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    PHOTON REDUCING AGENTS FOR FLUORESCENCE ASSAYS
    3.
    发明申请
    PHOTON REDUCING AGENTS FOR FLUORESCENCE ASSAYS 有权
    用于荧光测定的光子还原剂

    公开(公告)号：US20090162926A1

    公开(公告)日：2009-06-25

    申请号：US12398744

    申请日：2009-03-05

    申请人： Tom Knapp ,  Gregor Zlokarnik ,  Paul Negulescu ,  Roger Y. Tsien ,  Timothy James Rink

    发明人： Tom Knapp ,  Gregor Zlokarnik ,  Paul Negulescu ,  Roger Y. Tsien ,  Timothy James Rink

    IPC分类号： C12M1/34

    CPC分类号： G01N33/582 ,  C12Q1/682 ,  G01N33/5005 ,  G01N33/542 ,  Y10S436/80 ,  Y10S436/809 ,  Y10T436/13 ,  C12Q2563/107 ,  C12Q2527/125

    摘要： The present invention provides a method for reducing undesirable light emission from a sample using at least one photon producing agent and at least one photon reducing agent (e.g. dye-based photon reducing agents). The present invention further provides a method for reducing undesirable light emission from a sample (e.g. a biochemical or cellular sample) with at least one photon producing agent and at least one collisional quencher. The present invention also provides a method for reducing undesirable light emission from a sample (e.g., a biochemical or cellular sample) with at least one photon producing agent and at least one quencher, such as an electronic quencher. The present invention also provides a system and method of screening test chemicals in fluorescent assays using photon reducing agents. The present invention also provides compositions, pharmaceutical compositions, and kits for practicing these methods.

    摘要翻译： 本发明提供一种使用至少一种光子产生剂和至少一种光子还原剂（例如基于染料的光子还原剂）来减少来自样品的不希望的光发射的方法。 本发明还提供了一种用至少一种光子产生剂和至少一种碰撞猝灭剂来减少来自样品（例如生物化学或细胞样品）的不希望的光发射的方法。 本发明还提供了用至少一种光子产生剂和至少一种猝灭剂（例如电子猝灭剂）减少来自样品（例如，生物化学或细胞样品）的不希望的光发射的方法。 本发明还提供了使用光子还原剂在荧光测定中筛选测试化学品的系统和方法。 本发明还提供了用于实施这些方法的组合物，药物组合物和试剂盒。

    OPTICAL MOLECULAR SENSORS FOR CYTOCHROME P450 ACTIVITY
    4.
    发明申请
    OPTICAL MOLECULAR SENSORS FOR CYTOCHROME P450 ACTIVITY 审中-公开

    公开(公告)号：US20070072256A1

    公开(公告)日：2007-03-29

    申请号：US11531136

    申请日：2006-09-12

    申请人： Lewis MAKINGS ,  Gregor ZLOKARNIK

    发明人： Lewis MAKINGS ,  Gregor ZLOKARNIK

    IPC分类号： C12Q1/26

    CPC分类号： C07D493/10 ,  C07D265/38 ,  C07D311/16 ,  C07D311/82 ,  C12Q1/26 ,  G01N2333/90245 ,  G01N2500/02

    摘要： The invention provides a compound, useful as an optical probe or sensor of the activity of at least one cytochrome P450 enzyme, and methods of using the compound to screen candidate drugs, and candidate drugs identified by these methods. The optical probe of the invention is a compound having the generic structure Y-L-Q, wherein Y is selected from the group consisting of Q as herein defined, saturated C1-C20 alkyl, unsaturated C1-C20 alkenyl, unsaturated C1-C20 alkynyl, substituted saturated C1-C20 alkyl, substituted unsaturated C1-C20 alkenyl, substituted unsaturated C1-C20 alkynyl, C1-C20 cycloalkyl, C1-C20 cycloalkenyl, substituted saturated C1-C20 cycloalkyl, substituted unsaturated C1-C20 cycloalkenyl, aryl, substituted aryl, heteroaryl and substituted heteroaryl; L is selected from the group of (—OCR2H)p—, wherein for each p, all R2 are separately selected from the group consisting of a hydrogen atom, saturated C1-C20 alkyl, unsaturated C1-C20 alkenyl, unsaturated C1-C20 alkynyl, substituted saturated C1-C20 alkyl, substituted unsaturated C1-C20 alkenyl, substituted unsaturated C1-C20 alkynyl, C1-C20 cycloalkyl, C1-C20 cycloalkenyl, substituted saturated C1-C20 cycloalkyl, substituted unsaturated C1-C20 cycloalkenyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, and p is a positive integer no greater than twelve; and Q is a chemical moiety that gives rise to optical properties in its hydroxy or hydroxylate, phenol or phenoxide form that are different from the optical properties that arise from its ether form. Most preferably, p is one, R2 is hydrogen, and Q is the ether form of a phenoxide fluorophore.

    Optical molecular sensors for cytochrome P450 activity
    7.
    发明授权
    Optical molecular sensors for cytochrome P450 activity 有权
    用于细胞色素P450活性的光学分子传感器

    公开(公告)号：US08153828B2

    公开(公告)日：2012-04-10

    申请号：US12499047

    申请日：2009-07-07

    申请人： Lewis Makings ,  Gregor Zlokarnik

    发明人： Lewis Makings ,  Gregor Zlokarnik

    IPC分类号： C07D311/06

    CPC分类号： C07D493/10 ,  C07D219/06 ,  C07D265/38 ,  C07D311/16 ,  C07D311/82 ,  C12Q1/26 ,  G01N2333/90245 ,  G01N2500/02 ,  Y10S435/968

    摘要： The invention provides a compound, useful as an optical probe or sensor of the activity of at least one cytochrome P450 enzyme, and methods of using the compound to screen candidate drugs, and candidate drugs identified by these methods. The optical probe of the invention is a compound having the generic structure Y-L-Q, wherein Q is a chemical moiety that gives rise to optical properties in its hydroxy or hyrdoxylate, phenol or phenoxide form that are different from the optical properties that arise from its ether form.

    摘要翻译： 本发明提供了可用作至少一种细胞色素P450酶的活性的光学探针或传感器的化合物，以及使用该化合物筛选候选药物的方法以及通过这些方法鉴定的候选药物。 本发明的光学探针是具有一般结构YLQ的化合物，其中Q是一种化学部分，其产生与其醚形式产生的光学性质不同的羟基或羟乙酸酯，苯酚或酚盐形式的光学性质 。

    Optical molecular sensors for cytochrome P450 activity
    9.
    发明授权
    Optical molecular sensors for cytochrome P450 activity 有权
    用于细胞色素P450活性的光学分子传感器

    公开(公告)号：US6143492A

    公开(公告)日：2000-11-07

    申请号：US301395

    申请日：1999-04-28

    申请人： Lewis R. Makings ,  Gregor Zlokarnik

    发明人： Lewis R. Makings ,  Gregor Zlokarnik

    IPC分类号： C07D265/38 ,  C07D311/16 ,  C07D311/82 ,  C07D493/10 ,  C12Q1/26 ,  C12Q1/00

    CPC分类号： C07D493/10 ,  C07D265/38 ,  C07D311/16 ,  C07D311/82 ,  C12Q1/26 ,  Y10S435/968

    摘要： The invention provides a compound, useful as an optical probe or sensor of the activity of at least one cytochrome P450 enzyme, and methods of using the compound to screen candidate drugs, and candidate drugs identified by these methods. The optical probe of the invention is a compound having the generic structure Y-L-Q, wherein Y is selected from the group consisting of Q as herein defined, saturated C.sub.1 -C.sub.20 alkyl, unsaturated C.sub.1 -C.sub.20 alkenyl, unsaturated C.sub.1 -C.sub.20 alkynyl, substituted saturated C.sub.1 -C.sub.20 alkyl, substituted unsaturated C.sub.1 -C.sub.20 alkenyl, substituted unsaturated C.sub.1 -C.sub.20 alkynyl, C.sub.1 -C.sub.20 cycloalkyl, C.sub.1 -C.sub.20 cycloalkenyl, substituted saturated C.sub.1 -C.sub.20 cycloalkyl, substituted unsaturated C.sub.1 -C.sub.20 cycloalkenyl, aryl, substituted aryl, heteroaryl and substituted heteroaryl; L is selected from the group of (--O(substituted ortho-phenyl)CR.sup.2 H).sub.p --, (--O(substituted meta-phenyl)CR.sup.2 H).sub.p --, and (--O(substituted para-phenyl)CR.sup.2 H).sub.p --, wherein for each p, all R.sup.2 are separately selected from the group consisting of a hydrogen atom, saturated C.sub.1 -C.sub.20 alkyl, unsaturated C.sub.1 -C.sub.20 alkenyl, unsaturated C.sub.1 -C.sub.20 alkynyl, substituted saturated C.sub.1 -C.sub.20 alkyl, substituted unsaturated C.sub.1 -C.sub.20 alkenyl, substituted unsaturated C.sub.1 -C.sub.20 alkynyl, C.sub.1 -C.sub.20 cycloalkyl, C.sub.1 -C.sub.20 cycloalkenyl, substituted saturated C.sub.1 -C.sub.20 cycloalkyl, substituted unsaturated C.sub.1 -C.sub.20 cycloalkenyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, and p is a positive integer no greater than twelve; and Q is a chemical moiety that gives rise to optical properties in its hydroxy or hyrdoxylate, phenol or phenoxide form that are different from the optical properties that arise from its ether form. Most preferably, p is one, R.sup.2 is hydrogen, and Q is the ether form of a phenoxide fluorophore.

    摘要翻译： 本发明提供了可用作至少一种细胞色素P450酶的活性的光学探针或传感器的化合物，以及使用该化合物筛选候选药物的方法以及通过这些方法鉴定的候选药物。 本发明的光学探针是具有一般结构YLQ的化合物，其中Y选自本文定义的Q，饱和C 1 -C 20烷基，不饱和C 1 -C 20烯基，不饱和C 1 -C 20炔基，取代的饱和C 1 -C 20烷基，取代的不饱和C 1 -C 20烯基，取代的不饱和C 1 -C 20炔基，C 1 -C 20环烷基，C 1 -C 20环烯基，取代的饱和C 1 -C 20环烷基，取代的不饱和C 1 -C 20环烯基，芳基，取代的芳基， 杂芳基; L选自（-O（取代的邻 - 苯基）CR2H）对 - ，（ - （ - （取代的间苯基）CR2H）对 - 和（ - （取代的对 - 苯基）CR2H）对 - 其中对于每个p，所有的R 2分别选自氢原子，饱和C 1 -C 20烷基，不饱和C 1 -C 20烯基，不饱和C 1 -C 20炔基，取代的饱和C 1 -C 20烷基，取代的不饱和C 1 -C 20烯基 取代的不饱和C 1 -C 20炔基，C 1 -C 20环烷基，C 1 -C 20环烯基，取代的饱和C 1 -C 20环烷基，取代的不饱和C 1 -C 20环烯基，芳基，取代的芳基，杂芳基，取代的杂芳基，p是不大于 十二岁以上 并且Q是一种化学部分，其产生与其醚形式产生的光学性质不同的其羟基或羟乙酸酯，苯酚或酚盐形式的光学性质。 最优选地，p是1，R2是氢，Q是醚形式的苯氧基荧光团。