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1. 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。

2. 发明授权

US06962783B2 Enhanced triple-helix and double-helix formation with oligomers containing modified pyrimidines 失效
标题翻译：增强的三螺旋和双螺旋形成与含有修饰嘧啶的低聚物
公开(公告)号：US06962783B2
公开(公告)日：2005-11-08
申请号：US10024818
申请日：2001-12-18
申请人： Brian Froehler , Rick Wagner , Mark Matteucci , Robert J. Jones , Arnold J. Gutierrez , Jeff Pudlo
发明人： Brian Froehler , Rick Wagner , Mark Matteucci , Robert J. Jones , Arnold J. Gutierrez , Jeff Pudlo
IPC分类号： C07H19/06 , C07H19/10 , C07H19/20 , C07H21/00 , C12Q1/68 , H04L12/24 , C07H21/02 , C12P19/34
CPC分类号： C07H19/06 , C07H19/10 , C07H19/20 , C07H21/00 , C12Q1/6839 , C12Q2525/101
摘要： Novel oligomers are disclosed which have enhanced ability with respect to forming duplexes or triplexes compared with oligomers containing only conventional bases. The oligomers contain the bases 5-(1-propynyl)uracil, 5-(1-propynyl)cytosine or related analogs. The oligomers of the invention are capable of (i) forming triplexes with various target sequences such as virus or oncogene sequences by coupling into the major groove of a target DNA duplex at physiological pH or (ii) forming duplexes by binding to single-stranded DNA or to RNA encoded by target genes. The oligomers of the invention can be incorporated into pharmaceutically acceptable carriers and can be constructed to have any desired sequence, provided the sequence normally includes one or more bases that is replaced with the analogs of the invention. Compositions of the invention can be used as pharmaceutical agents to treat various diseases such as those caused by viruses and can be used for diagnostic purposes in order to detect viruses or disease conditions.
摘要翻译：公开了与仅含有常规碱的低聚物相比，具有增强形成双链体或三链体的能力的新型低聚物。低聚物含有5-（1-丙炔基）尿嘧啶，5-（1-丙炔基）胞嘧啶或相关类似物的碱基。本发明的寡聚体能够（i）通过在生理pH下偶联到目标DNA双链体的主要沟槽中或（ii）通过结合单链DNA形成双链体，形成具有各种靶序列的病毒或致癌基因序列的三链体或由靶基因编码的RNA。本发明的寡聚体可以并入药学上可接受的载体中，并且可以被构建成具有任何所需的序列，条件是序列通常包括用本发明的类似物代替的一个或多个碱基。本发明的组合物可以用作药剂来治疗由病毒引起的各种疾病，并且可以用于诊断目的以检测病毒或疾病状况。

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

US5830653A Methods of using oligomers containing modified pyrimidines 失效
标题翻译：使用含有修饰嘧啶的寡聚物的方法
公开(公告)号：US5830653A
公开(公告)日：1998-11-03
申请号：US473481
申请日：1995-06-07
申请人： Brian Froehler , Rick Wagner , Mark Matteucci , Robert J. Jones , Arnold J. Gutierrez , Jeff Pudlo
发明人： Brian Froehler , Rick Wagner , Mark Matteucci , Robert J. Jones , Arnold J. Gutierrez , Jeff Pudlo
IPC分类号： C07H19/06 , C07H19/10 , C07H19/20 , C07H21/00 , C12Q1/68 , C12N5/06 , C12N5/10
CPC分类号： C07H19/06 , C07H19/10 , C07H19/20 , C07H21/00 , C12Q1/6839
摘要： Novel oligomers are disclosed which have enhanced ability with respect to forming duplexes or triplexes compared with oligomers containing only conventional bases. The oligomers contain the bases 5-(1-propynyl)uracil, 5-(1-propynyl)cytosine or related analogs. The oligomers of the invention are capable of (i) forming triplexes with various target sequences such as virus or oncogene sequences by coupling into the major groove of a target DNA duplex at physiological pH or (ii) forming duplexes by binding to single-stranded DNA or to RNA encoded by target genes. The oligomers of the invention can be incorporated into pharmaceutically acceptable carriers and can be constructed to have any desired sequence, provided the sequence normally includes one or more bases that is replaced with the analogs of the invention. compositions of the invention can be used as pharmaceutical agents to treat various diseases such as those caused by viruses and can be used for diagnostic purposes in order to detect viruses or disease conditions.
摘要翻译：公开了与仅含有常规碱的低聚物相比，具有增强形成双链体或三链体的能力的新型低聚物。低聚物含有5-（1-丙炔基）尿嘧啶，5-（1-丙炔基）胞嘧啶或相关类似物的碱基。本发明的寡聚体能够（i）通过在生理pH下偶联到目标DNA双链体的主要沟槽中或（ii）通过结合单链DNA形成双链体，形成具有各种靶序列的病毒或致癌基因序列的三链体或由靶基因编码的RNA。本发明的寡聚体可以并入药学上可接受的载体中，并且可以被构建成具有任何所需的序列，条件是序列通常包括用本发明的类似物代替的一个或多个碱基。本发明的组合物可以用作药剂来治疗由病毒引起的各种疾病，并且可以用于诊断目的以检测病毒或疾病状况。

5. 发明授权

US07057027B2 Enhanced triple-helix and double-helix formation with oligomers containing modified pyrimidines 失效
公开(公告)号：US07057027B2
公开(公告)日：2006-06-06
申请号：US10730643
申请日：2003-12-08
申请人： Brian Froehler , Rick Wagner , Mark Mattencci , Robert J. Jones , Arnold J. Gutierrez , Jeff Pudlo
发明人： Brian Froehler , Rick Wagner , Mark Mattencci , Robert J. Jones , Arnold J. Gutierrez , Jeff Pudlo
IPC分类号： C07H21/00 , C07H21/02 , C07H21/04
CPC分类号： C07H19/06 , C07H19/10 , C07H19/20 , C07H21/00 , C12Q1/6839 , C12Q2525/101
摘要： Novel oligomers are disclosed which have enhanced ability with respect to forming duplexes or triplexes compared with oligomers containing only conventional bases. The oligomers contain the bases 5-(1-propynyl)uracil, 5-(1-propynyl)cytosine or related analogs. The oligomers of the invention are capable of (i) forming triplexes with various target sequences such as virus or oncogene sequences by coupling into the major groove of a target DNA duplex at physiological pH or (ii) forming duplexes by binding to single-stranded DNA or to RNA encoded by target genes. The oligomers of the invention can be incorporated into pharmaceutically acceptable carriers and can be constructed to have any desired sequence, provided the sequence normally includes one or more bases that is replaced with the analogs of the invention. Compositions of the invention can be used as pharmaceutical agents to treat various diseases such as those caused by viruses and can be used for diagnostic purposes in order to detect viruses or disease conditions.

6. 发明授权

US06875593B2 Enhanced triple-helix and double-helix formation with oligomers containing modified pyrimidines 失效
公开(公告)号：US06875593B2
公开(公告)日：2005-04-05
申请号：US10294203
申请日：2002-11-14
申请人： Brian Froehler , Rick Wagner , Mark Matteucci , Robert J. Jones , Arnold J. Gutierrez , Jeff Pudlo
发明人： Brian Froehler , Rick Wagner , Mark Matteucci , Robert J. Jones , Arnold J. Gutierrez , Jeff Pudlo
IPC分类号： C07H19/06 , C07H19/10 , C07H19/20 , C07H21/00 , C12Q1/68 , H04L12/24 , C12P19/34 , C07H21/02
CPC分类号： C07H19/06 , C07H19/10 , C07H19/20 , C07H21/00 , C12Q1/6839 , C12Q2525/101
摘要： Novel oligomers are disclosed which have enhanced ability with respect to forming duplexes or triplexes compared with oligomers containing only conventional bases. The oligomers contain the bases 5-(1-propynyl)uracil, 5-(1-propynyl)cytosine or related analogs. The oligomers of the invention are capable of (i) forming triplexes with various target sequences such as virus or oncogene sequences by coupling into the major groove of a target DNA duplex at physiological pH or (ii) forming duplexes by binding to single-stranded DNA or to RNA encoded by target genes. The oligomers of the invention can be incorporated into pharmaceutically acceptable carriers and can be constructed to have any desired sequence, provided the sequence normally includes one or more bases that is replaced with the analogs of the invention. Compositions of the invention can be used as pharmaceutical agents to treat various diseases such as those caused by viruses and can be used for diagnostic purposes in order to detect viruses or disease conditions.

7. 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。

8. 发明授权

US06380368B1 Enhanced triple-helix and double-helix formation with oligomers containing modified pyrimidines 失效
标题翻译：增强的三螺旋和双螺旋形成与含有修饰嘧啶的低聚物
公开(公告)号：US06380368B1
公开(公告)日：2002-04-30
申请号：US08599738
申请日：1996-02-12
申请人： Brian Froehler , Rick Wagner , Mark Mattencci , Robert J. Jones , Arnold J. Gutierrez , Jeff Pudlo
发明人： Brian Froehler , Rick Wagner , Mark Mattencci , Robert J. Jones , Arnold J. Gutierrez , Jeff Pudlo
IPC分类号： C07H2102
CPC分类号： C07H19/06 , C07H19/10 , C07H19/20 , C07H21/00 , C12Q1/6839 , C12Q2525/101
摘要： Novel oligomers are disclosed which have enhanced ability with respect to forming duplexes or triplexes compared with oligomers containing only conventional bases. The oligomers contain the bases 5-(1-propynyl)uracil, 5-(1-propynyl)cytosine or related analogs. The oligomers of the invention are capable of (i) forming triplexes with various target sequences such as virus or oncogene sequences by coupling into the major groove of a target DNA duplex at physiological pH or (ii) forming duplexes by binding to single-stranded DNA or to RNA encoded by target genes. The oligomers of the invention can be incorporated into pharmaceutically acceptable carriers and can be constructed to have any desired sequence, provided the sequence normally includes one or more bases that is replaced with the analogs of the invention. Compositions of the invention can be used as pharmaceutical agents to treat various diseases such as those caused by viruses and can be used for diagnostic purposes in order to detect viruses or disease conditions.
摘要翻译：公开了与仅含有常规碱的低聚物相比，具有增强形成双链体或三链体的能力的新型低聚物。低聚物含有5-（1-丙炔基）尿嘧啶，5-（1-丙炔基）胞嘧啶或相关类似物的碱基。本发明的寡聚体能够（i）通过在生理pH下偶联到目标DNA双链体的主要沟槽中或（ii）通过结合单链DNA形成双链体，形成具有各种靶序列的病毒或致癌基因序列的三链体或由靶基因编码的RNA。本发明的寡聚体可以并入药学上可接受的载体中，并且可以被构建成具有任何所需的序列，条件是序列通常包括用本发明的类似物代替的一个或多个碱基。本发明的组合物可以用作药剂来治疗由病毒引起的各种疾病，并且可以用于诊断目的以检测病毒或疾病状况。

9. 发明授权

US5645985A Enhanced triple-helix and double-helix formation with oligomers containing modified pyrimidines 失效
标题翻译：增强的三螺旋和双螺旋形成与含有修饰嘧啶的低聚物
公开(公告)号：US5645985A
公开(公告)日：1997-07-08
申请号：US976103
申请日：1992-11-25
申请人： Brian Froehler , Rick Wagner , Mark Matteucci , Robert J. Jones , Arnold J. Gutierrez , Jeff Pudlo
发明人： Brian Froehler , Rick Wagner , Mark Matteucci , Robert J. Jones , Arnold J. Gutierrez , Jeff Pudlo
IPC分类号： A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/7064 , A61K31/7068 , A61K31/7072 , A61K48/00 , C07H19/00 , C07H19/06 , C07H19/067 , C07H19/073 , C07H19/10 , C07H19/20 , C07H21/00 , C07H21/02 , C07H21/04 , C12N15/09 , C12Q1/68
CPC分类号： C07H19/06 , C07H19/10 , C07H19/20 , C07H21/00 , C12Q1/6839 , Y02P20/55
摘要： Novel oligomers are disclosed which have enhanced ability with respect to forming duplexes or triplexes compared with oligomers containing only conventional bases. The oligomers contain the bases 5-(1-propynyl)uracil, 5-(1-propynyl)cytosine or related analogs. The oligomers of the invention are capable of (i) forming triplexes with various target sequences such as virus or oncogene sequences by coupling into the major groove of a target DNA duplex at physiological pH or (ii) forming duplexes by binding to single-stranded DNA or to RNA encoded by target genes. The oligomers of the invention can be constructed to have any desired sequence, provided the sequence normally includes one or more bases that is replaced with the analogs of the invention. Compositions of the invention can be used used for diagnostic purposes in order to detect viruses or disease conditions.
摘要翻译：公开了与仅含有常规碱的低聚物相比，具有增强形成双链体或三链体的能力的新型低聚物。低聚物含有5-（1-丙炔基）尿嘧啶，5-（1-丙炔基）胞嘧啶或相关类似物的碱基。本发明的寡聚体能够（i）通过在生理pH下偶联到目标DNA双链体的主要沟槽中或（ii）通过结合单链DNA形成双链体，形成具有各种靶序列的病毒或致癌基因序列的三链体或由靶基因编码的RNA。本发明的低聚物可被构建成具有任何所需的序列，条件是序列通常包括用本发明的类似物代替的一个或多个碱基。本发明的组合物可以用于诊断目的，以便检测病毒或疾病状况。

10. 发明授权

US06465649B1 Methods for the dealkylation of phosphonate esters 有权
标题翻译：膦酸酯的脱烷基化方法
公开(公告)号：US06465649B1
公开(公告)日：2002-10-15
申请号：US09641547
申请日：2000-08-17
申请人： Arnold J. Gutierrez , Ernest J. Prisbe , John C. Rohloff
发明人： Arnold J. Gutierrez , Ernest J. Prisbe , John C. Rohloff
IPC分类号： C07F902
CPC分类号： C07F9/38 , C07F9/409 , C07F9/65616
摘要： Disclosed are methods for the dealkylation of phosphonate esters by use of trimethylchlorosilane as the dealkylating agent. In particular, this invention is directed to the discovery that high yields for the dealkylation of phosphonate esters can be achieved within relatively short reaction times by the use of trimethylchlorosilane provided that the dealkylation procedure occurs in a sealed vessel containing a compatible solvent.
摘要翻译：公开了通过使用三甲基氯硅烷作为脱烷基化剂使膦酸酯脱烷基化的方法。特别地，本发明涉及如下发现：通过使用三甲基氯硅烷可以在相对较短的反应时间内实现膦酸酯的脱烷基化的高产率，条件是脱烷基化程序发生在含有相容溶剂的密封容器中。

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