Imidazopyrazine compounds and their methods for inhibiting protein kinases, preparation, pharmaceutical compositions and use in the treatment of protein kinase-associated diseases.

Abstract

The invention provides methods for inhibiting protein kinases selected from the group consisting of AKT, CHeckpoint kinase, Aurora kinase, Pim-1 kinase, and tyrosine kinase using imidazo[1,2-a]pyrazine compds. of formula I and methods of treatment, prevention, inhibition, or amelioration of one or more diseases assocd. with protein kinases using such compds. Compds. of formula I wherein R is H, halo, (un)substituted (hetero)aryl, (un)substituted cycloalkyl, (un)substituted arylalkyl, (un)substituted heterocyclyl, etc.; R1 is H, halo, and alkyl; R2 is alkyl, (un)substituted (hetero)aryl(alkyl), alkenyl, alkynyl, etc.; R3 is H, (un)substituted (hetero)aryl(alkyl), (un)substituted heterocyclyl(alkyl), (un)substituted (hetero)cycloalkyl, etc.; and their pharmaceutically acceptable salts, solvates, esters, and prodrugs thereof are claimed. Example compd. II was prepd. by amination of 3-(1-methylpyrazol-4-yl)-7-methylsulfonylimidazo[1,2-a]pyrazine with 3-(methylsulfonyl)aniline. All the invention compds. were evaluated for their protein kinase inhibitory activity (data given). [on SciFinder(R)]