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    SYK INHIBITORS
    15.
    发明申请
    SYK INHIBITORS 有权
    SYK抑制剂

    公开(公告)号：US20160058758A1

    公开(公告)日：2016-03-03

    申请号：US14795123

    申请日：2015-07-09

    申请人： Gilead Sciences, Inc.

    发明人： Peter A. Blomgren ,  Astrid Clarke ,  Kevin S. Currie ,  Julie Di Paolo ,  Jeffrey E. Kropf ,  Seung H. Lee ,  Jennifer R. Lo ,  Scott A. Mitchell ,  Aaron C. Schmitt ,  Sundaramoorthi Swaminathan ,  Jin-Ming Xiong ,  Jianjun Xu ,  Zhongdong Zhao

    IPC分类号： A61K31/4985 ,  A61K31/5377 ,  A61K31/475

    CPC分类号： A61K31/4985 ,  A61K31/475 ,  A61K31/519 ,  A61K31/5377 ,  A61K2300/00

    摘要： The present disclosure relates to compounds that are Syk inhibitors and to their use in the treatment of various disease states, including cancer and inflammatory conditions. In particular embodiments, the structure of the compounds is given by Formula I: wherein R1, R2, R3, and R4 are as described herein. The present disclosure further provides pharmaceutical compositions that include a compound of Formula I, or pharmaceutically acceptable salts thereof, and methods of using these compounds and compositions to treat conditions mediated by Syk. In certain embodiments, also disclosed are methods for treating a cancer in a subject (e.g., a human) in need thereof, comprising administering to the subject a therapeutically effective amount of a compound of formula I, or a pharmaceutically acceptable salt thereof, in combination with a vinca-alkaloid, or a pharmaceutically acceptable salt thereof.

    摘要翻译： 本公开涉及作为Syk抑制剂的化合物及其在治疗各种疾病状态（包括癌症和炎性病症）中的用途。 在具体实施方案中，化合物的结构由式I给出：其中R 1，R 2，R 3和R 4如本文所述。 本公开进一步提供包含式I化合物或其药学上可接受的盐的药物组合物，以及使用这些化合物和组合物治疗由Syk介导的病症的方法。 在某些实施方案中，还公开了用于治疗有需要的受试者（例如，人）中的癌症的方法，其包括给予受试者治疗有效量的式I化合物或其药学上可接受的盐，其组合 长春花生物碱或其药学上可接受的盐。

    Substituted imidazo[1,2-a]pyrazines as Syk inhibitors
    19.
    发明授权
    Substituted imidazo[1,2-a]pyrazines as Syk inhibitors 有权
    取代的咪唑并[1,2-a]吡嗪作为Syk抑制剂

    公开(公告)号：US09290505B2

    公开(公告)日：2016-03-22

    申请号：US14578973

    申请日：2014-12-22

    申请人： Gilead Sciences, Inc.

    发明人： Peter A. Blomgren ,  Kevin S. Currie ,  Jeffrey E. Kropf ,  Seung H. Lee ,  Jennifer R. Lo ,  Scott A. Mitchell ,  Aaron C. Schmitt ,  Jin-Ming Xiong ,  Jianjun Xu ,  Zhongdong Zhao ,  Sundaramoorthi Swaminathan

    IPC分类号： A61K31/4985 ,  C07D241/38 ,  C07D487/04

    CPC分类号： C07D487/04

    摘要： The present disclosure relates to compounds that are Syk inhibitors and to their use in the treatment of various disease states, including cancer and inflammatory conditions. In particular embodiments, the structure of the compounds is given by Formula I: wherein R1, R2, R3, and R4 are as described herein. The present disclosure further provides pharmaceutical compositions that include a compound of Formula I, or pharmaceutically acceptable salts or co-crystals thereof, and methods of using these compounds and compositions to treat conditions mediated by Syk.

    摘要翻译： 本公开涉及作为Syk抑制剂的化合物及其在治疗各种疾病状态（包括癌症和炎性病症）中的用途。 在具体实施方案中，化合物的结构由式I给出：其中R 1，R 2，R 3和R 4如本文所述。 本公开进一步提供包含式I化合物或其药学上可接受的盐或共晶的药物组合物，以及使用这些化合物和组合物治疗由Syk介导的病症的方法。