Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Phosphorus containing other than solely as part of an...
Patent
1988-01-11
1989-10-03
Sutto, Anton H.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Phosphorus containing other than solely as part of an...
558134, 558155, 562 21, A61K 3166, C07F 940
Patent
active
048717215
ABSTRACT:
Compounds which are useful as inhibitors of cholesterol biosynthesis and thus as hypocholesterolemic agents are provided which have the structure ##STR1## Z is --(CH.sub.2).sub.n -- or --(CH.sub.2).sub.p --CH.dbd.CH--(CH.sub.2).sub.m --, wherein n is 1 to 5; p is 0, 1 or 2; m is 0, 1 or 2;
REFERENCES:
Poulter, C. D., et al., Biosynthesis of Isoprenoid Compounds, "Conversion of Farnesyl Pyrophosphate to Squalene", vol. 1, Chapter 8, pp. 413-441, J. Wiley and Sons, 1981.
Faust, J. R. et al. Proc. Nat. Acad Sci., U.S.A., "Squalene Synthetase Activity in Human Fibroblasts: Regulation via the Low Density Lipoprotein Receptor", 1979, 76, 5018-5022.
de Montellano, P. Ortiz et al., J. Med. Chem., "Inhibition of Squalene Synthetase by Farnesyl Pyrophosphate Analogues", 1977, 20, 243-249.
Corey and Volante, J. Am. Chem. Cos. "Application of Unreactive Analogs of Terpenoid Pyrophosphates to Studies of Multistep Biosynthesis, Demonstration that `Presqualene Pyrophosphate' is an Essential Intermediate on the Path to Squalene", 1976, 98, 1291-3.
Sandifer, R. M. et al., J. Am. Chem. Soc., 1982, 104, 7376-8, "Squalene Synthetase, Inhibition by an Ammonium Analogue of a Carbocationic Intermediate in the Conversion of Presqualene Pyrophosphate to Squalene".
Bertolino, A. et al., Biochim. Biophys. Acta., 1978, 530, 17-23, "Polyisoprenoid Amphiphilic Compounds as Inhibitors of Squalene Synthesis and Other Microsomal Enzymes".
Poulter, C. D. et al., J. Org. Chem., 1986, 51, 4768-4779, "Phosphorylation of Isoprenoid Alcohols".
Poulter, C. D. et al., J.A.C.S., 1987, 109, 5542, "Methane and Difluoromethanediphosphonate Analogues of Geranyl Diphosphate: Hydrolysis-Inert Alternate Substrates".
McClard, R. W. et al., J. Am. Chem. Soc., 1987, 109, 5544-5545, "Novel Phosphonylphosphinyl (P-C-P-C) Analogues of Biochemically Interesting Diphosphates, Syntheses and Properties of P-C-P-C Analogues of Isopentenyl Diphosphate and Dimethylallyl Diphosphate".
Capson, Phd Dissertation, Jun. 1987, Dept. of Med. Chem. Univ., Utah, Abstract, Table d Contents, pp. 16, 17, 40-43, 48-51, Summary.
E. R. Squibb & Sons Inc.
Rodney Burton
Sutto Anton H.
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