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91. 发明申请

US20060135454A1 Modulation of immunostimulatory activity of immunostimulatory oligonucleotide analogs by positional chemical changes 失效
公开(公告)号：US20060135454A1
公开(公告)日：2006-06-22
申请号：US10694207
申请日：2003-10-27
申请人： Ekambar Kandimalla , Qiuyan Zhao , Dong Yu , Sudhir Agrawal
发明人： Ekambar Kandimalla , Qiuyan Zhao , Dong Yu , Sudhir Agrawal
IPC分类号： A61K48/00
CPC分类号： C12N15/117 , A61K31/7088 , A61K31/7115 , A61K2039/55561 , C07H21/00 , C12N2310/18 , C12N2310/3125 , C12N2310/317 , C12N2310/318 , C12N2310/32 , C12N2310/321 , C12N2310/33 , C12N2310/334 , C12N2310/336 , C12N2310/3521
摘要： The invention relates to the therapeutic use of oligonucleotides or oligonucleotide analogs as immunostimulatory agents in immunotherapy applications. The invention provides methods for enhancing the immune response caused by immunostimulatory oligonucleotide compounds.

92. 发明申请

US20060094680A1 Immunostimulatory oligonucleotide multimers 有权
公开(公告)号：US20060094680A1
公开(公告)日：2006-05-04
申请号：US11234074
申请日：2005-09-22
申请人： Sudhir Agrawal , Ekambar Kandimalla , Dong Yu
发明人： Sudhir Agrawal , Ekambar Kandimalla , Dong Yu
IPC分类号： A61K31/70 , A01N43/04
CPC分类号： A61K39/39 , A61K2039/55561
摘要： The invention provides an immunostimulatory nucleic acid. In certain embodiments according to this aspect of the invention, the sequence of the immunostimulatory oligonucleotide and/or immunomer is at least partially self-complementary.

93. 发明授权

US06509459B1 Base protecting groups and rapid process for oligonucleotide synthesis 失效
标题翻译：碱基保护基和寡核苷酸合成的快速过程
公开(公告)号：US06509459B1
公开(公告)日：2003-01-21
申请号：US08846303
申请日：1997-04-30
申请人： Sudhir Agrawal , Radhakrishnan P. Iyer , Ivan Habus , Dong Yu
发明人： Sudhir Agrawal , Radhakrishnan P. Iyer , Ivan Habus , Dong Yu
IPC分类号： C07H2100
CPC分类号： C07H21/00 , C07H19/10 , C07H19/16 , C07H19/20 , Y02P20/55
摘要： The invention provides new processes for synthesizing oligonucleotides that allow for deprotection of the oligonucleotide under more rapid and/or more mild conditions than existing methods. The invention further provides a nucleoside base protecting group that is stable under oligonucleotide synthesis conditions, but which can be removed under more mild conditions than existing protecting groups, as well as nucleoside synthons having such base protecting groups. The invention also provides oligonucleotides containing any of a variety of base labile functionalities and methods for using such oligonucleotides.
摘要翻译：本发明提供了合成寡核苷酸的新方法，其允许寡核苷酸在比现有方法更快和/或更温和的条件下脱保护。本发明还提供了在寡核苷酸合成条件下稳定但可被除去的核苷碱基保护基在比现有保护基更温和的条件下，以及具有这种碱保护基的核苷合成子。本发明还提供了含有各种碱不稳定功能的寡核苷酸的寡核苷酸和使用这些寡核苷酸的方法。

94. 发明授权

US6140482A Primary phosphoramidate internucleoside linkages and oligonucleotides containing the same 失效
标题翻译：初级氨基磷酸核苷间核苷键和含有其的寡核苷酸
公开(公告)号：US6140482A
公开(公告)日：2000-10-31
申请号：US519318
申请日：1995-08-25
申请人： Radhakrishnan P. Iyer , Theresa Devlin , Ivan Habus , Dong Yu , Sudhir Agrawal
发明人： Radhakrishnan P. Iyer , Theresa Devlin , Ivan Habus , Dong Yu , Sudhir Agrawal
IPC分类号： C07H19/10 , C07H19/16 , C07H19/20 , C07H21/00
CPC分类号： C07H19/10 , C07H19/16 , C07H19/20 , C07H21/00
摘要： The invention provides new primary phosphoramidate internucleoside linkages that are less sterically constrained than existing phosphoramidate linkages, as well as oligonucleotides containing such linkages and processes for making and methods for using such oligonucleotides.
摘要翻译：本发明提供了比现有氨基磷酸酯键更少的空间限制的新的初级氨基磷酸酯核苷间键，以及含有这种连接的寡核苷酸和制备方法以及使用这种寡核苷酸的方法。

95. 发明授权

US5631361A Method of synthesizing radioisotopically labeled oligonucleotides by direct solid-phase 5' phosphitylation 失效
标题翻译：通过直接固相5'磷酸化合成放射性同位素标记的寡核苷酸的方法
公开(公告)号：US5631361A
公开(公告)日：1997-05-20
申请号：US447092
申请日：1995-05-22
申请人： Weitian Tan , Radhakrishnan P. Iyer , Zhiwei Jiang , Dong Yu , Sudhir Agrawal
发明人： Weitian Tan , Radhakrishnan P. Iyer , Zhiwei Jiang , Dong Yu , Sudhir Agrawal
IPC分类号： C07H21/00 , C07H1/02
CPC分类号： C07H21/00
摘要： The present invention comprises a novel method of incorporating radiolabels and other type of labels at one or more predetermined sites within an oligonucleotide. In particular, the method comprises contacting a nascent, support-bound oligonucleotide having an unprotected 5' hydroxyl group with a suitable activating agent, followed by contacting the resulting activated nascent oligonucleotide with a labeled, Y-protected mononucleotide having an unprotected 3'-hydroxyl, thereby condensing the labeled mononucleotide and nascent oligonucleotide. Normal automated synthesis can then be continued to yield the oligonucleotide of desired length having the label in the desired location. This method advantageously yields oligonucleotides with high specific activity. The oligonucleotides thereby produced are useful for determining the pharmacokinetics and biodistribution of their non-radiolabeled counterparts, both in vitro and in vivo.
摘要翻译：本发明包括在寡核苷酸内的一个或多个预定位点掺入放射性标记和其他类型的标记的新方法。特别地，该方法包括将具有未保护的5'羟基的新生支持结合的寡核苷酸与合适的活化剂接触，然后将所得活化的新生寡核苷酸与具有未保护的3'-羟基的标记的受Y保护的单核苷酸接触从而使标记的单核苷酸和新生寡核苷酸缩合。然后可以继续进行正常的自动合成，得到所需长度的寡核苷酸，其具有所需位置的标记。该方法有利地产生具有高比活性的寡核苷酸。由此产生的寡核苷酸可用于在体外和体内测定其非放射性标记的对应物的药代动力学和生物分布。

96. 发明授权

US5614622A 5-pentenoyl moiety as a nucleoside-amino protecting group, 4-pentenoyl-protected nucleotide synthons, and related oligonucleotide syntheses 失效
标题翻译： 5-戊烯酰基部分作为核苷 - 氨基保护基，4-戊烯酰基保护的核苷酸合成子和相关的寡核苷酸合成
公开(公告)号：US5614622A
公开(公告)日：1997-03-25
申请号：US518921
申请日：1995-08-24
申请人： Radhakrishnan P. Iyer , Theresa Devlin , Ivan Habus , Dong Yu , Sudhir Agrawal
发明人： Radhakrishnan P. Iyer , Theresa Devlin , Ivan Habus , Dong Yu , Sudhir Agrawal
IPC分类号： C07H19/10 , C07H19/16 , C07H19/20 , C07H21/00 , C07H19/06
CPC分类号： C07H19/16 , C07H19/10 , C07H19/20 , C07H21/00 , Y02P20/55
摘要： The invention provides new methods for synthesizing oligonucleotides that allow for deprotection of the oligonucleotide under more mild conditions than existing methods. The invention further provides a nucleoside base protective group that is stable under oligonucleotide synthesis conditions, but which can be removed under more mild conditions than existing protective groups, as well as nucleoside synthons having such base protective groups.
摘要翻译：本发明提供了合成寡核苷酸的新方法，其允许寡核苷酸在比现有方法更温和的条件下脱保护。本发明还提供了在寡核苷酸合成条件下稳定但可在比现有保护基更温和的条件下除去的核苷碱基保护基以及具有这种碱性保护基的核苷合成子。

97. 发明授权

US07566702B2 Immunostimulatory oligonucleotide multimers 失效
标题翻译：免疫刺激寡核苷酸多聚体
公开(公告)号：US07566702B2
公开(公告)日：2009-07-28
申请号：US11234075
申请日：2005-09-22
申请人： Sudhir Agrawal , Ekambar Kandimalla , Dong Yu
发明人： Sudhir Agrawal , Ekambar Kandimalla , Dong Yu
IPC分类号： C07H21/02 , C07H21/04 , A01N43/04 , A61K31/70
CPC分类号： A61K39/39 , A61K2039/55561
摘要： The invention provides an immunostimulatory nucleic acid. In certain embodiments according to this aspect of the invention, the sequence of the immunostimulatory oligonucleotide and/or immunomer is at least partially self-complementary.
摘要翻译：本发明提供免疫刺激性核酸。在根据本发明的该方面的某些实施方案中，免疫刺激性寡核苷酸和/或免疫反应物的序列至少部分自身互补。

98. 发明申请

US20070179103A1 Immunostimulatory oligonucleotide multimers 失效
标题翻译：免疫刺激寡核苷酸多聚体
公开(公告)号：US20070179103A1
公开(公告)日：2007-08-02
申请号：US11234396
申请日：2005-09-22
申请人： Sudhir Agrawal , Ekambar Kandimalla , Dong Yu
发明人： Sudhir Agrawal , Ekambar Kandimalla , Dong Yu
IPC分类号： A61K48/00 , A61K8/96 , A61K39/395 , A61K39/00 , C07H21/04
CPC分类号： A61K31/711 , A61K38/2013 , A61K39/39 , A61K2039/55561 , A61N2005/1098 , C12N15/117 , C12N2310/17 , C12N2310/315 , C12N2310/318 , C12N2310/334 , C12N2310/336 , C12N2310/3519 , A61K2300/00
摘要： The invention provides an immunostimulatory nucleic acid. In certain embodiments according to this aspect of the invention, the sequence of the immunostimulatory oligonucleotide and/or immunomer is at least partially self-complementary.
摘要翻译：本发明提供免疫刺激性核酸。在根据本发明的该方面的某些实施方案中，免疫刺激性寡核苷酸和/或免疫反应物的序列至少部分自身互补。

99. 发明申请

US20070105800A1 Immunostimulatory properties of oligonucleotide-based compounds comprising modified immunostimulatory dinucleotides 有权
标题翻译：包含修饰的免疫刺激二核苷酸的基于寡核苷酸的化合物的免疫刺激性质
公开(公告)号：US20070105800A1
公开(公告)日：2007-05-10
申请号：US11268683
申请日：2005-11-07
申请人： Sudhir Agrawal , Dong Yu , Ekambar Kandimalla
发明人： Sudhir Agrawal , Dong Yu , Ekambar Kandimalla
IPC分类号： A61K48/00 , C07H21/04
CPC分类号： A61K39/39 , A61K2039/55561
摘要： The invention relates to the therapeutic use of oligonucleotides as immunostimulatory agents in immunotherapy applications. More particularly, the invention provides an immunostimulatory oligonucleotides for use in methods for generating an immune response or for treating a patient in need of immunostimulation. The immunostimulatory oligonucleotides of the invention preferably comprise novel purines. The immunostimulatory oligonucleotides according to the invention further comprise at least two oligonucleotides linked at their 3′ ends, internucleoside linkages or functionalized nucleobase or sugar to a non-nucleotidic linker, at least one of the oligonucleotides being an immunostimulatory oligonucleotide and having an accessible 5′ end.
摘要翻译：本发明涉及在免疫治疗应用中寡核苷酸作为免疫刺激剂的治疗用途。更具体地，本发明提供了用于产生免疫应答的方法或用于治疗需要免疫刺激的患者的免疫刺激性寡核苷酸。本发明的免疫刺激性寡核苷酸优选包含新的嘌呤。根据本发明的免疫刺激性寡核苷酸还包含至少两个在其3'末端连接的寡核苷酸，核苷间键或官能化核碱基或糖与非核酸连接体，至少一个寡核苷酸是免疫刺激性寡核苷酸并具有可接近的5' 结束。

100. 发明申请

US20070072198A1 Modulation of immunostimulatory activity of immunostimulatory oligonucleotide analogs by positional chemical changes 有权
标题翻译：通过位置化学变化调节免疫刺激性寡核苷酸类似物的免疫刺激活性
公开(公告)号：US20070072198A1
公开(公告)日：2007-03-29
申请号：US11270805
申请日：2005-11-09
申请人： Ekambar Kandimalla , Qiuyan Zhao , Dong Yu , Sudhir Agrawal
发明人： Ekambar Kandimalla , Qiuyan Zhao , Dong Yu , Sudhir Agrawal
IPC分类号： C12Q1/70 , C12Q1/68
CPC分类号： C12N15/117 , A61K31/7088 , A61K31/7115 , A61K2039/55561 , C07H21/00 , C12N2310/18 , C12N2310/3125 , C12N2310/317 , C12N2310/318 , C12N2310/32 , C12N2310/321 , C12N2310/33 , C12N2310/334 , C12N2310/336 , C12N2310/3521
摘要： The invention relates to the therapeutic use of oligonucleotides or oligonucleotide analogs as immunostimulatory agents in immunotherapy applications. The invention provides methods for enhancing the immune response caused by immunostimulatory oligonucleotide compounds.
摘要翻译：本发明涉及在免疫治疗应用中寡核苷酸或寡核苷酸类似物作为免疫刺激剂的治疗用途。本发明提供了增强由免疫刺激性寡核苷酸化合物引起的免疫应答的方法。

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