2,4,5-trisubstituted thiazolyl derivatives and their...

C - Chemistry – Metallurgy – 07 – D

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C07D 277/24 (2006.01) A61K 31/506 (2006.01) C07D 417/04 (2006.01)

Patent

CA 2451981

This invention concerns the use of a compound of formula (I), a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein Z is halo; C1-6alkyl; C1- 6alkyl substituted with hydroxy, carboxyl, cyano, amino, mono -or di(C1- 6alkyl)amino, aminocarbonyl, mono -or di(C1-6alkyl)aminocarbonyl, C1- 6alkyloxycarbonyl or C1-6alkyloxy; polyhaloC1-4alkyl; C1-4alkyloxy; cyano; amino; aminocarbonyl; mono -or di(C1-6alkyl)aminocarbonyl; C1- 6alkyloxycarbonyl; C1-6alkylcarbonyloxy; H2N-S(=O)2-; mono -or di(C1- 6alkyl)amino-S(=O)2; -C(=N-Rx)NRyRz; Q is an optionally substituted carbocycle or an optionally substituted heterocycle; L is substituted phenyl or an optionally substituted monocyclic 5 or 6-membered partially saturated or aromatic heterocycle or a bicyclic partially saturated or aromatic heterocycle; aryl is optionally substituted phenyl; for the manufacture of a medicament for the prevention or the treatment of diseases mediated through TNF-.alpha. and/or IL-12.

L'invention concerne l'utilisation d'un composé de formule (I), d'un <i>N</i>-oxyde, d'un sel d'addition acceptable sur le plan pharmaceutique, d'une amine quaternaire et d'une forme isomère sur le plan stéréochimique de celui-ci. Dans cette formule, Z désigne un halo; un alkyle en C¿1-6?; un alkyle en C¿1-6? substitué par un hydroxy, un carboxyle, un cyano, un amino, un mono -ou di(C¿1-6?alkyl)amino, un aminocarbonyle, un mono -ou di(C¿1-6?alkyl)aminocarbonyle, un alkyloxycarbonyle en C¿1-6? ou un alkyloxy en C¿1-6?; un polyhaloC¿1-4?alkyl; un alkyloxy en C¿1-4?; un cyano; un amino; un aminocarbonyle; un mono -ou di(C¿1-6?alkyl)aminocarbonyle; un alkyloxycarbonyle en C¿1-6?; un alkylcarbonyloxy en C¿1-6?; H¿2?N-S(=O)¿2?-; un mono -ou di(C¿1-6?alkyl)amino-S(=O)¿2?; -C(=N-R?x¿)NR?y¿R?z¿; Q représente un carbocycle éventuellement substitué ou un hétérocycle éventuellement substitué; L désigne un phényle substitué ou un hétérocycle éventuellement substitué, monocyclique, à 5 ou 6 chaînons, partiellement saturé ou aromatique ou un hétérocycle bicyclique partiellement saturé ou aromatique; un aryle désigne un phényle éventuellement substitué; aux fins de fabrication d'un médicament destiné à la prévention ou au traitement de maladies induites par TNF-.alpha. et/ou IL-12.

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