To obtain a new compound having a high selectivity for thrombin and against trypsin and useful as a new orally administrable thrombin inhibitor.
This thrombin inhibitor is a compound of formula I [R1 is acetyl which is substituted with an aryl or an aryloxy, or sulfonyl which is substituted with a (substituted) aryl; X is formula II (R2 and R3 together with an adjacent nitrogen atom form piperidine) or formula III (R4 is H, an alkyl, etc.; R5 is an alkanesulfonyl, an alkyl, etc.); R6 and R7 are each H, an alkyl or an amino], its pharmaceutically permissible salt, hydrate or solvate, or an isomer, e.g. 1-[3-(4-amidrazonophenyl)-(S)-2-(naphthalene-2-sulfonylamino) propionyl]piperidine-(R)-2-carboxylic acid methyl ester. A compound of formula I can be obtained by reacting a compound of formula IV with a compound of formula V.
KIM SANG SOO
HWANG SANG YEUL
YUN MI KYUNG
HWANG SEONG RYUL
HONG SEONG WON
LEE YONG HEE
JEONG YI NA
LEE KOO
SHIN YOU SEUNG