Pyrazolothiazole compound
    9.
    发明授权
    Pyrazolothiazole compound 失效
    吡唑并噻唑化合物

    公开(公告)号:US08530504B2

    公开(公告)日:2013-09-10

    申请号:US12900026

    申请日:2010-10-07

    IPC分类号: A61K31/429 A61P25/24

    CPC分类号: C07D513/04

    摘要: 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.

    摘要翻译: 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。

    Imidazo[1,2-b]pyridazine compound
    10.
    发明授权
    Imidazo[1,2-b]pyridazine compound 失效
    咪唑并[1,2-b]哒嗪化合物

    公开(公告)号:US07772249B2

    公开(公告)日:2010-08-10

    申请号:US12397132

    申请日:2009-03-03

    IPC分类号: A61K31/44

    CPC分类号: C07D471/04 C07D487/04

    摘要: The present invention provides a novel compound having an excellent corticotrophin-releasing-factor receptor antagonistic activity. That is, it provides a compound represented by the following formula or a salt thereof. Wherein R1 denotes a hydrogen atom, a C1-6 alkyl group, a C1-6 alkoxy group and the like; R2 denotes a halogen atom, a cyano group, a nitro group, a C1-10 alkyl group, a C2-10 alkenyl group, C2-10 alkynyl group and the like; R3 denotes a C6-14 aromatic hydrocarbon cyclic group or a 5- to 14-membered aromatic heterocyclic group, each of which may have a substituent; and X, Y and X are independent of each other and each denotes N or CR4 (wherein R4 denotes a hydrogen atom, a halogen atom, a cyano group, a nitro group, an optionally halogenated C1-6 alkyl group and the like) and, in this case, at least two of X, Y and Z denote CR4.

    摘要翻译: 本发明提供具有优异的促肾上腺皮质激素释放因子受体拮抗活性的新型化合物。 也就是说,它提供由下式表示的化合物或其盐。 其中R1表示氢原子,C1-6烷基,C1-6烷氧基等; R2表示卤素原子,氰基,硝基,C1-10烷基,C2-10烯基,C2-10炔基等; R3表示可以具有取代基的C 6-14芳族烃环状基团或5〜14元芳香族杂环基团。 X,Y和X彼此独立地表示N或CR4(其中R4表示氢原子,卤素原子,氰基,硝基,任意卤代的C 1-6烷基等)和 在这种情况下,X,Y和Z中的至少两个表示CR 4。