18-substituted-19-nor-vitamin D compounds
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Abstract
This invention provides a novel class of vitamin D compounds, namely, 13-ethyl and 13-vinyl-18,19-dinor-vitamin D derivatives, as well as a general method for their chemical synthesis. The compounds have the formula:
where Y1 and Y2, which may be the same or different, are each selected from the group consisting of hydrogen and a hydroxy-protecting group, R6 is selected from the group consisting of an ethyl or vinyl radical, and where the group R represents any of the typical side chains known for vitamin D type compounds. These 18-substituted compounds are characterized by minimal intestinal calcium transport activity and minimal bone calcium mobilization activity resulting in novel therapeutic agents for the treatment of secondary hyperparathyroidism. These compounds also exhibit pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as anti-cancer agents and for the treatment of diseases such as psoriasis.
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41 Claims
- 1. A compound having the formula:
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2. The compound of claim I where R is a side chain of the formula
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8. The compound of claim I where R is a side chain of the formula
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12. 13-ethyl-18,19-dinor-1α
- ,25-dihydroxyvitamin D3.
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13. 13-vinyl-18,19-dinor-1α
- ,25-dihydroxyvitamin D3.
- 17. A method of treating psoriasis comprising administering to a patient with said disease an effective amount of a compound having the formula:
- 21. A method of treating secondary hyperparathyroidism comprising supressing parathyroid activity by administering to a patient with said disorder an effective amount of a compound having the formula:
- 25. A method of treating a patient having renal osteodystrophy while avoiding hyperphosphatemia comprising administering to a patient with said disease an effective amount of a vitamin D compound that has minimal effect on blood serum phosphorus of said patient, said vitamin D compound having the formula:
- 29. A method of treating a cancer selected from the group consisting of leukemia, breast cancer, colon cancer and prostate cancer comprising administering to a patient with said cancer an effective amount of a compound having the formula,
Specification