DIAZEPANE DERIVATIVES OR SALTS THEREOF

摘要

PURPOSE: Provided are diazepane derivatives or their salts which exhibit a blood-anticoagulant effect on the basis of the inhibition of activated blood coagulation factor X and are useful as blood anticoagulants or preventive or therapeutic drugs for diseases caused by thrombus or embolus. CONSTITUTION: The diazepane derivative is represented by the formula(1), wherein A and B are identical or different, and each is aryl or heteroaryl which may contain 1-3 substituent; X1 is -C(=O)-NR¬2- or -NR¬2-C(=O)-; X¬2 is -C(=O)-NR¬3- or -NR¬3-C(=O)-; R is hydrogen, halogen, lower alkyl or -O- lower alkyl; and R¬1, R¬2 and R¬3 are identical or different and each represents hydrogen or lower alkyl;. The diazepane derivatives such as 4-((3-carbamidoylphenylamino)methyl)- 3-(4-(4-methyl-1,4-diazepan-1-yl)benzoylamino)benzoic acid and 3-hydroxy-4'-methoxy-2-((4-(4-methyl-1,4-diazepan-1- yl)benzoyl)amino))benzanilide or their salts are used as active ingredients of the drugs.