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    • 9. 发明授权
    • Pyrazolothiazole compound
    • 吡唑并噻唑化合物
    • US08530504B2
    • 2013-09-10
    • US12900026
    • 2010-10-07
    • Kogyoku ShinTaro TerauchiYoshinori TakahashiMinako HashizumeKunitoshi TakedaKodo ShikataAkira Inomata
    • Kogyoku ShinTaro TerauchiYoshinori TakahashiMinako HashizumeKunitoshi TakedaKodo ShikataAkira Inomata
    • A61K31/429A61P25/24
    • C07D513/04
    • A compound represented by the formula (I) or pharmacologically acceptable salt thereof exhibits an excellent CRF receptor antagonism wherein X is a nitrogen atom or CH; R1 is -A11-A12; A11 is a single bond or a C1-6 alkylene group; A12 is a hydrogen atom, a C1-6 alkyl group or a C3-6 cycloalkyl group, etc.; R2 is -A21-A22; A21 is a single bond or a C1-6 alkylene group; A22 is a hydrogen atom, a C1-6 alkyl group, a C3-6 cycloalkyl group, a non-aromatic heterocyclic group, or a heteroaryl group, etc.; R3 is a C1-6 alkyl group, a C3-6 cycloalkyl group, a C1-6 alkoxy group, a C3-6 cycloalkoxy C1-6 alkyl group, di-C1-6 alkyl amino group, a halogen atom, a cyano group, a formyl group, or a carboxyl group, etc; R4 is a hydrogen atom or a C1-6 alkoxy group; R5 is a halogen atom, a C1-6 alkyl group, or a C1-6 alkoxy group; R6 is a hydrogen atom, a C1-6 alkyl group, a C1-6 alkoxy group, a C1-6 alkylthio group, or a C1-6 alkyl sulfinyl group etc.; and R7 is a C1-6 alkyl group, a C1-6 alkoxy group, or a C1-6 alkylthio group.
    • 由式(I)表示的化合物或其药理学上可接受的盐表现出优异的CRF受体拮抗作用,其中X为氮原子或CH; R1为-A11-A12; A11是单键或C1-6亚烷基; A12是氢原子,C1-6烷基或C3-6环烷基等; R2为-A21-A22; A21是单键或C1-6亚烷基; A22为氢原子,C1-6烷基,C3-6环烷基,非芳族杂环基或杂芳基等; R3是C1-6烷基,C3-6环烷基,C1-6烷氧基,C3-6环烷氧基C1-6烷基,二C1-6烷基氨基,卤素原子,氰基 ,甲酰基或羧基等; R4是氢原子或C1-6烷氧基; R5是卤素原子,C1-6烷基或C1-6烷氧基; R6是氢原子,C1-6烷基,C1-6烷氧基,C1-6烷硫基或C1-6烷基亚磺酰基等; 且R 7为C 1-6烷基,C 1-6烷氧基或C 1-6烷硫基。