THE USE OF 70(2-OXA-5,8-DIAZABICYCLO4.3.0NON-8-YL)-QUINOLONE CARBOXYLIC ACID AND NAPHTHRYIDON CARBOXYLIC ACID DERIVATIVES FOR THE TREATMENT OF HELICOBASTER PYLORI INFECTIONS AND ASSOCIATED GASTRODUODENAL DISEASES

摘要

1. Use of compounds comprising quinoline carboxylic acid derivatives as an active agent of the general formula (I) in which R1 represents alkyl having 1 to 4 C atoms, which is optionally mono- or disubstituted by halogen, phenyl which is optionally substituted by 1 or 2 fluorine atoms or cyclopropyl which is optionally substituted by 1 or 2 fluorine atoms, R2 represents hydrogen, alkyl having 1 to 4 carbon atoms, which is optionally substituted by hydroxyl, methoxy, amino, methylamino or dimethylamino, or (5-methyl-2-oxo-l,3-dioxol-4-yl)-methyl, A represents N or C-R3, where R3 represents hydrogen, halogen, methyl, methoxy, difluoromethoxy or cyano alternatively, together with R1 , can form a bridge of the structure -*O-CH2-CH-CH3 or -*O-CH2-N-CH3, where the atom marked by * is connected to the carbon atom of A, R4 represents hydrogen, benzyl, C1-C3-alkyl, (5-methyl-2-oxo-l,3-dioxol-4-yl)-methyl, radicals of the structures -CH=CH-COOR5, -CH2CH2COOR5, -CH2CH2CN, -CH2CH2COCH3, -C2COCH3, in which R5 represents methyl or ethyl, R6 represents hydrogen, amino, hydroxyl, methyl or halogen, in the form of racemates, diastereomer mixtures or as enantiomerically pure or diastereomerically pure compounds, and their pharmaceutically utilizable hydrates and/or salts for the therapy of Helicobacter pylori infections and the gastroduodenal disorders associated therewith. 2. Use of compounds of the formula (I), in which R1 represents tert-butyl which is optionally mono- or disubstituted by fluorine or cyclopropyl which is optionally substituted by 1 fluorine atom, R2 represents hydrogen, alkyl having 1 to 4 carbon atoms or (5-methyl-2-oxo-1,3-dioxol-4-yl)-methyl, A represents C-R3, where R3 represents hydrogen, fluorine, methoxy, difluoromethoxy or cyano or alternatively, together with R1, can form a bridge of the structure -*O-CH2-CH-CH3 or -*O-CH2-N-CH3, where the atom marked by * is connected to the carbon atom of A, R4 represents hydrogen, C1-C3-alkyl, radicals of the structures, -CH2CH2COOR5, -CH2C2CN, -CH2COCH3 in which R5 represents methyl or ethyl, R6 represents hydrogen, amino or methyl, and their pharmaceutically utilizable hydrates and/or salts for the therapy of Helicobacter pylori infections and the gastroduodenal disorders associated therewith. 3. Use a pharmaceutical compound of the formula (I), in which R1 represents tert-butyl which is optionally mono- or disubstituted by fluorine, or cyclopropyl, R2 represents hydrogen, methyl or ethyl, A represents C-R3, where R3 represents hydrogen, methoxy, difluoromethoxy or cyano or alternatively, together with R1, can form a bridge of the structure -*O-CH2-CH-CH3 or -*O-CH2-N-CH3, where the atom marked by * is connected to the carbon atom of A, R4 represents hydrogen or methyl or pharmaceutically acceptable hydrate and/or a salt thereof. 4. Use a pharmaceutical compound according to Claims 1 to 3 for the therapy of Helicobacter pylon infections and the gastroduodenal disorders associated therewith. 5. Use a pharmaceutical compound according to Claim 1, comprising 8-cyano-l-cyclopropyl-6-fluoro-7-((1S,6S)-2-oxa-5,8-diazabicyclo-[4.3.0]non-8-yl)-l,4-dihydro-4-oxo-3-quinolinecarboxylic acid and its pharmaceutically utilizable hydrates and/or salts. 6. Use a pharmaceutical compound according to Claim 1, comprising a diastereomerically pure and enantiomerically pure compounds from the group consisting of 8-cyano-1-cyclopropyl-6-fluoro-7-(2-oxa-5,8-diazabicyclo[4.3,0]non-8-yl)-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid, 1-cyclopropyl-8-difluoromethoxy-6-fluoro-1,4-dihydro-7-(2-oxa-5,8-diaza-bicyclo[4.3.0]non-8-yl)-4-oxo-3-quinolinecarboxylic acid and their pharmaceutically utilizable hydrates and/or salts. 7. Use a pharmaceutical compound according to Claim 6, comprising 8-cyano-l-cyclopropyl-6-fluoro-7-((lS,6S)-2-oxa-5,8-diazabicyclo[4.3.0]-non-8-yl)-l,4-dihydro-4-oxo-3-quinolinecarboxylic acid and its pharmaceutically utilizable hydrates and/or salts. 8. Quinolinecarboxylic acid derivatives of the general formula (II) in which R represents cyano- or difluoromethoxy group, diastereomers, enanstomers thereof and pharmaceutically utilizable hydrates and/or salts 9. Quinolinecarboxylic acid derivatives according to Claim 8 of the general formula (II), comprising 8-cyano-l-cyclopropyl-6-fluoro-7-((lS,6S)-2-oxa-5,8-diazabicyclo[4.3.0]non-8-yl)-1,4-dihydro-4-oxo-3-qumolinecarboxylic acid and its phannaceutically utilizable hydrates and/or salts.