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公开(公告)号:US07812021B2
公开(公告)日:2010-10-12
申请号:US12195545
申请日:2008-08-21
申请人: Philippe Jablonski , Kenichi Kawasaki , Henner Knust , Anja Limberg , Matthias Nettekoven , Hasane Ratni , Claus Riemer , Xihan Wu
发明人: Philippe Jablonski , Kenichi Kawasaki , Henner Knust , Anja Limberg , Matthias Nettekoven , Hasane Ratni , Claus Riemer , Xihan Wu
IPC分类号: A61K31/496 , A61K31/454 , A61K31/506 , A61K31/5377 , C07D207/12 , C07D401/12 , C07D403/12 , C07D487/04 , C07D491/107
CPC分类号: C07D401/14 , C07D207/08 , C07D401/06 , C07D403/06 , C07D403/14 , C07D487/04 , C07D491/04 , C07D491/10
摘要: The invention relates to a compound of general formula wherein Ar, R1, R2, R3, R4, n, o, p, s, X and are as defined herein or to a pharmaceutically active salt thereof, including all stereoisomeric forms, individual diastereoisomers and enantiomers of the compound of formula (I) as well as racemic and non-racemic mixtures thereof. The 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: 本发明涉及通式的化合物,其中Ar,R 1,R 2,R 3,R 4,n,o,p,s,X和如本文所定义或其药物活性盐,包括所有立体异构形式,各个非对映异构体和 式(I)化合物的对映异构体以及其外消旋和非外消旋混合物。 这些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:US08063075B2
公开(公告)日:2011-11-22
申请号:US12476267
申请日:2009-06-02
申请人: Philippe Jablonski , Kenichi Kawasaki , Henner Knust , Anja Limberg , Matthias Nettekoven , Hasane Ratni , Claus Riemer
发明人: Philippe Jablonski , Kenichi Kawasaki , Henner Knust , Anja Limberg , Matthias Nettekoven , Hasane Ratni , Claus Riemer
IPC分类号: A61K31/40 , A61K31/44 , C07D207/04 , C07D401/06
CPC分类号: C07D401/14 , C07D401/12
摘要: The present invention relates to compounds of formula I wherein R1, R2, R3, R′, Ar, m, n, and o are as defined herein. The invention also relates to pharmaceutical compositions containing compounds of formula I and methods for the manufacture of such compounds and compositions. 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: 本发明涉及式I化合物,其中R 1,R 2,R 3,R',Ar,m,n和o如本文所定义。 本发明还涉及含有式I化合物的药物组合物和制备这些化合物和组合物的方法。 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:US20090054644A1
公开(公告)日:2009-02-26
申请号:US12195545
申请日:2008-08-21
申请人: Philippe Jablonski , Kenichi Kawasaki , Henner Knust , Anja Limberg , Matthias Nettekoven , Hasane Ratni , Claus Riemer , Xihan Wu
发明人: Philippe Jablonski , Kenichi Kawasaki , Henner Knust , Anja Limberg , Matthias Nettekoven , Hasane Ratni , Claus Riemer , Xihan Wu
IPC分类号: C07D498/04 , C07D403/06 , C07D401/06 , C07D413/06 , C07D403/14
CPC分类号: C07D401/14 , C07D207/08 , C07D401/06 , C07D403/06 , C07D403/14 , C07D487/04 , C07D491/04 , C07D491/10
摘要: The invention relates to a compound of general formula wherein Ar, R1, R2, R3, R4, n, o, p, s, X and are as defined herein or to a pharmaceutically active salt thereof, including all stereoisomeric forms, individual diastereoisomers and enantiomers of the compound of formula (I) as well as racemic and non-racemic mixtures thereof. The 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: 本发明涉及通式的化合物,其中Ar,R 1,R 2,R 3,R 4,n,o,p,s,X和如本文所定义或其药物活性盐,包括所有立体异构形式,各个非对映异构体和 式(I)化合物的对映异构体以及其外消旋和非外消旋混合物。 这些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:US07893062B2
公开(公告)日:2011-02-22
申请号:US12102121
申请日:2008-04-14
申请人: Caterina Bissantz , Torsten Hoffmann , Philippe Jablonski , Henner Knust , Matthias Nettekoven , Hasane Ratni , Xihan Wu
发明人: Caterina Bissantz , Torsten Hoffmann , Philippe Jablonski , Henner Knust , Matthias Nettekoven , Hasane Ratni , Xihan Wu
IPC分类号: A61K31/4015 , A61K31/5377 , C07D207/04 , C07D413/02
CPC分类号: C07D207/14 , C07D401/06 , C07D403/06 , C07D405/06 , C07D471/10
摘要: The invention relates to pyrrolidine derivatives of formula wherein R1, R2, R3, n, and o are defined in the specification and to pharmaceutically active acid-addition salts thereof. Compounds of formula I have a high affinity simultaneously to both the NK1 and the NK3 receptors (dual NK1/NK3 receptor antagonists), useful in the treatment of schizophrenia.
摘要翻译: 本发明涉及下式的吡咯烷衍生物其中R1,R2,R3,n和o在本说明书中定义及其药学活性的酸加成盐。 式I化合物与NK1和NK3受体(双重NK1 / NK3受体拮抗剂)同时具有高亲和力,可用于治疗精神分裂症。
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公开(公告)号:US08318759B2
公开(公告)日:2012-11-27
申请号:US12703804
申请日:2010-02-11
申请人: Henner Knust , Anja Limberg , Matthias Nettekoven , Hasane Ratni , Claus Riemer
发明人: Henner Knust , Anja Limberg , Matthias Nettekoven , Hasane Ratni , Claus Riemer
IPC分类号: A61K31/496 , C07D241/04 , C07D401/14
CPC分类号: C07D207/08 , C07D207/09 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14
摘要: The present invention relates to a compounds of formula I wherein A, Ar, R, R2, R3, R4, p, and o are as defined in the specification and claims 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, bipolar disorders, anxiety and attention deficit hyperactivity disorder (ADHD).
摘要翻译: 本发明涉及式I化合物,其中A,Ar,R,R 2,R 3,R 4,p和o如说明书和权利要求中所定义,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,双相情感障碍,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:US20100256126A1
公开(公告)日:2010-10-07
申请号:US12721587
申请日:2010-03-11
申请人: Henner Knust , Anja Limberg , Matthias Nettekoven , Hasane Ratni , Claus Riemer , Walter Vifian
发明人: Henner Knust , Anja Limberg , Matthias Nettekoven , Hasane Ratni , Claus Riemer , Walter Vifian
IPC分类号: A61K31/451 , C07D417/10 , C07D211/62 , C07D401/10 , C07D413/10 , C07D413/14 , C07D417/14 , A61K31/541 , A61K31/4545 , A61K31/5377 , A61K31/506 , A61K31/497 , A61K31/454
CPC分类号: C07D401/10 , A61K31/4409 , A61K31/4465 , C07D211/32 , C07D401/14 , C07D409/14 , C07D413/10 , C07D417/10 , C07D417/14
摘要: The present application relates to compounds of formula wherein the definitions are as described herein. The present compounds are high potential NK-3 receptor antagonists that are useful 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,其中定义如本文所述。 本发明化合物是可用于治疗抑郁症,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:US08324250B2
公开(公告)日:2012-12-04
申请号:US12721587
申请日:2010-03-11
申请人: Henner Knust , Anja Limberg , Matthias Nettekoven , Hasane Ratni , Claus Riemer , Walter Vifian
发明人: Henner Knust , Anja Limberg , Matthias Nettekoven , Hasane Ratni , Claus Riemer , Walter Vifian
IPC分类号: A61K31/445 , C07D413/02
CPC分类号: C07D401/10 , A61K31/4409 , A61K31/4465 , C07D211/32 , C07D401/14 , C07D409/14 , C07D413/10 , C07D417/10 , C07D417/14
摘要: The present application relates to compounds of formula wherein the definitions are as described herein. The present compounds are high potential NK-3 receptor antagonists that are useful 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,其中定义如本文所述。 本发明化合物是可用于治疗抑郁症,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:US08318749B2
公开(公告)日:2012-11-27
申请号:US12614474
申请日:2009-11-09
申请人: Henner Knust , Anja Limberg , Matthias Nettekoven , Hasane Ratni , Claus Riemer , Walter Vifian
发明人: Henner Knust , Anja Limberg , Matthias Nettekoven , Hasane Ratni , Claus Riemer , Walter Vifian
IPC分类号: A61K31/517 , C07D239/70 , C07D401/04
CPC分类号: C07D401/04 , C07D401/14 , C07D405/14 , C07D409/14
摘要: The present invention relates to a compounds of formula I wherein R1, R2, R3, R4, R5, and n are as defined herein and to a pharmaceutically active salt, a racemic mixture, an enantiomer, an optical isomer or a tautomeric form 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: 本发明涉及式Ⅰ化合物,其中R 1,R 2,R 3,R 4,R 5和n如本文所定义,并且涉及药物活性盐,外消旋混合物,对映异构体,旋光异构体或其互变异构形式。 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:US20100125078A1
公开(公告)日:2010-05-20
申请号:US12614474
申请日:2009-11-09
申请人: Henner Knust , Anja Limberg , Matthias Nettekoven , Hasane Ratni , Claus Riemer , Walter Vifian
发明人: Henner Knust , Anja Limberg , Matthias Nettekoven , Hasane Ratni , Claus Riemer , Walter Vifian
IPC分类号: A61K31/498 , C07D401/14 , C07D403/04 , A61K31/517 , A61P25/18
CPC分类号: C07D401/04 , C07D401/14 , C07D405/14 , C07D409/14
摘要: The present invention relates to a compounds of formula I wherein R1, R2, R3, R4, R5, and n are as defined herein and to a pharmaceutically active salt, a racemic mixture, an enantiomer, an optical isomer or a tautomeric form 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: 本发明涉及式Ⅰ化合物,其中R 1,R 2,R 3,R 4,R 5和n如本文所定义,并且涉及药物活性盐,外消旋混合物,对映异构体,旋光异构体或其互变异构形式。 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: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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