公开(公告)号：US09526801B2

公开(公告)日：2016-12-27

申请号：US14994378

申请日：2016-01-13

Applicant: Bristol-Myers Squibb Company

Inventor： Ivar M. McDonald ,  Naidu S. Chowdari ,  Walter Lewis Johnson ,  Yong Zhang ,  Robert M. Borzilleri ,  Sanjeev Gangwar

IPC: C07D487/04 ,  C07D519/00 ,  A61K47/48 ,  C07K5/062

CPC classification number: C07D471/04 ,  A61K47/6803 ,  A61K47/6851 ,  A61K47/6889 ,  C07D487/04 ,  C07D519/00 ,  C07K5/06052

Abstract: Benzodiazepine dimers having a structure represented by wherein X comprises a heteroaromatic moiety and is as further defined in the application; R1 is 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 in an antibody-drug conjugate (ADC).

Abstract translation: 并且式（I），（Ia）和（Ib）中的其它变量如申请中所定义。 这种二聚体可用作抗癌剂，特别是当用于抗体 - 药物偶联物（ADC）时。

公开(公告)号：US20160108050A1

公开(公告)日：2016-04-21

申请号：US14976476

申请日：2015-12-21

Applicant: Bristol-Myers Squibb Company

Inventor： Ashok Vinayak Purandare ,  Brian E. Fink ,  Walter Lewis Johnson ,  Amy C. Hart ,  Liqi He ,  Tram N. Huynh ,  Jennifer lnghrim ,  Harold Mastalerz ,  Xiaopeng Sang ,  Christine M. Tarby ,  Honghe Wan ,  Wayne Vaccaro ,  Guifen Zhang ,  Yufen Zhao ,  Kurt Zimmermann ,  Yong Zhang ,  Libing Chen ,  Bin Chen ,  John S. Tokarski ,  Ashvinikumar V. Gavai

IPC: C07D487/04 ,  C07F9/6561 ,  C07F7/18 ,  C07D519/00

CPC classification number: C07D487/04 ,  A61K31/53 ,  A61K31/5377 ,  A61K31/5383 ,  A61K31/541 ,  A61K31/55 ,  A61K31/551 ,  A61K31/675 ,  A61K45/06 ,  C07D471/10 ,  C07D487/08 ,  C07D487/10 ,  C07D487/22 ,  C07D498/04 ,  C07D519/00 ,  C07F7/1804 ,  C07F9/6521 ,  C07F9/6561 ,  C07F9/65616

Abstract: The invention provides compounds of Formula (I) and pharmaceutically acceptable salts thereof. The Formula (I) imidazotriazines inhibit protein kinase activity thereby making them useful as anticancer agents.

公开(公告)号：US10112975B2

公开(公告)日：2018-10-30

申请号：US15785675

申请日：2017-10-17

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Yong Zhang ,  Ivar M. McDonald ,  Naidu S. Chowdari ,  Tram N. Huynh ,  Robert M. Borzilleri ,  Sanjeev Gangwar

IPC: C07D487/04 ,  C07D519/00 ,  C07K5/062

Abstract: Benzodiazepine dimers having a structure represented by wherein R1 is wherein the variables in formulae (I), (Ia), and (Ib) are as defined in the application. Such dimers are useful as anti-cancer agents, especially when used 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.

公开(公告)号：US20140309265A1

公开(公告)日：2014-10-16

申请号：US14356911

申请日：2012-11-09

Applicant: Ensemble Therapeutics ,  Bristol-Myers Squibb Company

Inventor： Benjamin Adam Seigal ,  Nicholas Terrett ,  Percy H. Carter ,  Robert M. Borzilleri ,  Yong Zhang ,  Michael M. Miller

IPC: C07D498/22 ,  C07D498/16

CPC classification number: C07D498/22 ,  A61K38/00 ,  C07D249/04 ,  C07D498/16 ,  C07K5/1008 ,  C07K7/56 ,  Y02A50/411 ,  Y02A50/414

Abstract: The invention relates generally to macrocyclic compounds and their therapeutic use. More particularly, the invention relates to macrocyclic compounds that modulate the activity of inhibitors of apoptosis (IAPs) and/or are useful in the treatment of medical conditions, such as cancer.

Abstract translation: 本发明一般涉及大环化合物及其治疗用途。 更具体地，本发明涉及调节凋亡抑制剂（IAP）的活性的大环化合物和/或可用于治疗诸如癌症的医学病症。

公开(公告)号：US20200253997A1

公开(公告)日：2020-08-13

申请号：US16642424

申请日：2018-08-30

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Dharmpal S. Dodd ,  Brian E. Fink ,  Yong Zhang

IPC: A61K31/708 ,  C07H21/04 ,  A61K39/395

Abstract: The present invention is directed to compounds of the formula (I) wherein all substituents are defined herein, as well as pharmaceutically acceptable compositions comprising compounds of the invention and methods of using said compositions in the treatment of various disorders.

公开(公告)号：US09676794B2

公开(公告)日：2017-06-13

申请号：US15351843

申请日：2016-11-15

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Yong Zhang ,  Ivar M. McDonald ,  Naidu S. Chowdari ,  Tram N. Huynh ,  Robert M. Borzilleri ,  Sanjeev Gangwar

IPC: C07D487/04 ,  C07D519/00

CPC classification number: C07K5/06052 ,  A61K47/6843 ,  A61K47/6849 ,  C07D487/04 ,  C07D519/00 ,  C07K16/18 ,  C07K16/28 ,  C07K16/30 ,  C07K2317/76

Abstract: Benzodiazepine dimers having a structure represented by wherein R1 is wherein the variables in formulae (I), (Ia), and (Ib) are as defined in the application. Such dimers are useful as anti-cancer agents, especially when used in an antibody-drug conjugate (ADC).

公开(公告)号：US09676775B2

公开(公告)日：2017-06-13

申请号：US15351955

申请日：2016-11-15

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Ivar M. McDonald ,  Naidu S. Chowdari ,  Walter Lewis Johnson ,  Yong Zhang ,  Robert M. Borzilleri ,  Sanjeev Gangwar

IPC: C07D487/04 ,  C07D519/00 ,  C07D471/04

CPC classification number: C07D471/04 ,  A61K47/6803 ,  A61K47/6851 ,  A61K47/6889 ,  C07D487/04 ,  C07D519/00 ,  C07K5/06052

Abstract: Benzodiazepine dimers having a structure represented by wherein X comprises a heteroaromatic moiety and is as further defined in the application; R1 is 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 in an antibody-drug conjugate (ADC).

公开(公告)号：US09527871B2

公开(公告)日：2016-12-27

申请号：US14994296

申请日：2016-01-13

Applicant: Bristol-Myers Squibb Company

Inventor： Yong Zhang ,  Ivar M. McDonald ,  Naidu S. Chowdari ,  Tram N. Huynh ,  Robert M. Borzilleri ,  Sanjeev Gangwar

IPC: C07D487/04 ,  C07D519/00 ,  A61K47/48 ,  C07K16/18 ,  C07K16/28 ,  C07K16/30

CPC classification number: C07K5/06052 ,  A61K47/6843 ,  A61K47/6849 ,  C07D487/04 ,  C07D519/00 ,  C07K16/18 ,  C07K16/28 ,  C07K16/30 ,  C07K2317/76

Abstract: Benzodiazepine dimers having a structure represented by wherein R1 is wherein the variables in formulae (I), (Ia), and (Ib) are as defined in the application. Such dimers are useful as anti-cancer agents, especially when used in an antibody-drug conjugate (ADC).

Abstract translation: 具有由其中R1表示的结构的苯并二氮杂二聚体，其中式（I），（Ia）和（Ib）中的变量如本申请中所定义。 这种二聚体可用作抗癌剂，特别是当用于抗体 - 药物偶联物（ADC）时。