| 摘要 |
5-Substituted trans-1-piperazinoindan derivatives having general formula (I) , wherein X is halogen, trifluoromethyl, alkyl, alkylthio, alkyloxy, hydroxy, alkylsulphonyl, alkyl- or dialkylamino, trifluoromethylthio or cyano; R is hydrogen, or alkyl, alke- nyl, cycloalkyl, or cycloalkyl lower alkyl, optionally substituted with hydroxy, or R is a substituent (a), wherein n is an integer from 1 to 6; U is CH or N; Y is CH2, O, S or N-R1, R1 being hydrogen or cycloalkyl, cycloalkylmethyl, alkyl or alkenyl op- tionally substituted with hydroxy or an optionally substituted phenyl group; W is O or S; Z is -(CH2)4-, (b), (c), where R2 and R3 are hydrogen or lower alkyl, -CH=CH-, -CH=CH-CH2-, optionally substituted 1,2-phenylene, 1,2-C6H4CH2- (to form a quinazolidinone or -thione ring system) or 1,2-C6H4CO- (to form a quinazolidindion or thioxoquinazolidinon ring system); and Ar is an optionally substituted phenyl, thiophene or furane rin g; are selective, centrally acting 5-HT2 antagon- ists useful in the treatment of anxiety, depression, sleeping disorders, negative symptoms of schizophrenia and migraine.
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