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1. 发明申请

US20120149888A1 SYNTHESIS OF ARA-2'-O-METHYL-NUCLEOSIDES, CORRESPONDING PHOSPHORAMIDITES AND OLIGONUCLEOTIDES INCORPORATING NOVEL MODIFICATIONS FOR BIOLOGICAL APPLICATION IN THERAPEUCTICS, DIAGNOSTICS, G- TETRAD FORMING OLIGONUCLEOTIDES AND APTAMERS 审中-公开
标题翻译：合成ARA-2'-O-甲基核苷酸，相应的磷酸酰胺和寡核苷酸，用于生物应用于治疗，诊断，G-TETRAD形成寡核苷酸和APTAMERS的新的修饰
公开(公告)号：US20120149888A1
公开(公告)日：2012-06-14
申请号：US13138465
申请日：2010-02-23
申请人： Suresh C. Srivastava , Divya Pandey , Naveen P. Srivastava , Alok Srivastava
发明人： Suresh C. Srivastava , Divya Pandey , Naveen P. Srivastava , Alok Srivastava
IPC分类号： C07H21/00 , C07H19/09 , C07H19/19
CPC分类号： C07H19/19 , A61K31/7052 , C07H19/09 , C07H21/00
摘要： The present invention relates to synthesis, purification and methods to obtain high purity novel 2′-arabino-O-methyl nucleosides and the corresponding phosphoramidites of various arabinonucleoside bases and introduction of such units into defined sequence synthetic DNA and RNA. Various synthetic oligonucleotides, such as HIV integrase inhibitor 14-mer and thrombin binding oligonucleotide, thrombin-1, bearing ara-2′-omethyl modification have been synthesized. It is anticipated the oligonucleotides incorporating these monomers will exhibit biological activities related to antisense approach approach, design of better SiRNA's, diagnostic agents. Similarly, it is anticipated that oligonucleotides incorporating such novel nucleosides will be useful to develop therapeutic candidates designing stable G-quadruplexes and Aptamers for oligonucleotide structure, folding topology, evaluation of biochemical properties and design and develop as therapeutic agents. It is further anticipated that the nucleosides, phosphates and triphosphates of this invention could develop as therapeutic agents.
摘要翻译：本发明涉及获得高纯度的新型2'-阿拉伯糖-O-甲基核苷和各种阿拉伯核苷碱基的相应亚磷酰胺的合成，纯化和方法，并将这些单元引入定义的顺序合成的DNA和RNA。已经合成了各种合成寡核苷酸，如HIV整合酶抑制剂14聚体和凝血酶结合寡核苷酸，凝血酶-1，带有ara-2'-甲基修饰。预期结合这些单体的寡核苷酸将显示与反义方法方法相关的生物活性，更好的SiRNA的设计，诊断剂。类似地，预期掺入这种新型核苷的寡核苷酸可用于开发用于寡核苷酸结构，折叠拓扑结构，生物化学性质的评估和设计和开发作为治疗剂的稳定的G-四链体和Aptamers的治疗候选物。进一步预期本发明的核苷，磷酸酯和三磷酸可以作为治疗剂发展。

2. 发明授权

US08309707B2 RNA synthesis-phosphoramidites for synthetic RNA in the reverse direction, and application in convenient introduction of ligands, chromophores and modifications of synthetic RNA at the 3′-end 有权
标题翻译： RNA合成 - 亚磷酰胺的合成RNA在相反方向，适用于方便引入配体，发色团和修饰的合成RNA在3'末端
公开(公告)号：US08309707B2
公开(公告)日：2012-11-13
申请号：US12584625
申请日：2009-09-08
申请人： Suresh C. Srivastava , Divya Pandey , Satya P Bajpai , Naveen P Srivastava
发明人： Suresh C. Srivastava , Divya Pandey , Satya P Bajpai , Naveen P Srivastava
IPC分类号： C07H21/00 , C07H19/20 , C07H19/10 , C07H19/048
CPC分类号： C12N15/113 , C07H1/00 , C07H19/067 , C07H19/167 , C07H21/02 , C12N2310/14
摘要： Novel technology for RNA synthesis in the reverse direction, involving a new class of products, 3′-DMT-5’-CE ribonucleoside phosphoramidites and 3′-DMT-5’-succinyl ribonucleoside solid supports, with per step coupling efficiency surpassing 99% in the RNA synthesis. This leads to high purity RNA. Examples of a large number of 20-21 mers and a few examples of long chain oligonucleotides are demonstrated. The data indicates dramatic improvement in coupling efficiency per step during oligonucleotide synthesis using the reverse RNA monomers (5′→′ direction) as compared to 3′-CE ribonucleoside phosphoramidites used in the conventional method of RNA synthesis (3′→5′ direction). The new process requires shorter coupling cycle time, approx. 4 minutes as compared to approx. 10 minutes using conventional RNA synthesis method (3′→5′ direction). Furthermore, almost complete absence of M+1 impurities in the reverse RNA synthesis methodology were observed, even when the last phosphoramidite was a macromolecule. The process resulted in very high purity 3′-modified oligonucleotides after HPLC purification. As a result of high purity of synthesized RNA and clean introduction of various 3′-end modified RNA requiring long chain ligands, chromophores, fluorophores and quenchers, this method of RNA synthesis is expected to be a very useful method of choice for therapeutic grade RNA. The novel phosphoramidites of this invention, Rev-A-n-bz, Rev-C-n-bz, Rev-C-n-ac, Rev-G-n-ac and Rev-rU show HPLC purity greater than 98% and 31P NMR purity greater than 99.5%.
摘要翻译： RNA反向新技术涉及新产品，3'-DMT-5-CE核糖核苷亚磷酰胺和3'-DMT-5-琥珀酰基核糖核苷固体支持物，每步耦合效率超过99％ RNA合成。这导致高纯度RNA。证明了大量20-21个多个实例和长链寡核苷酸的几个实例。与用于RNA合成的常规方法（3'→5'方向）中使用的3'-CE核糖核苷亚磷酰胺相比，使用反向RNA单体（5'→'方向）的寡核苷酸合成期间，每个步骤的偶联效率显着提高，。新工艺需要较短的耦合周期时间。 4分钟相比大约使用常规RNA合成方法（3'→5'方向）10分钟。此外，即使当最后一个亚磷酰胺是大分子时，也观察到反向RNA合成方法中几乎完全不存在M + 1杂质。该方法在HPLC纯化后产生非常高纯度的3'-修饰的寡核苷酸。由于高纯度的合成RNA和清洁引入需要长链配体，发色团，荧光团和猝灭剂的各种3'-末端修饰的RNA，这种RNA合成方法有望成为治疗级RNA的一种非常有用的方法。本发明的新型亚磷酰胺Rev-A-n-bz，Rev-C-n-bz，Rev-C-n-ac，Rev-G-n-ac和Rev-rU显示HPLC纯度大于98％，31P NMR纯度大于99.5％。

3. 发明申请

US20100324278A1 RNA synthesis-phosphoramidites for synthetic RNA in the reverse direction, and application in convenient introduction of ligands, chromophores and modifications of synthetic RNA at the 3'-end 有权
标题翻译： RNA合成 - 亚磷酰胺的合成RNA在相反方向，适用于方便引入配体，发色团和修饰的合成RNA在3'末端
公开(公告)号：US20100324278A1
公开(公告)日：2010-12-23
申请号：US12584625
申请日：2009-09-08
申请人： Suresh C. Srivastava , Divya Pandey , Satya P. Bajpai , Naveen P. Srivastava
发明人： Suresh C. Srivastava , Divya Pandey , Satya P. Bajpai , Naveen P. Srivastava
IPC分类号： C07H21/02 , C07H19/067 , C07H19/048
CPC分类号： C12N15/113 , C07H1/00 , C07H19/067 , C07H19/167 , C07H21/02 , C12N2310/14
摘要： The present invention relates to novel phosphoramidites, A-n-bz, C-n-bz, C-n-ac, G-n-ac and U are produced with an HPLC purity of greater than 98% and 31P NMR purity greater than 99%. A novel process of reverse 5′→3′ directed synthesis of RNA oligomers has been developed and disclosed. Using that method demonstrated high quality RNA synthesis with coupling efficiency approaching 99%.
摘要翻译：本发明涉及新型亚磷酰胺A-n-bz，C-n-bz，C-n-ac，G-n-ac和U，其HPLC纯度大于98％，31P NMR纯度大于99％。已经开发并公开了反向5'→3'反向RNA合成的新方法。使用该方法证明了高效率的RNA合成，偶联效率接近99％。

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