FIELD: organic chemistry, pharmacy. SUBSTANCE: invention relates to novel compounds of the formula (I) where R0 means phenyl; R1 means phenyl, heteroaryl, lower alkyl that can be free or substituted; R2 means free or substituted phenyl, lower alkyl; R3 means hydrogen atom, acyl-group, sulfonyl-group; X and Y mean independently nitrogen or carbon atom; Z is methylene group. These compounds show inhibitory activity with respect to proteases of chymotrypsin type and can be used as inhibitors of indicated enzymes, especially as inhibitors of chymase and as an active component in pharmaceutical composition. Invention relates to a novel method of synthesis of derivatives of acetamide of the formula (I) by oxidation of compound of the formula (II) after removal of protective group of indicated compound if it presents. EFFECT: new compounds indicated above, improved method of their synthesis, valuable biochemical properties. 24 cl, 17 tbl
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Authors
Dates
2002-04-20—Published
1997-09-05—Filed