NITROGEN-BRANCHED NON-LINEAR PEGYLATED LIPID CONTAINING A TERTIARY AMINE AND APPLICATION THEREOF

Abstract: a nitrogen-branched non-linear pegylated lipid containing a tertiary amine, which is represented by the formula (1); wherein, band bare linking bonds or alkylene groups; l, l, land lare linking bonds or divalent linking groups l; rand rare caliphatic hydrocarbon groups or cresidues of aliphatic hydrocarbon derivative, each containing 0-10 heteroatoms; nis a multivalent group of valence y+1 and contains a trivalent nitrogen-atom branching core connected to l; y is 2, 3, 4, 5, 6, 7, 8, 9, or ≥10; xpeg are polyethylene glycol components. compared with linear pegylated lipids, the nitrogen-branched pegylated lipid herein can realize better surface modification of lnp. the present invention also provides a lipid pharmaceutical composition and its formulation containing the pegylated lipid, which can enhance the targeting ability of drugs and improve the transfection efficiency of nucleic acid drugs.

Inventor(s): Wengui WENG, Chao LIU, Dandan CHEN, Sheng LIN, Ailan WANG, Guohua WEI, Congming LIN, Qi ZHU

CPC Classification: A61K9/1272 (PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms ; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles ; soap compositions ))

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