| abstract |
6-and/or 2-substituted 1-arylindole derivative of general formula (I), where Ar is optionally substituted phenyl or a hetero aromatic group; X and X' are hydrogen, halogen, alkyl, alkoxy, hydroxy, alkylthio, alkylsulfonyl, alkyl- or dialkylamino, cyano, trifluoromethyl, or trifluoromethylthio; or X and X' are linked to constitute a 5-7 membered carbocyclic ring; R<1> is hydrogen, or lower alkyl, provided that when X is hydrogen or fluoro, then R<1> is not hydrogen; Y is nitrogen or carbon; R is hydrogen, alkyl, alkenyl, cycloalkyl, or cycloalkylmethyl, or R is a substituent of formula (1a) or (1b), wherein n is 2-6; W is oxygen or sulfur; U is nitrogen or carbon; Z is -(CH2)m-, -CH=CH-, -COCH2-, -CSCH2- or 1,2-phenylene; V is oxygen, sulfur, CH2 or NR<2>; V<1> is -O-R<4>, -S-R<4>, -CHR<4>R<5> or -NR<4>R<5>; and R<3>, R<4> and R<5> are hydrogen, alkyl, alkenyl, cycloalkyl, or cycloalkylmethyl; inhibit the firing of spontaneously active dopamine neurones in the ventral tegmental area of the brain and are thus useful for the treatment of psychoses in humans. |