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    • 8. 发明公开
    • Antibiotic carbapenem compounds
    • 抗生素碳青霉烯
    • EP0581502A1
    • 1994-02-02
    • EP93305609.5
    • 1993-07-16
    • ZENECA LIMITEDZENECA Pharma S.A.
    • Jung, Frederic HenriLohmann, Jean Jacques
    • C07D477/00C07F9/568C07D417/12C07D403/12C07D207/34C07D417/14C07D403/14A61K31/40
    • C07D477/20C07D207/34C07D403/12C07D403/14C07D417/12C07D417/14C07F9/5683
    • The present invention relates to carbapenems and provides a compound of the formula (I)

      wherein :

      R 1 is i-hydroxyethyl, 1-fluoroethyl or hydroxymethyl ;
      R 2 is hydrogen or C 1-4 alkyl;
      R 3 is hydrogen or C 1-4 alkyl;
      A is a 5-membered heteroaryl ring containing one nitrogen atom and up to two additional heteroatoms selected from nitrogen, oxygen and sulphur ; and is bonded to the nitrogen of the linking carbamoyl group by a carbon atom in the ring, is substituted with the carboxy group on a carbon atom in the ring and is optionally further substituted on a carbon atom in the ring ; and

      in any ring -NH-, H is optionally replaced by C 1-4 alkyl;
      or a pharmaceutically acceptable salt or in vivo hydrolysable ester thereof. Processes for their preparation, intermediates in their preparation, their use as therapeutic agents and pharmaceutical compositions containing them are also described.
    • 本发明涉及碳青霉烯并提供式(I)化合物其中:R 1是1-羟乙基,1-氟乙基或羟甲基; R 2是氢或C 1-4烷基; R 3是氢或C 1-4烷基; A是含有一个氮原子和多达两个另外选自氮,氧和硫的杂原子的5元杂芳基环; 并且通过环中的碳原子与连接的氨基甲酰基的氮键合,被环中的碳原子上的羧基取代,并且任选地在环中的碳原子上进一步取代; 并且在任何环-NH-中,H任选被C 1-4烷基取代; 或其药学上可接受的盐或体内可水解的酯。 还描述了其制备方法,其制备中的中间体,它们作为治疗剂的用途和含有它们的药物组合物。