18,19-dinor-vitamin D compounds

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – 9,10-seco- cyclopentanohydrophenanthrene ring system doai

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552563, C07C40100, A61K 3159

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active

057564892

ABSTRACT:
18,19-dinor-vitamin D.sub.3 analogs in which the angular methyl group attached to carbon 13 of the CD-ring and the exocyclic methylene group attached to carbon 10 of the A-ring have been removed and replaced by a hydrogen atom. The 18,19-dinor vitamin D compounds are characterized by relatively high cell differentiation activity, and marked intestinal calcium transport activity while exhibiting lower activity than 1.alpha.,25-dihydroxyvitamin D.sub.3 in their ability to mobilize calcium from bone. These compounds would be useful for the treatment of diseases where bone formation is desired, such as osteoporosis, because of their preferential calcemic activity, and for the treatment of psoriasis due to their cell differentiation activity.

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Biorganic & Medicinal Chemistry Letters, vol. 3, No. 9, pp. 1855-1858, 1993, "Synthesis and Biological Evaluation of 18-Substituted Analogs of 1 .alpha.,25-Dihydroxyvitamin D.sub.3 ", Nilsson et al.
J. Org. Chem., vol. 57, No. 11, pp. 3214-3217, 1992, "18-Substituted Derivatives of Vitamin D: 18-Acetoxy-1.alpha.,25-Dihydroxyvitamin D.sub.3 and Related Analogues", Maynard et al.

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