Bisphosphonate squalene synthetase inhibitors and method

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United States of America Patent

PATENT NO 5157027
SERIAL NO

07699429

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Abstract

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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 ##STR1## and analogs thereof, wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are the same or different and are H, lower alkyl, a metal ion or a prodrug ester; R.sup.5 is H, halogen or lower alkyl; Zq is substituted alkenyl, substituted alkynyl, mixed alkenyl-alkynyl or substituted phenylalkyl or, phenylalkenyl or phenylalkynyl, or alkyl, including all stereoisomers thereof. New methods for using such compounds to inhibit cholesterol biosynthesis are also provided.

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Patent Owner(s)

Patent OwnerAddress
E R SQUIBB & SONS INCP O BOX 4000 PRINCETON NEW JERSEY 08543-4000

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Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Biller, Scott A Ewing, NJ 50 1452
Magnin, David R Hamilton, NJ 31 1184

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