QUINOLINE DERIVATIVES FOR DIAGNOSIS AND TREATMENT OF ALZHEIMER'S DISEASE
    3.
    发明申请
    QUINOLINE DERIVATIVES FOR DIAGNOSIS AND TREATMENT OF ALZHEIMER'S DISEASE 审中-公开
    用于诊断和治疗阿尔茨海默病的喹啉衍生物

    公开(公告)号:WO2016183578A1

    公开(公告)日:2016-11-17

    申请号:PCT/US2016/032700

    申请日:2016-05-16

    Abstract: A new class of quinoline compounds is useful for the detection and treatment of Alzheimer's disease and other neurodegenerative diseases such as amyloidoses and tauopathies. The compounds can be synthesized in radiolabeled form for use as imaging agents, which can be used for early detection of aggregates in the brain or other tissues prior to onset of symptoms, allowing early therapeutic intervention. The compounds are also useful for the prevention and treatment of such diseases.

    Abstract translation: 一类新的喹啉化合物可用于检测和治疗阿尔茨海默病和其他神经变性疾病如淀粉样变性和tau蛋白病。 化合物可以以放射性标记形式合成用作显像剂,其可用于在症状出现之前脑或其他组织中的聚集体的早期检测,从而允许早期治疗干预。 这些化合物也可用于预防和治疗这些疾病。

    NOVEL ANTHRANILIC ACID DERIVATIVES
    4.
    发明申请
    NOVEL ANTHRANILIC ACID DERIVATIVES 审中-公开
    新型硫代酸衍生物

    公开(公告)号:WO2016051306A3

    公开(公告)日:2016-10-13

    申请号:PCT/IB2015057254

    申请日:2015-09-21

    CPC classification number: A61K51/0455 C07B2200/05 C07D401/12

    Abstract: The present invention is directed to a novel compound of Formula 1 wherein the radiolabeled compound of Formula 1 is capable of being used as a radiotracer in PET imaging of a targeted localized tissue and targeted radionuclide therapy of one or more conditions that may be regulated or normalized via inhibition of transporter such as Pgp, BCRP or MRP I. The novel compounds of Formula 1 can also be used as substrates for binding with one or more ABC transporters. In particular, the present invention aids in diagnosis and therapeutic treatment of MDR disorders in all forms of cancers and neurological disorders of the central nervous system. The present invention further provides methods of preparation of compounds of Formula 1 and novel intermediates used in the preparation of compounds of Formula 1.

    Abstract translation: 本发明涉及式1的新型化合物,其中放射性标记的式1化合物能够用作靶向局部组织的PET成像中的放射性示踪剂,并且靶向放射性核素治疗可被调节或归一化的一种或多种病症 通过抑制转运蛋白如Pgp,BCRP或MRP I。式1的新化合物也可以用作与一种或多种ABC转运蛋白结合的底物。 特别地,本发明有助于诊断和治疗所有形式的癌症和中枢神经系统神经系统疾病的MDR疾病。 本发明还提供制备式1化合物的方法和用于制备式1化合物的新中间体。

    METHODS AND COMPOSITIONS FOR 18F-RADIOLABELING OF BIOLOGICS
    5.
    发明申请
    METHODS AND COMPOSITIONS FOR 18F-RADIOLABELING OF BIOLOGICS 审中-公开
    生物制品的18F-放射性组合物的方法和组合物

    公开(公告)号:WO2016086036A3

    公开(公告)日:2016-07-07

    申请号:PCT/US2015062502

    申请日:2015-11-24

    Inventor: DONNELLY DAVID

    CPC classification number: A61K51/0455 A61K51/088 C07B59/002 C07B59/008

    Abstract: The invention relates to water soluble 18 F-prosthetic groups and the synthesis and use of 18 F-labeled biological molecules containing the 18 F-prosthetic groups for imaging various processes within the body, for detecting the location of molecules associated with disease pathology, and for monitoring disease progression are disclosed.

    Abstract translation: 本发明涉及水溶性18 F-假体组和包含18 F-假体组的18 F-标记的生物分子的合成和用途,用于成像身体内的各种过程,用于检测与疾病病理相关的分子的位置,以及 用于监测疾病进展的公开。

    4-OXO-1,4-DIHYDROQUINOLINE-3-CARBOXAMIDE AS SELECTIVE LIGAND FOR CANNABINOID RECEPTOR 2 FOR DIAGNOSIS AND THERAPY
    8.
    发明申请
    4-OXO-1,4-DIHYDROQUINOLINE-3-CARBOXAMIDE AS SELECTIVE LIGAND FOR CANNABINOID RECEPTOR 2 FOR DIAGNOSIS AND THERAPY 审中-公开
    4-OXO-1,4-二氢喹啉-3-羧酰胺作为CANNABINOID受体2的选择性配体用于诊断和治疗

    公开(公告)号:WO2016005419A1

    公开(公告)日:2016-01-14

    申请号:PCT/EP2015/065537

    申请日:2015-07-08

    CPC classification number: C07D215/56 A61K51/0455

    Abstract: The present invention is directed to new compounds of formula (I) selectively binding the cannabinoid 2 receptor. In addition, the invention relates to the use of said compounds for determining cannabinoid receptor 2 (CB2)-selective receptor localization and density, preferably in the central nervous system (CNS), the peripheral nervous system (PNS), heart, liver, gastrointestinal tract, spleen, pancreas, kidney, testis, ovary and/or the prostate. Moreover, the invention pertains to the use of said compounds in the diagnosis, prophylaxis and/or therapy of CB2 receptor-related diseases.

    Abstract translation: 本发明涉及式(I)的新化合物选择性地结合大麻素2受体。 此外,本发明涉及所述化合物用于确定大麻素受体2(CB2)选择性受体定位和密度的用途,优选在中枢神经系统(CNS),周围神经系统(PNS),心脏,肝脏,胃肠道 肠,脾,胰腺,肾,睾丸,卵巢和/或前列腺。 此外,本发明涉及所述化合物在CB2受体相关疾病的诊断,预防和/或治疗中的用途。

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