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US07642369B2 Epoxyketone-based immunoproteasome inhibitors 失效
基于环氧酮的免疫蛋白酶体抑制剂

Epoxyketone-based immunoproteasome inhibitors
Abstract:
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.
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