2,3-dihydroindol-1-yl-[(5R)-4,5,6,7-tetrahydro-1H-benzimidazol-5-yl]methanone

• 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: 2,3-dihydroindol-1-yl-[(5R)-4,5,6,7-tetrahydro-1H-benzimidazol-5-yl]methanone
• 化学式: C₁₆H₁₇N₃O
• 分子量: 267.33
• InChiKey: GKNHGZIVTFCIOE-GFCCVEGCSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.8
• 重原子数：
  20
• 可旋转键数：
  1
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  49
• 氢给体数：
  1
• 氢受体数：
  2

文献信息

• Combination treatment for depression
  申请人：——

  公开号：US20020107244A1

  公开（公告）日：2002-08-08

  The present invention relates to a method of treating depression or anxiety in a mammal, including a human, by administering to the mammal a 5-HT3 receptor antagonist in combination with an SRI antidepressant agent with improvement in sexual function and/or reduction in gastro-intestinal side effects. It also relates to pharmaceutical compositions containing a pharmaceutically acceptable carrier, a 5-HT3 receptor antagonist and an SRI antidepressant.

  本发明涉及一种治疗哺乳动物，包括人类的抑郁症或焦虑症的方法，通过给哺乳动物同时注射5-HT3受体拮抗剂和SRI抗抑郁剂来改善性功能和/或减少胃肠道副作用。它还涉及含有药用载体、5-HT3受体拮抗剂和SRI抗抑郁剂的制药组合物。
• Novel aryloxypropanamines
  申请人：Tung Roger

  公开号：US20070116643A1

  公开（公告）日：2007-05-24

  The present invention relates to an aryloxypropanamine containing one or more deuterium or 13 C in place of a hydrogen or carbon, respectively. These isotopic aryloxypropanamines of the invention are inhibitors of serotonin and norepinephrine uptake and possess unique biopharmaceutical and pharmacokinetic properties compared to the responding light atom isotopologues. The invention further provides compositions comprising these isotopic aryloxypropanamines and methods of treating diseases and conditions linked to reduced neurotransmission of norepinephrine and/or serotonin. It further provides methods for using these isotopic aryloxypropanamines to accurately determine the concentration of the light atom isotopologues in biological fluids and of studying the metabolism of the light atom isotopologues.

  本发明涉及一种含有一个或多个氘或13C代替氢或碳的芳氧基丙胺，这些同位素芳氧基丙胺是血清素和去甲肾上腺素再摄取抑制剂，并且与响应的轻原子同位素相比具有独特的生物制药和药代动力学特性。本发明还提供了包含这些同位素芳氧基丙胺的组合物以及治疗与去甲肾上腺素和/或血清素神经递质减少相关的疾病和病况的方法。它进一步提供了使用这些同位素芳氧基丙胺精确测定生物流体中轻原子同位素浓度和研究轻原子同位素代谢的方法。
• Method of treating lower urinary tract disorders
  申请人：Dynogen Pharmaceuticals, Inc.

  公开号：EP1795196A2

  公开（公告）日：2007-06-13

  The invention relates to the treatment of at least one symptom of a lower urinary tract disorder in a subject in need of treatment wherein the symptom is selected from the group consisting of urinary frequency, urinary urgency, urinary urge incontinence, nocturia and enuresis, and wherein to a subject in need of treatment a therapeutically effective amount of a compound that has 5-HT3 receptor antagonist activity and NorAdrenaline Reuptake Inhibitor (NARI) activity is to be administered. The invention further relates to the treatment of at least one symptom of a lower urinary tract disorder in a subject in need of treatment wherein the symptom is selected from the group consisting of urinary frequency, urinary urgency, urinary urge incontinence, nocturia and enuresis, comprising coadministering to said subject a first amount of a 5HT3 antagonist and a second amount of a NARI, wherein the first and second amounts together comprise a therapeutically effective amount or are each present in a therapeutically effective amount.

  本发明涉及需要治疗的受试者至少一种下尿路疾病症状的治疗，其中该症状选自由尿频、尿急、尿失禁、夜尿和遗尿组成的组，并且对需要治疗的受试者施用治疗有效量的具有5-HT3受体拮抗剂活性和去甲肾上腺素再摄取抑制剂（NARI）活性的化合物。本发明进一步涉及对需要治疗的受试者的至少一种下尿路疾病症状的治疗，其中该症状选自由尿频、尿急、尿失禁、夜尿和遗尿组成的组，包括向所述受试者联合施用第一量的5-HT3受体拮抗剂和第二量的NARI，其中第一量和第二量共同组成治疗有效量或各自以治疗有效量存在。
• Method of treating functional bowel disorders
  申请人：Edusa Pharmaceuticals, Inc

  公开号：EP2286817A2

  公开（公告）日：2011-02-23

  The invention relates to a method of treating functional bowel disorders in a subject in need of treatment. The method comprises administering to a subject in need of treatment a therapeutically effective amount of a compound that has 5-HT3 receptor antagonist activity and NorAdrenaline Reuptake Inhibitor (NARI) activity. The invention further relates to a method of treating a functional bowel disorder in a subject in need thereof, comprising coadministering to said subject a first amount of a 5-HT3 antagonist and a second amount of a NARI, wherein the first and second amounts together comprise a therapeutically effective amount or are each present in a therapeutically effective amount. In addition, the method of the invention comprises administering a NARI alone. The functional bowel disorders which can be treated according to the method of the invention include IBS, functional abdominal bloating, functional constipation and functional diarrhea.

  本发明涉及一种治疗需要治疗的对象的功能性肠紊乱的方法。该方法包括向需要治疗的受试者施用治疗有效量的具有 5-HT3 受体拮抗剂活性和去甲肾上腺素再摄取抑制剂（NARI）活性的化合物。本发明进一步涉及一种治疗有需要的受试者的功能性肠紊乱的方法，包括向所述受试者联合施用第一量的5-HT3拮抗剂和第二量的NARI，其中第一量和第二量共同构成治疗有效量或各自以治疗有效量存在。此外，本发明的方法还包括单独施用一种 NARI。根据本发明的方法可以治疗的功能性肠道疾病包括肠易激综合征、功能性腹胀、功能性便秘和功能性腹泻。
• Method of treating nausea, vomiting, retching or any combination thereof
  申请人：Dynogen Pharmaceuticals, Inc.

  公开号：US20040147510A1

  公开（公告）日：2004-07-29

  The invention relates to a method of treating nausea, vomiting, retching or any combination thereof in a subject in need of treatment. The method comprises administering to a subject in need of treatment a therapeutically effective amount of a compound that has 5-HT 3 receptor antagonist activity and NorAdrenaline Reuptake Inhibitor (NARI) activity. The invention further relates to a method of treating nausea, vomiting, retching or any combination thereof in a subject in need thereof, comprising coadministering to said subject a first amount of a 5-HT 3 antagonist and a second amount of a NARI, wherein the first and second amounts together comprise a therapeutically effective amount or are each present in a therapeutically effective amount. In addition, the method of the invention comprises administering a NARI alone.

  本发明涉及一种治疗需要治疗的对象的恶心、呕吐、反胃或其任何组合的方法。该方法包括向需要治疗的受试者施用治疗有效量的化合物，该化合物具有 5-HT 3 受体拮抗剂活性和肾上腺素再摄取抑制剂（NARI）活性的化合物。本发明进一步涉及一种治疗需要治疗的受试者的恶心、呕吐、反胃或其任何组合的方法，包括向所述受试者联合施用第一量的5-HT 3 拮抗剂和第二量的 NARI，其中第一量和第二量共同构成治疗有效量或各自存在治疗有效量。此外，本发明的方法还包括单独施用一种 NARI。