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公开(公告)号：US08415379B2
公开(公告)日：2013-04-09
申请号：US12768762
申请日：2010-04-28
IPC分类号： A61K31/443 , C07D413/14
CPC分类号： C07D413/12 , C07D413/14 , C07D417/14
摘要： The present invention is concerned with isoxazole-pyridines of formula I, having affinity and selectivity for GABA A α5 receptor, their manufacture, pharmaceutical compositions containing them and their use as pharmaceuticals. The active compounds of the present invention are useful as cognitive enhancer 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 - 吡啶，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药物的用途。 本发明的活性化合物可用作认知增强剂或用于治疗和/或预防性治疗认知障碍如阿尔茨海默氏病。
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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：US08178522B2
公开(公告)日：2012-05-15
申请号：US12768779
申请日：2010-04-28
IPC分类号： A61K31/397 , A61K31/427 , A61K31/4439 , A61K31/541 , A61K31/5377 , C07D417/06 , C07D417/14
CPC分类号： C07D417/06 , C07D417/12 , C07D417/14
摘要： The present invention is concerned with isoxazole-thiazole derivatives of formula I, having affinity and selectivity for GABA A α5 receptor, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful as cognitive enhancer 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 - 噻唑衍生物，其具有对GABA Aα5受体的亲和性和选择性，它们的制备，含有它们的药物组合物及其作为治疗活性物质的用途。 本发明的活性化合物可用作认知增强剂或用于治疗和/或预防性治疗认知障碍如阿尔茨海默氏病。
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公开(公告)号：US20100286116A1
公开(公告)日：2010-11-11
申请号：US12768779
申请日：2010-04-28
IPC分类号： A61K31/397 , C07D417/06 , A61K31/427 , C07D417/14 , A61K31/4439 , A61K31/541 , A61K31/5377 , A61P25/00
CPC分类号： C07D417/06 , C07D417/12 , C07D417/14
摘要： The present invention is concerned with isoxazole-thiazole derivatives of formula I, having affinity and selectivity for GABA A α5 receptor, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful as cognitive enhancer 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 - 噻唑衍生物，其具有对GABA Aα5受体的亲和性和选择性，它们的制备，含有它们的药物组合物及其作为治疗活性物质的用途。 本发明的活性化合物可用作认知增强剂或用于治疗和/或预防性治疗认知障碍如阿尔茨海默氏病。
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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：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：US20100280020A1
公开(公告)日：2010-11-04
申请号：US12766202
申请日：2010-04-23
IPC分类号： A61K31/541 , A61K31/5377 , A61K31/4439 , C07D417/14 , C07D413/14 , C07D401/12 , A61P25/28 , A61P25/18 , A61P25/30 , A61P25/16 , A61P25/24
CPC分类号： C07D413/12 , C07D413/14
摘要： The present invention is concerned with novel isoxazole derivatives of formula I wherein X, R1, R2, R3, R4 and R5 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.
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公开(公告)号：US20100280019A1
公开(公告)日：2010-11-04
申请号：US12766125
申请日：2010-04-23
IPC分类号： A61K31/4439 , C07D413/12 , C07D413/14 , C07D417/14 , A61K31/5377 , A61K31/4545 , A61K31/541
CPC分类号： C07D413/12 , C07D413/14
摘要： The present invention is concerned with novel isoxazole derivatives of formula I wherein X, R1, R2, R3, R4 and R5 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的新型异恶唑衍生物，其中X，R 1，R 2，R 3，R 4和R 5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：US20100286115A1
公开(公告)日：2010-11-11
申请号：US12768770
申请日：2010-04-28
IPC分类号： A61K31/422 , A61K31/541 , A61K31/5377 , A61K31/454 , A61K31/4439 , C07D417/14 , C07D413/14 , C07D413/12 , A61P25/00
CPC分类号： C07D413/12 , C07D413/14
摘要： The present invention is concerned with isoxazole-pyrazoles of formula I, having affinity and selectivity for GABA A a5 receptor, their manufacture, pharmaceutical compositions containing them and their use as therapeutics. The active compounds of the present invention are useful as cognitive enhancer 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 - 吡唑，其具有对GABA A a5受体的亲和力和选择性，它们的制备，含有它们的药物组合物及其作为治疗剂的用途。 本发明的活性化合物可用作认知增强剂或用于治疗和/或预防性治疗认知障碍如阿尔茨海默氏病。
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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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