PURPOSE: To provide the subject new peptide that is derived from boronic acid, has selectively inhibitory action of trypsin-like serine protease as thrombin or the like and is useful for treating arterial thrombosis.
CONSTITUTION: This new compound is a peptide represented by formula I [R1 is H, a 1-6C acyl, a 1-6C alkoxycarbonyl or the like; R2 is H, (substituted) phenyl, (substituted) benzyl or the like; R'2 is H, benzyl; R3 is a group of formula II (1≤m≤6) or the like; R4 and R5 are each H, a 1-6C alkyl; A is a group of formula III (n is 1 or 2; A2 is phenyl, indanyl, a 3-7C cycloalkyl, a 3-7C cycloalkenyl, bicyclo[2,1,1]hexyl)] or its salts, its enantiomers, diastereomers, epimers. This compound is prepared by allowing a protected amino acid of formula IV (R'1 is the same as R1 except H) to link to an amino acid ester, succinimidizing the product followed by reaction of the product with a compound of formula V (R'3 is a bromoalkyl; R'4 and R'5 are R4 and R5 except H, respectively).
KURISUTEIN RIRA
FUIRITSUPU GUROONESU
MISHIERU ROUBII
TONII BUERUBIYURAN
SERUJIYU SHIMONE
ARAN RIYUPAN