LACTAM DERIVATIVE AND ITS SALT

摘要

PROBLEM TO BE SOLVED: To obtain a new lactam derivative having potent anticoagulation action due to reversibly inhibiting thrombin, and useful for therapy and/or prevention of various diseases caused by thrombus and embolus of cerebral embolism, myocardial infarction and pulmonary infarction, etc. SOLUTION: This new compound is a lactam derivative or its salt of formula I [R<1> is a (carboxyl substituted) 1-6C alkyl; (n) is an integer of 2-4; Ar is phenyl, or a condensed polycyclic compound residue], e.g. 1-butyl-3-(6,7-dimethoxy-2- naphthylsulfonyl)amino-3-(3-guanidinopropyl)-2-pyrrolidinone hydrochloride. The compound of formula I is obtained by e.g. eliminating the protecting group Y1 of a compound of formula II (Y1 is an amino protecting group), then reacting with an amidino compound of formula III (R<2> is an alkoxy, alkylthio, sulfonyl, or pyrazolyl).