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    COMPOSITIONS AND METHODS FOR FLUID BIOPSY OF MELANOMA
    1.
    发明公开
    COMPOSITIONS AND METHODS FOR FLUID BIOPSY OF MELANOMA 审中-公开

    公开(公告)号：EP3140656A4

    公开(公告)日：2017-11-22

    申请号：EP15788742

    申请日：2015-05-08

    申请人： SCRIPPS RESEARCH INST

    发明人： KUHN PETER ,  VELASCO CARMEN RUIZ

    IPC分类号： G01N33/574 ,  G01N33/50 ,  G01N33/569

    CPC分类号： G01N33/5743 ,  G01N33/56972 ,  G01N33/57488 ,  G01N2333/70589

    摘要： The present invention provides methods for identifying circulating melanoma cells (CMCs) in a biological sample and methods for diagnosing metastatic melanoma in a subject. The methods disclosed can be used on non-enriched blood samples to identify CMC using detectable agents that are specific for a biomarker of CMCs and assessing the morphology of the cells having the detectable agents. The presence or absence of a detectable agent in combination with morphological characteristics of the cells can be used diagnose a subject with metastatic melanoma based on the number of CMCs is present in the sample.

    PHARMACOPHORE FOR TRAIL INDUCTION
    2.
    发明公开
    PHARMACOPHORE FOR TRAIL INDUCTION 审中-公开
    PHARMAKOPHORFÜRTRAIL-INDUKTION

    公开(公告)号：EP3125898A4

    公开(公告)日：2017-08-16

    申请号：EP15772254

    申请日：2015-03-30

    申请人： SCRIPPS RESEARCH INST

    发明人： JANDA KIM D ,  JACOB NICHOLAS T ,  LOCKNER JONATHAN W

    IPC分类号： A61K31/519 ,  A61P35/00 ,  C07D471/14

    CPC分类号： C07D471/14 ,  A61K31/519

    摘要： There are disclosed imidazolinopyrimidinone compounds that have activity to induce TRAIL gene expression in macrophages. There is further disclosed a method for treating various cancers comprising administering effective amounts of an imidazolinopyrimidinone having the structure of Formula I herein.

    摘要翻译： 公开了具有在巨噬细胞中诱导TRAIL基因表达的活性的咪唑啉嘧啶酮化合物。 还公开了一种治疗各种癌症的方法，包括给予有效量的具有本文式I结构的咪唑啉并嘧啶酮。 在各种实施方案中，本发明涉及化合物和药物组合物，其包含有效量的能够在能够表达TRAIL基因的细胞中诱导TRAIL基因表达以产生细胞因子TRAIL的化合物。

    CYCLIC N-ACYL O-AMINO PHENOL CBI DERIVATIVE
    4.
    发明公开
    CYCLIC N-ACYL O-AMINO PHENOL CBI DERIVATIVE 审中-公开
    环化合物N-酰基-α-氨基酚-CBI-衍生物

    公开(公告)号：EP2978760A4

    公开(公告)日：2016-11-16

    申请号：EP14772747

    申请日：2014-03-20

    申请人： SCRIPPS RESEARCH INST

    发明人： BOGER DALE L

    IPC分类号： C07D413/14 ,  A61K31/5365 ,  C07D209/04 ,  C07D498/04 ,  C07D498/06 ,  C07D519/00

    CPC分类号： C07D498/06 ,  A61K31/5365 ,  C07D519/00

    摘要： A group of cyclic N-acyl O-amino phenol CBI derivatives were synthesized and shown to be pro-drugs, subject to reductive activation by cleavage of a N-0 bond, effectively releasing the free drug in functional in vitro cellular assays for cytotoxic activity approaching the activity of the free drug, yet remain essentially stable to ex vivo DNA alkylation conditions. Assessment of the in vivo antitumor activity of a representative pro-drug indicates that a contemplated pro-drug approaches the potency and exceeds the efficacy of the free drug itself (CBI-indole2), indicating that the inactive pro-drugs not only effectively release the free drug in vivo, but that they offer additional advantages related to a controlled or targeted release in vivo.

    POLYMERIZATION METHOD AND POLYMERS FORMED THEREWITH
    10.
    发明公开
    POLYMERIZATION METHOD AND POLYMERS FORMED THEREWITH 有权
    聚对苯二甲酸丁二醇酯共聚物（DARAUS HERGESTELLTE POLYMERE）

    公开(公告)号：EP2925803A4

    公开(公告)日：2016-06-29

    申请号：EP13860053

    申请日：2013-12-03

    申请人： SCRIPPS RESEARCH INST

    发明人： DONG JIAJIA ,  FOKIN VALERY ,  KRASNOVA LARISA ,  KWISNEK LUKE R ,  OAKDALE JAMES S ,  SHARPLESS K BARRY

    IPC分类号： C08G65/40

    CPC分类号： C08G75/00 ,  C08G64/06 ,  C08G64/24 ,  C08G65/40 ,  C08G65/4012 ,  C08G2650/40 ,  C08J5/18 ,  C08J2369/00 ,  C08J2381/00

    摘要： Condensation of fluoro-substituted and silyl-substituted monomers provides polymers suitable for use, e.g., as engineering polymers. A monomer composition is condensed in the presence of a basic catalyst. The monomer composition contains a compound of formula F—X—F and a compound of formula (R1)3Si—Z—Si(R1)3, and forms an alternating X—Z polymer chain and a silyl fluoride byproduct. X has the formula -A(-R2-A)n-; each A is SO2, C(═O), or Het; R2 is an organic moiety; n is 0 or 1; Het is an aromatic nitrogen heterocycle; Z has the formula -L-R3-L-; each L is O, S, or N(R4); and each R3 is an organic moiety, and R4 comprises H or an organic moiety.

    摘要翻译： 氟取代的和甲硅烷基取代的单体的缩合提供适用于例如工程聚合物的聚合物。 单体组合物在碱性催化剂存在下缩合。 单体组合物含有式F-X-F化合物和式（R1）3Si-Z-Si（R1）3化合物，形成交替的X-Z聚合物链和甲硅烷基氟化物副产物。 X具有式-A（-R 2-A）n - ; 每个A是SO 2，C（= O）或Het; R2是有机部分; n为0或1; Het是芳香族氮杂环; Z具有式-L-R 3 -L-; 每个L为O，S或N（R4）; 并且每个R 3是有机部分，并且R 4包含H或有机部分。