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.

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。