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公开(公告)号：US20090054459A1
公开(公告)日：2009-02-26
申请号：US12245416
申请日：2008-10-03
申请人： Oliver Schadt , Henning Bottcher , Joachim Leibrock , Kai Schiemann , Timo Heinrich , Gunter Holzemann , Christoph van Amsterdam , Gerd Bartoszyk , Christoph Seyfried
发明人： Oliver Schadt , Henning Bottcher , Joachim Leibrock , Kai Schiemann , Timo Heinrich , Gunter Holzemann , Christoph van Amsterdam , Gerd Bartoszyk , Christoph Seyfried
IPC分类号： A61K31/496 , C07K1/113 , A61K31/438 , A61K31/454
CPC分类号： C07D231/12 , C07D209/42 , C07D233/56 , C07D249/08 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D417/12 , C07D417/14 , C07D471/04
摘要： Substituted indoles of the formula (I) and physiologically acceptable derivatives and salts thereof, in which R1, D, E, R12, p, X1, E, G, X2 and Z are as defined in claim 1, exhibit particular actions on the central nervous system, especially 5HT reuptake-inhibiting and 5 HTx-agonistic and/or -antagonistic actions and in particular serotonin-agonistic and -antagonistic properties and can be employed as antipsychotics, neuroleptics, antidepressants, anxiolyties and/or antihypertonics. They can furthermore be employed as excitatory amino acid antagonists for combating neurodegenerative diseases, including cerebrovascular diseases, epilepsy, schizophrenia, Alzheimer's disease, Parkinson's disease, Huntington's disease, cerebral ischaemia, infarction or psychoses
摘要翻译： 其中R1，D，E，R12，p，X1，E，G，X2和Z如权利要求1所定义的式（I）的取代吲哚及其生理上可接受的衍生物和盐表现出对中心的特定作用 神经系统，特别是5HT再摄取抑制和5 HTx-激动和/或拮抗作用，特别是5-羟色胺 - 激动和 - 拮抗性质，并且可以用作抗精神病药，神经安定药，抗抑郁药，抗焦虑药和/或抗高血压药。 此外，它们还可用作用于对抗神经变性疾病的兴奋性氨基酸拮抗剂，包括脑血管疾病，癫痫，精神分裂症，阿尔茨海默病，帕金森病，亨廷顿病，脑局部缺血，梗塞或精神病
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公开(公告)号：US20070099933A1
公开(公告)日：2007-05-03
申请号：US10560734
申请日：2004-05-24
申请人： Timo Heinrich , Henning Bottcher , Kai Schiemann , Gunter Holzemann , Christoph van Amsterdam , Gerd Bartoszyk , Joachim Leibrock , Christoph Seyfried
发明人： Timo Heinrich , Henning Bottcher , Kai Schiemann , Gunter Holzemann , Christoph van Amsterdam , Gerd Bartoszyk , Joachim Leibrock , Christoph Seyfried
IPC分类号： A61K31/496 , A61K31/454 , C07D405/14
CPC分类号： C07D405/12
摘要： Compounds of the formula (I), the use thereof for the preparation of a medicament for the treatment of diseases associated with the serotonin receptor and/or serotonin reuptake, in particular for the preparation of a medicament as anxiolytic, antidepressant, neuroleptic and/or antihypertonic and/or for positively influencing obsessive-compulsive disorder (OCD), sleeping disorders, tardive dyskinesia, learning disorders, age-dependent memory disorders, eating disorders, such as bulimia, and/or sexual dysfunctions. The compounds bind to the 5-HT1A receptor
摘要翻译： 式（I）的化合物，其用于制备用于治疗与5-羟色胺受体和/或5-羟色胺再摄取有关的疾病的药物的用途，特别是制备抗焦虑药，抗抑郁药，精神安定药和/或 和/或积极影响强迫症（OCD），睡眠障碍，迟发性运动障碍，学习障碍，年龄依赖性记忆障碍，进食障碍如贪食症和/或性功能障碍。 该化合物与5-HT 1A 1A受体结合
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公开(公告)号：US20060160824A1
公开(公告)日：2006-07-20
申请号：US10560737
申请日：2004-05-24
申请人： Timo Heinrich , Henning Bottcher , Kai Schiemann , Gunter Holzemann , Christoph van Amsterdam , Gerd Bartoszyk , Joachim Leibrock , Christoph Seyfried
发明人： Timo Heinrich , Henning Bottcher , Kai Schiemann , Gunter Holzemann , Christoph van Amsterdam , Gerd Bartoszyk , Joachim Leibrock , Christoph Seyfried
IPC分类号： A61K31/496 , C07D405/14
CPC分类号： C07D405/12 , C07D405/14
摘要： Compounds of the formula (I), the use thereof for the preparation of a medicament for the treatment of diseases associated with the serotonin receptor and/or serotonin reuptake, in particular for the preparation of a medicament as anxiolytic, antidepressant, neuroleptic and/or antihypertonic and/or for positively influencing obsessive-compulsive disorder (OCD), sleeping disorders, tardive dyskinesia, learning disorders, age-dependent memory disorders, eating disorders, such as bulimia or IBS, and/or sexual dysfunctions. The compounds bind to the 5-HT1A receptor
摘要翻译： 式（I）的化合物，其用于制备用于治疗与5-羟色胺受体和/或5-羟色胺再摄取有关的疾病的药物的用途，特别是制备抗焦虑药，抗抑郁药，精神安定药和/或 和/或积极影响强迫症（OCD），睡眠障碍，迟发性运动障碍，学习障碍，年龄依赖性记忆障碍，进食障碍，如贪食症或IBS，和/或性功能障碍。 该化合物与5-HT 1A 1A受体结合
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公开(公告)号：US20060122191A1
公开(公告)日：2006-06-08
申请号：US10539516
申请日：2003-11-27
申请人： Timo Heinrich , Henning Bottcher , Kali Schiemann , Gunter Holzemann , Christoph Van Amsterdam , Gerd Bartoszyk , Joachim Leibrock , Christoph Seyfried
发明人： Timo Heinrich , Henning Bottcher , Kali Schiemann , Gunter Holzemann , Christoph Van Amsterdam , Gerd Bartoszyk , Joachim Leibrock , Christoph Seyfried
IPC分类号： A61K31/496 , C07D417/14 , C07D405/14
CPC分类号： C07D405/12 , C07D209/14 , C07D209/18 , C07D209/42 , C07D417/12
摘要： N-(indolethyl-)cycloamine compounds of the formula (I): in which R1′, R1″ X, Ar, and n have a meaning indicated in Claim 1, are serotonin reuptake inhibitors (SSRIs) and effectors of the serotonergic receptors 5-HT1A and 5-HT2A. They are therefore suitable for the prophylaxis or treatment of various diseases of the central nervous system, such as depression, dyskinesia, Parkinson's disease, dementia, strokes, schizophrenia, Alzheimer's disease, Lewy bodies dementia, Huntington's disease, Tourette's syndrome, anxiety, learning and memory impairment, pain, sleeping disorders and neurodegenerative diseases.
摘要翻译： 式（I）的N-（吲哚基 - ）环胺化合物：其中R 1，R 1，X，Ar和n具有以下含义： 权利要求1是5-羟色胺再摄取抑制剂（SSRI）和5-羟色胺受体5-HT 1A和5-HT 2A 2A的作用剂。 因此，它们适合于预防或治疗中枢神经系统的各种疾病，例如抑郁症，运动障碍，帕金森病，痴呆，中风，精神分裂症，阿尔茨海默病，路易体痴呆，亨廷顿病，图雷特综合征，焦虑症，学习和 记忆障碍，疼痛，睡眠障碍和神经退行性疾病。
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5.发明申请Benzofurane derivatives and the use the same as antidepressants and anxiolytics 失效苯并呋喃衍生物与抗抑郁药和抗焦虑药一样使用公开(公告)号：US20060142372A1
公开(公告)日：2006-06-29
申请号：US10545170
申请日：2004-01-10
申请人： Gunter Holzemann , Henning Bottcher , Kai Schiemann , Timo Heinrich , Joachim Leibrock , Christoph Van Amsterdam , Gerd Bartpszyk , Christoph Seyfried
发明人： Gunter Holzemann , Henning Bottcher , Kai Schiemann , Timo Heinrich , Joachim Leibrock , Christoph Van Amsterdam , Gerd Bartpszyk , Christoph Seyfried
IPC分类号： A61K31/405 , C07D405/02
CPC分类号： C07D405/12
摘要： Novel benzofuran derivatives of the formula (I) in which R1, R2, X, Y, Z and m have the meanings indicated in Patent Claim 1, they have a strong affinity to the 5-HT1A receptors. The compounds inhibit serotonin reuptake, exhibit serotonin-agonistic and -antagonistic properties and are suitable as antidepressants, anxiolytics, antipsychotics, neuroleptics and/or antihypertonics.
摘要翻译： 其中R 1，R 2，X，Y，Z和m的式（I）的新型苯并呋喃衍生物具有专利权利要求1中所示的含义，它们具有 对5-HT 1A 1A受体的强亲和力。 这些化合物抑制5-羟色胺再摄取，显示5-羟色胺 - 激动和拮抗性质，并且适合作为抗抑郁药，抗焦虑药，抗精神病药，精神安定药和/或抗高血压药。
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公开(公告)号：US20060116405A1
公开(公告)日：2006-06-01
申请号：US10538639
申请日：2003-11-17
申请人： Gunter Hoelzemann , Helene Crassier , Henning Bottcher , Timo Heinrich , Kai Schiemann , Joachim Leibrock , Chrisoph Van Amsterdam , Gerd Bartoszyk , Christoph Seyfried
发明人： Gunter Hoelzemann , Helene Crassier , Henning Bottcher , Timo Heinrich , Kai Schiemann , Joachim Leibrock , Chrisoph Van Amsterdam , Gerd Bartoszyk , Christoph Seyfried
IPC分类号： A61K31/433 , A61K31/4245 , C07D417/02 , C07D413/02
CPC分类号： C07D413/12 , C07D417/12
摘要： The invention relates to indol derivatives of Formula (I) in which R1, R2, R3, X, A, n, m and p have the meanings indicated above.
摘要翻译： 本发明涉及式（I）的吲哚衍生物，其中R 1，R 2，R 3，X，A，n，m和p具有上述含义。
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公开(公告)号：US20060084693A1
公开(公告)日：2006-04-20
申请号：US10546029
申请日：2004-01-19
申请人： Guenter Holzemann , Kai Schiemann , Henning Bottcher , Timo Heinrich , Christoph Seyfried , Joachim Leibrock , Chrisoph Van Amsterdam , Gerd Bartoszyk
发明人： Guenter Holzemann , Kai Schiemann , Henning Bottcher , Timo Heinrich , Christoph Seyfried , Joachim Leibrock , Chrisoph Van Amsterdam , Gerd Bartoszyk
IPC分类号： A61K31/405 , C07D405/02
CPC分类号： C07D405/12
摘要： Novel benzofuranoxyethylamines of the formula (1), in which R1, R2, R3, R4, m and n have the meanings indicated in Patent Claim (1), which have a strong affinity to the 5 HT1A receptors and/or 5HT1D receptors. The compounds inhibit serotonin reuptake, exhibit serotonin-agonistic and -antagonistic properties and are suitable as antidepressants, anxiolytics, antipsychotics, neuroleptics and/or antihypertonics.
摘要翻译： 式（1）的新型苯并呋喃氧基乙胺，其中R 1，R 2，R 3，R 4， ，m和n具有与专利权利要求（1）中所示的含义，其对5HT 1A受体和/或5HT 1D受体具有强亲和力。 这些化合物抑制5-羟色胺再摄取，显示5-羟色胺 - 激动和拮抗性质，并且适合作为抗抑郁药，抗焦虑药，抗精神病药，精神安定药和/或抗高血压药。
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公开(公告)号：US5418237A
公开(公告)日：1995-05-23
申请号：US262256
申请日：1994-06-13
IPC分类号： A61K31/495 , A61K31/40 , A61K31/496 , A61K31/5377 , A61P9/12 , A61P25/00 , A61P25/18 , A61P25/20 , A61P25/24 , A61P25/26 , A61P43/00 , C07D209/14 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/04 , C07D403/06 , C07D405/12 , C07D413/06 , C07D498/10 , C07D403/00
CPC分类号： C07D401/06 , C07D209/14 , C07D401/12 , C07D403/04 , C07D403/06 , C07D405/12
摘要： Indole derivatives of formula I ##STR1## wherein Ind, Q and Ar are as defined herein, and their salts, are active on the central nervous system.
摘要翻译： 其中Ind，Q和Ar如本文所定义的式I的吲哚衍生物及其盐在中枢神经系统上是有活性的。
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公开(公告)号：US5693655A
公开(公告)日：1997-12-02
申请号：US426405
申请日：1995-04-21
IPC分类号： A61K31/4427 , A61K31/445 , A61K31/454 , A61P9/10 , A61P9/12 , A61P25/04 , A61P25/20 , A61P25/24 , A61P43/00 , C07D209/14 , C07D211/14 , C07D401/14 , C07D491/04 , C07D491/056
CPC分类号： C07D401/14 , C07D491/04
摘要： 3-Indolylpiperidines of the formula I ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are in each case independently of one another H, A, OH, OA, F, Cl, Br, Z, CN, CF.sub.3, COOH, CONH.sub.2, CONHA, CONA.sub.2, or COOA, or R.sup.1 and R.sup.2 and also R.sup.3 and R.sup.4 in each case together are also methylenedioxy, R.sup.5 is H or OH, R.sup.6 is H or R.sup.5 and R.sup.6 together are also a bond, A is alkyl having 1 to 6 C atoms and n is 2, 3, 4, 5 or 6, and to their physiologically acceptable salts, exhibit action on the central nervous system, in particular dopamine-agonistic or dopamine-antagonistic action.
摘要翻译： 式I的3-吲哚基哌啶其中R 1，R 2，R 3和R 4各自独立地为H，A，OH，OA，F，Cl，Br，Z，CN，CF 3，COOH，CONH 2 ，CONHA，CONA2或COOA，或者R 1和R 2以及R 3和R 4在一起也是亚甲二氧基，R 5是H或OH，R 6是H或R 5，R 6一起也是键，A是具有1至 6个C原子，n为2,3,4,5或6及其生理上可接受的盐，对中枢神经系统，特别是多巴胺激动剂或多巴胺拮抗作用表现出作用。
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公开(公告)号：US06258813B1
公开(公告)日：2001-07-10
申请号：US09254489
申请日：1999-03-09
IPC分类号： A61K31496
CPC分类号： C07D213/74 , C07D213/38 , C07D239/42 , C07D295/073 , C07D295/096 , C07D295/155 , C07D401/12 , C07D405/12 , C07D409/12
摘要： Piperazine derivatives of the formula I in which R1 and R2 have the meanings given in claim 1 are dopamine ligands with a selectivity for the D4 receptor and are suitable for the treatment and prophylaxis of states of anxiety, depression, schizophrenia, obsessions, Parkinson's disease, tardive dyskinesia, nausea and disorders of the gastro-intestinal tract.
摘要翻译： R1和R2具有权利要求1中给出的含义的式Iin的哌嗪衍生物是对D4受体具有选择性的多巴胺配体，并且适用于治疗和预防焦虑，抑郁，精神分裂症，痴呆，帕金森病，迟发性 运动障碍，恶心和胃肠道疾病。
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