公开(公告)号：EP3262045A1

公开(公告)日：2018-01-03

申请号：EP16714606.7

申请日：2016-02-26

申请人： The Regents of The University of Michigan

发明人： WANG, Shaomeng ,  ZHAO, Yujun ,  ZHOU, Bing ,  AGUILAR, Angelo

IPC分类号： C07D487/04 ,  A61K31/519 ,  A61P35/00

CPC分类号： A61K31/437 ,  A61K31/519 ,  C07D231/38 ,  C07D261/06 ,  C07D471/04 ,  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 R 1a, W, B 1, B2, G, X 1, Y1, Y2, and Y 3 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 such as cancer. The present disclosure is also directed to the use of compound of Formula I as synthetic intermediates.

公开(公告)号：EP3131544A1

公开(公告)日：2017-02-22

申请号：EP15779988.3

申请日：2015-04-16

申请人： The Regents of the University of Michigan

发明人： WANG, Shaomeng ,  AGUILAR, Angelo ,  LIU, Liu ,  LU, Jianfeng ,  MCEACHERN, Donna

IPC分类号： A61K31/407 ,  A61P35/00 ,  C07D487/10

CPC分类号： C07D487/10 ,  A61K31/407 ,  A61K45/06 ,  A61N5/10 ,  A61N2005/1098

摘要： Inhibitors of MDM2 and MDM2-related proteins and compositions containing the same are disclosed. Methods of using the MDM2 inhibitors in the treatment of diseases and conditions wherein inhibition of an interaction between p53 and MDM2 provides a benefit, like cancers, also are disclosed.

摘要翻译： 公开了MDM2和MDM2相关蛋白的抑制剂和含有它们的组合物。 还公开了使用MDM2抑制剂治疗疾病和病症的方法，其中抑制p53和MDM2之间的相互作用提供了益处，如癌症。

公开(公告)号：EP2945940A1

公开(公告)日：2015-11-25

申请号：EP14741180.5

申请日：2014-01-15

申请人： The Regents of The University of Michigan

发明人： WANG, Shaomeng ,  CHEN, Jianfang ,  MCEACHERN, Donna ,  BAI, Longchuan ,  LIU, Liu ,  SUN, Duxin ,  LI, Xiaoqin ,  AGUILAR, Angelo

IPC分类号： C07D401/14 ,  A61K31/496 ,  A61P35/00

摘要： Inhibitors of Bcl-2/Bcl-xL and compositions containing the same are disclosed. Methods of using the Bcl-2/Bcl-xL inhibitors in the treatment of diseases and conditions wherein inhibition of Bcl-2/Bcl-xL provides a benefit, like cancers, also are disclosed.

公开(公告)号：EP3863720A1

公开(公告)日：2021-08-18

申请号：EP19794325.1

申请日：2019-10-07

申请人： The Regents Of The University Of Michigan

发明人： WANG, Shaomeng ,  AGUILAR, Angelo ,  LI, Yangbing ,  YANG, Jiuling ,  MCEACHERN, Donna

IPC分类号： A61P35/00 ,  C07D487/10

公开(公告)号：EP3860978A1

公开(公告)日：2021-08-11

申请号：EP19791390.8

申请日：2019-09-30

申请人： The Regents Of The University Of Michigan ,  Agios Pharmaceuticals, Inc.

发明人： WANG, Shaomeng ,  XU, Shilin ,  AGUILAR, Angelo ,  HUANG, Liyue ,  XU, Tianfeng ,  ZHANG, Meng ,  XU, Renqi ,  XU, Fuming ,  ZHOU, Haibin ,  LIU, Tao

IPC分类号： C07D211/34 ,  C07D401/06 ,  C07D401/14 ,  A61K31/4523 ,  A61K31/445 ,  A61P35/00

公开(公告)号：EP3459945A1

公开(公告)日：2019-03-27

申请号：EP18186324.2

申请日：2012-01-24

申请人： The Regents of The University of Michigan

发明人： WANG, Shaomeng ,  ZHOU, Haibin ,  CHEN, Jianfang ,  AGUILAR, Angelo ,  MEAGHER, Jennifer Lynn ,  SUN, Duxin ,  YANG, Chao-Yie ,  LIU, Liu ,  BAI, Longchuan ,  MCEACHERM, Donna ,  STUCKEY, Jeanne ,  LI, Xiaoqin

IPC分类号： C07D403/10 ,  C07D403/14 ,  A61K31/496 ,  A61P35/00

摘要： Inhibitors of Bcl-2/Bcl-xL and compositions containing the same are disclosed. Methods of using the Bcl-2/Bcl-xL inhibitors in the treatment of diseases and conditions wherein inhibition of Bcl-2/Bcl-xL provides a benefit, like cancers, also are disclosed.

公开(公告)号：EP3440082A1

公开(公告)日：2019-02-13

申请号：EP17718291.2

申请日：2017-04-06

申请人： The Regents of The University of Michigan

发明人： WANG, Shaomeng ,  LI, Yangbing ,  AGUILAR, Angelo ,  ZHOU, Bing ,  HU, Jiantao ,  XU, Fuming ,  QIN, Chong ,  HU, Yang ,  XIANG, Weiguo ,  REJ, Rohan ,  YANG, Jiuling ,  HAN, Xin ,  BAI, Longchuan ,  YANG, Chao-Yie

IPC分类号： C07D487/10 ,  C07D401/04 ,  A61K31/4745 ,  A61P35/00

公开(公告)号：EP3131544B1

公开(公告)日：2018-12-12

申请号：EP15779988.3

申请日：2015-04-16

申请人： The Regents of the University of Michigan

发明人： WANG, Shaomeng ,  AGUILAR, Angelo ,  LIU, Liu ,  LU, Jianfeng ,  MCEACHERN, Donna

IPC分类号： A61K31/407 ,  A61P35/00 ,  C07D487/10

CPC分类号： C07D487/10 ,  A61K31/407 ,  A61K45/06 ,  A61N5/10 ,  A61N2005/1098

摘要： Inhibitors of MDM2 and MDM2-related proteins and compositions containing the same are disclosed. Methods of using the MDM2 inhibitors in the treatment of diseases and conditions wherein inhibition of an interaction between p53 and MDM2 provides a benefit, like cancers, also are disclosed.

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。