Title:
AMINO LIPID AND APPLICATION THEREOF
Document Type and Number:
WIPO Patent Application WO/2023/029928
Kind Code:
A1
Abstract:
An amino lipid and an application thereof: using ethenesulfonyl fluoride (ESF), a dual-function electrophile, to build an amine head group and a hydrophobic chain into an amino lipid, fully utilizing the click chemical reaction properties of ESF; in the process of constructing the amino lipid, reaction conditions are mild, protection and deprotection are not needed, and atom economy is high. In vitro and in vivo delivery studies show an excellent ability to deliver nucleic acid into cells. The amino lipid compound is provided with two sulfonamides, and the introduction of the group significantly enhances the stability of lipid nanoparticles and improves the in-vivo cycle time, thereby improving in-vivo delivery efficiency. The preparation method of the amino lipid compound has the advantages of readily available raw materials, mild reaction conditions, good reaction selectivity, high reaction yield, low requirements for instruments and equipment, and simple operations.
Inventors:
ZHA GAOFENG (CN)
PENG XINHUA (CN)
XIA HENG (CN)
PENG XINHUA (CN)
XIA HENG (CN)
Application Number:
PCT/CN2022/111656
Publication Date:
March 09, 2023
Filing Date:
August 11, 2022
Export Citation:
Assignee:
SHENZHEN MAGICRNA BIOTECHNOLOGY CO LTD (CN)
International Classes:
C07C311/32; A61P31/00; A61P35/00; A61P35/02; A61P37/08; A61P39/02; C07C303/02; C07C303/38; C07C309/83; C07D295/13; C07D309/14; C12N15/87
Domestic Patent References:
| WO2021055849A1 | 2021-03-25 |
Foreign References:
| CN113461577A | 2021-10-01 | |||
| CN101346468A | 2009-01-14 | |||
| CN1041361A | 1990-04-18 | |||
| CN109414408A | 2019-03-01 |
Other References:
GAN LIN, OLSON JENNIFER L., RAGSDALE CLIFTON W., YU LUPING: "Poly(β-aminosulfonamides) as gene delivery vectors: synthesis and in vitro screening", CHEMICAL COMMUNICATIONS, ROYAL SOCIETY OF CHEMISTRY, UK, no. 5, 13 September 2007 (2007-09-13), UK , pages 573 - 575, XP093042483, ISSN: 1359-7345, DOI: 10.1039/B714278A
Attorney, Agent or Firm:
SHENZHEN CREATEFORTUNE INTELLECTUAL PROPERTY AGENCY CO., LTD. (CN)
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