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公开(公告)号:US20210121453A1
公开(公告)日:2021-04-29
申请号:US17012781
申请日:2020-09-04
发明人: Dalton King , Lorin A. Thompson, III , Jianliang Shi , Srinivasan Thangathirupathy , Jayakumar Sankara Warrier , Imadul Islam , John E. Macor
IPC分类号: A61K31/454 , C07D403/04 , C07D401/04
摘要: 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:US10961239B2
公开(公告)日:2021-03-30
申请号:US16475413
申请日:2018-01-03
发明人: Robert M. Borzilleri , Upender Velaparthi , Chetan Padmakar Darne , Peiying Liu , Manjunatha Narayana Rao Kamble , Balaji Seshadri , Raju Mannoori , Hasibur Rahaman , Jayakumar Sankara Warrier
IPC分类号: C07D487/04 , C07D401/14 , C07D471/04 , A61K45/06 , C07K16/28
摘要: 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:US10399987B2
公开(公告)日:2019-09-03
申请号:US15747843
申请日:2016-07-27
发明人: Lalgudi S. Harikrishnan , Brian E. Fink , Robert M. Borzilleri , Gopikishan Tonukunuru , Jayakumar Sankara Warrier
IPC分类号: C07D487/04 , A61P35/00 , A61K31/519
摘要: 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:US20180243312A1
公开(公告)日:2018-08-30
申请号:US15755636
申请日:2016-08-30
CPC分类号: A61K31/53 , A61K35/02 , A61K2121/00 , A61P35/00 , C07D487/04 , C07D519/00
摘要: The invention relates generally to compounds that modulate the activity of TGFBETA R-1 and TGFBETA R-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: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: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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公开(公告)号:US20230086933A1
公开(公告)日:2023-03-23
申请号:US17785585
申请日:2020-12-22
发明人: Upender Velaparthi , Chetan Padmakar Darne , Richard E. Olson , Prasada Rao Jalagam , Jayakumar Sankara Warrier
IPC分类号: C07D471/04 , C07D519/00 , A61P35/00 , A61P31/12
摘要: 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.
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公开(公告)号:US10961229B2
公开(公告)日:2021-03-30
申请号:US16502684
申请日:2019-07-03
发明人: Imadul Islam , Srinivasan Thangathirupathy , Jayakumar Sankara Warrier , Srinivas Cheruku , Poornima Shetty , Grandhi Venkat Ram Krishna Mohan Gupta , John E. Macor
IPC分类号: C07D403/14 , C07D401/12 , C07D471/08 , A61P25/28 , A61P25/02 , A61P25/24 , A61P25/16 , C07D401/14 , C07D487/08
摘要: 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:US10954238B1
公开(公告)日:2021-03-23
申请号:US16843024
申请日:2020-04-08
发明人: 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分类号: C07D403/04 , C07D487/04 , A61K31/196 , C07D471/04
摘要: 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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