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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。
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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。
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公开(公告)号:US20090197875A1
公开(公告)日:2009-08-06
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: A61K31/541 , C07D413/14 , A61K31/5377 , C07D417/14
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。
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公开(公告)号:US20070161686A1
公开(公告)日:2007-07-12
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: A61K31/4245 , C07D413/02
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,R 3和R 3为 在本说明书中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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公开(公告)号:US08404679B2
公开(公告)日:2013-03-26
申请号:US13452981
申请日:2012-04-23
申请人: Caterina Bissantz , Philippe Jablonski , Henner Knust , Andreas Koblet , Anja Limberg , Matthias Nettekoven , Hasane Ratni , Claus Riemer
发明人: Caterina Bissantz , Philippe Jablonski , Henner Knust , Andreas Koblet , Anja Limberg , Matthias Nettekoven , Hasane Ratni , Claus Riemer
IPC分类号: A61K31/496 , A61K31/498 , A61K31/5377 , A61K31/541 , C07D207/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D417/06 , A61K31/454 , A61K31/501 , C07D401/06 , C07D401/14 , C07D403/06 , C07D405/06
CPC分类号: C07D207/14 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/12 , C07D405/06 , C07D405/12 , C07D405/14 , C07D413/10
摘要: The present invention relates to compounds of formula I wherein R1, R2, R3, Ar and n are as defined herein and pharmaceutically active salts, racemic mixtures, enantiomers, optical isomers or tautomeric forms thereof. The compounds can be used for the treatment of depression, anxiety or schizophrenia.
摘要翻译: 本发明涉及其中R 1,R 2,R 3,Ar和n如本文所定义的药物活性盐,外消旋混合物,对映异构体,旋光异构体或其互变异构形式的式I化合物。 这些化合物可用于治疗抑郁,焦虑或精神分裂症。
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公开(公告)号:US20120208803A1
公开(公告)日:2012-08-16
申请号:US13452981
申请日:2012-04-23
申请人: Caterina Bissantz , Philippe Jablonski , Henner Knust , Andreas Koblet , Anja Limberg , Matthias Nettekoven , Hasane Ratni , Claus Riemer
发明人: Caterina Bissantz , Philippe Jablonski , Henner Knust , Andreas Koblet , Anja Limberg , Matthias Nettekoven , Hasane Ratni , Claus Riemer
IPC分类号: A61K31/496 , C07D403/14 , C07D405/14 , A61K31/498 , A61P25/24 , A61K31/541 , C07D413/06 , A61K31/5377 , A61P25/22 , C07D403/06 , C07D417/06
CPC分类号: C07D207/14 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/12 , C07D405/06 , C07D405/12 , C07D405/14 , C07D413/10
摘要: The present invention relates to compounds of formula I wherein R1, R2, R3, Ar and n are as defined herein and pharmaceutically active salts, racemic mixtures, enantiomers, optical isomers or tautomeric forms thereof. The compounds can be used for the treatment of depression, anxiety or schizophrenia.
摘要翻译: 本发明涉及其中R 1,R 2,R 3,Ar和n如本文所定义的药物活性盐,外消旋混合物,对映异构体,旋光异构体或其互变异构形式的式I化合物。 该化合物可用于治疗抑郁,焦虑或精神分裂症。
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公开(公告)号:US20110152233A1
公开(公告)日:2011-06-23
申请号:US12964769
申请日:2010-12-10
申请人: Henner Knust , Andreas Koblet , Matthias Nettekoven , Hasane Ratni , Claus Riemer , Walter Vifian
发明人: Henner Knust , Andreas Koblet , Matthias Nettekoven , Hasane Ratni , Claus Riemer , Walter Vifian
IPC分类号: A61K31/397 , A61K31/501 , A61K31/4965 , A61K31/506 , A61K31/4545 , C07D405/14 , C07D401/14 , C07D401/08
CPC分类号: C07D401/14 , C07D207/14 , C07D401/06 , C07D405/14
摘要: The present application relates to compounds of formula wherein R1, R2, R3, R4, and n are defined herein or to a pharmaceutically active salt thereof. The present compounds are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).
摘要翻译: 本申请涉及下式的化合物,其中R 1,R 2,R 3,R 4和n在本文中定义或其药物活性盐。 本发明化合物是用于治疗抑郁症,疼痛,精神病,帕金森病,精神分裂症,焦虑和注意缺陷多动障碍(ADHD)的高潜力NK-3受体拮抗剂。
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公开(公告)号:US20090312327A1
公开(公告)日:2009-12-17
申请号:US12482490
申请日:2009-06-11
申请人: Caterina Bissantz , Philippe Jablonski , Henner Knust , Andreas Koblet , Anja Limberg , Matthias Nettekoven , Hasane Ratni , Claus Riemer
发明人: Caterina Bissantz , Philippe Jablonski , Henner Knust , Andreas Koblet , Anja Limberg , Matthias Nettekoven , Hasane Ratni , Claus Riemer
IPC分类号: A61K31/5377 , C07D403/06 , A61K31/497 , A61K31/498 , C07D403/14 , C07D401/06 , A61K31/454 , C07D413/10 , C07D413/14
CPC分类号: C07D207/14 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/12 , C07D405/06 , C07D405/12 , C07D405/14 , C07D413/10
摘要: The present invention relates to compounds of formula I wherein R1, R2, R3, Ar and n are as defined herein and pharmaceutically active salts, racemic mixtures, enantiomers, optical isomers or tautomeric forms thereof. The compounds can be used for the treatment of depression, anxiety or schizophrenia.
摘要翻译: 本发明涉及其中R 1,R 2,R 3,Ar和n如本文所定义的药物活性盐,外消旋混合物,对映异构体,旋光异构体或其互变异构形式的式I化合物。 该化合物可用于治疗抑郁,焦虑或精神分裂症。
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公开(公告)号:US09226916B2
公开(公告)日:2016-01-05
申请号:US13779780
申请日:2013-02-28
申请人: Henner Knust , Andreas Koblet , Matthias Nettekoven , Hasane Ratni , Claus Riemer , Walter Vifian
发明人: Henner Knust , Andreas Koblet , Matthias Nettekoven , Hasane Ratni , Claus Riemer , Walter Vifian
IPC分类号: A61K31/445 , C07D401/06 , A61K31/40 , C07D207/14 , C07D403/06 , C07D405/06 , C07D407/04 , C07D413/06 , C07D417/14 , A61K31/4025 , A61K31/454 , A61K31/4545 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/5377
CPC分类号: A61K31/40 , A61K31/4025 , A61K31/454 , A61K31/4545 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/5377 , C07D207/14 , C07D401/06 , C07D403/06 , C07D405/06 , C07D407/04 , C07D413/06 , C07D417/14
摘要: The present invention relates to compounds of formula wherein R1, R2, R3, R4, Z, and n are as defined herein or to a pharmaceutically active salt thereof. Compounds of the invention are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).
摘要翻译: 本发明涉及下式的化合物,其中R 1,R 2,R 3,R 4,Z和n如本文所定义,或其药物活性盐。 本发明化合物是用于治疗抑郁,疼痛,精神病,帕金森病,精神分裂症,焦虑和注意缺陷多动障碍(ADHD)的高潜在NK-3受体拮抗剂。
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公开(公告)号:US20110144081A1
公开(公告)日:2011-06-16
申请号:US12961536
申请日:2010-12-07
申请人: Henner Knust , Andreas Koblet , Matthias Nettekoven , Hasane Ratni , Claus Riemer , Walter Vifian
发明人: Henner Knust , Andreas Koblet , Matthias Nettekoven , Hasane Ratni , Claus Riemer , Walter Vifian
IPC分类号: A61K31/454 , C07D401/06 , C07D405/14 , C07D207/14 , A61K31/40 , C07D401/14 , A61K31/4545 , C07D405/06 , A61K31/4025 , C07D413/06 , A61K31/5377 , C07D417/14 , A61K31/501 , C07D409/06 , C07D409/14 , C07D413/14 , A61K31/506 , A61K31/496 , A61P25/24 , A61P25/00 , A61P25/16 , A61P25/18 , A61P25/04 , A61P25/22
CPC分类号: A61K31/40 , A61K31/4025 , A61K31/454 , A61K31/4545 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/5377 , C07D207/14 , C07D401/06 , C07D403/06 , C07D405/06 , C07D407/04 , C07D413/06 , C07D417/14
摘要: The present invention relates to compounds of formula wherein R1, R2, R3, R4, Z, and n are as defined herein or to a pharmaceutically active salt thereof. Compounds of the invention are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).
摘要翻译: 本发明涉及下式的化合物,其中R 1,R 2,R 3,R 4,Z和n如本文所定义,或其药物活性盐。 本发明化合物是用于治疗抑郁,疼痛,精神病,帕金森病,精神分裂症,焦虑和注意缺陷多动障碍(ADHD)的高潜在NK-3受体拮抗剂。
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