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21. 发明申请

US20050009878A1 Imidazole derivatives 有权
标题翻译：咪唑衍生物
公开(公告)号：US20050009878A1
公开(公告)日：2005-01-13
申请号：US10874948
申请日：2004-06-23
申请人： Bernd Buettelmann , Simona Ceccarelli , Georg Jaeschke , Sabine Kolczewski , Richard Porter , Eric Vieira
发明人： Bernd Buettelmann , Simona Ceccarelli , Georg Jaeschke , Sabine Kolczewski , Richard Porter , Eric Vieira
IPC分类号： A61K31/4178 , A61K31/4439 , A61P25/00 , A61P25/22 , C07D401/06 , C07
CPC分类号： C07D401/06 , A61K31/4178 , A61K31/4439
摘要： The present invention relates to imidazole derivatives of the general formula wherein R1, R2, R3 and R4 are as defined hereinabove. This invention also relates to the compound's pharmaceutically acceptable salt and processes for the preparation thereof. These compounds can be used for the manufacture of pharmaceutical compositions for the treatment and 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's disease, cognitive disorders and memory deficit disorders, as well as chronic and acute pain.
摘要翻译：本发明涉及以下通式的咪唑衍生物：其中R 1，R 2，R 3和R 4如上所定义。本发明还涉及该化合物的药学上可接受的盐及其制备方法。这些化合物可用于制备用于治疗和预防mGluR5受体介导的病症的药物组合物。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障碍以及慢性和急性疼痛。

22. 发明授权

US06248901B1 Heterocyclic vinyl ethers 失效
标题翻译：杂环乙烯基醚
公开(公告)号：US06248901B1
公开(公告)日：2001-06-19
申请号：US09304909
申请日：1999-05-04
申请人： Geo Adam , Sabine Kolczewski , Vincent Mutel , Heinz Stadler , Jürgen Wichmann , Thomas Johannes Woltering
发明人： Geo Adam , Sabine Kolczewski , Vincent Mutel , Heinz Stadler , Jürgen Wichmann , Thomas Johannes Woltering
IPC分类号： C07D24908
CPC分类号： C07D257/04 , A61K31/41 , A61K31/4174 , A61K31/4196 , C07D231/12 , C07D233/56 , C07D249/08
摘要： The compounds of the formula wherein R signifies halogen or lower alkyl; n signifies 0-3; R1 signifies lower alkyl; cycloalkyl; benzyl optionally substituted by hydroxy, halogen, lower alkoxy or lower alkyl; benzoyl optionally substituted by amino, lower alkylamino or di-lower alkylamino; acetyl or cycloalkyl-carbonyl; and signifies an aromatic 5-membered residue which is bonded via a N-atom and which contains further 1-3 N atoms in addition to the linking N atom, as well as their pharmaceutically acceptable salts as therapeutically active substances, especially for the control or prevention of acute and/or chronic neurological disorders.
摘要翻译：化合物R表示卤素或低级烷基; n表示0-3; R1表示低级烷基; 环烷基任选被羟基，卤素，低级烷氧基或低级烷基取代的苄基; 任选被氨基，低级烷基氨基或二 - 低级烷基氨基取代的苯甲酰基; 乙酰基或环烷基 - 羰基; 并且通过N-原子键合并且除了连接的N原子还含有1-3个N原子的芳族5元残基以及它们的药学上可接受的盐作为治疗活性物质，特别是用于控制或预防的急性和/或慢性神经障碍。

23. 发明授权

US6054588A Heterocyclic vinyl ethers 失效
标题翻译：杂环乙烯基醚
公开(公告)号：US6054588A
公开(公告)日：2000-04-25
申请号：US304624
申请日：1999-05-04
申请人： Geo Adam , Sabine Kolczewski , Vincent Mutel , Heinz Stadler , Jurgen Wichmann , Thomas Johannes Woltering
发明人： Geo Adam , Sabine Kolczewski , Vincent Mutel , Heinz Stadler , Jurgen Wichmann , Thomas Johannes Woltering
IPC分类号： A61K31/41 , A61K31/4164 , A61K31/4174 , A61K31/4196 , A61P1/08 , A61P13/02 , A61P21/02 , A61P25/00 , A61P25/06 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/34 , A61P25/36 , A61P27/02 , A61P29/00 , C07D233/60 , C07D249/08 , C07D257/04 , C07D521/00
CPC分类号： C07D257/04 , A61K31/41 , A61K31/4174 , A61K31/4196 , C07D231/12 , C07D233/56 , C07D249/08
摘要： The compounds of the formula ##STR1## wherein R signifies halogen or lower alkyl;n signifies 0-3;R.sup.1 signifies lower alkyl; cycloalkyl; benzyl optionally substituted by hydroxy, halogen, lower alkoxy or lower alkyl; benzoyl optionally substituted by amino, lower alkyl-amino or di-lower alkylamino; acetyl or cycloalkyl-carbonyl; and ##STR2## signifies an aromatic 5-membered residue which is bonded via a N-atom and which contains further 1-3 N atoms in addition to the linking N atom,as well as their pharmaceutically acceptable salts as therapeutically active substances, especially for the control or prevention of acute and/or chronic neurological disorders.
摘要翻译：下式的化合物其中R表示卤素或低级烷基; n表示0-3; R1表示低级烷基; 环烷基任选被羟基，卤素，低级烷氧基或低级烷基取代的苄基; 任选被氨基，低级烷基 - 氨基或二 - 低级烷基氨基取代的苯甲酰基; 乙酰基或环烷基 - 羰基; 并且表示通过N-原子键合并且除了连接的N原子之外还含有1-3个N原子的芳族5元残基以及它们的药学上可接受的盐作为治疗活性物质，特别是用于对照或预防急性和/或慢性神经障碍。

24. 发明授权

US5869500A Pyridone compounds useful in treating Alzheimer's disease 失效
标题翻译：可用于治疗阿尔茨海默病的吡啶酮化合物
公开(公告)号：US5869500A
公开(公告)日：1999-02-09
申请号：US976541
申请日：1997-11-24
申请人： Gerda Huber Trottmann , Roland Jakob-Roetne , Sabine Kolczewski , Roger David Norcross , Thomas Johannes Woltering
发明人： Gerda Huber Trottmann , Roland Jakob-Roetne , Sabine Kolczewski , Roger David Norcross , Thomas Johannes Woltering
IPC分类号： C07D455/02 , C07D455/06 , C07D471/14 , C07D495/14 , A61K31/44 , A61K31/38 , A61K31/40 , A61K31/55
CPC分类号： C07D471/14 , C07D455/02 , C07D455/06 , C07D495/14
摘要： The invention is concerned with the use of bi- and tricyclic pyridone compounds of the formula ##STR1## where A, R.sup.1, R.sup.3, R.sup.4, and R.sup.7 are described herein and of their pharmaceutically acceptable salts for the production of medicaments for the prophylaxis or treatment of illnesses which are connected with an inhibition of .beta.-amyloid peptide activity, especially for the treatment of Alzheimer's disease.
摘要翻译：本发明涉及使用本文所述的式Ⅰ，R1，R3，R4和R7的式和其三价环吡啶酮化合物及其药学上可接受的盐，用于生产药物用于预防或治疗与抑制β-淀粉样蛋白肽活性相关的疾病，特别是用于治疗阿尔茨海默病。

25. 发明授权

US08293916B2 Diazole derivatives 失效
标题翻译：二唑衍生物
公开(公告)号：US08293916B2
公开(公告)日：2012-10-23
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： A61K31/4439 , C07D401/04 , C07D401/06 , C07D401/14
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。

26. 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。

27. 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。

28. 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。

29. 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。

30. 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。

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