发明公开
- 专利标题: Cephalosporin derivatives
- 专利标题(中): Cephalosporinderivate。
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申请号: EP92100119.4申请日: 1992-01-07
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公开(公告)号: EP0550775A1公开(公告)日: 1993-07-14
- 发明人: Albrecht, Harry Allen , Keith, Dennis Dalton , Wei, Chung-Chen
- 申请人: F. HOFFMANN-LA ROCHE AG
- 申请人地址: Postfach 3255 CH-4002 Basel CH
- 专利权人: F. HOFFMANN-LA ROCHE AG
- 当前专利权人: F. HOFFMANN-LA ROCHE AG
- 当前专利权人地址: Postfach 3255 CH-4002 Basel CH
- 代理机构: Martin, Björn (SE)
- 主分类号: C07D501/46
- IPC分类号: C07D501/46 ; C07D501/42 ; A61K31/545 ; C07D501/44
摘要:
Cephalosporin derivatives of the general formula
in which R³ is a group of the formula
R⁶⁰ and R⁶⁵ are hydrogen or lower alkyl, R¹⁵-R¹⁹ are each independently hydrogen, halogen or hydroxy, n is zero or 1, R⁴ and R⁵ are each hydrogen, halogen, lower alkyl, lower alkoxy or amino, R⁷ is hydrogen or lower alkyl and R⁸ is lower alkyl, halo- lower alkyl, C₃-C₇ cycloalkyl or mono-, di- or trihalophenyl, and Z is N or C-R⁹, where R⁹ is hydrogen, halogen, lower alkyl or lower alkoxy; and, when R⁴ is fluoro, R⁵ and R⁷ are hydrogen. R⁸ is cyclopropyl and Z is C-H, R³ can also be one of the groups
in which R⁶¹ and R⁶⁶ are hydrogen or methyl, R¹⁵-R¹⁹ are as above and R⁹⁰ is hydrogen, hydroxy, carboxy, amino or [[4-(lower alkyl)-2,3-dioxo-1-piperazinyl]carbonyl]amino;
pharmaceutically acceptable acid or base addition salts thereof, hydrates of compounds of formula I and hydrates of such salts.
The products have antibacterial activity.
in which R³ is a group of the formula
R⁶⁰ and R⁶⁵ are hydrogen or lower alkyl, R¹⁵-R¹⁹ are each independently hydrogen, halogen or hydroxy, n is zero or 1, R⁴ and R⁵ are each hydrogen, halogen, lower alkyl, lower alkoxy or amino, R⁷ is hydrogen or lower alkyl and R⁸ is lower alkyl, halo- lower alkyl, C₃-C₇ cycloalkyl or mono-, di- or trihalophenyl, and Z is N or C-R⁹, where R⁹ is hydrogen, halogen, lower alkyl or lower alkoxy; and, when R⁴ is fluoro, R⁵ and R⁷ are hydrogen. R⁸ is cyclopropyl and Z is C-H, R³ can also be one of the groups
in which R⁶¹ and R⁶⁶ are hydrogen or methyl, R¹⁵-R¹⁹ are as above and R⁹⁰ is hydrogen, hydroxy, carboxy, amino or [[4-(lower alkyl)-2,3-dioxo-1-piperazinyl]carbonyl]amino;
pharmaceutically acceptable acid or base addition salts thereof, hydrates of compounds of formula I and hydrates of such salts.
The products have antibacterial activity.
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