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    Possibly 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
    1.
    发明授权
    Possibly 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 有权
    可取代的8-氰基-1-环丙基-7-（2,8-二氮杂双环[4.3.0] - 壬烷-8-基）-6-氟-1,4-二氢-4-氧代-3-喹啉羧酸 酸及其衍生物

    公开(公告)号：US06323213B1

    公开(公告)日：2001-11-27

    申请号：US09125191

    申请日：1998-08-13

    申请人： Stefan Bartel ,  Thomas Jaetsch ,  Thomas Himmler ,  Hans-Georg Rast ,  Werner Hallenbach ,  Ernst Heinen ,  Franz Pirro ,  Martin Scheer ,  Michael Stegemann ,  Hans-Peter Stupp ,  Heinz-Georg Wetzstein

    发明人： Stefan Bartel ,  Thomas Jaetsch ,  Thomas Himmler ,  Hans-Georg Rast ,  Werner Hallenbach ,  Ernst Heinen ,  Franz Pirro ,  Martin Scheer ,  Michael Stegemann ,  Hans-Peter Stupp ,  Heinz-Georg Wetzstein

    IPC分类号： A61K31407

    CPC分类号： C07D471/04 ,  A01N43/90

    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 which R1 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, and Y is oxygen or sulfur, the process for their preparation and their use in antibacterial compositions.

    摘要翻译： 本发明涉及新的任选取代的8-氰基-1-环丙基-7-（2,8-二氮杂双环[4.3.0]壬烷-8-基）-6-氟-1,4-二氢-4- 甲氧基，氨基，甲基氨基或二甲基氨基取代的C 1 -C 4 - 烷基，或（5-甲基-2-羟基喹啉羧酸）或其衍生物，其中R 1表示氢， 氧代-1,3-二氧杂环戊烯-4-基）甲基，R 2表示氢，苄基，C 1 -C 3 - 烷基，（5-甲基-2-氧代-1,3-二氧杂环戊烯-4-基）甲基， 结构-CH = CH-COOR 3，-CH 2 CH 2 COOR 3，-CH 2 CH 2 CN，-CH 2 CH 2 COCH 3或-CH 2 COCH 3，其中R 3表示甲基或乙基，或通式结构R4-（NH-CHR5-CO）n - 的基团，其中R4 代表氢，C 1 -C 3 - 烷基或-COO-叔丁基，R 5表示氢，C 1 -C 4 - 烷基，羟基烷基，氨基烷基，硫代烷基，羧基烷基或苄基，n是1或2，Y是氧或硫， 其制备方法及其在抗菌组合物中的应用。