| abstract |
α-Phosphonocarboxylate compounds are provided which inhibit the enzyme squalene synthetase and thereby inhibit cholesterol biosynthesis. These compounds have the formulan n wherein R¹ is a lipophilic group which contains at least 7 carbons and is substituted alkyl, optionally substituted cycloalkyl, optionally substituted cycloalkylalkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted arylalkyl or optionally substituted aryl; n Z is H, halogen, hydroxy, hydroxyalkyl or lower alkyl; n R² and R³ are independently H, metal ion or other pharmaceutically acceptable cation, or a prodrug ester; n R⁴ is H, metal ion or other pharmaceutically acceptable cation, lower alkyl, lower alkenyl, arylalkyl, aryl or a prodrug ester. |