公开(公告)号：US10961239B2

公开(公告)日：2021-03-30

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: C07D487/04 ,  C07D401/14 ,  C07D471/04 ,  A61K45/06 ,  C07K16/28

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 disorders of dysregulated apoptosis, such as cancer, utilizing the compounds of the invention.

公开(公告)号：US20180221342A1

公开(公告)日：2018-08-09

申请号：US15749557

申请日：2016-07-27

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： David B. Frennesson ,  Piyasena Hewawasam ,  Omar D. Lopez ,  Van N. Nguyen ,  Mark G. Saulnier ,  Yong Tu ,  Alan Xiangdong Wang ,  Gan Wang ,  Ningning Xu ,  Roshan Yadavrao Nimje ,  Hasibur Rahaman ,  Samayamunthula Venkata Satya Arun Kumar Gupta ,  Nicholas A. Meanwell ,  Makonen Belema

IPC: A61K31/4178 ,  A61P31/14

CPC classification number: A61K31/4178 ,  A61K31/417 ,  A61K31/4184 ,  A61K31/4439 ,  A61K31/497 ,  A61K31/7056 ,  A61K38/21 ,  A61K45/06 ,  A61K2300/00 ,  A61P31/14

Abstract: The present disclosure is generally directed to antiviral compounds, and more specifically directed to combinations of compounds which can inhibit the function of the NS5A protein encoded by Hepatitis C virus (HCV), compositions comprising such combinations, and methods for inhibiting the function of the NS5A protein.

公开(公告)号：US20160264553A1

公开(公告)日：2016-09-15

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

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.

Abstract translation: 和其药学上可接受的盐，前药和N-氧化物（及其溶剂化物和水合物），其中R1，Z和n如本文所述。 在某些实施方案中，本文公开的化合物抑制GDF8，并且可以用于通过阻断GDF8信号传导来治疗疾病。

公开(公告)号：US10954238B1

公开(公告)日：2021-03-23

申请号：US16843024

申请日：2020-04-08

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 ,  C07D487/04 ,  A61K31/196 ,  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：US20190292179A1

公开(公告)日：2019-09-26

申请号：US16316714

申请日：2017-07-19

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Robert M. Borzilleri ,  Peiyung Liu ,  Andrew J. Tebben ,  Upender Velaparthi ,  Hasibur Rahaman ,  Gopikishan Tonukunuru ,  Jayakumar Sankara Warrier

IPC: C07D471/04 ,  A61K31/437 ,  A61K31/5383 ,  A61K31/416 ,  A61K31/5025 ,  A61K39/395 ,  C07D403/04 ,  C07D487/04 ,  C07D498/04

Abstract: The invention relates generally to compounds that modulate the activity of TGFβR-1 and TGFβR-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：US20180250303A1

公开(公告)日：2018-09-06

申请号：US15754311

申请日：2016-08-23

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Robert M. Borzilleri ,  Brian E. Fink ,  Lalgudi S. Harikrishnan ,  Upender Velaparthi ,  Vishweshwaraiah Baligar ,  Hasibur Rahaman ,  Jayakumar Sankara Warrier

IPC: A61K31/52 ,  A61P35/02

CPC classification number: A61K31/52 ,  A61K2121/00 ,  A61P35/02 ,  C07D473/34

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 disorders of dysregulated apoptosis, such as cancer, utilizing the compounds of the invention.

公开(公告)号：US20160257690A1

公开(公告)日：2016-09-08

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

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.

Abstract translation: 公开了咪唑和噻唑化合物，以及药物组合物及其使用方法。 一个实施方案是具有其结构和药学上可接受的盐，前药和N-氧化物（及其溶剂化物和水合物）的化合物，其中X，A，Z，R 1和R'如本文所述。 在某些实施方案中，本文公开的化合物抑制TGF-β，并且可用于通过阻断TGF-β信号传导治疗疾病。

公开(公告)号：US20240400563A1

公开(公告)日：2024-12-05

申请号：US18804699

申请日：2024-08-14

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.

公开(公告)号：US11584747B2

公开(公告)日：2023-02-21

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.

公开(公告)号：US10669272B2

公开(公告)日：2020-06-02

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: C07D403/04 ,  C07D487/04 ,  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.