申请人:Arbutus Biopharma Corporation
公开号:EP3243504A1
公开(公告)日:2017-11-15
The invention features an improved lipid formulation comprising a cationic lipid of formula (A), a neutral lipid, a sterol and a PEG or PEG-modified lipid, where R1 and R2 are independently alkyl, alkenyl or alkynyl, each can be optionally substituted, and R3 and R4 are independently lower alkyl or R3 and R4 can be taken together to form an optionally substituted heterocyclic ring. In one embodiment, R1 and R2 are independently selected from oleoyl, pamitoyl, steroyl, linoleyl and R3 and R4 are methyl. Also disclosed are targeting lipids, and specific lipid formulations comprising such targeting lipids.
该发明涉及一种改进的脂质配方,包括一种带有化学式(A)的阳离子脂质,一种中性脂质,一种固醇和一种PEG或PEG修饰脂质,其中R1和R2分别为烷基,烯基或炔基,每种均可选择性地被取代,R3和R4分别为较低烷基或R3和R4可以一起形成一个可选择性取代的杂环环。在一种实施例中,R1和R2分别选自油酰基,棕榈酰基,硬脂酰基,亚油酰基,R3和R4为甲基。还公开了靶向脂质和包括这种靶向脂质的特定脂质配方。