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公开(公告)号:US08183380B2
公开(公告)日:2012-05-22
申请号:US12393058
申请日:2009-02-26
申请人: Sabine Kolczewski , Claus Riemer , Olivier Roche , Lucinda Steward , Juergen Wichmann , Thomas Woltering
发明人: Sabine Kolczewski , Claus Riemer , Olivier Roche , Lucinda Steward , Juergen Wichmann , Thomas Woltering
IPC分类号: C07D215/38
CPC分类号: C07D401/12 , C07D401/14 , C07D405/14 , C07D451/14
摘要: The present invention is concerned with 2-aminoquinoline derivatives of formula I where R1, R2, R3, R4, R5, R6, A, and n are as defined in the specification and claims, their use 5-HT5A receptor antagonists, their manufacture, and pharmaceutical compositions containing them.
摘要翻译: 本发明涉及式I的2-氨基喹啉衍生物,其中R 1,R 2,R 3,R 4,R 5,R 6,A和n如说明书和权利要求书中所定义,它们的用途为5-HT5A受体拮抗剂, 和含有它们的药物组合物。
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公开(公告)号:US08133909B2
公开(公告)日:2012-03-13
申请号:US12481627
申请日:2009-06-10
IPC分类号: A61K31/44 , C07D213/02
CPC分类号: C07D213/40 , C07D213/56 , C07D213/75 , C07D215/38 , C07D231/40 , C07D261/08 , C07D277/46 , C07D333/20 , C07D401/12 , C07D405/12 , C07D409/12 , C07D413/12
摘要: The present invention is concerned with novel sulfonamides of formula wherein R1, R2, R3, R4, R5, Ar, Ar1, Ar2, n, o and p are as described in the description and claims. The compounds are orexin receptor antagonists that may be useful in the treatment of disorders, in which orexin pathways are involved.
摘要翻译: 本发明涉及下列新型磺酰胺,其中R1,R2,R3,R4,R5,Ar,Ar1,Ar2,n,o和p如说明书和权利要求中所述。 这些化合物是食欲素受体拮抗剂,其可用于治疗其中涉及食欲素途径的病症。
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公开(公告)号:US07923470B2
公开(公告)日:2011-04-12
申请号:US12506302
申请日:2009-07-21
IPC分类号: A61K31/39
CPC分类号: C07D413/12 , C07D403/12 , C07D413/14 , C07D417/12
摘要: The present invention is concerned with novel sulfonamides of formula I wherein R1, R2, Ar, Hetaryl, m and n are as described in the description and claims. The compounds are orexin receptor antagonists, useful in the treatment of disorders, in which orexin pathways are involved.
摘要翻译: 本发明涉及式I的新型磺酰胺,其中R 1,R 2,Ar,杂芳基,m和n如说明书和权利要求中所述。 这些化合物是食欲素受体拮抗剂,可用于治疗食欲素途径参与的疾病。
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公开(公告)号:US20110071154A1
公开(公告)日:2011-03-24
申请号:US12958440
申请日:2010-12-02
IPC分类号: A61K31/498 , C07D413/12 , A61K31/423 , C07D417/12 , A61K31/428 , C07D417/14 , C07D413/14 , C07D403/12 , A61P25/00 , A61P25/28 , A61P25/16 , A61P25/22 , A61P25/24 , A61P1/00
CPC分类号: C07D413/12 , C07D403/12 , C07D413/14 , C07D417/12
摘要: The present invention is concerned with novel sulfonamides of formula I wherein R1, R2, Ar, Hetaryl, m and n are as described in the description and claims. The compounds are orexin receptor antagonists, useful in the treatment of disorders, in which orexin pathways are involved.
摘要翻译: 本发明涉及式I的新型磺酰胺,其中R 1,R 2,Ar,杂芳基,m和n如说明书和权利要求中所述。 这些化合物是食欲素受体拮抗剂,可用于治疗食欲素途径参与的病症。
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公开(公告)号:US20090318467A1
公开(公告)日:2009-12-24
申请号:US12484552
申请日:2009-06-15
申请人: Jean-Michel Adam , Johannes Aebi , Alferd Binggeli , Luke Green , Guido Hartmann , Hans P. Maerki , Patrizio Mattei , Fabienne Ricklin , Olivier Roche
发明人: Jean-Michel Adam , Johannes Aebi , Alferd Binggeli , Luke Green , Guido Hartmann , Hans P. Maerki , Patrizio Mattei , Fabienne Ricklin , Olivier Roche
IPC分类号: A61K31/4545 , C07D401/14 , A61K31/506 , A61K31/497 , A61K31/496 , A61K31/437
CPC分类号: C07D401/06 , C07D401/14 , C07D471/04
摘要: The invention is concerned with novel heteroaryl carboxamide derivatives of formula (I), wherein m, X, Y, R1, R2, R3 and R4 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds are antagonists of CCR-2 receptor, CCR-5 receptor and/or CCR-3 receptor and can be used as medicaments.
摘要翻译: 本发明涉及式(I)的新型杂芳基羧酰胺衍生物,其中m,X,Y,R 1,R 2,R 3和R 4如说明书和权利要求书中所定义,以及其生理上可接受的盐。 这些化合物是CCR-2受体,CCR-5受体和/或CCR-3受体的拮抗剂,可用作药物。
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公开(公告)号:US20090227628A1
公开(公告)日:2009-09-10
申请号:US12394083
申请日:2009-02-27
申请人: Sabine Kolczewski , Claus Riemer , Olivier Roche , Lucinda Steward , Juergen Wichmann , Thomas Woltering
发明人: Sabine Kolczewski , Claus Riemer , Olivier Roche , Lucinda Steward , Juergen Wichmann , Thomas Woltering
IPC分类号: A61K31/4709 , C07D215/38 , A61K31/47 , A61P25/24 , A61P25/22 , A61P25/00
CPC分类号: C07D215/38 , C07D405/12
摘要: The present invention is concerned with 2-aminoquinoline derivatives of formula I wherein Z, R1, and Ar1 are as defined herein, pharmaceutical compositions containing them, methods for their manufacture. The compounds are 5-HT5A receptor antagonists and are useful in the prevention and/or treatment of depression, anxiety disorders, schizophrenia, panic disorders, agoraphobia, social phobia, obsessive compulsive disorders, post-traumatic stress disorders, pain, memory disorders, dementia, disorders of eating behaviors, sexual dysfunction, sleep disorders, abuse of drugs, motor disorders such as Parkinson's disease, psychiatric disorders or gastrointestinal disorders.
摘要翻译: 本发明涉及式I的2-氨基喹啉衍生物,其中Z,R 1和Ar 1如本文所定义,含有它们的药物组合物,其制备方法。 这些化合物是5-HT5A受体拮抗剂,可用于预防和/或治疗抑郁症,焦虑障碍,精神分裂症,恐慌症,广场恐怖症,社交恐惧症,强迫症,创伤后应激障碍,疼痛,记忆障碍,痴呆 饮食行为障碍,性功能障碍,睡眠障碍,药物滥用,运动障碍如帕金森病,精神病或胃肠疾病。
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公开(公告)号:US20090203736A1
公开(公告)日:2009-08-13
申请号:US12365911
申请日:2009-02-05
IPC分类号: A61K31/454 , C07D401/06 , A61P25/00 , A61K31/4545
CPC分类号: C07D401/06 , C07D211/96
摘要: The present invention relates to piperidine sulphonamide derivatives of formula wherein Ar1, Ar2, R1, R2, m and n are as defined in the description and claims, or pharmaceutically suitable acid addition salts thereof. The compounds of formula I are orexin receptor antagonists and the related compounds can be useful in the treatment of sleep apnea, narcolepsy, insomnia, parasomnia, jet lag syndrome, circadian rhythms disorder or sleep disorders associated with neurological diseases.
摘要翻译: 本发明涉及下式的哌啶磺酰胺衍生物其中Ar 1,Ar 2,R 1,R 2,m和n如说明书和权利要求中所定义,或其药学上合适的酸加成盐。 式I化合物是食欲蛋白受体拮抗剂,相关化合物可用于治疗睡眠呼吸暂停,发作性睡病,失眠,睡眠,夜间综合征,昼夜节律障碍或与神经疾病相关的睡眠障碍。
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公开(公告)号:US20090029963A1
公开(公告)日:2009-01-29
申请号:US12173847
申请日:2008-07-16
申请人: Johannes Aebi , Alfred Binggeli , Luke Green , Guido Hartmann , Hans P. Maerki , Patrizio Mattei , Fabienne Ricklin , Olivier Roche
发明人: Johannes Aebi , Alfred Binggeli , Luke Green , Guido Hartmann , Hans P. Maerki , Patrizio Mattei , Fabienne Ricklin , Olivier Roche
IPC分类号: A61K31/454 , A61K31/551 , C07D403/06 , C07D401/04 , C07D401/14 , A61K31/496 , C07D413/14 , A61K31/5377
CPC分类号: C07D231/14 , C07D401/04 , C07D403/06
摘要: The invention is concerned with novel pyrazol derivatives of formula (I), wherein R1, R2, R3, R4, X and Y are as defined herein, as well as physiologically acceptable salts thereof. These compounds are antagonists of CCR-2 receptor and/or CCR-5 receptor and can be used as medicaments.
摘要翻译: 本发明涉及式(I)的新型吡唑衍生物,其中R 1,R 2,R 3,R 4,X和Y如本文所定义,以及其生理上可接受的盐。 这些化合物是CCR-2受体和/或CCR-5受体的拮抗剂,可用作药物。
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公开(公告)号:US07351708B2
公开(公告)日:2008-04-01
申请号:US11634563
申请日:2006-12-06
申请人: Matthias Nettekoven , Olivier Roche
发明人: Matthias Nettekoven , Olivier Roche
IPC分类号: A61K31/5377 , A61K31/496 , A61K31/55 , C07D487/04
CPC分类号: C07D471/04
摘要: The present invention relates to compounds of formula I wherein R1 to R4 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.
摘要翻译: 本发明涉及式I化合物,其中R 1至R 4如在说明书和权利要求书中所定义,及其药学上可接受的盐。 该化合物可用于治疗和/或预防与H3受体的调节相关的疾病。
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公开(公告)号:US20060122187A1
公开(公告)日:2006-06-08
申请号:US11290675
申请日:2005-11-30
IPC分类号: A61K31/496 , C07D403/04
CPC分类号: C07D213/74 , C07D213/82 , C07D213/83
摘要: The present invention relates to compounds of formula I wherein R1, R2 and A are as defined in the description and claims, and pharmaceutically acceptable salts thereof as well as to pharmaceutical composition comprising these compounds and to methods for their preparation. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.
摘要翻译: 本发明涉及其中R 1,R 2和A如说明书和权利要求书中所定义的式I化合物及其药学上可接受的盐以及药物 包含这些化合物的组合物及其制备方法。 该化合物可用于治疗和/或预防与H3受体的调节相关的疾病。
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