公开(公告)号：US20120101148A1

公开(公告)日：2012-04-26

申请号：US13147189

申请日：2010-01-29

申请人： Akin Aking ,  William Querbes ,  Frances M.P. Wong ,  Joseph R. Dorkin ,  Xiaojun Qin ,  William Cantley ,  Anna Borodovsky ,  Soma De ,  Muthiah Manoharan ,  Muthusamy Jayaraman ,  Kallanthottathil G. Rajeev

发明人： Akin Aking ,  William Querbes ,  Frances M.P. Wong ,  Joseph R. Dorkin ,  Xiaojun Qin ,  William Cantley ,  Anna Borodovsky ,  Soma De ,  Muthiah Manoharan ,  Muthusamy Jayaraman ,  Kallanthottathil G. Rajeev

IPC分类号： A61K31/713 ,  A61P43/00 ,  A61K31/7088 ,  A61K47/42 ,  A61K47/28 ,  A61K31/7105

CPC分类号： A61K48/0008 ,  A61K9/1272

摘要： 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.

摘要翻译： 本发明的特征在于改进的脂质制剂，其包含式（A）的阳离子脂质，中性脂质，固醇和PEG或PEG修饰的脂质，其中R 1和R 2独立地为烷基，烯基或炔基，各自可任选被取代， 并且R 3和R 4独立地为低级烷基或R 3和R 4可以一起形成任选取代的杂环。 在一个实施方案中，R 1和R 2独立地选自油酰基，苯甲酰基，甾烷基，亚油酰基，并且R 3和R 4是甲基。 还公开了靶向脂质和包含这种靶向脂质的特定脂质制剂。