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    • 71. 发明授权
    • Oligonucleotide tagged nucleoside triphosphates (OTNTPs) for genetic analysis
    • 寡核苷酸标记核苷三磷酸(OTNTP)用于遗传分析
    • US07109316B2
    • 2006-09-19
    • US10226734
    • 2002-08-23
    • Shiv KumarAnup SoodSudhakar RaoJohn Nelson
    • Shiv KumarAnup SoodSudhakar RaoJohn Nelson
    • C07H21/02C07H21/04C07H19/04C12Q1/68
    • C07H19/04
    • Oligonucleotide tagged nucleoside triphosphates, OTNTPs, which are substrates for polymerases and or terminal nucleotidyl transferases are provided as well as methods of making these OTNTPs. Further provided are OTNTPs with fluorescent dyes including energy transfer dyes, attached to the oligonucleotide chain, OTNTPs with unnatural bases incorporated in the oligonucleotide sequence and methods for incorporating these OTNTPs in DNA or RNA. Also provided are methods for using the oligonucleotides on OTNTPs for amplifying the oligo sequence on the OTNTP using an amplification method described above. Further provided are reactive bifunctional amidites, methods of making these compounds and methods for detecting single nucleotide polymorphisms using the above OTNTPs. Methods for detecting differential gene expression using the OTNTPs and methods of separating specifically modified DNA or RNA using the OTNTPs are also provided.
    • 提供了寡聚核苷酸标记的核苷三磷酸酯,OTNTP,其是用于聚合酶和末端核苷酸转移酶的底物,以及制备这些OTNTP的方法。 还提供了含有荧光染料的OTNTP,其包括与寡核苷酸链连接的能量转移染料,掺入寡核苷酸序列中的非天然碱基的OTNTP以及将这些OTNTP引入DNA或RNA中的方法。 还提供了使用寡核苷酸在OTNTP上使用上述扩增方法在OTNTP上扩增寡核苷酸序列的方法。 还提供了反应性双官能脒,制备这些化合物的方法和使用上述OTNTP检测单核苷酸多态性的方法。 还提供了使用OTNTP检测差异基因表达的方法和使用OTNTP分离特异性修饰的DNA或RNA的方法。
    • 73. 发明授权
    • Heterocyclic amine-boranes, and method of inhibiting DNA topoisomerase
activity and/or combatting inflammation, hyperlipidemia, and/or
neoplasia using amine-borane compounds
    • 杂环胺 - 硼烷和使用胺 - 硼烷化合物抑制DNA拓扑异构酶活性和/或抵抗炎症,高脂血症和/或瘤形成的方法
    • US5280119A
    • 1994-01-18
    • US786279
    • 1991-11-01
    • Bernard F. SpielvogelAnup SoodIris H. Hall
    • Bernard F. SpielvogelAnup SoodIris H. Hall
    • C07F5/02A61K33/22A61K43/00
    • C07F5/022C07F5/027
    • Heterocyclic amine-borane compounds of the formula: ##STR1## wherein: A is a heterocyclic amine moiety selected from the group consisting of piperidine, substituted piperidine, piperazine, substituted piperazine, imidazole, substituted imidazole, pyrazole, substituted pyrazole, pyrazine, substituted pyrazine, pyrrole, substituted pyrrole, pyrrolidine, substituted pyrrolidine, indole, substituted indole, indoline, substituted indoline, quinoline, substituted quinoline, isoquinoline, substituted isoquinoline, thiazole, substituted thiazole, oxazole, substituted oxazole, thiazolidine, and substituted thiazolidine, wherein substitution is at any or all substituent positions, and comprises substituents selected from the group consisting of alkyl (preferably C.sub.1 -C.sub.10 linear or branched alkyl), alkylaryl, aryl, aralkyl, nitro, alkoxy, hydroxy, cyano, thiol, and halo;R.sub.1 is selected from H, alkyl (preferably C.sub.1 -C.sub.10 linear or branched alkyl), alkylaryl, aryl, and arylalkyl; andR.sub.2 is selected from CN, COOH, COOR.sub.3, and CONHR.sub.3 where R.sub.3 is selected from H, alkyl (preferably C.sub.1 -C.sub.10 linear or branched alkyl), alkylaryl, aryl, aralkyl.The heterocyclic amine-borane compounds of the invention are bioactive in character, variously exhibiting anti-tumor, anti-inflammatory, and anti-hyperlipidemic activity. In another aspect, the invention relates to a method of inhibiting enzyme activity (e.g., DNA topoisomerase II, PRPP amidotransferase, IMP dehydrogenase, dihydrofolate reductase, and/or ribonucleotide reductase) in an in vitro or in vivo system, comprising administering to the system an enzyme-inhibitingly effective amount of a Lewis-base borane adduct, such as for example a heterocyclic amine-borane compound of the foregoing formula.
    • 式(I)的杂环胺 - 硼烷化合物,其中:A是杂环胺部分; R1选自H,烷基,烷基芳基,芳基和芳基烷基; 并且R 2选自CN,COOH,COOR 3和CONHR 3,其中R 3选自H,烷基,烷基芳基,芳基,芳烷基。 本发明的杂环胺 - 硼烷化合物是具有生物活性的,各种表现出抗肿瘤,抗炎和抗高血脂活性。 本发明还包括在体外或体内系统中抑制酶活性的方法(例如,DNA拓扑异构酶II,PRPP氨基转移酶,IMP脱氢酶,二氢叶酸还原酶和/或核糖核苷酸还原酶),包括向系统施用酶抑制 有效量的路易斯碱硼烷加合物,例如上述式的杂环胺 - 硼烷化合物。