公开(公告)号：US20190055245A1

公开(公告)日：2019-02-21

申请号：US16103581

申请日：2018-08-14

Applicant: BRISTOL-MYERS SQUIBB COMPANY

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

IPC: C07D473/18 ,  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：US20190055244A1

公开(公告)日：2019-02-21

申请号：US16103511

申请日：2018-08-14

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, R5X1, 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：US20230122249A1

公开(公告)日：2023-04-20

申请号：US17793162

申请日：2021-01-26

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Yam B. POUDEL ,  Matthew COX ,  Liqi HE ,  Daniel O'MALLEY ,  Ashvinikumar V. GAVAI ,  Sanjeev GANGWAR ,  Matthias BROEKEMA ,  Prasanna SIVAPRAKASAM ,  Christine M. TARBY ,  Murugaiah ANDAPPAN MURUGAIAH SUBBAIAH,Murugaiah

IPC: C07D487/04 ,  C07D519/00

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：US20230041738A1

公开(公告)日：2023-02-09

申请号：US17793174

申请日：2021-01-26

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Yam B. POUDEL ,  Matthew COX ,  Liqi HE ,  Ashvinikumar V. GAVAI ,  Sanjeev GANGWAR ,  Mathias BROEKEMA ,  Christine M. TARBY ,  Murugaiah ANDAPPAN MURUGAIAH SUBBAIAH

IPC: A61K31/519 ,  C07D519/00 ,  C07D487/04 ,  A61K31/5386 ,  A61K39/395

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：US20200317672A1

公开(公告)日：2020-10-08

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: C07D473/18 ,  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：US20200255429A1

公开(公告)日：2020-08-13

申请号：US16865009

申请日：2020-05-01

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：US20200048255A1

公开(公告)日：2020-02-13

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 ,  A61K47/68 ,  A61K47/60 ,  A61P37/04

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：US20200039986A1

公开(公告)日：2020-02-06

申请号：US16529457

申请日：2019-08-01

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Yam B. POUDEL ,  Sanjeev Gangwar ,  Liqi He ,  Prasanna Sivaprakasam

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

Abstract: Compounds according to formula 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：US20200024279A1

公开(公告)日：2020-01-23

申请号：US16583869

申请日：2019-09-26

Applicant: BRISTOL-MYERS SQUIBB COMPANY

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

IPC: C07D473/18 ,  A61P37/04

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：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.