PURPOSE: To provide a new N,N'-disubstituted amide derivative having strong and selective 5-HT3 receptor antagonistic action and useful as an antiemetic, an enterokinetic function controlling agent, a therapeutic agent for migraine, an antipsychotic agent, an antianxiety agent, etc.
CONSTITUTION: The compound of formula I [R1 is H or lower alkyl; R2 and R3 are H, lower alkyl, lower alkenyl, (substituted)aryl-lower alkyl, acyl or lower alkoxycarbonyl; R4 is H, lower alkyl or lower alkoxy; A is CH or N; (n) is 1-3], its hydrate or acid addition salt, e.g. cis-3-amino-4-methyl-1-(1- methylindazol-3-ylcarbonyl)pyrrolidine hydrochloride. The compound of formula can be produced by reacting a carboxylic acid of formula II or its reactive derivative with a compound of formula III.
Maeda Toshio
Kawahara Tomio
Fukutaro Taga
