公开(公告)号：US11964973B2

公开(公告)日：2024-04-23

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

CPC classification number: 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：US20230118629A1

公开(公告)日：2023-04-20

申请号：US17785749

申请日：2020-12-22

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Upender Velaparthi ,  Chetan Padmakar Darne ,  Richard E. Olson ,  Jayakumar Sankara Warrier

IPC: C07D471/04 ,  A61P35/00 ,  C07D519/00

Abstract: Disclosed are compounds of Formula (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 proliferatve disorders, such as cancer.

公开(公告)号：US20230086933A1

公开(公告)日：2023-03-23

申请号：US17785585

申请日：2020-12-22

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Upender Velaparthi ,  Chetan Padmakar Darne ,  Richard E. Olson ,  Prasada Rao Jalagam ,  Jayakumar Sankara Warrier

IPC: C07D471/04 ,  C07D519/00 ,  A61P35/00 ,  A61P31/12

Abstract: Disclosed are compounds of Formula (I): (I) or a salt thereof, wherein: X is CR6 or N; Y is CR3 or N; 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 (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：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：US09556179B2

公开(公告)日：2017-01-31

申请号：US14653895

申请日：2013-12-20

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Upender Velaparthi ,  Chetan Padmakar Darne ,  Dharmpal S. Dodd ,  Anthony J. Sampognaro ,  Mark D. Wittman ,  Selvakumar Kumaravel ,  Dibakar Mullick ,  Peiying Liu ,  Chandrasekhar Reddy Rachamreddy

IPC: C07D487/04 ,  C07D519/00

CPC classification number: C07D487/04 ,  C07D519/00

Abstract: The invention provides compounds of Formula (I) and pharmaceutically acceptable salts thereof. The compounds of Formula (I) inhibit protein kinase activity thereby making them useful as anticancer agents.

Abstract translation: 本发明提供式（I）化合物及其药学上可接受的盐。 式（I）的化合物抑制蛋白激酶活性，从而使它们用作抗癌剂。

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：US11866430B2

公开(公告)日：2024-01-09

申请号：US17254914

申请日：2019-06-26

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Louis S. Chupak ,  Min Ding ,  Robert G. Gentles ,  Yazhong Huang ,  Scott W. Martin ,  Ivar M. Mcdonald ,  Stephen E. Mercer ,  Richard E. Olson ,  Upender Velaparthi ,  Michael Wichroski ,  Xiaofan Zheng

IPC: C07D471/04 ,  A61K31/4375 ,  A61P35/00

CPC classification number: C07D471/04 ,  A61K31/4375 ,  A61P35/00

Abstract: Disclosed are compounds of Formula (I): or a salt thereof, wherein: R1, R2, R3, and R4 are defined herein. Also disclosed are methods of using such compounds to inhibit the activity of one or both of diacylglycerol kinase alpha (DGK α) 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：US20210277004A1

公开(公告)日：2021-09-09

申请号：US17254914

申请日：2019-06-26

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Louis S. Chupak ,  Min Ding ,  Robert G. Gentles ,  Yazhong Huang ,  Scott W. Martin ,  Ivar M. Mcdonald ,  Stephen E. Mercer ,  Richard E. Olson ,  Upender Velaparthi ,  Michael Wichroski ,  Xiaofan Zheng

IPC: C07D471/04 ,  A61P35/00

Abstract: Disclosed are compounds of Formula (I): or a salt thereof, wherein: R1, R2, R3, and R4 are defined herein. Also disclosed are methods of using such compounds to inhibit the activity of one or both of diacylglycerol kinase alpha (DGK α) 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.