公开(公告)号：EP2970312B1

公开(公告)日：2017-11-15

申请号：EP14779458.0

申请日：2014-03-11

申请人： The Regents of The University of Michigan

发明人： WANG, Shaomeng ,  RAN, Xu ,  ZHAO, Yujun ,  YANG, Chao-yie ,  LIU, Liu ,  BAI, Longchuan ,  MCEACHERN, Donna ,  STUCKEY, Jeanne ,  MEAGHER, Jennifer, Lynn ,  SUN, Duxin ,  LI, Xiaoqin ,  ZHOU, Bing ,  KARATAS, Hacer ,  LUO, Ruijuan ,  CHINNAIYAN, Arul ,  ASANGANI, Irfan, A.

IPC分类号： C07D487/04 ,  C07D413/10 ,  C07D413/04 ,  A61K31/4745 ,  A61P35/00

CPC分类号： A61K45/06 ,  C07D471/04 ,  C07D487/04 ,  C07D491/056

摘要： Inhibitors of BET bromodomains and compositions containing the same are disclosed. Methods of using the BET bromodomain inhibitors in the treatment of diseases and conditions wherein inhibition of BET bromodomain provides a benefit, like cancers, also are disclosed.

公开(公告)号：EP2970312A1

公开(公告)日：2016-01-20

申请号：EP14779458.0

申请日：2014-03-11

申请人： The Regents of The University of Michigan

发明人： WANG, Shaomeng ,  RAN, Xu ,  ZHAO, Yujun ,  YANG, Chao-yie ,  LIU, Liu ,  BAI, Longchuan ,  MCEACHERN, Donna ,  STUCKEY, Jeanne ,  MEAGHER, Jennifer, Lynn ,  SUN, Duxin ,  LI, Xiaoqin ,  ZHOU, Bing ,  KARATAS, Hacer ,  LUO, Ruijuan ,  CHINNAIYAN, Arul ,  ASANGANI, Irfan, A.

IPC分类号： C07D487/04 ,  C07D413/10 ,  C07D413/04 ,  A61K31/4745 ,  A61P35/00

CPC分类号： A61K45/06 ,  C07D471/04 ,  C07D487/04 ,  C07D491/056

摘要： Inhibitors of BET bromodomains and compositions containing the same are disclosed. Methods of using the BET bromodomain inhibitors in the treatment of diseases and conditions wherein inhibition of BET bromodomain provides a benefit, like cancers, also are disclosed.

摘要翻译： 公开了BET溴结构域的抑制剂和含有它们的组合物。 也公开了使用BET溴结构域抑制剂治疗其中抑制BET溴结构域提供益处的疾病和病症的方法，如癌症。

公开(公告)号：EP3110818A1

公开(公告)日：2017-01-04

申请号：EP15711599.9

申请日：2015-02-27

申请人： The Regents of The University of Michigan

发明人： WANG, Shaomeng ,  ZHAO, Yujun ,  ZHOU, Bing ,  AGUILAR, Angelo ,  LIU, Liu ,  BAI, Longchuan ,  MCEACHERN, Donna ,  SUN, Duxin ,  WEN, Bo ,  LUO, Ruijuan ,  ZHAO, Ting ,  CHINNAIYAN, Arul ,  ASANGANI, Irfan, A. ,  STUCKEY, Jeanne ,  MEAGHER, Jennifer, Lynn ,  RAN, Xu ,  HU, Yang

IPC分类号： C07D487/04 ,  A61K31/519

CPC分类号： C07D519/00 ,  A61K31/437 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/538 ,  C07D487/04 ,  C07D487/14

摘要： The present disclosure provides substituted 9H-pyrimido[4,5-b]indoles and 5H-pyrido[4,3-b]indoles and related analogs represented by Formula I: and the pharmaceutically acceptable salts, hydrates, and solvates thereof, wherein R1a, A, B1, B2, G, X1, Y1, Y2, and Y3 are as defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula I to treat a condition or disorder responsive to inhibition of BET bromodomains. Compounds of the present disclosure are especially useful for treating cancer.

摘要翻译： 本公开提供取代的9H-嘧啶并[4,5-b]吲哚和5H-吡啶并[4,3-b]吲哚和由式I表示的相关类似物及其药学上可接受的盐，水合物和溶剂合物，其中R1a A，B1，B2，G，X1，Y1，Y2和Y3如说明书中所述。 本公开还涉及式I化合物用于治疗对抑制BET溴结构域有反应的病症或病症。 本公开的化合物特别可用于治疗癌症。