1,3-diaclyated,26,27-alkyl/haloalkyl vitamin d3 compounds...

A - Human Necessities – 61 – K

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A61K 31/59 (2006.01) C07C 401/00 (2006.01)

Patent

CA 2539708

The invention provides (1,3)di-acylated vitamin D3 analogs of cholecalciferol, substituted at carbon (20) with methyl or cyclopropyl wherein carbon (16) is a single or double bond, and carbon (23) is a single, double, or triple bond. Various alkyl or haloalkyl substitutions are incorporated at carbon (25). The invention provides pharmaceutically acceptable esters, salts, and prodrugs thereof. Methods for using the compounds to treat vitamin D3 associated states, and pharmaceutical compositions containing the compounds are also disclosed.

L'invention concerne des analogues de la vitamine D¿3? (1,3)di-acylatée de cholécalciférol, substitué sur le carbone (20) par du méthyle ou du cyclopropyle, le carbone (16) étant en liaison simple ou double, et le carbone (23) est une liaison simple, double ou triple. De nombreuses substitutions d'alkyle ou d'haloalkyle sont incorporés dans le carbone (25). L'invention concerne des esters pharmaceutiquement acceptables, leurs sels ou leurs promédicaments. L'invention concerne également des procédés pour utiliser les composés dans le traitement des états pathologiques associés à la vitamine D¿3?, et des compositions pharmaceutiques contenant lesdits composés.

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