C - Chemistry – Metallurgy – 07 – C
Patent
C - Chemistry, Metallurgy
07
C
C07C 401/00 (2006.01) A61K 31/59 (2006.01) A61P 3/04 (2006.01) A61P 17/00 (2006.01) A61P 17/06 (2006.01) A61P 29/00 (2006.01) A61P 35/00 (2006.01) A61P 35/02 (2006.01) A61P 37/06 (2006.01)
Patent
CA 2662864
This invention discloses 2-methylene-(20S,25S)-19,27-dinor-(22E)-vitamin D analogs, and specifically 2-methylene-(20S,25S)-19,27-dinor-(22E)-1.alpha.,25- dihydroxyvitamin D3, 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 2-méthylène-(20S, 25S)-19,27-dinor-(22E)-vitamine D, et, spécifiquement, du 2-méthylène-(20S, 25S)-19,27-dinor-(22E)-1.alpha.,25-dihydroxyvitamine D3, et leur utilisation pharmaceutique. Ledit composé présente une efficacité prononcée pour inhiber la prolifération de cellules non différenciées et pour induire leur différentiation en monocyte, ce qui démontre son utilité comme agent anticancéreux, dans le traitement de maladies de la peau telles que le psoriasis ainsi que des troubles cutanés tels que rides, relâchement cutané, sécheresse cutanée et insuffisance de sécrétion de sébum. Ledit composé présente également une activité calcémique faible, voire nulle, et peut donc être utilisé pour traiter des troubles auto-immuns ou des maladies inflammatoires chez l'homme ainsi que l'ostéodystrophie rénale. Enfin, ledit composé peut également être utilisé pour traiter ou prévenir l'obésité.
Chiellini Grazia
Clagett-Dame Margaret
Deluca Hector F.
Grzywacz Pawel
Plum Lori A.
Riches Mckenzie & Herbert Llp
Wisconsin Alumni Research Foundation
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