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公开(公告)号：US09067961B2
公开(公告)日：2015-06-30
申请号：US13485592
申请日：2012-05-31
申请人： Douglas J. Dellinger , Agnieszka B. Sierzchala , John Turner , Joel Myerson , Zoltan Kupihar , Fernando Ferreira , Marvin H. Caruthers , Geraldine F. Dellinger
发明人： Douglas J. Dellinger , Agnieszka B. Sierzchala , John Turner , Joel Myerson , Zoltan Kupihar , Fernando Ferreira , Marvin H. Caruthers , Geraldine F. Dellinger
IPC分类号： C07H13/12 , C07H21/02 , C07H19/073 , C07H19/16
CPC分类号： C07H19/073 , C07H13/12 , C07H19/16 , C07H21/02 , Y02P20/55
摘要： Aspects of the invention include 2′ protected nucleoside monomers that are protected at the 2′ site with thiocarbon protecting groups. Thiocarbon protecting groups of interest include thiocarbonate, thionocarbonate, dithiocarbonate groups, as well as thionocarbamate protecting groups. Aspects of the invention further include nucleic acids that include the protecting groups of the invention, as well as methods of synthesizing nucleic acids using the protecting groups of the invention.
摘要翻译： 本发明的方面包括2'受保护的核苷单体，其在2'位置被硫代保护基团保护。 感兴趣的硫代碳保护基包括硫代碳酸酯，硫代碳酸酯，二硫代碳酸酯基，以及硫羰氨基保护基。 本发明的方面还包括包含本发明的保护基团的核酸以及使用本发明的保护基合成核酸的方法。
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公开(公告)号：US20120238737A1
公开(公告)日：2012-09-20
申请号：US13485592
申请日：2012-05-31
申请人： Douglas J. Dellinger , Agnieszka Sierzchala , John Turner , Joel Myerson , Zoltan Kupihar , Fernando Ferreira , Marvin H. Caruthers , Geraldine F. Dellinger
发明人： Douglas J. Dellinger , Agnieszka Sierzchala , John Turner , Joel Myerson , Zoltan Kupihar , Fernando Ferreira , Marvin H. Caruthers , Geraldine F. Dellinger
CPC分类号： C07H19/073 , C07H13/12 , C07H19/16 , C07H21/02 , Y02P20/55
摘要： Aspects of the invention include 2′ protected nucleoside monomers that are protected at the 2′ site with thiocarbon protecting groups. Thiocarbon protecting groups of interest include thiocarbonate, thionocarbonate, dithiocarbonate groups, as well as thionocarbamate protecting groups. Aspects of the invention further include nucleic acids that include the protecting groups of the invention, as well as methods of synthesizing nucleic acids using the protecting groups of the invention.
摘要翻译： 本发明的方面包括2'受保护的核苷单体，其在2'位置被硫代保护基团保护。 感兴趣的硫代碳保护基包括硫代碳酸酯，硫代碳酸酯，二硫代碳酸酯基，以及硫羰氨基保护基。 本发明的方面还包括包含本发明的保护基团的核酸以及使用本发明的保护基合成核酸的方法。
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公开(公告)号：US08202983B2
公开(公告)日：2012-06-19
申请号：US12118655
申请日：2008-05-09
申请人： Douglas J. Dellinger , Agnieszka Sierzchala , John Turner , Joel Myerson , Zoltan Kupihar , Fernando Ferreira , Marvin H. Caruthers , Geraldine F. Dellinger
发明人： Douglas J. Dellinger , Agnieszka Sierzchala , John Turner , Joel Myerson , Zoltan Kupihar , Fernando Ferreira , Marvin H. Caruthers , Geraldine F. Dellinger
CPC分类号： C07H19/073 , C07H13/12 , C07H19/16 , C07H21/02 , Y02P20/55
摘要： Aspects of the invention include 2′ protected nucleoside monomers that are protected at the 2′ site with thiocarbon protecting groups. Thiocarbon protecting groups of interest include thiocarbonate, thionocarbonate, dithiocarbonate groups, as well as thionocarbamate protecting groups. Aspects of the invention further include nucleic acids that include the protecting groups of the invention, as well as methods of synthesizing nucleic acids using the protecting groups of the invention.
摘要翻译： 本发明的方面包括2'受保护的核苷单体，其在2'位置被硫代保护基团保护。 感兴趣的硫代碳保护基包括硫代碳酸酯，硫代碳酸酯，二硫代碳酸酯基，以及硫羰氨基保护基。 本发明的方面还包括包含本发明的保护基团的核酸以及使用本发明的保护基合成核酸的方法。
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公开(公告)号：US20090209479A1
公开(公告)日：2009-08-20
申请号：US12118655
申请日：2008-05-09
申请人： Douglas J. Dellinger , Agnieszka Sierzchala , John Turner , Joel Myerson , Zoltan Kupihar , Fernando Ferreira , Marvin H. Caruthers
发明人： Douglas J. Dellinger , Agnieszka Sierzchala , John Turner , Joel Myerson , Zoltan Kupihar , Fernando Ferreira , Marvin H. Caruthers
CPC分类号： C07H19/073 , C07H13/12 , C07H19/16 , C07H21/02 , Y02P20/55
摘要： Aspects of the invention include 2′ protected nucleoside monomers that are protected at the 2′ site with thiocarbon protecting groups. Thiocarbon protecting groups of interest include thiocarbonate, thionocarbonate, dithiocarbonate groups, as well as thionocarbamate protecting groups. Aspects of the invention further include nucleic acids that include the protecting groups of the invention, as well as methods of synthesizing nucleic acids using the protecting groups of the invention.
摘要翻译： 本发明的方面包括2'受保护的核苷单体，其在2'位置被硫代保护基团保护。 感兴趣的硫代碳保护基包括硫代碳酸酯，硫代碳酸酯，二硫代碳酸酯基，以及硫羰氨基保护基。 本发明的方面还包括包含本发明的保护基团的核酸以及使用本发明的保护基合成核酸的方法。
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公开(公告)号：US07427679B2
公开(公告)日：2008-09-23
申请号：US10652048
申请日：2003-08-30
摘要： Precursors for use in the synthesis of polynucleotides are disclosed. The precursors include a heterocyclic base having an exocyclic amine group and a substituted or unsubstituted triaryl methyl protecting group bound to the exocyclic amine group. In particular embodiments, the precursor has the structure: wherein: O and H represent oxygen and hydrogen, respectively, R1 is hydrido, hydroxyl, protected hydroxyl, lower alkyl, modified lower alkyl, or alkoxy, one of R2 or R3 is a hydroxyl protecting group; and the other of R2 or R3 is a reactive group capable of reacting with a reactive site hydroxyl, Base is a heterocyclic base having an exocyclic amine group, and Tram is a triaryl methyl group having the structure (V) wherein the broken line represents a bond to the amino nitrogen of the exocyclic amine group, and R4, R5 and R6 are independently selected from unsubstituted or substituted aryl groups, provided that at least one of R4, R5, and R6 is an aryl group other than phenyl and other than substituted phenyl.
摘要翻译： 公开了用于合成多核苷酸的前体。 前体包括具有环外胺基的杂环碱基和与环外胺基结合的取代或未取代的三芳基甲基保护基。 在具体实施方案中，前体具有以下结构：其中：O和H分别表示氧和氢，R 1是氢，羟基，被保护的羟基，低级烷基，经修饰的低级烷基或烷氧基，R 2或R 3之一是 羟基保护基; R 2或R 3中的另一个为可与反应性位点羟基反应的反应性基团，碱基为具有环外胺基的杂环碱基，Tram为具有结构（V）的三芳基甲基，其中虚线 表示与环外胺基团的氨基氮的键，并且R 4，R 5和R 6独立地选自未取代或取代的芳基，条件是R 4，R 5和R 6中的至少一个是芳基 除苯基以外的基团，而不是取代的苯基。
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6.发明授权Exocyclic amine triaryl methyl protecting groups in two-step polynucleotide synthesis 有权环二胺三芳基甲基保护基团在两步多核苷酸合成中的应用公开(公告)号：US07193077B2
公开(公告)日：2007-03-20
申请号：US10652064
申请日：2003-08-30
摘要： Precursors for use in the synthesis of polynucleotides and methods of using the precursors in synthesizing polynucleotides are disclosed. The precursors include a heterocyclic base having an exocyclic amine group and a substituted or unsubstituted triaryl methyl protecting group bound to the exocyclic amine group.
摘要翻译： 公开了用于合成多核苷酸的前体和在合成多核苷酸中使用前体的方法。 前体包括具有环外胺基的杂环碱基和与环外胺基结合的取代或未取代的三芳基甲基保护基。
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公开(公告)号：US20080206851A1
公开(公告)日：2008-08-28
申请号：US11713424
申请日：2007-02-28
摘要： In some embodiments, the present disclosure relates to new phosphoramidite compositions, that have Silyl-containing carbonate or thiocarbonate or ether as 5′-hydroxyl protecting groups useful fo the syntheis of RNA, and in particular for the synthesis of long sequences of RNA (e.g., >50 mer). In some embodiments, there are provided methods for simultaneous oxidation of the internucleoside phosphate triester linkages and removal of the 5′-hydroxyl-protecting group, making this process a new 2-step RNA synthesis, that involves the use of peroxyanions in combination with fluoride anions.
摘要翻译： 在一些实施方案中，本公开涉及新的亚磷酰胺组合物，其具有含有甲硅烷基的碳酸酯或硫代碳酸酯或醚作为用于RNA合成的5'-羟基保护基，特别是用于合成长序列的RNA（例如 ，> 50 mer）。 在一些实施方案中，提供了同时氧化核苷磷酸三酯键并除去5'-羟基保护基团的方法，使该方法成为新的2步RNA合成，其涉及使用过氧阴离子与氟化物 阴离子
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公开(公告)号：US20080206850A1
公开(公告)日：2008-08-28
申请号：US11713221
申请日：2007-02-28
摘要： In some embodiments, the present disclosure relates to new phosphoramidite compositions, that have Silyl-containing carbonate or thiocarbonate or ether as 5′-hydroxyl protecting groups useful of the synthesis of DNA, and in particular for the synthesis of long sequences of DNA (e.g., >50 mer). In some embodiments, there are provided methods for simultaneous oxidation of the internucleoside phosphate triester linkages and removal of the 5′-hydroxyl-protecting group, making this process a new 2-step DNA synthesis, that involves the use of peroxyanions in combination with fluoride anions.
摘要翻译： 在一些实施方案中，本公开涉及新的亚磷酰胺组合物，其具有含有甲硅烷基的碳酸酯或硫代碳酸酯或醚作为可用于合成DNA的5'-羟基保护基团，特别是用于合成长序列DNA（例如 ，> 50 mer）。 在一些实施方案中，提供了同时氧化核苷磷酸三酯键并除去5'-羟基保护基团的方法，使该方法成为新的2-步DNA合成，其涉及使用过氧阴离子与氟化物 阴离子
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9.发明申请公开(公告)号：US20080227964A1
公开(公告)日：2008-09-18
申请号：US11985598
申请日：2007-11-15
IPC分类号： C07H19/00
摘要： Nucleoside monomers, nucleic acids, e.g., oligonucleotides and polynucleotides, methods of making each, methods of deprotecting each, and the like are disclosed herein. Aspects of the invention include 2′ silyl containing thiocarbonate protecting groups. Corresponding compositions and methods are provided.
摘要翻译： 本文公开了核苷单体，核酸，例如寡核苷酸和多核苷酸，制备各种方法，各自的脱保护方法等。 本发明的方面包括2'含甲硅烷基的硫代碳酸酯保护基。 提供了相应的组合物和方法。
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10.发明授权公开(公告)号：US07999087B2
公开(公告)日：2011-08-16
申请号：US11985598
申请日：2007-11-15
摘要： Nucleoside monomers, nucleic acids, e.g., oligonucleotides and polynucleotides, methods of making each, methods of deprotecting each, and the like are disclosed herein. Aspects of the invention include 2′ silyl containing thiocarbonate protecting groups. Corresponding compositions and methods are provided.
摘要翻译： 本文公开了核苷单体，核酸，例如寡核苷酸和多核苷酸，制备各种方法，各自的脱保护方法等。 本发明的方面包括2'含甲硅烷基的硫代碳酸酯保护基。 提供了相应的组合物和方法。
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