| abstract |
The present invention provides compounds of the formula: (I) and their pharmaceutically acceptable salts, wherein R is C3-C7 cycloalkyl, aryl or C1-C6 alkyl, said C1-C6 alkyl being optionally substituted by fluorine, - COOH, -COO (C1-C4 alkyl), C3-C7 cycloalkyl, adamantyl, aryl or het1, and said C3-C7 cycloalkyl being optionally substituted by 1 or 2 substituents, each independently selected from C1-C4 alkyl , C3-C7 cycloalkyl, C1-C4 alkoxy), hydroxy, fluoro, (C1-C4) fluoroalkyl and (C1-C4) fluoroalkoxy, R1 is phenyl, naphthyl, thienyl, benzothienyl or indolyl, each optionally substituted by 1 or 2 substituents, each independently selected from C1-C4 alkyl, C1-C4 alkoxy, halo and trifluoromethyl; R2 is -CO2H, -CONR3R4, -CONR5 (C3-C7 cycloalkyl), -NR5- (C2-C5 alkanoyl), -NR3R4, -NR5CONR5R6, (C3-C7-C1-C4 alkyl) R5N- , (C3-C7-cycloalkyl-C1-C4-alkyl) 2N, -NR5COCF3, -NR5SO2CF3, -NR5 (SO2 C1-C4-alkyl), -NR5SO2NR5R6, -NR5 (SO2 aryl), -N (aryl) (SO2 C-1-C4 alkyl), -OR5, -O (C3-C7 cycloalkyl), -SO2NR5R6, het3 or a group of formula X is C1-C4 alkylene; X1 is a direct bond or C1-C6 alkylene; X2 is a direct bond, CO, SO2, or NR5CO; and m is 0, 1 or 2; together with intermediates used in the preparation of such derivatives, compositions containing them and the use of such derivatives as tachykinin antagonists. |