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公开(公告)号：US08518974B2
公开(公告)日：2013-08-27
申请号：US13370444
申请日：2012-02-10
IPC分类号： A61K31/4427 , C07D413/12
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：US07851469B2
公开(公告)日：2010-12-14
申请号：US12139535
申请日：2008-06-16
IPC分类号： A61K31/541 , A61K31/422 , A61K31/4439 , A61K31/506 , C07D261/06 , C07D241/10 , C07D239/24 , C07D213/02
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，其制造方法，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氏病的用途。 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：US20090143385A1
公开(公告)日：2009-06-04
申请号：US12277331
申请日：2008-11-25
IPC分类号： A61K31/5377 , C07D413/02 , C07D413/14 , A61K31/501
CPC分类号： C07D413/12 , C07D413/14 , C07D487/04
摘要： The invention relates to isoxazolo-pyridazine compounds, in particular those of formula I as described above and to a pharmaceutically acceptable salts thereof, having affinity and selectivity for the GABA A α5 receptor binding site, their manufacture, pharmaceutical compositions containing them and their use as cognitive enhancers or for the treatment of cognitive disorders like Alzheimer's disease.
摘要翻译： 本发明涉及异恶唑并哒嗪化合物，特别是上述式I化合物及其可药用盐，对GABA Aα5受体结合位点具有亲和力和选择性，其制备方法，含有它们的药物组合物及其作为 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：US08357703B2
公开(公告)日：2013-01-22
申请号：US12772250
申请日：2010-05-03
IPC分类号： A61K31/4427 , C07D413/12
CPC分类号： C07D413/12 , C07D413/14
摘要： The present invention is concerned with novel isoxazoles of formula I wherein X, R1, R2, R3 and R4 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 therapeutics.
摘要翻译： 本发明涉及式I的新异恶唑，其中X，R 1，R 2，R 3和R 4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 Aα5受体具有亲和性和选择性。 此外，本发明涉及制备式I的活性化合物，含有它们的药物组合物及其作为治疗剂的用途。
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公开(公告)号：US07943619B2
公开(公告)日：2011-05-17
申请号：US12277331
申请日：2008-11-25
IPC分类号： C07D417/12 , A61K31/501 , A61P25/28
CPC分类号： C07D413/12 , C07D413/14 , C07D487/04
摘要： The invention relates to isoxazolo-pyridazine compounds, in particular those of formula I as described above and to a pharmaceutically acceptable salts thereof, having affinity and selectivity for the GABA A α5 receptor binding site, their manufacture, pharmaceutical compositions containing them and their use as cognitive enhancers or for the treatment of cognitive disorders like Alzheimer's disease.
摘要翻译： 本发明涉及异恶唑并哒嗪化合物，特别是上述式I化合物及其可药用盐，对GABA Aα5受体结合位点具有亲和力和选择性，其制备方法，含有它们的药物组合物及其作为 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：US07618973B2
公开(公告)日：2009-11-17
申请号：US12277326
申请日：2008-11-25
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 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：US20120184538A1
公开(公告)日：2012-07-19
申请号：US13370444
申请日：2012-02-10
IPC分类号： A61K31/541 , C07D413/14 , C07D417/14 , A61P25/28 , A61K31/444 , A61K31/501 , A61K31/4545 , A61K31/5377 , C07D413/12 , A61K31/4439
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。 该化合物对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：US20100286117A1
公开(公告)日：2010-11-11
申请号：US12772250
申请日：2010-05-03
IPC分类号： A61K31/397 , C07D413/12 , A61K31/4439 , C07D279/12 , A61K31/54 , A61P25/00
CPC分类号： C07D413/12 , C07D413/14
摘要： The present invention is concerned with novel isoxazoles of formula I wherein X, R1, R2, R3 and R4 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 therapeutics.
摘要翻译： 本发明涉及式I的新异恶唑，其中X，R 1，R 2，R 3和R 4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 Aα5受体具有亲和性和选择性。 此外，本发明涉及制备式I的活性化合物，含有它们的药物组合物及其作为治疗剂的用途。
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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：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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