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公开(公告)号：US20130203836A1
公开(公告)日：2013-08-08
申请号：US13638891
申请日：2011-03-31
IPC分类号： C12N15/113 , C07H19/16 , A61K48/00 , C07H19/06
CPC分类号： C12N15/113 , A61K48/00 , C07H19/06 , C07H19/067 , C07H19/16
摘要： The present invention provides nucleosides of formula (1) and oligonucleotides comprising at least on nucleoside of formula (2):Formula (1) and Formula (2). Another aspect of the invention relates to a method of inhibiting the expression of a gene in call, the method comprising (a) contacting an oligonucleotide of the invention with the cell; and (b) maintaining the cell from step (a) for a time sufficient to obtain degradation of the mRNA of the target gene.
摘要翻译： 本发明提供式（1）的核苷和至少包含式（2）核苷的寡核苷酸：式（1）和式（2）。 本发明的另一方面涉及一种抑制基因表达的方法，所述方法包括（a）使本发明的寡核苷酸与细胞接触; 和（b）将来自步骤（a）的细胞维持足以获得靶基因的mRNA降解的时间。
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公开(公告)号：US20130156845A1
公开(公告)日：2013-06-20
申请号：US13643940
申请日：2011-04-29
申请人： Muthiah Manoharan , Sayda Elbashir , Kallanthottathil G. Rajeev , Thazha P. Prakash , Walter F. Lima , Eric E. Swayze
发明人： Muthiah Manoharan , Sayda Elbashir , Kallanthottathil G. Rajeev , Thazha P. Prakash , Walter F. Lima , Eric E. Swayze
IPC分类号： A61K9/127 , A61K31/7088
CPC分类号： A61K9/1272 , A61K9/1275 , A61K31/7088 , C12N15/111 , C12N15/88 , C12N2310/11 , C12N2320/32
摘要： The present invention provides compositions comprising a nucleic acid lipid particle and an oligomeric compound and uses thereof. In certain embodiments, such compositions are useful as antisense compounds. Certain such antisense compounds are useful as RNase H antisense compounds or as RNAi compounds.
摘要翻译： 本发明提供了包含核酸脂质颗粒和寡聚化合物的组合物及其用途。 在某些实施方案中，这样的组合物可用作反义化合物。 某些这样的反义化合物可用作RNase H反义化合物或作为RNAi化合物。
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63.发明申请MODIFIED 5' DIPHOSPHATE NUCLEOSIDES AND OLIGOMERIC COMPOUNDS PREPARED THEREFROM 有权改良的5'二磷酸核苷和其制备的低聚物公开(公告)号：US20130109850A1
公开(公告)日：2013-05-02
申请号：US13642804
申请日：2011-04-26
申请人： Thazha P. Prakash , Punit P. Seth , Muthiah Manoharan , Eric E. Swayze , Kallanthottathil G. Rajeev , Ivan Zlatev
发明人： Thazha P. Prakash , Punit P. Seth , Muthiah Manoharan , Eric E. Swayze , Kallanthottathil G. Rajeev , Ivan Zlatev
IPC分类号： C07H19/10 , C12N15/113
CPC分类号： C07H19/10 , C12N15/113
摘要： Provided herein are modified 5′ diphosphate nucleosides and oligomeric compounds prepared therefrom. More particularly, modified 5′ diphosphate nucleosides are provided that can be further modified at the 2′ and 5′ positions. In some embodiments, the oligomeric compounds provided herein are expected to hybridize to a portion of a target RNA resulting in loss of normal function of the target RNA. The oligomeric compounds are also expected to be useful as primers and probes in diagnostic applications.
摘要翻译： 本文提供修饰的5'二磷酸核苷和由其制备的低聚化合物。 更具体地，提供修饰的5'-二磷酸核苷，其可以在2'和5'位置进一步修饰。 在一些实施方案中，预期本文提供的寡聚化合物与靶RNA的一部分杂交，导致靶RNA的正常功能丧失。 还预期寡聚化合物可用作诊断应用中的引物和探针。
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公开(公告)号：US08426378B2
公开(公告)日：2013-04-23
申请号：US12922832
申请日：2009-03-19
CPC分类号： C12N15/113 , A61K31/7042 , A61K31/7052 , A61K31/7088 , A61K31/712 , A61K31/7125 , C07H19/10 , C07H21/04 , C12N2310/11 , C12N2310/3125 , C12N2310/314 , C12N2310/316 , C12N2310/3231
摘要： The present disclosure provides tricyclic nucleosides, oligomeric compounds comprising at least one of the tricyclic nucleosides and methods of using the oligomeric compounds. The methods provided herein include contacting a cell or administering to an animal at least one of the oligomeric compounds. In certain embodiments, the oligomeric compounds hybridize to a portion of a target RNA resulting in loss of normal function of the target RNA.
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公开(公告)号：US08278425B2
公开(公告)日：2012-10-02
申请号：US12602074
申请日：2008-05-22
摘要： Provided herein are bicyeMc nucleosides comprising a substituted amino group in the bridge, oligomeric compounds having at least one of these bicyclic nucleosides and methods of using the oligomeric compounds. The bicyclic nucleosides comprising a substituted amino group in the bridge are useful for enhancing properties of oligomeric compounds including nuclease resistance, in certain embodiments, the oligomeric compounds hybridize to a portion of a target RNA resulting in loss of normal function of the target RNA.
摘要翻译： 本文提供了包含桥中取代的氨基的双体核苷，具有这些双环核苷中的至少一种的低聚化合物和使用低聚化合物的方法。 在桥中包含取代的氨基的双环核苷可用于增强包括核酸酶抗性的寡聚化合物的性质，在某些实施方案中，寡聚化合物与目标RNA的一部分杂交导致靶RNA的正常功能丧失。
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公开(公告)号：US06914148B2
公开(公告)日：2005-07-05
申请号：US10247893
申请日：2002-09-20
IPC分类号： C07H21/02 , A61K31/712 , A61K48/00 , A61P35/00 , C07C335/38 , C07F9/24 , C07H21/00 , C07H21/04 , C07F9/02
CPC分类号： C07H21/00
摘要： The present invention provides oligomers which are specifically hybridizable with a selected sequence of RNA or DNA wherein at least one of the nucleoside moieties of the oligomer is modified to include a guanidinium group. These oligomers are useful for diagnostic, therapeutic and investigative purposes.
摘要翻译： 本发明提供了与选定的RNA或DNA序列特异性杂交的寡聚体，其中低聚物的至少一个核苷部分被修饰成包括胍基。 这些低聚物可用于诊断，治疗和调查目的。
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公开(公告)号：US06403779B1
公开(公告)日：2002-06-11
申请号：US09227782
申请日：1999-01-08
IPC分类号： C07H2102
摘要： Methods for the regioselective alkylation at the 2′-hydroxy position over the 3′-hydroxy position of nucleosides and nucleoside analogs, forming 2′-O-ester modified compounds, are disclosed. Reduction and derivatization of the 2′-O-ester provides 2′-O-modified nucleosides and nucleoside analogs useful for the synthesis of oligomeric compounds having improved hybridization affinity and nuclease resistance.
摘要翻译： 公开了在形成2'-O-酯改性化合物的核苷和核苷类似物的3'-羟基位置上2'-羟基位置选择性烷基化的方法。 2'-O-酯的还原和衍生化提供可用于合成具有改善的杂交亲和性和核酸酶抗性的寡聚化合物的2'-O-修饰的核苷和核苷类似物。
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公开(公告)号：US06624294B2
公开(公告)日：2003-09-23
申请号：US10123597
申请日：2002-04-16
IPC分类号： C07H2102
摘要： Methods for the regioselective alkylation at the 2′-hydroxy position over the 3′-hydroxy position of nucleosides and nucleoside analogs, forming 2′-O-ester modified compounds, are disclosed. Reduction and derivatization of the 2′-O-ester provides 2′-O-modified nucleosides and nucleoside analogs useful for the synthesis of oligomeric compounds having improved hybridization affinity and nuclease resistance.
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公开(公告)号：US06147200A
公开(公告)日：2000-11-14
申请号：US378568
申请日：1999-08-19
申请人： Muthiah Manoharan , Andrew M. Kawasaki , Phillip Dan Cook , Allister S. Fraser , Thazha P. Prakash
发明人： Muthiah Manoharan , Andrew M. Kawasaki , Phillip Dan Cook , Allister S. Fraser , Thazha P. Prakash
IPC分类号： C12N15/09 , A61K31/7068 , A61K31/7072 , A61K31/7076 , A61K31/708 , A61K31/712 , A61K38/00 , A61K48/00 , A61P43/00 , C07H19/04 , C07H19/067 , C07H19/10 , C07H19/167 , C07H19/20 , C07H21/00 , C07H21/02
摘要： Nucleosidic monomers and oligomeric compounds prepared therefrom are provided. Also provided is a novel method of deprotection of oligomeric compounds. Oligomeric compounds having at least one 2'-O-acetamido modified nucleosidic monomer are expected to have increased nuclease resistance and binding affinity to a complementary strand of nucleic acid. Such oligomeric compounds are useful for diagnostics and other research purposes, for modulating the expression of a protein in organisms, and for the diagnosis, detection and treatment of other conditions responsive to oligonucleotide therapeutics.
摘要翻译： 提供了由其制备的核苷单体和寡聚化合物。 还提供了低聚化合物的脱保护的新方法。 具有至少一个2'-O-乙酰氨基修饰的核糖单体的低聚化合物预期具有增加的核酸酶抗性和与核酸互补链的结合亲和力。 这样的低聚化合物可用于诊断和其他研究目的，用于调节生物体中的蛋白质的表达，以及用于诊断，检测和治疗对寡核苷酸治疗剂有反应的其它病症。
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公开(公告)号：US06921812B1
公开(公告)日：2005-07-26
申请号：US10058740
申请日：2002-01-28
IPC分类号： C07H19/06 , C12N15/113 , C07H21/00 , C07H21/02 , C07H21/04
CPC分类号： C12N15/113 , C07H19/06 , C12N2310/321 , C12N2310/3527
摘要： 2′-O-(2-Methylthioethyl), has been incorporated into oligonucleotides and evaluated for antisense properties in comparison with the known 2′-O-(2-methoxyethyl) 2′-O-MOE modification. The 2′-O-MTE modified oligonucleotides exhibit improved binding to human serum albumin compared with the 2′-O-MOE modified oligonucleotides and maintain high binding affinity to target RNA.
摘要翻译： 与已知的2'-O-（2-甲氧基乙基）2'-O-MOE修饰相比，已经将2'-O-（2-甲硫基乙基）引入寡核苷酸并评估其反义性质。 与2'-O-MOE修饰的寡核苷酸相比，2'-O-MTE修饰的寡核苷酸显示出与人血清白蛋白的改善的结合，并保持与靶RNA的高结合亲和力。
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