The Johns Hopkins University

Opko Ireland Global Holdings, Limited

Lindsey C Hess

Gary H Posner

P Martin Petkovich

Uttam Saha

Rachel D Slack

Alvin S Kalinda

Kimberly S Petersen

Douglas T Genna

Scott Borella

This present disclosure is directed to novel prodrugs of activated vitamin D3 compounds. The prodrugs can be designed to have one or more beneficial properties, such as selective inhibition of the enzyme CYP24, low calcemic activity, and anti-proliferative activity. Specifically, these prodrugs are 1-deoxy prohormones of active Vitamin D analogs, e.g. analogs of calcitriol. This disclosure is also directed to pharmaceutical and diagnostic compositions containing the prodrugs of the invention, and to their medical use, particularly as prodrugs in the treatment and/or prevention of diseases.

1-deoxy analogs of 1,25-dihydroxyvitamin D3 compounds

The disclosure provides compounds, compositions and methods using these compounds and compositions to stimulate the differentiation of cells and inhibit excessive cell proliferation of certain cells, including cancer cells and skin cells, which may be useful in the treatment of diseases characterized by abnormal cell proliferation and/or cell differentiation such as leukemia, myelofibrosis and psoriasis without the well known effect on calcium metabolism, which gives rise to hypercalcemia.

Low calcemic, highly antiproliferative, analogs of calcitriol

Growing community of inventors

Pflugerville, TX, United States of America

Lindsey C Hess