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71. 发明授权

US07960413B2 Pyrazole compounds 失效
标题翻译：吡唑化合物
公开(公告)号：US07960413B2
公开(公告)日：2011-06-14
申请号：US10551905
申请日：2004-03-08
申请人： Oliver Schadt , Kai Schiemann , Christoph Van Amsterdam , Gerd Bartoszyk , Christoph Seyfried
发明人： Oliver Schadt , Kai Schiemann , Christoph Van Amsterdam , Gerd Bartoszyk , Christoph Seyfried
IPC分类号： A61K31/44 , A61K31/40 , C07D401/00 , C07D231/10 , C07D231/12
CPC分类号： C07D231/12 , C07D403/06 , C07D405/04 , C07D405/14
摘要： Compounds of the formula (I) and salts and solvates thereof, in which X, R1, R2, R3, R4, R5 and R6 have the meanings indicated in Claim 1, are suitable as ligands of 5 HT receptors.
摘要翻译：式（I）化合物及其盐和溶剂合物，其中X，R 1，R 2，R 3，R 4，R 5和R 6具有权利要求1所示的含义，适合作为5HT受体的配体。

72. 发明授权

US07741343B2 6H-oxazolo[4,5 e]indole derivatives as nicotinic acetylcholine receptor ligands and/or serotonergic ligands 失效
标题翻译： 6H-恶唑并[4,5 e]吲哚衍生物作为烟碱乙酰胆碱受体配体和/或5-羟色胺能配体
公开(公告)号：US07741343B2
公开(公告)日：2010-06-22
申请号：US11928961
申请日：2007-10-30
申请人： Kai Schiemann , Henning Böttcher , Joachim Leibrock
发明人： Kai Schiemann , Henning Böttcher , Joachim Leibrock
IPC分类号： A61K31/424 , A61K31/5377 , C07D413/14 , C07D498/02
CPC分类号： C07D498/04 , C07D519/00
摘要： Compounds of the formula I in which R1, R2, R3 and R4 are as defined in Claim 1, are ligands of the nicotinic acetylcholine receptor and/or serotonergic ligands and are suitable for the prophylaxis or treatment of psychoses, schizophrenia, depression, anxiety states, dementia, in particular Alzheimer's disease and Lewy bodies dementia, neurodegenerative disorders, Parkinson's disease, amyotrophic lateral sclerosis, Huntington's disease, Tourette's syndrome, learning and memory restrictions, bulimia, anorexia nervosa or other eating disorders, compulsive behavior, premenstrual syndrome, age-induced memory impairment, amelioration of withdrawal symptoms in nicotine dependence, strokes or brain damage by toxic compounds, and for the treatment of disorders which are characterized by an excess of circulating serotonin or by serotonergic hyperactivity.
摘要翻译：其中R1，R2，R3和R4如权利要求1所定义的式I化合物是烟碱型乙酰胆碱受体和/或血清素能配体的配体，并且适用于预防或治疗精神病，精神分裂症，抑郁症，焦虑状态，痴呆症，特别是阿尔茨海默病和路易体痴呆，神经变性疾病，帕金森病，肌萎缩性侧索硬化，亨廷顿病，图雷特综合征，学习和记忆限制，贪食症，神经性厌食症或其他进食障碍，强迫行为，经前期综合征，诱发记忆障碍，改善尼古丁依赖戒断症状，中毒或脑损伤的毒性化合物，以及治疗以循环血清素过多或血清素过多为特征的疾病。

73. 发明授权

US07572796B2 Substituted indoles 失效
标题翻译：取代的吲哚
公开(公告)号：US07572796B2
公开(公告)日：2009-08-11
申请号：US10511155
申请日：2003-04-11
申请人： Oliver Schadt , Henning Böttcher , Joachim Leibrock , Kai Schiemann , Timo Heinrich , Günter Hölzemann , Christoph van Amsterdam , Gerd Bartoszyk , Christoph Seyfried
发明人： Oliver Schadt , Henning Böttcher , Joachim Leibrock , Kai Schiemann , Timo Heinrich , Günter Hölzemann , Christoph van Amsterdam , Gerd Bartoszyk , Christoph Seyfried
IPC分类号： A61K31/497 , C07D405/00
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：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，脑缺血，梗死或精神病。

74. 发明授权

US07432282B2 Pyridinalkyl-aminoalkyl-IH-indole derivatives having an inhibitory action on 5-HT and serotonin reuptake as antidepressants and anxiolytics 失效
标题翻译：具有抑制作用的5-二羟基烷基 - 氨基烷基-1H-吲哚衍生物作为抗抑郁药和抗焦虑药
公开(公告)号：US07432282B2
公开(公告)日：2008-10-07
申请号：US10535916
申请日：2003-10-30
申请人： Günter Hölzemann , Kai Schiemann , Timo Heinrich , Henning Böttcher , Joachim Leibrock , Christoph van Amsterdam , Gerd Bartoszyk , Christoph Seyfried
发明人： Günter Hölzemann , Kai Schiemann , Timo Heinrich , Henning Böttcher , Joachim Leibrock , Christoph van Amsterdam , Gerd Bartoszyk , Christoph Seyfried
IPC分类号： A61K31/4709 , A61K31/4439 , C07D215/12 , C07D401/12
CPC分类号： C07D401/12
摘要： Novel indole derivatives of the formula (I), in which X, Y, R1, R1′, m and n have the meanings indicated in Patent Claim 1, have a strong affinity to the 5-HT1A and in some cases to the 5-HT1D receptors. The compounds inhibit serotonin reuptake, exhibit serotonin-agonistic and -antagonistic properties and are suitable as antidepressants, anxiolytics and for the treatment of neurodegenerative diseases
摘要翻译：式（I）的新型吲哚衍生物，其中X，Y，R 1，R 1'，m和n具有专利权利要求1中所示的含义，具有对5-HT 1A受体具有强亲和力，在某些情况下与5-HT 1D 1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，并且适合作为抗抑郁药，抗焦虑药和用于治疗神经变性疾病

75. 发明授权

US07253202B2 Substituted benzodioxepines 失效
标题翻译：取代苯并二氧杂环庚烯
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

76. 发明申请

US20060142372A1 Benzofurane derivatives and the use the same as antidepressants and anxiolytics 失效
标题翻译：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。

77. 发明授权

US08754097B2 Piperidine and piperazine derivatives 有权
标题翻译：哌啶和哌嗪衍生物
公开(公告)号：US08754097B2
公开(公告)日：2014-06-17
申请号：US13591765
申请日：2012-08-22
申请人： Kai Schiemann , Melanie Schultz , Andree Blaukat , Ingo Kober
发明人： Kai Schiemann , Melanie Schultz , Andree Blaukat , Ingo Kober
IPC分类号： A61K31/454 , A61K31/438 , C07D498/10 , C07D471/10 , C07D413/06 , C07D413/14
CPC分类号： C07D263/58 , C07D209/34 , C07D235/26 , C07D249/18 , C07D277/68 , C07D413/12 , C07D417/12 , C07D471/10 , C07D491/10 , C07D498/10
摘要： Compounds of the formula (I), in which R1, R2, R3, D, G, Q and W have the meanings indicated in claim (1), can and be employed for the treatment of tumors.
摘要翻译：其中R1，R2，R3，D，G，Q和W具有权利要求（1）所示含义的式（I）化合物可用于治疗肿瘤。

78. 发明授权

US08058277B2 Substituted indoles 失效
标题翻译：取代的吲哚
公开(公告)号：US08058277B2
公开(公告)日：2011-11-15
申请号：US12245416
申请日：2008-10-03
申请人： Oliver Schadt , Henning Böttcher , Joachim Leibrock , Kai Schiemann , Timo Heinrich , Günter Hölzemann , Christoph van Amsterdam , Gerd Bartoszyk , Christoph Seyfried
发明人： Oliver Schadt , Henning Böttcher , Joachim Leibrock , Kai Schiemann , Timo Heinrich , Günter Hölzemann , Christoph van Amsterdam , Gerd Bartoszyk , Christoph Seyfried
IPC分类号： A61K31/497
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）的取代的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，脑缺血，梗死或精神病。

79. 发明授权

US07968551B2 Chromenoneindoles 失效
标题翻译：色酮酮
公开(公告)号：US07968551B2
公开(公告)日：2011-06-28
申请号：US10551997
申请日：2004-03-08
申请人： Kai Schiemann , Henning Böttcher , Timo Heinrich , Günter Hölzemann , Christoph Van Amsterdam , Gerd Bartoszyk , Joachim Leibrock , Christoph Seyfried
发明人： Kai Schiemann , Henning Böttcher , Timo Heinrich , Günter Hölzemann , Christoph Van Amsterdam , Gerd Bartoszyk , Joachim Leibrock , Christoph Seyfried
IPC分类号： A61K31/497 , C07D403/00
CPC分类号： C07D405/12
摘要： Chromenoneindole derivatives of the formula (I), in which R1, R2, R3, R, A and B are as defined in Claim 1, and pharmaceutically usable prodrugs, derivatives, solvates, stereoisomers and salts thereof, exhibit particular actions on the central nervous system, in particular 5-HT reuptake-inhibiting and 5-HTx-agonistic and/or -antagonistic actions. They are distinguished by particularly high bioavailability and particularly high inhibition of 5-HT reuptake.
摘要翻译：其中R1，R2，R3，R，A和B如权利要求1所定义的式（I）的色酮酮吲哚衍生物及其药学上可用的前药，衍生物，溶剂合物，立体异构体和盐在中枢神经中表现出特别的作用系统，特别是5-HT再摄取抑制和5-HTx-激动和/或拮抗作用。它们的特征在于特别高的生物利用度和特别高的5-HT再摄取抑制。

80. 发明申请

US20100222341A1 PIPERIDINE AND PIPERAZINE DERIVATIVES 有权
标题翻译：哌啶和哌嗪衍生物
公开(公告)号：US20100222341A1
公开(公告)日：2010-09-02
申请号：US12681440
申请日：2008-09-19
申请人： Kai Schiemann , Melanie Schultz , Andree Blaukat , Ingo Kober
发明人： Kai Schiemann , Melanie Schultz , Andree Blaukat , Ingo Kober
IPC分类号： A61K31/495 , C07D241/04 , C07D403/10 , C07D401/14 , C07D413/14 , A61K31/496 , A61K31/5377 , A61P35/00 , A61P35/02
CPC分类号： C07D263/58 , C07D209/34 , C07D235/26 , C07D249/18 , C07D277/68 , C07D413/12 , C07D417/12 , C07D471/10 , C07D491/10 , C07D498/10
摘要： Compounds of the formula (I), in which R1, R2, R3, D, G, Q and W have the meanings indicated in claim (1), can and be employed for the treatment of tumours.
摘要翻译：其中R1，R2，R3，D，G，Q和W具有权利要求（1）所示含义的式（I）化合物可用于治疗肿瘤。

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