(20s)-23,23-difluoro-2-methylene-19-nor-bishomopregnacalcife...

Details (20s)-23,23-difluoro-2-methylene-19-nor-bishomopregnacalcife... (20s)-23,23-difluoro-2-methylene-19-nor-bishomopregnacalcife...

C - Chemistry, Metallurgy

07

C

C07C 401/00 (2006.01) A61K 31/593 (2006.01) A61P 3/14 (2006.01) A61P 17/06 (2006.01) A61P 19/02 (2006.01) A61P 35/02 (2006.01) A61P 37/06 (2006.01)

Patent

CA 2710954

This invention discloses (20S)-23,23-difluoro-2-methylene-19-nor- bishomopregnacalciferol-vitamin D analogs, and specifically (20S)-23,23-difluoro- 1 .alpha.- hydroxy-2-methylene-19-nor- bishomopregnacalciferol, 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 vitamine D (20S)-23,23-difIuoro-2-méthylène-19-nor-bishomopregnacalciférol, et leurs utilisations pharmaceutiques. Ce composé présente une activité prononcée d'arrêt de la prolifération des cellules non différenciées et d'induction de leur différenciation par rapport au monocyte, mettant ainsi en évidence son utilisation comme agent anticancéreux et dans le traitement des maladies cutanées telles que le psoriasis, ainsi que des conditions cutanées tels que les rides, la peau flasque, la peau sèche et une sécrétion de sébum insuffisante. Ce composé possède également une faible activité calcémique et peut ainsi être utilisé pour traiter les troubles auto-immuns ou les maladies inflammatoires chez les humains, ainsi que l'ostéodystrophie rénale. Ce composé peut également être utilisé dans le traitement ou la prévention de l'obésité.

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