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81. 发明申请

US20080193437A1 IMMUNOSTIMULATORY OLIGONUCLEOTIDE MULTIMERS 审中-公开
标题翻译：免疫组织寡核苷酸多态性
公开(公告)号：US20080193437A1
公开(公告)日：2008-08-14
申请号：US11876913
申请日：2007-10-23
申请人： Sudhir Agrawal , Ekambar Kandimalla , Dong Yu
发明人： Sudhir Agrawal , Ekambar Kandimalla , Dong Yu
IPC分类号： A61K39/35 , A61K31/711 , A61K39/395 , A61K38/02 , A61K39/00 , A61K45/00
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。

82. 发明授权

US07405285B2 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：US07405285B2
公开(公告)日：2008-07-29
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： C07H21/02
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。

83. 发明授权

US06531589B1 Base protecting groups and synthons for oligonucleotide synthesis 失效
标题翻译：用于寡核苷酸合成的碱基保护基和合成子
公开(公告)号：US06531589B1
公开(公告)日：2003-03-11
申请号：US08598320
申请日：1996-02-08
申请人： Radhakrishnan P. Iyer , Theresa Devlin , Ivan Habus , Dong Yu , Sudhir Agrawal , Nan-Hui Ho
发明人： Radhakrishnan P. Iyer , Theresa Devlin , Ivan Habus , Dong Yu , Sudhir Agrawal , Nan-Hui Ho
IPC分类号： C07H2100
CPC分类号： C07H19/10 , C07H19/16 , C07H19/20 , C07H21/00 , Y02P20/55
摘要： The invention provides new methods for synthesizing oligonucleotides that allow for deprotection of the oligonucleotides under 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.
摘要翻译：本发明提供了合成寡核苷酸的新方法，其允许在比现有方法更温和的条件下对寡核苷酸进行脱保护。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保护基，以及具有这种碱保护基的核苷合成子。

84. 发明授权

US6117993A Synthons for oligonucleotide synthesis 失效
标题翻译：合成寡核苷酸合成
公开(公告)号：US6117993A
公开(公告)日：2000-09-12
申请号：US15472
申请日：1998-01-29
申请人： Radhakrishnan P. Iyer , Dong Yu , Mao-Jun Guo , Sudhir Agrawal
发明人： Radhakrishnan P. Iyer , Dong Yu , Mao-Jun Guo , Sudhir Agrawal
IPC分类号： C07H19/11 , C07H19/10 , C07H19/16 , C07H19/20 , C07H19/213 , C07H21/00 , C07H19/04
CPC分类号： C07H19/10 , C07H19/16 , C07H19/20 , C07H21/00
摘要： The invention provides new reagents and processes for synthesizing oligonucleotides, including stereoselective oligonucleotide synthesis. In a first aspect, the invention provides novel monomer synthons for the synthesis of oligonucleotides. Monomer synthons according to this aspect of the invention are useful in the synthesis of oligonucleotides and can be used in place of the well known beta-cyanoethyl phosphoramidite monomer synthon in the phosphoramidite synthesis procedure. Certain monomer synthons according to this aspect of the invention are useful in this procedure for producing oligonucleotides having defined stereochemistry.In a second aspect, the invention provides processes for synthesizing monomer synthons according to the invention, including diastereomerically enriched or purified monomer synthons. In the processes according to this aspect of the invention, the chemical reactions are stereoretentive so that the products of each reaction retain the same stereoconfiguration as their precursor reagent.In a third aspect, the invention provides processes for synthesizing oligonucleotides using the well known phosphoramidite approach. In the processes according to this aspect of the invention, any of the monomer synthons according to the invention is used in place of the conventional beta-cyanoethyl phosphoramidite.
摘要翻译：本发明提供用于合成寡核苷酸的新试剂和方法，包括立体选择性寡核苷酸合成。在第一方面，本发明提供了用于合成寡核苷酸的新型单体合成子。根据本发明该方面的单体合成子可用于寡核苷酸的合成，并可用于代替在亚磷酰胺合成方法中众所周知的β-氰乙基亚磷酰胺单体合成子。根据本发明该方面的某些单体合成子可用于制备具有确定的立体化学的寡核苷酸的该方法中。在第二方面，本发明提供了合成根据本发明的单体合成子的方法，包括非对映体富集或纯化的单体合成子。在根据本发明的这个方面的方法中，化学反应是立体反应性的，使得每个反应的产物保持与其前体试剂相同的立体构型。在第三方面，本发明提供使用公知的亚磷酰胺方法合成寡核苷酸的方法。在根据本发明的这个方面的方法中，使用根据本发明的任何单体合成物代替常规的β-氰基乙基亚磷酰胺。

85. 发明授权

US5962674A Synthesis of oligonucleotides containing alkylphosphonate internucleoside linkages 失效
标题翻译：含有烷基膦酸酯核苷间键的寡核苷酸的合成
公开(公告)号：US5962674A
公开(公告)日：1999-10-05
申请号：US606915
申请日：1996-02-26
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 , Y02P20/55
摘要： The invention provides new reagents and an improved process for synthesizing oligonucleotides that contain methylphosphonate internucleoside linkages. The reagents and process utilize 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.
摘要翻译：本发明提供新的试剂和用于合成含有甲基膦酸核苷间键的寡核苷酸的改进方法。试剂和方法利用在寡核苷酸合成条件下稳定的核苷碱基保护基，但可以在比现有保护基更温和的条件下除去。

86. 发明授权

US5955599A Process for making oligonucleotides containing o- and s- methylphosphotriester internucleoside linkages 失效
标题翻译：制备含有O-和S-甲基磷酸核苷间核苷键的寡核苷酸的方法
公开(公告)号：US5955599A
公开(公告)日：1999-09-21
申请号：US570390
申请日：1995-12-11
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 , C07H21/04
CPC分类号： C07H19/10 , C07H19/16 , C07H19/20 , C07H21/00
摘要： The invention provides oligonucleotides containing methyl phosphotriester linkages and processes for making and methods for using such oligonucleotides.
摘要翻译：本发明提供了含有甲基磷酸三酯键的寡核苷酸及其制备方法和使用这些寡核苷酸的方法。

87. 发明授权

US5750674A Methods and compounds for the stereoselective enrichment of oligonucleotide diastereomers and oligonucleotides thereby produced 失效
标题翻译：由此制备寡核苷酸非对映异构体和寡核苷酸的立体选择性富集的方法和化合物
公开(公告)号：US5750674A
公开(公告)日：1998-05-12
申请号：US448131
申请日：1995-05-23
申请人： Radhakrishnan P. Iyer , Dong Yu , Sudhir Agrawal , Weitian Tan
发明人： Radhakrishnan P. Iyer , Dong Yu , Sudhir Agrawal , Weitian Tan
IPC分类号： C07H19/10 , C07H19/20 , C07H21/00
CPC分类号： C07H21/00 , C07H19/10 , C07H19/20
摘要： The present invention provides new mononucleotide synthons useful in the synthesis of oligonucleotides having from one to all P-chiral centers that are predominantly and independently in the R or S configuration. The invention also provides methods of synthesizing these synthons, methods of synthesizing oligonucleotides having from one to all P-chiral centers predominantly and independently in the R or S configuration, and such oligonucleotides. Oligonucleotides synthesized with the novel synthons are useful for modulating nucleic acid expression, both in vitro and in vivo, as well as in traditional hybridization assays.
摘要翻译：本发明提供了可用于合成寡核苷酸的新的单核苷酸合成子，所述寡核苷酸具有主要且独立于R或S构型的一个至所有P-手性中心。本发明还提供了合成这些合成子的方法，合成寡核苷酸的方法，所述寡核苷酸主要以R或S构型主要且独立地具有一个至所有的P-手性中心，以及这些寡核苷酸。用新型合成子合成的寡核苷酸可用于在体外和体内以及传统杂交测定中调节核酸表达。

88. 发明授权

US07498426B2 Immunostimulatory oligonucleotide multimers 有权
公开(公告)号：US07498426B2
公开(公告)日：2009-03-03
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： C07H21/02 , C07H21/00 , C07H19/00
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.

89. 发明授权

US07427405B2 Immunostimulatory oligonucleotide multimers 有权
公开(公告)号：US07427405B2
公开(公告)日：2008-09-23
申请号：US11174282
申请日：2005-07-01
申请人： Sudhir Agrawal , Ekambar Kandimalla , Dong Yu
发明人： Sudhir Agrawal , Ekambar Kandimalla , Dong Yu
IPC分类号： A61K39/00 , C07H21/02
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.

90. 发明申请

US20070105801A1 Immunostimulatory properties of oligonucleotide-based compounds comprising modified immunostimulatory dinucleotides 失效
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：US20070105801A1
公开(公告)日：2007-05-10
申请号：US11268714
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： A61K31/70 , A01N43/04
CPC分类号： A61K31/70
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, intemucleoside linkages or finctionalized 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进一步包含至少两个在其3'末端连接的寡核苷酸，核苷键或核苷酸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，具有可接近的5' 结束。

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