FLUORESCENT PROBE FOR USE IN DETECTION OF BRAIN TUMOR

    公开(公告)号:US20220341922A1

    公开(公告)日:2022-10-27

    申请号:US17612378

    申请日:2020-05-19

    摘要: 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.

    METHOD FOR DIAGNOSING CANCER
    3.
    发明申请
    METHOD FOR DIAGNOSING CANCER 审中-公开
    用于诊断癌症的方法

    公开(公告)号:US20140206992A1

    公开(公告)日:2014-07-24

    申请号:US14163422

    申请日:2014-01-24

    IPC分类号: A61K49/00

    摘要: Methods for identifying the presence of cancerous cells or tissue by: applying a compound of formula (I), or salts thereof, to a living body, wherein R1 represents hydrogen or the same or different one to four substituents; R2, R3, R4, R5, R6, and R7 independently represent hydrogen, hydroxy, alkyl, or halogen; R8 and R9 independently represent hydrogen or alkyl; and X represents C1-C3 alkylene; and detecting fluorescence emitted by a compound of formula (II), wherein R1, R2, R3, R4, R5, R6, R7, R8, and R9 are as defined above; wherein fluorescence emitted by a compound of formula (II) is indicative of the presence of cancerous cells or tissue.

    摘要翻译: 通过以下方法鉴定癌细胞或组织的存在:将式(I)化合物或其盐施用于活体,其中R 1表示氢或相同或不同的一至四个取代基; R2,R3,R4,R5,R6和R7独立地表示氢,羟基,烷基或卤素; R8和R9独立地表示氢或烷基; X表示C1-C3亚烷基; 并检测由式(II)化合物发射的荧光,其中R 1,R 2,R 3,R 4,R 5,R 6,R 7,R 8和R 9如上定义; 其中由式(II)化合物发射的荧光指示癌细胞或组织的存在。

    SUPER-RESOLUTION FLUORESCENT IMAGING PROBE
    4.
    发明申请

    公开(公告)号:US20180052109A1

    公开(公告)日:2018-02-22

    申请号:US15551149

    申请日:2016-02-23

    IPC分类号: G01N21/64 A61K49/00 C09K11/06

    摘要: [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

    IPC分类号: C07D311/04 C12Q1/40

    摘要: 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.

    摘要翻译: 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。