C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 498/10 (2006.01) A61K 31/537 (2006.01) A61P 25/18 (2006.01) A61P 25/24 (2006.01)
Patent
CA 2598530
This invention concerns substituted oxa-diaza-spiro-[5.5]-undecanone derivatives having neurokinin antagonistic activity, in particular an NK1 antagonistic activity, an NK3 antagonistic activity, a combined NK1/NK2 antagonistic activity and a combined NK1/NK2/NK3 antagonistic activity, their preparation, 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 incont inence. 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.
Cette invention concerne des dérivés d~oxa-diaza-spiro-[5.5]-undécanone substitués possédant une activité antagoniste de la neurokinine, en particulier une activité antagoniste NK1, NK3, NK1/NK2 combinée et NK1/NK2/NK3 combinée, leur préparation, des compositions les renfermant et leur utilisation comme médicaments, en particulier pour le traitement et/ou la prophylaxie de la schizophrénie, du vomissement, de l~anxiété et de la dépression, du syndrome du colon irritable (SCI), des troubles du rythme circadien, de la prééclampsie, de la nociception, de la douleur, en particulier viscérale et neuropathique, de la pancréatite, de l~inflammation neurogène, de l~asthme, de la bronchopneumopathie chronique obstructive (BPCO) et des troubles de la miction du type incontinence urinaire. Les composés décrits peuvent être représentés par la formule générale (I) et comprennent également leurs sels d~addition d~acide ou de base acceptables sur le plan pharmaceutique, les formes stéréochimiquement isomères correspondantes, la forme N-oxide correspondante et les promédicaments correspondants, tous les substituants étant tels que définis dans la revendication 1.
Coupa Sophie
Janssens Frans Eduard
Poncelet Alain Philippe
Schoentjes Bruno
Gowling Lafleur Henderson Llp
Janssen Pharmaceutica N.v.
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