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
SCHEER, MARTIN DR,HALLENBACH, WERNER DR,JAETSCH, THOMAS DR,WETZSTEIN, HEINZ-GEORG DR,PIRRO, FRANZ DR,HIMMLER, THOMAS DR,STEGEMANN, MICHAEL DR,BARTEL, STEFAN,HEINEN, ERNST,STUPP, HANS-PETER,RAST, HANS-
申请号:
HU9900502
公开号:
HU228036B1
申请日:
1997.02.12
申请国别(地区):
HU
年份:
2012
代理人:
摘要:
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.