AMIDINOPHENOL DERIVATIVE, ITS PRODUCTION AND LEUKOTRIENE B4 ANTAGONISTIC AGENT, PHOSPHOLIPASE A2 AND/OR TRYPSIN INHIBITOR CONTAINING AMIDINOPHENOL DERIVATIVE AS ACTIVE INGREDIENT

摘要

PURPOSE: To obtain an amidinophenol derivative useful for preventing and treating inflammatory and allergic diseases, disseminated intravascular coagulation, pancreatitis, multiple organ disorder, etc. CONSTITUTION: Thus compound of formula I [ring D is formula II, III (R0 is H, a 1-4C alkyl or a 1-4C alkoxy), etc.; T is NH or O; E is a single bond or formula IV (R300 and R400 are each H or a 1-4C alkyl); A0 is a single bond, a 1-4C alkylene, an oxy- or a thio-1-4C alkylene or a substitutive 2-8C alkenylene; R is formula V to VII (R50 and R60 are each H, a 1-8C alkyl, a 2-8C alkenyl, phenyl, a 1-4C alkylene-O-benzoyl, etc.; R80 and R90 are each an alkyl, a 1-4C alkylene-phenyl), etc.], e.g. N-2-propenyl-N- ethoxycarbonylmethyl-4-(4-amidinophenoxycarbonyl)phenoxyacetamide. The leukotriene B4 (LTB4 ) antagonistic agent, phospholipase A2 (PLA2 ) and/or trypsin inhibitor contain the compound of formula I or VIII [R1 and R2 are each H or COR4 (R4 is a 1-3C alkyl); A is a single bond, a 1-4C alkylene, etc.; R3 is CON(R7 )R8 (R7 and R8 are each H, phenyl, etc.)].