17,20(e)-dehydro vitamin d analogs and their uses

Details 17,20(e)-dehydro vitamin d analogs and their uses 17,20(e)-dehydro vitamin d analogs and their uses

C - Chemistry, Metallurgy

07

C

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 2588396

This invention discloses 17,20(E)-dehydro vitamin D analogs, and specifically 17(E)-1.alpha.,25-dihydroxy-17(20)-dehydro-2-methylene-19-nor-vitamin 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 and inflammatory diseases in humans as well as renal osteodystrophy and obesity.

L'invention concerne des analogues de 17,20(E)-deshydro vitamine D, spécifiquement 17(E)-1a,25-dihydroxy-17(20)-deshydro-2-méthylène-19-nor-vitamine 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 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 et les maladies inflammatoires chez l'homme ainsi que l'ostéodystrophie rénale et l'obésité.

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