abstract |
The present invention relates to compounds of formula (I), their prodrugs, N-oxides, addition salts, quaternary amines and stereochemically isomeric forms, wherein the bivalent radical -A- represents a saturated or an unsaturated homopiperidinyl having one double bond, and wherein said bivalent radical -A- is substituted with R2 being hydrogen, hydroxy, C¿1-4?alkyl, or C1-4alkyloxy; -a?1=a2-a3=a4¿- represents an optionally substituted bivalent radical; R1 is hydrogen, C¿1-6?alkyl, aryl?1, C¿1-6alkyl substituted with aryl1, C1-4alkyloxycarbonyl, aryl1carbonyl, aryl1C1-6alkylarbonyl C1-4alkylcarbonyl, trifluoromethyl, trifluoromethylcarbonyl, C1-6alkylsulfonyl, aryl1sulfonyl, methanesulfonyl, benzenesulfonyl, trifluoromethanesulfonyl, dimethylsulfamoyl; X represents O, S or NR3, wherein R3 is hydrogen, C¿1-6?alkyl, methanesulfonyl, benzenesulfonyl, trifluoromethanesulfonyl, dimethylsulfamoyl, C1-4alkyl substituted with aryl?2¿ and optionally with hydroxy, C¿1-4?alkylcarbonylC1-4alkyl substituted with aryl?2; aryl1¿ is optionally substituted phenyl, optionally substituted pyridinyl, naphthyl, quinolinyl, or 1,3-benzodioxolyl; aryl2 is optionally substituted phenyl; fundic relaxating activity. Processes for preparing said products, formulations comprising said products and their use as a medicine are disclosed, in particular for treating dyspeptic symptoms, irritable bowel syndrome and other conditions related to a hampered or impaired relaxation of the fundus. |