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公开(公告)号:US10919928B2
公开(公告)日:2021-02-16
申请号:US16009533
申请日:2018-06-15
申请人: AJINOMOTO CO., INC.
发明人: Kunihiro Hirai , Satoshi Katayama , Naoko Hirose , Taisuke Ichimaru , Ken Yamashita , Daisuke Takahashi
IPC分类号: C07H21/02 , C07H21/04 , C12N15/09 , C07H19/167 , C07H19/20 , C07H1/00 , C07H19/10 , C07H21/00 , C07H19/073 , C07H19/173 , C07H19/067
摘要: Oligonucleotides may be produced by a process, including (1) condensing a nucleoside, nucleotide or oligonucleotide (b), and a nucleoside, nucleotide or oligonucleotide (a), or a substituted nucleotide or oligonucleotide (α) in a non-polar solvent to give a reaction solution containing a phosphite triester product (c); (3) oxidizing or sulfurizing the phosphite triester product (c) to give a reaction solution containing an oligonucleotide (d) wherein the 5′-hydroxy group is protected; (4) deprotecting the oligonucleotide (d) to give a reaction solution containing an oligonucleotide (e) wherein the 5′-hydroxy group is not protected; and (6) adding a polar solvent to the reaction solution containing the oligonucleotide (e) and purifying the oligonucleotide (e) by solid-liquid separation, wherein said nucleoside, nucleotide or oligonucleotide (a) or said substituted nucleotide or oligonucleotide (α) is a compound represented by formula (a-i): wherein Base, Rp1, R10, m, L, Y, and Z are defined herein.
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公开(公告)号:US20220348602A1
公开(公告)日:2022-11-03
申请号:US17608802
申请日:2020-05-08
发明人: Xianglin Shi , William F. Kiesman , Firoz Antia , Yannick Fillon , Xuan Zhou , Wuming Yan , Hong Jiang , Hien Nguyen , Robert S. Gronke , Taisuke Ichimaru , Takuya Hamagaki , Daisuke Takahashi
摘要: The present disclosure describes a convergent liquid phase process for manufacturing oligonucleotides by coupling two or more oligonucleotide fragments, each of which have two or more nucleotides. Also provided by the present disclosure are reaction steps involved the convergent liquid phase process.
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公开(公告)号:US09227949B2
公开(公告)日:2016-01-05
申请号:US14567506
申请日:2014-12-11
申请人: AJINOMOTO CO., INC.
发明人: Takahiro Koshiba , Munetaka Tokumasu , Taisuke Ichimaru , Koji Ohsumi , Tadakiyo Nakagawa , Tatsuhiro Yamada , Kayo Matsumoto , Tamotsu Suzuki
IPC分类号: A61K31/38 , C07D319/12 , C07D333/38 , C07D409/06 , C07D409/12 , C07D333/40
CPC分类号: A61K31/381 , A61K31/19 , A61K31/396 , A61K31/397 , A61K31/4025 , A61K31/41 , A61K31/4436 , A61K31/4535 , A61K31/4725 , A61K38/05 , C07D319/12 , C07D333/38 , C07D333/40 , C07D409/06 , C07D409/12
摘要: Compounds represented by the following formula (I); wherein each symbol is as defined in the specification, are useful as hyperglycemic inhibitors having a serine protease inhibitory action and as prophylactic or therapeutic drugs for diabetes.
摘要翻译: 由下式(I)表示的化合物; 其中每个符号如说明书中所定义,可用作具有丝氨酸蛋白酶抑制作用的高血糖抑制剂和用作糖尿病的预防或治疗药物。
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公开(公告)号:US20180282365A1
公开(公告)日:2018-10-04
申请号:US16009533
申请日:2018-06-15
申请人: AJINOMOTO CO., INC.
发明人: Kunihiro HIRAI , Satoshi Katayama , Naoko Hirose , Taisuke Ichimaru , Ken Yamashita , Daisuke Takahashi
IPC分类号: C07H21/02
摘要: Oligonucleotides may be produced by a process, including (1) condensing a nucleoside, nucleotide or oligonucleotide (a) or the like wherein a 5′-hydroxy group is not protected and a nucleoside, nucleotide or oligonucleotide (b) wherein a 5′-hydroxy group is protected in a non-polar solvent to give a reaction solution containing a phosphite triester product (c); (3) oxidizing or sulfurizing the phosphite triester product (c) to give a reaction solution containing an oligonucleotide (d) wherein the 5′-hydroxy group is protected; (4) deprotecting the oligonucleotide (d) to give a reaction solution containing an oligonucleotide (e) wherein the 5′-hydroxy group is not protected; and (6) adding a polar solvent to the reaction solution containing the oligonucleotide (e) and purifying the oligonucleotide (e) by solid-liquid separation or extraction.
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公开(公告)号:US10464966B2
公开(公告)日:2019-11-05
申请号:US15655280
申请日:2017-07-20
申请人: AJINOMOTO CO., INC.
发明人: Kunihiro Hirai , Satoshi Katayama , Naoko Hirose , Ken Yamashita , Taisuke Ichimaru , Daisuke Takahashi
IPC分类号: C07K1/32 , C07H21/02 , C07K1/30 , C07H21/04 , C07H21/00 , C07H23/00 , C07F7/18 , C07C43/10 , C07C43/205 , C07C49/84 , C07C69/157 , C07C69/78 , C07C233/47 , C07D295/108 , C07C69/017 , C07C69/24 , C07C69/757 , C07C69/92 , C07C69/94 , C07C43/23
摘要: Precipitation promoters, which are an organic compound having one or more linear aliphatic hydrocarbon groups having not less than 10 carbon atoms, wherein the aliphatic hydrocarbon group has not less than 20 carbon atoms in total are useful for precipitating an organic compound protected by an organic group having one or more aliphatic hydrocarbon groups having not less than 10 carbon atoms from a solvent.
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公开(公告)号:US20180291056A1
公开(公告)日:2018-10-11
申请号:US16014536
申请日:2018-06-21
申请人: AJINOMOTO CO., INC.
发明人: Ken YAMASHITA , Kunihiro Hirai , Satoshi Katayama , Taisuke Ichimaru , Daisuke Takahashi , Naoko Hirose
IPC分类号: C07H21/04
摘要: The present invention aims to provide a more stable and efficient method for producing oligonucleotide, particularly, oligonucleotide having various functional groups linked to the 3′-terminal and the like. Efficient production of oligonucleotide becomes possible by a production method of an oligonucleotide represented by the formula (Ia-2) (each symbol is as defined in the DESCRIPTION) and having a functional group at the 3′-terminal, the method including a step of subjecting an oligonucleic acid with 3′-terminal protected by a silyl-protecting group to 3′-terminal-selective deprotection under desilylation conditions that do not affect protecting groups other than the silyl group, subjecting same to phosphitylation conditions with a phosphoramidite reagent that do not affect protecting groups on the oligonucleic acid to give a 3′-terminal-phosphoramidited oligonucleotide represented by the formula (Ia-1) (each symbol is as defined in the DESCRIPTION), and linking a functional group to the 3′-terminal of the 3′-terminal phosphoramidited oligonucleotide directly or via a linker, and the like.
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公开(公告)号:US20160058734A1
公开(公告)日:2016-03-03
申请号:US14934386
申请日:2015-11-06
申请人: AJINOMOTO CO., INC.
发明人: Takahiro KOSHIBA , Munetaka Tokumasu , Taisuke Ichimaru , Koji Ohsumi , Tadakiyo Nakagawa , Tatsuhiro Yamada , Kayo Matsumoto , Tamotsu Suzuki
IPC分类号: A61K31/381 , A61K31/4025 , A61K31/4535 , A61K38/05 , A61K31/397 , A61K31/4725 , A61K31/396 , A61K31/41 , A61K31/19 , A61K31/4436
CPC分类号: A61K31/381 , A61K31/19 , A61K31/396 , A61K31/397 , A61K31/4025 , A61K31/41 , A61K31/4436 , A61K31/4535 , A61K31/4725 , A61K38/05 , C07D319/12 , C07D333/38 , C07D333/40 , C07D409/06 , C07D409/12
摘要: Compounds represented by the following formula (I); wherein each symbol is as defined in the specification, are useful as hyperglycemic inhibitors having a serine protease inhibitory action and as prophylactic or therapeutic drugs for diabetes.
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