公开(公告)号：US20200017501A1

公开(公告)日：2020-01-16

申请号：US16578733

申请日：2019-09-23

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Ian S. YOUNG ,  Sanjeev Gangwar ,  Shoshana L. Posy ,  Yam B. Poudel ,  Prasanna Sivaprakasam

IPC: C07D473/18

Abstract: Compounds having a structure according to formula (I), (II), or (III) where R1, R2, R3, R5 X1, X2, and X3 are as defined herein, are agonists for the Toll-like receptor 7 (TLR7) and can be used as adjuvants for stimulating the immune system. Some such compounds can be used in conjugates for targeted delivery to the organ or tissue of intended action.

公开(公告)号：US10398783B2

公开(公告)日：2019-09-03

申请号：US15789027

申请日：2017-10-20

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Ivar M. McDonald ,  Prasanna Sivaprakasam ,  Christiana I. Iwuagwu ,  Kevin M. Peese ,  Heng Cheng ,  Naidu S. Chowdari ,  Sanjeev Gangwar

IPC: C07D471/04 ,  A61K47/68 ,  C07D519/00 ,  C07F7/08 ,  C07K5/062

Abstract: A compound capable of inhibiting cell proliferation, having a structure according to formula (I) wherein the variables in formula (I) are as defined in the specification. Such compounds are useful as anti-cancer agents, especially in antibody-drug conjugates.

公开(公告)号：US10233192B2

公开(公告)日：2019-03-19

申请号：US15677959

申请日：2017-08-15

Applicant: WILLIAM MARSH RICE UNIVERSITY ,  BRISTOL-MYERS SQUIBB COMPANY ,  THE SCRIPPS RESEARCH INSTITUTE

Inventor： Kyriacos C. Nicolaou ,  Min Lu ,  Debashis Mandal ,  Sanjeev Gangwar ,  Naidu S. Chowdari ,  Yam B. Poudel

IPC: C07D491/08 ,  A61K47/68

Abstract: In one aspect, the present disclosure provides new analogs of uncialamycin. The present disclosure also provides novel synthetic pathways to obtaining uncialamycin and analogs thereof. Additionally, the present disclosure also describes methods of use of uncialamycin and analogs thereof. In another aspect, the present disclosure provides antibody-drug conjugates which may be used to treat cancer or another disease or disorder.

公开(公告)号：US20190055246A1

公开(公告)日：2019-02-21

申请号：US16103601

申请日：2018-08-14

Applicant: Bristol-Myers Squibb Company

Inventor： Liqi HE ,  Sanjeev Gangwar ,  Shoshana L. Posy ,  Yam B. Poudel ,  Prasanna Sivaprakasam

IPC: C07D473/18 ,  A61K47/60 ,  A61K47/68 ,  A61K31/52

Abstract: Compounds having a structure according to formula (I) or (II) where R1, R2, and Ar are as defined herein, are agonists for the Toll-like receptor 7 (TLR7) and can be used as adjuvants for stimulating the immune system. Some such compounds can be used in conjugates for targeted delivery to the organ or tissue of intended action.

公开(公告)号：US09822112B2

公开(公告)日：2017-11-21

申请号：US15587679

申请日：2017-05-05

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：US20170233392A1

公开(公告)日：2017-08-17

申请号：US15587679

申请日：2017-05-05

Applicant: BRISTOL-MYERS SQUIBB COMPANY

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

IPC: 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：US09688721B2

公开(公告)日：2017-06-27

申请号：US15171592

申请日：2016-06-02

Applicant: Bristol-Myers Squibb Company

Inventor： Qiang Cong ,  Heng Cheng ,  Sanjeev Gangwar

IPC: A61K38/00 ,  C07K5/117 ,  A61K47/48 ,  C07K7/06 ,  C07K5/10 ,  A61K38/07 ,  C07K5/06 ,  C07K5/078 ,  A61K38/05 ,  C07K5/107

CPC classification number: C07K5/1024 ,  A61K38/05 ,  A61K38/07 ,  A61K47/48246 ,  A61K47/48415 ,  A61K47/48569 ,  A61K47/48592 ,  A61K47/48607 ,  A61K47/48615 ,  A61K47/48638 ,  A61K47/6811 ,  A61K47/6851 ,  A61K47/6857 ,  A61K47/6861 ,  A61K47/6863 ,  A61K47/6869 ,  C07K5/06 ,  C07K5/06139 ,  C07K5/06165 ,  C07K5/10 ,  C07K5/1016 ,  C07K7/06

Abstract: Tubulysin compounds of the formula (I) where R1, R2 R3a, R3b, R4, R5, W, and n are as defined herein, are anti-mitotic agents that can be used in the treatment of cancer, especially when conjugated to a targeting moiety.

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：US20160264624A1

公开(公告)日：2016-09-15

申请号：US15171592

申请日：2016-06-02

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Qiang CONG ,  Heng Cheng ,  Sanjeev Gangwar

IPC: C07K5/117

CPC classification number: C07K5/1024 ,  A61K38/05 ,  A61K38/07 ,  A61K47/48246 ,  A61K47/48415 ,  A61K47/48569 ,  A61K47/48592 ,  A61K47/48607 ,  A61K47/48615 ,  A61K47/48638 ,  A61K47/6811 ,  A61K47/6851 ,  A61K47/6857 ,  A61K47/6861 ,  A61K47/6863 ,  A61K47/6869 ,  C07K5/06 ,  C07K5/06139 ,  C07K5/06165 ,  C07K5/10 ,  C07K5/1016 ,  C07K7/06

Abstract: Tubulysin compounds of the formula (I) where R1, R2 R3a, R3b, R4, R5, W, and n are as defined herein, are anti-mitotic agents that can be used in the treatment of cancer, especially when conjugated to a targeting moiety.

Abstract translation: 其中R1，R2 R3a，R3b，R4，R5，W和n如本文所定义，是可用于治疗癌症的抗有丝分裂剂，特别是当与靶向部分缀合时。

公开(公告)号：US09382289B2

公开(公告)日：2016-07-05

申请号：US14605549

申请日：2015-01-26

Applicant: Bristol-Myers Squibb Company

Inventor： Qiang Cong ,  Heng Cheng ,  Sanjeev Gangwar

IPC: A61K38/00 ,  C07K5/117 ,  A61K47/48 ,  C07K7/06 ,  C07K5/10 ,  A61K38/07 ,  C07K5/06 ,  C07K5/078 ,  A61K38/05 ,  C07K5/107

CPC classification number: C07K5/1024 ,  A61K38/05 ,  A61K38/07 ,  A61K47/48246 ,  A61K47/48415 ,  A61K47/48569 ,  A61K47/48592 ,  A61K47/48607 ,  A61K47/48615 ,  A61K47/48638 ,  A61K47/6811 ,  A61K47/6851 ,  A61K47/6857 ,  A61K47/6861 ,  A61K47/6863 ,  A61K47/6869 ,  C07K5/06 ,  C07K5/06139 ,  C07K5/06165 ,  C07K5/10 ,  C07K5/1016 ,  C07K7/06

Abstract: Tubulysin compounds of the formula (I) where R1, R2, R3a, R3b, R4, R5, W, and n are as defined herein, are anti-mitotic agents that can be used in the treatment of cancer, especially when conjugated to a targeting moiety.