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    • 2. 发明公开
    • NOVEL COMPOUND HAVING HETEROCYCLIC RING
    • NEER VERBINDUNG MIT HETEROCYCLISCHEM RING
    • EP2009012A1
    • 2008-12-31
    • EP07740496.0
    • 2007-03-30
    • Research Foundation Itsuu LaboratoryShionogi Co., Ltd.
    • SUZUKI, HideyukiHIZATATE, ShojiUTSUNOMIYA, IwaoSHUDO, Koichi
    • C07D413/10A61K31/55A61K31/553A61P31/04C07D413/14C07D417/14C07D471/14
    • C07D273/06C07D255/02C07D413/10C07D413/14C07D417/14C07D471/14Y02P20/55
    • The invention provides a novel oxazolidinone derivative represented by the formula (I):

      wherein
      Ring A is optionally substituted or fused and represents
      (A-1) at least 7-membered monocyclic hetero ring containing at least three N atoms; (A-2) at least 6-membered monocyclic hetero ring containing at least two N atoms and at least one O atom; or (A-3) at least 7-membered monocyclic hetero ring containing at least two N atoms and at least one S atom;
      X 1 is a single bond, -O-, -S-, -NR 2 -, -CO-, -CS-, - CONR 3 -, -NR 4 CO-, -SO 2 NR 5 -, and -NR 6 SO 2 - (wherein R 2 - R 6 are independently hydrogen or lower alkyl), or lower alkylene or lower alkenylene in which one of the preceding groups may intervene;
      Ring B is optionally substituted carbocycle or optionally substituted heterocycle;
      R 1 is hydrogen, or an organic residue which is able to bind to the 5-position of oxazolidinone ring in oxazolidinone antimicrobial agent,
      and an antibacterial agent containing the same.
    • 本发明提供由式(I)表示的新型恶唑烷酮衍生物:其中环A任选被取代或稠合并且代表(A-1)含有至少三个N原子的至少七元单环杂环; (A-2)至少含有至少两个N原子和至少一个O原子的6元单环杂环; 或(A-3)至少含有至少两个N原子和至少一个S原子的7元单环杂环; X 1是单键,-O - , - S-,-NR 2 - , - CO - , - CS-, -​​ CONR 3 - , - NR 4 CO - , - SO 2 NR 5 - 和-NR 6 SO 2 - (其中R 2 -R 6独立地是氢或低级烷基)或其中一个前述基团可以介导的低级亚烷基或低级亚烯基; 环B是任选取代的碳环或任选取代的杂环; R 1为氢,或能够与恶唑烷酮抗微生物剂中的恶唑烷酮环的5位结合的有机残基,以及含有该残基的抗菌剂。