公开(公告)号：US09688694B2

公开(公告)日：2017-06-27

申请号：US15189388

申请日：2016-06-22

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Yong Zhang ,  Robert M. Borzilleri ,  Andrew J. Tebben ,  Erik M. Stang ,  Andrew F. Donnell ,  Gretchen M. Schroeder ,  Heidi L. Perez ,  Donna D. Wei

IPC: C07D487/04 ,  C07D519/00 ,  C07D498/22 ,  A61K31/5513 ,  A61K31/5517 ,  A61K47/48 ,  C07K16/30

CPC classification number: C07D498/22 ,  A61K31/5513 ,  A61K31/5517 ,  A61K47/48384 ,  A61K47/48569 ,  A61K47/48592 ,  A61K47/48615 ,  A61K47/48638 ,  A61K47/48715 ,  A61K47/6801 ,  A61K47/6803 ,  A61K47/6851 ,  A61K47/6857 ,  A61K47/6859 ,  A61K47/6863 ,  A61K47/6869 ,  A61K47/6889 ,  C07D519/00 ,  C07K16/30 ,  C07K16/3023 ,  C07K16/3046 ,  C07K16/3069

Abstract: Macrocyclic benzodiazepine dimers having a structure represented by formula I where A and B are independently according to formulae Ia or Ib and the other variables in formulae I, Ia, and Ib are as defined in the application. Such dimers are useful as anti-cancer agents, especially when used as the drug component in an antibody-drug conjugate (ADC).

公开(公告)号：US09902740B2

公开(公告)日：2018-02-27

申请号：US15606512

申请日：2017-05-26

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Yong Zhang ,  Robert M. Borzilleri ,  Andrew J. Tebben ,  Erik M. Stang ,  Andrew F. Donnell ,  Gretchen M. Schroeder ,  Heidi L. Perez ,  Donna D. Wei

IPC: C07D519/00 ,  C07D498/22 ,  A61K47/48 ,  C07K16/30 ,  A61K31/5513 ,  A61K31/5517

CPC classification number: C07D498/22 ,  A61K31/5513 ,  A61K31/5517 ,  A61K47/48384 ,  A61K47/48569 ,  A61K47/48592 ,  A61K47/48615 ,  A61K47/48638 ,  A61K47/48715 ,  A61K47/6801 ,  A61K47/6803 ,  A61K47/6851 ,  A61K47/6857 ,  A61K47/6859 ,  A61K47/6863 ,  A61K47/6869 ,  A61K47/6889 ,  C07D519/00 ,  C07K16/30 ,  C07K16/3023 ,  C07K16/3046 ,  C07K16/3069

Abstract: Macrocyclic benzodiazepine dimers having a structure represented by formula I where A and B are independently according to formulae Ia or Ib and the other variables in formulae I, Ia, and Ib are as defined in the application. Such dimers are useful as anti-cancer agents, especially when used as the drug component in an antibody-drug conjugate (ADC).

公开(公告)号：US09708316B2

公开(公告)日：2017-07-18

申请号：US14977709

申请日：2015-12-22

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Brian E. Fink ,  Yufen Zhao ,  Robert M. Borzilleri ,  Liping Zhang ,  Kyoung S. Kim ,  Muthoni G. Kamau ,  Andrew J. Tebben ,  Yong Zhang ,  Andrew F. Donnell

IPC: A61K31/4709 ,  A61K31/501 ,  C07D487/04 ,  C07D471/04 ,  A61K31/5377 ,  A61K31/437 ,  A61K31/496 ,  A61K31/4985 ,  A61K31/506 ,  A61K31/541

CPC classification number: C07D471/04 ,  A61K31/437 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/4985 ,  A61K31/501 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/541 ,  C07D487/04 ,  Y02P20/582

Abstract: The invention relates generally to compounds that modulate the activity of TGFβR-1 and TGFβR-2, pharmaceutical compositions containing said compounds and methods of treating proliferative disorders and disorders of dysregulated apoptosis, such as cancer, utilizing the compounds of the invention.