Diaryl and arylheteroaryl urea derivatives as modulators of...

C - Chemistry – Metallurgy – 07 – D

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C07D 231/16 (2006.01) A61K 31/415 (2006.01) C07D 231/12 (2006.01)

Patent

CA 2533369

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 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 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.

L'invention concerne certains dérivés de pyrazole de formule (I) et des compositions pharmaceutiques les comprenant, modulant l'activité du récepteur de la sérotonine 5-HT¿2A?. Les composés et compositions pharmaceutiques de l'invention sont particulièrement destinés à des procédés utiles dans la prophylaxie et le traitement de l'agrégation plaquettaire, de la coronaropathie, de l'infarctus du myocarde, de l'accident ischémique transitoire, de l'angine de poitrine, de l'attaque, de la fibrillation auriculaire, réduisant le risque de formation de caillots sanguins, le risque d'asthme ou d'un de ses symptômes, d'agitation ou d'un symptôme d'agitation, de troubles comportementaux, de psychose médicamenteuse, de psychose à forme d'état d'excitation, de syndrome de Gilles de la Tourette, de trouble maniaque, de psychose organique ou NOS, de trouble psychotique, de psychose, de schizophrénie aiguë, de schizophrénie chronique, de schizophrénie NOS et de troubles associés, de troubles du sommeil, de troubles associés au diabète et similaire. L'invention porte également sur une méthode de prophylaxie ou de traitement de troubles médiés par le récepteur de la sérotonine 5-HT¿2A?, combinée à un antagoniste du récepteur de la dopamine D2, tel que l'halopéridol, administrés séparément ou ensemble.

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