Phosphorus-containing HMG-CoA reductase inhibitors

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

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514274, 544243, A61K 31505, C07F 902

Patent

active

052023273

ABSTRACT:
Novel phosphorus-containing compounds which inhibit the activity of HMG-CoA reductase, including a 5-pyrimidinyl-containing moiety. Pharmaceutical compositions and methods of use for the treatment or prevention of hypercholesterolemia, atheroschlerosis, hyperlipoproteinaemia and hyperlipidemia are provided.

REFERENCES:
patent: 4904646 (1990-02-01), Karanewsky et al.
patent: 4925852 (1990-05-01), Kesseler et al.
Karanewsky, et al.; Phosphorus-Containing Inhibitors of HMG-CoA Reductase. 1. 4-[2-Arylethyl)Hydroxyphosphinyl]-3-Hydroxybutanoic Acids: A New Class of Cell-Selective Inhibitors of Cholesterol Biosynthesis. J. Med. Chem. v. 33, no. 11, p. 2952, 1990.
Relationahip Between Tissue Selectivity and Lipophilicity for Inhibitors of HMG-CoA Reductase, Roth, et al.; J. Med. Chem. v. 34, pp. 463-466, 1991.

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