New Analogs of the Hormone 1(alpha)25-Dihydroxyvitamin D with Side Chain Carbonyl Groups

Medicinal chemists are designing analogs to be at least as potent as, but less calcemic than, the natural hormone la, 25-dihydroxyvitamin D3 (calcitriol) for chemotherapy of diverse human illnesses. Scientists at JHU have previously shown that some new vitamin D analogs, even though lacking the classical side-chain terminal OH group, are transcriptionally active and low-calcemic. They have now created a new series of calcitriol analogs that do not possess the 16, 17-unsaturation characteristic that is thought to be potentiating, and is present in some side-chain ketones having high antiproliferative potency. Some of the novel 16, 17-saturated analogs are considerably more antiproliferative in vitro than calcitriol even at low nanomolar concentrations and also are desirably low calcemic in vivo. Description (Set) Proposed Use (Set) The combination of desirably high antiproliferative potency and desirably low calcemic activity make these new chemical entities promising candidates for further preclinical evaluation as potential drug candidates to improve human health. Patent (Set) WO2006/074227 A2

Inventor(s): Posner, Gary H.

Type of Offer: Licensing



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