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    METHYLSULFONAMIDE DERIVATIVES AND USES RELATED THERETO
    1.
    发明申请
    METHYLSULFONAMIDE DERIVATIVES AND USES RELATED THERETO 审中-公开
    甲磺酰胺衍生物及其相关用途

    公开(公告)号：WO2017023999A1

    公开(公告)日：2017-02-09

    申请号：PCT/US2016/045288

    申请日：2016-08-03

    Applicant: EMORY UNIVERSITY

    Inventor： SHIM, Hyunsuk ,  GOODMAN, Mark M. ,  SHETTY, Dinesh ,  OUM, Yoon Hyeun

    IPC: A61P35/04 ,  A61K51/04

    CPC classification number: A61K51/0463 ,  A61K51/0453 ,  A61K51/0459

    Abstract: This disclosure relates to methylsulfonamide derivatives and uses as imaging agents and other uses related to CXCR4 inhibition. In certain embodiments, the disclosure relates to pharmaceutical compositions comprising compounds disclosed herein, derivatives, or pharmaceutically acceptable salts or prodrugs thereof. In certain embodiments, the compositions disclosed herein are used for imaging to study CXCR4 related conditions.

    Abstract translation: 本公开涉及甲基磺酰胺衍生物并用作显像剂和与CXCR4抑制相关的其它用途。 在某些实施方案中，本公开涉及包含本文公开的化合物，衍生物或其药学上可接受的盐或前药的药物组合物。 在某些实施方案中，本文公开的组合物用于成像以研究CXCR4相关病症。

    RADIOTRACER DERIVATIVES OF TRIMETHOPRIM FOR DIAGNOSTIC IMAGING
    2.
    发明申请
    RADIOTRACER DERIVATIVES OF TRIMETHOPRIM FOR DIAGNOSTIC IMAGING 审中-公开
    用于诊断成像的TRIMETHOPRIM的放射线衍生物

    公开(公告)号：WO2016183057A1

    公开(公告)日：2016-11-17

    申请号：PCT/US2016/031600

    申请日：2016-05-10

    Applicant: THE TRUSTEES OF THE UNIVERSITY OF PENNSYLVANIA

    Inventor： SELLMYER, Mark ,  MACH, Robert, H. ,  MANKOFF, David, A. ,  LEE, Iljung

    IPC: A61K31/395 ,  A61K31/495 ,  A61K51/00 ,  A61K51/04

    CPC classification number: A61K51/0459 ,  A61K31/395 ,  A61K31/495 ,  A61K31/505 ,  A61K47/547 ,  A61K49/0021 ,  A61K49/0052 ,  A61K51/0453

    Abstract: The present invention provides radiolabeled trimethoprim which are useful in imaging tests such as PET scans. The compounds show robust bacterial uptake in vitro and identify infections from inflammation or tumor when administered to a subject. The compounds show rapid and sensitive detection of Ec DHFR containing tumors from control tumors and background tissue. In one aspect, a compound having the structure of formula (I) is provided or a pharmaceutically acceptable salt or prodrug thereof, wherein R is defined herein. Also provided are compositions containing these compounds, positron emission tomography reporter probe comprising these compounds, and methods of imaging a bacterial infection, tracking or monitoring bacteria, distinguishing a bacterial infection from inflammation or tumor, monitoring genetically fused protein expression, and monitoring genetically engineered cells in clinical scenarios such as immunotherapy for cancer treatment.

    Abstract translation: 本发明提供放射性标记的甲氧苄啶，其可用于诸如PET扫描的成像测试。 化合物在体外显示出强烈的细菌摄取，并且当施用于受试者时鉴定炎症或肿瘤的感染。 该化合物显示对来自对照肿瘤和背景组织的Ec DHFR含量的快速和灵敏的检测。 一方面，提供具有式（I）结构的化合物或其药学上可接受的盐或前药，其中R在本文中定义。 还提供含有这些化合物的组合物，包含这些化合物的正电子发射断层摄影报告基因探针，以及细菌感染，跟踪或监测细菌，区分细菌感染与炎症或肿瘤，监测基因融合蛋白表达和监测基因工程细胞 在临床情况如癌症治疗的免疫治疗。

    PROCESS FOR PRODUCING RADIOHALOGENATED BIOCONJUGATES AND PRODUCTS THEREOF
    8.
    发明申请
    PROCESS FOR PRODUCING RADIOHALOGENATED BIOCONJUGATES AND PRODUCTS THEREOF 审中-公开
    生产放射性生物素化合物及其制品的方法

    公开(公告)号：WO2012022932A1

    公开(公告)日：2012-02-23

    申请号：PCT/GB2011/001216

    申请日：2011-08-12

    Applicant: UCL BUSINESS PLC ,  ARSTAD, Erik ,  YAN, Ran

    Inventor： ARSTAD, Erik ,  YAN, Ran

    IPC: A61K49/00 ,  A61K51/04 ,  A61K51/10 ,  A61P35/00 ,  A61K101/02

    CPC classification number: A61K51/0453 ,  A61K49/0002 ,  A61K49/0039 ,  A61K49/0041 ,  A61K49/0058 ,  A61K51/1048 ,  A61K51/1093

    Abstract: The present invention relates to a new synthetic process in which an alkyne and an azide react to form a radioisotopic bioconjugate construct. The reaction is particularly useful for producing compounds for use in imaging and radiotherapy applications. The present invention also provides bioconjugate labels and further relates to the use of these compounds in diagnostic and therapeutic methods. In addition, the invention provides a related process for introducing a radioisotopic halogen atom into a terminal alkyne.

    Abstract translation: 本发明涉及一种新的合成方法，其中炔和叠氮化物反应形成放射性同位素生物缀合物构建体。 该反应对于制备用于成像和放射治疗应用的化合物特别有用。 本发明还提供了生物缀合物标记，并且还涉及这些化合物在诊断和治疗方法中的用途。 此外，本发明提供了将放射性同位素卤素原子引入末端炔烃的相关方法。

    COMPOUNDS USEFUL IN IMAGING AND THERAPY
    9.
    发明申请
    COMPOUNDS USEFUL IN IMAGING AND THERAPY 审中-公开
    化合物可用于成像和治疗

    公开(公告)号：WO2011160216A3

    公开(公告)日：2012-02-16

    申请号：PCT/CA2011000751

    申请日：2011-06-27

    Applicant: UNIV ALBERTA ,  KUMAR PIYUSH ,  WIEBE LEONARD ,  MCEWAN ALEXANDER

    Inventor： KUMAR PIYUSH ,  WIEBE LEONARD ,  MCEWAN ALEXANDER

    IPC: C07H19/052 ,  A61K31/7056 ,  A61K49/00 ,  A61K51/00 ,  C08B37/00

    CPC classification number: C07H19/052 ,  A61K51/0453 ,  A61K51/0491 ,  C08B37/0057

    Abstract: Provided in the following specification are precursors or synthons that are useful for the synthesis of various arabinose-based chemical and radiochemical derivatives of nitroimidazole-containing azomycin arabinosides, such as radioiodinated l-a-D-( 5-deoxy-5-[I*]- iodoarabinofuranosyl)-2-nitroimidazole (*IAZA), and radiofluorinated l-a-D-( 5-deoxy-5-[18F]-iodoarabinofuranosyl)-2-nitroimidazole ( 18FAZA). Such compounds are useful in imaging, therapy, or radiotherapy. Further, various syntheses of said precursors/synthons and the incorporation of said precursors/synthons into kits is provided. The precursors/ synthons provided herein allow for an improved and facile manufacturing process for nitroimidazole-containing azomycin arabinosides.

    Abstract translation: 在以下说明书中提供了可用于合成基于阿拉伯糖的各种基于硝基咪唑的阿奇霉素的化学和放射化学衍生物的前体或合成子，例如放射性碘化的laD-（5-脱氧-5- [I *] - 碘代尿烷呋喃糖基） -2-硝基咪唑（* IAZA）和放射性氟化的LaD-（5-脱氧-5- [18 F] - 碘代阿拉伯呋喃糖基）-2-硝基咪唑（18FAZA）。 这些化合物可用于成像，治疗或放射治疗。 此外，提供所述前体/合成子的各种合成以及所述前体/合成子掺入试剂盒中。 本文提供的前体/合成物允许用于含有硝基咪唑的阿拉伯糖苷的改良且易于制造的方法。

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