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    IMPROVED METHODS FOR TREATING HER2-POSITIVE BREAST CANCER
    1.
    发明申请
    IMPROVED METHODS FOR TREATING HER2-POSITIVE BREAST CANCER 审中-公开
    改进的治疗HER2阳性乳腺癌的方法

    公开(公告)号：WO2017100663A1

    公开(公告)日：2017-06-15

    申请号：PCT/US2016/065955

    申请日：2016-12-09

    申请人： EXPRESSION PATHOLOGY, INC.

    发明人： BLACKLER, Adele ,  HEMBROUGH, Todd ,  CECCHI, Fabiola ,  NUCIFORD, Paulo

    IPC分类号： G01N33/48 ,  G01N30/72 ,  C12Q1/68

    CPC分类号： A61K31/517 ,  A61K39/3955 ,  A61K45/06 ,  G01N33/57415 ,  G01N33/5748 ,  G01N33/6848 ,  G01N2333/71 ,  G01N2333/91205 ,  G01N2560/00

    摘要： Methods of treating breast cancer are provided where a quantitative Her2 assay is used to identify whether a breast tumor will be responsive to treatment with anti-Her2 therapeutic agents such as lapatinib and trastuzumab, followed by selection of a suitable treatment regimen and administration of the regimen. A specific Her2 fragment peptide is precisely quantitated by SRM-mass spectrometry directly in breast tumor cells collected from breast tumor tissue that was obtained from a cancer patient and compared to a reference level in order to determine if the breast cancer patient will positively respond to treatment with a therapeutic agent that specifically targets the Her2 protein.

    摘要翻译： 提供了治疗乳腺癌的方法，其中使用定量Her2测定法来鉴定乳腺肿瘤是否将对用抗-Her2治疗剂如拉帕替尼和曲妥珠单抗的治疗有反应，随后选择 适合的治疗方案和给药方案。 通过SRM质谱法直接在从癌症患者获得的乳腺肿瘤组织收集的乳腺肿瘤细胞中精确定量特定的Her2片段肽，并与参考水平比较以确定乳腺癌患者是否将对治疗产生积极响应 用特异性靶向Her2蛋白的治疗剂。

    METHODS FOR MEASUREMENT OF INHIBITION OF C-JUN N-TERMINAL KINASE IN SKIN
    2.
    发明申请
    METHODS FOR MEASUREMENT OF INHIBITION OF C-JUN N-TERMINAL KINASE IN SKIN 审中-公开
    C-JUN N末端激酶在皮肤中的抑制测定方法

    公开(公告)号：WO2016100308A1

    公开(公告)日：2016-06-23

    申请号：PCT/US2015/065767

    申请日：2015-12-15

    申请人： SIGNAL PHARMACEUTICALS, LLC

    发明人： HORAN, Gerald Scott, Barden ,  YE, Ying

    IPC分类号： C07D239/48

    CPC分类号： G01N33/6881 ,  A61K9/0053 ,  A61K31/505 ,  G01N33/5008 ,  G01N33/5082 ,  G01N2333/4706 ,  G01N2333/91205 ,  G01N2440/14 ,  G01N2800/20 ,  G01N2800/52

    摘要： Provided herein are methods for evaluating the effect of 2-( tert -butylamino)-4- ((1R,3R,4R)-3-hydroxy-4-methylcyclohexylamino)-pyrimidine-5-carboxamide or a pharmaceutically acceptable stereoisomer, tautomer, solid form, polymorph, salt, hydrate, clathrate, or solvate thereof in a patient with an assay based on UVB-irradiation and phosphorylated c-Jun expression. The analyses allow for evaluation of dose-response and identification of patient populations who are sensitive to 2-( tert -butylamino)-4-((1R,3R,4R)-3- hydroxy-4-methylcyclohexylamino)-pyrimidine-5-carboxamide or a pharmaceutically acceptable stereoisomer, tautomer, solid form, polymorph, salt, hydrate, clathrate, or solvate thereof.

    摘要翻译： 本文提供了评价2-（叔丁基氨基）-4-（（1R，3R，4R）-3-羟基-4-甲基环己基氨基） - 嘧啶-5-甲酰胺或其药学上可接受的立体异构体互变异构体， 固体形式，多晶型物，盐，水合物，包合物或溶剂合物在基于UVB照射和磷酸化c-Jun表达的测定的患者中。 该分析允许评价对2-（叔丁基氨基）-4 - （（1R，3R，4R）-3-羟基-4-甲基环己基氨基） - 嘧啶-5-基 甲酰胺或其药学上可接受的立体异构体，互变异构体，固体形式，多晶型物，盐，水合物，包合物或溶剂合物。

    PKC DELTA INHIBITORS FOR USE AS THERAPEUTICS
    8.
    发明申请
    PKC DELTA INHIBITORS FOR USE AS THERAPEUTICS 审中-公开
    PKC DELTA抑制剂用作治疗药物

    公开(公告)号：WO2014047328A3

    公开(公告)日：2015-07-16

    申请号：PCT/US2013060683

    申请日：2013-09-19

    申请人： FALLER DOUGLAS V ,  WILLIAMS ROBERT M

    发明人： FALLER DOUGLAS V ,  WILLIAMS ROBERT M

    IPC分类号： A01N43/16 ,  A61K31/35 ,  C07D311/00

    CPC分类号： A61K31/403 ,  A61K9/0019 ,  A61K31/404 ,  A61K45/06 ,  C07D209/86 ,  C07D405/06 ,  C07D487/14 ,  C12Y207/10002 ,  G01N33/5011 ,  G01N2333/91205

    摘要： The invention directed to compounds that are specific inhibitors of PKC delta, and methods and compositions for the treatment and prevent of cancers and other disorders. Compositions comprising compounds of the invention are used to treat cancers such as, for example, carcinoid and neuroendocrine tumors, malignant melanomas, pancreatic, gastrointestinal and lung cancers. Neuroendocrine tumor cell lines of pulmonary and gastrointestinal origin are surprisingly sensitive to PKC delta inhibition by the compounds of the invention. The invention is further directed to methods, compositions and kits containing compounds of the formulas (Ia), (Ib), (IIa), (IIb), (IIIa), (IIIb), (IVa), (IVb), and (V) as disclosed and described in Figures 11 and 12.

    摘要翻译： 本发明涉及作为PKCδ特异性抑制剂的化合物，以及用于治疗和预防癌症和其它疾病的方法和组合物。 包含本发明化合物的组合物用于治疗癌症例如类癌和神经内分泌肿瘤，恶性黑素瘤，胰腺癌，胃肠癌和肺癌。 肺和胃肠道起源的神经内分泌肿瘤细胞系对本发明化合物对PKCδ抑制的惊人的敏感性。 本发明还涉及包含式（Ia），（Ib），（IIa），（IIb），（IIIa），（IIIb），（IVa），（IVb）和（IVb） V），如图11和12所示。