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    • 5. 发明公开
    • GLYCOPEPTIDE ANTIBIOTIC DERIVATIVE
    • 抗生素治疗糖尿病
    • EP2030982A1
    • 2009-03-04
    • EP07744107.9
    • 2007-05-25
    • SHIONOGI & CO., LTD.
    • NISHITANI, YasuhiroYOSHIDA, OsamuIWAKI, TsutomuKATO, Issei
    • C07K9/00A61K38/00A61P31/04C07K7/06C07K14/36
    • C07K9/008A61K38/00A61K38/04
    • The present invention provides a novel glycopeptide antibiotic derivative.
      These derivatives are represented by the formula (I)

      or a pharmaceutically acceptable salt or solvate thereof,
      wherein
      R A is

              -X 1 -Ar 1 -X 2 -Y-X 3 -Ar 2

      wherein
      X 1 , X 2 and X 3 are single bond; heteroatom-containing group selected from the group consisting of -N=, =N-, - NR 1 - (R 1 is hydrogen or lower alkyl), -O-, -S-, -SO- and -SO 2 -, or a linkage thereof; or alkylene or alkenylene optionally substituted and optionally interrupted by one or more of said heteroatom-containing group;
      Y is -NR 2 CO-, -CONR 2 - (R 2 is hydrogen or lower alkyl), or a group of the formula (II) wherein R 3 is alkylene;
      Ar 1 and Ar 2 are a carbocycle or a heterocycle which is optionally substituted and may have an unsaturated bond;
      R B is

              -NHNR X R Y or -NR Z OR W

      wherein
      R X is hydrogen or lower alkyl;
      R Y is hydrogen, optionally substituted lower alkyl, C(=NH)NH 2 , CSNH 2 , COCONH 2 , CN, optionally substituted heterocyclic group, and optionally substituted carbamoyl;
      R Z is hydrogen or lower alkyl;
      R W is hydrogen, optionally substituted lower alkyl, optionally substituted lower alkenyl, optionally substituted heterocyclic group, optionally substituted heterocyclic carbonyl or optionally substituted carbamoyl;
      R C is hydrogen or optionally substituted alkyl, wherein said alkyl may be interrupted by a heteroatom-containing group selected from N=, =N-, -NR 1 - (R 1 is hydrogen or lower alkyl), -O-, -S-, -SO- and -SO 2 -; and
      R is optionally substituted alkyl.
    • 本发明提供了一种新型糖肽抗生素衍生物。 这些衍生物由式(I)表示或其药学上可接受的盐或溶剂化物,其中RA为€ƒ€ƒ€ƒ€ƒ€ƒ-X 1 -Ar 1 -X 2 -YX 3 -Ar 2其中X 1,X 2和X 3为单键; 选自-N =,= N - , - NR 1 - (R 1为氢或低级烷基), - O - , - S - , - SO-和-SO 2 - 的含杂原子的基团,或 其联系; 或任选被取代并任选被一个或多个所述含杂原子基团中断的亚烷基或亚烯基; Y是-NR 2 CO-,-CONR 2 - (R 2是氢或低级烷基)或式(II)的基团,其中R 3是亚烷基; Ar 1和Ar 2是任选被取代并可具有不饱和键的碳环或杂环; R B是€ƒ€ƒ€ƒ€ƒ€ƒ-NHNR X R Y或-NR Z OR W其中R X是氢或低级烷基; R Y是氢,任选取代的低级烷基,C(= NH)NH 2,CSNH 2,COCONH 2,CN,任选取代的杂环基和任选取代的氨基甲酰基; R Z是氢或低级烷基; R W是氢,任选取代的低级烷基,任选取代的低级烯基,任选取代的杂环基,任选取代的杂环羰基或任选取代的氨基甲酰基; RC是氢或任选取代的烷基,其中所述烷基可以被选自N =,N-,-NR 1 - (R 1是氢或低级烷基),-O-,-S- ,-SO-和-SO 2 - ; 和R是任选取代的烷基。
    • 7. 发明公开
    • OXAZOLIDINONE DERIVATIVE HAVING 7-MEMBERED HETERO RING
    • OXAZOLIDINONDERIVAT MIT 7-GLIEDRIGEM HETERORING
    • EP2208729A1
    • 2010-07-21
    • EP08836063.1
    • 2008-10-01
    • Research Foundation Itsuu LaboratoryShionogi&Co., Ltd.
    • SUZUKI, HideyukiUTSUNOMIYA, IwaoSHUDO, KoichiIWAKI, TsutomuYASUKATA, Tatsuro
    • C07D413/10A61K31/55A61K31/553A61P31/04C07D413/14C07D471/14C07D487/04
    • C07D413/14C07D271/02C07D413/10C07D471/14C07D487/04Y02P20/55
    • The present invention provides a novel oxazolidinone derivative of the formula (I):

      wherein
      Ring A is

      (A-1) a 7-membered monocyclic heterocycle containing three N atoms;
      (A-2) a 7-membered monocyclic heterocycle containing two N atoms and one O atom; or
      (A-3) a 7-membered monocyclic heterocycle containing two N atoms and one S atom, SO or SO 2 ,
      wherein said monocyclic heterocycle is optionally substituted, optionally unsaturated and optionally fused with another ring;
      X 1 is a single bond, or a heteroatom-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 heteroatom-containing group;
      Ring B is optionally substituted carbocycle or optionally substituted heterocycle; and
      R 1 is hydrogen, or an organic residue which is able to bind to the 5-position of the oxazolidinone ring in oxazolidinone antimicrobial agents,
      pharmaceutically acceptable salts and solvates thereof which are useful as an antibacterial agent.
    • 本发明提供了式(I)的新型恶唑烷酮衍生物:其中环A为(A-1)含有三个N原子的7-元单环杂环; (A-2)含有两个N原子和一个O原子的7-元单环杂环; 或(A-3)含有两个N原子和一个S原子,SO或SO 2的7-元单环杂环,其中所述单环杂环任选被取代,任选地不饱和并任选地与另一个环稠合; X 1是单键或选自-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为氢的化合物,或可用作抗菌剂的恶唑烷酮抗微生物剂,其药学上可接受的盐和溶剂合物中能够结合恶唑烷酮环的5-位的有机残基。