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NUCLEOSIDE DERIVATIVE AND USE THEREFOR NEW コモンズ

外国特許コード F180009510
整理番号 (GI-H28-25,S2017-0195-N0)
掲載日 2018年11月2日
出願国 世界知的所有権機関(WIPO)
国際出願番号 2017JP044995
国際公開番号 WO 2018110678
国際出願日 平成29年12月14日(2017.12.14)
国際公開日 平成30年6月21日(2018.6.21)
優先権データ
  • 特願2016-244916 (2016.12.16) JP
発明の名称 (英語) NUCLEOSIDE DERIVATIVE AND USE THEREFOR NEW コモンズ
発明の概要(英語) [Problem] To provide a nucleoside that is more practical for RNA pharmaceuticals and other applications and a use therefor.
[Solution] A nucleoside derivative indicated by formula (1) or (2) or a salt thereof. (In formula (1), R1 indicates a hydrogen atom, a hydroxyl group, a hydroxyl group having a hydrogen atom substituted by an alkyl group or an alkenyl group, or a protected group. In formula (2), X indicates a halogen atom. In formulas (1) and (2), R2 and R4 can be the same or different and indicate a hydrogen atom, a protecting group for a hydroxyl group, a phosphate group, a protected phosphate group, or –P(=0)nR5R6 (n indicates 0 or 1 and R5 and R6 can be the same or different and indicate either a hydrogen atom, a hydroxyl group, a protected hydroxyl group, a thiol group, a protected thiol group, a lower alkoxy group, a cyano lower alkoxy group, an amino group, or a substituted amino group. When n is 1, however, R5 and R6 are never both hydrogen atoms.) R3 indicates NHR7 having a linking group for each (R7 indicating a hydrogen atom, an alkyl group, an alkenyl group, or a protecting group for an amino group), an azide group, an amidino group, or a guanidino group. B indicates a purine-9-yl group, a 2-oxo-pyrimidin-1-yl group, a substituted purine-9-il group, or a substituted 2-oxo-pyrimidin-1-yl group.)
従来技術、競合技術の概要(英語) BACKGROUND ART
Including cancer, gene mutation or gene expression caused by disease or abnormality associated with the known multiple.RNA such as siRNA gene to inhibit expression of the medicament, which is useful for such diseases, said to have excellent pharmaceutical potential.
On the other hand, such as siRNA is, the cell membrane is difficult, prone to degradation by nucleases problem.Further, target selectivity is high, it is difficult to selective transport of the target tissue in a problem.In order to improve this point, such as lipid nanoparticles (LNP) has been studied is the carrier for delivery.In addition, RNA ribose oxycarbonylaminomethyl group is introduced into the modified such as to attempt has also been performed (non-patent document 1-4).
However, in spite of such attempts, even more improvement of the effectiveness of a medicament for the RNA is demanded.Carrier for delivery is also insufficient in various points in addition, also by the modification of such RNA, a sufficient cell membrane permeability, ribonuclease-resistant and the target tissue can be delivered is not met.For this reason, even in the state, such as siRNA that exhibit an excellent pharmaceutical in the original are not.
Is described herein, such as pharmaceutical RNA to be applied to practical use and to provide a nucleoside, and the purpose.
  • 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)
  • UENO YOSHIHITO
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 DJ DK DM DO DZ EC EE EG ES FI GB GD GE GH GM GT HN HR HU ID IL IN IR IS JO JP KE KG KH KN KP KR KW 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
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