1.alpha.-hydroxy-2-(3'-hydroxypropylidene)-19-n0r-vitamin d...

C - Chemistry – Metallurgy – 07 – C

Patent

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Details

C07C 401/00 (2006.01) A61K 31/59 (2006.01) A61P 3/04 (2006.01) A61P 17/00 (2006.01) A61P 17/06 (2006.01) A61P 29/00 (2006.01) A61P 35/00 (2006.01) A61P 37/06 (2006.01)

Patent

CA 2648521

This invention discloses l.alpha.-hydroxy-2-(3'-hydroxypropylidene)-19-nor- vitamin D compounds with a 1,1-dimethylpropyl side chain, and pharmaceutical uses therefor. These compounds exhibit pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent and for the treatment of skin diseases such as psoriasis as well as skin conditions such as wrinkles, slack skin, dry skin and insufficient sebum secretion. These compounds also have little, if any, calcemic activity and therefore may be used to treat autoimmune disorders or inflammatory diseases in humans as well as renal osteodystrophy. These compounds may also be used for the treatment or prevention of obesity.

La présente invention concerne des composés de la 1-a-hydroxy-2-(3'-hydroxypropylidène)-19-nor-vitamine D ayant une chaîne latérale 1,1-diméthylpropyle et des utilisations pharmaceutiques de ceux-ci. Ces composés présentent une forte activité d'arrêt de la prolifération de cellules non différenciées et d'induction de leur différenciation en monocyte ce qui démontre une utilisation possible de ceux-ci en tant qu'agents anticancéreux et pour le traitement de maladies cutanées telles que le psoriasis ainsi que d'affections cutanées telles que des rides, la peau détendue, la peau sèche et une sécrétion insuffisante de sébum. Ces composés ont également peu ou pas d'effet sur la calcémie et peuvent par conséquent être utilisés pour traiter des troubles auto-immuns ou des maladies inflammatoires chez des humains ainsi que l'ostéodystrophie rénale. Ces composés peuvent également être utilisés pour le traitement ou la prévention de l'obésité.

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