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首页> 外国专利> AMINOOXYLIPIDS FOR THE CONSTRUCTION OF SELF-ASSEMBLING LIPOSOMAL SYSTEMS ENABLING THEIR SUBSEQUENT MODIFICATION BY BIOLOGICALLY FUNCTIONAL MOLECULES

AMINOOXYLIPIDS FOR THE CONSTRUCTION OF SELF-ASSEMBLING LIPOSOMAL SYSTEMS ENABLING THEIR SUBSEQUENT MODIFICATION BY BIOLOGICALLY FUNCTIONAL MOLECULES

机译：用于构建自组装脂质体体系的氨基氧化磷脂，可以通过生物学功能分子进行后续改性

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New aminooxylipids of general formula (I), wherein n1 = 5-30 and X is polymethylene linker of the general formula (II) where n2 = 2 -10, or X is polyethylene glycol linker of the general formula (III), wherein n3 = 1-14, are provided. A method of preparation of the aminooxylipids of general formula (I) characterized in that the acylation of N-tert-butoxycarbonyl-polymethylenediamine {(CH3)3C-0-(C=0)-HN-(CH2)n-N H2, n = 2 -13}, or N-tert- butoxycarbonyl-polyethyleglycoldiamine {(CH3)3C-0-(C=0)-HN-(CH2)2-[0-(CH2)]n-0-(CH2)2NH2, n = 1-14} with in position C(2) symmetrically branched fatty acids of general formula (IV), wherein n1 = 5-30, in the presence of condensation reagent, or from acid of general formula (IV) derived acylchloride of general formula (V) wherein n1 = 5-30, produces N-Boc-aminolipids of general formula (VI), wherein n1 = 5-30 a X is polymethylene linker of the general formula (II) or X is polyethylene glycol linker of the general formula (III). These are converted by debocylation to aminolipids of general formula (VII), wherein n1 = 5-30 and X is polymethylene linker of the general formula (II) or X is polyethylene glycol linker of the general formula (III). By their condensation with N-terf-butoxycarbonyl-aminooxyacetic acid in the presence of condensation reagent, N-Boc-aminooxylipids of general formula (VIII), where in n1 = 5- 30 and X is polymethylene linker of the general formula (II) or X is polyethylene glycol linker of the general formula (III), are obtained, which by debocylation afford aminooxylipids of general formula (I). Acylchlorides of general formula (V) are prepared by reaction of acid of general formula (IV) with oxalylchloride in the presence of catalytic amount of N, N-dimethylformamide in organic aprotic solvent. The use of nontoxic aminooxylipids of the general formula I for construction of nontoxic self-assembly liposomal carriers of therapeutics presenting aminooxy groups and so-called "post-liposomal" modification of these carriers with biologically functional molecules using oxime ligation technique (binding counterparts: aminooxy group and aldehyde or ketone group).
机译：通式（I）的新氨氧化脂，其中N1 = 5-30和X是通式（II）的聚亚甲基接头，其中N 2 = 2 -10或X是通式（III）的聚乙二醇接头，其中N3提供= 1-14。一种制备通式（I）的氨基氧化磷脂的方法，其特征在于，N-叔丁氧基羰基 - 聚甲基二甲基二胺的酰化{（CH 3）3C-0-（C = 0）-HN-（CH2）NN H2，n = 2 -13}，或N-叔丁氧基羰基 - 聚乙基丙烯酸胺{（CH 3）3 C-0-（C = 0）-HN-（CH 2）2-[0-（CH 2）] N-0-（CH 2）2NH2， n = 1-14}与位置C（2）对称支链通式（IV）的脂肪酸，其中在缩合试剂存在下的N1 = 5-30，或来自通式（IV）的酸衍生的酰基氯化物其中N1 = 5-30的通式（V）产生通式（VI）的N-Boc-氨基吡啶，其中N1 = 5-30A X是通式（II）的聚亚甲基接头，或X是聚乙二醇接头通式（III）。这些通过Debocynation转化为通式（VII）的氨基吡啶，其中N1 = 5-30和X是通式（II）的聚亚甲基接头，或X是通式（III）的聚乙二醇接头。通过在缩合试剂存在下与N-Terf-丁氧基羰基氨基氧基乙酸的缩合，通式（VIII）的N-BOC-氨基氧化哌啶，其中在N1 = 5-30和X中是通式（II）的聚亚甲基接头或X是通式（III）的聚乙二醇接头，得到通式（I）的氨基氧化氨基氧化剂。通式（V）的酰氯是通过在有机非质子溶剂中的N，N-二甲基甲酰胺的催化量N，N-二甲基甲酰胺存在下与草氯化乙酰丙烷反应制备。使用Nontoxic氨基氧化哌脂的通式I用于施用治疗剂的无毒自组装脂质体载体，其具有使用肟连接技术的生物功能分子的这些载体的氨基氧基和所谓的“后脂质体”改变（结合对应物：氨基氧基组和醛或酮组）。

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