公开(公告)号：US20210188845A1

公开(公告)日：2021-06-24

申请号：US17130022

申请日：2020-12-22

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Robert G. Gentles ,  Upender Velaparthi ,  Min Ding ,  Richard E. Olson ,  Scott W. Martin ,  Saumya Roy ,  Prasada Rao Jalagam ,  Jayakumar Sankara Warrier ,  Louis S. Chupak ,  Denise Christine Grunenfelder

IPC: C07D471/04 ,  C07D401/04

Abstract: Disclosed are compounds of Formula (I): or a salt thereof, wherein: X is CR6 or N; Y is CR3 or N; R1, R2, R3, R4, R5, R6, R7, and m are defined herein. Also disclosed are methods of using such compounds to inhibit the activity of one or both of diacylglycerol kinase alpha (DGKα) and diacylglycerol kinase zeta (DGKζ), and pharmaceutical compositions comprising such compounds. These compounds are useful in the treatment of viral infections and proliferative disorders, such as cancer.

公开(公告)号：US20200031832A1

公开(公告)日：2020-01-30

申请号：US16360162

申请日：2019-03-21

Applicant: Rigel Pharmaceuticals, Inc. ,  Bristol-Myers Squibb Company

Inventor： Todd Kinsella ,  Marina Gelman ,  Hui Hong ,  Ihab S. Darwish ,  Rajinder Singh ,  Jiaxin Yu ,  Robert M. Borzilleri ,  Upender Velaparthi ,  Peiying Liu ,  Chetan Padmakar Darne ,  Hasibur Rahaman ,  Jayakumar Sankara Warrier

IPC: C07D487/04 ,  C07D471/04 ,  C07D417/04 ,  C07D403/04 ,  C07D401/04

Abstract: Disclosed are imidazole and thiazole compounds, as well as pharmaceutical compositions and methods of use thereof. One embodiment is a compound having the structure and pharmaceutically acceptable salts, prodrugs and N-oxides thereof (and solvates and hydrates thereof), wherein X, A, Z, R1 and R′ are as described herein. In certain embodiments, a compound disclosed herein inhibits TGF-β, and can be used to treat disease by blocking TGF-β signaling.

公开(公告)号：US10336761B2

公开(公告)日：2019-07-02

申请号：US15746597

申请日：2016-07-21

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Lalgudi S. Harikrishnan ,  Brian E. Fink ,  Robert M. Borzilleri ,  Gopikishan Tonukunuru ,  Hasibur Rahaman ,  Jayakumar Sankara Warrier ,  Balaji Seshadri

IPC: A61K31/53 ,  A61K31/541 ,  C07D487/04

Abstract: The invention relates generally to compounds that modulate the activity of TGFβR-1 and TGFβ R-2, pharmaceutical compositions containing said compounds and methods of treating proliferative disorders and disorders of dysregulated apoptosis, such as cancer, utilizing the compounds of the invention.

公开(公告)号：US10287295B2

公开(公告)日：2019-05-14

申请号：US15860379

申请日：2018-01-02

Applicant: Rigel Pharmaceuticals, Inc. ,  Bristol-Myers Squibb Company

Inventor： Todd Kinsella ,  Marina Gelman ,  Hui Hong ,  Ihab S. Darwish ,  Rajinder Singh ,  Jiaxin Yu ,  Robert M. Borzilleri ,  Upender Velaparthi ,  Peiying Liu ,  Chetan Padmakar Darne ,  Hasibur Rahaman ,  Jayakumar Sankara Warrier

IPC: C07D487/04 ,  C07D471/04 ,  C07D401/04 ,  C07D403/04 ,  C07D417/04

Abstract: Disclosed are imidazole and thiazole compounds, as well as pharmaceutical compositions and methods of use thereof. One embodiment is a compound having the structure and pharmaceutically acceptable salts, prodrugs and N-oxides thereof (and solvates and hydrates thereof), wherein X, A, Z, R1 and R′ are as described herein. In certain embodiments, a compound disclosed herein inhibits TGF-β, and can be used to treat disease by blocking TGF-β signaling.

公开(公告)号：US20180312495A1

公开(公告)日：2018-11-01

申请号：US15767385

申请日：2016-10-13

Applicant: Bristol-Myers Squibb Company

Inventor： Imadul Islam ,  Srinivasan Thangathirupathy ,  Jayakumar Sankara Warrier ,  Srinivas Cheruku ,  Poornima Shetty ,  John E. Macor

IPC: C07D413/04 ,  A61P25/24 ,  C07D413/14 ,  C07D413/12

CPC classification number: C07D413/04 ,  C07D413/14

Abstract: The present disclosure provides compounds of Formula (I) and pharmaceutically acceptable salts thereof. The Formula (I) compounds are ligands for NR2B N-Methyl-D-aspartate (NMD A) receptor and thereby making them useful for the treatment of various disorders of the central nervous system.

公开(公告)号：US20180250283A1

公开(公告)日：2018-09-06

申请号：US15971067

申请日：2018-05-04

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Dalton King ,  Lorin A. Thompson, III ,  Jianliang Shi ,  Srinivasan Thangathirupathy ,  Jayakumar Sankara Warrier ,  Imadul Islam ,  John E. Macor

IPC: A61K31/454 ,  C07D403/04 ,  C07D401/04

CPC classification number: A61K31/454 ,  C07D401/04 ,  C07D403/04

Abstract: The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands of the NR2B receptor and may be useful for the treatment of various disorders of the central nervous system.

公开(公告)号：US20180127426A1

公开(公告)日：2018-05-10

申请号：US15860379

申请日：2018-01-02

Applicant: Rigel Pharmaceuticals, Inc. ,  Bristol-Myers Squibb Company

Inventor： Todd Kinsella ,  Marina Gelman ,  Hui Hong ,  Ihab S. Darwish ,  Rajinder Singh ,  Jiaxin Yu ,  Robert M. Borzilleri ,  Upender Velaparthi ,  Peiying Liu ,  Chetan Darne ,  Hasibur Rahaman ,  Jayakumar Sankara Warrier

IPC: C07D487/04 ,  C07D417/04 ,  C07D403/04 ,  C07D471/04 ,  C07D401/04

CPC classification number: C07D487/04 ,  C07D401/04 ,  C07D403/04 ,  C07D417/04 ,  C07D471/04

Abstract: Disclosed are imidazole and thiazole compounds, as well as pharmaceutical compositions and methods of use thereof. One embodiment is a compound having the structure and pharmaceutically acceptable salts, prodrugs and N-oxides thereof (and solvates and hydrates thereof), wherein X, A, Z, R1 and R′ are as described herein. In certain embodiments, a compound disclosed herein inhibits TGF-β, and can be used to treat disease by blocking TGF-β signaling.

公开(公告)号：US20180110766A1

公开(公告)日：2018-04-26

申请号：US15846672

申请日：2017-12-19

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Dalton King ,  Lorin A. Thompson, III ,  Jianliang Shi ,  Srinivasan Thangathirupathy ,  Jayakumar Sankara Warrier ,  Imadul Islam ,  John E. Macor

IPC: A61K31/454 ,  C07D403/04 ,  C07D401/04

CPC classification number: A61K31/454 ,  C07D401/04 ,  C07D403/04

Abstract: The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands of the NR2B receptor and may be useful for the treatment of various disorders of the central nervous system.

公开(公告)号：US20170258777A1

公开(公告)日：2017-09-14

申请号：US15604904

申请日：2017-05-25

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Dalton King ,  Lorin A. Thompson, III ,  Jianliang Shi ,  Srinivasan Thangathirupathy ,  Jayakumar Sankara Warrier ,  Imadul Islam ,  John E. Macor

IPC: A61K31/454 ,  C07D401/04 ,  C07D403/04

CPC classification number: A61K31/454 ,  C07D401/04 ,  C07D403/04

Abstract: The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands of the NR2B receptor and may be useful for the treatment of various disorders of the central nervous system.

公开(公告)号：US20160081995A1

公开(公告)日：2016-03-24

申请号：US14882041

申请日：2015-10-13

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Dalton King ,  Lorin A. Thompson, III ,  Jianliang Shi ,  Srinivasan Thangathirupathy ,  Jayakumar Sankara Warrier ,  Imadul Islam ,  John E. Macor

IPC: A61K31/454

CPC classification number: A61K31/454 ,  C07D401/04 ,  C07D403/04

Abstract: The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands of the NR2B receptor and may be useful for the treatment of various disorders of the central nervous system.