.alpha.-phosphonocarboxylate squalene synthetase inhibitors

Details .alpha.-phosphonocarboxylate squalene synthetase inhibitors .alpha.-phosphonocarboxylate squalene synthetase inhibitors

1992-12-09

1994-05-17

Lee, Mary C.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Carbohydrate doai

514 54, 514120, 558179, 558182, 560102, 560183, 560205, 560219, 562 24, A61K 3173, A61K 3166, C07F 940, C07F 938

Patent

active

053128141

ABSTRACT:
.alpha.- Phosphonocarboxylate compounds are provided which inhibit the enzyme squalene synthetase and thereby inhibit cholesterol biosynthesis. These compounds have the formula ##STR1## wherein R.sup.1 is a lipophilic group which contains at least 7 carbons and is substituted alkyl, optionally substituted cycloalkyl, optionally substituted cycloalkylalkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted arylalkyl or optionally substituted aryl;

REFERENCES:
patent: 3313735 (1967-04-01), McCune
patent: 4525289 (1985-06-01), Howie et al.
Snider, B. B. et al. J. Org. Chem. 1983, 48(21), 3685-3689.
Chem. Abstr. 1992, 117(11), 111841; Li, Y. et al. Chin. Chem. Lett. 1992, 3(1), 15-18.
Marshall, J. A. et al. J. Org. Chem. 1986, 51(10), 1735-1741.
Eriksson, B. et al, "Pyrophosphate Analogues as Inhibitors of DNA Polymerases of Cytomegalovirus, Herpes Simplex Virus and Cellular Origin," Biochimica et Biophysica Acta, 1982, 696, 115-123.
Lofgren, B. et al, "Inhibition of RNA- and DNA-dependent duck hepatitis B virus DNA polymerase activity by nucleoside and pyrophosphate analogs," Antiviral Research, 1989, 12, 301-310.
Widell, A. et al, "Influence of twenty potentially antiviral substances on in vitro multiplication of hepatitis A virus," Antiviral Research, 1986, 6, 103-112.
Maurer, E. et al, "Long Chain .alpha.-Phosphono Fatty Acids, Salts and Esters," J. Am. Oil Chemists' Soc., 1964, 41(3), 206-208.
Ackerman, B. et al, "Phosphorus Derivatives of Fatty Acids. III..sup.2 Trialkyl .alpha.-Phosphonates" J. Am. Chem. Soc., 1957, 79, 6524-6526.
Eriksson, B. et al, "Inhibition of Herpesvirus DNA Polymerases by Foscarnet and Related Pyrophosphate Analogues" Proc. Int. Congr. Chemother. 13th, 1983, 6, 114/29-114/32.
Okamoto, Y. et al, "The properties of (.alpha.-carboxy-n-alkyl)phosphonic acids" Kogyo Kagaku Zasshi, 1966, 69(9), 1871-1875.

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