Organic compounds -- part of the class 532-570 series – Organic compounds – Oxygen containing
Patent
1998-09-10
1999-08-10
Lambkin, Deborah C.
Organic compounds -- part of the class 532-570 series
Organic compounds
Oxygen containing
568470, 568 14, 560126, 560128, 556436, 556437, 556482, C07C 3508, C07C 4500, C07C 6974
Patent
active
059361336
ABSTRACT:
This invention provides a novel class of vitamin D related compounds, namely, the 2-alkylidene-19-nor-vitamin D derivatives, as well as a general method for their chemical synthesis. The compounds have the formula: ##STR1## where Y.sub.1 and Y.sub.2, which may be the same or different, are each selected from the group consisting of hydrogen and a hydroxy-protecting group, R.sub.6 and R.sub.8, which may be the same or different, are each selected from hydrogen, alkyl, hydroxyalkyl and fluoroalkyl, or when taken together represent the group --(CH.sub.2).sub.x -- where x is an integer from 2 to 5, and where the group R represents any of the typical side chains known for vitamin D type compounds. These 2-substituted compounds are characterized by low intestinal calcium transport activity and high bone calcium mobilization activity resulting in novel therapeutic agents for the treatment of diseases where bone formation is desired, particularly low bone turnover osteoporosis. These compounds also exhibit pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as anti-cancer agents and for the treatment of diseases such as psoriasis.
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DeLuca Hector F.
Sicinski Rafal R.
Lambkin Deborah C.
Wisconsin Alumni Research Foundation
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