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INFLUENZA VIRUS NEURAMINIDASE INHIBITOR, PREPARATION METHOD THEREFOR AND APPLICATION THEREOF

机译:流感病毒神经氨酸酶抑制剂,其制备方法及其应用

摘要

The present invention relates to an influenza virus neuraminidase inhibitor, a preparation method therefor and an application thereof, which belong to the technical field of pharmaceutical chemistry. The structural general formula of the influenza virus neuraminidase inhibitor is shown in formula I, wherein: m is any natural number selected from 2-11, n is any natural number selected from 3-12, X is selected from OCOO or O; y is selected from formula aa, formula bb and formula cc; R in formula cc is selected from H or formula dd; R' in formula dd is H or a fluorescence labeling group; and Z is any natural number selected from 3-6. The described influenza virus neuraminidase inhibitor has significant inhibitory activity on various influenza viruses, especially on zanamivir-resistant influenza viruses (H3N2, E119V). The water solubility of an original medicine is remarkably improved, the lipid-water distribution coefficient is tens of times higher than that of the original medicine, and the inhibitor can be made into an oral preparation, which is a great breakthrough in pharmaceutical dosage forms.
机译:本发明涉及流感病毒神经氨酸酶抑制剂,其制备方法及其应用,其属于药物化学技术领域。流感病毒神经氨酸酶抑制剂的结构通式示于式I中,其中:M是选自2-11的任何自然数,N是选自3-12,x的任何自然数选自OCOO或O; Y选自式AA,式BB和式CC;式CC中的R选自H或式DD;式DD中的R'是H或荧光标记组; z是选自3-6的自然数。所述流感病毒神经氨酸酶抑制剂对各种流感病毒具有显着的抑制活性,特别是在Zanamivir抗性流感病毒(H3N2,E119V)上。原始药物的水溶性显着改善,脂质分布系数比原药的时间高度高,抑制剂可以制成口服制剂,这是药物剂型的突破。

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