3-phenylpyrazolo[5,1-b]thiazole compounds
    1.
    发明授权
    3-phenylpyrazolo[5,1-b]thiazole compounds 有权
    3-苯基吡唑并[5,1-b]噻唑化合物

    公开(公告)号:US08431603B2

    公开(公告)日:2013-04-30

    申请号:US12421182

    申请日:2009-04-09

    IPC分类号: A61K31/4439 C07D513/02

    CPC分类号: C07D513/04

    摘要: A compound represented by the following formula (I), or salt thereof exhibits excellent CRF receptor antagonism, and sufficient pharmacological activity, safety and pharmacokinetic properties as a drug. wherein R1 represents the formula -A11-A12; R2 represents tetrahydrofurylmethyl, tetrahydropyranylmethyl or tetrahydropyranyl; A11 represents a single bond, methylene or 1,2-ethylene; A12 represents C1-6 alkyl, C3-6 cycloalkyl or C3-6 cycloalkyl having methyl; R3 represents methoxy, cyano, cyclobutyloxymethyl, methoxymethyl or ethoxymethyl; and R4 represents methoxy or chlorine.

    摘要翻译: 由下式(I)表示的化合物或其盐表现出优异的CRF受体拮抗作用,作为药物具有充分的药理活性,安全性和药代动力学性质。 其中R1表示式-A11-A12; R2表示四氢呋喃基甲基,四氢吡喃基甲基或四氢吡喃基; A11表示单键,亚甲基或1,2-亚乙基; A12表示C1-6烷基,C3-6环烷基或具有甲基的C3-6环烷基; R3表示甲氧基,氰基,环丁氧基甲基,甲氧基甲基或乙氧基甲基; R4表示甲氧基或氯。

    3-PHENYLPYRAZOLO[5,1-b]THIAZOLE COMPOUNDS
    2.
    发明申请
    3-PHENYLPYRAZOLO[5,1-b]THIAZOLE COMPOUNDS 有权
    3-苯基吡唑并[5,1-b]噻唑化合物

    公开(公告)号:US20090259049A1

    公开(公告)日:2009-10-15

    申请号:US12421182

    申请日:2009-04-09

    IPC分类号: C07D513/02

    CPC分类号: C07D513/04

    摘要: A compound represented by the following formula (I), or salt thereof exhibits excellent CRF receptor antagonism, and sufficient pharmacological activity, safety and pharmacokinetic properties as a drug. wherein R1 represents the formula -A11-A12; R2 represents tetrahydrofurylmethyl, tetrahydropyranylmethyl or tetrahydropyranyl; A11 represents a single bond, methylene or 1,2-ethylene; A12 represents C1-6 alkyl, C3-6 cycloalkyl or C3-6 cycloalkyl having methyl; R3 represents methoxy, cyano, cyclobutyloxymethyl, methoxymethyl or ethoxymethyl; and R4 represents methoxy or chlorine.

    摘要翻译: 由下式(I)表示的化合物或其盐表现出优异的CRF受体拮抗作用,作为药物具有充分的药理活性,安全性和药代动力学性质。 其中R1表示式-A11-A12; R2表示四氢呋喃基甲基,四氢吡喃基甲基或四氢吡喃基; A11表示单键,亚甲基或1,2-亚乙基; A12表示C1-6烷基,C3-6环烷基或具有甲基的C3-6环烷基; R3表示甲氧基,氰基,环丁氧基甲基,甲氧基甲基或乙氧基甲基; R4表示甲氧基或氯。

    Pyrazolothiazole compound
    3.
    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。

    PYRAZOLOOXAZOLE COMPOUND
    4.
    发明申请
    PYRAZOLOOXAZOLE COMPOUND 审中-公开
    吡唑并噻唑化合物

    公开(公告)号:US20110086898A1

    公开(公告)日:2011-04-14

    申请号:US12900046

    申请日:2010-10-07

    CPC分类号: C07D498/04

    摘要: A compound represented by the formula (I) or pharmacologically acceptable salt thereof exhibits an excellent CRF receptor antagonism. wherein R1 and R2 are the same or different and are a hydrogen atom, a C1-6 alkyl group, a cyclic group selected from a C3-6 cycloalkyl group, a tetrahydropyranyl group, a dihydropyranyl group, a tetrahydrofuryl group, a dioxanyl group, a tetrahydrothienyl group, a dithianyl group and a hexahydrothiepinyl group, a C1-6 alkyl group substituted with a cyclic group selected from a C3-6 cycloalkyl group, a tetrahydropyranyl group, a dihydropyranyl group, a tetrahydrofuryl group, a dioxanyl group, a tetrahydrothienyl group, a dithianyl group and a hexahydrothiepinyl group, etc; R3, R4 and R5 are the same or different and are a hydrogen atom, a C1-6 alkyl group, a C3-6 cycloalkyl group, a C1-6 alkoxy group, a C1-6 alkoxy-C1-6 alkyl group, a C3-6 cycloalkoxy-C1-6 alkyl group or a halogen atom; R6 is a hydrogen atom or a C1-6 alkyl group; 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R1和R2相同或不同,为氢原子,C1-6烷基,选自C 3-6环烷基,四氢吡喃基,二氢吡喃基,四氢呋喃基,二氧杂环己烷基, 四噻吩基,二噻烷基和六氢硫杂基,被选自C 3-6环烷基,四氢吡喃基,二氢吡喃基,四氢呋喃基,二烷基,四氢噻吩基中的环状基取代的C 1-6烷基 二硫代基,六氢噻吩基等; R 3,R 4和R 5相同或不同,为氢原子,C 1-6烷基,C 3-6环烷基,C 1-6烷氧基,C 1-6烷氧基-C 1-6烷基, C 3-6环烷氧基-C 1-6烷基或卤素原子; R6是氢原子或C1-6烷基; 并且R 7是C 1-6烷基,C 1-6烷氧基或C 1-6烷硫基。

    Imidazo[1,2-b]pyridazine compound
    8.
    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。