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11.发明公开POLYCYCLIC SUGAR SURROGATE-CONTAINING OLIGOMERIC COMPOUNDS AND COMPOSITIONS FOR USE IN GENE MODULATION 有权多环芳烃SUGAR SPARE LEG AMUSING低聚物化合物和组合物用于基因调节
公开(公告)号：EP1562971A2
公开(公告)日：2005-08-17
申请号：EP03768647.4
申请日：2003-11-04
发明人： ALLERSON, Charles , BHAT, Balkrishen , ELDRUP, Ann, B. , MANOHARAN, Muthiah , GRIFFEY, Richard , BAKER, Brenda, F. , SWAYZE, Eric, E.
CPC分类号： C12N15/1135 , C07H21/04 , C12N15/1137 , C12N2310/11 , C12N2310/14 , C12N2310/315 , C12N2310/322 , C12N2310/3231 , C12N2310/341 , C12N2310/346 , C12N2310/53
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 modification comprising a polycyclic sugar surrogate. 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 nucleoside of the oligomer has a polycyclic sugar surrogate modification.
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公开(公告)号：EP1677822B1
公开(公告)日：2014-04-23
申请号：EP04816222.6
申请日：2004-09-20
发明人： BHAT, Balkrishen , DANDE, Prasad , PRAKASH, Thazha P. , ALLERSON, Charles , SWAYZE, Eric E. , GRIFFEY, Richard H.
IPC分类号： A01N43/00 , A01N43/04 , A61K31/33 , A61K31/70 , C07H19/00 , C07D333/02 , C07D333/32 , C07D333/34 , C07D333/42
CPC分类号： C12N15/113 , C12N2310/11 , C12N2310/14 , C12N2310/32
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公开(公告)号：EP1765074B1
公开(公告)日：2012-10-03
申请号：EP04754153.7
申请日：2004-06-03
发明人： BHAT, Balkrishen , SWAYZE, Eric , PRAKASH, Thazha, P. , ALLERSON, Charles , DANDE, Prasad , GRIFFEY, Richard, H.
CPC分类号： C12N15/113 , C12N15/111 , C12N15/1137 , C12N2310/14 , C12N2310/315 , C12N2310/32 , C12N2310/321 , C12N2310/322 , C12N2310/3231 , C12N2320/50 , C12Y301/03048 , C12N2310/3525 , C12N2310/3521
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14.发明公开
公开(公告)号：EP1984499A2
公开(公告)日：2008-10-29
申请号：EP07710352.1
申请日：2007-01-27
CPC分类号： C12N15/111 , C12N15/113 , C12N2310/11 , C12N2310/315 , C12N2310/321 , C12N2310/322 , C12N2310/3231 , C12N2310/341 , C12N2310/346 , C12N2320/51 , C12N2310/3527 , C12N2310/3525
摘要： Compounds, compositions and methods are provided for modulating the levels expression, processing and function of miRNAs. The compositions comprise oligomeric compounds targeted to small non-coding RNAs and miRNAs. The oligomeric compounds possess potent miRNA inhibitory activity, and further exhibit improved therapuetic index. Further provided are methods for selectively modulating miRNA activity in a cell.
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公开(公告)号：EP1765415A2
公开(公告)日：2007-03-28
申请号：EP05756325.6
申请日：2005-06-02
发明人： SWAYZE, Eric, E. , BHAT, Balkrishen , GRIFFEY, Richard, H. , PRAKASH, Thazha, P. , ALLERSON, Charles
CPC分类号： C12N15/113 , C07H21/02 , C12N15/111 , C12N2310/14 , C12N2310/315 , C12N2310/32 , C12N2310/321 , C12N2310/322 , C12N2310/3231 , C12N2310/341 , C12N2310/346 , C12N2320/30 , C12N2320/51 , C12N2310/3521
摘要： The present invention provides double stranded compositions wherein one of the strands is useful in, for example, influencing the preferential loading the opposite strand into the RISC (or cleavage) complex. In particular, the present invention provides oligomeric compounds that comprise chemical modifications in at least one of the strands to drive loading of the opposite strand into the RISC (or cleavage) complex. Such modifications can be used to increase potency of duplex constructs that have been modified to enhance stability. Examples of chemical modifications that drive loading of the second strand include, but are not limited to, MOE (2'-O(CH2)2OCH3), 2'-O-methyl, -ethyl, -propyl, and -N-methylacetamide. Such modifications can be distributed throughout the strand, or placed at the 5' and/or 3' ends to make a gapmer motif on the sense strand. The activity of the 4'-thio gapmer RNA antisense strand can be improved by incorporating alternating MOE or MOE gapmer motif into the sense strand.
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16.发明公开
公开(公告)号：EP1730309A2
公开(公告)日：2006-12-13
申请号：EP05725530.9
申请日：2005-03-15
发明人： MIGAWA, Michael, T. , LIMA, Walter, F. , SWAYZE, Eric, E. , NICHOLS, Joshua , WU, Hongjiang , PRAKASH, Thazha, P. , WYRZYKIEWICZ, Tadeusz, Krzysztof , BHAT, Balkrishen , CROOKE, Stanley, T.
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 emboediments, 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.
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17.发明公开OLIGOMERIC COMPOUNDS AND COMPOSITIONS FOR USE IN MODULATION OF SMALL NON-CODING RNAS 审中-公开低聚物化合物和组合物应用于小型非KODIENDEREN RNA的调制
公开(公告)号：EP1648914A2
公开(公告)日：2006-04-26
申请号：EP04780181.6
申请日：2004-07-30
发明人： ESAU, Christine , LOLLO, Bridget , BENNETT, C., Frank , FREIER, Susan, M. , GRIFFEY, Richard, H. , BAKER, Brenda, F. , VICKERS, Timothy , MARCUSSON, Eric, G. , KOLLER, Erich , SWAYZE, Eric, E. , JAIN, Ravi , BHAT, Balkrishen , PERALTA, Eigen
CPC分类号： C12N15/113 , C12N15/111 , C12N2310/11 , C12N2310/113 , C12N2310/14 , C12N2310/141 , C12N2310/31 , C12N2310/315 , C12N2310/317 , C12N2310/3181 , C12N2310/32 , C12N2310/321 , C12N2310/3231 , C12N2310/3341 , C12N2310/341 , C12N2310/346 , C12N2310/351 , C12N2310/3515 , C12N2320/11 , C12N2320/30 , C12N2320/50 , C12N2310/3525
摘要： Compounds, compositions and methods are provided for modulating the expression and function of small non-coding RNAs. The compositions comprise oligomeric compounds, targeted to small non-coding RNAs. Methods of using these compounds for modulation of small non-coding RNAs as well as downstream targets of these RNAs and for diagnosis and treatment of disease associated with small non-coding RNAs are also provided.
摘要翻译： 化合物，组合物和方法提供了用于调节的小非编码RNA的表达和功能。 所述组合物包含低聚化合物，有针对性的小非编码RNA。 因此，提供了使用这些化合物用于小非编码RNA的调制以及合成的RNA和用于诊断和治疗与小的非编码RNA相关的疾病的下游靶的方法。
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18.发明公开SUGAR SURROGATE-CONTAINING OLIGOMERIC COMPOUNDS AND COMPOSITIONS FOR USE IN GENE MODULATION 审中-公开糖代用品遏制和组合物的用途在DERGENMODULATION低聚物化合物
公开(公告)号：EP1578765A2
公开(公告)日：2005-09-28
申请号：EP03783131.0
申请日：2003-11-04
发明人： BAKER, Brenda, F. , ELDRUP, Anne, B. , MANOHARAN, Muthiah , BHAT, Balkrishen , GRIFFEY, Richard , SWAYZE, Eric, E. , CROOKE, Stanley, T.
IPC分类号： C07H21/04
CPC分类号： C07H21/00 , C07H21/04 , C12N15/111 , C12N15/113 , C12N2310/14 , C12N2310/321 , C12N2310/322 , C12N2310/323 , C12N2310/343 , C12N2310/3521 , C12N2310/3533 , C12N2320/51
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 modification comprising a sugar surrogate. 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 nucleoside of the oligomer has a sugar surrogate modification.
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19.发明公开2'-SUBSTITUTED OLIGOMERIC COMPOUNDS AND COMPOSITIONS FOR USE IN GENE MODULATIONS 审中-公开2'-取代低聚物化合物和组合FOR USE IN GENMODULATIONEN
公开(公告)号：EP1563070A2
公开(公告)日：2005-08-17
申请号：EP03786574.8
申请日：2003-11-04
发明人： BAKER, Brenda , ELDRUP, Anne B. , MANOHARAN, Muthiah , BHAT, Balkrishen , GRIFFEY, Richard , SWAYZE, Eric, E. , CROOKE, Stanely, T. , PRAKASH, Thazha, P.
CPC分类号： C12N15/1135 , C07H21/00 , C07H21/02 , C07H21/04 , C12N15/1137 , C12N2310/11 , C12N2310/14 , C12N2310/315 , C12N2310/321 , C12N2310/322 , C12N2310/341 , C12N2310/345 , C12N2310/346 , C12N2310/53 , 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.
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20.发明公开CARBOCYCLIC NUCLEOSIDE DERIVATIVES AS INHIBITORS OF RNA-DEPENDENT RNA VIRAL POLYMERASE 审中-公开碳环核苷病毒RNA依赖的RNA聚合酶的抑制剂
公开(公告)号：EP1515971A2
公开(公告)日：2005-03-23
申请号：EP03760371.9
申请日：2003-06-14
发明人： BHAT, Balkrishen , BHAT, Neelima , DANDE, Prasad , ELDRUP, Anne, B. , OLSEN, David, B. , MACCOSS, Malcolm
IPC分类号： C07D473/00 , C07D473/02 , C07D473/04 , C07D473/16 , C07D473/18 , C07D473/20 , C07D473/22 , C07D473/24 , C07D473/26 , C07D473/28 , C07D473/30 , C07D473/32 , C07D473/34 , C07D473/36 , C07D473/38 , C07D473/40 , A61K31/52 , A61K31/522 , A61P31/14
CPC分类号： C07H21/00
摘要： The present invention provides carbocyclic nucleoside compounds and certain derivatives thereof which are inhibitors of RNA-dependent RNA viral polymerase. These compounds are inhibitors of RNA-dependent RNA viral replication and are useful for the treatment of RNA-dependent RNA viral infection. They are particularly useful as inhibitors of hepatitis C virus (HCV) NS5B polymerase, as inhibitors of HCV replication, and/or for the treatment of hepatitis C infection. The invention also describes pharmaceutical compositions containing such carbocyclic nucleoside compounds alone or in combination with other agents active against RNA-dependent RNA viral infection, in particular HCV infection. Also disclosed are methods of inhibiting RNA-dependent RNA polymerase, inhibiting RNA-dependent RNA viral replication, and/or treating RNA-dependent RNA viral infection with the carbocyclic nucleoside compounds of the present invention
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