公开(公告)号：US20230124641A1

公开(公告)日：2023-04-20

申请号：US17800339

申请日：2021-02-17

Applicant: Osaka University ,  Japan as Represented by Director General of National Institute of health Sciences

Inventor： Satoshi OBIKA ,  Takao YAMAGUCHI ,  Yota SAKURAI ,  Chika YAMAMOTO ,  Kei SUGITA ,  Takao INOUE ,  Tokuyuki YOSHIDA

IPC: C07D493/08 ,  C07H21/04 ,  C07D239/10

Abstract: A cross-linked nucleoside of the present invention is a compound represented by the formula (I) below. The cross-linked 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 cross-linked nucleoside also has excellent industrial productivity.

公开(公告)号：US20220170020A1

公开(公告)日：2022-06-02

申请号：US17666341

申请日：2022-02-07

Applicant: Osaka University

Inventor： Satoshi OBIKA ,  Reiko WAKI ,  Takao INOUE ,  Tokuyuki YOSHIDA ,  Kunihiko MORIHIRO ,  Yuya KASAHARA ,  Atsushi MIKAMI

IPC: C12N15/113 ,  A61K31/7115 ,  A61K31/712

Abstract: The present invention aims to provide an antisense oligonucleic acid with reduced hepatotoxicity. The antisense oligonucleic acid according to the present invention is characterized in that it has a base length of not less than 7 nt and not more than 30 nt, wherein nucleic acid residues of not less than 1 nt and not more than 5 nt respectively from the both terminals are 2′,4′-bridged nucleic acids, 2′,4′-non-bridged nucleic acid residue(s) is(are) present between the above-mentioned both terminals, and one or more bases in the nucleic acid residue(s) of the above-mentioned 2′,4′-non-bridged nucleic acid residue(s) is/are modified.

公开(公告)号：US20210277398A1

公开(公告)日：2021-09-09

申请号：US17261653

申请日：2019-07-31

Applicant: Osaka University ,  National Institutes of Biomedical Innovation, Health and Nutrition ,  Luxna Biotech Co., Ltd.

Inventor： Masahito SHIMOJO ,  Satoshi OBIKA ,  Yuya KASAHARA ,  Takao SUZUKI ,  Masaki YAMAGAMI ,  Tadashi UMEMOTO

IPC: C12N15/113

Abstract: Disclosed is an oligonucleotide or a pharmacologically acceptable salt thereof, wherein the oligonucleotide comprises at least one defined nucleoside structure, can bind to a human nSR100 gene and has human nSR100 expression inhibiting activity. The oligonucleotide has a length of 12 to 20 mer, and is complementary to a defined target region. Further, disclosed is an nSR100 gene expression inhibitor and a cancer therapeutic agent containing the oligonucleotide or the pharmacologically acceptable salt thereof. The cancer therapeutic agent is used for treatment of small cell lung cancer, prostate cancer, or breast cancer.

公开(公告)号：US20160130583A1

公开(公告)日：2016-05-12

申请号：US14898630

申请日：2014-06-16

Applicant: NATIONAL UNIVERSITY CORPORATION TOKYO MEDICAL AND DENTAL UNIVERSITY ,  OSAKA UNIVERSITY

Inventor： Takanori YOKOTA ,  Kazutaka NISHINA ,  Kotaro YOSHIOKA ,  Satoshi OBIKA ,  Takenori SHIMO

IPC: C12N15/113

CPC classification number: C12N15/113 ,  A61K31/713 ,  C12N2310/11 ,  C12N2310/315 ,  C12N2310/3231 ,  C12N2310/341 ,  C12N2310/351 ,  C12N2310/3513 ,  C12N2310/533 ,  C12N2320/33 ,  C12N2310/321 ,  C12N2310/3521

Abstract: Disclosed are double-stranded antisense nucleic acid complexes that can efficiently alter the processing of RNA in a cell via an antisense effect, and methods for using the same. One method comprises contacting with the cell a double-stranded nucleic acid complex comprising: a first nucleic acid strand annealed to a second nucleic acid strand, wherein: the first nucleic acid strand comprises (i) nucleotides independently selected from natural DNA nucleotides, modified DNA nucleotides, and nucleotide analogs, (ii) no regions that have 4 or more consecutive natural DNA nucleotides, (iii) the total number of natural DNA nucleotides, modified DNA nucleotides, and nucleotide analogs in the first nucleic acid strand is from 8 to 100, and (iv) the first nucleic acid strand is capable of hybridizing to RNA inside of the cell; and the second nucleic acid strand comprises nucleotides independently selected from natural RNA nucleotides, modified RNA nucleotides, and nucleotide analogs.

Abstract translation: 公开了可以通过反义效应有效地改变细胞中RNA的加工的双链反义核酸复合物及其使用方法。 一种方法包括与细胞接触双链核酸复合物，其包含：退火至第二核酸链的第一核酸链，其中：所述第一核酸链包含（i）独立地选自天然DNA核苷酸，经修饰的DNA 核苷酸和核苷酸类似物，（ii）没有具有4个或更多个连续天然DNA核苷酸的区域，（iii）第一个核酸链中天然DNA核苷酸，修饰的DNA核苷酸和核苷酸类似物的总数为8至100个 ，和（iv）第一核酸链能够与细胞内的RNA杂交; 并且第二核酸链包含独立地选自天然RNA核苷酸，修饰的RNA核苷酸和核苷酸类似物的核苷酸。

公开(公告)号：US20150337002A1

公开(公告)日：2015-11-26

申请号：US14759099

申请日：2014-01-14

Applicant: OSAKA UNIVERSITY ,  SHIONOGI & CO., LTD.

Inventor： Satoshi OBIKA ,  Yasunori MITSUOKA

IPC: C07H19/10 ,  C07H19/20

CPC classification number: C07H19/067 ,  C07H19/06 ,  C07H19/10 ,  C07H19/16 ,  C07H19/167 ,  C07H19/20 ,  C07H21/04 ,  Y02P20/55

Abstract: The present invention provides compounds shown by the formula: wherein Y1-Y2 is S(═O)2—NR6, NR6—S(═O)2 or the like, R6 is a hydrogen atom, substituted or unsubstituted alkyl or the like, Bx is a nucleic acid base moiety, Z1 and Z2 are each independently, a hydrogen atom, a hydroxyl protecting group or a reactive phosphorus group, R1 to R5 are each independently, a hydrogen atom, halogen, cyano, substituted or unsubstituted alkyl or the like, and n is an integer of 0 to 3, or salts thereof, that are novel nucleosides or nucleotides that can be useful as materials for synthesizing nucleic acid pharmaceuticals.

Abstract translation: 本发明提供下式所示的化合物：其中Y1-Y2是S（= O）2-NR6，NR6-S（= O）2等，R6是氢原子，取代或未取代的烷基等， Bx是核酸碱基部分，Z1和Z2各自独立地为氢原子，羟基保护基或反应性磷基，R1至R5各自独立地为氢原子，卤素，氰基，取代或未取代的烷基或 类似，n为0〜3的整数，或其盐，其可用作合成核酸药物的材料的新型核苷或核苷酸。