Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1985-05-30
1987-01-13
Ford, John M.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
544 9, 540546, 540555, 540578, C07D51304, C07D51312, A61K 3154
Patent
active
046364994
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 perferably 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 an 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.
REFERENCES:
patent: 4255431 (1981-03-01), Junggren et al.
patent: 4359465 (1982-11-01), Ruwart
Im et al., The Journal of Biological Chemistry, vol. 260, No. 8, pp. 4591-4597 (1985).
J.P.O.S., vol. 65, No. 7, pp. 403-407 (Jul. 1983).
McArthur et al., Gastroenterology, vol. 86, p. 1178, (1984) May 20-23, New Orleans, ACA.
Rackur et al., Biochemical and Biophysical Research Communications, vol. 128, No. 1, pp. 477-484 (Apr. 16, 1985).
Brandstrom Arne E.
Lindberg Per L.
Wallmark Bjorn
Aktiebolaget Hassle
Ford John M.
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