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公开(公告)号：US07902201B2
公开(公告)日：2011-03-08
申请号：US12788338
申请日：2010-05-27
IPC分类号： A61K31/4965
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 the present invention are inverse agonists of GABAAα5. 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力和选择性，其制备和含有它们的药物组合物。 本发明的化合物是GABAAα5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：US20100286132A1
公开(公告)日：2010-11-11
申请号：US12768762
申请日：2010-04-28
IPC分类号： A61K31/541 , C07D413/12 , A61K31/4439 , C07D413/14 , A61K31/5377 , A61K31/444 , C07D279/12 , C07D211/60 , A61K31/4545 , A61P25/28
CPC分类号： C07D413/12 , C07D413/14 , C07D417/14
摘要： The present invention is concerned with isoxazole-pyridines of formula I, having affinity and selectivity for GABA A α5 receptor, their manufacture, pharmaceutical compositions containing them and their use as pharmaceuticals. 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，对GABA Aα5受体具有亲和性和选择性，其制备方法，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。
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公开(公告)号：US20100256154A1
公开(公告)日：2010-10-07
申请号：US12788338
申请日：2010-05-27
IPC分类号： A61K31/498 , C07D403/02 , A61K31/497 , A61P25/28
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 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力和选择性，其制备和含有它们的药物组合物。 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：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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