| 摘要 |
6-substituted or 2-alkyl substituted indole or 2,3-dihydroindole derivatives having the general formula I: where Ar is optionally substituted phenyl, or a hetero aromatic group; X is hydro- gen, halogen, alkyl, alkoxy, hydroxy, alkylthio, alkylsulfonyl, alkyl- or dialkylamino, cyano, trifluoromethyl, or trifluoromethylthio; X' is a substituent taken fr om the X- substituents; or X and X' are linked to constitute a 5-7 membered carbocycii c ring; R1 is hydrogen or optionally hydroxy substituted lower alkyl, provided that when X is hydrogen or fluoro, R1 cannot be hydrogen; Y is nitrogen or carbon; the dotted lines indicate optional bonds, provided that the two dotted lines may not at the same time indicate bonds; R is hydrogen, alkyl, alkenyl, cycloalkyl, or cycloalkyl- methyl optionally substituted with hydroxy, or R is a group taken from structures 1a and 1b: wherein n is an integer from 2 to 6; W is oxygen or sulfur; U is nitrogen or carbon; Z is an optionally substituted 2 or 3 membered divalent carbon chain; V is oxygen, sulfur, CH2, or NR2 , wherein R2 is hydrogen, optionally hydroxy substituted alkyl or alkenyl, or a cycloalkyl or cycloalkylmethyl group; V1 is oxygen, sulfur, CH 2 or N- R5, R5 being defined as R2 above; R3 is hydrogen, optionally hydroxy substituted alkylor alkenyl, or a cycloalkyl group; and R4 is one or two groups taken from the 52 R3-substituents, have long lasting serotonin activity with specific binding to the 5-HT2 receptors in the CNS, thus being suitable for therapeutical treatment of CNS disorders such as anxiety, depression, sleep disturbances, migraine , negative symptoms of schizophrenia, and Parkinson's disease.
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