19-Nor-vitamin D.sub.3 compounds with substitutent at 2-position
AssigneeWisconsin Alumni Research Foundation
InventorsHector F. Deluca, Kato L. Perlman, Rafal R. Sicinski
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AssigneeWisconsin Alumni Research Foundation
InventorsHector F. Deluca, Kato L. Perlman, Rafal R. Sicinski
Estimating the term…
The 2.alpha. and 2.beta.-hydroxy as well as the 2.alpha.(3'-hydroxypropoxy)- and 2.beta.(3'-hydroxypropoxy)- and 2.alpha.(benzyloxy)- analogs of 19-nor-1.alpha.,25-dihydroxyvitamin D.sub.3 are disclosed. The two 2-hydroxy analogs showed in vivo calcium transport with little or no bone calcium mobilization; the 2.beta.- more than the 2.alpha.- analog. Both analogs induced differentiation of malignant cells. The two analogs thus show promise in the treatment of osteoporosis. The 2.alpha.-hydroxypropoxy analog showed a selective activity profile, combining high potency in inducing differentiation of malignant cells with very low or no bone calcification activity, a possible use in the treatment of malignancies.
A vitamin D compound having the structure:
1.alpha.,2.alpha.,25-trihydroxy-19-nor-vitamin D.sub.3.
1.alpha.,2.beta.,25-trihydroxy-19-nor-vitamin D.sub.3.
1.alpha.,25-dihydroxy-2.alpha.-(3'-hydroxypropoxy)-19-nor-vitamin D.sub.3.
1.alpha.,25-dihydroxy-2.beta.-(3'-hydroxypropoxy)-19-nor-vitamin D.sub.3.
1.alpha.,25-dihydroxy-2.alpha.-(benzyloxy)-19-nor-vitamin D.sub.3.
A method of treating osteoporosis comprising administering to a patient an effective amount of a vitamin D.sub.3 compound selected from the group consisting of 1.alpha.,2.alpha.,25-trihydroxy-19-nor-vitamin D.sub.3, 1.alpha.,2.beta.,25-trihydroxy-19-nor-vitamin D.sub.3, 1.alpha.,25-dihydroxy-2.alpha.-(3'-hydroxypropoxy)-19-nor-vitamin D.sub.3, 1.alpha.,25-dihydroxy-2.beta.-(3'-hydroxypropoxy)-19-nor-vitamin D.sub.3, 1.alpha.,25-dihydroxy-2.alpha.-(benzyloxy)-19-nor-vitamin D.sub.3 and mixtures thereof.
Dependencies are inferred from the claim text.