Oxindole derivatives
    3.
    发明授权
    Oxindole derivatives 失效
    羟吲哚衍生物

    公开(公告)号:US06720332B2

    公开(公告)日:2004-04-13

    申请号:US10362744

    申请日:2003-02-27

    IPC分类号: A61K3144

    CPC分类号: C07D471/04

    摘要: Oxindole derivatives, specifically pyrrolo[3,2-f]quinoline-2-ones, which are useful as CDK4 inhibitors are described herein. The described invention also includes methods of making such oxindole derivatives as well as methods of using the same in the treatment of hyperproliferative diseases.

    摘要翻译: 本文描述了可用作CDK4抑制剂的羟吲哚衍生物,特别是吡咯并[3,2-f]喹啉-2-酮。 所述的发明还包括制备这种羟吲哚衍生物的方法及其用于治疗过度增殖性疾病的方法。

    Chemical Compounds
    7.
    发明申请
    Chemical Compounds 审中-公开
    化学化合物

    公开(公告)号:US20080275062A1

    公开(公告)日:2008-11-06

    申请号:US10597473

    申请日:2005-01-28

    摘要: There is provided compounds of Formula (I) and salts, solvates, and physiologically functional derivatives thereof: wherein R1 is hydrogen or C1-6alkyl; n is 1, 2, 3 or 4; R2 is aryl, optionally substituted by one or two groups selected from the group consisting of halogen, hydroxy, cyano, C1-4alkyl, C1-4alkoxy, C1-4alkanoyl, haloC1-4alkyl, haloC1-4alkoxy, aryl, aryloxy, C1-4alkoxycarbonyl, C1-4alkylsulfonyl and a group R3R4NSO2 (wherein R3 and R4 are independently hydrogen or C1-4alkyl) and a 5- or 6-membered heteroaryl group; or n is 0 and R1 and R2, together with the nitrogen atom to which they are joined, form a 5- or 6-membered monocyclic heterocyclic ring or a 9- or 10-membered bicyclic heterocyclic ring wherein at least the ring which contains the nitrogen atom to which R1 and R2 are joined is non-aromatic, and wherein the 5- or 6-membered monocyclic heterocyclic ring or the 9- or 10-membered bicyclic heterocyclic ring is optionally substituted by one or two groups selected from the group consisting of halogen, hydroxy, cyano, oxo, C1-4alkyl, C1-4alkanoyl, C1-4alkoxy, haloC1-4alkyl, haloC1-4alkoxy, aryl, aryloxy and C1-4alkoxycarbonyl; and X is indazolyl, pyrazolyl or a group: wherein G is CH or N; and Y1 and Y2 are independently hydrogen, halogen and a group NR5R6 (wherein R5 and R6 are independently hydrogen, C1-6alkyl or C2-6alkenyl).

    摘要翻译: 提供式(I)化合物及其盐,溶剂化物和生理功能衍生物:其中R1是氢或C 1-6烷基; n为1,2,3或4; R2是芳基,任选地被一个或两个选自卤素,羟基,氰基,C 1-4烷基,C 1-4烷氧基,C 1-4烷基, 烷基,卤代C 1-4烷基,卤代C 1-4烷氧基,芳基,芳氧基,C 1-4烷基, 烷氧基羰基,C 1-4烷基磺酰基和基团R 3 R 4 NSO 2(其中R 3和R 4独立地是氢或C 1-4烷基 )和5-或6-元杂芳基; 或n为0,并且R 1和R 2与它们连接的氮原子一起形成5-或6-元单环杂环或9-或10-元双环杂环,其中至少含有 R 1和R 2连接的氮原子是非芳族的,其中5或6元单环杂环或9或10元双环杂环任选被一个或两个选自以下的基团取代: 卤素,羟基,氰基,氧代,C 1-4烷基,C 1-4烷酰基,C 1-4烷氧基,卤代C 1-4烷基, 烷基,卤代C 1-4烷氧基,芳基,芳氧基和C 1-4烷氧基羰基; 并且X是吲唑基,吡唑基或基团:其中G是CH或N; 和Y 1和Y 2独立地是氢,卤素和基团NR 5 R 6(其中R 5和R 6独立地是氢,C 1-6烷基 或C 2-6烯基)。