(R)-4,6-dimethyl-1,2,3,4-tetrahydro-pyrazino[1,2-a]indole | 459816-14-9

• 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: (R)-4,6-dimethyl-1,2,3,4-tetrahydro-pyrazino[1,2-a]indole
• 英文别名: (4R)-4,6-dimethyl-1,2,3,4-tetrahydropyrazino[1,2-a]indole
• CAS: 459816-14-9
• 化学式: C₁₃H₁₆N₂
• 分子量: 200.283
• InChiKey: KYWYASJHTQNPQN-SNVBAGLBSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.9
• 重原子数：
  15
• 可旋转键数：
  0
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  17
• 氢给体数：
  1
• 氢受体数：
  1

反应信息

• 作为反应物：
  描述：

  (R)-4,6-dimethyl-1,2,3,4-tetrahydro-pyrazino[1,2-a]indole 在 sodium tetrahydroborate 、 三氟乙酸 作用下， 以 四氢呋喃 为溶剂， 生成 (4R,10aS)-4,6-Dimethyl-1,2,3,4,10,10a-hexahydro-pyrazino[1,2-a]indole 、 (4R,10AR)-4,6-Dimethyl-1,2,3,4,10,10a-hexahydro-pyrazino[1,2-a]indole
  参考文献：
  名称：

  Identification of 4-methyl-1,2,3,4,10,10a-hexahydropyrazino[1,2-a]indoles as 5-HT2C receptor agonists

  摘要：

  Synthesis and evaluation of the activity of new 4-methyl-1,2,3,4,10,10a-hexahydropyrazino[1,2-a]indoles as 5-HT2C receptor agonists are described. Appropriately substituted, several analogs displayed selectivity against the other 5-HT2 receptor subtypes of I order of magnitude or more. Selectivity was improved for several compounds versus the lead 1, increasing the therapeutic interest in this series of 5-HT2C receptor agonists. (c) 2005 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2005.05.074
• 作为产物：
  描述：

  (R)-1-(2-tert-butoxycarbonylamino-1-methyl-ethyl)-7-methyl-1H-indole-2-carboxylic acid ethyl ester 在 lithium aluminium tetrahydride 、 potassium carbonate 、 三氟乙酸 作用下， 以 甲醇 、 乙醚 、 二氯甲烷 为溶剂， 生成 (R)-4,6-dimethyl-1,2,3,4-tetrahydro-pyrazino[1,2-a]indole
  参考文献：
  名称：

  Identification of 4-methyl-1,2,3,4,10,10a-hexahydropyrazino[1,2-a]indoles as 5-HT2C receptor agonists

  摘要：

  Synthesis and evaluation of the activity of new 4-methyl-1,2,3,4,10,10a-hexahydropyrazino[1,2-a]indoles as 5-HT2C receptor agonists are described. Appropriately substituted, several analogs displayed selectivity against the other 5-HT2 receptor subtypes of I order of magnitude or more. Selectivity was improved for several compounds versus the lead 1, increasing the therapeutic interest in this series of 5-HT2C receptor agonists. (c) 2005 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2005.05.074

文献信息

• Piperazine derivatives
  申请人：——

  公开号：US20020169163A1

  公开（公告）日：2002-11-14

  Piperazine derivatives, as well as pharmaceutically acceptable salts, solvates and esters thereof, can be used in the form of pharmaceutical preparations for the treatment or prevention of disorders of the central nervous system, damage to the central nervous system, cardiovascular disorders, gastrointestinal disorders, diabetes insipidus, type II diabetes, obesity and sleep apnoea.

  哌嗪衍生物以及其中医药可接受的盐、溶剂合物和酯，可用于制药制剂的形式，用于治疗或预防中枢神经系统疾病、中枢神经系统损伤、心血管疾病、胃肠疾病、尿崩症、2型糖尿病、肥胖和睡眠呼吸暂停。
• Treatment of incontinence with 5htc2 agonists
  申请人：Pfizer Inc.

  公开号：EP2277513A2

  公开（公告）日：2011-01-26

  The present invention relates to the use of agonists of 5-HT2C receptors for the treatment of stress urinary incontinence. The present invention also relates to a method of treatment of stress urinary incontinence, to assays to screen for compounds useful in the treatment of stress urinary incontinence, and to methods of preparing compositions for the treatment of stress urinary incontinence.

  本发明涉及使用5-HT2C受体激动剂治疗压力性尿失禁。本发明还涉及一种治疗压力性尿失禁的方法，涉及筛选用于治疗压力性尿失禁的化合物的检测方法，以及涉及制备治疗压力性尿失禁的组合物的方法。
• Treatment of incontinence
  申请人：Pfizer Inc

  公开号：US20040235856A1

  公开（公告）日：2004-11-25

  The present invention relates to the use of agonists of 5-HT2C receptors for the treatment of urinary incontinence, preferably mixed incontinence or stress urinary incontinence. The invention also relates to the use of antagonists of 5-HT2C receptors for the treatment of urine retention. The present invention also relates to a method of treatment of incontinence, to assays to screen for compounds useful in the treatment of incontinence, and to methods of preparing compositions for the treatment of urinary incontinence.

  本发明涉及使用 5-HT2C 受体的激动剂治疗尿失禁，最好是混合性尿失禁或压力性尿失禁。本发明还涉及使用 5-HT2C 受体拮抗剂治疗尿潴留。本发明还涉及一种治疗尿失禁的方法，涉及筛选治疗尿失禁有用化合物的检测方法，以及制备治疗尿失禁组合物的方法。
• INTERHETEROARYL 7-OXABICYCLIC 2.2.1]HEPTANE OXAZOLES AS PROSTAGLANDIN F 2$g(a)? ANTAGONISTS
  申请人：Allergan, Inc.

  公开号：EP1317457A2

  公开（公告）日：2003-06-11
• TETRAHYDRO-PYRAZINO[1,2-A]INDOLES FOR THE TREATMENT OF CENTRAL NERVOUS DISORDERS
  申请人：F. Hoffmann-La Roche AG

  公开号：EP1370561B1

  公开（公告）日：2009-02-11