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11. 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。

12. 发明授权

US06951931B2 Pyrimidine derivatives for labeled binding partners 有权
标题翻译：用于标记结合配偶体的嘧啶衍生物
公开(公告)号：US06951931B2
公开(公告)日：2005-10-04
申请号：US10294181
申请日：2002-11-14
申请人： Kuei-Ying Lin , Mark D. Matteucci
发明人： Kuei-Ying Lin , Mark D. Matteucci
IPC分类号： C07H19/06 , C07H21/00 , C12Q1/68 , C07H21/04
CPC分类号： C07H19/06 , C07H21/00 , C12Q1/6813 , C12Q2525/101 , Y02P20/55 , C12Q2563/107
摘要： Compounds having structure (1) wherein R1 is —H a protecting group, a linker or a binding partner; and R2 and R34 are as defined in the specification. The invention also provides intermediates and methods make the structure (1) compounds, as well as methods to use the compounds as labels in diagnostic assays and to enhance binding to complementary bases.
摘要翻译：具有结构（1）的化合物，其中R 1是-H是保护基，连接基或结合配偶体; R 2和R 34如说明书中所定义。本发明还提供中间体和方法制备结构（1）化合物，以及在诊断测定中使用化合物作为标记并增强与互补碱基的结合的方法。

13. 发明授权

US6028183A Pyrimidine derivatives and oligonucleotides containing same 失效
标题翻译：嘧啶衍生物和含有其的寡核苷酸
公开(公告)号：US6028183A
公开(公告)日：2000-02-22
申请号：US966392
申请日：1997-11-07
申请人： Kuei-Ying Lin , Mark D. Matteucci
发明人： Kuei-Ying Lin , Mark D. Matteucci
IPC分类号： C07H19/06 , C07H21/00 , C12Q1/68 , C07H19/00
CPC分类号： C07H19/06 , C07H21/00 , C12Q1/6813 , C12Q2525/101 , Y02P20/55
摘要： Compounds having structure (1) ##STR1## wherein R.sup.1 is --H a protecting group, a linker or a binding partner; and R.sup.2 and R.sup.34 are as defined in the specification. The invention also provides intermediates and methods make the structure (1) compounds, as well as methods to use the compounds as labels in diagnostic assays and to enhance binding to complementary bases.
摘要翻译：具有结构（1）的化合物，其中R 1为-H，保护基，连接基或结合配偶体; R2和R34如说明书中所定义。本发明还提供中间体和方法制备结构（1）化合物，以及在诊断测定中使用化合物作为标记并增强与互补碱基的结合的方法。

14. 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.

15. 发明授权

US5153319A Process for preparing polynucleotides 失效
标题翻译：制备多核苷酸的方法
公开(公告)号：US5153319A
公开(公告)日：1992-10-06
申请号：US846453
申请日：1986-03-31
申请人： Marvin H. Caruthers , Mark D. Matteucci
发明人： Marvin H. Caruthers , Mark D. Matteucci
IPC分类号： A61K47/48 , B01J19/00 , C07H21/00 , C40B40/06 , C40B60/14
CPC分类号： C07H21/00 , A61K47/48015 , B01J19/0046 , B01J2219/00286 , B01J2219/0059 , B01J2219/00596 , B01J2219/00686 , B01J2219/00698 , B01J2219/00722 , C40B40/06 , C40B60/14 , Y02P20/582
摘要： New and useful intermediate nucleotides bound to an inorganic polymer support, including the preparation thereof, and processes for the conversion to oligonucleotides which are especially useful for the synthesis of polynucleotides, particularly ribonucleic (RNA) and deoxyribonucleic (DNA) acids, are described.
摘要翻译：描述了与无机聚合物载体结合的新的和有用的中间核苷酸，包括其制备，以及转化成寡核苷酸的方法，其特别可用于合成多核苷酸，特别是核糖核酸（RNA）和脱氧核糖核酸（DNA）酸。

16. 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。

17. 发明授权

US5777153A Cationic lipids 失效
标题翻译：阳离子脂质
公开(公告)号：US5777153A
公开(公告)日：1998-07-07
申请号：US273045
申请日：1994-07-08
申请人： Kuei-Ying Lin , Jason G. Lewis , Mark D. Matteucci , Richard W. Wagner
发明人： Kuei-Ying Lin , Jason G. Lewis , Mark D. Matteucci , Richard W. Wagner
IPC分类号： A61K9/127 , A61K38/00 , C07C237/06 , C07C237/20 , C07C237/22 , C07C271/22 , C07C279/14 , C07C279/22 , C07C279/24 , C07J41/00 , C07K5/068 , C07K5/072 , C12N15/88 , C07C271/20
CPC分类号： C07K5/06095 , A61K9/1272 , C07C237/06 , C07C237/20 , C07C237/22 , C07C271/22 , C07C279/14 , C07C279/22 , C07C279/24 , C07J41/0055 , C07K5/06086 , C12N15/88 , A61K38/00
摘要： The present invention is directed to new cationic lipids and intermediates in their synthesis that are useful for transfecting nucleic acids or peptides into prokaryotic or eukaryotic cells. The lipids comprise one or two arginine, lysine or ornithine residues linked to a lipophilic moiety. The lipids form a composition when mixed with polyanions such as nucleic acids. The compositions permit efficient transfer of polyanions into cells without significant toxicity to the cells.
摘要翻译：本发明涉及其合成中的新的阳离子脂质和中间体，其可用于将核酸或肽转染到原核或真核细胞中。脂质包含与亲油部分连接的一个或两个精氨酸，赖氨酸或鸟氨酸残基。当与聚阴离子如核酸混合时，脂质形成组合物。组合物允许聚阴离子有效转移到细胞中，而对细胞没有显着的毒性。

18. 发明授权

US5502177A Pyrimidine derivatives for labeled binding partners 失效
标题翻译：用于标记结合配偶体的嘧啶衍生物
公开(公告)号：US5502177A
公开(公告)日：1996-03-26
申请号：US123505
申请日：1993-09-17
申请人： Mark D. Matteucci , Robert J. Jones , Kuei-Ying Lin
发明人： Mark D. Matteucci , Robert J. Jones , Kuei-Ying Lin
IPC分类号： C12N15/09 , A61K31/565 , A61K31/70 , A61K31/7042 , A61K31/7052 , C07D239/46 , C07D239/47 , C07D239/52 , C07D239/54 , C07D405/04 , C07D487/04 , C07D487/14 , C07D491/14 , C07D498/04 , C07D498/14 , C07F7/22 , C07F9/09 , C07H19/00 , C07H19/04 , C07H19/06 , C07H19/22 , C07H21/00 , C07H21/02 , C12P19/34 , C12Q1/68 , C07H21/04
CPC分类号： C07D239/47 , C07D239/54 , C07D405/04 , C07D487/04 , C07F7/2212 , C07H19/06 , C07H19/073 , C07H21/00 , C12Q1/6816 , C12Q1/686 , Y02P20/55
摘要： A compound having the structure: ##STR1## wherein R.sup.1 is an oligonucleotide;a is 1 and b is 0;A is C or CH;X is S, O, NH or NCH.sub.2 R.sup.6 ;Z is taken together with A to form an aryl ring structure comprising 6 ring atoms wherein the aryl ring carbon atoms are unsubstituted with other than H or at least 1 nonbridging ring carbon atom is substituted with R.sup.6 or .dbd.O;R.sup.6 is independently H, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, NO.sub.2, N(R.sup.3).sub.2, C.tbd.N or halo, or an R.sup.6 is taken together with an adjacent Z group R.sup.6 to complete a phenyl ring; andR.sup.3 is a protecting group or H; and tautomers, solvates and salts thereof.
摘要翻译：具有以下结构的化合物：其中R1是寡核苷酸; a为1，b为0; A是C或CH; X是S，O，NH或NCH 2 R 6; Z与A一起形成包含6个环原子的芳环结构，其中芳环碳原子未被取代，除了H或至少1个非桥环环碳原子被R6或= O取代; R6独立地为H，C1-C6烷基，C2-C6烯基，C2-C6炔基，NO2，N（R3）2，C 3BONDN或卤素，或R6与相邻的Z基团R6一起以完成苯基环; 且R 3为保护基或H; 和其互变异构体，溶剂化物和盐。

19. 发明授权

US5132418A Process for preparing polynucleotides 失效
标题翻译：制备多核苷酸的方法
公开(公告)号：US5132418A
公开(公告)日：1992-07-21
申请号：US601813
申请日：1984-06-18
申请人： Marvin H. Caruthers , Mark D. Matteucci
发明人： Marvin H. Caruthers , Mark D. Matteucci
IPC分类号： B01J19/00 , C07H19/04 , C07H21/00 , C07H23/00 , C40B40/06 , C40B60/14
CPC分类号： C07H21/00 , B01J19/0046 , C07H19/04 , C07H23/00 , B01J2219/00286 , B01J2219/00389 , B01J2219/005 , B01J2219/0059 , B01J2219/00596 , B01J2219/0068 , B01J2219/00686 , B01J2219/00722 , C40B40/06 , C40B60/14 , Y02P20/582
摘要： This invention is a process for the production of oligonucleotides which comprises:(a) converting an inorganic polymer into a coupling agent-polymer;(b) combining the coupling agent-polymer with a blocked nucleoside to obtain a blocked nucleoside-modified support; and(c) removing the blocking group from the blocked nucleoside-modified support to provide for the coupling of nucleotides to the nucleoside-modified support.
摘要翻译：本发明是制备寡核苷酸的方法，其包括：（a）将无机聚合物转化为偶联剂 - 聚合物; （b）将偶联剂 - 聚合物与封闭的核苷组合以获得封闭的核苷修饰的载体; 和（c）从封闭的核苷修饰的载体中除去封闭基团以提供核苷酸与核苷修饰的载体的偶联。

20. 发明授权

US4923808A Method for identifying mutants secreting high levels of heterologous proteins 失效
标题翻译：用于鉴定分泌高水平异源蛋白质的突变体的方法
公开(公告)号：US4923808A
公开(公告)日：1990-05-08
申请号：US220901
申请日：1988-07-18
申请人： Mark D. Matteucci
发明人： Mark D. Matteucci
IPC分类号： C07K14/61 , C12N9/16 , C12N15/62 , C12N15/65
CPC分类号： C07K14/61 , C12N15/62 , C12N15/65 , C12N9/16 , C07K2319/00
摘要： A method is provided for identifying mutants that leads to the enhanced expression and periplasmic secretion of heterologous preproteins from host cells. Mutants in the host cell or in the gene encoding the heterologous preprotein are identified readily by transforming the host cell with a fusion which comprises DNA encoding the heterologous preprotein and a detectable marker protein. A marker protein is chosen that only becomes active in the periplasmic or extracellular environment. Thus, desired mutants are identified by enhanced marker expression and secretion. The ability of the preprotein DNA or host cell mutants to enhance expression and secretion of the heterologous protein-enzyme fusions is found to correlate with similar enhancement of the expression and secretion of the heterologous protein alone and not as a fusion. Screening assays led to the identification of a preprotein silent mutation resulting in high-yield secretion that could not be explained under current theories and which provides a new method for obtaining high-yielding host-vector systems.
摘要翻译：提供了用于鉴定导致来自宿主细胞的异源前蛋白的增强的表达和周质分泌的突变体的方法。通过用包含编码异源前蛋白和可检测标记蛋白的DNA的融合物转化宿主细胞，容易地鉴定宿主细胞中或编码异源前蛋白的基因中的突变体。选择仅在周质或细胞外环境中变得活跃的标记蛋白。因此，通过增强的标志物表达和分泌来鉴定所需的突变体。发现原蛋白DNA或宿主细胞突变体增强异源蛋白质 - 酶融合物的表达和分泌的能力与单独的异源蛋白质的表达和分泌的类似增强相关，而不是融合。筛选测定导致鉴定导致高产量分泌的蛋白质沉默突变，这在目前的理论中无法解释，并且提供了获得高产量宿主载体系统的新方法。

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