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    • 2. 发明公开
    • Cephalosporins, processes for their preparation and pharmaceutical compositions containing them
    • 头孢菌素类,它们的制备方法和含有它们的药物组合物。
    • EP0304158A1
    • 1989-02-22
    • EP88306420.6
    • 1988-07-13
    • IMPERIAL CHEMICAL INDUSTRIES PLCICI PHARMA
    • Arnould, Jean ClaudeJung, Frederick HenriBoucherot, DominiqueStrawson, Colin JohnDavies, David Huw
    • C07D501/46C07D501/40
    • C07D501/46C07D501/40
    • Cephalosporin derivatives having a 3-position substituent of the formula I are described:
      wherein R 1 is hydrogen, alkenyl or optionally substituted alkyl, Het is a 5- or 6-membered heterocyclic ring bonded via a carbon atom to the amide linkage, wherein Het is selected from a group of the formulae II - III:
      wherein A is CH or a nitrogen atom; B is oxygen, sulphur or a group NR 4 ; one or two of D, E, F and G are nitrogen atoms and the remainder are CH groups: or Het is a pyrazinone, pyridinone, pyridazinone or pyrimidinone ring, or is a thione equivalent of such a ring, said rings having a substituent R 4 on one nitrogen atom, or is pyranone, or pyranthione; the ring Het being fused by any two adjacent carbon atoms to the benzene ring; and Het being attached to the -CH 2 NR'CO- group via a carbon atom;

      R 2 is hydroxy or an in vivo hydrolysable ester thereof;
      R 3 is ortho to R 2 and is hydroxy or an in vivo hydrolysable ester thereof; and R 4 has various values. The use of such compounds as antibacterial agents is described as are processes for their preparation and intermediates therefor.
    • 具有下式的3位取代基的头孢菌素衍生物我描述: worin - [R <1>为氢,烯基或任选substituiertem烷基,Het是经由碳原子键合的5-或6-元杂环 酰胺键,worin Het是选自式餐饮II的选择 - III: worin A为CH或氮原子; B是氧,硫或基团NR <4>; 一个或两个的D,E,F和G为氮原子,其余的是CH基团:或Het是吡嗪酮,吡啶酮,哒嗪酮或嘧啶酮环,或者是一个硫酮等价搜索一个环的,所述具有取代基R的环 <4>在一个氮原子,或是吡喃酮,或pyranthione; 所述环的Het由任何两个相邻碳原子与苯环稠合; 和Het被附接到经由碳原子的-CH 2 NR <1> CO-基团; [R <2>为羟基或其体内可水解酯; [R <3>是邻至R <2>和是羟基或其体内可水解酯; 且R <4>具有各种值。 因为是它们的制备方法及其中间体测试作为抗菌剂的化合物的用途进行说明。