OPTIONALLY SUBSTITUTED 8-CYANO-1-CYCLOPROPYL-7-(2,8-DIAZABICYCLO-[4,3,0]-NONAN-8-YL)-6-FLUORO-1,4-DIHYDRO-4-OXO-3-QUINOLIN CARBOXYLIC ACIDS AND THEIR DERIVATIVES, PROCESS PRODUCING THEM AND MEDICAMENTS THEREOF

• Main Authors: HIMMLER, THOMAS DR, BARTEL, STEFAN, RAST, HANS-GEORG, JAETSCH, THOMAS DR, HALLENBACH, WERNER DR, WETZSTEIN, HEINZ-GEORG DR, HEINEN, ERNST, SCHEER, MARTIN DR, STEGEMANN, MICHAEL DR, STUPP, HANS-PETER, PIRRO, FRANZ DR
• Format: Patent
• Language: English
• Published: 28.08.2012
• Subjects: AGRICULTURE; ANIMAL HUSBANDRY; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES, AS HERBICIDES; CHEMISTRY; FISHING; FORESTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HUNTING; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTSTHEREOF; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS; TRAPPING

The present invention relates to novel optionally substituted 8-cyano-1-cyclo-propyl-7-(2,8-diazabicyclo[4.3.0]nonan-8-yl)-6-fluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acids and their derivatives, of the general formula (I)in whichR1 represents hydrogen, C1-C4-alkyl which is optionally substituted by hydroxyl, methoxy, amino, methylamino or dimethylamino, or (5-methyl-2-oxo-1,3-dioxol-4-yl)methyl,R2 represents hydrogen, benzyl, C1-C3-alkyl, (5-methyl-2-oxo-1,3-dioxol-4-yl)methyl, radicals having the structures -CH=CH-COOR3, -CH2CH2COOR3, -CH2CH2CN, -CH2CH2COCH3 or -CH2COCH3, in which R3 represents methyl or ethyl, or a radical of the general structure R4-(NH-CHR5-CO)n-, in which R4 represents hydrogen, C1-C3-alkyl or the radical -COO-tert-butyl, R5 represents hydrogen, C1-C4-alkyl, hydroxyalkyl, aminoalkyl, thioalkyl, carboxyalkyl or benzyl and n is 1 or 2, andY is oxygen or sulfur,the process for their preparation and their use in antibacterial compositions.