A-ring modified 19-nor-vitamin D analogs and their uses
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Abstract
Disclosed are 19-nor-vitamin D compounds, and specifically seco-A-2,19-dinor-1,25-dihydroxyvitamin D3 as well as pharmaceutical uses therefor. These compounds exhibit relatively high activity in vivo, specifically in intestinal tissues, but relatively low VDR binding activity, cell differentiation activity and gene transcription activity. There is thus potential for these compounds to have strong cell selectivity for use as therapeutic agents against some cancers, such as colon cancer or polyps, as well as hyperplastic intestinal disorders, such as Crohn'"'"'s disease, ulcerative colitis and celiac disease. These compounds also have relatively high intestinal calcium transport activity evidencing potential in the treatment of bone diseases.
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Citations
35 Claims
- 1. A compound having the formula:
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8. A compound having the formula:
- 9. A pharmaceutical composition containing an effective amount of seco-A-2,19-dinor-1,25-dihydroxyvitamin D3 together with a pharmaceutically acceptable excipient.
- 12. A method of treating a disease selected from the group consisting of colon cancer, Crohn'"'"'s disease, ulcerative colitis, and celiac disease comprising administering to a subject with said disease an effective amount of a 19-nor-vitamin D having the formula:
- 21. A method of treating metabolic bone disease where it is desired to maintain or increase bone mass comprising administering to a patient with said disease an effective amount of a compound having the formula:
Specification