Lek Pharmaceuticals D.d.

Klementina Fon Tacer

Darko Kocjan

Breda Rode

Damjana Rozman

The novel derivatives of pyridilethanol (phenylethyl) amines of formula I are described wherein n is an integer from 1 to 4, Ris a hydrogen atom, hydroxyl group or lower Calkoxy group Ris a hydrogen atom or a straight or branched lower Calkyl group X, is hydrogen, fluorine, chlorine, bromine, hydroxyl group, trifluoromethyl group, 3,4-di-Cl,2,4-di-Cl or lower Calkoxy 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).

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

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Ljubljana, Slovenia

Klementina Fon Tacer