| abstract |
The present invention is directed to compounds that are proteasome inhibitors, pharmaceutical composition comprising such compounds and methods of treating diseases mediated by unregulated proteasome activity. In particular, the peptide derivatives wherein Het is a heteroaryl ring, and R3'is -(C1-3-CONH-CHR6R7 (where R6 is hydrogen or alkyl and R7 is branched (C4-10)alkyl or cycloalkyl), -(C1-3)-COOR8 (where R8 is branched (C4-10)alkyl or cycloalkyl), or -(C1-3)-Y(C1-3)n1Ar (where Y is -O-, -NH-, or -S(O)n2- where n2 is 0 to 2, nl is 0 or 1, and Ar is aryl); inhibit the 205 and/or 265 proteasomes. |