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：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：US09242967B2

公开(公告)日：2016-01-26

申请号：US14598721

申请日：2015-01-16

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Upender Velaparthi ,  Peiying Liu

IPC: C07D413/00 ,  C07D333/00 ,  C07D409/14 ,  C07D498/04 ,  C07D413/14 ,  C07D409/04 ,  C07D413/04 ,  C07D487/04 ,  C07D417/14 ,  C07D471/04 ,  C07D495/04 ,  C07D519/00 ,  C07D413/06

CPC classification number: C07D498/04 ,  C07D409/04 ,  C07D409/14 ,  C07D413/04 ,  C07D413/06 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04 ,  C07D519/00

Abstract: Disclosed are azaindazole compounds of Formula (I): or a pharmaceutically acceptable salt thereof, wherein: X is O and Y is N; or X is S and Y is CH; Z is CR2 or N; Q is a heteroaryl; and R1 is defined herein. Also disclosed are methods of using such compounds in the treatment of at least one CYP17 assoC1ated condition, such as, for example, cancer, and pharmaceutical compositions comprising such compounds.

Abstract translation: 公开了式（I）的氮杂吲唑化合物或其药学上可接受的盐，其中：X为O且Y为N; 或X为S，Y为CH; Z是CR2或N; Q是杂芳基; 并且R1在本文中定义。 还公开了使用这些化合物治疗至少一种CYP17相关病症（例如癌症）和包含这些化合物的药物组合物的方法。

公开(公告)号：US20150126529A1

公开(公告)日：2015-05-07

申请号：US14598721

申请日：2015-01-16

Applicant: Bristol-Myers Squibb Company

Inventor： Upender Velaparthi ,  Peiying Liu

IPC: C07D409/14 ,  C07D409/04 ,  C07D495/04

CPC classification number: C07D498/04 ,  C07D409/04 ,  C07D409/14 ,  C07D413/04 ,  C07D413/06 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04 ,  C07D519/00

Abstract: Disclosed are azaindazole compounds of Formula (I): or a pharmaceutically acceptable salt thereof, wherein: X is O and Y is N; or X is S and Y is CH; Z is CR2 or N; Q is a heteroaryl; and R1 is defined herein. Also disclosed are methods of using such compounds in the treatment of at least one CYP17 associated condition, such as, for example, cancer, and pharmaceutical compositions comprising such compounds.

Abstract translation: 公开了式（I）的氮杂吲唑化合物或其药学上可接受的盐，其中：X为O且Y为N; 或X为S，Y为CH; Z是CR2或N; Q是杂芳基; 并且R1在本文中定义。 还公开了使用这些化合物治疗至少一种CYP17相关病症例如癌症的方法，以及包含这些化合物的药物组合物。

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.

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.