发明公开
- 专利标题： Erythromycin derivatives
- 专利标题（中）： 红霉素衍。
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申请号： EP88311785.5申请日： 1988-12-13
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公开(公告)号： EP0321185A2公开(公告)日： 1989-06-21
- 发明人: Davies, John Sidney
- 申请人： BEECHAM GROUP PLC
- 申请人地址： Beecham House, Great West Road Brentford, Middlesex TW8 9BD GB
- 专利权人： BEECHAM GROUP PLC
- 当前专利权人： BEECHAM GROUP PLC
- 当前专利权人地址： Beecham House, Great West Road Brentford, Middlesex TW8 9BD GB
- 代理机构： Dayneswood, Trevor
- 优先权： GB8729369 19871216
- 主分类号： C07H17/08
- IPC分类号： C07H17/08 ; A61K31/70
摘要：
9- N ,11- O -methylene derivatives of erythromycin-9-imine (wherein the methylene group is optionally substituted) of the general formula IA or IB:
or a pharmaceutically acceptable ester or acid addition salt thereof,
wherein
R¹ denotes hydrogen, an unsubstituted or substituted hydrocarbon group, a heterocyclyl group, or an acyl group;
R³ denotes hydrogen or hydroxy;
R⁶ denotes hydrogen or methyl;
one of R⁷ and R⁸ denotes hydrogen, hydroxy, alkoxy,alkanoyloxy, amino, substituted amino, or a group of the formula R⁹-SO₂-O-, and the other of R⁷ and R⁸ denotes hydrogen, or
R⁷ and R⁸ together denote an oxo group, an oxime group, or a substituted oxime group; and
R⁹ denotes an organic group,
possess improved acid stability, compared with erythromycin A, whilst retaining good antibacterial activity.
or a pharmaceutically acceptable ester or acid addition salt thereof,
wherein
R¹ denotes hydrogen, an unsubstituted or substituted hydrocarbon group, a heterocyclyl group, or an acyl group;
R³ denotes hydrogen or hydroxy;
R⁶ denotes hydrogen or methyl;
one of R⁷ and R⁸ denotes hydrogen, hydroxy, alkoxy,alkanoyloxy, amino, substituted amino, or a group of the formula R⁹-SO₂-O-, and the other of R⁷ and R⁸ denotes hydrogen, or
R⁷ and R⁸ together denote an oxo group, an oxime group, or a substituted oxime group; and
R⁹ denotes an organic group,
possess improved acid stability, compared with erythromycin A, whilst retaining good antibacterial activity.
公开/授权文献
- EP0321185A3 Erythromycin derivatives 公开/授权日：1989-11-02
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