公开(公告)号：US06969766B2

公开(公告)日：2005-11-29

申请号：US10424181

申请日：2003-04-25

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： C12N15/09 ,  A61K31/513 ,  A61K31/52 ,  C07D277/80 ,  C07D405/12 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14 ,  C07D473/02 ,  C07D473/18 ,  C07D473/32 ,  C07D473/34 ,  C07D247/02 ,  C07D413/12

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。

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。

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。

公开(公告)号：US07145006B2

公开(公告)日：2006-12-05

申请号：US11183034

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： C07D473/34 ,  C07D473/18 ,  C07D247/02 ,  C07D417/12 ,  C07D413/12

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.

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。

公开(公告)号：US07125994B2

公开(公告)日：2006-10-24

申请号：US11182672

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： C07D473/34 ,  C07D473/18 ,  C07D247/02 ,  C07D417/12 ,  C07D413/12

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.

公开(公告)号：US06284912B1

公开(公告)日：2001-09-04

申请号：US09540597

申请日：2000-03-31

申请人： Bong Chan Kim ,  Sang Yeul Hwang ,  Jong Chan Lim ,  Do Hyun Nam ,  Hyun Ik Shin

发明人： Bong Chan Kim ,  Sang Yeul Hwang ,  Jong Chan Lim ,  Do Hyun Nam ,  Hyun Ik Shin

IPC分类号： C07C25500

CPC分类号： C07C253/16 ,  Y02P20/55 ,  C07C255/57

摘要： The present invention relates to a process for preparing a useful medicinal intermediate represented by the following formula (1): in which, R1, A and n are defined as described in the specification, or its stereoisomer, characterized in that a compound represented by the following formula (2): in which, R, R1, A and n are defined as described in the specification, is reacted with a cyanide in the presence of a nickel catalyst.

摘要翻译： 本发明涉及一种制备由下式（1）表示的有用药物中间体的方法：其中R1，A和n如说明书中所述定义，或其立体异构体，其特征在于，由 下式（2）：其中，R，R1，A和n如说明书所述定义，在镍催化剂存在下与氰化物反应。

公开(公告)号：US20100292471A1

公开(公告)日：2010-11-18

申请号：US12299665

申请日：2007-12-17

申请人： Hee Kyung Park ,  Jong Chan Lim ,  Sung Jin Ha ,  Serka Kim ,  Jae Jin Choi ,  Jung Hyun Min ,  Jin Won Yun

发明人： Hee Kyung Park ,  Jong Chan Lim ,  Sung Jin Ha ,  Serka Kim ,  Jae Jin Choi ,  Jung Hyun Min ,  Jin Won Yun

IPC分类号： C07D473/18

CPC分类号： C07H21/00 ,  C07K14/003

摘要： Disclosed is a PNA oligomer with increased solubility in water and specificity upon hybridization with nucleic acid, which comprises at least one universal base, capable of forming a base pair with natural DNA or RNA bases, incorporated in its base sequence, the base sequence having at least 60% purine bases or at least four contiguous purine bases.

摘要翻译： 公开了一种具有增加的在水中的溶解度和与核酸杂交的特异性的PNA低聚物，该核酸包含至少一个通用碱基，其能够与天然的DNA或RNA碱基形成碱基对，并且其碱基序列具有 至少60％的嘌呤碱基或至少四个相邻的嘌呤碱基。

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。

公开(公告)号：US07211668B2

公开(公告)日：2007-05-01

申请号：US10819769

申请日：2004-04-06

申请人： Sung Kee Kim ,  Hyunil Lee ,  Jong Chan Lim ,  Sung Hee Lee

发明人： Sung Kee Kim ,  Hyunil Lee ,  Jong Chan Lim ,  Sung Hee Lee

IPC分类号： C07D473/34 ,  C07D473/30 ,  C07D473/18 ,  C07D239/47 ,  C07D239/54

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。