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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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![SUBSTITUTED IMIDAZO[1,5-A][1,2,4]TRIAZOLO[1,5-D][1,4]BENZODIAZEPINE DERIVATIVES](/abs-image/US/2010/03/25/US20100075954A1/abs.jpg.150x150.jpg)
92.发明申请SUBSTITUTED IMIDAZO[1,5-A][1,2,4]TRIAZOLO[1,5-D][1,4]BENZODIAZEPINE DERIVATIVES 失效取代的咪唑并[1,5-A] [1,2,4]三唑并[1,5-D] [1,4]苯并恶嗪衍生物公开(公告)号：US20100075954A1
公开(公告)日：2010-03-25
申请号：US12618802
申请日：2009-11-16
IPC分类号： A61K31/551 , C07D243/10 , A61P25/28
CPC分类号： A61K31/5517 , C07D487/14
摘要： The present invention is concerned with a method of treating Alzheimer's disease by administering a therapeutically effective amount of a substituted imidazo[1,5-a][1,2,4]triazolo[1,5-d][1,4]benzodiazepine of formula I wherein R1, R2, and R3 are as defined herein, and their pharmaceutically acceptable acid addition salts. The invention also provides novel compounds of formula I-A and pharmaceutical compositions containing them.
摘要翻译： 本发明涉及通过施用治疗有效量的取代咪唑并[1,5-a] [1,2,4]三唑并[1,5-d] [1,4]苯并二氮杂治疗阿尔茨海默病的方法 其中R 1，R 2和R 3如本文所定义，并且其药学上可接受的酸加成盐。 本发明还提供新颖的式I-A化合物和含有它们的药物组合物。
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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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![Aryl-isoxazol-4-yl-imidazo[1,2-a]pyridine derivatives](/abs-image/US/2009/09/08/US07585874B2/abs.jpg.150x150.jpg)
公开(公告)号：US07585874B2
公开(公告)日：2009-09-08
申请号：US11654183
申请日：2007-01-16
申请人： Bernd Buettelmann , Bo Han , Henner Knust , Andrew Thomas
发明人： Bernd Buettelmann , Bo Han , Henner Knust , Andrew Thomas
IPC分类号： A61K31/4353 , C07D471/02
CPC分类号： C07D471/04
摘要： The present invention is concerned with aryl-isoxazol-4-yl-imidazo[1,2-a]pyridine derivatives of formula I: wherein R1 to R5 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： 本发明涉及式I的芳基 - 异恶唑-4-基 - 咪唑并[1,2-a]吡啶衍生物：其中R 1至R 5如本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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![Substituted imidazol[1,5-A][1,2,4]triazolo[1,5-D][1,4]benzodiazepine derivatives](/abs-image/US/2009/04/07/US07514426B2/abs.jpg.150x150.jpg)
95.发明授权Substituted imidazol[1,5-A][1,2,4]triazolo[1,5-D][1,4]benzodiazepine derivatives 有权取代的咪唑[1,5-A] [1,2,4]三唑并[1,5-D] [1,4]苯并二氮杂衍生物公开(公告)号：US07514426B2
公开(公告)日：2009-04-07
申请号：US11252025
申请日：2005-10-17
IPC分类号： A61P25/28 , A61K31/55 , C07D243/00
CPC分类号： C07D487/14
摘要： The present invention is concerned with substituted imidazo[1,5-a][1,2,4]triazolo[1,5-d][1,4]benzodiazepine derivatives of formula I wherein R1 is hydrogen, halogen, lower alkyl, lower alkynyl, cycloalkyl, heterocycloalkyl, benzyl, cyano, lower alkoxy, OCF3, —NHR, —NHC(O)R or —NHSO2R; R2 is lower alkyl substituted by halogen; R3 is hydrogen, methyl or aryl; R is lower alkyl, cycloalkyl or aryl; and pharmaceutically acceptable acid addition salts thereof.
摘要翻译： 本发明涉及式I的取代咪唑并[1,5-a] [1,2,4]三唑并[1,5-d] [1,4]苯并二氮杂衍生物，其中R 1是氢，卤素，低级烷基， 低级炔基，环烷基，杂环烷基，苄基，氰基，低级烷氧基，OCF 3，-NHR，-NHC（O）R或-NHSO 2 R; R2是被卤素取代的低级烷基; R3是氢，甲基或芳基; R是低级烷基，环烷基或芳基; 及其药学上可接受的酸加成盐。
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![Aryl-isoxazol-4-yl-imidazo[1,5-a]pyridine derivatives](/abs-image/US/2008/07/15/US07399769B2/abs.jpg.150x150.jpg)
公开(公告)号：US07399769B2
公开(公告)日：2008-07-15
申请号：US11640768
申请日：2006-12-18
申请人： Bernd Buettelmann , Jiaqiang Dong , Bo Han , Henner Knust , Andrew Thomas
发明人： Bernd Buettelmann , Jiaqiang Dong , Bo Han , Henner Knust , Andrew Thomas
IPC分类号： A61K31/4353 , C07D471/02
CPC分类号： C07D471/04
摘要： The present invention is concerned with aryl-isoxazol-4-yl-imidazo[1,5-a]pyridine derivatives of formula wherein: R1, R2, and R3 are as defined herein and pharmaceutically acceptable acid addition salts thereof. These compounds have high affinity and selectivity for GABA A α5 receptor binding sites. The invention also relates to methods for enhancing cognition and treating cognitive disorders like Alzheimer's disease.
摘要翻译： 本发明涉及下式的芳基 - 异恶唑-4-基 - 咪唑并[1,5-a]吡啶衍生物其中：R 1，R 2，R 2，R 3和本文所定义的药学上可接受的酸加成盐。 这些化合物对GABA Aα5受体结合位点具有高亲和力和选择性。 本发明还涉及用于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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![Aryl-isoxazol-4-yl-imidazo[1,2-a]pyridine derivatives](/abs-image/US/2007/08/02/US20070179178A1/abs.jpg.150x150.jpg)
公开(公告)号：US20070179178A1
公开(公告)日：2007-08-02
申请号：US11654183
申请日：2007-01-16
申请人： Bernd Buettelmann , Bo Han , Henner Knust , Andrew Thomas
发明人： Bernd Buettelmann , Bo Han , Henner Knust , Andrew Thomas
IPC分类号： A61K31/4745 , C07D471/04
CPC分类号： C07D471/04
摘要： The present invention is concerned with aryl-isoxazol-4-yl-imidazo[1,2-a]pyridine derivatives of formula I: wherein R1 to R5 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： 本发明涉及式I的芳基 - 异恶唑-4-基 - 咪唑并[1,2-a]吡啶衍生物：其中R 1至R 5各自为 在本说明书中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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![Substituted imidazo-[1,5-a][1,2,4]triazolo[1,5-d][1,4] benzodiazepine derivatives](/abs-image/US/2007/04/12/US20070082890A1/abs.jpg.150x150.jpg)
98.发明申请Substituted imidazo-[1,5-a][1,2,4]triazolo[1,5-d][1,4] benzodiazepine derivatives 失效取代的咪唑并[1,5-a] [1,2,4]三唑并[1,5-d] [1,4]苯并二氮杂衍生物公开(公告)号：US20070082890A1
公开(公告)日：2007-04-12
申请号：US11542944
申请日：2006-10-04
申请人： Bernd Buettelmann , Henner Knust , Andrew Thomas
发明人： Bernd Buettelmann , Henner Knust , Andrew Thomas
IPC分类号： A61K31/551 , C07D487/14
CPC分类号： C07D487/14
摘要： The present invention is concerned with substituted imidazo[1,5-a][1,2,4]triazolo[1,5-d][1,4]benzodiazepine derivatives of the following formula wherein the definition of substituents is described in the claims. This class of compounds shows high affinity and selectivity for GABA A α5 receptor binding sites and might be useful as a cognitive enhancer or for the treatment of cognitive disorders like Alzheimer's disease.
摘要翻译： 本发明涉及下式的取代咪唑并[1,5-a] [1,2,4]三唑并[1,5-d] [1,4]苯并二氮杂衍生物，其中取代基的定义描述于 声称。 这类化合物对GABA Aα5受体结合位点显示出高亲和力和选择性，可能作为认知增强剂或治疗阿尔茨海默病等认知障碍。
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公开(公告)号：US09260408B2
公开(公告)日：2016-02-16
申请号：US13612956
申请日：2012-09-13
申请人： Johannes Aebi , Kurt Amrein , Benoit Hornsperger , Henner Knust , Bernd Kuhn , Yongfu Liu , Hans P. Maerki , Alexander V. Mayweg , Peter Mohr , Xuefei Tan , Mingwei Zhou
发明人： Johannes Aebi , Kurt Amrein , Benoit Hornsperger , Henner Knust , Bernd Kuhn , Yongfu Liu , Hans P. Maerki , Alexander V. Mayweg , Peter Mohr , Xuefei Tan , Mingwei Zhou
IPC分类号： C07D401/04 , C07D401/14 , C07D405/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D471/06 , C07D487/10 , C07F7/18 , A61P13/12 , A61P9/04 , A61P9/12
CPC分类号： C07D401/04 , C07D401/14 , C07D405/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D471/06 , C07D487/10 , C07F7/1804
摘要： The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6, R7, A1, A2 and A3 are as described herein, compositions including the compounds and methods of using the compounds. These compounds are useful for therapy or prophylaxis in a mammal, and in particular as aldosterone synthase (CYP11B2 or CYP11B1) inhibitors for the treatment or prophylaxis of chronic kidney disease, congestive heart failure, hypertension, primary aldosteronism and Cushing syndrome.
摘要翻译： 本发明提供具有通式（I）的新化合物，其中R1，R2，R3，R4，R5，R6，R7，A1，A2和A3如本文所述，包括该化合物的组合物和使用该化合物的方法。 这些化合物可用于治疗或预防哺乳动物，特别是用于治疗或预防慢性肾脏疾病，充血性心力衰竭，高血压，原发性醛固酮增多症和库兴综合征的醛固酮合酶（CYP11B2或CYP11B1）抑制剂。
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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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