Invention Grant
- Patent Title: Epoxyketone-based immunoproteasome inhibitors
- Patent Title (中): 基于环氧酮的免疫蛋白酶体抑制剂
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Application No.: US11531129Application Date: 2006-09-12
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Publication No.: US07642369B2Publication Date: 2010-01-05
- Inventor: Kyung Bo Kim , Yik Khuan Ho
- Applicant: Kyung Bo Kim , Yik Khuan Ho
- Applicant Address: US KY Lexington
- Assignee: University of Kentucky Research Foundation
- Current Assignee: University of Kentucky Research Foundation
- Current Assignee Address: US KY Lexington
- Agency: Stites & Harbison PLLC
- Agent Stephen J. Weyer; Mandy W. Decker
- Main IPC: C07C269/00
- IPC: C07C269/00

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.
Public/Granted literature
- US20080064659A1 EPOXYKETONE-BASED IMMUNOPROTEASOME INHIBITORS Public/Granted day:2008-03-13
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