Vitamin d3 derivatives and remedies using the same

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 307/58 (2006.01) A61K 31/593 (2006.01) A61P 3/02 (2006.01) A61P 3/10 (2006.01) A61P 3/14 (2006.01) A61P 5/18 (2006.01) A61P 9/12 (2006.01) A61P 11/00 (2006.01) A61P 17/02 (2006.01) A61P 17/06 (2006.01) A61P 17/10 (2006.01) A61P 17/14 (2006.01) A61P 19/08 (2006.01) A61P 19/10 (2006.01) A61P 29/00 (2006.01) A61P 35/00 (2006.01) A61P 43/00 (2006.01)

Patent

CA 2476679

Vitamin D~3 derivatives represented by the following general formula (1) or pharmaceutically acceptable solvates thereof: (1) wherein R represents hydrogen or methyl; and A represents a single bond, -CH~2-, -CH=CH-, -CH~2- CH=CH-, -CH=CH-CH=CH-, -C.ident.C- or -CH~2-C.ident.C-, provided that the case wherein R is hydrogen, A is -CH~2-, the configuration at the 1-position is (S) and the configuration at the 3-position is (R) is excluded. These compounds are usable as the active ingredients of remedies for osteoporosis, malignant tumor, psoriasis, parathyroid hyperfunction, inflammatory respiratory disease, rheumatoid arthritis, diabetes mellitus, hypertension, hair loss, acne, dermatitis, hypercalcemia or Paget~s disease of bone.

Dérivés de vitamine D3 représentés par la formule (1) ou leurs solvates acceptables sur le plan pharmaceutique, dans laquelle R représente hydrogène ou méthyle; et A représente une liaison simple, -CH2-, -CH=CH-, -CH2CH=CH-, -CH=CH-CH=CH-, -C ou -CH2C-, dans la mesure où R représente hydrogène, A représente -CH2-, ce qui exclue que la configuration au niveau de la position 1 soit (S) et au niveau de la position 3 (R). Ces composés sont utilisables sous forme d'ingrédient actif de médicaments contre l'ostéoporose, les tumeurs malignes, le psoriasis, l'hyperfonctionnement parathyroïdien, l'inflammation respiratoire, la polyarthrite rhumatoïde, le diabète sucré, l'hypertension, la perte des cheveux, l'acné, la dermatite, l'hypercalcémie ou la maladie osseuse de Paget.

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