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1. 发明申请

US20110077390A1 BICYCLIC CYCLOHEXITOL NUCLEIC ACID ANALOGS 有权
标题翻译：双环环孢素核酸类似物
公开(公告)号：US20110077390A1
公开(公告)日：2011-03-31
申请号：US12866708
申请日：2009-02-06
申请人： Punit P. Seth , Michael T. Migawa , Eric E. Swayze , Quanlai Song , Mingmin Han , Bruce S. Ross
发明人： Punit P. Seth , Michael T. Migawa , Eric E. Swayze , Quanlai Song , Mingmin Han , Bruce S. Ross
IPC分类号： C07H19/16 , C07H19/20
CPC分类号： C07H21/00
摘要： The present disclosure provides bicyclic cyclohexitol nucleoside analogs of formula I and oligomeric compounds comprising these nucleoside analogs. These bicyclic nucleoside analogs are expected to be useful for enhancing properties of oligomeric compounds including for example nuclease resistance.
摘要翻译：本公开提供式I的双环体醇核苷类似物和包含这些核苷类似物的低聚化合物。预期这些双环核苷类似物可用于增强低聚化合物的性质，包括例如核酸酶抗性。

2. 发明授权

US08530640B2 Bicyclic cyclohexitol nucleic acid analogs 有权
标题翻译：双环体醇核酸类似物
公开(公告)号：US08530640B2
公开(公告)日：2013-09-10
申请号：US12866708
申请日：2009-02-06
申请人： Punit P. Seth , Michael T. Migawa , Eric E. Swayze , Quanlai Song , Mingming Han , Bruce S. Ross
发明人： Punit P. Seth , Michael T. Migawa , Eric E. Swayze , Quanlai Song , Mingming Han , Bruce S. Ross
IPC分类号： C07H19/24 , C07H19/04
CPC分类号： C07H21/00
摘要： The present disclosure provides bicyclic cyclohexitol nucleoside analogs of formula I and oligomeric compounds comprising these nucleoside analogs. These bicyclic nucleoside analogs are expected to be useful for enhancing properties of oligomeric compounds including for example nuclease resistance.
摘要翻译：本公开提供式I的双环体醇核苷类似物和包含这些核苷类似物的低聚化合物。预期这些双环核苷类似物可用于增强低聚化合物的性质，包括例如核酸酶抗性。

3. 发明授权

US09012421B2 Bicyclic cyclohexose nucleic acid analogs 有权
标题翻译：双环环己糖核酸类似物
公开(公告)号：US09012421B2
公开(公告)日：2015-04-21
申请号：US13388115
申请日：2010-08-05
申请人： Michael T. Migawa , Punit P. Seth , Eric E. Swayze , Bruce S. Ross , Quanlai Song , Mingming Han
发明人： Michael T. Migawa , Punit P. Seth , Eric E. Swayze , Bruce S. Ross , Quanlai Song , Mingming Han
IPC分类号： A61K31/712 , C07H19/06 , C07H21/00 , C12N5/071 , C07H19/16
CPC分类号： C12N15/113 , C07H19/06 , C07H19/16 , C07H21/00
摘要： The present invention provides bicyclic cyclohexose nucleoside analogs and oligomeric compounds comprising these nucleoside analogs. These bicyclic nucleoside analogs are useful for enhancing properties of oligomeric compounds including nuclease resistance.
摘要翻译：本发明提供了包含这些核苷类似物的双环环己酮核苷类似物和低聚化合物。这些双环核苷类似物可用于增强包括核酸酶抗性的寡聚化合物的性质。

4. 发明申请

US20120172414A1 BICYCLIC CYCLOHEXOSE NUCLEIC ACID ANALOGS 有权
标题翻译：双环环孢菌素核酸类似物
公开(公告)号：US20120172414A1
公开(公告)日：2012-07-05
申请号：US13388115
申请日：2010-08-05
申请人： Michael T. Migawa , Punit P. Seth , Eric E. Swayze , Bruce S. Ross , Quanlai Song , Mingming Han
发明人： Michael T. Migawa , Punit P. Seth , Eric E. Swayze , Bruce S. Ross , Quanlai Song , Mingming Han
IPC分类号： A61K31/712 , C07H19/06 , C07H21/00 , C12N5/071
CPC分类号： C12N15/113 , C07H19/06 , C07H19/16 , C07H21/00
摘要： The present invention provides bicyclic cyclohexose nucleoside analogs and oligomeric compounds comprising these nucleoside analogs. These bicyclic nucleoside analogs are useful for enhancing properties of oligomeric compounds including nuclease resistance.
摘要翻译：本发明提供了包含这些核苷类似物的双环环己酮核苷类似物和低聚化合物。这些双环核苷类似物可用于增强包括核酸酶抗性的寡聚化合物的性质。

5. 发明授权

US07002006B2 Protection of nucleosides 有权
标题翻译：保护核苷
公开(公告)号：US07002006B2
公开(公告)日：2006-02-21
申请号：US10365183
申请日：2003-02-12
申请人： Quanlai Song , Bruce S. Ross
发明人： Quanlai Song , Bruce S. Ross
IPC分类号： C07H19/00
CPC分类号： C07H19/22 , C07H19/048
摘要： A process of manufacturing protected nucleosides comprises reacting a nucleoside with a protecting reagent in the presence of a regioselective activator to produce a regioselectively protected nucleoside. In some embodiments of the inventive method, an optionally substituted trityl or optionally substituted pixyl group is selectively added to the 5′-O-position of a nucleoside in the presence of lutidine as activator or activator/solvent. The inventive method results in improved selectivity of the 5′-O-position over the 3′-O-position, thereby improving overall product yield and purity, and permitting simplified purification protocols, in some cases obviating the need for chromatography to produce a purified protected nucleoside suitable for automated synthesis of oligonucleotides, such as primers, probes and antisense molecules.
摘要翻译：制备受保护的核苷的方法包括在区域选择性活化剂存在下使核苷与保护试剂反应以产生区域选择性保护的核苷。在本发明方法的一些实施方案中，在作为活化剂或活化剂/溶剂的二甲基吡啶存在下，将任选取代的三苯甲基或任选取代的吡啶基选择性地加入到核苷的5'-O-位。本发明的方法导致5'-O-位置相对于3'-O-位置的选择性提高，从而提高总体产物产率和纯度，并且允许简化的纯化方案，在一些情况下，不需要色谱法来产生纯化的保护的核苷适用于自动合成寡核苷酸，如引物，探针和反义分子。

6. 发明申请

US20080119645A1 Amidites and Methods of Rna Synthesis 审中-公开
标题翻译：苎麻和Rna合成方法
公开(公告)号：US20080119645A1
公开(公告)日：2008-05-22
申请号：US11568696
申请日：2005-05-03
申请人： Richard H. Griffey , Bruce S. Ross , Quanlai Song
发明人： Richard H. Griffey , Bruce S. Ross , Quanlai Song
IPC分类号： C07H21/04 , C07H21/02
CPC分类号： C07H19/06 , C07H21/00 , Y02P20/55
摘要： The present invention is directed to amidites useful in the synthesis of oligonucleotides comprising at least one RN moiety, and to methods of using such amidites in the synthesis of such oligonucleotides. The inventive amidites possess surprising coupling efficiency as compared to prior art amidites, while providing convenient intermediates in the synthesis of oligonucleotides possessing at least one free 2′-OH moiety.
摘要翻译：本发明涉及可用于合成包含至少一个RN部分的寡核苷酸的脒基，以及在合成这些寡核苷酸时使用这种脒基的方法。与现有技术的脒基相比，本发明的脒基具有惊人的偶联效率，同时在合成具有至少一个游离2'-OH部分的寡核苷酸的合成中提供方便的中间体。

7. 发明授权

US07030230B2 Process of purifying phosphoramidites 失效
标题翻译：亚磷酰胺的纯化方法
公开(公告)号：US07030230B2
公开(公告)日：2006-04-18
申请号：US10280383
申请日：2002-10-25
申请人： Bruce Ross , Quanlai Song
发明人： Bruce Ross , Quanlai Song
IPC分类号： C07H21/04 , C07H19/04
CPC分类号： C07H21/04 , C07H19/04
摘要： A process of purifying phosphoramidite precursors useful in inter alia synthesis of oligonucleotides comprises dissolving a crude phosphoramidite in a polar phase, adding a basic compound to the polar phase, adding a portion of water to the polar phase, contacting the polar phase with a first apolar phase to extract impurity into the apolar phase, separating the first apolar phase from the polar phase, adding a second aliquot of water to the polar phase, and contacting the polar phase with a second apolar phase, whereby the phosphoramidite partitions into the second apolar phase.
摘要翻译：用于尤其合成寡核苷酸的亚磷酰胺前体的纯化方法包括将极亚极亚胺中的粗亚磷酰胺溶解在极性相中，向极性相中加入碱性化合物，向极性相中加入一部分水，使极性相与第一非极性相接触将杂质萃取到非极性相中，从极性相分离第一非极性相，向极性相中加入第二等分试样的水，并将极性相与第二非极性相接触，由此亚磷酰胺分隔成第二非极性相。

8. 发明授权

US07019127B2 Solution phase synthesis of oligonucleotides 有权
公开(公告)号：US07019127B2
公开(公告)日：2006-03-28
申请号：US10294794
申请日：2002-11-15
申请人： Colin Bernard Reese , Quanlai Song
发明人： Colin Bernard Reese , Quanlai Song
IPC分类号： C07H21/00 , C07H21/02 , C07H21/04
CPC分类号： C07D265/33 , C07D207/48 , C07F9/165 , C07F9/18 , C07H19/10 , C07H19/20 , C07H21/00 , C07H21/04 , Y02P20/55
摘要： A process for the synthesis in solution phase of a phosphorothioate triester is provided. The process comprises the solution phase coupling of an H-phosphonate with an alcohol in the presence of a coupling agent to form an H-phosphonate diester. The H-phosphonate diester is oxidised in situ with a sulfur transfer agent to produce the phosphorothioate triester. Preferably, the H-phosphonate and alcohol are protected nucleosides or oligonucleotides. Oligonucleotide H-phosphonates which can be used in the formation of phosphorothioate triesters are also provided.

9. 发明申请

US20060040308A1 Compounds and methods for the characterization of oligonucleotides 有权
标题翻译：用于表征寡核苷酸的化合物和方法
公开(公告)号：US20060040308A1
公开(公告)日：2006-02-23
申请号：US11209160
申请日：2005-08-22
申请人： Daniel Capaldi , Hans-Joachim Gaus , Claus Rentel , Philip Olsen , Christine Kurata , Quanlai Song
发明人： Daniel Capaldi , Hans-Joachim Gaus , Claus Rentel , Philip Olsen , Christine Kurata , Quanlai Song
IPC分类号： C12Q1/68 , C07H21/04
CPC分类号： C07H21/04
摘要： The present invention relates to oligonucleotide synthesis. In particular, the present invention provides methods for characterizing samples useful for making oligonucleotides.
摘要翻译：本发明涉及寡核苷酸合成。特别地，本发明提供用于表征可用于制备寡核苷酸的样品的方法。

10. 发明授权

US06884881B1 2′-Substituted RNA preparation 失效
标题翻译： 2'-取代的RNA制剂
公开(公告)号：US06884881B1
公开(公告)日：2005-04-26
申请号：US09914596
申请日：2000-03-15
申请人： Colin Bernard Reese , Quanlai Song
发明人： Colin Bernard Reese , Quanlai Song
IPC分类号： C07H19/067 , C07H19/04 , C07H19/06 , C07H21/00 , C07H21/02 , C07H19/00 , C07H19/048
CPC分类号： C07H19/06 , C07H19/04 , C07H21/00 , Y02P20/55
摘要： A process for the preparation of a compound of formula (1): is provided, which comprises the reaction a compound of formula (2): with a compound of formula Al(OR)3 under substantially anhydrous conditions. X, and X1 are each independently H or a protecting group, B is a base; R is an alkyl, alkoxyalkyl, alkenyl or alkynyl group, each of which may be optionally substituted, and L is a leaving group.
摘要翻译：提供了制备式（1）化合物的方法：其包括在基本无水条件下使式（2）化合物与式A1（OR）3的化合物反应：。 X和X 1各自独立地为H或保护基，B为碱; R是烷基，烷氧基烷基，烯基或炔基，它们各自可以被任意取代，L是离去基团。

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