公开(公告)号：US20180111936A1

公开(公告)日：2018-04-26

申请号：US15558692

申请日：2016-03-17

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Hai-Yun XIAO ,  Murali T.G. DHAR ,  Jingwu DUAN ,  Bin JIANG ,  Andrew J. TEBBEN

IPC: C07D471/14 ,  A61P37/00 ,  A61P29/00

CPC classification number: C07D471/14 ,  A61P29/00 ,  A61P37/00 ,  C07D487/06

Abstract: Disclosed are compounds of Formula (I) or a salt thereof, wherein: X is N; W is: (i) —(CR3R3)1-4—; (ii) —(CR3R3)x—Y—(CR3R3)y—; Or (iii) —Y—(CR3R3)2—Y—; and Y, R1, R2, R3, R5, R6, R8, x, and y are defined herein. Also disclosed are methods of using such compounds as modulators of TNFα, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating inflammatory and autoimmune diseases.

公开(公告)号：US20160376288A1

公开(公告)日：2016-12-29

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: C07D498/22 ,  C07K16/30 ,  A61K47/48

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).

Abstract translation: 并且式I，Ia和Ib中的其它变量如本申请中所定义。 这种二聚体可用作抗癌剂，特别是用作抗体 - 药物偶联物（ADC）中的药物成分时。

公开(公告)号：US20180111937A1

公开(公告)日：2018-04-26

申请号：US15558708

申请日：2016-03-17

Applicant: Bristol-Myers Squibb Company

Inventor： Stephen T. WROBLESKI ,  Gregory D. BROWN ,  Shuqun LIN ,  Jingwu DUAN ,  Zhonghui LU ,  Murali T.G. DHAR ,  Hai-Yun XIAO ,  Andrew J. TEBBEN

IPC: C07D471/14 ,  A61P29/00 ,  A61P37/00 ,  C07D491/147

CPC classification number: C07D471/14 ,  A61P29/00 ,  A61P37/00 ,  C07D487/06 ,  C07D491/147

Abstract: Disclosed are compounds of Formula (I) or a salt thereof, wherein: X is N; W is: —(CR3R3)2-5-, —(CR3R3)x-Y—(CR3R3)y-, —Y—(CR3R3)2-3-Y—, —CR3R3-Y—(CR3R3)2-Y—, —Y—(CR3R3)2-Y—CR3R3-; and Y, R1, R2, R3, R5, R6, R8, x, and y are define herein. Also disclosed are methods of using such compounds as modulators of TNFα, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating inflammatory and autoimmune diseases.

公开(公告)号：US20170260205A1

公开(公告)日：2017-09-14

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 STANG ,  Andrew F. DONNELL ,  Gretchen M. SCHROEDER ,  Heidi L. PEREZ ,  Donna D. WEI

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

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).