Title:
PHENYLALANINE-AMIDATED NUCLEOTIDE DERIVATIVE, PREPARATION METHOD THEREFOR AND APPLICATION THEREOF
Document Type and Number:
WIPO Patent Application WO/2021/098379
Kind Code:
A1
Abstract:
Provided are a phenylalanine-amidated nucleotide derivative, a preparation method therefor and an application thereof. In the present invention, a compound is formed by binding halogenated phenylalanine to an amino group of an amino-containing nucleoside compound, phosphorylation is carried out at the same time, and a phosphate ester and a phosphamide prodrug are used to promote absorption, thus avoiding a rate-limiting step of monophosphate synthesis, and reducing or avoiding the effect of nucleoside deaminase so as to enhance drug efficacy. Meanwhile, the halogenated phenylalanine has the synergistic effect of inhibiting protein synthesis, and has the effects of increasing bioavailability, improving drug efficacy, and reducing drug resistance in anti-tumor and anti-hepatitis B virus aspects.
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Inventors:
WANG WEI (CN)
LU YONGZHANG (CN)
TAN JINHUI (CN)
LU YONGZHANG (CN)
TAN JINHUI (CN)
Application Number:
PCT/CN2020/118025
Publication Date:
May 27, 2021
Filing Date:
September 27, 2020
Export Citation:
Assignee:
GUANGDONG ZHONGKE MEDICINE R&D LTD (CN)
International Classes:
C07H19/10; A61P1/18; A61P31/20; A61P35/00; C07F9/6512; C07F9/6558; C07F9/6561; C07H19/207
Domestic Patent References:
| WO2017207986A1 | 2017-12-07 |
Foreign References:
| CN107698639A | 2018-02-16 | |||
| CN110845560A | 2020-02-28 | |||
| CN102115485A | 2011-07-06 | |||
| CN101525361A | 2009-09-09 |
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