发明授权
EP0546179B1 4-O-(AMINOGLYCOSYL)- OR 4,6-DI-O-(AMINOGLYCOSYL)-2,5-DIDEOXY-5,5-DIFLUOROSTREPTAMINE DERIVATIVE AND PRODUCTION THEREOF
失效
4-O-(氨基糖基) - 或4,6-DI-O-(氨基糖基)-2,5-二脱氧-5,5-二氟右啡肽衍生物及其生产
- 专利标题: 4-O-(AMINOGLYCOSYL)- OR 4,6-DI-O-(AMINOGLYCOSYL)-2,5-DIDEOXY-5,5-DIFLUOROSTREPTAMINE DERIVATIVE AND PRODUCTION THEREOF
- 专利标题(中): 4-O-(氨基糖基) - 或4,6-DI-O-(氨基糖基)-2,5-二脱氧-5,5-二氟右啡肽衍生物及其生产
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申请号: EP91914768.6申请日: 1991-08-22
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公开(公告)号: EP0546179B1公开(公告)日: 1997-02-12
- 发明人: TAKEUCHI, Tomio , UMEZAWA, Sumio , TSUCHIYA, Tsutomu , SHITARA, Tetsuo , FUKATSU, Shunzo , UMEMURA, Eijiro
- 申请人: ZAIDAN HOJIN BISEIBUTSU KAGAKU KENKYU KAI
- 申请人地址: 14-23, Kami Ohsaki 3-chome Shinagawa-ku Tokyo JP
- 专利权人: ZAIDAN HOJIN BISEIBUTSU KAGAKU KENKYU KAI
- 当前专利权人: ZAIDAN HOJIN BISEIBUTSU KAGAKU KENKYU KAI
- 当前专利权人地址: 14-23, Kami Ohsaki 3-chome Shinagawa-ku Tokyo JP
- 代理机构: Goddar, Heinz J., Dr.
- 优先权: JP221085/90 19900824
- 国际公布: WO9203460 19920305
- 主分类号: C07H15/224
- IPC分类号: C07H15/224 ; C07H15/234 ; C07H15/236 ; A61K31/71
摘要:
The invention provides 5-deoxy-5,5-difluoro derivatives of aminoglycoside antibiotics of neamine, kanamycin A, kanamycin B, gentamicin and seldomycin, each synthesized as a novel compound, and also 1-N-(α-hydroxy-φ-aminoalkanoyl) derivatives synthesized from the newly obtained 5-deoxy-5,5-difluorokanamycins A and B and analogs thereof. The 5-deoxy-5,5-difluoro derivatives thus obtained have antibacterial activities superior or substantially equivalent to those of the amino-glycoside antibiotics from which they are derived and further have a remarkably improved median lethal dose (LD50) when intravenously administered to mice and a remarkably reduced toxicity on mammals.
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