TWI322688B - Pyrazole compounds and antidiabetics comprising the pyrazole compounds - Google Patents

Description

IX. Description of the invention: • Technical field to which the invention pertains. The present invention relates to a pharmaceutical composition for treating or preventing diabetes, comprising a pyrazole compound having a hepatic phosphatase inhibitory activity and a pharmaceutically acceptable carrier The present invention also relates to a novel pyrazole compound having such hepatic phosphatase inhibitory activity, and a pharmaceutical composition comprising the same for treating or preventing diabetes and another agent (for example, an antihyperlipidemic agent, an obesity treatment or prophylactic agent, diabetes) A pharmaceutical composition of a combination of a therapeutic agent, a therapeutic agent for diabetic complications, or an anti-hypertension agent. [Prior Art] Diabetes is a chronic disease caused by abnormal metabolism of glucose, lipids and amino acids due to loss of insulin action. If diabetes is not treated, it can cause hyperglycemia and glycosuria. Diabetes is classified as type 1 diabetes (insulin-dependent diabetes mellitus, IDDM), which is characterized by the destruction of small island cells caused by autoantibodies in the pancreatic islets, causing hypocholesterol secretion; and type II diabetes ( Non-insulin-dependent diabetes mellitus; NIDM) is a disease caused by insulin secretion dysfunction of the pancreas and insulin resistance of peripheral tissues such as muscle tissue and the liver. Insulin-dependent diabetes mellitus may cause ketosis and acidosis due to the loss of tensin-secreting ability, and if untreated, it may become diabetic coma. Treatment with diet or oral hypoglycaemic agents is ineffective and effective only with insulin. On the other hand, non-Tengol-dependent diabetes mellitus (8) surface only causes a very low degree of _ septicemia and acid sputum 4 denier effect is lower than normal, and it is not always necessary to use 318197 6 1322688 sin. About 90% to 95% of diabetes is a non-insulin-dependent type of diabetes. 0 Diabetes due to long-term hyperglycemia may cause complications such as neuropathy, retinopathy, and microvascular disease of the kidney, which may further lead to fatal diseases such as coronary artery disease and stroke. complication. Hypoglycemic agents currently used to treat hyperglycemia include insulin preparations, sulfonylurea preparations (eg, glibenclamide, tolbutamide), biguanides (eg, metfom (metf〇) Rmin)) e, an insulin resistance improving agent (for example, pi〇gl i taz〇ne) and an alpha glucosidase inhibitor (for example, arabinose). Insulin preparations for insulin-dependent diabetes do reduce blood sugar levels, but insulin preparations must be administered by injection and may cause hypoglycemia. _ Both urea preparations can stimulate the spleen cells and promote the secretion of endogenous sputum from pancreatic cells. However, the secretion time and secretion of insulin are determined by the time of administration or dosage, rather than the concentration of sugar. . & Fruits often cause side effects of hypoglycemia due to long-term drug action. In addition, ° may have digestive symptoms such as anorexia. Sulfaquine formulations are contraindicated in patients with severe ketone poisoning or liver and kidney dysfunction. Double: The class does not stimulate the sputum cells, and it can cause hypoglycemia in healthy people or diabetic patients. Possible mode of action for biguanides: Straw: Oxygen vinegar solution (glycoly_ increases glucose utilization, gluec neGgenesis), and inhibits intestinal absorption of sugar. A possible side effect of biguanides is that lactic acidosis is more serious. 318197 7 1322688 The thiazole bite derivative contained in the insulin resistance improver (insulin sensitizer) enhances insulin action, does not stimulate insulin secretion, activates insulin receptor kinase, promotes glucose absorption from peripheral tissues, and improves liver Increase in the manufacture of liver glucose. The known side effects of thiazolidine derivatives include digestive symptoms and edema, including red blood cell count, hematocrit and hemoglobin reduction, and LDH alpha-glucosidase-giucosidase inhibitors via delayed carbohydrates. Digestion/absorption of the digestive tract, while preventing an increase in postprandial blood glucose concentration, but may cause side effects such as bloating, belching or diarrhea (see, for example, Non-Patent Document 1). Therefore, these drugs require a hypoglycemic agent with novel effects due to side effects and use of non-responsive patients. Recently, NIDDM patients reported an increase in glucose released from the liver during fasting compared to normal subjects. The report suggests that glucose released from the liver may become a target for medical treatment of spring NIDDM. According to recent findings of diabetes, pancreatic dysfunction of cells and increased glucose release from the liver may involve the occurrence and severity of diabetes (see, for example, Non-Patent Document 2). Glucose released from the liver is expressed as the sum of two pathways, namely the breakdown of glycogen and the regeneration of glucose. In diabetes, the hepatic glycolysis system is enhanced (see, for example, Non-Patent Documents 3 and 4). Further, the blood glucose concentration is lowered by a diabetic animal which inhibits the decomposition of hepatic sugar or a normal person who is stimulated by glucagon (for example, refer to Non-Patent Document 5). These findings suggest that hepatic glycolysis is enhanced by 318197 8 1322688 and diabetes. On the other hand, it is known that this hepatic saccharide decomposition is caused by hepatic phosphatase catalyzed 'hepatic hearing (n glucose units) by phosphorolysis degradation results in the formation of glucosamine 1-acid (G-1- P) and liver vinegar (glycogen) (n-1 glucose units). Therefore, an anti-diabetic agent with a novel mechanism of action has been developed, which has the effect of inhibiting hepatic phosphatase. The hepatic phosphatase system is significantly involved in the hepatic syrup solution but has not yet found an anti-diabetic agent with satisfactory activity. . In addition, several hepatic glycoproteinase inhibitors have been reported to have various effects and are effective therapeutic or prophylactic agents for diabetes. For example, a compound having hepatic phosphatase inhibitory activity can be treated with ash for "diabetes, insulin resistance, diabetic neuropathy, diabetic nephropathy, diabetic retinopathy, cataract, hyperglycemia, hypercholesterolemia, high Blood pressure, hyperinsulinemia, hyperlipidemia, atherosclerosis, tissue ischemia, and myocardial ischemia" (for example, refer to Patent Document 1).

In addition, a compound having hepatic-acidase inhibitory activity can be effectively used as a therapeutic agent for the treatment of obesity, and is effective for treating or preventing a decrease in blood concentration, such as dyslipidemia, high triglyceride. :=. Hyperlipoproteinemia, cardiovascular disease, and hypertensive inhibitors are effective in the treatment and prevention of diseases associated with metabolism, such as diabetes, especially urinary diseases, including long-term complications (such as retinopathy glycosemia, nephropathy, and microvessels). Diseases and macrovascular diseases) (eg, Ref.::: 318197 9 1322688) In addition, the human isoforms of the three hepatic phosphatases have been identified, namely, hepatic homomorphisms, muscle homomorphisms and The brain isogenic isoforms. This isoform is a product of three different genes, with 80 to 83% amino acid homology. Hepatic phosphatase is also present in bacteria, a compound with hepatic phosphatase inhibitory activity. It can provide treatment and prevention means for infections such as bacterial infections, fungal infections, parasitic infections or viral infections' and can be effectively used for the treatment and prevention of such infections (for example, refer to Patent Document 4). Enzyme inhibitors can be used to treat and prevent diabetes, and are also expected to act as insulin resistance, diabetic neuropathy, diabetic nephropathy, diabetes Retinopathy, cataract, hypercholesterolemia, hypertension, hyperinsulinemia, hyperlipidemia, atherosclerosis, tissue ischemia and myocardial ischemia; and as a therapeutic agent for appetite control and obesity, and A therapeutic agent for infection such as a bacterial, fungal, parasitic or viral infection. The following compounds are known as hepatic glycophosphatase inhibitors of the liver, or compounds having a structural formula quite similar to the compounds of the present invention. W096/39384C International Patent The national publication of the application No. PCT No. PCT No. 1687 discloses a ruthenium compound having no hepatic phosphatase inhibitor activity (refer to Patent Document 5). 318197

In the formula, 'I is a phenylalkyl group, Rs is a hydrogen group, and R2 is a hydrogen atom, and R1, RlQ, and Ru are each divided into a group of a few oxygen atoms, etc., and 4 is a hydrogen atom, and A is H is a wind atom, and a dentogen is exemplified. The following compounds are disclosed as specific compounds.

W001(10)GGM discloses a thiol-derived gland derivative represented by the following formula (1) which is effective for (d) treatment of π-type diabetes, and a patent document 6) thereof. Skillful

(I) In the formula, Α represents a phenyl or naphthyl group which may be substituted with various substituents, and R1 and R2 represent a hydrogen atom, an alkyl group, etc., and a hydrogen atom, a halogen atom, etc. 'X represents an oxygen atom or The sulfur atom, and R7 represents an alkyl group substituted with a carboxy 11 318197 1322688 group, a strepyl or a heterocyclic group, and the like. W002/096864A1 discloses a benzoguanidine-substituted phenylurea derivative represented by the following formula (I) which is effective for the treatment of type 2 diabetes, and a method for producing the same (refer to Patent Document 7)

In the formula, A represents a phenyl or naphthyl group which may be substituted with various substituents, R1 and R2 represent a hydrogen atom, an alkyl group, etc., R3, R4, R5 and R6 represent a hydrogen atom = a tooth atom, etc., and R7 represents a hydrogen atom. And an alkyl group, etc., R8 represents a hydrogen atom, a substituted or unsubstituted alkyl group, etc., and R9 represents a tooth atom. WO 03/015774 A1 discloses a derivative represented by the following formula (1) for treating a disease caused by glucokinase (GLK) such as a π-type diabetes (refer to Patent Document 8).

= 0, U2'n is 〇, Bu, 2, 3 or 4, ... is greater than (2) independently, can be replaced by c, _6 alkyl, 3 a Fa, halogen, Ch alkyl, phenyl, heterocyclic ring, etc. ; f is a bond of n, a direct bond, etc.; Z is a direct bond, a & 6 is an extension of 318197 12; Y is an aryl {, heterocyclic ring substituted by R7. The group - z_, Cl-6 alkyl group, etc.; and R is pharmaceutically acceptable. 1. The exemplified by the following examples of the compounds of the examples gg2 and 5, as a special case of the compound of the salivary trunk.

As the essay document, the compound represented by the following formula (Ib) is also disclosed in the specification.

In the main formula, R1 is a hydroxyl group, a hydroxyalkyl group, a fluorinated alkyl group, a tooth atom, an alkane 318197 13 1322688 gas group, a burnt group, etc.; R2 is a -Χ-γ, wherein χ is _〇_Z_, etc.; Is an aryl group or the like; and R2 does not contain a halogen atom or an alkyl group; 10 is ruthenium, 1 or 2, n is ι, 2 or 3, and m+n is 2 or 3. It is apparent from the foregoing that m is at most 2, and the stupid base has not been replaced by three tooth atoms at the same time. W003/084922A1 discloses a mercapto-4-carboxyphenylurea derivative represented by the following formula which can be used as an antidiabetic agent (refer to Patent Document 9). R4 Ο

The mR9 and the cut are identical or different and each other has a table atom, a _ atom, an alkoxy group, etc.; R1*R2 represents a hydrogen atom, a halogen atom, a hydrogen atom, a (tetra), a phenoxy group, a phenyl group, a phenyl group R5 represents a gas atom, a cardinal; oxygen: a primary alkyl group, and R6 represents a hydrogen atom, a halogen atom, a stupid oxy group, a burnt soil W〇G3/G8 side A1_ can be (iv) an anti-diabetic society such as earth The fluorenyl-3-carboxyphenylurea derivative represented by the formula () refers to Patent Document 1 叼. " 318197 14 1322688

The shirts M are K1Us which are the same or different from each other and have a halogen atom, a halogen atom, an alkoxy group, etc., etc. 13 represents a hydrogen atom, a tooth, a * atom, a nitro group, a phenoxy group, etc. R5: an oxygen group; Represents a hydrogen atom, a sheet η. a non-deuterium atom, a south atom, a benzene soil, and R6 represents a hydrogen atom, a tooth atom, a phenoxy group, a hospital base, etc. W0〇3/10 side A1 reveals that it can be used as an antidiabetic agent. The N-benzhydrylureido cinnamic acid ester derivative represented by 9 (I) is as follows (Reference Patent 0

R11 In the formula, R7, R8, R9 and R10 are the same or different from each other and represent a wind atom, 4 atom, a methoxy group, etc.; R1 and a hydrogen atom, a hospital group, etc., R3H R5 and R6 represent a hydrogen atom. , a tooth atom, a thiol group, etc.; and R11 represents -0R12 or -N(R18)(R19). 318197 15 ^22688 W02GQ4/Hidden 55A1# can be used as the (10) diabetes agent as shown in the formula (1), which is substituted by a heterocyclic aryl group.

R4 矣 in Ϊ 'R1 and R2 represent a hydrogen atom, an alkyl group, an amine group, etc.; the ruler 3 and: represent an i atom, a thiol group, an alkyl group, an alkoxy group, etc.; R5 represents a hydrogen atom, an atom, a thiol group, A base or the like; A represents a hydrogen atom, a tooth atom, a burnt group, a pit base, etc., and A Het represents a hetero group such as a triple saliva, a tetrasigma or a (tetra). The next pass l〇^i/G3341 _ reveals that as a type 11 diabetes agent, such as 4 = di-n-oxide substituted fermented Wei derivative (see

Sub 318197 丄 322688 and η represent integers from 1 to 8. WO2004/065356A1 discloses a mercaptophenylurea derivative substituted with a carbonylamino group represented by the following formula (I) which can be used as a U-type diabetes agent (refer to Patent Document 14). > R4

R10 R11 In the formula, '8, 1? 9, 1^10 and 1^1 represent a hydrogen atom, a tooth atom, a hydroxyl group, a nitro group, an alkoxy group, etc.; R1 and R2 represent a hydrogen atom, substituted or unsubstituted The alkyl group, the alkoxy group and the like; the R3, R4 and the hydrazine group represent a hydrogen atom, a halogen atom, a nitro group, a phenoxy group, a hydroxyl group or the like; and R7 represents a hydrogen atom, an alkyl group or a cycloalkyl group. It has also been reported that the η has a substituent of the amine and the salic compound. For example, WO2004/098589A1 discloses a pyrazole compound represented by the following formula (I) or (η) 4-bromo-5-(2-chloro-benzhydrylamino)_1^-pyrazole-3-carboxylate A decylamine derivative. However, these compounds are bradykinir OB! receptor antagonists (see Patent Document 15) for the treatment of inflammatory diseases. 318197 17

丄JZZOOO

〇, s or NH; Q represents n(r4)(r5), 〇h, 2 n is not 11 atoms, a substituent, a substituted group, an aryl group, a 2 group, a heterocyclic group, a substituted Heterocyclic group, etc.; R3 means Yan

==, substituted alkyl, aryl, etc.; R4 and R5 represent a nitrogen atom, a terpenes, an alkyl group, an alkoxy group, a cycloalkyl group, a substituted cycloalkyl group, a heterocyclic group, a substituted heterocyclic group or the like; and χ represents a hydrogen atom, an _alkyl group or the like. Further, in page 333 of the specification, a plurality of substituents are disclosed, including 2-phenylphenyl, 2-fluorophenyl, 2-phenylphenyl, 2-canylphenyl, and the like, more particularly 2, [Dihydrophenyl and 3'4,5-trifluorophenyl, as a special case of r1. However, according to the description on page 17 of the patent specification, the preferred r1 group is 2-chlorophenyl, 2-fluorophenyl, 2-(quinolin-8-yl)-phenyl, or 2_[(3_曱). • Benzyl-1-ylthio)methyl]phenyl-1-yl group without specifically specifying or even mentioning 2-chloro-4,5-difluorophenyl, 4,5-difluoro-2-methyl Phenyl, & 4_dichloro-5 monofluorophenyl. 1. In the foregoing documents, the following compounds are disclosed as examples of derivatives; but the main features of the specific compounds including the examples described herein are characterized by having 2 318197 18 chloro-phenyl groups as R1, and pyrazole substituents, The case name of the case ""=t or the base of the institute base" Η 咐 咐 衍生 衍生 derivative 2 (2: "bristamine 4 gentleman 4 king" is clearly known. In addition, it is available with ^ system For the treatment of inflamed bradykinin & receptor, but different from diabetes 0 Example 2

Example 7 318197 19 1322688

Example 16

Example 20

Example 33 20 318197 1322688

Example 34

Example 79

Example 93

Example 121 21 318197 fe)

Temple 4/〇9859〇A1 reveals a compound that can be used as a therapeutic inflammatory agent; it is an antagonist of the body (refer to the patent a Μ & amp ^ ^ AU / ^ AL.). But this case is especially about the specific pyrene

It is easy to know, such as by its A, 1H L 八月月名4-bromo-5-(2-chloro-benzylideneamine tertsite sitting -3 A sulphuric acid (1 monoamino)diethyl hydrazide derivative.

R7 R1 represents a hydrogen atom, a substituted or unsubstituted alkyl group, a substituted or unsubstituted aryl group, etc.; R2 and R4 represent a hydrogen atom, substituted or unsubstituted 22 318197 1322688 dynasty, R Table is not a gas atom, you -A> 4-, Tintin, substituted or unsubstituted alkyl, substituted or unsubstituted aryl, etc.; Rule 5 and |?6矣>& K夂K represents an atom; an amino acid branch; etc.; and R7 represents -NRbRc, -〇Rb, and the like. The following compounds are also disclosed as examples of the aforementioned derivatives. Example 1

W02004/099155A2 discloses a substituted organism represented by the following general formula (1) or ((1), which can be used as a stimulating B1 receptor antagonist for treating an inflammatory disease (refer to Patent Document 17).

0)

Wherein Z represents o, MNH; R1 represents a gas atom, a pyridyl group, a substituted aryl group, an aryl group substituted aryl group, etc.; R2 represents a hydrogen atom, a leuko group, a substituted alkyl group, etc.; and R3 represents hydrogen. "Sub, rolled atomic alkyl, substituted alkyl, square, substituted aryl, etc.; R4 table thousand - K-formed unsubstituted, substituted aryl, hetero- or substituted And the like; R5 represents an atom of an atom, an alkyl group or an alkyl group substituted by 318197 23 1322688; and X represents a hydrogen atom, a substituted or unsubstituted alkyl group, and the like. The following compounds are disclosed as examples of the aforementioned derivatives. Example 2

24 318197 1322688 W02004/072060A1 discloses a 3-(benzolic-glycosyl)-porphin derivative which can be used for the treatment and prevention of type 2 diabetes (refer to Patent Document 18).

R5sn^^xci . where R25 represents F, C1 or Br; R1 represents a hydrogen atom, F, C1, or Br; R2 represents a hydrogen atom, F, Cl, Br, alkyl, etc.; R3 represents a hydrogen atom, an alkane And the like; and R4 represents a hydrogen atom, a burnt group or the like. W02004/078743 A1 discloses substituted phenylmercaptopyridyl-piperidiine and - which are useful for the treatment and prevention of type 2 diabetes. A pyrrolidinecarboxylic acid derivative (refer to Patent Document 19).

In the formula, R1 and R2 represent a hydrogen atom, F or Cl; x represents 〇H, NH2. 虱 虱, etc.; AmE represents 〇ι or 2 [Non-Patent Document 1] JOLSLIN'S Diabetes 苐 13 Edition, 52 卜 52 Page 318197 25 1322688 [Non-Patent Document 2] Withers DJ, Endocrinology 141; 1917-1921 [Non-Patent Document 3] Tayek JA, Am. J. Physiol. 270; E709-E717, 1996 [Non-Patent Document 4] Diraison F., Diabetes 41; 212-220, 1998 [Non-Patent Document 5] William H. Martin, Proc. Natl. Acad. Sci. USA 95; 1776-1781, 1998, Judith L., ® ADA 61 Abstract of the scientific conference [Patent Document 1] 专利 Patent Publication No. 2004-00231 1 [Patent Document 2] International Patent Application No. 2002-53641 No. 0 [International Patent Application No. 2002] International Patent Application No. 2002 [National Patent Publication No. 515,064] [Patent Document 4] PCT Patent Publication No. 20 (Π-247565 φ [Patent Document 5] W096/39384C International Patent Application No. 1998-51 1687 [Patent Document 6] W001/94300A1 [Patent Document 7] W002/096864A1 [Patent Document 8] W003/015774A1 [Patent Document 9] W003/08492 2A1 [Patent Document 10] W003/084923A1 [Patent Document 11] W003/104188A1 [Patent Document 12] W02004/007455A1 26 318197 1322688 [Patent Document 13] W02004/033416A2 [Patent Document 14] W02004/065356A1 [Patent Document 15] W02004 [098 file A1] [Patent Document 16] W02004/098590A1 [Patent Document 17] W02004/099155A2 [Patent Document 18] W02004/072060A1 [Patent Document 19] W02004/078743A1 [Disclosed] Φ Invention The problem to be solved by the invention Diabetes is used in the pancreas (promotes insulin secretion), peripheral (improves insulin resistance), small intestine (inhibition of glucose absorption), and insulin itself. However, in recent years, it is necessary to develop anti-diabetic agents based on novel modes of action. The development of diabetes agents for hepatic glucoamylase is striking. However, no drug has been developed to any satisfactory activity. No drugs have been developed to meet the g requirements for oral absorption and metabolic stability. Therefore, it is required to develop a hepatic phosphatase inhibitor which has potent activity and less side effects than conventional anti-diabetic agents, and which is excellent in oral absorption and metabolic stability. The object of the present invention is to provide a hepatic phosphatase inhibitor which has potent activity and less side effects than conventional anti-diabetic agents, and oral absorption and metabolic stability. Another object of the present invention is to provide insulin resistance, diabetic neuropathy, diabetic nephropathy, diabetic retinopathy, intrathecal 27 318197 f, hypercholesterolemia, hypertension, hypertonic acidemia, hyperlipidemia Disease, atherosclerosis, (4) H (four) for ischemia and money ischemia; therapeutic control for appetite _/, obesity; and therapeutic agents for infections such as bacterial, fungal, parasitic, t-virus infections' Wherein the therapeutic agent contains a hepatic phosphatase inhibitor as an active ingredient. Means for Solving the Problem In view of the foregoing problems, intensive research has been conducted to find a useful anti-diabetic agent having liver vinegar activity, and as a result, it has been found that the pyrazole compound represented by the following formula (I) has strong hepatic glycophosphatase inhibition. active. The present invention is more particularly described in the following items 1 to 57. A pharmaceutical composition for the treatment or rib diabetes comprising a pyrazole compound of the following formula (I) or a pharmaceutically acceptable salt thereof, and a medically acceptable carrier:

Wherein ring Q represents an aryl or heteroaromatic group; 'there is a hydrogen atom, a halogen atom, a Cl 6 alkyl group or a Ci 6 alkoxy group; R: represents a tooth atom, a Ci 6 courtyard group, a & oxy group or azide a radical, a radical, a Ci6 alkyl group, a dentate base, an alkoxy group, a nitrogen-based 5-amino group, an oligoamino group or a Cl-6 alkyl group; the R4 and R5 are the same or Distinct and represents (1) a hydrogen atom; 28 31819? 1322688 (2) Ch hospital base can be substituted by one or more substituents selected from group A below.

[Group A] A1. hydroxy, A2.C!-6 alkoxy, A3. -N(R41)(r4丨.), wherein R41 and R41' are the same or different and represent a hydrogen atom or a Ci_6 alkyl group. Or R41 and R41 may form a saturated 5-membered monocyclic heterocycle together with an adjacent nitrogen atom, /A4.aryl, A5.heteroaryl, A6.-C0-N(R411)(R411'), wherein R411 And R411' are the same or different and represent a hydrogen atom or a Cl_6 alkyl group; or R411 and R4" may together form a saturated 5 member or an e member monocyclic heterocycle, A7. a group, and A8 together with an adjacent nitrogen atom. Ci-6 oxyl'' (3) C2-6 dilute; (4) C2-6 alkynyl; (5) C3-8 cycloalkyl; wherein the ring may be via a base, a carboxyl group or a Cl -e methoxyl group substituted, or condensable with a pyridine ring, (6) C3-8 cycloalkyl C1-6 alkyl, 318197 29 1322688 wherein the C3-8 cycloalkyl Cm alkyl cycloalkyl group Substituted by a hydroxyl group, a carboxyl group or a Ci | alkoxy group, or may be condensed with n to a bite ring, (7) a saturated 5 member or 6 membered monocyclic heterocyclic group may be selected from one or more of the following group c Substituent substitution: [C group] C1 · Cl-6 alkyl, C2. sulfhydryl, C 3 · C1 - 6 dazzle! , C4. Carboxyl, C5. Ch alkoxycarbonyl, C6. -CO-(Alk)n-COOR52, wherein P is a hydrogen atom or a Cl_6 ndyl group; Alk is a c-alkyl group, and η is 0 or 1 An integer of up to 3, substituted with one or more substituents

(8) an aryl group which may be selected from the group [D group] D1. vial, D2. Ci-6 alkoxy group, D3. cyano group, D4. Ch alkyl group, wherein the Cm alkyl group can be selected. Free hydroxyl, ^ ^ ^ , m storm and C a 6 alkoxycarbonyl, and substituted by one or more substituents of the group, D5. -N(R53)CR53 ), wherein R53 and R53' Is identical or different to each other and represents a hydrogen atom, Cl-6 318197 30 1322688 alkyl or Cl-6 alkyl, D6. -CO-N(R531)(R531'), wherein R531 and R531 are each other The same or different and represents a hydrogen atom, a hydrazine-based group or a Cl-6-based base, D7. -COOR54, wherein R is a hydrogen atom, C!-6 alkyl group, Cm alkylcarbonyloxy Ci6 alkyl group Or C3-8i smoldering oxyoxyl Cl-6 cyclyl, D8·-C(NH(OH))=N-R55, wherein R5 is a hydrogen atom or a Ci-e thiol group, D9. 5 or 6 membered monocyclic heterocyclic groups, and D 10. 5 or 6 membered monocyclic heteroaryl groups which may be substituted by keto or thioketo groups, ^5 members or 6 S mono(10)heteroaryl groups or 5 or 6 members of the benzene ring, 'Women's heteroaromatic group', wherein the 56-shell heteroaryl group may be selected from a group of a group and a C" alkoxy group Substituting one or more substituents of the constituent group; 〇〇) C7-lfl aralkyl; wherein the alkyl portion of the 4-arylalkyl group may be substituted with one or two substituents selected from Group E below. And the aryl moiety can be substituted with one or more substituents selected from Group F below. [Group E]

El· Ci-e can be substituted by a radical, E2. cyano, 318197 31 1322688 E3. carboxy, E4. Ci-6 alkoxycarbonyl, and E5. phenyl, [Group F] F1. Ci- 6 alkyl group, F2. halogen atom, F3. cyano group, F4. thiol group, F5. Cm alkoxy group which may be substituted by one or more substituents selected from the group consisting of a carboxyl group and a Cl_6 alkoxycarbonyl group. , F6. HaloCh alkyl, F7.carboxyl, F8. Cm alkoxycarbonyl, F9. -C0-N(R56a)(R56a), wherein R56aA are broadly identical or different from each other and represent a gas atom, containing to: a saturated 5-membered or 6-membered monocyclic heterocyclic group of a nitrogen atom, or a dialkyl-8 may be substituted with a diamine group, one or more substituents selected from the following group f, f 2. - Cl-6 Amino group, f3. di-Cm alkylamino group, carboxyl group,

Ci-6 alkoxycarbonyl, 318197 32 and f 7. a saturated 5- or 6-membered monocyclic heterocyclic group having at least one nitrogen atom, F10. -CO-N(R56b)(R56b), wherein R56b and R56b' One or the same or different from each other, which is the same or different and represents a hydrogen atom, a Cl_6 alkyl group which may be substituted with an imine group, and an aralkyl group which may be selected from the group consisting of an imido group and a halogen atom. a substituent substituted, an aryl fluorenyl group which may be via a Cl-e alkyl group, a Ci ealkyl sulfonyl group, a fluorenyl group, an amine fluorenyl group, a C 1-6 alkyl amide fluorenyl group or a di Ci -ealkylaminomethylindenyl,

Fll. -N=CR57(-N(R58)(r58,)), wherein R57 is a hydrogen atom or a Cl_6 alkyl group, and r58 and r58 are the same or different from each other and represent a hydrogen atom or a Cl-6 alkyl group, F12 5 or 6 members of a monocyclic heteroaryl group, and a methylenedioxy or ethylenedioxy group, F13, or a 6 membered monocyclic heteroaryl group and a member formed with a stupid ring or " a Ci_6 alkyl group substituted with the same or different substituents of the group consisting of heteroaromatic groups; wherein the heteroaromatic or condensed heteroaromatic group may be selected from one or more of the following Substituents substituted: ,, and [G group] 318197 33 1322688

Gl. Ci-e alkyl which may be substituted by one or more substituents selected from the group consisting of g group [g group] g 1. halogen atom, g2. amine group, — Cl-6 alkylamino group, g4· DiCl-6 alkylamino, 奵·Ch alkoxycarbonylamino, ® and hydroxyimino, G2. Halogen, G3. Ci-6, which can be substituted by a halogen atom, G4·aryloxy , G5. cyano, G6. -N(R59a)(R59a,), wherein R59a&R59a are the same or different from each other and represent a hydrogen atom or a c-group and a combination of R- and an adjacent nitrogen atom. a saturated 5 ^ or 6 membered monocyclic heterocyclic ring, and the saturated heterocyclic ring may be selected from the group consisting of a hydroxyl group, an amine group, a Ci-e alkyl amine group, and a diCi-e alkyl amine group. Or 'a plurality of identical or different substituents substituted, G7. -CO-N(R59b)(R59b), wherein R and R59b are the same or different from each other and represent a hydrogen atom, a saturated 5 member or a 6 membered single ring system a heterocyclic group, or a C 6 alkyl group which may be taken through a heterocyclic group, 318197 34 G8. An aryl group and a 6 membered monocyclic heteroaryl group which may be substituted with a mercapto group or a thiol group, or a hetero/2 5 group. Adjacent nitrogen atoms together form a saturated 5- or 6-membered monocyclic system. The di- and heterocyclic ring-portion may have a double bond, and the saturated hetero-bicycle may be condensed to form a condensed ring, which may be condensed with a benzene ring to form a condensation = a residue and a heterocyclic ring may be selected from the group consisting of (4) and a thiol group. , c! 6 alkoxy, : and C 丨 4 oxy (4) substituted groups of one or more substituents. According to the pharmaceutical composition for treating or preventing diabetes according to Item 1, the D-wow compound represented by the following formula (1) or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier are as follows:

Wherein 0 represents an aryl group or a heteroaryl group; 'is not a hydrogen atom, a halogen atom, a Ci 6 alkyl group or. 6 alkoxy; 'not a halogen atom. -6 alkyl, Ci6 alkoxy or azide; R represents a halogen atom, a thiol group, a Ci 4 alkyl group, a dentate group, a C alkoxy group, a aryl group, an amine group, a aryl group Or G16 alkyl group; R4 represents 35 318197 ^^2688 〇) hydrogen atom; Substitution: [Α group] A1. Merid, A2·C!-6 alkoxy group ^Cl-channel group One or more substituents selected from the group consisting of A3·-N(R41)(r41·), the group SCΐζ: the same or different and representing a chlorine atom or. The clerk is a monocyclic heterocycle, and the adjacent mouse atoms of R form a saturated 5 member or e A4. aryl group, A5. heteroaromatic group, A6·~C〇-N(R411)(R4n,), wherein R4U& R411 , identical or different from each other - calcined; or ^ and succinctly together with an adjacent nitrogen atom ^ gas atom or k Lu or a 6-membered monocyclic heterocycle, which together form a saturated 5 member A7. carboxyl group, and A8. Cl~ 6 alkoxycarbonyl (3) 〇 2-6 alkenyl; (4) 〇 2-6 alkynyl; (5) 〇 3-8 cycloalkyl; (6) 〇 3-8 cycloalkyl Ch alkyl; Or 318197 36 1322688 (7) aryl; and R5 represents (1) C丨_6 alkyl which may be selected from the group consisting of: B, and one or more substituents are taken [Group B] B1. Hydrol, B2 Ci-6 alkoxy, B3. -N(R5,)(r51), wherein R5i and R51' are each a phase π 炫; or r and r. may be = or different and represent a gas atom or. 6 members of single ring heterocyclic ring, 8 material common wire and 5 members: and Β 4. -CO-N (R511) (K5i'·where R5n &R5" are identical or phase filaments, or R * wide can be used together Adjacent nitrogen atom or 6-membered monocyclic heterocyclic ring, 〃(10) is saturated with 5 members (2) C3-8 cycloalkyl; wherein the ring-based group can be condensed by a base, county or c with a bite ring, silk generation, Or (3) a C3-8 cycloalkylphosphonium-6 alkyl group; the ring filament of the C3-8 ring-based group Cl group may be substituted by a (iv) alkoxycarbonyl group, or may be condensed with a pyridine ring, earth, (4) A saturated 5- or 6-membered monocyclic heterocyclic group; which may be substituted with one or more substituents selected from the group consisting of: 318,197, 37, 1322,688 [Group C]

Cl. Ci-6 alkyl, C2. fluorenyl, C3. Ci-6, aryl, C4. carboxy, C5. C!-6 alkoxycarbonyl, and C6. -CO-(Alk)n- COOR52, wherein R52 is a hydrogen atom or a Ci-e alkyl group; Aik is a Ci_4 alkyl group; and η is an integer of 0 or 1 to 3, and (5) an aryl group may be selected from one or more of the following group d Substituent substitution: [DM] D1. trans group, D2. Cm alkoxy, D3. cyano, D4. Ch alkyl, wherein the Ch alkyl group may be selected from the group consisting of a hydroxyl group, a carboxyl group and a Ci 6 alkoxycarbonyl group. Substituting one or more substituents of the constituent group, D5. -N(R53)(R53,), wherein R53 and R53 are the same or different from each other and represent a hydrogen atom, C, -alkyl or Cl-6基 ,, D6. -C0-N(R53,)(R53丨.), wherein R531 is the same or different from each other and represents a hydrogen atom, a 6 alkyl group or a C1-6 alkylsulfonyl group, 318197 38 D7. 'COOR54, /, where R is a hydrogen atom, Cm alkyl group, Cl_6 alkylcarbonyloxy C1-6 alkyl group or Cm cycloalkyloxycarbonyloxy Ci6 alkyl group, D8· 'C(NH(0H)) =N-R55 > wherein R55 is a hydrogen atom or a Cl_6 alkylsulfonyl group, D9·saturated 5 or 6 membered monocyclic heterocyclic groups, and D1G. 5 or 6 members a heteroaromatic group which may be substituted with a sulfhydryl group or a sulfur group, a m-shell or a 6-membered monocyclic heteroaromatic group or a 5- or 6-shell, condensed heteroaromatic ring formed with a stupid ring, wherein the ^vn^ betaryl group may be One or more substituted (7) C7-10 aralkyl groups selected from the group consisting of: a base and a silk group;

One of the following E groups or one selected from the group consisting of F such that the alkyl group of the C?-u aryl group may be substituted with a plurality of substituents, and the aryl moiety may be substituted with one or more substituents. . [Group E]

El. Cm alkyl which may be substituted by hydroxy, Ε2. cyano, decyl, E4·Cm alkoxycarbonyl, phenyl, 318197 39 1322688 [F group] F1 · Ci-6, F2. Halogen, F3. cyano group, F4. thiol group, F5. Cm alkoxy group which may be substituted by one or more substituents selected from the group consisting of a carboxyl group and a Cl_6 alkoxycarbonyl group, F6. Halogen Ci-6 , F7. carboxy, F8·Cm alkoxycarbonyl, F9. -CO-N(R56a)(R56a), [f group] fl. Amine, f2. Cm alkylamino group f3. DiCh alkylamine Base f4. carboxy, f5. 匕-6 alkoxycarbonyl, f6. thiol, and wherein R and R are the same or different from each other and represent a hydrogen atom, a saturated 5-member or 6-membered single ring containing at least one nitrogen atom A heterocyclic group, or a fluorenyl 6 alkyl group, which may be substituted with one or more substituents selected from the group consisting of: a single ring system f7. a saturated 5 member or a 6 heterobasic group containing at least one nitrogen atom' 318197 40 1322688 F10. _C0-N(R56b)(R56b), wherein R56b and R56b are the same or different from each other and represent a hydrogen atom, a 6 alkyl group which may be substituted with an imido group, and an aralkyl group which may be selected from the group consisting of Amine group and tooth atom One or more substituents of the same or different substituents, arylsulfonyl groups which may be via Cl-e alkyl, Ci_e alkylsulfonyl, fluorenyl, amineyl, and -ei. Substituted by a arylamino or a mercaptoamine group,

Fll. -N=CR57(-N(R58)(R58')), wherein R57 is a hydrogen atom or a Cl_6 yard group, only 58 and R58, which are the same or different from each other and represent a hydrogen atom or a Cl_6 alkyl group, F12· 5- or 6-membered monocyclic heteroaryl, or F13. Methylenedioxy having a substituted or 6 M monocyclic heteroaryl group or substituted with 1 or 6 (tetra) condensed heteroaryl The g 6 alkyl group; the heteroaryl group in the group & can be substituted by one or more of the following 6 groups [Group G] G1. Group substitution: The alkyl group can be selected from the group consisting of g Or a plurality of substitutions [g group] g1·halogen atom, g2.amino group, 318197 41 1322688 §3. — Cl-6 alkylamino group, g4. diCh alkylamino group, g5. Cm alkoxycarbonylamine And § 6. via imine, G2. a halogen atom, G3. Cm alkoxy which may be substituted by a halogen atom, G4 aryloxy, G5. cyano, G6. -N(R59a) (R59a . . , where R and R 3 are the same or different from each other and represent a hydrogen atom or 〇_6 ί f : or broadly and a together with an adjacent nitrogen atom form a saturated 5-membered or 6-membered monocyclic heterocyclic ring, and The saturated heterocyclic ring may be selected from the group consisting of a hydroxyl group, an amine group, a CH alkyl amine group and a diCl-6 alkyl amine group. Substituting one or more identical or different substituents of the group, G7. -CO-N(R59b)(R59b), wherein W are the same or different from each other and represent a chlorine atom, a saturated 5 Å or "I ring" a heterocyclic group or a Ci 6 leukoyl group which may be substituted by a heterocyclic group, a G8.aryl group, and a G9. 5 member or a 6 membered monocyclic heteroaryl group, which may be keto or thioketo group or 318197 42 R and R5 together with an adjacent nitrogen atom form a saturated 5- or 6-membered monocyclic heterocyclic ring wherein one of the saturated heterocyclic rings may have a double bond and the saturated heterocyclic ring may be condensed with a stupid ring to form a fused ring. Condensation with a benzene ring to form a condensed saturated heterocyclic ring may be selected from the group consisting of a tooth atom, a Cl 6 alkyl group, a Ch alkoxy group, a thiol group, and a Ci-e alkoxy group. Multiple substituents are substituted.

3. The diabetic pharmaceutical composition for treatment or prevention according to the above item 1, wherein the pyrazole compound is a pyrazole compound represented by the following formula (π,):

Wherein R, R2, R3, R4 and R5 are as defined in the preceding paragraphs. 4. The pharmaceutical composition for treating or preventing diabetes according to the above item 1, wherein the pyrazole compound is a pyrazole compound represented by the following formula (π):

R5 is as defined in the above item 1, ru represents a tooth atom or a ruthenium atom ^ represents a south atom and R3a is a tooth atom or a Ci6 yard group. The pharmaceutical composition for the treatment or prevention of diabetes in the former ^4, /, " is a wind atom or a fluorine atom 'R, a fluorine atom or a chlorine atom, and R3a is a 318197 43 1322688 gas atom or a Cl-6 Hyun base. 6. The pharmaceutical composition for treating or preventing diabetes according to the above 5, wherein the pyrazole compound is a pyrazole compound represented by the following formula (111):

Wherein R4 and R5 are as defined above. The pharmaceutical composition for treating or preventing diabetes according to any one of the preceding items 2 to 6, wherein R4 is a group selected from the group consisting of: (1) a hydrogen atom; (2) a C alkyl group which may be selected from the group consisting of Substituting A for one or more substituents of the group: [A' group] A' 1. trans group, A 2 · Ci-4 oxy, A' 3. ~N(R41)(r41'), alkane A or the middle two 1 Μ1 are identical or different from each other and represent a hydrogen atom or a 16-series heterogeneous:: together with adjacent nitrogen atoms to form a saturated 5! A'4. Stupid, A'5·5 members Or 6 members of a monocyclic heteroaromatic group, A'6·~C〇, (R41丨)(R4 丨丨·), 318197 44 1322688 wherein R and R4n are the same or different from each other and represent a hydrogen atom or a Ci 'morphology Or R and R411 together with adjacent nitrogen atoms to form a saturated or 6 membered monocyclic heterocycle, A' 7. carboxyl, and A 8. Ci-4 alkoxy, (3) C2 -6 alkenyl, (4) C2-6 alkynyl, (5) (: 3-8 cycloalkyl; • and (6) 〇3-8 calcyl-based Cl-4 alkyl. 8. According to the aforementioned 2 A pharmaceutical composition for the treatment or prevention of diabetes, wherein R5 is a Cl_6 alkyl group, according to any one of the above items 2 to 7. a pharmaceutical composition for treating or preventing diabetes, wherein r5 is a Gw cycloalkyl group which may be one or more identical or _ phase selected from the group consisting of a hydroxyl group, a carboxyl group and a Ch alkoxycarbonyl group The pharmaceutical composition for treating or preventing diabetes according to any one of the above items 2 to 7 wherein R 5 is a CM cycloalkyl C 6 alkyl group. 11 according to the aforementioned items 2 to 7 A pharmaceutical composition for treating or preventing diabetes, wherein F is a saturated 5 member or 6 membered monocyclic heterocyclic group which may be selected from the group consisting of sulfhydryl and -CO-(Alk)n-COOR52 Substituting one or more substituents of the constituent group, wherein R52 is a hydrogen atom or a Ci s alkyl group, 9 is a Ci-4 alkylene group, and n is 〇 or an integer of 1 to 3. 12· according to the foregoing 2 to 7 A 318197 45 pharmaceutical composition for the treatment or prevention of diabetes, wherein R5 is a phenyl group which may be substituted with one or more substituents selected from the group consisting of D, Group D'1 · Cm alkyl group can be substituted by a carboxyl group, D'2. -C0-N(R53)(R53,), where R and R3 are the same or different from each other and represent a hydrogen atom and a ci4 appearance. Or Ch alkylsulfonyl; D' 3 · -COOR54, π wherein R 4 is a hydrogen atom, C, -4 alkyl, c, -4 alkylcarbonyloxy (;; " alkyl or Ch ring oxime A carbonyloxyChalkyl group, and a D 4·5 member or a 6 membered monocyclic heteroaryl group may be substituted by a keto group or a thioketo group. - 13. The pharmaceutical composition for the treatment or pre-p-diabetes according to any one of items 2 to 7, wherein R5 is "aryl aryl and the aryl aryl β 77 of the C 7-14 Substituted by one or more substituents selected from the group F below: [F, group] F 1. Ci-6 alkyl, F' 2 · halogen atom, F' 3. cyano group, F' 4. F'5. Ch alkoxy which may be substituted by one or more substituents selected from the group consisting of a carboxy group and a Cie alkoxycarbonyl group, F' 6. haloCh alkyl, 318197 46 1322688 F'7· Carboxyl, F 8 · Cm alkoxycarbonyl, F 9. -c〇-N(R56a)(R56a'), wherein the 'same' are the same or different from each other and represent a saturated atom of a hydrogen atom to a y-nitrogen atom Or a 6-membered monocyclic heterocyclic group which may be substituted with one or more substituents selected from the group f' below [f' group] * f' 1 · amine group, f 2 · - Cl-6 Alkylamino ' ί 3 · a Cl-6 alkylamino group 'f' 4. carboxyl group, f' 5. Cm alkoxycarbonyl group, f ' 6. trans group, and f'7· having at least one nitrogen atom a saturated 5- or 6-membered monocyclic heterocyclic group, F, 10. -N(R56b)(R56b.), wherein R56b and R5ba' Is the same or different and represents a hydrogen atom, a Cl_6 alkyl group which may be substituted with an imido group, and an aryl group which may be identical or different from one or more selected from the group consisting of an imine group and a tooth atom Substituent substituted, arylsulfonyl group which may be via Ci-e alkyl, C]-e alkyl fluorenyl, fluorenyl, amino fluorenyl, monoCl 6 alkyl fluorenyl or 6-alkylamino fluorenyl substituted, F, 11. -N=CR57(R58)(R58'), 47 318197 wherein R57 is a hydrogen atom or a Ci 4 alkyl group, r or a different hydrogen atom or an alkyl group , which is the same as the F1. 5 or 6 membered monocyclic heteroaryl, F 13. methylene dioxy or ethyl dioxy. 14. According to the above 2 to 7一埴少田# A pharmaceutical composition, which is a Cm-sintered by a 5- or 6-membered monocyclic heteroaryl group, and the heteroaromatic group can be selected from the group consisting of g, Replacement of substituents: 丨u名夕[G, group] G,1. Base substitution:

Ci-e may be substituted by one or more selected from the group of g' below [g, group] g 1. _ atom, g' 2. amine group, g' 3. -alkylalkyl group, g '4·DiCl-6 alkylamino group, g' 5. Ch alkoxycarbonylamino group, and g' 6. hydroxyimino group, G' 2. halogen atom, G'3. Cm alkoxy group Can be substituted by a halogen atom, G'4. aryloxy, G' 5. cyano, 318197 48 1322688 G'6. -N(R59a)(R59a·), corpse A, I La and '9 are identical to each other or Different from each other and representing a hydrogen atom or a Cl. 6 t member, together with an adjacent nitrogen atom, may form a saturated 5 member or 6 moles of early mixed earth, and the saturated heterocyclic ring may be selected from a hydroxyl group, an amine group, a -Ch alkyl group. a group consisting of an amine group and a di-Ch-alkylamino group: one or more substituents substituted, G, 7. -CO-N(R59b)(R59b), wherein P and Yan are identical or different from each other And a G 6 8. The miscellaneous material may be substituted with a thiol or thioketo group. 15. (4) (d) of the items 2 to 6 for the treatment or prevention of diabetes, wherein a saturated 5- or 6-membered monocyclic heterocyclic group is formed together with an adjacent nitrogen atom, wherein the saturated heterocyclic group a moiety may have a double bond, and the saturated heterocyclic group may be condensed with a benzene ring to form a condensed ring, and the saturated heterocyclic group which may be condensed with a benzene ring to form a condensed ring may be selected from a tooth atom, & Substituting one or more substituents of the group consisting of a channel, a ch-oxyl group, a slow group, and a Ch alkoxy group. The pharmaceutical composition for treating or preventing diabetes according to the above 2, wherein the pyrazole compound is a pyrazole compound represented by the following formula (ίν): 318197 49 1 East as 2 items $ t ¥ is different And 蛊 thousand & 広, 弋, RX1, RX2 and RX3 are mutually different and represent an integer of 1 to 2. a substituent of the following F ′ group, and 10 η] Γ κ alkyl 'F” 2. a halogen atom, a F 3 · cyano group, an F hydroxy group, a hydroxy group, a 4-membered earth, which may be selected from a carboxyl group and a C group.丨-4 alkoxycarbonyl, and substituted by one or more substituents of the group, F" 6. halogen Ci-6 alkyl, φ F" 7. carboxyl, F 8. Ci-6 oxygenated A thiol group, F" 9 -CO-N(R56a)(R56a), wherein R56a and R56a are the same or different from each other and represent a hydrogen atom, a saturated 5-membered or 6-membered monocyclic steroid having at least one nitrogen atom a cyclic group, or a Ci alkyl group, which may be substituted with one or more substituents selected from the group "f" below.

[Γ group] Γ 1. Amine group, f" 2. - Ci-6 alkylamino group, 318197 50 1322688 f 3. DiCl-6 Hyun "Amino group, f" 4. Carboxyl group, 5. Ch alkoxylate Alkylcarbonyl, f" 6. hydroxy, and f 7. a saturated 5- or 6-membered monocyclic heterocyclic group having at least one gas atom, F" 10. -N(R56b)(R56b.), wherein R56b and R56b ' mutually identical or different and represents a hydrogen atom, a Ch alkyl group which may be substituted with an imido group, an aralkyl group which may be selected from one or more of the same or a group selected from the group consisting of an imido group and a halogen atom. a hetero-substituent substituted, arylsulfonyl group which may be via a C-6 alkyl group, a Cl_e alkylsulfonyl group, a fluorenyl group, an aminomethyl fluorenyl group, a C]-e alkylaminocarbamyl group or two Cl_6 alkylaminocarbinyl substituted, F" 11. -n=cr57(-n(r58)(r58')), wherein R is a hydrogen atom or a Cm alkyl group, and R58 and R58 are the same or different from each other. And represents a hydrogen atom or a C, -6 alkyl group, a F 12·5 member or a 6 membered monocyclic heteroaryl group, and a F I3.methylenedioxy group or an extended ethyldioxy group. a pharmaceutical composition for treating or preventing diabetes, wherein the pyrazole compound is as follows The pyrazole compound represented by the formula (v): 318197

The single Yin 1, the middle R4 is as defined in the above two items, the ring Het represents 5 members or 6 members of the long doped aromatic group, and Rn, ^ and γ are identical or different from each other and represent a halogen atom or are selected from the following G a substituent of the group, and m, an integer of 0 or 1 to, < [G, group] or a plurality of substituted 1 Ch alkyl groups which may be substituted by a group selected from the group consisting of g, g Group] g1·halogen atom, ^ 2.amino group, ^ 3· —Ch alkylamino group, g 4·diCl-6 alkylamino group, g Cl-6 alkoxyamino group, t 6· Hydroxyimino group, ^ 2 · halogen atom, Γ 9 〇

Cm alkoxy which may be substituted by a tooth atom, G 4 · aryloxy, 5 · cyano, 318197 52 G' 6 · -N(R59a)(R59a ), • wherein R59a& R59a are identical or different from each other And one &

a Cu6 alkyl group, or R59a and R59a, a porphyrin-free atom or a 6-membered mono-product, ", and a sub-form together form a saturated 5-member or - an early-coating hydrazine, and the saturated heterocyclic ring may be selected from a hydroxyl group, Amine,

Substituted by a plurality of substituents consisting of a chalcylamino group and a diCi 6 alkylamino group, each of A G '7. 'CO-N(R59b)(R59b,), M R59b and R59b' are identical or phase to each other. XOR represents a hydrogen atom, a saturated 5-membered or 6-membered monocyclic heterocyclic group, or a Cl-6-alkyl group which can be substituted, G' 8. aryl, and a G 9. 5 member or a 6 membered monocyclic ring The aryl group may be substituted by a keto group or a thioketo group. 18. The pharmaceutical composition for the treatment or prevention of diabetes according to the above item 17, wherein the Het ring is a pyridine ring, a triazole ring or an oxazole ring. 19. The pharmaceutical composition for treating or preventing diabetes according to the above 18, wherein the pyrazole compound is a pyrazole compound represented by the following formula (VI):

318197 53 1322688 20. The pharmaceutical composition for treating or preventing diabetes according to the above item 2, wherein the pyrazole compound or a pharmaceutically acceptable salt thereof is selected from the group consisting of 5-(2-gas-4, 5-difluoro) -phenylphenylamino)-1Η-pyrazole-3-carboxylic acid (pyridin-3-ylmethyl)-decylamine, 5-(2_g-4, 5-difluoro-benzoguanamine Base)-1Η-carbazole-3-carboxylic acid hydrazin-3-ylindenyl)-nonylamine dihydrochloride, 5-(2-chloro-4,5-difluoro-benzoinylamino) -1Η-carbazole-3-carboxylic acid gin (pyridin-3-ylindenyl)-decylamine hydrochloride, 5-(2-chloro-4, 5-difluoro-benzylidenylamino)- 1Η-carbazole-3-carboxylic acid (4-mercapto-oxazol-5-ylindenyl)-nonylamine, 5-(2-chloro-4,5-difluoro-benzoinylamino)- 1Η-pyrazole-3-carboxylic acid (4-methyl-oxazol-5-ylmethyl)-decylamine, 5-(2-chloro-4, 5-difluoro-benzoinylamino)- 1Η-pyrazole-3-carboxylic acid (4-methyl-oxazol-5-ylmethyl)-nonylamine p-toluenesulfonate, φ 5-(2-chloro-4, 5-difluoro-benzoquinone Mercaptoamino)-1Η-pyrazole-3-carboxylic acid (4-methyl-oxazol-5-ylindenyl)-nonylamine L-(+) tartrate, 5-(2-chloro-4, 5-difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid (2,4- Mercapto-oxazol-5-ylindenyl)-nonylamine p-toluenesulfonate, 5-(2-chloro-4,5-difluoro-benzylidenylamino)-1Η-pyrazole-3- Carboxylic acid (2,4-dimercapto-oxazol-5-ylindenyl)-nonylamine, 5-(2-chloro-4,5-difluoro-benzoguanidino)-1Η-pyrazole 3-carboxylic acid (2,4-dimethyl-pyridin-3-ylindenyl)-decylamine, 5-(2-chloro-4,5-difluoro-benzoinyl)-1Η- Pyrazole-3-carboxylic acid 54 318197 1322688 diethyl decylamine, 5-(2-chloro-4, 5-difluoro-phenylhydrazinoamino)-1 Η-pyrazole-3-carboxylic acid ethyl- («bipyridin-4-ylmethyl)-decylamine, • 5-(2-Gas-4, 5-difluoro-phenylhydrazinoyl)-1Η-pyrazole-3-carboxylic acid (2-曱oxy-ethyl)-mercapto-nonylamine, 5-(2- gas-4, 5-difluoro-phenylhydrazinoamino)-1 fluorene-carbazole-3-carboxylic acid ethyl-(2 -decyloxy-ethyl)-decylamine, 5-(2- gas-4, 5-difluoro-phenylhydrazino)-1Η-°biazole-3-carboxylic acid _ 2-fluoro-section Indoleamine, 5-(2-chloro-4, 5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylic acid 3-fluoro-tuberamine, 5-(2-chloro-4 , 5-difluoro-phenylhydrazinoamino)-1Η-°biazole-3-carboxylic acid 2-didecylamino-benzylamine, 5-(2- gas-4, 5-difluoro- Benzoylamino)- 1Η-pyrazole-3-carboxylic acid (4-ethoxycarbonyl-cyclohexyl)-propyl-decylamine, φ 5-(2-gas-4, 5-difluoro-benzhydrylamino)-1Η -pyrazole-3-carboxylic acid (6-decyloxy-pyridin-3-ylmethyl)-decylamine, 5-(2-chloro-4,5-difluoro-benzoinyl)-1Η -. Bis-zolyl-3-carboxylic acid 2,3-dimethoxy-benzylamine, 5-(2-chloro-4,5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylate Acid 2,4-dimethoxy-benzylamine, 5-(2-chloro-4,5-difluoro-benzoylaminopyrazole-3-carboxylic acid 2,6-dimethoxy- Benzylamine, 5-(2-Gas-4,5-difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid 55 318197 1322688 3, 5-Dimethoxy-benzylamine , 5-(2-chloro-4, 5-difluoro-anthracenylamino)-1Η-pyrazole-3-carboxylic acid 3,4-dimethoxy-benzylamine, 5-(2- Gas-4, 5-difluoro-phenylhydrazinoamino)-1Η-η-pyrazole-3-carboxylic acid 2,3-difluoro-nodal amine, 5-(2-chloro-4, 5-di Fluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid 2. 4-Difluoro-tubular amine ' 5-(2-chloro-4, 5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylic acid• 2, 5-difluoro-benzyl hydrazine Amine, 5-(2- gas-4, 5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylic acid 2,6-difluoro-benzylamine, 5-(2-chloro -4, 5-difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid 3,4-difluoro-benzylamine, 5-(2-chloro-4, 5-difluoro- Benzoylamino)-1Η-carbazole-3-carboxylic acid 3. 5-difluoro-tuberamine, φ 5-(2-chloro-4, 5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylic acid (2-isopropoxy-pyridine 3--3-indenyl)-nonylamine, 5-(2-chloro-4,5-difluoro-anthracenylamino)-1Η-pyrazole-3-carboxylic acid (2-phenoxy-oxime) Pyridin-3-ylindenyl)-nonylamine, 5-(2-chloro-4,5-difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid (3, 5-difluoro -pyridin-2-ylmethyl)-decylamine, 5-(2-chloro-4,5-difluoro-benzylcarboxyamino)-1Η-σ ratio α-sodium-3-nonanoate Benzo-benzylamine, 5-(2-chloro-4,5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid 56 318197 1322688 3-trifluorodecyl-peptidylamine , 5-(2-chloro-4,5-difluoro-phenylhydrazino)-1Η-°Bizozol-3-glycolic acid 4-trifluorodecyl-tuberamine, 5-(2-gas -4, 5-difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-buffer acid 4_t-butyl-tuberamine, 5-(2-chloro-4,5-difluoro- Benzoylamino)-1Η-pyrazole-3-decanoic acid (6-isopropoxy-° ratio _3-ylindenyl)-bristamine, 5-(2- gas-4, 5- Difluoro-benzoylamino)-1Η_〇 is more than saliva-3-acidic fist [2-(2,2,2-trifluoro-ethoxy)-indenyl-3-ylmethyl] - Amine, 5-(2-gas- 4, difluoro-benzhydrylamino)-1Η-π ratio -3--3-acid 4-(2-didecylamino-ethylamino fluorenyl)-benzylguanamine, 5-( 2-ox-4, 5-difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carbamic acid 4-ethyl-peptidylamine, 5-(2-gas-4, 5-difluoro -benzimidylamino)-1Η-pyrazole-3-hypoacid 4-isopropyl-benzylguanamine, ^ 5-(2-chloro-4, 5-difluoro-benzoinyl) -111-〇 《 "Sit-3-or acid 2-gas-6-fluoro-benzylamine, 5-(2-chloro-4,5_di-benzoylamino)-111-«» Ratio of salicylic acid (6-ethoxy-pyridin-3-ylindenyl)-decylamine dihydrochloride, 5-(2-chloro-4,5-difluoro-benzoylamino) )-1Η-β is more than 嗤-3-glycolic acid (thiazol-4-ylmethyl)-decylamine, 5-(2-chloro-4, 5-difluoro-benzoylamino)-1Η-11 Thirty-seven retinoic acid [6-(2,2,2-trifluoro-ethoxy)-σ ratio biting-ylmercapto]-decylamine dihydrochloride, 57 318197 1^^2688 5 (2-Ga-4, 5-difluoro-phenylhydrazino)-ΐη-pyrazole-3-hypoacid 2'6-monomethyl-tuberamine, 5-(2-chloro-4, 5-difluoro-phenylhydrazinoamino)-ιη-pyrazole-3-hypoacid [2-indolyl-3-yl)thiazole-4-ylmethyl]-decylamine dihydrochloride 5-(2-gas-4, 5-difluoro-benzylidenylamino)-ιη-pyrazole-3-carboxylic acid (1Η-stupidimido-2-ylindenyl)-decylamine dihydrochloride Salt, [4~({ [5-(2-Gas-4,5-difluoro-phenylhydrazino)]mium-pyrazol-3-yl]aminoindole monomethyl)-Benzyl Mercaptoamine]-methyl acetate, "3-[5-(2-gas-4, 5-difluoro-benzhydrylamino)-indole-pyrazole-3-carbonyl]amino}- Sulfhydryl)- benzoylaminol] decyl propionate, 5-(2- gas-4, 5-difluoro-benzhydrylamino)-ιη-pyrazole-3-buffer acid (2 -methyl-thiazol-4-ylindenyl)-nonylamine dihydrochloride, 5-(2- gas-4,5-difluoro-phenylhydrazinoyl)-ιη-pyrazole-3-carboxylate Acid (3,5-dimethyl-isooxasin-4-ylmethyl)-decylamine, 5-(2-chloro-4,5-difluoro-benzylidenylamino)-ιη-pyrazole —3-carboxylic acid• 4-(2-indole-(2-acetoxyethyl)-amino-ethylaminomethylmercaptobenzylamine, 5 (2 gas-4,5-fluoro) Benzoylamino)-lH-0 ratio. 3-O-acid 4-(2-trans-ethylaminomethylmercapto)-benzylamine, 5-(2-chloro-4,5-difluoro-benzofuranylamino)-ih -〇比嗤-3--acid 4-(2-[(2-acetoxyethyl)-(2-hydroxyethyl)-amino]-ethylaminomethylindenyl}-benzylguanamine , 5-(2-chloro-4,5-dioxo-benzhydrylamino)_ΐΗ-.嗤-3-Zero-acid (1-methyl-1 Η-benzimidazol-2-ylindenyl)-decylamine hydrochloride, 58 318197 1322688 5-(2-chloro-4, 5-difluoro-benzene Mercaptoamine)-1 Η-pyrazole-3-carboxylic acid (thiazol-2-ylindenyl)-guanamine dihydrochloride, 5-(2-gas-4, 5-difluoro-benzoic acid Mercaptoamino)-1Η-pyrazole-3-carboxylic acid (benzothiazol-2-ylindenyl)-guanamine dihydrochloride, 5-(2- gas-4, 5-difluoro-phenylhydrazine Mercaptoamine)-1Η-pyrazole-3-carboxylic acid (2,5-dimercapto-thiazol-4-ylindenyl)-guanamine dihydrochloride, 5-(2-gas-4, 5 -difluoro-phenylhydrazinoamino)-1Η-η-pyrazole-3-carboxylic acid [2-(morpholin-4-yl)-thiazol-4-ylmethyl]-decylamine dihydrochloride, 5-(2-chloro-4,5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylic acid (1,3,5-tridecyl-1Η-pyrazol-4-yl Methyl)-nonylamine, 5-(2-chloro-4,5-difluoro-benzylidenylamino)-1Η-°biazole-3-carboxylic acid (2-chloro-6-mercapto-pyridine -3-ylmethyl)-guanamine dihydrochloride, 5-(2-chloro-4,5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylic acid (2-di Nonylamino-thiazol-4-ylindenyl)-nonylamine dihydrochloride, 5-(2-chloro-4,5-difluoro-benzoinyl)-1Η-pyrazole-3- Carbohydrate (1-methyl-1Η-pyrrol-2-ylindenyl)-decylamine, 5-(2-gas-4, 5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylate Acid (3,4-dimethoxy-pyridin-2-ylmethyl)-guanamine dihydrochloride, 5-(2-chloro-4, 5-difluoro-phenylhydrazino)-1Η -pyrazole-3-carboxylic acid (5-tert-butyl-thiazol-2-ylindenyl)-guanamine dihydrochloride, 5-(2- gas-4, 5-difluoro-phenylhydrazine Aminopyrazole-3-carboxylic acid (5-mercapto-2-phenyl-2indole-[1,2,3]triazol-4-indolyl)-decylamine, 5-(2-chloro-4 , 5-difluoro-phenylhydrazinoamino)-1Η-indazole-3-carboxylic acid [4-(Third-butoxy-amino-amino)-methyl-indenyl-2-methyl Base]-bristamine' 59 318197 1322688 5-(2-Gas-4, 5-difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid [4-mercapto-2-(? Phenyl-4-yl)-thiazol-5-ylmethyl]-indolyl dihydrochloride, 5-(2- gas-4, 5-difluoro-phenylhydrazino)-1Η-pyrazole- 3-carboxylic acid (pyridin-3-ylmethyl)-nonylamine 3/2 hydrochloride hemihydrate, 5-(2-chloro-4, 5-difluoro-phenylhydrazino)-1Η-比-pyrazole-3-carboxylic acid 2-amino-benzylguanamine, 5-(2-chloro-4, 5-difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid 2- Methoxy-benzylamine, 5-( 2-ox-4, 5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid 3-methoxy-benzylamine, 5-(2-chloro-4, 5-di Fluoro-benzoguanidino)-1Η-pyrazole-3-carboxylic acid 4-decyloxy-benzylamine, 5-(2-chloro-4,5-difluoro-benzhydrylamino) -1Η-pyrazole-3-carboxylic acid 4-methyl-benzylamine, 5-(2-chloro-4, 5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylic acid 4-fluoro-benzylamine, 5-(2-chloro-4,5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid 4-oxobenzylamine, 5-( 2-Chloro-4, 5-difluoro-adenylamino)-1Η-pyrazole-3-carboxylic acid 4-ethoxycarbonyl-benzylamine, 5-(2-chloro-4, 5-di Fluoro-benzoguanidino)-1Η-pyrazole-3-carboxylic acid 4-carboxy-benzylamine, 5-(2-chloro-4, 5-difluoro-benzylidenylamino)-1Η -pyrazole-3-carboxylic acid dibenzylamine, 60 318197 1322688 5-(2-gas-4,5-difluoro-benzhydrylamino)-1 Η-pyrazole-3-carboxylic acid (cyanide) -Phenyl-methyl)-decylamine, 5-(2-chloro-4,5-difluoro-phenylhydrazinoyl)-1Η-pyrazole-3-carboxylic acid Amine, 5-(2- gas-4, 5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylic acid (2-hydroxy-ethyl)-phenyl-decylamine, 5- (2-gas-4, 5- Difluoro-benzoguanidino)-1Η-pyrazole-3-carboxylic acid cyclohexyl-fluorenyl-nonylamine, ® 5-(2-chloro-4, 5-difluoro-anthracenylamino -1 - pyrazole-3-carboxylic acid cyclohexyl decylamine, 5-(2- gas-4, 5-difluoro-phenylhydrazino)-1 Η-° ratio. Benzyl phthalate-ethyl-bristamine, 5-(2-chloro-4, 5-difluoro-phenylhydrazino)-indole-pyrazole-3-carboxylic acid allyl ring Hexyl-decylamine, 5-(2-chloro-4,5-difluoro-phenylhydrazino)-ιη-pyrazole-3-hypoacid 0-cyclohexyl-(p-but-2-ylmethyl) ) _ guanamine, 5_(2- gas-4,5-fluoro-benzylamino)-1Η_〇 than 〇 sit-3-reductive methyl-(1-methyl-Β bottom bite- 4-yl)-nonylamine, 5-(2-chloro-4,5-difluoro-phenylhydrazinyl)-1-indole-pyrazole_3_carboxylic acid [(3,4-indenyl-oxyl) Phenyl)-methyl]-chiral amine hydrochloride, 5-(2-chloro-4, 5-difluoro-benzylidenylamino)-1-indole-pyrazole-3-ylcarboxylic acid benzyl-butyl - decylamine, 5-(2-chloro-4, 5-difluoro-benzylidenylamino)-1-indole-pyrazole-3-carboxylic acid benzyl-(4-hydroxy-butyl)-nonylamine hydrochloride , 318197 61 1322688 5-(2-Chloro-4,5-difluoro-phenylhydrazinylamino)_1Η~·π ratio 0 sitting-3-tagamic acid butyl-ethyl-decylamine, 5-(2 - gas-4, 5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid cyclohexyl-propyl-decylamine, 5-(2-chloro-4,5-di-fail- Benzene arylamino)-1Η-πι^0 sitting-3-oxo acid butyl-cyclohexyl-decylamine, 5-(2-chloro-4, 5- Difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid cyclohexyl-(2-decyloxyethyl)-decylamine, 5-(2_chloro-4,5-dioxin- Benzoylamino-sulfonic acid cyclohexyl-(pyridin-3-ylmethyl)-decylamine, 5-(2-chloro-4, 5-difluoro-phenylhydrazino)-1Η-pyridyl Zyridin-3-carboxylic acid [2-norphin-4-yl]-phenyl]-nonylamine, 5-(2-chloro-4,5-difluoro-benzylidenylamino)-1Η-pyrazole 3-carboxylic acid dibutyl-branched amine, 5-(2-chloro-4, 5-difluoro-phenylhydrazinyl)-1Η-pyrazole-3-carboxylic acid φ贰-(2-methoxy Ethyl ethyl)-nonylamine, 5-(2-chloro-4, 5-difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid (2-methoxyethyl)-propan Base-bristamine, 5-(2-chloro-4, 5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylic acid • butyl _ (four-page base-4-yl) -N-amine, 5-(2-chloro-4, 5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylic acid (2-methoxyethyl)-(tetrahydro-britt -4-4-yl)-bristamine' 5-(2-gas-4,5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid Wang 戍 戍 - (2 - A Oxy-ethyl)-bristamine ' 62 318197 1322688 5-(2-Gas-4, 5-difluoro-benzylidenylamino)-ΐη-pyrazole-3-carboxylic acid cyclohexyl-(3 -methoxy-propyl)-nitramine, 5-(2-gas-4, 5-difluoro-benzylidenylamino)-ιη-pyrazole-3-carboxylic acid cyclohexyl-(2-B Oxy-ethyl)-decylamine, 5-(2-gas-4, 5-difluoro-benzoamitoylamino)-ιη-pyrazole-3-carboxylic acid cyclohexyl-(2-isopropoxy -ethyl)-guanamine, 5-(2-gas-4, 5-difluoro-benzylidenylamino)-ιη-pyrazole-3-carboxylic acid cyclohexyl-(2-propoxy- Ethyl)-guanamine, ® 5_(2-Gas-4, 5-difluoro-phenylhydrazino)-indole-pyrazole-3-carboxylic acid (ethyl-propyl)-(2-oxo) -ethyl)-decylamine, 5-(2-gas-4, 5-difluoro-benzoamitoylamino)-lH-pyrazole-3-carboxylic acid butyl-(1_second butoxy Alkyl-pyro--4_yl)-bristamine, 5-(2-chloro-4,5-difluoro-benzoindolyl)-1Η-pyrazole-3-carboxylic acid butyl-(four Hydrogen-sulfur-norm-4-yl)-decylamine, 5-(2-gas-4, 5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid φ butyl-( 2-methoxy-ethyl)-decylamine, 5-(2-gas-4, 5-difluoro-benzylidenylamino)-1Η-pyrazole-3-carboxylic acid butyl-(pyridine- 3-ylmercapto)-indolamine, 5-(2-chloro-4, 5-difluoro-benzoinylamino)-1Η-πϋ〇 sitting-3-o-acid benzyl-(2-oxime Base-B )--Amine, 5-(2_fluoro-4,5-difluoro-benzofuranylamino)-1Η-0 ratio 0 sitting-3-o-acid butyl-(precipitate-4-yl)- Amine, 5-(2- gas-4, 5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid (1-acetic acid-Chen-4-yl-4-yl)-butyl Base-decylamine, 63 318197 1322688 5-(2-Gas-4, 5-difluoro-benzhydrylamino)-1H-pyrazole-3-carboxylic acid butyl-(1-曱 酿 酿 - Piece-4-yl)-bristamine, 5-(2-chloro-4, 5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid butyl-(1_ethoxy陶-基派-4-基)-Taolin, 5-(2-chloro-4, 5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylic acid butyl-( 1-acidic acid-branched 4-yl)-guanamine, 5-(2-chloro-4, 5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylic acid Base-(1,1-dimercapto-hexahydro-1 and 6-sulfur 0-pyranyl-4-iso)-decylamine, 5-(2-chloro-4, 5-difluoro-benzimidamide Base)-1Η-pyrazole-3-carboxylic acid butyl-(1_mercapto-hexanitro-1 λ 4-sulfur D ratio 0 base)-bristamine, 5-(2_gas-4,5-di Fluoro-benzoylamino)-1Η-η ratio 0 -3-carboxylic acid (6-methoxy-pyridin-3-ylmethyl)-propyl-decylamine, 5-(2-chloro- 4,5-difluoro-benzoguanidino _1Η- * Ό sit -3- betray acid propyl - (. Bipyridin-3_ylmercapto)-nonylamine, 5-(2- gas-4, 5-difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid 4-diethylamine Benzyl-benzylamine, 5-(2-chloro-4,5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylic acid 3-diethylaminocarbamyl -benzamide, 5_(2-gas-4, 5-difluoro-benzoquinone-based amine group β-sodium-3-sulphate 4-ethylaminomercapto-benzylamine, 5-(2 - gas-4, 5-difluoro-phenylhydrazinoamino)-1-pyridazole-3-carboxylic acid 3-ethylaminomercapto-benzylamine, 5-(2-gas-4, 5-difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid 4-aminomercapto-benzylamine, 64 318197 1322688 5-(2-chloro-4, 5-difluoro -benzoylamino)-1Η-pyrazole-3-carboxylic acid (1-acid oxalyl-piperidin-4-yl)-propyl-decylamine, 5-(2-chloro-4, 5 -difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid (1_ 叛 乙 乙 - - 底 _ _ 4 - base) _ propyl-bristamine, 5-(2- Gas-4, 5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid [1-(2-carboxypropenyl)-piperidin-4-yl]-propyl-oxime Amine, 5-(2-chloro-4,5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylic acid cyclopropyl-(6-methoxypyridin-3-yl-methyl) - indoleamine, 5-(2-chloro-4, 5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid cyclobutyl-(6-methoxy-pyridine-3 -mercapto)-nonylamine, 5-(2- gas-4, 5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylic acid cyclopropyl fluorenyl-(6-曱Oxypyridin-3-ylmethyl)-decylamine, 5-(2-chloro-4,5-difluoro-phenylhydrazinoylamino)-1indole-pyrazole-3-carboxylic acid (6-di Nonylamino-pyridin-3-ylindenyl)-nonylamine, 5-(2-chloro-4,5-difluoro-benzylidenylamino)-1Η-pyrazole-3-carboxylic acid (6 -didecylamino-pyridin-3-ylindenyl)-propyl-decylamine, 5-(2- gas-4,5-difluoro-phenylhydrazino)-1Η-carbazole-3 -carboxylic acid benzyl-(2-sulfo-ethyl)-bristamine' 5-(2-chloro-4,5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid Alkyl _(2-ethoxyxo-ethyl)-bristamine, 5-(2- gas-4,5-difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid ( 6-Chloro-pyridin-3-ylindenyl)-propyl-decylamine, 5-(2-chloro-4,5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylate Acid 2,6-dichloro-tubergic amine, 65 318197 1322688 5-(2- gas-4,5-dioxa-benzoic acid amine)_1Η-πΛα sitting-3 - oxic acid (3,5- Dichloro- Pyridin-4-ylindenyl)-nonylamine, 5-(2-chloro-4,5-difluoro-benzylidenylamino)-1Η-pyrazole-3-carboxylic acid (3,5-digas -pyridin-4-ylindenyl)-propyl-decylamine, 5-(2- gas-4,5-difluoro-phenylhydrazinoyl)-111-pyrazole-3-carboxylic acid [6- (1Η-pyrazole-buyl)-pyridin-3-ylmethyl]-nonylamine dihydrochloride, 5-(2-chloro-4,5-difluoro-benzoinyl)-111- Pyrazole-3-carboxylic acid [6-(4-hydroxy-piperidin-bu)-pyridin-3-ylindenyl]-nonylamine dihydrochloride, 5-(2-chloro-4,5-di Fluoro-benzoguanidino)-111-pyrazole-3-carboxylic acid (2-pyridin-2-yl-ethyl)-decylamine, 5-(2- gas-4,5-difluoro-benzene Nonylamino)-111-pyrazole-3-carboxylic acid (2-pyridin-3-yl-ethyl)-decylamine, 5-(2-chloro-4, 5-difluoro-phenylhydrazine Amino)-1Η-°biazole-3-carboxylic acid (2-pyridin-4-yl-ethyl)-decylamine, 5-(2-chloro-4,5-difluoro-anthracenylamino )-111-pyrazole-3-carboxylic acid (4-[1,2,3]thiadiazol-4-yl-benzyl)-decylamine, 5-(2-chloro-4, 5-difluoro- Benzoylamino)-1Η-pyrazole-3-carboxylic acid (5-fluorenyl-pyridin-2-yl-methyl)-decylamine, 5-(2-chloro-4, 5-difluoro -benzimidylamino)-1Η-pyrazole-3-carboxylic acid pyridin-2-yl-indole , 5-(2- gas-4,5-difluoro-benzoylaminosyl-3-pyrexate-5-yl-decylamine, 5-(2-chloro-4,5-difluoro - Benzene arylamino)_1H - 0 than 吐-3 - 酸酸喧琳-8-yl-amine, 66 318197 1322688 5-(2-chloro-4, 5-difluoro-benzimidamide Base)-ιη-pyrazole-3-carboxylic acid isoindolin-5-yl-bristamine, 5-(2-chloro-4,5-difluoro-benzoguanidino)-ιη-pyrazolecarboxylate Acid [3-ethoxy-5-U-ethoxycarbonyl-1-indenyl-ethyl)-pyridin-2-yl-nitramine, 5-(2-chloro-4, 5-difluoro-phenylhydrazine Hydrazinyl)-ιη-pyrazole-3 retinoic acid [3-ethoxy-5-(ethyloxycarbonyl-hydroxy-ethyl)-pyridin-2-yl-bristamine, 5-(2 -chloro-4,5-difluoro-phenylhydrazinoamino)-lH-pyrazole-3-retadic acid [5-(bucarboxy-1-indenyl-ethyl)-3-ethoxy-pyridine -5-(2-chloro-4,5-difluoro-phenylhydrazino)-1Η-pyrazole-3-decanoic acid [5-U-carboxy-1-hydroxy-ethyl )-3-ethoxy-pyridin-2-yl]-nonylamine ' 5-(2-gas-4, 5-difluoro-benzhydrylamino)-1Η-pyrazole 2-ylmethyl)-nonylamine, 5-(2-chloro-4,5-difluoro-phenylhydrazinoyl)-111_° ratio. -3-Resouric acid [6-(thiomorpholin-4-yl)-pyridin-3-ylmethyl]-decylamine, 5-(2- gas-4, 5-difluoro-benzoguanamine Base retinoic acid [6-(1,podiketo-1 λ 6-thiomorpholin-4-yl)-pyridine-3-ylmethyl]-acid amine, 5-(2-chloro-4, 5 -difluoro-phenylhydrazinoamino)-1Η-° ratio. sit _3-repulsive acid (4,5-dibromo-thiophen-2-ylmethyl)-decylamine, 5-(2-gas- 4, 5-Difluoro-benzylidenylamino)-lH-n ratio. Sit a 3-acidic acid (5-chloro-indol-2-ylmethyl)-bristamine, 5-(2-chloro -4, 5-difluoro-benzhydrylamino)-1Η-0 ratio biting a 3-tert-acid 318197 67 1322688 (4-ethyl-2-mercapto-oxazol-5-ylindenyl)- Indoleamine, 5-(2-chloro-4,5-difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid (2-ethyl-2-methyl-oxazole-4- Benthyl)-nonylamine dihydrochloride, 5-(2-chloro-4,5-difluoro-benzoindolyl)-1Η-pyrazole-3-carboxylic acid ([2, 2'] Dithiophene-5-ylindenyl)-nonylamine, 5-(2-chloro-4,5-difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid (3-methoxyl) -thiophen-2-ylindenyl)-nonylamine, 5-(2-chloro-4,5-difluoro-benzoindolyl)-1Η-pyrazole-3-carboxylic acid (4,5- Dioxo-thiophen-2-ylindenyl)-fluorene , 5-(2-chloro-4, 5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid (2,5-dimercapto-oxazol-4-ylindenyl) - decylamine, 5-(2-chloro-4, 5-difluoro-benzhydrylamino)-1 Η-pyrazole-3-carboxylic acid (2-hexyl-4-methyl-oxazole-5- Benthyl)-nonylamine, 5-(2-chloro-4,5-difluoro-benzylidenylamino)-1 oxime-carbazole-3-carboxylic acid (4-methoxy-thiophene-3- Benthyl)-nonylamine, φ 5-(2-chloro-4,5-difluoro-benzhydrylamino)-1Η-°biazole-3-carboxylic acid (4-mercapto-2-phenyl) 5-oxazol-5-ylmethyl)-nonylamine, 5-(2-chloro-4,5-difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid (2-oxime 4-phenyl-oxazole-5-ylindenyl)-nonylamine, 5-(2-chloro-4,5-difluoro-phenylhydrazino)-1Η-carbazole-3-carboxylate Acid (4-hexyl-2-methyl-oxazol-5-ylmethyl)-nonylamine dihydrochloride, 5-(2-chloro-4,5-difluoro-benzoinyl)- 1Η-°Bizozole-3-carboxylic acid (6-chloro-pyridin-3-ylindenyl)-nonylamine, 5-(2-chloro-4, 5-difluoro-benzylidenylamino)-1Η -carbazole-3-carboxylic acid 68 318197 1322688 (6-chloro-pyridin-3-ylindenyl)-decylamine dihydrochloride, 5-(2-chloro-4, 5-difluoro-benzoinyl Amino)-1Η-«biazole-3-carboxylic acid (4H -[1,2,4]triazol-3-ylindenyl)-nonylamine 5-(2-chloro-4,5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylate Acid (xian-[1,2,4]triazol-3-ylindenyl)-guanamine dihydrochloride, 5-(2- gas-4,5-difluoro-benzoinyl)- 1Η-pyrazole-3-carboxylic acid (5-fluoro-4H-quinazolin-3-yl)-decylamine 5-(2-gas-4, 5-difluoro-phenylhydrazino)-1Η -pyrazole-3-carboxylic acid H (5-fluoro-4H-quinazolin-3-yl)-nonylamine dihydrochloride, 5-(2-chloro-4,5-difluoro-benzoinyl) Amino)-1Η-pyrazole-3-carboxylic acid (4,6-dimercapto-pyridin-3-ylindenyl)-decylamine, 5-(2-chloro-4, 5-difluoro-phenylhydrazine Hydrazinyl)-1Η-°biazole-3-carboxylic acid (4,6-dimercapto-pyridin-3-ylmethyl)-guanamine dihydrochloride, 5-(2-gas-4, 5-difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid (2-decyloxy-6-mercaptopyridin-3-ylindenyl)-decylamine, φ 5-( 2-oxo-4,5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid (4-oximeoxy-6-indolyl-pyridin-3-ylindenyl)-oxime Amine, 5-(2- gas-4, 5-difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid (4-methoxy-6-mercapto-pyridin-3-yl) Methyl)-guanamine dihydrochloride, 5-(2-chloro-4, 5-difluoro- Mercaptoamino)-1Η-pyrazole-3-carboxylic acid (2-oxime-4,6-dimercapto-acridin-3-ylindenyl)-nonylamine, 5-(2-chloro -4,5-difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid (2-methoxy-4,6-dimethyl-pyridin-3-ylmethyl)-indole Amine dihydrochloride, 5-(2- gas-4,5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid 69 318197 1322688 (3-indolyl-pyridine-2- Methyl)-decylamine, 5-(2-wind_4, 5-fluoro-benzoylamino)-ιη_ο than 0-sodium-3-acid (5-mercaptobital -3-3-based Methyl)-nonylamine, 5-(2-chloro-4,5-difluoro-phenylhydrazinoamino)_ih-pyrazole-3-carboxylic acid (6-mercapto ratio -3-ylmethyl) ) - Amine, 5-(2- gas-4, 5-difluoro-phenylhydrazino) -ih-.嗤-3-carboxylic acid (6-fluorenylbi-2-ylindenyl)-bristamine, 5-(2-chloro-4,5-one gas_this arylamino group)-1Η_π ratio α sitting_ 3_slow acid•(pyridin-3_ylmercapto)-decylamine dihydrochloride, 5-(2-chloro-4, 5-difluoro-benzoylamino group than 嗤-3-televic acid ( 6-fluoro-° ratio -3-ylindenyl)-bristamine dihydrochloride, 5-(2-chloro-4, 5-difluoro-benzylidenylamino)-111-indoleazole- 3-carboxylic acid (3-recarbyl-phenyl)-mercapto-nonylamine, 5-(2-chloro-4, 5-difluoro-benzhydrylamino)-ih-pyrazole-3-carboxylate Acid 3-methanesulfonylamino-benzylamine, • 5-(2-chloro-4,5-difluoro-phenylhydrazino)-ih-pyrazole-3-carboxylic acid 4-methane Mercaptoamine-benzylamine, 5-(2-chloro-4, 5-difluoro-phenylhydrazino)-ih-pyrazole-3-carboxylic acid 3-acetamido-benzylamine ' 5-(2-Gas-4,5-difluoro-benzoquinone-based amino group ratio. Sit-3-remediate 4-acetamido-benzylguanamine' 5-(2-gas-4, 5 -difluoro-benzhydrylamino)-ΐΗ-η-pyrazole-3-carboxylic acid (2-phenyl-thiazol-4-ylindenyl)-decylamine, 5-(2-gas-4, 5 -difluoro-crackanylamino)-indole-pyrazole-3-carboxylic acid 1322688 ((R)-l-phenyl-ethyl)-decylamine, 5-(2- gas-4, 5- Difluoro-benzene Mercaptoamino)-1Η-pyrazole-3-carboxylic acid ((S)_l_phenyl-ethyl)-bristamine, 5-(2- gas-4, 5-difluoro-benzoguanamine -1 -pyridazole-3-carboxylic acid (6-phenoxypyridin-3-ylindenyl)-nonylamine dihydrochloride, 5-(2-mercapto-4, 5-difluoro- Benzylamino)-1Η-pyrazole-3-carboxylic acid (6-chloro-pyridin-3-ylindenyl)-guanamine dihydrochloride, 5-(2-chloro-4, 5-di Fluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid® (2-chloro-pyridin-3-ylmethyl)-decylamine dihydrochloride, 5-(2-mercapto-4 , 5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid (6-chloro-pyridin-3-ylindenyl)-nonylamine sodium salt, 5-(2-chloro-4 , 5-difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid [1-(pyridin-3-yl)-ethyl]-decylamine dihydrochloride, 5-(2- Gas-4, 5-difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid (2-fluoro-pyridin-3-ylmethyl)-guanamine dihydrochloride, φ 5- (2-Ga-4, 5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylic acid (2-methyl-pyridin-3-ylindenyl)-decylamine dihydrochloride , 5-(2-chloro-4,5-difluoro-benzoquinoneamino-3-carboxylic acid (biphenyl-3-ylindenyl)-bristamine 5 • 5-(2-chloro-4, 5-difluoro-benzoquinone Mercaptoamino)-1Η-pyrazole-3-carboxylic acid ((lR,2S)-2-hydroxy-indole-yl)-decylamine, 5-(2-chloro-4, 5-difluoro-benzene Mercaptoamine)-1Η-η-pyrazole-3-carboxylic acid ((lS,2R)-2-hydroxy-indole-bu)-guanamine, 5-(2-gas-4, 5-difluoro -benzoylamino)-1Η-pyrazole-3-carboxylic acid 71 318197 1322688 (6-phenyl-pyridin-3-ylindenyl)-decylamine dihydrochloride, 5-(2-gas- 4,5-Difluoro-benzylidenylamino)-1Η-pyrazole-3-carboxylic acid (6-fluorenyl-2-pyridin-3-ylindenyl)-decylamine hydrochloride, 5 -(2-Gas-4, 5-difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid benzyl-methyl-decylamine, 5-(2-chloro-4, 5- Difluoro-benzoguanidino)-1Η-«biazole-3-carboxylic acid benzamide, 5-(2-gas-4,5-difluoro-benzhydrylamino)-1Η-吼Oxazole-3-carboxylic acid phenyl-nonylamine, 5-(2- gas-4, 5-difluoro-benzylidenylamino)-1Η-°biazole-3-carboxylic acid methyl-phenyl- Amine amine ' 5-(2-chloro-4,5-difluoro-phenylhydrazino)-indole-pyrazole-3-carboxylic acid (chitin-1-yl)-nitramine, 5-(2) - gas-4, 5-difluoro-phenylhydrazinoamino)-1-pyridazole-3-carboxylic acid (4-ethoxycarbonyl-piperidin-1-yl)-decylamine, φ 5-(2 -chloro-4, 5-difluoro-benzene Mercaptoamino)-1Η-pyrazole-3-carboxylic acid (4-indolyl-piperidin-1-yl)-decylamine, 5-(2-gas-4, 5-difluoro-benzoinyl) Amino)-1Η-pyrazole-3-carboxylic acid (4-carboxy-piperidin-1-yl)-decylamine, 5-(2-chloro-4, 5-difluoro-benzhydrylamino) -1 Η-pyrazole-3-carboxylic acid phenethyl decylamine, 5-(2-chloro-4, 5-difluoro-phenylhydrazinoamino)-1 Η-pyrazole-3-carboxylic acid fluorenyl- Phenylethyl-decylamine, 5-(2-chloro-4,5-difluoro-phenylhydrazino)-1Η-η-pyrazole-3-carboxylic acid 72 318197 1322688 Ethyl-phenyl-decylamine , 5-(2-Chloro-4, 5-difluoro-benzhydrylamino)-pyrazole-3-monocarboxylic acid stupid (1,2,3,4-tetrahydroisoindolin-2-yl )--Amine, 5-(2-chloro-4, 5-difluoro-phenylhydrazinoyl H-pyrazole-3-carboxylic acid ((S) α-methoxy bupyl-nodal) Amine, 5-(2- gas-4, 5-difluoro-benzhydrylamino)_1Η-pyrazole_3_carboxylic acid ((R) (2-methoxyl-aryl)-nitramine , 5-(2-chloro-4, 5-difluoro-phenylhydrazinyl)_work η-ο比azole-3-carbic acid® benzene (1,2,3,4-tetrahydrophthalene-基基)--Amine, 5-(2-chloro-4, 5-difluoro-benzhydrylamino)_ιη-π than 〇3 carboxylic acid phenyl-propyl-decylamine, 5- (2-gas-4, 5 -difluoro-phenylhydrazinoamino)-1-indole-pyrazole_3_carboxylic acid butyl-phenyl-bristamine, 5-(2-chloro-4, 5-difluoro-benzoinylamino) ΐΗ _ pyrazole _3 monocarboxylic acid pentyl-phenyl-bristamine, Lu 5-(2-chloro-4, 5-difluoro-benzhydrylamino)- 1H-pyrazole-3_carboxylate Acid diphenyl decyl-decylamine, 5-(2- gas-4, 5-difluoro-phenylhydrazinylamino)-ih-pyrazole-3-carboxylic acid•(pyridin-2-ylindenyl) - guanamine hydrochloride, 5-(2-Gas-4, 5-difluoro-anthracenylamino)-ih-pyrazole-3-carboxylic acid (pyridin-4-ylindenyl)-decylamine Hydrochloride, 5-(2-chloro-4, 5-difluoro-anthracenylamino)-ih-pyrazole-3-carboxylic acid ((R)-2-yl-1-yl- Ethyl)-guanamine, 5-(2- gas-4, 5-difluoro-adolylamino)-ιη-〇 ratio. Sodium-3-acid 73 318197 1322688 ((S)-2-yl-1-phenyl-ethyl)-decylamine, 5-(2- gas-4, 5-difluoro-crackamine Base) -1Η-0 ratio 0 竣 一 甲基 甲基 甲基 甲基 节 节 节 节 节 节 节 节 节 节 节 节 节 节 节 节 节 节 节 节 节 节 节 节 节Furan-2-ylindenyl)-nonylamine, 5-(2-aero-4,5-difluoro-phenylhydrazino)-1Η-0-pyrazole-3-derivative (thiophen-2-yl) Indole, decylamine, 5-(2- gas-4, 5-difluoro-anthracenylamino)-1Η-0-pyrazole-3-carboxylic acid• (2-decyloxy-phenyl) - decylamine, 5-(2-chloro-4, 5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid (2-methoxy-phenyl)-indenyl- Amine, 5-(2-chloro-4, 5-difluoro-benzylidenylamino)-1H-pyrazole-3-carboxylic acid 4-didecylamino-benzylamine hydrochloride, 5- (2-Ga-4, 5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid 3-Amino-benzylguanamine, φ 5-(2-chloro-4, 5- Difluoro-benzylidenylamino)_1H-pyrazole-3-carboxylic acid 4-amino-benzylamine, 5-(2-gas-4, 5-difluoro-benzoinyl)- 1Η-pyrazole-3-deoxy acid 2-methyl-benzylamine, 5-(2-chloro-4, 5-difluoro-benzylidenylamino)-1Η-pyrazole-3-carboxylic acid 3 - methyl-section Amine, 5-(2-chloro-4, 5-difluoro-phenylhydrazino)-1Η-pyrazole-3-deoxyl 3-didecylamino-benzylamine, 5-(2- Chloro-4, 5-difluoro-benzylidenylamino)-1Η-carbazole-3-deoxy acid 318197 74 1322688 (2-anoxo-° ratio -3-ylindenyl)-nonylamine, 5-(2-chloro-4, 5-difluoro-phenylhydrazino)1H_pyrazole-carboxylic acid 2-chloro-benzylamine, 5-(2-chloro-4, 5-difluoro- Benzylguanidino H-pyrazole_3_carboxylic acid 3-gas ''branched amine, 5-(2-chloro-4,5-difluoro-phenylhydrazino)1Η-Πbazole-3 _carboxylic acid 3_oxime oxycarbonyl-benzylamine, 5-(2-chloro-4, 5-difluoro-phenylhydrazinoyl)-1Η-pyrazole-3-carboxylic acid _ 3-regiving-section Amine, 5-(2-chloro-4,5-difluoro-benzoindolyl)-1Η-pyrazole-3-carboxylic acid (6-trifluoromethyl-pyridin-3-ylindenyl)_ Indoleamine, 5-(2-chloro-4, 5-difluoro-phenylhydrazinyl hydrazine-obbazole -3-carboxylic acid (2-ethoxy-indolyl-3-ylindenyl) _ Amine, 5-(2-chloro-4, 5-difluoro-benzhydrylamino)_ιη-pyrazole-3-carboxylic acid (2-didecylamino-ethyl) monodecylamine, Lu 5-(2-Ga-4, 5-difluoro-phenylhydrazino)-indole-pyrazole-3-carboxylic acid ethyl-(2-didecylamino-B - indoleamine dihydrochloride, 5-(2- gas-4, 5-difluoro-phenylhydrazino)1Η-pyrazole-3-carboxylic acid% hexyl-(2-didecylamino) -ethyl)-bristamine, 5-(2-gas-4, 5-difluoro-benzoquinoneamino)-1Η-pyrazole_3_carboxylic acid (4-methoxy-β ratio bite- 2-ylindenyl)-bristamine, 5-(2- gas-4,5-difluoro-benzoindolyl)-1Η-pyrazole-3-carboxylic acid (2,6-didecyloxy) -pyridin-3-ylindenyl)-decylamine, 5-(2- gas-4,5-difluoro-phenylhydrazinoamino)_1Η-0-pyrazole-3-retiny 75 318197 1322688 2-曱Oxycarbonylcarbonyl-benzylamine, 5-(2-Gas-4, 5-difluoro-phenylhydrazino)-ih-pyrazole-3-carboxylic acid 2-carboxymethoxy-benzylhydrazine Amine, 5-(4,5-difluoro-2-methyl-benzylguanamine)_ih-pyrazole-3-carboxylic acid (6-decyloxypyran-3-ylmethyl)-nitramine, 5 -(2,4-·一乱-午牛胺)_1Η-π ratio 0 sitting-3-reaction acid (6-decyloxy-*»pyridin-3-ylindenyl)-nonylamine, 5-( 2-Chloro-4, 5-difluoro-phenylhydrazinoamino)-ιη-pyrazole-3-carboxylic acid® (3,5-dimethoxy-pyridin-4-ylmethyl)-decylamine , 5-(4,5-difluoro-2-methyl-benzylamine)-111-〇 ratio" sit-3-reaction acid (2,4-dimercapto-oxazol-5-ylmethyl) - indoleamine, 5_(2,4_one gas-tubergic amine than sputum-3_acid (2,4-dimercapto-oxazol-5-ylindenyl)-nonylamine, 5-(2 -Chloro-4,5-difluoro-adenylamino)-1Η-pyrazole-3-carboxylic acid (4-oximeoxycarbonyl-phenyl)-indenyl-decylamine, Lu 5-(2 -Chloro-4,5-difluoro-benzoamitoylamino)-1Η-pyrazole-3-carboxylic acid (4-sulfo-phenyl)-indolyl-decylamine, . 4-{[5-(2-Gas-4, 5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carbonyl]-indolyl-amino}-benzoic acid sodium salt, 5- (2-Ga-4, 5-difluoro-anthracenylamino)-1Η-pyrazole-3-carboxylic acid isopropyl-phenyl-bristamine, 5-(2-gas-4, 5- Difluoro-benzoguanidino)-1Η-pyrazole-3-carboxylic acid (ethoxymethyl-methyl)-styl-bristamine, 5-(2- gas-4, 5-difluoro-曱醯 曱醯 胺 ) Η Η 吡 吡 吡 吡 丄 丄 丄 丄 丄 丄 丄 丄 丄 丄 丄 丄 丄 丄 丄 丄 丄 688 688 688 688 688 688 688 688 688 688 688 688 688 688 688 688 688 688 688 688 688 -iH-pyrazole-3-carboxylic acid benzamide ' 5-(2, 4-dioxa-benzhydrylamino)_ih-pyrazole-3-carboxylic acid benzamide, 5- (2- Gas-5-fluoro-benzyl-mercaptoaminopyrazole-3-carboxylic acid benzamide, 5-(2-gas-4,5-difluoro-benzoguanidino)-1Η-β-pyrazole A 3-benzoic acid® ¥yl-phenyl-bristamine, 5-(2-gas-4, 5-difluoro-benzhydrylamino)_ιΗ-pyrazolecarboxylic acid (1-methyl-1- Phenyl-ethyl)-nonylamine, 5-(2-chloro-4,5-difluoro-benzylidenylamino)-ιη-pyrazole-3-carboxylic acid [2-keto-2-(carboxylic acid) Piperidin-1-yl)-iethyl]-phenylmonodecylamine, 5-(5-fluoro-2-methyl-benzylidenylamino)-ih-pyrazole-3-carboxylic acid benzyl Amine, 5_(5-gas-2-fluorenyl-benzoquinoneamino) ΐΗ-η ratio 0 sitting -3 - decanoic acid, 5-(4-methoxy-2-methyl-benzene Methionylamino)_ιη-pyrazole-3-carboxylic acid benzamide, 5-(4-chloro-2-indolyl-benzhydrylamino)-1-pyrazole-3-carboxylic acid benzidine Amine, 5-(5-fluoro-2-methoxy-benzhydrylamino)_^ fj-pyrazole-3-decanoic acid benzylamine, 5-(5-Ga-2-methoxy- Benzyl arylamino) _^|_0 〇 一 3 3 3 3 3 3 77 77 77 77 77 δ δ δ δ δ δ δ δ δ δ δ δ δ δ δ δ δ δ δ δ δ δ δ δ δ δ δ δ δ δ δ a pyrazole_3_carboxylic acid (2-ethoxy-ethyl)-styl-decylamine, 5-(2-fluoro-5-methyl-benzhydrylamino)-indolyl-pyrazole- 3-carboxylic acid benzamide, 5-(5-vapor-2-fluoro-phenylhydrazinoamine 1Η_β-pyrazole_3_carboxylic acid benzamide, 5-(3-gas-2, 6-difluoro Monophenylhydrazinyl)-1-indole-pyrazole-3-carboxybenzamide, 5-(2- gas-3-fluoro-phenylhydrazinoamine; hydrazine-pyrazole-3-carboxylate Amine, 5-(2-Gas-4, 5-difluoro-benzhydrylamino)-ιη-pyrazole-3-carboxylic acid ethylaminomethylmercaptomethyl-phenyl-decylamine, 5 -(2-Ga-4, 5-difluoro-benzhydrylamino)- Ιη-pyrazole-3-carboxylic acid isobutyl-phenyl-decylamine, 5-(2-gas-4, 5-difluoro-phenylhydrazinoyl)-indole-pyrazole-3-carboxylic acid (2-oxocarbonylethyl)-phenyl-decylamine, 5-(2- gas-4, 5-difluoro-phenylhydrazinoyl)-lH-pyrazole-3-carboxylic acid (3- Ethoxycarbonyl-propyl)-phenyl-decylamine 5-(2-chloro-4,5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid (2-vvyl) -ethyl)-phenyl-bristamine, 5-(2- gas-4,5-difluoro-m-decylamino)-1Η-pyrazole-3-carboxylic acid (3-recarbyl-propyl) )-Phenyl-bristamine, 5-(2-hydroxy-4-decyloxy-benzoylamino)-1Η-pyrazole-3-carboxy 78 318197 1322688 benzyl amide, 5_(2- Hydroxy _5-decyloxy-phenylhydrazinoamino)-lH -11 than bite-3_budic acid benzamide, + 5-(5-fluoro-2-hydroxy-phenylnonylamino)- 1Η-pyrazole-3 acylic acid decylamine, 5-(4-fluoro-2-trifluoromethyl-benzhydrylamino)-lH-benzyl benzyl hydrazide, 5-(5-fluoro -2-trifluoromethyl-benzimidyl® acid, decylamine, 5-(2-chloro-4, 5-difluoro-benzhydrylamino)-1Η-ΰΛ bite one (2-曱oxy-ethyl)-phenyl-decylamine, 5-(2,5-dimethyl-benzhydrylamino)-1Η- Oxazol-3-pyranic acid amylamine 5-(2-chloro-5-mercapto-phenylhydrazino)-1Η-pyrazole-3 although acid segment j 5_(2-chlorobite bite- 3-monoamino)-1Η-β ratio α--3-slow acid saponin 5 -(4-gas ratio bitent-2-weirylamine group)-1Η-σΛα sit -3-.  -(2,6-dichloro-π ratio -3- ylamino)-1Η-° ratio cough octylamine amine carboxylic acid benzyl 3-carboxylic acid carboxylic acid % benzyl hydrazine 5-(2 - gas-4, 5-difluoro-abidomethylamino)-1Η~<butyl-(4-ethoxyxo-phenyl)-bristamine, 5-(2-gas-4, 5 -difluoro-benzhydrylamino)-1 hydrazine, % butyl-(4-mercapto-phenyl)-decylamine, 5-(2-methyl-pyridine-3-carbonylamino)-1Η -pyrazole, 3 318197 79 1322688 amine, 5-(2-chloro-6-mercapto-pyridine-3-carbonylamino)-1 Η-pyridinium, benzamidine, carboxy 55-(3-gas- Pyridine-4-carbonylamino)-1Η-pyrazole-3-carboxylic acid 卞 卞 ,, 酉 酉 5 5 5 5 5 5 5 5 5 5 5 5 5 5 5 5 5 5 5 5 5 5 5 5 5 5 5 5 ° ratio 嗓~3 butyl-(4-ethoxycarbonylmethyl-phenyl)-decylamine, carboxylic acid 5_(2-dis-4,5-difluorobenzoylamino)-1Η-β唉~& Butyl-(4-carboxyindenyl-phenyl)-decylamine,

5-(2-chloro-4,5_digas-benzoquinoneamino)-1Η-β ratio (4-oxocarbonyl-phenyl)-(2-methoxy-ethyl)-decylamine , 5-(2-chloro-4,5-difluoro-benzhydrylamino)-1Η-η-Bistazole~(4_Rexyl-phenyl)-(2-decyloxy-ethyl)- Amine amine, 5_(2- gas-4, 5-difluoro-benzofuranylamino)-1Η_ο than salivation acid (6-decyloxy-pyridin-3-ylmethyl)-guanamine dihydrochloride Salt, 5-(2-methyl-4,5-difluoro-benzoylamino)-1Η-η ratio. Sit __3__acid (6-decyloxy-pyridin-3-ylmethyl)-guanamine dihydrochloride, 5-(2- gas-4, 5-difluoro-benzoinyl) -1Η-pyrazole-3-succinic acid (thiazol-4-yl-methyl)-guanamine dihydrochloride, 5-(2- gas-4, 5-difluoro-benzhydrylamino)- 111-° ratio ° -3- acid 4-[2-(morphin-4-yl)-ethylamino aryl]-tyrosamine dihydrochloride, 5-(2-gas-4 , 5-difluoro-phenylhydrazinoamino)-111-0 ratio ° -3-acid acid 4_(morpholin-4-ylaminoguanidino)-benzylguanamine dihydrochloride, [4 -({[5-(2-chloro-4,5-difluoro-benzhydrylamino)-111-pyrazole-3-carbonyl]-amino}-indenyl)-phenyl hydrazino] -Sodium acetate, 80 318197 1322688 3-[4-({[5-(2-Gas-4, 5-difluoro-phenylhydrazino)-1 Η-pyrazole-3-carbonyl]-amine (5-(2-gas-4, 5-difluoro-benzhydrylamino)-lH-pyrazole-3-carboxylate Acid (3,5-dimethyl-isoxazol-4-ylmethyl)-decylamine hydrochloride, [5_(2-gas-4,5-mono-benzoylamino)_111_11 〇 Sitting -3_slow acid (1, 3, 5_tridecyl-1Η-° than sal-4-ylindenyl)-guanamine dihydrochloride, 5-(2-gas-4, 5-difluoro -benzoquinone Mercaptoamine)-1Η-pyrazole-3-carboxylic acid (3,5-dimercapto-isoxazole-4-ylindenyl)-guanamine sulfonate, 5-(2-gas-4 ,5-difluoro-benzoammonylamino)-111-indole 嗤-3-glycol 3-(2-(morpholin-4-yl)-ethylaminomethylindenyl]-benzylguanamine Dihydrochloride, 5-(2-Gas-4, 5-difluoro-phenylhydrazino)-1Η-indazole-3-carboxylic acid 3-(morpholin-4-ylaminocarbazinyl) )-benzylguanamine dihydrochloride, 5-(2- gas-4,5-difluoro-benzhydrylamino)-1Η-° ratio 坐-3-敌酸{2-[2-( Morpholin-4-yl)-ethylaminomethylindenyl]-pyridin-4-ylmethyl}monodecylamine trihydrochloride, 5-(2- gas-4,5-difluoro-phenylhydrazine Aminoamino)_1Η-σϋ°Sodium-3-o-acid [2-(N-Phen-4-ylaminocarbamimidyl)-°-precipitated 4-ylmethyl]-nitramine trihydrochloride, 5 -(2-chloro-4,5-difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid (6-decyloxy-pyridin-3-ylmethyl)-decylamine sulfonate Acid salt, 5-(2- gas-4,5-difluoro-benzoquinone-based amino-sodium-3-o-acid (6-decyloxy-pyridine-3-ylmethyl)-decylamine hemisulfate , 5-(2-chloro-4, 5-difluoro-benzylidenylamino)-1Η-η-pyrazole-3-carboxylic acid (3,5-dimethoxy-pyridin-4-ylmethyl) )- Indoleamine dihydrochloride, \. 81 318197 1322688 5-(2-chloro-4, 5-mono-benzoinyl)-iH-. η 竣-3-decanoic acid (4-aminomethyl-pyridin-2-ylmethyl)-decylamine trihydrochloride, 5-(2- gas-4,5-·-gas-benzoquinone胺 ) ΐΗ η η _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ -Benzyl arylamino-acid (6-a-pyridin-3-ylmethyl)-decylamine dimethanesulfonate, 5-(2-chloro-4,5-a-L-benzoquinone Amino group)-1Η-° ratio. Sodium-3-o-acid (2,4-dimethyl-pyridin-3-ylindenyl)-decylamine hydrochloride, ® 5-(2-chloro-4, 5-difluoro-benzhydrylamino)-lH-pyrazole-3-hypoacid (pyridin-3-ylindenyl) monodecylamine hydrochloride, 5-(2-chloro-4,5- Fluoro-benzoylamino)-1Η_〇 than sal-3-reaction (6-methoxy-n-pyridin-3-ylindenyl)-propyl-decylamine dihydrochloride, 5- (2-Chloro-4,5-fluoro-benzoguanidino)-1Η_ο than sal-3-actic acid [6-(piperidin-bu)-pyridin-3-ylindenyl]]-decylamine Dihydrochloride, 5-(2-chloro-4,5-·-fluoro-stupylamino)-1Η-π than 嗤--3-acidic acid [6-(morpholin-4-yl) -pyridin-3-ylmethyl]]-nonylamine dihydrochloride, 5-(2-chloro-4,5--disorganized-benzoquinoneamino-3 Acid (3,5-diox ratio -4-mercapto)-decylamine hydrochloride, 5-(2-chloro-4,5--fluoro-benzoylamino)-1Η-πΛ^- 3-dihydro acid (6-didecylamino-pyridin-3-ylindenyl)-nonylamine dihydrochloride, 5-(2-chloro-4,5-difluoro-benzofuranylamino )-1Η-πΛ^-3-acid (6-diamidino-pyridin-3-ylmethyl)-propyl-guanamine dihydrochloride, 5-(2- gas-4, 5- Di-I-benzamide amino)-1Η-π than saliva-3-carboxylic acid (6-diethylamino-pyridin-3-ylindenyl)-decylamine dihydrochloride,

318197 82 1322688 5-(2-Gas-4,5-difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid (6-Gas-2-didecylamino-pyridine-3 - fluorenyl)-nonylamine dihydrochloride, 5-(2- gas-4,5-difluoro-benzhydrylamino)-1 fluorene-carbazole-3-carboxylic acid (4-[1, 2,3]thiadiazol-4-yl-benzyl)-indolamine hydrochloride, 5-(2-chloro-4,5-difluoro-benzhydrylamino)-1Η-η-pyrazole- 3-carboxylic acid (4-mercapto-thiazol-5-ylindenyl)-indolyl hydrochloride, 5-(2- gas-4, 5-difluoro-benzoguanidino)-1H-pyrazole 3-carboxylic acid (2,4-dimercapto-thiazol-5-ylindenyl)-guanamine hydrochloride,

5-(2-chloro-4,5-difluoro-phenylhydrazinylamino)-1Η-pyrazole-3-carboxylic acid [6_(4-carbyl-Brigade bite_1_yl)_π比唆_ 3_ylmercapto]-bristamine dihydrochloride, 5-(2-chloro-4,5-difluoro-benzoindolyl)-1Η-pyrazole-3-carboxylic acid 5-mercapto- Pyridox-2-ylindoleamine dihydrochloride, 5-(2- gas-4, 5-difluoro-phenylglycosylamino)_1Η-β than 0--3-reoquinol-5- Base amine dihydrochloride, 5-(2-chloro-4, 5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylic acid quinoline-8-ylguanamine dihydrochloride Salt, 5-(2-chloro-4, 5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylic acid isoquinolin-5-ylguanamine dihydrochloride, 5-( 2- gas-4,5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid [6-(4-mercaptopiperazin-1-yl)-pyridin-3-ylindole ]]-nonylamine dihydrochloride, 5-(2-chloro-4,5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylic acid [6-(4-didecyl) Amino-piperidin-1-yl)-pyridin-3-ylindenyl]-nonylamine dihydrochloride, 5-(2-gas-4, 5-difluoro-benzhydrylamino)-1Η - «Bizozole-3-carboxylic acid 83 318197 1322688 [6-(β 比洛 bit-1-yl)-° ratio -3-ylmethyl]-nitramine dihydrochloride, 5-(2-chloro -4, 5-difluoro-benzoquinone Amino)-ih-pyrazole-3-carboxylic acid (σ-pyridin-2-ylindenyl)-nitramine dihydrochloride, 5-(2- gas-4, 5-difluoro-benzhydryl) Amino)-ιη-pyrazole-3-buffer acid [6-(thiophene-4-yl)-n ratio -3-ylindenyl]-bristamine dihydrochloride, 5-(2- Gas-4, 5-difluoro-benzhydrylamino)-!Η-pyrazole-3-resorcinic acid [6-(1,1-dione-116-thio-indol-4-yl) -° ratio -3-methylmethyl] decylamine dihydrochloride, • 5-(2-Gas-4, 5-difluoro-benzhydrylamino)-indole-pyrazole-3- Acid amine fluorenyl decyl-nonylamine, 5-(2,4-branched-5-fluoro-phenylglycosylamino)-1 Η-β than wow-3-acid (4-aminocarba Mercapto-phenyl)-methyl-decylamine, 5-(2,4-dioxa-5-fluoro-benzhydrylamino)-lH-pyrazole-3-hydantosyl-(4- Mercaptoamine-based broth-phenyl)-bristamine, 5-(2,4-di-milk-5-gas-benzoylamino)-1Η-° than salivary-3-reoacid φ (4 -didecylaminoindenyl-phenyl)-fluorenyl-decylamine, 5-(2-gas-4,5-difluoro-benzoquinoneamino)-111-〇 〇 -3-3 - slow acid (4-methylsulfonylaminocarbonyl-phenyl)-mercapto-nonylamine, 5-(2-chloro-4,5-difluoro-phenylhydrazino)-1H-pyrazole 3-carboxylic acid (4-anthracenylaminocarbonyl-phenyl)-mercapto-guanamine sodium salt, 5-(2- gas-4, 5-difluoro-benzhydrylamino)_1H -pyrazole-3-carboxylic acid (4-cyano-phenyl)-methyl-bristamine, 5-(2-chloro-4,5-difluoro-benzylidenylamino)_1H-pyrazole- 3-carboxylic acid decyl-[4-(4Η-[1,2,4]triazol-3-yl)-phenyl]-decylamine hydrochloride, 84 318197 1322688 5-(4-layer-2 - gas-5-fluoro-benzamide amino group) -1 Η-σ ratio. Benzyl-o-acid (4-cyano-phenyl)-methyl-decylamine, 5-(4-azido-2-a-5-fluoro-crackamine)-1Η-pyrazole- 3-carboxylic acid methyl-[4-(1Η-tetrazol-5-yl)-phenyl]-decylamine, 5-(2- gas-4, 5-difluoro-benzhydrylamino)- lH-pyrazole-3-carboxylic acid [4-(Ν-hydroxyaminocarbamicimin fluorenyl)-phenyl]-methyl-decylamine, 5-(2- gas-4, 5-difluoro- Benzoylamino)-indole-pyrazole-3-carboxylic acid fluorenyl-[4-(5-keto-2,5-dihydro-[1,2,4]oxadiazol-3-yl )-phenyl] •-chatoletamine, 5-(2-gas-4, 5-difluoro-benzhydrylamino)-ih-pyrazole-3-carboxylic acid {4-[(2, 2- Dimethyl-propenyloxy)-nonyloxycarbonyl]-phenyl-p-decyl-decylamine, 5-(2- gas-4, 5-difluoro-phenylhydrazino)-ih-pyrazole-3- 4-[N-decyloxy-thiocarbonyloxy]-aminocarboximimine] carboxylic acid]-mercapto-nonylamine, 5-(2-3⁄4-4, 5-fluoro-benzazole Amino group is more than salino-3-glycolyl-[4-(5-thioketo-4,5-dihydro-[1,2,4]oxadiazol-3-yl)-phenyl]- Indoleamine, 5-(2-chloro-4, 5-difluoro-stupylamino) than salivary 3-methyl-acid methyl-[4-(5-keto-4, 5-dihydro-[ 1,2,4]thiadiazol-3-yl)-phenyl]-bristamine, 5 (2 Milk 4,5 - rat _ 曱 基 基 ) ΐΗ β β β β 唾 唾 唾 - 3- 3- 4- 4- 4- 4- {4-[1-(cyclohexyloxy-carbonyloxy)-ethoxycarbonyl]-phenylhydrazine _曱基_醯amine, 5-(2-chloro-4,5-fluoro-benzylamino)-ΐΗ-<» than salino-3-acid 318197 85 1322688 (4-ethoxycarbonyl-thiazole -2-yl)-ethyl-decylamine, 5-(2-chloro-4, 5-difluoro-benzoquinoneamino)-1Η-° than sal-3-actic acid 2-nonylsulfonylamine Base-benzylamine, 5-(2-gas-4,5-diox-branched amine group. sit-3-sodium acid 2-acetamido-benzylamine, 5-(2-gas -4, 5-Difluoro-benzoylamino)-1Η-n ratio "• sitting-3-o-acid 2-(dimethylamino-methyleneamino)-benzylamine hydrochloride , 5-(2-Gas-4, 5-difluoro-phenylhydrazino)1Η-pyrazole-3-carboxylic acid® 3-(dimethylamino-ylideneamino)-benzylhydrazine Amine hydrochloride, 5-(2-chloro-4, 5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylic acid 4-(dimethylamino-arylene) )-benzylguanamine hydrochloride, 5-(2- gas-4, 5-difluoro-phenylhydrazino)1Η-pyrazole-3-carbamic acid 2-[1-(didecylamino) Ethyleneamino]-benzylguanamine dihydrochloride, 5-(2- gas-4, 5-difluoro-benzoguanamine )-1Η-pyrazole-3-carbamic acid 3-[1-(didecylamino)ethylidene]-benzylguanamine dihydrochloride, 5-(2- gas-4,5-di Fluoro-phenyl fluorenylamino)-1Η-η ratio salicin-3-3-acid 4-[1-(dimethylamino)ethylamino]-benzylguanamine dihydrochloride, 5-( 2-Chloro-4,5-difluoro-benzhydrylamino)_1Η-σ ratio 嗤~3 -2,2-acidic 2-(diethylamino-methyleneamino)-benzylguanamine dihydrochloride Salt, • 5-(2-Gas-4, 5-difluoro-benzoylamino)-1Η-° ratio. 3-oxo acid 3-(diethylamino-methyleneamino)-benzylguanamine dihydrochloride, 5-(2- gas-4, 5-difluoro-benzofuranylamino )- 1Η-〇 than sal-3-actic acid 4- (diethylamino-ylideneamino)-benzylguanamine dihydrochloride, 5-(2-chloro-4, 5-difluoro- Benzoylamino)-111-indole 嗤-3-carbamic acid 318197 86 1322688 2-Iminoethylamino-benzylguanamine dihydrochloride, 5-(2-chloro-4,5-di Fluoro-benzoquintonylamino)-111-indole 〇 sitting-3-oxo acid 3-imine ethylamino-benzylamine dihydrochloride, 5-(2- gas-4, 5-di Fluorobenzoylamino)-1Η-β ratio 0--3-sodium 4-imidoethylamino-benzylamine dihydrochloride, 5-(2- gas-4,5-di Fluoro-benzoquinone-based amine)-1Η-β ratio 0--3-s-acid 4-cyano-benzylamine, 5-(2-chloro-4,5-difluoro-benzofuranylamino )-1Η-°ϋσ sit-3-reaction acid Φ 3-[(2-fluoro-benzylidene iminyl)-amino]-benzylamine hydroiodide, 5-(2-gas-4, 5-difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid 4-[(2-fluoro-iminophenylphenyl)-amino]-benzylamine hydroiodide, 5_ (2_gas-4,5-diqi-benzoquinone-based amine group)-1Η_0 ratio 0 sitting_3_rebel acid 3- (3,3_two Sulfhydryl-yl)-pyristylamine 5-(2-chloro-4,5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid 4- (3,3-di Methyl-ureido)-benzylamine, φ 5-C2-gas-4, 5-difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid 2-(toluene-4-sulfonate醯Amino)-benzylamine, 5-(2-Gas-4,5-difluoro-phenylhydrazinoamino)_1H-pyrazole-3-carboxylic acid 2-Amino-6-fluoro-benzazole Amine hydrochloride, - 5-(2-Gas-4, 5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylic acid 2-Amino-4, 5-difluoro-benzyl Indoleamine hydrochloride, 5-(2- gas-4, 5-difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid (indoline-1-yl)-bristamine, 5-(2-Gas-4, 5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid 87 318197 1322688 (indoline-2-yl)-decylamine, 5-( 2-Gas-4,5-difluoro-benzoquinoneamino)1Η-β ratio. Benzene-acid (411-啥嗤琳-3-yl)-Siamine, * 5-(2-Ga-4, 5-difluoro-phenylhydrazino)-1Η-carbazole-3 -carboxylic acid (4H-quinazolin-3-yl)-guanamine dihydrochloride, 5-(2- gas-4,5-difluoro-phenylhydrazino)-1Η-η-r-azole- 3-carboxylic acid (7-fluoro-4H-quinazolin-3-yl)-nonylamine dihydrochloride, 5-(2-chloro-4,5-difluoro-phenylhydrazinoaminopyrazole- 3-carboxylic acid • (6-fluoro-4-indolyl-quinazolin-3-yl)-indolyl hydrochloride, 5-(2-chloro-4, 5-difluoro-benzoinyl)-1Η -pyrazole-3-carboxylic acid (2-ethoxy-2-indolyl-1,4-dihydro-2-indole-quinazolin-3-yl)-decylamine, 5-(2- gas-4, 5-difluoro-phenylhydrazinoamino)-1Η-indazole-3-carboxylic acid (2-cyanopyridin-4-ylindenyl)-decylamine, 5-(2-chloro-4, 5 -difluoro-phenylhydrazinoamino)-1 Η-pyrazole-3-carboxylic acid [2-(Ν-hydroxyamino)imine fluorenyl)-pyridin-4-ylmethyl]-decylamine, φ 5-(2-Chloro-4, 5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylic acid [2-(5-keto-4, 5-dihydro-[1 , 2, 4]oxadiazol-3-yl)-pyridin-4-ylindenyl]-decylamine, 4-{[5-(4, 5-difluoro-2-methyl-benzoguanamine) )-1Η-pyrazole-3--carbonyl]-mercapto-amino}-benzoate , 5-(4,5-difluoro-2-methyl-phenylhydrazino)-1Η-pyrazole-3-carboxylic acid fluorenyl-[4-(1Η-tetrazol-5-yl)- Phenyl]-nonylamine, 5-(2,4-dichloro-benzoguanidino)-1Η-pyrazole-3-carboxylic acid (pyridin-3-ylmethyl)-decylamine, 88 318197 1322688 5 -(2,4-dichloro-5-fluoro-benzamideamino)-1H-pyrazole-3-carboxylic acid (pyridyl-3-ylmethyl)-nitramine, 5-(2,6-di Gas-5-fluoro-» than biting 3-carbonylamino)_111-° ratio of sitting--3-lower acid than biting-3-ylindenyl)-bristamine, 5-[(3-gas-benzo) [b]Thiophene-2-carbonyl)-amino]-1H-pyrazole-3-derivative (pyridin-3-ylmethyl)-decylamine, 5-[(3- gas-thiophene-2-carbonyl) -amino]-1H-pyrazole-3-carboxylic acid (pyridyl-3-ylmercapto)-nonylamine, 5-phenylhydrazinoamino-1H-pyrazole-3-carboxylic acid (pyridine_3 -ylmethyl)-nonylamine, 5-phenylethylamino-1H-pyrazole-3-carboxylic acid (pyridin-3-ylindenyl)-nonylamine, 5-(2-indolyl-4, 5-difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid (pyridin-3-ylindenyl)-decylamine dihydrochloride, 5-(2-amino-4, 5 -difluoro-benzoguanamine)-1Η-pyrazole-3-carboxylic acid

Specific bite-ylmethyl)-bristamine' 5-(4,5-difluoro-2-indolesulfonylamino-benzimidamide)-1Η-pyrazole-3-carboxylic acid (pyridine-3-曱 ))-nonylamine ' 5-(2-acetamido-4, 5-difluoro-benzamide MH-pyrazole-3- oxo acid (〇 咬-3-yl fluorenyl) - Stearic amine ' 5-[(3,4,5-trichloro-nonyl-2-ylamino)] 嗤-3-decanoic acid (〇 咬-3-yl fluorenyl)- guanamine ' 5 -(4,5-difluoro-2-methyl-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid (2-cyano-0pyridin-4-ylindenyl)-decylamine ' 89 318197 丄5-(4, 5-Difluoro-2-methyl-benzylidenylamino)_1H-pyrazole_3_carboxy•acid [2-(1H-tetrazol-5-yl)- Pyridin-4-ylmethyl]-decylamine, and pyrazole-3,5-dicarboxylic acid 3-benzylguanamine 5-[(2,4-dichloro-phenyl)-decylamine], 21 A pharmaceutical composition comprising a pharmaceutical composition for treating or preventing diabetes according to any one of the above items i to 2, in combination with another therapeutic or prophylactic agent for diabetes. Another therapeutic or prophylactic agent for diabetes is Tengdaosu preparation (injection), low molecular weight insulin oral preparation, and continuous urea stimulant SU preparation), non-sulfonylurea insulin activator, potassium-dependent ATP (KATP) channel opener, alpha glucosidase inhibitor, alpha amylase inhibitor, insulin sensitizer, low molecular tGLp i receptor agonist , tGLP-1 peptide analog, dipeptidyl peptidase IV (Dpp_IV) inhibitor, glycosaminoglycan receptor antagonist, glucocorticoid receptor antagonist, biguanide, SGLUT inhibitor, fructose-1,6 -Deuterium phosphatase (FBPase) inhibitor, hepatic synthase spring kinase 3 (GSK-3) inhibitor, phosphoenolpyruvate carboxylic acid kinase (pEPCK) inhibitor, protein tyrosine phosphatase 1B (pTPaselB) inhibition Agent, SHTP2 inhibitor of SH2, hepatic phosphatase (gp) inhibitor, glucokinase activator, GPR40 receptor agonist, pyruvate dehydrogenase kinase (PDHK) Inhibitor, glutamine: fructose-6-phosphate aminotransferase (GFAT) inhibitor, antioxidant, nitric oxide scavenger, carnitine palmitoyl transferase 1 (CPT-1) inhibitor, growth hormone releasing factor (GHRF), trimercaptoglycerol lipase (hormone sensitive lipase) inhibitor, ppARr receptor Agent, PPAR 7 receptor antagonist, ppAR α / r receptor agonist, AMP-activating protein 90 318197 1322688 plasmin kinase (AMPK) activator, liposome receptor agonist or; δ 3 adrenergic receptor agonist The medicament according to the above item 21 or 22, wherein the other therapeutic or prophylactic agent for diabetes is insulin, tolbutamide, glycocyramide, and acitretin (acetohexamide), chlorpropamide, glybuzole, glibenclamide, gliclazide, glimepiride, mitige丽尼得_ (mi t igl inide), repagi inide, nategl inide, VOgHbose, acarbose, mig Migiitol, rosiglitazone cis-succinate, metformin hydrochloride, pi〇glitazone hydrochloride or buffing ( Buformin) hydrochloride. A pharmaceutical composition comprising a pharmaceutical composition for treating or preventing diabetes according to any one of the preceding paragraphs to 2, in combination with another therapeutic or prophylactic agent for diabetic complications. 25. According to the aforementioned 24 cases of diabetes, wherein the other diabetic remedy comprises a therapeutic or prophylactic agent such as a protein kinase (pKC/5) inhibitor, a vasopressin 11 morphogen antagonist, an aldose reductase inhibitor, An vasopressin converting enzyme (ACE) inhibitor, an advanced glycation end product (AGE) manufacturing inhibitor, a neuropathy therapeutic, or a diabetic neuropathy therapeutic. 26. According to the aforementioned item 24 or 25, the diabetes of the * + > β is produced, wherein the other therapeutic or prophylactic agent for diabetes is epal 牦 匕 匕 ep ep (epalrestat), mexiletine 318197 1322688 (mexile^ine) hydrochloride or imidaprii hydrochloride. A pharmaceutical composition comprising a pharmaceutical composition for treating, treating or preventing diabetes according to any one of items 1 to 20 above, in combination with another therapeutic or prophylactic agent for hyperlipemia. 28. The drug according to the aforementioned item 27, wherein the other therapeutic or prophylactic agent for hyperlipemia is fibrate (; ppARa receptor agonist), ppAR styling agonist, microsome three Acid glyceride transfer protein (MTP) inhibitor, cholesterol ester transfer protein (CETP) inhibitor, statin ® (HMG-CoA reductase inhibitor), anion exchanger, probucol, smoke Alkali drugs, phytosterols, lipoprotein _A1 (Apolip〇protein-Al) inducer, lipoprotein lipase (LpL) activator, lipase inhibitor of endothelial cells, ezetimibu, IBAT inhibitor, squalene synthetase inhibitor, ACAT inhibitor, LXR receptor agonist, FXR receptor agonist, FXR receptor antagonist or adenosine M agonist. Lu 29. According to the drug of item 27 or 28, the other therapeutic or prophylactic agent for hyperlipemia is cl〇f ibrate, bezafibrate, Finofiber ( Fenofibrate), lovastatin, simvastatin, pravastatin, fiuvastatin, atorvastatin , pitavastatin, rosuvastatin, cerivastatin, cholestyramine, colestyramine, tocopherol nicotine Acid ester, nicom〇i, 92 318197 1322688 Niceritrol, soy sterol (s〇yster〇1) or orizanol. • A pharmaceutical composition comprising a pharmaceutical composition for treating or preventing diabetes according to any one of the preceding paragraphs to 2, in combination with another therapeutic or prophylactic agent for obesity. 31. The medicament according to the above 30, wherein the another therapeutic or prophylactic agent for obesity is a leptin preparation, a pancreatic lipase inhibitor, a norepinephrine-serotonin reuptake inhibitor, a cannabinoid receptor antagonist, a single Amine reuptake inhibitors, • Dimercaptoglycerol-glycosyltransferase (DG AT) inhibitors, glucose-dependent membrane glycoprotein (GIP) receptor antagonists, leptin receptor agonists, and alizarin receptors Subtype 3 (BRS-3) agonist, periiipin inhibitor, acetyl-CoA carboxylase 1 (ACCl) inhibitor, acetyl-C〇A carboxylase 2CACC2) inhibitor , fatty acid synthase inhibitor, sn-di-decyl-glycerol-3-phosphate thiotransferase (AGPAT) inhibitor, trypsinase A2 (pPLA2) inhibitor, melanocortin (MC) receptor agonist, neuropeptide Υ5(ΝΡΥ5) receptor antagonist, non-φ coupling protein (UCP) inducing agent or activator, carnitine palmitoyl transferase 1 (CPT-1) activator, CCK1 (CCKA) agonist, ciliary nerve function Factor (CNTF), CRF2 agonist, neuropeptide Υ2 (ΝΡΥ2) receptor antagonist, neuropeptide Y4 (NPY4) receptor antagonist, thyroid hormone receptor A beta agonist, a growth hormone, a citrate citrate degrading enzyme inhibitor, a 5-ΗΤ6 antagonist or a 5-HT2C agonist. 32. The medicament according to the aforementioned item 30 or 31, wherein the other therapeutic or prophylactic agent for obesity is alizarin, oristat, sibutramine, rimonabant Or a medicinal composition for treating or preventing diabetes according to any one of the above items 1 to 20, and another treatment for hypertension or A combination of prophylactic agents. 34. The medicament according to the above item 33, wherein the other therapeutic or prophylactic agent for hypertension is thiazide diuretic, thiazide diuretic, loop diuretic, potassium retention diuretic, point block Agent, alpha, 10,000 blocker, alpha blocker, central paternal nerve inhibitor, peripheral sympathetic inhibitor (snake root wood agent), mom antagonist (benz〇thiazepin), antagonism Agent (dihydroacridine), vasodilator, angipertensin (ACE) inhibitor, vasopressin η receptor antagonist' nitrate preparation, endothelin receptor antagonist, Endothelin-converting enzyme inhibitor, neprilysin inhibitor, prostaglandin, prostanoid FP agonist, renin inhibitor, N〇S3 performance enhancer; shovel cyclin (prostacycl In) an analog, a diesterase v (pde5A) inhibitor, a prostacyclin analog or an aldosterone antagonist. 35. According to the shovel 33 or 34 of the drugs, the other treatment or preventive agent for hypertension is hydrochlorothiazide, trichlormethiazide, Banhai with Closset ( Bentylhydrochlorothiazide), meticrane, indapamide, tripamide, chlortalidone, mefruside, furosemide, Spiron 〇 steroid (Spiron〇iact〇ne), Triamteren, aten〇i〇i, Besopro 318197 94 1322688 (bisoprolol) anti-butyric acid, shellfish It is betaxolol hydrochloride, bevantolol hydrochloride, metoprolol (met〇pr〇1〇1) tartrate, acebutolol hydrochloride, Xili Celiprolol hydrochloride, nipradil (1), tilisolol hydrochloride, nad〇i〇i, propranolol hydrochloride Salt, indenol〇1 hydrochloride, carteolol hydrochloride, pindolol Pindolol), pindolo sustained release agent, bunitrolol hydrochloride, penbutolol sulfate, bopindolol malonate, amosularo (amosulalol) hydrochloride, arotinol(1) hydrochloride, carvedilol, iabetalol hydrochloride, urapidil, terra Terazosin hydrochloride, doxazosin sulfonate, bunazosin hydrochloride, prazosin hydrochloride, phentolamine Methanesulfonate, ci〇nidine hydrochloride, guanfacine hydrochloride, guanabenz acetate, methyl dopa, reserpine Reserpine), rescinnamine, amlodipine benzoate, aranidipine, efonidipine hydrochloride, cilnidipine , nicardipine hydrochloride, nisoldipine, nitrendipine, nifidipi Ne), sustained release of rifampicin, nilvadipine, barnidipine salt, felodipine, benidipine 95 318197 1322688 hydrochloride, Manidipine hydrochloride, azelnidipine, di 1 tiazem hydrochloride, hydrazine monohydrochloride, todolarazine hydrochloride, Budulaazine, cadralazine, captopril, enalapril (enaiapriD maleate, aracepril, adipripri, di Lapriril hydrochloride, cilazapril, 1 isinopri 1 , benazepri 1 hydrochloride, Imi® Iridar i 1 hydrochloride, tara〇capri丄 hydrochloride, quinapril (qUinapri 1) hydrochloride, chuandolapril (trandolapri 1) ), perind〇pri 1 erbumine, kensaltan (ci lexeti 1), washatan (vaisar) Tan), telmisartan, omisaltan, 朵imesartan, 1116 (1〇乂〇111丨1), nittuside (11丨1叩1*1135丨(^) ) or nitroglycerin. • 36. The η specific oxime compound represented by the following formula (I) or a pharmaceutically acceptable salt thereof:

Wherein represents an aryl or heteroaromatic group; \ represents a gas atom, a tooth atom, a 6 alkyl group or a C 6 alkoxy group; R represents a halogen atom, a Cl 6 alkyl group, a C 6 6 alkoxy group or an azide 96 318197 1322688 R represents a non-dentate atom, a sulphate, an azide group, an amine A: a μ' group, a halogen C, a -6 alkyl group, a C, a 6 alkoxy group: a sulphide, an amine group or Ci group continues to brew amine groups; and breaks this to be the same or different and represents (υ hydrogen atom, · selected from one of the following groups (2) C!-6 alkyl which can be replaced by: one or more Base

[Group A J A2 · Cn6 alkoxy, A3 ·, wherein K41 and R- are the same or a phase group ' or P and γ may be combined with a phase 11 atom or a Chalane single-ring heterocycle, which together form a saturated 5 Or A4. aryl, A5. Heteroaryl, A6. ~C〇-n(R4")(r4丨1,), where R4丨丨 and R4", know m base, or R and R4". 0T, go to the door, and the table does not 虱 虱 卜 俨 俨 俨 俨 俨 俨 俨 俨 俨 俨 连同 虱 虱 虱 虱 虱 虱 虱 虱 虱 虱 虱 虱 虱 虱 虱 虱 虱 虱 虱 虱 虱 虱 虱 虱 虱 虱 虱 虱 虱 虱 虱 虱Carbonyl group, (3) C2-6 alkenyl group; (4) C2-6 alkynyl group; 318197 97 1322688 (5) C3-8 cycloalkyl group; wherein the cycloscyclyl group may be substituted by a hydroxyl group, a carboxyl group or a Cl-6 alkoxycarbonyl group. Or may be condensed with a bite ring, (6) a C3-8 cycloalkyl-Ch alkyl group; wherein the cycloalkyl group of the G-8 cycloalkyl Cm alkyl group may be substituted with a hydroxyl group, a carboxyl group or a Cm alkoxy group , or can be condensed with a 咬 bite ring,

(Ό5- or 6-membered monocyclic heterocyclic group which may be substituted by one or more substituents selected from the group c below:

[Group C] C1. 匕-6 alkyl, C2. fluorenyl, C3. Cl-6 alkyl base, C4. carboxy^ C5. Cl-6 alkoxy group, and C6. ~C0-( Alk)n-C00R5 wherein R52 is a hydrogen atom or (^-6 alkyl; Aik is C: 4 alkyl; and π is an integer of 0 or 1 to 3, (8) aryl which may be selected from the group consisting of Substituting one or more substituents of group d: [Group D]

Dl. hydroxy, D2.heart-6 alkoxy, D3. cyano, D4. 匕-6 alkyl, 98 318197 1322688 wherein the Ch alkyl group may be selected from the group consisting of a hydroxyl group, a carboxyl group and a Ci 6 alkoxycarbonyl group. Substituting one or more substituents of the group, D5. -N(R53)(R53,), wherein R53 and R53 are the same or different from each other and represent a hydrogen atom, a G 6 alkyl group or a C 6 alkyl group. Stuffed base, D6. -C〇-N(R53丨)(R531,), wherein R and r531 are the same or different from each other and represent a hydrogen atom, Ci (alkyl or Cl-6) -C00R54, wherein R54 is a hydrogen atom, a Ch alkyl group, a C1-6 alkyloxy Ci 6 alkyl group or a (^-83⁄4 alkoxyoxyl-6 alkyl group, D8.-C (NH( OH)) = N-R55, wherein R55 is a hydrogen atom or a Ci-e alkyl group, D9. a saturated 5- or 6-membered monocyclic heterocyclic group, and D10. 5 or 6 members of a single ring system a cyclic aryl group which may be substituted by a keto group or a thio(tetra) group, (9) a 5- or 6-membered monocyclic heteroaryl group or a 5- or 6-membered condensed heteroaryl group formed with a benzene ring, wherein the 5 members or The 6-membered heteroaryl group may be substituted with one or more substituents selected from a poor carboxyl group and a Ci-6 alkoxycarbonyl group. (10) C7-1 4 aralkyl; wherein the alkyl portion of the C7-M aralkyl group may be substituted with one substituent selected from the group consisting of the following two, and the aryl moiety may be substituted with one or more substituted filaments. 318197 99 1322688 [Group E]

El. Ch alkyl which may be substituted by a hydroxy group, E2. cyano group, E3. fluorenyl 'E4. Ci-6 alkoxy group, and E5. phenyl group, [F group] FI. Cw alkyl group, F2. Halogen atom, F3. cyano group, F4. thiol group, F5. Ch alkoxy group which may be substituted by one or more substituents selected from the group consisting of a carboxyl group and a Cl-6 alkoxycarbonyl group, F6·halogen Ci- 6 alkyl group, F7. carboxyl group, F8. Ci-6 alkoxy group, F9. -C0-N(R56a)(R56a·), wherein R56a& R56a' are identical or different from each other and represent a hydrogen atom, at least A saturated 5- or 6-membered monocyclic heterocyclic group of a nitrogen atom, or an alkyl group, may be substituted with one or more substituents selected from the group f below: μ [f group] Π·amine group, — Cl -6 alkylamino ' 318197 100 丄j厶厶υοο f 3 · di Cl-6 alkylamino group, f4 · carboxyl group, f5 · C1_6 alkoxycarbonyl group, via group, 'and f7. having at least one nitrogen atom a saturated 5- or 6-membered monocyclic heterocyclic group, pl〇. -C0-N(R56b)(R56b'), wherein R56b and R56b are the same or different from each other and represent a hydrogen atom and a Cm alkyl group. An imido substituted, aralkyl group which may be selected from the group consisting of an imido group and a halogen atom Substituting one or more identical or different substituents for a substituted aryl fluorenyl group which may be via Cm alkyl, (^-6 alkylsulfonyl, fluorenyl, aminoglycolyl, -Ch-cholylamine Substituted with a di-Ci 6 alkylamino group, FH. ~N=CR57(-N(R58)(R58 )), wherein R57 is a hydrogen atom or a Cl_e alkyl group, and R58' is the same as each other or Different from each other and representing a hydrogen atom or a Cl 6 alkyl group, a F12. 5 member or 6 membered monocyclic heteroaryl group, and a F13.methylenedioxy or ethylidene dioxy group, or (11) selected from 5 C,-6 substituted by one or more identical or different substituents of a group consisting of a member of a group consisting of a 5-membered or 6-membered condensed heteroaryl group formed by a stupid ring Alkyl; 318197 101 1322688 wherein the heteroaryl group may be substituted with one or more substituents selected from Group G: Group 1 [Group G] G1. Ch alkyl group which may be selected from one or more of the following g groups Substituted: [g group] g 1. halogen atom, g2. amine group, g3. — Ci-6 alkylamino group, g4·diCl-6 alkylamino group, g5. Cm alkoxycarbonylamino group And g6.hydroxyimino group, G2. halogen atom, G3. Ci-e alkoxy group Substituted by a halogen atom, G4. aryloxy, G5. cyano, G6.-N(R59a)(R59a,), wherein R59a and R59a are the same or different from each other and represent a hydrogen atom 戋匕alkyl group, or 1^ 593 and R59a may form a saturated 5- or 6-membered monocyclic heterocyclic ring together with an adjacent nitrogen atom, and the saturated heterocyclic ring may be selected from the group consisting of a trans group and an amine.

Substituting one or more identical or different substituents of a group consisting of a Ci-e sulfhydryl group and a di-Ci-e alkylamino group, > G7. -CO-N(R59b)(R59b·) , 318197 102 厶厶υοο wherein R and R are the same or different from each other and represent a hydrogen atom, a saturated 5- or 6-membered monocyclic heterocyclic group, or a & 6 alkyl group which may be substituted, G8. aryl , and G9. 5 or 6 member substituted or a single J-based heteroaromatic group which may be a ketone group or a thioketone group R4 and R5 together with an adjacent nitrogen material and a 5 or 6 membered monocyclic heterocyclic ring. Wherein the moiety of the saturated heterocyclic ring may have a double bond, and the saturated heterocyclic ring may be condensed with a benzene ring to form a condensed ring, and the saturated heterocyclic ring which may be condensed with the benzene ring to form a condensed ring may be selected from the group consisting of Substituting one or more substituents of a material consisting of Ci e, k alkoxy, fluorenyl and C" 37. The hydrazine compound according to the above item 36, or a pharmaceutically acceptable salt thereof, which is represented by the following formula (1):

^ Central ring Q represents an aryl or heteroaryl group; a sub, a halogen atom, a Ci_6 alkyl group or. 6 alkoxy R3 - atom, Cl 6 alkyl, Cl 6 alkoxy or azide; non-dentate, mesogenic, (calcene, C | 6 -, C 318 197 103 azide, amine a hydrazino group or a hydrazine -6 group; the R4 represents (1) a hydrogen atom; (2) a Cm alkyl group which may be substituted with one or more substituents selected from the group A below: [A Group] A1. Merid, A2. Cl-6 alkoxy, A3·-N(R41)(R41'), "Medium β and r are the same or different from each other and represent a hydrogen atom or ci6 or rm together with The nitrogen atom together forms a saturated 5- or 6-membered monocyclic heterocyclic ring, A4. aryl, A5.heteroaryl, A6·-c〇-N(R4U)(r4",), 炫基其Γκ:: : 二彼? identical or different and represents a hydrogen atom or a c 1 member or a fluorene monocyclic heterocycle which may be bonded together with an adjacent nitrogen atom and a 5 Α 7. fluorenyl group, and a Α 8 · Cm alkoxycarbonyl group (3) C2-6 alkenyl; (4) C2-6 alkynyl; (5) C3-8 cycloalkyl; 318197 104 (6) C3-8 cycloalkyl Cl_6 alkyl; or α) aryl; and R5 (1) Ch The alkyl group may be selected from, for example, a substituent: one or more substituents of Group B [Group B] D1 B2. Cl-6 alkoxy, B3· 'N (R51)(R51) ^ wherein R5丨 and R51' are the same as the alkyl group; or RS1 and R-linkable; the same or different and representing a hydrogen atom or a member or a monocyclic heterocyclic ring: 4 (4) The nitrogen atoms together form a residual and Β4. -C0-NCR51,)CR511'), mτ together with an adjacent nitrogen atom form a shell or a 6-shell early ring heterocycle, (2) a C3-8 cycloalkyl; Substituted by a benzylidene group, (d) or a Ci e group (tetra) or a cycloalkyl group condensable with a pyridine ring, (3) a C3-8 cycloalkyl c, _6 alkyl group; wherein t the Cw cycloalkyl group C, The cycloalkyl group of _6 alkyl group may be substituted by a hydroxyl group, a few groups or an oxy group, or may be condensed with a bite ring, 318197 105 1322688 as shown in the following group C (4) saturated Μ or U single shot, miscellaneous county Substituted by one or more substituents: [c group] C1·Cl-6 alkyl, C2·fluorenyl, C 3. C1 -6 alkyl, C4.carboxy, C5. Oxyl group,

C6. -CO-(Alk)n-COOR52, wherein R52 is a hydrogen atom or a Ch thiol group; Alk is 〇 or an integer from 1 to 3, (iv) and η = group may be selected from one of the following Group D or a plurality of substituents are substituted for D1. thiol, D2. Ch alkoxy, D3. cyano, M. Cl-6, wherein the CH alkyl group may be selected from the group consisting of a trans group, a carboxyl group, and a fluorene alkoxy group. Substituting one or more substituents of the group consisting of a carbonyl group, D5. -N(R53)(R53.), wherein R and R are the same or different from each other and represent a hydrogen atom, a Ci 6 or a Cl- 6 succinyl sulfhydryl groups, D6·-C0-N(R531)(R531,), 318197 106 1322688 wherein R53〗 & R53丨 are the same appearance base or Cl-6 base, D7·-C00R54 , or different and represents a hydrogen atom

Wherein R54 is a hydrogen atom, a Ci-6 alkyl group, a Ci or a C3-8 cycloalkoxycarbonyloxyl group, D8.-C(NH(OH)) = N-R55, a decyloxy-Cl- 6 calcined group wherein R55 is a hydrogen atom or Cl_e alkylsulfonyl D9·saturated 5 member or 6 membered monocyclic heterocyclic group, and D10. 5 member or 6 membered group substituted, mono-% heterocyclic aromatic group A 5- or 6-membered monocyclic heteroaryl group or a 5-membered or 6-condensed heteroaryl ring formed by a ketone group or a thioketone (.6), wherein the 5 or 6 member heteroaromatic group may be Substituting one of the substituents of the sulfhydryl group and the Gh silk group; (Ό C?-14 aryl group; wherein the alkyl group of the c7-14 aryl group may be selected from one of the following E groups Or a substituent substituted, and the aryl moiety may be substituted with one or more substituents selected from Group F below. [Em]

El. Ch alkyl which may be substituted by hydroxy group, E2. cyano group, E3. retinoyl group, E4. Cm alkoxycarbonyl group, 318197 107 1322688 E5. phenyl group, [F group] F1. C1 -6 alkyl group, F2 Halogen atom, F3. cyano group, F4. thiol group, F5. Ch alkoxy group which may be substituted by one or more substituents selected from the group consisting of a carboxyl group and a Cw alkoxycarbonyl group, F6. Ci-6 alkyl, F7. carboxy, F8. Cm alkoxycarbonyl, F9. -CO-N(R56a)(R56a), wherein R56a&R... are identical or different from each other and represent a hydrogen atom, having at least - A saturated 5-membered or 6-membered monocyclic heterocyclic group of a nitrogen atom, 'or Cl-1^' may be substituted with one or more substituents selected from the group consisting of: fl. Amino, f 2 · Early C 1 - 6 alkylamino group, f 3 · di Cl-6 alkylamino group, carboxyl group, f5 · Cm alkoxycarbonyl group, f6. via group, and member or 6 member single ring system · have at least Saturated by a nitrogen atom 108 318197 1322688 Heterocyclic group, F10. -N(R56b)(R56b'), wherein R56b and R56b are the same or different from each other and represent a hydrogen atom, a Ci-6 alkyl group which can be imine a substituted or aralkyl group which may be selected from the group consisting of an imido group and a halogen atom Substituted by one or more identical or different substituents of the group, the arylsulfonyl group may be via a Ci-6 alkyl group, a Ci-6 alkylsulfonyl group, an anthracenyl group, an aminomethylcarbenyl group, Substituted with a mono Cm alkylamino fluorenyl group or a di Cm alkylamino fluorenyl group,

Fll. -N=CR57(-N(R58)(R58,)), wherein R57 is a hydrogen atom or a Ch alkyl group, and r58 and r58 are the same or different from each other and represent a hydrogen atom or a Cl_6 alkyl group, F12·5 Or 6 members of a monocyclic heteroaromatic group, and F13.methylenedioxy or ethylidene dioxy, or ^5 5 or 6 membered monocyclic heteroaryl substituted Gl_6 The following:: 5 or 6 members of the alkyl group substituted by a condensed heteroaryl group; the base: the heteroaromatic group may be selected from one or more of the following groups G or one of [group G] g or A plurality of substituted G1·Cm alkyl groups may be substituted by a group selected from the group consisting of: [g group] halogen atom, 318197 109 1322688 g2. amine group, g3. mono-Cl-6 alkylamino group, S4. diCi-6 burning Amino group, g5. Ci-6 alkoxycarbonylamino group, and g6. hydroxyimino group, G2. tooth atom, G3. Ci-e alkoxy group which may be substituted by a halogen atom, G4 aryloxy group, G5. cyano, G6. -N(R59a)(R59a), alkyl, or R59a wherein R59a and R59a are the same or different from each other and represent a hydrogen atom or Cl and R59a• may form a saturated state together with an adjacent nitrogen atom. 5 single C!-6 alkylamino group and two c16 members or 6 members single ring ring 'and the saturation The heterocyclic ring may be substituted by a substituent selected from the group consisting of a hydroxyl group, an amine group 10 or a plurality of the same or different substituents, and a group consisting of alkylamino acids, G7.-C0-N(R59b)(R59b.),

芳.aryl, substituted, G9·5 member or 6贞monocyclic (tetra)aryl group which can be saturated with 5 or 6 members by sulfhydryl or thiol 318197 110 1322688 and 1^ together with adjacent nitrogen atoms Early dressing is a %, wherein one part of the saturated heterocyclic ring may have a double bond, and the impurity! It can be condensed with a benzene ring to form a condensed ring, which can be condensed with a benzene ring to form a saturated heterocyclic ring of a condensed ring. The saturated heterocyclic ring can be composed of a functional group selected from a functional atom, a group, a k oxo group and a C hexaoxy group. Substituting one or more substituents of the group. 38. The pyrazole compound according to 36 above, or a pharmaceutically acceptable salt thereof,

It is represented by the following general formula (II,):

R

R

5/N 2 (10 wherein R, R2, R3, R4 and R5 are as defined in the aforementioned 36 items.

39. The pyrazole compound according to the above 36 or a pharmaceutically acceptable compound thereof is represented by the following formula (II):

Wherein R4 and R5 are as defined in the aforementioned 36 items, RU is a main group, R2a represents a halogen atom, and R3a is a functional atom or a k-burning group. Atom or hydrogenogen 40. A pyrazole compound according to the above 39 or a pharmaceutically acceptable salt thereof, 318197 111 1322688 wherein R is a halogen atom or a fluorine atom, R 2a is a fluorine atom or a gas atom, and R 3 a is a chlorine atom or Cl-6 yard base. 41. The pyrazole compound according to the above item 40, or a pharmaceutically acceptable salt thereof, which is represented by the following formula (III):

Wherein R4 and R5 are as defined in item 37 above. The pyraridin compound according to any one of the preceding items 37 to 41, wherein R4 is a group selected from the group consisting of: (1) a hydrogen atom; One or more substituents are taken as (2) Ci-6 alkyl groups which may be selected from the group consisting of:

LA, group J A' 1. thiol, A' 2. Cm alkoxy, A' 3. _N(R4丨) (anti 41,), or 6 membered monocyclic heterocycle, ortho nitrogen And 5 members of A'4. Phenyl, A'5. 5 or 6 members of monocyclic heteroaryl, 318197

112 1322688 AJ6. -C0-N(R41,)(R4]1), wherein R4U and R411' are the same or different from each other and represent a gas source, a base; or a wide range together with an adjacent nitrogen atom to form a member or 6 members of the monocyclic heterocycle, u 5 Α' 7·carboxyl, and A' 8. C!-4 alkoxycarbonyl, (3) C2-6, (4) C2-6 alkynyl, Lu (5) C&quot ; cycloalkyl; and (6) C3-8^ alkyl-based C-4 alkyl. 43. A pyrazole-acceptable salt according to any one of the preceding items 37 to 42, wherein "5 is a Cl_6 alkyl group. The pyrazole compound according to any one of the above items 37 to 42 or a pharmaceutically acceptable salt thereof, wherein R5 is a Cm cycloalkyl group which may be selected from the group consisting of a hydroxyl group, a carboxyl group and a Cm alkoxy group. Substituting one or more substituents of the group consisting of a carbonyl group. The pyrazole compound according to any one of items 37 to 42 or a pharmaceutically acceptable salt thereof, wherein R5 is a Cm cycloalkyl group (^6 alkyl group. ', 46. According to the items 37 to 42 A pyrazole compound or a pharmaceutically acceptable salt thereof, wherein R5 is a saturated 5 member or 6 M monocyclic heterocyclic group which may be selected from the group consisting of thiol and -CO-(Alk)n_COOR52 Substituting one or more substituents of the group 'wherein r52 is a hydrogen atom or a Ci 6 alkyl group, Aik is a C1-4 stretching group and η is an anthracene or an integer of 1 to 3. 318197 113 1322688 47. A compound according to any one of the preceding items 37 to 42 wherein R5 is a phenyl group which may be substituted with one or more substituents selected from the group consisting of: d, group: D'l. Ci-4 can be substituted by a ring group, D,2. -CO-N(R53)(r53'), wherein R53 and R53 are mutually phase @ or different and represent & atom, "Acrylic or Cl-4 alkyl group; ® D' 3. -C00R54, wherein R54 is a hydrogen atom, a Cl-4 alkyl group, a Ci_4 alkylcarbonyloxy C! 4 alkyl group or a C3-8 cycloalkane Oxycarbonyloxy Cm alkyl, and D 4. 5 or 6 membered monocyclic The aryl group may be substituted by a keto group or a thioketo group. 48. The compound according to any one of clauses 37 to 42 wherein the compound is a salt or a pharmaceutically acceptable salt thereof, wherein R5 is a C7_u aralkyl group. And the aryl moiety of the C7_14 aralkyl group may be substituted with one or more substituents selected from the group consisting of F: [Fi] F 1. Ci-6 alkyl, F' 2. halogen atom, F' 3. Cyano, F' 4. thiol, F 5. Ci-e alkoxy which may be substituted by one or more substituents selected from the group consisting of carboxy and Cl-6 alkoxycarbonyl, 114 318197 1322688 F ' 6. From Ci-6 alkyl, F' 7·carboxyl, F' 8 · Ci-6 alkoxycarbonyl, F'9. -c〇-N(R56a)(R56a,), wherein R56a and ! a 5- or 6-membered monocyclic system that is the same or different and represents a gas atom and has at least one nitrogen atom saturated ^

a Cl-6 alkyl group which may be selected from the group consisting of one or more substituents;

[Γ group] f' 1 · amine group, f 2. early Cl-6 alkylamino group, f 3. diCl-6 alkyl group 'f' 4 carboxyl group, f' 5. Ch alkoxycarbonyl group, f ' 6. 经基,

And f'7. a 5- or 6-membered monocyclic heterocyclic group having at least one nitrogen atom, F'10. -N(R56b)(R56b·)' wherein R56b and R5ba are the same or different from each other Represents a hydrogen atom, a Gy alkyl group which may be substituted with an imido group which may be substituted with one or more identical or different substituents selected from the group consisting of an imine group and a halogen atom, and an arylsulfonyl group thereof It can be replaced by Ci-e, C,-6 alkyl, sulfhydryl, aminomethylmercapto, mono-Ci-6 alkylaminocarbamyl or di-Ci6 alkylaminocarbamyl , 115 318197 1322688 F 11. -N=CR57(-N(R58)(r58.)), R58' are the same as each other or wherein R is a hydrogen atom or a ClM alkyl group, π and are different and represent a hydrogen atom or a Ci4 alkane Base, F'12. 5- or 6-membered monocyclic heteroaryl, and F 13. methylenedioxy or ethylenedioxy. 49. According to any one of the aforementioned 37 to 42, the pyrazole compound of the above formula, or the pharmaceutically acceptable salt thereof, wherein R5 is a member of 5 戎昌留^ ra 贝次6贝早裱The heteroaryl-substituted CH alkyl group and the heteroaryl group may be substituted with a substituent selected from the group consisting of G or a group of one or more substituted G'l·Cm alkyl groups. It may be substituted by a group selected from the group consisting of: [g, group] g' 1. a halogen atom, g' 2. an amine group, g' 3. a mono C16 alkylamino group, g' 4. a diCl-6 alkyl group Amino group, g' 5. Ch alkoxycarbonylamino group, and g' 6. hydroxyimino group, G' 2. halogen atom, G'3. Cm alkoxy group which may be substituted by a halogen atom, G' 4 . aryloxy, 318197 116 1322688 G' 5. Cyano, G, 6. -N(R59a)(R59a ), wherein R59a and R59a• are each other due to the relationship between seven and wr... The Cl_6 filament, or R and R, together with the (iv) nitrogen atom, form a saturated 5 or 6-shell early-heterocyclic ring, and the saturated heterocyclic ring can be selected from the group consisting of a mono-chromic amine group and a di-alkylamine. Group consisting of a group ^^^ substituted by multiple substituents, G' 7. -CO-N(R59b)(R59 b), wherein R59b and R59b are the same or different from each other and represent a gas atom, a saturated 5-membered or 6-membered monocyclic heterocyclic group, or a calcinyl group which may be substituted with a 'G' 8. aryl group via a heterocyclic group, And G'9. 5 or 6 membered monocyclic heteroaryl which may be substituted by a keto or thioketo group. Xin 50. The bite according to any of the items 37 to 41. a compound or a pharmaceutically acceptable salt thereof, wherein R4 and R5 form a saturated 5- or 6-membered monocyclic heterocyclic group together with an adjacent nitrogen atom, and a portion of the saturated heterocyclic group may have a double bond and may The benzene ring is condensed to form a condensed ring, and the saturated heterocyclic group which can be condensed with a stupid ring to form a condensed ring may be selected from the group consisting of a tooth atom, a C, a 6 alkyl group, a Ci-6 alkoxy group, a slow group, and a Cl- group. Substituting one or more substituents of the group consisting of 6 alkoxy groups. The pyrazole compound according to the above item 37 or a pharmaceutically acceptable salt thereof, wherein the compound is a compound represented by the following formula (IV): * sitting compound: 117 318197

Wherein, as defined by the item 37, RH rX3 are the same or different from each other and represent a milk atom or are selected from the group consisting of F, the substituent of the group and m being an integer of two. • η] F” i· alkyl, F” 2. halogen atom, F” 3·cyano, F” 4. hydroxy, F 5 · C1-4 alkoxy which may be selected from carboxyl and Cl 4 alkoxy Substituted by one or more substituents of the group consisting of a carbonyl group, φ F" 6. Halo Cl-6 alkyl, F" 7. fluorenyl, F 8 · Ci-6, gas group, 'F" 9. -c〇-N(R56a)(R56a), wherein R56a& R56a are the same or different from each other and represent a hydrogen atom, a saturated 5-membered or 6-membered monocyclic heterocyclic group having at least one nitrogen atom, or Ci The -6 alkyl group may be substituted by one or more substituted molybdenum selected from the group F below. [f,, group] 318197 118 1322688 f" 1. amine group, f" 2. mono-Ch alkylamino group, f" 3. Di-Cm alkylamino, Γ' 4. carboxy, * Γ 5. Ch alkoxycarbonyl, f" 6. trans-group, and oxime 7. 5 or 6 with at least one nitrogen atom saturated A single ring of a heterocyclic group, F" 10. -N(R56b)(R56b'), wherein R56b and R56b' are the same or different from each other and represent a hydrogen atom, and the Ci·alkyl group can be substituted with an imine group. An aralkyl group which may be one or more selected from the group consisting of an imido group and a halogen atom Substituted by the same or a different substituent, the arylsulfonyl group may be Cm alkyl, C!-6 alkylsulfonyl, fluorenyl, aminoglycol, mono-Ci-e alkylamino Substituted by a mercapto or a di-Ch-cholylamino-based group, F"11·-N=CR57(-N(R58)(R58,)), wherein R57 is a hydrogen atom or a Cm alkyl group, R58 and R58, Are identical or different from each other and are not represented by a wind atom or Cl-6, F" 12. 5 or 6 membered monocyclic heteroaryl, and F" 13 methylene dioxy or Ethyl The pyrazole compound according to the above item 37 or a pharmaceutically acceptable salt thereof, wherein the pyrazole compound is a pyrazole compound represented by the following formula (v): 318197 119

The definition of the above 2 'ring Het means that the 5-member or 6-membered monocyclic moieties are selected from 2 κ and κ which are identical or different from each other and represent a hydrogen atom or a substituent of [G, 魬; G' group as follows, and m, Or 1 or an integer of 1 to 2, G, * V^l-6 is substituted: alkyl which may be substituted by one or more of the following g groups: [g'

Meeting

Halogen atom, amine group, monoCh alkylamino group, diCl-6 alkylamino group, G-6 alkoxycarbonylamino group, g 6. hydroxyimino group, 2·halogen atom, G, 3 G, 4 G, G,

Cl-6 alkoxylate which can be substituted with an aryloxy group via a tooth atom, cyano, N(R59a)(R59a), 120 318197 1322688 which makes 俨 and π identical or different from each other and is either ~ or adjacent The nitrogen atom together form a member or a 6-shell (tetra)-heterocyclic ring, and the remainder and the heterocyclic ring may be one selected from the group consisting of a group of an amino group, an early Cm alkyl group, and a fluorenyl group. Substituted by a plurality of substituents, 7. -CO-N(R59b)(R59b), wherein R59lR59b are the same or different from each other and represent a hydrogen atom, a saturated 5 member or a 6 S monocyclic heterocyclic group or a silk It may be substituted with a heterocyclic group, a G' 8. aryl group, and a G'9 5 member or a 6 fluorene monocyclic heteroaryl group substituted with a sulphonyl group or a thiol group. 53. The pyrazole compound according to the above item 52, wherein the Het ring is a pyridine ring, a triazole ring or an oxazole ring, or a pharmaceutically acceptable salt thereof. The pyrazole compound according to the above item 53, or a pharmaceutically acceptable salt thereof, wherein the pyrazole compound is a pyrazole compound represented by the following formula (VI):

Wherein R4, RY1, RY2, RY3 and m' are as described above. 55. The pyrazole compound according to the above item 37 or a pharmaceutically acceptable salt thereof, 318197 121 1322688 wherein the pyrazole compound or a pharmaceutically acceptable salt thereof is selected from the group consisting of 5-(2-chloro-4, 5-difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid (pyridin-3-ylindenyl)-decylamine, 5-(2-chloro-4, 5-difluoro-benzene Mercaptoamino)-1Η-pyrazole-3-carboxylic acid (pyridin-3-ylindenyl)-decylamine dihydrochloride, 5-(2-chloro-4, 5-difluoro-phenylhydrazine Amino-pyridyl-3-carboxylic acid (pyridin-3-ylindenyl)-decylamine hydrochloride, 5-(2-chloro-4,5-difluoro-benzoinylamino) -1Η-pyrazole-3-carboxylic acid (4-mercapto-oxazol-5-ylindenyl)-decylamine, 5-(2-a-4,5-difluoro-benzoinylamino) -1Η-carbazole-3-carboxylic acid (4-methyl-oxazol-5-ylmethyl)-decylamine, 5-(2-gas-4, 5-difluoro-benzhydrylamino) -1Η-carbazole-3-carboxylic acid (4-mercapto-oxazol-5-ylmethyl)-nonylamine p-toluenesulfonate, 5-(2-chloro-4, 5-difluoro- Benzoylamino)-1Η-η-pyrazole-3-carboxylic acid (4-mercapto-oxazol-5-ylmethyl)-nonylamine-L-(+) tartrate, 5-(2- Gas-4, 5-difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylate (2,4-dimethyl-oxazol-5-ylindenyl)-nonylamine p-toluenesulfonate, 5-(2-chloro-4,5-difluoro-benzoinylamino)- 1Η-pyrazole-3-carboxylic acid (2,4-dimethyl-oxazol-5-ylindenyl)-decylamine, 5-(2-chloro-4, 5-difluoro-benzoguanamine -1Η-carbazole-3-carboxylic acid (2,4-dimethyl-pyridin-3-ylindenyl)-decylamine, 5-(2-chloro-4, 5-difluoro-phenylhydrazine Aminoguanidino)-pyridazole-3-carboxylic acid diethyl decylamine, 122 318197 1322688 5-(2-chloro-4,5-difluoro-benzoinylamino)-1Η-η-rhizozolyl 3-carboxylic acid ethyl-(pyridin-4-ylindenyl)-decylamine, 5-(2- gas-4, 5-difluoro-benzoinyl)-1Η-pyrazole-3- Carboxylic acid (2-decyloxy-ethyl)-mercapto-nonylamine, 5-(2- gas-4, 5-difluoro-phenylhydrazino)-1Η-. Bis-azole-3-carboxylic acid ethyl-(2-decyloxy-ethyl)-decylamine, 5-(2-chloro-4, 5-difluoro-phenylhydrazino)-1Η-pyrazole 3-carboxylic acid 2-fluoro-nodalamine, 5-(2-chloro-4, 5-difluoro-phenylhydrazino)-1Η-°biazole-3-carboxylic acid 3-fluoro-section Indoleamine, 5-(2-Gas-4, 5-difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid 2-didecylamino-benzylamine, 5-(2 - gas-4, 5-difluoro-benzhydrylamino)-1Η-carbazole-3-carboxylic acid (4-ethoxycarbonyl-cyclohexyl)-propyl-decylamine, 5-(2-chloro -4,5-difluoro-phenylhydrazinoamino)-1Η-°biazole-3-carboxylic acid (6-decylpyridin-3-ylmethyl)-decylamine, 5-(2- Gas-4, 5-difluoro-adenylamino)-1Η-pyrazole-3-carboxylic acid 2,3-dimethoxy-benzylamine, 5-(2-gas-4, 5- Difluoro-benzoguanidino)-1Η-pyrazole-3-carboxylic acid 2,4-dimethoxy-benzylamine, 5-(2-chloro-4, 5-difluoro-benzamide Amino)pyrazine-3-pyrazole-3-carboxylic acid 2,6-dimethoxy-benzylamine, 5-(2-gas-4,5-difluoro-anthracenylamino)-1Η -pyrazole-3-carboxylic acid 3,5-dimethoxy-benzylamine, 123 318197 1322688 5-(2-chloro-4,5-difluoro-phenylhydrazino)-1 Η-. Bis-zolyl-3-carboxylic acid 3,4-dimethoxy-benzylguanamine, 5-(2-chloro-4, 5-difluoro-phenylhydrazinoyl)-1Η-pyrazole-3-carboxylic acid 2,3-Difluoro-tubular amine ' 5-(2-chloro-4, 5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid 2,4 - 二气_节Amine amine ' 5-(2-chloro-4, 5-difluoro-benzylidenylamino)-1Η-pyrazole-3-carboxylic acid 2,5-difluoro-tuberamine' 5-(2- Gas-4, 5-difluoro-phenylhydrazinoamino)-1Η-. Bis-zolyl-3-carboxylic acid 2,6-difluoro-branched amine ' 5-(2-chloro-4,5-difluoro-benzoindolyl)-1Η-η-pyrazole-3-carboxylic acid 3 , 4-difluoro-benzylamine, 5-(2-chloro-4, 5-difluoro-benzylidenylamino)-1Η-pyrazole-3-carboxylic acid 3, 5-difluoro-benzazole Amine, 5-(2-chloro-4, 5-difluoro-benzylidenylamino)-1Η-pyrazole-3-carboxylic acid (2-isopropoxy-pyridin-3-ylindenyl)- Indoleamine, 5-(2-chloro-4, 5-difluoro-benzylidenylamino)-1Η-. Bis-zolyl-3-carboxylic acid (2-phenoxy-pyridin-3-ylindenyl)-decylamine, 5-(2-gas-4, 5-difluoro-phenylhydrazino)-1Η- Pyrazole-3-carboxylic acid (3,5-difluoropyridin-2-ylindenyl)-nonylamine, 5-(2-chloro-4,5-difluoro-benzoinyl)-1Η -carbazole-3-carboxylic acid 2-trifluorodecyl-benzylamine, 5-(2-chloro-4,5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylic acid 3-Trifluorodecyl-benzylguanamine, 124 318197 1322688 5-(2-Gas-4, 5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid 4-trifluoroindole Base-benzylamine, 5-(2-chloro-4, 5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylic acid 4-tert-butyl-benzylamine, 5- (2-Chloro-4, 5-difluoro-phenylhydrazino)-1H-pyrazole-3-carboxylic acid (6-isopropoxy-pyridin-3-ylindenyl)-decylamine, 5 -(2-chloro-4,5-difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid [2-(2,2,2-trifluoro-ethoxy)-β ratio Bite-3-ylindenyl]-bristamine, 5-(2-chloro-4,5-difluoro-benzoinylamino)_1Η-π ratio 17-spin-3-rebel 4-(2-di Mercaptoamino-ethylaminopurinyl)-benzylamine, 5-(2-Gas-4,5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylic acid 4 -ethyl-benzylamine , 5-(2-chloro-4, 5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid 4-isopropyl-benzylguanamine, 5-(2-chloro-4 , 5-difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid 2-gas-6-fluoro-benzylchiral, 5-(2-chloro-4, 5-difluoro-benzene Mercaptoamino)-1Η-pyrazole-3-carboxylic acid (6-ethoxy-pyridin-3-ylindenyl)-decylamine dihydrochloride, 5-(2-gas-4, 5- Difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid (thiazol-4-ylindenyl)-decylamine, 5-(2-chloro-4, 5-difluoro-benzoquinone [amino]amino)pyrazole-3-carboxylic acid [6-(2,2,2-trifluoro-ethoxy)-pyridin-3-ylindolyl]-nonylamine dihydrochloride, 5 -(2-chloro-4,5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid/❻\ 125 318197 1322688 2,6-dimethyl-benzylamine, 5- (2-Gas-4,5-difluoro-phenylhydrazino)-111-°Bizozole~3-carboxylic acid [2-(pyridin-3-yl)-thiazol-4-ylmethyl]- Indoleamine dihydrochloride, 5-(2- gas-4, 5-difluoro-phenylhydrazinoyl)-1Η-pyrazole-3-carboxylic acid (1H-benzimidazol-2-ylmethyl) - indoleamine dihydrochloride, [4-({[5~(2- gas-4, 5-difluoro-benzylidylamino)-1Η-β than sal-3-carbonyl]amino} -mercapto)-phenyl fluorenyl Amino]-acetic acid decyl ester, 3-[4-({[5-(2-gas-4,5-difluoro-benzylidenylamino)-111-pyranyl-3-carbonyl]-amine Benzylmethyl)-benzylideneamino]-propionic acid decyl ester, 5-(2-chloro-4,5-difluoro-benzoinylamino)-lH-pyrazole-3-indoleic acid (2 _Mercapto-thiazol-4-ylmethyl)-guanamine dihydrochloride, 5-(2- gas-4, 5-difluoro-phenylhydrazino)-indole-pyrazole-3- Acid (3,5-methyl-iso-oxan-4-ylmethyl)-decylamine, 5-(2- gas-4, 5-difluoro-phenylhydrazinyl)-ιη-吼4-(2-indole-(2-ethyloxyethyl)-amino-ethylaminopurinyl-benzylhydrazine-amine, 5-(2-gas-4, 5 -difluoro-phenylhydrazinoamino)-ιη-pyrazole-3-carboxylic acid 4-(2-hydroxy-ethylaminocarbamimidyl)-benzylamine, 5-(2-gas-4, 5-difluoro-benzhydrylamino)-ih-pyrazole-3-carboxylic acid 4-{2-[(2-acetoxyethyl)-(2-hydroxyethylamino)-B Amino-based amine, 5-(2-chloro-4, 5-difluoro-benzylidenylamino)_1H-pyrazole-3-carboxylic acid 0-mercapto-1H-benzene And imidazol-2-ylindenyl)-decylamine hydrochloride, 5-(2-chloro-4,5-difluoro-benzoindolyl)-1H-pyrazole-3-carboxylic acid 126 3 18197 1322688 (thiazol-2-ylindenyl)-guanamine dihydrochloride, 5-(2-chloro-4,5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylic acid (benzothiazol-2-ylindenyl)-guanamine dihydrochloride, ' 5-(2-gas-4, 5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylate Acid (2,5-dimercapto-thiazol-4-ylindenyl)-nonylamine dihydrochloride, 5-(2-chloro-4,5-difluoro-benzhydrylamino)-1Η- Pyrazole-3-carboxylic acid [2-(morpholin-4-yl)-thiazol-4-ylmethyl]-decylamine dihydrochloride, 5-(2-chloro-4, 5-difluoro-benzene Methionylamino)-1Η-°biazole-3-carboxylic acid• (1,3,5-trimethyl-1H-pyrazol-4-ylmethyl)-decylamine, 5-(2-chloro -4,5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid (2-chloro-6-methyl-pyridin-3-ylindenyl)-nonylamine dihydrochloride , 5-(2-Gas-4, 5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid (2-didecylamino-thiazol-4-ylindenyl)- Indoleamine dihydrochloride, 5-(2- gas-4, 5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid (diphenyl-1H-pyrrol-2-ylmethyl) )-decylamine, & 5-(2- gas-4, 5-difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid (3,4-dimethoxy-pyridine- 2-ylmethyl)-guanamine dihydrochloride, 5-(2-chloro-4,5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylic acid (5-third Butyl-thiazol-2-ylindenyl)-nonylamine dihydrochloride, 5-(2-gas-4,5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid (5-methyl-2-phenyl-2H-[1,2,3]triazol-4-ylindenyl)-decylamine, 5-(2- gas-4,5-difluoro-benzoquinone Amino)-111-pyrazole-3-carboxylic acid [4-(t-butoxycarbonyl-amino)-indenyl-pyridin-2-ylmethyl]-decylamine, 5-(2-chloro- 4,5-difluoro-phenylhydrazinoamino)-1Η-«biazole-3-carboxylic acid 127 318197 1322688 [4-methyl-2-(morpholin-4-yl)-thiazol-5-yl Hydrazinyl]-nonylamine dihydrochloride, 5-(2-chloro-4,5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid (pyridin-3-ylmethyl) )-guanamine 3/2 hydrochloride hemihydrate, .  5-(2-chloro-4,5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylic acid '2-amino-benzylamine, 5-(2-chloro-4, 5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid 2-methoxy-benzylamine, 5-(2-chloro-4, 5-difluoro-benzoinyl Amino)-1Η-°biazole-3-carboxylic acid•3-methoxy-benzylamine, 5-(2-chloro-4, 5-difluoro-phenylhydrazino)-1Η-pyridyl Oxazole-3-carboxylic acid 4-methoxy-benzylamine, 5-(2-chloro-4,5-difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid 4-carboxylate Benzo-benzylamine, 5-(2-chloro-4,5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylic acid 4-fluoro-benzylamine, φ 5-(2 -chloro-4,5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid 4-a-benzylamine, ' 5-(2-chloro-4, 5-difluoro- Benzoylamino)-1Η-pyrazole-3-carboxylic acid 4-ethoxyxo-aryl amine' 5-(2-chloro-4, 5-difluoro-phenylhydrazino)- 1-Η-pyrazole-3-carboxylic acid 4-carboxy-benzylamine, 5-(2-chloro-4, 5-difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid dibenzyl Indoleamine, 5-(2-chloro-4,5-difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid 128 318197 1322688 (cyano-phenyl-methyl)-nitramine , 5-(2-chloro-4,5-di -phenylhydrazinoamino)-111-pyrazole-3-carboxylic acid cyclohexylmethyl-decylamine, 5-(2-chloro-4,5-difluoro-benzoinylamino)-ih- Pyrazole-3-carboxylic acid•(2-trans-ethyl-ethyl)-phenyl, tyrosine, 5-(2-milo-4,5-mono-benzoylamino)-1Η-σ ratio 0 _3 - Cyclohexyl decyl-methyl-decylamine, 5-(2-chloro-4, 5-difluoro-phenylhydrazino)-ιη-pyrazole-3-carboxylic acid Cyclohexyl decylamine , 5-(2-Gas-4, 5-difluoro-benzhydrylamino)-ιη-pyrazole-3-carboxylic acid cyclohexyl-ethyl-bristamine, 5-(2-chloro-4, 5-difluoro-phenylhydrazinoamino)-ιη-pyrazole-3-carboxylic acid allylcyclohexyl-decylamine, 5-(2_qi_4, 5-dioxo-benzimidamide Base)-ΐΗ-〇 〇 -3--3--3- 叛 环 环 环 环 -3- -3- -3- -3- -3- ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( (坐-3-Oxanoic acid-(1_曱基辰咬-4-yl)-nonylamine, 5-(2-chloro-4,5-difluoro-benzoic acid amino)-ΐΗ- *»Sit 3 - decanoic acid [(3, 4-decyldioxyphenyl)-mercapto]-decylamine hydrochloride, 5-(2_gas_4,5-difluoro- Benzoylamino-acid benzyl-butyl-decylamine, 5-(2-gas-4, 5- Difluoro-benzoguanidino)-lH-pyrazole-3-challic acid benzyl-(4-hydroxy-butyl)-decylamine hydrochloride, 5-(2-chloro-4, 5-di Fluoro-benzoguanidino)-ih-pyrazole-3-acid 318197 129 1322688 butyl-ethyl-decylamine, 5_(2-chloro-4-, 5-difluoro-phenylhydrazino -1Η-pyrazole-3-carboxylic acid cyclohexyl-propyl-decylamine, 5-(2- gas-4, 5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylate Acid • Butyl-cyclohexyl-decylamine, 5_(2_gas_4, 5-difluoro-benzylidenylamino)-1Η-pyrazole-3-carboxylic acid cyclohexyl-(2-decyloxy) Ethyl)-guanamine ' 5-(2-gas-4, 5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylic acid rucyclohexyl-(pyridin-3-ylfluorenyl) Indoleamine 5-(2-chloro-4, 5-difluoro-benzofuranylamino)-1Η-pyrazole-3-carboxylic acid [2-morpholin-4-yl]-phenyl]-indole Amine, 5-(2-Gas-4,5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylic acid dibutyl decylamine, 5-(2- gas-4,5- Difluoro-benzoquinone-based amino group)-specifically 0-3-anthracene-(2-decyloxy-ethyl)-decylamine, 5-(2-chloro-4,5-digas-benzene Brewing aryl-deoxy acid (2-decyloxy-ethyl)-propyl-decylamine, 5-(2- gas-4,5-difluoro-benzene曱 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基1Η-σ ratio 0 -3-carboxylic acid (2-decyloxy-ethyl)-(tetraz-halo-4-yl)-nitramine, 5-(2- gas-4, 5-difluoro -phenylhydrazinylamino)-1Η-π ratio 0 -3-oxocyclopentyl-(2-methoxy-ethyl)-decylamine, 5-(2- gas-4, 5-di Fluoro- benzhydrylamino)-1Η-η-pyrazole-3-buffer acid 1322688 cyclohexyl-(3-decyloxy-propyl)-decylamine, 5-(2-chloro-4, 5-di Fluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid cyclohexyl-(2-ethoxy-ethyl)-decylamine, 5-(2-chloro-4,5-difluoro- Benzoylamino) _111-〇 〇 -3 -3 --acidic cyclohexyl-(2-isopropoxy-ethyl)-bristamine' 5-(2-chloro-4, 5-difluoro- Benzoylamino)-1Η-pyrazole-3-carboxylic acid cyclohexyl-(2-propoxy-ethyl)-enamine-5-(2-chloro-4, 5-difluoro-phenylhydrazine Mercaptoamino)-1Η-pyrazole-3-carboxylic acid® (1-ethyl-propyl)-(2-decyloxy-ethyl)-decylamine, 5-(2-chloro-4, 5 -difluoro-phenylhydrazinoamino)-1 Η-pyrazole-3-carboxylic acid butyl-(1-tert-butoxy-based π-purin-4-yl)-nitramine 5-(2-chloro-4,5-difluoro-anthracenylamino)-1Η-pyrazole-3-carboxylic acid butyl-(tetrahydro-thiopiperazin-4-yl)-decylamine, 5-(2-chloro-4,5-difluoro-phenylhydrazinyl)_1Η-° ratio 0 sit-3-ortho acid butyl-(2-decyloxy-ethyl)-decylamine, φ 5-(2-Ga-4, 5-difluoro-benzylidenylamino)-1Η-pyrazole-3-carboxylic acid butyl-(°-pyridin-3-ylindenyl)-decylamine, ' 5-(2-chloro-4,5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylic acid benzyl-(2-methoxy-ethyl)-bristamine, 5- (2-Chloro-4,5-difluoro-benzoindolyl)-1Η-»biazole-3-carboxylic acid butyl-(piperidin-4-yl)-decylamine, 5-(2- Chloro-4, 5-difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid (ethylidene-piperidin-4-yl)-butyl-decylamine, 5-(2 -Chloro-4,5-difluoro-phenylhydrazinoamino)-1Η-indazole-3-carboxylic acid 131 318197 1322688 Butyl-(1-methanesulfonyl-piperidin-4-yl)-indole Amine, 5-(2- gas-4, 5-difluoro-benzoylaminopyrazole-3-carboxylic acid butyl-U-ethoxyoxalyl-piperidin-4-yl)-guanamine , 5-(2-chloro-4, 5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylic acid butyl oxalate-piperidin-4-yl)-nonylamine, 5-(2-gas-4, 5- Difluoro-phenylhydrazinoamino)-1 Η-pyrazole-3-carboxylic acid butyl-(1,1-dimercapto-hexanitro-1 and 6-sulfo0 bottom 嗔4-yl)-stuffed Amine ' 5-(2- gas-4, 5-difluoro-phenylhydrazino)-1Η-indazole-3-carboxylic acid butyl-(1-keto-hexahydro-1 λ4-sulfo α Decano-4-yl)-bristamine, 5-(2-chloro-4, 5-difluoro-benzoamitoyl)-1Η-pyrazole-3-carboxylic acid (6-methoxypyridinium) -3-ylmethyl)-propyl-decylamine, 5-(2- gas-4, 5-difluoro-adolylamino)-1Η-pyrazole-3-carboxylic acid propyl-(° Bispin-3-ylmercapto)-decylamine, 5-(2- gas-4, 5-difluoro-phenylhydrazino)-1Η-η-pyrazole-3-carboxylic acid 4-diethyl Aminomethylmercapto-benzylamine, φ 5-(2-chloro-4,5-difluoro-anthracenylamino)-1Η-pyrazole-3-carboxylic acid 3-diethylaminopurine Mercapto-benzylamine, 5-(2-Gas-4, 5-difluoro-anthracenylamino)-1Η-pyrazole-3-carboxylic acid 4-ethylaminopurinyl-benzylhydrazine Amine, 5-(2-chloro-4, 5-difluoro-anthraceneamino)-1Η-. Bis-zolyl-3-carboxylic acid 3-ethylaminomercapto-benzylamine, 5-(2-chloro-4,5-difluoro-benzoinyl)-1Η-pyrazole-3- Carboxylic acid 4-aminomercapto-benzylamine, 5-(2-chloro-4,5-difluoro-benzylidenylamino)-1Η-pyrazole-3-carboxylic acid 132 318197 〇1322688 ( 1-acid oxalate-σ bottom bit-4-yl)-propyl-bristamine, 5-(2-chloro-4,5-difluoro-benzylidenylamino)-1Η-pyrazole-3 -carboxylic acid (1-carboxyethyl-piperidin-4-yl)-propyl-decylamine, 5-(2-chloro-4,5-difluoro-benzylidenylamino)-1Η-pyridyl [3-(2-carboxypropenyl)-piperidin-4-yl]-propyl-decylamine, 5-(2-chloro-4, 5-difluoro-benzoinyl) Amino)-1Η-indazole-3-carboxylic acid cyclopropyl-(6-decyloxy-pyridin-3-ylindenyl)-decylamine, 5-(2- gas-4, 5-difluoro- Benzoylamino)-1Η-η-pyrazole-3-carboxylic acid chuncyclobutyl-(6-methoxypyridin-3-ylmethyl)-decylamine, 5-(2-gas-4 , 5-difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid cyclopropyl decyl-(6-methoxypyridin-3-ylmethyl)-decylamine, 5- (2-chloro-4,5-difluoro-benzylidenylamino)-1Η-pyrazole-3-carboxylic acid (6-didecylamino-pyridin-3-ylindenyl)-decylamine, 5-( 2-Chloro-4, 5-difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid (6-didecylamino-pyridin-3-ylindenyl)-propyl-oxime Amine, 0 5-(2-chloro-4,5-difluoro-phenylhydrazinoamino)-111-pyrazole-3-carboxylic acid benzyl-(2-mercapto-ethyl)-bristamine 5-(2-chloro-4,5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylic acid benzyl-(2-ethoxy-yl-ethyl)-bristamine, 5-(2-Gas-4, 5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylic acid (6-chloro-pyridin-3-ylindenyl)-propyl-oxime Amine, 5-(2-chloro-4, 5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid 2,6-di-benzylamine, 5-(2-chloro -4,5-difluoro-benzoylamino acid 133 318197 1322688 (3, 5-dichloro-pyridin-4-ylindenyl)-nonylamine, 5-(2-chloro-4, 5-dioxo-benzoquinoneamino)-1Η-0 to 0 sits-3-oxo acid (3,5-dichloro-pyridin-4-ylindenyl)-propyl-nonylamine, 5-( 2-Chloro-4, 5-difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid • [6-(1Η-pyrazole-buyl)-pyridin-3-ylindenyl] - indoleamine dihydrochloride, 5-(2-chloro-4,5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid [6-(4-hydroxy-pyridinidine- 1-yl)-pyridin-3-ylindole ]-nonylamine dihydrochloride, 5-(2-chloro-4, 5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid Φ (2-pyridin-2-yl) -ethyl)-decylamine, 5-(2-chloro-4,5-difluoro-benzoylaminopyrazole-3-carboxylic acid (2-pyridin-3-yl-ethyl)-decylamine , 5-(2-chloro-4, 5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylic acid (2-pyridin-4-yl-ethyl)-decylamine, 5- (2-Chloro-4, 5-difluoro-benzylidenylamino)-1Η-pyrazole-3-carboxylic acid (4-[1,2,3]thiadiazol-4-yl-benzyl) - indoleamine, 0 5-(2-chloro-4,5-difluoro-phenylhydrazino)-111-°-pyrazole-3-carboxylic acid (5-methyl-pyroxy-2-yl- Indenylamine, decylamine, 5-(2-chloro-4,5-difluoro-phenylhydrazinoylamino)-1 Η-pyrazole-3-carboxylic acid pyridin-2-yl decylamine, 5-( 2-ox-4,5-difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid lysyl-5-ylamine, 5-(2-chloro-4, 5-difluoro- Benzyl decylamino)-1 Η-pyrazole-3-carboxylic acid -8-8-yl decylamine, 5-(2-chloro-4, 5-difluoro-benzylidenylamino)-1 Η- «Bizozole-3-carboxylic acid 134 318197 1322688 isoindolin-5-yl-decylamine, 5-(2-chloro-4,5-difluoro-abidomethylamino)_1{1-. 〇 -3- 缓 缓 [3-ethoxy-5-(1-ethoxyl-1-yl-ethyl) than bit-2-yl-guanamine, 5-(2-chloro -4,5-difluoro-benzoinylamino)-;[{{-«» than 〇--3_acid [3-ethoxy-5-(1-ethoxymethyl-1) -trans-yl-ethyl) than bit-2-yl-bristamine, 5-(2-gas-4, 5-difluoro-benzoquinoneamino)-ΐΗ-ηΛσ sit-3·"修 [5_(卜基基-1-indolyl-ethyl)-3-ethoxy-p-pyridin-2-yl]-indole' 5-(2-chloro-4, 5-difluoro-benzene Mercaptoamine)-1Η-0 ratio bite_3-carboxylic acid [5-(1-regi-I-carbyl-ethyl)-3-ethoxy-α than 唆-2-yl]- Γ Γ 5-(2-chloro-4, 5-difluoro-benzylidenylamino)-1 Η-pyrazole-3_carboxylic acid hydrazin-2-ylindenyl)-nonylamine, 5 -(2-Gas-4, 5-difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-hypoacid [6-(thiophene-4-yl)-0-biti-3-yl曱基]-Taking amine ' 0 5-(2-gas-4,5-difluoro-benzhydrylamino)-111-pyrazole _3-sodium acid [6-(1,1-diyl) -1 λ 6-thiophene _4-yl)-n ratio biting _3_ylmethyl]-bristamine, 5-(2-chloro-4, 5-difluoro-benzhydrylamino)-lH -pyrazole-3-buffer acid (4,5-dibromo-thiophen-2-ylmethyl)-decylamine, 5-( 2-Chloro-4, 5-difluoro-benzylidenylamino)-lH-pyrazole-3-reaction acid (5-a-thiophen-2-ylmethyl)-decylamine, 5-(2- Chloro-4, 5-difluoro-benzhydrylamino)-lH-pyrazole-3-hypoacid (4-ethyl-2-methyl- ° oxaβ--5-ylmethyl)- Amine, 318197 135 1322688 5-(2-Gas-4, 5-difluoro-phenylhydrazino)-1 Η-«Bizozole-3-carboxylic acid (2-ethyl-4-indenyl-acecible Zyrid-5-ylindenyl)-nonylamine dihydrochloride, 5-(2- gas-4,5-difluoro-benzoguanidino)-1indole-pyrazole-3. Carboxylic acid ([2, 2']bithiophenyl-5-ylindenyl)-decylamine, 5-(2- gas-4, 5-difluoro-benzoinyl)-1Η-pyrazole- 3-carboxylic acid (3-decyloxy-thiophen-2-ylindenyl)-decylamine, 5-(2- gas-4, 5-difluoro-benzoguanidino)-1Η-pyrazole- 3-carboxylic acid (4, 5-dioxa-thiophen-2-ylindenyl)-nonylamine, 5-(2-chloro-4, 5-difluoro-benzhydrylamino)-lH-indole Oxazole-3-carboxylic acid (2,5-dimercapto-oxazol-4-ylmethyl)-decylamine, 5-(2-chloro-4,5-difluoro-benzoinylamino)- 1-indole-pyrazole-3-carboxylic acid (2-hexyl-4-mercapto-oxazol-5-ylindenyl)-decylamine, 5-(2- gas-4, 5-difluoro-benzoinyl) Amino)-1Η-pyrazole-3-carboxylic acid (4-methoxy-thiophen-3-ylmethyl)-decylamine, 5-(2-chloro-4, 5-difluoro-phenylhydrazine Amino)-1Η-pyrazole-3-carboxylic acid (4-methyl-2-phenyl-oxazole-5-ylmethyl)-guanamine, 5-(2-gas-4, 5-difluoro -benzylideneamino)-1Η-pyrazole-3-carboxylic acid (2-mercapto-4-phenyl-oxazol-5-ylindenyl)-decylamine, 5-(2-gas-4 , 5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid (4-hexyl-2-mercapto-oxazol-5-ylindenyl)-guanamine dihydrochloride, 5-(2-chloro-4, 5-difluoro-benzoinylamino) -1Η-pyrazole-3-carboxylic acid (6-chloro-pyridin-3-ylmethyl)-decylamine, 5-(2-chloro-4, 5-difluoro-phenylhydrazino)-1Η -pyrazole-3-carboxylic acid (6-chloro-pyridin-3-ylindenyl)-decylamine dihydrochloride, 136 318197 1322688 5-(2-chloro-4,5-difluoro-benzoinyl Amino)-1Η-pyrazole-3-carboxylic acid (4H-[1,2,4]triazol-3-ylindenyl)-nonylamine 5-(2-chloro-4, 5-difluoro-benzene Mercaptoamine)-1Η-pyrazole-3-carboxylic acid (4H-[1,2,4]triazol-3-ylindenyl)-decylamine dihydrochloride, 5-(2-chloro- 4, 5-Difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid (5-fluoro-azolin-3-yl)-decylamine 5-(2-gas-4, 5- Difluoro-benzoguanidino)-1Η-pyrazole-3-carboxylic acid (5-fluoro-4H-quinazolin-3-yl)-guanamine dihydrochloride, 5-(2-chloro- 4,5-difluoro-benzoguanidino)-1Η-α-pyrazole-3-carboxylic acid (4,6-dimercapto-pyridin-3-ylindenyl)-nonylamine, 5-(2 -Chloro-4,5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid (4,6-dimercapto-pyridin-3-ylindenyl)-decylamine dihydrochloride Salt, 5-(2-chloro-4, 5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylic acid (2-methoxy-6-methyl-pyridin-3-yl) Mercapto)-nonylamine, 5-(2-chloro-4, 5-di -benzylideneamino)-1Η-carbazole-3-carboxylic acid (4-methoxy-6-indenyl-pyridin-3-ylindenyl)-decylamine, 5-(2-chloro-4 ,5-difluoro-benzoquinone-based amine)_111-〇 〇 -3-3 - tempering acid (4-methoxy-6-methylpyridin-3-ylindenyl)-guanamine dihydrochloride Salt, 5-(2- gas-4, 5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylic acid (2-decyloxy-4,6-dimercapto-pyridine- 3-ylmethyl)-nonylamine, 5-(2-chloro-4,5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid (2-decyloxy-4, 6-Dimethylpyridin-3-ylmercapto)-decylamine dihydrochloride, 5-(2-Gas-4,5-difluoro-benzoinyl)-1Η-pyrazole-3 -carboxylic acid (3-methyl-pyridin-2-ylindenyl)-nonylamine, 137 318197 1322688 5-(2-chloro-4,5-difluoro-benzoylamino)-1Η-11 ratio坐3--3- oxo acid (5-methyl-pyridin-3-ylindenyl)-nonylamine, 5-(2-chloro-4,5-di-phenyl- decanoylamino)-1Η-σΛσ Sit-3-reaction (6-mercapto-indenyl-3-methyl)-nitramine, • 5-(2-chloro-4, 5-difluoro-phenylhydrazino)-1Η -pyrazole-3-carboxylic acid (6-fluorenyl-pyridin-2-ylindenyl)-decylamine, 5-(2,4-dioxa-5-fluoro-phenylnonylamino)-1Η -pyrazole-3-carboxylic acid (pyridin-3-ylindenyl)-guanamine dihydrochloride, ^ 5-(2-gas-4, 5-difluoro-phenylhydrazino)-1Η- Pyrazole-3-carboxylic acid (6-fluoro-pyridin-3-ylmethyl)-guanamine dihydrochloride, 5-(2-chloro-4,5-difluoro-benzoinyl)- 1Η-indopazole-3-carboxylic acid (3-endo-phenyl)-methyl-bristamine, 5-(2-chloro-4, 5-difluoro-phenylhydrazino)-1Η- Pyrazole-3-carboxylic acid 3-indolesulfonylamino-benzylamine, 5-(2-chloro-4,5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylate Acid 0 4-methyl decylamino-branched amine, 5-(2-chloro-4, 5-difluoro-benzhydrylamino)-1 Η-pyrazole-3-carboxylic acid 3- acetyl Amino-benzylguanamine, 5-(2-chloro-4,5-difluoro-phenylhydrazino)-1Η-indazole-3-carboxylic acid 4-acetamido-benzylamine, 5 -(2-chloro-4, 5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid (2-phenyl-thiazol-4-ylmethyl)-decylamine, 5- (2-Chloro-4, 5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylic acid ((R)-phenyl-ethyl)-decylamine, 138 318197 1322688 5- (2-Chloro-4, 5-difluoro-phenylhydrazino)-1Η-η-pyrazole-3-carboxylic acid ((S)-l-phenyl-ethyl)-bristamine, 5-( 2-chloro-4, 5-di -phenylphenylamino)-1Η-pyrazole-3-carboxylic acid • (6-phenoxy-pyridin-3-ylmercaptodecylamine dihydrochloride, 5-(2-indolyl-4, 5-difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid (6-chloro-pyridin-3-ylindenyl)-decylamine dihydrochloride, 5-(2-chloro- 4, 5-Difluoro-benzylidenylamino)-1Η-°biazole-3-carboxylic acid (2-chloro-pyridin-3-ylindenyl)-decylamine dihydrochloride, # 5-( 2-mercapto-4, 5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid (6_gas_0 than bite_3_ylindenyl)-branched amine salt 5-(2-chloro-4,5-difluoro-benzylidenylamino)-1Η-pyrazole-3-carboxylic acid [1-(pyridin-3-yl)-ethyl]-nonanimide di-salt Acid salt, 5-(2- gas-4, 5-difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid (2-fluoro-pyridin-3-ylindenyl)-decylamine Dihydrochloride, 5-(2-Gas-4, 5-difluoro-benzylidenylamino)-1Η-trazole-3-carboxylic acid φ (2-indolyl-pyridin-3-ylfluorenyl) - indoleamine dihydrochloride, 5-(2-chloro-4, 5-difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid (biphenyl-3-ylmethyl) - guanamine, 5-(2-chloro-4,5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylic acid ((lR,2S)-2-hydroxy-hydroquinone-1 -yl)-guanamine , 5-(2-chloro-4, 5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylic acid ((lS,2R)-2-hydroxy-hydroquinone-bu)- Indoleamine, 5-(2-chloro-4, 5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylic acid (6-phenyl-pyridin-3-ylindenyl)-oxime Amine dihydrochloride, 139 318197 1322688 5-(2-Gas-4,5-difluoro-benzoindolyl)-1Η-η-pyrazole-3-carboxylic acid (6-fluorenyl-pyridine-3 -hydrazinyl)-indole hydrochloride, 5-(2-chloro-4,5-difluoro-benzoinylamino)_1Η_ο than 0 benzoic acid benzyl-mercapto-nonylamine, 5- (2-Chloro-4, 5-difluoro-benzimidyl)-1Η-pyrazole-3-carboxylic acid benzamide, 5-(2-chloro-4, 5-difluoro-phenylhydrazine Amino-pyridyl-3-carboxylic acid phenyl decylamine, 5-(2-chloro-4,5-difluoro-phenylhydrazinoamino)-1 fluorene-pyrazole-3-carboxylic acid Methyl-phenyl-decylamine, 5-(2-chloro-4, 5-difluoro-benzhydrylaminopyrazole-3-carboxylic acid (Bridden-1-yl)-imidamine, 5- (2-Chloro-4,5-difluoro-phenylhydrazino)-1Η-°biazole-3-carboxylic acid (4-ethoxycarbonyl-piperidin-1-yl)-decylamine, 5 -(2-chloro-4,5-difluoro-benzoindolyl)-1Η-pyrazole-3-carboxylic acid (4-indolyl-piperidin-1-yl)-decylamine, 5-( 2-chloro-4, 5-difluoro-phenylhydrazinoamino)-1 fluorene-indazole-3-carboxylic acid (4-keto-α-heptan-1-yl)-nitramine, 5-(2-chloro-4, 5 -difluoro-phenylhydrazinoamino)-1Η-°biazole-3-carboxylic acid phenethyl decylamine, 5-(2-chloro-4, 5-difluoro-benzhydrylamino)- 1Η-pyrazole-3-carboxylic acid mercapto-phenethyl-decylamine, 5-(2-chloro-4, 5-difluoro-benzylidenylamino)-1Η-pyrazole-3-carboxylic acid Ethyl-phenyl-bristamine, 140 318197 1322688 5-(2-Gas-4, 5-difluoro-anthracenylamino)-1Η-pyrazole-3-carboxylic acid benzene (1,2,3 , 4-tetrahydroisoquinolin-2-yl)-nonylamine, 5-(2- gas-4, 5-difluoro-acidylamino)-1Η-σ-pyrazole-3-carboxylic acid ( (S)-a-decyloxy-benzyl-benzyl)-decylamine, 5-(2- gas-4, 5-difluoro-phenylhydrazinoyl)_1H-pyrazole-3-carboxylic acid ( (R)-a-methoxycarbonyl-benzyl)-decylamine, 5-(2-gas-4,5-difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid benzene (1,2,3,4-tetrahydroindenyl-1 -yl)-bristamine, ^ 5-(2- gas-4, 5-difluoro-phenylhydrazino)-1Η-pyrazole 3-carboxylic acid phenyl-propyl-bristamine' 5-(2-gas-4,5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid butyl-phenyl - guanamine, 5-(2- -4, 5-difluoro-benzhydrylamino)-1Η-°biazole-3-carboxylic acid pentyl-phenyl-bristamine, 5-(2-chloro-4, 5-difluoro-benzene Hydrazinyl)-1H-d-pyrazole-3-carboxylic acid φdiphenylhydrazine-decylamine, 5-(2- gas-4,5-difluoro-benzoylamino)_1Η-° Benzene-o-acid (pyridin-2-ylindenyl)-decylamine hydrochloride, 5-(2-chloro-4,5-difluoro-benzylidenylamino)-1Η-pyrazole 3-carboxylic acid (pyridin-4-ylindenyl)-decylamine hydrochloride, 5-(2-chloro-4,5-difluoro-benzoinyl)-1Η-pyrazole-3- Carboxylic acid (00-2-hydroxy-1-phenyl-ethyl)-decylamine, 5-(2-chloro-4,5-di-n-benzoylamino)-111-0 _ acid ((S)_2-carbyl-1-phenyl-ethyl)-nitramine, 141 318197 1322688 5-(2-chloro-4, 5-difluoro-abidomethylamino)-ΐΗ -η ratio tr -3- s-acid 4-didecylamino-benzylamine, 5-(2- gas-4, 5-difluoro-benzoylamino)-iH-indole saliva- 3-dihydro acid (furan-2-ylmethyl)-decylamine, 5-(2-chloro-4,5-difluoro-phenylglycosylamino)-ΐΗ-π than salivary-3-deoxy Thiophen-2-ylindenyl)-nonylamine, 5-(2-chloro-4,5-difluoro-benzofuranylamino)-1H-d than indole-3-indole (2-methoxyl) -benzene - indoleamine, 5-(2- gas-4,5-difluoro-benzoylamino group 〇 竣-3-decanoic acid (2-decyloxy-phenyl)-indenyl-bristamine, 5-(2- gas-4,5-difluoro-benzoquinone-amino-azino-acid 4-dimethylamino-benzylamine hydrochloride, 5-(2- gas-4, 5-difluoro-benzoylamino)-1Η-° ratio 嗤-3-carbamic acid 3-amino-benzylamine, 5-(2- gas-4, 5-difluoro-phenylhydrazine Amino)-ΐΗ_〇 ratio. Sodium-3-indole 4-amino-benzylamine, 5-(2-gas-4,5-difluoro-phenylhydrazino)-111-indole ratio 2-methyl-tuberamine, 5-(2-chloro-4, 5-difluoro-benzoguanidino)-lH-n ratio jun-3-decanoic acid 3-methyl-tuberamine 5-(2-chloro-4,5-difluoro-benzofuranylamino)-ΐΗ-πΛβ--3-carboxylic acid 3-dimethylamino-benzamide, 5-(2-chloro- 4,5-difluoro-benzoinylamino)-111->1 than saliva-3-retinic acid (2-methoxy-indole-p--3-ylmethyl)-bristamine, 142 318197 1322688 5-(2-Gas-4, 5-difluoro-benzoinylamino)-1Η-0 ratio. Sodium-3-Resin 2-Chloro-tuberamine ' 5-(2-Chloro-4, 5-difluoro-benzhydrylamino)-1Η-indazole-3-carboxylic acid 3-Chloro-benzyl Indoleamine, • 5-(2-chloro-4, 5-difluoro-benzhydrylamino)-1Η-β-pyrazole-3-carboxylic acid 3-decyloxycarbonyl-benzylamine, 5-( 2-Chloro-4, 5-difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid 3-enyl-nodal amine ' ^ 5-(2-chloro-4, 5-di Fluoro-benzimidyl)-1Η-°biazole-3-carboxylic acid (6-trifluorodecyl-pyridin-3-ylmethyl)-decylamine, 5-(2-chloro-4, 5 -difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid (2-ethoxy-n-pyridin-3-ylmethyl)-decylamine, 5-(2-chloro-4 , 5-difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid (2-dimethylamino-ethyl)-bristamine' 5-(2-chloro-4, 5_ Difluoro-benzoguanidino)-1Η-pyrazole-3-carboxylic acid φethyl-(2-didecylamino-ethyl)-guanamine dihydrochloride, 5-(2-chloro -4,5-difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid cyclohexyl-(2-dimethylamino-ethyl)-decylamine, 5-(2-chloro -4,5-difluoro-phenylhydrazinoamino)- 1 -pyrazol-3-carboxylic acid (4-methoxy-indolyl-2-ylmethyl)-decylamine, 5-(2 -chloro-4, 5-difluoro- Benzoylamino)-1Η-pyrazole-3-carboxylic acid (2,6-dimethoxy-pyridine-3-ylindenyl)-decylamine, 5-(2-gas-4,5- Difluoro-benzoinylamino)-1Η-0 to 嗤-3-indolizan 2 monomethoxycarbonylcarbonyloxy-benzylamine, 143 318197 1322688 5-(2-gas-4, 5-di Fluoro-benzoguanidino)-1H-pyrazole_3_carboxylic acid 2-carboxydecyloxy-benzylamine, 5-(4,5-difluoro-2-indolyl-benzylguanamine)- 1H-pyrazolecarboxylic acid methyl 'oxy-pyridin-3-ylindenyl)-nonylamine, • 5-(2,4-dichloro-benzylguanamine)-1Η-pyrazole-3-carboxylic acid (6 _ 曱 methoxy-pyridin-3-ylmethyl)-decylamine, 5-(2- gas-4, 5-difluoro-benzhydrylamino group sitting on a 3-reposter (3,5-dimethyl Oxy-pyridin-4-ylindenyl)-decylamine '5-(4,5-difluoro-2-methyl-benzylguanamine)-1Η-pyrazole-3-carboxylic acid (2, 4-di Methyl-oxazole-5-ylmercapto)-decylamine, 5-(2,4-dioxa-5-fluoro-benzylamine)-1-indole-pyrazole-3-carboxylic acid (2,4-dimethyl 5-oxazol-5-ylmercapto)-decylamine, 5-(2-aza-4,5-difluorophenylhydrazinoyl)-1Η-pyrazole-3-carboxylic acid (4-methoxyl) Carbonyl-phenyl)-mercapto-nonylamine, 5-(2- gas-4,5-difluoro-benzoguanidino)-1Η-pyrazole-3 -carboxylic acid φ (4-carboxyphenyl)-methyl-decylamine, 4-{[5-(2-chloro-4, 5-difluoro-benzylidenylamino)-111_0 than 〇-3 -carbonyl]-methyl-amino}-benzoic acid sodium salt, 5-(2- gas-4,5-difluoro-benzoylamino)-1Η-0 ratio 0 sitting-3-oxo acid isopropyl -Phenyl-bristamine, 5-(2- gas-4, 5-difluoro-benzoamitoyl)-1Η-pyrazole-3-carboxylic acid (ethoxymethyl-methyl)- Phenyl-bristamine, 5-(2- gas-4, 5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid (carboxy-methyl)-phenyl-decylamine, 144 318197 1322688 5-(2-Chloro-4-oxo-benzhydrylamino)-iH-0 is 0 -3- benzoic acid benzylamine, 5-(2,4-dichloro-benzoquinone Benzyl)-1Η-β-pyrazole-3-carboxylic acid benzamide, 5-(2-chloro-5-fluoro-adolylamino group (2-Chloro-4, 5-difluoro-phenylhydrazino)-lH-pyrazole-3-carboxylic acid benzyl-styl-bristamine 5-(2-chloro-4,5-di Fluoro-benzoylamino)-1Η-° ratio 0 竣-3-decanoic acid (1_mercapto-1-phenyl-ethyl)-nitramine, 5-(2-gas-4, 5- Difluoro-phenylhydrazinoamino)-lH-pyrazole-3-carboxylic acid [2-keto-2-oxan-1-yl)-ethyl]-phenyl-bristamine, 5_ (5 -fluorine -2-mercapto-phenylhydrazinoamino)-iH-pyrazole-3-carboxylic acid amine, 5_(5-gas-2-mercapto-benzoglylamino)-1(]_1 * ° 坐 竣 竣 竣 醯 , ,, 5-(4-methoxy-2-methyl-benzylidenylamino)-iH-pyrazole-3-buprole bromide, 5- (4-Ga-2-methyl-benzoylamino)-iH-indole-3-indenyl decylamine, 5-(5-fluoro-2-methoxy-benzhydrylamino) )-ih-pyrazole-3-buminated acid benzamide ' 5-(5-gas-2-methoxy-benzhydrylamino)-ih-pyrazole-3-carboxylic acid benzamide 145 318197 1322688 5-(2-Chloro-4,5-difluoro-phenylhydrazino)-1 Η-pyrazole-3-carboxylic acid (2-ethoxy-ethyl)-styl-decylamine , 5-(2-Fluoro-5-methyl-phenylhydrazino)-1Η-pyrazole-3-carboxylic acid decylamine, ' 5-(5-chloro-2-fluoro-phenylhydrazino) Amino)-1Η-pyrazole-3-carboxylic acid benzamide, 5-(3-aero-2,6-difluoro-benzylidenylamino)-1Η-pyrazole-3-carboxylic acid Amine, ® 5-(2-chloro-3-fluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylic acid benzamide, 5-(2-chloro-4, 5-difluoro-benzene Mercaptoamino)-1Η-pyrazole-3-carboxylic acid ethylamino methoxymethyl-phenyl-bristamine, 5-(2-chloro-4,5-difluoro-phenylhydrazine Amino)-111-pyrazole-3-carboxylic acid isobutyl-phenyl-decylamine, 5-(2-gas-4,5-difluoro-benzoguanidino)-1Η-pyrazole- 3-carboxylic acid • (2-methoxycarbonyl-ethyl)-phenyl-decylamine, 5-(2-milo-4,5-digas-benzoinylamino)-lH-nit〇- 3-acidic acid (3-ethoxycarbonyl-propyl)-phenyl-decylamine, 5-(2-fluoro-4,5-difluoro-benzoinylamino)-1Η-0 ratio 0 sitting- 3-Resin (2-carboxy-ethyl)-phenyl-decylamine, 5_(2- gas-4,5-difluoro-benzoinylamino)-1Η-σ ratio 0 sitting-3-rebel Acid (3-carboxy-propyl)-phenyl-decylamine, 5-(2-hydroxy-4-decyloxy-benzylidenylamino)-1Η-pyrazole-3-carboxylic acid amine, 146 318197 1322688 '^azole-3-carboxy-5-(2-hydroxy-5-methoxy-phenylhydrazinyl)-1 η, benzamide, amide-(5-fluoro-2-hydroxyl) - benzhydrylamino)-1 Η-pyrazole, 3, carboxylic acid benzyl azole -3 carboxy-(4-fluoro-2-trifluoromethyl-phenylhydrazino)-1 Η.  Benzoylamine, 5-(5-fluoro-2-trifluoromethyl-benzhydrylamino)-111, is called, ^ & azole-3-carboxybenzylamide,

5-(2-chloro-4,5-difluoro-benzhydrylamino)-1Η-pyridone, 3-hypo-acid (2-methoxy-ethyl)-phenyl-bristamine, 5 -(2,5-didecyl-phenylhydrazinylamino)-1Η_° than olfactory ~3, slow-acting stimulating amine, guanamine benzylamine amide benzyl amide 5-(2-gas -pyridine-3-carbonylamino)-lH-pyrazole-3~ 5-(4-chloro-pyridine-2-carbonylamino)-lH-pyrazole-3~-branched amine,-(2,6-di Gas-pyridine-3-carbonylamino)-1Η-pyrazole, 3-decanoic acid 5-(2- gas-4, 5-difluoro-benzoquinoneamino)-1Η~η ratio. -3-s-acid butyl-(4-ethoxycarbonyl-phenyl)-decylamine, 5-(2-indole-4, 5-difluoro-benzoquinoneamino)-1Η-%Π Sit-3-butyl phthalate-(4-reyl-phenyl)-bristamine, 5-(2-mercapto-pyridine-3-carbonylamino)-1Η-pyrazole~3~dicarboxylic acid Amine, 318197 147 1322688 5-(2-Ga-6-methyl-pyridine-3-carbonylamino)-1 Η-pyrazole-3-carboxylic acid benzamide, 5-(3-chloro-pyridine-4 -carbonylamino)-ιη-pyrazole-3-carboxylic acid benzamide, 5-(2- gas-4, 5-difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid Butyl-(4-ethoxycarbonylmercapto-phenyl)monodecylamine, 5-(2-chloro-4,5-difluoro-phenylhydrazinoyl)-lH-pyrazole-3-carboxylate Acid butyl-(4-carboxyindenyl-phenyl)-decylamine, 5-(2-gas-4, 5-difluoro-phenylhydrazinoyl)-lH-pyrazole-3-carboxylic acid# (4-decyloxycarbonyl-phenyl)-(2-methoxy-ethyl)monodecylamine, 5-(2-gas-4,5-difluoro-benzhydrylamino)-111- Pyrazole-3-carboxylic acid (4-carboxy-phenyl)-(2-methoxy-ethyl)-decylamine, 5 (2 gas - 4,5_-gas-benzoylamino)-1Η_ο 〇3_ _3_ 叛 acid (6 - methoxy-n than bit-3-yl methyl) _ guanamine di-salt Acid salt, 5-(2-methyl-4, 5-difluoro-phenylhydrazinyl)-ιη-pyrazole-3-carboxylic acid (6-decyloxy-pyridin-3-ylindenyl)醯 醯 amine dihydrochloride, Lu 5-(2-chloro-4, 5-difluoro-phenylhydrazino)-ιη-pyrazole-3-carboxylic acid ( sold in 嗤-4-yl fluorenyl) -Acetamine dihydrochloride, 5-(2-Gas-4, 5-difluoro-benzhydrylamino)_1Η-pyrazole_3_carboxylic acid 4-[2-(Merlin-4-yl) )-ethylaminomercapto]-benzylguanamine dihydrochloride, 5-(2-gas-4,5-difluoro-benzhydrylamino)-indole-pyrazole-3-carboxylic acid 4 -(morpholin-4-ylaminoindolyl)-benzylamine dihydrochloride, [4-({[5-(2-gas-4,5-difluoro-benzhydrylamino)) -111-pyrazole-3-carbonyl]-amino}-indenyl)-azanocarbazide]-sodium acetate, 3-[4-({[5-(2- gas-4, 5-) Fluoro-benzhydrylamino)-1Η-°bazole 148 318197 1322688 -3-carbonyl]-amino}-methyl)-benzoguanidino]-propionic acid sodium salt, [5-(2- Gas-4, 5-difluoro-phenylhydrazinoamino)-lH-pyrazole-3-carboxylic acid (3,5-dimercapto-isoxazole-4-ylindenyl)-nonylamine hydrochloride Salt, [5-(2-gas-4, 5-difluoro-benzhydrylamino)-1Η-pyrazole-3-hypoacid (1,3,5-trimethyl-1H-pyrazole- 4-base group - guanamine dihydrochloride, 5-(2-chloro-4, 5-difluoro-phenylhydrazino)-1Η-pyrazole-3-hypoacid (3, 5-dimercapto-isoxine) Zyzol-4-ylindenyl)-nonylamine mesylate, 5-(2- gas-4, 5-difluoro-phenylhydrazino)-1Η-pyrazole-3-hygroic acid® 3- [2-(morpholin-4-yl)-ethylaminocarbamimidyl]-benzylguanamine dihydrochloride, 5-(2- gas-4, 5-difluoro-benzoinyl) -1Η-pyrazole-3-carboxylic acid 3-(morpholin-4-ylaminoindolyl)-benzylguanamine dihydrochloride, 5-(2-chloro-4, 5-difluoro-benzoic acid醯-ylamino)-1Η-πϋ〇 sitting-3-o-acid {2-[2-(morphin-4-yl)-ethylaminomethylindenyl]-π butyl-4-ylmethylhydrazine Amine trihydrochloride, 5-(2-chloro-4,5-difluoro-benzoinylamino)_1Η-° ratio 0 sit-3-acid [2-(Merlin-4-ylamino) Brewing base)-<»Phenyl-4-ylindenyl]-bristamine trihydrochloride, 5-(2-chloro-4,5-difluoro-benzhydrylamino)-111-indole . -3 -decanoic acid (6-methoxy-pyridin-3-ylindenyl)-decyl methanesulfonate, 5-(2-chloro-4,5-difluoro-benzoylamino) -1Η-° ratio 0 -3-acid (6-methoxy-pyridin-3-ylindenyl)-decylamine hemisulfate, 5-(2-chloro-4, difluoro-benzamide Amino)-1Η-π ratio 0 sit-3-protective acid (3,5-dimethoxy-pyridin-4-ylindenyl)-decylamine dihydrochloride, 5_(2 - gas-4,5 -difluoro-benzoinylamino)-111-11biw-3-dicarboxylic acid 318197 149 1322688 (4-aminomethyl-pyridin-2-ylmethyl)-decylamine trihydrochloride, 5 -(2- gas-4, 5-difluoro-benzylideneamino)-1Η-π ratio. Sodium-3-carboxylic acid (6-chloro-pyridin-3-ylmethyl)-decyl methanesulfonate, 5-(2- gas-4, difluoro-benzoylaminopurine-3- Acid '(6-Gas-pyridin-3-ylmethyl)-guanamine dioxime sulfonate, 5-(2-chloro-4, 5-difluoro-benzoquinoneamino)-1Η-0 ratio Salic-3-oxo acid (2,4-dimethyl-pyridin-3-ylmethyl)-decylamine hydrochloride, 5-(2-gas-4, 5-difluoro-benzoinylamino) )-1Η-° ratio. Sodium-3-acidic acid® (pyridin-3-ylmercapto)-decylamine hydrochloride, 5-(2-chloro-4, 5-difluoro-benzoylamino) Benzyl phthalic acid (6-methoxy-pyridin-3-ylmethyl)-propyl-decylamine dihydrochloride, 5-(2-chloro-4,5-difluoro-phenylhydrazine Alkyl)-1Η-σ ratio® sit-3-decanoic acid [6-(piperidinyl-bu)-pyridin-3-ylindolyl]]-nonylamine dihydrochloride, 5-(2-chloro -4,5-difluoro-phenylhydrazinoamino)-111-. than saliva-3-acid [6-(morpholin-4-yl)-pyridin-3-ylindenyl]]-decylamine Dihydrochloride, φ 5-(2-chloro-4, 5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylic acid (3,5-dichloro-pyridin-4-yl Indoleamine-p-amine hydrochloride, 5-(2-chloro-4,5-difluoro-benzylidenylamino)-1-pyridazole-3-carboxylic acid (6-didecylamino)- Pyridine Pyridyl-3-ylmethyl)-guanamine dihydrochloride, 5-(2- gas-4, 5-difluoro-benzylidenylamino)-1Η-pyrazole-3-carboxylic acid (6- Dimethylamino-pyridyl~3-ylmethyl)-propyl-decylamine dihydrochloride, 5-(2-gas-4,5-difluoro-benzhydrylamino)-1Η-pyridyl Oxazole-3-carboxylic acid (6-diethylamino-pyridin-3-ylmethyl)-guanamine dihydrochloride, 5-(2-chloro-4, 5-difluoro-benzoguanamine Base)-1Η-pyrazole-3-carboxylic acid 150 318197 1322688 (6-chloro-2-didecylamino-pyridin-3-ylindenyl)-guanamine dihydrochloride, 5-(2-chloro -4,5-difluoro-benzhydrylamino)-1Η-indazole-3-carboxylic acid (4-[1,2,3]thiadiazol-4-yl-benzyl)-nonylamine salt Acid salt, 5-(2- gas-4, 5-difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid (4-methyl-thiazol-5-ylmethyl)-indole Amine hydrochloride, 5-(2- gas-4, 5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylic acid (2,4-dimercapto-thiazol-5-yl) Sulfhydryl)-decylamine hydrochloride, 5-(2- gas-4, 5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylic acid·[6-(4-hydroxy- Piperidin-1-yl)-pyridin-3-ylindenyl]-nonylamine dihydrochloride, 5-(2-chloro-4,5-difluoro-benzoguanidino)-1Η-carbazole -3 -carboxylic acid 5-methyl-pyroxy-2-ylguanamine dihydrochloride, 5-(2-gas-4,5-difluoro-benzylidenylamino)-1Η-pyrazole-3- Carboxylic acid quinoline-5-ylguanamine dihydrochloride, 5-(2-chloro-4,5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylic acid quinoline-8 - ketamine dihydrochloride, φ 5-(2-chloro-4, 5-difluoro-benzylidenylamino)-1 Η-pyrazole-3-carboxylic acid isoquinolin-5-yl decylamine Dihydrochloride, 5-(2-chloro-4, 5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylic acid [6-(4-mercapto-peptidin-1-yl) )-pyridin-3-ylindenyl]-nonylamine dihydrochloride, 5-(2-chloro-4,5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylic acid [ 6-(4-Didecylamino-piperidin-1-yl)-pyridin-3-ylmethyl]-indolyl dihydrochloride, 5-(2-chloro-4, 5-difluoro-benzene Nonylamino)-1Η-pyrazole-3-carboxylic acid [6-(pyrrolidinyl-bu)-pyridin-3-ylindenyl]-nonylamine dihydrochloride, 151 318197 8 1322688 5-( 2-Chloro-4, 5-difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid (pyroxy-2-ylmethyl)-guanamine dihydrochloride, 5-(2 -chloro-4,5-difluoro-phenylhydrazinoamino)-1Η-«biazole-3-carboxylic acid '[6-(thiomorpholin-4-yl)-pyridin-3-ylmethyl] - guanamine Dihydrochloride, 5-(2-chloro-4,5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylic acid [6-(1,didone-1 λ 6 -thiomorpholin-4-yl)-pyridin-3-ylmethyl]-nonylamine dihydrochloride, 5-(2-gas-4,5-difluoro-benzhydrylamino)-1Η- °Bizozol-3-carboxylic acid®Aminomethylmercaptomethyl-decylamine, 5-(2,4-dioxa-5-fluoro-benzoindolyl)-1Η-carbazole-3-carboxylate Acid (4-aminomethylindenyl-phenyl)-methyl-nonylamine, 5-(2,4-dichloro-5-fluoro-benzoindolyl)-1Η-pyrazole-3-carboxylate Acid methyl-(4-decylaminomethylindenyl-phenyl)-decylamine, 5-(2,4-dioxa-5-fluoro-benzoguanidino)-1Η-pyrazole-3 -carboxylic acid (4-dimethylaminodecyl-phenyl)-indolyl-decylamine, φ 5-(2-chloro-4, 5-difluoro-benzoinyl)-1Η- Pyrazole-3-carboxylic acid (4-oxasulfonylaminocarbonyl-phenyl)-mercapto-nonylamine, 5-(2-chloro-4,5-difluoro-benzhydrylamino)- 1-indole-pyrazole-3-carboxylic acid (4-oxasulfonylaminocarbonyl-phenyl)-indolyl-decylamine sodium salt, 5-(2-gas-4, 5-difluoro-benzhydryl) Amino)-1Η-. Bis-zolyl-3-carboxylic acid (4-cyano-phenyl)-indolyl-decylamine, 5-(2-chloro-4,5-difluoro-benzoinyl)-1Η-pyrazole- 3-carboxylic acid decyl-[4-(4Η-[1,2,4]triazol-3-yl)-phenyl]-indolyl hydrochloride, 5-(4-azido-2- gas- 5-fluoro-benzoguanamine)-1Η-pyrazole-3-carboxylic acid 152 318197 1322688 (4-ranyl-benyl)-mercapto-bristamine, 5-(4-azido-2-chloro -5-fluoro-benzoguanamine)-1Η-pyrazole-3-carboxylic acid methyl-[4-(1Η-tetrazol-5-yl)-phenyl]-nonylamine, 5-(2- Gas-4, 5-difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid* [4-(N-hydroxyaminoiminoindolyl)-phenyl]-indenyl-anthracene Amine, 5-(2- gas-4, 5-difluoro-benzoquinoneamino)-ΐΗ-σ ratio sit-3-carboxylic acid methyl-[4-(5-keto-2,5- Dihydro-[1,2,4]oxadiazol-3-yl)-phenyl]-bristamine, • 5_(2- gas-4, 5-difluoro-benzhydrylamino)-ιη- Pyrazole-3-carboxylic acid {4-[(2'2-dimercapto-propenyloxy)-nonyloxycarbonyl]-phenyl-methyl-monodecylamine, 5 (2 chaotic-4, 5-fluoro) -benzimidylamino)-1Η-0 to 0 -3-retat 4-[Ν-methoxy-thiocarbonyloxyimine fluorenyl]-mercapto-amine, 5 (2 Rat-4,5-difluoro- Brewing arylamino)_1||-» than 〇 -3- 叛 叛 - -[4-(5-thioketo-4, 5-dihydro-[1,2, 4]oxadiazole- 3-yl)-phenoyl]-bristamine, 5-(2-chloro-4,5-difluoro-phenylhydrazinoyl)-1-indole-pyrazole-3-carboxylate-yl-[4-( 5-keto-4,5-dihydro-[1,2,4]thiadiazol-3-yl)-phenyl]-bristamine, 5 —(2_ gas-4,5-difluoro'• Benzoylamino)-1Η-pyrazole-3-carboxylic acid cyclohexyloxy-carbonyloxy)-ethoxycarbonyl]phenylindoleyl-nitramine, 5 (2-gas-4, 5-di Fluoro-benzoguanidino)1Η_pyrazole_3_carboxylic acid (4-ethoxycarbonyl-thiazol-2-yl)-ethyl-decylamine, 318197 153 1322688 5 (2-gas-4, 5-difluoro-benzhydrylamino group than saliva-3-retinic acid 2-methyl 26-bristylamino-tuberamine, 5-(2-chloro-4, 5-difluoro-benzimidamide Base)-ih-pyrazole-3-nonanoic acid 2-ethylammonium-tuberamine, 5-(2-gas-4, 5-difluoro-phenylhydrazino)-lH-pyrazole- 3-acidic acid 2-(dimethylamino-methyleneamino)-benzylamine hydrochloride, 5-(2-gas-4, 5-difluoro-benzhydrylamino)-1Η -pyrazole-3-carboxylic acid 3-(dimethylamino-ylideneamino)-benzylamine hydrochloride, • 5-(2-milk-4, 5-difluoro-phenylhydrazinoamino)-1H-b is more than 4-indole-3-acid di(didecylamino-methyleneamino)-benzylguanamine hydrochloride, 5-(2 - gas-4, 5-difluoro-phenylhydrazinoamino)-1 Η-pyrazole-3-carboxylic acid 2- [1-(didecylamino)ethylidene]-benzyl amide Hydrochloride, 5-(2-chloro-4, 5-difluoro-phenylhydrazino)-1Η-β is more than 3-benzyl-1-[1-(didecylamino)-ethylidene Aminoamino]-benzylguanamine dihydrochloride, 5-(2-chloro-4, 5-difluoro-benzoquinoneamino)-1Η-β ratio 0 sitting-3-decanoic acid φ 4-[1 -(didecylamino)ethylidene]-benzylguanamine dihydrochloride, 5_(2-chloro-4, 5-difluoro-benzoylamino)_1Η-σ than saliva-3 - Physic acid 2-(diethylamino-ylideneamino)-benzylguanamine dihydrochloride, 5-(2-gas-4, 5-difluoro-benzoquinoneamino)-1Η -° than saliva-3-sodium 3-(diethylamino-methyleneamino)-benzylamine dihydrochloride, 5-(2-gas-4, 5-difluoro-benzoic acid Aminoamine 嗤-3-teric acid 4-(diethylamino-methyleneamino)-benzylguanamine dihydrochloride, 5-(2-chloro-4, 5-difluoro-phenylhydrazine Stearic amine than 嗤-3-glycolic acid 2-imine ethylamino-benzylguanamine dihydrochloride' 154 318197 1322688 5-(2-Gas-4, 5-difluoro-phenylhydrazinyl H-pyrazole-3-carboxylate 3-iminoethylamino-benzylamine dihydrochloride, 5-( 2-Chloro-4, 5-difluoro-benzylidenylamino)_1H_pyrazole-3-carboxylic acid 4-imine ethylamino-benzylamine dihydrochloride, 5-(2-gas -4, 5-difluoro-benzhydrylaminopyrazole-3-carboxylic acid 4-cyano-tuberamine, 5-(2-chloro-4, 5-difluoro-benzhydrylamino) )_[H-pyrazole-3-carboxylic acid 3-[(2-fluoro-iminobenzyl)-amino]-benzylamine hydroiodide, ^ 5_(2-gas-4, 5 -difluoro-benzhydrylamino)-ih-pyrazole-3-carboxylic acid 4-[(2-fluoro-iminophenylphenyl)-amino]-benzylamine hydroiodide, 5 ( 2 gas 4,5-one gas-benzoquinone-based amine group)_1Η_ο than 0--3-indole 3-(3,3-dimethyl-ureido)-benzylamine, 5-(2-gas- 4, 5-difluoro-benzhydrylamino)-ih-pyrazole-3-carboxylic acid 4-(3,3-monomethyl-glycine)-tuberamine, 5-(2-gas- 4, 5-Difluoro-benzylidenylamino)-1Η-pyrazole-3-carboxylic acid φ 2-(methyl 4-phenylamino)-benzylamine, 5_(2•' gas- 4, 5-Difluoro-benzoylamino)-1Η-α ratio. Benzene 2-acid-6-fluoro-benzyl octaamine hydrochloride, 5_(2- gas-4, 5-diqi-benzoquinoneamino)-1Η_ο比〇 sitting-3- 2-acid 4-amino-4,5-difluoro-benzylguanamine hydrochloride, 5-(2-chloro-4,5-difluoro-benzoguanidinoamine MH-pyrazole-3-carboxylic acid (hydroquinone-1-yl)-bristamine, 5-(2-gas-4,5-difluoro-benzhydrylamino)-1Η-carbazole-3-derivative (argon-2-yl) )-N-amine, 155 318197 (Φ 1322688 5-(2-Gas-4, 5-difluoro-benzhydrylamino)-1 Η-pyrazole-3-carboxylic acid (4Η-0!:嗤琳3-yl)-bristamine, 5-(2- gas-4, 5-difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid (4Η-quinazolin-3-yl) - guanamine dihydrochloride, 5-(2- gas-4, 5-difluoro-phenylhydrazino)-1Η-° azole-3-carboxylic acid (7-fluoro-4-indole-quinazoline) Benz-3-yl)-nonylamine dihydrochloride, 5-(2- gas-4,5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylic acid (6-fluoro- 4Η-quinazolin-3-yl)-indolamine hydrochloride, 5-(2-chloro-4,5-difluoro-phenylhydrazinoyl)-111-pyrazole-3-carboxylic acid (2 -ethoxy-2-mercapto-1,4-dihydro-2-indole-quinazolin-3-yl)-nonylamine, 5-(2-chloro-4, 5-difluoro-benzoguanamine Base)-1Η-pyrazole-3-carboxylic acid (2-cyano) -pyridin-4-ylindenyl)-decylamine, 5-(2- gas-4,5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid [2-(Ν- Hydroxylamimimine fluorenyl)-pyridin-4-ylmethyl]-decylamine, 5-(2- gas-4, 5-difluoro-phenylhydrazino)-1Η-pyrazole-3- Carboxylic acid [2-(5-mercapto-4,5-diaza-[1,2,4] σ dioxin. sit-3-yl)-° than bit -4-mercapto]-guanamine, 4-{[5-(4, 5-Difluoro-2-methyl-phenylguanidino)-1Η-pyrazole-3-carbonyl]-indolyl-amino}-benzoate sodium salt, 5 - (4,5-difluoro-2-indolyl-benzoylamino)-1H-d ratio 0--3-reductive methyl-[4-(1Η-tetrazol-5-yl)- Phenyl]-nonylamine, 5-(2,4-dichloro-benzoinylamino)_lH-ntbo sitting_3_slow acid (〇比 bit-3_ylmercapto)-nonylamine, 5-(2 , 4-dichloro-5-fluoro-benzoguanidino)-1Η-pyrazole-3-carboxylic acid (pyridyl 156 318197 1322688 pyridine-3-ylindenyl)-nonylamine, 5-(2, 6- Dichloro-5-fluoro-pyridine-3-carbonylaminos--3-hypo-acid (pyridin-3-ylmethyl)-decylamine, 5-[(3- gas-benzo[1)]thiophene-2 -carbonyl)-amino]-11^^_3_ • carboxylic acid (pyridin-3-ylindenyl)-decylamine, 5-[(3- gas-thiophene-2-carbonyl)-amino]-111-pyridyl Azole _3_acid 0-pyridin-3-ylmethylguanamine, 5-phenylhydrazinoamino-1H-pyrazole-3-carboxylic acid (pyridin-3-ylmethyl)-r-decylamine, 5-phenylethylhydrazine Amino-1H-pyrazole-3-carboxylic acid (pyridin-3-ylmethyl)-decylamine, 5-(2-methyl-4, 5-difluoro-phenylhydrazino)-1Η- ° than 嗤-3-glycolic acid (p-pyrimidin-3-ylmethyl)-bristamine dihydrochloride, 5-(2-amino-4, 5-difluoro-benzamide)-111- °Bizozol-3-deoxy acid (pyridin-3-ylmethyl)-decylamine, φ 5-(4, 5-difluoro-2-methanesulfonylamino-benzamide-based ratio -3_ Carboxylic acid (pyridin-3-ylindenyl)-nonylamine, 5-(2-acetamido-4,5-difluoro-benzylidinium)-1Η-0 than sal-3-carboxylic acid (° Than -3-ylmethyl)-bristamine, 5-[(3,4,5-tris-thiophen-2-yl)-amino]-1Η-° than ol-3-oxo acid Bite-3-ylmercapto)-chatty amine' 5-(4,5-difluoro-2-indolyl-phenylhydrazino)1Η-σ than 嗤-3-buffer acid (2-cyano- Pyridin-4-ylmethyl)-decylamine, 5-(4,5-difluoro-2-indolyl-benzylidenylamino)-1Η-pyrazole-3-slow 318197 157 1322688 acid [2- (1Η-tetrazol-5-yl)-pyridylmethyl]-decylamine, and 111 than saliva-3,5-dicarboxylic acid 3- Benzylamine 5-[(2,4-dichloro-phenyl)-bristamine]. 56. Insulin resistance, diabetic neuropathy, diabetic nephropathy, diabetic retinopathy, cataract, hypercholesterolemia, hypertension, insulinism, hyperlipidemia, atherosclerosis, tissue ischemia A therapeutic or prophylactic agent for myocardial infarction, obesity or bacterial, fungal, parasitic or viral infection, comprising the pyrazole-based climbing compound according to any one of the aforementioned items 36 to 55 or a pharmaceutically acceptable salt thereof as an activity ingredient. 57. A medicament comprising a combination of a therapeutic or prophylactic agent according to the foregoing 56 item with another drug. Advantages of the Invention The pyrazole compound of the present invention has hepatic phosphatase inhibitory activity, has potent activity and has less adverse reactions and superior oral absorption and metabolic stability than conventional antidiabetic agents, and can provide extremely useful novel diabetes spring. A therapeutic or prophylactic pharmaceutical composition, and can be used as insulin resistance, diabetes, pathological neuropathy, diabetic nephropathy, diabetic retinopathy, cataract, hypercholesterolemia, hypertension, hyperinsulinemia, hyperlipidemia Useful therapeutic agents for atherosclerosis, tissue ischemia and myocardial infarction, therapeutic agents for chyme control and obesity, and therapeutic agents for infections such as bacterial, fungal, parasitic, or viral infections. [Embodiment] The η-pyrazole skeleton of the hydrazine compound of the present invention includes not only the following formula: 318197 158 1322688 Ο

It also includes the following isoforms:

Four goods η. Two =::: The above general formula (1)

Good 0

R 2 3 0 R1

R (η) The substituents and the various moieties used herein are defined as "halogen atoms" as fluorine, chlorine, or fluorene atoms. Fluorine or chlorine atoms are "匕-6 alkyl" which means linearity of 1 to 6 carbon atoms or Branched alkyl, for example, including methyl, ethyl, propyl, isopropyl, butyl, isobutyl, t-butyl, t-butyl, pentyl, isopentyl, 2-decyl butyl, Neopentyl, ethylidene, hexyl, isohexyl, 4-methylpentyl, 3-methylpentyl, 2-mercaptopentyl, diphenylpentyl, 3,3-dimercaptobutyl, 2, 2-dimethylbutyl, 1,didecylbutyl, 1,2-dimethylbutyl, 1,3-dimercapto 159 318197, 2'3-dimethylbutyl, ethyl Butyl and 2 ethyl butyl. Preferably, "C 4 alkyl" means a linear or branched alkyl group having 1 to 4 carbon atoms, and includes, for example, a methyl group, an ethyl group, a propyl group, Isopropyl, butyl, isobutyl, t-butyl and tert-butyl. Methyl is preferred. C26 cation means that it has 2 to 6 carbon atoms and has one or more double bonds as needed. Branched alkenyl group, and includes, for example, vinyl, propylene 2-propenyl, bebutenyl, 2-butenyl, 3-butenyl, 2-methyl-propylidene, 1-pentyl, 2-pentenyl, 3-pentenyl, 4 _Pentyl, 3-methyl-2-butenyl, hexenyl, 3-hexenyl, 2 4-hexadienyl and 5 hexenyl. As desired, containing 2 to 4 carbon atoms Branched C24 alkenyl is preferred, such as vinyl, propenyl, 2-propenyl and nonylbutenyl. It is more preferred to be an ethyl group and a propenyl group. "C2-6 alkynyl" means 2 to 6 a carbon atom and having one or more alkynyl groups as desired, and including, for example, an ethynyl group, a propynyl group, a lan-2-propynyl '1-butynyl group, a 2-butynyl group, 3_ Butynyl, pentynyl, 2-pentynyl, 3-pentynyl, 4-pentynyl, hexenyl, 2-hexopenynyl, 3-hexopenynyl, 4-hexyl Alkynyl and 5-hexynynyl. Preferred are C2_4 alkynyl groups having 2 to 4 carbon atoms as desired, such as ethynyl, 丨-propynyl, 2-propynyl, 1-butynyl And a 2-butyl group. "Ci-e stretching group" means an alkyl group having 1 to 6 carbon atoms as desired, and includes, for example, a methylene group and an ethyl group. a propyl group, a butyl group, a pentyl group and a hexyl group, and preferably a branched C!-4 alkyl group having 1 to 4 carbon atoms, such as a methylene group, an ethyl group, and a stretching group. Propyl and butyl

160 318197 (D 1322688 yl 0 halogen Cw alkyl group) means the above-mentioned ".substituent" substituted by one or more, preferably from 丨 to 6, particularly preferably from 1 to 3 of the above-mentioned "halogen atoms". Trifluoromethyl, tris-decyl, difluorodecyl, di-methyl, di-methyl, fluoromethyl, 2,2,2-trifluoroethyl, 2,2,2-trichloroethyl 2, dimethyl ethyl, 2-oxyethyl, 2-fluoroethyl, 2-iodoethyl, 3-chloropropyl, decyl hexyl hexyl hexyl and 2,2-dibromoethyl It is preferably a halogenated Cl-4 alkyl group having 1 to 4 carbon atoms.

C!-6 alkoxy" means an alkoxy group having 1 to 6 carbon atoms, wherein the alkyl moiety is a "Ci 6 alkyl group" as defined above, as defined above, and includes, for example, a methoxy group and an ethoxy group. Base, propoxy, isopropoxy, butoxy, isobutoxy, second butoxy, tert-butoxy, pentyloxy, isopentyloxy, 2-yylbutoxy, ethyl Propyloxy, 2-ethylpropoxy, neopentyloxy, hexyloxy, 4-methylpentyloxy, 3-methylpentyloxy, 2-methylpentyloxy, 3'3-di Methylbutoxy, 2,2-dimethylbutoxy, M-dimethylbutoxy, 1,2-dimethylbutoxy, l 3 -dimethylbutoxy and 2,3 _ dimethylbutoxy. Preferred are Cm alkoxy groups having 1 to 4 carbon atoms such as methoxy, ethoxy, propoxy, isopropoxy and butoxy groups. "Ci-6 alkoxy-substituted Cu alkyl group" or "Cl_s alkoxy c]_6 alkyl group" means a "Cl_e alkyl group" branched as described above, which is branched as described above. Oxy substituted, and includes, for example, methoxymethyl, ethoxymethyl, propoxymethyl, isopropoxymethyl, butoxymethyl, isobutoxymethyl, second butoxy Base group, third butoxymethyl group, L methoxyethyl group, 2-ethoxyethyl group, 2-propoxyethyl group, 2-isopropyl isopropoxide 318197 161 1322688 ethyl group, 2-butyl group Oxyethyl, 2-isobutoxyethyl, 2-(second butoxy)ethyl, 2-(t-butoxy)ethyl, 丨-methoxyethyl, ethoxy Ethyl, 1-propoxyethyl, 1-isopropoxyethyl, dibutoxyethyl, isobutoxyethyl, 1-(second butoxy)ethyl, 1_(third Butoxy)ethyl and 3-isopropoxypropyl. Preferred are alkoxy moiety and a C 4 alkoxy Ci_4 alkyl group having 1 to 4 carbon atoms in the alkyl moiety, such as an anthranyloxy group, an ethoxymethyl group, a 1-decyloxyethyl group, 2_ Alkoxyethyl and 2-butoxyethyl.

"Cm alkoxycarbonyl" means an alkoxy group optionally having 1 to 6 carbon atoms as defined above bonded to a carbonyl group, and includes, for example, methoxycarbonyl, ethoxycarbonyl, propoxycarbonyl, or the like. Propoxycarbonyl, butoxycarbonyl, isobutoxycarbonyl, second butoxycarbonyl, third butoxyx, pentyloxy, isopentyloxycarbonyl, 2-methylbutoxycarbonyl, neopentyloxycarbonyl, ethyl Propoxycarbonyl, hexyloxycarbonyl, 4-methylpentyloxycarbonyl, 3-methylpentyloxycarbonyl, 2-methylpentoxym-yl, benzylamyl(tetra)yl, 3 3 dimethyloxylocyl, 2 , 2-dimercaptooxycarbonyl, i, bisdimethylbutoxycarbonyl, 12-dimethylbutoxycarbonyl: 1,3-dimethylbutoxycarbonyl, 2,3-dimethylbutoxycarbonyl And 2-ethylbutoxycarbonyl. Preferred are (Cm alkoxy)carbonyl groups in which the alkyl moiety contains fluorene to 4 carbon atoms, such as methoxycarbonyl, ethoxycarbonyl, propoxycarbonyl and isopropoxy.

Ci-fi alkoxycarbonyloxy" means an optionally defined branch as defined above, ". 丨-6 alkoxycarbonyl" which is bonded to an oxygen atom and includes, for example, a methoxycarbonyloxy group, an ethoxy group. Alkoxy, propoxyoxy, propyloxyoxy, Toxysiloxy, isobutoxycarbonyl 1 318197 162 1322688 dibutoxycarbonyloxy, third Butoxycarbonyloxy, pentyloxycarbonyloxy, isopentyloxycarbonyloxy, 2-mercaptobutoxycarbonyloxy, neopentyloxyoxy, 1-ethylpropoxycarbonyloxy, Hexyloxycarbonyloxy, 4-methylpentyloxycarbonyloxy, 3-mercaptopentyloxycarbonyloxy, 2-methylpentyloxycarbonyloxy, b-methylpentyloxycarbonyloxy, 3,3-dimethyl Butoxycarbonyloxy, 2,2-dimethylbutoxycarbonyloxy, 1,1-dimercaptobutoxycarbonyloxy, L 2 dimethylbutoxycarbonyloxyl, 1,3- Methylbutoxymethyloxy, 2,3-dimethylbutoxycarbonyloxy or 2-ethylbutoxycarbonyloxy. Preferred is a (Cm alkoxy)carbonyloxy group having 1 to 4 carbon atoms in the oxime moiety of the oxime, such as a methoxycarbonyloxy group, an ethoxycarbonyloxy group, a propoxycarbonyloxy group, and a different Propoxycarbonyloxy and propoxycarbonyloxy. "Ci-e burned carbonyloxy" means a 6 alkyl group as defined above, which is bonded to a carbonyloxy group, and includes, for example, an ethoxylated group, a propyloxy group, a butoxy group, an isobutyl group. Alkoxy, pentyl, isoamyloxy, pentyloxy and hexyloxy. • "Ch alkylcarbonyloxy Cm alkyl" means "Ci-e alkyl" substituted by the aforementioned rCie alkylcarbonyloxy group, and preferably Ci-4 substituted by Cl; i alkylcarbonyloxy group alkyl. "Ch alkoxy which may be substituted by Cl_e alkoxycarbonyl" means an unsubstituted C1-6 alkoxy group or a Ci 6 alkoxy group substituted by a Cm alkoxycarbonyl group, and substituted by a Ch alkoxycarbonyl group Cl_e alkoxy represents re"alkoxy" substituted by "Cm alkoxycarbonyl" as defined above. Preferred are unsubstituted Ch alkoxy groups and Ci-alkoxy groups substituted by c,-4 alkoxycarbonyl groups. "Methylenedioxy" and "extended ethyldioxy" represent 318197 8 163 1322688 -0-CH2-0- and -〇-C2H4-〇-, respectively. "Wheat base" means a C2-7 aliphatic fluorenyl group or an aromatic aryl group which is branched as needed, wherein a saturated hydrocarbon group or an unsaturated hydrocarbon group is bonded to the carbonyl group. The aliphatic sulfhydryl group includes, for example, an ethyl fluorenyl group, a propyl fluorenyl group, a butyl sulfonyl group, an isobutyl fluorenyl group, an amyl aryl group, an isovaleryl group, a pentylene group, a hexyl group, an acryl group, a methyl propylene group, and a croton. Stuffed base. The aromatic fluorenyl group includes an arylcarbonyl group such as a phenylhydrazine group, an α-naphthyl anthracenyl group and a phenanthrenyl group, a dentate arylcarbonyl group such as a 2-bromobenzoinyl group and a 4-benzophenone group. An arylcarbonyl group in which Cm is alkylated, such as 2,4,6-trimercaptophenyl fluorenyl and 4-indolylbenzhydryl, and an alkoxylated arylcarbonyl group such as 4-anisyl, a nitrated arylcarbonyl group such as 4-nitrophenylhydrazino and 2-nitrobenzylidene, (V6 via alkoxycarbonylated arylcarbonyl such as 2-(methoxycarbonyl)benzylidene and An arylated aryl group such as a 4-phenyl benzoyl group. "C!-6 alkylamino group" means the following "mono-Cl-6 alkylamino group" or "two

Ch alkylamino group". It is preferably a Cl 4 alkylamine group having 1 to 4 carbon atoms. "Single Ci-ealkylamino" means an amine group substituted by Γ匕6-6" as defined above and includes, for example, methylamino, ethylamino, propylamino, isopropylamino. , butylamino, isobutylamino, t-butylamino, tert-butylamino, pentylamino, isoamylamino, 2-methylbutylamino, neopentylamine Base, 1-ethylpropylamino, hexylamino, isohexylamino, 4-decylpentylamino, 3-methylpentylamino, 2-methylpentylamino, 1-anthracene Pentylamino, 3,3-dimethylbutylamino, 2,2-dimethylbutylamino, M-dimethylbutylamino, 1,2-didecylbutylamine Base, 1,3-two 318197 1322688 methylbutylamino, 2,3-dimethylbutylamino and 2-ethylbutylamino. Preferred is a mono-Ci_4 deuteroamine group substituted with a Cl-4 group, such as a mercaptoamine group, an ethylamino group, a propylamino group, an isopropylamino group, a butylamino group, and an isobutylamine. base. 'DiCl·6 alkylamino group' means an amine group substituted by two identical or different "Ci-e alkyl groups" as defined above, and includes, for example, a dimethylamino group, a diethylamino group, N-ethyl-N-methylamino, dipropylamino, dibutylamino, dipentylamino and dihexylamino. Preferably, the two _Cl_4 alkylamino groups, such as dimethylamino and diethylamino groups, are substituted by two Cl 4 alkyl groups. "Mercaptoamine" means an amine group substituted by "mercapto" as defined above, and includes, for example, a lower carbon aliphatic mercaptoamine group having an optionally branched branch having 2 to 7 carbon atoms, such as an acetamino group. , propyl decylamino, butyl sulfhydryl, isobutyl decyl amide, amyl decyl amide, isoamyl ylamino, pentyl amide, hexyl amide, acryl yl, methyl Acrylhydrazino group and crotonylamino group, or aromatic mercaptoamine group such as phenylhydrazino group. "Ci-e alkoxycarbonylamino" means an amine group substituted by the rCi6 alkoxy group Ik group as defined above and includes, for example, an anthranylamino group, an ethoxylated amino group, a propoxycarbonylamine. And isopropoxycarbonylamino group. Preferred is a Ch alkoxycarbonylamino group such as a methoxycarbonylamino group, an ethoxycarbonylamino group and a propoxycarbonylamino group. The limited definition of "aminomethan" means _c〇NH2, and the broad definition means -C0NH2, "mono-Cm alkylaminocarbamyl", "di-Cl_6 alkylamine broth", "Di-arylaminomercapto" or rN_Ci_6 alkyl N-arylamino fluorenyl. 318197 165 1322688 "Single-Ch-alkylaminocarboxyalkyl" means an aminomethylmercapto group bonded to a 6-alkyl group as defined above, and includes, for example, methylaminocarbamimidyl, ethylaminomethylguanidinyl, Propylaminomethyl decyl, iso-diylaminomethyl decyl, butylaminomethyl decyl, isobutylaminomethyl decyl, second butylamino fluorenyl, • tert-butylamine Basementyl, pentylaminomethyl decyl, isoamylaminomethyl hydrazino, 2-methylbutyl fluorenyl, neopentylaminomethyl hydrazino, ethyl propyl propyl methionyl and hexylamine a mercapto group; preferably a monoalkylaminoalkyl group, wherein the group is an alkyl group having 1 to 4 carbon atoms, such as a methylamino fluorenyl group or an ethylaminomethyl fluorenyl group. , propylamino fluorenyl, isopropylaminomethyl decyl and butylaminomethyl fluorenyl. "Di-Ch alkylaminocarbamyl" means an aminomethylcarbenyl group bonded to two identical or different "Cm alkyl" groups as defined above, and includes, for example, dimethylamino fluorenyl, diethyl Aminomethyl sulfhydryl group, N-ethyl_N_decylamino fluorenyl group, dipropylaminocarbamyl group, dibutylaminomethyl fluorenyl group, dipentylamino fluorenyl group and two Hexylaminomethyl fluorenyl; and preferably di-Cw alkylamine fluorenyl fluorenyl wherein the alkyl group is an alkyl group having 1 to 4 carbon atoms, such as dimethylaminocarbamyl and diethyl Aminomethylmercapto group. "N-Cm alkyl-N-arylaminocarbamyl" means an aminomethyl group attached to the "aryl" and "Cl ealkyl" as defined above on its nitrogen atom, and includes, for example, N- Methylphenylaminocarbamyl, N-ethyl-N-phenylaminocarbamimidyl, N-phenyl-N-propylaminocarbamimidyl, N-isopropyl-N-phenyl Amino fluorenyl, N-butyl-N-phenylaminomethyl fluorenyl, N-pentyl-N-phenylamino fluorenyl, N-hexyl-N-phenylaminocarbamyl, N-methyl-N-naphthylamino fluorenyl, N-ethyl-N-naphthylaminomethyl fluorenyl, N-naphthyl-N-propyl 166 318197 8 !322688 Aminomethyl decyl, N-isopropyl-N-naphthylaminocarboxamyl, N-butyl-N-naphthylaminoindenyl, N-naphthyl-N-pentylaminoindenyl and N-hexyl- N-naphthylaminomethyl fluorenyl; and preferably N-Ch alkyl-N-phenylamino fluorenyl, wherein the alkyl group is an alkyl group having 1 to 4 carbon atoms and the aryl group thereof is Stupid, such as N-fluorenyl-N-phenylaminoindenyl and n-ethyl-N-phenylaminocarbamyl. "Ci-e alkylsulfonyl" means a sulfonyl group bonded to "Cl6 alkyl" as defined above, and includes, for example, fluorenylsulfonyl, ethylsulfonyl, propylsulfonyl, isopropyl. Sulfonyl, butylsulfonyl, isobutylsulfonyl, second butyl fluorenyl, tert-butyl fluorenyl, pentyl fluorenyl, isoamyl fluorenyl, 2-fluorenyl Butylsulfonyl, neopentylsulfonyl, i_ethylpropylsulfonyl, hexylsulfonyl, isohexylsulfonyl, 4-methylpentylsulfonyl, 3-decylpentyl Sulfonyl, 2-methylpentylsulfonyl, 1-methylpentylsulfonyl, 3,3-dimercaptobutylsulfonyl, 2,2-didecylbutylphosphino, 1, 1-dimercaptobutylsulfonyl, 1,2-dimethylbutylsulfonyl, iota, dimethylbutanylsulfonyl, 2,3-dimercaptobutylsulfonyl And 2-ethylbutylsulfonyl; and preferably a Ci-4 sulfonyl group wherein the alkyl moiety is an alkyl group having 1 to 4 carbon atoms, such as a fluorenylsulfonyl group or an ethyl sulfonate. Mercapto, propylsulfonyl, isopropylsulfonyl and butylsulfonyl. More preferably, it is a sulfhydryl group. "Ci-e aryl-based amine group" means an amine group which binds to "Ci-6 sulfonylsulfonyl" as defined above, and includes, for example, fluorenylsulfonylamino group, ethylsulfonylamino group, and propyl group. Alkylamino, isopropyl arylamino, butyl-readylamino, isobutylsulfonylamino, t-butylsulfonylamino, tert-butylsulfonyl Amine, pentylsulfonylamino, isopentylsulfonylamino, 167 318197 1322688 2-mercaptobutylsulfonylamino, neopentylsulfonylamino, ethylidene Amino, hexylamino, isohexyl arylamino, 4-mercaptosylsulfonylamino, 3-methylpentylsulfonylamino, 2-methylpentyl hydrazide Amino, 1-methylpentyl arylamino, 3, 3-dimerylbutyl decylamino, 2, 2-dimethylbutylsulfonylamino, ι, ΐ- Dimethylbutyl arylamino, 1,2-dimethylbutyl decylamino, 1,3-dimethylbutylsulfonylamino, 2,3-dimethylbutylsulfonate An amino group and a 2-ethylbutyl aryl amine group; and preferably a Cl-4 fluorenyl amine group, wherein the alkyl group is a An alkyl group of 1 to 4 carbon atoms such as methylsulfonylamino, ethylsulfonylamino, propylsulfonylamino, isopropylsulfonylamino and butylsulfonylamino . The C3-8 cycloalkyl group means a saturated cycloalkyl group having 3 to 8 carbon atoms and preferably 3 to 6 carbon atoms, or a Cw cycloalkenyl group having one or two double bonds in the ring. Examples of the "saturated CM cycloalkyl group" include a cyclopropyl group, a cyclobutyl group, a cyclopentyl group, a cyclohexyl group, a cycloheptyl group, and a cyclooctyl group. Further, "C3 8 cycloalkenyl group" means a cycloalkenyl group having 3 18 carbon atoms and preferably 5 to 7 carbon atoms and containing at least one and preferably one or two double bonds in the interior of the ring. Specific examples include a cyclopropenyl group, a cyclobutenyl group, a cyclopentyl group, a cyclohexyl hexanyl group, a 2,5-cyclohexanedoxinyl group and a cyclooctenyl group. C"cycloalkyl group L-channel" means a "Ci6 alkyl group" as defined above, and includes, for example, cyclopropylmethyl, propylpropylethyl, cyclodecylmethyl, as defined above. Cyclopentylethyl, cyclohexyl and cyclohexylethyl. Preferably, the alkyl group has a carbon group 318197 168 1322688 "C3-8 cycloalkyl CV4 alkyl group" such as cyclopropylmethyl, cyclopropylethyl, cyclopentylmethyl, % amyl B And cyclohexylmethyl. The "C3-8 cycloalkoxy group" means a "C38 cycloalkyl group" as defined above bonded to an oxygen atom, and includes, for example, a cyclopropoxy group, a cyclobutoxy group, a cyclopentyloxy group, a cyclohexyloxy group, a cycloheptyl group. Oxyl and cyclooctyloxy. Preferred is a C36 cycloalkoxy group wherein the cyclodextant group is a (tetra) group having 3 to 6 carbon atoms, such as a cyclopropoxy group, a cyclobutoxy group, a cyclopentyloxy group and a cyclohexyloxy group. "C3-8^ alkoxycarbonyloxy" means that "C38 cycloalkoxy" as defined above is bonded to a pure radical ' and includes, for example, cyclopropoxy (tetra)yl, cyclobutoxyoxy, cyclopentyloxy Keweiyl, cyclohexyloxy(tetra)yl, cycloheptyloxycarbooxy and cyclooctyloxycarbonyloxy. Preferred is a Cs 6 cycloalkoxycarbonyloxy group, wherein the cycloalkyl group is a cycloalkyl group having 3 to 6 carbon atoms such as a cyclopropoxy (tetra) group, a cycloτoxy (tetra) group, and a cyclosyl group. Cyclooxycarbonyloxy. "C3-8 cycloalkoxycarbonyloxy-6 alkyl" means "G1•alkyl group" substituted by the above-mentioned "Cy ring alkoxy (tetra) group", and (d) is a G36 ring oxyalkyloxy group. The cycloalkyl group is a cycloalkyl group having 3 to 6 carbon atoms, and a cycloalkoxycarbonyloxyalkyl group wherein the alkyl group is *alkyl group. "Aryl" means "smoke radical" having from 6 to one carbon atom and includes, for example, phenyl, decyl, base 1 and phenanthryl. The aryl group may be partially saturated, as the case may be. Examples of partially saturated aryl groups include dihydroindenyl and tetrahydronaphthyl. Preferred is Ce~aryl, more naphthyl and most preferably phenyl. It is preferable that the soil or the stupid base is the "Q" of the formula (I). 318197 169 1322688 "Aralkyl" may be a "Cl-6 alkyl" group as defined above which incorporates one or two aryl groups having 6 to 14 carbon atoms, such as benzyl, naphthylquinone, fluorenylmethyl, phenanthrene. Anthracenyl, fluorenylmethyl, diphenylfluorenyl, phenethyl, naphthylethyl, phenylpropyl, naphthylpropyl, phenylbutyl, naphthylbutyl, phenylpentyl, naphthylpentyl and benzohexyl; A preferred aryl group, wherein the aryl group is a phenyl group, and the alkyl group is a Cl-4 alkyl group such as a benzyl group, a naphthylquinone group, a diphenylfluorenyl group and a phenethyl group; more preferably a benzyl group or a phenethyl group And particularly preferred is benzyl. The "aryloxy group" is an "aryl group" as defined above which binds to an oxygen atom and includes, for example, a phenoxy group and a naphthyloxy group. Phenoxy is preferred. "Arylsulfonyl" means a sulfonyl group bonded to an "aryl" group as defined above, and includes, for example, a C6-14 arylsulfonyl group such as a phenylsulfonyl group, a sulfonylsulfonyl group, a naphthylsulfonyl group. , phenanthrylsulfonyl, fluorenylsulfonyl and fluorenylsulfonyl; preferably C6M. The arylsulfonyl group wherein the CeMO aryl group is bonded to a sulfonyl group; more preferably a phenylsulfonyl group or a naphthylsulfonyl group and most preferably a phenylsulfonyl group. The "arylsulfonyl group which may be substituted by a CH alkyl group" means φ "arylsulfonyl" as defined above, wherein the aryl group is one or more and preferably 1 to 3 "Cl" as defined above. The -6 alkyl group is preferably replaced by a "Cl-4 alkyl group", and includes, for example, a fluorene-based fluorene group. "Arylsulfonylamino" means an "arylsulfonyl" group as defined above bonded to an amine group, and includes, for example, a Ce-nonylsulfonylamino group such as a phenylsulfonylamino group, a sulfhydryl group Amidino, naphthylsulfonylamino, phenanthrylsulfonylamino, mercaptosulfonylamino and mercaptosulfonylamino; preferably Cm arylsulfonylamino, more preferably phenylsulfonyl Amino or naphthylsulfonylamino, and most preferably phenylsulfonylamino. 170 318197 1322688 A phenyl group which may be substituted by a halogen atom means one or more and: 1 to 3 of the same or different self-atoms selected from the group consisting of a fluorine atom, a gas atom, a bromine atom and an iodine atom. Replace the stupid base. — "A phenyl group which may be substituted by a halogen (^6 alkyl group) means a phenyl group substituted by a plurality of "_Cl_6 alkyl groups" having the same or different meanings as defined above. "Heterocyclyl" means a carbon atom other than a carbon atom. a saturated ring, a partially unsaturated ring or an aromatic ring selected from the group consisting of a shield atom, a nitrogen atom and a sulfur atom as a ring-forming atom, = two and preferably 5 Up to 7 rings form an atom, and the ring may be a monosaturated early per-heterocyclic group "representing a saturated or partially saturated heterocyclic group" and includes, for example, anthracene, tetrahydro Df-butyl, tetrazolium (4) base silk, in-cyclopentyl base, 13 "oxathiolanyl", ° 恶 ° sit bite + sit silk " Chen bite base, base, tetrahydrosulfuric acid (tetra), di(tetra),琳琳基, thiophene ketone, pyrrolidinyl, 2-ketopiperidinyl, 4-ketopiperidinyl and 2,6-= base groups. Preferably saturated 5 or 6 members A cyclic group such as a pyridyl group, a piperidinyl group or a morpholinyl group. "Saturated 5- or 6-membered monocyclic heterocyclic group" means a "residue and a monocyclic heterocyclic group" having the definition of 5. base The heterozygous % is especially a 5- or 6-membered monocyclic heterocyclic ring such as tetrachloropyran, U-diguana, tetracycline, == member--, one has been built, (four) dnehU one or two mountains , Niang Bite, Niang, and Shout. Hetero 318197 171 The ring group may have a double bond. "A 5-membered heterocyclic ring having 1 to 4 heteroatoms selected from the group consisting of sulfur, oxygen and nitrogen atoms. "Based" means, for example, a 5-membered heteroaryl group such as a bitter base, thienyl, pyrrolyl, pyrazolyl, imidazolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, oxadiazolyl, triazole Examples of a saturated or partially saturated monocyclic heterocyclic group include a tetrazirfuran-2-yl group, a tetrahydrofuran-3-yl group, an imidazolidinium group, an imidazolidinyl group, and an imidazole group. Pyridin-4-yl, pyrrolidine-fluorenyl, pyrrolidine-2-yl, pyrrolidinyl, 1,3-oxazolidin-3-yl, isothiazolidinyl, 13-thiazolyl-3-yl, 1 2_ pyrazolidine-2-yl and 1,2-pyrazolidine__byl. , "Saturated 5 or 6 membered monocyclic heterocyclic ring having at least one nitrogen atom" does not have at least one nitrogen atom And may have) to 3 selected from , ^, And (iv) heteroatoms and five of the group consisting of milk atom or a 6-membered monocyclic heteroaryl nucleus ^ group. Examples of the heterocyclic ring constituting the 5-membered heterocyclic group include, for example, abbreviations: 1 sitting <#钱,1和^线; 6-membered heterocyclic group j--T θ ^ ^ Chenjing, morpholine and evil Second ploughing. Partially saturated heteronuclei can have double bonds. Examples of the "(10) aryl group" include a thiol group, a thiol group, a pyrimidine group, a morphine group, a hydrazone, a ruthenium group, a pyrrolyl group, a pyrazolyl group, an imidazolyl group. , U,4-diazolyl, tetrazolyl, .. oxazol, read @ 嚜%, fluoromethyl, oxazolyl, oxazolyl, isothiazolyl and aryl are preferred. I (four) or 6 shells can be combined with the adjacent nitrogen atom ugly and heterocyclic ring "for example, 5 to 7 V? into saturated soil" _ used "sufficient shell to 7 shell %" nitrogen-containing heterocyclic ring in addition to carbon atoms Further, 318197 172, a group consisting of at least one nitrogen atom and further containing a scuba, sulfur and nitrogen atom is selected from the group consisting of, for example, w,::= to form an atomic morpholine. Morpholine and sulphur form a condensation with the present condensate _ benzene ring to form a condensed ring" means a cleavable group, an isotinoline, 2,3-dihydrobenzoin: ", '; ...a spray base. The π-open (tetra)-based group, the present-opening sulfonyl group, and the hydrazine "heteroaryl group" means a ring having the same or different hetero atoms selected from the group consisting of oxygen, IS, and I: in addition to a carbon atom. The two 3 have 3 to 14, preferably 5 to 7, more preferably 5 to 6 % of a heteroaryl group forming an atom, or a condensed group thereof. The heteroaromatic group may be substituted with a '' or a poly- or a thioketo group. Such keto- or thioketo-substituted heteroaryl groups also include heterocyclic groups in which a keto group or a thioke group is present due to I-coupling tautomerism in a heteroaryl group substituted with a thiol group or a thiol group. . Examples of heteroaromatic groups include, but are not limited to, beta ratio thiol, thaphthyl, miso base, "tough base, trisyl" "biphthyl, fluorenyl, isoindolyl, tetrazole Base, thiol group, porphinyl, isoindolyl, oxime, carbazolyl, iso-salt, squara, cylinyl, iso-indolyl, decyl, benzo- succinyl, Benzoindolyl, sulphate-based; 〇 〇 sit, mouth bow 哄 哄 base, 呔 well base ° 卩 well base, di- 11-mercapto, iso-decyl, fluorenyl, oxadiazolyl , thiazolyl, thiadiazolyl, furazanyl, benzofurazyl, benzothienyl, benzotriazolyl, benzothiazolyl, benzoxazolyl, quinazolinyl, quinoxalinyl , naphthoquinone, dihydroquinolyl, furoacridinyl, π-pyrrolopyrimidine 173 318197 8 base and fluorenyl. The 5-membered or 6-membered heteroaryl group means that, in addition to a carbon atom, there are from 4 to 4 hetero atoms selected from the group consisting of an oxygen atom, a nitrogen atom and a sulfur atom as a ring-forming atom, and a heteroaromatic group having 5 to 6 ring-forming atoms, or a condensed group thereof. Examples include fluorenyl, fluranyl, thienyl, imidazolyl, pyrazolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, 12,4-triazolyl, 12,3-triazole , tetrazolyl, 1' 3' 4-oxadiazolyl, 1,2,4-oxadiazolyl, anthracene, 3, 4-thiadiazolyl, 1 ' 2, 4 thiazolyl, fur Mercapto, pyridyl, pyrimidinyl, hydrazine, pyridyl, 1,3,5-trimethyl, imidazolinyl, pyrazolinyl, oxazolinyl (2-oxazoline, 3- Oxazolinyl, 4-oxazolyl), isoxazolinyl, thiazoline f, isothiazolinyl, piperidyl, 2-ketopiperidyl and 2-keto-2, 5-di Hydrofuranyl. Preferred are pyrrolyl, furyl, thienyl, imidazolyl, pyrazolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, pyridyl and 2-keto-2,5-dihydrofuran. base. A "5-membered or 6-membered heteroaryl group which may be substituted by a keto group or a thioketone group" means that the 5-membered or 6-membered heteroaryl group as defined above may be selected from one or more selected from the group consisting of _ group (=〇) or sulfur. The substituents of the keto group (=s) are the same or differently substituted. Such 5- or 6-membered heteroaryl groups substituted with a keto group or a sulfur-based group also include a keto group or sulfur in which a keto-enol tautomerization in a heteroaryl group substituted with a hydroxy group or a thiol group is present. A 5- or 6-membered heterocyclic group of a keto group. "5-membered or 6-membered heteroaryl group which may be substituted by a carboxyl group or a Cm alkoxycarbonyl group" means that a "5-membered or 6-membered heteroaryl group" as defined above may have one or more carboxy or rCl_e alkoxycarbonyl groups as defined above. Replace it. 318197 174 丄美1 = mono-% soil or condensed ring heteroaryl" means the heteroaromatic arsenic early (four), heteroaromatic or its associated with one or more aromatic carbon rings such as benzene rings County Qing Xu condensation group. Fangxiang (4) is a heteroaromatic group or a heteroaromatic group condensed with a benzene ring" means "monopolyheteroaryl" such as porphinyl "fujiji"biloyl, imidinyl, iso(tetra)yl, (iv) saliva a base group, a base group, a base group, a money base, a soil and a mouth cavity, or a heteroaryl group condensed with a benzene ring such as a benzocylation group, an isobenzofuranyl group, a benzo[b]thienyl group, Sulfhydryl, isodecyl, lH, t°, succinimidazolyl, benzoxazolyl, benzothiazolyl, 1H-benzodiazolyl, quinolinyl, isoquinolinyl, Porphyrin group, quinazolinyl group, quinoxaline group and hydrazine base. "=1-6 alkyl group substituted by a monocyclic heteroaromatic group or a heteroaryl group condensed with a benzene ring" means substituted by a "monocyclic heteroaryl group or a heteroaryl group condensed with a fluorene" as defined above rCie alkyl". Preferably, "C"-6 alkyl group substituted by "monocyclic heteroaromatic group" is preferred. The condensed heterocyclic group includes an anthracenyl group (e.g., 4-fluorenyl, 7-fluorenyl), isodecyl, anthracene, 3_dihydro-indole, 3-diketoisodecyl, a benzofuranyl group (e.g., 4-benzofuranyl, 7-benzofuranyl), carbazolyl, hetero- and a-family, benzophenantyl (e.g., 4-benzoindole, gamma benzo) Thiophenanyl), stupid and oxazolyl (eg 4-benzoxazolyl, 7-benzoxazolyl), benzimidazolyl (eg 4-benzimidazolyl, 7-benzimidazolyl), a benzothiazolyl group (for example, 4-phenylthiazolyl, 7-phenylthiazolyl), hydrazine, quinolyl, isoquinolyl, 1,2-dihydro-2-ketoquinolinyl, Quinazolinyl, quinoxalinyl, porphyrinyl, hydrazine, quinoxalyl, fluorenyl, hydrazine 318197 175 1322688 pyridine, porphyrin, isoindolyl, 5, 6, 7, 8-tetrahydroquinolinyl, 1,2,3,4-tetrahydroquinolinyl, 2-keto-anthracene, 2,3,4-tetrahydroquinolyl, benzo[1,3]2° Oxacyclopentyl, 3,4-methylenedioxy phthalate, 4, ethyldioxypyrimidyl, pentene, spray, and isopropanyl. The term "substituted with a plurality of substituents" means substituted by one or more, preferably 1 to 6, and particularly preferably to 3 identical or different substituents. Further, even if the number of substituents is not specified, it means "substitutable by one or more substituents". The term "identical or different" means that all of the substituents are the same, all substituents are different from each other, or two of the two or more substituents are the same. Preferred groups in the above formula (1) are described later, but the compounds of the present invention are not limited to these groups. The aryl group in the coating Q is preferably a CeiD aryl group, more preferably a phenyl group or a phenyl group and most preferably a phenyl group. The "heteroaromatic group" in 裱Q is preferably "5 or 6 membered hetero-aromatics containing i to 4 hetero atoms selected from the group consisting of = oxygen and nitrogen atoms", and more preferably It is a thiophene or a bite base. % Q is preferably a stupid or a terpene base, and particularly preferably a phenyl group. R is preferably a halogen atom, a tooth atom, a C ^ is preferably a hydrogen atom h alkyl group or a C 4 alkoxy group; more preferably, it is a hydrogen atom, a fluorine atom or a gas atom; Good for fluorine atoms. Preferably, it is composed of an m atom, a ci-4 alkyl group, a Ci-4 alkoxy group or an azide group; more preferably ν is an atom or a gas atom, and more preferably a fluorine atom. Preferably, it is a functional atom, a meridine, a Cl_6 alkyl group, a tooth 318197 176 oxo and a nitrogen group, an amine group, a mercaptoamine group or a Ci-e alkyl group; more preferably an atom or a Cl group Particularly preferred is a fluorine atom, a gas atom or a methyl group; more preferably a gas atom or a sulfhydryl group. The preferred substituent of the ring Q (r1, r2 & R3) is a hydrogen atom at the position of Rl5, an atom or a chlorine atom, more preferably a fluorine atom or a hydrogen atom, a fluorine atom or a gas atom at the position of the ruler 24, Preferably, it is a fluorine atom, and a gas atom or a methyl group at the fluorene position, and more preferably a gas atom.

Substituent R1, ! ^ and R3 substituted ring oxime are preferably as follows.

Cl, M· % is better as shown below 2-gas-4, 5-

F

Preferably, R4 is selected from the group consisting of ruthenium to ruthenium, and the substituent of the group A is substituted by a Ci-alkyl group: 2. The group of the group is selected from the group consisting of, for example, [A, group] A' I hydroxy; A 2. C丨-4 alkoxy such as methoxy ethoxylated ethoxypropyl, isopropoxy 318197 177 1322688 and butoxy; especially preferred for methoxy, ethoxy, propoxy And isopropoxy group, A 3. -N(R )(R41 ), wherein r41 and r41. are preferably the same or different from each other and represent a hydrogen atom or a Cl-4 alkyl group, or f and R are Further examples of the formation of a saturated 5- or 6-membered monocyclic ring heterocyclic ring N(R41)(R4r) by an adjacent nitrogen atom include an amine group, a methylamino group, an ethylamino group, a dimethylamino group, and a second Ethylamino, N-piperidinyl, N-morpholinyl, N-pyrrolidinyl and piperidinyl; more preferably an amine group, a methylamino group, an ethylamino group, a dimethylamino group , diethylamino, N-piperidinyl, N-morpholinyl, N-pyrrolidinyl and piperidinyl, A 4.phenyl or naphthyl (preferably phenyl), A 5. 5- or 6-membered heteroaryl (preferably „pyridyl), A'6·-C0-N(R41)(R41·) such as _C0NH2'singed single Si 4 alkylamino group Mercapto, di-Ch alkylaminocarbazinyl, N_Ci*alkyl N-arylaminocarbamimidyl, dimethylaminocarbamyl, ethylaminomethylmercapto, morpholinyl a carbonyl group, a pyrrolidinylcarbonyl group and a piperidinylcarbonyl group; more preferably a methylaminocarbyl group, an ethylaminocarbyl group, a dimethylaminomethyl fluorenyl group and a diethylaminomethyl fluorenyl group, φ A' 7. Carboxyl and A'8. Ch alkoxycarbonyl such as methoxycarbonyl, ethoxycarbonyl, propoxycarbonyl, isopropoxycarbonyl, butoxycarbonyl, isobutoxycarbonyl; preferably methoxycarbonyl, ethoxy Carbonyl, propoxycarbonyl and isopropoxycarbonyl, 3 · C 2 -4 alkenyl such as ethenyl, propenyl, 2-propenyl, iota-butyl, 2-butadienyl, 3-butenyl and 2- a methyl-1-propenyl group; preferably a vinyl group, a 1-propyl group or a 2-propenyl group, and a 4 C 4-4 group such as an ethyl group, a 1-propyl block group, a 2-propynyl group and Butynyl' is preferably ethynyl, propynyl and 2-propynyl; 178 318197

(C 丄 322688 5 . CM cycloalkyl such as cyclopropyl, cyclobutyl, cyclopentyl and cyclohexyl; 6 · Cw cycloalkyl C 4 alkyl, preferably cyclopropyl decyl, cyclopropylethyl , cyclobutylhydrazino, cyclobutylethyl, cyclopentylmethyl, cyclopentylethyl, cyclohexylmethyl and cyclohexylethyl; ?-aryl such as phenyl and naphthyl, preferably stupid Preferably, R5 is a group selected from the group consisting of Γ to 8': C. C alkyl or an alkyl group substituted with a substituent selected from the group B below, preferably a Cl-6 group; _ [B , group] B' 1. fluorenyl, Β 2. Cw alkoxy such as methoxy, ethoxy, propoxy, isopropoxy, butoxy and isobutoxy, B 3. -N ( R ) ( R 51 ) wherein |^ and γ are preferably the same or different from each other and represent a hydrogen atom or a Ch alkyl group, or R 51 and R 5 ! ' may form a saturated heterocyclic ring together with an adjacent nitrogen atom, examples of which include Amino, mercaptoamine, ethylamine ruthenyl, dimethylamino, diethylamino, N-ethyl-N-methylamino, dipropylamino, N-piperidinyl, N-morpholinyl, N-pyrrolidinyl and piperidin; preferably amino, methylamino, ethylamino Dimethylamino and diethylamino and B'4. -C0-N(R51)(R5")' wherein r51 and r51 are as defined above. Examples thereof include methylaminomethyl decyl and ethylamine. Methyl mercapto, dimethylaminomethyl hydrazino, monoethylaminomethyl hydrazino, morpholinylcarbonyl, pyrrolidinylcarbonyl and piperidinyl; preferably methylaminomethyl, Ethylaminoglycolyl, dimethylaminomethylindenyl and diethylaminomethylindenyl, 318197 179 丄厶uoo 班. (: 3-8 ring, such as cyclopropyl, cyclobutyl, Cyclodecyl, cyclohexyl, hexylheptyl octyl, preferably C3 6 cycloalkyl selected from the group consisting of cyclopropyl, cyclobutyl, cyclodecyl and cyclohexyl, in: The % alkyl group may be substituted by a hydroxyl group, a carboxyl group or a c14 alkoxycarbonyl group (preferably a carbaryl group, an ethoxy group, a propoxy group or an isopropoxy group), or a pyridine ring. Condensation to form the following groups;

• c, -6 alkyl group substituted by C3-8 decyl group, preferably a C alkyl group substituted by a c3 6 cycloalkyl group, particularly preferably a Ci 2 alkyl group substituted by a cycloalkyl group, and specific examples thereof include a ring Propylmethyl, cyclopropylethyl, cyclobutylhydrazino, cyclobutylethyl, cyclopentylmethyl, cyclopentylethyl, cyclohexylmethyl and cyclohexylethyl, wherein the C3-8 The cycloalkyl group of the cycloalkyl group may be substituted by a hydroxyl group, a carboxyl group or a Ci-6 alkoxycarbonyl group; preferably a Ch alkoxycarbonyl group such as an anthraceneoxycarbonyl group, an ethoxycarbonyl group or a propoxy group. Carbonyl and isopropoxycarbonyl; 4'-saturated 5- or 6-membered monocyclic heterocyclic group which may be substituted by one or more substituents selected from the group C' below, wherein the saturated 5 member or 6 Preferred examples of the monocyclic heterocyclic group include, for example, pyrrolidinyl, tetrahydrofuranyl, tetrahydrothiophenyl, imidazolidinyl, pyrazolyl, 1,3-dioxolyl, 1,3-caxa Thiazinyl, oxazolidinyl, thiazolidinyl, piperidinyl, piperidinyl, tetrahydro-nitrithyl' tetrahydrosulfide brigade, dioxin 0 sylylene, sulfonyl, thiophenanyl, 2 -Cu base ratio ° each bite base, 2-_ base brigade bite 4__基基基基和2,6-diketone-based bite group; preferably biting base, ketone base and morphine; best 180 318197 1322688 showing 6-member saturated heterocyclic group ·

[C, group] C'l. C, -6 alkyl group, preferably. —4 alkyl such as methyl, ethyl, propyl isopropyl and butyl, i-butyl fluorenyl and benzhydryl; preferably C 2. bromo, such as ethyl, propyl, butyl, butyl , propyl ketone and butyl base, ethyl sulfonate, propyl is preferably methyl thiol C 3. C 〗 - e yl base yellow wine base such as methyl sulfhydryl, sulfonyl, isopropyl Alkylsulfonyl and butylsulfonyl; and ethylsulfonyl, C' 4. Carboxyl, C'5. Ch alkoxycarbonyl, preferably Cl_4 alkoxycarbonyl, such as methoxycarbonyl, B Oxycarbonyl, propoxycarbonyl, isopropoxycarbonyl, butoxycarbonylcarbonyl and isobutoxycarbonyl and C'6. _CO-(Alk)n-COOR52, wherein π is preferably a hydrogen atom or a ci4 alkane a group, Aik is a Ci-4 stretching group and η is 〇 or an integer of 1 to 2, 5'. aryl, or substituted by one or more and preferably 丨 to 3 selected from the group D' below a substituted aryl group, wherein the aryl group is, for example, a strepyl or naphthyl group and is preferably a phenyl group; [D' group] D' 1. a trans group, D'2. Ch alkoxy group, preferably ch-alkane Oxyl groups such as decyloxy, ethoxy, 181 318197 8 1322688 propoxy, isopropoxy , butoxy and isobutoxy, D' 3. cyano, D' 4. Cm alkyl ' is preferably c, -4 alkyl, such as methyl, ethyl, propyl, isopropyl, butyl a base, an isobutyl group and a second butyl group, wherein the Cl 6 alkyl group may be selected from a hydroxyl group, a carboxyl group and a Ch alkoxycarbonyl group (for example, a methoxycarbonyl group, an ethenyl group, a propoxy group, and a different group). Substituted by one or more substituents of the group consisting of propoxyl groups, D'5. -N(R53)(R53') where! And r53' are preferably a hydrogen atom, a tetraalkyl® or a C-4-alkylsulfonyl group, and the specific examples include an amine group, a mercaptoamine group, an ethylamino group, a dimethylamino group, and a diethyl group. Amino, methylsulfonylamino and ethylsulfonylamino, D'6.-C0-N(R53)(R53')' wherein r53&r53, preferably a hydrogen atom, an alkyl group or a Ch The alkylsulfonyl group, a specific example thereof includes an aminomethyl fluorenyl group, a dimethylaminomethyl fluorenyl group, and a diethylaminomethyl fluorenyl group, preferably a dimethylaminomethyl fluorenyl group or a diethylamino group. Mercapto, dimethylaminocarbamyl, diethylaminoglutamyl and fluorenylsulfonylaminomethyl, .D'7·-COOR54, preferably a hydrogen atom or an alkane Base (eg, methyl, ethyl, propyl, isopropyl, and butyl), Cl_4 nonyloxyalkyl (eg, fluorenyl, oxymethyl, ethyloxymethyl, and propyloxy) Methyl) or C3-6% alkoxycarbonyloxy Cl_4 alkyl (such as cyclohexyloxycarbonyloxymethyl and cyclohexoxyoxyethyl), preferably a gas atom or a C14 alkyl group ,

D>8. -CCNHCOH))=NR^*tR55r^i44^^^Ci^A Sulfhydryl group such as methylsulfonyl, D'9. Saturated 5- or 6-membered monocyclic heterocyclic group Tons of (tetra)yl, tetrachloro 318197 182 1322688 fluorenyl, tetrahydrothiophenyl, imidazolidinyl, pyrazolyl, fluorene, 3 dioxacyclopentanyl, 1,3-dithiad-d-yl, oxazolidine , thiazolidinyl, piperidinyl, piperidinyl, tetrahydropyranyl, tetrahydrothiopyranyl, dioxoyl, morpholinyl, thiomorpholinyl, 2-ketopyrrolidinyl, 2-ketopiperidinyl, 4-ketopipidine and 2,6-dionepiperidinyl, preferably a 5- or 6-membered heterocyclic group having at least one nitrogen atom, such as pyrrolidine Base, piperidinyl and morpholinyl; more than the lower 6-saturated saturated heterocyclic group:

And D'10. 5- or 6-membered monocyclic heteroaryl groups which may be substituted by keto or thioketo groups, such as pyrrolyl, furyl, thienyl, imidazolyl, pyrazolyl, oxazolyl, iso 11 Orythracene, oxime, isodecyl, 1,2,4-trimethyl, 1,2,3-triazolyl, tetrazolyl, 1,3,4-oxadiazolyl, 1 , 2, 4-oxadiazolyl, 1,3,4-dioxadiyl, 1,2,4-diyldiyl, sulfhydryl, octagonal, thiol, thiol, °哄基,1,3,5-三哄基,咪吐琳基' »比峻基基, °恶唾琳基(2-°嗤琳基, 3-°恶β坐淋基,4-嗯°坐琳基), iso-tr-oxazolidinyl, thiazolidinyl, isothiazolinyl, piperidyl, 2-ketopiperazinyl and 2-branched 1-yl- 2,5-dihydro-fluoropropanyl ; preferably. Biloki, thiol base, singular base '°m β sitting group, η ratio ° sitting group, β oxo group, isodecyl group, 坐 "sitylene, isothiazolyl, pyridyl and 2-keto a -2,5-dihydrofuranyl group; more preferably a 5-membered heterocyclic group having at least two nitrogen atoms: 183 318197 8

More preferably, the following 5-membered heterocyclic group:

Wherein D, 1 to D, D, 4, D, 6' D, 7 and D' are preferred as the preferred substituents in the substituent of R5, 10 selected from the group consisting of 10, Substituted phenyl is also b. 5 shells of a 6-membered monocyclic heteroaryl or a condensed ring with a benzene ring which may be substituted by one or more groups selected from the group consisting of a carboxyl group and a Ch alkoxycarbonyl group. a substituent, wherein the Gl_6&oxy group is preferably a G 4 -oxy.carbonyl group such as a fluorenyloxycarbonyl group, an ethoxycarbonyl group, a propoxycarbonyl group, an isopropoxycarbonyl group, and a butoxycarbonyl group; and the heteroaromatic group is, for example, Pyrrolyl 'furanyl, thienyl, imidazolyl, pyrazolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, 1,2,4-triazolyl, 1,2,3-triazole Base, tetrazolyl, 1,3, 4-oxadiyl, 1,2,4-oxadiazolyl, 1,3,4-thiadiazolyl, 1,2, 4-thiadithio ,furazanyl, pyridyl, pyrimidinyl, fluorenyl, pyridyl, anthracene, 3,5-trimethyl, imidazolinyl, pyrazolinyl, oxazolinyl (2-oxazolinyl, 3 -. Bad sputum base, 4-° sullen base), different.恶 t*坐琳基, sold 嗤琳基, 嗟 嗟 184 318 197197 1322688 scare base, pedicyl, 2 - cyanopyranyl and 2-keto-2,5-diazepine It is lalotyl, fluorenyl, thienyl, imidazolyl, pyrazolyl. Anthracene, isoxazolyl, thiazolyl, isothiazolyl, pyridyl and 2-keto-2,5-dihydrofuranyl; preferably p-Roleyl, furyl, thienyl, imidyl, Pyrazolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, i 2 4-triazolyl, pyridyl, pyrimidinyl, indolyl, pyridyl, thiazolinyl, isothiazolinyl And piperidyl;

The excellent 5- or 6-member heteroaryl group is shown below:

7'. OH aralkyl, such as Ci 4 alkane substituted with an aromatic hydrocarbon group, such as benzyl, dimethylmethyl, benzyl fluorenyl, fluorenylmethyl, decylmethyl, diphenyl fluorenyl, stupid Base, naphthylethyl, phenylpropyl, naphthylpropyl, phenylbutyl, and decyl butyl, preferably fluorenyl, benzylmethyl 'diphenyl fluorenyl' and phenethyl, more preferably benzyl Or a phenethyl group, wherein the alkyl moiety of the c?i4 aralkyl group may be unsubstituted or substituted with one or two substituents selected from the group consisting of E, preferably the alkyl moiety is Substituted, or the aryl moiety of the C7 i4 aralkyl group may be substituted with one or more, and preferably 1 to 3, substituents selected from the group F' below, [E' group] E' 1. Anthracene-4 alkyl which may be substituted with a hydroxy group, such as methyl, ethyl, propyl, isopropyl, butyl, isobutyl, hydroxymethyl and hydroxyethyl, 318197 185 1322688 E' 2. Cyano, E' 3. Carboxyl, E'4. Cm alkoxycarbonyl is preferably a (Cl_4 alkoxy)carbonyl group such as a methoxy group, an ethoxy group, a propoxy group, an isopropoxy group Butoxyxyl group, isobutoxy a base, a second butoxycarbonyl group and a third butoxycarbonyl group and an E' 5. phenyl group, [Γ group] F' 1 · Ch alkyl group, preferably an alkyl group such as a methyl group, an ethyl group, a propyl group, or a different group a propyl group, a butyl group, an isobutyl group and a second butyl group, F'2. a tooth atom such as a fluorine atom, a gas atom, a bromine atom and an iodine atom, preferably a fluorine atom or a gas atom, F' 3 · cyano group, F'4, a C, -6 alkoxy group, a Ci_6 alkoxy group substituted by a carboxyl group or a Ch alkoxy group substituted with a fluorenyl 6 alkoxycarbonyl group, wherein the Cl_e alkoxy group is preferably Is Ci 4 • alkoxy such as methoxy, ethoxy, propoxy, isopropoxy, butoxy and isobutoxy, and Cl6 substituted with Ci-6 alkoxycarbonyl The alkoxy group of the C!-6 alkoxycarbonyl group is preferably a Cl_4 alkoxycarbonyl group such as an anthraceneoxycarbonyl group, an ethoxycarbonyl group, a propoxycarbonyl group, an isopropoxycarbonyl group and a butoxycarbonyl group, and a F 6·halogenated Cu alkyl group. For example, trifluoromethyl, fluoromethyl and 2,2,2-trifluoroethyl' are preferably from a Cl-4 group such as trifluoromethyl, carboxyl, F 8 · Cl-6 alkoxycarbonyl, Preferred is C,-4 alkoxycarbonyl such as methoxycarbonyl, ethoxylated, propoxy , isopropoxy, butyloxy, butyl 318197 186 1322688 oxycarbonyl and second butoxycarbonyl, wherein f?56a and R56a are identical to each other or phase F'9. -CO-N (R56a (R56a' represents a hydrogen atom, a 5-membered or 6-membered monocyclic heterocyclic group having at least one nitrogen atom, such as N-piperidinyl, N-morpholinyl, pyrrolidinyl and N - a piperylene group, or a Ch alkyl group which may be substituted with one or more substituents selected from the group consisting of the following groups, preferably a saturated heterocyclic group of which is a 6-membered saturated heterocyclic group:

or

S and the Cm alkyl group are preferably a Ch alkyl group such as a mercapto group, an ethyl group, a propyl group, an isopropyl group, a butyl group, an isobutyl group and a second butyl group, [Γ group] Γ 1. an amine group, f 2 · "Single-pH-based amine group" such as mercaptoamine, ethylamine, propylamino, isopropylamino, butylamino, isobutylamino, and butylamino , tert-butylamino, pentylamino, isoamylamino, 2-mercaptobutylamino, neopentylamino, ethylpropylamino, hexylamino, isohexylamino, 4- Meryl pentylamino, 3-mercapto amylamino, 2-decylpentylamino, 1-decylpentylamino, 3,3-dimethylbutylamino, 2, 2- Dimercaptobutylamino, 1,1-dimethylbutylamino, 1,2-didecylbutylamino, 1,3-didecylbutylamino, 2,3-dimethyl Butylamino group and 2-ethylbutylamino group; preferably mono-indol-4-alkylamino group, ί 3. — Ci-6-based amine group such as dinonylamino group, diethyl Amine 187 318197 1322688, N-ethyl-N-methylamino, dipropylamino, dibutylamino, dipentylamino and dihexylamino; preferably di-C,-4 Alkylamine , Γ 4. carboxy, Γ5 · Ch alkoxycarbonyl group, preferably. -* Alkoxycarbonyl such as decyloxycarbonyl, ethoxycarbonyl, propoxycarbonyl, isopropoxycarbonyl, butoxycarbonyl and isobutoxycarbonyl. f' 6. a meridine, and f'7. a 5- or 6-membered monocyclic heterocyclic group having at least one nitrogen atom saturated such as N-piperidinyl, N-morpholinyl, N-pyrrolidinyl And N-piperidinyl, F 10 · -N(R56b)(R56b'), wherein R56b&R56b· are identical or different from each other and represent a hydrogen atom, a C alkyl group which may be substituted with an imine group, an aralkyl group It may be substituted with one or more substituents selected from the group consisting of an imine group and an _ atom, an arylsulfonyl group which may be substituted with a Ci ealkyl group, an alkylsulfonyl group, an anthracene a base, an amine fluorenyl group, a mono-Ch alkylaminocarbamyl group or a di-Ci6 alkylamino fluorenyl group; the Cl_e alkyl group is preferably a hydrazine "alkyl group such as methyl, ethyl, propyl, iso a propyl group, a butyl group, an isobutyl group, a second butyl group, and a third butyl group, which may be the same or different from one or more selected from the group consisting of an imine group and a ruthenium atom. a substituent substituted, for example, (imino) (halogenated phenyl)methyl; an arylsulfonyl group which may be substituted with a Ci 6 alkyl group, for example, a sulfonyl sulfonyl group; and a Ci β alkylamino group Mercapto or di-C! 6 alkylaminocarbamidine The Cm alkyl group is preferably Ci 4 alkyl, F, 11. -N=CR57(-N(R58)(R58,, 318197 188 wherein R57 is preferably free of & ithia i5i -3⁄4 4 w horse atom or Cl-4 alkyl, R58 and P58, and represents a gas atom... group, and R is a group such as 12·5 or 6 members | Lumo's group: Heteroaryl group is preferably represented by the following

N and "its: an oxy group bonded to two adjacent carbon atoms constituting a C7·14 aralkyl group such as a benzyl group or a native ring, and one or more selected from a C--6 alkyl group substituted with the same or a different substituent of a 5-membered or 6-membered heteroaryl group and a group consisting of a condensed 5-membered or 6-membered heteroaromatic group of benzene, wherein the 5 member or The 6-membered heteroaryl group is, for example, pyrrolyl, furyl, thienyl, imidazolyl, pyrazolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, indole, 2,4-triazolyl, 1, 2, 3_ oxazolyl, tetrazolyl, 1,3,4-oxadiazolyl, 1,2,4-oxadiazolyl, 1,3,4-thiadiazolyl, 1,2, 4-thiadiazolyl, furazinyl, pyridyl, pyrimidinyl, fluorenyl, pyridinyl, 1,3,5-tridecyl, imidazolinyl, pyrazolinyl, oxazolinyl (2 -oxazolinyl, 3-oxazolinyl, 4-oxazolinyl), oxazolidine, 嗟σ sityl, iso-indenyl, α-chenyl, 2-keto Front base and 2-_yl-2,5-dihydrofuranyl group; preferably *» than fluorenyl, anthracene, porphinyl, _β, and σ , 11 αα 坐基, iso 恶 坐 坐 sit, 隹α siting base, 嗟 嗟 ° sit base, ° ratio bite base and 2-_ base-2,5-dihydro 吱 基 base ' which should have 189 318197 The condensed 5- or 6-membered heteroaryl group is, for example, a benzofuranyl group, an isobenzofuranyl group, a benzo[b]thienyl group, a fluorenyl group, an isodecyl group, a 1H-carbazolyl group, a benzo group. Imidazolyl, benzoxazolyl 'benzothiazolyl, 1H-benzotriazolyl, quinolyl, #quinolinyl, porphyrinyl, toxazoline & quinoxaline and morphine More preferably, the Cm alkyl moiety is a C 4 alkyl group such as a methyl group, an ethyl group and a propyl group; and the heteroaromatic group is a heterocyclic group as shown below:

Such heteroaromatic groups are particularly preferred but not limited ("radical, 4 4 and trisal, δ heteroaryl or condensed heteroaryl may be selected through one or more and preferably 1 f3 selected from Substituted by the following G' group of substituents: [G, group]

Cl 6 alkyl group may be substituted with one or more substituents selected from the group consisting of G, 190 197197 1322688, preferably Ch alkyl; [g, group] g' 1. A tooth atom such as a fluorine atom or a gas atom And preferably a gas atom, '',, ', g' 2. an amine group, g'3. a mono--6-alkylamino group, preferably a mono-Ci4 alkylamino group, such as a methylamino group And an ethylamino group and a propylamino group, g 4. The di-Ch-alkylamino group is preferably a di-Cl 4 alkylamino group such as a dimethylamino group and a diethylamino group, "g'5· Alkoxycarbonylamino group, such as methoxycarbonylamino group, ethoxy (tetra)amino group, propoxysilylamino group and isopropoxy (tetra)amino group, and preferably (Ci-4 alkoxy)carbonyl group An amine group, and an S' 6. hydroxyimino group, G'2. a halogen atom such as a fluorine atom or a chlorine atom, and preferably a gas atom, and a ruthenium G 3 Cl-6 methoxy group which may be substituted by a halogen atom, preferably For example, a Cl_4 alkoxy group substituted with one or a fluorine atom or a gas atom, a G, 4. aryloxy group, preferably a siloxy group, an oxy group G 5 · a chaotic group, G' 6. -N (R59a)(R59a), where R and R are the same or different from each other and represent hydrogen Child. Ge. 4 alkane :: and! ^ can form a saturated ring with a neighboring nitrogen atom, which is preferably a m (tetra) group, a member of the group, a member, or a thiol group! 318197 191 1322688 and the saturated heterocyclic group may be selected from one or more selected from the group consisting of a hydroxyl group, an amine group, and a single

Substituents of the group consisting of a Cl-4 alkylamino group and a diCh alkylamino group are substituted,

Gf7. -CO-N(R59b)(R59b), wherein 5 and 6 s monocyclic indenocyclic groups which are the same or different from each other and which represent a hydrogen atom and which are saturated with an adjacent nitrogen atom, Such as pyrrolidinyl, imidazolidinyl"bisazolidine, piperidinyl, piperidinyl, morpholinyl and thiomorpholinyl, or Ch alkyl which may be substituted by the heterocyclic group, G'8. The base 'for example is preferably a phenyl group, and a G1 5 member or a 6 fluorene monocyclic (10) aryl group which is substituted with a sulfhydryl group or a thiol group, for example, a pyridyl group, a fluorenyl group, an imidazolyl group, a pyrimidinyl group, a pyrazolyl group, or a third group. Azolyl, pyridinyl, tetrazolyl, furyl, thienyl, isoxazole =,; oxazolyl, oxazolyl, isothiazolyl, pyrrolyl 'quinolinyl, isoquino, decamyl, benzene (tetra) Money, materialy, 28 bases ^ 娜 基, 哄 哄, β 荅哄 、, 哄 哄, 啊 ... ... 吟 ... ... ... 吟 吟 吟 吟 吟 吟 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 : : : : : : : : : : Benzene thiophene, benzotrienyl, benzo (tetra), benzoxanth, hydrazone, aryl, yl, dihydrogen, benzo-pyry Base, material and (four) base and ten (four) base, preferably the following heteroaromatic Base: 318197 192 J322688

MR5 together with adjacent nitrogen atoms form a saturated 5- or 6-membered monocyclic heterocyclic ring, wherein the "saturated heterocyclic" moiety has a double bond and can be condensed with a benzene ring to form a condensed ring, such as a noisy ring. A ring group such as a sulfhydryl group is prepared by condensing a base with a bite base, a thiophenanyl group, a morphinyl group, and a thiomorpholinyl group; or a condensation of a saturated heterocyclic group with a benzene ring. The 4H quinazolinyl group is preferably a group represented by the following formula:

Or a saturated heterocyclic group may be selected from one or more selected from the group consisting of a halogen atom, a Ci 4 alkyl group,

Substituents of the group consisting of Cl_4 alkoxy groups, buffer groups and Cl-4 house oxygen groups are substituted. Preferred specific examples of the compound (I) of the present invention are illustrated in the following examples. Tegapyrazole compounds include, but are not limited to, the following. 5 (2 - gas-4,5_ - machine - this brewylamino) _ 1 Η 0 to 0 sitting -3- slow acid 318197 193 1322688 (pyridin-3-ylindenyl)-nonylamine, 5-(2- Gas-4, 5-difluoro-phenylhydrazinoamino)-1Η-°biazole-3-carboxylic acid (pyridin-3-ylindenyl)-decylamine dihydrochloride, . 5-(2- Chloro-4, 5-difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid* (pyridin-3-ylindenyl)-decylamine hydrochloride, 5-(2-gas- 4, 5-Difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid (4-methyl-oxazol-5-ylmethyl)-decylamine, 5-(2-chloro- 4,5-difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid ginseng (4-mercapto-oxazol-5-ylmethyl)-decylamine, 5-(2-chloro -4,5-difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid (4-methyl-oxazol-5-ylmethyl)-nonylamine p-toluenesulfonate, 5-(2-Gas-4, 5-difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid (4-mercapto-oxazol-5-ylmethyl)-decylamine L -( + ) tartrate, 5-(2-chloro-4, 5-difluoro-phenylhydrazino)-1Η-α-pyrazole-3-carboxylic acid (2,4-dimercapto-oxazole -5-ylmethyl)-nonylamine p-toluenesulfonate, φ 5-(2- gas-4, 5-difluoro-phenylhydrazinoyl)-1Η-pyrazole-3-carboxylic acid (2,4-dimercapto-oxazol-5-ylmethyl)-decylamine, ' 5-(2-chloro-4, 5-difluoro-phenylhydrazino)-1Η-pyrazole- 3-carboxylic acid (2,4-dimercapto-pyridin-3-ylmethyl)-decylamine, 5-(2-chloro-4,5-difluoro-benzhydrylamino)-1Η-pyridyl Oxazol-3-carboxylic acid diethyl decylamine, 5-(2- gas-4, 5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylic acid ethyl-(pyridine-4 -hydrazinyl)-nonylamine, 5-(2-chloro-4,5-difluoro-phenylhydrazinoamino)-1 fluorene-carbazole-3-carboxylic acid 194 318197 1322688 (2-decyloxy- Ethyl)-mercapto-nonylamine, 5-(2-gas-4, 5-difluoro-phenylhydrazino)-1Η-°biazole-3-carboxylic acid ethyl-(2-methoxy -ethyl)-guanamine, '5-(2-chloro-4,5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylic acid '2-fluoro-benzylamine, 5-(2-chloro-4,5-difluoro-benzylidenylamino)-1Η-pyrazole-3-carboxylic acid 3-fluoro-benzylamine, 5-(2-chloro-4, 5- Difluoro-benzoguanidino)-1Η-indazole-3-carboxylic acid® 2-dimercaptoamino-benzylamine, 5-(2-gas-4, 5-difluoro-phenylhydrazine Amino-pyridyl-3-carboxylic acid (4-ethoxycarbonyl-cyclohexyl)-propyl-decylamine, 5-(2-chloro-4, 5-difluoro-benzoguanamine Base)-1Η-pyrazole- 3-carboxylic acid (6-decyloxy-D-pyridin-3-ylmethyl)-decylamine, 5-(2-chloro-4, 5-difluoro-phenylhydrazino)-1Η-pyridyl Oxazole-3-carboxylic acid 2,3-dimethoxy-benzylamine, φ 5-(2- gas-4, 5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylate Acid 2, 4-dimethoxy-benzylamine, * 5-(2- gas-4, 5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylic acid 2, 6- Dimethoxy-benzylamine, 5-(2-Gas-4, 5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylic acid 3, 5-dimethoxy-benzyl Indoleamine, 5-(2-chloro-4, 5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylic acid 3,4-dimethoxy-benzylamine, 5-( 2- gas-4,5-difluoro-phenylhydrazinoamino)-1Η-°biazole-3-carboxylic acid 195 318197 1322688 2,3-dioxane-nodal amine, 5-(2-chloro- 4,5-difluoro-benzhydrylamino)-1Η-carbazole-3-carboxylic acid 2.4-difluoro-membered amine' • 5-(2-chloro-4, 5-difluoro-benzamide Mercaptoamine)-1Η-pyrazole-3-carboxylic acid• 2,5-difluoro-tuberamine, 5-(2-gas-4, 5-difluoro-benzhydrylamino)-1Η -pyrazole-3-carboxylic acid 2,6-difluoro-tuberamine' 5-(2-gas-4,5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid • 3, 4-difluoro-benzylamine , 5-(2-chloro-4,5-difluoro-benzoindolyl)-1Η-pyrazole-3-carboxylic acid 3.5-difluoro-tuberamine ' 5-(2-gas-4, 5-difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid (2-isopropoxy-pyridin-3-ylindenyl)-decylamine, 5-(2-chloro-4 , 5-difluoro-benzhydrylamino)-1Η-°biazole-3-carboxylic acid (2-phenoxy-acridin-3-ylindenyl)-decylamine, φ 5-(2- Chloro-4, 5-difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid (3,5-difluoropyridin-2-ylindenyl)-nonylamine, ' 5-( 2-Chloro-4, 5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid 2-trifluorodecyl-benzylamine, 5-(2-gas-4, 5- Difluoro-phenylhydrazinoamino)-1Η-η-pyrazole-3-carboxylic acid 3-trifluoromethyl-tuberamine 5-(2-chloro-4, 5-difluoro-benzoinyl) Amino)-1Η-pyrazole-3-carboxylic acid 4-trifluoromethyl-benzylamine, 5-(2-chloro-4,5-difluoro-phenylhydrazino)-1Η-pyrazole 3-carboxylic acid 196 318197 8 1322688 4-tert-butyl-benzylamine, 5-(2-chloro-4, 5-difluoro-phenylhydrazino)-1Η-pyrazole_3_carboxylate Acid (6-isopropoxy-pyridin-3-ylindenyl)-decylamine, • 5-(2-Gas-4,5-difluoro-benzhydrylamino)-1Η-pyrazole-3 -carboxylic acid • [2-( 2, 2, 2-trifluoro-ethoxy)-indoletriazyl-3-ylmethyl]-bristamine, 5-(2-chloro-4, 5-difluoro-benzhydrylamino)- 1-Η-pyrazole-3-carboxylic acid 4-(2-dimethylamino-ethylaminopurinyl)-benzylamine, 5-(2-chloro-4-, 5-difluoro-phenylhydrazine The amino group is more than 0. _3-Resorcinol 4-ethyl-benzylamine, 5-(2-chloro-4, 5-difluoro-benzylidenylamino)-1Η-pyrazole_3_ 4-isopropyl-benzylamine, 5-(2- gas-4, 5-difluoro-phenylhydrazino)-1H-pyrazole-3-carboxylic acid 2_gas_6_fluorine - an amine amine '5-(2- gas-4, 5-difluoro-phenylhydrazino)-lH-pyrazole-3-carboxylic acid (6-ethoxy-pyridine-3-ylmethyl) - indoleamine dihydrochloride, I 5-(2-chloro-4,5-difluoro-benzylidenylamino)-lH-pyrazole-3-carboxylic acid (sit-4-ylindenyl) _ guanamine, ' 5-(2-chloro-4, 5-difluoro-phenylhydrazino)-iH-pyrazole-3-carboxylic acid [6-(2, 2, 2-trifluoro-B Oxy)-° ratio -3--3-methylglycol]-bristamine dihydrochloride, 5-(2-chloro-4, 5-difluoro-phenylhydrazino)-lH-pyrazole-3 a buffered acid 2,6-dimethyl-benzylamine, 5-(2-chloro-4,5-difluoro-anthracenylamino)-ih-pyrazole-3-decanoic acid [2-( Pyridin-3-yl)thiazol-4-ylindenyl]- Amine dihydrochloride, 318,197

197 1322688 5_(2-Fluoro-4,5-difluoro-benzofuranylamino)- lH-η ratio 〇3 - decanoic acid (1H-benzimidazol-2-ylmethyl)-decylamine Dihydrochloride, [4-({ [5-(2- gas-4, 5-difluoro-phenylhydrazino)-pyran-3-yl]amino}-mercapto)-benzamide Ethylamino]- decyl acetate, 3-[4-({ [5-(2-gas-4, 5-difluoro-phenylhydrazino)]iH_pyraki]amino}_ ))-Benzene arylamino]-propionic acid 甲g, 5-(2-chloro-4,5-difluoro-benzoquinoneamino)-ΐΗ-β ratio (2-mercapto-thiazol-4-ylmethyl)-guanamine dihydrochloride, 5-(2_a-4,5-difluoro-benzoinylamino)-ΐΗ-πϋβ sitting--3 - oxic acid (3, 5-dimercapto-isoindolyl-4-ylindenyl)-nonylamine, 5-(2- gas-4, 5-difluoro-phenylhydrazino)-ιη -pyrazole-3-carboxylic acid 4-(2-indole-(2-acetoxyethyl)-amino-ethylaminocarbamimidylamine, 5-(2-gas-4, 5 -difluoro-benzhydrylamino)-ιη-pyrazole-3-carboxylic acid 4_(2-hydroxy-ethylaminomethyl)-benzylamine, 5-(2-gas-4, 5-difluoro-benzhydrylamino)-ιη-pyrazole-3-carboxylic acid 4-{2-[(2-acetoxyethyl)-(2-hydroxyethyl)-amine ]-ethylaminomercapto}-benzylamine, 5-(2-gas-4, 5-difluoro-benzylidenylamino)-ih-pyrazole-3-carboxylic acid (1-A) -1H-benzimidazol-2-ylmethyl)-indolylamine hydrochloride, 5-(2- gas-4,5-difluoro-adenylamino)-111-pyrazole-3- Carboxylic acid (indol-2-ylindenyl)-bristamine dihydrochloride, 5-(2-chloro-4,5-difluoro-abdoximidyl)-ih-pyrazole-3-carboxylate Acid (benzopyranoquinone-2-ylindenyl)-bristamine dihydrochloride, 198 318197 1322688 5-(2-gas-4, 5-difluoro-benzhydrylamino)-1Η-« Bis-zolyl-3-carboxylic acid (2,5-dimethyl-thiazol-4-ylindenyl)-nonylamine dihydrochloride, 5-(2-chloro-4,5-difluoro-benzoinyl) Amino)-1 Η-carbazole-3-carboxylic acid [2_(Merline _4_yl)-supplement β _4_ylmethyl]- with amine dihydrochloride, 5-(2-chloro-4 , 5-difluoro-phenylhydrazinoamino)-1Η-indazole-3-carboxylic acid (1,3,5-trimethyl-111-pyrazol-4-ylmethyl)-decylamine, 5 -(2-Ga-4, 5-difluoro-benzylidenylamino)-1Η-η-pyrazole-3-carboxylic acid (2-Ga-6-methyl-pyridin-3-ylmethyl)- Indoleamine dihydrochloride, 5-(2-chloro-4,5-difluoro-benzoindolyl)-1Η-pyrazole-3-carboxylic acid (2-didecylamino-thiazole-4 - Foundation - indoleamine dihydrochloride, 5-(2-chloro-4, 5-difluoro-benzylidenylamino)-1Η-η-pyrazole-3-carboxylic acid (1-methyl-1Η-pyrrole) -2-ylmethyl)-decylamine, 5-(2- gas-4, 5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid (3,4-dimethoxy -pyridin-2-ylindenyl)-decylamine dihydrochloride, 5-(2- gas-4,5-difluoro-phenylhydrazinoamino)-1 -pyrazol-3-carboxylic acid ( 5-t-butyl-thiazol-2-ylindenyl)-nonylamine dihydrochloride, 5-(2-chloro-4,5-difluoro-benzylidenylamino)-1H-d-pyrazole 3-carboxylic acid (5-methyl-2-phenyl-2H-[1,2,3]triazol-4-ylindenyl)-decylamine, 5-(2- gas-4, 5-di Fluoro-benzoguanidino)-1Η-pyrazole-3-carboxylic acid [4-(t-butoxycarbonyl-amino)-indolyl-2-ylindenyl]-nonylamine, 5- (2-Chloro-4, 5-difluoro-benzylidenylamino)-1Η-pyrazole-3-carboxylic acid [4-indolyl-2-(morpholin-4-yl)-thiazole-5- 5-mercaptoamine dihydrochloride, 5-(2- gas-4, 5-difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid (pyridin-3-ylindole) ))-nonylamine 3/2 hydrochloride salt hemihydrate, 199 318197 1322688 5-(2-chloro-4,5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid 2 -amino-benzylamine 5-(2-chloro-4,5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid 2-methoxy-benzylamine, 5-(2-chloro-4, 5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid 3-decyloxy-benzylamine, 5-(2-chloro-4, 5-difluoro-benzylidene Amino)-1Η-pyrazole-3-carboxylic acid 4-decyloxy-benzylamine, 5-(2-chloro-4,5-difluoro-benzoinyl)-1Η-pyrazole- 3-carboxylic acid 4-mercapto-benzylamine, 5-(2- gas-4, 5-difluoro-phenylhydrazinoamino)-1H-pyrazole-3-carboxylic acid 4-fluoro-benzyl hydrazine Amine, 5-(2-chloro-4, 5-difluoro-phenylhydrazinyl)-1Η-pyrazole-3-carboxylic acid 4-chloro-benzylamine, 5-(2- gas-4, 5-difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid 4-ethoxycarbonyl-benzylamine, 5-(2-chloro-4, 5-difluoro-benzoinyl Amino)-1Η-«biazole-3-carboxylic acid 4-carboxy-benzylamine, 5-(2-gas-4,5-difluoro-crackanylamino)-1Η-pyrazole-3 - Dibenzylguanidinium carboxylate, 5-(2-chloro-4,5-difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid (cyano-phenyl-methyl)- Indoleamine, 5-(2-chloro-4, 5-difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid cyclohexylmethyl-decylamine, 200 318197 ^S) 1322688 "----what? "-Difluoro-benzoylamino-amino-pyrazole-carboxylic acid (2-trans-ethyl-ethyl)-phenyl-bristamine, 5-(2-gas-4, 5-fluoro) -benzimidylamino)_ιη_π than 嗤-3-teric acid ▲, cyclohexyl-methyl-decylamine, 5-(2-gas-4, 5-difluoro-benzhydrylamino)_1Η_ Pyrazole_3_carboxylic acid cyclohexyl decylamine, 5-(2-chloro-4, 5-difluoro-benzhydrylaminopyridinyl-pyrazole-3-carboxylic acid cyclohexyl-ethyl-decylamine , ^ 5 —(2_Chloro-4,5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid allyl-cyclohexyl-decylamine, 5-(2-gas- 4,5-difluoro-benzhydrylamino)_111_pyrazole_3_carboxylic acid cyclohexyl-(pyridin-2-ylindenyl)-decylamine, 5-(2-gas-4, 5- Difluoro-benzhydrylamino)_ih-pyrazole-3-carboxylic acid fluorenyl-(1-methyl-bottom-4-yl)-decylamine, 5-(2-gas-4, 5-di Fluorine-benzoylamino) — ιη-η ratio. Benzene-o-acid 0 [(3,4-]-indolyl-oxyphenyl)-indenyl]-bristamine hydrochloride, 5-(2-chloro-4, 5-difluoro-benzhydrazide Benzyl)-ιη-pyrazole-3-carboxylic acid benzyl-butyl-decylamine, • 5-(2-chloro-4,5-difluoro-benzhydrylamino)-ιη-pyrazole 3-carboxylic acid benzyl-(4-carbyl-butyl)-chiral amine hydrochloride, 5-(2- gas-4,5-difluoro-benzhydrylamino)-indole-. ratio. Oxy-3-oxobutyl-ethyl-decylamine, 5-(2-chloro-4,5-difluoro-benzoylamino)-indole-n-p--3-carboxylic acid cyclohexyl- Propyl-guanamine, 201 318197 1322688 5-(2-chloro-4,5-difluoro-anthracenylamino)-1 Η-pyrazole-3-carboxylic acid butyl-cyclohexyl-decylamine, 5-(2-chloro-4,5-difluoro-o-carboxylamido)-1Η-pyrazole-3-carboxylic acid cyclohexyl-(2-methoxy-ethyl)-decylamine, 5- (2-Chloro-4, 5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid cyclohexyl-(0-pyridin-3-ylindenyl)-decylamine, 5-( 2-Chloro-4, 5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid [2-morphin-4-yl]-phenyl]-bristamine, 5-(2 -Chloro-4,5-difluorobenzoylamino)-1Η_ο比〇-3 - Trehalic acid dibutylamine, 5-(2-chloro-4, 5-difluoro-benzamide Amino-pyridyl-3-carboxylic acid-(2-decyloxy-ethyl)-bristamine, 5-(2-chloro-4,5-difluoro-benzoinylamino )-1Η-β ratio ° -3- _ acid (2-decyloxy-ethyl) propyl-bristamine, 5-(2-chloro-4, 5-difluoro-benzofuranamine ))-1Η-β ratio 0 -3- oxo acid butyl-(tetrahydro-α-flavor-4-yl)-nitramine, 5-(2-chloro-4, 5-difluoro-benzamide Amine -1Η-pyrazole-3-carboxylic acid (2-methoxyethyl)-(tetraqi-π-bottom sigma-4-yl)-nitramine, 5-(2-chloro-4, 5-di Fluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid cyclopentyl-(2-methoxy-ethyl)-decylamine, 5-(2-chloro-4, 5-difluoro -phenylhydrazinylamino)-lH-pyrazole-3-carboxylic acid cyclohexyl-(3-methoxy-propyl)-decylamine, 5-(2-chloro-4,5-disorder-benzene甲 胺 胺 - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - -benzimidylamino)-1 Η-pyrazole-3-carboxylic acid cyclohexyl-(2-isopropoxy-ethyl)-decylamine, • 5_(2-gas-4, 5-difluoro -benzimidylamino)-1Η-pyrazole-3-carboxylic acid. Cyclohexyl~(2-propoxy-ethyl)-decylamine, 5-(2- gas-4, 5-difluoro- Benzoylamino)-1Η-pyrazole-3-carboxylic acid (Buethyl-propyl)-(2-methoxy-ethyl)-decylamine, 5-(2-gas-4, 5-di Fluoro-benzoguanidino)-1Η-pyrazole-3-carboxylic acid butyl second butyl group - 底 bottom-4-yl)-bristamine, ® 5_(2_gas-4, 5 -difluoro-benzoguanidino)-1Η-pyrazole-3-carboxylic acid butyl-(tetrahydro-thiopyran-4-yl)- Amine, 5-(2-chloro-4, 5-difluoro-phenylhydrazino)-1Η-0 than sal-3-carboxylic acid (2-decyloxy-ethyl)-decylamine, 5- (2-Ga-4, 5-difluoro-phenylhydrazino)-1-indole-pyrazole-3-carboxylic acid butyl-(pyridin-3-ylindenyl)-decylamine, 5-(2- Chloro-4, 5-difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid $benzyl-(2-methoxy-ethyl)-decylamine, 5-(2-chloro -4,5-difluoro-phenylhydrazinoamino)-1 Η-pyrazole-3-carboxylic acid butyl-〇 咬-4-yl)-bristamine, • 5-(2-gas-4, 5-difluoro-phenylhydrazinoamino)-lH-pyrazole-3-carboxylic acid. (1-ethylhydrazine base -4-yl)-butyl-decylamine, 5-(2-chloro-4 , 5-difluoro-phenylhydrazinoamino)-lH-pyrazole-3-carboxylic acid butyl _(1-methyl continuation base _4_yl)-nitramine, 5-(2-chloro -4,5-difluoro-phenylhydrazinoamino)-1-indole-pyrazole-3-carboxylic acid butyl-(1-ethoxyoxalyl-piperidin-4-yl)-decylamine, 203 318197 8 1322688 5-(2-Gas-4, 5-difluoro-benzylidenylamino)-1Η-η-pyrazole-3-carboxylic acid butyl-U-acid oxalyl-piperidin-4-yl - indoleamine, 5-(2-chloro-4, 5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid butyl-(1,1-dimercapto-hexanitrogen -1 λ 6-sulfur ** ratio ° _4-yl)-bristamine, 5-(2-chloro-4,5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylic acid butyl-(1-keto-hexahydro -1 λ4-thiopyran-4-yl)-nonylamine, 5-(2-chloro-4,5-difluoro-phenylhydrazino)-1Η-«biazole-3-carboxylic acid (6 -decyloxy-D-pyridin-3-ylmethyl)-propyl-decylamine, 5-(2-chloro-4,5-difluoro-phenylhydrazino)-1Η-pyrazole-3 -Carboxylic propyl-indoleridin-3-ylmethyl)-decylamine, 5-(2-chloro-4,5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylate Acid 4-diethylaminomercapto-benzylguanamine, 5-(2-chloro-4,5-difluoro-benzoinylamino)-1Η-pyrazole-3-carboxylic acid 3-II Ethylaminomethylmercapto-benzylguanamine, 5-(2-chloro-4,5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid 4-ethylamino hydrazine Mercapto-benzylamine, 5-(2-chloro-4, 5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylic acid 3-ethylaminopurinyl-benzylhydrazine Amine, 5-(2-chloro-4, 5-difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid 4-aminomercapto-benzylamine, 5-(2- Gas-4, 5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid (1-acidic acid-based base-4-ylpropyl-bristamine, 5-( 2-chloro-4, 5-di -phenylhydrazinylamino)-p-pyrazole-3-carboxylic acid (1-carboxyethenyl-piperidin-4-yl)-propyl-decylamine, 204 318197 1322688 5-(2-gas- 4, 5-Difluoro-phenylhydrazinoamino)-1 Η-pyrazole-3-carboxylic acid [1-(2-carboxypropenyl)-piperidin-4-yl]-propyl-decylamine , 5-(2-Gas-4, 5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylic acid cyclopropyl-(6-methoxy-pyridin-3-ylfluorenyl) - indoleamine, 5-(2- gas-4, 5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylic acid cyclobutyl-(6-decyloxypyridin-3 -ylmethyl)-decylamine, 5-(2-gas-4, 5-difluoro-benzylidenylamino)-1Η-pyrazole-3-carboxylic acid cyclopropylmethyl-(6-oxime Oxy-acridin-3-ylmethyl)-decylamine, 5-(2- gas-4, 5-difluoro-phenylhydrazinoamino)-1 fluorene-indazole-3-carboxylic acid (6- Dimercaptoamino-pyridin-3-ylindenyl)-decylamine, 5-(2-chloro-4,5-difluoro-benzylidenylamino)-1indole-pyrazole-3-carboxylic acid ( 6-Dimercaptoamino-pyridin-3-ylmethyl)-propyl-decylamine, 5-(2-gas-4, 5-difluoro-phenylhydrazinoyl)-1Η-°bazole -3-carboxylic acid benzyl-(2-carboxy-ethyl)-decylamine, 5-(2-chloro-4, 5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylate Acid festival -(2-ethoxyxo-ethylchiral, 5-(2-chloro-4,5-difluoro-benzhydrylamino)-1 fluorene-carbazole-3-carboxylic acid (6-chloro group) -pyridin-3-ylindenyl)-propyl-decylamine, 5-(2-gas-4,5-difluoro-phenylglycosylamino)_1Η-α is 0 -3- oxo acid 2 6_Dichlorobenzylamine ' 5-(2-chloro-4, 5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylic acid (3,5-di-pyridine--4 -hydrazinyl)-nonylamine, 5-(2- gas-4, 5-difluoro-benzhydrylamino)-1-indole-pyrazole-3-carboxylic acid (3,5-dichloro-pyridine-4 -ylmercapto)-propyl-nonylamine, 205 318197 8 1322688 5-(2-chloro-4,5-difluoro-phenylhydrazinoamino)-1H-pyrazole-3-carboxylic acid [6- (1Η-pyrazol-1-yl)-pyridin-3-ylmethyl]-nonylamine dihydrochloride, 5-(2-gas-4, 5-difluoro-phenylhydrazino)-1Η -pyrazole-3-carboxylic acid [6-(4-hydroxy-piperidin-1-yl)-pyridin-3-ylindenyl]-nonylamine dihydrochloride, 5-(2-chloro-4, 5 -difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid (2-pyridin-2-yl-ethyl)-decylamine, 5-(2- gas-4, 5-difluoro -phenylphenylamino)-1Η-pyrazole-3-carboxylic acid (2-pyridin-3-yl-ethyl)-decylamine, 5-(2- gas-4, 5-difluoro-phenylhydrazine Mercaptoamine)-1Η-pyrazole-3- Acid (2-pyridin-4-yl-ethyl)-decylamine, 5-(2-chloro-4, 5-difluoro-benzylidenylamino)-1Η-pyrazole-3-carboxylic acid (4 -[1,2,3]thiadiazol-4-yl-benzyl)-decylamine, 5-(2- gas-4,5-difluoro-phenylhydrazino)-1Η-pyrazole- 3-carboxylic acid (5-fluorenyl-pyroxy-2-yl-indenyl)-nonylamine, 5-(2-chloro-4,5-difluoro-benzoguanidino)-1Η-pyrazole 3-carboxylic acid pyridin-2-ylamine, 5-(2-chloro-4, 5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylic acid 啥琳-5- Base amine, 5-(2-chloro-4, 5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylic acid quinoline-8-yl decylamine, 5-(2-chloro -4,5-difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid isoindolin-5-yl decylamine, 5-(2-chloro-4, 5-difluoro-benzene Hydrazinyl)-1Η-pyrazole-3-carboxylic acid [3-ethoxy-5-(1-ethoxycarbonyl-1-methyl-ethyl)-pyridin-2-yl-hydrazine 206 318197 8 1322688 Amine, 5-(2-chloro-4, 5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylic acid [3-ethoxy-5-(1-ethoxycarbonyl) 1-hydroxy-ethyl)-pyridin-2-yl]-nonylamine, 5-(2-chloro-4, 5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylic acid [5-(1-carboxy-1-indenyl-ethyl)-3-ethyl Oxy-pyridin-2-yl]-nonylamine, 5-(2-chloro-4,5-difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid [5-(1- Mercapto-1-yl-ethyl)-3-ethoxy-π butyl-2-yl]-bristamine, 5-(2-chloro-4,5-difluoro-benzoinylamino -1Η-pyrazole-3-carboxylic acid (pyridin-2-ylindenyl)-decylamine, 5-(2-chloro-4, 5-difluoro-phenylhydrazino)-1Η-pyrazole 3-carboxylic acid [6-(thiomorpholin-4-yl)-pyridin-3-ylmethyl]-decylamine, 5-(2-chloro-4, 5-difluoro-benzoguanamine Base)-1Η-α-pyrazole-3-carboxylic acid [6-(1,1_dimercapto-1 λ 6_thio?, _4-yl)-π ratio bite_3_ylmethyl]- Amine, 5-(2-chloro-4,5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylic acid (4,5-dibromo-thiophen-2-ylmethyl)- Indoleamine, 5-(2-chloro-4, 5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylic acid (5-chloro-thiophen-2-ylindenyl)-decylamine , 5-(2-chloro-4, 5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylic acid (4-ethyl-2-methyl-oxazole-5-ylindole) -p-amine, 5-(2-chloro-4,5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylic acid (2-ethyl-4-mercapto-oxazole -5-ylindenyl)-nonylamine dihydrochloride, 5-(2-chloro-4, 5-difluoro- Hydrazinyl)-1Η-pyrazole-3-carboxylic acid 207 318197 1322688 ([2, 2' ]bithiophene-5-ylindenyl)-nonylamine, 5-(2-chloro-4, 5- Difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid (3-methoxy-thiophen-2-ylindenyl)-nonylamine, 5-(2-chloro-4, 5- Difluoro-benzoguanidino)-1Η-pyrazole-3-carboxylic acid (4,5-di-thiophen-2-ylindenyl)-decylamine, 5-(2-chloro-4, 5 -difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid (2,5-dimercapto-oxazol-4-ylindenyl)-nonylamine, 5-(2-chloro- 4, 5-Difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid hydrazine (2-hexyl-4-mercapto-oxazol-5-ylindenyl)-nonylamine, 5- (2-Chloro-4, 5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylic acid (4-methoxy-thiophen-3-ylmethyl)-decylamine, 5- (2-Chloro-4, 5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylic acid (4-mercapto-2-phenyl-oxazole-5-ylindenyl)- Indoleamine, 5-(2- gas-4, 5-difluoro-benzylidenylamino)-1Η-pyrazole-3-carboxylic acid (2-mercapto-4-phenyl-oxazole-5-曱-) guanamine, φ 5-(2-chloro-4, 5-difluoro-benzylidenylamino)-1 Η-pyrazole-3-carboxylic acid (4-hexyl-2-fluorenyl- Oxazol-5-ylmercapto)amine Hydrochloride, 5-(2-chloro-4, 5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid (6-a-pyridin-3-ylindenyl)-oxime Amine, 5-(2-chloro-4, 5-difluoro-benzylidenylamino)-1Η-pyrazole-3-carboxylic acid (6-a-pyridin-3-ylindenyl)-decylamine Hydrochloride, 5-(2-chloro-4, 5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid (4H-[1,2,4]triazole-3- Benthyl)-nonylamine 5-(2- gas-4,5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid 208 318197 1322688 (4H-[1,2,4 Triazol-3-ylmethyl)-guanamine dihydrochloride, 5-(2-chloro-4,5-difluoro-benzylidenylamino)-1Η-. Bis-zolyl-3-carboxylic acid (5-fluoro-4-indolyl-quinazolin-3-yl)-nonylamine 5-(2-chloro-4,5-difluoro-benzoinyl)-1Η-pyridyl Zyridin-3-carboxylic acid (5-fluoro-4-indolyl-quinazolin-3-yl)-nonylamine dihydrochloride, 5-(2-chloro-4,5-difluoro-benzhydrylamino) -1Η-pyrazole-3-carboxylic acid (4,6-dimercapto-pyridin-3-ylindenyl)-decylamine, 5-(2-chloro-4, 5-difluoro-benzoguanamine -1Η-pyrazole-3-carboxylic acid® (4,6-dimercapto-pyridin-3-ylindenyl)-decylamine dihydrochloride, 5-(2-chloro-4, 5-di Fluoro-benzoguanidino)-1Η-pyrazole-3-carboxylic acid (2-decyloxy-6-indolyl-pyridin-3-ylindenyl)-decylamine, 5-(2-chloro- 4, 5-Difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid (4-methoxy-6-indenyl-pyridin-3-ylindenyl)-nonylamine, 5- (2-Ga-4, 5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylic acid (4-oximeoxy-6-indolyl-pyridin-3-ylindenyl)- Indoleamine dihydrochloride, φ 5-(2-Gas-4,5-difluoro-benzoindolyl)-1Η-pyrazole-3-carboxylic acid (2-decyloxy-4, 6- Dimethylpyridin-3-ylmercapto)amine, 5-(2-chloro-4,5-difluoro-phenylhydrazino)-1Η-η-pyrazole-3-carboxylic acid. 2-methoxy-4,6-dimercapto-pyridin-3-yl -p-amine dihydrochloride, 5-(2-chloro-4,5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylic acid (3-indolyl-pyridine-2 -mercapto)-nonylamine, 5-(2- gas-4, 5-difluoro-phenylhydrazinoamino)-1 fluorene-carbazole-3-carboxylic acid (5-mercaptopyridine-3- Benthyl)-nonylamine, 5-(2- gas-4, 5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid 209 318197 1322688 (6-fluorenyl-n ratio Pyridin-3-ylindenyl)-nonylamine, 5-(2,4-dichloro-5-fluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid (6-mercaptopyridine) -2-ylmethyl)-nonylamine, 5-(2-chloro-4,5-difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid (pyridin-3-ylfluorenyl) - indoleamine dihydrochloride, 5-(2-chloro-4, 5-difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid (6-fluoro-pyridin-3-yl) Hydrazinyl)-nonylamine dihydrochloride, 5-(2-chloro-4,5-difluoro-anthracenylamino)-1Η-pyrazole-3-carboxylic acid® (3-carboxy-phenyl -methyl-decylamine, 5-(2- gas-4, 5-difluoro-phenylhydrazinyl MH-pyrazole-3-carboxylic acid 3-methylsulfonylamino-benzamide, 5_(2_气~4,5-diqi-benzoquinone-based amine group is 0-sodium _3-slow acid 4_a stone to buy aramidyl-tuberamine, 5-(2-chloro-4, 5-difluoro - aluminylamino)-1Η-pyrazole-3-carboxylic acid 3-ethylamino-branched amine, φ 5-(2-chloro-5-difluoro-benzhydrylamino)-1Η -pyrazole-3-carboxylic acid 4-ethylamino-barred amine, 5-(2-chloro-4, 5-difluoro-phenylhydrazino)-ih-pyrazole-3-carboxylic acid • monophenyl-thiazol-4-ylindenyl)-decylamine, * 5-(2-gas~4,5-difluoro-benzoquinone-based amine group than "sit-3-oxic acid ((R) -l-phenyl-ethyl)-decylamine, 5-(2-gas-4, 5-difluoro-benzhydrylamino)-ih-pyrazole-3-carboxylic acid ((S)-b Phenyl-ethyl)-nonylamine, 5-(2-gas-4, 5-difluoro-benzhydrylamino)-ih-pyrazole_3_carboxylic acid 210 318197 1322688 (6-phenoxy) -°bipyridin-3-ylindenyl)-nonylamine dihydrochloride, 5-(2-indolyl-4,5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylate Acid (6-Gas-pyridin-3-ylindenyl)-decylamine dihydrochloride, 5-(2-Gas-4,5-difluoro-benzylidenylamino)-1Η-pyrazole-3 -carboxylic acid (2-chloro-pyridin-3-ylmethyl)-decylamine dihydrochloride, 5-(2-methyl-4,5-difluoro-benzhydrylamino)-1Η-pyridyl Oxazole-3-carboxylic acid (6-chloro-pyridin-3-ylindenyl)-guanamine sodium salt, 5-(2-gas-4, 5-difluoro-benzhydrylamino)-1Η-pyridyl Oxazol-3-carboxylic acid hydrazine [1-(pyridin-3-yl)-ethyl]-nonylamine dihydrochloride, 5-(2- gas-4, 5-difluoro-benzhydrylamino) -1Η-pyrazole-3-carboxylic acid (2-fluoro-pyridin-3-ylindenyl)-guanamine dihydrochloride, 5-(2-chloro-4, 5-difluoro-benzoguanamine -1Η-pyrazole-3-carboxylic acid (2-methyl-0-pyridin-3-ylindenyl)-decylamine dihydrochloride, 5-(2-chloro-4, 5-difluoro- Benzhydrylamino)-1Η-pyrazole-3-carboxylic acid (biphenyl-3-ylmethyl)-decylamine, φ 5-(2-chloro-4, 5-difluoro-benzhydryl) Amino)-1Η-pyrazole-3-carboxylic acid ((lR,2S)-2-hydroxy-hydroquinone-bu)-guanamine, 5-(2-chloro-4,5-difluoro-phenylhydrazine Mercaptoamine)-111-pyrazole-3-carboxylic acid ((lS,2R)-2-hydroxy-hydroindol-1-yl)-nonylamine, 5-(2-chloro-4, 5-difluoro -Benzylamino)-1Η-η-pyrazole-3-carboxylic acid (6-phenyl-pyridin-3-ylindenyl)-decylamine dihydrochloride, 5-(2-chloro-4, 5-difluoro-phenylhydrazinoamino)-1Η-η-pyrazole-3-carboxylic acid (6-fluorenyl-pyridin-3-ylindenyl)-decylamine hydrochloride, 5-(2-chloro -4,5-difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid 211 318197 8 1322688 benzyl-indenyl-decylamine, 5-(2-chloro-4, 5-di Fluoro-benzoguanamine -1Η-pyrazole-3-carboxylic acid. Benzylamine, 5-(2-chloro-4,5-difluoro-phenylhydrazino)-1Η-°biazole-3-carboxylic acid phenylhydrazine Amine, 5-(2-chloro-4, 5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylic acid methyl-phenyl-decylamine, 5-(2-chloro-4 , 5-difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid ru (° 变 _ _ _ base) _ nitamine, 5- (2-chloro-4, 5-difluoro -benzylideneamino)-1Η-pyrazole-3-carboxylic acid (4-ethoxycarbonyl-piperidin-1-yl)-decylamine, 5-(2- gas-4, 5-difluoro- Benzoylamino)-1Η-pyrazole-3-carboxylic acid (4-methyl-piperidin-1-yl)-decylamine, 5-(2- gas-4, 5-difluoro-phenylhydrazine Stiffylamino)-111-〇 〇 -3- -3- 叛 叛 ( 4- 4- 4- 4- 4- 叛 叛 叛 叛 叛 叛 叛 叛 4- 4- 4- 4- 4- 4- ' ' ' ' ' ' ' ' ' ' ' ' ' ' Mercaptoamino)-1Η-pyrazole-3-carboxylic acid phenethylguanamine, 5-(2-gas-4, 5-difluoro-benzoguanidino)-1Η-pyrazole-3 -carboxylic acid. mercapto-phenethyl-decylamine, . 5-(2-chloro-4,5-difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid ethyl-benzene Base-bristamine, 5-(2-chloro-4, 5-difluoro-phenylhydrazino)-1Η-°biazole-3-carboxylic acid benzene (1,2,3,4-tetrahydroiso Quinoline-2-yl)-nonylamine, 5-(2- Chloro-4, 5-difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid 318197 212 .Ο / 1322688 ((S ) α-methoxy-benzyl)__decylamine, 5-(2-chloro-4' 5-difluoro-phenylhydrazino)1H pyrazole-3-carboxylic acid ((R)α-methoxy-benzyl)-bristamine, • 5-( 2-Chloro-4' 5-difluoro-adenylamino)1Η-pyrazole-3-carboxylic acid (1,2,3,4-tetrahydroindolyl~1~yl)-decylamine, 5 -(2-Gas-4, 5-difluoro-phenylhydrazinoamino)_1Η-pyrazole_3_carboxylic acid phenyl-propyl-decylamine, 5-(2-chloro-4, 5-di Fluorine- alum amide hydrazine _pyrazole _3 monocarboxylic acid _ butyl-styl-bristamine, 5-(2-chloro-4, 5-difluoro-benzhydrylamino)_1Η_ Pyrazole_3_carboxylic acid pentyl-phenyl-decylamine, 5-(2- gas-4' 5-difluoro-phenylhydrazino)1Η-pyrazole_3_carboxylic acid diphenyl fluorenyl - guanamine, 5-(2-chloro-4, 5-difluoro-phenylhydrazinyl hydrazine-pyrazole-3-carboxycarboxylic acid (D-But-2-ylmethyl)-nitramine hydrochloride , φ 5-(2-chloro-4, 5-difluoro-phenylhydrazinoyl H-pyrazole-3-carboxylic acid (deuterium 4-methyl)-bristamine hydrochloride, 5_ (2-Gas-4,5-one-benzoylamino)_1H-0 is more than 0-O-acid-(00-2-hydroxy-1-phenyl) -ethyl)-decylamine, • 5-(2-chloro-4, 5-difluoro-benzhydrylamino)-ih-pyrazole-3-carboxylic acid ((S)-2-hydroxy-1 -phenyl-ethyl)-chiral amine, 5-(2-chloro-4,5-difluoro-benzylidenylamino)-iH-pyrazole-3-carboxylic acid 4-dimethylamino- Benzylamine, 5-(2_乱_4,5-digas-benzoylamino group than salicyl-3_acid 213 318197 1322688 (furan-2-ylindenyl)-nonylamine, 5-( 2-Chloro-4, 5-difluoro-phenylhydrazinoamino)-1Η-indazole-3-carboxylic acid (thiophen-2-ylindenyl)-nonylamine, 5-(2-chloro-4, 5-difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid (2-methoxy-phenyl)-decylamine, 5-(2-chloro-4, 5-difluoro- Benzoylamino)-1Η-pyrazole-3-carboxylic acid (2-methoxy-phenyl)-indolyl-decylamine, 5-(2- gas-4, 5-difluoro-phenylhydrazine Hydrazinyl)-1Η-pyrazole-3-carboxylic acid• 4_didecylamino-benzylamine hydrochloride, 5-(2-chloro-4,5-difluoro-benzoguanamine Base)-111-°biazole-3-carboxylic acid 3-amino-benzylguanamine, 5-(2-chloro-4,5-difluoro-benzoguanidino)-1Η-carbazole-3 -carboxylic acid 4-amino-benzylamine, 5-(2-chloro-4,5-difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid 2-mercapto-benzylhydrazine Amine, φ 5-( 2-Chloro-4, 5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid 3-mercapto-benzylamine, 5-(2-gas-4, 5-difluoro -phenylhydrazinoamino)-1-pyridazole-3-carboxylic acid 3-didecylamino-benzylamine, 5-(2-chloro-4,5-difluoro-benzhydrylamino -1Η-pyrazole-3-carboxylic acid (2-methoxy-pyridin-3-ylindenyl)-nonylamine, 5-(2-chloro-4, 5-difluoro-benzoinylamino) -1Η-pyrazole-3-carboxylic acid 2-chloro-benzylamine, 5-(2-chloro-4, 5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylic acid 214 318197 8 1322688 3~Chloro-benzyl octaamine, 5~(2-chloro-4, 5_- disorder-stupidylamino)-ΐΗ-«» than saliva_3_ around acid-3~曱oxycarbonyl - benzalkonium, . 5-(2-chloro-4, 5-fluoro-adolino)-indole-. ratio. Sit _3_ temperate 3-carboxy-benzylamine, 5-(2-gas-4,5-di-I-abidocarbylamino group than α _3_acid (6-trifluorodecyl- Pyridin-3-ylmethyl)-decylamine, 5-(2- gas-4, 5-dioxo-benzhydrylamino)_1Η-η than salivary-3-dicarboxylic acid® (2-ethoxyl) -pyridin-3-ylmethyl)-decylamine, 5-(2-chloro-4,5-difluoro-benzhydrylamino)-1Η-π than sal-3-hydroxyacid (2-dimethyl Amino-ethyl)-bristamine, 5~(2-chloro-4,5-di-benzoylamino)_1Η-η than 嗤-3-carboxyl-acid ethyl-(2-di Hydrazinyl-ethyl)-guanamine dihydrochloride, 5-(2- gas-4, 5-dift-benzhydrylamino)-1Η-° than 嗤-3- oxic acid $ mourning Hexyl-(2-dimethylamino-ethyl)-nitramine, φ 5-(2-chloro-4,5-difluoro-benzhydrylamino)-1Η-pyrazole-3-dexamic acid (4-decyloxy-pyridin-2-ylmethyl)-decylamine, 5-(2-aza-4, 5-di-n-benzoguanidino)-1Η-α than sal-3-actate • (2,6-dimethoxy-tonoxa-3-ylmethyl)-decylamine, 5-(2- gas-4,5-difluoro-benzoylaminosyl-3-carboxylic acid 2-oxocarbonylcarbonyloxy-benzylamine, 5-(2-gas-4,5-difluoro-benzhydrylamino)-1Η-βΛ^-3-hypoacid 2-carboxyl Oxy-benzylamine, 5-(4,5-difluoro-2-indolyl-benzhydrylamino)-1Η-η-pyrazole-3-carboxy 215 318197 1322688 acid (6-methoxy- Pyridin-3-ylmethyl)-decylamine, 5-(2,4-dichloro-benzylidenylamino)-1Η-pyrazole-3-carboxylic acid (6_曱.oxy-pyridine-3 -ylmethyl)-decylamine, 5-(2- gas-4, 5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid (3,5-dimethoxy- Pyridin-4-ylindenyl)-nonylamine, 5-(4,5-difluoro-2-methyl-phenylglycosylamino)-1Η-α is more than 〇 -3- 叛 ( (2, 4 - dimethyl-oxazole-5-ylmercapto)-decylamine, 5-(2,4-di-5-a-benzo-ylamino)-1Η-α ratio 0 Acid® (2,4-dimercapto-purine. Sodium-5-ylmethyl)-bristamine, 5-(2- gas-4, 5-difluoro-phenylhydrazino)-1Η-pyridyl Oxazole-3-carboxylic acid (4-oximeoxycarbonyl-phenyl)-indolyl-decylamine, 5-(2-chloro-4, 5-difluoro-benzoinyl)-1Η-pyrazole- 3-carboxylic acid (4-repoylphenyl)-methyl-decylamine, 4-{[5-(2-gas-4, 5-difluoro-benzoguanidino)-1Η-pyrazole- 3-carbonyl]-mercapto-amino}-benzoic acid sodium salt, • 5-(2- gas-4, 5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylate Isopropyl-phenyl-decylamine, 5-(2-gas-4, 5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid (ethoxycarbonyl-methyl)- Phenyl-decylamine, 5-(2-Gas-4, 5-difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid (slow-methyl)-styl-decylamine , 5-(2-Ga-4-fluoro-benzhydrylamino)-lH-indazole-3-carboxylic acid benzamide, 5-(2,4-dichloro-benzoguanidino) - ΐΗ-η-biazole-3-carboxylic acid benzamidine 216 318197 1322688 amine, 5-(2-gas-5-fluoro-benzhydrylamino)-1Η-. Benzazole-3-carboxylic acid benzamide, 5-(2- gas-4, 5-difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid benzyl-phenyl-bristamine , 5-(2-chloro-4, 5-difluoro-phenylhydrazino)-1Η-°biazole-3-carboxylic acid (1-mercapto-1-phenyl-ethyl)-decylamine , 5-(2-Gas-4, 5-difluoro-phenylhydrazino)-1Η-°Bizozole-3-carboxylic acid H [2-keto-2-(piperidin-1-yl) -ethyl]-phenyl-decylamine, 5-(5-fluoro-2-methyl-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid benzamide, 5-(5-gas -2-mercapto-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid benzamide, 5-(4-decyloxy-2-mercapto-benzylideneamino)-1Η -pyrazole-3-carboxylic acid benzamide, φ 5-(4-chloro-2-methyl-phenylnonylamino)-1Η-pyrazole-3-carboxylic acid benzamide, 5-(5 -fluoro-2-indolyl-phenylhydrazinoamino)-1-indole-pyrazole-3-carboxylic acid benzamide, 5-(5-chloro-2-indolyl-benzoylamino) -1Η-pyrazole-3-carboxylic acid benzamide, 5-(2-chloro-4, 5-difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid (2-ethoxylated) 5-ethyl)-phenyl-bristamine 5 5-(2-fluoro-5-mercapto-benzylidenylamino)-1Η-pyrazole-3-carboxylic acid benzyl 217 318197 1322688 decylamine, 5- (5-gas-2- -benzimidylamino)-1 Η-pyrazole-3-carboxylic acid benzamide ' 5-(3-chloro-2,6-difluoro-phenylhydrazino)-1Η-pyrazole- 3-carboxylic acid benzylamine, 5-(2-chloro-3-fluoro-benzhydrylamino)-indole-indazole-3-carboxylic acid benzamide, 5-(2-chloro-4, 5 -difluoro-phenylhydrazinoamino)-1 Η-pyrazole-3-carboxylic acid ethylaminomethylmercaptomethyl-phenyl-decylamine, 5-(2-chloro-4, 5-difluoro -benzimidylamino)-1Η-pyrazole-3-carboxylic acid isobutyl-phenyl-decylamine, 5-(2-chloro-4,5-difluoro-benzoinylamino)- 1Η-pyrazole-3-carboxylic acid (2-oximeoxycarbonyl-ethyl)-phenyl-decylamine, 5-(2-gas-4, 5-difluoro-phenylhydrazino)-lH- Pyrazole-3-carboxylic acid (3-ethoxycarbonyl-propyl)-phenyl-decylamine, 5-(2-chloro-4,5-difluoro-benzoguanidino)-indole-pyrazole 3-carboxylic acid (2-sulfo-ethyl)-styl-decylamine, 5-(2-a-4,5-difluoro-anthracenylamino)-indole-pyrazole-3-carboxylate Acid (3-carbo-propyl)-phenyl-bristamine, 5-(2-carbo-4-methoxy-benzylidenylamino)-1-indole-pyrazole-3-carboxybenzamide , 5-(2-amino-5-methoxy-benzylidenylamino)-1-indole-pyrazole-3-carboxybenzamide, 5-(5-fluoro-2-hydroxy- Mercapto-amino) Η-pyrazole _3_carboxylic acid benzyl 218 318197 8 1322688 Amine, 5-(4-fluoro-2-trifluoromethyl-benzoguanidino)-lH" 嗓- 3-benzylidene, 5-(5-fluoro-2-trifluoromethyl-benzhydrylamino)-lH- than 0-sodium-benzylic acid, 5-(2- Chloro 5-difluoro-benzoinylamine-specific 3-indole (2-methoxy-ethyl)-phenyl-bristamine, 5_(2, 5-dimercapto-benzylidene Amino)-1Η-pyrazole-3-rebel acid _amine, 5-(2-chloro-5-mercapto-phenylhydrazino)-1Η-pyrazole-3 , 5-(2-Chloro-pyridin-3-carbonylamino)-1Η-pyrazole-3-reoxylated amine, 5-(4-chloro-pyridine-2-carbonylamino)-1Η-pyrazole 3-carboxylic acid ester amine, 5-(2,6-dichloro-pyridine-3-carbonylamino)-1Η-pyrazole-3-carboxylic acid benzamide, φ 5-(2-gas-4 , 5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid butyl-(4-ethoxyxo-phenyl)-bristamine' 5-(2-gas-4, 5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid butyl-(4-carboxy-phenyl)-decylamine, 5-(2-anthracene-0-pyrene- 3 -monoaminol)-1Η_ο than 0 sit-3~ benzyl myramine, 5 -(2-chloro-6-fluorenyl_0 Biting -3- several ylamino) -1Η ~ η ratio. Sitting on a tacrotic acid, 5-(3-chlorobite-4-m-amino-amine)-1Η-° ratio Jun-3, carboxy-junction amine, 318197 219 1322688 5-(2-gas-4 , 5-difluoro-arachnidylamino)-ih-° than saliva-3-pentanoic acid butyl-(4-ethoxycarbonylmethyl-phenyl)monodecylamine, • 5-(2-gas -4, 5-difluoro-benzoquinone-based amino group than sal-3-actinyl butyl-(4-carboxymethyl-phenyl)-decylamine, 5-(2- gas-4, 5-di Fluoro-phenylhydrazinoamino)-ιη-pyrazole-3-carboxylic acid (4-oxo-oxyl-phenyl)-(2-methoxy-ethyl)-decylamine, 5-(2- Gas-4, 5-difluoro-benzhydrylamino)-ιη-pyrazole-3-acid (4-carboxy-phenyl)-(2-methoxy-ethyl)-decylamine, ® 5-(2-gas-4, 5-difluoro-benzhydrylamino)-ιη-pyrazole-3-reaction acid (6-decyloxy-pyridin-3-ylindenyl)-decylamine Hydrochloride, 5-(2-mercapto-4, 5-difluoro-azalylamino)-1Η-pyrazole-3-acid (6-methoxy-pyridin-3-ylmethyl) - guanamine dihydrochloride, 5-(2- gas-4, 5-difluoro-phenylhydrazino)-lH-pyrazole-3-carboxylic acid (thiazol-4-yl-indenyl) - guanamine dihydrochloride, 5-(2-chloro-4, 5-difluoro-phenylhydrazino)-lH-pyrazole-3-carboxylic acid 4-[2-(morpholin-4-yl)-ethylaminomethylmercapto]-benzylguanamine dihydrochloride, 5-(2- gas-4,5-difluoro-benzoinylamino) )-1Η-σ ratio 0 sitting-3-o-acid 4-(morpholin-4-ylaminoindolyl)-benzylguanamine dihydrochloride, [4-({[5-(2-chloro-) 4,5-difluoro-phenylhydrazinoamino)-111-pyridin-3-carbonyl]-amino}-indolyl)-phenylhydrazinyl]-acetic acid sodium salt, 3-[4-( {[5-(2-Gas-4, 5-difluoro-phenylhydrazino)- 1 Η-to-mouth 羰-3-carbonyl]-amino}-indenyl)-phenylhydrazinyl] Sodium propionate, [5-(2-Gas-4, 5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylic acid (3,5-dimethyl-isoxazole- 4-ylmercapto)-indolyl hydrochloride, 220 318197 1322688 [5-(2-chloro-4,5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylic acid (1 ,3,5-tridecyl-1H-pyrazol-4-ylindenyl)-decylamine dihydrochloride, 5-(2- gas-4, 5-difluoro-benzhydrylamino)- 1Η-pyrazole-3-carboxylic acid (3,5-dimercapto-isoxazol-4-ylmethyl)-guanamine sulfonate, 5-(2- gas-4, 5-difluoro- Benzoylamino)-1Η-pyrazole-3-carboxylic acid 3-[2-(morpholin-4-yl)-ethylaminopurinyl]-benzylguanamine dihydrochloride, 5- (2-gas-4, 5- Difluoro-benzoguanidino)-1Η-»bisazole-3-carboxylic acid 3-(morpholin-4-ylaminoindolyl)-benzylguanamine dihydrochloride, • 5-(2 -chloro-4,5-difluoro-benzylidenylamino)-1Η-pyrazole-3-carboxylic acid {2-[2-(morpholin-4-yl)-ethylamino fluorenyl] -°pyridin-4-ylindenyl}-indoleamine trihydrochloride, 5-(2-chloro-4,5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylic acid [2-(morpholin-4-ylaminoindolyl)-pyridin-4-ylindenyl]-nonylamine trihydrochloride

trHL salt, 5-(2-gas-4, 5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid φ (6-decyloxy-pyridin-3-ylindenyl) - amidoxime sulfonate, 5-(2- gas-4, 5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid (6-decyloxypyridin-3- Benthyl)-guanamine hemisulfate, 5-(2-gas-4, 5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid (3,5-dioxane -Pyridin-4-ylmethyl)-decylamine dihydrochloride, 5-(2-Gas-4,5-difluoro-benzoinylamino)-1Η-η-pyrazole-3-carboxylic acid (4-Aminomethyl-pyridin-2-ylindenyl)-nonylamine trihydrochloride, 5-(2-chloro-4,5-difluoro-phenylhydrazino)-1Η-pyrazole 3-carboxylic acid (6-chloro-pyridin-3-ylindenyl)- amidoxime sulfonate, 221 318197 1322688 5-(2-chloro-4, 5_-gas-seeking amine group)- 1 Η-σ is more than cis-3-carboxylic acid (6-chloro butyl-3-ylmethyl octaamine di phthalate, 5-(2-chloro-4, 5-mono- benzoylamino) )-lH-nit^-3-acid (2,4-dimercapto-n-pyridin-3-ylmethyl)-decylamine hydrochloride, 5-(2- gas_4, 5- mess _Benzene arylamino)-1Η_〇 than 嗤-3-glycolic acid (pyridin-3-ylmethyl)-decylamine hydrochloride, 5-(2-chloro-4, 5- Monofluoro-methionylamino)-111-indole quinone-3-decanoic acid (6-decyloxypyridin-3-ylindenyl)-propyl-decylamine dihydrochloride, 5- (2_Chloro-4,-gas-present-branched amine-amino-3-pyreo[6-(piperidin-1-yl)-pyridin-3-ylindenyl]-nonylamine dihydrochloride, 5_(2- gas-4,5_-fluoro-benzylamino)-111-° than sputum-3-o-acid [6-(N-Phen-4-yl)-0-pyridin-3-yl曱基]-nonylamine dihydrochloride, 5_(2-chloro-4,5-·one gas-presentylamino)-1Η-πΛβ sit-3-oxo acid (3,5-dichloro-pyridine 4--4-mercapto)-indolyl hydrochloride, 5-(2-chloro-4, 5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylic acid (6-dimethyl Amino-pyridin-3-ylmethyl)-guanamine dihydrochloride, 5_(2_chloro-4,5-·one-n-bristylamino)-1Η-° than wow-3- Acid (6-dimethylamino-pyridin-3-ylindenyl)-propyl-decylamine dihydrochloride, 5-(2-chloro-4,5-difluoro-benzoinylamino) )-1Η-pyrazole-3-buffer acid (6-diethylamino-pyridin-3-ylmethyl)-guanamine dihydrochloride, 5_(2_chloro-4, 5-difluoro-benzene曱 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基Hydrochloride, 5_(2_chloro-4, 5-difluoro-benzoinylamino)-1Η-Β is more than 0 sitting-3-low acid (4-[1,2,3]嗟2° sitting -4-yl-aryl)-bristamine hydrochloride, 318197 222 1322688 5-(2-chloro-4,5-difluoro-phenylhydrazino)-1 Η-σ-pyrazole-3-carboxylate Acid (4-methyl-thiazol-5-ylindenyl)-nonylamine hydrochloride, 5-(2-chloro-4,5-difluoro-phenylhydrazino)-1Η-pyrazole-3 -carboxylic acid (2,4-dimercapto-thiazol-5-ylindenyl)-nonylamine hydrochloride, 5-(2- gas-4,5-difluoro-benzoinyl)-1Η -pyrazole-3-carboxylic acid [6-(4-hydroxy-piperidin-1-yl)-pyridin-3-ylindenyl]-nonylamine dihydrochloride, 5-(2-chloro-4, 5 -difluoro-benzoguanidino)-1Η-pyrazole-3-carboxylic acid 5-mercapto-pyrrol-2-ylguanamine dihydrochloride, 5-(2-gas-4, 5- Difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid quinolin-5-ylguanamine dihydrochloride, 5-(2-chloro-4, 5-difluoro-phenylhydrazine Amino-pyridyl-3-pyrazole-3-carboxylic acid quinoline-8-ylguanamine dihydrochloride, 5-(2-gas-4,5-difluoro-benzoinyl)-1Η -pyrazole-3-carboxylic acid isoquinolin-5-ylguanamine dihydrochloride, 5-(2-gas-4,5-difluoro-benzoinyl)-111-pyrazole-3 -carboxylic acid [6-(4-曱Piperidin-1-yl)-pyridin-3-ylmethyl]-nonylamine dihydrochloride, 5-(2-chloro-4, 5-difluoro-phenylhydrazino)-1Η-carbazole 3-carboxylic acid [6-(4-didecylamino-piperidin-1-yl)-pyridin-3-ylmethyl]-indolyl dihydrochloride, 5-(2-chloro-4, 5-difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid [6-(pyrrolidin-1-yl)-pyridin-3-ylindenyl]-nonylamine dihydrochloride, 5-(2-chloro-4,5-difluoro-benzylidenylamino)-1Η-pyrazole-3-carboxylic acid (pyridin-2-ylmethyl)-decylamine dihydrochloride, 5 -(2-chloro-4,5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid 223 318197 (S) 1322688 [6-(thiomorpholin-4-yl)_ Pyridin-3-ylmethyl]-nonylamine dihydrochloride, 5-(2-chloro-4, 5-difluoro-phenylhydrazino)-1 fluorene-pyrazole-3-carboxylic acid. 6-(1,1-di-yl-1 λ 6 thiazol-4-yl) 〇 咬 咬 -3-ylmethyl]-nitramine dihydrochloride, 5-(2-chloro-4 , 5-difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid aminomethylmercaptomethyl-decylamine, 5-(2-chloro-4, 5-difluoro-benzoic acid Mercaptoamino)-1Η-pyrazole-3-carboxylic acid (4-aminomercapto-phenyl)-mercapto-decylamine, zero 5-(2-, 4-di-5-fluoro-benzene Mercaptoamine)- 1Η-pyrazole-3-carboxylic acid fluorenyl-(4-mercaptoaminoindenyl-phenyl)-decylamine, 5-(2,4-dioxa-5-fluoro-benzhydrylamino group -1Η-pyrazole-3-carboxylic acid (4-didecylaminoindenyl-phenyl)-methyl-decylamine, 5-(2,4-dioxa-5-fluoro-phenylhydrazine Amino group)-1Η-°biazole-3-carboxylic acid (4-methylsulfonylaminocarbonyl-phenyl)-mercapto-nonylamine, 5-(2-chloro-4, 5-difluoro- Benzyl decylamino)-1 Η-pyrazole-3-carboxylic acid • (4-indolesulfonylaminocarbonyl-phenyl)-indolyl-decylamine sodium salt, 5-(2-gas-4, 5-difluoro-phenylhydrazinoamino)-1Η-°biazole-3-carboxylic acid (4·cyano-phenyl)-indenyl-decylamine, 5-(2-gas-4, 5- Difluoro-phenylhydrazinoaminopyrazole-3-carboxylic acid decyl-[4-(4Η-[1,2,4]triazol-3-yl)-phenyl]-indolylamine hydrochloride 5-(4-Azide-2-a-5-fluoro-benzimidamide)-1Η-β than quaternary-3-acid (4-cyano-phenyl)-methyl-decylamine, 5 -(4-azido-2-chloro-5-fluoro-benzoguanamine-based oxime-3-sodium sulfhydryl-[4-(1Η-tetrazol-5-yl)-phenyl]-decylamine , 318197 8 224 1322688 5 (2-Chloro-4,5-·--gas-presentylamine ratio. Sodium -3-acid [4-(Ν-hydroxyaminoiminoindolyl)-phenyl] methalamine, 5 (2 - chaotic-4,5_&lt;-fluoro-benzylamino )-1Η_β is more than 〇 -3- 缓 缓 缓 缓 缓 [4-(5-keto-2,5-dihydro-[1,2,4]βcarbazin-3-yl)-phenyl] -N-amine, 5 (2 gas - 4,5_-fluoro-branched amine group than "sit-3-low acid {4-[(2,2-dimercapto-propoxy)-methoxy Carbonyl]-phenyl-methyl-decylamine, 5-(2-gas-4, 5-difluoro-phenylhydrazino)-1Η-pyrazole-3-oxoic acid 4-[Ν-methoxy- Thiocarbonyloxy]-aminoimine fluorenyl]-mercapto-nonylamine, 5-(2-chloro-4,5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylate Acid sulfhydryl-[4-(5-thioketo-4,5-dihydro-[1,2,4]oxadiazol-3-yl)-phenyl]-bristamine, 5-(2-chloro -4,5-difluoro-phenylhydrazinoamino)-indenyl-pyrazole-3-carboxylate-yl-[4-(5-keto-4,5-dihydro-[^4]thiadiene Azole _3-yl) _ stupid = - guanamine, earth" 5_(2-chloro~4,5-difluoro-phenylhydrazino)- 1H_pyrazole-carboxylic acid {4-[1-( Cyclohexyloxy-carbonyloxy)-ethoxycarbonyl]-phenylindolyl-amine, 5-(2-chloro~4,5-difluoro-benzoinylamino) — 1H_pyrazole_3 monocarboxylic acid (4-ethoxycarbonyl-thiazol-2-yl)-ethyl-decylamine, 5-(2- gas-4, 5-difluoro-benzoinylamino ) _1H-pyrazolecarboxylic acid 2-methanesulfonylamino-benzamide, 5 (gas 4,5-fluoro-benzoylamino)-1}]-« than saliva-3-acid 318197 225 1322688 2-Ethylamino-tuberamine, 5_(2-Gas-4,5-difluoro-benzoquinone-based amine)-1Η~ο than saliva-3-acidic acid 2-- Hydrazinyl-n-decylamino)-benzylguanamine hydrochloride, 5-(2- gas-4,5-difluoro-phenylhydrazinoamino)-1 Η-pyrazole-3- oxo acid 3-(Didecylamino-methyleneamino)-benzylguanamine hydrochloride, 5-(2-wind)-4,5-difluoro-benzoquinone-based amine ratio. Acidic 4-(didecylamino-methyleneamino)-benzylguanamine hydrochloride, 5-(2- gas-4, 5-difluoro-phenylhydrazino)-indole-pyridyl Azole-3-decanoic acid #2-[1-(didecylamino)ethylidene]-benzylguanamine dihydrochloride, 5-(2- gas-4, 5-difluoro-phenylhydrazine Mercaptoamine)-ιη-pyrazole-3-dibenzoic acid 3-[1-(didecylamino)ethylamino]-benzylamine dihydrochloride, 5-(2- gas-4 , 5-fluoro-benzylamino)-1Η~σ than salino-3-decanoate 4-[1-(Didecylamino)ethylidene]-benzylamine dihydrochloride, 5_(2-gas_4,5-mono-p-bristylamino)-lH~n比3 _3 - oleic acid 2- (diethylamino-methyleneamino)-benzyl octaamine dihydrochloride, 5_(2 gas-4,5_&lt;-gas-branched amine Υ3-3-weilic acid 3-(diethylamino-methyleneamino)-benzylguanamine dihydrochloride, 5-(2-chloro-4,5-·monofluoro-branched The amino group is ≤3_decanoic acid 4-(diethylamino-ylideneamino)-benzylguanamine dihydrochloride, 5-(2-chloro-4, 5-difluoro-benzoic acid Mercapto-aminopyrazole-3-carboxylic acid 2-imine ethylamino-barred amine dihydrochloride, 5-(2-chloro-4,5-difluoro-benzhydrylamino)_11 }—Pyrazole_3_carboxylic acid 3-imine ethylamino-barred amine dihydrochloride, 5-(2-chloro-4, 5-difluoro-benzhydrylamino)_1Η_pyridyl Azole-3 carboxylic acid 318197 226 1322688 4-imine ethylamino-benzylguanamine dihydrochloride, 5-(2-chloro-4,5-difluoro-benzhydrylamino)-1Η-pyridyl Oxazole-3-carboxylic acid 4-cyano-benzylamine, 5-(2-chloro-4,5-difluoro-benzoinylamino)-1Η-pyrazole-3-carboxylic acid 3- [( 2-fluoro-iminophenylphenyl)-amino]-benzylamine hydroiodide Salt, 5-(2-chloro-4, 5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylic acid 4-[(2-fluoro-iminobenzyl)-amino ]-benzylamine hydroiodide, 5-(2- gas-4, 5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylic acid 3_(3,3-dimethyl _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ -ureido)-benzylamine, 5-(2-chloro-4,5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylic acid 2-(indolyl-4-sulfonate) Amino)-benzylamine, 5-(2-chloro-4, 5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylic acid 2-amino-6-fluoro-benzazole Amine hydrochloride, 5-(2-chloro-4,5-difluoro-benzofuranylamino)-111-° ratio -3 -acidic acid 2-amino-4, 5-difluoro- Benzylamine hydrochloride, 5-(2-chloro-4,5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid (hydroindol-1-yl)-decylamine, 5-(2-chloro-4,5-difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid (hydroindol-2-yl)-decylamine, 5-(2-gas- 4, 5-Difluoro-benzylidenylamino)-1Η-pyrazole-3-carboxylic acid (4H-indole-3-yl)-nitramine, 5-(2-chloro-4, 5- Difluoro-benzoguanidino)-1Η-pyrazole-3-carboxylic acid 227 318197 1322688 (4H-quinazolin-3-yl)-guanamine dihydrochloride, 5-(2-chloro-4,5-difluoro-phenylhydrazino)-1Η-indazole-3- Carboxylic acid (7-fluoro-4H-quinazolin-3-yl)-decylamine dihydrochloride, 5-(2- gas-4, 5-difluoro-benzhydrylamino)-1Η-pyridyl Oxazole-3-carboxylic acid (6-fluoro-4H-quinazolin-3-yl)-indolyl hydrochloride, 5-(2-chloro-4,5-difluoro-benzoinyl)- 1Η-pyrazole-3-carboxylic acid (2-ethoxy-2-methyl-1,4-dihydro-2H-quinazolin-3-yl)-decylamine, 5-(2-chloro-4 , 5-difluoro-phenylhydrazinoamino)-1Η-«biazole-3-carboxylic acid hydrazine (2-cyanopyridin-4-ylindenyl)-decylamine, 5-(2-gas- 4, 5-Difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid [2-(Ν-hydroxyaminoiminomethyl)-acridin-4-ylindenyl]-oxime Amine, 5-(2- gas-4, 5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid [2-(5-keto-4, 5-dihydro-[ 1,2,4]oxadiazol-3-yl)-pyridin-4-ylindenyl]-decylamine, 4_{[5_(4, 5_digas_2_mercapto-phenylindoleamine) -1Η-σ ratio. Sodium-3-φcarbonyl]-mercapto-amino}-benzoate sodium salt, 5-(4,5-difluoro-2-indolyl-benzoylamino)-1Η-pyrazole-3 -Carboxylic acid _[[4-(1Η-tetrakis-5-yl)-phenyl]-bristamine' 5-(2,4-dichloro-phenylhydrazino)-1Η-pyrazole 3-carboxylic acid (pyridin-3-ylmethyl)-decylamine, 5-(2,4-dichloro-5-fluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid ( Pyridin-3-ylindenyl)-nonylamine, 5-(2,6-dichloro-5-fluoro-pyridine-3-carbonylamino)-1Η-pyrazole-3-carboxylic acid (pyridin-3-yl) Indole, guanamine, 228 318197 1322688 5-[(3-Gas-benzo[b]thiophene-2-carbonyl)-amino]pyrimidine-3-carboxylic acid (pyridin-3-ylindenyl)- Indoleamine, 5-[(3-Gas-thiophene-2-carbonyl)-amino]-111-°Bizozole-3-Resin (11-bite-3_ylindenyl)-bristamine, 5-benzene Mercaptoamino-1Η-pyrazole-3-carboxylic acid (pyridin-3-ylmethyl)_bristamine' 5-phenylethylamino-1 -pyridazole-3-carboxylic acid (pyridine-3 -ylmethyl)monoamine, #5(2-indolyl-4,5-difluoro-benzylidenylamino)-1Η-° ratio. Oxy-3-(2-pyridin-3-ylindenyl)-nonylamine dihydrochloride, 5-(2-amino-4, 5-difluoro-benzylideneamine). Rounding acid (σ ratio 唆_3_ylmethyl)_bristamine' 5-(4,5-difluoro-2-indolesulfonylamino-phenylhydrazinyl)_1!1-° ratio ° -3-acidic acid (fl is a bit of a 3-methyl group) _ decylamine, 5-(2-acetamido-4,5-difluoro-phenyl fluorenylamine 嗤-3 - _ Acid (0 to bite_3_ylindenyl)_bristamine' 5_[(3,4,5-trichloro-thiophene-2-carbonyl)-amino]-1H-pyrazole-3-carboxylic acid (〇咬-3-ylindenyl)-bristamine' 5-(4,5-difluoro-2-indolyl-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid (2-cyano) -σ 咬-4-yl fluorenyl)-bristamine, 5_(4, 5-difluoro-2-indolyl-phenylhydrazinoamino)-1 Η-pyrazole-3-carboxylic acid [2 one ( 111_四零坐基)-〇比咬-4-ylmethyl]-bristamine '111-** than 啥5-di-hypo-acid 3-mercaptoamine 5-[(2,4-dichloro-benzene) </ RTI> </ RTI> </ RTI> </ RTI> </ RTI> </ RTI> </ RTI> </ RTI> </ RTI> </ RTI> </ RTI> </ RTI> </ RTI> </ RTI> </ RTI> </ RTI> </ RTI> </ RTI> </ RTI> <RTIgt; Salt, hydrobromide and hydriodic acid Inorganic acid salts such as nitrates, perchlorates, sulfates and phosphates; lower alkanoic acid salts such as decane sulfonates, trifluoromethanesulfonates and ethanesulfonates; aryl sulfonates Such as besylate and p-toluenesulfonate; carboxylates such as acetate, malate, fumarate, succinate, citrate, ascorbate, tartrate, oxalate and a maleic acid salt; and an amine acid salt such as glycine, lysine, arginine, auramine, amylin, and aspartic acid. Further examples thereof include alkali metal salts such as sodium salts, Potassium salts and bell salts; soil-measuring metal salts such as calcium salts and magnesium salts; metal salts such as aluminum salts; inorganic salts such as ammonium, amine salts, etc. such as third octylamine, dimethylamine, morphine, glucosamine , alkyl phenylglycine, ethylenediamine, N-methylglucamine, hydrazine, diethylamine, diethylamine, dicyclohexylamine, NN' dibenzylethylenediamine, gas Chicoro procaine, procaine (pr〇caine), diethanolamine, N-benzylphenethylamine, piperidine, tetramethylammonium, and cisplatin The compound of the present invention represented by the formula (I) may exist in various isomeric forms such as 'optical isomers, geometric isomers and tautomers. All such isomers And mixtures thereof are within the scope of the invention. The prodrugs and their metabolites can be derived from the ketone derivatives of the formula (1), their brews or other derivatives of the invention. Further, the compounds of the invention and their pharmacological effects Acceptable salts can be present in the form of various 318197 230 1322688 ^ conjugates (10) such as hydrates. These solvents are within the scope of the invention. The "prodrug" as used in the present invention is a derivative of the compound (1) of the present invention which has a chemically or metabolically decomposable group and which exhibits medicinal activity by hydrolysis and solvolysis, or decomposes under physiological conditions. And present drug activity. Examples include such compounds wherein the group is substituted by the following groups: -C0-alkyl, -C00-alkyl, _C0NH_alkyl-c〇-alkenyl, _c(9)-, and -(10)H-saturated, -C0-aryl, _c〇〇_aryl, _c_-aryl, zero-C0-heterocyclic, -C00_heterocyclic, _C0NH_heterocyclic (the alkyl group, aryl group and heterocyclic ring can be halogenated) Atom, alkyl group, mercapto group, alkoxy group, alkoxy group, amine group, amino acid, -P〇3H2, -S〇3H, -〇P〇3H2, -〇s〇3H, etc.), -C0- Polyethylene glycol residue, -coo-polyethylene glycol residue, -co_polyethylene glycol single alkyl residue, -coo-polyethylene glycol single-yard acid residue, _p〇3H2, etc.; The amine group in such compounds is substituted by the following groups: _co-alkyl, -(3)bualkyl, -C0-alkenyl, -C00-alkenyl, -C00-aryl, -C0-aryl' -C0-face|heterocyclic ring, -C00-heterocyclic ring (the alkyl group, alkenyl group, aryl group and heterocyclic ring may be via a halogen atom, an alkyl group, a hydroxyl group, an alkoxy group, a carboxyl group, an amine group, an amino acid, _p 〇3ll2, _s〇3H, -OPO3H2, -OSO3H, etc.), -CO-polyethylene glycol residue, _c〇〇-polyethylene glycol residue, -C0-polyethylene glycol monoalkyl Residue, -c〇〇-polyethylene glycol monoalkyl hydrazine residue, -p〇3H2, etc.; or the carboxyl group of these compounds is a trans-oxyl group, an aryloxy group (the alkoxy group and the aryloxy group) It can be replaced by a tooth atom, a burnt group, a thiol group, an alkoxy group, an ester group, an amine group, an amino acid, -P〇3H2, -SO3H, -OPO3H2, -〇S〇3H, etc.) Substituted by a base such as a polyethylene glycol monoalkyl ether residue. 318197 231 ^22688 The carbazole compound of the present invention or a salt thereof, an ester or other derivative thereof, a drug and a metabolite thereof, or a hydrate thereof and a solvate thereof, may be combined with a pharmaceutically acceptable carrier and orally Or it is administered parenterally in the form of a solid dosage form such as a tablet, a sac, a granule, or a powder, or a liquid dosage form such as a syrup or an injection. As used herein, "pharmaceutical composition" means a pyrazole compound or a pharmaceutically acceptable salt thereof, an ester or other derivative thereof, a prodrug or a metabolite thereof, or a hydrate or solvate thereof, as an active ingredient, and An excipient 'lubricant and a binder for preparing a solid formulation; or a homogeneous mixture of a third component such as a solvent, a solubilizer, a suspending agent, an isotonic agent, and a buffering agent for preparing a liquid formulation. Administration may be carried out orally using a tablet, a pill, a capsule, a granule, a powder or a liquid; or may be administered externally via the use of an injection such as intravenous administration and intramuscular administration, suppository or transdermal formulation. Parenteral administration includes intravenous muscle, subcutaneous, interstitial, nasal, intradermal, intraperitoneal, intraperitoneal, rectal, transvaginal, and intraperitoneal administration. The oral pharmaceutical solid composition according to the present month includes a key, a powder, and a granule. Such a solid composition H or a poly(tetra) substance is mixed with less - an inactive excipient such as lactose, mannitol, glucose propyl cellulose, microcrystalline cellulose, activated powder, polyethylene hydrazine Luo bite and Ming Cai acid town. According to the method, the (4) may also contain an excipient: an external additive such as a disintegrating agent, a stabilizer such as an antioxidant, and a solubilizing agent. Ingredients for intestines in the gastrointestinal tract, (4) (4) to be packaged (four) or as old as sugar, gelatin, hydroxypropyl cellulose, 318197 232 1322688 hydroxypropyl methylcellulose, m propyl methylcellulose, vitamins O-dibenzoic acid vinegar, macrogol, titanium dioxide and talc. 「 “Liquid composition for oral administration” includes pharmaceutically acceptable emulsions, solutions, suspensions, syrups and elixirs; it also includes commonly used solvents such as pure water and ethanol. The composition may contain a monthly adjuvant other than an inert solvent such as a solubilizing agent, a wetting agent and a suspending agent, a sweetener substance, a fragrance, and a preservative. "Intestinal injection of medicinal injection" can be prepared by a specified amount of activity =!, 1 float or emulsified in an aqueous solvent (such as steaming water for injection, Ringer's solution), or a solvent (for example, vegetable oil). Such as eucalyptus oil, sesame oil: Γ聚:: et al. B) dispersing agent (such as polypyrrolidine ethyl vaporized castor oil 6 〇, _, etc.), preservative (for example, p-phenylene difluoride: base It is prepared by using an isotonic agent (for example, in the process of sodium chloride or glycerol treatment, depending on the desired alcohol, glucose, etc.), such as cellulose, oil, D-glycan, etc. In this case), stabilizer C: such as solubilizer (such as sodium salicylate and acetic acid additives, if necessary, also ^), and a buffer (such as cut), etc. can add antioxidants, colorants and Other additives may be used as a material for the formulation, a lubricant, or a viscous material; for example, a shaped solubilizer suitable for a solid formulation, a county, 1 And a powder; a solvent for a liquid formulation, a dose, an isotonic agent, a buffer, and a demulcent. If desired, 233 318197 Φ) 1322688 It is also possible to use formulating additives such as preservatives, antioxidants, colorants, sweeteners, adsorbents and gelling agents according to conventional methods. Preferred examples of the "excipient" may include lactose, corn starch, sucrose, D-mannitol, d-sorbitol, starch, dextrin, crystalline cellulose, low-substituted hydroxypropylcellulose, carboxyindole Cellulose sodium, gum arabic, glucose and cerium oxide. Preferred examples of the hydrazine oxidizing agent may include sulfite and ascorbic acid. Suitable "disintegrating agents" include carboxymethyl cellulose, calcium carboxymethyl cellulose, sodium carboxymethyl starch, sodium croscarmellose, crosslinked Pirsspovidone, low substitution. Hydroxypropylcellulose and hydroxypropyl starch 0 binders include, for example, hydroxypropylcellulose, hydroxypropylmethylcellulose, polyvinylpyrrolidone, crystalline cellulose, sucrose, and powdered acacia (acacia). . The binder is preferably hydroxypropylcellulose or polyvinylpyrrolidone. Preferred examples of the lubricant may include magnesium stearate, stearic acid, talc, and colloidal silica. Preferred examples of "isotonic agent" include glucose, D_sorbitol, sodium carbonate, glycerin and D-mannitol. "pH adjusting agents" include citrates, phosphates, carbonates, tartrates, fumarates, acetates, and amine salts. Preferable examples of the "solubilizing agent" include polyethylene glycol, propylene glycol, D-mannitol, benzyl acetophenate, ethanol, arginyl decane, cholesterol, triethanolamine, sodium carbonate, and citric acid. 234 318197 1322688 Preferred examples of "solvent" include water for injection, alcohol, propylene glycol, diatomaceous earth, sesame oil, corn oil and eucalyptus oil. Preferred examples of the "suspending agent" include hydrophilic macromolecules such as polyethylene glycol, polyvinyl ketone, methyl cellulose, methyl cellulose, hydroxymethyl cellulose, hydroxyethyl cellulose, and hydroxy group. Propyl cellulose. Preferred examples of the "surfactant" may include sodium lauryl sulfate, lauryl alanine, an imprinted phospholipid, a gasification section, a chlorination section, and a monostearate. Preferred examples of # "moderator" include benzyl alcohol. Preferred examples of "buffering agents" include phosphate, acetate, carbonate and citrate buffers. Preferred examples of the "preservative" include paraoxybenzoic acid, butyl alcohol, benzyl alcohol, stupid ethanol, dehydroacetic acid and sorbic acid. When the present invention is used as an anti-diabetic agent, it can be administered systemically or locally by oral route or parenteral route. The dose can be changed according to age, body weight, symptoms and curative effect 'usually 1 mg to gram dose for adults It is administered once a week or several times a day. The compound (I) of the present invention may be prepared by mixing a suitable diluent, a dispersing agent, a adsorbent, a solubilizing agent or the like to prepare a solid composition or a liquid composition for oral administration or a formulation for parenteral administration such as an injection. The compound (I) of the present invention can also be used for the treatment and prevention of diabetes in animals other than humans such as mammals. The compound (I) of the present invention can be used in combination with a 318197 235 Γ 322688 or a plurality of other pharmaceutical agents in a manner commonly used in pharmaceutical practice. The present invention and an antidiabetic agent are used. "Combination use == Table does not contain the combination of the compound of the present invention (1) - one or more and is LI = but not particularly limited. Other agents may be administered in the form of a mixture containing the present invention or in a mixture. The drug can be administered at the same time, or the individual formulations can be used; =; the two formulations can be used in the present invention, and the compound, the pharmaceutical composition or the drug can be combined with other medicines, drugs, or drugs (hereinafter also referred to as With the administration of the drug), - the time of administration of the invented medical music or drugs and their accompanying drugs is not specifically based on clinical = simultaneous or at regular intervals. The dose of the accompanying drug may be based on the bed, according to the individual, The age and weight of the individual, the time of administration, the dosage form, the method of administration, and the combination are appropriately selected. The form of the same is not particularly limited, and the limitation is that the pharmaceutical composition of the present invention is combined with any of the medicinal compositions or Drug administration. Complicated medications include, (1) therapeutic or prophylactic agents for dyslipidemia, (2) therapeutic or prophylactic agents for obesity, (3) therapeutic or prophylactic agents for diabetes, and (4) diabetic complications. Treatment Or a prophylactic agent, and (5) a therapeutic or prophylactic agent for the use of the smear, and the sputum to 3 of these agents may be used in combination with the compound of the present invention.

318197 236 丄(1) Fibret (PPAR Q: receptor agonist), (2) PPAR5 receptor agonist, (3) microsomal triglyceride transfer protein (MTP) inhibitor, ( 4) cholesterol ester transfer protein (CETP) inhibitor, (5) statin (HMG-CoA reductase inhibitor), (6) anion exchange resin, (7) probuco (pr〇buc〇i ), (8) final acid, ® (9) phytosterol, (10) lipoprotein-Al (Ap〇lip〇pr〇tein-Al) inducer, (11) lipoprotein lipase (lpl) Activator, (12) endothelial lipase inhibitor, (13) ezetimibu, (14) I BAT inhibitor, (15) 鲛: 3⁄4: ene synthase inhibitor, • (16) ACAT Inhibitors, (Π) LXR receptor agonists, (18) FXR receptor agonists, (19) FXR receptor antagonists, and (20) adenosine A1 agonists, and their special cases include Crofi伯 (c 1 〇fi brate), bezaf ibrate, fenof ibrate, lovastatin, simvastatin, prava Pravastatin, fiurastatin, alto瓦 237 318197 1322688 atorvastatin, pi tavastatin, rosuvastatin, cerivastatin, cholestyramine, Clostem (cloestimide), fertility is the test of acid g (tocopherol 1^〇〇1^11&amp;16), Nicomo (111 (:0111〇1), Nislite (11"61^1:1 *〇1), soysterol or τ-orizan〇i. (1) (2) (3) (4) (5) (6) (7) (8) (9 "Therapeutic or preventive agents for obesity" include, for example, leptin formulations, pancreatic lipase inhibitors, norepinephrine-serotonin reuptake inhibitors, cannabinoid receptor antagonists, monoamine reuptake inhibition Agent, di-branched glycerol-glycotransferase (DGAT) inhibitor, glucose-dependent insulin-acting polypeptide (GIP) receptor antagonist, alizarin receptor agonist, bombesin receptor subtype 3 (BRS) -3) agonist, (10) perilipin inhibitor, (11) acetaminophen A carboxylase 1 (ACC1) inhibitor, (12) acetaminophen A carboxylase 2 ( ACC2) inhibitor, (1 3) fatty acid synthase inhibitors, (14) sn-dimercapto-glycero-3-phosphate thiol transferase (AGPAT) inhibitor, (15) pancreatic lipase A2 (pPLA2) inhibitor, (16) black skin Mel (melanocortin, MC) receptor agonist ' 238 318197 8 1322688 (17) neuropeptide Y5CNPY5) receptor antagonist, (18) non-coupling protein (UCP) inducer or activator, (19) carnitine palm醯-transferase l (CPT-1) activator, (20) CCK1 (CCKA) agonist, (21) ciliary neurokinetic factor (CNTF), (22) CRF2 agonist, (23) neuropeptide Y2 ( NPY2) receptor antagonist, (24) neuropeptide Y4 (NPY4) receptor antagonist, • (25) sigmoid receptor/3 agonist, (26) growth hormone, (27) ATP citrate decomposition Enzyme inhibitors, (28) 5-HT6 antagonists, and (29) 5-HT2C agonists, and their special cases include alizarin, oristat, sibutramine, "rimonabant" and "mazindol" ° "Therapeutic or preventive agents for diabetes" include, for example, (1) insulin preparations (injections), (2) low molecular weight insulin oral agents, (3) sulfonamides Urea receptor Agent (SU preparation), (4) non-sulfonylurea insulin activator, (5) potassium-dependent ATP (KATP) channel opener, (6) alpha glucosidase inhibitor, (7) alpha powder enzyme inhibitor , 239 318197 1322688 (8) Insulin sensitizer, (9) Low molecular tGLP-Ι receptor agonist, (1G) tGLP-Ι peptide analogue, (11) Dipeptide-based peptide peptidase IV (DPP- IV) inhibitors, (12) glycoside receptor antagonists, (13) glucocorticoid receptor antagonists, (14) biguanide, (15) SGLUT inhibitor, 隹(16) fructose-1, 6-bisphosphatase (FBPase) inhibitor, (17) glycogen synthase kinase 3 (GSK-3) inhibitor, (18) phosphoenolpyruvate carboxykinase (PEPCK) inhibitor, (19) protein tyramine Acid phosphatase 1B (PTPaselB) inhibitor, (20) Inositol phosphatase (SHIP2) inhibitor containing SH2 functional region, (21) Hepatic glucose phosphorylase (GP) inhibitor, (22) Glucose kinase activator , φ (23) GPR40 receptor agonist, (24) pyruvate dehydrogenase kinase (PDHK) inhibitor, (25) glutamic acid: fructose-6-phosphate aminotransferase (GFAT) inhibitor, (2 6) antioxidants; nitric oxide Remover, (27) carnitine palmitoyl transferase l (CPT-1) inhibitor, (28) growth hormone releasing factor (GHRF), (29) trimethyl glycerol lipase (hormone sensitive lipase) Inhibitor, (30) PPARr receptor agonist, (31) PPARr receptor antagonist, 240 318197 1322688 (32) PPARa/τ receptor agonist, (33) AMP-activated protein kinase (ΑΜΡΚ) activator , (34) adiponectin receptor agonist, and (35) point 3 adrenergic receptor agonist, and its special cases include insulin, tolbutamide, grixo Glyclopyramide, acetohexamide, chi〇rpropamide, glybuzole, gUbenclamide, geek ginseng Glcrazide, glimepiride, mitiglinide, repagl inide, nateglinide, VOgiib〇 Se), acarbose, migiitol, rosigridine cis-succinate Azone maleate), metformin hydrochloride, picochlor hydrochloride (?1〇运143201^11丫(11'0.111〇1^(16) and buffing salt Acid form • (buformin hydrochloride). "Therapeutic or preventive agents for diabetic complications" include, for example, (1) protein kinase cold (PKC; 5) inhibitors, (2) vasopressin (H) receptor antagonists, (3) aldose Reductase inhibitors, (4) vasopressin-converting enzyme (ACE) inhibitors, (5) advanced glycation end products (AGE) manufacturing inhibitors, (6) neuropathic therapeutics, and (7) diabetic neuropathy Therapeutic agents, 318197 241 1322688 and its special cases include epalrestat (kinedak), mesile, mexi letine hychochloride and imidapril hydrochloride. _ "Treatment or prophylaxis for hypertension" includes, for example, (1) thiazide, (2) thiazide diuretics, (3) loop diuretic, (4) Potassium retention diuretics, Lu (5) /5 blockers, (6) alpha, /3 blockers, (7) alpha blockers, (8) central sympathetic inhibitors, (9) peripheral sympathetic nerves Inhibitor (snake root wood), (10) #5 antagonist (benzothiazepin), (11) #5 antagonist (dihydro alpha ratio bite), φ (12) vasodilator, (13) vasopressin-converting enzyme (ACE) inhibitor, (14) vasopressin π receptor antagonist, (15) citrate, (16) endothelin ETA receptor antagonist, (17) endothelium Invertase inhibitor; Nipriloxime (Μρρ丨1 y S丨n) inhibitor, (18) prostaglandin; prostaglandin Fp agonist, (19) renin inhibitor, 242 318197 1322688 (20 N0S3 performance enhancer; prostacyclin analogue, (21) phosphodiesterase KPDE5A) inhibitor, (22) prostacyclin analogue, and (23) aldosterone antagonist,

And its special cases include hydrochlorothiazide, Treklo Messet (1:1*丨0:111〇0^1:11丨82丨(16), Banhai with bentylhydrochlorothiazide) , meticrane, indapamide, tripamide, chlortalidone, mefruside, furosemide, Spirone spironolactone, triamteren, atenolol, bisoprolol fumarate, betaxolol hydrochloride , bevantolol hydrochloride, metoprolol tartrate, acebutolol hydrochloride, cilipro hydrochloride (cel i pro 1〇1 hydrochloride) ), nipradi lol, tilsiolol hydrochloride, nadolol, propranolol hydrochloride, indone hydrochloride (i ndeno 1 ο 1 hydroch 1 or i de ), card Carteolol hydrochloride, pindolol, pindolo sustained release tablets, bunitrolol hydrochloride, penbutolol sulfate Bopindolol malonate, 243 318197 1322688 mosulalol hydrochloride, arotinolol hydrochloride, carvedilol, pull Labetalol hydrochloride, urapidil, terazosin hydrochloride, doxazosin mesilate, bonaxolone salt Bunazosin hydrochloride, prazosin hydrochloride, phentolamine • mesilate, cion idine hydrochloride, Guanxin Guanfacine hydrochloride, guanabenz acetate, methyldopa, reserpine, rescinnamine, azurepine benzoate Mlodipine besylate), aranidipine, efonidipine hydrochloride, cilnidipine, nicardipine hydrochloride, nisol Nisoldipine, ni trendipine, ni f edipine, sustained release rifapine, ni lvadipine, barnidipine hydrochloride ), felodipine, benidipine hydrochloride, manidipine hydrochloride, azelnidipine, didizine hydrochloride Di 11iazem hydrochloride), hydrazine hydrochloride, 244 318197 1322688 todoralazine hydrochloride, budralazine, cadralazine, caltopril (captopri 1), enalapri 1 maleate, aracepri 1 (alacepri 1), delapril hydrochloride, siraprox Lil (ci Lazapri 1), 1 isinopri 1 , benazepr i 1 hyolrochloride, imidapri 1 hydrochloride, tamoca Tamicapril hydrochloride, quinapri 1 hydrochloride, trandolapri 1 , perindopri 1 erbumine ), candesartan ci lexeti 1 , valsartan, telmisartan, olmesartan medoxomi 1 , nittopide sodium (sodium nitroprusside) or Shixiao I acid glycerin. Hereinafter, a method for preparing a compound (I) to give a ratio of a compound to a living room is described, but the production method of the present invention is not limited thereto. The amount of the solvent used in each step is not particularly limited as long as the reaction mixture can be thoroughly stirred. Further, in each step, the reaction can be carried out in a conventional manner, and the separation/purification can be carried out by using any of the routine methods or any of the routine methods, such as recrystallization or reprecipitation, or for separating and purifying the organic compound. Methods such as adsorption column chromatography, dispense column chromatography, ion exchange chromatography, and gel filtration chromatography. 245 318197 8 1322688 The following describes the preparation of the compound represented by the general formula of the present invention, but the present invention is not limited thereto. Thus, the compounds of the present invention can be prepared via the following Preparation Methods A (A-1 to A-3), Method B or Process c (C-1 to C-6) or according to the following examples, or by reference to such methods. When the compound of the present invention is prepared, the reaction sequence can be appropriately changed. The reaction can begin with steps that are considered reasonable. Protection and protection (deprotection) are available if required. Reactions other than the aforementioned steps can also be applied to the field. Reagents other than those described above can be suitably used to promote the reaction. The ί non-reaction diagram is an example of a representative preparation method, but the compounds of the present invention can be regarded as being limited to this. Any compound from each step Steps: Isolation and purification, or skip separation/purification as needed. A-1 Fortunately m: The aforementioned phase method 2 is shown below. Each reference symbol in the reaction formula is used in the sense of the word. Also applies to the description below. 318197 246 1322688

step 1

247 318197

1322688

Step 1: Preparation of Compound (A2); Compound (A2) can be obtained by hydrogenating a nitro group of Compound (A1) to an amine group in a solvent in the presence of a catalyst.

Examples of the solvent used in the reaction card include alcohols such as alcohols, ethanols, etc.; ethers such as dioxane, tetrahydrofuran, etc.; esters such as ethyl acetate; etc.;: solvent such as N, M-dimethyl F-amine, etc.; and water, etc. These solvents may be used singly or in combination. Examples of catalysts used in the rock-and-stone reaction include catalysts such as &amp; black, quaternary/secondary lock catalysts such as Raney, and starting catalysts such as oxidized chains, platinum oxide-carbon, etc. (Reference: M. fiudlicky ,

Reductions in 318197

248 1322688

Organic Chemistry, Wiley-Interscience, New York, 1984). The reaction temperature is from about 0 ° C to 100 ° C, and preferably from about 〇 ° c to room temperature. The reaction time is from about 1 minute to 48 hours, and preferably from about 30 minutes to 24 hours. Other hydrogen donors other than hydrogen may also be used, such as formic acid, ammonium formate, % hexapril, spelt, etc. (Reference: M. Hudlicky, Reductions in Organic Chemistry, Wiley-Interscience, New York, 1984 ♦ y). Further, 'other nitro reduction methods include methods in which zinc/hydrochloric acid, tin (II) chloride, sodium hydrogen sulfite, titanium (III) chloride, and the like can also be used (reference: M. Hudlicky, Reductions in Organic Chemistry, Wiley-Interscience, New York, 1984). Step 2: Compound (A5) is prepared from compound (A3) by the method of chlorine synthesis, and the compound (A2) is deuterated by using the compound (A4) in the presence of a base. Compound (A5) can be obtained from an amine group.

HOOC (A3) (A4)

Step 2

Examples of the reactant used in the formation of the sulfhydryl group include oxasulfone gas, sulfinic acid 249 318197 1322688 helium gas, phosphorus pentachloride, and the like. If desired, N,N-dimethylformamide can be used to promote the reaction. Further, examples of the solvent used in the reaction include ethers such as diacetyl, tetrahydrofuran, dioxane, 1,2-dimethoxyethane, diglyme, etc.; hydrocarbons such as benzene , toluene, hexane, xylene, etc.; halogenated hydrocarbons such as monochloromethane, chloroform, carbon tetrachloride, iota, dichloroethane, etc.; esters such as ethyl acetate, methyl acetate, butyl acetate, etc. These solvents may be used singly or in combination. • The reaction temperature is from about -20 ° C to 120 Torr, and preferably from about TC to 80 ◦ C. The reaction time is from about 10 minutes to 48 hours, and preferably from about 30 minutes to 24 hours. Examples of the solvent for the deuteration reaction include _ such as diethyl hydrazine, tetrahydrofuran, monomethane, 1,2-dimethoxyoxyl, diethylene glycol dioxime, etc.; hydrocarbons such as benzene, toluene, hexane , xylene, etc.; toothed hydrocarbons such as dioxane, chloroform, tetragas fossil, 1,2-chloroethane, etc.; esters such as ethyl acetate, ethyl ketone, butyl acetate | etc., a polar solvent such as acetone, n, n-didecylacetamide, dimethyl hydrazine, etc.; and water, etc. These solvents may be used singly or in combination. Examples of the base used in the reaction include an organic base such as Triethylamine, pyridine, 4-didecylaminopyridine, N-mercaptomorpholine, etc.; inorganic bases such as lithium hydroxide, sodium hydroxide, potassium hydroxide, sodium carbonate, potassium carbonate, sodium hydrogencarbonate, carbonic acid Wind discharge, etc. The reaction temperature is from about 〇 °C to 12 (TC, and preferably from about 〇.〇 to 95 318197 250 1322688 0C. The reaction time is from about 10 minutes to 48 hours. And preferably from about 30 minutes to 24 hours. The compound (A5) can also be obtained by directly coupling the compound (A3) with the compound (A4) by another method for forming a reaction of a guanamine bond. Examples of useful methods include liquid The phase synthesis method comprises a mixed acid needle method, an acid stack method, a DCC method, an EDC method, an EDC-ΗΟΒΐ method, an EDC-HOSu method, another active ester method, a CDI method, and a peptide solid phase synthesis method. 0 (DCC; 1 , 3-dicyclohexylcarbodiimide) (EDC, 1-ethyl-3-(3'-dimethylaminopropyl)carbodiimide) (HOBt: 1-aminobenzotriene) Squatting) (HOSu; 1-hydroxybutanediimine) (CD I; 1, hydrazine - alkyl bis-platinum) Compound (A6) is obtained by solvent hydrolysis of the ester group of the compound (A5) to obtain a compound • (A6) °

(A5) Step 3

Examples of the solvent used in the reaction include alcohols such as decyl alcohol, acetamidine, etc., ethers such as dioxane, tetrahydrofuran, etc.; hydrazines such as acetone, etc., such as Ν'N-didecyl decylamine, two Sulfoxide, etc.; and water can be used singly or in combination. Etc., 318197 251 1322688 Examples of the use of the reaction include metal hydroxides such as sodium hydroxide, potassium hydroxide; alkaline earth metal hydroxides such as barium hydroxide. The reaction temperature is from about 〇 ° c to loot, and preferably from about 〇 t to room temperature. The reaction time is from about 10 minutes to 48 hours, and preferably from about minute to 24 hours. Step 4 to Step 8" compound (a π 掣偌 will now explain the summary of Step 4 to Step 8. The preparation of the compound represented by the formula (1) can be carried out by separating the compound (A6) in which the carboxychun group is activated. Amidoxime such as imidazolide (compound (A7); Step 4 and Step 5 of Preparation Method A_i) or active ester such as oral HOBt ester (compound (Α8); Step 6 and Step of Preparation Method Α_2 or HOSu Ester; For example Next, the isolated active carbonyl compound (A6) and the amine (A9) are coupled by a guanamine bond. &quot; The compound represented by the formula (I) is directly reacted from the compound (A6) by a known amine bond formation reaction. Preparation, such conventional guanamine bond formation reactions such as hydrazine liquid phase synthesis methods such as mixed acid anhydride method, sulfhydryl azide method, DCC method, edc method, EDC-HOBt method, EDC-HOSu method, other active ester method Or a CDI method, or a peptide solid phase synthesis method to form a guanamine bond with a compound as an amine (a旳 without separating the aforementioned reactive carbonyl compound (step 8 of the following Preparation Method A-3). E. Gross., The Peptides, Learning Press, 198] years): Compound (I) is permeated through ruthenium [A7]; Preparation of compound (A7) 318197 252 丄 Compound (A7) can be used in solvent and CDI via compound (A6) Obtained by reaction.

Examples of the solvent used in the reaction include ethers such as tetrahydrofuran and the like; halogenated hydrocarbons such as chloroform and the like; hydrocarbons such as toluene and the like; and polar solvents such as NN-dimethyl carbamide and the like. These solvents may be used singly or in combination. The reaction temperature is from about 0 ° C to 1 Torr. Oh, and preferably from room temperature to about 8 Torr. The reaction time is from about 1 minute to 48 hours, and preferably from about 3 minutes to 24 hours. When a CDI analog such as hydrazine, i,-carbonyl hydrazine (2-mercaptoimidazole) is used instead of CD I, the corresponding reactive lanthanide can be obtained. The compound (A7) or the corresponding active guanamine can be obtained by using other active guanamine synthesis reactions. Step 5: From the compound (A7), the compound represented by the formula (I) can be obtained by reacting the compound (A7) with a solvent (A9) in a solvent. 253 318197 1322688

R· (A7) .N-H (A 9) Step 5

Examples of the solvent used in the reaction include ethers such as tetrahydrofuran and the like; esters such as ethyl acetate; halogenated hydrocarbons such as gas; etc.; hydrocarbons such as toluene and the like; and polar solvents such as N,N-dimethylformamidine. Amines, etc. These solvents can be used alone or in combination. The reaction temperature is about 〇.匚 to 10 (rc, and preferably from about 〇. 匚 to room temperature. The reaction time is from about 10 minutes to 48 hours, and preferably from about 3 minutes to 24 hours. : Preparation of a ruthenium by a compound 厶铷 丨 ^ ^ ^ ^ 6 : From the compound (A6) prepared bismuth active vinegar compound (10) can be obtained by coupling with HOBt via the compound (10) in the presence of a solvent in a solvent.

ΜΗ I N

) 6 A c 6 _ΚΛ· exhaustion

Examples of the coupling agent include carbodiimides such as EDC, dcc, etc.; and haloformates such as ethyl chloroformate and the like. Examples of the solvent used in the reaction include ethers such as tetrahydrofuran, vinegars such as ethyl acetate, etc.; toluene hydrocarbons such as chloroform; hydrocarbons such as toluene, etc. and polar solvents such as N,N-dimethyl Amine and so on. These solvents can be used alone or in combination 318197 C0 254 1322688. The reaction temperature is about 〇. (: to 10 (rc, and preferably from about 〇. 匸 to room temperature. The reaction time is from about 10 minutes to 4 Torr, and preferably from minute to 24 hours. When hydrazine-hydroxy quinone is used) For example, when H〇Su is substituted for H〇Bt, the corresponding active vinegar is obtained. 'Step 7: The compound represented by the formula (1) can be obtained from the compound (A8), and the compound represented by the formula (1) can be via the compound (A8). It is obtained by reacting a solvent with an amine # compound (A9).

Examples of the solvent used in the reaction include ethers such as tetrahydrofuran and the like; esters such as ethyl acetate; etc.; toluene hydrocarbons such as gas imitation, etc.; hydrocarbons such as toluene, etc.; and polar solvents such as N,N-didecyl Formamide, etc.; and water. These solvents may be used singly or in combination. The reaction temperature is from about rc to 10 (rc, and preferably from about 〇 &lt; t to room temperature. The reaction time is from about 1 minute to 48 hours, and preferably from about 3 minutes to 24 hours. Preparation method A.-3: directly from compound Q6)f", compound ancient, soil; Step 8: preparation of compound r τ from compound (A6), compound represented by general formula (I) Directly prepared from the compound (A6) by knowing the amine bond formation reaction, such as the guanamine bond formation reaction such as 318197 255 1322688 'DCC method, EDC CDi method; or liquid phase synthesis method such as mixing method, The sulfhydryl method, the rhyme method, and other active vinegar 4 peptide solid phase synthesis methods. In or

The solvent used in the reaction (4) includes _ such as vinegar such as acetic acid, gfc, occupant, etc.; hydrazines such as B1, E1, etc., (4) hydrocarbons such as gas, etc.; Such as N, N-dimethylformamide, etc.; and water I, etc., used alone or in combination. Special, the agent can be, and preferably by about. The enthalpy to the chamber is hourly, and preferably from about 3 Torr, the reaction temperature is from about 〇 °C to 1 〇 〇. The reaction time is from about 1 minute to 48 minutes to 24 hours. Preparation Method B:

Preparation Method B is shown below. The individual component symbols in the formula are defined in the same manner as described above. This also applies to the following instructions. 318197 256 1322688

1322688 Free funeral 1: Preparation of compound (B2)

In the same manner as the formation of the mercapto chloride in the second step of the production method A, the compound (B2) can be obtained from the compound (B1). X Step 1

CI Ν-Ν (Β1)

N-N (B2) Step 2: Preparation of Compound (B4) The compound (B4) can be obtained by reacting the compound (B2) with a solvent, if necessary, in the presence of the compound (B3).

N-N (B2) ί&gt;-Η

R (Β3) Step 2

NO, (Β4) Examples of the solvent used in the reaction include ethers such as diethyl ether, tetrahydrofuran 'dioxane, 1,2-dimethoxyethane, diethylene glycol dimethyl ether, and the like; hydrocarbons such as benzene, Toluene, hexane, xylene, etc.; todenated hydrocarbons such as dichloromethane, gas, four gas fossils, 1,2-diethylene, etc.; esters such as ethyl acetate, acetic acid, methyl sulfonium, acetic acid Butyl ester and the like; polar solvents such as C-, N, dimethyl-methylamine, etc.; and water. These solvents may be used singly or in combination. Examples of the base to be used include organic bases such as triethylamine, pyridine, 4-dimethylaminopyridine, N-methylmorpholine, etc.; inorganic bases such as lithium hydroxide, sodium hydroxide, potassium hydroxide, sodium carbonate , potassium carbonate, sodium hydrogencarbonate, potassium hydrogencarbonate 318197 258 ^ 22688 and so on. The reaction temperature is from about 0 C to 12 0 C ' and preferably from about 〇 ° c to 60. Hey. The reaction time is from about 10 minutes to 48 hours, and preferably from about 3 minutes to 24 hours. t (3) The compound (B6) can be hydrogenated with a nitro group of the compound (B4) in the same manner as in the step 1 of the preparation method a to obtain a compound (B6). Another

(B4) rSn

Nh2 NN CB6) (Step 3) No. 4: The compound π is prepared from the compound (B6), and the compound represented by the formula (I) can be passed through a solvent in the presence of a base in the same manner as in the step 2 of the production method. It is obtained by using the compound (A4) to oxime the amine group of the compound (B6).

Preparation Method C: Pyrazole compound _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ The resulting solution is allowed to stand, and the formed solid is filtered, whereby a salt of the compound represented by the formula (1) can be obtained. _Preparation method The compound represented by the formula (I) is dissolved in the solvent A, and an acid or a base (either in itself or in a solution) is added thereto. The resulting solution was concentrated and allowed to stand. The formed solid is filtered and discharged, whereby a salt of the compound represented by the formula (1) is obtained. σ Preparation Method C-3 The compound represented by the formula (1) is dissolved in a solvent, and an acid or a test (either in itself or in a solution) is added thereto. The solvent hydrazine was added to the resulting solution, and after the autumn, the compound was placed. The solid formed is filtered to thereby obtain a salt of the compound represented by the formula (I). The compound represented by the preparation method C-4 is dissolved in the solvent A, and an acid or a test (either in itself or in a liquid) is added thereto. The resulting solution is allowed to stand to form a 遽 遽 ’ ’ to thereby obtain a hydrazine of the compound represented by the formula (1). I preparation method c-5 Once the compound is dissolved in the solvent, the acid or the test (self. The solution is concentrated and allowed to be released. The second: &lt; the solid is filtered out] The compounding method C-6 represented by the formula (1) wherein the compound represented by the formula (I) is dissolved or dissolved in a solution is added thereto. An acid or test (self y Β is added to the resulting solution, and then 318197 260 is allowed to stand. The formed solid is filtered, whereby a salt of the compound of the formula (I) can be obtained. The addition of the monoacid addition salt can be carried out by adding the diacid addition residue L prepared according to the aforementioned preparation method to C 6) to the above (4) A, and letting it be placed. Examples of the mono-addition salt include dihydrochloride, dimethanesulfonate and the like. Examples of monoacid addition salts include monohydrochloride and monomethanesulfonate. Examples of the "solvent A" used in the production methods C_1 to C-6 include alcohols such as methanol, ethanol, propanol, etc.; ethers such as diethyl ether, tetrahydrofuran, dioxane, 1'2-dimethoxyethane , diethylene glycol dimethyl ether, etc.; hydrocarbons such as benzene, toluene, hexane, xylene, etc.; halogenated hydrocarbons such as dichloromethane, chloroform, carbon tetrachloride, 1 '2-dioxaethane, etc.; Such as ethyl acetate, methyl acetate, butyl acetate, etc.; polar solvents such as propyl, N, N-dimethyl ketoamine, disulfoxide, water, and the like. Examples of the "solvent B" used include ethers such as diethyl ether, tetrahydrofuran, dioxane, 1,2-dimethoxyethane, diethylene glycol dimethyl ether, etc.; hydrocarbons such as stupid, Toluene, hexane, xylene, etc.; abusive hydrocarbons such as Erqijiayuan, chloroform four gasification, 1,2-dichloroethane, etc.; esters such as ethyl acetate, methyl acetate, butyl acetate, etc. . Examples of useful "acids" include inorganic acids such as hydrogen acid, hydrobromic acid, sulfuric acid, etc.; carboxylic acids such as malic acid, citric acid, oxalic acid, etc.; sulfonic acids such as methanesulfonic acid, benzenesulfonic acid, p-toluenesulfonic acid, etc. . Hydrogen acid and p-toluenesulfonic acid are preferred. Examples of the "base" to be used include inorganic bases such as sodium hydroxide, sodium hydride, 318197 261 and organic amines such as ethanolamine hydroxide, carbonic acid dance, and the like; and diethylamine and the like. Preferably, the aqueous sodium hydroxide is as follows. However, the present invention will now be described with reference to the accompanying examples. Reference Example 1: ~^-虱丰甲1基胺基呻隹一-3_carboxylic acid imidazole, amidoxime, a certain amine, 1_Η-carbazole-3-carboxylate soap, 埽; 5-difluoro-laughing

To a solution of 2-gas-4,5-difluoro-benzoic acid (508·20 g) in toluene (250 ml) was added hydrazine, dimethyl-dimethylamine (0.2 ml). At 65 ° C, sulfinium chloride (230 liters) was added dropwise. After stirring at 120 ° C for 3 hours, the reaction solution was concentrated under reduced pressure, and the obtained residue was evaporated to dryness ( bp 51 ° C to 64 ° C (130 Pa to 140 Pa)) to give an oily title. Compound (534. 45 g). Step 2: Preparation of ethyl 5-nitro-3-pyrazolecarboxylate; Η 广. Ν°2

H3l n-N Η 262 To a solution of 5-nitro-3-pyrazolecarboxylic acid (310.24 g) in ethanol (3 liters) was added hydrazine sulfonic acid (143 ml). (: stirring separator. After the obtained reaction solution was concentrated under reduced pressure, water (1.5 L) was added to the residue, followed by cooling in an ice bath to remove aqueous carbonic acid (by dissolving 15 3 g of potassium carbonate in 750) The resulting solid was filtered to give the title compound (343.09 g) as white crystals.

Ethyl 5-nitro-3-pyrazolecarboxylate (331.48 g) in tetrahydrogen. A solution of 7.5% K-carbon (30. 036 g) was added to a solution of EtOAc (1.5 L) and ethyl acetate (1.5 L), and the mixture was stirred overnight at room temperature under a hydrogen atmosphere. After the catalyst was removed by filtration, the filtrate was evaporated. m. Step 4: 5-(2-f-/ · • ‘ acid ethyl ester

Pyridine (丨53 ml) was added to a solution of ethyl 5-amino-3-pyrazolecarboxylate (265-38 g) in tetrahydro-di-fusin 318197 263 1322688 (1 · 33 liters). Reference Example ^ The obtained 2-gas-4,5-difluorobenzhydrazide (362·g) was added dropwise with ice-cooling. The obtained mixture was added, and the mixture was stirred at room temperature for 2 hours. The obtained reverse-concentrated mixture was concentrated under reduced pressure and crystallised from 2-propanol-water to give the title compound (538.85 g. @ K2-氯-4, 5-difluoro-benzyl base) - preparation of -3-

η υ C1 in 5-(2-Gas-4, 5-difluoro-phenylhydrazino)-1 Η-pyrazole-3-carboxylic acid ethyl vinegar (568·22 g) in ethanol (1 L) Into the suspension, water (soak) was added, followed by cooling with an ice bath to add 4 aqueous sodium hydroxide (500 ml). The reaction mixture was added dropwise to 3 ν • hydrochloric acid (1.2 L). Water (2 L) was added to the resulting suspension, and the mixture was stirred at room temperature. The obtained crystals were filtered, dried mjjjjjjjj • Triazole-Bu-5-(2-Aza-4, 5-difluorobenzamide) An amine preparation

264 318197 in 5-(2-Gas-4, 5-difluoro-benzoamitoylamino)_iH-pyrazole-3-carboxylic acid (4.88 g) in n,N-dimethylformamide To a solution of (7 mL) was added 1-d-phenyl and tri-hydrazine monohydrate (2.73 g), followed by edc hydrochloride (3.42 g). After stirring at room temperature for 24 hours, 120 ml of water was added to the reaction mixture in portions over a period of about 2 hours. The solid formed was filtered to give the title compound (j. H NMR (400MHz, DMSO-de) ^ · 13.52(3H, s s), 11.25(2H, s), 8. 01-7. 82(4H, ra), 75-7. 71(1H, m), 7. 60-7. 54(1H, m), 7. 45-7. 41 (1H, m), T. 〇4(lH, s). Oxygen-4, 5-diindole-lamomethylamine ))-iH-pyrazole-3-carboxyl

Add 5-(2-gas-4, 5-difluoro-benzene) dropwise at 55 ° C in a suspension of 1' Γ-carbonyldiimidazole (64·65 g) in tetrahydrofuran (1.3 liter) A solution of mercaptoamine MH-pyrazole-3-carboxylic acid (loo· 5 g) in tetrahydrofuran (7 mL). After stirring at 73 ° C for 1 hour, ethyl acetate (5 mL) was added. Then, it was concentrated under reduced pressure. To the residue was added ethyl acetate (yield) and hexanes (2 liters). The obtained suspension was added to ice water (1 liter) under ice-cooling. The solid which formed was filtered to give the title compound ( </RTI> 10.42 g) as white crystals. 265 318197 1322688 * NMR (400 MHz, DMSO-de) (5: 13.97 (1H, br s), li· 66 ( 1H, br s), 8· 76 (1H, s), 8.05-7.87 (3H, m), 7.18 (1H, s), 6.90 (1H, s). Gold test 2: 3-amino-methyl- 2—Mu and lift it _ pyridine 槊偌 辉 一 1 1 : 2-isopropyl aldehyde-nicotine guanamine

60% sodium hydride (640 mg) was added to a solution of 2-oxo-nicotinamide (0.5 g) in 2-propanol (45 ml). After stirring at 10 °C for 2 days, the mixture was evaporated. The organic layer was washed with 1 N hydrochloric acid, dried over anhydrous sodium sulfate and then concentrated. The residue was purified by EtOAc EtOAc (EtOAc:EtOAc:

Triethylamine (2.8 mL) was added to the solution. The product was added dropwise trioxane (1.1 ml) dropwise. Adding the saturated aqueous sodium hydrogencarbonate to the obtained reaction solution, and then adding the solution to the obtained solution of the 2-isopropoxy group (1.64 chloroform (16 ml) in an ice bath and stirring at room temperature overnight, the solution was obtained. The mixture was stirred for 318 197 266 1322 </ br> </ br> </ br> </ RTI> </ RTI> </ RTI> <RTIgt; </ RTI> </ RTI> </ RTI> </ RTI> <RTIgt; Hyperthyroid-2-pyrene-capped 吼咭-吼咭夕事Α CH,

To a solution of 2-isopropoxy-nicotinyl nitrile (137 g) in methanol (25 ml), concentrated hydrochloric acid (2.1 ml) and 7. 5% K-carbon (780 mg), the resulting mixture was stirred at room temperature under a hydrogen atmosphere for 18 hr. After the catalyst was removed by filtration, the filtrate was concentrated under reduced pressure and the residue was dissolved in water and washed with ethyl acetate. The aqueous layer was then alkalized and extracted with chloroform. The residue was purified by EtOAc EtOAc (EtOAc) elute Next, the following compounds were prepared according to the aforementioned preparation methods. φ [Examples 1] H 2 -oxy-4, 5-di^- bromo-based carboxylic acid (pyridine bis 3-ylmethyl valine amine preparation;

5-(2-Chloro-45-difluoro-bromo-ylamino)-1Η_^嗤-3-resinic acid oxime (6 〇() g) obtained in Step 7 of Reference Example 1 at n, n _Dimethyl 318197 267 !322688 A suspension of decylamine (50 ml) was added with 3-picolylamine (1·72 ml) in an ice bath. After stirring overnight at room temperature, water (25 mL) and saturated aqueous sodium hydrogen carbonate (50 mL) The solid formed was filtered to give the title compound (4.49 g. [Example 1-1 -1] 5-(2 - chaotic-4,5--gas-the present brewylamine is a bit more than p--3-weilic acid (° than bite

5-(2-Ga-4, 5-difluoro-benzylidenylamino)-1H-pyrazole-3-carboxylic acid (pyridine-3-ylmethyl)-decylamine obtained in Example 1-1 To a suspension of methanol (10 ml) was added 4N hydrochloric acid / ethyl acetate (18 ml), and the obtained mixture was concentrated under reduced pressure to a residue of about 5 ml. After filtration, the title compound (yield: 13 crystals) was obtained. [Example 1-1-2]

318197 268 1322688

F

5-(2- gas-4,5-difluoro-benzofuranylamino)-1H-pyrazole-3-carboxylic acid (pyridin-3-ylmercapto)-decylamine given in Example 1-1 (700 g) Into a suspension of methanol (15 ml) was added 4 N hydrochloric acid / ethyl acetate (1.5 ml). The reaction mixture was concentrated under reduced pressure. &lt;EMI ID=9.1&gt;&gt; The reaction mixture was cooled to room temperature. [Example 1-2] -milk-4,5 --milk--stupidylamino)-1Η-° ratio 0--3-thanoic acid (4-methyl-oxazol-5-ylmethyl) )-Y-amine y 偌, · Step 1: 5-Gasyl-4-methyl--. Licking the buttocks;

To a solution of 5-hydroxymercapto-4-methyl-oxazole (1 〇 1 g) in a solution (1 ml) was added triethylamine (1.4 ml). The reaction mixture was cooled with ice-cooled EtOAc (EtOAc:EtOAc) Saturated aqueous sodium hydrogencarbonate was added to the resulting mixture and stirred for 30 minutes. Then, the koji was separated and washed with brine, and dried over anhydrous sodium sulfate, and then reduced to afford the title compound (955 mg) as brown oil. 269 318197 (S) 1322688

Preparation of rabbit 2 amide amine 1 ki-4_f its oxime; H, C

To a solution of 5-chloromethyl-4-methyl-oxazole (955 mg) in dioxane (20 ml) was added 28% aqueous ammonia (1 mL) and the mixture was stirred at room temperature. Overnight. The resulting reaction mixture was concentrated under reduced pressure. &lt;RTI ID=0.0&gt;&gt;&gt; The organic layer was dried over anhydrous sodium sulfate. References: Synth. Commun. 22 (13), 1939-1948, 1992 Step 3: 5-(2-oxo-carbamoylamine 吔n-acid (4-methyl-oxo-5-diyl-methyl) A dazzling eve.

5-(2-Chloro-4,5-dia-benzoylamino)-1Η-pyrazole-3-carboxylic acid imidazolide (2 g) obtained in Step 7 of Reference Example 1 at N, To the suspension of N-dimethylformamide (6 ml), the aminoaminomethyl group + sulfhydryl group (5 〇 2 mg) obtained in the above step 2 was added, and the resulting mixture was dropped overnight at room temperature. Saturated aqueous sodium bicarbonate (30 mL) and then water (30 mL) were then added to the obtained mixture. The solid (4) (iv) formed, the compound (1.11 g), was a white solid. 318197 270 1322688 [Example 1_ 2 -1 a ] 5-(2-milk-4,5~difluoro'-armored amine)-ΐΗ-°υ·. 〇 sitting—3一游酸(4-甲Base-oxazole-5-yl-methyl amide sesquiamine _;

3/2HC1 F

5-(2-chloro-4,5-difluoro-abidocarboxamido) obtained in Example 1-2. Spring-1Η-σ ratio 0 sitting-3-acidic acid (4-mercapto-disgusting saliva- To a suspension of methanol (2 ml) was added 4 mL of hydrochloric acid / ethyl acetate (0. 15 mL). The title compound (53 mg) was obtained as a white solid. [Example l-2-lb] 5-(2-Ga-4, 5-difluoro-mutecarboxylic acid amino)-1Η-° than 嗤-3-decanoic acid (4-methyl-oxazole-5- The base of a certain V-amine to methanesulfonate;

5-(2-Gas-4, 5-difluoro-phenylhydrazinylamino) is 0-position--3-acid (4-mercapto-oxazol-5-ylmethyl)-decylamine (828 mg) A solution of p-toluenesulfonic acid monohydrate (380 mg) in ethanol (1.9 liter) was added to a solution of acetone (8 mL) at 55 ° C. After 2 hours, the reaction mixture was cooled to 271 318 197. After stirring to room temperature for 2 hours, the solid formed was filtered, and the compound (1. 052 g) was white solid. [Example l-2-lc]

5-(2-Gas-4, 5-difluoro-phenylhydrazino)-ih-pyrazole-3-carboxylic acid (4-mercapto-oxazol-5-ylindenyl)-decylamine (1 mg) A solution of L-(+)-tartrate (45 mg) was added to a solution of EtOAc (1 mL). The solid formed was filtered to give the title compound (m. • [Example 2-2] 5-(2-Gas-4, 5-difluoro-abidomethylamino)-lH-pyrazole-3-carboxylic acid (2,4-dimethyl-oxazole) Preparation of 5-5-methyl decylamine saponin; Step 1 · Preparation of 2, 4-dimercaptopurine-5-weiric acid vinegar;

• Η ^ 0 Add acetamidine (17. 01 g) to 2-chloroacetic acid ethyl acetate (22. 91 272 318197 1322688 g) and mix at 28 C for 28 hours. Water (75 ml) and ethanol (7.5 ml) were added to the obtained mixture, and the mixture was evaporated.

H3c

Ethyl 2,4-dimercapto-oxazole-5-carboxylate (7.845 g) was added dropwise to tetrahydrofuran in a suspension of hydrogenated aluminum (1.82 g) in tetrahydrofuran (30 ml) with ice-cooling. 3 〇 ml) solution. After stirring for 1 hour and 3 minutes, water (1.8 ml), 15% aqueous sodium hydroxide (18 ml) and water (5.4 ml) were successively added to the obtained reaction mixture, and the mixture was poured at room temperature. The resulting mixture was dried over anhydrous sodium sulfate. Preparation of 4-dimethyl-oxazole hydrochloride

In a solution of 2' 4-dimercapto-5-hydroxyindolyl-oxazole (5. 539 g) in chloroform (5 〇 升), sulfoximine gas was added dropwise with cooling in an ice bath (4. 2 pens up). After stirring at room temperature for 3 hours, EtOAc EtOAc m. Preparation of mercapto-2,4-dimethylhydrazine-oxazole; 273 318197 1322688

Y is added to triethylethyl 5-cyclodecyl-2,4-dimethyl-oxohydrochloride (6.626 g) in a solution of hydrazine, hydrazine-dimethylformamide (8 ml) Amine (6 ml) was then added to 20% aqueous lithium azide (1 mL) and the mixture was stirred at 60 C for 6 hours. Ethyl acetate (1 ml) was added to the obtained mixture. The obtained mixture was washed with water and brine, and then dried over anhydrous sodium sulfate. Brown oil. Free amidinomethyl-2,4-dimercapto-oxazole di-salt sulphate rate]

Add 3-phenylphosphine (8.47 g) to tetrahydrogen in a solution of 5-azidodecyl-2,4-dimethyl-indole (4.31 g) in tetrahydrofuran (45 ml) A solution of furan (25 ml) followed by 5 Torr. Add water (1.2 liters) and mix overnight. The resulting reaction mixture was concentrated under reduced pressure and then diethyl ether (5 EtOAc) The filtrate was concentrated under reduced pressure. EtOAcjjjjjjjjjj It is yellow solid. Free fluorescein 6 : 5-(2-chloro-4, 5 bis-methyl hydrazone certain amine > ^ 1H pyrazole - 3 _ disc (2, 4- dimethyl-noise methyl amide). 318197 274 1322688

F

Addition of triethylamine to a solution of 5-aminoguanidino-2,4-dimercapto-β- oxazepine dihydrochloride (772 mg) in hydrazine, hydrazine-didecyl decylamine (3 ml) (1. 14 g), and 5-(2- gas-4, 5-difluoro-benzoamitoylamino)-ιη-paraxazole-3-carboxylic acid imidazolide (1.37 g), Stir overnight at room temperature. Water (24 ml) was added to the reaction mixture, and the obtained solid was filtered to afford title compound (1. Step 7: 5-(^-_-4.5-Difluoro-benzhydrylamino)-1^1-pyridin-3-indole (2,4-dimethyl-anthrace-5-armor) Rex rabbits with guanidinium and methotrexate;

5-(2-gas_4,5-difluoro-benzylamino)-1Η_0 to 0 sitting_3-sodium acid (2,4-dimethyl-oxazole-5-ylmethyl) -Acetamine (1. gram) was added i-propanol (6 ml) and heated under reflux. A solution of p-toluic acid (466 mg) in 1-propanol (0.5 ml) was added to the resulting solution, and the mixture was stirred under reflux 30 275 318197 1322688

The title compound (1.36 g) was obtained as colorless crystal. [Example 1-3] Oxy-4, 5-fluorofluoro-benzhydryl-?-amino-amino acid (2,4-methyl-pyridine-3-indolyl)-guanamine; 3-hydroxymethyl-2. 4-dimercaptopyrazine.

To a solution of ethyl 2,4-dimethylpyridine-3-carboxylate (3.0 g) in tetrahydrofuran (30 ml), EtOAc (. After stirring for 2 hours, water (1·2 ml), π% aqueous sodium hydroxide (1.2 ml) and water (3.6 ml) were successively added to the obtained reaction mixture, and the mixture was stirred at room temperature. The organic layer was obtained, evaporated, evaporated, evaporated Preparation of Huangji 2: 3-chloromethyl-2,4-dimethylpyridine;

Add sulfinamide gas to a solution of 3-glycosyl-2,4-dimercaptopyridine (3. gram) in chloroform (30 liters) with ice bath cooling (2.8) ML). After stirring at room temperature for 1 hour and 3 minutes, it was cooled in an ice-bath, and saturated aqueous sodium hydrogen carbonate (60 ml) was added to the obtained mixture. The organic layer was washed with EtOAc EtOAc EtOAc. iAXl 3-# mercaptomethyl-2. 4-dimethylpyridine

Add 20% aqueous lithium azide (5·) to a solution of 3-chloroindolyl-2,4-dimercaptopyridine (3.45 g) in N,N-dimethyl decylamine (15 ml) 5 mM liter), the resulting mixture was stirred at 60 ° C overnight. Ethyl acetate (1 mL) was added to the obtained mixture. The mixture was washed with water and brine, dried over anhydrous sodium sulfate oil. Step 4: Aminoguanidino-2,4-dimethylpyridine f偌:

Oxidation-carbon (613 mg) was added to a solution of 3-azidomethyl-2,4-dimethylpyridine (3.18 g) in ethanol (45 ml). The atm) was stirred under a hydrogen atmosphere for 30 minutes. The title compound (2.53 g) was obtained as a brown oil. Step 5: 5-(2-oxo-4, trifluoro-benzyl hydrazine, a certain VIH-pyrazole-3-oxy acid (2, 4-di-fyridinyl fluorenyl)-醯 之318; 318197 277 1322688

To a solution of the 3-amino-mercapto-2,4-dimercaptopyridine (2.53 g) monomethylguanamine (15 ml) obtained in the step 4, was added to the 5-(2) obtained in Step 1 of Reference Example 1. - Gas-4, 5-difluoro-benzylidenylamino) _1H-pyrazole _3 carboxy carbamide (6 21 g) 'The resulting mixture was stirred overnight at room temperature. Water (5 mL) was added to the obtained mixture, then EtOAc (EtOAc) [Example 1-3-1] -~^ spoon ~~4,5 - gas-brown arylamino)-1Η-η ratio. Sitting on the monument of -3-cyanic acid (2.4-I methyl-pyridin-3-ylindenyl)-nonylamine dihydrochloride

5-(2-Gas-4, 5-difluoro-benzhydrylamino)-1H-pyrazole-3-carboxylic acid (2,4-dimethyl-pyridine-3-) obtained in Example 1-3 To a solution of methanol (1 ml) was added 4N hydrochloric acid / ethyl acetate (EtOAc). Ethyl acetate was added to the obtained reaction mixture. The compounds of Examples 1-4 to 1-167 were prepared in the same manner as in the above Examples 1-1 to 278 318197 1322688 Examples 1-3-1. The structural formulas and NMR data of these compounds are shown in Tables 1 to 24 below. Table 1 Example Molecular Structure Formula NMR 1-1 1H-NMR (300 MHzt DMSO-d6) δ: 13.26 (1H.s). 11.41 (0.1H.s). 11.15 (0.9H.s), 9.18 (0.9H ( Brs). 8.78 (0.1 H. br s). 8.56 (1H. d. J = 1.5 Hz). 8.47 (1H, ddt J = 4.9, 1.5 Hz), 7.96-7.66 (2.9H, m), 7.41-7.30 (2H.m), 6.43 (0.1H, s). 4.47 (2H.d, J = 6.0 Hz). 1-1-1 'H-NMR (400 MHz· DMSOde) δ: 11.22 (1H, s&gt;. 9.34 (1Hf m)f 8.90 (1H. s), 8.84 (1H, m). 8.50 (1H. m). 8.04 (1Ht m), 7.87-7.80 (2H, m) ( 7.24 (1Ht bf s). 4.65 (2H. db s), 8.76 (1H, NMR) Br s), 8.69 (1H, br s). 8.17 (1H, br s), 7.90-7.80 (2H, m), 7.76 (1H, br s), 7.30 (1H, br s), 4.57 (2H, br s). 1-2 Η 'H-NMRi^O MHz, DMSO-de) δ: 13.27 (1H, s)t 11.52 (1H, s), 9.09 (1H, t, J = 5.6 Hz)f 8.19 (1H .s)( 7.89-7.79 (2H, m), 7.32 (1H, s). 4.45 (2H, d. J = 5.6 Hz). 2.14 (3H(s). l-2-la 3/2HCI F NK 8 1. 1H-NMR (400 MHz, DMSO-de) δ: 11.18 (1H, s)f 9.07 (1H, brs), 8.19 (1H. s), 7.87-7.80 (2H, m), 7.24 (1H, s ). 4.45 (2H, dt J = 5.6 Hz). 2.14 (3H, s). 1-2-1b HC-^-VS-OH H h 〇Cl 'H^NMRWOOMHz· DMSOde> δ: 9.05(1H,m&gt;, 8.19(1H,s ) 7.86 &gt; 7.80 (2H, m}· 7.49 (1HtdtJ=8.0Hz) l 7.24(1H.s)t 7A2(\Htd, J=SA»z)t 4.45(2H.d, J=5.6Hz) , 2.29(3H,s), 2.14(3H,s). l-2-lc Η,Ο^ΟΟ, NH 〇Cl 'ΚμΝΜΡΜΟΟΜΗζ^ΜβΟ·^) 9.05(1H_s), 8.72&lt;1H,s&gt;, 7.85 »7.80(2H,m}, 7.25(1H,s), 4_45(2H_d, J=5.6Hz&gt;, 4_31&lt;2H.S&gt;· 2.14(3H.s). 279 318197 1322688

Example molecular structure NMR 1-2-2 HaC—O^f—〇HFH^^TT H,C 'H-mR(400 MHz, DMSO&lt;/e) δ: 11.18 (1H(s). 9.04 (1H. Tf J = 5.2 Hz). 7.87-7.80 (2Ht m)t 7.48 (2H. d, J = 7.8 Hz), 7.25 (1H. s), 7.12 (2Ht d. J = 7.8 Hz), 4.40 (2H, d , J = 5.2 Hz), 2.35 (3Ht s). 2.29 (3H, s). 2.09 (3H. s). 1-3 1H-NMR (400 MHz, DMSO-de) δ: 13.23 (1H, br s) , 11.13 (1H, brs), 9.00 (1H, br s). 8.22 (1H. d. J = 4.8 Hz), 7.85-7.78 (2H, m), 7.34 (1H. brs), 7.06 (1H. dt J = 4.8 Hz), 4.49 (2H, d. J = 4.8 Hz), 2.55 (3H. s), 2.36 (3H, s). 1-3-1 ^NMRi^ MHz, DMSO-de) δ: 11.21 (1H , s), 9.00 (1H, br s), 8.59 (1H, dr J = 6.0 Hz), 7.86-7.80 (2H, m), 7.79 (1H, d, J * 6.0Hz), 7.21 (1H, br s 4.58 (2H, d( J = 4.8 Hz), 2.87 (3H, s), 2.67 (3H. s). 1 - 4 1H-NMR (400 MHz, DMSO-de) δ: 13.12 (1H. br s ), 11.17 (1H( br s), 7.Θ7-7.80 (2H, m), 6.87 (1H, br s), 3.60-3.40 (4H, m), 1.26-1.10 (6H, m). 1-5 Ο^/^ΤΊ^ 1H*NMR (400 MHz, DMSOcy δ: 13.29 (1H, br s). 11.20 (1H, m), 8.60-8.50 (2H.m). 7.89-7.70 (2H, m), 7.31 -7.30 (2H. m), 7.01 (1H. br s), 4.90* 4.68 (2H, m), 3.75-3.35 (2H, m)( 1.18 (3H. m). 1 —6 ' Η ^H-mR(400 MHz, DMSO -de) δ: 13.12 (1H, M), 11.15 (1H, br s), 7.86-7.79 (2H, m)t 6.93 (1Hf br s), 3.71-3.63 (2H, m) ( 3.54 (2H. t) J = 5.2 Hz), 3.28 (6H, m). 1-7 1H-NMR (400 MHz, DMSO-de) δ: 13.11 (1H, m), 11.17 (1H, br s), 7.87-7.80 (2H m), 6.86 (1H. br s), 3.71-3.49 (6H, m). 3.28 (3H, s). 1.15 (3H, m). 1-8 1H-NMR (300 MHzt DMSO-de) δ: 13.23 (1H, s), 11.13 (1H, s). 9.10 (1H. m). 7.85-7.77 (2H, m). 7.41-7.30 (3H, m), 7.22-7.16 (2H. m), 4.49 ( 2H. d. J = 5.7 Hz).. 280 318197

1322688

Example molecular structure NMR 1-9 'H-NMROOO MHz, DMSO-de) δ: 13.24 (1H, s), 11.14 (1H.s). 9.16 (1H.m), 7.83-7.77 (2H, m). 7.42-7.36 (2H, m), 7.17-7.06 (3H, m). 4.46 (2H. d( J = 5.7 Hz). 1 - 10 ^ NMROOO MHz. DMSO-de) δ: 13.21 (1Hf s). 11.11 (1H, s). 9.02 (1H. m), 7.86-7.77 (2H, m), 7.37 (1H, s). 7.25-7.20 (2H, m). 7.13 (1H, m). 7.03 (1H, m ), 4.54 (2H, d. J = 5.7 Hz). 2.66 (6H, s). 1-11 ^-NMRC^O MHzt DMSO-de) δ: 13.11 (1H, br s), 11.16 (1H, br s ), 7.86-7.79 {2H( m), 6.84 (1H, br s), 4.13 (2Hr q, J = 7.2 Hz)f 4.06 (1H, m), 3^9 (1H, m), 2.67-0.85 ( 15H( m), 1.22 (3H, t, J = 7.2 HZ). 1-12 , ο^αητ^ιγν^ ^NMRCAOO MHz. DMSO-de) δ: 13.24 (1H, s)t 11.15 (1H, brs) , 9.10 (1H.t. J = 6.4Hz). 8.12 (1Hf d, J = 2.4 Hz), 7.86-7.79 (2H, m), 7.66 (1H, dd, J = 8.4, 2.4 Hz), 7.31 (1H d. J = 2.4 Hz). 6.80 (1Ht d, J = 8.4 HZ), 4.37 (2H, d, J = 6.4 Hz), 3,83 (3H. S&gt;. 1-13 W-NMR (400 MHz , DMSO&quot;de) δ: 13.22 (1H, br s), 11.14 (1H, brs), .9.01 (1H, brs), 7.86-7.80 (2H. m). 7.37 (1 H. br s), 7.03 (1H, dd. J = 8.4, 7.2 Hz), 6.96 (1 Hf dd, J = 8.4, 1.2 Hz), 6.86 (1H, dd, J = 7.2, 1.2 Hz), 4.45 ( 2H, d. J = 6.0 Hz), 3.80 (3Ht s), 3.77 (3H. s). 1-14 1H-NMR (400 MHz, DMSO-de) δ: 13.18 (1Ht br s). 11.13 (1H, Br s). 8.85 (1H, br s). 7.86-7.80 (2H, m). 7.35 (1H, br s), 7.03 (1H, d, J = 8.4 Hz), 6.56 (1H. d. J = 2.4 Hz). 6.49 (1H. dd, J = 8.4, 2.4 Hz), 4.33 (2H. d. J = 5.6 Hz). 3.Θ1 (3H, s)t 3.74 (3H. s). 1 a 15 1H- NMR (400 MHz, DMSO-de) δ: 8.19 (1H, br s), 7.83-7.76 (2H, m), 7.27 (1H. 1, J = 8.4 Hz). 7.17 (1H. br s), 6.68 ( 2H, d. J = 8.4 Hz), 4.43 (2H, d. J = 4.4 Hz). 3.79 (6H. s). 281 318197 1322688 Table 4 Example Molecular Structure Formula NMR 1 —16 H ^-NMRtAOO MHz, OMSO- De) δ: 13.24 (1H, br s), 11.15 (1H, br s). 9.10 (1H, m) ( 7.86-7.79 (2H, m), 7.36 (1H, br s), 6.48 (2H, d. J = 2.4 Hz), 6.39 (1H, t, J = 2.4 Hz), 4.37 (2H. d, J = 6.4 Hz). 372 (6Hf s). 1-17 ^-NMRC^O MHz, DMSOd6) δ: 13.23 (1Ht br s), 11.15 {1H, br$)( 9,06 (1H, brs), 7.86-7.80 (2H, m). 7.34 (1Ht br s), 6.94 ( 1H, d, J = 2.0 Hz), 6.90 (1H, d, J = 8.0 Hz), 6.83 (1H( dd, J = 8.0, 2.0 Hz) t 4.37 (2H, d. J = 6.0 Hz)f 3. , 74 (3H, s). 3.72 (3H, s). 1-18 1H-NMR (400 MHzt DMSO-de) δ: 13.27 (1H, s), 11.16 (1H, m). 9.18 (1HP m), 7.86-7.79 (2H, m), 7.37-7.31 (2H, m), 7.23-7.16 (2H, m), 4.52 (2H, d, J = 5.6 Hz). 1-1Θ 1H-NMR (400 MHz, DMSOdB&gt ; δ: 13.25 (1H. br s), 11.16 (1H, br s), 9.10 (1H. br s), 7.86-7.80 (2H, m), 7.43 (1H, dd, J = 15.6, 8.4 Hz). 7.35 (1H, brs), 7.23 (1H, m), 7.08 (1Hf m). 4,45 (2H. dt J = 5.6 Hz). 1-20 c^Vr^ 1H-NMR (400 MHz (DMSO-de δ: 13.28 (1H( br s), 11.17 (1Ht br s), 9.15 (1Ht brs), 7.87-7.80 (2H, m), 7.38 (1H, br s). 7.27 (1Hf m), 7.20-7.15 (2H, m), 4.47 (2H. d. J = 5.6 Hz). 1-21 ^H-Um(AOO MHz, DMSO-de) 5:13.22 (1H, br s), 11.13 (1H, br s) , 8.98 (1H, br s), 7.85-7.78 (2H, m). 7.41 (1H, m), 7.31 (1Hf br s), 7.14-7.05 (2H, m), 4.45 (2H, d, J = 5.2 Hz). 1-22 χτΛγν^ MHz, DMSO-de) δ: 13.22 (1Ht br s). 11.21 (1H. brs), 9.13 {1H, brs)t 7.86-7.80 (2H, m). 7.43-7.34 ( 2H, m), 7.28 (1H, br s), 7.17 (1H. m), 4.42 (2H. d. J = 5.6 Hz). 1-23 'xpnrSrV^ MHz. DMSO-de) δ: 13.28 (1H, br s ), 11.19 (1H. br s), 9.19 (1H. brs), 7.87-7.80 (2H, m). 7.36 (1H. br s). 7.12 (1H, m), 7.09-7.02 (2H. m), 4.46 (2H, df J = 6.0 Hz). 282 318197 1322688

Example Molecular Structure NMR 1-24 'H-NMR (400 Mhte·DMSO&quot;&lt;/e&gt; δ: 13.26 (1Η· s), 11.17 (1H, brs)f 8.95 (1H, br s), 8.04 (1H , dd, J = 5.2, 2.0 Hz), 7.87-7.80 (2H, m), 7.51 (1H, d. J = 6.8 Hz), 7.37 (1H. m), 6.92 (1H. dd. J = 6.8, 5.2 Hz). 5.32 (1H, m), 4.35 (2H( d, J = 5.6 Hz), 1.31 (6H. d. J = 6.4 Hz). 1-25 'H«NMR(400 MHz, DMSO&gt;de) δ : 13.29 (1H. br s). 11.20 (1H, s) ( 9.13 (1H, brs), 8.01 (1H, dd ( J = 5.2, 1.6 Hz), 7.87-7.81 (2H. m). 7.75 (1H ( Dd, J = 7.2, 1.6 Hz). 7.44-7.40 (2H, m), 7.26 (1Ht m), 7.20 (1H. m). 7.16-7.11 (3H. m). 4.55 (2H. d. J = 5.6 Hz). 1-26 'H-NMRiAOO MHz, DMSO-de) δ: 13.23 (1H. s). 11.14 (1H, s) ( 9.11 (1H, d, J = 5.6 Hz), 8.48 (1H, m) , 7.94 (1H, m)( 7.86-7.78 (2H, m), 7.35 (1H, d, J = 1.6 Hz), 4.59 (2H, d. J = 5.6 Hz). 1-27 DMSO~de) δ: 13.30 (1H, br s), 11.19 (1H, br s), 9.22 (1H, br s). 7.87-7.81 (2H. m), 7.74 (1H. d, J = 8.0 Hz), 7.68 (1Ht dd, J = 7.2, 72 Hz), 7.55-7.48 (2H# m)t 7.42 (1H, br s), 4.63 (2H, d, J = 5.2 H2). 1-28 ^Sonr^t^V ^ W-NMR (400 MHz, DMSO^e) δ: 13.28 &lt;1H, br s). 11.18 (1H, br s), 9.23 (1H, br s), 7.87-7.80 (2H.m), 7.67- 7.57 (4H.m). 7.36 (1H, br s), 4.53 (2H, d. J = 6.0Hz), 1-29 1H-NMR (400 MHz, DMSO-de) δ: 13.29 (1H, s) 11.18 (1H, s), 9.25 (1Ht t, J = 5.6 Hz), 7.87-7.80 (2H, m), 7.71 (2H, d, J = 8.0 Hz), 7.54 (2H, d, J = 8.0 Hz) , 7,38 (1H, m), 4.53 (2H, d, J = 5.6 Hz). 1-30 'H-NMRC^ MHz. DliASO&lt;f6) δ: 13.21 (1H. br s), 11.15 (1H, Brs), 9.07 (1H. br s), 7.86-7.80 (2H, m). 7.35 (2H, d. J »= 8.4 Hz), 7.34 (1H, br δ), 7.24 (2H, d. J = 8.4 Hz), 4.40 (2H.d, J = 6.0 Hz). 1.26 (9H, s). 1-31 'H*NMR (400 MHz, DMSCWe) δ: 13.24 (1H, s), 11.15 (1H. br s ) ( 9.08 (1H. t. J = 5.2 Hz), 8.09 (1H. d. J = 2.4 Hz). 7.86-7.79 (2H. m). 7.63 (1H, dd. J = 8.4, 2.4 Hz). 7.32 (1H, s). 6.71 (1H, d. J = 8.4 Hz). 5.21 (1Ht m), 4.35 (2H, d, J = 5.2 Hz), 1.27 (6H. d, J = 6.0Hz). 283 318197

1322688

Example Molecular Structure NMR 1-32 Η 1H-NMR (400 MHz. DMSO-de) δ: 13.27 (1H. s). 11.17 (1H, s). 9.06 (1H, t ( J = 5.6 Hz). 8.11 ( 1Ht dd, J = 5.2r 2.0 Hz). 7.86-7.79 (2H, m), 7.66 (1H, d, J = 6.4 Hz), 7.38 (1H, d. J = 2.0 Hz), 7.12 (1H. dd, J = 6.4, 5.2 Hz). 5.05 (2Ht q. J = 9.2 Hz), 4.42 (2H, d, J = 5.6 Hz) · 1—33 ^NMROOO MHz, DMSO-de) 6:11.19 (1H. br s )t 11.13 (1H, br s), 9.16 (1H, brs), 8.55 (1H. br s), 7.92-7.71 (4H. m). 7.40 (2H. d. J = 8.1 Hz), 7.28 (1H, Br s). 4.49 (2H, d. J = 5.5 Hz). 3.48 (2H, d. J = 5.9 Hz). 2.82 (2H, dr J = 6.6 Hz), 2.49 (6H. s). 1-34 Η ^NMRi^ MHz, DMSO-de) 6:13.22 (1Hf br s), 11.15 (1H. br s). 9.08 (1H. brs), 7.86-7.80 (2Hf m), 7.33 (1H, br s). 7.22 (2Ht d. J = 7.6 Hz), 7.17 (2H, d, J = 7.6 Hz). 4.40 (2H. d, J = 6.0 Hz). 2.57 (2H· q· J = 7.6 Hz), 1.16 (3H· t, J : 7.6 Hz&gt;. 1-35 1H-NMR (400 MHz, DMSO-de) δ: 13.22 (1H. br s), 11.14 (1H, br s). 9.09 (1H. br s), 7.86- 7.80 (2H(m), 7.34 (1 Hf br s), 7.24 (2H, d, J = 8.4 Hz), 7.20 (2H. d, J = 8.4 Hz), 4 .40 (2H, d, J = 6.0 Hz). 2.86 (1H, m), 1.18 (6H. d. J = 6.8 Hz). 1-36 'H-NMFU^ MHz· DMSOde> δ: 13.22《1H, Br s). 11.13 (1H, br s). 8.89 (1H. br s), 7.85-778 (2H# m), 7.44-7.34 (3H, m), 7.25 (1H, m). 4.57 (2H, d (J = 4.0 Hz). 1-37 1H-NMR (400 MHz, DMSO-de) δ: 11.19 (1H, s), 9.13 (1H, br s), 8.14 (1H, 8), 7.87-7.79 (2H (m), 7.74 (1H, m), 7.23 (1H, s), 6.86 (1H. m), 4.38 (2H( d, J = 5.6 Hz), 4.30 (2H, m), 1.31 (3H, t, J = 7.2 Hz). 1-38 Η 1H-NMR (400 MHz, DMSO-de) δ: 13.23 (1H, br S), 11.16 (1H, s) ( 9.14 (1H, br s), 9.06 (1H, d, J = 2Ό Hz), 7.87-7.Θ0 (2Ht m), 7,47 (1H, s), 7.34 (1H, br s)· 4.58 &lt;2H_ d· J = 6.0 Hz&gt;_ Ί-3Θ ^H-mRiAOQ MHz. DMSO-de) δ: 11.18 (1H. s), 9.13 (1H. brs) ( 8.16 (1H, d, J = 2.4 Hz). 7.87-7.80 (2H, m), 7.77 (1H Dd, J = 8.4. 2.4 Hz), 7.24 (1H, s), 6.97 (1H, d( J = 8.4 Hz), 4.98 (2H. q. J = 8.8 Hz). 4.41 (2H, d, J = 6.0 Hz). 284 318197 1322688 Table Example Molecular Structure NMR 1-40 ^H-HMRiAOO MHz, DMSOde) δ: 13.15 (1H, br s). 11.12 (1H. brs). 8.61 (1H, brs)t 7.85-7.77 (2H, m), 7.32 (1H, br s), 7.10 (1H. m), 7.03 (2Ht d. J = 7.2 Hz). 4.47 (2H. d, J = 4.4 Hz), 2.35 (6H. s). 1—41 ΛΗΉΜηίΛ00 MHz, DMSO-de) δ: 11.21 (1H. br s). 9.30 (2H, br s), 8.83 (1H, m), 8.70 (1H. m), 7.94 {1H. m), 7.87-7.81 (2H. m), 7.71 (1H. m). 7.31 (1H. s), 4.65 (2H. d, J = 6.0 Hz). 1-42 W- NMRWOO MHz. DMSO»de} δ: 11.28 (1H, br s). 9.55 (1Ht br s), 7.89-7.82 (2Ht m), 7.79-7.77 (2H.m), 7.55-7.53 (2H? m), 7.34 (1H, br s), 4.94 (2H.m). 1—43 \〇nrVr^ 1H-NMR (300MHz.DMSO-(/e) 6 :13.25 (1H,br s), 11.16 (1H. brs) 9.18 (1H. brs), 8.90 (1H, t( J =5.9 Hz). 7.94-7.75 (4H, m). 7.38 (2H, d. J = 8.4 Hz). 7.27 (1H, br s). 4.50 (2H, df J = 5.9 Hz), 4.02 (2H, dt J = 5.9 Hz), 3.65 (3Hr s). 1-44 0 1H-NMR (300MHz, DMSO-de) &lt;S: 13.19 (1 H, Br s), 1110 (1H. br s), 9.13 (1H, br s), 8.46 (1H, t, J = 5.5 Hz), 8.22 (1H, d, J = 0.7 Hz), 7.80 (2H. d, J = 8.1 Hz), 7.74-7.64 (2H, m), 7.38 (2H, d, J = 8.1 Hz). 4.50 (2H, d, J = 5.9 Hz), 3.62 (3H, s), 3.51 (2H, q( J = 6.5 Hz), 2.59 (2H, t. J *= 7.0 Hz). 1-45 Η 1H-NMR (400 MHz, DMSO-de) 6: 11.18 (1H. s). 9.12 (1Hf br s), 7.87- 7.80 (2H, m), 7.29 (1H. s), 7.27 (1H. br s), 4.49 (2H, d, J = 4.0 Hz). 2.67 (3Ht brs). 1-46 'H-NMRi^ MHz, DMSO-de) δ: 13.25 (1H, s), 11.15 (1H. s) ( 8.91 (1ΗΛ J = 5.2 Hz). 7.86-7.79 (2Ht m), 7.31 (1H. m). 4.19-4.18 (2H, m), 2.40 (3H.s).2.22 (3H. s). 1-47 0 1H-NMR (300MHz.CD3OD)) δ: 7.78(2H,d,J =8.4 Hz), 7.55 (4H.m) , 7.45 (2H. d, J = 8.4 Hz). 4.60 (2H, br s), 4.13 (4H, t, J = 4.2Hz) t 3.45 (2H. t, J = 9.6 Hz). 2.84 (4H , t , J = 4.2 Hz). 2.79 (2H( t. J = 4.8 Hz), 1.94 (6H, s).

285 318197 1322688 table

Example molecular structure NMR 1-48 0 'H-NMROOO MHz, DMSO-de) d: 13.27 (1H, br s)p 11.17 (1Hf br s), 9.20 (1H, br s), 8.40 (1H. br s 7.87 (3H, m). 7.35 (2H. d. J = 9.9 Hz). 4.73 (1H, t. J = 8.1 Hz). 4.50 (2H. d. J = 6.2 Hz). 3.55-3.47 (2H m)f 3.34-3.30 (2H.m). 1-49 0 'H-NMROOOMHz, DMSO-de) 6: 9.02 (1H, br s). 8.29 (1H, br s), 7.85-7.64 (4H. m). 7.38 (2H, d, J = 8.4 Hz), 7.09 (1H. br s). 4.46 (2H, d, J = 6.2 Hz). 4.04 (2H, t, J = 4.2Hz), 3.32 (2H , m), 2.76-2.55 (6H.rn). 1.96 PH. s). 1-50 1H-NMR (400 MHz. DMSO-de) δ: 11.29 (1H, br s)t 9*53 (1H, br s), 7*95 (1H. m), 7.89-7.78 (3H, m). 7.63-7.57 (2H(m), 7.34 (1H, br s), 5.00 (2H, m). 4.04 (3H, s Preparation 1-51 Η 1H-NMR (400 MHz. DMSO-de) δ: 11.23 (1Hf s), 9.49 (1H. br s), 7.88-7.82 (2H, m), 7.76 (1H, m), 7.66 (1H, m), 7.29 (1H, s), 4.73 (2H. d, J = 5.6 Hz). 1-52 'H-mRiAOO MHz, DMSO-de) δ: 11 29 (1H, br s). 9.53 (1H, br s), 8.06 (1H, d, J = 7.2 Hz) ( 7.97 (1H, d, J = 7.2 Hz), 7.87-7.83 (2HP m), 7.51 (1H, t, J = 7, 2 Hz). 7.42 (1H, t, J = 7.2 Hz), 7.31 (1H, s).4.85(2H,d·J = 6*0Hz). 1-53 ^NMRi^O MHz, DMSO-de) δ: 11.15 (1H. s)t 9.02 (1H, Br s)· 7_87-7·80 (2H, m). 727 (1H, br s), 4.40 (2H( m), 2.59 (3H, br s), 2.43 (3H, br s). 1-54 h -NMRMOO MHz, DMSO^e) &amp; 11.21 (1H. br s). 9.09 (1Ht br s), 7.88-7.81 (2H, m). 7.27 (1Hf m). 671 (1H, br s). 4.38 ( 2H, m). 3.74 (4H, m), 3.53 (4H, m). 286 318197

1322688

EXAMPLES Molecular Structures NMR 1-55 HjC H 1H-NMR (400 MHz, DMSO-de) δ: 13.18 (1H. s). 11.12 (1H. s), 8.72 (1H.m), 7.86-7.78 (2H. m), 7.30 (1H, s), 4.16 (2H, d. J = 5.6 Hz), 3.61 (3H. s), 2.22(3H, s)( 2.11 (3H. s). 1-56 'H-NMROOO MHz, DMSO-dt) 5:11.22 (1H, s), 9.16 (1H.t, J = 5.8 Hz). 7.88-7.80 (2Hf m), 7.67 (1H, d. J = 7.9 Hz), 7.31-^ .26 (2H.m). 4.45 (2H, d. J = 5.6 Hz). 2.44 (3H, s). 1-57 1H-NMR (400 MHz, DMSO-de) δ: 11.22 (1H. s). 9.12 (1H, m)( 7.88-7.81 (2H, m), 7.26 (1Ht s), 6.69 (1H. br s), 4.40 (2Hf m), 3.20 (6H, s). 1-58 Η 1H-NMR (400 MHz, DMSO-de) δ: 13.21 (1H, br s). 11.13 (1H. br s), 8.90 (1H, br s), 7.86-7.79 (2H, m), 7.35 (1H, brs), 6.67 (1H, m), 5.97 (1Hf m), 5.90 (1H, m), 4.40 (2H, d, J = S2 Hz), 3.58 (3H. s). 1-59 'H-NMRt^O MHz, DMSO-tfe) δ: 11.25 (1H, s), 9.28 (1H, br s). 8.59 (1H, d. J = 6.8 Hz), 7.88-7.81 (2H, m), 7.65 (1H, d, J = 6.8 Hz), 7.24 (1H, br s), 4.73 (2H, d, J = 4.4 Hz), 4.15 (3H, 8). 3.91 (3H. s). 1-60 Test 'H-NMRC^ MHz, OMSO-de) 5:11.25 (1H, s). 9.47 (1H, br s), 7.88-7.81 (2H, m), 7.59 (1H, m), 7.27 (1H, s). 4.66 (2H, m). 1.32 (9H, s). 1-61 η 'H-NMRC^ MHz, DMSO-de) δ: 13.29 (1H, s)t 11.16 (1H, s)t 9.18 (1H, brs), 7.93 (2H, d, J = 7.2 Hz), 7.86-7.80 ( (2H, m).

1322688 Table 10

Example Molecular Structure NMR 1-62 Η 1H-NMR (300 MHz, DMSO-de) δ: 9.05 (1 Η. br s), 8.43 {1H. d. J = 4.8 Hz), 7.86-7.70 (2H.m) , 7.47 (1H. t. J = 6.1 Hz), 7.23-7.05 (3H, m), 4.51 (2H, d. J = 5.9 Hz), 4.12 (2H. d. J = 6.2 Hz). 1.34 (9Ht s 1-63 'H^MRi-lOO MHz, DMSO-de) δ: 11.22 (1H, s) ( 9.23 (1H. br s). 7.87-7.81/(2Hi m). 7.18 (1H. br s) , 4.38 (2H. d. J = 6.0 Hz), 3.72 (4Ht m), 3.53 (4H. m). 2.30 (3H. s). 1 —64 3/2HCI 1/2ΗΖ0 ί 1H-NMR (400 MHz, DMSO-de) δ: 11.26 (1H, br s), 9.37 (1H, t. J = 5.8 Hz), 8.92 (1H, br s), 8.86 (1H( d ( J = 5.6 Hz), 8.54 (1H. Dt J = 8.3 Hz). 8.07 (1H. dd. J = 8.1, 5.8 Hz), 7.90-7.81 (2H, m), 7.26 (1H, br s). 4.66 (2H, d ( J = 5.6 Hz). 1-65 NMR (300 MHz. DMSO-&lt;ie) δ: 13.22 (1H, s), 11.12 (1H, s). 9.00 (1H, br t, J = 4.9 Hz), 7.85-7.75 (2H. m), 7.32 (1Hf s), 7.01 (1H, d. J = 7.2 Hz), 6.95 (1H, t J = 7.5 Hz). 6.61 (1H, d, J = 7.9 Hz)f 6.50 (1H, t. J = 7.3 Hz), 5.10 (2H. s), 4.26 (2H, d( J = 6.0 Hz). 1-66 ^-NMR (300 MHz, DMSO-de) δ: 13.21 (1HP s ), 11.13(1H( s), 8.95 (1H, t, J = 5.8 Hz), 7.88-776 (2H, m), 7.39 (1H. d. J = 1.5 Hz), 7.29-7.15 (2H, m) , 7.00 (1H, d, J = 7.9 Hz), 6.92 (1H, t· J = 7.2 Hz), 4.42 (2H. d, J = 5.7 Hz). 3.84 (3H? d. J = 6.4 Hz). 1 -67 'H-NMR (300 MHz, DMSO-de) δ: 13.22 (1Ht br s). 11.14 (1H# brs), 9.11 (1H( brs). 7.87-7.77 (2H. m). 7.35 (1H. Br s). 7.25 (1H, dd. J = 10.9, 5.3 Hz). 6.91-6.87 (2Hf m), 6.85^.79 (1H. m). 4.42 (2H( d, J = 6.0 Hz), 3.74 ( 3Ht s). 1-68 1H^MR (300 MH2, DMSO-de) δ: 13.20 (1H, s). 11.12 (1H, s), 9.06 (1H, tf J = 6.0 Hz), 7.86-7.77 (2H m). 7.33 (1H, d, J = 1.9 Hz), 7.25 (2H, d, J = 9.0 Hz). 6.90 (2H, d, J = 9.4 Hz), 4.37 (2H( d. J = 9.0 Hz) ), 3.73 (3H, s). 1-69 'H-NMR (300 MHz, DMSO-de) δ: 12.43 (1H. br s). 11.20 (1H. br s), 9.04 (1H. t. J = 5.8 Hz), 7.87-7.78 (2H, m)p 72S (1H, s)t 7.20 (2H, d, J = 7.9 Hz), 7.14 (2H, d, J = 7.5 Hz), 4.39 (2H. d, J = 6.0 Hz), 2.27 (3H. s). 288 318197 1322688 Table 11 Example Molecular Structure NMR 1-70 'H*NMR (300 MHz, DMSO-de) δ: 13.23 (1H, s), 11.14 (1H. s), 9.13 (1H. s). 7.86-7.78 (2Hf m), 7.39-7.33 (3H. m). 7.17-7.14 (2H, m), 4.42 (2H. d, J=6.0 Hz 1—71 eij〇rA^V^ ^-NMR (300 MHz, DMSO-de) δ: 13.23 (1H. br s). 11.15 (1H, br s), 9.14 (1H, br s), 7.86- 7.79 (2H.m). 7.40 (2H, d, J = 7.2 Hz), 7.34 (2H, d, J = 8.7 Hz) ( 4.43 (3Hf d, J = 6.0 Hz). 1-72 ^jQnrVV^ ^NMR (300 MHz, DMSO-de) δ: 13.26 (1H, s), 11.15 (1H, s), 9.22 (1H, t. J = 5.8 Hz), 7.94 (2H, d, J = 8.3 Hz). 7.86- 7.78 (2H, m), 7.46 (2H, d, J = 8.3 Hz). 7.37 (1H, s), 4.53 (2H, d, J = 5.7 Hz). 3.85 (3H. s). 1-73 'H -NMR (300 MHz, DMSO-de) δ: 13.05 (2H, br 8), 11.16 (1H, s). 9.16 (1H, t, J = 5.7 Hz). 7.90 (2H, d, J = 8.3 Hz) , 7.84-7.77 (2H, m), 7.41 (2H. d, J = 8.3 Hz), 7.27 (1H, s), 4.50 (2H, d, J = 6.0 Hz). 1-74 'H-NMR (300 MHz, DMSO-de) δ: 13.38 (0.8H, brs), 13.11 &lt;0.2H, brs&gt;. 11.43 (0.2H, brs), 11.11 (0.8H, s), 7.92-7.66 (2H, m), 7.45-7.17 (10Hf m), 6.80 (0.8H, br s), 6.51 (0.2H, br s), 5.05-4.42 (4H, m). 1-75 ^NMR (300 MHz, DMSO-de) δ: 13.44 (1H, 8). 11.20 (1H. s), 9.91 (1H, d, J = 7.9 Hz), 7.93-7.76 (2H.m), 7.57-7.38 (6H, m), 6.40 (1H; d. J = 7.9 Hz). 1 -76 crr\r\4^ 'H-NMR (300 MHz. DMSO-rfe) 6:13.13 (1H. s). 11.10 (1H. s)t 8.51 (1Hf t, J = 5.8 Hz), 7.86-7.77 (2H, m), 7.31 (1Ht d, J = 2.3 Hz), 3.08 (2H( t( J = 6.4 Hz). 178-1.43 (6H( m), 1.29-1.05 (3H. m). 1.02^) .81 (2H, m). 1-77 1H-NMR (300 MHz, DMSO-de) δ: 13.70 (1H, s), 11.26 (1H, s). 7.87-7.79 (2H, m), 7.16 (1H , s), 7.09 (2H, t. J = 8.5 Hz), 6.65 (2H, d, J = 7.9 Hz), 6.55 (1H, t. J = 7.2 Hz), 5.79 (1H, tt J = 6.0 Hz) , 4·39 (2H·t·J = 5_7 Hz&gt;· 3.42 (2H. dd. J = 5.7, 2.8 Hz). 289 318197 5 1322688 Table 12

EXAMPLES Molecular Structures NMR 1-78 3 Η 'H-NMR (300 MHz. DMSO-c/e) δ: 13.10 (1H. s)t 11.13 (1H.s). 7.84-7.76 (2H.m). 6.86 (1H, s). 4.13-4.10 (1H, m), 3.12-276 (3H, m), 1.87-1.00 (10H.m). 1-79 Η ^-NMR (300 MHz, DMSOd^) δ: 13 ,12 (1H. s), 11.09(1H, s)t 8.34 (1H( d, J = 7.9 Hz). 7.86-7.77 (2H, m). 7.34 (1H. d. J = 2.3 Hz), 3.80- 3.64 (1H, m), 1.88-1.53 (5H, m). 1.40-1.03 (5H, m). 1-80 [^Λ5Λί4ΪΓ&quot; 1H-NMR (300 MHz, DMSO-cfe) δ: 13.10 (1H, s ), 11.14 (1H. S), 7.88-7.78 (2H, m). 6.84 (1H. s). 4.02 (1Ht s), 1.86-1.47 (8H, m), 1.38-1.02 (7H, m). 1 -81 1H-NMR (300 MHz, DMSCWe) 6:13.13 (1H, s), 11.11 (1H. s). 7.93-776 (2H.m), 6.88 (1H, s), 5.98-5.79 (1H(m 5.26-5.00 (2H, m), 4.25-3.86 (3H, m) (1.80-1.58 (7H, m), 1.38-1.03 (3H, m). 1 - 82 1H-NMR (300 MHz, DMSOde) δ: 13.23 (1H, br s), 11.19 (1H, br s)f 8.51 (1H( br s), 7.95-7.64 (3H, m), 7.45-7.12 (2HP m), 6.96 (0.4H, br s ) ( 6.66 (0.3Ht br s), 6.40 (O^H. br s), 5.18 (0.1H, br s), 4.91-4.51 (2H, m), 4.39-4.07 (1H. m). 1.90* 0.89 (1 0H,m&gt;· 1 -83 'H-NMR (300 MHz, OMSO-de) δ: 13.12 (1H. br s). 11.19 (1H. brs), 7.88-7.76 (2H, m), 6.81 (1H, Br s), 4.35-3.83 (1H. m). 3.16-2.72 (7H. m). 2.20 (3H, brs). 2.06-1.45 (4H,m). 1-84 ocr/^r^ Η ^-NMR (300 MHz, DMSO-d,) δ: 11.15 (1H, s), 9.02 (1H, t, J 5.7 Hz), 7.87-7.78 (2H, m), 7.26 (1H, s), 6.89-6.77 (4H , m)( 5.98 (2H, s). 4.34 (2H, d, J = 6.0 Hz). 1-85 οςΛγν? Hj(/ 1H-NMR (300 MHz, DMSO-de) 6: 13.26 (1H, s) , 11.18 (1H, s), 7.97-7.68 (2H.m), 7.50-7.17 (5H, m), 6.97 (0.4H, br s). 6.76 (0^5H. br s). 6.43 (0.15H, Br s), 5.10 (0.1H, s)f 4.93-4.59 (2H. m), 3.72-3.17 (2H, m), 1.68-1.42 (2Ht m), 1.39-1.13 (2H, m), 0.94-0.75 (3H, m). 290 318197 5 1322688 Table 13

Example molecular structure NMR 1-86 HO^J ^-NMR (300 MHz, DMSO-d6) δ: 11.33 (1H, s). 9.37 (2Ht br s) ( 7.89-7.78 (2Ht m), 7.65-7.51 ( (2H, m). 7.47-7.41 (3H. 1.92-1.71 (4Htm). 1-87 1H-NMR (300 MHz, DMSO-de) δ: 13.12 (1Hf s)t 11.15 (1H. s). 7.97-7.73 (2H. m). 6.88 (1H s). 3.76-3.15 (4H, m). 1.69-144 (2H, m). 1.4M.05 (5H, m). 0.90 (3H, t, J = 8.0 Hz). 1-88 CH 'H -NMR (300 MHz. OMSO-de) δ: 13.09 (1Ht s), 11.14 (1H. s), 7.9S-7.74 (2H, m), 6.83 (1H, s), 4.39-3.85 (1H, m) , 3.42-3.13 (2H, m)f 1.86-1.45 (9H, m). 1.39-1.04 (3H, m), 0.87 (3H, t, J * 6.9 Hz). 1-89 cV4rV^r 〆H 1H- NMR (300 MHz, DMSO-de) δ: 13.08 (1H, s), 11.14 (1H, s), 7.95-7.75 (2H, m), 6.84 (1H, s), 4.23-3.85 (1H, m), 3.48-3.19 (2H, m), 1.M-1.46 (9H.m). 1.41-1.04 (5H, m), 0.91 (3Hf t, J = 72 Hz). 1-90 , / h 1H-NWIR ( 300 MHz. DMSOd〇) 5:13.05 (1H, br s) ( 11.39 (OH, s), 11.14 (1H, s)f 7.96-7.74 (2H, m), 6.88 (1H, br s), 6.32 (OH , br s). 4.47-4 .29 (OH, m)( 4.10-3.91 (1H, m), 3.67-3.40 (4H, m), 3.32-3.24 (3H, m), 1.89-1.43 (7H, m), 1.41-0.99 (3H, m). 1-91 ^MR (300 MHz. DMSO-de) δ: 13.26 (1H, s), 8.59 (1H, s) ( 8.52-8.47 (2H, m). 8.02-7.57 (3H, m). 7.46-7.24 (1H, m), 6.93 (0.5H, br s), 6.41 (0.2H, br s). 5.13 (0.1H, br s). 4.99-4.45 (2H. m). 4.38-4.01 (1H , m), 1.8S-1.39 (7H, m), 1.34-0.95 {3H, m). 1—92 0 H ^-NMR (300 MHz. DMSOd^) δ: 13.49 (1H. br s), 11.55 ( Br s), 11.26 (br s). 9.98 (br s). 9.60 (br s). 8.31 (br s). 7.90 (2H, s), 7.48-7.04 (4H, m). 6.56 (br s). 3.94-3.70 (4H. m). 2.92-2.82 (4H, m). 291 318197

1322688 Table 14

Example molecular structure NMR 1-93 Η3 (Γ 1H-NMR (300 MHz. DMSO-de) δ: 13.11 (0.8H. br s), 12.97 (0.2Ht br s). 11.37 (0.2H, s). 11.15 (0.8H, s). 7.95-7.76 (2H.m). 6.91-6.85 (0.8H, m), 6.34-6.31 (0.2H, m), 3.75-3.33 (4H, m), 1.68-1.46 (4H m), 1.40 (1H, s) (0.1H, s). 11.13 (0.9Ht s). 7.96-7.68 (2Hf m), 6.94 (0.9H. br s). 6.38 (0.1 H. br s). 3.84-3.58 (4H. m), 3.59 -3.48 (4H, m), 3.27 (6H, s). 1-95 1H-NMR (300 MHz (DMSO-de) δ: 13.09 (1H, br s). 11.38 (0.2H, br s)t 11.14 ( 0.ΘΗ, br s). 7.98-7.73 (2H, m), 6.90 (0.8H, br s), 6.36 (0.2H, br s), 3.98-3.35 (6H, m), 3.29 (3H. s) , 1.72-1.51 (2H, m), 0.88 (3H, t J * 7.3 Hz). 1-96 HatT 1H-NMR (300 MHz, DMSO-de) δ: 13.12 (0.8H, br s), 12.98 (0.2 H, br s). 11.38 (0.2H, br s). 11.15 (0.8H, br s), 7.97-774 (2H. m). 6.86 (Ο βΗ. br s). 6.33 (02H, br s). 4.64 (OH. br s), 4.24 (1H. br s), 4.02-3.84 (2H, m), 3.66-3.12 (4H, m), 2.05-1.79 (2H. m). 1.72*1.47 (4 H, m)f 1.42-1.18 (2H, m)t 0.91 (3H, t, J = 7.3 Hz). 1-97 ϊ:^Λγν^ 'H-NMR (300 MHz, OMSO-de) δ: 13.12 ( 1H, br s), 11.40 (0.2H. s) ( 11.14 (0.8H, brs). 7.99-772 (2H· πή_ 6. (0.8H, br s&gt;·6_36 (0.2H, br s), 4.71 (0.2H, m), 4.20 (0.8H, m). 4.01-3.84 (2Hf m), 3.71-3.10 (9Ht m), 2.09-1.72 (2H. m), 1.7M.54 (2H, m). 1-98 h3c^° 1H-NMR (300 MHz, DMSO-de) & 13.11 (1H, br s). 11.15 (1H, brs). 7.86-7.82 (2H, m), 6.87 (0.8H, br s ), 6.33 (0.2H, br s). 4.43-4.39 (1H( m). 3.52-3.49 (4H, m). 3.27 (3H, s). 1.75-1.57 (8H. m). 1-99 oy^ yV^ N-Jj 〇Cl 'H-NMR (300 MHz, OMSO-de) δ: 13.10 (1Ht s). 11.14 (1H, s). 7.95-7.72 (2H, m), 6.85 (1H, br s) t 4.43-3.B4 (1H. m), 3.64-3.26 (4H, m). 3.22 (3H, s). 1.90-1.45 (9H. m). 1.40-1.00 (3H. m). 292 318197 1322688 15

Example molecular structure NMR 1-100 'H-NMR (300 MHz, DMSOtfe) δ: 13.09 (1H. s s). 11.12 (1H. s). 7.93-7.73 (2H, m), 6.85 (1H, br s ), 4.09-3.86 (1H. m). 3.67*3.29 (6H, m). 1.83-1.48 (7H, m). 1.38-0.97 (6H. m). 1-101 Η3°γ°^ Μ 0 Cl ch3 1H-NMR (300 MHz, DMSO-de) 6:13.11 (1H. br s), 11.14 (1H, s), 7.94-7.75 (2H.m). 6.86 (1H, br s). 4.01-3.98 (1Ht m), 3.74-3.34 (5H, m), 1.87-1.45 (7H.m). 1.36-1.01 (QH.m). 1-102 H ^-NMR (300 MHz, DMSO-de) δ: 13.09 (1H , br s). 11.12 (1Ht s). 7.87-7.80 (2H, m), 6.85 (1H. br s), 4.09-3.88 (1H, m), 3.65-3.41 (4H, m), 3.35 (2Hf t , J = 6.6 Hz), 1.84-1.43 (9H, m), 1.36-1.02 (3H, m)t 0.85 (3H, t. J = 7.3 Hz). 1-103 1H-NMR (300 MHz, DMSCMe) δ : 13.10 (1H. s). 11.16 (1H. s), 7.99-7.68 (2Ht m), 6.81 (1H, s), 3.97-3.83 (1H, m)f 3.58-3.15 (7Ht m), 1.77-1.37 (4H, m), 0.98-0.67 (6H, m). 1-104 HjC^ 1H-NMR (300 MHz. DMSOde) δ: 13.11 (0.8H, S), 12.98 (0.2H, S). 11.37 (0.2 H, s). 11.15 (0.8H, s), 7.94-7.75 (2H, m)f 6.87 (0.8H, s). 6.32 (0.2H, s), 4.6&amp;4.50 (0. 2H, m). 4.33-3.87 (2.8H, m), 3.63·3·11 PH, m)· 2·98^2·55 (2H. m&gt;·1·91·1·12 (16H, m) , 0.89 (3ΗΛ J = 7.3 Hz). 1-105 i:=:yLtYv4r&quot; h3/ h 'H-NMR (300 MHz, DMSCMe) 5:13.11 (1H, s)t 11.15(1Ht s), 7.94-7.75 (2H, m), 6.84 (2H. brs), 4.08-3.87 (1H, m), 3.49-3.24 (2H, m), 2.87-2.57 (3H, m). 2.17-1.88 (4H, m), 1.66 -1.45 (2H, m), 1.3W · 23 "2H· m>, 0. &lt;3H·t· J = 6.7 Hz&gt;. 1-106 H 'H-NMR (300 MHz, DMSOd6) δ: 13.15 (1H, s), 11.09 (1H, s), 8.60 (1H. t. J = 5.3 Hz). 7.98-773 (2H.m). 7.29 (1Ht s), 3.47-3.33 (4H. m), 326 (3H. s). 293 318197 1322688 Table 16

Example molecular structure NMR 1-107 η3 (γ 'H-NMR (300 MHzt DMSO-&lt;/6) δ: 13.27 (0.8H. br S), 13.09 (0.2H, br$), 11.42 (0.2H, Brs), 11.18 (0.8H. br s)t 8.62-8.39 (2H, m), 7.97-7.60 (3H, m), 7.46-7.28 (1H(m), 7.07-6.64 (0.8H, m)t 6.45 (0.2Hf br s)( 5.14 &lt;0.2H. br s), 4.74-4.71 (1.8H, m), 3.82-3.16 (2H, m), 1.60-1.18 (4Ht m). 0.93-0.74 (3H. m). 1-108 Η〆&quot; 1H-NMR C300 MHz, DMSO-tfe) δ: 13.20 (1H, br s). 11,50-11.00(1 H, brs), 7.97-7.69 (2H, m) 7.51-6.27 (6Ht m), 5.28-4^58 (2H(m), 4.00-3.36 (4Ht m). 3.23 (3H, s). 1-109 'H-NMR (300 MHz, DMSO-de) δ: 12.79 (1H, br s). 11.09 (1H, br s). 7.88-7.78 (2H. m), 6.76 (1H, br s), 4.28-3.95 (1Hr m), 3.53-3.10 (4H. m ) ( 3.00 (1H. d, J = 12.4 Hz), 2.59-2.32 (2H. m), 1.78-1.49 (6H. m). 1.38-1.22 (2H. m), 0.90 (3H, t. J = 7.3 Hz). Ί 1Ί0 'H-NMR (300 MHz (DMSO-&lt;/6) δ: 13.12 (1H, s). 11.16 (1H, s), 7.99-7.73 (2H, m), 6.88 (1H. s). 4.55 (1H. brdf J = 12.8 Hz), 4.23 (1Ht brs), 3.95 (1H, brdf J = 12.8 Hz), 3.65-2.85 (3H, m), 2.63-2.2 7 (1H. m). 2.08-1.41 (9H.m), 1.40-1.21 (2H, m), 0.90 (3H, t, J = 7.2 Hz). 1-111 1H-NMR (300 MHz, DMSO-tfe δ: 13.12 (1H, br 8). 11.18 (1H, s)t 7.89-776 (2H, m), 6.84 (1H, br s), 4.31-3.99 (1H, m), 3.67 (2H. d( J = 11.7 Hz), 3.56-3.18 (2H, m). 2.98-2.59 (5H. m), 2.10-1.73 (4H, m) (1.65-1.46 (2H, m). 1.40-1.22 (2H, m) , 0.90 (3H, t, J = 7.2 Hz). 1-112 ^NMR (300 MHzt DMSO-de) 5:13.12 (1H, s). 11.15 (1H. s). 7.93-7.74 (2H. m), 6.88 (1H. br s), 4.41-4.18 (4H, m). 3.62 (1H. d, J = 13.6 Hz), 3.52-3.01 (3H, m). 2.91-2.64 (1H, m). 2ΌΜ.67 (4H, m). 1.64-1.44 (2H, m). 1.37-1.14 (5H, m). 0.93-0.78 (3H, m). 294 318197 1322688 Table 17

Example molecular structure NMR 1-113 Η3 (Γ ^-NMR (300 MHz. DMSO-d6) δ: 13.53 (1H. br s). 11.21 (1H, s)f 7.88-7.78 (2H, m), 6.75 ( 1H, br s). 4.3 &amp; 4.20 (2H. m). 3.63 (1H. br d, J = 12.4 Hz), 3.57-3.01 (4H, m), 2.84-2.61 (1H, m). 1.96-1.46 (6H. m), 1.38-1.21 (2H, m). 0.89 (3H, t. J = 7.3 Hz). 1-114 h3 (t 'H-NMR (300 MHz, DMSOde) δ: 13.13 (1Ht s) 11.16 (1H, s). 7.96-7.72 (2H. m), 6.89 (1H, brs), 4.34-4.11 (1H, m), 3.69-3.24 (4H, m). 3.19-3.02 (2H, m) , 2.65-2.36 (2H, m), 2.15-1.93 (2H, m), 1.68-1.50 (2H, m), 1.39-1.21 (2H, m). 0.87 (3H, t. J = 7.2 Hz). 1 —115 H,(T ^-NMR (300 MHz, DMSO-de) δ: 13.12 (1H. ε). 11.16 (1H, s), 7.98-7.67 (2H, m)f 6.88 (1H, br s), 4.60-3.98 (1H, m), 370-3.18 (4H, m), 3.06-2.12 (4H, m), 2.06-1.44 (4H. m), 1.42-1.15 (2H. m). 1.0W).78 (3H, m). 1-116 »3 CH, 'H-NMR (300 MHz, DMSO-de) δ: 13.21 (1H, br s), 11.27 (1H, br s), 8.24-7.53 (4H, m ), 7.00-6,30 (2H, m), 5.09-4.45 (2H, m), 3.84 (3H, s), 3.7Q-3.10 (2H, m), 1.74-1.43 (2H, m), 0.92- 0.77 (3Hf m). 1-117 CH 3 ^ NMR (300 MHz, DMSO-de) δ: 13.34 (1H. br s). 11.31 (1H( brs), 8.65-8.43 (2H, m), 7.93-7.63 (3H, m). 7.47-7.34 ( 1H. m), 7.09-6.37 (1HP m), 5.26-4.55 (2H. m), 3.78-3.14 (2H, m), 1.77-1.41 (2H, m)t 0.93-0.73 (3H, m). 1 -118 0 1H-NMR (300 MHz, DMS0^6) δ: 13.25 (1H, br s). 11.14 (1H, brs), 9.17{1H. brs)f 7.90-7.75 (2H, m). 7.45-7 ^5 (5H.m) ( 4.48 (2H, d, J = 5.5 Hz), 3.55-3.05 (4H. br d), 1.09 (6H, br s). 1-119 1H-NMR (300 MHz, DMSO- De) δ: 13.24 (1H, br s), 11.14 (1H, br s). 9.17 (1H, br s)t 7.90-7.75 (2H, m). 7.45-7.15 (5H. m), 4.47 (2H, d. J = 5.9 Hz), 3.50-3.00 (4H, br d), 1.05 (6HP br s). 295 318197 1322688 Table 18

Example molecular structure NMR 1-120 0 1H»NMR {300 MHz, DMSO &lt;W δ: 13.24 〇H· br s), 11.14 (1H. brs), 9.17 (1H. brs). 8.39 (1H, br t, J = 5.1 Hz). 7.95-7.60 (4H.m), 7.38 (3H, d, J ^ 8.1 Hz&gt;_ 4.49 (2H·d. J : 5.9 Hz}. 3.27 &lt;2H, q, J = 7.2 Hz ), 1.11 (3H, t, J = 7.2 Hz). 1-121 1H-NMR (300 MHz. DMSO-de) δ: 13.24 (1Ht br s), 11.14 (1H, br s), 9.18 (1H, brs ), 8.44 (1H, br s), 7.86-7.70 (4H.m) ( 7.45-7.38 (3H, m), 4.49 (2H, d, J = 5.5 Hz), 3.28 (2H, dt. J = 14.4, 6.2 H2), 1.11t3H, t, J = 7.2Hz). 1-122 F nn ο α ο M-NMR (300 MHz, DMSO-de) δ: 9.14 (1H, br 8)t 7.95-7.75 (5H, m), 7.42-7.25 (4H, m). 4.49 (2H.d, J = 5.9 Hz). 1-123 ^NMR (300 MHz, DMSO-Cfe) 6:11.24 (1H, S), 7.90-7.78 ( 2H. m), 6.78 (1H, br s)f 4.44-4.25 (2H, m), 3.76-2.56 (6H, m), 2.02-1.45 (6H, m)# 0.87 (3H, t. J = 7.2 Hz 1-124 1H-NMR (300 MHz. DMSO-de) δ: 12.87 (1H, br s), 11.22 (1H. s), 7.90-7.77 (2H, m)t 6.79 (1H. br s&gt;, 4·51 (1H· br d· J = 12.8 Hz&gt;. 4_32 (1H, s&gt;, 3·(1H. brd, J = 12.8 Hz), 3.65-2.91 (6H, m). 2.68-2.41 (1H, m), 2.00-1.46 (6H, m), 0.87 (3H, t, J = 7.3 Hz). 1-125 CH, 1H-NMR (300 MHzf DMSO-de) 6:13.39-11.87 (1H, brs)t 11.22 (1H, brs), 7.89-7.79 (2H, m), 6.83 (1H. br s), 4.51 (1H, d, J = 13.2 Hz) , 4.40-4.18 (1H, m), 3.99 (1H, d, J = 13.2 Hz), 3.54-2.84 (4H, m), 2.70-2.31 (4H. m) (1.96-1.46 (6H, m). 0.86 &lt;3H,t, J = 7.2 Hz). 1-126 CHj 1H-NMR (300 MHz, DMSO-de) δ: 13.20 (1H, s) ( 11.14 (1H, s) ( 8.13 (1H, d, J = 1.9 Hz). 7.87-7.77 (2H, m). 7.63 (1H, dd, J = 8.5 (2.4 Hz), 7.16 (1Hf s). 6.82 (1Hf d, J = B.3 Hz). 4.65 (2Ht s) ( 3.83 (3H, s), 3.02-2.90 (1Hf m), 0.87-0.67 (4H, m). 296 318197 1322688 Table 19

EXAMPLES Molecular Structures NMR 1-127 ^-NMR (300 MHz, DMSO-dQ) δ: 13.24 (1H, lx S), 11.21 (1Hf br s), 8.07 (1H, s), 7.89-7.78 (2Ht m) , 7.58 (1H, d, J = 6.8 Hz), 6.94-6.71 (2H(m), 4.94-4.57 (3H, m)( 3.83 (3H, s)t 2.32-1.97 (4H, m), 1.70-1.44 (1H. br s). 11.23 (1K br s). 8.14 (1H. m), 7.72-7.59 (1H.m). 7.05-6.59 (2H.m). 5.0&amp;4.52 (2H. m), 3.84 (3H, s). 3.58-3.13 (2H( m). 1.09- 0.94 (1H.m). 0.56-0.34 (2H, m). 0.21-0.19 {2H. m). 1-129^NMR (300 MHz. DMSO-d6) δ: 13.21 (1H. 8), 11.13 (1H s), 9.01 (1H, s), 8.05 (1H, dt J = 2.3 Hz), 7.88-7.77 (2H, m). 7.48 (1H. dd, J = 8.7t 2.6 Hz), 7.31 (1H(s) ), 6.62 (1H, d. J = 9.0 Hz), 4.29 (2H. d. J = 5.7 Hz&gt;, 3.00 (6H·s). 1-130 HjCj〇TTVjl^ ch3 ch, 1H-NMR (300 MHz. DMSO-de) δ: 13.24 (1H, br s), 11.18 (1H, br s)t 8.16-7.73 (3H, m). 7.57-7.27 (1H, m), 6.89 (0.8H, br s), 6.63 (1H, d, J = 8.3 Hz)t 6.41 (0.2H, br s), 4.99-4.30 (2H, m), 3.66-3,15 (2H, m), 3.00 (6H, s), 1.73-1.44 (2H, m), 0.83 (3H.t, J = 6.8 Hz). 1-131 CrV^yVr HOT^ ^-NMR (300 MHz, DMSO-de) δ: 13.77-11.97 (1H. m) 11.22 (1H, brs). 7.83 (2H, br s). 7.41-7.24 (5H, m). 6.92-6.58 (1H, m), 5.04-4.60 (2H, m), 3.85-3.63 (1H. m ), 3.62-3.42 (1H, m), 2.70-2.52 (2H, m). 1-132 1H-NMR (300 MHz, DMSO-de) δ: 13.29 (1H, br s). 11.15 (1H, br s 7.98-7.67 (2H.m), 7.4&-7.19 (5H, m), 7.13-6.35 (1H, m), 5.2-M.62 (2H, m), 4.12-3.38 (4Hf m). 2J6-2.55 (2H, m), 1.16 (3H. t, J = 6.8 Hz). 1-133 eija^VV^ 'H-NMR (300 MHz. DMSO-de) 5:13.25 (1H, br s), 11.26 (1H, br s), 8.45-8.32 (1H. m), 7.90-7.78 (3H, m), 7.57-7.43 (1H, m), 7.01-6.51 (1H. m), 5.08-4.56 (2H, m), 3.64-3.19 (2H, m), 1.7&amp;-1.50 (2H. m), 0.85 (3H, t. J = 7.3 Hz). 297 318197

1322688 Table 20 Example Molecular Structure NMR 1-134 'H-NMR (300 ΜΗζ( DMSO-d6) δ: 13.23 (1Η, br s). 11.13 (1Η. br s). 8.80 (1H. br t), 7.87 -7.76 (2H.m). 7.55-7.49 (2H, m). 7.45^7.32 (2H, m), 4.70 (2H. d. J = 4.5 Hz). 1-135 'H-NMR (300 MHz, DMS0 -de) δ: 13.28 (1H, s), 11.15 (1H, s), 8.94 (1H, t. J = 4.5 Hz). 8.66 (2H, s). 7.90-7.74 (2H. m). 7.33 (1H , s). 4.67 (2H. d, J = 4.5 Hz). 1-136 1H-NMR (300 MHzt DMSO-&lt;/B) δ: 13.37-13.01 (1H, m), 11.53-11.03 (1H, m ) ( 8.65 (2H, s). 7.98-7.70 (2.5H, m), 6.93 (0.5H, 3), 5.61-4.68 (2H, m) ( 3.80-3.00 (2H, m), 1.71-1.36 (2H , m), 0.85 (3Ht t, J = 6.4 Hz). 1-137 'H-NMR (300 MHz, DMSO-dt) δ: 11.20 (1H. s), 9.24 (1H, t (J = 5.8 Hz) , 8.61 (1Hf d. J = 2.6 Hz), 8.60 (br s), 8.44 (1H, s), 7.97-7.79 (5H, m), 7.26 (1H, s)f 6.56 (1H, dd, J = 1 , 9.2.6 Hz), 4.51 (2H, d, J = 5.7 Hz). 1-138 1H-NMR (300 MHz, DMSO-de) δ: 13.20 (1H, br s), 11.16 (1H( brs), 9.00 (1H, brs), 8.06 (1H, d, J = 2.3 Hz), 7.89-7.79 (2H, m) ( 7.48 (1H, dd, J = 8.9, 2.4 Hz). 7.30 (1H, Br s), 6.82 (1H, d, J = 8.7 Hz), 4.67 (1H. d, J = 4.1 Hz), 4.29 (2H, d, J = 5.7 Hz). 4.03-3.94 (2H, m), 3.73 -3.62 (1H, m), 3.10-3.00 (2H(m). 1.80-1.71 (2H(m), 1.40-1.26 (2H, m). 1-139 'H-NMR (400 MHz, DMSOde) δ: 13*17 (1H, br s). 11.13 (1H, brs)t8.67 (1H. brt, J = 5.6 Hz), 8.50 (1H, br d. J = 3.0 Hz), 7.87-7.77 (2H, m ), 7.70 (1H, td, J = 7.4.1.9 Hz). 7.2T(2Hfc d( J = 7.9 Hz), 7.24-7.19 (1H, m), 3.59 (2H. q, J = 6.8 Hz), 2.98 (2H. t, J = 7.4 Hz). 1-140 'H-NMR (400 MHz. DMSOde) δ: 13.17 (1Ht br S), 11.14 (1H, s), 8.66 (1H, t, J = 5.6 Hz ), 8.44 (1H, d, J = 1.9 Hz), 8.40 (1H, dd, J = 4.6 (1.4 Hz), 7.87-7.77 (2H.m). 7.65 (1H. dl, J = 7.9.1.9 Hz) , 7.31 (1H, q, J = 42 Hz). 7^6 (1H, d, J = 1.9 Hz), 3.49 (2H, q. J - 6.6 Hz), 2.86 (2H, t, J = 6.7 Hz) .

298 318197 1322688 Table 21 Example Molecular Structure NMR 1-141 N-N 〇α 1H-NMR (400 MHz. DMSO-de) 6:13.18 (1H. s), 11.14 (1H, s). 8.67 (1H, t , J = 5.6 Hz). 8.46 (2Ht d. J = 5.6 Hz). 7.87-7.77 (2H.m). 7.26 (3H. q. J = 2.0 Hz), 3.51 (2H. qf J = 6.5 Hz). 2.86 (2H. tJ = 7.0 Hz). 1-142. Cl 'H-NMR (400 MHz, DMSOtf6) 6:13.27 (1H. br s). 11.17 (1H, s). 9.59 (1H, s), 9.23 (1H, t. J = 6.0 Hz), 8.11 (2H d. J = 8.3 Hz), 7.87-7.78 (2H.m). 7.49 (2H.d, J = 8.3 Hz). 7.38 (1H. d. J = 2.3 Hz), 4.52 (2H, d, J = 6_0 Hz). 1-143 W 1H-NMR (400 MHz. DMSO-de) δ: 13.25 (1H. br s), 11.15 (1H, brs), 9.22 (1H. brs), 8.48 (2H, br s) 7.89-7.77 (2H, m). 7.35 (1H, brs). 4.53 (2H, d, J = 6.0 Hz). 2.46 (3H, s). 1-144 N-N 〇Cl 'H-NMR (400 MHz, DMSO-tfe) δ: 13.54 (1H, s). 11.33(1H, S). 11.21 (1H, s), 9.40 (1H, d, J - 1.4 Hz). 8.49 (1H. br s), 8.43 (1H, d, J = 2.8 Hz). 7.91-7.80 (2H.m)f 7.77 (1H, s). 1-145 nn ο a ^NMR (400 MHz, DMSOd^) δ: 13.48 (1H, s) 11.27 (1H, s), 10.65 (1H, s), 8.95 (1H, q, J = 1.9 Hz), 8.40 (1H, d, J = 8.3 Hz), 7.97 (1H, d, J = 8.3 Hz) , 7.92-7.78 (3H, m), 7.70 (2H, d, J = 7.4 Hz), 7.59 (1H, q, J = 4.2 Hz). 1-146 1H-NMR (400 MHz. DMSO^fe) δ: 13.71 (0.24H, s). 13.47 (0.75H. s). 11.61 (0.74H, s). 11.34 (0^6H, s), 11.21 (0.80H, d, J = 15.0 Hz), 10.48 (0.23H , s). 9.02 (0.16H, s), 8.98 (0.68H. q. J = 1.9 Hz)f 8.70 (0.74H.t, J * 3.7 Hz), 8.62 (0.22H, df J * 7.4 Hz), 8.47-8.43 ( 1.06H, m), 8.00-7.82 (1.90Hr m) ( 7.77 (0.19H, d. J = 7.4 Hz). 7.73-7.59 (2.75H, m). 7.42 (0.26H, s), 6.59 (0.71H , d. J = 1.4 Hz). 1-147 'H-NMR (400 MHz. DMSO-de) δ: 13.48 (1Ht br S), 11.25 (1H, S), 10.63 (1H. s). 9.36 (1H , s), 8.54 (1H. d( J = 6.0 Hz). 8.07 (1H, d, J = 8.3 Hz), 7.91-7.80 (3H, m), 7.77-7.66 (2H, m). 1-148 H ^NMR (400 MHz, DMSCMe) δ: 13.37 (1H, br s). 11.20 (1H. br s) ( 10.30 (1H. br s). 7.96 (1H, d. J = 1.9 Hz). 7.87-7.84 ( 2H. m), 7.47 (1H, br s), 7.37 (1H. d, J = 1.9 Hz). 4.1W.09 (4H, m). 1.57 (6H_ s)· 1.28 (3ΗΛ J = 6.7 Hz). 1_15 (3ΗΛ J = 7.2 Hz). 299 318197 1322688 Table 22

EXAMPLES Molecular Structures NMR 1-149 Η 1H-NMR (400 MHz, DMSO-d6) δ: 13.37 (1H, br s). 11.19 (1H, br s), 10.33 (1H. br s), 8.10 (1H. Br s). 7.84 {2H, br s). 7.54 (1H. br s), 7.50 (1H, br s). 6.25 (1H, br s), 4.13-4.04 (4H, m), 1.70 (3H, s&gt ;, 1.29 (3H. t, J = 6.7 Hz). 1.17 (3H. t. J = 7.0 Hz). 1-150 Η 'H-NMR (400 MHz, DMSO-de) δ: 13.36 (1H. br s 11.18 (1H. br s), 10.27 (1H, br s), 7.99 (1H, d. J = 1.9 Hz), 7.90-7.80 (2Hf m), 7.39 (1H, d. J = 1.9 Hz), 4.12 (2H. qt J = 7.0 Hz) t 3.32 (2Hf s). 1.54 (6H. s), 1.28 (3H. t. J = 7.0 Hz). 1-151 Η ^NMR (400 MHz, DMSOde) δ: 13.35 (1H. br s), 11.23 (1H, br s) ( 10.30 (1H, br s). 8.13 (1H. d, J = 1.9 Hz), 7.91-7.79 (2H, m), 7.5β (1H. d. J 1.9 Hz), 4.10 (2H, q, J = 7.1 Hz), 3.32 (2H, s)t 1.69 (3H, s), 1.29 (3H, t. J = 7.0 Hz). 1-152 F Ors ^r8^ ^NMR (400 MHz, DMSO-tfe) δ: 13.30 (1H( br s). 11.19 (1H, br s). 9.29 (1H, br s), 8.65 (1H, br s). 8.62 (1H , t, J = 2.1 Hz), 8.57 (1H, d, J = 2.3 Hz), 7.92-7.79 (2H, m), 7.39 (1H, br s). 4.61 (2H, d, J = 6.0Hz). 1-153 'H-NMR (300 MHz, DMSO-de) δ: 13.24 (1H, br s), 11.17 (1H, br s), 9.03 (1H, br s), 8.09 (1H , d, J = 1.9 Hr), 7.87-7.81 (2H. m), 7.52 (1H, dd, J = 8.8. 2.3 Hz). 7.32 (1H, br s) ( 6.84 (1H, d, J = 8.3 Hz) ), 4.31 (2H, dt J = 6.0 Hz), 3.90-3.87 (4H.m) ( 2.60-2.56 (4H, m). 1-154 0 'H-NMR (300 MHz, DMSO-de) δ: 13.24 (1H. br s), 11.19 (1H, br s), 9.05 (1H, br s)t 8.15 (1H, d, J = 2.3 Hz). 7.8&amp;-7.81 (2H. m), 7.59 (1H. Dd, J 2.8. 8.8 Hz). 7.30 (1H, br s). 7.03 (1H, dr J » 8.8 Hz), 4.34 (2H, d, J = 5.6 Hz), 4.07-4.03 (4H, m). 3.10 -3.06 (4H, m). 1-155 Br NMR (400 MHz, OMSO-de) δ: 13.33 (1H, br s). 11.21 (1H, br s), 9.29 (1H, br s), 7.87- 7.81 (2H.m), 7.29 (1H, br s), 7.05 (1H, 8), 4.52 (2H, d( J = 5.80 Hz). 300 318197 8 1322688 Table 23 Example Molecular Structure NMR 1-156 Η ^ -NMR (400 MHz, DMSO-d6) δ: 13.31 (1H. br s), 11.19 (1H, br s). 9.26 (1H. br s) ( 7.87-7.81 (2H, m). 7.29 (1H. br s), 6.97 (1Hf d. J = 3.8 Hz), 6.90 (1H, d, J = 3.8 Hz), 4.51 (2H, d, J = 5.8 Hz). 1- 157 H^C ^-NMR (400 MHz, DMSO-d6) δ: 13.26 (1H, s), 11.15 (1H, s), 9.06 (1H. s). 7.86-7.80 (2H, m). 7.32 (1H ( s ), 4.39 (2H, d. J = 5.3 Hz). 2.47 (2H. q, J = 7.5 Hz). 2.33 (3H, s)* 1.12 (3H. t J = 7.5 Hz). 1-158 ' H-NMR (400 MHz, DMSO-tf β) δ: 11.19 (1H, s), 9.07 (1H, t, J = 5.6 Hz), 7.87-7.80 (2H, m), 7.25 (1H. s), 4.41 (2H, d. J = 5.6 Hz). 2.70 (2H, qt J = 7.6 Hz), 2.11 (3H. s). 1.21 (3H, t, J = 7.6 Hz). 1-159 Η 'H-NMR ( 400 MHz, DMSOde) δ: 13.30 (1H. br s), 11.19 (1H. brs), 9.27(1H, brs), 7.85-7.82 (2H, m). 7.48 (1H, dd, J = 5.1, 1.2 Hz ), 7.32 (1H. br s), 725 (1H, dd, J = 3.7, 1.2 Hz), 7.13 (1H, d, J = 3.7 Hz), 7.06 (1H, dd. J = 5.1, 3.7 Hz). 6.97 (1H, d, J = 3.7 Hz), 4.58 (2Hf d, J = 5.8 Hz). 1-160 η/ 1H-NMR (400 MHz, DMSO^e) 13.24 (1H, br s). 11.14 (1H , s s). 9.09 (1H, br s). 7.84-7.81 (2H, m). 7.33 (1Ht d, J = 5.5 Hz), 7.30 (1H. br s), 6.97 (1H, d, J = 5.5 Hz). 4.44 (2H, d, J = 57 Hz), 3.82 {3H( s). 1—161 c'^prV4rV^ 'H-NMR (400 MHz, DMSO-de) δ: 13.34 (1H, s) , 11.19 (1H , 8), 9.34 (1H. t. J = 5.6 Hz). 7.87-7.80 (2H( m), 7.33 (1H, s), 7.08 (1H, s), 4.52 (2H. d, J =5.6 Hz) 1-162 η/^ η ,H-NMR (400 MHz. DMSO-de) δ: 13.21 (1Hf s), 11.13 (1Ht s), 8.96 (1H. br s), 7.86-7.80 (2H, m) 7.32 (1H, s), 4.19 (2H, d, J = 5.6 Hz), 2.31 (3H, s). 2.29 (3H, s). 301 318197 8 1322688 Table 24 Example Molecular Structure NMR 1-163 ^- NMRi^ MHz, DMSO-d6) δ: 13.26 (1Ηβ s). 11.15 (1Η, s), 9.05 (1Η, br s), 7.86-7.79 (2H, m), 7.32 (1H. s). 4.39 (2H d. J = 5.2 Hz), 2.63 (2H.t, J = 7.2 Hz), 2.08 (3H, s), 1.64-1.59 (2H.m), 1.31-1.24 (6H·m), 0.84 (3ΗΛ J = 7.2 Hz). 1-164 b Η MHz, DMSO-d6) δ: 13.23 (1H, s). 11.15 (1H, s), 8.98 (1H, t, J = 5.6 Hz). 7.86-7.80 (2H. m), 7.37 (1H. s). 7.19 (1H, d, J = 3.6 Hz). 6.57 (1Ht d. J = 3.6 Hz), 4.26 (2H. d. J = 5.6 Hz), 3.79 (3H, s&gt ; 1-165 'H-NMRMOO DMSO&gt;de&gt; δ: 13.30 (1H, s)· 11.17 (1H, s), 9.16 (1H.t, J ^ 5.2 Hz), 7.94-7.92 (2H, m), 7.87-7.80 (2H.m). 7.55-7.49 (3H, m), 7.35 (1H, s)t 4.52 (2H, d, J = 5.2 Hz), 2.22 ( 3H. s). 1-166 η/ η 1H-NMR (400 MHz, DMSO-tfe) δ: 13.31 (1H, s) ( 11.16 (1H. s), 9.24 (1H, t. J * 5.2 Hz), 7.88-7.81 (4H, m), 7.49-7.45 (2H, m), 7.38-7.35 (2Ht m), 4.67 (2Hf d, J = 5.2 Hz), 2.46 (3H, s). 1-167 Η, / Η 'H-_R(400 MHz, DMS(&gt;de&gt; δ: 11·18 (1H. s), 9.07 (1Hr br s), 7.87-7.79 (2H, m), 7.25 (1H, s), 4.41 (2Hf d, J = 4.0 Hz), 2.47-2.44 {2H( m), 2.38 (3H, s), 1.56-1.49 (2H, m), 1.30-1.16 (6H. m) (0.84 (3H, t. J = 6.6 Hz). *;_ Next, the following compounds were prepared according to the aforementioned Preparation Method A-. ^ [Example 2-1] 5-(2-Ga-4, 5-difluoro-benzoamitoylamino)-1Η-pyrazole-3-carboxylic acid (6-gas-pyridin-3-ylmethyl) )-Preparation of guanamine; 302 318197 1322688

, 5-(2-Ga-4, 5-difluoro-benzoamitoylamino)~1Η~η obtained in the first step of Reference Example 1, is more than the benzo-3-benzoic acid benzotris-l-yl ester. Preparation (2.15 g) A solution of hydrazine, dimethylformamide (11 ml) was added to a commercially-purified mixture of the amino-aminomethyl-6-gas-pyridine (0.77 g), and stirred at room temperature for 3 hours. The resulting mixture was added dropwise with water (10 ml), and the obtained solid was filtered to give the title compound (2·1 g). [Example 2-1-1] 5 II ijjUL - 4. 5 - difluoro-benzoammonium amino)-lH-g is more than -3-acid (6-oxo-pyridine-3-f The ratio of guanamine dihydrochloride _

5-(2-Ga-4, 5-difluoro-benzylidenylamino)-1H-pyrazole-3-carboxylic acid (6-chloro-pyridin-3-ylindenyl) obtained in Example 2-1 To a solution of methanol (10 ml) in tetrahydrofuran (10 ml) was added 4N <RTI ID=0.0> The solid formed was filtered to give the title compound (1. [Example 2-2] 5-(2-chloro-4,5-diindole-jasmonylamino)-1Η-pyrazole-3-carboxylic acid 303 318197 1322688 2, 4~|三0企-3 -ylmethyl)-branched amine preparation;

In the same manner as in Examples 2 to 1, from 5-(2-chloro-4,5-difluoro-benzoindolyl)-1H-pyrazole-3-carboxylic acid benzotriazol-1-yl ester (160 mg) and UH-[1,2,4]triazol-3-ylmethyl)-amine (42 mg) (prepared according to Biomedical Chemical Letters, 4, 2441, 1994) to obtain the title compound ( Mg). [Example 2-2-1] 5-(2- Mu ~4, 5^ _1,2,4]7-yl 1 -aminoamino-yl)-decylamine dihydrochloride t

N

Fluorine-stupid base ^^^7 7 sigh, lil i λ j ZLy 4 - guanamine (37 mg) 獾π#

The title compound (30 mg) was obtained [Example 2-3] J

318197 304 1322688

F &quot; In the same manner as in Example 2-11, from 5-(2-chloro-4,5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylic acid benzotriazole-b The title compound (155 mg) was obtained from the title compound (m.p. Reference [Example 2-3-1] ^(2-Oxo-4, 5-diylamino)_1H_pyrazole-3 phthalic acid (5_Fluorine = 4H-啥 嘛 -3- 上上: 醯Amine di-salt 醯_ Xi N;

2HC1 F

Λτνκ In the same manner as in Example 2-1-1, from 5~(2_chloro-4,5~difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid (5-fluoro~4Η) - quinazoline 〜3_yl) monoamine (48 mg) gave the title compound (23 mg). [Example 2-4] 5^(2-oxo-4,5-, fluorene-benzoylamino)-indole||-indolozole-3~:^ acid (4,6-* _ dimethyl Preparation of pyridine-pyridin-3-ylindenyl)-decylamine; Step 1: Preparation of 3-aminomercapto-4,6-dimethyl-ρ ratio bite; N&quot;^r^^NH2

318197

305 1322688 Preparation of 3-cyano-4,6-lutidine from 2-ox-3-cyano-4,6-dimethylpyridine (2.0 g) according to Tetrahedron, 22, 3417, 1996 ( 1. 23 grams). • The title compound (436 mg) was prepared from 3-cyano-4,6-, dimethyl-pyridine according to the title of the Heterocyclic Chemical Journal, 30, 473, 993. Step 2: 5-(2-Gas-4, 5-difluoro-momehydrylamine)-1Η-pyrazole-3-$ 6-dimercapto-pyridin-3-ylmethylguanamine Preparation

F

In the same manner as in Example 2-1, 5-(2-chloro-4,5-difluoro-benzoamidinoamine-pyrazine-3-carboxylic acid (140 mg) and 3-aminomethyl- 4 , 6-Dimethyl-pyridine (70 mg) obtained the title compound ( 〇. 110 g). [Example 2-4-1] R-(&quot;2-chloro-4. 5_difluoro-stupylmethyl Preparation of amino-based)-111-° ratio of -3-acid (4·di-fluorene-pyrimidin-3-ylmethyl)-guanamine dihydrochloride;

5-(2-Gayl-4,5-difluoro-benzhydrylamino)-1H-0 is 0-O-acid (4,6-dimethyl-pyridin-3-ylfluorenyl) A suspension of decylamine (430 mg) in MeOH (5 mL) - THF (25 mL). The resulting solution was concentrated under reduced pressure to EtOAc (EtOAc). [Example 2_5] jr(2-oxo-4,5-difluoro-benzoamitoylamino)-1{{-carbazole-3-carboxylic acid (2-methyl-1-yl-6-methyl-pyridine) -3-ylformamidine) l-amine hydrochloride; free of the preparation of 1: 3-aminomethyl-2-methyl argon-6-methyl-pyridine;

According to the Journal of Heterocyclic Chemistry, 36, 653, 1 999, from 2-chloro-3-cyano-6-indenyl. 3_Cyano-2-methoxy_6-methylpyridine (2.77 g) was prepared by a bite (3. gram). Subsequently, the title compound (608 mg) was prepared from 3-cyano-2-methoxy-6-mercaptoacridine (739 mg) from the title of the title compound (3, 473, 1 993).

Preparation of Li-(2-decyloxy-6-methyldi-n-bipyridin-3-anthracenyl)-decylamine;

F

In the same manner as in Example 2-1, 5-(2-chloro-4,5-difluoro-benzoinylamino)-1 hydrazine-carbazole-3-carboxylic acid benzotriazole-bupropionate ( 1. 66 g) and 3-aminomercapto-2-indolyl-6-methylpyridinium (6〇3 mg) obtained the title 318197

307 1322688 Compound (501 mg). [Example 2-6] 5-(2-gas-4. 5-difluoro-benzoicylamine)-ΐΗ-° ratio peak gas group-6-methyl-tf ratio -3-methylmethyl )--the increase of the amine; * Step 1: The case of 4-methylhydro-6-methylnicotinate ethyl ester f.

Chlorine ~ 6, according to Synthesis, 6, 479, 1988, from 2, 4, ethyl nicotinic acid (1.0 g) to prepare 2-gas-4-methoxy-6, methyl / methyl 7 Ester (0.387 g). Title 1 was then prepared according to the same document; acidity was determined). . (21 2 : 3-hydroxymethyl-4- yl-6-methylpyrazole

H, C

The title compound (μ mg) was prepared from 4-methoxy-6-mercaptonicotinate (212 mg). Aminomethyl-4-methyl -6-methylpyrazine cold preparation; f 丫~NH,

0 I CH H, C* 3 Reference J. Med. Chem., 46, 453, 2003, from 3-hydroxymethyl; 318197 308 ^ 22688 based on methoxy-6 methyl^ to bite (553 mg) 3 Gas 曱4_曱 曱 曱 比 将 将 未经 未经 未经 未经 未经 未经 未经 未经 未经 未经 未经 未经 未经 未经 未经 未经 未经 未经 未经 未经 未经 未经 未经 未经 未经 未经 未经 未经 未经 未经 未经 未经 未经 未经 未经 未经 未经The title compound (331 mg) was further prepared according to the procedure. -Alkaloids, an amine group, -1 -pyrazol-3-carboxyl,pyridin-3-one

In the same manner as in Example 2-1, 5-(2-chloro-4,5-difluoro-benzylidenylamino)-1 Η-pyrazole-3-carboxylic acid benzotriazole-indole-yl ester ( 413 mg) and 3-aminomercapto-4-methoxy-6-methylpyridine (15 mg) gave the title compound (368 mg). [Example 2-6-1] 5-(2-Oxo_-4"5-·^^-曱醯曱醯曱醯脍)-1Η-pyrazole-3-recording gas (4-methoxy-6-) A. base - ° ratio _ ^ - 3 dimethyl carbamide dihydrochloride _ eve.

In the same manner as in Example 2-4-1, 5-(2-gas-4,5-difluoro-stupid 318197 309 1322688 decylamino)-1 H-° ratio 0--3-acid ( The title compound (124 mg) was obtained from EtOAc (m. [Example 2-7] 5-(2-Ga-4,5-difluoro-stupylamino)-1!!-° than beer-3-# acid (2-methoxy~~4, 6-Dimethyl butyl-3-ylmethyl)-bristamine hip # ; Step 1: Preparation of 3-aminoguanidino-2 -methoxy-4,6-diindenyl- η ratio bite ;

Preparation of 3-cyano-2-methoxy-4 from 3-cyano-2-chloro-4,6-dimethylpyridine (1. 50 g) according to the Journal of Heterocyclic Chemistry, 36, 653, 1 999 , 6-lutidine (1. 31 g). The title compound (826 mg) was prepared from the title compound (3,,,,,,,,,,,,,,,,,,,,,,,,,,, Step 2: 5-(2-Ke-4,5-difluoro-benzhydrylaminopyrazole-3-borrowed dish (2-mercapto-4,6-diinyl ratio -3- Based on the base of the base;

In the same manner as in Example 2-1, 5-(2-chloro-4,5-difluoro-benzylidenylamino)-1 Η-pyrazole-3-carboxylic acid benzotriazol-1-yl ester ( The title compound (1. 23 g) was obtained from the title compound (1. 26 g). 318197 310 1322688 [Example 2-7-1] H2-gas-4, 5-; fluoro-benzoguanamine A)-ih-pyrazole-3-carboxylate^j Xun A-4, 6-di Kebita-3-yl-methyl guanamine dihydrochloride

In the same manner as in Example 2-1-1, from 5_(2_gas_45-difluoro-p-carbamoylamino)-1Η-pyrazole-3-carboxylic acid (2-indolyl- 4, 6-Dimethyl-pyridyl-3-ylhydrazinylamine (261 mg) was used to prepare the title compound (288 gram). % Next, using the aforementioned Example 24 to Example 2-7. 2_33. The same way to prepare

3 1 8 1 ft-» 311 1322688 Table 25 Example Molecular Structure NMR 2-1 CIj〇rV4yV^ 1H-NMR (400 MHz. DMSO-&lt;ie) ¢: 4.46 (2H, d. J = 5.5 Hz). 7.34 (1H. s), 7.50 (1Hf d. J= 8.1 Hz). 7.79-7.81 (3Ht m). 8.38 (1H. s). 9.18 (1Hf s). 11.17 (1H, s)f 13.27 (1H. s). 2-1-1 1H-NMR (400 MHz, DMSO-de&gt;:: 4.46 (2H, d. J = 5.9 Hz). 7,24 (1H. s). 7.50 (1H. dt J = 8.1 Hz). 7.81-7.84 (3H, m). 8.38 (1H. d. J = 2.2 Hz). 9.19 (1H. s). 11.19 (1H. s). 2-2 Η 'H-NMR (400 MHz, DMSO-rfi) 3: 4.52 (2H, d, J = 5.6 Hz). 7, 34 (lH, bre &gt;, 7.83 · 7.87 (2H, n0, 9.14 (lH, a &gt;, 11.18 (lH, sU3.26 ( lH, s)· 2-2-1 Η 1H-NMR (400 MHzt DMSO-de) δ: 11.24 (1H, s), 9.26 (1H, d. J = 5.8 Hz), 8.89 (1H, s). 7.89 -7.83 (2H.m), 7.28 (1H, s). 4.65 (2H. d. J = 5.6 Hz). 2-3 H-NMR (400 MHz, DMSCW«) S: 4.92 (2H, s), 7.06 * 7.14 (2H, m), 7.33 (lH, m &gt;, 7.9 〇 (lH, m), 11.52 (lH, m), 13.71 (lH, bre). 2-3-1 1H-NMR (400 MHz. DMSO -c/β) δ: 11β4(1Η.&), 8·99(1Η,_, 7_92(2H,m&gt;, 7.43{1H,m}_ 7.19(2H,m&gt;·6·(IH. s)· 5.01&lt;2H,s&gt;· 2-4 h^JCQrVV^ 'H-NMR (400 MHz, DMSCMt) 5:2.30 (3H, s), 2.39 (3H. s), 4.42 (2H, d, J = 5.5 Hz). 7.06 (1H, a), 7.34 (1H, e ), 7.78-7.86 (2H, m), 8.29 (1H, a). 8.97 (1H, a), 11.14 (1H. s), 13.23 (1H. b). 2-4-1 'H&gt; NMR (400 MHz, DMSO~de) δ : 2.58 (3H. s)· 2.68 (3H. s), 4.56 (2H, df J = 5,5 Hz), 7.25 (1H, s), 7.79-7.85 (3H, m) , 8.54 (1H, s), 9.19 (1Ht s), 1122 (1H. s).

312 318197 1322688 Table 26 Example Molecular Structure NMR 2-5 1H-NMR (400 MHz, DMSO-de)) ¢: 2.37 (3H, s), 3.89 (3Hf s). 4.33 (2H. d. J = 5.5 Hz ), 6.81 (1H. dt J =7.7 Hz), 7.36 (1Ht s), 7.43 (1H, d, J = 7.3 Hz), 7.79-7.87 (2H.m), 8.96 (1H. S), 11.16 (1H .s), 13.22 (1H. s). 2-6 H3Cj〇7JLqV^ CH, 'H-NMR (400 MHz, DMSO-i/6) 5:2.42 (3H, s), 3.86 (3H, a), 4.36 (2H, d, J = 5.5 Hz). 6.93 (1H, s), 7.35 (1H, s), 7.82 (2H, dt, J = 10.0, 5.0 Hz), 8.14 (1H, s). 8.91 (1H , t, J = 10.0 Hz), 11.13 (1H, s), 13.22 (1H. s). 2-β-Ι λΗ-ΝΜΛ{ΑΟΟ MHz, DMSO-de) 5:2.70 (3H, s), 4.12 ( 3.H (s). t, J = 5.6 Hz). 11.23 (1H. s). 15.43 (1Hf s). 2-7 H-NMR (400 MHz, DMSO &lt;/6) 6:2.29 (SH, e), 2.33 (3H. a ), 3.85 (3H, a), 4.40 (2H, d, J = 4.8 Hz). 6.70 (1H, a), 7.30 (1H, a), 7.76-7.85 (2H, m), 8.54 (1H, s) , 11.09 (13⁄4 8), 13.15 (1H, a). 2-7-1 1H-NMR (400 MHz, DMSOde) δ : 2.30 (3H, s). 2.34 (3H. s). 3.87 (3H, s) , 4.40 (2H, d, J = 4.8 Hz). 6.72 (1H. s), 7.24 (1H, s), 7.76-7.85 (2H, m). 8.53 (1H. t, J = 4.8 Hz). 11.11 (1H, s). 2-β 1H-NMR (300 MHz. DMSO-de) δ: 13.21 (1H. s), 11.14 (1H. s). 8.92 (1H.S). 8.37 (1H. d, J = 4.2 Hz ), 7.84 (2H, dd. J = 10.0, 7.2 Hz). 7.59 (1H, d. J = 7.4 Hz), 7.35 (1H, s), 7.23 (1H, ddt J = 7.4t 4.6 Hz), 4.56 ( 2H, d. J = 5.1 Hz), 2.34 (3H. s). 2-9 1H-NMR (300 MHz, DMSO-de) ^ 13.27 (1H, s), 11.16 (1H, s). 9.14 (1H, s). 8.33 (2H, d. J = 15.0 Hz), 7.86-7.79 (2H, m), 7.53 (1H, s). 7.33 (1H. s), 4.43 (2H, d. J = 6.0 Hz), 2.29 (3H, s). 313 318197 1322688 Table 27

Example molecular structure NMR 2-10 'H-NMROOO MHz. DMSO-&lt;/6) δ: 13.27 (1Η, s)t 11.17 (1Η. s). 9.14 (1H. s), 8.41 (1H, s) 7.86-7.80 (2H, m). 7.60 (1H. dd. J = 7.9.2.3 Hz), 7.32 (1H, s). 7.22 (1H. d. J = 7.9 Hz), 4.41 (2H. d. J = 5.6 Hz). 2.44 "3H, 2-11 1H-NMR (300 MHz. DMSOde) δ: 13.27 (1H. s), 11.17 (1H. s). 9.16 (1H, s). 7.87-7.79 (3H. m). 7.64 (1H, t, J - 7.7 Hz). 7.12 (2H, t, J = 6.4 Hz), 4.48 (2H, d. J = 5.9 HzJ, 2.46 (3H. s). 2-12 1H- NMR (300MHz.DMSO-d6) 5: 11.28(1H, s)t 9.36 (1H, t, J = 5.8 Hz) ( 8.90 (1H, s), 8.85 (1H, dt J =5.6 Hr), 8.52 (1H , d, J = 8.3 Hz), 8.05 (1H, dd, J = 7.9. 5.6 Hz), 7.95 (1H. d. J = 6.5 Hz), 7.78 (1H. d. J = 9.3 Hz). 7.25 (1H s). 4*65 (2H, d, J = 5.6 Hz)* 2-13 ^-NMROOO MHz, DMSO-de) 6: 11.19 (1H. s), 8.20-8.11 (1H. m). 7.94- 7.68 (2Hf m), 7.24 (1H, 8). 7.18 (1H, m)( 4.33 (2H, d, J = 5.7 Hz). 2-14 ' Η tH-NMR (300MHzlDMSC&gt;(/e) 13.24 (2H , s)t 10.98 (1H, s), 7.97-7.49 (5Hf m). 5.57 (2H. d. J = 5.2 Hz). 3.38 (3H, s). 2-15 Η 1H-NMR (300 MHz, D MSO-tfe) δ: 13.23 (1Ht s). 11.14 (1H, s), 9.73 (1H( s). 9.14 (1H. s). 7.83 (2H. q. J = 8.8 Hz). 7.34-7.28 (2H , m). 7.17-7.04 (3H, m), 4.42 (2H. d. J = 5.5 Hz). 2.97 (3H. s). 2-16 0 Η Η 1H-NMR (300 MHz, DMSOde) δ: 13.22 (1H, s), 11.13 (1H, s), 9.65 (1H. s). 9.10 (1H. s), 7.87-7.77 (2H, m). 7.32-7.29 (5H, m). 4.40 (2H. d J = 5.9 Hz). 2.95 (3H, s). 314 318197 1322688 Table 28 Example Molecular Structure NMR 2-17 1H-NMR (300 MHz. DMS0-de) δ: 13.22 (1H, s). 11.13 (1H , s), 9.91 (1H. s)t 9.14 (1H. s). 7.86-7.78 (2H, m). 7.54-7.44 (1H, m), 7.36 (1H, s). 7.25-7.23 (1Ht m) , 6.98 (1H. d. J = 7.0 Hz). 6.50-6.43 (1H. m)t 4.41 (2H. d. J = 5.5 Hz), 2.01 (3H( s). 2-18 •3 Η π 'H -NMROOO MHz, DMSO-de) δ: 13.21 (1H. s). 11.12 (1H. s), 9.89 (1H, s). 9.07 (1H. s). 7.88-7.76 (2H. m). 7.52 (2H ;d, J = 8.4 Hz). 7.34 (1H, s), 7.23 (2H( d, J = 8.4 Hz), 4,38 (2H, d, J = 5.1 Hz), 2.02 (3H, s). 2 -19 1H*NMR (300MHztDMSO-de) δ: 13.28 (1H, s). 11.17 (1H, 8). 9.23 (1H. s), 7.93-7.B2 (4H, m). 7.49-7.40 (5H, m) , 4.60 {2H, d, J = 5.6 Hz). 2-20 1H-NMR (300 MHz, DMSO-d6) δ: 13.15 (1H(s), 11.13 (1H. s), 8.93 (1H, s), 7.95-7.81 (1H, m), 7.39-728 (7H·m>. S.14 (1H, t. J = 6.8 Hz&gt;· 1.47 (3H. d· J =6.6 Hz). 2-21 'H- NMROOO MHz, E&gt;MSOde) δ: 13.15 (1H. s). 11.12 (1H, s), 8.93 (1H, s), 7.84-7.81 (2H, m). 7.53-7.17 (6H. m), 5.14 ( 1H, 1, J = 6.8 Hz). 1.47 (3H, d. J = 6.2 Hz). 2-22 OgO^i^ 'H-NMROOO MHz. DMSO-d6) δ: 11.18 (1H, s), 9.13 ( 1Hr t, J = 6.0 H2). B.12 (1H. d. J = 2.3 Hz). 7.87-7.80 (3H.m). 7.41 (2H, td. J = 6.8, 1.7 Hz). 725-7.18 ( 2H, m). 7.12-7.09 (2H, m), 7.01 (1H.d, J = 8.3 Hz), 4.41 (2H, d, J - 5.6 Hz). 2-23 'H-NMROOO MHz. DMSO-de δ: 10.99 (1H. s), 9.15 (1H, t, J = 6.2 Hz). 8.38 (1H. d, J = 2.6 Hz). 7.80 (1H, dd, J = 8.1, 2.6 Hz), 7.59 ( 1H. dd. J = 10.8. 8.3 Hz). 7.50 (1H. d. J = 8.1 Hz). 7.40 (1H. dd. J = 11.6, 7.5 Hz), 7.19 (1H. s). 4.45 (2H, d J * 5.9 Hz), 2.36 (3H, s). 2-24 ^^MROOO MHz, DMSO-de) δ: 11.20 (1H, s). 9.18 (1H, t, J = 6.1 Hz), 8.34 (1H , q. J = 2.2 H z), 7.88-7.77 (3H.m), 7.44 (1H, dd, J = 7.7, 4.8 Hz). 7.30 (1H, s). 4.50 (2H. d, J = 5.5 Hz).

315 318197 1322688 Table 29

Example Molecular Structure NMR 2-25 Na&quot; 1H-NMR (300 MHz. DMSO-de) δ: 8.69 (1 Η. br s), 8.35 (1H.d, J = 2.2 Hz), 7.81-7.76 (1H, m 7.59-7.44 (2H.m). 7.25-7.19 (1H.m). 6.52 (1H. s). 4.41 (2H, s).2.41 (3H. s). 2-26 1H-NMR (300 MHz DMSO-de) δ: 11.22 (1H. s). 9.22-9.12 8.91 (1H, s), 8.82-8.72 (1H, m), 8.50-8.40 (1H, m). 7.94-7.80 (3H( m) 7.36 (1H. s). 5.31-5.28 (1H. m). 1.51 (3H, s). 2-27 ^-NMROOO MHz, DMSO-d6) δ: 11^0 (Wt s). 9.16 (1H, t J - 5.8 Hz), 8.15 (1H, d, J = 4.6 Hz), 7.91-7.80 (3H(m), 7.37-7.34 (1H.m). 7.29 (1H. s)f 4.47 (2H, d. J = 6.0Hz). 2-28 9«3 (1 2HCI H όη^νν ^-NMROOO MHz, DMSO-de) δ: 11.24(1H, 8). 9.29 (1H, s). 8.68 (1H, d, J = 4.6 Hr), 8.35 (1H, d, J = 7.9 Hz). 7.89-7.79 (3H, m), 7.29 (1H, s). 4.58 (2H, d, J = 5.6 Hz), 2.80 (3H, d. J - 7.4 Hz). 2-29 1H-NMR (300 MHz, DMSO-de) δ: 13.29 (1H, s), 11.15 (1Ht s), 9.16 (1H, s), 7.86-7.31 (12H, m), 4.52 (2H, d, J = 5.9 Hz). 2-30 Η 1H-NMR (300 MHz. DMSO-de) δ: 8.37 (1H, s). 7.87-7.77 (2H, m&gt;. 7.28- 7.17 ( 5H. m), 5.40 (1H. dd, J = 8.4f 5.1 Hz). 5.16 {1H( s), 4.51 (1H. s). 3.10 (1H, dd; J = 16.3. 5.0 Hz). 2.93-2.85 (2H, m), 2.74-2.71 (1H, m). 2-31 (54^rV^ Η ^MROOO MHz. DMSO-de) δ: 13.24 (1Ht s). 11.11 (1H. s). 8.48 (1H s), 7.95-7.73 (2H.m), 7.49-7.15 (3Ht m), 5.40 (1H. t, J = 6.8 Hz). 5.10 (1H, s). 4.51 (1H, d, J = 2.6 Hz ), 3.10 (1H, dd. J = 16.1, 5.1 Hz). 2.93-2.85 (2H.m). 2.73 (1H, s). 316 318197 8 1322688 Table 30 Example Molecular Structure ' NMR 2-32 Q 2HC. „ 1H-NMR (300 MHz. DMSO*&lt;/e) δ: 11.22 (1Η· s), 9^8 (1H. t. J = 5.8 Hz). 8.73 (1H. s). 8.16-8.06 (4H m), 7.88-7.80 (3Hr m). 7.59-7.52 (3H, m), 727 (1H, s), 4.58 (2H,d,J= 6.0 Hz). 2-33 'H-NMROOO MHz. DMSO -de) δ: 11.69(1H, s), 11.17 (1H. s). 8.84 (1H, t, J = 5.9 Hz), 7.88-7.78 (2H, m), 7.27 (1H. s). 7.18 (1H d, J = 7.0 Hz). 5.98 (1H. d. J = 7.3 Hz). 4.17 (2H. d. J = 5.5 Hz). 2.16 (3H.s). The following compounds were prepared according to the aforementioned Preparation Method A-3. [Example 3-1]

Preparation of methyl-decylamine;

Amino-based) 1H-pyrazole-3 monocarboxylic acid (7 g), N-methylbenzylamine (ml) and ^1-pyridyl triazole hydrate (43 mg) in NN-dimethyl EDC hydrochloride (5 () mg) was added to the solution of liters, and the resulting mixture was stirred overnight to fox. Saturated aqueous sodium hydrogencarbonate (2 ml) and water (5) were added to the obtained mixture. [Example 3-2]

318197 317 丄J厶厶uoo 丄J厶厶uoo 5-(2-chloro-4· 5-. Preparation of amine pyrazole-3-carboxylic acid benzyl sulfide

5-(2. gas _4,5-difluoro-benzyl aryl group such as ketone-3 citric acid (7 〇 mg), benzylamine (〇〇 28 ml) and ^ prepared in the first step of Example 1 Ethyl benzodiazepine (45 mg) was added to a solution of n, n-dimethyl ketoamine (1 ml) with EDC hydrochloride (50 g), and the mixture was obtained at room temperature overnight. 0. 1 N aqueous sodium hydroxide (1 ml) and then water (3 ml) was added to the obtained reaction mixture, and the solid formed was filtered to give the title compound (66 mg) as white solid. 3-53 was prepared in the same manner as in the above Example 3-1 to Example 3-2. 318 318197 1322688 Table 31 Molecular structure formula NMR 3-1 1H-NMR (400 MHz. DMSO-de) δ: 13.29 (1H s). 11.44 (02H.brs). 11.19 (0.5H. brs). 11.14 (0.3H, brs). 7.95-7.75 (2H.m), 7.45-7.23 (5H.m). 7.00 (0.5H, m). 6.77 (0.3H. m). 6.44 (0.2H. m). 5.11 (0.3H, m). 4.82 (0.6H, m). 4.70 (11H. m). 3.17 (1.7H. s), 2t94 (0.9 H, s). 2.86 (0.4 H. s). 3-2 1H-NMR (400MHz, DMSO-d6) δ: 13.24 (1H.s)t 1115 (1H. s). 9.14 (1H. t J = 6.0 Hz). 7.86-7. (2H, m). 7.38-7.31 (5H. : 13.41 (1Ht s). 11.23 (1H, s), 10.30 (1H. s). 7.89-7.79 (4H. m), 7.62 (1H. s). 7.40-7.32 (2H, m). 7.12 (1H. m). 3-4 3 Η 'H-NMRC^O MHz. DMSO-de) 6:13.20 (1H, s). 10.91 (1H. s), 7.81-7.67 (2Ht m). 7.51-7.43 (3H. m). 7.40-7.36 (2H.m), 5.48 (1H.s), 3.32 (3H.s). 3-5 1H-NMR (400MHz. DMSO-d6) δ: 13.14 (1H, s), 11.17 ( 1H. s)t 7.87-7.79 (2Hf m). 6.81 (1H. s), 3.64-3.57 (4H, m), 1.68-1.52 (6H.m) 3-β 0 1H-NMR (400 MHzf DMSO-de δ: 13.16 (1H. s). 11.18 (1H. s), 7.86-7.78 (2H. m). 6.83 (1H. d. J = 1.6 Hz). 4.31 (1H. m), 4.09 (2H. q J = 6.8 Hz). 3.10-2.90 (2H, m). 2.70-2.65 (2Ht m). 1.94-1.91 (2H. m). 1.58-1.52 (2H, m), 1.19 (3H. t, J = 6.8 Hz). 3-7 nrSyVV^ Η,ΟΤ*^ W~J 0 Cl 'H-NMRMOO MHz. DMSOde) δ: 13.17 (1H. br s). 11.19 (1H. brs). 7.86-7.83 (2H. m). 6.83 (1H, br s), 3.70-3.65 (4H. m), 2.36-2.34 (4H, m). 2.20 (3H, s). 3-8 MHz, DMSO-de) δ: 11.21 (1H Brs), 7.87-7.80 (2H, m), 6.76 (1H. br s). 4,36-4.05 (2H. m), 3.32-2.98 (2H, m). 2.57 (1Ht m). 1.93-1.89 (2H. m), 1.55-1.48 (2H, m ).

319 318197 1322688 Table 32

Example molecular structure NMR 3-β Η 'H-NMRi^O MHz. DMSCWe) δ: 13,17 (1H. s), 11.13 (1Ht s), 8.67 (1H. m), 7.86-7 J9 (2H. m), 7.36-7.18 (6H.m). 3.47 (2Ht m). 2.85 (2H. t, J = 7.2 Hz). 3-10 3 H MHz. DMSOde) δ: 13.17 (1H. m>· 11.17 ( 1H. brs) ( 7.92-7.84 (2H. m). 7.29-7.23 (5H. m), 6.93 (1H. m). 3.92 (1H. m). 3.69 (2H. m) ( 3.25-2.89 (4H. m). 3-11 ^rJLQJli4rF 'H-NMRC^ MHz, DMSO-ds) δ: 13.1B (1H, s). 10.89 (1H, s), 7.77 (1Ht dd, J = 10.4, Hz). 7.69 ( 1H. dd, J = 10.8. 8.4 Hz), 7.52-7.44 (3H, m). 7.34-7.32 {2H, m). 5.40 (1H. br s), 3.81 (2H, q, J = 7.2 Hz)t 1.12 (3H, t. J = 7.2 Hz). 3-12 ocArV^ H 'hl-NMRtAOO MHzt DMSO-^β) δ: 13.21 (1H, 8). 11.20 (1H. s). 7.87-7.80 (2H. m). 7.26-7.15 (4H.m). 6.97 (1H. s). 477 (2H(m). 3.88 (2H.m)t 2.93 (2H.m). a-13 1H-NMR (400 MHz, DMSO-de) 5: 13.28 (1Ht s), 11.15 (1Ht s). 9.40 (1H, d, J = Hz), 7.86-7.79 (2H.m). 7.52-7.35 (6H. m). 5.67 (1H d. J = 7.2 Hz). 3.β7 (3H. s). &gt;-14 ^-NMRinOO MHz. DMSO-de) S: 13.28 (1H, S), 11.15 (1H. s). 9.40 (1H, d. J = Hz). 7.86-7.79 (2H. m). 7.52-7.37 (6H. m). 5.67 (1H. d, J = 7.2 Hz). 3.67 (3H, s). 3-15 H 1H-NMR (400 MHz, DMSO-de) 5: 13.25 (1H. s s). 11.09 (1H. s). 7.83-7.74 (2H.m) r 7.25 (1H.d, J = 6.4 Hz), 7.18-7.04 (3H, m). 6.45 (1H. s). 3.85 (2H. t, J = 6.4 Hz). 2.80 (2H. t, J = 6.4 Hz), 1.95 (2H. m). 320 318197 1322688 Table 33

Example molecular structure NMR 3-16 'Η-ΝΜΡ (400 MHz, DMSO-de) δ: 13.16 (1H. s)t 10.86 (1H.s). 7.77 (1H. dd. J = 10.4, 7.2 Hz). 7 69(1H. dd. J - 10 0. 8.4 Hz), 7.51-7.43 (3H. m). 7.34-7.32 (2H, m)t 5.39 (1H. br s). 3.75 (2H. t, J = 7.2 Hz). 1.53 (2H.m). 0.89 (3H. J = 7.2 Hz). 3-17 ^-NMRCAOO MHz. DMSO-de) δ: 13.16 (1H. s). 10.68 (1H. s). 7.77 (1H. dd. J = 10.4, 7.2), 7.69 (1H. dd. J = 10.0, 8.4), 7.51-7.43 (3H, m), 7.33-7.31 (2H. m). 5.39 (1H, br s) , 3.79 (2Ht t, J = 7.2 Hz) t 1.50 (2H, m), 1.34 (2H, m). 0.88 (3Hf t, J = 7.2 Hz). 3-18 , lhiJ 0 Cl H 'H-NMRCAOO MHz , DMSO-de) 5:13.16 (1H. br s), 10.88 (1H, s)t 7.77 (1H. m), 7.69 (1H. m), 7.51-7.45 (3H. m). 7.33-7.31 {2H , m). 5.38 (1Ht br s)t 3.78 (2H. t. J = 7.6 Hz), 1.56-1.47 (2H, m) (1.34-1.28 (4H. m), 0.85 (3H. m). 3- 19 1H-NMR (400 MHz. DMSO-de) 5:13^3 (1H, s), 11.14 (1H, s). 9.43 (1H. d. J - 8.8 Hz). 7.85-7.78 (2H, m) , 7.55 (1H, m), 7.39-7.35 (8H. m). 7.31-7.26 (2Hf m), 6.39 (1H. d, J = 8.8Hz). 3-20 MHz, DMSO^e) δ: 11^ 5 (1H, s), 9.41 (1H, brs), 8.79 (1H, m), 8.40 (1H, m), 7.88-7.79 (4H, m), 7.29 (1H. s), 4.73 (2H. m). 3-21 crV^V^ ^H4im{AOO MHz, DMSO-de) δ: 11.25 (1H, s). 9.45 (1H, br s), 8.85 (2Hf d, J = 9.6 Hz), 7.92 (2K d, J -9.6 Hz), 7.88-7.80 (2H.m), 7.27 (1H, s). 4.79 (2H.m). 3-22 1H-MMR (400 MHz. DMSO-d^S: 13.15 (1H. m), 11.14 (1H, s), 8.85 (1H, d. J = 8.0 Hz), 7.B6-7.79 (2H, m), 7.4a (1H. m) ( 7.39-7.31 (4H, m). 7.24 (1H, m). 5.04 (1H.m) ( 4.95 (1H(t, J = 5.6 Hz). 3.74-3.62 (2H, m). 3-23 'H-NMRCAOO MHz, DMSO-de) δ: 13.16 (1H. m). 11.14 (1H, s). 8.85 (1H, d. J = 8.0 Hz). 7.8S-7.79 (2H. m), 7.48 (1H. m). 7.39-7.31 (4H. m). 7.24 ( 1Ht m)( 5.05 (1H. m). 4.95 (1H, t J = 5.6 Hz), 3.7«.62 (2H. m). 321 318197 1322688 Table 34

EXAMPLES Molecular Structures NMR 3-24 'H-NMR (400 MHz. DMS0-de) 6: 13.18 (1H.S), 11.11 (1H, s), 9.14 (1ΗΛ J = 6.0 Hz), 7.85-7.78 {2H , m), 7.31 (1Ht d, J = 1.6 Hz). 7.14 (2H, dt J = 8.4 Hz), 6.69 (2H. d. J = 8.4 Hz). 4.31 (2H, dt J = 6.0 Hz). 2.86 (6H, s). 3-25 Η 'H-NMRCAOO MHz. DMSO-de) 0; 13.24 (1H.S), 11.15 (1H. s). 9.08 (1H, t J = 5.6 Hz). 7.86-7.79 (2H. m), 7.58 (1H.m). 7.34 (1H. d. J = 2.8 Hz)t 6.41 (1H. m). 6.29 (1H, d. J = 2.8 Hz). 4.43 (2H. d. J = 5.6 Hz). 3-26 Η MHz, DMSO-de) 6:13.26 (1H.s), 11.14 (1H. s). 9.24 (1H. brs), 7.77-7.75 (2H, m), 7.40 ( 1H. m), 7.33 (1H, m). 7.02 (1H. m), 6.97 (1H. m)t4.60 (2H.m). 3-27 MHz, DMSO-de) δ: 13.38 (1H. br s). 11.56 (0.45H, brs). 11.16 (0.55 brs). 9.63 (0.55H, br s). 9.35 (0.45H. br s). 8.34 (0.45H. m). 7.94-7.83 (1.55H. m). 7.β3 (0.45H. m). 7.48 (0.55H, m). 7.21-7.10 (2.55H, m)f 6.98 (1H. m). 6.54 (0.45H, m). 3.92 (1.35H , brs). 3.85 (1.65Hfbrs). 3-28 ^H-mRiAOO MHz. DMSO-de) δ: 13.13 (1H, s). 10.86 (1H. s). 7.78 (1H. dd, J = 10.0.6 .8 Hz). 7.70 (1H. m), 7.44 (1H, m)t 7.33 (1H. dd. J = 7.6, 1.2 H2). 7.18 (1H, d, J = 8.4 Hz). 7.05 (1H. m 5.51 (1H. bf s), 3.74 (3H. S). 3.23 (3H. s). 3-29 ^Onr^ MHz, DMSO-de) δ: 11.16 (1H, 8), 9.14 (1Ht m) 7.86-7.81 (2H, m), 7.55-7.41 (4H. m), 7.25 (1K s). 4.43 (2H. m), 3.05 (6H, m). 3-30 MHz, DMSO-de) δ: 13.21 (1H, brs), 11.12 (1H. br s)f 9.04 (1H, br s). 7.76-7.90 (2H. m), 7.35 (1H, br s). 6.97 (1H, m). 6.52-6.46 (3H.m). 5.23 (2H, brs). 4.61 (2H.m). 3-31 ^-NMRCAOO MHz. DMSO-de) δ: 13.19 (1H.s). 11.11 (1H. s). 8.96 ( 1H, brs). 7.85-7.78 (2H.m). 7.32 (1H. br s). 6.99 (2H. d. J = 7.6 Hz). 6.55 (2H. d. J = 7.6 Hz). 5^8 ( 2H, br s). 4.27 (2H. d. J = 5.6 Hz). 322 318197 1322688 Table 35

Example molecular structure NMR 3-32 Η 'H-NMRMOO MHa DMSO^s) δ: 13_22 (1H. brs}, 11.14 (IH.brs), 9.00 (1H, brs). 7.86-7.79 (2H. m). 7.38 (1H, br s), 7.25 (1H. m), 7.18-7.13 (3H, m). 4.43 (2H, df J = 6.0 Hz). 2.32 {3H, s). 3-33 'H-NMRC^ MHz, DMSO-ds) 6:13.22 (1H, br s). 11.14 (1H# brs). 9.10 (1H. brs). 7.86-779 (2H. m), 7.35 (1H. br s). 7.22 (1H .m). 7.13-7.06 (3H, m). 4.41 (2H( d. J = 6.0 Hz). 2.29 {3H. s). 3-34 ^OrV^V^ h-NMR M00 MHz· DMSCWe) δ: 13.21 (1H. s)· 11.13 (1H. 5), 9.07 (1H, m). 7.85-7.79 (2H. m), 7.35 (1H, s), 7.13 (1H. m). 6.70 (1H. m) 6.62-6.60 (2H, m)t 4.38 (2H, d. J = 5.6 Hz). 2.88 (6H, s). 3-35 1H^NMR (400 MHt DMSCWe) δ: 13*25 (1H, 8) _ 11*16 (1H, br s). 9.02 (1H, br s). 8.07 (1H. d. J = Hz), 7.8S-7.80 (2H. m). 7.55 (1H. d, J = 7.2 Hz ), 7.38 (1H. br s), 6.97 (1H. ckJ, J = 7.2, 5.2 Hz). 4.38 (2H, d. J * 5.6 Hz). 3.92 (3H, s). 3-36 1H-NMR ( 400 MHz, DMSC^de) δ: 13.27 (1H, s). 11.16 (1H. brs). 9.13 (1H, brs), 7.86-7.80 (2H, m), 7.53-7.29 (5H, m). 4.52 ( 2H. d, J = 5.6 Hz). 3-37 MHz. DMSO-de) δ: 13.26 (1H, 8). 11.16 (1H. brs). 9.17 (1Ht brs), 7.86-7.79 (2H, m). 7.40-7.28 (5H , m), 4.45 (2H, d, J = 6.0 Hz). 3-38 ^-NMROOO MHz. DMSO-de) δ: 13.24 (1H, S). 11.14 (1H. s), 9.10 (1H. m) 7.94 (1H. s). 7.86-7.69 (3Ht m). 7.60 (1H. m). 7.50 (1H, m). 7^8 (1H. m). 4,50 (2H, d, J = 5.7 (2H. s) 5: 13.09 (2H. 7.88-7.80 (3H.m). 7.56 (1H, d( J = 8.0 Hz). 7.47 (1Ht m)( 7.31 (1H. br s). 4.50 (2H. d, J = 6.0 Hz). 323 318197 1322688 Table 36 Example Molecular Structure NMR 3-40 1H-NMR (300 MHz. DMSO-de) ^ 13.29 (1H. s). 11.17 (1H, s). 9.26 (1H. s). 8.74 (1H, s). 8.00 (1H. d. J = 7.4 Hz). 7.90 (1H. d, J = 7.9 Hz). 7.83 (2H. q. J = 7.9 Hz). 7.35 (1H, s), 4.57 (2H. d, J = 5.6 Hz). 3-41 'H-NMR (400 MHz, DMSO»de&gt; δ: 13.25 &lt;1H. brs&gt;. 11.16 (1H, brs). 9.00 (1H, brs). 8.05 (1H, dd, J = 5.2, 2.0 Hz), 7.86-7.80 (2H, m). 7.53 (1H. d. J = 6.β Hz). 7.38 (1H, br s), 6.95 (1H. dd, J = 6.8, 5.2 Hz). 4.40-4.34 (4Ht m), 1.34 (3Ht LJ = 7.2 Hz). 3-42 Η 1H-NMR (400 MHz. DMSO-ds) δ: 13.16 (1H, br s), 11.15 (1H. brs), 8.44 (1Ht brs). 7.86-7.80 (2H, m). 7.23 (1H, br s). 3.33 (2H, t J = 6.8 Hz), 2.39 (2H, t. J = 6.8 Hz ), 2.17 (6H, s). 3-43 as e ^01 η rY 'H-NMRC^O MHz, DMSO-c/e) δ: 13.24 (1H, br s), 11.22 (1H. br s). 10.24 (2H. br s), 7.89-779 (2H, m) ( 6.94 (1H, br 5). 3.80-3.33 (6H, m). 2.β3 (6H, m) ( 1.20 0H, called 3-44 H3C^S«3 MHz. DMSO-de) 5: 13.15 (1H, br s). 11.17 (1H, brs). 7.86-7.81 (2H.m). 6.81 (IH.bre), 4.04 (1H. m) 3.55-3.48 (2H, m). 2.42 (2H, t J = 7.2 Hz), 2.20 (6H. s). 1.81-1.12 (10H, m). 3-45 ^H^NMRWOO MHz· DMSCWe) δ: 13.26 &lt;1H.s&gt;. 11.16 (1H, 8), 9.16 {1H, t J = 6.0 Hz), 6.34 (1Η» d. J = 6.4 Hz), 7.86-7.80 (2H. m). 7.38 (1H , s). 6.88 (1H, S). 6*87 (1H, d. J = 6.4 Hz) t 4.46 (2H. d. J = 6.0 Hz). 3.81 (3H. s). 3-4β MHz, DMSO -de) 5: 13.21 (1H. br s). 11.15 (1H, br s), 8.91 (1H, br s). 7.8S-7.80 (2H, m). 7.52 (1H, d, J = β.4 Hz), 7.35 (1H. Br s), 6.36 (1H. d, J = 8.4 Hz), 4.30 (2H, d, J = 5.6 Hz). 3.92 (3H. s). 3.85 (3H, s).

324 318197 1322688 Table 37 Example Molecular Structure NMR 3-47 'H-NMRiAOO MHz, DMSOde) δ: 13.25 (1 Η. s) 11.15 (1Κ 5). 8.95 (1Η, m), 7.86-7.Θ0 (2Η , m). 7.39 (1Η( br s). 7.24-7.20 (2H. m). 6.92-6.98 (2H, m), 4.89 (2H, s). 4.49 (2H, d. J = 6.0 Hz). 3.72 (3H. s). 3-48 'H&gt; NMR (400 DMSOds) 6: 13.15 (2H. br s&gt; 11.17(1H, 5). 8.93 (1Hf brs). 7.87-7.80 (2H, m). 7.36 ( 1H. br s), 7.24-7.17 (2H. m), 6.96-6.8B (2H. m). 4.76 (2H. s), 4.48 (2H. d. J = 6.0 Hz). 3-49 'H- NMRC^O MHz. DMSO-d6) δ: 13.19 (1H. s), 10.94 (1H. s). 9.07 (1H. t J - 5.6 Hz). 8.12 (1H, d. J = 2.0 Hz). 7.66 ( 1Ht dd. J = 8.8, 2.0 Hz). 7.66 (1H. dd. J = 10.4. 8.8 Hz), 7.38 (1H. dd. J = 11.6, 7.6 Hz), 7.32 (1H. s)t 6.80 (1H, d. J = 8.8 Hz). 4.37 (2H( d( J = 5.6 Hz), 3.83 (3Ht s)( 2.34 (3Ht s). 3-50 'H-NMRi^ MHz. DMSO-de) δ: 13.23 ( 1H. s), 11.12 (1H. b). 9.09 (1H. t J = 5.6 Hz). 8.12 (1H. d. J = 2.4 Hz), 7.72 (1H. d, J =*= 2.4 Hr). 7.66 (1Ht dd. J = 8.4, 2.4 Hz), 7.57 (1H. d. J = 8.4 Hz). 7.51 (1H. dd. J = 8.4. 2.4 Hz) 7.32 (1H, m). 6.80 (1H. d, J = 8.4 Hz). 4.37 (2H. d# J = 5.6 Hz), 3.83 (3H, s). 3-51 〇«3 'H-NMRC^ MHz DMSO-d^O: 13.16 (1H. S). 11.19 (1H, s). 8.51 (1H. m)f 6.11 (2H. s). 7.89-7.77 (2H, m). 7.30 (1H. br 8 ), 4.41 (2H.m), 3.90 (6H. 8). 3-52 :^τΛγν^ 'H-NMRC^ MHz. OMSO-d5) 6:13.22 (1H. s). 10.95 (1H. s), 9.04 &lt;1H, t J = 5.6 Hz). 7.57 (1H, m). 7.39 (1H, m), 7.33 (1H. s). 4.39 (2H, d. J = 5.6 te). 2.39 (3H, 8 2.32 (3H, s). 2.08 (3H. s). 3-53 Factory Η 'H-NMRt^O MHz, DMSO-de) δ: 13.2β (1H. s)t 11.19 (1Ht s), 9.06 (1H.t. J = 5.6 Hz), 7.93 (1H. d. J = 6.4 Hz). 7.77 (1H, d, J = 8.8 Hz), 7.33 (1H. s). 4.39 (2H, d, J = 5.6 Hz), 2.32 (3H. s), 2.07 (3H. s).

325 318197

丄J厶ZrUOO The following compounds were prepared according to the aforementioned Preparation Method B. [Example 4-1] ^ -~~^~~^~ Benefit, 5~~ - pro i~~ This is a simmered face, 1U. -Pyrazol-3-indole [4-methylcarbonylamine 1 - jasmine lacto-phenyl)-methyl-gj|face step 1: 4 bis [methyl-(5-nitrogen

〇NO. CH, N-N 加入In a solution of 5-nitro-3-oxazolecarboxylic acid (400 mg) in chloroform (1 ml), added with sputum under ice cooling (〇·27 ML) and N,N-dimercaptocaramine (1 drop). After stirring overnight at room temperature, the resulting reaction mixture was concentrated under reduced dust to give a 5-nitro-3-[rho] ratio. Then add triethylamine (1.2 ml) to a suspension of 5-nitro-3-nt β-reactive chloro and 4-nonylaminobenzoic acid hydrazine (410 mg) in EtOAc (25 mL) The resulting mixture was stirred overnight at room temperature. The obtained reaction mixture was washed successively with saturated aqueous sodium hydrogen sulfate, brine, and brine, The residue was purified by EtOAc EtOAc (EtOAc:EtOAc) Free of 2: 4-(5-Amino- Η-pyridin-3-carbonyl)-fluorenyl-amine a l-methyl phthalate; 326 318197 1322688

NH, 4- 4-[Indolyl-(5-nitro-1Η-pyrazole-3-carbonyl)-amino]- benzoic acid oxime ester (394 mg) in tetrahydrofuran (1 mL) EtOAc. 5% palladium-carbon (60 mg) was added to the solution of 〇 ml). The resulting mixture was stirred overnight at room temperature under a hydrogen atmosphere. The catalyst was removed by filtration. 13: 5-(2-gas-4, 5-difluoro-stupylcarbylamine, -1H-pyrazole-3-! Ι·Ι1τ曱 oxycarbonyl-stupyl-yl-decylamine;

F is added to a solution of 4-[(5-amino-1 Η-pyrazole-3-carbonyl)-methyl-amino]-benzoic acid decyl ester (244 mg) in tetrahydrofuran (5 ml). 1. 1 ml), 2 -milk-4,5_-purine benzoic acid (0.135 ml) obtained in the first step of Reference Example 1 was added dropwise under ice-cooling. After stirring overnight at room temperature, the reaction mixture was concentrated under reduced pressure. &lt;RTI ID=0.0&gt;&gt; (228 mg) in white crystals. [Example 4-2]

318197 327 1322688 Preparation of a certain methionine-guanamine;

5-(2-Gas-4,5-difluoro-benzoylamino)-1Η-pyrazole-3-carboxylic acid (4-methoxycarbonyl-phenyl)-prepared according to Example 4-1 To a solution of methyl decylamine (100 mg) in MeOH (2 mL) EtOAc (EtOAc) The title compound (78 mg) was obtained as a white solid. [Example 4-2-1] 17{[5-(2-oxo-4.5-difluoro-anthracene-yl-amino)-111-pyrazole-3-heterobiphenyl-amine-anthracene-mole Preparation of sodium formate salt;

5-(2-Chloro-4,5-difluoro-benzylidenylamino)-1Η-pyrazole-3-carboxylic acid (4-carboxyphenyl)-fluorenyl-based according to Example 4-2 A suspension of 4N aqueous sodium hydroxide (0. 025 ml) was added to a suspension of decylamine (49. 4 mg) in ethanol (EtOAc). The solution was allowed to stand at rt. The compound examples 4-3 to 4-48 shown in the following table were produced in the same manner as in the foregoing examples 328 318197 1322688 4-1 to the examples 4-2-1. Table 38

329 318197 1322688 Table 39

Example molecular structure NMR 4-7 'Η-ΝΜβΟΟΟΜΗζ, ΟΜβΟ-ΐΙβ) (S: 13.19 (1H. br s). 11.09 (1H. br s). 9.11 (1H. br s). 7.72 (1H. br s 7.58 (1H. d. J = 7.7 Hz). 7.51 (1H. d. J = 7.7 Hz), 7.34-7.20 (6H, m), 4.44 (2H. d, J = 5.9 Hz). 4-8 οτΛ^ν^1 ^MROOO MHz. DMSO-de) S : 13.20 (1H. br s), 11.11 (1H, br s). 9.12 (1H. t. J = 5.7 Hz), 7.58 (1H. q, J = 4.5 Hz). 7.48 (1H. dd. J = 8.6, 3.1 Hz), 7.41-7.19 (7Ht m)t 4.45 (2H. d. J = 5.9 Hz). 4-β MHz. DMSO-de) 6: 13.35 (1H, s s). 10.93 (1H, s), 7.92-7.68 (2H, m), 7.42-7.17 (10H, m). 5.47 (1H, br s), 5.04 (2H. s). 4- 10 Η 'H~NMR (400 MHz· DMSO^e) δ: 13.00 (1H· br s). 11.11 (1H, brs), 8.58 (1H. bre), 7.86-7.79 (2H, m), 7.47 (1H Br s)( 7.39-7.37 (2H, m), 7.33-7.23 (2H, m). 7.14 (1Hr t, J = Hz). 1.68 (6H, e). 4-11 0 'H&gt;NMR(400 MHz· DMSOdJ δ: 13.30 (1H. br s), 10.92 (1H, br s), 7.78 (1H, m), 7.71 (1H, m). 7.47- 7.39 (5Ht m). 5.44 (1H. br s) , 4.64 (2H, s). 3.45- 3.39 (4H, m), 1.58-1.44 (6Ht m). 4-12 H, H-NMR (300 MHz. DMS &amp;ds) δ: 13.16 (1H. br s). 10.89 (1H, br s)f 9.10 (1H, br s). 7.39-7.17 (9H. m). 4.44 (2H, d, J = 5.5 Hz) , 2.34 (3H, s). 330 318197 1322688 Table 40

Example molecular structure NMR 4-13 Η 'H-NMROOO MHz. DMSO&lt;/6) 0: 13.16 (1H, br s). 10.93 (1H, brs). 9.10 (1H. brs), 7.55-7.18 (9H, m), 4.45 (2H.d, J = 5.9 Hz). 2.35 (3H, $). 4-14 1H-NMR (300MHz, DMSO-de) ¢: 13.09(1H. brs). 10.63 (1H. br s 9.07 (1H. br 6), 7.52-7.18(7H.m). 6.83 {2H, br s). 4.44 (2H. d. J = 5.9 Hz). 3.79 (3H. s). 2.39 (3H. s). 4-15 CnrSrV?&quot; Η ^MROOOMHz.DMSO-de) ί: 13.16 (1Ht br s). 10.88 (1H, br s). 9.10 (1H, br s). 7.5&amp;-7.16 (9H , m), 4.45 (2H, d. J = 6.2 Hz). 2.38 (3H. s). 4-1β 'H-NMROOO MHz, DMSO-de) 13.22 (1H, br 8), 10.47 (1H. br s 9.11 (1Hr br s). 7.53 (1H. dt J = 9.5 Hz) ( 7.40-7.20 (8H, m), 4.43 (2H, d, J = 6.2 Hz), 3.93 (3H, s). 4- 17 'Η-ΝΜΗΟΟΟΜΗζ,ΟΜδΟ^β) d :13^2 (1H.br s). 10.49 (1H. br s). 9.12 (1H. t. J = 57 Hz), 7.69 (1H. d, J = Z6 Hz). 7.56 (1H. dd, J = 8.8.29 Hz), 7.40-7.18 (7H.m). 4.45 (2H. d. J = 5.9 Hz). 3.93 (3H. s). 4-18 π </ RTI> <RTIgt; 7.2 Hz). 7.69 (1H. dd, J = 10.4, 8.4 Hz). 7.49-7.44 (3H. m). 7.36-7.34 (2H. m). 5.38 (1H, br s). 3.93 (2H. t, J = 6.0 Hz). 3.54 (2H. t J s 6.0 Hz). 3.40 (2H. q, j = 6.8 Hz) t 1.07 (3H, t. J = 6.8 Hz). ♦-1Θ 'H&lt;NMR(300 MHz. DMSO^) δ: 13.19 "1H· br s). 10.82 (1H. brs), 9.13 (1H, l, J - 4.5 Hz), 7.46 (1H. d. J = 4.6 Hz), 7.40-7.14 ( 8H, m). 4.45 (2H, d. J = 5.9 Hz). 3.31 (3H, s). 331 318197 1322688 Table 41

Example molecular structure NMR 4-20 'H-NMROOO MHz, DMS0-de)«: 13.24 (1H. brs), 11.07 (1H. br s), 9.13 (1H, t, J = 4.5 Hz). 7.70 (1H , t. J = 2.7 H2). 7.60 (1H. dd. J = 4.7t 2.7 Hz). 7.41-7.24 (7H. m). 4.46 (2H. d. J = 4.5 Hz). 4-21 Η 'H -NMROOO MHz, DMSO-de) 6:13.29 (1H. brs), 11.42 (1Ht br s). 9.15 (1H, br s). 7.77 (1H. brs), 7.34-7.24 (7H. m). 4.45 ( 2H, d, J = 6.2 Hz). 4-22 1H-NMR (300 MHz, DMSO-de) 6 : 13.24 (1H. br s). 11.15 (1H. br s). 9.14 (1H, br s). 7.57-7.19 (9H.m), 4.43 (2H, d(J = 5.5 Hz). 4-23 Η3°ν^ΝΗ 'H-NMRC^ MHz, DMSOde) 5:13.22 (1Ht br s)t 10.91 (1H , s), 8.00 (1H, t. J = 5.2 Hz). 7.78 (1H, dd. J = 10.0. 7.2 Hz), 7.70 (1H. cid, J = 10.8.8.4 Hz), 7.50-7.42 (5Ht m 5.45 (1H. br s), 4.34 (2H, s), 3.10 (2H. qt. J = 7.2, 5.2 Hz). 1.01 (3H, U~72 Hr). 4-24 HjC^J h-tj 0 Cl C«3 ,H-NMR (400 MHz, DMSCMe) δ: 13.17 (1H. s). 10.87 (1Ht s) ( 7.77 (1H, dd, J = 10.4, 7.2 Hz), 7.68 (1H. dd, J = 10.4, 8.4 Hz), 7.51-7.42 &lt;3H# m). 7.35-7.34 (2H, m). 5.37 (1H, br s). 3.68 (2H. d. J * 7.6 Hz), 1.78 (1H, qt, J = 7.6. 7.6 Hz). 0.91 (6H, d. J = 7.6 Hz). 4-25 &quot;aSA) H 'H-NMRCAOO MHz. DMSO-de) δ: 13.22 (1H. s). 10.89 (1H, s), 7.77 (1H. dd. J = 10.0.6.8 Hz). 7.69 (1H. dd. J = 10.0, 8.4 Hz). 7.52-7.44 (3H. m) 7.36-7.35 (2H, m). 5.38 (1H, s), 4.03 (2H. t. J = 7.2 Hz). 3.55 (3H( s). Z62 (2Ht t J = 7.2 H2). 332 318197 1322688 42

EXAMPLES Molecular Structures NMR 4-26 N-fj 0 Cl 0 'H-NMRtW MHz, DMSO-&lt;/e) δ: 13.17 (1H. s) ( 10.B9 (1H, 5), 7.77 (1H, cW J = 10.0, 6.8 Hz). 7.69 (1H, dd. J = 10.4, 8.4 Hz), 7.51-7.43 (3H, m). 7.35-7.34 (2Ht m). 5.40 (1H. s), 4.03 (2H , q . J = 7.2 Hz). 3.82 (2H, t, J = 7.2 Hz). 2.37 (2H. t. J = 7.2 Hz). 1.77 (2H, H. J = 7.2, 7.2 Hz). 1.16 (3H , t. J = 7.2 Hz). 4-27 1 NMR (400 MHz. DMS04ft) δ: 13.19 (1H· br s}· 12.34 (1H. br s). 10.90 (1H, s). 7.77 (1H. Dd. J = 10.0.72 Hz). 7.69 (1H. dd. J = 10Ό. B.4 Hz). 7.51-7.44 (3Ht m). 7.37-7.35 (2H. m). 5.40 (1H. br s) 4.00 (2Ht t. J = 7.2 Hz). 2.55 (2H, t. J = 7.2 Hz). 4-ZB 'H-NMRCAOO MHz, DMSO-de) δ: 13.17 (1H. br s), 12.08 (1H Br s)t 10.88 (1H. s). 7.77 (1H, dd. J = 10 4.12 Hz), 7.69 (1H, dd, J = 10.4, 8.8 Hz), 7.51-7.43 (3H, m). 7.35- 7.33 (2H(m), 5.40 (1H. brs), 3.62 (2H,t (J = 7.2 Hz), 2^9 (2H, t, J = 7.2 Hz), 1.75 (2^3⁄4 J = 7.2, 7.2 Hz). 4-29 ο-ΛτΛ^ ^-NMROOO MHz, DMSO-c/e) δ: 12.51 (1H( br 8), 8.42 (1H. t, J = 4.5 Hz). 8.05 (1H. s ) f 7.30-7.19 (5H, m). 6.17 (1Ht s) ( 4.39 (2H. d. J = 4.8 Hz). 3.31 (3H, s). 4-30 Cn^Vi 1H-NMR (300MHz.DMSO- De)) ¢: 13.30(1H, br s) J1.68 (1H, br s). 11.01 (1H, br s), 9.12 (1H, br s). 7.60 {1Ht br s). 7.39-7.19 (6Hf m), 7.05 (1H, q, J = 4.5 Hz), 6.93 (1H. d, J = 6.6 Hz), 4.46 (2H. d. J = Hz). 3.76 (3H. 6). 4-31 (χΛ ^νί Η 1H*NMR (300 MHz. DMSO-de) δ : 13.29 (1H. br s). 11.84 (1H. brs). 10.92 (1H, br s). 9.12 (1H, br s). 7.81 (1H d, J = Hz), 7.39-7.19 {7H. m). 7.02 (1H· q_ J = 4.5 Hz)·45 (2H_d, J = 6'2 Hr)* 4-32, H-NMR( 300MHz.DMSO-de) 5:13.20(1H, s). 11.14 (1H. s)( 9.13 (1H, d. J = 5.5 Hz), 7.79-7.70 (2H, m). 7.64 (1H. t J = 6.2 Hz). 7.39-7.19 (6H. m). 4.44 (2H, d, J = 5.9Hz). 333 318197 1322688 Table 43

Example molecular structure NMR 4-33 'H-NMROOO MHz. DMSO-de&gt; 6:13.20 (1H, br s). 11.18 (1H, br s). 9.12 (1H, br s). 7.94-7.86 (1H, m), 7.66-7.47 (2H.m). 7.39-7.20 (6H, m), 4.44 (2H. d. J = 6.2 Hz). 4-34 1H-NMR (400 MHz. DMSO-de) δ: 13.20 (1H, s), 10.88 (1H. s) ( 7.77 (1H. dd ( J = 10.4, 7.2 Hz). 7.69 (1H. dd. J = 10 4. 8.4 Hz). 7.52-7.45 (3H. m) 7.35-7.33 (2H, m), 5.38 (1H, br s). 3.95 (2H, l, J = 5.6 Hz). 3.49 (2H. t, J = 5.6 Hz). 3.31 (3H. s). 4 -35 QtV^yVx Η fH-NMR (300 MHz, DMSO-de) δ : 13.11 (1H, br s), 10.72 (1Hf br s). 9.12 (1H, br s), 7.40-7.10 (9H, m) , 4.44 (2H, d. J = 6.2 Hz). 2.33 (3H, e). 2.31 (3H. s). 4-36 'H-NMROOO MHz, DMSO-tf*) d: 7.40-7.15 (6H. m 6.92(1H. br s)t 5.99 (1H. s). 5.66 (1H, br s). 4.46 (2H, d. J = 6.6 Hz), 1.55(3H. $). 4-37 Crr^yV ? 'H-NMR (300MHz, OMSO-(/e)) e: 8.58 (1H, d. J = 1.8 Hz) f 8.44 (1H. t. J = 5.9 Hz). Θ.18 (1H. dd, J = 7.3.1.8Hz), 7.59 (1H. dd, J « 7.7,4.8 Hz), 7.32-7.18 [5H, m). β.94(1Η, br s). 5.75 (1H. br s), 4.46 ( 2H( d. J = 6.6Hz). 4 -38 Η ^MROOO MHz, DMSCMe) d: 13.32 (1H, br s), 10.58 (1H. br s), 9.15 (1H. br s), 8.72 (1H. br s), 8.14 (1Ht s). 7.85 (1H. 8). 7.42-7.18 (6H.m), 4.46 (2H. d. J = 6.6Hz). 4-39 〇rVLtrV?^ 'H-NMROOO MHz. DMSO-de) δ: 13.26 (1Ht br s). 11.25 (1H. br s). 9.14 (1H. br s), 8.13 (1H. d( J = 7.7 Hz). 7.69 (1H. d. J = 8.1 Hz). 7.41-7.19 (6H. m ) ( 4.45 (2H. d, J = 5.9Hz). 334 318197 1322688 Table 44

Example molecular structure NMR 4-40 H ^ NMR CAOO MHz. DMSO-de) δ: 13.26 (1H. m), 10.95 (1H. s). 8.04 (2H. d. J = 8.4 Hz). 7.78 (1H. d J = 10.4.7.2 Hz), 7.71 (1H, dd. J = 9.6. 8.4 Hz). 7.48 (2H. d. J = 8.4 Hz). 5.57 (1H. br s). 4.32 (2H. q, J = 7.2 Hz). 3.84 (2H. t J = 7.2 Hz). 1.52-1.45 (2H. m). 1.35-1.26 (2H. m), 1*32 (3H. 1, J = 7.2 Hz) t 0.87 ( 3H, t. J = 7.2 Hz). 4-41 η3(Τ 'hUIMRWOO MHz. DMSO~d〇) δ: 13.17 &lt;2H. br s). 10.95 (1H, s). 8.01 (2H, d. J = 8.0 Hz), 7.80-7.72 (2H.m). 7.44 (2H. d. J = 8.0 Hz). 5.57 (1H, s). 3.84 (2H. t J = 7.2 Hz). 1.51-1.48 (2H, (m), 1.34-1 (3H, t, J = 7.2 Hz). (1H. br s). 9.12 (1H, br s). 8.52 (1H. brs). 7.82 (1H. br s). 7.41-722 (5H, m). 4.44 (2H. d. J = 6 6 Hz ). 2.55 (3H. s). 4-43 'H-NMROOO MHz, DMSO-de) 5:13.22 (1H, brs), 11.12 (1H_ br s), 9.13 (1ΗΛ J = 6·2 7.89 (1H_ d J = 7.7 Hz). 7.41-7.20 (7H. m). 4.45 (2H. d. J = 5.9 Hz), 2.49 (3H, s). 4^44 cnr^rV? 'H -NMROOO MHz. DMSO-de) δ: 13^8 (1H, br s). 11.31 (1H. brs), 9.16 (1Ht brs), 8.75 (1H, 8). 8.62 (1H. br s), 7.61 ( 1H, br s), 7.41-7.22 (6H.m), 4.44 (2H, d( J»6.6Hz). 4-45 %H4mR(A0Q MHz. OMSO-de) δ: 13.16 (1H. s). 10.87 (1H, s). 7.78 (1H. dd, J = 10.4. 7.2 Hz). 7.69 (1H, dd. J = 10.4, 8.8 Hz). 7.38 (2H. df J = 8.4 Hz). 7.26 (2H, d , J = 8.4 Hz). 5.44 {1H. br 5), 4.47 (2H, q, J = 7.2 Hz), 3.77 (2H, t, J = 7.2 Hz), 3.71 (2Ht s). 1.52-1.46 (2H m), 1.34-1.29 (2H.m). 1.15 (3H. t J = 7.2 Hz), 0.88 (3H. t, J = Hz). 4-4β , / Η ^H^MRIAQO MHz, DMSO-de δ: 13.11 (1H, brs), 12.49 (1H, br s). 10.89 (1H, s). 7.80-7.68 (2H.m). 7.37 (2H. df J = 8.4 Hz), 7.25 (2H. d , J = 8.4 Hz), 5.50 (1H, br s), 3.78 (2H. ζ J = 7.2 Hz), 3.62 (2H, s), 1.51^1.48 (2Ht m), 1.34-1.30 (2H. m). 0.89 (3H, t. J = 7.2Hz). 335 318197 1322688

Table 45

The compound examples 5-1 to 5-44 shown in the following table were prepared in the same manner as the above-mentioned production methods A, B, C or the above individual examples.

336 318197 1322688 Table 46

Example molecular structure NMR 5-1 ^I^RC^O MHz, DMSO-Cfc;) δ: 11.18 (1Ht s), 9.11 (1H, m). 8.14 (1H, s). 7.86-7.80 (2H. m 7.72 (1H.m). 7.23 (1H, s). 6.86 (1H. m). 4.38 (2H. d, J = 5.2 Hz). 3.86 (3H, s). 5-2 'H-NMRC^ O MHz. DMSO-de) δ: 10.98 (1H. s), 9.07 (1H, br s). 8.14 (1H. s). 7.72 (1H. m). 7.5Θ (1H, dd, J = 11.2, 8.4 H2) ( 7.40 {1H, dd, J = 11.6, 8.0 Hz). 7.19 (1H. s), 6.85 (1H, m), 4.37 (2H. d. J =5.6 Hz), 3.85 (3H, s), 2.35 {3H, s). 5-3 ^H4mR(A00 MHz. DMSO-de) δ: 11-16 (1H. s). 9.16 (1H. m). 9.10 (1H. m). 7.87-7.81 (2H , m). 7.49 (1H, br s)· 7*29 (1H· s), 4.59 (2H· &lt;U = Se Hz). 5-4 0 1H-^R (300 MHz, DMSO-&lt;/ e) δ: 11.20 (1H, br s), 10.49 (1Hf brs), 9.19 (1H. bre), 8.83 (1H, t, J = 4.2 Hz), 7.92-7.75 (4H. m). 7.43 (2H, d. J = 8.1 Hz), 7.29 (1H, br s). 4.49 (2H. d, J = 5.5 Hz), 4.0W.42 (10H, m)t 3.30 (2H. d, J = 5.4 Hz), 2.49 pH.brd, J = 6.1 Hz). 0 'H-NMROOOMHz. DMSO-&lt;/e) 6:11.19 (1H, br s)t 9.57 (1H, br s), 9.17 (1H, l, J = 4.5 Hr), 7.84-7.73 (2H, m), 7.74 (2Ht dt J = 6.7 Hz). 7.40 (2H. d( J = 6.7 Hz). 7J2B (1H. br s). 4.49 (2H. d, J = 5.5 Hz), 3.90 (2H, br s). 3.60 (4H, br 6), 2.91 (4H, br s) 5-« 0 'H-NMROOO MHz. DMS0^6) 6: 8.88 (1H, br s), 7.90-7.60 (5H, m), 7.38 (2Ht d. J = 8.1 Hz). 4,47 (2H, d, J = 4.2 Hz), 3.46 (2H, s). 337 318197 1322688

Table 47

338 318197 1322688 Table 48

Example molecular structure NMR 5-13 fi 3HCI η fY ^-NMROOOMHz. DMSO-d6) ¢: 11.25 (1H, br s)t 10.27 (1H. br s). 9.34 (1H. t. J = 4.5 Hz), 9.18 (1H, t, J = 4.5 Hz), 8.61 (1H, d, J = 4.3 Hz). 8.00 (1H. s), 7.89-7.80 (2H, m), 7,57 (1H. d, J = 3.6 Hz), 7.30 (1H, br s), 4.55 (2Ht d, J = 4.5 Hz), 4.01-3.97 (2H. m). 3.77-3.05 (10H, m). 5-14 'H-NMROOOMHz, DMSO -d6) &lt;5:11.24 (1H. br 5), 9.97 (1H. brs), 9.30 (1H, tt J = 4.5 Hz). 8.56 (1H. dt J = 3.6 Hz). 7.97 (1H, s) 7.89-7.80 (2H, m), 7.55 (1H, d. J = 3.6 Hz). 7.30 (1H. s). 4.55 (2H. d. J = 4.5 Hz), 3.67 (4H, d. J = 8.1 Hz). 2.90 (4H. d. J = 7.8 Hz). 5-15 ^H-HMR(AOO MHz, DMSO-&lt;/6) δ: 11.18 (1H, s), 9.08 (1H( t, J = (6H. = 6.0 Hz). 3.β5 (3H. s), 2.39 (3H, s). 5-1β 1/2 H2S04 Xj: W-NMRUOO MHz&gt; DMSO~de) δ: 11.18 (1H, s). 9.08 ( 1H, t. J = 6.0 Hz), 8.14 (1H, s). 7.87-7.80 (2H, m). 7.70 (1H, m), 7.25 (1H, s) ( 6.83 (1H, m), 4.38 (2H d, J = 6 .0 Hz). 3.84 (3H. s). 5-17 CH3 'H-NMRC^ MHz, DMSO-de) δ: 11.17 (1H,$). 8.67 (1H. br s). 8.41 (2H, s) 7.86-7.78 (2H, m), 7.20 (1H, s), 4.52 (2H, d. J = 5.2 Hz). 4.02 (6H, s). &amp;-18 Hjir 'H-NMROOO MHz, DMSO*&lt ;#e) δ: 11.23 (1H, s), 9.33 (1H, t, J = 5.5 Hz), 8.84^.57 (3H, m), 7.91-7.77 (2H, m), 7,76-7.65 ( 2H, m), 7.29 (1H( s), 4.68 (2H, d( J = 5.5 Hz), 4.20 (2Hf d, J = 5.5 Hz).

339 318197 1322688 Table 49 Molecular structural formula NMR 5-19 1H-T^R (300MHz, DMSO-d6) δ: 11.19(1H.s). 9.15 (1H. t J = 5*7 Hz). 8.38 ( 1H, d( J = 2.2 Hz), 7.88-7.77 (3H, m), 7.50 (1H, d. J = 8.1 Hr), 7.24 (1H. s), 4.46 (2H. d. J = 5.9 Hz), 2.37 (3H, s). 5-20 2H3〇-|-&lt;)H 'H-NMROOOMHz, DMSO-d6) δ: 11.19 (1H. s). 9.15 (1H, t, J = 5.9 Hz), 8.38 (1Hr d, J = 2.2 Hz), 7.88-7.77 (3H, m)t 7.50 (1H, d. J = 8.4 Hz), 7.24 (1H, s), 4.46 (2H, d, J = 5.9 Hz). 2.44 (6H. s). 5-21 'H-NMRC^ MHz, DMSO-de) 6:13.33 (1Mk br s), 11.21 (1H, br s). 9.00 (1H, brs), 8.58 (1H, d , J = 6.4 Hz), 7.87-7.81 (2H, m), 7.78 (1H, d ( J = 6.4 Hz), 724 (1 Hf br s)t 4.58 (2H, d, J = 4.8 Hz), 2.86 ( 3H, s), 2.66 (3H.s). 5-22 crV^V^ 'H-NMRWOO MHz. DMSOde) δ: 11.25 (1H. s), 9.34 (1H, m), 8.87 (1Ht m), 8.81 (1H, m). 8.45 (1H. m). 7.98 (1Ht m), 7.88-7.81 (2Ht m). 7.25 4.63 (2H, m). 5-23 CH, CH3 'H-NMR (300 MHz, DMSO -de) 0:11.25 (1H. s), 9.37 (br s)f 8.25-7.98 (1H. m), 7.90-7.53 (3H, m). 6.91-6.58 (2Hf m), 4.94-4.43 (2Ht m ). 3 .86 (3H, s), 3.58-3.14 (2H, m). 1.64-1.60 (2H, m), 0.84 (3H. t. J = 7.5 Hz). 5-24 axr^r^ 'H-NMR ( 300 MHz, DMSO-de) δ: 11.22 (1H( s), 9.19 (1H, t. J = 5.7 Hz), 7.99-7.77 (4H, m), 7.43 (1H, d, J = 9.4 Hz), 7.21 (1H, s), 4.37 (2H, d, J = 5.7 Hz), 3.83-3.62 (4H, m). 1.72-1.50 (6H. m).

340 318197 1322688 Table 50

Example molecular structure NMR 5-25 ^-NMR (300 MHz, DMSO-dB) δ 11*22 (1Hf s). 9.21 (1H.t. J = 5.8 Hz), 8.04-7.99 (2H.m), 7.8 &amp;-7.80 (2H.m), 7.41 (1H, d. J = 10.2 Hz). 7.22 {1H, s). 4.40 (2H, d. J = 57 Hz). 3.81-3.59 (8H. m). 5-2β 'H-NMR (300 MHz, OMSO-dJ 6:11.18 (1H, s). 8.91 (1H. s). 8.65 (2H, d. J = 5.7 Hz). 7.87-7.78 (2H. m) 7.27 (1H, s), 4.67 (2H. d. J = 4.5 Hz). S-27 ^-NMR (300 MHz. DMSO-de) 6: 11.23 (1H( s). 9.24 (1H, t( J = 5.8 Hz), 8.02-7.79 (4H, m). 7.30-7.18 (2H, m)( S.68 (br s), 4.38 (2Ht d, J = 5.7 Hz), 3.24 (6H. s). 5 -28 CH, CHj ^-NMR (300 MHz, OMSO-ds) δ: 13.85 (1H, br s). 11.31 (1H. s). 8.05-7.80 (4H. m), 7.25 (1H. d, J = 9.4 Hz), 6.83 (1Ht br s). 5.01-4.49 (2Ht m). 3.63-3.42 (1H, m), 3.38 (br s). 3.25 (7H. m), 1.75-1.51 (2H, m), 0.85 (3H, t. J - 7.3 Hz). 5-29 Η3(Τ 'H-NMR (300 MHz, DMSO-de) 6:13.81 (brs), 11.23 (1H, s). 9.20 (1H( br t ), 8.01-7.78 (4H.m). 7.30-7.13 (2H, m). 4.37 (2H, d, J = 5.7 Hz), 3.65 (4H, q, J = 7.0 Hz), 1.18 (6H, t, J = 7.0 Hz). 5-3 0 〇2HCI ^-NMR (300 MHz, DMSO-c/β) δ: 11.18 (1H, s), 10.08 (br s), 9.01 (1H, t( J = 5.7 Hz). 7.8&amp;-7.79 (2H , m). 7.53 (1H, d, J = β.7 Hz). 7.28 (1H, s). 6.62 (1H. d, J = 8.3 Hz), 4.36 (2H. d, J = 5.7 Hz). 3.00 (6H. s). 341 318197 1322688 Table 51

Example molecular structure NMR 5-31 'H^JMR (400 MHz, DMSO-d6) δ: 11.18 (1H, s), 9.59 {1H( s). 9.19 (1H. t. J = 5.8 Hz). 8.10 ( 2H. d, J = 7.9 Hz). 7.84-7.81 (2H. m). 7.48 (2H, d. J = 8.3 Hz). 7.30 (1H. br s). 4.51 (2H. d. J = 6.0 Hz) 5-32 Η 'H-NMR (300 MHz. DMSO*dfi) 5: 11.59 (br s). 9.49-9.32 (2H. m). 7.88-7.81 (2H. m). 7.21 (1H, s), 4.60 (2H. d. J = 5.7 Hz). 2.48 (3H. s). 5-33 H3/H fH-NMR (300 MHz. DMSO-de) δ: 11.25 (1H, s), 9.90 (br s) , 9.45 (1H, t. J = 5.7 Hz), 7.88-7.79 (2H, m). 7.18 (1H, s). 4.54 (2H, d. J = 5.7 Hz). 2.82 (3H, s)r 2.48 ( 3H, s). 5-34 'H-NMR (300 MHz, DMSOde) δ: 11.23 (1H, s), 9.20 (1H.t, J = 5.8 Hz), 8.00-7.80 (4H, m) ( 7.45 ( 1H, d. J = 9.4 Hz), 7.22 (1H, s), 4.37 (2H, d, J = 5.7 Hz). 3.94-4.04 (2H. m). 3.79-3.87 (1H( m). 3.48-3.60 (2H.m), 1.79-1.90 (2H, m). 1.42-1.54 (2H, m). 5-35 fH-NMR (400 MHz, DMSO-de) δ: 11.19 (1H. s). 9.21 (1H , t. J = 5.8 Hz). 8.49 (2H, s). 7.88-7.78 (2H, m), 7.26 (1H. s). 4.53 (2H. d. J = 5.6 Hz), 2.47 (3H. 5) 5-36 ^NMR (40 0 MHz, DMSO-de) 6: 11.33 (1H. s). 10.95 (1H, s)t 9.26 (1H, d ( J = 4.2 Hz), 9.02 (1H, brdr J = 8.3 Hz). 8.23 (1H, d, J = 8.3 H2), 8.11 (1H. t. J = 7.9 Hz), 7.99 (2H, d. J = 7.4 Hz), 7.91-7.83 (2H. m). 7.59 (1H. brs). 342 318197 Table 52 Example Molecular Structure NMR 5-37 1H-NMR (400 MHz. DMSO-de) 6: 11.59 (1H. br s). 11.02 (1Ht brs). 9.01 (1H. dd. J = 4.2, 1.4 Hz) 8.73 (1H. d. J = 7.4 Hz). 8.50 (1H. dd, J = 8.3.1.4 Hz). 7. Run 7 (2H. m>. 7.80^7.62 (3H. m>. 6.84 (1Ht Brs). 5.81-5.79 (2Htbrs). 5-38 'H-NMR (400 MHz, DMSO-de) 6:11.33 (1Ht s), 10.92 (1H, s), 9.87 (1H. s), 8.68 (1H , d, J = 6.5 Hz), 8.40 (1H, dt J = 8.3 Hz), 8.34 (1H, df J = 7.0 Hz), 8.23 (1H. d, J = 7.0 Hz). 8.02 (1H, t, J 7.9 Hz), 7.91-7.83 (2H. ), 9.21 (1H, s), 8.09 (1H, 3). 8.00-7.76 (3H, m), 7.38-7.26 (1H. m). 7.22 (1H. s). 4.5&amp;4.29 (4H. m) 3.63-3.40 (4H, m). 3.26-3.06 (2H, m). 2.79-2.76 (3H, m). 5-40 1H-NMR (300 M Hz, DMSO-de) 6: 11.22 (1H( s). 11.06 (1Hf br s). 9.20 (1H. br t, J = 5.3 Hz). 8.01-7.91 (2H. m). 7.88-7.80 (2H, m), 7.40 (1H, brd, J = 9.8 Hz). 7.22 (1H. s). 4.52 (2H, brd( J = 13^ Hz), 4.37 (2H, br d. J = 6.0 Hz), 3.54- 3.40 (1H. m), 3.14 (2H, br t, J = 8.3 Hz), 2.70 (3H, s) ( 2.69 (3Ht s). 2.17 (2H, br d. J - 12.4 Hz). 1.79*1.65 ( 2H, m). 5-41 aXX^l^ 1H-NMR (300 MHz, DMSCM^Q: 13.80(brs). 11.23 (1H, s), 9.23 (1Ht t J = 5.8 Hz). 8.01-7.79 (4H .m). 7.22 (1H, s). 7.12 (1H, d. J = 9.4 Hr), 4.38 (2H, d, J = 5.7 Hz), 3.62-3.48 (4H. m). 2.10-1.95 (4H, m). 5-i2 'H-NMR (400 MHz, DMSO-de) 5:11.22 (1H. s), 9.28 (1H, t. J = 5.8 Hz). 8.66 (1H. d, J = 1.4 Hz) , 8.62 (1H. dd, J = 2.8, 1.4 Hz), 8.57 (1H, d. J = 2.8 Hz), 7.90-7.81 (2Ht m), 729 (1H, s), 4.61 (2H. d ( J = </ RTI> </ RTI> <RTIgt; -7.95 (2H.m), 7.86-776 (2H, m). 7.42 (1H, d, J = 9.4 H2). 7.20 (1H, s). 4.36 (2H, d. J = 6. 0 Hz). 4.10-4.02 (4H, m). 2.75-2.70 (4H. m). 5-44 0 'H-NMR (300 MHz, DM$Ode) δ: 11.23 (1H. 8), 9.21 (1H , br t, J = 6.0 Hz)t 8.09 (1H. s). 7.94 (1H, d( J = 8.3 Hz), 7.89-7.81 (2H, m), 7.40 (1H, br d, J = 8.8 Hz) , 7.24 (1Hf s), 4.40 (2H, d, J = 6.0 Hz), 4.18 (4H. br s) ( 3.28 (4H. br s).

Further, the compound examples 6-1 to 6-50 and the examples 7-1 to 7-17 compounds shown in the following Table were prepared in the same manner.

344 318197 Table 54 Example Molecular Structure NMR 6-1 Η iH-NMR (300 MHz. DMSO-de) δ: 13.24 (1H, s &gt; _ 11.14 (1H, brs &gt; 8.80 {1H, brs) · 7.94-7.80 (2Η.πι). 7.69(1 Hs). 7.40-7.32(1Η,ηΓ!). 7.06(lHfs)( 3.79(2H,dJ=5.6Hz). 6-2 3 Η ^-NMR (400MHZ.DMSO- C/6) δ: 13.26 (1H, s). 10.96 (1H. s). 7.98(2H, d. J = 8.3 Hz). 7.81-7.80(2Htm)f 7.45 2H. d. J = 8.1 Hz), 5.67 (1H. s). 3.36 (3H.s). 6-3 ^ Η YH-NMR (400MHz, DMSO-de) δ: 13.27 (1H, s). 10.96 (1H, s). 8.55 (1 Hd, J=4.0Hz), 7.95 (2H. d. J = 8.3 Hz), 7.82^7.70(2H.m). 7.46 (2H, d, J = 8.1 Hz), 3.38 (3H. s). 2.82 (3H, dJ = 4.6 Hz). 6-4 ^ Η iH-NMR C400 MHz. DMSO-de) δ: 13.27 (1 Η sentence, 10.98 (1H, s)· 7.79 (1H, m&gt;, 7.69 (1H, m), 7.52-7.43(4Hlm), 5.56(1Hts), 3.38(3H.s)t 2.98(6H,m). 6-6 ' Η iH-NMR (400 MHz, DMSO-&lt;/e) δ: 13^9 (1H, brs), 11.00 (1H(brs)f 8·05(2Η, &lt;υ=7·2Ηζ&gt;, 7.82·7.74(2Η_ιη), 7.51{2H,d,J=6.5Hz), 5.81 (1H,m)f 3.39{3h.s). 6-6 'H-NMR (400 MHz, DMSO-de) δ: 13.20(1^8). 10.89(1H,s). 7.98(2H,d, J=8.0Hz), 7.78(2H,m). 7.27(2 H, d, J = 8.0 Hz) l 5.69 (^.8). 4.34 (1h.dJ = 4.4 Hz), 3.35 (3H, s&gt;, 2.84 (3H, s&gt;. 6-7 3 Η iH-NMR ( DMSO-de) δ: 13.30(1Hfs). 11.01(1H,s), 7.96(2HtdtJ=8.0Hz), 7.8S-7.74(2H.m). 7.62(2H.d, J=7.8Hz) 5.70(1 Hs), 3.39(3H,s). 345 318197 1322688

Table 55

346 318197 1322688 Table 56

Example molecular structure NMR 6-15 , Η ^-NMR (400 MHz, DMSOdt) δ: 13.25 (1H.s) ( 10.94 (1H, s), 7.95 (2Ht d, J = 7.7 Hz). 7.80-7.70 ( 2H,m)f, 7.47 (2H. d. J = 7.7 Hz). 5.73(1 Hs)f 3.38 (3H, s). 6-16 ^ Η iH-NMR (400 MHz, DMSO-de) δ: 13.52 ((1H, s&gt;· 13*29(1H, s&gt;. 10-98(1H, s&gt;, 8.05 (2H. d. J = 8.6 Hz), 7.81-7.69 (2H, m), 7.56 (2H. d. J = 8.3 Hz), 5.74 (1 Hs), 3.39 (3H. s). 6-17 'H&gt; NMR (400MHz, CDCI3) δ: 13.43(1H,m), 10.59(1 H,brs), 8.15 (1H, d, J = 8.6 Hz), 7-56 (1H_m&gt;, 7.33-7.24 (3H, m}_ 7.04 (1H.m&gt;· 6.00(1 Η,η), 4.65(1 Hem), 3.20 (3H, s). 1.73-1.23(12H, m). 6-18 iH-NMR (400 MHz. OMSO-de) 5:13.73 (0.6H.s&gt;. 13.56&lt;0.4H,s&gt;. 11.60( 0.4H.s&gt;. 11.36 &lt;0.6Hs)t 8.35(0.6H,s} 8.17(0.4H,s), 7.97-7.84{2H.m), 7.23(0.6^,5), 6.66(0.4H, s). 4.76(1 Hm), i.4S(2H.m). 4.30(2H,m), 1.37(3H,m), 1.34(3H,U= 6-19 HlVtr^ 1H-NMR (400 MHz, DMSO-de) 5:13.32(1H,s)( 11.20(1H.s), 9.43(1H,s). 9^0(1 H,s), 7.83(2H,m)e 7.35-7.25(4H. m), (50(2H.(U=8.4H2&gt;. 3.05&lt;3H,s}. 6-20 Ih-NMR (4 00 MHz, DMSO-C/e) 5:13.31 (1H(s). 11.17-11.01(1h,m), 9.69(1H,m), 9.14(1H_m), 7.93(1H,m). 7.82{1H( m) „ 7.53(1H,m)t 7.36-7.15(4H,m)t 4.42(2H,m)t 2.11(3H.s). 347 318197 1322688 Table 57 Reference Example Molecular Structure Formula NMR 6-21 iH-NMR (400 MHz. DMSO-dB) 6:13.36 (1H, s), 11.60 (1H, s), 11.20 (1H. s) (9.52 (0.4H, s), 8.52 (1H. s). 7.83 (2H, m)( 7.41-7.34 (5H.m), 4.56 (2H. s). 3.33(6H, s). 6-22 iH-NMR (400 MHz, DMSO-de) 6:13.31 (1H,S). 11.32 (1H, s), 11.17 (1H. 8).9.26 (1H, s), 8.70 (1H, s), 7.86 (2H, m), 7.41-7.35 (3H, m), 7.22 (1H. d. J =7.0Hz). 4.47 (2H. d, J = 6.0 Hz), 3.24 (3H. s). 6-23 Η3(Τ^Η3 ^H-NMR (400 MHz, DMSO-de) 5:13.28 (1H· S&gt;, 11·37(1Η. s)· s}, 9.22 (1H, m)t 8.68 (1H, s), 7.94-7.78 (2H, m), 7.3645-7.37 (5H. m), 4.44 (2Ht d, J = 5.6 Hz) t 3.26 (3H.S). 6-24 H3C/S^3 iy: 1H-NMR (300 MHz. DMSOde) &1121&lt;1H, s).10_42 (1H, s&gt;. 9.18 (1H, s &gt;, 7. knee 7.78 (2H, m), 7-5 CK7_45 (2H.m &gt; 7.3.2 - 7.24 (3Htm). 4.47 (2Htd, J = 5.5H2) lt 3.45 (3H, m), 3.21 (3H, s). 2.03 (3H. s). 6-25 iH-NMR (300 MHzf DMSO- De) 6:11.20 (1H. s). 10.46 (1H. s), 9.23 (1H. s), 7.88-7.69 (2H, m). 7.50-7.09(5H,m). 4.50 (2H. d. J = Hz), 3.27-3.17 (6H. m). 2.33-2.29 (3H. m). 6-26 HjC^CH, ^H-NMR (300 MHz. DMSCWe) 6:11.19 (1H. s). 10.52( 1H(s)t9.21(1H,m), 7.83 (2H. dd. J = 18.2. 8.6 Hz). 7.49-725 (4H.m). , 7.11(1H.m).4.49 (2H.d. J = 5.9 Hz), 3.28 (6H.m), 2.16 (3H, s). 348 318197 8 1322688 Table 58 Example Molecular Structure NMR β-27 H3Cs^W^ 丄1H-NMR (300 MHz, DMSO-de) 6:11.47 (1H, &lt;U=12.0H2) (9.47(1H.s). 8.49 (1H. d. J = 12.8 Hz), 7.88-7.79 (2H, m). 7.45-7.35 (4H, m) 7.25(1 H(m)(4.55 (2Ht d, J = 5.9 Hz). 3.78-3.63 (4H. m). 1.34-1.26 (6H. m).. 6-28 1H44MR (300 MHz. DMSO-d6 δ: 11.34 (1 H, dtJ = 13.2 Hz), 11.20 (1H. s). 9.21 {1Hem), 8.66 (1H.dJ = 12.8H2), 7.8»-7.79 (2H, m), 7.47-7.42 ( 2H,m),7 34-7.26 (2H, m), 4.47 (2H, d, J = 5.5 Hz), 3.74-3.64 (4H,m), 1.3M.18(6H,m). 6-29 C \iH-NMR (300 MHz, DMSO-de) s), 9.17 (1H, m &gt;. β·63 (1H, d·J = 13.2 Hz). 7.87-7.78 (2Hf m), 7.48 (2Htd, J= 8.4H2), 7.40 (2H. dd, J = 8.4 Hz). 7.26(1 Htm) , 4.44 (2H, d, J = 5.9 Hz), 3.69 (4Hf dd. J = 16.0. 72 Hz), _ 1.30*1.20 (6H_m)· 6-30 Ο 2HCI Η fY (WS^yV iH-NMR (400 MHz, DMSO-&lt;/fl) 5: 11.26 (1H.s&gt;. 11, 21 (1H, s&gt;· 9.45(1H,s)· 9.10(1H,m), 829(1Hts). 7.88-7.79( 2H,m), 7.51-7.43(3Η,Γη). 7.32-7.23(2H,m), 4.42(2H,dJ=8.8Hz). 6-31 Η Q 2HCI Η ^H-NMR (400 MHz, DMSO- Tfe) δ: 11.39(1H, s)· 11.21(1H, s&gt;· 9.55{1H, s&gt;, 9.21(1H, s)f 7.88-7.80(2H.m), 7.48-7.21(5H.m), 4.49 (2HldIJ=6.0Hz)1 2.34(3H.s). 6-32 °3 Η Μ iH-NMR (400 MHz, DMSO-de) δ: 11.34{1H_s&gt;. 11.21(1H.s&gt;· 9.48(1H .s&gt;, 9.24(1H.brs&gt;. 8.52(1H.s&gt;. 7.88*7_B2&lt;2H,m}, 7.46(2H.d, J=9.2H2), 7.30(2H,d,J=9.2H2&gt; 4.47 (2H.m), 2.33 (3H.s).

349 318197 1322688 Table 59

Example molecular structure NMR 6-33 'H-NMR (400 MHz. DMSO-de) 0: 13.26 (1H. s). 11.17 (1H. s). 924 (1H. m). 7.94-7.80 (4H. m 7.50(2H .d. J=8.1H2). 7.36(1h. s)· 4.52 (2H. d. J = 5.8 Hz). 6-34 lH> NMR (400 MHz, DMSOde) 5:11.69 (1H s), 11.20 (1H. s). 10.02 (1H. s). 9.36 (1H, s). 9.17(1H, s), 8.31 (1H, d, J = 2.6 Hz)t 7.8B-7.79 (4H , m). 7.58-7.31 (8H, m). 4.53 (2H. d. J = 6.0Hz). 6-35 1H-NMR (400 MHz, DMSO-de) 5: 11.63 (1H. s). 11.19 ( 1H. s). 9.98 (1H. s), 9.33 (1H. s), 9J27(1H. s). 7.87-7.79 (5H.m). 7.56-7.42(7H,). 4.51 (2H. d. J = 6.0 Hz). 6-36 1H-NMR (400 MHz, DMSO-de) 6: 13.24 &lt;1Hts) t11.15 (1H, s), e.12 (1H.m) (8.26 (1 H, s) ) f7.84- 7.80 (2H.m&gt;, 7.41 (1H, s), 7.3e (2H, brs) 7.16 (1 Η·υ=8·0Ηζ)_β·89(1Η, πι)Λ39(2Η.( υ=β.0Η z)m2.91(6H,s). 6-37 CH, H iH-NMR (400 MHz, DMSO &lt;/e) δ: 1H-NMR (DMSO-d6) 5:13.22 (1H. s). 11.13 (1H·d. J = 7.9 Hz). 9.08(1H.m}_ 8.24 (1H_ s), 7.85-7.78 (2H, m&gt;( 7.42-7.15 (5H. m). 4.36 (2H, d. J * 6.0 Hz). 2.96 (6H, 8). 6-38 H 1H-NMR (300 MHz, DMSO-de) 5:13.35 (1H.brs), 11.19 (1H.s&gt;.9.84 (1H.s&gt;.9.1 4(1H.s), 7.79-7.87(2H,m)f7.59 (2Hf d. J = 8.4 Hz). 7.0-7.35 (7Hfm)t425(2Hid.J=6.0H2)i 2.36 (3H, m), 6-39 iH-NMR (400 MHz, DMSO-de) δ: 11.20 (1H.s 922(1 Hs), 7.84 (2H.m), 7.30(1 Hs). 7.18(1H.m), 8.78(1 H_m}.6.6.9{1H.fn&gt;.4·42 (2H·d J = 5_6 Hz).. 350 318197 1322688 Table 60

Example molecular structure NMR 6-40 1H-NMR (300 MHz, DMSO-de) 6:1120 (1 Η. s)» 9.08 (1H, t, J = 5.7 Hz). 7.83 (2H. ddd, J = 11.6. 6.7, 3.9 Hz). 7.23(1 Hs).7.05 (1.0H, t, J=12H2) ( 6.72 (1H. dd. J = 12.7, 72 Hz). 4.26 (2H. d, J=6.0Hz) 6 -41 (5V^rr^ Η [Η-NMR (400MHz, DMSO-de) 5:13.24 (1H. s). 11.12 (1H. s). 7.84-7.77(2H. m). 7.37(1H, s) , 7.28-7.18(4H, m). 5.52 (1H. q. J = 8.0 Hz). 2.99 (1H, m), 2.87(1H. m). 2.43 (1Htm), 2.00-1.95 (1H, m). 6-42 Η lH*NMR (400 MHz, DMSOc/e) δ: 13.19 {1H. d, J = 1.6 Hz), 11.12 (1H, s). 8.79 (1H( d, J * 7.0 Hz). 7.84- 7.77 (2H.m). 7.35 (1H, d, J=2.1Hz), 7.2S-7.22(2H, m). 7.17-7.14(2Ht m). 4.67 (1H, q. J = 7.2 Hz), 3.30 -3.20 (2H.m), 2.97-2.92 (2H.m). 6-43 α/ιγν^ iH-NMR (400 MHz. DMSOdt) δ: 13.74 (1H, m). 11.46 (1Η.πγι). 7.95 -7.89(2H,m)t 7.28-7.22(4Hfm), 6.86(1 Hm), 4.92(2H,s). 6-44 1H-NMR (400 MHz, CDCI3) 6: il.e^lH.s) , 7.92(2H.m), 7.40(4H(m), 6.92(1H,brs). 5.08(2H,3). &amp;45 iH-NMR (400 MHz, DMSO-de) 5: 12.09 (1H.S9) 11.61 (1H.2H.S), 7.91-7.83 ( 3H.m)· 7.24(1 Hm), 7.24»7.16(3H,m}, 6.88(1H,brs), 5.10(2H.s&gt;·6-46 (400 MHz, DMSO-tf 6) ^ 11·66 {1Η, 幻·9·10(1Η·ηη}·7.93 (2H· dd· J = 10.6, 7.1 Hz), 7.42(1 Htm), 7.34 (1H.m), 7.25(1Hfm).6.91(1H. Brs).5.05 (2H. s). 351 318197 1322688 Table 61 Example Molecular Structure NMR 6-47 ^CH3 'H-NMR (400 MHz. DMSO-de) 6:13.23 (1H. s), 11.16 (H, s). 8.91 (1H, S). 7.84 (2H, dd. J = 18.6, 8.3 Hz), 7.37-7.01 (5H.m). 6.70 (1H. d. J = 7.7 Hz), 4.30 (2H. d , J = 5.6 Hz). 4.23 (2H, d, J = 7.1 Hz) l 1.77 (3H. s). 1.29 (4.6Ht J = 7.1 Hz).. 6-48 !H-NMR (400 MHzt DMSO-tfe 5:13.31(1H,s). 11^0(1H.s). 9«27&lt;1H,t,J=6.0Hz&gt;, 8.71 (1H, dJ=5.2Hz>. 7.87(1Η, πι). 7.82(2H.m). 7.65(1H.m), 7.39(1H.s), 4.55(2H,(U=6.0Hz). 6-49 lH&lt;NMR (400 MHz. DMSCMe) 5:13.34 (1H, s). 11.21(1H, s&gt;, 9·88(1Η·3&gt;, 9.29(1 HtJ=6.0Hz). 8.49(1 Hm). 7.88(2H.m), 7.79(1H,s), 7.40( 1H(s)( 7.34(1h,m)( 4.50(2H,m). 6-50 iH-NMR (400 MHz, DMS0-de) 5:13.26(1H(s), 11.18(1H.s)t 9.32 (1H,m), 8.69(1H,m)· 7_94·7.83(4Η·Γ ) Β 7.57 (1H, S} · 7.40 (1H, s), 4.56 (2H_m) _

352 318197 1322688

Example NMR 7-1 CHg N-N 〇CH3 ^-NMR (400 MHz, DMSO-de) δ: 7.78 (2H, d, J = 8.6 Hz), 7.49-7.43 (2H, m), 7.12 -7.05 (3H, m). 5.54 (1H, m), 3.37 (3H. s). 7-2 Η 'H-NMR (400 MHz, DMSO-d6) 5: 13.26 (1 H.brs), 10.77 ( 1H, brs), 8.13 (2H, d, J = 7.0 Hz). 7.62 (2H, s). 7.46(1 H,m), 7.33(1 Hm). 3.43 (3H, s). 7-3 οτΛ^ ν?&quot; lH-NMR (400MHz, DMSO-de) 6:13.26 (1H, s), 11.13 (1H, S), 9.19 (1H.t, J = 5.9 Hz), 8.57 (1 Hs), 8.49 ( 1H, d, J = 3.5 Hz), 7.75(2H,m), 7.60-7.51 (2H, m), 7.40*7.35(2H,m>, 4.48 (1.1H.d, J = 6.0 Hz).. 7 · 4 〇n^qV^ lH-NMR (400 MHz, DMSO-d6) δ : 13.28 (1H, s), 11.20 (1H, s), 9.20 (1H, t, J = 5.9 Hz), 8.55 (1 H , s), 8.48 (1H, d, J = 3.5 Hz). 7.93 (1H, d, J = 6.5Hz), 7.79-7.73(2H,m), 7.40-7.35 (2H, m), 4.48 (2H, d, J = 5.8 Hz). 7-5 lH-NMR (300 MHz. DMSO-de) δ: 13.32 (1 H, m) t 11.32-11.27 (1 Htm), 9.19 (1 H(m)t 8.60- 8.40(3H,m)( 7.58(1 H,m), 7.35(2Η,Γη), 4.46(2Hfs). 7-6 lH-NMR(300 MHz, DMSO-de) δ: 9.10(1 H,m) , 8.55(1 Hs). 8.47(1H,d,J=3.7Hz),8.11(1H,m)· 7.91(1 Hm), 7.73(1 H,d,J=8.1 Hz). 7.60-7.57(2H,m), 7.39-7.35(2H,m). 4.47(2H.d,J=6.2Hz). 7-7 lH -NMR (400 MHz, DMSOde) δ: 13.30 (1 Hs), 10.62 (1 H (s), 9.14 (1Hlt, J = 5.4 Hz), β.δδίΙΗ, ε), 8.47 (1 H, dJ = 4.5 Hz ), 7.89(1 H,d,J=5.5Hz)m 7 72(1 H,d,J=7.3Hz), 7.37ilH.dd.J=7.5.4.9H2V 7.29i1H.sV 353 318197 1322688

Example molecular structure NMR 7-8 crV^rV^ lH-NMR (400 MHz. DMSOde) 6: 13.33 &lt;1H.s), 11O6 (1H, s&gt;, 9.19 (1H, brs&gt;. 8.57 (1h, s ), 8.48 (1H. m). 8.02 (2H. d. J = 7.4 Hz), 7.74 (1H, dt J = 7.7 Hz), 7.59-7.52 (3H, m) ( 7.37 (2Hfm), 4.48 (1Ht s 7-9 Η lH-NMR (400 MHz, DMSO-cfe) 6: 13.12 (1H, s), 10.74 (1H, s), 9.08 (1H, s), 8.52 (1H. s), 8.46 (1) Hs), 7.70 (1H, d, J = 7.4 Hz), 7.32-7.12 (7H, m), 4.44 (2H, d. J = 4.9 Hz). 3.63 (2H, s). 7-10 Η lH-NMR (400 MHz, DMSO-d#) &lt;5: 11.06 (1H, s), 9.32 (1.0H, s), 8.88 (2H, t. J = 11.0 Hz), 8.53 (1H, d. J = 8.1 Hz) 8.06 (1H, dd, J = 8.0, 5.7 Hz), 7.63 (1H, m). 7.40(1 Hm), 7.20 (1H, s), 4.66 (2H, d. J = 6.0 Hz), 2.37 ( 3H, s). 7-11 lH-NMR (300 MHz, DMSO-de) &lt;5:13_24 (1H.s&gt;.10_69(1H,s).9.15(1H.s}. 8.56(1 H,s ), 8.48(1 H,s), 7.79(1 Hm), 7.72(1 H, m), 7.38(1 H,s), 7.27(1 H,s), 6.67(3H,m),4_46(2h .s). 7-12 OnrSyV^ 2H-NMR (400MHz, DMSO-de) 6 : 11.31 (1H, s). 9.25 (1H, brs), 8.77 (1H, s), 8.72 (1H, d, J = 4.6 Hz), 8.25 (1 H, d, J = 7.8 Hz), 8.14 (1 H. dd, J=11. 4, 8.8 Hz), 7.83 (1 H.dd, J=7.9, 5.3 Hz), 7,52 (1 H.dd, J = 12.3, 7.9 Hz), 7.26 (1 H,bra), 4.58 (2H, d, J = 5.8 Hz) 3.19(3H, s). 7-13 lH-NMR (400 MHz, DMSO-de) 6 : 13.34 (1H, s). 11.22 (1H. s), 10.83 (1H, S) , 9.19 (1H, t, J = 5.9 Hz). 8.56(1 H,s), 8.46(1 H,m), 8.30(1 Hm), 7.72 (1H, d. J =7.9 Hz), 7.38-7.32 (2H, m), 4.458 (2H, d. J = 5.8 Hz). 2.09 (3H, s). 7-14 lH-NMR (400 MHz, DMSO-de) δ: 13.48 (1 H.brs). 10.99 (1H, s), 9.17(1H, s), 8.57 (1H, d, J = 1.6Hz), 8.49(1^01), 7.74 (H, dt, J = 7.8, 1.8 Hz), 7.39 (1H, Dd, J = 7.8, 4.8 Hz), 7.29 (1 H, m), 4.50 (2H, t J = 8.9 Hz). 354 318197 1322688 Table 64 Example Molecular Structure NMR 7-15 ^H-NMR (400 MHz, DMSO-de) &amp; 13.27 (1H, s&gt;. 10.99 (1H.s), 9.25 (1 H, t, J = 6.0 Hz &gt;, 8.71 (^, (1^=5^2), 7.90 (^, 01), 7.66-7.54{2H(m)( 7.40(2Htm), 4.45(2H,d,J=5.6Hz}. 7-16 Η lH-NMR(400 MHz, DMS0-cf6) 6: 13.28(1H, S), 10.98 (1H, s), 9.31 (1H, s), 8.54 (1 Hs). 8.00 (1 hs). 7.59 (1 Hm), 7.38 (2H, m), 7.27 (1 H, m), 4.53(2H,m). 7-17 lH-NMR (400 MHz, DMSO-de) δ: 9.70 (1H.s), 9.23 (1H, s), 8_12 (1H, d, J=8.6H z), 7.76(1 H.s), 751-7.27(7H,m)4.51 (2H,d, J=5.3Hz).

[Pharmacological test] 1. Test 彳 ( (1) liver liver 酉 酉 phosph phosph phosph phosph 、 、 、 、 、 、 、 、 、 肝脏 肝脏 肝脏 肝脏 肝脏 肝脏 肝脏 肝脏 肝脏 肝脏 肝脏 肝脏 肝脏 肝脏 肝脏 肝脏 肝脏 肝 肝 肝 肝 肝 肝 肝 肝 肝 肝 肝 肝 肝 肝. The hepatic phosphatase activity was measured using a prospective reaction system as follows. Glucose-1-phosphate prepared from glycogen by hepatic phosphatase, through the use of phosphoglucomutase and glucose-6-acid dehydrogenase (G6PDH), through transphosphory lation and Hydrogen reaction and conversion to glucose-(5-lactone 6-phosphate. Detection of NADPH ° 355 318197 1J22688 produced by NADP during dehydrogenation by G6PDH. Sf 9 of human liver analysing enzyme exhibiting exogenous recombination The cell homogenate was diluted in 1 mM ML/LBES buffer (pH 6.8 containing 2 mmol/L EDTA). This dilution was used as an enzyme solution for liver glycophosphatase in human liver. Use phosphate buffer (containing 16 mmol/L 'KH2P〇4' 24 mmol/L Na2HP〇4). 8 units/ml (U/mL) glucosamine mutant and 60 mg/ml G6PDH mixture Prepared in BES buffer. Separate preparation of buffer solution for reaction (containing 14 millimoles per liter of NADP, 30 millimoles per liter of MgClz, 8 micromoles per liter, glucose-i, 6-di-phosphate, 8 Mg/ml glycogen, 4 〇 millimol/L BES, os millimolar / liter EDTA), and Portuguese Sugar solution (containing 75 millimoles per liter of glucose, ι〇〇m / liter of BES, 2 millimoles per liter of EDTA). The test compound is dissolved in the MSO solution. The enzyme reaction begins with 20 microliters of recombinant human liver. The hepatic sugar phosphatase solution and a mixture of 20 μl of phosphoglucose mutant enzyme and G6PDH are added to 20 μl of glucose solution, 20 μl of matrix, 1 μl of microliter reaction buffer solution, and 20 μl of test compound solution. For the control group, 1Z DMSO solution was added instead of the test compound. The matrix-free mixture was used as a blank group. The absorbance at 34 Å was measured just after the start of the reaction. After 75 minutes at room temperature, it was measured again at 340. The absorbance of nanometer. 75 minutes • The change in absorbance value is subtracted from the absorbance value of the blank group after 75 minutes, and the value is obtained as the enzyme activity. 2. Test example (2) The measurement method of plasma glucose concentration is small using db/db. The mouse represents an experimental model of obesity diabetes, which is used to test the effect of the compound (1) of the present invention on plasma glucose concentration. The plasma glucose concentration of db/db 318197 356 1322688 mice (9 to 18 weeks old) was measured. 'Mice were divided into groups, each group of five mice or 8' to let blood polydextrose) no difference in the average value of e. Four hours after the fasting, the exemplified compound or solvent (0.5% thiol cellulose) was orally administered to db/db mice, and the sucrose concentration was measured at 1 hour and 3 hours after administration. Analysis of the hypoglycemic efficacy of the example compounds between the receiving solvent group and the example compound group was performed by statistical tests per hour (Dunnett test). The test results of the foregoing test examples are shown in the table below. The inhibition rate (%) of the test compound was calculated by the expression "丨 - test compound enzyme activity / control enzyme activity χΙΟΟ". The linear equation is determined from the two "intensity points" and the 50% inhibition rate between them, and the IC5Q value is obtained from the concentration of the intersection of the line and the 50% inhibition rate. The "ICm" in the table indicates the aforementioned enzyme inhibitory activity against hepatic glycophosphatase of the liver, and inhibits the activity of hepatic phosphatase in ICs. Value (Nemo/L) is expressed as ++ below 100 nm/L, and 1C when ICs() is 1 〇〇Nemo/Lising to 300 NM/L The inhibition rate (3) of the compound (1) of the present invention at a certain concentration when it is 3 (10) namol / liter or more is shown in the table. When the inhibition rate at a concentration of 300 nmer is 2%, The inhibition rate is described as 20% (300). In addition, 'vivo' refers to the hypoglycemic effect of db/db mice, with a statistically significant hypoglycemic effect at the dose of mg/kg or less. Compounds with a non-significant hypoglycemic effect at 10 mg/kg but with significant hypoglycemic efficacy are indicated by the symbol "+". 318197 357 1322688 Table 65

Example IC50 vivo 1-1 ++ 1-1-1 ++ ++ 1-1-2 ++ 1-2 ++ ++ 1 2-1 a 4+ ++ 1-2-2 ++ 1- 3-1 ++ ++ 1-4 ++ 1-5 ++ 1-6 + 1-7 + 1-8 ++ 1-9 ++ 1-10 + 1-11 + 1-12 ++ 4+ 1-13 ++ 1-14 1-15 ++ + 1-16 ++ 1-17 ++ 1-18 ++ + 1-19 4+ + 1-20 ++ 1-21 ++ + 1-22 ++ 1-23 ++ 1-24 + 1-25 ++ + 1-26 -Η- + 1-27 ++ 1-28 ++ 1-29 ++ 1-30 ++ 1-31 ++ + 1-32 ++ 1-33 ++ 1-34 ++ 1-35 ++ 358 318197 1322688

Table 66 Example ic50 vivo 1-36 ++ 1-37 ++ + 1-38 ++ + 1-39 ++ + 1-40 ++ + 1-41 ++ + 1-42 ++ + 1-43 + + 1-44 ++ 1-45 ++ 1-46 ++ ++ 1-47 ++ 1-48 ++ 1—49 ++ 1-50 ++ + 1-51 ++ 1-52 ++ + 1-53 ++ 1-54 1-55 ++ 1-56 ++ + 1-57 ++ 1-58 1—59 ++ ++ 1-60 ++ 1-61 ++ 1-62 ++ 1 -63 ++ + 1—64 ++ ++ 1-65 ++ 1-66 ++ + 1-67 ++ + 1-68 ++ + 1-69 ++ + 1-70 ++ ++ 1- 71 ++ + 1-72 ++ + 1-73 ++ 1-74 + 1-75 • H- 359 318197 1322688

Example vivo 1-76 ++ 1-77 43.8%(1000) 1 -78 ++ + 1-79 23.3%(300) 1-80 ++ + 1-81 ++ + 1-82 ++ + 1-83 6.1%(300) 1-84 ++ ++ 1-85 ++ 1-86 17.0%(300) 1-87 ++ + 1-88 ++ + 1-89 ++ 1-90 ++ + 1- 91 ++ + 1-92 11.7%(300) 1-93 ++ 1-94 36.5%(300) 1-95 ++ + 1-96 ++ + 1-97 ++ 1-98 ++ + 1- 99 ++ + 1-100 ++ + 1-101 +4- 1-102 ++ 1-103 21.6%(300) 1-104 32.3%(300) 1-105 + 1-106 + . 1-107 + + 4+ 1-108 45.3% (300) 1-109 33.3% (300) 1-110 ++ 1-111 + 1-112 49.9% (300) 1-113 ++ ++ 1-114 38.9% (300 ) 1-115 39.7% (300) 360 318197 1322688

Table 68 Example 1〇50 vivo 1-116 ++ ++ 1—117 ++ + 1—118 ++ 1-119 + 1-120 ++ 1-121 ++ 1-122 ++ 1-123 ++ + 1-124 ++ 1-125 ++ 1-126 ++ + 1-127 + 1-128 ++ + 1-129 ++ + 1-130 ++ + 1-131 ++ 1-132 +4- 1 -133 ++ + 1-134 ++ + 1-135 ++ + 1-136 ++ + 1-137 ++ + 1-138 ++ + 1-139 22.9% (100) 1-140 30.8% (100 ) 1-141 31.4% (100) 1-142 4+ 1-143 ++ 1-144 5% (100) 1-145 12.8% (100) 1-146 11.3% (100) 1-147 9.6% (100) 1-148 14.1%(100) 1-149 20.8%(100) 1-150 13.8%(100) 1-151 13.3%(100) 1-152 ++ 1-153 ++ 1-154 ++ 1- 155 ++ 361 318197 1322688

Table 69 Example IC50 vivo 1-156 ++ 1-157 ++ 1-158 ++ 1-159 + 1-160 ++ 1-161 ++ 1-162 ++ 1-163 ++ 1-164 ++ 1 -165 ++ 1-166 ++ 1-167 ++ 362 318197 1322688 Table 70 Example vivo 2-1 ++ 2-1-1 ++ + 2-2-1 ++ 2-3-1 ++ 2— 4—1 ++ ++ 2- 5 ++ ++ 2-6 ++ ++ 2~6—1 ++ 2-7-1 ++ ++ 2-8 ++ + 2-9 ++ + 2 -10 ++ + 2-11 ++ + 2-12 4+ ++ 2-13 +4· + 2-14 37.5%(300) 2-15 ++ + 2-16 ++ 2-17 ++ 2 -18 +4- 2-19 ++ 2-20 43.1%(100) 2-21 5-7W100) 2-22 ++ 2-23 ++ + 2-24 ++ + 2-25 ++ + 2- 26 36.4%(100) 2-27 ++ + 2-28 ++ + 2-29 45.8%(100) 2-30 1.8%(100) 2-31 5.5M100) 2-32 ++ 2-33 ++ 363 318197 1322688

Example 1〇50 vivo 3-1 50%(490) 3-2 + + 3-3 50%(640) 3-4 + + 3- 5 41.1%(1000) 3-6 42.5%(1000) 3-8 11.7% (1000) 3-9 50% (480) 3-10 23.2% (1000) 3-11 ++ + 3-12 50% (400) 3-13 25.5% (1000) 3-14 41.7% (1000 3-15 + 3-16 ++ 3-17 ++ 3-18 + 3-19 9.2%(1000) 3-20 ++ + 3-21 ++ ++ 3-22 50%(640) 3- 23 26.1%(1000) 3-24 ++ + 3-25 M- + 3-26 ++ + 3-27 41.5%(300) 3-28 + 3-29 ++ + 3-30 ++ 3-31 ++ + 3-32 ++ + 3-33 ++ s + 3-34 ++ 3-35 ++ ++ 3-36 ++ 3-37 ++ 3-38 ++ + 3-39 ++ + 3-40 ++ ++ 364 318197 1322688

Table 72 Example IC50 vivo 3-41 ++ ++ 3-42 1.1%(300) 3-43 13.4%(300) 3-44 + 3-45 ++ + 3-46 ++ + 3-47 ++ 3 -48 4+ 3-49 ++ 3-50 ++ 3-51 ++ 3-52 ++ 3-53 ++

365 318197 1322688

Table 73 Example 1〇50 vivo 4-1 13.8%(1000) 4-2 ++ ++ 4-2-1 ++ ++ 4-3 + 4一 4 -Η- + 4-5 + 4-6 + 4-7 + 4 - 8 + 4-9 ++ + 4-10 50% (590) 4-11 ++ 4-12 + 4-13 38.0XC300) 4-14 10.6% (300) 4-15 + 4 -16 5.1%(300) 4-17 1.1%(300) 4-18 ++ + 4-19 3.3%(300) 4-20 3.3%(300) 4-21 24.2%(300) 4-23 ++ + 4-24 + 4-25 ++ 4-26 ++ 4-27 + 4-28 + 4-32 7.8%(300) 4-33 15.2%(300) 4-34 ++ + 4-35 9.7% (300) 4-39 5.3%(300) 4-40 3.6%(300) 4-41 ++ + 4-42 8.5%(300) 4-43 3.8%(300) 4-44 5.7%(100) 366 318197 1322688

Table 74 Example 1〇50 vivo 4—45 5.9%(100) 4-46 ++ + 4-47 1.2%(100) 4-48 ++ ++ 367 318197 1322688 Table 75

Example IC50 vivo 5-1 ++ + 5-2 ++ + 5-3 ++ 5-4 ++ 5-5 ++ 5-6 ++ 5-7 ++ 5-8 ++ + 5-9 + + + 5-10 ++ + 5-11 ++ 5-12 ++ + 5-13 ++ + . 5-14 ++ + 5-15 ++ + 5-16 ++ + 5-17 ++ + 5-18 ++ 5-19 ++ 5-20 ++ 5-21 ++ 5-22 ++ 5-23 ++ ++ 5-24 ++ ++ 5-25 ++ ++ 5-26 + + 5-27 ++ ++ 5-28 ++ + 5-29 ++ ++ 5-30 ++ + 5-31 ++ + 5-32 ++ + 5-33 ++ + 5-34 ++ 368 318197 1322688

Table 76 Example IC50 vivo 5-35 ++ + 5-36 17.8% (100) 5-37 22.3% (100) 5-38 15.2% (100) 5-39 ++ 5-40 ++ 5-41 ++ + 5-42 ++ + 5-43 ++ + 5-44 ++ +

369 318197 1322688 Table 77 Example Cso vivo 6-1 15.5% (100) 6-2 12.3% (300) 6-3 9.7% (300) 6-4 46.8% (300) 6-5 ++ 6-6 ++ 6-7 12.9% (300) 6-8 11.7% (300) \ 6-9 5.5% (300) 6-10 + 6·11 2.1% (100) 6-12 ++ + 6-13 17.5% (100 6-14 20.1%(100) 6-15 ++ 6-16 ++ + 6-17 9.8%(100) + 6-18 6.8%(100) 6-19 ++ 6-20 ++ 6-21 ++ ++ 6-22 ++ + 6-23 ++ + 6-24 ++ 6-25 ++ 6-26 ++ 6-27 ++ 6-28 ++ 6-29 ++ 6-30 + + 6-31 ++ 6-32 ++ 6-33 ++ + 6-34 ++ 6-35 ++ 6-36 ++ 370 318197 1322688 Table 78 Example C50 vivo 6-37 ++ 6-38 ++ 6-39 ++ + 6-40 ++ 6-41 12.3% (100) 6-42 21.7% (100) 6-43 ++ \ 6-44 ++ 6-45 ++ 6-46 ++ 6- 47 41.1%(100) 6-48 ++ ++ 649 ++ 6-50 ++ Table 79 Example Cso In vivo 7-1 ++ + 7-2 ++ 7-3 ++ 7Λ ++ ++ 7- 5 8.5% (300). 7-7 2.9% (300) 7-8 6.8% (300) 7-10 ++ ++ 7-11 47.3% (100) 7-12 8.0% (100) 7-13 1.9 %(100) 7-14 4.6%(100) 7-15 ++ 7-16 ++

Industrial Applicability From the foregoing test results, it is apparent that the compound of the present invention and its pharmaceutically acceptable salt of 371 318197 1322688 have an inhibitory effect on human hepatic glycophosphatase. Therefore, the compound of the present invention can be used as a novel hypoglycemic agent based on the novel GP inhibitory efficacy mode of action. At the same time, it has the possibility of combining with other hypoglycemic drugs or hypolipidemic drugs, so the compound of the present invention has anti-resistance, diabetic-neuropathic, diabetic nephropathy, diabetic retinopathy, cataract, hypercholesterolemia, high Blood pressure, high-membrane gray matter, hyperlipidemia, atherosclerosis, tissue ischemia and myocardial ischemia; and available Lu as an appetite control and obesity therapeutic; and as such as bacteria, fungi, parasites Or the potential of a therapeutic agent for infection with a viral infection.

318197 372

Claims (6)

Scope: ;&gt;月^' 1^5118217 Patent Application 9 (more) Original July 7th - A pharmaceutical composition for treating or preventing diabetes, comprising pyrazole represented by the following formula U) a compound or a pharmaceutically acceptable salt thereof' and a pharmaceutically acceptable carrier: Wherein ring Q represents an aryl or heteroaromatic group; represents a hydrogen atom, a halogen atom, a &amp; aryl or an alkoxy group; ^ represents a (tetra), a Ch group, a Cl_6 alkoxy group or an azide group; R3 represents Tooth atom, thiol group, Cl_6 alkyl group, tooth Ch county, "alkoxy group, azido group, amine group, county amine group or L county heteroamine group; R4 and R5 are the same or different from each other and represent (1) Nitrogen atom; (2) a Ci-6 alkyl group which may be substituted with one or more substituents selected from the group [A group], a radical, A2. Ci-6 alkoxy, Δύ wherein R41 and R41' are each The same or different and representing the hydrogenogen Cl -6 alkyl group; or R41 and ρ4 ...... ... the adjacent nitrogen atom together form a 5-shell or 6-shell early ring heterocyclic ring, (Revision iL) 318197 373 1322688 A4. Patent application No. 95118217 (July 1st, 1998) A5. Heteroaromatic group, A6. -C0-N(R411)(ru), wherein R411 and R411· are mutually opposed to each other, and 4 is equivalent to each other. Or different and represent a hydrogen atom or a CBu 6 yard; or R and R4U can be a contiguous milk atom to form a saturated 5 or 6 membered monocyclic heterocycle, A7. as well as A8. C16 alkoxycarbonyl, (3) C2-6 alkenyl; (4) C 2 - 6 fast radical; (5) C3-8 cycloalkyl; alkoxycarbonyl substituted, or a cycloalkyl group a hydroxyl group, a carboxyl group or a Ci may be condensed with a pyridine ring, (6) a C3-8 cycloalkyl-based Ci-6 alkyl group; Wherein the C3-8 cycloalkyl Cl-6 alkyl ring 焓萁I γ soil can be substituted by a hydroxyl group, a carboxyl group or an Ll-6 alkoxycarbonyl group, or can be condensed with a pyridine ring, (7) saturating 5 members Or a 6-membered monocyclic heterocyclic group which may be substituted by one or more substituents selected from the group c below: [C group] C1 · Cl-6 alkyl, C2. fluorenyl, C3. Base-crossed turtle base 'C4. Carboxyl group, (amendment) 318197 374 1322688 Patent application No. 95118217 • (July 1st, 1998) C5· Ci-6 oxygen-burning base, ' and C6. -C0-( Alk)n-C00R52 &gt; wherein R52 is a hydrogen atom or a Ch alkyl group; human 1 is a Ch alkyl group; and η is an integer of 0 or 1 to 3, and (8) an aryl group may be selected from the group consisting of d Substituted by one or more substituents: [Group D] • D1. Merid, D2. G-6 alkoxy, D3. cyano, D4. Ci-6, wherein the Ch alkyl can be selected Substituted by one or more substituents of the group consisting of a hydroxyl group, a carboxyl group and a Ci 6 alkoxycarbonyl group, D5. -N(R53)(R53.), wherein the ruler and R53' are identical or different from each other And means that the hydrogen atom, C1 - 6 alkyl or C1-6 is burned! The base is D6·-C0-N(R53!)(R53丨,), wherein R531 and R531 are the same or different from each other and represent a chlorine atom, a Ci-6 appearance group or a Ci-e sleek base. Base, D7. -C00R54, wherein ^ is a hydrogen atom, a Cl_6 surface group, c "a methoxy group CM thio group or a C3.8 ring oxy group oxy group c1-6 alkyl group, D8. _C (NH (0H))=N-R55, (amendment) 318197 375 1322688 Patent Application No. 95118217, R55 A gas® 2 (July 10, 1998), Τ I (for helium atom or Ci 6 alkyl group) Sulfhydryl, D9. Saturated 5- or 6-membered monocyclic heterocyclic group, and D10. 5 or 6 membered monocyclic heteroaryl which may be substituted by _ or thiol, (9) 5 members Or a 6-membered monocyclic heteroaryl group or a heteroaryl group condensed with 5 or 6 members formed by a stupid ring, wherein the 5 member or 6 membered heteroaryl group may be selected from a carboxyl group and a C!-6 alkoxy group. One or more substituents of the carbonyl group are substituted with; 1 (10) C7-1. aralkyl; wherein the alkyl group of the C?-h alkyl group may be substituted by one or two selected from the group e below. Substituted, and the aryl moiety can be via one or more substituents selected from Group F below Substituted: [E group] El. Ci-6 alkyl group which can be substituted by a radical, φ E2. cyano group, E3. group, E4. Ci-6 alkoxycarbonyl group, and E5. phenyl group, [Group F] F1. Ci-6 alkyl group F2. Halogen atom, F3. cyano group, (amendment) 318197 376 F4. Hydroxy group, F5. C, -6-yard oxy group which can be selected from the county and Ci 6 Substituted by one or more substituents of a group consisting of several groups, F6. Tetra C!-6 alkyl, F7. carboxyl, F8. Ch alkoxycarbonyl, F9. -CO-N(R5Ga) (R56a And wherein R6a&amp;C are the same or different from each other and represent a gas atom, a saturated 5-membered or 6 S monocyclic heterocyclic group containing at least a nitrogen atom, or a C:-:alkyl group which may be selected from One or more substituents of group f below [f group] 胺. amine group, f2. mono Cl-6 alkylamino group, - Cl-6 alkylamino group, • f4. carboxyl group, Cl-6 courtyard oxygen a benzyl group, a f group, a 6 member, a single f, a 5-membered ring heterocyclic group having at least one nitrogen atom, ~ F10. -N(R56b)(R56b), 1-6 wherein R 6b And Ra6b are the same or different from each other and represent a hydrogen atom, the alkyl group may be substituted with an imido group, and the aralkyl group may be selected from an imido group. (Amendment) 318197 377 1322688 u In the patent No. 95118217, the request ' (July 1st, 1998) and one or more of the same or different groups of halogen atoms are replaced by An arylsulfonyl group which may be substituted by a Cm alkyl group, a Cl_6 alkyl group, a ketone group, a ketone group, an amine group, a mono-Ci-based amine group, or a Cl-alkylamino group, Fll -N=CR57(-N(R58)(R58)), wherein R57 is a gas atom or a Ch alkyl group, R5« and r58. are the same or different from each other and represent a hydrogen atom or a Cm alkyl group, F12. 5 members Or 6 members of a monocyclic heteroaromatic group, • and F13. a fluorenylenedioxy or ethylenedioxy group, or (11) selected from a 5- or 6-membered monocyclic heteroaryl group and a benzene ring a Cl_6 building group substituted with one or more identical or different substituents of a group consisting of 5 or 6 members of a condensed heteroaromatic group; wherein the heteroaromatic group may be selected from the group consisting of G Substituted by one or more φ substituents: [Group G] Gl. C&quot; Alkyl which may be substituted by one or more substituents selected from the group consisting of: g group] gl. halogen atom, g2. amine Base, g3. single Cl-6 Anthranylamine, g4. Di-Ch-alkylamino, (amendment) 318197 378 1322688, No. 95118217 (Patent application, month 10, No. 7 of September 8) g5. Cl-6, alkoxyamino group And g6.hydroxyimino group, G2. tooth atom, G3. Ci-6 alkoxy group which may be substituted by a tooth atom, G4. aryloxy group, G5. cyano group, G6.-N(R59a)(R59a,) , wherein R and R59a are the same or different from each other and represent a hydrogen atom or a Ch alkyl group, or R59a and R59a· together with an adjacent nitrogen atom form a saturated 5- or 6-membered monocyclic heterocyclic ring, and the saturation The heterocyclic ring may be substituted with one or more identical or different substituents selected from the group consisting of a trans-group, an amine group, a mono-Ch-alkylamino group and a di-Cl-e alkylamino group, G7.-C〇 -N(R59b)(R59b), wherein R59l R59b• are the same or different from each other and represent a gas atom, a _saturated 5 member or 6 M monocyclic heterocyclic group, or a &lt; Substituted, G8. aryl, and G9. 5 member or radical substituted, or 6 membered monoterpenoid heteroaryl which may be ketone or thioketone. / Μ can be combined with (iv) a nitrogen atom to form a saturated 5 member or 6 beryl early 糸 heterocyclic ring 'where one of the saturated heterocyclic rings can have a double bond, (Amendment) 318197 379 Patent No. 95,921,217 (98) On the 1st of the month, the condensed ring ' can be condensed with a benzene ring. The saturated heterocyclic ring can be condensed with a benzene ring to form a saturated heterocyclic ring which forms a condensed ring. C]~6 alkoxy group, carboxyl group and C! - may be substituted with one or more substituents selected from the group consisting of a functional atom, a Cl-6 alkoxy group. - The medical treatment for the treatment or prevention of diabetes according to the scope of claim 1 includes the sigma compound of the following general formula (I) or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier Agent: N—NH 〇 wherein ring Q represents an aryl or heteroaryl group; ' represents a hydrogen atom, a halogen atom, a Cl-6 alkyl group or a Cl-6 alkoxy group; ^ represents a halogen atom, c 6 alkyl group, Ci 6 Alkoxy or azide; R represents a halogen atom, a hydroxyl group, a C 4 alkyl group, a chiCh alkyl group, a cv 6 alkoxy group, a nitrogen atom, an amine group, a mercaptoamine group or a C1_6 alkylsulfonamide (1) a hydrogen atom; (2) a Cm alkyl group which may be substituted with one or more substituents selected from the group consisting of: [Group A] A1. Alkyl group, A2. Ci-6 alkoxy group, 380 (amendment) 318197 1322688 A3. -N(R41)(R41), where R41' is known to each other a. This is the same or different C丨-6 alkyl; or R4丨 and R4丨 can be made ^ # And a non-oxygen atom or a 5- or 6-membered monocyclic heterocyclic ring/a nitrogen atom to form a saturated A4. aryl group, A5. heteroaromatic group, A6. -CO-N(R411)(R川·) , =i2vr (9) where R and each other are the same or different and 矣r, a · ^ p4.i B d411. The flying phase is different from the atom or the base, and the 'and' can form a saturation together with the adjacent nitrogen atoms. 5 or 6 membered monocyclic heterocycles, "A7. Carboxyl, and A8. Ci-6 alkoxycarbonyl, (3) C2-6; (4) C2-6 alkynyl; 5) C3-8 cycloalkyl; (6) C3-8 cycloalkylphosphonium-6 alkyl; or (7) aryl; and R5 represents (1) Cm alkyl which may be selected from the group consisting of 8 Or a plurality of substituents substituted: [Group B] B1. Meridional, (amendment) 318197 381 Ch alkoxy (July 10, 2014 β3· -N(R5,)CR51'), where R5丨 and f And each of: or a different or different and represents a hydrogen atom or a 5-membered or 6-membered monocyclic heterocyclic ring, 1 atom together form a saturation and B4. ~C0-NCR5,1)(R51·), wherein R and R 11 are each known to have a Cm alkyl group, or a reverse (1) group, and are different from each other and represent a ruthenium atom or a Λ together with an adjacent nitrogen atom to form a saturated 5 or 6 membered monocyclic ring system. Ring, money (2) C3-8 cycloalkyl; wherein the cycloalkyl group can be passed through the base group. (d) ring condensation, alkoxycarbonyl substitution, or (3) C3-8 ring-based Ch-yard base; wherein the G-8 cycloalkyl C- 6 alkane oxime A # 凡基的裱 alkyl can pass through the hydroxyl group , a sulfhydryl or a decyloxy fluorenyl group, or a fluorene ring, or a (4) saturated 5 fluorene or W monocyclic heterocyclyl group, may be substituted with one or more substituents selected from Group C below. Substituting · · [C group] Cl. Ch alkyl, C2. fluorenyl, C3. Ci-6 alkyl singular, C4. carboxyl, C5. Ch alkoxycarbonyl, (amendment) 318197 382 No. 95118217 Patent application (July 10, 1998) and C6·-CO-(Alk)n-COOR52, wherein R52 is a hydrogen atom or (^-6 alkyl; Aik is a C1-4 alkylene; and n is 0 Or an integer from 1 to 3, (5) a square group which may be substituted with one or more substituents selected from the group d below: [Group D] D1. Merid, D2. Ci-6 alkoxy, D3. a cyano group, D4. Ch alkyl, wherein the Cl 6 alkyl group may be substituted with one or more substituents selected from the group consisting of a hydroxyl group, a carboxyl group and a Ch alkoxycarbonyl group, D5. -N(R53) (R53), - wherein R and R are the same or different from each other and represent a hydrogen atom, a Cl-6 alkyl group or a Cl-6 Base, D6. -C0-N(R531)(r53i), which: is the same or different from each other and represents a hydrogen atom, a Cl-6 alkyl group or a Cl-6 building base, "D7. -C00R54 , alkylcarbonyloxy C,-6 wherein R54 is a hydrogen atom, a Cl_e alkyl group, a c alkyl group or a C3-8 cycloalkoxycarbonyloxy Ci 6 alkane 1^D8. -C(NH(〇H)) =N-R55, Alumina where R55 is a hydrogen atom, a hydrazine base, (amendment) 318197 383 1322688 and D9. Saturated 5 or 6 membered monocyclic heterocyclic groups &lt; July 1, 1 Dl 〇· 5 members or β 嗣 嗣 取代 , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , 5 members of the pattern or selected cores: one or more of the group consisting of 5 or 6 members of the heteroaromatic group 2 (7) C?-丨4 aralkyl; wherein the alkyl moiety of the OH aramid may be substituted with one or more substituents selected from the group e below, and the aryl moiety may be selected from the group F below. Substituted by one or more substituents: [EM] El · Ci-e alkyl which may be substituted by a hydroxyl group E2. cyano, E3. Rebel, E4·C!-6 alkoxycarbonyl 'E5. phenyl , [F group] F1. Ci-e alkyl group, F2. halogen atom, F3. cyano group, F4. warp group, (amendment) 318197 384 1^22688 m217Tf. Application F5. Cl_e alkoxy which may be substituted by one or more substituents selected from the group consisting of a carboxyl group and a Cie alkoxycarbonyl group, earth &quot; F6. Teeth Ci-6, F7. , F8. Cm alkoxycarbonyl, F9. -CO-N(R56a)(R56a.), wherein R56a&amp; R56a' are the same or different from each other and represent a hydrogen atom, 3 to a saturated atom of a nitrogen atom or a 6-membered monocyclic heterocyclic group, or a Ch alkyl group, which may be substituted with one or more substituents selected from the group f below: Group [f] anthracene, mono-Cl-6 alkylamino group, 3. Cl - 6 姨 (ylamino, f4. fluorenyl, φ f5. Ch alkoxycarbonyl, f 6. thiol, and f 7. saturated 5 or 6 membered monocyclic ring containing at least one nitrogen atom a heterocyclic group, F10. -N(R56b)(R56b)' wherein Rs6b and Rs6b are the same or different from each other and represent a hydrogen atom, Ch alkyl may be substituted with an imine group, and an aralkyl group may be selected from One or more of the groups consisting of an imine group and a halogen atom are the same or different. 385 (Revised) 318197 Patent No. 95,921,217 (July 1st, 1998) ^Parts taken The brewing base can be substituted by &amp; calcination, Ch calcination: - aryl-based 'amino-branched' 'mono-CH-amino-indenyl group, Fll. -N=CR7(~n(r58)( R58·)), wherein R 4 虱 or Cie alkyl, r 58 and r 58 are the same or different from each other and represent a hydrogen atom or a 6 alkyl group, a monocyclic heteroaryl group, an oxy group or an ethyl group 5 or 6 and F13. fluorenylene or alkyl and 5 and/ or: alkyl: one or more of the following G groups, wherein the heteroaryl can be substituted with a substituent : [G Group] One or more of the S groups Take Gl. Ci-e, which can be substituted by the following substituents: [g group] gl. halogen atom, g2. amine group, g3. early Cl-6 alkylamino group, g4. diCl-6 Anthranyl 'g5. Cl-6 alkoxy-l-amino group, (amendment) 318197 386 1322688 Patent No. 95,921,217, supra (July 1st, 1998) and g6. hydroxyimido group, G2·Tooth atom, G3. Ci-6, which can be substituted by a halogen atom, G4. aryloxy, G5. cyano, G6.-N(R59a)(R59a), Wherein R59a and R59a are the same or different from each other and represent a hydrogen atom or a Cm alkyl group, or R59a&amp; may together form a saturated 5- or 6-membered monocyclic heterocyclic ring together with an adjacent nitrogen atom, and the saturated heterocyclic ring may be Substituted by one or more identical or different substituents selected from the group consisting of hydroxyl, amine, mono-Cl-6 alkylamino and di-Ci-e alkylamine, G7.-C0- N(R59b)(R59b), wherein R and R59b are the same or different from each other and represent a hydrogen atom, a saturated 5 贞 or 6 贞 monocyclic (tetra) ring group, or a Gi e silk ring group substituted, a hetero G8. aryl group, and a benzyl substituted ', a member of a monocyclic aryl group which can be succinct or turned or R and FT Together with the adjacent nitrogen, this member is a monocyclic heterocyclic ring in which _ and saturated 5 members or 6 and the saturated heterocyclic ring may have a double bond with the benzene ring to form a condensed ring, which may be abruptly entangled (revision) 318197 387 丄 422688 No. 951182; nicknamed patent application (July 1st, 1998; the saturated heterocyclic ring forming a condensed ring can be selected from the group consisting of il atom, Cm alkyl group, Cm alkoxy group 'carboxy group and C! Substituting one or more substituents of the group consisting of -6 alkoxycarbonyl groups. The pharmaceutical grade for treating or preventing diabetes according to claim 1, wherein the ratio of salic compounds is as follows The formula (II,) represents the ratio of ° to the compound: Wherein R, R, R3, R4 and R5 are as defined in the scope of the patent application. 4) If you apply for a patent scope! A pharmaceutical renter for treating or preventing diabetes, wherein the sputum compound is a β-salt represented by the following formula (1)) Wherein V and R5 represent a halogen atom or a hydrogen atom Cj-6 alkyl group.辛 请 专利 专利 专利 专利 专利 专利 专利 专利 专利 专利 专利 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 a pharmaceutical composition, wherein Rla is a hydrogen atom and R3a is a gas atom or Cm alkyl f. Patent Application No. 95,921,217 (July 1, 2008), R2a is a fluorine atom or as a patent application The composition, the pyrazole compound: The medicinal compound for the treatment or prevention of diabetes in the fifth item is represented by the following formula (III) OID is a pharmaceutical composition of diabetes according to any one of claims 2 to 6, wherein r is selected from the group consisting of (1) a hydrogen atom; a group for treating or preventing the following groups·· One or more substituents (2) Ch alkyl which may be substituted by a group selected from the group consisting of: / [A ' group] A' 1. hydroxyl group, 2. Ci-4 methoxy, -N(R41)(R4r), wherein R41 and R4r沘a represent the same hydrogen atom or the same saturation, and are the same or different from each other; W of the two together with an adjacent nitrogen atom or a 6-shell early ring heterocycle, A 4. phenyl, (amendment) 318197 389 A, 5 A, 6 5 or 6 membered monocyclic heteroaryl-C0- N(R411)(r4ii.), &quot; Patent Application No. 95,921,217 (July 1, 1998) wherein R41丨 and R4丨1 are mutually cypresses π Γ 4Π λ C equine or different and represent hydrogen Atom or Ch alkyl; or R4丨1 and R4丨丨' can be linked to a 5- or 6-membered monocyclic heterocycle, A' 7.carboxy, and A' 8 Cm alkoxycarbonyl, (3) C2-6 alkenyl, (4) C2-6 block, (5) C3-8 cycloalkyl; and (6) cycloalkyl Ch alkyl. The pharmaceutical composition for treating or preventing diabetes according to any one of claims 2 to 6, wherein R5 is a G-alkyl group. The pharmaceutical composition for treating or preventing diabetes mellitus according to any one of claims 2 to 6, wherein r5 is c&quot; cycloalkyl group, which can be selected from 2 &amp; base, suspending group and Ci-e One or more identical or different substituents of the group consisting of an alkoxy group are substituted. The pharmaceutical composition for treating or preventing glycocalyx according to any one of claims 2 to 6, wherein R5 is a C3 s cycloalkyl 6 alkyl group. The pharmaceutical composition for treating or preventing diabetes according to any one of claims 2 to 6, wherein the saturated 5- or 6-membered single &amp; heterocyclic group may be selected from the group consisting of sulfhydryl groups. And one or more substituents of the group consisting of _c〇_(Alk)n_c〇〇R52, wherein R52 is hydrogenogen 390 (revision) 3]8]97 1322688 • called Ding υ 睛 宏Or Cl-6 alkyl base integer. (July, 1998, Aik is a Ci-4 extension and a medicinal composition for the treatment or prevention of diabetes, as in 〇 or 1 to 3, as claimed in any one of claims 2 to 6. Wherein R5 is phenyl which may be substituted by one or more substituents selected from the group D' below: [D' group] D'l. Ci-4 may be substituted by a thiol group, D, 2. CO-N(R53)(R53,), wherein R53 and R53 are the same or different from each other and represent a hydrogen atom, a Cl-4 alkyl group or a C1-4 alkylsulfonyl group; D, 3. -C00R54, wherein R Is a hydrogen atom, a Ci-4 alkyl group, a Ch alkylcarbonyloxyCl_4 alkyl group or a C3-8 cycloalkyloxy oxyalkyl group, and a D'4.5 or 6 membered monocyclic aromatic The pharmaceutical composition for treating or preventing diabetes according to any one of claims 2 to 6, wherein 1^5 is a C7-aralkyl group and The C7, aryl moiety of the aralkyl group may be substituted with one or more substituents selected from the group consisting of F, group F' 1. Cm alkyl group, F' 2. halogen atom, F' 3. Cyano, (Revised) 318197 391 U22688 Patent No. 95118217 The request (July 1, 1998) F 5 · Cm alkoxy which may be substituted by one or more substituents selected from the group consisting of a carboxyl group and a Ci6 alkoxycarbonyl group, F' 6. Ci-6 alkyl, F' 7. carboxyl, F 8 · Ci-6 alkoxy, F' 9. -CO-N(R56a)(R56a,), wherein R and R5 3 are the same or each other Iso and represents a hydrogen atom, a saturated 5- or 6-membered monocyclic heterocyclic group containing at least one nitrogen atom, or a Cm alkyl group which may be substituted with one or more substituents selected from the group f' below: f' group] f' 1. amine group, f' 2. mono-Ch alkylamino group, ί 3. a Cl-6-based amine group, F' 4. Hydroxy, f' 4. Carboxy, f' 5. Cm alkoxycarbonyl, f '6 · hydroxy, and f'7. 5 or 6 membered monocyclic odors with at least one nitrogen atom saturated a ring group, 'F'10. -N(R56b)(R56b'), wherein the ruler and RS6b are identical or different from each other and represent a hydrogen atom, and the Cm alkyl group may be substituted with an arylene group by an imine group. It can be substituted with one or more identical or different substituents of the halogen atom selected from the imine (Amendment) 318197 392 1322688 patent No. 9591817 (July 10, 1998? and the halogen atom), the aryl stone yellow ugly Alkyl-substituted, C,-6 alkylsulfonyl, fluorenyl, aminomethyl-mono-Ci-6 alkylaminocarbazino or di-Ci-6 alkylamino fluorenyl, F , ll· -N=CR57(-N(R58)(R58·)), wherein R57 is a hydrogen atom or a C1-4 alkyl group, and R58 and r58 are the same or different from each other and represent a hydrogen atom or a Cl_4 alkyl group. F'12·5 or 6 members of a monocyclic heteroaromatic group, • and F'13. anthracenylenedioxy or an ethylenedioxy group. 14. As disclosed in any of claims 2 to 6. Medical composition for the treatment or prevention of diabetes The compound 'wherein R5 is a Cl-6 group substituted by a 5- or 6-membered monocyclic heteroaryl group, and the heteroaryl group may be substituted with one or more substituents selected from the group G' below: [G , Group] • G'丨.Ci-6 alkyl which may be substituted by one or more substituents selected from the group g' below: [g, group] g' 1. halogen atom, g' 2. amine group , g 3. early Cl-6-homo-amino group, S 4.-Ci-6-homo-amine group, g' 5·Ch alkoxycarbonylamino group, and (amendment) 318197 393 1322688 Patent No. 95118217 Case • (July 10, 1998) g' 6. Hydroxyimine, * G' 2. Halogen, 3. Ci_6 alkoxylate which may be substituted by a halogen atom, G'4. aryloxy, G' 5. cyano, G'6. -N(R59a)(R59a'), wherein R59a and R59a' are identical to each other Or a heterogeneous and representing a hydrogen atom or a Ch alkyl group, or R59a and R... together with an adjacent nitrogen atom to form a saturated 5- or 6-membered monocyclic heterocyclic ring, and the saturated heterocyclic ring may be selected from the group consisting of Composition of a group, an amine group, a mono-Ch alkylamino group and a di-Ch-alkylamino group: substituted by one or more substituents of the group, G5 7. -CO-N(R59b)(R59b), wherein R and R59b is the same or different from each other and represents a hydrogen atom, a saturated 5-membered or 6-membered monocyclic heterocyclic group, or a subgroup which may be substituted by a group, φ G' 8. aryl, and, or a 6 member The monocyclic heteroaromatic group may be substituted with a keto group or a sulfur-bearing I group. 15.2 The pharmaceutical composition for the treatment or prevention of diseases in any of the items 2 to 6 of the patent scope, wherein only 4 and r5 together with the adjacent nitrogen atom form one, 5 or 6 members of the single ring system a cyclic group 'wherein the saturated heterocyclic group=the knives may have a double bond and the saturated heterocyclic group may be condensed with the benzene ring, 7, and each ' and # may be condensed with the benzene ring to form the condensed ring. ) 318197 394 1322688 Patent No. 9511821*7 (98 years *7 θ, and heterocyclic groups may be selected from the group consisting of a tooth atom, a Ci_Domain, an oxygen group) and a C alkoxy group Substituting one or more substituents of the group consisting of the groups. 16. The pharmaceutical composition for use in the treatment or prevention of diabetes according to the second aspect of the patent application, wherein the bismuth is incorporated into the preparation. The substance is a pyrazole compound represented by the following formula (IV): (IV) Six 丫 κ 1 is shown as . τ q is defined as the definition of two items, RX丨, χ and RX3 are the same or different from each other and * _ &amp; represents an atom or a substituent selected from group f and &quot;〇 or j to 2 Whole η] F 1 · Cl-6 alkyl, F" 2. Atomic atom, F" 3. Cyano, F" 4. Hydroxy, alkoxy which can be selected from (4) and L-oxyl groups One or more substituents of the group consisting of the sunburst and the C group are substituted for the group 6. Halo c,-6 alkyl F" 7. Carboxyl, F 8 · Cm alkoxycarbonyl (Revised) 3] 幻97 395 1322688 F" 9. _CO-N(R56a)(R56a) wherein R and R56a are the same or different from each other and represent a hydrogen atom, a saturated 5- or 6-membered monocyclic system having at least one nitrogen atom a heterocyclic group, or a Cm alkyl group, which may be substituted with one or more substituents selected from the group consisting of: [Γ] Γ 1. Amino group, Patent Application No. 95,921,217 (July, 1998, pp., f, 2. 2. Single Ch alkylamino group, f 3. a Cl-6 alkylamino group, Γ 4. carboxyl group, Γ 5· (V6 alkoxylate) a carbonyl group, a hydrazone 6. a hydroxyl group, and a f'' 7. a 5- or 6-membered monocyclic heterocyclic group having at least one nitrogen atom, F" 10. -N(R56b)(R56b), wherein R56b and R56b is the same or different from each other and represents a hydrogen atom, and the 匕-6 alkyl group may be substituted with an imido group which may be the same by one or more selected from the group consisting of an imine group and a halogen atom. Substituted by a different substituent, the 'aryl group can be substituted with a Cl-6 alkyl group, a C-6 alkylsulfonyl 'mercapto' aminocarbamyl group, a monoCi-6 alkylamino group Mercapto or di-Cl-6 alkylaminocarboxamidine, F" 11. -N=CR57(-N(R58)(R58·)), wherein R37 is a hydrogen atom or a Ci-e alkyl group, R58 and R58' is a phase 396 (Revised) 318197 13226^ Patent No. 95118217 • pi v, , m (July 1st, 1998) Same or different and represents a hydrogen atom or CH 炫, &quot; F I2. 5- or 6-membered monocyclic heteroaromatic, . and F 13. methylene dioxy Or an ethylene dioxy group. 17. The pharmaceutical composition for treating or preventing diabetes according to Item 2, wherein the pyrazole compound is a pyridinium compound represented by the following formula (v): Wherein R4 is as defined in the second item of the patent application scope, and ring W represents a 5-membered member of a monocyclic heteroaromatic group, and Ryi, RY^Ry3 are the same or different from each other and represent a hydrogen atom selected from the group consisting of u氺卞A The following is given to G, the substituent of the group 'and m is 〇 or an integer of 1 to 2, [G, group] G' 1. The Ci-6 can be selected from the following group, one of the S groups or Substituted by a plurality of substituents: [g, group] g' 1. halogen atom, g' 2. amine group, g' 3. mono C!-6 alkylamino group, g' 4. di Cm alkylamino group , (Amendment) 318197 397 ^22688, Patent Application No. 95118217 (July 10, 1998) 5. Ci_6 alkoxyamino group, and C. g' 6. hydroxyimine group, G' 2. halogen atom, G'3. C!-6 alkoxy group which can be substituted by a functional atom, G' 4. aryloxy, G' 5. cyano, G,6. -N(R59a)(R59a'), wherein R and R are the same or different from each other and represent a hydrogen atom or C -6 alkyl group or R591 R... together with adjacent nitrogen atoms to form a saturated a 5- or 6-membered monocyclic heterocyclic ring' and the saturated heterocyclic ring may be selected from the group consisting of a trans-group, an amine group, a mono-Ch-alkylamino group, and a di-Ci 6-based amine group: one or more of the groups Substituted by a substituent, 7. -C0-NCR59b)(R59b), wherein the broad and broad are identical or different and represent a hydrogen atom, a 5- or 6-membered monocyclic heterocyclic group of =, or a Ci_. It can be substituted by fluorenyl, G 8. aryl, and uy. fluorenyl substituted. A ring-based heteroaromatic group which can be used for the treatment or prevention of diabetes by the sulfhydryl group or sulfur 18. 2, for example, the claim 11 ring is a (four) ring, a three-presence scorpion ring. Patent Application No. 18, for the treatment or prevention of diabetes (amendment) 318197 398 1322688 Patent Application No. 95218217 (J1 Pharmaceutical Composition of July 10, 2008) wherein the η-pyrazole compound is as follows The general formula (VI) represents the bismuth compound: (VD wherein R4, RY1, RY2, RY3, and m' are as described above. The pharmaceutical composition for treating or preventing diabetes according to claim 2, wherein the pyrazole compound or pharmaceutically acceptable thereof The salt is selected from the group consisting of 5-(2-gas-4,5-difluoro-benzoinylamino)-iH-pyrazole-3-derivative (pyridin-3-ylindenyl) - decylamine, 5-(2- gas-4,5-difluoro-phenylhydrazino)-lH-pyrazole-3-hypoacid (pyridin-3-ylindenyl)-nonylamine dihydrochloride Salt, Lu 5_(2-chloro-4, 5-difluoro-benzylidenylamino)_1H-pyrazole-3-carboxylic acid (pyridin-3-ylindenyl)-decylamine hydrochloride, 5- (2-Ga-4, 5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid (4-mercapto-oxazol-5-ylindenyl)-nonylamine, 5- (2-Ga-4, 5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid (4-mercaptopurin-5-ylmethyl)-decylamine, 5-( 2-chloro-4, 5-difluoro-benzylidenylamino)-1Η-pyrazole-3-carboxylic acid (4-methyl-oxazol-5-ylmethyl)-nonylamine p-benzenesulfonate Acid salt, 5-(2-chloro-4,5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxy 399 (amendment) 318197 1322688 No. 95118217 Application (July 1998, 1 ''acid (4-mercapto-iso-s-hydrazinyl)-nonylamine L-(+) tartrate, 5-(2-chloro-4, 5-difluoro- Benzoylaminopyrazole~3, phthalic acid (2,4-dimercapto-oxazol-5-ylindenyl)-nonylamine p-toluenesulfonate, 5-(2-chloro-4, 5-difluoro-phenylhydrazinoamino)_1Η-. than 嗤-3 - acid (2,4-dimethyl-. oxa-sodium-5-yl fluorenyl)-nonylamine, 5-(2 -Chloro-4,5-difluoro-benzhydrylamino)-1Η-% sal _3~~ acid (2,4-dimethyl-pyridine-3-ylmethyl)-decylamine, 5-(2-chloro-4,5-difluoro-phenylhydrazinoamino)-1Η~-bizozolyl-3-diethyl decylamine, 5-(2-chloro-4, 5-di Fluoro-benzoguanidino)-1Η-specific than s__3~ decanoic acid ethyl-(pyridin-4-ylmethyl)-decylamine, 5-(2-chloro-4, 5-difluoro-benzene曱醯.Amino-amino)-1Η~pyrazine-3 tacrotic acid (2-methoxy-ethyl)-methyl-decylamine, 5-(2 - gas-4,5_-gas-branched Amino group)-1Η~π is more than salicyl-3-ethylo-(2-methoxy-ethyl)-amidamide, • 5 —(2~chloro-4, 5-difluoro-benzamide Amino)-1{}-pyrazole-3-carboxylic acid 2-fluoro-tuberamine, 5-(2-gas-4, 5-difluoro-benzhydrylamino)-1H_D-biazole 3-carboxylic acid 3-fluoro-tuberamine, 5-(2- gas-4, 5-difluoro-benzylidenylamino)_1H-pyrazole-3-carboxylate 2-didecylamino- Benzylamine, 5-(2-chloro-4, 5-difluoro-phenylhydrazinyl)-pyrazole. Monocarboxylic acid (4-ethoxycarbonyl-cyclohexyl)-propyl-decylamine, 5-(2-Chloro-4,5-difluoro-benzhydrylaminopyridyl- 3 -carboxyl (Revised) 318197 400 Patent Application No. 95,921,217 (July 10, 1998) Acid (6-曱oxypyridin-3-ylmercapto)-nonylamine, 5-(2- -4, 5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid 2,3-dimethoxy-benzylamine, 5-(2-chloro-4, 5-di Fluoro-benzoguanidino)-1Η-pyrazole-3-carboxylic acid 2,4-dimethoxy-benzylamine, 5-(2-chloro-4, 5-difluoro-phenylhydrazine Amino)-1Η-°biazole-3-carboxylic acid 2,6-dimethoxy-benzylamine, 5-(2-chloro-4,5-difluoro-benzoinyl)-1Η -pyrazole-3-carboxylic acid 3,5-dimethoxy-benzylguanamine, 5-(2-chloro-4,5-difluoro-benzylidenylamino)-1Η-pyrazole-3- Carboxylic acid 3,4-dimethoxy-benzylamine, 5-(2-gas-4,5-difluoro-phenylhydrazino)-1Η-°biazole-3-carboxylic acid 2, 3 -difluoro-benzylamine, 5-(2- gas-4, 5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylic acid 2,4-difluoro-benzylamine, 5-(2-Gas-4, 5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylic acid 2, 5-difluoro-benzylamine, 5-(2-chloro-4 , 5-difluoro-phenylhydrazinoamino)-1Η-°biazole-3-carboxylic acid 2,6-difluoro-benzylamine, 5-(2-chloro-4, 5-difluoro-benzene Mercaptoamino)-1Η-pyrazole-3-carboxylic acid 3,4-difluoro i-tuberamine, 5-(2-chloro-4, 5-difluoro-benzoinyl) 1Η-pyrazole-3-carboxylic acid 3,5-difluoro- Amine, 5-(2-chloro-4,5-difluoro-benzoylaminopyrazole-3-carboxyl 401 (Revised) 318197 1322688 Patent Application No. 95118217. (July 10, 1998) ) acid (2-isopropoxyl-indol-3-ylindenyl)-nonylamine, • 5-(2-chloro-4,5-difluoro-benzoamitoyl)-1Η-pyrazole- 3-carboxylic acid (2-octyloxy-π ratio -3-ylindenyl)-bristamine, .5_(2-gas-4,5_two-machine-branched amine group)-111_〇 〇3* tempering acid (3,5-difluoro-pyridin-2-ylmethyl)-decylamine, 5-(2- gas-4, 5-difluoro-benzoylamino)- 111-〇比〇 sit-3-pyreoic acid 2-trifluoromethyl-benzylamine, 5-(2-chloro-4,5-difluoro-phenylhydrazinoyl)-1Η-°-by-azole- 3-carboxy-acid 3-trifluoromethyl-benzylamine, 5-(2-chloro-4,5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid 4-three Fluorinyl-benzylguanamine, 5-(2-chloro-4,5-difluoro-phenylhydrazino)-1Η-° ratio 0 sit-3-rebel 4-tert-butyl-benzyl hydrazine Amine, 5_(2_乱-4,5_-gas-presentylamino)_ 1Η_0 ratio 0 sitting_3_capric acid (6-isopropoxy-pyridin-3-ylmethyl)-decylamine , Lu 5_(2_气-4,5_* —Mouse-Benchanoylamino)-1Η _β is 0-acidic [2-(2,2,2-trifluoro-ethoxy)-indole-triazyl-3-ylmethyl]-nonylamine, 5-(2-chloro-4, 5-difluoro-phenylhydrazinoamino)-ιη-pyrazole-3-carboxylic acid 4-(2-dimethylamino-ethylaminomethylindenyl)-benzylamine, 5-(2 -Wind-4, 5-difluoro-benzoylamino-salt-3-sodium 4-ethyl-tertiary amine, 5-(2-chloro-4, 5-difluoro-benzoguanamine Base]~ih-pyrazole-3-carboxylic acid 4-isopropyl-benzylguanamine, 5-(2-chloro-4,5-difluoro-benzylidenylamino)-11|-pyrazole- 3-Carboxy 402 (Revised) 318197 1322688 Patent Application No. 95118217 • ^ (July 1st, 1998) Acid 2 Gas-6-Fluorine-Manicamine, • 5 (2~Ga-4, 5- Difluoro-benzhydrylamino)-1H-pyrazole-3-carboxylic acid (6 ethoxy_. Than -3-ylindenyl)-bristamine dihydrochloride, chloro- 4, 5-difluoro-phenylhydrazino-yl)_1{1_pyrazole-3-carboxylic acid (sold ~4 -ylmethyl)-nonylamine, 5-(2-chloro-4,5-difluoro-phenylhydrazinoyl)_iη-pyrazole-3-carboxylic acid [6-(2, 2, 2-three Fluorine-ethoxy)-pyridin-3-ylindenyl]-nonylamine dihydrochloride, Lu 5 (2 gas-4,5-one mouse-benzylamino)- ιη_〇 than saliva- 2-nonanoic acid 2,6-dimethyl-benzylamine, 5-(2-chloro-4,5-difluoro-benzhydrylamino)_1珏-pyrazole-3-carboxylic acid [2- (pyridin-3-yl)-thiazol-4-ylindenyl]-nonylamine dihydrochloride, 5-(2-chloro-4,5-difluoro-phenylhydrazinoyl)_ιη-pyrazole- 3-carboxylic acid (1Η-benzopyran-2-ylindenyl)-guanamine dihydrochloride, [4-({[5-(2- gas-4,5-difluoro-benzhydryl) Amino)- 11]-pyridazolium-3-ylcarbonyl]monoaminophenyl)-benzylideneamino]-acetic acid decyl ester, 3-[4-({[5-(2- gas-4, 5-difluoro-phenylhydrazinoamino)-111- ° than sal-3-cyano]-aminophenylmethyl)-benzhydrylamino]-propionic acid formazan, 5-(2-chloro- 4, 5-Difluoro-benzhydrylamino)-ιη-pyrazole-3-carboxylic acid (2-mercapto-thiazol-4-yl) Methyl)-decylamine dihydrochloride, 5-(2- gas-4, 5-difluoro-phenylhydrazinoyl)-ιη-pyrazole-3-carboxylic acid (3, 5-dimethyl -isoxazole-4-ylmethyl)-decylamine, 5-(2-chloro-4,5-difluoro-phenylhydrazinoamino)_1Η-pyrazole-3-carboxylate 403 (amendment) 318197 1322688 Patent Application No. 95118217 (July 10, 1998) 4_[2_贰-(2-Ethyloxyethyl)-amino-ethylaminomethylmercapto]-benzylamine, 5-(2-chloro-4, 5-difluoro-benzamide Amino)1H_pyrazole-3-carboxylic acid 4-(2-trans-ethylaminomethylmercapto)-benzylamine, 5-(2-chloro-4, 5-difluoro-benzoic acid 4-{2-[(2-Ethyloxyethyl)-(2-hydroxyethyl)-amino]-ethylamine based on mercaptoamine)-ih-pyrazole-3-carboxylic acid Base} ~ 醯amine, 5-(2-chloro-4,5-difluoro-phenylhydrazino)-ih-pyrazole-3-carboxylic acid (1-methyl-1H-benzimidazole_2-ylindenyl)_ Indole hydrochloride, 5-(2-chloro-4, 5-difluoro-phenylhydrazino)-ih-pyrazole-3-carboxylic acid (嗟哇-2-ylmethylguanamine diphosphate) Acid salt, 5-(2-a-4,5-difluoro-phenylhydrazino)-ih-pyrazole-3-carboxyl (benzopyrene~2~yl)-醯Amine dihydrochloride, 5~(2'' gas-4, 5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxyg complex (2 5__ 'monomethyl''嗟嗤-4-ylmethyl)-chiral amine dihydrochloride, ^ 5~(2~5-difluoro-benzhydrylamino)-lH-pyrazole-3-carboxy&amp;[2(马嘴-4-yl)-thiazol-4-ylindenyl]- Indoleamine dihydrochloride, 5 ~ ~~ ^ 〇 "one gas-4, 5-difluoro-phenylhydrazinoamino)-1 Η-pyrazole-3-carboxylic acid (1 3 ς _ ' ' dimethyl Base-1Η-° ratio. sit-4-yl fluorenyl)-bristamine, chloro-4, 5-difluoro-phenylhydrazinoamino)-1 Η-pyrazole-3-carboxylic acid (2-, β,~Bumethyl-η-pyridin-3-ylindenyl)-decylamine dihydrochloride, 5, (? & ^~虱-4, 5-difluoro-benzhydrylamino)-1Η- Pyrazol-3-monoamino-thiazol-4-ylindenyl)-decylamine dihydrochloride, gas ~4,5-difluoro-benzhydrylamino)-1Η-π than saliva-3 - 404 (Revised) 318197 1322688 Patent Application No. 95118217. (July 1st, 1998) Acid (I-Methyl-1H-*» 比略_2-ylmethyl)-decylamine, 5 (2 gas - 4,5_ - gas - this brewing · arylamino group 〇 竣 竣 竣 acid (3,4-dimethoxyl than butyl-2-ylmethyl)-nitramine dihydrochloride , 5-(2-chloro-4,5-difluoro-phenylhydrazino)-111-pyrazole-3-carboxylic acid (5-t-butyl-thiazol-2-ylmethyl)-oxime Amine dihydrochloride , 5 (2 chaos - 4,5 a gas _ 曱 基 基 )) - ΐΗ - ° than 〇 sitting -3- acid (5-methyl-2-phenyl-2 Η - [1, 2, 3] Triazol-4-ylmethyl)-decylamine, 5 (2 chloro-4,5-fluoro-benzylamino)-iH-u ratio. Sodium-3-pyruic acid [4-( Dibutyloxycarbonyl-amino)-methyl-n ratio nitr-2-ylindenyl] monoamine, 5 (2 chaotic-4,5-&gt;-fluoro-benzylamino)-oxime- π 〇 竣 竣 竣 竣 [4-methyl-2-(morpholin-4-yl)-thiazol-5-ylindolyl]-nonylamine dihydrochloride, 5-(2-chloro-4 , 5-difluoro-phenylhydrazinoamino)_1H_pyrazole-3-carboxylic acid (pyridin-3-ylindenyl)-decylamine 3/2 hydrochloride hemihydrate, φ 5-(2- Gas-4,5-difluoro-phenylhydrazinylaminopyrazine-monopyrazole 2-amino-benzylamine, 5-(2-chloro-4, 5-difluoro-benzamide Aminopyrazole, benzoic acid, 2-methoxy-benzylamine, 5-(2-gas-4, 5-difluoro-benzhydrylamino)-ih-pyrazole _3 Acid 3-decyloxy-benzylamine, 5-(2-chloro-4,5-difluoro-phenylhydrazino)-ih-pyrazole-3-acidic 4-methoxy-benzylhydrazine Amine, 5-(2-chloro-4, 5-difluoro-phenylhydrazino)-111-indoleazole-3 identical 405 (corrected Patent application No. 318,197, No. 95,921,217 (July, 1998) 醆 4-mercapto-benzylamine '5-(2-chloro-4,5-difluoro-benzoamitoyl)_1H-pyridyl Oxazole-3-carboxylate 4~fluoro-benzylamine '5 (2-gas-4, 5-difluoro-benzhydrylamino)-ih_0 than vomit 3--------- 4~ gas-tuber , 5-(2-chloro-4, 5-difluoro-anthracenylamino)_1H_0-biazole-3-carboxylic acid·4-ethoxycarbonyl-benzylamine, 5 (2-fluoro-4, 5 - iih- 甲 基 胺 ) _ _ -3- -3- -3- -3- -3- -3- 4- 4- 2- 2- 4- 4- 4- 4- 4- 4- 4- 4- 4- 4- 4- 4- 4- 4- 4- 4- 4- 4- 4- 4- 4- 4- 4- 4- 4- 4- 4- 4- 4- 4- 4- 4- _pyrazole-3-carboxylic acid dibenzylamine, 5-(2-gas-4, 5-difluoro-benzhydrylamino)-ιη-indopazole-3-carboxy, (cyano-benzene Base-methyl)-bristamine, 5 (2 gas 4,5 - one gas - the present arylamino group)_1Η_π ratio 0 sitting -3_slow acid cyclohexyl decyl-decylamine, 5-(2-chloro- 4,5-difluoro-phenylhydrazinoamino)-ιη-pyrazole-3-carboxy^(2-propionyl-ethyl)-phenyl-bristamine, 5-(2-gas-4, 5 -difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid cyclohexyldecyl-decylamine, 5-(2-chloro-4, 5-difluoro-benzoinylamino) -1Η-pyrazole-3-carboxylic acid cyclohexyl decylamine, 5-(2-chloro-4,5-difluoro-phenylhydrazino)-1Η-pyrazole-3-rebellious cyclohexyl-ethyl-decylamine, 5_(2_chloro-4, 5- Difluoro-benzhydrylamino)-1Η-pyrazole-3-rebel 406 (amendment) 318197 Patent Application No. 95,921,217 (July 1st, 1998) Acid allylcyclohexyl-decylamine, 5-(2-Gas-4, 5-difluoro-phenylhydrazino)-ih-indole-3-hydroxy-cyclohexyl-indole-But-2-ylindenyl--bristamine, 5-( 2-Chloro-4,5-difluoro-phenylhydrazinoylaminopyranyl-3-carbazinyl-(1-methyl-piperidin-4-yl)-decylamine, 5-(2-chloro -4, 5-Difluoro-benzoylamino)-lH_o is 0--3-carboxylic acid [(3,4-ylidenedioxyphenyl)-fluorenyl]-decylamine hydrochloride , 5-(2-chloro-4, 5-difluoro-benzoylamino)-1H-d than s--3-hydroxybenzoic acid benzyl-butyl-decylamine, 5_(2-gas_4, 5_-murine-benzolic amino group)-1Η-α is more than 0--3-oxalinyl-(4-carboxy-butyl)-guanamine hydrochloride, 5-(2-chloro-4, 5-difluoro-benzhydrylamino)-1Η-pyrazole-3-tagamic acid butyl-ethyl-decylamine, 5-(2-chloro-4, 5-difluoro-benzimidamide Base)-1Η-°biazole-3-carboxylic acid cyclohexyl-propyl-decylamine, 5-(2-chloro-4, 5-di Fluoro-benzoguanidino)-1Η-pyrazole-3-carboxylic acid butyl-cyclohexyl-decylamine, 5-(2-chloro-4, 5-difluoro-benzhydrylamino)- 1Η-pyrazole-3-carboxylic acid cyclohexyl-(2-decyloxy-ethyl)-decylamine, 5-(2-chloro-4, 5-difluoro-phenylhydrazino)-1Η- Pyrazole-3-carboxylic acid cyclohexylpyridin-3-ylindenyl)-decylamine, 5-(2-chloro-4, 5-difluoro-benzoinyl)-1Η-pyrazole-3 -carboxylic acid [2-(morphin-4-yl)-phenyl]-nonylamine, 5-(2-chloro-4,5-difluoro-phenylhydrazino)-1Η-pyrazole-3 - Carboxy 407 (Revised) 318197 1322688 * Patent Application No. 9511821 - (July 10, 1998) Dibutylammonium, 5-(2-chloro-4, 5-difluoro-phenylhydrazine) Amino-based)-1H-0-pyrazole-3-monocarboxylic acid-(2-decyloxy-ethyl)-amidamine, 5-(2-chloro-4,5-difluoro-benzoinyl)_1H 1-pyrazole_3_decanoic acid (2-methoxy-ethyl)-propyl-decylamine, 5-(2-chloro-4, 5-difluoro-benzylidenylamino)_1H_pyrazole _3-Carboxylic acid butyl-(tetrahydro-l-butan-4-yl)-nitramine, 5-(2-chloro-4, 5-difluoro-abidocarboxamido) 1H_pyrazole_3 _Carboplatin (2_methyllacyl-ethyl)_(tetrahydro-〇辰味~4-yl)-bristamine, 5-(2-chloro-4,5-difluoro-benzylidenylamino)- 1H-pyrazole-3-carboxycarboxylic acid cyclopentyl-(2-decyloxy-ethyl)monodecylamine, 5 -(2-Gas-4, 5-difluoro-phenylhydrazinoamino)- 1H_pyrazole_3_carboxylic acid cyclohexyl-(3-methoxy-propyl)-bristamine, 5-( 2- gas-4,5-difluoro-benzhydrylamino)_;[η-pyrazole_3_carboxylic acid cyclohexyl-(2-ethoxy-ethyl)-decylamine, • 5_( 2—Gas-4,5-Difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid cyclohexyl-(2-isopropoxy-ethyl)-decylamine, 5 (2 - gas-4, 5-fluoro-benzylamino)-1{]-〇 ratio ° sit-3-oxocyclohexyl-(2-propoxy-ethyl)didecylamine, 5- (2-Chloro-4, 5-difluoro-benzoylamino)-ΐΗ-η than 嗤-3-carboxylic acid (1-ethyl-propyl)-(2-methoxy-ethyl) _ 醯 ,, 5-(2-chloro-4, 5-difluoro-benzylidenylamino) Η 吡 pyrazole _3 carboxylic acid butyl-(1-tert-butoxycarbonyl-piperidine _4 _ base)-nonylamine, 5 (2 gas - 4,5 - one gas - benzoquinone amino group) - 1 {1-〇 ratio ° sitting -3 slow 408 (amendment) 318197 Patent 95118217 patent Shen Hong ( July 1998 1 〇3 3 acid butyl-(tetrahydro-thiopiperazin-4-yl)- Amine, 5-(2-chloro-4, 5-difluoro-benzhydrylamino)-lH-pyrazole-3-furoic acid (2-decyloxy-ethyl)-decylamine, 5-( 2-Chloro-4, 5-difluoro-phenylhydrazinoamino)-lH-pyrazole-3-carbamic acid butyl-(β-pyridin-3-ylindenyl)-decylamine, 5-(2 - gas-4, 5-difluoro-phenylhydrazinoamino)-lH-pyrazole-3-decanoic acid benzyl-(2-decyloxy-ethyl)-decylamine, 5-(2-chloro -4,5-difluoro-phenylhydrazinoamino)-indole-pyrazole-3-decanoic acid butyl-(17-bottom-4-yl)-nitramine, 5-(2- gas-4, 5-difluoro-phenylhydrazinoamino)-lH-pyrazole-3-sodium acid (1-ethyl ketone _tI base)-butyl-decylamine, 5-(2- gas-4, 5-difluoro^-benzoquinoneamino)- 1H-0 than salino-3-butanoic acid butyl-(1-anthracene-branched 4-yl)-nitramine, 5-(2 -Chloro-4,5-difluoro-anthracenylamino)-iH-pyrazole-3-hypoacid butyl-(1-ethoxyxyl-based base-4-yl)-guanamine, 5- (2-Chloro-4, 5-difluoro-benzhydrylamino)-ιη-pyrazole-3-buffered acid butyl _(1_acidic liquor-D bottom bit-4-yl)-stuffed Amine, 5-(2-gas-4, 5-difluoro-anthracenylamino)-ih-pyrazole-3-hypoacid butyl-(1,1-dimercapto-hexahydro-1 λ 6-sulfur 0 bottom _ -4- - indoleamine, 5-(2-chloro-4, 5-difluoro-phenylhydrazino)-ιη-pyrazole-3-buffer acid butyl _(1-_yl_hexahydro-1λ4- Thiophenan-4-yl)-bristamine, 5-(2-chloro-4,5-difluoro-benzhydrylamino)-ιη-carbazole-3-carboxylic acid (6-decyloxy- ° than biting-3-ylmethyl)-propyl-decylamine, 5_(2-gas_4,5_·- disorder-benzanoylamino)- 1Η_α than 〇-3 - Rebel 409 (Revised ) 318197 1322688 Patent Application No. 95118217 (July 1, 1998) Acid propyl-(〇比咬-3-ylmethyl)-imidamine' • 5-(2-chloro-4, 5-di Fluoro-benzoguanidino)-1Η-pyrazole-3-carboxyl-acid 4-diethylaminocarbazyl-benzylamine, 5-(2-chloro-4, 5-difluoro-benzene Mercaptoamino)-1Η-indazole-3-carboxylic acid 3-diethylaminoindenyl-benzylguanamine, 5-(2-chloro-4,5-difluoro-benzoguanamine -1Η-pyrazole-3-carboxylic acid 4-ethylaminopurinyl-benzylguanamine, 5-(2-chloro-4,5-difluoro-benzoquinoneamino)-1Η- π is 0 -3--3-致 _ acid 3-ethylaminomethyl hydrazino-benzyl hydrazine, 5- (2-chloro-4,5-di-n-phenyl fluorenylamino)-111-0 ratio ° sit-3 - dihydro acid 4-aminoformyl-benzylamine, 5-(2-chloro-4, 5-difluoro-benzhydrylamino)-111-0-pyrazole-3-carboxylic acid (1-acid oxalyl-piperidin-4-yl)-propyl-decylamine, 5-(2- Chloro-4,5-dioxa-benzimidylamino)-1Η_0 is 0 -3- oxo acid (1-carboxyethyl-piperidin-4-yl)-propyl-decylamine, • 5 -(2-chloro-4,5-difluoro-benzoylamino)- 1H-° ratio 0 sitting-3-decanoic acid [1-(2 - succinyl propyl aryl)-ninus -4- 5-propyl-nonylamine, 5-(2- gas-4, 5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylic acid cyclopropyl-(6-methoxy Bispin-3-ylindenyl)-nonylamine, 5-(2-chloro-4,5-difluoro-benzylidenylamino)_1H-pyrazole-3-carboxylic acid cyclobutyl-(6- Methoxy-pyridin-3-ylmethyl)-decylamine, 5-(2-chloro-4,5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid cyclopropyl Methyl-(6-decyloxy-pyridin-3-ylmethyl)-decylamine, 5-(2- gas-4, 5-difluoro-phenylhydrazino)-1Η-pyrazole-3 -Carboxy 410 (Revised) 318197 1322688 Patent Application No. 95118217 (July 1st, 1998) Acid (6-Didecylamino-pyridin-3-ylindenyl)-nonylamine, 5-(2) -Chloro-4, 5-difluoro-abidocarboylamino)-1H-b-pyrazole-3-derivative (6-didecylamine) Yue than bite-3-yl) - propyl - Amides, 5- (2-chloro-4,5-difluoro - phenyl stuffed Yue-ylamino) -ih-.嗤-3-carboxylic acid aryl-(2-mono-ethyl)-bristamine, 5-(2-chloro-4, 5-difluoro-benzoguanidino)-ιη-pyrazole- 3-carboxylic acid nodal group - (2-ethoxylated-ethyl)-bristamine, 5-(2-chloro-4, 5-difluoro-benzoinyl)-ιη-pyrazole-3 -Carboxylic acid (6-chlorobite _3_ylmethyl)-propyl-decylamine, 5-(2-chloro-4, 5-difluoro-phenylhydrazino)-iH-pyrazole 3-carboxylic acid 2,6-dioxa-benzylamine, 5-(2-chloro-4,5-difluoro-benzylidenylamino)_ih-pyrazole-3-carboxylic acid (3, 5 _Di-pyridin-4-ylindenyl)-decylamine, 5-(2-gas-4,5-difluoro-phenylhydrazinoylamino)-ih-pyrazole-3-carboxylic acid (3, 5-Dichloro-pyridin-4-ylindenyl)-propyl-decylamine, I 5-(2-Gas-4, 5-difluoro-phenylhydrazinoyl)_ih-pyrazole-3-carboxylate Acid [6-(1Η-°Bizozol-1-yl)~pyridin-3-ylmethyl]-decylamine dihydrochloride, 5-(2-chloro-4, 5-difluoro-benzhydryl) Amino)_}η-pyrazole_3_carboxylic acid [6-(4-hydroxy-piperidin-1·yl)-pyridin-3-ylmethyl]-decylamine dihydrochloride, 5-(2 _Chloro-4, 5-difluoro-benzylidenylamino)-ih-pyrazole-3-carboxylic acid (2-D ratio bite-2-yl-ethyl)-acid amine, 5-(2- Chlorine-4, 5_two -benzimidylamino)-ih-pyrazole-3-carboxyl 411 (amendment) 318197 132268" Patent Application No. 95118217 (July 1, 1998) Acid (2-. Benzyl-ethyl)-bristamine, 5 (2chloro~4'5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid (2-pyridyl, ethyl)-decylamine , 5 (2-gas-4,5-difluoro-benzhydrylamino)-pyrazole-3-carboxylic acid (4-[1'2,3]thiadiazole-4-yl-benzyl)_ Indoleamine, 5 (2chloro~4,5-difluoro-l-decylamino)_1H-pyrazole-3-carboxylic acid (5-fluorenyl, wellsyl-methyl)-acid amine, 5 ( 2 chloro ~4'1~difluoro-benzhydrylamino)-1 Η-pyrazole _3-carboxy φ acid ° ratio 卩 well-2-yl- ugly amine, 5 (2 gas-4, 5-two Fluoro-alum-based amino)-1H_pyrazole_3-carboxylic acid quinoline-5-yl-decylamine, 5-(2-gas-4,5-difluoro-benzoinylamino) _1H_pyrazole-3-carboxylic acid quinolin-8-yl-decylamine, 412 (amendment) 318197 1 one (2~ gas~4,5-difluoro-phenylhydrazino)-iH-pyridyl Oxazole-3-carboxylic acid isoindole~5~•yl-bristamine, φ 5 —(2_chlorodifluoro-benzoylamino)_1H-pyrazolecarboxylic acid [3-ethoxy~5 -(Buethoxycarbonyl-1-methyl-B Pyridin-2-yl-decylamine, 5~(2-Gas-4,5-difluoro-benzoamitoylamino)- 1{1-pyrazole-3-carboxylic acid [3_ethoxy-5 -(1-ethoxycarbonyl-1-hydroxy-ethyl)-pyridin-2-yl-decylamine, 5~(2~chloro-4, 5-difluoro-benzylidenylamino)-iH-pyridyl Azole_3-carboxylic acid [1_(1~ aryl-1-methyl-ethyl)_3_ethoxy-pyridine-2-yl]-decylamine patent application No. 95182217 (July 1, 1998) 〇)) 5-(2-chloro-4,5-difluoro-benzhydrylamino)_ih-pyrazole-3-carboxy(1-sulfo--trans-yl-ethyl)_3_ethoxy Specific bite_2_yl]-acid amine, 5-(2-chloro-4, 5-difluoro-phenylhydrazinoyl)_ih-pyrazole-3-carboxylic acid (pyridin-2-ylindenyl) - indoleamine, 5-(2-chloro-4, 5-difluoro-phenylhydrazinylamino)_ih-pyrazole-3-carboxylic acid [6-(thiomorpholin-4-yl)-pyridine- 3-ylindenyl]-nonylamine, 5-(2-chloro-4, 5-difluoro-benzylidenylamino)_in-pyrazole-3-carboxylic acid [6-(1, bis-dione —1 a L-thiomorpholine_4_yl)-pyridine-3-ylmethyl]-bristamine, 5-(2-chloro-4, 5-difluoro-phenylhydrazino)-ih-pyrazole 3-carboxylic acid (4, 5-dibromo-thiophen-2-ylindenyl)-nonylamine, 5-(2- gas-4, 5-difluoro-benzoguanidino)_ih-pyrazole -3- Carboxylic acid (5-a-thiophen-2-ylindenyl)-decylamine, 5-(2- gas-4, 5-difluoro-phenylhydrazinoyl)_ih-pyrazole-3-carboxylic acid ( 4-ethyl-2-methyl-oxazol-5-ylmercapto)-decylamine, 5-(2-gas-4, 5-difluoro-benzhydrylamino)_ih-pyrazole-3 -carboxylic acid (2-ethyl-4-mercapto-oxazol-5-ylindenyl)-guanamine dihydrochloride, 5-(2- gas-4,5-difluoro-benzoguanamine _iH-pyrazole-3-carboxylic acid ([2, 2']bithiophen-5-ylmethyl)-decylamine, 5-(2- gas-4, 5-difluoro-benzoguanamine Base)_ih-pyrazole-3-carboxylic acid (3-decyloxy-thiophen-2-ylmethyl)-nonylamine, 5-(2-chloro-4,5-difluoro-benzoinylamino ) 111-pyrazole-3-carboxylic acid (4,5-dichloro-thiophen-2-ylmethyl)-decylamine, 413 (amendment) 318197 1322688 Patent Application No. 95118217 (June 98) 10曰) 5-(2-chloro-4, 5-difluoro-benzhydrylamino)-1Η-pyrazole_3_carboxy•acid (2, 5-dimercapto-oxazol-4-yl) Methyl)-nonylamine, 5-(2-chloro-4,5-difluoro-benzylidenylamino)-111-°biazole-3-carboxylic acid (2-hexyl-4-methyl-σ Ester-5-ylindenyl)-bristamine, 5-(2- gas-4,5----benzoylamino)- 1Η-σ ratio 17 sits _3-some_acid (4-methoxy-thiophen-3-ylmethyl)-decylamine, 5-(2-chloro-4, 5-difluoro-benzoguanamine Base)-ιη-pyrazole-3-carboxylic acid (4-mercapto-2-phenyl-oxazole-5-ylindenyl)-decylamine, ♦ 5-(2_gas~4,5-difluoro _Benzyl decylamino)-1-pyrazole_3_carboxylic acid (2-methyl-4-phenyl-oxazole-5-ylmethyl)-decylamine, 5-(2-gas-4 , 5-difluoro-phenylhydrazinoamino)_1Η_pyrazole-3-carboxylate (4-hexyl-2-methyl-oxazole-5-ylmethyl)-decylamine dihydrochloride, 5 -(2-Gas-4, 5-difluoro-phenylhydrazino)1Η-pyrazole_3_carboxylic acid (6-chloro-pyridin-3-ylmethylguanamine, 5-(2-gas) -4,5-difluoro-phenylhydrazinoamino)_1Η-pyrazole_3_carboxy•acid (6-chloro-pyridylmethyl)-guanamine dihydrochloride, 5 (2_ gas) 4' 5-Difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid (4Η-[1,2'4]triazolylmethyl)-decylamine, 5-(2- Gas-4, 5-difluoro-phenylhydrazinoamino)_1Η_pyrazole_3_carboxylic acid (4Η-[1,2,4]triazolylmethyl)-decylamine dihydrochloride, 5 -(2-chloro-4,5-difluoro-benzhydrylamino)-1,4-pyrazole-3-carboxylic acid (5-fluoro-4Η -quinazoline, 3_yl)-decylamine, 5-(2-chloro-4,5-difluoro-phenylhydrazinoyl)-1Η-pyrazole_3_carboxylic acid (5-fluoro-4Η- Quinazoline-yl)-nonylamine dihydrochloride, 414 (amendment) 318197 Patent No. 95,921,217 (July 1st, 1998) 5 (2_chloro-4,5~difluoro-benzene) Mercaptoamine)-1Η-pyrazole-3-carboxylic acid (4,6-dimethyl-pyridine~3_ylmethyl)-decylamine, 5-(2-chloro-4' 5~difluoro -benzoylamino)_1H-pyrazole_3_carboxylic acid (4,6-dimercapto-% pyridine~3_ylindenyl)-decylamine dihydrochloride, 5-(2-gas- 4' 5-Difluoro-phenylhydrazinoamino)_1H_pyrazole-3-carboxylic acid (2-methoxy-6-methyl-pyridine-3-ylmethyl)decylamine, 5-(2 -Chloro-4,5-difluoro-phenylhydrazinoamino)_1H_pyrazole-3-carboxylic acid (4-oximeoxy-6-methyl-pyridyl-3-ylhydrazino)-decylamine, 5-(2-Gas-4,5-difluoro-phenylhydrazinoamino)_1H_pyrazole_3_carboxy K4-methoxy-6-methyl~pyridine_3_ylindenyl)_醯Amine dihydrochloride, 5-(2- gas-4,5-acid (2-decyloxy-4,6-5-(2- gas-4, 5-acid (2-methoxy-4, 6-acid salt, a mouse-benzimidyl dimethyl-pyridin-3-ylmethyl)-oxime Amine, difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxydimethyl-pyridin-3-ylindenyl)-nonylamine di-salt 5-(2- gas-4, 5~2 Fluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid (3-mercapto-pyridin-2-ylindenyl)-decylamine 5-(2-chloro-4, 5-difluoro -phenylhydrazinylamino)_1H_pyrazole-3-carboxylic acid (5-fluorenyl-pyridin-3-ylindenyl)-decylamine, 5-(2-ethane-4, 5-difluoro-phenylhydrazine) Nonylamino)_1H_pyrazole-3-carboxylic acid (6-fluorenyl-pyridine-3-ylmethyl) monodecylamine, 5-(2-chloro-4, 5-difluoro-benzoinyl) Amino)_1H_pyrazole-3-carboxylic acid (6-methyl-pyridin-2-ylmethylguanamine, 5-(2,4-dichloro-5-fluoro-phenylnonylamino)_ih -»Bizozole-3-carboxyl 415 (amendment) 318197 Patent No. 95,921,217 (July 1, 1998) Acid (pyridin-3-ylindenyl)-guanamine dihydrochloride, 5- (2-Chloro-4, 5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid (6-fluoro-indenyl-3-ylmethyl)-bristamine dihydrochloride a salt, 5-(2-chloro-4,5-difluoro-benzofuranylamino)-1Η-0 to 0--3-rexamic acid (3-carboxy-phenyl)-methyl-decylamine, 5-(2-chloro-4, 5-difluoro-benzhydrylamino)- 1-indole-pyrazole-3-carboxylic acid 3-indolesulfonylamino-benzamide, 5-(2-chloro-4,5-difluoro-benzylidenylamino)-1Η-pyrazole-3 -carboxylic acid 4-methanesulfonylamino-benzamide, 5-(2-chloro-4,5-difluoro-benzhydrylamino)-iH-pyrazole-3-carboxylic acid 3-B Amidino-benzylamine, 5-(2-chloro-4,5-difluoro-phenylhydrazino)-ih-pyrazole-3-carboxylic acid 4-acetamido-benzylamine, 5-(2-chloro-4,5-difluoro-benzoamitoylamino)-ih-pyrazole-3-carboxylic acid (2-phenyl-indol-4-ylmethyl)-decylamine, 5-(2-Gas-4, 5-difluoro-benzoamitoylamino)_1H_pyrazole-3-carboxylic acid ((R)-l-phenyl-ethyl)-decylamine, 5-( 2-gas-4,5-difluoro-benzhydrylamino)_1H_pyrazole_3_carboxylic acid ((S)-l-styl-ethyl)-decylamine, 5-(2-chloro -4,5-difluoro-phenylhydrazinoamino)_1H-pyrazole-3-carboxylic acid (6-phenoxy-n-pyridin-3-ylmethylguanamine dihydrochloride, 5-( 2-methyl-4,5-difluoro-benzylidenylamino)_1Η-pyrazole-3-carboxylic acid (6-chloro-pyridin-3-ylindenyl)-decylamine dihydrochloride, 5 -(2-chloro-4,5-difluoro-phenylhydrazinoylamino)-indolyl-pyrazole-3-carboxylate (amendment) 318197 416 Patent No. 95118217 Request (July 10, 1998) Acid (2-chloro-pyridin-3-ylmethyl)-guanamine dihydrochloride, 5-(2-amidino-4, 5-difluoro-phenylhydrazine Amino-pyridyl-3-carboxylic acid (6-chloro-pyridin-3-ylindenyl)-guanamine sodium salt, 5-(2-chloro-4, 5-difluoro-benzoquinone Alkyl)-1Η-°biazole-3-carboxylic acid [1-(pyridin-3-yl)-ethyl]-nonylamine dihydrochloride, 5-(2-chloro-4, 5-difluoro -benzoylamino)-1Η-pyrazole-3-carboxylic acid (2-fluoro-pyridin-3-ylindenyl)-decylamine dihydrochloride, 5-(2-chloro-4, 5- Difluoro-benzoguanidino)-1Η-pyrazole-3-carboxylic acid (2-indolyl-pyridin-3-ylmethyl)-guanamine dihydrochloride, 5-(2-gas-4 , 5-difluoro-benzhydrylamino)-1Η-°biazole-3-carboxylic acid (biphenyl-3-ylindenyl)-decylamine, 5-(2-gas-4, 5-di Gas-benzoic acid amine)-1Η-αΛπ sit-3-acid ((lR,2S)-2-hydroxy-indan-1-yl)-decylamine, 5-(2-chloro-4 , 5-difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid ((lS,2R)-2-hydroxy-indan-1-yl)-decylamine, 5-(2 -Chloro-4, 5-difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid (6-phenyl-pyridin-3-ylindenyl)-nonylamine diphosphate Acid salt, 5-(2- gas-4, 5-difluoro-phenylhydrazino)-1Η-°biazole-3-carboxylic acid (6-fluorenyl-pyridin-3-ylindenyl)- Indole hydrochloride, 5-(2-chloro-4, 5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylic acid benzyl-indolyl-decylamine, 5-(2 - gas-4, 5-difluoro-phenylhydrazinoamino)-1Η-«biazole-3-carboxylic acid benzamide, 5-(2-chloro-4, 5-difluoro-phenylhydrazine Amino)-1Η-pyrazole-3-carboxy 417 (amendment) 318197 1322688 Patent Application No. 95,921,217 (July 1, 1998) Acidic decylamine, 5-(2-gas-4, 5 -difluoro-phenylhydrazinoamino)-ih-pyrazole-3-carboxylic acid methyl-phenyl-bristamine, 5-(2-chloro-4, 5-difluoro-benzhydrylamino )-ih-pyrazole-3 tricarboxylic acid decyl-1-yl)-nonylamine, 5-(2-chloro-4, 5-difluoro-phenylhydrazino)-ih-pyrazole- 3-carboxyk (4-ethoxylated-branched-1 -yl)-bristamine, 5-(2-chloro-4,5-difluoro-phenylhydrazino)-ih-pyrazole- 3-sulphonic acid U-methyl-piperidin-1-yl)-decylamine, 5-(2-chloro-4, 5-difluoro-phenylglycosylamino)-ih-indole-3- Acid (4-carboxy-piperidin-1-yl)-decylamine, 5-(2-chloro-4, 5-difluoro-benzhydrylamino)-ih- Benzene-3-decanoic acid phenethyl decylamine, 5-(2-gas-4, 5-difluoro-phenylhydrazinoyl H-pyrazole-3 carboxylic acid thiol &quot; 'this ethyl- Amine, 5_(2'' gas-4, difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid ethyl-benyl-bristamine, 5-(2-gas-4 , 5-difluoro-benzhydrylamino 1H_pyrazole_3_carboxylic acid (1,2,3,4-tetraisoindolin-2-yl)-nitramine, 5-(2-chloro -4,5-difluoro-phenylhydrazinoamino)-1H_pyrazole-3-carboxylic acid ((S)-a-oximeoxycarbonyl-benzyl)-decylamine, 5_(2-chloro-4 , 5-difluoro-phenylhydrazinoamino)_1H_pyrazole-3-carboxylic acid ((R)-a-oximeoxycarbonyl-benzyl)-decylamine, 5-(2-chloro-4, 5- Difluoro-benzoguanidino)1H_pyrazole_3_carboxyl 418 (amendment) 318197 1322688 Patent Application No. 95118217 - (July 10, 1998) Acid (1, 2, 3, 4) -tetrahydroquinolin-1-yl decylamine, - 5-(2-gas-4, 5-difluoro-crackanylamino)_1H_pyrazole-3-carboxyl' acid phenyl-propyl- Indamine, cloud-^-gas-'^-difluoro-phenylhydrazinyl^^pyrazole^-carboxylic acid butyl-phenyl-decylamine, 5-(2-gas-4, 5-di Fluorine-acnemethylamino) 4H-pyrazole_3_carboxylic acid pentyl-phenyl-indole , 5-(2-Gas-4, 5-difluoro-benzylidenylamino)_1H_pyrazole_3-carboxylate diphenyl decyl-decylamine, 5-(2-chloro-4, 5 -difluoro-benzoammonylamino) 4H-pyrazole-3-carboxylic acid (pyridin-2-ylmethyl)-decylamine hydrochloride, 5-(2- gas-4, 5-difluoro- Benzoylamino)_1H_pyrazole-3-carboxylic acid (0-bito-4-ylindenyl)-guanamine hydrochloride, 5-(2- gas-4, 5-difluoro-phenylhydrazine Mercaptoaminopyridyl-3-carboxylic acid ((R)-2-yl-l-phenyl-ethyl)-decylamine, φ 5_(2-chloro-4, 5-difluoro-phenylhydrazine Amino)-1H-pyrazole-3-carboxylic acid ((S)-2-hydroxy-1-phenyl-ethyl)-decylamine, 5-(2-chloro-4, 5-difluoro-benzene Mercaptoamino)-ih-pyrazole-3-carboxylic acid 4-didecylamino-benzylamine, 5-(2-chloro-4, 5-difluoro-phenylglycosylamino)- 1Η-0 ratio. Sodium -3-acid (furan-2-ylmethyl)-decylamine, 5-(2-chloro-4, 5-difluoro-benzhydrylamino)-1Η-πώσ sitting -3-acid (thiophen-2-ylmethyl)-nonylamine, 5-(2-chloro-4, 5-difluoro-anthracenylamino)-1Η-pyrazole-3-carboxy 419 (amendment) 318197 1322688 Patent Application No. 95118217. (July 10, 1998) Acid (2-methoxy-phenyl)-decylamine, • 5-(2-Gas-4, 5-difluoro-benzimidamide )H-pyrazole-3-carboxy' acid (2-methoxy-phenyl)-methyl-decylamine, 5-(2-gas-4, 5-difluoro-benzhydrylamino) Η σ-σ ratio 0 sitting -3- oxo acid 4-dimethylamino-benzylguanamine hydrochloride, 5-(2-gas-4, 5-difluoro-phenylhydrazino)-1Η- Σβ-azole-3-carboxylic acid 3-amino-tubular amine, 5-(2-chloro-4, 5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxy•acid 4 -amino-benzylamine, 5-(2-chloro-4, 5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid 2-indolyl-benzylamine, 5- (2-Chloro-4, 5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid 3-mercapto-benzylamine, 5-(2-chloro-4,5-di Fluoro-benzoquinone-based amine)_1Η-α than salivary 3-sulfonic acid 3-didecylamino-branched amine , $ 5-(2- gas-4,5-difluoro-benzoylamino)-1Η-〇Λ^-3 - tacrotic acid (2-methoxypyridin-3-ylindenyl)- Indoleamine, 5-(2-Gas-4,5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid 2-a-benzylamine, 5-(2-ethane-4, 5-Difluoro-benzoquinone-based amine)-1Η-° ratio 0 sitting-3-sodium acid 3-chloro-tuberamine, 5-(2- gas-4, 5-difluoro-phenylhydrazine Amino)-1Η-pyrazole-3-carboxylic acid 3_曱oxycarbonyl-benzylamine, 5-(2-chloro-4,5-difluoro-benzoquinoneamino)-1Η-η than saliva -3- Slow 420 (Revised) 318197 Patent No. 95118217 Applicant (July 1st, 1998) Acid 3_Slow Base-Filling Amine, 5-(2-chloro-4, 5-difluoro- Benzoquinone-based amino acid (6-trifluoromethyl-pyridyl-3-ylhydrazinyl)-nonylamine, 5-(2-chloro-4,5-difluoro-benzhydrylamino)-1Η -carbazole-3-o-acid (2-ethoxy-β-pyridin-3-ylindenyl)-decylamine, 5-(2-gas-4,5-difluoro-benzhydrylamino) -1Η-0-pyrazole-3-carboxylic acid (2-didecylamino-ethyl)-decylamine, 5-(2-chloro-4,5-difluoro-benzhydrylamino)-1Η -pyrazole-3-carboxylic acid ethyl-(2-dimethylamino-ethyl)-guanamine dihydrochloride, 5-(2-chloro-4, 5- Difluoro-phenylhydrazinoamino)_1Η-pyrazole-3-carboxylic acid cyclohexyl-(2-didecylamino-ethyl)-decylamine, 5-(2-chloro-4, 5-di Fluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid (4-methoxy-pyridin-2-ylindenyl)-decylamine, 5-(2-chloro-4, 5-di Fluoro-benzhydrylamino)1Η-η-pyrazole-3-carboxylic acid (2,6-dimethoxy-pyridin-3-ylmethyl)-decylamine, 5-(2-gas-4, 5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid 2-indoleoxycarbonylmethoxy-benzylamine, 5-(2-gas-4, 5-difluoro-benzene Mercaptoamino)-1Η-pyrazole-3-carboxylic acid 2-carboxydecyloxy-benzylamine, 5-(4,5-difluoro-2-indolyl-benzhydrylamino)- 1Η-pyrazole-3-carboxylic acid (6-decyloxy-pyridin-3-ylindenyl)-decylamine, 5-(2,4-dioxa-benzoylamino)-1Η-pyrazole 3-carboxylic acid (6-decyloxy~p-precipitate-3-3-indenyl)-bristamine, 5-(2-chloro-4, 5-difluoro-phenylhydrazino)-1Η- Pyrazole-3-carboxy 421 (amendment) 318197 Patent No. 95,921,217 (July 10, 1998) Acid (3, 5-dimethoxy-pyridine-4-ylindenyl)-decylamine, 5-(4,5-difluoro-2-indenyl-benzofuranylamino)- 1Η-σ ratio c 3-carboxylic acid (2,4-dimercapto-oxazol-5-ylmethyl)-decylamine, 5-(2,4-di-2-carbon-5-fluoro-acidylamino)-1Η -σΛσ sit-3-reaction acid (2,4--mercaptopurin-5-ylmethyl)-decylamine, 5-(2-gas-4, 5-difluorophenylhydrazino)-1Η -pyrazole-3-carboxylic acid (4-oximeoxycarbonyl-phenyl)-indenyl-nonylamine, 5-(2-gas-4,5-difluoro-benzoinyl)-1Η- Pyrazole-3-carboxylic acid (4-sulfophenyl)-mercapto-decylamine, {[5-(2-chloro-4, 5-difluoro-benzoguanidino)-1Η-pyrazole 3-carbonyl]-fluorenyl-amino}-benzoate sodium salt, 5-(2-chloro-4, 5-difluoro-benzylidenylamino)-lH-pyrazole-3-carboxylic acid Isopropyl-phenyl-bristamine, 5-(2- gas-4, 5-difluoro-phenylhydrazinoamino)-indole-pyrazole-3-carboxylic acid (ethoxymethyl-methyl) -phenyl-decylamine, 5-(2- gas-4, 5-difluoro-phenylhydrazino)-indole-pyrazole-3-acid (carboxy-methyl)-phenyl-decylamine , 5-(2-Ga-4-fluoro-benzhydrylamino)-1-indole-pyrazole-3-benzylcarbazide, 5-(2,4-dioxa-benzimidylamine ratio. Sit _3-Resinamide, 5-(2-Ga-5-fluoro-benzhydrylamino)pyrazole_3_carboxylic acid benzylamine, 5-(2-chloro-4, 5- Difluoro-phenylhydrazinoamino)_1Η_pyrazole-3-carboxycarboxylate 422 (amendment) 318197 1322688 Patent No. 95118217 Patent application macro (July 1998 1 bismuth decyl phenyl) -(2-chloro-4,5-difluoro-benzylideneamino)- 1 Η-° than sal-3-actic acid (1-mercapto-1-phenyl-ethyl)-decylamine, 5 -(2-chloro-4, 5-difluoro-benzhydrylamino acid [2-keto-2-(piperidin-1-yl)-1-ethyl]-phenyl-decylamine, 5 -(5-fluoro-2-methyl-benzhydrylamino)-1Η-β is more than 0-benzyl benzyl hydrazide, 5-(5-Gas-2-indolyl-benzoylamino)-111-° than 3-indole-3-carbobenzylamine, 5-(4-methoxy-2-indenyl-benzene Methionylamino)-1Η-pyrazole-3-carboxylic acid decylamine, 5-(4-gas-2-methyl-benzhydrylamino)-1Η-π ratio 0 sitting-3-rebel Benzyl benzamide, 5-(5-fluoro-2-methoxy-benzimidylamino)-lH-pyrazole-3-carboxylic acid benzamide 5-(5-Chloro-2-methoxy-benzylidenylamino)-ιη-pyrazole-3_bupropion benzylamine, 5-(2-chloro-4, 5-difluoro-benzoic acid Mercaptoamine)-ιη-pyrazole-3-tagamic acid (2-ethoxy-ethyl)-phenyl-decylamine, 5-(2-fluoro-5-mercapto-phenylhydrinylamino Η 吡 吡 吡 吡 吡 致 致 致 致 致 致 致 致 致 致 致 致 致 致 致 致 致 致 。 。 。 。 。 。 。 。 。 。 。 。 。 Sitting on a 3-glycolic acid decylamine, 5-(3-chloro-2,6-difluoro-benzhydrylamino)_ιΗ_pyrazole_3_carboxy 423 (amendment) 318197 1322688 patent 95118217 Application • (July 10, 1998) Benzoylamide, 5-(2-chloro-3-fluoro-adenylamino)-iH-pyrazole-3-carboxylic acid benzyl, styling amine, 5 -(2-Gas-4, 5-difluoro-phenylhydrazinoamino)-1 Η-pyrazole-3-carboxylic acid ethylaminomethylmercapto-yl-phenyl-decylamine, 5-( 2-chloro-4, 5-difluoro-benzylidenylamino)-lH-pyrazole-3-carboxylic acid isobutyl-phenyl-bristamine, 5-(2-chloro-4, 5-di Fluoro-benzhydrylamino)-indole-pyrazole-3-carboxy-acid (2-oxocarbonyl-ethyl)-phenyl-decylamine, 5-(2-chloro-4, 5-difluoro -phenylhydrazinoamino)-lH-pyrazole-3-carboxylic acid (3-ethoxylated-propyl)-phenyl-decylamine, 5-(2-chloro-4, 5-difluoro- Benzyl decylamino)-ιη-pyrazole-3-carboxylic acid (2-vvyl-ethyl)-phenyl-decylamine, 5-(2-chloro-4, difluoro-benzoguanamine Base)-ιη-pyrazole-3-carboxylic acid (3-sulfo-propyl)-phenyl-bristamine, φ 5-(2-hydroxy-4-oxime-benzoylamino)- Ιη-pyrazole-3-carboxylic acid decylamine, 5-(2-hydroxyl 5-yloxy-benzhydrylamino)-ιη-pyrazole-3-carboxylic acid decylamine, 5-(5-fluoro-2-hydroxy-benzhydrylamino)-ιη- Pyrazole-3-carboxylic acid benzamide, 5-(4-fluoro-2-dimethyl-benzoylamino) than 0--3-carboxylic acid decylamine, 5-(5-fluoro- 2-Trifluoromethyl-benzoylamino)-ih-pyrazole-3- 424 (amendment) 318197 1322688 • Patent Application No. 95182217 (July 10, 1998) ^ Carboxylic acid decylamine , - 5-(2-chloro-4, 5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxy• acid (2-methoxy-ethyl)-phenyl-bristamine ' 5-(2,5-Dimercapto-phenylhydrazino)-1Η-pyrazole-3-carboxylic acid benzamide, 5-(2-a-5-mercapto-benzimidamide Base)-1Η-pyrazole-3-carboxylic acid decylamine, specific precipitation _3_alkylamino group)-1Η_π ratio 0 sitting_3_retensive acid seasoning_amine, 5-(4_chlorine ratio bite Aminopyrazine _3_ retinoic acid amine, 5_(2,6-dichloro-pyridine-3-carbonylamino)-1Η-pyrazole-3-carboxylic acid benzamide, 5-(2-gas -4,5-difluoro-phenylhydrazinoamino)-1-indole-pyrazole-3-carboxylic acid butyl-(4-ethoxycarbonyl-phenyl)-decylamine, Lu 5-(2-chloro- 4,5-difluoro-benzamide amino group -1Η-σ ratio salivary-3_sodium butyl-(4-carboxy-phenyl)-decylamine, 5-(2-indolyl-pyridine-3-carbonylamino)-indole-pyrazole-3- Benzoyl carboxamide, 5-(2-Ga-6-methyl-0 ratio -3-amino-amino group)-1Η_ο比哇- 3-绔benzylammonium, 5-(3-chloro-°咬 缓 缓 缓 胺 -11 -11-11-11 嗤 嗤 -3- benzyl benzyl hydrazide, 5- (2-chloro-4, 5-difluoro-benzhydrylamino)-ιη- Pyrazole-3-carboxylate 425 (amendment) 318197 1322688 Patent Application No. 95118217 • ' (July 1st, 1998) Acid Butyl-(4-ethoxycarbonylmethyl-phenyl)-decylamine, 5-(2-Gas-4, 5-difluoro-phenylhydrazino)-1Η-pyrazole-3-trans-butyl butyl-(4-carboxymethyl-phenyl)-decylamine, 5 -(2-chloro-4,5-difluoro-phenylhydrazino)-1Η-pyrazole-3-hypoacid (4-methoxycarbonyl-phenyl)-(2-methoxy-ethyl - guanamine, 5_(2-a gas-4,5-di-gas-benzamide-based acid (4-reyl-phenyl)-(2-methoxy-ethyl)-bristamine, 5-(2-Gas-4, 5-difluoro-phenylhydrazinylamino)-1Η-pyrazole-3-slow# acid (6-decyloxy-pyridin-3-ylindenyl)-decylamine Dihydrochloride, 5-(2-mercapto-4, 5-difluoro-phenylhydrazino) -1Η-pyrazole-3-carboxylic acid (6-decyloxypyridinyl-3-ylindenyl)-decylamine dihydrochloride, 5-(2-gas-4,5-difluoro-phenylhydrazine Stearic amine)-1Η-π than saliva-3-retinic acid (thiazol-4-yl-indenyl)-guanamine dihydrochloride, 5-(2-rat-4, 5-difluoro-benzene Mercaptoamine group - lH ~ 〇 ratio. Sodium-3-reaction 4-[2-(morphin-4-yl)-ethylaminomethylmercapto]-peptidylamine salt, 5-(2-chloro-4, 5-di Fluoro-phenyl-mercaptoamino)-lH-pyrazole-3-identified acid 4-(wherein-4-ylaminoindolyl)-benzylamine dihydrochloride, [4-({[5- (2-Ga-4,5-difluoro-benzoindolyl)-111_pyt»»-3-ylamino]-amino}-indenyl)-cracked amino]-acetic acid Salt, 3-[4-({ [5-(2-chloro-4, 5-difluoro-benzhydrylamino)_1Η_pyrazole_3_carbonyl]-amino}-indenyl)-phenylhydrazine醯Amino]-propionic acid sodium salt, [5-(2-chloro-4, 5-difluoro-phenylhydrazinyl)-ιη-pyrazole_3_ succinic acid (3,5 -methyl group Iso-ββ-4-ylmethyl)-bristamine hydrochloride, (amendment) 318197 426 1322688 Patent Application No. 95182217 (July 10, 1998) '[5-(2-chloro-4) , 5-difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid (1,3,5-trimethyl-1H-pyrazol-4-ylindenyl)-nonylamine diphosphate Acid salt, 5-(2-chloro-4, 5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid (3, 5-dimercapto-isoxazole-4-yl Mercapto)-nonylamine mesylate, 5-(2-chloro-4, 5-difluoro-benzoylamino)-1Η-° ratio3-(2-(morpholin-4-yl)-ethylaminomethylmercapto]-benzylguanamine dihydrochloride, 5-(2-chloro-4, 5-difluoro) -benzylideneamino)-1Η-pyrazole-3-carboxylic acid 3-(morpholin-4-ylaminocarbamoyl)-benzylguanamine dihydrochloride, 5-(2-gas-4 , 5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid {2-[2-(morpholin-4-yl)-ethylaminomethylindenyl]-pyridine-4 -yl hydrazide}-decylamine trihydrochloride, 5-(2- gas-4,5-difluoro-phenylhydrazinoamino)-1 Η-pyrazole-3-carboxylic acid [2_( 4-aminoaminomethyl keto-4-ylindenyl]-nitramine trihydrochloride, 5-(2-chloro-4,5-difluoro-benzoquinoneamino)_1H-n than saliva -3-Resin (6-decyloxy-pyridin-3-ylindenyl)-nonylamine mesylate, 5-(2-chloro-4, 5-difluoro-benzoinylamino)_1Η -° ratio. Oxy-3-acid (6-decyloxy-pyridin-3-ylindenyl)-decylamine hemisulfate, 5-(2-gas-4, 5-difluoro-benzhydryl) Amino)-1Η-pyrazole-3-carboxylic acid (3,5-dimethoxy-pyridin-4-ylindenyl)-decylamine dihydrochloride, 5-(2-chloro-4, 5- Difluoro-benzoinylamino)_1Η-° than salivary-3-remediation (4-aminomercapto-pyridin-2-ylindenyl)-decylamine trihydrochloride , 427 (amendment) 318197 丄丄ozx / (98 years pit application date July 10) 5_(2 - gas-4, 5-difluoro-benzoylamino)-1Η-σ ratio 0 sit-3~slow acid (6-chlorobite-3-ylindenyl)-amine amine acid salt, 5_(2-gas-4, 5-difluoro-abidomethylamino)-1Η -pyrazole-3~nonanoic acid (6-chloro-pyridin-3-ylindenyl)-nonylamine dimethanesulfonate, 5-(2-gas-4, 5-difluoro-anthracenylamino -1Η-pyrazole-3-# acid (2,4-dimercapto-pyridin-3-ylmethyl)-decylamine hydrochloride, 5-(2- gas-4, 5-difluoro-benzene Mercaptoamino)-1Η-pyrazole-3-acid (〇 咬-3-ylmethyl)-guanamine hydrochloride, 5-(2-chloro-4, 5-difluoro-phenylhydrazine) Stearylamino)-1Η-° than salino-3-butyric acid (6-decyloxy-D ratio thiol-yl)-propyl-bristamine dihydrochloride, 5-(2-gas-4, 5-difluoro-stupyl-based amino acid [6-•(piperidin-1-yl)_° ratio -3-ylindenyl]]-guanamine dihydrochloride, 5_(2- gas- 4,5_digas-benzoquinoneamino)-111-indole wow-3-some_acid [6-(morphin-4-yl)-0-bito-3-ylindenyl]]- Indoleamine dihydrochloride, 5-(2- gas-4,5-diqi-benzoquinoneamino)-111-° ratio -3 - Oreic acid (3, 5-dichloro-pyridine-4-ylmethyl)-guanamine hydrochloride, 5_(2-chloro-4,5-di-phenyl-phenylamino)-1Η -0 than π sit-3-acid (6-didecylaminopyridin-3-ylmethyl)-guanamine dihydrochloride, 5-(2- gas-4, 5-difluoro-benzene Brewing arylamino)-1Η-° than salino-3-acid (6-diamidino-pyridin-3-ylindenyl)-propyl decylamine dihydrochloride, 5-(2-chloro -4,5-difluoro-phenylhydrazinyl)-ΐΗ_ο than sal-3-hydroxy acid (6-diethylaminopyridin-3-yl)-decylamine dihydrochloride, 5 -(2-Chloro-4,5-difluoro-crackanylamino)-ΐΗ-α ratio.坐-3-protection (amendment) 318197 428 1322688 'patent application No. 95182217 (July 10, 1998) acid (6-chloro-2-didecylamino-pyridin-3-ylindenyl)- Indoleamine dihydrochloride, • 5-(2-chloro-4, 5-difluoro-benzhydrylamino)-1Η-η-pyrazole-3-carboxylic acid (4-[1,2,3] Thiazol-4-yl-benzyl)-indoleamine hydrochloride, 5-(2-chloro-4,5-difluoro-benzylidenylamino)-1Η-pyrazole-3-carboxylic acid ( 4-mercapto-thiazol-5-ylindenyl)-nonylamine hydrochloride, 5-(2-chloro-4,5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylate Acid (2,4-dimercapto-thiazol-5-ylmethyl)-indolyl hydrochloride, ginseng 5-(2-chloro-4, 5-difluoro-benzylidenylamino)-1Η- Pyrazole-3-carboxylic acid [6-(4-hydroxy-piperidin-1-yl)-pyridin-3-ylmethyl]-nonylamine dihydrochloride, 5-(2-chloro-4, 5- Difluoro-benzoguanidino)-1Η-pyrazole-3-carboxylic acid 5-mercapto-pyridin-2-ylguanamine dihydrochloride, 5-(2-chloro-4, 5-di Fluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid quinolin-5-ylguanamine dihydrochloride, φ 5-(2-gas-4, 5-difluoro-phenylhydrazine Amino-based)-1Η-pyrazole-3-carboxylic acid quinoline-8-ylguanamine dihydrochloride, 5-(2- -4, 5-difluoro-phenylhydrazinoaminopyrazole-3-carboxylic acid isoquinolin-5-ylguanamine dihydrochloride, 5-(2-chloro-4,5-difluoro-benzene曱 基 胺 ) Η Η 。 。 。 。 竣 竣 竣 竣 竣 竣 竣 竣 竣 竣 竣 竣 竣 竣 竣 6 [6-(4-methylpipedino-1-yl)-pyridin-3-ylindolyl]-nonylamine dihydrochloride, 5-( 2- gas-4,5-difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid [6-(4-dimethylamino-trans--1-yl)-α ratio bite _3-基曱基]-醮429 (Revised) 318197 1322688 » Patent Application No. 95112217_(July 10, 1998) Amine Dihydrochloride, • 5-(2-Chloro-4, 5- Difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxy-acid [6-(pyrrolidinyl-bu)-pyridin-3-ylindenyl]-nonylamine dihydrochloride, 5- (2-Chloro-4,5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylic acid (pyridin-2-ylindenyl)-decylamine dihydrochloride, 5-( 2- gas-4,5-difluoro-benzhydrylamino)-1Η-indazole-3-carboxylic acid [6-(thiomorpholin-4-yl)-pyridin-3-ylmethyl]- Indoleamine dihydrochloride, 5-(2- gas-4, 5-difluoro-phenylhydrazino)-1Η-indazole-3-carboxyluic acid [6-(1, bis-dione- 1 and 6-thiomorpholin-4-yl)-pyridin-3-ylmethyl]-nonylamine dihydrochloride, 5-(2- Gas-4, 5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid aminomethylmercaptomethyl-decylamine, 5-(2,4-dichloro-5-fluoro -benzylideneamino)-1Η-pyrazole-3-carboxylic acid (4-aminomethylindenyl-phenyl)-indenyl-decylamine, 5-(2,4-dichloro-5-fluoro -benzoylamino)-1 Η-pyrazole-3-carboxy φ acid methyl-(4-hydrazinoaminoindenyl-phenyl)-decylamine, 5-(2,4-dichloro- 5-fluoro-adenylamino)1H-pyrazole-3-carboxylic acid (4-didecylaminomethylindenyl-phenyl)-methyl-decylamine, 5-(2-chloro-4 , 5-difluoro-benzoylaminopyrazole-3-carboxylic acid (4-oxasulfonylaminocarbonyl-phenyl)-mercapto-decylamine, 5-(2-chloro-4, 5 -difluoro-adolylamino)_ih-pyrazole-3-carboxylic acid (4-曱醯 mercaptoaminocarbonyl ''phenyl)-indolyl-decylamine sodium salt, 5-(2-gas -4,5-difluoro-azinomethylamino)-ih-pyrazole-3-carboxylic acid (4-cyano-phenyl)-indenyl-bristamine, 430 (amendment) 318197 1322688 No. 95118217 Patent Application (July 10, 1998) 5-(2-Chloro-4, 5-difluoro-benzoamitoylamino)-1Η-pyrazole-3-carboxylic acid methyl-[4-(4Η -[1,2,4]triazol-3-yl)-phenyl]-nonylamine hydrochloride. Salt, 5-(4-azido-2-chloro-5-fluoro-benzimidamide)-1Η-pyrazole-3-carboxylic acid (4-cyano-phenyl)-indolyl-decylamine, 5- (4-azido-2-chloro-5-fluoro-benzimidamide)-1Η-pyrazole-3-carboxylic acid fluorenyl-[4-(1Η-tetrazol-5-yl)-phenyl] - indoleamine, 5-(2-chloro-4,5-difluoro-benzoinylamino)-111-° than hydrazine-3-lower® acid-[4-(N-hydroxyaminoimine) Methyl)-phenyl]-mercapto-nonylamine, 5-(2-chloro-4,5-difluoro-benzoindolyl)-1Η-pyrazole-3-carboxylic acid methyl-[4 -(5-keto-2,5-dihydro-[1,2,4]oxadiazol-3-yl)-phenyl]-nonylamine, 5-(2-chloro-4, 5-difluoro -benzylideneamino)-1Η-pyrazole-3-carboxylic acid {4-[(2,2-dimercapto-propenyloxy)-indolyloxycarbonyl]-phenyl}-indenyl-anthracene Amine, φ 5-(2-chloro-4,5-difluoro-phenylhydrazinoamino)-lH-pyrazole-3-carboxylic acid 4-[N-methoxy-thiocarbonyloxy]-amine Iminoimine]-methylmonodecylamine, 5-(2-chloro-4,5-difluoro-benzoindolyl)-ih-pyrazole-3-hydantosyl-[4- (5-thioketo-4,5-dihydro-[1,2,4]oxadiazol-3-yl)-phenyl]-decylamine, 5-(2-gas-4,-disorder-benzene Brewing amide-based 3-oxo-acid methyl-[4-(5-keto-4, 5-di -[1,2,4]thiadiazol-3-yl)-phenyl]-decylamine, 431 (amendment) 318197 1322688 Patent Application No. 95118217 (July 10, 1998) 5-(2- Chloro-4, 5-difluoro-phenylhydrazinoamino)_1H-pyrazole_3_carboxylic acid {4-[1-(cyclohexyloxy-carbonyloxy)-ethoxycarbonyl]-phenyl} _Methyl-nonylamine, 5-(2-chloro-4, 5-difluoro-benzylidenylamino)_1H_pyrazole-3-carboxylic acid (4-ethoxycarbonyl-hydrazin-2-yl) -ethyl-decylamine, 5-(2-chloro-4, 5-difluoro-benzoamitoylamino)_1H-pyrazole-3-carboxylic acid 2-indolesulfonylamino-benzamide 5-(2-chloro-4,5-difluoro-phenylhydrazinyl)_;[η-pyrazole_3-carboxylate 2-ethylammonium-tuberamine, 5-(2- Chloro-4, 5-difluoro-crackanylamino)_1 ugly-〇 〇 〇-3-(2-decylamino-methyleneamino)-benzylamine hydrochloride , 5-(2-Gas-4, 5-difluoro-phenylhydrazinylamino)-sial-3-carboxylic acid 3-(dimethylamino-ylideneamino)-benzylamine hydrochloride , 5-(2-Gas-4, 5-difluoro-phenylhydrazineacetic acid group than saliva-3-carboxylic acid 4-(didecylamino-fluorenylamino)-benzylguanamine hydrochloride , φ 5-(2-gas-4,5-difluoro-adolylamino group One to π sit a 3-reposted 2-[1-(dimethylamino)ethylamino]-benzylamine dihydrochloride, 5-(2-chloro-4, 5-difluoro- Benzoylaminopyrazole-3-dicarboxylic acid 3-[1_(dimethylamino)ethylidene]benzylguanamine dihydrochloride, 5-(2-chloro-4, 5-di Fluoro-benzhydrylamino)-ih-pyrazole-1-3-Sx 4-[1-(didecylamino)ethylidene]-benzylamine dihydrochloride, 5-(2 - gas-4, 5-difluoro-benzhydrylaminopyrazole-3-dicarboxylic acid 2-(diethylamino-methyleneamino)-benzylamine dihydrochloride, 5-( 2-Chloro-4, 5-difluoro-benzhydrylamino)-ih-carbazole _3 竣 432 (amendment) 318197 1322688 Patent Application No. 95118217 (July 1st, 1998) Acid 3_(-ethyl-glycol-hydrazinylamino)-tuberamine dihydrochloride, 5-(2-chloro-4,5-difluoro-crackanylaminopyrazole-3-carboxylate 4-(ethylethylamino-methyleneamino)-tuberamine dihydrochloride, 5-(2-chloro-4, 5-difluoro-phenylhydrazino)-1H-pyrazole 3-carboxylic acid 2-iminoethylamino-barred amine dihydrochloride, 5-(2-chloro-4,5-difluoro-benzhydrylamino)_1H-pyrazolic acid 3 - Iminoethylamino-section Amine dihydrochloride, 5-(2-gas-4, 5-difluoro-benzhydrylamino) 4H-pyrazole-3-carboxypyrrolic acid 4-imine ethylaminosyl»» Dihydrochloride, 5-(2-Gas-4, 5-difluoro-phenylhydrazinylaminobu- 1H-n-pyrazole_3_decanoic acid 4-cyano-tuberamine, 5-(2-gas- 4, 5-difluoro-phenylhydrazinoamino)_1H-pyrazole-3-carboxylate 3-[(2-fluoro-imidomethyl)-amino]-thretonamine hydroiodide, 5-(2-Gas-4, 5-difluoro-phenylhydrazino)1H-pyrazole-3-carboxylic acid 4-[(2-fluoro-iminophenylphenyl)-aminobenzylamide Hydroiodide, • 5-(2-Gas-4, 5-difluoro-benzhydrylamino)- 1H-pyrazole-3-carboxylic acid 3-(3,3-dimethyl-ureido Monobenzylamine, 5-(2-aryl-4, 5-difluoro-benzoamitoylamino)_1H_pyrazole-3-carboxylic acid 4-(3,3-dimethyl-ureido) Benzylamine, 5-(2-chloro-4, 5-difluoro-benzhydrylamino) 1H_pyrazole-3-carboxylic acid 2-(toluene-4-sulfonylamino)-benzyl hydrazine Amine, 5 (2-gas 4, 5-fluoro-benzhydrylamino)-ΐΗ-σ ratio, sal-3-resine 2-amino-6-fluoro-tuberamine hydrochloride, 5-( 2-Gas-4, 5-difluoro-phenylhydrazinoamino 1 Η-pyrazole _3 Carboxy 433 (Revised) 318197 Acid 2-Amino- 4, 5-II &amp; (July 1998 ίο日), a 虱~benzylamine hydrochloride, 5-(2-gas-4 5 舻r bird ~, '~Fluorine-stupylaminolamine )-1Η-pyrazole-3-carboxyindole (indole-1-yl)~nonylamine, 5-(2-gas-4,5----------------------------- -pyrazole-3-carboxylic acid (anthraceti-2-yl)-decylamine, 5-(2-gas-4 5__d, ττ, a murine- alumidylamino)-1Η-pyrazole -3_carboxylic acid (4Η-quinazoline_3_volume)~bristamine, 5_c ^ . wind ~ '5~difluoro-phenylhydrazinoamino)-1Η-pyrazole-3_carboxy I 4Η圭坐Porphyrin-3__yl)~decylamine dihydrochloride, 5-(2-^-4 c: _^'difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxyindole (7F 4H quinazolinyl)-nonylamine dihydrochloride, 5 (2-one-4'-5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxyl (6F-4H-) Quinazoline _3_yl)-decylamine hydrochloride, 5-(2~chloro-4,5-difluoro-benzhydrylamino)-1H_pyrazole_3_carboxylic acid (2_B Oxy-2_mercapto-1,4-dihydro-2H-quinazolin-3-yl)-decylamine, 5-(2'-gas-4, 5-difluoro-benzhydrylamino) -ih-pyrazole-3-carboxylic acid (2-cyano -pyridine-4-ylhydrazinylamine, 5_(2~gas-4,5-difluoro-phenylhydrazinoamino)-ih-pyrazole-3-carboxylic acid [2-(N-hydroxyamino group) Iminoindolyl)-pyridyl-4-ylmethyl]monodecylamine, 5-(2- gas-4, 5-dioxa-benzoquinoneamino)-1Η-η than saliva-3-slow Ssl [2 (5-_yl-4, 5-dihydro-[1,2,4]°oxadiazol-3-yl)-π ratio -4-ylindenyl]-bristamine, 4-hydrazine 5-(4,5-Difluoro-2-indolyl-phenylhydrazino)-ih-pyridinium 434 (amendment) 318197 1322688 Patent Application No. 95118217 (July 1st, 1998) -3 -monoyl]-mercapto-amino}-succinic acid sodium salt, 5-(4,5-difluoro-2-indolyl-benzoylamino)-1Η-pyrazole_3_carboxylic acid -[4-(1Η-tetrazol-5-yl)-phenyl]-nonylamine, 5-(2,4-dichloro-benzylidinium)-1Η-pyrazole-3-carboxylic acid ( Pyridin-3-ylmethyl)-decylamine, 5-(2,4-dichloro-5-fluoro-benzimidamide)-1H-0 is 0 ≤3_slow acid (pyridin-3-yl) Mercapto)-nonylamine, 5-(2,6-dichloro-5-fluoropyridin-3-ylamino)_1Η-α ratio 0-chun-3-carboxylic acid (pyridin-3-ylmethyl) - indoleamine, 5-[(3-chloro-benzo-[&gt;]thiophene-2-carbonyl)-amino]-111-°bazole-3- Acid (pyridin-3-ylindenyl)-decylamine, 5-[(3- gas-thiophene-2-carbonyl)-amino]-111-pyrazole-3-carboxylic acid (° ratio bite 3-yl) Indenylamine, decylamine, 5-phenylhydrazinoamino-1 Η-pyrazole-3-carboxylic acid (pyridin-3-ylindenyl)-nonylamine, _ 5-phenethylaminol-1Η Pyrazole-3-carboxylic acid (pyridin-3-ylindenyl)-nonylamine, 5-(2-methyl-4,5-di-benzoylamino)_1Η-σ ratio 0 sitting - 3_ Carboxylic acid (pyridin-3-ylindenyl)-nonylamine dihydrochloride, 5-(2-amino-4, 5-difluoro-benzylamino)-1Η-pyrazole-3-carboxylic acid (pyridin-3-ylmethyl)-decylamine, 5-(4,5-difluoro-2-indolesulfonylamino-phenylguanidino)-1Η-pyridinium-3-oxo acid (吼Bite_3-ylindenyl)-bristamine, 5-(2-acetamido-4,5-difluoro-benzoguanidino)-1Η-pyrazole 435 (amendment) 318197 1322688 No. 95118217 Patent application (July 1, 2008 〇°曰; - 3-acidic (η ratio bit-3-ylmethyl)-decylamine, 5-[(3, 4, 5-trichloro-thiophene-2) -carbonyl)-amino]-1Η-mouth ratio η--3-acid ratio bit-3-ylmethyl)-bristamine, 5-(4,5-difluoro-2-methyl-benzoquinone Amino)-indole-pyrazole-3-carboxylic acid (2-cyano) Bipyridin-4-ylmethyl)-decylamine, 5~(4,5-difluoro-2-indolyl-benzhydrylamino)-lH-pyrazole-3-decanoic acid [2-(1Η - tetrazol-5-yl)-pyridin-4-ylmethyl]-decylamine, and 1 Η-» ratio. Sit _3,5-di-rebel acid 3-benzyl stearamine 5-[(2,4-di-phenyl)-bristamine]. 2] - * - a pyrazole compound represented by the formula (III) or a pharmaceutically acceptable salt thereof, N-NH 0 CI Substituted: [Α group] A1 · Mercury, A2. Cw alkoxy, A3. -N(R41)(r41.), 436 (amendment) 318197 Patent No. 95,921,217 patent, .. . ( 98 R and R are the same or different from each other and represent a hydrogen atom or an alkyl group; or R41 and a 5- or 6-membered monocyclic heterocyclic ring which may form a saturated state together with an adjacent nitrogen atom, on July 1, 2017. A4. aryl, A5. heteroaryl, A6. -C0-N(R411)(R411'), wherein R and R are the same or different from each other and represent a hydrogen atom or a Ch alkyl group; or Adjacent nitrogen atoms together form a saturated 5- or 6-membered monocyclic heterocycle, A7.carboxyl, and A8.C!-6 alkoxycarbonyl, (3) C2-6 dilute; (4) C2-6 (5) C3-8 ring yard base; spring (6) C3-8 ring yard base Cl-6 burnt base; or (7) aryl group; and R5 means (1) C丨-6 alkyl group Substituted by one or more substituents selected from Group B, such as τ D ei: [Group B] B1. Hydroxy, B2. Ch alkoxy, (Revised) 318197 437 J322688 B3. -N(R51) (R51' where R and F1 are the same as each other &lt; phase one r···, β d51. ^ is different and does not represent hydrogen The sub or C"6^, e R may form a saturated 5 or 6 membered monocyclic heterocyclic ring together with an adjacent nitrogen atom, and B4. -CO-N(R511) (R511, wherein R and R are the same as each other Or a different one and the same: and R can be combined with an adjacent nitrogen atom to form a 5- or 6-membered monocyclic heterocyclic ring, (2) a C3-8 cycloalkyl group; It can be condensed with a base group, a ruthenium group or a "# 玫 U U -6 -6 U 或 或 或 或 或 或 或 或 或 或 或 或 或 或 或 或 或 或 或 或 或 或 或 或 或 或 或 或 或 或 或 或 或 或Wherein the C&quot;cycloalkyl group of the cycloalkyl group may be substituted by a thioloxycarbonyl group, or may be condensed with a pyridine ring, and the 5 (4) saturated 5 or 6 membered monocyclic (10) ring group ^Substituted from one or more substituents of group c below: [C group] C1. 匕-6 alkyl, C2. bromo, C3. Ci-6, aryl, C4. carboxy, C5. Ci-6 alkoxycarbonyl, and (amendment) 318197 438 k Patent No. 95118217. (July 1st, 1998, C6·-C0-(Alk)n-C00R52, VIII, R is hydrogen An atom or a Ci-6 alkyl group; A1 k is a C1-4 stretching group; and n is an integer of 0 or 1 to 3, and (5) an aryl group Substituted by one or more substituents selected from the group consisting of: Group D] D1. Merid, D2. C!-6 alkoxy, D3. Cyano, D4.Ch alkyl, wherein the Ch alkane The group may be substituted with one or more substituents selected from the group consisting of a hydroxyl group, a carboxyl group and a Cl_6 alkoxy group, D5. _N(R53)(R53,), wherein R53 and R33 are the same or each other And R represents a hydrogen atom, a Cl-6 alkyl group or a Cl-6 group-based fluorenyl group, φ D6. -C0-N(R53,)(R531'), wherein R and r531 are the same or different from each other and represent hydrogen. Atom, Cl-6 leumino or Cl-6, a fluorenyl group, D7. -C00R54, wherein R is a hydrogen atom, a Ch alkyl group, a Cm alkylcarbonyloxy oxime 6 leukoyl group or a C3-8 cycloalkoxy group. a benzyloxy Ci_6 alkyl group, D8. -C(NH(0H))=N-R55, wherein Raa is a hydrogen atom or a C1-6 alkyl group, D9. A saturated 5- or 6-membered monocyclic system Heterocyclic group, (amendment) 318197 439 1322688 Patent Application No. 95118217 (July 10, 1998 and D10·5 or 6 members of a monocyclic heterocyclic aromatic group which may be substituted with a keto or thioketo group, ( 6) 5 or 6 members of the monocyclic heteroaromatic group or 5 or 6 members formed by the agglomerated ring a heteroaryl group, wherein the 5- or 6-membered heteroaryl group is substituted with one or more substituents selected from the group consisting of a buffer group and a Cm alkoxycarbonyl group; 1 (7) a C7-h aryl group; Wherein the alkyl portion of the C7_14 aralkyl group may be substituted with one or more substituents selected from Group E below, and the aryl moiety may be substituted with one or more substituents selected from Group F below: Group E] El. Cw alkyl which may be substituted by a hydroxy group, E2. cyano group, E3. thiol group, _E4. Ch alkoxycarbonyl group, and E5. phenyl group, [F group] F1 · Ci-6 alkyl group , F2. halogen atom, F3. cyano group, F4. thiol group, F5. Cm fluorene group which can be selected from the group consisting of carboxyl group and 匕6 alkoxycarbonyl group (amendment) 318197 440 1322688 No. 95918217 On July 1, 1998, one or more substituents of the group formed were replaced by 'F6. From Cm alkyl, F7. carboxyl, F8. Ci-6 alkoxycarbonyl, F9. -CO-N (R56a) (R56a,): wherein R56a and R56a are the same or different from each other and represent a hydrogen atom, a saturated 5- or 6-membered monocyclic heterocyclic group having at least one nitrogen atom, or a Ci-e alkyl group. It can be selected from One or more substitutions of the lower group f are substituted: [f group] f 1. amine group, f2. mono Cl-6 alkylamino group, f3 · a Cl-6 alkylamino group, f 4. a group of 5-hydroxy or 6-membered monocyclic heterocyclic groups having at least one nitrogen atom, 'F10. -N(R56b)(R56b), wherein R and R36b They are the same or different from each other and represent a hydrogen atom, and the Ch group may be substituted with an imine group which may be identical or different through one or more of the group consisting of an imine group and a tooth atom. Substituents substituted by 'aryl gamma', which can be substituted by (4)-dosyl group, Cl_6 is burned (amendment) 318197 441, patent application No. 95,921,217 «w (July 10, 1998); Tu Yin, Kei, Yanji, Amino fluorenyl, mono C 丨-6 alkylaminocarbamyl or di-Ci-e alkylaminocarboxamidine, Fll. -N=CR57(-N(R58)(R58 )), wherein R37 Is a hydrogen atom or a Cm alkyl group, and R58· are the same or different from each other and represent a hydrogen atom or a Ci ealkyl group, a F12·5 member or a 6 membered monocyclic heteroaryl group, and a F13. fluorenylene dioxy group. Or ethylene dioxy, or (8) by 5 or 6 members a cyclo-heteroaryl-substituted Ci 6 danyl group or a Ch alkyl group substituted with a heteroaryl group condensed with 5 or 6 members of the benzene ring; wherein the heteroaromatic group may be selected from one of the following Group G or Substituted by a plurality of substituents: [Group G] Gl. Ch alkyl which may be substituted by one or more substituents selected from the group consisting of: g group] gl. halogen atom, g2. amine group, g3· Mono Cl-6 alkylamino group, ^4. - Cl-6-homo-amine group, g5. Cm alkoxycarbonylamino group, and 442 (amendment) 318197 1322688 Patent No. 95118217 (98 years 7) 10th) g6.hydroxyimino, 'G2. tooth atom, · G3. Ch alkoxy which may be substituted by a halogen atom, G4. aryloxy, G5. cyano, G6. -N(R59a)( R59a), wherein R and R9a are the same or different from each other and represent a hydrogen atom or an alkyl group, or ... may form a saturated 5- or 6-membered monocyclic heterocyclic ring together with an adjacent nitrogen atom, and the saturated heterocyclic ring may be Substituted by one or more identical or different substituents selected from the group consisting of a hydroxyl group, an amine group, a mono Cm alkylamino group and a diCi-alkylamine group, G7.-C0-N (R59b )(R59b ), Wherein R and R are the same or different from each other and represent a hydrogen atom, a saturated 5-membered or 6-membered monocyclic heterocyclic group, or a Ci6 alkyl group which may be substituted by a hetero-based group _ G8. aryl, and G9' A 5- or 6-membered monocyclic aryl group which may be substituted with a thiol or thiocopper group, or .../and R3 may form a saturated 5 member or 6 = ring heterocyclic ring together with an adjacent nitrogen atom. The heterocyclic material may have a double bond, the saturated monocyclic ring may be condensed with the benzene ring to form a condensed ring, and the saturated heterocyclic ring which may be condensed with the benzene ring to form a condensed ring may be selected from the group consisting of (tetra) and Cl-channels. (Amendment) 318197 443 1322688 Patent Application No. 95,192,217 (Substituted on July 1, 1998, a group of alkoxy, carboxy, and Cm alkoxycarbonyl groups, substituted by one or more substituents. 22. The pyrazole compound or a pharmaceutically acceptable salt thereof according to claim 21, wherein R4 is a group selected from the group consisting of: (1) a hydrogen atom; (2) a Ch alkyl group which is selectable Substituted from one or more of the substituents of Group A below: &amp; [A, group] A' 1. a radical, A' 2. Ch alkoxy, A, 3. -N(R41)(R41,), which &quot;41 and R41 are identical or different from each other and represent a hydrogen atom or a C 4 thiol group; or R41 and R 4 丨 'cocoa ρ η 知 — — — — — — % % % % % % % % % % % % % % % % % % % % % % 相邻 相邻 相邻 相邻 相邻 相邻 相邻 相邻 相邻 相邻 相邻 相邻 Mussel or 6-membered monocyclic heteroaromatic group A5 6. -C0-N(R411)(r4h· where R and R4n are the same C丨-4 yard base; or Rchuan and can, the door is different 5 or 6 members of the non-atom atom or a mixture of 6 or 6 members of the same material, the same as the same phase (4), forming a full A 7. slow base, and A 8. Ci-4 alkoxy group, (3) C2-6 alkenyl group, (4) C2-6 Fast Base, (amendment) 318197 ^^688 ^^688 Patent Application No. 95118217 (July 1st, 1998), (5) C3-8 cycloalkyl; and (6) 〇 3-8 院院基基-4-4. 23. If the application is in the scope of claim 21, the D compound or its pharmaceutically acceptable salt, wherein R5 is a Cl_6 alkyl group. Item 21. The bisazole compound or a pharmaceutically acceptable salt thereof, wherein R5 is a C3-8 cycloalkyl group which may be selected from the group consisting of a hydroxyl group, a carboxyl group and a Ci-e alkoxycarbonyl group. Substituted by one or more substituents. The pyrazole compound of claim 21, or a pharmaceutically acceptable salt thereof, wherein R5 is a C3-8 cycloalkylCh alkyl group. a π-salt compound or a pharmaceutically acceptable salt thereof, in the range 21 Wherein R5 is a saturated 5 or 6 membered monocyclic heterocyclic group, which is substituted with two 'multiple substituents selected from the group consisting of thiol and Α1 k) Is a hydrogen atom or G 6 , Alk is a C 4 -alkyl group and η is G or an integer of 1 to 3. 'Study IS: 2nd item 21...the compound or its medicinal connection, wherein R is It may be substituted by a plurality of substituents selected from, for example, TD: ', or 'D, group D', i. Cw alkyl which may be substituted by a carboxyl group, D 2. -c〇-n(R53) (r53.), wherein the same or different and 〇4 alkyl or Ci*alkylsulfonyl; 虱 atom, (修 JL本) 318197 445 丄乂 2688 Patent No. 95918217 (July 98) 10)), D.3. -C00R54, wherein R34 is a hydrogen atom, a Cl_4 alkyl group, a Cl_4 alkylcarbonyloxy group C4 alkyl group or a C3-8 cycloalkyloxycarbonyloxy group C-4, and D' 4. A 5- or 6-membered monocyclic heteroaromatic group which may be substituted by a keto group or a thioketo group. 28. A pi-quinone compound according to claim 21 of the scope of the patent application or a pharmaceutically acceptable salt thereof, wherein Rs is an Ou aralkyl group, and the aryl group of the aralkyl group It may be substituted by one or more substituents selected from the group F' below: [F 'group] F' 1. C!-6 alkyl, F' 2. halogen atom, F' 3. cyano, F' 4. Jingji, F'5. Ch alkoxy which may be substituted by one or more substituents selected from the group consisting of a carboxy group and a Cie alkoxycarbonyl group, F' 6. a halogen Cm alkyl group, a F' 7. carboxyl group, F' 8 · Cm alkoxycarbonyl, F'9 · -C0-N(R56a)(R56a ), ' wherein R36a and rw are phase (5) or different from each other and represent a gas atom, having at least one nitrogen atom saturated 5 or 6 members of the single ring system of heterocyclic soil, or. -6 alkyl which may be substituted by one or more of the following f' groups (amendment) 318197 446 No. 95118217 _ 谙 Hong (July 1st, 1998) base replaced: [Γ group] Γ 1. Amine, Γ 2. Mono-Ch alkylamino, Γ 3. Di- -6-alkyl, f' 4. Carboxyl, Γ 5. Ch alkoxycarbonyl, Φ f ' 6 · thiol, and f '7. A 5- or 6-membered monocyclic heterocyclic group having at least one nitrogen atom, F, 10. -N(R56b)(R56b,), wherein R5ba' are the same or different from each other and represent a hydrogen atom a Ci-e alkyl group which may be substituted with an imido group which may be substituted with one or more identical or different substituents selected from the group consisting of an imido group and a halogen atom, and an aryl φ sulfonyl group thereof Can be substituted by Ch alkyl, Cl_e alkylsulfonyl, fluorenyl, aminopurinyl, mono-Ci-e-based amine-based or di-c, 6-alkylamino-based, F' 11 · -N=CR57(R58)(r58,), wherein R is a hydrogen atom or a C1-4 alkyl group, and R58 and f are the same or different from each other and represent a hydrogen atom or a C1_4 alkyl group, F' 12. 5 or 6 members of a monocyclic heteroaromatic group, and F 13·methylenediyl or ethyl (Amendment) 318197 447 1322688 29, a salt thereof, wherein R5 is a 5- or 6-membered single Cl-6 alkyl group, and the heteroaryl group may be substituted with a plurality of substituents: G' group] Gf 1. Ci-e can be substituted by a substituent selected from the group consisting of: [g, group] g, 1· halogen atom, g' 2. amine group, g 3. single C!-6 Alkylamino group, g, 4. a Cl-6 alkylamino group, g' 5. Cl-6 alkoxycarbonylamino group, and g' 6. hydroxyimino group, Patent No. 9511 S217 (98) July 1st, one or more G 2 halogen atoms, 3. Ci-e alkoxy which may be substituted by a halogen atom, G'4. aryloxy, G' 5. cyano, 6. -NCR59a)(R59a), wherein β and R:&gt;9a are identical or different from each other and exhibit gas shield C, - orthoquinone II or may be combined with two adjacent nitrogen atoms: 6 Å as early as each ring heterocyclic ring' and the saturated heterocyclic ring may be selected from the group consisting of a trans-group, an amine group, a mono-amino group and a di-(tetra)amino group (Revised) 318197 448 1322688 1 Substituted by one or more substituents of the group, S] G, 7. -C〇-N(R59b)(R59b,), wherein R and R are the same or different from each other and represent a hydrogen atom, a saturated 5 member or 6 a monocyclic heterocyclic group, or a Ci-e alkyl group which may be substituted by a heterocyclic group, a G' 8. aryl group, and a G 9.5 member or a 6 membered monocyclic aryl group which may be keto group or Sulfur steel base substitution. 30. A beta ruthenium compound according to claim 21 of the patent application or a pharmaceutically acceptable salt thereof, wherein R and R form a saturated 5-member or 6-shell monocyclic fluorenyl heterocyclic group together with an adjacent nitrogen atom and One of the saturated heterocyclic groups may have a double bond 'and condense with the ring to form a condensed ring, and the saturated heterocyclic group which may be condensed with a stupid ring to form a condensed ring may be selected from a tooth atom, a Cl 6 alkyl group, and a Ci- Substituting one or more substituents of group #, which consists of an alkoxy group, a thiol group, and a Ci-6 alkoxy group. 31. If you apply for Article 21 of the patent scope. A compound or a pharmaceutically acceptable salt thereof wherein the pyrazole compound is a pyridinium compound represented by the following formula (IV): (Amendment) 318197 449 1322688 wherein R4 denotes patent application No. 9511821*7 (July 1, 1998) (1) a hydrogen atom; (2) a Ci-e alkyl group which may be substituted by a selected one: Group A] A1. hydroxy, AZ. U-6 alkoxy, A3. -N(R41)(R^), Wherein R41 and R41' are 5 or 6 membered monocyclic heterocycles of each other, ',, and form a saturated A4. aryl group, A5. heteroaromatic group, A6. -C0-N(R4n)(R Chuan.), where R and R411 are identical or different from each other and One or more substituents of Group A, such as Group A, may be substituted with a 5- or 6-membered monocyclic heterocyclic ring of the adjacent nitrogen atom, 冋, a saturated carboxylic acid, and Α 8. Ci -6 alkoxy group, (3) C2-6 alkyl; (4) C2-6 alkynyl; (5) C3-8 ring-based; (6) C3-8 cycloalkyl-Ch alkyl; Amendment 318 197 450 1322688 Patent Application No. 95118217 or (July 9 10 * 曰; () Fang R, only and RX3 are identical or different from each other and represent a hydrogen atom or are selected from the group F below) Substituent, and m is 0 or an integer from 丨 to 2, i [F" group] F 1 · Cl -6 alkyl, F" 2. halogen atom, F" 3 · cyano, ® F" 4. hydroxy , F 5· Cl-4 alkoxy which may be substituted by one or more substituents selected from the group consisting of a carboxyl group and a Ch alkoxy group, F" 6 · halo-6 alkyl, F "Carboxy, F" 8. Cm alkoxycarbonyl, F" 9. -CO-N(R56a)(R56a.), wherein the ruthenium and R56a' are identical or different from each other and represent a hydrogen atom, At least one nitrogen atom saturated with 5 members or 6 members of a monocyclic heterocyclic group, or an alkyl group thereof Substituted by one or more substituents selected from the group consisting of: Α [Γ group] f" 1 · amine group, f 2. early Cl-6 compound amine group, f 3. diCl-6 yard group Amine, f" 4. Carboxy, (amendment) 318197 451 1322688 Patent Application No. 95118217 (July 10, 1998) f" 5. Cl-6 alkoxycarbonyl, 'f" 6. , and f" 7. A 5- or 6-membered monocyclic heterocyclic group having at least one nitrogen atom, F" 10. -N(R56b)(R55b,), wherein R56b and R56b are the same or Different and representing a hydrogen atom 'Cm alkyl group which may be substituted with an imido group which may be substituted by one or more identical or different substituents selected from the group consisting of a sub-amino group and a tooth atom Substituted 'arylsulfonyl" which may be substituted by Ci-6 alkyl, Cl-6 alkylsulfonyl, fluorenyl, aminomethylguanidino, mono-Ch-alkylaminomethylhydrazine or di-Cl-6 Aminoguanidino group, F" 11. -n=cr57(-n(r58)(r58')), wherein R57 is a hydrogen atom or Cm alkyl group 'R58 and r58· are the same or different from each other and represent hydrogen Atom or Cl6 alkyl ' • F" 12. 5 or 6 members of single ring Hong group, and F 13. methylenedioxy or ethylenedioxy-stretched. %· The carbazole compound of claim 21 or a pharmaceutically acceptable salt thereof, wherein the pyrazole compound is a pyridium compound represented by the following formula (¥): (amendment) 318197 452 No. 95118217 Application (July 1, 1998) Wherein R4 is as defined above, a heteroaromatic group, R'RlRY3; Het represents a 5- or 6-membered monocyclic atom or is selected from the group consisting of G, &amp; H being the same or different and representing an integer of hydrogen 2, , a substituent, and m, is 0 or 4 [Group of G] One or more of G 1 · Ci-e alkyl groups of the following g group may be substituted with a substituent selected from the group consisting of: [g, group] g' 1 · halogen atom, g' 2. amine group, g' 3. mono C!-6 alkylamino group, g 4. a Cl-6 alkylamino group, g'5. Cl-6 alkoxycarbonylamino group , g' 6 hydroxyimino group, G' 2 · halogen atom, G'3. Cm alkoxy group which may be substituted by _ atom, G'4. aryloxy group, G' 5. cyano group, (amendment) ) 318197 453 1322688 Patent Application No. 95118217 Gs 6. ~N(R59a)(R59a,) (July 10, 1998) where W' are identical or different from each other and are represented by the table G-6 alkyl, or ... And R59a. can be ', the second and the 5th or the Chang-戸 phase nitrogen atom together form a full I - dd, early clothing ', miscellaneous, and the saturated heterocyclic ring can be selected from the group consisting of hydroxyl soil, amine soil, early Cm silk Substituting one or more substituents of the group consisting of an amine group and a di &amp; G,7.~CO-N(R59b)(R59b), wherein R59b and R59b' are the same or different from each other and represent a hydrogen atom, a saturated 5 member or 6 membered monocyclic heterocyclic group, or &amp; 6 alkane The group may be substituted by a heterocyclic group, a 'G 8. aryl group, and a G 9 · 5 member or a 6 membered monocyclic heteroaryl group which may be substituted by a keto group or a sulfur group. 33. The pyrazole compound of claim 32, or a pharmaceutically acceptable salt thereof, wherein the Het ring is beta-bite, tri-salt or oxime. Sitting on the ring. 34. The pyrazole compound of claim 33, or a pharmaceutically acceptable salt thereof, wherein the pyrazole compound is a pyridinium compound represented by the following formula (VI): 454 (Revised) 318197 1322688 - Patent Application No. 95118217 _ wherein, as described above. (July 10, 1998) 35. The pyrazole compound of claim 21 or a pharmaceutically acceptable salt thereof, wherein the pyrazole compound or a pharmaceutically acceptable salt thereof is selected from the following Group: 5-(2-chloro-4, 5-difluoro-anthracenylamino)- 1H-pyrazole-3-carboxylic acid (pyridin-3-ylmethyl)-decylamine, 5_(2 - gas-4, 5-difluoro-phenylhydrazinylaminol than hydrazine-3-glycolic acid (pyridin-3-ylmethyl)-guanamine dihydrochloride, _ 5 - (2-gas-4, 5-difluoro-benzhydrylamino)-?-pyrazole-3-carboxylic acid (pyridin-3-ylmethyl)-decylamine hydrochloride, 5-(2-gas-4, 5-di) Fluoro-benzoguanidino)-ih-«bazole-3-deoxy acid (4-indolyl. sit-5-ylmethyl)-nitramine, 5-(2-gas-4, 5- Difluoro-benzoylamino)-ιη-° is more than oxo-acid (4-indolyl 1»--5-ylmethyl)-nonylamine, 5_(2-chloro-4, 5-Difluoro-phenylhydrazinoamino)-ΐΗ-β ratio 0 -3- 鲅 φ acid (4-methyl-oxazol-5-ylmethyl)-nonylamine p-toluene sulfonate ' 5 _ (2-Ga-4, 5-difluoro-benzoylamino)-1Η-0 ratio 0 sitting- 3-sodium (4-mercapto-oxazol-5-ylindenyl) guanamine L- ( + ) tartar Salt, 5-(2-chloro-4, 5-difluoro-benzylidenylamino)-1Η-°biazole-3-carboxylic acid (2,4-dimercapto-oxazol-5-ylindole ))-nonylamine p-toluenesulfonate '5_(2-chloro-4, 5-difluoro-benzhydrylamino) than salido-3-carboxylic acid (2,4-dimercapto-oxazole-5 -hydrazinyl)-nonylamine, 5-(2- gas-4,5-difluoro-benzoylamino acid (2,4-dimethyl-0 to -3-ylindenyl)- Amine, 455 (Revised) 318197 1322688 - Patent Application No. 95118217 (July 10, 1998) 5-(2-Chloro-4, 5-difluoro-benzhydrylamino)-1Η-pyridyl Zyridin-3-carboxy-acid diethyl decylamine, - 5-(2- gas-4, 5-difluoro-benzhydrylamino)-1 Η-pyrazole-3-carboxylic acid ethyl-(pyridine 4--4-mercapto)-nonylamine, 5-(2-chloro-4,5-difluoro-benzylidenylamino)-1Η-pyrazole-3-carboxylic acid (2-methoxy-B -Methyl-nonylamine, 5-(2-chloro-4, 5-difluoro-phenylhydrazino)-1Η-«biazole-3-carboxylic acid ethyl-(2-decyloxy) -ethyl)-nonylamine, 5-(2-gas-4,5-difluoro-phenylhydrazinoyl)_1H-pyrazole-3-carboxylic acid 2-fluoro-benzylamine, 5-( 2-chloro-4, 5-difluoro-benzylidenylamino)-1H-dbiazole-3-carboxylic acid 3-fluoro-benzazole , 5-(2-chloro-4, 5-difluoro-phenylhydrazinyl)-1Η-pyrazole-3-carboxylic acid 2-dimethylamino-benzamide, 5-(2-gas -4,5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxyl acid (4-ethoxycarbonyl-cyclohexyl)-propyl-decylamine, 5-(2-chloro- 4,5-difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid (6-decyloxypyridin-3-ylindenyl)-decylamine, 5-(2-chloro- 4,5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid 2,3-dimethoxy-benzylguanamine, 5-(2-chloro-4, 5-difluoro -benzoylamino)-1Η-α-pyrazole-3-carboxylic acid 2,4-dimethoxy-benzylamine, 5-(2-chloro-4, 5-difluoro-benzhydryl) Amino)-1Η-pyrazole-3-carboxylic acid 2,6-dimethoxy-benzylamine, 456 (amendment) 318197 1322688 - Patent Application No. 95118217 (July 10, 1998) 5- (2-Chloro-4, 5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxy-acid 3, 5-dimethoxy-benzylamine, 5-(2-chloro- 4,5-difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid 3,4-dimethoxy-benzylamine, 5-(2-chloro-4, 5-difluoro -benzylideneamino)-1Η-carbazole-3-carboxylic acid 2, 3-difluoro-tuberamine, 5-(2-chloro-4, 5- Fluoro - phenyl Yue acyl group) -1Η-. Bis-zolyl-3-carboxylic acid 2,4-difluoro-benzylamine, • 5-(2-chloro-4,5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid 2,5-difluoro-benzylamine, 5-(2-chloro-4,5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylic acid 2,6-difluoro-benzyl Indoleamine, 5-(2-chloro-4, 5-difluoro-phenylhydrazinylamino)-1Η-0-pyrazole-3-carboxylic acid 3,4-difluoro-benzylamine, 5-(2 - gas-4, 5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxyφ acid 3,5-difluoro-benzylamine, 5-(2-chloro-4, 5- Difluoro-benzhydrylamino)-1Η-°biazole-3-carboxylic acid (2-isopropoxy-π-pyridin-3-ylindenyl)-decylamine, 5-(2-chloro- 4,5-difluoro-phenylhydrazinoamino)-1Η_°biazole-3-carboxylic acid (2-phenoxypyridin-3-ylindenyl)-decylamine, 5-(2-chloro- 4, 5-difluoro-benzylidenylamino)-1Η-°biazole-3-carboxylic acid (3,5-difluoro-pyridin-2-ylindenyl)-decylamine, 5-(2- Chloro-4, 5-difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid 2-trifluorodecyl-benzylamine, 457 (amendment) 318197 1322688 Patent No. 95118217 (July 10, 1998) 5-(2-Chloro-4' 5~difluoro-benzoamylamino H-pyrazole-3-carboxylic acid 3-dimethylmethyl Amine, 5-(2-chloro-4,5-difluoro-phenylhydrazino)-1H-. ratio. -3 - traconic 4-trifluoromethyl-benzylamine, 5-(2- Gas-4, 5-difluoro-phenylhydrazinoamino)_1Η-pyrazole-3-carboxylic acid 4_t-butyl-benzylamine, 5-(2-chloro-4, 5-difluoro- Benzylamino-aminopyrazole-3-carboxylic acid (6-isopropoxy-pyridin-3-ylindenyl)-decylamine, \• 5_(2-chloro-4, 5-difluoro-crack Mercaptoamine)-ιη-pyrazole-3-carboxylic acid [2-(2, 2, 2-trifluoro-ethoxy)- acridine-3-ylsulfonyl]-nonylamine, 5-(2 - gas-4, 5-difluoro-phenylhydrazinoamino)-ιη-pyrazole-3-carboxylic acid 4-(2-dimethylamino-ethylaminopurinyl)-benzylamine , 5-(2-chloro-4, 5-difluoro-benzhydrylamino)-iH-pyrazole-3-carboxylic acid 4-ethyl-peptidylamine, 5-(2- gas-4, 5-difluoro-phenylhydrazinoamino)-iH-pyrazole-3-carboxylic acid 4-isopropyl-tyranamine, 5-(2- gas-4, 5-difluoro-benzamide Amino-based)-lH-pyrazole-3-carboxylic acid 2-aero-6-fluoro-benzylamine, 5~(2-chloro-4,5-difluoro-benzoinyl)-1Η- Pyrazole-3-carboxylic acid (6-ethoxy-pyridin-3-ylindenyl)-decylamine dihydrochloride, 5-(2~chloro-4, 5-difluoro-phenylhydrazine) Amino)-1Η-pyrazole-3-carboxylic acid (嗟 -4--4-ylmethyl) monodecylamine, 5-(2-chloro-4, 5-difluoro-benzylidenylamino)-1Η -pyrazole-3-carboxylic acid [6~(2,2,2-trifluoro-ethoxy)-bipyridin-3-ylindenyl]-decylamine II 458 (amendment) 318197 1322688 • Section 9591817 Patent Application - (July 1st, 1998) Hydrochloride, 5-(2-chloro-4, 5-difluoro-benzoylamino)_1H-pyrazole-3-carboxylate • Acid 2 , 6-dimercapto-benzylamine, 5-(2-chloro-4,5--fluoro-p-bromo-aminol group 一 3 3 3 3 3 [2_(pyridin-3-yl)-thiazole- 4-ylmercapto]-nonylamine dihydrochloride, 5-(2-chloro-4,5-difluoro-crackanylamino)_1Η-pyrazole-3-carboxylic acid (1Η-benzimidazole) _22-mercapto)monoamine dihydrochloride, [4-({[5-(2-chloro-4, 5-difluoro-benzhydrylamino)) Η 吡 嗤 嗤 -3 Methyl]-aminophenylmethyl)-benzylideneamino]-acetic acid methyl ester, 3-[4-({ [5-(2-gas-4, 5-difluoro-benzoguanidino)) _ιη- °pyrazole-3-carbonyl]-amino}-methyl)-phenylhydrazinyl]-propionic acid vinegar, 5-(2- gas-4, 5-difluoro-phenylhydrazine Amino)-ιη-η-pyrazole_3-a sulphuric acid (2-indenyl group) -11 塞 ° sit-4-yl fluorenyl)-nonylamine dihydrochloride, 5_(2-gas-4,5-·-rat~benylamino)-lU_o ratio 0--3 φ acid (3,5-dimethyl-isoxazol-4-ylindenyl)-decylamine, 5-(2- gas-4, 5-difluoro-phenylhydrazino)-ih-pyridyl Azole-3-buffer acid 4_[2_贰-(2-acetoxyethyl)-amino-ethylaminocarbamyl;| _ tanning amine, 5-(2-milk-4,5 -difluoro-benzhydrylamino)-1Η-° than saliva-3-acid 4-(2-hydroxy-ethylaminomethylindenyl)-benzylamine, 5_(2 - chaos ~4, 5-difluoro-benzoquinone-based amine))Η~·° ratio 0--3-sodium 4-(2-[(2-acetoxyethyl)-(2-hydroxyethyl)-amine Base]-ethylaminoglycolyl}-tuberamine, 459 (amendment) 318197 Patent No. 9511^217 &lt;July 1, 1998, -C-chloro-4,5-difluoro-phenylhydrazino)1Η_pyrazole-3_carboxylate (1methyl-1Η-stupidimide _ 2_ylmercapto)-indoleamine hydrochloride, 5-(2-chloro-4,5-difluoro-benzhydrylamino)-1-indole-pyrazole-3-oxoic acid (thiazole-2-yl group) Base) - guanamine dihydrochloride, (gas 4,5 gas-benzamide amino) ΐΗ ΐΗ-π than 嗤-3-carbamic acid (benzothiazol-2-ylmethyl) monoamine dihalide Acid salt, 5-(2-chloro-4, 5-difluorophenylindolyl)-1-indole-pyrazole_3_decanoic acid (2, 5-dimethyl-thiazolylhydrazyl) monodecylamine Dihydrochloride, 5-(2-chloro-4' 5-difluoro-phenylhydrazinyl)-1Η-pyrazole_3_carboxylic acid [2-(morpholin-4-yl)-thiazole_4 _ 曱 曱 ] 醯 醯 ] ] ] ] ] ] 5 5 5 5 5 5 5 5 5 5 5 5 5 5 5 5 5 5 5 5 5 5 5 5 5 5 5 5 5 5 5 5 5 吡 吡_Dimethyl-if]-pyrazole_4-ylmethyl)-decylamine, 5-(2- gas-4' 5-difluoro-benzhydrylamino) 4Η-pyrazole-3-carboxylate Acid (2-chloro-6-methyl-pyridine-3-ylmethyl) monodecylamine dihydrochloride, 5-(2- gas-4, 5-difluoro-benzhydrylamino)- 1 Η _pyrazole_3-carboxylic acid (2-dimethylamine) a thiazole-4_ylmethyl)-guanamine dihydrochloride, 5 (2 gas 4,5 a mouse 'this sylvanyl salivary-3 -acid (1-methyl-1H-pyrrole-2) -ylmethyl)-nonylamine, 5-(2- gas-4,5-difluoro-benzoinylamino). Compared with salic-3-carboxylic acid (3,4-dimethoxy-pyridine-2 Monodecylamine monoamine dihydrochloride, 5-(2-chloro-4,5-difluoro-benzhydrylamino)- 1H-pyrazole-3-carboxylic acid (5 dibutyl butyl) -嗟σ sit-2-ylmethyl)-chiral amine dihydrochloride, 5-(2-chloro-4,5-difluoro-benzhydrylamino)_1{1_pyrazole-3_carboxylate Acid (5-methyl-2-phenyl-2H-[1,2,3]triazol-4-ylmethyl)-bristamine (amendment) 318197 460 Patent No. 95118217 (July 1998) 10th) 5-(2-chloro-4, 5-difluoro-phenylhydrazino)-1Η-«biazole-3-carboxylic acid [4-(t-butoxycarbonyl-amino)-indole -pyridin-2-ylindenyl]-nonylamine, 5-(2-chloro-4,5-difluoro-benzoindolyl)-1Η-pyrazole-3-carboxylic acid [4-indenyl] -2-(morpholin-4-yl)-thiazol-5-ylindenyl]-nonylamine dihydrochloride, 5-(2-chloro-4,5-difluoro-benzhydrylamino)- 1Η-pyrazole-3-carboxylic acid (pyridin-3-ylindenyl)-decylamine 3/2 hydrochloride half-water , 5-(2-chloro-4, 5-difluoro-phenylhydrazino)-1Η-indazole-3-carboxylic acid 2-amino-benzylamine, 5-(2-chloro- 4, 5-Difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid 2-decyloxy-benzylamine, 5-(2-chloro-4, 5-difluoro-benzoic acid Mercaptoamine)-1Η-η-pyrazole-3-carboxylic acid 3-decyloxy-benzylamine, 5-(2-chloro-4,5-difluoro-benzoinyl)-1Η- Oxazole-3-carboxylic acid 4-methoxy-benzylamine, 5-(2-chloro-4, 5-difluoro-phenylhydrazino)-1Η-indazole-3-carboxylic acid 4- Methyl-benzylamine, 5-(2-chloro-4,5-difluoro-benzofuranylamino)_111-〇 ratio ° sit-3-retinic acid 4-fluoro-benzylamine, 5-( 2-chloro-4,5-difluoro-benzylidenylamino)-1Η-η-pyrazole-3-carboxylic acid 4-chloro-benzylamine, 5-(2-chloro-4, 5-difluoro -Phenylhydrazinoamino)-1-pyridazole-3-carboxylic acid 4-ethoxycarbonyl-benzylamine, 461 (amendment) 318197 Patent No. 95,921,217 (July 1st, 1998) 5-(2-Gas-4,5-di-fluoro-phenylhydrazino)-1Η-pyrazole-3-carboxyjun, fluorenyl-tuberamine, 5-(2-chloro-4, 5 -difluoro-benzoguanidino)-1Η-pyrazole-3-carboxyindole di-p-nonylamine, 5-(2-gas-4,5-di-fluoro -benzoylamino)-1Η-pyrazole-3-carboxylate (cyano-p-styl-methyl)-decylamine, 5-(2-chloro-4, 5-difluoro-benzamide Amino-pyrazole-3-carboxyl cyclohexylmethyl-decylamine, 5-(2-gas-4,5-difluoro-benzoinylamino)-ΐΗ-σ ratio 0 -3-tagamic acid (2-hydroxy-ethyl)-phenyl-decylamine, 5-(2-gas-4, 5-difluoro-benzhydrylamino)-iH-pyrazole-3-carboxylate Acid cyclohexyl-mercapto-nonylamine, 5-(2-gas-4,5-difluoro-phenylhydrazino)-!!]-pyrazole-3-carboxylic acid cyclohexyl decylamine, 5- (2-Chloro-4, 5-difluoro-phenylhydrazino)- 1H_pyrazole-3-carboxylate Wangshenyl-ethylamine, 5-(2-chloro-4, 5- Difluoro-benzoylamino)_ih-indole ratio salivary-3-decanoic acid dipropylcyclohexyl-bristamine, 5-(2-chloro-4, 5-difluoro-benzoylamino) _η_β is more than cyclohexyl-(pyridin-2-ylindenyl)-decylamine, 5-(2-chloro-4' 5-difluoro-benzoguanidino)-1H-pyrazole-3 Carboxylic acid thiol-(1-methyl-slightly -4-yl)-nitramine, 5-(2-chloro-4,5-difluoro-phenylhydrazinoyl)_111_pyrazole_3_ Carboxylic acid [(3,4-decylenedioxyphenyl)-indenyl]-decylamine hydrochloride, ( Amendment) 318197 462 丄 688 Patent Application No. 95118217 • (July 1, 1998) 5-(2-chloro-4, 5-difluoro-stupyl arylamino)-1|}- ° ratio ® sit-3-acid benzyl-butyl-decylamine, 5-(2-chloro-4, 5-difluoro-benzoammonium amino group than salino-3-acid benzyl-(4 -trans-butyl-butyl)-chiral amine hydrochloride, 5-(2-chloro-4,5-difluoro-anthracenylamino)-ih-pyrazole-3-indole butyl-ethyl - guanamine, 5-(2-chloro-4, 5-dioxo-stupholylamino-pyrrol-3-salicylate cyclohexyl-propyl-decylamine, 5-(2-chloro-4, 5 _Digas-phenylhydrazino)-iH-0 than saliva-3-acid butyl-cyclohexyl-decylamine, 5-(2-chloro-4, 5-difluoro-benzoquinone比 0 0 sit-3-oxocyclohexyl-(2-methoxy-ethyl)-decylamine, 5-(2-chloro-4, 5-difluoro-benzoquinone)-111-〇 Ratio of -3-oxocyclohexyl-(pyridin-3-ylindenyl)-nonylamine, 5-(2-chloro-4,5-difluoro-benzoinyl)-1Η-ηΛ° Sitting -3- retinoic acid [2_(Methyl- 4:-yl)-phenyl]-bristamine, 5-(2- gas-4, 5-difluoro-phenylamino) Dibutyl decylamine, 5-(2-gas-4, 5-difluoro-benzofuranylamino)-1Η-σ ratio 嗤- 3-sodium bismuth-(2-methoxyethyl)-decylamine, 5-(2-chloro-4, 5-difluoro-benzofuranylamino)-1Η-π than saliva-3-quinone Acid (2-methoxyethyl)-propyl-decylamine, 5-(2-chloro-4,5-dioxa-benzoylamino)-1Η_ο ratio. -3-Oxyl butyl-(tetrahydro-n-butyl-4-yl)-nitramine, 463 (Revised) 318197 1322688 Patent Application No. 95118217 (July 10, 1998) 5-(2-gas -4' 5-difluoro-phenylhydrazinoamino)_1H_pyrazole-3-carboxylic acid (2-methoxy-ethyl)-(tetrahydro-pyran-4-yl)-decylamine, 5-(2-Gas-4, 5-difluoro-phenylhydrazino)1H_pyrazole_3_carboxylic acid cyclopentyl-(2-methoxy-ethyl)-decylamine, 5-( 2-gas-4,5-difluoro-phenylhydrazinoamino)_1H_pyrazole_3_carboxylic acid cyclohexyl-(3-decyloxy-propyl)-decylamine, 5-(2-gas -4,5-difluoro-phenylhydrazinoyl H_pyrazole-3_reoxycyclohexyl-(2-ethoxy, ethyl)-decylamine, _ 5-(2-chloro- 4' 5-difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid cyclohexyl-(2-isopropoxy-ethyl)-decylamine, 5-(2-gas-4, 5 -difluoro-phenylhydrazinoamino)_1H-pyrazole_3_carboxylic acid cyclohexyl-(2-propoxy-ethyl decylamine, 5-(2 gas-4, 5-difluoro-benzoic acid)酿 胺 ) _ — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — - awkward amino-amine η is more than a saliva _ acid butyl-(bt-butoxycarbonyl-piperidin-4-yl)-decylamine, 5-(2- gas-4, 5-difluoro-benzoguanidino)-1Η-pyrazole_ 3-carboxylic acid butyl-(tetrahydro-sulfanyl-4-yl)-decylamine, 5-(2- gas-4, 5-difluoro-benzoylamino)-1-indole-pyrazole_3 _Carboxylic acid butyl-(2-decyloxy-ethyl) monodecylamine, 5-(2- gas-4, 5-difluoro-adolylamino)-1-indole-pyrazole-3-carboxylic acid Butyl-indole butyl-3-yl hydrazino) monoamine, 5-(2-chloro-4, 5-difluoro-crackanylamino hydrazine-pyrazolecarboxylic acid benzyl-(2-oxime Oxy-ethyl)-decylamine, (amendment) 318197 464 1322688 Patent No. 95118217 (July 1st, 1998) 5-(2-gas-4, 5-difluoro-benzoquinone Amino-)-ih-pyrazole-3-carboxylic acid butyl-(piperidin-4-yl)-decylamine, 5-(2-a-4,5-difluoro-benzoinyl) -ih-pyrazole-3-carboxylic acid (1-ethenyl hydrazin-4'-yl)-butyl-decylamine, 5-(2- gas-4, 5-difluoro-benzoammonium amide ι)-ιη-pyrazole-3-carboxylic acid butyl-(1-methyl-mercapto-bran-4-yl)-nitramine, 5-(2-chloro-4, 5-difluoro-benzoic acid Mercaptoamine)-ih-d-pyrazole-3-carboxylic acid butyl _(ethoxyphenoxyl- π chen -4- )-decylamine, 5-(2- gas-4, 5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid butyl-(1-acid oxalate-bite 4-yl)-nonylamine, 5-(2-gas-4, 5-difluoro-benzhydrylamino)-1-indole-pyrazole_3_carboxylic acid butyl _(1, _yl-hexa Hydrogen-1 and 6-thioindole-4-yl)-decylamine, 5_(2-qi_4,5-one gas-benzoquinone-based amine group 〇3--------- Keto-hexahydro-1 λ4-thiopiperazin-4-yl)-decylamine, 5-(2- gas-4, 5-difluoro-benzhydrylamino)-1Η-pyrazole_3_carboxylate φ acid (6-decyloxy-pyridin-3-ylindenyl)-propyl-decylamine, 5-(2-chloro-4,5-difluoro-benzoinyl)-1Η-pyrazole_ 3-carboxylic acid propyl-(pyridin-3-ylmethyl)-decylamine, 5-(2- gas-4,5-difluoro-benzoinylamino)-1Η-pyrazole_3_carboxylate Acid 4-diethylaminocarboxamyl-benzylamine, 5-(2-chloro-4,5-difluoro-benzhydrylamino)-! Η-pyrazole_3_carboxylic acid 3-diethylamino aryl-alkenylamine, 5-(2-chloro-4,5-difluoro-benzhydrylamino)-pyrazole_3 _carboxylic acid 4-ethylaminomethylmercapto-benzylamine, (amendment) 318197 465 1322688 Patent No. 95118217 (July 1, 1998) 5-(2-chloro-4, 5 -difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid 3-ethylaminomercapto-benzylamine, 5-(2-ethane-4, 5-difluoro-benzene Hydrazinyl)-1Η-pyrazole-3-carboxylic acid 4-aminomethylindolyl-benzylguanamine, 5-(2-chloro-4, 5-difluoro-benzhydrylamino)- 1Η-pyrazole-3-carboxylic acid (1-acid oxalyl-1-l-pyridine-4-yl)-propyl-decylamine, 5-(2-gas-4, 5-difluoro-benzamide) Amino-pyridyl-3-carboxylic acid U-carboxyethyl-piperidin-4-yl)-propyl-decylamine, Lu 5-(2-chloro-4, 5-difluoro- Benzoylamino)-ih-carbazole-3-carboxylic acid [1-(2-carboxypropenyl)-piperidin-4-yl]-propyl-decylamine, 5-(2-gas- 4, 5-Difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid cyclopropyl-(6-methoxy-pyridin-3-ylmethyl)-decylamine, 5_(2 _ gas-4,5_digas-benzoquinone-based amine)-111_11 than salivary-3-reoxycyclobutyl-(6- Methoxy-pyridin-3-ylindenyl)-decylamine, 5-(2-chloro-4,5-difluoro-benzoylamino)-1Η-0 ratio 0 sitting-3-slow acid Cyclopropyl decyl-(6-decyloxy-pyridin-3-ylindenyl)-decylamine, 5-(2-chloro-4, 5-difluoro-phenylhydrazino)-1Η-pyridyl Oxazole-3-carboxylic acid (6-didecylamino-indenyl-3-ylmethyl)-decylamine, 5-(2-chloro-4, 5-difluoro-benzoinylamino) -1Η_pyrazole-3-carboxylic acid (6-didecylamino-pyridin-3-ylindenyl)-propyl-decylamine, 5_(2-disorder-4,5_digas-benzoquinone Amino group) -1Η_0 ratio 0 sitting -3 - benzoic acid benzyl-(2-carboxy-ethyl)-decylamine, 5-(2-chloro-4, 5-difluoro-benzhydrylamino) -1 Η-pyrazole-3-carboxylic acid benzyl-(2-ethoxycarbonyl-ethyl)-decylamine, 466 (amendment) 318197 Patent No. 95118217 (July 1st, 1998) 5- (2-Chloro-4, 5-difluoro-phenylhydrazinylamino)_ih-pyrazole-3-carboxylic acid (6-chloro-pyridin-3-ylmethyl)-propyl-decylamine, 5- (2-Chloro-4, 5-difluoro-phenylhydrazinyl)-iH-pyrazole-3-carboxylic acid 2,6-dichloro-benzylamine, 5-(2-chloro-4, 5- Difluoro-benzoguanidino)-in-pyrazole-3-carboxylic acid (3, 5-dichloro-0-pyridinyl-4- Methyl)-nonylamine, 5-(2_chloro-4,5-difluoro-cracked arylamino group than sputum-3-sodium sulphate (3,5-dichloro-0-pyridinyl 4-曱-)-propyl-nonylamine, 5-(2-chloro-4, 5-difluoro-phenylhydrazino)-indole-pyrazole-3-carboxylic acid [6-(1Η-pyrazole) -1-yl)-pyridin-3-ylmethyl]-indolyl dihydrochloride, 5-(2-chloro-4,5-difluoro-crackanylamino)_1Η-pyrazole_3 Carbonic acid [6_(4-hydroxy-0 benzo-1-yl)-pyridin-3-ylindenyl]-nonylamine dihydrochloride, 5-(2-wind &lt;_4,5-monofluoro-benzoquinone-based amine)-1^0 is more than sputum--3-acid (2-11 than biti-ethyl)-nitramine, 5-(2-gas_ 4,5_&gt;One gas-benzoquinone-based amino group-probiotic-3-hypo-acid (2-pyridine-3-yl-ethyl)-decylamine, 5-(2-chaotic_4,5-one gas-benzene Brewing base amino group ratio. sit a 3_slow acid (2-° ratio bite-yl-ethyl)-bristamine ' 5-(2-chloro-4, 5-difluoro-benzoguanidino) -1H-pyrazole_3_oleic acid (4-[1,2,3]thiadiazol-4-yl-benzyl)-decylamine, 5-(2_乳一4,5-一ii-stupid Brewing arylamino)-ΐΗ-«» than salino-3-acid (5-mercaptopyrimidin-2-ylindenyl)-bristamine, (amendment) 318197 467 5~(2-gas-4 , 5- 2: Fluorine - Patent Application No. 95118217 (July 1st, 1998) 'Benzane Amine Group' -1Η-0 ratio ° sit-3-carboxylic acid 0 than phenyl-2-ylindole Amine, 5-(2-chloro-4, 5-di:fluoro-benzylamino)-1 Η-〇pyr-3-quinic acid quinolin-5-yl decylamine, 5-(2-oxo -4,5-difluoro-benzoylamino)-1Η-pyrazole-3-decanoic acid 喧-8-8-ylamine, 1322688 5-(2- gas-4' 5-difluoro-benzene Mercapto Aminopyrazole-3 Monocarboxylic Acid Isoquinolin-5-ylguanamine, 5-(2- -4,5-difluoro-phenylhydrazinoamino)_1H_pyrazole_3-sodium acid [3_ethoxy-5-(1-ethoxycarbonyl-i-methyl-ethylpyridine_2_ ]-amine, 5-(2- gas-4, 5-difluoro-phenylhydrazino)-ih-«biazole-3-carboxylic acid [3-ethyl lactyl_5-(1- Ethoxyl-1-yl-trans-ethyl)-n-r-but-2-yl]-decylamine, 5-(2-gas-4, 5-difluoro-phenylhydrazino)-in- Pyrazole-3-carboxylic acid [5-(1-methyl-1-yl-1-fluorenyl-ethyl)-3-ethoxy-indole ratio 0-but-2-yl]-nonylamine, 5-(2-chloro -4,5-difluoro-phenylhydrazinoamino)-ih-pyrazole-3-carboxylic acid [5-(indolyl-ethyl)-3-ethoxyl-butyl-2-yl ]-Anthracene ' 5-(2-chloro-4, 5-difluoro-benzylidenylamino)-ιη-pyrazole-3-carboxylic acid (〇比哄_2-ylindenyl)-nitramine , 5-(2-chloro-4, 5-difluoro-phenylhydrazino)-indole-pyrazole-3-carboxylic acid [6-(thiomorpholin-4-yl)-pyridin-3-yl曱 ] 醯 醯 , 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 Sodium sulphate [6-(1,1-disteel-1 λ 6-thiophene-4-yl)-n ratio bite_3_ylmercapto]-nonylamine, 5-(2-chloro-4 , 5-difluoro-benzhydrylamino)-ιη-pyrazole-3-carboxylic acid (4, 5-dibromo-thiophen-2-ylmethyl)-decylamine, 5-(2-chloro- 4,5-difluoro-phenylhydrazinoamino)-ιη-pyrazole-3-carboxylic acid (5-chloro-thiophen-2-ylmethyl)-decylamine, 5-(2-chloro-4, 5-difluoro-phenylhydrazinoamino)-ιη-pyrazole-3-carboxy-acid (4-ethyl-2-methylisoindol-5-ylindenyl)-nitramine, 5-(2) - gas-4, 5-difluoro-benzhydrylamino)-ih-pyrazole-3-carboxylic acid (2-ethyl-4-methyl-causal-5-ylmethyl)-nitramine Dihydrochloride, 5-(2-chloro-4, 5-difluoro-benzylidenylamino)_ih-pyrazole-3-carboxylic acid ([2, 2']bithiophen-5-ylfluorenyl - indoleamine, 5-(2-chloro-4, 5-difluoro-benzylidenylamino)-ιη-π-pyrazole-3-carboxylic acid (3-methoxy-thiophen-2-ylindenyl) )-decylamine, φ 5 -(2_gas~4, difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid (4, 5-dioxa-thiophen-2-ylindenyl) - indoleamine, 5-(2-chloro-4, 5-difluoro-benzhydrylamino)-ιη-pyrazole-3-carboxylic acid (2, 5-dimercapto-oxazole-4 Base -p-amine, 5-(2-chloro-4, 5-difluoro-phenylhydrazinyl)-ιη-pyrazole-3-carboxylic acid (2-hexyl-4-methyl-oxazole- 5-ylmethyl decylamine, 5-(2-chloro-4, 5-difluoro-benzylidenylamino)-ιη-pyrazole-3-buffer acid (4-decyloxy-thiophene-3-曱 ) 醯 醯 , , , , 让 让 让 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 Request (July 10, 1998) Acid (4-methyl-2-phenyl-oxazole-5-ylmethyl)-decylamine, 5-(2-chloro-4,5-difluoro-benzene Formic acid amino)-1Η-π ratio 0 decanoic acid (2-mercapto-4-phenyl-oxazol-5-ylindenyl)-decylamine, 5-(2-chloro-4, 5-di Fluorine-acnemethylamino)-1Η-°biazole-3-carboxylic acid (4-hexyl-2-mercapto-oxazol-5-ylmethyl)-guanamine dihydrochloride, 5-( 2-Chloro-4, 5-difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid (6-a-pyridin-3-ylindenyl)-decylamine, 5-(2- Chloro-4, 5-difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxydecanoic acid (6-chloro-pyridin-3-ylmethyl)-guanamine dihydrochloride, 5 - (2 - gas - 4,5 - a chaotic - benzoquinone-based amino group) - sitting --3-rebel (4H-[1,2,4] Zyridin-3-ylmethyl)-decylamine, 5-(2- gas-4, 5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid (4H-[1,2 , 4] triazol-3-ylmercapto)-decylamine dihydrochloride, 5-(2-chloro-4, 5-difluoro-benzhydrylamino)-lH-pyrazole-3- Acid (5-fluoro-4H-quinoxaline-3~yl)-nonylamine•5-(2-chloro-4,5-difluoro-phenylhydrazino)-ih-pyrazole-3-indole Acid (5-fluoro-4H-quinazolin-3-yl)-guanamine dihydrochloride, 5-(2-chloro-4, 5-difluoro-phenylhydrazino)-ih-pyrazole a 3-acidic acid (4,6-dimethyl-pyridin-3-ylindenyl)-decylamine, 5-(2- gas-4,5-methyl-benzoylamino)-1Η- 〇 η η -3- ̄ ̄ ̄ ̄ ̄ ̄ ̄ ̄ ̄ ̄ ̄ ̄ ̄ ̄ ̄ ̄ ̄ ̄ ̄ ̄ ̄ ̄ ̄ ̄ ̄ ̄ ̄ ̄ ̄ ̄ ̄ ̄ ̄ ̄ ̄ ̄ ̄ ̄ ̄ ̄ Stearylamino)-lH_〇 〇 竣-3-decanoic acid (2-decyloxy-6-fluorenyl-pyridin-3-ylindenyl)-decylamine, 5-(2-disorganized-4, 5-Fluoro-benzoquinone-based amine group than saliva-3-slow 470 (amendment) 318197 1322688. Patent application No. 95118217 (July 1st, 1998) Climbing acid (4-methoxy-6) _Methyl-pyridin-3-ylindenyl)-decylamine, • 5-(2-chloro-4, 5-difluoro-benzamide Amino)-1Η-°biazole-3-carboxylic acid (4-methoxyoxy-6-indolyl~pyridin-3-ylindenyl)-guanamine dihydrochloride, 5-(2-chloro-4 , 5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid (2-decyloxy-4,6-dimethyl-pyridin-3-ylmethyl)-decylamine, 5-(2-chloro-4, 5-difluoro-benzylidenylamino)-1Η-pyrazole-3-carboxylic acid (2-methoxy-4,6-dimercapto-pyridine-3- Methyl)-nonylamine dihydrochloride, • 5-(2-chloro-4,5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid (3-methyl- Pyridin-2-ylmethyl)-decylamine, 5-(2-chloro-4, 5-difluoro-benzylidenylamino)-1Η-σ-pyrazole-3-carboxylic acid (5-methyl- 〇 唆 3- 3- 3- 3- 3- 3- 3- 3- 酿 酿 酿 酿 酿 酿 酿 酿 酿 酿 酿 酿 酿 酿 酿 酿 酿 酿 酿 酿 酿 酿 酿 酿 酿 酿 , 酿-pyridin-3-ylmethyl)-decylamine, 5-(2-chloro-4,5-difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid (6-methyl -〇 0 0 _2 _ _ ) ) ) 酿 酿 酿 酿 酿 酿 酿 酿 酿 ' ' ' ' ' ' ' ' ' ' ' ' ' ' ' ' ' ' ' ' ' ' 5- 5- 2- 2- Bite -3_ylmethyl)-bristamine dihydrochloride ' 5-(2-gas-4, 5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylic acid ( 6-fluoro-pyridin-3-ylmethyl)-guanamine dihydrochloride, 5-(2-chloro-4,5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylate Acid (3-carboxy-phenylmethyl-decylamine' 5-(2- gas-4, 5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid 3-methylsulfonate Amino-benzylguanamine, 471 (amendment) 318197 1322688 951182; Π mirror patent application (July 10, 1998) 5-(2-chloro-4' 5-difluoro-benzoamylamine Base) Η 吡 _ _ azole _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _Citrate 3-acetic acid amine-tuberculating amine, 5-(2-chloro-4, 5-difluoro-crackanylaminos-sodium sulphate 4-acetamido-ylamine, 5-(2-Gas-4, 5-difluoro-anthracenylamino)_1H-pyrazole_3-dicarboxylic acid (2-phenyl-snap-4-ylmethyl)-decylamine, 5 -(2-Gas-4,5-difluoro-abidomethylamino)- 1H_pyrazole_3-acid (00_1-phenyl-ethyl)-nitramine, 5-(2_gas- 4,5_-gas-present arylamino)_1H-ntb〇-3-oxanoic acid ((S)-l-phenyl-ethyl)-nitramine, 5-(2-gas-4, 5 -difluoro-benzoammonium amino)-ih-pyrazole-3-acid (6-benzene -Pyridin-3-ylindenyl)-nonylamine dihydrochloride, 5-(2-methyl-4,5-difluoro-phenylhydrazino)-ih-pyrazole-3-acid (6-chloro-0 to dimethyl sulfhydryl)-bristamine dihydrochloride, 5-(2-chloro-4,5-difluoro-crackanylamino)-1Η-pyrazole-3-carboxylate Acid (2_chloro-° ratio biting_3_ylindenyl)-guanamine dihydrochloride, 5_(2-methyl-4, 5-difluoro-phenylhydrazino)-1Η-° ratio . Sodium - 3-decanoic acid (6-gas-D ratio-ylmethyl)-guanidine sodium salt 5_(2-chloro-4,5-difluoro-benzhydrylamino)-1Η-π ratio Salivation-3-acidic acid [1_(π 比 _3 -yl)-ethyl]-acid amine dihydrochloride, 5-(2-chloro-4, 5-difluoro-benzoylamino) -1Η-° than saliva-3-retinic acid (2-fluoro-pyridine-3-ylmethyl)-nitramine dihydrochloride' 472 (amendment) 318197 Patent Application No. 9'5118217 (98 years 7) 1st day of the month) 5_(2-chloro-4, 5-difluoro-phenylhydrazino)-1Η-°Bizozole-3-derivative (2-mercapto-pyridin-3-ylindenyl) I-amine dihydrochloride ' 5 —(2-chloro-4,5-difluoro-benzoindolyl)_1Η-η-pyrazole-3-carboxylic acid (biphenyl-3-ylmethyl)-indole Amine, 5-(2-chloro-4, 5-difluoro-benzylidenylamino)_1H-pyrazole-3-carboxylic acid ((lR, 2S)-2-hydroxy-hydroindol-1-yl) _Acetamine ' 5-(2-chloro-4, 5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylic acid ((lS,2R)-2-hydroxy-hydroquinone-1 -yl)-nonylamine, 5-(2-chloro-4,5-difluoro-phenylhydrazinylamino)-1 -pyrazol-3-carboxylic acid (6-phenyl-pyridine-3-ylindole) Monoamine dihydrochloride, 5-(2-chloro-4, 5-difluoro-phenylhydrazino) -1Η-pyrazole-3-carboxylic acid (6-methyl-2-π-pyridyl_3~ylindenyl)-decylamine hydrochloride, 5-(2- gas-4,5-difluoro-benzene Alkylamino)-1Η-π ratio. Sodium-3-reactive benzyl-methyl-decylamine, 5-(2-chloro-4,5-difluoro-benzylidenylamino)-lH-pyrazole-3-carboxylic acid benzamide 5-(2-chloro-4, 5-difluoro-phenylhydrazino)-ιη-pyrazole-3-carboxylic acid phenyl decylamine, 5-(2- gas-4, 5-difluoro- Benzoylamino)-ιη-pyrazole-3-indolyl-phenyl-decylamine, 5-(2-gas-4, 5-difluoro-benzoinyl)-ιη- Pyrazole-3-resolic acid (Brigade _1-yl)-nitramine, 5-(2-Gas-4, 5-difluoro-benzhydrylamino)- 1 Η-pyrazole_3_carboxylic acid (4_Ethoxycarbonyl-Big pyridine~; yl)- decylamine, (amendment) 318197 473 1322688 Patent application No. 95118217 (July 10, 1998) 5-(2-chloro-4, 5-di Fluorine-acidyl mercaptoamine H_pyrazole_3_carboxylic acid (4-methyl-pyridin-1-yl)- ugly amine, 5-(2-gas_4, 5-difluoro-armamo Mercaptoamine)_1H_0-pyrazole_3_carboxylic acid (4-sulfanyl-indenyl-1-yl)-bristamine, 5-(2-chloro-4,5-difluoro-m-decylamino Η-pyrazole-3 carboxylic acid stupid ethyl decylamine, 5-(2-chloro-4, 5-difluoro- cumylamino)- 1 Η-pyrazole- 3 carboxylic acid fluorenyl-benzene Ethyl-decylamine, Lu 5-(2-chloro-4,5-difluoro-stupylamine Base)-1Η-pyrazole-3-carboxylic acid ethyl-phenyl-decylamine, 5-(2-milo-4,5-difluoro-benzhydrylamino group than 嗤-3-acid acid stupid ( 1,2,3,4-tetrahydroisoquinolin-2-yl)-nonylamine, 5-(2-chloro-4, 5-difluoro-crackanylamino)-ιη-pyrazole-3 -carboxylic acid hydrazinocarbonyl-benzyl)-decylamine, 5-(2-chloro-4,5-difluoro-phenylhydrazinoamino)-1H-pyrazole-3-carboxy φ acid ((R) -a-methoxycarbonyl-benzyl)-nonylamine, 5-(2-chloro-4, 5-difluoro-benzoamitoylamino)-ih-pyrazole-3-carboxylic acid benzene (1,2 ,3,4-tetrahydroquinoline-byl)-decylamine, 5-(2- gas-4,5-difluoro-phenylhydrazinoamino)-1Η-η-pyrazole-3-carboxylic acid benzene -propyl-decylamine, 5-(2- gas-4, 5-difluoro-benzoguanidino)-1Η-pyrazole-3-carboxylic acid butyl-phenyl-decylamine, 5- (2 - gas-4,5_diqi-benzhydrylamino)-111-° than sputum -3-sodium pentyl-phenyl-decylamine, 474 (amendment) 318197 1322688 No. 95118217 Patent Application (July 1st, 1998) 5-(2-Chloro-4, 5-difluoro-benzylidenylamino)-ih-pyridin-3-carboxylic acid diphenylmethyl-decylamine , 5-(2-Gas-4, 5-difluoro-benzhydrylamino)_ih-pyrazole-3-carboxylic acid (pyridine-2 -ylmethyl)-guanamine hydrochloride, 5-(2-gas-4,5-difluoro-phenylhydrazino)-ih-pyrazole-3-carboxylic acid (° ratio pyridine-4- Hydrazinium hydrochloride, 5-(2-chloro-4, 5-difluoro-benzylidenylamino)-ih-pyrazole-3-carboxylic acid ((R)-2-hydroxyl -1-phenyl-ethyl)-decylamine, fen. (2-chloro-4, 5-difluoro-benzylidenylamino)_ih-pyrazole-3-carboxylic acid ((S)-2- Hydroxy-1-phenyl-ethyldoximine, 5-(2-gas-4, 5-difluoro-benzylidenylamino)- 1H-pyrazole-3-carboxylic acid 4-dimethylamine Base-benzylamine, 5 (2 gas - 4,5_·-rat-branched amine-based sit-_3_saucy acid (furan-2-ylmethyl)-decylamine, 5-(2-gas- 4,5-difluoro-benzhydrylamino)-ih-pyrazole-3-carboxy φ acid (thienylmethyl) monoamine, 5-(2- gas-4, 5-difluoro-benzene Mercaptoamine)-iH-pyrazole-3-carboxylic acid (2-methoxy-phenyl)-decylamine, 5-(2- gas-4, 5-difluoro-benzhydrylamino group嗤-3-teric acid (2-decyloxy-phenyl)-methyl-decylamine, 5-(2-chloro-4, 5-difluoro-phenylhydrazino)-1珏-〇 Ratio -3 - oxalic acid 4-dimethylamino-benzylamine hydrochloride, 5_(2-chloro-4, 5-difluoro-benzene Methyl decylamino)-lH-pyrazole-3-carboxylic acid 3-amino-benzamide 475 (amendment) 318197 1322688 Patent No. 9511821 &quot; Patent No. 7 (July 1st, 1998) 5-(2-chloro-4, 5-difluoro-benzhydrylaminopyrazole-3-oxoic acid 4-amino-benzylguanamine ' 5-(2-chloro-4, 5-difluoro- Benzoylamino)_ιΗ_pyrazole_3_acid acid 2-methyl-benzylamine, 5-(2-chloro-4,5-difluoro-benzylideneamino)_1H-pyrazole _3-monocarboxylic acid 3-methyl-benzylamine, 5-(2-chloro-4,5-difluoro-benzoylamino)-ijj-e than 3--3-carboxylic acid Amino-benzylguanamine, Lu 5-(2-chloro-4,5-difluoro-phenylhydrazino)-1Η-°biazole-3-decanoic acid (2-methoxy-anthracene) -3-ylmethyl)-bristamine, 5-(2-chloro-4, 5-difluoro-phenylhydrazino)-indole-pyrene-3-deoxy-2-mercaptoamine , 5-(2-chloro-4,5_-fluoro-benzylamino)_1Η-0-嗤-3-glycolic acid 3-chloro-benzylamine, 5-(2_气-4,5- ·一乱-本本基基基基)_1Η_π ratio 0 sit-3_ 叛 φ acid 3-曱 oxycarbonyl-benzyl hydrazine ' 5- (2- gas-4,5-difluoro-benzamide) Base) - 11}-° ratio * sit-3 - slow acid 3-carboxy-benzylamine, 5-(2- -4,5-difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid (6-trifluoromethyl-indole ratio-3-ylindenyl)-nonylamine, 5-( 2-Chloro-4, 5-difluoro-benzylamino group is more than 0--3-acid (2_ethoxy-oxime ratio _3_yl fluorenyl)-bristamine, 5_(2_ Gas-4, two gas, one brewing amine group ratio, sit--3-resorcinate (2-didecylamino-ethyl)-decylamine 476 (amendment) 318197 1322688 patent application No. 95118217 (July 1st, 1998) 5-(2-chloro-4, 5-difluoro-phenylhydrazino)-lH-pyrazole-3-carboxylic acid ethyl-(2-didecylamine 5-ethyl)-guanamine dihydrochloride, 5-(2-gas-4, 5-difluoro-phenylhydrazino)-lH-pyrazole-3-decanoic acid cyclohexyl-(2- Dimethylamino-ethyl)-decylamine, 5-(2-gas-4, 5-difluoro-phenylhydrazino)-lH-D-pyrazole-3-furic acid (4-methoxy -Pyridin-2-ylmethyl)-decylamine, 5-(2-chloro-4,5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid (2, 6- Dimethoxy-pyridin-3-ylindenyl)-decylamine, 5-(2-chloro-4,5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid 2-曱 oxycarbonyl methoxy-benzylamine, 5-(2- gas-4, 5-difluoro-benzoquinone Amino) -1Η- pyrazole-3-carboxylic acid 2-carboxy Yue group - Amides benzyl, 5- (4,5 - difluoro-2 - Yue yl - section stuffed amine) -111-0 ratio. Sodium-3 - oxo acid (6-decyloxy-pyridin-3-ylmethyl)-decylamine, 5-(2,4-dichloro-benzylamine)-1Η-pyrazole-3-carboxylic acid ( 6-methoxy-pyridin-3-ylmethyl)-decylamine, 5-(2-chloro-4,5-difluoro-benzylidenylamino)_1Η-πΛα sitting-3-carboxylic acid (3 , 5-dimethoxy-pyridin-4-ylindenyl)-nonylamine, 5-(4,5-difluoro-2-methyl-phenylnonylamino)-1Η-pyrazole-3- Carboxylic acid (2,4-dimercapto-oxazol-5-ylindenyl)-nonylamine, 5-(2,4-dichloro-5-fluoro-benzoinyl)-1Η-η ratio Oxazole-3-carboxylic acid (2,4-dimethyl-oxazol-5-ylindenyl)-nonylamine, 5-(2-chloro-4,5-difluoro-adolylamino)-111 -pyrazole-3-carboxylic acid (4-methoxycarbonyl-phenyl)-mercapto-decylamine, 477 (amendment) 318197 Patent No. 95,921,217 (July 10, 1998) 5 (2) _Chlorine~4,5~difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid (4-carboxy-styl)-methyl-decylamine, 4- {[5-(2 - gas-4,5-difluoro-anthracenylamino)_11{-pyrazole-3-carbonyl]-methyl-aminopurine-benzoic acid monosodium salt, 5 (2-chloro-4, 5-difluoro-benzhydrylamino)_ιη_0 ratio _3-rebel acid isopropyl-phenyl-stuffed , 5-(2-chloro-4, 5-difluoro-anthracenylamino)-1-indole-pyrazole-3-carboxylic acid (ethoxycarbonyl-methyl)-styl-decylamine, 5-(2 -Chloro-4,5-difluoro-phenylhydrazinoamino)_1Η_pyrazole_3 monocarboxylic acid (carboxy-indenyl)-styl-decylamine, 5-(2-vapor-4-fluoro- Benzomidine amino) 4Η_η-pyrazole_3_carboxylic acid benzalkonium, 5-(2,4-dioxa- amidinoamino)_1Η_pyrazole_3_carboxylic acid benzamide, 5 -(2-Ga-5-fluoro-phenylhydrazino)1Η-pyrazole-3-carboxylic acid benzamide, 5-(2- gas-4, 5-difluoro-benzhydrylamino group )_1Η_pyrazole_3-carboxylic acid nodal group _phenyl-decylamine, 5-(2-gas-4, 5-difluoro-benzoinylamino) &lt;Η-pyrazole-3-carboxylic acid (1-methyl-1-phenyl-ethyl)-decylamine, 5-(2-gas-4, 5-difluoro-benzhydrylamino) -ih_pyrazole-3-carboxylic acid [2-keto-2-(piperidine-i-ylindole-indole-ethylphenyl-decylamine, 5-(5-fluoro-2-indolyl)- Benzoylamino)_1H-pyrazole_3_carboxylic acid benzamide, 478 (amendment) 318197 Patent No. 95,921,217 (July 10, 1998) 5-(5-Chloro-2-indole) Benzo-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid benzamide, 5-(4-methoxy-2-indolyl-benzoguanidinoamine)-1Η-°bazole 3-carboxylic acid decylamine, 5-(4-chloro-2-indolyl-phenylhydrazino)-1Η-pyrazole-3-carboxylic acid benzamide, 5-(5-fluoro-2 -Methoxy-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid benzamide, 5-(5-chloro-2-methoxy-benzhydrylamino)-1Η-pyridyl Benzazole-3-carboxylic acid benzamide, 5-(2-chloro-4,5-difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid (2-ethoxy-ethyl )-Phenyl-bristamine' 5-(2-fluoro-5-methyl-phenylnonylamino)-1Η-pyrazole-3-carboxylic acid benzamide, 5-(5-gas-2- Fluoro-benzoguanidino)-1Η-η-pyrazole-3-carboxylic acid benzylamine, 5-(3- gas-2, 6-difluoro -benzoylamino)-1Η-indazole-3-carboxylic acid benzamide, 5-(2-vapor-3-fluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid Benzylamine, 5-(2-chloro-4, 5-difluoro-phenylhydrazino)-1Η-η-pyrazole-3-carboxylic acid ethylaminomethylmethylmethyl-phenyl-hydrazine Amine, 5-(2-chloro-4,5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylic acid isobutyl-phenyl-decylamine, 479 (amendment) 318197 1322688 Patent Application No. 95118217 (July 1st, 1998) 5-(2-chloro-4,5-difluoro-benzhydrylamino)-ih-pyrazole-3-carboxylic acid (2-oxime) Oxycarbonyl-ethyl)~phenyl-decylamine 5-(2-chloro-4,5-difluoro-benzhydrylamino)-ih-pyrazole-3-carboxylic acid (3-ethoxycarbonyl) -propyl)~phenyl-decylamine, 5-(2-chloro-4,5-difluoro-phenylhydrazinylamino)-ih-pyrazole-3-carboxylic acid (2-hydroxy-ethyl) -Phenyl-decylamine, 5-(2-chloro-4-, 5-difluoro-phenylhydrazino)-ih-pyrazole-3-carboxylic acid (3-regi-propyl)-phenyl - decylamine, 5-(2-amino-4-methoxy-phenylhydrazinylamino)-1 Η-° ratio 〇3-carboxylic acid benzylamine, 5-(2-radio-5 -methoxy-phenylhydrazinoamino)-1Η-β ratio.β sit-3-carboxylic acid Indoleamine, 5-(5-fluoro-2-yl-phenyl-phenylhydrazinyl)-1Η-β ratio 0-sodium-acid benzylamine, 5_(4-0ι-2 -tris-fluoroindolyl- Benzoylamino)-1Η-η ratio 0 _3_ benzyl benzyl hydrazide, 5-(5-fluoro-2-trifluoromethyl-benzoic acid amino)-1Η-° _3-carboxylic acid decylamine, 5-(2- gas-4, 5-difluoro-phenylhydrazino)-1Η-° azole-3-carboxylic acid (2-decyloxy-ethyl )-stupyl-decylamine, 5_(2,5-dimethyl- adenylamino)-1Η-pyrazole-3-carboxylic acid benzylic acid amine, 5-(2-gas-5-methyl -Benzylamino)-1Η-pyrazole-3-carboxylic acid benzylamine, 480 (amendment) 318197 Patent 95118217 patent application to Hong (July 1998 ι〇5-(2-gas ratio bite - 3-decylamino)-1Η-ηΛ*^-3-acid-lowering, 5-(4-gas-° ratio biting 2-amino group)-1H-d than 嗤-3- Rebel acid stagnation saddle, 5-(2,6-dichloro-° ratio biting 3-glycosylamino)-111-° ratio ° sitting -3 acid decylamine, 5-(2-gas- 4,5-difluoro-azinocarbylamino)_1H-pyrazole-3-carboxyindole butyl-(4-ethoxycarbonyl-phenyl)-decylamine, 5-(2-gas·~4, 5-dioxo-benzoylamino)-1Η-β is more than salino-3-dimmantyl-(4-carboxyl -phenyl)-decylamine, 5-(2-indolyl-pyridine-3-carbonylamino)-1Η-pyrazole-3-carboxylic acid benzylamine, 5-(2-chloro-6-indenyl- Pyridine-3-carbonylamino)-111-pyrazole-3-sweet benzamide, 5-(3-a-pyridyl-4-carbonylamino)-indole-pyrazole-3-carboxylic acid benzamide , 5-(2-chloro-4, 5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid butyl-(4-ethoxycarbonylmethyl-phenyl)- decylamine , 5-(2-Gas-4, 5-difluoro-benzoindolyl)-iH_pyrazole-3-carboxylic acid butyl-(4-carboxyindolyl-styl)monodecylamine, 5 -(2-chloro-4,5-difluoro-benzylidenylamino)-iH-pyrazole-3-carboxylic acid (4-oxocarbonyl-phenyl)-(2-decyloxy-ethyl - indoleamine, 5-(2- gas-4, 5-difluoro-phenylhydrazino)-iH-pyrazole-3-carboxylic acid (4-carboxy-phenyl)-(2-oxo) —-ethyl) amide, 481 (amendment) 318197 Patent No. 9511181·7 (July 1st, 1998) 5-(2-gas-4, 5-difluoro-benzoquinone Amino-based)-1Η-η-pyrazole-3-carboxylic acid (6-decyloxy-pyridin-3-ylindenyl)-nonylamine dihydrochloride, 5-(2-methyl-4, 5- Difluoro-benzoguanidino)-1Η-°biazole-3-carboxylic acid (6-decyloxy-pyridine -3-ylindenyl)-nonylamine dihydrochloride, 5-(2- gas-4,5-difluoro-phenylhydrazinoylamino)-1Η-pyrazole-3-carboxylic acid (thiazole-4 -yl-fluorenyl)-guanamine dihydrochloride, 5-(2- gas-4, 5-difluoro-benzhydrylamino)_1Η-π than wow-3-rebel 4-[2- (morpholin-4-yl)-ethylaminomercapto]-benzylguanamine dihydrochloride, 5-(2-chloro-4,5-difluoro-benzhydrylamino)-1Η- σ 〇 -3- -3- -3- 4- 4- 4- 4- 4- 4- 4- 4- 4- 4- 4- 4- 4- 4- 4- 4- 4- 4- 4- 4- 4- 4- 4- 4- 4- 4- 4- 4- 4- 4- 4- 4- 4- 4- 4- 4- 4- 4- 4- 4- 4- 4- 4- 4- 4- 4- 4- 4- 4- 4- 4- 4- 4- 4- 4- 4- 4- 4- 4- 4- 4- 4- 4- 4- 4- 4- 4- 4- 4- 4- 4- Difluoro-benzhydrylamino)-111-pyrazole-3-carbonyl]-amino}-methyl)-benzoguanidino]-acetic acid sodium salt, 3-[4-({[5- (2-Chloro-4,5-difluoro-phenylhydrazino)-111-pyrazole-3-carbonyl]-amino}-methyl)-benzimidamide]-propionic acid sodium salt, [5-(2-Chloro-4, 5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylic acid (3, 5-dimercapto-isoxazole-4-ylindenyl) - guanamine hydrochloride, [5-(2-chloro-4, 5-difluoro-benzylideneamino)-1Η_0 to 0--3-carboxylic acid (1,3,5-trimethyl -1Η-pyrazol-4-ylmethyl)-guanamine dihydrochloride, 5-(2-chloro-4,5-diqi-benzoquinoneamino)-1Η-σΛσ sitting-3-竣acid 3,5-Dimethyl-isoxazol-4-ylindenyl)-guanamine sulfonate, 5-(2_gas_4,5-di-gas-benzoquinoneamino)-1Η_π ratio. -3 -3 -(2-(morpholin-4-yl)-ethylaminomethylmercapto]-benzylamine diammonium 482 (Revised) 318197 Patent No. 95118217 (98) Month 10 9) Acidate, 5-(2-chloro-4, 5-difluoro-adolizylaminopyrazole-3-carboxylic acid 3-(morpholin-4-ylaminocarbamoyl)- Benzylamine dihydrochloride, 5-(2-chloro-4,5-difluoro-benzoylaminopyrazole-3-carboxylic acid {2-[2-(morpholin-4-yl)_ Ethylaminoindenyl]-pyridin-4-ylmethyl}•decalamine trihydrochloride, 5-(2-chloro-4,5-difluoro-benzhydrylamino)-1Η-η Bis-zolyl-3-carboxylic acid [2-(morpholin-4-ylaminoindolyl)-pyridin-4-ylmethyl]-decylamine trihydrochloride, 5-(2-gas-4, 5 -difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid (6-methoxy-pyridine-3-ylhydrazinyl)- amidoxime sulfonate, 5-(2-chloro -4, 5-difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid (6-decyloxy-pyridin-3-ylindenyl)-decylamine hemisulfate, 5-( 2-Ga-4, 5-difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-carboxylic acid (3, 5-dimethoxy-pyridin-4-ylmethyl)-decylamine Hydrochloride, 5-(2-chloro-4, 5-difluoro-phenylhydrazino)- 1H-pyrazole-3- Acid (4-aminomethyl-pyridin-2-ylindenyl)-decylamine trihydrochloride, 5-(2- gas-4,5-di-benzoylamino)-1Η-0嗤-3--lower acid (6-chlorobite-3-ylindenyl)_bristamine acid salt, 5_(2- gas-4,5-difluoro-benzhydrylamino group -3 -slow acid (6_chloro_0 to bite_3_ylindenyl)_bristamine dibasic acid salt 5--2-(2-a-4,5-di-phenyl-phenylamino)-111 -° 嗤-3-teric acid (2,4-dimethyl-pyridin-3-ylindenyl)-decylamine hydrochloride, 5_(2- gas-4,5-difluoro-benzamide Amino)-1Η-π ratio 0 sitting-3-rebellion 483 (amendment) 318197 Patent No. 95118217 (July 1 9 9 ? 〇 〇 〇 咬 咬 咬 咬 咬 基 基) Hydrochloride, 5-(2- gas-4, 5-difluoro-benzoylamino)-ΐΗ-π ratio. Sit _3 monodecanoic acid (6-decyloxy-pyridylmethyl)- Propyl-guanamine dihydrochloride, 5_(2_chloro-4, 5-difluoro-benzoinylamino)-1{]-〇 ratio ° sitting-3-decanoic acid [6-(piperidine) -buki)-pyridin-3-ylindenyl]]-nonylamine dihydrochloride, 5-(2-chloro-4,5-fluoro-arachnidylamino)-ΐΗ-° -3-decanoic acid [6-(morpholin-4-yl)-pyridin-3-ylindenyl]]- Indoleamine dihydrochloride, 5_(2-chloro-4,5--fluoro-benzoinylamino)-111-indole quinone -3-butylic acid (3,5-diox-° ratio唆_4-ylmethyl)-indoleamine hydrochloride, 5-(2-chloro-4,5*··-fluoro-benzoylamino)-111-indole ratio (6-Didecylamino _σ-pyridyl 3-ylindenyl)-nonylamine dihydrochloride, 5-(2-chloro-4,5-difluoro-benzoinyl)-111 - 〇 ratio ° sitting -3-acid (6 - dimercaptoamine than dimethyl group) - propyl-guanamine dihydrochloride, 5- (2-chloro-4, 5-difluoro-benzene Hydrazinyl)-1Η-pyrazole-3-buffer acid (6-diethylamino-pyridin-3-ylindenyl)-decylamine dihydrochloride, 5-(2-chloro-4, 5-difluoro-benzoylamino)-1{1-° ratio °-3-oxo acid (6-chloro-2-dimethylamino-indole-3-ylmethyl)-醯Amine dihydrochloride, 5-(2_chloro-4,5-difluoro-benzoylamino)-1Η-η than sal-3-hydroxy acid (4-[1,2,3]thiadi Zyzol-4-yl-benzyl)-indolyl hydrochloride, 5-(2-chloro-5-difluoro-benzhydrylamino)-1Η-π ratio 0 sitting-3-tagacid (4-A -thiazol-5-ylindenyl)-indolamine hydrochloride, 5-(2-chloro-4-, difluoro-benzoinylamino)-1Η- π ratio 0 sitting -3- slow 484 (amendment) 318197 1322688 Patent No. 95118217 (July 10, 1998) Acid (2, 4-dimercapto-thiazol-5-ylmethyl)-guanamine Hydrochloride, 5-(2-chloro-4,5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylic acid [6-(4- via base-bit-1)- π 咬 -3- 曱 曱 ] ] ] ] ] ] ] 酿 酿 酿 酿 酿 酿 酿 酿 酿 酿 酿 酿 酿 酿 酿 酿 酿 酿 酿 酿 酿 酿 酿 酿-methyl-pyridin-2-ylindoleamine dihydrochloride, 5-(2- gas-4,5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid quinoline 5-5-decylamine dihydrochloride, 5-(2-chloro-4, 5-difluoro-benzylidenylamino)-1 Η-pyrazole-3-carboxylic acid quinolin-8-yl decylamine Dihydrochloride, 5-(2-chloro-4, 5-difluoro-benzylidenylamino)-1Η-pyrazole-3-carboxylic acid isoquinolin-5-ylguanamine dihydrochloride, 5-(2-chloro-4,5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylic acid [6-(4-mercapto-peptidyl)-pyridine-3- Methyl]-nonylamine dihydrochloride, 5-(2-chloro-4,5-difluoro-benzhydrylamino)-111-pyrazole-3-carboxylic acid [6-(4-di) Mercaptoamine-precipitate_1_yl)_π ratio _3-ylmethyl]-bristamine dihydrochloride, 5-(2-gas-4, 5-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid [6-(pyrrolidin-1-yl)-pyridin-3-ylmethyl]-nonylamine dihydrochloride, 5-(2-chloro-4,5-difluoro-phenylhydrazinoamino)-1Η-η-pyrazole-3-carboxylic acid (pyroxy-2-ylmethyl)-guanamine dihydrochloride, 5-(2-Chloro-4,5-difluoro-benzoindolyl)-1Η-pyrazole-3-carboxylic acid [6_(thioxan-4-yl)_.唆 3- 3- 3- 3- 3- 3- 3- 485 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 318 - 笨 醯 醯 胺 ) ) 吡 吡 吡 吡 吡 吡 吡 吡 吡 6 6 6 6 6 6 6 6 6 6 6 6 6 6 6 6 6 6 6 6 6 6 6 6 6 6 6 6 6 6 6 6 Indoleamine dihydrochloride, 5-(2-chloro-4,5-difluoro-phenylhydrazinoyl)-1-indole-pyrazole_3-sodium sulphate-based alkyl-branched amine, 5- (2, 4-dioxa-5-fluorophenylindenylamino)-1-indole-pyrazole-3-enic acid (4-aminomethylindenyl-phenyl)-methyl-decylamine, 5-( 2,4-Dichloro-5-fluoro-phenylhydrazinoamino)_1Η_pyrazole_3_decanoic acid methyl-(4-methylaminomethylindenyl-phenyl)-decylamine, 5- (2,4-dichloro-5-fluoro-benzhydrylamino)_1{1_pyrazole-3-oxanoic acid (4-dimethylaminodecyl-phenylmethyl-decylamine, 5-(2-chloro-4, 5-difluoro-phenylhydrazinyl)- ιη-pyrazole-3-carboxylic acid (4-methylsulfonylaminocarbonyl-phenylmethyl-decylamine, 5-(2-chloro-4,5-difluoro-benzylidenylamino)_ιη-pyrazole-3-carboxylic acid (4-oxasulfonylaminocarbonyl-phenyl)-methyl-decylamine Sodium salt, 5-(2-chloro-4, 5 -difluoro-phenylhydrazinoamino)-1Η-pyrazole-3-3⁄4 acid (4-cyano-phenyl)-methyl-decylamine, 5-(2-chloro-4,5-difluoro -benzimidylamino)-111-0biazole-3-carboxylic acid methyl-[4-(4Η-[1,2,4]triazol-3-yl)-phenyl]-nonylamine salt Acid salt, 5-(4-azido-2-ethane-5-fluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylic acid (4-cyano-phenyl)-methyl-decylamine , 5-(4-azido_2-chloro-5-fluoro-benzamide)- 1H-pyrazole-3-carboxylic acid methyl-[4-(1Η-tetrazol-5-yl)- Phenyl]-nonylamine, 486 • (Revised) 3] 8] 97 1322688 Patent Application No. 95118217 (July 1, 2017) ' 5-(2-chloro-4, 5-difluoro- Benzoylamino)-1Η-βΛο sit-3-acid-[4-(Ν-hydroxyaminoiminoindolyl)-phenyl]-indolyl-decylamine, 5-(2-chloro- 4, 5-Difluoro-benzylidenylamino)-indole-pyrazole-3-carbamic acid-yl-[4-(5-keto-2,5-dihydro-[1,2, 4] °oxadiazol-3-yl)-phenyl]-nonylamine, 5-(2-chloro-4,5-difluoro-benzoinylamino)-ΐΗ-° than salivary-3-acidic { 4-[(2,2-Dimercapto-propenyloxy)-indolyloxycarbonyl]-phenylindoleyl-decylamine, ^ 5-(2-chloro-4, 5-difluoro-phenylhydrazine) Mercaptoamine -ιη-〇 唾 唾 -3- -3- 4- Ν 曱 曱 曱 曱 4- 4- 4- -3- -3- -3- -3- -3- -3- -3- -3- -3- -3- -3- -3- -3- -3- -3- -3- -3- -3- -3- -3- -3- -3- -3- -3- -3- 唾 -3- 唾 唾-difluoro-benzhydrylamino)-1Η-pyrazole-3-carboxylate-[4-(5-thioketo-4, 5-dihydro-[1,2, 4]oxadi Zyridin-3-yl)-phenyl]-bristamine, 5-(2-chloro-4,5-difluoro-benzoindolyl)-indolyl-pyrazole-3-derivative methyl (5- Keto 5-dohydro-[1,2,4]oxadiazol-3-yl)-phenyl]-nonylamine, 5-(2- gas-4,5-difluoro-benzoinylamino _1H_pyrazole-3-carboxylic acid {4-[1-(cyclohexyloxy-carbonyloxy)-ethoxycarbonyl]-phenyl}monomethyl-bristamine, 5 (2 chaos - 4,5_ - rat - benzoylamino group than 0 sitting --3-acid (4-ethoxycarbonyl-thiazol-2-yl)-ethyl-decylamine, 5 - (2-gas-4, 5-difluoro -benzoylamino)_1H_pyrazole_3_carboxylic acid 2_methanesulfonylamino-benzamide, 487 (amendment) 318197 1322688 Patent Application No. 95118217 (July 1, 9) 〇日)' 5-(2-Gas-4, 5-difluoro-benzhydrylamino)-lH-pyrazole-3-carbamic acid 2-Ethylamino-benzamide, 5-(2 -chloro-4, 5-difluoro-benzhydrylamino)-lH-pyrazole-3-acid 2_(-曱Amino-methyleneamino)-tuberamine hydrochloride, 5-(2-chloro-4,5-difluoro-benzhydrylamino)-1Η-pyrazole-3-buffer acid 3- (dimethylamino-ylideneamino)-benzylguanamine hydrochloride, 5-(2-chloro-4, 5-difluoro-benzylidenylamino)-1Η-pyrazole-3-carboxylic acid 4-(dimethylamino-methyleneamino)-benzylguanamine Hydrochloride, 5-(2- gas-4,5-dioxa-phenylhydrazino)-111-° than 〇3--3-acid 2-[1-(didecylamino)ethyleneamine 5-benzylamine dihydrochloride, 5-(2-gas-4, 5-difluoro-benzoquinoneamino)-1Η-pyria-3-acid 3-[1-(dioxin Aminoamino)ethylamino]-benzylamine dihydrochloride, 5-(2-chloro-4,5-difluoro-phenylhydrazino)-1Η_ο than sal-3-ret-4- [1-(Didecylamino)ethylamino]-benzylguanamine dihydrochloride, 5-(2-chloro·_4,5-difluoro-phenylhydrazino)-1Η-η Bis-(3-ethylamino-methyleneamino)-benzylguanamine dihydrochloride, 5-(2-chloro-4,5-difluoro-benzofuranylamine Base) Η Η-η than saliva 3 - retinoic acid 3-(diethylamino-methyleneamino)-benzylguanamine dihydrochloride, 5-(2-chloro-4,5-difluoro- Benzoylamino)-1Η-πϋ〇^-3-carbamic acid 4-(diethylamino-methyleneamino)-benzylguanamine dihydrochloride, 5-(2- gas-4 , 5-difluoro-benzoquinone-based amine)-1Η-° ratio -3-carboxylic acid 2-imine ethylamino-benzylguanamine dihydrochloride, 5-(2-chloro-4, 5-difluoro-phenylhydrazinoamino)-1 Η-pyrazole-3-carboxylic acid 3-imine ethylamino-benzylguanamine Hydrochloride, 488 (amendment) 318197 1322688 Patent Application No. 95118217 (July 1, 1998) 5-(2-Gas-4, 5-difluoro-benzoylaminopyrazole-3 -carboxylic acid 4-imine ethylamino-barred amine dihydrochloride, 5-(2-disorganized-4,5--murine-benzoquinoneamino)_1H-1* than 0 sitting-rebel Acid 4-cyano-benzylguanamine, 5-(2-chloro-4, 5-difluoro-benzhydrylamino) 4η-pyrazole-3-carboxylic acid 3-[(2-fluoro-imine) Benzyl)-amino]-benzylamine hydroiodide, 5-(2-chloro-4,5-difluoro-benzhydrylamino)_1H-pyrazole-3-carboxylic acid 4-[ (2-fluoro-iminobenzyl)-amino]-benzylamine hydroiodide, 5-(2-gas-4,5-difluoro-adenylamino)-ih-pyrazole 3-carboxylic acid 3-(3?3-indolyl-yl)-tubular amine ' 5-(2- gas-4, 5-difluoro-phenylhydrazino)-1H-pyrazole 3-carboxylic acid 4-(3,3-dimercapto-ureido)-benzylamine, 5-(2-gas-4,5-difluoro-benzhydrylamino)-^-pyrazole 3-carboxylic acid 2-(toluene-4-sulfonylamino)-benzylguanamine, 5-(2-gas-4, 5-difluoro-benzhydrylamino)-iH_pyrazole_3 2-carboxylic acid 2-amino-6-fluoro-benzylamine hydrochloride, 5-(2-chloro-4,5-difluoro-phenylhydrazino)-11 ] - β 比哇-3 - decanoic acid 2-amino-4, 5-difluoro-benzylguanamine hydrochloride, 5-(2-chloro-4, 5-difluoro-phenylhydrazino) 1Η_pyrazole-3-carboxylic acid (hydroindol-1-yl)-decylamine, 5-(2-gas-4, 5-difluoro-benzhydrylamino)_1Η_pyrazole_3_carboxylate Acid (hydroquinone-2-yl)-nonylamine, 5-(2- gas-4, 5-difluoro-phenylhydrazinoamino)_1Η-pyrazole-3-carboxylate (4Η-quinazoline- 3-yl)-nonylamine, (amendment) 318197 489 1322688 Patent Application No. 95118217 (July, 1998) 5~(2~gas-4, 5-difluoro-benzhydrylamino)- 1Η-pyrazole-3-hypoacid (4H-quinazoline-3-yl)~nonylamine dihydrochloride, 5~(2-chloro-4, 5-difluoro-benzhydrylamino)- 1Η-pyrazole-3-decanoic acid (7-fluoro-4H-quinazolin-3-yl)-guanamine dihydrochloride, 5~(2- gas-4, 5-difluoro-phenylhydrazine Amino)-lH-°biazole-3-decanoic acid (6-fluoro-4H-quinazolin-3-yl)-guanamine hydrochloride, 5~(2- gas-4, 5-difluoro- Phenylhydrazino)-1H-d is more than saliva-3-acid (2-ethoxy-2-indolyl-1,4-dihydro-2H-quinazolin-3-yl)-guanamine , 5-(2-Gas-4, 5-difluoro-phenylhydrazino)-1Η-pyrazole-3-carboxylic acid (2-cyano-n ratio Pyridin-4-ylmethyl)-decylamine, 5-(2-chloro-4, 5-difluoro-benzylidenylamino)-1Η-pyrazole-3-carboxylic acid [2-(Ν-hydroxyl) Aminoimine fluorenyl)-pyridin-4-ylindenyl]-nonylamine, 5-(2- gas-4, 5-difluoro-phenylhydrazinoyl)-1Η-pyrazole-3-carboxylate Acid [2-(5-keto-4,5-dihydro-[1,2,4] °oxadiazol-3-yl)-° ratio biting 4-ylmethyl]-bristamine, 4- {[5-(4, 5-Difluoro-2-methyl-benzoguanidino)-1Η-pyrazole_3-peptidyl]-methyl-amino}-benzoic acid sodium salt, 5- 4, 5-Difluoro-2-indolyl-benzhydrylamino)-1Η-. Butyrazole-3-acid sulfhydryl-[4-(111-tetramethylene-5-yl)-phenyl]-bristamine, 5-(2,4-dichloro-benzoguanamine)-1Η -pyrazole-3-carboxylic acid (pyridin-3-ylindenyl)-decylamine, 5-(2,4-dichloro-5-fluoro-benzoguanidino)-1Η-pyrazole-3-carboxylate Acid (pyridin-3-ylmethyl)-decylamine, 490 (amendment) 318197 1322688 Patent Application No. 95118217 (July 10, 1998) 5-(2,6-di-gas-5-fluoro-pyridine 3-carbonylamino)-1Η-pyrazole-3 -hyaloacid (° ratio -3-ylmercapto)-decylamine, 5-[(3-chloro-benzo[1)]thiophene-2- Carbonyl)-amino]-111-pyrazole-3-carboxylic acid (pyridin-3-ylmethyl)-decylamine, 5-[(3-chloro-porphin-2-carboyl)-amino]- 1Η-° ratio 嗤3~~-acid (pyridin-3-ylmethyl)-decylamine, 5-phenylhydrazinoamino-1H-pyrazole-3-carboxylic acid (pyridin-3-ylmethyl) - decylamine, 5-phenylethylamino-1H-pyrazole-3-carboxylic acid (pyridin-3-ylmethyl)-nonylamine, 5-(2-methyl-4, 5-difluoro- Benzylguanidino)-1Η-η-pyrazole-3-carboxylic acid (pyridin-3-ylmethyl)-guanamine dihydrochloride, 5-(2-amino-4, 5-difluoro- Benzylamino)-1Η-pyrazole-3-carboxylic acid (pyridin-3-ylindenyl)-decylamine , 5-(4,5-difluoro-2-oxo-anhydro-amino-benzoylamino)-1Η-pyrazole-3-carboxylic acid (pyridin-3-ylindenyl)-decylamine, 5-(2-Ethylamino-4, 5-difluoro-benzamide)-1Η-pyrazole-3-carboxylic acid (pyridyl-3-ylmethyl)-decylamine, 5-[ (3, 4, 5-trichloro-thiophene-2-carbonyl)-amino group: Ι_1Η-pyrazole-3-carboxylic acid (pyridin-3-ylmethyl)-decylamine, 5-(4, 5-di Fluoro-2-methyl-benzylidenylamino)-1Η-pyrazole-3-carboxylic acid (2-cyano-pyridin-4-ylmethyl)-decylamine, 5-(4, 5-di Fluoro-2-methyl-phenylhydrazinoamino)-lH-η-pyrazole-3-carboxylic acid [2-(1Η-tetrazol-5-yl)-pyridin-4-ylindenyl]-decylamine And 491 (amendment) 318197 1322688 111-°bizozol-3, 5-dicarboxylic acid 3-benzyl aryl)-decylamine]. Patent Application No. 95118217 (July 10, 2008) Amine 5-[(2,4-dichloro-benzene 36-therapeutic or prophylactic agent for insulin resistance to diabetic neuropathy) , diabetic nephropathy, diabetic retinopathy, cataract, hypercholesterolemia, hypertension, hyperinsulinemia, hyperlipidemia, arteriosclerosis, tissue ischemia, money infarction, obesity, or bacterial fungi, parasites Or a therapeutic or prophylactic agent for viral infection, which comprises, as an active ingredient, a bismuth compound or a pharmaceutically acceptable salt as claimed in any of claims 21 to 35 of the patent. (Revised) 318197 492