Title:
INFLUENZA VIRUS NEURAMINIDASE INHIBITOR, PREPARATION METHOD THEREFOR AND APPLICATION THEREOF
Document Type and Number:
WIPO Patent Application WO/2021/179513
Kind Code:
A1
Abstract:
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.
Inventors:
LI XUEBING (CN)
LV XUN (CN)
WANG PENGFEI (CN)
CHEN JIANZHONG (CN)
LV XUN (CN)
WANG PENGFEI (CN)
CHEN JIANZHONG (CN)
Application Number:
PCT/CN2020/105256
Publication Date:
September 16, 2021
Filing Date:
July 28, 2020
Export Citation:
Assignee:
INST MICROBIOLOGY CAS (CN)
International Classes:
C07J41/00; A61K31/58; A61P31/16
Foreign References:
| CN111233962A | 2020-06-05 | |||
| CN103068378A | 2013-04-24 | |||
| CN103819665A | 2014-05-28 |
Other References:
BAI YUNHAO: "An Influenza Inhibitor Zanzmivir Modified with Cholesterol", MASTER THESIS, 1 December 2016 (2016-12-01), CN, pages 1 - 56, XP009530309
KAZUYUKI KUBOTA, TOSHIMI MIZUKOSHI , HIROSHI MIYANO: "A new approach for quantitative analysis of L -phenylalanine using a novel semi-sandwich immunometric assay", ANALYTICAL AND BIOANALYTICAL CHEMISTRY, vol. 405, no. 25, 1 October 2013 (2013-10-01), DE, pages 8093 - 8103, XP055845086, ISSN: 1618-2642, DOI: 10.1007/s00216-013-7081-0
KAZUYUKI KUBOTA, TOSHIMI MIZUKOSHI , HIROSHI MIYANO: "A new approach for quantitative analysis of L -phenylalanine using a novel semi-sandwich immunometric assay", ANALYTICAL AND BIOANALYTICAL CHEMISTRY, vol. 405, no. 25, 1 October 2013 (2013-10-01), DE, pages 8093 - 8103, XP055845086, ISSN: 1618-2642, DOI: 10.1007/s00216-013-7081-0
Attorney, Agent or Firm:
HAIHONG JIACHENG INTELLECTUAL PROPERTY & PARTNERS (CN)
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