SUBSTITUTED AMINOPYRIMIDINES AS ANGIOTENSINE II ANTAGONISTS

摘要

There are disclosed compounds of formula (I) wherein R1 is alkyl of 1-6 carbon atoms, perfluoroalkyl of 1-6 carbon atoms, cycloalkyl of 3-7 carbon atoms, fluoro, chloro, or bromo; R2 is hydrogen, alkyl of 1-6 carbon atoms, perfluoroalkyl of 1-6 carbon atoms, trifluoromethylalkyl of 1-6 carbon atoms, cycloalkyl of 3-7 carbon atoms, alkoxy of 1-6 carbon atoms, hydroxy, fluoro, chloro, bromo, or cyano; R3 is hydrogen, perfluoroalkyl of 1-6 carbon atoms, trifluoromethylalkyl of 1-6 carbon atoms, alkyl of 1-6 carbon atoms, alkenyl of 3-5 carbon atoms, alkynyl of 3-5 carbon atoms, aryl of 6-10 carbon atoms; aryl of 6-10 carbon atoms substituted with fluorine, chlorine or bromine; aralkyl of 7-12 carbon atoms; aralkyl of 7-12 carbon atoms substituted with alkyl of 1-6 carbon atoms, fluorine, chlorine or bromine; alkoxy of 1-6 carbon atoms or alkyl of 1-6 carbon atoms, cycloalkyl of 3-7 carbon atoms, pyridylmethyl, thienylmethyl, fluoro, chloro, bromo, cyano, hydroxyalkyl of 1-6 carbon atoms, (CH¿2?)mCO2R?5, (CH¿2)mCONR5R6; or taken together with R2 is a methylene chain of 2-3 carbon atoms; m is 1 to 4; n is 0 to 3; R4 is hydrogen, alkyl of 1-6 carbon atoms, aryl of 6-10 carbon atoms, aryl of 6-10 carbon atoms substituted with halogen, alkylcarbonyl of 2-6 carbon atoms, pyridyl, or pyrimidinyl; R?5 and R6¿ are H or alkyl of 1-6 carbon atoms; Ar1 is (a), (b), or (c); Ar2 is (d), (e), (f) or (g); wherein X is CO¿2?H, CO2R?7¿, NHSO¿2?CF3, or (h); wherein R?7¿ is hydrogen, alkyl of 1-6 carbon atoms, benzyl, triphenylmethyl, or Sn(alkyl of 1-6 carbon atoms)¿3?; and the pharmaceutically acceptable salts thereof, which by virtue of their ability to antagonize angiotensin II are useful for the treatment of hypertension and congestive heart-failure. The compounds are also useful for reducing lipid levels in the blood plasma and are thus useful for treating hyperlipidemia and hypercholesterolemia. Also disclosed are processes for the production of said compounds and pharmaceutical compositions containing said compounds.