7-oxo pyridopyrimidines as inhibitors of a cellular...

C - Chemistry – Metallurgy – 07 – D

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C07D 471/04 (2006.01) A61K 31/519 (2006.01) A61P 29/00 (2006.01) A61P 31/00 (2006.01) C07D 221/00 (2006.01) C07D 239/00 (2006.01)

Patent

CA 2420286

Compounds of formula (I) wherein R1 is hydrogen or alkyl; R2 is substituted cycloalkyl, heterosubstituted cycloalkyl, heteroalkylsubstituted cycloalkyl, heterosubstituted cycloalkyl-aryl, heterocyclyl, heterocyclyl spiro cycloalkyl, aralkoxy, alkoxy, -alkylene-S(O)n-alkyl(where n is 1 or 2) or - SO2Ar2; R3 is hydrogen, amino, monoalkylamino, dialkylamino, acylamino, -NRa- C(=O)-Rb (where Ra is hydrogen or alkyl and Rb is hetericyclyl or heteroalkyl) alkyl, cycloalkyl, aryl, aralkyl, haloalkyl, heteroalkyl, cyanoalkyl, - alkylene-C(O)-R (where R is hydrogen, alkyl, hydroxy, alkoxy, amino, monoalkylamino or dialkylamino) acyl, or phthalimidoalkyl; and each of Ar1 and Ar2 is independently aryl, and their use for treatment of disorders selected from the group consisting of arthritis, Crohns disease, Alzheimer's disease, irritable bowel syndrome, adult respiratory distress syndrome, and chronic obstructive pulmonary disease.

L'invention concerne des composés de formule (I), dans laquelle R?1¿ représente un hydrogène ou un alkyle, R?2¿ représente un cycloalkyle substitué, un cycloalkyle hétérosubstitué, un cycloalkyle hétéroalkylsubstitué, un cycloalkyl-alkyle hétérosubstitué, un hétérocyclyle, un spiro cycloalkyle hétérocyclyle, un aralcoxy, un alcoxy, un -alkylène-S(O)¿n?-alkyle (dans lequel n est égal à 1 ou 2) ou -SO¿2?Ar?2¿; R?3¿ représente un hydrogène, un amino, un monoalkylamino, un dialkylamino, un acylamino, -Nr?a¿.C(=O)-R?b¿ (dans lequel R?a¿ désigne un hydrogène ou un alkyle et R?b¿ désigne un hétérocyclyle ou un hétéroalkyle), un alkyle, un cycloalkyle, un aryle, un aralkyle, un haloalkyle, un hétéroalkyle, un cyanoalkyle, un -alkylène-C(O)-R (dans lequel R désigne un hydrogène, un alkyle, un hydroxy, un alcoxy, un amino, un monoalkylamino ou un dialkylamino), un acyle ou un phtalimidoalkyle; Ar?1¿ et Ar?2¿ représentent, de manière indépendante, un aryle. L'invention concerne également l'utilisation de ces composés dans le traitement de maladies sélectionnées dans le groupe comprenant l'arthrite, la maladie de Crohn, la maladie d'Alzheimer, le syndrome du côlon irritable, la détresse respiratoire adulte et la maladie respiratoire obstructive chronique.

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