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    REAGENT FOR IMAGING INTRACELLULAR ACETYLATION
    1.
    发明申请
    REAGENT FOR IMAGING INTRACELLULAR ACETYLATION 审中-公开
    用于成像细胞内乙酰化的试剂

    公开(公告)号：US20150276751A1

    公开(公告)日：2015-10-01

    申请号：US14434270

    申请日：2013-10-10

    Applicant: JAPAN SCIENCE AND TECHNOLOGY AGENCY

    Inventor： Motomu Kanai ,  Hirokazu Komatsu

    IPC: G01N33/58 ,  C07D311/90

    CPC classification number: G01N33/582 ,  A61K49/0041 ,  C07D311/90 ,  C12Q1/48 ,  G01N2333/91051 ,  G01N2440/10

    Abstract: A reagent for imaging an advancing intracellular acetylation, for example, an acetylation that is advanced by the action of acetyl-CoA in the mitochondria, at high sensitivity and high efficiency, which comprises a combination of a rhodamine derivative that is substantially non-fluorescent before being acetylated, and emits strong fluorescence after being acetylated, and an acylation catalyst and/or an acylation reaction-promoting agent.

    Abstract translation: 用于成像前进的细胞内乙酰化的试剂，例如在线粒体中通过乙酰辅酶A的作用促进的乙酰化，其具有高灵敏度和高效率，其包括基本上不荧光的罗丹明衍生物的组合 乙酰化，乙酰化后发出强荧光，酰化催化剂和/或酰化反应促进剂。

    Curcumin-boron complex and pharmaceutical containing same
    3.
    发明授权
    Curcumin-boron complex and pharmaceutical containing same 审中-公开

    公开(公告)号：US10669287B2

    公开(公告)日：2020-06-02

    申请号：US16087017

    申请日：2017-03-21

    Applicant: JAPAN SCIENCE AND TECHNOLOGY AGENCY

    Inventor： Motomu Kanai ,  Yohei Soma ,  Jizhi Ni ,  Atsuhiko Taniguchi

    IPC: C07F5/02 ,  A61P25/16 ,  A61P25/28 ,  A61P3/10 ,  A61K31/69

    Abstract: Provided is a compound which is bioapplicable and amyloid-selective, and is useful as an amyloid oxygenation catalyst applicable not only to Aβ peptides but also to other amyloids, and a preventive/therapeutic drug for an amyloid-related disease using the same. A curcumin-boron complex represented by the following formula (1): wherein X1 and X2 are identical or different, and each represent a halogenoalkyl group or a halogen atom; X3 represents a bromine atom, an iodine atom, or a selenium atom; R1 and R2 are identical or different, and each represent a hydrogen atom or an optionally substituted alkyl group; R3 and R4 are identical or different, and each represent a hydrogen atom, a halogen atom, an alkoxy group, or an optionally substituted alkyl group, or R1 and R3 or R2 and R4 are optionally taken together to form an optionally substituted alkylene group or alkenylene group; R5 and R6 are identical or different, and each represent a hydrogen atom or an optionally substituted alkyl group; R7 and R8 are identical or different, and each represent a hydrogen atom, a halogen atom, an alkoxy group, or an optionally substituted alkyl group, or R5 and R7 or R6 and R8 are optionally taken together to form an optionally substituted alkylene group or alkenylene group; and m and n each represent an integer of 1 to 3, or a salt thereof.

    Bipyridyl compound
    4.
    发明授权
    Bipyridyl compound 有权

    公开(公告)号：US10280142B2

    公开(公告)日：2019-05-07

    申请号：US15819180

    申请日：2017-11-21

    Applicant: JAPAN SCIENCE AND TECHNOLOGY AGENCY

    Inventor： Yoichiro Kuninobu ,  Motomu Kanai ,  Haruka Ida ,  Mitsumi Nishi

    IPC: C07D213/53 ,  B01J31/22 ,  C07F15/00 ,  B01J31/18

    Abstract: There are provided a compound capable of being a novel ligand allowing regioselective borylation to be performed in the aromatic borylation reaction, and a catalyst using the same compound. There is provided a bipyridyl compound represented by a general formula (1): (wherein A represents a single bond, a vinylene group or an ethynylene group; X represents an oxygen atom or a sulfur atom; n pieces of R1 may be the same or different, and R1 represents a hydrogen atom, a halogen atom, an optionally substituted hydrocarbon group, an optionally substituted alkoxy group, an optionally substituted aryloxy group, an optionally substituted amino group, a cyano group, a nitro group, or an alkoxycarbonyl group, or two adjacent R1 may form a saturated or unsaturated ring structure optionally containing a hetero atom together with the carbon atoms bonded to the two R1; R2 represents a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted alkoxy group, or an optionally substituted aryloxy group; and n represents a number of 1 to 4).

    Amide compound and pharmaceutical comprising same
    5.
    发明授权
    Amide compound and pharmaceutical comprising same 有权

    公开(公告)号：US09796677B2

    公开(公告)日：2017-10-24

    申请号：US15100866

    申请日：2014-12-09

    Applicant: JAPAN SCIENCE AND TECHNOLOGY AGENCY

    Inventor： Motomu Kanai ,  Yohei Soma ,  Tadamasa Arai ,  Takushi Araya

    IPC: A61K31/44 ,  A61K31/505 ,  C07D213/81 ,  C07D239/28 ,  C07D239/30

    CPC classification number: C07D213/81 ,  C07D239/30

    Abstract: Provided is a novel compound which has an excellent Aβ aggregation inhibitory effect and is useful as a pharmaceutical. An amide compound represented by the formula (1) or a salt thereof, wherein Z represents CH or N; A and B are the same or different and each represents —CH2—, —O—, —S—, or —NH—; R1 and R2 are the same or different and each represents a branched alkyl group, a branched alkenyl group, an optionally substituted aromatic hydrocarbon group, an optionally substituted aralkyl group, an optionally substituted cycloalkyl group, or an optionally substituted aromatic heterocyclic group; and R3 represents a branched alkyl group, a branched alkenyl group, an optionally substituted cycloalkyl group, or an optionally substituted aralkyl group.

    Curcumin-boron complex and pharmaceutical containing same
    6.
    发明授权
    Curcumin-boron complex and pharmaceutical containing same 有权

    公开(公告)号：US10626128B2

    公开(公告)日：2020-04-21

    申请号：US16087017

    申请日：2017-03-21

    Applicant: JAPAN SCIENCE AND TECHNOLOGY AGENCY

    Inventor： Motomu Kanai ,  Yohei Soma ,  Jizhi Ni ,  Atsuhiko Taniguchi

    IPC: C07F5/02 ,  A61P25/16 ,  A61P25/28 ,  A61P3/10 ,  A61K31/69

    Abstract: Provided is a compound which is bioapplicable and amyloid-selective, and is useful as an amyloid oxygenation catalyst applicable not only to Aβ peptides but also to other amyloids, and a preventive/therapeutic drug for an amyloid-related disease using the same. A curcumin-boron complex represented by the following formula (1): wherein X1 and X2 are identical or different, and each represent a halogenoalkyl group or a halogen atom; X3 represents a bromine atom, an iodine atom, or a selenium atom; R1 and R2 are identical or different, and each represent a hydrogen atom or an optionally substituted alkyl group; R3 and R4 are identical or different, and each represent a hydrogen atom, a halogen atom, an alkoxy group, or an optionally substituted alkyl group, or R1 and R3 or R2 and R4 are optionally taken together to form an optionally substituted alkylene group or alkenylene group; R5 and R6 are identical or different, and each represent a hydrogen atom or an optionally substituted alkyl group; R7 and R8 are identical or different, and each represent a hydrogen atom, a halogen atom, an alkoxy group, or an optionally substituted alkyl group, or R5 and R7 or R6 and R8 are optionally taken together to form an optionally substituted alkylene group or alkenylene group; and m and n each represent an integer of 1 to 3, or a salt thereof.

    Curcumin-boron complex and pharmaceutical containing same
    7.
    发明授权
    Curcumin-boron complex and pharmaceutical containing same 有权

    公开(公告)号：US10526348B2

    公开(公告)日：2020-01-07

    申请号：US16087017

    申请日：2017-03-21

    Applicant: JAPAN SCIENCE AND TECHNOLOGY AGENCY

    Inventor： Motomu Kanai ,  Yohei Soma ,  Jizhi Ni ,  Atsuhiko Taniguchi

    IPC: C07F5/02 ,  A61P25/16 ,  A61P25/28 ,  A61P3/10 ,  A61K31/69

    Abstract: Provided is a compound which is bioapplicable and amyloid-selective, and is useful as an amyloid oxygenation catalyst applicable not only to Aβ peptides but also to other amyloids, and a preventive/therapeutic drug for an amyloid-related disease using the same. A curcumin-boron complex represented by the following formula (1): wherein X1 and X2 are identical or different, and each represent a halogenoalkyl group or a halogen atom; X3 represents a bromine atom, an iodine atom, or a selenium atom; R1 and R2 are identical or different, and each represent a hydrogen atom or an optionally substituted alkyl group; R3 and R4 are identical or different, and each represent a hydrogen atom, a halogen atom, an alkoxy group, or an optionally substituted alkyl group, or R1 and R3 or R2 and R4 are optionally taken together to form an optionally substituted alkylene group or alkenylene group; R5 and R6 are identical or different, and each represent a hydrogen atom or an optionally substituted alkyl group; R7 and R8 are identical or different, and each represent a hydrogen atom, a halogen atom, an alkoxy group, or an optionally substituted alkyl group, or R5 and R7 or R6 and R8 are optionally taken together to form an optionally substituted alkylene group or alkenylene group; and m and n each represent an integer of 1 to 3, or a salt thereof.

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