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公开(公告)号：US20100256154A1
公开(公告)日：2010-10-07
申请号：US12788338
申请日：2010-05-27
IPC分类号： A61K31/498 , C07D403/02 , A61K31/497 , A61P25/28
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 invention also relates to methods for enhancing cognition and for treating cognitive disorders like Alzheimer's disease.
摘要翻译： 本发明涉及异恶唑并吡嗪衍生物及其药学上可接受的盐，其对GABA Aα5受体结合位点具有亲和力和选择性，其制备和含有它们的药物组合物。 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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公开(公告)号：US20100041886A1
公开(公告)日：2010-02-18
申请号：US12581192
申请日：2009-10-19
IPC分类号： C07D413/02
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： 本发明涉及异恶唑并吡嗪衍生物及其药学上可接受的盐，其对GABA Aα5受体结合位点具有亲和性和选择性，其制备和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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公开(公告)号：US20090143407A1
公开(公告)日：2009-06-04
申请号：US12277326
申请日：2008-11-25
IPC分类号： A61K31/497 , C07D413/02
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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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：US20090005370A1
公开(公告)日：2009-01-01
申请号：US12139535
申请日：2008-06-16
IPC分类号： A61K31/541 , C07D261/06 , A61K31/422 , A61K31/4439 , A61K31/506 , A61K31/497 , A61P25/00 , C07D241/10 , C07D239/24 , C07D213/02 , C07D417/14
CPC分类号： C07D413/04 , C07D413/14
摘要： The present invention is concerned isoxazole-imidazole derivatives having affinity and selectivity for GABA A α5 receptor binding site, their manufacture, pharmaceutical compositions containing them and their use for enhancing cognition or for the treatment of cognitive disorders like Alzheimer's disease. In particular, the present invention is concerned with aryl-isoxazol-4-yl-imidazole derivatives of formula I wherein R1, R2 and R3 are as described in the specification.
摘要翻译： 本发明涉及对GABA Aα5受体结合位点具有亲和性和选择性的异恶唑咪唑衍生物，其制备方法，含有它们的药物组合物及其用于增强认知或治疗认知障碍如阿尔茨海默病的用途。 特别地，本发明涉及式I的芳基 - 异恶唑-4-基 - 咪唑衍生物，其中R 1，R 2和R 3如说明书中所述。
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![Substitued imidazo [1,5-A][1,2,4]triazolo[1,5-D][1,4]benzodiazepine derivatives](/abs-image/US/2008/10/07/US07432256B2/abs.jpg.150x150.jpg)
36.发明授权Substitued 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：US07432256B2
公开(公告)日：2008-10-07
申请号：US11297691
申请日：2005-12-08
IPC分类号： A61P25/28 , A61K31/551 , C07D487/12
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 formula I wherein R1 is hydrogen, halogen, lower alkyl, lower alkyl substituted by halogen, lower alkoxy, lower alkoxy substituted by halogen, nitro, cycloalkyl, —O(CH2)mO(CH2)mOH or —C≡C—R′; R2 is hydrogen or methyl; R3 is lower alkyl, lower alkyl substituted by halogen, lower alkenyl, lower alkenyl substituted by halogen, lower alkynyl, —(CH2)n-cycloalkyl, —(CR′R″)m—CH3, phenyl that is unsubstituted or substituted by halogen, pyridinyl or thienyl each of which is unsubstituted or substituted by lower alkyl, —(CH2)n—NH-cycloalkyl, lower alkenyl-cycloalkyl, lower alkynyl-(CR′R″)mOH, or lower alkynyl-phenyl wherein the phenyl ring is unsubstituited or substituted by halogen, CF3, lower alkyl or lower alkoxy; R′ is hydrogen or lower alkyl; R″ is hydrogen, hydroxy or lower alkyl; n is 0, 1 or 2; m is 1, 2 or 3; and o is 1 or 2; and pharmaceutically acceptable acid addition salts thereof. This class of compounds have high affinity and selectivity for GABA A α5 receptor binding sites. Thus, the invention also relates to methods of enhancing cognition and treating cognitive disorders like Alzheimer's disease.
摘要翻译： 本发明涉及式I的取代的咪唑并[1,5-a] [1,2,4]三唑并[1,5-d] [1,4]苯并二氮杂衍生物，其中R 1， >是氢，卤素，低级烷基，被卤素取代的低级烷基，低级烷氧基，被卤素取代的低级烷氧基，硝基，环烷基，-O（CH 2 CH 2）m O （CH 2）2 OH或-C≡C-R'; R 2是氢或甲基; R 3是低级烷基，被卤素取代的低级烷基，低级烯基，被卤素取代的低级链烯基，低级炔基， - （CH 2 SO 2）n
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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：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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