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    Isotopically labeled trapping agent and method for identifying reactive metabolites
    2.
    发明授权
    Isotopically labeled trapping agent and method for identifying reactive metabolites 有权
    同位素标记的捕获剂和鉴定活性代谢物的方法

    公开(公告)号：US07884186B2

    公开(公告)日：2011-02-08

    申请号：US11860056

    申请日：2007-09-24

    Applicant: Norman D. Huebert ,  Zhengyin Yan

    Inventor： Norman D. Huebert ,  Zhengyin Yan

    IPC: A61K38/06

    CPC classification number: C07K5/0215 ,  C12Q1/26 ,  G01N2333/90258

    Abstract: The present invention is directed to an isotopically labeled trapping agent, methods for detecting reactive metabolites and methods of identifying drug candidates. More specifically, the isotopically labeled trapping agent and methods for detecting reactive metabolites may be used to detect both “hard” and “soft” reactive metabolites, thereby eliminating false positives.

    Abstract translation: 本发明涉及同位素标记的捕获剂，检测反应性代谢物的方法和鉴定候选药物的方法。 更具体地，同位素标记的捕获剂和检测反应性代谢物的方法可用于检测“硬”和“软”反应性代谢物，从而消除假阳性。

    Chemiluminescent compositions, methods, assays and kits for oxidative enzymes
    4.
    发明授权
    Chemiluminescent compositions, methods, assays and kits for oxidative enzymes 有权
    用于氧化酶的化学发光组合物，方法，测定和试剂盒

    公开(公告)号：US09067910B2

    公开(公告)日：2015-06-30

    申请号：US13254154

    申请日：2010-03-01

    Applicant: Rouh-Rong Juo ,  Brooks Edwards ,  Melissa Gee ,  Zhixian Wang ,  Kathleen Skaare

    Inventor： Rouh-Rong Juo ,  Brooks Edwards ,  Melissa Gee ,  Zhixian Wang ,  Kathleen Skaare

    IPC: C07D305/14 ,  C07D493/00 ,  C07D321/00 ,  C07D493/10 ,  C07D493/04 ,  C07D407/04 ,  C12Q1/26

    CPC classification number: C12Q1/26 ,  C07D305/14 ,  C07D321/00 ,  C07D323/00 ,  C07D407/04 ,  C07D409/04 ,  C07D493/04 ,  C07D493/10 ,  G01N2333/90245 ,  G01N2333/90251 ,  G01N2333/90258

    Abstract: Chemiluminescent compositions, methods, assays and kits for oxidative enzymes are described. Further disclosed are dioxetane compounds of the form: where R can independently be any branched alkyl or cycloalkyl group which provides stabilization for the dioxetane or where both R groups together form a cycloalkyl or polycycloalkyl moiety spiro bound to the dioxetane ring, wherein each R group or the spiro bound moiety can be unsubstituted or substituted with one or more electron-withdrawing groups or electron donating groups, or groups providing preferential oxidative isozyme substrate recognition, and wherein R1 is an aryl group, or an alkyl group of 1-20 carbon atoms, which can be optionally substituted with 1 or more halogen atoms, and wherein T is an aryl or heteroaryl ring capable of emitting light upon enzyme activated decomposition of the dioxetane I. Kits, methods and assays are also disclosed that comprise the dioxetane compounds.

    Abstract translation: 描述了用于氧化酶的化学发光组合物，方法，测定和试剂盒。 进一步公开的是以下形式的二氧杂环丁烷化合物：其中R可以独立地为任何为二氧杂环丁烷提供稳定化的支链烷基或环烷基，或者其中两个R基团一起形成与二氧杂环丁烷环结合的环烷基或多环烷基部分，其中每个R基团或 螺结合部分可以是未取代的或被一个或多个吸电子基团或给电子基团或提供优先氧化同功酶底物识别的基团取代，并且其中R1是芳基或1-20个碳原子的烷基， 其可以任选地被1个或多个卤素原子取代，并且其中T是在二氧杂环丁烷I的酶活化分解时能够发光的芳基或杂芳基环。还公开了包含二恶丁环化合物的方法和测定法。

    Identification of the genetic determinants of the polymorphic CYP3A5 expression
    5.
    发明申请
    Identification of the genetic determinants of the polymorphic CYP3A5 expression 审中-公开
    鉴定多态CYP3A5表达的遗传决定因子

    公开(公告)号：US20060282908A1

    公开(公告)日：2006-12-14

    申请号：US10607596

    申请日：2003-06-27

    Applicant: Leszek Wojnowski ,  Elisabeth Hustert ,  Michael Haberl

    Inventor： Leszek Wojnowski ,  Elisabeth Hustert ,  Michael Haberl

    IPC: A01K67/027 ,  C12Q1/68 ,  C07H21/04 ,  C12P21/06 ,  C12N9/02

    CPC classification number: C12Q1/6827 ,  C12N9/0077 ,  C12Q1/6883 ,  C12Q1/6886 ,  C12Q2600/156 ,  C12Q2600/158 ,  C12Q2600/172 ,  G01N2333/90258 ,  G01N2500/04

    Abstract: The present invention relates to a polymorphic CYP3A5 polynucleotide. Moreover, the invention relates to genes or vectors comprising the polynucleotides of the invention and to a host cell genetically engineered with the polynucleotide or gene of the invention. Further, the invention relates to methods for producing molecular variant polypeptides or fragments thereof, methods for producing cells capable of expressing a molecular variant polypeptide and to a polypeptide or fragment thereof encoded by the polynucleotide or the gene of the invention or which is obtainable by the method or from the cells produced by the method of the invention. Furthermore, the invention relates to an antibody which binds specifically the polypeptide of the invention. Moreover, the invention relates to a transgenic non-human animal. The invention also relates to a solid support comprising one or a plurality of the above mentioned polynucleotides, genes, vectors, polypeptides, antibodies or host cells. Furthermore, methods of identifying a polymorphism, identifying and obtaining a pro-drug or drug or an inhibitor are also encompassed by the present invention. In addition, the invention relates to methods for producing of a pharmaceutical composition and to methods of diagnosing a disease. Further, the invention relates to a method of detection of the polynucleotide of the invention. Furthermore, comprised by the present invention are a diagnostic and a pharmaceutical composition. Even more, the invention relates to uses of the polynucleotides, genes, vectors, polypeptides or antibodies of the invention. Finally, the invention relates to a diagnostic kit.

    Abstract translation: 本发明涉及多态CYP3A5多核苷酸。 此外，本发明涉及包含本发明的多核苷酸的基因或载体，并涉及用本发明的多核苷酸或基因进行遗传工程改造的宿主细胞。 此外，本发明涉及用于产生分子变体多肽或其片段的方法，用于产生能够表达分子变体多肽的细胞的方法及其由本发明的多核苷酸或基因编码的多肽或其片段，或可由 方法或由本发明方法生产的细胞。 此外，本发明涉及特异性结合本发明多肽的抗体。 此外，本发明涉及转基因非人动物。 本发明还涉及包含一种或多种上述多核苷酸，基因，载体，多肽，抗体或宿主细胞的固体支持物。 此外，鉴定多态性，鉴定和获得前药或药物或抑制剂的方法也包括在本发明中。 此外，本发明涉及制备药物组合物的方法和诊断疾病的方法。 此外，本发明涉及本发明的多核苷酸的检测方法。 此外，本发明包括诊断和药物组合物。 更进一步地，本发明涉及本发明的多核苷酸，基因，载体，多肽或抗体的用途。 最后，本发明涉及诊断试剂盒。

    CHEMILUMINESCENT COMPOSITIONS, METHODS, ASSAYS AND KITS FOR OXIDATIVE ENZYMES
    6.
    发明申请
    CHEMILUMINESCENT COMPOSITIONS, METHODS, ASSAYS AND KITS FOR OXIDATIVE ENZYMES 有权
    氧化酶的显色组合物，方法，测定和试剂

    公开(公告)号：US20150284766A1

    公开(公告)日：2015-10-08

    申请号：US14694758

    申请日：2015-04-23

    Applicant: LIFE TECHNOLOGIES CORPORATION

    Inventor： Rouh-Rong Juo ,  Brooks Edwards ,  Melissa GEE ,  Zhixian WANG ,  Kathleen SKAARE

    IPC: C12Q1/26 ,  C07D409/04 ,  C07D323/00

    CPC classification number: C12Q1/26 ,  C07D305/14 ,  C07D321/00 ,  C07D323/00 ,  C07D407/04 ,  C07D409/04 ,  C07D493/04 ,  C07D493/10 ,  G01N2333/90245 ,  G01N2333/90251 ,  G01N2333/90258

    Abstract: Chemiluminescent compositions, methods, assays and kits for oxidative enzymes are described. Further disclosed are dioxetane compounds of the form: where R can independently be any branched alkyl or cycloalkyl group which provides stabilization for the dioxetane or where both R groups together form a cycloalkyl or polycycloalkyl moiety spiro bound to the dioxetane ring, wherein each R group or the spiro bound moiety can be unsubstituted or substituted with one or more electron-withdrawing groups or electron donating groups, or groups providing preferential oxidative isozyme substrate recognition, and wherein R1 is an aryl group, or an alkyl group of 1-20 carbon atoms, which can be optionally substituted with 1 or more halogen atoms, and wherein T is an aryl or heteroaryl ring capable of emitting light upon enzyme activated decomposition of the dioxetane I.Kits, methods and assays are also disclosed that comprise the dioxetane compounds.

    Abstract translation: 描述了用于氧化酶的化学发光组合物，方法，测定和试剂盒。 进一步公开的是以下形式的二氧杂环丁烷化合物：其中R可以独立地为任何为二氧杂环丁烷提供稳定性的支链烷基或环烷基，或者其中两个R基团一起形成与二氧杂环丁烷环结合的环烷基或多环烷基部分，其中每个R基团或 螺结合部分可以是未取代的或被一个或多个吸电子基团或给电子基团或提供优先氧化同功酶底物识别的基团取代，并且其中R1是芳基或1-20个碳原子的烷基， 其可以任选地被1个或多个卤素原子取代，并且其中T是在二氧杂环丁烷I的酶活化分解时能够发光的芳基或杂芳基环。还公开了包含二恶丁环化合物的方法和测定法。

    CHEMILUMINESCENT COMPOSITIONS, METHODS, ASSAYS AND KITS FOR OXIDATIVE ENZYMES
    7.
    发明申请
    CHEMILUMINESCENT COMPOSITIONS, METHODS, ASSAYS AND KITS FOR OXIDATIVE ENZYMES 有权
    氧化酶的显色组合物，方法，测定和试剂

    公开(公告)号：US20120100566A1

    公开(公告)日：2012-04-26

    申请号：US13254154

    申请日：2010-03-01

    Applicant: Rouh-Rong Juo ,  Brooks Edwards ,  Melissa Gee ,  Zhixian Wang ,  Kathleen Skaare

    Inventor： Rouh-Rong Juo ,  Brooks Edwards ,  Melissa Gee ,  Zhixian Wang ,  Kathleen Skaare

    IPC: C12Q1/26 ,  C07D409/04 ,  C07D323/00

    CPC classification number: C12Q1/26 ,  C07D305/14 ,  C07D321/00 ,  C07D323/00 ,  C07D407/04 ,  C07D409/04 ,  C07D493/04 ,  C07D493/10 ,  G01N2333/90245 ,  G01N2333/90251 ,  G01N2333/90258

    Abstract: Chemiluminescent compositions, methods, assays and kits for oxidative enzymes are described. Further disclosed are dioxetane compounds of the form: 0-0 ΛR R R T (i) where R can independently be any branched alkyl or cycloalkyl group which provides stabilization for the dioxetane or where both R groups together form a cycloalkyl or polycycloalkyl moiety spiro bound to the dioxetane ring, wherein each R group or the spiro bound moiety can be unsubstituted or substituted with one or more electron-withdrawing groups or electron donating groups, or groups providing preferential oxidative isozyme substrate recognition, and wherein Ri is an aryl group, or an alkyl group of 1-20 carbon atoms, which can be optionally substituted with 1 or more halogen atoms, and wherein T is an aryl or heteroaryl ring capable of emitting light upon enzyme activated decomposition of the dioxetane I. Kits, methods and assays are also disclosed that comprise the dioxetane compounds.

    Abstract translation: 描述了用于氧化酶的化学发光组合物，方法，测定和试剂盒。 进一步公开的是以下形式的二氧杂环丁烷化合物：其中R可以独立地是任何分支烷基或环烷基，其为二氧杂环丁烷提供稳定性，或者其中两个R基团一起形成环烷基或多环烷基部分螺 二环氧环乙烷环，其中每个R基团或螺环结合的部分可以是未取代的或被一个或多个吸电子基团或给电子基团或提供优先氧化同功酶底物识别的基团取代，并且其中R 1是芳基或烷基 1-20个碳原子的基团，其可以任选地被1个或多个卤素原子取代，并且其中T是能够在二氧杂环丁烷I的酶活化分解时发光的芳基或杂芳基环。另外还公开了方法和测定 其包含二氧杂环丁烷化合物。

    ISOTOPICALLY LABELED TRAPPING AGENT AND METHOD FOR IDENTIFYING REACTIVE METABOLITES
    8.
    发明申请
    ISOTOPICALLY LABELED TRAPPING AGENT AND METHOD FOR IDENTIFYING REACTIVE METABOLITES 有权
    同位素标记代谢物和识别反应性代谢物的方法

    公开(公告)号：US20080081349A1

    公开(公告)日：2008-04-03

    申请号：US11860056

    申请日：2007-09-24

    Applicant: Norman D. Huebert ,  Zhengyin Yan

    Inventor： Norman D. Huebert ,  Zhengyin Yan

    IPC: C12Q1/26 ,  C07C229/02

    CPC classification number: C07K5/0215 ,  C12Q1/26 ,  G01N2333/90258

    Abstract: The present invention is directed to an isotopically labeled trapping agent, methods for detecting reactive metabolites and methods of identifying drug candidates. More specifically, the isotopically labeled trapping agent and methods for detecting reactive metabolites may be used to detect both “hard” and “soft” reactive metabolites, thereby eliminating false positives.

    Abstract translation: 本发明涉及同位素标记的捕获剂，检测反应性代谢物的方法和鉴定候选药物的方法。 更具体地，同位素标记的捕获剂和检测反应性代谢物的方法可用于检测“硬”和“软”反应性代谢物，从而消除假阳性。

    METHODS FOR CHARACTERIZING TIME-BASED HEPATOTOXICITY
    9.
    发明申请
    METHODS FOR CHARACTERIZING TIME-BASED HEPATOTOXICITY 审中-公开

    公开(公告)号：US20180113119A1

    公开(公告)日：2018-04-26

    申请号：US15559452

    申请日：2016-03-21

    Applicant: HUREL CORPORATION

    Inventor： Robert FREEDMAN ,  James MACDONALD ,  Eric NOVIK

    IPC: G01N33/50

    CPC classification number: G01N33/5067 ,  G01N33/5014 ,  G01N33/5044 ,  G01N2333/90258

    Abstract: Methods of characterizing the time-based hepatotoxicity of a test compound are provided. In some embodiments the provided methods allow prediction of the hepatotoxic potential of a test compound in a way that is improved relative to that achievable with prior art methods. In some embodiments the methods may be used to quantify the relationship between measurements or estimates of toxicity made at different, successive points in time, to provide highly meaningful tool to assess the likely in vivo hepatotoxicity of test compounds in vivo.

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