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1. 发明授权

US06831166B2 Derivatized oligonucleotides having improved uptake and other properties 失效
标题翻译：具有改善摄取和其他性质的衍生寡核苷酸
公开(公告)号：US06831166B2
公开(公告)日：2004-12-14
申请号：US10073718
申请日：2002-02-11
申请人： Muthiah Manoharan , Phillip Dan Cook , Clarence Frank Bennett
发明人： Muthiah Manoharan , Phillip Dan Cook , Clarence Frank Bennett
IPC分类号： C07H1900
CPC分类号： C07H21/04 , C07J1/00 , C12N2710/20022 , H04J2203/0042 , H04J2203/006
摘要： Linked nucleosides having at least one functionalized nucleoside that bears a substituent such as a steroid molecule, a reporter molecule, a non-aromatic lipophilic molecule, a reporter enzyme, a peptide, a protein, a water soluble vitamin, a lipid soluble vitamin, an RNA cleaving complex, a metal chelator, a porphyrin, an alkylator, a pyrene, a hybrid photonuclease/intercalator, or an aryl azide photo-crosslinking agent exhibit increased cellular uptake and other properties. The substituent can be attached at the 2′-position of the functionalized nucleoside via a linking group. If at least a portion of the remaining liked nucleosides are 2′-deoxy-2′-fluoro, 2′-O-methoxy, 2′-O-ethoxy, 2′-O-propoxy, 2′-O-aminoalkoxy or 2′-O-allyloxy nucleosides, the substituent can be attached via a linking group at any of the 3′ or the 5′ positions of the nucleoside or on the heterocyclic base of the nucleoside or on the inter-nucleotide linkage linking the nucleoside to an adjacent nucleoside.
摘要翻译：具有至少一个具有取代基的官能化核苷的连接核苷，例如类固醇分子，报道分子，非芳族亲脂性分子，报道酶，肽，蛋白质，水溶性维生素，脂溶性维生素， RNA切割复合物，金属螯合剂，卟啉，烷基化剂，芘，混合光子核酸酶/嵌入剂或芳基叠氮化物光交联剂表现出增加的细胞摄取和其它性质。取代基可以通过连接基团连接在官能化核苷的2'-位上。如果至少一部分剩余的核苷类为2'-脱氧-2'-氟，则2'-O-甲氧基，2'-O-乙氧基，2'-O-丙氧基，2'-O-氨基烷氧基或2 '-O-烯丙氧基核苷，取代基可以通过连接基团在核苷的3'或5'位置或核苷的杂环碱基上或连接核苷与核苷酸之间的核苷酸间连接相邻核苷。

2. 发明授权

US06797815B2 Xylofuranosly-containing nucleoside phosphoramidites and polynucleotides 失效
标题翻译：含有木糖呋喃糖的核苷亚磷酰胺和多核苷酸
公开(公告)号：US06797815B2
公开(公告)日：2004-09-28
申请号：US10277263
申请日：2002-10-22
申请人： Jasenka Matulic-Adamic , Leonid Beigelman
发明人： Jasenka Matulic-Adamic , Leonid Beigelman
IPC分类号： C07H1900
CPC分类号： C12N15/1135 , A61K38/00 , C12N15/1137 , C12N15/1138 , C12N2310/111 , C12N2310/12 , C12N2310/121 , C12N2310/122 , C12N2310/315 , C12N2310/317 , C12N2310/321 , C12N2310/322 , C12N2310/332 , C12Y204/02001 , C12Y207/01037 , C12N2310/3521
摘要： Novel xylo nucleoside or xylo nucleotide analogs, polynucleotides comprising xylo nucleotide substitution, processes for their synthesis and incorporation into polynucleotides.
摘要翻译：新的木糖核苷或木糖核苷酸类似物，包含木糖苷取代的多核苷酸，其合成方法和并入多核苷酸。

3. 发明授权

US06768000B1 Multi-fluorescent hairpin energy transfer oligonucleotides 有权
标题翻译：多荧光发夹能量转移寡核苷酸
公开(公告)号：US06768000B1
公开(公告)日：2004-07-27
申请号：US09701394
申请日：2001-01-17
申请人： Glenn Nardone
发明人： Glenn Nardone
IPC分类号： C07H1900
CPC分类号： C07H21/04 , C07H19/00 , C12Q1/6818 , C12Q2525/301
摘要： An oligonucleotide, labeled with a molecular energy transfer trio and containing two sequences capable of hairpin formation, is used in the detection of two targets by irradiation with a single wavelength of light. One of the two sequences contains an energy donor and a first energy acceptor, and the other sequence contains a second energy acceptor. The donor is in close proximity to the second acceptor only if the hairpin is formed, while the donor is always in close proximity to first acceptor. A sample is assayed, using this oligonucleotide in conjunction with another oligonucleotide which contains the donor fluorophore and the quencher, arranged as described above, but which lacks the acceptor fluorophore. The present oligonucleotide and the other oligonucleotide are specific to first and second targets, respectively. If a sample contains the first and second targets, then hairpin formation is prevented after each oligonucleotide is incorporated into a target amplification product or hybridized to a target. Subsequent irradiation of the sample with the single wavelength of light which excites the donor fluorophore, but not the acceptor fluorophore, causes two distinctive signals to be generated. The first signal is emitted by the second fluorophore of the present oligonucleotide, while the second signal is emitted by the first fluorophore of the other oligonucleotide. Thus, the first and second targets are detected when one observes the first and second signals, respectively.
摘要翻译：用分子能量转移三重标记并含有能够产生发夹形成的两个序列的寡核苷酸被用于通过用单一波长的光照射来检测两个靶。两个序列中的一个包含能量供体和第一能量受体，另一个序列包含第二能量受体。只有当发夹形成时，供体才靠近第二受体，而供体总是紧邻第一受体。测定样品，使用该寡核苷酸与包含供体荧光团和猝灭剂的另一种寡核苷酸结合，如上所述排列但缺少受体荧光团。本发明的寡核苷酸和其它寡核苷酸分别对于第一和第二靶标是特异性的。如果样品含有第一和第二靶标，则在将每个寡核苷酸并入目标扩增产物中或与靶标杂交后，可以防止发夹形成。用激发供体荧光团而不是受体荧光团的单波长光照射样品导致产生两个不同的信号。第一信号由本寡核苷酸的第二荧光团发射，而第二信号由另一寡核苷酸的第一荧光团发射。因此，当分别观察第一和第二信号时，检测第一和第二目标。

4. 发明授权

US06680378B1 Nucleic acid marker ladder for estimating mass 失效
标题翻译：用于估计质量的核酸标记梯
公开(公告)号：US06680378B1
公开(公告)日：2004-01-20
申请号：US09666890
申请日：2000-09-20
申请人： James L. Hartley
发明人： James L. Hartley
IPC分类号： C07H1900
CPC分类号： C12N15/10 , C12Q1/68 , C12Q1/686
摘要： The invention relates to a nucleic acid marker ladder which is a restriction endonuclease digest, wherein a nucleic acid restriction endonuclease digest is a collection of nucleic acid fragments resulting from complete digestion of one or more nucleic acids by one or more restriction endonucleases; the restriction endonuclease digest contains at least 3 fragments; and the size of the fragments in base pairs is a multiple of an integer, wherein the integer is 10 or more.
摘要翻译：本发明涉及作为限制性内切核酸酶消化物的核酸标记梯，其中核酸限制性内切核酸酶消化物是由一种或多种限制性内切核酸酶完全消化一种或多种核酸而产生的核酸片段的集合; 限制性内切酶消化物包含至少3个片段; 并且碱基对中的片段的大小是整数的倍数，其中整数为10以上。

5. 发明授权

US06555677B2 Phase transfer catalyzed glycosidation of an indolocarbazole 失效
公开(公告)号：US06555677B2
公开(公告)日：2003-04-29
申请号：US10002061
申请日：2001-10-22
申请人： Daniel E. Petrillo , Steven A. Weissman , Shouichi Hiraga , Nobuya Satake , Kai Rossen
发明人： Daniel E. Petrillo , Steven A. Weissman , Shouichi Hiraga , Nobuya Satake , Kai Rossen
IPC分类号： C07H1900
CPC分类号： C07H19/23 , C07H17/02
摘要： The present invention relates to a novel glycosidation process to make intermediates useful in the preparation of indolopyrrolocarbazole derivatives which inhibit the growth of tumor cells and are therefore useful in the treatment of cancer in mammals, and the like.

6. 发明授权

US06441161B1 Urea nucleosides as therapeutic and diagnostic agents 有权
标题翻译：尿素核苷作为治疗和诊断剂
公开(公告)号：US06441161B1
公开(公告)日：2002-08-27
申请号：US09707253
申请日：2000-11-06
申请人： Gary P. Kirschenheuter , Bruce Eaton
发明人： Gary P. Kirschenheuter , Bruce Eaton
IPC分类号： C07H1900
CPC分类号： C07H11/02 , C07H19/06 , C07H19/16
摘要： Modified nucleosides and methods of making and using the nucleosides are disclosed. The compounds can be prepared by reacting nucleoside starting materials that contain a suitable leaving group at one or more of the carbon atoms in the purine or pyrimidine ring, with a vinylstannane, carbon monoxide, and a palladium catalyst to provide 1-ene-3-one intermediates. These intermediates are then reacted with suitably functionalized primary or secondary amines via a Michael reaction. When the intermediate is a 5-position modified pyrimidine ring, and the amine contains a second hydrogen, it can do a second Michael reaction with the ene-one or the ene-imine in the pyrimidine ring. Appropriate modification of the amine reactant can yield products with various bioactivities. The nucleosides can be used therapeutically as anti-cancer, anti-bacterial or anti-viral drugs. The nucleosides can also be used for diagnostic applications, for example, by incorporating a radiolabel or fluorescent label into the molecule. The nucleosides can be used to prepare oligonucleotides for use in various applications, either alone or in combination with other modified nucleosides and/or naturally occurring nucleosides.
摘要翻译：公开了修饰的核苷和制备和使用核苷的方法。可以通过使含有嘌呤或嘧啶环中的一个或多个碳原子上的合适的离去基团的核苷起始原料与乙烯基苯烷，一氧化碳和钯催化剂反应来制备化合物，以提供1-烯-3-醇，一个中间体。然后通过迈克尔反应将这些中间体与适当官能化的伯胺或仲胺反应。当中间体是5-位修饰的嘧啶环，并且胺含有第二个氢时，它可以与嘧啶环中的一个或烯 - 亚胺进行第二个迈克尔反应。胺反应物的适当改性可产生具有各种生物活性的产物。核苷可以用作治疗性的抗癌，抗细菌或抗病毒药物。核苷也可用于诊断应用，例如通过在分子中掺入放射性标记或荧光标记。核苷可用于制备用于各种应用的寡核苷酸，单独使用或与其它修饰的核苷和/或天然存在的核苷组合。

7. 发明授权

US06348583B1 Poly(ether-thioether), poly(ether-sulfoxide) and poly(ether-sulfone) nucleic acids 有权
标题翻译：聚（醚 - 硫醚），聚（醚 - 亚砜）和聚（醚 - 砜）核酸
公开(公告)号：US06348583B1
公开(公告)日：2002-02-19
申请号：US09411862
申请日：1999-10-04
申请人： David Segev
发明人： David Segev
IPC分类号： C07H1900
CPC分类号： C07H21/00 , C07H19/10 , C07H19/20
摘要： A compound comprising a poly(ether-thioether), poly(ether-sulfoxide) or poly(ether-sulfone) backbone bearing a plurality of ligands that are individually bound to chiral carbon atoms located within the backbone, at least one of the ligands including a moiety such as a naturally occurring nucleobase, a nucleobase binding group or a DNA interchelator; a process of synthesizing the compound, monomers to be used in this process and their synthesis process and processes for using the compound in biochemistry and medicine.
摘要翻译：包含分别与位于骨架内的手性碳原子结合的多个配体的聚（醚 - 硫醚），聚（醚 - 亚砜）或聚（醚 - 砜）主链的化合物，至少一种配体包括诸如天然存在的核碱基，核碱基结合基团或DNA交换器的部分; 合成化合物的方法，该方法中使用的单体及其在生物化学和医药中使用该化合物的合成方法和方法。

8. 发明授权

US06313286B1 Nucleoside analogues 失效
标题翻译：核苷类似物
公开(公告)号：US06313286B1
公开(公告)日：2001-11-06
申请号：US09117494
申请日：1999-02-05
申请人： Daniel Brown , Alan Hamilton , David Loakes , Adrian Simmonds , Clifford Smith
发明人： Daniel Brown , Alan Hamilton , David Loakes , Adrian Simmonds , Clifford Smith
IPC分类号： C07H1900
CPC分类号： C07H19/06 , C07H21/00 , C12Q1/686 , C12Q1/6869 , G01N33/5308
摘要： Nucleoside analogues containing the degenerate base analogue P and derivatives thereof are provided with reporter moieties preferably comprising signal moieties. The nucleoside analogues are useful for labeling DNA or RNA or for incorporating in oligonucleotides.
摘要翻译：含有简并碱基类似物P及其衍生物的核苷类似物提供有优选包含信号部分的报道部分。核苷类似物可用于标记DNA或RNA或用于掺入寡核苷酸。

9. 发明授权

US06239265B1 Oligonucleotides having chiral phosphorus linkages 失效
公开(公告)号：US06239265B1
公开(公告)日：2001-05-29
申请号：US09208533
申请日：1998-12-09
申请人： Phillip Dan Cook
发明人： Phillip Dan Cook
IPC分类号： C07H1900
CPC分类号： A61K48/00 , A61K38/00 , C07H21/02 , C07H21/04 , C07J43/003 , C07K14/005 , C12N9/0069 , C12N15/113 , C12N15/1137 , C12N2310/3125 , C12N2310/315 , C12N2310/32 , C12N2310/321 , C12N2310/322 , C12N2310/33 , C12N2310/333 , C12N2310/336 , C12N2310/3511 , C12N2310/3521 , C12N2310/3523 , C12N2310/3527 , C12N2310/3531 , C12N2310/3533 , C12N2740/16322 , C12Q1/68 , C12Q1/6813 , C12Y113/11012
摘要： Sequence-specific oligonucleotides are provided having substantially pure chiral Sp phosphorothioate, chiral Rp phosphorothioate, chiral Sp alkylphosphonate, chiral Rp alkylphosphonate, chiral Sp phosphoamidate, chiral Rp phosphoamidate, chiral Sp phosphotriester, and chiral Rp phosphotriester linkages. The novel oligonucleotides are prepared via a stereospecific SN2 nucleophilic attack of a phosphodiester, phosphorothioate, phosphoramidate, phosphotriester or alkylphosphonate anion on the 3′ position of a xylonucleotide. The reaction proceeds via inversion at the 3′ position of the xylo reactant species, resulting in the incorporation of phosphodiester, phosphorothioate, phosphoramidate, phosphotriester or alkylphosphonate linked ribofuranosyl sugar moieties into the oligonucleotide.

10. 发明授权

US06191266B1 Sugar modified nucleosides 失效
标题翻译：糖改性核苷
公开(公告)号：US06191266B1
公开(公告)日：2001-02-20
申请号：US08766991
申请日：1996-12-16
申请人： Guangyi Wang
发明人： Guangyi Wang
IPC分类号： C07H1900
CPC分类号： C07H19/06 , C07H19/10 , C07H21/00
摘要： A number of modified nucleosides are disclosed composed of modified sugar moieties which contain substituents at C1 and C4 positions, or branched substituents at C3 and C5 positions of deoxyribose or ribose. Each nucleoside is converted to or properly protected and then converted to the corresponding phosphoramidites. These phosphoramidites are used to assemble oligonucleotides in which there is at least one of the forenoted nucleosides. These sugar modified oligonucleotides have the potential to be used as antisense therapies since they are expected to enhance nuclease resistance and cellular uptake while they maintain sequence-specificity and affinity to nucleic acid targets in vitro or in vivo.
摘要翻译：公开了一些修饰的核苷，其由在C1和C4位置含有取代基的修饰的糖部分或脱氧核糖或核糖的C3和C5位置的支链取代基组成。将每个核苷转化成或适当保护，然后转化成相应的亚磷酰胺。这些亚磷酰胺用于组装寡核苷酸，其中存在至少一种预先注射的核苷。这些糖修饰的寡核苷酸具有用作反义治疗的潜力，因为它们预期在体外或体内维持序列特异性和对核酸靶标的亲和力，从而增强核酸酶抗性和细胞摄取。

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