发明名称 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 form s, 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, C1-4alkyl, or C1-4alkyloxy; - a1=a2-a3=a4- represents an optionally substituted bivalent radical; R1 is hydrogen, C1-6alkyl, aryl1, C1-6alkyl substituted with aryl1, C1- 4alkyloxycarbonyl, aryl1carbonyl, aryl1C1-6alkylarbonyl C1-4alkylcarbonyl, trifluoromethyl, trifluoromethylcarbonyl, C1-6alkylsulfonyl, aryl1sulfonyl, methanesulfonyl, benzenesulfonyl, trifluoromethanesulfonyl, dimethylsulfamoy l; X represents O, S or NR3, wherein R3 is hydrogen, C1-6alkyl, methanesulfonyl , benzenesulfonyl, trifluoromethanesulfonyl, dimethylsulfamoyl, C1-4alkyl substituted with aryl2 and optionally with hydroxy, C1-4alkylcarbonylC1-4alk yl substituted with aryl2; 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.
申请公布号 CA2393158(A1) 申请公布日期 2001.06.28
申请号 CA20002393158 申请日期 2000.12.14
申请人 JANSSEN PHARMACEUTICA N.V. 发明人 JANSSENS, FRANS EDUARD;SOMMEN, FRANCOIS MARIA;GUILLEMONT, JEROME EMILE GEORGES
分类号 C07D487/04;A61K31/55;A61P1/04;A61P1/06;A61P43/00;C07D403/04;C07D403/14;C07D405/14;C07D413/04;C07D417/04;C07D471/04;C07D498/04;C07D513/04;(IPC1-7):C07D471/04;C07D221/00;C07D235/00;C07D401/14 主分类号 C07D487/04
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