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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
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.
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公开(公告)号：EP2578585B1
公开(公告)日：2016-07-20
申请号：EP11789754.6
申请日：2011-05-30
IPC分类号： C07D473/34 , A61K31/522 , A61P7/02 , A61P29/00 , A61P35/00 , A61P37/06 , A61P43/00
CPC分类号： C07D473/34 , A61K31/522
摘要： Compounds represented by general formula (I) (all of the symbols in the formula conform to the definitions in the Description) are compounds that, in addition to having a Btk-selective inhibitory activity, exhibit an excellent metabolic stability and can avoid hepatotoxicity or the like, and as a consequence can provide safe therapeutic agents for diseases in which B cells or mast cells participate.
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3.发明公开PROPHYLACTIC AGENT AND/OR THERAPEUTIC AGENT FOR DIFFUSE LARGE B-CELL LYMPHOMA 审中-公开PROPHYLAKTISCHER WIRKSTOFF UND / ODER THERAPEUTISCHER WIRKSTOFFFÜRDIFFUSES GROSSZELLIGES B-ZELL-LYMPHOM
公开(公告)号：EP3122360A1
公开(公告)日：2017-02-01
申请号：EP15768602.3
申请日：2015-03-24
发明人： YOSHIZAWA, Toshio , KOZAKI, Ryohei
CPC分类号： A61K31/522 , A61K45/06 , C07D473/34
摘要： To provide a medicament which shows more remarkable effect in treatment of activated B-cell like diffuse large B-cell lymphoma (ABC-CLBCL) than the existing Btk inhibitor, and is excellent in safety. The present compound exhibits more remarkable effect in treatment of activated B-cell like diffuse large B-cell lymphoma (ABC-DLBCL) patients, inter alia, ABC-DLBCL patients having CD79B wild-type gene background than the existing Btk inhibitor, and therefore, it can attain the object of the present invention.
摘要翻译： 提供一种比现有的Btk抑制剂治疗活化的B细胞如弥漫性大B细胞淋巴瘤（ABC-CLBCL）更显着效果的药物，其安全性优异。 本发明化合物在治疗活化的B细胞如弥漫性大B细胞淋巴瘤（ABC-DLBCL）患者尤其是具有比现有Btk抑制剂具有CD79B野生型基因背景的ABC-DLBCL患者更显着的效果，因此 ，可以实现本发明的目的。
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公开(公告)号：EP2786996B1
公开(公告)日：2016-09-14
申请号：EP12852725.6
申请日：2012-11-28
IPC分类号： C07D473/34 , A61K31/522 , A61P7/02 , A61P17/00 , A61P29/00 , A61P35/00 , A61P35/02 , A61P37/02 , A61P37/08 , A61P43/00
CPC分类号： C07D473/34 , A61K31/522 , C07B2200/13 , C07D473/00
摘要： The purinone derivative 6-amino-9-[(3R)-1-(2-butynoyl)-3-pyrrolidinyl]-7-(4-phenoxyphenyl)-7,9-dihydro-8H-purin-8-one hydrochloride has Btk-selective inhibitory activity and, in addition to having excellent metabolic stability, it is a compound that exhibits a high level of solubility and absorption with respect to the free base and can be crystallized, hence it can serve as a therapeutic agent for diseases involving B cells and mast cells.
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公开(公告)号：EP3112368B1
公开(公告)日：2020-02-12
申请号：EP16176735.5
申请日：2011-05-30
IPC分类号： C07D473/34 , A61K31/522 , A61P7/02 , A61P29/00 , A61P35/00 , A61P37/06 , A61P43/00
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公开(公告)号：EP2786996A1
公开(公告)日：2014-10-08
申请号：EP12852725.6
申请日：2012-11-28
IPC分类号： C07D473/34 , A61K31/522 , A61P7/02 , A61P17/00 , A61P29/00 , A61P35/00 , A61P35/02 , A61P37/02 , A61P37/08 , A61P43/00
CPC分类号： C07D473/34 , A61K31/522 , C07B2200/13 , C07D473/00
摘要： The purinone derivative 6-amino-9-[(3R)-1-(2-butynoyl)-3-pyrrolidinyl]-7-(4-phenoxyphenyl)-7,9-dihydro-8H-purin-8-one hydrochloride has Btk-selective inhibitory activity and, in addition to having excellent metabolic stability, it is a compound that exhibits a high level of solubility and absorption with respect to the free base and can be crystallized, hence it can serve as a therapeutic agent for diseases involving B cells and mast cells.
摘要翻译： 嘌呤酮衍生物6-氨基-9 - [（3R）-1-（2-丁炔酰基）-3-吡咯烷基] -7-（4-苯氧基苯基）-7,9-二氢-8H-嘌呤-8-酮盐酸盐 Btk选择性抑制活性，除了具有优异的代谢稳定性之外，还是对游离碱显示出高水平的溶解性和吸收性并且可以结晶的化合物，因此它可以用作涉及涉及疾病的治疗剂 B细胞和肥大细胞。
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公开(公告)号：EP3590938A1
公开(公告)日：2020-01-08
申请号：EP19190977.9
申请日：2011-05-30
IPC分类号： C07D473/34 , A61K31/522 , A61P7/02 , A61P29/00 , A61P35/00 , A61P37/06 , A61P43/00
摘要： Compounds represented by general formula (I) (all of the symbols in the formula conform to the definitions in the Description) are compounds that, in addition to having a Btk-selective inhibitory activity, exhibit an excellent metabolic stability and can avoid hepatotoxicity or the like, and as a consequence can provide safe therapeutic agents for diseases in which B cells or mast cells participate.
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公开(公告)号：EP3355875A2
公开(公告)日：2018-08-08
申请号：EP16782161.0
申请日：2016-09-30
IPC分类号： A61K31/122 , A61K31/351 , A61K31/4748 , A61K31/522 , A61K31/675 , A61P35/00
CPC分类号： A61K31/522 , A61K31/122 , A61K31/351 , A61K31/4748 , A61K31/675 , A61K2300/00
摘要： Provided herein are methods relating to a therapeutic strategy for treatment of cancer, including hematological malignancies. In particular, the methods include administration of a Btk inhibitor and a checkpoint inhibitor, including combinations in which the Btk inhibitor is 6-amino-9-[(3R)-I-(2-butynoyl)-3- pyrrolidinyl]-7-(4-phenoxyphenyl)-7,9-dihydro-8H-purin-8-one, or a pharmaceutically acceptable salt thereof, and the checkpoint inhibitor is selected from inhibitors of PD-1, PD-L1, and CTLA-4.
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公开(公告)号：EP3112368A1
公开(公告)日：2017-01-04
申请号：EP16176735.5
申请日：2011-05-30
IPC分类号： C07D473/34 , A61K31/522 , A61P7/02 , A61P29/00 , A61P35/00 , A61P37/06 , A61P43/00
摘要： Compounds represented by general formula (I) as drawn below (all of the symbols in the formula conform to the definitions in the Description) are compounds that, in addition to having a Btk-selective inhibitory activity, exhibit an excellent metabolic stability and can avoid hepatotoxicity or the like, and as a consequence can provide safe therapeutic agents for diseases in which B cells or mast cells participate.
摘要翻译： 由下述通式（I）表示的化合物（式中所有符号符合说明书中的定义）是除了具有Btk选择性抑制活性之外还表现出优异的代谢稳定性并且可以避免 肝毒性等，并且因此可以为其中B细胞或肥大细胞参与的疾病提供安全的治疗剂。
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公开(公告)号：EP2578585A1
公开(公告)日：2013-04-10
申请号：EP11789754.6
申请日：2011-05-30
IPC分类号： C07D473/34 , A61K31/522 , A61P7/02 , A61P29/00 , A61P35/00 , A61P37/06 , A61P43/00
CPC分类号： C07D473/34 , A61K31/522
摘要： Compounds represented by general formula (I) (all of the symbols in the formula conform to the definitions in the Description) are compounds that, in addition to having a Btk-selective inhibitory activity, exhibit an excellent metabolic stability and can avoid hepatotoxicity or the like, and as a consequence can provide safe therapeutic agents for diseases in which B cells or mast cells participate.
摘要翻译： 由通式（I）表示的化合物（式中所有符号符合说明书中的定义）是除了具有Btk选择性抑制活性之外还表现出优异的代谢稳定性并且可以避免肝毒性的化合物，或者 因此可以为B细胞或肥大细胞参与的疾病提供安全的治疗剂。
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