Organic compounds -- part of the class 532-570 series – Organic compounds – Phosphorus acids or salts thereof
Patent
1995-06-05
1996-10-22
Richter, Johann
Organic compounds -- part of the class 532-570 series
Organic compounds
Phosphorus acids or salts thereof
544232, 544243, 544244, 546 22, 546 23, 548112, 548113, 549218, 549220, C07F 938
Patent
active
055678416
ABSTRACT:
.alpha.-Phosphonosulfonate 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 H, alkyl, arylalkyl or aryl; R.sup.4 is H, alkyl, aryl, arylalkyl, or cycloalkyl;, 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 and or prodrug esters of the phosphonic (phosphinic) and/or sulfonic acids.
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Biller Scott A.
Dickson, Jr. John K.
Lawrence R. Michael
Magnin David R.
Sulsky Richard B.
Ambrose Michael G.
Bristol--Myers Squibb Company
Richter Johann
Rodney Burton
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