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Claims for Patent: 6,432,948

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Claims for Patent: 6,432,948

Title: USE OF 7-(2-OXA-5,8-DIAZABICYLCO[4.3.0]NON-8-YL)-QUINOLONE CARBOXYLIC ACID AND NAPHTHYRIDON CARBOXYLIC ACID DERIVATIVES FOR THE TREATMENT OF HELIOBACTER PYLORI INFECTIONS AND ASSOCIATED GASTRODUODENAL DISEASES
Abstract:The invention relates to the use of quinolone- and naphthyridonecarboxylic acid derivatives, which are substituted in the 7-position by a 2-oxa-5,8-diazabicyclo[4.3.0]-non-8-yl) radical, and their pharmaceutically utilizable hydrates and/or salts for the therapy of Helicobacter pylori infections and the gastroduodenal disorders associated therewith.
Inventor(s): Matzke; Michael (Wuppertal, DE), Petersen; Uwe (Leverkusen, DE), Jaetsch; Thomas (Koln, DE), Bartel; Stephan (Kurten, DE), Schenke; Thomas (Gladbach, DE), Himmler; Thomas (Odenthal-Globusch, DE), Baasner; Bernd (Gladbach, DE), Werling; Hans-Otto (Wuppertal, DE), Schaller; Klaus (Wuppertal, DE), Labischinski; Harald (Wuppertal, DE)
Assignee: Bayer Aktiengesellschaft (Leverkusan, DE)
Application Number:09/436,316
Patent Claims: 1. A method for treating a Helicobacter pylori infection and/or a gastroduodenal disorder associated with a Helicobacter pylori infection, said method comprising administering to a patient an effective amount therefor of at least one compound of the formula (I): ##STR43##

in which R.sup.1 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, R.sup.2 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-1,3-dioxol-4-yl)-methyl, A represents N or C--R.sup.3, where R.sup.3 represents hydrogen, halogen, methyl, methoxy, difluoromethoxy or cyano alternatively, together with R.sup.1, can form a bridge of the structure --*O--CH.sub.2 --CH--CH.sub.3 or --*O--CH.sub.2 --N--CH.sub.3, where the atom marked by * is connected to the carbon atom of A, R.sup.4 represents hydrogen, benzyl, C.sub.1 -C.sub.3 -alkyl, (5-methyl-2-oxo-1,3-dioxol-4-yl)-methyl, radicals of the structures --CH.dbd.CH--COOR.sup.5, --CH.sub.2 --CH.sub.2 COOR.sup.5, --CH.sub.2 --CH.sub.2 CN, --CH.sub.2 --CH.sub.2 COCH.sub.3, --CH.sub.2 --COCH.sub.3, in which R.sup.5 represents methyl or ethyl, R.sup.6 represents hydrogen, amino, hydroxyl, methyl or halogen,

or a pharmaceutically utilizable hydrate and/or salt thereof.

2. The method according to claim 1, which comprises administering to said patient at least one compound of formula (I), in which: R.sup.1 represents tert-butyl which is optionally mono- or disubstituted by fluorine or cyclopropyl which is optionally substituted by 1 fluorine atom, R.sup.2 represents hydrogen, alkyl having 1 to 4 carbon atoms or (5-methyl-2-oxo-1,3-dioxol-4-yl)-methyl, A represents C--R.sup.3, where R.sup.3 represents hydrogen, fluorine, methoxy, difluoromethoxy or cyano or alternatively, together with R.sup.1, can form a bridge of the structure --*O--CH.sub.2 --CH--CH.sub.3 or --*O--CH.sub.2 --N--CH.sub.3, where the atom marked by * is connected to the carbon atom of A, R.sup.4 represents hydrogen, C.sub.1 -C.sub.3 -alkyl, radicals of the structures --CH.sub.2 --CH.sub.2 COOR.sup.5, --CH.sub.2 --CH.sub.2 CN, --CH.sub.2 --COCH.sub.3, in which R.sup.5 represents methyl or ethyl, R.sup.6 represents hydrogen, amino, or methyl,

or a pharmaceutically utilizable hydrate and/or salt thereof.

3. The method according to claim 1, which comprises administering to said patient at least one compound of formula (I), in which: R.sup.1 represents tert-butyl which is optionally mono- or disubstituted by fluorine or cyclopropyl, R.sup.2 represents hydrogen, methyl or ethyl, A represents C--R.sup.3, where R.sup.3 represents hydrogen, methoxy, difluoromethoxy or cyano or alternatively, together with R.sup.1, can form a bridge of the structure --*O--CH.sub.2 --CH--CH.sub.3 or --*O--CH.sub.2 --N--CH.sub.3, where the atom marked by * is connected to the carbon atom of A, R.sup.4 represents hydrogen or methyl, R.sup.6 represents hydrogen,

or a pharmaceutically utilizable hydrate and/or salt thereof.

4. The method according to claim 1, which comprises administering to said patient at least one compound of formula (I) in the form of a racemic mixture thereof, or a pharmaceutically utilizable hydrate and/or salt of said racemic mixture.

5. The method according to claim 1, which comprises administering to said patient at least one compound of formula (I) in the form of a diastereomer mixture thereof, or a pharmaceutically utilizable hydrate and/or salt of said diastereomer mixture.

6. The method according to claim 1, which comprises administering to said patient at least one compound of formula (I) in the form of a purified enantiomer thereof, or a pharmaceutically utilizable hydrate and/or salt of said purified enantiomer.

7. The method according to claim 1, which comprises administering to said patient at least one compound of formula (I) in the form of a purified diastereomer thereof, or a pharmaceutically utilizable hydrate and/or salt of said purified diastereomer.

8. A diastereomerically pure and enantiomerically pure compound selected from the group consisting of diastereomerically pure and enantiomerically pure 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, diastereomerically pure and enantiomerically pure 1-cyclopropyl-8-difluoromethoxy-6-fluoro-1,4-dihydro-7-(2-oxa-5,8-diazabic yclo[4.3.0]non-8-yl)-4-oxo-3-quinolinecarboxylic acid, and pharmaceutically utilizable hydrates and/or salts of said diastereomerically pure and enantiomerically pure compound.

9. A pharmaceutical composition comprising at least one compound according to claim 8 and a pharmaceutically utilizable carrier.

10. A method for treating a Helicobacter pylori infection and/or a gastroduodenal disorder associated with a Helicobacter pylori infection, said method comprising administering to a patient an effective amount therefor of at least one compound according to claim 8.
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