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21. 发明申请

US20120232033A1 AMINES OR AMINO ALCOHOLS AS GLYT1 INHIBITORS 失效
标题翻译：氨基或氨基醇作为GLYT1抑制剂
公开(公告)号：US20120232033A1
公开(公告)日：2012-09-13
申请号：US13480520
申请日：2012-05-25
申请人： Sabine Kolczewski , Hans-Peter Marty , Robert Narquizian , Emmanuel Pinnard , Henri Stalder
发明人： Sabine Kolczewski , Hans-Peter Marty , Robert Narquizian , Emmanuel Pinnard , Henri Stalder
IPC分类号： C07C217/70 , A61K31/137 , C07D213/61 , A61K31/4418 , C07D309/10 , A61K31/351 , C07D213/38 , C07D401/04 , A61K31/444 , C07D405/12 , A61K31/443 , C07D307/20 , A61K31/341 , A61K31/4433 , A61K31/44 , C07D305/06 , A61K31/337 , C07F7/10 , A61K31/695 , C07D239/26 , A61K31/505 , C07D413/04 , A61K31/5377 , A61P25/18 , A61P25/28 , A61P25/00 , C07C317/32
CPC分类号： A61K31/16 , C07C215/30 , C07C215/68 , C07C217/70 , C07C233/43 , C07C237/30 , C07C317/32 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07D211/46 , C07D213/38 , C07D213/61 , C07D213/64 , C07D213/65 , C07D213/71 , C07D213/73 , C07D239/26 , C07D277/28 , C07D305/06 , C07D307/12 , C07D307/20 , C07D309/06 , C07D309/12 , C07D333/20 , C07D335/02 , C07D405/12
摘要： The invention relates to the use of compounds of formula I wherein the substituents are described in the description and claims for the treatment of psychoses, dysfunction in memory and learning, schizophrenia, dementia, attention deficit disorders or Alzheimer's disease. The invention also relates to some compounds of formula I and pharmaceutical compositions containing them.
摘要翻译：本发明涉及式I化合物的用途，其中取代基在描述和权利要求中描述用于治疗精神病，记忆障碍和学习功能障碍，精神分裂症，痴呆，注意力缺陷障碍或阿尔茨海默病。本发明还涉及一些式I化合物和含有它们的药物组合物。

22. 发明申请

US20110313165A1 QUINOLIZIDINE AND INDOLIZIDINE DERIVATIVES 有权
标题翻译：喹诺酮和吲哚来啶衍生物
公开(公告)号：US20110313165A1
公开(公告)日：2011-12-22
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： C07D471/04 , C07D455/00
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。

23. 发明授权

US07923561B2 Quinolines 失效
标题翻译：喹啉
公开(公告)号：US07923561B2
公开(公告)日：2011-04-12
申请号：US11946947
申请日：2007-11-29
申请人： Sabine Kolczewski , Claus Riemer , Lucinda Steward , Juergen Wichmann , Thomas Woltering
发明人： Sabine Kolczewski , Claus Riemer , Lucinda Steward , Juergen Wichmann , Thomas Woltering
IPC分类号： C07D215/38
CPC分类号： C07D215/38 , C07D401/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12
摘要： The present invention relates to 2-Aminoquinoline derivatives of general formula I and pharmaceutically-acceptable acid-addition salts thereof, wherein R1, R2 and X are as defined in the specification. The compounds may be used as 5-HT5A receptor antagonists. The present invention relates also to processes for making such a compound and a pharmaceutical composition comprising such a compound. Compounds of the present invention are useful in the prevention and/or treatment of anxiety 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, withdrawal from abuse of drugs, motor disorders such as Parkinson's disease, psychiatric disorders and gastrointestinal disorders.
摘要翻译：本发明涉及通式I的2-氨基喹啉衍生物及其药学上可接受的酸加成盐，其中R1，R2和X如说明书中所定义。该化合物可以用作5-HT5A受体拮抗剂。本发明还涉及制备这种化合物的方法和包含这种化合物的药物组合物。本发明的化合物可用于预防和/或治疗焦虑抑郁症，焦虑障碍，精神分裂症，恐慌症，广场恐惧症，社交恐惧症，强迫症，创伤后应激障碍，疼痛，记忆障碍，痴呆症，饮食行为，性功能障碍，睡眠障碍，戒毒，运动障碍如帕金森病，精神疾病和胃肠道疾病。

24. 发明授权

US07875645B2 Method for the treatment of CNS disorders with substituted 2-imidazoles or imidazole derivatives 失效
标题翻译：用取代的2-咪唑或咪唑衍生物治疗CNS障碍的方法
公开(公告)号：US07875645B2
公开(公告)日：2011-01-25
申请号：US11655468
申请日：2007-01-19
申请人： Guido Galley , Katrin Groebke Zbinden , Marius Hoener , Sabine Kolczewski , Roger Norcross , Henri Stalder
发明人： Guido Galley , Katrin Groebke Zbinden , Marius Hoener , Sabine Kolczewski , Roger Norcross , Henri Stalder
IPC分类号： A61K31/415 , C07D233/56
CPC分类号： C07D233/06 , A61K31/4164 , A61K31/4178 , C07D233/20 , C07D233/22 , C07D233/56 , C07D233/64 , C07D401/10 , C07D403/06 , C07D405/06 , C07D409/06
摘要： The present invention relates a method for treating depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder, stress-related disorders, psychotic disorders such as schizophrenia, neurological diseases such as Parkinson's disease, neurodegenerative disorders such as Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse and metabolic disorders such as eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders which comprises administering to an individual a therapeutically effective amount of a compound of formula I wherein R, R1, R2, A and n are as defined in the specification and to their pharmaceutically active salts. The invention also relates to novel compounds of formula I, pharmaceutical compositions containing them, and methods for their preparation.
摘要翻译：本发明涉及治疗抑郁症，焦虑障碍，双相情感障碍，注意缺陷多动障碍，应激相关障碍，精神病如精神分裂症，神经系统疾病如帕金森病，神经变性疾病如阿尔茨海默病，癫痫，偏头痛，高血压，药物滥用和代谢障碍如进食障碍，糖尿病，糖尿病并发症，肥胖症，血脂异常，能量消耗和同化障碍，体温平衡紊乱和失调，睡眠和昼夜节律紊乱以及心血管疾病，其包括给予个体治疗有效量的式I化合物，其中R，R 1，R 2，A和n如说明书中所定义，并且其药物活性盐。本发明还涉及式I的新型化合物，含有它们的药物组合物及其制备方法。

25. 发明授权

US07790732B2 5-Chloro-4-alkyl-3,4-dihydro-quinazolin-2-ylamine derivatives 失效
标题翻译： 5-氯-4-烷基-3,4-二氢 - 喹唑啉-2-基胺衍生物
公开(公告)号：US07790732B2
公开(公告)日：2010-09-07
申请号：US11472081
申请日：2006-06-21
申请人： Alexander Alanine , Luca Claudio Gobbi , Sabine Kolczewski , Thomas Luebbers , Jens-Uwe Peters , Lucinda Steward
发明人： Alexander Alanine , Luca Claudio Gobbi , Sabine Kolczewski , Thomas Luebbers , Jens-Uwe Peters , Lucinda Steward
IPC分类号： A61K31/517 , C07D239/84
CPC分类号： C07D239/42 , C07D403/12 , C07D405/12
摘要： The present invention relates to compounds of formula I wherein R1, R2, R3 are as described in the specification and pharmaceutically acceptable acid addition salts and tautomers thereof. Compounds of formula I have good activity on the 5-HT5A receptor. Therefore, the invention provides a method for treating diseases related to this receptor, for example, anxiety, depression, sleep disorders and schizophrenia.
摘要翻译：本发明涉及式I化合物，其中R 1，R 2，R 3如说明书及其药学上可接受的酸加成盐和互变异构体所述。式I化合物对5-HT5A受体具有良好的活性。因此，本发明提供了治疗与该受体有关的疾病的方法，例如焦虑症，抑郁症，睡眠障碍和精神分裂症。

26. 发明申请

US20100048569A1 DIAZOLE DERIVATIVES 失效
标题翻译：二唑衍生物
公开(公告)号：US20100048569A1
公开(公告)日：2010-02-25
申请号：US12613089
申请日：2009-11-05
申请人： Bernd Buettelmann , Simona Maria Ceccarelli , Georg Jaeschke , Sabine Kolczewski , Richard Hugh Philip Porter , Paul Spurr , Eric Vieira
发明人： Bernd Buettelmann , Simona Maria Ceccarelli , Georg Jaeschke , Sabine Kolczewski , Richard Hugh Philip Porter , Paul Spurr , Eric Vieira
IPC分类号： A61K31/5377 , C07D401/02 , A61K31/4439 , C07D413/14 , A61P25/00
CPC分类号： C07D401/06 , C07D401/14
摘要： The present invention relates to diazole derivatives of the general formula wherein A, E, R1, R2 and R3 are as defined in application and pharmaceutical compositions containing them. The invention also relates to use of such compounds for the treatment of diseases mediated by the metabotropic glutamate receptors (mGluR), such as anxiety, chronic and acute pain, protection against liver damage, urinary incontinence, obesity, Fragile-X and autism, Alzheimer's disease, epilepsy, schizophrenia, ischemia, Huntington's chorea, amyotrophic lateral sclerosis (ALS), dementia caused by AIDs, and Parkinson's disease.
摘要翻译：本发明涉及通式的二唑衍生物，其中A，E，R 1，R 2和R 3如申请中所定义，含有它们的药物组合物。本发明还涉及这种化合物用于治疗由代谢型谷氨酸受体（mGluR）介导的疾病的用途，例如焦虑，慢性和急性疼痛，防止肝损伤，尿失禁，肥胖，脆性-X和自闭症，阿尔茨海默病疾病，癫痫，精神分裂症，局部缺血，亨廷顿舞蹈病，肌萎缩性侧索硬化（ALS），AID引起的痴呆和帕金森病。

27. 发明申请

US20090233927A1 2-AMINOQUINOLINES 失效
标题翻译： 2-氨基喹啉
公开(公告)号：US20090233927A1
公开(公告)日：2009-09-17
申请号：US12398415
申请日：2009-03-05
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： A61K31/47 , C07D215/38 , C07D413/02 , A61K31/5377 , A61P25/00
CPC分类号： C07D405/12 , C07D215/38 , C07D491/08
摘要： The present invention is concerned with 2-aminoquinoline derivatives of formula I wherein R1 and R2 are as described herein and pharmaceutically acceptable salts thereof, pharmaceutical compositions containing them, and methods for their manufacture. These compounds are 5-HT5A receptor antagonists, useful for 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R 1和R 2如本文所述及其药学上可接受的盐，含有它们的药物组合物及其制备方法。这些化合物是可用于预防和/或治疗抑郁症，焦虑障碍，精神分裂症，恐慌症，广场恐惧症，社交恐惧症，强迫症，创伤后应激障碍，疼痛，记忆障碍，痴呆症，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，精神病或胃肠道疾病。

28. 发明申请

US20090227570A1 2-AMINOQUINOLINES 失效
标题翻译： 2-氨基喹啉
公开(公告)号：US20090227570A1
公开(公告)日：2009-09-10
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： A61K31/541 , C07D215/38 , A61K31/47 , C07D401/12 , A61K31/496 , C07D413/12 , A61K31/5377 , A61K31/4709 , C07D417/12 , A61P25/24 , A61P25/22 , A61P25/00
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。

29. 发明申请

US20080146567A1 QUINOLINES 失效
标题翻译：金刚石
公开(公告)号：US20080146567A1
公开(公告)日：2008-06-19
申请号：US11946947
申请日：2007-11-29
申请人： Sabine Kolczewski , Claus Riemer , Lucinda Steward , Juergen Wichmann , Thomas Woltering
发明人： Sabine Kolczewski , Claus Riemer , Lucinda Steward , Juergen Wichmann , Thomas Woltering
IPC分类号： A61K31/5377 , C07D215/00 , C07D295/00 , A61P25/00 , A61K31/47
CPC分类号： C07D215/38 , C07D401/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12
摘要： The present invention relates to 2-Aminoquinoline derivatives of general formula I and pharmaceutically-acceptable acid-addition salts thereof, wherein R1, R2 and X are as defined in the specification. The compounds may be used as 5-HT5A receptor antagonists. The present invention relates also to processes for making such a compound and a pharmaceutical composition comprising such a compound. Compounds of the present invention are useful in the prevention and/or treatment of anxiety 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, withdrawal from abuse of drugs, motor disorders such as Parkinson's disease, psychiatric disorders and gastrointestinal disorders.
摘要翻译：本发明涉及通式I的2-氨基喹啉衍生物及其药学上可接受的酸加成盐，其中R 1，R 2和X如规范。该化合物可以用作5-HT 5A受体拮抗剂。本发明还涉及制备这种化合物的方法和包含这种化合物的药物组合物。本发明的化合物可用于预防和/或治疗焦虑抑郁症，焦虑障碍，精神分裂症，恐慌症，广场恐惧症，社交恐惧症，强迫症，创伤后应激障碍，疼痛，记忆障碍，痴呆症，饮食行为，性功能障碍，睡眠障碍，戒毒，运动障碍如帕金森病，精神疾病和胃肠道疾病。

30. 发明申请

US20080119489A1 IMIDAZOLE DERIVATIVES 有权
标题翻译：咪唑衍生物
公开(公告)号：US20080119489A1
公开(公告)日：2008-05-22
申请号：US11930258
申请日：2007-10-31
申请人： Bernd Buettelmann , Simona Maria Ceccarelli , George Jaeschke , Sabine Kolczewski , Richard Hugh Philip Porter , Eric Vieira
发明人： Bernd Buettelmann , Simona Maria Ceccarelli , George Jaeschke , Sabine Kolczewski , Richard Hugh Philip Porter , Eric Vieira
IPC分类号： A61K31/497 , C07D401/06 , A61K31/4439 , C07D401/14 , A61K31/506
CPC分类号： C07D401/06 , C07D401/14
摘要： The present invention relates to imidazole derivatives of formula I wherein R1, R2, R3 and R4 are described hereinabove. These compounds can be used in the treatment or prevention of mGluR5 receptor mediated disorders. These compounds are useful, inter alia, in the treatment or prevention of acute and/or chronic neurological disorders such as psychosis, epilepsy, schizophrenia, Alzheimer' disease, cognititve disorders and memory deficits, as well as chronic and acute pain.
摘要翻译：本发明涉及式I的咪唑衍生物，其中R 1，R 2，R 3和R 4，如上所述。这些化合物可用于治疗或预防mGluR5受体介导的疾病。这些化合物尤其用于治疗或预防急性和/或慢性神经障碍如精神病，癫痫，精神分裂症，阿尔茨海默病，认知障碍和记忆缺陷以及慢性和急性疼痛。

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