Pharmaceutical pyrazole compositions useful as inhibitors of...

A - Human Necessities – 61 – K

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A61K 31/415 (2006.01) A61K 31/4155 (2006.01) A61K 31/4439 (2006.01) A61K 31/455 (2006.01)

Patent

CA 2203517

A method for selectively inhibiting a kinase is disclosed, which comprises contacting a composition containing a kinase with a compound of formula (I), wherein: R1 is lower alkyl, lower hydrocarbyl, aryl lower alkyl, heteroaryl lower alkyl, 5- or 6-membered heterocyclic aromatic, polyaromatic, polyaromatic carbonyl, polyheteroaromatic or polyheteroaromatic carbonyl; R2 is lower alkyl, lower hydrocarbyl, aryl lower alkyl, heteroaryl lower alkyl, 5- or 6-membered heterocyclic aromatic, lower hydrocarboyl, 5- or 6-membered heterocyclic aromatic carbonyl, polyaromatic or polyheteroaromatic; R3 is H or lower alkyl; R5 is H, lower alkyl, lower hydrocarbyl, aryl lower alkyl, heteroaryl lower alkyl, 5- or 6-membered heterocyclic aromatic, halogen, or cyano; and R6 is H or lower hydrocarboyl.

Procédé d'inhibition sélective d'une kinase, consistant à mettre une composition contenant une kinase en contact avec un composé de la formule (I), dans laquelle R¿1? représente alkyle inférieur, hydrocarbyle inférieur, arylalkyle inférieur, hétéroarylalkyle inférieur, un noyau hétérocyclique aromatique, un noyau polyaromatique, un carbonyle polyaromatique, un noyau polyhétéroaromatique ou un carbonyle polyhétéroaromatique à 5 ou 6 chaînons; R¿2? représente alkyle inférieur, hydrocarboyle inférieur, arylalkyle inférieur, hétéroarylalkyle inférieur, un noyau hétérocyclique aromatique à 5 ou 6 chaînons, hydrocarbyle inférieur, carbonyle aromatique hétérocyclique, un noyau polyaromatique ou un noyau polyhétéroaromatique à 5 ou 6 chaînons; R¿3? représente H ou alkyle inférieur; R¿5? représente H, alkyle inférieur, hydrocarbyle inférieur, arylalkyle inférieur, hétéroarylalkyle inférieur, un noyau aromatique hétérocyclique à 5 ou 6 chaînons, halogène ou cyano; et R¿6? représente H ou hydrocarboyle inférieur.

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