Calcitriol derivatives and their uses

C - Chemistry – Metallurgy – 07 – C

Patent

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

Patent

CA 2229316

A method of treating metabolic bone diseases such as osteoporosis, as well as other disease states treatable with vitamin D compounds, comprises administering an effective amount of one or more modified vitamin D compounds. The modified compound contains a typical vitamin D nucleus but with in vivo hydrolyzable groups at one or more of the 1, 3 and 25 carbon positions. The time of conversion of the modified compound to its active form, such as calcitriol, can be regulated to thus provide controlled release of the compound in vivo over time, by changing or modifying the hydrolyzable groups.

L'invention se rapporte à un procédé de traitement des maladies osseuses métaboliques telles que l'ostéoporose, ainsi que d'autres états pathologiques pouvant être traités avec des composés de la vitamine D, ce procédé consistant à administrer une quantité efficace d'un ou plusieurs composés modifiés de la vitamine D. Le composé modifié contient un noyau type de vitamine D, mais présentant des groupes hydrolysables in vivo à une ou plusieurs des positions de carbone 1, 3 et 25. Il est possible de réguler le temps de conversion à sa forme active du composé modifié, tel que le calcitriol, en vue d'obtenir une libération régulée du composé in vivo sur plusieurs heures, en changeant ou modifiant les groupes hydrolysables.

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