公开(公告)号：US20200071304A1

公开(公告)日：2020-03-05

申请号：US16502684

申请日：2019-07-03

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 ,  C07D401/12 ,  C07D471/08 ,  A61P25/28 ,  A61P25/02 ,  A61P25/24 ,  A61P25/16 ,  C07D401/14 ,  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：US20190337942A1

公开(公告)日：2019-11-07

申请号：US16475413

申请日：2018-01-03

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Robert M. Borzilleri ,  Upender Velaparthi ,  Chetan Padmakar Darne ,  Peiying Liu ,  Manjunatha Narayana Rao Kamble ,  Balaji Seshadri ,  Raju Mannoori ,  Hasibur Rahaman ,  Jayakumar Sankara Warrier

IPC: C07D471/04 ,  C07D401/14 ,  C07D487/04

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

公开(公告)号：US10344020B2

公开(公告)日：2019-07-09

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 ,  C07D401/12 ,  C07D471/08 ,  A61P25/28 ,  A61P25/02 ,  A61P25/24 ,  A61P25/16 ,  C07D401/14 ,  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：US20190117638A1

公开(公告)日：2019-04-25

申请号：US16225850

申请日：2018-12-19

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

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：US09884868B2

公开(公告)日：2018-02-06

申请号：US15054895

申请日：2016-02-26

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 ,  C07D471/04 ,  C07D401/04 ,  C07D403/04 ,  C07D417/04

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：US20180000807A1

公开(公告)日：2018-01-04

申请号：US15706172

申请日：2017-09-15

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：US09221796B2

公开(公告)日：2015-12-29

申请号：US14589205

申请日：2015-01-05

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: 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.

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，可用于治疗中枢神经系统的各种疾病。

公开(公告)号：US20150191452A1

公开(公告)日：2015-07-09

申请号：US14589205

申请日：2015-01-05

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: 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.

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，可用于治疗中枢神经系统的各种疾病。

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：US20230061608A1

公开(公告)日：2023-03-02

申请号：US17786239

申请日：2020-12-22

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Louis S. Chupak ,  Richard E. Olson ,  Upender Velaparthi ,  Xiaofan Zheng ,  Robert G. Gentles ,  Min Ding ,  Jayakumar Sankara Warrier

IPC: C07D401/04 ,  C07D401/14

Abstract: Disclosed are compounds of Formula (I) or a salt thereof, wherein: R1, R2, R3, 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 (DGKξ), and pharmaceutical compositions comprising such compounds. These compounds are useful in the treatment of viral infections and proliferative disorders, such as cancer.