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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.
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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
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.
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公开(公告)号：US20180215762A1
公开(公告)日：2018-08-02
申请号：US15747843
申请日：2016-07-27
Applicant: BRISTOL-MYERS SQUIBB COMPANY
Inventor： Lalgudi S. HARIKRISHNAN , Brian E. Fink , Robert M. Borzilleri , Gopikishan Tonukunuru , Jayakumar Sankara Warrier
IPC: C07D487/04 , A61K31/519 , A61P35/00
CPC classification number: C07D487/04 , A61K31/519 , A61P35/00
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.
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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。
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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.
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Patent Agency Ranking
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.
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公开(公告)号：US10954225B2
公开(公告)日：2021-03-23
申请号：US16707382
申请日：2019-12-09
Applicant: Bristol-Myers Squibb Company
Inventor： Imadul Islam , Srinivasan Thangathirupathy , Jayakumar Sankara Warrier , Srinivas Cheruku , Poornima Shetty , John E. Macor
IPC: C07D413/14 , C07D413/04 , A61K31/497 , A61K31/4523 , A61P25/24 , C07D413/12
Abstract: The present disclosure provides compounds of Formula (I) and pharmaceutically acceptable salts thereof. The Formula (I) compounds are ligands for NR2B N-Methyl-D-aspartate (NMDA) receptor and thereby making them useful for the treatment of various disorders of the central nervous system.
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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.
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公开(公告)号：US20200163949A1
公开(公告)日：2020-05-28
申请号：US16777114
申请日：2020-01-30
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 , 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.
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公开(公告)号：US20200109140A1
公开(公告)日：2020-04-09
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: 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.
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