.alpha.-phosphonosulfinate squalene synthetase inhibitors...

C - Chemistry – Metallurgy – 07 – F

Patent

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C07F 9/38 (2006.01) A61K 31/66 (2006.01) C07F 9/30 (2006.01) C07F 9/40 (2006.01) C07F 9/547 (2006.01) C07F 9/572 (2006.01) C07F 9/58 (2006.01) C07F 9/60 (2006.01) C07F 9/655 (2006.01) C07F 9/6553 (2006.01)

Patent

CA 2155986

.alpha.-Phosphonosulfinate compounds are provided which inhibit the enzyme squalene synthetase and thereby inhibit cholesterol biosynthesis. These compounds have the formula Image wherein R2 is OR5 or R5a; R3 and R5 are independently H, alkyl, arylalkyl, aryl or cycloalkyl; R5a is alkyl, arylalkyl or aryl; R4 is H or pharmaceutically acceptable cation;, Z is H, halogen, lower alkyl or lower alkenyl; and R1 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.

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