PURPOSE: To provide the title novel derivative having antiarrhythmic and bradycardic activity, thus hopeful of the use in the medical applications, in particular, as a therapeutic agent for arrhythmia, myocardial infarct and stenocardia.
CONSTITUTION: The objective compound of formula I [R1 and R2 are each alkyl, or combined into methylene; X1 is 1-5C alkylene which may bear alkyl group on the chain; R3 and R4 are each aryl or heteroaryl which may have 1-3 substituents (alkyl, alkoxy, halogen, NO2, OH, CN, alkanoyl, NH2, etc.); R5 is alkoxycarbonyl, alkylsulfonyl, of formula II (R7 and R8 are each alkyl which may bear substituent(s); X is O or S), alkanoyl etc.] or its salt permissible as a medicine. The present compound can be obtained by alkanoylation, alkoxycarbonylation, carbamoylation or sulfonylation of the 2-site of the isoquinoline ring of a compound of formula III into a compound of formula IV, which is, in turn, condensed with a compound of formula V at the 8-site hydroxyl group of the isoquinoline ring.
HAYAMA TAKASHI
NISHIKIBE MASARU
YANO MITSUO
