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公开(公告)号：US20150087673A1
公开(公告)日：2015-03-26
申请号：US14498921
申请日：2014-09-26
IPC分类号： A61K31/4545 , C07D401/14 , A61K45/06 , G01N33/573
CPC分类号： A61K31/4545 , A61K31/4427 , A61K31/501 , A61K31/5377 , A61K45/06 , C07D401/14 , G01N33/573 , G01N2500/04 , A61K2300/00
摘要： Disclosed are methods of using AMPK-activating compounds, for example, in the treatment of cancer and disorders of vascular flow. Also disclosed are biomarkers for AMPK and uses thereof, for example, in the diagnosis and treatment of AMPK-linked disorders. In certain embodiments, the AMPK-activating compounds have the structural formula wherein E, J, T, D1, D2, D3, the ring system denoted by “B”, T, R3, R4, w and x are as described herein.
摘要翻译： 公开了使用AMPK活化化合物的方法，例如用于治疗癌症和血管流动障碍。 还公开了AMPK的生物标志物及其用途，例如在AMPK相关疾病的诊断和治疗中。 在某些实施方案中，AMPK活化化合物具有其结构式，其中E，J，T，D1，D2，D3，由“B”，T，R3，R4，w和x表示的环系统如本文所述。
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公开(公告)号：US09005909B2
公开(公告)日：2015-04-14
申请号：US13333817
申请日：2011-12-21
IPC分类号： G01N33/573 , G01N33/49 , G01N33/53
CPC分类号： G01N33/573 , G01N33/49 , G01N33/4915 , G01N33/5041 , G01N33/53 , G01N2333/912 , G01N2333/91205 , G01N2800/02
摘要： A method of sample analysis is provided. In certain embodiments, the method comprises: a) labeling cells of a blood sample using an antibody that specifically binds to phospho-AMPK or a phosphorylated target thereof, to produce a labeled sample; and b) measuring antibody binding by a population of blood cells of the labeled sample using flow cytometry. In particular embodiments, the method may further comprise, prior to the labeling step: contacting blood with a test agent ex vivo or in vivo; and comparing the evaluation to results obtained from a reference sample of blood cells.
摘要翻译： 提供了样品分析的方法。 在某些实施方案中，所述方法包括：a）使用特异性结合磷酸化AMPK或其磷酸化靶标的抗体标记血液样品的细胞，以产生标记的样品; 和b）使用流式细胞术测量标记样品的血细胞群体的抗体结合。 在具体实施方案中，该方法还可以包括在标记步骤之前：离体或体内使血液与测试试剂接触; 并将评估与从血细胞的参考样品获得的结果进行比较。
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公开(公告)号：US20120178098A1
公开(公告)日：2012-07-12
申请号：US13333817
申请日：2011-12-21
IPC分类号： G01N21/64 , G01N33/573
CPC分类号： G01N33/573 , G01N33/49 , G01N33/4915 , G01N33/5041 , G01N33/53 , G01N2333/912 , G01N2333/91205 , G01N2800/02
摘要： A method of sample analysis is provided. In certain embodiments, the method comprises: a) labeling cells of a blood sample using an antibody that specifically binds to phospho-AMPK or a phosphorylated target thereof, to produce a labeled sample; and b) measuring antibody binding by a population of blood cells of the labeled sample using flow cytometry. In particular embodiments, the method may further comprise, prior to the labeling step: contacting blood with a test agent ex vivo or in vivo; and comparing the evaluation to results obtained from a reference sample of blood cells.
摘要翻译： 提供了样品分析的方法。 在某些实施方案中，所述方法包括：a）使用特异性结合磷酸化AMPK或其磷酸化靶标的抗体标记血液样品的细胞，以产生标记的样品; 和b）使用流式细胞术测量标记样品的血细胞群体的抗体结合。 在具体实施方案中，该方法还可以包括在标记步骤之前：离体或体内使血液与测试试剂接触; 并将评估与从血细胞的参考样品获得的结果进行比较。
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公开(公告)号：US08410093B2
公开(公告)日：2013-04-02
申请号：US12951949
申请日：2010-11-22
申请人： Hui Li , Ankush Argade , Rajinder Singh , Sambaiah Thota , David Carroll , Kin Tso , Vanessa Taylor , John McLaughlin , Vadim Markovtsov
发明人： Hui Li , Ankush Argade , Rajinder Singh , Sambaiah Thota , David Carroll , Kin Tso , Vanessa Taylor , John McLaughlin , Vadim Markovtsov
IPC分类号： C07D239/48 , A61K31/506
CPC分类号： C07D239/48 , A61K31/505 , A61K31/506 , C07D205/12 , C07D239/42 , C07D295/155 , C07D401/12 , C07D403/12 , C07D405/12 , C07D413/12 , C07D417/12 , C07D471/08 , C07D487/08
摘要： The present disclosure provides 2,4-pyrimidinediamine compounds having antiproliferative activity, compositions comprising the compounds and methods of using the compounds to inhibit cellular proliferation and to treat proliferate diseases such as tumorigenic cancers.
摘要翻译： 本公开提供具有抗增殖活性的2,4-嘧啶二胺化合物，包含该化合物的组合物和使用该化合物抑制细胞增殖并治疗增殖性疾病如致瘤性癌症的方法。
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公开(公告)号：US07947698B2
公开(公告)日：2011-05-24
申请号：US12053382
申请日：2008-03-21
申请人： Andy Atuegbu , Vadim Markovtsov , Somasekhar Bhamidipati , Rajinder Singh , Vanessa Taylor , Sambaiah Thota , Jeffrey Wayne Clough , David Carroll , Hui Li , Robin Cooper
发明人： Andy Atuegbu , Vadim Markovtsov , Somasekhar Bhamidipati , Rajinder Singh , Vanessa Taylor , Sambaiah Thota , Jeffrey Wayne Clough , David Carroll , Hui Li , Robin Cooper
IPC分类号： C07D239/02 , A01N43/54
CPC分类号： C07D239/48
摘要： The invention encompasses compounds having formula I and the compositions and methods using these compounds in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK3, are therapeutically useful.
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公开(公告)号：US08304422B2
公开(公告)日：2012-11-06
申请号：US12966839
申请日：2010-12-13
申请人： Andy Atuegbu , Vadim Markovtsov , Somasekhar Bhamidipati , Rajinder Singh , Vanessa Taylor , Sambaiah Thota , Jeffrey Wayne Clough , David Carroll , Hui Li , Robin Cooper
发明人： Andy Atuegbu , Vadim Markovtsov , Somasekhar Bhamidipati , Rajinder Singh , Vanessa Taylor , Sambaiah Thota , Jeffrey Wayne Clough , David Carroll , Hui Li , Robin Cooper
IPC分类号： C07D239/02 , A01N43/54
CPC分类号： C07D239/48
摘要： The invention encompasses compounds having formula I and the compositions and methods using these compounds in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK3, are therapeutically useful.
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公开(公告)号：US20110082146A1
公开(公告)日：2011-04-07
申请号：US12966839
申请日：2010-12-13
申请人： Andy Atuegbu , Vadim Markovtsov , Somasekhar Bhamidipati , Rajinder Singh , Vanessa Taylor , Sambaiah Thota , Jeffrey Wayne Clough , David Carroll , Hui Li , Robin Cooper
发明人： Andy Atuegbu , Vadim Markovtsov , Somasekhar Bhamidipati , Rajinder Singh , Vanessa Taylor , Sambaiah Thota , Jeffrey Wayne Clough , David Carroll , Hui Li , Robin Cooper
IPC分类号： A61K31/5377 , A61K31/505 , C07D239/48 , C07D403/02 , A61K31/496 , C07D401/14 , C07D413/02 , A61P37/06 , C12N9/99
CPC分类号： C07D239/48
摘要： The invention encompasses compounds having formula I and the compositions and methods using these compounds in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK3, are therapeutically useful.
摘要翻译： 本发明包括具有式I的化合物和使用这些化合物的组合物和方法用于治疗JAK途径的调节或JAK激酶，特别是JAK3的抑制在治疗上有用的条件。
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公开(公告)号：US08846908B2
公开(公告)日：2014-09-30
申请号：US13119950
申请日：2009-09-23
IPC分类号： C07D239/48 , C07D265/36 , C07D263/62 , C07D413/14 , A61K31/506 , A61K31/538 , A61K31/5383 , A61K31/423 , A61P35/00 , C07D413/12
CPC分类号： C07D417/14 , A61K31/423 , A61K31/506 , A61K31/538 , A61K31/5383 , A61K31/5415 , A61K45/06 , C07D239/48 , C07D263/62 , C07D265/36 , C07D413/12 , C07D413/14
摘要： The present disclosure relates to 2,4-pyrimidinediamines substituted with tricyclic carbamates and the compositions and methods using these compounds in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, such as JAK2 or JAK3, is therapeutically useful.
摘要翻译： 本公开涉及用三环氨基甲酸酯取代的2,4-嘧啶基和使用这些化合物的组合物和方法，用于治疗JAK途径的调节或JAK激酶（例如JAK2或JAK3）的抑制在治疗上有用的条件。
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公开(公告)号：US20110269749A1
公开(公告)日：2011-11-03
申请号：US13119950
申请日：2009-09-23
IPC分类号： A61K31/5415 , C07D413/14 , C07D417/14 , A61K31/506 , A61P3/00 , A61P35/00 , A61P35/02 , A61P37/06 , A61P29/00 , C07D413/12 , A61K31/538
CPC分类号： C07D417/14 , A61K31/423 , A61K31/506 , A61K31/538 , A61K31/5383 , A61K31/5415 , A61K45/06 , C07D239/48 , C07D263/62 , C07D265/36 , C07D413/12 , C07D413/14
摘要： The present disclosure relates to 2,4-pyrimidinediamines substituted with tricyclic carbamates and the compositions and methods using these compounds in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, such as JAK2 or JAK3, is therapeutically useful.
摘要翻译： 本公开涉及用三环氨基甲酸酯取代的2,4-嘧啶基和使用这些化合物的组合物和方法，用于治疗JAK途径的调节或JAK激酶（例如JAK2或JAK3）的抑制在治疗上有用的条件。
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公开(公告)号：US20110027856A1
公开(公告)日：2011-02-03
申请号：US12902052
申请日：2010-10-11
申请人： Hui Li , Vanessa Taylor , Somasekhar Bhamidipati , John Ramphal , Kin Tso , Arvinder Sran , Holger Keim , Vadim Markovtsov , David Carroll , Sambaiah Thota , Ankush Argade , Jeffrey Wayne Clough , Rajinder Singh , Robin Cooper
发明人： Hui Li , Vanessa Taylor , Somasekhar Bhamidipati , John Ramphal , Kin Tso , Arvinder Sran , Holger Keim , Vadim Markovtsov , David Carroll , Sambaiah Thota , Ankush Argade , Jeffrey Wayne Clough , Rajinder Singh , Robin Cooper
IPC分类号： C12N9/99
CPC分类号： A61K31/506 , A61K31/5375 , A61K31/538 , A61K31/5383 , C07D239/48 , C07D239/49 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D491/04 , C07D498/04
摘要： The invention encompasses compounds having formula I and the compositions and methods using these compounds in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK3, are therapeutically useful.
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