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1. 发明申请

US20120165514A1 SYNTHESIS OF LOCKED NUCLEIC ACID DERIVATIVES 有权
标题翻译：锁定核酸衍生物的合成
公开(公告)号：US20120165514A1
公开(公告)日：2012-06-28
申请号：US13336303
申请日：2011-12-23
申请人： Mads Detlef Sørensen , Jesper Wengel , Troels Koch , Signe M. Christensen , Christoph Rosenbohm , Daniel Sejer Pedersen
发明人： Mads Detlef Sørensen , Jesper Wengel , Troels Koch , Signe M. Christensen , Christoph Rosenbohm , Daniel Sejer Pedersen
IPC分类号： C07H19/02
CPC分类号： C07H19/20 , C07H19/00 , C07H19/04 , C07H19/048
摘要： The invention relates to a novel strategy for the synthesis of Locked Nucleic Acid derivatives, such as α-L-oxy-LNA, amino-LNA, α-L-amino-LNA, thio-LNA, α-L-thio-LNA, seleno-LNA and methylene LNA, which provides scalable high yielding reactions utilising intermediates that also can produce other LNA analogues such as oxy-LNA. Also, the compounds of the formula X are important intermediates that may be reacted with varieties of nucleophiles leading to a wide variety of LNA analogues.
摘要翻译：本发明涉及一种合成锁定核酸衍生物的新策略，如α-L-氧-LNA，氨基-LNA，α-L-氨基-LNA，硫代-LNA，α-L-硫代-LNA，硒代-LNA和亚甲基LNA，其利用也可以产生其他LNA类似物如oxy-LNA的中间体提供可伸缩的高产反应。此外，式X的化合物是可能与各种亲核试剂反应的重要中间体，导致各种各样的LNA类似物。

2. 发明授权

US08084458B2 Synthesis of locked nucleic acid derivatives 有权
标题翻译：锁定核酸衍生物的合成
公开(公告)号：US08084458B2
公开(公告)日：2011-12-27
申请号：US12534711
申请日：2009-08-03
申请人： Mads Detlef Sørensen , Jesper Wengel , Troels Koch , Signe M. Christensen , Christoph Rosenbohm , Daniel Sejer Pedersen
发明人： Mads Detlef Sørensen , Jesper Wengel , Troels Koch , Signe M. Christensen , Christoph Rosenbohm , Daniel Sejer Pedersen
IPC分类号： C07D473/06 , C07D473/16 , C07D473/18 , C07D473/34 , C07D473/40 , C07D239/10 , C07D239/52 , A61P31/22
CPC分类号： C07H19/20 , C07H19/00 , C07H19/04 , C07H19/048
摘要： Methods are described for the synthesis of Locked Nucleic Acid (LNA) derivatives using certain nitrogen-containing nucleophiles.
摘要翻译：描述了使用某些含氮亲核试剂合成锁定核酸（LNA）衍生物的方法。

3. 发明申请

US20110245327A1 Oligonucleotide Analogues 有权
标题翻译：寡核苷酸类似物
公开(公告)号：US20110245327A1
公开(公告)日：2011-10-06
申请号：US12793565
申请日：2010-06-03
申请人： Jesper WENGEL , Poul Nielsen
发明人： Jesper WENGEL , Poul Nielsen
IPC分类号： A61K31/7088 , C07H21/02 , C07H21/04 , A61K31/713 , A61P35/00 , C12Q1/68 , C12P19/34 , G01N33/53 , C07H1/06
CPC分类号： C07H21/04
摘要： The present invention relates to novel bicyclic and tricyclic nucleoside and nucleotide analogues as well as to oligonucleotides comprising such elements. The nucleotide analogues, LNAs (Locked Nucleoside Analogues), are able to provide valuable improvements to oligonucleotides with respect to affinity and specificity towards complementary RNA and DNA oligomers. The novel type of LNA modified oligonucleotides, as well as the LNAs as such, are useful in a wide range of diagnostic applications as well as therapeutic applications. Among these can be mentioned antisense applications, PCR applications, strand displacement oligomers, as substrates for nucleic acid polymerases, as nucleotide based drugs, etc. The present invention also relates to such applications.
摘要翻译：本发明涉及新型的双环和三环核苷和核苷酸类似物以及包含这些元件的寡核苷酸。核苷酸类似物LNA（锁定核苷类似物）能够在对互补RNA和DNA寡聚体的亲和力和特异性方面为寡核苷酸提供有价值的改进。新型LNA修饰的寡核苷酸以及LNA本身可用于广泛的诊断应用以及治疗应用。其中可以提及反义应用，PCR应用，链置换寡聚体，作为核酸聚合酶的底物，作为核苷酸的药物等。本发明还涉及这样的应用。

4. 发明申请

US20100279895A1 OLIGONUCLEOTIDE ANALOGUES 有权
公开(公告)号：US20100279895A1
公开(公告)日：2010-11-04
申请号：US12192581
申请日：2008-08-15
申请人： Jesper Wengel , Poul Nielsen
发明人： Jesper Wengel , Poul Nielsen
IPC分类号： C40B40/06 , C07H21/00
CPC分类号： C07H21/04
摘要： The present invention relates to novel bicyclic and tricyclic nucleoside and nucleotide analogues as well as to oligonucleotides comprising such elements. The nucleotide analogues, LNAs (Locked Nucleoside Analogues), are able to provide valuable improvements to oligonucleotides with respect to affinity and specificity towards complementary RNA and DNA oligomers. The novel type of LNA modified oligonucleotides, as well as the LNAs as such, are useful in a wide range of diagnostic applications as well as therapeutic applications. Among these can be mentioned antisense applications, PCR applications, strand displacement oligomers, as substrates for nucleic acid polymerases, as nucleotide based drugs, etc. The present invention also relates to such applications.

5. 发明授权

US08314227B2 Hydroxymethyl substituted RNA oligonucleotides and RNA complexes 有权
标题翻译：羟甲基取代的RNA寡核苷酸和RNA复合物
公开(公告)号：US08314227B2
公开(公告)日：2012-11-20
申请号：US12515403
申请日：2008-05-21
申请人： Jesper Wengel
发明人： Jesper Wengel
IPC分类号： C07H21/04
CPC分类号： C12N15/113 , C07H21/00 , C12N15/111 , C12N2310/14 , C12N2310/31 , C12N2310/321 , C12N2310/323 , C12N2310/3231 , C12N2320/51
摘要： The present invention is directed to RNA oligonucleotides or complexes of RNA oligonucleotides, denoted herein together as RNA complexes, containing at least one, but optionally more that one, hydroxymethyl substituted nucleotide monomer(s). By a hydroxymethyl substituted nucleotide monomer is understood a nucleotide monomer containing a hydroxymethyl group (that may be unsubstituted, O-substituted for example with a conjugating group, or converted into an optionally substituted or conjugated aminomethyl group). This hydroxymethyl group is not partaking in formation of an internucleotide linkage and is not the hydroxymethyl group (containing the 5′-hydroxy group) of a natural RNA monomer. The RNA complexes of the invention may be useful for therapeutic applications, diagnostic applications or research applications.
摘要翻译：本发明涉及RNA寡核苷酸或RNA寡核苷酸的复合物，其在本文中一起表示为RNA复合物，其含有至少一个但任选地更多一个羟甲基取代的核苷酸单体。羟甲基取代的核苷酸单体被理解为含有羟甲基（其可以是未取代的，O-取代的，例如用共轭基团或转化为任选取代或共轭的氨基甲基）的核苷酸单体。该羟甲基不参与核苷酸间键连接的形成，不是天然RNA单体的羟甲基（含有5'-羟基）。本发明的RNA复合物可用于治疗应用，诊断应用或研究应用。

6. 发明授权

US08080644B2 Oligonucleotide analogues 有权
标题翻译：寡核苷酸类似物
公开(公告)号：US08080644B2
公开(公告)日：2011-12-20
申请号：US12190939
申请日：2008-08-13
申请人： Jesper Wengel , Poul Nielsen
发明人： Jesper Wengel , Poul Nielsen
IPC分类号： C07H21/00 , C07H21/04 , C07H19/04 , C12Q1/68
CPC分类号： C07H21/04
摘要： The present invention relates to novel bicyclic and tricyclic nucleoside and nucleotide analogues as well as to oligonucleotides comprising such elements. The nucleotide analogues, LNAs (Locked Nucleoside Analogues), are able to provide valuable improvements to oligonucleotides with respect to affinity and specificity towards complementary RNA and DNA oligomers. The novel type of LNA modified oligonucleotides, as well as the LNAs as such, are useful in a wide range of diagnostic applications as well as therapeutic applications. Among these can be mentioned antisense applications, PCR applications, strand displacement oligomers, as substrates for nucleic acid polymerases, as nucleotide based drugs, etc. The present invention also relates to such applications.
摘要翻译：本发明涉及新型的双环和三环核苷和核苷酸类似物以及包含这些元件的寡核苷酸。核苷酸类似物LNA（锁定核苷类似物）能够在对互补RNA和DNA寡聚体的亲和力和特异性方面为寡核苷酸提供有价值的改进。新型LNA修饰的寡核苷酸以及LNA本身可用于广泛的诊断应用以及治疗应用。其中可以提及反义应用，PCR应用，链置换寡聚体，作为核酸聚合酶的底物，作为核苷酸的药物等。本发明还涉及这样的应用。

7. 发明申请

US20100056768A1 HYDROXYMETHYL SUBSTITUTED RNA OLIGONUCLEOTIDES AND RNA COMPLEXES 有权
标题翻译：羟基甲基取代的RNA寡核苷酸和RNA复合物
公开(公告)号：US20100056768A1
公开(公告)日：2010-03-04
申请号：US12515403
申请日：2008-05-21
申请人： Jesper Wengel
发明人： Jesper Wengel
IPC分类号： C07H21/02
CPC分类号： C12N15/113 , C07H21/00 , C12N15/111 , C12N2310/14 , C12N2310/31 , C12N2310/321 , C12N2310/323 , C12N2310/3231 , C12N2320/51
摘要： The present invention is directed to RNA oligonucleotides or complexes of RNA oligonucleotides, denoted herein together as RNA complexes, containing at least one, but optionally more that one, hydroxymethyl substituted nucleotide monomer(s). By a hydroxymethyl substituted nucleotide monomer is understood a nucleotide monomer containing a hydroxymethyl group (that may be unsubstituted, O-substituted for example with a conjugating group, or converted into an optionally substituted or conjugated aminomethyl group). This hydroxymethyl group is not partaking in formation of an internucleotide linkage and is not the hydroxymethyl group (containing the 5′-hydroxy group) of a natural RNA monomer. The RNA complexes of the invention may be useful for therapeutic applications, diagnostic applications or research applications. The complexes include short interfering RNA complexes (siRNA duplexes) comprising an antisense strand and a continued or a discontinued passenger strand (“sense strand”) capable of regulating gene expression. At least one of these strands, possible more than one of these strands, are modified with one or more hydroxymethyl substituted nucleotide monomer(s) of this invention, that can be positioned at the 3′-end, at the 5′-end or internally. The RNA complexes of the invention can also be single stranded RNA oligonucleotides (“RNA strands”) that are modified with at least one, but optionally more that one, hydroxymethyl substituted nucleotide monomer(s). Such single stranded RNA strands are to be considered included whenever the term RNA complexes is used in this patent application. The complexes of the invention display enhanced stability towards nucleolytic degradation relative to the corresponding complexes comprised entirely from natural RNA monomers.
摘要翻译：本发明涉及RNA寡核苷酸或RNA寡核苷酸的复合物，其在本文中一起表示为RNA复合物，其含有至少一个但任选地更多一个羟甲基取代的核苷酸单体。羟甲基取代的核苷酸单体被理解为含有羟甲基（其可以是未取代的，O-取代的，例如用共轭基团或转化为任选取代或共轭的氨基甲基）的核苷酸单体。该羟甲基不参与核苷酸间键连接的形成，不是天然RNA单体的羟甲基（含有5'-羟基）。本发明的RNA复合物可用于治疗应用，诊断应用或研究应用。复合物包括包含能够调节基因表达的反义链和连续或不连续的乘客链（“有义链”）的短干扰RNA复合物（siRNA双链体）。这些链中的至少一个，可能多于一个这些链，用本发明的一个或多个羟甲基取代的核苷酸单体修饰，其可以位于5'端的3'末端，或在内部本发明的RNA复合物还可以是用至少一种但任选地更多一个羟甲基取代的核苷酸单体修饰的单链RNA寡核苷酸（“RNA链”）。只要在本专利申请中使用术语RNA复合物，就认为这样的单链RNA链。本发明的复合物相对于完全由天然RNA单体组成的相应复合物显示出增强的对于核分解降解的稳定性。

8. 发明授权

US07569575B2 Synthesis of locked nucleic acid derivatives 有权
标题翻译：锁定核酸衍生物的合成
公开(公告)号：US07569575B2
公开(公告)日：2009-08-04
申请号：US10435607
申请日：2003-05-08
申请人： Mads Detlef Sørensen , Jesper Wengel , Troels Koch , Signe M. Christensen , Christoph Rosenbohm , Daniel Sejer Pedersen
发明人： Mads Detlef Sørensen , Jesper Wengel , Troels Koch , Signe M. Christensen , Christoph Rosenbohm , Daniel Sejer Pedersen
IPC分类号： C07D473/06 , C07D473/16 , C07D473/18 , C07D473/34 , C07D473/32 , C07D473/40 , C07D239/10 , C07D239/22 , A61K31/52 , A61K31/522 , A61K31/506 , A61P31/22
CPC分类号： C07H19/20 , C07H19/00 , C07H19/04 , C07H19/048
摘要： The invention relates to a novel strategy for the synthesis of Locked Nucleic Acid derivatives, such as α-L-oxy-LNA, amino-LNA, α-L-amino-LNA, thio-LNA, α-L-thio-LNA, seleno-LNA and methylene LNA, which provides scalable high yielding reactions utilizing intermediates that also can produce other LNA analogues such as oxy-LNA. Also, the compounds of the formula X are important intermediates that may be reacted with varieties of nucleophiles leading to a wide variety of LNA analogues.
摘要翻译：本发明涉及一种用于合成锁定核酸衍生物的新策略，例如α-小鼠，L

9. 发明授权

US07034133B2 Oligonucleotide analogues 有权
标题翻译：寡核苷酸类似物
公开(公告)号：US07034133B2
公开(公告)日：2006-04-25
申请号：US10208650
申请日：2002-07-29
申请人： Jesper Wengel , Poul Nielsen
发明人： Jesper Wengel , Poul Nielsen
IPC分类号： C07H21/00 , C07H21/02 , C07H21/04 , A01N43/04
CPC分类号： C07H21/00
摘要： Novel oligomers, and synthesis thereof, comprising one or more bi-, tri, or polycyclic nucleoside analogues are disclosed herein. The nucleoside analogues have a “locked” structure, termed Locked Nucleoside Analogues (LNA). LNA's exhibit highly desirable and useful properties. LNA's are capable of forming nucleobase specific duplexes and triplexes with single and double stranded nucleic acids. These complexes exhibit higher thermostability than the corresponding complexes formed with normal nucleic acids. The properties of LNA's allow for a wide range of uses such as diagnostic agents and therapeutic agents in a mammal suffering from or susceptible to, various diseases.
摘要翻译：本文公开了包含一种或多种双，三或多环核苷类似物的新型低聚物及其合成。核苷类似物具有“锁定”结构，称为“U型”（LNA）。 LNA的展示非常理想和有用的性能。 LNA能够用单链和双链核酸形成核碱基特异性双链体和三链体。这些配合物表现出比与正常核酸形成的相应复合物更高的热稳定性。 LNA的性质允许在各种疾病患有或易患各种疾病的哺乳动物中广泛使用诸如诊断剂和治疗剂。

10. 发明授权

US08492390B2 Synthesis of locked nucleic acid derivatives 有权
标题翻译：锁定核酸衍生物的合成
公开(公告)号：US08492390B2
公开(公告)日：2013-07-23
申请号：US13336303
申请日：2011-12-23
申请人： Mads Detlef Sorensen , Jesper Wengel , Troels Koch , Signe M. Christensen , Christoph Rosenbohm , Daniel Sejer Pedersen
发明人： Mads Detlef Sorensen , Jesper Wengel , Troels Koch , Signe M. Christensen , Christoph Rosenbohm , Daniel Sejer Pedersen
IPC分类号： C07D473/06 , C07D473/16 , C07D473/18 , C07D473/34 , C07D473/40 , C07D239/70 , C07D239/52 , A61P31/22
CPC分类号： C07H19/20 , C07H19/00 , C07H19/04 , C07H19/048
摘要： The invention relates to a novel strategy for the synthesis of Locked Nucleic Acid derivatives, such as α-L-oxy-LNA, amino-LNA, α-L-amino-LNA, thio-LNA, α-L-thio-LNA, seleno-LNA and methylene LNA, which provides scalable high yielding reactions utilising intermediates that also can produce other LNA analogues such as oxy-LNA. Also, the compounds of the formula X are important intermediates that may be reacted with varieties of nucleophiles leading to a wide variety of LNA analogues.
摘要翻译：本发明涉及一种用于合成锁定核酸衍生物的新策略，例如α-L-氧-LNA，氨基-LNA，α-L-氨基-LNA，硫代-LNA，α-L-硫代-LNA，硒代-LNA和亚甲基LNA，其利用也可以产生其他LNA类似物如oxy-LNA的中间体提供可伸缩的高产反应。此外，式X的化合物是可能与各种亲核试剂反应的重要中间体，导致各种各样的LNA类似物。

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