公开(公告)号：US07964728B2

公开(公告)日：2011-06-21

申请号：US11773111

申请日：2007-07-03

申请人： Axel Stoit ,  Hein K. A. C. Coolen ,  Martina A. W. Van Der Neut ,  Cornelis G. Kruse

发明人： Axel Stoit ,  Hein K. A. C. Coolen ,  Martina A. W. Van Der Neut ,  Cornelis G. Kruse

IPC分类号： C07D471/02

CPC分类号： C07D471/04 ,  C07D519/00

摘要： Azaindole derivatives of formula (I): wherein the symbols have the meanings given in the specification, are described. These compounds have a combination of partial nicotinic acetylcholine receptor agonism and dopamine reuptake inhibition. The invention also relates to pharmaceutical compositions containing these compounds, to methods for preparing them, methods for preparing novel intermediates useful for their synthesis, methods for preparing compositions, and uses of such compounds and compositions, for example, their use in administering them to patients to achieve a therapeutic effect in disorders in which nicotinic receptors and/or dopamine transporters are involved, or that can be treated via manipulation of those receptors.

摘要翻译： 描述了式（I）的Azaindole衍生物：其中符号具有说明书中给出的含义。 这些化合物具有部分烟碱乙酰胆碱受体激动和多巴胺再摄取抑制的组合。 本发明还涉及含有这些化合物的药物组合物，其制备方法，制备用于其合成的新型中间体的方法，制备组合物的方法，以及这些化合物和组合物的用途，例如其用于给予患者的用途 以在涉及烟碱受体和/或多巴胺转运蛋白的病症中获得治疗效果，或者可以通过这些受体的操纵来治疗。

公开(公告)号：US08252930B2

公开(公告)日：2012-08-28

申请号：US12940271

申请日：2010-11-05

申请人： Axel Stoit ,  Hein K. A. C. Coolen ,  Martina A. W. Van Der Neut ,  Cornelis G. Kruse

发明人： Axel Stoit ,  Hein K. A. C. Coolen ,  Martina A. W. Van Der Neut ,  Cornelis G. Kruse

IPC分类号： C07D471/02

CPC分类号： C07D471/04 ,  C07D519/00

摘要： Azaindole derivatives of formula (I): wherein the symbols have the meanings given in the specification, are described. These compounds have a combination of partial nicotinic acetylcholine receptor agonism and dopamine reuptake inhibition. The invention also relates to pharmaceutical compositions containing these compounds, to methods for preparing them, methods for preparing novel intermediates useful for their synthesis, methods for preparing compositions, and uses of such compounds and compositions, for example, their use in administering them to patients to achieve a therapeutic effect in disorders in which nicotinic receptors and/or dopamine transporters are involved, or that can be treated via manipulation of those receptors.

摘要翻译： 描述了式（I）的Azaindole衍生物：其中符号具有说明书中给出的含义。 这些化合物具有部分烟碱乙酰胆碱受体激动和多巴胺再摄取抑制的组合。 本发明还涉及含有这些化合物的药物组合物，其制备方法，制备用于其合成的新型中间体的方法，制备组合物的方法，以及这些化合物和组合物的用途，例如其用于给予患者的用途 以在涉及烟碱受体和/或多巴胺转运蛋白的病症中获得治疗效果，或者可以通过这些受体的操纵来治疗。

公开(公告)号：US08563723B2

公开(公告)日：2013-10-22

申请号：US12933182

申请日：2009-03-17

申请人： Arnold Van Loevezijn ,  Wouter I. Iwema Bakker ,  Axel Stoit ,  Agatha A. M. Rensink ,  Jennifer Venhorst ,  Martina A. W. Van Der Neut ,  Martin De Haan ,  Cornelis G. Kruse

发明人： Arnold Van Loevezijn ,  Wouter I. Iwema Bakker ,  Axel Stoit ,  Agatha A. M. Rensink ,  Jennifer Venhorst ,  Martina A. W. Van Der Neut ,  Martin De Haan ,  Cornelis G. Kruse

IPC分类号： C07D231/06 ,  C07D231/54 ,  C07D403/12 ,  C07D471/10 ,  C07D491/10

CPC分类号： C07D231/06 ,  A61K31/415 ,  A61K31/4155 ,  A61K31/4162 ,  A61K31/435 ,  A61K31/635 ,  A61K45/06 ,  C07D231/00 ,  C07D231/54 ,  C07D403/12 ,  C07D471/10 ,  C07D491/10 ,  C07D491/107

摘要： This invention concerns arylsulfonyl pyrazoline carboxamidine derivatives as antagonists of 5-ht6 receptors, to methods for the preparation of these compounds and to novel intermediates useful for their synthesis. The invention also relates to the uses of such compounds and compositions, particularly their use in administering them to patients to achieve a therapeutic effect in parkinson's disease, huntington's chorea, schizophrenia, anxiety, depression, manic depression, psychoses, epilepsy, obsessive compulsive disorders, mood disorders, migraine, alzheimer's disease, age related cognitive decline, mild cognitive impairment, sleep disorders, eating disorders, anorexia, bulimia, binge eating disorders, panic attacks, akathisia, attention deficit hyperactivity disorder, attention deficit disorder, withdrawal from abuse of cocaine, ethanol, nicotine or benzodiazepines, pain, disorders associated with spinal trauma or head injury, hydrocephalus, functional bowel disorder, irritable bowel syndrome, obesity and type-2 diabetes. The compounds have the general formula (1) wherein the symbols have the meanings given in the description.

摘要翻译： 本发明涉及作为5-HT 6受体的拮抗剂的芳基磺酰基吡唑啉甲脒衍生物，制备这些化合物的方法和用于它们合成的新型中间体。 本发明还涉及这些化合物和组合物的用途，特别是它们在给予患者以在帕金森病，亨廷顿氏舞蹈症，精神分裂症，焦虑症，抑郁症，躁狂抑郁症，精神病，癫痫，强迫症中的治疗效果方面的用途， 情绪障碍，偏头痛，阿尔茨海默病，年龄相关认知衰退，轻度认知障碍，睡眠障碍，进食障碍，厌食症，贪食症，暴饮暴食症，惊恐发作，静坐不动，注意力缺陷多动障碍，注意力缺陷障碍，可卡因滥用 ，乙醇，尼古丁或苯并二氮杂，疼痛，与脊髓损伤或头部损伤相关的疾病，脑积水，功能性肠病，肠易激综合征，肥胖症和2型糖尿病。 化合物具有通式（1），其中符号具有说明书中给出的含义。

公开(公告)号：US20080009514A1

公开(公告)日：2008-01-10

申请号：US11773111

申请日：2007-07-03

申请人： Axel STOIT ,  Hein K.A.C. Coolen ,  Martina A. W. Van Der Neut ,  Cornelis G. Kruse

发明人： Axel STOIT ,  Hein K.A.C. Coolen ,  Martina A. W. Van Der Neut ,  Cornelis G. Kruse

IPC分类号： C07D471/04 ,  A61K31/437 ,  A61P1/00 ,  A61P25/00 ,  A61P37/00

CPC分类号： C07D471/04 ,  C07D519/00

摘要： Azaindole derivatives of formula (I): wherein the symbols have the meanings given in the specification, are described. These compounds have a combination of partial nicotinic acetylcholine receptor agonism and dopamine reuptake inhibition. The invention also relates to pharmaceutical compositions containing these compounds, to methods for preparing them, methods for preparing novel intermediates useful for their synthesis, methods for preparing compositions, and uses of such compounds and compositions, for example, their use in administering them to patients to achieve a therapeutic effect in disorders in which nicotinic receptors and/or dopamine transporters are involved, or that can be treated via manipulation of those receptors

摘要翻译： 描述了式（I）的Azaindole衍生物：其中符号具有说明书中给出的含义。 这些化合物具有部分烟碱乙酰胆碱受体激动和多巴胺再摄取抑制的组合。 本发明还涉及含有这些化合物的药物组合物，其制备方法，制备用于其合成的新型中间体的方法，制备组合物的方法，以及这些化合物和组合物的用途，例如其用于给予患者的用途 以在涉及烟碱受体和/或多巴胺转运蛋白的病症中获得治疗效果，或者可以通过操纵那些受体来治疗

公开(公告)号：US08722887B2

公开(公告)日：2014-05-13

申请号：US12706279

申请日：2010-02-16

申请人： Arnold Van Loevezijn ,  Wouter I. Iwema Bakker ,  Hiskias G. Keizer ,  Jan Zorgdrager ,  Martina A. W. Van Der Neut ,  Cornelis G. Kruse

发明人： Arnold Van Loevezijn ,  Wouter I. Iwema Bakker ,  Hiskias G. Keizer ,  Jan Zorgdrager ,  Martina A. W. Van Der Neut ,  Cornelis G. Kruse

IPC分类号： C07D231/06 ,  C07D401/12 ,  C07D403/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/10

CPC分类号： C07D513/04 ,  A61K9/0019 ,  A61K9/0031 ,  A61K9/1652 ,  A61K9/2054 ,  C07D231/06 ,  C07D231/12 ,  C07D231/54 ,  C07D231/56 ,  C07D401/04 ,  C07D401/12 ,  C07D403/12 ,  C07D405/04 ,  C07D405/10 ,  C07D405/12 ,  C07D409/04 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D471/04 ,  C07D471/10 ,  C07D491/10 ,  C07D491/107 ,  C07D519/00

摘要： This invention concerns compounds of the general formula (1): and derivatives thereof, which are antagonists of 5-HT6 receptors, wherein the symbols have the meanings given in the description. The invention also concerns methods for the preparation of these compounds, to novel intermediates useful for their synthesis, and to uses of such compounds and compositions, particularly their use in administering them to patients to achieve a therapeutic effect in treating at least on disease or condition chosen from Parkinson's disease, Huntington's chorea, schizophrenia, anxiety, depression, manic depression, psychoses, epilepsy, obsessive compulsive disorders, mood disorders, migraine, Alzheimer's disease, age related cognitive decline, mild cognitive impairment, sleep disorders, eating disorders, anorexia, bulimia, binge eating disorders, panic attacks, akathisia, attention deficit hyperactivity disorder, attention deficit disorder, withdrawal from abuse of cocaine, ethanol, nicotine or benzodiazepines, pain, disorders associated with spinal trauma or head injury, hydrocephalus, functional bowel disorder, Irritable Bowel Syndrome, obesity and type-2 diabetes.

摘要翻译： 本发明涉及作为5-HT 6受体的拮抗剂的通式（1）的化合物及其衍生物，其中符号具有说明书中给出的含义。 本发明还涉及制备这些化合物的方法，可用于其合成的新型中间体，以及这些化合物和组合物的用途，特别是它们在将它们给予患者以达到治疗至少在疾病或病症上的治疗效果 选自帕金森病，亨廷顿氏舞蹈病，精神分裂症，焦虑症，抑郁症，躁狂抑郁症，精神病，癫痫症，强迫症，情绪障碍，偏头痛，阿尔茨海默病，年龄相关认知衰退，轻度认知障碍，睡眠障碍，进食障碍，厌食症， 注意缺陷障碍，注意力缺陷障碍，可卡因滥用，乙醇，尼古丁或苯二氮卓类药物的疼痛，疼痛，与脊髓创伤或头部损伤相关的疾病，脑积水，功能性肠病，肠易激综合征 肠综合征，肥胖症和2型糖尿病。

公开(公告)号：US07728018B2

公开(公告)日：2010-06-01

申请号：US11859323

申请日：2007-09-21

申请人： Arnold Van Loevezijn ,  Wouter I. Iwema Bakker ,  Hiskias G. Keizer ,  Jan Zorgdrager ,  Martina A. W. Van Der Neut ,  Cornelis G. Kruse

发明人： Arnold Van Loevezijn ,  Wouter I. Iwema Bakker ,  Hiskias G. Keizer ,  Jan Zorgdrager ,  Martina A. W. Van Der Neut ,  Cornelis G. Kruse

IPC分类号： A61K31/4155 ,  C07D231/06 ,  C07D403/12 ,  C07D413/14 ,  C07D487/04

CPC分类号： C07D513/04 ,  A61K9/0019 ,  A61K9/0031 ,  A61K9/1652 ,  A61K9/2054 ,  C07D231/06 ,  C07D231/12 ,  C07D231/54 ,  C07D231/56 ,  C07D401/04 ,  C07D401/12 ,  C07D403/12 ,  C07D405/04 ,  C07D405/10 ,  C07D405/12 ,  C07D409/04 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D471/04 ,  C07D471/10 ,  C07D491/10 ,  C07D491/107 ,  C07D519/00

摘要： This invention concerns compounds of the general formula (1): and derivatives thereof, which are antagonists of 5-HT6 receptors, wherein the symbols have the meanings given in the description. The invention also concerns methods for the preparation of these compounds, to novel intermediates useful for their synthesis, and to uses of such compounds and compositions, particularly their use in administering them to patients to achieve a therapeutic effect in treating at least on disease or condition chosen from Parkinson's disease, Huntington's chorea, schizophrenia, anxiety, depression, manic depression, psychoses, epilepsy, obsessive compulsive disorders, mood disorders, migraine, Alzheimer's disease, age related cognitive decline, mild cognitive impairment, sleep disorders, eating disorders, anorexia, bulimia, binge eating disorders, panic attacks, akathisia, attention deficit hyperactivity disorder, attention deficit disorder, withdrawal from abuse of cocaine, ethanol, nicotine or benzodiazepines, pain, disorders associated with spinal trauma or head injury, hydrocephalus, functional bowel disorder, Irritable Bowel Syndrome, obesity and type-2 diabetes.

摘要翻译： 本发明涉及作为5-HT 6受体的拮抗剂的通式（1）的化合物及其衍生物，其中符号具有说明书中给出的含义。 本发明还涉及制备这些化合物的方法，可用于其合成的新型中间体，以及这些化合物和组合物的用途，特别是它们在将它们给予患者以达到治疗至少在疾病或病症上的治疗效果 选自帕金森病，亨廷顿氏舞蹈病，精神分裂症，焦虑症，抑郁症，躁狂抑郁症，精神病，癫痫症，强迫症，情绪障碍，偏头痛，阿尔茨海默病，年龄相关的认知衰退，轻度认知障碍，睡眠障碍，进食障碍，厌食症， 注意缺陷障碍，注意力缺陷障碍，可卡因滥用，乙醇，尼古丁或苯二氮卓类药物的疼痛，疼痛，与脊髓创伤或头部损伤相关的疾病，脑积水，功能性肠病，肠易激综合征 肠综合征，肥胖症和2型糖尿病。