To obtain a new indoline derivative having pharmacological activities such as antagonistic activity to 5-hydroxytryptamine or the like and useful for treating a central nervous system disorder, a withdrawal symptom, schizophrenia or the like.
A compound of formula I [R1 is thiazolyl or a (substituted) imidazolyl; R2 is H, a halogen, a lower alkyl, a lower alkoxy, cyano or a trihalo (lower) alkyl; R3 is H or a lower alkylthio; X is NH, O or CH2], for example, 1-[[3-(imidazol-1-yl)phenyl]carbamoyl]-5-methylthio-6-trifluoromethylindoline. Further, a compound of formula I is obtained, for example, by reacting a compound of formula II with a compound of formula III (R4 and R5 are each a lower alkoxy) and subjecting the obtained compound of formula IV to a cyclization reaction with formaldehyde.
GLEN W SPEARS
SASAKI HIROSHI
TAKAHASHI FUMIE
