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公开(公告)号：US07511125B2
公开(公告)日：2009-03-31
申请号：US10921734
申请日：2004-08-19
申请人： Kuei-Ying Lin , Mark D. Matteucci
发明人： Kuei-Ying Lin , Mark D. Matteucci
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。
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公开(公告)号：USRE39324E1
公开(公告)日：2006-10-03
申请号：US10080074
申请日：2002-02-21
申请人： Kuei-Ying Lin , Mark D. Matteucci
发明人： Kuei-Ying Lin , Mark D. Matteucci
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。
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公开(公告)号：US5705693A
公开(公告)日：1998-01-06
申请号：US499699
申请日：1995-07-07
申请人： Randolph B. DePrince , Kevin L. Facchine , George S. Lewis , Jason G. Lewis , Kuei-Ying Lin , Mark D. Matteucci , Robert A. Mook, Jr. , Richard W. Wagner
发明人： Randolph B. DePrince , Kevin L. Facchine , George S. Lewis , Jason G. Lewis , Kuei-Ying Lin , Mark D. Matteucci , Robert A. Mook, Jr. , 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
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 substituted arginine, lysine or ornithine residues, or derivatives thereof, linked to a lipophilic moiety. The lipids form a complex when mixed with polyanions such as nucleic acids or peptides. The complexes permit efficient transfer of polyanions into cells, usually 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取代的精氨酸，赖氨酸或鸟氨酸残基或其衍生物。 当与聚阴离子例如核酸或肽混合时，脂质形成复合物。 复合物允许聚阴离子有效转移到细胞中，通常对细胞没有显着的毒性。
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公开(公告)号：US5646269A
公开(公告)日：1997-07-08
申请号：US234452
申请日：1994-04-28
申请人： Mark D. Matteucci , Jiancun Zhang
发明人： Mark D. Matteucci , Jiancun Zhang
摘要： The present invention is directed to improved methods to synthesize oligonucleotide analogs having an acetal linkage, such as a 3',5'-formacetal (3' --O--CH.sub.2 --O-- 5'), 3',5'-thioformacetal (3' --S--CH.sub.2 --O-- 5') or an analogous 2',5' linkage between adjacent nucleoside analog residues. Compositions comprising 5', 3' and 2' phosphinate nucleoside analogs useful in the methods are also provided.
摘要翻译： 本发明涉及合成具有缩醛键的寡核苷酸类似物的改进方法，例如3'，5'-甲缩醛（3'-O-CH 2 -O-5'），3'，5'-硫代缩甲醛（3 '-S-CH2-O-5'）或相邻核苷类似物残基之间的类似的2'，5'键。 还提供了包含用于该方法的5'，3'和2“次膦酸核苷类似物的组合物。
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5.发明授权Binding compentent oligomers containing unsaturated 3',5' and 2',5' linkages 失效含有不饱和3'，5'和2'，5'键的结合性低聚物
公开(公告)号：US5434257A
公开(公告)日：1995-07-18
申请号：US142785
申请日：1993-10-26
申请人： Mark D. Matteucci , Xiaodong Cao
发明人： Mark D. Matteucci , Xiaodong Cao
IPC分类号： C07H19/06 , C07H21/00 , C12N15/113 , C12Q1/68 , C07H19/00
CPC分类号： C07H21/00 , C07H19/06 , C12N15/113 , C12Q1/68 , C12N2310/319
摘要： Oligonucleotide analogs having one or more substitute linkages of the formula 2'/3'--S--CH.sub.2 --CH.dbd.5' or 2'/3'--O--CH.sub.2 --CH.dbd.5' between adjacent nucleomonomers are disclosed. The substitute linkage replace the usual phosphodiester linkage found in unmodified nucleic acids. The oligonucleotide analogs are easy to synthesize, stable in vivo, resistant to endogenous nucleases and are able to hybridize to target nucleic acid sequences in a sequence specific manner.
摘要翻译： 公开了具有相邻核单体之间的式2'/ 3'-S-CH2-CH = 5'或2'/ 3'-O-CH2-CH = 5'的一个或多个取代键的寡核苷酸类似物。 替代连接取代未修饰核酸中常见的磷酸二酯连接。 寡核苷酸类似物易于合成，体内稳定，对内源性核酸酶具有抗性，并且能够以序列特异性方式与靶核酸序列杂交。
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公开(公告)号：US4959463A
公开(公告)日：1990-09-25
申请号：US910048
申请日：1986-09-19
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 produce 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）。 产物被氧化以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。
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7.发明授权2-Aminopyridine and 2-pyridone C-nucleosides, oligonucleotides comprising, and tests using the same oligonucleotides 失效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
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。
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公开(公告)号：US5777153A
公开(公告)日：1998-07-07
申请号：US273045
申请日：1994-07-08
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。
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公开(公告)号：US5502177A
公开(公告)日：1996-03-26
申请号：US123505
申请日：1993-09-17
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。
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公开(公告)号：US5132418A
公开(公告)日：1992-07-21
申请号：US601813
申请日：1984-06-18
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。
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