Substituted 4-alkyl- and 4-alkanoyl-piperidine derivatives...

Details Substituted 4-alkyl- and 4-alkanoyl-piperidine derivatives... Substituted 4-alkyl- and 4-alkanoyl-piperidine derivatives...

C - Chemistry, Metallurgy

07

D

C07D 401/02 (2006.01) A61K 31/495 (2006.01) C07D 207/00 (2006.01) C07D 211/00 (2006.01) C07D 401/04 (2006.01) C07D 401/14 (2006.01) C07D 405/14 (2006.01) C07D 409/14 (2006.01) C07D 413/14 (2006.01) C07D 417/14 (2006.01)

Patent

CA 2561967

The invention concerns substituted 4-alkyl- and 4-alkanoyl-piperidine derivatives having neurokinin antagonistic activity, in particular NK1 antagonistic activity and a combined NK1/NK3 antagonistic activity, compositions comprising them and their use as a medicine, in particular for the treatment and/or prophylaxis of schizophrenia, emesis, anxiety and depression, irritable bowel syndrome (IBS), circadian rhythm disturbances, pre- eclampsia, nociception, pain, in particular visceral and neuropathic pain, pancreatitis, neurogenic inflammation, asthma, chronic obstructive pulmonary disease (COPD) and micturition disorders such as urinary incontinence. 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 des dérivés de 4-alkyl- et 4-alkanoyl-pipéridine substitués possédant une activité antagoniste des neurokinines, notamment l'activité antagoniste de NK¿1? et une activité antagoniste combinée de NK¿1?/NK¿3?, des compositions renfermant ceux-ci et l'utilisation de ceux-ci comme médicaments, notamment pour le traitement et/ou la prophylaxie de la schizophrénie, des vomissements, de l'anxiété et de la dépression, du syndrome du côlon irritable (IBS), des troubles du rythme circadien, de la pré-éclampsie, de la nociception, des douleurs, notamment viscérales et neuropathiques, de la pancréatite, des inflammations neurogènes, de l'asthme, de la maladie obstructive respiratoire (COPD) et des troubles de la miction, tels que l'incontinence urinaire. Les composés selon l'invention peuvent être représentés par la formule générale (I) et comprennent également un acide ou des sels d'ajout de base acceptables sur le plan pharmaceutique de ceux-ci, les formes stéréochimiquement isomères de ceux-ci, la forme <i>N</i>-oxyde de ceux-ci et des promédicaments de ceux-ci, tous les substituants étant définis dans la revendication 1.

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