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61. 发明授权

US09725479B2 5′-end derivatives 有权
公开(公告)号：US09725479B2
公开(公告)日：2017-08-08
申请号：US13696796
申请日：2011-04-22
申请人： Muthiah Manoharan , Kallanthottathil G. Rajeev , Ivan Zlatev , Eric E. Swayze , Thazha P. Prakash , Walter F. Lima
发明人： Muthiah Manoharan , Kallanthottathil G. Rajeev , Ivan Zlatev , Eric E. Swayze , Thazha P. Prakash , Walter F. Lima
IPC分类号： C07H17/02 , C07H19/067 , C07H21/02 , C12N15/113
CPC分类号： C07H17/02 , C07H19/067 , C07H21/02 , C12N15/113 , C12N15/1137 , C12N2310/14 , C12N2310/315 , C12N2310/321 , C12N2310/322 , C12N2310/344 , C12N2310/3521 , C12N2310/3525
摘要： The present invention provides compounds of formula (1). 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.

62. 发明授权

US08470988B2 Single-stranded and double-stranded oligonucleotides comprising a 2-arylpropyl moiety 有权
标题翻译：包含2-芳基丙基部分的单链和双链寡核苷酸
公开(公告)号：US08470988B2
公开(公告)日：2013-06-25
申请号：US12604897
申请日：2009-10-23
申请人： Muthiah Manoharan , Kallanthottathil G. Rajeev , Venkitasamy Kesavan
发明人： Muthiah Manoharan , Kallanthottathil G. Rajeev , Venkitasamy Kesavan
IPC分类号： C07H21/02 , C07H21/04
CPC分类号： C07H21/04 , C07H21/02 , C12N15/111 , C12N2310/14 , C12N2310/351 , C12N2320/51
摘要： The present invention provides single-stranded and double-stranded oligonucleotides comprising at least one aralkyl ligand that improvise the pharmacokinetic properties of the oligonucleotide. The aralkyl ligands of the present invention include naproxen, ibuprofen, and derivatives thereof. The present invention also provides method for modulating gene expression using the modified oligonucleotide compounds and compositions comprising those modified oligonucleotides.
摘要翻译：本发明提供了包含至少一种能够提高寡核苷酸的药代动力学性质的芳烷基配体的单链和双链寡核苷酸。本发明的芳烷基配体包括萘普生，布洛芬及其衍生物。本发明还提供了使用修饰的寡核苷酸化合物和包含那些经修饰的寡核苷酸的组合物调节基因表达的方法。

63. 发明申请

US20130130378A1 OLIGONUCLEOTIDES COMPRISING ACYCLIC AND ABASIC NUCLEOSIDES AND ANALOGS 审中-公开
标题翻译：包含ACYCLIC和ABASIC NUCLEOSIDES和模拟物的寡核苷酸
公开(公告)号：US20130130378A1
公开(公告)日：2013-05-23
申请号：US13642772
申请日：2011-04-22
申请人： Muthiah Manoharan , Kallanthottathil G. Rajeev , Jeremy Lackey , Narayanannair K. Jayaprakash
发明人： Muthiah Manoharan , Kallanthottathil G. Rajeev , Jeremy Lackey , Narayanannair K. Jayaprakash
IPC分类号： C07H21/02 , C07F9/655 , C07H19/20 , C07F9/6512 , C07F9/6558
CPC分类号： C07H21/02 , C07F9/6512 , C07F9/6552 , C07F9/65583 , C07H19/20 , C07H21/00 , C12N15/111 , C12N2310/14 , C12N2310/32 , C12N2310/332
摘要： This invention relates to acyclic and abasic nucleosides and oligonucleotides prepared therefrom. For instance, oligonucleotides can be prepared having one or more of the following formulas (I-III):, or isomers thereof.
摘要翻译：本发明涉及无环和非碱性核苷及其制备的寡核苷酸。例如，可以制备具有一个或多个下式（I-III）：或其异构体的寡核苷酸。

64. 发明授权

US08426377B2 iRNA agents with biocleavable tethers 有权
标题翻译：具有生物可清除系绳的iRNA试剂
公开(公告)号：US08426377B2
公开(公告)日：2013-04-23
申请号：US12724267
申请日：2010-03-15
申请人： Muthiah Manoharan , Kallanthottathil G. Rajeev
发明人： Muthiah Manoharan , Kallanthottathil G. Rajeev
IPC分类号： A61K31/70 , C07H21/04 , C07H5/06
CPC分类号： C12N15/113 , C12N15/111 , C12N2310/14 , C12N2310/323 , C12N2310/3511 , C12N2320/51
摘要： The invention relates to iRNA agents, which preferably include a monomer in which the ribose moiety has been replaced by a moiety other than ribose that further includes a tether having one or more linking groups, in which at least one of the linking groups is a cleavable linking group. The tether in turn can be connected to a selected moiety, e.g., a ligand, e.g., a targeting or delivery moiety, or a moiety which alters a physical property. The cleavable linking group is one which is sufficiently stable outside the cell such that it allows targeting of a therapeutically beneficial amount of an iRNA agent (e.g., a single stranded or double stranded iRNA agent), coupled by way of the cleavable linking group to a targeting agent—to targets cells, but which upon entry into a target cell is cleaved to release the iRNA agent from the targeting agent.
摘要翻译：本发明涉及iRNA试剂，其优选包括其中核糖部分已被核糖替代的单体，其进一步包括具有一个或多个连接基团的系链，其中至少一个连接基团是可切割的连接组。系链又可以连接到所选择的部分，例如配体，例如靶向或递送部分，或改变物理性质的部分。可切割连接基团是在细胞外部足够稳定的连接基团，使得其允许靶向治疗有益量的iRNA试剂（例如，单链或双链iRNA试剂），其通过可切割连接基团连接至靶向细胞靶向细胞，但是在进入靶细胞时被切割以从靶向剂释放iRNA试剂。

65. 发明申请

US20110224282A1 iRNA Agents Targeting VEGF 有权
标题翻译：靶向VEGF的iRNA试剂
公开(公告)号：US20110224282A1
公开(公告)日：2011-09-15
申请号：US13043228
申请日：2011-03-08
申请人： Antonin De Fougerolles , Maria Frank-Kamenetsky , Muthiah Manoharan , Kallanthottathil G. Rajeev , Philipp Hadwiger
发明人： Antonin De Fougerolles , Maria Frank-Kamenetsky , Muthiah Manoharan , Kallanthottathil G. Rajeev , Philipp Hadwiger
IPC分类号： A61K31/713 , C07H21/02 , A61P27/02 , C12N5/071 , C12N5/09
CPC分类号： C12N15/1136 , A61K9/0019 , A61K31/7088 , A61K31/712 , A61K31/713 , A61K47/02 , A61K47/10 , A61K47/12 , A61K47/549 , A61K47/551 , A61K47/60 , A61K48/00 , C07K14/475 , C12N2310/14 , C12N2310/3515 , C12N2310/533 , C12N2320/30 , C12N2320/32
摘要： The features of the present invention relate to compounds, compositions and methods useful for modulating the expression of vascular endothelial growth factor (VEGF), such as by the mechanism of RNA interference (RNAi). The compounds and compositions include iRNA agents that can be unmodified or chemically-modified.
摘要翻译：本发明的特征涉及用于调节血管内皮生长因子（VEGF）表达的化合物，组合物和方法，例如通过RNA干扰（RNAi）机制。化合物和组合物包括可以未修饰或化学修饰的iRNA试剂。

66. 发明授权

US08013136B2 Oligonucleotides comprising a non-phosphate backbone linkage 有权
标题翻译：包含非磷酸骨架键的寡核苷酸
公开(公告)号：US08013136B2
公开(公告)日：2011-09-06
申请号：US12496268
申请日：2009-07-01
申请人： Muthiah Manoharan , Kallanthottathil G. Rajeev
发明人： Muthiah Manoharan , Kallanthottathil G. Rajeev
IPC分类号： C07H21/02 , C07H21/04
CPC分类号： C12N15/111 , C07H19/04 , C07H19/12 , C07H19/16 , C07H19/167 , C07H19/173 , C07H21/02 , C12N15/1136 , C12N15/1137 , C12N2310/14 , C12N2310/312 , C12N2320/51
摘要： One aspect of the present invention relates to a ribonucleoside substituted with a phosphonamidite group at the 3′-position. In certain embodiments, the phosphonamidite is an alkyl phosphonamidite. Another aspect of the present invention relates to a double-stranded oligonucleotide comprising at least one non-phosphate linkage. Representative non-phosphate linkages include phosphonate, hydroxylamine, hydroxylhydrazinyl, amide, and carbamate linkages. In certain embodiments, the non-phosphate linkage is a phosphonate linkage. In certain embodiments, a non-phosphate linkage occurs in only one strand. In certain embodiments, a non-phosphate linkage occurs in both strands. In certain embodiments, a ligand is bound to one of the oligonucleotide strands comprising the double-stranded oligonucleotide. In certain embodiments, a ligand is bound to both of the oligonucleotide strands comprising the double-stranded oligonucleotide. In certain embodiments, the oligonucleotide strands comprise at least one modified sugar moiety. Another aspect of the present invention relates to a single-stranded oligonucleotide comprising at least one non-phosphate linkage. Representative non-phosphate linkages include phosphonate, hydroxylamine, hydroxylhydrazinyl, amide, and carbamate linkages. In certain embodiments, the non-phosphate linkage is a phosphonate linkage. In certain embodiments, a ligand is bound to the oligonucleotide strand. In certain embodiments, the oligonucleotide comprises at least one modified sugar moiety.
摘要翻译：本发明的一个方面涉及在3'-位被亚磷酰胺基取代的核糖核苷。在某些实施方案中，亚磷酰胺是烷基亚磷酰胺。本发明的另一方面涉及包含至少一种非磷酸键的双链寡核苷酸。代表性的非磷酸酯键包括膦酸酯，羟胺，羟基肼基，酰胺和氨基甲酸酯键。在某些实施方案中，非磷酸酯键是膦酸酯键。在某些实施方案中，非磷酸酯键仅出现在一条链中。在某些实施方案中，在两条链中都发生非磷酸连接。在某些实施方案中，配体与包含双链寡核苷酸的寡核苷酸链之一结合。在某些实施方案中，配体与包含双链寡核苷酸的两条寡核苷酸链结合。在某些实施方案中，寡核苷酸链包含至少一个修饰的糖部分。本发明的另一方面涉及包含至少一种非磷酸键的单链寡核苷酸。代表性的非磷酸酯键包括膦酸酯，羟胺，羟基肼基，酰胺和氨基甲酸酯键。在某些实施方案中，非磷酸酯键是膦酸酯键。在某些实施方案中，配体与寡核苷酸链结合。在某些实施方案中，寡核苷酸包含至少一个修饰的糖部分。

67. 发明申请

US20100222413A1 Chemically Modified Oligonucleotides for Use in Modulating Micro RNA and Uses Thereof 有权
标题翻译：用于调节微RNA的化学修饰的寡核苷酸及其用途
公开(公告)号：US20100222413A1
公开(公告)日：2010-09-02
申请号：US12714863
申请日：2010-03-01
申请人： Markus Stoffel , Muthiah Manoharan , Kallanthottathil G. Rajeev
发明人： Markus Stoffel , Muthiah Manoharan , Kallanthottathil G. Rajeev
IPC分类号： A61K31/7088
CPC分类号： C12N15/113 , C12N2310/11 , C12N2310/315 , C12N2310/321 , C12N2310/345 , C12N2310/346 , C12N2310/3515 , C12N2310/3521 , C12N2310/3527 , C12N2310/3531 , C12N2310/3533
摘要： This invention relates generally to chemically modified oligonuceotides useful for modulating expression of microRNAs and pre-microRNAs. More particularly, the invention relates to single stranded chemically modified oligonuceotides for inhibiting microRNA and pre-microRNA expression and to methods of making and using the modified oligonucleotides. Also included in the invention are compositions and methods for silencing microRNAs in the central nervous system.
摘要翻译：本发明一般涉及可用于调节微小RNA和pre-microRNAs表达的化学修饰的寡核苷酸。更具体地说，本发明涉及用于抑制微小RNA和pre-microRNA表达的单链化学修饰的寡核苷酸以及制备和使用修饰的寡核苷酸的方法。本发明还包括在中枢神经系统中沉默微小RNA的组合物和方法。

68. 发明授权

US09254327B2 Methods and compositions for delivery of active agents 有权
标题翻译：用于递送活性剂的方法和组合物
公开(公告)号：US09254327B2
公开(公告)日：2016-02-09
申请号：US13697229
申请日：2011-05-10
申请人： Muthiah Manoharan , Kallanthottathil G. Rajeev
发明人： Muthiah Manoharan , Kallanthottathil G. Rajeev
IPC分类号： C12N15/11 , A61K9/127 , A61K31/13 , A61K47/18 , C12N15/88 , A61K31/7088 , C07C219/08 , C07C229/12 , C07C233/38 , C07C237/06 , C07C271/12 , C07C271/64 , C07C275/20
CPC分类号： A61K47/18 , A61K9/1272 , A61K9/1278 , A61K31/7088 , C07C219/08 , C07C229/12 , C07C233/38 , C07C237/06 , C07C271/12 , C07C271/64 , C07C275/20 , C12N15/88
摘要： A lipid particle can include a cationic lipid. Synthesis of the cationic lipid can include a ylide-based reaction, such as a Wittig reaction or sulfur ylide reaction. In some cases, the synthesis can also include a Michael addition or a related addition reaction.
摘要翻译：脂质颗粒可以包括阳离子脂质。阳离子脂质的合成可以包括基于叶立德的反应，例如Wittig反应或硫叶立德反应。在某些情况下，合成还可以包括迈克尔加成或相关的加成反应。

69. 发明授权

US09156873B2 Modified 5′ diphosphate nucleosides and oligomeric compounds prepared therefrom 有权
标题翻译：修饰的5'二磷酸核苷和由其制备的低聚化合物
公开(公告)号：US09156873B2
公开(公告)日：2015-10-13
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： C07H21/04 , C07H19/00 , C07H19/04 , 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。

70. 发明授权

US09102938B2 2′ and 5′ modified monomers and oligonucleotides 有权
标题翻译： 2'和5'修饰的单体和寡核苷酸
公开(公告)号：US09102938B2
公开(公告)日：2015-08-11
申请号：US13638891
申请日：2011-03-31
申请人： Kallanthottathil G. Rajeev , Muthiah Manoharan , Eric E. Swayze , Thazha P. Prakash
发明人： Kallanthottathil G. Rajeev , Muthiah Manoharan , Eric E. Swayze , Thazha P. Prakash
IPC分类号： C07H21/02 , C12N15/113 , C07H19/067 , A61K48/00 , C07H19/06 , C07H19/16
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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