3-phenyl-pyrazole derivatives as modulators of the 5-ht2a...

C - Chemistry – Metallurgy – 07 – D

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C07D 231/16 (2006.01) A61K 31/4155 (2006.01) A61P 29/00 (2006.01) C07D 231/12 (2006.01) C07D 401/12 (2006.01) C07D 403/12 (2006.01) C07D 405/12 (2006.01) C07D 409/12 (2006.01) C07D 413/12 (2006.01) C07D 417/12 (2006.01) C07D 487/08 (2006.01)

Patent

CA 2588513

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 aggreagation, 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.

L'invention concerne des dérivés de 3-phényl-pyrazole de formule (Ia) et des compositions pharmaceutiques correspondantes qui modulent l'activité du récepteur de sérotonine 5-HT2A. (Ia). Les composés et les compositions pharmaceutiques correspondantes servent dans des méthodes utiles pour traiter l'agrégation plaquettaire, l'insuffisance coronaire, l'infarctus du myocarde, l'accident ischémique transitoire, l'angine, l'accident vasculaire cérébral, la fibrillation auriculaire, pour diminuer les risques de formation de caillots sanguins, pour traiter l'asthme et ses symptômes, l'agitation et un symptôme associé, des troubles du comportement, la psychose induite par des médicaments, la psychose d'excitation, le syndrome de Gilles de la Tourette, le trouble maniaque, la psychose organique ou NSA, le trouble psychotique, la psychose, la schizophrénie aigue, la schizophrénie chronique, la schizophrénie NSA et les troubles associés, les troubles du sommeil, les troubles associés au diabète, la leucoencéphalopathie multifocale progressive et des troubles similaires. La présente invention porte également sur des méthodes pour traiter des troubles liés au récepteur de sérotonine 5-HT2A en combinaison avec d'autres agents pharmaceutiques administrés séparément ou ensemble.

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