首页> 外国专利> OLIGO-GUANIDINES BASED CELLULAR TRANSPORTER COMPRISING HETEROCYCLIC RINGS WITH HYDROPHOBIC AND/OR LIPOPHILIC GROUPS AT N-TERMINAL FOR EFFECTIVE DELIVERY OF NONPENETRABLE CARGOS IN-VITRO AND IN-VIVO

OLIGO-GUANIDINES BASED CELLULAR TRANSPORTER COMPRISING HETEROCYCLIC RINGS WITH HYDROPHOBIC AND/OR LIPOPHILIC GROUPS AT N-TERMINAL FOR EFFECTIVE DELIVERY OF NONPENETRABLE CARGOS IN-VITRO AND IN-VIVO

机译:基于寡聚寡核苷酸的细胞转运体,在N端包含具有疏水和/或脂族基团的杂环,可有效地体内和体外递送不可渗透的货物

摘要

Oligo-guanidines based cellular transporter are provided comprising heterocyclic rings including 4-aminopiperidine, piperazine, morpholine having at least one N-terminal based heterocyclic ring or at least one O-heteroatom based heterocyclic ring tailored with hydrophobic and/or lipophilic group and related compounds adapted as cell penetrating agents/ carriers, and also relates to its method of preparation. Said oligo-guanidines are adapted as effective molecular transporters for transport and/or delivery of therapeutics, therapeutic candidates, probes, or other molecules of interest across biological barriers including oligonucleotides. Advantageously, said oligo-guanidines are capable of being internalized into cells (in-vitro and in-vivo) with enhanced cellular uptake in nanomolar concentration.
机译:提供了基于寡胍的细胞转运蛋白,其包含杂环,所述杂环包括4-氨基哌啶,哌嗪,具有至少一个基于疏水性和/或亲脂性基团的N-末端杂环或至少一个O-杂原子的杂环的吗啉和相关化合物用作细胞穿透剂/载体的化合物,还涉及其制备方法。所述寡胍适于作为有效的分子转运蛋白,用于跨生物屏障(包括寡核苷酸)转运和/或递送治疗剂,候选治疗剂,探针或其他目的分子。有利地,所述寡胍能够以纳摩尔浓度增加的细胞摄取而被内在化成细胞(体外和体内)。

著录项

  • 公开/公告号IN2015KO01328A

    专利类型

  • 公开/公告日2017-12-01

    原文格式PDF

  • 申请/专利权人

    申请/专利号IN1328/KOL/2015

  • 申请日2015-12-23

  • 分类号C12P21/06;

  • 国家 IN

  • 入库时间 2022-08-21 12:52:21

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