Mercaptoimidazoles as ccr2 receptor antagonists

Details Mercaptoimidazoles as ccr2 receptor antagonists Mercaptoimidazoles as ccr2 receptor antagonists

C - Chemistry, Metallurgy

07

D

C07D 403/04 (2006.01) A61K 31/4164 (2006.01) A61K 31/4178 (2006.01) A61K 31/4245 (2006.01) A61K 31/427 (2006.01) A61K 31/4439 (2006.01) A61K 31/506 (2006.01) C07D 233/84 (2006.01) C07D 401/04 (2006.01) C07D 405/04 (2006.01) C07D 413/04 (2006.01) C07D 417/04 (2006.01)

Patent

CA 2565280

The present invention relates to a compound of formula (I), a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine or a stereochemically isomeric form thereof, wherein R1 represents hydrogen, C1- 66alkyl, C3-7cycloalkyl, C1-66alkylo xyC1 -6alkyl, di(C1-6alkyl)aminoC1- 6alkyl, aryl or heteroaryl; each R2 independently represents halo, C1-6alkyl, C1-6alkyloxy, C1-6alkylthio, polyhaloC1-6alkyl, polyhaloC1-6alkyloxy, cyano, aminocarbonyl, amino, mono-or di(C1-4alkyl)amino, nitro, aryl or aryloxy; R3 represents hydrogen, cyano, optionally subst ituted C1-66alkyl, C(=O)-O-R5, C(=O)-NR6aR6b, C(=S)-NR6aR6b, S(=O)2-NR6aR6b or C(=O)-R7; R4 represents hydrogen or C1-6alkyl; n is 1, 2, 3, 4 or 5; Z represents a cyclic ring system. The invention also relates to processes for preparing the compounds of formula (I), their use as CCR2 antagonists and pharmaceutical compositions comprising them.

Présente invention concerne un composé représenté par la formule (I), un N-oxyde, un sel d'addition répondant aux normes pharmaceutiques, un amine quaternaire ou une forme stéréochimiquement isomère de celui-ci. Dans cette formule R¿1? représente hydrogène, C¿1-6?6alkyle, C¿3-7?cycloalkyle, C¿1-6?6alkyle oxyC1 6 alkyle, di(C¿1-6?alkyle)aminoC¿1-6?alkyle, aryle ou hétéroaryle; chaque R¿2? représente indépendament halo, C¿1-6?alkyle, C¿1-6?alkyloxy, C¿1-6?alkylthio, polyhaloC¿1-6?alkyle, polyhaloC¿1-6?alkyloxy, cyano, aminocarbonyle, amino, mono-ou di(C¿1-4?alkyle)amino, nitro, aryle ou aryloxy; R¿3? représente hydrogène, cyano, C¿1-6?6alkyle éventuellement substitué, C(=O)-O-R¿5?, C(=O)-NR¿6a?R¿6b?, C(=S)-NR¿6a?R¿6b?, S(=O)¿2?-NR¿6a?R¿6b? ou C(=O)-R¿7?; R¿4? représente hydrogène ou C¿1-6?alkyle; n est 1, 2, 3, 4 ou 5; Z représente un système de cycle cyclique. C'est invention concerne aussi un processus de préparation des composés représentés par la formule (I), leur utilisation comme antagonistes CCR2 et des compositions pharmaceutiques comprenant ces composés.

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