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Potent and specific immunoproteasome inhibitors

  • US 7,589,066 B2
  • Filed: 03/13/2006
  • Issued: 09/15/2009
  • Est. Priority Date: 03/11/2005
  • Status: Expired due to Fees
First Claim
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1. A compound having a 10-fold or greater preference for inhibiting an immunoproteasome as compared to a constitutive proteasome, wherein the compound is selected from the group consisting of:

  • N-carbobenzyloxy-phenylalanyl-phenylalanylal,N-carbobenzyloxy-homophenylalanyl-phenylalanylal,N-carbobenzyloxy-alanyl-phenylalanylal,N-carbobenzyloxy-glycyl-prolyl-alanyl-phenylalanylal,N-carbobenzyloxy-glycyl-prolyl-phenylalanyl-phenylalanylal,N-carbobenzyloxy-glycyl-phenylalanyl-phenylalanylal,N-carbobenzyloxy-leucyl-norleucine boronic acid,N-carbobenzyloxy-phenylalanyl-phenylalanine boronic acid,N-carbobenzyloxy-homophenylalanyl-phenylalanine boronic acid,N-carbobenzyloxy-leucyl-phenylalanine boronic acid,N-carbobenzyloxy-glycyl-prolyl-alanyl-phenylalanine boronic acid,N-carbobenzyloxy-glycyl-prolyl-phenylalanyl-phenylalanine boronic acid,N-carbobenzyloxy-leucyl-leucyl-phenylalanine boronic acid,N-carbobenzyloxy-glycyl-phenylalanyl-phenylalanine boronic acid,N-carbobenzyloxy-leucyl-norleucine methyl vinyl sulfone,N-carbobenzyloxy-phenylalanyl-phenylalanine methyl vinyl sulfone,N-carbobenzyloxy-homophenylalanyl-phenylalanine methyl vinyl sulfone,N-carbobenzyloxy-leucyl-phenylalanine methyl vinyl sulfone,N-carbobenzyloxy-alanyl-phenylalanine methyl vinyl sulfone,N-carbobenzyloxy-glycyl-prolyl-alanyl-phenylalanine methyl vinyl sulfone,N-carbobenzyloxy-glycyl-prolyl-phenylalanyl-phenylalanine methyl vinyl sulfone,N-carbobenzyloxy-leucyl-leucyl-phenylalanine methyl vinyl sulfone,N-carbobenzyloxy-glycyl-phenylalanyl-phenylalanine methyl vinyl sulfone,N-carbobenzyloxy-leucyl-norleucine epoxy ketone,N-carbobenzyloxy-phenylalanyl-phenylalanine epoxy ketone,N-carbobenzyloxy-homophenylalanyl-phenylalanine epoxy ketone,N-carbobenzyloxy-leucyl-phenylalanine epoxy ketone,N-carbobenzyloxy-alanyl-phenylalanine epoxy ketone,N-carbobenzyloxy-glycyl-prolyl-alanyl-phenylalanine epoxy ketone,N-carbobenzyloxy-glycyl-prolyl-phenylalanyl-phenylalanine epoxy ketone,N-carbobenzyloxy-leucyl-leucyl-phenylalanine epoxy ketone, andN-carbobenzyloxy-glycyl-phenylalanyl-phenylalanine epoxy ketone;

    ora pharmaceutically acceptable salt thereof.

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