公开(公告)号：US11202782B2

公开(公告)日：2021-12-21

申请号：US16337124

申请日：2017-09-27

申请人： BeiGene, Ltd.

发明人： Lai Wang ,  Zhiyu Tang ,  Lusong Luo ,  Min Wei ,  Kang Li ,  Jing Song ,  Tong Zhang ,  Hexiang Wang ,  Bo Ren ,  Changyou Zhou

IPC分类号： A61K31/551 ,  A61K45/00 ,  A61P35/00 ,  C07D471/16 ,  C07D487/06 ,  C07D487/16 ,  A61K31/282 ,  A61K31/337 ,  A61K31/357 ,  A61K39/395 ,  C07K16/28

摘要： Disclosed herein is a method for the prevention, delay of progression or treatment of cancer in a subject, comprising administering to the subject in need thereof a PARP inhibitor, particularly, (R)-2-fluoro-10a-methyl-7,8,9,10,10a,11-hexahydro-5,6,7a,11-tetraazacyclohepta[def]cyclopenta[a]fluoren-4(5H)-one, a sesqui-hydrate thereof, or a pharmaceutically acceptable salt thereof, in combination with an immune checkpoint inhibitor or a chemotherapeutic agent. Also, disclosed a pharmaceutical combination comprising a PARP inhibitor, particularly, (R)-2-fluoro-10a-methyl-7,8,9,10,10a,11-hexahydro-5,6,7a,11-tetraazacyclohepta[def]cyclopenta[a]fluoren-4(5H)-one, a sesqui-hydrate thereof, or a pharmaceutically acceptable salt thereof, in combination with an immune checkpoint inhibitor, or a chemotherapeutic agent and the use thereof.

公开(公告)号：US20200030339A1

公开(公告)日：2020-01-30

申请号：US16337124

申请日：2017-09-27

申请人： BeiGene, Ltd.

发明人： Lai Wang ,  Zhiyu Tang ,  Lusong Luo ,  Min Wei ,  Kang Li ,  Jing Song ,  Tong Zhang ,  Hexiang Wang ,  Bo Ren ,  Changyou Zhou

IPC分类号： A61K31/551 ,  A61K39/395 ,  C07K16/28 ,  A61K31/337 ,  A61K31/282 ,  A61K31/357 ,  A61P35/00

摘要： Disclosed herein is a method for the prevention, delay of progression or treatment of cancer in a subject, comprising administering to the subject in need thereof a PARP inhibitor, particularly, (R)-2-fluoro-10a-methyl-7,8,9,10,10a,11-hexahydro-5,6,7a,11-tetraazacyclohepta[def]cyclopenta[a]fluoren-4(5H)-one, a sesqui-hydrate thereof, or a pharmaceutically acceptable salt thereof, in combination with an immune checkpoint inhibitor or a chemotherapeutic agent. Also, disclosed a pharmaceutical combination comprising a PARP inhibitor, particularly, (R)-2-fluoro-10a-methyl-7,8,9,10,10a,11-hexahydro-5,6,7a,11-tetraazacyclohepta[def]cyclopenta[a]fluoren-4(5H)-one, a sesqui-hydrate thereof, or a pharmaceutically acceptable salt thereof, in combination with an immune checkpoint inhibitor, or a chemotherapeutic agent and the use thereof.

公开(公告)号：US09670203B2

公开(公告)日：2017-06-06

申请号：US14901634

申请日：2014-06-27

申请人： BeiGene, LTD.

发明人： Changyou Zhou ,  Guoliang Zhang

IPC分类号： C07D519/00 ,  C07D405/12 ,  C07D471/04 ,  C07D498/04 ,  C07D473/30

CPC分类号： C07D471/04 ,  C07D405/12 ,  C07D473/30 ,  C07D498/04

摘要： Provided are certain fused tricyclic urea compounds and salts thereof, compositions thereof, and methods of use therefor.

公开(公告)号：US20170027912A1

公开(公告)日：2017-02-02

申请号：US15174229

申请日：2016-06-06

申请人： Beigene, Ltd.

发明人： Bo Ren ,  Changyou Zhou ,  Hexiang Wang

IPC分类号： A61K31/422 ,  A61K31/5377 ,  A61K31/496 ,  A61K45/06 ,  A61K31/454

CPC分类号： A61K31/422 ,  A61K31/454 ,  A61K31/496 ,  A61K31/5377 ,  A61K45/06 ,  C07D413/04 ,  C07D413/14 ,  Y02A50/473

摘要： Disclosed are substituted 5-(3,5-dimethylisoxazol-4-yl)indoline-2-one compounds, pharmaceutical compositions comprising at least one such 4 substituted 5-(3,5-dimethylisoxazol-4-yl)indoline-2-one compound processes for the preparation thereof, and the use thereof for inhibiting BET family of bromodomains and for treating disorders mediated thereby, such as certain cancers.

摘要翻译： 公开了取代的5-（3,5-二甲基异恶唑-4-基）二氢吲哚-2-酮化合物，包含至少一种这样的取代的5-（3,5-二甲基异恶唑-4-基）二氢吲哚-2-酮的药物组合物 用于其制备的复合方法及其用于抑制溴结构域的BET家族和用于治疗由此介导的疾病例如某些癌症的用途。

公开(公告)号：US20150175617A1

公开(公告)日：2015-06-25

申请号：US14369374

申请日：2011-12-31

申请人： BEIGENE, LTD.

发明人： Changyou Zhou ,  Bo Ren ,  Hexiang Wang

IPC分类号： C07D487/06 ,  C07D471/22 ,  C07D471/16

CPC分类号： C07D487/06 ,  A61K31/551 ,  A61P29/00 ,  A61P35/00 ,  A61P37/00 ,  C07D471/16 ,  C07D471/22 ,  C07D487/04 ,  C07D487/14

摘要： Provided are certain fused tetra or penta-cyclic compounds and salts thereof, compositions thereof, and methods of use thereof.

摘要翻译： 提供一些稠合的四或五环化合物及其盐，其组合物及其使用方法。

公开(公告)号：US11534431B2

公开(公告)日：2022-12-27

申请号：US17099115

申请日：2020-11-16

申请人： BeiGene, Ltd.

发明人： Jing Song ,  Lai Wang ,  Kang Li ,  Tong Zhang ,  Lusong Luo ,  Min Wei ,  Zhiyu Tang ,  Guoliang Zhang ,  Changyou Zhou

IPC分类号： A61K31/4375 ,  A61P35/00 ,  C07K16/28

摘要： Disclosed herein is a pharmaceutical combination for use in the prevention, delay of progression or treatment of cancer, wherein the pharmaceutical combination exhibits a synergistic efficacy. The pharmaceutical combination comprises a humanized antagonist monoclonal antibody against PD- and a RAF inhibitor. Also disclosed herein is a combination for use in the prevention, delay of progression or treatment of cancer in a subject, comprising administering to the subject a therapeutically effective amount of a humanized antagonist monoclonal antibody against PD-1 and a therapeutically effective amount of a RAF inhibitor.

公开(公告)号：US11472811B2

公开(公告)日：2022-10-18

申请号：US16982681

申请日：2019-04-08

申请人： BEIGENE, LTD.

发明人： Guoliang Zhang ,  Changyou Zhou

IPC分类号： C07D487/14

摘要： Disclosed herein is a pyrazolotriazolopyrimidine derivative or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof useful as an A2A receptor antagonist, and a pharmaceutical composition comprising the same. Also disclosed herein is a method of treating cancer using the pyrazolotriazolopyrimidine derivative or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof as an A2A receptor antagonist.

公开(公告)号：US10899763B2

公开(公告)日：2021-01-26

申请号：US16488085

申请日：2018-02-27

申请人： BEIGENE, LTD.

发明人： Hexiang Wang ,  Xianzhao Kuang ,  Changyou Zhou

IPC分类号： C07D487/22 ,  A61K31/55 ,  A61P35/00 ,  C07D471/22

摘要： Disclosed herein are salts of (R)-2-fluoro-10a-methyl-7,8,9,10,10a,11-hexahydro-5,6,7a,11-tetraazacyclohepta[def]cyclopenta[a]fluoren-4(5H)-one, and crystalline forms (polymorphs) thereof. Also disclosed herein are methods of preparing those crystalline forms, and methods of using at least one of those crystalline forms in treating a cancer responsive to inhibition of PARP, especially a cancer associated with BRCA1/2 mutant activities or other HR deficiencies, in a subject.

公开(公告)号：US09670231B2

公开(公告)日：2017-06-06

申请号：US14901556

申请日：2014-06-27

申请人： BEIGENE, LTD.

发明人： Changyou Zhou ,  Gouliang Zhang

IPC分类号： C07D519/00 ,  C07D405/12 ,  C07D471/04 ,  C07D498/04

CPC分类号： C07D519/00 ,  C07D405/12 ,  C07D471/04 ,  C07D498/04

摘要： Provided are fused tricyclic amide compounds, pharmaceutical compositions comprising at least one such fused tricyclic compound, processes for the preparation thereof, and the use thereof in therapy. Disclosed herein are certain tricyclic amide compounds that can be useful for inhibiting multiple (specifically BRAF and/or EGFR-T790M) kinases and for treating disorders mediated thereby.

公开(公告)号：US09617273B2

公开(公告)日：2017-04-11

申请号：US14988484

申请日：2016-01-05

申请人： BEIGENE, LTD.

发明人： Changyou Zhou ,  Bo Ren ,  Hexiang Wang

IPC分类号： C07D487/06 ,  C07D487/14 ,  C07D487/04 ,  C07D471/16 ,  C07D471/22

CPC分类号： C07D487/06 ,  A61K31/551 ,  A61P29/00 ,  A61P35/00 ,  A61P37/00 ,  C07D471/16 ,  C07D471/22 ,  C07D487/04 ,  C07D487/14

摘要： Provided are certain fused tetra or penta-cyclic compounds and salts thereof, compositions thereof, and methods of use thereof.