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公开(公告)号：US20200172903A1
公开(公告)日：2020-06-04
申请号：US16616743
申请日：2018-07-03
发明人： Masayuki NAKAMORI , Hideki MOCHIZUKI , Satoshi OBIKA , Makoto KOIZUMI , Akifumi NAKAMURA , Kiyosumi TAKAISHI , Yumiko ASAHI
IPC分类号： C12N15/113 , A61P25/16 , A61P25/28
摘要： The objective of the present invention is to provide nucleic acid therapeutics which exhibits more excellent effect and which shows a substantivity for a prolonged period to suppress an expression of α-synuclein. The oligonucleotide or a pharmacologically acceptable salt thereof according to the present invention is characterized in comprising at least one 2′-O,4′-C-ethylene nucleoside, wherein the oligonucleotide can hybridize with α-synuclein gene, has an activity to suppress an expression of the α-synuclein gene, and is complementary to the α-synuclein gene, 5′ end of the oligonucleotide is a nucleotide complementary to the specific nucleotide, the oligonucleotide is complementary to at least a part of SEQ ID NO: 1, and the oligonucleotide has a length of 13 or more and 15 or less nucleotides.
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公开(公告)号：US20170044528A1
公开(公告)日：2017-02-16
申请号：US15118546
申请日：2015-02-17
申请人： OSAKA UNIVERSITY
发明人： Satoshi OBIKA , Takao YAMAGUCHI , Masahiko HORIBA , Reiko WAKI
IPC分类号： C12N15/113 , C07H19/16 , C07H19/06
CPC分类号： C12N15/113 , C07H19/06 , C07H19/16 , C07H21/00 , C12N2310/31
摘要： Disclosed are bridged nucleosides and nucleotides. The nucleosides of the present invention have a 2′,4′-bridged structure and are represented by formula I below: An oligonucleotide containing a 2′,4′-bridged artificial nucleotide of the present invention has a binding affinity for single-stranded RNA comparable to that of known 2′,4′-BNA/LNA and higher nuclease resistance than LNA. In particular, since the oligonucleotide has a much higher binding affinity for single-stranded RNA than S-oligo, it is expected that the oligonucleotide is applicable to nucleic acid drugs.
摘要翻译： 含有本发明的2'，4'-桥接人造核苷酸的寡核苷酸对于单链RNA具有与已知的2'，4'-BNA / LNA和比NNA更高的核酸酶抗性相当的结合亲和力。 特别是，由于寡核苷酸对单链RNA的结合亲和力高于S-寡聚体，所以预期该寡核苷酸适用于核酸药物。
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公开(公告)号：US20230113556A1
公开(公告)日：2023-04-13
申请号：US17907323
申请日：2021-03-26
发明人： Mariko SHIBA , Tsuyoshi YAMAMOTO , Fumito WADA , Tadayuki KOBAYASHI , Keisuke TACHIBANA , Satoshi OBIKA
IPC分类号： C12N15/113 , A61P3/06
摘要： The present invention provides an antisense oligomer having the base sequence depicted in SEQ ID NO: 26, an antisense oligomer having a base sequence resulting from substitution, deletion, insertion, or addition of 1 to 6 bases in the base sequence depicted in SEQ ID NO: 26, a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable hydrate thereof, an oligonucleotide conjugate in which the antisense oligomer is bound with a molecule capable of binding to an asialoglycoprotein receptor, and a pharmaceutical composition containing the same.
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公开(公告)号：US20190008886A1
公开(公告)日：2019-01-10
申请号：US16068163
申请日：2017-01-05
申请人： OSAKA UNIVERSITY , NATIONAL UNIVERSITY CORPORATION TOKYO MEDICAL AND DENTAL UNIVERSITY , NATIONAL INSTITUTES OF BIOMEDICAL INNOVATION, HEALTH AND NUTRITION
发明人： Masayuki NAKAMORI , Hideki MOCHIZUKI , Satoshi OBIKA , Takanori YOKOTA , Tetuya NAGATA , Yuya KASAHARA
IPC分类号： A61K31/712 , C12N15/113 , C07K14/47 , A61P25/28 , A61P25/16
摘要： The present invention can provide a nucleic acid medicine which has a higher effect and a more prolonged effect of inhibiting the expression of α-synudein can be provided. Disclosed is the oligonucleotide or a pharmacologically acceptable salt thereof, the oligonucleotide containing at least one nucleoside structure represented by Formula (I): (where each of Base and A are defined substituent or structure), can bind to an α-synudein gene, has activity for inhibiting expression of the α-synudein gene, and is complementary to the α-synudein gene, and the oligonucleotide has a length of twelve to twenty bases.
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公开(公告)号：US20220177509A1
公开(公告)日：2022-06-09
申请号：US17601326
申请日：2020-03-31
发明人： Takeshi BABA , Hiroshi OKAMOTO , Yumi NOMURA , Satoshi OBIKA , Takao YAMAGUCHI
摘要： Provided is a method for producing a compound represented by formula (III) from a compound represented by formula (I) as a starting material.
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公开(公告)号：US20220127300A1
公开(公告)日：2022-04-28
申请号：US17428998
申请日：2020-02-10
申请人： Osaka University
发明人： Satoshi OBIKA , Takao YAMAGUCHI , Takaki HABUCHI , Go KATO , Takao INOUE , Tokuyuki YOSHIDA , Md Ariful ISLAM
IPC分类号： C07H21/04
摘要： Disclosed are a 5′-modified nucleoside and a nucleotide using the same. The nucleoside of the present invention is represented by the formula (I) below. The 5′-modified nucleoside of the present invention is usable as a substitute for a phosphorothioate-modified nucleic acid, which has a risk of, for example, accumulation in a specific organ. The 5′-modified nucleoside also has excellent industrial productivity because a diastereomer separation step is not involved in the production process thereof.
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公开(公告)号：US20220002336A1
公开(公告)日：2022-01-06
申请号：US17292963
申请日：2019-11-11
发明人： Hiroaki SAWAMOTO , Shinji KUMAGAI , Hiroyuki FURUKAWA , Tomo ARAKI , Masayuki UTSUGI , Satoshi OBIKA
摘要： The present invention provides a novel bridged artificial nucleic acid and an oligomer containing the same as a monomer. The present invention provides specifically a compound represented by general formula (I) (wherein each symbol is the same as defined in the specification) or salts thereof; as well as an oligonucleotide compound represented by general formula (I′) (wherein each symbol is the same as defined in the specification) or salts thereof.
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公开(公告)号：US20180251488A1
公开(公告)日：2018-09-06
申请号：US15760513
申请日：2016-09-20
发明人： Satoshi OBIKA , Eiji KAWANISHI , Hiroaki SAWAMOTO , Shuhei YAMAKOSHI , Yuuki ARAI , Shinji KUMAGAI
CPC分类号： C07H19/06 , C07C279/16 , C07D498/04 , C07D498/08 , C07H1/00 , C07H9/06 , C07H19/16 , C07H21/00
摘要： The present invention provides a method for producing guanidine crosslinked artificial nucleic acid (abbreviated hereinafter as GuNA), and an intermediate compound for the production thereof. Specifically, the present invention provides a method for producing a compound represented by general formula I: (in the formula, R1, R2, R3, R4, R5, R6, m and ring A are as defined in the specification) or a salt thereof wherein a reducing agent is reacted with a compound represented by general formula II: (in the formula, R1, R2, R3, R4, R5, R6, m, and ring A′ are as defined in the specification).
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公开(公告)号：US20220372060A1
公开(公告)日：2022-11-24
申请号：US17427134
申请日：2020-01-31
申请人： Osaka University
发明人： Satoshi OBIKA , Takao YAMAGUCHI , Takaki HABUCHI , Go KATO , Takao INOUE , Tokuyuki YOSHIDA , Takaya SUGIURA
摘要： Disclosed are a 5′-modified nucleoside and a nucleotide using the same. The nucleoside of the present invention is represented by the formula (I) below. The 5′-modified nucleoside of the present invention is usable as a substitute for a phosphorothioate-modified nucleic acid, which has a risk of, for example, accumulation in a specific organ. The 5′-modified nucleoside also has excellent industrial productivity because a diastereomer separation step is not involved in the production process thereof.
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公开(公告)号：US20220169671A1
公开(公告)日：2022-06-02
申请号：US17667988
申请日：2022-02-09
申请人： Osaka University
发明人： Satoshi OBIKA , Kosuke ITO , Takaki HABUCHI , Masahiko HORIBA
IPC分类号： C07H19/10 , C07H21/02 , C12N15/113
摘要： The present invention aims to provide a nucleic acid compound that hardly forms non-Watson-Crick base pairs, and an oligonucleotide containing the nucleic acid compound and showing reduced non-specific binding with nucleic acids other than the target nucleic acid. The nucleic acid compound according to the present invention is characterized in that the 2-position carbonyl group of the pyrimidine base is functionally converted (X1 and X2 are each independently S or Se), and that the 2′-position and the 4′-position are bridged in a particular structure. The oligonucleotide according to the present invention is characterized in that at least one of thymidine and uridine is the nucleic acid compound.
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