公开(公告)号：US20190314358A1

公开(公告)日：2019-10-17

申请号：US16454831

申请日：2019-06-27

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

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：US10292985B2

公开(公告)日：2019-05-21

申请号：US15755636

申请日：2016-08-30

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Robert M. Borzilleri ,  Brian E. Fink ,  Lalgudi S. Harikrishnan ,  Jayakumar Sankara Warrier

IPC: C07D487/04 ,  C07D519/00 ,  A61P35/00 ,  A61K31/53 ,  A61K35/02

Abstract: The invention relates generally to compounds that modulate the activity of TGFBETA R-1 and TGFBETA 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：US20180312491A1

公开(公告)日：2018-11-01

申请号：US15767386

申请日：2016-10-13

Applicant: Bristol-Myers Squibb Company

Inventor： Imadul Islam ,  Srinivasan Thangathirupathy ,  Jayakumar Sankara Warrier ,  Srinivas Cheruku ,  Poornima Shetty ,  Grandhi Venkat Ram Krishna Mohan Gupta ,  John E. Macor

IPC: C07D403/14 ,  C07D401/14 ,  C07D487/08 ,  A61P25/24 ,  A61P25/28 ,  A61P25/02 ,  A61P25/16

CPC classification number: C07D403/14 ,  A61P25/02 ,  A61P25/16 ,  A61P25/24 ,  A61P25/28 ,  C07D401/12 ,  C07D401/14 ,  C07D471/08 ,  C07D487/08

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：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：US20130085138A1

公开(公告)日：2013-04-04

申请号：US13627130

申请日：2012-09-26

Applicant: Bristol-Myers Squibb Company

Inventor： Dalton King ,  Richard E. Olson ,  John E. Macor ,  Imadul Islam ,  Srinivasan Thangathirupathy ,  Jayakumar Sankara Warrier

IPC: A61K31/4709 ,  A61K31/4245 ,  C07D413/14 ,  A61K31/501 ,  A61K31/498 ,  A61P29/00 ,  C07D487/04 ,  A61K31/519 ,  A61K31/506 ,  A61P25/24 ,  A61P25/28 ,  A61P25/16 ,  C07D413/12 ,  A61K31/538

CPC classification number: C07D413/12 ,  C07D271/113 ,  C07D401/12 ,  C07D403/08 ,  C07D413/06 ,  C07D413/08 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04

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, antagonists of the NR2B receptor and may be useful for the treatment of various disorders of the central nervous system.

Abstract translation: 本公开内容通常涉及式I化合物，包括其盐，以及使用该化合物的组合物和方法。 这些化合物是NR2B受体的配体，拮抗剂，可用于治疗中枢神经系统的各种疾病。

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.

公开(公告)号：US11352360B2

公开(公告)日：2022-06-07

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 Dame ,  Hasibur Rahaman ,  Jayakumar Sankara Warrier

IPC: C07D487/04 ,  C07D401/04 ,  C07D403/04 ,  C07D471/04 ,  A61P35/00 ,  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：US20210061802A1

公开(公告)日：2021-03-04

申请号：US17004058

申请日：2020-08-27

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

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 (DGKζ), and pharmaceutical compositions comprising such compounds. These compounds are useful in the treatment of viral infections and proliferative disorders, such as cancer.