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公开(公告)号：US08278283B2
公开(公告)日：2012-10-02
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
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：US08207173B2
公开(公告)日：2012-06-26
申请号：US12620307
申请日：2009-11-17
IPC分类号： A61P31/14 , A61K31/415 , C07D491/00
CPC分类号： C07D401/04 , C04B35/632 , C07B2200/11 , C07D235/30 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D409/14 , C07D417/04 , C07D417/12 , C07D417/14 , C07D471/04 , C07D473/00 , C07D487/04 , C07D491/04 , C07D491/14
摘要： Provided are compounds of the formula: wherein RN1 is a substituent of formula G1-NX1X2, wherein G1 is an optionally further substituted alkylene, which optionally forms, together with RN2, a cyclic group, and each of X1 and X2 is independently H or an N-substituent, or X1 and X2 together form a heterocyclic ring, or X1 together with G1 forms a cyclic group and X2 is H or an N-substituent; and each of Z1, Z2, Z3 and Z4 is H or a substituent, or two of Z1, Z2, Z3 and Z4 together form an optionally substituted ring, and further wherein at least one of Z1, Z2, Z3 and Z4 is other than H, and salts thereof, pharmaceutical compositions and methods of using the compounds. The compounds have antiviral activity.
摘要翻译： 提供下式的化合物：其中RN1是式G1-NX1X2的取代基，其中G1是任选进一步取代的亚烷基，其任选地与RN2一起形成环状基团，并且X 1和X 2各自独立地为H或 X取代基或X1和X2一起形成杂环，或者X1与G1一起形成环状基团，X 2是H或N-取代基; Z1，Z2，Z3和Z4各自为H或取代基，Z1，Z2，Z3和Z4中的两个一起形成任选取代的环，其中Z1，Z2，Z3和Z4中的至少一个不是 H及其盐，药物组合物和使用该化合物的方法。 该化合物具有抗病毒活性。
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公开(公告)号：US20100184966A1
公开(公告)日：2010-07-22
申请号：US12751706
申请日：2010-03-31
申请人： Punit P. Seth , Eric E. Swayze , Balkrishen Bhat
发明人： Punit P. Seth , Eric E. Swayze , Balkrishen Bhat
IPC分类号： C07H21/04
摘要： The present invention provides 5′-modified bicyclic nucleoside analogs and oligomeric compounds comprising at least one of these nucleoside analogs. In preferred embodiments the nucleoside analogs have either (R) or (S)-chirality at the 5′-carbon. These bicyclic nucleoside analogs are useful for enhancing properties of oligomeric compounds including for example enhanced nuclease resistance.
摘要翻译： 本发明提供了包含这些核苷类似物中的至少一种的5'-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5'-碳上具有（R）或（S） - 亲和性。 这些双环核苷类似物可用于增强低聚化合物的性质，包括例如增强的核酸酶抗性。
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公开(公告)号：US20100130513A1
公开(公告)日：2010-05-27
申请号：US12620307
申请日：2009-11-17
IPC分类号： A61K31/4188 , C07D491/048 , C07D491/147 , A61K31/519 , C12N7/00
CPC分类号： C07D401/04 , C04B35/632 , C07B2200/11 , C07D235/30 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D409/14 , C07D417/04 , C07D417/12 , C07D417/14 , C07D471/04 , C07D473/00 , C07D487/04 , C07D491/04 , C07D491/14
摘要： Provided are compounds of the formula: wherein RN1 is a substituent of formula G1-NX1X2, wherein G1 is an optionally further substituted alkylene, which optionally forms, together with RN2, a cyclic group, and each of X1 and X2 is independently H or an N-substituent, or X1 and X2 together form a heterocyclic ring, or X1 together with G1 forms a cyclic group and X2 is H or an N-substituent; and each of Z1, Z2, Z3 and Z4 is H or a substituent, or two of Z1, Z2, Z3 and Z4 together form an optionally substituted ring, and further wherein at least one of Z1, Z2, Z3 and Z4 is other than H, and salts thereof, pharmaceutical compositions and methods of using the compounds. The compounds have antiviral activity.
摘要翻译： 提供下式的化合物：其中RN1是式G1-NX1X2的取代基，其中G1是任选进一步取代的亚烷基，其任选地与RN2一起形成环状基团，并且X 1和X 2各自独立地为H或 X取代基或X1和X2一起形成杂环，或者X1与G1一起形成环状基团，X 2是H或N-取代基; Z1，Z2，Z3和Z4各自为H或取代基，Z1，Z2，Z3和Z4中的两个一起形成任选取代的环，其中Z1，Z2，Z3和Z4中的至少一个不是 H及其盐，药物组合物和使用该化合物的方法。 该化合物具有抗病毒活性。
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公开(公告)号：US07642265B2
公开(公告)日：2010-01-05
申请号：US10946757
申请日：2004-09-22
IPC分类号： A61P31/12 , A61K31/4188 , C07D491/12
CPC分类号： C07D401/04 , C04B35/632 , C07B2200/11 , C07D235/30 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D409/14 , C07D417/04 , C07D417/12 , C07D417/14 , C07D471/04 , C07D473/00 , C07D487/04 , C07D491/04 , C07D491/14
摘要： Provided are compounds of the formula: wherein RN1 is a substituent of formula G1—NX1X2, wherein G1 is an optionally further substituted alkylene, which optionally forms, together with RN2, a cyclic group, and each of X1 and X2 is independently H or an N-substituent, or X1 and X2 together form a heterocyclic ring, or X1 together with G1 forms a cyclic group and X2 is H or an N-substituent; and each of Z1, Z2, Z3 and Z4 is H or a substituent, or two of Z1, Z2, Z3 and Z4 together form an optionally substituted ring, and further wherein at least one of Z1, Z2, Z3 and Z4 is other than H, and salts thereof, pharmaceutical compositions and methods of using the compounds. The compounds have antiviral activity.
摘要翻译： 提供下式的化合物：其中RN1是式G1-NX1X2的取代基，其中G1是任选进一步取代的亚烷基，其任选地与RN2一起形成环状基团，并且X 1和X 2各自独立地为H或 X取代基或X1和X2一起形成杂环，或者X1与G1一起形成环状基团，X 2是H或N-取代基; Z1，Z2，Z3和Z4各自为H或取代基，Z1，Z2，Z3和Z4中的两个一起形成任选取代的环，其中Z1，Z2，Z3和Z4中的至少一个不是 H及其盐，药物组合物和使用该化合物的方法。 该化合物具有抗病毒活性。
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公开(公告)号：US20090318532A1
公开(公告)日：2009-12-24
申请号：US12299607
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： A61K31/7088 , C07H21/02 , 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：US20090306357A1
公开(公告)日：2009-12-10
申请号：US12299583
申请日：2007-05-07
申请人： Sanjay Bhanot , Richard Geary , Robert McKay , Brett P. Monia , Punit P. Seth , Andrew M. Siwkowski , Eric E. Swayze , Edward Wancewicz
发明人： Sanjay Bhanot , Richard Geary , Robert McKay , Brett P. Monia , Punit P. Seth , Andrew M. Siwkowski , Eric E. Swayze , Edward Wancewicz
IPC分类号： C07H21/04
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：US20090306180A1
公开(公告)日：2009-12-10
申请号：US12299764
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 , A61P9/00
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：US07547684B2
公开(公告)日：2009-06-16
申请号：US11747057
申请日：2007-05-10
申请人： Punit P. Seth , Eric E. Swayze , Balkrishen Bhat
发明人： Punit P. Seth , Eric E. Swayze , Balkrishen Bhat
摘要： The present invention provides 5′-modified bicyclic nucleoside analogs and oligomeric compounds comprising at least one of these nucleoside analogs. In preferred embodiments the nucleoside analogs have either (R) or (S)-chirality at the 5′-carbon. These bicyclic nucleoside analogs are useful for enhancing properties of oligomeric compounds including for example enhanced nuclease resistance.
摘要翻译： 本发明提供了包含这些核苷类似物中的至少一种的5'-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5'-碳上具有（R）或（S） - 亲和性。 这些双环核苷类似物可用于增强低聚化合物的性质，包括例如增强的核酸酶抗性。
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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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