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1. 发明授权

US06756496B1 Nucleoside hydrogen phosphonodithioate diesters and activated phosphonodithioate analogues 失效
标题翻译：核苷氢二硫代磷酸二酯和活化的二硫代磷酸酯类似物
公开(公告)号：US06756496B1
公开(公告)日：2004-06-29
申请号：US08972998
申请日：1997-11-19
申请人： Brian C. Froehler , Chris A. Buhr
发明人： Brian C. Froehler , Chris A. Buhr
IPC分类号： C07H1904
CPC分类号： C07H19/10 , C07H19/04 , C07H19/20
摘要： Novel hydrogen-phosphonodithioate compositions are provided which are particularly useful for forming internucleotide and internucleoside linkages in oligonucleosides or oligonucleotides. The oligonucleotides and analogs thereof made by using the hydrogen-phosphonodithioate compositions may be therapeutically useful as antiviral and anticancer agents and may have other therapeutic or diagnostic uses. A method for making the hydrogen-phosphonodithioates is provided as well as a method for converting same to an activated intermediate for substitution on the phosphorus atom.
摘要翻译：提供新的氢 - 二硫代磷酸盐组合物，其特别可用于在寡核苷酸或寡核苷酸中形成核苷酸间核苷酸和核苷间键。通过使用二硫代磷酸氢盐组合物制备的寡核苷酸及其类似物可用作抗病毒和抗癌剂，并且可具有其它治疗或诊断用途。提供了制备氢二膦酸二氢盐的方法以及将其转化为活性中间体以在磷原子上进行取代的方法。

2. 发明授权

US5548076A Method of making oligonucleotides, oligonucleoside thiophosphates and oligonucleoside phosphotriesters using H-phosphonate intermediates 失效
标题翻译：使用H-膦酸酯中间体制备寡核苷酸，寡核苷酸硫代磷酸酯和寡核苷磷酸三酯的方法
公开(公告)号：US5548076A
公开(公告)日：1996-08-20
申请号：US106246
申请日：1993-08-13
申请人： Brian C. Froehler , Mark D. Matteucci
发明人： Brian C. Froehler , Mark D. Matteucci
IPC分类号： C07H1/00 , C07H21/00 , C07H21/02 , C07H21/04 , C12N15/00 , C12N15/09 , C12Q1/68
CPC分类号： C07H21/00
摘要： A method is provided for the high fidelity, rapid and economical in vitro synthesis of oligonucleotides. Nucleoside H-phosphonates are condensed in seriatim using a dehydrating agent to produce a poly (nucleoside H-phosphonate). The product is oxidized to yield the desired oligonucleotide. A novel reagent is provided for multiple nucleoside additions in single cycles.
摘要翻译：提供了用于寡核苷酸的高保真，快速和经济的体外合成的方法。使用脱水剂将核苷H-膦酸酯在seriatim中冷凝以产生聚（核苷H-膦酸酯）。将产物氧化产生所需的寡核苷酸。提供了一种新的试剂，用于单次循环中的多种核苷添加。

3. 发明授权

US06447998B1 2-Aminopyridine and 2-pyridone C-nucleosides, oligonucleotides comprising, and tests using the same oligonucleotides 失效
标题翻译： 2-氨基吡啶和2-吡啶酮C-核苷，寡核苷酸，并使用相同的寡核苷酸进行测试
公开(公告)号：US06447998B1
公开(公告)日：2002-09-10
申请号：US08906378
申请日：1997-08-05
申请人： Brian C. Froehler , Arnold J. Gutierrez , Mark D. Matteucci
发明人： Brian C. Froehler , Arnold J. Gutierrez , Mark D. Matteucci
IPC分类号： C12Q168
CPC分类号： C07D405/04 , C07H19/00 , C12Q1/6839 , C12Q2525/113
摘要： The present invention provides 2-aminopyridine and 2-pyridone C-nucleosides and oligonucleotides containing the subject nucleosides. The nucleosides are useful in the preparation of the subject oligonucleotides. The oligonucleotides are useful in oligonucleotide-based diagnosis and separation through triplex binding.
摘要翻译：本发明提供含有目标核苷的2-氨基吡啶和2-吡啶酮C-核苷和寡核苷酸。核苷可用于制备目标寡核苷酸。寡核苷酸可用于通过三重结合进行基于寡核苷酸的诊断和分离。

4. 发明授权

US06495672B1 Oligonucleotides including 2-aminopyridine and 2-pyridone C-nucleoside units 失效
标题翻译：包括2-氨基吡啶和2-吡啶酮C-核苷单位的寡核苷酸
公开(公告)号：US06495672B1
公开(公告)日：2002-12-17
申请号：US09717422
申请日：2000-11-21
申请人： Brian C. Froehler , Arnold J. Gutierrez , Mark D. Matteucci
发明人： Brian C. Froehler , Arnold J. Gutierrez , Mark D. Matteucci
IPC分类号： C07H2100
CPC分类号： C07D405/04 , C07H19/00 , C12Q1/6839 , C12Q2525/113
摘要： The present invention provides 2-aminopyridine and 2-pyridone C-nucleosides and oligonucleotides containing the subject nucleosides. The nucleosides are useful in the preparation of the subject oligonucleotides. The oligonucleotides are useful in oligonucleotide-based diagnosis and separation through triplex binding.
摘要翻译：本发明提供含有目标核苷的2-氨基吡啶和2-吡啶酮C-核苷和寡核苷酸。核苷可用于制备目标寡核苷酸。寡核苷酸可用于通过三重结合进行基于寡核苷酸的诊断和分离。

5. 发明授权

US5204455A Monomethoxytrityl protected oligonucleotides bound to a solid support 失效
标题翻译：结合固体支持物的单甲氧基三苯甲基保护的寡核苷酸
公开(公告)号：US5204455A
公开(公告)日：1993-04-20
申请号：US833242
申请日：1992-02-10
申请人： Brian C. Froehler , Kenneth M. Kent , Sylvia Wu
发明人： Brian C. Froehler , Kenneth M. Kent , Sylvia Wu
IPC分类号： B01J19/00 , C07H19/04 , C07H19/10 , C07H19/20 , C07H21/00 , C40B40/06 , C40B60/14
CPC分类号： C07H21/00 , B01J19/0046 , C07H19/04 , C07H19/10 , C07H19/20 , B01J2219/00286 , B01J2219/00497 , B01J2219/0059 , B01J2219/00596 , B01J2219/00722 , C40B40/06 , C40B60/14
摘要： The present invention describes methods for the production of oligonucleotides under conditions which exploit the desirable characteristics, such as the property of sustaining high degrees of substitution, of functionalized organic polymeric supports while avoiding the sluggish kinetics and low rates of conversion which normally plague syntheses involving such solid supports. By employing the methods and materials disclosed, functionalized support, substituted to a degree of about 250 .mu.mol/g, can be utilized at greater than 98% conversion levels for each sequential nucleotide coupling cycle, to provide unprecedented amounts of isolated oligonucleotide per gram of solid support.
摘要翻译：本发明描述了在消除官能化有机聚合物载体的所需特性（如维持高取代度的性质）的条件下生产寡核苷酸的方法，同时避免了通常的瘟疫合成涉及这样的动力学和低转化率固体支持。通过使用所公开的方法和材料，可以以每个顺序核苷酸偶联循环的大于98％的转化水平使用取代约250μmol/ g的功能化载体，以提供前所未有量的分离的寡核苷酸/克坚实的支持。

6. 发明授权

US08653248B2 2-aminopyridine and 2-pyridone C-nucleosides 失效
标题翻译： 2-氨基吡啶和2-吡啶酮C-核苷
公开(公告)号：US08653248B2
公开(公告)日：2014-02-18
申请号：US10171270
申请日：2002-06-13
申请人： Brian C. Froehler , Arnold J. Gutierrez , Mark D. Matteucci
发明人： Brian C. Froehler , Arnold J. Gutierrez , Mark D. Matteucci
IPC分类号： C07H21/02 , C07H21/04
CPC分类号： C07D405/04 , C07H19/00 , C12Q1/6839 , C12Q2525/113
摘要： The present invention provides 2-aminopyridine and 2-pyridone C-nucleosides and oligonucleotides containing the subject nucleosides. The nucleosides are useful in the preparation of the subject oligonucleotides. The oligonucleotides are useful in oligonucleotide-based diagnosis and separation through triplex binding.
摘要翻译：本发明提供含有目标核苷的2-氨基吡啶和2-吡啶酮C-核苷和寡核苷酸。核苷可用于制备目标寡核苷酸。寡核苷酸可用于通过三重结合进行基于寡核苷酸的诊断和分离。

7. 发明授权

US5264566A Method for in vitro oligonucleotide synthesis using H-phosphonates 失效
标题翻译：使用H-膦酸酯的体外寡核苷酸合成方法
公开(公告)号：US5264566A
公开(公告)日：1993-11-23
申请号：US515890
申请日：1990-04-26
申请人： Brian C. Froehler , Mark D. Matteucci
发明人： Brian C. Froehler , Mark D. Matteucci
IPC分类号： C07H1/00 , C07H21/00 , C07H21/02 , C07H21/04 , C12N15/00 , C12N15/09 , C12Q1/68
CPC分类号： C07H21/00
摘要： A method is provided for the high fidelity, rapid and economical in vitro synthesis of oligonucleotides. Nucleoside H-phosphonates are condensed in seriatim using a dehydrating agent to produce a poly (nucleoside H-phosphonate). The product is oxidized to yield the desired oligonucleotide. A novel reagent is provided for multiple nucleoside additions in single cycles.

8. 发明授权

US5565555A Nucleoside hydrogen phosphonodithioate diesters and activated phosphonodithioate analogues 失效
标题翻译：核苷氢二硫代磷酸二酯和活化的二膦酸二酯类似物
公开(公告)号：US5565555A
公开(公告)日：1996-10-15
申请号：US391338
申请日：1995-02-21
申请人： Brian C. Froehler , Chris A. Buhr
发明人： Brian C. Froehler , Chris A. Buhr
IPC分类号： C07F9/40 , C07F9/44 , C07F9/547 , C07H19/04 , C07H19/10 , C07H19/20 , C07H19/06 , C07H19/16
CPC分类号： C07H19/10 , C07H19/04 , C07H19/20
摘要： Novel hydrogen-phosphonodithioate compositions are provided which are particularly useful for forming internucleotide and internucleoside linkages in oligonucleosides or oligonucleotides, The oligonucleotides and analogs thereof made by using the hydrogen-phosphonodithioate compositions may be therapeutically useful as antiviral and anticancer agents and may have other therapeutic or diagnostic uses, A method for making the hydrogen-phosphonodithioates is provided as well as a method for converting same to an activated intermediate for substitution on the phosphorus atom.
摘要翻译：提供了新的二膦酰基二硫代磷酸酯组合物，其特别可用于在寡核苷酸或寡核苷酸中形成核苷酸间核苷键和核苷间键。通过使用二硫代磷酸二氢钠组合物制备的寡核苷酸及其类似物可用作抗病毒和抗癌剂，并且可具有其它治疗或诊断用途，提供了制备氢 - 二硫代磷酸酯的方法以及将其转化为活性中间体以在磷原子上进行取代的方法。

9. 发明授权

US5256775A Exonuclease-resistant oligonucleotides 失效
标题翻译：核酸外切酶寡核苷酸
公开(公告)号：US5256775A
公开(公告)日：1993-10-26
申请号：US555522
申请日：1990-06-05
申请人： Brian C. Froehler
发明人： Brian C. Froehler
IPC分类号： C07H21/00 , C07H21/02
CPC分类号： C07H21/00
摘要： A method is provided for making 3' and/or 5' end-capped oligonucleotides so as to render the oligonucleotide resistant to degradation by exonucleases. The exonuclease degradation resistance is provided by incorporating two or more phosphoramidate and phosphorocmonothioate and/or phosphorodithioate linkages at the 5' and/or 3' ends of the oligonucleotide, wherein the number of phosphoramidate linkages is less than a number which would interfere with hybridization to a complementary oligonucleotide strand and/or which would interfere with RNAseH activity when the oligonucleotide is hybridized to RNA.
摘要翻译：提供了一种制备3'和/或5'末端封端寡核苷酸的方法，以使寡核苷酸能够通过外切核酸酶降解。外切核酸酶降解抗性通过在寡核苷酸的5'和/或3'端掺入两个或多个氨基磷酸酯和磷酰硫氨酸和/或二硫代磷酸酯键来提供，其中氨基磷酸酯键的数目小于将干扰杂交的数目互补的寡核苷酸链和/或当寡核苷酸与RNA杂交时会干扰RNAseH活性。

10. 发明授权

US5194599A Hydrogen phosphonodithioate compositions 失效
标题翻译：氢化磷酸盐组合物
公开(公告)号：US5194599A
公开(公告)日：1993-03-16
申请号：US248517
申请日：1988-09-23
申请人： Brian C. Froehler , Chris A. Buhr
发明人： Brian C. Froehler , Chris A. Buhr
IPC分类号： C07F9/40 , C07F9/44 , C07F9/547 , C07H19/04 , C07H19/10 , C07H19/20
CPC分类号： C07H19/10 , C07H19/04 , C07H19/20
摘要： Novel hydrogen-phosphonodithioate compositions are provided which are particularly useful for forming internucleotide and internucleoside linkages in oligonucleosides or oligonucleotides. The oligonucleotides and analogs thereof made by using the hydrogen-phosphonodithioate compositions may be therapeutically useful as antiviral and anticancer agents and may have other therapeutic or diagnostic uses. A method for making the hydrogen-phosphonodithioates is provided as well as a method for converting same to an activated intermediate for substitution on the phosphorus atom.

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