Muthiah Manoharan,Muthusamy Jayaraman,Laxman Eltepu,Kallanthottathil G. Rajeev,David Butler,Jayaprakash K. Narayanannair,Martin Maier
申请号：
MX2011004974
公开号：
MX347860B
申请日:
2009.11.10
申请国别(地区):
MX
年份:
2017
代理人:
摘要：
The present invention provides lipids that are advantageously used in lipid particles for the in vivo delivery of therapeutic agents to cells. In particular, the invention provides lipids having the following structure (I) wherein R1 and R2 are each independently for each occurrence optionally substituted C10-C30 alkyl, optionally substituted C10-C30 alkenyl, optionally substituted C10-C30 alkynyl, optionally substituted C10-C30 acyl, or -linker-ligand； R3 is H, optionally substituted C1-C10 alkyl, optionally substituted C2-C10 alkenyl, optionally substituted C2-C10 alkynyl, alkylhetrocycle, alkylphosphate, alkylphosphorothioate, alkylphosphorodithioate, alkylphosphonates, alkylamines, hydroxyalkyls, ω-aminoalkyls, ω -(substituted)aminoalkyls, ω-phosphoalkyls, ω -thiophosphoalkyls, optionally substituted polyethylene glycol (PEG, mw 100-40K), optionally substituted mPEG (mw 120-40K), heteroaryl, heterocycle, or linker-ligand； E is O, S, N(Q), C(O), N(Q)C(O), C(O)N(Q), (Q)N(CO)O, O(CO)N(Q), S(O), NS(O)2N(Q), S(O)2, N(Q)S(O)2, SS, O=N, aryl, heteroaryl, cyclic or heterocycle； and, Q is H, alkyl, ω-aminoalkyl, ω-(substituted)aminoalky, ω-phosphoalkyl or ω-thiophosphoalkyl.La presente invención se refiere a un lípido que tiene la estructura XXXIII o sales o isómeros del mismo, en donde R1 y R2 son cada uno de manera independiente para cada vez que aparecen alquilo de C10 -C30 opcionalmente sustituido, alquenilo de C10-C30 sustituido； R3 es ?-aminoalquilo, ?-aminoalquilo (substituido), heteroarilo； E es O, S, C(O), N(Q)C(O), C(O)N(Q), (Q)N(CO)O, O(CO)N(Q), S(O), NS(O)2N(Q), S(O)2, N(Q)S(O)2, SS, O=N, arilo, heteroarilo, cíclico o heterociclo； y Q es H, alquilo.
