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1. 发明申请

US20100331532A1 Use Of N-Alkyl Imidazole For Sulfurization Of Oligonucleotides With An Acetyl Disulfide 有权
标题翻译：使用N-烷基咪唑用乙酰二硫化物对寡核苷酸进行硫化
公开(公告)号：US20100331532A1
公开(公告)日：2010-12-30
申请号：US12494118
申请日：2009-06-29
申请人： Agnieszka B. Sierzchala , Douglas J. Dellinger , Paul A. Metz , Victor R. Mokler
发明人： Agnieszka B. Sierzchala , Douglas J. Dellinger , Paul A. Metz , Victor R. Mokler
IPC分类号： C07H21/00 , C09K3/00
CPC分类号： C07H21/02
摘要： A method and compositions for sulfurizing at least one phosphite or thiophosphite linkage in an oligonucleotide. The addition of N-alkyl imidazole to the acetyldisulfide sulfurization solution enables the use of industrially preferred solvents or solvents that are derived from renewable resources.
摘要翻译：一种在寡核苷酸中硫化至少一种亚磷酸酯或硫代亚磷酸酯键的方法和组合物。向乙酰二硫化硫化溶液中加入N-烷基咪唑可以使用衍生自可再生资源的工业上优选的溶剂或溶剂。

2. 发明授权

US08309710B2 Use of N-alkyl imidazole for sulfurization of oligonucleotides with an acetyl disulfide 有权
标题翻译：使用N-烷基咪唑用乙酰基二硫化物硫化寡核苷酸
公开(公告)号：US08309710B2
公开(公告)日：2012-11-13
申请号：US12494118
申请日：2009-06-29
申请人： Agnieszka B. Sierzchala , Douglas J Dellinger , Paul A. Metz , Victor R Mokler
发明人： Agnieszka B. Sierzchala , Douglas J Dellinger , Paul A. Metz , Victor R Mokler
IPC分类号： C07H1/00 , C07H21/00 , C07D233/58 , C07C321/12
CPC分类号： C07H21/02
摘要： A method and compositions for sulfurizing at least one phosphite or thiophosphite linkage in an oligonucleotide. The addition of N-alkyl imidazole to the acetyldisulfide sulfurization solution enables the use of industrially preferred solvents or solvents that are derived from renewable resources.
摘要翻译：一种在寡核苷酸中硫化至少一种亚磷酸酯或硫代亚磷酸酯键的方法和组合物。向乙酰二硫化硫化溶液中加入N-烷基咪唑可以使用衍生自可再生资源的工业上优选的溶剂或溶剂。

3. 发明授权

US08642755B2 Use of thioacetic acid derivatives in the sulfurization of oligonucleotides with phenylacetyl disulfide 有权
标题翻译：硫代乙酸衍生物在寡核苷酸与苯乙酰二硫化物硫化中的应用
公开(公告)号：US08642755B2
公开(公告)日：2014-02-04
申请号：US12494493
申请日：2009-06-30
申请人： Agnieszka B. Sierzchala , Douglas J Dellinger , Victor R Mokler , Zoltan Timar
发明人： Agnieszka B. Sierzchala , Douglas J Dellinger , Victor R Mokler , Zoltan Timar
IPC分类号： C07H21/00 , C07D233/58 , C07C321/12
CPC分类号： C07H21/02
摘要： A method and compositions for sulfurizing at least one phosphite or thiophosphite linkage in an oligonucleotide. The methods employ a phenylacetyl disulfide reagent (known as PADS), phenylthioacetic acid (PTAA) in the presence or absence or N-alkyl imidazole in industrially preferred solvents or solvents that are derived from renewable resources. The use of PTAA eliminates the need to “age” the PADS solution prior to its use in sulfurization reactions.
摘要翻译：一种在寡核苷酸中硫化至少一种亚磷酸酯或硫代亚磷酸酯键的方法和组合物。该方法在工业上优选的可再生资源溶剂或溶剂中，在存在或不存在或N-烷基咪唑的情况下使用苯乙酰二硫化物（称为PADS），苯硫基乙酸（PTAA）。使用PTAA消除了在使用硫化反应之前“PADS”溶液的“老化”的需要。

4. 发明申请

US20100331533A1 Use Of Thioacetic Acid Derivatives In The Sulfurization Of Oligonucleotides With Phenylacetyl Disulfide 有权
标题翻译：硫代乙酸衍生物在使用苯乙酰基二硫化物的寡核苷酸硫化中的应用
公开(公告)号：US20100331533A1
公开(公告)日：2010-12-30
申请号：US12494493
申请日：2009-06-30
申请人： Agnieszka B. Sierzchala , Douglas J. Dellinger , Victor R. Mokler , Zoltan Timar
发明人： Agnieszka B. Sierzchala , Douglas J. Dellinger , Victor R. Mokler , Zoltan Timar
IPC分类号： C07H21/00 , C09K3/00
CPC分类号： C07H21/02
摘要： A method and compositions for sulfurizing at least one phosphite or thiophosphite linkage in an oligonucleotide. The methods employ a phenylacetyl disulfide reagent (known as PADS), phenylthioacetic acid (PTAA) in the presence or absence or N-alkyl imidazole in industrially preferred solvents or solvents that are derived from renewable resources. The use of PTAA eliminates the need to “age” the PADS solution prior to its use in sulfurization reactions.
摘要翻译：一种在寡核苷酸中硫化至少一种亚磷酸酯或硫代亚磷酸酯键的方法和组合物。该方法在工业上优选的可再生资源溶剂或溶剂中，在存在或不存在或N-烷基咪唑的情况下使用苯乙酰二硫化物（称为PADS），苯硫基乙酸（PTAA）。使用PTAA消除了在使用硫化反应之前“PADS”溶液的“老化”的需要。

5. 发明申请

US20120184724A1 PROTECTED MONOMERS AND METHODS OF DEPROTECTION FOR RNA SYNTHESIS 审中-公开
标题翻译：保护单体和RNA合成的保护方法
公开(公告)号：US20120184724A1
公开(公告)日：2012-07-19
申请号：US13339082
申请日：2011-12-28
申请人： Agnieszka B. Sierzchala , Brian Phillip Smart , Douglas J. Dellinger , Geraldine Dellinger , Joel Myerson , Zoltan Timar
发明人： Agnieszka B. Sierzchala , Brian Phillip Smart , Douglas J. Dellinger , Geraldine Dellinger , Joel Myerson , Zoltan Timar
IPC分类号： C07H21/02 , C07H19/067 , C07H19/20 , C07H19/167 , C07H19/10 , C07H1/00
CPC分类号： C07H23/00 , C07B59/005 , C07H19/067 , C07H19/167 , C07H21/02 , Y02P20/55
摘要： A nucleoside monomer that is protected by a thionocarbamate protecting group and contains one or more 2H, 13C, or 15N isotopes in the ribose and/or base part 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并在核糖和/或碱部分含有一个或多个2H，13C或15N同位素的核苷单体，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。

6. 发明授权

US07417139B2 Method for polynucleotide synthesis 失效
标题翻译：多核苷酸合成方法
公开(公告)号：US07417139B2
公开(公告)日：2008-08-26
申请号：US10652054
申请日：2003-08-30
申请人： Douglas J Dellinger , Agnieszka B. Sierzchala , Marvin H Caruthers , Geraldine F Dellinger
发明人： Douglas J Dellinger , Agnieszka B. Sierzchala , Marvin H Caruthers , Geraldine F Dellinger
IPC分类号： C07H21/00
CPC分类号： C07H21/00 , Y02P20/55
摘要： Methods of forming an internucleotide bond are disclosed. Such methods find use in synthesis of polynucleotides. The method involves contacting a functionalized support with a precursor having an exocyclic amine triaryl methyl protecting group under conditions and for a time sufficient to result in internucleotide bond formation. The functionalized support includes a solid support, a triaryl methyl linker group, and a nucleoside moiety having a reactive site hydroxyl, the nucleoside moiety attached to the solid support via the triaryl methyl linker 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 the reactive site hydroxyl, Base is a heterocyclic base having an exocyclic amine group, and Tram is the exocyclic amine triaryl methyl protecting group.
摘要翻译：公开了形成核苷酸间键的方法。这些方法可用于多核苷酸的合成。该方法包括使官能化载体与具有环外胺三芳基甲基保护基团的前体在足以导致形成核苷酸键的条件下进行接触。官能化载体包括固体支持物，三芳基甲基连接基团和具有反应性位点羟基的核苷部分，所述核苷部分通过三芳基甲基连接基团连接到固体支持物上。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为氢，羟基，保护的羟基，低级烷基，经修饰的低级烷基或烷氧基，R2或R3中的一个为羟基保护基 ; R2或R3中的另一个是能够与反应性位点羟基反应的反应性基团，碱是具有环外胺基的杂环基，Tram是环外胺三芳基甲基保护基。

7. 发明授权

US09273086B2 Protected monomer and method of final deprotection for RNA synthesis 有权
标题翻译：受保护的单体和RNA合成的最终脱保护方法
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。

8. 发明授权

US07427679B2 Precursors for two-step polynucleotide synthesis 失效
标题翻译：两步多核苷酸合成的前体
公开(公告)号：US07427679B2
公开(公告)日：2008-09-23
申请号：US10652048
申请日：2003-08-30
申请人： Douglas J. Dellinger , Agnieszka B. Sierzchala , Marvin H. Caruthers
发明人： Douglas J. Dellinger , Agnieszka B. Sierzchala , Marvin H. Caruthers
IPC分类号： C07H19/10 , C07H19/20
CPC分类号： C07H21/00 , C07H19/00 , Y02P20/55
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。

9. 发明授权

US09067961B2 Thiocarbon-protecting groups for RNA synthesis 有权
标题翻译：用于RNA合成的硫代保护基团
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。

10. 发明授权

US07193077B2 Exocyclic amine triaryl methyl protecting groups in two-step polynucleotide synthesis 有权
标题翻译：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
申请人： Douglas J. Dellinger , Agnieszka B. Sierzchala , Marvin H. Caruthers
发明人： Douglas J. Dellinger , Agnieszka B. Sierzchala , Marvin H. Caruthers
IPC分类号： C07H21/00 , C07H21/02 , C07H21/04 , A01N43/04 , A61K31/70
CPC分类号： C07H19/06 , C07H19/10 , C07H19/16 , C07H19/20 , C07H21/00 , Y02P20/55
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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