Pyrrolo[2, 3-d] pyrimidine derivatives as corticotropin releasing factor antagonists
    1.
    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

    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。

    Corticotropin releasing factor antagonists
    2.
    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

    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。

    Sulfonamido derivatives of 3,4-diarylpyrazoles as protein kinase inhibitors
    7.
    发明授权
    Sulfonamido derivatives of 3,4-diarylpyrazoles as protein kinase inhibitors 有权
    3,4-二芳基吡唑的磺酰胺衍生物作为蛋白激酶抑制剂

    公开(公告)号:US08791265B2

    公开(公告)日:2014-07-29

    申请号:US13574168

    申请日:2011-01-19

    CPC分类号: C07D401/04 A61K31/4439

    摘要: Compounds which are sulfonamido 3,4-diarylpyrazole derivatives, or pharmaceutically acceptable salts thereof, their preparation process and pharmaceutical compositions comprising them are disclosed; these compounds are useful in the treatment of diseases caused by and/or associated with an altered protein kinase activity such as cancer, viral infection, prevention of AIDS development in HIV-infected individuals, cell proliferative disorders, autoimmune and neurodegenerative disorders; also disclosed is their use as prodrugs.

    摘要翻译: 公开了作为磺酰氨基3,4-二芳基吡唑衍生物的化合物或其药学上可接受的盐,其制备方法和包含它们的药物组合物; 这些化合物可用于治疗由改变的蛋白激酶活性引起的和/或与其相关的疾病,例如癌症,病毒感染,HIV感染个体中的AIDS发展的预防,细胞增殖性疾病,自身免疫和神经变性疾病; 也公开了它们作为前药的用途。