Novel Heterocycles (Case 1975)



Women and Infant’s Hospital

Providence, RI


Brief Description:


Vitamin D and various analogs have demonstrated mechanism-based anti-cancer activity and other therapeutic applications for diseases such as psoriasis and anti-inflammatory conditions in animal models and humans. However, pharmacologic doses of vitamin D lead to lethal hypercalcemia, to avoid these unwanted side effects, a large number of synthetic analogs of vitamin D have been developed and used to inhibit tumor progression and metastastic spread in animal models of various cancer types. However, the therapeutic efficacy of systemically applied vitamin D analogs in treating cancer has not yet fulfilled its promise because of hypercalcemia, at the supraphysiological doses need to reach clinical improvement. Moreover, the analogs described to date are difficult to synthesize and routes of synthesis are unlikely to be commercialized given their complexity. Therefore, the discovery of a non-calcemic, easily synthesized, and potent analog is the ultimate goal of vitamin D research for the treatment of human diseases.


The compounds discovered in the current invention represent a potent class of novel antiproliferative molecules with a novel mechanism of action. Potent biological activity, short-path high yield syntheses, and significantly improved stability have been achieved.




US Patent 9,024,039 is issued (05/05/2015)
Corresponding foreign applications are granted

Patent Information:
For Information, Contact:
Margaret Shabashevich,
Manager of Operations
Technology Ventures Office
Brown University
Laurent Brard
Rakesh Singh
Satyan Kalkunte
© 2017. All Rights Reserved. Powered by Inteum