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1. 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。

2. 发明申请

US20120238737A1 THIOCARBON-PROTECTING GROUPS FOR RNA SYNTHESIS 有权
标题翻译：用于RNA合成的THIOCARBON保护组
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
IPC分类号： C07H1/00 , C07H19/20 , C07H21/02 , C07H19/10
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。

3. 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。

4. 发明申请

US20090082554A1 Thiocarbonate linkers for polynucleotides 有权
标题翻译：多核苷酸的硫代碳酸酯接头
公开(公告)号：US20090082554A1
公开(公告)日：2009-03-26
申请号：US11903821
申请日：2007-09-24
申请人： Douglas J. Dellinger , Zoltan Timar , Joel Myerson , Geraldine Dellinger , Marvin H. Caruthers
发明人： Douglas J. Dellinger , Zoltan Timar , Joel Myerson , Geraldine Dellinger , Marvin H. Caruthers
IPC分类号： C07H21/00 , C07H21/02 , C07H21/04
CPC分类号： C07H21/00 , C07H21/02 , C07H21/04
摘要： In various embodiments of the invention, novel compositions having a polynucleotide bound to a substrate via a cleavable linker are provided, and methods of cleaving a polynucleotide from a substrate are provided.
摘要翻译：在本发明的各种实施方案中，提供了具有通过可切割连接子与底物结合的多核苷酸的新型组合物，并提供了从底物切割多核苷酸的方法。

5. 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。

6. 发明申请

US20080206850A1 Methods and compositions for DNA synthesis 审中-公开
标题翻译： DNA合成的方法和组合物
公开(公告)号：US20080206850A1
公开(公告)日：2008-08-28
申请号：US11713221
申请日：2007-02-28
申请人： Douglas J. Dellinger , Geraldine F. Dellinger , Marvin H. Caruthers
发明人： Douglas J. Dellinger , Geraldine F. Dellinger , Marvin H. Caruthers
IPC分类号： C07H21/04 , C12M1/34
CPC分类号： C07H21/04 , Y02P20/55
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

7. 发明申请

US20080146787A1 Thioether substituted aryl carbonate protecting groups 有权
标题翻译：硫醚取代的芳基碳酸酯保护基
公开(公告)号：US20080146787A1
公开(公告)日：2008-06-19
申请号：US11897898
申请日：2007-08-31
申请人： Zoltan Timar , Zoltan Kupihar , Douglas J. Dellinger , Marvin H. Caruthers
发明人： Zoltan Timar , Zoltan Kupihar , Douglas J. Dellinger , Marvin H. Caruthers
IPC分类号： C07H21/00 , C07H19/04 , C07H21/04 , C07H21/02
CPC分类号： C07H19/04 , C07H21/00 , C07H21/02 , C07H21/04 , Y02P20/55
摘要： Embodiments of the invention include thioether substituted aryl carbonate protecting groups, and nucleoside monomers protected with thioether substituted aryl carbonate protecting groups. Aspects of the invention further included methods of synthesizing nucleic acids, e.g., oligonucleotides, using such protected nucleoside monomer monomers, as well as nucleic acids produced using methods of the invention and compositions thereof.
摘要翻译：本发明的实施方案包括硫醚取代的芳基碳酸酯保护基，和用硫醚取代的芳基碳酸酯保护基保护的核苷单体。本发明的方面还包括使用这种受保护的核苷单体/单体合成核酸例如寡核苷酸的方法，以及使用本发明的方法和其组合物制备的核酸。

8. 发明申请

US20070224602A1 Thiocarbonate linkers for polynucleotides 有权
标题翻译：多核苷酸的硫代碳酸酯接头
公开(公告)号：US20070224602A1
公开(公告)日：2007-09-27
申请号：US11389326
申请日：2006-03-23
申请人： Douglas J. Dellinger , Zoltan Timar , Joel Myerson , Geraldine Dellinger , Marvin Caruthers
发明人： Douglas J. Dellinger , Zoltan Timar , Joel Myerson , Geraldine Dellinger , Marvin Caruthers
IPC分类号： C12Q1/68 , C07H21/04
CPC分类号： C07H21/04
摘要： In various embodiments of the invention, novel compositions having a polynucleotide bound to a substrate via a cleavable linker are provided, and methods of cleaving a polynucleotide from a substrate are provided.
摘要翻译：在本发明的各种实施方案中，提供了具有通过可切割连接子与底物结合的多核苷酸的新型组合物，并提供了从底物切割多核苷酸的方法。

9. 发明授权

US07135565B2 Synthesis of polynucleotides using combined oxidation/deprotection chemistry 有权
公开(公告)号：US07135565B2
公开(公告)日：2006-11-14
申请号：US09916369
申请日：2001-07-27
申请人： Douglas J. Dellinger , Michael G. M. Perbost , Marvin H. Caruthers , Jason R. Betley
发明人： Douglas J. Dellinger , Michael G. M. Perbost , Marvin H. Caruthers , Jason R. Betley
IPC分类号： C07H21/00 , C07H21/02 , C07H21/04 , A01N43/04 , A61K31/70
CPC分类号： C07H21/00 , Y02P20/55
摘要： A method of synthesizing a polynucleotide which can, for example, be used during fabrication of an array. A second nucleoside is coupled to a first nucleoside through a phosphite linkage, with the second nucleoside having a hydroxyl protecting group that is a non-carbonate protecting group. The product of the foregoing step is exposed to a composition which both oxidizes the formed phosphite to a phosphate and deprotects the protected hydroxyl of the coupled nucleoside. The method has particular application to fabricating an addressable array of polynucleotides on a substrate which carries substrate bound moieties each with a hydroxyl group.

10. 发明授权

US06319674B1 Methods for attaching substances to surfaces 失效
标题翻译：将物质附着于表面的方法
公开(公告)号：US06319674B1
公开(公告)日：2001-11-20
申请号：US09397527
申请日：1999-09-16
申请人： Geraldine Fulcrand , Douglas J. Dellinger , Steven M. Lefkowitz
发明人： Geraldine Fulcrand , Douglas J. Dellinger , Steven M. Lefkowitz
IPC分类号： G01N3353
CPC分类号： G01N33/54353
摘要： Methods are disclosed for immobilizing a substance to a surface. A surface is employed that comprises a linking group consisting of a first portion comprising a hydrocarbon chain, optionally substituted, and a second portion comprising an alkylene oxide or an alkylene imine wherein the alkylene is optionally substituted. One end of the first portion is attached to the surface and one end of the second portion is attached to the other end of the first portion chain by means of an amine or an oxy functionality. The second portion terminates in an amine or a hydroxy functionality. The surface is reacted with the substance to be immobilized under conditions for attachment of the substance to the surface by means of the linking group. Compositions of matter and reaction systems are also disclosed.
摘要翻译：公开了将物质固定在表面上的方法。使用表面，其包含由包含任选取代的烃链的第一部分和包含烯化氧或亚烷基亚胺的第二部分组成的连接基团，其中所述亚烷基是任选取代的。第一部分的一端附接到表面，并且第二部分的一端通过胺或氧官能团连接到第一部分链的另一端。第二部分终止于胺或羟基官能团。在通过连接基团将物质附着到表面的条件下，表面与要固定的物质反应。还公开了物质和反应体系的组成。

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