US Patent Number
An efficient new route for the preparation of dihydroeponemycin, an active eponemycin derivative, is provided, which includes the synthesis of the intermediate compound, a hydroxymethyl-substituted enone. In addition, a method is provided for synthesizing inhibitors, which includes PI′-modified analogues. These analogues selectively bind to a major immunoproteasome catalytic subunit LMP2 and inactivate its proteolytic activity in a method of treating diseases, including myeloma and other cancers, Huntington's disease and Alzheimer's disease.
University of Kentucky Research Foundation, Lexington, KY (US)
Kim, Kyung Bo and Ho, Yik Khuan, "Epoxyketone-Based Immunoproteasome Inhibitors" (2010). Pharmaceutical Sciences Faculty Patents. 50.