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

Details 17,20(z)-dehydro vitamin d analogs and their uses 17,20(z)-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 2588401

This invention discloses 17,20(Z)-dehydro vitamin D analogs, and specifically 17(Z)-1a,25-dihydroxy-17(20)-dehydro-2-methylene-19-nor-vitamin D3and 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 may be used to treat autoimmune disorders and inflammatory diseases in humans as well as renal osteodystrophy and obesity. This compound also has significant calcemic activity making it a therapeutic agent for the treatment or prophylaxis of osteoporosis, osteomalacia, renal osteodystrophy and hypoparathyroidism.

L'invention concerne des analogues de 17,20(Z)-déhydro vitamine D et, spécifiquement, la 17(Z)-1a,25-dihydroxy-17(20)-déhydro-2-méthylène-19-nor-vitamine D3et leurs utilisations pharmaceutiques. Ce composé fait preuve d'une activité notoire pour le blocage de la prolifération des cellules indifférentiées et pour l'induction de leur différentiation en monocyte, ce qui le destine à une utilisation comme agent anti-cancéreux et au traitement d'affections dermatologiques telles que le sporiasis, et certains états de la peau tels que rides, peau flasque, peau sèche et sécrétion insuffisante de sébum. Ce composé peut être également utilisé pour traiter des troubles autoimmunitaires et des maladies inflammatoires chez l'être humain, ainsi que l'ostéodystrophie rénale et l'obésité. Ce composé présente également une activité calcémique notoire, ce qui fait de lui un agent thérapeutique pour le traitement ou la prophylaxie de l'ostéoporose, l'ostéomalacie, l'ostéodystrophie rénale et l'hypoparathyroïdisme.

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