Oxadiazole derivatives with crth2 receptor activity

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 271/06 (2006.01) A61K 31/4245 (2006.01) A61P 11/00 (2006.01) C07D 413/04 (2006.01)

Patent

CA 2631652

Compounds of formula (I) are CRTH2 ligands, useful for treatment of inflammatory, autoimmune, respiratory or allergy disease: wherein R1 is hydrogen or methyl and R2 is optionally substituted cycloalkyl, or optionally substituted non-aromatic heterocyclyl having 4 to 6 ring atoms; or R1 and R2, taken together with the carbon atom to which they are attached form an optionally substituted cycloalkyl, or optionally substituted non-aromatic heterocyclyl ring having 4 to 6 ring atoms; R is hydrogen or an optional substituent; the phenyl ring containing the substituent R is optionally substituted by 1 , 2 or 3 optional substituents; A is hydrogen or C1-C3 alkyl; and ring Ar is an optionally substituted phenyl or 5- or 6- membered monocyclic heteroaryl ring.

L~invention concerne des composés de formule (I), lesdits composés étant des ligands de CRTH2 utiles pour le traitement de maladies inflammatoires, auto-immunes, respiratoires ou allergiques : R1 représentant l~hydrogène ou un méthyle et R2 représentant un cycloalkyle éventuellement substitué ou un hétérocyclyle non aromatique éventuellement substitué ayant de 4 à 6 atomes cycliques ; ou R1 et R2 forment ensemble avec l~atome de carbone auquel ils sont attachés un cycloalkyle éventuellement substitué ou un cycle hétérocyclyle non aromatique éventuellement substitué ayant de 4 à 6 atomes cycliques ; R représentant l~hydrogène ou un éventuel substituant ; le cycle phényle contenant le substituant R étant éventuellement substitué par 1, 2 ou 3 substituants éventuels ; A représentant l~hydrogène ou un alkyle en C1 à C3 ; et le cycle Ar représentant un cycle phényle éventuellement substitué ou hétéroaryle monocyclique à 5 ou 6 éléments.

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