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公开(公告)号:US20100041886A1
公开(公告)日:2010-02-18
申请号:US12581192
申请日:2009-10-19
IPC分类号: C07D413/02
CPC分类号: C07D413/12 , C07D413/14
摘要: The invention relates to isoxazolo-pyrazine derivatives and their pharmaceutically acceptable salts having affinity and selectivity for the GABA A α5 receptor binding site, their manufacture, and pharmaceutical compositions containing them. The compounds of present invention are inverse agonists of GABA A α5. The invention also relates to methods for enhancing cognition and for treating cognitive disorders like Alzheimer's disease.
摘要翻译: 本发明涉及异恶唑并吡嗪衍生物及其药学上可接受的盐,其对GABA Aα5受体结合位点具有亲和性和选择性,其制备和含有它们的药物组合物。 本发明的化合物是GABA Aα5的反向激动剂。 本发明还涉及增强认知和治疗认知障碍如阿尔茨海默病的方法。
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公开(公告)号:US20090143407A1
公开(公告)日:2009-06-04
申请号:US12277326
申请日:2008-11-25
IPC分类号: A61K31/497 , C07D413/02
CPC分类号: C07D413/12 , C07D413/14
摘要: The invention relates to isoxazolo-pyrazine derivatives and their pharmaceutically acceptable salts having affinity and selectivity for the GABA A α5 receptor binding site, their manufacture, and pharmaceutical compositions containing them. The compounds of present invention are inverse agonists of GABA A α5. The invention also relates to methods for enhancing cognition and for treating cognitive disorders like Alzheimer's disease.
摘要翻译: 本发明涉及对于GABA Aα5受体结合位点具有亲和性和选择性的异恶唑并吡嗪衍生物及其药学上可接受的盐,其制备方法以及含有它们的药物组合物。 本发明的化合物是GABA Aα5的反向激动剂。 本发明还涉及增强认知和治疗认知障碍如阿尔茨海默病的方法。
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公开(公告)号:US20090143371A1
公开(公告)日:2009-06-04
申请号:US12325293
申请日:2008-12-01
IPC分类号: A61K31/541 , C07D413/02 , A61K31/4439 , C07D413/14 , C07D417/14 , C07D487/02 , A61P25/00 , A61K31/519 , A61K31/501 , A61K31/4545 , C07D295/00 , A61K31/5377
CPC分类号: C07D413/12 , C07D413/14 , C07D417/14 , C07D487/04 , C07D491/08 , C07D491/10
摘要: The present invention is concerned with isoxazole-pyridine derivatives of formula I wherein X, R1 to R6 are as described herein. The compounds are active on the GABA A α5 receptor binding site and useful for the treatment of cognitive disorders, such as Alzheimer's disease.
摘要翻译: 本发明涉及式I的异恶唑 - 吡啶衍生物,其中X,R 1至R 6如本文所述。 这些化合物对GABA Aα5受体结合位点是有活性的,可用于治疗认知障碍,如阿尔茨海默病。
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公开(公告)号:US07541372B2
公开(公告)日:2009-06-02
申请号:US11639695
申请日:2006-12-15
申请人: Bernd Buettelmann , Bo Han , Henner Knust , Andreas Koblet , Andrew Thomas
发明人: Bernd Buettelmann , Bo Han , Henner Knust , Andreas Koblet , Andrew Thomas
IPC分类号: A61K31/422 , A61K31/4245 , C07D261/06 , C07D271/07
CPC分类号: C07D413/04 , C07D413/14
摘要: The present invention is concerned with isoxazol-4-yl-oxadiazole derivatives of formula wherein R1, R2, and R3, are as defined in the specification and pharmaceutically acceptable acid addition salts thereof. This class of compounds has 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.
摘要翻译: 本发明涉及下式的异恶唑-4-基 - 恶二唑衍生物,其中R 1,R 2和R 3如说明书中所定义及其药学上可接受的酸加成盐。 这类化合物对GABA Aα5受体结合位点具有高亲和力和选择性,可用作认知增强剂或用于治疗认知障碍如阿尔茨海默病。
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公开(公告)号:US20090131463A1
公开(公告)日:2009-05-21
申请号:US12359541
申请日:2009-01-26
申请人: Bernard Barlaam , Andrew Pape , Andrew Thomas
发明人: Bernard Barlaam , Andrew Pape , Andrew Thomas
IPC分类号: A61K31/506 , C07D401/02 , A61P35/00
CPC分类号: C07D401/14 , C07D403/14 , C07D405/14 , C07D413/14
摘要: The invention provides compounds of formula in which R1, R2, R3 and R4 have the meanings defined in the specification; processes for their preparation; pharmaceutical compositions containing them; a process for preparing the pharmaceutical compositions; and their use in therapy.
摘要翻译: 本发明提供式R1化合物,其中R1,R2,R3和R4具有本说明书中定义的含义; 其准备过程; 含有它们的药物组合物; 制备药物组合物的方法; 及其在治疗中的应用。
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公开(公告)号:US07512234B2
公开(公告)日:2009-03-31
申请号:US09816683
申请日:2001-03-23
申请人: James Thomas Edward McDonnell , Andrew Thomas , Michael P. Spratt , John Deryk Waters , Simon E. Crouch
发明人: James Thomas Edward McDonnell , Andrew Thomas , Michael P. Spratt , John Deryk Waters , Simon E. Crouch
IPC分类号: H04K1/00
CPC分类号: H04W64/00 , H04L63/0442 , H04L67/18 , H04M15/00 , H04M15/80 , H04M15/8033 , H04M2215/2026 , H04M2215/74 , H04M2215/7435 , H04W4/02 , H04W4/24 , H04W12/02
摘要: Location data about a mobile entity (20) is provided in encrypted form by a location server (79) to a recipient that is one of the mobile entity (20) or a service system (40) usable by the mobile entity. The location data (P) is encrypted such that it can only to be decrypted using a secret available to a decryption entity (80) that is not under the control of the recipient. This permits location data (P) to be provided in a confidential manner to service systems (40) and also protects billing relationships between participants. A mechanism is also described for limiting the accuracy of decrypted location data (L) made available to a service system (40).
摘要翻译: 关于移动实体(20)的位置数据由位置服务器(79)以加密形式提供给作为移动实体可用的移动实体(20)或服务系统(40)之一的接收者。 位置数据(P)被加密,使得其仅能够使用对不在接收者的控制下的解密实体(80)可用的秘密进行解密。 这允许以保密方式向服务系统(40)提供位置数据(P),并且还保护参与者之间的计费关系。 还描述了一种用于限制可用于服务系统(40)的解密位置数据(L)的精度的机制。
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公开(公告)号:US20090005370A1
公开(公告)日:2009-01-01
申请号:US12139535
申请日:2008-06-16
IPC分类号: A61K31/541 , C07D261/06 , A61K31/422 , A61K31/4439 , A61K31/506 , A61K31/497 , A61P25/00 , C07D241/10 , C07D239/24 , C07D213/02 , C07D417/14
CPC分类号: C07D413/04 , C07D413/14
摘要: The present invention is concerned isoxazole-imidazole derivatives having affinity and selectivity for GABA A α5 receptor binding site, their manufacture, pharmaceutical compositions containing them and their use for enhancing cognition or for the treatment of cognitive disorders like Alzheimer's disease. In particular, the present invention is concerned with aryl-isoxazol-4-yl-imidazole derivatives of formula I wherein R1, R2 and R3 are as described in the specification.
摘要翻译: 本发明涉及对GABA Aα5受体结合位点具有亲和性和选择性的异恶唑咪唑衍生物,其制备方法,含有它们的药物组合物及其用于增强认知或治疗认知障碍如阿尔茨海默病的用途。 特别地,本发明涉及式I的芳基 - 异恶唑-4-基 - 咪唑衍生物,其中R 1,R 2和R 3如说明书中所述。
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公开(公告)号:US20080072866A1
公开(公告)日:2008-03-27
申请号:US11659695
申请日:2005-08-31
申请人: Anthony Wallis , Andrew Thomas
发明人: Anthony Wallis , Andrew Thomas
IPC分类号: F01L7/16
摘要: An axial flow rotary valve (1) for an internal combustion engine comprising a cylinder head (10) having a bore in which an axial flow rotary valve (1) rotates. The valve having a cylindrical centre portion (4), and an inlet and an exhaust port (2, 3) terminating as openings (7, 8) in the centre portion, the openings periodically communicating with a combustion chamber (23) through a window (15) in the bore. The clearance between the centre portion and the bore being sealed by an array of floating seals comprising at least two axial seals (16a, 16b) spaced apart on opposite sides of the window. The assembly further comprising at least one floating axially extending masking seal (5) being disposed outside the window and circumferentially remote from the axial seals.
摘要翻译: 一种用于内燃机的轴流式旋转阀(1),其包括具有轴向流动旋转阀(1)旋转的孔的气缸盖(10)。 所述阀具有圆柱形中心部分(4),以及在中心部分终止于开口(7,8)的入口和排气口(2,3),所述开口通过窗口周期性地连通燃烧室(23) (15)。 中心部分和孔之间的间隙由浮动密封件阵列密封,其包括在窗的相对侧上间隔开的至少两个轴向密封件(16a,16b)。 所述组件还包括至少一个浮动的轴向延伸的掩蔽密封件(5),所述掩蔽密封件设置在所述窗户的外部并且周向地远离所述轴向密封件。
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公开(公告)号:US20070117791A1
公开(公告)日:2007-05-24
申请号:US11652970
申请日:2007-01-12
IPC分类号: A61K31/55
CPC分类号: C07D223/16
摘要: The present invention relates to methods for making and using novel benzazepine derivatives of the following formula: wherein R1, R2, R3, R4 and R5, X, X′, Y and Y′ are as defined in the description and claims, processes for their preparation, pharmaceutical compositions containing said derivatives and their use for the preparation of medicaments useful for the prevention and treatment of diseases in which selective inhibition of monoamine oxidase B activity plays a role or is implicated.
摘要翻译: 本发明涉及制备和使用下式的新型苯并氮杂衍生物的方法:其中R 1,R 2,R 3,R 3, 其中,X,X',Y和Y'如说明书和权利要求书中所定义,其制备方法,含有所述衍生物的药物组合物及其用途 用于制备可用于预防和治疗单胺氧化酶B活性的选择性抑制发挥作用或牵连的疾病的药物。
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公开(公告)号:US07171361B2
公开(公告)日:2007-01-30
申请号:US10013934
申请日:2001-12-13
CPC分类号: G10L15/19 , G10L2015/228
摘要: The grammar of the speech input to a voice service system is normally specified by the voice service system. However, this can produce problems in respect of idioms, such as dates, which are expressed different ways by different users. To facilitate the handling of idioms, a user is permitted to specify their own idiom grammar which is then used by the voice service system to interpret idioms in speech input from that user. Typically, the normal grammar of speech input is specified by grammar tags used to mark up a voice page script interpreted by a voice page browser; in this case, it will generally be the voice browser that is responsible for employing the user-specified idiom grammar to interpret the corresponding idiom in the speech input by the user. The user-specified grammar can be pre-specified directly to the voice browser by the user or fetched by the browser from a remote location on the fly.
摘要翻译: 输入到语音服务系统的语音语法通常由语音服务系统指定。 然而,这可能会在诸如日期之间的成语中产生问题,这些习惯用不同的用户表示不同的方式。 为了便于处理成语,允许用户指定自己的成语语法,然后由语音服务系统使用该语法来解释来自该用户的语音输入中的成语。 通常,语音输入的正常语法由用于标记语音页面浏览器解释的语音页面脚本的语法标签指定; 在这种情况下,通常是语音浏览器,负责采用用户指定的习语语法来解释用户输入的语音中的相应成语。 用户指定的语法可以由用户直接预先指定给语音浏览器,或者由浏览器从远程位置即时获取。
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