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1.发明授权Process for the synthesis of 2′-O-substituted pyrimidines and oligomeric compounds therefrom 失效用于合成2'-O-取代的嘧啶及其低聚化合物的方法公开(公告)号：US06642367B2
公开(公告)日：2003-11-04
申请号：US09747009
申请日：2000-12-22
申请人： Phillip Dan Cook , Yogesh S. Sanghvi , Kelly G. Sprankle , Bruce S. Ross , Rich H. Griffey , Robert H. Springer
发明人： Phillip Dan Cook , Yogesh S. Sanghvi , Kelly G. Sprankle , Bruce S. Ross , Rich H. Griffey , Robert H. Springer
IPC分类号： C07H1900
CPC分类号： C07H19/06 , C07H21/00 , Y02P20/55 , Y02P20/582
摘要： Oligonucleotide analogs are disclosed having pyrimidine monomeric sub-units therein that are modified at the 2′ and 5′ positions. Monomeric sub-units having these modifications may be further modified at the 2′ position. Improved processes for the synthesis of 2′-O-substituted pyrimidine nucleosides are also provided. The processes feature alkylation of a 2,2′-anhydropyrimidine nucleoside or a 2S,2′-anhydropyrimidine nucleoside with a weak nucleophile in the presence of a Lewis acid.
摘要翻译： 公开了寡核苷酸类似物，其中具有在2'和5'位置被修饰的嘧啶单体亚单位。 具有这些修饰的单体子单元可以在2'位置进一步修饰。 还提供了用于合成2'-O-取代的嘧啶核苷的改进方法。 该方法的特征是在路易斯酸存在下，使用具有弱亲核试剂的2,2'-脱水嘧啶核苷或2S，2'-脱水嘧啶核苷进行烷基化。
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2.发明授权Process for the synthesis of 2′-O-substituted pyrimidines and oligomeric compounds therefrom 失效用于合成2'-O-取代的嘧啶及其低聚化合物的方法公开(公告)号：US06222025B1
公开(公告)日：2001-04-24
申请号：US08894899
申请日：1998-01-07
申请人： Phillip Dan Cook , Yogesh S. Sanghvi , Kelly G. Sprankle , Bruce S. Ross , Rich H. Griffey , Robert H. Springer
发明人： Phillip Dan Cook , Yogesh S. Sanghvi , Kelly G. Sprankle , Bruce S. Ross , Rich H. Griffey , Robert H. Springer
IPC分类号： C07H1900
CPC分类号： C07H19/06 , C07H21/00 , Y02P20/55 , Y02P20/582
摘要： Oligonucleotide analogs are disclosed having pyrimidine monomeric sub-units therein that are modified at the 2′ and 5 positions. Monomeric sub-units having these modifications may be further modified at the 2 position. Improved processes for the synthesis of 2′-O-substituted pyrimidine nucleosides are also provided. The processes feature alkylation of a 2,2′-anhydropyrimidine nucleoside or a 2S,2′-anhydropyrimidine nucleoside with a weak nucleophile in the presence of a Lewis acid.
摘要翻译： 公开了寡核苷酸类似物，其中具有在2'和5位修饰的嘧啶单体亚单位。 具有这些修饰的单体子单元可以在2位进一步修饰。 还提供了用于合成2'-O-取代的嘧啶核苷的改进方法。 该方法的特征是在路易斯酸存在下，使用具有弱亲核试剂的2,2'-脱水嘧啶核苷或2S，2'-脱水嘧啶核苷进行烷基化。
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3.发明授权Oligomeric compounds having pyrimidine nucleotide (S) with 2'and 5 substitutions 失效具有嘧啶核苷酸（S）的具有2'-5个取代基的低聚化合物
公开(公告)号：US06166197A
公开(公告)日：2000-12-26
申请号：US398901
申请日：1995-03-06
CPC分类号： C07H19/06 , C07H21/00 , Y02P20/582
摘要： Oligonucleotide analogs are disclosed having pyrimidine monomeric sub-units therein that are modified at the 2' and 5 positions. Monomeric sub-units having these modifications may be further modified at the 2 position.
摘要翻译： 公开了寡核苷酸类似物，其中具有在2'和5位修饰的嘧啶单体亚单位。 具有这些修饰的单体子单元可以在2位进一步修饰。
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公开(公告)号：US5861493A
公开(公告)日：1999-01-19
申请号：US890084
申请日：1997-07-09
IPC分类号： C07H19/067 , A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/7064 , A61K31/7068 , A61K31/7072 , A61K31/7088 , A61K31/712 , A61K48/00 , A61P31/12 , A61P31/18 , A61P35/00 , A61P37/04 , C07H19/06 , C07H19/09 , C07H19/10 , C07H21/00 , C12N15/09 , C07H19/00 , C07H21/02
CPC分类号： C07H19/06 , C07H21/00 , Y02P20/55 , Y02P20/582
摘要： Improved processes for the synthesis of 2'-O-substituted pyrimidine nucleosides are provided. The processes feature alkylation of a 2,2'-anhydropyrimidine nucleoside or a 2S,2'-anhydropyrimidine nucleoside with a weak nucleophile in the presence of a Lewis acid.
摘要翻译： 提供了用于合成2'-O-取代的嘧啶核苷的改进方法。 该方法的特征是在路易斯酸存在下，使用具有弱亲核试剂的2,2'-脱水嘧啶核苷或2S，2'-脱水嘧啶核苷进行烷基化。
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公开(公告)号：US5760202A
公开(公告)日：1998-06-02
申请号：US475467
申请日：1995-06-07
CPC分类号： C07H19/06 , C07H21/00 , Y02P20/582
摘要： Improved processes for the synthesis of 2'-O-substituted pyrimidine nucleosides are provided. The processes feature alkylation of a 2,2'-anhydropyrimidine nucleoside or a 2S,2'-anhydropyrimidine nucleoside with a weak nucleophile in the presence of a Lewis acid.
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公开(公告)号：US06750344B1
公开(公告)日：2004-06-15
申请号：US08924851
申请日：1997-09-05
IPC分类号： C07D24136
CPC分类号： C07D487/04 , C07D243/08 , C12Q1/18 , C40B40/00 , G01N33/68
摘要： The present invention provides monocyclic, bicyclic and oligomeric amine compounds with at least two sites of diversity. These compounds are formed from monocyclic scaffolds which can be cyclized to form bicyclic amine scaffolds. These can then be reacted with building blocks to form the amine compounds of the invention. This invention further provides libraries or monocyclic, bicyclic and oligomeric amine compounds. Also provided are methods for preparing monocyclic, bicyclic and oligomeric amine compounds and libraries thereof. The present invention also provides pharmaceutical compositions of the monocyclic, bicyclic and oligomeric amine compounds.
摘要翻译： 本发明提供具有至少两个多样性位点的单环，双环和低聚胺化合物。 这些化合物由可以环化形成双环胺支架的单环支架形成。 然后可将它们与结构单元反应形成本发明的胺化合物。 本发明还提供了文库或单环，双环和低聚胺化合物。 还提供了制备单环，双环和低聚胺化合物及其文库的方法。 本发明还提供单环，双环和低聚胺化合物的药物组合物。
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公开(公告)号：US08618289B2
公开(公告)日：2013-12-31
申请号：US12933402
申请日：2009-03-17
申请人： Sunny Abraham , Shripad S. Bhagwat , Brian T. Campbell , Qi Chao , Raffaella Faraoni , Mark W. Holladay , Andiliy G. Lai , Martin W. Rowbottom , Eduardo Setti , Kelly G. Sprankle
发明人： Sunny Abraham , Shripad S. Bhagwat , Brian T. Campbell , Qi Chao , Raffaella Faraoni , Mark W. Holladay , Andiliy G. Lai , Martin W. Rowbottom , Eduardo Setti , Kelly G. Sprankle
IPC分类号： C07D239/70 , A01N43/54
CPC分类号： C07D239/88 , A61K9/20 , A61K9/48 , A61K31/517 , A61K45/06 , C07D239/93 , C07D261/14 , C07D413/12
摘要： Compounds according to formula (I), compositions and methods are provided for modulating the activity of RAF kinases, including BRAF kinase and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder mediated by RAF kinases. Formula (I): or a pharmaceutically acceptable salt, solvate, clathrate of hydrate thereof, wherein X is O or S(O)t; Ra is O or S.
摘要翻译： 提供根据式（I）的化合物，组合物和方法用于调节RAF激酶（包括BRAF激酶）的活性，并用于治疗，预防或改善由RAF激酶介导的疾病或病症的一种或多种症状。 式（I）：或其药学上可接受的盐，溶剂合物，其水合物的包合物，其中X为O或S（O）t; Ra是O或S.
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公开(公告)号：US07820657B2
公开(公告)日：2010-10-26
申请号：US11724992
申请日：2007-03-16
IPC分类号： A61K31/5377 , A61K31/496 , A61K31/454 , A61K31/429 , C07D513/12 , C07D413/14 , C07D211/06
CPC分类号： A61K31/5377 , A61K31/429 , A61K31/454 , A61K31/496 , C07D513/04
摘要： Compounds, compositions and methods are provided for modulating the activity of receptor kinases and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder mediated by receptor kinases.
摘要翻译： 提供化合物，组合物和方法用于调节受体激酶的活性和用于治疗，预防或改善由受体激酶介导的疾病或病症的一种或多种症状。
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公开(公告)号：US08557810B2
公开(公告)日：2013-10-15
申请号：US13357477
申请日：2012-01-24
IPC分类号： A61K31/5377 , A61K31/496 , A61K31/454 , A61K31/429 , C07D513/12 , C07D413/14 , C07D211/06
CPC分类号： A61K31/5377 , A61K31/429 , A61K31/454 , A61K31/496 , C07D513/04
摘要： Compounds, compositions and methods are provided for modulating the activity of receptor kinases and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder mediated by receptor kinases.
摘要翻译： 提供化合物，组合物和方法用于调节受体激酶的活性和用于治疗，预防或改善受体激酶介导的疾病或病症的一种或多种症状。
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公开(公告)号：US20110118245A1
公开(公告)日：2011-05-19
申请号：US12933402
申请日：2009-03-17
申请人： Sunny Abraham , Shripad S. Bhagwat , Brian T. Campbell , Qi Chao , Raffaella Faraoni , Mark W. Holladay , Andiliy G. Lai , Martin W. Rowbottom , Eduardo Setti , Kelly G. Sprankle
发明人： Sunny Abraham , Shripad S. Bhagwat , Brian T. Campbell , Qi Chao , Raffaella Faraoni , Mark W. Holladay , Andiliy G. Lai , Martin W. Rowbottom , Eduardo Setti , Kelly G. Sprankle
IPC分类号： A61K31/517 , C07D413/12 , C07D491/056 , A61K31/519 , C07D413/14 , A61K31/5377 , C07D417/14 , A61K31/541 , C07D403/12 , C07D239/88 , C07D401/12 , A61P19/10 , A61P29/00 , A61P3/10 , A61P1/00 , A61P19/02 , A61P37/00 , A61P35/04
CPC分类号： C07D239/88 , A61K9/20 , A61K9/48 , A61K31/517 , A61K45/06 , C07D239/93 , C07D261/14 , C07D413/12
摘要： Compounds according to formula (I), compositions and methods are provided for modulating the activity of RAF kinases, including BRAF kinase and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder mediated by RAF kinases. Formula (I): or a pharmaceutically acceptable salt, solvate, clathrate of hydrate thereof, wherein X is O or S(O)t; Ra is O or S.
摘要翻译： 提供根据式（I）的化合物，组合物和方法用于调节RAF激酶（包括BRAF激酶）的活性，并用于治疗，预防或改善由RAF激酶介导的疾病或病症的一种或多种症状。 式（I）：或其药学上可接受的盐，溶剂合物，其水合物的包合物，其中X为O或S（O）t; Ra是O或S.
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