公开(公告)号：US20170233436A1

公开(公告)日：2017-08-17

申请号：US15587715

申请日：2017-05-05

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Yong ZHANG ,  Ivar M. MCDONALD ,  Naidu S. CHOWDARI ,  Tram N. HUYNH ,  Robert M. BORZILLERI ,  Sanjeev GANGWAR

IPC: C07K5/062

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：US20160185791A1

公开(公告)日：2016-06-30

申请号：US14911881

申请日：2014-08-14

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 ,  A61K47/48

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

Abstract: In one aspect, the present disclosure provides new analogs of uncialamycin of formulae (I) and (II). 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 comprising the compounds of formulae (I) and (II).

Abstract translation: 一方面，本公开提供式（I）和（II）的新型类似物。 本公开还提供了获得非丝氨酸霉素及其类似物的新型合成途径。 另外，本公开还描述了使用非丝氨酸霉素及其类似物的方法。 另一方面，本公开提供包含式（I）和（II）化合物的抗体 - 药物偶联物。

公开(公告)号：US20230131192A1

公开(公告)日：2023-04-27

申请号：US17793155

申请日：2021-01-26

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Christine M. TARBY ,  Matthias BROEKEMA ,  Ashvinikumar V. GAVAI ,  Sanjeev GANGWAR ,  Naidu S. CHOWDARI ,  Walter L JOHNSON ,  Murugaiah ANDAPPAN MURUGAIAH SUBBAIAH

IPC: C07D487/04 ,  A61K45/06

Abstract: Compounds according to formula I are useful as agonists of Toll-like receptor 7 (TLR7). (I) 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：US20230118688A1

公开(公告)日：2023-04-20

申请号：US17792869

申请日：2021-01-26

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Heng CHENG ,  Christine M. TARBY ,  Sanjeev GANGWAR ,  Ashvinikumar V. GAVAI ,  Walter L. JOHNSON ,  Yam B. POUDEL ,  Prasanna SIVAPRAKASAM ,  Patrice GILL ,  Andrew F. DONNELL ,  Murugaiah Andappan Murugaiah SUBBAIAH

IPC: A61K31/519 ,  C07D487/04 ,  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：US20210053979A1

公开(公告)日：2021-02-25

申请号：US17043886

申请日：2019-04-23

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Ashok V. PURANDARE ,  Honghe WAN ,  Liqi HE ,  Sanjeev GANGWAR ,  Shoshana L. POSY ,  Yam B. POUDEL ,  Prasanna SIVAPRAKASAM ,  Naidu S. CHOWDARI

IPC: C07D487/16 ,  A61K47/60

Abstract: Compounds having a structure according to formula are modulators of TLR7 activity and can be used to treat conditions amenable to treatment by the modulation of TLR7 activity.

公开(公告)号：US20200095248A1

公开(公告)日：2020-03-26

申请号：US16676870

申请日：2019-11-07

Applicant: BRISTOL-MYERS SQUIBB COMPANY

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

IPC: C07D473/18 ,  A61P37/04

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：US20200038403A1

公开(公告)日：2020-02-06

申请号：US16527802

申请日：2019-07-31

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Yam B. POUDEL ,  Sanjeev GANGWAR ,  Liqi HE ,  Prasanna SIVAPRAKASAM ,  Matthias BROEKEMA ,  Matthew COX ,  Christine M. TARBY ,  Qian ZHANG

IPC: A61K31/519 ,  C07D487/04 ,  A61K39/395 ,  A61K47/60

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：US20180110873A1

公开(公告)日：2018-04-26

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

CPC classification number: A61K47/6803 ,  C07D471/04 ,  C07D519/00 ,  C07F7/0814 ,  C07K5/06026

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：US20170326249A1

公开(公告)日：2017-11-16

申请号：US15587963

申请日：2017-05-05

Applicant: Bristol-Myers Squibb Company

Inventor： Chin PAN ,  Josephine M. CARDARELLI ,  Haichun HUANG ,  Sanjeev GANGWAR ,  Qiang CONG ,  Karla A. HENNING ,  Chetana RAO-NAIK ,  Mohan SRINIVASAN ,  Vangipuram S. RANGAN ,  Francis Y. LEE ,  Ginger C. RAKESTRAW

IPC: A61K47/68 ,  C07K16/30 ,  A61K9/00 ,  C07K5/02

CPC classification number: A61K47/6829 ,  A61K9/0019 ,  A61K47/6803 ,  A61K47/6849 ,  A61K47/6853 ,  C07K5/0205 ,  C07K16/303 ,  C07K2317/51 ,  C07K2317/515 ,  C07K2317/52 ,  C07K2317/56 ,  C07K2317/565 ,  C07K2317/77 ,  C07K2317/92

Abstract: An antibody-drug conjugate having a structure represented by formula (I) wherein m is 1, 2, 3, or 4 and Ab is an anti-glypican-3 antibody having heavy and light chain CDRs as disclosed herein.

公开(公告)号：US20170260232A1

公开(公告)日：2017-09-14

申请号：US15602156

申请日：2017-05-23

Applicant: Bristol-Myers Squibb Company

Inventor： Qiang CONG ,  Heng CHENG ,  Sanjeev GANGWAR

IPC: C07K5/117 ,  C07K5/06 ,  C07K5/078 ,  C07K5/10 ,  C07K7/06 ,  A61K38/07 ,  A61K38/05

CPC classification number: C07K5/1024 ,  A61K38/05 ,  A61K38/07 ,  A61K47/64 ,  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.