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POLYMERIZABLE COMPOUND, COMPOUND, AND METHOD FOR PRODUCING BORANOPHOSPHATE OLIGOMER

外国特許コード F190009680
整理番号 S2017-0112-C0
掲載日 2019年1月22日
出願国 世界知的所有権機関(WIPO)
国際出願番号 2017JP040469
国際公開番号 WO 2018088491
国際出願日 平成29年11月9日(2017.11.9)
国際公開日 平成30年5月17日(2018.5.17)
優先権データ
  • 特願2016-221656 (2016.11.14) JP
発明の名称 (英語) POLYMERIZABLE COMPOUND, COMPOUND, AND METHOD FOR PRODUCING BORANOPHOSPHATE OLIGOMER
発明の概要(英語) Provided is a polymerizable compound represented by formula A-1 and A-2. In formula A-1 or A-2: R1 represents an electron donor group; n represents an integer of 1 to 5; R2 represents a hydrogen atom, a halogen atom, or -ORO; RO represents a hydrogen atom, an alkyl group, or a hydroxyl group protecting group; R3 represents a hydrogen atom or a hydroxyl group protecting group; and X represents a structure represented by any of formulas B-1 through B-5.
従来技術、競合技術の概要(英語) BACKGROUND ART
Having a base sequence complementary to target nucleic acid is an antisense molecule, a target nucleic acid that is complementary to the double strand formation, from the target nucleic acid of the protein production can be inhibited.Is selected as the target nucleic acid when the disease-associated genes, antisense molecules, disease-associated gene for direct readout, as a medicament useful in gene therapy has been attracting attention.
Antisense molecules (nucleic acid oligomers) is, effectively inhibiting the generation of the target protein from the viewpoint of mainly, cell membrane permeability, nuclease resistance, the body (for example, environment pH7.4) chemical stability, and only a specific base sequence to form a stable duplex nature is obtained.Antisense molecules include, for example, phosphoric acid diester structure of nucleic acid oligomers, at least a portion of an oligomer having a structure in which the substituted phosphorothioate linkages, phosphodiester structure of nucleic acid oligomers, borano at least a portion of an oligomer having a structure substituted by a structure (hereinafter, referred to as' ') and the like are known, many extensive study to this example and, are in practical use as a medicament.Boranophosphates structure, phosphoric acid diester structure, one of the non-bridging oxygen atom of the amino groups of the borazine (- BH3) replaced by the coupling means. is, increased resistance to nucleases, RNAi (RNA interference) has a high activity, high affinity for RNA than DNA, protein low nonspecific interactions, neutron capture therapy (BNCT) boron also be applied to have the advantage.
The method of manufacturing the conventional , J.AM.Chem.Soc. 1990,112,9000.,Tetrahedron Lett. 1997,38,4957.,J.AM.Chem.Soc. 1998,120,9417.,Tetrahedron Lett. 1998,39,3899.,T.Angew.Chem.INt.Ed. 2009,48,496-499,T.RSC adv. 2015,5,2392-2395, and, of Tetrahedron Lett. 2012,53,4361-4364. and the like.
  • 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
  • TOKYO UNIVERSITY OF SCIENCE FOUNDATION
  • 発明者(英語)
  • WADA, Takeshi
  • SAITO, Tatsuya
  • ISHII, Yuka
  • NUKAGA, Yohei
国際特許分類(IPC)
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