PURPOSE: To obtain a new compound useful in the prophylaxis or treatment of diseases caused by serotoninergic system, which has an agonist activity against 5-HT3 receptor.
CONSTITUTION: The new compound is a compound of formula I (wherein A is -CH=CH-, -CH=N- or the like; R is H, halogen, 1-4C alkyl, alkoxy, cyano, carboxamide, amino, 1-piperidino or the like; R1 is H or methyl; R2 and R3 are each H or 1-4C alkyl; (n) is 1 or 2; (m) is 0 or 1; and m+n≥2), e.g. 2-(3- aminomethylazetidin-1-yl)-6-chloropyridine hydrochloride. The compound of formula I is obtained by allowing a halo-substituted heterocyclic compound of formula II (wherein R' is identical to R or the like; and Hal is halogen) to react with a blocked amine of formula III (wherein P is an amino protective group) to obtain a compound of formula IV, which is then deprotected. The compound of formula I is useful in the treatment or prophylaxis of dysthymic diseases, anxiety or psychotic disorders or intestinal motoricity diseases, especially constipation.
UNBERUTO GUTSUTSUI
ANTONIINA GIYUDEIICHIE
MARUKO RANDEI
BIBIAN MATSUTSUA
