发明名称 SUBSTITUTED HOMOPIPERIDINYL BENZIMIDAZOLE ANALOGUES AS FUNDIC RELAXANTS
摘要 The present invention relates to compounds of formula their prodrugs, N-oxides, addition salts, quaternary amines and stereochemically isomeric forms, wherein the bivalent radical -A- represents a saturated or unsaturated homopiperidinyl having one double bond, and wherein said bivalent radical -A- is substituted with R2 being hydrogen, hydroxy, C1-C4alkyl, or C1-C4 alkoxy; -a1=a2-a3=a4 represents an optionally substituted bivalent radical; R1 is hydrogen, C1-6alkyl, aryl1, C1-6alkyl substituted with aryl1,C1-4alkyloxycarbonyl, aryl1carbonyl, aryl1C1-6alkylcarbonyl, C1-4alkylcarbonyl, trifluoromethyl, truifluoromethylcarbonyl, C1-6alkylsulfonyl, aryl1sulfonyl, methanesulfonyl, benzenesulfonyl, trifluoromethanesulfonyl, dimethylsulfamoyl; X represents O, S or NR3, wherein R3 is hydrogen, C1-6alkyl, methanesulfonyl, benzenesulfonyl, truifluoromethanesulfonyl, dimethylsulfamoyl, C1-4alkyl, substituted with aryl2 and optionally with hydroxy, C1-4alkylcarbonylC1-4alkyl substituted with aryl2; aryl1 is optionally substituted phenyl, optionally substituted pyridinyl, naphthyl, quinolinyl, or 1,3-benzodioxolyl; aryl 2 is optionally substituted phenyl, fundic relaxing 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. 10 claims
申请公布号 BG106749(A) 申请公布日期 2003.01.31
申请号 BG20020106749 申请日期 2002.05.29
申请人 JANSSEN PHARMACEUTICA N.V. 发明人 JANSSENS, FRANS E.;GUILLEMONT, JEROME E.;SOMMEN, FRANCOIS M.
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 主分类号 C07D487/04
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