N-(3-chloro-5-hydroxyphenyl)sulfonyl-N'-ethyl-2,3,8-triazaspiro[4.5]dec-3-ene-2-carboximidamide | 1187966-17-1

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 氮杂螺癸烷衍生物
• 英文名称: N-(3-chloro-5-hydroxyphenyl)sulfonyl-N'-ethyl-2,3,8-triazaspiro[4.5]dec-3-ene-2-carboximidamide
• CAS: 1187966-17-1
• 化学式: C₁₆H₂₂ClN₅O₃S
• 分子量: 399.901
• InChiKey: BAVBRRMADIQCMG-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.8
• 重原子数：
  26
• 可旋转键数：
  5
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  115
• 氢给体数：
  3
• 氢受体数：
  6

文献信息

• ARYLSULFONYL PYRAZOLINE CARBOXAMIDINE DERIVATIVES AS 5-HT6 ANTAGONISTS
  申请人：Loevezijn Arnold Van

  公开号：US20110046171A1

  公开（公告）日：2011-02-24

  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.

  本发明涉及芳基磺酰基吡唑啉羧酰胺衍生物，其作为5-ht6受体拮抗剂，以及用于制备这些化合物的方法和有用于它们的合成的新型中间体。该发明还涉及这些化合物和组合物的用途，特别是它们用于给患者治疗帕金森病、亨廷顿病、精神分裂症、焦虑症、抑郁症、躁郁症、精神病、癫痫、强迫症、情绪障碍、偏头痛、阿尔茨海默病、年龄相关的认知下降、轻度认知障碍、睡眠障碍、进食障碍、厌食症、贪食症、暴食症、惊恐发作、不安静脚症候群、注意力缺陷多动障碍、注意力缺陷障碍、戒断可卡因、乙醇、尼古丁或苯二氮平的滥用、疼痛、与脊髓创伤或头部损伤有关的疾病、脑积水、功能性肠道紊乱、肠易激综合征、肥胖症和2型糖尿病。这些化合物具有通式（1），其中符号的含义如描述中所给。
• ARYLSULFONYL PYRAZOLINE CARBOXAMIDINE DERIVATIVES AS 5-HT6 ANTAGONISTS
  申请人：AbbVie Bahamas Limited

  公开号：US20150051239A1

  公开（公告）日：2015-02-19

  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.

  本发明涉及苯磺酰基吡唑啉羧酰胺衍生物作为5-ht6受体拮抗剂，以及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成物的用途，特别是将它们用于治疗帕金森病、亨廷顿舞蹈症、精神分裂症、焦虑症、抑郁症、躁郁症、精神病、癫痫、强迫症、情感障碍、偏头痛、阿尔茨海默病、与年龄相关的认知下降、轻度认知障碍、睡眠障碍、进食障碍、厌食症、贪食症、暴食症、惊恐发作、不安静脚症候群、注意力缺陷多动障碍、注意力缺陷障碍、戒断可卡因、乙醇、尼古丁或苯二氮卓类药物的滥用、疼痛、与脊髓损伤或头部损伤相关的疾病、脑积水、功能性肠道紊乱、肠易激综合征、肥胖症和2型糖尿病等方面。这些化合物具有通式（1），其中符号的含义在说明中给出。
• Arylsulfonyl pyrazoline carboxamidine derivatives as 5-HT6 antagonists
  申请人：Abbott Healthcare Products B.V.

  公开号：EP2610247A1

  公开（公告）日：2013-07-03

  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.

  本发明涉及作为 5-HT6 受体拮抗剂的芳基磺酰基吡唑啉羧脒衍生物、制备这些化合物的方法以及用于合成这些化合物的新型中间体。睡眠障碍、饮食失调、厌食症、贪食症、暴饮暴食症、惊恐发作、肌痉挛、注意力缺陷多动障碍、注意力缺陷障碍、滥用可卡因、乙醇、尼古丁或苯二氮卓的戒断、疼痛、与脊柱创伤或头部损伤有关的失调、脑积水、功能性肠病、肠易激综合征、肥胖症和 2 型糖尿病。这些化合物的通式为 (1)： 其中符号的含义见说明。
• US8563723B2
  申请人：——

  公开号：US8563723B2

  公开（公告）日：2013-10-22
• US8901108B2
  申请人：——

  公开号：US8901108B2

  公开（公告）日：2014-12-02