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公开(公告)号:US08822671B2
公开(公告)日:2014-09-02
申请号:US13990441
申请日:2011-11-28
申请人: Mamoru Shimizu , Takeshi Wada , Kouichiro Arai
发明人: Mamoru Shimizu , Takeshi Wada , Kouichiro Arai
IPC分类号: C07H21/02 , C07H19/10 , C07H23/00 , C07H19/06 , C07H1/00 , C07H19/067 , C07H19/167
CPC分类号: C07H21/02 , C07H1/00 , C07H19/06 , C07H19/067 , C07H19/10 , C07H19/167 , C07H23/00 , Y02P20/55
摘要: A 2′-modified ribonucleoside having an alkoxymethyl protective group can be imparted with a high duplex-forming ability by introducing, as a substituent, a halogen atom into the protective group moiety. A modified form of RNA having a halogen-substituted alkoxymethyl protective group exhibits a high duplex-forming ability that is comparable to the duplex-forming ability of a 2′-O-methyl modified nucleic acid.
摘要翻译: 具有烷氧基甲基保护基的2'-修饰的核糖核苷可通过将卤素原子引入保护基部分而赋予高双相形成能力。 具有卤素取代的烷氧基甲基保护基的RNA的修饰形式表现出与2'-O-甲基修饰的核酸的双链体形成能力相当的高双相形成能力。
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公开(公告)号:US20130253178A1
公开(公告)日:2013-09-26
申请号:US13990441
申请日:2011-11-28
申请人: Mamoru Shimizu , Takeshi Wada , Kouichiro Arai
发明人: Mamoru Shimizu , Takeshi Wada , Kouichiro Arai
CPC分类号: C07H21/02 , C07H1/00 , C07H19/06 , C07H19/067 , C07H19/10 , C07H19/167 , C07H23/00 , Y02P20/55
摘要: [Problem]To provide a 2′-modified ribonucleoside or the like which has a high duplex-forming ability.[Solution]The present invention is generally based on the finding in embodiments that a modified form of a ribonucleoside or the like having an alkoxymethyl protective group can be imparted with a high duplex-forming ability by introducing, as a substituent, a halogen atom into the protective group moiety. As explained before, a modified form of RNA having an alkoxymethyl protective group has a low duplex-forming ability. A modified form of RNA having a halogen-substituted alkoxymethyl protective group, however, exhibits a high duplex-forming ability that is comparable to the duplex-forming ability of a 2′-O-methyl modified nucleic acid.
摘要翻译: [问题]提供具有高双相形成能力的2'-修饰的核糖核苷等。 [解决方案]本发明通常基于实施方案中发现,通过将卤素原子引入作为取代基的卤素原子,可以赋予具有烷氧基甲基保护基的核糖核苷等的修饰形式具有高双相形成能力 保护基团部分。 如前所述,具有烷氧基甲基保护基的RNA的修饰形式具有低的双链体形成能力。 然而,具有卤素取代的烷氧基甲基保护基的RNA的修饰形式表现出与2'-O-甲基修饰的核酸的双链体形成能力相当的高双相形成能力。
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公开(公告)号:US08470987B2
公开(公告)日:2013-06-25
申请号:US12882390
申请日:2010-09-15
申请人: Takeshi Wada , Mamoru Shimizu
发明人: Takeshi Wada , Mamoru Shimizu
CPC分类号: C07F9/65586 , C07F9/65616 , C07F9/65844 , C07H19/067 , C07H19/167 , Y02P20/55
摘要: A protective group represented by the following general formula (I) (the oxygen atom attached with * represents oxygen atom of 2′-hydroxyl group of a ribonucleoside, a ribonucleotide or a derivative thereof; R1 and R2 both represent hydrogen atom, or represent a halogen atom, a C1-6 alkyl group, or a C1-6 halo-substituted alkyl group; R3 and R4 represent hydrogen atom, a halogen atom, a C1-6 alkyl group, or a C1-6 halo-substituted alkyl group; and R5 and R6 represent a halogen atom, a C1-6 halo-substituted alkyl group, cyano group, nitro group, or the like), which is stable under the reaction conditions of the nucleic acid synthetic cycles and has little steric hindrance, and can be removed under mild conditions using fluoride ions as a base.
摘要翻译: 由下述通式(I)表示的保护基(与*相连的氧原子表示核糖核苷,2核苷酸或其衍生物的2'-羟基的氧原子; R1和R2均表示氢原子, 卤素原子,C 1-6烷基或C 1-6卤素取代的烷基; R 3和R 4表示氢原子,卤素原子,C 1-6烷基或C 1-6卤素取代的烷基; R5和R6表示卤素原子,C1-6卤代烷基,氰基,硝基等),其在核酸合成循环的反应条件下是稳定的,几乎没有空间位阻, 可以在温和条件下使用氟离子作为基底去除。
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公开(公告)号:US20110294124A1
公开(公告)日:2011-12-01
申请号:US13131591
申请日:2009-12-02
申请人: Takeshi Wada , Mamoru Shimizu
发明人: Takeshi Wada , Mamoru Shimizu
摘要: Described herein are methods of syntheses of phosphorous atom-modified nucleic acids comprising chiral X-phosphonate moieties. The methods described herein provide backbone-modified nucleic acids in high diasteteomeric purity via an asymmetric reaction of an achiral molecule comprising a chemically stable H-phophonate moiety with a nucleoside/nucleotide.
摘要翻译: 本文描述了合成包含手性X-膦酸酯部分的磷原子修饰的核酸的方法。 本文描述的方法通过包含化学稳定的H-膦酸酯部分与核苷/核苷酸的非手性分子的不对称反应提供具有高度对映纯度的骨架修饰的核酸。
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公开(公告)号:US20130178612A1
公开(公告)日:2013-07-11
申请号:US13825627
申请日:2011-09-22
申请人: Takeshi Wada , Mamoru Shimizu
发明人: Takeshi Wada , Mamoru Shimizu
IPC分类号: C07D207/12 , C07D211/42 , C07D221/18 , C07D209/62 , C07D211/62 , C07H21/04 , C07H21/02 , C07H1/00 , C07D207/16 , C07D217/24 , C07D221/10
CPC分类号: C07D207/12 , C07D207/16 , C07D209/62 , C07D211/42 , C07D211/44 , C07D211/62 , C07D217/24 , C07D221/10 , C07D221/18 , C07H1/00 , C07H19/06 , C07H19/16 , C07H21/00 , C07H21/02 , C07H21/04
摘要: Chiral auxiliaries useful for efficiently producing a phosphorus atom-modified nucleic acid derivative with high stereoregularity, and compounds represented by the following the general formula (I) or the general formula (XI) for introducing the chiral auxiliaries.
摘要翻译: 用于有效生产具有高立构规整性的磷原子修饰的核酸衍生物的手性助剂,以及用于引入手性助剂的由通式(I)或通式(XI)表示的化合物。
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公开(公告)号:US10428019B2
公开(公告)日:2019-10-01
申请号:US13825627
申请日:2011-09-22
申请人: Takeshi Wada , Mamoru Shimizu
发明人: Takeshi Wada , Mamoru Shimizu
IPC分类号: C07H21/02 , C07H21/00 , C07H19/00 , C07H19/04 , C07H19/20 , C07D221/06 , C07D217/22 , C07D211/56 , C07D211/40 , C07D221/18 , C07D209/56 , C09B7/02 , C07D207/12 , C07D207/16 , C07D211/44 , C07D211/62 , C07D217/24 , C07H19/06 , C07H19/16 , C07D209/62 , C07D211/42 , C07D221/10 , C07H1/00 , C07H21/04
摘要: The disclosed and claimed compounds are chiral auxiliaries useful for efficiently producing a phosphorus atom-modified nucleic acid derivative with high stereoregularity. The disclosed and claimed compounds include those represented by the following formula (I) or formula (XI) for introducing the chiral auxiliaries.
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公开(公告)号:US09394333B2
公开(公告)日:2016-07-19
申请号:US13131591
申请日:2009-12-02
申请人: Takeshi Wada , Mamoru Shimizu
发明人: Takeshi Wada , Mamoru Shimizu
摘要: Described herein are methods of syntheses of phosphorous atom-modified nucleic acids comprising chiral X-phosphonate moieties. The methods described herein provide backbone-modified nucleic acids in high diasteteomeric purity via an asymmetric reaction of an achiral molecule comprising a chemically stable H-phophonate moiety with a nucleoside/nucleotide.
摘要翻译: 本文描述了合成包含手性X-膦酸酯部分的磷原子修饰的核酸的方法。 本文描述的方法通过包含化学稳定的H-膦酸酯部分与核苷/核苷酸的非手性分子的不对称反应提供具有高度对映纯度的骨架修饰的核酸。
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公开(公告)号:US09279186B2
公开(公告)日:2016-03-08
申请号:US13574854
申请日:2010-10-22
申请人: Hidemi Kato , Takeshi Wada , Kunio Yubuta , Akihisa Inoue
发明人: Hidemi Kato , Takeshi Wada , Kunio Yubuta , Akihisa Inoue
CPC分类号: C23C26/02 , B22F2998/00 , C22B9/02 , C22B26/22 , C23F1/00 , C23F4/04 , Y02P10/234 , Y10T428/12479 , C22C1/0425 , C22C1/0433 , C22C33/02
摘要: A metallic material containing both a second constituent and a third constituent having positive and negative heats of mixing relative to a first constituent, respectively, and including a compound, an alloy or a nonequilibrium alloy having a melting point that is higher than the solidifying point of a metal bath made of the first constituent is placed in the metal bath. The metal bath is controlled to a temperature lower than a minimum value of a liquidus temperature within a range of compositional variations in which the amount of the third constituent in the metallic material decreases down to a point where the metallic material becomes substantially the second constituent so that the third constituent is selectively dissolved into the metal bath.
摘要翻译: 一种含有第二成分和第三成分的金属材料,分别具有相对于第一成分的正和负的混合热,并且包括熔点高于凝固点的化合物,合金或非平衡合金 将由第一成分制成的金属浴放置在金属浴中。 将金属浴控制在低于液相线温度的最小值的温度范围内,其中金属材料中的第三成分的量减少到金属材料基本上变成第二成分的程度 第三组分选择性地溶解到金属浴中。
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公开(公告)号:US08859755B2
公开(公告)日:2014-10-14
申请号:US13582531
申请日:2011-03-04
申请人: Takeshi Wada , Yohei Nukaga
发明人: Takeshi Wada , Yohei Nukaga
摘要: A method for preparing a phosphorothioate RNA based on the oxazaphospholidine method, wherein cyanoethoxymethyl group is used instead of tert-butyldimethylsilyl group as a protective group of 2′-hydroxyl group of RNA.
摘要翻译: 基于氧氮杂磷烷基方法制备硫代磷酸酯RNA的方法,其中使用氰基乙氧基甲基代替叔丁基二甲基甲硅烷基作为RNA的2'-羟基的保护基。
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公开(公告)号:US20120320623A1
公开(公告)日:2012-12-20
申请号:US13581381
申请日:2011-03-01
申请人: Takeshi Wada
发明人: Takeshi Wada
IPC分类号: F21V8/00
CPC分类号: G02F1/133615 , G02B6/0088 , G02B6/009
摘要: An illuminating device includes a light guide plate; a light source that is located opposite at least two adjacent end faces of four end faces of the light guide plate; and a chassis that has an opening through which light emanating from a light emission surface of the light guide plate passes. At least one optical sheet that includes a corner portion with an interior angle of greater than 90 degrees in a position corresponding to a corner portion of the light guide plate that is sandwiched between the two end faces opposite the light source is disposed between the light emission surface of the light guide plate and the chassis.
摘要翻译: 照明装置包括导光板; 光源,其与所述导光板的四个端面的至少两个相邻的端面相对; 以及具有从导光板的发光面发出的光通过的开口的底架。 至少一个光学片包括在对应于导光板的夹在与光源相对的两个端面之间的导光板的角部的位置处具有大于90度的内角的角部, 导光板和底盘的表面。
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