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公开(公告)号:US20180207197A1
公开(公告)日:2018-07-26
申请号:US15738224
申请日:2016-06-27
Applicant: Kyowa Hakko Kirin Co., Ltd.
Inventor: Junichiro YAMAMOTO , Takashi SAWADA , Kenji HAGIWARA , Toshiyuki ATSUMI , Fumikazu SHINOHARA
IPC: A61K31/7125 , C12N15/113 , A61K31/712
CPC classification number: A61K31/7125 , A61K31/712 , C07H21/00 , C12N15/113 , C12N2310/14
Abstract: The present invention provides an oligonucleotide derivative having, at an oxygen atom of at least one phosphate group of an oligonucleotide, a group represented by formula (I): (wherein R1 represents lower alkyl or the like; and R2 and R3 are the same or different and respectively represent an electron-withdrawing group or the like), or a salt thereof.
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公开(公告)号:US20170354673A1
公开(公告)日:2017-12-14
申请号:US15123438
申请日:2015-03-03
Applicant: Kyowa Hakko Kirin Co., Ltd.
Inventor: Fumikazu SHINOHARA , Asana MAKINO , Junichiro YAMAMOTO , Takahiro NAKAJIMA , Taiji OASHI , Michihiko SUZUKI , Jun-ichi SAITO , Tomoyuki NISHIKAWA , Masayoshi NAKOJI , Yuichi TAKAHASHI , Yasuo KOUDA
IPC: A61K31/7115 , C07H19/20 , C07H19/10 , C12N15/113
CPC classification number: A61K31/7115 , A61K31/5377 , A61K31/7076 , A61K31/713 , C07H19/06 , C07H19/10 , C07H19/16 , C07H19/167 , C07H19/173 , C07H19/20 , C07H21/00 , C07H23/00 , C12N15/111 , C12N15/113 , C12N2310/14 , C12N2310/32 , C12N2310/33 , C12N2320/31
Abstract: An oligonucleotide having a nucleotide residue or a nucleoside residue represented by formula (I) {wherein X1 is an oxygen atom or the like, R1 is formula (IIA) (wherein R5A is halogen or the like, and R6A is a hydrogen atom or the like), formula (IVA) (wherein Y3A is a nitrogen atom or the like, and Y4A is CH or the like), or the like, R2 is a hydrogen atom, hydroxy, halogen, or optionally substituted lower alkoxy, and R3 is a hydrogen atom or the like, or formula (VI) (wherein n2 is 1, 2 or 3)} at the 5′ end thereof, wherein the nucleotide residue or the nucleoside residue binds to an adjacent nucleotide residue through the oxygen atom at position 3, is provided.
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公开(公告)号:US20150376611A1
公开(公告)日:2015-12-31
申请号:US14423749
申请日:2013-09-02
Applicant: Kyowa Hakko Kirin Co., Ltd.
Inventor: Fumikazu SHINOHARA , Asana MAKINO , Junichiro YAMAMOTO , Taiji OASHI , Michihiko SUZUKI , Jun-ichi SAITO , Takahiro NAKAJIMA , Tomoyuki NISHIKAWA , Masayoshi NAKOJI , Yuichi TAKAHASHI
IPC: C12N15/113
CPC classification number: C12N15/113 , A61K31/713 , C07H21/02 , C12N15/111 , C12N2310/14 , C12N2310/32 , C12N2310/33 , C12N2320/50 , C12N2320/51 , C12N2330/30
Abstract: The present invention provides an oligonucleotide having improved affinity for AGO2, and the like. The oligonucleotide has a nucleotide residue or a nucleoside residue represented by formula (I) {wherein X1 is an oxygen atom or the like, R1 is formula (IIA) (wherein R5A is halogen or the like, and R6A is a hydrogen atom or the like) or formula (IVA) (wherein Y3A is a nitrogen atom or the like, and Y4A is CH or the like), or the like, R2 is a hydrogen atom, hydroxy, halogen, or optionally substituted lower alkoxy, and R3 is a hydrogen atom or the like} at the 5′ end thereof, and the nucleotide residue or the nucleoside residue binds to an adjacent nucleotide residue through the oxygen atom at position 3.
Abstract translation: 本发明提供了对AGO 2具有改善的亲和力的寡核苷酸等。 寡核苷酸具有由式(I)表示的核苷酸残基或核苷残基(其中X1是氧原子等,R1是式(ⅡA)(其中R5A是卤素等,R6A是氢原子或 (IVA)(式中,Y3A为氮原子等,Y4A为CH等)等,R2为氢原子,羟基,卤素或任意取代的低级烷氧基,R3为 氢原子等),核苷酸残基或核苷残基通过第3位的氧原子与相邻的核苷酸残基结合。
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公开(公告)号:US20140330004A1
公开(公告)日:2014-11-06
申请号:US13972128
申请日:2013-12-06
Applicant: Kyowa Hakko Kirin Co., Ltd.
Inventor: Fumikazu SHINOHARA , Asana MAKINO , Junichiro YAMAMOTO , Taiji OASHI , Michihiko SUZUKI , Jun-ichi SAITO
IPC: C12N15/113
CPC classification number: C12N15/113 , C12N2310/333
Abstract: An oligonucleotide, which has a nucleotide residue or a nucleoside residue represented by formula (I) at the 5′ end thereof, wherein the nucleotide residue or the nucleoside residue binds to an adjacent nucleotide residue via the oxygen atom at position 3, or the like; wherein X represents an oxygen atom or the like, R1 represents formula (II) wherein Y1 represents a nitrogen atom or the like, R5 represents halogen or the like, R6 and R7 may be the same or different, and each represents a hydrogen atom or the like, and R3 represents a hydrogen atom or the like.
Abstract translation: 在5'末端具有由式(I)表示的核苷酸残基或核苷残基的寡核苷酸,其中所述核苷酸残基或核苷残基经由位置3处的氧原子等与相邻核苷酸残基结合 ; 其中X表示氧原子等,R 1表示式(II),其中Y 1表示氮原子等,R 5表示卤素等,R 6和R 7可以相同或不同,表示氢原子或 并且R 3表示氢原子等。
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