2-.alpha.-methyl and 2-.beta.-methyl analogs of...

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 2588406

This invention discloses 2.alpha.-methyl and 2~-methyl analogs of 19,26,27- trinor~ (20S)-l.alpha.-hydroxyvitamin D3and pharmaceutical uses therefor. These compounds exhibit 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. These compounds also have little, if any, calcemic activity and therefore may be used to treat autoimmune disorders or inflammatory diseases in humans as well as renal osteodystrophy. These compounds may also be used for the treatment or prevention of obesity.

La présente invention concerne des analogues 2.alpha.-méthyl et 2.beta.-méthyl de 19,26,27-trinor-(20S)-1.alpha.-hydroxyvitamine D3 et les utilisations pharmaceutiques de ceux-ci. Ces composés font preuve d'une forte activité d'interruption de la prolifération de cellules indifférenciées et d'induction de leur différenciation par rapport au monocyte, ce qui met en évidence leur utilisation comme agent anticancéreux et dans le traitement de maladies cutanées telles que le psoriasis et d'états cutanés tels que les rides, le relâchement cutané, la peau sèche et l'insuffisance de sécrétion de sébum. Ces composés, qui présentent très peu, voire aucune activité calcémique, peuvent ainsi servir au traitement de troubles auto-immuns ou de maladies inflammatoires chez les êtres humains ainsi que de l'ostéodystrophie rénale. Ces composés peuvent également être utilisés dans le traitement ou la prévention de l'obésité.

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