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    • 2. 发明公开
    • Oxazolidinone derivative having 7-membered hetero ring
    • 恶唑烷酮衍生物7-gliedrigem Heteroring
    • EP2669283A1
    • 2013-12-04
    • EP13178030.6
    • 2008-10-01
    • Shionogi & Co., Ltd.Research Foundation Itsuu Laboratory
    • Suzuki, HideyukiUtsunomiya, IwaoShudo, KoichiIwaki, TsutomuYasukata, Tatsuro
    • C07D413/10C07D413/14C07D471/14C07D487/04A61K31/553A61P31/04
    • C07D413/14C07D271/02C07D413/10C07D471/14C07D487/04Y02P20/55
    • A compound of the formula:

      or a pharmaceutically acceptable salt or solvate thereof wherein
      Y 1 is NP 2 or O;
      P 1 and P 2 are independently hydrogen, or a substituent selected from Substituent Group S1 and amino protecting group;
      R 11 is hydrogen, or a substituent selected from Substituent Group S1 and amino protecting group, with the proviso that R 11 is not -CO(CH 2 ) 3 -CO 2 H, -Ph, -CH 2 Ph, and -(CH 2 ) 3 CH(4-F-Ph) 2 wherein Ph is phenyl;
      Substituent Group S1 consists of optionally substituted lower alkyl, optionally substituted lower alkenyl, optionally substituted cycloalkyl, optionally substituted formyl, optionally substituted (lower alkyl) carbonyl, optionally substituted cycloalkylcarbonyl, optionally substituted (lower alkyl) oxycarbonyl, optionally substituted (lower alkyl) oxythiocarbonyl, optionally substituted arylcarbonyl, optionally substituted aryloxycarbonyl, optionally substituted heterocyclecarbonyl, optionally substituted heterocycleoxycarbonyl, optionally substituted carbamoyl, optionally substituted carbamoylcarbonyl, optionally substituted thiocarbamoyl, optionally substituted (lower alkyl) thiocarbonyl, optionally substituted cycloalkylthiocarbonyl, optionally substituted arylthiocarbonyl, optionally substituted heterocyclic thiocarbonyl, optionally substituted (lower alkyl) sulfonyl, optionally substituted phenylsulfonyl, optionally substituted aromatic heterocyclesulfonyl, optionally substituted aminosulfonyl, optionally substituted aryl, optionally substituted heterocyclic group, cyano, optionally substituted thioformyl, optionally substituted (lower alkenyl) carbonyl, and optionally substituted heterocycleoxycarbonyl;
      with the proviso that the compound is not the following compound:


      wherein Ph is phenyl.
    • 下式的化合物或其药学上可接受的盐或溶剂化物,其中Y 1是NP 2或O; P 1和P 2独立地为氢,或选自取代基组S1和氨基保护基的取代基; R 11是氢或选自取代基组S1和氨基保护基的取代基,条件是R 11不是-CO(CH 2)3 -CO 2 H,-Ph,-CH 2 Ph和 - (CH 2)3 CH(4-F-Ph)2,其中Ph是苯基; 取代基组S1由任选取代的低级烷基,任选取代的低级烯基,任选取代的环烷基,任选取代的甲酰基,任选取代的(低级烷基)羰基,任选取代的环烷基羰基,任选取代的(低级烷基)氧羰基,任选取代的(低级烷基)氧硫基羰基 任选取代的芳基羰基,任选取代的芳基羰基,任选取代的杂芳基羰基,任选取代的杂环羰基,任选取代的氨基甲酰基,任选取代的氨基甲酰基,任选取代的氨基甲酰基,任选取代的硫代氨基甲酰基,任选取代的(低级烷基)硫代羰基,任选取代的环烷硫基羰基,任选取代的芳硫基羰基,任选取代的杂环硫代羰基, 任选取代的(低级烷基)磺酰基,任选取代的苯磺酰基,任选取代的芳族杂环磺酰基,任选取代的 氨基磺酰基,任选取代的芳基,任选取代的杂环基,氰基,任选取代的硫代甲酰基,任选取代的(低级烯基)羰基和任选取代的杂环氧羰基; 条件是该化合物不是以下化合物:其中Ph是苯基。
    • 6. 发明公开
    • Antimicrobial oxazolidinone derivatives
    • 抗恶唑烷恶唑烷酮
    • EP2181993A1
    • 2010-05-05
    • EP10001092.5
    • 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
    • A compound of the formula:

      or a pharmaceutically acceptable salt or solvate thereof, wherein
      Ring A is
      (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, wherein said monocyclic hetero ring is optionally substituted, and said monocyclic hetero ring is optionally condensed with another ring,

      X 1 is a single bond, or a hetero atom-containing group selected from the group consisting of -O-, -S-, -NR 2 -, -CO-, -CS-, -CONR 3 -, -NR 4 CO-, -SO 2 NR 5 -, and -NR 6 SO 2 -, wherein R 2 , R 3 , R 4 , R 5 and R 6 are independently hydrogen or lower alkyl, or lower alkylene or lower alkenylene each optionally interrupted by said hetero atom-containing group;
      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.
    • 下式的化合物或其药学上可接受的盐或溶剂化物,其中环A是含有至少三个N原子的至少7元单环杂环的(A-1) (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,其中所述单环杂环任选被取代,并且所述单环杂环任选地与另一个环X 1缩合 或选自-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 3,R 4,R 5和R 6独立地为氢或低级烷基,或低级亚烷基或低级亚烯基,各自任意地被所述杂原子 包含组; 环B是任选取代的碳环或任选取代的杂环; R 1是氢,或者可以在恶唑烷酮抗微生物剂中结合恶唑烷酮环的5-位的有机残基。