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    • 8. 发明授权
    • PNA monomer and precursor
    • PNA单体和前体
    • US07211668B2
    • 2007-05-01
    • US10819769
    • 2004-04-06
    • Sung Kee KimHyunil LeeJong Chan LimSung Hee Lee
    • Sung Kee KimHyunil LeeJong Chan LimSung Hee Lee
    • C07D473/34C07D473/30C07D473/18C07D239/47C07D239/54
    • C07D271/113C07D263/46C07D413/12C07D417/12Y02P20/55
    • This application relates to monomers of the general formula (I) for the preparation of PNA (peptide nucleic acid) oligomers and provides method for the synthesis of both predefined sequence PNA oligomers and random sequence PNA oligomers: wherein E is sulfur or oxygen; J is nitrogen or C—R′; R1, R′ is independently H, halogen, alkyl, nitro, nitrile, alkoxy, halogenated alkyl, halogenated alkoxy or a functional group having one of following general formulae: wherein A1, A2, A3, A4, A5, is independently selected from H, halogen such as F, Cl, Br or I, CF3, alkyl, preferably C1–C4 alkyl, nitro, nitrile, alkoxy, preferably C1–C4 alkoxy, halogenated (such as F, Cl, Br and I) alkyl, preferably halogenated C1–C4 alkyl, halogenated (such as F, Cl, Br and I) alkoxy, preferably halogenated C1–C4 alkoxy, phenyl, and halogenated (such as F, Cl, Br and I phenyl; R2 is H or protected or unprotected side chain of natural or unnatural α-amino acid; and B is a natural or unnatural nucleobase, wherein when said nucleobase has an exocyclic amino function, said function is protected by protecting group which is labile to acids but stable to weak to medium bases in the presence of thiol.
    • 本申请涉及用于制备PNA(肽核酸)寡聚体的通式(I)的单体,并提供合成预定义的序列PNA寡聚体和随机序列PNA寡聚体的方法:其中E为硫或氧; J为氮或C-R'; R1,R'独立地为H,卤素,烷基,硝基,腈,烷氧基,卤代烷基,卤代烷氧基或具有以下通式之一的官能团:其中A 1, A 3,A 4,A 5 H独立地选自H,卤素如F,Cl,Br或 I,CF 3,烷基,优选C 1 -C 4烷基,硝基,腈,烷氧基,优选C 1〜 卤代(如F,Cl,Br和I)烷基,优选卤代C 1 -C 4烷基,C 1 -C 4烷基, ,卤代(如F,Cl,Br和I)烷氧基,优选卤代C 1 -C 4烷氧基,苯基和卤代(如F,Cl,Br 和I苯基; R2是H或天然或非天然α-氨基酸的保护或未保护的侧链; B是天然或非天然核碱基,其中当所述核碱基具有外来氨基功能时,所述功能受保护基团 不稳定酸,但稳定 在硫醇存在下为弱至中等碱。
    • 10. 发明申请
    • Synthesis of Peptide Nucleic Acids Conjugated with Amino Acids and Their Application
    • 氨基酸共轭肽核酸的合成及其应用
    • US20110014715A1
    • 2011-01-20
    • US12810453
    • 2009-01-08
    • Hyunil LeeJung Hyun Min
    • Hyunil LeeJung Hyun Min
    • G01N33/48C07K9/00C07C271/06C08G64/00
    • C07H7/00C07K14/003Y10T436/143333
    • This invention relates to a peptide nucleic acid (PNA) oligomer which is conjugated with one or more linear-type amino acid containing a plurality of alkyleneglycols and to a synthesis method thereof. In addition, this invention related to a linear amino acid spacer in a device for detection for detecting a target gene using the PNA oligomers which is fixed on a surface of a functionalized solid support. The linear amino acid spacer contains a plurality of alkyleneglycols and maintains enough space between the solid support and PNA oligomer in the device in order to prevent the interference of the interaction between the PNA oligomer and a target gene. Furthermore, this invention relates to a PNA array, a PNA chip and a gene diagnosis kit whereof sensitivity and specificity are improved by being manufactured with the PNA conjugated with the amino acid spacer.
    • 本发明涉及与含有多个亚烷基二醇的一种或多种线型氨基酸缀合的肽核酸(PNA)寡聚体及其合成方法。 此外,本发明涉及使用固定在官能化固体支持物表面上的PNA低聚物检测靶基因的检测装置中的线性氨基酸间隔物。 线性氨基酸间隔物包含多个亚烷基二醇并且在该装置中的固体支持物和PNA低聚物之间保持足够的空间,以便防止PNA低聚物与靶基因之间的相互作用的干扰。 此外,本发明涉及一种PNA阵列,PNA芯片和基因诊断试剂盒,其通过用氨基酸间隔基缀合的PNA制备灵敏度和特异性。