NOVEL PYRROLOPYRIMIDINE COMPOUNDS AS INHIBITORS OF PROTEIN KINASES

    公开(公告)号:US20170224689A1

    公开(公告)日:2017-08-10

    申请号:US15435722

    申请日:2017-02-17

    Abstract: The present invention relates to certain pyrrolopyrimidine derivatives, pharmaceutical compositions containing them, and methods of using them, including methods for the treatment of proliferation disorders and other diseases related to the dysregulation of kinase (such as, but not limited to, EGFR (including HER), Alk, PDGFR, BLK, BMX/ETK, BTK, FLT3(D835Y), ITK, JAK1, JAK2, JAK3, TEC and TXK) and/or the respective pathways.

    Real-time electronic cell sensing system and applications for cytotoxicity profiling and compound assays
    13.
    发明授权
    Real-time electronic cell sensing system and applications for cytotoxicity profiling and compound assays 有权
    实时电子细胞感测系统及其细胞毒性分析和化合物分析的应用

    公开(公告)号:US09399787B2

    公开(公告)日:2016-07-26

    申请号:US13720124

    申请日:2012-12-19

    Abstract: A method of performing an assay of a response of two or more cell types to a test compound, including: providing a device for monitoring cell-substrate impedance, adding at least two different cell types to the device; adding at least one test compound to form at least two test compound wells; providing at least two control wells; monitoring impedance of the at least two test compound wells and of the at least two control wells at three or more time points after adding the at least one test compound; and analyzing measured impedance from the at least two test compound wells and from the at least two control wells at the three or more time points to obtain information on the response of the different cell types to the at least one test compound.

    Abstract translation: 一种对测试化合物进行两种或多种细胞类型的反应测定的方法,包括:提供用于监测细胞 - 基底阻抗的装置,向装置添加至少两种不同的细胞类型; 加入至少一种测试化合物以形成至少两个测试化合物孔; 提供至少两个对照孔; 在加入至少一种测试化合物之后,在三个或更多个时间点监测所述至少两个测试化合物孔和所述至少两个对照孔的阻抗; 以及在所述三个或更多个时间点分析来自所述至少两个测试化合物孔和所述至少两个对照孔的测量阻抗,以获得关于所述不同细胞类型对所述至少一种测试化合物的响应的信息。

    CO-CULTURE DEVICE ASSEMBLY
    15.
    发明申请
    CO-CULTURE DEVICE ASSEMBLY 有权
    文化设备组合

    公开(公告)号:US20130143254A1

    公开(公告)日:2013-06-06

    申请号:US13309209

    申请日:2011-12-01

    Abstract: An insert device and co-culture device assembly incorporating the insert device, which includes an insert chamber with two fluid impermeable side walls that extend from a microporous bottom to an open top to form an inner cavity. The first side wall is shaped to form a convex arc that follows between about half of a circumference of the well and less than an entire circumference of the well. The second side wall joins ends of the first side wall and protrudes inward towards a center of the convex arc. A flange extends outward from or beneath the top and is notched to form a gap adjacent to the second side wall, which forms an access port allowing access to the lower chamber with a micropipette tip when the insert device is inserted into a well of a single or multi-well plate.

    Abstract translation: 包括插入装置的插入装置和共培养装置组件,其包括具有从微孔底部延伸到开口顶部以形成内腔的两个流体不可渗透侧壁的插入室。 第一侧壁成形为形成沿着井的圆周的大约一半且小于井的整个圆周的凸弧。 第二侧壁连接第一侧壁的端部并朝向凸弧的中心向内突出。 凸缘从顶部向下或从顶部向外延伸并且被切口以形成与第二侧壁相邻的间隙,当形成插入装置插入到单个孔中时,形成允许通过微量移液管尖端进入下腔室的进入口 或多孔板。

    REAL-TIME ELECTRONIC CELL SENSING SYSTEM AND APPLICATIONS FOR CYTOTOXICITY PROFILING AND COMPOUND ASSAYS
    16.
    发明申请
    REAL-TIME ELECTRONIC CELL SENSING SYSTEM AND APPLICATIONS FOR CYTOTOXICITY PROFILING AND COMPOUND ASSAYS 有权
    实时电子细胞感测系统及其在细胞毒性分析和化合物测定中的应用

    公开(公告)号:US20130123136A1

    公开(公告)日:2013-05-16

    申请号:US13720124

    申请日:2012-12-19

    Abstract: A method of performing an assay of a response of two or more cell types to a test compound, including: providing a device for monitoring cell-substrate impedance, adding at least two different cell types to the device; adding at least one test compound to form at least two test compound wells; providing at least two control wells; monitoring impedance of the at least two test compound wells and of the at least two control wells at three or more time points after adding the at least one test compound; and analyzing measured impedance from the at least two test compound wells and from the at least two control wells at the three or more time points to obtain information on the response of the different cell types to the at least one test compound.

    Abstract translation: 一种对测试化合物进行两种或多种细胞类型的反应测定的方法,包括:提供用于监测细胞 - 基底阻抗的装置,向装置添加至少两种不同的细胞类型; 加入至少一种测试化合物以形成至少两个测试化合物孔; 提供至少两个对照孔; 在加入至少一种测试化合物之后,在三个或更多个时间点监测所述至少两个测试化合物孔和所述至少两个对照孔的阻抗; 以及在所述三个或更多个时间点分析来自所述至少两个测试化合物孔和所述至少两个对照孔的测量阻抗,以获得关于所述不同细胞类型对所述至少一种测试化合物的响应的信息。

    Impedance based devices and methods for use in assays
    17.
    发明授权
    Impedance based devices and methods for use in assays 有权
    基于阻抗的装置和方法用于测定

    公开(公告)号:US08420363B2

    公开(公告)日:2013-04-16

    申请号:US12325530

    申请日:2008-12-01

    Inventor: Xiaobo Wang Xiao Xu

    Abstract: A device for detecting cells and/or molecules on an electrode surface is disclosed. The device detects cells and/or molecules through measurement of impedance changes resulting from the cells and/or molecules. A disclosed embodiment of the device includes a substrate having two opposing ends along a longitudinal axis. A plurality of electrode arrays are positioned on the substrate. Each electrode array includes at least two electrodes, and each electrode is separated from at least one adjacent electrode in the electrode array by an expanse of non-conductive material. The electrode has a width at its widest point of more than about 1.5 and less than about 10 times the width of the expanse of non-conductive material. The device also includes electrically conductive traces extending substantially longitudinally to one of the two opposing ends of the substrate without intersecting another trace. Each trace is in electrical communication with at least one of the electrode arrays.

    Abstract translation: 公开了一种用于检测电极表面上的电池和/或分子的装置。 该装置通过测量由细胞和/或分子产生的阻抗变化来检测细胞和/或分子。 所述装置的公开实施例包括具有沿着纵向轴线的两个相对端部的基板。 多个电极阵列位于基板上。 每个电极阵列包括至少两个电极,并且每个电极由电极阵列中的至少一个相邻的电极通过一片非导电材料分开。 电极的最宽点处的宽度大于非导电材料的宽度的大约1.5倍且小于约10倍。 该器件还包括基本上纵向延伸到衬底的两个相对端之一的导电迹线,而不与另一迹线相交。 每个迹线与至少一个电极阵列电连通。

    Heterocyclic compounds and uses as anticancer agents
    18.
    发明授权
    Heterocyclic compounds and uses as anticancer agents 有权
    杂环化合物和用作抗癌剂

    公开(公告)号:US08252822B2

    公开(公告)日:2012-08-28

    申请号:US12175154

    申请日:2008-07-17

    CPC classification number: C07D487/04 C07D498/04 C07D513/04

    Abstract: Novel compounds having a fused bicyclic heteroaromatic ring system substituted with a heteroaryl five-membered ring are disclosed. The compounds inhibit growth of a variety of types of cancer cells, and are thus useful for treating cancer. Efficacy of these compounds is demonstrated with a system for monitoring cell growth/migration, which shows they are potent inhibitors of growth and/or migration of cancer cells. In addition, compounds of the invention were shown to stop growth of tumors in vivo, and to reduce the size of tumors in vivo. Compositions comprising these compounds, and methods to use these compounds and compositions for treatment of cancers, are disclosed.

    Abstract translation: 公开了具有被杂芳基五元环取代的稠合双环杂芳环系的新型化合物。 这些化合物抑制多种类型的癌细胞的生长,因此可用于治疗癌症。 通过用于监测细胞生长/迁移的系统来证明这些化合物的功效,这表明它们是癌细胞的生长和/或迁移的有效抑制剂。 此外,本发明的化合物被证明可以在体内停止肿瘤生长,并减少体内肿瘤的大小。 公开了包含这些化合物的组合物,以及使用这些化合物和用于治疗癌症的组合物的方法。

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