Antiproliferative Vitamin D3 Hybrids

The present invention is based on the unexpected finding that certain modifications to the A-ring portion of vitamin D.sub.3 analogues produce compounds of superior biological activity. In its broadest aspects, the invention provides vitamin D.sub.3 analogues which include a 1-hydroxyalkyl group or 1-fluoroalkyl group in a trans- configuration with a 3-hydroxyl group on the A ring. Thus, the invention includes analogues in which a fluorine or hydroxyl group is substituted at one or more positions on a straight or branch-chain alkyl group at the 1-position on the A-ring. Description (Set) Proposed Use (Set) The present invention relates to novel biologically active vitamin D.sub.3 analogues which include trans substituents at the 1- and 3-positions on the A-ring. More specifically, the present invention relates to hybrid compounds which are vitamin D.sub.3 analogues, each of which includes a 1-hydroxyalkyl or 1-fluoroalkyl group on the A ring and a modified D-ring side chain.

Patent (Set) 5,830,885

Patents:
US 5,830,885

Inventor(s): Posner, Gary H.

Type of Offer: Licensing



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