| abstract |
Pyrimidinylsulfonamide derivatives of the general formula (1), in which: R 1 represents lower alkyl; R2 represents aryl; heteroaryl; lower alkyl; R3 represents aryl, heteroaryl; R4 represents hydrogen; trifluoromethyl; lower alkyl; lower alkyl amino; lower alkoxy; lower alkoxy-lower alkoxy; hydroxy lower alkoxy; lower alkyl sulfinyl; lower alkylthio; lower alkylthio-lower alkyl; hydroxy lower alkyl; lower alkoxy-lower alkyl; hydroxy-lower alkoxy-lower alkyl, hydroxy-lower alkyl-amino; lower alkyl amino lower alkyl; Not me; di-lower alkyl amino; [N- (hydroxy-lower alkyl) -N- (lower alkyl)] -amino; aryl, aryl-mood; aryl-lower alkyl-amino; aryl-uncle; aryl-lower alkyl-thio, aryloxy; aryl lower alkoxy; aryl-lower alkyl; aryl sulfinyl; heteroaryl; heteroaryl-oxy; heteroaryl-lower alkyl-oxy; heteroaryl amino; heteroaryl-lower alkyl-amino; heteroaryl-thio; heteroaryl-lower alkyl-thio; heteroaryl-lower alkyl; heteroaryl sulfinyl; heterocyclyl; heterocyclyl-lower alkoxy; heterocyclyl-oxy; heterocyclyl amino; heterocyclyl-lower alkyl-amino; heterocyclylthio; heterocyclyl-lower alkyl-thio; heterocyclyl-lower alkyl; heterocyclyl sulfinyl; cycloalkyl; cycloalkyl-oxy; cycloalkyl lower alkoxy; cycloalkyl amino; cycloalkyl-lower alkyl-amino; cycloalkylthio; cycloalkyl-lower alkyl-thio; cycloalkyl-lower alkyl; cycloalkyl sulfinyl; X represents oxygen; a link; Y represents oxygen; -NH-; -NH-SO2-; -NH-SO2NH-; -O-CO-NH-; -NH-CO-O-; -NH-CO-NH-; Z represents oxygen; sulfur; -NH-; n represents an integer equal to 2, 3 or 4; and optically pure enantiomers or diastereomers, mixtures of enantiomers or diastereomers, diastereomeric racemates, mixtures of diastereomeric racemates, and pharmaceutically acceptable meso-forms and salts thereof and their use as active ingredients in the production of pharmaceutical compositions , especially to its use as antagonists of the endothelin receptor in the treatment and prevention of diseases associated with the endothelin system, also to related aspects that include the processes for the preparation of pharmaceutical compositions containing one or more of said compounds . |