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1.发明申请Compounds having inhibitive activity of phosphatidylinositol 3-kinase and methods of use thereof 审中-公开具有磷脂酰肌醇3-激酶抑制活性的化合物及其使用方法公开(公告)号：US20070010548A1
公开(公告)日：2007-01-11
申请号：US10560591
申请日：2004-06-14
申请人： Beth Drees , Leena Chakravarty , Glenn Prestwich , Gyorgy Dorman , Mariann Kavecz , Andras Lukacs , Laszlo Urge , Ferenc Darvas , Piotr Rzepecki , Colin Ferguson
发明人： Beth Drees , Leena Chakravarty , Glenn Prestwich , Gyorgy Dorman , Mariann Kavecz , Andras Lukacs , Laszlo Urge , Ferenc Darvas , Piotr Rzepecki , Colin Ferguson
IPC分类号： A61K31/4745 , C07D471/02 , C12Q1/48
CPC分类号： C07D471/04 , C12Q1/485 , G01N2500/02
摘要： Compounds inhibiting phosphatidylinositol 3-kinase (PI 3-K) activities and methods of preparing and using thereof in treating diseases are disclosed. Compounds inhibiting PI 3-K activity and methods of using PI 3-K inhibitory compounds to inhibit cancer cell grwoth or to treat disorders of immunity and inflammation, in which PI 3-K plays a role in leukocyte function are also provided.
摘要翻译： 公开了抑制磷脂酰肌醇3-激酶（PI 3-K）活性的化合物及其制备及其在治疗疾病中的应用的方法。 还提供了抑制PI3-K活性的化合物和使用PI 3-K抑制化合物抑制癌细胞凋亡或治疗PI3-K在白细胞功能中起作用的免疫和炎症疾病的方法。
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公开(公告)号：US20050148042A1
公开(公告)日：2005-07-07
申请号：US10510197
申请日：2003-03-31
申请人： Glenn Prestwich , Piotr Rzepecki , Colin Ferguson , Paul Neilsen , Angie Branch , Lee Crosby
发明人： Glenn Prestwich , Piotr Rzepecki , Colin Ferguson , Paul Neilsen , Angie Branch , Lee Crosby
IPC分类号： C07F9/117 , C07F9/653 , C07F9/655 , C12Q1/42 , C12Q1/44 , C12Q1/48 , G01N33/92 , C07F9/144 , C07K14/47
CPC分类号： C12Q1/42 , C07F9/117 , C07F9/65324 , C07F9/65517 , C12Q1/44 , C12Q1/485 , G01N33/92
摘要： The methods and compositions disclosed herein concern the synthesis of a novel class of “two-headed” phospholipid-phosphoinositide hybrids possessing a carbon backbone, such as 2,3-diacylthreitol, erythritol or a synthetic module. The second phospholipid head group allows introduction of a biochemical or chemical moiety in a position orthogonal in space to those occupied by the phosphoinositide head group and the two acyl chains. The diacyl moieties allow for the incorporation of Pea-PIP2 into a lipid bilayer, while the Ptdlns(4,5)P2 moiety in the aqueous layer is specifically recognized by lipid binding proteins. In alternative embodiments of the invention, reporters, for example biotin, fluorophores and/or spin labels, are attached to the free amino group of the head groups of such molecules to specifically target the reporters to the lipid-water interface.
摘要翻译： 本文公开的方法和组合物涉及具有碳骨架的新型“双头”磷脂 - 磷酸肌醇混合物的合成，例如2,3-二酰基硫代糖，赤藓糖醇或合成模块。 第二个磷脂头组允许在与磷酸肌醇头基和两个酰基链占据的位置上在空间正交的位置引入生物化学或化学部分。 二酰基部分允许将Pea-PIP 2 N 2掺入脂质双层中，而水层中的Ptdlns（4,5）P 2 H 2部分被 脂质结合蛋白。 在本发明的替代实施方案中，记录者例如生物素，荧光团和/或旋转标记连接到这些分子的头基的游离氨基上，以将记录特异性地靶向脂质 - 水界面。
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3.发明授权Compounds and methods of use thereof for assaying lysophospholipase D activity 有权用于测定溶血磷脂酶D活性的化合物及其使用方法公开(公告)号：US07989663B2
公开(公告)日：2011-08-02
申请号：US12290293
申请日：2008-10-28
申请人： Colin Ferguson , Glenn Prestwich
发明人： Colin Ferguson , Glenn Prestwich
IPC分类号： C07F9/02
CPC分类号： G01N33/689 , C07F9/65522 , C07F9/6596 , C12Q1/34 , G01N33/542 , G01N33/57407 , G01N2333/918
摘要： Fluorogenic lysophosphatidic acid derivatives which can be used as substrates in a continuous, fluorogenic assay that can be performed in microtiter plates. The assays permit measuring LysoPLD activity levels in normal events such as pregnancy or disease states such as cancer. In addition, the present invention can be adopted to high throughout screening (HTS) for identification of potential inhibitors of lysoPLD activity.
摘要翻译： 荧光生成的溶血磷脂酸衍生物，可在连续荧光测定中用作底物，可在微量滴定板中进行。 该测定允许在正常事件如妊娠或疾病状态如癌症中测量LysoPLD活性水平。 此外，本发明可以用于高度整体筛选（HTS），用于鉴定潜在的溶菌酶活性抑制剂。
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4.发明申请Compounds and methods of use thereof for assaying lysophospholipase D activity 有权用于测定溶血磷脂酶D活性的化合物及其使用方法公开(公告)号：US20090068697A1
公开(公告)日：2009-03-12
申请号：US12290293
申请日：2008-10-28
申请人： Colin Ferguson , Glenn Prestwich
发明人： Colin Ferguson , Glenn Prestwich
CPC分类号： G01N33/689 , C07F9/65522 , C07F9/6596 , C12Q1/34 , G01N33/542 , G01N33/57407 , G01N2333/918
摘要： Fluorogenic lysophosphatidic acid derivatives which can be used as substrates in a continuous, fluorogenic assay that can be performed in microtiter plates. The assays permit measuring LysoPLD activity levels in normal events such as pregnancy or disease states such as cancer. In addition, the present invention can be adopted to high throughout screening (HTS) for identification of potential inhibitors of lysoPLD activity.
摘要翻译： 荧光生成的溶血磷脂酸衍生物，可在连续荧光测定中用作底物，可在微量滴定板中进行。 该测定允许在正常事件如妊娠或疾病状态如癌症中测量LysoPLD活性水平。 此外，本发明可以用于高度整体筛选（HTS），用于鉴定潜在的溶菌酶活性抑制剂。
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5.发明授权Compounds and methods of use thereof for assaying lysophospholipase D activity 有权用于测定溶血磷脂酶D活性的化合物及其使用方法公开(公告)号：US07459285B2
公开(公告)日：2008-12-02
申请号：US10732166
申请日：2003-12-09
申请人： Colin Ferguson , Glenn Prestwich
发明人： Colin Ferguson , Glenn Prestwich
CPC分类号： G01N33/689 , C07F9/65522 , C07F9/6596 , C12Q1/34 , G01N33/542 , G01N33/57407 , G01N2333/918
摘要： Fluorogenic lysophosphatidic acid derivatives which can be used as substrates in a continuous, fluorogenic assay that can be performed in microtiter plates. The assays permit measuring LysoPLD activity levels in normal events such as pregnancy or disease states such as cancer. In addition, the present invention can be adopted to high throughout screening(HTS) for identification of potential inhibitors of lysoPLD activity.
摘要翻译： 荧光生成的溶血磷脂酸衍生物，可在连续荧光测定中用作底物，可在微量滴定板中进行。 该测定允许在正常事件如妊娠或疾病状态如癌症中测量LysoPLD活性水平。 此外，本发明可以用于高度整体筛选（HTS），用于鉴定潜在的溶菌酶活性抑制剂。
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公开(公告)号：US08512971B2
公开(公告)日：2013-08-20
申请号：US12800339
申请日：2010-05-12
申请人： Colin Ferguson , Glenn Prestwich , Damian Madan
发明人： Colin Ferguson , Glenn Prestwich , Damian Madan
CPC分类号： C07F9/65522 , C07F9/6596 , C12N9/16 , C12Q1/34 , G01N33/542 , G01N33/57407 , G01N33/689 , G01N2333/918
摘要： Fluorogenic lysophosphatidic acid derivatives which can be used as substrates in a continuous, fluorogenic assay that can be performed in microtiter plates. The assays permit measuring LysoPLD activity levels in normal events such as pregnancy or disease states such as cancer. In addition, the present invention can be adopted to high throughout screening (HTS) for identification of potential inhibitors of lysoPLD activity.
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7.发明申请Compounds and methods of use thereof for assaying lysophospholipase D activity 有权用于测定溶血磷脂酶D活性的化合物及其使用方法公开(公告)号：US20100260682A1
公开(公告)日：2010-10-14
申请号：US12800339
申请日：2010-05-12
申请人： Colin Ferguson , Glenn Prestwich , Damian Madan
发明人： Colin Ferguson , Glenn Prestwich , Damian Madan
IPC分类号： A61K49/00 , G01N33/573 , A61P35/00
CPC分类号： C07F9/65522 , C07F9/6596 , C12N9/16 , C12Q1/34 , G01N33/542 , G01N33/57407 , G01N33/689 , G01N2333/918
摘要： Fluorogenic lysophosphatidic acid derivatives which can be used as substrates in a continuous, fluorogenic assay that can be performed in microtiter plates. The assays permit measuring LysoPLD activity levels in normal events such as pregnancy or disease states such as cancer. In addition, the present invention can be adopted to high throughout screening (HTS) for identification of potential inhibitors of lysoPLD activity.
摘要翻译： 荧光生成的溶血磷脂酸衍生物，可在连续荧光测定中用作底物，可在微量滴定板中进行。 该测定允许在正常事件如妊娠或疾病状态如癌症中测量LysoPLD活性水平。 此外，本发明可以用于高度整体筛选（HTS），用于鉴定潜在的溶菌酶活性抑制剂。
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公开(公告)号：US20060030954A1
公开(公告)日：2006-02-09
申请号：US11247079
申请日：2005-10-11
申请人： Gabriel Bergman , Eugene Takach , Marcus Stoner , John Amundson , Philip Readio , Paul Schwendinger , James Wolfbauer , Jeff Boll , Ian Thomson , Colin Ferguson , George McLeod
发明人： Gabriel Bergman , Eugene Takach , Marcus Stoner , John Amundson , Philip Readio , Paul Schwendinger , James Wolfbauer , Jeff Boll , Ian Thomson , Colin Ferguson , George McLeod
CPC分类号： G05B19/106 , B60H1/00985 , G05D23/1904
摘要： A controller equipped with a user interface having multiple-day programming capabilities, including methods of programming such devices, are disclosed. The user interface may include one or more menus or screens that can be used to program a schedule for one or more selected days during the week. An illustrative method of programming the controller may include the steps of entering a scheduling routine, selecting multiple days for schedule modification, changing the schedule parameters for one or more periods during the selected days, and then exiting the scheduling routine.
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公开(公告)号：US20070016311A1
公开(公告)日：2007-01-18
申请号：US11532355
申请日：2006-09-15
申请人： Gabriel Bergman , Eugene Takach , Marcus Stoner , John Amundson , Philip Readio , Paul Schwendinger , James Wolfbauer , Jeff Boll , Ian Thomson , Colin Ferguson , George Mcleod
发明人： Gabriel Bergman , Eugene Takach , Marcus Stoner , John Amundson , Philip Readio , Paul Schwendinger , James Wolfbauer , Jeff Boll , Ian Thomson , Colin Ferguson , George Mcleod
IPC分类号： G05B11/01
CPC分类号： G05B19/106 , B60H1/00985 , G05D23/1904
摘要： A controller equipped with a user interface having multiple-day programming capabilities, including methods of programming such devices, are disclosed. The user interface may include one or more menus or screens that can be used to program a schedule for one or more selected days during the week. An illustrative method of programming the controller may include the steps of entering a scheduling routine, selecting multiple days for schedule modification, changing the schedule parameters for one or more periods during the selected days, and then exiting the scheduling routine.
摘要翻译： 公开了一种配备有具有多天编程功能的用户界面的控制器，包括编程这种设备的方法。 用户界面可以包括一个或多个菜单或屏幕，其可以用于对一周内的一个或多个所选日期的日程表进行编程。 编程控制器的说明性方法可以包括以下步骤：输入调度例程，选择调度修改的多天，在所选择的日期内改变一个或多个周期的调度参数，然后退出调度例程。
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公开(公告)号：US20070008116A1
公开(公告)日：2007-01-11
申请号：US11532406
申请日：2006-09-15
申请人： Gabriel Bergman , Eugene Takach , Macus Stoner , John Amundson , Philip Readio , Paul Schwendinger , James Wolfbauer , Jeff Boll , Ian Thomson , Colin Ferguson , George Mcleod
发明人： Gabriel Bergman , Eugene Takach , Macus Stoner , John Amundson , Philip Readio , Paul Schwendinger , James Wolfbauer , Jeff Boll , Ian Thomson , Colin Ferguson , George Mcleod
CPC分类号： G05B19/106 , B60H1/00985 , G05D23/1904
摘要： A controller equipped with a user interface having multiple-day programming capabilities, including methods of programming such devices, are disclosed. The user interface may include one or more menus or screens that can be used to program a schedule for one or more selected days during the week. An illustrative method of programming the controller may include the steps of entering a scheduling routine, selecting multiple days for schedule modification, changing the schedule parameters for one or more periods during the selected days, and then exiting the scheduling routine.
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