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    PNA monomer and precursor
    2.
    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。

    Method of making PNA oligomers
    4.
    发明授权
    Method of making PNA oligomers 有权
    制备PNA低聚物的方法

    公开(公告)号：US07179896B2

    公开(公告)日：2007-02-20

    申请号：US11182936

    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： C07H21/02 ,  C07H21/04 ,  C07H21/00

    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，所述功能由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
    5.
    发明授权
    PNA monomer and precursor 有权
    PNA单体和前体

    公开(公告)号：US07411065B2

    公开(公告)日：2008-08-12

    申请号：US11182977

    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： C07D403/06 ,  C07D239/34 ,  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) oglimers 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）激发剂的通式（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是氮或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。

    PNA monomer and precursor
    6.
    发明授权
    PNA monomer and precursor 有权
    PNA单体和前体

    公开(公告)号：US07371860B2

    公开(公告)日：2008-05-13

    申请号：US11183025

    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： C07D413/06 ,  C07D417/06

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

    公开(公告)号：US07022851B2

    公开(公告)日：2006-04-04

    申请号：US10351173

    申请日：2003-01-24

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

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

    IPC分类号： C07D473/18 ,  C07D473/34 ,  C07D239/47 ,  C07D239/54 ,  C07D247/02

    CPC分类号： C07D403/06 ,  C07D473/18 ,  C07D473/30 ,  C07D473/34 ,  C07K14/003 ,  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 R1, R2, R3, R4, R5 is independently H, halogen, C1–C4 alkyl, nitro, nitrile, C1–C4 alkoxy, halogenated C1–C4 alkyl, or halogenated C1–C4 alkoxy, wherein at least one of R1, R3, and R5 is nitro; R6 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.

    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R1，R2，R3，R4， R 5独立地是H，卤素，C 1 -C 4烷基，硝基，腈，C 1 -C 4 烷氧基，卤代C 1 -C 4烷基或卤代C 1 -C 4烷氧基，其中在 R 1，R 3和R 5中的至少一个是硝基; R6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环外氨基功能时，所述功能受到对酸不稳定但对弱至中碱稳定的保护基保护。

    PNA monomer and precursor
    10.
    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。