.alpha.-phosphonosulfinic squalene synthetase inhibitors
AssigneeBristol-Myers Squibb Company
InventorsR. Michael Lawrence, Scott A. Biller, Olga M. Fryszman
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AssigneeBristol-Myers Squibb Company
InventorsR. Michael Lawrence, Scott A. Biller, Olga M. Fryszman
Estimating the term…
.alpha.-Phosphonosulfinate compounds are provided which inhibit the enzyme squalene synthetase and thereby inhibit cholesterol biosynthesis. These compounds have the formula ##STR1## wherein R.sup.2 is OR.sup.5 or R.sup.5a ; R.sup.3 and R.sup.5 are independently H, alkyl, arylalkyl, aryl or cycloalkyl; R.sup.5a is alkyl, arylalkyl or aryl; R.sup.4 is H or pharmaceutically acceptable cation;, Z is H, halogen, lower alkyl or lower alkenyl; and R.sup.1 is a lipophilic group which contains at least 7 carbons and is alkyl, alkenyl, alkynyl, mixed alkenyl-alkynyl, aryl, arylalkyl, cycloalkyl, cycloalkylalkyl, heteroaryl, heteroarylalkyl, cycloheteroalkyl, cycloheteroalkylalkyl; as further defined above; including pharmaceutically acceptable salts.
A compound having the structure ##STR103## wherein R.sup.2 is OR.sup.5 or R.sup.5a,
A compound having the structure ##STR110## wherein R.sup.2 is OR.sup.5 or R.sup.5a,
3-Phenoxy-.alpha.-phosphonobenzenebutanesulfinic acid, or an ester thereof, a pharmaceutically acceptable salt thereof or a mixed ester salt.
##STR112## wherein x is 1 to 8 ##STR113## wherein m is 1 to 5;
Dependencies are inferred from the claim text.