公开(公告)号：US10723736B2

公开(公告)日：2020-07-28

申请号：US16660365

申请日：2019-10-22

Applicant: BRISTOL-MYERS SQUIBB COMPANY

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

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

Abstract: Compounds having a structure according to formula (I) where R1 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：US10689382B2

公开(公告)日：2020-06-23

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: A61K31/52 ,  A61K31/522 ,  C07D473/14 ,  C07D473/18 ,  A61P37/04 ,  A61K47/68

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：US10508115B2

公开(公告)日：2019-12-17

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: A61K31/52 ,  A61K31/522 ,  C07D473/14 ,  A61P31/14 ,  A61P31/20 ,  C07D473/18 ,  A61P37/04 ,  A61K47/68

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：US10112975B2

公开(公告)日：2018-10-30

申请号：US15785675

申请日：2017-10-17

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Yong Zhang ,  Ivar M. McDonald ,  Naidu S. Chowdari ,  Tram N. Huynh ,  Robert M. Borzilleri ,  Sanjeev Gangwar

IPC: C07D487/04 ,  C07D519/00 ,  C07K5/062

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：US09777013B2

公开(公告)日：2017-10-03

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).

公开(公告)号：US20140227295A1

公开(公告)日：2014-08-14

申请号：US14177376

申请日：2014-02-11

Applicant: Bristol-Myers Squibb Company

Inventor： Qiang CONG ,  Heng Cheng ,  Sanjeev Gangwar

IPC: C07K5/117 ,  C07K7/06 ,  A61K47/48

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R 1，R 2，R 3a，R 3b，R 4，R 5，W和n如本文所定义的式（I）的调节素化合物是可用于治疗癌症的抗有丝分裂剂，特别是当与 靶向部分。

公开(公告)号：US11911483B2

公开(公告)日：2024-02-27

申请号：US17126555

申请日：2020-12-18

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Yam B. Poudel ,  Sanjeev Gangwar

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

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

Abstract: 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：US11554120B2

公开(公告)日：2023-01-17

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 ,  Naidu S. Chowdari

IPC: C07D487/04 ,  A61K31/519 ,  A61K47/60 ,  A61K39/395 ,  A61P35/00 ,  A61K31/395

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：US10927114B2

公开(公告)日：2021-02-23

申请号：US16904337

申请日：2020-06-17

Applicant: BRISTOL-MYERS SQUIBB COMPANY

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

IPC: C07D473/16 ,  C07D473/18 ,  A61P37/04 ,  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：US10919895B2

公开(公告)日：2021-02-16

申请号：US16902860

申请日：2020-06-16

Applicant: BRISTOL-MYERS SQUIBB COMPANY

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

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

Abstract: Compounds having a structure according to formula (I) where R1 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.