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11.发明授权公开(公告)号：US07262216B2
公开(公告)日：2007-08-28
申请号：US10545170
申请日：2004-01-10
申请人： Günter Hölzemann , Henning Böttcher , Kai Schiemann , Timo Heinrich , Joachim Leibrock , Christoph Van Amsterdam , Gerd Bartoszyk , Christoph Seyfried
发明人： Günter Hölzemann , Henning Böttcher , Kai Schiemann , Timo Heinrich , Joachim Leibrock , Christoph Van Amsterdam , Gerd Bartoszyk , Christoph Seyfried
IPC分类号： A61K31/404 , C07D405/12
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。 该化合物抑制5-羟色胺再摄取，显示5-羟色胺 - 激动和拮抗性，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：US06723725B1
公开(公告)日：2004-04-20
申请号：US10031566
申请日：2002-01-22
申请人： Henning Böttcher , Joachim März , Hartmut Greiner , Jürgen Harting , Gerd Bartoszyk , Christoph Seyfried , Christoph van Amsterdam
发明人： Henning Böttcher , Joachim März , Hartmut Greiner , Jürgen Harting , Gerd Bartoszyk , Christoph Seyfried , Christoph van Amsterdam
IPC分类号： A61K31404
CPC分类号： C07D209/12
摘要： Indole derivatives of formula I, their salts and solvates, have valuable pharmacological properties together with good tolerability, as they have actions on the central nervous system: wherein R1 and R3 are as defined herein. The compounds have a strong affinity for 5-HT2A receptors, and furthermore exhibit 5HT2A receptor-antagonistic properties. These are therefore suitable both in veterinary and in human medicine for the treatment of functional disorders of the central nervous system and also of inflammation.
摘要翻译： 式I的吲哚衍生物及其盐和溶剂合物具有有价值的药理学性质以及良好的耐受性，因为它们对中枢神经系统具有作用：其中R 1和R 3如本文所定义。 这些化合物对5-HT2A受体具有强亲和力，并且还表现出5HT2A受体拮抗特性。 因此，这些在兽医和人类医学中都适用于治疗中枢神经系统的功能障碍以及炎症。
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公开(公告)号：US07425574B2
公开(公告)日：2008-09-16
申请号：US10546029
申请日：2004-01-19
申请人： Günter Hölzemann , Kai Schiemann , Henning Böttcher , Timo Heinrich , Christoph Seyfried , Joachim Leibrock , Chrisoph Van Amsterdam , Gerd Bartoszyk
发明人： Günter Hölzemann , Kai Schiemann , Henning Böttcher , Timo Heinrich , Christoph Seyfried , Joachim Leibrock , Chrisoph Van Amsterdam , Gerd Bartoszyk
IPC分类号： A61K31/404 , C07D405/12
CPC分类号： C07D405/12
摘要： Novel benzofuranoxyethylamines of the formula (I), 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（I）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：US06251908B1
公开(公告)日：2001-06-26
申请号：US09462468
申请日：2000-04-03
IPC分类号： C07D40514
CPC分类号： C07D405/12
摘要： Piperazine derivatives of the formula I in which R1, m, k and R2 have the meanings indicated in claim 1, are potent 5-HT1A agonists and exhibit 5-HT-reuptake-inhibiting actions and are suitable for the treatment and prophylaxis of anxiety states, depression, schizophrenia, obsessions, tardive dyskinesias, learning disorders, age-dependent memory disorders, for positively affecting obsessive-compulsive disorder, and also for the treatment and for the control of the sequelae of cerebral infarcts such as stroke and cerebral ischaemias.
摘要翻译： R1，m，k和R2具有权利要求1所述含义的式Iin的哌嗪衍生物是有效的5-HT1A激动剂，具有5-HT-再摄取抑制作用，适用于治疗和预防焦虑状态，抑郁 ，精神分裂症，痴迷症，迟发性运动障碍，学习障碍，年龄依赖性记忆障碍，积极影响强迫症，以及用于治疗和控制脑梗死如脑卒中和脑缺血的后遗症。
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公开(公告)号：US06310068B1
公开(公告)日：2001-10-30
申请号：US08628250
申请日：1996-04-05
IPC分类号： A61K31496
CPC分类号： C07D209/14
摘要： Compound of the formula I in which Q and Ar have the meanings indicated herein, and their salts, exhibit actions on the central nervous system.
摘要翻译： Q和Ar具有本文所示含义的式Iin化合物及其盐在中枢神经系统上表现出作用。
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公开(公告)号：US07618988B2
公开(公告)日：2009-11-17
申请号：US10489960
申请日：2002-08-12
申请人： Henning Böttcher , Ralf Devant , Maria Devant, legal representative , Gerd Bartoszyk , Hermann Russ , Frank Weber , Christoph Seyfried
发明人： Henning Böttcher , Ralf Devant , Gerd Bartoszyk , Hermann Russ , Frank Weber , Christoph Seyfried
IPC分类号： A61K31/135 , A61K31/33 , A61K31/395 , A61K31/535 , A61K31/54 , A61K31/58
CPC分类号： C07D405/12
摘要： Compounds of formula I in which R has a meaning as indicated in claim 1, or one of their optical isomers or pharmaceutically acceptable salts, used for the treatment of extrapyramidal movement disorders and/or adverse effects in extrapyramidal movement disorders and/or for the treatment of extrapyramidal symptoms (EPS) induced by neuroleptics.
摘要翻译： 其中R具有权利要求1所述含义的式I化合物或其用于治疗锥体束外运动障碍和/或锥体外系运动障碍和/或治疗中的副作用的其旋光异构体或药学上可接受的盐之一 的精神分裂症引起的锥体外系症状（EPS）。
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公开(公告)号：US07482465B2
公开(公告)日：2009-01-27
申请号：US10538639
申请日：2003-11-17
申请人： Günter Hölzemann , Helene Crassier , Henning Böttcher , Timo Heinrich , Kai Schiemann , Joachim Leibrock , Chrisoph Van Amsterdam , Gerd Bartoszyk , Christoph Seyfried
发明人： Günter Hölzemann , Helene Crassier , Henning Böttcher , Timo Heinrich , Kai Schiemann , Joachim Leibrock , Chrisoph Van Amsterdam , Gerd Bartoszyk , Christoph Seyfried
IPC分类号： C07D271/12 , C07D285/10
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：US20060229339A1
公开(公告)日：2006-10-12
申请号：US10489960
申请日：2002-08-12
申请人： Henning Böttcher , Ralf Devant , Maria Devant , Gerd Bartoszyk , Hermann Russ , Frank Weber , Christoph Seyfried
发明人： Henning Böttcher , Ralf Devant , Maria Devant , Gerd Bartoszyk , Hermann Russ , Frank Weber , Christoph Seyfried
IPC分类号： A61K31/4433
CPC分类号： C07D405/12
摘要： Compounds of formula I in which R has a meaning as indicated in claim 1, or one of their optical isomers or pharmaceutically acceptable salts, used for the treatment of extrapyramidal movement disorders and/or adverse effects in extrapyramidal movement disorders and/or for the treatment of extrapyramidal symptoms (EPS) induced by neuroleptics.
摘要翻译： 其中R具有权利要求1所述含义的式I化合物或其用于治疗锥体束外运动障碍和/或锥体外系运动障碍和/或治疗中的副作用的其旋光异构体或药学上可接受的盐之一 的精神分裂症引起的锥体外系症状（EPS）。
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公开(公告)号：US06462056B1
公开(公告)日：2002-10-08
申请号：US09380202
申请日：1999-08-25
IPC分类号： A61K31454
CPC分类号： C07D413/14
摘要： The invention relates to novel oxazolidine derivatives of the formula in which R1, R2 and R3 have the meanings stated in claim 1, their salts and processes for preparing the compounds according to the invention. The compounds of the formula I act as 5-HT2A antagonists with a 5-HT reuptake-inhibiting, antidepressant or anxiolytic effect and can be used to produce pharmaceuticals.
摘要翻译： 本发明涉及式（1）的新的恶唑烷衍生物，其中R1，R2和R3具有权利要求1所述的含义，其盐和制备本发明化合物的方法。式I化合物作为5-HT2A拮抗剂， 5-HT再摄取抑制，抗抑郁或抗焦虑作用，可用于生产药物。
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公开(公告)号：US06441013B1
公开(公告)日：2002-08-27
申请号：US09868097
申请日：2001-06-14
IPC分类号： A61K3142
CPC分类号： C07D263/48
摘要： The present invention relates to sulphonylexazolamines of general formula (I), wherein R1, R2 represent independently from each other H, A, —(CH2)n—Ar or alkenyl with 2-6 C atoms, R1 and R2 together also represent a mononuclear saturated heterocycle with 1-2 N, O and/or S atoms, Z is H, A, CF3, NO2, Hal, OH, OA, NH2, NHA or NH2. A represents alkyl with 1-6 C atoms, Ar is Z-monosubstituted or Z-disubstituted phenyl, Hal is F, Cl, Br, or L n is 1 or 2 of the physiologically acceptable salts or solvates thereof. Said sulphonyloxazolamines are used as therapeutic active ingredients. The invention also relates to the use of sulphonyloxazolamines as therapeutic active ingredients and/or to the production of pharmaceutical preparations to combat diseases of the central nervous system. The invention further relates to a pharmaceutical preparation and the production thereof.
摘要翻译： 本发明涉及通式（I）的磺酰基唑胺，其中R 1，R 2彼此独立地表示H，A， - （CH 2）n -Ar或具有2-6个C原子的烯基，R 1和R 2一起也表示单核 具有1-2个N，O和/或S原子的饱和杂环，Z是H，A，CF 3，NO 2，Hal，OH，OA，NH 2，NHA或NH 2。 A表示具有1-6个C原子的烷基，Ar是Z-单取代或Z-二取代的苯基，Hal是F，Cl，Br或L n是其生理上可接受的盐或溶剂化物的1或2。 所述磺酰基恶唑胺用作治疗活性成分。 本发明还涉及磺酰氯唑胺作为治疗活性成分和/或用于制备用于对抗中枢神经系统疾病的药物制剂的用途。 本发明还涉及药物制剂及其制备。
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