C - Chemistry – Metallurgy – 07 – C
Patent
C - Chemistry, Metallurgy
07
C
C07C 401/00 (2006.01) A61K 31/593 (2006.01) A61P 17/06 (2006.01) A61P 19/10 (2006.01) A61P 35/00 (2006.01) A61P 37/06 (2006.01) C07C 49/443 (2006.01)
Patent
CA 2483409
This invention discloses (20S)-1.alpha.-hydroxy-2.alpha.-methyl-19-nor-vitamin D3 and (20S)-1.alpha.-hydroxy-2.beta.-methyl-19-nor-vitamin D3 and 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 very significant calcemic activity and therefore may be used to treat immune disorders in humans as well as metabolic bone diseases such as osteoporosis.
L'invention concerne les composés (20S)-1.alpha.-hydroxy-2.alpha.-méthyl-19-nor-vitamine D¿3? et (20S)-1?-hydroxy-2?-méthyl-19-nor-vitamine D¿3? ainsi que les utilisations pharmaceutiques de ceux-ci. Ces composés présentent une activité prononcée d'arrêt de la prolifération des cellules indifférenciées, et d'amorçage de leur différenciation en monocytes, justifiant ainsi leur utilisation en tant qu'agents anticancéreux et pour le traitement des maladies cutanées telles que le psoriasis ainsi que de problèmes cutanés tels que rides, relâchement de la peau, sécheresse cutanée, et sécrétion insuffisante de sébum. Ces composés ont en outre une importante activité calcémique et peuvent par conséquent servir à traiter les troubles immunitaires chez les patients humains ainsi que les maladies osseuses métaboliques telles que l'ostéoporose.
Deluca Hector F.
Grzywacz Pawel K.
Sicinski Rafal R.
Borden Ladner Gervais Llp
Wisconsin Alumni Research Foundation
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