| abstract |
Compounds presented by the general formula: <IMAGE> (IB) [wherein when Y is oxygen, R2 is H, alkyl, alkoxy, alkoxymethyl, -COOR3, -CH2COOR3, -CH=CH-COOR3, halogen, -CF3, -COR4, -OCOR4, -CH2OCOR4, -SO2R4, -OSO2R4, -CONR5R6, -OCONR5R6, -SO2NR5R6, -CONH-SO2NR5R6, -NHSO2R7, -NO2, -OH, -CH2OH, guanidino, benzyloxy, guanidinophenylthiomethyl, morpholinosulfonylphenoxymethyl, pyridyloxymethyl, or (1,1-dioxothiazol-3-yl)carbonyl, or when Y is sulfur, R2 is H, alkyl, alkoxy, halogen, -COOR3, -CH2COOR3, -NO2, or -SO2NR5R6, and n represents an integer of one to five, and when n represents more than two, each of R2 may be the same group or the different group.] and acid addition salts thereof have inhibitory effect on elastase, and, therefore, are useful for the treatment and/or prevention of diseases induced by abnormal enhancing of degradation of proteins such as elastin and the like, by the action of elastase in mammals, especially in human beings. |