公开(公告)号：US20180051031A1

公开(公告)日：2018-02-22

申请号：US15680424

申请日：2017-08-18

Applicant: BRISTOL-MYERS SQUIBB COMPANY ,  THE SCRIPPS RESEARCH INSTITUTE

Inventor： Fukang YANG ,  Qian ZHANG ,  Lawrence B. SNYDER ,  Sanjeev GANGWAR ,  Dale L. BOGER

IPC: C07D487/04 ,  A61K31/407 ,  A61K39/00

CPC classification number: C07D487/04 ,  A61K31/407 ,  A61K39/0011 ,  A61K39/44 ,  A61K47/6803 ,  A61K47/6851 ,  A61K47/6857 ,  A61K47/6863 ,  A61P35/00 ,  C07D519/00 ,  C07K16/30

Abstract: seco-Cyclopropapyrroloindole compounds of formula (I) where Hal, R1, R2, and R3 are as defined in the application, are potent anti-cancer agents that can be used in antibody-drug conjugates.

公开(公告)号：US20180037581A1

公开(公告)日：2018-02-08

申请号：US15785608

申请日：2017-10-17

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 ,  C07D487/04 ,  C07D519/00 ,  A61K47/68 ,  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).

公开(公告)号：US20170326247A1

公开(公告)日：2017-11-16

申请号：US15587927

申请日：2017-05-05

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Qiang CONG ,  Sanjeev GANGWAR ,  Vangipuram S. RANGAN ,  Mei-Chen SUNG

IPC: A61K47/68 ,  C07K16/28

CPC classification number: A61K47/6803 ,  A61K47/6811 ,  A61K47/6851 ,  C07K16/28 ,  C07K2317/565 ,  C07K2317/94

Abstract: The drug component of an antibody-drug conjugate having a structure according to formula (II), where Ab, m, n, R1, R2, R3, R4, and R5 are as defined in the application, exhibits unexpectedly improved stability.

公开(公告)号：US20240165249A1

公开(公告)日：2024-05-23

申请号：US18413928

申请日：2024-01-16

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Yam B. POUDEL ,  Sanjeev GANGWAR

IPC: A61K47/65 ,  A61K45/06 ,  A61K47/64 ,  A61K47/68 ,  A61P35/00

CPC classification number: A61K47/65 ,  A61K45/06 ,  A61K47/6425 ,  A61K47/6865 ,  A61P35/00

Abstract: Methods of making compounds represented by formula (I)




can be used to make antibody-drug conjugates. The conjugates so made are stable in both human and mouse serum, enabling the performance of pre-clinical studies using a mouse model.

公开(公告)号：US20230144824A1

公开(公告)日：2023-05-11

申请号：US17793248

申请日：2021-01-26

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Liqi HE ,  Ashvinikumar V. GAVAI ,  Sanjeev GANGWAR ,  Qiang CONG ,  Yam B. POUDEL ,  Prasanna SIVAPRAKASAM ,  Christine M. TARBY ,  Patrice GILL ,  Andrew F. DONNELL ,  Murugaiah ANDAPPAN MURUGAIAH SUBBAIAH

IPC: C07D487/04

CPC classification number: C07D487/04

Abstract: Compounds according to formula I or II are useful as agonists of Toll-like receptor 7 (TLR7). Such compounds can be used in cancer treatment, especially in combination with an anti-cancer immunotherapy agent, or as a vaccine adjuvant.

公开(公告)号：US20230130516A1

公开(公告)日：2023-04-27

申请号：US17792878

申请日：2021-01-26

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Qian ZHANG ,  Sanjeev GANGWAR ,  Ashvinikumar V. GAVAI ,  Qiang CONG ,  Yam B. POUDEL ,  Liqi HE ,  Prasanna SIVAPRAKASAM ,  Christine M. TARBY

IPC: A61K31/519 ,  C07D487/04 ,  C07D519/00 ,  A61K31/5377 ,  A61K39/395

Abstract: Compounds according to formula I are useful as agonists of Toll-like receptor 7 (TLR7). Such compounds can be used in cancer treatment, especially in combination with an anti-cancer immunotherapy agent, or as a vaccine adjuvant.

公开(公告)号：US20200048254A1

公开(公告)日：2020-02-13

申请号：US16659735

申请日：2019-10-22

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Liqi HE ,  Sanjeev GANGWAR ,  Shoshana L. POSY ,  Yam B. POUDEL ,  Prasanna SIVAPRAKASAM

IPC: C07D473/18 ,  A61K31/52 ,  A61K47/68 ,  A61K47/60 ,  A61P37/04

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：US20190055247A1

公开(公告)日：2019-02-21

申请号：US16103619

申请日：2018-08-14

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Liqi HE ,  Sanjeev GANGWAR ,  Yam B. POUDEL ,  Prasanna SIVAPRAKASAM

IPC: C07D473/18

Abstract: Compounds having a structure according to formula (I) or (II) where R1, R2, R3, R4, Ar and X1 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：US20190055243A1

公开(公告)日：2019-02-21

申请号：US16103210

申请日：2018-08-14

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Yam B. POUDEL ,  Sanjeev GANGWAR ,  Prasanna SIVAPRAKASAM ,  Shoshana L. POSY

IPC: C07D473/18

Abstract: Compounds having a structure according to formula (I) where R1, R2, and R3 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：US20180065976A1

公开(公告)日：2018-03-08

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

CPC classification number: C07D491/08 ,  A61K47/6803 ,  A61K47/6851

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.