PURPOSE: To obtain an antithrombotic agent of a specific formula which has a high anticoagulant effect, antithrombotic effect and thrombine selectivity.
CONSTITUTION: This compound is a compound of formula I {wherein R1 is H; X is prolinyl or azetidinyl-2-carbonyl; and Y is formula II [wherein Z is hydroxy, a 1-4C alkoxy or -NHR2 (wherein R2 is H, a 1-6C alkyl, cyclopentyl, cyclohexyl or the like); R3 is a 1-4C alkyl, (non)substituted phenyl or (non) substituted benzyl; Z1 is a bond or -CH2-; and R4 is a 1-6C alkyl, 1-4C alkoxy, cyclopentyl, cyclohexyl or (non)substituted aryl]} or a salt or solvate thereof, preferably 1-methylindolyl-2-carbonyl-D-(α-methyl)phenylglycinyl-L-azetidinyl-2- carbonyl-L-arginine aldehyde or the like. Here, the objective compound is obtained, e.g. via binding PY-COOH (wherein P is an amino protective group) to a carboxy-protected proline, etc.
ROBAATO SEODOA SHIYUUMAN
JIERARUDO FUROIDO SUMISU
MAIKERU ROBAATO UIRII
Next Patent: ANTITHROMBOTIC AGENT