Use of arylindole derivatives for the treatment of psychoses

A - Human Necessities – 61 – K

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A61K 31/495 (2006.01) A61K 31/44 (2006.01) A61K 31/445 (2006.01)

Patent

CA 2126571

2126571 9312790 PCTABS00024 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; R1 is hydrogen, or lower alkyl, provided that when X is hydrogen or fluoro, then R1 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 NR2; V1 is -O-R4, -S-R4, -CHR4R5 or -NR4R5; and R3, R4 and R5 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.

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