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    Pyrazolothiazole compound
    1.
    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

    申请人： Kogyoku Shin ,  Taro Terauchi ,  Yoshinori Takahashi ,  Minako Hashizume ,  Kunitoshi Takeda ,  Kodo Shikata ,  Akira Inomata

    发明人： Kogyoku Shin ,  Taro Terauchi ,  Yoshinori Takahashi ,  Minako Hashizume ,  Kunitoshi Takeda ,  Kodo Shikata ,  Akira Inomata

    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。

    3-phenylpyrazolo[5,1-b]thiazole compounds
    2.
    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

    申请人： Hisashi Shibata ,  Kodo Shikata ,  Akira Inomata ,  Kogyoku Shin ,  Taro Terauchi ,  Yoshinori Takahashi ,  Minako Hashizume ,  Kunitoshi Takeda

    发明人： Hisashi Shibata ,  Kodo Shikata ,  Akira Inomata ,  Kogyoku Shin ,  Taro Terauchi ,  Yoshinori Takahashi ,  Minako Hashizume ,  Kunitoshi Takeda

    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。

    PYRAZOLOOXAZOLE COMPOUND
    3.
    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

    申请人： Kogyoku SHIN ,  Taro Terauchi ,  Yoshinori Takahashi ,  Minako Hashizume ,  Kunitoshi Takeda ,  Kodo Shikata ,  Akira Inomata

    发明人： Kogyoku SHIN ,  Taro Terauchi ,  Yoshinori Takahashi ,  Minako Hashizume ,  Kunitoshi Takeda ,  Kodo Shikata ,  Akira Inomata

    IPC分类号： A61K31/4162 ,  C07D487/04 ,  A61P25/00 ,  A61P1/00

    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。

    3-PHENYLPYRAZOLO[5,1-b]THIAZOLE COMPOUNDS
    4.
    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

    申请人： Hisashi Shibata ,  Kodo Shikata ,  Akira Inomata ,  Kogyoku Shin ,  Taro Terauchi ,  Yoshinori Takahashi ,  Minako Hashizume ,  Kunitoshi Takeda

    发明人： Hisashi Shibata ,  Kodo Shikata ,  Akira Inomata ,  Kogyoku Shin ,  Taro Terauchi ,  Yoshinori Takahashi ,  Minako Hashizume ,  Kunitoshi Takeda

    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。