(20S,22E)-2-Methylene-19-Nor-22-Ene-1Alpha,25-Dihydroxyvitamin D3
AssigneeWisconsin Alumni Research Foundation
InventorsHector F. DeLuca, Pawel Grzywacz, Lori A. Plum, Margaret Clagett-Dame
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Abstract
This invention discloses (20S,22E)-2-methylene-19-nor-22-ene-1α,25-dihydroxyvitamin D3 analogs, and specifically(20S,22E)-2-methylene-19-nor-22-ene-1α,25-dihydroxyvitamin D3, and pharmaceutical uses therefor. This compound exhibits significant vitamin D receptor binding activity and transcription activity as well as 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 leukemia, colon cancer, breast cancer, skin cancer or prostate cancer.
Claims23
A compound having the formula:
- where X1, X2 and X3, which may be the same or different, are each selected from hydrogen or a hydroxy-protecting group.
(20S,22E)-2-Methylene-19-nor-22-ene-1α,25-dihydroxyvitamin D3 having the formula:
A pharmaceutical composition containing an effective amount of (20S,22E)-2-Methylene-19-nor-22-ene-1α,25-dihydroxyvitamin D3 together with a pharmaceutically acceptable excipient.
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 compound having the formula:
- where X1, X2 and X3 which may be the same or different, are each selected from hydrogen or a hydroxy-protecting group.
A compound having the formula:
- where X3 is selected from hydrogen or a hydroxy-protecting group.
Dependencies are inferred from the claim text.