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公开(公告)号：US20050096330A1
公开(公告)日：2005-05-05
申请号：US11013908
申请日：2004-12-17
申请人： Henning Boettcher , Hartmut Greiner , Juergen Harting , Gerd Bartoszyk , Christoph Seyfried , Christoph van Amsterdam
发明人： Henning Boettcher , Hartmut Greiner , Juergen Harting , Gerd Bartoszyk , Christoph Seyfried , Christoph van Amsterdam
IPC分类号： C07D403/06 , A61K31/496 , A61P3/04 , A61P21/02 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , C07D209/04 , C07D209/08 , C07D209/12 , C07D209/38 , C07D209/40 , C07D209/42 , C07D209/82 , C07D295/04 , C07D409/12 , C07D43/02
CPC分类号： C07D409/12 , C07D209/08
摘要： The invention relates to compounds of formula (I) wherein R1, R2, R4 and R5 have the meaning given in Claim 1. Said compounds are potent 5-HT2A-antagonists and are suitable for the treatment of psychosis, schizophrenia, depression, neurological disorders, memory disorders. Parkinson's disease, amyntrophic lateral schlerosis, Alzheimer's disease, Huntington's disease, eating disorders, e.g. nervous bulimia and anorexia and premenstrual syndrome and/or for positively influencing compulsive behaviours (obsessive-compulsive disorder, OCD).
摘要翻译： 本发明涉及式（I）的化合物，其中R 1，R 2，R 4和R 5， 具有权利要求1中给出的含义。所述化合物是有效的5-HT 2A拮抗剂，适用于治疗精神病，精神分裂症，抑郁症，神经障碍，记忆障碍。 帕金森氏病，融合性侧脑硬化，阿尔茨海默氏病，亨廷顿病，进食障碍等。 紧张性贪食症和厌食症和经前期综合征和/或积极影响强迫性行为（强迫症，强迫症）。
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公开(公告)号：US20060167078A1
公开(公告)日：2006-07-27
申请号：US10539515
申请日：2003-11-27
申请人： Timo Heinrich , Henning Boettcher , Kai Schiemann , Geunter Holzemann , Christoph van Amsterdam , Gerd Bartoszyk , Hartmut Greiner , Christoph Seyfried , Michel Brunet , Jean Zeiller , Jean Berthelon
发明人： Timo Heinrich , Henning Boettcher , Kai Schiemann , Geunter Holzemann , Christoph van Amsterdam , Gerd Bartoszyk , Hartmut Greiner , Christoph Seyfried , Michel Brunet , Jean Zeiller , Jean Berthelon
IPC分类号： A61K31/405 , C07D407/02
CPC分类号： C07D405/12
摘要： Benzodioxepines of the formula (I) and physiologically tolerated salts and solvates thereof, in which R1, R2, R3, R4, A, B, a and b have the meanings indicated in claim 1, are ligands of the 5HT1A receptors and/or the 5HT4 receptors with simultaneously strong serotonin reuptake inhibition. They can be employed for the treatment and prophylaxis of various diseases.
摘要翻译： 式（I）的苯并二氧杂环庚烷及其生理上耐受的盐和溶剂合物，其中R 1，R 2，R 3，R SUP > 4，A，B，a和b具有权利要求1中所示的含义，是具有同时强烈的5-羟色胺再摄取抑制的5HT1A受体和/或5HT4受体的配体。 可用于治疗和预防各种疾病。
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公开(公告)号：US07329749B2
公开(公告)日：2008-02-12
申请号：US10466487
申请日：2001-12-24
申请人： Henning Boettcher , Gerd Bartoszyk , Juergen Harting , Christoph van Amsterdam , Christoph Seyfried
发明人： Henning Boettcher , Gerd Bartoszyk , Juergen Harting , Christoph van Amsterdam , Christoph Seyfried
IPC分类号： A61K31/496 , C07D403/06
CPC分类号： C07D215/48 , A61K31/495 , C07D217/26
摘要： Compound of the formula (I) in which R1, R2 and alk are as defined in Claim 1, are potent 5-HT2A antagonist and are suitable for the treatment of psychoses, schizophrenia, depression, neurological disorders, memory disorders, Parkinson's disease, amyotrophic lateral sclerosis, Alzheimer's disease, Hutington's disease, eating disorders, such as bulimia, anorexia nervosa, premenstrual syndrome and/or for positively influencing obsessive-compulsive disorder (OCD).
摘要翻译： 其中R 1，R 2和R 2如权利要求1所定义的式（I）化合物是有效的5-HT 2A 2A 拮抗剂，适用于治疗精神病，精神分裂症，抑郁症，神经障碍，记忆障碍，帕金森病，肌萎缩性侧索硬化，阿尔茨海默氏病，Hutington氏病，进食障碍，贪食症，神经性厌食症，经前期综合征和/或正面 影响强迫症（OCD）。
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4.发明申请Combinations of Serotonin Reuptake Inhibitors and Imidazoline I 2 Agonists 审中-公开5-羟色胺再摄取抑制剂和咪唑啉I 2激动剂的组合公开(公告)号：US20080027140A1
公开(公告)日：2008-01-31
申请号：US10586457
申请日：2004-12-15
IPC分类号： A61K31/135 , A61P25/00
CPC分类号： A61K45/06 , A61K31/138 , A61K31/4178 , A61K2300/00
摘要： The present invention relates to combinations of serotonin reuptake inhibitors and imidazoline I2 agonists as separate chemical units or both properties combined in a single molecule and to the use thereof for the preparation of medicaments for the treatment of depression, obsessive-compulsive disorders (OCDs), obsessive-compulsive spectrum disorders (OCSDs) and other anxiety states.
摘要翻译： 本发明涉及作为分开的化学单元的5-羟色胺再摄取抑制剂和咪唑啉I 2激动剂的组合，或者在单个分子中组合的两种性质以及用于制备用于治疗抑郁症的药物的用途， 强迫症（强迫症），强迫症频谱障碍（OCSD）和其他焦虑症状。
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公开(公告)号：US20050153980A1
公开(公告)日：2005-07-14
申请号：US10511155
申请日：2003-04-11
申请人： Oliver Schadt , Henning Boettcher , Joachim Leibrock , Kai Schiemann , Timo Heinrich , Gunter Hoelzemann , Christoph van Amsterdam , Gerd Bartoszyk , Christoph Seyfried
发明人： Oliver Schadt , Henning Boettcher , Joachim Leibrock , Kai Schiemann , Timo Heinrich , Gunter Hoelzemann , Christoph van Amsterdam , Gerd Bartoszyk , Christoph Seyfried
IPC分类号： A61K31/404 , A61K31/454 , A61K31/496 , A61P1/04 , A61P3/00 , A61P3/04 , A61P9/00 , A61P9/10 , A61P9/12 , A61P15/08 , A61P21/04 , A61P25/02 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P43/00 , C07D209/42 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D417/12 , C07D417/14 , C07D471/04 , C07D471/10 , C07D521/00 , C07D43/02
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, anxiolytics 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： 式（I）的取代吲哚及其生理上可接受的衍生物和盐，其中R 1，D，E，R 12，p，X 1， E，G，X 2和Z如权利要求1中所定义，表现出对中枢神经系统的特别作用，特别是5HT再摄取抑制和5 HTx激动和/或拮抗作用 动作，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：US06756370B1
公开(公告)日：2004-06-29
申请号：US10069054
申请日：2002-02-21
申请人： Helmut Prücher , Henning Böttcher , Karl-August Ackermann , Rudolf Gottschlich , Christoph van Amsterdam , Christoph Seyfried , Jürgen Harting , Gerd Bartoszyk , Hartmut Greiner
发明人： Helmut Prücher , Henning Böttcher , Karl-August Ackermann , Rudolf Gottschlich , Christoph van Amsterdam , Christoph Seyfried , Jürgen Harting , Gerd Bartoszyk , Hartmut Greiner
IPC分类号： A61K3154
CPC分类号： C07D401/06 , C07D211/22 , C07D405/06 , C07D409/06 , C07D417/06
摘要： The invention relates to compounds of formula (I), wherein R1, R2 and A have the meanings given in claim 1, are potent 5-HT2A antagonists and are suitable for treating psychoses, schizophrenia, depression, neurological disorders, impaired memory, Parkinson's disease, amyotrophic lateral sclerosis, Alzheimer's disease, Huntington's disease, eating disorders such as bulimia and anorexia nervosa, Pre-Menstrual Syndrome and/or for positively influencing obsessive-compulsive disorders, (OCD).
摘要翻译： 本发明涉及式（I）化合物，其中R 1，R 2和A具有权利要求1中给出的含义，它们是有效的5-HT2A拮抗剂，适用于治疗精神病，精神分裂症，抑郁症，神经障碍 记忆障碍，帕金森病，肌萎缩性侧索硬化症，阿尔茨海默氏病，亨廷顿疾病，进食障碍如贪食症和神经性厌食症，前月经综合征和/或积极影响强迫症（OCD）。
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公开(公告)号：US20050026927A1
公开(公告)日：2005-02-03
申请号：US10495456
申请日：2002-10-14
IPC分类号： C07D231/12 , A61K31/454 , A61K31/4545 , A61K31/496 , A61K45/00 , A61P9/10 , A61P15/10 , A61P25/00 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P39/00 , A61P43/00 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/12 , C07D403/14 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/12 , C07D417/14 , C07D498/04 , C07D513/04 , C07
CPC分类号： C07D403/06 , C07D403/14 , C07D413/14 , C07D417/14
摘要： The invention relates to pyrazole derivatives of Formula (I), in which R?1, X, Z and n have the meanings indicated above, their preparation and their use as psychopharmaceuticals and/or as active compounds of medicaments for the treatment and prophylaxis of movement disorders and/or for the manufacture of a medicament for the treatment of adverse effects of anti-Parkinsonian drugs in extrapyramidal movement disorders and/or for the manufacture of a medicament for the treatment of extrapyramidal symptoms (EPS) induced by neuroleptics.
摘要翻译： 本发明涉及式（I）的吡唑衍生物，其中R 1 <定制字符文件=“US20050026927A1-20050203-P00900.TIF”wi =“20”he =“20”id =“custom-character-00001 “/>，X，Z和n具有上述含义，它们的制备及其作为精神药物和/或用作治疗和预防运动障碍的药物的活性化合物和/或用于制备治疗药物的用途 抗帕金森药物在锥体外系运动障碍中的不利影响和/或用于制备用于治疗由精神安定药诱发的锥体束外症状（EPS）的药物。
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公开(公告)号：US07253202B2
公开(公告)日：2007-08-07
申请号：US10539515
申请日：2003-11-27
申请人： Timo Heinrich , Henning Böttcher , Kai Schiemann , Günter Hölzemann , Christoph van Amsterdam , Gerd Bartoszyk , Hartmut Greiner , Christoph Seyfried , Michel Brunet , Jean Zeiller , Jean Berthelon
发明人： Timo Heinrich , Henning Böttcher , Kai Schiemann , Günter Hölzemann , Christoph van Amsterdam , Gerd Bartoszyk , Hartmut Greiner , Christoph Seyfried , Michel Brunet , Jean Zeiller , Jean Berthelon
IPC分类号： C07D405/12 , A61K31/357 , A61K31/404
CPC分类号： C07D405/12
摘要： Benzodioxepines of the formula (I) and physiologically tolerated salts and solvates thereof, in which R1, R2, R3, R4, A, B, a and b have the meanings indicated in claim 1, are ligands of the 5HT1A receptors and/or the 5HT4 receptors with simultaneously strong serotonin reuptake inhibition. They can be employed for the treatment and prophylaxis of various diseases
摘要翻译： 式（I）的苯并二氧杂环庚烷及其生理上耐受的盐和溶剂合物，其中R 1，R 2，R 3，R SUP > 4，A，B，a和b具有权利要求1中所示的含义，是具有同时强烈的5-羟色胺再摄取抑制的5HT1A受体和/或5HT4受体的配体。 可用于治疗和预防各种疾病
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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：US5242925A
公开(公告)日：1993-09-07
申请号：US933556
申请日：1992-08-24
IPC分类号： A61K31/495 , A61K31/357 , A61K31/496 , A61P9/02 , A61P9/08 , A61P9/10 , A61P9/12 , A61P25/00 , A61P25/04 , A61P25/20 , A61P25/24 , A61P25/26 , A61P25/28 , A61P35/00 , C07D405/04 , C07D405/12 , C07D405/14 , C07D453/02
CPC分类号： C07D405/12 , C07D405/14 , C07D453/02
摘要： Piperazinylbenzodioxane derivatives of formula I ##STR1## wherein B is an indol-3-yl or benzimidazol-1-yl radical which is unsubstituted or monosubstituted by CN, CO--R.sup.1, C.sub.n H.sub.2n --R.sup.1, Hal, OH, OA, O--C.sub.n H.sub.2n --CO--R.sup.1, or NHR.sup.2, and Q is C.sub.n H.sub.2n, or a physiologically acceptable salt thereof. The derivatives are active in the central nervous system, especially as serotonin agonists and antagonists.
摘要翻译： 式I的哌嗪基苯并二恶烷衍生物其中B是未被取代或被CN，CO-R 1，C n H 2n-R 1，Hal，OH，OA，O-C n H 2n的单取代的吲哚-3-基或苯并咪唑-1-基 -CO-R 1或NHR 2，Q为C n H 2n，或其生理上可接受的盐。 衍生物在中枢神经系统中是有活性的，特别是作为血清素激动剂和拮抗剂。
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