公开(公告)号：US20160200742A1

公开(公告)日：2016-07-14

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: C07D519/00 ,  A61K47/48 ,  C07K16/28 ,  C07K16/18 ,  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。

公开(公告)号：US20160199510A1

公开(公告)日：2016-07-14

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: A61K47/48 ,  C07K5/062 ,  C07D487/04

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).

Abstract translation: 苯并二氮杂二聚体具有由其中X表示的结构，其包含杂芳族部分并且在本申请中进一步定义; R1和式（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，特别是当用于抗体 - 药物偶联物（ADC）时。

公开(公告)号：US20140135270A1

公开(公告)日：2014-05-15

申请号：US14074062

申请日：2013-11-07

Applicant: Ensemble Therapeutics Corp. ,  BRISTOL-MYERS SQUIBB COMPANY

Inventor： Robert M. Borzilleri ,  Yong Zhang ,  Michael M. Miller ,  Benjamin A. Seigal

IPC: C07K7/54

CPC classification number: C07K7/06 ,  C07D471/08 ,  C07D471/18 ,  C07D498/08 ,  C07D498/18 ,  C07D498/22 ,  C07K7/56

Abstract: There are disclosed compounds that modulate the activity of inhibitors of apoptosis (IAPs), 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.

Abstract translation: 公开了利用本发明化合物调节凋亡抑制剂（IAP）的活性的化合物，含有所述化合物的药物组合物和治疗增殖性疾病和失调性细胞凋亡障碍的疾病的方法。