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公开(公告)号：US08877731B2
公开(公告)日：2014-11-04
申请号：US13236486
申请日：2011-09-19
IPC分类号： A61K31/70 , A01N43/04 , C07H19/00 , C07H19/04 , C07H19/10 , C07H19/048 , C07H19/20 , C07H19/167 , C07H19/173 , A61K31/7068 , C07H19/056 , C07H19/09 , A61K31/7056 , A61K45/06 , A61K31/7072 , A61K31/708 , A61K31/7105 , C07H19/11 , C07H19/067 , C07H19/19 , A61K31/7076 , C07H19/073
CPC分类号： C07H19/06 , A61K31/7056 , A61K31/7068 , A61K31/7072 , A61K31/7076 , A61K31/708 , A61K31/7105 , A61K45/06 , C07H19/056 , C07H19/067 , C07H19/073 , C07H19/09 , C07H19/10 , C07H19/11 , C07H19/16 , C07H19/167 , C07H19/19 , C07H19/20 , A61K2300/00
摘要： Disclosed herein are nucleosides, nucleotides and analogs thereof, pharmaceutical compositions that include one or more of nucleosides, nucleotides and analogs thereof, and methods of synthesizing the same. Also disclosed herein are methods of ameliorating and/or treating a disease and/or a condition, including an infection from a paramyxovirus and/or an orthomyxovirus, with a nucleoside, a nucleotide and an analog thereof. Examples of viral infections include a respiratory syncytial viral (RSV) and influenza infection.
摘要翻译： 本文公开了核苷，核苷酸及其类似物，包括核苷，核苷酸及其类似物中的一种或多种的药物组合物及其合成方法。 本文还公开了改善和/或治疗疾病和/或病症（包括副粘病毒和/或正粘病毒的感染）与其核苷，核苷酸和类似物的方法。 病毒感染的实例包括呼吸道合胞病毒（RSV）和流感感染。
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公开(公告)号：US20130210757A1
公开(公告)日：2013-08-15
申请号：US13838071
申请日：2013-03-15
发明人： Qiang Huang , Runcong Liu
CPC分类号： C07H19/10 , C07D405/04 , C07D473/34 , C07D473/40 , C07F9/2429 , C07F9/26 , C07F9/65586 , C07F9/65616 , C07H19/06 , C07H19/073 , C07H19/09 , C07H19/12 , C07H19/16 , C07H19/173 , C07H19/19 , C07H19/20 , C07H19/207
摘要： This application discloses phosphoramidate and phosphonoamidate prodrugs of alcohol-based therapeutic agents, such as nucleosides, nucleotides, acyclonucleosides, C-nucleosides, and C-nucleotides, and use of these prodrugs for treatment of diseases or disorders, including infectious diseases and cancers. This application also discloses a general method for enhancing bioavailability and/or liver-targeting property of alcohol drugs through converting the alcohol drugs to phosphoramidate or phosphonoamidate prodrugs, and methods of preparation of these prodrugs.
摘要翻译： 本申请公开了基于醇的治疗剂如核苷，核苷酸，无环鸟苷，C-核苷和C-核苷酸的氨基磷酸酯和膦酰胺酸酯前药，以及这些前药用于治疗疾病或病症，包括感染性疾病和癌症的用途。 本申请还公开了通过将醇类药物转化为氨基磷酸酯或膦酰胺酸酯前药来提高醇类药物的生物利用度和/或肝靶向性的一般方法，以及制备这些前药的方法。
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3.发明申请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
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。
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公开(公告)号：US07589076B2
公开(公告)日：2009-09-15
申请号：US11804165
申请日：2007-05-17
CPC分类号： C07H19/19
摘要： A2A agonists of formula (I) is provided, wherein R1, R2, R4, R5, X, Y, Z, n, p, and q are as described herein. Also provided are compositions comprising and methods of using compounds of formula (I).
摘要翻译： 提供式（I）的A2A激动剂，其中R1，R2，R4，R5，X，Y，Z，n，p和q如本文所述。 还提供了组合物和使用式（I）化合物的方法。
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公开(公告)号：US20070270373A1
公开(公告)日：2007-11-22
申请号：US11804165
申请日：2007-05-17
IPC分类号： A61K31/7076 , C07H19/19
CPC分类号： C07H19/19
摘要： A2A agonists of formula (I) is provided, wherein R1, R2, R4, R5, X, Y, Z, n, p, and q are as described herein. Also provided are compositions comprising and methods of using compounds of formula (I).
摘要翻译： 提供式（I）的2AA激动剂，其中R 1，R 2，R 4，R 4， X，Y，Z，n，p和q如本文所述。 还提供了组合物和使用式（I）化合物的方法。
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公开(公告)号：US09346848B2
公开(公告)日：2016-05-24
申请号：US14531552
申请日：2014-11-03
IPC分类号： A61K31/70 , A01N43/04 , C07H19/00 , C07H19/04 , C07H19/044 , C07H19/048 , C07H19/10 , C07H19/20 , C07H19/056 , C07H19/167 , C07H19/173 , C07H19/067 , C07H19/073 , C07H19/09 , C07H19/11 , C07H19/19 , A61K45/06 , A61K31/7056 , A61K31/7068 , A61K31/7072 , A61K31/7076 , A61K31/708 , A61K31/7105 , C07H19/06 , C07H19/16
CPC分类号： C07H19/06 , A61K31/7056 , A61K31/7068 , A61K31/7072 , A61K31/7076 , A61K31/708 , A61K31/7105 , A61K45/06 , C07H19/056 , C07H19/067 , C07H19/073 , C07H19/09 , C07H19/10 , C07H19/11 , C07H19/16 , C07H19/167 , C07H19/19 , C07H19/20 , A61K2300/00
摘要： Disclosed herein are 4′-azido-substituted nucleosides, nucleotides and analogs thereof, pharmaceutical compositions that include one or more of 4′-azido-substituted nucleosides, nucleotides and analogs thereof, and methods of synthesizing the same. Also disclosed herein are methods of ameliorating and/or treating a disease and/or a condition, including an infection from a paramyxovirus and/or an orthomyxovirus, with a 4′-azido-substituted nucleoside, a nucleotide and/or an analog thereof. Examples of viral infections include a respiratory syncytial viral (RSV) and influenza infection.
摘要翻译： 本文公开的是4'-叠氮基取代的核苷，其核苷酸及其类似物，包含4'-叠氮基取代的核苷，其核苷酸及其类似物中的一种或多种的药物组合物及其合成方法。 本文还公开了通过4'-叠氮取代的核苷，其核苷酸和/或类似物来改善和/或治疗疾病和/或病症，包括副粘病毒和/或正粘病毒的感染的方法。 病毒感染的实例包括呼吸道合胞病毒（RSV）和流感感染。
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7.发明申请公开(公告)号：US20140329768A1
公开(公告)日：2014-11-06
申请号：US14236178
申请日：2012-08-01
IPC分类号： C07H19/10
CPC分类号： A61K31/7068 , C07D213/65 , C07D213/76 , C07H19/10 , C07H19/12 , C07H19/19 , C07H19/20 , C07H19/23
摘要： Provided herein are compounds, compositions, and methods of using them to treat infections, neoplastic disease, inflammatory disease, and pain. Such compounds are nucleotides, acyclonucleotides, and ANP phosphonates conjugated with forms and/or moieties of Vitamin B6 for delivery past the cell membrane and into the cell.
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公开(公告)号：US08815830B2
公开(公告)日：2014-08-26
申请号：US14229292
申请日：2014-03-28
发明人： Carston R. Wagner
CPC分类号： C07H19/23 , C07F9/6561 , C07F9/65616 , C07H1/00 , C07H19/052 , C07H19/10 , C07H19/16 , C07H19/167 , C07H19/19 , C07H19/20 , C07H19/207 , C07K2/00 , C07K4/00
摘要： The invention provides a compound of formula (I), wherein R1-R6 and X have any of the values described, as well as pharmaceutical compositions comprising such compounds and therapeutic methods comprising the administration of such compounds.
摘要翻译： 本发明提供式（I）化合物，其中R1-R6和X具有所述的任何值，以及包含这些化合物的药物组合物和包括施用这些化合物的治疗方法。
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公开(公告)号：US20120149657A1
公开(公告)日：2012-06-14
申请号：US13320492
申请日：2010-05-12
IPC分类号： A61K31/706 , A61P35/00 , A61K31/7076 , C07H19/073 , A61K31/7068
摘要： A method of treating cancer using certain 2′-fluoro arabino nucleosides is provided. Also provided are compounds represented by the formula: (I & A) wherein R is alkyl; and pharmaceutically acceptable salts thereof; and pharmaceutical compositions containing these compounds.
摘要翻译： 提供了使用某些2'-阿拉伯核苷治疗癌症的方法。 还提供了由下式表示的化合物：（I＆A）其中R是烷基; 及其药学上可接受的盐; 和含有这些化合物的药物组合物。
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公开(公告)号：US20110091385A1
公开(公告)日：2011-04-21
申请号：US12981308
申请日：2010-12-29
IPC分类号： A61K31/7076 , C07H19/16 , C07H19/167 , A61K49/00 , A61P37/02 , A61P29/00 , A61P37/08 , A61P31/00 , A61P17/00 , A61P43/00 , A61P17/02 , A61P9/00 , A61P9/10 , A61P13/12 , A61P11/00
CPC分类号： C07H19/19
摘要： A2A agonists of formula (I) is provided, wherein R1, R2, R4, R5, X, Y, Z, n, p, and q are as described herein. Also provided are compositions comprising and methods of using compounds of formula (I).
摘要翻译： 提供式（I）的A2A激动剂，其中R1，R2，R4，R5，X，Y，Z，n，p和q如本文所述。 还提供了组合物和使用式（I）化合物的方法。
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