17,20(Z)-dehydro vitamin D analogs and their uses
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Abstract
This invention discloses 17,20(Z)-dehydro vitamin D analogs, and specifically 17(Z)-1α,25-dihydroxy-17(20)-dehydro-2-methylene-19-nor-vitamin D3 and pharmaceutical uses therefor. This compound exhibits pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent and for the treatment of skin diseases such as psoriasis as well as skin conditions such as wrinkles, slack skin, dry skin and insufficient sebum secretion. This compound also may be used to treat autoimmune disorders and inflammatory diseases in humans as well as renal osteodystrophy and obesity. This compound also has significant calcemic activity making it a therapeutic agent for the treatment or prophylaxis of osteoporosis, osteomalacia, renal osteodystrophy and hypoparathyroidism.
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Citations
82 Claims
- 1. A compound having the formula:
- 8. A compound having the formula:
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15. 17(Z)-1α
- ,25-dihydroxy-17(20)-dehydro-2-methylene-19-nor-vitamin D3 having the formula;
- View Dependent Claims (17, 18)
- ,25-dihydroxy-17(20)-dehydro-2-methylene-19-nor-vitamin D3 having the formula;
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16. A pharmaceutical composition containing an effective amount of 17(Z)-1α
- ,25-dihydroxy-17(20)-dehydro-2-methylene-19-nor-vitamin D3 together with a pharmaceutically acceptable excipient.
- 19. A method of treating psoriasis comprising administering to a subject with psoriasis an effective amount of a 17(20)-dehydro vitamin D compound having the formula:
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25. A method of treating psoriasis comprising administering to a subject with psoriasis an effective amount of 17(Z)-1α
- ,25-dihydroxy-17(20)-dehydro-2-methylene-19-nor-vitamin D3 having the formula;
- View Dependent Claims (26, 27, 28, 29, 30)
- ,25-dihydroxy-17(20)-dehydro-2-methylene-19-nor-vitamin D3 having the formula;
- 31. A method of treating a disease selected from the group consisting of leukemia, colon cancer, breast cancer, skin cancer or prostate cancer comprising administering to a subject with said disease an effective amount of a 17(20)-dehydro vitamin D compound having the formula:
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36. A method of treating a disease selected from the group consisting of leukemia, colon cancer, breast cancer, skin cancer or prostate cancer comprising administering to a subject with said disease an effective amount of 17(E)-1α
- ,25-dihydroxy-17(20)-dehydro-2-methylene-19-nor-vitamin D3 having the formula;
- View Dependent Claims (37, 38, 39, 40)
- ,25-dihydroxy-17(20)-dehydro-2-methylene-19-nor-vitamin D3 having the formula;
- 41. A method of treating an autoimmune disease selected from the group consisting of multiple sclerosis, lupus, diabetes mellitus, hot versus graft rejection, and rejection of organ transplants, comprising administering to a subject with said disease an effective amount of a 17(20)-dehydro vitamin D compound having the formula:
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46. A method of treating an autoimmune disease selected from the group consisting of multiple sclerosis, lupus, diabetes mellitus, host versus graft rejection, and rejection of organ transplants, comprising administering to a subject with said disease an effective amount of 17(Z)-1α
- ,25-dihydroxy-17(20)-dehydro-2-methylene-19-nor-vitamin D3 having the formula;
- View Dependent Claims (47, 48, 49, 50)
- ,25-dihydroxy-17(20)-dehydro-2-methylene-19-nor-vitamin D3 having the formula;
- 51. A method of treating an inflammatory disease selected from the group consisting of rheumatoid arthritis, asthma, and inflammatory bowel diseases, comprising administering to a subject with said disease an effective amount of a 17(20)-dehydro vitamin D compound having the formula:
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56. A method of treating an inflammatory disease selected from the group consisting of rheumatoid arthritis, asthma, and inflammatory bowel diseases, comprising administering to a subject with said disease an effective amount of 17(Z)-1α
- ,25-dihydroxy-17(20)-dehydro-2-methylene-19-nor-vitamin D3 having the formula;
- View Dependent Claims (57, 58, 59, 60)
- ,25-dihydroxy-17(20)-dehydro-2-methylene-19-nor-vitamin D3 having the formula;
- 61. A method of treating a skin condition selected from the group consisting of wrinkles, lack of adequate skin firmness, lack of adequate dermal hydration and insufficient sebum secretion which comprises administering to a subject with said skin condition an effective amount of a 17(20)-dehydro vitamin D compound having the formula:
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67. A method of treating a skin condition selected from the group consisting of wrinkles, lack of adequate skin firmness, lack of adequate dermal hydration and insufficient sebum secretion which comprises administered to a subject with said skin condition an effective amount of 17(Z)-1α
- ,25-dihydroxy-17(20)-dehydro-2-methylene-19-nor-vitamin D3 having the formula;
- View Dependent Claims (68, 69, 70, 71, 72)
- ,25-dihydroxy-17(20)-dehydro-2-methylene-19-nor-vitamin D3 having the formula;
- 73. A method of treating renal osteodystrophy comprising administering to a subject with renal osteodystrophy an effective amount of a 17(20)-dehydro vitamin D compound having the formula:
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78. A method of treating renal osteodystrophy comprising administering to a subject with renal osteodystrophy an effective amount of 17(E)-1α
- ,25-dihydroxy-17(20)-dehydro-2-methylene-19-nor-vitamin D3 having the formula;
- View Dependent Claims (79, 80, 81, 82)
- ,25-dihydroxy-17(20)-dehydro-2-methylene-19-nor-vitamin D3 having the formula;
Specification