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    • 5. 发明授权
    • Aminoacid derivatives of cephalosporin compounds
    • 头孢菌素化合物的氨基酸衍生物
    • US4311699A
    • 1982-01-19
    • US112656
    • 1980-01-31
    • Theodore H. HaskellThomas F. MichJoseph P. SanchezDietrich Schweiss
    • Theodore H. HaskellThomas F. MichJoseph P. SanchezDietrich Schweiss
    • C07D239/36C07D501/24C07D521/00A61K31/545C07D501/34C07D501/56
    • C07D239/36C07D231/12C07D233/56C07D249/08
    • Novel organic amide compounds which are N-[2-[(acylaminoacylamino or aminoacylamino)phenyl]-4-hydroxy-5-pyrimidinylcarbonyl]cephalosporin compounds having broad spectrum antibacterial utility are provided by (a) reacting the free amino acid of the appropriate cephalosporin or the acid salt or silylated derivative or complex thereof with a reactive derivative of the corresponding N-2-[(acylaminoacylamino or aminoacylamino)phenyl]-4-hydroxy-5-pyrimidine carboxylic acid or (b) reacting the free amino acid 7-aminocephalosporanic acid or a related compound or the acid salt or silylated derivative thereof with a reactive derivative of the corresponding D-N-[2-[(acylaminoacylamino or aminoacylamino)phenyl]-4-hydroxy-5-pyrimidinylcarbonyl]-2-substituted glycine. Pharmaceutical compositions containing said compounds and methods for treating infections using said compositions are also disclosed.
    • 通过(a)使适当头孢菌素的游离氨基酸反应,得到具有广谱抗菌效用的N- [2 - [(酰氨基酰氨基或氨基酰氨基)苯基] -4-羟基-5-嘧啶基羰基]头孢菌素的新型有机酰胺化合物 或其相应的N-2 - [(酰氨基酰基氨基或氨酰基氨基)苯基] -4-羟基-5-嘧啶羧酸的反应性衍生物的酸式盐或甲硅烷基化衍生物或其配合物,或(b)使游离氨基酸7- 氨基头孢烷酸或相关化合物或其酸盐或甲硅烷基化衍生物与相应的DN- [2 - [(酰氨基酰基氨基或氨酰基氨基)苯基] -4-羟基-5-嘧啶基羰基] -2-取代的甘氨酸的反应性衍生物。 还公开了含有所述化合物的药物组合物和使用所述组合物治疗感染的方法。