18-nor-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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A61K 3159

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056611404

ABSTRACT:
18-nor-vitamin D.sub.3 analogs in which the angular methyl group attached to carbon 13 of the CD-ring has been removed and replaced by a hydrogen atom. The 18-nor vitamin D compounds are characterized by relatively high cell differentiation activity, while exhibiting much 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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Maynard et al, "18-Substituted Derivatives of Vitamin D: 18-Acetoxy-1,25-Dihydroxyvitamin D.sub.3 and Related Analogues", J. Org. Chem., vol. 57, 1992, pp. 3214-3217.
Nilsson et al, "Synthesis and Biological Evaluation of 18-Substituted Analogs of 1,25-Dihydroxyvitamin D.sub.3 ", Bioorg. Med. Chem. Letters, vol. 3, No. 9, 1993, pp. 1855-1858.
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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