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1. 发明申请

WO2005009998A1 PNA MONOMER AND PRECURSOR 审中-公开
标题翻译： PNA单身和前辈
公开(公告)号：WO2005009998A1
公开(公告)日：2005-02-03
申请号：PCT/IB2004/050406
申请日：2004-04-07
申请人： PANAGENE INC. , KIM, Sung Kee , LEE, Hyunil , LIM, Jong Chan , LEE, Sung Hee
发明人： KIM, Sung Kee , LEE, Hyunil , LIM, Jong Chan , LEE, Sung Hee
IPC分类号： C07D413/12
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 (A, B) wherein A 1 , A 2 , A 3 , A 4 , A 5 , is independently selected from H, halogen such as F, Cl, Br or I, CF 3 , alkyl, preferably C 1 ,-C 4 alkyl, nitro, nitrile, alkoxy, preferably C 1 ,-C 4 alkoxy, halogenated (such as F, Cl, Br and I) alkyl, preferably halogenated C 1 -C 4 alkyl, halogenated (such as F, Cl, Br and I) alkoxy, preferably halogenated Ci-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（A，B）的官能团，其中A1，A2，A3，A4，A5为独立地选自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是天然或非天然α-氨基酸的H或保护或未保护的侧链; 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。

2. 发明申请

WO2003091231A1 PNA MONOMER AND PRECURSOR 审中-公开
标题翻译： PNA单身和前辈
公开(公告)号：WO2003091231A1
公开(公告)日：2003-11-06
申请号：PCT/IB2003/001595
申请日：2003-04-28
申请人： PANAGENE, INC. , KIM, Sung, Kee , LEE, Hyunil , LIM, Jong, Chan , CHOI, Hoon , JEON, Jae, Hoon , AHN, Sang, Youl , LEE, Sung, Hee , YOON, Won, Jun
发明人： KIM, Sung, Kee , LEE, Hyunil , LIM, Jong, Chan , CHOI, Hoon , JEON, Jae, Hoon , AHN, Sang, Youl , LEE, Sung, Hee , YOON, Won, Jun
IPC分类号： C07D277/76
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 PNA (peptide nucleic acid) oligomers and provides method for the synthesis of both predefined sequence PNA oligomers and random sequence PNA oligomers: (I) wherein E is nitrogen or C-R'; J is sulfur or oxygen; R', Rl, R2, R3, R4 is independently H, halogen, alkyl, nitro, nitrile, alkoxy, halogenated alkyl, halogenated alkoxy, phenyl or halogenated phenyl, RS is H or protected or unprotected side chain of natural or unnatural a-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：（I）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，RS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。

3. 发明申请

WO2003062212A1 PEPTIDE NUCLEIC ACID OLIGOMERS FROM 1-BENZENESULFONYL-3-AMINO ACID SIDE CHAIN-4-(2-NUCLEOBASE(ACETYL))-PIPERAZIN-2-ONES 审中-公开
标题翻译：来自1-苯甲酰基-3-氨基酸的链肽-4-（2-核苷酸（乙酰）） - 哌嗪-2-酮的肽核酸低聚物
公开(公告)号：WO2003062212A1
公开(公告)日：2003-07-31
申请号：PCT/IB2003/000164
申请日：2003-01-23
申请人： PANAGENE, INC. , KIM, Sung, Kee , LEE, Hyunil , LIM, Jong, Chan , CHOI, Hoon , JEON, Jae, Hoon , AHN, Sang, Youl , LEE, Sung, Hee
发明人： KIM, Sung, Kee , LEE, Hyunil , LIM, Jong, Chan , CHOI, Hoon , JEON, Jae, Hoon , AHN, Sang, Youl , LEE, Sung, Hee
IPC分类号： C07D241/08
CPC分类号： C07D403/06 , C07D473/18 , C07D473/30 , C07D473/34 , C07K14/003 , Y02P20/55
摘要： This application relates to monomers of 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, C 1 -C 4 alkyl, nitro, nitrile, C 1 -C 4 alkoxy, halogenated C 1 -C 4 alkyl, or halogenated C 1 -C 4 alkoxy, wherein at least one of R1, R3, and R5 is nitro; R6 is H or protected or unprotected side chain of natural or unnatrual α-amino acid; and B is a natural or unnatrual 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，R5 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R 1，R 3和R 5中的至少一个是硝基; R6是H或保护或未受保护的天然或不需要的α-氨基酸的侧链; 并且B是天然或不合格的核碱基，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等碱基稳定的保护基保护。

4. 发明公开

EP1470114A1 PEPTIDE NUCLEIC ACID OLIGOMERS FROM 1-BENZENESULFONYL-3-AMINO ACID SIDE CHAIN-4-(2-NUCLEOBASE(ACETYL))-PIPERAZIN-2-ONES 有权
标题翻译：的1-苯磺酰基-3-氨基酸侧链基-4-（2-核蛋白基（乙酰基））哌嗪-2-酮的肽核酸寡聚物
公开(公告)号：EP1470114A1
公开(公告)日：2004-10-27
申请号：EP03700408.2
申请日：2003-01-23
申请人： Panagene, Inc.
发明人： KIM, Sung Kee , LEE, Hyunil , LIM, Jong Chan , CHOI, Hoon , JEON, Jae Hoon , AHN, Sang Youl , LEE, Sung Hee
IPC分类号： C07D241/08 , C07D473/18 , C07D473/34 , C07D239/47 , C07D239/54 , C07D403/06 , C07C311/18
CPC分类号： C07D403/06 , C07D473/18 , C07D473/30 , C07D473/34 , C07K14/003 , Y02P20/55
摘要： This application relates to monomers of 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 unnatrual α-amino acid; and B is a natural or unnatrual 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.

5. 发明授权

EP1651642B1 PNA MONOMER AND PRECURSOR 有权
标题翻译： PNA单体和PRE-PRESS
公开(公告)号：EP1651642B1
公开(公告)日：2009-11-04
申请号：EP04726242.3
申请日：2004-04-07
申请人： Panagene Inc.
发明人： KIM, Sung Kee , LEE, Hyunil , LIM, Jong Chan , LEE, Sung Hee
IPC分类号： C07D413/12 , C07D417/12 , C07D263/46 , C07D271/113
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 (A, B) 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 Ci-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.

6. 发明授权

EP1470114B1 PEPTIDE NUCLEIC ACID OLIGOMERS FROM 1-BENZENESULFONYL-3-AMINO ACID SIDE CHAIN-4-(2-NUCLEOBASE(ACETYL))-PIPERAZIN-2-ONES 有权
标题翻译：的1-苯磺酰基-3-氨基酸侧链基-4-（2-核蛋白基（乙酰基））哌嗪-2-酮的肽核酸寡聚物
公开(公告)号：EP1470114B1
公开(公告)日：2009-08-19
申请号：EP03700408.2
申请日：2003-01-23
申请人： Panagene, Inc.
发明人： KIM, Sung Kee , LEE, Hyunil , LIM, Jong Chan , CHOI, Hoon , JEON, Jae Hoon , AHN, Sang Youl c/o Panagene, Inc. , LEE, Sung Hee
IPC分类号： C07D241/08 , C07D473/18 , C07D473/34 , C07D239/47 , C07D239/54 , C07D403/06 , C07C311/18
CPC分类号： C07D403/06 , C07D473/18 , C07D473/30 , C07D473/34 , C07K14/003 , Y02P20/55
摘要： This application relates to monomers of 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 unnatrual α-amino acid; and B is a natural or unnatrual 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.

7. 发明公开

EP1651642A1 PNA MONOMER AND PRECURSOR 有权
标题翻译： PNA单体和前体
公开(公告)号：EP1651642A1
公开(公告)日：2006-05-03
申请号：EP04726242.3
申请日：2004-04-07
申请人： Panagene Inc.
发明人： KIM, Sung Kee , LEE, Hyunil , LIM, Jong Chan , LEE, Sung Hee
IPC分类号： C07D413/12 , C07D417/12 , C07D263/46 , C07D271/113
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 (A, B) 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 Ci-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）寡聚物的通式（I）的单体，并且提供用于合成预定义序列PNA寡聚体和随机序列PNA寡聚体的方法，其中E是硫或氧; J是氮或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（A，B）之一的官能团：其中A1，A2，A3，A4，A5是卤素如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（例如F，Cl，Br和I）烷基，优选卤代C 1 -C 4烷基，优选卤代C 1 -C 4烷氧基，苯基和卤代（例如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; 并且B是天然或非天然的核碱基，其中当所述核碱基具有环外氨基官能时，所述官能团受到对酸不稳定但在硫醇存在下对弱至中等碱稳定的保护基的保护。

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