Novel unsaturated tetracyclic tetrahydrofuran derivatives

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 493/04 (2006.01) A61K 31/34 (2006.01) C07D 491/04 (2006.01) C07D 495/04 (2006.01) C07D 495/16 (2006.01)

Patent

CA 2568752

This invention concerns novel substituted unsaturated tetracyclic tetrahydrofuran derivatives with binding affinities towards serotonine receptors, in particular 5-HT2A and 5-HT2C receptors, and towards dopamine receptors, in particular dopamine D2 receptors and with norepinephrine reuptake inhibition properties, pharmaceutical compositions comprising the compounds according to the invention, the use thereof as a medicine, in particular for the prevention and/or treatment of a range of psychiatric and neurological disorders, in particular certain psychotic, cardiovascular and gastrokinetic disorders and processes for their production. The compounds according to the invention can be represented by general Formula (I), and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in Claim 1.

L'invention concerne de nouveaux dérivés de tétrahydrofurane tétracycliques insaturés substitués présentant des affinités de liaison avec les récepteurs de la sérotonine, en particulier les récepteurs 5-HT2A et 5-HT2C, et avec les récepteurs de la dopamine, en particulier les récepteurs de la dopamine D2, ainsi que des propriétés d'inhibition de recaptage de la norépinéphrine. La présente invention porte également sur des compositions pharmaceutiques contenant lesdits composés, leur utilisation comme médicaments, en particulier pour la prévention et/ou le traitement de divers troubles psychiatriques et neurologiques, notamment certains troubles psychotiques, cardio-vasculaires et gastrocinétiques. Enfin, l'invention concerne aussi des procédés de production associés. Les composés de l'invention sont de formule (I) et comportent également leurs sels d'addition basiques ou acides pharmaceutiquement acceptables, leurs formes stéréochimiquement isomériques, leur forme <I>N</I>-oxyde et leurs promédicaments, tous les substituants étant définis à la revendication 1.

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