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    FLUORESCENT PROBE FOR USE IN DETECTION OF BRAIN TUMOR
    3.
    发明申请
    FLUORESCENT PROBE FOR USE IN DETECTION OF BRAIN TUMOR 有权

    公开(公告)号：US20220341922A1

    公开(公告)日：2022-10-27

    申请号：US17612378

    申请日：2020-05-19

    Applicant: The University of Tokyo

    Inventor： Yosuke KITAGAWA ,  Shota TANAKA ,  Nobuhito SAITO ,  Yugo KURIKI ,  Mako KAMIYA ,  Yasuteru URANO

    IPC: G01N33/533 ,  C07K5/06 ,  C09B11/24 ,  G01N33/574

    Abstract: Provided is a novel fluorescent probe which can be used in a spray manner, has an outstandingly high sensitivity-specificity with instantaneousness, and enables detection of a brain tumor.
    A fluorescent probe for detecting a brain tumor, including a compound of the following formula (I) or a salt thereof: wherein P1 represents an arginine residue, a histidine residue or a tyrosine residue, P2 represents a proline residue or a glycine residue, where P1 is linked to an adjacent N atom by forming an amide bond, and P2 is linked to P1 by forming an amide bond; R1 represents a hydrogen atom, or 1 to 4 identical or different substituents each independently selected from the group consisting of an optionally substituted alkyl group, a carboxyl group, an ester group, an alkoxy group, an amide group and an azide group; R2, R3, R4, R5, R6 and R7 each independently represent a hydrogen atom, a hydroxyl group, an optionally substituted alkyl group or a halogen atom; R8 and R9 each independently represent a hydrogen atom or an alkyl group;
    X represents O, Si(Ra)(Rb), Ge(Ra)(Rb), Sn(Ra)(Rb), C(Ra) (Rb) or P(═O)(Ra); Ra and Rb each independently represent a hydrogen atom, an alkyl group or an aryl group; and Y represents a C1-C3 alkylene group.

    SUPER-RESOLUTION FLUORESCENT IMAGING PROBE
    4.
    发明申请
    SUPER-RESOLUTION FLUORESCENT IMAGING PROBE 审中-公开

    公开(公告)号：US20180052109A1

    公开(公告)日：2018-02-22

    申请号：US15551149

    申请日：2016-02-23

    Applicant: The University of Tokyo

    Inventor： Yasuteru URANO ,  Mako KAMIYA ,  Akihiko MOROZUMI ,  Shinnosuke UNO ,  Keitaro UMEZAWA

    IPC: G01N21/64 ,  A61K49/00 ,  C09K11/06

    CPC classification number: G01N21/6458 ,  A61K49/0019 ,  A61K49/005 ,  C09K11/06 ,  C09K2211/1007 ,  C09K2211/1011 ,  C09K2211/1029 ,  C09K2211/1074 ,  C09K2211/1096 ,  G01N21/6428 ,  G01N33/533 ,  G01N33/68 ,  G01N2021/6439 ,  G02B21/0076 ,  G02B27/58

    Abstract: [Problem] To provide a novel fluorescent probe for super-resolution imaging that uses fluorescent light emission characteristics that originate from an intermolecular nucleophilic addition-dissociation equilibrium reaction, and to provide a super-resolution fluorescent imaging method that uses the probe. [Solution] A fluorescent probe for super-resolution imaging that comprises a compound represented by formula (I) or a salt thereof(in the formula, X represents an oxygen atom, C(Ra) (Rb), or Si(Ra) (Rb) (wherein Ra and Rb each independently represent a hydrogen atom or an alkyl group), R1 represents a hydrogen atom or an optionally substituted aryl (provided that, if R1 is a phenyl group, the benzene ring of the phenyl group does not have a substituent at position 2 or position 6), R2 and R3 each independently represent 1-3 identical or differing substituents that are independently selected from the group that consists of hydrogen atoms, hydroxyl groups, halogen atoms, optionally substituted alkyl groups, optionally substituted sulfo groups, optionally substituted carboxyl groups, optionally substituted ester groups, optionally substituted amide groups, and optionally substituted azide groups, R4 and R5 each independently represent a hydrogen atom or an optionally substituted alkyl group or N(R4) (R5) forms an amide group or a carbamate group (provided that, if R4 or R5 is an alkyl group, each may form, together with R2, a ring structure that contains the nitrogen atom that is bonded thereto), and R6 and R7 each independently represent a hydrogen atom or an optionally substituted alkyl group or N(R6)(R7) forms an amide group or a carbamate group (provided that, if R6 or R7 is an alkyl group, each may form, together with R3, a ring structure that contains the nitrogen atom that is bonded thereto)), the fluorescent probe for super-resolution imaging being characterized in that the compound represented by formula (I) or the salt thereof undergoes a nucleophilic addition-dissociation equilibrium reaction with a nucleophilic compound that contains an —SH group.

    ENZYME-SPECIFIC FLUORESCENT COMPOUND CAPABLE OF BEING RETAINED IN CELLS
    5.
    发明申请
    ENZYME-SPECIFIC FLUORESCENT COMPOUND CAPABLE OF BEING RETAINED IN CELLS 有权
    在细胞中保留的酶特异性荧光化合物

    公开(公告)号：US20170073321A1

    公开(公告)日：2017-03-16

    申请号：US15310641

    申请日：2015-05-13

    Applicant: The University of Tokyo

    Inventor： Yasuteru URANO ,  Mako KAMIYA ,  Tomohiro DOURA

    IPC: C07D311/04 ,  C12Q1/40

    CPC classification number: C07D311/04 ,  C07H17/04 ,  C12Q1/40 ,  G01N2333/938

    Abstract: Provided is an enzyme-specific fluorescent compound capable of being retained in cells, which can emit fluorescence specifically in a target cell, particularly a cell capable of expressing a reporter enzyme such as β-galactosidase, and can covalently bind to a protein in the cell to exhibit an excellent property of being retained in the cell. The fluorescent compound comprises a compound represented by formula (I′) or a salt thereof. In formula (I′), A, X, Y and R1 to R9 are as described in claim 1.

    Abstract translation: 提供能够保留在细胞中的酶特异性荧光化合物，其可以在靶细胞，特别是能够表达报告酶如β-半乳糖苷酶的细胞中特异性发射荧光，并且可以共价结合细胞中的蛋白质 以表现出保留在细胞中的优异性质。 荧光化合物包含由式（I'）表示的化合物或其盐。 在式（I'）中，A，X，Y和R 1至R 9如权利要求1所述。

    FLUORESCENT PROBE FOR DETECTING ACTIVATION OF SIALIDASE
    7.
    发明申请
    FLUORESCENT PROBE FOR DETECTING ACTIVATION OF SIALIDASE 有权

    公开(公告)号：US20220186286A1

    公开(公告)日：2022-06-16

    申请号：US17593009

    申请日：2020-03-05

    Applicant: The University of Tokyo

    Inventor： Yasuteru URANO ,  Mako KAMIYA ,  Charlotte RIVAS

    IPC: C12Q1/40 ,  C07H17/04

    Abstract: A fluorescent probe for sialidase activity detection, is a compound represented by the following general formula or a salt thereof. R1, if present, represents the same or different monovalent substituent present on a benzene ring. R2 and R3 each independently represent a hydrogen atom, an alkyl group having 1 to 6 carbon atoms, or a halogen atom. R4 and R5 each independently represent a hydrogen atom, an alkyl group having 1 to 6 carbon atoms, or a halogen atom. R6 represents a hydrogen atom, an alkyl group having 1 to 5 carbon atoms, or a fluorinated alkyl group having 1 to 5 carbon atoms. R6′ represents a hydrogen atom or an alkyl group having 1 to 6 carbon atoms, and R6′ may form, together with R3 or R5 a five to seven-membered heterocyclyl or heteroaryl containing a nitrogen atom to which R6′ is bonded.

    FLUORESCENT PROBE FOR DETECTING CARBOXYPEPTIDASE ACTIVITY
    9.
    发明申请
    FLUORESCENT PROBE FOR DETECTING CARBOXYPEPTIDASE ACTIVITY 有权

    公开(公告)号：US20220017940A1

    公开(公告)日：2022-01-20

    申请号：US17298477

    申请日：2019-12-02

    Applicant: The University of Tokyo

    Inventor： Yasuteru URANO ,  Mako KAMIYA ,  Yugo KURIKI

    IPC: C12Q1/37 ,  G01N33/542 ,  G01N21/64

    Abstract: A compound is represented by the following general formula (I): The compound or a salt thereof provides a fluorescent probe for detecting carboxypeptidase activity. In the formula, R1 represents an alkyl group having 1 to 6 carbon atoms or an alkoxy group having 1 to 6 carbon atoms; T represents an amino acid residue or a residue of an amino acid derivative; S represents a C-terminal amino acid residue. represents a fluorophore, and the fluorophore is a fluorophore in which an absorption/fluorescence wavelength greatly changes or a quenched state changes to a fluorescent state by elimination of the —P(═O)(—R1)-T-S moiety.

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