发明授权
US06323213B1 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
- 专利标题: 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
- 专利标题(中): 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
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申请号: US09125191申请日: 1998-08-13
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公开(公告)号: US06323213B1公开(公告)日: 2001-11-27
- 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
- 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
- 优先权: DE19606762 19960223; DE19633805 19960822
- 主分类号: A61K31407
- IPC分类号: A61K31407
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.
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