发明公开
- 专利标题： Cephalosporins and their homologues, process for their preparation and pharmaceutical compositions
- 专利标题（中）： 头孢菌素及其同系物，其制备方法和药物制剂工艺。
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申请号： EP90303177.1申请日： 1990-03-26
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公开(公告)号： EP0395219A2公开(公告)日： 1990-10-31
- 发明人: Bateson, John Hargreaves , Burton, George , Fell, Stephen Christopher Martin
- 申请人： Beecham Group p.l.c.
- 申请人地址： SB House Great West Road Brentford Middlesex TW8 9BD GB
- 专利权人： Beecham Group p.l.c.
- 当前专利权人： Beecham Group p.l.c.
- 当前专利权人地址： SB House Great West Road Brentford Middlesex TW8 9BD GB
- 代理机构： Moore, James William, Dr.
- 优先权： GB8907171 19890330; GB8920791 19890914
- 主分类号： C07D501/20
- IPC分类号： C07D501/20 ; C07D463/00 ; C07D498/053 ; C07D501/18 ; A61K31/545
摘要：
β-Lactam compounds of the formula (Ia) including pharmaceutically acceptable salts and in vivo hydrolysable esters, processes for their preparation and their use as antibiotics:
wherein
R¹ is hydrogen, methoxy or formamido;
R² is an acyl group, in particular that of an antibacterially active cephalosporin;
CO₂R⁶ is a carboxy group or a carboxylate anion;
R³ is a γ-lactone ring optionally containing an endocyclic double bond, which ring is optionally substituted at any carbon atom by alkyl, dialkylamino, alkoxy, hydroxy, halogen or aryl, which in the case of more than one substituent may be the same or different, or is optionally di-substituted at two adjacent carbon atoms, which are available for substitution, to form an aromatic fused bicyclic system; and X is S, SO, SO₂, O or CH₂.
wherein
R¹ is hydrogen, methoxy or formamido;
R² is an acyl group, in particular that of an antibacterially active cephalosporin;
CO₂R⁶ is a carboxy group or a carboxylate anion;
R³ is a γ-lactone ring optionally containing an endocyclic double bond, which ring is optionally substituted at any carbon atom by alkyl, dialkylamino, alkoxy, hydroxy, halogen or aryl, which in the case of more than one substituent may be the same or different, or is optionally di-substituted at two adjacent carbon atoms, which are available for substitution, to form an aromatic fused bicyclic system; and X is S, SO, SO₂, O or CH₂.
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