公开(公告)号：US20200109140A1

公开(公告)日：2020-04-09

申请号：US16452679

申请日：2019-06-26

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Upender VELAPARTHI ,  Louis S. Chupak ,  Chetan Padmakar Darne ,  Min Ding ,  Robert G. Gentles ,  Yazhong Huang ,  Manjunatha Narayana Rao Kamble ,  Scott W. Martin ,  Raju Mannoori ,  Ivar M. McDonald ,  Richard E. Olson ,  Hasibur Rahaman ,  Prasada Rao Jalagam ,  Saumya Roy ,  Gopikishan Tonukunuru ,  Sivasudar Velaiah ,  Jayakumar Sankara Warrier ,  Xiaofan Zheng ,  John S. Tokarski ,  Bireshwar Dasgupta ,  Kotha Rathnakar Reddy ,  Thiruvenkadam Raja

IPC: C07D471/04

Abstract: Disclosed are compounds of Formula (I): or a salt thereof, wherein: R1, R2, R3, R4, R5, 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：US09981944B2

公开(公告)日：2018-05-29

申请号：US15043729

申请日：2016-02-15

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

Inventor： Pingyu Ding ,  Marina Gelman ,  Todd Kinsella ,  Rajinder Singh ,  Somasekhar Bhamidipati ,  Upender Velaparthi ,  Robert M. Borzilleri ,  Hasibur Rahaman ,  Jayakumar Sankara Warrier

IPC: C07D401/04 ,  C07D471/04 ,  C07D487/04 ,  C07B59/00 ,  C07C53/06 ,  C07C53/18 ,  C07D401/14

CPC classification number: C07D401/14 ,  C07B59/002 ,  C07B2200/05 ,  C07C53/06 ,  C07C53/18 ,  C07D471/04 ,  C07D487/04

Abstract: Disclosed are 2,2′-bipyridyl 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 R1, Z and n are as described herein. In certain embodiments, a compound disclosed herein inhibits GDF8, and can be used to treat disease by blocking GDF8 signaling.

公开(公告)号：US20230094758A1

公开(公告)日：2023-03-30

申请号：US17785648

申请日：2020-12-22

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Upender Velaparthi ,  Richard E. Olson ,  Jayakumar Sankara Warrier ,  Hasibur Rahaman

IPC: C07D239/80

Abstract: Disclosed are compounds of Formula (I): (I) or a salt thereof, wherein: R1, R2, R4, R5, R6, 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：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：US11713316B2

公开(公告)日：2023-08-01

申请号：US17164009

申请日：2021-02-01

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Upender Velaparthi ,  Louis S. Chupak ,  Chetan Padmakar Darne ,  Min Ding ,  Robert G. Gentles ,  Yazhong Huang ,  Manjunatha Narayana Rao Kamble ,  Scott W. Martin ,  Raju Mannoori ,  Ivar M. McDonald ,  Richard E. Olson ,  Hasibur Rahaman ,  Prasada Rao Jalagam ,  Saumya Roy ,  Gopikishan Tonukunuru ,  Sivasudar Velaiah ,  Jayakumar Sankara Warrier ,  Xiaofan Zheng ,  John S. Tokarski ,  Bireshwar Dasgupta ,  Kotha Rathnakar Reddy ,  Thiruvenkadam Raja

IPC: C07D403/04 ,  C07D471/04 ,  C07D487/04 ,  A61K31/196

CPC classification number: C07D471/04

Abstract: Disclosed are compounds of Formula (I):




or a salt thereof, wherein: R1, R2, R3, R4, R5, 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：US20230151007A1

公开(公告)日：2023-05-18

申请号：US17983097

申请日：2022-11-08

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Upender Velaparthi ,  Richard E. Olson ,  Chetan Padmakar Darne ,  Bireshwar Dasgupta ,  Jayakumar Sankara Warrier ,  Hasibur Rahaman ,  Prasada Rao Jalagam ,  Saumya Roy ,  Denise Christine Grunenfelder

IPC: C07D471/04

CPC classification number: C07D471/04

Abstract: Disclosed are compounds of Formula (I):





or a salt thereof, wherein: R1, R2, R4, R5, 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 (DGKξ), 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：US20220324859A1

公开(公告)日：2022-10-13

申请号：US17164009

申请日：2021-02-01

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Upender Velaparthi ,  Louis S. Chupak ,  Chetan Padmakar Darne ,  Min Ding ,  Robert G. Gentles ,  Yazhong Huang ,  Manjunatha Narayana Rao Kamble ,  Scott W. Martin ,  Raju Mannoori ,  Ivar M. McDonald ,  Richard E. Olson ,  Hasibur Rahaman ,  Prasada Rao Jalagam ,  Saumya Roy ,  Gopikishan Tonukunuru ,  Sivasudar Velaiah ,  Jayakumar Sankara Warrier ,  Xiaofan Zheng ,  John S. Tokarski ,  Bireshwar Dasgupta ,  Kotha Rathnakar Reddy ,  Thiruvenkadam Raja

IPC: C07D471/04

Abstract: Disclosed are compounds of Formula (I): or a salt thereof, wherein: R1, R2, R3, R4, R5, 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.