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公开(公告)号：US20080139802A1
公开(公告)日：2008-06-12
申请号：US11973748
申请日：2007-10-10
申请人： Steven D. Axt , Byoung-Kwon Chun , Qingwu Jin , Suguna Rachakonda , Bruce Ross , Keshab Sarma , Justin Vitale , Jiang Zhu
发明人： Steven D. Axt , Byoung-Kwon Chun , Qingwu Jin , Suguna Rachakonda , Bruce Ross , Keshab Sarma , Justin Vitale , Jiang Zhu
IPC分类号： C07H19/06 , C07H13/04 , C07D307/20
摘要： The present process provides an improved method for converting 2′-deoxy-2′-fluoro-2′-methyl-D-ribonolactones derivatives to 3-fluoro-3-methyl-2-chlorofuran compounds which are useful for the synthesis of nucleosides and improved processes for the synthesis of the D-ribonolactone compounds.
摘要翻译： 本发明提供了将2'-脱氧-2'-氟-2'-甲基-D-核糖内酯衍生物转化成可用于合成核苷的3-氟-3-甲基-2-氯呋喃化合物的改进方法， 用于合成D-核糖内酯化合物的改进方法。
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公开(公告)号：US20100056770A1
公开(公告)日：2010-03-04
申请号：US12444608
申请日：2007-10-05
申请人： Steven D. Axt , Keshab Sarma , Justin Vitale , Jiang Zhu , Bruce Ross , Suguna Rachakonda , Qingwu Jin , Byoung-kwon Chun
发明人： Steven D. Axt , Keshab Sarma , Justin Vitale , Jiang Zhu , Bruce Ross , Suguna Rachakonda , Qingwu Jin , Byoung-kwon Chun
IPC分类号： C07H19/067
摘要： The present process provides an improved method for the preparation of 4-amino-1-((2R,3R,4R,5R)-3-fluoro-4-hydroxy-5-hydrox-ymethyl-3-methyl-tetrahydro-furan-2-yl)-1H-pyrimidin-2-one of the formula (IV) which is a potent inhibitor of Hepatitis C Virus (HCV) NS5B polymerase.
摘要翻译： 本发明方法提供了制备4-氨基-1 - （（2R，3R，4R，5R）-3-氟-4-羟基-5-羟基 - 甲基-3-甲基 - 四氢 - 呋喃-2-基） 吡啶-2-基）-1H-嘧啶-2-酮，其是丙型肝炎病毒（HCV）NS5B聚合酶的有效抑制剂的式（IV）。
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公开(公告)号：US08912321B2
公开(公告)日：2014-12-16
申请号：US12444608
申请日：2007-10-05
申请人： Steven D. Axt , Keshab Sarma , Justin Vitale , Jiang Zhu , Bruce Ross , Suguna Rachakonda , Quingwu Jin , Byoung-Kwon Chun
发明人： Steven D. Axt , Keshab Sarma , Justin Vitale , Jiang Zhu , Bruce Ross , Suguna Rachakonda , Quingwu Jin , Byoung-Kwon Chun
摘要： The present process provides an improved method for the preparation of 4-amino-1-((2R,3R,4R,5R)-3-fluoro-4-hydroxy-5-hydroxymethyl-3-methyl-tetrahydrofuran-2-yl)-1H-pyrimidin-2-one of the formula (IV) which is a potent inhibitor of Hepatitis C Virus (HCV) NS5B polymerase.
摘要翻译： 本方法提供了制备4-氨基-1 - （（2R，3R，4R，5R）-3-氟-4-羟基-5-羟甲基-3-甲基 - 四氢呋喃-2-基） （IV）的1H-嘧啶-2-酮，其是丙型肝炎病毒（HCV）NS5B聚合酶的有效抑制剂。
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公开(公告)号：US08716263B2
公开(公告)日：2014-05-06
申请号：US12645821
申请日：2009-12-23
申请人： Byoung-Kwon Chun , Jinfa Du , Suguna Rachakonda , Bruce Ross , Michael Joseph Sofia , Ganapati Reddy Pamulapati , Wonsuk Chang , Hai-Ren Zhang , Dhanapalan Nagarathnam
发明人： Byoung-Kwon Chun , Jinfa Du , Suguna Rachakonda , Bruce Ross , Michael Joseph Sofia , Ganapati Reddy Pamulapati , Wonsuk Chang , Hai-Ren Zhang , Dhanapalan Nagarathnam
CPC分类号： C07H19/20 , C07H1/00 , C07H5/02 , C07H15/04 , C07H19/167 , C07H19/213 , Y02P20/55
摘要： A process for preparing phosphoramidate prodrugs or cyclic phosphate prodrugs of nucleoside derivatives, which is a compound, its stereoisomers, salts (acid or basic addition salts), hydrates, solvates, or crystalline forms thereof.
摘要翻译： 制备核苷衍生物的氨基磷酸酯前药或环磷酸酯前药的方法，其为化合物，其立体异构体，盐（酸或碱加成盐），水合物，溶剂合物或其结晶形式。
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公开(公告)号：US20120316327A1
公开(公告)日：2012-12-13
申请号：US13491437
申请日：2012-06-07
申请人： Byoung-Kwon Chun , Jinfa Du , Suguna Rachakonda , Bruce Ross , Michael Joseph Sofia , Ganapati Reddy Pamulapati , Wonsuk Chang , Hai-Ren Zhang , Dhanapalan Nagarathnam
发明人： Byoung-Kwon Chun , Jinfa Du , Suguna Rachakonda , Bruce Ross , Michael Joseph Sofia , Ganapati Reddy Pamulapati , Wonsuk Chang , Hai-Ren Zhang , Dhanapalan Nagarathnam
IPC分类号： C07H1/00 , C07H19/20 , C07H19/213 , C07H15/207
CPC分类号： C07H19/20 , C07H1/00 , C07H5/02 , C07H15/04 , C07H19/167 , C07H19/213 , Y02P20/55
摘要： A process for preparing phosphoramidate prodrugs or cyclic phosphate prodrugs of nucleoside derivatives, which is a compound, its stereoisomers, salts (acid or basic addition salts), hydrates, solvates, or crystalline forms thereof.
摘要翻译： 制备核苷衍生物的氨基磷酸酯前药或环磷酸酯前药的方法，其为化合物，其立体异构体，盐（酸或碱加成盐），水合物，溶剂合物或其结晶形式。
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公开(公告)号：US09045520B2
公开(公告)日：2015-06-02
申请号：US13491437
申请日：2012-06-07
申请人： Byoung-Kwon Chun , Jinfa Du , Suguna Rachakonda , Bruce Ross , Michael Joseph Sofia , Ganapati Reddy Pamulapati , Wonsuk Chang , Hai-Ren Zhang , Dhanpalan Nagarathnam
发明人： Byoung-Kwon Chun , Jinfa Du , Suguna Rachakonda , Bruce Ross , Michael Joseph Sofia , Ganapati Reddy Pamulapati , Wonsuk Chang , Hai-Ren Zhang , Dhanpalan Nagarathnam
IPC分类号： C07H1/00 , C07H5/02 , C07H15/04 , C07H19/20 , C07H19/167 , C07H19/213
CPC分类号： C07H19/20 , C07H1/00 , C07H5/02 , C07H15/04 , C07H19/167 , C07H19/213 , Y02P20/55
摘要： A process for preparing phosphoramidate prodrugs or cyclic phosphate prodrugs of nucleoside derivatives, which is a compound, its stereoisomers, salts (acid or basic addition salts), hydrates, solvates, or crystalline forms thereof.
摘要翻译： 制备核苷衍生物的氨基磷酸酯前药或环磷酸酯前药的方法，其为化合物，其立体异构体，盐（酸或碱加成盐），水合物，溶剂合物或其结晶形式。
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公开(公告)号：US08642756B2
公开(公告)日：2014-02-04
申请号：US12783680
申请日：2010-05-20
申请人： Bruce Ross , Michael Joseph Sofia , Ganapati Reddy Pamulapati , Suguna Rachakonda , Hai-Ren Zhang , Byoung-Kwon Chun , Peiyuan Wang
发明人： Bruce Ross , Michael Joseph Sofia , Ganapati Reddy Pamulapati , Suguna Rachakonda , Hai-Ren Zhang , Byoung-Kwon Chun , Peiyuan Wang
IPC分类号： A61K31/716 , C07H19/10
CPC分类号： C07H19/10 , A61K31/7072 , A61K31/716 , A61K45/00 , C07F9/24 , C07F9/242 , C07F9/65586 , C07H1/00 , C07H17/02 , Y02A50/463 , Y02P20/55
摘要： Disclosed herein are nucleoside phosphoramidates and their use as agents for treating viral diseases. These compounds are inhibitors of RNA-dependent 5 RNA viral replication and are useful as inhibitors of HCV NS5B polymerase, as inhibitors of HCV replication and for treatment of hepatitis C infection in mammals.
摘要翻译： 本文公开了核苷氨基磷酸酯及其作为治疗病毒性疾病的药剂的用途。 这些化合物是RNA依赖性5 RNA病毒复制的抑制剂，可用作HCV NS5B聚合酶的抑制剂，作为HCV复制的抑制剂和用于治疗哺乳动物的丙型肝炎感染。
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8.发明授权Preparation of 2′-fluoro-2′-alkyl-substituted or other optionally substituted ribofuranosyl pyrimidines and purines and their derivatives 有权2'-氟-2'-烷基取代或其它任选取代的呋喃核糖嘧啶嘧啶和嘌呤及其衍生物的制备公开(公告)号：US08492539B2
公开(公告)日：2013-07-23
申请号：US11225425
申请日：2005-09-13
申请人： Byoung-Kwon Chun , Peiyuan Wang , Jinfa Du , Suguna Rachakonda
发明人： Byoung-Kwon Chun , Peiyuan Wang , Jinfa Du , Suguna Rachakonda
IPC分类号： C07H1/00 , C07H3/00 , C07H19/00 , C07H21/00 , C07D307/00
CPC分类号： C07D411/04 , A61K31/7072 , C07D307/20 , C07D307/33 , C07D317/30 , C07D405/04 , C07D407/04 , C07H15/203 , C07H19/06
摘要： The present invention provides (i) processes for preparing a 2′-deoxy-2′-fluoro-2′-methyl-D-ribonolactone derivatives, (ii) conversion of intermediate lactones to nucleosides with potent anti-HCV activity, and their analogues, and (iii) methods to prepare the anti-HCV nucleosides containing the 2′-deoxy-2′-fluoro-2′-C-methyl-β-D-ribofuranosyl nucleosides from a preformed, preferably naturally-occurring, nucleoside.
摘要翻译： 本发明提供（i）制备2'-脱氧-2'-氟-2'-甲基-D-核糖内酯衍生物的方法，（ii）具有有效抗HCV活性的中间体内酯转化为核苷及其类似物 ，和（iii）从预先形成的，优选天然存在的核苷制备含有2'-脱氧-2'-氟-2'-C-methyl-β-D-呋喃核糖核苷的抗HCV核苷的方法。
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公开(公告)号：US20110251152A1
公开(公告)日：2011-10-13
申请号：US13076552
申请日：2011-03-31
申请人： Bruce S. Ross , Michael Joseph Sofia , Ganapati Reddy Pamulapati , Suguna Rachakonda , Hai-Ren Zhang , Byoung-Kwon Chun , Peiyuan Wang
发明人： Bruce S. Ross , Michael Joseph Sofia , Ganapati Reddy Pamulapati , Suguna Rachakonda , Hai-Ren Zhang , Byoung-Kwon Chun , Peiyuan Wang
IPC分类号： A61K31/7072 , A61P31/14 , C07H19/10
CPC分类号： A61K31/7072 , A61K9/20 , A61K45/06 , C07B2200/13 , C07F9/2479 , C07H19/06 , C07H19/10 , C07H23/00
摘要： Disclosed herein are nucleoside phosphoramidates and their use as agents for treating viral diseases. These compounds are inhibitors of RNA-dependent RNA viral replication and are useful as inhibitors of HCV NS5B polymerase, as inhibitors of HCV replication and for treatment of hepatitis C infection in mammals.
摘要翻译： 本文公开了核苷氨基磷酸酯及其作为治疗病毒性疾病的药剂的用途。 这些化合物是RNA依赖性RNA病毒复制的抑制剂，可用作HCV NS5B聚合酶的抑制剂，作为HCV复制的抑制剂和用于治疗哺乳动物的丙型肝炎感染。
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公开(公告)号：US08618076B2
公开(公告)日：2013-12-31
申请号：US13076552
申请日：2011-03-31
申请人： Bruce S. Ross , Michael Joseph Sofia , Ganapati Reddy Pamulapati , Suguna Rachakonda , Hai-Ren Zhang , Byoung-Kwon Chun , Peiyuan Wang
发明人： Bruce S. Ross , Michael Joseph Sofia , Ganapati Reddy Pamulapati , Suguna Rachakonda , Hai-Ren Zhang , Byoung-Kwon Chun , Peiyuan Wang
CPC分类号： A61K31/7072 , A61K9/20 , A61K45/06 , C07B2200/13 , C07F9/2479 , C07H19/06 , C07H19/10 , C07H23/00
摘要： Disclosed herein are nucleoside phosphoramidates and their use as agents for treating viral diseases. These compounds are inhibitors of RNA-dependent RNA viral replication and are useful as inhibitors of HCV NS5B polymerase, as inhibitors of HCV replication and for treatment of hepatitis C infection in mammals.
摘要翻译： 本文公开了核苷氨基磷酸酯及其作为治疗病毒性疾病的药剂的用途。 这些化合物是RNA依赖性RNA病毒复制的抑制剂，可用作HCV NS5B聚合酶的抑制剂，作为HCV复制的抑制剂和用于治疗哺乳动物的丙型肝炎感染。
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