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    • 6. 发明专利
    • Nucleoside-type antibiotic
    • 核苷类抗生素
    • JP2012096997A
    • 2012-05-24
    • JP2009043189
    • 2009-02-25
    • Hokkaido UnivShionogi & Co Ltd国立大学法人北海道大学塩野義製薬株式会社
    • MATSUDA AKIRAICHIKAWA SATOSHI
    • C07H19/06A61K31/7072A61P31/04A61P43/00
    • C07H19/067
    • PROBLEM TO BE SOLVED: To provide a compound having an antibacterial activity and a derivative thereof, more preferably an antibacterial nucleoside compound that can inhibit the activity of MraY to exert an antibacterial activity and a derivative of the nucleoside compound, particularly a novel derivative of Muraymycin that is an MraY inhibitor.SOLUTION: A novel derivative of Muraymycin or a pharmaceutically acceptable salt thereof is provided. The compound has good intracellular penetration properties and a potent antibacterial activity. The compound also has resistance against enzymes such as an esterase occurring in blood. A preferred embodiment of the compound has an inhibitory activity on MraY. The preferred embodiment of the compound is effective against resistant bacteria such as VRE and MRSA.
    • 待解决的问题:为了提供具有抗菌活性的化合物及其衍生物,更优选可以抑制MraY发挥抗菌活性的活性的抗菌核苷化合物和核苷化合物的衍生物,特别是新颖的 作为MraY抑制剂的Muraymycin的衍生物。 解决方案:提供了Muraymycin或其药学上可接受的盐的新型衍生物。 该化合物具有良好的细胞内渗透性能和有效的抗菌活性。 该化合物还具有对诸如血液中发生的酯酶等酶的抗性。 化合物的优选实施方案对MraY具有抑制活性。 该化合物的优选实施方案对抗抗性细菌如VRE和MRSA是有效的。 版权所有(C)2012,JPO&INPIT