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公开(公告)号：US20180086764A1
公开(公告)日：2018-03-29
申请号：US15563075
申请日：2015-04-01
Applicant: Rigel Pharmaceuticals, Inc.
Inventor： Marina Gelman , Todd Kinsella , Somasekhar Bhamidipati , Ihab Darwish , Rajinder Singh , Jiaxin Yu
IPC: C07D487/04 , C07D519/00 , C07D471/04
Abstract: Disclosed are pyrazole 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 A, X, Z, m, p, and R2 are as described herein. In certain embodiments, a compound disclosed herein inhibits the activity of one or more members of the TGF-β superfamily, and can be used to treat disease by blocking such activity.
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公开(公告)号：US20170342048A1
公开(公告)日：2017-11-30
申请号：US15366981
申请日：2017-07-13
Applicant: Rigel Pharmaceuticals, Inc.
Inventor： Somasekhar Bhamidipati , Marina Gelman , Pingyu Ding , Rajinder Singh , Jeffrey Clough , Todd Kinsella , Donald Payan
IPC: C07D401/04 , C07D513/04 , C07D498/04 , C07D487/04 , C07D471/04 , C07D417/14 , C07D213/26 , C07D417/04 , C07D413/04 , C07D405/14 , C07D405/04 , C07D401/14 , C07F9/6503 , C07D453/02
CPC classification number: C07D401/04 , C07D213/26 , C07D401/14 , C07D405/04 , C07D405/14 , C07D413/04 , C07D417/04 , C07D417/14 , C07D453/02 , C07D471/04 , C07D487/04 , C07D498/04 , C07D513/04 , C07F9/65038
Abstract: Described are GCF-8 inhibitors of the formula (I), and pharmaceutically acceptable salts thereof, wherein n, R1, R2, R5, R6, X and Z are defined herein. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for inhibiting GDF-8 in a cell and methods for treating a patient suffering from a disease or disorder, wherein the patient would therapeutically benefit from an increase in mass or strength of muscle tissue.
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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：US20140323460A1
公开(公告)日：2014-10-30
申请号：US14325012
申请日：2014-07-07
Applicant: RIGEL PHARMACEUTICALS, INC.
Inventor： Donald Payan , Yasumichi Hitoshi , Todd Kinsella
IPC: A61K31/4545 , A61K31/506 , A61K31/437 , A61K31/496 , A61K31/4709 , A61K31/454 , A61K31/5377 , A61K31/4525
CPC classification number: A61K31/437 , A61K31/4427 , A61K31/4525 , A61K31/454 , A61K31/4545 , A61K31/4709 , A61K31/496 , A61K31/506 , A61K31/5377
Abstract: Disclosed are uses of carboxamide, sulfonamide and amine compounds for the treatment and amelioration of disorders and conditions related to oxidative stress, mitochondrial dysfunction, free radical damage and metabolic inefficiency, among others. Also described are methods for increasing exercise endurance, exercise efficiency and aerobic workload using the compounds described herein.
Abstract translation: 公开了羧酰胺，磺酰胺和胺化合物用于治疗和改善与氧化应激，线粒体功能障碍，自由基损伤和代谢低效等相关的病症和病症的用途。 还描述了使用本文所述化合物增加运动耐力，运动效率和有氧工作量的方法。
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公开(公告)号：US20140107073A1
公开(公告)日：2014-04-17
申请号：US14046834
申请日：2013-10-04
Applicant: Rigel Pharmaceuticals, Inc.
Inventor： Somasekhar Bhamidipati , Marina Gelman , Pingyu Ding , Rajinder Singh , Jeffrey Clough , Todd Kinsella , Donald Payan
IPC: C07F9/6503 , C07D417/04 , C07D498/04 , C07D405/14 , C07D401/14 , C07D213/26 , C07D401/04 , C07D471/04
CPC classification number: C07D401/04 , C07D213/26 , C07D401/14 , C07D405/04 , C07D405/14 , C07D413/04 , C07D417/04 , C07D417/14 , C07D453/02 , C07D471/04 , C07D487/04 , C07D498/04 , C07D513/04 , C07F9/65038
Abstract: Described are GCF-8 inhibitors of the formula (I), and pharmaceutically acceptable salts thereof, wherein n, R1, R2, R5, R6, X and Z are defined herein. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for inhibiting GDF-8 in a cell and methods for treating a patient suffering from a disease or disorder, wherein the patient would therapeutically benefit from an increase in mass or strength of muscle tissue.
Abstract translation: 描述了式（I）的GCF-8抑制剂及其药学上可接受的盐，其中n，R1，R2，R5，R6，X和Z如本文所定义。 还提供了包含其的药物组合物。 这样的化合物和组合物可用于抑制细胞中的GDF-8的方法和用于治疗患有疾病或病症的患者的方法，其中患者将从肌肉组织的质量或强度的增加中治疗获益。
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Patent Agency Ranking
公开(公告)号：US20230123591A1
公开(公告)日：2023-04-20
申请号：US17962305
申请日：2022-10-07
Applicant: Rigel Pharmaceuticals, Inc.
Inventor： Marina Gelman , Todd Kinsella , Somasekhar Bhamidipati , Ihab Darwish , Rajinder Singh , Jiaxin Yu
IPC: C07D487/04 , C07D401/04 , C07D403/04 , C07D417/04 , C07D471/04 , C07D519/00
Abstract: Disclosed are pyrazole 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 A, X, Z, m, p, and R2 are as described herein. In certain embodiments, a compound disclosed herein inhibits the activity of one or more members of the TGF-β superfamily, and can be used to treat disease by blocking such activity.
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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
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 Darne , Hasibur Rahaman , Jayakumar Sankara Warrier
IPC: C07D487/04 , C07D471/04 , C07D417/04 , C07D403/04 , C07D401/04
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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公开(公告)号：US10287295B2
公开(公告)日：2019-05-14
申请号：US15860379
申请日：2018-01-02
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 Darne , Hasibur Rahaman , Jayakumar Sankara Warrier
IPC: C07D487/04 , C07D471/04 , C07D401/04 , C07D403/04 , 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.
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公开(公告)号：US20180346487A1
公开(公告)日：2018-12-06
申请号：US15527908
申请日：2015-11-16
Applicant: Rigel Pharmaceuticals, Inc.
Inventor： Rajinder Singh , Todd Kinsella , Jiaxin Yu , Marina Gelman , Ihab S. Darwish
IPC: C07D519/00 , C07D487/04 , C07D498/04 , A61K45/06 , A61K31/437 , A61K31/4365 , A61K31/428 , A61K31/4709 , A61K31/498 , A61K31/517 , A61K31/5377 , A61K31/4188 , A61K31/416 , A61K31/519
Abstract: Disclosed are imidazole compounds, as well as pharmaceutical compositions and methods of use thereof. One embodiment is a compound having the structure Formula (I) and pharmaceutically acceptable salts, prodrugs and N-oxides thereof (and solvates and hydrates thereof), wherein A, Z, X, R1, R2 m, p and a 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：US20180155422A1
公开(公告)日：2018-06-07
申请号：US15829422
申请日：2017-12-01
Applicant: Rigel Pharmaceuticals, Inc.
Inventor： Ramesh R. Bhatt , Todd Kinsella , Wei Li
Abstract: Provided herein are antigen binding molecules that bind to TIGIT, include antibodies and antigen binding fragments thereof.
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