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1. 发明申请

US20070082936A1 Aryl-isoxazole-4-carbonyl-indole-carboxylic acid amide derivatives 失效
标题翻译：芳基异恶唑-4-羰基 - 吲哚羧酸酰胺衍生物
公开(公告)号：US20070082936A1
公开(公告)日：2007-04-12
申请号：US11543178
申请日：2006-10-04
申请人： Bernd Buettelmann , Bo Han , Henner Knust , Matthias Nettekoven , Andrew Thomas
发明人： Bernd Buettelmann , Bo Han , Henner Knust , Matthias Nettekoven , Andrew Thomas
IPC分类号： A61K31/42 , C07D413/02
CPC分类号： C07D413/14
摘要： The present invention is concerned with aryl-isoxazole-4-carbonyl-indole-carboxylic acid amide derivatives of formula I wherein R1, R2, R3, R4, and R5 are as defined in the specification and claims and with their pharmaceutically acceptable acid addition salts. The invention also relates to methods for preparing such compounds. This class of compounds has a 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. Thus, the invention also is concerned with pharmaceutical compositions containing compounds of formula I or their pharmaceutically acceptable acid addition salts and methods for the treatment of GABA A α5 mediated diseases, including Alzheimer's disease.
摘要翻译：本发明涉及式I的芳基 - 异恶唑-4-羰基 - 吲哚 - 羧酸酰胺衍生物，其中R 1，R 2，R 3， R 4，R 4和R 5如说明书和权利要求书及其药学上可接受的酸加成盐所定义。本发明还涉及制备这些化合物的方法。这类化合物对GABA Aα5受体结合位点具有高亲和力和选择性，可能作为认知增强剂或治疗阿尔茨海默病等认知障碍。因此，本发明还涉及含有式I化合物或其药学上可接受的酸加成盐的药物组合物和用于治疗包括阿尔茨海默氏病在内的GABA Aα5介导的疾病的方法。

2. 发明申请

US20070066668A1 Isoxazolo derivatives 失效
标题翻译：异恶唑衍生物
公开(公告)号：US20070066668A1
公开(公告)日：2007-03-22
申请号：US11520394
申请日：2006-09-13
申请人： Bernd Buettelmann , Bo Han , Henner Knust , Matthias Nettekoven , Andrew Thomas
发明人： Bernd Buettelmann , Bo Han , Henner Knust , Matthias Nettekoven , Andrew Thomas
IPC分类号： A61K31/42 , C07D413/02
CPC分类号： C07D413/14 , C07D413/06 , C07D451/06
摘要： The present invention is concerned with aryl-isoxazole-4-carbonyl-pyrrole-2-carboxylic acid amide derivatives of formula wherein R1, R2, R3, R4, and R5, and m are as defined herein and with their pharmaceutically acceptable acid addition salts. This class of compounds have high affinity and selectivity for GABA A α5 receptor binding sites and therefore may be useful as cognitive enhancer or for the treatment of cognitive disorders like Alzheimer's disease.
摘要翻译：本发明涉及下式的芳基 - 异恶唑-4-羰基 - 吡咯-2-羧酸酰胺衍生物其中R 1，R 2，R 3， R 4，R 4和R 5，m如本文所定义，并与其药学上可接受的酸加成盐反应。这类化合物对GABA Aα5受体结合位点具有高亲和力和选择性，因此可用作认知增强剂或治疗认知障碍如阿尔茨海默病。

3. 发明授权

US07388025B2 3-aryl-isoxazole-4-carbonyl-benzofuran derivatives 失效
标题翻译： 3-芳基 - 异恶唑-4-羰基 - 苯并呋喃衍生物
公开(公告)号：US07388025B2
公开(公告)日：2008-06-17
申请号：US11590571
申请日：2006-10-31
申请人： Bernd Buettelmann , Bo Han , Henner Knust , Matthias Nettekoven , Andrew Thomas
发明人： Bernd Buettelmann , Bo Han , Henner Knust , Matthias Nettekoven , Andrew Thomas
IPC分类号： A61K31/42 , C07D413/02
CPC分类号： C07D413/06 , C07D413/14
摘要： The present invention is concerned with 3-aryl-isoxazole-4-carbonyl-benzofuran derivatives of formula I wherein R1, R2, and R3 are as defined in the specification and claims and with their pharmaceutically acceptable acid addition salts. These compounds have a 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3-芳基 - 异恶唑-4-羰基 - 苯并呋喃衍生物，其中R 1，R 2，R 3和R 3， SUP>如说明书和权利要求书及其药学上可接受的酸加成盐所定义。这些化合物对GABA Aα5受体结合位点具有高亲和力和选择性，并且可用作认知增强剂或用于治疗诸如阿尔茨海默病的认知障碍。

4. 发明申请

US20070105922A1 3-aryl-isoxazole-4-carbonyl-indole derivatives 失效
标题翻译： 3-芳基 - 异恶唑-4-羰基 - 吲哚衍生物
公开(公告)号：US20070105922A1
公开(公告)日：2007-05-10
申请号：US11590571
申请日：2006-10-31
申请人： Bernd Buettelmann , Bo Han , Henner Knust , Matthias Nettekoven , Andrew Thomas
发明人： Bernd Buettelmann , Bo Han , Henner Knust , Matthias Nettekoven , Andrew Thomas
IPC分类号： A61K31/42 , C07D413/02
CPC分类号： C07D413/06 , C07D413/14
摘要： The present invention is concerned with 3-aryl-isoxazole-4-carbonyl-benzofuran derivatives of formula I wherein R1, R2, and R3 are as defined in the specification and claims and with their pharmaceutically acceptable acid addition salts. These compounds have a 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3-芳基 - 异恶唑-4-羰基 - 苯并呋喃衍生物，其中R 1，R 2，R 3和R 3， SUP>如说明书和权利要求书及其药学上可接受的酸加成盐所定义。这些化合物对GABA Aα5受体结合位点具有高亲和力和选择性，并且可用作认知增强剂或用于治疗诸如阿尔茨海默病的认知障碍。

5. 发明授权

US07378435B2 Aryl-isoxazole-4-carbonyl-indole-carboxylic acid amide derivatives 失效
标题翻译：芳基异恶唑-4-羰基 - 吲哚羧酸酰胺衍生物
公开(公告)号：US07378435B2
公开(公告)日：2008-05-27
申请号：US11543178
申请日：2006-10-04
申请人： Bernd Buettelmann , Bo Han , Henner Knust , Matthias Nettekoven , Andrew Thomas
发明人： Bernd Buettelmann , Bo Han , Henner Knust , Matthias Nettekoven , Andrew Thomas
IPC分类号： A61K31/42 , C07D413/02
CPC分类号： C07D413/14
摘要： The present invention is concerned with aryl-isoxazole-4-carbonyl-indole-carboxylic acid amide derivatives of formula I wherein R1, R2, R3, R4, and R5 are as defined in the specification and claims and with their pharmaceutically acceptable acid addition salts. The invention also relates to methods for preparing such compounds. This class of compounds has a 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. Thus, the invention also is concerned with pharmaceutical compositions containing compounds of formula I or their pharmaceutically acceptable acid addition salts and methods for the treatment of GABA Aα5 mediated diseases, including Alzheimer's disease.
摘要翻译：本发明涉及式I的芳基 - 异恶唑-4-羰基 - 吲哚 - 羧酸酰胺衍生物，其中R 1，R 2，R 3， R 4，R 4和R 5如说明书和权利要求书及其药学上可接受的酸加成盐所定义。本发明还涉及制备这些化合物的方法。这类化合物对GABA Aα5受体结合位点具有高亲和力和选择性，可能作为认知增强剂或治疗阿尔茨海默病等认知障碍。因此，本发明还涉及含有式I化合物或其药学上可接受的酸加成盐和用于治疗包括阿尔茨海默病在内的GABA Aalpha5介导的疾病的方法的药物组合物。

6. 发明申请

US20070191421A1 Aryl-isoxazol-4-yl-imidazo[1,5-a]pyridine derivatives 失效
标题翻译：芳基异恶唑-4-基 - 咪唑并[1,5-a]吡啶衍生物
公开(公告)号：US20070191421A1
公开(公告)日：2007-08-16
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： A61K31/4745 , 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。

7. 发明申请

US20070161654A1 Aryl-isoxazol-4-yl-imidazole derivatives 失效
标题翻译：芳基异恶唑-4-基 - 咪唑衍生物
公开(公告)号：US20070161654A1
公开(公告)日：2007-07-12
申请号：US11640622
申请日：2006-12-18
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： A61K31/506 , A61K31/4439 , A61K31/42 , C07D413/14
CPC分类号： C07D413/04
摘要： The present invention is concerned with aryl-isoxazol-4-yl-imidazole derivatives of formula I: wherein R1 to R6 are as defmed 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 - 咪唑衍生物：其中R 1至R 6如本说明书和药学上可接受的酸所定义其加成盐。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。

8. 发明授权

US07541372B2 Aryl-isoxazolo-4-yl-oxadiazole derivatives 失效
标题翻译：芳基异恶唑-4-基 - 恶二唑衍生物
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。

9. 发明授权

US07956074B2 Aryl-isoxazolo-4-yl-oxadiazole derivatives 失效
标题翻译：芳基异恶唑-4-基 - 恶二唑衍生物
公开(公告)号：US07956074B2
公开(公告)日：2011-06-07
申请号：US12422317
申请日：2009-04-13
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 , C07D271/10
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，可能作为认知增强剂或治疗阿尔茨海默病等认知障碍。

10. 发明授权

US07585874B2 Aryl-isoxazol-4-yl-imidazo[1,2-a]pyridine derivatives 失效
标题翻译：芳基异恶唑-4-基 - 咪唑并[1,2-a]吡啶衍生物
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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