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公开(公告)号：US07381736B2
公开(公告)日：2008-06-03
申请号：US11219402
申请日：2005-09-02
申请人： Zacharia S. Cheruvallath , Colin J. Loweth , Ruth F. Nutt , Darryl Rideout , Joseph E. Semple , Jing Wang , Feiyue Wu , Shankari Mylvaganam , Hengyi Zhu , Jianzhong Sun
发明人： Zacharia S. Cheruvallath , Colin J. Loweth , Ruth F. Nutt , Darryl Rideout , Joseph E. Semple , Jing Wang , Feiyue Wu , Shankari Mylvaganam , Hengyi Zhu , Jianzhong Sun
IPC分类号： A61K31/427 , C07D277/18
CPC分类号： C07D277/38 , C07D277/42 , C07D285/135 , C07D417/12 , C07D417/14 , C07F9/6539 , C07F9/65395
摘要： Compounds and compositions are provided for modulating the activity of protein tyrosine phosphatases. In one embodiment, the compounds and compositions are thiazoles and thiadiazoles that inhibit the activity of protein tyrosine phosphatase 1B.
摘要翻译： 提供化合物和组合物用于调节蛋白酪氨酸磷酸酶的活性。 在一个实施方案中，化合物和组合物是抑制蛋白酪氨酸磷酸酶1B活性的噻唑和噻二唑。
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公开(公告)号：US5959099A
公开(公告)日：1999-09-28
申请号：US103399
申请日：1998-06-24
IPC分类号： C07C253/00 , C07C255/50 , C07H19/10 , C07H19/20 , C07H21/00 , C07H19/04
CPC分类号： C07H19/10 , C07C253/00 , C07H19/20 , C07H21/00 , Y02P20/55
摘要： A 2-N-amidoethyl protected nucleoside analog phosphoramidite of formula (1): ##STR1## is useful in the synthesis of a wide variety of oligonucleotide analogs. Coupling yields with phosphoramidite (1) in solution or solid phase oligonucleotide analog synthesis are high and the 2-N-amidoethyl protecting group can be removed easily under standard conditions.
摘要翻译： 式（1）的2-N-酰氨基保护的核苷类似物亚磷酰胺：可用于合成多种寡核苷酸类似物。 在溶液或固相寡核苷酸类似物合成中，亚磷酰胺（1）的偶联产率高，在标准条件下可以容易地除去2-N-酰氨基乙基保护基。
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公开(公告)号：US06399831B1
公开(公告)日：2002-06-04
申请号：US09451913
申请日：1999-12-01
IPC分类号： C07C32100
CPC分类号： C07H21/00 , C07C329/14
摘要： The present invention is directed to a method of synthesizing sulfurized oligonucleotide analogs by reacting an oligonucleotide analog containing a phosphorous(III) linkage with a dithiocarbonic acid diester polysulfide having the formula to produce a sulfurized oligonucleotide analog. The diester polysulfide reagent is useful in solution and solid phase oligonucleotide analog synthesis.
摘要翻译： 本发明涉及通过使含有磷（III）键的寡核苷酸类似物与具有制备硫化寡核苷酸类似物的二硫代碳酸二酯多硫化物反应来合成硫化寡核苷酸类似物的方法。 二酯多硫化物试剂可用于溶液和固相寡核苷酸类似物合成。
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公开(公告)号：US06399756B1
公开(公告)日：2002-06-04
申请号：US09349659
申请日：1999-07-08
IPC分类号： C07H2100
摘要： Synthetic processes are provided wherein oligomeric compounds are prepared having phosphodiester, phosphorothioate, phosphorodithioate, or other covalent linkages. Also provided are synthetic intermediates useful in such processes.
摘要翻译： 提供合成方法，其中制备具有磷酸二酯，硫代磷酸酯，二硫代磷酸酯或其它共价键的低聚化合物。 还提供了可用于这些方法的合成中间体。
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公开(公告)号：US5783690A
公开(公告)日：1998-07-21
申请号：US933133
申请日：1997-09-18
IPC分类号： C07C253/00 , C07C255/50 , C07H19/10 , C07H19/20 , C07H21/00 , C07H1/02 , C07F9/02 , C07F9/08
CPC分类号： C07H19/10 , C07C253/00 , C07H19/20 , C07H21/00 , Y02P20/55
摘要： A 2-N-amidoethyl protected nucleoside analog phosphoramidite of formula (1): ##STR1## is useful in the synthesis of a wide variety of oligonucleotide analogs. Coupling yields with phosphoramidite (1) in solution or solid phase oligonucleotide analog synthesis are high and the 2-N-amidoethyl protecting group can be removed easily under standard conditions.
摘要翻译： 式（1）的2-N-酰氨基保护的核苷类似亚磷酰胺：
（1）。 可用于合成多种寡核苷酸类似物。 在溶液或固相寡核苷酸类似物合成中，亚磷酰胺（1）的偶联产率高，在标准条件下可以容易地除去2-N-酰氨基乙基保护基。 -
公开(公告)号：US07723511B2
公开(公告)日：2010-05-25
申请号：US12106889
申请日：2008-04-21
IPC分类号： C07H21/00 , C07C321/00 , C07C323/00 , C07C381/00
CPC分类号： C07H21/00
摘要： Methods for the formation of sulfurized oligonucleotides are provided. The methods allow for the formation of phosphorothioate linkages in the oligonucleotides or derivatives, without the need for complex solvent mixtures and repeated washing or solvent changes. Oligonucleotides having from about 8, and up to about 50, nucleotides can be sulfurized according to the methods of the invention with higher yields than have been previously reported.
摘要翻译： 提供了形成硫化寡核苷酸的方法。 所述方法允许在寡核苷酸或衍生物中形成硫代磷酸酯键，而不需要复杂的溶剂混合物和重复的洗涤或溶剂变化。 具有约8个至多约50个核苷酸的寡核苷酸根据本发明的方法可以以比先前报道的更高的产率被硫化。
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公开(公告)号：US06114519A
公开(公告)日：2000-09-05
申请号：US950779
申请日：1997-10-15
CPC分类号： C07H21/00
摘要： Methods for the formation of sulfurized oligonucleotides are provided. The methods allow for the formation of phosphorothioate linkages in the oligonucleotides or derivatives, without the need for complex solvent mixtures and repeated washing or solvent changes. Oligonucleotides having from about 8, and up to about 50, nucleotides can be sulfurized according to the methods of the invention with higher yields than have been previously reported.
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公开(公告)号：US06677471B2
公开(公告)日：2004-01-13
申请号：US10290587
申请日：2002-11-08
IPC分类号： C07C6988
摘要： Synthetic processes are provided wherein oligomeric compounds are prepared having phosphodiester, phosphorothioate, phosphorodithioate, or other covalent linkages. Also provided are synthetic intermediates useful in such processes.
摘要翻译： 提供合成方法，其中制备具有磷酸二酯，硫代磷酸酯，二硫代磷酸酯或其它共价键的低聚化合物。 还提供了可用于这些方法的合成中间体。
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公开(公告)号：US06242591B1
公开(公告)日：2001-06-05
申请号：US09481486
申请日：2000-01-11
IPC分类号： C07H2100
CPC分类号： C07H21/00
摘要： Methods for the formation of sulfurized oligonucleotides are provided. The methods allow for the formation of phosphorothioate linkages in the oligonucleotides or derivatives, without the need for complex solvent mixtures and repeated washing or solvent changes. Oligonucleotides having from about 8, and up to about 50, nucleotides can be sulfuiized according to the methods of the invention with higher yields than have been previously reported.
摘要翻译： 提供了形成硫化寡核苷酸的方法。 所述方法允许在寡核苷酸或衍生物中形成硫代磷酸酯键，而不需要复杂的溶剂混合物和重复的洗涤或溶剂变化。 具有约8个和至多约50个核苷酸的寡核苷酸可根据本发明的方法被亚硫酸化，其产率高于先前报道的产率。
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公开(公告)号：US5902881A
公开(公告)日：1999-05-11
申请号：US811233
申请日：1997-03-03
IPC分类号： C07H21/04 , C07C329/14 , C07H21/00 , C07H21/02
CPC分类号： C07H21/00 , C07C329/14
摘要： The present invention is directed to a method of synthesizing sulfurized oligonucleotide analogs by reacting an oligonucleotide analog containing a phosphorous(III) linkage with a dithiocarbonic acid diester polysulfide having the formula ##STR1## to produce a sulfurized oligonucleotide analog. The diester polysulfide reagent is useful in solution and solid phase oligonucleotide analog synthesis.
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