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    QUINOLINE DERIVATIVES AS BROMODOMAIN INHIBITORS
    1.
    发明公开
    QUINOLINE DERIVATIVES AS BROMODOMAIN INHIBITORS 审中-公开
    喹啉衍生物作为BROMODOMAIN抑制剂

    公开(公告)号：EP3074389A1

    公开(公告)日：2016-10-05

    申请号：EP13802824.6

    申请日：2013-11-26

    申请人： Gilead Sciences, Inc.

    发明人： BABAOGLU, Kerim ,  CORKEY, Britton Kenneth ,  JIANG, Robert H. ,  SPERANDIO, David ,  YANG, Hai

    IPC分类号： C07D413/14 ,  C07D413/04 ,  A61K31/517 ,  A61K31/4709 ,  A61K35/00

    CPC分类号： C07D413/04 ,  C07D413/14

    摘要： This application relates to chemical compounds which may act as inhibitors of, or which may otherwise modulate the activity of a bromodomain-containing protein, including bromodomain-containing protein 4 (BRD4), and to compositions and formulations containing such compounds, and methods of using and making such compounds. Compounds include compounds of Formula I, wherein R, R2, R3, R4, R7, W, X are as described herein and Z is selected from the group consisting of unsubstituted or substituted isoxazolyl, and unsubstituted or substituted pyrazolyl. Provided herein are also methods for the preparation and use of the compounds, and to pharmaceutical compositions containing the same.

    摘要翻译： 本申请涉及可用作抑制剂或可调节含溴结构域的蛋白质（包括含溴结构域的蛋白质4（BRD4））的活性的化合物，涉及含有此类化合物的组合物和制剂，以及使用 并制造这样的化合物。 化合物包括其中R，R 2，R 3，R 4，R 7，W，X如本文所述且Z选自未取代或取代的异恶唑基和未取代或取代的吡唑基的式I化合物。 本文还提供了用于制备和使用这些化合物的方法，以及包含它们的药物组合物。