trans-8-chloro-1-(4-(phenoxy)cyclohexyl)-4H,6H-5-oxa-2,3,10b-triazabenzo[e]azulene | 1428523-49-2

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯二氮卓类
• 英文名称: trans-8-chloro-1-(4-(phenoxy)cyclohexyl)-4H,6H-5-oxa-2,3,10b-triazabenzo[e]azulene
• CAS: 1428523-49-2
• 化学式: C₂₂H₂₂ClN₃O₂
• 分子量: 395.889
• InChiKey: OHEWOQPIVCCPNY-RHDGDCLCSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.06
• 重原子数：
  28.0
• 可旋转键数：
  3.0
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.36
• 拓扑面积：
  49.17
• 氢给体数：
  0.0
• 氢受体数：
  5.0

文献信息

• [EN] OXY-CYCLOHEXYL-4H,6H-5-OXA-2,3,10B-TRIAZA-BENZO[E]AZULENES AS V1A ANTAGONISTS<br/>[FR] OXY-CYCLOHEXYL-4H,6H-5-OXA-2,3,10B-TRIAZA-BENZO[E]AZULÈNES EN TANT QU'ANTAGONISTES DE V1A
  申请人：HOFFMANN LA ROCHE

  公开号：WO2013045373A1

  公开（公告）日：2013-04-04

  The present invention provides 4H,6H-5-oxa-2,3,10b-triaza-benzo[e]azulenes, which act as V1a receptor modulators, and in particular as Via receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are useful as therapeutics acting peripherally and centrally in the conditions of dysmenorrhea, male or female sexual dysfunction, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephrotic syndrome, anxiety, depressive disorders, obsessive compulsive disorder, autistic spectrum disorders, schizophrenia, and aggressive behavior.

  本发明提供了4H,6H-5-氧杂-2,3,10b-三氮杂苯并[e]吖啶烯，其作为V1a受体调节剂，特别是作为V1a受体拮抗剂，以及它们的制备方法、含有它们的药物组合物和它们作为药物的用途。本发明的活性化合物在经前痛、男性或女性性功能障碍、高血压、慢性心力衰竭、抗利尿素分泌异常、肝硬化、肾病综合征、焦虑、抑郁障碍、强迫症、自闭症谱系障碍、精神分裂症和攻击性行为等情况中作为治疗药物具有作用，既可在外周起作用，也可在中枢起作用。
• OXY-CYCLOHEXYL-4H,6H-5-OXA-2,3,10B-TRIAZA-BENZO[E]AZULENES AS V1A ANTAGONISTS
  申请人：Dolente Cosimo

  公开号：US20130079333A1

  公开（公告）日：2013-03-28

  The present invention provides 4H,6H-5-oxa-2,3,10b-triaza-benzo[e]azulenes of the formula wherein R 1 and R 2 are as defined herein and which act as V1a receptor modulators, and in particular as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments.

  本发明提供了4H，6H-5-氧杂-2,3,10b-三氮杂苯并[e]吲哚的化合物，其化学结构如下所示： 其中R1和R2如本文所定义，并且这些化合物作为V1a受体调节剂，特别是作为V1a受体拮抗剂，其制备方法，含有它们的药物组合物以及它们作为药物的用途。
• US8828989B2
  申请人：——

  公开号：US8828989B2

  公开（公告）日：2014-09-09