C - Chemistry – Metallurgy – 07 – C
Patent
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 2588399
This invention discloses 2.alpha.-methyl-19-nor-(20S)-vitamin D analogs, and specifically 2.alpha.-methyl-l9-nor-(20S)-1.alpha.-hydroxy- 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 2a-méthyl-19-nor-(20S)-vitamine D et, spécifiquement, le 2a-méthyl-l9-nor-(20S)-1a-hydroxy-bishomoprégnacalciférol et 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 psoriasis, et certains états de la peau tels que rides, peau flasque, peau sèche et sécrétion insuffisante de sébum. Ce composé qui ne présente pas, ou très peu, d'activité calcémique, convient particulièrement au traitement de troubles autoimmunitaires ou de maladies inflammatoires chez l'être humain, ainsi que l'ostéodystrophie rénale. Ce composé peut également être utilisé pour le traitement ou la prévention de l'obésité.
Clagett-Dame Margaret
Deluca Hector F.
Plum Lori A.
Sicinski Rafal R.
Borden Ladner Gervais Llp
Wisconsin Alumni Research Foundation
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