公开(公告)号：EP4129999A1

公开(公告)日：2023-02-08

申请号：EP22179906.7

申请日：2017-08-04

申请人： The Regents Of The University Of Michigan

发明人： WANG, Shaomeng ,  CHEN, Jianyong

IPC分类号： C07D471/04 ,  A61K31/437 ,  A61P35/00

摘要： The present disclosure provides compounds having Formula I-A:

and the pharmaceutically acceptable salts and solvates thereof, wherein A, X 1 , X 2 , X 3 R 1a , R 1b , E, and

are as defined as set forth in the specification. The present disclosure also provides compounds of Formula I-A for use to treat a disease, disorder, or condition responsive to Bcl-2 protein inhibition such as cancer.

公开(公告)号：EP4021580A1

公开(公告)日：2022-07-06

申请号：EP20775094.4

申请日：2020-08-27

申请人： The Regents Of The University Of Michigan

发明人： WANG, Shaomeng ,  XU, Tianfeng ,  WANG, Mingliang ,  HU, Jiantao ,  HAN, Xin ,  XIANG, Weiguo ,  REJ, Rohan

IPC分类号： A61P35/00 ,  C07D401/04 ,  C07D471/04 ,  C07D471/10 ,  C07D487/04 ,  C07D487/10 ,  A61K31/454 ,  A61K31/4545

公开(公告)号：EP3600313A1

公开(公告)日：2020-02-05

申请号：EP18776755.3

申请日：2018-03-30

申请人： The Regents of The University of Michigan

发明人： WANG, Shaomeng ,  AGUILAR, Angelo ,  XU, Shilin ,  HUANG, Liyue ,  STUCKEY, Jeanne ,  TIANFENG, Xu

IPC分类号： A61K31/445 ,  C07D211/26 ,  C07D401/06

公开(公告)号：EP3442976A1

公开(公告)日：2019-02-20

申请号：EP17717993.4

申请日：2017-04-06

申请人： The Regents of The University of Michigan

发明人： WANG, Shaomeng ,  ZHOU, Bing ,  XU, Fuming ,  HU, Jiantao ,  BAI, Longchuan ,  YANG, Chao-Yie

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

公开(公告)号：EP2707372B1

公开(公告)日：2016-12-21

申请号：EP12782304.5

申请日：2012-05-11

申请人： The Regents of The University of Michigan ,  SANOFI

发明人： WANG, Shaomeng ,  SUN, Wei ,  AGUILAR, Angelo ,  GARCIA-ECHEVERRIA, Carlos

IPC分类号： C07D487/10 ,  C07D413/12 ,  A61K31/407 ,  A61P35/00

CPC分类号： C07D487/10

公开(公告)号：EP2888265A1

公开(公告)日：2015-07-01

申请号：EP13831176.6

申请日：2013-08-16

申请人： The Regents of The University of Michigan

发明人： WANG, Shaomeng ,  SHENG, Rong ,  SUN, Haiying ,  LIU, Liu ,  LU, Jianfeng ,  MCEACHERN, Donna

IPC分类号： C07D487/04 ,  A61K31/395 ,  A61P35/00

CPC分类号： C07D519/00 ,  A61K31/407 ,  A61K31/496 ,  A61K45/06

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

公开(公告)号：EP2019671B1

公开(公告)日：2014-09-24

申请号：EP07794581.4

申请日：2007-05-04

申请人： THE REGENTS OF THE UNIVERSITY OF MICHIGAN

发明人： WANG, Shaomeng ,  SUN, Haiying ,  QIN, Dongguang ,  NIKOLOVSKA-COLESKA, Zaneta ,  QIU, Su ,  PENG, Yuefeng ,  CAI, Qian , 

IPC分类号： C07D487/04 ,  C07D519/00 ,  A61K31/407 ,  A61K31/4192 ,  A61K31/496 ,  A61K31/395 ,  A61K38/19

CPC分类号： C07D519/00 ,  A61K38/191 ,  C07D487/04

公开(公告)号：EP2668180A2

公开(公告)日：2013-12-04

申请号：EP12739376.7

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

CPC分类号： C07D239/28 ,  C07D207/34 ,  C07D231/12 ,  C07D233/28 ,  C07D233/56 ,  C07D261/08 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D471/04

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：EP2491041A2

公开(公告)日：2012-08-29

申请号：EP10825596.9

申请日：2010-10-20

申请人： The Regents of the University of Michigan

发明人： WANG, Shaomeng ,  SUN, Haiying

IPC分类号： C07D487/04 ,  C07D403/14 ,  C07D245/04 ,  A61P35/00

CPC分类号： C07D519/00 ,  C07D487/04

摘要： The invention relates to diazo bicyclic Smac mimetics that are tethered through a covalent linker to give a bivalent species. Bivalent diazo bicyclic Smac mimetics function as inhibitors of Inhibitor of Apoptosis Proteins (IAPs). The invention also relates to the use of bivalent diazo bicyclic Smac mimetics for inducing or sensitizing cells to the induction of apoptotic cell death. Thus, compounds of the invention are useful in the treatment, amelioration, or prevention of hyperproliferative diseases such as cancer.

公开(公告)号：EP2063887A2

公开(公告)日：2009-06-03

申请号：EP07837579.7

申请日：2007-08-31

申请人： The Regents of the University of Michigan

发明人： WANG, Shaomeng ,  QIN, Dongguang ,  CHEN, Jianyong ,  YU, Shanghai

IPC分类号： A61K31/407 ,  A61K31/497 ,  C07D209/96 ,  C07D211/06 ,  A61K31/5377

CPC分类号： C07D487/10

摘要： The invention relates to small molecules which function as inhibitors of the interaction between p53 and MDM2. The invention also relates to the use of these compounds for inhibiting cell growth, inducing cell death, inducing cell cycle arrest and/or sensitizing cells to additional agent(s).