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1.发明申请公开(公告)号：US20120035115A1
公开(公告)日：2012-02-09
申请号：US13120389
申请日：2009-09-23
申请人： Muthiah Manoharan , Kallanthottathil G. Rajeev , Takeshi Yamada , David Butler , K. Narayanannair Jayaprakash , Muthusamy Jayraman , Shigeo Matsuda , Rajendra K. Pandey , Chang Geng Peng
发明人： Muthiah Manoharan , Kallanthottathil G. Rajeev , Takeshi Yamada , David Butler , K. Narayanannair Jayaprakash , Muthusamy Jayraman , Shigeo Matsuda , Rajendra K. Pandey , Chang Geng Peng
IPC分类号： A61K38/14 , C07H19/10 , C07F9/6561 , C07H21/02 , A61K31/7072 , A61K31/675 , C07H1/00 , A61P31/12 , A61P31/04 , A61P33/00 , A61P35/00 , A61P37/08 , A61P37/06 , A61P37/04 , C07K9/00 , A61K31/7088
CPC分类号： C12N15/113 , A61K31/713 , A61K47/544 , A61K47/64 , C07H21/00 , C12N2310/14 , C12N2310/141 , C12N2310/3513 , C12N2310/3515 , H04L65/602 , H04L67/36 , Y02A50/465
摘要： The invention features compounds of formula I or II: In one embodiment, the invention relates compounds and processes for conjugating ligand to oligonucleotide. The invention further relates to methods for treating various disorders and diseases such as viral infections, bacterial infections, parasitic infections, cancers, allergies, autoimmune diseases, immunodeficiencies and immunosuppression.
摘要翻译： 本发明的特征在于式I或II化合物：在一个实施方案中，本发明涉及将配体与寡核苷酸缀合的化合物和方法。 本发明还涉及治疗各种病症和疾病如病毒感染，细菌感染，寄生虫感染，癌症，过敏症，自身免疫疾病，免疫缺陷和免疫抑制的方法。
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2.发明授权公开(公告)号：US08962580B2
公开(公告)日：2015-02-24
申请号：US13120389
申请日：2009-09-23
申请人： Muthiah Manoharan , Kallanthottathil G. Rajeev , Takeshi Yamada , David Butler , Narayanannair K. Jayaprakash , Muthusamy Jayaraman , Shigeo Matsuda , Rajendra K. Pandey , Chang Geng Peng
发明人： Muthiah Manoharan , Kallanthottathil G. Rajeev , Takeshi Yamada , David Butler , Narayanannair K. Jayaprakash , Muthusamy Jayaraman , Shigeo Matsuda , Rajendra K. Pandey , Chang Geng Peng
CPC分类号： C12N15/113 , A61K31/713 , A61K47/544 , A61K47/64 , C07H21/00 , C12N2310/14 , C12N2310/141 , C12N2310/3513 , C12N2310/3515 , H04L65/602 , H04L67/36 , Y02A50/465
摘要： The invention features compounds of formula I or II: In one embodiment, the invention relates compounds and processes for conjugating ligand to oligonucleotide. The invention further relates to methods for treating various disorders and diseases such as viral infections, bacterial infections, parasitic infections, cancers, allergies, autoimmune diseases, immunodeficiencies and immunosuppression.
摘要翻译： 本发明的特征在于式I或II化合物：在一个实施方案中，本发明涉及将配体与寡核苷酸缀合的化合物和方法。 本发明还涉及治疗各种病症和疾病如病毒感染，细菌感染，寄生虫感染，癌症，过敏症，自身免疫疾病，免疫缺陷和免疫抑制的方法。
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公开(公告)号：US20120046478A1
公开(公告)日：2012-02-23
申请号：US13211094
申请日：2011-08-16
申请人： Muthiah MANOHARAN , Kallanthottathil G. Rajeev , Akin Akinc , Narayanannair K. Jayaprakash , Muthusamy Jayraman , Martin Maier
发明人： Muthiah MANOHARAN , Kallanthottathil G. Rajeev , Akin Akinc , Narayanannair K. Jayaprakash , Muthusamy Jayraman , Martin Maier
IPC分类号： C07C271/16 , C07C235/74 , C07C69/40
CPC分类号： C07C219/06 , A61K9/1272 , A61K9/1273 , A61K31/325 , A61K47/34 , C07C209/78 , C07C233/36 , C07C271/10 , C07C323/25
摘要： Compositions and methods useful in administering nucleic acid based therapies, for example association complexes such as liposomes and lipoplexes are described.
摘要翻译： 描述了用于施用基于核酸的疗法，例如缔合复合物如脂质体和脂质复合物的组合物和方法。
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公开(公告)号：US08034376B2
公开(公告)日：2011-10-11
申请号：US12056230
申请日：2008-03-26
申请人： Muthiah Manoharan , Kallanthottathil G. Rajeev , Akin Akinc , Narayanannair K. Jayaprakash , Muthusamy Jayraman , Martin Maier
发明人： Muthiah Manoharan , Kallanthottathil G. Rajeev , Akin Akinc , Narayanannair K. Jayaprakash , Muthusamy Jayraman , Martin Maier
IPC分类号： A61K9/127
CPC分类号： C07C219/06 , A61K9/1272 , A61K9/1273 , A61K31/325 , A61K47/34 , C07C209/78 , C07C233/36 , C07C271/10 , C07C323/25
摘要： Compositions and methods useful in administering nucleic acid based therapies, for example association complexes such as liposomes and lipoplexes are described.
摘要翻译： 描述了用于施用基于核酸的疗法，例如缔合复合物如脂质体和脂质复合物的组合物和方法。
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公开(公告)号：US20090023673A1
公开(公告)日：2009-01-22
申请号：US12056230
申请日：2008-03-26
申请人： Muthiah Manoharan , Kallanthottathil G. Rajeev , Akin Akinc , Narayanannair K. Jayaprakash , Muthusamy Jayraman , Martin Maier
发明人： Muthiah Manoharan , Kallanthottathil G. Rajeev , Akin Akinc , Narayanannair K. Jayaprakash , Muthusamy Jayraman , Martin Maier
IPC分类号： A61K47/14 , A61K31/7088
CPC分类号： C07C219/06 , A61K9/1272 , A61K9/1273 , A61K31/325 , A61K47/34 , C07C209/78 , C07C233/36 , C07C271/10 , C07C323/25
摘要： Compositions and methods useful in administering nucleic acid based therapies, for example association complexes such as liposomes and lipoplexes are described.
摘要翻译： 描述了用于施用基于核酸的疗法，例如缔合复合物如脂质体和脂质复合物的组合物和方法。
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6.发明申请SINGLE-STRANDED AND DOUBLE-STRANDED OLIGONUCLEOTIDES COMPRISING A METAL-CHELATING LIGAND 审中-公开包含金属链条的单条和双拉链的双绞线公开(公告)号：US20110250138A1
公开(公告)日：2011-10-13
申请号：US12671677
申请日：2008-07-30
申请人： Yupeng Fan , Martin Maier , Rajendra K. Pandey , Muthiah Manoharan , Kallanthottathil G. Rajeev
发明人： Yupeng Fan , Martin Maier , Rajendra K. Pandey , Muthiah Manoharan , Kallanthottathil G. Rajeev
CPC分类号： A61K49/0017 , A61K49/0052 , A61K49/085 , A61K49/126
摘要： The invention provides modified oligonucleotides of formula (I), comprising at least one metal chelator which provides a powerful tool for study of the pharmacokinetics of siRNA and its correlation with in vivo activity. The chelated metals provide luminescent properties enable detection of the oligonucleotides through the use of time-resolved fluorescent quenching based on energy transfer from the metal ion to a nonfluorescent quencher which can be used as non-isotopic labels of oligonucleotides for diagnostics and evaluation of cellular uptake.
摘要翻译： 本发明提供了修饰的式（I）寡核苷酸，其包含至少一种金属螯合剂，其提供用于研究siRNA的药代动力学的强大工具及其与体内活性的相关性。 螯合金属提供了通过使用基于从金属离子到非荧光猝灭剂的能量转移的时间分辨荧光猝灭来检测寡核苷酸，其可以用作用于诊断和评价细胞摄取的寡核苷酸的非同位素标记 。
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公开(公告)号：US08058448B2
公开(公告)日：2011-11-15
申请号：US12351605
申请日：2009-01-09
申请人： Muthiah Manoharan , Michael E. Jung , Kallanthottathil G. Rajeev , Rajendra K. Pandey , Gang Wang
发明人： Muthiah Manoharan , Michael E. Jung , Kallanthottathil G. Rajeev , Rajendra K. Pandey , Gang Wang
IPC分类号： C07D285/01 , C07H21/00
摘要： The present invention relates to processes and reagents for oligonucleotide synthesis and purification. One aspect of the present invention relates to compounds useful for activating phosphoramidites in oligonucleotide synthesis. Another aspect of the present invention relates to a method of preparing oligonucleotides via the phosphoramidite method using an activator of the invention. Another aspect of the present invention relates to sulfur-transfer agents. In a preferred embodiment, the sulfur-transfer agent is a 3-amino-1,2,4-dithiazolidine-5-one. Another aspect of the present invention relates to a method of preparing a phosphorothioate by treating a phosphite with a sulfur-transfer reagent of the invention. In a preferred embodiment, the sulfur-transfer agent is a 3-amino-1,2,4-dithiazolidine-5-one. Another aspect of the present invention relates to compounds that scavenge acrylonitrile produced during the deprotection of phosphate groups bearing ethylnitrile protecting groups. In a preferred embodiment, the acrylonitrile scavenger is a polymer-bound thiol. Another aspect of the present invention relates to agents used to oxidize a phosphite to a phosphate. In a preferred embodiment, the oxidizing agent is sodium chlorite, chloramine, or pyridine-N-oxide. Another aspect of the present invention relates to methods of purifying an oligonucleotide by annealing a first single-stranded oligonucleotide and second single-stranded oligonucleotide to form a double-stranded oligonucleotide; and subjecting the double-stranded oligonucleotide to chromatographic purification. In a preferred embodiment, the chromatographic purification is high-performance liquid chromatography.
摘要翻译： 本发明涉及寡核苷酸合成和纯化的方法和试剂。 本发明的一个方面涉及可用于在寡核苷酸合成中活化亚磷酰胺的化合物。 本发明的另一方面涉及使用本发明的活化剂通过亚磷酰胺方法制备寡核苷酸的方法。 本发明的另一方面涉及硫转移剂。 在优选的实施方案中，硫转移剂是3-氨基-1,2,4-二噻唑烷-5-酮。 本发明的另一方面涉及通过用本发明的硫转移试剂处理亚磷酸酯制备硫代磷酸酯的方法。 在优选的实施方案中，硫转移剂是3-氨基-1,2,4-二噻唑烷-5-酮。 本发明的另一方面涉及清除在带有乙腈基保护基团的磷酸酯基团去保护过程中产生的丙烯腈的化合物。 在优选的实施方案中，丙烯腈清除剂是聚合物结合的硫醇。 本发明的另一方面涉及用于将亚磷酸盐氧化成磷酸盐的试剂。 在优选的实施方案中，氧化剂是亚氯酸钠，氯胺或吡啶-N-氧化物。 本发明的另一方面涉及通过退火第一单链寡核苷酸和第二单链寡核苷酸来纯化寡核苷酸以形成双链寡核苷酸的方法; 并对双链寡核苷酸进行色谱纯化。 在优选的实施方案中，色谱纯化是高效液相色谱法。
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公开(公告)号：US08431693B2
公开(公告)日：2013-04-30
申请号：US13036788
申请日：2011-02-28
申请人： Muthiah Manoharan , Michael F. Jung , Kallanthottathil G. Rajeev , Rajendra K. Pandey , Gang Wang
发明人： Muthiah Manoharan , Michael F. Jung , Kallanthottathil G. Rajeev , Rajendra K. Pandey , Gang Wang
摘要： The present invention relates to processes and reagents for oligonucleotide synthesis and purification. One aspect of the present invention relates to compounds useful for activating phosphoramidites in oligonucleotide synthesis. Another aspect of the present invention relates to a method of preparing oligonucleotides via the phosphoramidite method using an activator of the invention. Another aspect of the present invention relates to sulfur-transfer agents. In a preferred embodiment, the sulfur-transfer agent is a 3-amino-1,2,4-dithiazolidine-5-one. Another aspect of the present invention relates to a method of preparing a phosphorothioate by treating a phosphite with a sulfur-transfer reagent of the invention. In a preferred embodiment, the sulfur-transfer agent is a 3-amino-1,2,4-dithiazolidine-5-one. Another aspect of the present invention relates to compounds that scavenge acrylonitrile produced during the deprotection of phosphate groups bearing ethylnitrile protecting groups. In a preferred embodiment, the acrylonitrile scavenger is a polymer-bound thiol. Another aspect of the present invention relates to agents used to oxidize a phosphite to a phosphate. In a preferred embodiment, the oxidizing agent is sodium chlorite, chloroamine, or pyridine-N-oxide. Another aspect of the present invention relates to methods of purifying an oligonucleotide by annealing a first single-stranded oligonucleotide and second single-stranded oligonucleotide to form a double-stranded oligonucleotide; and subjecting the double-stranded oligonucleotide to chromatographic purification. In a preferred embodiment, the chromatographic purification is high-performance liquid chromatography.
摘要翻译： 本发明涉及寡核苷酸合成和纯化的方法和试剂。 本发明的一个方面涉及可用于在寡核苷酸合成中活化亚磷酰胺的化合物。 本发明的另一方面涉及使用本发明的活化剂通过亚磷酰胺方法制备寡核苷酸的方法。 本发明的另一方面涉及硫转移剂。 在优选的实施方案中，硫转移剂是3-氨基-1,2,4-二噻唑烷-5-酮。 本发明的另一方面涉及通过用本发明的硫转移试剂处理亚磷酸酯制备硫代磷酸酯的方法。 在优选的实施方案中，硫转移剂是3-氨基-1,2,4-二噻唑烷-5-酮。 本发明的另一方面涉及清除在带有乙腈基保护基团的磷酸酯基团去保护过程中产生的丙烯腈的化合物。 在优选的实施方案中，丙烯腈清除剂是聚合物结合的硫醇。 本发明的另一方面涉及用于将亚磷酸盐氧化成磷酸盐的试剂。 在优选的实施方案中，氧化剂是亚氯酸钠，氯胺或吡啶-N-氧化物。 本发明的另一方面涉及通过退火第一单链寡核苷酸和第二单链寡核苷酸来纯化寡核苷酸以形成双链寡核苷酸的方法; 并对双链寡核苷酸进行色谱纯化。 在优选的实施方案中，色谱纯化是高效液相色谱法。
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公开(公告)号：US20090005549A1
公开(公告)日：2009-01-01
申请号：US12050633
申请日：2008-03-18
申请人： Muthiah Manoharan , Michael E. Jung , Kallanthottathil G. Rajeev , Rajendra K. Pandey , Gang Wang
发明人： Muthiah Manoharan , Michael E. Jung , Kallanthottathil G. Rajeev , Rajendra K. Pandey , Gang Wang
IPC分类号： C07H19/00
摘要： The present invention relates to processes and reagents for oligonucleotide synthesis and purification. One aspect of the present invention relates to compounds useful for activating phosphoramidites in oligonucleotide synthesis. Another aspect of the present invention relates to a method of preparing oligonucleotides via the phosphoramidite method using an activator of the invention. Another aspect of the present invention relates to sulfur-transfer agents. In a preferred embodiment, the sulfur-transfer agent is a 3-amino-1,2,4-dithiazolidine-5-one. Another aspect of the present invention relates to a method of preparing a phosphorothioate by treating a phosphite with a sulfur-transfer reagent of the invention. In a preferred embodiment, the sulfur-transfer agent is a 3-amino-1,2,4-dithiazolidine-5-one. Another aspect of the present invention relates to compounds that scavenge acrylonitrile produced during the deprotection of phosphate groups bearing ethylnitrile protecting groups. In a preferred embodiment, the acrylonitrile scavenger is a polymer-bound thiol. Another aspect of the present invention relates to agents used to oxidize a phosphite to a phosphate. In a preferred embodiment, the oxidizing agent is sodium chlorite, chloroamine, or pyridine-N-oxide. Another aspect of the present invention relates to methods of purifying an oligonucleotide by annealing a first single-stranded oligonucleotide and second single-stranded oligonucleotide to form a double-stranded oligonucleotide; and subjecting the double-stranded oligonucleotide to chromatographic purification. In a preferred embodiment, the chromatographic purification is high-performance liquid chromatography.
摘要翻译： 本发明涉及寡核苷酸合成和纯化的方法和试剂。 本发明的一个方面涉及可用于在寡核苷酸合成中活化亚磷酰胺的化合物。 本发明的另一方面涉及使用本发明的活化剂通过亚磷酰胺方法制备寡核苷酸的方法。 本发明的另一方面涉及硫转移剂。 在优选的实施方案中，硫转移剂是3-氨基-1,2,4-二噻唑烷-5-酮。 本发明的另一方面涉及通过用本发明的硫转移试剂处理亚磷酸酯制备硫代磷酸酯的方法。 在优选的实施方案中，硫转移剂是3-氨基-1,2,4-二噻唑烷-5-酮。 本发明的另一方面涉及清除在带有乙腈基保护基团的磷酸酯基团去保护过程中产生的丙烯腈的化合物。 在优选的实施方案中，丙烯腈清除剂是聚合物结合的硫醇。 本发明的另一方面涉及用于将亚磷酸盐氧化成磷酸盐的试剂。 在优选的实施方案中，氧化剂是亚氯酸钠，氯胺或吡啶-N-氧化物。 本发明的另一方面涉及通过退火第一单链寡核苷酸和第二单链寡核苷酸来纯化寡核苷酸以形成双链寡核苷酸的方法; 并对双链寡核苷酸进行色谱纯化。 在优选的实施方案中，色谱纯化是高效液相色谱法。
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公开(公告)号：US08063198B2
公开(公告)日：2011-11-22
申请号：US12050633
申请日：2008-03-18
申请人： Muthiah Manoharan , Michael E. Jung , Kallanthottathil G. Rajeev , Rajendra K. Pandey , Gang Wang
发明人： Muthiah Manoharan , Michael E. Jung , Kallanthottathil G. Rajeev , Rajendra K. Pandey , Gang Wang
摘要： The present invention relates to processes and reagents for oligonucleotide synthesis and purification. One aspect of the present invention relates to compounds useful for activating phosphoramidites in oligonucleotide synthesis. Another aspect of the present invention relates to a method of preparing oligonucleotides via the phosphoramidite method using an activator of the invention. Another aspect of the present invention relates to sulfur-transfer agents. In a preferred embodiment, the sulfur-transfer agent is a 3-amino-1,2,4-dithiazolidine-5-one. Another aspect of the present invention relates to a method of preparing a phosphorothioate by treating a phosphite with a sulfur-transfer reagent of the invention. In a preferred embodiment, the sulfur-transfer agent is a 3-amino-1,2,4-dithiazolidine-5-one. Another aspect of the present invention relates to compounds that scavenge acrylonitrile produced during the deprotection of phosphate groups bearing ethylnitrile protecting groups. In a preferred embodiment, the acrylonitrile scavenger is a polymer-bound thiol. Another aspect of the present invention relates to agents used to oxidize a phosphite to a phosphate. In a preferred embodiment, the oxidizing agent is sodium chlorite, chloroamine, or pyridine-N-oxide. Another aspect of the present invention relates to methods of purifying an oligonucleotide by annealing a first single-stranded oligonucleotide and second single-stranded oligonucleotide to form a double-stranded oligonucleotide; and subjecting the double-stranded oligonucleotide to chromatographic purification. In a preferred embodiment, the chromatographic purification is high-performance liquid chromatography.
摘要翻译： 本发明涉及用于寡核苷酸合成和纯化的方法和试剂。 本发明的一个方面涉及可用于在寡核苷酸合成中活化亚磷酰胺的化合物。 本发明的另一方面涉及使用本发明的活化剂通过亚磷酰胺方法制备寡核苷酸的方法。 本发明的另一方面涉及硫转移剂。 在优选的实施方案中，硫转移剂是3-氨基-1,2,4-二噻唑烷-5-酮。 本发明的另一方面涉及通过用本发明的硫转移试剂处理亚磷酸酯制备硫代磷酸酯的方法。 在优选的实施方案中，硫转移剂是3-氨基-1,2,4-二噻唑烷-5-酮。 本发明的另一方面涉及清除在带有乙腈基保护基团的磷酸酯基团去保护过程中产生的丙烯腈的化合物。 在优选的实施方案中，丙烯腈清除剂是聚合物结合的硫醇。 本发明的另一方面涉及用于将亚磷酸盐氧化成磷酸盐的试剂。 在优选的实施方案中，氧化剂是亚氯酸钠，氯胺或吡啶-N-氧化物。 本发明的另一方面涉及通过退火第一单链寡核苷酸和第二单链寡核苷酸来纯化寡核苷酸以形成双链寡核苷酸的方法; 并对双链寡核苷酸进行色谱纯化。 在优选的实施方案中，色谱纯化是高效液相色谱法。
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