Fluorescent probe for measuring protease
    1.
    发明授权
    Fluorescent probe for measuring protease 有权
    用于测量蛋白酶的荧光探针

    公开(公告)号:US08461358B2

    公开(公告)日:2013-06-11

    申请号:US13201537

    申请日:2010-02-19

    IPC分类号: C07D313/00 A61K39/00

    CPC分类号: C07D493/10 C09B11/24

    摘要: A compound represented by the formula (I) or a salt thereof (R1 represents hydrogen atom, or a substituent; R2 to R7 represent hydrogen atom, hydroxyl group, an alkyl group, or a halogen atom; R8 and R9 represent hydrogen atom, or an alkyl group; X represents a C1-C3 alkylene group; and R10 represents an acyl group), which promptly causes a structural change from a non-fluorescent closed ring structure to a strongly fluorescent open ring structure by hydrolysis of an acyl group, and is useful as a fluorescent probe for measuring a protease showing superior suitability for quantification.

    摘要翻译: 由式(I)表示的化合物或其盐(R1表示氢原子或取代基; R2表示氢原子,羟基,烷基或卤素原子; R8和R9表示氢原子或 烷基; X表示C1-C3亚烷基; R10表示酰基),其通过酰基水解迅速导致从非荧光闭环结构向强荧光开环结构的结构变化,以及 作为用于测定显示出优异的定量适用性的蛋白酶的荧光探针是有用的。

    DIAGNOSTIC FOR CANCER
    2.
    发明申请
    DIAGNOSTIC FOR CANCER 审中-公开
    癌症诊断

    公开(公告)号:US20130023675A1

    公开(公告)日:2013-01-24

    申请号:US13521326

    申请日:2011-01-12

    IPC分类号: C07D493/10

    摘要: An agent for diagnosing cancer comprising, as an active ingredient, a compound represented by the following formula (I) (R1 represents hydrogen atom, or a substituent; R2 to R7 represent hydrogen atom, hydroxyl group, an alkyl group, or a halogen atom; R8 and R9 represent hydrogen atom, or an alkyl group; and X represents a C1-C3 alkylene group), which specifically emits fluorescence in a cancerous tissue within a short time when applied to a part in which presence of a cancerous tissue is suspected.

    摘要翻译: 作为活性成分的下述式(I)表示的化合物(R1表示氢原子或取代基),R2〜R7表示氢原子,羟基,烷基或卤素原子,作为活性成分 ; R8和R9表示氢原子或烷基,X表示C1-C3亚烷基),当在怀疑存在癌组织的部位应用时,在短时间内特异性地发生癌组织中的荧光 。

    FLUORESCENT PROBE FOR MEASURING PROTEASE
    3.
    发明申请
    FLUORESCENT PROBE FOR MEASURING PROTEASE 有权
    用于测量蛋白质的荧光探针

    公开(公告)号:US20120052518A1

    公开(公告)日:2012-03-01

    申请号:US13201537

    申请日:2010-02-19

    IPC分类号: C12Q1/48 C07D493/10

    CPC分类号: C07D493/10 C09B11/24

    摘要: A compound represented by the formula (I) or a salt thereof (R1 represents hydrogen atom, or a substituent; R2 to R7 represent hydrogen atom, hydroxyl group, an alkyl group, or a halogen atom; R8 and R9 represent hydrogen atom, or an alkyl group; X represents a C1-C3 alkylene group; and R10 represents an acyl group), which promptly causes a structural change from a non-fluorescent closed ring structure to a strongly fluorescent open ring structure by hydrolysis of an acyl group, and is useful as a fluorescent probe for measuring a protease showing superior suitability for quantification.

    摘要翻译: 由式(I)表示的化合物或其盐(R1表示氢原子或取代基; R2表示氢原子,羟基,烷基或卤素原子; R8和R9表示氢原子或 烷基; X表示C1-C3亚烷基; R10表示酰基),其通过酰基水解迅速导致从非荧光闭环结构向强荧光开环结构的结构变化,以及 作为用于测定显示出优异的定量适用性的蛋白酶的荧光探针是有用的。

    Reagent for measuring active nitrogen
    5.
    发明授权
    Reagent for measuring active nitrogen 有权
    用于测量活性氮的试剂

    公开(公告)号:US08895317B2

    公开(公告)日:2014-11-25

    申请号:US13131173

    申请日:2009-12-04

    摘要: A compound represented by the general formula (I) [R1 and R2 are amino groups that substitute at adjacent positions on the benzene ring; R3 and R4 are halogen atoms; R5 and R6 represent hydrogen atom, an acyl group or an acyloxy(C1-6 alkyl) group; R7 and R8 represent —(CH2)p—N(R9)(R10) (p is 1 to 4, and R9 and R10 represent —(CH2)n—COOH (n is 1 to 4))], which is useful for measuring a reactive nitrogen species existing in cells such as nitrogen monoxide or peroxynitrite at high sensitivity over a long period of time.

    摘要翻译: 由通式(I)表示的化合物[R1和R2是在苯环上的相邻位置取代的氨基; R3和R4是卤素原子; R5和R6代表氢原子,酰基或酰氧基(C1-6烷基)基团; R7和R8表示 - (CH2)p-N(R9)(R10)(p为1至4,R9和R10表示 - (CH2)n-COOH(n为1至4))] 在长时间内以高灵敏度测量存在于细胞中的活性氮物质,例如一氧化氮或过氧亚硝酸盐。

    Fluorescent probe for measurement of UDP-glucuronosyltransferase
    8.
    发明授权
    Fluorescent probe for measurement of UDP-glucuronosyltransferase 有权
    用于测量UDP-葡糖醛酸基转移酶的荧光探针

    公开(公告)号:US08309319B2

    公开(公告)日:2012-11-13

    申请号:US12527793

    申请日:2008-02-26

    IPC分类号: C12Q1/48

    CPC分类号: G01N33/582 C12Q1/48

    摘要: A fluorescent probe for measurement of UDP-glucuronosyltransferase, which comprises a fluorescein derivative, wherein in the fluorescein derivative, the 2-carboxy group on the benzene ring of fluorescein is replaced with another monovalent substituent, provided that said substituent is a substituent other than sulfo group, and the substituent does not have carboxy group or sulfo group, and wherein the fluorescein derivative may have an arbitrary substituent at a position on the benzene ring other than the 2-position, and the fluorescein derivative may have a substituent selected from the group consisting of an alkoxy group and a halogen atom at the 2-position and/or the 7-position of fluorescein.

    摘要翻译: 用于测量UDP-葡糖醛酸基转移酶的荧光探针,其包含荧光素衍生物,其中在荧光素衍生物中,荧光素的苯环上的2-羧基被另外的一价取代基取代,条件是所述取代基是除磺基以外的取代基 并且取代基不具有羧基或磺基,并且其中所述荧光素衍生物在除2-位之外的苯环上的位置可以具有任意的取代基,并且所述荧光素衍生物可以具有选自下列基团的取代基 由荧光素的2-位和/或7-位上的烷氧基和卤素原子组成。

    Fluorescent Probe
    9.
    发明申请
    Fluorescent Probe 审中-公开
    荧光探针

    公开(公告)号:US20100120160A1

    公开(公告)日:2010-05-13

    申请号:US12688625

    申请日:2010-01-15

    IPC分类号: G01N33/00 C07F5/02

    摘要: A compound represented by the formula (I) wherein R1 and R2 represent amino groups that substitute at adjacent positions on the benzene ring, wherein one of the amino groups may have one alkyl group; R3 and R4 represent hydrogen atom, a C1-6 alkyl group, or a C1-6 alkoxy group, R9 and R8 independently represent a C1-6 alkyl group, R6 and R9 represent a carboxy-substituted C1-6 alkyl group, an alkoxycarbonyl-substituted C1-6 alkyl group, a sulfo-substituted C1-6 alkyl group, or an alkyl sulfonate-substituted C1-6 alkyl group, and R7 and R10 represent a C1-6 alkyl group, an aryl group, a C1-6 alkoxycarbonyl group, a vinyl group, a thienyl group, or a pyrrolyl group, and an agent for measurement of nitrogen monoxide containing the compound. Said compound can give a fluorescent substance that is free from change in fluorescence intensity in a wide pH range.

    摘要翻译: 由式(I)表示的化合物,其中R 1和R 2表示在苯环上的相邻位置取代的氨基,其中一个氨基可以具有一个烷基; R3和R4表示氢原子,C1-6烷基或C1-6烷氧基,R9和R8独立地表示C1-6烷基,R6和R9表示羧基取代的C1-6烷基,烷氧基羰基 取代的C 1-6烷基,磺基取代的C 1-6烷基或烷基磺酸酯取代的C 1-6烷基,R 7和R 10表示C 1-6烷基,芳基,C 1-6 烷氧基羰基,乙烯基,噻吩基或吡咯基,以及含有该化合物的一氧化氮测定用试剂。 所述化合物可以产生在宽pH范围内没有荧光强度变化的荧光物质。

    Coumarin derivative
    10.
    发明授权
    Coumarin derivative 失效
    香豆素衍生物

    公开(公告)号:US07482473B2

    公开(公告)日:2009-01-27

    申请号:US11470820

    申请日:2006-09-07

    IPC分类号: C07D405/00

    CPC分类号: C07D405/12 C07D405/14

    摘要: A compound represented by the following general formula (I) or a salt thereof [R1 represents hydrogen atom, or a C1-12 alkyl group; R2 represents a C1-12 alkyl group having one or more maleimide groups, an aryl group having two or more maleimide groups, a group represented by the formula (A): —(CH2)n—CO—N(R11)(R12) (R11 and R12 represent hydrogen atom, a C1-12 alkyl group, a C1-12 alkyl group having one or more maleimide groups, or an aryl group having one or more maleimide groups, and n represents an integer of 1 to 6), or a group represented by the formula (B): —(CH2)m—NH—CO—R13 (R13 represents a C1-12 alkyl group having one or more maleimide groups, or an aryl group having one or more maleimide groups, and m represents an integer of 1 to 6); R3 and R5 represent hydrogen atom, or a halogen atom; R4 represents hydroxyl group, a C1-12 acyloxy group, a C1-12 acyloxymethyloxy group, or an amino group], which is useful as a novel fluorescent labeling agent having a property of emitting intense fluorescence only after reacting with a thiol group.

    摘要翻译: 由以下通式(I)表示的化合物或其盐[R1表示氢原子或C1-12烷基; R2表示具有一个或多个马来酰亚胺基团的C1-12烷基,具有两个或更多个马来酰亚胺基团的芳基,由式(A)表示的基团: - (CH 2)n -CO-N(R 11)(R 12) (R11和R12表示氢原子,C1-12烷基,具有一个或多个马来酰亚胺基的C1-12烷基或具有一个或多个马来酰亚胺基团的芳基,n表示1至6的整数), 或由式(B)表示的基团: - (CH 2)m -NH-CO-R 13(R 13表示具有一个或多个马来酰亚胺基团的C1-12烷基或具有一个或多个马来酰亚胺基团的芳基, m表示1〜6的整数); R3和R5代表氢原子或卤原子; R 4表示羟基,C 1-12酰氧基,C 1-12酰氧基甲氧基或氨基],其仅在与硫醇基反应后具有发射强荧光性质的新型荧光标记剂是有用的。