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公开(公告)号:US06225460B1
公开(公告)日:2001-05-01
申请号:US09247497
申请日:1999-02-10
申请人: Norbert W. Bischofberger , Robert J. Jones , Murty N. Arimilli , Kuei-Ying Lin , Michael S. Louie , Lawrence R. McGee , Ernest J. Prisbe , William A. Lee , Kenneth C. Cundy
发明人: Norbert W. Bischofberger , Robert J. Jones , Murty N. Arimilli , Kuei-Ying Lin , Michael S. Louie , Lawrence R. McGee , Ernest J. Prisbe , William A. Lee , Kenneth C. Cundy
IPC分类号: C07H1904
CPC分类号: C07F9/657181 , C07F9/6512 , C07F9/65616 , C07F9/65742 , C07F9/65744 , C07F9/65785 , C07H19/10 , C07H19/20
摘要: Nucleotide analogs characterized by the presence of an amidate linked amino acid or an ester linked group which is bonded to the phosphorus atom of phosphonate nucleotide analogs are disclosed. The analogs comprise a phosphoamidate or ester bond that is hydrolyzed in vivo to yield a corresponding phosphonate nucleotide analog. Methods and intermediates for their synthesis and use are described.
摘要翻译: 公开了以与磷酸酯核苷酸类似物的磷原子结合的氨基酸连接的氨基酸或酯连接基团的存在为特征的核苷酸类似物。 类似物包含在体内水解以产生相应的膦酸酯核苷酸类似物的氨基磷酸酯或酯键。 描述了其合成和使用的方法和中间体。
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公开(公告)号:US5798340A
公开(公告)日:1998-08-25
申请号:US617849
申请日:1996-05-06
申请人: Norbert W. Bischofberger , Robert J. Jones , Murty N. Arimilli , Michael S. Louie , Ernest J. Prisbe , William A. Lee
发明人: Norbert W. Bischofberger , Robert J. Jones , Murty N. Arimilli , Michael S. Louie , Ernest J. Prisbe , William A. Lee
IPC分类号: C07F9/6512 , C07F9/6561 , C07F9/6571 , C07F9/6574 , C07F9/6578 , C07H19/10 , C07H19/20 , A61K31/70
CPC分类号: C07F9/657181 , C07F9/65121 , C07F9/65616 , C07F9/65742 , C07F9/65744 , C07F9/65785 , C07H19/10 , C07H19/20
摘要: Nucleotide analogs characterized by the presence of an amidate lirked amino acid or an ester linked group which is bonded to the phosphorus atom of phosphonate nucleotide analogs are disclosed. The analogs comprise a phosphoamidate or ester bond that is hydrolysed in vivo to yield a corresponding phosphonate nucleotide analog. Methods and intermediates for the synthesis and use are described.
摘要翻译: PCT No.PCT / US94 / 10539 Sec。 371日期:1996年5月6日 102(e)日期1996年5月6日PCT 1994年9月16日PCT公布。 公开号WO95 / 07920 日期:1995年3月23日公开了以磷酸酯核苷酸类似物的磷原子结合的氨基酸化的氨基酸或酯连接基团的存在为特征的核苷酸类似物。 类似物包含在体内水解产生相应的膦酸酯核苷酸类似物的磷酰胺化物或酯键。 描述了合成和使用的方法和中间体。
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公开(公告)号:US07439350B2
公开(公告)日:2008-10-21
申请号:US10882022
申请日:2004-06-29
申请人: Norbert W. Bischofberger , Robert J. Jones , Murty N. Arimilli , Kuei-Ying Lin , Michael S. Louie , Lawrence R. McGee , Ernest J. Prisbe , William A. Lee , Kenneth C. Cundy
发明人: Norbert W. Bischofberger , Robert J. Jones , Murty N. Arimilli , Kuei-Ying Lin , Michael S. Louie , Lawrence R. McGee , Ernest J. Prisbe , William A. Lee , Kenneth C. Cundy
IPC分类号: C07H19/04
CPC分类号: C07F9/657181 , C07F9/6512 , C07F9/65616 , C07F9/65742 , C07F9/65744 , C07F9/65785 , C07H19/10 , C07H19/20
摘要: Nucleotide analogs characterized by the presence of an amidate linked amino acid or an ester linked group which is bonded to the phosphorus atom of phosphonate nucleotide analogs are disclosed. The analogs comprise a phosphoamidate or ester bond that is hydrolyzed in vivo to yield a corresponding phosphonate nucleotide analog. Methods and intermediates for their synthesis and use are described.
摘要翻译: 公开了以与磷酸酯核苷酸类似物的磷原子结合的氨基酸连接的氨基酸或酯连接基团的存在为特征的核苷酸类似物。 类似物包含在体内水解以产生相应的膦酸酯核苷酸类似物的氨基磷酸酯或酯键。 描述了其合成和使用的方法和中间体。
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公开(公告)号:US5886179A
公开(公告)日:1999-03-23
申请号:US581147
申请日:1995-12-29
申请人: Murty N. Arimilli , Norbert W. Bischofberger , Robert J. Jones , William A. Lee , Ernest J. Prisbe
发明人: Murty N. Arimilli , Norbert W. Bischofberger , Robert J. Jones , William A. Lee , Ernest J. Prisbe
IPC分类号: C07D239/47 , A61K31/66 , A61K31/665 , A61K31/67 , A61K31/685 , A61K31/70 , A61K38/00 , A61K49/00 , A61P27/02 , A61P31/12 , A61P33/02 , A61P35/00 , C07F9/547 , C07F9/553 , C07F9/58 , C07F9/6512 , C07F9/6518 , C07F9/653 , C07F9/6533 , C07F9/6539 , C07F9/6558 , C07F9/6561 , C07F9/6571 , C07F9/6574 , C07F9/6578 , C07F9/6584 , C07H11/04 , C07H19/10 , C07H19/20 , C07J9/00 , C07K2/00 , G01N33/53 , C07D239/22 , C07F9/02 , A61K31/675
CPC分类号: C07F9/65785 , C07F9/65121 , C07F9/65616 , C07F9/657181 , C07F9/65742 , C07F9/65744 , C07H19/10 , C07H19/20
摘要: Nucleotide phosphonate esters characterized by the presence of an ester linked group which is bonded to the phosphorus atom of phosphonate nucleotide analogs are disclosed. The analogs comprise an ester bond that is hydrolyzed in vivo to yield a corresponding phosphonate nucleotide analog. Methods and intermediates for their synthesis and use are described.
摘要翻译: 公开了以与磷酸酯核苷酸类似物的磷原子结合的酯连接基团的存在为特征的核苷酸膦酸酯。 类似物包括在体内水解以产生相应的膦酸酯核苷酸类似物的酯键。 描述了其合成和使用的方法和中间体。
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公开(公告)号:US20090149648A1
公开(公告)日:2009-06-11
申请号:US12211745
申请日:2008-09-16
申请人: Norbert W. Bischofberger , Robert J. Jones , Murty N. Armilli , Kuei-Ying Lin , Michael S. Louie , Lawrence R. McGee , Ernest J. Prisbe , William A. Lee , Kenneth C. Cundy
发明人: Norbert W. Bischofberger , Robert J. Jones , Murty N. Armilli , Kuei-Ying Lin , Michael S. Louie , Lawrence R. McGee , Ernest J. Prisbe , William A. Lee , Kenneth C. Cundy
IPC分类号: C07F9/02
CPC分类号: C07F9/657181 , C07F9/6512 , C07F9/65616 , C07F9/65742 , C07F9/65744 , C07F9/65785 , C07H19/10 , C07H19/20
摘要: Nucleotide analogs characterized by the presence of an amidate linked amino acid or an ester linked group which is bonded to the phosphorus atom of phosphonate nucleotide analogs are disclosed. The analogs comprise a phosphoamidate or ester bond that is hydrolyzed in vivo to yield a corresponding phosphonate nucleotide analog. Methods and intermediates for their synthesis and use are described.
摘要翻译: 公开了以与磷酸酯核苷酸类似物的磷原子结合的氨基酸连接的氨基酸或酯连接基团的存在为特征的核苷酸类似物。 类似物包含在体内水解以产生相应的膦酸酯核苷酸类似物的氨基磷酸酯或酯键。 描述了其合成和使用的方法和中间体。
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公开(公告)号:US5717095A
公开(公告)日:1998-02-10
申请号:US774240
申请日:1996-12-27
IPC分类号: C07F9/6571 , C07H19/10 , C07H19/20 , C07F9/6574
CPC分类号: C07H19/10 , C07F9/657181 , C07H19/20
摘要: A cyclic nucleotide phosphonate ester characterized by the presence of an n-butyl salicylate ester group linked to the phosphorus atom of cHPMPC is disclosed. The analog comprises an ester bond that is hydrolyzed in vivo to yield a corresponding phosphonate nucleotide analog.
摘要翻译: 公开了一种特征在于存在与cHPMPC的磷原子连接的水杨酸正丁酯基团的环状核苷酸膦酸酯。 该类似物包括在体内水解以产生相应的膦酸酯核苷酸类似物的酯键。
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公开(公告)号:US06451340B1
公开(公告)日:2002-09-17
申请号:US09950031
申请日:2001-09-10
申请人: Murty N. Arimilli , Daphne E. Kelly , Thomas T. K. Lee , Lawrence V. Manes , John D. Munger, Jr. , Ernest J. Prisbe , Lisa M. Schultze
发明人: Murty N. Arimilli , Daphne E. Kelly , Thomas T. K. Lee , Lawrence V. Manes , John D. Munger, Jr. , Ernest J. Prisbe , Lisa M. Schultze
IPC分类号: A61K920
CPC分类号: A61K31/675 , C07F9/65616
摘要: The invention provides crystalline forms of adefovir dipivoxil and methods to prepare the crystals. The compositions and methods of the present invention have desirable properties for large scale synthesis of crystalline adefovir dipivoxil or for its formulation into therapeutic dosages. Invention compositions include an anhydrous crystal form of adefovir dipivoxil.
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公开(公告)号:US5656745A
公开(公告)日:1997-08-12
申请号:US123483
申请日:1993-09-17
申请人: Norbert Bischofberger , Robert J. Jones , Murty Arimilli , Kuei-Ying Lin , Michael Louie , Lawrence R. McGee , Ernest J. Prisbe
发明人: Norbert Bischofberger , Robert J. Jones , Murty Arimilli , Kuei-Ying Lin , Michael Louie , Lawrence R. McGee , Ernest J. Prisbe
IPC分类号: C07F9/6512 , C07F9/6561 , C07F9/6571 , C07F9/6574 , C07F9/6578 , C07H19/10 , C07H19/20 , C07H19/06 , C07H19/16 , C07D239/00 , C07D473/00
CPC分类号: C07H19/10 , C07F9/65121 , C07F9/65616 , C07F9/657181 , C07F9/65742 , C07F9/65744 , C07F9/65785 , C07H19/20
摘要: Nucleotide analogs characterized by the presence of an amidate linked amino acid or an ester linked group which is bonded to the phosphorus atom of phosphonate nucleotide analogs are disclosed. The analogs comprise a phosphoamidate or ester bond that is hydrolyzed in vivo to yield a corresponding phosphonate nucleotide analog. Methods and intermediates for their synthesis and use are described.
摘要翻译: 公开了以与磷酸酯核苷酸类似物的磷原子结合的氨基酸连接的氨基酸或酯连接基团的存在为特征的核苷酸类似物。 类似物包含在体内水解以产生相应的膦酸酯核苷酸类似物的氨基磷酸酯或酯键。 描述了其合成和使用的方法和中间体。
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公开(公告)号:US07803788B2
公开(公告)日:2010-09-28
申请号:US12110829
申请日:2008-04-28
申请人: Mark W. Becker , Harlan H. Chapman , Tomas Cihlar , Eugene J. Eisenberg , Gong-Xin He , Michael R. Kernan , William A. Lee , Ernest J. Prisbe , John C. Rohloff , Mark L. Sparacino
发明人: Mark W. Becker , Harlan H. Chapman , Tomas Cihlar , Eugene J. Eisenberg , Gong-Xin He , Michael R. Kernan , William A. Lee , Ernest J. Prisbe , John C. Rohloff , Mark L. Sparacino
IPC分类号: A61K31/675 , A61P31/12
CPC分类号: C07H19/10 , C07F9/65616 , C07H19/20 , C07H21/00 , C12Q1/18 , G01N33/5011
摘要: A novel method has led to the identification of novel mixed ester-amidates of PMPA for retroviral or hepadnaviral therapy, including compounds of structure (5a) having substituent groups as defined herein. Compositions of these novel compounds in pharmaceutically acceptable excipients and their use in therapy and prophylaxis are provided.
摘要翻译: 一种新的方法导致鉴定用于逆转录病毒或肝炎病毒治疗的PMPA的新型混合酯酰胺化物,包括具有如本文所定义的取代基的结构(5a)的化合物。 提供这些新化合物在药学上可接受的赋形剂中的组合物及其在治疗和预防中的用途。
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公开(公告)号:US20080227754A1
公开(公告)日:2008-09-18
申请号:US12110829
申请日:2008-04-28
申请人: Mark W. Becker , Harlan H. Chapman , Tomas Cihlar , Eugene J. Eisenberg , Gong-Xin He , Michael R. Kernan , William A. Lee , Ernest J. Prisbe , John C. Rohloff , Mark L. Sparacino
发明人: Mark W. Becker , Harlan H. Chapman , Tomas Cihlar , Eugene J. Eisenberg , Gong-Xin He , Michael R. Kernan , William A. Lee , Ernest J. Prisbe , John C. Rohloff , Mark L. Sparacino
IPC分类号: A61K31/675 , A61P31/12
CPC分类号: C07H19/10 , C07F9/65616 , C07H19/20 , C07H21/00 , C12Q1/18 , G01N33/5011
摘要: A novel method has led to the identification of novel mixed ester-amidates of PMPA for retroviral or hepadnaviral therapy, including compounds of structure (5a) having substituent groups as defined herein. Compositions of these novel compounds in pharmaceutically acceptable excipients and their use in therapy and prophylaxis are provided.
摘要翻译: 一种新的方法导致鉴定用于逆转录病毒或肝炎病毒治疗的PMPA的新型混合酯酰胺化物,包括具有如本文所定义的取代基的结构(5a)的化合物。 提供这些新化合物在药学上可接受的赋形剂中的组合物及其在治疗和预防中的用途。
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