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    SYK INHIBITORS
    4.
    发明申请
    SYK INHIBITORS 审中-公开
    SYK抑制剂

    公开(公告)号：WO2015100217A1

    公开(公告)日：2015-07-02

    申请号：PCT/US2014/071842

    申请日：2014-12-22

    Applicant: GILEAD SCIENCES, INC.

    Inventor： BLOMGREN, Peter, A. ,  CURRIE, Kevin, S. ,  KROPF, Jeffrey E. ,  LEE, Seung H. ,  LO, Jennifer R. ,  MITCHELL, Scott A. ,  SCHMITT, Aaron C. ,  XIONG, Jin-Ming ,  XU, Jiangjun ,  ZHAO, Zhongdong

    IPC: C07D487/04 ,  A61K31/519 ,  A61P35/00 ,  A61P25/00

    CPC classification number: A61K31/4985 ,  A61K9/0053 ,  A61K31/5377 ,  C07D487/04

    Abstract: 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 R 1 , R 2 , R 3 , and R 4 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.

    Abstract translation: 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。

    SYK INHIBITORS
    7.
    发明申请
    SYK INHIBITORS 审中-公开
    SYK抑制剂

    公开(公告)号：WO2016010809A1

    公开(公告)日：2016-01-21

    申请号：PCT/US2015/039677

    申请日：2015-07-09

    Applicant: GILEAD SCIENCES, INC.

    Inventor： BLOMGREN, Peter, A. ,  CLARKE, Astrid ,  CURRIE, Kevin, S. ,  DI PAOLO, Julie ,  KROPF, Jeffrey, E. ,  LEE, Seung, H. ,  LO, Jennifer, R. ,  MITCHELL, Scott, A. ,  SCHMITT, Aaron, C. ,  SWAMINATHAN, Sundaramoorthi ,  XIONG, Jin-Ming ,  XU, Jianjun ,  ZHAO, Zhongdong

    IPC: A61K31/519 ,  A61K31/475 ,  A61P35/00 ,  A61P25/00

    CPC classification number: A61K31/4985 ,  A61K31/475 ,  A61K31/519 ,  A61K31/5377 ,  A61K2300/00

    Abstract: The present disclosure relates to compounds that are Syk inhibitors and to their use in the treatment of various disease slates, including cancer and inflammatory conditions. In particular embodiments, the structure of the compounds is given by Formula I: wherein R 1 , R 2 , R 3 , and R 4 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.

    Abstract translation: 本公开涉及作为Syk抑制剂的化合物及其在治疗各种疾病鳞状细胞，包括癌症和炎症病症中的用途。 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此需要的个体（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。

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