3-desoxy-2-methylene-19-nor-vitamin D analogs and their uses
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Abstract
This invention discloses 3-desoxy-2-methylene-19-nor-vitamin D analogs, and specifically (20S)-3-desoxy-2-methylene-1α,25-dihydroxy-19-nor-vitamin D3 and (20R)-3-desoxy-2-methylene-1α,25-dihydroxy-19-nor-vitamin D3 as well as pharmaceutical uses therefor. These compounds exhibit relatively high binding activity and pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to monocytes thus evidencing use as anti-cancer agents especially for the treatment or prevention of osteosarcoma, leukemia, colon cancer, breast cancer, skin cancer or prostate cancer. These compounds also exhibit relatively high calcemic activity evidencing use in the treatment of bone diseases.
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Citations
43 Claims
- 1. A compound of the formula:
- 8. A compound of the formula:
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15. A compound of the formula:
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16. A pharmaceutical composition containing an effective amount of (20S)-3-desoxy-2-methylene-1α
- ,25-dihydroxy-19-nor-vitamin D3 together with a pharmaceutically acceptable excipient.
- View Dependent Claims (17, 18)
- 19. A method of treating a disease selected from the group consisting of osteosarcoma, leukemia, colon cancer, breast cancer, skin cancer or prostate cancer comprising administering to a subject with said disease an effective amount of a 3-desoxy-2-methylene-19-nor-vitamin D analog having of the formula:
- 24. A method of treating metabolic bone disease comprising administering to a patient with said disease an effective amount of a compound of the formula:
- 30. A compound of the formula:
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37. A compound of the formula:
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38. A Pharmaceutical composition containing an effective amount of (20R)-3-desoxy-2-methylene-1α
- ,25-dihydroxy-19-nor-vitamin D3 together with a pharmaceutically acceptable excipient.
- View Dependent Claims (39, 40)
- 41. A compound of the formula:
Specification