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    • 40. 发明公开
    • Antibiotic carbapenem compounds
    • 抗生素碳青霉烯化合物
    • EP0590885A1
    • 1994-04-06
    • EP93307551.7
    • 1993-09-23
    • ZENECA LIMITEDZENECA Pharma S.A.
    • Betts, Michael JohnDavies, Gareth MorseJung, Frederic Henri
    • C07D477/00C07F9/568C07D207/16C07D409/12C07D403/12C07D409/14A61K31/40
    • C07D477/20C07D207/16C07D403/12C07D409/12C07D409/14C07F9/5683
    • The present invention provided a compound of the formula:

      or a pharmaceutically acceptable salt or in vivo hydrolysable ester thereof wherein:
      A is a group of the formula (IA) or (IB):

      R¹ is 1-hydroxyethyl, 1-fluoroethyl or hydroxymethyl;
      R² is hydrogen or C₁₋₄alkyl;
      R³ and R⁴ are the same or different and are a variety of substituents X is alkanediyl containing 1-6 carbon atoms optionally interrupted by O, S(O) x (wherein x is zero, one or two), -CONR⁵- or -NR⁵- wherein R⁵ is hydrogen or C₁₋₄alkyl;
      or X is alkenediyl containing 2-6 carbon atoms optionally interrupted by O, S(O) x or -NR⁵- wherein x and R⁵ are as hereinbefore defined; with the provisos that:

      i) the interrupting function (O,S(O) x ,NR⁵,-CONR⁵-) may be directly linked to the ring A, but is not directly linked to the -COOH function or to any carbon-carbon double bond in X; and
      (ii) when the interrupting function is -SO- or -SO₂- it is not β to the COOH function or δ if there is an intervening carbon-carbon double bond in X.
    • 本发明提供下式化合物或其药学上可接受的盐或其体内可水解的酯,其中:A是式(IA)或(IB)的基团: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和R 4是相同的或不同的,并且是各种取代基X是任选被O,S(O)x(其中x为0,1或2)插入的含有1-6个碳原子的链烷二基,-CONR 5 - 或-NR 5 - 其中R 5是氢或C 1-4烷基; 或X是含有2-6个碳原子的链烯二基,任选被O,S(O)x或-NR 5 - 中断,其中x和R 5如上所定义; 其条件是:i)中断功能(O,S(O)x,NR 5,-CONR 5 - )可直接与环A连接,但不直接与-COOH官能团或与任何碳 - 碳 X中的双键; 和(ii)当中断功能是-SO-或-SO 2时,如果X中存在插入的碳 - 碳双键,则其不是COOH官能团的β或δ。