(S)-2-(6-bromo-2,3-dihydro-indol-1-yl)-1-methyl-ethylamine | 259857-99-3

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吲哚及其衍生物
• 英文名称: (S)-2-(6-bromo-2,3-dihydro-indol-1-yl)-1-methyl-ethylamine
• 英文别名: (S)-(6-bromoindolin-1-yl)-2-propylamine；(2S)-1-(6-bromo-2,3-dihydroindol-1-yl)propan-2-amine
• CAS: 259857-99-3
• 化学式: C₁₁H₁₅BrN₂
• 分子量: 255.157
• InChiKey: QGRQJMXAQYGAKK-QMMMGPOBSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.3
• 重原子数：
  14
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.45
• 拓扑面积：
  29.3
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为产物：
  描述：

  6-溴吲哚 在 盐酸 、 氢氧化钾 、 sodium cyanoborohydride 、 溶剂黄146 作用下， 以 1,4-二氧六环 、 甲醇 、 二氯甲烷 、 二甲基亚砜 为溶剂， 生成 (S)-2-(6-bromo-2,3-dihydro-indol-1-yl)-1-methyl-ethylamine
  参考文献：
  名称：

  Indoline derivatives as 5-HT 2C receptor agonists

  摘要：

  A series of 1-(1-indolinyl)-2-propylamines was synthesised and evaluated as 5-HT2C receptor agonists for the treatment of obesity. The general methods of synthesis of the precursor indoles are described. The functional efficacy and radioligand binding data for all of the compounds at 5-HT2 receptor subtypes are reported. A number of compounds were found to reduce food intake in rats after oral administration. (C) 2004 Published by Elsevier Ltd.

  DOI：

  10.1016/j.bmcl.2003.05.001

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。
• CONDENSED PYRIDINE DERIVATIVE AND USE THEREOF
  申请人：Matsumoto Takahiro

  公开号：US20100266504A1

  公开（公告）日：2010-10-21

  Provided are a condensed pyridine derivative having a serotonin 5-HT 2C 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-HT 2C 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-HT 2c receptor activator containing a compound represented by the formula: wherein each symbol is as defined in the specification, or a salt thereof.

  提供了一种具有血清素5-HT2C受体激活作用的缩合吡啶衍生物，以及包含该缩合吡啶衍生物的预防或治疗下尿路症状、肥胖和/或器官脱垂等药物，以及增加膀胱内压力时增加泄漏点压力或预防或治疗压力性尿失禁的药物筛选方法，包含激活血清素5-HT2C受体的物质的预防或治疗膀胱脱垂或肠脱垂的药物，以及通过双侧切断动物的会阴神经和耻骨神经后增加膀胱内压力并测量尿道、直肠或阴道在此时观察到的闭合反应的膀胱脱垂或肠脱垂的治疗药物筛选方法。其中包含式的化合物的血清素5-HT2C受体激活剂：式中每个符号如规范中定义的那样，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：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。
• Method of screening preventives/remedies for stress urinary incontinence
  申请人：Takeda Pharmaceutical Company Limited

  公开号：EP2400300A1

  公开（公告）日：2011-12-28

  The invention relates to a method of screening for a substance that increases the leak point pressure during increase in abdominal pressure and a method of screening for a drug for the prophylaxis or treatment of abdominal pressure incontinence.

  本发明涉及一种在腹压增加时增加漏点压力的物质的筛选方法，以及一种用于预防或治疗腹压失禁的药物的筛选方法。