Thiazole derivatives as a2b antagonists

Details Thiazole derivatives as a2b antagonists Thiazole derivatives as a2b antagonists

C - Chemistry, Metallurgy

07

D

C07D 417/04 (2006.01) A61K 31/501 (2006.01) A61K 31/506 (2006.01) A61P 11/00 (2006.01) C07D 417/14 (2006.01)

Patent

CA 2553010

Compounds of formula (I) in free or salt form, where Ar is phenyl substituted by one or more substituents selected from halogen, cyano and C1- C8-haloalkyl, or naphthyl, R1 is hydrogen, phenyl optionally substituted by one or more substituents selected from halogen, cyano, hydroxy, C1-C8-alkyl, C1-C8- haloalkyl, C1-C8-alkoxy, C1-C8-alkoxy-Cl-C8~ alkyl, carboxy, C1-C8- alkoxycarbonyl and acyloxy, or R1 is a 5- or 6- membered monovalent heterocyclic group, R2 is hydrogen, Cl-C8-alkyl, acyl or -CON(R3)R4, R3 and R4 are each independently hydrogen or C1-Cs-alkyl, or together with the nitrogen atom to which they are attached denote a 5- or 6- membered heterocyclic group, and Y is a pyrimidinyl or pyridazinyl group, optionally substituted by at least one C1-Cs-alkyl, C1-C8-alkoxy, C1-C8-alkylthio, C1-C8-alkyl amino, di(Cl- C8-alkyl) amino or acylamino group. The compounds are useful as pharmaceuticals.

La présente invention concerne des composés de formule (I) sous forme libre ou sous forme de sels. Dans la formule (I): Ar est phényle substitué par un ou plusieurs substituants choisis parmi halogène, cyano et haloalkyle en C¿1-? C¿8?, ou naphthyle; R?1¿ est hydrogène, phényle éventuellement substitué par un ou plusieurs substituants choisi parmi halogène, cyano, hydroxy, alkyle en C¿1?-C¿8?, haloalkyle en C¿1?-C¿8?, alcoxy en C¿1?-C¿8?, C¿1?-C¿8?-alcoxy-C¿l?-C¿8?- alkyle, carboxy, alcoxycarbonyle en C¿1?-C¿8? et acyloxy; ou R?1¿ est un groupe hétérocyclique monovalent à 5 ou 6 éléments; R?2¿ est hydrogène, alkyle en C¿l?-C¿8?, acyle ou -CON(R?3¿)R?4¿; R?3¿ et R?4¿ représentent chacun indépendamment hydrogène ou alkyle en C¿1?-C¿8?, ou forment avec l'atome d'azote auquel ils sont liés, un groupe hétérocyclique à 5 ou 6 éléments; Y est un groupe pyrimidinyle ou pyridazinyle, éventuellement substitué par au moins un groupe alkyle en C¿1?-C¿8?, alcoxy en C¿1?-C¿8?, alkylthio en C¿1?-C¿8?, alkylamino en C¿1?-C¿8?, di(C¿l?-C¿8?-alkyl) amino ou acylamino. Ces composés sont utiles en tant que produits pharmaceutiques.

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