5-(2,6-difluorophenyl)-10a-ethyl-1,2,6b,7,8,9,10,10a-octahydropyrido[4,3-b][1,4]thiazino[2,3,4-hi]indole | 497956-01-1

• 分子结构分类: 有机化合物 - 有机杂环化合物
• 英文名称: 5-(2,6-difluorophenyl)-10a-ethyl-1,2,6b,7,8,9,10,10a-octahydropyrido[4,3-b][1,4]thiazino[2,3,4-hi]indole
• 英文别名: 7-(2,6-Difluorophenyl)-15-ethyl-4-thia-1,12-diazatetracyclo[7.6.1.05,16.010,15]hexadeca-5,7,9(16)-triene
• CAS: 497956-01-1
• 化学式: C₂₁H₂₂F₂N₂S
• 分子量: 372.482
• InChiKey: IVIQMJBLNBZXPH-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.5
• 重原子数：
  26
• 可旋转键数：
  2
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.43
• 拓扑面积：
  40.6
• 氢给体数：
  1
• 氢受体数：
  5

文献信息

• Therapeutic 5-HT ligand compounds
  申请人：——

  公开号：US20030050300A1

  公开（公告）日：2003-03-13

  The present invention provides compounds of Formula (I): 1 wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , and R 8 have any of the values defined in the specification, as well as pharmaceutical compositions comprising the compounds. The invention also provides therapeutic methods as well as processes and intermediates useful for preparing compounds of Formula (I). The compounds are 5-HT ligands, and are useful for treating diseases whereas modulation of 5-HT activity is desired.

  本发明提供了化合物的公式（I）：1，其中R1，R2，R3，R4，R5，R6，R7和R8具有规范中定义的任何值，以及包含该化合物的制药组合物。本发明还提供了治疗方法以及用于制备公式（I）化合物的过程和中间体。这些化合物是5-HT配体，并且对于治疗需要调节5-HT活性的疾病是有用的。
• 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。
• TREATMENT OF INCONTINENCE WITH 5HTC2 AGONISTS
  申请人：Pfizer Limited

  公开号：EP1620081A2

  公开（公告）日：2006-02-01
• Treatment of Incontinence
  申请人：McMurray Gordon

  公开号：US20080146583A1

  公开（公告）日：2008-06-19

  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.