ENHANCED ANTI-INFLUENZA AGENTS CONJUGATED WITH ANTI-INFLAMMATORY ACTIVITY
摘要
<p>Novel dual-targeted, bifunctional anti-influenza drugs formed by conjugation with anti-inflammatory agents are disclosed. Exemplary drugs according to the invention include caffeic acid (CA)-bearing zanamivir (ZA) conjugates ZA-7-CA (1), ZA-7-CA-amide (7) and ZA-7-Nap (43) for simultaneous inhibition of influenza virus neuraminidase and suppression of proinflammatory cytokines. Synthetic methods for preparation of these enhanced anti-influenza conjugate drugs are provided. The synthetic bifunctional ZA conjugates act synergistically towards protection of mice lethally infected by H1N1 or H5N1 influenza viruses. The efficacy of ZA-7-CA, ZA-7-CA-amide and ZA-7-Nap conjugates is much greater than the combination therapy of ZA with anti-inflammatory agents.</p>
申请公布号
EP2841066(A4)
申请公布日期
2015.11.25
申请号
EP20130775664
申请日期
2013.04.12
申请人
ACADEMIA SINICA;WONG, CHI-HEUY;FANG, JIM-MIN;LIU, KUNG-CHENG;JAN, JIA-TSRONG;CHENG, YIH-SHYUN E.;CHENG, TING-JEN R.
发明人
WONG, CHI-HUEY;FANG, JIM-MIN;LIU, KUNG-CHENG;JAN, JIA-TSRONG;CHENG, YIH-SHYUN, E.;CHENG, TING-JEN, R.