| abstract |
6- and / or 2-substituted 1-arylindole derivatives of general formula (I) Y 'NR (D / -4 -4, c (1a) 11 W R 3 - (CH 2) -NCV W (1b) wherein Ar is optionally substituted phenyl or a heteroaromatic group; X and X1 are hydrogen, halogen, alkyl, alkoxy, hydroxy, alkylthio, alkylsulfonyl, alkyl or dialkylamino, cyano, trifluoromethyl or trifluoromethylthio; or X and X1 are bonded to form a 5-7 membered carboxyl ring; R 1 is hydrogen or lower alkyl, provided that when X is hydrogen or fluorine, 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 (Ia) or (1b) wherein n is 2-6; W is oxygen or sulfur; U is nitrogen or carbon; Z is - (CH2) m-, -CH = CH-, -COCH2- , -CSCH, - or 1,2-phenylene; V is oxygen, sulfur, CH2 or NR2; V1 is -O-R4, -S-R4-, CHR4R5; and R3, R4 and R5 are hydrogen, alkyl, alkenyl, cycloalkyl or cycloalkylmethyl; inhibits the activation of spontaneously active dopamines urons in the ventral tegmental area of the brain and are thus useful for the treatment of psychoses in humans. |