2-methylene-18,19-dinor-1.alpha.-hydroxy-homopregnacalcifero...

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 2588417

This invention discloses 2-methylene-18,19-dinor-vitamin D analogs, and specifically 2-methylene-18,19-dinor-1.alpha.-hydroxy-homopregnacalciferol 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.

La présente invention concerne des analogues de 2-méthylène-18,19-dinor-vitamine D, et spécifiquement du 2-méthylène-18,19-dinor-1a-hydroxy-homoprégnacalciférol et ses utilisations pharmaceutiques. Ce composé a une activité prononcée pour stopper la prolifération de cellules non différenciées, et favoriser leur différenciation en monocyte, ce qui explique son utilité en tant qu'agent anticancéreux et dans le cadre du traitement de maladies de peau telles que le psoriasis ainsi que les troubles cutanés tels que les rides, le relâchement cutané, la sécheresse cutanée et l'insuffisance de sécrétion de sébum. Ce composé a une activité calcémique faible, voire nulle, et peut ainsi être utilisé pour traiter des troubles auto-immuns ou des maladies inflammatoires chez des êtres humains, ainsi que pour traiter l'ostéodystrophie rénale. Ce composé peut également être utilisé pour traiter ou prévenir l'obésité.

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