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31. 发明申请

WO2010071837A1 PYRAZINE DERIVATIVES USEFUL AS INHIBITORS OF ATR KINASE 审中-公开
标题翻译：吡嗪衍生物作为ATR激酶的抑制剂有用
公开(公告)号：WO2010071837A1
公开(公告)日：2010-06-24
申请号：PCT/US2009/068827
申请日：2009-12-18
申请人： VERTEX PHARMACEUTICALS INCORPORATED , CHARRIER, Jean-Damien , DURRANT, Steven , KAY, David , KNEGTEL, Ronald , MACCORMICK, Somhairle , MORTIMORE, Michael , O'DONNELL, Michael , PINDER, Joanne , RUTHERFORD, Alistair , VIRANI, Anisa, Nizarali , YOUNG, Stephen , REAPER, Philip, Michael
发明人： CHARRIER, Jean-Damien , DURRANT, Steven , KAY, David , KNEGTEL, Ronald , MACCORMICK, Somhairle , MORTIMORE, Michael , O'DONNELL, Michael , PINDER, Joanne , RUTHERFORD, Alistair , VIRANI, Anisa, Nizarali , YOUNG, Stephen , REAPER, Philip, Michael
IPC分类号： C07D413/04 , C07D417/04 , C07D401/14 , C07D403/12 , C07D409/14 , C07D413/12 , C07D417/12 , C07D471/04 , A61K31/497 , A61P35/00
CPC分类号： C07D413/14 , A61P35/00 , C07D241/28 , C07D401/04 , C07D401/10 , C07D401/14 , C07D403/04 , C07D403/10 , C07D403/12 , C07D403/14 , C07D405/04 , C07D405/12 , C07D405/14 , C07D409/04 , C07D409/14 , C07D413/04 , C07D413/12 , C07D417/04 , C07D417/12 , C07D417/14 , C07D471/04
摘要： The present invention relates to pyrazine 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 of 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。

32. 发明申请

WO2009141616A1 ULTRASONIC TISSUE DISSECTOR 审中-公开
标题翻译：超声组织分离器
公开(公告)号：WO2009141616A1
公开(公告)日：2009-11-26
申请号：PCT/GB2009/001278
申请日：2009-05-21
申请人： SRA DEVELOPMENTS LIMITED , SLIPSZENKO, James, Anton , EDE, Michael, James , YOUNG, Stephen, Michael, Radley
发明人： SLIPSZENKO, James, Anton , EDE, Michael, James , YOUNG, Stephen, Michael, Radley
IPC分类号： A61B17/32 , B06B1/00 , B06B3/00 , A61B17/22
CPC分类号： A61B17/320068 , A61B17/320092 , A61B2017/22011 , A61B2017/22018 , A61B2017/22024 , A61B2017/22027 , A61B2017/320072 , A61B2017/320076 , A61B2017/320078 , A61B2017/320096 , A61B2017/320098 , Y10T29/49005
摘要： An ultrasonic surgical tool has an elongate waveguide (102) operatively connected or connectable to a source of ultrasonic vibrations. An operative element (100, 130, 140) at a distal end of the waveguide (102) has a diameter less than that of the waveguide (102). A connecting portion of intermediate diameter may connect the operative element (100, 130, 140) and the waveguide (102). A proximal end of the operative element (100, 130, 140) forms a first step junction (126, 134), located at a nodal plane of ultrasonic vibrations in the waveguide (102) and operative element, producing a velocity amplitude gain across the step junction. A second zero- gain step junction between the connecting portion and the waveguide (102) is located at an antinodal plane. The operative element (100, 130) may comprise a curved distal cutting and welding element (114) having a pair of elongate welding grooves defining a cutting ridge. Alternatively, the operative element (140) may comprise a welding element having a flat or slightly ridged operative face (136).
摘要翻译：超声波手术工具具有可操作地连接或连接到超声波振动源的细长波导（102）。在波导（102）的远端处的操作元件（100,130,140）的直径小于波导（102）的直径。中间直径的连接部分可以连接操作元件（100,130,140）和波导（102）。操作元件（100,130,140）的近端形成位于波导（102）和操作元件中的超声振动的节点平面处的第一阶跃接合（126,134），从而产生横跨一步连接。连接部分和波导（102）之间的第二零增益阶跃连接位于反平面。操作元件（100,130）可以包括弯曲的远端切割和焊接元件（114），其具有限定切割脊的一对细长的焊接槽。或者，操作元件（140）可以包括具有平坦或稍微脊状的操作面（136）的焊接元件。

33. 发明申请

WO2009073300A1 [1H- PYRAZOLO [3, 4-B] PYRIDINE-4-YL] -PHENYLE OR -PYRIDIN-2-YLE DERIVATIVES AS PROTEIN KINASE C-THETA 审中-公开
标题翻译： [1H-吡唑并[3,4-B]吡啶-4-基] - 苯基或 - 吡啶-2-基衍生物作为蛋白激酶C-THETA
公开(公告)号：WO2009073300A1
公开(公告)日：2009-06-11
申请号：PCT/US2008/081933
申请日：2008-10-31
申请人： VERTEX PHARMACEUTICALS INCORPORATED , JIMENEZ, Juan-Miguel , MORTIMORE, Michael , COLLIER, Philip , MILLER, Andrew , YOUNG, Stephen , MAK, Chau , DAVIS, Christopher , TWIN, Heather , BRENCHLEY, Guy , BOYALL, Dean , SHAZIA, Keily , LUCA, Settimo
发明人： JIMENEZ, Juan-Miguel , MORTIMORE, Michael , COLLIER, Philip , MILLER, Andrew , YOUNG, Stephen , MAK, Chau , DAVIS, Christopher , TWIN, Heather , BRENCHLEY, Guy , BOYALL, Dean , SHAZIA, Keily , LUCA, Settimo
IPC分类号： C07D471/04 , A61K31/437 , A61P29/00 , A61P35/00 , A61P11/06 , A61P17/06 , A61P19/02 , A61P3/10
CPC分类号： C07D471/04
摘要： The present invention relates to compounds of formula (I) and (IA) useful as inhibitors of protein kinase (1a). 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. (a) : in particular protein kinase C theta, wherein A and A' are independently -N- or -C(R+) -. Ring B is five- or six-membered saturated carbocyclic or heterocyclic R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , x and y are as described herein.
摘要翻译：本发明涉及可用作蛋白激酶（1a）抑制剂的式（I）和（IA）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。（a）：特别是蛋白激酶Cθ，其中A和A'独立地为-N-或-C（R +） - 。环B是五或六元饱和碳环或杂环R 1，R 2，R 3，R 4，R 5，R 6，R 7，x和y如本文所述。

34. 发明申请

WO2008152378A3 SWITCH FOR ULTRASONIC SURGICAL TOOL 审中-公开
标题翻译：超声波手术刀开关
公开(公告)号：WO2008152378A3
公开(公告)日：2009-02-05
申请号：PCT/GB2008001994
申请日：2008-06-11
申请人： SRA DEV LTD , YOUNG MICHAEL JOHN RADLEY , YOUNG STEPHEN MICHAEL RADLEY
发明人： YOUNG MICHAEL JOHN RADLEY , YOUNG STEPHEN MICHAEL RADLEY
IPC分类号： A61B17/32 , A61B18/00 , H01H9/06
CPC分类号： A61B17/320068 , A61B2017/00367 , H01H9/06 , H01H2009/0083
摘要： A switch unit (40) is mountable to a distal end of a handpiece of an electrically-activatable surgical tool, such as an ultrasonically-vibratable surgical tool. The switch unit (40) has a generally bullet-shaped outer form with an axial bore (42) through which a waveguide of the tool extends. A resiliently deformable band (1) extends around the switch unit (40) above a polygonal-section contact zone (2), such that fingertip pressure on the band (1) may locally depress the band (1) towards a flat area (12) of the contact zone (2). Switch contacts (11) are mounted to an inner surface of the band (1) opposite a plated circuit (10) located on each flat area (12) so as to form a plurality of switches. A switch to activate the tool is thus easily accessible to a user's fingertip in any orientation of the handpiece in the user's hand. The switch contacts (11) may each comprise a body having an electrical resistance dependent on a pressure exerted thereon. A magnitude of a response from the tool may thus be controlled by the pressure exerted by the user's fingertip.
摘要翻译：开关单元（40）可安装到可激活的外科手术工具（例如超声波可振动的外科手术工具）的手持件的远端。开关单元（40）具有通常具有子弹形的外部形式，其具有轴向孔（42），工具的波导通过所述轴向孔延伸。可弹性变形的带（1）围绕开关单元（40）围绕多边形截面接触区域（2）延伸，使得带（1）上的指尖压力可以朝向平坦区域（12）局部地将带（1））接触区域（2）。开关触点（11）安装到位于每个平坦区域（12）上的电镀电路（10）相对的带（1）的内表面上，以形成多个开关。因此，用户的手中的手持件的任何方向，用户的指尖可以容易地访问激活该工具的开关。开关触点（11）可以各自包括具有取决于施加在其上的压力的电阻的主体。因此，来自工具的响应的大小可以由用户的指尖施加的压力来控制。

35. 发明申请

WO2008115973A3 AMINOPYRIMIDINES USEFUL AS KINASE INHIBITORS 审中-公开
公开(公告)号：WO2008115973A3
公开(公告)日：2008-12-04
申请号：PCT/US2008057465
申请日：2008-03-19
申请人： VERTEX PHARMA , BINCH HAYLEY , YOUNG STEPHEN , DAVIS CHRISTOPHER , MORTIMORE MICHAEL , GOLEC JULIAN , STUDLEY JOHN , ROBINSON DANIEL , O'DONNELL MICHAEL , BOYALL DEAN , PINDER JOANNE , EVERITT SIMON
发明人： BINCH HAYLEY , YOUNG STEPHEN , DAVIS CHRISTOPHER , MORTIMORE MICHAEL , GOLEC JULIAN , STUDLEY JOHN , ROBINSON DANIEL , O'DONNELL MICHAEL , BOYALL DEAN , PINDER JOANNE , EVERITT SIMON
IPC分类号： C07D403/14 , A61K31/33 , A61K35/00 , C07D413/14 , C07D417/14 , C07D471/04
CPC分类号： C07D471/04 , C07D403/14 , C07D413/14 , C07D417/14
摘要： The present invention relates to compounds useful as inhibitors of Aurora protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, and disorders. The invention also provides processes for preparing compounds of the invention.

36. 发明申请

WO2008094992A3 2-AMINOPYRIDINE DERIVATIVES USEFUL AS KINASE INHIBITORS 审中-公开
标题翻译： 2-氨基吡啶衍生物作为激酶抑制剂有用
公开(公告)号：WO2008094992A3
公开(公告)日：2008-12-04
申请号：PCT/US2008052443
申请日：2008-01-30
申请人： VERTEX PHARMA , JIMENEZ JUAN-MIGUEL , BEMIS GUY , MALTAIS FRANCOIS , WANG TIANSHENG , KNEGTEL RONALD , DAVIS CHRIS , FRAYSSE DAMIEN , BOYALL DEAN , SETTIMO LUCA , YOUNG STEPHEN , MORTIMORE MICHAEL
发明人： JIMENEZ JUAN-MIGUEL , BEMIS GUY , MALTAIS FRANCOIS , WANG TIANSHENG , KNEGTEL RONALD , DAVIS CHRIS , FRAYSSE DAMIEN , BOYALL DEAN , SETTIMO LUCA , YOUNG STEPHEN , MORTIMORE MICHAEL
IPC分类号： C07D213/73 , A61K31/444 , A61K31/529 , A61P25/00 , A61P35/00 , C07D401/14 , C07D409/06 , C07D409/14 , C07D417/06 , C07D417/14 , C07D487/04 , C07D487/08
CPC分类号： C07D213/73 , C07D401/04 , C07D401/12 , C07D401/14 , C07D409/06 , C07D409/14 , C07D417/06 , C07D417/14 , C07D487/04 , C07D487/08
摘要： The present invention relates to compounds represented by the following structural formula: (I) useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of µsing 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：本发明涉及由以下结构式表示的化合物：（I）可用作蛋白激酶的抑制剂。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。

37. 发明申请

WO2008065323A1 IMPROVED ULTRASONIC SURGICAL TOOL 审中-公开
标题翻译：改进的超声外科工具
公开(公告)号：WO2008065323A1
公开(公告)日：2008-06-05
申请号：PCT/GB2007/003560
申请日：2007-09-18
申请人： SRA DEVELOPMENTS LIMITED , YOUNG, Michael, John, Radley , YOUNG, Stephen, Michael, Radley
发明人： YOUNG, Michael, John, Radley , YOUNG, Stephen, Michael, Radley
IPC分类号： A61B17/32
CPC分类号： A61B17/320068 , A61B2017/22008 , A61B2017/320076 , A61B2017/320078
摘要： The shaped output is for use with an ultrasonic surgical tool vibratable in torsional mode. The output has a generally cylindrical first waveguide (1) with, at a distal end a second waveguide extension member (3) of reduced diameter. The second waveguide (3) is curved in one plane from the axis of the first waveguide. It has at least two blade faces (4) extending radially outwardly from its distal end.
摘要翻译：成形输出用于可在扭转模式下振动的超声手术工具。输出具有大致圆柱形的第一波导（1），在远端处具有减小直径的第二波导延伸构件（3）。第二波导（3）从与第一波导的轴线的一个平面中弯曲。它具有从其远端径向向外延伸的至少两个叶片面（4）。

38. 发明申请

WO2006020830A3 BISARYL-SULFONAMIDES 审中-公开
标题翻译：二芳基磺酰胺
公开(公告)号：WO2006020830A3
公开(公告)日：2007-04-12
申请号：PCT/US2005028673
申请日：2005-08-11
申请人： AMGEN INC , BERGERON PHILIPPE , FARTHING CHRISTOPHER N , JONES STUART D , LIEBESCHUETZ JOHN W , LIVELY SARAH E , MCGEE LAWRENCE R , MCKENDRY SHARON , SHEPPARD DAVID , YOUNG STEPHEN C
发明人： BERGERON PHILIPPE , FARTHING CHRISTOPHER N , JONES STUART D , LIEBESCHUETZ JOHN W , LIVELY SARAH E , MCGEE LAWRENCE R , MCKENDRY SHARON , SHEPPARD DAVID , YOUNG STEPHEN C
IPC分类号： C07D239/48 , A61K31/506 , C07D239/42 , C07D239/46 , C07D239/54 , C07D239/58
CPC分类号： C07D239/47 , C07D213/75 , C07D237/22 , C07D239/42 , C07D239/46 , C07D239/48 , C07D239/52 , C07D239/54 , C07D239/58
摘要： Compounds, compositions and methods are provided that are useful in. the treatment or preventionTof a condition or disorder mediated by PPAR? or PPARd. In particular, the compounds of the invention modulate the function of PPAR? or PPARd. The subject methods are particularly useful in the treatment and/or prevention of diabetes, obesity, hypercholesterolemia, rheumatoid arthritis and atherosclerosis. The subject, compounds include bisaryl-sulfonamides that have general formula (I): wherein Ar, R 1 , X, Y, Z. W, L, B and R 2 are described herein.
摘要翻译：提供了可用于治疗或预防PPAR介导的病症或障碍的化合物，组合物和方法。或PPARd。特别地，本发明的化合物调节PPAR的功能？或PPARd。本发明的方法在治疗和/或预防糖尿病，肥胖，高胆固醇血症，类风湿性关节炎和动脉粥样硬化方面特别有用。本发明的化合物包括具有通式（I）的二芳基磺酰胺：其中Ar，R 1，X，Y，Z.W，L，B和R 2，在此描述。

39. 发明申请

WO2004081051A1 BISPECIFIC ANTIBODIES 审中-公开
标题翻译：双重抗体
公开(公告)号：WO2004081051A1
公开(公告)日：2004-09-23
申请号：PCT/GB2004/001026
申请日：2004-03-11
申请人： THE UNIVERSITY OF BIRMINGHAM , YOUNG, Stephen, Peter
发明人： YOUNG, Stephen, Peter
IPC分类号： C07K16/46
CPC分类号： B82Y5/00 , A61K47/6897 , A61K51/109 , A61K51/1093 , A61K2039/505 , C07K16/468
摘要： The present invention discloses a bispecific antibody (BAb) comprising two antibodies, each of which has a binding specificity to a different epitope situated on the surface of a target structure. Each of said antibodies has a relatively low binding affinity for its respective epitope. The BAbs produced according to the present invention have much lower affinity for cross-reactive non-target tissue due to the lower affinity of the MAbs used to produce them. These BAbs still provide high avidity for target tissue due to the cumulative nature of the binding interactions.
摘要翻译：本发明公开了包含两种抗体的双特异性抗体（BAb），每种抗体对位于靶结构表面上的不同表位具有结合特异性。所述抗体中的每一种对其各自的表位具有相对低的结合亲和力。由于用于制备它们的MAb的亲和力较低，根据本发明生产的BAb对交叉反应性非靶组织的亲和力低得多。由于结合相互作用的累积性质，这些BAb仍然为目标组织提供高亲合力。

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