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公开(公告)号：US20130281690A1
公开(公告)日：2013-10-24
申请号：US13916264
申请日：2013-06-12
IPC分类号： C07D413/12 , C07D417/14 , C07D487/04 , C07D413/14
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.
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公开(公告)号：US20130274467A1
公开(公告)日：2013-10-17
申请号：US13916068
申请日：2013-06-12
IPC分类号： C07D413/14 , 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.
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3.发明公开公开(公告)号：US20230183225A1
公开(公告)日：2023-06-15
申请号：US18107741
申请日：2023-02-09
IPC分类号： C07D413/12 , A61K31/444 , A61K31/4985 , A61K31/5377 , A61K31/541 , A61K31/551 , A61K31/5517 , A61K31/4439 , C07D413/14 , C07D487/04 , C07D487/14
CPC分类号： C07D413/12 , A61K31/444 , A61K31/541 , A61K31/551 , A61K31/4439 , A61K31/4985 , A61K31/5377 , A61K31/5517 , C07D413/14 , C07D487/04 , C07D487/14
摘要： The present invention relates to the pharmaceutical use of selective GABA A α5 negative allosteric modulators for the treatment, prevention and/or delay of progression of central nervous system (CNS) conditions related to excessive GABAergic inhibition in the brain.
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公开(公告)号：US08785435B2
公开(公告)日：2014-07-22
申请号：US13650159
申请日：2012-10-12
发明人： Pascal Dott , Olaf Grassmann , Michael Kammerer , Joachim Manns , Urs Schwitter , Andrew Thomas , Nicole Wyttenbach
IPC分类号： C07D413/12 , C07D417/14
CPC分类号： C07D413/12
摘要： The instant invention relates to novel solid forms of the compound of formula (I) as well as solvates, inclusion complexes with other suitable compounds, processes for their manufacture, pharmaceutical compositions containing these solid forms, and their use as pharmaceuticals.
摘要翻译： 本发明涉及式（I）化合物的新型固体形式以及溶剂合物，与其它合适化合物的包合物，其制备方法，含有这些固体形式的药物组合物及其作为药物的用途。
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公开(公告)号：US08604062B2
公开(公告)日：2013-12-10
申请号：US13650202
申请日：2012-10-12
发明人： Pascal Dott , Steven Paul Hanlon , Stefan Hildbrand , Hans Iding , Andrew Thomas , Pius Waldmeier
IPC分类号： A01N43/40 , A61K31/44 , C07D413/00 , C07D401/00 , C07D211/78 , C07D211/84
CPC分类号： C07D413/12 , C07D413/14 , C07D417/14 , C07D487/04
摘要： The present invention relates to a process for the preparation of a compound of formula (I) wherein R1 and R2 are as defined herein, which is useful as an intermediate in the preparation of active pharmaceutical compounds.
摘要翻译： 本发明涉及制备其中R 1和R 2如本文所定义的式（I）化合物的方法，其可用作制备活性药物化合物的中间体。
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公开(公告)号：US20220411415A1
公开(公告)日：2022-12-29
申请号：US17378410
申请日：2021-07-16
发明人： Bernd BUETTELMANN , Giuseppe Cecere , Bernhard Fasching , Katrin Groebke Zbinden , Maria-Clemencia Hernandez , Henner Knust , Andreas Koblet , Emmanuel Pinard , Andrew Thomas
IPC分类号： C07D413/14 , A61P25/28 , C07D471/04 , C07D487/10
摘要： Compounds having the formula (I) wherein R1, R2, R3, R4, R5, R6, X, Y and Z are as described herein, compositions including the compounds and methods of using the compounds.
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公开(公告)号：US20210053959A1
公开(公告)日：2021-02-25
申请号：US17094172
申请日：2020-11-10
IPC分类号： C07D413/12 , A61K31/444 , A61K31/4985 , A61K31/5377 , A61K31/541 , A61K31/551 , A61K31/5517 , A61K31/4439 , C07D413/14 , C07D487/04 , C07D487/14
摘要： The present invention relates to the pharmaceutical use of selective GABA A α5 negative allosteric modulators for the treatment, prevention and/or delay of progression of central nervous system (CNS) conditions related to excessive GABAergic inhibition in the brain.
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公开(公告)号：US09073908B2
公开(公告)日：2015-07-07
申请号：US13916317
申请日：2013-06-12
IPC分类号： A61K31/422 , C07D261/08 , C07D413/12 , C07D413/14 , C07D417/14 , C07D487/04 , C07D491/08 , C07D491/10
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：US08975397B2
公开(公告)日：2015-03-10
申请号：US14295535
申请日：2014-06-04
发明人： Pascal Dott , Olaf Grassmann , Michael Kammerer , Joachim Manns , Urs Schwitter , Andrew Thomas , Nicole Wyttenbach
IPC分类号： C07D413/12 , C07D417/14
CPC分类号： C07D413/12
摘要： The instant invention relates to novel solid forms of the compound of formula (I) as well as solvates, inclusion complexes with other suitable compounds, processes for their manufacture, pharmaceutical compositions containing these solid forms, and their use as pharmaceuticals.
摘要翻译： 本发明涉及式（I）化合物的新型固体形式以及溶剂合物，与其它合适化合物的包合物，其制备方法，含有这些固体形式的药物组合物及其作为药物的用途。
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公开(公告)号：US20130274468A1
公开(公告)日：2013-10-17
申请号：US13916191
申请日：2013-06-12
IPC分类号： C07D413/14 , C07D417/14 , C07D487/04 , 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.
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