Vitamin d3 derivatives and remedies for inflammatory...

C - Chemistry – Metallurgy – 07 – C

Patent

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C07C 401/00 (2006.01) A61K 31/59 (2006.01)

Patent

CA 2263940

Vitamin D3 derivatives represented by general formula [1] and a process for producing the same: wherein R1 and R2 represent each hydrogen, trialkylsilyl, etc.; R3 and R4 represent each hydrogen, hydroxy, etc.; R5 to R8 represent each hydrogen, hydroxy, alkyl or acyloxy; R9 represents hydrogen, hydroxy, alkyl or alkylthio; R10 represents hydrogen, alkyl or alkyloxy; A and B represent each hydrogen, hydroxy, etc.; X and Y represent each carbonyl oxygen, or one of X and Y represents hydrogen while another represents hydroxy, etc.; and n and m are each 0 to 2. These compounds are usable as the active ingredients of remedies for inflammatory respiratory diseases, malignant tumors, articular rheumatism, osteoporosis, diabetes mellitus, hypertension, baldness, acne, psoriasis, and dermatitis.

L'invention concerne des dérivés de vitamine D¿3? de formule générale [1] et un procédé pour leur élaboration. Dans ladite formule, R¿1? et R¿2? sont chacun hydrogène, trialkylsilyle, etc.; R¿3? et R¿4? sont chacun hydrogène, hydroxy, etc.; R¿5? à R¿8? sont chacun hydrogène, hydroxy, alkyle ou acyloxy; R¿9? est hydrogène, hydroxy, alkyle ou alkylthio; R¿10? est hydrogène, alkyle ou alkyloxy; A et B sont chacun hydrogène, hydroxy, etc.; X et Y sont chacun oxygène d'un groupe carbonyle, ou bien, soit X soit Y est hydrogène tandis que l'autre est hydroxy, etc.; et n et m sont compris chacun entre 0 et 2. Les composés considérés sont utilisés en tant que principe actif dans des médicaments pour le traitement des affections suivantes : maladies respiratoires inflammatoires, tumeurs malignes, rhumatisme articulaire, ostéoporose, diabète sucré, hypertension, calvitie, acné, psoriasis, et dermatite.

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