Substituted homopiperidinyl benzimidazole analogues as fundic relaxants

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United States of America Patent

PATENT NO 7304052
SERIAL NO

10169011

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Abstract

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The present invention relates to compounds of formula (I) ##STR00001## their prodrugs, N-oxides, addition salts, quaternary amines and stereochemically isomeric forms, wherein the bivalent radical -{circle around (A)}- represents a saturated or an unsaturated homopiperidinyl having one double bond, and wherein said bivalent radical -{circle around (A)}- is substituted with R.sup.2 being hydrogen, hydroxy, C.sub.1-4alkyl, or C.sub.1-4alkyloxy; -a.sup.1=a.sup.2-a.sup.3=a.sup.4-represents an optionally substituted bivalent radical; R.sup.1 is hydrogen, C.sub.1-6alkyl, aryl.sup.1, C.sub.1-6alkyl substituted with aryl.sup.1, C.sub.1-4alkyloxycarbonyl, aryl.sup.1carbonyl, aryl.sup.1C.sub.1-6alkylarbonyl C.sub.1-4alkylcarbonyl, trifluoromethyl, trifluoromethylcarbonyl, C.sub.1-6alkylsulfonyl, aryl.sup.1sulfonyl, methanesulfonyl, benzenesulfonyl, trifluoromethanesulfonyl, dimethylsulfamoyl; X represents O, S or NR.sup.3, wherein R.sup.3 is hydrogen, C.sub.1-6alkyl, methanesulfonyl, benzenesulfonyl, trifluoromethanesulfonyl, dimethylsulfamoyl, C.sub.1-4alkyl substituted with aryl.sup.2 and optionally with hydroxy, C.sub.1-4alkylcarbonylC.sub.1-4alkyl substituted with aryl.sup.2; aryl.sup.1 is optionally substituted phenyl, optionally substituted pyridinyl, naphthyl, quinolinyl, or 1,3-benzodioxolyl; aryl.sup.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.

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Patent Owner(s)

Patent OwnerAddress
JANSSEN PHARMACEUTICA N VBEERSE BEERSE ANTWERP

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Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Guillemont, Jeo Issy-les-Moulineaux, FR 6 86
Janssens, Frans Eduard Beerse, BE 45 270
Sommen, Franc Beerse, BE 4 7

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