Isoprenoid phosphinylformic acid squalene synthetase...

C - Chemistry – Metallurgy – 07 – F

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C07F 9/38 (2006.01) A61K 31/66 (2006.01) A61K 31/695 (2006.01) C07F 9/30 (2006.01) C07F 9/32 (2006.01) C07F 9/40 (2006.01)

Patent

CA 2023763

HX28 Abstract ISOPRENOID PHOSPHINYLFORMIC ACID SQUALENE SYNTHETASE INHIBITORS AND METHOD Compounds which are inhibitors of cholesterol biosynthesis (by inhibiting de novo squalene biosynthesis), and thus are useful as hypocholesterolemic agents and antiatherosclerotic agents, are provided which have the structure Image wherein R2 is a metal ion, lower alkyl or H; R3 is a metal ion or lower alkyl; R is R1-(CH2)n-, R1-(CH2)m-O- or R1-(CH2)m-OCH2-, wherein n is 1 to 4 and m is 0 to 3, and R1 is R5-Q1-Q2-Q3- wherein R5, Q1, Q2 and Q3 are as defined herein. New intermediates, new methods of preparation and a method for using such compounds to inhibit cholesterol biosynthesis are also provided.

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