Derivatives of p-substituted phenyl ester of pivalic acid.

摘要

A derivative of general formula: <CHEM> wherein Y is -SO2- or - @-, (i) R<1> and R<2> each represents, same or different, (1) -H, (2) C1-16 alkyl or (3) the formula: -X @@@@(R<4>)n wherein X is single-bond, -SO2-, C1-4 alkylene, C1-4 alkylene substituted by -COOH or <CHEM> @ @@ @ is carbocyclic or heterocyclic ring, n is 1 SIMILAR 5, R<4> is -H or C1-8 alkyl, C1-14 alkoxy, C1-6 alkylthio, -OH, halogen, -NO2 or trihalomethyl, the formula: -NR<4><1>R<4><2> wherein R<4><1> and R<4><2> each represents halogen or C1-4 alkyl, tetrazole, -SO3H or -CH2OH, the formula:-SO2NR<4><1>R<4><2> the formula: -Z<4><1>-COOR<4><3> wherein Z<4><1> is single-bond, C1-4 alkylene or C2-4 alkenylene, R<4><3> is -H, C1-4 alkyl or benzyl, the formula: -CONR<4><1>R<4><2> the formula:-COO-Z<4><2>-COOR<4><3> wherein Z<4><2> is C1-4 alkylene, R<4><3> is -H or C1-4 alkyl, the formula: -COO-Z<4><2>-CONR<4><1>R<4><2> the formula: -OCO-R<4><5> wherein R<4><5> is is C1-8 alkyl or p-guanidinophenyl, the formula: -CO-R<4><6> is wherein R<4><6> is C1-4 alkyl, the formula: -O-Z<4><3>-COOR<4><5> wherein Z<4><3> is C1-6 alkylene, the formula: <CHEM> wherein - @-Z<4><4>-CO is an amino acid residue, R<4><8> is -H or C1-4 alkyl, R<4><9> is -OH, C1-4 alkoxy, -NH2, amino substituted by one or two C1-4 alkyl, carbamoylmethoxy or carbamoylmethoxy substituted by one or two C1-4 alkyl at N atom of carbamoyl, wherein <CHEM> is C3-6 heterocyclic ring, (ii) R<1>, R<2> and N atom bonded to R<1> and R<2> together represents heterocyclic ring containing at least a N atom(s) and substituted by -COOH or unsubstituted heterocyclic ring containing at least a N atom(s), R<3> is (1) -H, (2) -OH, (3) C1-6 alkyl, (4) halogen, (5) C1-4 alkoxy or (6) C2-5 acyloxy, m is 1-4, and non-toxic salts thereof which possess inhibitory activity on elastase, and are therefore useful for treating and/or preventing pulmonary emphysema, atherosclerosis and rheumatoid arthritis.