4-hydroxytetrahydropyran-2-ones and the corresponding dihydroxyc

Details 4-hydroxytetrahydropyran-2-ones and the corresponding dihydroxyc 4-hydroxytetrahydropyran-2-ones and the corresponding dihydroxyc

1990-09-06

1994-03-15

Ivy, C. Warren

Organic compounds -- part of the class 532-570 series

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

560 17, 560 60, 560 61, 560 62, C07D30930, C07C 69612, C07C32104, C07C32126

Patent

active

052947246

ABSTRACT:
4-Hydroxytetrahydropyran-2-ones and the corresponding dihydroxycarboxylic acid derivatives, salts and esters, process for their preparation, their use as pharmaceuticals, and pharmaceutical preparations and precursors.
Compounds of the formula I ##STR1## and the corresponding open-chain dihydroxycarboxylic acids of the formula II ##STR2## in which X, Y, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 have the meanings indicated, and also their pharmacologically tolerable salts with bases and their pharmacologically tolerable esters, processes for the preparation of these compounds, their use as pharmaceuticals and pharmaceutical preparations are described. In addition, compounds of the formula III ##STR3## in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, X and Y have the meanings indicated are described.

REFERENCES:
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Nestel et al., "Effects of Probucol on Low Density Lipoprotein Removal and High Density Lipoprotein Synthesis," Artheroscierosis, 38, pp. 203-209 (1981).
Eder, "A Symposium: New Developments in the Treatment of Hypercholesterolemia--Probucol," The American Journal of Cardiology, vol. 57, No. 16, pp. 1H-54H (1986).
Fogelman, et al., "Malondialdehyde alteration of low density lipoproteins leads to cholesteryl ester accumulation in human monocyte-macrophages," Proc. Natl. Acad. Sci., USA, vol. 77, No. 4, pp. 2214-2218 (1980).
Stokker, et al., "3-Hydroxy-3-methylglutaryl-coenzyme A Reductase Inhibitors. 1. Structural Modification of 5-Substituted 3,5-Dihydroxypentanoic Acids and Their Lactone Derivatives," J. Med. Chem 1985, vol. 28, pp. 347-358 (1985).

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