2-methylene-19,26,27-trinor-(20s)-1-alpha-hydroxyvitamin d3...

C - Chemistry – Metallurgy – 07 – C

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C07C 401/00 (2006.01) A61K 31/59 (2006.01) A61P 11/06 (2006.01) A61P 17/06 (2006.01) A61P 29/00 (2006.01) A61P 35/00 (2006.01) A61P 37/00 (2006.01)

Patent

CA 2588415

This invention discloses 2-methylene-19,26,27-trinor-(20S)-vitamin D analogs, and specifically 2-methylene-19,26,27-trinor-(20S)-l.alpha.-hydroxyvitamirt D3 and pharmaceutical uses therefor. This compound exhibits 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. This compound also has little, if any, calcemic activity and therefore may be used to treat autoimmune disorders or inflammatory diseases in humans as well as renal osteodystrophy. This compound may also be used for the treatment or prevention of obesity.

L'invention concerne des analogues de 2-méthylène-19,26,27-trinor-(20S)-vitamine D, spécifiquement 2-méthylène-19,26,27-trinor-(20S)-1a-hydroxyvitamine D3 et leurs utilisations pharmaceutiques. Ce type de composé a une activité prononcée de blocage de la prolifération des cellules indifférenciées et de démarrage de leur différentiation au niveau du monocyte, ce qui met en évidence une utilisation comme anticancéreux et comme médicament pour le traitement des maladies de la peau comme le psoriasis et aussi de certains états de la peau, à savoir par exemple rides, peau flasque, peau sèche et sécrétion de sébum insuffisante. Un tel composé présente peu d'activité calcémique ou il n'en présente pas et peut donc être utilisé pour traiter les troubles auto-immunes ou les maladies inflammatoires chez l'homme ainsi que l'ostéodystrophie rénale, et aussi pour traiter ou prévenir l'obésité

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