α-KETOAMIDE INHIBITORS OF 20S-PROTEASOME Russian patent published in 2002 - IPC

FIELD: organic chemistry, biochemistry, pharmacy. SUBSTANCE: invention describes novel compounds of the general formula (I): where X₂ means Ar or Ar-X₃ where X₃ means C=O or -CH₂CO- and Ar means phenyl or indole; R₁ and R₂ each is taken independently among hydrogen atom or by-side chains of natural α-amino acids presented by linear or branched (C₁-C₁₀)--alkyl that can be substituted with hydroxy-group, carboxy-group, amino-group, cyclohexyl, phenyl or hydroxy-substituted phenyl, biphenyl, naphthyl or pyridyl; X₁ is taken among -OH or group: where X₄ means OH; R₃ is taken among hydrogen atom or by-side chains of natural α-amino acids presented by linear or branched (C₁-C₁₀)-alkyl that can be substituted with hydroxy-group, phenyl or hydroxy-substituted phenyl. Also, invention describes pharmaceutical composition showing ability to inhibit chymotrypsin-like effect of 20S- -proteasome comprising compound of the formula (I) and one or some pharmaceutical excipients and presented as solution or tablet. EFFECT: valuable biochemical properties of compounds. 15 cl, 2 tbl, 6 ex