2-methylene-vitamin D analogs and their uses
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Abstract
This invention discloses 2-methylene-vitamin D analogs, and specifically (20S)-1α,25 -dihydroxy-2-methylene-vitamin D3 as well as (5E)-(20S)-1α,25-dihydroxy-2 -methylene-vitamin D3 and (20R)-1α,25-dihydroxy-2-methylene-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 the monocyte thus evidencing use as an anti-cancer agent especially for the treatment or prevention of osteosarcoma, leukemia, colon cancer, breast cancer, skin cancer or prostate cancer. These compounds also have relatively high calcemic activities evidencing use in the treatment of bone diseases.
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Citations
47 Claims
- 1. A compound having the formula:
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8. A compound having the formula:
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9. A pharmaceutical composition containing an effective amount of (20S)-1α
- ,25-dihydroxy-2-methylene-vitamin D3 together with a pharmaceutically acceptable excipient.
- View Dependent Claims (10, 11)
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12. A compound having the formula:
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13. A pharmaceutical composition containing an effective amount of (5E)-(20S)-1α
- ,25-dihydroxy-2-methylene-vitamin D3 together with a pharmaceutically acceptable excipient.
- View Dependent Claims (14, 15)
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16. A compound having the formula:
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17. A pharmaceutical composition containing an effective amount of (20R)-1α
- ,25-dihydroxy-2-methylene-vitamin D3 together with a pharmaceutically acceptable excipient.
- View Dependent Claims (18, 19)
- 20. 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 2-methylene-vitamin D analog having the formula:
- 31. 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