PURPOSE: To provide a new amidine derivative having excellent fibrinogen antagonistic action and useful as an agent for the prevention and treatment of ischemic diseases such as thrombosis, cerebral infarction, myocardial infarction, etc., and arteriosclerosis, etc.
CONSTITUTION: The compound of formula I or formula II (A is CONH or CH2O; B is CH2S or NHCO; B may be CONH when A is CH2O; (n) is 1, 2 or 3; R1 is OH, lower alkoxy, NH2 or OCH2CONR22; R2 is lower alkyl; R3 is OH or lower alkoxy) and its pharmaceutically permissible salt, e.g. 3-[3-(4- amidinobenzyloxy)benzamide]propionic acid. These compounds can be produced by reacting a compound of formula III or IV with hydrogen sulfide using a base as a catalyst or heating the compound together with a compound of the formula RCSNH2 (R is lower alkyl) to convert the R4 group into aminothiocarbonyl, alkylating the S of the group and treating the product with ammonia or an ammonium salt.
JP4853888 | Method for preparing substituted octanoyl amide |
WO/2002/002512 | COMPOUNDS TO TREAT ALZHEIMER'S DISEASE |
KAWASE MASAHIRO
MANNAKA AKIRA
KAWASHIMA YUTAKA
HATAYAMA KATSUO