4-,5-,6-and 7-indole derivatives useful for the treatment of...

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

Reexamination Certificate

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C544S373000, C546S201000, C546S277400, C546S277700, C546S278100, C514S323000, C514S339000

Reexamination Certificate

active

06958338

ABSTRACT:
The present invention relates to 4-, 5-, 6- or 7-methylene substituted indolyl derivatives of formula Iwherein R is aryl or heteroaryl, where said aryl or heteroaryl groups may be substituted one or more times with a substituent selected from hydrogen, halogen, cyano, nitro, C1-6-alkyl, C2-6-alkenyl, C2-6-alkynyl, C3-8-cycloalkyl, C3-8-cycloalkyl-C1-6-alkyl, C1-6-alkoxy, C1-6-alkylthio, hydroxy, hydroxy-C1-6-alkyl trifluoromethyl, trifluoromethylsulfonyl, C1-6-alkylsulfonyl, amino, C1-6-alkylamino, di-(C1-6-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;R1is hydrogen, C1-6-alkyl, C2-6-alkenyl, C2-6-alkynyl, C3-8-cycloalkyl, C3-8-cycloalkyl-C1-6-alkyl, aryl, aryl-C1-6-alkyl, acyl, thioacyl, C1-6-alkylsulfonyl, trifluoromethylsulfonyl or arylsulfonyl; andR2and R3are independently selected from hydrogen, halogen, cyano, nitro, C1-6-alkyl, C2-6-alkenyl, C2-6-alkynyl, C3-8-cycloalkyl, C3-8-cycloalkyl-C1-6-alkyl, C1-6-alkoxy, C1-6-alkylthio, hydroxy, hydroxy-C1-6-alkyl trifluoromethyl, trifluoromethylsulfonyl, C1-6-alkylsulfonyl, amino, C1-6-alkylamino, di-(C1-6-alkyl)amino, acyl and aminocarbonyl.The compounds of the invention are selective dopamine D4ligands.

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