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系统的氨基氧化磷脂，可以通过生物学功能分子进行后续改性

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摘要

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—O—(C═O)—HN—(CH2)n—NH2, n=2-13}, or N-tert-butoxycarbonyl-polyethyleglycoldiamine {(CH3)3C—O—(C═O)—HN—(CH2)2—[O—(CH2)]n—O—(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.

机译：通式I的新氨基氧化钛合体，其中N1 = 5-30和X是通式II的通式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，其中提供N3 = 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 - 聚甲基二亚胺的酰化酰基化金属{（CH 3）3C-O-（C = O）-HN-（CH 2）N-NH2，N = 2 -13}，或N-叔丁氧基羰基 - 聚乙基丙烯酸胺{（CH 3）3C-O-（C = O）-HN-（CH 2）2-[O-（CH2）] N-O-（CH 2）2NH2，N = 1-14}与位于C（2）对称支链的通式IV，其中N1 = 5-30在缩合试剂存在下，或由通式V的通式IV的酸酸，其中通式V的酰氯，其中N1 = 5-30，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是通式III的聚乙二醇接头。

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公开/公告号US2021292275A1

专利类型
公开/公告日2021-09-23

原文格式PDF
申请/专利权人 VYSOKA SKOLA CHEMICKO-TECHNOLOGICKA V PRAZE;VYZKUMNY USTAV VETERINARNIHO LEKARSTVI V.V.I.;APIGENEX S.R.O.;
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申请/专利号US201716336844
发明设计人 MIROLAV LEDVINA;ROMAN EFFENBERG;JAROSLAV TURANEK;ELISSA BARTHELDYOVA;LADISLAV DROZ;JOSEF MASEK;FRANTISEK HUBATKA;
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申请日2017-11-02
分类号C07C239/20;A61K9/127;A61K47/69;A61K47/68;A61K47/54;A61K47/61;
国家 US
入库时间 2022-08-24 21:13:00

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