| abstract |
It is described α-phosphonosulfonate compounds which inhibit the enzyme squalene synthetase and thereby inhibit cholesterol biosynthesis. The compounds have the formula wherein R is OR5 or R5a; R 3 and R 5 are independently H, alkyl, arylalkyl, aryl or cycloalkyl; R5a is H, alkyl, arylalkyl or aryl; R 4 is H, alkyl, aryl, arylalkyl or cycloalkyl; z is H, halogen, lower alkyl or lower alkenyl; and R 1 is a lipophilic group containing at least 7 carbon atoms and is alkyl, alkenyl, alkynyl, mixed alkenyl alkynyl, aryl, arylalkyl, cycloalkyl, cycloalkylalkyl, heteroaryl, heteroarylalkyl, cycloheteroalkyl, cycloheteroalkylalkyl; further defined above; including pharmaceutically acceptable salts and / or prodrug esters of the phosphonic (phosphine) and / or sulfonic acids. |