Chinese Academy of Medical Sciences

Xinchang Pharmaceutical Factory, Zhejiang Medicine Co. Ltd.

Jiuyu Liu

Huiyuan Guo

This invention discloses novel quinolonecarboxylic acid derivatives, pharmaceutically acceptable salts or hydrates thereof, and their preparation methods and medical uses. The compounds in this invention show potent antibacterial activity against broad-spectrum pathogenic bacteria, with favorable pharmacokinetics and very low toxicity. The quinolinecarboxylic acid derivatives, which possess a hydrogen atom or an amino group at C-5 position, cis-substituted optical or racemic 2,8-diazo-dicyclo[4,3,0]nonanyl at C-7 position, and difluoromethoxyl at C-8 position of quinolone core, have superior activity against gram-positive bacteria and broad spectrum antibacterial activity compared with the known quinolones.

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Beijing, China

Jiuyu Liu