PURPOSE: To obtain a new compound, having inhibiting actions on serine proteases and useful for treating and preventing various diseases such as hemorrhagic diseases, thrombus or pancreatitis.
CONSTITUTION: This compound is expressed by formula I [A is (CH2)n or styrene; (n) is 0-5; R1 is H, a halogen or a lower alkyl; R2 is (CH2)mCOR3, etc.; R3 is 2-thiazolylamino, etc.; (m) is 2 or 3] and its salts. The compound of formula I is obtained by reacting a compound of formula II with a compound of formula III in the presence of a condensing agent (e.g. dicyclohexylcarbodiimide) in a solvent (e.g. pyridine). An inhibitor of serine proteases containing the compound of formula I can orally or parenterally and stably be administered and the daily dose thereof is 10-500mg at a time in the case of oral administration.
INOUE TOSHITAKA
IKESUE KOICHI
FUJIMOTO NORIYUKI
TAKEDA KAZUHISA
