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1. 发明申请

WO2011017521A2 BICYCLIC CYCLOHEXOSE NUCLEIC ACID ANALOGS 审中-公开
标题翻译：双环葡萄糖核酸类似物
公开(公告)号：WO2011017521A2
公开(公告)日：2011-02-10
申请号：PCT/US2010/044549
申请日：2010-08-05
申请人： ISIS PHARMACEUTICALS, INC. , MIGAWA, Michael, T. , SETH, Punit, P. , SWAYZE, Eric, E. , ROSS, Bruce, S. , SONG, Quanlai , HAN, Mingming
发明人： MIGAWA, Michael, T. , SETH, Punit, P. , SWAYZE, Eric, E. , ROSS, Bruce, S. , SONG, Quanlai , HAN, Mingming
IPC分类号： C07H21/00
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：本发明提供双环环己糖核苷类似物和包含这些核苷类似物的寡聚化合物。这些双环核苷类似物可用于增强寡聚化合物的性质，包括核酸酶抗性。

2. 发明申请

WO2009100320A2 BICYCLIC CYCLOHEXITOL NUCLEIC ACID ANALOGS 审中-公开
标题翻译：双环环孢素核酸类似物
公开(公告)号：WO2009100320A2
公开(公告)日：2009-08-13
申请号：PCT/US2009/033373
申请日：2009-02-06
申请人： ISIS PHARMACEUTICALS, INC. , SETH, Punit, P. , MIGAWA, Michael, T. , SWAYZE, Eric, E. , SONG, Quanlai , HAN, Mingming , ROSS, Bruce
发明人： SETH, Punit, P. , MIGAWA, Michael, T. , SWAYZE, Eric, E. , SONG, Quanlai , HAN, Mingming , ROSS, Bruce
IPC分类号： C07H21/00
CPC分类号： C07H21/00
摘要： The present disclosure provides bicyclic cyclohexitol nucleoside analogs 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：本公开提供了包含这些核苷类似物的双环体醇酯核苷类似物和低聚化合物。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. 发明申请

WO2005077966A1 SUBSTITUTED PIXYL PROTECTING GROUPS FOR OLIGONUCLEOTIDE SYNTHESIS 审中-公开
标题翻译：用于寡核苷酸合成的取代的PIXYL保护组
公开(公告)号：WO2005077966A1
公开(公告)日：2005-08-25
申请号：PCT/US2005/004875
申请日：2005-02-10
申请人： ISIS PHARMACEUTICALS, INC. , SONG, Quanlai , KHAMMUNGKHUNE, Sak , ROSS, Bruce, S. , GRIFFEY, Richard, H.
发明人： SONG, Quanlai , KHAMMUNGKHUNE, Sak , ROSS, Bruce, S. , GRIFFEY, Richard, H.
IPC分类号： C07H19/06
CPC分类号： C07H19/06 , C07H21/00 , Y02P20/55
摘要： The present invention describes an improved hydroxyl protecting group of formula (1), wherein R 2 and R 7 are specified substituents and Q is O, S, NR 10 or N(C=O)R 10 .
摘要翻译：本发明描述了一种改进的式（1）羟基保护基，其中R 2和R 7是指定的取代基，Q是O，S，NR 10或N（C = O）R 10 。

4. 发明申请

WO2004072234A2 PROTECTION OF NUCLEOSIDES 审中-公开
标题翻译：保护核苷酸
公开(公告)号：WO2004072234A2
公开(公告)日：2004-08-26
申请号：PCT/US2004/002807
申请日：2004-02-02
申请人： ISIS PHARMACEUTICALS, INC. , SONG, Quanlai , ROSS, Bruce, S.
发明人： SONG, Quanlai , ROSS, Bruce, S.
IPC分类号： C12N
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’-0-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-位上。本发明的方法导致5'-O-位置在3'- 0位上的选择性提高，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。

5. 发明申请

WO2006023880A2 COMPOUNDS AND METHODS FOR THE CHARACTERIZATION OF OLIGONUCLEOTIDES 审中-公开
标题翻译：化合物和方法用于表征寡核苷酸
公开(公告)号：WO2006023880A2
公开(公告)日：2006-03-02
申请号：PCT/US2005/029850
申请日：2005-08-22
申请人： ISIS PHARMACEUTICALS, INC. , CAPALDI, Daniel, C. , GAUS, Hans-Joachim, Josef , RENTEL, Claus, Andre, Frank , OLSEN, Philip, Dmitri , KURATA, Christine, C. , SONG, Quanlai
发明人： CAPALDI, Daniel, C. , GAUS, Hans-Joachim, Josef , RENTEL, Claus, Andre, Frank , OLSEN, Philip, Dmitri , KURATA, Christine, C. , SONG, Quanlai
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。

6. 发明申请

WO2003087130A3 PROCESS FOR MANUFACTURING PURIFIED PHOSPHORODIAMIDITE 审中-公开
公开(公告)号：WO2003087130A3
公开(公告)日：2003-10-23
申请号：PCT/US2003/011016
申请日：2003-04-11
申请人： ISIS PHARMACEUTICALS, INC. , SONG, Quanlai , ROSS, Bruce
发明人： SONG, Quanlai , ROSS, Bruce
IPC分类号： C07F09/28
摘要： A scalable process for purification of phosphorodiamidite includes steps of solubilizing a crude phosphorodiamidite in an apolar organic solvent, contacting the non-polar organic solvent with a polar phase comprising a polar organic solvent to remove impurities from the solubilized phosphorodiamidite, and removing the non-polar organic solvent from the phosphorodiamidite.

7. 发明申请

WO2004039469A3 PROCESS OF PURIFYING PHOSPHORAMIDITES 审中-公开
公开(公告)号：WO2004039469A3
公开(公告)日：2004-05-13
申请号：PCT/US2003/031794
申请日：2003-10-07
申请人： ISIS PHARMACEUTICALS, INC. , ROSS, Bruce , SONG, Quanlai
发明人： ROSS, Bruce , SONG, Quanlai
IPC分类号： C07H21/04
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.

8. 发明申请

WO2002057287A3 NUCLEOSIDE DERIVATIVES AS INHIBITORS OF RNA-DEPENDENT RNA VIRAL POLYMERASE 审中-公开
公开(公告)号：WO2002057287A3
公开(公告)日：2002-07-25
申请号：PCT/US2002/003086
申请日：2002-01-18
申请人： MERCK & CO., INC. , ISIS PHARMACEUTICALS, INC. , CARROLL, Steven, S. , MACCOSS, Malcolm , OLSEN, David, B. , BHAT, Balkrishen , BHAT, Neelima , COOK, Phillip Dan , ELDRUP, Anne, B. , PRAKASH, Thazha, P. , PRHAVC, Marija , SONG, Quanlai
发明人： CARROLL, Steven, S. , MACCOSS, Malcolm , OLSEN, David, B. , BHAT, Balkrishen , BHAT, Neelima , COOK, Phillip Dan , ELDRUP, Anne, B. , PRAKASH, Thazha, P. , PRHAVC, Marija , SONG, Quanlai
IPC分类号： C07H19/14
摘要： The present invention provides nucleoside compounds and certain derivatives thereof which are inhibitors of RNA-dependent RNA viral polymerase. These compounds are inhibitors of RNA-dependent RNA viral replication and are useful for the treatment of RNA-dependent RNA viral infection. They are particularly useful as inhibitors of hepatitis C virus (HCV) NS5B polymerase, as inhibitors of HCV replication, and/or for the treatment of hepatitis C infection. The invention also describes pharmaceutical compositions containing such nucleoside compounds alone or in combination with other agents active against RNA-dependent RNA viral infection, in particular HCV infection. Also disclosed are methods of inhibiting RNA-dependent RNA polymerase, inhibiting RNA-dependent RNA viral replication, and/or treating RNA-dependent RNA viral infection with the nucleoside compounds of the present invention.

9. 发明公开

EP1492800A2 PROCESS FOR MANUFACTURING PURIFIED PHOSPHORODIAMIDITE 审中-公开
标题翻译：工艺生产纯化PHOSPHORDIAMIDIT
公开(公告)号：EP1492800A2
公开(公告)日：2005-01-05
申请号：EP03738877.4
申请日：2003-04-11
申请人： ISIS PHARMACEUTICALS, INC.
发明人： SONG, Quanlai , ROSS, Bruce
IPC分类号： C07F9/28
CPC分类号： C07H19/20 , C07F9/025 , C07F9/2408 , C07F9/65515 , C07H19/10 , Y02P20/582
摘要： A scalable process for purification of phosphorodiamidite includes steps of solubilizing a crude phosphorodiamidite in an apolar organic solvent, contacting the non-polar organic solvent with a polar phase comprising a polar organic solvent to remove impurities from the solubilized phosphorodiamidite, and removing the non-polar organic solvent from the phosphorodiamidite.

10. 发明公开

EP1311526A1 PROCESSES FOR THE PREPARATION OF OLIGONUCLEOTIDES 审中-公开
标题翻译：制备寡核苷酸的过程
公开(公告)号：EP1311526A1
公开(公告)日：2003-05-21
申请号：EP01959753.3
申请日：2001-08-16
申请人： ISIS PHARMACEUTICALS, INC.
发明人： SANGHVI, Yogesh, S. , SONG, Quanlai
IPC分类号： C07H21/00 , C07H19/00
CPC分类号： C07H21/00 , C07H19/04
摘要： The present invention discloses methods for synthesizing oligomeric compounds. The methods include a modified phosphoramidite protocol wherein the oxidation and capping steps are combined into a single step. The methods result in increased efficiency and are especially amenable to the large scale synthesis of oligomeric compounds.
摘要翻译：本发明公开了合成寡聚化合物的方法。该方法包括修改的亚磷酰胺方案，其中氧化和封端步骤组合成单一步骤。这些方法导致效率提高，特别适用于大规模合成低聚化合物。

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