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公开(公告)号：US20100256127A1
公开(公告)日：2010-10-07
申请号：US12748524
申请日：2010-03-29
申请人： Bernd Buettelmann , Stephen Deems Gabriel , Steven Paul Hanlon , Roland Jakob-Roetne , Matthew C. Lucas , Paul Spurr , Andrew Thomas , Pius Waldmeier
发明人： Bernd Buettelmann , Stephen Deems Gabriel , Steven Paul Hanlon , Roland Jakob-Roetne , Matthew C. Lucas , Paul Spurr , Andrew Thomas , Pius Waldmeier
IPC分类号： A61K31/465 , C07D413/12 , C07D417/14 , A61K31/541 , C07D413/14 , A61K31/5377 , A61P25/28
CPC分类号： C07D413/12 , C07D413/14
摘要： The present invention is concerned with novel hydroxy-methyl isoxazole derivatives of formula I wherein R1, R2 and R3 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 pharmaceuticals.
摘要翻译： 本发明涉及式I的新型羟基 - 甲基异恶唑衍生物，其中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的活性化合物，含有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：US20100216845A1
公开(公告)日：2010-08-26
申请号：US12706722
申请日：2010-02-17
IPC分类号： A61K31/4439 , C07D413/06 , C07D413/14
CPC分类号： C07D413/06 , C07D413/14
摘要： The present invention is concerned with novel isoxazole-pyridines of formula I wherein R1, R2, R3 and L 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 pharmaceutical agents.
摘要翻译： 本发明涉及式I的新的异恶唑 - 吡啶，其中R 1，R 2，R 3和L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药剂的用途。
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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：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：US08389550B2
公开(公告)日：2013-03-05
申请号：US12706722
申请日：2010-02-17
IPC分类号： A61K31/4439 , C07D413/06
CPC分类号： C07D413/06 , C07D413/14
摘要： The present invention is concerned with novel isoxazole-pyridines of formula I wherein R1, R2, R3 and L 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 pharmaceutical agents.
摘要翻译： 本发明涉及式I的新的异恶唑 - 吡啶，其中R 1，R 2，R 3和L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药剂的用途。
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公开(公告)号：US08222246B2
公开(公告)日：2012-07-17
申请号：US12748524
申请日：2010-03-29
申请人： Bernd Buettelmann , Stephen Deems Gabriel , Steven Paul Hanlon , Roland Jakob-Roetne , Matthew C. Lucas , Paul Spurr , Andrew Thomas , Pius Waldmeier
发明人： Bernd Buettelmann , Stephen Deems Gabriel , Steven Paul Hanlon , Roland Jakob-Roetne , Matthew C. Lucas , Paul Spurr , Andrew Thomas , Pius Waldmeier
IPC分类号： C07D413/02 , A61K31/44
CPC分类号： C07D413/12 , C07D413/14
摘要： The present invention is concerned with novel hydroxy-methyl isoxazole derivatives of formula I wherein R1, R2 and R3 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 pharmaceuticals.
摘要翻译： 本发明涉及式I的新型羟基 - 甲基异恶唑衍生物，其中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的活性化合物，含有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：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：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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![Substituted imidazo-[1,5-a][1,2,4]triazolo[1,5-d][1,4] benzodiazepine derivatives](/abs-image/US/2009/03/24/US07507729B2/abs.jpg.150x150.jpg)
10.发明授权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：US07507729B2
公开(公告)日：2009-03-24
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： 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 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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