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公开(公告)号：US20090092981A1
公开(公告)日：2009-04-09
申请号：US12192847
申请日：2008-08-15
申请人： Eric E. Swayze , Andrew M. Siwkowski , Balkrishen Bhat , Thazha P. Prakash , Charles Allerson , Punit P. Seth
发明人： Eric E. Swayze , Andrew M. Siwkowski , Balkrishen Bhat , Thazha P. Prakash , Charles Allerson , Punit P. Seth
IPC分类号： A61K31/7105 , C07H19/06 , C12Q1/00 , C07H19/16
CPC分类号： C12N15/113 , C07H19/10 , C07H19/20 , C07H21/00 , C12N15/111 , C12N2310/323 , C12N2320/51
摘要： The present disclosure describes tetrahydropyran nucleoside analogs, oligomeric compounds prepared therefrom and methods of using the oligomeric compounds. More particularly, tetrahydropyran nucleoside analogs are provided, having one or more chiral substituents, that are useful for enhancing properties of oligomeric compounds including nuclease resistance and binding affinity. In some embodiments, the oligomeric compounds provided herein hybridize to a portion of a target RNA resulting in loss of normal function of the target RNA.
摘要翻译： 本公开描述了四氢吡喃核苷类似物，由其制备的低聚化合物和使用寡聚化合物的方法。 更具体地，提供四氢吡喃核苷类似物，其具有一个或多个手性取代基，其可用于增强低聚化合物的性质，包括核酸酶抗性和结合亲和力。 在一些实施方案中，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。
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公开(公告)号：US08088904B2
公开(公告)日：2012-01-03
申请号：US12192847
申请日：2008-08-15
申请人： Eric E. Swayze , Andrew M. Siwkowski , Balkrishen Bhat , Thazha P. Prakash , Charles Allerson , Punit P. Seth
发明人： Eric E. Swayze , Andrew M. Siwkowski , Balkrishen Bhat , Thazha P. Prakash , Charles Allerson , Punit P. Seth
CPC分类号： C12N15/113 , C07H19/10 , C07H19/20 , C07H21/00 , C12N15/111 , C12N2310/323 , C12N2320/51
摘要： The present disclosure describes tetrahydropyran nucleoside analogs, oligomeric compounds prepared therefrom and methods of using the oligomeric compounds. More particularly, tetrahydropyran nucleoside analogs are provided, having one or more chiral substituents, that are useful for enhancing properties of oligomeric compounds including nuclease resistance and binding affinity. In some embodiments, the oligomeric compounds provided herein hybridize to a portion of a target RNA resulting in loss of normal function of the target RNA.
摘要翻译： 本公开描述了四氢吡喃核苷类似物，由其制备的低聚化合物和使用寡聚化合物的方法。 更具体地，提供四氢吡喃核苷类似物，其具有一个或多个手性取代基，其可用于增强低聚化合物的性质，包括核酸酶抗性和结合亲和力。 在一些实施方案中，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。
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公开(公告)号：US08440803B2
公开(公告)日：2013-05-14
申请号：US13308750
申请日：2011-12-01
申请人： Eric E. Swayze , Andrew M. Siwkowski , Balkrishen Bhat , Thazha P. Prakash , Charles Allerson , Punit P. Seth
发明人： Eric E. Swayze , Andrew M. Siwkowski , Balkrishen Bhat , Thazha P. Prakash , Charles Allerson , Punit P. Seth
CPC分类号： C12N15/113 , C07H19/10 , C07H19/20 , C07H21/00 , C12N15/111 , C12N2310/323 , C12N2320/51
摘要： The present disclosure describes tetrahydropyran nucleoside analogs, oligomeric compounds prepared therefrom and methods of using the oligomeric compounds. More particularly, tetrahydropyran nucleoside analogs are provided, having one or more chiral substituents, that are useful for enhancing properties of oligomeric compounds including nuclease resistance and binding affinity. In some embodiments, the oligomeric compounds provided herein hybridize to a portion of a target RNA resulting in loss of normal function of the target RNA.
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4.发明申请METHODS OF USING OLIGOMERIC COMPOUNDS COMPRISING 2'-SUBSTITUTED NUCLEOSIDES 审中-公开使用包含2'-取代核苷酸的低聚化合物的方法公开(公告)号：US20120059045A1
公开(公告)日：2012-03-08
申请号：US13125560
申请日：2009-10-23
IPC分类号： A61K31/712 , C12Q1/68 , C12N5/071
摘要： The present disclosure provides oligomeric compounds comprising at least one 2′-fluoroethoxy modified nucleoside of formula I and methods of using these 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.
摘要翻译： 本公开提供了包含至少一种式I的2'-氟乙氧基修饰的核苷的低聚化合物和使用这些低聚化合物的方法。 本文提供的方法包括使细胞接触或向动物施用至少一种低聚化合物。 在某些实施方案中，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。
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公开(公告)号：US20120071645A1
公开(公告)日：2012-03-22
申请号：US13308750
申请日：2011-12-01
申请人： Eric E. Swayze , Andrew M. Siwkowski , Balkrishen Bhat , Thazha P. Prakash , Charles Allerson , Punit P. Seth
发明人： Eric E. Swayze , Andrew M. Siwkowski , Balkrishen Bhat , Thazha P. Prakash , Charles Allerson , Punit P. Seth
CPC分类号： C12N15/113 , C07H19/10 , C07H19/20 , C07H21/00 , C12N15/111 , C12N2310/323 , C12N2320/51
摘要： The present disclosure describes tetrahydropyran nucleoside analogs, oligomeric compounds prepared therefrom and methods of using the oligomeric compounds. More particularly, tetrahydropyran nucleoside analogs are provided, having one or more chiral substituents, that are useful for enhancing properties of oligomeric compounds including nuclease resistance and binding affinity. In some embodiments, the oligomeric compounds provided herein hybridize to a portion of a target RNA resulting in loss of normal function of the target RNA.
摘要翻译： 本公开描述了四氢吡喃核苷类似物，由其制备的低聚化合物和使用寡聚化合物的方法。 更具体地，提供四氢吡喃核苷类似物，其具有一个或多个手性取代基，其可用于增强低聚化合物的性质，包括核酸酶抗性和结合亲和力。 在一些实施方案中，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。
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公开(公告)号：US20120021515A1
公开(公告)日：2012-01-26
申请号：US13148288
申请日：2010-02-05
申请人： Eric E. Swayze , Andrew M. Siwkowski , Balkrishen Bhat , Thazha P. Prakash , Charles Allerson , Punit P. Seth
发明人： Eric E. Swayze , Andrew M. Siwkowski , Balkrishen Bhat , Thazha P. Prakash , Charles Allerson , Punit P. Seth
CPC分类号： C07H21/00
摘要： The present invention provides oligomeric compounds and uses thereof. In certain embodiments, such oligomeric compounds are useful as antisense compounds. Certain such antisense compounds are useful as RNase H antisense compounds, as RNAi compounds, and/or as modulators of splicing.
摘要翻译： 本发明提供低聚化合物及其用途。 在某些实施方案中，这些低聚化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，作为RNAi化合物，和/或作为剪接调节剂。
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7.发明申请DOUBLE STRAND COMPOSITIONS COMPRISING DIFFERENTIALLY MODIFIED STRANDS FOR USE IN GENE MODULATION 审中-公开包含用于基因调控的差异化修饰条纹的双重条纹组合公开(公告)号：US20130035369A1
公开(公告)日：2013-02-07
申请号：US13566864
申请日：2012-08-03
申请人： Balkrishen Bhat , Thazha P. Prakash , Charles Allerson , Garth A. Kinberger , Eric G. Marcusson , Eric E. Swayze
发明人： Balkrishen Bhat , Thazha P. Prakash , Charles Allerson , Garth A. Kinberger , Eric G. Marcusson , Eric E. Swayze
IPC分类号： A61K31/7125 , A61P35/00 , A61P29/00 , C12N5/07 , A61K31/7088
CPC分类号： C12N15/111 , C12N15/113 , C12N15/1137 , C12N2310/14 , C12N2310/315 , C12N2310/317 , C12N2310/321 , C12N2310/322 , C12N2310/323 , C12N2310/341 , C12N2310/346 , C12N2310/3515 , C12N2310/3525 , C12N2310/3533 , C12N2320/51 , C12Y301/03048 , C12N2310/3521
摘要： The present invention provides double stranded compositions wherein the first strand is modified to have a particular motif and the second strand is modified a selected motif. More particularly, the present compositions comprise an antisense strand that is modified to have a positional/full motif and the sense strand is modified to have an alternating motif, a hemimer motif, a blockmer motif, a gapped motif, a positional motif, a positional/full motif or a fully modified motif. Each strand further comprises one or more phosphorothioate internucleoside linkage. The compositions are useful for targeting selected nucleic acid molecules and modulating the expression of one or more genes.
摘要翻译： 本发明提供双链组合物，其中第一链被修饰成具有特定的基序，第二链被修饰为选定的基序。 更具体地，本发明的组合物包含被修饰为具有位置/完整基序的反义链，并且有义链被修饰为具有交替基序，半缩氨酸基序，阻断基序，间隙基序，位置基序，位置 /完整的图案或完全修饰的图案。 每条链还包含一个或多个硫代磷酸酯核苷间键。 该组合物可用于靶向选定的核酸分子并调节一个或多个基因的表达。
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8.发明授权2′-substituted oligomeric compounds and compositions for use in gene modulations 有权2'-取代的寡聚化合物和用于基因调节的组合物公开(公告)号：US07919612B2
公开(公告)日：2011-04-05
申请号：US10701316
申请日：2003-11-04
申请人： Brenda F. Baker , Anne B. Eldrup , Muthiah Manoharan , Balkrishen Bhat , Richard Griffey , Eric E. Swayze , Stanley T. Crooke , Thazha P. Prakash
发明人： Brenda F. Baker , Anne B. Eldrup , Muthiah Manoharan , Balkrishen Bhat , Richard Griffey , Eric E. Swayze , Stanley T. Crooke , Thazha P. Prakash
CPC分类号： C12N15/113 , A61K38/00 , C07H21/00 , C12N9/22 , C12N15/1135 , C12N2310/311 , C12N2310/312 , C12N2310/314 , C12N2310/315 , C12N2310/316 , C12N2310/318 , C12N2310/3181 , C12N2310/321 , C12N2310/322 , C12N2310/3341 , C12N2310/335 , C12N2310/341 , C12N2310/346 , Y02A50/395 , Y02P20/582 , C12N2310/3527 , C12N2310/3525 , C12N2310/3521
摘要： Compositions comprising first and second oligomers are provided wherein at least a portion of the first oligomer is capable of hybridizing with at least a portion of the second oligomer, at least a portion of the first oligomer is complementary to and capable of hybridizing to a selected target nucleic acid, and at least one of the first or second oligomers includes a modified sugar and/or backbone modification. In some embodiments the modification is a 2′ substituent group on a sugar moiety that is not H or OH. Oligomer/protein compositions are also provided comprising an oligomer complementary to and capable of hybridizing to a selected target nucleic acid and at least one protein comprising at least a portion of an RNA-induced silencing complex (RISC), wherein at least one nucleotide of the oligomer has a modified sugar and/or backbone modification.
摘要翻译： 提供包含第一和第二寡聚体的组合物，其中至少一部分第一寡聚体能够与至少一部分第二寡聚物杂交，至少一部分第一寡聚体与选定的靶互补并能够与选定的靶 核酸，并且第一或第二寡聚体中的至少一种包括修饰的糖和/或骨架修饰。 在一些实施方案中，修饰是糖部分上不是H或OH的2'取代基。 还提供低聚物/蛋白质组合物，其包含与选定的靶核酸互补并且能够与选定的靶核酸杂交的寡聚体和至少一种包含至少一部分RNA诱导的沉默复合物（RISC）的蛋白质，其中至少一个核苷酸 低聚物具有修饰的糖和/或骨架修饰。
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9.发明申请公开(公告)号：US20080207541A1
公开(公告)日：2008-08-28
申请号：US10592919
申请日：2005-03-15
申请人： Michael T. Migawa , Walter F. Lima , Eric E. Swayze , Joshua Nichols , Hongjiang Wu , Thazha P. Prakash , Tadeusz Krzysztof Wyrzykiewicz , Balkrishen Bhat , Stanley T. Crooke
发明人： Michael T. Migawa , Walter F. Lima , Eric E. Swayze , Joshua Nichols , Hongjiang Wu , Thazha P. Prakash , Tadeusz Krzysztof Wyrzykiewicz , Balkrishen Bhat , Stanley T. Crooke
CPC分类号： C12N15/85 , C12N15/111 , C12N2310/11 , C12N2310/315 , C12N2310/318 , C12N2310/321 , C12N2310/346 , C12N2310/3519 , C12N2310/3525
摘要： The present invention provides compositions and methods for the optimization of cleavage of RNA species by RNase H. In some embodiments, the invention provides oligonucleotides that possess two or more regions of differing conformation, and at least one transitional nucleobase positioned between the regions that is capable of modulating transfer of the helical conformation characteristic of the region bound to the 3′hydroxy thereof, to the region bound to the 5′ hydroxyl thereof.
摘要翻译： 本发明提供了通过RNA酶H优化RNA种类的切割的组合物和方法。在一些实施方案中，本发明提供具有不同构象的两个或更多个区域的寡核苷酸，以及位于能够区分的区域之间的至少一个过渡核碱基 调节与其3'-羟基结合的区域的螺旋构象特征转移到与其5'羟基结合的区域。
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10.发明申请OLIGOMERIC COMPOUNDS COMPRISING TRICYCLIC NUCELOSIDES AND METHODS FOR THEIR USE 有权包含三聚核苷酸的低分子化合物及其使用方法公开(公告)号：US20110092570A1
公开(公告)日：2011-04-21
申请号：US12922832
申请日：2009-03-19
IPC分类号： A61K31/712 , C07H21/04 , C07H19/10
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.
摘要翻译： 本公开提供三环核苷，包含至少一种三环核苷的寡聚化合物和使用寡聚化合物的方法。 本文提供的方法包括使细胞接触或向动物施用至少一种低聚化合物。 在某些实施方案中，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。
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