PURPOSE: To provide cyclic imino-derivatives having beneficial pharmacological properties such as platelet aggregation inhibiting activities.
CONSTITUTION: The compounds of the formula, for instance, (3S,5S)-5-[[4-(5- amidino-2-pyridyl)phenyl]oxymethyl]-3-carboxymethyl-2-pyrrolidinone and (3S,5 S)-5-[[4-(5-amidino-2-thiazolyl)phenyl]oxymethyl]-3-carboxymethyl-2-pyrrolidinone are provided. In the formula, A is a 4-7 member cyclic alkylene imino replaced by R1, R2 and R3 (R1 is H, an alkyl, aryl, heteroaryl or the like; R2 is H, an alkyl-aryl, aralkyl or the like; R3 is H, an alkyl); X1 is a bond, alkylene; X2 is a bond, O, SO2NH, NH, carbonyl or the like; X3, X5 are each a cycloalkylene, and further, either of the two is alkylene, alkenylene or the like; X4 is a bond, O, CH2, CO, NH, sulphenyl or the like; B is cyano, amidino or the like; Y is an alkylene, O-CH2, S-CH2 or the like; E is carboxy, alkoxycarbonyl or the like.
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