TOP > 外国特許検索 > OLIGONUCLEOTIDE DERIVATIVE, OLIGONUCLEOTIDE CONSTRUCT USING SAME, AND METHODS FOR PRODUCING THESE

OLIGONUCLEOTIDE DERIVATIVE, OLIGONUCLEOTIDE CONSTRUCT USING SAME, AND METHODS FOR PRODUCING THESE

外国特許コード F170008931
整理番号 (S2015-0845-N0)
掲載日 2017年1月19日
出願国 世界知的所有権機関(WIPO)
国際出願番号 2016JP059398
国際公開番号 WO 2016152980
国際出願日 平成28年3月24日(2016.3.24)
国際公開日 平成28年9月29日(2016.9.29)
優先権データ
  • 特願2015-060689 (2015.3.24) JP
発明の名称 (英語) OLIGONUCLEOTIDE DERIVATIVE, OLIGONUCLEOTIDE CONSTRUCT USING SAME, AND METHODS FOR PRODUCING THESE
発明の概要(英語) [Problem] To provide a novel oligonucleotide derivative that is easy to synthesize and can be introduced into cells without using a lipofection reagent.
[Solution] The oligonucleotide derivative of the present invention is shown by, e.g., (1). This derivative is considered to bind an aminoglycan moiety to a ligand on the surface of a cell and be introduced into the cell, and can be expected to have selective drug delivery functions. In the formula, R1 and R2 each independently represent a hydrogen or phosphate group; a, b, and c independently represent integers of 0 or higher, at least one of a, b, and c being 1 or higher; A and B independently represent optionally modified oligonucleotides having a combined chain length of A and B of 3 or higher. However, A and B do not include hydroxyl groups at the 3' end and 5' end of the oligonucleotide. Furthermore, S in the formula indicates a sugar substituent, a peptide chain, or a tocopherol binding group. Additionally, an alkyl group may be bonded, in lieu of hydrogen, to the benzene ring in the formula.
従来技術、競合技術の概要(英語) BACKGROUND ART
In recent years, various substrates such as DNA or RNA oligonucleotide treatment, such as a diagnosis applications has been to be used.For example, a nucleic acid of interest as a technology, interference RNA (RNAi) using, of a specific gene knock-down method can be used.RNAi is, by the action of the double-stranded RNA (dsRNA), such that sequences homologous to a phenomenon in which the action of the genes is suppressed.The medicament is a nucleic acid using RNAi, next generation as a therapeutic agent, are great expectations.
On the other hand, the chemical modification of oligonucleotide, are not present in the native, given a new function studies have also been carried out.The present inventors, ethynyl groups are introduced to the end of the oligonucleotide, further, the ethynyl groups, a benzene ring using the click reaction was new substituent modified to develop a technique (patent document 1).In addition, in this technique the resulting artificial oligonucleotides, natural type oligonucleotide is higher than the nuclease are resistant, hardly degraded inside the cell the result is obtained.
And have a negative charge at the nucleic acid itself is however, not able to pass through the cell membrane.For this reason, in a nucleic acid drug, such as a drug delivery system (DDS) nucleotides to pass through the cell membrane is required.The current, as a method for introducing nucleotides into cells, using liposomes are ribonucleic transfection method has been developed.The method, having a negative charge around DNA, cationic liposomes with a positive charge to form a complex that has bound, phenomenon from the cell surface by endocytosis into the cell DNA is incorporated into the method and the like.
However, lipofection reagent is used in the lipofection method, and toxicity to the liver and the kidney, has been a problem.In addition, lipofection method, and using a simple endocytosis DDS, is a lack of selectivity for the cells.
In order to solve such a problem, the oligonucleotide 3' - terminus of the peptide chain is introduced into the asialoglycoprotein, the asialoglycoprotein receptor (ASGPR) that introducing into the cell through, chemically modified oligonucleotides have been developed (Patent Document 2, 3).However, in this method, such as shown in Fig. 4, three asialoglycoprotein - peptide chain and a complex has a chemical structure, in order to synthesize a complex operation is required.
  • 出願人(英語)
  • ※2012年7月以前掲載分については米国以外のすべての指定国
  • GIFU UNIVERSITY
  • 発明者(英語)
  • KITADE YUKIO
  • SHIBATA AYA
国際特許分類(IPC)
指定国 National States: AE AG AL AM AO AT AU AZ BA BB BG BH BN BR BW BY BZ CA CH CL CN CO CR CU CZ DE DK DM DO DZ EC EE EG ES FI GB GD GE GH GM GT HN HR HU ID IL IN IR IS JP KE KG KN KP KR KZ LA LC LK LR LS LU LY MA MD ME MG MK MN MW MX MY MZ NA NG NI NO NZ OM PA PE PG PH PL PT QA RO RS RU RW SA SC SD SE SG SK SL SM ST SV SY TH TJ TM TN TR TT TZ UA UG US UZ VC VN ZA ZM ZW
ARIPO: BW GH GM KE LR LS MW MZ NA RW SD SL SZ TZ UG ZM ZW
EAPO: AM AZ BY KG KZ RU TJ TM
EPO: AL AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HR HU IE IS IT LT LU LV MC MK MT NL NO PL PT RO RS SE SI SK SM TR
OAPI: BF BJ CF CG CI CM GA GN GQ GW KM ML MR NE SN ST TD TG
岐阜大学産官学連携推進本部では、岐阜大学における知的財産の創出・管理・活用のマネジメントをしています。上記の特許・技術に関心のある方は、下記問い合わせ先に整理番号とともにご相談下さい。

PAGE TOP

close
close
close
close
close
close