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公开(公告)号：US20110053881A1
公开(公告)日：2011-03-03
申请号：US12667684
申请日：2008-07-01
申请人： Punit P. Seth , Eric E. Swayze
发明人： Punit P. Seth , Eric E. Swayze
IPC分类号： A61K31/7088 , C07H19/00 , C07H19/06 , C12N5/071 , A61K31/7042 , A61P43/00
摘要： The present disclosure describes 6-disubstituted bicyclic nucleosides, oligomeric compounds prepared therefrom and methods of using the oligomeric compounds. More particularly, the 6-disubstituted bicyclic nucleosides each comprise a 2′-O—C(Ri)(R2)-4′ or 2′-O—C=(R3)(R.4)-4′ bridge wherein each R is, independently a substituent group and Ri and R2 include H. The 6-disubstituted bicyclic nucleosides are useful for enhancing properties of oligomeric compounds including nuclease resistance. In certain 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6-二取代的双环核苷，由其制备的低聚化合物和使用低聚化合物的方法。 更具体地，6-二取代的双环核苷各自包含2'-O-C（R 1）（R 2）-4'或2'-O-C =（R 3）（R 4）-4'桥，其中每个R 独立地是取代基，R 1和R 2包括H.6-二取代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，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：US20100233806A1
公开(公告)日：2010-09-16
申请号：US12602993
申请日：2008-06-06
申请人： Punit P. Seth , Eric E. Swayze
发明人： Punit P. Seth , Eric E. Swayze
摘要： Provided herein are saturated and unsaturated carbocyclic bicyclic nucleosides, oligomeric compounds prepared therefrom and methods of using these oligomeric compounds. The saturated and unsaturated carbocyclic bicyclic nucleosides are useful for enhancing properties of oligomeric compounds including nuclease resistance.
摘要翻译： 本文提供了饱和和不饱和的碳环双环核苷，由其制备的低聚化合物和使用这些低聚化合物的方法。 饱和和不饱和的碳环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。
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公开(公告)号：US07741457B2
公开(公告)日：2010-06-22
申请号：US12129154
申请日：2008-05-29
申请人： Punit P. Seth , Eric E. Swayze
发明人： Punit P. Seth , Eric E. Swayze
摘要： The present invention provides 6-modified bicyclic nucleoside analogs and oligomeric compounds comprising these nucleoside analogs. In preferred embodiments the nucleoside analogs have either (R) or (S)-chirality at the 6-position. These bicyclicnucleoside analogs are useful for enhancing properties of oligomeric compounds including nuclease resistance.
摘要翻译： 本发明提供了包含这些核苷类似物的6-修饰的双环核苷类似物和寡聚化合物。 在优选的实施方案中，核苷类似物在6-位具有（R）或（S） - 双键。 这些双环核苷类似物可用于增强包括核酸酶抗性的寡聚化合物的性质。
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公开(公告)号：US20090306179A1
公开(公告)日：2009-12-10
申请号：US12299609
申请日：2007-05-07
申请人： Sanjay Bhanot , Richard S. Geary , Robert McKay , Brett P. Monia , Punit P. Seth , Andrew M. Siwkowski , Eric E. Swayze , Edward Wancewicz
发明人： Sanjay Bhanot , Richard S. Geary , Robert McKay , Brett P. Monia , Punit P. Seth , Andrew M. Siwkowski , Eric E. Swayze , Edward Wancewicz
IPC分类号： A61K31/7052 , C07H21/00 , C12N5/00 , A61P3/00
CPC分类号： C12N15/113 , C12N15/1137 , C12N2310/11 , C12N2310/31 , C12N2310/315 , C12N2310/321 , C12N2310/322 , C12N2310/3231 , C12N2310/341 , C12N2310/3515 , C12Y203/0102 , C12N2310/3521
摘要： The present disclosure describes short antisense compounds, including such compounds comprising chemically-modified high-affinity monomers 8-16 monomers in length. Certain such short antisense compound are useful for the reduction of target nucleic acids and/or proteins in cells, tissues, and animals with increased potency and improved therapeutic index. Thus, provided herein are short antisense compounds comprising high-affinity nucleotide modifications useful for reducing a target RNA in vivo. Such short antisense compounds are effective at lower doses than previously described antisense compounds, allowing for a reduction in toxicity and cost of treatment. In addition, the described short antisense compounds have greater potential for oral dosing.
摘要翻译： 本公开描述了短反义化合物，包括长度为化学修饰的高亲和力单体8-16单体的这类化合物。 某些这样的短反义化合物可用于在增加的效力和改善的治疗指数的细胞，组织和动物中还原靶核酸和/或蛋白质。 因此，本文提供了包含用于在体内降低靶RNA的高亲和力核苷酸修饰的短反义化合物。 这样的短反义化合物在比以前描述的反义化合物低的剂量下是有效的，允许降低毒性和治疗成本。 此外，所述短反义化合物具有更大的口服给药潜力。
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公开(公告)号：US20090292006A1
公开(公告)日：2009-11-26
申请号：US12299605
申请日：2007-05-07
申请人： Sanjay Bhanot , Richard S. Geary , Robert McKay , Brett P. Monia , Punit P. Seth , Andrew M. Siwkowski , Eric E. Swayze , Edward Wancewicz
发明人： Sanjay Bhanot , Richard S. Geary , Robert McKay , Brett P. Monia , Punit P. Seth , Andrew M. Siwkowski , Eric E. Swayze , Edward Wancewicz
CPC分类号： C12N15/113 , C12N15/1137 , C12N2310/11 , C12N2310/31 , C12N2310/315 , C12N2310/321 , C12N2310/322 , C12N2310/3231 , C12N2310/341 , C12N2310/3515 , C12Y203/0102 , C12N2310/3521
摘要： The present disclosure describes short antisense compounds, including such compounds comprising chemically-modified high-affinity monomers 8-16 monomers in length. Certain such short antisense compound are useful for the reduction of target nucleic acids and/or proteins in cells, tissues, and animals with increased potency and improved therapeutic index. Thus, provided herein are short antisense compounds comprising high-affinity nucleotide modifications useful for reducing a target RNA in vivo. Such short antisense compounds are effective at lower doses than previously described antisense compounds, allowing for a reduction in toxicity and cost of treatment. In addition, the described short antisense compounds have greater potential for oral dosing.
摘要翻译： 本公开描述了短反义化合物，包括长度为化学修饰的高亲和力单体8-16单体的这类化合物。 某些这样的短反义化合物可用于在增加的效力和改善的治疗指数的细胞，组织和动物中还原靶核酸和/或蛋白质。 因此，本文提供了包含用于在体内降低靶RNA的高亲和力核苷酸修饰的短反义化合物。 这样的短反义化合物在比以前描述的反义化合物低的剂量下是有效的，允许降低毒性和治疗成本。 此外，所述短反义化合物具有更大的口服给药潜力。
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公开(公告)号：US20140323707A1
公开(公告)日：2014-10-30
申请号：US14238441
申请日：2012-08-08
IPC分类号： C12N15/113
CPC分类号： C12N15/113 , C12N15/111 , C12N2310/11 , C12N2310/312 , C12N2310/3125 , C12N2310/315 , C12N2310/316 , C12N2310/321 , C12N2310/3231 , C12N2310/3341 , C12N2310/341 , C12N2310/351 , C12N2320/34 , C12N2310/3525
摘要： The present invention provides oligomeric compounds. Certain such oligomeric compounds are useful for hybridizing to a complementary nucleic acid, including but not limited, to nucleic acids in a cell. In certain embodiments, hybridization results in modulation of the amount activity or expression of the target nucleic acid in a cell.
摘要翻译： 本发明提供低聚化合物。 某些这样的寡聚化合物可用于与互补核酸杂交，包括但不限于细胞中的核酸。 在某些实施方案中，杂交导致细胞中靶核酸的活性或表达的调节。
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27.发明授权Substituted 2′-amino and 2′-thio-bicyclic nucleosides and oligomeric compounds prepared therefrom 有权由其制备的取代的2'-氨基和2'-硫代双环核苷和寡聚化合物公开(公告)号：US08846637B2
公开(公告)日：2014-09-30
申请号：US13697970
申请日：2011-06-02
申请人： Punit P. Seth , Thazha P. Prakash , Eric E. Swayze
发明人： Punit P. Seth , Thazha P. Prakash , Eric E. Swayze
IPC分类号： A61K31/70 , C07H17/00 , C07H21/04 , C07H19/06 , C07H21/00 , C12N15/113 , C07H19/173 , C07H19/073
CPC分类号： C07H19/06 , C07H19/073 , C07H19/173 , C07H21/00 , C07H21/04 , C12N15/113 , C12N2310/3231 , C12N2310/3341 , C12N2310/341
摘要： Provided herein are 2′-amino and 2′-thio bicyclic nucleosides and oligomenc compounds prepared therefrom. The novel bicyclic nucleosides provided herein are expected to be useful for enhancing one or more properties of the oligomeric compounds they are incorporated into such as nuclease resistance.
摘要翻译： 本文提供了由其制备的2'-氨基和2'-硫代双环核苷和寡聚化合物。 预期本文提供的新型双环核苷可用于增强其掺入诸如核酸酶抗性的寡聚化合物的一种或多种性质。
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公开(公告)号：US08546556B2
公开(公告)日：2013-10-01
申请号：US12741444
申请日：2008-11-21
申请人： Punit P. Seth , Eric E. Swayze
发明人： Punit P. Seth , Eric E. Swayze
IPC分类号： C07H21/00
CPC分类号： C07H21/00
摘要： The present invention provides novel carbocyclic α-L-bicyclic nucleosides and oligomeric compounds comprising at least one of these carbocyclic α-L-bicyclic nucleosides. The carbocyclic α-L-bicyclic nucleosides are useful for enhancing one or more properties of the oligomeric compounds they are incorporated into including nuclease resistance.
摘要翻译： 本发明提供了包含这些碳环α-L-双环核苷中的至少一种的新型碳环α-L-双环核苷和寡聚化合物。 碳环α-L-双环核苷可用于增强其掺入的寡聚化合物的一种或多种性质，包括核酸酶抗性。
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公开(公告)号：US08530640B2
公开(公告)日：2013-09-10
申请号：US12866708
申请日：2009-02-06
申请人： Punit P. Seth , Michael T. Migawa , Eric E. Swayze , Quanlai Song , Mingming Han , Bruce S. Ross
发明人： Punit P. Seth , Michael T. Migawa , Eric E. Swayze , Quanlai Song , Mingming Han , Bruce S. Ross
CPC分类号： C07H21/00
摘要： The present disclosure provides bicyclic cyclohexitol nucleoside analogs of formula I 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： 本公开提供式I的双环体醇核苷类似物和包含这些核苷类似物的低聚化合物。 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。
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公开(公告)号：US08278426B2
公开(公告)日：2012-10-02
申请号：US12602993
申请日：2008-06-06
申请人： Punit P. Seth , Eric E. Swayze
发明人： Punit P. Seth , Eric E. Swayze
摘要： Provided herein are saturated and unsaturated carbocyclic bicyclic nucleosides, oligomeric compounds prepared therefrom and methods of using these oligomeric compounds. The saturated and unsaturated carbocyclic bicyclic nucleosides are useful for enhancing properties of oligomeric compounds including nuclease resistance.
摘要翻译： 本文提供了饱和和不饱和的碳环双环核苷，由其制备的低聚化合物和使用这些低聚化合物的方法。 饱和和不饱和的碳环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。
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