专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明申请

WO2018082723A1 AMINOOXYLIPIDS FOR THE CONSTRUCTION OF SELF-ASSEMBLING LIPOSOMAL SYSTEMS ENABLING THEIR SUBSEQUENT MODIFICATION BY BIOLOGICALLY FUNCTIONAL MOLECULES 审中-公开
标题翻译：用于构建自组装脂质体系统的氨基甲酰脂质使其能够通过生物功能分子进行后续修饰
公开(公告)号：WO2018082723A1
公开(公告)日：2018-05-11
申请号：PCT/CZ2017/050054
申请日：2017-11-02
申请人： VYSOKA SKOLA CHEMICKO-TECHNOLOGICKA V PRAZE , VYZKUMNY USTAV VETERINARNIHO LEKARSTVI, V. V. I. , APIGENEX S.R.O.
发明人： LEDVINA, Miroslav , EFFENBERG, Roman , TURANEK, Jaroslav , BARTHELDYOVA, Elissa , DROZ, Ladislav , MASEK, Josef , HUBATKA, Frantisek
IPC分类号： C07C235/08 , A61K9/127 , C07C235/10 , A61K47/50
CPC分类号： C07C235/10 , A61K9/1271 , A61K47/543 , A61K47/61 , A61K47/6835 , A61K47/6911 , A61K47/6913 , C07C235/08
摘要： New aminooxylipids of general formula (I), wherein n 1 = 5-30 and X is polymethylene linker of the general formula (II) where n 2 = 2 -10, or X is polyethylene glycol linker of the general formula (III), wherein n 3 = 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 {(CH 3 ) 3 C-0-(C=0)-HN-(CH 2 ) n -N H 2 , n = 2 -13}, or N -tert- butoxycarbonyl-polyethyleglycoldiamine {(CH 3 ) 3 C-0-(C=0)-HN-(CH 2 ) 2 -[0-(CH 2 )] n -0-(CH 2 ) 2 NH 2 , n = 1-14} with in position C(2) symmetrically branched fatty acids of general formula (IV), wherein n 1 = 5-30, in the presence of condensation reagent, or from acid of general formula (IV) derived acylchloride of general formula (V) wherein n 1 = 5-30, produces N -Boc-aminolipids of general formula (VI), wherein n 1 = 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 n 1 = 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 n 1 = 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).
摘要翻译：通式（I）的新的氨氧基脂类（其中n 1 = 5-30且X是通式（II）的聚亚甲基连接基，其中n 2 = / X =通式（III）的聚乙二醇接头，其中n 3 = 1-14。制备通式（I）的氨氧基脂类的方法，其特征在于N-叔丁氧基羰基 - 多亚甲基二胺{（CH 3）3} （C = O）-HN-（CH 2）n -N 2 H 2，n = 2 -13 }或N'-叔丁氧基羰基 - 聚乙二醇二胺{（CH 3）3 C-O-（C = O）-HN-（ CH <子> 2 ）<子> 2 - [O-（CH <子> 2 ）] <子>名词 -O-（CH <子> （2）对称支链脂肪酸的通式（IV）的化合物，其中n（n）为1或2，其中n （IV）衍生的通式（V）的酰氯中，其中n1 = 5- 30产生通式（VI）的N-Boc-氨基脂质，其中n1 = 5-30，X是通式（II）的聚亚甲基连接体或X 是通式（III）的聚乙二醇接头。通过去核作用将它们转化为通式（VII）的氨基脂质，其中n 1 = 5-30，X是通式（II）的聚亚甲基连接基或X是通式（III）。通过它们在缩合剂存在下与N-叔丁氧羰基氨基氧乙酸缩合，得到通式（VIII）的N-Boc-氨氧基脂类，其中n

IPRDB

热门服务

关于我们

友情链接

联系方式