Title:
NITROGEN-BRANCHED NONLINEAR PEGYLATED LIPID CONTAINING TERTIARY AMINE AND USE THEREOF
Document Type and Number:
WIPO Patent Application WO/2023/198085
Kind Code:
A1
Abstract:
Disclosed in the present invention is a nitrogen-branched nonlinear PEGylated lipid containing a tertiary amine as shown in formula (1), wherein B1 and B2 are linking bonds or alkylidene, L1, L2, Ld and Lx are linking bonds or divalent linking groups L, R1 and R2 are C1-50 aliphatic hydrocarbon groups or C1-50 aliphatic hydrocarbon derivative residues containing 0-10 heteroatoms, Ncore is a multivalent group with a valence of y+1 and a trivalent-nitrogen-atom-branched core linked to Ld, y is 2, 3, 4, 5, 6, 7, 8, 9 or y ≥ 10, and XPEG is a polyethylene glycol component. Compared with a linear PEGylated lipid, the nitrogen-branched PEGylated lipid provided by the present invention can achieve better surface modification of LNP. Further provided in the present invention are a lipid-drug composition containing the PEGylated lipid and a preparation thereof, which can improve the targeting property of a drug and the transfection efficiency of a nucleic acid-based drug.
Inventors:
WENG WENGUI (CN)
LIU CHAO (CN)
CHEN DANDAN (CN)
LIN SHENG (CN)
WANG AILAN (CN)
WEI GUOHUA (CN)
LIN CONGMING (CN)
ZHU QI (CN)
LIU CHAO (CN)
CHEN DANDAN (CN)
LIN SHENG (CN)
WANG AILAN (CN)
WEI GUOHUA (CN)
LIN CONGMING (CN)
ZHU QI (CN)
Application Number:
PCT/CN2023/087702
Publication Date:
October 19, 2023
Filing Date:
April 11, 2023
Export Citation:
Assignee:
XIAMEN SINOPEG BIOTECH CO LTD (CN)
International Classes:
C08G65/00; A61K9/127; A61K47/60; C07C235/10
Foreign References:
| CN104530417A | 2015-04-22 | |||
| CN112694608A | 2021-04-23 | |||
| AU2014200910A1 | 2014-03-13 | |||
| CN104109235A | 2014-10-22 | |||
| CN104530415A | 2015-04-22 | |||
| CN104725628A | 2015-06-24 | |||
| CN108530617A | 2018-09-14 | |||
| CN110591079A | 2019-12-20 | |||
| CN113429559A | 2021-09-24 | |||
| US20050180946A1 | 2005-08-18 | |||
| US20140200257A1 | 2014-07-17 |
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