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1. 发明申请

WO1998016540A1 IMPROVED COUPLING ACTIVATORS FOR OLIGONUCLEOTIDE SYNTHESIS 审中-公开
标题翻译：改进的联合激活剂用于寡核苷酸合成
公开(公告)号：WO1998016540A1
公开(公告)日：1998-04-23
申请号：PCT/US1997015744
申请日：1997-10-08
申请人： NEXSTAR PHARMACEUTICALS, INC. , VARGEESE, Chandra , PIEKEN, Wolfgang , CARTER, Jeffrey, D. , YEGGE, John
发明人： NEXSTAR PHARMACEUTICALS, INC.
IPC分类号： C07H21/00
CPC分类号： C07H21/00 , C07H19/04
摘要： A method for coupling phosphoramidite monomers with nucleophiles, for example, the 5'-hydroxyl group on the growing oligonucleotide chain, using a coupling activator that is less acidic than and at least as nucleophilic as tetrazole and that provides comparable or better coupling efficiency than tetrazole. The pKa of the coupling activator is between 5.0 and 6.0, preferably between 5.0 and 5.5, and, more preferably, between 5.1 and 5.3. Suitable coupling activators include 4,5-dicyanoimidazole (DCI), 4-alkylthioimidazole, 2-alkylthioimidazole, 2-nitroimidazole, 4-nitroimidazole, 4,5-dihaloimidazole, 4-haloimidazole, 2-haloimidazole and 5-alkoxytetrazole. DCI is the most preferred coupling activator. Alternatively, a combination of an acidic coupling activator and a suitable buffer, such as a tertiary amine, can be employed. The tertiary amine can be a tertiary amine with three alkyl groups or a heterocyclic compound containing one or more tertiary amines. Preferably the tertiary amine is less nucleophilic than DMAP, which is known to cause side reactions at the 6-position oxygen of guanosines due to its relatively high nucleophilicity. N-methylimidazole (NMI) is the preferred tertiary amine.
摘要翻译：使用比四唑低至少至少亲核的偶联活化剂，并且提供与四唑相当或更好的偶联效率的亚磷酰胺单体与亲核试剂偶联的方法，例如生长的寡核苷酸链上的5'-羟基。偶联活化剂的pKa为5.0至6.0，优选5.0至5.5，更优选为5.1至5.3。合适的偶联活化剂包括4,5-二氰基咪唑（DCI），4-烷基硫代咪唑，2-烷基硫代咪唑，2-硝基咪唑，4-硝基咪唑，4,5-二卤代咪唑，4-卤代咪唑，2-卤代咪唑和5-烷氧基四唑。 DCI是最优选的偶联活化剂。或者，可以使用酸性偶合活化剂和合适的缓冲剂如叔胺的组合。叔胺可以是具有三个烷基的叔胺或含有一个或多个叔胺的杂环化合物。优选地，叔胺的亲核性低于DMAP，由于其相对高的亲核性，已知它们在鸟苷的6-位氧引起副反应。 N-甲基咪唑（NMI）是优选的叔胺。

2. 发明申请

WO1997028178A1 HIGH AFFINITY NUCLEIC ACID LIGANDS OF COMPLEMENT SYSTEM PROTEINS 审中-公开
标题翻译：补充系统蛋白质的高亲和核酸配体
公开(公告)号：WO1997028178A1
公开(公告)日：1997-08-07
申请号：PCT/US1997001739
申请日：1997-01-30
申请人： NEXSTAR PHARMACEUTICALS, INC. , BIESECKER, Gregory , GOLD, Larry
发明人： NEXSTAR PHARMACEUTICALS, INC.
IPC分类号： C07H21/02
CPC分类号： C12N15/115 , A61K38/00 , A61K45/06 , C12N2310/151 , C12N2310/315
摘要： Methods are described for the identification and preparation of high affinity nucleic acid ligands to Complement System Proteins. Methods are described for the identification and preparation of high affinity nucleic acid ligands to Complement System Protein, C1q. Included in the invention are specific RNA ligands to C1q identified by the SELEX method.
摘要翻译：描述了用于鉴定和制备补体系统蛋白质的高亲和力核酸配体的方法。描述了用于鉴定和制备补体系统蛋白C1q的高亲和力核酸配体的方法。包括在本发明中的是通过SELEX方法鉴定的C1q的特异性RNA配体。

3. 发明申请

WO1996041010A1 NUCLEIC ACID LIGANDS THAT BIND TO AND INHIBIT DNA POLYMERASES 审中-公开
标题翻译：包含和抑制DNA聚合物的核酸配体
公开(公告)号：WO1996041010A1
公开(公告)日：1996-12-19
申请号：PCT/US1996009451
申请日：1996-06-05
申请人： NEXSTAR PHARMACEUTICALS, INC. , GOLD, Larry , JAYASENA, Sumedha
发明人： NEXSTAR PHARMACEUTICALS, INC.
IPC分类号： C12Q01/68
CPC分类号： C12Q1/6811 , C12N15/115 , C12N2310/16 , C12Q1/6848 , C12Y207/07007 , G01N2333/96433 , Y10S435/81 , C12Q2541/101 , C12Q2521/101 , C12Q2527/101 , C12Q2525/205
摘要： This invention discloses high-affinity oligonucleotide ligands to the thermostable Taq polymerase and Tth polymerase. Specifically, this invention discloses DNA ligands having the ability to bind to the Taq and Tth polymerases and the methods for obtaining such ligands. The ligands are capable of inhibiting polymerases at ambient temperatures.
摘要翻译：本发明公开了耐热Taq聚合酶和Tth聚合酶的高亲和力寡核苷酸配体。具体地，本发明公开了具有结合Taq和Tth聚合酶的能力的DNA配体和获得这种配体的方法。配体能够在环境温度下抑制聚合酶。

4. 发明申请

WO1996016972A1 PURINE NUCLEOSIDE MODIFICATIONS BY PALLADIUM CATALYZED METHODS 审中-公开
标题翻译： PURINE NUCLEOSIDE改性通过钯催化方法
公开(公告)号：WO1996016972A1
公开(公告)日：1996-06-06
申请号：PCT/US1995015124
申请日：1995-11-20
申请人： NEXSTAR PHARMACEUTICALS, INC.
发明人： NEXSTAR PHARMACEUTICALS, INC. , TU, Chi , EATON, Bruce
IPC分类号： C07H01/00
CPC分类号： C07H19/16 , B01J31/2404 , B01J2231/4255 , B01J2531/824 , C07H19/06 , C07H19/10 , C07H19/20 , C07H21/00
摘要： This invention discloses an improved method for the preparation of modified purine nucleosides using a palladium catalyst.
摘要翻译：本发明公开了一种使用钯催化剂制备修饰的嘌呤核苷的改进方法。

5. 发明申请

WO1995021853A1 HIGH-AFFINITY LIGANDS OF BASIC FIBROBLAST GROWTH FACTOR AND THROMBIN 审中-公开
标题翻译：基础成纤维细胞生长因子和血红蛋白的高亲属关系
公开(公告)号：WO1995021853A1
公开(公告)日：1995-08-17
申请号：PCT/US1995001458
申请日：1995-02-06
申请人： NEXSTAR PHARMACEUTICALS, INC. , JANJIC, Nebojsa , GOLD, Larry , TASSET, Diane
发明人： NEXSTAR PHARMACEUTICALS, INC.
IPC分类号： C07H21/02
CPC分类号： C12N15/115 , C07H21/00 , C12N15/1048 , C12N2310/13 , C12N2310/322 , C12N2310/53 , C12Q1/6811 , C40B40/00 , G01N2333/96433
摘要： The present invention utilizes the SELEX (Systematic Evolution of Ligands for EXponential Enrichment) method for identifying and preparing nucleic acid ligands to basic fibroblast growth factor (bFGF) and thrombin. Included in the invention are nucleic acid ligands to bFGF which are inhibitors of bFGF and 2' -amino-modified RNA ligands to bFGF. Further included in the present invention are modified nucleotide sequences to thrombin based on the sequences of the RNA ligands identified. The modified RNA ligands to bFGF and thrombin exhibit increased in vivo stability.
摘要翻译：本发明利用SELEX（用于指数浓缩的配体的系统演化）方法来鉴定和制备碱性成纤维细胞生长因子（bFGF）和凝血酶的核酸配体。本发明中包括bFGF的核酸配体，其是bFGF的抑制剂和bFGF的2'-氨基修饰的RNA配体。进一步包括在本发明中的是基于所鉴定的RNA配体的序列的凝血酶的修饰的核苷酸序列。 bFGF和凝血酶的修饰的RNA配体表现出增加的体内稳定性。

6. 发明申请

WO1996040991A1 ENZYME LINKED OLIGONUCLEOTIDE ASSAYS (ELONAS) 审中-公开
标题翻译：酶联系寡核苷酸测定（ELONAS）
公开(公告)号：WO1996040991A1
公开(公告)日：1996-12-19
申请号：PCT/US1996007439
申请日：1996-05-22
申请人： NEXSTAR PHARMACEUTICALS, INC.
发明人： NEXSTAR PHARMACEUTICALS, INC. , DROLET, Dan , JAYASENA, Sumedha , GOLD, Larry
IPC分类号： C12Q01/68
CPC分类号： G01N33/76 , A61K47/549 , B82Y5/00 , C07H19/06 , C07H19/10 , C07H21/00 , C07K14/001 , C12N9/1276 , C12N15/1048 , C12N15/115 , C12N2310/13 , C12N2310/322 , C12N2310/53 , C12Q1/37 , C12Q1/68 , C12Q1/6811 , C12Q1/6813 , C40B40/00 , F02B2075/027 , G01N33/531 , G01N33/532 , G01N33/535 , G01N33/56988 , G01N33/68 , G01N2333/16 , G01N2333/163 , G01N2333/503 , G01N2333/8125 , G01N2333/96433 , G01N2333/96436 , G01N2333/96486 , G01N2333/966 , G01N2333/974 , C12Q2525/101 , C12Q2563/131
摘要： This invention discloses novel immunoassay termed as ELONA, employing nucleic acid ligands as capture molecules and/or detector molecules.
摘要翻译：本发明公开了使用核酸配体作为捕获分子和/或检测分子的称为ELONA的新型免疫测定法。

7. 发明申请

WO1996040703A1 HIGH AFFINITY NUCLEIC ACID LIGANDS TO LECTINS 审中-公开
标题翻译：高亲和性核酸配体
公开(公告)号：WO1996040703A1
公开(公告)日：1996-12-19
申请号：PCT/US1996009455
申请日：1996-06-05
申请人： NEXSTAR PHARMACEUTICALS, INC. , PARMA, David, H. , HICKE, Brian , BRIDONNEAU, Philippe , GOLD, Larry
发明人： NEXSTAR PHARMACEUTICALS, INC.
IPC分类号： C07H19/00
CPC分类号： C12Q1/6811 , G01N33/53 , G01N2333/4724 , G01N2333/7056 , G01N2333/96433
摘要： This invention discloses high-affinity oligonucleotide ligands to lectins, specifically nucleic acid ligands having the ability to bind to the lectins, wheat germ agglutinin, L-selectin, E-selectin and P-selectin. Also disclosed are the methods for obtaining such ligands.
摘要翻译：本发明公开了具有凝集素的高亲和力寡核苷酸配体，特别是具有与凝集素结合的能力的核酸配体，小麦胚芽凝集素，L-选择蛋白，E-选择蛋白和P-选择蛋白。还公开了获得这种配体的方法。

8. 发明申请

WO1996040064A1 LIPOSOMAL CYCLOSPORIN FORMULATIONS AS AGENTS FOR IMMUNOSUPPRESSION AND MULTIPLE DRUG RESISTANT INDICATIONS 审中-公开
标题翻译：作为免疫抑制剂和多种耐药性物质的药物环磷酰胺制剂
公开(公告)号：WO1996040064A1
公开(公告)日：1996-12-19
申请号：PCT/US1996009053
申请日：1996-06-06
申请人： NEXSTAR PHARMACEUTICALS, INC.
发明人： NEXSTAR PHARMACEUTICALS, INC. , MOYNIHAN, Karen, L. , ADLER-MOORE, Jill , CHIANG, Su-Ming
IPC分类号： A61K09/127
CPC分类号： A61K38/13 , A61K9/127
摘要： Improved liposomal encapsulated cyclosporin formulations are disclosed. The liposomes are efficacious as immunosuppressant agents and in the treatment of drug resistant cancers. The formulations include liposomes comprised of a phosphatidylcholine, cholesterol, a phosphatidylglycerol and a cyclosporin. In one embodiment, the mole ratios of phosphatidylcholine, cholesterol, phosphatidylglycerol and cyclosporin are about 21:0.5:3:1 to 21:1.5:3:1 and 24:0.5:3:1 to 24:1.5:31 wherein the liposomes comprise unilamellar vesicles having a size less than 100 nm. In a preferred embodiment, the compositions are stable upon injection into the blood stream of a mammal, preferably a human. In this embodiment, the preferred ratios of PC:chol:PG:CSA are from about 28:1:3:1 to 40:1:3:1. The preferred formulas are PC:chol:DMPG:CSA wherein the PC is HSPC and the molar ratios are: 28:1:3:1, 30:1:3:1, 32:1:3:1, 34:1:3:1, 35:1:3:1, 36:1:3:1, and 40:1:3:1. Also provided is a liposome encapsulated cyclosporin which provides for a cyclosporin which associates to a significant degree with a liposomal/plasma fraction (vs. cell fraction) of blood as a function of time. Liposomes having these properties are comprised of phosphatidylcholine, cholesterol, dimyristoylphosphatidylglycerol and cyclosporin. These liposomes are unilamellar and have a size less than 75 nanometers and are stable in whole mammal blood. Further provided are liposomes having increased therapeutic indices. The liposomes are stable on storage, contain a therapeutically effective amount of a cyclosporin, provide a liposomal cyclosporin formulation having reduced toxicity, and, in the preferred embodiment, provides a liposomal formulation which is stable in whole blood.
摘要翻译：公开了改进的脂质体包封的环孢菌素制剂。脂质体作为免疫抑制剂和用于治疗耐药性癌症是有效的。制剂包括由磷脂酰胆碱，胆固醇，磷脂酰甘油和环孢菌素组成的脂质体。在一个实施方案中，磷脂酰胆碱，胆固醇，磷脂酰甘油和环孢菌素的摩尔比为约21：0.5：3：1至21：1.5：3：1和24：0.5：3：1至24：1.5：31，其中脂质体包含具有小于100nm尺寸的单层囊泡。在优选的实施方案中，组合物在注射到哺乳动物，优选人的血液中时是稳定的。在本实施例中，PC：chol：PG：CSA的优选比例为约28：1：3：1至40：1：3：1。优选的配方是PC：chol：DMPG：CSA，其中PC是HSPC，摩尔比为：28：1：3：1,30：1：3：1，32：1：3： 3：1,35：1：3：1，36：1：3：1和40：1：3：1。还提供了一种脂质体包封的环孢菌素，其提供了一种环状细胞，其显着程度地与作为时间的函数的血液的脂质体/血浆部分（相对于细胞部分）相关联。具有这些性质的脂质体由磷脂酰胆碱，胆固醇，二肉豆蔻酰磷脂酰甘油和环孢菌素组成。这些脂质体是单层的，其尺寸小于75纳米，在整个哺乳动物血液中是稳定的。还提供了具有增加的治疗指数的脂质体。脂质体在储存时稳定，含有治疗有效量的环孢菌素，提供具有降低的毒性的脂质体环孢菌素制剂，并且在优选的实施方案中，提供在全血中稳定的脂质体制剂。

9. 发明申请

WO1996039539A1 METHOD AND APPARATUS FOR DETERMINING CONSENSUS SECONDARY STRUCTURES FOR NUCLEIC ACID SEQUENCES 审中-公开
标题翻译：用于确定核酸序列的共同二级结构的方法和装置
公开(公告)号：WO1996039539A1
公开(公告)日：1996-12-12
申请号：PCT/US1996009452
申请日：1996-06-06
申请人： NEXSTAR PHARMACEUTICALS, INC.
发明人： NEXSTAR PHARMACEUTICALS, INC. , DAVIS, Jeffrey, P. , JANJIC, Nebojsa , ZICHI, Dominic, A.
IPC分类号： C12Q01/68
CPC分类号： G06F19/16 , C07K1/00 , G06F19/22 , Y10T436/143333
摘要： The present invention utilizes a dot matrix display to visualize consensus secondary structures of functionally related sequence sets.
摘要翻译：本发明利用点阵显示来观察功能相关序列集合的一致二级结构。

10. 发明申请

WO1996027605A1 SYSTEMATIC EVOLUTION OF LIGANDS BY EXPONENTIAL ENRICHMENT: CHEMI-SELEX 审中-公开
标题翻译：通过经验丰富的配方系统演变：CHEMI-SELEX
公开(公告)号：WO1996027605A1
公开(公告)日：1996-09-12
申请号：PCT/US1996003097
申请日：1996-03-05
申请人： NEXSTAR PHARMACEUTICALS, INC. , UNIVERSITY RESEARCH CORPORATION , GOLD, Larry , EATON, Bruce , SMITH, Drew , WECKER, Matthew , JENSEN, Kirk
发明人： NEXSTAR PHARMACEUTICALS, INC. , UNIVERSITY RESEARCH CORPORATION
IPC分类号： C07H21/02
CPC分类号： G01N33/76 , A61K47/547 , A61K47/549 , B82Y5/00 , C07H19/06 , C07H19/10 , C07H21/00 , C07K14/001 , C12N9/1276 , C12N15/1048 , C12N15/115 , C12N2310/13 , C12N2310/322 , C12N2310/53 , C12Q1/37 , C12Q1/6811 , C40B40/00 , F02B2075/027 , G01N33/531 , G01N33/532 , G01N33/535 , G01N33/56988 , G01N33/68 , G01N2333/163 , G01N2333/575 , G01N2333/62 , G01N2333/8125 , G01N2333/96433 , G01N2333/96436 , G01N2333/96455 , G01N2333/96486 , G01N2333/966 , G01N2333/9726 , G01N2333/974 , G01N2333/976 , C12Q2525/101
摘要： This application provides methods for identifying nucleic acid ligands capable of covalently interacting with targets of interest. The nucleic acids can be associated with various functional units. The method also allows for the identification of nucleic acids that have facilitating activities as measured by their ability to facilitate formation of a covalent bond between the nucleic acid, including it associated functional unit, and its target.
摘要翻译：该应用提供了用于鉴定能够与感兴趣的靶标共价相互作用的核酸配体的方法。核酸可以与各种功能单元相关联。该方法还允许鉴定具有促进活性的核酸，其通过其促进核酸（包括其相关功能单元）与其靶标之间形成共价键的能力来测量。

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