Hydroxyphosphinyl phosphonate squalene synthetase inhibitors...

Details Hydroxyphosphinyl phosphonate squalene synthetase inhibitors... Hydroxyphosphinyl phosphonate squalene synthetase inhibitors...

C - Chemistry, Metallurgy

07

F

C07F 9/38 (2006.01) A61K 31/66 (2006.01) C07F 9/48 (2006.01)

Patent

CA 2104748

Abstract HYDROXYPHOSPHINYL PHOSPHONATE SQUALENE SYNTHETASE INHIBITORS AND METHOD Hydroxyphosphinyl phosphonate compounds are provided which inhibit the enzyme squalene synthetase and thereby inhibit cholesterol biosynthesis. These compounds have the formula Image wherein R2, R3 and R4 are independently H, alkyl, metal ion or a prodrug ester; and R1 is a lipophilic group which contains at least 6 carbons and is alkyl, alkenyl, alkynyl, mixed alkenyl- alkynyl, a hetero-containing moiety as defined herein, or a phenylalkyl or phenylalkenyl group including those containing a biphenyl group.

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