4,5-pyrazinoxindoles
    6.
    发明授权
    4,5-pyrazinoxindoles 失效
    4,5 - 吡嗪并吲哚

    公开(公告)号:US06221867B1

    公开(公告)日:2001-04-24

    申请号:US09464534

    申请日:1999-12-15

    CPC classification number: C07D487/04

    Abstract: Disclosed are novel 4,5-pyrazinoxindoles having the formula These compounds inhibit or modulate protein kinases, in particular JNK protein kinases. These compounds and their pharmaceutically acceptable salts, and prodrugs of said compounds, are useful as anti-inflammatory agents, particularly useful in the treatment of rheumatoid arthritis. Also disclosed are pharmaceutical compositions containing such compounds, and methods for the treatment and/or control of inflammation, particularly in the treatment or control of rheumatoid arthritis, using these compounds.

    Abstract translation: 公开了具有下式的新的4,5-吡嗪氧吲哚:这些化合物抑制或调节蛋白激酶,特别是JNK蛋白激酶。 这些化合物及其药学上可接受的盐和所述化合物的前药可用作抗炎剂,特别可用于治疗类风湿性关节炎。 还公开了含有这些化合物的药物组合物,以及使用这些化合物治疗和/或控制炎症,特别是治疗或控制类风湿性关节炎的方法。

    4,5-azolo-oxindoles
    10.
    发明授权
    4,5-azolo-oxindoles 失效
    4,5-azo-oxindoles

    公开(公告)号:US6153634A

    公开(公告)日:2000-11-28

    申请号:US464507

    申请日:1999-12-15

    CPC classification number: C07D403/06 C07D487/04 C07D513/04 C09B23/04

    Abstract: Disclosed are novel 4,5-azolo-oxindoles having the formula ##STR1## These compounds inhibit cyclin-dependent kinases (CDKs), in particular CDK2. Thus, these compounds and their pharmaceutically acceptable salts, and prodrugs of said compounds, are anti-proliferative agents useful in the treatment or control of cell proliferative disorders, in particular cancer. Also disclosed are pharmaceutical compositions containing these compounds, and methods for the treatment and/or prevention of cancer, particularly in the treatment or control of solid tumors using these compounds, as well as intermediates useful in the preparation of compounds of formula I.

    Abstract translation: 公开了具有下式的新的4,5-azo-oxindoles这些化合物抑制细胞周期蛋白依赖性激酶(CDK),特别是CDK2。 因此,这些化合物及其药学上可接受的盐和所述化合物的前药是用于治疗或控制细胞增殖性疾病,特别是癌症的抗增殖剂。 还公开了含有这些化合物的药物组合物,以及用于治疗和/或预防癌症的方法,特别是使用这些化合物治疗或控制实体瘤的方法,以及可用于制备式I化合物的中间体。

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