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Details for Patent: 4,725,691

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Details for Patent: 4,725,691

Title: 2-[8-quinolinyl]-sulphinyl-1H-benzimidazole
Abstract:Novel compounds of the formula IIIa ##STR1## wherein R.sup.1a, R.sup.2a, R.sup.3a and R.sup.4a are the same or different and are hydrogen, an alkyl, alkoxy optionally completely or predominantly substituted by fluorine or chlorine, halogen, --CN, --CF.sub.3, --NO.sub.2, --COR, --COOR, aryl, aryloxy or arylalkoxy group, or adjacent groups R.sup.1a, R.sup.2a, R.sup.3a and R.sup.4a together with the adjacent carbon atoms in the benzimidazole ring form a 5-, 6- or 7-membered monocyclic ring or a 9-, 10- or 11-membered bicyclic ring, which rings may be saturated or unsaturated and may contain 0-3 heteroatoms selected from N and O and which rings may be optionally substituted with 1-4 substitutents selected from alkyl groups with 1-3 carbon atoms, halogen preferably F or Cl, alkylene radicals containing 4-5 carbon atoms giving spiro compounds, or two or four of these substituents together form one or two oxy groups ##STR2## whereby if R.sup.1a, R.sup.2a, R.sup.3a and R.sup.4a together with the adjacent carbon atoms in the benzimidazole ring form two rings they may be condensed with each other, R.sup.5a is hydrogen or an alkyl group, R.sup.6a is hydrogen or an alkyl group or R.sup.5a and R.sup.6a are joined together to form an alkylene chain, R.sup.7a is hydrogen, an alkyl, alkoxy, alkenyloxy or alkynyloxy group, R.sup.8a is hydrogen or an alkyl group, or R.sup.6a and R.sup.7a, or R.sup.7a and R.sup.8a together with the adjacent carbon atoms in the pyridinium ring form a ring wherein the part constituted by R.sup.6a and R.sup.7a or R.sup.7a and R.sup.8a, is --CH.dbd.CH--CH.dbd.CH--, --O--(CH.sub.2).sub.p --, --CH.sub.2 (CH.sub.2).sub.p --, --O--CH.dbd.CH--, --NH--CH.dbd.CH--, ##STR3## or --S--(CH.sub.2).sub.p --, wherein p is 2, 3 or 4 and the O, S and N atoms always are attached to position 3 in the compound IIIa, R is a alkyl, cycloalkyl, aryl or arylalkyl group, and X.sup.- is a pharmaceutically acceptable anion, process for preparation thereof, pharmaceutical compositions containing such compounds and their use in medicine.
Inventor(s): Brandstrom; Arne E. (Gothenburg, SE), Lindberg; Per L. (Askim, SE), Wallmark; Bjorn (Molnlycke, SE)
Assignee: Aktiebolaget Hassle (Molndal, SE)
Filing Date:Sep 30, 1986
Application Number:06/913,689
Claims:1. A compound of the formula ##STR18## wherein R.sup.1a, R.sup.2a, R.sup.3a and R.sup.4a are the same or different and are selected from the group consisting of

hydrogen,

alkyl of 1-7 carbon atoms,

alkoxy of 1-7 carbon atoms,

fluorine or chlorine substituted alkoxy of 1-7 carbon atoms,

halogen,

--CN,

--CF.sub.3,

--NO.sub.2,

--COR,

--COOR,

aryl of up to 10 carbon atoms, and

aryloxy of up to 10 carbon atoms, wherein R is alkyl of 1 to 7 carbon atoms, cycloalkyl or 3 to 10 carbon atoms, aryl of up to 10 carbon atoms or aralkyl of up to 10 carbon atoms in the aryl group and 1 to 7 carbon atoms in the alkyl group;

R.sup.7a is selected from the group consisting of

hydrogen,

alkyl of 1-7 carbon atoms,

alkoxy of 1-7 carbon atoms,

alkenyloxy of 2-5 carbon atoms, and

alkynyloxy of 2-5 carbon atoms; and

R.sup.8a is hydrogen or an alkyl group of 1-7 carbon atoms.
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