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公开(公告)号：US08173652B2
公开(公告)日：2012-05-08
申请号：US12704548
申请日：2010-02-12
IPC分类号： A61K31/5377 , A61K31/42 , A61K31/454 , C07D413/06 , C07D413/14
CPC分类号： C07D261/18 , C07D413/14 , C07D417/12 , C07D487/10
摘要： The present invention is concerned with isoxazole-isoxazoles and isoxazole-isothiazoles of formula I, having affinity and selectivity for GABA A α5 receptor, their manufacture, pharmaceutical compositions containing them and their use as cognitive enhancers 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 - 异恶唑和异恶唑 - 异噻唑，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认知增强剂的用途或用于治疗和/或预防性治疗 认知障碍如阿尔茨海默病。
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2.发明申请公开(公告)号：US20100210651A1
公开(公告)日：2010-08-19
申请号：US12704548
申请日：2010-02-12
IPC分类号： A61K31/5377 , C07D413/06 , A61K31/42 , C07D413/14 , A61K31/454 , A61P25/28
CPC分类号： C07D261/18 , C07D413/14 , C07D417/12 , C07D487/10
摘要： The present invention is concerned with isoxazole-isoxazoles and isoxazole-isothiazoles of formula I, having affinity and selectivity for GABA A α5 receptor, their manufacture, pharmaceutical compositions containing them and their use as cognitive enhancers 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 - 异恶唑和异恶唑 - 异噻唑，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认知增强剂的用途或用于治疗和/或预防性治疗 认知障碍如阿尔茨海默病。
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公开(公告)号：US08742097B2
公开(公告)日：2014-06-03
申请号：US13287149
申请日：2011-11-02
IPC分类号： C07D401/12 , C07D403/10 , C07D403/12 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D471/04 , C07D491/107
CPC分类号： C07D401/12 , C07D403/10 , C07D403/12 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D471/04 , C07D491/107
摘要： The present invention is concerned with novel triazole compounds of formula (I) wherein A, X, Y, Z, R1, R2, and R3 are as described herein, as well as pharmaceutically acceptable salts and esters 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）的新型三唑化合物，其中A，X，Y，Z，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 Aα5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。
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公开(公告)号：US20120115844A1
公开(公告)日：2012-05-10
申请号：US13287149
申请日：2011-11-02
IPC分类号： A61K31/4439 , C07D413/14 , A61K31/5377 , C07D471/04 , A61K31/437 , C07D417/14 , A61K31/541 , C07D401/14 , A61K31/444 , A61P25/00 , A61P25/28 , A61P25/18 , A61P25/22 , A61P25/30 , A61P25/14 , A61P25/16 , C07D401/12
CPC分类号： C07D401/12 , C07D403/10 , C07D403/12 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D471/04 , C07D491/107
摘要： The present invention is concerned with novel triazole compounds of formula (I) wherein A, X, Y, Z, R1, R2, and R3 are as described herein, as well as pharmaceutically acceptable salts and esters 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）的新型三唑化合物，其中A，X，Y，Z，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 Aα5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。
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5.发明申请USE OF SELECTIVE GABA A ALPHA 5 NEGATIVE ALLOSTERIC MODULATORS FOR THE TREATMENT OF CENTRAL NERVOUS SYSTEM CONDITIONS 有权选择性GABA A ALPHA 5用于治疗中枢神经系统病症的阴性调节剂的使用公开(公告)号：US20120115839A1
公开(公告)日：2012-05-10
申请号：US13286240
申请日：2011-11-01
IPC分类号： A61K31/5517 , A61K31/4985 , A61P25/00 , A61K31/5377 , A61K31/444 , A61K31/4439 , A61K31/541
CPC分类号： C07D413/12 , A61K31/4439 , A61K31/444 , A61K31/4985 , A61K31/5377 , A61K31/541 , A61K31/551 , A61K31/5517 , C07D413/14 , C07D487/04 , C07D487/14
摘要： The present invention relates to the pharmaceutical use of selective GABA A α5 negative allosteric modulators for the treatment, prevention and/or delay of progression of central nervous system (CNS) conditions related to excessive GABAergic inhibition in the brain.
摘要翻译： 本发明涉及用于治疗，预防和/或延缓与脑中过量的GABA能抑制有关的中枢神经系统（CNS）病症进展的选择性GABA Aα5负变构调节剂的药物用途。
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6.发明授权Use of selective GABA A α5 negative allosteric modulators for the treatment of central nervous system conditions 有权使用选择性GABA Aα5负变构调节剂治疗中枢神经系统疾病公开(公告)号：US08835425B2
公开(公告)日：2014-09-16
申请号：US13286240
申请日：2011-11-01
IPC分类号： A61K31/54 , A01N43/16 , A61K31/42 , A61K31/5377 , A61K31/541 , A61K31/5517 , A61K31/551 , A61K31/444 , A61K31/4439 , A61K31/4985
CPC分类号： C07D413/12 , A61K31/4439 , A61K31/444 , A61K31/4985 , A61K31/5377 , A61K31/541 , A61K31/551 , A61K31/5517 , C07D413/14 , C07D487/04 , C07D487/14
摘要： The present invention relates to the pharmaceutical use of selective GABA A α5 negative allosteric modulators for the treatment, prevention and/or delay of progression of central nervous system (CNS) conditions related to excessive GABAergic inhibition in the brain.
摘要翻译： 本发明涉及用于治疗，预防和/或延缓与脑中过量的GABA能抑制有关的中枢神经系统（CNS）病症进展的选择性GABA Aα5负变构调节剂的药物用途。
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