2-methylene-19-nor-20(s)-25-methyl-1.alpha.-hydroxycalcifero...

A - Human Necessities – 61 – K

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Details

A61K 31/59 (2006.01) A61P 3/14 (2006.01) A61P 17/06 (2006.01) A61P 19/10 (2006.01) A61P 35/00 (2006.01) A61P 35/02 (2006.01) C07C 401/00 (2006.01)

Patent

CA 2531294

This invention provided a novel vitamin D analog, namely, 2-methylene-19-nor- 20(S)-25-methyl-1.alpha.-hydroxycalciferol. The compound has the formula (I). This 2-substituted compound is characterized by relatively high intestinal calcium transport activity and relatively low bone calcium mobilization activity resulting in novel therapeutic agents for the treatment of diseases where bone formation is desired, particularly osteoporosis. These compounds also exhibit pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as anti-cancer agents and for the treatment of diseases such as psoriasis.

L'invention concerne un nouvel analogue de la vitamine D, à savoir, le 2-méthylène-19-nor-20(S)-25-méthyl-1.alpha.-hydroxycalciférol. Ce composé est représenté par la formule (I). Ce composé substitué en deux est caractérisé par une activité de transport de calcium intestinal relativement élevée et une activité de mobilisation de calcium osseux relativement faible, ce qui permet d'obtenir de nouveaux agents thérapeutiques pour le traitement de maladies dans lesquelles une formation osseuse est souhaitée, en particulier l'ostéoporose. Ces composés présentent également une activité prononcée pour arrêter la prolifération de cellules non différenciées et pour induire leur différenciation pour le monocyte, ce qui en fait de très bons agents anticancéreux, et également utiles pour le traitement de maladies comme le psoriasis.

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