Substituted pyrazinone derivatives for use as a medicine

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 401/12 (2006.01) A61K 31/501 (2006.01) A61P 25/00 (2006.01) C07D 241/20 (2006.01)

Patent

CA 2659923

The present invention concerns substituted pyrazinone derivatives according to the general Formula (I) a pharmaceutically acceptable acid or base addition salt thereof, a stereochemically isomeric form thereof, an N-oxide form thereof or a quaternary ammonium salt thereof, wherein the variables are defined in Claim 1, having selective 2C-adrenoceptor antagonist activity. It further relates to their preparation, compositions comprising them and their use as a medicine. The compounds according to the invention are usefull for the prevention and/or treatment of central nervous system disorders, mood disorders, anxiety disorders, stress-related disorders associated with depression and/or anxiety, cognitive disorders, personality disorders, schizoaffective disorders, Parkinson's disease, dementia of the Alzheimer's type, chronic pain conditions, neurodegenerative diseases, addiction disorders, mood disorders and sexual dysfunction.

La présente invention concerne des dérivés de pyrazinone substitués conformes à la formule générale (I), un sel, de ceux-ci, d'addition à l'acide ou à la base acceptable du point de vue pharmaceutique, une forme d'isomère stéréochimique de ceux-ci, une forme N-oxyde de ceux-ci ou un sel d'ammonium quaternaire de ceux-ci, les variables étant définies dans la revendication 1. Ces dérivés ont une activité antagoniste du récepteur 2C adrénergique. L'invention concerne en outre la préparation de ces dérivés, des compositions les comprenant, et leur utilisation comme médicament. Les composés selon l'invention sont utiles pour la prévention et/ou le traitement de troubles du système nerveux central, de troubles de l'humeur, de troubles dus à l'anxiété, de troubles liés au stress associés à la dépression et/ou à l'anxiété, de troubles cognitifs, de troubles de la personnalité, de troubles schizoaffectifs, de la maladie de Parkinson, de la démence du type Alzheimer, d'états de douleur chronique, de maladies neurodégénératives, de troubles de l'addiction, de dysthymie et de dysfonctionnement sexuel.

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