Novel substituted tetracyclic tetrahydrofuran, pyrrolidine...

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 487/04 (2006.01) A61K 31/403 (2006.01) A61K 31/407 (2006.01) A61P 25/00 (2006.01) C07D 209/94 (2006.01) C07D 221/18 (2006.01) C07D 307/93 (2006.01) C07D 311/94 (2006.01) C07D 333/80 (2006.01) C07D 491/04 (2006.01)

Patent

CA 2604165

This invention concerns novel substituted tetracyclic tetrahydrofuran, pyrrolidine and tetrahydrothiophene derivatives with binding affinities towards serotonin 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 tétrahydrothiophène pyrolidine et tétrahydrofurane tétracyclique substitués présentant des affinités de liaison envers des récepteurs de sérotonine, notamment des récepteurs 5-HT2A et 5-HT2C, et envers des récepteurs de dopamine, notamment des récepteurs D2 dopamine et des propriétés d'inhibition de réabsorption de noréphinephrine, des compositions pharmaceutiques contenant les composés de l'invention, l'utilisation de ceux-ci en tant que médicaments, notamment dans la prévention et/ou le traitement d'un niveau de trouble psychiatrique et neurologique, plus particulièrement certains troubles psychotiques, cardiovasculaires et gastrocinétiques, ainsi que des procédés destinés à leur production. Les composés de l'invention peuvent être représentés par la formule générale (I) et contiennent également des sels de ceux-ci d'addition basiques ou acides acceptables sur le plan pharmaceutique, des formes isomères stéréochimiques de ceux-ci et des formes N-oxyde et promédicaments de ceux-ci, dans lesquels tous les substituants sont tels que définis dans la revendication 1.

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