Title:
CATIONIC LIPID CONTAINING FUNCTIONAL GROUP ON SIDE CHAIN, AND USE THEREOF
Document Type and Number:
WIPO Patent Application WO/2023/126006
Kind Code:
A1
Abstract:
Disclosed are a novel cationic lipid and a PEGylated derivative thereof, and a cationic liposome, cationic liposome nucleic acid pharmaceutical composition, and cationic liposome nucleic acid pharmaceutical composition preparation containing same. Provided in the invention is an ionisable lipid compound with the structure shown in formula (1). The compound is less ionised or electrically neutral at physiological pH, has a greater degree of ionisation under acidic conditions, and has lower systemic toxicity and higher endosomal escape capability; the polar head of the compound has an ionisable tertiary amine group, the side chain may have a functional group, and the tail chain may contain an easily degradable linkage; the cationic liposome containing the compound has higher nucleic acid drug compounding capability and serum stability, no obvious cytotoxicity, and also has high transfection efficiency. Compared with traditional liposomes, the cationic liposome provided in the present invention has higher nucleic acid delivery and transfection efficiency, and can be used as a novel carrier functional reagent in nucleic acid drugs and vaccines.
Inventors:
LIN SHENG (CN)
LIN MINGGUI (CN)
CHEN DANDAN (CN)
WANG AILAN (CN)
LIN CONGMING (CN)
ZHU QI (CN)
WENG WENGUI (CN)
LIU CHAO (CN)
YUAN JINCHUN (CN)
LIN MINGGUI (CN)
CHEN DANDAN (CN)
WANG AILAN (CN)
LIN CONGMING (CN)
ZHU QI (CN)
WENG WENGUI (CN)
LIU CHAO (CN)
YUAN JINCHUN (CN)
Application Number:
PCT/CN2023/070008
Publication Date:
July 06, 2023
Filing Date:
January 01, 2023
Export Citation:
Assignee:
XIAMEN SINOPEG BIOTECH CO LTD (CN)
International Classes:
C07C229/02; A61K31/7088; A61K39/00; A61K47/18; C07C227/08
Domestic Patent References:
| WO2016206540A1 | 2016-12-29 |
Foreign References:
| CN112979483A | 2021-06-18 | |||
| CN104109235A | 2014-10-22 | |||
| US20190167811A1 | 2019-06-06 | |||
| US20100104629A1 | 2010-04-29 | |||
| CN104877127A | 2015-09-02 | |||
| CN106967213A | 2017-07-21 | |||
| CN108530637A | 2018-09-14 | |||
| CN108530617A | 2018-09-14 | |||
| CN113402405A | 2021-09-17 | |||
| CN104530413A | 2015-04-22 | |||
| CN104530415A | 2015-04-22 | |||
| CN104530417A | 2015-04-22 |
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