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公开(公告)号：US07935707B2
公开(公告)日：2011-05-03
申请号：US12215104
申请日：2008-06-25
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： A61K31/4025 , A61K31/4178 , A61K31/497 , A61K31/4468 , C07D239/42 , C07D401/14 , C07D211/58
CPC分类号： C07D401/14 , C07D401/06 , C07D403/06 , C07D405/14
摘要： The invention is concerned with novel imidazole derivatives of formula (I), wherein m, E, R1, R2, R3, R4, R5, R6 and R7 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）的新咪唑衍生物，其中m，E，R 1，R 2，R 3，R 4，R 5，R 6和R 7如在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：US07829563B2
公开(公告)日：2010-11-09
申请号：US12037975
申请日：2008-02-27
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： A61K31/50 , A61K31/501 , A61K31/497 , A01N43/54 , C07D239/42 , C07D401/04 , A01N43/40 , A61K31/435 , A01N43/78 , A61K31/425 , A01N43/50 , A61K31/415 , A01N43/56 , A01N43/08 , A61K31/34 , C07D279/00 , C07D285/00 , C07D401/00 , C07D421/00 , C07D419/00 , C07D277/04 , C07D277/08 , C07D409/00 , C07D335/00 , C07D333/02 , C07D321/00 , C07D307/00 , C07D317/00 , C07D323/02
CPC分类号： C07D213/36 , A61K9/2018 , A61K9/4858 , C07C237/20 , C07C2601/02 , C07C2601/04
摘要： The present invention relates to compounds of formula I wherein Ar1, Ar2, Ar3, n, and R1 to R8 are as defined herein and to pharmaceutically suitable acid addition salts, optically pure enantiomers, racemates or diastereomeric mixtures thereof. These compounds 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，Ar3，n和R1至R8如本文所定义，以及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。 这些化合物是食欲肽受体拮抗剂，并且可用于治疗涉及食欲素途径的疾病，例如睡眠障碍。
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公开(公告)号：US20100029664A1
公开(公告)日：2010-02-04
申请号：US12506302
申请日：2009-07-21
IPC分类号： A61K31/498 , C07D413/12 , A61K31/423 , C07D417/12 , A61K31/428 , C07D413/14 , C07D417/14 , C07D403/12
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：US20100022518A1
公开(公告)日：2010-01-28
申请号：US12507858
申请日：2009-07-23
申请人： Jean-Michel Adam , Johannes Aebi , Alfred Binggeli , Luke Green , Guido Hartmann , Hans P. Maerki , Patrizio Mattei , Fabienne Ricklin , Olivier Roche
发明人： Jean-Michel Adam , Johannes Aebi , Alfred Binggeli , Luke Green , Guido Hartmann , Hans P. Maerki , Patrizio Mattei , Fabienne Ricklin , Olivier Roche
IPC分类号： A61K31/5513 , A61K31/5377 , A61K31/497 , C07D243/08 , C07D413/06 , C07D401/06 , C07D401/14
CPC分类号： C07D401/06 , C07D241/08 , C07D243/08 , C07D401/14 , C07D413/06
摘要： The invention is concerned with novel heterocyclyl compounds of formula (I): wherein A, X, R3, R4, R5, R6, R7, R8, R9, R10, m, n and p are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds are antagonists of CCR2 receptor, CCR5 receptor and/or CCR3 receptor and may be used as medicaments.
摘要翻译： 本发明涉及式（I）的新型杂环基化合物：其中A，X，R3，R4，R5，R6，R7，R8，R9，R10，m，n和p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CCR2受体，CCR5受体和/或CCR3受体的拮抗剂，可用作药物。
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公开(公告)号：US07632829B2
公开(公告)日：2009-12-15
申请号：US11788252
申请日：2007-04-19
申请人： Johannes Aebi , Luke Green , Patrizio Mattei , Fabienne Ricklin , Olivier Roche , Peter Zahm
发明人： Johannes Aebi , Luke Green , Patrizio Mattei , Fabienne Ricklin , Olivier Roche , Peter Zahm
IPC分类号： C07D243/14 , C07D405/12 , C07D401/06 , C07D401/14 , C07D413/12 , A61K31/551
CPC分类号： C07D405/06 , C07D243/14 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/12 , C07D405/12 , C07D413/12 , C07D471/10
摘要： The invention is concerned with novel diazepan derivatives of formula (I) wherein A, X, R3, R4, R5, R6, R8, R9, R10, R11, R12, R13, m and n 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）的新的二氮杂衍生物，其中A，X，R 3，R 4，R 5，R 6，R 8，R 9，R 10，R 11，R 12，R 13，m和n如说明书和 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：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：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：US20090048238A1
公开(公告)日：2009-02-19
申请号：US12239055
申请日：2008-09-26
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 , C07D401/04 , C07D243/14 , A61K31/506 , A61P9/00 , A61P25/00 , A61K31/551 , C07D401/14
CPC分类号： C07D211/58 , C07D295/192 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/14 , C07D403/06
摘要： The invention is concerned with novel biaryl derivatives of formula (I), wherein m, R1, R2, R3, X1, X2 and X3 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）的新型联芳衍生物，其中m，R 1，R 2，R 3，X 1，X 2和X 3如在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：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：US20080103174A1
公开(公告)日：2008-05-01
申请号：US11876007
申请日：2007-10-22
IPC分类号： A61K31/47 , A61K31/454 , C07D215/14 , C07D401/02
CPC分类号： C07D401/12 , C07D211/46 , C07D401/14 , C07D405/12 , C07D409/12 , C07D413/12
摘要： The present invention relates to ether derivatives according to general formula I, and to their pharmaceutically-acceptable salts, which may be used in treating or preventing cognitive disorders, drug addiction, depression, anxiety, drug dependence, dementias, memory impairment, psychotic disorders comprising schizophrenia, schizoaffective disorders, bipolar disease, mania, psychotic depression, or psychoses comprising paranoia and delusions.
摘要翻译： 本发明涉及根据通式I的醚衍生物及其药学上可接受的盐，其可用于治疗或预防认知障碍，药物成瘾，抑郁，焦虑，药物依赖，痴呆，记忆障碍，精神病，包括 精神分裂症，分裂情感障碍，双相性精神障碍，躁狂症，精神病性抑郁症或精神病，包括偏执狂和妄想。
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