4-, 5-, 6- AND 7-INDOLE DERIVATIVES USEFUL FOR THE TREATMENT OF CNS DISORDERS.

摘要

The present invention relates to 4-, 5-, 6- or 7-methylene substituted indolyl derivatives of formula I wherein R is aryl or heteroaryl, where said aryl or heteroaryl groups may be substituted one or more times with a substituent seleceted from hydrogen, halogen, cyano, nitro, C_1-6-alkyl, C_2-6-alkenyl, C_2-6-alkynyl, C_3-8-cycloalkyl, C_3-8-cycloalkyl-C_1-6-alkyl, C_1-6-alkoxy, C_1-6-alkylthio, hydroxy, hydroxy-C_1-6-alkyl trifluoromethyl, trifluoromethylsulfonyl, C_1-6-alkylsulfonyl, amino, C_1-6-alkylamino, di-(C_1-6-alkyl)amino, acyl, aminocarbonyl and a methylene dioxy group; X is N, C or CH; provided that the dotted line indicates a bond when X is C and no bond when X is N or CH; R¹ is hydrogen, C_1-6-alkyl, C_2-6-alkenyl, C_2-6-alkynyl, C_3-8-cycloalkyl, C_3-8-cycloalkyl-C _1-6-alkyl, aryl, aryl-C_1-6-alkyl, acyl, thioacyl, C_1-6-alkylsulfonyl, trifluoromethylsulfonyl or arylsulfonyl; and R² and R³ are independently selected from hydrogen, halogen, cyano, nitro, C_1-6-alkyl, C_2-6-alkenyl, C_2-6-alkynyl, C_3-8-cycloalkyl, C_3-8-cycloalkyl-C_1-6-alkyl, C_1-6-alkoxy, C_1-6-alkylthio, hydroxy, hydroxy-C_1-6-alkyl trifluoromethyl, trifluoromethylsulfonyl, C_1-6-alkylsulfonyl, amino, C_1-6-alkylamino, di-(C_1-6-alkyl)amino, acyl and aminocarbonyl. The compounds of the invention are selective dopamine D₄ ligands.