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1. 发明授权

US3994882A Nitrofuran derivatives, process for the preparation thereof and compositions containing same as active ingredient 失效
标题翻译：硝基呋喃衍生物，其制备方法和含有活性成分的组合物
公开(公告)号：US3994882A
公开(公告)日：1976-11-30
申请号：US504987
申请日：1974-09-10
申请人： Ichiro Hirao , Ryuzo Ueno
发明人： Ichiro Hirao , Ryuzo Ueno
IPC分类号： C07D307/71 , C07D307/72
CPC分类号： C07D307/71
摘要： A nitrofuran derivative having the general formula ##SPC1##Wherein R is a group selected from the class consisting of hydroxyl group, hydroxyalkyl group, hydroxyalkoxylakyl group, hydroxyalkylaminoalkyl group, alkoxyalkyl group, sulfoalkyl group, which sulfoalkyl group may be that forming a salt, mercaptoalkyl group, an amino acid, and a residue resulting from the removal of the amino group from an amino acid amide, the amino group or carboxyl group of which residue may be that forming a salt. The nitrofuran derivative is useful as antimicrobial agent.
摘要翻译：具有通式WHEREIN R的硝基呋喃衍生物是选自羟基，羟基烷基，羟基烷氧基烷基，羟基烷基氨基烷基，烷氧基烷基，磺基烷基的基团，该磺基烷基可以是形成盐，巯基烷基，氨基酸和从氨基酰胺除去氨基而得到的残基，其残基可以是形成盐的氨基或羧基。硝基呋喃衍生物可用作抗微生物剂。

2. 发明授权

US07745417B2 Nucleosides or nucleotides having novel unnatural bases and use thereof 有权
标题翻译：具有新的非天然碱基的核苷或核苷及其用途
公开(公告)号：US07745417B2
公开(公告)日：2010-06-29
申请号：US10521454
申请日：2003-02-28
申请人： Ichiro Hirao , Shigeyuki Yokoyama , Michiko Hirao , Tsuneo Mitsui
发明人： Ichiro Hirao , Shigeyuki Yokoyama , Michiko Hirao , Tsuneo Mitsui
IPC分类号： A61K31/70 , C07H19/00 , C07H21/00 , C07H21/02
CPC分类号： C07H11/04 , C07H7/06
摘要： The object of the present invention is to provide a nucleoside or nucleotide having an unnatural base. The nucleoside or nucleotide of the present invention has a 5-substituted-2-oxo(1H)-pyridin-3-yl group as a base. Preferably, the 5-position of the above base is substituted with a substituent selected from the group consisting of the following: 1) a photoreactive group selected from iodine and bromine; 2) an alkenyl group, an alkynyl group or an amino group, or a derivative thereof; 3) biotin or a derivative thereof; and 4) a fluorescent molecule selected from fluorescein, 6-carboxyfluorescein, tetramethyl-6-carboxyrhodamine, and derivatives thereof.
摘要翻译：本发明的目的是提供具有非天然碱基的核苷或核苷酸。本发明的核苷或核苷酸具有5-取代-2-氧代（1H） - 吡啶-3-基作为碱基。优选地，上述碱的5位被选自下列的取代基取代：1）选自碘和溴的光反应性基团; 2）烯基，炔基或氨基或其衍生物; 3）生物素或其衍生物; 和4）选自荧光素，6-羧基荧光素，四甲基-6-羧基罗丹明及其衍生物的荧光分子。

3. 发明申请

US20100036111A1 METHOD FOR REPLICATING NUCLEIC ACIDS AND NOVEL UNNATURAL BASE PAIRS 有权
标题翻译：用于替代核酸和新型基础配对的方法
公开(公告)号：US20100036111A1
公开(公告)日：2010-02-11
申请号：US12096517
申请日：2006-12-07
申请人： Ichiro Hirao , Shigeyuki Yokoyama
发明人： Ichiro Hirao , Shigeyuki Yokoyama
IPC分类号： C12P19/34 , C07H19/04 , C07H19/20
CPC分类号： C12P19/34 , C07H19/04 , C07H21/00 , C12Q1/6844 , C12Q2525/101 , C12Q2525/117 , C12Q2525/113
摘要： The present invention relates to a method for nucleic acid replication and novel artificial base pairs.The method of the present invention for nucleic acid replication is characterized in that a deoxyribonucleoside 5′-triphosphate, in which the hydroxyl group of phosphoric acid at the γ-position is substituted with a group selected from the group consisting of an amino group, a methylamino group, a dimethylamino group, a mercapto group and a fluoro group, is used as a substrate during replication reaction. The novel artificial base pairs of the present invention are characterized in that 7-(2-thienyl)-imidazo[4,5-b]pyridine (Ds) or an analog thereof forms a base pair with pyrrole-2-carbaldehyde (Pa) or an analog thereof.
摘要翻译：本发明涉及核酸复制的方法和新的人造碱基对。用于核酸复制的本发明的方法的特征在于，其中在γ-位上的磷酸的羟基被选自下列的基团取代的脱氧核糖核苷5'-三磷酸：氨基，甲基氨基，二甲基氨基，巯基和氟基在复制反应期间用作底物。本发明的新型人造碱基对的特征在于7-（2-噻吩基） - 咪唑并[4,5-b]吡啶（Ds）或其类似物与吡咯-2-甲醛（Pa）形成碱基对，或其类似物。

4. 发明申请

US20090275017A1 Novel Nucleoside or Nucleotide Derivative and Use Thereof 失效
标题翻译：新型核苷或其衍生物及其用途
公开(公告)号：US20090275017A1
公开(公告)日：2009-11-05
申请号：US11667146
申请日：2005-11-08
申请人： Ichiro Hirao , Shigeyuki Yokoyama
发明人： Ichiro Hirao , Shigeyuki Yokoyama
IPC分类号： C12Q1/68 , C07H21/00 , C07H21/02 , C07H21/04
CPC分类号： C07H21/02
摘要： The object of the present invention is to provide a nucleoside or nucleotide having a 5-substituted-2-oxo(1H)pyridin-3-yl group as a base, as well as a method using the same.In one embodiment, the nucleoside or nucleotide of the present invention has a fluorescent dye selected from the group consisting of 5-FAM, 6-FAM, 5-TAMRA, 6-TAMRA, DANSYL, 5-HEX, 6-HEX, 5-TET, 6-TET, 5-ROX and 6-ROX or a quencher dye selected from the group consisting of DABCYL, BHQ1 and BHQ2, which is attached either directly or through a linker to the 5-position of the above base.
摘要翻译：本发明的目的是提供具有5-取代-2-氧代（1H）吡啶-3-基作为碱的核苷或核苷酸，以及使用其的方法。在一个实施方案中，本发明的核苷或核苷酸具有选自5-FAM，6-FAM，5-TAMRA，6-TAMRA，DANSYL，5-HEX，6-HEX，5- TET，6-TET，5-ROX和6-ROX或选自DABCYL，BHQ1和BHQ2的猝灭剂染料，其直接或通过接头连接到上述碱基的5位上。

5. 发明申请

US20130122506A1 NUCLEIC ACID BASE ANALOGS WITH QUENCHING AND FLUORESCENT ACTIVITIES AND APPLICATIONS THEREOF 有权
标题翻译：具有猝灭和荧光活性的核酸碱基模拟物及其应用
公开(公告)号：US20130122506A1
公开(公告)日：2013-05-16
申请号：US13642111
申请日：2011-04-21
申请人： Ichiro Hirao , Michiko Hirao , Shigeyuki Yokoyama , Tsuneo Mitsui , Rie Yamashige
发明人： Ichiro Hirao , Michiko Hirao , Shigeyuki Yokoyama , Tsuneo Mitsui , Rie Yamashige
IPC分类号： G01N21/64
CPC分类号： G01N21/6486 , C07H19/044 , C12Q1/6818 , C12Q2525/117
摘要： It is an object of the present invention to provide quenching or fluorescent nucleic acid base analogs and applications thereof. The quencher of the present invention has a 2-nitropyrrole structure represented by Formula I:[Formula 1] (in Formula I, R1 and R2 are groups independently selected from the group consisting of: ribose and deoxyribose; hydrogen, hydroxyl and SH groups, and halogens; substituted or unsubstituted alkyl, alkenyl, and alkynyl groups each having 2 to 10 carbon atoms; one or more five-membered heterocyclic rings, one or more six-membered heterocyclic rings, and one or more fused heterocyclic rings, these heterocylic rings containing nitrogen or sulfur, and one or more aromatic rings; sugars, sugar chains, amino acids, and peptides; and fluorescent molecules linked via linkers).
摘要翻译：本发明的目的是提供淬灭或荧光核酸碱基类似物及其应用。本发明的猝灭剂具有由式I表示的2-硝基吡咯结构：[式1]（式I中，R 1和R 2分别独立地选自：核糖和脱氧核糖;氢，羟基和SH基团，卤素;取代或未取代的各自具有2-10个碳原子的烷基，烯基和炔基;一个或多个五元杂环，一个或多个六元杂环和一个或多个稠合杂环，这些杂环含有氮或硫，以及一个或多个芳环;糖，糖链，氨基酸和肽;以及通过接头连接的荧光分子）。

6. 发明申请

US20120245340A1 NOVEL ARTIFICIAL FLUORESCENT BASES 有权
标题翻译：新人造荧光基
公开(公告)号：US20120245340A1
公开(公告)日：2012-09-27
申请号：US13500303
申请日：2010-10-06
申请人： Ichiro Hirao , Michiko Hirao , Shigeyuki Yokoyama , Tsuneo Mitsui
发明人： Ichiro Hirao , Michiko Hirao , Shigeyuki Yokoyama , Tsuneo Mitsui
IPC分类号： C07H19/20 , C07H21/02 , C07H19/173 , C07H21/04 , C12P19/34 , C07H19/048
CPC分类号： C07D471/04 , C07D473/32 , C07H19/173 , C07H19/23 , C09K11/06 , C09K2211/1074
摘要： The present invention relates to novel unnatural fluorescent nucleic acid bases, that is, a purine base, a 1-deazapurine base, and a 1,7-deazapurine base each having a functional group which consists of two or more heterocyclic moieties linked together, at the 6-position thereof (the 6-position of purine ring). The present invention also relates to a compound containing the unnatural base, a derivative thereof, and a nucleic acid containing a nucleotide having the unnatural base. The present invention also relates to a method of preparing the nucleic acid. The unnatural base of the present invention has excellent fluorescence characteristics and also has excellent properties as a universal base.
摘要翻译：本发明涉及新型非天然荧光核酸碱基，即嘌呤碱，1-脱氮嘌呤碱和1,7-deazapurine碱，其各自具有由两个或多个连接在一起的杂环基部分组成的官能团，在其6-位（嘌呤环的6-位）。本发明还涉及含有非天然碱，其衍生物和含有具有非天然碱基的核苷酸的核酸的化合物。本发明还涉及制备核酸的方法。本发明的非天然碱具有优异的荧光特性，也具有优异的作为通用基材的特性。

7. 发明授权

US07667031B2 Nucleic acid base pair 失效
标题翻译：核酸碱基对
公开(公告)号：US07667031B2
公开(公告)日：2010-02-23
申请号：US11078607
申请日：2005-03-10
申请人： Ichiro Hirao , Masahide Ishikawa , Tsuyoshi Fujihara , Shigeyuki Yokoyama
发明人： Ichiro Hirao , Masahide Ishikawa , Tsuyoshi Fujihara , Shigeyuki Yokoyama
IPC分类号： C07H21/00 , C07H21/04 , C07H19/06 , C07H19/048
CPC分类号： C07H11/04 , C07H19/207 , C07H21/00 , C12N15/11 , C12P21/02
摘要： A novel artificial nucleic acid base pair which is obtained by forming a selective base pair by introducing a group having steric hindrance (preferably a group having steric hindrance and static repulsion and a stacking effect) and can be recognized by a polymerase such as DNA polymerase; a novel artificial gene; and a method of designing nucleic acid bases so as to form a selective base pair with the use of steric hindrance, static repulsion and stacking effect at the base moiety of the nucleic acid. An artificial nucleic acid comprising these bases; a process for producing the same; a codon containing the same; a nucleic acid molecule containing the same; a process for producing a non-natural gene by using the same; a process for producing a novel protein by using the above nucleic acid molecule or non-natural gene, and the like.
摘要翻译：通过引入具有空间位阻的基团（优选具有空间位阻和静电排斥和堆叠效应的基团）形成选择性碱基对而获得的新型人造核酸碱基对，可以通过聚合酶如DNA聚合酶识别; 一种新型人工基因; 以及设计核酸碱基以在核酸的碱基部分上使用空间位阻，静电排斥和堆叠效应形成选择性碱基对的方法。包含这些碱的人造核酸; 其制造方法; 含有相同的密码子; 含有该核酸分子的核酸分子; 通过使用该方法生产非天然基因的方法; 通过使用上述核酸分子或非天然基因来生产新型蛋白质的方法等。

8. 发明授权

US06995249B1 Nucleic acid capable of binding specifically to Ras target protein 失效
标题翻译：能够特异性结合Ras靶蛋白的核酸
公开(公告)号：US06995249B1
公开(公告)日：2006-02-07
申请号：US09529397
申请日：1999-08-13
申请人： Shigeyuki Yokoyama , Ichiro Hirao , Kensaku Sakamoto
发明人： Shigeyuki Yokoyama , Ichiro Hirao , Kensaku Sakamoto
IPC分类号： C07H21/02 , C07H21/04
CPC分类号： C12N15/1135 , A61K38/00 , C12N2310/13
摘要： A novel nucleic acid (aptamer) which binds specifically to the target protein of Ras, more particularly, a novel RNA aptamer which binds specifically to Raf-1; a method for screening an RNA capable of binding specifically to the target protein of Ras which comprises selecting an RNA capable of binding to the target protein of Ras from a pool of RNAs having various base sequences; a method for regulating the signal transduction causing the proliferation or differentiation of cells by using the above-described nucleic acid; and medicinal compositions with the use of the same.
摘要翻译：特异性结合Ras靶蛋白的新型核酸（适配体），特别是与Raf-1特异性结合的新型RNA适体; 用于筛选能够特异性结合Ras的靶蛋白的RNA的方法，其包括从具有各种碱基序列的RNA库中选择能够结合Ras的靶蛋白的RNA; 通过使用上述核酸调节引起细胞增殖或分化的信号转导的方法; 和使用它们的药物组合物。

9. 发明授权

US08895712B2 Artificial base pair capable of forming specific base pair 有权
标题翻译：能够形成特定碱基对的人造碱基对
公开(公告)号：US08895712B2
公开(公告)日：2014-11-25
申请号：US13500635
申请日：2010-10-06
申请人： Ichiro Hirao , Michiko Hirao , Shigeyuki Yokoyama
发明人： Ichiro Hirao , Michiko Hirao , Shigeyuki Yokoyama
IPC分类号： C07H21/02 , C07H21/04
CPC分类号： C07H21/02 , C07H21/04 , C12Q1/6827 , C12Q1/6832 , C12Q2527/107 , C12Q2525/117
摘要： The present invention provides a double-stranded nucleic acid in which at least one nucleic acid strand includes an unnatural base that forms a self-complementary base pair or an unnatural base that forms a base pair with any natural base with substantially the same thermal stability. The present invention also provides a method of hybridizing a first nucleic acid strand with a second nucleic acid strand, wherein the first nucleic acid strand includes an unnatural base that forms a self-complementary base pair or an unnatural base that forms a base pair with any natural base with substantially the same thermal stability, and a method of applying the nucleic acid to SNP detection, a DNA chip, DNA/RNA computing, or an in vitro translation system. The present invention provides a method of introducing an unnatural base into a nucleic acid strand and thereby controlling the thermodynamic stability in hybridization of the nucleic acid strand.
摘要翻译：本发明提供双链核酸，其中至少一个核酸链包含形成自身互补碱基对的非天然碱基或与任何具有基本上相同热稳定性的天然碱形成碱基对的非天然碱基。本发明还提供了将第一核酸链与第二核酸链杂交的方法，其中所述第一核酸链包含形成自身互补碱基对的非天然碱基或与任意形成碱基对的非天然碱基具有基本上相同的热稳定性的天然碱基，以及将核酸应用于SNP检测，DNA芯片，DNA / RNA计算或体外翻译系统的方法。本发明提供了将非天然碱引入核酸链，从而控制核酸链杂交时的热力学稳定性的方法。

10. 发明申请

US20120231462A1 ARTIFICIAL BASE PAIR CAPABLE OF FORMING SPECIFIC BASE PAIR 有权
标题翻译：人造基础配对形成特定基础对
公开(公告)号：US20120231462A1
公开(公告)日：2012-09-13
申请号：US13500635
申请日：2010-10-06
申请人： Ichiro Hirao , Michiko Hirao , Shigeyuki Yokoyama
发明人： Ichiro Hirao , Michiko Hirao , Shigeyuki Yokoyama
IPC分类号： C12Q1/68 , C07K1/00 , G01N33/566 , C07H21/02 , C07H21/04
CPC分类号： C07H21/02 , C07H21/04 , C12Q1/6827 , C12Q1/6832 , C12Q2527/107 , C12Q2525/117
摘要： The present invention provides a double-stranded nucleic acid in which at least one nucleic acid strand includes an unnatural base that forms a self-complementary base pair or an unnatural base that forms a base pair with any natural base with substantially the same thermal stability. The present invention also provides a method of hybridizing a first nucleic acid strand with a second nucleic acid strand, wherein the first nucleic acid strand includes an unnatural base that forms a self-complementary base pair or an unnatural base that forms a base pair with any natural base with substantially the same thermal stability, and a method of applying the nucleic acid to SNP detection, a DNA chip, DNA/RNA computing, or an in vitro translation system. The present invention provides a method of introducing an unnatural base into a nucleic acid strand and thereby controlling the thermodynamic stability in hybridization of the nucleic acid strand.
摘要翻译：本发明提供双链核酸，其中至少一个核酸链包含形成自身互补碱基对的非天然碱基或与任何具有基本上相同热稳定性的天然碱形成碱基对的非天然碱基。本发明还提供了将第一核酸链与第二核酸链杂交的方法，其中所述第一核酸链包含形成自身互补碱基对的非天然碱基或与任意形成碱基对的非天然碱基具有基本上相同的热稳定性的天然碱基，以及将核酸应用于SNP检测，DNA芯片，DNA / RNA计算或体外翻译系统的方法。本发明提供了将非天然碱引入核酸链，从而控制核酸链杂交时的热力学稳定性的方法。

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