Novel derivatives of pyridilethanol (phenylethyl) amines as inhibitors of cholesterol biosynthesis, process for their preparation and pharmaceutical compositions containing them

摘要

The novel derivatives of pyridilethanol (phenylethyl) amines of formula I are described wherein n is an integer from 1 to 4, R₁ is a hydrogen atom, hydroxyl group or lower C_1-6alkoxy group R₂ is a hydrogen atom or a straight or branched lower C_1-6alkyl group X, is hydrogen, fluorine, chlorine, bromine, hydroxyl group, trifluoromethyl group, 3,4-di-Cl,2,4-di-Cl or lower C_1-6alkoxy group, the enantiomers, diastereoisomers or racemates thereof or the physiologically acceptable acid addition salts thereof which are ligands of sigma receptors for inhibiting cholesterol biosynthesis and are thus appropriate for the treatment of hypercholesterolemia and hyperlipemia in humans. The greatest lowering of cholesterol was observed by 1-(d-pyridyl)-2-(N-(2-(3,4-dicholorophenyl)ethyl-N-propylamino)ethanol in the form of dihydrobromide salt (signature BK-35, 2HBr).