The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.

The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.

Date of Patent:
Nov. 20, 2018

Filed:

Mar. 15, 2013
Applicant:

Academia Sinica, Taipei, TW;

Inventors:

Chi-Huey Wong, Rancho Sante Fe, CA (US);

Jim-Min Fang, Taipei, TW;

Kung-Cheng Liu, Taipei, TW;

Jia-Tsrong Jan, Taipei, TW;

Yih-Shyun E. Cheng, Taipei, TW;

Ting-Jen R. Cheng, Taipei, TW;

Assignee:

ACADEMIA SINICA, Taipei, TW;

Attorney:
Primary Examiner:
Int. Cl.
CPC ...
A61K 31/351 (2006.01); C07D 309/28 (2006.01); A61K 47/55 (2017.01); A61K 47/48 (2006.01);
U.S. Cl.
CPC ...
A61K 47/481 (2013.01); A61K 31/351 (2013.01); A61K 47/55 (2017.08); C07D 309/28 (2013.01);
Abstract

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.


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