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31. 发明申请

WO2007074078A3 ARYL-ISOXAZOL-4-YL-IMIDAZOLE DERIVATIVES 审中-公开
公开(公告)号：WO2007074078A3
公开(公告)日：2007-07-05
申请号：PCT/EP2006/069722
申请日：2006-12-14
申请人： F. HOFFMANN-LA ROCHE AG , BUETTELMANN, Bernd , HAN, Bo , KNUST, Henner , THOMAS, Andrew
发明人： BUETTELMANN, Bernd , HAN, Bo , KNUST, Henner , THOMAS, Andrew
IPC分类号： C07D413/04 , A61K31/42 , A61K31/4178
摘要： The present invention is concerned with aryl-isoxazol-4-yl-imidazole derivatives of formula (I), wherein R 1 to R 3 are each independently hydrogen or halogen; R 4 is hydrogen, lower alkyl, cycloalkyl, -(CH 2 ) n -O-lower alkyl or lower alkyl substituted by hydroxy; R 5 is -(CH 2 ) m -aryl or -(CH 2 ) m -heteroaryl which are optionally substituted by one or more substituents selected from the group consisting of halogen, cyano, nitro, lower alkyl, lower alkoxy, lower alkylsulfanyl, lower alkyl substituted by halogen, -C(O)-lower alkyl, -C(O)-O-lower alkyl, -NH-C(O)-O-lower alkyl or -C(O)-NH-R', wherein R' is lower alkynyl or lower alkyl substituted by halogen, or is -(CH 2 ) n -cycloalkyl, -(CH 2 ) n -heterocyclyl, -(CH 2 ) n -heteroaryl or -(CH 2 ) n -aryl, optionally substituted by halogen; R 6 is hydrogen, -C(O)H, -(CH 2 ) n -O-lower alkyl, -C(O)O-lower alkyl, lower alkyl substituted by hydroxy or halogen, or is cycloalkyl, aryl, or is -(CH 2 ) n -O-CH 2 -aryl, optionally substituted by halogen or lower alkyl, or is -(CH 2 ) n -O-CH 2 -heteroaryl, optionally substituted by halogen, lower alkyl or lower alkyl substituted by halogen, or is -(CH 2 ) n -NH-(CH 2 ) o -heterocyclyl; n is 0, 1, 2 or 3 m is 0 or 1; o is 1, 2 or 3; as well as with pharmaceutically acceptable acid addition salts thereof. It has been found that this class of compounds show high affinity and selectivity for GABA A α5 receptor binding sites and might be useful as cognitive enhancer or for the treatment of cognitive disorders like Alzheimer's disease.

32. 发明申请

WO2007071598A1 ARYL-ISOXAZOLO-4-YL-OXADIAZOLE DERIVATIVES 审中-公开
公开(公告)号：WO2007071598A1
公开(公告)日：2007-06-28
申请号：PCT/EP2006/069625
申请日：2006-12-13
申请人： F. HOFFMANN-LA ROCHE AG , BUETTELMANN, Bernd , HAN, Bo , KNUST, Henner , KOBLET, Andreas , THOMAS, Andrew
发明人： BUETTELMANN, Bernd , HAN, Bo , KNUST, Henner , KOBLET, Andreas , THOMAS, Andrew
IPC分类号： C07D413/04 , C07D413/14 , A61K31/4245 , A61K31/4439 , A61P25/28
CPC分类号： C07D413/04 , C07D413/14
摘要： The present invention is concerned with isoxazol-4-yl-oxadiazole derivatives of formula (I) wherein R 1 is hydrogen, halogen, aryl, heterocyclyl, heteroaryl, cyano, lower alkyl, -(CH 2 ) n -cycloalkyl, -(CH 2 ) n -N(R) 2 , -(CH 2 ) n -O-lower alkyl or -(CH 2 ) n -OH; n is 0,1 or 2 R is hydrogen or lower alkyl; R 2 is cycloalkyl, aryl, heteroaryl or heterocyclyl, which are optionally substituted by one or more substituents, selected from the group consisting of halogen, cyano, nitro, lower alkyl, lower alkoxy, lower alkoxy substituted by halogen, lower alkyl substituted by halogen, C(O)O-lower alkyl, lower alkylsulfonyl, -NR a R b , -C(O)-NR a R b , -C(O)-heterocyclyl, benzyloxy, heterocyclyl optionally substituted by hydroxy, halogen or lower alkyl, or is heteroaryl optionally substituted by lower alkyl; R a and R b are independently hydrogen, lower alkylsulfonyl, -C(O)H, -(CH 2 ) n -N(R) 2 , -(CH 2 ) n -O-lower alkyl, -(CH 2 ) n -S-lower alkyl, -(CH 2 ) n -S(O) 2 -lower alkyl, heteroarylsulfonyl, lower alkyl, -(CH2)n-heterocyclyl, optionally substituted by lower alkyl, or is -(CH 2 ) n -cycloalkyl, -(CH 2 ) n -heteroaryl, -(CH 2 ) n -OH, -(CO)-R', wherein R' is lower alkyl, cycloalkyl or heteroaryl; R 3 is aryl or heteroaryl, which are optionally substituted by halogen or lower alkyl substituted by halogen; as well as pharmaceutically acceptable acid addition salts thereof. It has been found that this class of compounds show high affinity and selectivity for GABA α5 receptor binding sites and might be useful as cognitive enhancer or for the treatment of cognitive disorders like Alzheimer's disease.
摘要翻译：本发明涉及式（I）的异恶唑-4-基 - 恶二唑衍生物，其中R 1是氢，卤素，芳基，杂环基，杂芳基，氰基，低级烷基， - （CH

33. 发明申请

WO2007054444A3 3-ARYL-ISOXAZOLE-4-CARBONYL-BENZOFURAN DERIVATIVES 审中-公开
公开(公告)号：WO2007054444A3
公开(公告)日：2007-05-18
申请号：PCT/EP2006/067879
申请日：2006-10-27
申请人： F. HOFFMANN-LA ROCHE AG , BUETTELMANN, Bernd , HAN, Bo , KNUST, Henner , NETTEKOVEN, Matthias , THOMAS, Andrew
发明人： BUETTELMANN, Bernd , HAN, Bo , KNUST, Henner , NETTEKOVEN, Matthias , THOMAS, Andrew
IPC分类号： C07D413/06 , C07D413/14 , A61K31/42 , A61P25/28
摘要： The present invention is concerned with 3-aryl-isoxazole-4-carbonyl-benzofuran derivatives of formula (I) wherein R1 is hydrogen or halogen; R2 is hydrogen, halogen, hydroxy, lower alkoxy, OCF3, -OCH2-R, R3 is hydrogen or lower alkoxy; or R2 and R3 form together with the carbon atom to which they are attached a ring with -CH=CH-CH=-CH-; R is aryl or heteroaryl, optionally substituted by halogen or lower alkyl, or is C(O)NH-lower alkyl, or is -C(O)-heteroaryl, wherein the heteroaryl group is optionally substituted by lower alkyl or phenyl, and with their pharmaceutically acceptable acid addition salts. It has been found that this class of compounds show high affinity and selectivity for GABA A cc5 receptor binding sites and might be useful as cognitive enhancer or for the treatment of cognitive disorders like Alzheimer's disease.

34. 发明申请

WO2007047018A2 ULTRASONIC FAULT DETECTION SYSTEM USING A HIGH DYNAMIC RANGE ANALOG TO DIGITAL CONVERSION SYSTEM 审中-公开
标题翻译：使用高动态范围模拟数字转换系统的超声波故障检测系统
公开(公告)号：WO2007047018A2
公开(公告)日：2007-04-26
申请号：PCT/US2006/036908
申请日：2006-09-22
申请人： OLYMPUS NDT , THOMAS, Andrew
发明人： THOMAS, Andrew
IPC分类号： G01N29/00
CPC分类号： G01N29/44 , G01N29/043 , G01N29/262 , G01N29/42 , G01N29/4463 , G01N2291/044 , G01N2291/102 , H03M1/188
摘要： A method and apparatus for effecting ultrasonic flaw detection of an object processes an echo signal received from the object being tested in at least three signal channels, wherein the echo signal is scaled to different degrees along each channel to increase and extend the dynamic range of an associated A/D converter system, in a manner which dispenses with the need for using numerous analog high pass and low pass filters and a variable gain amplifier. This reduces complexity and avoids performance limitations. The digital to analog converters sample the differently scaled input signal and a selection circuit selects the output of the digital output obtained from that analog to digital converter which has the highest gain, but which has not overflowed. The digital outputs are seamlessly merged to produce an output that can be displayed as a scan display which shows the location of faults.
摘要翻译：用于实现物体的超声波探伤的方法和装置处理在至少三个信号通道中从被测试对象接收的回波信号，其中回波信号沿着每个通道被缩放到不同程度以增加和扩展一个相关的A / D转换器系统，其不需要使用大量模拟高通和低通滤波器和可变增益放大器。这降低了复杂性并避免了性能限制。数模转换器对不同比例的输入信号进行采样，并且选择电路选择从具有最高增益但尚未溢出的模数转换器获得的数字输出的输出。数字输出无缝合并，产生可显示为显示故障位置的扫描显示的输出。

35. 发明申请

WO2012062623A1 TRIAZOLE DERIVATIVES AS LIGANDS FOR GABA RECEPTORS 审中-公开
标题翻译：三唑衍生物作为GABA受体的配体
公开(公告)号：WO2012062623A1
公开(公告)日：2012-05-18
申请号：PCT/EP2011/069192
申请日：2011-11-02
申请人： F. HOFFMANN-LA ROCHE AG , GABRIEL, Stephen Deems , THOMAS, Andrew
发明人： GABRIEL, Stephen Deems , THOMAS, Andrew
IPC分类号： C07D403/12 , C07D405/14 , C07D413/14 , C07D417/06 , C07D417/14 , A61K31/4155 , A61K31/4192 , A61K31/427 , A61P25/28
CPC分类号： C07D413/14 , C07D403/12 , C07D405/14 , C07D417/06 , C07D417/14
摘要： The present invention is concerned with novel triazole compounds of formula (I) wherein A, X, Y, u,v, R 1 , R 2 , and R 3 are as described herein, as well as pharmaceutically acceptable salts thereof. The active compounds of present invention have affinity and selectivity for the GABA A α5 receptor. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as medicaments.
摘要翻译：本发明涉及式（I）的新三唑化合物，其中A，X，Y，u，v，R 1，R 2和R 3如本文所述，以及其药学上可接受的盐。本发明的活性化合物对GABA A a5受体具有亲和性和选择性。此外，本发明涉及制备式（I）化合物，包含它们的药物组合物及其作为药物的用途。

36. 发明申请

WO2011044686A1 SYSTEM AND METHOD FOR PROVIDING REAL-TIME DATA 审中-公开
标题翻译：用于提供实时数据的系统和方法
公开(公告)号：WO2011044686A1
公开(公告)日：2011-04-21
申请号：PCT/CA2010/001616
申请日：2010-10-15
申请人： COGENT REAL-TIME SYSTEMS INC. , THOMAS, Andrew
发明人： THOMAS, Andrew
IPC分类号： H04L12/16
CPC分类号： H04L67/02 , H04L65/1066 , H04L65/4007 , H04L65/4015
摘要： A system and method for providing real-time data to a Rich Internet Application is disclosed. The graphical and networking features of RIA frameworks in conjunction with at least one real-time data server provides low-latency real-time data applications in a web browser. In one embodiment data is produced at a data source, propagated to a server, and collected at the server. A persistent connection is created from a RIA to the server and the RIA is subscribed to the data, wherein the subscribed data comprises at least some of the data collected at the server and wherein the server propagates the subscribed data to the RIA through the persistent connection as the data is collected at the server.
摘要翻译：公开了一种用于向富互联网应用提供实时数据的系统和方法。 RIA框架的图形和网络功能与至少一个实时数据服务器相结合，可在Web浏览器中提供低延迟实时数据应用程序。在一个实施例中，数据在数据源处产生，传播到服务器，并在服务器处收集。持久连接从RIA创建到服务器，并且RIA订阅数据，其中订阅的数据包括在服务器处收集的至少一些数据，并且其中服务器通过持续连接将订阅的数据传播到RIA 因为数据是在服务器上收集的。

37. 发明申请

WO2010136799A2 DEVICE POSITIONING SYSTEM 审中-公开
标题翻译：设备定位系统
公开(公告)号：WO2010136799A2
公开(公告)日：2010-12-02
申请号：PCT/GB2010/050871
申请日：2010-05-26
申请人： THE MAGSTIM COMPANY LIMITED , ROGUE RESEARCH IN. , THOMAS, Andrew , COMEAU, Roch
发明人： THOMAS, Andrew , COMEAU, Roch
IPC分类号： A61B19/00 , A61B17/00
CPC分类号： A61B34/70 , A61B90/11 , A61B90/50 , A61B2017/00022 , A61B2017/00398 , A61B2017/00535 , A61B2017/00557 , A61B2034/304 , A61N2/02
摘要： A positioning system for positioning a scientific or medical device (particularly a TMS coil) in a predetermined location with respect to a living subject, includes a manipulator arrangement which is movable to position the device and a mounting platform for mounting the device. The mounting platform includes a displacement device for displacing the device with respect to the manipulator arrangement; the displacement device being a variable volume displacement device (such as a bag or pouch for example) supplied with a fluid.
摘要翻译：用于将科学或医疗装置（特别是TMS线圈）定位在相对于活体的预定位置的定位系统包括可移动以定位装置的操纵器装置和用于安装装置的安装平台。安装平台包括用于相对于操纵器装置移动装置的位移装置; 该位移装置是一个可变体积排量装置（例如，一个袋子或袋子），供给流体。

38. 发明申请

WO2010127976A1 ISOXAZOLE-PYRIDINE DERIVATIVES 审中-公开
标题翻译：异佛唑酮衍生物
公开(公告)号：WO2010127976A1
公开(公告)日：2010-11-11
申请号：PCT/EP2010/055695
申请日：2010-04-28
申请人： F. HOFFMANN-LA ROCHE AG , JAKOB-ROETNE, Roland , LUCAS, Matthew, C. , THOMAS, Andrew
发明人： JAKOB-ROETNE, Roland , LUCAS, Matthew, C. , THOMAS, Andrew
IPC分类号： C07D413/12 , C07D413/14 , C07D417/14 , A61K31/4439 , A61P25/28
CPC分类号： C07D413/12 , C07D413/14 , C07D417/14
摘要： The present invention is concerned with isoxazole-pyridine derivatives of formula I, having affinity and selectivity for GABA A α5 receptor, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are useful as cognitive enhancer or for the therapeutic and/or prophylactic treatment of cognitive disorders like Alzheimer's disease.
摘要翻译：本发明涉及式I的异恶唑 - 吡啶衍生物，其具有对GABA A a5受体的亲和性和选择性，它们的制备，含有它们的药物组合物及其作为药物的用途。本发明的活性化合物可用作认知增强剂或用于治疗和/或预防性治疗认知障碍如阿尔茨海默氏病。

39. 发明申请

WO2010112475A1 HYDROXY-METHYL ISOXAZOLE DERIVATIVES AS GABA A MODULATORS 审中-公开
标题翻译：羟基 - 甲基异恶唑衍生物作为GABA A调节剂
公开(公告)号：WO2010112475A1
公开(公告)日：2010-10-07
申请号：PCT/EP2010/054141
申请日：2010-03-30
申请人： F. HOFFMANN-LA ROCHE AG , BUETTELMANN, Bernd , GABRIEL, Stephen, Deems , HANLON, Steven, Paul , JAKOB-ROETNE, Roland , LUCAS, Matthew, C. , SPURR, Paul , THOMAS, Andrew , WALDMEIER, Pius
发明人： BUETTELMANN, Bernd , GABRIEL, Stephen, Deems , HANLON, Steven, Paul , JAKOB-ROETNE, Roland , LUCAS, Matthew, C. , SPURR, Paul , THOMAS, Andrew , WALDMEIER, Pius
IPC分类号： C07D413/12 , C07D413/14 , A61K31/4439 , A61P25/28
CPC分类号： C07D413/12 , C07D413/14
摘要： The present invention is concerned with novel hydroxy-methyl isoxazole derivatives of formula (I) wherein R 1 , R 2 and R 3 are as described herein, as well as pharmaceutically acceptable salts and esters thereof. The active compounds of the present invention have affinity and selectivity for GABA A α5 receptor. Further the present invention is concerned with the manufacture of the active compounds of formula I, pharmaceutical compositions containing them and their use as medicaments.
摘要翻译：本发明涉及式（I）的新型羟基 - 甲基异恶唑衍生物，其中R 1，R 2和R 3如本文所述，以及其药学上可接受的盐和酯。本发明的活性化合物对GABA A a5受体具有亲和性和选择性。此外，本发明涉及式I的活性化合物，含有它们的药物组合物及其作为药物的用途的制备。

40. 发明申请

WO2009071464A1 ISOXAZOLO-PYRAZINE DERIVATIVES 审中-公开
标题翻译： ISOXAZOLO-PYRAZINE DORIVATIVES
公开(公告)号：WO2009071464A1
公开(公告)日：2009-06-11
申请号：PCT/EP2008/066127
申请日：2008-11-25
申请人： F. HOFFMANN-LA ROCHE AG , BUETTELMANN, Bernd , JAKOB-ROETNE, Roland , KNUST, Henner , THOMAS, Andrew
发明人： BUETTELMANN, Bernd , JAKOB-ROETNE, Roland , KNUST, Henner , THOMAS, Andrew
IPC分类号： C07D413/12 , C07D413/14 , A61K31/497 , A61P25/28
CPC分类号： C07D413/12 , C07D413/14
摘要： The present invention is concerned with isoxazolo-pyrazine derivatives of formula (I) wherein X is O or NH; R 1 is phenyl or pyridine-2-yl, wherein the rings may be optionally substituted with one, two or three halo; R 2 is H or C 1-4 alkyl; R 3 and R 4 each are independently H, optionally substituted C 1-7 alkyl, optionally substituted C 1-7 alko.xy, CN, halo, NO 2 , -C(0)-R a -C(0)-NR b R c or R 3 and R 4 together form an optionally substituted annelated benzo ring, or a pharmaceutically acceptable salt thereof, having affinity and selectivity for GABA A α5 receptor binding site, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are useful as cognitive enhancer or for the treatment of cognitive disorders like Alzheimer's disease.
摘要翻译：本发明涉及式（I）的异恶唑并吡嗪衍生物，其中X是O或NH; R 1是苯基或吡啶-2-基，其中环可以任选地被一个，两个或三个卤素取代; R2是H或C1-4烷基; R 3和R 4各自独立地为H，任选取代的C 1-7烷基，任选取代的C 1-7烷基，CN，卤素，NO 2，-C（O）-R a -C（O）-NR b R c或R 3和R 4一起形成任选地其具有对GABA A a5受体结合位点的亲和性和选择性，其制备，含有它们的药物组合物及其作为药物的用途的取代的环状苯并环或其药学上可接受的盐。本发明的活性化合物可用作认知增强剂或用于治疗认知障碍如阿尔茨海默氏病。

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