AMIDINOPHENOL DERIVATIVE AND MEDICINE CONTAINING THE DERIVATIVE AS ACTIVE COMPONENT

摘要

PURPOSE: To provide the subject new compound having phospholipase A2 inhibiting activity and proteinase inhibiting activity, especially trypsin inhibiting activity and useful as an agent for the prevention and/or treatment of the aggravation of inflammatory diseases, pancreatitis, etc., or multiple organ failure. CONSTITUTION: This amidinophenol derivative is a compound expressed by formula I [R<1> and R<2> are each independently H, a 1-4C alkyl, a 2-5C acyl, a halogen, etc.; A is single bond, a 1-4C alkylene, etc.; R<3> is group of formula II (R<7> and R<8> are each independently H, phenyl, a 7-10C phenylalkyl, etc.), group of formula III (R<9> is H, a 1-8C alkyl, a 2-10C alkenyl having 1-3 double bonds, etc). etc.), etc.] or its acid addition salt, e.g. p-(p-amidinophenoxycarbonyl)-α- methylcinnamic acid N-ethoxycarbonyl-N-phenylamide. The compound of formula I can be produced e.g. by esterifying a compound of formula IV (R<3a> is same as R<3> provided that all of R<7> to R<10> in R<3> do not contain COOH and COOt-Bu) with a compound of formula V.