Quinolonecarboxylic acid compounds, preparation methods and pharmaceutical uses thereof

US7759362B2 · kind B2 · utility

Assignees

• Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences · CN
• Xinchang Pharmaceutical Factory, Zhejiang Medicine Co. Ltd. · CN

Inventors

• Huiyuan Guo · Beijing, CN
• Jiuyu Liu · Beijing, CN

Key dates

• Filing date: Apr 13, 2005
• Grant date: Jul 20, 2010
• Expiry date: Jun 2, 2027

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D471/04
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

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.