Novel thienopyrimidine derivatives, processes for the preparation thereof and therapeutic uses thereof.

Abstract

The invention relates to compds. of formula I, process for the prepn. thereof and therapeutic use thereof. Compds. of formula I wherein R6 is CONH2 and CRaRbOH; Ra and Rb are independently H and C1-6 alkyl; RaRb are independently 3- to 5-membered cycloalkyl; R is (un)substituted Ph and (un)substituted heteroaryl; R7 is (un)substituted aryl and (un)substituted heteroaryl; and pharmaceutically acceptable salts thereof, are claimed. Example compd. II was prepd. by amination of Me 7-(2-methoxyphenyl)-2-(methylsulfonyl)thieno[3,2-d]pyrimidine-6-carboxylate with N-[4-(1-methylpiperidin-4-yl)-2-(propan-2-yloxy)phenyl]formamide; the resulting Me 7-(2-methoxyphenyl)-2-{[4-(1-methylpiperidin-4-yl)-2-(propan-2-yloxy)phenyl]amino}thien [3,2-d]pyrimidine-6-carboxylate underwent amidation to give compd. II. The invention compds. were evaluated for their ALK kinase inhibitory activity. From the assay, it was detd. that compd. II exhibited IC50 value of 7 nM. [on SciFinder(R)]