2-(R)-(1-(S)-(3,5-bis(trifluoromethyl)phenyl)-2-hydroxyethoxy)-4-(4-(N,N-dimethylamino)but-2-yn-yl)-3-(S)-(4-fluorophenyl)morpholine | 627083-03-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 恶嗪烷类
• 英文名称: 2-(R)-(1-(S)-(3,5-bis(trifluoromethyl)phenyl)-2-hydroxyethoxy)-4-(4-(N,N-dimethylamino)but-2-yn-yl)-3-(S)-(4-fluorophenyl)morpholine
• 英文别名: (2S)-2-[3,5-bis(trifluoromethyl)phenyl]-2-[(2R,3S)-4-[4-(dimethylamino)but-2-ynyl]-3-(4-fluorophenyl)morpholin-2-yl]oxyethanol
• CAS: 627083-03-8
• 化学式: C₂₆H₂₇F₇N₂O₃
• 分子量: 548.501
• InChiKey: MAAQKNNGFXGCNW-TZRRMPRUSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.2
• 重原子数：
  38
• 可旋转键数：
  7
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.46
• 拓扑面积：
  45.2
• 氢给体数：
  1
• 氢受体数：
  12

文献信息

• Method of treating cancer
  申请人：——

  公开号：US20030215456A1

  公开（公告）日：2003-11-20

  The present invention relates to methods of treating cancer using a combination of a compound which is a PSA conjugate and a tachykinin receptor antagonist, which methods comprise administering to said mammal, either sequentially in any order or simultaneously, amounts of at least two therapeutic agents selected from a group consisting of a compound which is a PSA conjugate and a tachykinin receptor antagonist. The invention also relates to methods of preparing such compositions.

  本发明涉及使用一种PSA结合物和一种催吐肽受体拮抗剂的组合来治疗癌症的方法，该方法包括向所述哺乳动物施用来自PSA结合物和催吐肽受体拮抗剂组成的一组中至少两种治疗剂的剂量，可以按任意顺序依次施用或同时施用。该发明还涉及制备这种组合物的方法。
• Method for treating premenstrual or late luteal phase syndrome
  申请人：Merck & Co. Inc.

  公开号：US20020142942A1

  公开（公告）日：2002-10-03

  A tachykinin receptor antagonist is useful for alleviating or managing symptoms associated with premenstrual syndrome in a woman, in particular, for the treatment or prevention of disturbances of appetite, disturbances of mood, or both, associated with premenstrual syndrome.

  一种速激肽受体拮抗剂对于缓解或管理与经前综合症相关的症状在女性中是有用的，特别是用于治疗或预防与经前综合症相关的食欲紊乱、情绪紊乱或两者都有的症状。
• Method for treating or preventing psychosomatic and psychoimmunologic disorders
  申请人：Merck & Co., Inc.

  公开号：US20010029244A1

  公开（公告）日：2001-10-11

  A tachykinin receptor antagonist is useful for treating or preventing a psychosomatic or a psychoimmunological disorder in a patient.

  速激肽受体拮抗剂可用于治疗或预防患者的心身疾病或精神免疫疾病。
• Use of a NK-1 receptor antagonist and an antidepressant and/or an anti-anxiety agent
  申请人：Merck Sharp & Dohme Ltd.

  公开号：US20020042361A1

  公开（公告）日：2002-04-11

  The present invention relates to the treatment or prevention of depression and/or anxiety by the administration of a combination of a specific class of NK-1 receptor antagonists and an antidepressant or anti-anxiety agent. The present invention also provides preclinical screens for anxiolytic and antidepressant activity of NK-1 receptor antagonists.

  本发明涉及通过服用特定类别的 NK-1 受体拮抗剂和抗抑郁剂或抗焦虑剂的组合来治疗或预防抑郁症和/或焦虑症。本发明还提供了 NK-1 受体拮抗剂抗焦虑和抗抑郁活性的临床前筛选。
• MORPHOLINE DERIVATIVES AND THEIR USE AS THERAPEUTIC AGENTS
  申请人：MERCK SHARP & DOHME LTD.

  公开号：EP0777659B1

  公开（公告）日：2001-06-06