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公开(公告)号：US08202888B2
公开(公告)日：2012-06-19
申请号：US12365911
申请日：2009-02-05
IPC分类号： A61K31/454 , C07D401/06
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：US20120035195A1
公开(公告)日：2012-02-09
申请号：US13196933
申请日：2011-08-03
申请人： David Banner , Emanuele Gabellieri , Wolfgang Guba , Hans Hilpert , Benoit Hornsperger , Roland Humm , Harald Mauser , Alexander V. Mayweg , Robert Narquizian , Emmanuel Pinard , Mark Rogers-Evans , Thomas Woltering , Wolfgang Wostl
发明人： David Banner , Emanuele Gabellieri , Wolfgang Guba , Hans Hilpert , Benoit Hornsperger , Roland Humm , Harald Mauser , Alexander V. Mayweg , Robert Narquizian , Emmanuel Pinard , Mark Rogers-Evans , Thomas Woltering , Wolfgang Wostl
IPC分类号： A61K31/513 , A61P3/10 , C07D239/47
CPC分类号： C07D417/12 , A61K31/513 , C07D239/22 , C07D239/70 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12
摘要： This invention relates to compounds of the formula wherein R1 to R9 are as described below, or to pharmaceutically acceptable salts thereof. These compounds are BACE2 inhibitors and can be used as medicaments for the therapeutic and/or prophylactic treatment of diseases such as diabetes, particularly type 2 diabetes, and other metabolic disorders.
摘要翻译： 本发明涉及下式化合物或其药学上可接受的盐：其中R 1至R 9如下所述。 这些化合物是BACE2抑制剂，可用作治疗和/或预防性治疗诸如糖尿病，特别是2型糖尿病和其它代谢疾病的药物。
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公开(公告)号：US07951836B2
公开(公告)日：2011-05-31
申请号：US11818676
申请日：2007-06-15
IPC分类号： A61K31/5355 , C07D413/08
CPC分类号： C07D207/06 , C07D207/08 , C07D211/16 , C07D403/10 , C07D407/10
摘要： The present invention relates to compounds of formula I wherein R1, R2, R3, X, n, and m are as defined herein and to pharmaceutically acceptable acid addition salts thereof, to pharmaceutical compositions containing them, and to methods for treating neurological and neuropsychiatric disorders.
摘要翻译： 本发明涉及式I化合物，其中R 1，R 2，R 3，X，n和m如本文所定义，及其药学上可接受的酸加成盐，含有它们的药物组合物，以及治疗神经和神经精神障碍 。
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![SOLID FORMS OF [4-(3-FLUORO-5-TRIFLUOROMETHYL-PYRIDIN-2-YL)-PIPERAZIN-1-YL-[5-METHANESULFONYL-2-((S)-2,2,2-TRIFLUORO-1-METHYL-ETHOXY)-PHENYL]-METHANONE](/abs-image/US/2010/12/09/US20100311971A1/abs.jpg.150x150.jpg)
54.发明申请SOLID FORMS OF [4-(3-FLUORO-5-TRIFLUOROMETHYL-PYRIDIN-2-YL)-PIPERAZIN-1-YL-[5-METHANESULFONYL-2-((S)-2,2,2-TRIFLUORO-1-METHYL-ETHOXY)-PHENYL]-METHANONE 有权[4-（3-氟-5-三氟甲基 - 吡啶-2-基） - 哌嗪-1-基] - [5-甲磺酰基-2 - （（S）-2,2,2-三氟-1- 甲基 - 乙氧基） - 苯基] - 甲基公开(公告)号：US20100311971A1
公开(公告)日：2010-12-09
申请号：US12841195
申请日：2010-07-22
申请人： Andre Bubendorf , Annette Deynet-Vucenovic , Ralph Diodone , Olaf Grassmann , Kai Lindenstruth , Emmanuel Pinard , Franziska E. Rohrer , Urs Schwitter
发明人： Andre Bubendorf , Annette Deynet-Vucenovic , Ralph Diodone , Olaf Grassmann , Kai Lindenstruth , Emmanuel Pinard , Franziska E. Rohrer , Urs Schwitter
IPC分类号： C07D401/04
CPC分类号： C07D213/74
摘要： The present invention relates to four distinct crystalline forms and to an amorphous form of [4-(3-Fluoro-5-trifluoromethyl-pyridin-2-yl)-piperazin-1-yl]-[5-methanesulfonyl-2-((S)-2,2,2-trifluoro-1-methyl-ethoxy)-phenyl]-methanone, and to their use in the preparation of pharmaceutical compositions. The compounds of present invention are suitable for the treatment of psychoses, pain, neurodegenerative disfunction in memory and learning, schizophrenia, dementia and other diseases in which cognitive processes are impaired, such as attention deficit disorders or Alzheimer's disease.
摘要翻译： 本发明涉及四种不同的结晶形式和无定形形式的[4-（3-氟-5-三氟甲基 - 吡啶-2-基） - 哌嗪-1-基] - [5-甲磺酰基-2 - （（ S）-2,2,2-三氟-1-甲基 - 乙氧基） - 苯基] - 甲酮，以及它们在制备药物组合物中的用途。 本发明的化合物适合于治疗精神病，疼痛，记忆和学习中的神经变性功能障碍，精神分裂症，痴呆等认知过程受损的其他疾病，如注意力缺陷障碍或阿尔茨海默病。
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公开(公告)号：US20100111862A1
公开(公告)日：2010-05-06
申请号：US12607111
申请日：2009-10-28
IPC分类号： A61K51/04 , C07D209/02 , A61P25/18
CPC分类号： C07D405/10
摘要： The present invention relates to novel radiolabelled inhibitors of formula I for the Glycine 1 transporter (GlyT1), useful for the labelling and diagnostic imaging of the glycine 1 transporter functionality. whereinR1 is isopropoxy or 2,2,2-trifluoro-1-methyl-ethoxy; andR2 is a radiolabelled group CH3, wherein the radionuclide is 3H or 11C. The radiolabelled compounds of formula I may be used as PET (Positron Emission Tomography) radiotracer for the labelling and diagnostic molecular imaging of the glycine 1 transporter functionality.
摘要翻译： 本发明涉及用于甘氨酸1转运蛋白（GlyT1）的式I的新型放射性标记抑制剂，其可用于甘氨酸1转运蛋白官能度的标记和诊断成像。 其中R1是异丙氧基或2,2,2-三氟-1-甲基 - 乙氧基; 并且R 2是放射性标记的基团CH 3，其中放射性核素是3H或11C。 放射性标记的式I化合物可用作PET（正电子发射断层扫描）放射性示踪剂，用于甘氨酸1转运蛋白功能的标记和诊断分子成像。
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公开(公告)号：US20090312314A1
公开(公告)日：2009-12-17
申请号：US12481627
申请日：2009-06-10
IPC分类号： A61K31/536 , C07D213/56 , A61K31/44 , C07D401/02 , A61K31/4439 , A61K31/444 , C07D277/20 , A61K31/426 , C07D215/38 , A61K31/47 , C07D265/36 , A61P25/00
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：US07605163B2
公开(公告)日：2009-10-20
申请号：US11931379
申请日：2007-10-31
申请人： Synese Jolidon , Robert Narquizian , Matthias Heinrich Nettekoven , Roger David Norcross , Emmanuel Pinard , Henri Stalder
发明人： Synese Jolidon , Robert Narquizian , Matthias Heinrich Nettekoven , Roger David Norcross , Emmanuel Pinard , Henri Stalder
IPC分类号： A61K31/495 , C07D295/192
CPC分类号： C07D239/42 , C07D213/85 , C07D241/20 , C07D251/42 , C07D257/04 , C07D263/32 , C07D271/06 , C07D295/192 , C07D309/12
摘要： The invention relates to compounds of formula wherein the substituents are described herein. The compounds may be used in the treatment of illnesses based on the glycine uptake inhibitor, such as psychoses, pain, neurodegenerative disfunction in memory and learning, schizophrenia, dementia and other diseases in which cognitive processes are impaired, such as attention deficit disorders or Alzheimer's disease.
摘要翻译： 本发明涉及下式的化合物，其中取代基在本文中描述。 该化合物可用于基于甘氨酸摄取抑制剂治疗疾病，例如精神病，疼痛，记忆和学习中的神经变性功能障碍，精神分裂症，痴呆等认知过程受损的其他疾病，如注意力缺陷障碍或阿尔茨海默氏症 疾病。
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公开(公告)号：US07442710B2
公开(公告)日：2008-10-28
申请号：US11338266
申请日：2006-01-24
IPC分类号： A61K31/4725 , A61K31/4741 , A61K31/4745 , A61K31/44 , A61K31/497 , C07D217/16 , C07D217/24 , C07D279/12 , C07D295/00 , C07D413/12 , C07D413/14 , C07D471/04 , C07D471/14 , C07D487/04 , C07D487/14 , C07D491/147 , C07D401/04 , A61P25/18 , A61K31/472 , A61K31/519 , A61K31/4453 , C07D215/14 , C07D471/22 , C07D487/22 , C07D491/048 , C07D491/052 , C07D491/056 , C07D491/153 , C07D491/22
CPC分类号： C07D471/04 , C07D215/14 , C07D217/06 , C07D491/04
摘要： The present invention relates to compounds of general formula IA or IB wherein X1 and X2 are each independently N or C—R″ and R1, R2,R3, R4, R5, and R6 are as defined in the specification and to pharmaceutically acceptable acid addition salts thereof. The compounds can be used for the treatment of diseases related to the glycine transporter inhibitor, such as schizophrenia and Alzheimer's disease.
摘要翻译： 本发明涉及通式IA或IB的化合物，其中X 1和X 2各自独立地为N或C-R“和R 1' R 2，R 2，R 3，R 4，R 5和R 6， / SUP>如说明书中所定义及其药学上可接受的酸加成盐。 该化合物可用于治疗与甘氨酸转运蛋白抑制剂相关的疾病，如精神分裂症和阿尔茨海默病。
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公开(公告)号：US20080249125A1
公开(公告)日：2008-10-09
申请号：US12056324
申请日：2008-03-27
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： A61K31/437 , C07D471/02 , C07D513/02 , A61K31/4365 , A61K31/4375 , A61P25/00
CPC分类号： C07D471/04 , C07D495/04
摘要： The present invention relates to compounds of formula wherein R1, R2, R3, and R4 are as defined herein and hetaryl is a one or two ring-membered heteroaromatic ring system, connected to the carbon atoms of the piperidine group selected from the group consisting of or 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： 本发明涉及下式的化合物其中R 1，R 2，R 3和R 4是 如本文所定义，杂芳基是与哌啶基的碳原子连接的一个或两个环 - 元杂芳族环系统，所述哌啶基团选自由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组成的组。 这些化合物是食欲素受体拮抗剂，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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![SOLID FORMS OF [4-(3-FLUORO-5-TRIFLUOROMETHYL-PYRIDIN-2-YL)-PIPERAZIN-1-YL-[5-METHANESULFONYL-2-((S)-2,2,2-TRIFLUORO-1-METHYL-ETHOXY)-PHENYL]-METHANONE](/abs-image/US/2008/09/04/US20080214561A1/abs.jpg.150x150.jpg)
60.发明申请SOLID FORMS OF [4-(3-FLUORO-5-TRIFLUOROMETHYL-PYRIDIN-2-YL)-PIPERAZIN-1-YL-[5-METHANESULFONYL-2-((S)-2,2,2-TRIFLUORO-1-METHYL-ETHOXY)-PHENYL]-METHANONE 审中-公开[4-（3-氟-5-三氟甲基 - 吡啶-2-基） - 哌嗪-1-基] - [5-甲磺酰基-2 - （（S）-2,2,2-三氟-1- 甲基 - 乙氧基） - 苯基] - 甲基公开(公告)号：US20080214561A1
公开(公告)日：2008-09-04
申请号：US12002997
申请日：2007-12-19
申请人： Andre Bubendorf , Annette Deynet-Vucenovic , Ralph Diodone , Olaf Grassmann , Kai Lindenstruth , Emmanuel Pinard , Franziska E. Rohrer , Urs Schwitter
发明人： Andre Bubendorf , Annette Deynet-Vucenovic , Ralph Diodone , Olaf Grassmann , Kai Lindenstruth , Emmanuel Pinard , Franziska E. Rohrer , Urs Schwitter
IPC分类号： A61K31/496 , C07D401/04
CPC分类号： C07D213/74
摘要： The present invention relates to four distinct crystalline forms and to an amorphous form of [4-(3-Fluoro-5-trifluoromethyl-pyridin-2-yl)-piperazin-1-yl]-[5-methanesulfonyl-2-((S)-2,2,2-trifluoro-1-methyl-ethoxy)-phenyl]-methanone, and to their use in the preparation of pharmaceutical compositions. The compounds of present invention are suitable for the treatment of psychoses, pain, neurodegenerative disfunction in memory and learning, schizophrenia, dementia and other diseases in which cognitive processes are impaired, such as attention deficit disorders or Alzheimer's disease.
摘要翻译： 本发明涉及四种不同的结晶形式和无定形形式的[4-（3-氟-5-三氟甲基 - 吡啶-2-基） - 哌嗪-1-基] - [5-甲磺酰基-2 - （（ S）-2,2,2-三氟-1-甲基 - 乙氧基） - 苯基] - 甲酮，以及它们在制备药物组合物中的用途。 本发明的化合物适合于治疗精神病，疼痛，记忆和学习中的神经变性功能障碍，精神分裂症，痴呆等认知过程受损的其他疾病，如注意力缺陷障碍或阿尔茨海默病。
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