# US 8,785,441 B2 · 3-phenyl-pyrazole derivatives as modulators of the 5-HT2A serotonin receptor useful for the treatment of disorders related thereto > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 8,785,441 B2 - Document ID: US8785441B2 - Status: Granted - Kind: B2 - Application number: 13/616,842 - Filed: 2012-09-14 - Published: 2013-09-12 - Granted: 2014-07-22 - Earliest claimed: 2004-11-19 - Assignees: Arena Pharmaceuticals, Inc. - Applicants: Bradley Teegarden; Yifeng Xiong; Sonja Strah-Pleynet; Honnappa Jayakumar; Peter I. Dosa; Konrad Feichtinger; Martin Casper; Juerg Lehmann; Robert M. Jones; David J. Unett; Jin Sun Karoline Choi - Inventors: Bradley Teegarden; Yifeng Xiong; Sonja Strah-Pleynet; Honnappa Jayakumar; Peter I. Dosa; Konrad Feichtinger; Martin Casper; Juerg Lehmann; Robert M. Jones; David J. Unett; Jin Sun Karoline Choi - Web page: https://patentgrep.com/patent/US8785441B2 ## CPC - C07D 231/12: with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms - A61K 31/5377: not condensed and containing further heterocyclic rings, e.g. timolol - A61P 3/00: Drugs for disorders of the metabolism (of the blood or the extracellular fluid A61P7/00) - A61P 3/10: for hyperglycaemia, e.g. antidiabetics - A61P 7/02: Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors - A61P 9/00: Drugs for disorders of the cardiovascular system - A61P 9/10: for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis - A61P 9/12: Antihypertensives - A61P 11/06: Antiasthmatics - A61P 25/00: Drugs for disorders of the nervous system - A61P 25/18: Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia - A61P 25/20: Hypnotics; Sedatives - A61P 25/28: for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia - A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] - A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00 - C07D 231/16: Halogen atoms or nitro radicals - C07D 401/12: linked by a chain containing hetero atoms as chain links - C07D 403/12: linked by a chain containing hetero atoms as chain links - C07D 405/12: linked by a chain containing hetero atoms as chain links - C07D 409/12: linked by a chain containing hetero atoms as chain links - C07D 413/10: linked by a carbon chain containing aromatic rings - C07D 413/12: linked by a chain containing hetero atoms as chain links - C07D 417/12: linked by a chain containing hetero atoms as chain links - C07D 487/08: Bridged systems - Y02A 50/30: Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change - C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08) - A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D) - A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS - Y02A: TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE ## Abstract The present invention relates to certain 3-phenyl-pyrazole derivatives of Formula (Ia) 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 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, progressive multifocal leukoencephalopathy and the like. The present invention also relates to the methods for the treatment of 5-HT2A serotonin receptor mediated disorders in combination with other pharmaceutical agents administered separately or together. ## Claims ### Claim 1 A method for treating a 5-HT2A mediated disorder selected from the group consisting of coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, and atrial fibrillation in an individual comprising administering to said individual in need thereof a therapeutically effective amount of a compound having the structure or a pharmaceutically acceptable salt or solvate thereof. ### Claim 2 A method for treating a condition associated with platelet aggregation selected from the group consisting of claudication, peripheral artery disease, vasoconstriction, vasospasm, arterial occlusion, thrombosis, and stroke in an individual comprising administering to said individual in need thereof a therapeutically effective amount of a compound having the structure or a pharmaceutically acceptable salt or solvate thereof. ### Claim 3 A method for reducing the risk of blood clot formation in an angioplasty or coronary bypass surgery individual comprising administering to said individual in need thereof a therapeutically effective amount of a compound having the structure or a pharmaceutically acceptable salt or solvate thereof. ### Claim 4 A method for reducing the risk of blood clot formation in an individual suffering from atrial fibrillation, comprising administering to said individual in need thereof a therapeutically effective amount of a compound having the structure or a pharmaceutically acceptable salt or solvate thereof. ### Claim 5 A method for treating a sleep disorder in an individual comprising administering to said individual in need thereof a therapeutically effective amount of a compound having the structure or a pharmaceutically acceptable salt or solvate thereof, wherein said sleep disorder is a dyssomnia. ### Claim 6 A method for treating a sleep disorder in an individual comprising administering to said individual in need thereof a therapeutically effective amount of a compound having the structure or a pharmaceutically acceptable salt or solvate thereof, wherein said sleep disorder is a parasomnia. ### Claim 7 A method for treating progressive multifocal leukoencephalopathy in an individual comprising administering to said individual in need thereof a therapeutically effective amount of a compound having the structure or a pharmaceutically acceptable salt or solvate thereof. ### Claim 8 A method for treating hypertension in an individual comprising administering to the individual in need thereof a therapeutically effective amount of a compound having the structure or a pharmaceutically acceptable salt or solvate thereof. ### Claim 9 A method for treating pain in an individual comprising administering to the individual in need thereof a therapeutically effective amount of a compound having the structure or a pharmaceutically acceptable salt or solvate thereof. ### Claim 10 (depends on 2) The method according to claim 2, wherein said condition associated with platelet aggregation is claudication. ### Claim 11 (depends on 2) The method according to claim 2, wherein said condition associated with platelet aggregation is peripheral artery disease. ### Claim 12 (depends on 2) The method according to claim 2, wherein said condition associated with platelet aggregation is vasoconstriction. ### Claim 13 (depends on 2) The method according to claim 2, wherein said condition associated with platelet aggregation is vasospasm. ### Claim 14 (depends on 2) The method according to claim 2, wherein said condition associated with platelet aggregation is arterial occlusion. ### Claim 15 (depends on 2) The method according to claim 2, wherein said condition associated with platelet aggregation is thrombosis. ### Claim 16 (depends on 2) The method according to claim 2, wherein said condition associated with platelet aggregation is stroke.