首页> 外国专利> New aminoindazole derivatives are kinase inhibitors, useful in the treatment of neurodegenerative diseases, obesity, metabolic disorders, diabetes, hypertension, polycystic ovarian syndrome, cancers and other disorders

New aminoindazole derivatives are kinase inhibitors, useful in the treatment of neurodegenerative diseases, obesity, metabolic disorders, diabetes, hypertension, polycystic ovarian syndrome, cancers and other disorders

机译：新的氨基吲唑衍生物是激酶抑制剂，可用于治疗神经退行性疾病，肥胖，代谢紊乱，糖尿病，高血压，多囊卵巢综合征，癌症和其他疾病

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摘要

Aminoindazole derivatives (I), their racemates, enantiomers, diastereoisomers, mixtures, tautomers and their salts are new. Aminoindazole derivatives (I), their racemates, enantiomers, diastereoisomers, mixtures, tautomers and their salts are new. R3 = H, 1-6C alkyl, aryl, aryl alkyl, heteroaryl, heteroaryl alkyl, aryl or heteroaryl fused to 1-10C cycloalkyl, heterocycle, heterocycloalkyl, cycloalkyl, adamantyl, polycycloalkyl, alkenyl, alkynyl, CONR1R2, COOR1, SO2R1, or C(=NH)NR1 (all optionally substituted by one or more of halogen, CN, NO2, NH2, OH, OR1, COOH, COOR1, -O-CO-R1, NR1R2, NHCO-R1, CO-NR1R2, SR1, SO-R1, SO2R1, NHSO2-R1, SO2NR1R2, CS-NR1R2, NH-CS-R1, -O-SO2-R1, -SO2-O-R1, aryl, heteroaryl, formyl, oxo, trifluoromethyl, trifluoromethyl sulfanyl, trifluoromethoxy, and 1-6C alkyl); R5, R6, and R7 = halogen, CN, NO2, NH2, OH, OR8, COOH, COOR8, -O-CO-R8, NR8R9, NHCO-R8, CO-NR8R9, NH-CS-R8, CS-NR8R9, SR8, SO-R8, SO2R8, NHSO2-R8, SO2NR8R9, -O-SO2-R8, -SO2-O-R8, CF3, CF3O-, 1-6C alkyl or alkoxy, aryl, aryl alkyl, heteroaryl, heteroaryl alkyl, heterocycle, cycloalkyl, alkenyl, alkynyl, adamantyl, polycycloalkyl (all optionally substituted by one or more of halogen, CN, NO2, NH2, OH, OR10, COOH, COOR10, -O-CO-R10, NR10R11, NHCO-R10, CO-NR10R11, NH-CS-R10, -CS-NR10R11, SR10, SO-R10, SO2R10, NHSO2R10, SO2NR10R11, -O-SO2-R10, -SO2-O-R10, aryl, heteroaryl, formyl, oxo, CF3, CF3O, and 1-6C alkyl); R1, R2, R8, R9, R10, and R11 = H, 1-6C alkyl, aryl, alkenyl, alkynyl, heteroaryl, cycloalkyl, or heterocycloalkyl (all optionally substituted by 1 or more halogen, alkyl, alkoxy, CN, NO2, NH2, OH, COOH, COOalkyl, CONH2, formyl, oxo, CF3, and CF3O); and provided that when R3 is 5-imidazolyl, 5-oxazolyl, 5-thiazolyl, 3-pyridinyl, or 5-pyrimidinyl, optionally substituted by halogen or alkyl, then at least one of R5, R6, and R7 is CN, NO2, NH2, OH, -O-CO-R8, NHCO-R8, NH-CS-R8, CS-NR8R9, NHSO2-R8, -O-SO2-R8, -SO2-O-R8, CF3, CF3O, alkoxy, aryl, arylalkyl, heteroaryl, heteroaryl alkyl, heterocycle, cycloalkyl, alkenyl, alkynyl, adamantyl, or polycycloalkyl (all optionally substituted by halogen, CN, NO2, NH2, OH, OR10, COOH, COOR10, -O-CO-R10, NR10R11, NHCO-R10, CO-NR10R11, NH-CS-R10, -CS-NR10R11, SR10, SO-R10, SO2R10, NHSO2R10, SO2NR10R11, -O-SO2-R10, -SO2-O-R10, aryl, heteroaryl, formyl, oxo, CF3, CF3O, and 1-6C alkyl). Independent claims are also included for the following: (1) preparation of (I); and (2) 6,7-difluoro-1H-indazole-3-amine. N-(6,7-difluoro-1H-indazol-3-yl)butanamide, N-(6,7-difluoro-1-((2-(trimethylsilyl)ethoxy)methyl)-1H-indazol-3-yl)butanamide, N-(5-bromo-6,7-difluoro-1-((2-(trimethylsilyl)ethoxy)methyl)-1H-indazol-3-yl)butanamide, N-(6,7-difluoro-5-phenyl-1-((2-(trimethylsilyl)ethoxy)methyl)-1H-indazol-3-yl)butanamide, 6,7-difluoro-5-phenyl-1-((2-(trimethylsilyl)ethoxy)methyl)-1H-indazole-3-amine and N-(6,7-difluoro-5-phenyl-1-((2-(trimethylsilyl)ethoxy)methyl)-1H-indazol-3-yl)-N'-phenylurea as new intermediates in the preparation of (I).

机译：氨基吲唑衍生物（I），其外消旋物，对映异构体，非对映异构体，混合物，互变异构体及其盐是新的。氨基吲唑衍生物（I），其外消旋物，对映异构体，非对映异构体，混合物，互变异构体及其盐是新的。 R3 =与1-10C环烷基，杂环，杂环烷基，环烷基，金刚烷基，多环烷基，烯基，炔基，CONR1R2，COOR1，SO2R1或-稠合的H，1-6C烷基，芳基，芳基烷基，杂芳基，杂芳基烷基，芳基或杂芳基C（= NH）NR1（全部可选地被一个或多个卤素，CN，NO2，NH2，OH，OR1，COOH，COOR1，-O-CO-R1，NR1R2，NHCO-R1，CO-NR1R2，SR1， SO-R1，SO2R1，NHSO2-R1，SO2NR1R2，CS-NR1R2，NH-CS-R1，-O-SO2-R1，-SO2-O-R1，芳基，杂芳基，甲酰基，氧代，三氟甲基，三氟甲基硫烷基，三氟甲氧基和1-6C烷基）; R5，R6和R7 =卤素，CN，NO2，NH2，OH，OR8，COOH，COOR8，-O-CO-R8，NR8R9，NHCO-R8，CO-NR8R9，NH-CS-R8，CS-NR8R9， SR8，SO-R8，SO2R8，NHSO2-R8，SO2NR8R9，-O-SO2-R8，-SO2-O-R8，CF3，CF3O-，1-6C烷基或烷氧基，芳基，芳基烷基，杂芳基，杂芳基烷基，杂环，环烷基，烯基，炔基，金刚烷基，多环烷基（全部可选地被卤素，CN，NO2，NH2，OH，OR10，COOH，COOR10，-O-CO-R10，NR10R11，NHCO-R10，CO中的一个或多个取代-NR10R11，NH-CS-R10，-CS-NR10R11，SR10，SO-R10，SO2R10，NHSO2R10，SO2NR10R11，-O-SO2-R10，-SO2-O-R10，芳基，杂芳基，甲酰基，氧代，CF3， CF 3 O和1-6C烷基）; R1，R2，R8，R9，R10和R11 = H，1-6C烷基，芳基，烯基，炔基，杂芳基，环烷基或杂环烷基（均可选被1个或多个卤素，烷基，烷氧基，CN，NO2取代， NH2，OH，COOH，COO烷基，CONH2，甲酰基，氧代，CF3和CF3O）;并且当R3为5-咪唑基，5-恶唑基，5-噻唑基，3-吡啶基或5-嘧啶基并任选地被卤素或烷基取代时，则R5，R6和R7中的至少一个为CN，NO2， NH2，OH，-O-CO-R8，NHCO-R8，NH-CS-R8，CS-NR8R9，NHSO2-R8，-O-SO2-R8，-SO2-O-R8，CF3，CF3O，烷氧基，芳基，芳基烷基，杂芳基，杂芳基烷基，杂环基，环烷基，烯基，炔基，金刚烷基或多环烷基（全部可选地被卤素，CN，NO2，NH2，OH，OR10，COOH，COOR10，-O-CO-R10，NR10R11， NHCO-R10，CO-NR10R11，NH-CS-R10，-CS-NR10R11，SR10，SO-R10，SO2R10，NHSO2R10，SO2NR10R11，-O-SO2-R10，-SO2-O-R10，芳基，杂芳基，甲酰基，氧代，CF3，CF3O和1-6C烷基）。还包括以下方面的独立权利要求：（1）（I）的制备; （2）6，7-二氟-1H-吲唑-3-胺。 N-（6,7-二氟-1H-吲唑-3-基）丁酰胺，N-（6,7-二氟-1-（（2-（三甲基甲硅烷基）乙氧基）甲基）-1H-吲唑-3-基）丁酰胺，N-（5-溴-6,7-二氟-1-（（2-（三甲基甲硅烷基）乙氧基）甲基）-1H-吲唑-3-基）丁酰胺，N-（6,7-二氟-5-苯基-1-（（（2-（三甲基甲硅烷基）乙氧基）甲基）-1H-吲唑-3-基）丁酰胺，6,7-二氟-5-苯基-1-（（2-（三甲基甲硅烷基）乙氧基）甲基）-作为新的1H-吲唑-3-胺和N-（6,7-二氟-5-苯基-1-（（（2-（三甲基甲硅烷基）乙氧基）甲基）-1H-吲唑-3-基）-N'-苯基脲制备（I）的中间体。

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公开/公告号FR2848554A1

专利类型
公开/公告日2004-06-18

原文格式PDF
申请/专利权人 AVENTIS PHARMA SA;
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申请/专利号FR20020015720
发明设计人
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申请日2002-12-12
分类号C07D231/56;A61K31/416;A61P25/00;
国家 FR
入库时间 2022-08-21 22:39:20

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