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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：US5952375A
公开(公告)日：1999-09-14
申请号：US606624
申请日：1996-02-26
IPC分类号： C07D277/20 , A61K31/13 , A61K31/185 , A61K31/19 , A61K31/195 , A61K31/196 , A61K31/215 , A61K31/33 , A61K31/336 , A61K31/35 , A61K31/351 , A61K31/357 , A61K31/395 , A61K31/396 , A61K31/40 , A61K31/4015 , A61K31/425 , A61K31/426 , A61K31/44 , A61K31/443 , A61K31/4433 , A61K31/445 , A61K31/66 , A61K31/675 , A61P31/12 , A61P31/16 , C07B53/00 , C07C69/757 , C07C233/52 , C07C233/63 , C07C247/14 , C07C279/16 , C07C311/07 , C07C311/14 , C07C317/46 , C07C321/22 , C07C323/63 , C07D203/08 , C07D203/26 , C07D207/27 , C07D207/40 , C07D211/68 , C07D213/74 , C07D257/04 , C07D277/40 , C07D303/40 , C07D309/28 , C07D311/14 , C07D317/72 , C07D335/00 , C07D405/04 , C07D409/04 , C12N9/99 , C12Q1/34 , A61K31/28
CPC分类号： C07D309/28 , Y02P20/55
摘要： Novel compounds are described. The compounds generally comprise an acidic group, a basic group, a substituted amino or N-acyl and a group having an optionally hydroxylated alkane moiety. Pharmaceutical compositions comprising the inhibitors of the invention are also described. Methods of inhibiting neuraminidase in samples suspected of containing neuraminidase are also described. Antigenic materials, polymers, antibodies, conjugates of the compounds of the invention with labels, and assay methods for detecting neuraminidase activity are also described.
摘要翻译： 描述了新的化合物。 化合物通常包含酸性基团，碱性基团，取代的氨基或N-酰基和具有任选羟基化的烷烃部分的基团。 还描述了包含本发明抑制剂的药物组合物。 还描述了怀疑含有神经氨酸酶的样品中抑制神经氨酸酶的方法。 还描述了抗原物质，聚合物，抗体，本发明化合物与标记物的缀合物，以及用于检测神经氨酸酶活性的测定方法。
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公开(公告)号：US5705524A
公开(公告)日：1998-01-06
申请号：US473876
申请日：1995-06-07
IPC分类号： C07D337/04 , C07D495/04 , A61K31/38
CPC分类号： C07D495/04 , C07D337/04
摘要： Tri- and tetra substituted thiepane and compositions having use as immunogens, therapeutics, diagnostics and for other industrial purposes are disclosed. The compositions inhibit proteolytic activity of viral enzymes and are useful for the inhibition of such enzymes as well as in assays for the detection of such enzymes. Embodiments in which antigenic polypeptides are bonded to the compositions are useful in raising antibodies against the thiepane haptens or the polypeptide. Labeled thiepanes of this invention are useful as diagnostic reagents.
摘要翻译： 公开了三 - 和四取代的硫代环烷和作为免疫原，治疗，诊断和其他工业目的使用的组合物。 组合物抑制病毒酶的蛋白水解活性，并且可用于抑制这些酶以及用于检测这些酶的测定。 其中抗原性多肽与组合物结合的实施方案可用于产生针对硫替平半抗原或多肽的抗体。 本发明的标记的thiepane可用作诊断试剂。
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公开(公告)号：US5672697A
公开(公告)日：1997-09-30
申请号：US652978
申请日：1991-02-08
IPC分类号： A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/7064 , A61K31/7068 , A61K31/7072 , A61K31/7076 , A61K31/708 , A61K31/7088 , A61P31/12 , A61P33/00 , A61P35/00 , C07H19/04 , C07H19/06 , C07H19/10 , C07H19/16 , C07H19/20 , C07H21/00 , C07H21/04 , C07H19/073 , C07H19/173
摘要： Novel oligonucleotides analogs and nucleoside analogs as well as methods for their synthesis are described. The oligonucleotides are useful in diagnostic and therapeutic applications. The oligonucleotides are stable to nuclease degradation.
摘要翻译： 描述了新的寡核苷酸类似物和核苷类似物及其合成方法。 寡核苷酸可用于诊断和治疗应用。 寡核苷酸对核酸酶降解稳定。
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公开(公告)号：US6034118A
公开(公告)日：2000-03-07
申请号：US552429
申请日：1995-11-03
申请人： Norbert W. Bischofberger , Choung U. Kim , Steven H. Krawczyk , Lawrence R. McGee , Michael J. Postich , Wenjin Yang
发明人： Norbert W. Bischofberger , Choung U. Kim , Steven H. Krawczyk , Lawrence R. McGee , Michael J. Postich , Wenjin Yang
IPC分类号： C07D337/04 , C07D495/04 , A61K31/38 , C07D337/00
CPC分类号： C07D337/04 , C07D495/04
摘要： Tri- and tetra substituted thiepane compositions having use as immunogens, therapeutics, diagnostics and for other industrial purposes are disclosed. The compositions inhibit proteolytic activity of viral enzymes and are useful for the inhibition of such enzymes as well as in assays for the detection of such enzymes. Embodiments in which antigenic polypeptides are bonded to the compositions are useful in raising antibodies against the thiepane haptens or the polypeptide. Labeled thiepanes of this invention are useful as diagnostic reagents.
摘要翻译： 公开了用作免疫原，治疗学，诊断和用于其它工业目的的三取代和四取代的硫代吡喃组合物。 组合物抑制病毒酶的蛋白水解活性，并且可用于抑制这些酶以及用于检测这些酶的测定。 其中抗原性多肽与组合物结合的实施方案可用于产生针对硫替平半抗原或多肽的抗体。 本发明的标记的thiepane可用作诊断试剂。
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公开(公告)号：US5763483A
公开(公告)日：1998-06-09
申请号：US774345
申请日：1996-12-27
IPC分类号： C07C233/52 , A61K31/21
CPC分类号： C07C233/52 , C07C2101/16
摘要： Novel carbocyclic compounds are described. The compounds generally comprise an acidic group, a basic group, a substituted amino or N-acyl and a group having an optionally hydroxylated alkane moiety. Pharmaceutical compositions comprising the inhibitors of the invention are also described. Methods of inhibiting neuraminidase in samples suspected of containing neuraminidase are also described. Antigenic materials, polymers, antibodies, conjugates of the compounds of the invention with labels, and assay methods for detecting neuraminidase activity are also described.
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