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公开(公告)号：US20110082186A1
公开(公告)日：2011-04-07
申请号：US12869185
申请日：2010-08-26
申请人： Sudhir Agrawal , Ekambar Kandimalla , Mallikarjuna Putta , Tao Lan , Lakshmi Bhagat , Daqing Wang , Dong Yu
发明人： Sudhir Agrawal , Ekambar Kandimalla , Mallikarjuna Putta , Tao Lan , Lakshmi Bhagat , Daqing Wang , Dong Yu
IPC分类号： C07H21/00 , C07H21/02 , C07H21/04 , A61K31/7088 , A61P35/00 , A61P37/00 , A61P29/00 , A61P31/00 , A61P37/08 , A61P11/06 , A61P31/04 , A61P31/12 , A61P33/00 , A61P31/10
CPC分类号： C12N15/1138 , C12N2310/11 , C12N2310/152 , C12N2310/321 , C12N2310/3519 , C12N2310/51
摘要： The inventors have examined the means for providing more efficacious gene expression blocking compounds. The inventors have discovered new structural features that surprisingly improve the efficacy of gene expression blocking molecules. These features include the presence of multiple 3′ ends and a linker at the 5′ ends. Surprisingly, these features improve the efficacy of the gene expression blocking compounds in a manner that decreases the compound's biologic instability. Even more surprisingly, this effect has been found to be applicable to both DNA and RNA oligonucleotide-based compounds and to have application in traditional antisense and RNAi technologies.
摘要翻译： 本发明人已经研究了提供更有效的基因表达阻断化合物的方法。 发明人已经发现了惊人地改善基因表达阻断分子的功效的新结构特征。 这些特征包括多个3'末端的存在和在5'端的接头。 令人惊讶的是，这些特征以降低化合物生物学不稳定性的方式提高了基因表达阻断化合物的功效。 更令人惊奇的是，这种效应已经被发现适用于基于DNA和RNA的寡核苷酸类化合物，并且应用于传统的反义和RNAi技术。
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公开(公告)号：US08431544B1
公开(公告)日：2013-04-30
申请号：US12869209
申请日：2010-08-26
申请人： Sudhir Agrawal , Ekambar Kandimalla , Mallikarjuna Putta , Tao Lan , Lakshmi Bhagat , Daqing Wang , Dong Yu
发明人： Sudhir Agrawal , Ekambar Kandimalla , Mallikarjuna Putta , Tao Lan , Lakshmi Bhagat , Daqing Wang , Dong Yu
CPC分类号： C12N15/1138 , C12N2310/11 , C12N2310/152 , C12N2310/321 , C12N2310/3519 , C12N2310/51
摘要： The inventors have examined the means for providing more efficacious gene expression blocking compounds. The inventors have discovered new structural features that surprisingly improve the efficacy of gene expression blocking molecules. These features include the presence of multiple 3′ ends and a linker at the 5′ ends. Surprisingly, these features improve the efficacy of the gene expression blocking compounds in a manner that decreases the compound's biologic instability. Even more surprisingly, this effect has been found to be applicable to both DNA and RNA oligonucleotide-based compounds and to have application in traditional antisense and RNAi technologies.
摘要翻译： 本发明人已经研究了提供更有效的基因表达阻断化合物的方法。 发明人已经发现了惊人地改善基因表达阻断分子的功效的新结构特征。 这些特征包括多个3'末端的存在和在5'端的接头。 令人惊讶的是，这些特征以降低化合物生物学不稳定性的方式提高了基因表达阻断化合物的功效。 更令人惊奇的是，这种效应已经被发现适用于基于DNA和RNA的寡核苷酸类化合物，并且应用于传统的反义和RNAi技术。
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3.发明申请公开(公告)号：US20100111937A1
公开(公告)日：2010-05-06
申请号：US12612413
申请日：2009-11-04
申请人： Ekambar Kandimalla , Mallikarjuna Putta , Lakshmi Bhagat , Daqing Wang , Dong Yu , Sudhir Agrawal
发明人： Ekambar Kandimalla , Mallikarjuna Putta , Lakshmi Bhagat , Daqing Wang , Dong Yu , Sudhir Agrawal
IPC分类号： A61K48/00 , C07H21/02 , A61K39/00 , A61K39/395 , A61K39/35 , A61K38/02 , A61P29/00 , A61P31/00
CPC分类号： A61K39/39 , A61K2039/55561 , C07H21/04 , C12N15/1138 , C12N2310/11 , Y02A50/401 , Y02A50/412 , Y02A50/414
摘要： Antisense oligonucleotide compounds, compositions and methods are provided for down regulating the expression of TLR5. The compositions comprise antisense oligonucleotides targeted to nucleic acids encoding TLR5. The compositions may also comprise antisense oligonucleotides targeted to nucleic acids encoding TLR5 in combination with other therapeutic and/or prophylactic compounds and/or compositions. Methods of using these compounds and compositions for down-regulating TLR5 expression and for prevention or treatment of diseases wherein modulation of TLR5 expression would be beneficial are provided.
摘要翻译： 提供反义寡核苷酸化合物，组合物和方法用于下调TLR5的表达。 组合物包含靶向编码TLR5的核酸的反义寡核苷酸。 组合物还可以包含靶向编码TLR5的核酸与其它治疗和/或预防化合物和/或组合物组合的反义寡核苷酸。 提供这些化合物和组合物用于下调TLR5表达和预防或治疗TLR5表达调节将是有益的疾病的方法。
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公开(公告)号：US20080292648A1
公开(公告)日：2008-11-27
申请号：US11954726
申请日：2007-12-12
申请人： Ekambar Kandimalla , Mallikarjuna Putta , Dong Yu , Lakshmi Bhagat , Daqing Wang , Sudhir Agrawal
发明人： Ekambar Kandimalla , Mallikarjuna Putta , Dong Yu , Lakshmi Bhagat , Daqing Wang , Sudhir Agrawal
CPC分类号： C12N15/117 , C12N2310/17 , C12N2310/315 , C12N2310/317 , C12N2310/3183 , C12N2310/321 , C12N2310/336 , C12N2310/3521
摘要： The invention provides novel oligonucleotide-based compounds that individually provide distinct immune response profiles through their interactions as agonists with TLR9. The TLR9 agonists according to the invention are characterized by specific and unique chemical modifications, which provide their distinctive immune response activation profiles.
摘要翻译： 本发明提供了新的基于寡核苷酸的化合物，其通过作为具有TLR9的激动剂的相互作用单独提供不同的免疫应答谱。 根据本发明的TLR9激动剂的特征在于特异性和独特的化学修饰，其提供其独特的免疫应答活化谱。
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5.发明授权Modulation of toll-like receptor 5 expression by antisense oligonucleotides 失效通过反义寡核苷酸调节toll样受体5的表达公开(公告)号：US08153777B2
公开(公告)日：2012-04-10
申请号：US12612413
申请日：2009-11-04
申请人： Ekambar Kandimalla , Mallikarjuna Putta , Lakshmi Bhagat , Daqing Wang , Dong Yu , Sudhir Agrawal
发明人： Ekambar Kandimalla , Mallikarjuna Putta , Lakshmi Bhagat , Daqing Wang , Dong Yu , Sudhir Agrawal
IPC分类号： C07H21/04 , C07H21/02 , A61K48/00 , A61K39/395 , C12N15/63
CPC分类号： A61K39/39 , A61K2039/55561 , C07H21/04 , C12N15/1138 , C12N2310/11 , Y02A50/401 , Y02A50/412 , Y02A50/414
摘要： Antisense oligonucleotide compounds, compositions and methods are provided for down regulating the expression of TLR5. The compositions comprise antisense oligonucleotides targeted to nucleic acids encoding TLR5. The compositions may also comprise antisense oligonucleotides targeted to nucleic acids encoding TLR5 in combination with other therapeutic and/or prophylactic compounds and/or compositions. Methods of using these compounds and compositions for down-regulating TLR5 expression and for prevention or treatment of diseases wherein modulation of TLR5 expression would be beneficial are provided.
摘要翻译： 提供反义寡核苷酸化合物，组合物和方法用于下调TLR5的表达。 组合物包含靶向编码TLR5的核酸的反义寡核苷酸。 组合物还可以包含靶向编码TLR5的核酸与其它治疗和/或预防化合物和/或组合物组合的反义寡核苷酸。 提供这些化合物和组合物用于下调TLR5表达和预防或治疗TLR5表达调节将是有益的疾病的方法。
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6.发明申请公开(公告)号：US20100047188A1
公开(公告)日：2010-02-25
申请号：US12534476
申请日：2009-08-03
申请人： Ekambar Kandimalla , Mallikarjuna Putta , Lakshmi Bhagat , Daqing Wang , Dong Yu , Sudhir Agrawal
发明人： Ekambar Kandimalla , Mallikarjuna Putta , Lakshmi Bhagat , Daqing Wang , Dong Yu , Sudhir Agrawal
IPC分类号： A61K9/12 , C07H21/04 , A61K31/7088 , A61K39/395 , A61K38/00 , A61K39/00
CPC分类号： A61K31/7125 , A61K9/127 , C12N15/1138 , C12N2310/11 , C12N2310/315 , C12N2310/321 , C12N2310/341 , Y02A50/401 , Y02A50/411 , Y02A50/414 , C12N2310/3521
摘要： Antisense oligonucleotide compounds, compositions and methods are provided for down regulating the expression of TLR8. The compositions comprise antisense oligonucleotides targeted to nucleic acids encoding TLR8. The compositions may also comprise antisense oligonucleotides targeted to nucleic acids encoding TLR8 in combination with other therapeutic and/or prophylactic compounds and/or compositions. Methods of using these compounds and compositions for down-regulating TLR8 expression and for prevention or treatment of diseases wherein modulation of TLR8 expression would be beneficial are provided.
摘要翻译： 提供反义寡核苷酸化合物，组合物和方法用于下调TLR8的表达。 组合物包含靶向编码TLR8的核酸的反义寡核苷酸。 组合物还可包含靶向编码TLR8的核酸与其它治疗和/或预防化合物和/或组合物组合的反义寡核苷酸。 提供这些化合物和组合物用于下调TLR8表达和预防或治疗其中调节TLR8表达将是有益的疾病的方法。
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7.发明申请MODULATION OF TOLL-LIKE RECEPTOR 7 EXPRESSION BY ANTISENSE OLIGONUCLEOTIDES 审中-公开抗体寡核苷酸表达类似受体受体7的表达调控公开(公告)号：US20100041734A1
公开(公告)日：2010-02-18
申请号：US12534462
申请日：2009-08-03
申请人： Ekambar Kandimalla , Mallikarjuna Putta , Lakshmi Bhagat , Daqing Wang , Dong Yu , FuGang Zhu , Sudhir Agrawal
发明人： Ekambar Kandimalla , Mallikarjuna Putta , Lakshmi Bhagat , Daqing Wang , Dong Yu , FuGang Zhu , Sudhir Agrawal
CPC分类号： A61K31/7105 , Y02A50/401 , Y02A50/411 , Y02A50/414
摘要： Antisense oligonucleotide compounds, compositions and methods are provided for down regulating the expression of TLR7. The compositions comprise antisense oligonucleotides targeted to nucleic acids encoding TLR7. The compositions may also comprise antisense oligonucleotides targeted to nucleic acids encoding TLR7 in combination with other therapeutic and/or prophylactic compounds and/or compositions. Methods of using these compounds and compositions for down-regulating TLR7 expression and for prevention or treatment of diseases wherein modulation of TLR7 expression would be beneficial are provided.
摘要翻译： 提供反义寡核苷酸化合物，组合物和方法用于下调TLR7的表达。 组合物包含靶向编码TLR7的核酸的反义寡核苷酸。 组合物还可以包含靶向编码TLR7的核酸与其它治疗和/或预防化合物和/或组合物组合的反义寡核苷酸。 提供了这些化合物和组合物用于下调TLR7表达和预防或治疗其中调节TLR7表达将是有益的疾病的方法。
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8.发明申请Modulation of Toll-Like Receptor 2 Expression By Antisense Oligonucleotides 审中-公开通过反义寡核苷酸调节Toll样受体2表达公开(公告)号：US20100111935A1
公开(公告)日：2010-05-06
申请号：US12612370
申请日：2009-11-04
申请人： Lakshmi Bhagat , Ekambar Kandimalla , Mallikarjuna Putta , Daqing Wang , Dong Yu , Sudhir Agrawal
发明人： Lakshmi Bhagat , Ekambar Kandimalla , Mallikarjuna Putta , Daqing Wang , Dong Yu , Sudhir Agrawal
CPC分类号： C12N15/1138 , C07H21/00 , C12N2310/11
摘要： Antisense oligonucleotide compounds, compositions and methods are provided for down regulating the expression of TLR2. The compositions comprise antisense oligonucleotides targeted to nucleic acids encoding TLR2. The compositions may also comprise antisense oligonucleotides targeted to nucleic acids encoding TLR2 in combination with other therapeutic and/or prophylactic compounds and/or compositions. Methods of using these compounds and compositions for down-regulating TLR2 expression and for prevention or treatment of diseases wherein modulation of TLR2 expression would be beneficial are provided.
摘要翻译： 提供反义寡核苷酸化合物，组合物和方法用于下调TLR2的表达。 组合物包含靶向编码TLR2的核酸的反义寡核苷酸。 组合物还可以包含靶向编码TLR2的核酸与其它治疗和/或预防化合物和/或组合物组合的反义寡核苷酸。 提供这些化合物和组合物用于下调TLR2表达和预防或治疗其中调节TLR2表达将是有益的疾病的方法。
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公开(公告)号：US07960362B2
公开(公告)日：2011-06-14
申请号：US12183439
申请日：2008-07-31
申请人： Ekambar Kandimalla , Mallikarjuna Putta , Daqing Wang , Dong Yu , Lakshmi Bhagat , Sudhir Agrawal
发明人： Ekambar Kandimalla , Mallikarjuna Putta , Daqing Wang , Dong Yu , Lakshmi Bhagat , Sudhir Agrawal
CPC分类号： A61K31/711 , A61K39/39
摘要： The invention relates to synthetic chemical compositions that are useful for modulation of Toll-Like Receptor (TLR)-mediated immune responses. In particular, the invention relates to agonists of Toll-Like Receptor 9 (TLR9) that generate unique cytokine and chemokine profiles.
摘要翻译： 本发明涉及可用于调节Toll样受体（TLR）介导的免疫应答的合成化学组合物。 特别地，本发明涉及产生独特细胞因子和趋化因子分布的Toll样受体9（TLR9）的激动剂。
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公开(公告)号：US07884197B2
公开(公告)日：2011-02-08
申请号：US11954726
申请日：2007-12-12
申请人： Ekambar Kandimalla , Mallikarjuna Putta , Dong Yu , Lakshmi Bhagat , Daqing Wang , Sudhir Agrawal
发明人： Ekambar Kandimalla , Mallikarjuna Putta , Dong Yu , Lakshmi Bhagat , Daqing Wang , Sudhir Agrawal
CPC分类号： C12N15/117 , C12N2310/17 , C12N2310/315 , C12N2310/317 , C12N2310/3183 , C12N2310/321 , C12N2310/336 , C12N2310/3521
摘要： The invention provides novel oligonucleotide-based compounds that individually provide distinct immune response profiles through their interactions as agonists with TLR9. The TLR9 agonists according to the invention are characterized by specific and unique chemical modifications, which provide their distinctive immune response activation profiles.
摘要翻译： 本发明提供了新的基于寡核苷酸的化合物，其通过作为具有TLR9的激动剂的相互作用单独提供不同的免疫应答谱。 根据本发明的TLR9激动剂的特征在于特异性和独特的化学修饰，其提供其独特的免疫应答活化谱。
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