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公开(公告)号:US20090163485A1
公开(公告)日:2009-06-25
申请号:US12334559
申请日:2008-12-15
IPC分类号: A61K31/5365 , C07D263/54 , A61K31/421 , C07D241/36 , A61K31/498 , C07D417/02 , A61K31/428 , C07D221/00 , A61K31/4245 , A61P25/00 , A61K31/501 , C07D403/02 , A61K31/505 , C07D239/24 , C07D271/06 , A61K31/454 , C07D215/38 , A61K31/4709 , C07D239/72 , A61K31/517 , C07D265/12
CPC分类号: C07D413/12 , C07D401/12 , C07D409/14 , C07D413/14 , C07D417/12 , C07D417/14 , C07D498/04
摘要: The present invention relates to compounds of formula wherein Ar, Het, R1 and n are as defined herein and to pharmaceutically suitable acid addition salts, optically pure enantiomers, racemates or diastereomeric mixtures thereof. Compounds of formula I are orexin receptor antagonists and are useful in the treatment of sleep apnea, narcolepsy, insomnia, parasomnia, jet lag syndrome, circadian rhythms disorder and sleep disorders associated with neurological diseases.
摘要翻译: 本发明涉及下式的化合物其中Ar,Het,R 1和n如本文所定义,并且与药学上合适的酸加成盐,光学纯对映异构体,外消旋物或非对映体混合物相关。 式I化合物是食欲蛋白受体拮抗剂,可用于治疗睡眠呼吸暂停,发作性睡病,失眠,睡眠不正,夜间综合征,昼夜节律障碍和与神经疾病相关的睡眠障碍。
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公开(公告)号:US07528136B2
公开(公告)日:2009-05-05
申请号:US12129718
申请日:2008-05-30
申请人: Bo Han , Henner Knust , Matthias Nettekoven , Hasane Ratni , Xihan Wu
发明人: Bo Han , Henner Knust , Matthias Nettekoven , Hasane Ratni , Xihan Wu
IPC分类号: A61K31/496 , A61K31/4725 , A61K31/401 , C07D401/06 , C07D207/16 , C07D487/10
CPC分类号: C07D207/16 , C07D401/06 , C07D471/10
摘要: The present invention relates to a compound of formula I wherein R1, R2, R3, R4, R5, X, n, and o are as defined herein and to a pharmaceutically acceptable acid addition salt thereof which 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: 本发明涉及其中R 1,R 2,R 3,R 4,R 5,X,n和o如本文所定义的式I化合物及其药学上可接受的酸加成盐,其为高度潜在的NK-3受体拮抗剂 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)的治疗。
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公开(公告)号:US20090076081A1
公开(公告)日:2009-03-19
申请号:US12207596
申请日:2008-09-10
申请人: Henner Knust , Matthias Nettekoven , Hasane Ratni , Walter Vifian , Xihan Wu
发明人: Henner Knust , Matthias Nettekoven , Hasane Ratni , Walter Vifian , Xihan Wu
IPC分类号: A61K31/445 , C07D211/22 , A61K31/4523 , A61P25/24 , A61P25/16 , C07D401/04
CPC分类号: C07D211/58 , C07D401/04
摘要: The invention relates to a compound of formula wherein Ar1, Ar2, R1, R2, R3, R4, R5, and R5′ or to a pharmaceutically active salt 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: 本发明涉及下式化合物其中Ar1,Ar2,R1,R2,R3,R4,R5和R5'或其药物活性盐。 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:US07501541B2
公开(公告)日:2009-03-10
申请号:US12044002
申请日:2008-03-07
申请人: Luca Gobbi , Henner Knust , Parichehr Malherbe , Matthias Nettekoven , Emmanuel Pinard , Olivier Roche , Mark Rogers-Evans
发明人: Luca Gobbi , Henner Knust , Parichehr Malherbe , Matthias Nettekoven , Emmanuel Pinard , Olivier Roche , Mark Rogers-Evans
IPC分类号: C07C233/05 , A61K31/65
CPC分类号: C07C233/29 , C07C233/15 , C07C233/32 , C07C233/88 , C07C2601/02 , C07C2601/08 , C07D211/16 , C07D211/46 , C07D213/40 , C07D213/75 , C07D295/185 , C07D309/14
摘要: The present invention relates to compounds of formula I wherein Ar1, Ar2, R, R1, R2, R3 and n are as defined herein or to pharmaceutically suitable acid addition salts, optically pure enantiomers, racemates or diastereomeric mixtures thereof. Compounds of formula I are orexin receptor antagonists and may be useful in the treatment of disorders, in which orexin pathways are involved like sleep disorders.
摘要翻译: 本发明涉及式I化合物,其中Ar1,Ar2,R,R1,R2,R3和n如本文所定义,或其药学上合适的酸加成盐,光学纯对映异构体,外消旋物或非对映体混合物。 式I化合物是食欲素受体拮抗剂,可用于治疗其中食欲素途径如睡眠障碍的疾病。
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公开(公告)号:US20090042896A1
公开(公告)日:2009-02-12
申请号:US12185157
申请日:2008-08-04
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: A61K31/501 , C07D207/04 , A61K31/40 , C07D401/02 , A61K31/4439 , C07D239/24 , A61K31/506 , C07D213/02 , A61P25/18 , A61K31/497 , A61K31/444 , C07D417/02 , A61K31/4436 , C07D413/02 , A61K31/443 , C07D403/14
CPC分类号: C07D401/06 , C07D401/08
摘要: The invention relates to a compound of formula I wherein Ar1, Ar2, R1, R2, R3, R4, n, o, p, and q are as defined herein and 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: 本发明涉及式Ⅰ化合物,其中Ar 1,Ar 2,R 1,R 2,R 3,R 4,n,o,p和q如本文所定义,及其药物活性盐,包括所有立体异构形式,个别非对映异构体和 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:US20090036422A1
公开(公告)日:2009-02-05
申请号:US12178688
申请日:2008-07-24
IPC分类号: A61K31/397 , A61K31/165 , A61K31/52 , A61K31/437 , C07C233/88 , C07D471/04 , C07D487/04 , C07D491/107
CPC分类号: C07D405/12 , C07C233/29 , C07C235/38 , C07C235/80 , C07C237/20 , C07C237/22 , C07C251/48 , C07C255/58 , C07C255/60 , C07C271/22 , C07D205/04 , C07D207/12 , C07D209/44 , C07D211/46 , C07D213/56 , C07D231/56 , C07D235/06 , C07D235/08 , C07D235/10 , C07D235/16 , C07D235/26 , C07D277/62 , C07D305/02 , C07D305/08 , C07D307/14 , C07D307/52 , C07D307/79 , C07D317/28 , C07D317/46 , C07D317/66 , C07D319/20 , C07D333/24 , C07D471/04 , C07D487/04 , C07D491/107
摘要: The present invention relates to compounds of formula wherein Ar, R1, R2, R3, R4, R5, n, o, and p are as defined herein or to pharmaceutically suitable acid addition salts, optically pure enantiomers, racemates or diastereomeric mixtures thereof. The compounds of formula I can be used for the treatment of sleep disorders, such as sleep apnea, narcolepsy, insomnia, parasomnia, jet lag syndrome, circadian rhythms disorder or sleep disorders associated with neurological diseases.
摘要翻译: 本发明涉及下式的化合物其中Ar,R 1,R 2,R 3,R 4,R 5,n,o和p如本文所定义,或其药学上合适的酸加成盐,光学纯对映异构体,外消旋体或非对映体混合物。 式I化合物可用于治疗睡眠呼吸暂停,发作性睡病,失眠,睡眠不正常,时差综合征,昼夜节律障碍或与神经疾病相关的睡眠障碍的睡眠障碍。
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公开(公告)号:US20080306086A1
公开(公告)日:2008-12-11
申请号:US12129718
申请日:2008-05-30
申请人: Bo Han , Henner Knust , Matthias Nettekoven , Hasane Ratni , Xihan Wu
发明人: Bo Han , Henner Knust , Matthias Nettekoven , Hasane Ratni , Xihan Wu
IPC分类号: A61K31/496 , C07D403/02 , C07D217/00 , A61K31/4709 , C07D211/00 , A61K31/454 , A61K31/438 , A61P25/00
CPC分类号: C07D207/16 , C07D401/06 , C07D471/10
摘要: The present invention relates to a compound of formula I wherein R2 R3, R4, R5, X, n, and o are as defined herein and to a pharmaceutically acceptable acid addition salt thereof which 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: 本发明涉及其中R2 R3,R4,R5,X,n和o如本文所定义的式I化合物及其药学上可接受的酸加成盐,其为高度潜在的NK-3受体拮抗剂,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)。
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68.
公开(公告)号:US20080275021A1
公开(公告)日:2008-11-06
申请号:US12102121
申请日:2008-04-14
申请人: Caterina Bissantz , Torsten Hoffmann , Philippe Jablonski , Henner Knust , Mathias Nettekoven , Hasane Ratni , Xihan Wu
发明人: Caterina Bissantz , Torsten Hoffmann , Philippe Jablonski , Henner Knust , Mathias Nettekoven , Hasane Ratni , Xihan Wu
IPC分类号: A61K31/5377 , C07D413/06 , C07D417/06 , A61K31/541 , A61K31/40 , A61P25/18 , A61K31/397 , A61K31/496 , C07D403/06 , C07D207/14
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R 1,R 2,R 3,n和o在本说明书中定义为 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: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: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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