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1.
公开(公告)号:US20250034090A1
公开(公告)日:2025-01-30
申请号:US18841455
申请日:2023-03-07
Applicant: Arena Pharmaceuticals, Inc.
Inventor: Anthony C. Blackburn , Jui-Chen LIN
IPC: C07D209/60 , A61K31/404 , C07C211/05 , C07C215/08
Abstract: The present invention relates to crystalline salts of (R)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclo-penta[b]indol-3-yl)acetic acid, and pharmaceutical compositions comprising them that are useful as SiP1 receptor modulator. The compound (R)-2-(9-chloro-7-(4-isopropoxy-3-(trifluoromethyl)benzyloxy)-2,3-dihydro-1H-pyrrolo[1,2-a]indol-1-yl)acetic acid identified as an SiP1 receptor modulator is useful in the treatment of SiP1 receptor-associated disorders, for example, diseases and disorders mediated by lymphocytes, transplant rejection, autoimmune diseases and disorders, inflammatory diseases and disorders (e.g., acute and chronic inflammatory conditions), cancer, and conditions characterized by an underlying defect in vascular integrity or that are associated with angiogenesis such as may be pathologic (e.g., as may occur in inflammation, tumor development, and atherosclerosis).
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2.
公开(公告)号:USRE50267E1
公开(公告)日:2025-01-14
申请号:US17747917
申请日:2022-05-18
Applicant: Arena Pharmaceuticals, Inc.
Inventor: Thuy-Anh Tran , Weichao Chen , Bryan A. Kramer , Abu J. M. Sadeque , Anna Shifrina , Young-Jun Shin , Pureza Vallar , Ning Zou
IPC: A61K31/195 , A61K31/27 , A61K31/325 , A61K31/381 , A61K31/426 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4965 , C07C271/12 , C07C271/28 , C07C275/24 , C07C275/28 , C07C275/30 , C07C275/34 , C07C309/15 , C07D213/75 , C07D241/20 , C07D277/48 , C07D333/36
Abstract: The present invention relates to amide derivatives of Formula (XIIIa) and pharmaceutical compositions thereof that modulate the activity of the PGI2 receptor. Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of: Pulmonary arterial hypertension (PAH); idiopathic PAH; familial PAH; PAH associated with a collagen vascular disease, a congenital heart disease, portal hypertension, HIV infection, ingestion of a drug or toxin, hereditary hemorrhagic telangiectasia, splenectomy, pulmonary veno-occlusive disease (PVOD) or pulmonary capillary hemangiomatosis (PCH); PAH with significant venous or capillary involvement; platelet aggregation; coronary artery disease; myocardial infarction; transient ischemic attack, angina; stroke; ischemia-reperfusion injury; restenosis; atrial fibrillation; blood clot formation in an angioplasty or coronary bypass surgery individual or in an individual suffering from atrial fibrillation; atherosclerosis; atherothrombosis; asthma or a symptom thereof; a diabetic-related disorder such as diabetic peripheral neuropathy, diabetic nephropathy or diabetic retinopathy; glaucoma or other disease of the eye with abnormal intraocular pressure; hypertension; inflammation; psoriasis; psoriatic arthritis; rheumatoid arthritis; Crohn's disease; transplant rejection; multiple sclerosis; systemic lupus erythematosus (SLE); ulcerative colitis; ischemia-reperfusion injury; restenosis, atherosclerosis; acne; type 1 diabetes; type 2 diabetes; sepsis; and chronic obstructive pulmonary disorder (COPD).
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公开(公告)号:US12109219B2
公开(公告)日:2024-10-08
申请号:US16849216
申请日:2020-04-15
Applicant: Arena Pharmaceuticals, Inc.
Inventor: Jayant Thatte , Anthony C. Blackburn , Sangdon Han , Robert M. Jones , Jae-Kyu Jung , Antonio Garrido Montalban , Biman B. Pal , Jaimie Karyn Rueter , Sonja Strah-Pleynet , Lars Thoresen , Yifeng Xiong , Dawei Yue , Xiuwen Zhu
IPC: A61K31/675 , A61K31/416 , A61K31/4439 , A61K31/497 , A61K45/06
CPC classification number: A61K31/675 , A61K31/416 , A61K31/4439 , A61K31/497 , A61K45/06 , A61K31/416 , A61K2300/00
Abstract: Provided are certain methods useful in the treatment of cancer comprising administering a compound of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the cannabinoid CB2 receptor;
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公开(公告)号:US20240216392A1
公开(公告)日:2024-07-04
申请号:US18524124
申请日:2023-11-30
Applicant: Arena Pharmaceuticals, Inc.
Inventor: Chadwick J. Orevillo , Randall Kaye , Nuggehally Srinivas
IPC: A61K31/5517 , A61P25/08
CPC classification number: A61K31/5517 , A61P25/08
Abstract: Provided herein are treatment methods including administering a 5-hydroxytryptamine (HT)2C receptor agonist to a patient in need thereof. An exemplary method includes treating or preventing a 5-hydroxytryptamine (HT)2C receptor-associated disorder in a patient in need thereof, wherein the method comprises administering to the patient (R)—N-(2,2-difluoroethyl)-7-methyl-1,2,3,4,6,7-hexahydro-[1,4]diazepino[6,7,1-hi]indole-8-carboxamide (Compound 1), or a pharmaceutically acceptable salt thereof, wherein Compound 1, or a pharmaceutically acceptable salt thereof, is administered twice daily.
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公开(公告)号:US11987588B2
公开(公告)日:2024-05-21
申请号:US17726807
申请日:2022-04-22
Applicant: Arena Pharmaceuticals, Inc.
Inventor: Thuy-Anh Tran , Brett Ullman , Bryan Aubrey Kramer , Quyen-Quyen Thuy Do , Young-Jun Shin
IPC: C07D491/048 , A61P9/00 , A61P9/04 , C07D491/10
CPC classification number: C07D491/048 , A61P9/00 , A61P9/04 , C07D491/10
Abstract: The present invention relates to compounds of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the beta-3 adrenergic receptor. Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of a beta-3 adrenergic receptor-mediated disorder, such as, heart failure and related disorders thereto.
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公开(公告)号:US11780827B2
公开(公告)日:2023-10-10
申请号:US17215759
申请日:2021-03-29
Inventor: Kai Gerlach , Graeme Semple , Yifeng Xiong , Barbara Bertani , Marco Ferrara , Giacomo Fossati , Scott Hobson , Uta Friederike Lessel , Frank Runge , Ursula Mueller-Vieira , Julian Wippich
IPC: C07D403/14
CPC classification number: C07D403/14
Abstract: The invention relates to substituted 3-phenoxyazetidin-1-yl-pyrazines of general formula (I) which are agonists of GPR52, useful in treating central nervous system diseases and other diseases. In addition, the invention relates to the 3-phenoxyazetidin-1-yl-pyrazines of general formula (I) for use as a medicament, pharmaceutical compositions comprising the 3-phenoxyazetidin-1-yl-pyrazines of general formula (I) and processes for preparing pharmaceutical compositions as well as processes for manufacture the compounds according to the invention.
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公开(公告)号:US20230277505A1
公开(公告)日:2023-09-07
申请号:US18079941
申请日:2022-12-13
Applicant: Arena Pharmaceuticals, Inc.
Inventor: Bradley Teegarden , Honnappa Jayakumar , Hongmei Li , Sonja Strah-Pleynet , Peter I. Dosa
IPC: A61K31/415 , C07D231/12 , C07D231/16 , C07D405/12 , C07D401/12 , A61K31/4155 , A61K31/454 , A61K31/496 , A61K31/5377
CPC classification number: A61K31/415 , C07D231/12 , C07D231/16 , C07D405/12 , C07D401/12 , A61K31/4155 , A61K31/454 , A61K31/496 , A61K31/5377
Abstract: The present invention relates to certain pyrazole derivatives of Formula (I) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor.
Compounds and pharmaceutical compositions thereof are directed to methods useful in the prophylaxis or treatment of platelet aggregation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, reducing the risk of blood clot formation, asthma or symptoms thereof, agitation or a symptom, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorder, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, and sleep disorders, sleep disorders, diabetic-related disorders and the like.
The present invention also relates to the method of prophylaxis or treatment of 5-HT2A serotonin receptor mediated disorders in combination with a dopamine D2 receptor antagonist such as haloperidol, administered separately or together.-
公开(公告)号:US20230257349A1
公开(公告)日:2023-08-17
申请号:US17885683
申请日:2022-08-11
Applicant: Arena Pharmaceuticals, Inc.
Inventor: Robert M. Jones , Daniel J. Buzard , Sangdon Han , Sun Hee Kim , Juerg Lehmann , Brett Ullman , Jeanne V. Moody , Xiuwen Zhu , Scott Stirn
IPC: C07D209/94 , A61K31/404 , A61K31/497 , A61K31/4439 , A61K31/433 , A61K31/198 , A61K31/137 , C07D209/70 , C07D209/88 , C07D401/12 , C07D403/12 , C07D417/12 , C07C211/27 , C07C229/26 , C07C255/03 , C07C279/14 , C07D401/14
CPC classification number: C07D209/94 , A61K31/404 , A61K31/497 , A61K31/4439 , A61K31/433 , A61K31/198 , A61K31/137 , C07D209/70 , C07D209/88 , C07D401/12 , C07D403/12 , C07D417/12 , C07C211/27 , C07C229/26 , C07C255/03 , C07C279/14 , C07D401/14 , Y02A50/30
Abstract: The present invention relates to certain substituted 1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid derivatives of Formula (Ia) and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists of the S1P1 receptor.
Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of S1P1 receptor-associated disorders, for example, psoriasis, rheumatoid arthritis, Crohn's disease, transplant rejection, multiple sclerosis, systemic lupus erythematosus, ulcerative colitis, type I diabetes, acne, microbial infections or diseases and viral infections or diseases.-
公开(公告)号:US11555015B2
公开(公告)日:2023-01-17
申请号:US17273681
申请日:2019-09-05
Applicant: Arena Pharmaceuticals, Inc.
Inventor: Abu J. M. Sadeque , Daniel J. Buzard
IPC: C07D209/94 , C07H15/26
Abstract: The present invention relates to certain compounds of Formula (Ia) and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists of the S1P1 receptor: Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of S1P1 receptor-associated disorders, for example, a disease or disorder mediated by lymphocytes, an autoimmune disease or disorder, an inflammatory disease or disorder, an inflammatory skin disease or disorder, cancer, psoriasis, atopic dermatitis, rheumatoid arthritis, Crohn's disease, transplant rejection, multiple sclerosis, systemic lupus erythematosus, ulcerative colitis, type I diabetes, and acne, microbial infections or diseases and viral infections or diseases.
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公开(公告)号:US20220142977A1
公开(公告)日:2022-05-12
申请号:US17421299
申请日:2020-01-08
Applicant: ARENA PHARMACEUTICALS, INC.
Inventor: Snehal U. NAIK
IPC: A61K31/404 , A61K45/06 , A61P37/00
Abstract: Provided are methods for selecting individuals for treatment with (R)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid (Compound 1), or a pharmaceutically acceptable salt, hydrate, or solvate thereof.
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