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    Corticotropin releasing factor antagonists
    1.
    发明申请
    Corticotropin releasing factor antagonists 失效
    促肾上腺皮质激素释放因子拮抗剂

    公开(公告)号：US20050054661A1

    公开(公告)日：2005-03-10

    申请号：US10480958

    申请日：2002-06-11

    申请人： Romano Di Fabio ,  Chiara Marchionni ,  Fabrizio Micheli ,  Alessandra Pasquarello ,  Yves St-Denis

    发明人： Romano Di Fabio ,  Chiara Marchionni ,  Fabrizio Micheli ,  Alessandra Pasquarello ,  Yves St-Denis

    IPC分类号： A61K31/519 ,  A61K51/00 ,  A61K51/04 ,  A61P1/04 ,  A61P25/00 ,  A61P25/22 ,  A61P25/24 ,  A61P43/00 ,  C07D239/70 ,  C07D239/94 ,  C07D471/04 ,  C07D487/04 ,  C07D487/02

    CPC分类号： C07D487/04 ,  A61K51/0459 ,  C07B2200/05 ,  C07D239/70 ,  C07D239/94 ,  C07D471/04

    摘要： The present invention provides compounds of formula (I) including stereoisomers, prodrugs and pharmaceutically acceptable salts or solvates thereof wherein R is aryl or heteroaryl and each of the above groups R may be substituted by 1 to 4 groups selected from: halogen, C1-C6 alkyl, C1-C6 alkoxy, halo C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, halo C1-C6 alkoxy, —COR4, nitro, —NR3R4 cyano, or a group R5; R1 is hydrogen, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, halo C1-C6 alkyl, halo C1-C6 alkoxy, halogen, NR3R4 or cyano; R2 corresponds to a group CHR6R7; R3 is hydrogen, C1-C6 alkyl; R4 independently from R3, has the same meanings; R5 is C3-C7 cycloalkyl, which may contain one or more double bonds; aryl; or a 5-6 membered heterocycle; wherein each of the above groups R5 may be substituted by one or more groups selected from: halogen, C1-C6 alkyl, C1-C6 alkoxy, halo C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, halo C1-C6 alkoxy, C1-C6 dialkylamino, nitro or cyano; R6 is hydrogen, C2-C6 alkenyl or C1-C6 alkyl, wherein each of the above groups R6 may be substituted by one or more groups selected from: C1-C6 alkoxy and hydroxy; R7 independently from R6, has the same meanings; X is carbon or nitrogen; to processes for their preparation, to pharmaceutical compositions containing them and to their use in the treatment of conditions mediated by corticotropin-releasing factor (CRF).

    摘要翻译： 本发明提供式（I）化合物，其包括立体异构体，前药和药学上可接受的盐或溶剂合物，其中R是芳基或杂芳基，并且上述基团中的每一个R可以被1至4个选自以下的基团取代：卤素，C 1 -C 6 烷基，C 1 -C 6烷氧基，卤代C 1 -C 6烷基，C 2 -C 6烯基，C 2 -C 6炔基，卤代C 1 -C 6烷氧基，-COR 4，硝基，-NR 3 R 4氰基或基团R 5; R 1是氢，C 1 -C 6烷基，C 2 -C 6烯基，C 2 -C 6炔基，卤代C 1 -C 6烷基，卤代C 1 -C 6烷氧基，卤素，NR 3 R 4或氰基; R2对应于CHR6R7基团; R3是氢，C1-C6烷基; R4独立于R3，具有相同的含义; R5是C3-C7环烷基，其可以含有一个或多个双键; 芳基; 或5-6元杂环; 其中每个上述基团R 5可以被一个或多个选自以下的基团取代：卤素，C 1 -C 6烷基，C 1 -C 6烷氧基，卤代C 1 -C 6烷基，C 2 -C 6烯基，C 2 -C 6炔基，卤代C 1 -C 6 烷氧基，C1-C6二烷基氨基，硝基或氰基; R 6是氢，C 2 -C 6烯基或C 1 -C 6烷基，其中上述基团R 6可以被一个或多个选自以下的基团取代：C 1 -C 6烷氧基和羟基; R7独立于R6，具有相同的含义; X是碳或氮; 其制备方法，含有它们的药物组合物及其用于治疗由促肾上腺皮质激素释放因子（CRF）介导的病症的用途。

    Chemical Compounds
    5.
    发明申请
    Chemical Compounds 审中-公开

    公开(公告)号：US20070219232A1

    公开(公告)日：2007-09-20

    申请号：US11749433

    申请日：2007-05-16

    申请人： Romano Di Fabio ,  Fabrizio Micheli ,  Yves St-Denis

    发明人： Romano Di Fabio ,  Fabrizio Micheli ,  Yves St-Denis

    IPC分类号： A61K31/44 ,  C07D211/00 ,  C07D471/00

    CPC分类号： C07D471/04

    摘要： The present invention provides compounds of formula (I) including stereoisomers, prodrugs and pharmaceutically acceptable salts or solvates thereof wherein R is aryl or heteroaryl, each of which may be substituted by 1 to 4 groups selected from: halogen, C1-C6 alkyl, C1-C6 alkoxy, halo C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, halo C1-C6 alkoxy, —C(O)R5, nitro, —NR6R7, cyano, and a group R8; R1 is hydrogen, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, halo C1-C6 alkyl, halo C1-C6 alkoxy, halogen, NR6R7 or cyano; R2 is hydrogen, C3-C7 cycloalkyl, or a group R9; R3 is C3-C7 cycloalkyl, or a group R9; or R2 and R3 together with N form a 5-14 membered heterocycle, which may be substituted by 1 to 3 R10 groups; R4 is hydrogen, C1-C6 alkyl, halogen or halo C1-C6 alkyl; R5 is a C1-C4 alkyl, —OR6 or —NR6R7; R6 is hydrogen or C1-C6 alkyl; R7 is hydrogen or C1-C6 alkyl; R8 is a 5-6 membered heterocycle, which may be saturated or may contain one to three double bonds, and which may be substituted by 1 or more R11 groups; R9 is a C1-C6 alkyl that may be substituted by one or more groups selected from: C3-C7 cycloalkyl, C1-C6 alkoxy, haloC1-C6 alkoxy, hydroxy, haloC1-C6 alkyl; R10 is a group R8, C3-C7 cycloalkyl, C1-C6 alkyl, C1-C6 alkoxy, halo C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, halo C1-C6 alkoxy, hydroxy, halogen, nitro, cyano, C(O)NR6R7, phenyl which may be substituted by 1 to 4 R11 groups; R11 is C3-C7 cycloalkyl, C1-C6 alkyl, C1-C6 alkoxy, halo C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, halo C1-C6 alkoxy, hydroxy, halogen, nitro, cyano, or C(O)NR6R7; X is carbon or nitrogen; n is 1 or 2; to processes for their preparation, to pharmaceutical compositions containing them and to their use in the treatment of conditions mediated by corticotropin-releasing factor (CRF).

    Pyrrolo[2, 3-d] pyrimidine derivatives as corticotropin releasing factor antagonists
    6.
    发明授权
    Pyrrolo[2, 3-d] pyrimidine derivatives as corticotropin releasing factor antagonists 失效
    吡咯并[2,3-d]嘧啶衍生物作为促肾上腺皮质激素释放因子拮抗剂

    公开(公告)号：US07462622B2

    公开(公告)日：2008-12-09

    申请号：US10480958

    申请日：2002-06-11

    申请人： Romano Di Fabio ,  Chiara Marchionni ,  Fabrizio Micheli ,  Alessandra Pasquarello ,  Bendetta Perini ,  Yves St-Denis

    发明人： Romano Di Fabio ,  Chiara Marchionni ,  Fabrizio Micheli ,  Alessandra Pasquarello ,  Bendetta Perini ,  Yves St-Denis

    IPC分类号： A61K31/519 ,  C07D487/04 ,  A61P25/24 ,  A61P25/22

    CPC分类号： C07D487/04 ,  A61K51/0459 ,  C07B2200/05 ,  C07D239/70 ,  C07D239/94 ,  C07D471/04

    摘要： The present invention provides compounds of formula (I) including stereoisomers, prodrugs and pharmaceutically acceptable salts or solvates thereof wherein R is aryl or heteroaryl and each of the above groups R may be substituted by 1 to 4 groups selected from: halogen, C1-C6 alkyl, C1-C6 alkoxy, halo C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, halo C1-C6 alkoxy, —COR4, nitro, —NR3R4 cyano, or a group R5; R1 is hydrogen, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, halo C1-C6 alkyl, halo C1-C6 alkoxy, halogen, NR3R4 or cyano; R2 corresponds to a group CHR6R7; R3 is hydrogen, C1-C6 alkyl; R4 independently from R3, has the same meanings; R5 is C3-C7 cycloalkyl, which may contain one or more double bonds; aryl; or a 5-6 membered heterocycle;  wherein each of the above groups R5 may be substituted by one or more groups selected from: halogen, C1-C6 alkyl, C1-C6 alkoxy, halo C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, halo C1-C6 alkoxy, C1-C6 dialkylamino, nitro or cyano; R6 is hydrogen, C2-C6 alkenyl or C1-C6 alkyl, wherein each of the above groups R6 may be substituted by one or more groups selected from: C1-C6 alkoxy and hydroxy; R7 independently from R6, has the same meanings; X is carbon or nitrogen; to processes for their preparation, to pharmaceutical compositions containing them and to their use in the treatment of conditions mediated by corticotropin-releasing factor (CRF).

    摘要翻译： 本发明提供式（I）化合物，其包括立体异构体，前药和药学上可接受的盐或溶剂合物，其中R是芳基或杂芳基，并且上述基团中的每一个R可以被1至4个选自以下的基团取代：卤素，C 1 -C 6 烷基，C 1 -C 6烷氧基，卤代C 1 -C 6烷基，C 2 -C 6烯基，C 2 -C 6炔基，卤代C 1 -C 6烷氧基，-COR 4，硝基，-NR 3 R 4氰基或基团R 5; R 1是氢，C 1 -C 6烷基，C 2 -C 6烯基，C 2 -C 6炔基，卤代C 1 -C 6烷基，卤代C 1 -C 6烷氧基，卤素，NR 3 R 4或氰基; R2对应于CHR6R7基团; R3是氢，C1-C6烷基; R4独立于R3，具有相同的含义; R5是C3-C7环烷基，其可以含有一个或多个双键; 芳基; 或5-6元杂环; 其中每个上述基团R 5可以被一个或多个选自以下的基团取代：卤素，C 1 -C 6烷基，C 1 -C 6烷氧基，卤代C 1 -C 6烷基，C 2 -C 6烯基，C 2 -C 6炔基，卤代C 1 -C 6 烷氧基，C1-C6二烷基氨基，硝基或氰基; R 6是氢，C 2 -C 6烯基或C 1 -C 6烷基，其中上述基团R 6可以被一个或多个选自以下的基团取代：C 1 -C 6烷氧基和羟基; R7独立于R6，具有相同的含义; X是碳或氮; 其制备方法，含有它们的药物组合物及其用于治疗由促肾上腺皮质激素释放因子（CRF）介导的病症的用途。