公开(公告)号：US09745275B2

公开(公告)日：2017-08-29

申请号：US15105985

申请日：2014-12-18

Applicant: KYOTO UNIVERSITY ,  KAGOSHIMA UNIVERSITY

Inventor： Masatoshi Hagiwara ,  Masayasu Toyomoto ,  Takamitsu Hosoya ,  Suguru Yoshida ,  Takashi Kurihara

IPC: A61K31/428 ,  C07D277/64

CPC classification number: C07D277/64

Abstract: Provided is a pain-related compound, a pain-related pharmaceutical composition, and use of the same. Provided in one or more embodiments is a compound represented by Formula (I), a prodrug of the same, or a pharmaceutically permissible salt of any of the same.

公开(公告)号：US20150133467A1

公开(公告)日：2015-05-14

申请号：US14406101

申请日：2013-06-06

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

Inventor： Masatoshi Hagiwara ,  lsao Kii ,  Takamitsu Hosoya ,  Yuto Sumida ,  Suguru Yoshida

IPC: A61K31/496

CPC classification number: A61K31/496 ,  A61K31/426 ,  A61K31/437 ,  A61K31/495 ,  A61K31/695 ,  C07D213/83 ,  C07D277/20 ,  C07D277/36 ,  C07D471/04

Abstract: Provided is a screening method with which it is possible to determine the cause of a decrease or an increase in the amount of a target protein that is expressed by a cell. One or a plurality of embodiments include: conducting cultivation that includes bringing an assay cell into contact with a test substance, and measuring a relative amount (A) of the target protein in relation to an internal standard; conducting cultivation in which an assay cell is not brought into contact with a test substance, and measuring a relative amount (B) in relation to an internal standard; comparing the relative amount (A) and the relative amount (B); and, based on the comparison, selecting a candidate substance that induces instability and/or stability in the target protein. The assay cell is a cell that is able to express mRNA of the target protein and mRNA of the internal standard protein under the identical regulation of gene expression, or a cell having a means for expressing mRNA of the target protein and mRNA of the internal standard protein under the identical regulation of gene expression.

Abstract translation: 提供了可以确定由细胞表达的靶蛋白的量的减少或增加的原因的筛选方法。 一个或多个实施方案包括：进行培养，其包括使测定细胞与测试物质接触，并测量靶蛋白相对于内标的相对量（A）; 进行培养，其中测定细胞不与测试物质接触，并测量相对于内标的相对量（B）; 比较相对量（A）和相对量（B）; 并且基于比较，选择诱导靶蛋白的不稳定性和/或稳定性的候选物质。 测定细胞是能够在基因表达相同调节下表达内标蛋白的靶蛋白和mRNA的mRNA的细胞，或具有​​表达靶蛋白的mRNA和内标的mRNA的方法的细胞 蛋白质在相同的基因表达调控下。

公开(公告)号：US09879014B2

公开(公告)日：2018-01-30

申请号：US14904609

申请日：2014-07-14

Applicant: KYOTO UNIVERSITY

Inventor： Masatoshi Hagiwara ,  Suguru Yoshida ,  Takamitsu Hosoya

IPC: C07D473/40 ,  C12Q1/68 ,  A61K31/52

CPC classification number: C07D473/40 ,  A61K31/52 ,  C12Q1/6897 ,  C12Q2600/136

Abstract: A compound and a pharmaceutical composition for disease associated with an abnormal splice variant, use of the compound and the pharmaceutical composition, or a screening method of the compound and the pharmaceutical composition are provided. One or more embodiments disclose a compound expressed by the following formula (I) or (I′) or prodrugs or pharmaceutically acceptable salts thereof. Another one or more embodiments disclose a screening method using a DNA construct that is fused, arranged, or constructed so as to express different reporter genes for a wild-type splice variant and an abnormal splice variant that contributes to the development or progression of disease;

公开(公告)号：US11318126B2

公开(公告)日：2022-05-03

申请号：US16329063

申请日：2017-08-31

Applicant: KYOTO UNIVERSITY

Inventor： Masatoshi Hagiwara ,  Akiko Kobayashi ,  Takamitsu Hosoya ,  Suguru Yoshida ,  Yuto Sumida

IPC: A61K31/47 ,  A61K31/443 ,  A61P43/00 ,  A61P25/24 ,  A61K31/4709 ,  A61P25/16 ,  A61K45/00 ,  A61P25/14 ,  A61P25/02 ,  A61K31/4439 ,  A61K31/4725 ,  A61P25/28 ,  A61P25/00 ,  A61K31/416 ,  C12N5/0793

Abstract: Provided is a composition for activating neurogenesis, use of the composition, and a method for preventing, improving, inhibiting the development of, and/or treating a disease or the like of the central nervous system and or the peripheral nervous system using the composition. A composition for activating neurogenesis contains, as an active ingredient, a compound having an ability to inhibit phosphorylation activity of a protein kinase or a prodrug thereof, or a pharmaceutically acceptable salt thereof, and a composition for preventing, improving, inhibiting the development of, and/or treating a disease of the central nervous system and/or the peripheral nervous system, or for improving, inhibiting the development of, and/or treating a functional disorder of the central nervous system and/or the peripheral nervous system, the composition containing, as an active ingredient, a compound having an ability to inhibit phosphorylation activity of a protein kinase or a prodrug thereof, or a pharmaceutically acceptable salt thereof.