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1. 发明申请

WO2016010862A1 COMBINATIONS FOR TREATING CANCERS 审中-公开
标题翻译：治疗癌症的联合
公开(公告)号：WO2016010862A1
公开(公告)日：2016-01-21
申请号：PCT/US2015/040029
申请日：2015-07-10
申请人： GILEAD SCIENCES, INC.
发明人： DI PAOLO, Julie , CLARKE, Astrid
IPC分类号： A61K45/06 , A61K31/475 , A61K31/4985 , A61P35/00
CPC分类号： A61K31/5377 , A61K31/475 , A61K31/4985 , A61K45/06 , A61K2300/00
摘要： Disclosed are combinations for treating a cancer in a subject (e.g., a human) in need thereof, comprising a therapeutically effective amount of a compound of formula (I): or a pharmaceutically acceptable salt thereof, and a vinca-alkaloid, or a pharmaceutically acceptable salt thereof. The subject may be very high risk or high risk for the cancer and may not respond to either agent administered as a sole therapy. The subject who has the cancer may also be refractory to at least one chemotherapy treatment, or is in relapse after treatment with chemotherapy, or both. The cancer may be a hematologic malignancy, such as leukemia or lymphoma, or a solid tumor cancer, such as pancreatic, lung and colon cancer.
摘要翻译：公开了用于治疗有需要的受试者（例如，人）中的癌症的组合，其包含治疗有效量的式（I）化合物或其药学上可接受的盐，长春花生物碱或药学上可接受的盐其可接受的盐。该受试者可能具有非常高的风险或癌症的高风险，并且可能不对作为单独治疗施用的任一药物作出反应。患有癌症的受试者对于至少一种化学疗法治疗也可能是难以治疗的，或者在化学疗法治疗后复发，或两者兼有。癌症可能是血液恶性肿瘤，如白血病或淋巴瘤，或实体肿瘤，如胰腺，肺癌和结肠癌。

2. 发明申请

WO2018085069A1 COMBINATION OF A BCL-2 INHIBITOR AND A BROMODOMAIN INHIBITOR FOR TREATING CANCER 审中-公开
标题翻译： BCL-2抑制剂与BROMODOMAIN抑制剂联合治疗癌症
公开(公告)号：WO2018085069A1
公开(公告)日：2018-05-11
申请号：PCT/US2017/057848
申请日：2017-10-23
申请人： GILEAD SCIENCES, INC.
发明人： BATES, Jamie Geier , CLARKE, Astrid , KENNEY, Thomas F. , KUSAM, Saritha , TANNHEIMER, Stacey
IPC分类号： A61K45/06 , A61K31/444 , A61K31/4709 , A61K31/496 , A61P35/00
CPC分类号： A61K31/496 , A61K31/444 , A61K31/4709 , A61K31/495 , A61K31/5377 , A61K45/06 , A61P35/00 , A61K2300/00
摘要： Provided herein are methods and compositions for the treatment of cancer. In particular, the methods include administration of a Bcl-2 inhibitor and a BET inhibitor.
摘要翻译：本文提供了用于治疗癌症的方法和组合物。具体而言，所述方法包括施用Bcl-2抑制剂和BET抑制剂。

3. 发明申请

WO2016010809A1 SYK INHIBITORS 审中-公开
标题翻译： 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
申请人： GILEAD SCIENCES, INC.
发明人： 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分类号： A61K31/519 , A61K31/475 , A61P35/00 , A61P25/00
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 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.
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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