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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.
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![Substituted 4,5,6,7-tetrahydropyrazolo[1,5-A]pyrazine derivatives as casein kinase 1 D/E inhibitors](/abs-image/US/2017/03/21/US09598423B2/abs.jpg.150x150.jpg)
22.发明授权公开(公告)号：US09598423B2
公开(公告)日：2017-03-21
申请号：US15034217
申请日：2014-11-14
Applicant: BRISTOL-MYERS SQUIBB COMPANY
Inventor： Upender Velaparthi , Chetan Padmakar Darne , Peiying Liu , Mark D. Wittman , Bradley C. Pearce , Erika M. V. Araujo , Bireshwar Dasgupta , Jalathi Surendran Nair , Sakthi Kumaran Janakiraman , Chandrasekhar Reddy Rachamreddy , Mallikarjuna Rao Mettu , Arul Mozhi Selvan Subbiah Karuppiah , Bandreddy Subba Reddy , Pulicharla Nagalakshmi , Rajesh Onkardas Bora , Shilpa Holehatti Maheshwarappa , Selvakumar Kumaravel , Dibakar Mullick , Ramesh Sistla
IPC: A61K31/498 , C07D487/04 , C07D491/147 , C07D487/10 , C07D491/20 , C07D487/20 , C07D519/00
CPC classification number: C07D487/04 , C07D487/10 , C07D487/20 , C07D491/147 , C07D491/20 , 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.
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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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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：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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Patent Agency Ranking
公开(公告)号：US09981944B2
公开(公告)日：2018-05-29
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: C07D401/04 , C07D471/04 , C07D487/04 , C07B59/00 , C07C53/06 , C07C53/18 , C07D401/14
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.
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公开(公告)号：US09956220B2
公开(公告)日：2018-05-01
申请号：US15319028
申请日：2015-06-18
Applicant: Bristol-Myers Squibb Company
Inventor： Upender Velaparthi , Selvakumar Kumaravel , Arul Mozhi Selvan Subbiah Karupplah , Shilpa Holehatti Maheshwarappa , Chandrasekhar Reddy Rachamreddy , Mark D. Wittman
IPC: A61K31/5025 , C07D487/04 , C07D519/00
CPC classification number: A61K31/5025 , 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.
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![SUBSTITUTED 4,5,6,7-TETRAHYDROPYRAZOLO[1,5-A]PYRAZINE DERIVATIVES AS CASEIN KINASE 1 D/E INHIBITORS](/abs-image/US/2016/10/27/US20160311824A1/abs.jpg.150x150.jpg)
28.发明申请SUBSTITUTED 4,5,6,7-TETRAHYDROPYRAZOLO[1,5-A]PYRAZINE DERIVATIVES AS CASEIN KINASE 1 D/E INHIBITORS 审中-公开取代4,5,6,7-四氢吡唑并[1,5-A]吡啶衍生物作为CASEIN KINASE 1 D / E抑制剂公开(公告)号：US20160311824A1
公开(公告)日：2016-10-27
申请号：US15034217
申请日：2014-11-14
Applicant: BRISTOL-MYERS SQUIBB COMPANY
Inventor： Upender Velaparthi , Chetan Padmakar Dame , Peiying Liu , Mark D Wittman , Bradley C. Pearce , Erika M.V. Araujo , Bireshwar Dasgupta , Jalathi Surendran Nair , Sakthi Kumaran Janakiraman , Chandrasekhar Reddy Rachamreddy , Mallikarjuna Rao Mettu , Arul Mozhi Selvan Subbiah Karuppiah , Bandreddy Subba Reddy , Pulicharla Nagalakshmi , Rajesh Onkardas Bora , Shilpa Holehatti Maheshwarappa , Selvakumar Kumaravel , Dibakar Mullick , Ramesh Sistla
IPC: C07D487/04 , C07D487/20 , C07D491/147 , C07D491/20 , C07D519/00 , C07D487/10
CPC classification number: C07D487/04 , C07D487/10 , C07D487/20 , C07D491/147 , C07D491/20 , 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: 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。
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29.发明授权Pyrazole substituted imidazopyrazines as casein kinase 1 d/e inhibitors 有权吡唑取代的咪唑并吡嗪作为酪蛋白激酶1 d / e抑制剂公开(公告)号：US09475817B2
公开(公告)日：2016-10-25
申请号：US14653878
申请日：2013-12-20
Applicant: BRISTOL-MYERS SQUIBB COMPANY
Inventor： Upender Velaparthi , Chetan Padmakar Darne , Dharmpal S. Dodd , Peiying Liu , Christopher P. Mussari , Mark D. Wittman , Selvakumar Kumaravel , Dibakar Mullick
IPC: C07D487/04
CPC classification number: C07D487/04
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.
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公开(公告)号：US20160122358A1
公开(公告)日：2016-05-05
申请号：US14994346
申请日：2016-01-13
Applicant: BRISTOL-MYERS SQUIBB COMPANY
Inventor： Upender Velaparthi , Chetan Padmakar Darne , Peiying Liu , Mark D. Wittman , Bradley C. Pearce , Erika M. V. Araujo , Bireshwar Dasgupta , Jalathi Surendran Nair , Sakthi Kumaran Janakiraman , Chandrasekhar Reddy Rachamreddy , Mallikarjuna Rao Mettu , Arul Mozhi Subbiah Karuppiah , Subba Reddy Bandreddy , Nagalakshmi Pulicharla , Rajesh Onkardas Bora , Shilpa Maheshwarappa Holehatti , Selvakumar Kumaravel , Dibakar Mullick , Ramesh Kumar Sistla
IPC: C07D487/04 , C07D487/20 , C07D491/20 , C07D487/10 , C07D491/147
CPC classification number: C07D487/04 , C07D487/10 , C07D487/20 , C07D491/147 , C07D491/20 , 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.
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