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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
发明人： 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分类号： C07D487/04 , C07D471/04
CPC分类号： C07D487/04 , C07D401/04 , C07D403/04 , C07D417/04 , C07D471/04
摘要： 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.
摘要翻译： 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：US20160264553A1
公开(公告)日：2016-09-15
申请号：US15043729
申请日：2016-02-15
发明人： Pingyu Ding , Marina Gelman , Todd Kinsella , Rajinder Singh , Somasekhar Bhamidipati , Upender Velaparthi , Robert M. Borzilleri , Hasibur Rahaman , Jayakumar Sankara Warrier
IPC分类号： C07D401/14 , C07B59/00 , C07D471/04 , C07D487/04 , C07C53/18 , C07C53/06
CPC分类号： C07D401/14 , C07B59/002 , C07B2200/05 , C07C53/06 , C07C53/18 , C07D471/04 , C07D487/04
摘要： 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.
摘要翻译： 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。
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公开(公告)号：US11352360B2
公开(公告)日：2022-06-07
申请号：US16360162
申请日：2019-03-21
发明人： 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分类号： C07D487/04 , C07D401/04 , C07D403/04 , C07D471/04 , A61P35/00 , C07D417/04
摘要： 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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公开(公告)号：US09884868B2
公开(公告)日：2018-02-06
申请号：US15054895
申请日：2016-02-26
发明人： 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分类号： C07D487/04 , C07D471/04 , C07D401/04 , C07D403/04 , C07D417/04
CPC分类号： C07D487/04 , C07D401/04 , C07D403/04 , C07D417/04 , C07D471/04
摘要： 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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公开(公告)号：US09981944B2
公开(公告)日：2018-05-29
申请号：US15043729
申请日：2016-02-15
发明人： Pingyu Ding , Marina Gelman , Todd Kinsella , Rajinder Singh , Somasekhar Bhamidipati , Upender Velaparthi , Robert M. Borzilleri , Hasibur Rahaman , Jayakumar Sankara Warrier
IPC分类号： C07D401/04 , C07D471/04 , C07D487/04 , C07B59/00 , C07C53/06 , C07C53/18 , C07D401/14
CPC分类号： C07D401/14 , C07B59/002 , C07B2200/05 , C07C53/06 , C07C53/18 , C07D471/04 , C07D487/04
摘要： 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：US20200031832A1
公开(公告)日：2020-01-30
申请号：US16360162
申请日：2019-03-21
发明人： Todd Kinsella , Marina Gelman , Hui Hong , Ihab S. Darwish , Rajinder Singh , Jiaxin Yu , Robert M. Borzilleri , Upender Velaparthi , Peiying Liu , Chetan Padmakar Darne , Hasibur Rahaman , Jayakumar Sankara Warrier
IPC分类号： C07D487/04 , C07D471/04 , C07D417/04 , C07D403/04 , C07D401/04
摘要： 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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公开(公告)号：US10287295B2
公开(公告)日：2019-05-14
申请号：US15860379
申请日：2018-01-02
发明人： Todd Kinsella , Marina Gelman , Hui Hong , Ihab S. Darwish , Rajinder Singh , Jiaxin Yu , Robert M. Borzilleri , Upender Velaparthi , Peiying Liu , Chetan Padmakar Darne , Hasibur Rahaman , Jayakumar Sankara Warrier
IPC分类号： C07D487/04 , C07D471/04 , C07D401/04 , C07D403/04 , C07D417/04
摘要： 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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公开(公告)号：US20180127426A1
公开(公告)日：2018-05-10
申请号：US15860379
申请日：2018-01-02
发明人： 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分类号： C07D487/04 , C07D417/04 , C07D403/04 , C07D471/04 , C07D401/04
CPC分类号： C07D487/04 , C07D401/04 , C07D403/04 , C07D417/04 , C07D471/04
摘要： 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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公开(公告)号：US11964973B2
公开(公告)日：2024-04-23
申请号：US17130022
申请日：2020-12-22
发明人： 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分类号： C07D471/04 , C07D401/04
CPC分类号： C07D471/04 , C07D401/04
摘要： 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
IPC分类号： C07D471/04 , A61P35/00 , C07D519/00
摘要： 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.
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