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公开(公告)号：US20060264419A1
公开(公告)日：2006-11-23
申请号：US10552065
申请日：2004-03-08
申请人： Kai Schiemann , Karl-August Ackermann , Michael Arlt , Dirk Finsinger , Christoph Van Amsterdam , Gerd Bartoszyk , Christoph Seyfried , Oliver Schadt
发明人： Kai Schiemann , Karl-August Ackermann , Michael Arlt , Dirk Finsinger , Christoph Van Amsterdam , Gerd Bartoszyk , Christoph Seyfried , Oliver Schadt
IPC分类号： A61K31/551 , A61K31/5377 , A61K31/496 , A61K31/4439 , A61K31/416
CPC分类号： C07D231/12 , A61K31/415 , C07D231/14 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/14 , C07D403/06 , C07D403/10 , C07D403/12 , C07D403/14 , C07D405/04 , C07D409/06 , C07D409/10 , C07D413/12 , C07D451/06 , C07D453/06 , C07D471/04 , C07D471/10 , C07D487/08 , C07D491/08
摘要： The compounds of the formula (I) and salts and solvates thereof, in which X, R1, R2, R3, R4 and R5 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 3， SUP> 4和R 5具有权利要求（1）所示的含义，适合作为5HT受体的配体。
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公开(公告)号：US07842695B2
公开(公告)日：2010-11-30
申请号：US10552064
申请日：2004-03-10
申请人： Oliver Schadt , Michael Arlt , Dirk Finsinger , Kai Schiemann , Christoph Van Amsterdam , Gerd Bartoszyk , Christoph Seyfried
发明人： Oliver Schadt , Michael Arlt , Dirk Finsinger , Kai Schiemann , Christoph Van Amsterdam , Gerd Bartoszyk , Christoph Seyfried
IPC分类号： A61K31/497 , A61K31/435 , A01N43/40 , C07D403/00 , C07D405/00 , C07D409/00
CPC分类号： C07D231/12 , C07D231/40 , C07D401/04 , C07D401/14 , C07D403/04 , C07D405/04 , C07D405/10 , C07D405/14 , C07D409/10 , C07D409/14 , C07D413/04 , C07D413/14
摘要： Compounds of formula (I) and salts thereof, in which the following definitions apply: X is N or CH; R1 is H, A, Hal, (CH2)nHet, (CH2)nAr, C3-7-cycloalkyl, CF3, NO2, CN, C(NH)(OH), or OCF3; R2 is (CH2)nHet, (CH2)nAr, or C3-7-cycloalkyl, or CF3; R3 and R4 denote H or an organic radical. Compounds of formula (I) are useful as ligands of 5-HT receptors and useful in the treatment of disorders such as anxiety, depression, obsessive-compulsive disorder and pain.
摘要翻译： 式（I）化合物及其盐，其中适用以下定义：X为N或CH; R1是H，A，Hal，（CH2）nHet，（CH2）nAr，C3-7-环烷基，CF3，NO2，CN，C（NH）（OH）或OCF3; R2是（CH2）nHet，（CH2）nAr或C3-7-环烷基或CF3; R3和R4表示H或有机基团。 式（I）化合物可用作5-HT受体的配体，可用于治疗焦虑，抑郁，强迫症和疼痛等疾病。
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公开(公告)号：US20070010531A1
公开(公告)日：2007-01-11
申请号：US10552064
申请日：2004-03-10
申请人： Oliver Schadt , Michael Arlt , Dirk Finsinger , Kai Schiemann , Christoph Van Amsterdam , Gerd Bartoszyk , Christoph Seyfried
发明人： Oliver Schadt , Michael Arlt , Dirk Finsinger , Kai Schiemann , Christoph Van Amsterdam , Gerd Bartoszyk , Christoph Seyfried
IPC分类号： A61K31/497 , A61K31/4439 , A61K31/416 , C07D403/02
CPC分类号： C07D231/12 , C07D231/40 , C07D401/04 , C07D401/14 , C07D403/04 , C07D405/04 , C07D405/10 , C07D405/14 , C07D409/10 , C07D409/14 , C07D413/04 , C07D413/14
摘要： Compounds of the formula (I) and salts and solvates thereof, in which X, R1, R2, R3, and R5 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和R 3， SUP> 5具有权利要求1所示的含义，适合作为5个HT受体的配体。
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公开(公告)号：US20090291963A1
公开(公告)日：2009-11-26
申请号：US12511320
申请日：2009-07-29
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： A61K31/496 , C07D401/06 , A61K31/454 , C07D405/14 , C07D403/14 , C07D417/14 , C07D401/14 , C07D471/10 , A61K31/438 , A61P25/24 , A61P25/18 , A61P25/22 , A61P25/28 , A61P25/16 , A61P25/34 , A61P25/00 , A61P25/04
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，脑局部缺血，梗塞或精神病
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公开(公告)号：US07960413B2
公开(公告)日：2011-06-14
申请号：US10551905
申请日：2004-03-08
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。
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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。
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公开(公告)号：US20060276650A1
公开(公告)日：2006-12-07
申请号：US10551905
申请日：2004-03-08
IPC分类号： A61K31/496 , C07D403/14 , C07D403/04
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 SUP > 5，R 5和R 6具有权利要求1所示的含义，适合作为5个HT受体的配体。
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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：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。
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10.发明授权1,3,4-Substituted pyrazoles as 5-HT receptor antagonists for the treatment of psychoses and neurological disorders 失效1,3,4-取代的吡唑作为治疗精神病和神经障碍的5-HT受体拮抗剂公开(公告)号：US07566709B2
公开(公告)日：2009-07-28
申请号：US10551998
申请日：2004-03-08
IPC分类号： A61K31/4155 , A61K31/4025 , A61K31/5377 , A61K31/497 , C07D231/02 , C07D207/09 , C07D413/06 , C07D403/06
CPC分类号： C07D231/12 , C07D403/06 , C07D405/04 , C07D405/14 , C07D409/14
摘要： Compounds of the formula (I) and salts and solvates thereof, in which X, R1, R2, R5 and Q have the meanings indicated in Claim 1, are suitable as ligands of 5 HT receptors; as well as intermediate compounds of the formula (IA).
摘要翻译： 式（I）化合物及其盐和溶剂化物，其中X，R 1，R 2，R 5和Q具有权利要求1所示的含义，适合作为5HT受体的配体; 以及式（IA）的中间体化合物。
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