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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：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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4.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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公开(公告)号：US20120289691A1
公开(公告)日：2012-11-15
申请号：US13531191
申请日：2012-06-22
申请人： Douglas J. Dellinger , Joel Myerson , Agnieszka Sierzchala , Geraldine F. Dellinger , Zoltan Timar
发明人： Douglas J. Dellinger , Joel Myerson , Agnieszka Sierzchala , Geraldine F. Dellinger , Zoltan Timar
IPC分类号： C07H1/00
CPC分类号： C07H19/067 , A61K31/712 , A61K31/7125 , C07H1/00 , C07H13/12 , C07H19/00 , C07H19/167 , C07H21/00 , C07H21/02 , C07H21/04 , C07H23/00 , Y02P20/55
摘要： A method of deprotecting a solid support bound polynucleotide includes the step of contacting the polynucleotide with a composition comprising a diamine under conditions sufficient to deprotect the 2′-protected ribonucleotide residue. The solid support bound polynucleotide has at least one 2′-protected ribonucleotide residue, which has the following structure: wherein BP is a protected or unprotected heterocycle; R12 is a protecting group selected from a hydrocarbyl, a substituted hydrocarbyl, an aryl, and a substituted aryl; X is O or S; and PG is a thionocarbamate protecting group.
摘要翻译： 使固体支持物结合的多核苷酸去保护的方法包括在足以使2'-保护的核糖核苷酸残基脱保护的条件下使多核苷酸与包含二胺的组合物接触的步骤。 固体支持结合的多核苷酸具有至少一个2'-保护的核糖核苷酸残基，其具有以下结构：其中BP是被保护或未被保护的杂环; R 12是选自烃基，取代的烃基，芳基和取代的芳基的保护基; X是O或S; PG是硫代氨基甲酸酯保护基。
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6.发明申请公开(公告)号：US20100076183A1
公开(公告)日：2010-03-25
申请号：US12466326
申请日：2009-05-14
申请人： Douglas J. Dellinger , Joel Myerson , Agnieszka Sierzchala , Geraldine F. Dellinger , Zoltan Timar
发明人： Douglas J. Dellinger , Joel Myerson , Agnieszka Sierzchala , Geraldine F. Dellinger , Zoltan Timar
IPC分类号： C07H17/00 , C07H21/00 , C07C211/10
CPC分类号： C07H19/067 , A61K31/712 , A61K31/7125 , C07H1/00 , C07H13/12 , C07H19/00 , C07H19/167 , C07H21/00 , C07H21/02 , C07H21/04 , C07H23/00 , Y02P20/55
摘要： A nucleoside monomer that is protected by a thionocarbamate protecting group is provided, as well as a method for making a polynucleotide that uses the same. Also provided is a polynucleotide synthesis method that employs a diamine to deprotect a protected polynucleotide.
摘要翻译： 提供了由硫羰氨基保护基保护的核苷单体，以及制备使用该核苷单体的多核苷酸的方法。 还提供了使用二胺去保护受保护的多核苷酸的多核苷酸合成方法。
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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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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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9.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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10.发明授权公开(公告)号：US09273086B2
公开(公告)日：2016-03-01
申请号：US13531191
申请日：2012-06-22
申请人： Douglas J. Dellinger , Joel Myerson , Agnieszka B. Sierzchala , Geraldine F. Dellinger , Zoltan Timar
发明人： Douglas J. Dellinger , Joel Myerson , Agnieszka B. Sierzchala , Geraldine F. Dellinger , Zoltan Timar
IPC分类号： C07H21/02 , C07H13/12 , C07H19/067 , A61K31/7125 , A61K31/712 , C07H19/00 , C07H19/167 , C07H21/00 , C07H23/00
CPC分类号： C07H19/067 , A61K31/712 , A61K31/7125 , C07H1/00 , C07H13/12 , C07H19/00 , C07H19/167 , C07H21/00 , C07H21/02 , C07H21/04 , C07H23/00 , Y02P20/55
摘要： A method of deprotecting a solid support bound polynucleotide includes the step of contacting the polynucleotide with a composition comprising a diamine under conditions sufficient to deprotect the 2′-protected ribonucleotide residue. The solid support bound polynucleotide has at least one 2′-protected ribonucleotide residue, which has the following structure: wherein BP is a protected or unprotected heterocycle; R12 is a protecting group selected from a hydrocarbyl, a substituted hydrocarbyl, an aryl, and a substituted aryl; X is O or S; and PG is a thionocarbamate protecting group.
摘要翻译： 使固体支持物结合的多核苷酸去保护的方法包括在足以使2'-保护的核糖核苷酸残基脱保护的条件下使多核苷酸与包含二胺的组合物接触的步骤。 固体支持结合的多核苷酸具有至少一个2'-保护的核糖核苷酸残基，其具有以下结构：其中BP是被保护或未被保护的杂环; R 12是选自烃基，取代的烃基，芳基和取代的芳基的保护基; X是O或S; PG是硫代氨基甲酸酯保护基。
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