tert-butyl 11-(furan-3-yl)-1-methyl-3,4,6,7,9,10-hexahydro-2H-pyrido[3,2-h][3]benzazepine-8-carboxylate | 1334435-12-9

• 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: tert-butyl 11-(furan-3-yl)-1-methyl-3,4,6,7,9,10-hexahydro-2H-pyrido[3,2-h][3]benzazepine-8-carboxylate
• CAS: 1334435-12-9
• 化学式: C₂₃H₃₀N₂O₃
• 分子量: 382.503
• InChiKey: FQSCAVXAAFXZHQ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.3
• 重原子数：
  28
• 可旋转键数：
  3
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.52
• 拓扑面积：
  45.9
• 氢给体数：
  0
• 氢受体数：
  4

文献信息

• Benzazepine Compound
  申请人：KOSHIO Hiroyuki

  公开号：US20110269744A1

  公开（公告）日：2011-11-03

  [Problem] Provided is a compound which is useful as an agent for treating or preventing 5-HT 2C receptor-related diseases, particularly incontinence such as stress urinary incontinence, urge urinary incontinence, mixed urinary incontinence, and the like, sexual dysfunction such as erectile dysfunction syndrome and the like, obesity, and the like. [Means for Solution] The present inventors have investigated compounds having a 5-HT 2C receptor agonist activity, which is promising as an active ingredient of a pharmaceutical composition for treating or preventing incontinence such as stress urinary incontinence, urge urinary incontinence, mixed urinary incontinence, and the like, sexual dysfunction such as erectile dysfunction syndrome and the like, obesity, and the like, and have found that the benzazepine compounds of the present invention have an excellent 5-HT 2C receptor agonist activity, thereby completing the present invention. That is, the benzazepine compounds of the present invention have a 5-HT 2C receptor agonist activity and can be used as an agent for treating or preventing 5-HT 2C receptor-related diseases, particularly incontinence such as stress urinary incontinence, urge urinary incontinence, mixed urinary incontinence, and the like, sexual dysfunction such as erectile dysfunction syndrome and the like, obesity, and the like.

  提供的是一种化合物，可用作治疗或预防与5-HT 2C 受体相关的疾病的药剂，特别是尿失禁，如压力性尿失禁、急迫性尿失禁、混合性尿失禁等，性功能障碍，如勃起功能障碍综合征等，肥胖等。 【解决方案】本发明者研究了具有5-HT 2C 受体激动剂活性的化合物，这种活性有望作为治疗或预防尿失禁，如压力性尿失禁、急迫性尿失禁、混合性尿失禁等，性功能障碍，如勃起功能障碍综合征等，肥胖等的药物组合物的有效成分。他们发现本发明的苯并环己酮类化合物具有出色的5-HT 2C 受体激动剂活性，从而完成了本发明。换句话说，本发明的苯并环己酮类化合物具有5-HT 2C 受体激动剂活性，可用作治疗或预防与5-HT 2C 受体相关的疾病的药剂，特别是尿失禁，如压力性尿失禁、急迫性尿失禁、混合性尿失禁等，性功能障碍，如勃起功能障碍综合征等，肥胖等。
• BENZAZEPINE COMPOUND
  申请人：KOSHIO Hiroyuki

  公开号：US20130059837A1

  公开（公告）日：2013-03-07

  Provided is a compound which is useful as an agent for treating or preventing 5-HT 2C receptor-related diseases, particularly incontinence such as stress urinary incontinence, urge urinary incontinence, mixed urinary incontinence, and the like, sexual dysfunction such as erectile dysfunction syndrome and the like, obesity, and the like. The present inventors have investigated compounds having a 5-HT 2C receptor agonist activity and have found that the benzazepine compounds of the present invention have an excellent 5-HT 2C receptor agonist activity, thereby completing the present invention. That is, the benzazepine compounds of the present invention have a 5-HT 2C receptor agonist activity and can be used as an agent for treating or preventing 5-HT 2C receptor-related diseases, particularly incontinence such as stress urinary incontinence, urge urinary incontinence, mixed urinary incontinence, and the like, sexual dysfunction such as erectile dysfunction syndrome and the like, obesity, and the like.

  提供的是一种化合物，其作为治疗或预防5-HT2C受体相关疾病的药剂特别是尿失禁，如压力性尿失禁、急迫性尿失禁、混合性尿失禁等，性功能障碍如勃起功能障碍综合症等，肥胖症等方面非常有用。本发明人研究了具有5-HT2C受体激动剂活性的化合物，并发现本发明的苯并氮杂环化合物具有出色的5-HT2C受体激动剂活性，从而完成了本发明。也就是说，本发明的苯并氮杂环化合物具有5-HT2C受体激动剂活性，可用作治疗或预防5-HT2C受体相关疾病的药剂，特别是尿失禁，如压力性尿失禁、急迫性尿失禁、混合性尿失禁等，性功能障碍如勃起功能障碍综合症等，肥胖症等方面。
• US9108977B2
  申请人：——

  公开号：US9108977B2

  公开（公告）日：2015-08-18
• US9598434B2
  申请人：——

  公开号：US9598434B2

  公开（公告）日：2017-03-21
• [EN] BENZAZEPINE COMPOUND<br/>[FR] COMPOSÉ DE BENZAZÉPINE
  申请人：ASTELLAS PHARMA INC

  公开号：WO2011111817A1

  公开（公告）日：2011-09-15

  【課題】5-HT2C受容体に関係する疾患、特に、腹圧性尿失禁、切迫性尿失禁、混合型尿失禁等の尿失禁、勃起不全症等の性機能障害、肥満等の治療又は予防剤として有用な化合物を提供する。 【解決手段】本発明者らは、腹圧性尿失禁、切迫性尿失禁、混合型尿失禁等の尿失禁、勃起不全症等の性機能障害、肥満等の治療又は予防用医薬組成物の有効成分として有望な、5-HT2C受容体アゴニスト作用を有する化合物について検討し、本発明のベンゾアゼピン化合物が優れた5-HT2C受容体アゴニスト作用を有することを確認し、本発明を完成した。即ち、本発明のベンゾアゼピン化合物は、5-HT2C受容体アゴニスト作用を有し、5-HT2C受容体に関係する疾患、特に、腹圧性尿失禁、切迫性尿失禁、混合型尿失禁等の尿失禁、勃起不全症等の性機能障害、肥満等の治療又は予防剤として使用できる。