NOVEL ACETAMIDE DERIVATIVES AND PROTEASE INHIBITORS

摘要

Novel acetamide derivatives having a substituted heterocycle and consecutive dicarbonyl structures represented by chemical formula (I), for example, 1-pyrimidinylacetamide compounds, 1-pyrazinylacetamide compounds and 1-triazinylacetamide compounds. Because of showing inhibitory activities on proteases of the chymotrypsin type, these compounds are useful as inhibitors for these enzymes, in particular, chymase inhibitors. In formula (I) R0 represents optionally substituted phenyl; R1 represents optionally substituted aryl, heteroaryl or aliphatic lower alkyl; R2 represents optionally substituted alkyl, arylalkyl or heteroarylalkyl; R3 represents hydrogen; acyl; sulfonyl; isocyanato; thiourea; hydrogen, optionally substituted lower alkyl; aryl(C¿1-7?)alkyl, heteroaryl(C1-7)alkyl, aryl or heteroaryl; X and Y independently represent each nitrogen or carbon; and Z represents polymethylene optionally substituted at the hydrogen atoms thereon.