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1. 发明申请

WO2011143399A1 COMPOUNDS USEFUL AS INHIBITORS OF ATR KINASE 审中-公开
标题翻译：化合物作为ATR激酶的抑制剂有用
公开(公告)号：WO2011143399A1
公开(公告)日：2011-11-17
申请号：PCT/US2011/036214
申请日：2011-05-12
申请人： VERTEX PHARMACEUTICALS INCORPORATED , CHARRIER, Jean-Damien , DURRANT, Steven, John , KNEGTEL, Ronald, Marcellus Alphonsus , PINDER, Joanne , YOUNG, Stephen, Clinton , REAPER, Philip, Michael
发明人： CHARRIER, Jean-Damien , DURRANT, Steven, John , KNEGTEL, Ronald, Marcellus Alphonsus , PINDER, Joanne , YOUNG, Stephen, Clinton , REAPER, Philip, Michael
IPC分类号： A61K31/4965 , A61K31/497 , C07D241/20 , A61P35/00
CPC分类号： C07D241/20 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/06 , C07D405/12 , C07D409/06
摘要： The present invention relates to pyrazine and pyridine compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula (I): wherein the variables are as defined herein.
摘要翻译：本发明涉及可用作ATR蛋白激酶抑制剂的吡嗪和吡啶化合物。本发明还涉及包含本发明化合物的药学上可接受的组合物; 使用本发明化合物治疗各种疾病，病症和病症的方法; 制备本发明化合物的方法; 用于制备本发明化合物的中间体; 以及在体外应用中使用化合物的方法，如生物和病理现象中激酶的研究; 由这种激酶介导的细胞内信号转导途径的研究; 和新型激酶抑制剂的比较评估。本发明的化合物具有式（I）：其中变量如本文所定义。

2. 发明申请

WO2011094283A1 PYRAZOLOPYRIDINE KINASE INHIBITORS 审中-公开
标题翻译：吡唑并吡啶激酶抑制剂
公开(公告)号：WO2011094283A1
公开(公告)日：2011-08-04
申请号：PCT/US2011/022536
申请日：2011-01-26
申请人： VERTEX PHARMACEUTICALS INCORPORATED , JIMENEZ, Juan-Miguel , GOLEC, Julian, M.C. , SETTIMO, Luca , FRAYSSE, Damien , BRENCHLEY, Guy , BOYALL, Dean , TWIN, Heather , YOUNG, Stephen , MILLER, Andrew, W. , DAVIS, Christopher, John
发明人： JIMENEZ, Juan-Miguel , GOLEC, Julian, M.C. , SETTIMO, Luca , FRAYSSE, Damien , BRENCHLEY, Guy , BOYALL, Dean , TWIN, Heather , YOUNG, Stephen , MILLER, Andrew, W. , DAVIS, Christopher, John
IPC分类号： C07D471/04 , A61K31/496 , A61P25/00 , A61P29/00 , A61P35/00 , A61P37/00
CPC分类号： C07D471/04
摘要： The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.
摘要翻译：本发明涉及用作蛋白激酶抑制剂的化合物。本发明还提供了包含所述化合物的药学上可接受的组合物以及使用该组合物治疗各种疾病，病症或障碍的方法。本发明还提供了制备本发明化合物的方法。

3. 发明申请

WO2011094273A1 PYRAZOLOPYRIDINE KINASE INHIBITORS 审中-公开
标题翻译：吡唑啉激酶抑制剂
公开(公告)号：WO2011094273A1
公开(公告)日：2011-08-04
申请号：PCT/US2011/022522
申请日：2011-01-26
申请人： VERTEX PHARMACEUTICALS INCORPORATED , JIMENEZ, Juan-miguel , GOLEC, Julian, M.c. , SETTIMO, Luca , FRAYSSE, Damien , BRENCHLEY, Guy , BOYALL, Dean , TWIN, Heather , YOUNG, Stephen , MILLER, Andrew, W. , DAVIS, Christopher, John
发明人： JIMENEZ, Juan-miguel , GOLEC, Julian, M.c. , SETTIMO, Luca , FRAYSSE, Damien , BRENCHLEY, Guy , BOYALL, Dean , TWIN, Heather , YOUNG, Stephen , MILLER, Andrew, W. , DAVIS, Christopher, John
IPC分类号： C07D471/04 , A61K31/444 , A61K31/496 , A61P25/00 , A61P29/00 , A61P35/00 , A61P37/00
CPC分类号： C07D471/04 , A61K31/437 , A61K31/496
摘要： The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.
摘要翻译：本发明涉及可用作蛋白激酶抑制剂的化合物。本发明还提供包含所述化合物的药学上可接受的组合物和使用该组合物治疗各种疾病，病症或病症的方法。本发明还提供了制备本发明化合物的方法。

4. 发明申请

WO2010075567A4 SECURED ROOM MONITORING 审中-公开
公开(公告)号：WO2010075567A4
公开(公告)日：2010-12-16
申请号：PCT/US2009069500
申请日：2009-12-23
申请人： BERNER JOHN M , YOUNG STEPHEN
发明人： BERNER JOHN M , YOUNG STEPHEN
IPC分类号： G08B23/00 , E05D3/06 , G01L9/04 , G08B21/02
CPC分类号： E05D11/00 , E05F15/00 , E05Y2400/44 , E05Y2400/81 , E05Y2800/252 , E05Y2900/132 , G01G19/413 , G01G19/52 , G01G23/3728
摘要： A system and method for providing warnings of a suicide attempt provides monitoring of specific hardware, fixtures, or objects, or structure supporting or associated with same, within an isolation room by way of sensors to provide notice exterior the room that a monitored condition has changed. The sensor can be a load sensor, proximity sensor, contact sensor, or the like. More particularly, an object in an isolation room that provides an attachment potential for hanging is monitored such as by monitoring the load of said object, detecting changes in the load, and providing an alarm of the change in condition. Doors and associated hardware are particularly suitable for such monitoring.

5. 发明申请

WO2010075567A2 SECURED ROOM MONITORING 审中-公开
标题翻译：安全室监控
公开(公告)号：WO2010075567A2
公开(公告)日：2010-07-01
申请号：PCT/US2009069500
申请日：2009-12-23
申请人： BERNER JOHN M , YOUNG STEPHEN
发明人： BERNER JOHN M , YOUNG STEPHEN
IPC分类号： G08B23/00 , E05D3/06 , G01L9/04 , G08B21/02
CPC分类号： E05D11/00 , E05F15/00 , E05Y2400/44 , E05Y2400/81 , E05Y2800/252 , E05Y2900/132 , G01G19/413 , G01G19/52 , G01G23/3728
摘要： A system and method for providing warnings of a suicide attempt provides monitoring of specific hardware, fixtures, or objects, or structure supporting or associated with same, within an isolation room by way of sensors to provide notice exterior the room that a monitored condition has changed. The sensor can be a load sensor, proximity sensor, contact sensor, or the like. More particularly, an object in an isolation room that provides an attachment potential for hanging is monitored such as by monitoring the load of said object, detecting changes in the load, and providing an alarm of the change in condition. Doors and associated hardware are particularly suitable for such monitoring.
摘要翻译：用于提供自杀企图的警告的系统和方法通过传感器在监视条件已改变的房间的外部提供通知的方式监视隔离房间内的特定硬件，固定装置或物体或支撑或关联于其的结构。传感器可以是负载传感器，接近传感器，接触传感器等。更具体地说，例如通过监视所述物体的负载，检测负载的变化并提供状况变化的警报来监视提供悬挂的附着可能性的隔离室中的物体。门和相关硬件特别适合这种监测。

6. 发明申请

WO2010049684A1 TORSIONAL MODE ULTRASONIC GENERATOR 审中-公开
标题翻译：扭力超声波发生器
公开(公告)号：WO2010049684A1
公开(公告)日：2010-05-06
申请号：PCT/GB2009/002562
申请日：2009-10-27
申请人： SRA DEVELOPMENTS LIMITED , YOUNG, Michael, John, Radley , YOUNG, Stephen, Michael, Radley , SLIPSZENKO, James, Anton , EDE, Michael, James
发明人： YOUNG, Michael, John, Radley , YOUNG, Stephen, Michael, Radley , SLIPSZENKO, James, Anton , EDE, Michael, James
IPC分类号： A61B17/32
CPC分类号： A61B17/320068 , A61B2017/320096 , A61B2017/320098
摘要： Apparatus (5, 50) for generating torsional-mode ultrasonic vibrations comprises a stack of axially-polarised piezo-electric ceramic rings (10) having a torsional converter (1, 51, 53) mounted coaxially to either one face of the stack or to two opposite faces thereof. Each torsional converter (1, 51, 53) has a cross-sectional inhomogeneity comprising a plurality of helically-extending grooves (2, 55) extending substantially from end to end of the converter. The grooves (2, 55) each have a length, measured axially along the converter (1, 51, 53), of approximately half the wavelength of ultrasonic vibrations therein. When the stack is energised, the stack and the converter (1) or converters (51, 53) resonate together in a purely torsional-mode vibration. The apparatus (5, 50) is compact and axisymmetric, and is straightforward to incorporate into a simple tool handpiece. The ultrasonic vibrations may be transmitted along a conventional elongate waveguide (3) of a tool to a distal operative tip (35). A very high amplitude torsional oscillation may thus be induced at the operative tip (35) of the tool. Alternatively, a further converter element (32) may be located at a distal end of the waveguide (3) in order partially to convert torsional-mode to longitudinal-mode vibrations for tool operative tips requiring combined-mode oscillations.
摘要翻译：用于产生扭转模式超声波振动的装置（5,50）包括一组轴向偏振的压电陶瓷环（10），其具有同轴地安装在叠层的任一个面上的扭转变换器（1,51,53），或者两个相对的面。每个扭转变换器（1,51,53）具有横截面不均匀性，其包括基本上从转换器的端部到端部延伸的多个螺旋形延伸的槽（2,55）。槽（2,55）各自具有沿着转换器（1,51,53）轴向测量其长度大约为其中超声振动波长的一半的长度。当堆叠通电时，堆叠和转换器（1）或转换器（51,53）以纯扭转模式振动共振。该装置（5,50）紧凑且轴对称，并且可以简单地结合到简单的工具手柄中。超声波振动可以沿着工具的常规细长波导（3）传输到远端操作尖端（35）。因此，可能在工具的操作尖端（35）处引起非常高的幅度扭转振荡。或者，另外的转换器元件（32）可以位于波导（3）的远端，以便部分地将扭转模式转换为需要组合模式振荡的工具操作尖端的纵向模式振动。

7. 发明申请

WO2003049737A1 CHEMICAL COMPOUNDS 审中-公开
标题翻译：化学化合物
公开(公告)号：WO2003049737A1
公开(公告)日：2003-06-19
申请号：PCT/US2002/036149
申请日：2002-12-09
申请人： ELI LILLY AND COMPANY , HISCOCK, Steven, Douglas , JONES, Stuart, Donald , SALL, Daniel, Jon , YOUNG, Stephen, Clinton , WILEY, Michael, Robert
发明人： HISCOCK, Steven, Douglas , JONES, Stuart, Donald , SALL, Daniel, Jon , YOUNG, Stephen, Clinton , WILEY, Michael, Robert
IPC分类号： A61K31/4545
CPC分类号： C07D401/12 , C07D401/14
摘要： Compounds of formula (I) in which R 1 , R 2 , R 3 and R 4 , have the meanings given in the specification are Factor Xa inhibitors useful in the treatment of thrombotic disorders.
摘要翻译：其中R 1，R 2，R 3和R 4具有本说明书中给出的含义的式（I）化合物是可用于治疗血栓形成障碍的因子Xa抑制剂。

8. 发明申请

WO2013049719A1 COMPOUNDS USEFUL AS INHIBITORS OF ATR KINASE 审中-公开
标题翻译：化合物作为ATR激酶的抑制剂有用
公开(公告)号：WO2013049719A1
公开(公告)日：2013-04-04
申请号：PCT/US2012/058117
申请日：2012-09-28
申请人： VERTEX PHARMACEUTICALS INCORPORATED , CHARRIER, Jean-Damien , YOUNG, Stephen, Clinton , DAVIS, Christopher, John , STUDLEY, John
发明人： CHARRIER, Jean-Damien , YOUNG, Stephen, Clinton , DAVIS, Christopher, John , STUDLEY, John
IPC分类号： C07D265/30 , C07D401/04 , C07D413/04 , C07D413/14 , A61K31/497 , A61P35/00
CPC分类号： A61K31/5377 , A61K33/24 , C07D265/30 , C07D267/10 , C07D401/04 , C07D413/04 , C07D413/10 , C07D413/14
摘要： The invention relates to the compound 5-(4-isopropylsulfonylphenyl) -3-[3-[4-[(3R)-morpholin-3-yl]phenyl]isoxazol-5-yl]pyrazine-2-amine and pharmaceutically acceptable salts thereof. The compounds are useful as inhibitors of ATR kinase.
摘要翻译：本发明涉及化合物5-（4-异丙基磺酰基苯基）-3- [3- [4 - [（3R） - 吗啉-3-基]苯基]异恶唑-5-基]吡嗪-2-胺及其药学上可接受的盐它们。该化合物可用作ATR激酶的抑制剂。

9. 发明申请

WO2011143423A3 COMPOUNDS USEFUL AS INHIBITORS OF ATR KINASE 审中-公开
标题翻译：化合物作为ATR激酶的抑制剂有用
公开(公告)号：WO2011143423A3
公开(公告)日：2012-03-01
申请号：PCT/US2011036243
申请日：2011-05-12
申请人： VERTEX PHARMA , CHARRIER JEAN-DAMIEN , DURRANT STEVEN JOHN , YOUNG STEPHEN CLINTON , STORCK PIERRE-HENRI , VIRANI ANIZA NIZARALI , REAPER PHILIP MICHAEL , PINDER JOANNE
发明人： CHARRIER JEAN-DAMIEN , DURRANT STEVEN JOHN , YOUNG STEPHEN CLINTON , STORCK PIERRE-HENRI , VIRANI ANIZA NIZARALI , REAPER PHILIP MICHAEL , PINDER JOANNE
IPC分类号： C07D239/46 , A61K31/422 , A61P35/00 , C07D413/04
CPC分类号： C07D241/20 , C07D401/04 , C07D403/04
摘要： The present invention relates to pyrazine and pyridine compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula (V): (Formula (v)) wherein the variables are as defined herein.
摘要翻译：本发明涉及可用作ATR蛋白激酶抑制剂的吡嗪和吡啶化合物。本发明还涉及包含本发明化合物的药学上可接受的组合物; 使用本发明化合物治疗各种疾病，病症和病症的方法; 制备本发明化合物的方法; 用于制备本发明化合物的中间体; 以及在体外应用中使用化合物的方法，如生物和病理现象中激酶的研究; 由这种激酶介导的细胞内信号转导途径的研究; 和新型激酶抑制剂的比较评估。本发明的化合物具有式（V）：（式（v）），其中变量如本文所定义。

10. 发明申请

WO2011050440A1 DEPOSITING AND FARMING METHODS FOR DRYING OIL SAND MATURE FINE TAILINGS 审中-公开
标题翻译：用于干燥油砂砂的沉积和加工方法
公开(公告)号：WO2011050440A1
公开(公告)日：2011-05-05
申请号：PCT/CA2009/001578
申请日：2009-10-30
申请人： SUNCOR ENERGY INC. , BUGG, Trevor , EASTWOOD, Jamie , REVINGTON, Adrian, Peter , WEISS, Marvin, Harvey , WELLS, Patrick, Sean , HANN, Thomas, Charles , YOUNG, Stephen, Joseph , O'NEILL, Hugues, Robert
发明人： BUGG, Trevor , EASTWOOD, Jamie , REVINGTON, Adrian, Peter , WEISS, Marvin, Harvey , WELLS, Patrick, Sean , HANN, Thomas, Charles , YOUNG, Stephen, Joseph , O'NEILL, Hugues, Robert
IPC分类号： B01D21/01 , B03B9/02 , C10G1/04 , F26B5/00
CPC分类号： F26B7/00 , B09C1/08 , F26B5/00 , F26B2200/14
摘要： The invention relates to methods for drying oil sand fine tailings treated to comprise flocculated fine tailings, by deposition and farming techniques. A deposition cell is provided with a sloped bottom surface and the flocculated fine tailings are deposited to undergo channelless advancement in the cell while allowing drainage of release water. When the deposit is uneven, it may be plowed deposit may be plowed while wet for spreading and ensuring water release conditioning is imparted thereto, while avoiding over-shearing, and maintaining sufficient shear strength to allow standing. Once a dried upper crust forms, the deposit may be harrowed to break up the crust, expose wet regions there-beneath and create furrows in the standing deposit. The methods improve the dewatering and drying of mature fine tailings in oil sands.
摘要翻译：本发明涉及通过沉积和养殖技术处理包含絮凝细尾矿的油砂细尾矿干燥方法。沉积池设置有倾斜的底表面，并且沉积絮凝的细尾矿以在池中进行无通道的推进，同时允许释放水的排放。当沉积物不均匀时，可以采用犁耕方法，同时在湿润铺展的同时，还可以避免过度剪切，并保持足够的剪切强度，从而保持放水调节。一旦形成干燥的上部地壳，沉积物可能会被破坏，以破坏地壳，暴露在其下方的湿润区域，并在立方沉积物中形成沟槽。该方法改善了油砂成熟细尾矿的脱水和干燥。

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