COMPOSITIONS AND METHODS FOR TREATING MULTIPLE MYELOMA

    公开(公告)号:WO2017030987A9

    公开(公告)日:2018-07-12

    申请号:PCT/US2016046856

    申请日:2016-08-12

    IPC分类号: C07D471/04 C07D401/12

    CPC分类号: C07C311/51 C07B2200/05

    摘要: In one aspect, the present invention provides a method of inhibiting proliferation of a multiple myeloma cell, the method comprising contacting the cell with BRD9647, thereby inhibiting proliferation of the cell. In another aspect, the present invention provides a method of treating multiple myeloma in a pre-selected subject, the method comprising administering an effective amount of BRD9647 to the subject, wherein the subject is pre-selected by detecting a mutation in an AZIN1 polynucleotide or polypeptide relative to a reference in a biological sample obtained from the subject. In another aspect, the present invention provides a method of modulating benzoylation of an agent in a cell, the method comprising contacting the cell with BRD9647, thereby modulating benzoylation of an agent in the cell.

    FUNCTIONALLY MODIFIED POLYPEPTIDES AND RADIOBIOSYNTHESIS
    4.
    发明申请
    FUNCTIONALLY MODIFIED POLYPEPTIDES AND RADIOBIOSYNTHESIS 审中-公开
    功能性修饰的多肽和放射性合成酶

    公开(公告)号:WO2018045376A2

    公开(公告)日:2018-03-08

    申请号:PCT/US2017/050082

    申请日:2017-09-05

    申请人: IKARIA INC.

    发明人: DIMAGNO, Stephen

    IPC分类号: C12P21/02 C12N9/00

    摘要: Provided herein are compositions and methods for generating polypeptides using non-natural amino acids (nnAAs) and genetic machinery, wherein the modified polypeptides, such as therapeutic polypeptides, bind to albumin, such as serum albumin. Methods of substituting a non-natural amino acid in a first polypeptide to obtain a modified polypeptide, the nnAA in some instances comprising an albumin targeting group, are disclosed, as are methods for making populations of such modified polypeptides. A therapeutic polypeptide, interleukin-1 receptor antagonist (IL-1RA) is exemplified using the disclosed methods.

    摘要翻译: 本文提供了使用非天然氨基酸(nnAAs)和遗传机制产生多肽的组合物和方法,其中修饰的多肽例如治疗性多肽与白蛋白例如血清白蛋白结合。 公开了取代第一多肽中的非天然氨基酸以获得修饰多肽的方法,其中nnAA在一些情况下包含白蛋白靶向基团,以及用于制备此类修饰多肽的群体的方法。 使用所公开的方法来举例说明治疗性多肽白细胞介素-1受体拮抗剂(IL-1RA)。

    RADIOFLUORINATED CARBOXIMIDAMIDES AS IDO TARGETING PET TRACER FOR CANCER IMAGING
    5.
    发明申请
    RADIOFLUORINATED CARBOXIMIDAMIDES AS IDO TARGETING PET TRACER FOR CANCER IMAGING 审中-公开
    作为IDO靶向PET示踪剂用于癌变成像的放射性氟代甲亚胺酰胺

    公开(公告)号:WO2018039430A1

    公开(公告)日:2018-03-01

    申请号:PCT/US2017/048370

    申请日:2017-08-24

    摘要: Radiofluorinated carboximidamides are disclosed as selective IDO enzyme radioligands and generate specific binding in accordance with IDO expression in vitro. MicroPET experiments indicate [ 18 F]IDO49 specifically accumulate in IDO-expressing tumors which confirmed by Western blot and IHC analysis supported. Using Hela tumor bearing models with IFN-γ treatment confirmed that [ 18 F]IDO49 accumulation in the IFN- γ treatment tumor mouse. These results can have implications that [ 18 F]IDO49 has substantial potential as an imaging agent that targets IDO in tumors.

    摘要翻译: 作为选择性IDO酶放射性配体公开了放射性氟代羧酰亚胺,并根据体外IDO表达产生特异性结合。 MicroPET实验表明[18 F] IDO49特异性积累在表达IDO的肿瘤中,这通过Western印迹和IHC分析证实得到证实。 使用带有IFN-γ处理的Hela肿瘤模型证实在IFN-γ治疗肿瘤小鼠中[18 F] IDO49积累。 这些结果可能意味着[18 F] IDO49具有作为靶向肿瘤中IDO的显像剂的巨大潜力。

    TRACER SUBSTANCES FOR SVC ANALYSIS
    8.
    发明申请
    TRACER SUBSTANCES FOR SVC ANALYSIS 审中-公开
    用于SVC分析的追踪物质

    公开(公告)号:WO2017008815A1

    公开(公告)日:2017-01-19

    申请号:PCT/DK2016/050244

    申请日:2016-07-08

    申请人: TWO TEKNIK APS

    摘要: The present invention relates to novel tracer substances useful in the analysis for semi-volatile organic contaminants (SVCs) such as PCBs (polychlorinated biphenyls). The invention also describes methods for establishing multilayered sealant barriers towards SVCs, which barriers contain said tracer substances, and methods for assessing the integrity of such barriers.

    摘要翻译: 本发明涉及可用于分析半挥发性有机污染物(SVC)如PCB(多氯联苯)的新型示踪剂物质。 本发明还描述了建立针对SVC的多层密封剂屏障的方法,该障碍物包含所述示踪剂物质,以及评估这种障碍物的完整性的方法。