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    Hydroxylases and modulators thereof
    3.
    发明申请
    Hydroxylases and modulators thereof 失效
    羟基酶及其调节剂

    公开(公告)号：US20070048728A1

    公开(公告)日：2007-03-01

    申请号：US10531662

    申请日：2003-10-16

    申请人： Peter Ratcliffe ,  Christopher Pugh ,  Christopher Schofield ,  Kirsty Hewitson

    发明人： Peter Ratcliffe ,  Christopher Pugh ,  Christopher Schofield ,  Kirsty Hewitson

    IPC分类号： C12Q1/00 ,  G06F19/00 ,  C07D471/02 ,  C07D211/72

    CPC分类号： A61K31/16 ,  A61K31/395 ,  G06F19/16 ,  G06F19/706

    摘要： A method of identifying, screening, characterising or designing a chemical entity, which mimics or binds to FIH, is described. The method comprises comparing a structural model of FIH with a structural model for said chemical entity, wherein said structural model of FIH is derived from structural factors or structural coordinates determined by subjecting to X-ray diffraction measurements a crystal comprising FIH. Such chemical entities may be used in the treatment of a condition associated with increased or decreased HIF levels or activity.

    摘要翻译： 描述了识别，筛选，表征或设计模拟或结合FIH的化学实体的方法。 该方法包括将FIH的结构模型与所述化学实体的结构模型进行比较，其中FIH的结构模型来源于通过对包含FIH的晶体进行X射线衍射测量确定的结构因子或结构坐标。 这些化学实体可用于治疗与增加或降低的HIF水平或活性相关的病症。

    High throughput assay
    4.
    发明申请
    High throughput assay 审中-公开
    高通量测定

    公开(公告)号：US20050214894A1

    公开(公告)日：2005-09-29

    申请号：US11090320

    申请日：2005-03-28

    申请人： Christopher Schofield ,  Kirsty Hewitson ,  Luke McNeill

    发明人： Christopher Schofield ,  Kirsty Hewitson ,  Luke McNeill

    IPC分类号： C12Q1/26 ,  G01N33/58

    CPC分类号： C12Q1/26 ,  G01N33/582

    摘要： A method for detecting 2-oxoglutarate oxygenase activity, which method comprises: (i) contacting a 2-oxoglutarate oxygenase and a substrate of the 2-oxoglutarate oxygenase in the presence of 2-oxoglutarate; (ii) adding a derivatisation reagent capable of forming a fluorescent product with 2-oxoglutarate; (iii) detecting the fluorescent product produced by the reaction between the derivatisation reagent and 2-oxoglutarate, if any, thereby detecting 2-oxoglutarate oxgenase activity.

    摘要翻译： 一种检测2-氧戊二烯加氧酶活性的方法，该方法包括：（i）在2-氧戊二酸的存在下使2-氧戊二酸加氧酶与2-氧戊二酸加氧酶的底物接触; （ii）加入能够与2-氧戊二酸形成荧光产物的衍生试剂; （iii）检测由衍生化试剂和2-氧戊二酸之间的反应产生的荧光产物（如果有的话），从而检测2-氧戊二酸氧合酶活性。

    Degradation fragments
    6.
    发明申请
    Degradation fragments 失效

    公开(公告)号：US20070015816A1

    公开(公告)日：2007-01-18

    申请号：US11479024

    申请日：2006-06-30

    申请人： Joseph Clark ,  Thomas Cadoux-Hudson ,  Christopher Schofield

    发明人： Joseph Clark ,  Thomas Cadoux-Hudson ,  Christopher Schofield

    IPC分类号： A61K31/4025 ,  A61K31/4015 ,  C07D403/14 ,  C07D403/02 ,  G01N33/53

    CPC分类号： C07D207/44 ,  A61K31/40 ,  A61K31/4015 ,  A61K31/4025 ,  A61K41/0019 ,  C07D207/448 ,  C07D413/06 ,  G01N33/728 ,  Y10S436/822

    摘要： A pharmaceutical composition comprising a compound of formula (I) wherein X is an electron withdrawing group, Y1 is hydrogen, alkyl, alkenyl, alkynyl, aryl, heterocyclyl, —SO2R4, —CO2R4, —CONHR4 or —COR4, and each of R1, R2 and R4, which may be the same or different, is hydrogen, alkyl, cycloalkyl, alkenyl, cycloalkenyl, alkynyl, aryl or heterocyclyl, or a compound of formula (II) wherein each of Y2 and Y3, which may be the same or different, is hydrogen, alkyl, alkenyl, alkynyl, aryl, heterocyclyl, —SO2R9, —CO2R9, —CONHR9 or —COR9, Z is hydrogen, alkyl, cycloalkyl, alkenyl, cycloalkenyl, alkynyl, aryl, heterocyclyl, —CH═C(NHR10)CH((CH2)mCO2R11)(C═O)CH3 or —CH2(C═O)CH((CH2)mCO2R11)(C═O)CH3, R8 is —(CH2)nCO2R12, each of R5 to R7 and R9 to R12, which may be the same or different, is hydrogen, alkyl, cycloalkyl, alkenyl, cycloalkenyl, alkynyl, aryl or heterocyclyl, and each of m and n, which may be the same or different, is 1 to 6 or a compound of formula (III) wherein each of Y4 to Y6, which may be the same or different, is hydrogen, alkyl, alkenyl, alkynyl, aryl, heterocyclyl, —SO2R19, —CO2R19, —CONHR19 or —COR19, each of R16 and R17, which may be the same or different, is —(CH2)pCO2R20, each of R13 to R15 and R18 to R20, which may be the same or different, is hydrogen, alkyl, cycloalkyl, alkenyl, cycloalkenyl, alkynyl, aryl or heterocyclyl, and p is 1 to 6, or other photolabile degradation product of bilirubin or biliverdin or derivative of a photolabile degradation fragment of bilirubin or biliverdin, or a pharmaceutically acceptable salt thereof, together with a pharmaceutically acceptable carrier or diluent.