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11. 发明授权

US06359138B1 4-hydroxy-piperidine derivatives 失效
标题翻译： 4-羟基 - 哌啶衍生物
公开(公告)号：US06359138B1
公开(公告)日：2002-03-19
申请号：US08976540
申请日：1997-11-24
申请人： Alexander Alanine , Bernd Büttelmann , Marie-Paule Heitz Neidhart , Emmanuel Pinard , René Wyler
发明人： Alexander Alanine , Bernd Büttelmann , Marie-Paule Heitz Neidhart , Emmanuel Pinard , René Wyler
IPC分类号： C07D40106
CPC分类号： C07D401/06 , C07D211/48 , C07D405/06
摘要： The present invention relates to 4-hydroxy-piperidine derivatives of the general formula wherein X denotes —O—, —NH—, —CH2—, —CH═, —CHOH—, —CO—, —S—, —SO— or —SO2—; R1-R4 are, independently from each other, hydrogen, hydroxy, lower-alkyl-sulfonylamino, 1- or 2-imidazolyl or acetamido; R5-R8 are, independently from each other, hydrogen, hydroxy, lower-alkyl, halogen, lower-alkoxy, trifluoromethyl or trifluoromethyloxy; a and b may be a double bond, provided that when “a” is a double bond, “b” cannot be a double bond; n is 0-2; m is 1-3; p is 0 or 1 and to pharmaceutically acceptable addition salts thereof. Compounds of the present invention are NMDA(N-methyl-D-aspartate)-receptor subtype selective blockers, which can be used in mediating processes underlying development of CNS including learning and memory formation and function.
摘要翻译：本发明涉及通式为Ⅳ的4-羟基 - 哌啶衍生物，其中X表示-O - ， - NH - ， - CH 2 - ， - CH =， - CHOH-， - CO - ， - S - ， - SO-或-SO 2 - ; R 1 -R 4彼此独立地为氢，羟基，低级 - 烷基 - 磺酰基氨基，1-或2-咪唑基或乙酰氨基; R5-R8彼此独立地为氢，羟基，低级 - 烷基，卤素低级烷氧基，三氟甲基或三氟甲氧基; a和b可以是双键，条件是当“a”是双键时，“b”不能是双键; n是0-2; m是1-3; p是0或1，以及其药学上可接受的加成盐。本发明的化合物是NMDA（N-甲基-D-天冬氨酸） - 受体亚型选择性阻断剂，其可用于介导中枢神经系统发育的过程，包括学习和记忆形成和功能。

12. 发明授权

US06265426B1 Triazole derivatives 失效
标题翻译：三唑衍生物
公开(公告)号：US06265426B1
公开(公告)日：2001-07-24
申请号：US09619518
申请日：2000-07-19
申请人： Alexander Alanine , Bernd Büttelmann , Marie-Paule Heitz Neidhart , Georg Jaeschke , Emmanuel Pinard , René Wyler
发明人： Alexander Alanine , Bernd Büttelmann , Marie-Paule Heitz Neidhart , Georg Jaeschke , Emmanuel Pinard , René Wyler
IPC分类号： C07D24914
CPC分类号： C07D233/64 , C07D249/08 , C07D401/06 , C07D403/10 , C07D405/10
摘要： The present invention relates to triazole and imidazole derivatives of formula I and to their pharmaceutically acceptable acid addition salts. These compounds are NMDA receptor subtype blockers and are useful for the treatment of diseases related to the NMDA receptor.
摘要翻译：本发明涉及式I的三唑和咪唑衍生物及其药学上可接受的酸加成盐。这些化合物是NMDA受体亚型阻断剂，可用于治疗与NMDA受体有关的疾病。

13. 发明申请

US20130072478A1 N-(3-(2-AMINO-6,6-DIFLUORO-4,4A,5,6,7,7A-HEXAHYDRO-CYCLOPENTA[E][1,3]OXAZIN-4-YL)-PHENYL-AMIDES AS BACE1 INHIBITORS 有权
标题翻译： N-（3-（2-氨基 - 6,6-二氟-4,4A，5,6,7,7a-十六氢 - 环戊二烯并[E] [1,3]氧杂-4-基） - 苯甲酰胺 BACE1抑制剂
公开(公告)号：US20130072478A1
公开(公告)日：2013-03-21
申请号：US13609304
申请日：2012-09-11
申请人： Hans Hilpert , Emmanuel Pinard , Thomas Woltering
发明人： Hans Hilpert , Emmanuel Pinard , Thomas Woltering
IPC分类号： C07D413/12 , C07D265/12 , A61P25/28 , A61K31/536
CPC分类号： C07D413/12
摘要： The present invention provides N-(3-(2-amino-6,6-difluoro-4,4a,5,6,7,7a-hexahydro-cyclopenta[e][1,3]oxazin-4-yl)-phenyl)-amides of formula I having BACE1 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease.
摘要翻译：本发明提供N-（3-（2-氨基-6,6-二氟-4,4a，5,6,7,7a-六氢 - 环戊二烯并[e] [1,3]恶嗪-4-基） - 苯基） - 具有BACE1抑制活性的式I的酰胺，其制备，含有它们的药物组合物及其作为治疗活性物质的用途。本发明的活性化合物可用于例如治疗和/或预防性治疗。阿尔茨海默氏病。

14. 发明授权

US08207220B2 Substituted benzothiazoles as orexin antagonists 有权
标题翻译：取代的苯并噻唑作为食欲素拮抗剂
公开(公告)号：US08207220B2
公开(公告)日：2012-06-26
申请号：US12958440
申请日：2010-12-02
申请人： Henner Knust , Matthias Nettekoven , Emmanuel Pinard , Olivier Roche , Mark Rogers-Evans
发明人： Henner Knust , Matthias Nettekoven , Emmanuel Pinard , Olivier Roche , Mark Rogers-Evans
IPC分类号： A61K31/38
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。

15. 发明授权

US08153679B2 Radiolabelled inhibitors of the glycine 1 transporter 有权
标题翻译：甘氨酸1转运蛋白的放射性标记抑制剂
公开(公告)号：US08153679B2
公开(公告)日：2012-04-10
申请号：US12607111
申请日：2009-10-28
申请人： Daniela Alberati , Edilio Maurizio Borroni , Thomas Hartung , Roger David Norcross , Emmanuel Pinard
发明人： Daniela Alberati , Edilio Maurizio Borroni , Thomas Hartung , Roger David Norcross , Emmanuel Pinard
IPC分类号： A61K31/4035 , C07D209/44 , C07D405/04
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. wherein R1 is isopropoxy or 2,2,2-trifluoro-1-methyl-ethoxy; and R2 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。

16. 发明授权

US08143273B2 Quinolizidine and indolizidine derivatives 有权
标题翻译：喹诺啶和吲哚来啶衍生物
公开(公告)号：US08143273B2
公开(公告)日：2012-03-27
申请号：US13161534
申请日：2011-06-16
申请人： Sabine Kolczewski , Emmanuel Pinard
发明人： Sabine Kolczewski , Emmanuel Pinard
IPC分类号： A61K31/44 , C07D217/02
CPC分类号： C07D455/02 , C07D471/04
摘要： The present invention relates to a compound of formula I-A or I-B wherein X, R1, R2 and R3 are defined herein; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer thereof. The compounds of formulas I-A and I-B are good inhibitors of the glycine transporter 1 (GlyT-1), and have a good selectivity to glycine transporter 2 (GlyT-2) inhibitors, suitable in the treatment of neurological and neuropsychiatric disorders.
摘要翻译：本发明涉及式I-A或I-B化合物，其中X，R 1，R 2和R 3在本文中定义; 或其药学上可接受的酸加成盐，或其相应的对映异构体和/或其旋光异构体。式I-A和I-B的化合物是甘氨酸转运蛋白1（GlyT-1）的良好抑制剂，并且对甘氨酸转运蛋白2（GlyT-2）抑制剂具有良好的选择性，适用于治疗神经和神经精神障碍。

17. 发明申请

US20110312993A1 AMIDO-TROPANE DERIVATIVES 有权
标题翻译： AMIDO-TROPANE衍生物
公开(公告)号：US20110312993A1
公开(公告)日：2011-12-22
申请号：US13160559
申请日：2011-06-15
申请人： Sabine Kolczewski , Emmanuel Pinard
发明人： Sabine Kolczewski , Emmanuel Pinard
IPC分类号： A61K31/46 , A61P25/00 , A61P25/18 , C07D451/02 , A61P25/28
CPC分类号： C07D451/02 , A61K9/2018 , A61K9/2054 , A61K9/4858 , A61K9/4866
摘要： The present invention relates to a compound of formula I wherein R1, R2 and R3 are each independently hydrogen, lower alkyl, lower alkoxy, cycloalkyl, lower alkyl substituted by halogen or S-lower alkyl; or to a pharmaceutically acceptable acid addition salt, racemic mixture, or corresponding enantiomer and/or optical isomer thereof. The compounds of formula I are good inhibitors of the glycine transporter 1 (GlyT-1), and have a good selectivity to glycine transporter 2 (GlyT-2) inhibitors. The compounds can be used in the treatment of neurological and neuropsychiatric disorders.
摘要翻译：本发明涉及式I化合物，其中R 1，R 2和R 3各自独立地为氢，低级烷基，低级烷氧基，环烷基，被卤素或S-低级烷基取代的低级烷基; 或其药学上可接受的酸加成盐，外消旋混合物或其相应的对映异构体和/或其光学异构体。式I化合物是甘氨酸转运蛋白1（GlyT-1）的良好抑制剂，对甘氨酸转运蛋白2（GlyT-2）抑制剂具有良好的选择性。该化合物可用于治疗神经和神经精神障碍。

18. 发明授权

US07829563B2 Aminoamides as orexin antagonists 失效
标题翻译：氨基酰胺作为食欲肽拮抗剂
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。

19. 发明授权

US07790763B2 Substituted phenyl methanone derivatives 失效
标题翻译：取代苯甲酮衍生物
公开(公告)号：US07790763B2
公开(公告)日：2010-09-07
申请号：US11332999
申请日：2006-01-17
申请人： Synese Jolidon , Robert Narquizian , Roger David Norcross , Emmanuel Pinard
发明人： Synese Jolidon , Robert Narquizian , Roger David Norcross , Emmanuel Pinard
IPC分类号： A61K31/40 , C07D295/27
CPC分类号： C07D207/12 , C07D205/04 , C07D211/46 , C07D401/12
摘要： The present invention relates to compounds of formula I wherein R1, R2, R3, n, and m, are as defined in the specification and to pharmaceutically acceptable acid addition salts thereof. These compounds are good inhibitors of the glycine transporter 1 (GlyT-1) and are useful for the treatment of CNS disorders such as schizophrenia, cognitive impairment, and Alzheimer's disease.
摘要翻译：本发明涉及式I化合物，其中R 1，R 2，R 3，n和m如说明书中所定义，及其药学上可接受的酸加成盐。这些化合物是甘氨酸转运蛋白1（GlyT-1）的良好抑制剂，可用于治疗中枢神经系统疾病如精神分裂症，认知障碍和阿尔茨海默病。

20. 发明申请

US20100029664A1 PYRROLIDIN-3-YLMETHYL-AMINE AS OREXIN ANTAGONISTS 有权
标题翻译：吡咯烷-3-基甲基胺作为OREXIN拮抗剂
公开(公告)号：US20100029664A1
公开(公告)日：2010-02-04
申请号：US12506302
申请日：2009-07-21
申请人： Henner Knust , Matthias Nettekoven , Emmanuel Pinard , Olivier Roche , Mark Rogers-Evans
发明人： Henner Knust , Matthias Nettekoven , Emmanuel Pinard , Olivier Roche , Mark Rogers-Evans
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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