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1. 发明申请

WO2016209961A1 COMBINATION THERAPIES FOR TREATING B-CELL MALIGNANCIES 审中-公开
标题翻译：用于治疗B细胞恶性肿瘤的组合疗法
公开(公告)号：WO2016209961A1
公开(公告)日：2016-12-29
申请号：PCT/US2016/038763
申请日：2016-06-22
申请人： GILEAD SCIENCES, INC. , ONO PHARMACEUTICAL CO., LTD.
发明人： COLLINS, Helen , DI PAOLO, Julie , KEEGAN, Kathy , KOZAKI, Ryohei , MEADOWS, Sarah , NELSON, Cara , QUEVA, Christophe , RAMANATHAN, Srinivasan , TANNHEIMER, Stacey , TUMAS, Daniel , YASUHIRO, Tomoko , YOSHIZAWA, Toshio
IPC分类号： A61K31/52 , A61K31/522 , A61K9/00 , A61P35/00 , A61P35/02
CPC分类号： A61K31/52 , A61K9/2004 , A61K31/522 , A61K2300/00
摘要： Provided herein are methods that relate to a therapeutic strategy for treatment of a E cell malignancy. In particular, the methods include administration of a PI3K inhibitor and BTK inhibitor.
摘要翻译：本文提供了涉及用于治疗E细胞恶性肿瘤的治疗策略的方法。特别地，所述方法包括施用PI3K抑制剂和BTK抑制剂。

2. 发明公开

EP3313405A1 COMBINATION THERAPIES FOR TREATING B-CELL MALIGNANCIES 审中-公开
标题翻译：联合疗法治疗B细胞恶性肿瘤
公开(公告)号：EP3313405A1
公开(公告)日：2018-05-02
申请号：EP16741427.5
申请日：2016-06-22
申请人： Gilead Sciences, Inc. , Ono Pharmaceutical Co., Ltd.
发明人： COLLINS, Helen , DI PAOLO, Julie , KEEGAN, Kathy , KOZAKI, Ryohei , MEADOWS, Sarah , NELSON, Cara , QUEVA, Christophe , RAMANATHAN, Srinivasan , TANNHEIMER, Stacey , TUMAS, Daniel , YASUHIRO, Tomoko , YOSHIZAWA, Toshio
IPC分类号： A61K31/52 , A61K31/522 , A61K9/00 , A61P35/00 , A61P35/02
CPC分类号： A61K31/522 , A61K9/2004 , A61K31/52 , A61P35/00 , A61K2300/00
摘要： Provided herein are methods that relate to a therapeutic strategy for treatment of a B-cell malignancy. In particular, the methods include administration of a PI3K inhibitor and a BTK inhibitor.

3. 发明申请

WO2017023584A1 COMBINATION THERAPIES FOR TREATING CANCERS 审中-公开
标题翻译：治疗癌症的组合治疗
公开(公告)号：WO2017023584A1
公开(公告)日：2017-02-09
申请号：PCT/US2016/043676
申请日：2016-07-22
申请人： GILEAD SCIENCES, INC.
发明人： ABELLA, Esteban, M. , COLLINS, Helen , DI PAOLO, Julie , QUÉVA, Christophe , TUMAS, Daniel
IPC分类号： A61K31/522 , A61K39/395 , A61K31/496 , A61K31/519 , A61K31/52 , C07K16/28 , A61P35/02
CPC分类号： A61K31/522 , A61K31/496 , A61K31/519 , A61K31/52 , A61K2300/00
摘要： Methods for treatment of cancer, including hematological malignancies. In particular, the methods include administration of a BTK inhibitor and a BCL-2 inhibitor or pharmaceutically acceptable salts or hydrates thereof, a Btk inhibitor and a Syk inhibitor or pharmaceutically acceptable salts or hydrates thereof, and administration of a Btk inhibitor and a P13K inhibitor or pharmaceutically acceptable salts or hydrates thereof.
摘要翻译：治疗癌症的方法，包括血液恶性肿瘤。特别地，所述方法包括施用BTK抑制剂和BCL-2抑制剂或其药学上可接受的盐或水合物，Btk抑制剂和Syk抑制剂或其药学上可接受的盐或水合物，以及施用Btk抑制剂和P13K抑制剂或其药学上可接受的盐或水合物。

4. 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。

5. 发明申请

WO2015084992A1 METHODS FOR TREATING CANCERS 审中-公开
标题翻译：治疗癌症的方法
公开(公告)号：WO2015084992A1
公开(公告)日：2015-06-11
申请号：PCT/US2014/068423
申请日：2014-12-03
申请人： GILEAD SCIENCES, INC.
发明人： DI PAOLO, Julie , HAWKINS, Michael, J. , HU, Jing , JIN, Feng , MELCHOR-KHAN, Flordeliza , REDDY, Anita
IPC分类号： A61K31/5377 , A61P35/02 , A61P35/00
CPC分类号： A61K31/5377
摘要： 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. The subject may be very high risk or high risk for the cancer. 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.
摘要翻译：公开了用于治疗有需要的受试者（例如人）中的癌症的方法，其包括向受试者施用治疗有效量的式（I）化合物或其药学上可接受的盐。该问题可能是非常高的风险或癌症的高风险。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。

6. 发明申请

WO2017059252A1 COMBINATIONS OF THE BTK INHIBITOR GS-4059 WITH INHIBITORS SELECTED FROM A JAK, ASK1, BRD AND/OR MMP9 INHIBITOR TO TREAT CANCER, ALLERGIC DISORDERS, AUTOIMMUNE DISEASES OR INFLAMMATORY DISEASES 审中-公开
标题翻译： BTK抑制剂GS-4059与来自JAK，ASK1，BRD和/或MMP9的抑制剂的组合抑制癌症，过敏性疾病，自身免疫性疾病或炎症性疾病
公开(公告)号：WO2017059252A1
公开(公告)日：2017-04-06
申请号：PCT/US2016/054780
申请日：2016-09-30
申请人： GILEAD SCIENCES, INC.
发明人： DI PAOLO, Julie , BRECKENRIDGE, David , BATES, Jamie , TUMAS, Daniel
IPC分类号： A61K31/00 , A61K31/437 , A61K31/4545 , A61K31/506 , A61K31/519 , A61K31/522 , A61K31/5375 , A61K31/541 , A61K31/553 , A61P35/00 , A61P29/00
CPC分类号： A61K31/522 , A61K31/00 , A61K31/437 , A61K31/4545 , A61K31/506 , A61K31/519 , A61K31/5375 , A61K31/541 , A61K31/553 , A61K2300/00
摘要： Provided herein are methods that relate to a therapeutic strategy for treatment of cancer, and allergic, autoimmune, and inflammatory disorders including hematological malignancies. In particular, the methods include administration of a BTK inhibitor and with one or more inhibitor. For example, the one or more inhibitor may be a JAK inhibitor, a ASK1 inhibitor, a BRD4 inhitibor or an MMP9 inhibitor.
摘要翻译：本文提供了涉及用于治疗癌症，过敏性，自身免疫性和炎症性疾病（包括血液恶性肿瘤）的治疗策略的方法。特别地，所述方法包括施用BTK抑制剂和一种或多种抑制剂。例如，一种或多种抑制剂可以是JAK抑制剂，ASK1抑制剂，BRD4抑制剂或MMP9抑制剂。

7. 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。

8. 发明公开

EP3169366A1 COMBINATIONS FOR TREATING CANCERS 无效
标题翻译：治疗癌症的组合
公开(公告)号：EP3169366A1
公开(公告)日：2017-05-24
申请号：EP15744790.5
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 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. 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）的癌症的方法，其包括向受试者施用治疗有效量的式I化合物或其药学上可接受的盐; 与长春花生物碱或其药学上可接受的盐组合。受试者可能是非常高风险或高风险的癌症，并且可能对作为唯一疗法施用的任一药剂都不响应。患有癌症的受试者对于至少一种化学疗法治疗也是难治性的，或者在用化学疗法治疗后复发或两者兼有。癌症可以是血液恶性肿瘤，如白血病或淋巴瘤，或实体肿瘤癌症，如胰腺癌，肺癌和结肠癌。

9. 发明公开

EP3355871A1 COMBINATIONS OF THE BTK INHIBITOR GS-4059 WITH INHIBITORS SELECTED FROM A JAK, ASK1, BRD AND/OR MMP9 INHIBITOR TO TREAT CANCER, ALLERGIC DISORDERS, AUTOIMMUNE DISEASES OR INFLAMMATORY DISEASES 审中-公开
公开(公告)号：EP3355871A1
公开(公告)日：2018-08-08
申请号：EP16785022.1
申请日：2016-09-30
申请人： Gilead Sciences, Inc.
发明人： DI PAOLO, Julie , BRECKENRIDGE, David , BATES, Jamie , TUMAS, Daniel
IPC分类号： A61K31/00 , A61K31/437 , A61K31/4545 , A61K31/506 , A61K31/519 , A61K31/522 , A61K31/5375 , A61K31/541 , A61K31/553 , A61P35/00 , A61P29/00
CPC分类号： A61K31/522 , A61K31/00 , A61K31/437 , A61K31/4545 , A61K31/506 , A61K31/519 , A61K31/5375 , A61K31/541 , A61K31/553 , A61K2300/00
摘要： Provided herein are methods that relate to a therapeutic strategy for treatment of cancer, and allergic, autoimmune, and inflammatory disorders including hematological malignancies. In particular, the methods include administration of a BTK inhibitor and with one or more inhibitor. For example, the one or more inhibitor may be a JAK inhibitor, a ASK1 inhibitor, a BRD4 inhitibor or an MMP9 inhibitor.

10. 发明授权

EP3076976B1 METHODS FOR TREATING CANCERS 有权转让
公开(公告)号：EP3076976B1
公开(公告)日：2020-09-02
申请号：EP14821005.7
申请日：2014-12-03
申请人： Gilead Sciences, Inc.
发明人： DI PAOLO, Julie , HAWKINS, Michael, J. , HU, Jing , JIN, Feng , MELCHOR-KHAN, Flordeliza , REDDY, Anita
IPC分类号： A61K31/5377 , A61P35/02 , A61P35/00

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