DERIVATIVES OF P-GUANIDINOBENZOIC ACID AND PHARMACEUTICAL AGENTS CONTAINING THEM AS ACTIVE INGREDIENT

摘要

Compounds presented by the general formula: (IB) wherein Y is oxygen, R2 is H, alkyl, alkoxy, alkoxymethyl, -COOR3, -CH2COOR3, -CH=CH-COOR3, halogen, -CF3, -COR4, -OCOR4, -CH2OCOR4, -SO2R4, -OSO2R4, -CONR5R6, -OCONR5R6, -SO2NR5R6, -COHN- 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 or 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.