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    Method of making PNA oligomers
    4.
    发明申请
    Method of making PNA oligomers 有权
    制备PNA低聚物的方法

    公开(公告)号：US20060003374A1

    公开(公告)日：2006-01-05

    申请号：US11182936

    申请日：2005-07-15

    申请人： Sung Kim ,  Hyunil Lee ,  Jong Lim ,  Hoon Choi ,  Jae Jeon ,  Sang Ahn ,  Sung Lee ,  Won Yoon

    发明人： Sung Kim ,  Hyunil Lee ,  Jong Lim ,  Hoon Choi ,  Jae Jeon ,  Sang Ahn ,  Sung Lee ,  Won Yoon

    IPC分类号： C12Q1/68 ,  C07D473/02 ,  C07D473/14 ,  C07D43/14

    CPC分类号： C07D417/04 ,  C07B2200/11 ,  C07D277/80 ,  C07D417/12 ,  C07D417/14 ,  Y02P20/55

    摘要： 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 nitrogen or C—R′; J is sulfur or oxygen; R′, R1, R2, R3, R4 is independently H, halogen, alkyl, nitro, nitrile, alkoxy, halogenated alkyl, halogenated alkoxy, phenyl or halogenated phenyl, R5 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.

    摘要翻译： 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为氮或C-R' ; J为硫或氧; R'，R 1，R 2，R 3，R 4独立地是H，卤素，烷基，硝基，腈，烷氧基，卤代烷基，卤代烷氧基，苯基或卤代苯基，R 5是H或被保护或未被保护的天然或非天然α- 氨基酸; 并且B是天然或非天然核碱基，其中当所述核碱基具有环外氨基功能时，所述功能受到在硫醇存在下对酸不稳定但对弱至中碱稳定的保护基保护。

    PNA monomer and precursor
    6.
    发明申请
    PNA monomer and precursor 有权
    PNA单体和前体

    公开(公告)号：US20050250786A1

    公开(公告)日：2005-11-10

    申请号：US11183025

    申请日：2005-07-15

    申请人： Sung Kim ,  Hyunil Lee ,  Jong Lim ,  Hoon Choi ,  Jae Jeon ,  Sahn Ahn ,  Sung Lee ,  Won Yoon

    发明人： Sung Kim ,  Hyunil Lee ,  Jong Lim ,  Hoon Choi ,  Jae Jeon ,  Sahn Ahn ,  Sung Lee ,  Won Yoon

    IPC分类号： C12N15/09 ,  A61K31/513 ,  A61K31/52 ,  C07D277/80 ,  C07D405/12 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14 ,  C07D473/02 ,  C07D473/18 ,  C07D473/32 ,  C07D473/34 ,  C07D43/14

    CPC分类号： C07D417/04 ,  C07B2200/11 ,  C07D277/80 ,  C07D417/12 ,  C07D417/14 ,  Y02P20/55

    摘要： 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 nitrogen or C—R′; J is sulfur or oxygen; R′, R1, R2, R3, R4 is independently H, halogen, alkyl, nitro, nitrite, alkoxy, halogenated alkyl, halogenated alkoxy, phenyl or halogenated phenyl, R5 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.

    摘要翻译： 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为氮或C-R' ; J为硫或氧; R'，R 1，R 2，R 3，R 4独立地为H，卤素，烷基，硝基，亚硝酸根，烷氧基，卤代烷基，卤代烷氧基，苯基或卤代苯基，R 5为H或保护或未保护的天然或非天然α- 氨基酸; 并且B是天然或非天然核碱基，其中当所述核碱基具有环外氨基功能时，所述功能受到在硫醇存在下对酸不稳定但对弱至中碱稳定的保护基保护。

    PNA monomer and precursor
    7.
    发明申请
    PNA monomer and precursor 有权
    PNA单体和前体

    公开(公告)号：US20050026930A1

    公开(公告)日：2005-02-03

    申请号：US10819769

    申请日：2004-04-06

    申请人： Sung Kim ,  Hyunil Lee ,  Jong Lim ,  Sung Lee

    发明人： Sung Kim ,  Hyunil Lee ,  Jong Lim ,  Sung Lee

    IPC分类号： A61K31/496 ,  C07D263/46 ,  C07D271/10 ,  C07D271/113 ,  C07D413/12 ,  C07D417/02 ,  C07D417/12

    CPC分类号： C07D271/113 ,  C07D263/46 ,  C07D413/12 ,  C07D417/12 ,  Y02P20/55

    摘要： 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.

    摘要翻译： 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A1，A2，A3，A4，A5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 -C 4烷氧基，卤代（如F，Cl，Br和I）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或被保护或未被保护的一侧 天然或非天然α-氨基酸的链; 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，所述功能受到对酸不稳定的保护基保护，但在弱碱性至中等碱基中稳定 存在硫醇。

    PNA monomer and precursor
    8.
    发明授权
    PNA monomer and precursor 有权
    PNA单体和前体

    公开(公告)号：US07371859B2

    公开(公告)日：2008-05-13

    申请号：US11182935

    申请日：2005-07-15

    申请人： Sung Kee Kim ,  Hyunil Lee ,  Jong Chan Lim ,  Hoon Choi ,  Jae Hoon Jeon ,  Sang Youl Ahn ,  Sung Hee Lee ,  Won Jun Yoon

    发明人： Sung Kee Kim ,  Hyunil Lee ,  Jong Chan Lim ,  Hoon Choi ,  Jae Hoon Jeon ,  Sang Youl Ahn ,  Sung Hee Lee ,  Won Jun Yoon

    IPC分类号： C07D405/14 ,  C07D407/14 ,  C07D409/14 ,  C07D417/14 ,  C07D239/54 ,  C07D241/18

    CPC分类号： C07D417/04 ,  C07B2200/11 ,  C07D277/80 ,  C07D417/12 ,  C07D417/14 ,  Y02P20/55

    摘要： 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 nitrogen or C—R′; J is sulfur or oxygen; R′, R1, R2, R3, R4 is independently H, halogen, alkyl, nitro, nitrile, alkoxy, halogenated alkyl, halogenated alkoxy, phenyl or halogenated phenyl, R5 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.

    摘要翻译： 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为氮或C-R' ; J为硫或氧; R'，R 1，R 2，R 3，R 4独立地为H，卤素，烷基，硝基，腈，烷氧基，卤代烷基，卤代烷氧基，苯基或卤代苯基，R 5为H或保护或未保护的天然或非天然α- 氨基酸; 并且B是天然或非天然核碱基，其中当所述核碱基具有环外氨基功能时，所述功能受到在硫醇存在下对酸不稳定但对弱至中碱稳定的保护基保护。