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, B1 and B2 are linking bonds or alkylene groups; 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 residues of aliphatic hydrocarbon derivative, each containing 0-10 heteroatoms; Ncore is a multivalent group of valence y+1 and contains a trivalent nitrogen-atom branching core connected to Ld; 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.

Dependencies are inferred from the claim text.