3-EPI COMPOUNDS OF VITAMIN D3 AND USES THEREOF
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United States of America Patent
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Issued Date -
Jul 12, 2001
app pub date -
May 15, 1998
filing date -
May 16, 1997
priority date (Note) -
Abandoned
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Abstract
Novel 3-epi vitamin D.sub.3 compounds having the orientation of the substituent attached to the carbon at position 3 of the A-ring of vitamin D.sub.3 inverted from a beta (.beta.) to an alpha (.alpha.) configuration are described. These 3-epi vitamin D.sub.3 compounds were first identified as metabolites produced via a novel tissue-specific metabolic pathway which catalyzes the 3-.beta.-hydroxy epimerization of vitamin D.sub.3 compounds. Isolated 3-epimer forms of vitamin D.sub.3 compounds have been characterized and shown to have improved biological properties compared to their isomeric counterparts, such as reduced hypercalcemic activity and enhanced stability in vivo. The vitamin D.sub.3 compounds of the present invention can be used as substitutes for natural and synthetic vitamin D.sub.3 compounds.
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