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1. 发明申请

WO2012027017A3 NOVEL AGONISTS OF TOLL-LIKE RECEPTOR 3 AND METHODS OF THEIR USE 审中-公开
公开(公告)号：WO2012027017A3
公开(公告)日：2012-03-01
申请号：PCT/US2011/041796
申请日：2011-06-24
申请人： IDERA PHARMACEUTICALS, INC. , KANDIMALLA, Ekambar , LAN, Tao , PHILBIN, Victoria, Jane , AGRAWAL, Sudhir
发明人： KANDIMALLA, Ekambar , LAN, Tao , PHILBIN, Victoria, Jane , AGRAWAL, Sudhir
IPC分类号： A61K48/00 , C07H21/00
摘要： TLR3 agonist compounds, compositions and methods are provided for stimulating the activity of TLR3. The compositions comprise oligonucleotide-based compounds that bind to and activate TLR3. The compositions may also comprise oligonucleotide-based compounds that bind to and activate TLR3 in combination with other therapeutic and/or prophylactic compounds and/or compositions. Methods of using these compounds and compositions for stimulation of TLR3 activity and for prevention or treatment of diseases wherein modulation of TLR3 activity would be beneficial are provided.

2. 发明申请

WO02074910A3 SELECTIVE ANTI-VIRAL NUCLEOSIDE CHAIN TERMINATORS 审中-公开
标题翻译：选择性抗病毒核素链终止子
公开(公告)号：WO02074910A3
公开(公告)日：2003-03-20
申请号：PCT/US0207447
申请日：2002-03-13
申请人： TRUSTEES OF BOSTON COLLEGE THE , MCLAUGHLIN LARRY W , FRALEY ANDREW W , CHEN DONGLI , LAN TAO
发明人： MCLAUGHLIN LARRY W , FRALEY ANDREW W , CHEN DONGLI , LAN TAO
IPC分类号： A61K31/70 , A61P31/12 , C07D471/02 , C07H19/048 , C07H19/052 , C07H19/06 , C07H19/10 , C07H19/23 , A61K31/44 , A61K31/505 , A61K31/675 , C07D213/02 , C07D239/02 , C07D405/04 , C07F9/02 , C07F9/06 , C04D471/02
CPC分类号： C07H19/048 , C07H19/052 , C07H19/06 , C07H19/10 , C07H19/23
摘要： The present invention relates to dideoxynucleoside analog compounds containing a dideoxy ribofuranosyl moiety that exhibit selective anti-viral activity coupled with substantially low toxicity toward the host cells. In particular, the compoounds according to the present invention show potent inhibition of the replication of the human immunodeficience virus (HIV), while remaining substantially inert toward host cell DNA. Compounds according to the present invention exhibit primary utility as agents for inhibiting the growth or replication of retroviruses, particularly HIV. The compounds of the invention comprise a (2, 3'-dideoxy- beta -ribofuranosyl) ring coupled to a heterocyclic nucleobase that lacks an "02 carbonyl", that enables them to selectively react with and inhibit viral reverse transcriptase, while remaining substantially unreactive toward human DNA polymerases.
摘要翻译：本发明涉及含有双脱氧呋喃核糖基部分的双脱氧核苷类似物化合物，其表现出选择性抗病毒活性，同时对宿主细胞具有显着低毒性。特别地，根据本发明的组合物显示对人免疫缺陷病毒（HIV）的复制的有效抑制，同时对宿主细胞DNA保持基本上惰性。根据本发明的化合物表现出用于抑制逆转录病毒，特别是HIV的生长或复制的药剂的主要用途。本发明的化合物包含与缺少“02羰基”的杂环核碱基偶联的（2，3'-二脱氧-β-呋喃核糖基）环，其使得它们能够选择性地与病毒逆转录酶反应并抑制病毒逆转录酶，同时保持基本上不反应针对人类DNA聚合酶。

3. 发明申请

WO2012135152A1 COMPOSITIONS FOR INHIBITING GENE EXPRESSION AND USES THEREOF 审中-公开
标题翻译：用于抑制基因表达的组合物及其用途
公开(公告)号：WO2012135152A1
公开(公告)日：2012-10-04
申请号：PCT/US2012/030626
申请日：2012-03-26
申请人： IDERA PHARMACEUTICALS, INC. , AGRAWAL, Sudhir , KANDIMALLA, Ekambar , PUTTA, Mallikarjuna , LAN, Tao , BHAGAT, Lakshmi , WANG, Daqing , YU, Dong
发明人： AGRAWAL, Sudhir , KANDIMALLA, Ekambar , PUTTA, Mallikarjuna , LAN, Tao , BHAGAT, Lakshmi , WANG, Daqing , YU, Dong
IPC分类号： C12N15/113 , A61K31/7088 , A61P35/00
CPC分类号： C12N15/113 , A61K31/7088 , A61K31/7105 , A61K31/712 , A61K31/713 , A61K38/02 , A61K39/00 , A61K39/35 , A61K39/395 , A61K45/06 , C12N15/111 , C12N15/1138 , C12N2310/113 , C12N2310/14 , C12N2310/317 , C12N2310/318 , C12N2310/344 , C12N2310/50 , C12N2310/51 , C12N2310/52 , C12N2320/30
摘要： The inventors have examined the means for providing more efficacious miRNA blocking compounds. The inventors have discovered new structural features that surprisingly improve the efficacy of miRNA 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 technology.
摘要翻译：本发明人已经研究了提供更有效的miRNA阻断化合物的方法。本发明人已经发现了惊人地改善miRNA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。

4. 发明申请

WO2010093705A3 SYNTHETIC RNA-BASED AGONISTS OF TLR7 审中-公开
标题翻译：合成基于RNA的TLR7激动剂
公开(公告)号：WO2010093705A3
公开(公告)日：2010-11-11
申请号：PCT/US2010023769
申请日：2010-02-10
申请人： IDERA PHARMACEUTICALS INC , LAN TAO , KANDIMALLA EKAMBAR R , WANG DAQING , AGRAWAL SUDHIR
发明人： LAN TAO , KANDIMALLA EKAMBAR R , WANG DAQING , AGRAWAL SUDHIR
IPC分类号： C12N15/117 , A61K31/7115 , A61K31/7125 , A61K39/39 , C07H21/02
CPC分类号： C12N15/117 , A61K2039/55561 , C12N2310/17 , C12N2310/315 , C12N2310/317 , C12N2310/3183 , C12N2310/333 , C12N2310/51 , C12N2320/31 , C12N2320/51
摘要： The invention relates to the therapeutic use of novel stabilized oligoribonucleotides as immune modulatory agents for immune therapy applications. Specifically, the invention provides novel RNA-based oligoribonucleotides with improved nuclease and RNase stability and that selectively induce immune modulatory activity through TLR7.
摘要翻译：本发明涉及新型稳定的寡核糖核苷酸作为免疫治疗应用的免疫调节剂的治疗用途。具体地说，本发明提供了具有改进的核酸酶和核糖核酸酶稳定性的新型基于RNA的寡核糖核苷酸，并通过TLR7选择性诱导免疫调节活性。

5. 发明申请

WO2010093705A2 SYNTHETIC RNA-BASED AGONISTS OF TLR7 审中-公开
标题翻译：合成RNA为基础的TLR7激动剂
公开(公告)号：WO2010093705A2
公开(公告)日：2010-08-19
申请号：PCT/US2010/023769
申请日：2010-02-10
申请人： IDERA PHARMACEUTICALS, INC. , LAN, Tao , KANDIMALLA, Ekambar, R. , WANG, Daqing , AGRAWAL, Sudhir
发明人： LAN, Tao , KANDIMALLA, Ekambar, R. , WANG, Daqing , AGRAWAL, Sudhir
IPC分类号： C12N15/113
CPC分类号： C12N15/117 , A61K2039/55561 , C12N2310/17 , C12N2310/315 , C12N2310/317 , C12N2310/3183 , C12N2310/333 , C12N2310/51 , C12N2320/31 , C12N2320/51
摘要： The invention relates to the therapeutic use of novel stabilized oligoribonucleotides as immune modulatory agents for immune therapy applications. Specifically, the invention provides novel RNA-based oligoribonucleotides with improved nuclease and RNase stability and that selectively induce immune modulatory activity through TLR7.
摘要翻译：本发明涉及新型稳定的寡核糖核苷酸作为用于免疫治疗应用的免疫调节剂的治疗用途。具体而言，本发明提供了具有改进的核酸酶和RNA酶稳定性并且通过TLR7选择性诱导免疫调节活性的新型基于RNA的寡核糖核苷酸。

6. 发明申请

WO2007117686A2 STABILIZED IMMUNE MODULATORY RNA (SIMRA) COMPOUNDS FOR TLR7 AND TLR8 审中-公开
标题翻译：稳定的免疫调节剂RNA（SIMRA）化合物用于TLR7和TLR8
公开(公告)号：WO2007117686A2
公开(公告)日：2007-10-18
申请号：PCT/US2007008739
申请日：2007-04-06
申请人： IDERA PHARMACEUTICALS INC , KANDIMALLA EKAMBAR R , LAN TAO , LI YUKUI , YU DONG , WANG DAQING , PUTTA MALLIKARJUNA REDDY , AGRAWAL SUDHIR
发明人： KANDIMALLA EKAMBAR R , LAN TAO , LI YUKUI , YU DONG , WANG DAQING , PUTTA MALLIKARJUNA REDDY , AGRAWAL SUDHIR
IPC分类号： A61K48/00 , A61K39/395 , C12N15/117
CPC分类号： C07K14/665 , A61K31/713 , A61K39/0005 , A61K39/395 , A61K39/3955 , C12N15/117 , C12N2310/17 , C12N2310/315 , C12N2310/318 , C12N2310/3183 , C12N2310/321 , C12N2310/33 , C12N2310/331 , C12N2310/336 , C12N2310/3521
摘要： The invention relates to the therapeutic use of stabilized oligoribonucleotides as immune modulatory agents for immune therapy applications. Specifically, the invention provides RNA based oligoribonucleotides with improved nuclease and RNase stability and that have immune modulatory activity through TLR7 and/or TLR8.
摘要翻译：本发明涉及稳定的寡核糖核苷酸作为免疫治疗应用的免疫调节剂的治疗用途。具体地，本发明提供具有改进的核酸酶和核糖核酸酶稳定性的基于RNA的寡核糖核苷酸，并且通过TLR7和/或TLR8具有免疫调节活性。

7. 发明申请

WO2009014887A3 STABILIZED IMMUNE MODULATORY RNA (SIMRA) COMPOUNDS 审中-公开
公开(公告)号：WO2009014887A3
公开(公告)日：2009-01-29
申请号：PCT/US2008/069335
申请日：2008-07-07
申请人： IDERA PHARMACEUTICALS, INC. , KANDIMALLA, Ekambar, R. , LAN, Tao , WANG, Daqing , BHAGAT, Lakshmi , AGRAWAL, Sudhir
发明人： KANDIMALLA, Ekambar, R. , LAN, Tao , WANG, Daqing , BHAGAT, Lakshmi , AGRAWAL, Sudhir
IPC分类号： A61K48/00
摘要： The invention relates to the therapeutic use of novel stabilized oligoribonucleotides as immune modulatory agents for immune therapy applications. Specifically, the invention provides novel RNA-based oligoribonucleotides with improved nuclease and RNase stability and that have immune modulatory activity through TLR7 and/or TLR8.

8. 发明申请

WO2007117686A3 STABILIZED IMMUNE MODULATORY RNA (SIMRA) COMPOUNDS FOR TLR7 AND TLR8 审中-公开
公开(公告)号：WO2007117686A3
公开(公告)日：2007-10-18
申请号：PCT/US2007/008739
申请日：2007-04-06
申请人： IDERA PHARMACEUTICALS, INC. , KANDIMALLA, Ekambar, R. , LAN, Tao , LI, Yukui , YU, Dong , WANG, Daqing , PUTTA, Mallikarjuna, Reddy , AGRAWAL, Sudhir
发明人： KANDIMALLA, Ekambar, R. , LAN, Tao , LI, Yukui , YU, Dong , WANG, Daqing , PUTTA, Mallikarjuna, Reddy , AGRAWAL, Sudhir
IPC分类号： A61K31/70 , A01N43/04 , C07H21/02 , C07H21/04 , A61K49/00 , A61K39/00
摘要： The invention relates to the therapeutic use of stabilized oligoribonucleotides as immune modulatory agents for immune therapy applications. Specifically, the invention provides RNA based oligoribonucleotides with improved nuclease and RNase stability and that have immune modulatory activity through TLR7 and/or TLR8.

9. 发明申请

WO2002074910A2 SELECTIVE ANTI-VIRAL NUCLEOSIDE CHAIN TERMINATORS 审中-公开
标题翻译：选择性抗病毒核素链终止子
公开(公告)号：WO2002074910A2
公开(公告)日：2002-09-26
申请号：PCT/US2002/007447
申请日：2002-03-13
申请人： TRUSTEES OF BOSTON COLLEGE, THE , MCLAUGHLIN, Larry, W. , FRALEY, Andrew, W. , CHEN, DongLi , LAN, Tao
发明人： MCLAUGHLIN, Larry, W. , FRALEY, Andrew, W. , CHEN, DongLi , LAN, Tao
IPC分类号： C12N
CPC分类号： C07H19/048 , C07H19/052 , C07H19/06 , C07H19/10 , C07H19/23
摘要： The present invention relates to dideoxynucleoside analog compounds containing a dideoxy ribofuranosyl moiety that exhibit selective anti-viral activity coupled with substantially low toxicity toward the host cells. In particular, the compoounds according to the present invention show potent inhibition of the replication of the human immunodeficience virus (HIV), while remaining substantially inert toward host cell DNA. Compounds according to the present invention exhibit primary utility as agents for inhibiting the growth or replication of retroviruses, particularly HIV. The compounds of the invention comprise a (2, 3'-dideoxy-β-ribofuranosyl) ring coupled to a heterocyclic nucleobase that lacks an "02 carbonyl", that enables them to selectively react with and inhibit viral reverse transcriptase, while remaining substantially unreactive toward human DNA polymerases.
摘要翻译：本发明涉及含有双脱氧呋喃核糖基部分的双脱氧核苷类似物化合物，其表现出选择性抗病毒活性，同时对宿主细胞具有显着低毒性。特别地，根据本发明的组合物显示对人免疫缺陷病毒（HIV）的复制的有效抑制，同时对宿主细胞DNA保持基本上惰性。根据本发明的化合物表现出用于抑制逆转录病毒，特别是HIV的生长或复制的药剂的主要用途。本发明的化合物包含与缺少“02羰基”的杂环核碱基偶联的（2，3'-二脱氧-β-呋喃核糖基）环，其使得它们能够选择性地与病毒逆转录酶反应并抑制病毒逆转录酶，同时保持基本上不反应针对人类DNA聚合酶。

10. 发明申请

WO2012027017A2 NOVEL AGONISTS OF TOLL-LIKE RECEPTOR 3 AND METHODS OF THEIR USE 审中-公开
标题翻译： TOLL样受体3的新激动剂及其使用方法
公开(公告)号：WO2012027017A2
公开(公告)日：2012-03-01
申请号：PCT/US2011041796
申请日：2011-06-24
申请人： IDERA PHARMACEUTICALS INC , KANDIMALLA EKAMBAR , LAN TAO , PHILBIN VICTORIA JANE , AGRAWAL SUDHIR
发明人： KANDIMALLA EKAMBAR , LAN TAO , PHILBIN VICTORIA JANE , AGRAWAL SUDHIR
IPC分类号： A61K39/00 , A61P37/04 , C07H21/02
CPC分类号： A61K39/39 , A61K2039/55561 , C12N15/117 , C12N2310/17 , C12N2310/315
摘要： TLR3 agonist compounds, compositions and methods are provided for stimulating the activity of TLR3. The compositions comprise oligonucleotide-based compounds that bind to and activate TLR3. The compositions may also comprise oligonucleotide-based compounds that bind to and activate TLR3 in combination with other therapeutic and/or prophylactic compounds and/or compositions. Methods of using these compounds and compositions for stimulation of TLR3 activity and for prevention or treatment of diseases wherein modulation of TLR3 activity would be beneficial are provided.
摘要翻译：提供TLR3激动剂化合物，组合物和方法用于刺激TLR3的活性。该组合物包含结合并活化TLR3的基于寡核苷酸的化合物。组合物还可以包含与其他治疗性和/或预防性化合物和/或组合物组合的结合并活化TLR3的基于寡核苷酸的化合物。提供了使用这些化合物和组合物刺激TLR3活性并预防或治疗其中TLR3活性的调节将是有益的疾病的方法。

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