SUBSTITUTED HOMOPIPERIDINYL BENZIMIDAZOLE ANALOGUES AS FUNDIC RELAXANTS

摘要

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 represents a saturated or an unsaturated homopiperidinyl having one double bond, and wherein said bivalent radical - is substituted with R<2> being hydrogen, hydroxy, C1-4alkyl, or C1-4alkyloxy; -a1=a<2>-a<4>=a<4>- represents an optionally substituted bivalent radical; R<1> is hydrogen, C1-6alkyl, aryl<1>, C1-6alkyl substituted with aryl<1>, C1-4alkyloxycarbonyl, aryl<1>carbonyl, aryl<1>C1-6alkylarbonyl C1-4alkylcarbonyl, trifluoromethyl, trifluoromethylcarbonyl, C1-6alkylsulfonyl, aryl<1>sulfonyl, methanesulfonyl, benzenesulfonyl, trifluoromethanesulfonyl, dimethylsulfamoyl; X represents O, S or NR<3>, wherein R<3> is hydrogen, C1-6alkyl, methanesulfonyl, benzenesulfonyl, trifluoromethanesulfonyl, dimethylsulfamoyl, C1-4alkyl substituted with aryl<2> and optionally with hydroxy, C1-4alkylcarbony C1-4alkyl substituted with aryl<2>; aryl<1> is optionally substituted phenyl, optionally substituted pyridinyl, naphthyl, quinolinyl, or 1,3-benzodioxolyl; aryl<2> 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.