Optically pure 4-alkenyl- or 4-alkanyl-2-hydroxytetronic acids a

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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Details

514474, 549315, 549316, A61K 31365, C07D30762

Patent

active

055041078

ABSTRACT:
The present invention relates to a method for synthesis of optically pure 4-alkenyl or 4-alkanyl-2-hydroxytetronic acids from an optically pure aldehyde. The invention further relates to the use of such optically pure compounds as potent inhibitors of platelet aggregation by working at the level of cyclooxygenase. The invention further relates to the pharmaceutical use of such compounds in the treatment of coronary artery diseases, especially in the treatment and/or prevention of atherosclerosis.

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Witiak and Tehim, "Synthetic approaches to 4-spiro-2-hydroxytetronic acids" J. Org. Chem., 1987, 52:2324-2327.
Witiak et al., "Hypocholesterolemic and antiaggregatory properties of 2-hydroxytetronic acid redox and analogues and their relationship to clofibric acid" J. Med. Chem., 1986, 29:2170-2174.
Witiak et al., "Comparative antiaggregatory activity in human platelets of a benzopyranone aci-reductone, clofibric acid, and a 2,3 dihydrobenzofuran analogue" J. Med. Chem., 1982, 25:90-93.

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