Potent and specific immunoproteasome inhibitors
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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Abstract
Compounds and methods of selectively inhibiting an immunoproteasome are described. Also described are methods of treating a cancer, an inflammation, and/or an autoimmune disease and methods of suppressing endogenous antigenic peptide generation by administering to a subject in need of treatment thereof a therapeutic amount of an immunoproteasome specific inhibitor.
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1 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:
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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, and N-carbobenzyloxy-glycyl-phenylalanyl-phenylalanine epoxy ketone;
ora pharmaceutically acceptable salt thereof.
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Specification