Trans-6-[2-[2-(substituted-phenyl)-3- (or 4-) heteroaryl-5-substituted-1H-pyrrol-1-yl]-ethyl]tetrahydro-4-hydroxy-2H-p yran-2-one inhibitors of cholesterol biosynthesis
AssigneeWarner-Lambert Company
InventorsBruce D. Roth, Drago R. Sliskovic
Life of this patent
Estimating the term…
Abstract
Certain trans-6-[2-[2-(substituted-phenyl)-3- (or 4-)heteroaryl-5-substituted-1H-pyrrol-1-yl]ethyl]tetrahydro-4-hydroxy-2H-p yran-2-ones and the corresponding lactone-ring-opened acids are potent inhibitors of the enzyme 3-hydroxy-3-methylglutaryl-coenzyme A reductase (HMG CoA reductase) and are thus useful hypolipidemic or hypocholesterolemic agents. Pharmaceutical compositions containing such compounds, and a method of inhibiting the biosynthesis of cholesterol employing such pharmaceutical compositions are also disclosed.
Claims9
A compound of structural formula I ##STR6## wherein R.sub.1 is alkyl of from one to four carbon atoms, cyclopropyl, or trifluoromethyl;
- R.sub.2 and R.sub.3 are independently selected from hydrogen, alkyl of from one to four carbon atoms, chlorine, and fluorine;
- Het is a heteroaromatic ring selected from ##STR7## where R.sub.4 and R.sub.5 are hydrogen or alkyl of from one to four carbon atoms;
- or
- the corresponding lactone-ring opened hydroxy acid and the pharmaceutically acceptable salts thereof.
Dependencies are inferred from the claim text.