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Lipides d'acides aminés et utilisations associées
专利权人:
Marina Biotech; Inc.
发明人:
申请号:
EP12158867.7
公开号:
EP2494993A3
申请日:
2008.05.02
申请国别(地区):
EP
年份:
2012
代理人:
摘要:
The present invention provides a compound comprising the structure shown in Formula I for use in delivering a therapeutic nucleic acid, one or more drug agents, or a biologically active agent to a cell,         R3-(C=O)-Xaa-Z-R4     Formula IwhereinXaa is histidine, 1-methylhistidine, pyridylalanine, lysine, arginine, homoarginine, nor-norarginine, ornithine, homolysine, asparagine, N ethylasparagine, glutamine, 4-aminophenylalanine, and nor-arginine, or an N-methylated version thereof; R3 is independently a lipophilic tail derived from a naturally-occurring or synthetic lipid, phospholipid, glycolipid, triacylglycerol, glycerophospholipid, sphingolipid, ceramide, sphingomyelin, cerebroside, or ganglioside, wherein the tail may contain a steroid; or a substituted or unsubstituted C(3-22)alkyl, C(6-12)cycloalkyl, C(6-12)cycloalkyl-C(3-22)alkyl, C(3-22)alkenyl, C(3-22)alkynyl, C(3-22)alkoxy, or C(6-12)alkoxy-C(3-22)alkyl;R4 is independently a lipophilic tail derived from a naturally-occurring or synthetic lipid, phospholipid, glycolipid, triacylglycerol, glycerophospholipid, sphingolipid, ceramide, sphingomyelin, cerebroside, or ganglioside, wherein the tail may contain a steroid; or a substituted or unsubstituted C(3-22)alkyl, C(6-12)cycloalkyl, C(6-12)cycloalkyl-C(3-22)alkyl, C(3-22)alkenyl, C(3-22)alkynyl, C(3-22)alkoxy, or C(6-12)alkoxy-C(3-22)alkyl;wherein both R3 and R4 are lipophilic tails; andZ is NH, O, S, -CH2S-, -CH2S(O)-, or an organic linker consisting of 1-40 atoms selected from hydrogen, carbon, oxygen, nitrogen, and sulfur atoms;and salts thereof.
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