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    • 2. 发明申请
    • NOVEL ANTIBIOTICS AGAINST RESISTANT BACTERIA
    • 抗抗生素的新型抗生素
    • WO2010030808A2
    • 2010-03-18
    • PCT/US2009056552
    • 2009-09-10
    • CHANG CHENG-WEI TUNIV UTAH STATE
    • CHANG CHENG-WEI T
    • A61K31/7036A61K31/702A61P31/04
    • A61K31/702A61K31/7036C07H15/232Y02P20/55
    • The present invention is in the technical field of antimicrobials. More particularly, the present invention is in the technical field of aminoglycoside antimicrobials. In one aspect the present invention provides novel methods of synthesizing new classes of antimicrobial aminoglycosides. In a second aspect the present invention also provides two novel aminoglycosides useful as antimicrobials. The present invention relates to novel antibacterial aminoglycoside derivatives that exhibit improved antimicrobial properties. One advantage of the present invention is a facile synthetic protocol for the production of neomycin B derivatives with various modifications at the 5" position, which enables the direct modification of commercially available aminoglycosides using carbamate type protecting groups. Also provided are methods of using the compound of the present invention. The compounds of the present invention are useful in treating or preventing bacterial infection and may be especially useful in the treatment of infections with MRSA and VRE.
    • 本发明在抗菌药物的技术领域。 更具体地说,本发明在氨基糖苷类抗菌药物的技术领域。 一方面,本发明提供了合成新类型的抗微生物氨基糖苷类的新方法。 在第二方面,本发明还提供了两种用作抗微生物剂的新型氨基糖苷类。 本发明涉及具有改善的抗微生物性质的新型抗菌氨基糖苷衍生物。 本发明的一个优点是用于生产在5“位上具有各种修饰的新霉素B衍生物的简便的合成方案,其能够使用氨基甲酸酯型保护基团直接修饰市售的氨基糖苷类,还提供了使用化合物 本发明的化合物可用于治疗或预防细菌感染,并且可特别用于治疗MRSA和VRE的感染。