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    PROSTATE CANCER PROGNOSTIC COMPOSITIONS AND KITS
    92.
    发明申请
    PROSTATE CANCER PROGNOSTIC COMPOSITIONS AND KITS 审中-公开

    公开(公告)号：US20180223375A1

    公开(公告)日：2018-08-09

    申请号：US15924040

    申请日：2018-03-16

    Applicant: Stichting Katholieke Universiteit, The University Medical Centre Nijmegen

    Inventor： Daphne Hessels ,  Gerald Verhaegh ,  Jack A. Schalken ,  J. Alfred Witjes

    IPC: C12Q1/6886 ,  G01N33/574

    Abstract: Described herein are method, compositions and kits for prognosis of prostate cancer. The methods include determining the ratio of PCA3 and of a prostate-specific marker expression in a urine sample and correlating the value of the PCA3/prostate-specific marker ratio with the aggressiveness and mortality risk of prostate cancer in the subject. The method for prognosing prostate cancer in a sample of a patient includes assessing the amount of a prostate cancer specific PCA3 mRNA and the amount of prostate-specific marker in the sample; determining a ratio value of this amount of prostate cancer specific PCA3 mRNA over the amount of prostate-specific marker; comparing the ratio value to at least one predetermined cut-off value, wherein a ratio value above the predetermined cut-off value is indicative of a higher risk of mortality of prostate cancer as compared to a ratio value below the predetermined cut-off value.

    Aminomethylene pyrazolones with therapeutic activity
    96.
    发明授权
    Aminomethylene pyrazolones with therapeutic activity 有权

    公开(公告)号：US09676764B2

    公开(公告)日：2017-06-13

    申请号：US15216884

    申请日：2016-07-22

    Applicant: Compound Handling B.V. ,  Stichting Katholieke Universiteit

    Inventor： Onno Van Hooij ,  Jacobus Antonius Schalken ,  Hendrik Engelbertus Vietor ,  Dennis Patrick Piet ,  Petrus Emmanuel Marie Maas ,  Johann Heinrich Tijhuis ,  Sirik Deerenberg ,  Nanda Elisabeth Sprenkels ,  Siu Ha Tang

    IPC: C07D417/04 ,  C07D417/14 ,  A61K31/428 ,  A61K31/454 ,  A61K31/4184 ,  A61K45/06 ,  C07D403/04

    CPC classification number: C07D403/04 ,  A61K31/4155 ,  A61K31/4184 ,  A61K31/428 ,  A61K31/454 ,  A61K45/06 ,  C07D417/04 ,  C07D417/14

    Abstract: A compound having the structure according to formula III wherein: X is NH or S; R1 is H or (1C-4C)alkyl; R2 is (1C-4C)alkyl, phenyl or a monocyclic aromatic ring having one or more N-, O- or S-atoms in the ring, which alkyl, phenyl or aromatic ring is optionally substituted with one or more groups selected from (1C-4C)alkyl, (1C-4C)alkyloxy, halo(1C-4C)alkyl, halo(1C-4C)alkyloxy, phenyloxy, phenylthio, halogen, or nitro; R3 and R4 are each independently H, (1C-6C)alkyl, (2C-6C) alkenyl, (2C-6C)alkynyl, cyano, (3C-6C)cycloalkyl, phenyl, a monocyclic aromatic ring having one or more N-, O- or S-atoms in the ring, a monocyclic non-aromatic ring having one or more N-, O- or S-atoms in the ring, each optionally substituted with hydroxyl, (1C-4C)alkoxy, phenyl, cycloalkyl, piperidyl, piperazinyl, furyl, thienyl, pirazinyl, pyrrolyl, 2H-pyrrolyl, pyrazolyl, isoxazolyl, isothiazolyl, pyrrolidonyl, pyrrolinyl, imidazolinyl, imidazolyl, a monocyclic aromatic ring having one or more N-, O- or S-atoms in the ring, whereby each of these optional substituents is optionally further substituted with (1C-4C)alkyl, (1C-4C)alkyloxy, halo(1C-4C)alkyl, halo(1C-4C)alkyloxy, halogen, nitro or (1C-2C)dioxol forming a ring; or R3 and R4 form together pyrrolyl, imidazolyl, pyrazolyl, pyrrolidinyl, pyrrolinylimidazolidinyl, imidazolinyl, piperidyl, piperazinylmorpholinyl, each optionally substituted with (1C-6C)alkyl, phenyl(1C-4C)alkyl, phenylketo(1C-4C)alkyl; R5 is H, Cl, F, Br, Me, NO2, t-butyl, OCF3, OCH3, CF3; R6 is H, (1C-4C)alkyl, (1C-4C)alkyloxy, halo(1C-4C)alkyl, halo(1C-4C)alkyloxy, nitro or halogen; R7 is H, F, Cl, Br, Me, NO2, t-butyl, OCF3, OCH3, CF3; or pharmaceutically acceptable addition salts thereof for use in treatments of carcinoma, in particular, to delay, prevent or reverse metastasis in prostate cancer.

    COMPUTER-IMPLEMENTED METHOD OF ANALYSING DATA FROM MEASURED VALUES OF CHARACTERISTICS OF OBJECTS IN SAMPLES
    97.
    发明申请
    COMPUTER-IMPLEMENTED METHOD OF ANALYSING DATA FROM MEASURED VALUES OF CHARACTERISTICS OF OBJECTS IN SAMPLES 审中-公开
    计算机实验方法从样品中特征对象的测量值分析数据

    公开(公告)号：US20170003212A1

    公开(公告)日：2017-01-05

    申请号：US15106064

    申请日：2014-12-18

    Applicant: STICHTING KATHOLIEKE UNIVERSITEIT, MORE PARTICULA- RLY THE FACULTY OF SCIENCE OF RADBOUD UNIVERSITY ,  UNIVERSITY MEDICAL CENTER UTRECHT TE UTRECHT

    Inventor： Jeroen JANSE ,  Lutgarde BUYDENS ,  Leo KOENDERMAN ,  Bart HILVERING ,  Oscar VAN DEN BRINK

    IPC: G01N15/10

    CPC classification number: G01N15/10 ,  G01N15/1429 ,  G01N2015/1006 ,  G01N2015/1402 ,  G06K9/0014 ,  G06K9/6247 ,  G16B15/00 ,  G16H50/20

    Abstract: The invention relates to a computer implemented method of analysing data comprising measured values of characteristics of objects in samples, the data comprising —a first set of data (Xireference) with measured values of characteristics of objects in reference samples; —a test set of data (Xitest) with measured values of the characteristics of objects in a test sample; characterised by the method comprising; —fitting a control model to the first set of data to determine control loadings (Pcontrol) each representing an independent correlation between characteristics; —projecting the first set of data (Xireference) onto the control loadings (Pcontrol) for determining a first set control scores (Tcontrol,ireference) and determining one or more confidence intervals for the first set of control scores (Tcontrol,ireference); —projecting the test data onto the control loadings (Pcontrol) for determining test control scores; —determining if the test control scores are within one or more the confidence intervals.

    Abstract translation: 本发明涉及一种分析数据的计算机实现方法，该数据包括样本中对象的特征的测量值，该数据包括 - 具有参考样本中对象特征的测量值的第一数据集（Xireference） - 测试样本中的对象特征的测量值（Xitest）的测试集合; 其特征在于该方法包括： 将控制模型拟合到第一组数据，以确定每个表示特性之间的独立相关性的控制负载（Pcontrol）; - 将第一组数据（Xireference）投影到控制负载（Pcontrol）上，以确定第一组控制分数（Tcontrol，ireference）并确定第一组控制分数（Tcontrol，ireference）的一个或多个置信区间; 将测试数据投影到控制负载（Pcontrol）上，以确定测试控制分数; - 确定测试控制分数是否在一个或多个置信区间内。

    Aminomethylene pyrazolones with therapeutic activity
    99.
    发明授权
    Aminomethylene pyrazolones with therapeutic activity 有权
    具有治疗活性的氨基亚甲基吡唑啉酮

    公开(公告)号：US09453012B2

    公开(公告)日：2016-09-27

    申请号：US14383083

    申请日：2013-03-05

    Applicant: Compound Handling B.V. ,  Stichting Katholieke Universiteit

    Inventor： Onno Van Hooij ,  Jacobus Antonius Schalken ,  Hendrik Engelbertus Vietor ,  Dennis Patrick Piet ,  Petrus Emmanuel Marie Maas ,  Johann Heinrich Tijhuis ,  Sirik Deerenberg ,  Nanda Elisabeth Sprenkels ,  Siu Ha Tang

    IPC: A61K31/454 ,  A61K31/428 ,  C07D417/04 ,  C07D417/14

    CPC classification number: C07D403/04 ,  A61K31/4155 ,  A61K31/4184 ,  A61K31/428 ,  A61K31/454 ,  A61K45/06 ,  C07D417/04 ,  C07D417/14

    Abstract: A compound having the structure according to formula III wherein: X is NH or S; R1 is H or (1C-4C)alkyl; R2 is (1C-4C)alkyl, phenyl or a monocyclic aromatic ring having one or more N—, O— or S— atoms in the ring, which alkyl, phenyl or aromatic ring is optionally substituted with one or more groups selected from (1C-4C)alkyl, (1C-4C)alkyloxy, halo(1C-4C)alkyl, halo(1C-4C)alkyloxy, phenyloxy, phenylthio, halogen, or nitro; R3 and R4 are each independently H, (1C-6C)alkyl, (2C-6C) alkenyl, (2C-6C)alkynyl, cyano, (3C-6C)cycloalkyl, phenyl, a monocyclic aromatic ring having one or more N—, O— or S— atoms in the ring, a monocyclic non-aromatic ring having one or more N—, O— or S— atoms in the ring, each optionally substituted with hydroxyl, (1C-4C)alkoxy, phenyl, cycloalkyl, piperidyl, piperazinyl, furyl, thienyl, pirazinyl, pyrrolyl, 2H-pyrrolyl, pyrazolyl, isoxazolyl, isothiazolyl, pyrrolidonyl, pyrrolinyl, imidazolinyl, imidazolyl, a monocyclic aromatic ring having one or more N—, O— or S— atoms in the ring, whereby each of these optional substituents is optionally further substituted with (1C-4C)alkyl, (1C-4C)alkyloxy, halo(1C-4C)alkyl, halo(1C-4C)alkyloxy, halogen, nitro or (1C-2C)dioxol forming a ring; or R3 and R4 form together pyrrolyl, imidazolyl, pyrazolyl, pyrrolidinyl, pyrrolinylimidazolidinyl, imidazolinyl, piperidyl, piperazinylmorpholinyl, each optionally substituted with (1C-6C)alkyl, phenyl(1C-4C)alkyl, phenylketo(1C-4C)alkyl; R5 is H, Cl, F, Br, Me, NO2, t-butyl, OCF3, OCH3, CF3; R6 is H, (1C-4C)alkyl, (1C-4C)alkyloxy, halo(1C-4C)alkyl, halo(1C-4C)alkyloxy, nitro or halogen; R7 is H, F, Cl, Br, Me, NO2, t-butyl, OCF3, OCH3, CF3; or pharmaceutically acceptable addition salts thereof for use in treatments of carcinoma, in particular to delay, prevent or reverse metastasis in prostate cancer.

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