PURPOSE: To obtain a new 4-phthalazine derivative, having powerful inhibitory action on blood platelet agglutination and further direct action on contraction of cardiac infarction lesions even by oral administration as a preventive and therapeutic agent for cerebral angiopathy, ischemic cardiopathy and circulation disorder.
CONSTITUTION: A compound, e.g. D-1-α-methylbenzylamino-4-phenylphthalazine expressed by formula I [R1 is 1-5C alkyl or 1-5C hydroxyalkyl; R2 is H or 1-5C alkyl or R1 and R2 mutually link to form 2-6C alkylene which may have 0; R3 to R5 are H, halogen, 1-4C alkyl or 1-4C alkoxy; the adjacent R3 and R4 or R5 may mutually form 0(CH2)pO (p is 1, 2 or 3) or further R5 is CF3 or OH; l and m are 1 or 2; m is 1, 2 or 3], its optical antipode or pharmaceutically permissible acid addition salt. The aforementioned compound is obtained by reacting a compound expressed by formula V with a compound expressed by formula VI and useful as a preventive and therapeutic agent for cerebral thrombosis, cerebral embolism, cardiac infarction, peripheral circulation disorder, etc.
IWASE NORIMICHI
TAMAO YOSHIKUNI
KANAYAMA TOSHIMOTO
Next Patent: TRIFLUORO-AND CHLORODIFLUORO-METHOXYPYRIMIDINES AND THEIR PREPARATION