| 摘要 |
NEW MATERIAL:A guanidinobenzoic acid derivative of formula I [R is 4-(imidazol-1-yl)phenyl, 4-indolyl, 5-indolyl, 5-isoquinolyl, 2-carbozolyl, 1,4- benzodioxan-2-yl-methyl, 2-picolineamidyl or 2-dibenzofuryl] or an acid adduct salt thereof. EXAMPLE:4-(Imidazol-1-yl)phenyl 4-(guanidinobenzoate.dimethanesulfonic acid salt). USE:The compound of formula I or the salt has an excellent trypsin-resistant activity and is useful as a remedy for diseases caused by the activation of the protease. PREPARATION:p-Guanidino benzoic acid of formula II is reacted with e.g. 4-(imidazole-1-yl)phenol in the presence of a catalyst, a condensing agent, etc., to provide the compound of formula I. |
