IP Library › Granted Patent US 7,589,066
Granted Patent B2
US 7,589,066 · App. 11/374,652 · Granted Sep 15, 2009

Potent and specific immunoproteasome inhibitors

Assignees: The University of North Carolina at Chapel Hill; Mount Sinai School of Medicine of New York University
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Quick Facts
Patent No.
US 7,589,066
App. No.
11/374,652
Granted
Sep 15, 2009
Kind
B2
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.

Claims (34)

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, and

N-carbobenzyloxy-glycyl-phenylalanyl-phenylalanine epoxy ketone; or

a pharmaceutically acceptable salt thereof.

Continuity (2)
Provisional Application 6066059600 · Mar 11, 2005
Related Publication 20060241056A1 · Oct 26, 2006