发明授权
US06841562B2 Quinolylpropylpiperidine derivatives, intermediates and compositions containing them, and preparation therefor
失效
醌基丙基哌啶衍生物,含有它们的中间体和组合物及其制备方法
- 专利标题: Quinolylpropylpiperidine derivatives, intermediates and compositions containing them, and preparation therefor
- 专利标题(中): 醌基丙基哌啶衍生物,含有它们的中间体和组合物及其制备方法
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申请号: US10659095申请日: 2003-09-10
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公开(公告)号: US06841562B2公开(公告)日: 2005-01-11
- 发明人: Eric Bacqué , Antony Bigot , Youssef El Ahmad , Jean-Luc Malleron , Serge Mignani , Baptiste Ronan , Michel Tabart , Fabrice Viviani
- 申请人: Eric Bacqué , Antony Bigot , Youssef El Ahmad , Jean-Luc Malleron , Serge Mignani , Baptiste Ronan , Michel Tabart , Fabrice Viviani
- 申请人地址: FR Antony
- 专利权人: Aventis Pharma S.A.
- 当前专利权人: Aventis Pharma S.A.
- 当前专利权人地址: FR Antony
- 代理商 Balaram Gupta
- 优先权: FR0211213 20020911
- 主分类号: A61P31/04
- IPC分类号: A61P31/04 ; C07D211/60 ; C07D401/06 ; C07D409/14 ; A61K31/44 ; C07D215/12 ; C07D215/18
摘要:
Quinolylpropylpiperidine derivatives of general formula (I) in which R1a is hydrogen, halogen, hydroxyl, amino, alkylamino, dialkylamino, hydroxyamino, alkoxyamino or alkylalkoxyamino and R1b is hydrogen, or R1a and R1b form an oxo, R2 is carboxyl, carboxymethyl or hydroxymethyl, R3 is alkyl either substituted with phenylthio optionally substituted with halogen, hydroxyl, alkyl, alkoxy, trifluoromethyl, trifluoromethoxy, carboxyl, alkoxycarbonyl, cyano or amino, or with cycloalkylthio (3 to 7 members) optionally substituted with halogen or trifluoromethyl, or with heteroarylthio (5 to 6 members and 1 to 4 heteroatoms chosen from N, O and S), optionally substituted with halogen, hydroxyl, alkyl, alkoxy, trifluoromethyl, trifluoromethoxy, carboxyl, alkoxycarbonyl, cyano or amino or R3 is propargyl substituted with phenyl or heteroaryl as defined above, R4 is alkyl, alkenyl-CH2— or alkynyl-CH2—, cycloalkyl or cycloalkylalkyl, in their various isomeric forms, separate or as mixtures, and also their salts, their preparation process and intermediates and the compositions containing them. These novel derivatives are potent antibacterial agents.
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