Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Cyclopentanohydrophenanthrene ring system doai
Patent
1992-08-03
1994-12-06
Richter, Johann
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Cyclopentanohydrophenanthrene ring system doai
514177, 514178, 514180, 514182, A61K 3156
Patent
active
053710770
ABSTRACT:
Pharmaceutical compositions are provided for lowering the activity of HMG-CoA reductase and/or lowering serum cholesterol, comprising an amount effective to lower the activity of HMG-CoA reductase and/or lower serum cholesterol of a side chain derivatized 15-oxygenated sterol having the formula (I): ##STR1## the basic ring structure being saturated or unsaturated, wherein R.sub.1 is --OH, .dbd.O, --OR.sub.7, ##STR2## a sulfate group, a sugar moiety, or a Mg, Na, or K salt of a sulfate group;
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S. Swaminathan et al., "Inhibitors of Sterol Synthesis. 3.beta.,25-Dihydroxy-5.alpha.-cholest-8(14)-en-15-one, an Active Metabolite of 3.beta.-Hydroxy-5.alpha.-cholest-8(14)-en-15-one," J. Med. Chem., 35, 793-795 (1992).
J. E. Herz et al., "Inhibitors of Sterol Synthesis. A Highly Efficient and Specific Side Chain Oxidation of 3.beta.-Acetoxy-5.alpha.-cholest-8(14)-en-15-one for Construction of Metabolites and Analogs of the 15-Ketosterol," J. Lipid Res., 33(4), 579-598 (1992).
J. E. Herz et al., "Inhibitors of Sterol Synthesis. An Efficient and Specific Side Chain Oxidation of 3.beta.-Hydroxy-5.alpha.-cholest-8(14)-en-15-one. Facile Access to its Metabolites and Analogs," Tetrahedron Lett., 32(32), 3923-3926 (1991).
J. E. Herz et al., "Inhibitors of Sterol Synthesis. Synthesis and Spectral Properties of 3.beta.-Hydroxy-24-dimethylamino-5.alpha.-chol-8(14)-en-15-one and its Effects on HMG-CoA Reductase Activity in CHO-K1 Cells," Chem. Phys. Lipids, 60, 61-69 (1991).
M. M. Kabat, "Synthesis of 26,27-Difluoro-25-hydroxy- and (25R,S)-27-Fluoro-25,26-Dihydroxy-cholesterol Derivatives from Methyl 3.beta.-Hydroxy 5-Cholenate," J. Fluorine Chem., 49, 207-215 (1990).
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Herz Josef E.
Schroepfer, Jr. George J.
Swaminathan Shankar
Wilson William K.
Kestler Kimberly J.
Richter Johann
William Marsh Rice University
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