2-(2,4-dichlorophenyl)-5,6,6b,7,8,9,10,10a-octahydro-4-oxa-3,6a,9-triaza-fluoranthene | 514787-11-2

• 分子结构分类: 有机化合物 - 有机杂环化合物
• 英文名称: 2-(2,4-dichlorophenyl)-5,6,6b,7,8,9,10,10a-octahydro-4-oxa-3,6a,9-triaza-fluoranthene
• 英文别名: 7-(2,4-Dichlorophenyl)-4-oxa-1,6,12-triazatetracyclo[7.6.1.05,16.010,15]hexadeca-5(16),6,8-triene
• CAS: 514787-11-2
• 化学式: C₁₈H₁₇Cl₂N₃O
• 分子量: 362.258
• InChiKey: DYUXHGLOHHQSDJ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.6
• 重原子数：
  24
• 可旋转键数：
  1
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.39
• 拓扑面积：
  37.4
• 氢给体数：
  1
• 氢受体数：
  4

文献信息

• Fused heterocyclic compound and use thereof
  申请人：Shirai Junya

  公开号：US20090131402A1

  公开（公告）日：2009-05-21

  The present invention relates to a serotonin 5-HT 2C receptor activator containing a compound represented by the formula wherein ring A is a 5- or 6-membered aromatic heterocycle optionally having substituent(s), and ring B is a 7- to 9-membered ring optionally having substituent(s) other than an oxo group wherein the combination of m and n (m,n) is (1,2), (2,1), (2,2), (3,1), (3,2) or (4,1), or a salt thereof or a prodrug thereof, and a fused heterocyclic compound having a serotonin 5-HT 2C receptor activating action and the like.

  本发明涉及一种含有化合物的5-羟色胺5-HT2C受体激动剂，所述化合物的结构式为：其中，环A是一种5-或6-成员的芳香杂环，可选地具有取代基；环B是一种7-至9-成员的环，可选地具有除氧基以外的取代基，其中m和n（m，n）的组合为（1，2）、（2，1）、（2，2）、（3，1）、（3，2）或（4，1），或其盐或前药，以及具有5-羟色胺5-HT2C受体激活作用等的融合杂环化合物。
• FUSED HETEROCYCLIC COMPOUND AND USE THEREOF
  申请人：SHIRAI Junya

  公开号：US20120165312A1

  公开（公告）日：2012-06-28

  The present invention relates to a serotonin 5-HT 2C receptor activator containing a compound represented by the formula wherein ring A is a 5- or 6-membered aromatic heterocycle optionally having substituent(s), and ring B is a 7- to 9-membered ring optionally having substituent(s) other than an oxo group wherein the combination of m and n (m,n) is (1,2), (2,1), (2,2), (3,1), (3,2) or (4,1), or a salt thereof or a prodrug thereof, and a fused heterocyclic compound having a serotonin 5-HT 2C receptor activating action and the like.

  本发明涉及一种含有由以下式表示的化合物的血清素5-HT2C受体激动剂： 其中环A是一种5-或6-成员芳香杂环，可选地具有取代基，环B是一种7-至9-成员环，除了一个氧代基外还可选地具有取代基，其中m和n（m，n）的组合为（1，2），（2，1），（2，2），（3，1），（3，2）或（4，1），或其盐或前药，以及具有血清素5-HT2C受体激活作用的融合杂环化合物等。
• PREVENTIVES/REMEDIES FOR STRESS URINARY INCONTINENCE AND METHOD OF SCREENING THE SAME
  申请人：Takeda Pharmaceutical Company Limited

  公开号：EP1792629A1

  公开（公告）日：2007-06-06

  An agent for the prophylaxis or treatment of stress urinary incontinence, which contains a substance that activates a serotonin 5-HT2C receptor, an agent for the prophylaxis or treatment of stress urinary incontinence, which contains a substance that stimulates an androgen binding site, and a method of screening for a drug for the prophylaxis or treatment of abdominal pressure incontinence, which includes electrostimulating the abdominal muscles or a nerve controlling them of an animal to increase the abdominal pressure, and measuring the leak point pressure at that time.

  一种预防或治疗压力性尿失禁的药物，其中含有一种能激活5-羟色胺5-HT2C受体的物质；一种预防或治疗压力性尿失禁的药物，其中含有一种能刺激雄激素结合位点的物质、以及一种筛选预防或治疗腹压性尿失禁药物的方法，其中包括电刺激动物的腹部肌肉或控制腹部肌肉的神经以增加腹压，并测量当时的漏点压力。
• CONDENSED PYRIDINE DERIVATIVE AND USE THEREOF
  申请人：Takeda Pharmaceutical Company Limited

  公开号：EP2216023A1

  公开（公告）日：2010-08-11

  Provided are a condensed pyridine derivative having a serotonin 5-HT2C receptor activation action, a prophylactic or therapeutic agent for a lower urinary tract symptom, obesity and/or organ prolapse and the like containing the condensed pyridine derivative, a screening method for a substance that increases leak point pressure upon a rise in the intravesical pressure or a prophylactic or therapeutic drug for stress urinary incontinence, a prophylactic or therapeutic drug for cystoceles or enteroceles, containing a substance that activates serotonin 5-HT2C receptor, and a method of screening for a therapeutic drug for cystoceles or enteroceles, including increasing an intravesical pressure after bilateral transection of the hypogastric nerve and pudendal nerve of an animal, and measuring a closure response in the urethra, the rectum or the vagina observed at that time. A serotonin 5-HT2C receptor activator containing a compound represented by the formula: wherein each symbol is as defined in the specification, or a salt thereof.

  提供了一种具有激活5-羟色胺5-HT2C受体作用的缩合吡啶衍生物，一种含有该缩合吡啶衍生物的下尿路症状、肥胖和/或器官脱垂等的预防或治疗药物，一种在膀胱内压升高时增加漏点压力的物质的筛选方法，或一种压力性尿失禁的预防或治疗药物、一种预防或治疗膀胱阴道炎或肠阴道炎的药物，含有一种激活5-羟色胺5-HT2C受体的物质，以及一种筛选膀胱阴道炎或肠阴道炎治疗药物的方法，包括在双侧横断动物的胃下神经和阴部神经后增加膀胱内压，并测量当时观察到的尿道、直肠或阴道的闭合反应。一种血清素 5-HT2C 受体激活剂，含有由式表示的化合物： 其中各符号如说明书中所定义，或其盐。
• Preventives/remedies for stress urinary incontinence and method of screening the same
  申请人：Takeda Pharmaceutical Company Limited

  公开号：EP2248524A2

  公开（公告）日：2010-11-10

  APD-356 for use as an agent for the prophylaxis or treatment of stress urinary incontinence.

  APD-356 用于预防或治疗压力性尿失禁。