclic radical alkyl ,-NQ1Q2 ,-S-naphthenic base ,-S-cycloalkylalkyl ,-S-aryl ,-S-arylalkyl;-S-heteroaryl ,-S-heteroarylalkyl ,-S-heterocyclic radical ,-S-heterocyclic radical alkyl ,-O-naphthenic base ,-O-cycloalkylalkyl;-O-arylalkyl ,-O-heteroaryl ,-O-heteroarylalkyl ,-O-heterocyclic radical ,-O-heterocyclic radical alkyl ,-O (Q 3-O) _p-H (p=1,2,3,4,5) ,-O (Q4-O) _p-Q5 (p=1,2,3,4,5) ,-OP (O) is (OQ7) (OQ6) ,-C (O) O-Q8 ,-C (O) NH ₂,-C (O) NH-Q9 ,-C (O) NQ10Q11 ,-S (O ₂)-Q12 ,-P (O) (OH) ₂,-P (O) is (OQ14) (OQ13), and-Si (Q15) is (Q17) (Q16), and-O-Si (Q18) is (Q20) (Q19);-O-C (O)-O-Q21 ,-O-C (O)-NH-Q22 ,-O-C (O)-NQ23Q24 ,-NH-C (O)-O-Q25;-NH-C (O)-NH-Q26 ,-NH-C (O)-NQ27Q28 ,-NQ29-C (O)-O-Q30;-NQ31-C (O)-NH-Q32 ,-NQ33-C (O)-NQ34Q35 ,-NQ36-S (O ₂)-Q37 ,-NH-S (O ₂)-Q38 ,-O-S (O ₂)-Q39 ,-NH-C (O)-Q40 ,-NQ41-C (O)-Q42 ,-C (O)-Q43 ,-OC (O)-Q44 ,-S (O)-Q45 ,-S (O ₂)-NHQ46 ,-S (O ₂)-NQ47Q48 ,-S (O ₂)-OQ49 ";

Other condition is " N (alkyl) ₂" be selected from following substituting group group substituting group (ii) by at least one and further replace;

Q1 wherein, Q2, Q3, Q4, Q5, Q6, Q7, Q8, Q9, Q10, Q11, Q12, Q13; Q14, Q15, Q16, Q17, Q18, Q19, Q20, Q21, Q22, Q23, Q24, Q25, Q26; Q27, Q28, Q29, Q30, Q31, Q32, Q33, Q34, Q35, Q36, Q37, Q38; Q39, Q40, Q41, Q42, Q43, Q44, Q45, Q46, Q47, Q48, Q49 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, Q10, Q11 and/or Q23; Q24 and/or Q27, Q28 and/or Q34, Q35 and/or Q47, Q48 also can form " heterocyclic radical " in each case together;

Wherein randomly, the above-mentioned substituting group of substituting group group (a) and/or substituting group group (i) can and then be selected from following substituting group replacement by at least one independently of one another identically or differently:

(ii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHQ50 ,-NQ51Q52 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-Q53 ,-C (O) O-Q54 ,-C (O) NH-Q55 ,-C (O) NQ56Q57 ,-O-Q58 ,-O are (Q59-O) _r-H (r=1,2,3,4,5) ,-O (Q 60-O) _r-Q61 (r=1,2,3,4,5) ,-OC (O)-Q62 ,-OC (O)-O-Q63 ,-OC (O)-NHQ64 ,-O-C (O)-NQ65Q66 ,-OP (O) is (OQ68) (OQ67), and-OSi (Q69) is (Q71) (Q70) ,-OS (O ₂)-Q72 ,-NHC (O)-Q73 ,-NQ74C (O)-Q75 ,-NH-C (O)-O-Q76 ,-NH-C (O)-NH-Q77 ,-NH-C (O)-NQ78Q79 ,-NQ80-C (O)-O-Q81 ,-NQ82-C (O)-NH-Q83 ,-NQ84-C (O)-NQ85Q86 ,-NHS (O ₂)-Q87 ,-NQ88S (O ₂)-Q89 ,-S-Q90 ,-S (O)-Q91 ,-S (O ₂)-Q92 ,-S (O ₂) NH-Q93 ,-S (O ₂) NQ94Q95 ,-S (O ₂) O-Q96 ,-P (O) is (OQ98) (OQ97), and-Si (Q99) is (Q101) (Q100) ";

Q50 wherein, Q51, Q52, Q53, Q54, Q55, Q56, Q57, Q58, Q59, Q60, Q61, Q62, Q63; Q64, Q65, Q66, Q67, Q68, Q69, Q70, Q71, Q72, Q73, Q74, Q75, Q76; Q77, Q78, Q79, Q80, Q81, Q82, Q83, Q84, Q85, Q86, Q87, Q88, Q89; Q90, Q91, Q92, Q93, Q94, Q95, Q96, Q97, Q98, Q99, Q100, Q101 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, Q56, Q57 and/or Q65; Q66 and/or Q78, Q79 and/or Q85, Q86 and/or Q94, Q95 also can form " heterocyclic radical " in each case together;

(iii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHQ102 ,-NQ103Q104 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-Q105 ,-C (O) O-Q106 ,-C (O) NH-Q107 ,-C (O) NQ108Q109 ,-O-Q110 ,-O are (Q111-O) _s-H (s=1,2,3,4,5) ,-O (Q112-O) _s-Q113 (s=1,2,3,4,5) ,-OC (O)-Q114 ,-OC (O)-O-Q115 ,-OC (O)-NHQ116 ,-O-C (O)-NQ117Q118 ,-OP (O) is (OQ120) (OQ119), and-OSi (Q121) is (Q123) (Q122) ,-OS (O ₂)-Q124 ,-NHC (O)-Q125 ,-NQ126C (O)-Q127 ,-NH-C (O)-O-Q128 ,-NH-C (O)-NH-Q129 ,-NH-C (O)-NQ130Q131 ,-NQ132-C (O)-O-Q133 ,-NQ134-C (O)-NH-Q135 ,-NQ136-C (O)-NQ137Q138 ,-NHS (O ₂)-Q139 ,-NQ140S (O ₂)-Q141 ,-S-Q142 ,-S (O)-Q143 ,-S (O ₂)-Q144 ,-S (O ₂) NH-Q145 ,-S (O ₂) NQ146Q147 ,-S (O ₂) O-Q148 ,-P (O) is (OQ150) (OQ149), and-Si (Q151) is (Q153) (Q152) ";

Q102 wherein, Q103, Q104, Q105, Q106, Q107, Q108, Q109, Q110, Q111, Q112, Q113, Q114, Q115; Q116, Q117, Q118, Q119, Q120, Q121, Q122, Q123, Q124, Q125, Q126, Q127, Q128; Q129, Q130, Q131, Q132, Q133, Q134, Q135, Q136, Q137, Q138, Q139, Q140, Q141; Q142, Q143, Q144, Q145, Q146, Q147, Q148, Q149, Q150, Q151, Q152, Q153 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, Q108, Q109 and/or Q117; Q118 and/or Q130, Q131 and/or Q137, Q138 and/or Q146, Q147 also can form " heterocyclic radical " in each case together;

(b) " (C ₉-C ₃₀) alkyl ,-C (O)-Q154 ,-C (O) O-Q155 ,-C (O)-NQ156Q157 ,-S (O ₂)-Q158 ,-S (O ₂) O-Q159 ";

Q154 wherein, Q155, Q156, Q157, Q158, Q159 is selected from independently of one another: " hydrogen, alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl " and wherein, perhaps, Q156, Q157 also can form " heterocyclic radical " together;

Wherein randomly, the above-mentioned substituting group of substituting group group (b) can and then be selected from following substituting group replacement by at least one independently of one another identically or differently:

(i) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHQ160 ,-NQ161Q162 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-Q163 ,-C (O) O-Q164 ,-C (O) NH-Q165 ,-C (O) NQ166Q167 ,-O-Q168 ,-O are (Q169-O) _t-H (t=1,2,3,4,5) ,-O (Q170-O) _t-Q171 (t=1,2,3,4,5) ,-OC (O)-Q172 ,-OC (O)-O-Q173 ,-OC (O)-NHQ174 ,-O-C (O)-NQ175Q176 ,-OP (O) is (OQ178) (OQ177), and-OSi (Q179) is (Q181) (Q180) ,-OS (O ₂)-Q182 ,-NHC (O)-Q183 ,-NQ184C (O)-Q185 ,-NH-C (O)-O-Q186 ,-NH-C (O)-NH-Q187 ,-NH-C (O)-NQ188Q189 ,-NQ190-C (O)-O-Q191 ,-NQ192-C (O)-NH-Q193 ,-NQ194-C (O)-NQ195Q196 ,-NHS (O ₂)-Q197 ,-NQ198S (O ₂)-Q199 ,-S-Q200 ,-S (O)-Q201 ,-S (O ₂)-Q202 ,-S (O ₂) NH-Q203 ,-S (O ₂) NQ204Q205 ,-S (O ₂) O-Q206 ,-P (O) is (OQ208) (OQ207), and-Si (Q209) is (Q211) (Q210) ";

Q160 wherein, Q161, Q162, Q163, Q164, Q165, Q166, Q167, Q168, Q169, Q170, Q171, Q172, Q173; Q174, Q175, Q176, Q177, Q178, Q179, Q180, Q181, Q182, Q183, Q184, Q185, Q186; Q187, Q188, Q189, Q190, Q191, Q192, Q193, Q194, Q195, Q196, Q197, Q198, Q199; Q200, Q2O1, Q202, Q203, Q204, Q205, Q206, Q207, Q208, Q209, Q210, Q211 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, Q166, Q167 and/or Q175; Q176 and/or Q188, Q189 and/or Q195, Q196 and/or Q204, Q205 also can form " heterocyclic radical " in each case together;

(ii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHQ212 ,-NQ213Q214 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-Q215 ,-C (O) O-Q216 ,-C (O) NH-Q217 ,-C (O) NQ218Q219 ,-O-Q220 ,-O are (Q221-O) _u-H (u=1,2,3,4,5) ,-O (Q 222-O) _u-Q223 (u=1,2,3,4,5) ,-OC (O)-Q224 ,-OC (O)-O-Q225 ,-OC (O)-NHQ226 ,-O-C (O)-NQ227Q228 ,-OP (O) is (OQ230) (OQ229), and-OSi (Q231) is (Q233) (Q232) ,-OS (O ₂)-Q234 ,-NHC (O)-Q235 ,-NQ236C (O)-Q237 ,-NH-C (O)-O-Q238 ,-NH-C (O)-NH-Q239 ,-NH-C (O)-NQ240Q241 ,-NQ242-C (O)-O-Q243 ,-NQ244-C (O)-NH-Q245 ,-NQ246-C (O)-NQ247Q248 ,-NHS (O ₂)-Q249 ,-NQ250S (O ₂)-Q251 ,-S-Q252 ,-S (O)-Q253 ,-S (O ₂)-Q254 ,-S (O ₂) NH-Q255 ,-S (O ₂) NQ256Q257 ,-S (O ₂) O-Q258 ,-P (O) is (OQ260) (OQ259), and-Si (Q261) is (Q263) (Q262) ";

Q212 wherein, Q213, Q214, Q215, Q216, Q217, Q218, Q219, Q220, Q221, Q222, Q223, Q224, Q225; Q226, Q227, Q228, Q229, Q230, Q231, Q232, Q233, Q234, Q235, Q236, Q237, Q238; Q239, Q240, Q241, Q242, Q243, Q244, Q245, Q246, Q247, Q248, Q249, Q250, Q251; Q252, Q253, Q254, Q255, Q256, Q257, Q258, Q259, Q260, Q261, Q262, Q263 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, Q218, Q219 and/or Q227; Q228 and/or Q240, Q241 and/or Q247, Q248 and/or Q256, Q257 also can form " heterocyclic radical " in each case together;

(iii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHQ264 ,-NQ265Q266 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-Q267 ,-C (O) O-Q268 ,-C (O) NH-Q269 ,-C (O) NQ270Q271 ,-O-Q272 ,-O are (Q273-O) _v-H (v=1,2,3,4,5) ,-O (Q274-O) _v-Q275 (v=1,2,3,4,5) ,-OC (O)-Q276 ,-OC (O)-O-Q277 ,-OC (O)-NHQ278 ,-O-C (O)-NQ279Q280 ,-OP (O) is (OQ282) (OQ281), and-OSi (Q283) is (Q285) (Q284) ,-OS (O ₂)-Q286 ,-NHC (O)-Q287 ,-NQ288C (O)-Q289 ,-NH-C (O)-O-Q290 ,-NH-C (O)-NH-Q291 ,-NH-C (O)-NQ292Q293 ,-NQ294-C (O)-O-Q295 ,-NQ296-C (O)-NH-Q297 ,-NQ298-C (O)-NQ299Q300 ,-NHS (O ₂)-Q301 ,-NQ302S (O ₂)-Q303 ,-S-Q304 ,-S (O)-Q305 ,-S (O ₂)-Q306 ,-S (O ₂) NH-Q307 ,-S (O ₂) NQ308Q309 ,-S (O ₂) O-Q310 ,-P (O) is (OQ312) (OQ311), and-Si (Q313) is (Q315) (Q314) ";

Q264 wherein, Q265, Q266, Q267, Q268, Q269, Q270, Q271, Q272, Q273, Q274, Q275, Q276, Q277; Q278, Q279, Q280, Q281, Q282, Q283, Q284, Q285, Q286, Q287, Q288, Q289, Q290; Q291, Q292, Q293, Q294, Q295, Q296, Q297, Q298, Q299, Q300, Q301, Q302, Q303; Q304, Q305, Q306, Q307, Q308, Q309, Q310, Q311, Q312, Q313, Q314, Q315 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, Q270, Q271 and/or Q279; Q280 and/or Q292, Q293 and/or Q299, Q300 and/or Q308, Q309 also can form " heterocyclic radical " in each case together;

OrOne of Z10, Z11 group or Z10, Z11 group none are selected from independently of one another:

(c) " hydrogen, alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, heterocyclic radical, heterocyclic radical alkyl ,-C (O)-Q316 ,-C (O) O-Q317 ,-C (O)-NQ318Q319 ,-S (O ₂)-Q320 ,-S (O ₂) O-Q321 ";

Q316 wherein, Q317, Q318, Q319, Q320, Q321 is selected from independently of one another: " hydrogen, alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl " and wherein, perhaps, Q318, Q319 also can form " heterocyclic radical " together;

Wherein randomly, the above-mentioned substituting group of substituting group group (c) can and then be selected from following substituting group by at least one independently of one another identically or differently and replace when being not hydrogen:

(i) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHQ322 ,-NQ323Q324 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-Q325 ,-C (O) O-Q326 ,-C (O) NH-Q327 ,-C (O) NQ328Q329 ,-O-Q330 ,-O are (Q331-O) _w-H (w=1,2,3,4,5) ,-O (Q332-O) _w-Q333 (w=1,2,3,4,5) ,-OC (O)-Q334 ,-OC (O)-O-Q335 ,-OC (O)-NHQ336 ,-O-C (O)-NQ337Q338 ,-OP (O) is (OQ340) (OQ339), and-OSi (Q341) is (Q343) (Q342) ,-OS (O ₂)-Q344 ,-NHC (O)-Q345 ,-NQ346C (O)-Q347 ,-NH-C (O)-O-Q348 ,-NH-C (O)-NH-Q349 ,-NH-C (O)-NQ350Q351 ,-NQ352-C (O)-O-Q353 ,-NQ354-C (O)-NH-Q355 ,-NQ356-C (O)-NQ357Q358 ,-NHS (O ₂)-Q359 ,-NQ360S (O ₂)-Q361 ,-S-Q362 ,-S (O)-Q363 ,-S (O ₂)-Q364 ,-S (O ₂) NH-Q365 ,-S (O ₂) NQ366Q367 ,-S (O ₂) O-Q368 ,-P (O) is (OQ370) (OQ369), and-Si (Q371) is (Q373) (Q372) ";

Q322 wherein, Q323, Q324, Q325, Q326, Q327, Q328, Q329, Q330, Q331, Q332, Q333, Q334, Q335; Q336, Q337, Q338, Q339, Q340, Q341, Q342, Q343, Q344, Q345, Q346, Q347, Q348; Q349, Q350, Q351, Q352, Q353, Q354, Q355, Q356, Q357, Q358, Q359, Q360, Q361; Q362, Q363, Q364, Q365, Q366, Q367, Q368, Q369, Q370, Q371, Q372, Q373 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, Q328, Q329 and/or Q337; Q338 and/or Q350, Q351 and/or Q357, Q358 and/or Q366, Q367 also can form " heterocyclic radical " in each case together;

(ii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHQ374 ,-NQ375Q376 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-Q377 ,-C (O) O-Q378 ,-C (O) NH-Q379 ,-C (O) NQ380Q381 ,-O-Q382 ,-O are (Q383-O) _x-H (x=1,2,3,4,5) ,-O (Q384-O) _x-Q385 (x=1,2,3,4,5) ,-OC (O)-Q386 ,-OC (O)-O-Q387 ,-OC (O)-NHQ388 ,-O-C (O)-NQ389Q390 ,-OP (O) is (OQ392) (OQ391), and-OSi (Q393) is (Q395) (Q394) ,-OS (O ₂)-Q396 ,-NHC (Q)-Q397 ,-NQ398C (O)-Q399 ,-NH-C (O)-O-Q400 ,-NH-C (O)-NH-Q401 ,-NH-C (O)-NQ402Q403 ,-NQ404-C (O)-O-Q405 ,-NQ406-C (O)-NH-Q407 ,-NQ408-C (O)-NQ409Q410 ,-NHS (O ₂)-Q411 ,-NQ412S (O ₂)-Q413 ,-S-Q414 ,-S (O)-Q415 ,-S (O ₂)-Q416 ,-S (O ₂) NH-Q417 ,-S (O ₂) NQ418Q419 ,-S (O ₂) O-Q420 ,-P (O) is (OQ422) (OQ421), and-Si (Q423) is (Q425) (Q424) ";

Q374 wherein, Q375, Q376, Q377, Q378, Q379, Q380, Q381, Q382, Q383, Q384, Q385, Q386, Q387; Q388, Q389, Q390, Q391, Q392, Q393, Q394, Q395, Q396, Q397, Q398, Q399, Q400; Q401, Q402, Q403, Q404, Q405, Q406, Q407, Q408, Q409, Q410, Q411, Q412, Q413; Q414, Q415, Q416, Q417, Q418, Q419, Q420, Q421, Q422, Q423, Q424, Q425 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, Q380, Q381 and/or Q389; Q390 and/or Q402, Q403 and/or Q409, Q410 and/or Q418, Q419 also can form " heterocyclic radical " in each case together;

(iii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHQ426 ,-NQ427Q428 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-Q429 ,-C (O) O-Q430 ,-C (O) NH-Q431 ,-C (O) NQ432Q433 ,-O-Q434 ,-O are (Q435-O) _y-H (y=1,2,3,4,5) ,-O (Q436-O) _y-Q437 (y=1,2,3,4,5) ,-OC (O)-Q438 ,-OC (O)-O-Q439 ,-OC (O)-NHQ440 ,-O-C (O)-NQ441Q442 ,-OP (O) is (OQ444) (OQ443), and-OSi (Q445) is (Q447) (Q446) ,-OS (O ₂)-Q448 ,-NHC (O)-Q449 ,-NQ450C (O)-Q451 ,-NH-C (O)-O-Q452;-NH-C (O)-NH-Q453 ,-NH-C (O)-NQ454Q455 ,-NQ456a-C (O)-O-Q456b;-NQ456c-C (O)-NH-Q456d ,-NQ456e-C (O)-NQ456fQ456g ,-NHS (O ₂)-Q456h ,-NQ456iS (O ₂)-Q456j ,-S-Q456k ,-S (O)-Q4561 ,-S (O ₂)-Q456m ,-S (O ₂) NH-Q456n ,-S (O ₂) NQ456oQ456p ,-S (O ₂) O-Q456q ,-P (O) is (OQ456s) (OQ456r), and-Si (Q456t) is (Q456v) (Q456u) ";

Q426 wherein, Q427, Q428, Q429, Q430, Q431, Q432, Q433, Q434, Q435, Q436; Q437, Q438, Q439, Q440, Q441, Q442, Q443, Q444, Q445, Q446, Q447; Q448, Q449, Q450, Q451, Q452, Q453, Q454, Q455, Q456a, Q456b, Q456c; Q456d, Q456e, Q456f, Q456g, Q456h, Q456i, Q456j, Q456k, Q4561, Q456m; Q456n, Q456o, Q456p, Q456q, Q456r, Q456s, Q456t, Q456u, Q456v is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, Q432, Q433 and/or Q441; Q442 and/or Q454, Q455 and/or Q456f, Q456g and/or Q456o, Q456p also can form " heterocyclic radical " in each case together;

AndOne of Z3, Z4 group or Z3, Z4 group none are independently selected from:

(d) hydrogen;

(e) halogen, F, Cl, Br, I;

(f) unsubstituted or substituted alkyl or (C ₉-C ₃₀) alkyl, wherein randomly, said alkyl or (C ₉-C ₃₀) alkyl can or different are selected from following substituting group and replace by at least one identical ground:

(i) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHQ457 ,-NQ458Q459 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-Q460 ,-C (O) O-Q461 ,-C (O) NH-Q462 ,-C (O) NQ463Q464 ,-O-Q465 ,-O are (Q466-O) _z-H (z=1,2,3,4,5) ,-O (Q467-O) _z-Q468 (z=1,2,3,4,5) ,-OC (O)-Q469 ,-OC (O)-O-Q470 ,-OC (O)-NHQ471 ,-O-C (O)-NQ472Q473 ,-OP (O) is (OQ475) (OQ474), and-OSi (Q476) is (Q478) (Q477) ,-OS (O ₂)-Q479 ,-NHC (O)-Q480 ,-NQ481C (O)-Q482 ,-NH-C (O)-O-Q483 ,-NH-C (O)-NH-Q484 ,-NH-C (O)-NQ485Q486 ,-NQ487-C (O)-O-Q488 ,-NQ489-C (O)-NH-Q490 ,-NQ491-C (O)-NQ492Q493 ,-NHS (O ₂)-Q494 ,-NQ495S (O ₂)-Q496 ,-S-Q497 ,-S (O)-Q498 ,-S (O ₂)-Q499 ,-S (O ₂) NH-Q500 ,-S (O ₂) NQ501Q502 ,-S (O ₂) O-Q503 ,-P (O) is (OQ505) (OQ504), and-Si (Q506) is (Q508) (Q507) ";

Q457 wherein, Q458, Q459, Q460, Q461, Q462, Q463, Q464, Q465, Q466, Q467, Q468, Q469, Q470; Q471, Q472, Q473, Q474, Q475, Q476, Q477, Q478, Q479, Q480, Q481, Q482, Q483; Q484, Q485, Q486, Q487, Q488, Q489, Q490, Q491, Q492, Q493, Q494, Q495, Q496; Q497, Q498, Q499, Q500, Q501, Q502, Q503, Q504, Q505, Q506, Q507, Q508 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, Q463, Q464 and/or Q472; Q473 and/or Q485, Q486 and/or Q492, Q493 and/or Q501, Q502 also can form " heterocyclic radical " in each case together;

(ii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHQ509 ,-NQ510Q511 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-Q512 ,-C (O) O-Q513 ,-C (O) NH-Q514 ,-C (O) NQ515Q516 ,-O-Q517 ,-O are (Q518-O) _a-H (a=1,2,3,4,5) ,-O (Q519-O) _a-Q520 (a=1,2,3,4,5) ,-OC (O)-Q521 ,-OC (O)-O-Q522 ,-OC (O)-NHQ523 ,-O-C (O)-NQ524Q525 ,-OP (O) is (OQ527) (OQ526), and-OSi (Q528) is (Q530) (Q529) ,-OS (O ₂)-Q531 ,-NHC (O)-Q532 ,-NQ533C (O)-Q534 ,-NH-C (O)-O-Q535 ,-NH-C (O)-NH-Q536 ,-NH-C (O)-NQ537Q538 ,-NQ539-C (O)-O-Q540 ,-NQ541-C (O)-NH-Q542 ,-NQ543-C (O)-NQ544Q545 ,-NHS (O ₂)-Q546 ,-NQ547S (O ₂)-Q548 ,-S-Q549 ,-S (O)-Q550 ,-S (O ₂)-Q551 ,-S (O ₂) NH-Q552 ,-S (O ₂) NQ553Q554 ,-S (O ₂) O-Q555 ,-P (O) is (OQ557) (OQ556), and-Si (Q558) is (Q560) (Q559) ";

Q509 wherein, Q510, Q511, Q512, Q513, Q514, Q515, Q516, Q517, Q518, Q519, Q520, Q521, Q522; Q523, Q524, Q525, Q526, Q527, Q528, Q529, Q530, Q531, Q532, Q533, Q534, Q535; Q536, Q537, Q538, Q539, Q540, Q541, Q542, Q543, Q544, Q545, Q546, Q547, Q548; Q549, Q550, Q551, Q552, Q553, Q554, Q555, Q556, Q557, Q558, Q559, Q560 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, Q515, Q516 and/or Q524; Q525 and/or Q537, Q538 and/or Q544, Q545 and/or Q553, Q554 also can form " heterocyclic radical " in each case together;

(iii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHQ561 ,-NQ562Q563 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-Q564 ,-C (O) O-Q565 ,-C (O) NH-Q566 ,-C (O) NQ567Q568 ,-O-Q569 ,-O are (Q570-O) _b-H (b=1,2,3,4,5) ,-O (Q571-O) _b-Q572 (b=1,2,3,4,5) ,-OC (O)-Q573 ,-OC (O)-O-Q574 ,-OC (O)-NHQ575 ,-O-C (O)-NQ576Q577 ,-OP (O) is (OQ579) (OQ578), and-OSi (Q580) is (Q582) (Q581) ,-OS (O ₂)-Q583 ,-NHC (O)-Q584 ,-NQ585C (O)-Q586 ,-NH-C (O)-O-Q587 ,-NH-C (O)-NH-Q588 ,-NH-C (O)-NQ589Q590 ,-NQ591-C (O)-O-Q592 ,-NQ593-C (O)-NH-Q594 ,-NQ595-C (O)-NQ596Q597 ,-NHS ( _O2)-and Q598 ,-NQ599S (O ₂)-Q600 ,-S-Q601 ,-S (O)-Q602 ,-S (O ₂)-Q603 ,-S (O ₂) NH-Q604 ,-S (O ₂) NQ605Q606 ,-S (O ₂) O-Q607 ,-P (O) is (OQ609) (OQ608), and-Si (Q610) is (Q612) (Q611) ";

Q561 wherein, Q562, Q563, Q564, Q565, Q566, Q567, Q568, Q569, Q570, Q571, Q572, Q573, Q574; Q575, Q576, Q577, Q578, Q579, Q580, Q581, Q582, Q583, Q584, Q585, Q586, Q587; Q588, Q589, Q590, Q591, Q592, Q593, Q594, Q595, Q596, Q597, Q598, Q599, Q600; Q601, Q602, Q603, Q604, Q605, Q606, Q607, Q608, Q609, Q610, Q611, Q612 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, Q567, Q568 and/or Q576; Q577 and/or Q589, Q590 and/or Q596, Q597 and/or Q605, Q606 also can form " heterocyclic radical " in each case together;

(g) unsubstituted or substituted aryl, wherein randomly, said aryl can be selected from following substituting group by at least one identically or differently and replace:

(i) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHQ613 ,-NQ614Q615 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-Q616 ,-C (O) O-Q617 ,-C (O) NH-Q618 ,-C (O) NQ619Q620 ,-O-Q621 ,-O are (Q622-O) _c-H (c=1,2,3,4,5) ,-O (Q623-O) _c-Q624 (c=1,2,3,4,5) ,-OC (O)-Q625 ,-OC (O)-O-Q626 ,-OC (O)-NHQ627 ,-O-C (O)-NQ628Q629 ,-OP (O) is (OQ631) (OQ630), and-OSi (Q632) is (Q634) (Q633) ,-OS (O ₂)-Q635 ,-NHC (O)-Q636 ,-NQ637C (O)-Q638 ,-NH-C (O)-O-Q639 ,-NH-C (O)-NH-Q640 ,-NH-C (O)-NQ641Q642 ,-NQ643-C (O)-O-Q644 ,-NQ645-C (O)-NH-Q646 ,-NQ647-C (O)-NQ648Q649 ,-NHS (O ₂)-Q650 ,-NQ651S (O ₂)-Q652 ,-S-Q653 ,-S (O)-Q654 ,-S (O ₂)-Q655 ,-S (O ₂) NH-Q656 ,-S (O ₂) NQ657Q658 ,-S (O ₂) O-Q659 ,-P (O) is (OQ661) (OQ660), and-Si (Q662) is (Q664) (Q663) ";

Q613 wherein, Q614, Q615, Q616, Q617, Q618, Q619, Q620, Q621, Q622, Q623, Q624, Q625, Q626; Q627, Q628, Q629, Q630, Q631, Q632, Q633, Q634, Q635, Q636, Q637, Q638, Q639; Q640, Q641, Q642, Q643, Q644, Q645, Q646, Q647, Q648, Q649, Q650, Q651, Q652; Q653, Q654, Q655, Q656, Q657, Q658, Q659, Q660, Q661, Q662, Q663, Q664 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, Q619, Q620 and/or Q628; Q629 and/or Q641, Q642 and/or Q648, Q649 and/or Q657, Q658 also can form " heterocyclic radical " in each case together;

(ii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHQ665 ,-NQ666Q667 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-Q668 ,-C (O) O-Q669 ,-C (O) NH-Q670 ,-C (O) NQ671Q672 ,-O-Q673 ,-O are (Q674-O) _d-H (d=1,2,3,4,5) ,-O (Q675-O) _d-Q676 (d=1,2,3,4,5) ,-OC (O)-Q677 ,-OC (O)-O-Q678 ,-OC (O)-NHQ679 ,-O-C (O)-NQ680Q681 ,-OP (O) is (OQ683) (OQ682), and-OSi (Q684) is (Q686) (Q685) ,-OS (O ₂)-Q687 ,-NHC (O)-Q688 ,-NQ689C (O)-Q690 ,-NH-C (O)-O-Q691 ,-NH-C (O)-NH-Q692 ,-NH-C (O)-NQ693Q694 ,-NQ695-C (O)-O-Q696 ,-NQ697-C (O)-NH-Q698 ,-NQ699-C (O)-NQ700Q701 ,-NHS (O ₂)-Q702 ,-NQ703S (O ₂)-Q704 ,-S-Q705 ,-S (O)-Q706 ,-S (O ₂)-Q707 ,-S (O ₂) NH-Q708 ,-S (O ₂) NQ709Q710 ,-S (O ₂) O-Q711 ,-P (O) is (OQ713) (OQ712), and-Si (Q714) is (Q716) (Q715) ";

Q665 wherein, Q666, Q667, Q668, Q669, Q670, Q671, Q672, Q673, Q674, Q675, Q676, Q677, Q678; Q679, Q680, Q681, Q682, Q683, Q684, Q685, Q686, Q687, Q688, Q689, Q690, Q691; Q692, Q693, Q694, Q695, Q696, Q697, Q698, Q699, Q700, Q701, Q702, Q703, Q704; Q705, Q706, Q707, Q708, Q709, Q710, Q711, Q712, Q713, Q714, Q715, Q716 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, Q671, Q672 and/or Q680; Q681 and/or Q693, Q694 and/or Q700, Q701 and/or Q709, Q710 also can form " heterocyclic radical " in each case together;

(iii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHQ717 ,-NQ718Q719 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-Q720 ,-C (O) O-Q721 ,-C (O) NH-Q722 ,-C (O) NQ 723Q724 ,-O-Q725 ,-O are (Q726-O) _e-H (e=1,2,3,4,5) ,-O (Q727-O) _e-Q728 (e=1,2,3,4,5) ,-OC (O)-Q729 ,-OC (O)-O-Q730 ,-OC (O)-NHQ731 ,-O-C (O)-NQ732Q733 ,-OP (O) is (OQ735) (OQ734), and-OSi (Q736) is (Q738) (Q737) ,-OS (O ₂)-Q739 ,-NHC (O)-Q74O ,-NQ741C (O)-Q742 ,-NH-C (O)-O-Q743 ,-NH-C (O)-NH-Q744 ,-NH-C (O)-NQ745Q746 ,-NQ747-C (O)-O-Q748 ,-NQ749-C (O)-NH-Q750 ,-NQ751-C (O)-NQ752Q753 ,-NHS (O ₂)-Q754 ,-NQ755S (O ₂)-Q756 ,-S-Q757 ,-S (O)-Q758 ,-S (O ₂)-Q759 ,-S (O ₂) NH-Q760 ,-S (O ₂) NQ761Q762 ,-S (O ₂) O-Q763 ,-P (O) is (OQ765) (OQ764), and-Si (Q766) is (Q768) (Q767) ";

Q717 wherein, Q718, Q719, Q720, Q721, Q722, Q723, Q724, Q725, Q726, Q727, Q728, Q729, Q730; Q731, Q732, Q733, Q734, Q735, Q736, Q737, Q738, Q739, Q740, Q741, Q742, Q743; Q744, Q745, Q746, Q747, Q748, Q749, Q750, Q751, Q752, Q753, Q754, Q755, Q756; Q757, Q758, Q759, Q760, Q761, Q762, Q763, Q764, Q765, Q766, Q767, Q768 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, Q723, Q724 and/or Q732; Q733 and/or Q745, Q746 and/or Q752, Q753 and/or Q761, Q762 also can form " heterocyclic radical " in each case together;

(h) unsubstituted or substituted heteroaryl, wherein randomly, said heteroaryl can be selected from following substituting group by at least one identically or differently and replace:

(i) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHQ769 ,-NQ770Q771 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-Q772 ,-C (O) O-Q773 ,-C (O) NH-Q774 ,-C (O) NQ775Q776 ,-O-Q777 ,-O are (Q778-O) _f-H (f=1,2,3,4,5) ,-O (Q779-O) _f-Q780 (f=1,2,3,4,5) ,-OC (O)-Q781 ,-OC (O)-O-Q782 ,-OC (O)-NHQ783 ,-O-C (O)-NQ784Q785 ,-OP (O) is (OQ787) (OQ786), and-OSi (Q788) is (Q790) (Q789) ,-OS (O ₂)-Q791 ,-NHC (O)-Q792 ,-NQ793C (O)-Q794 ,-NH-C (O)-O-Q795 ,-NH-C (O)-NH-Q796 ,-NH-C (O)-NQ797Q798 ,-NQ799-C (O)-O-Q800 ,-NQ801-C (O)-NH-Q802 ,-NQ803-C (O)-NQ804Q805 ,-NHS (O ₂)-Q806 ,-NQ807S (O ₂)-Q808 ,-S-Q809 ,-S (O)-Q810 ,-S (O ₂)-Q811 ,-S (O ₂) NH-Q812 ,-S (O ₂) NQ813Q814 ,-S (O ₂) O-Q815 ,-P (O) is (OQ817) (OQ816), and-Si (Q818) is (Q820) (Q819) ";

Q769 wherein, Q770, Q771, Q772, Q773, Q774, Q775, Q776, Q777, Q778, Q779, Q780, Q781, Q782; Q783, Q784, Q785, Q786, Q787, Q788, Q789, Q790, Q791, Q792, Q793, Q794, Q795; Q796, Q797, Q798, Q799, Q800, Q801, Q802, Q803, Q804, Q805, Q806, Q807, Q808; Q809, Q810, Q811, Q812, Q813, Q814, Q815, Q816, Q817, Q818, Q819, Q820 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, Q775, Q776 and/or Q784; Q785 and/or Q797, Q798 and/or Q804, Q805 and/or Q813, Q814 also can form " heterocyclic radical " in each case together;

(ii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHQ821 ,-NQ822Q823 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-Q824 ,-C (O) O-Q825 ,-C (O) NH-Q826 ,-C (O) NQ827Q828 ,-O-Q829 ,-O are (Q830-O) _g-H (g=1,2,3,4,5) ,-O (Q831-O) _g-Q832 (g=1,2,3,4,5) ,-OC (O)-Q833 ,-OC (O)-O-Q834 ,-OC (O)-NHQ835 ,-O-C (O)-NQ836Q837 ,-OP (O) is (OQ839) (OQ838), and-OSi (Q840) is (Q842) (Q841) ,-OS (O ₂)-Q843 ,-NHC (O)-Q844 ,-NQ845C (O)-Q846 ,-NH-C (O)-O-Q847 ,-NH-C (O)-NH-Q848 ,-NH-C (O)-NQ849Q850 ,-NQ851-C (O)-O-Q852 ,-NQ853-C (O)-NH-Q854 ,-NQ855-C (O)-NQ856Q857 ,-NHS (O ₂)-Q858 ,-NQ859S (O ₂)-Q860 ,-S-Q861 ,-S (O)-Q862 ,-S (O ₂)-Q863 ,-S (O ₂) NH-Q864 ,-S (O ₂) NQ865Q866 ,-S (O ₂) O-Q867 ,-P (O) is (OQ869) (OQ868), and-Si (Q870) is (Q872) (Q871) ";

Q821 wherein, Q822, Q823, Q824, Q825, Q826, Q827, Q828, Q829, Q830, Q831, Q832, Q833, Q834; Q835, Q836, Q837, Q838, Q839, Q840, Q841, Q842, Q843, Q844, Q845, Q846, Q847; Q848, Q849, Q850, Q851, Q852, Q853, Q854, Q855, Q856, Q857, Q858, Q859, Q860; Q861, Q862, Q863, Q864, Q865, Q866, Q867, Q868, Q869, Q870, Q871, Q872 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, Q827, Q828 and/or Q836; Q837 and/or Q849, Q850 and/or Q856, Q857 and/or Q865, Q866 also can form " heterocyclic radical " in each case together;

(iii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHQ873 ,-NQ874Q875 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-Q876 ,-C (O) O-Q877 ,-C (O) NH-Q878 ,-C (O) NQ879Q880 ,-O-Q881 ,-O are (Q882-O) _h-H (h=1,2,3,4,5) ,-O (Q883-O) _h-Q884 (h=1,2,3,4,5) ,-OC (O)-Q885 ,-OC (O)-O-Q886 ,-OC (O)-NHQ887 ,-O-C (O)-NQ888Q889 ,-OP (O) is (OQ891) (OQ890), and-OSi (Q892) is (Q894) (Q893) ,-OS (O ₂)-Q895 ,-NHC (O)-Q896 ,-NQ897C (O)-Q898 ,-NH-C (O)-O-Q899 ,-NH-C (O)-NH-Q900 ,-NH-C (O)-NQ901Q902 ,-NQ903-C (O)-O-Q904 ,-NQ905-C (O)-NH-Q906 ,-NQ907-C (O)-NQ908Q909 ,-NHS (O ₂)-Q910 ,-NQ911S (O ₂)-Q912 ,-S-Q913 ,-S (O)-Q914 ,-S (O ₂)-Q915 ,-S (O ₂) NH-Q916 ,-S (O ₂) NQ917Q918 ,-S (O ₂) O-Q919 ,-P (O) is (OQ921) (OQ920), and-Si (Q922) is (Q924) (Q923) ";

Q873 wherein, Q874, Q875, Q876, Q877, Q878, Q879, Q880, Q881, Q882, Q883, Q884, Q885, Q886; Q887, Q888, Q889, Q890, Q891, Q892, Q893, Q894, Q895, Q896, Q897, Q898, Q899; Q900, Q901, Q902, Q903, Q904, Q905, Q906, Q907, Q908, Q909, Q910, Q911, Q912; Q913, Q914, Q915, Q916, Q917, Q918, Q919, Q920, Q921, Q922, Q923, Q924 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, Q879, Q880 and/or Q888; Q889 and/or Q901, Q902 and/or Q908, Q909 and/or Q917, Q918 also can form " heterocyclic radical " in each case together;

(j) OZ6, wherein Z6 is independently selected from:

(ii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHQ925 ,-NQ926Q927 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-Q928 ,-C (O) O-Q929 ,-C (O) NH-Q930 ,-C (O) NQ931Q932 ,-O-Q933 ,-O are (Q934-O) _i-H (i=1,2,3,4,5) ,-O (Q935-O) _i-Q936 (i=1,2,3,4,5) ,-OC (O)-Q937 ,-OC (O)-O-Q938 ,-OC (O)-NHQ939 ,-O-C (O)-NQ940Q941 ,-OP (O) is (OQ943) (OQ942), and-OSi (Q944) is (Q946) (Q945) ,-OS (O ₂)-Q947 ,-NHC (O)-Q948 ,-NQ949C (O)-Q950 ,-NH-C (O)-O-Q951 ,-NH-C (O)-NH-Q952 ,-NH-C (O)-NQ953Q954 ,-NQ955-C (O)-O-Q956 ,-NQ957-C (O)-NH-Q958 ,-NQ959-C (O)-NQ960Q961 ,-NHS (O ₂)-Q962 ,-NQ963S (O ₂)-Q964 ,-S-Q965 ,-S (O)-Q966 ,-S (O ₂)-Q967 ,-S (O ₂) NH-Q968 ,-S (O ₂) NQ969Q970 ,-S (O ₂) O-Q971 ,-P (O) is (OQ973) (OQ972), and-Si (Q974) is (Q976) (Q975) ";

Q925 wherein, Q926, Q927, Q928, Q929, Q930, Q931, Q932, Q933, Q934, Q935, Q936, Q937, Q938; Q939, Q940, Q941, Q942, Q943, Q944, Q945, Q946, Q947, Q948, Q949, Q950, Q951; Q952, Q953, Q954, Q955, Q956, Q957, Q958, Q959, Q960, Q961, Q962, Q963, Q964; Q965, Q966, Q967, Q968, Q969, Q970, Q971, Q972, Q973, Q974, Q975, Q976 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, Q931, Q932 and/or Q940; Q941 and/or Q953, Q954 and/or Q960, Q961 and/or Q969, Q970 also can form " heterocyclic radical " in each case together;

(iii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHQ977 ,-NQ978Q979 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-Q980 ,-C (O) O-Q981 ,-C (O) NH-Q982 ,-C (O) NQ983Q984 ,-O-Q985 ,-O are (Q986-O) _j-H (j=1,2,3,4,5) ,-O (Q987-O) _j-Q988 (j=1,2,3,4,5) ,-OC (O)-Q989 ,-OC (O)-O-Q990 ,-OC (O)-NHQ991 ,-O-C (Q)-NQ992Q993 ,-OP (O) is (OQ995) (OQ994), and-OSi (Q996) is (Q998) (Q997) ,-OS (O ₂)-Q999 ,-NHC (O)-Q1000 ,-NQ1001C (O)-Q1002 ,-NH-C (O)-O-Q1003;-NH-C (O)-NH-Q1004 ,-NH-C (O)-NQ1005Q1006 ,-NQ1007-C (O)-O-Q1008;-NQ1009-C (O)-NH-Q1010 ,-NQ1011-C (O)-NQ1012Q1013 ,-NHS (O ₂)-Q1014 ,-NQ1015S (O ₂)-Q1016 ,-S-Q1017 ,-S (O)-Q1018 ,-S (O ₂)-Q1019 ,-S (O ₂) NH-Q1020 ,-S (O ₂) NQ1021Q1022 ,-S (O ₂) O-Q1023 ,-P (O) is (OQ1025) (OQ1024), and-Si (Q1026) is (Q1028) (Q1027) ";

Q977 wherein, Q978, Q979, Q980, Q981, Q982, Q983, Q984, Q985, Q986, Q987; Q988, Q989, Q990, Q991, Q992, Q993, Q994, Q995, Q996, Q997, Q998; Q999, Q1000, Q1001, Q1002, Q1003, Q1004, Q1005, Q1006, Q1007, Q1008, Q1009; Q1010, Q1011, Q1012, Q1013, Q1014, Q1015, Q1016, Q1017, Q1018, Q1019; Q1020, Q1021, Q1022, Q1023, Q1024, Q1025, Q1026, Q1027, Q1028 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, Q983, Q984 and/or Q992; Q993 and/or Q1005, Q1006 and/or Q1012, Q1013 and/or Q1021, Q1022 also can form " heterocyclic radical " in each case together;

(k) SZ7, wherein Z7 is independently selected from:

(ii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHQ1029 ,-NQ1030Q1031 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-Q1032 ,-C (O) O-Q1033 ,-C (O) NH-Q1034 ,-C (O) NQ1035Q1036 ,-O-Q1037 ,-O are (Q1038-O) _k-H (k=1,2,3,4,5) ,-O (Q1039-O) _k-Q1040 (k=1,2,3,4,5) ,-OC (O)-Q1041 ,-OC (O)-O-Q1042 ,-OC (O)-NHQ1043 ,-O-C (O)-NQ1044Q1045 ,-OP (O) is (OQ1047) (OQ1046), and-OSi (Q1048) is (Q1050) (Q1049) ,-OS (O ₂)-Q1051 ,-NHC (O)-Q1052 ,-NQ1053C (O)-Q1054 ,-NH-C (O)-O-Q1055;-NH-C (O)-NH-Q1056 ,-NH-C (O)-NQ1057Q1058 ,-NQ1059-C (O)-O-Q1060;-NQ1061-C (O)-NH-Q1062 ,-NQ1063-C (O)-NQ1064Q1065 ,-NHS (O ₂)-Q1066 ,-NQ1067S (O ₂)-Q1068 ,-S-Q1069 ,-S (O)-Q1070 ,-S (O ₂)-Q1071 ,-S (O ₂) NH-Q1072 ,-S (O ₂) NQ1073Q1074 ,-S (O ₂) O-Q1075 ,-P (O) is (OQ1077) (OQ1076), and-Si (Q1078) is (Q1080) (Q1079) ";

Q1029 wherein, Q1030, Q1031, Q1032, Q1033, Q1034, Q1035, Q1036, Q1037, Q1038, Q1039; Q1040, Q1041, Q1042, Q1043, Q1044, Q1045, Q1046, Q1047, Q1048, Q1049, Q1050; Q1051, Q1052, Q1053, Q1054, Q1055, Q1056, Q1057, Q1058, Q1059, Q1060, Q1061; Q1062, Q1063, Q1064, Q1065, Q1066, Q1067, Q1068, Q1069, Q1070, Q1071; Q1072, Q1073, Q1074, Q1075, Q1076, Q1077, Q1078, Q1079, Q1080 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base 2 cycloalkylalkyls, heterocyclic radical, heterocyclic radical alkyl; Aryl, arylalkyl, heteroaryl, heteroarylalkyl " and wherein; perhaps, Q1035, Q1036 and/or Q1044, Q1045 and/or Q1057; Q1058 and/or Q1064, Q1065 and/or Q1073, Q1074 also can form " heterocyclic radical " in each case together;

(iii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHQ1081 ,-NQ1082Q1083 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-Q1084 ,-C (O) O-Q1085 ,-C (O) NH-Q1086 ,-C (O) NQ1087Q1088 ,-O-Q1089 ,-O are (Q1090-O) _l-H (1=1,2,3,4,5) ,-O (Q1091-O) _l-Q1092 (1=1,2,3,4,5) ,-OC (O)-Q1093 ,-OC (O)-O-Q1094 ,-OC (O)-NHQ1095 ,-O-C (O)-NQ1096Q1097 ,-OP (O) is (OQ1099) (OQ1098), and-OSi (Q1100) is (Q1102) (Q1101) ,-OS (O ₂)-Q1103 ,-NHC (O)-Q1104 ,-NQ1105C (O)-Q1106 ,-NH-C (O)-O-Q1107;-NH-C (O)-NH-Q1108 ,-NH-C (O)-NQ1109Q1110 ,-NQ1111-C (O)-O-Q1112;-NQ1113-C (O)-NH-Q1114 ,-NQ1115-C (O)-NQ1116Q1117 ,-NHS (O ₂)-Q1118 ,-NQ1119S (O ₂)-Q1120 ,-S-Q1121 ,-S (O)-Q1122 ,-S (O ₂)-Q1123 ,-S (O ₂) NH-Q1124 ,-S (O ₂) NQ1125Q1126 ,-S (O ₂) O-Q1127 ,-P (O) is (OQ1129) (OQ1128), and-Si (Q1130) is (Q1132) (Q1131) ";

Q1081 wherein, Q1082, Q1083, Q1084, Q1085, Q1086, Q1087, Q1088, Q1089, Q1090, Q1091; Q1092, Q1093, Q1094, Q1095, Q1096, Q1097, Q1098, Q1099, Q1100, Q1101, Q1102; Q1103, Q1104, Q1105, Q1106, Q1107, Q1108, Q1109, Q1110, Q1111, Q1112, Q1113; Q1114, Q1115, Q1116, Q1117, Q1118, Q1119, Q1120, Q1121, Q1122, Q1123; Q1124, Q1125, Q1126, Q1127, Q1128, Q1129, Q1130, Q1131, Q1132 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, Q1087, Q1088 and/or Q1096; Q1097 and/or Q1109, Q1110 and/or Q1116, Q1117 and/or Q1125, Q1126 also can form " heterocyclic radical " in each case together;

(1) NZ8Z9, Z8 wherein, Z9 is selected from independently of one another:

(i) " hydrogen, alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl ,-C (O)-Q1133 ,-C (O) O-Q1134 ,-C (O)-NQ1135Q1136 ,-S (O ₂)-Q1137 ,-S (O ₂) O-Q1138 ";

Q1133 wherein, Q1134, Q1135, Q1136, Q1137, Q1138 is selected from independently of one another: hydrogen, alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl " and wherein, perhaps, Q1135, Q1136 also can form " heterocyclic radical " together;

(ii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHQ1139 ,-NQ1140Q1141 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-Q1142 ,-C (O) O-Q1143 ,-C (O) NH-Q1144 ,-C (O) NQ1145Q1146 ,-O-Q1147 ,-O are (Q1148-O) _m-H (m=1,2,3,4,5) ,-O (Q1149-O) _m-Q1150 (m=1,2,3,4,5) ,-OC (O)-Q1151 ,-OC (O)-O-Q1152 ,-OC (O)-NHQ1153 ,-O-C (O)-NQ1154Q1155 ,-OP (O) is (OQ1157) (OQ1156), and-OSi (Q1158) is (Q1160) (Q1159) ,-OS (O ₂)-Q1161 ,-NHC (O)-Q1162 ,-NQ1163C (O)-Q1164 ,-NH-C (O)-O-Q1165;-NH-C (O)-NH-Q1166 ,-NH-C (O)-NQ1167Q1168 ,-NQ1169-C (O)-O-Q1170;-NQ1171-C (O)-NH-Q1172 ,-NQ1173-C (O)-NQ1174Q1175 ,-NHS (O ₂)-Q1176 ,-NQ1177S (O ₂)-Q1178 ,-S-Q1179 ,-S (O)-Q1180 ,-S (O ₂)-Q1181 ,-S (O ₂) NH-Q1182 ,-S (O ₂) NQ1183Q1184 ,-S (O ₂) O-Q1185 ,-P (O) is (OQ1187) (OQ1186), and-Si (Q1188) is (Q1190) (Q1189) ";

Q1139 wherein, Q1140, Q1141, Q1142, Q1143, Q1144, Q1145, Q1146, Q1147, Q1148, Q1149; Q1150, Q1151, Q1152, Q1153, Q1154, Q1155, Q1156, Q1157, Q1158, Q1159, Q1160; Q1161, Q1162, Q1163, Q1164, Q1165, Q1166, Q1167, Q1168, Q1169, Q1170, Q1171; Q1172, Q1173, Q1174, Q1175, Q1176, Q1177, Q1178, Q1179, Q1180, Q1181; Q1182, Q1183, Q1184, Q1185, Q1186, Q1187, Q1188, Q1189, Q1190 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, Q1145, Q1146 and/or Q1154; Q1155 and/or Q1167, Q1168 and/or Q1174, Q1175 and/or Q1183, Q1184 also can form " heterocyclic radical " in each case together;

(iii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHQ1191 ,-NQ1192Q1193 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-Q1194 ,-C (O) O-Q1195 ,-C (O) NH-Q1196 ,-C (O) NQ1197Q1198 ,-O-Q1199 ,-O are (Q1200-O) _n-H (n=1,2,3,4,5) ,-O (Q1201-O) _n-Q1202 (n=1,2,3,4,5) ,-OC (O)-Q1203 ,-OC (O)-O-Q1204 ,-OC (O)-NHQ1205 ,-O-C (O)-NQ1206Q1207 ,-OP (O) is (OQ1209) (OQ1208), and-OSi (Q1210) is (Q1212) (Q1211) ,-OS (O ₂)-Q1213 ,-NHC (O)-Q1214 ,-NQ1215C (O)-Q1216 ,-NH-C (O)-O-Q1217;-NH-C (O)-NH-Q1218 ,-NH-C (O)-NQ1219Q1220 ,-NQ1221-C (O)-O-Q1222;-NQ1223-C (O)-NH-Q1224 ,-NQ1225-C (O)-NQ1226Q1227 ,-NHS (O ₂)-Q1228 ,-NQ1229S (O ₂)-Q1230 ,-S-Q1231 ,-S (O)-Q1232 ,-S (O ₂)-Q1233 ,-S (O ₂) NH-Q1234 ,-S (O ₂) NQ1235Q1236 ,-S (O ₂) O-Q1237 ,-P (O) is (OQ1239) (OQ1238), and-Si (Q1240) is (Q1242) (Q1241) ";

Q1191 wherein, Q1192, Q1193, Q1194, Q1195, Q1196, Q1197, Q1198, Q1199, Q1200, Q1201; Q1202, Q1203, Q1204, Q1205, Q1206, Q1207, Q1208, Q1209, Q1210, Q1211, Q1212; Q1213, Q1214, Q1215, Q1216, Q1217, Q1218, Q1219, Q1220, Q1221, Q1222, Q1223; Q1224, Q1225, Q1226, Q1227, Q1228, Q1229, Q1230, Q1231, Q1232, Q1233; Q1234, Q1235, Q1236, Q1237, Q1238, Q1239, Q1240, Q1241, Q1242 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, Q1197, Q1198 and/or Q1206; Q1207 and/or Q1219, Q1220 and/or Q1226, Q1227 and/or Q1235, Q1236 also can form " heterocyclic radical " in each case together;

And

Z1, Z2 group are selected from independently of one another: " hydrogen, NZ14Z15 ";

Condition is, when Z1=H, and Z2=NZ14Z15, and when Z1=NZ14Z15, Z2=H;

Wherein Z14, Z15 are selected from independently of one another:

(a) " hydrogen, alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, the heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl ,-C (Y1) NZ16Z17 ,-C (=NZ18)-and Z19 ,-C (Y2) NZ20-Y3-Z21 ";

Condition is that Z14, Z15 are not hydrogen or " alkyl, (C simultaneously ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl ";

Other condition is, when one of Z14, Z15 group are hydrogen or " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " time, other Z14, Z15 group be in each case " C (Y1) NZ16Z17 ", " C (=NZ18)-Z19 " or " C (Y2) NZ20-Y3-Z21 ";

Y1 wherein, Y2, Y3 are selected from " O, S ,=NH ,=NZ22 " independently of one another;

Z16 wherein, Z17, Z18, Z19, Z20, Z21, Z22 is selected from independently of one another:

(1) hydrogen

(2) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, heterocyclic radical, heterocyclic radical alkyl ";

Wherein the above-mentioned substituting group of substituting group group (a) and/or substituting group group (2) can randomly be selected from following substituting group replacement by at least one independently of one another identically or differently:

(i) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHU1 ,-NU2U3 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-U4 ,-C (O) O-U5 ,-C (O) NH-U6 ,-C (O) NU7U8 ,-O-U9 ,-O are (U10-O) _r-H (r=1,2,3,4,5) ,-O (U11-O) _r-U12 (r=1,2,3,4,5) ,-OC (O)-U13 ,-OC (O)-O-U14 ,-OC (O)-NHU15 ,-O-C (O)-NU16U17 ,-OP (O) is (OU19) (OU18), and-OSi (U20) is (U22) (U21) ,-OS (O ₂)-U23 ,-NHC (O)-U24 ,-NU25C (O)-U26 ,-NH-C (O)-O-U27 ,-NH-C (O)-NH-U28 ,-NH-C (O)-NU29U30 ,-NU31-C (O)-O-U32 ,-NU33-C (O)-NH-U34 ,-NU35-C (O)-NU36U37 ,-NHS (O ₂)-U38 ,-NU39S (O ₂)-U40 ,-S-U41 ,-S (O)-U42 ,-S (O ₂)-U43 ,-S (O ₂) NH-U44 ,-S (O ₂) NU45U46 ,-S (O ₂) O-U47 ,-P (O) is (OU49) (OU48), and-Si (U50) is (U52) (U51) ";

U1 wherein, U2, U3, U4, U5, U6, U7, U8, U9, U10, U11, U12, U13, U14; U15, U16, U17, U18, U19, U20, U21, U22, U23, U24, U25, U26, U27; U28, U29, U30, U31, U32, U33, U34, U35, U36, U37, U38, U39, U40; U41, U42, U43, U44, U45, U46, U47, U48, U49, U50, U51, U52 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl; Arylalkyl, heteroaryl, heteroarylalkyl " and wherein, perhaps, U7; U8 and/or U16, U17 and/or U29, U30 and/or U36, U37 and/or U45, U46 also can form " heterocyclic radical " in each case together;

(ii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHU53 ,-NU54U55 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ₂-P (O) (OH) ₂,-C (O)-U56 ,-C (O) O-U57 ,-C (O) NH-U58 ,-C (O) NU59U60 ,-O-U61 ,-O are (U62-O) _r-H (r=1,2,3,4,5) ,-O (U63-O) _r-U64 (r=1,2,3,4,5) ,-OC (O)-U65 ,-OC (O)-O-U66 ,-OC (O)-NHU67 ,-O-C (O)-NU68U69 ,-OP (O) is (OU71) (OU70), and-OSi (U72) is (U74) (U73) ,-OS (O ₂)-U75 ,-NHC (O)-U76 ,-NU77C (O)-U78 ,-NH-C (O)-O-U79 ,-NH-C (O)-NH-U80 ,-NH-C (O)-NU81U82 ,-NU83-C (O)-O-U84 ,-NU85-C (O)-NH-U86 ,-NU87-C (O)-NU88U89 ,-NHS (O ₂)-U90 ,-NU91S (O ₂)-U92 ,-S-U93 ,-S (O)-U94 ,-S (O ₂)-U95 ,-S (O ₂) NH-U96 ,-S (O ₂) NU97U98 ,-S (O ₂) O-U99 ,-P (O) (OU 100) (OU101) ,-Si (U102) is (U104) (U103) ";

U53 wherein, U54, U55, U56, U57, U58, U59, U60, U61, U62, U63, U64, U65, U66; U67, U68, U69, U70, U71, U72, U73, U74, U75, U76, U77, U78, U79; U80, U81, U82, U83, U84, U85, U86, U87, U88, U89, U90, U91, U92; U93, U94, U95, U96, U97, U98, U99, U100, U101, U102, U103, U104 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, U59, U60 and/or U68; U69 and/or U81, U82 and/or U88, U89 and/or U97, U98 also can form " heterocyclic radical " in each case together;

(iii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHU105 ,-NU106U107 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-U108 ,-C (O) O-U109 ,-C (O) NH-U110 ,-C (O) NU111U112 ,-O-U113 ,-O are (U114-O) _s-H (s=1,2,3,4,5) ,-O (U115-O) _s-U116 (s=1,2,3,4,5) ,-OC (O)-U117 ,-OC (O)-O-U118 ,-OC (O)-NHU119 ,-O-C (O)-NU120U121 ,-OP (O) is (OU123) (OU122), and-OSi (U124) is (U126) (U125) ,-OS (O ₂)-U127 ,-NHC (O)-U128 ,-NU129C (O)-U130 ,-NH-C (O)-O-U131 ,-NH-C (O)-NH-U132 ,-NH-C (O)-NU133U134 ,-NU135-C (O)-O-U136 ,-NU137-C (O)-NH-U138 ,-NU139-C (O)-NU140U141 ,-NHS (O ₂)-U142 ,-NU143S (O ₂)-U144 ,-S-U145 ,-S (O)-U146 ,-S (O ₂)-U147 ,-S (O ₂) NH-U148 ,-S (O ₂) NU149U150 ,-S (O ₂) O-U151 ,-P (O) is (OU153) (OU152), and-Si (U154) is (U156) (U155) ";

U105 wherein, U106, U107, U108, U109, U110, U111, U112, U113, U114, U115, U116, U117, U118; U119, U120, U121, U122, U123, U124, U125, U126, U127, U128, U129, U130, U131; U132, U133, U134, U135, U136, U137, U138, U139, U140, U141, U142, U143, U144; U145, U146, U147, U148, U149, U150, U151, U152, U153, U154, U155, U156 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, U111, U112 and/or U120; U121 and/or U133, U134 and/or U140, U141 and/or U149, U150 also can form " heterocyclic radical " in each case together;

(3)-and C (O)-Z23, wherein Z23 is independently selected from:

(a) " hydrogen, alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl ";

Wherein the above-mentioned substituting group of substituting group group (a) can randomly be selected from following substituting group replacement by at least one independently of one another identically or differently:

(i) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHU157 ,-NU158U159 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-U160 ,-C (O) O-U161 ,-C (O) NH-U162 ,-C (O) NU163U164 ,-O-U165 ,-O are (U166-O) _t-H (t=1,2,3,4,5) ,-O (U167-O) _t-U168 (t=1,2,3,4,5) ,-OC (O)-U169 ,-OC (O)-O-U170 ,-OC (O)-NHU171 ,-O-C (O)-NU172U173 ,-OP (O) is (OU175) (OU174), and-OSi (U176) is (U178) (U177) ,-OS (O ₂)-U179 ,-NHC (O)-U180 ,-NU181C (O)-U182 ,-NH-C (O)-O-U183 ,-NH-C (O)-NH-U184 ,-NH-C (O)-NU185U186 ,-NU187-C (O)-O-U188 ,-NU189-C (O)-NH-U190 ,-NU191-C (O)-NU192U193 ,-NHS (O ₂)-U194 ,-NU195S (O ₂)-U196 ,-S-U197 ,-S (O)-U198 ,-S (O ₂)-U199 ,-S (O ₂) NH-U200 ,-S (O ₂) NU201U202 ,-S (O ₂) O-U203 ,-P (O) is (OU205) (OU204), and-Si (U206) is (U208) (U207) ";

U157 wherein, U158, U159, U160, U161, U162, U163, U164, U165, U166, U167, U168, U169, U170; U171, U172, U173, U174, U175, U176, U177, U178, U179, U180, U181, U182, U183; U184, U185, U186, U187, U188, U189, U190, U191, U192, U193, U194, U195, U196; U197, U198, U199, U200, U201, U202, U203, U204, U205, U206, U207, U208 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, U163, U164 and/or U172; U173 and/or U185, U186 and/or U192, U193 and/or U201, U202 also can form " heterocyclic radical " in each case together;

(ii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHU209 ,-NU210U211 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-U212 ,-C (O) O-U213 ,-C (O) NH-U214 ,-C (O) NU215U216 ,-O-U217 ,-O are (U218-O) _u-H (u=1,2,3,4,5) ,-O (U219-O) _u-U220 (u=1,2,3,4,5) ,-OC (O)-U221 ,-OC (O)-O-U222 ,-OC (O)-NHU223 ,-O-C (O)-NU224U225 ,-OP (O) is (OU227) (OU226), and-OSi (U228) is (U230) (U229) ,-OS (O ₂)-U231 ,-NHC (O)-U232 ,-NU233C (O)-U234 ,-NH-C (O)-O-U235 ,-NH-C (O)-NH-U236 ,-NH-C (O)-NU237U238 ,-NU239-C (O)-O-U240 ,-NU241-C (O)-NH-U242 ,-NU243-C (O)-NU244U245 ,-NHS (O ₂)-U246 ,-NU247S (O ₂)-U248 ,-S-U249 ,-S (O)-U250 ,-S (O ₂)-U251 ,-S (O ₂) NH-U252 ,-S (O ₂) NU253U254 ,-S (O ₂) O-U255 ,-P (O) is (OU257) (OU256), and-Si (U258) is (U260) (U259) ";

U209 wherein, U210, U211, U212, U213, U214, U215, U216, U217, U218, U219, U220, U221, U222; U223, U224, U225, U226, U227, U228, U229, U230, U231, U232, U233, U234, U235; U236, U237, U238, U239, U240, U241, U242, U243, U244, U245, U246, U247, U248; U249, U250, U251, U252, U253, U254, U255, U256, U257, U258, U259, U260 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, U215, U216 and/or U224; U225 and/or U237, U238 and/or U244, U245 and/or U253, U254 also can form " heterocyclic radical " in each case together;

(iii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHU261 ,-NU262U263 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-U264 ,-C (O) O-U265 ,-C (O) NH-U266 ,-C (O) NU267U268 ,-O-U269 ,-O are (U270-O) _v-H (v=1,2,3,4,5) ,-O (U271-O) _v-U272 (v=1,2,3,4,5) ,-OC (O)-U273 ,-OC (O)-O-U274 ,-OC (O)-NHU275 ,-O-C (O)-NU276U277 ,-OP (O) is (OU279) (OU278), and-OSi (U280) is (U282) (U281) ,-OS (O ₂)-U283 ,-NHC (O)-U284 ,-NU285C (O)-U286 ,-NH-C (O)-O-U287 ,-NH-C (O)-NH-U288 ,-NH-C (O)-NU289U290 ,-NU291-C (O)-O-U292 ,-NU293-C (O)-NH-U294 ,-NU295-C (O)-NU296U297 ,-NHS (O ₂)-U298 ,-NU299S (O ₂)-U300 ,-S-U301 ,-S (O)-U302 ,-S (O ₂)-U303 ,-S (O ₂) NH-U304 ,-S (O ₂) NU305U306 ,-S (O ₂) O-U307 ,-P (O) is (OU309) (OU308), and-Si (U310) is (U312) (U311) ";

U261 wherein, U262, U263, U264, U265, U266, U267, U268, U269, U270, U271, U272, U273, U274; U275, U276, U277, U278, U279, U280, U281, U282, U283, U284, U285, U286, U287; U288, U289, U290, U291, U292, U293, U294, U295, U296, U297, U298, U299, U300; U301, U302, U303, U304, U305, U306, U307, U308, U309, U310, U311, U312 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, U267, U268 and/or U276; U277 and/or U289, U290 and/or U296, U297 and/or U305, U306 also can form " heterocyclic radical " in each case together;

(4) Z16, Z17 can independently, randomly also form " heterocyclic radical " together;

(5)“-C(O)-C(O)-U313，-S(O ₂)-NU314U315”；

U313 wherein, U314, U315 is selected from independently of one another:

(I) " hydrogen, alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHU316 ,-NU317U318 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-U319 ,-C (O) O-U320 ,-C (O) NH-U321 ,-C (O) NU322U323 ,-O-U324 ,-O are (U325-O) _w-H (w=1,2,3,4,5) ,-O (U326-O) _w-U327 (w=1,2,3,4,5) ,-OC (O)-U328 ,-OC (O)-O-U329 ,-OC (O)-NHU330 ,-O-C (O)-NU331U332 ,-OP (O) is (OU334) (OU333), and-OSi (U335) is (U337) (U336) ,-OS (O ₂)-U338 ,-NHC (O)-U339 ,-NU340C (O)-U341 ,-NH-C (O)-O-U342 ,-NH-C (O)-NH-U343 ,-NH-C (O)-NU344U345 ,-NU346-C (O)-O-U347 ,-NU348-C (O)-NH-U349 ,-NU350-C (O)-NU351U352 ,-NHS (O ₂)-U353 ,-NU354S (O ₂)-U355 ,-S-U356 ,-S (O)-U357 ,-S (O ₂)-U358 ,-S (O ₂) NH-U359 ,-S (O ₂) NU360U361 ,-S (O ₂) O-U362 ,-P (O) is (OU364) (OU363), and-Si (U365) is (U367) (U366) ";

U316 wherein, U317, U318, U319, U320, U321, U322, U323, U324, U325, U326, U327, U328, U329; U330, U331, U332, U333, U334, U335, U336, U337, U338, U339, U340, U341, U342; U343, U344, U345, U346, U347, U348, U349, U350, U351, U352, U353, U354, U355; U356, U357, U358, U359, U360, U361, U362, U363, U364, U365, U366, U367 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, U322, U323 and/or U331; U332 and/or U344, U345 and/or U351, U352 and/or U360, U361 also can form " heterocyclic radical " in each case together;

Wherein randomly, the above-mentioned substituting group of substituting group group (I) can be independently of one another by at least one identical ground or different are selected from following substituting group and further replace:

(i) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHU368 ,-NU369U370 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-U371 ,-C (O) O-U372 ,-C (O) NH-U373 ,-C (O) NU374U375 ,-O-U376 ,-O are (U377-O) _x-H (x=1,2,3,4,5) ,-O (U378-O) _x-U379 (x=1,2,3,4,5) ,-OC (O)-U380 ,-OC (O)-O-U381 ,-OC (O)-NHU382 ,-O-C (O)-NU383U384 ,-OP (O) is (OU386) (OU385), and-OSi (U387) is (U389) (U388) ,-OS (O ₂)-U390 ,-NHC (O)-U391 ,-NU392C (O)-U393 ,-NH-C (O)-O-U394 ,-NH-C (O)-NH-U395 ,-NH-C (O)-NU396U397 ,-NU398-C (O)-O-U399 ,-NU400-C (O)-NH-U401 ,-NU402-C (O)-NU403U404 ,-NHS (O ₂)-U405 ,-NU406S (O ₂)-U407 ,-S-U408 ,-S (O)-U409 ,-S (O ₂)-U410 ,-S (O ₂) NH-U411 ,-S (O ₂) NU412U413 ,-S (O ₂) O-U414 ,-P (O) is (OU416) (OU415), and-Si (U417) is (U419) (U418) ";

U368 wherein, U369, U370, U371, U372, U373, U374, U375, U376, U377, U378, U379, U380, U381; U382, U383, U384, U385, U386, U387, U388, U389, U390, U391, U392, U393, U394; U395, U396, U397, U398, U399, U400, U401, U402, U403, U404, U405, U406, U407; U408, U409, U410, U411, U412, U413, U414, U415, U416, U417, U418, U419 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, U374, U375 and/or U383; U384 and/or U396, U397 and/or U403, U404 and/or U412, U413 also can form " heterocyclic radical " in each case together;

(ii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHU420 ,-NU421U422 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-U423 ,-C (O) O-U424 ,-C (O) NH-U425 ,-C (O) NU426U427 ,-O-U428 ,-O are (U429-O) _y-H (y=1,2,3,4,5) ,-O (U430-O) _y-U431 (y=1,2,3,4,5) ,-OC (O)-U432 ,-OC (O)-O-U433 ,-OC (O)-NHU434 ,-O-C (O)-NU435U436 ,-OP (O) is (OU438) (OU437), and-OSi (U439) is (U441) (U440) ,-OS (O ₂)-U442 ,-NHC (O)-U443 ,-NU444C (O)-U445 ,-NH-C (O)-O-U446 ,-NH-C (O)-NH-U447 ,-NH-C (O)-NU448U449 ,-NU450-C (O)-O-U451 ,-NU452-C (O)-NH-U453 ,-NU454-C (O)-NU455U456 ,-NHS (O ₂)-U457 ,-NU458S (O ₂)-U459 ,-S-U460 ,-S (O)-U461 ,-S (O ₂)-U462 ,-S (O ₂) NH-U463 ,-S (O ₂) NU464U465 ,-S (O ₂) O-U466 ,-P (O) is (OU468) (OU467), and-Si (U469) is (U471) (U470) ";

U420 wherein, U421, U422, U423, U424, U425, U426, U427, U428, U429, U430, U431, U432, U433; U434, U435, U436, U437, U438, U439, U440, U441, U442, U443, U444, U445, U446; U447, U448, U449, U450, U451, U452, U453, U454, U455, U456, U457, U458, U459; U460, U461, U462, U463, U464, U465, U466, U467, U468, U469, U470, U471 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, U426, U427 and/or U435; U436 and/or U448, U449 and/or U455, U456 and/or U464, U465 also can form " heterocyclic radical " in each case together;

(iii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHU472 ,-NU473U474 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-U475 ,-C (O) O-U476 ,-C (O) NH-U477 ,-C (O) NU478U479 ,-O-U480 ,-O are (U481-O) _z-H (z=1,2,3,4,5) ,-O (U482-O) _z-U483 (z=1,2,3,4,5) ,-OC (O)-U484 ,-OC (O)-O-U485 ,-OC (O)-NHU486 ,-O-C (O)-NU487U488 ,-OP (O) is (OU490) (OU489), and-OSi (U491) is (U493) (U492) ,-OS (O ₂)-U494 ,-NHC (O)-U495 ,-NU496C (O)-U497 ,-NH-C (O)-O-U498 ,-NH-C (O)-NH-U499 ,-NH-C (O)-NU500U501 ,-NU502-C (O)-O-U503 ,-NU504-C (O)-NH-U505 ,-NU506-C (O)-NU507U508 ,-NHS (O ₂)-U509 ,-NU510S (O ₂)-U511 ,-S-U512 ,-S (O)-U513 ,-S (O ₂)-U514 ,-S (O ₂) NH-U515 ,-S (O ₂) NU516U517 ,-S (O ₂) O-U518 ,-P (O) is (OU520) (OU519), and-Si (U521) is (U523) (U522) ";

U472 wherein, U473, U474, U475, U476, U477, U478, U479, U480, U481, U482, U483, U484, U485; U486, U487, U488, U489, U490, U491, U492, U493, U494, U495, U496, U497, U498; U499, U500, U501, U502, U503, U504, U505, U506, U507, U508, U509, U510, U511; U512, U513, U514, U515, U516, U517, U518, U519, U520, U521, U522, U523 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, U478, U479 and/or U487; U488 and/or U500, U501 and/or U507, U508 and/or U516, U517 also can form " heterocyclic radical " in each case together;

And wherein, perhaps, U314, U315 also can form " heterocyclic radical " together;

And

Said Z5 group is independently selected from:

(i) " hydrogen, alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHA1 ,-NA2A3 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-A4 ,-C (O) O-A5 ,-C (O) NH-A6 ,-C (O) NA7A8 ,-O-A9 ,-O are (A10-O) _r-H (r=1,2,3,4,5) ,-O (A11-O) _r-A12 (r=1,2,3,4,5) ,-OC (O)-A13 ,-OC (O)-O-A14 ,-OC (O)-NHA15 ,-O-C (O)-NA16A17 ,-OP (O) is (OA19) (OA18), and-OSi (A20) is (A22) (A21) ,-OS (O ₂)-A23 ,-NHC (O)-A24 ,-NA25C (O)-A26 ,-NH-C (O)-O-A27 ,-NH-C (O)-NH-A28 ,-NH-C (O)-NA29A30 ,-NA31-C (O)-O-A32 ,-NA33-C (O)-NH-A34 ,-NA35-C (O)-NA36A37 ,-NHS (O ₂)-A38 ,-NA39S (O ₂)-A40 ,-S-A41 ,-S (O)-A42 ,-S (O ₂)-A43 ,-S (O ₂) NH-A44 ,-S (O ₂) NA45A46 ,-S (O ₂) O-A47 ,-P (O) is (OA49) (OA48), and-Si (A50) is (A52) (A51) ";

A1 wherein, A2, A3, A4, A5, A6, A7, A8, A9, A10, A11, A12, A13, A14; A15, A16, A17, A18, A19, A20, A21, A22, A23, A24, A25, A26, A27; A28, A29, A30, A31, A32, A33, A34, A35, A36, A37, A38, A39, A40; A41, A42, A43, A44, A45, A46, A47, A48, A49, A50, A51, A52 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl; Arylalkyl, heteroaryl, heteroarylalkyl " and wherein, perhaps, A7; A8 and/or A16, A17 and/or A29, A30 and/or A36, A37 and/or A45, A46 also can form " heterocyclic radical " in each case together;

(ii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHA53 ,-NA54A55 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-A56 ,-C (O) O-A57 ,-C (O) NH-A58 ,-C (O) NA59A60 ,-O-A61 ,-O are (A62-O) _s-H (s=1,2,3,4,5) ,-O (A63-O) _t-A64 (t=1,2,3,4,5) ,-OC (O)-A65 ,-OC (O)-O-A66 ,-OC (O)-NHA67 ,-O-C (O)-NA68A69 ,-OP (O) is (OA71) (OA70), and-OSi (A72) is (A74) (A73) ,-OS (O ₂)-A75 ,-NHC (O)-A76 ,-NA77C (O)-A78 ,-NH-C (O)-O-A79 ,-NH-C (O)-NH-A80 ,-NH-C (O)-NA81A82 ,-NA83-C (O)-O-A84 ,-NA85-C (O)-NH-A86 ,-NA87-C (O)-NA88A89 ,-NHS (O ₂)-A90 ,-NA91S (O ₂)-A92 ,-S-A93 ,-S (O)-A94 ,-S (O ₂)-A95 ,-S (O ₂) NH-A96 ,-S (O ₂) NA97A98 ,-S (O ₂) O-A99 ,-P (O) is (OA101) (OA100), and-Si (A102) is (A104) (A103) ";

A53 wherein, A54, A55, A56, A57, A58, A59, A60, A61, A62, A63, A64, A65, A66; A67, A68, A69, A70, A71, A72, A73, A74, A75, A76, A77, A78, A79; A80, A81, A82, A83, A84, A85, A86, A87, A88, A89, A90, A91, A92; A93, A94, A95, A96, A97, A98, A99, A100, A101, A102, A103, A104 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, A59, A60 and/or A68; A69 and/or A81, A82 and/or A88, A89 and/or A97, A98 also can form " heterocyclic radical " in each case together;

(iii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHA105 ,-NA106A107 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-A108 ,-C (O) O-A109 ,-C (O) NH-A110 ,-C (O) NA111A112 ,-O-A113 ,-O are (A114-O) _t-H (t=1,2,3,4,5) ,-O (A115-O) _t-A116 (t=1,2,3,4,5) ,-OC (O)-A117 ,-OC (O)-O-A118 ,-OC (O)-NHA119 ,-O-C (O)-NA120A121 ,-OP (O) is (OA123) (OA122), and-OSi (A124) is (A126) (A125) ,-OS (O ₂)-A127 ,-NHC (O)-A128 ,-NA129C (O)-A130 ,-NH-C (O)-O-A131 ,-NH-C (O)-NH-A132 ,-NH-C (O)-NA133A134 ,-NA135-C (O)-O-A136 ,-NA137-C (O)-NH-A138 ,-NA139-C (O)-NA140A141 ,-NHS (O ₂)-A142 ,-NA143S (O ₂)-A144 ,-S-A145 ,-S (O)-A146 ,-S (O ₂)-A147 ,-S (O ₂) NH-A148 ,-S (O ₂) NA149A150 ,-S (O ₂) O-A151 ,-P (O) is (OA153) (OA152), and-Si (A154) is (A156) (A155) ";

A105 wherein, A106, A107, A108, A109, A110, A111, A112, A113, A114, A115, A116, A117, A118; A119, A120, A121, A122, A123, A124, A125, A126, A127, A128, A129, A130, A131; A132, A133, A134, A135, A136, A137, A138, A139, A140, A141, A142, A143, A144; A145, A146, A147, A148, A149, A150, A151, A152, A153, A154, A155, A156 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, A111, A112 and/or A120; A121 and/or A133, A134 and/or A140, A141 and/or A149, A150 also can form " heterocyclic radical " in each case together;

Or

(E) one of Z1, Z2 group or Z1, Z2 group the two be selected from independently of one another:

(a)-NZ24Z25；

Condition is, the two is selected from one of Z24, Z25 group or Z24, Z25 group independently of one another:

(1)“-C(O)-C(O)-T1，-S(O ₂)-NT2T3”；

T1 wherein, T2, T3 is selected from independently of one another:

(I) " hydrogen, alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHT4 ,-NT5T6 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-T7 ,-C (O) O-T8 ,-C (O) NH-T9 ,-C (O) NT10T11 ,-O-T12 ,-O are (T13-O) _p-H (p=1,2,3,4,5) ,-O (T14-O) _p-T15 (p=1,2,3,4,5) ,-OC (O)-T16 ,-OC (O)-O-T17 ,-OC (O)-NHT18 ,-O-C (O)-NT19T20 ,-OP (O) is (OT22) (OT21), and-OSi (T23) is (T25) (T24) ,-OS (O ₂)-T26 ,-NHC (O)-T27 ,-NT28C (O)-T29 ,-NH-C (O)-O-T30 ,-NH-C (O)-NH-T31 ,-NH-C (O)-NT32T33 ,-NT34-C (O)-O-T35 ,-NT36-C (O)-NH-T37 ,-NT38-C (O)-NT39T40 ,-NHS (O ₂)-T41 ,-NT42S (O ₂)-T43 ,-S-T44 ,-S (O)-T45 ,-S (O ₂)-T46 ,-S (O ₂) NH-T47 ,-S (O ₂) NT48T49 ,-S (O ₂) O-T50 ,-P (O) is (OT52) (OT51), and-Si (T53) is (T55) (T54) ";

T4 wherein, T5, T6, T7, T8, T9, T10, T11, T12, T13, T14, T15, T16, T17; T18, T19, T20, T21, T22, T23, T24, T25, T26, T27, T28, T29, T30; T31, T32, T33, T34, T35, T36, T37, T38, T39, T40, T41, T42, T43; T44, T45, T46, T47, T48, T49, T50, T51, T52, T53, T54, T55 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl; Arylalkyl, heteroaryl, heteroarylalkyl " and wherein, perhaps, T10; T1 and/or T19, T20 and/or T32, T33 and/or T39, T40 and/or T48, T49 also can form " heterocyclic radical " in each case together;

(i) alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHT56 ,-NT57T58 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-T59 ,-C (O) O-T60 ,-C (O) NH-T61 ,-C (O) NT62T63 ,-O-T64 ,-O are (T65-O) _r-H (r=1,2,3,4,5) ,-O (T66-O) _r-T67 (r=1,2,3,4,5) ,-OC (O)-T68 ,-OC (O)-O-T69 ,-OC (O)-NHT70 ,-O-C (O)-NT71T72 ,-OP (O) is (OT74) (OT73), and-OSi (T75) is (T77) (T76) ,-OS (O ₂)-T78 ,-NHC (O)-T79 ,-NT80C (O)-T81 ,-NH-C (O)-O-T82 ,-NH-C (O)-NH-T83 ,-NH-C (O)-NT84T85 ,-NT86-C (O)-O-T87 ,-NT88-C (O)-NH-T89 ,-NT90-C (O)-NT91T92 ,-NHS (O ₂)-T93 ,-NT94S (O ₂)-T95 ,-S-T96 ,-S (O)-T97 ,-S (O ₂)-T98 ,-S (O ₂) NH-T99 ,-S (O ₂) NT100T101 ,-S (O ₂) O-T102 ,-P (O) is (OT104) (OT103), and-Si (T105) is (T107) (T106) ";

T56 wherein, T57, T58, T59, T60, T61, T62, T63, T64, T65, T66, T67, T68, T69; T70, T71, T72, T73, T74, T75, T76, T77, T78, T79, T80, T81, T82; T83, T84, T85, T86, T87, T88, T89, T90, T91, T92, T93, T94, T95; T96, T97, T98, T99, T100, T101, T102, T103, T104, T105, T106, T107 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, T62, T63 and/or T71; T72 and/or T84, T85 and/or T91, T92 and/or T100, T101 also can form " heterocyclic radical " in each case together;

(ii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHT108 ,-NT109T110 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-T111 ,-C (O) O-T112 ,-C (O) NH-T113 ,-C (O) NT114T115 ,-O-T116 ,-O are (T117-O) _s-H (s=1,2,3,4,5) ,-O (T118-O) _s-T119 (s=1,2,3,4,5) ,-OC (O)-T120 ,-OC (O)-O-T121 ,-OC (O)-NHT122 ,-O-C (O)-NT123T124 ,-OP (O) is (OT126) (OT125), and-OSi (T127) is (T129) (T128) ,-OS (O ₂)-T130 ,-NHC (O)-T131 ,-NT132C (O)-T133 ,-NH-C (O)-O-T134 ,-NH-C (O)-NH-T135 ,-NH-C (O)-NT136T137 ,-NT138-C (O)-O-T139 ,-NT140-C (O)-NH-T141 ,-NT142-C (O)-NT143T144 ,-NHS (O ₂)-T145 ,-NT146S (O ₂)-T147 ,-S-T148 ,-S (O)-T149 ,-S (O ₂)-T150 ,-S (O ₂) NH-T151 ,-S (O ₂) NT152T153 ,-S (O ₂) O-T154 ,-P (O) is (OT156) (OT155), and-Si (T157) is (T159) (T158) ";

T108 wherein, T109, T110, T111, T112, T113, T114, T115, T116, T117, T118, T119, T120, T121; T122, T123, T124, T125, T126, T127, T128, T129, T130, T131, T132, T133, T134; T135, T136, T137, T138, T139, T140, T141, T142, T143, T144, T145, T146, T147; T148, T149, T150, T151, T152, T153, T154, T155, T156, T157, T158, T159 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, T114, T115 and/or T123; T124 and/or T136, T137 and/or T143, T144 and/or T152, T153 also can form " heterocyclic radical " in each case together;

(iii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHT160 ,-NT161T162 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-T163 ,-C (O) O-T164 ,-C (O) NH-T165 ,-C (O) NT166T167 ,-O-T168 ,-O are (T169-O) _t-H (t=1,2,3,4,5) ,-O (T170-O) _t-T171 (t=1,2,3,4,5) ,-OC (O)-T172 ,-OC (O)-O-T173 ,-OC (O)-NHT174 ,-O-C (O)-NT175T176 ,-OP (O) is (OT178) (OT177), and-OSi (T179) is (T181) (T180) ,-OS (O ₂)-T182 ,-NHC (O)-T183 ,-NT184C (O)-T185 ,-NH-C (O)-O-T186 ,-NH-C (O)-NH-T187 ,-NH-C (O)-NT188T189 ,-NT190-C (O)-O-T191 ,-NT192-C (O)-NH-T193 ,-NT194-C (O)-NT195T196 ,-NHS (O ₂)-T197 ,-NT198S (O ₂)-T199 ,-S-T200 ,-S (O)-T201 ,-S (O ₂)-T202 ,-S (O ₂) NH-T203 ,-S (O ₂) NT204T205 ,-S (O ₂) O-T206 ,-P (O) is (OT208) (OT207), and-Si (T209) is (T211) (T210) ";

T160 wherein, T161, T162, T163, T164, T165, T166, T167, T168, T169, T170, T171, T172, T173; T174, T175, T176, T177, T178, T179, T180, T181, T182, T183, T184, T185, T186; T187, T188, T189, T190, T191, T192, T193, T194, T195, T196, T197, T198, T199; T200, T201, T202, T203, T204, T205, T206, T207, T208, T209, T210, T211 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, T166, T167 and/or T175; T176 and/or T188, T189 and/or T195, T196 and/or T204, T205 also can form " heterocyclic radical " in each case together;

Wherein, perhaps, T2, T3 also can form " heterocyclic radical " together;

AndOne of Z24, Z25 group or Z24, Z25 group none are independently selected from:

(2) " hydrogen, alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl ";

Wherein randomly, the above-mentioned substituting group of substituting group group (2) can be independently of one another by at least one identical ground or different are selected from following substituting group and further replace:

(i) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHT212 ,-NT213T214 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-T215 ,-C (O) O-T216 ,-C (O) NH-T217 ,-C (O) NT218T219 ,-O-T220 ,-O are (T221-O) _u-H (u=1,2,3,4,5) ,-O (T222-O) _u-T223 (u=1,2,3,4,5) ,-OC (O)-T224 ,-OC (O)-O-T225 ,-OC (O)-NHT226 ,-O-C (O)-NT227T228 ,-OP (O) is (OT230) (OT229), and-OSi (T231) is (T233) (T232) ,-OS (O ₂)-T234 ,-NHC (O)-T235 ,-NT236C (O)-T237 ,-NH-C (O)-O-T238 ,-NH-C (O)-NH-T239 ,-NH-C (O)-NT240T241 ,-NT242-C (O)-O-T243 ,-NT244-C (O)-NH-T245 ,-NT246-C (O)-NT247T248 ,-NHS (O ₂)-T249 ,-NT250S (O ₂)-T251 ,-S-T252 ,-S (O)-T253 ,-S (O ₂)-T254 ,-S (O ₂) NH-T255 ,-S (O ₂) NT256T257 ,-S (O ₂) O-T258 ,-P (O) is (OT260) (OT259), and-Si (T261) is (T263) (T262) ";

T212 wherein, T213, T214, T215, T216, T217, T218, T219, T220, T221, T222, T223, T224, T225; T226, T227, T228, T229, T230, T231, T232, T233, T234, T235, T236, T237, T238; T239, T240, T241, T242, T234, T244, T245, T246, T247, T248, T249, T250, T251; T252, T253, T254, T255, T256, T257, T258, T259, T260, T261, T262, T263 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, T218, T219 and/or T227; T228 and/or T240, T241 and/or T247, T248 and/or T256, T257 also can form " heterocyclic radical " in each case together;

(ii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHT264 ,-NT265T266 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-T267 ,-C (O) O-T268 ,-C (O) NH-T269 ,-C (O) NT270T271 ,-O-T272 ,-O are (T273-O) _v-H (v=1,2,3,4,5) ,-O (T274-O) _v-T275 (v=1,2,3,4,5) ,-OC (O)-T276 ,-OC (O)-O-T277 ,-OC (O)-NHT278 ,-O-C (O)-NT279T280 ,-OP (O) is (OT282) (OT281), and-OSi (T283) is (T285) (T284) ,-OS (O ₂)-T286 ,-NHC (O)-T287 ,-NT288C (O)-T289 ,-NH-C (O)-O-T290 ,-NH-C (O)-NH-T291 ,-NH-C (O)-NT292T293 ,-NT294-C (O)-O-T295 ,-NT296-C (O)-NH-T297 ,-NT298-C (O)-NT299T300 ,-NHS (O ₂)-T301 ,-NT302S (O ₂)-T303 ,-S-T304 ,-S (O)-T305 ,-S (O ₂)-T306 ,-S (O ₂) NH-T307 ,-S (O ₂) NT308T309 ,-S (O ₂) O-T310 ,-P (O) is (OT312) (OT311), and-Si (T313) is (T315) (T314) ";

T264 wherein, T265, T266, T267, T268, T269, T270, T271, T272, T273, T274, T275, T276, T277; T278, T279, T280, T281, T282, T283, T284, T285, T286, T287, T288, T289, T290; T291, T292, T293, T294, T295, T296, T297, T298, T299, T300, T301, T302, T303; T304, T305, T306, T307, T308, T309, T310, T311, T312, T313, T314, T315 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, T270, T271 and/or T279; T280 and/or T292, T293 and/or T299, T300 and/or T308, T309 also can form " heterocyclic radical " in each case together;

(iii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHT316 ,-NT317T318 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-T319 ,-C (O) O-T320 ,-C (O) NH-T321 ,-C (O) NT322T323 ,-O-T324 ,-O are (T325-O) _w-H (w=1,2,3,4,5) ,-O (T326-O) _w-T327 (w=1,2,3,4,5) ,-OC (O)-T328 ,-OC (O)-O-T329 ,-OC (O)-NHT330 ,-O-C (O)-NT331T332 ,-OP (O) is (OT334) (OT333), and-OSi (T335) is (T337) (T336) ,-OS (O ₂)-T338 ,-NHC (O)-T339 ,-NT340C (O)-T341 ,-NH-C (O)-O-T342 ,-NH-C (O)-NH-T343 ,-NH-C (O)-NT344T345 ,-NT346-C (O)-O-T347 ,-NT348-C (O)-NH-T349 ,-NT350-C (O)-NT351T352 ,-NHS (O ₂)-T353 ,-NT354S (O ₂)-T355 ,-S-T356 ,-S (O)-T357 ,-S (O ₂)-T358 ,-S (O ₂) NH-T359 ,-S (O ₂) NT360T361 ,-S (O ₂) O-T362 ,-P (O) is (OT364) (OT363), and-Si (T365) is (T367) (T366) ";

T316 wherein, T317, T318, T319, T320, T321, T322, T323, T324, T325, T326, T327, T328, T329; T330, T331, T332, T333, T334, T335, T336, T337, T338, T339, T340, T341, T342; T343, T344, T345, T346, T347, T348, T349, T350, T351, T352, T353, T354, T355; T356, T357, T358, T359, T360, T361, T362, T363, T364, T365, T366, T367 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, T322, T323 and/or T331; T332 and/or T344, T345 and/or T351, T352 and/or T360, T361 also can form " heterocyclic radical " in each case together;

(b)-NZ26Z27, wherein one of Z26, Z27 group or Z26, Z27 group the two be selected from independently of one another:

(1)“-C(Y4)NZ28Z29，-C(＝NZ30)-Z31”；

Wherein Y4 is independently selected from " O, S ,=NH ,=NZ32 ";

Condition is that at least one at least one in Z28, the Z29 group and Z30, the Z31 group is independently selected from:

(I) " alkyl, naphthenic base, heterocyclic radical, aryl, heteroaryl ,-C (O)-alkyl ,-C (O)-aryl ,-C (O)-heteroaryl ";

Other condition is, the above-mentioned substituting group of substituting group group (I) is independently of one another by at least one identical ground or different are selected from following substituting group and further replace:

(i) " (C ₉-C ₃₀) alkyl, cycloalkylalkyl, heterocyclic radical alkyl, arylalkyl, heteroarylalkyl, N ₃,-NT368T369 ,-NHC (O)-cycloalkylalkyl;-NHC (O)-heterocyclic radical alkyl ,-NT370C (O)-T371 ,-NH-C (O)-O-T372;-NH-C (O)-NH-T373 ,-NH-C (O)-NT374T375 ,-NT376-C (O)-O-T377;-NT378-C (O)-NH-T379 ,-NT380-C (O)-NT381T382 ,-NHS (O ₂)-cycloalkylalkyl ,-NHS (O ₂)-heterocyclic radical alkyl ,-NT383S (O ₂)-T384 ,-O-T385 ,-O are (T386-O) _x-T387 (x=1,2,3,4,5) ,-O (T388-O) _x-H (x=1,2,3,4,5) ,-OC (O)-cycloalkylalkyl ,-OC (O)-heterocyclic radical alkyl ,-OC (O)-O-T389 ,-OC (O)-NHT390 ,-O-C (O)-NT391T392 ,-OS (O ₂)-cycloalkylalkyl ,-OS (O ₂)-heterocyclic radical alkyl ,-OP (O) is (OT394) (OT393), and-OSi (T395) is (T397) (T396) ,-CHO ,-C (O)-naphthenic base;-C (O)-heterocyclic radical ,-C (O)-cycloalkylalkyl ,-C (O)-heterocyclic radical alkyl ,-C (O)-arylalkyl ,-C (O)-heteroarylalkyl;-S-cycloalkylalkyl ,-S-heterocyclic radical alkyl ,-S-arylalkyl ,-S-heteroarylalkyl;-S (O)-naphthenic base ,-S (O)-heterocyclic radical ,-S (O)-heteroaryl ,-S (O)-cycloalkylalkyl;-S (O)-heterocyclic radical alkyl ,-S (O)-arylalkyl ,-S (O)-heteroarylalkyl ,-S (O ₂)-naphthenic base ,-S (O ₂)-heterocyclic radical ,-S (O ₂)-heteroaryl ,-S (O ₂)-cycloalkylalkyl ,-S (O ₂)-heterocyclic radical alkyl ,-S (O ₂)-arylalkyl ,-S (O ₂)-heteroarylalkyl ,-S (O ₂) the NH-naphthenic base ,-S (O ₂) the NH-heterocyclic radical ,-S (O ₂) the NH-cycloalkylalkyl ,-S (O ₂) NH-heterocyclic radical alkyl ,-S (O ₂) the NH-heteroarylalkyl ,-S (O ₂) NT398T399 ,-S (O ₂) the O-naphthenic base ,-S (O ₂) the O-heterocyclic radical ,-S (O ₂) the O-heteroaryl ,-S (O ₂) the O-cycloalkylalkyl ,-S (O ₂) O-heterocyclic radical alkyl ,-S (O ₂) the O-heteroarylalkyl ,-P (O) is (OH) ₂,-P (O) is (OT401) (OT400), and-Si (T402) is (T404) (T403) ";

Other condition is " N (alkyl) ₂", " C (O) N (alkyl) ₂", " C (O) N (naphthenic base) ₂", " C (O) N (aryl) ₂", " C (O) N (heteroaryl) ₂" be selected from following substituting group group substituting group (ii) by at least one and further replace;

T368 wherein, T369, T370, T371, T372, T373, T374, T375, T376, T377; T378, T379, T380, T381, T382, T383, T384, T385, T386, T387; T388, T389, T390, T391, T392, T393, T394, T395, T396; T397, T398, T399, T400, T401, T402, T403, T404 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl; Aryl, arylalkyl, heteroaryl, heteroarylalkyl " and wherein, perhaps; T374, T375 and/or T381, T382 and/or T391, T392 and/or T398, T399 also can form " heterocyclic radical " in each case together;

Wherein randomly, the above-mentioned substituting group of substituting group group (i) can so that independently of one another by at least one identical ground or different are selected from following substituting group and further replace:

(ii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHT405 ,-NT406T407 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-T408 ,-C (O) O-T409 ,-C (O) NH-T410 ,-C (O) NT411T412 ,-O-T413 ,-O are (T414-O) _y-H (y=1,2,3,4,5) ,-O (T415-O) _y-T416 (y=1,2,3,4,5) ,-OC (O)-T417 ,-OC (O)-O-T418 ,-OC (O)-NHT419 ,-O-C (O)-NT420T421 ,-OP (O) is (OT423) (OT422), and-OSi (T424) is (T426) (T425) ,-OS (O ₂)-T427 ,-NHC (O)-T428 ,-NT429C (O)-T430 ,-NH-C (O)-O-T431 ,-NH-C (O)-NH-T432 ,-NH-C (O)-NT433T434 ,-NT435-C (O)-O-T436 ,-NT437-C (O)-NH-T438 ,-NT439-C (O)-NT440T441 ,-NHS (O ₂)-T442 ,-NT443S (O ₂)-T444 ,-S-T445 ,-S (O)-T446 ,-S (O ₂)-T447 ,-S (O ₂) NH-T448 ,-S (O ₂) NT449T450 ,-S (O ₂) O-T451 ,-P (O) is (OT453) (OT452), and-Si (T454) is (T456) (T455) ";

T405 wherein, T406, T407, T408, T409, T410, T411, T412, T413, T414, T415, T416, T417, T418; T419, T420, T421, T422, T423, T424, T425, T426, T427, T428, T429, T430, T431; T432, T433, T434, T435, T436, T437, T438, T439, T440, T441, T442, T443, T444; T445, T446, T447, T448, T449, T450, T451, T452, T453, T454, T455, T456 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, T411, T412 and/or T420; T421 and/or T433, T434 and/or T440, T441 and/or T449, T450 also can form " heterocyclic radical " in each case together;

(iii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHT457 ,-NT458T459 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-T460 ,-C (O) O-T461 ,-C (O) NH-T462 ,-C (O) NT463T464 ,-O-T465 ,-O are (T466-O) _z-H (z=1,2,3,4,5) ,-O (T467-O) _z-T468 (z=1,2,3,4,5) ,-OC (O)-T469 ,-OC (O)-O-T470 ,-OC (O)-NHT471 ,-O-C (O)-NT472T473 ,-OP (O) is (OT475) (OT474), and-OSi (T476) is (T478) (T477) ,-OS (O ₂)-T479 ,-NHC (O)-T480 ,-NT481C (O)-T482 ,-NH-C (O)-O-T483 ,-NH-C (O)-NH-T484 ,-NH-C (O)-NT485T486 ,-NT487-C (O)-O-T488 ,-NT489-C (O)-NH-T490 ,-NT491-C (O)-NT492T493 ,-NHS (O ₂)-T494 ,-NT495S (O ₂)-T496 ,-S-T497 ,-S (O)-T498 ,-S (O ₂)-T499 ,-S (O ₂) NH-T500 ,-S (O ₂) NT501T502 ,-S (O ₂) O-T503 ,-P (O) is (OT505) (OT504), and-Si (T506) is (T508) (T507) ";

T457 wherein, T458, T459, T460, T461, T462, T463, T464, T465, T466, T467, T468, T469, T470; T471, T472, T473, T474, T475, T476, T477, T478, T479, T480, T481, T482, T483; T484, T485, T486, T487, T488, T489, T490, T491, T492, T493, T494, T495, T496; T497, T498, T499, T500, T501, T502, T503, T504, T505, T506, T507, T508 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, T463, T464 and/or T472; T473 and/or T485, T486 and/or T492, T493 and/or T501, T502 also can form " heterocyclic radical " in each case together;

OrCondition is that at least one at least one in Z28, the Z29 group and Z30, the Z31 group is independently selected from:

(II) " (C ₉-C ₃₀) alkyl, cycloalkylalkyl, heterocyclic radical alkyl, arylalkyl, heteroarylalkyl ,-C (O)-(C ₉-C ₃₀) alkyl ,-C (O)-naphthenic base ,-C (O)-cycloalkylalkyl ,-C (O)-arylalkyl ,-C (O)-heteroarylalkyl ,-C (O)-heterocyclic radical ,-C (O)-heterocyclic radical alkyl ,-S (O ₂)-alkyl ,-S (O ₂)-(C ₉-C ₃₀) alkyl ,-S (O ₂)-naphthenic base ,-S (O ₂)-cycloalkylalkyl ,-S (O ₂)-aryl ,-S (O ₂)-arylalkyl ,-S (O ₂)-heteroaryl ,-S (O ₂)-heteroarylalkyl ,-S (O ₂)-heterocyclic radical ,-S (O ₂)-heterocyclic radical alkyl ";

Wherein randomly, the above-mentioned substituting group of substituting group group (II) can be independently of one another by at least one identical ground or different are selected from following substituting group and further replace:

(i) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHT509 ,-NT510T511 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-T512 ,-C (O) O-T513 ,-C (O) NH-T514 ,-C (O) NT515T516 ,-O-T517 ,-O are (T518-O) _a-H (a=1,2,3,4,5) ,-O (T519-O) _a-T520 (a=1,2,3,4,5) ,-OC (O)-T521 ,-OC (O)-O-T522 ,-OC (O)-NHT523 ,-O-C (O)-NT524T525 ,-OP (O) is (OT527) (OT526), and-OSi (T528) is (T530) (T529) ,-OS (O ₂)-T531 ,-NHC (O)-T532 ,-NT533C (O)-T534 ,-NH-C (O)-O-T535 ,-NH-C (O)-NH-T536 ,-NH-C (O)-NT537T538 ,-NT539-C (O)-O-T540 ,-NT541-C (O)-NH-T542 ,-NT543-C (O)-NT544T545 ,-NHS (O ₂)-T546 ,-NT547S (O ₂)-T548 ,-S-T549 ,-S (O)-T550 ,-S (O ₂)-T551 ,-S (O ₂) NH-T552 ,-S (O ₂) NT553T554 ,-S (O ₂) O-T555 ,-P (O) is (OT557) (OT556), and-Si (T558) is (T560) (T559) ";

T509 wherein, T510, T511, T512, T513, T514, T515, T516, T517, T518, T519, T520, T521, T522; T523, T524, T525, T526, T527, T528, T529, T530, T531, T532, T533, T534, T535; T536, T537, T538, T539, T540, T541, T542, T543, T544, T545, T546, T547, T548; T549, T550, T551, T552, T553, T554, T555, T556, T557, T558, T559, T560 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, T515, T516 and/or T524; T525 and/or T537, T538 and/or T544, T545 and/or T553, T554 also can form " heterocyclic radical " in each case together;

(ii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHT561 ,-NT562T563 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-T564 ,-C (O) O-T565 ,-C (O) NH-T566 ,-C (O) NT567T568 ,-O-T569 ,-O are (T570-O) _b-H (b=1,2,3,4,5) ,-O (T571-O) _b-T572 (b=1,2,3,4,5) ,-OC (O)-T573 ,-OC (O)-O-T574 ,-OC (O)-NHT575 ,-O-C (O)-NT576T577 ,-OP (O) is (OT579) (OT578), and-OSi (T580) is (T582) (T581) ,-OS (O ₂)-T583 ,-NHC (O)-T584 ,-NT585C (O)-T586 ,-NH-C (O)-O-T587 ,-NH-C (O)-NH-T588 ,-NH-C (O)-NT589T590 ,-NT591-C (O)-O-T592 ,-NT593-C (O)-NH-T594 ,-NT595-C (O)-NT596T597 ,-NHS (O ₂)-T598 ,-NT599S (O ₂)-T600 ,-S-T601 ,-S (O)-T602 ,-S (O ₂)-T603 ,-S (O ₂) NH-T604 ,-S (O ₂) NT605T606 ,-S (O ₂) O-T607 ,-P (O) is (OT609) (OT608), and-Si (T610) is (T612) (T611) ";

T561 wherein, T562, T563, T564, T565, T566, T567, T568, T569, T570, T571, T572, T573, T574; T575, T576, T577, T578, T579, T580, T581, T582, T583, T584, T585, T586, T587; T588, T589, T590, T591, T592, T593, T594, T595, T596, T597, T598, T599, T600; T601, T602, T603, T604, T605, T606, T607, T608, T609, T610, T611, T612 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, T567, T568 and/or T576; T577 and/or T589, T590 and/or T596, T597 and/or T605, T606 also can form " heterocyclic radical " in each case together;

(iii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHT613 ,-NT614T615 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-T616 ,-C (O) O-T617 ,-C (O) NH-T618 ,-C (O) NT619T620 ,-O-T621 ,-O are (T622-O) _c-H (c=1,2,3,4,5) ,-O (T623-O) _c-T624 (c=1,2,3,4,5) ,-OC (O)-T625 ,-OC (O)-O-T626 ,-OC (O)-NHT627 ,-O-C (O)-NT628T629 ,-OP (O) is (OT631) (OT630), and-OSi (T632) is (T634) (T633) ,-OS (O ₂)-T635 ,-NHC (O)-T636 ,-NT637C (O)-T638 ,-NH-C (O)-O-T639 ,-NH-C (O)-NH-T640 ,-NH-C (O)-NT641T642 ,-NT643-C (O)-O-T644 ,-NT645-C (O)-NH-T646 ,-NT647-C (O)-NT648T649 ,-NHS (O ₂)-T650 ,-NT651S (O ₂)-T652 ,-S-T653 ,-S (O)-T654 ,-S (O ₂)-T655 ,-S (O ₂) NH-T656 ,-S (O ₂) NT657T658 ,-S (O ₂) O-T659 ,-P (O) is (OT661) (OT660), and-Si (T662) is (T664) (T663) ";

T613 wherein, T614, T615, T616, T617, T618, T619, T620, T621, T622, T623, T624, T625, T626; T627, T628, T629, T630, T631, T632, T633, T634, T635, T636, T637, T638, T639; T640, T641, T642, T643, T644, T645, T646, T647, T648, T649, T650, T651, T652; T653, T654, T655, T656, T657, T658, T659, T660, T661, T662, T663, T664 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, T619, T620 and/or T628; T629 and/or T641, T642 and/or T648, T649 and/or T657, T658 also can form " heterocyclic radical " in each case together;

AndOne of Z28, Z29 group or Z28, Z29 group the two not and one of Z30, Z31 group or Z30, Z31 group the two be not independently selected from the Z32 group:

(III) " hydrogen, alkyl, naphthenic base, heterocyclic radical, aryl, heteroaryl ,-C (O)-alkyl ,-C (O)-aryl ,-C (O)-heteroaryl ";

Wherein randomly, the above-mentioned substituting group of substituting group group (III) can be selected from following substituting group replacement independently of one another and then by at least one identically or differently:

(i) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHT665 ,-NT666T667 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-T668 ,-C (O) O-T669 ,-C (O) NH-T670 ,-C (O) NT671T672 ,-O-T673 ,-O are (T674-O) _d-H (d=1,2,3,4,5) ,-O (T675-O) _d-T676 (d=1,2,3,4,5) ,-OC (O)-T677 ,-OC (O)-O-T678 ,-OC (O)-NHT679 ,-O-C (O)-NT680T681 ,-OP (O) is (OT683) (OT682), and-OSi (T684) is (T686) (T685) ,-OS (O ₂)-T687 ,-NHC (O)-T688 ,-NT689C (O)-T690 ,-NH-C (O)-O-T691 ,-NH-C (O)-NH-T692 ,-NH-C (O)-NT693T694 ,-NT695-C (O)-O-T696 ,-NT697-C (O)-NH-T698 ,-NT699-C (O)-NT700T701 ,-NHS (O ₂)-T702 ,-NT703S (O ₂)-T704 ,-S-T705 ,-S (O)-T706 ,-S (O ₂)-T707 ,-S (O ₂) NH-T708 ,-S (O ₂) NT709T710 ,-S (O ₂₎O-T711 ,-P (O) is (OT713) (OT712) ,-Si (T714) is (T716) (T715) ";

T665 wherein, T666, T667, T668, T669, T670, T671, T672, T673, T674, T675, T676, T677, T678; T679, T680, T681, T682, T683, T684, T685, T686, T687, T688, T689, T690, T691; T692, T693, T694, T695, T696, T697, T698, T699, T700, T701, T702, T703, T704; T705, T706, T707, T708, T709, T710, T711, T712, T713, T714, T715, T716 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, T671, T672 and/or T680; T681 and/or T693, T694 and/or T700, T701 and/or T709, T710 also can form " heterocyclic radical " in each case together;

(ii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHT717 ,-NT718T719 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-T720 ,-C (O) O-T721 ,-C (O) NH-T722 ,-C (O) NT723T724 ,-O-T725 ,-O are (T726-O) _e-H (e=1,2,3,4,5) ,-O (T727-O) _e-T728 (e=1,2,3,4,5) ,-OC (O)-T729 ,-OC (O)-O-T730 ,-OC (O)-NHT731 ,-O-C (O)-NT732T733 ,-OP (O) is (OT735) (OT734), and-OSi (T736) is (T738) (T737) ,-OS (O ₂)-T739 ,-NHC (O)-T740 ,-NT741C (O)-T742 ,-NH-C (O)-O-T743 ,-NH-C (O)-NH-T744 ,-NH-C (O)-NT745T746 ,-NT747-C (O)-O-T748 ,-NT749-C (O)-NH-T75O ,-NT751-C (O)-NT752T753 ,-NHS (O ₂)-T754 ,-NT755S (O ₂)-T756 ,-S-T757 ,-S (O)-T758 ,-S (O ₂)-T759 ,-S (O ₂) NH-T760 ,-S (O ₂) NT761T762 ,-S (O ₂) O-T763 ,-P (O) is (OT765) (OT764), and-Si (T766) is (T768) (T767) ";

T717 wherein, T718, T719, T720, T721, T722, T723, T724, T725, T726, T727, T728, T729, T730; T731, T732, T733, T734, T735, T736, T737, T738, T739, T740, T741, T742, T743; T744, T745, T746, T747, T748, T749, T750, T751, T752, T753, T754, T755, T756; T757, T758, T759, T760, T761, T762, T763, T764, T765, T766, T767, T768 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, T723, T724 and/or T732; T733 and/or T745, T746 and/or T752, T753 and/or T761, T762 also can form " heterocyclic radical " in each case together;

(iii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHT769 ,-NT770T771 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-T772 ,-C (O) O-T773 ,-C (O) NH-T774 ,-C (O) NT775T776 ,-O-T777 ,-O are (T778-O) _f-H (f=1,2,3,4,5) ,-O (T779-O) _f-T780 (f=1,2,3,4,5) ,-OC (O)-T781 ,-OC (O)-O-T782 ,-OC (O)-NHT783 ,-O-C (O)-NT784T785 ,-OP (O) is (OT787) (OT786), and-OSi (T788) is (T790) (T789) ,-OS (O ₂)-T791 ,-NHC (O)-T792 ,-NT793C (O)-T794 ,-NH-C (O)-O-T795 ,-NH-C (O)-NH-T796 ,-NH-C (O)-NT797T798 ,-NT799-C (O)-O-T800 ,-NT801-C (O)-NH-T802 ,-NT803-C (O)-NT804T805 ,-NHS (O ₂)-T806 ,-NT807S (O ₂)-T808 ,-S-T809 ,-S (O)-T810 ,-S (O ₂)-T811 ,-S (O ₂) NH-T812 ,-S (O ₂) NT813T814 ,-S (O ₂) O-T815 ,-P (O) is (OT817) (OT816), and-Si (T818) is (T820) (T819) ";

T769 wherein, T770, T771, T772, T773, T774, T775, T776, T777, T778, T779, T780, T781, T782; T783, T784, T785, T786, T787, T788, T789, T790, T791, T792, T793, T794, T795; T796, T797, T798, T799, T800, T801, T802, T803, T804, T805, T806, T807, T808; T809, T810, T811, T812, T813, T814, T815, T816, T817, T818, T819, T820 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, T775, T776 and/or T784; T785 and/or T797, T798 and/or T804, T805 and/or T813, T814 also can form " heterocyclic radical " in each case together;

(2)“-C(Y5)NZ33-Y6-Z34”；

Y5 wherein, Y6 is selected from " O, S ,=NH ,=NZ35 " independently of one another;

Z33 wherein, Z34, Z35 is selected from independently of one another:

(I) " hydrogen, alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl ,-C (O)-alkyl ,-C (O)-(C ₉-C ₃₀) alkyl ,-C (O)-naphthenic base ,-C (O)-cycloalkylalkyl ,-C (O)-aryl ,-C (O)-arylalkyl ,-C (O)-heteroaryl ,-C (O)-heteroarylalkyl ,-C (O)-heterocyclic radical ,-C (O)-heterocyclic radical alkyl ,-S (O ₂)-alkyl ,-S (O ₂)-(C ₉-C ₃₀) alkyl ,-S (O ₂)-naphthenic base ,-S (O ₂)-cycloalkylalkyl ,-S (O ₂)-aryl ,-S (O ₂)-arylalkyl ,-S (O ₂)-heteroaryl ,-S (O ₂)-heteroarylalkyl ,-S (O ₂)-heterocyclic radical ,-S (O ₂)-heterocyclic radical alkyl ";

Wherein randomly, the above-mentioned substituting group of substituting group group (I) can be selected from following substituting group replacement independently of one another and then by at least one identically or differently:

(i) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHT821 ,-NT822T823 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-T824 ,-C (O) O-T825 ,-C (O) NH-T826 ,-C (O) NT827T828 ,-O-T829 ,-O are (T830-O) _g-H (g=1,2,3,4,5) ,-O (T831-O) _g-T832 (g=1,2,3,4,5) ,-OC (O)-T833 ,-OC (O)-O-T834 ,-OC (O)-NHT835 ,-O-C (O)-NT836T837 ,-OP (O) is (OT839) (OT838), and-OSi (T840) is (T842) (T814) ,-OS (O ₂)-T843 ,-NHC (O)-T844 ,-NT845C (O)-T846 ,-NH-C (O)-O-T847 ,-NH-C (O)-NH-T848 ,-NH-C (O)-NT849T850 ,-NT851-C (O)-O-T852 ,-NT853-C (O)-NH-T854 ,-NT855-C (O)-NT856T857 ,-NHS (O ₂)-T858 ,-NT859S (O ₂)-T860 ,-S-T861 ,-S (O)-T862 ,-S (O ₂)-T863 ,-S (O ₂) NH-T864 ,-S (O ₂) NT865T866 ,-S (O ₂) O-T867 ,-P (O) is (OT869) (OT868), and-Si (T870) is (T872) (T871) ";

T821 wherein, T822, T823, T824, T825, T826, T827, T828, T829, T830, T831, T832, T833, T834; T835, T836, T837, T838, T839, T840, T841, T842, T843, T844, T845, T846, T847; T848, T849, T850, T851, T852, T853, T854, T855, T856, T857, T858, T859, T860; T861, T862, T863, T864, T865, T866, T867, T868, T869, T870, T871, T872 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, T827, T828 and/or T836; T837 and/or T849, T850 and/or T856, T857 and/or T865, T866 also can form " heterocyclic radical " in each case together;

(ii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHT873 ,-NT874T875 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-T876 ,-C (O) O-T877 ,-C (O) NH-T878 ,-C (O) NT879T880 ,-O-T881 ,-O are (T882-O) _h-H (h=1,2,3,4,5) ,-O (T883-O) _h-T884 (h=1,2,3,4,5) ,-OC (O)-T885 ,-OC (O)-O-T886 ,-OC (O)-NHT887 ,-O-C (O)-NT888T889 ,-OP (O) is (OT891) (OT890), and-OSi (T892) is (T894) (T893) ,-OS (O ₂)-T895 ,-NHC (O)-T896 ,-NT897C (O)-T898 ,-NH-C (O)-O-T899 ,-NH-C (O)-NH-T900 ,-NH-C (O)-NT901T902 ,-NT903-C (O)-O-T904 ,-NT905-C (O)-NH-T906 ,-NT907-C (O)-NT908T909 ,-NHS (O ₂)-T910 ,-NT911S (O ₂)-T912 ,-S-T913 ,-S (O)-T914 ,-S (O ₂)-T915 ,-S (O ₂) NH-T916 ,-S (O ₂) NT917T918 ,-S (O ₂) O-T919 ,-P (O) is (OT921) (OT920), and-Si (T922) is (T924) (T923) ";

T873 wherein, T874, T875, T876, T877, T878, T879, T880, T881, T882, T883, T884, T885, T886; T887, T888, T889, T890, T891, T892, T893, T894, T895, T896, T897, T898, T899; T900, T901, T902, T903, T904, T905, T906, T907, T908, T909, T910, T911, T912; T913, T914, T915, T916, T917, T918, T919, T920, T921, T922, T923, T924 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, T879, T880 and/or T888; T889 and/or T901, T902 and/or T908, T909 and/or T917, T918 also can form " heterocyclic radical " in each case together;

(iii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHT925 ,-NT926T927 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-T928 ,-C (O) O-T929 ,-C (O) NH-T930 ,-C (O) NT931T932 ,-O-T933 ,-O are (T934-O) _i-H (i=1,2,3,4,5) ,-O (T935-O) _i-T936 (i=1,2,3,4,5) ,-OC (O)-T937 ,-OC (O)-O-T938 ,-OC (O)-NHT939 ,-O-C (O)-NT940T941 ,-OP (O) is (OT943) (OT942), and-OSi (T944) is (T946) (T945) ,-OS (O ₂)-T947 ,-NHC (O)-T948 ,-NT949C (O)-T950 ,-NH-C (O)-O-T951 ,-NH-C (O)-NH-T952 ,-NH-C (O)-NT953T954 ,-NT955-C (O)-O-T956 ,-NT957-C (O)-NH-T958 ,-NT959-C (O)-NT960T961 ,-NHS (O ₂)-T962 ,-NT963S (O ₂)-T964 ,-S-T965 ,-S (O)-T966 ,-S (O ₂)-T967 ,-S (O ₂) NH-T968 ,-S (O ₂) NT969T970 ,-S (O ₂) O-T971 ,-P (O) is (OT973) (OT972), and-Si (T974) is (T976) (T975) ";

T925 wherein, T926, T927, T928, T929, T930, T931, T932, T933, T934, T935, T936, T937, T938; T939, T940, T941, T942, T943, T944, T945, T946, T947, T948, T949, T950, T951; T952, T953, T954, T955, T956, T957, T958, T959, T960, T961, T962, T963, T964; T965, T966, T967, T968, T969, T970, T971, T972, T973, T974, T975, T976 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, T931, T932 and/or T940; T941 and/or T953, T954 and/or T960, T961 and/or T969, T970 also can form " heterocyclic radical " in each case together;

AndThe two all dependently is selected from one of Z26, Z27 group or Z26, Z27 group:

(2) " hydrogen, alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl ,-C (O)-alkyl ,-C (O)-(C ₉-C ₃₀) alkyl ,-C (O)-naphthenic base ,-C (O)-cycloalkylalkyl ,-C (O)-aryl ,-C (O)-arylalkyl ,-C (O)-heteroaryl ,-C (O)-heteroarylalkyl ,-C (O)-heterocyclic radical ,-C (O)-heterocyclic radical alkyl ,-C (Y7) NZ36Z37 ,-C (=NZ38)-and Z39 ,-S (O ₂)-alkyl ,-S (O ₂)-(C ₉-C ₃₀) alkyl ,-S (O ₂)-naphthenic base ,-S (O ₂)-cycloalkylalkyl ,-S (O ₂)-aryl ,-S (O ₂)-arylalkyl ,-S (O ₂)-heteroaryl ,-S (O ₂)-heteroarylalkyl ,-S (O ₂)-heterocyclic radical ,-S (O ₂)-heterocyclic radical alkyl ";

Wherein Y7 is independently selected from " O, S ,=NH ,=NZ40 ";

Wherein said Z36, Z37, Z38, Z39, the Z40 group is selected from independently of one another:

(I) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl ,-C (O)-alkyl ,-C (O)-(C ₉-C ₃₀) alkyl ,-C (O)-naphthenic base ,-C (O)-cycloalkylalkyl ,-C (O)-aryl ,-C (O)-arylalkyl ,-C (O)-heteroaryl ,-C (O)-heteroarylalkyl ,-C (O)-heterocyclic radical ,-C (O)-heterocyclic radical alkyl ,-S (O ₂)-alkyl ,-S (O ₂)-(C ₉-C ₃₀) alkyl ,-S (O ₂)-naphthenic base ,-S (O ₂)-cycloalkylalkyl ,-S (O ₂)-aryl ,-S (O ₂)-arylalkyl ,-S (O ₂)-heteroaryl ,-S (O ₂)-heteroarylalkyl ,-S (O ₂)-heterocyclic radical ,-S (O ₂)-heterocyclic radical alkyl ";

Wherein randomly, the above-mentioned substituting group of substituting group group (3) and/or substituting group group (I) can be selected from following substituting group replacement independently of one another and then by at least one identically or differently:

(i) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHT977 ,-NT978T979 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-T980 ,-C (O) O-T981 ,-C (O) NH-T982 ,-C (O) NT983T984 ,-O-T985 ,-O are (T986-O) _j-H (j=1,2,3,4,5) ,-O (T987-O) _j-T988 (j=1,2,3,4,5) ,-OC (O)-T989 ,-OC (O)-O-T990 ,-OC (O)-NHT991 ,-O-C (O)-NT992T993 ,-OP (O) is (OT995) (OT994), and-OSi (T996) is (T998) (T997) ,-OS (O ₂)-T999 ,-NHC (O)-T1000 ,-NT1001C (O)-T1002 ,-NH-C (O)-O-T1003;-NH-C (O)-NH-T1004 ,-NH-C (O)-NT1005T1006 ,-NT1007-C (O)-O-T1008;-NT1009-C (O)-NH-T1010 ,-NT1011-C (O)-NT1012T1013 ,-NHS (O ₂)-T1014 ,-NT1015S (O ₂)-T1016 ,-S-T1017 ,-S (O)-T1018 ,-S (O ₂)-T1019 ,-S (O ₂) NH-T1020 ,-S (O ₂) NT1021T1022 ,-S (O ₂) O-T1023 ,-P (O) is (OT1025) (OT1024), and-Si (T1026) is (T1028) (T1027) ";

T977 wherein, T978, T979, T980, T981, T982, T983, T984, T985, T986, T987; T988, T989, T990, T991, T992, T993, T994, T995, T996, T997, T998; T999, T1000, T1001, T1002, T1003, T1004, T1005, T1006, T1007, T1008, T1009; T1010, T1011, T1012, T1013, T1014, T1015, T1016, T1017, T1018, T1019; T1020, T1021, T1022, T1023, T1024, T1025, T1026, T1027, T1028 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, T983, T984 and/or T992; T993 and/or T1005, T1006 and/or T1012, T1013 and/or T1021, T1022 also can form " heterocyclic radical " in each case together;

(ii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHT1029 ,-NT1030T1031 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-T1032 ,-C (O) O-T1033 ,-C (O) NH-T1034 ,-C (O) NT1035T1036 ,-O-T1037 ,-O are (T1038-O) _k-H (k=1,2,3,4,5) ,-O (T1039-O) _k-T1040 (k=1,2,3,4,5) ,-OC (O)-T1041 ,-OC (O)-O-T1042 ,-OC (O)-NHT1043 ,-O-C (O)-NT1044T1045 ,-OP (O) is (OT1047) (OT1046), and-OSi (T1048) is (T1050) (T1049) ,-OS (O ₂)-T1051 ,-NHC (O)-T1052 ,-NT1053C (O)-T1054 ,-NH-C (O)-O-T1055;-NH-C (O)-NH-T1056 ,-NH-C (O)-NT1057T1058 ,-NT1059-C (O)-O-T1060;-NT1061-C (O)-NH-T1062 ,-NT1063-C (O)-NT1064T1065 ,-NHS (O ₂)-T1066 ,-NT1067S (O ₂)-T1068 ,-S-T1069 ,-S (O)-T1070 ,-S (O ₂)-T1071 ,-S (O ₂) NH-T1072 ,-S (O ₂) NT1073T1074 ,-S (O ₂) O-T1075 ,-P (O) is (OT1077) (OT1076), and-Si (T1078) is (T1080) (T1079) ";

T1029 wherein, T1030, T1031, T1032, T1033, T1034, T1035, T1036, T1037, T1038, T1039; T1040, T1041, T1042, T1043, T1044, T1045, T1046, T1047, T1048, T1049, T1050; T1051, T1052, T1053, T1054, T1055, T1056, T1057, T1058, T1059, T1060, T1061; T1062, T1063, T1064, T1065, T1066, T1067, T1068, T1069, T1070, T1071; T1072, T1073, T1074, T1075, T1076, T1077, T1078, T1079, T1080 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, T1035, T1036 and/or T1044; T1045 and/or T1057, T1058 and/or T1064, T1065 and/or T1073, T1074 also can form " heterocyclic radical " in each case together;

(iii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHT1081 ,-NT1082T1083 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-T1084 ,-C (O) O-T1085 ,-C (O) NH-T1086 ,-C (O) NT1087T1088 ,-O-T1089 ,-O are (T1090-O) _l-H (1=1,2,3,4,5) ,-O (T1091-O) _l-T1092 (1=1,2,3,4,5) ,-OC (O)-T1093 ,-OC (O)-O-T1094 ,-OC (O)-NHT1095 ,-O-C (O)-NT1096T1097 ,-OP (O) is (OT1099) (OT1098), and-OSi (T1100) is (T1102) (T1101) ,-OS (O ₂)-T1103 ,-NHC (O)-T1104 ,-NT1105C (O)-T1106 ,-NH-C (O)-O-T1107;-NH-C (O)-NH-T1108 ,-NH-C (O)-NT1109T1110 ,-NT1111-C (O)-O-T1112;-NT1113-C (O)-NH-T1114 ,-NT1115-C (O)-NT1116T1117 ,-NHS (O ₂)-T1118 ,-NT1119S (O ₂)-T1120 ,-S-T1121 ,-S (O)-T1122 ,-S (O ₂)-T1123 ,-S (O ₂) NH-T1124 ,-S (O ₂) NT1125T1126 ,-S (O ₂) O-T1127 ,-P (O) is (OT1129) (OT1128), and-Si (T1130) is (T1132) (T1131) ";

T1081 wherein, T1082, T1083, T1084, T1085, T1086, T1087, T1088, T1089, T1090, T1091; T1092, T1093, T1094, T1095, T1096, T1097, T1098, T1099, T1100, T1101, T1102; T1103, T1104, T1105, T1106, T1107, T1108, T1109, T1110, T1111, T1112, T1113; T1114, T1115, T1116, T1117, T1118, T1119, T1120, T1121, T1122, T1123; T1124, T1125, T1126, T1127, T1128, T1129, T1130, T1131, T1132 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, T1087, T1088 and/or T1096; T1097 and/or T1109, T1110 and/or T1116, T1117 and/or T1125, T1126 also can form " heterocyclic radical " in each case together;

AndThe two all dependently is selected from one of Z1, Z2 group or Z1, Z2 group:

(c) hydrogen, alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHT1133 ,-NT1134T1135 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-T1136 ,-C (O) O-T1137 ,-C (O) NH-T1138 ,-C (O) NT1139T1140 ,-O-T1141 ,-O are (T1142-O) _m-H (m=1,2,3,4,5) ,-O (T1143-O) _m-T1144 (m=1,2,3,4,5) ,-OC (O)-T1145 ,-OC (O)-O-T1146 ,-OC (O)-NHT1147 ,-O-C (O)-NT1148T1149 ,-OP (O) is (OT1151) (OT1150), and-OSi (T1152) is (T1154) (T1153) ,-OS (O ₂)-T1155 ,-NHC (O)-T1156 ,-NT1157C (O)-T1158 ,-NH-C (O)-O-T1159;-NH-C (O)-NH-T1160 ,-NH-C (O)-NT1161T1162 ,-NT1163-C (O)-O-T1164;-NT1165-C (O)-NH-T1166 ,-NT1167-C (O)-NT1168T1169 ,-NHS (O ₂)-T1170 ,-NT1171S (O ₂)-T1172 ,-S-T1173 ,-S (O)-T1174 ,-S (O ₂)-T1175 ,-S (O ₂) NH-T1176 ,-S (O ₂) NT1177T1178 ,-S (O ₂) O-T1179 ,-P (O) is (OT1181) (OT1180), and-Si (T1182) is (T1184) (T1183) ";

T1133 wherein, T1134, T1135, T1136, T1137, T1138, T1139, T1140, T1141, T1142, T1143; T1144, T1145, T1146, T1147, T1148, T1149, T1150, T1151, T1152, T1153, T1154; T1155, T1156, T1157, T1158, T1159, T1160, T1161, T1162, T1163, T1164, T1165; T1166, T1167, T1168, T1169, T1170, T1171, T1172, T1173, T1174, T1175; T1176, T1177, T1178, T1179, T1180, T1181, T1182, T1183, T1184 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, T1139, T1140 and/or T1148; T1149 and/or T1161, T1162 and/or T1168, T1169 and/or T1177, T1178 also can form " heterocyclic radical " in each case together;

Wherein randomly, the above-mentioned substituting group of substituting group group (c) can so that independently of one another by at least one identical ground or different are selected from following substituting group and further replace:

(i) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHT1185 ,-NT1186T1187 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-T1188 ,-C (O) O-T1189 ,-C (O) NH-T1190 ,-C (O) NT1191T1192 ,-O-T1193 ,-O are (T1194-O) _n-H (n=1,2,3,4,5) ,-O (T1195-O) _n-T1196 (n=1,2,3,4,5) ,-OC (O)-T1197 ,-OC (O)-O-T1198 ,-OC (O)-NHT1199 ,-O-C (O)-NT1200T1201 ,-OP (O) is (OT1203) (OT1202), and-OSi (T1204) is (T1206) (T1205) ,-OS (O ₂)-T1207 ,-NHC (O)-T1208 ,-NT1209C (O)-T1210 ,-NH-C (O)-O-T1211;-NH-C (O)-NH-T1212 ,-NH-C (O)-NT1213T1214 ,-NT1215-C (O)-O-T1216;-NT1217-C (O)-NH-T1218 ,-NT1219-C (O)-NT1220T1221 ,-NHS (O ₂)-T1222 ,-NT1223S (O ₂)-T1224 ,-S-T1225 ,-S (O)-T1226 ,-S (O ₂)-T1227 ,-S (O ₂) NH-T1228 ,-S (O ₂) NT1229T1230 ,-S (O ₂) O-T1231 ,-P (O) is (OT1233) (OT1232), and-Si (T1234) is (T1236) (T1235) ";

T1185 wherein, T1186, T1187, T1188, T1189, T1190, T1191, T1192, T1193, T1194, T1195; T1196, T1197, T1198, T1199, T1200, T1201, T1202, T1203, T1204, T1205, T1206; T1207, T1208, T1209, T1210, T1211, T1212, T1213, T1214, T1215, T1216, T1217; T1218, T1219, T1220, T1221, T1222, T1223, T1224, T1225, T1226, T1227; T1228, T1229, T1230, T1231, T1232, T1233, T1234, T1235, T1236 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, T1191, T1192 and/or T1200; T1201 and/or T1213, T1214 and/or T1220, T1221 and/or T1229, T1230 also can form " heterocyclic radical " in each case together;

(ii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHT1237 ,-NT1238T1239 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-T1240 ,-C (O) O-T1241 ,-C (O) NH-T1242 ,-C (O) NT1243T1244 ,-O-T1245 ,-O are (T1246-O) _o-H (o=1,2,3,4,5) ,-O (T1247-O) _o-T1248 (o=1,2,3,4,5) ,-OC (O)-T1249 ,-OC (O)-O-T1250 ,-OC (O)-NHT1251 ,-O-C (O)-NT1252T1253 ,-OP (O) is (OT1255) (OT1254), and-OSi (T1256) is (T1258) (T1257) ,-OS (O ₂)-T1259 ,-NHC (O)-T1260 ,-NT1261C (O)-T1262 ,-NH-C (O)-O-T1263;-NH-C (O)-NH-T1264 ,-NH-C (O)-NT1265T1266 ,-NT1267-C (O)-O-T1268;-NT1269-C (O)-NH-T1270 ,-NT1271-C (O)-NT1272T1273 ,-NHS (O ₂)-T1274 ,-NT1275S (O ₂)-T1276 ,-S-T1277 ,-S (O)-T1278 ,-S (O ₂)-T1279 ,-S (O ₂) NH-T1280 ,-S (O ₂) NT1281T1282 ,-S (O ₂) O-T1283 ,-P (O) is (OT1285) (OT1284), and-Si (T1286) is (T1288) (T1287) ";

T1237 wherein, T1238, T1239, T1240, T1241, T1242, T1243, T1244, T1245, T1246, T1247; T1248, T1249, T1250, T1251, T1252, T1253, T1254, T1255, T1256, T1257, T1258; T1259, T1260, T1261, T1262, T1263, T1264, T1265, T1266, T1267, T1268, T1269; T1270, T1271, T1272, T1273, T1274, T1275, T1276, T1277, T1278, T1279; T1280, T1281, T1282, T1283, T1284, T1285, T1286, T1287, T1288 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, T1243, T1244 and/or T1252; T1253 and/or T1265, T1266 and/or T1272, T1273 and/or T1281, T1282 also can form " heterocyclic radical " in each case together;

(d)-and NZ41Z42, wherein said Z41, the Z42 group is selected from independently of one another:

(1) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl ,-C (O)-alkyl ,-C (O)-(C ₉-C ₃₀) alkyl ,-C (O)-naphthenic base ,-C (O)-cycloalkylalkyl ,-C (O)-aryl ,-C (O)-arylalkyl ,-C (O)-heteroaryl ,-C (O)-heteroarylalkyl ,-C (O)-heterocyclic radical ,-C (O)-heterocyclic radical alkyl ";

Wherein randomly, the above-mentioned substituting group of substituting group group (1) can be independently of one another by at least one identical ground or different are selected from following substituting group and further replace:

(i) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHT1289 ,-NT1290T1291 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-T1292 ,-C (O) O-T1293 ,-C (O) NH-T1294 ,-C (O) NT1295T1296 ,-O-T1297 ,-O are (T1298-O) _Rr-H (rr=1,2,3,4,5) ,-O (T1299-O) _Rr-T1300 (rr=1,2,3,4,5) ,-OC (O)-T1301 ,-OC (O)-O-T1302 ,-OC (O)-NHT1303 ,-O-C (O)-NT1304T1305 ,-OP (O) is (OT1307) (OT1306), and-OSi (T1308) is (T1310) (T1309) ,-OS (O ₂)-T1311 ,-NHC (O)-T1312 ,-NT1313C (O)-T1314 ,-NH-C (O)-O-T1315;-NH-C (O)-NH-T1316 ,-NH-C (O)-NT1317T1318 ,-NT1319-C (O)-O-T1320;-NT1321-C (O)-NH-T1322 ,-NT1323-C (O)-NT1324T1325 ,-NHS (O ₂)-T1326 ,-NT1327S (O ₂)-T1328 ,-S-T1329 ,-S (O)-T1330 ,-S (O ₂)-T1331 ,-S (O ₂) NH-T1332 ,-S (O ₂) NT1333T1334 ,-S (O ₂) O-T1335 ,-P (O) is (OT1337) (OT1336), and-Si (T1338) is (T1340) (T1339) ";

T1289 wherein, T1290, T1291, T1292, T1293, T1294, T1295, T1296, T1297, T1298, T1299; T1300, T1301, T1302, T1303, T1304, T1305, T1306, T1307, T1308, T1309, T1310; T1311, T1312, T1313, T1314, T1315, T1316, T1317, T1318, T1319, T1320, T1321; T1322, T1323, T1324, T1325, T1326, T1327, T1328, T1329, T1330, T1331; T1332, T1333, T1334, T1335, T1336, T1337, T1338, T1339, T1340 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, T1295, T1296 and/or T1304; T1305 and/or T1317, T1318 and/or T1324, T1325 and/or T1333, T1334 also can form " heterocyclic radical " in each case together;

(ii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHT1341 ,-NT1342T1343 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-T1344 ,-C (O) O-T1345 ,-C (O) NH-T1346 ,-C (O) NT1347T1348 ,-O-T1349 ,-O are (T1350-O) _Rs-H (rs=1,2,3,4,5) ,-O (T1351-O) _Rs-T1352 (rs=1,2,3,4,5) ,-OC (O)-T1353 ,-OC (O)-O-T1354 ,-OC (O)-NHT1355 ,-O-C (O)-NT1356T1357 ,-OP (O) is (OT1359) (OT1358), and-OSi (T1360) is (T1362) (T1361) ,-OS (O ₂)-T1363 ,-NHC (O)-T1364 ,-NT1365C (O)-T1366 ,-NH-C (O)-O-T1367;-NH-C (O)-NH-T1368 ,-NH-C (O)-NT1369T1370 ,-NT1371-C (O)-O-T1372;-NT1373-C (O)-NH-T1374 ,-NT1375-C (O)-NT1376T1377 ,-NHS (O ₂)-T1378 ,-NT1379S (O ₂)-T1380 ,-S-T1381 ,-S (O)-T1382 ,-S (O ₂)-T1383 ,-S (O ₂) NH-T1384 ,-S (O ₂) NT1385T1386 ,-S (O ₂) O-T1387 ,-P (O) is (OT1389) (OT1388), and-Si (T1390) is (T1392) (T1391) ";

T1341 wherein, T1342, T1343, T1344, T1345, T1346, T1347, T1348, T1349, T1350, T1351; T1352, T1353, T1354, T1355, T1356, T1357, T1358, T1359, T1360, T1361, T1362; T1363, T1364, T1365, T1366, T1367, T1368, T1369, T1370, T1371, T1372, T1373; T1374, T1375, T1376, T1377, T1378, T1379, T1380, T1381, T1382, T1383; T1384, T1385, T1386, T1387, T1388, T1389, T1390, T1391, T1392 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, T1347, T1348 and/or T1356; T1357 and/or T1369, T1370 and/or T1376, T1377 and/or T1385, T1386 also can form " heterocyclic radical " in each case together;

(iii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHT1393 ,-NT1394T1395 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-T1396 ,-C (O) O-T1397 ,-C (O) NH-T1398 ,-C (O) NT1399T1400 ,-O-T1401 ,-O are (T1402-O) _Rt-H (rt=1,2,3,4,5) ,-O (T1403-O) _Rt-T1404 (rt=1,2,3,4,5) ,-OC (O)-T1405 ,-OC (O)-O-T1406 ,-OC (O)-NHT1407 ,-O-C (O)-NT1408T1409 ,-OP (O) is (OT1411) (OT1410), and-OSi (T1412) is (T1414) (T1413) ,-OS (O ₂)-T1415 ,-NHC (O)-T1416 ,-NT1417C (O)-T1418 ,-NH-C (O)-O-T1419;-NH-C (O)-NH-T1420 ,-NH-C (O)-NT1421T1422 ,-NT1423-C (O)-O-T1424;-NT1425-C (O)-NH-T1426 ,-NT1427-C (O)-NT1428T1429 ,-NHS (O ₂)-T1430 ,-NT1431S (O ₂)-T1432 ,-S-T1433 ,-S (O)-T1434 ,-S (O ₂)-T1435 ,-S (O ₂) NH-T1436 ,-S (O ₂) NT1437T1438 ,-S (O ₂) O-T1439 ,-P (O) is (OT1441) (OT1440), and-Si (T1442) is (T1444) (T1443) ";

T1393 wherein, T1394, T1395, T1396, T1397, T1398, T1399, T1400, T1401, T1402, T1403; T1404, T1405, T1406, T1407, T1408, T1409, T1410, T1411, T1412, T1413, T1414; T1415, T1416, T1417, T1418, T1419, T1420, T1421, T1422, T1423, T1424, T1425; T1426, T1427, T1428, T1429, T1430, T1431, T1432, T1433, T1434, T1435; T1436, T1437, T1438, T1439, T1440, T1441, T1442, T1443, T1444 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, T1399, T1400 and/or T1408; T1409 and/or T1421, T1422 and/or T1428, T1429 and/or T1437, T1438 also can form " heterocyclic radical " in each case together;

(2)“-C(O)-C(O)-T1445，-S(O ₂)-NT1446T1447”；

T1445 wherein, T1446, T1447 is selected from independently of one another:

(I) " hydrogen, alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHT1448 ,-NT1449T1450 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-T1451 ,-C (O) O-T1452 ,-C (O) NH-T1453 ,-C (O) NT1454T1455 ,-O-T1456 ,-O are (T1457-O) _Ru-H (ru=1,2,3,4,5) ,-O (T1458-O) _Ru-T1459 (ru=1,2,3,4,5) ,-OC (O)-T1460 ,-OC (O)-O-T1461 ,-OC (O)-NHT1462 ,-O-C (O)-NT1463T1464 ,-OP (O) is (OT1466) (OT1465), and-OSi (T1467) is (T1469) (T1468) ,-OS (O ₂)-T1470 ,-NHC (O)-T1471 ,-NT1472C (O)-T1473 ,-NH-C (O)-O-T1474;-NH-C (O)-NH-T1475 ,-NH-C (O)-NT1476T1477 ,-NT1478-C (O)-O-T1479;-NT1480-C (O)-NH-T1481 ,-NT1482-C (O)-NT1483T1484 ,-NHS (O ₂)-T1485 ,-NT1486S (O ₂)-T1487 ,-S-T1488 ,-S (O)-T1489 ,-S (O ₂)-T1490 ,-S (O ₂) NH-T1491 ,-S (O ₂) NT1492T1493 ,-S (O ₂) O-T1494 ,-P (O) is (OT1496) (OT1495), and-Si (T1497) is (T1499) (T1498) ";

T1448 wherein, T1449, T1450, T1451, T1452, T1453, T1454, T1455, T1456, T1457, T1458; T1459, T1460, T1461, T1462, T1463, T1464, T1465, T1466, T1467, T1468, T1469; T1470, T1471, T1472, T1473, T1474, T1475, T1476, T1477, T1478, T1479, T1480; T1481, T1482, T1483, T1484, T1485, T1486, T1487, T1488, T1489, T1490; T1491, T1492, T1493, T1494, T1495, T1496, T1497, T1498, T1499 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, T1454, T1455 and/or T1463; T1464 and/or T1476, T1477 and/or T1483, T1484 and/or T1492, T1493 also can form " heterocyclic radical " in each case together;

(i) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHT1500 ,-NT1501T1502 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-T1503 ,-C (O) O-T1504 ,-C (O) NH-T1505 ,-C (O) NT1506T1507 ,-O-T1508 ,-O are (T1509-O) _Rv-H (rv=1,2,3,4,5) ,-O (T1510-O) _Rv-T1511 (rv=1,2,3,4,5) ,-OC (O)-T1512 ,-OC (O)-O-T1513 ,-OC (O)-NHT1514 ,-O-C (O)-NT1515T1516 ,-OP (O) is (OT1518) (OT1517), and-OSi (T1519) is (T1521) (T1520) ,-OS (O ₂)-T1522 ,-NHC (O)-T1523 ,-NT1524C (O)-T1525 ,-NH-C (O)-O-T1526;-NH-C (O)-NH-T1527 ,-NH-C (O)-NT1528T1529 ,-NT1530-C (O)-O-T1531;-NT1532-C (O)-NH-T1533 ,-NT1534-C (O)-NT1535T1536 ,-NHS (O ₂)-T1537 ,-NT1538S (O ₂)-T1539 ,-S-T1540 ,-S (O)-T1541 ,-S (O ₂)-T1542 ,-S (O ₂) NH-T1543 ,-S (O ₂) NT1544T1545 ,-S (O ₂) O-T1546 ,-P (O) is (OT1548) (OT1547), and-Si (T1549) is (T1551) (T1550) ";

T1500 wherein, T1501, T1502, T1503, T1504, T1505, T1506, T1507, T1508, T1509, T1510; T1511, T1512, T1513, T1514, T1515, T1516, T1517, T1518, T1519, T1520, T1521; T1522, T1523, T1524, T1525, T1526, T1527, T1528, T1529, T1530, T1531, T1532; T1533, T1534, T1535, T1536, T1537, T1538, T1539, T1540, T1541, T1542; T1543, T1544, T1545, T1546, T1547, T1548, T1549, T1550, T1551 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, T1506, T1507 and/or T1515; T1516 and/or T1528, T1529 and/or T1535, T1536 and/or T1544, T1545 also can form " heterocyclic radical " in each case together;

(ii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHT1552 ,-NT1553T1554 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-T1555 ,-C (O) O-T1556 ,-C (O) NH-T1557 ,-C (O) NT1558T1559 ,-O-T1560 ,-O are (T1561-O) _Rw-H (rw=1,2,3,4,5) ,-O (T1562-O) _Rw-T1563 (rw=1,2,3,4,5) ,-OC (O)-T1564 ,-OC (O)-O-T1565 ,-OC (O)-NHT1566 ,-O-C (O)-NT1567T1568 ,-OP (O) is (OT1570) (OT1569), and-OSi (T1571) is (T1573) (T1572) ,-OS (O ₂)-T1574 ,-NHC (O)-T1575 ,-NT1576C (O)-T1577 ,-NH-C (O)-O-T1578;-NH-C (O)-NH-T1579 ,-NH-C (O)-NT1580T1581 ,-NT1582-C (O)-O-T1583;-NT1584-C (O)-NH-T1585 ,-NT1586-C (O)-NT1587T1588 ,-NHS (O ₂)-T1589 ,-NT1590S (O ₂)-T1591 ,-S-T1592 ,-S (O)-T1593 ,-S (O ₂)-T1594 ,-S (O ₂) NH-T1595 ,-S (O ₂) NT1596T1597 ,-S (O ₂) O-T1598 ,-P (O) is (OT1600) (OT1599), and-Si (T1601) is (T1603) (T1602) ";

T1552 wherein, T1553, T1554, T1555, T1556, T1557, T1558, T1559, T1560, T1561, T1562; T1563, T1564, T1565, T1566, T1567, T1568, T1569, T1570, T1571, T1572, T1573; T1574, T1575, T1576, T1577, T1578, T1579, T1580, T1581, T1582, T1583, T1584; T1585, T1586, T1587, T1588, T1589, T1590, T1591, T1592, T1593, T1594; T1595, T1596, T1597, T1598, T1599, T1600, T1601, T1602, T1603 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, T1558, T1559 and/or T1567; T1568 and/or T1580, T1581 and/or T1587, T1588 and/or T1596, T1597 also can form " heterocyclic radical " in each case together;

(iii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHT1604 ,-NT1605T1606 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-T1607 ,-C (O) O-T1608 ,-C (O) NH-T1609 ,-C (O) NT1610T1611 ,-O-T1612 ,-O are (T1613-O) _Rx-H (rx=1,2,3,4,5) ,-O (T1614-O) _Rx-T1615 (rx=1,2,3,4,5) ,-OC (O)-T1616 ,-OC (O)-O-T1617 ,-OC (O)-NHT1618 ,-O-C (O)-NT1619T1620 ,-OP (O) is (OT1622) (OT1621), and-OSi (T1623) is (T1625) (T1624) ,-OS (O ₂)-T1626 ,-NHC (O)-T1627 ,-NT1628C (O)-T1629 ,-NH-C (O)-O-T1630;-NH-C (O)-NH-T1631 ,-NH-C (O)-NT1632T1633 ,-NT1634-C (O)-O-T1635;-NT1636-C (O)-NH-T1637 ,-NT1638-C (O)-NT1639T1640 ,-NHS (O ₂)-T1641 ,-NT1642S (O ₂)-T1643 ,-S-T1644 ,-S (O)-T1645 ,-S (O ₂)-T1646 ,-S (O ₂) NH-T1647 ,-S (O ₂) NT1648T1649 ,-S (O ₂) O-T1650 ,-P (O) is (OT1652) (OT1651), and-Si (T1653) is (T1655) (T1654) ";

T1604 wherein, T1605, T1606, T1607, T1608, T1609, T1610, T1611, T1612, T1613, T1614; T1615, T1616, T1617, T1618, T1619, T1620, T1621, T1622, T1623, T1624, T1625; T1626, T1627, T1628, T1629, T1630, T1631, T1632, T1633, T1634, T1635, T1636; T1637, T1638, T1639, T1640, T1641, T1642, T1643, T1644, T1645, T1646; T1647, T1648, T1649, T1650, T1651, T1652, T1653, T1654, T1655 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, T1610, T1611 and/or T1619; T1620 and/or T1632, T1633 and/or T1639, T1640 and/or T1648, T1649 also can form " heterocyclic radical " in each case together;

Wherein, perhaps, T1446, T1447 also can form " heterocyclic radical " together;

(3)“-C(Y8)NZ43Z44，-C(＝NZ45)-Z46，-C(Y9)NZ47-Y10-Z48”；

Y8 wherein, Y9, Y10 be selected from independently of one another " O, S ,=NH ,=NZ49 "

Wherein said Z43, Z44, Z45, Z46, Z47, Z48, the Z49 group is selected from independently of one another:

Wherein randomly, the above-mentioned substituting group of substituting group group (I) also can be selected from following substituting group replacement by at least one independently of one another identically or differently:

(i) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHT1656 ,-NT1657T1658 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-T1659 ,-C (O) O-T1660 ,-C (O) NH-T1661 ,-C (O) NT1662T1663 ,-O-T1664 ,-O are (T1665-O) _Ry-H (ry=1,2,3,4,5) ,-O (T1666-O) _Ry-T1667 (ry=1,2,3,4,5) ,-OC (O)-T1668 ,-OC (O)-O-T1669 ,-OC (O)-NHT1670 ,-O-C (O)-NT1671T1672 ,-OP (O) is (OT1674) (OT1673), and-OSi (T1675) is (T1677) (T1676) ,-OS (O ₂)-T1678 ,-NHC (O)-T1679 ,-NT1680C (O)-T1681 ,-NH-C (O)-O-T1682;-NH-C (O)-NH-T1683 ,-NH-C (O)-NT1684T1685 ,-NT1686-C (O)-O-T1687;-NT1688-C (O)-NH-T1689 ,-NT1690-C (O)-NT1691T1692 ,-NHS (O ₂)-T1693 ,-NT1694S (O ₂)-T1695 ,-S-T1696 ,-S (O)-T1697 ,-S (O ₂)-T1698 ,-S (O ₂) NH-T1699 ,-S (O ₂) NT1700T1701 ,-S (O ₂) O-T1702 ,-P (O) is (OT1704) (OT1703), and-Si (T1705) is (T1707) (T1706) ";

T1656 wherein, T1657, T1658, T1659, T1660, T1661, T1662, T1663, T1664, T1665, T1666; T1667, T1668, T1669, T1670, T1671, T1672, T1673, T1674, T1675, T1676, T1677; T1678, T1679, T1680, T1681, T1682, T1683, T1684, T1685, T1686, T1687, T1688; T1689, T1690, T1691, T1692, T1693, T1694, T1695, T1696, T1697, T1698; T1699, T1700, T1701, T1702, T1703, T1704, T1705, T1706, T1707 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, T1662, T1663 and/or T1671; T1672 and/or T1684, T1685 and/or T1691, T1692 and/or T1700, T1701 also can form " heterocyclic radical " in each case together;

Wherein randomly, the above-mentioned substituting group of substituting group group (i) also can so that independently of one another by at least one identical ground or different are selected from following substituting group and further replace:

(ii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHT1708 ,-NT1709T1710 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-T1711 ,-C (O) O-T1712 ,-C (O) NH-T1713 ,-C (O) NT1714T1715 ,-O-T1716 ,-O are (T1717-O) _Rz-H (rz=1,2,3,4,5) ,-O (T1718-O) _Rz-T1719 (rz=1,2,3,4,5) ,-OC (O)-T1720 ,-OC (O)-O-T1721 ,-OC (O)-NHT1722 ,-O-C (O)-NT1723T1724 ,-OP (O) is (OT1726) (OT1725), and-OSi (T1727) is (T1729) (T1728) ,-OS (O ₂)-T1730 ,-NHC (O)-T1731 ,-NT1732C (O)-T1733 ,-NH-C (O)-O-T1734;-NH-C (O)-NH-T1735 ,-NH-C (O)-NT1736T1737 ,-NT1738-C (O)-O-T1739;-NT1740-C (O)-NH-T1741 ,-NT1742-C (O)-NT1743T1744 ,-NHS (O ₂)-T1745 ,-NT1746S (O ₂)-T1747 ,-S-T1748 ,-S (O)-T1749 ,-S (O ₂)-T1750 ,-S (O ₂) NH-T1751 ,-S (O ₂) NT1752T1753 ,-S (O ₂) O-T1754 ,-P (O) is (OT1756) (OT1755), and-Si (T1757) is (T1759) (T1758) ";

T1708 wherein, T1709, T1710, T1711, T1712, T1713, T1714, T1715, T1716, T1717, T1718; T1719, T1720, T1721, T1722, T1723, T1724, T1725, T1726, T1727, T1728, T1729; T1730, T1731, T1732, T1733, T1734, T1735, T1736, T1737, T1738, T1739, T1740; T1741, T1742, T1743, T1744, T1745, T1746, T1747, T1748, T1749, T1750; T1751, T1752, T1753, T1754, T1755, T1756, T1757, T1758, T1759 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, T1714, T1715 and/or T1723; T1724 and/or T1736, T1737 and/or T1743, T1744 and/or T1752, T1753 also can form " heterocyclic radical " in each case together;

(iii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHT1760 ,-NT1761T1762 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-T1763 ,-C (O) O-T1764 ,-C (O) NH-T1765 ,-C (O) NT1766T1767 ,-O-T1768 ,-O are (T1769-O) _Ra-H (ra=1,2,3,4,5) ,-O (T1770-O) _Ra-T1771 (ra=1,2,3,4,5) ,-OC (O)-T1772 ,-OC (O)-O-T1773 ,-OC (O)-NHT1774 ,-O-C (O)-NT1775T1776 ,-OP (O) is (OT1778) (OT1777), and-OSi (T1779) is (T1781) (T1780) ,-OS (O ₂)-T1782 ,-NHC (O)-T1783 ,-NT1784C (O)-T1785 ,-NH-C (O)-O-T1786;-NH-C (O)-NH-T1787 ,-NH-C (O)-NT1788T1789 ,-NT1790-C (O)-O-T1791;-NT1792-C (O)-NH-T1793 ,-NT1794-C (O)-NT1795T1796 ,-NHS (O ₂)-T1797 ,-NT1798S (O ₂)-T1799 ,-S-T1800 ,-S (O)-T1801 ,-S (O ₂)-T1802 ,-S (O ₂) NH-T1803 ,-S (O ₂) NT1804T1805 ,-S (O ₂) O-T1806 ,-P (O) is (OT1808) (OT1807), and-Si (T1809) is (T1811) (T1810) ";

T1760 wherein, T1761, T1762, T1763, T1764, T1765, T1766, T1767, T1768, T1769, T1770; T1771, T1772, T1773, T1774, T1775, T1776, T1777, T1778, T1779, T1780, T1781; T1782, T1783, T1784, T1785, T1786, T1787, T1788, T1789, T1790, T1791, T1792; T1793, T1794, T1795, T1796, T1797, T1798, T1799, T1800, T1801, T1802; T1803, T1804, T1805, T1806, T1807, T1808, T1809, T1810, T1811 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, T1766, T1767 and/or T1775; T1776 and/or T1788, T1789 and/or T11795, T1796 and/or T1804, T1805 also can form " heterocyclic radical " in each case together;

And

Said Z3, Z4 group are selected from independently of one another:

(e) hydrogen;

(f) halogen, F, Cl, Br, I;

(i) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHB457 ,-NB458B459 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-B460 ,-C (O) O-B461 ,-C (O) NH-B462 ,-C (O) NB463B464 ,-O-B465 ,-O are (B466-O) _x-H (x=1,2,3,4,5) ,-O (B467-O) _x-B468 (x=1,2,3,4,5) ,-OC (O)-B469 ,-OC (O)-O-B470 ,-OC (O)-NHB471 ,-O-C (O)-NB472B473 ,-OP (O) is (OB475) (OB474), and-OSi (B476) is (B478) (B477) ,-OS (O ₂)-B479 ,-NHC (O)-B480 ,-NB481C (O)-B482 ,-NH-C (O)-O-B483 ,-NH-C (O)-NH-B484 ,-NH-C (O)-NB485B486 ,-NB487-C (O)-O-B488 ,-NB489-C (O)-NH-B490 ,-NB491-C (O)-NB492B493 ,-NHS (O ₂)-B494 ,-NB495S (O ₂)-B496 ,-S-B497 ,-S (O)-B498 ,-S (O ₂)-B499 ,-S (O ₂) NH-B500 ,-S (O ₂) NB501B502 ,-S (O ₂) O-B503 ,-P (O) is (OB505) (OB504), and-Si (B506) is (B508) (B507) ";

B457 wherein, B458, B459, B460, B461, B462, B463, B464, B465, B466, B467, B468, B469, B470; B471, B472, B473, B474, B475, B476, B477, B478, B479, B480, B481, B482, B483; B484, B485, B486, B487, B488, B489, B490, B491, B492, B493, B494, B495, B496; B497, B498, B499, B500, B501, B502, B503, B504, B505, B506, B507, B508 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, B463, B464 and/or B472; B473 and/or B485, B486 and/or B492, B493 and/or B501, B502 also can form " heterocyclic radical " in each case together;

(ii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHB509 ,-NB510B511 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-B512 ,-C (O) O-B513 ,-C (O) NH-B514 ,-C (O) NB515B516 ,-O-B517 ,-O are (B518-O) _y-H (y=1,2,3,4,5) ,-O (B519-O) _y-B520 (y=1,2,3,4,5) ,-OC (O)-B 521 ,-OC (O)-O-B522 ,-OC (O)-NHB523 ,-O-C (O)-NB524B525 ,-OP (O) is (OB527) (OB526), and-OSi (B528) is (B530) (B529) ,-OS (O ₂)-B531 ,-NHC (O)-B532 ,-NB533C (O)-B534 ,-NH-C (O)-O-B535 ,-NH-C (O)-NH-B536 ,-NH-C (O)-NB537B538 ,-NB539-C (O)-O-B540 ,-NB541-C (O)-NH-B542 ,-NB543-C (O)-NB544B545 ,-NHS (O ₂)-B546 ,-NB547S (O ₂)-B548 ,-S-B549 ,-S (O)-B550 ,-S (O ₂)-B551 ,-S (O ₂) NH-B552 ,-S (O ₂) NB553B554 ,-S (O ₂) O-B555 ,-P (O) is (OB557) (OB556), and-Si (B558) is (B560) (B559) ";

B509 wherein, B510, B511, B512, B513, B514, B515, B516, B517, B518, B519, B520, B521, B522; B523, B524, B525, B526, B527, B528, B529, B530, B531, B532, B533, B534, B535; B536, B537, B538, B539, B540, B541, B542, B543, B544, B545, B546, B547, B548; B549, B550, B551, B552, B553, B554, B555, B556, B557, B558, B559, B560 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, B515, B516 and/or B524; B525 and/or B537, B538 and/or B544, B545 and/or B553, B554 also can form " heterocyclic radical " in each case together;

(iii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF3, N ₃, NH ₂,-NHB561 ,-NB562B563 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-B564 ,-C (O) O-B565 ,-C (O) NH-B566 ,-C (O) NB567B568 ,-O-B569 ,-O are (B570-O) _z-H (z=1,2,3,4,5) ,-O (B571-O) _z-B572 (z=1,2,3,4,5) ,-OC (O)-B573 ,-OC (O)-O-B574 ,-OC (O)-NHB575 ,-O-C (O)-NB576B577 ,-OP (O) is (OB579) (OB578), and-OSi (B580) is (B582) (B581) ,-OS (O ₂)-B583 ,-NHC (O)-B584 ,-NB585C (O)-B586 ,-NH-C (O)-O-B587 ,-NH-C (O)-NH-B588 ,-NH-C (O)-NB589B590 ,-NB591-C (O)-O-B592 ,-NB593-C (O)-NH-B594 ,-NB595-C (O)-NB596B597 ,-NHS (O ₂)-B598 ,-NB599S (O ₂)-B600 ,-S-B601 ,-S (O)-B602 ,-S (O ₂)-B603 ,-S (O ₂) NH-B604 ,-S (O ₂) NB605B606 ,-S (O ₂) O-B607 ,-P (O) is (OB609) (OB608), and-Si (B610) is (B612) (B611) ";

B561 wherein, B562, B563, B564, B565, B566, B567, B568, B569, B570, B571, B572, B573, B574; B575, B576, B577, B578, B579, B580, B581, B582, B583, B584, B585, B586, B587; B588, B589, B590, B591, B592, B593, B594, B595, B596, B597, B598, B599, B600; B601, B602, B603, B604, B605, B606, B607, B608, B609, B610, B611, B612 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, B567, B568 and/or B576; B577 and/or B589, B590 and/or B596, B597 and/or B605, B606 also can form " heterocyclic radical " in each case together;

(i) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHB613 ,-NB614B615 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-B616 ,-C (O) O-B617 ,-C (O) NH-B618 ,-C (O) NB619B620 ,-O-B621 ,-O are (B622-O) _a-H (a=1,2,3,4,5) ,-O (B623-O) _a-B624 (a=1,2,3,4,5) ,-OC (O)-B625 ,-OC (O)-O-B626 ,-OC (O)-NHB627 ,-O-C (O)-NB628B629 ,-OP (O) is (OB631) (OB630), and-OSi (B632) is (B634) (B633) ,-OS (O ₂)-B635 ,-NHC (O)-B636 ,-NB637C (O)-B638 ,-NH-C (O)-O-B639 ,-NH-C (O)-NH-B640 ,-NH-C (O)-NB641B642 ,-NB643-C (O)-O-B644 ,-NB645-C (O)-NH-B646 ,-NB647-C (O)-NB648B649 ,-NHS (O ₂)-B650 ,-NB651S (O ₂)-B652 ,-S-B653 ,-S (O)-B654 ,-S (O ₂)-B655 ,-S (O ₂) NH-B656 ,-S (O ₂) NB657B658 ,-S (O ₂) O-B659 ,-P (O) is (OB661) (OB660), and-Si (B662) is (B664) (B663) ";

B613 wherein, B614, B615, B616, B617, B618, B619, B620, B621, B622, B623, B624, B625, B626; B627, B628, B629, B630, B631, B632, B633, B634, B635, B636, B637, B638, B639; B640, B641, B642, B643, B644, B645, B646, B647, B648, B649, B650, B651, B652; B653, B654, B655, B656, B657, B658, B659, B660, B661, B662, B663, B664 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, B619, B620 and/or B628; B629 and/or B641, B642 and/or B648, B649 and/or B657, B658 also can form " heterocyclic radical " in each case together;

(ii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHB665 ,-NB666B667 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-B668 ,-C (O) O-B669 ,-C (O) NH-B670 ,-C (O) NB671B672 ,-O-B673 ,-O are (B674-O) _b-H (b=1,2,3,4,5) ,-O (B675-O) _b-B676 (b=1,2,3,4,5) ,-OC (O)-B677 ,-OC (O)-O-B678 ,-OC (O)-NHB679 ,-O-C (O)-NB680B681 ,-OP (O) is (OB683) (OB682), and-OSi (B684) is (B686) (B685) ,-OS (O ₂)-B687 ,-NHC (O)-B688 ,-NB689C (O)-B690 ,-NH-C (O)-O-B691 ,-NH-C (O)-NH-B692 ,-NH-C (O)-NB693B694 ,-NB695-C (O)-O-B696 ,-NB697-C (O)-NH-B698 ,-NB699-C (O)-NB700B701 ,-NHS (O ₂)-B702 ,-NB703S (O ₂)-B704 ,-S-B705 ,-S (O)-B706 ,-S (O ₂)-B707 ,-S (O ₂) NH-B708 ,-S (O ₂) NB709B710 ,-S (O ₂) O-B711 ,-P (O) is (OB713) (OB712), and-Si (B714) is (B716) (B715) ";

B665 wherein, B666, B667, B668, B669, B670, B671, B672, B673, B674, B675, B676, B677, B678; B679, B680, B681, B682, B683, B684, B685, B686, B687, B688, B689, B690, B691; B692, B693, B694, B695, B696, B697, B698, B699, B700, B701, B702, B703, B704; B705, B706, B707, B708, B709, B710, B711, B712, B713, B714, B715, B716 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, B671, B672 and/or B680; B681 and/or B693, B694 and/or B700, B701 and/or B709, B710 also can form " heterocyclic radical " in each case together;

(iii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHB717 ,-NB718B719 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-B720 ,-C (O) O-B721 ,-C (O) NH-B722 ,-C (O) NB723B724 ,-O-B725 ,-O are (B726-O) _c-H (c=1,2,3,4,5) ,-O (B727-O) _c-B728 (c=1,2,3,4,5) ,-OC (O)-B729 ,-OC (O)-O-B730 ,-OC (O)-NHB731 ,-O-C (O)-NB732B733 ,-OP (O) is (OB735) (OB734), and-OSi (B736) is (B738) (B737) ,-OS (O ₂)-B739 ,-NHC (O)-B740 ,-NB741C (O)-B742 ,-NH-C (O)-O-B743 ,-NH-C (O)-NH-B744 ,-NH-C (O)-NB745B746 ,-NB747-C (O)-O-B748 ,-NB749-C (O)-NH-B750 ,-NB751-C (O)-NB752B753 ,-NHS (O ₂)-B754 ,-NB755S (O ₂)-B756 ,-S-B757 ,-S (O)-B758 ,-S (O ₂)-B759 ,-S (O ₂) NH-B760 ,-S (O ₂) NB761B762 ,-S (O ₂) O-B763 ,-P (O) is (OB765) (OB764), and-Si (B766) is (B768) (B767) ";

B717 wherein, B718, B719, B720, B721, B722, B723, B724, B725, B726, B727, B728, B729, B730; B731, B732, B733, B734, B735, B736, B737, B738, B739, B740, B741, B742, B743; B744, B745, B746, B747, B748, B749, B750, B751, B752, B753, B754, B755, B756; B757, B758, B759, B760, B761, B762, B763, B764, B765, B766, B767, B768 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, B723, B724 and/or B732; B733 and/or B745, B746 and/or B752, B753 and/or B761, B762 also can form " heterocyclic radical " in each case together;

(i) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHB769 ,-NB770B771 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-B772 ,-C (O) O-B773 ,-C (O) NH-B774 ,-C (O) NB775B776 ,-O-B777 ,-O are (B778-O) _d-H (d=1,2,3,4,5) ,-O (B779-O) _d-B780 (d=1,2,3,4,5) ,-OC (O)-B781 ,-OC (O)-O-B782 ,-OC (O)-NHB783 ,-O-C (O)-NB784B785 ,-OP (O) is (OB787) (OB786), and-OSi (B788) is (B790) (B789) ,-OS (O ₂)-B791 ,-NHC (O)-B792 ,-NB793C (O)-B794 ,-NH-C (O)-O-B795 ,-NH-C (O)-NH-B796 ,-NH-C (O)-NB797B798 ,-NB799-C (O)-O-B800 ,-NB801-C (O)-NH-B802 ,-NB803-C (O)-NB804B805 ,-NHS (O ₂)-B806 ,-NB807S (O ₂)-B808 ,-S-B809 ,-S (O)-B810 ,-S (O ₂)-B811 ,-S (O ₂) NH-B812 ,-S (O ₂) NB813B814 ,-S (O ₂) O-B815 ,-P (O) is (OB817) (OB816), and-Si (B818) is (B820) (B819) ";

B769 wherein, B770, B771, B772, B773, B774, B775, B776, B777, B778, B779, B780, B781, B782; B783, B784, B785, B786, B787, B788, B789, B790, B791, B792, B793, B794, B795; B796, B797, B798, B799, B800, B801, B802, B803, B804, B805, B806, B807, B808; B809, B810, B811, B812, B813, B814, B815, B816, B817, B818, B819, B820 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, B775, B776 and/or B784; B785 and/or B797, B798 and/or B804, B805 and/or B813, B814 also can form " heterocyclic radical " in each case together;

(ii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHB821 ,-NB822B823 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-B824 ,-C (O) O-B825 ,-C (O) NH-B826 ,-C (O) NB827B828 ,-O-B829 ,-O are (B830-O) _e-H (e=1,2,3,4,5) ,-O (B831-O) _e-B832 (e=1,2,3,4,5) ,-OC (O)-B833 ,-OC (O)-O-B834 ,-OC (O)-NHB835 ,-O-C (O)-NB836B837 ,-OP (O) is (OB839) (OB838), and-OSi (B840) is (B842) (B841) ,-OS (O ₂)-B843 ,-NHC (O)-B844 ,-NB845C (O)-B846 ,-NH-C (O)-O-B847 ,-NH-C (O)-NH-B848 ,-NH-C (O)-NB849B850 ,-NB851-C (O)-O-B852 ,-NB853-C (O)-NH-B854 ,-NB855-C (O)-NB856B857 ,-NHS (O ₂)-B858 ,-NB859S (O ₂)-B860 ,-S-B861 ,-S (O)-B862 ,-S (O ₂)-B863 ,-S (O ₂) NH-B864 ,-S (O ₂) NB865B866 ,-S (O ₂) O-B867 ,-P (O) is (OB869) (OB868), and-Si (B870) is (B872) (B871) ";

B821 wherein, B822, B823, B824, B825, B826, B827, B828, B829, B830, B831, B832, B833, B834; B835, B836, B837, B838, B839, B840, B841, B842, B843, B844, B845, B846, B847; B848, B849, B850, B851, B852, B853, B854, B855, B856, B857, B858, B859, B860; B861, B862, B863, B864, B865, B866, B867, B868, B869, B870, B871, B872 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, B827, B828 and/or B836; B837 and/or B849, B850 and/or B856, B857 and/or B865, B866 also can form " heterocyclic radical " in each case together;

(iii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHB873 ,-NB874B875 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-B876 ,-C (O) O-B877 ,-C (O) NH-B878 ,-C (O) NB879B880 ,-O-B881 ,-O are (B882-O) _f-H (f=1,2,3,4,5) ,-O (B883-O) _f-B884 (f=1,2,3,4,5) ,-OC (O)-B885 ,-OC (O)-O-B886 ,-OC (O)-NHB887 ,-O-C (O)-NB888B889 ,-OP (O) is (OB891) (OB890), and-OSi (B892) is (B894) (B893) ,-OS (O ₂)-B895 ,-NHC (O)-B896 ,-NB897C (O)-B898 ,-NH-C (O)-O-B899 ,-NH-C (O)-NH-B900 ,-NH-C (O)-NB901B902 ,-NB903-C (O)-O-B904 ,-NB905-C (O)-NH-B906 ,-NB907-C (O)-NB908B909 ,-NHS (O ₂)-B910 ,-NB911S (O ₂)-B912 ,-S-B913 ,-S (O)-B914 ,-S (O ₂)-B915 ,-S (O ₂) NH-B916 ,-S (O ₂) NB917B918 ,-S (O ₂) O-B919 ,-P (O) is (OB921) (OB920), and-Si (B922) is (B924) (B923) ";

B873 wherein, B874, B875, B876, B877, B878, B879, B880, B881, B882, B883, B884, B885, B886; B887, B888, B889, B890, B891, B892, B893, B894, B895, B896, B897, B898, B899; B900, B901, B902, B903, B904, B905, B906, B907, B908, B909, B910, B911, B912; B913, B914, B915, B916, B917, B918, B919, B920, B921, B922, B923, B924 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, B879, B880 and/or B888; B889 and/or B901, B902 and/or B908, B909 and/or B917, B918 also can form " heterocyclic radical " in each case together;

(k) OZ6, wherein Z6 is independently selected from:

(ii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHB925 ,-NB926B927 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-B928 ,-C (O) O-B929 ,-C (O) NH-B930 ,-C (O) NB931B932 ,-O-B933 ,-O are (B934-O) _g-H (g=1,2,3,4,5) ,-O (B935-O) _g-B936 (g=1,2,3,4,5) ,-OC (O)-B937 ,-OC (O)-O-B938 ,-OC (O)-NHB939 ,-O-C (O)-NB940B941 ,-OP (O) is (OB943) (OB942), and-OSi (B944) is (B946) (B945) ,-OS (O ₂)-B947 ,-NHC (O)-B948 ,-NB949C (O)-B950 ,-NH-C (O)-O-B951 ,-NH-C (O)-NH-B952 ,-NH-C (O)-NB953B954 ,-NB955-C (O)-O-B956 ,-NB957-C (O)-NH-B958 ,-NB959-C (O)-NB960B961 ,-NHS (O ₂)-B962 ,-NB963S (O ₂)-B964 ,-S-B965 ,-S (O)-B966 ,-S (O ₂)-B967 ,-S (O ₂) NH-B968 ,-S (O ₂) NB969B970 ,-S (O ₂) O-B971 ,-P (O) is (OB973) (OB972), and-Si (B974) is (B976) (B975) ";

B925 wherein, B926, B927, B928, B929, B930, B931, B932, B933, B934, B935, B936, B937, B938; B939, B940, B941, B942, B943, B944, B945, B946, B947, B948, B949, B950, B951; B952, B953, B954, B955, B956, B957, B958, B959, B960, B961, B962, B963, B964; B965, B966, B967, B968, B969, B970, B971, B972, B973, B974, B975, B976 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, B931, B932 and/or B940; B941 and/or B953, B954 and/or B960, B961 and/or B969, B970 also can form " heterocyclic radical " in each case together;

(iii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHB977 ,-NB978B979 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-B980 ,-C (O) O-B981 ,-C (O) NH-B982 ,-C (O) NB983B984 ,-O-B985 ,-O are (B986-O) _h-H (h=1,2,3,4,5) ,-O (B987-O) _h-B988 (h=1,2,3,4,5) ,-OC (O)-B989 ,-OC (O)-O-B990 ,-OC (O)-NHB991 ,-O-C (O)-NB992B993 ,-OP (O) is (OB995) (OB994), and-OSi (B996) is (B998) (B997) ,-OS (O ₂)-B999 ,-NHC (O)-B1000 ,-NB1001C (O)-B1002 ,-NH-C (O)-O-B1003;-NH-C (O)-NH-B1004 ,-NH-C (O)-NB1005B1006 ,-NB1007-C (O)-O-B1008;-NB1009-C (O)-NH-B1010 ,-NB1011-C (O)-NB1012B1013 ,-NHS (O ₂)-B1014 ,-NB1015S (O ₂)-B1016 ,-S-B1017 ,-S (O)-B1018 ,-S (O ₂)-B1019 ,-S (O ₂) NH-B1020 ,-S (O ₂) NB1021B1022 ,-S (O ₂) O-B1023 ,-P (O) is (OB1025) (OB1024), and-Si (B1026) is (B1028) (B1027) ";

B977 wherein, B978, B979, B980, B981, B982, B983, B984, B985, B986, B987; B988, B989, B990, B991, B992, B993, B994, B995, B996, B997, B998; B999, B1000, B1001, B1002, B1003, B1004, B1005, B1006, B1007, B1008, B1009; B1010, B1011, B1012, B1013, B1014, B1015, B1016, B1017, B1018, B1019; B1020, B1021, B1022, B1023, B1024, B1025, B1026, B1027, B1028 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, B983, B984 and/or B992; B993 and/or B1005, B1006 and/or B1012, B1013 and/or B1021, B1022 also can form " heterocyclic radical " in each case together;

(1) SZ7, wherein Z7 is independently selected from:

(ii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHB1029 ,-NB1030B1031 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-B1032 ,-C (O) O-B1033 ,-C (O) NH-B1034 ,-C (O) NB1035B1036 ,-O-B1037 ,-O are (B1038-O) _i-H (i=1,2,3,4,5) ,-O (B1039-O) _i-B1040 (i=1,2,3,4,5) ,-OC (O)-B1041 ,-OC (O)-O-B1042 ,-OC (O)-NHB1043 ,-O-C (O)-NB1044B1045 ,-OP (O) is (OB1047) (OB1046), and-OSi (B1048) is (B1050) (B1049) ,-OS (O ₂)-B1051 ,-NHC (O)-B1052 ,-NB1053C (O)-B1054 ,-NH-C (O)-O-B1055;-NH-C (O)-NH-B1056 ,-NH-C (O)-NB1057B1058 ,-NB1059-C (O)-O-B1060;-NB1061-C (O)-NH-B1062 ,-NB1063-C (O)-NB1064B1065 ,-NHS (O ₂)-B1066 ,-NB1067S (O ₂)-B1068 ,-S-B1069 ,-S (O)-B1070 ,-S (O ₂)-B1071 ,-S (O ₂) NH-B1072 ,-S (O ₂) NB1073B1074 ,-S (O ₂) O-B1075 ,-P (O) is (OB1077) (OB1076), and-Si (B1078) is (B1080) (B1079) ";

B1029 wherein, B1030, B1031, B1032, B1033, B1034, B1035, B1036, B1037, B1038, B1039; B1040, B1041, B1042, B1043, B1044, B1045, B1046, B1047, B1048, B1049, B1050; B1051, B1052, B1053, B1054, B1055, B1056, B1057, B1058, B1059, B1060, B1061; B1062, B1063, B1064, B1065, B1066, B1067, B1068, B1069, B1070, B1071; B1072, B1073, B1074, B1075, B1076, B1077, B1078, B1079, B1080 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, B1035, B1036 and/or B1044; B1045 and/or B1057, B1058 and/or B1064, B1065 and/or B1073, B1074 also can form " heterocyclic radical " in each case together;

(iii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHB1081 ,-NB1082B1083 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-B1084 ,-C (O) O-B1085 ,-C (O) NH-B1086 ,-C (O) NB1087B1088 ,-O-B1089 ,-O are (B1090-O) _j-H (j=1,2,3,4,5) ,-O (B1091-O) _j-B1092 (j=1,2,3,4,5) ,-OC (O)-B1093 ,-OC (O)-O-B1094 ,-OC (O)-NHB1095 ,-O-C (O)-NB1096B1097 ,-OP (O) is (OB1099) (OB1098), and-OSi (B1100) is (B1102) (B1101) ,-OS (O ₂)-B1103 ,-NHC (O)-B1104 ,-NB1105C (O)-B1106 ,-NH-C (O)-O-B1107;-NH-C (O)-NH-B1108 ,-NH-C (O)-NB1109B1110 ,-NB1111-C (O)-O-B1112;-NB1113-C (O)-NH-B1114 ,-NB1115-C (O)-NB1116B1117 ,-NHS (O ₂)-B1118 ,-NB1119S (O ₂)-B1120 ,-S-B1121 ,-S (O)-B1122 ,-S (O ₂)-B1123 ,-S (O ₂) NH-B1124 ,-S (O ₂) NB1125B1126 ,-S (O ₂) O-B1127 ,-P (O) is (OB1129) (OB1128), and-Si (B1130) is (B1132) (B1131) ";

B1081 wherein, B1082, B1083, B1084, B1085, B1086, B1087, B1088, B1089, B1090, B1091; B1092, B1093, B1094, B1095, B1096, B1097, B1098, B1099, B1100, B1101, B1102; B1103, B1104, B1105, B1106, B1107, B1108, B1109, B1110, B1111, B1112, B1113; B1114, B1115, B1116, B1117, B1118, B1119, B1120, B1121, B1122, B1123; B1124, B1125, B1126, B1127, B1128, B1129, B1130, B1131, B1132 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, B1087, B1088 and/or B1096; B1097 and/or B1109, B1110 and/or B1116, B1117 and/or B1125, B1126 also can form " heterocyclic radical " in each case together;

(m) NZ8Z9, Z8 wherein, Z9 is selected from independently of one another:

(i) " hydrogen, alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl ,-C (O)-B1133 ,-C (O) O-B1134 ,-C (O)-NB1135B1136 ,-S (O ₂)-B1137 ,-S (O ₂) O-B1138 ";

B1133 wherein, B1134, B1135, B1136, B1137, B1138 is selected from independently of one another: hydrogen, alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl " and wherein, perhaps, B1135, B1136 also can form " heterocyclic radical " together;

(ii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHB1139 ,-NB1140B1141 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-B1142 ,-C (O) O-B1143 ,-C (O) NH-B1144 ,-C (O) NB1145B1146 ,-O-B1147 ,-O are (B1148-O) _k-H (k=1,2,3,4,5) ,-O (B1149-O) _k-B1150 (k=1,2,3,4,5) ,-OC (O)-B1151 ,-OC (O)-O-B1152 ,-OC (O)-NHB1153 ,-O-C (O)-NB1154B1155 ,-OP (O) is (OB1157) (OB1156), and-OSi (B1158) is (B1160) (B1159) ,-OS (O ₂)-B1161 ,-NHC (O)-B1162 ,-NB1163C (O)-B1164 ,-NH-C (O)-O-B1165;-NH-C (O)-NH-B1166 ,-NH-C (O)-NB1167B1168 ,-NB1169-C (O)-O-B1170;-NB1171-C (O)-NH-B1172 ,-NB1173-C (O)-NB1174B1175 ,-NHS (O ₂)-B1176 ,-NB1177S (O ₂)-B1178 ,-S-B1179 ,-S (O)-B1180 ,-S (O ₂)-B1181 ,-S (O ₂) NH-B1182 ,-S (O ₂) NB1183B1184 ,-S (O ₂) O-B1185 ,-P (O) is (OB1187) (OB1186), and-Si (B1188) is (B1190) (B1189) ";

B1139 wherein, B1140, B1141, B1142, B1143, B1144, B1145, B1146, B1147, B1148, B1149; B1150, B1151, B1152, B1153, B1154, B1155, B1156, B1157, B1158, B1159, B1160; B1161, B1162, B1163, B1164, B1165, B1166, B1167, B1168, B1169, B1170, B1171; B1172, B1173, B1174, B1175, B1176, B1177, B1178, B1179, B1180, B1181; B1182, B1183, B1184, B1185, B1186, B1187, B1188, B1189, B1190 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, B1145, B1146 and/or B1154; B1155 and/or B1167, B1168 and/or B1174, B1175 and/or B1183, B1184 also can form " heterocyclic radical " in each case together;

(iii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHB1191 ,-NB1192B1193 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-B1194 ,-C (O) O-B1195 ,-C (O) NH-B1196 ,-C (O) NB1197B1198 ,-O-B1199 ,-O are (B1200-O) _l-H (1=1,2,3,4,5) ,-O (B1201-O) _l-B1202 (1=1,2,3,4,5) ,-OC (O)-B1203 ,-OC (O)-O-B1204 ,-OC (O)-NHB1205 ,-O-C (O)-NB1206B1207 ,-OP (O) is (OB1209) (OB1208), and-OSi (B1210) is (B1212) (B1211) ,-OS (O ₂)-B1213 ,-NHC (O)-B1214 ,-NB1215C (O)-B1216 ,-NH-C (O)-O-B1217;-NH-C (O)-NH-B1218 ,-NH-C (O)-NB1219B1220 ,-NB1221-C (O)-O-B1222;-NB1223-C (O)-NH-B1224 ,-NB1225-C (O)-NB1226B1227 ,-NHS (O ₂)-B1228 ,-NB1229S (O ₂)-B1230 ,-S-B1231 ,-S (O)-B1232 ,-S (O ₂)-B1233 ,-S (O ₂) NH-B1234 ,-S (O ₂) NB1235B1236 ,-S (O ₂) O-B1237 ,-P (O) is (OB1239) (OB1238), and-Si (B1240) is (B1242) (B1241) ";

B1191 wherein, B1192, B1193, B1194, B1195, B1196, B1197, B1198, B1199, B1200, B1201; B1202, B1203, B1204, B1205, B1206, B1207, B1208, B1209, B1210, B1211, B1212; B1213, B1214, B1215, B1216, B1217, B1218, B1219, B1220, B1221, B1222, B1223; B1224, B1225, B1226, B1227, B1228, B1229, B1230, B1231, B1232, B1233; B1234, B1235, B1236, B1237, B1238, B1239, B1240, B1241, B1242 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, B1197, B1198 and/or B1206; B1207 and/or B1219, B1220 and/or B1226, B1227 and/or B1235, B1236 also can form " heterocyclic radical " in each case together;

And

Said Z5 group is independently selected from:

(i) " hydrogen, alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHD1 ,-ND2D3 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-D4 ,-C (O) O-D5 ,-C (O) NH-D6 ,-C (O) ND7D8 ,-O-D9 ,-O are (D10-O) _r-H (r=1,2,3,4,5) ,-O (D11-O) _r-D12 (r=1,2,3,4,5) ,-OC (O)-D13 ,-OC (O)-O-D14 ,-OC (O)-NHD15 ,-O-C (O)-ND16D17 ,-OP (O) is (OD19) (OD18), and-OSi (D20) is (D22) (D21) ,-OS (O ₂)-D23 ,-NHC (O)-D24 ,-ND25C (O)-D26 ,-NH-C (O)-O-D27 ,-NH-C (O)-NH-D28 ,-NH-C (O)-ND29D30 ,-ND31-C (O)-O-D 32 ,-ND33-C (O)-NH-D34 ,-ND35-C (O)-ND36D37 ,-NHS (O ₂)-D38 ,-ND39S (O ₂)-D40 ,-S-D41 ,-S (O)-D42 ,-S (O ₂)-D43 ,-S (O ₂) NH-D44 ,-S (O ₂) ND45D46 ,-S (O ₂) O-D47 ,-P (O) is (OD49) (OD48), and-Si (D50) is (D52) (D51) ";

D1 wherein, D2, D3, D4, D5, D6, D7, D8, D9, D10, D11, D12, D13, D14; D15, D16, D17, D18, D19, D20, D21, D22, D23, D24, D25, D26, D27; D28, D29, D30, D31, D32, D33, D34, D35, D36, D37, D38, D39, D40; D41, D42, D43, D44, D45, D46, D47, D48, D49, D50, D51, D52 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl; Arylalkyl, heteroaryl, heteroarylalkyl " and wherein, perhaps, D7; D8 and/or D16, D17 and/or D29, D30 and/or D36, D37 and/or D45, D46 also can form " heterocyclic radical " in each case together;

(ii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHD53 ,-ND54D55 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-D56 ,-C (O) O-D57 ,-C (O) NH-D58 ,-C (O) ND59D60 ,-O-D61 ,-O are (D62-O) _s-H (s=1,2,3,4,5) ,-O (D63-O) _t-D64 (t=1,2,3,4,5) ,-OC (O)-D65 ,-OC (O)-O-D66 ,-OC (O)-NHD67 ,-O-C (O)-ND68D69 ,-OP (O) is (OD71) (OD70), and-OSi (D72) is (D74) (D73) ,-OS (O ₂)-D75 ,-NHC (O)-D76 ,-ND77C (O)-D78 ,-NH-C (O)-O-D79 ,-NH-C (O)-NH-D80 ,-NH-C (O)-ND81D82 ,-ND83-C (O)-O-D84 ,-ND85-C (O)-NH-D86 ,-ND87-C (O)-ND88D89 ,-NHS (O ₂)-D90 ,-ND91S (O ₂)-D92 ,-S-D93 ,-S (O)-D94 ,-S (O ₂)-D95 ,-S (O ₂) NH-D96 ,-S (O ₂) ND97D98 ,-S (O ₂) O-D99 ,-P (O) is (OD101) (OD100), and-Si (D102) is (D104) (D103) ";

D53 wherein, D54, D55, D56, D57, D58, D59, D60, D61, D62, D63, D64, D65, D66; D67, D68, D69, D70, D71, D72, D73, D74, D75, D76, D77, D78, D79; D80, D81, D82, D83, D84, D85, D86, D87, D88, D89, D90, D91, D92; D93, D94, D95, D96, D97, D98, D99, D100, D101, D102, D103, D104 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, D59, D60 and/or D68; D69 and/or D81, D82 and/or D88, D89 and/or D97, D98 also can form " heterocyclic radical " in each case together;

(iii) " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical, heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF ₃, N ₃, NH ₂,-NHD105 ,-ND106D107 ,-NO ₂,-OH ,-OCF ₃,-SH ,-O-SO ₃H ,-OP (O) (OH) ₂,-CHO ,-COOH ,-C (O) NH ₂,-SO ₃H ,-P (O) (OH) ₂,-C (O)-D108 ,-C (O) O-D109 ,-C (O) NH-D110 ,-C (O) ND111D112 ,-O-D113 ,-O are (D114-O) _t-H (t=1,2,3,4,5) ,-O (D115-O) _t-D116 (t=1,2,3,4,5) ,-OC (O)-D117 ,-OC (O)-O-D118 ,-OC (O)-NHD119 ,-O-C (O)-ND120D121 ,-OP (O) is (OD123) (OD122), and-OSi (D124) is (D126) (D125) ,-OS (O ₂)-D127 ,-NHC (O)-D128 ,-ND129C (O)-D130 ,-NH-C (O)-O-D131 ,-NH-C (O)-NH-D132 ,-NH-C (O)-ND133D134 ,-ND135-C (O)-O-D136 ,-ND137-C (O)-NH-D138 ,-ND139-C (O)-ND140D141 ,-NHS (O ₂)-D142 ,-ND143S (O ₂)-D144 ,-S-D145 ,-S (O)-D146 ,-S (O ₂)-D147 ,-S (O ₂) NH-D148 ,-S (O ₂) ND149D150 ,-S (O ₂) O-D151 ,-P (O) is (OD153) (OD152), and-Si (D154) is (D156) (D155) ";

D105 wherein, D106, D107, D108, D109, D110, D111, D112, D113, D114, D115, D116, D117, D118; D119, D120, D121, D122, D123, D124, D125, D126, D127, D128, D129, D130, D131; D132, D133, D134, D135, D136, D137, D138, D139, D140, D141, D142, D143, D144; D145, D146, D147, D148, D149, D150, D151, D152, D153, D154, D155, D156 is selected from independently of one another: " alkyl, (C ₉-C ₃₀) alkyl, naphthenic base, cycloalkylalkyl, heterocyclic radical; The heterocyclic radical alkyl, aryl, arylalkyl, heteroaryl; Heteroarylalkyl " and wherein, perhaps, D111, D112 and/or D120; D121 and/or D133, D134 and/or D140, D141 and/or D149, D150 also can form " heterocyclic radical " in each case together.

For fear of ambiguity, preceding text are that the situation (A) to (E) that general formula (I) details is explained as follows:

In situation (A), said new pyrido [2,3-b] pyrazines derivatives can be replaced by " substituted aryl " at their Z3, at least one place in the Z4 group, because subcase (a) or because subcase (c) produces novelty.If only Z3, a Z4 group are new " substituted aryl ", other Z3, Z4 group can have any replacement in said maximum range [(in the subcase (d) " and (with) " be connected] in each case.Randomly, Z3, Z4 group the two also can have other replacement [subcase (b) or (d)].Said Z1, Z2 and Z5 group can have said maximum range [in the situation (A) to (D) " and (with) " be connected] in any replacement.

In situation (B), said new pyrido [2,3-b] pyrazines derivatives can be replaced by " substituted heteroaryl " at their Z3, at least one place in the Z4 group, because subcase (a) or because subcase (c) generation novelty.If only Z3, a Z4 group are new " substituted heteroaryl ", other Z3, Z4 group can have any replacement in said maximum range [(in the subcase (d) " and (with) " be connected] in each case.Randomly, Z3, Z4 group the two also can have other replacement [subcase (b) or (d)].Said Z1, Z2 and Z5 group can have any replacement in said maximum range [" and (with) " in the situation (A) to (D) is connected].

In situation (C), at least one place that said new pyrido [2,3-b] pyrazines derivatives can be in their Z3, Z4 group is by " substituted alkyl " or " (C ₉-C ₃₀) alkyl " replace.If only Z3, a Z4 group be new " substituted alkyl " or " (C ₉-C ₃₀) alkyl ", other Z3, Z4 group can have at said maximum range [(subcase " (C in each case ₉-C ₃₀) alkyl " and in " and (with) " be connected] in the replacement of any hope.Said Z1, Z2 and Z5 group can have any replacement in said maximum range [" and (with) " in the situation (A) to (D) is connected].

In situation (D), said new pyrido [2,3-b] pyrazines derivatives can be replaced by " NZ10Z11 ,-OZ12 ,-SZ13 " at their Z3, at least one place in the Z4 group, because subcase (a) or because subcase (b) generation novelty.If only Z3, a Z4 group be new " NZ10Z11 ,-OZ12 ,-SZ13 ", other Z3, Z4 group can have the replacement of any hope in said maximum range [(" and (with) " in the subcase (b) is connected] in each case.Said Z1, Z2 and Z5 group can have the replacement of any hope in said maximum range [" and (with) " in the situation (A) to (D) is connected].

In situation (E), said new pyrido [2,3-b] pyrazines derivatives can be replaced by " NZ24Z25 ;-NZ26Z27 " at their Z1, at least one place in the Z2 group; Because subcase (a) (1), subcase (b) (1) are (I), subcase (b) (1) (II) or subcase (b) (2) produce novelty.If only Z1, a Z2 group be new " NZ24Z25 ,-NZ26Z27 ", other Z1, Z2 group can have any replacement in said maximum range [subcase (c), (d)] [" and (with) " in the subcase (b) (2) is connected] in each case.Said Z3, Z4 and Z5 group group can have any replacement in said maximum range [" and (with) " in the subcase (d) is connected].

In a preferred embodiment, new pyrido [2, the 3-b] pyrazines derivatives of general formula (I) is provided, wherein, in (A),

Said Z1 group is " NZ14Z15 " independently; Wherein Z14 is that hydrogen or " aryl " and Z15 are " C (O) NH-alkyl "; Wherein " C (O) NH-alkyl " can be extraly, randomly replaced by " OH ";

Said Z2 group is hydrogen independently;

Said Z3 group is " substituted aryl " independently, and wherein " substituted aryl " is selected from following substituting group replacement by at least one identically or differently:

(a) " alkyl ,-OC (O)-alkyl ,-O-alkyl ,-NHC (O)-alkyl ";

(i) " aryl, heterocyclic radical ,-O-alkyl-O-alkyl ,-O-arylalkyl ";

OrSaid Z3 group is " substituted aryl " independently, and wherein " substituted aryl " is selected from following substituting group replacement by at least one identically or differently:

(c) " OC (O)-O-alkyl ,-OC (O)-O-aryl ,-OC (O)-N (alkyl) ₂,-OC (O)-NH-alkyl ,-OC (O)-(C ₉-C ₃₀) alkyl ,-NHC (O)-O-alkyl ,-NHC (O)-NH-alkyl ,-NHC (O)-N (alkyl) ₂,-Si (alkyl) ₃";

Wherein randomly, the above-mentioned substituting group of substituting group group (c) can and then be selected from following substituting group replacement by at least one independently of one another identically or differently:

(i) " O-alkyl ,-O-arylalkyl ";

Wherein randomly, said Z3 group also can be selected from following substituting group replacement by at least one independently identically or differently:

(d) " halogen, F, Cl, Br, I ,-O-alkyl ";

Said Z4 group is hydrogen independently;

Said Z5 group is hydrogen independently.

Said Z1 group is independently selected from " NHC (O) NH-ethyl ,-NHC (O) NH-butyl-OH ";

Said Z2 group is hydrogen independently;

Said Z3 group is independently selected from " 4-phenyl methyl carbonic ether, 3-phenyl 2-methoxy ethyl carbonic ether, 4-phenyl 2-methoxy ethyl carbonic ether; 4-phenyl carbonic ether, 4-phenyl N-diethylamino manthanoate, 4-phenyl 3-phenyl acrylate; 4-phenyl nonadecane acid esters, 4-phenyl isobutyl-carbonic ether, 4-phenyl fourth-2-alkynyl carbonic ether; 4-phenyl N-dimethylcarbamate, 4-phenyl N-ethyl carbamate, tertiary butyl N-(4-phenyl) carbamate; 2-methoxy ethyl N-(4-phenyl) carbamate, 4-(3-ethyl carbamide) phenyl, 4-(3; 3-methyl urea) phenyl, 4-morpholine-4-ylmethyl phenyl, 4-[2-(2-methoxy ethoxy) oxyethyl group] phenyl; N-(4-phenyl)-2-(2-methoxy ethoxy) ethanamide, 4-(2-methoxyl group) phenyl 2-methoxy ethyl carbonic ether, 4-phenyl 2-benzyloxy ethyl carbonate ester; 4-(2-methoxyl group) phenyl 2-benzyloxy ethyl carbonate ester, N-(4-phenyl)-2-benzyloxy ethanamide, 3-TMS phenyl; 4-(2-methoxyl group) phenyl N-diethylamino manthanoate, 4-(2-chloro-6-methoxyl group) phenyl N-diethylamino manthanoate, 4-(2-methoxyl group) phenyl 2-[2-(2-methoxy ethoxy) oxyethyl group] ethyl carbonate ester ";

Said Z4 group is hydrogen independently;

Said Z5 group is hydrogen independently.

In another preferred embodiment, new pyrido [2, the 3-b] pyrazines derivatives of general formula (I) is provided, wherein, in (B),

Said Z1 group is " NZ14Z15 " independently; Wherein Z14 is that hydrogen and Z15 are " C (O) NH-alkyl ";

Said Z2 group is hydrogen independently;

Said Z3 group is " substituted heteroaryl " independently, and wherein " substituted heteroaryl " is selected from following substituting group replacement by at least one identically or differently:

(a) " NHC (O)-NH-alkyl ";

Said Z4 group is hydrogen independently;

Said Z5 group is hydrogen independently.

Said Z1 group is independently selected from " NHC (O) NH-ethyl ";

Said Z2 group is hydrogen independently;

Said Z3 group is independently selected from " 6-(3-ethyl carbamide) pyridin-3-yl ";

Said Z4 group is hydrogen independently;

Said Z5 group is hydrogen independently.

In another preferred embodiment, new pyrido [2, the 3-b] pyrazines derivatives of general formula (I) is provided, wherein, in (C),

Said Z2 group is hydrogen independently;

Said Z3 group is " substituted alkyl " independently, and wherein " substituted alkyl " is selected from following substituting group replacement by at least one identically or differently:

(a) " aryl, heteroaryl, naphthenic base ,-N (alkyl) ₂,-O-alkyl ";

(i) " halogen, F, Cl, Br, I ";

Said Z4 group is hydrogen independently;

Said Z5 group is hydrogen independently.

Said Z1 group is independently selected from " NHC (O) NH-ethyl ";

Said Z2 group is hydrogen independently;

Said Z3 group is independently selected from " phenylacetylene base, thiene-3-yl-ethynyl, cyclopropyl acethlene base, N-dimethylamino third-1-alkynyl, 2-cyclohexyl vinyl, 3-methoxy propyl thiazolinyl, benzyl, 2-(4-fluorophenyl) ethyl, 2-(4-fluorophenyl) vinyl ";

Said Z4 group is hydrogen independently;

Said Z5 group is hydrogen independently.

In another preferred embodiment, new pyrido [2, the 3-b] pyrazines derivatives of general formula (I) is provided, wherein, in (D),

Said Z2 group is hydrogen independently;

Said Z3 group is independently selected from:

(1)“-NZ10Z11”；

Wherein said Z10, Z11 group are selected from independently of one another:

(a) " hydrogen, aryl ";

Condition is, the above-mentioned substituting group of substituting group group (a) is when being not hydrogen, independently of one another by at least one identical ground or different are selected from following substituting group and further replace:

(i) " naphthenic base, heteroaryl, heterocyclic radical alkyl ,-S (O) ₂-alkyl ,-NH-S (O) ₂-alkyl ,-C (O) NH-alkyl ,-NH-C (O)-alkyl ,-C (O) O-alkyl ";

(b) " C (O)-aryl ";

Wherein randomly, the above-mentioned substituting group of substituting group group (a) and/or substituting group group (b) can be selected from following substituting group replacement by at least one independently of one another identically or differently:

(i) " alkyl ";

Said Z4 group is hydrogen independently;

Said Z5 group is hydrogen independently.

Said Z1 group is independently selected from " NHC (O) NH-ethyl ";

Said Z2 group is hydrogen independently;

Said Z3 group is independently selected from " 4-methyl benzamide, the 4-cyclohexyl phenyl is amino, 4-methane sulfonyl phenyl amino; 3-(N-NSC-249992)-4-aminomethyl phenyl is amino; the 3-N-methyl benzamide is amino, 4-piperidines-1-ylmethyl phenyl amino, 4-thiene-3-yl-phenyl amino; 4-N-acetamido phenyl amino, 3-(ethyl benzoate) amino ";

Said Z4 group is hydrogen independently;

Said Z5 group is hydrogen independently.

In another preferred embodiment, new pyrido [2, the 3-b] pyrazines derivatives of general formula (I) is provided, wherein, in (E),

Said Z1 group is independently selected from:

(a) " NZ24Z25 "; Wherein Z24 is that hydrogen and Z25 are " C (O)-C (O)-O-alkyl " or " C (O)-C (O)-NH-alkyl " or " C (O)-NH-O-alkyl ";

Wherein randomly, the above-mentioned substituting group of substituting group group (a) can be selected from following substituting group replacement by at least one independently of one another identically or differently:

(i) " OSi (alkyl) ₃,-OC (O)-NH-alkyl ,-OC (O)-O-alkyl ,-P (O) (O-alkyl) ₂,-P (O) (OH) ₂,-O-alkyl ";

Wherein randomly, the above-mentioned substituting group of substituting group group (i) also can be independently of one another by at least one identical ground or different are selected from following substituting group and further replace:

(ii) " heterocyclic radical, OH ,-N (alkyl) ₂,-OC (O)-alkyl ";

Wherein randomly, substituting group group above-mentioned substituting group (ii) also can be independently of one another by at least one identical ground or different are selected from following substituting group and further replace:

(ii) " alkyl ";

(b) " NZ26Z27 "; Wherein Z26 is that hydrogen and Z27 are " C (O)-NH-alkyl ";

Condition is, the above-mentioned substituting group of substituting group group (b) is independently of one another by at least one identical ground or different are selected from following substituting group and further replace:

(ii) " heterocyclic radical, OH ,-N (alkyl) ₂,-OC (O)-alkyl ";

(iii) " alkyl ";

Said Z2 group is hydrogen independently;

Said Z3 group is independently selected from:

(a) " aryl ";

(i) " O-alkyl, OH ";

Said Z4 group is hydrogen independently;

Said Z5 group is hydrogen independently.

Said Z1 group is independently selected from that " 4-[(2 for 3-methoxyl group-1-base urea, 3-(third-1-alkynes-3-yl)-1-base urea, 3-[4-(tertiary butyl dimethylsilyl oxygen base) butyl]-1-base urea; 4-(N-ethyl carbamate) butyl-1-base urea, 4-(methyl carbonic) butyl-1-base urea, 4-(2; 3-dihydroxypropyl carbonic ether) butyl-1-base urea, 4-(2,2-dimethyl--[1; 3] dioxolane-4-ylmethyl carbonic ether) butyl-1-base urea, 4-(diethylammonium SULPHOSUCCINIC ACID ESTER) butyl-1-base urea, 4-(butyl phosphoric acid ester)-1-base urea; N-oxalic monoamide ethyl ester, N-ethyl-N '-oxamide, 2-(diethylammonium SULPHOSUCCINIC ACID ESTER) ethyl-1-base urea; 2-(ethyl phosphonic acid ester)-1-base urea, the basic urea of 3-(2-diethylin-oxyethyl group) propyl group-1-; 2-dimethyl propylene acyloxy methoxyl group) inferior phosphonato methyl 2,2-dimethyl propylene acid esters] butyl-1-base urea, 4-[1-(1-acetoxyethoxy) oxyethyl group time phosphonato acetic ester] butyl-1-base urea ";

Said Z2 group is hydrogen independently;

Said Z3 group is independently selected from " phenyl, 4-hydroxy 3-methoxybenzene base ";

Said Z4 group is hydrogen independently;

Said Z5 group is hydrogen independently.

Another aspect of the application relates to coming the new compound of pyrido [2,3-b] the pyrazine group of self-drifting (II),

Wherein each is as follows self-defined for substituent R 1-R4:

R1 and R2 can be hydrogen or NR5R6 independently of one another, and prerequisite is, when R1=NR5R6, and R2=H, and when R2=NR5R6, R1=H,

Wherein R5 can be a hydrogen, alkyl, R38, naphthenic base, heterocyclic radical, aryl; Heteroaryl, alkyl-cycloalkyl, alkyl heterocyclic, alkylaryl or miscellaneous alkyl aryl, and said alkyl, naphthenic base; Heterocyclic radical, aryl and heteroaryl, alkyl-cycloalkyl, alkyl heterocyclic, alkylaryl or miscellaneous alkyl aryl substituting group itself can and then be replaced or polysubstituted by the identical or different ground of following substituting group is single: F; Cl, Br, I, CN, CF ₃, NH ₂, NH-alkyl, NH-aryl, N (alkyl) ₂, NO ₂, SH, S-alkyl, OH, OCF ₃, O (alkyl O) _p-alkyl, O-aryl, OSO ₃H, OP (O) (OH) ₂, OP (O) (O alkyl) ₂, OP (O) (O aryl) ₂, CHO, C (O) OH, C (O) OR12, C (O) NH ₂, C (O) NHR12, C (O) NR12R13, SO ₃H, SO ₂Alkyl, SO ₂Aryl, P (O) (OH) ₂, P (O) (O alkyl) ₂, P (O) (O aryl) ₂, alkyl, naphthenic base, heterocyclic radical; Aryl, heteroaryl, p can be 0,1,2,3,4 or 5 values, and said R12 and R13 group can be alkyl independently of one another; Naphthenic base, heterocyclic radical, aryl, heteroaryl; Alkyl-cycloalkyl, alkyl heterocyclic, alkylaryl or miscellaneous alkyl aryl, or R12 and R13 can form heterocyclic ring together

And R6:

Can be-C (Y) NR7R8, wherein Y can be O or S independently, and R7 and R8 can be independently of one another

Hydrogen,

Unsubstituted or substituted alkyl, wherein said alkyl can be replaced or polysubstituted by the identical or different ground of following substituting group is single: F, Cl, Br, I, CF ₃, CN, NH ₂, NH-alkyl, NH-naphthenic base, NH-heterocyclic radical, NH-aryl, NH-heteroaryl, NH-alkyl-cycloalkyl, NH-alkyl heterocyclic, NH-alkylaryl, NH-miscellaneous alkyl aryl, N (alkyl) ₂, NHC (O)-alkyl, NHC (O)-naphthenic base, NHC (O)-heterocyclic radical, NHC (O)-aryl, NHC (O)-heteroaryl, NHC (O)-alkylaryl, NHC (O)-miscellaneous alkyl aryl, NHSO ₂-alkyl, NHSO ₂-naphthenic base, NHSO ₂-heterocyclic radical, NHSO ₂-aryl, NHSO ₂-heteroaryl, NHSO ₂-alkylaryl, NHSO ₂-miscellaneous alkyl aryl, NO ₂, SH, S-alkyl, S-naphthenic base, S-heterocyclic radical, S-aryl, S-heteroaryl, OH, OCF ₃, O (alkyl O) _p-alkyl, O-naphthenic base, O-heterocyclic radical, O-aryl, O-heteroaryl; The O-alkyl-cycloalkyl, O-alkyl heterocyclic, O-alkylaryl, O-miscellaneous alkyl aryl; OC (O)-alkyl, OC (O)-naphthenic base, OC (O)-heterocyclic radical, OC (O)-aryl; OC (O)-heteroaryl, OC (O)-alkylaryl, OC (O)-miscellaneous alkyl aryl, OSO ₃H, OSO ₂-alkyl, OSO ₂-naphthenic base, OSO ₂-heterocyclic radical, OSO ₂-aryl, OSO ₂-heteroaryl, OSO ₂-alkylaryl, OSO ₂-miscellaneous alkyl aryl, OP (O) (OH) ₂, C (O)-alkyl, C (O)-aryl, C (O)-heteroaryl, CO ₂H, CO ₂-alkyl, CO ₂-naphthenic base, CO ₂-heterocyclic radical, CO ₂-aryl, CO ₂-heteroaryl, CO ₂-alkyl-cycloalkyl, CO ₂-alkyl heterocyclic, CO ₂-alkylaryl, CO ₂-miscellaneous alkyl aryl, C (O)-NH ₂, C (O) NH-alkyl, C (O) NH-naphthenic base, C (O) NH-heterocyclic radical, C (O) NH-aryl, C (O) NH-heteroaryl, C (O) NH-alkyl-cycloalkyl, C (O) NH-alkyl heterocyclic, C (O) NH-alkylaryl, C (O) NH-miscellaneous alkyl aryl, C (O) N (alkyl) ₂, C (O) N (naphthenic base) ₂, C (O) N (aryl) ₂, C (O) N (heteroaryl) ₂, SO-alkyl, SO-aryl, SO ₂-alkyl, SO ₂-aryl, SO ₂NH ₂, SO ₂The NH-alkyl, SO ₂The NH-aryl, SO ₂The NH-heteroaryl, SO ₂The NH-alkylaryl, SO ₃H, SO ₂The O-alkyl, SO ₂The O-aryl, SO ₂The O-alkylaryl, naphthenic base, heterocyclic radical, aryl or heteroaryl, wherein p can be 0,1,2,3,4 or 5 value,

Unsubstituted or substituted naphthenic base, wherein said naphthenic base can be replaced or polysubstituted by the identical or different ground of following substituting group is single: F, Cl, Br, I, NH ₂, NH-alkyl, NH-naphthenic base, NH-heterocyclic radical, NH-aryl, NH-heteroaryl, NH-alkylaryl, NH-miscellaneous alkyl aryl, N (alkyl) ₂, NHC (O)-alkyl, NHC (O)-naphthenic base, NHC (O)-heterocyclic radical, NHC (O)-aryl, NHC (O)-heteroaryl, NHC (O)-alkylaryl, NHC (O)-miscellaneous alkyl aryl, NHSO ₂-alkyl, NHSO ₂-naphthenic base, NHSO ₂-heterocyclic radical, NHSO ₂-aryl, NHSO ₂-heteroaryl, NHSO ₂-alkylaryl, NHSO ₂-miscellaneous alkyl aryl, OH, O (alkyl O) _p-alkyl, O-naphthenic base, O-heterocyclic radical, O-aryl, O-heteroaryl; The O-alkylaryl, O-miscellaneous alkyl aryl, OC (O)-alkyl, OC (O)-naphthenic base, OC (O)-heterocyclic radical; OC (O)-aryl, OC (O)-heteroaryl, OC (O)-alkylaryl, OC (O)-miscellaneous alkyl aryl, OSO ₃H, OSO ₂-alkyl, OSO ₂-naphthenic base, OSO ₂-heterocyclic radical, OSO ₂-aryl, OSO ₂-heteroaryl, OSO ₂-alkylaryl, OSO ₂-miscellaneous alkyl aryl, OP (O) (OH) ₂, CO ₂H, CO ₂-alkyl, CO ₂-naphthenic base, CO ₂-heterocyclic radical, CO ₂-aryl, CO ₂-heteroaryl, CO ₂-alkyl-cycloalkyl, CO ₂-alkyl heterocyclic, CO ₂-alkylaryl, CO ₂-miscellaneous alkyl aryl, C (O)-NH ₂, C (O) NH-alkyl, C (O) NH-naphthenic base, C (O) NH-heterocyclic radical, C (O) NH-aryl, C (O) NH-heteroaryl, C (O) NH-alkyl-cycloalkyl, C (O) NH-alkyl heterocyclic, C (O) NH-alkylaryl, C (O) NH-miscellaneous alkyl aryl, C (O) N (alkyl) ₂, C (O) N (naphthenic base) ₂, C (O) N (aryl) ₂, C (O) N (heteroaryl) ₂, alkyl, or aryl, wherein p can be 0,1,2,3,4 or 5 value,

Unsubstituted or substituted heterocyclic radical, wherein said heterocyclic radical can be replaced or polysubstituted by the identical or different ground of following substituting group is single: OH, O-alkyl, O-aryl, NH ₂, the NH-alkyl, the NH-aryl, alkyl, alkylaryl or aryl,

Unsubstituted or substituted aryl, wherein said aryl can be replaced or polysubstituted by the identical or different ground of following substituting group is single: F, Cl, Br, I, CF ₃, CN, NH ₂, NH-alkyl, NH-R38, NH-naphthenic base, NH-heterocyclic radical, NH-aryl, NH-heteroaryl, NH-alkyl-cycloalkyl, NH-alkyl heterocyclic, NH-alkylaryl, NH-miscellaneous alkyl aryl, NH-alkyl NH ₂, NH-alkyl OH, N (alkyl) ₂, NHC (O)-alkyl, NHC (O)-R38, NHC (O)-naphthenic base, NHC (O)-heterocyclic radical, NHC (O)-aryl, NHC (O)-heteroaryl, NHC (O)-alkylaryl, NHC (O)-miscellaneous alkyl aryl, NHSO ₂-alkyl, NHSO ₂-naphthenic base, NHSO ₂-heterocyclic radical, NHSO ₂-aryl, NHSO ₂-heteroaryl, NHSO ₂-alkylaryl, NHSO ₂-miscellaneous alkyl aryl, NO ₂, SH, S-alkyl, S-naphthenic base, S-heterocyclic radical, S-aryl, S-heteroaryl, OH, OCF ₃, O (alkyl O) _p-alkyl, O-R38, O-naphthenic base, O-heterocyclic radical, O-aryl, O-heteroaryl, O-alkyl-cycloalkyl, O-alkyl heterocyclic, O-alkylaryl, O-miscellaneous alkyl aryl, O-alkyl OH, O-(CH ₂) _n-O, OC (O)-alkyl, OC (O)-R38, OC (O)-naphthenic base, OC (O)-heterocyclic radical, OC (O)-aryl, OC (O)-heteroaryl, OC (O)-alkylaryl, OC (O)-miscellaneous alkyl aryl, OSO ₃H, OSO ₂-alkyl, OSO ₂-naphthenic base, OSO ₂-heterocyclic radical, OSO ₂-aryl, OSO ₂-heteroaryl, OSO ₂-alkylaryl, OSO ₂-miscellaneous alkyl aryl, OP (O) (OH) ₂, C (O)-alkyl, C (O)-aryl, C (O)-heteroaryl, CO ₂H, CO ₂-alkyl, CO ₂-R38, CO ₂-naphthenic base, CO ₂-heterocyclic radical, CO ₂-aryl, CO ₂-heteroaryl, CO ₂-alkyl-cycloalkyl, CO ₂-alkyl heterocyclic, CO ₂-alkylaryl, CO ₂-miscellaneous alkyl aryl, C (O)-NH ₂, C (O) NH-alkyl, C (O) NH-R38, C (O) NH-naphthenic base, C (O) NH-heterocyclic radical, C (O) NH-aryl, C (O) NH-heteroaryl, C (O) NH-alkyl-cycloalkyl, C (O) NH-alkyl heterocyclic, C (O) NH-alkylaryl, C (O) NH-miscellaneous alkyl aryl, C (O) N (alkyl) ₂, C (O) N (naphthenic base) ₂, C (O) N (aryl) ₂, C (O) N (heteroaryl) ₂, SO-alkyl, SO-aryl, SO ₂-alkyl, SO ₂-aryl, SO ₂NH ₂, SO ₂The NH-alkyl, SO ₂The NH-aryl, SO ₂The NH-heteroaryl, SO ₂The NH-alkylaryl, SO3H, SO ₂The O-alkyl, SO ₂The O-aryl, SO ₂The O-alkylaryl, alkyl, naphthenic base, heterocyclic radical, aryl or heteroaryl, wherein p can be 0,1,2,3,4 or 5 value, and n is 1,2 or 3 value,

Unsubstituted or substituted heteroaryl, wherein said heteroaryl can be replaced or polysubstituted by the identical or different ground of following substituting group is single: F, Cl, Br, I, CF ₃, CN, NH ₂, NH-alkyl, NH-R38, NH-naphthenic base, NH-heterocyclic radical, NH-aryl, NH-heteroaryl, NH-alkyl-cycloalkyl, NH-alkyl heterocyclic, NH-alkylaryl, NH-miscellaneous alkyl aryl, NH-alkyl NH ₂, NH-alkyl OH, N (alkyl) ₂, NHC (O)-alkyl, NHC (O)-R38, NHC (O)-naphthenic base, NHC (O)-heterocyclic radical, NHC (O)-aryl, NHC (O)-heteroaryl, NHC (O)-alkylaryl, NHC (O)-miscellaneous alkyl aryl, NHSO ₂-alkyl, NHSO ₂-naphthenic base, NHSO ₂-heterocyclic radical, NHSO ₂-aryl, NHSO ₂-heteroaryl, NHSO ₂-alkylaryl, NHSO ₂-miscellaneous alkyl aryl, NO ₂, SH, S-alkyl, S-aryl, S-heteroaryl, OH, OCF ₃, O (alkyl O) _p-alkyl, O-R38, O-naphthenic base, O-heterocyclic radical, O-aryl; The O-heteroaryl, O-alkyl-cycloalkyl, O-alkyl heterocyclic, O-alkylaryl, O-miscellaneous alkyl aryl; OC (O)-alkyl, OC (O)-R38, OC (O)-naphthenic base, OC (O)-heterocyclic radical, OC (O)-aryl; OC (O)-heteroaryl, OC (O)-alkylaryl, OC (O)-miscellaneous alkyl aryl, OSO ₃H, OSO ₂-alkyl, OSO ₂-naphthenic base, OSO ₂-heterocyclic radical, OSO ₂-aryl, OSO ₂-heteroaryl, OSO ₂-alkylaryl, OSO ₂-miscellaneous alkyl aryl, OP (O) (OH) ₂, C (O)-alkyl, C (O)-aryl, C (O)-heteroaryl, CO ₂H, CO ₂-alkyl, CO ₂-R38, CO ₂-naphthenic base, CO ₂-heterocyclic radical, CO ₂-aryl, CO ₂-heteroaryl, CO ₂-alkyl-cycloalkyl, CO ₂-alkyl heterocyclic, CO ₂-alkylaryl, CO ₂-miscellaneous alkyl aryl, C (O)-NH ₂, C (O) NH-alkyl, C (O) NH-R38, C (O) NH-naphthenic base, C (O) NH-heterocyclic radical, C (O) NH-aryl, C (O) NH-heteroaryl, C (O) NH-alkyl-cycloalkyl, C (O) NH-alkyl heterocyclic, C (O) NH-alkylaryl, C (O) NH-miscellaneous alkyl aryl, C (O) N (alkyl) ₂, C (O) N (naphthenic base) ₂, C (O) N (aryl) ₂, C (O) N (heteroaryl) ₂, SO ₂NH ₂, SO ₂The NH-alkyl, SO ₂The NH-aryl, SO ₂The NH-heteroaryl, SO ₂The NH-alkylaryl, SO ₃H, SO ₂The O-alkyl, SO ₂The O-aryl, SO ₂The O-alkylaryl, alkyl, naphthenic base, heterocyclic radical, aryl or heteroaryl, wherein p can be 0,1,2,3,4 or 5 value,

-C (O)-R39, wherein R39 can be an alkyl, aryl or heteroaryl, and said alkyl, aryl and heteroaryl substituting group can and then be substituted itself,

Or R7 and R8 can form heterocyclic ring together,

R3 and R4 can be independently of one another:

Hydrogen, wherein R3 and R4 are not hydrogen simultaneously,

Substituted alkyl, wherein said alkyl can be replaced or polysubstituted by the identical or different ground of following substituting group is single: F, Cl, Br, I, CN, CF ₃, NH ₂, NH-alkyl, NH-aryl, N (alkyl) ₂, SH, S-alkyl, OH, OCF ₃, O (alkyl O) _p-alkyl, O-aryl, OSO ₃H, OP (O) (OH) ₂, OP (O) (O alkyl) ₂, OP (O) (O aryl) ₂, C (O) OH, C (O) OR14, C (O) NH ₂, C (O) NHR14, C (O) NR14R15, SO ₃H, SO ₂Alkyl, SO ₂Aryl, P (O) (OH) ₂, P (O) (O alkyl) ₂, P (O) (O aryl) ₂, naphthenic base, heterocyclic radical, aryl or heteroaryl; Wherein p can be 0,1,2,3,4 or 5 value, and said R14 and R15 group can be alkyl independently of one another, naphthenic base, heterocyclic radical; Aryl, heteroaryl, alkyl-cycloalkyl, alkyl heterocyclic; Alkylaryl or miscellaneous alkyl aryl, or R14 and R15 can form heterocyclic ring together

Substituted aryl, wherein said aryl are selected from the single replacement in the identical or different ground of following substituting group or polysubstituted: NH-alkyl, NH-naphthenic base, NH-heterocyclic radical; The NH-aryl, NH-heteroaryl, NH-alkyl-cycloalkyl, NH-alkyl heterocyclic; The NH-alkylaryl, NH-miscellaneous alkyl aryl, N (alkyl) ₂, N (aryl) ₂, NHC (O)-alkyl, NHC (O)-naphthenic base, NHC (O)-heterocyclic radical, NHC (O)-aryl, NHC (O)-heteroaryl, NHC (O)-alkylaryl, NHC (O)-miscellaneous alkyl aryl, NHSO ₂-alkyl, NHSO ₂-naphthenic base, NHSO ₂-heterocyclic radical, NHSO ₂-aryl, NHSO ₂-heteroaryl, NHSO ₂-alkylaryl, NHSO ₂-miscellaneous alkyl aryl, S-alkyl, S-aryl, S-heteroaryl, O-alkyl, O-naphthenic base; The O-heterocyclic radical, O-aryl, O-heteroaryl, O-alkyl-cycloalkyl, O-alkyl heterocyclic; The O-alkylaryl, O-miscellaneous alkyl aryl, OC (O)-alkyl, OC (O)-naphthenic base, OC (O)-heterocyclic radical; OC (O)-aryl, OC (O)-heteroaryl, OC (O)-alkylaryl, OC (O)-miscellaneous alkyl aryl, OSO ₂-alkyl, OSO ₂-naphthenic base, OSO ₂-heterocyclic radical, OSO ₂-aryl, OSO ₂-heteroaryl, OSO ₂-alkylaryl, OSO ₂-miscellaneous alkyl aryl, C (O)-alkyl, C (O)-aryl, C (O)-heteroaryl, CO ₂-alkyl, CO ₂-naphthenic base, CO ₂-heterocyclic radical, CO ₂-aryl, CO ₂-heteroaryl, CO ₂-alkyl-cycloalkyl, CO ₂-alkyl heterocyclic, CO ₂-alkylaryl, CO ₂-miscellaneous alkyl aryl, C (O) NH-alkyl, C (O) NH-naphthenic base, C (O) NH-heterocyclic radical, C (O) NH-aryl, C (O) NH-heteroaryl, C (O) NH-alkyl-cycloalkyl, C (O) NH-alkyl heterocyclic, C (O) NH-alkylaryl, C (O) NH-miscellaneous alkyl aryl, C (O) N (alkyl) ₂, C (O) N (naphthenic base) ₂, C (O) N (aryl) ₂, C (O) N (heteroaryl) ₂, SO-alkyl, SO-aryl, SO ₂-alkyl, SO ₂-aryl, SO ₂The NH-alkyl, SO ₂The NH-aryl, SO ₂The NH-heteroaryl, SO ₂The NH-alkylaryl, SO ₂The O-alkyl, SO ₂The O-aryl, SO ₂The O-alkylaryl, alkyl, naphthenic base, heterocyclic radical, aryl; Heteroaryl, and said alkyl, naphthenic base, heterocyclic radical, aryl; Heteroaryl, alkyl-cycloalkyl, alkyl heterocyclic, alkylaryl and miscellaneous alkyl aryl substituting group and then replaced: O (alkyl O) itself by following substituting group _p-alkyl, OP (O) (O alkyl) ₂, OP (O) (O aryl) ₂, C (O) OR16, C (O) NH ₂, C (O) NHR16, C (O) NR16R17, SO ₂Alkyl, SO ₂Aryl, P (O) (OH) ₂, P (O) (O alkyl) ₂, P (O) (O aryl) ₂, naphthenic base, heterocyclic radical, aryl; Heteroaryl or alkylaryl, wherein p can be 1,2,3,4 or 5 value, and said R16 and R17 group can be alkyl independently of one another, naphthenic base; Heterocyclic radical, aryl, heteroaryl, alkyl-cycloalkyl; Alkyl heterocyclic, alkylaryl or miscellaneous alkyl aryl, or R16 and R17 can form heterocyclic ring together

Prerequisite is, when R3 or R4 were alkyl heterocyclic-substituted aryl, R4 or R3 correspondingly were not aryl,

And wherein said aryl is selected from the single replacement in the identical or different ground of following substituting group or polysubstituted: NR20-alkyl, NH-R38, NHC (O)-R38, NR19C (O)-alkyl; NR19C (O)-naphthenic base, NR19C (O)-heterocyclic radical, NR19C (O)-aryl, NR19C (O)-heteroaryl, NR18C (O)-alkyl-cycloalkyl; NR18C (O)-alkyl heterocyclic, NR 19C (O)-alkylaryl, NR19C (O)-miscellaneous alkyl aryl, NR18C (O) O-R19; NR18C (O) NR18R18, O-R38, OC (O)-R38, OC (O)-alkyl-cycloalkyl; OC (O)-alkyl heterocyclic, OC (O) O-R19, OC (O) NR18R18, OP (O) (O alkyl) ₂, OP (O) (O aryl) ₂, C (O) O-R38, C (O) NH-R38, C (O) NR20-alkyl, C (O) NR19-alkyl R21; C (O) NR18O-R18, C (O) NR18NR18R18, and said alkyl, naphthenic base, heterocyclic radical; Aryl, heteroaryl, alkyl-cycloalkyl, alkyl heterocyclic, alkylaryl and miscellaneous alkyl aryl substituting group itself can and then be replaced by following substituting group: F; Cl, Br, I, CN, CF ₃, NH ₂, NH-alkyl, NH-aryl, N (alkyl) ₂, NO ₂, SH, S-alkyl, OH, OCF ₃, O (alkyl O) _p-alkyl, O-aryl, OSO ₃H, OP (O) (OH) ₂, OP (O) (O alkyl) ₂, OP (O) (O aryl) ₂, CHO, C (O) OH, C (O) OR22, C (O) NH ₂, C (O) NHR22, C (O) NR22R23, SO ₃H, SO ₂Alkyl, SO ₂Aryl, P (O) (OH) ₂, P (O) (O alkyl) ₂, P (O) (O aryl) ₂, alkyl, naphthenic base, heterocyclic radical, aryl; Heteroaryl or alkylaryl, wherein p can be 0,1,2,3,4 or 5 value, and said R22 and R23 group can be alkyl independently of one another, naphthenic base; Heterocyclic radical, aryl, heteroaryl, alkyl-cycloalkyl; Alkyl heterocyclic, alkylaryl or miscellaneous alkyl aryl, or R22 and R23 can form heterocyclic ring together

Substituted heteroaryl, wherein said heteroaryl are selected from the single replacement in the identical or different ground of following substituting group or polysubstituted: NH-alkyl, NH-naphthenic base; The NH-heterocyclic radical, NH-aryl, NH-heteroaryl; The NH-alkyl-cycloalkyl, NH-alkyl heterocyclic, NH-alkylaryl; The NH-miscellaneous alkyl aryl, N (alkyl) ₂, N (aryl) ₂, NHC (O)-alkyl, NHC (O)-naphthenic base, NHC (O)-heterocyclic radical, NHC (O)-aryl, NHC (O)-heteroaryl, NHC (O)-alkylaryl, NHC (O)-miscellaneous alkyl aryl, NHSO ₂-alkyl, NHSO ₂-naphthenic base, NHSO ₂-heterocyclic radical, NHSO ₂-aryl, NHSO ₂-heteroaryl, NHSO ₂-alkylaryl, NHSO ₂-miscellaneous alkyl aryl, S-alkyl, S-aryl, S-heteroaryl, O-alkyl; The O-naphthenic base, O-aryl, O-heteroaryl, O-alkyl-cycloalkyl, O-alkyl heterocyclic; The O-alkylaryl, O-miscellaneous alkyl aryl, OC (O)-alkyl, OC (O)-naphthenic base, OC (O)-heterocyclic radical; OC (O)-aryl, OC (O)-heteroaryl, OC (O)-alkylaryl, OC (O)-miscellaneous alkyl aryl, OSO ₂-alkyl, OSO ₂-naphthenic base, OSO ₂-heterocyclic radical, OSO ₂-aryl, OSO ₂-heteroaryl, OSO ₂-alkylaryl, OSO ₂-miscellaneous alkyl aryl, C (O)-alkyl, C (O)-aryl, C (O)-heteroaryl, CO ₂-alkyl, CO ₂-naphthenic base, CO ₂-heterocyclic radical, CO ₂-aryl, CO ₂-heteroaryl, CO ₂-alkyl-cycloalkyl, CO ₂-alkyl heterocyclic, CO ₂-alkylaryl, CO ₂-miscellaneous alkyl aryl, C (O) NH-alkyl, C (O) NH-naphthenic base, C (O) NH-heterocyclic radical, C (O) NH-aryl, C (O) NH-heteroaryl, C (O) NH-alkyl-cycloalkyl, C (O) NH-alkyl heterocyclic, C (O) NH-alkylaryl, C (O) NH-miscellaneous alkyl aryl, C (O) N (alkyl) ₂, C (O) N (naphthenic base) ₂, C (O) N (aryl) ₂, C (O) N (heteroaryl) ₂, SO ₂The NH-alkyl, SO ₂The NH-aryl, SO ₂The NH-heteroaryl, SO ₂The NH-alkylaryl, SO ₂The O-alkyl, SO ₂The O-aryl, SO ₂The O-alkylaryl, alkyl, naphthenic base, heterocyclic radical, aryl; Heteroaryl, and said alkyl, naphthenic base, heterocyclic radical, aryl; Heteroaryl, alkyl-cycloalkyl, alkyl heterocyclic, alkylaryl and miscellaneous alkyl aryl substituting group and then replaced: O (alkyl O) itself by following substituting group _p-alkyl, OP (O) (O alkyl) ₂, OP (O) (O aryl) ₂, C (O) OR16, C (O) NH ₂, C (O) NHR16, C (O) NR16R17, SO ₂Alkyl, SO ₂Aryl, P (O) (OH) ₂, P (O) (O alkyl) ₂, P (O) (O aryl) ₂, naphthenic base, heterocyclic radical, aryl; Heteroaryl or alkylaryl, wherein p can be 1,2,3,4 or 5 value, and said R16 and R17 group can be alkyl independently of one another, naphthenic base; Heterocyclic radical, aryl, heteroaryl, alkyl-cycloalkyl; Alkyl heterocyclic, alkylaryl or miscellaneous alkyl aryl, or R16 and R17 can form heterocyclic ring together

And wherein said heteroaryl is selected from the single replacement in the identical or different ground of following substituting group or polysubstituted: NR20-alkyl, NH-R38, NHC (O)-R38; NR19C (O)-alkyl, NR19C (O)-naphthenic base, NR19C (O)-heterocyclic radical, NR19C (O)-aryl; NR19C (O)-heteroaryl, NR18C (O)-alkyl-cycloalkyl, NR18C (O)-alkyl heterocyclic, NR19C (O)-alkylaryl; NR19C (O)-miscellaneous alkyl aryl, NR18C (O) O-R19, NR18C (O) NR18R18, NHSO ₂-alkyl heterocyclic, O-R38, O-heterocyclic radical, OC (O)-R38, OC (O)-alkyl-cycloalkyl, OC (O)-alkyl heterocyclic, OC (O) O-R19, OC (O) NR18R18, OP (O) (O alkyl) ₂, OP (O) (O aryl) ₂, C (O) O-R38, C (O) NH-R38, C (O) NR20-alkyl, C (O) NR19-alkyl R21; C (O) NR180-R18, C (O) NR18NR18R18, and said alkyl, naphthenic base, heterocyclic radical; Aryl, heteroaryl, alkyl-cycloalkyl, alkyl heterocyclic, alkylaryl and miscellaneous alkyl aryl substituting group itself can and then be replaced by following substituting group: F; Cl, Br, I, CN, CF ₃, NH ₂, NH-alkyl, NH-aryl, N (alkyl) ₂, NO ₂, SH, S-alkyl, OH, OCF ₃, O (alkyl O) _p-alkyl, O-aryl, OSO ₃H, OP (O) (OH) ₂, OP (O) (O alkyl) ₂, OP (O) (O aryl) ₂, CHO, C (O) OH, C (O) OR22, C (O) NH ₂, C (O) NHR22, C (O) NR22R23, SO ₃H, SO ₂Alkyl, SO ₂Aryl, P (O) (OH) ₂, P (O) (O alkyl) ₂, P (O) (O aryl) ₂, alkyl, naphthenic base, heterocyclic radical, aryl; Heteroaryl or alkylaryl, wherein p can be 0,1,2,3,4 or 5 value, and said R22 and R23 group can be alkyl independently of one another, naphthenic base; Heterocyclic radical, aryl, heteroaryl, alkyl-cycloalkyl; Alkyl heterocyclic, alkylaryl or miscellaneous alkyl aryl, or R22 and R23 can form heterocyclic ring together

NR24R25, wherein R24 can be-C (O)-R26 ,-SO ₂R26 ,-C (O) OR26 or-C (O)-NR27R28, and wherein R25 can be a hydrogen, alkyl, naphthenic base, aryl or heteroaryl, and wherein R26 can be an alkyl; Naphthenic base, heterocyclic radical, aryl, heteroaryl, alkyl-cycloalkyl, alkyl heterocyclic, alkylaryl; Miscellaneous alkyl aryl, and R27 and R28 can be hydrogen independently of one another, alkyl, naphthenic base, heterocyclic radical, aryl, heteroaryl; Alkyl-cycloalkyl, alkyl heterocyclic, alkylaryl, miscellaneous alkyl aryl, or R27 and R28 can form heterocyclic ring together, and said alkyl, naphthenic base; Heterocyclic radical, aryl and heteroaryl, alkyl-cycloalkyl, alkyl heterocyclic, alkylaryl or miscellaneous alkyl aryl substituting group can and then be substituted itself

And R18 can be a hydrogen, alkyl, and naphthenic base, heterocyclic radical, aryl, heteroaryl, alkyl-cycloalkyl, alkyl heterocyclic, alkylaryl or miscellaneous alkyl aryl,

And R19 can be an alkyl, naphthenic base, and heterocyclic radical, aryl, heteroaryl, alkyl-cycloalkyl, alkyl heterocyclic, alkylaryl or miscellaneous alkyl aryl,

And R20 can be a naphthenic base, heterocyclic radical, and aryl, heteroaryl, alkyl-cycloalkyl, alkyl heterocyclic, alkylaryl or miscellaneous alkyl aryl,

And R21 can be a naphthenic base, heterocyclic radical, and aryl, heteroaryl,

And R38 can be an alkyl, and wherein said alkyl can be straight chain or ramose saturated or unsaturated, that have 9-30 carbon atom, i.e. C _9-30-alkyl, C _9-30-alkenyl and C _9-30-alkynyl.Alkenyl has the two keys of at least one C-C, and alkynyl has at least one C-C triple bond, and wherein alkenyl can exist with (E)-or (Z)-conformation.Preferably, said alkyl is selected from: nonyl, decyl, dodecyl, hexadecyl, octadecyl, eicosyl, henicosyl, docosyl, tetracosyl, nonacosyl, octadecylene base, docosene base, two tetradecene bases and two octadecylene bases.

In yet another aspect, the application has described the new compound of pyrido [2,3-b] the pyrazine group of coming self-drifting (II),

Wherein each is as follows self-defined for substituent R 1-R4:

Wherein R5 can be a hydrogen, alkyl, R38, naphthenic base, heterocyclic radical, aryl; Heteroaryl, alkyl-cycloalkyl, alkyl heterocyclic, alkylaryl or miscellaneous alkyl aryl, and said alkyl, naphthenic base; Heterocyclic radical, aryl and heteroaryl, alkyl-cycloalkyl, alkyl heterocyclic, alkylaryl or miscellaneous alkyl aryl substituting group itself can and then be replaced or polysubstituted by the identical or different ground of following substituting group is single: F; Cl, Br, I, CN, CF ₃, NH ₂, NH-alkyl, NH-aryl, N (alkyl) ₂, NO ₂, SH, S-alkyl, OH, OCF ₃, O (alkyl O) _p-alkyl, O-aryl, OSO ₃H, OP (O) (OH) ₂, OP (O) (O alkyl) ₂, OP (O) (O aryl) ₂, CHO, C (O) OH, C (O) NH ₂, C (O) OR12, C (O) NHR12, C (O) NR12R13, SO ₃H, SO ₂Alkyl, SO ₂Aryl, P (O) (OH) ₂, P (O) (O alkyl) ₂, P (O) (O aryl) ₂, alkyl, naphthenic base, heterocyclic radical; Aryl, heteroaryl, p can be 0,1,2,3,4 or 5 values, and said R12 and R13 group can be alkyl independently of one another; Naphthenic base, heterocyclic radical, aryl, heteroaryl; Alkyl-cycloalkyl, alkyl heterocyclic, alkylaryl or miscellaneous alkyl aryl, or R12 and R13 can form heterocyclic ring together

And R6:

Can be-C (O) NR9-Y-R10, wherein Y can be 0 or NR11 independently

And R9 can be a hydrogen, alkyl, naphthenic base, heterocyclic radical, aryl; Heteroaryl, alkyl-cycloalkyl, alkyl heterocyclic, alkylaryl, miscellaneous alkyl aryl; And said alkyl, naphthenic base, heterocyclic radical, aryl and heteroaryl; Alkyl-cycloalkyl, alkyl heterocyclic, alkylaryl or miscellaneous alkyl aryl substituting group can be substituted itself

And R10 and R11 can be independently of one another

Hydrogen,

Unsubstituted or substituted alkyl,

Unsubstituted or substituted naphthenic base,

Or R10 and R11 can form heterocyclic ring together,

R3 and R4 can be independently of one another:

Hydrogen

Hydroxyl

Halogen is fluorine for example, chlorine, bromine, iodine

Unsubstituted or substituted alkyl, wherein said alkyl can be replaced or polysubstituted by the identical or different ground of following substituting group is single: F, Cl, Br, I, CN, CF ₃, NH ₂, NH-alkyl, NH-aryl, N (alkyl) ₂, SH, S-alkyl, OH, OCF ₃, O (alkyl O) _p-alkyl, O-aryl, OSO ₃H, OP (O) (OH) ₂, OP (O) (O alkyl) ₂, OP (O) (O aryl) ₂, C (O) OH, C (O) OR14, C (O) NH ₂, C (O) NHR14, C (O) NR14R15, SO ₃H, SO ₂Alkyl, SO ₂Aryl, P (O) (OH) ₂, P (O) (O alkyl) ₂, P (O) (O aryl) ₂, naphthenic base, heterocyclic radical, aryl or heteroaryl; Wherein p can be 0,1,2,3,4 or 5 value, and said R14 and R15 group can be alkyl independently of one another, naphthenic base, heterocyclic radical; Aryl, heteroaryl, alkyl-cycloalkyl, alkyl heterocyclic; Alkylaryl or miscellaneous alkyl aryl, or R14 and R15 can form heterocyclic ring together

Unsubstituted or substituted aryl, wherein said aryl can be replaced or polysubstituted by the identical or different ground of following substituting group is single: F, Cl, Br, I, CF ₃, CN, NH ₂, NH-alkyl, NH-R38, NH-naphthenic base, NH-heterocyclic radical, NH-aryl, NH-heteroaryl, NH-alkyl-cycloalkyl, NH-alkyl heterocyclic, NH-alkylaryl, NH-miscellaneous alkyl aryl, N (alkyl) ₂, N (aryl) ₂, NR20-alkyl, NHC (O)-alkyl, NHC (O)-R38, NR19 (O)-alkyl; NHC (O)-naphthenic base, NR19C (O)-naphthenic base, NHC (O)-heterocyclic radical, NR19C (O)-heterocyclic radical, NHC (O)-aryl; NR19C (O)-aryl, NHC (O)-heteroaryl, NR19C (O)-heteroaryl, NR18C (O)-alkyl-cycloalkyl; NR18C (O)-alkyl heterocyclic, NHC (O)-alkylaryl, NR19C (O)-alkylaryl, NHC (O)-miscellaneous alkyl aryl; NR19C (O)-miscellaneous alkyl aryl, NR18C (O) O-R19, NR18C (O) NR18R18, NHSO ₂-alkyl, NHSO ₂-naphthenic base, NHSO ₂-heterocyclic radical, NHSO ₂-aryl, NHSO ₂-heteroaryl, NHSO ₂-alkyl heterocyclic, NHSO ₂-alkylaryl, NHSO ₂-miscellaneous alkyl aryl, NO ₂, SH, S-alkyl, S-aryl, S-heteroaryl, OH, OCF ₃, O-alkyl, O-R38, O-naphthenic base, O-heterocyclic radical, O-aryl, O-heteroaryl, O-alkyl-cycloalkyl, O-alkyl heterocyclic, O-alkylaryl, O-miscellaneous alkyl aryl, O-(CH ₂) _n-O, OC (O)-alkyl, OC (O)-R38, OC (O)-naphthenic base, OC (O)-heterocyclic radical; OC (O)-aryl, OC (O)-heteroaryl, OC (O)-alkyl-cycloalkyl, OC (O)-alkyl heterocyclic OC (O)-alkylaryl; OC (O)-miscellaneous alkyl aryl, OC (O) O-R19, OC (O) NR18R18, OSO ₃H, OSO ₂-alkyl, OSO ₂-naphthenic base, OSO ₂-heterocyclic radical, OSO ₂-aryl, OSO ₂-heteroaryl, OSO ₂-alkylaryl, OSO ₂-miscellaneous alkyl aryl, OP (O) (OH) ₂, OP (O) (O alkyl) ₂, OP (O) (O aryl) ₂, C (O)-alkyl, C (O)-aryl, C (O)-heteroaryl, CO ₂H, CO ₂-alkyl, CO ₂-R38, CO ₂-naphthenic base, CO ₂-heterocyclic radical, CO ₂-aryl, CO ₂-heteroaryl, CO ₂-alkyl-cycloalkyl, CO ₂-alkyl heterocyclic, CO ₂-alkylaryl, CO ₂-miscellaneous alkyl aryl, C (O)-NH ₂, C (O) NH-alkyl, C (O) NH-R38, C (O) NH-naphthenic base, C (O) NH-heterocyclic radical, C (O) NH-aryl, C (O) NH-heteroaryl, C (O) NH-alkyl-cycloalkyl, C (O) NH-alkyl heterocyclic, C (O) NH-alkylaryl, C (O) NH-miscellaneous alkyl aryl, C (O) N (alkyl) ₂, C (O) N (naphthenic base) ₂, C (O) N (aryl) ₂, C (O) N (heteroaryl) ₂, C (O) NR20-alkyl, C (O) NR19-alkyl R21 ,-C (O) NR18O-R18 ,-C (O) NR18NR18R18, SO-alkyl, SO-aryl, SO ₂-alkyl, SO ₂-aryl, SO ₂NH ₂, SO ₂The NH-alkyl, SO ₂The NH-aryl, SO ₂The NH-heteroaryl, SO ₂The NH-alkylaryl, SO ₃H, SO ₂The O-alkyl, SO ₂The O-aryl, SO ₂The O-alkylaryl, alkyl, alkyl-cycloalkyl, alkyl heterocyclic, alkylaryl; Miscellaneous alkyl aryl, naphthenic base, heterocyclic radical, aryl or heteroaryl, n can be 1,2 or 3 values; And said alkyl, naphthenic base, heterocyclic radical, aryl, heteroaryl; Alkyl-cycloalkyl, alkyl heterocyclic, alkylaryl and miscellaneous alkyl aryl substituting group can and then be substituted itself

Unsubstituted or substituted heteroaryl, wherein said heteroaryl can be replaced or polysubstituted by the identical or different ground of following substituting group is single: F, Cl, Br, I, CF ₃, CN, NH ₂, NH-alkyl, NH-R38, NH-naphthenic base, NH-heterocyclic radical, NH-aryl, NH-heteroaryl, NH-alkyl-cycloalkyl, NH-alkyl heterocyclic, NH-alkylaryl, NH-miscellaneous alkyl aryl, N (alkyl) ₂, N (aryl) ₂, NR20-alkyl, NHC (O)-alkyl, NHC (O)-R38, NR19C (O)-alkyl; NHC (O)-naphthenic base, NR19C (O)-naphthenic base, NHC (O)-heterocyclic radical, NR19C (O)-heterocyclic radical, NHC (O)-aryl; NR19C (O)-aryl, NHC (O)-heteroaryl, NR19C (O)-heteroaryl, NR18C (O)-alkyl-cycloalkyl; NR18C (O)-alkyl heterocyclic, NHC (O)-alkylaryl, NR19C (O)-alkylaryl, NHC (O)-miscellaneous alkyl aryl; NR19C (O)-miscellaneous alkyl aryl, NR18C (O) O-R19, NR18C (O) NR18R18, NHSO ₂-alkyl, NHSO ₂-naphthenic base, NHSO ₂-heterocyclic radical, NHSO ₂-aryl, NHSO ₂-heteroaryl, NHSO ₂-alkyl heterocyclic, NHSO ₂-alkylaryl, NHSO ₂-miscellaneous alkyl aryl, NO ₂, SH, S-alkyl, S-aryl, S-heteroaryl, OH, OCF ₃, O-alkyl, O-R38, O-naphthenic base, O-heterocyclic radical, O-aryl; The O-heteroaryl, O-alkyl-cycloalkyl, O-alkyl heterocyclic, O-alkylaryl, O-miscellaneous alkyl aryl, OC (O)-alkyl; OC (O)-R38, OC (O)-naphthenic base, OC (O)-heterocyclic radical, OC (O)-aryl, OC (O)-heteroaryl, OC (O)-alkyl-cycloalkyl; OC (O)-alkyl heterocyclic OC (O)-alkylaryl, OC (O)-miscellaneous alkyl aryl, OC (O) O-R19, OC (O) NR18R18, OSO ₃H, OSO ₂-alkyl, OSO ₂-naphthenic base, OSO ₂-heterocyclic radical, OSO ₂-aryl, OSO ₂-heteroaryl, OSO ₂-alkylaryl, OSO ₂-miscellaneous alkyl aryl, OP (O) (OH) ₂, OP (O) (O alkyl) ₂, OP (O) (O aryl) ₂, C (O)-alkyl, C (O)-aryl, C (O)-heteroaryl, CO ₂H, CO ₂-alkyl, CO ₂-R38, CO ₂-naphthenic base, CO ₂-heterocyclic radical, CO ₂-aryl, CO ₂-heteroaryl, CO ₂-alkyl-cycloalkyl, CO ₂-alkyl heterocyclic, CO ₂-alkylaryl, CO ₂-miscellaneous alkyl aryl, C (O)-NH ₂, C (O) NH-alkyl, C (O) NH-R38, C (O) NH-naphthenic base, C (O) NH-heterocyclic radical, C (O) NH-aryl, C (O) NH-heteroaryl, C (O) NH-alkyl-cycloalkyl, C (O) NH-alkyl heterocyclic, C (O) NH-alkylaryl, C (O) NH-miscellaneous alkyl aryl, C (O) N (alkyl) ₂, C (O) N (naphthenic base) ₂, C (O) N (aryl) ₂, C (O) N (heteroaryl) ₂, C (O) NR20-alkyl, C (O) NR19-alkyl R21 ,-C (O) NR180-R18 ,-C (O) NR18NR18R18, SO ₂NH ₂, SO ₂The NH-alkyl, SO ₂The NH-aryl, SO ₂The NH-heteroaryl, SO ₂The NH-alkylaryl, SO3H, SO ₂The O-alkyl, SO ₂The O-aryl, SO ₂The O-alkylaryl, alkyl, alkyl-cycloalkyl, alkyl heterocyclic, alkylaryl; Miscellaneous alkyl aryl, naphthenic base, heterocyclic radical, aryl or heteroaryl, and said alkyl; Naphthenic base, heterocyclic radical, aryl, heteroaryl; Alkyl-cycloalkyl, alkyl heterocyclic, alkylaryl and miscellaneous alkyl aryl substituting group can and then be substituted itself

OR29, wherein R29 can be an alkyl, naphthenic base, heterocyclic radical, aryl; Heteroaryl, alkyl-cycloalkyl, alkyl heterocyclic, alkylaryl or miscellaneous alkyl aryl, and said alkyl; Naphthenic base, heterocyclic radical, aryl, heteroaryl; Alkyl-cycloalkyl, alkyl heterocyclic, alkylaryl or miscellaneous alkyl aryl substituting group can and then be substituted itself

SR30, wherein R30 can be an alkyl, naphthenic base, heterocyclic radical, aryl; Heteroaryl, alkyl-cycloalkyl, alkyl heterocyclic, alkylaryl or miscellaneous alkyl aryl; And said alkyl, naphthenic base, heterocyclic radical, aryl and heteroaryl; Alkyl-cycloalkyl, alkyl heterocyclic, alkylaryl or miscellaneous alkyl aryl substituting group can and then be substituted itself

NR31R32, wherein R31 and R32 can be hydrogen independently of one another, alkyl, naphthenic base, heterocyclic radical, aryl, heteroaryl, alkyl-cycloalkyl, alkyl heterocyclic, alkylaryl, miscellaneous alkyl aryl ,-C (O)-R33 ,-SO ₂R33 ,-C (O) OR33 and-C (O)-NR34R35, wherein R33 can be an alkyl, naphthenic base, heterocyclic radical, aryl; Heteroaryl, alkyl-cycloalkyl, alkyl heterocyclic, alkylaryl, miscellaneous alkyl aryl, and R34 and R35 can be hydrogen independently of one another; Alkyl, naphthenic base, heterocyclic radical, aryl, heteroaryl, alkyl-cycloalkyl; Alkyl heterocyclic, alkylaryl, miscellaneous alkyl aryl, or R34 and R35 can form heterocyclic ring together

Or R31 and R32 can form heterocyclic ring together,

And said alkyl, naphthenic base, heterocyclic radical, aryl and heteroaryl, alkyl-cycloalkyl, alkyl heterocyclic, alkylaryl or miscellaneous alkyl aryl substituting group can and then be substituted itself,

And R21 can be a naphthenic base, heterocyclic radical, and aryl, heteroaryl,

And R38 can be an alkyl, and wherein alkyl can be straight chain or ramose saturated or unsaturated, that have 9-30 carbon atom, i.e. C _9-30-alkyl, C _9-30-alkenyl and C _9-30-alkynyl.Alkenyl has the two keys of at least one C-C, and alkynyl has at least one C-C triple bond, and wherein alkenyl can exist with (E)-or (Z)-conformation.Preferably, said alkyl is selected from: nonyl, decyl, dodecyl, hexadecyl, octadecyl, eicosyl, henicosyl, docosyl, tetracosyl, nonacosyl, octadecylene base, docosene base, two tetradecene bases and two octadecylene bases.

Pyrido [2,3-b] pyrazines derivatives, the wherein R2=H of special preference general formula (II).

Pyrido [2, the 3-b] pyrazines derivatives of further special preference general formula (II), wherein R2 and R4=H.

Special following general formula (I) and pyrido (II) [2, the 3-b] pyrazines derivatives of preference, they can exist with their free alkali form or as the sour pharmacologically acceptable salt of physiological tolerance:

Compound 1 1-ethyl-3-(3-phenylacetylene yl pyridines is [2,3-b] pyrazine-6-yl also) urea

Compound 2 1-ethyl-3-(3-thiene-3-yl-ethynyl pyridine is [2,3-b] pyrazine-6-yl also) urea

Compound 3 1-(3-cyclopropyl acethlene yl pyridines is [2,3-b] pyrazine-6-yl also)-3-ethyl carbamide

Compound 4 1-[3-(3-dimethylamino third-1-alkynyl) pyrido [2,3-b] pyrazine-6-yl]-3-ethyl carbamide

Compound 5 1-[3-((E)-2-cyclohexyl vinyl) pyrido [2,3-b] pyrazine-6-yl]-3-ethyl carbamide

Compound 6 1-ethyl-3-[3-((E)-3-methoxy propyl thiazolinyl) pyrido [2,3-b] pyrazine-6-yl] urea

Compound 7

Compound 8

Compound 9 4-[6-(3-ethyl carbamide) pyrido [2,3-b] pyrazine-3-yl] phenyl methyl carbonic ether

Compound 10 4-[6-(3-ethyl carbamide) pyrido [2,3-b] pyrazine-3-yl] phenyl 2-methoxy ethyl carbonic ether

Compound 11 4-[6-(3-ethyl carbamide) pyrido [2,3-b] pyrazine-3-yl] phenyl carbonic ether

Compound 12 4-[6-(3-ethyl carbamide) pyrido [2,3-b] pyrazine-3-yl] diethylamino phenyl aminocarbamic acid ester

Compound 13 4-[6-(3-ethyl carbamide) pyrido [2,3-b] pyrazine-3-yl] phenyl (E)-3-phenyl acrylate

Compound 14 4-[6-(3-ethyl carbamide) pyrido [2,3-b] pyrazine-3-yl] phenyl nonadecane acid esters

Compound 15 1-(the 3-benzyl-pyridine is [2,3-b] pyrazine-6-yl also)-3-ethyl carbamide

Compound 16 3-[6-(3-ethyl carbamide) pyrido [2,3-b] pyrazine-3-yl] phenyl 2-methoxy ethyl carbonic ether

Compound 17 4-[6-(3-ethyl carbamide) pyrido [2,3-b] pyrazine-3-yl] phenyl isobutyl-carbonic ether

Compound 18 fourths-2-alkynyl 4-[6-(3-ethyl carbamide) pyrido [2,3-b] pyrazine-3-yl] benzol carbonate

Compound 19 4-[6-(3-ethyl carbamide) pyrido [2,3-b] pyrazine-3-yl] phenyl dimethylcarbamate

Compound 20 4-[6-(3-ethyl-1-phenylurea) pyrido [2,3-b] pyrazine-3-yl] phenyl ethyl carbamate

Compound 21 tertiary butyls { 4-[6-(3-ethyl carbamide) pyrido [2,3-b] pyrazine-3-yl] phenyl }-carbamate

Compound 22 2-methoxy ethyl 4-[6-(3-ethyl carbamide) pyrido [2,3-b] pyrazine-3-yl] phenyl }-carbamate

Compound 23 1-ethyl-3-{3-[4-(3-ethyl carbamide) phenyl] pyrido [2,3-b] pyrazine-6-yl } urea

Compound 24 1-{3-[4-(3, the 3-dimethyl urea) phenyl] pyrido [2,3-b] pyrazine-6-yl }-the 3-ethyl carbamide

Compound 25 1-ethyl-3-{3-[6-(3-ethyl carbamide) pyridin-3-yl] pyrido [2,3-b] pyrazine-6-yl } urea

Compound 26 1-ethyl-3-{3-[2-(4-fluorophenyl) ethyl] pyrido [2,3-b] pyrazine-6-yl } urea

Compound 27 1-ethyl-3-{3-[(E)-and 2-(4-fluorophenyl) vinyl] pyrido [2,3-b] pyrazine-6-yl }-urea

Compound 28 1-ethyl-3-[3-(4-morpholine-4-ylmethyl phenyl) pyrido [2,3-b] pyrazine-6-yl] urea

Compound 29 1-ethyl-3-(3-{4-[2-(2-methoxy ethoxy) oxyethyl group] phenyl } pyrido [2,3-b] pyrazine-6-yl) urea

Compound 30 N-{4-[6-(3-ethyl carbamide) pyrido [2,3-b] pyrazine-3-yl] phenyl }-2-(2-methoxy ethoxy) ethanamide

Compound 31 N-[6-(3-ethyl carbamide) pyrido [2,3-b] pyrazine-3-yl]-4-methyl benzamide

Compound 32 4-[6-(3-ethyl carbamide) pyrido [2,3-b] pyrazine-3-yl]-2-p-methoxy-phenyl 2-methoxy ethyl carbonic ether

Compound 33 2-benzyloxy ethyl 4-[6-(3-ethyl carbamide) pyrido [2,3-b] pyrazine-3-yl] benzol carbonate

Compound 34 2-benzyloxy ethyl 4-[6-(3-ethyl carbamide) pyrido [2,3-b] pyrazine-3-yl]-2-p-methoxy-phenyl carbonic ether

Compound 35 2-benzyloxy-N-{4-[6-(3-ethyl carbamide) pyrido [2,3-b] pyrazine-3-yl] phenyl }-ethanamide

Compound 36 1-[4-(tertiary butyl dimethylsilyl oxygen base) butyl]-3-(the 3-phenylpyridine is [2,3-b]-pyrazine-6-yl also) urea

Compound 37 1-[4-(tertiary butyl dimethylsilyl oxygen base) butyl]-3-[3-(4-hydroxy 3-methoxybenzene base) pyrido [2,3-b] pyrazine-6-yl] urea

Compound 38 4-[3-(the 3-phenylpyridine is [2,3-b] pyrazine-6-yl also) urea] butyl ethyl carbamate

Compound 39 methyl 4-[3-(the 3-phenylpyridine is [2,3-b] pyrazine-6-yl also) urea] butyl carbonic ether

Compound 40 2,2-dimethyl-[1,3] dioxolane-4-ylmethyl 4-[3-(the 3-phenylpyridine is [2,3-b] pyrazine-6-yl also) urea] butyl carbonic ether

Compound 41 2,3-dihydroxypropyl 4-[3-(the 3-phenylpyridine is [2,3-b] pyrazine-6-yl also) urea]-butyl carbonic ether

Compound 42 diethylammonium { 4-[3-(the 3-phenylpyridine is [2,3-b] pyrazine-6-yl also) urea] butyl }-SULPHOSUCCINIC ACID ESTER

Compound 43 { 4-[3-(the 3-phenylpyridine is [2,3-b] pyrazine-6-yl also) urea] butyl } phosphoric acid

Compound 44 diethylammonium (4-{3-[3-(4-hydroxy 3-methoxybenzene base) pyrido [2,3-b] pyrazine-6-yl] urea } butyl) SULPHOSUCCINIC ACID ESTER

Compound 45 (4-{3-[3-(4-hydroxy 3-methoxybenzene base) pyrido [2,3-b] pyrazine-6-yl] urea } butyl) phosphoric acid

Compound 46 1-ethyl-3-[3-(3-TMS phenyl) pyrido [2,3-b] pyrazine-6-yl] urea

Compound 47 1-[3-(the 4-cyclohexyl phenyl is amino) pyrido [2,3-b] pyrazine-6-yl]-3-ethyl carbamide

Compound 48 1-ethyl-3-[3-(4-methane sulfonyl phenyl amino) pyrido [2,3-b]-pyrazine-6-yl] urea

Compound 49 N-{5-[6-(3-ethyl carbamide) pyrido [2,3-b] pyrazine-3-base is amino]-2-methyl-phenyl } NSC-249992

Compound 50 3-[6-(3-ethyl carbamide) pyrido [2,3-b] pyrazine-3-base is amino]-N-methyl-BM

Compound 51 1-ethyl-3-[3-(4-piperidines-1-ylmethyl phenyl amino) pyrido [2,3-b]-pyrazine-6-yl] urea

Compound 52 1-ethyl-3-[3-(4-thiene-3-yl-phenyl amino) pyrido [2,3-b] pyrazine-6-yl] urea

Compound 53 N-{4-[6-(3-ethyl carbamide) pyrido [2,3-b] pyrazine-3-base is amino] phenyl }-ethanamide

Compound 54 3-[6-(3-ethyl carbamide) pyrido [2,3-b] pyrazine-3-base is amino] ethyl benzoate

Compound 55 4-[6-(3-ethyl carbamide) pyrido [2,3-b] pyrazine-3-yl] phenyl 2-methoxy ethyl carbonate salt hydrochlorate

Compound 56 2-methoxy ethyl 4-[6-(3-ethyl carbamide) pyrido [2,3-b] pyrazine-3-yl] benzol carbonate tosilate

Compound 57 4-{6-[3-(4-hydroxybutyl) urea] pyrido [2,3-b] pyrazine-3-yl } phenyl 2-methoxy ethyl carbonic ether

Compound 58 4-{6-[3-(4-hydroxybutyl) urea] pyrido [2,3-b] pyrazine-3-yl } phenyl 2-methoxy ethyl carbonate salt hydrochlorate

Compound 59 N-(the 3-phenylpyridine is [2,3-b] pyrazine-6-yl also) oxalic monoamide ethyl ester

Compound 60 N-ethyl-N '-(the 3-phenylpyridine is [2,3-b] pyrazine-6-yl also) oxamide

Compound 61

Compound 62 diethylammonium { 2-[3-(the 3-phenylpyridine is [2,3-b] pyrazine-6-yl also) urea] ethyl }-SULPHOSUCCINIC ACID ESTER

Compound 63 { 2-[3-(the 3-phenylpyridine is [2,3-b] pyrazine-6-yl also) urea] ethyl } phosphoric acid

Compound 64 1-[3-(2-diethylamino ethoxy) propyl group]-3-[3-(4-hydroxyl-3-methoxyl group-phenyl) pyrido [2,3-b] pyrazine-6-yl] urea

Compound 65 (2,2-dimethyl propylene acyloxy methoxyl group)-(4-{3-[3-(4-hydroxyl-3-methoxyl group-phenyl) pyrido [2,3-b] pyrazine-6-yl] urea } butyl) inferior phosphonato methyl 2,2-dimethyl--propionic ester

Compound 66 1-[(1-acetoxyethoxy)-(and 4-{3-[3-(4-hydroxy 3-methoxybenzene base)-pyrido [2,3-b] pyrazine-6-yl] urea } butyl) inferior phosphonato] ETHYLE ACETATE

Compound 67 4-[6-(3-ethyl carbamide) pyrido [2,3-b] pyrazine-3-yl] 2-p-methoxy-phenyl diethylamino manthanoate

Compound 68 2-chloro-4-[6-(3-ethyl carbamide) pyrido [2,3-b] pyrazine-3-yl]-6-methoxyl group-diethylamino phenyl aminocarbamic acid ester

Compound 69 4-[6-(3-ethyl carbamide) pyrido [2,3-b] pyrazine-3-yl]-2-p-methoxy-phenyl 2-[2-(2-methoxy ethoxy) oxyethyl group] ethyl carbonate ester

Compound 70 1-ethyl-3-{3-[4-(morpholine-4-alkylsulfonyl) phenyl amino] pyrido [2,3-b] pyrazine-6-yl } urea

Compound 71 5-[6-(3-ethyl urea groups) pyrido [2,3-b] pyrazine-3-base is amino]-2-hydroxy-benzoic acid ethyl ester

Compound 72 1-[3-(3-diethylin methyl-4-hydroxy phenyl is amino) pyrido [2,3-b] pyrazine-6-yl]-3-ethyl carbamide

Compound 73 1-ethyl-3-[3-(6-morpholine-4-yl pyridines-3-base is amino) pyrido [2,3-b] pyrazine-6-yl] urea

Compound 74 1-ethyl-3-{3-[3-(1H-tetrazolium-5-yl) phenyl amino] pyrido [2,3-b] pyrazine-6-yl } urea

Compound 75 1-ethyl-3-[3-(3-morpholine-4-base phenyl amino) pyrido [2,3-b] pyrazine-6-yl] urea

Compound 76 1-ethyl-3-[3-(4-imidazoles-1-base phenyl amino) pyrido [2,3-b] pyrazine-6-yl] urea

Compound 77 1-ethyl-3-[3-(4-tetramethyleneimine-1-base phenyl amino) pyrido [2,3-b] pyrazine-6-yl] urea

Compound 78 1-ethyl-3-{3-[4-(4-N-METHYL PIPERAZINE-1-yl) phenyl amino] pyrido [2,3-b] pyrazine-6-yl } urea

Compound 79 1-ethyl-3-[3-(3-piperidines-1-ylmethyl phenyl amino) pyrido [2,3-b] pyrazine-6-yl] urea

Compound 80 1-ethyl-3-[3-(4-morpholine-4-ylmethyl phenyl amino) pyrido [2,3-b] pyrazine-6-yl] urea

Compound 81 1-{3-[3-(2-cyclohexyl oxyethyl group) phenyl amino] pyrido [2,3-b] pyrazine-6-yl }-the 3-ethyl carbamide

Compound 82 1-ethyl-3-[3-(3-[1,2,4] triazol-1-yl aminomethyl phenyl is amino) pyrido [2,3-b] pyrazine-6-yl] urea

Compound 83 2,2-dimethyl-[1,3] dioxolane-4-ylmethyl 4-{3-[3-(4-hydroxy 3-methoxybenzene base) pyrido [2,3-b] pyrazine-6-yl] urea groups } the butyl carbonic ether

Compound 84 2,3-dihydroxypropyl 4-{3-[3-(4-hydroxy 3-methoxybenzene base) pyrido [2,3-b] pyrazine-6-yl] urea groups } the butyl carbonic ether

Compound 85 1-[3-(2-diethylamino ethoxy) propyl group]-3-[3-(4-hydroxy 3-methoxybenzene base) pyrido [2,3-b] pyrazine-6-yl] urea

For fear of ambiguity: when the chemical structure of the compound of top demonstration and chemical name did not match by error each other, said chemical structure defined the compound of certain well definitely.

Unified hereinafter be called " compound of the present invention " of the general formula (I) that shows above and generalize compound (II), preferred embodiment and specifically mentioned pyridopyrazine compound 1-85.

Only if explanation is arranged in specification sheets or claims in addition, each is as follows self-defined in principle for statement and the term that is used to explain compound of the present invention:

In context of the present invention, statement " alkyl " comprises acyclic saturated or unsaturated alkyl, and it can be ramose or straight chain, and has 1-8 carbon atom, i.e. C _1-8-alkyl, C _2-8-alkenyl and C _2-8-alkynyl.Alkenyl has the two keys of at least one C-C, and alkynyl has at least one C-C triple bond.Alkynyl also can have the two keys of at least one C-C in addition.Preferred alkyl is a methyl, ethyl, n-propyl, 2-propyl group, normal-butyl, sec.-butyl, the tertiary butyl, n-pentyl; Isopentyl, neo-pentyl, n-hexyl, 2-hexyl, n-heptyl, n-octyl; N-nonyl, positive decyl, n-undecane base, dodecyl, ethylenyl (vinyl), ethynyl, propenyl (CH ₂CH=CH ₂-CH=CH-CH ₃,-C (=CH ₂)-CH ₃), proyl (CH ₂-C ≡ CH ,-C ≡ C-CH ₃), crotonyl, butynyl, pentenyl, pentynyl, hexenyl, hexyn, heptenyl, heptyne base, octenyl, octadienyl and octyne base.

In context of the present invention, statement " (C ₉-C ₃₀) alkyl " acyclic saturated or unsaturated alkyl has been described, it can be ramose or straight chain, and has 9-30 carbon atom, i.e. C _9-30-alkyl, C _9-30-alkenyl and C _9-30-alkynyl.C _9-30-alkenyl has the two keys of at least one C-C, and C _9-30-alkynyl has at least one C-C triple bond.C _9-30-alkynyl also can have the two keys of at least one C-C in addition.Preferred (C ₉-C ₃₀) alkyl is tetradecyl, hexadecyl, octadecyl, eicosyl, cis-13-docosene base (erucyl), anti-form-1 3-docosene base (brassidyl), cis-15-two tetradecene bases (nervonyl) and anti-form-1 5-two tetradecene bases.

For the purposes of the present invention, statement " naphthenic base " is meant the non-aromatic hydrocarbon of ring-type, and it has 1-3 and has 3-20, the ring of preferred 3-12 carbon atom, and it can be saturated or undersaturated, more preferably (C ₃-C ₈) naphthenic base.Said naphthenic base also can be the part of dicyclo or multi-loop system, and wherein for example, said naphthenic base is through any possible and ring members that hope, and the aryl, heteroaryl or the heterocyclic radical that define with this paper condense.Through any possible ring members of naphthenic base, can realize bonding with the compound of general formula (I), (II).Preferred naphthenic base is a cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, suberyl, ring octyl group, ring decyl, cyclohexenyl, cyclopentenyl and cyclooctadiene base.

3-to 14-unit, preferred 3-, 4-, 5-, 6-are represented in statement " heterocyclic radical "; 7-or 8-unit, cyclic organic group, it contains at least 1 heteroatoms, and randomly 2; 3,4 or 5 heteroatomss, especially nitrogen, oxygen and/or sulphur; Said heteroatoms is identical or different, and said cyclic group is saturated or unsaturated, but is not aromatics.Said heterocyclic radical also can be the part of dicyclo or multi-loop system, and wherein for example, said heterocyclic radical is through any possible and ring members that hope, with aryl, the heteroaryl or Cycloalkylfused of this paper definition.Through any possible ring members of heterocyclic radical, can realize bonding with the compound of general formula (I), (II).Preferred heterocyclic radical is a tetrahydrofuran base, pyrrolidyl, and imidazolidyl, thiazolidyl, THP trtrahydropyranyl, piperidyl, piperazinyl, morpholinyl, the thia pyrrolidyl, the oxa-piperazinyl, the oxa-piperidyl is with the oxadiazole base.

In context of the present invention, statement " aryl " be meant have 3-14 carbon atom, preferably 5-14 carbon atom, the more preferably aromatic hydrocarbon of 6-14 carbon atom.Said aryl also can be the part of dicyclo or multi-loop system, and wherein for example, said aryl is through any possible and ring members that hope, and heterocyclic radical, heteroaryl or Cycloalkylfused with this paper definition for example condense with following substances: THF; THTP, tetramethyleneimine, imidazolidine, thiazolidine, tetrahydropyrans; Dihydropyrane, piperidines, furans, thiophene; Imidazoles, thiazole ， oxazole ， isoxazole.Through any possible ring members of aryl, can realize bonding with the compound of general formula (I), (II).Preferred aryl groups is a phenyl, xenyl, and naphthyl and anthryl, but also can be indanyl, indenyl or 1,2,3,4-tetralyl.

5-represent in statement " heteroaryl ", the first ring-type aromatic group of 6-or 7-, and it contains at least 1 heteroatoms, if suitable, also contains 2,3,4 or 5 heteroatomss, especially nitrogen, oxygen and/or sulphur, said heteroatoms is identical or different.The number of nitrogen-atoms is 0-3 preferably, the number of oxygen and sulphur atom preferably 0 or 1.Said heteroaryl also can be the part of dicyclo or multi-loop system, and wherein for example, said heteroaryl is through any possible and ring members that hope, with heterocyclic radical, the aryl or Cycloalkylfused of this paper definition.Through any possible ring members of heteroaryl, can realize bonding with the compound of general formula (I), (II).Preferred heteroaryl is a pyrryl, furyl, thienyl, thiazolyl, isothiazolyl ， oxazolyl ， oxadiazole base ， isoxazolyl; Pyrazolyl, imidazolyl, triazole, tetrazolium, pyridyl, pyrimidyl, pyridazinyl, pyrazinyl; Triazine, phthalazinyl, indyl, indazolyl, indolizine, quinolyl, isoquinolyl; Quinoxalinyl, quinazolyl, pteridyl, carbazyl, phenazinyl ， phenoxazinyl, phenothiazinyl and acridyl.

For the purposes of the present invention, statement " alkyl-naphthenic base ", " cycloalkylalkyl ", " alkyl-heterocyclic radical "; " heterocyclic radical alkyl ", " alkyl-aryl ", " arylalkyl ", " alkyl-heteroaryl " and " heteroarylalkyl " is meant alkyl; Naphthenic base, heterocyclic radical, aryl and heteroaryl as above define separately; And said naphthenic base, heterocyclic radical, aryl and heteroaryl are through alkyl, preferred C ₁-C ₈-alkyl, more preferably C ₁-C ₄-alkyl is bonded to the compound of general formula (I), (II).

With " alkyl ", " naphthenic base ", " heterocyclic radical ", " aryl "; " heteroaryl ", " alkyl-naphthenic base ", " alkyl-heterocyclic radical ", " alkyl-aryl " and " alkyl-heteroaryl " combines; Term " replacement " is only if clear and definite definition above in specification sheets or claims, providing is meant that in context of the present invention one or more hydrogen are replaced by following substituting group: F, Cl, Br; I, CN, CF ₃, NH ₂, NH-alkyl, NH-aryl, N (alkyl) ₂, NO ₂, SH, S-alkyl, OH, OCF ₃, O (alkyl-O) _p-alkyl, O-aryl, OSO ₃H, OP (O) (OH) ₂, OP (O) (O alkyl) ₂, OP (O) (O aryl) ₂, CHO, C (O) OH, C (O) OR36, C (O) NH ₂, C (O) NHR36, C (O) NR36R37, SO ₃H, SO ₂Alkyl, SO ₂Aryl, P (O) (OH) ₂, P (O) (O alkyl) ₂, P (O) (O aryl) ₂, alkyl, naphthenic base, heterocyclic radical; Aryl, heteroaryl or alkylaryl, wherein p can be 0,1,2,3,4 or 5 value, and wherein said R36 and R37 group can be alkyl independently of one another; Naphthenic base, heterocyclic radical, aryl, heteroaryl; Alkyl-naphthenic base, alkyl-heterocyclic radical, alkyl-aryl or alkyl-heteroaryl, and R36 and R37 can form heterocyclic ring together.Substituting group can be identical or different, and replacement can occur in any hope and the possible position of alkyl, naphthenic base, heterocyclic radical, aryl and heteroaryl.

In context of the present invention, " halogen " comprises the halogen atom fluorine, chlorine, bromine and iodine in statement.

Polysubstituted group is meant,, for example on same carbon atom, replaced by three by the group of polysubstituted (for example two-or three replace) at homoatomic place not or at same atom place, as at CF ₃,-CH ₂CF ₃Situation under, or be substituted, as at-CH (OH)-CH=CH-CHCl at different positions ₂Situation under.Polysubstituted can the realization with identical substituting group or different substituting groups.

When compound of the present invention has at least one asymmetric center; Their existence form can be: their racemic compound; Pure enantiomorph and/or diastereomer, or the mixture of these enantiomorphs and/or diastereomer and in material or as the pharmacologically acceptable salt of these compounds.Said mixture can exist with the steric isomer blending ratio of any hope.

For example, through known method itself, can be with having one or more chiral centres and becoming their optically active isomer, i.e. enantiomorph or diastereomer as the compound separation of the present invention that racemic compound exists.Said separation can realize as follows, and the post of going up mutually through chirality separates, or through from optically active solvent recrystallization, or uses optically active acid or alkali, or through deriving with optically active reagent (for example optically active alcohol), subsequently this group of desorption.

Compound of the present invention can exist with their double bond isomer form, as " pure " E or Z isomer, or exists with the form of mixtures of these double bond isomers.

Wherein possible, compound of the present invention can exist with the form of tautomer.

If compound of the present invention has enough bases, for example primary amine, secondary amine or tertiary amine, they can change into their physiological tolerance salt with mineral acid and organic acid.The pharmacologically acceptable salt of compound of the present invention is preferably used hydrochloric acid, Hydrogen bromide, sulfuric acid, phosphoric acid, methylsulfonic acid, tosic acid, carbonic acid, formic acid, acetate, trifluoroacetic acid, sulfoacetic acid, oxalic acid, propanedioic acid, toxilic acid, succsinic acid, tartrate, pyruvic acid, oxysuccinic acid, pamoic acid, racemic melic acid, fumaric acid, lactic acid, Hydrocerol A, L-glutamic acid or aspartic acid.The salt that forms comprises hydrochloride, hydrobromide, vitriol, hydrosulfate, phosphoric acid salt, mesylate, tosylate, carbonate, supercarbonate, formate, acetate, trifluoroacetate, sulfosalicylic acetate, oxalate, malonate, PHENRAMINE MALEATE, SUMATRIPTAN SUCCINATE, tartrate, pyruvate salt, malate, embonate, mandelate, fumarate, lactic acid salt, Citrate trianion, glutaminate or aspartate.The stoichiometry of the salt of the compound of the present invention that forms can be 1 integer or fractional multiple.

If compound of the present invention has enough acidic groups, for example carboxyl or phosphate, they can change into their physiological tolerance salt with mineral alkali and organic bases.The instance of useful mineral alkali comprises sodium hydroxide, Pottasium Hydroxide, calcium hydroxide; The instance of useful organic bases comprises thanomin, diethylolamine, trolamine, hexahydroaniline, dibenzyl-ethylenediamin and Methionin.The stoichiometry of the salt of the compound of the present invention that forms can be 1 integer or fractional multiple.

The solvolyte of same preference compound of the present invention, hydrate especially, they can be through for example obtaining from solvent or aqueous solution crystallization.Can have 1,2,3 or solvolyte as much as possible or water molecules bonding compound of the present invention, form solvolyte and hydrate.

The known chemical material forms solid, and it exists with different order states, is called polymorphic forms or variant.The physical properties of the different variants of polymorphic material can have a great difference.

Compound of the present invention can exist with different polymorphic forms; Some variant possibly be metastable.

Compound of the present invention possibly exist with the form of any prodrug equally, for example ester, carbonic ether, carbamate, urea, acid amides or SULPHOSUCCINIC ACID ESTER, and wherein actual biologically active form only discharges through metabolism.

The known chemical material changes into meta-bolites in vivo, and they are in the biological effect that can cause hope in some cases equally---in some cases, even with more outstanding form.

The corresponding prodrug and the meta-bolites of compound of the present invention should be regarded a part of the present invention as.

Astoundingly and advantageously find that now compound of the present invention also can act on (promptly have and regulate or restraining effect) enzyme in 2 or a plurality of signal transduction pathway or these approach.Have been found that compound highly selective of the present invention works, promptly regulate or inhibition.

2 or a plurality of signal transduction pathway (ras-Raf-Mek-Erk signal pathway for example; PI3K-Akt signal pathway and/or SAPK signal pathway; More specifically Erk1/Erk2 and/or PI3K and/or Jnk and/or p38) (for example dual) adjusting or inhibition of this while; Surpass the only single adjusting or the inhibition of 1 signal transduction pathway, because can realize the Synergistic treatment effect, for example enhanced cell apoptosis and faster and more effective tumor regression.

The wonderful advantageous effect of compound of the present invention; Help to the treatment of 2 or a plurality of signal transduction pathways regulate responsive or physiology and/or pathological and physiological condition or condition by 2 or the mediation of a plurality of signal transduction pathway in, pursue a plurality of regimens.

Also find astoundingly and advantageously; Compound of the present invention also can the highly selective effect (promptly have and regulate or restraining effect), and in the enzyme of ras-Raf-Mek-Erk signal transduction pathway or this approach, a plurality of mechanisms of action and the regimen that detail above also can be used for this signal pathway or enzyme.

Also find astoundingly and advantageously; Compound of the present invention also can the highly selective effect (promptly have and regulate or restraining effect), and in the enzyme of PI3K-Akt signal transduction pathway or this approach, a plurality of mechanisms of action and the regimen that detail above also can be used for this signal pathway or enzyme.

Also find astoundingly and advantageously; Compound of the present invention also can the highly selective effect (promptly have and regulate or restraining effect), and in the enzyme of SAPK signal transduction pathway or this approach, a plurality of mechanisms of action and the regimen that detail above also can be used for this signal pathway or enzyme.

Astoundingly and advantageously find in addition, compound of the present invention also can highly selective effect (promptly have and regulate or restraining effect) in enzyme, ATM for example; ATR; MTOR, DNA-PK and/or hSMG-1, a plurality of mechanisms of action and the regimen that detail above also can be used for these enzymes.

Based on the present invention, term " adjusting " is used in reference to following: " activate, part activates, and suppresses, and part suppresses ".Measuring and measure such activation, part activation, suppress or the part inhibition by means of measurement commonly used and measuring method, is in those of ordinary skills' technical know-how scope.For example, can measure and the activation of determination part branch with respect to activating fully; With respect to suppressing fully, measure and measure part and suppress equally.

According to the present invention, " inhibition " is used in reference to following: " partially or completely suppressing " term.Measuring and measure so partially or completely inhibition by means of measurement commonly used and measuring method, is in those of ordinary skills' technical know-how scope.For example, can measure and measure part and suppress with respect to suppressing fully.

In context of the present invention, the certain enzyme and/or the kinases that all are meant inactive form (non-enzymatic activity) and/or activity form (enzymic activity is arranged) with term " adjusting " and " inhibition " of " enzyme " and/or " kinases " coupling.In context of the present invention, this means that compound of the present invention can be to the enzyme and/or its regulating effect of kinases performance of inactive form, activity form or 2 kinds of forms.

In yet another aspect, through the medicine that comprises at least a compound of the present invention is provided, realized the object of the invention astoundingly.

In yet another aspect, through the medicine that comprises at least a compound of the present invention and at least a other active pharmaceutical ingredient and/or pharmaceutically acceptable carrier and/or vehicle is provided, realized the object of the invention astoundingly.

In yet another aspect; Through the method for producing medicine is provided, realized the object of the invention astoundingly, the method is characterized in that; With pharmaceutically acceptable carrier and/or vehicle processing (promptly processing pharmaceutically acceptable form) one or more compounds of the present invention, to produce pharmaceutical prepn.

In yet another aspect, through compound of the present invention is provided, realized the object of the invention astoundingly, said compound of the present invention can be as the activeconstituents of medicine; Said medicine is used to regulate the cell signalling process of misdirection, and being particularly useful for influences the receptor tyrosine kinase of activated and non-activity and the function of kytoplasm tyrosine, serine/threonine and lipid kinase, and said kinases is c-Raf for example, B-Raf; Mek, MAPKs, PDGFR β, Flt-3; IGF1R, PI3K, PKB/Akt1; C-Kit, c-Ab1, FGFR1 and KDR.

In yet another aspect; Through compound of the present invention is provided; Realized the object of the invention astoundingly, said compound of the present invention can be used to produce medicine, and said medicine is used for treatment or prevents mammiferous physiology and/or pathological and physiological condition; Said treatment or prevention are selected from following signal transduction pathway through adjusting and realize: " the ras-Raf-Mek-Erk signal transduction pathway, PI3K-Akt signal transduction pathway and/or SAPK signal transduction pathway ".

In yet another aspect, through compound of the present invention is provided, realized the object of the invention astoundingly; Said compound of the present invention can be used to produce medicine; Said medicine is used to treat or prevents mammiferous by the physiology and/or the pathophysiological state that are selected from following enzyme mediation: " ATM, ATR, mTOR; DNA-PK, hSMG-1 ".

In yet another aspect, through compound of the present invention is provided, realized the object of the invention astoundingly; Said compound of the present invention can be used to produce medicine, and said medicine is used for treatment or prevents mammiferous physiology and/or pathological and physiological condition, and said treatment or prevention are selected from following enzyme and realize through modifying one or more: " ATM; ATR; mTOR, DNA-PK, hSMG-1 ".

In a preferred embodiment; Compound of the present invention is provided; Be used to produce medicine; Said medicine is used to treat and/or prevent mammiferous physiology and/or pathological and physiological condition by ras-Raf-Mek-Erk signal transduction pathway and/or the mediation of PI3K-Akt signal transduction pathway; And/or be used to produce medicine, and said medicine is used for treatment or prevents mammiferous physiology and/or pathological and physiological condition, and said treatment or prevention realize through regulating ras-Raf-Mek-Erk signal transduction pathway and PI3K-Akt signal transduction pathway.

In yet another aspect; Through compound of the present invention is provided; Realized the object of the invention astoundingly; Said compound of the present invention can be used to produce medicine, and said medicine is used to treat or prevents mammiferous physiology and/or pathophysiological state by the mediation of ras-Raf-Mek-Erk signal transduction pathway.

In yet another aspect; Through compound of the present invention is provided; Realized the object of the invention astoundingly; Said compound of the present invention can be used to produce medicine, and said medicine is used to treat or prevents mammiferous physiology and/or pathological and physiological condition by the mediation of PI3K-Akt signal transduction pathway.

In yet another aspect; Through compound of the present invention is provided; Realized the object of the invention astoundingly; Said compound of the present invention can be used to produce medicine, and said medicine is used for treatment or prevents mammiferous physiology and/or pathological and physiological condition, and said treatment or prevention realize through regulating the PI3K-Akt signal transduction pathway.

In a preferred embodiment; Compound of the present invention is provided; Be used to produce medicine; Said medicine is used to treat and/or prevent mammiferous physiology and/or pathological and physiological condition by SAPK signal transduction pathway and/or the mediation of PI3K-Akt signal transduction pathway; And/or be used to produce medicine, and said medicine is used for treatment or prevents mammiferous physiology and/or pathological and physiological condition, and said treatment or prevention realize through regulating SAPK signal transduction pathway and PI3K-Akt signal transduction pathway.

In yet another aspect; Through compound of the present invention is provided; Realized the object of the invention astoundingly, said compound of the present invention can be used to produce medicine, and said medicine is used to treat or prevents mammiferous physiology and/or pathological and physiological condition by the mediation of SAPK signal transduction pathway.

In yet another aspect; Through compound of the present invention is provided; Realized the object of the invention astoundingly; Said compound of the present invention can be used to produce medicine, and said medicine is used for treatment or prevents mammiferous physiology and/or pathological and physiological condition, and said treatment or prevention realize through regulating the SAPK signal transduction pathway.

In a preferred embodiment, compound of the present invention is provided, is used for such use; The adjusting of ras-Raf-Mek-Erk signal transduction pathway is selected from the enzyme of " Tyrosylprotein kinase, serine/threonine kinase, receptor tyrosine kinase; cytoplasmic tyrosine kinase, kytoplasm serine/threonine kinase " and realizes that said enzyme preferably is selected from through regulating one or more: " Erk; Erk1, Erk2 ".

In another preferred embodiment, compound of the present invention is provided, is used for such use; The adjusting of PI3K-Akt signal transduction pathway realizes that through the enzyme of regulating one or more and be selected from " lipid kinase " said enzyme preferably is selected from: " PI3K, PI3K α; PI3K β, PI3K γ, PI3K δ; PI3K-C2 α, PI3K-C2 β, PI3K-Vps34p ".

In another preferred embodiment, compound of the present invention is provided, is used for such use, the adjusting of SAPK signal transduction pathway is selected from the enzyme of " Tyrosylprotein kinase, serine/threonine kinase; receptor tyrosine kinase, cytoplasmic tyrosine kinase, kytoplasm serine/threonine kinase " and realizes that said enzyme preferably is selected from through regulating one or more: " Jnk; Jnk1, Jnk2, Jnk3, p38; p38 α, p38 β, p38 γ, p38 δ ".

In yet another aspect; Through the compound of the present invention according to above-mentioned aspect, preferred embodiment and purposes is provided; Realized the object of the invention astoundingly; Said compound of the present invention can be used to produce medicine, and said medicine is used for treatment or prevents mammiferous physiology and/or pathological and physiological condition, and said treatment or prevention realize through regulating 2 kinds or plurality of enzymes.

In a preferred embodiment, compound of the present invention is provided, be used for such use, at least a enzyme in treatment or the prevention is through regulating 2 kinds or more kinds ofly be selected from following enzyme and realize: " Erk; Erk1, Erk2 ", and at least a enzyme is selected from: " PI3K, PI3K α; PI3K β, PI3K γ, PI3K δ; PI3K-C2 α, PI3K-C2 β, PI3K-Vps34p ".

In a preferred embodiment, compound of the present invention is provided, be used for such use, at least a enzyme in treatment or the prevention is through regulating 2 kinds or multiplely be selected from following enzyme and realize: " Jnk, Jnk1; Jnk2, Jnk3, p38, p38 α, p38 β; p38 γ, p38 δ ", and at least a enzyme is selected from: " PI3K, PI3K α, PI3K β; PI3K γ, PI3K δ, PI3K-C2 α, PI3K-C2 β, PI3K-Vps34p ".

In a preferred embodiment, compound of the present invention is provided, be used for such use; At least a enzyme in treatment or the prevention is through regulating 2 kinds or more kinds ofly be selected from following enzyme and realize: " Erk, Erk1, Erk2 "; And at least a enzyme is selected from: " ATM, ATR, mTOR; DNA-PK, hSMG-1 ".

In a preferred embodiment, compound of the present invention is provided, be used for such use, at least a enzyme in treatment or the prevention is through regulating 2 kinds or more kinds ofly be selected from following enzyme and realize: " Jnk, Jnk1; Jnk2, Jnk3, p38, p38 α; p38 β, p38 γ, p38 δ ", and at least a enzyme is selected from: " ATM; ATR, mTOR, DNA-PK, hSMG-1 ".

In a preferred embodiment, compound of the present invention is provided, be used for such use, at least a enzyme in treatment or the prevention is through regulating 2 kinds or more kinds ofly be selected from following enzyme and realize: PI3K; PI3K α, PI3K β, PI3K γ, PI3K δ; PI3K-C2 α, PI3K-C2 β, PI3K-Vps34p ", and at least a enzyme is selected from: " ATM; ATR, mTOR, DNA-PK, hSMG-1 ".

In another preferred embodiment, compound of the present invention is provided, is used for such use, said adjusting is to suppress.

In context of the present invention, compound of the present invention can be used to all known Mammalss, people especially, is used to treat and/or prevent.

In another preferred embodiment, the present invention provides compounds for the above purposes, the mammal is selected from: "Man, useful animal, livestock, domesticated pets, cattle, cows, sheep, pigs, goats , horse, pony, donkeys, hinnies, mules, rabbits, rabbits, cats, dogs, guinea pigs, hamsters, rats, mice, "preferably a human.

In context of the present invention, compound of the present invention can be used to treat and/or prevent all known physiology/or pathological and physiological condition.

In a preferred embodiment, compound of the present invention is provided, is used for such use, said physiology and/or pathological and physiological condition are selected from: " malignant tumour, innocent tumour, inflammatory disorder, inflammation, pain, rheumatosis; arthritis, HIV infects, neuroscience or neurodegenerative disorders, rheumatosis, sacroiliitis, AIDS, ARC (AIDS be correlated with complex), Kaposi sarcoma is derived from the tumour of brain and/or neural system and/or meninx; dementia, alzheimer's disease, excess proliferative disease, psoriatic, endometriosis, cicatrization, benign prostatic hyperplasia (BPH), disorder of immune system, autoimmune disease; immune deficiency disorder, colon knurl, gastric tumor, intestinal tumor, lung tumor, pancreas tumor, ovarian tumor, prostate tumor, white blood disease; melanoma, liver tumor, tumor of kidney, a tumour, laryngeal neoplasm, neurospongioma, mastoncus, uterus carcinoma; carcinoma of endometrium, cervical cancer, cerebral tumor, gland cancer, bladder cancer, gastric tumor, colorectum tumour, the esophageal carcinoma; Gynecological tumor, ovarian tumor, thyroid carcinoma, lymphoma, chronic leukemia, acute leukemia, restenosis, mellitus; Diabetic nephropathy, fibrotic conditions, cystic fibrosis, malignant nephrosclerosis, thrombotic microangiopathy syndrome, organ-graft refection, glomerulopathy, metabolic disease; Solid tumor, rheumatic arthritis, diabetic retinopathy, asthma, transformation reactions, allergic disorder, chronic obstructive pulmonary disease, inflammatory bowel; Fibrosis, atherosclerosis, heart trouble, cardiovascular diseases, myocardosis, vascular disorder, blood vessel originality illness, ephrosis; Rhinitis, Graves disease, local asphyxia, heart failure, ischemic, cardiac hypertrophy, renal failure, myocardial cell's dysfunction; Hypertension, vasoconstriction, apoplexy, anaphylactic shock, platelet aggregation, skeletal muscle atrophy, obesity is overweight; The glucose homeostasis, congestive heart failure, stenocardia, heart attack, myocardial infarction, hyperglycemia, hypoglycemia, hypertension ".

In another aspect of the present invention; Through the compound of the present invention according to above-mentioned aspect, preferred embodiment and purposes is provided; Realized the object of the invention astoundingly; Said compound of the present invention is used to produce medicine, and said medicine is used for treatment or prevents mammiferous physiology and/or pathological and physiological condition, said medicine to comprise at least a other pharmacological active substance.

In another aspect of the present invention; Through the compound of the present invention according to above-mentioned aspect, preferred embodiment and purposes is provided; Realized the object of the invention astoundingly; Said compound of the present invention is used to produce medicine, and said medicine is used for treatment or prevents mammiferous physiology and/or pathological and physiological condition, and said medicine is before treating with at least a other pharmacological active substance and/or in the process and/or use afterwards.

In another aspect of the present invention; Through the compound of the present invention according to above-mentioned aspect, preferred embodiment and purposes is provided; Realized the object of the invention astoundingly; Said compound of the present invention is used to produce medicine, and said medicine is used for treatment or prevents mammiferous physiology and/or pathological and physiological condition, and said medicine is before with radiotherapy and/or operative treatment and/or in the process and/or use afterwards.

In context of the present invention, compound of the present invention can be used with all known pharmacological active substances in described combination therapy.

In a preferred embodiment, compound of the present invention is provided, is used for such use; Other pharmacological active substance is selected from: " DNA topoisomerase I and/or II suppressor factor, DNA intercalator, alkylating agent; tubulin destabilizing agent, hormone and/or growth factor receptors agonist and/or antagonist are to the antibody of growth factor and their acceptor; SU11752, antimetabolite ".

In a preferred embodiment, compound of the present invention is provided, is used for such use, other pharmacological active substance is selected from: " Asparaginase, bleomycin, carboplatin, carmustine, TV, cis-platinum; Asparaginase, endoxan, cytosine arabinoside, dicarbazine, gengshengmeisu, daunorubicin, Dx (Zorubicin), epirubicin, VP; 5 FU 5 fluorouracil, altretamine, hydroxyurea, ifosfamide, irinotecan, LV, lomustine, mustargen, 6-mercaptopurine; mesna, methotrexate, ametycin, mitoxantrone, prednisolone, prednisone, Procarbazine, raloxifene, streptozocin; tamoxifen, Tioguanine, hycamtin, vinealeucoblastine(VLB), vincristine(VCR), vindesine, aminoglutethimide, altheine enzyme, azathioprine; 5-azacytidine, CldAdo, busulfan, stilboestrol, 2 ', 2 '-the difluoro Deoxyribose cytidine, docetaxel, red moss hydroxyl nonyl VITAMIN B4 (erythrohydroxynonyladenine), ethinylestradiol; The 5 FU 5 fluorouracil deoxynucleoside, 5 FU 5 fluorouracil deoxynucleoside monophosphate, NSC-328002, Ultrene, flutamide, Hydroxyprogesterone caproate bp 98, idarubicin, Interferon, rabbit; Veramix, acetate megestrol, melphalan, mitotane, taxol, oxaliplatin, pentostatin, N-phosphono ethanoyl-L-aspartic acid (PALA); Plicamycin, semustine, teniposide, testosterone propionate, plug is for group, trimethylammonium melamine, uridine, vinorelbine; Ebormycine, gemcitabine, TX, BCNU, CCNU, DTIC, 5 FU 5 fluorouracil, Trastuzumab; A Wasiting, IMC-C225, Xarelto, imatinib mesylate, Iressa, tower Western method, rapamycin, dactinomycin ".

Can realize oral administration, for example, with solid form, like tablet, capsule, gel capsule, coated tablet, particle or powder, but also can be with the drinkable solutions form.For oral administration, the new compound of the present invention of definition can be combined with known, commonly used, physiologically acceptable carrier and vehicle above, gum arabic for example, talcum powder, starch; Sucrose, N.F,USP MANNITOL for example, methylcellulose gum, lactose, gelatin; Tensio-active agent, Magnesium Stearate, Schardinger dextrins, water-based or non-aqueous carrier, thinner; Dispersion agent, emulsifying agent, lubricant, sanitas and seasonings (for example essential oil).Compound of the present invention also can be dispersed in the particulate, nano particle for example, compsn.

Can realize non-oral administration, for example, through intravenously, subcutaneous or intramuscular injection sterile aqueous or oily solution, suspension-s or emulsion, by means of implant or by means of ointment, emulsion or suppository.If suitable, also could be with the sustained release form administration.Implant can comprise nonreactant, for example biodegradable polymkeric substance or synthetic silicone, for example Zylox.Can realize intravaginal administration, for example, by means of pesseulum.Can realize the intrauterine administration, for example, by means of barrier film or other suitable intrauterine device.Expection can transdermal administration in addition, especially by means of appropriate formulation and/or proper tools, for example plaster.

Medicine of the present invention can be applied to skin with suitable form of medication, uses with solution, suspension-s, emulsion, foam, ointment, paste or plaster epidermis; Oral and periglottis contain clothes ground, with tablet, lozenge, coated tablet, syrup or mouth wash shua to tongue ground or hypogloeeis use; Through stomach and intestines mucosa, to use in tablet, coated tablet, capsule, solution, suspension-s or the emulsion intestines; Through mucous membrane of rectum, with suppository, rectal capsule or ointment rectal administration; Through nasal mucosa, with drops, ointment or sprays nasal administration; Through segmental bronchus and alveolar epithelium, use through lung or through suction with aerosol or inhalation; Through conjunctiva, use through conjunctiva with eye drops, eye ointment, eye disk, lamella or eyewash; Through the reproductive organ mucous membrane,, use to the hysterophore intravaginal intrauterine and use with vaginal suppository, ointment and irrigating solution; Through urethra, to use in irrigating solution, ointment or the bougie urethra; Use the precession arteries and veins, use with the injection intra-arterial; Use into vein, with injection or infusion agent intravenous administration; Use into skin, with injection or implant intradermal administration; Subcutaneous, with injection or implant subcutaneous administration; Use into muscle, use with injection or implant intramuscular; Use into abdominal cavity, use with injection or infusion intraperitoneal.

About putting into practice the treatment demand,, can prolong the drug effect of compound of the present invention by means of suitable measure.Through chemistry and/or pharmacy approach, can realize this purpose.Realize that long lasting instance is to use implant and liposome, form sl. sol. salt and mixture, or use crystal suspension-s.

Explained that as top said new compound of the present invention also can be combined with other pharmacy activity component.Under the background of combination therapy, can be simultaneously or the single active ingredient of separate administration, no matter be the still approach through separating (for example oral and as injection) through identical approach (for example oral).They can exist in unitary dose or use with identical amount or different amounts.When suitable, also can use some dosage regimen.In this way, also can the many new compounds of the present invention of combination with one another.

Dosage can change in wide scope, and this depends on the seriousness, administration type of indication type, illness and experimenter's to be treated age, sex, body weight and susceptibility.Confirming " the pharmacologically active amount " of the pharmaceutical composition of combination, is in those skilled in the art's limit of power.Administration can realize in single dosage or a plurality of dosage that separates.

Suitable unitary dose is, for example, every kg weight in patients, the 0.001mg-100mg activeconstituents is at least a compound of the present invention and other optional active pharmaceutical ingredient.

In another aspect of the present invention, the present invention correspondingly also comprises pharmaceutical composition, and it comprises the compound at least a of the present invention of pharmacologically active amount, preferred compound 1,2,3,4,5,6,7,8,9,10,11,12,13,14,15; 16,17,18,19,20,21,22,23,24,25,26,27,28,29,30,31,32,33; 34,35,36,37,38,39,40,41,42,43,44,45,46,47,48,49,50; 51,52,53,54,55,56,57,58,59,60,61,62,63,64,65,66,67; 68,69,70,71,72,73,74,75,76,77,78,79,80,81,82,83,84 and/or the carrier and/or the vehicle of compound 85 and randomly pharmacy tolerance.

Preferred and preferred especially compsn of the present invention is to comprise at least a aforesaid preferred compound compositions of the present invention.In pharmaceutical composition according to the present invention, not only there is the compound of the present invention of at least a top definition, and has at least a other medicines activeconstituents that has detailed in the above.

In pharmaceutical composition of the present invention, the new compound of the present invention of at least a top definition exists with the pharmacologically active amount, preferably exists with unitary dose, and for example aforementioned unitary dose preferably exists with the form of medication that can realize oral administration.

About the pharmaceutical composition that comprises compound of the present invention with about the application of compound of the present invention as medicine, can be with reference to the statement that has provided about the application of new compound of the present invention itself, about possible purposes and administering mode.

In another aspect of the present invention; Through test kit is provided; Realized the object of the invention astoundingly, said test kit comprises at least a above-mentioned preferred compound of the present invention of pharmacologically active amount and at least a top other pharmacological component that defines of pharmacologically active amount.

The general compound method of compound of the present invention

Explained later the method for preparation substituted pyrido of the present invention [2,3-b] pyrazine.

Compound of the present invention can obtain according to following proposal (scheme 1-9) and corresponding method well known by persons skilled in the art:

The definition of the R1-R36 group that in following proposal, shows combines general formula (I) and the substituting group that (II) defines above corresponding, Z group for example, and the R group, the X group, the T group, etc.Those skilled in the art can accomplish single appointment with simple mode on the basis of the ordinary skill knowledge that it has.

Scheme 1

The precursor of the selected instance of pyrido of the present invention [2,3-b] pyrazine, wherein substituent R 2 will be replaced by hydrogen with R4, for example, can obtain through the method or the corresponding method well known by persons skilled in the art of scheme 2.

Scheme 2

The precursor of the selected instance of pyrido of the present invention [2,3-b] pyrazine, wherein substituent R 3 and/or R4 will be OR31, SR32, the NR33R34 group for example, can obtain through the method or the corresponding method well known by persons skilled in the art of scheme 3.

Scheme 3

About the precursor 11 of top demonstration, can use from the midbody 22 of scheme 6 or from the midbody 20,21 of scheme 5,21a and 21b.

The precursor of the selected instance of pyrido of the present invention [2,3-b] pyrazine, wherein substituent R 9 is not H, for example, can obtain through the method or the corresponding method well known by persons skilled in the art of scheme 4.

Scheme 4

Can the precursor 4,7,9 and 15 of scheme 1-4 be changed into substituted pyrido of the present invention [2,3-b] pyrazine, for example, through the method or the corresponding method well known by persons skilled in the art of scheme 5.

Scheme 5

Fs

Scheme 5

Fs

The selected instance of pyrido of the present invention [2,3-b] pyrazine, wherein substituent R 3 and/or R4 can be selected from substituted aryl; Heteroaryl, alkyl, alkenyl or alkynyl; For example, can obtain through the method or the corresponding method well known by persons skilled in the art of scheme 6.

Scheme 6

Fs

The selected instance of pyrido of the present invention [2,3-b] pyrazine, wherein substituent R 3 and/or R4 be-N-C (O)-,-N-SO ₂-,-N-C (O)-O-and-N-C (O)-N-for example, can obtain through the method or the corresponding method well known by persons skilled in the art of scheme 7.

Scheme 7

Fs

Pyrido [2 of the present invention; 3-b] the selected instance of pyrazine, wherein substituent R 3 and/or R4 can be selected from urea-, carbamate-or carbonic ether-substituted group; For example, can obtain through the method or the corresponding method well known by persons skilled in the art of scheme 8.

8 fs of scheme

The selected instance of pyrido of the present invention [2,3-b] pyrazine, wherein substituent R 3 and/or R4 can be selected from O-, S-, the substituted group of N-for example, can obtain through the method or the corresponding method well known by persons skilled in the art of scheme 9.

Scheme 9

Fs

Initial compounds and midbody can commercially obtain, and maybe can prepare through own known or method known to those skilled in the art.Reactant 4,7,9-15,22,26,31,34 and 37 is valuable midbodys of preparation pyrido-pyrazine of the present invention.

About the preparation of initial compounds, midbody and pyrido-pyrazine of the present invention, with reference to especially patent WO 2004/104002 and WO 2004/104003 draw, for example, following main literature, their content are introduced in the application's the disclosure hereby:

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The general method for preparing compound of the present invention:

1: the 1 stage of scheme

With 2,6-diamino--3-nitropyridine or 2-are amino-3, and the 5-di nitryl pyridine is dissolved in suitable inert solvent, methyl alcohol for example, ethanol, N Huo diox.After adding catalyzer (for example Raney nickel, palladium carbon or platinum dioxide (IV)), reaction mixture is placed under the nitrogen atmosphere, set up the pressure of 1-5bar.Make reaction mixture stoichiometric number hour, for example 1-16 hour, TR was 20 ℃ to 60 ℃.After finishing reaction, leach insoluble resistates, the filtration medium of use can be made up of silica gel, zeyssatite or business-like glass fibre filter, with suitable solvent wash.The crude product that in solution, exists is used for next step reaction without being further purified.

The 2nd stage

At first with 1, the inert solvent that it is suitable that the 2-derovatives is packed into, methyl alcohol for example, ethanol ， diox, toluene or N.2,3,6-triamino pyridine or 2,3,5-triamino pyridine directly after reduction, as the solution of crude product in one of above-mentioned solvent, add 1 of initial filling, in the 2-diketone, randomly add acid like acetate or alkali such as Pottasium Hydroxide.Make reaction mixture react certain hour, for example 20 minutes to 40 hours 20 ℃-80 ℃ TR.Reaction leaches any precipitated solid after finishing, and the filtration medium of use can be made up of for example business-like filter paper, and with the The suitable solvent washing, remaining solid drying under reduced pressure, or make said reaction mixture under reduced pressure remove solvent.When using N, reaction mixture is stirred in the into big water gaging, leach precipitated solid, or, under reduced pressure concentrate organic phase with appropriate organic solvent (like methylene dichloride or ETHYLE ACETATE) aqueous phase extracted.Through from suitable solvent such as diox recrystallization, or through column chromatography or flash chromatography on silica gel or the aluminum oxide, the remaining crude product of purifying.The elutriant that uses is, for example, and the mixture of methyl alcohol and methylene dichloride.

2: the 1 stages of scheme

Initial with inert solvent such as N ， diox or the toluene that it is suitable that pyrido-pyrazine ketone derivatives 8 is packed into, or do not have solvent.Add chlorizating agent in room temperature, for example phosphoryl chloride or THIONYL CHLORIDE 97 make reaction mixture react certain hour, for example 1 hour to 24 hours 20 ℃-100 ℃ TR.After reaction finishes, reaction mixture is poured into waterborne, neutralizes with suitable alkali aqueous solution such as sodium hydroxide solution.Leach any precipitated solid; The filtration medium that uses can be made up of for example business-like filter paper, and with The suitable solvent washing, remaining resistates drying under reduced pressure; Or, under reduced pressure concentrate organic phase with appropriate organic solvent (like methylene dichloride or ETHYLE ACETATE) aqueous phase extracted.Through from suitable solvent such as diox or toluene recrystallization, or through column chromatography or flash chromatography on silica gel or the aluminum oxide, the remaining crude product of purifying.The elutriant that uses is, for example, and the mixture of methyl alcohol and methylene dichloride.

3: the 1 stages of scheme

2,3,6-triamino pyridine or 2,3,5-triamino pyridine are directly after reduction, as the solution of crude product, in one of the above-mentioned solvent of packing at first.After having added oxalic acid verivate such as oxalic acid diethyl ester or oxalyl chloride, randomly add sour example hydrochloric acid, sulfuric acid or glacial acetic acid, 20 ℃-150 ℃ TR reaction certain hour, for example 10 minutes to 24 hours to reaction mixture.Reaction leaches any precipitated solid after finishing, and the filtration medium of use can be made up of for example business-like filter paper, and with the The suitable solvent washing, remaining solid drying under reduced pressure, or make said reaction mixture under reduced pressure remove solvent.Perhaps, reaction mixture is stirred in the into big water gaging, leaches precipitated solid, or with appropriate organic solvent (like methylene dichloride or ETHYLE ACETATE) extraction with suitable alkali aqueous solution for example in the sodium hydroxide solution with the water of crossing, and under reduced pressure concentrated organic phase.Through from suitable solvent such as diox or toluene recrystallization, or through column chromatography or flash chromatography on silica gel or the aluminum oxide, the remaining crude product of purifying.The elutriant that uses is, for example, and the mixture of methyl alcohol and methylene dichloride.

The 2nd stage

Initial with inert solvent such as N ， diox or the toluene that it is suitable that derovatives 10 is packed into, or do not have solvent.Add chlorizating agent in room temperature, for example phosphoryl chloride or THIONYL CHLORIDE 97 make reaction mixture react certain hour, for example 1 hour to 24 hours 20 ℃-100 ℃ TR.After reaction finishes, reaction mixture is poured into waterborne, neutralizes with suitable alkali aqueous solution such as sodium hydroxide solution.Leach any precipitated solid; The filtration medium that uses can be made up of for example business-like filter paper, and with The suitable solvent washing, remaining resistates drying under reduced pressure; Or, under reduced pressure concentrate organic phase with appropriate organic solvent (like methylene dichloride or ETHYLE ACETATE) aqueous phase extracted.Through from suitable solvent such as diox or toluene recrystallization, or through column chromatography or flash chromatography on silica gel or the aluminum oxide, the remaining crude product of purifying.The elutriant that uses is, for example, and the mixture of methyl alcohol and methylene dichloride.

The 3rd stage

In methyl alcohol, suitable inert solvent (like N, DMSO 99.8MIN.; Methyl alcohol, toluene) in, or alkali as solvent such as pyridine or triethylamine in; Or do not have solvent, make midbody 11 and suitable alcohol, mercaptan or amine and randomly suitable alkali (preferred sodium hydride, pyridine; Triethylamine, the sodium methylate in salt of wormwood or the methyl alcohol) reaction.Make reaction mixture reaction certain hour, for example 30 minutes to 2 days, TR was 20 ℃ to 140 ℃.Perhaps; In suitable solvent such as toluene or N, make midbody 11 and suitable amine and for example three (dibenzalacetones), two palladiums (0) or tetrakis triphenylphosphine palladium (0) and suitable for example 2-(dicyclohexyl phosphanyl) biphenyl and suitable for example sodium tert-butoxide reaction of alkali of part of appropriate catalyst.Make reaction mixture reaction certain hour, for example 2 hours to 30 hours, TR was 60 ℃ to 120 ℃.Reaction leaches any precipitated solid after finishing, and the filtration medium of use can be made up of for example business-like filter paper, and with the The suitable solvent washing, remaining solid drying under reduced pressure, or make reaction mixture under reduced pressure remove solvent.Perhaps, reaction mixture is stirred in the into big water gaging, leach precipitated solid, or, under reduced pressure concentrate organic phase with the water that appropriate organic solvent (like methylene dichloride or ETHYLE ACETATE) extraction neutralized with suitable aqueous acid (example hydrochloric acid).Through from suitable solvent such as diox, ETHYLE ACETATE or toluene recrystallization, or through column chromatography or flash chromatography on silica gel or the aluminum oxide, the remaining crude product of purifying.The elutriant that uses is, for example, and the mixture of methyl alcohol and methylene dichloride.

4: the 1 stages of scheme

In methyl alcohol, suitable inert solvent (like N, DMSO 99.8MIN.; Methyl alcohol) in, or alkali as solvent such as pyridine or triethylamine in, or do not have solvent; Make midbody 4 and 7 and suitable, suitable muriate, bromide or tosylate and randomly suitable alkali (sodium hydride for example; Pyridine, triethylamine, the sodium methylate in salt of wormwood or the methyl alcohol) reaction.Make reaction mixture reaction certain hour, for example 1 hour to 24 hours, TR was 20 ℃ to 150 ℃.Perhaps, in suitable solvent such as toluene Huo diox, make midbody 4 and 7 and suitable aromatic bromide or iodide and appropriate catalyst for example acid chloride or Pd ₂(dba) ₃, and for example BINAP and suitable for example salt of wormwood or sodium tert-butoxide reaction of alkali of suitable part.Make reaction mixture reaction specified time, for example 10 hours to 30 hours, TR was 60 ℃ to 120 ℃.Reaction leaches any precipitated solid after finishing, and the filtration medium of use can be made up of for example business-like filter paper; And wash with The suitable solvent; Remaining solid drying under reduced pressure, or leach any relict catalyst, and wash with The suitable solvent; The drying under reduced pressure solvent, or make reaction mixture under reduced pressure remove solvent.Perhaps, reaction mixture is stirred in the into big water gaging, leach precipitated solid, or, under reduced pressure concentrate organic phase with the water that appropriate organic solvent (like methylene dichloride or ETHYLE ACETATE) extraction neutralized with suitable aqueous acid (example hydrochloric acid).Through from suitable solvent such as ethanol or toluene recrystallization, or through column chromatography or flash chromatography on silica gel or the aluminum oxide, the remaining crude product of purifying.The elutriant that uses is, for example, and the mixture of methyl alcohol and methylene dichloride.

5: the 1 stages of scheme

After the alkaline purification, in method known to those skilled in the art, the product that can in conversion reaction, alkaline purification be formed changes into converted product of the present invention.

For example, when product will be the verivate according to the compound 16 of scheme 5, suitable inert solvent (like N, DMSO 99.8MIN.; Acetonitrile, methylene dichloride, 1; 2-ethylene dichloride Huo diox) in, or alkali as solvent such as pyridine or triethylamine in, or do not have solvent; Make reaction product 4,7,9 or 15 and suitable isocyanic ester and randomly suitable alkali (preferred sodium hydride; Hexamethyldisilazane potassium (potassium hexamethyldisilazide), pyridine, triethylamine or salt of wormwood) reaction.Make reaction mixture stoichiometric number hour, for example 1-24 hour, TR was 0-80 ℃.Reaction leaches any precipitated solid after finishing, and the filtration medium of use can be made up of for example business-like filter paper, and with the The suitable solvent washing, remaining solid drying under reduced pressure, or make reaction mixture under reduced pressure remove solvent.Perhaps, reaction mixture is stirred in the into big water gaging, leach precipitated solid, or, under reduced pressure concentrate organic phase with the water that appropriate organic solvent (like methylene dichloride or ETHYLE ACETATE) extraction neutralized with suitable aqueous acid (example hydrochloric acid).Through from suitable solvent such as ethanol or re-crystallizing in ethyl acetate, or through column chromatography or flash chromatography on silica gel or the aluminum oxide, the remaining crude product of purifying.The elutriant that uses is, for example, and the mixture of methyl alcohol and methylene dichloride.

Perhaps, when product will be the verivate according to the compound 17 of scheme 5, at suitable inert solvent (like N; THF, toluene, methylene dichloride or acetonitrile) in; Make reaction product 4,7,9 or 15 and phosgene or carbonyl dimidazoles and suitable amine reaction.If suitable, use suitable alkali, preferred pyridine, sodium hydrogencarbonate, triethylamine, N-methylmorpholine or sodium acetate.Make reaction mixture reaction certain hour, for example 15 minutes to 24 hours, TR was 0 to 60 ℃.Perhaps, at suitable inert solvent (like THF ， diox; Methylene dichloride, N or acetonitrile) in, or alkali as solvent such as pyridine or triethylamine in; Or do not have solvent, make reaction product 4,7; 9 or 15 and suitable amine-phenyl-carbamate reagent react with randomly suitable alkali (preferred pyridine, yellow soda ash, triethylamine or sodium hydride).Make reaction mixture reaction certain hour, for example 1 hour to 18 hours, TR was 0 ℃ to 120 ℃.Reaction leaches any precipitated solid after finishing, and the filtration medium of use can be made up of for example business-like filter paper, and with the The suitable solvent washing, remaining solid drying under reduced pressure, or make reaction mixture under reduced pressure remove solvent.Perhaps, reaction mixture is stirred in the into big water gaging, leach precipitated solid, or, under reduced pressure concentrate organic phase with the water that appropriate organic solvent (like methylene dichloride or ETHYLE ACETATE) extraction neutralized with suitable aqueous acid (example hydrochloric acid).Through from suitable solvent such as ethanol or re-crystallizing in ethyl acetate, or through column chromatography or flash chromatography on silica gel or the aluminum oxide, the remaining crude product of purifying.The elutriant that uses is, for example, and the mixture of methyl alcohol and methylene dichloride.

For example, when product will be the verivate according to the compound 18 of scheme 5, at suitable inert solvent (like N; THF, acetone or toluene) in, or in alkali solvent such as pyridine or triethylamine; Or do not have solvent, make reaction product 4,7; 9 or 15 and suitable lsothiocyanates react with suitably suitable alkali (preferred sodium hydride, triethylamine, salt of wormwood or pyridine).Make reaction mixture reaction certain hour, for example 30 minutes to 90 hours, TR was 0 to 115 ℃.Reaction leaches any precipitated solid after finishing, and the filtration medium of use can be made up of for example business-like filter paper, and with the The suitable solvent washing, remaining solid drying under reduced pressure, or make reaction mixture under reduced pressure remove solvent.Perhaps, reaction mixture is stirred in the into big water gaging, leach precipitated solid, or, under reduced pressure concentrate organic phase with the water that appropriate organic solvent (like methylene dichloride or ETHYLE ACETATE) extraction neutralized with suitable aqueous acid (example hydrochloric acid).Through from suitable solvent such as ethanol or re-crystallizing in ethyl acetate, or through column chromatography or flash chromatography on silica gel or the aluminum oxide, the remaining crude product of purifying.The elutriant that uses is, for example, and the mixture of methyl alcohol and methylene dichloride.

Perhaps, when product will be the verivate according to the compound 19 of scheme 5, suitable inert solvent (like N, THF; Toluene, methylene dichloride, ethanol or acetonitrile) in; Make reaction product 4,7,9 or 15 and thio phosgene or thiocarbonyl base diimidazole and suitable amine reaction.Randomly, use suitable alkali, preferred pyridine, sodium hydrogencarbonate, salt of wormwood, triethylamine or imidazoles.Make reaction mixture stoichiometric number hour, for example 1 to 24 hour, TR was-10 to 80 ℃.Reaction leaches any precipitated solid after finishing, and the filtration medium of use can be made up of for example business-like filter paper, and with the The suitable solvent washing, remaining solid drying under reduced pressure, or make reaction mixture under reduced pressure remove solvent.Perhaps, reaction mixture is stirred in the into big water gaging, leach precipitated solid, or, under reduced pressure concentrate organic phase with the water that appropriate organic solvent (like methylene dichloride or ETHYLE ACETATE) extraction neutralized with suitable aqueous acid (example hydrochloric acid).Through from suitable solvent such as ethanol or re-crystallizing in ethyl acetate, or through column chromatography or flash chromatography on silica gel or the aluminum oxide, the remaining crude product of purifying.The elutriant that uses is, for example, and the mixture of methyl alcohol and methylene dichloride.

For example, when product will be the verivate according to the compound 20 of scheme 5, at suitable inert solvent (like N; THF ， diox, methylene dichloride or toluene) in; Make reaction product 4,7,9 or 15 and phosgene or carbonyl dimidazoles and suitable azanol reaction.Randomly, use suitable alkali, preferred pyridine, yellow soda ash, triethylamine or sodium acetate.Make reaction mixture reaction certain hour, for example 1 hour to 24 hours, TR was 0 to 100 ℃.Perhaps, at suitable inert solvent (like THF ， diox; Methylene dichloride, N or toluene) in, or alkali as solvent such as pyridine or triethylamine in; Or do not have solvent, make reaction product 4,7; 9 or 15 and suitable azanol-phenyl-carbamate reagent react with suitably suitable alkali (preferred pyridine, yellow soda ash, triethylamine or sodium acetate).Make reaction mixture reaction certain hour, for example 1 hour to 18 hours, TR was a room temperature to 100 ℃.Reaction leaches any precipitated solid after finishing, and the filtration medium of use can be made up of for example business-like filter paper, and with the The suitable solvent washing, remaining solid drying under reduced pressure, or make reaction mixture under reduced pressure remove solvent.Perhaps, reaction mixture is stirred in the into big water gaging, leach precipitated solid, or, under reduced pressure concentrate organic phase with the water that appropriate organic solvent (like methylene dichloride or ETHYLE ACETATE) extraction neutralized with suitable aqueous acid (example hydrochloric acid).Through from suitable solvent such as ethanol or re-crystallizing in ethyl acetate, or through column chromatography or flash chromatography on silica gel or the aluminum oxide, the remaining crude product of purifying.The elutriant that uses is, for example, and the mixture of methyl alcohol and methylene dichloride.

For example, when product will be the verivate according to the compound 21 of scheme 5, at suitable inert solvent ianthone such as diox, chloroform, toluene or ethanol) in, make reaction product 4,7,9 or 15 and phosgene or carbonyl dimidazoles and suitable hydrazine reaction.Randomly, use suitable alkali, preferred pyridine, yellow soda ash, diisopropylethylamine or sodium acetate.Make reaction mixture reaction certain hour, for example 1 hour to 24 hours, TR was 0 to 100 ℃.Perhaps, at suitable inert solvent (like THF ， diox; Methylene dichloride, N or toluene) in, or in alkali solvent such as pyridine or triethylamine; Or do not have solvent, make reaction product 4,7; 9 or 15 and suitable hydrazine-phenyl-carbamate reagent react with randomly suitable alkali (preferred pyridine, yellow soda ash, triethylamine or sodium acetate).Make reaction mixture reaction certain hour, for example 1 hour to 15 hours, TR was 0 ℃ to 100 ℃.Reaction leaches any precipitated solid after finishing, and the filtration medium of use can be made up of for example business-like filter paper, and with the The suitable solvent washing, remaining solid drying under reduced pressure, or make reaction mixture under reduced pressure remove solvent.Perhaps, reaction mixture is stirred in the into big water gaging, leach precipitated solid, or, under reduced pressure concentrate organic phase with the water that appropriate organic solvent (like methylene dichloride or ETHYLE ACETATE) extraction neutralized with suitable aqueous acid (example hydrochloric acid).Through from suitable solvent such as ethanol or re-crystallizing in ethyl acetate, or through column chromatography or flash chromatography on silica gel or the aluminum oxide, the remaining crude product of purifying.The elutriant that uses is, for example, and the mixture of methyl alcohol and methylene dichloride.

Perhaps, when product will be the verivate according to the compound 21a of scheme 5, at suitable inert solvent (like THF; Toluene, methylene dichloride, ethanol) in; Or alkali as solvent such as pyridine or triethylamine in, make reaction product 4,7; 9 or 15 and oxalyl chloride and suitable alcohol, randomly with suitable alkali (preferred pyridine, sodium hydroxide, triethylamine) reaction.Make reaction mixture reaction certain hour, for example 15 minutes to 24 hours, TR was-10 to 60 ℃.Reaction leaches any precipitated solid after finishing, and the filtration medium of use can be made up of for example business-like filter paper, and with the The suitable solvent washing, remaining solid drying under reduced pressure, or make reaction mixture under reduced pressure remove solvent.Perhaps, reaction mixture is stirred in the into big water gaging, leach precipitated solid, or, under reduced pressure concentrate organic phase with the water that appropriate organic solvent (like methylene dichloride or ETHYLE ACETATE) extraction neutralized with suitable aqueous acid (example hydrochloric acid).Through from suitable solvent such as ethanol or re-crystallizing in ethyl acetate, or through column chromatography or flash chromatography on silica gel or the aluminum oxide, the remaining crude product of purifying.The elutriant that uses is, for example, and the mixture of methyl alcohol and methylene dichloride.

Perhaps, when product will be the verivate according to the compound 21b of scheme 5, at suitable inert solvent (like THF; Toluene, methylene dichloride, ethanol) in; Or alkali as solvent such as pyridine or triethylamine in, make reaction product 4,7; 9 or 15 and oxalyl chloride or ethyl oxalyl chloride and suitable amine, randomly suitable alkali (preferred pyridine, sodium hydroxide, triethylamine) reaction.Make reaction mixture reaction certain hour, for example 15 minutes to 24 hours, TR was-10 to 60 ℃.Perhaps, in suitable inert solvent (like THF, toluene, methylene dichloride, ethanol), or alkali as solvent such as pyridine or triethylamine in, make midbody 21a and suitable amine, randomly suitable alkali (preferred pyridine, sodium hydride or triethylamine) reaction.Make reaction mixture reaction certain hour, for example 1 hour to 50 hours, TR was 10 to 120 ℃.Reaction leaches any precipitated solid after finishing, and the filtration medium of use can be made up of for example business-like filter paper, and with the The suitable solvent washing, remaining solid drying under reduced pressure, or make reaction mixture under reduced pressure remove solvent.Perhaps, reaction mixture is stirred in the into big water gaging, leach precipitated solid, or, under reduced pressure concentrate organic phase with the water that appropriate organic solvent (like methylene dichloride or ETHYLE ACETATE) extraction neutralized with suitable aqueous acid (example hydrochloric acid).Through from suitable solvent such as ethanol or re-crystallizing in ethyl acetate, or through column chromatography or flash chromatography on silica gel or the aluminum oxide, the remaining crude product of purifying.The elutriant that uses is, for example, and the mixture of methyl alcohol and methylene dichloride.

6: the 1 stages of scheme

For example; When product will be the verivate according to the compound 23 of scheme 6, suitable solvent (like N, N/water; Toluene; Acetonitrile, glycol dimethyl ether Huo diox) in, makes reaction product 22 and suitable aryl/hetaryl boric acid derivatives or aryl/hetaryl organo-tin compound and appropriate catalyst (Pd (PPh for example ₃) ₄, [1,1 '-two (diphenylphosphine) ferrocene] dichloro palladium (II) or Pd ₂(dba) ₃) and suitable alkali (for example yellow soda ash, cesium carbonate or triethylamine) reaction.Make reaction mixture reaction certain hour, for example TR was 60 ℃ to 120 ℃ to a couple of days in 6 hours.Reaction leaches any precipitated solid after finishing, and the filtration medium of use can be made up of for example business-like filter paper; And wash with The suitable solvent; Remaining solid drying under reduced pressure, or leach any relict catalyst of existence, and wash with The suitable solvent; Under reduced pressure remove solvent, or make reaction mixture under reduced pressure remove solvent.Perhaps, reaction mixture is stirred in the into big water gaging, leach precipitated solid, or, under reduced pressure concentrate organic phase with the water that appropriate organic solvent (like methylene dichloride or ETHYLE ACETATE) extraction neutralized with suitable aqueous acid (example hydrochloric acid).Through from suitable solvent such as ethanol or re-crystallizing in ethyl acetate, or through column chromatography or flash chromatography on silica gel or the aluminum oxide, the remaining crude product of purifying.The elutriant that uses is, for example, and the mixture of methyl alcohol and methylene dichloride.

For example, when product will be the verivate according to the compound 23a of scheme 6, at suitable solvent (like N; THF; Toluene, glycol dimethyl ether Huo diox) in, makes reaction product 22 and suitable alkyl zinc halide and appropriate catalyst (Pd (PPh for example ₃) ₄, [1,1 '-two (diphenylphosphine) ferrocene] dichloro palladium (II) or PdCl ₂(PPh ₃) ₂) reaction.Make reaction mixture reaction certain hour, for example 30 minutes to 48 hours, TR was a room temperature to 120 ℃.Reaction leaches any precipitated solid after finishing, and the filtration medium of use can be made up of for example business-like filter paper; And wash with The suitable solvent; Remaining solid drying under reduced pressure, or leach any relict catalyst of existence, and wash with The suitable solvent; Under reduced pressure remove solvent, or make reaction mixture under reduced pressure remove solvent.Perhaps, reaction mixture is stirred in the into big water gaging, leach precipitated solid, or, under reduced pressure concentrate organic phase with appropriate organic solvent (like methylene dichloride or ETHYLE ACETATE) aqueous phase extracted.Through from suitable solvent such as ethanol or re-crystallizing in ethyl acetate, or through column chromatography or flash chromatography on silica gel or the aluminum oxide, the remaining crude product of purifying.The elutriant that uses is, for example, and the mixture of methyl alcohol and methylene dichloride.

For example; When product will be the verivate according to the compound 24 of scheme 6, suitable solvent (like toluene, N; N/water; Acetonitrile, glycol dimethyl ether or N,N-DIMETHYLACETAMIDE) in, make reaction product 22 and vinyl boric acid derivatives, vinyl organo-tin compound or alkene derivatives and appropriate catalyst (Pd (PPh for example ₃) ₄, [1,1 '-two (diphenylphosphine) ferrocene] dichloro palladium (II) or Pd (OAc) ₂) and suitable part (for example triphenylphosphine or tri-o-tolyl phosphine) and suitable alkali (for example salt of wormwood, yellow soda ash, triethylamine or sodium acetate) reaction.Make reaction mixture reaction certain hour, for example 3 hours to 24 hours, TR was 60 ℃ to 140 ℃.Reaction leaches any precipitated solid after finishing, and the filtration medium of use can be made up of for example business-like filter paper; And wash with The suitable solvent; Remaining solid drying under reduced pressure, or leach any relict catalyst of existence, and wash with The suitable solvent; Under reduced pressure remove solvent, or make reaction mixture under reduced pressure remove solvent.Perhaps, reaction mixture is stirred in the into big water gaging, leach precipitated solid, or, under reduced pressure concentrate organic phase with the water that appropriate organic solvent (like methylene dichloride or ETHYLE ACETATE) extraction neutralized with suitable aqueous acid (example hydrochloric acid).Through from suitable solvent (like ethanol or toluene) recrystallization, or through column chromatography or flash chromatography on silica gel or the aluminum oxide, the remaining crude product of purifying.The elutriant that uses is, for example, and the mixture of methyl alcohol and methylene dichloride.

For example, when product will be the verivate according to the compound 25 of scheme 6, at suitable solvent (like N; THF; THF/water, toluene or N,N-DIMETHYLACETAMIDE) in, make reaction product 22 and suitable alkynes verivate and appropriate catalyst (Pd (PPh for example ₃) ₄, PdCl ₂(PPh ₃) ₂Or Pd ₂(dba) ₃) and suitable additive (for example cupric iodide (I)) and suitable alkali (for example salt of wormwood, triethylamine or potassium acetate) reaction.Make reaction mixture reaction certain hour, for example 1 hour to a couple of days, and TR is a room temperature to 120 ℃.Reaction leaches any precipitated solid after finishing, and the filtration medium of use can be made up of for example business-like filter paper; And wash with The suitable solvent; Remaining solid drying under reduced pressure, or leach any relict catalyst of existence, and wash with The suitable solvent; Under reduced pressure remove solvent, or make reaction mixture under reduced pressure remove solvent.Perhaps, reaction mixture is stirred in the into big water gaging, leach precipitated solid, or, under reduced pressure concentrate organic phase with the water that appropriate organic solvent (like methylene dichloride or ETHYLE ACETATE) extraction neutralized with suitable aqueous acid (example hydrochloric acid).Through from suitable solvent (like ethanol or toluene) recrystallization, or through column chromatography or flash chromatography on silica gel or the aluminum oxide, the remaining crude product of purifying.The elutriant that uses is, for example, and the mixture of methyl alcohol and methylene dichloride.

7: the 1 stages of scheme

In methyl alcohol, suitable inert solvent (like N, DMSO 99.8MIN.; Methyl alcohol, toluene) in, or alkali as solvent such as pyridine or triethylamine in; Or do not have solvent, make midbody 22 and suitable amine and randomly suitable alkali (preferred sodium hydride, pyridine; Triethylamine, the sodium methylate in salt of wormwood or the methyl alcohol) reaction.Make reaction mixture reaction certain hour, for example TR was 20 ℃ to 140 ℃ to a couple of days in 1 hour.Perhaps, in suitable solvent such as toluene Huo diox, make midbody 22 and suitable amine and appropriate catalyst (for example acid chloride or Pd ₂(dba) ₃) and suitable part (for example BINAP) and suitable alkali (for example salt of wormwood or sodium tert-butoxide) reaction.Make reaction mixture reaction certain hour, for example 10 hours to 30 hours, TR was 60 ℃ to 120 ℃.Reaction leaches any precipitated solid after finishing, and the filtration medium of use can be made up of for example business-like filter paper; And wash with The suitable solvent; Remaining solid drying under reduced pressure, or leach any relict catalyst of existence, and wash with The suitable solvent; Under reduced pressure remove solvent, or make reaction mixture under reduced pressure remove solvent.Perhaps, reaction mixture is stirred in the into big water gaging, leach precipitated solid, or, under reduced pressure concentrate organic phase with the water that appropriate organic solvent (like methylene dichloride or ETHYLE ACETATE) extraction neutralized with suitable aqueous acid (example hydrochloric acid).Through from suitable solvent! like diox, ETHYLE ACETATE or toluene) recrystallization, or through column chromatography or flash chromatography on silica gel or the aluminum oxide, the remaining crude product of purifying.The elutriant that uses is, for example, and the mixture of methyl alcohol and methylene dichloride.

The 2nd stage

For example, when product will be the verivate according to the compound 27 of scheme 7, suitable inert solvent (like THF, toluene; Acetonitrile, methylene dichloride, acetone Huo diox) in; Or alkali as solvent such as pyridine or triethylamine in, or do not have solvent, make reaction product 26 and randomly suitable alkali (preferred sodium hydride; Pottasium Hydroxide, pyridine, triethylamine or salt of wormwood) and randomly catalyzer (for example Dimethylamino pyridine) reaction.Make reaction mixture reaction certain hour, for example 30 minutes to 24 hours, TR was 0 to 110 ℃.Reaction leaches any precipitated solid after finishing, and the filtration medium of use can be made up of for example business-like filter paper, and with the The suitable solvent washing, remaining solid drying under reduced pressure, or make reaction mixture under reduced pressure remove solvent.Perhaps, reaction mixture is stirred in the into big water gaging, leach precipitated solid, or, under reduced pressure concentrate organic phase with the water that appropriate organic solvent (like methylene dichloride or ETHYLE ACETATE) extraction neutralized with suitable aqueous acid (example hydrochloric acid).Through from suitable solvent such as ethanol or re-crystallizing in ethyl acetate, or through column chromatography or flash chromatography on silica gel or the aluminum oxide, the remaining crude product of purifying.The elutriant that uses is, for example, and the mixture of methyl alcohol and methylene dichloride.

For example, when product will be the verivate according to the compound 28 of scheme 7, suitable inert solvent (like THF, toluene; Acetonitrile, methylene dichloride, acetone, N Huo diox) in; Or alkali as solvent such as pyridine or triethylamine in, or do not have solvent, make reaction product 26 and suitable SULPHURYL CHLORIDE and randomly suitable alkali (preferred sodium hydride; Pottasium Hydroxide, pyridine, triethylamine or salt of wormwood) and randomly catalyzer (for example Dimethylamino pyridine) reaction.Make reaction mixture reaction certain hour, for example 30 minutes to 16 hours, TR was 0 to 120 ℃.Reaction leaches any precipitated solid after finishing, and the filtration medium of use can be made up of for example business-like filter paper, and with the The suitable solvent washing, remaining solid drying under reduced pressure, or make reaction mixture under reduced pressure remove solvent.Perhaps, reaction mixture is stirred in the into big water gaging, leach precipitated solid, or, under reduced pressure concentrate organic phase with the water that appropriate organic solvent (like methylene dichloride or ETHYLE ACETATE) extraction neutralized with suitable aqueous acid (example hydrochloric acid).Through from suitable solvent such as ethanol or re-crystallizing in ethyl acetate, or through column chromatography or flash chromatography on silica gel or the aluminum oxide, the remaining crude product of purifying.The elutriant that uses is, for example, and the mixture of methyl alcohol and methylene dichloride.

For example, when product will be the verivate according to the compound 29 of scheme 7, at suitable inert solvent ianthone such as diox, THF; Methylene dichloride, acetone, N or ethylene dichloride) in; Or alkali as solvent such as pyridine or triethylamine in, or do not have solvent, make reaction product 26 and suitable chloro-formic ester and randomly suitable alkali (preferred sodium hydride; Sodium hydroxide, pyridine, triethylamine or salt of wormwood) and randomly catalyzer (for example Dimethylamino pyridine) reaction.Make reaction mixture reaction certain hour, for example 1 hour to 24 hours, TR was-10 ℃ to 100 ℃.Reaction leaches any precipitated solid after finishing, and the filtration medium of use can be made up of for example business-like filter paper, and with the The suitable solvent washing, remaining solid drying under reduced pressure, or make reaction mixture under reduced pressure remove solvent.Perhaps, reaction mixture is stirred in the into big water gaging, leach precipitated solid, or, under reduced pressure concentrate organic phase with the water that appropriate organic solvent (like methylene dichloride or ETHYLE ACETATE) extraction neutralized with suitable aqueous acid (example hydrochloric acid).Through from suitable solvent such as ethanol or re-crystallizing in ethyl acetate, or through column chromatography or flash chromatography on silica gel or the aluminum oxide, the remaining crude product of purifying.The elutriant that uses is, for example, and the mixture of methyl alcohol and methylene dichloride.

For example, when product will be the verivate according to the compound 30 of scheme 7, at suitable inert solvent ianthone such as diox; THF, N, toluene or acetonitrile) in; Or alkali as solvent such as pyridine or triethylamine in, or do not have solvent, make reaction product 26 and suitable isocyanic ester or urea chloride and randomly suitable alkali (preferred sodium hydride; Pyridine, triethylamine, piperidines or salt of wormwood) and randomly catalyzer (for example Dimethylamino pyridine) reaction.Make reaction mixture reaction certain hour, for example 2 hours to 40 hours, TR was a room temperature to 100 ℃.Reaction leaches any precipitated solid after finishing, and the filtration medium of use can be made up of for example business-like filter paper, and with the The suitable solvent washing, remaining solid drying under reduced pressure, or make reaction mixture under reduced pressure remove solvent.Perhaps, reaction mixture is stirred in the into big water gaging, leach precipitated solid, or, under reduced pressure concentrate organic phase with the water that appropriate organic solvent (like methylene dichloride or ETHYLE ACETATE) extraction neutralized with suitable aqueous acid (example hydrochloric acid).Through from suitable solvent such as ethanol or re-crystallizing in ethyl acetate, or through column chromatography or flash chromatography on silica gel or the aluminum oxide, the remaining crude product of purifying.The elutriant that uses is, for example, and the mixture of methyl alcohol and methylene dichloride.

8: the 1 stages of scheme

For example, when product will be the verivate according to the compound 32 of scheme 8 or 35, at suitable inert solvent ianthone such as diox, THF; Methylene dichloride, acetone, N or ethylene dichloride) in; Or alkali as solvent such as pyridine or triethylamine in, or do not have solvent, make reaction product 31 or 34 and suitable chloro-formic ester and randomly suitable alkali (preferred sodium hydride; Sodium hydroxide, pyridine, triethylamine or salt of wormwood) and randomly catalyzer (for example Dimethylamino pyridine) reaction.Make reaction mixture reaction specified time, for example 1 hour to 24 hours, TR was-10 ℃ to 100 ℃.Reaction leaches any precipitated solid after finishing, and the filtration medium of use can be made up of for example business-like filter paper, and with the The suitable solvent washing, remaining solid drying under reduced pressure, or make reaction mixture under reduced pressure remove solvent.Perhaps, reaction mixture is stirred in the into big water gaging, leach precipitated solid, or, under reduced pressure concentrate organic phase with the water that appropriate organic solvent (like methylene dichloride or ETHYLE ACETATE) extraction neutralized with suitable aqueous acid (example hydrochloric acid).Through from suitable solvent such as ethanol or re-crystallizing in ethyl acetate, or through column chromatography or flash chromatography on silica gel or the aluminum oxide, the remaining crude product of purifying.The elutriant that uses is, for example, and the mixture of methyl alcohol and methylene dichloride.

For example, when product will be the verivate according to the compound 33 of scheme 8 or 36, at suitable inert solvent ianthone such as diox; THF, N, toluene or acetonitrile) in; Or alkali as solvent such as pyridine or triethylamine in, or do not have solvent, make reaction product 31 or 34 and suitable isocyanic ester or urea chloride and randomly suitable alkali (preferred sodium hydride; Pyridine, triethylamine, piperidines or salt of wormwood) and randomly catalyzer (for example Dimethylamino pyridine) reaction.Make reaction mixture reaction specified time, for example 2 hours to 40 hours, TR was a room temperature to 100 ℃.Reaction leaches any precipitated solid after finishing, and the filtration medium of use can be made up of for example business-like filter paper, and with the The suitable solvent washing, remaining solid drying under reduced pressure, or make reaction mixture under reduced pressure remove solvent.Perhaps, reaction mixture is stirred in the into big water gaging, leach precipitated solid, or, under reduced pressure concentrate organic phase with the water that appropriate organic solvent (like methylene dichloride or ETHYLE ACETATE) extraction neutralized with suitable aqueous acid (example hydrochloric acid).Through from suitable solvent such as ethanol or re-crystallizing in ethyl acetate, or through column chromatography or flash chromatography on silica gel or the aluminum oxide, the remaining crude product of purifying.The elutriant that uses is, for example, and the mixture of methyl alcohol and methylene dichloride.

9: the 1 stages of scheme

For example, when product will be the verivate according to the compound 38 of scheme 9, in methyl alcohol, at suitable inert solvent (like N; DMSO 99.8MIN., methyl alcohol ， diox, THF; Toluene) in, or alkali as solvent such as pyridine or triethylamine in, or do not have solvent, make reaction product 37 and for example suitable muriate, bromide or iodide and randomly suitable alkali (preferred sodium hydride; Pyridine, triethylamine, the sodium methylate in salt of wormwood or the methyl alcohol) reaction.Make reaction mixture reaction certain hour, for example 30 minutes to 2 days, TR was 0 ℃ to 140 ℃.Perhaps; In suitable solvent such as toluene or N, make amino-substituted midbody 37 and for example suitable muriate, bromide or iodide and appropriate catalyst (for example three (dibenzalacetones), two palladiums (0) or tetrakis triphenylphosphine palladium (0)) and suitable part (for example 2-(dicyclohexyl phosphanyl) biphenyl) and suitable alkali (for example sodium tert-butoxide) reaction.Make reaction mixture reaction certain hour, for example 2 hours to 30 hours, TR was 60 ℃ to 120 ℃.Reaction leaches any precipitated solid after finishing, and the filtration medium of use can be made up of for example business-like filter paper, and with the The suitable solvent washing, remaining solid drying under reduced pressure, or make reaction mixture under reduced pressure remove solvent.Perhaps, reaction mixture is stirred in the into big water gaging, leach precipitated solid, or, under reduced pressure concentrate organic phase with the water that appropriate organic solvent (like methylene dichloride or ETHYLE ACETATE) extraction neutralized with suitable aqueous acid (example hydrochloric acid).Through from suitable solvent! like diox, ETHYLE ACETATE or toluene) recrystallization, or through column chromatography or flash chromatography on silica gel or the aluminum oxide, the remaining crude product of purifying.The elutriant that uses is, for example, and the mixture of methyl alcohol and methylene dichloride.

Under some specified reaction conditions, OH, SH and NH ₂Group possibly get into undesirable side reaction.Therefore, be preferably them the protection base is provided, or at NH ₂Situation under, it is replaced with NO ₂, eliminate protection base or reductive NO then ₂Group.For example, in the variant of aforesaid method, can replace at least one OH group of initial compounds, for example, replace with benzyloxy, and/or can replace at least one SH group, for example, replace with the S-benzyl, and/or can replace at least one NH ₂Group for example, replaces with NH-benzyl or NO ₂Group.Subsequently, can eliminate at least one (preferably all) benzyloxies or NH-benzyl, for example; With hydrogen and palladium carbon, and/or can eliminate at least one (preferably all) S-benzyl, for example; Be used in the sodium in the ammoniacal liquor, and/or can reduce at least one (preferably all) NO ₂Group for example, becomes NH with hydrogen with Raney nickel ₂

Under some reaction conditions of mentioning, OH, NH ₂Possibly get into undesirable side reaction with the COOH group.Therefore, preferably will contain at least one OH group and/or at least one NH ₂The initial compounds of group and/or at least one COOH group and midbody change into corresponding carboxylicesters and carboxamide derivative.In the variant of aforesaid method, through reacting with activatory hydroxy-acid group (for example carbonyl chloride group), can be with having at least one OH group and/or having at least one NH ₂The initial compounds of group and midbody change into carboxylicesters or carboxamide derivative.In the variant of aforesaid method,, with suitable alcohol or amine reaction, can initial compounds that contain at least one COOH and midbody be changed into carboxylicesters or carboxamide derivative subsequently through reacting with acvator (for example THIONYL CHLORIDE 97 or carbonyl dimidazoles).Subsequently, can break away from least one (preferably all) carboxylicesters or the carboxylacyl amine group in initial compounds and the midbody, for example, with diluted acid or alkali aqueous solution, so that discharge (preferably all) OH group and/or NH ₂Group and/or COOH group.

Compound of the present invention, especially compound 1-85 (ISISTM/Draw 2.5 with AutoNom 2000 softwares; MDL) name.

Will be with reference to following embodiment, illustrated in detail the present invention, but the invention is not restricted to these embodiment.

Embodiment

I) preparation of compound of the present invention

Use is synthesized following compound of the present invention based on the general compound method of synthetic schemes 1-9.In addition, the NMR spectral data and mass-spectrometric data and the fusing point that have comprised them.

Known by one of skill in the art method can be synthesized the precursor that is used to prepare compound of the present invention, except as otherwise noted.

The chemical reagent that uses and solvent commercial from conventional supplier obtain (Acros, Aldrich, Fluka, Lancaster, Maybridge, Merck, Sigma, TCI, etc.) or synthesize.

Embodiment 1:

1-ethyl-3-(3-phenylacetylene yl pyridines is [2,3-b] pyrazine-6-yl also) urea (compound 1)

The preparation (according to the reaction of scheme 5) of 1-(the 3-chloropyridine is [2,3-b] pyrazine-6-yl also)-3-ethyl carbamide

With 100mg 3-chloropyridine also [2,3-b] pyrazine-6-base amine (0.55mmol) put into the 5ml pyridine at first, add 44 μ l ethyl isocyanates (0.55mmol) in room temperature.Mixture is stirred 3h at 75 ℃,, divide small portion in reaction mixture, to add in addition totally 132 μ l ethyl isocyanates (1.65mmol) then through 18h.Under reduced pressure remove solvent then.By means of silica gel column chromatography (methylene chloride elutriant), the solid that purifying obtains.This produces the glassy yellow solid.

The preparation (according to the reaction of scheme 6) of 1-ethyl-3-(3-phenylacetylene yl pyridines is [2,3-b] pyrazine-6-yl also) urea

As under the shielding gas, with 98.1mg 1-(the 3-chloropyridine is [2,3-b] pyrazine-6-yl also)-3-ethyl carbamide (0.39mmol), 10.1mg cupric iodide (I) (0.05mmol) is put into the 2ml anhydrous dimethyl formamide with 193 μ l triethylamines (1.38mmol) at first at nitrogen.Subsequently, add two (triphenylphosphine) palladiums (II) of 29.1mg dichloro (0.04mmol) with 54 μ l phenylacetylenes (0.49mmol), at the said mixture 16h of stirring at room.For aftertreatment,, and add Hydrogen chloride with methylene dichloride diluted mixture thing.Suction leaches precipitated solid, with Hydrogen chloride and distilled water wash organic phase.After being separated, under reduced pressure remove organic solvent.Realize being further purified through silica gel column chromatography (methylene chloride elutriant).It produces yellow solid.

Fusing point: 236-238 ℃ (decomposition)

ESI-MS: measured value m/z=318.0 (M+H ⁺); Calculated value 317 atomic mass units

¹H?NMR(d ₆-DMSO)：δ＝1.20(t，3H)，3.35-3.45(m，2H)，7.51-7.59(m，3H)，7.68(d，1H)，7.75(d，2H)，8.37(d，1H)，9.01(s，1H)，9.14(s，1H)，10.23(s，1H)ppm。

According to embodiment 1 and general compound method, synthetic following embodiment:

Embodiment 2:

1-ethyl-3-(3-thiene-3-yl-ethynyl pyridine is [2,3-b] pyrazine-6-yl also) urea (compound 2)

Fusing point: 239-242 ℃ (decomposition)

ESI-MS: measured value m/z=324.2 (M+H ⁺); Calculated value 323 atomic mass units

¹H?NMR(d ₆-DMSO)：δ＝1.20(t，3H)，3.25-3.35(m，2H)，7.43(d，1H)，7.66(d，1H)，7.76(dd，1H)，8.21(d，1H)，8.36(d，1H)，8.97(s，1H)，9.14(s，1H)，10.23(s，1H)ppm。

Embodiment 3:

1-(3-cyclopropyl acethlene yl pyridines is [2,3-b] pyrazine-6-yl also)-3-ethyl carbamide (compound 3)

Fusing point: 227-228 ℃ (decomposition)

ESI-MS: measured value m/z=282.3 (M+H ⁺); Calculated value 281 atomic mass units

¹H?NMR(d ₆-DMSO)：δ＝1.00-1.10(m，2H)，1.19(t，3H)，1.69-1.79(m，1H)，3.25-3.35(m，2H)，7.63(d，1H)，8.32(d，1H)，8.77(s，1H)，9.11(s，1H)，10.18(s，1H)ppm。

Embodiment 4:

1-[3-(3-dimethylamino third-1-alkynyl) pyrido [2,3-b] pyrazine-6-yl]-3-ethyl carbamide (compound 4)

ESI-MS: measured value m/z=299.2 (M+H ⁺); Calculated value 298 atomic mass units

¹H?NMR(d ₆-DMSO)：δ＝1.19(t，3H)，2.33(s，6H)，3.27-3.35(m，2H)，3.67(s，2H)，7.67(d，1H)，8.34(d，1H)，8.85(s，1H)，9.05(s，1H)，10.19(s，1H)ppm。

Embodiment 5:

1-[3-((E)-2-cyclohexyl vinyl) pyrido [2,3-b] pyrazine-6-yl]-3-ethyl carbamide (compound 5)

The preparation (according to the reaction of scheme 6) of 1-[3-((E)-2-cyclohexyl vinyl) pyrido [2,3-b] pyrazine-6-yl]-3-ethyl carbamide

Under nitrogen; With 99.6mg 1-(3-chloropyridine also [2; 3-b] pyrazine-6-yl)-3-ethyl carbamide (0.40mmol); 73.6mg cyclohexyl vinyl boric acid (0.48mmol), 84.4mg yellow soda ash (0.80mmol) and 33.4mg [1,1 '-two (diphenylphosphine) ferrocene] dichloro palladium (II) (0.04mmol) are put into 6ml N/water (1: 1) at first.Then with mixture heating up to 90 ℃ lasting 6.5h.Then zero(ppm) water is added reaction mixture, suction leaches precipitated solid.Realize being further purified through silica gel column chromatography (ethyl acetate/heptane mixture of eluents).Obtain light brown solid.

Fusing point: 202-204 ℃ (decomposition)

ESI-MS: measured value m/z=326.0 (M+H ⁺); Calculated value 325 atomic mass units

¹H?NMR(d ₆-DMSO)：δ＝1.10-1.40(m，8H)，1.65-1.90(m，5H)，2.28-2.38(m，1H)，3.25-3.35(m，2H)，6.69(d，1H)，7.15(dd，1H)，7.58(d，1H)，8.28(d，1H)，8.98(s，1H)，9.15(s，1H)，10.05(s，1H)ppm。

According to embodiment 5 and general compound method, synthetic following embodiment:

Embodiment 6:

1-ethyl-3-[3-((E)-3-methoxy propyl thiazolinyl) pyrido [2,3-b] pyrazine-6-yl] urea (compound 6)

ESI-MS: measured value m/z=288.3 (M+H ⁺); Calculated value 287 atomic mass units

¹H?NMR(d ₆-DMSO)：δ＝1.20(t，3H)，3.25-3.35(m，2H)，3.39(s，3H)，4.25(d，2H)，6.92(d，1H)，7.15-7.25(m，1H)，7.62(d，1H)，8.30(d，1H)，9.02(s，1H)，9.15(s，1H)，10.10(s，1H)ppm。

Embodiment 7:

1-ethyl-3-{3-[(E)-and 2-(4-fluorophenyl) vinyl] pyrido [2,3-b] pyrazine-6-yl } urea (compound 27)

Fusing point: 217-219 ℃

ESI-MS: measured value m/z=338.2 (M+H ⁺); Calculated value 337 atomic mass units

¹H?NMR(d ₆-DMSO)：δ＝1.20(t，3H)，3.25-3.38(m，2H)，7.10(t，2H)，7.32(dd，2H)，7.54(d，1H)，7.61(d，1H)，7.87(t，2H)，8.02(d，1H)，8.31(d，1H)，9.09(s，1H)，9.17(bs，1H)，10.09(s，1H)ppm。

Embodiment 8

4-[6-(3-ethyl carbamide) pyrido [2,3-b] pyrazine-3-yl] phenyl methyl carbonic ether (compound 9)

The preparation (according to the reaction of scheme 5) of 1-ethyl-3-[3-(4-hydroxy phenyl) pyrido [2,3-b] pyrazine-6-yl] urea

0.50g 4-(the 6-EL-970 is [2,3-b] pyrazine-3-yl also) phenol (2.10mmol) is put in the 5.0ml pyridine at first.Dropwise add 183 μ l ethyl isocyanates (2.31mmol) in room temperature, with mixture heating up to 70-80 ℃ of lasting 2h.After this, add other 183 μ l ethyl isocyanates, mixture heating up is continued other 2h to 70-80 ℃.After reaction finishes, reactant mixture is added ice-water, with the neutralization of 1N hydrochloric acid.Suction leaches sedimentary product, and dry.Filtering product partly is dissolved in ethanol, and mixes with 52mg Pottasium Hydroxide (0.93mmol), and is water-soluble.With mixture heating up to 40 ℃ lasting about 1h.After this, with 1N hydrochloric acid neutralization reaction solution, under reduced pressure remove solvent.The solid that obtains through silica gel column chromatography (methylene chloride elutriant) purifying.It produces yellow solid.

The preparation (according to the reaction of scheme 8) of 4-[6-(3-ethyl carbamide) pyrido [2,3-b] pyrazine-3-yl] phenyl methyl carbonic ether

With 100mg 1-ethyl-3-[3-(4-hydroxy phenyl) pyrido [2; 3-b] pyrazine-6-yl] urea (0.32mmol); 30 μ l methyl-chloroformates (0.39mmol) and 45 μ l triethylamines (0.32mmol) are put in the no Shui diox of 10ml at first, are heated to 100 ℃ of lasting 1h.After the cooling, suction leaches precipitated solid, and dry.From ethyl alcohol recrystallization, obtain faint yellow solid.

Fusing point: 243-245 ℃

ESI-MS: measured value m/z=368.2 (M+H ⁺); Calculated value 367 atomic mass units

¹H?NMR(d ₆-DMSO)：δ＝1.20(t，3H)，3.30-3.39(m，2H)，3.90(s，3H)，7.49(d，2H)，7.70(d，1H)，8.38(d，1H)，8.42(d，2H)，9.03(s，1H)，9.47(s，1H)，10.09(s，1H)ppm。

According to embodiment 8 and general compound method, synthetic following embodiment:

Embodiment 9:

4-[6-(3-ethyl carbamide) pyrido [2,3-b] pyrazine-3-yl] phenyl (2-methoxy ethyl) carbonic ether (compound 10)

Fusing point: 230-232 ℃

ESI-MS: measured value m/z=412.2 (M+H ⁺); Calculated value 411 atomic mass units

¹H?NMR(d ₆-DMSO)：δ＝1.20(t，3H)，3.30-3.39(m，5H)，3.68(t，2H)，4.40(t，2H)，7.50(d，2H)，7.70(d，1H)，8.38(d，1H)，8.41(d，2H)，9.10(s，1H)，9.50(s，1H)，10.15(s，1H)ppm。

Embodiment 10:

4-[6-(3-ethyl carbamide) pyrido [2,3-b] pyrazine-3-yl] phenyl carbonic ether (compound 11)

ESI-MS: measured value m/z=430.2 (M+H ⁺); Calculated value 429 atomic mass units

¹H?NMR(d ₆-DMSO)：δ＝1.21(t，3H)，3.30-3.33(m，2H)，7.33-7.38(m，1H)，7.43(d，2H)，7.51(t，2H)，7.65(d，2H)，8.39(d，1H)，8.45(d，2H)，9.11(s，1H)，9.50(s，1H)，10.19(s，1H)ppm。

Embodiment 11:

4-[6-(3-ethyl carbamide) pyrido [2,3-b] pyrazine-3-yl] diethylamino phenyl aminocarbamic acid ester (compound 12)

ESI-MS: measured value m/z=409.4 (M+H ⁺); Calculated value 408 atomic mass units

¹H?NMR(d ₆-DMSO)：δ＝1.15(t，3H)，1.20(t，3H)，1.24(t，3H)，3.30-3.39(m，4H)，3.45(q，2H)，7.37(d，2H)，7.69(d，1H)，8.34-8.39(m，3H)，9.11(s，1H)，9.48(s，1H)，10.15(s，1H)ppm。

Embodiment 12:

3-[6-(3-ethyl carbamide) pyrido [2,3-b] pyrazine-3-yl] phenyl 2-methoxy ethyl carbonic ether (compound 16)

¹H?NMR(d ₆-DMSO)：δ＝1.20(t，3H)，3.33-3.38(m，5H)，3.63-3.66(m，2H)，4.37-4.39(m，2H)，7.48(d，2H)，7.68(t，1H)，7.72(d，1H)，8.22(s，1H)，8.29(d，1H)，8.39(d，1H)，9.06(s，1H)，9.48(s，1H)，10.14(s，1H)ppm。

Embodiment 13:

4-[6-(3-ethyl carbamide) pyrido [2,3-b] pyrazine-3-yl] phenyl isobutyl-carbonic ether (compound 17)

ESI-MS: measured value m/z=410.3 (M+H ⁺); Calculated value 409 atomic mass units

¹H?NMR(d ₆-DMSO)：δ＝0.97(d，6H)，1.20(t，3H)，2.02(sep，1H)，3.25-3.38(m，2H)，4.06(d，2H)，7.50(d，2H)，7.70(d，1H)，8.38(d，1H)，8.41(d，2H)，9.10(s，1H)，9.47(s，1H)，10.14(s，1H)ppm。

Embodiment 14:

Fourth-2-alkynyl 4-[6-(3-ethyl carbamide) pyrido [2,3-b] pyrazine-3-yl] benzol carbonate (compound 18)

ESI-MS: measured value m/z=406.1 (M+H ⁺); Calculated value 405 atomic mass units

¹H?NMR(d ₆-DMSO)：δ＝1.20(t，3H)，1.89(t，3H)，3.25-3.38(m，2H)，4.90(q，2H)，7.50(d，2H)，7.70(d，1H)，8.38(d，1H)，8.41(d，2H)，9.09(s，1H)，9.47(s，1H)，10.14(s，1H)ppm。

Embodiment 15:

4-[6-(3-ethyl carbamide) pyrido [2,3-b] pyrazine-3-yl] phenyl dimethylcarbamate (compound 19)

Use sodium hydride as alkali, use N, preparation embodiment 15 as solvent.

Fusing point:＞230 ℃ (decomposition)

ESI-MS: measured value m/z=381.2 (M+H ⁺); Calculated value 380 atomic mass units

¹H?NMR(d ₆-DMSO)：δ＝1.20(t，3H)，2.95(s，3H)，3.09(s，3H)，3.25-3.38(m，2H)，7.37(d，2H)，7.68(d，1H)，8.35-8.38(m，3H)，9.11(s，1H)，9.46(s，1H)，10.12(s，1H)ppm。

Embodiment 16:

4-[6-(3-ethyl carbamide) pyrido [2,3-b] pyrazine-3-yl]-2-p-methoxy-phenyl 2-methoxy ethyl carbonic ether (compound 32)

ESI-MS: measured value m/z=442.3 (M+H ⁺); Calculated value 441 atomic mass units

¹H?NMR(d ₆-DMSO)：δ＝1.20(t，3H)，3.25-3.38(m，5H)，3.62(dd，2H)，3.97(s，3H)，4.35(dd，2H)，7.45(d，1H)，7.74(d，1H)，7.97(d，1H)，8.06(s，1H)，8.39(d，1H)，8.99(bs，1H)，9.52(s，1H)，10.15(s，1H)ppm。

Embodiment 17:

2-benzyloxy ethyl 4-[6-(3-ethyl carbamide) pyrido [2,3-b] pyrazine-3-yl] benzol carbonate (compound 33)

ESI-MS: measured value m/z=488.2 (M+H ⁺); Calculated value 487 atomic mass units

¹H?NMR(d ₆-DMSO)：δ＝1.20(t，3H)，3.28-3.38(m，2H)，3.75(t，2H)，4.43(t，2H)，4.57(s，2H)，7.31(t，1H)，7.36-7.40(m，4H)，7.48(d，2H)，7.70(d，1H)，8.38(d，1H)，8.41(d，2H)，9.09(bs，1H)，9.47(s，1H)，10.13(s，1H)ppm。

Embodiment 18:

2-benzyloxy ethyl 4-[6-(3-ethyl carbamide) pyrido [2,3-b] pyrazine-3-yl]-2-p-methoxy-phenyl carbonic ether (compound 34)

Fusing point: 172-174 ℃

ESI-MS: measured value m/z=518.3 (M+H ⁺); Calculated value 517 atomic mass units

¹H?NMR(d ₆-DMSO)：δ＝1.20(t，3H)，3.28-3.38(m，2H)，3.74(dd，2H)，3.96(s，3H)，4.41(dd，2H)，4.56(s，2H)，7.31(t，1H)，7.35-7.40(m，3H)，7.44(d，2H)，7.74(d，1H)，7.97(d，1H)，8.06(s，1H)，8.39(d，1H)，8.99(bs，1H)，9.51(s，1H)，10.14(s，1H)ppm。

Embodiment 19:

4-[6-(3-ethyl carbamide) pyrido [2,3-b] pyrazine-3-yl]-2-p-methoxy-phenyl diethylamino manthanoate (compound 67)

Fusing point: 220-222 ℃

ESI-MS: measured value m/z=439.3 (M+H ⁺); Calculated value 438 atomic mass units

¹H?NMR(d ₆-DMSO)：δ＝1.13(t，3H)，1.20(t，3H)，1.24(t，3H)，3.28-3.36(m，4H)，3.44(q，2H)，3.94(s，3H)，7.31(d，1H)，7.73(d，1H)，7.94(d，1H)，8.01(s，1H)，8.37(d，1H)，8.97(bs，1H)，9.50(s，1H)，10.11(s，1H)ppm。

Embodiment 20:

2-chloro-4-[6-(3-ethyl carbamide) pyrido [2,3-b] pyrazine-3-yl]-6-p-methoxy-phenyl diethylamino manthanoate (compound 68)

Fusing point: 237-239 ℃

ESI-MS: measured value m/z=473.4 (M+H ⁺); Calculated value 472 atomic mass units

¹H?NMR(d ₆-DMSO)：δ＝1.14(t，3H)，1.19(t，3H)，1.27(t，3H)，3.25-3.38(m，4H)，3.46(q，2H)，3.97(s，3H)，7.76(d，1H)，8.00(s，1H)，8.09(s，1H)，8.39(d，1H)，8.94(bs，1H)，9.55(s，1H)，10.13(s，1H)ppm。

Embodiment 21:

4-[6-(3-ethyl carbamide) pyrido [2,3-b] pyrazine-3-yl]-2-p-methoxy-phenyl 2-[2-(2-methoxy ethoxy)-oxyethyl group] ethyl carbonate ester (compound 69)

Fusing point: 166-167 ℃

ESI-MS: measured value m/z=530.2 (M+H ⁺); Calculated value 529 atomic mass units

¹H?NMR(d ₆-DMSO)：δ＝1.20(t，3H)，3.25(s，3H)，3.28-3.35(m，2H)，3.45(t，2H)，3.53-3.60(m，6H)，3.71(t，2H)，3.98(s，3H)，4.35(t，2H)，7.45(d，1H)，7.74(d，1H)，7.96(d，1H)，8.06(s，1H)，8.39(d，1H)，8.96(bs，1H)，9.51(s，1H)，10.12(s，1H)ppm。

Embodiment 22:

4-[6-(3-ethyl carbamide) pyrido [2,3-b] pyrazine-3-yl] phenyl (E)-3-phenyl acrylate (compound 13)

The preparation of 4-[6-(3-ethyl carbamide) pyrido [2,3-b] pyrazine-3-yl] phenyl (E)-3-phenyl acrylate

38.9mg 1-ethyl-3-[3-(4-hydroxy phenyl) pyrido [2,3-b] pyrazine-6-yl] urea (0.13mmol) is put in the 3.0ml exsiccant pyridine at first.Room temperature add 17.5mg Dimethylamino pyridine (0.14mmol) and 22.9mg trans-cinnamyl chloride (0.13mmol), at the stirring at room reaction mixture.Behind the 3h, add other 22.9mg trans-cinnamyl chloride (0.13mmol), at the other 3h of stirring at room mixture.For aftertreatment, reaction mixture is added ice-water, neutralize with 1N hydrochloric acid.Suction leaches precipitated solid and drying under reduced pressure.Without being further purified, the product that obtains is a yellow solid.

Fusing point: 236-238 ℃

ESI-MS: measured value m/z=440.3 (M+H ⁺); Calculated value 439 atomic mass units

¹H?NMR(d ₆-DMSO)：δ＝1.20(t，3H)，3.25-3.40(m，2H)，6.95(d，1H)，7.46-7.51(m，5H)，7.70(d，1H)，7.83-7.87(m，2H)，7.94(d，1H)，8.38(d，1H)，8.43(d，2H)，9.12(s，1H)，9.49(s，1H)，10.19(s，1H)ppm。

Embodiment 23:

4-[6-(3-ethyl carbamide) pyrido [2,3-b] pyrazine-3-yl] phenyl nonadecane acid esters (compound 14)

The preparation of 4-[6-(3-ethyl carbamide) pyrido [2,3-b] pyrazine-3-yl] phenyl nonadecane acid esters

50.0mg 1-ethyl-3-[3-(4-hydroxy phenyl) pyrido [2,3-b] pyrazine-6-yl] urea (0.16mmol) is put in the 5.0ml exsiccant pyridine at first.Add 19.7mg Dimethylamino pyridine (0.16mmol) and 51.2mg nonadecane acyl chlorides (0.16mmol) in room temperature, at stirring at room reaction mixture 4h.For aftertreatment, reaction mixture is added about 200ml zero(ppm) water.Suction leaches precipitated solid, and uses water washing.Purified crude product on silica gel (methylene chloride elutriant) obtains white solid.

Fusing point: 147.2 ℃

¹H?NMR(d ₆-DMSO)：δ＝0.90(t，3H)，1.20-1.50(m，33H)，1.75-1.85(m，2H)，2.60-2.68(m，2H)，3.50-3.60(m，2H)，7.26-7.36(m，3H)，8.25-8.31(m，3H)，8.71(s，1H)，9.22(s，1H)，9.75(s，1H)ppm。

Embodiment 24:

1-(the 3-benzyl-pyridine is [2,3-b] pyrazine-6-yl also]-3-ethyl carbamide (compound 15)

1-(the 3-benzyl-pyridine is [2,3-b] pyrazine-6-yl also]-preparation (according to the reaction of scheme 6) of 3-ethyl carbamide

Under nitrogen, solution and the 24.7mg tetrakis triphenylphosphine palladium (0) of 2.4ml 0.5M bromination benzyl zinc (1.20mmol) in THF (0.02mmol) put in the 1ml diox at first.Subsequently, portions adds 102.4mg 1-(the 3-chloropyridine is [2,3-b] pyrazine-6-yl also)-3-ethyl carbamide (0.41mmol) and 1ml diox.Then with mixture heating up to 100 ℃.Behind the 7h, reaction mixture adds saturated ammonium chloride solution then.With methylene dichloride re-extract water, the organic phase with the saturated nacl aqueous solution washing is collected through dried over sodium sulfate, under reduced pressure removes solvent.Purified on silica gel (methylene chloride elutriant) obtains yellow solid.

ESI-MS: measured value m/z=308.3 (M+H ⁺); Calculated value 307 atomic mass units

¹H?NMR(d ₆-DMSO)：δ＝1.19(t，3H)，3.25-3.35(m，2H)，4.35(s，2H)，7.25(t，1H)，7.30-7.39(m，4H)，7.64(d，1H)，8.32(d，1H)，8.77(s，1H)，9.05(s，1H)，10.08(s，1H)ppm。

Embodiment 25:

1-methoxyl group-3-(the 3-phenylpyridine is [2,3-b] pyrazine-6-yl also) urea (compound 7)

The 3-phenylpyridine is the preparation (according to the reaction of scheme 6) of [2,3-b] pyrazine-6-base amine also

At nitrogen as under the shielding gas; With 1.00g 3-chloropyridine also [2; 3-b] pyrazine-6-base amine (5.54mmol); 743mg phenyl-boron dihydroxide (6.09mmol), 640mg tetrakis triphenylphosphine palladium (0) (0.55mmol) are put in 100ml N/water (1: 1) with 1.76g yellow soda ash (16.6mmol) at first, stir 2h at 80 ℃.After reaction finished, suction leached mixture, pours filtrating into 800ml zero(ppm) water.With ETHYLE ACETATE re-extract water.Under reduced pressure make organic phase remove solvent.The solid that obtains by means of silica gel column chromatography (methylene chloride elutriant) purifying.It produces yellow solid.

The preparation (according to the reaction of scheme 5) of 1-methoxyl group-3-(the 3-phenylpyridine is [2,3-b] pyrazine-6-yl also) urea

With 100mg 3-phenylpyridine also [2,3-b] pyrazine-6-base amine (0.45mmol) be dissolved in pyridine ,-nitrophenyl N-methoxyl group carbamate (0.90mmol) right with 191mg mixes.Heated mixt 4h under refluxing.For aftertreatment, under reduced pressure remove pyridine, resistates is distributed in ETHYLE ACETATE and zero(ppm) water.Separate phase, with ethyl acetate extraction water 2 times.The organic phase that merges is through MgSO ₄Drying is under reduced pressure removed solvent.Through silica gel column chromatography (methylene chloride elutriant), purifying resistates.Isolate light brown solid.

ESI-MS: measured value m/z=296.2 (M+H ⁺); Calculated value 295 atomic mass units

¹H?NMR(d ₆-DMSO)：δ＝3.75(s，3H)，7.58-7.65(m，3H)，8.03(s，1H)，8.36(d，2H)，8.45(d，1H)，9.52(s，1H)，10.16(s，1H)，11.01(s，1H)ppm。

According to embodiment 25 and general compound method, synthetic following embodiment:

Embodiment 26:

1-allyloxy-3-(the 3-phenylpyridine is [2,3-b] pyrazine-6-yl also) urea (compound 8)

ESI-MS: measured value m/z=322.2 (M+H ⁺); Calculated value 321 atomic mass units

¹H?NMR(d ₆-DMSO)：δ＝4.44(d，2H)，5.33(d，1H)，5.41(d，1H)，6.02-6.10(m，1H)，7.58-7.65(m，3H)，8.00(s，1H)，8.36(d，2H)，8.45(d，1H)，9.52(s，1H)，10.13(s，1H)，11.07(s，1H)ppm。

Embodiment 27:

1-[4-(tertiary butyl dimethylsilyl oxygen base) butyl]-3-(the 3-phenylpyridine is [2,3-b] pyrazine-6-yl also) urea (compound 36)

ESI-MS: measured value m/z=452.6 (M+H ⁺); Calculated value 451 atomic mass units

¹H?NMR(DMSO-d ₆)δ＝0.02(s，6H)，0.84(s，9H)，1.62-1.65(m，4H)，3.30-3.33(m，2H)，3.66-3.69(m，2H)，7.59-7.62(m，3H)，7.64(d，1H)，8.35(d，2H)，8.38(d，1H)，9.37(s，1H)，9.47(s，1H)，10.15(s，1H)ppm。

Embodiment 28:

1-[4-(tertiary butyl dimethylsilyl oxygen base) butyl]-3-[3-(4-hydroxy 3-methoxybenzene base) pyrido [2,3-b] pyrazine-6-yl] urea (compound 37)

ESI-MS: measured value m/z=498.5 (M+H ⁺); Calculated value 497 atomic mass units

¹H?NMR(DMSO-d ₆)δ＝0.01(s，6H)，0.83(s，9H)，1.61-1.66(m，4H)，3.30-3.33(m，2H)，3.65-3.68(m，2H)，3.93(s，3H)，6.96(d，1H)，7.59(d，1H)，7.86(dd，1H)，7.92(d，1H)，8.32(d，1H)，9.29(s，1H)，9.42(s，1H)，9.73(s，1H)，10.08(s，1H)ppm。

Embodiment 29:

Diethylammonium { 4-[3-(the 3-phenylpyridine is [2,3-b] pyrazine-6-yl also) urea] butyl } phosphonic acid ester (compound 42)

ESI-MS: measured value m/z=458.2 (M+H ⁺); Calculated value 457 atomic mass units

¹H?NMR(DMSO-d ₆)δ＝1.16(t，6H)，1.59-1.69(m，4H)，1.77-1.84(m，2H)，3.33-3.36(m，2H)，3.90-3.99(m，4H)，7.58-7.63(m，3H)，7.68(d，1H)，8.36(d，2H)，8.38(d，1H)，9.22(s，1H)，9.47(s，1H)，10.16(s，1H)ppm。

Embodiment 30:

Diethylammonium (4-{3-[3-(4-hydroxy 3-methoxybenzene base) pyrido [2,3-b] pyrazine-6-yl] urea } butyl) phosphonic acid ester (compound 44)

ESI-MS: measured value m/z=504.5 (M+H ⁺); Calculated value 503 atomic mass units

¹H?NMR(DMSO-d ₆)δ＝1.15(t，6H)，1.58-1.69(m，4H)，1.76-1.82(m，2H)，3.30-3.33(m，2H)，3.89-3.97(m，7H)，6.97(d，1H)，7.63(d，1H)，7.86(dd，1H)，7.91(d，1H)，8.32(d，1H)，9.13(s，1H)，9.41(s，1H)，9.71(s，1H)，10.07(s，1H)ppm。

Embodiment 31:

1-methoxyl group-3-[3-(4-hydroxy 3-methoxybenzene base) pyrido [2,3-b] pyrazine-6-yl] urea (compound 61)

ESI-MS: measured value m/z=342.3 (M+H ⁺); Calculated value 341 atomic mass units

¹H?NMR(d ₆-DMSO)：δ＝3.74(s，3H)，3.93(s，3H)，6.98(d，1H)，7.87(dd，1H)，7.91(d，1H)，8.02(d，1H)，8.39(d，1H)，9.46(s，1H)，9.74(s，1H)，10.03(s，1H)，10.84(s，1H)ppm。

Embodiment 32:

Diethylammonium { 2-[3-(the 3-phenylpyridine is [2,3-b] pyrazine-6-yl also) urea] ethyl } phosphonic acid ester (compound 62)

ESI-MS: measured value m/z=430.1 (M+H ⁺); Calculated value 429 atomic mass units

¹H?NMR(d ₆-DMSO)：δ＝1.21(t，6H)，2.08-2.14(m，2H)，3.48-3.55(m，2H)，3.98-4.08(m，4H)，7.58-7.63(m，3H)，7.72(d，1H)，8.35(d，2H)，8.39(d，1H)，9.14(s，1H)，9.47(s，1H)，10.22(s，1H)ppm。

Embodiment 33:

4-[3-(the 3-phenylpyridine is [2,3-b] pyrazine-6-yl also) urea] butyl ethyl carbamate (compound 38)

The preparation of 1-(4-hydroxybutyl)-3-(the 3-phenylpyridine is [2,3-b] pyrazine-6-yl also) urea

360mg (0.22mmol) 1-[4-(tertiary butyl dimethylsilyl oxygen base) butyl]-3-(the 3-phenylpyridine is [2,3-b] pyrazine-6-yl also) urea is dissolved in the 20ml methylene dichloride, and mixes with 2 moles of Viraholizations of 5ml (isopropanolic) HCl solution.Behind stirring at room 12h, water washing reaction mixture, dry (Na ₂SO ₄).Under reduced pressure remove solvent, obtain the glassy yellow solid.

ESI-MS: measured value m/z=338.3 (M+H ⁺); Calculated value 337 atomic mass units

¹H?NMR(DMSO-d ₆)δ＝1.58-1.64(m，4H)，3.30-3.34(m，2H)，3.48-3.53(m，2H)，4.48(t，1H)，7.57-7.63(m，3H)，7.66(d，1H)，8.35-8.38(m，2H)，9.30(s，1H)，9.46(s，1H)，10.13(s，1H)ppm。

The preparation of 4-[3-(the 3-phenylpyridine is [2,3-b] pyrazine-6-yl also) urea] butyl ethyl carbamate

30mg (0.08mmol) 1-(4-hydroxybutyl)-3-(the 3-phenylpyridine is [2,3-b] pyrazine-6-yl also) urea is dissolved in the 5ml pyridine, mixes, stir 6h at 100 ℃ with 7.6 μ l (0.10mmol) ethyl isocyanates.Pour reaction mixture into 200ml water, stir 15min.Leach precipitated solid, and dry.This produces white solid.

¹H?NMR(DMSO-d ₆)δ＝0.97(t，3H)，1.60-1.77(m，4H)，2.96-3.00(m，2H)，3.33-3.35(m，2H)，4.01-4.04(m，2H)，7.07(t，1H)，7.58-7.64(m，3H)，7.66(d，1H)，8.35(d，2H)，8.38(d，1H)，9.32(s，1H)，9.47(s，1H)，10.17(s，1H)ppm。

Embodiment 34:

Methyl 4-[3-(the 3-phenylpyridine is [2,3-b] pyrazine-6-yl also) urea] butyl carbonic ether (compound 39)

The preparation of methyl 4-[3-(the 3-phenylpyridine is [2,3-b] pyrazine-6-yl also) urea] butyl carbonic ether

With 30mg (0.08mmol) 1-(4-hydroxybutyl)-3-(3-phenylpyridine also [2; 3-b] pyrazine-6-yl) urea is suspended in the 2ml methylene dichloride; And with 9.3 μ l (0.12mmol) methyl-chloroformates, 23 μ l (0.16mmol) triethylamines and 1mg (0.01mmol) Dimethylamino pyridine mix.At stirring at room solution 4h.With 50ml methylene dichloride diluted reaction mixture, use water washing, dry (Na ₂SO ₄).Under reduced pressure remove solvent, through silica gel column chromatography (methylene chloride elutriant), purifying resistates.Isolate white solid.

ESI-MS: measured value m/z=396.3 (M+H ⁺); Calculated value 395 atomic mass units

¹H?NMR(DMSO-d ₆)δ＝1.61-1.66(m，2H)，1.76-1.78(m，2H)，3.34-3.36(m，2H)，3.67(s，1H)，4.17-4.19(m，2H)，7.59-7.63(m，3H)，7.66(d，1H)，8.35(d，2H)，8.38(d，1H)，9.34(s，1H)，9.47(s，1H)，10.17(s，1H)ppm。

According to embodiment 34 and general compound method, synthetic following instance:

Embodiment 35:

2,2-dimethyl-[1,3] dioxolane-4-ylmethyl 4-[3-(the 3-phenylpyridine is [2,3-b] pyrazine-6-yl also) urea] butyl carbonic ether (compound 40)

ESI-MS: measured value m/z=496.0 (M+H ⁺); Calculated value 495 atomic mass units

¹H?NMR(DMSO-d ₆)δ＝1.24(s，3H)，1.29(s，3H)，1.61-1.67(m，2H)，1.77-1.82(m，2H)，3.34-3.37(m，2H)，3.65(dd，1H)，3.98(dd，1H)，4.03(dd，1H)，4.15(dd，1H)，4.17-4.28(m，3H)，7.58-7.63(m，3H)，7.67(d，1H)，8.36(d，2H)，8.38(d，1H)，9.34(s，1H)，9.47(s，1H)，10.17(s，1H)ppm。

Embodiment 36:

2,3-dihydroxypropyl 4-[3-(the 3-phenylpyridine is [2,3-b] pyrazine-6-yl also) urea] butyl carbonic ether (compound 41)

2, the preparation of 3-dihydroxypropyl 4-[3-(the 3-phenylpyridine is [2,3-b] pyrazine-6-yl also) urea] butyl carbonic ether

With 50mg (0.10mmol) 2; 2-dimethyl-[1,3] dioxolane-4-ylmethyl 4-[3-(the 3-phenylpyridine is [2,3-b] pyrazine-6-yl also) urea] butyl carbonic ether is dissolved in the 20ml methylene dichloride; Mix with 17 μ l (0.13mmol) boron trifluoride ethyl ether compounds, at stirring at room 4h.Under reduced pressure remove solvent, through silica gel column chromatography (methylene chloride elutriant), purifying resistates.Isolate white solid.

ESI-MS: measured value m/z=456.4 (M+H ⁺); Calculated value 455 atomic mass units

¹H?NMR(DMSO-d ₆)δ＝1.62-1.67(m，2H)，1.76-1.82(m，2H)，3.28-3.52(m，4H)，3.62-3.66(m，1H)，3.96(dd，1H)，4.11(dd，1H)，4.16-4.20(m，2H)，4.66(t，1H)，4.96(d，1H)，7.58-7.65(m，3H)，7.67(d，1H)，8.35(d，2H)，8.38(d，1H)，9.31(s，1H)，9.47(s，1H)，10.17(s，1H)ppm。

Embodiment 37:

{ 4-[3-(the 3-phenylpyridine is [2,3-b] pyrazine-6-yl also) urea] butyl } phosphoric acid (compound 43)

The preparation of { 4-[3-(the 3-phenylpyridine is [2,3-b] pyrazine-6-yl also) urea] butyl } phosphoric acid

60mg (0.13mmol) diethylammonium { 4-[3-(the 3-phenylpyridine is [2,3-b] pyrazine-6-yl also) urea] butyl } phosphonic acid ester is dissolved in 5ml methylene dichloride and 5ml hexamethyldisilazane, mixes with 100mg (0.66mmol) bromo trimethyl silane.Behind stirring at room 6h, concentrated reaction mixture under reduced pressure, resistates 2h blunges.It produces yellow solid.

ESI-MS: measured value m/z=402.3 (M+H ⁺); Calculated value 401 atomic mass units

¹H?NMR(DMSO-d ₆)δ＝1.51-1.68(m，6H)，3.33-3.36(m，2H)，7.58-7.63(m，3H)，7.73(d，1H)，8.33-8.37(m，3H)，9.06(S，1H)，9.44(s，1H)，10.12(s，1H)ppm。

According to embodiment 37 and general compound method, synthetic following instance:

Embodiment 38:

(4-{3-[3-(4-hydroxy 3-methoxybenzene base) pyrido [2,3-b] pyrazine-6-yl] urea } butyl) phosphoric acid (compound 45)

ESI-MS: measured value m/z=448.3 (M+H ⁺); Calculated value 447 atomic mass units

¹H?NMR(DMSO-d ₆)δ＝1.48-1.67(m，6H)，3.24-3.28(m，2H)，3.92(s，3H)，6.98(d，1H)，7.70(d，1H)，7.85(dd，1H)，7.89(d，1H)，8.28(d，1H)，8.95(s，1H)，9.38(s，1H)，10.02(s，1H)ppm。

Embodiment 39:

{ 2-[3-(the 3-phenylpyridine is [2,3-b] pyrazine-6-yl also) urea] ethyl } phosphoric acid (compound 63)

ESI-MS: measured value m/z=374.2 (M+H ⁺); Calculated value 373 atomic mass units

¹H?NMR(d ₆-DMSO)：δ＝1.86-1.93(m，2H)，3.45-3.52(m，2H)，7.57-7.63(m，3H)，7.76(d，1H)，8.35(d，2H)，8.37(d，1H)，8.96(s，1H)，9.45(s，1H)，10.17(s，1H)ppm。

Embodiment 40:

Ethyl n-(the 3-phenylpyridine is [2,3-b] pyrazine-6-yl also) oxamide (compound 59)

The preparation (according to the reaction of scheme 5) of ethyl n-(the 3-phenylpyridine is [2,3-b] pyrazine-6-yl also) oxamide

With 200mg (0.90mmol) 3-phenylpyridine also [2,3-b] pyrazine-6-base amine be dissolved in the 20ml pyridine, mix with 0.11ml (0.99mmol) ethyl oxalyl chloride.Behind stirring at room 2h, pour solution into ice-water.Leach precipitated solid, water thoroughly washs.It produces the glassy yellow solid.

ESI-MS: measured value m/z=323.2 (M+H ⁺); Calculated value 322 atomic mass units

¹H?NMR(DMSO-d ₆)δ＝1.37(t，3H)，4.35-4.41(m，2H)，7.60-7.66(m，3H)，8.38(d，2H)，8.43(bs，1H)，8.61(d，1H)，9.63(s，1H)，11.67(s，1H)ppm。

Embodiment 41:

N-ethyl-N '-(the 3-phenylpyridine is [2,3-b] pyrazine-6-yl also) oxamide (compound 60)

The preparation (according to the reaction of scheme 5) of N-ethyl-N '-(the 3-phenylpyridine is [2,3-b] pyrazine-6-yl also) oxamide

23mg (0.07mmol) ethyl n-(the 3-phenylpyridine is [2,3-b] pyrazine-6-yl also) oxamide is dissolved among the 5ml exsiccant THF, and mixes with the solution of 0-15ml (0.38mmol) 2.0M ethylamine in THF.

In stirring at room after 48 hours, the neutralization reaction mixture.Leach precipitated solid, under reduced pressure concentrated filtrate is to dry.The solid that obtains through silica gel column chromatography (methylene chloride elutriant) purifying.It produces the glassy yellow solid.

ESI-MS: measured value m/z=322.3 (M+H ⁺); Calculated value 321 atomic mass units

¹H?NMR(DMSO-d ₆)δ＝1.13(t，3H)，3.27(q，2H)，7.60-7.66(m，3H)，8.39(d，2H)，8.54(d，1H)，8.65(d，1H)，9.24(t，1H)，9.64(s，1H)，10.31(s，1H)ppm。

Embodiment 42:

Ethyl 4-[6-(3-ethyl-1-phenylurea) pyrido [2,3-b] pyrazine-3-yl] phenylcarbamate (compound 20)

The preparation (according to the reaction of scheme 5) of ethyl 4-[6-(3-ethyl-1-phenylurea) pyrido [2,3-b] pyrazine-3-yl] phenylcarbamate

100mg 4-(6-phenyl amino pyrido [2,3-b] pyrazine-3-yl) phenolate acidulants (0.28mmol) is put in the 3ml pyridine at first, added 65.3mg ethyl isocyanate (0.90mmol) in room temperature.Mixture is stirred 5h at 80 ℃, add other 32.0mg ethyl isocyanate (0.45mmol) then, mixture is stirred other 4h at 80 ℃.Under reduced pressure remove solvent then.The solid that obtains by means of silica gel column chromatography (methylene chloride and normal heptane/acetone elutriant) purifying 2 times.It produces the glassy yellow solid.

Fusing point: 147-151 ℃

ESI-MS: measured value m/z=457.3 (M+H ⁺); Calculated value 456 atomic mass units

¹H?NMR(CDCl3)：δ＝1.28(t，3H)，1.40(t，3H)，3.39(quint，2H)，3.57(quint，2H)，5.09(t，1H)，6.80(d，1H)，7.37(d，2H)，7.40(d，2H)，7.50(t，1H)，7.57(t，2H)，8.10(d，1H)，8.30(d，2H)，9.25(s，1H)，10.76(t，1H)ppm。

About the preparation of 4-(6-phenyl amino pyrido [2,3-b] pyrazine-3-yl) phenolate acidulants, with reference to WO 99/17759.

Embodiment 43:

The tertiary butyl { 4-[6-(3-ethyl carbamide) pyrido [2,3-b] pyrazine-3-yl] phenyl } carbamate (compound 21)

The preparation (according to the reaction of scheme 6) of the tertiary butyl { 4-[6-(3-ethyl carbamide) pyrido [2,3-b] pyrazine-3-yl] phenyl } carbamate

With 83mg 1-(3-chloropyridine also [2; 3-b] pyrazine-6-yl)-3-ethyl carbamide (0.33mmol), [4-(4 for the 120mg tertiary butyl; 4,5,5-tetramethyl-[1; 3,2] phenyl dioxane pentaborane-2-yl)] carbamate (0.36mmol), 106mg yellow soda ash (1.00mmol) and 19mg four-(triphenylphosphine) palladium (0.02mmol) put into the N/water mixture of the 7ml degassing at first.With mixture heating up to 100 ℃ lasting 4h.The refrigerative mixture is mixed with water.Leach precipitated solid, water and washed with dichloromethane.It produces beige solid.

Fusing point: 281-283 ℃

¹H?NMR(d ₆-DMSO)：δ＝1.20(t，3H)，1.52(s，9H)，3.25-3.38(m，2H)，7.65(d，1H)，7.69(d，2H)，8.29(d，2H)，8.33(d，1H)，9.09(bs，1H)，9.41(s，1H)，9.72(s，1H)，10.09(s，1H)ppm。

According to embodiment 43 and general compound method, synthetic following embodiment:

Embodiment 44:

2-methoxy ethyl { 4-[6-(3-ethyl carbamide) pyrido [2,3-b] pyrazine-3-yl] phenyl } carbamate (compound 22)

Fusing point: 249-251 ℃

ESI-MS: measured value m/z=411.3 (M+H ⁺); Calculated value 410 atomic mass units

¹H?NMR(d ₆-DMSO)：δ＝1.20(t，3H)，3.31(s，3H)，3.45-3.38(m，2H)，3.58-3.64(m，2H)，4.24-4.27(m，2H)，7.65(d，1H)，7.70(d，2H)，8.31(d，2H)，8.37(d，1H)，9.08(bs，1H)，9.41(s，1H)，10.09(s，1H)，10.11(s，1H)ppm。

Embodiment 45:

1-ethyl-3-{3-[4-(3-ethyl carbamide) phenyl] pyrido [2,3-b] pyrazine-6-yl } urea (compound 23)

Fusing point:＞350 ℃ (decomposition)

ESI-MS: measured value m/z=380.2 (M+H ⁺); Calculated value 379 atomic mass units

¹H?NMR(d ₆-DMSO)：δ＝1.08(t，3H)，1.20(t，3H)，3.14(quint，2H)，3.32-3.38(m，2H)，6.33(t，1H)，7.60-7.64(m，3H)，8.25(d，2H)，8.32(d，1H)，8.88(s，1H)，9.12(bs，1H)，9.39(s，1H)，10.06(s，1H)ppm。

Embodiment 46:

1-{3-[4-(3, the 3-dimethyl urea) phenyl] pyrido [2,3-b] pyrazine-6-yl }-3-ethyl carbamide (compound 24)

Fusing point:＞350 ℃

ESI-MS: measured value m/z=380.3 (M+H ⁺); Calculated value 379 atomic mass units

¹H?NMR(d ₆-DMSO)：δ＝1.20(t，3H)，2.98(s，6H)，3.25-3.38(m，2H)，7.63(d，1H)，7.74(d，2H)，8.26(d，2H)，8.33(d，1H)，8.63(s，1H)，9.12(bs，1H)，9.41(s，1H)，10.07(s，1H)ppm。

Embodiment 47:

1-ethyl-3-{3-[6-(3-ethyl carbamide) pyridin-3-yl] pyrido [2,3-b] pyrazine-6-yl } urea (compound 25)

¹H?NMR(d ₆-DMSO)：δ＝1.13(t，3H)，1.20(t，3H)，3.23(quint，2H)，3.25-3.38(m，2H)，7.63(d，1H)，7.67(d，1H)，8.25(d，1H)，8.00(bs，1H)，8.35(d，1H)，8.61(d，1H)，9.08(bs，1H)，9.17(s，1H)，9.44(s，1H)，9.55(s，1H)，10.12(s，1H)ppm。

Embodiment 48:

1-ethyl-3-[3-(4-morpholine-4-ylmethyl phenyl) pyrido [2,3-b] pyrazine-6-yl] urea (compound 28)

ESI-MS: measured value m/z=393.4 (M+H ⁺); Calculated value 392 atomic mass units

¹H?NMR(d ₆-DMSO)：δ＝1.20(t，3H)，2.41(bs，4H)，3.33-3.38(m，2H)，3.58(s，2H)，3.61(t，4H)，7.55(d，2H)，7.69(t，1H)，8.30(d，2H)，8.37(d，1H)，9.10(bs，1H)，9.44(s，1H)，10.13(s，1H)ppm。

Embodiment 49:

N-{4-[6-(3-ethyl carbamide) pyrido [2,3-b] pyrazine-3-yl] phenyl }-2-(2-methoxy ethoxy) ethanamide (compound 30)

Fusing point: 212-215 ℃

ESI-MS: measured value m/z=425.2 (M+H ⁺); Calculated value 424 atomic mass units

¹H?NMR(d ₆-DMSO)：δ＝1.20(t，3H)，3.32(s，3H)，3.34-3.38(m，2H)，3.56(dd，2H)，3.71(dd，2H)，4.15(s，2H)，7.66(d，1H)，7.89(d，2H)，8.33-8.36(m，3H)，9.11(bs，1H)，9.43(s，1H)，9.97(s，1H)，10.11(s，1H)ppm。

Embodiment 50:

2-benzyloxy-N-{4-[6-(3-ethyl carbamide) pyrido [2,3-b] pyrazine-3-yl] phenyl } ethanamide (compound 35)

Fusing point: 254-256 ℃

¹H?NMR(d ₆-DMSO)：δ＝1.20(t，3H)，3.28-3.38(m，2H)，4.16(S，2H)，4.66(s，2H)，7.31(t，1H)，7.33(t，1H)，7.40(t，2H)，7.44(d，1H)，7.66(d，1H)，7.91(d，2H)，8.33-8.36(m，3H)，9.11(bs，1H)，9.44(s，1H)，10.10(s，1H)，10.14(s，1H)ppm。

Embodiment 51:

1-ethyl-3-[3-(3-TMS phenyl) pyrido [2,3-b] pyrazine-6-yl] urea (compound 46)

Fusing point: 224-228 ℃

ESI-MS: measured value m/z=366.4 (M+H ⁺); Calculated value 365 atomic mass units

¹H?NMR(d ₆-DMSO)：δ＝0.35(s，9H)，1.21(t，3H)，3.28-3.38(m，2H)，7.60(t，1H)，7.73(t，2H)，8.32(d，1H)，8.37(d，1H)，8.46(s，1H)，9.04(bs，1H)，9.48(s，1H)，10.12(s，1H)ppm。

In embodiment 51, use diox/water as solvent, substitute N/water.

Through following method or method known to those skilled in the art, prepare commercial unavailable boric acid derivatives:

The preparation of 2-methoxy ethyl [4-(4,4,5,5-tetramethyl-[1,3,2] dioxane pentaborane-2-yl) phenyl] carbamate

107mg 4-(4,4,5,5-tetramethyl-[1,3,2] dioxane pentaborane-2-yl) phenyl amine (0.48mmol) is dissolved in THF.Add 96mg 2-methoxy ethyl chloro-formic ester (0.68mmol) and 79mg N-methylmorpholine (0.78mmol) in room temperature.In stirring at room mixture 1 day, leach precipitated solid, under reduced pressure remove solvent.It produces light yellow oil, without being further purified, is used for next reaction.

Through aforesaid method or method known to those skilled in the art, prepare following boric acid derivatives:

1-ethyl-3-[4-(4,4,5,5-tetramethyl--[1,3,2] dioxane pentaborane-2-yl) phenyl] urea

1,1-dimethyl--3-[4-(4,4,5,5-tetramethyl--[1,3,2] dioxane pentaborane-2-yl) phenyl] urea

1-ethyl-3-[5-(4,4,5,5-tetramethyl--[1,3,2] dioxane pentaborane-2-yl) pyridine-2-yl] urea

2-(2-methoxy ethoxy)-N-[4-(4,4,5,5-tetramethyl--[1,3,2] dioxane pentaborane-2-yl) phenyl] ethanamide

2-benzyloxy-N-[4-(4,4,5,5-tetramethyl--[1,3,2] dioxane pentaborane-2-yl) phenyl] ethanamide

Embodiment 52:

1-ethyl-3-{3-[2-(4-fluorophenyl) ethyl] pyrido [2,3-b] pyrazine-6-yl } urea (compound 26)

1-ethyl-3-{3-[2-(4-fluorophenyl) ethyl] pyrido [2,3-b] pyrazine-6-yl } preparation of urea

With 108mg 1-ethyl-3-{3-[2-(4-fluorophenyl) vinyl] pyrido [2,3-b] pyrazine-6-yl } urea (0.32mmol) (embodiment 27) is dissolved in hot ethanol.Add 112mg ammonium formiate (1.78mmol) and 110mg palladium carbon (10%), reacting by heating mixture 7.5h under refluxing.Leach catalyzer from the refrigerative reaction mixture, mother liquor is removed solvent.Through silica gel column chromatography (methylene chloride elutriant), purifying crude product.It produces yellow solid.

Fusing point: 207-209 ℃

ESI-MS: measured value m/z=340.2 (M+H ⁺); Calculated value 339 atomic mass units

¹H?NMR(d ₆-DMSO)：δ＝1.20(t，3H)，3.12(t，2H)，3.25-3.38(m，4H)，7.10(t，2H)，7.32(dd，2H)，7.63(d，1H)，8.31(d，1H)，8.71(s，1H)，9.09(bs，1H)，10.06(s，1H)ppm。

Embodiment 53:

1-ethyl-3-(3-{4-[2-(2-methoxy ethoxy) oxyethyl group] phenyl } pyrido [2,3-b] pyrazine-6-yl) urea (compound 29)

The preparation (according to the reaction of scheme 9) of 1-ethyl-3-(3-{4-[2-(2-methoxy ethoxy) oxyethyl group] phenyl } pyrido [2,3-b] pyrazine-6-yl) urea

29mg sodium hydride (0.71mmol) (60% suspension-s in MO) is put in the 4ml exsiccant N at first.At 0 ℃, add 70mg 1-ethyl-3-[3-(4-hydroxyl-phenyl) pyrido [2,3-b] pyrazine-6-yl] urea (0.23mmol), be dissolved in the 2.5ml N.At stirring at room mixture 1h.Subsequently, add 68mg 1-bromo-2-(2-oxyethyl group methoxy base) ethane (0.34mmol) at 0 ℃, at stirring at room reaction mixture 17h.After this, add other 22mg 1-bromo-2-(2-oxyethyl group methoxy base) ethane (0.12mmol), at 80 ℃ of stirred reaction mixture 2h.Water is added the refrigerative reaction mixture, use the dichloromethane extraction water.Organic phase is removed solvent, through silica gel column chromatography (methylene chloride elutriant), purifying crude product after dried over sodium sulfate.This produces yellow solid.

ESI-MS: measured value m/z=412.3 (M+H ⁺); Calculated value 411 atomic mass units

¹H?NMR(d ₆-DMSO)：δ＝1.20(t，3H)，3.26(s，3H)，3.29-3.38(m，2H)，3.48(dd，2H)，3.62(dd，2H)，3.80(dd，2H)，4.22(dd，2H)，7.17(d，2H)，7.64(t，1H)，8.31-8.35(m，3H)，9.14(bs，1H)，9.42(s，1H)，10.09(s，1H)ppm。

Embodiment 54:

N-[6-(3-ethyl carbamide) pyrido [2,3-b] pyrazine-3-yl]-4-methyl benzamide (compound 31)

The preparation (according to the reaction of scheme 7) of N-[6-(3-ethyl carbamide) pyrido [2,3-b] pyrazine-3-yl]-4-methyl benzamide

100mg 1-(the 3-EL-970 is [2,3-b] pyrazine-6-yl also)-3-ethyl carbamide (0.43mmol) is put in the 5ml exsiccant pyridine at first, dropwise added 57 μ l p-methylphenyl chlorine (0.43mmol).At 60 ℃ of 2h that stir the mixture.After this, dropwise add other 29 μ l p-methylphenyl chlorine (0.22mmol), at 60 ℃ of other 2h of stirred reaction mixture.The refrigerative reaction mixture is added ice-water, and with 1N HCl neutralization, suction leaches solid.Through silica gel column chromatography (methylene chloride elutriant) purifying crude product.It produces light yellow solid.

ESI-MS: measured value m/z=351.1 (M+H ⁺); Calculated value 350 atomic mass units

¹H?NMR(d ₆-DMSO)：δ＝1.18(t，3H)，2.42(s，3H)，3.31(quint，2H)，7.37(d，2H)，7.55(d，1H)，8.04(d，2H)，8.31(d，1H)，9.10(bs，1H)，9.56(s，1H)，9.96(s，1H)，11.39(bs，1H)ppm。

Embodiment 55:

1-[3-(the 4-cyclohexyl phenyl is amino) pyrido [2,3-b] pyrazine-6-yl]-3-ethyl carbamide (compound 47)

The preparation (according to the reaction of scheme 3) of 1-[3-(the 4-cyclohexyl phenyl is amino) pyrido [2,3-b] pyrazine-6-yl]-3-ethyl carbamide

With 83mg 1-(3-chloropyridine also [2; 3-b] pyrazine-6-yl)-3-ethyl carbamide (0.33mmol); 99mg 4-cyclohexyl aniline (0.55mmol); 30mg sodium tert-butoxide (0.30mmol), 29mg three (dibenzalacetone) two palladiums (0) (0.03mmol) are put in the 1.5ml exsiccant toluene with 68mg 2-(dicyclohexyl phosphanyl) biphenyl (0.19mmol) at first.Under nitrogen, reacting by heating mixture to 100 ℃ continues 30 minutes in microwave (100 watts).Under reduced pressure remove solvent, through silica gel column chromatography (methylene chloride elutriant), purifying crude product.It produces yellow solid.

Fusing point: 246-248 ℃

ESI-MS: measured value m/z=391.3 (M+H ⁺); Calculated value 390 atomic mass units

¹H?NMR(d ₆-DMSO)：δ＝1.18(t，3H)，1.22-1.26(m，1H)，1.33-1.44(m，4H)，1.71(d，1H)，1.80(d，4H)，2.45-2.51(m，1H)，3.25-3.30(m，2H)，7.22(d，2H)，7.40(d，1H)，7.89(d，2H)，8.08(d，1H)，8.37(s，1H)，8.73(bs，1H)，9.87(s，1H)，10.06(s，1H)ppm。

According to embodiment 55 and general compound method, synthetic following embodiment:

Embodiment 56:

1-ethyl-3-[3-(4-methane sulfonyl phenyl amino) pyrido [2,3-b] pyrazine-6-yl] urea (compound 48)

Fusing point: 275-280 ℃

ESI-MS: measured value m/z=387.3 (M+H ⁺); Calculated value 386 atomic mass units

¹H?NMR(d ₆-DMSO)：δ＝1.20(t，3H)，3.19(s，3H)，3.25-3.38(m，2H)，7.54(d，1H)，7.92(d，2H)，8.16(d，1H)，8.24(d，2H)，8.49(s，1H)，8.62(bs，1H)，9.93(s，1H)，10.56(s，1H)ppm。

Embodiment 57:

N-{5-[6-(3-ethyl carbamide) pyrido [2,3-b] pyrazine-3-base is amino]-2-aminomethyl phenyl } NSC-249992 (compound 49)

Fusing point: 247-250 ℃

ESI-MS: measured value m/z=416.2 (M+H ⁺); Calculated value 415 atomic mass units

¹H?NMR(d ₆-DMSO)：δ＝1.17(t，3H)，2.28(s，3H)，3.03(s，3H)，3.25-3.38(m，2H)，7.23(d，1H)，7.33(d，1H)，7.75(d，1H)，8.06-8.09(m，2H)，8.37(s，1H)，8.92(bs，1H)，9.09(s，1H)，9.77(s，1H)，10.09(s，1H)ppm。

Embodiment 58:

3-[6-(3-ethyl carbamide) pyrido [2,3-b] pyrazine-3-base is amino]-N-methyl-benzamide (compound 50)

Fusing point: 228-234 ℃

¹H?NMR(d ₆-DMSO)：δ＝1.19(t，3H)，2.80(d，3H)，3.25-3.38(m，2H)，7.39-7.48(m，3H)，8.09-8.11(m，2H)，8.41(s，2H)，8.46(s，1H)，8.83(bs，1H)，9.86(s，1H)，10.22(s，1H)ppm。

Embodiment 59:

1-ethyl-3-[3-(4-piperidines-1-ylmethyl phenyl amino) pyrido [2,3-b] pyrazine-6-yl] urea (compound 51)

Fusing point: 221-224 ℃

ESI-MS: measured value m/z=406.4 (M+H ⁺); Calculated value 405 atomic mass units

¹H?NMR(d ₆-DMSO)：δ＝1.19(t，3H)，1.39(bs，2H)，1.49(quint，4H)，2.32(bs，4H)，3.25-3.35(m，2H)，3.39(s，2H)，7.27(d，2H)，7.39(d，1H)，7.92(d，2H)，8.08(d，1H)，8.38(s，1H)，8.78(bs，1H)，9.82(s，1H)，10.05(s，1H)ppm。

Embodiment 60:

1-ethyl-3-[3-(4-thiene-3-yl-phenyl amino) pyrido [2,3-b] pyrazine-6-yl] urea (compound 52)

Fusing point: 264-267 ℃

ESI-MS: measured value m/z=391.4 (M+H ⁺); Calculated value 390 atomic mass units

¹H?NMR(d ₆-DMSO)：δ＝1.21(t，3H)，3.25-3.35(m，2H)，7.47(d，1H)，7.58(d，1H)，7.65(dd，1H)，7.74(d，2H)，7.82(d，1H)，8.05(d，2H)，8.11(d，1H)，8.42(s，1H)，8.62(bs，1H)，9.86(s，1H)，10.18(s，1H)ppm。

Embodiment 61:

N-{4-[6-(3-ethyl carbamide) pyrido [2,3-b] pyrazine-3-base is amino] phenyl } ethanamide (compound 53)

ESI-MS: measured value m/z=366.2 (M+H ⁺); Calculated value 365 atomic mass units

¹H?NMR(d ₆-DMSO)：δ＝1.20(t，3H)，2.03(s，3H)，3.25-3.35(m，2H)，7.27(d，1H)，7.34(d，2H)，7.57(d，2H)，7.90(d，1H)，8.07(d，1H)，8.94(bs，1H)，9.79(s，1H)，9.89(s，1H)，10.03(s，1H)ppm。

Embodiment 62:

Ethyl 3-[6-(3-ethyl carbamide) pyrido [2,3-b] pyrazine-3-base is amino] benzoic ether (compound 54)

Fusing point: 252-255 ℃

ESI-MS: measured value m/z=381.3 (M+H ⁺); Calculated value 380 atomic mass units

¹H?NMR(d ₆-DMSO)：δ＝1.19(t，3H)，1.35(t，3H)，3.25-3.35(m，2H)，4.35(q，2H)，7.40(d，1H)，7.52(t，1H)，7.64(d，1H)，8.12(d，1H)，8.29(d，1H)，8.41(s，1H)，8.62(s，1H)，8.90(bs，1H)，9.86(s，1H)，10.31(s，1H)ppm。

Embodiment 63:

4-[6-(3-ethyl carbamide) pyrido [2,3-b] pyrazine-3-yl] phenyl 2-methoxy ethyl carbonate salt acidulants (compound 55)

The preparation of 4-[6-(3-ethyl carbamide) pyrido [2,3-b] pyrazine-3-yl] phenyl 2-methoxy ethyl carbonate salt acidulants

21mg 4-[6-(3-ethyl carbamide) pyrido [2,3-b] pyrazine-3-yl] phenyl 2-methoxy ethyl carbonic ether (0.05mmol) (embodiment 10) is dissolved in 2.5ml methylene chloride (2: 1).The 2-propanol solution that adds 0.02ml 5-6N HCl was in stirring at room mixture 1 day.Remove solvent then.It produces yellow solid.

Fusing point: 190-193 ℃

¹H?NMR(d ₆-DMSO)：δ＝1.20(t，3H)，3.31-3.35(m，5H)，3.63-3.66(m，2H)，4.37(dd，2H)，7.50(d，2H)，7.70(d，1H)，8.38(d，1H)，8.41(d，2H)，9.09(bs，1H)，9.47(s，1H)，1O.14(s，1H)ppm。

Embodiment 64:

4-[6-(3-ethyl carbamide) pyrido [2,3-b] pyrazine-3-yl] phenyl 2-methoxy ethyl carbonic ether p-toluenesulfonic esters (compound 56)

The preparation of 4-[6-(3-ethyl carbamide) pyrido [2,3-b] pyrazine-3-yl] phenyl 2-methoxy ethyl carbonic ether p-toluenesulfonic esters

48mg 4-[6-(3-ethyl carbamide) pyrido [2,3-b] pyrazine-3-yl] phenyl 2-methoxy ethyl carbonic ether (0.12mmol) is put in 4ml methylene dichloride and the 0.7ml methyl alcohol at first.Add 23mg tosic acid monohydrate (0.12mmol) in room temperature, be dissolved in 2ml methylene dichloride and 0.5ml methyl alcohol.At 0 ℃ of stirred reaction mixture 1h, stirring at room 1 day.Remove solvent, from methylene dichloride/normal heptane recrystallization resistates.Suction leaches sedimentary product, washs with normal heptane.It produces yellow solid.

Fusing point: 145-147 ℃

¹H?NMR(d ₆-DMSO)：δ＝1.20(t，3H)，2.29(s，3H)，3.30-3.36(m，5H)，3.64(dd，2H)，4.38(dd，2H)，7.11(d，2H)，7.47(d，2H)，7.50(d，2H)，7.70(d，1H)，8.38(d，1H)，8.41(d，2H)，9.09(bs，1H)，9.47(s，1H)，10.14(s，1H)ppm。

Embodiment 65:

4-{6-[3-(4-hydroxybutyl) urea] pyrido [2,3-b] pyrazine-3-yl } phenyl 2-methoxy ethyl carbonate salt acidulants (compound 58)

4-{6-[3-(4-hydroxybutyl) urea] pyrido [2,3-b] pyrazine-3-yl } preparation of phenyl 2-methoxy ethyl carbonate salt acidulants

With 117mg 4-{6-[3-(4-(tertiary butyl dimethylsilyl oxygen base) butyl) urea] pyrido [2,3-b] pyrazine-3-yl }-phenyl 2-methoxy ethyl carbonic ether (0.21mmol) is dissolved in the pre-dried methylene dichloride of 40ml.The 2-propanol solution that adds 0.5ml 5-6N HC l was stirring at room reaction mixture 15 minutes.Use the water washing organic phase,, concentrate through dried over sodium sulfate.It produces yellow solid.

Fusing point: 165-168 ℃

ESI-MS: measured value m/z=456.2 (M+H ⁺); Calculated value 455 atomic mass units

¹H?NMR(d ₆-DMSO)：δ＝1.61(quint，4H)，2.29(s，3H)，3.30-3.36(m，2H)，3.49(t，2H)，3.64(dd，2H)，4.38(dd，2H)，7.49(d，2H)，7.66(d，1H)，8.38(d，1H)，8.43(d，2H)，9.33(bs，1H)，9.48(s，1H)，10.17(s，1H)ppm。

About 4-{6-[3-(4-(tertiary butyl dimethylsilyl oxygen base) butyl) urea] pyrido [2,3-b] pyrazine-3-yl } preparation of phenyl 2-methoxy ethyl carbonic ether, referring to scheme 5,6 and 8, general compound method and method known to those skilled in the art.

Embodiment 66:

2,2-dimethyl propylene acyloxy methoxyl group-(4-{3-[3-(4-hydroxy 3-methoxybenzene base) pyrido [2,3-b] pyrazine-6-yl] urea } butyl) phosphinoyl oxygen ylmethyl 2,2-dimethyl propylene acid esters (compound 65)

2,2-dimethyl propylene acyloxy methoxyl group-(4-{3-[3-(4-hydroxy 3-methoxybenzene base) pyrido [2,3-b] pyrazine-6-yl] urea } butyl) phosphinoyl oxygen ylmethyl 2, the preparation of 2-dimethyl propylene acid esters

With 94mg 4-{3-[3-(4-hydroxy 3-methoxybenzene base) pyrido [2; 3-b] pyrazine-6-yl] urea } butyl) phosphoric acid (0.20mmol) is dissolved in 15ml DMF; Mix with 360 μ l PIVALIC ACID CRUDE (25) chloromethyl esters (2.40mmol) and 30 μ l triethylamines (0.21mmol), stir 10h at 60 ℃.Pour reaction mixture into 50ml water, with ethyl acetate extraction 3 times.The organic phase that merges is through MgSO ₄Drying is under reduced pressure removed solvent.Subsequently through column chromatography (elutriant: methylene chloride) purifying resistates.Isolate beige solid.

ESI-MS: measured value m/z=676.4 (M+H ⁺); Calculated value 675 atomic mass units

¹H?NMR(d ₆-DMSO)：δ＝1.12(s，18H)，1.57-1.68(m，4H)，1.90-1.97(m，2H)，3.28-3.31(m，3.93(s，3H)，5.54-5.59(m，4H)，6.97(d，1H)，7.64(d，1H)，7.86(dd，1H)，7.91(d，1H)，8.32(d，1H)，9.08(s，1H)，9.41(s，1H)，9.70(s，1H)，10.06(s，1H)ppm。

II) biological effect of compound of the present invention

II.1) acellular kinase assay (by means of the ALPHA technology)

In enzyme test, on different human serine/threonine kinases, Tyrosylprotein kinase and lipid kinase, tested the retarding effect of compound of the present invention.Used the recombinant human kinases, Erk2 for example, PI3K α ,-β ,-γ ,-δ, p38 α, p38 γ, Jnkl, Jnk2 etc., in some cases as the total length kinases, in some cases as the fragment of brachymemma---but form by the kinase function territory at least.(Proqinase is Upstate) as the recombination fusion protein with GST (glutathione S-transferase) mark or His mark with business-like kinase protein.According to the substrate type, by means of proper A LPHA ^TMPearl (PerkinElmer), quantitatively different kinase reactions.

Test

Be discussed in more detail below the substrate test of in the Erk test, carrying out.Quoted Erk2 below, the experimental result of the selection of PI3K α test.In order to measure IC ₅₀Value at 10 semilog gradient concentrations of 3.16nM-100 μ M, has been studied potential suppressor factor material.

A) Erk2-ALPHA: on 384-hole Optiplate (Perkin Elmer), at 25mM Tris, the 10mM MgCl of 15 μ l volumes ₂, 0.1% tween 20,100 μ M NaVO ₄, (0.625ng Erk2 (#14-173, Upstate), 10 μ M ATP and the biotinylated MBP of 15nM (MBP) substrate) 1h of incubation experiment material among the 2mM DTT pH 7.5.Then through adding 10 μ l ALPHA bead mixtures (10 μ g/ml; #6760617/PerkinElmer) stop kinase reaction; In 25mM Tris, 200mM NaCl, 100mM EDTA and 0.3% BSA, use anti--phosphoric acid MBP antibody (320pM; #05-429/Upstate) preincubation, and hold over night.

B) PI3K-ALPHA (for example PI3K α): on 384-hole Optiplate (PerkinElmer), at 50mM Hepes, 50mM NaCl, 5mM MgCl ₂, incubation experiment material among 0.05% Chaps, 5mM DTT pH 7.4 (1ng PI3K α (#14-602, Upstate), 100 μ M ATP and 20 μ M PIP ₂Substrate (#P4508, Echelon)) 1h.Then through adding ALPHA bead mixtures (10 μ g/ml; #6760603/PerkinElmer) stop kinase reaction; In 50mM Hepes, 50mM NaCl, 50mM EDTA and 0.1% BSA with 1nM GST:Grp1 fusion rotein (Upstate) and the biotinylated PIP3 of 15nM (#C-39B6/Echelon) preincubation, and hold over night.

Morning next day is at Fusion ^TMDetect fluorescence in the α device (Perkin Elmer).

Estimate

By means of following formula, from Fusion ^TMThe raw data that records among the α, calculate the % inhibiting value of every kind of material concentration:

Contrast is respectively measured 8 times, and material sample is respectively measured 2 times.0% contrast does not contain any ATP or any substrate; 100% contrast does not contain the experiment thing.Measure IC with GraphPadPrism ₅₀Value.

Compound of the present invention shows Erk, PI3K, effective inhibition of p38 α and Jnk1+Jnk2, IC ₅₀Value is up to 88nM (referring to table 1).

Table 1:MAPK and PI3K alpha kinase determination experiment result (IC50 [μ M] is at 10 μ M or 100 μ M*ATP)

Compound	Erk2	PI3Kα	p38α	Jnk1+Jnk2
					3	5.8	16.8	Not test	Not test
6	2.4	21.3	Not test	Not test
					7	0.407	27.9	＞100	11.4
8	4.1	27.2	＞100	19.4
					9	0.117	7.8	＞100	＞100
10	0.088	2.6	＞100	2.9
					11	0.27	＞31.6	＞100	＞100
12	2.8	3.4	8.8	0.637
					13	0.64	＞31.6	＞100	＞100
16	0.513	3.3	＞100	5.6
					17	0.167	11.8	＞100	＞100

19	3.9	2.3	＞100	10.1
					21	＞100	1.2	＞100	＞31.6
22	＞100	1.2	＞100	＞31.6
					23	1.9	1.3	＞100	5.7
25	3.4	4.4	＞100	24.2
					28	0.364	1.8	＞100	5
29	0.396	2.3	＞100	24.2
					30	＞31.6	0.749	＞100	13.8
32	0.824	1.3	＞100	4.2
					44	2.8	10.7	＞100	8.4
45	0.243	12.5	＞100	0.974
					48	＞100	1.1	＞100	＞31.6
49	9.6	1.9	4	＞31.6
					50	4.7	0.683	18.1	＞31.6
51	19.1	7.5	＞100	＞31.6
					53	16.5	0.677	＞100	20.4
55	0.812	3.6	＞100	2.9
					56	0.272	1.3	＞100	3.1
58	0.763	4.3	＞31.6	2.5
					61	0.3	1.5	＞100	2.1

II.2) test cell line: test antiproliferative effect (XTT test)

This experiment principle is based on mitochondrial dehydrogenase with tetrazolium dye XTT (3 '-[1-(phenyl amino carbonyl)-3; The 4-tetrazolium] two (4-methoxyl group-6-nitro) Supragil GN, Sigma) reduction in the cell of first

dyestuff.Dyestuff is only formed by the cell of metabolic activity; The measurable intensity of its photometer is the quantitative target that has viable cell.The minimizing that the dyestuff that causes with material incubation cell forms is as the parameter of antiproliferative effect.

Test

(for BxPC3 and Hct116, is 5000 cells/well with tumor cell line (ATCC) with the cell count of confirming; For MDA MB468, be 10000 cells/well) inoculate 96-hole microtiter plate, then at 37 ℃, 5% CO ₂With overnight cultures in the incubator of 95% atmospheric moisture.The experiment thing is formed in the stock solution (10mM) among the DMSO.In order to measure EC ₅₀Value adds cell with potential suppressor factor material with four times of logarithm gradient dilutions, thereby produces the final concentration of 0.28 μ M-50 μ M.Then at 37 ℃, 5% CO ₂With the dull and stereotyped 45h of culturing cell in the incubator of 95% atmospheric moisture.

For detection reaction, (N-methyldiphenyl and pyrazine methylsulfuric acid ester Sigma) mix, and add to cell, thereby produce the final concentration of 325 μ g XTT/ml and 2.5 μ g PMS/ml with XTT substrate and PMS.Then at 37 ℃, 95% atmospheric moisture incubation mixture.Subsequently; In the 490nm absorbancy, first salt that quantitative cell desaturase forms.

Estimate

By means of following formula, the value of the optical density(OD) of measuring at 490nm under every kind of situation, estimate the % inhibiting value:

Contrast is respectively measured 8 times, and material sample is respectively measured 2 times.0% contrast does not contain cell; 100% contrast does not contain the experiment material.Measure EC with GraphPadPrism ₅₀Value.

Compound of the present invention shows effective inhibition of on cell proliferation, in some cases, and EC ₅₀Value is up to 2.2 μ M (referring to table 2).

Table 2:XTT determination experiment result (EC ₅₀[μ M])

Compound	BxPC3	MDA-MB468	Hct116
				9	20	15	10
10	9	7	5
				16	＞25	11	11
17	＞25	＞25	3.4
				23	＞50	＞25	16
32	5.9	4.5	2.2
				49	Not test	16	About 20
56	＞20	15.5	9.4
				61	Not test	7.1	6

II.3) test cell line: measure substrate and suppress (western blotting)

Whether the kinase modulator that this method has been described research also can produce the effect of hoping under the cell background, in this case promptly, inspection is at the phosphorylation state of the substrate protein in target kinase downstream.For this reason, cracking separates total protein with the cell of material incubation on the reduction polyacrylamide gel.Subsequently,, albumen is transferred to pvdf membrane,, the substrate band of searching is manifested with specific antibody and suitable detection method by means of western blotting.Be used in specific resisting-phosphoric acid antibody and total antibody of discerning the substrate total protein under every kind of situation simultaneously, detect substrate protein in the target kinase downstream.The double technique of ODYSSEY imager (LiCOR) can be realized this and measure simultaneously.The intensity of total substrate band is used for stdn and quantitatively phosphorylation inhibition or activation.

Test

With the cell count confirmed (for example for BxPC3 and Hct116; 350000 cells/well); Suitable tumor cell line (for example BxPC3, Hct116 or MDA MB468) inoculation is advanced in the specific criteria perfect medium of 6-hole microtiter plate, then at 37 ℃, 5% CO ₂With overnight cultures in the incubator of 95% atmospheric moisture.Reducing under the serum condition then, promptly in defined medium, exception is that 0.25% serum is only arranged, further the other 24h of culturing cell.The experiment thing is formed in the stock solution (10mM) among the DMSO, at the final concentration culturing cell 5h of 5,15.8 and 50 μ M.Lysing cell in 25mM Tris, 150mM NaCl, 10mM trisodium phosphate, 2mMEGTA, 25mM β-glycerophosphate, 25mM NaF, 10% glycerine, 0.75% NP-40,100 μ M NaVO4 damping fluids subsequently.By means of BCA (two cinchonic acid albumen test kits, Sigma) test protein quantification after,

The protein content that separates the about 20 μ g of every swimming lane on the polyacrylamide gel is then by means of half-dried egg white trace, with 0.8mA/cm ²Transfer to pvdf membrane (Millipore) and go up 1h.Prehybridization film 1 hour in I-blocking-up reagent (AppliedBiosystems) is incubated overnight with specific antibody subsequently.Suppress in order to measure Erk and PI3K; With total antibody (Rsk #sc-231g C-21; Santa Cruz) and phosphoric acid antibody (phosphoric acid-p90RSK (S380) #9341, NEB Cell Signalling) detect following a kind of substrate Rsk1 in downstream, with total antibody (Akt1 #sc-1618 C-20; Santa Cruz) and phosphoric acid antibody (phosphoric acid-Akt (Ser 473) #9271, NEB Cell Signaling) detect Akt.Behind the washing film, (#611-732-127, Rockland) incubation SA (for phosphoric acid antibody) is with anti--goat Alexa Fluor 680 (#A-21081, Molecular samples) incubation SA (for total protein antibody) with anti--rabbit IR dyestuff 800.In the dark behind the incubation 30min,, on film, detect the hybridization of antibody in room temperature through scanning in ODYSSEY imager (LiCOR).

Estimate

In the concentration of 5-50 μ M, compound of the present invention shows the double inhibition (table 3) to Erk (MAPK1/2) and PI3K, the inhibition indication of the band strength of its phosphoric acid by 2 kinds of correspondences-substrate protein Rsk1 and Akt.

The inhibition of table 3 cell substrate phosphorylation (50 μ M)

Compound	Erk→ pRsk	PI3K→pAkt
			9	90％	50％
10	100％	100％
			23	0％	70％
32	100％	90％
			49	0％	90％

Abbreviation

Akt is from mouse Akt8 retrovirus or protein kinase B (PKB)

Ask1 apoptosis signal-adjusting kinases

The ATR ataxia telangiectasia is relevant with Rad3-

The sudden change of ATM ataxia telangiectasia

The athanogene-1 that Bag1 Bc1-2 is relevant

Bc1-2 B-cell white blood disease/lymphoma-2 gene

The dependent protein kinase of DNA-PK DNA-

The kinases of Erk extracellular signal-adjusting

Flt-3 fms appearance Tyrosylprotein kinase 3

The GSK-3 glycogen synthase kinase-3

People's orthogenesis homologue of the product of 7 kinds of nematode genes-1 of hSMG-1

JAK-3 Janus kinases 3

The terminal kinases of JNK c-jun N-

MAPK mitogen activated protein kinase

Mek MAP or Erk kinases

The mammalian target thing of mTOR rapamycin

The growth factor receptors that PDGFR is platelet-derived

The PI3K phosphoinositide 3-kinase

The kinases that the PIKK phosphoinositide 3-kinase is relevant

PIP ₂The phosphatidylinositol diphosphate ester

PIP ₃The PI triguaiacyl phosphate

The PtdIns PI

The fibrosarcoma that Raf quickens fast

Ras rat sarcoma

The RTK receptor tyrosine kinase

SAPK stress-the activated protein kinase

The Ser Serine

The Syk spleen tyrosine kinase

The Thr Threonine

Tyr tyrosine

The VEGFR vascular endothelial growth factor receptor

Claims

1. pyrido [2,3-b] pyrazines derivatives, it is selected from:

Compound 61-ethyl-3-[3-((E)-3-methoxy propyl thiazolinyl) pyrido [2,3-b] pyrazine-6-yl] urea

Compound 7

Compound 8

Compound 231-ethyl-3-{3-[4-(3-ethyl carbamide) phenyl] pyrido [2,3-b] pyrazine-6-yl } urea

Compound 481-ethyl-3-[3-(4-methane sulfonyl phenyl amino) pyrido [2,3-b]-pyrazine-6-yl] urea

Compound 61

2. medicine, it comprises at least a pyrido according to claim 1 [2,3-b] pyrazines derivatives.

3. produce method according to the medicine of claim 2; The method is characterized in that, process one or more pyridos [2,3-b] pyrazines derivatives according to claim 1 with pharmaceutically acceptable carrier and/or vehicle; Obtaining pharmaceutical prepn, but and process treatment and go up type of service.

4. pyrido [2, the 3-b] pyrazines derivatives according to claim 1 is used to produce the purposes of medicine, and said medicine is used to regulate the cell signalling process of misdirection.

5. according to the purposes of claim 4, said medicine is used to influence the receptor tyrosine kinase of activated and non-activity and the function of kytoplasm tyrosine, serine/threonine and lipid kinase.

6. according to the purposes of claim 5, said kinases is selected from c-Raf, B-Raf, Mek, MAPKs, PDGFR β, Flt-3, IGF1R, PI3K, PKB/Akt1, c-Kit, c-Abl, FGFR1 and KDR.

7. according to the pyrido [2 of claim 1; 3-b] pyrazines derivatives is used to produce the purposes of medicine; Said medicine is used for treatment or prevents mammiferous by being selected from: the physiology and/or the pathological and physiological condition of the signal transduction pathway mediation of " ras-Raf-Mek-Erk signal transduction pathway, PI3K-Akt signal transduction pathway and/or SAPK signal transduction pathway ".

8. according to the purposes of claim 7, wherein said treatment or prevention realize through the signal transduction pathway that adjusting is selected from " ras-Raf-Mek-Erk signal transduction pathway, PI3K-Akt signal transduction pathway and/or SAPK signal transduction pathway ".

9. according to the purposes of claim 7, wherein said physiology and/or pathological and physiological condition are by the enzyme mediation that is selected from " ATM, ATR, mTOR, DNA-PK, hSMG-1 ".

10. according to the purposes of claim 7, wherein said treatment or prevention are selected from following enzyme and realize through regulating one or more: " ATM, ATR, mTOR, DNA-PK, hSMG-1 ".

11. according to the purposes of claim 7, the signal transduction pathway of wherein said mediation and/or adjusting is ras-Raf-Mek-Erk signal transduction pathway and PI3K-Akt signal transduction pathway.

12. according to the purposes of claim 7, the signal transduction pathway of wherein said mediation and/or adjusting is the ras-Raf-Mek-Erk signal transduction pathway.

13. according to the purposes of claim 7, the signal transduction pathway of wherein said mediation and/or adjusting is the PI3K-Akt signal transduction pathway.

14. according to the purposes of claim 7, the signal transduction pathway of wherein said mediation and/or adjusting is SAPK signal transduction pathway and PI3K-Akt signal transduction pathway.

15. according to the purposes of claim 7, the signal transduction pathway of wherein said mediation and/or adjusting is the SAPK signal transduction pathway.

16. purposes according to claim 7; Wherein the adjusting of ras-Raf-Mek-Erk signal transduction pathway is selected from following enzyme and realizes through regulating one or more: " Tyrosylprotein kinase; serine/threonine kinase; acceptor-Tyrosylprotein kinase, cytoplasmic tyrosine kinase, kytoplasm serine/threonine kinase ".

17. according to the purposes of claim 16, wherein said enzyme is selected from: " Erk, Erk1, Erk2 ".

18. according to the purposes of claim 7, wherein the adjusting of PI3K-Akt signal transduction pathway is selected from following enzyme and realizes through regulating one or more: " PI3K, PI3K α; PI3K β, PI3K γ, PI3K; PI3K-C2 α, PI3K-C2 β, PI3K-Vps34p ".

19. purposes according to claim 7; Wherein the adjusting of SAPK signal transduction pathway is selected from following enzyme and realizes through regulating one or more: " Tyrosylprotein kinase, serine/threonine kinase, acceptor-Tyrosylprotein kinase; cytoplasmic tyrosine kinase, kytoplasm serine/threonine kinase ".

20. according to the purposes of claim 19, wherein said enzyme is selected from: " Jnk, Jnk1, Jnk2, Jnk 3, p38, p38 α, p38 β, p38 γ, p38 δ ".

21., wherein regulate 2 kinds or more kinds of enzyme according to each purposes of claim 4-7.

22. according to the purposes of claim 21, wherein at least a enzyme is selected from: " Erk, Erk1, Erk2 ", and at least a enzyme is selected from: " PI3K, PI3K α, PI3K β, PI3K γ, PI3K δ, PI3K-C2 α, PI3K-C2 β, PI3K-Vps34p ".

23. according to the purposes of claim 21, wherein at least a enzyme is selected from: " Jnk, Jnk1, Jnk2, Jnk3; p38, p38 α, p38 β, p38 γ, p38 δ "; And at least a enzyme is selected from: " PI3K, PI3K α, PI3K β, PI3K γ; PI3K δ, PI3K-C2 α, PI3K-C2 β, PI3K-Vps34p ".

24. according to the purposes of claim 21, wherein at least a enzyme is selected from: " Erk, Erk1, Erk2 ", and at least a enzyme is selected from: " ATM, ATR, mTOR, DNA-PK, hSMG-1 ".

25. according to the purposes of claim 21, wherein at least a enzyme is selected from: " Jnk, Jnk1, Jnk2, Jnk3, p38, p38 α, p38 β, p38 γ, p38 δ ", and at least a enzyme is selected from: " ATM, ATR, mTOR, DNA-PK, hSMG-1 ".

26. according to the purposes of claim 21, wherein at least a enzyme is selected from: " PI3K, PI3K α, PI3K β, PI3K γ; PI3K δ, PI3K-C2 α, PI3K-C2 β, PI3K-Vps34p ", and at least a enzyme is selected from: " ATM; ATR, mTOR, DNA-PK, hSMG-1 ".

27. according to each purposes of claim 4-7, wherein said adjusting is to suppress.

28. according to the purposes of claim 7, wherein said Mammals is selected from: " people, domestic animal, cavy, hamster, rat, mouse ".

29. according to the purposes of claim 28, wherein said Mammals is behaved.

30. according to the purposes of claim 7, wherein said physiology and/or pathological and physiological condition are selected from: " malignant tumour, innocent tumour, inflammatory disorder, inflammation, pain, rheumatosis, arthritis, HIV infects; neuroscience or neurodegenerative disorders, rheumatosis, sacroiliitis, AIDS, the AIDS complex of being correlated with, Kaposi sarcoma is derived from the tumour of brain and/or neural system and/or meninx, dementia, Alzheimer; excess proliferative disease, psoriatic, endometriosis, cicatrization, benign prostatic hyperplasia, disorder of immune system, autoimmune disease, immune deficiency disorder, colon tumor; gastric tumor, intestinal tumor, lung tumor, pancreas struma, ovarian tumor, prostate tumor, white blood disease, melanoma, liver tumor; tumor of kidney, a tumour, laryngeal neoplasm, neurospongioma, mastoncus, uterus carcinoma, carcinoma of endometrium, cervical cancer, cerebral tumor; gland cancer, bladder cancer, gastric tumor, colorectum tumour, the esophageal carcinoma, gynecological tumor, ovarian tumor, thyroid carcinoma, lymphoma; Chronic leukemia, acute leukemia, restenosis, mellitus, diabetic nephropathy, fibrotic conditions, cystic fibrosis, malignant nephrosclerosis, thrombotic microangiopathy syndrome; The organ-graft refection, glomerulopathy, metabolic disease, solid tumor, rheumatic arthritis, diabetic retinopathy, asthma, transformation reactions, allergic disorder; Chronic obstructive pulmonary disease, inflammatory bowel, fibrosis, atherosclerosis, heart trouble, cardiovascular diseases, myocardosis, vascular disorder, blood vessel originality illness; Ephrosis, rhinitis, Graves disease, local asphyxia, heart failure, ischemic, cardiac hypertrophy, renal failure, myocardial cell's dysfunction; Hypertension, vasoconstriction, apoplexy, anaphylactic shock, platelet aggregation, skeletal muscle atrophy, obesity is overweight; The glucose homeostasis, congestive heart failure, stenocardia, heart attack, myocardial infarction, hyperglycemia, hypoglycemia, hypertension ".

31. according to the purposes of claim 7, wherein said medicine is before with radiotherapy and/or operative treatment and/or in the process and/or use afterwards.

32. pharmaceutical composition, it comprises at least a pyrido according to claim 1 [2, the 3-b] pyrazines derivatives of pharmacologically active amount.

33. according to the pharmaceutical composition of claim 32, wherein said activeconstituents exists with the unitary dose of 0.001mg-100mg/kg weight in patients.

34. according to each pharmaceutical composition of claim 32-33, wherein said compsn also comprises the carrier and/or the vehicle of at least a pharmacy tolerance.