3-methyl-1-(1-methyl-1H-imidazol-4-yl)-3-pyrimidin-5-ylmethyl-5-[3-(2,2,2-trifluoro-ethoxy)-phenyl]-1,3-dihydro-indol-2-one | 1141080-39-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡咯并吡啶类
• 英文名称: 3-methyl-1-(1-methyl-1H-imidazol-4-yl)-3-pyrimidin-5-ylmethyl-5-[3-(2,2,2-trifluoro-ethoxy)-phenyl]-1,3-dihydro-indol-2-one
• 英文别名: 3-Methyl-1-(1-methylimidazol-4-yl)-3-(pyrimidin-5-ylmethyl)-5-[3-(2,2,2-trifluoroethoxy)phenyl]indol-2-one
• CAS: 1141080-39-8
• 化学式: C₂₆H₂₂F₃N₅O₂
• 分子量: 493.488
• InChiKey: VSZCXWTXQOBBOG-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.3
• 重原子数：
  36
• 可旋转键数：
  6
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.23
• 拓扑面积：
  73.1
• 氢给体数：
  0
• 氢受体数：
  8

文献信息

• [EN] N-SUBSTITUTED OXINDOLINE DERIVATIVES AS CALCIUM CHANNEL BLOCKERS<br/>[FR] DÉRIVÉS D'OXINDOLINE N-SUBSTITUÉE COMME BLOQUEURS DE CANAUX CALCIQUES
  申请人：MERCK & CO INC

  公开号：WO2009045386A1

  公开（公告）日：2009-04-09

  A series of N-substituted oxindole derivatives represented by Formula I, or pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, calcium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, urinary incontinence, itchiness, allergic dermatitis, epilepsy, diabetic neuropathy, irritable bowel syndrome, depression, anxiety, multiple sclerosis, sleep disorder, bipolar disorder and stroke, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds.

  一系列由公式I所表示的N-取代的氧吲哚衍生物或其药学上可接受的盐。药物组合物包括有效量的该化合物，单独或与一个或多个其他治疗活性化合物联合使用，并与药学上可接受的载体一起使用。治疗与钙通道活性相关或由其引起的疾病的方法，包括例如急性疼痛、慢性疼痛、内脏疼痛、炎症性疼痛、神经病理性疼痛、尿失禁、瘙痒、过敏性皮炎、癫痫、糖尿病神经病变、肠易激综合征、抑郁症、焦虑症、多发性硬化、睡眠障碍、躁郁症和中风，包括单独或与一个或多个其他治疗活性化合物联合使用的有效量的该化合物的给药。
• N-SUBSTITUTED OXINDOLINE DERIVATIVES AS CALCIUM CHANNEL BLOCKERS
  申请人：Duffy Joseph L.

  公开号：US20100216815A1

  公开（公告）日：2010-08-26

  A series of N-substituted oxindole derivatives represented by Formula I, or pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, calcium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, urinary incontinence, itchiness, allergic dermatitis, epilepsy, diabetic neuropathy, irritable bowel syndrome, depression, anxiety, multiple sclerosis, sleep disorder, bipolar disorder and stroke, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds.

  一系列以式I表示的N-取代吲哚衍生物，或其药学上可接受的盐。制药组合物包括有效量的本化合物，单独使用或与一种或多种其他治疗活性化合物结合，并含有药学上可接受的载体。治疗与钙通道活性相关或由其引起的病症的方法，包括急性疼痛、慢性疼痛、内脏疼痛、炎症性疼痛、神经病理性疼痛、尿失禁、瘙痒、过敏性皮炎、癫痫、糖尿病神经病变、肠易激综合征、抑郁症、焦虑症、多发性硬化症、睡眠障碍、躁狂症和中风，包括单独使用或与一种或多种其他治疗活性化合物结合的本化合物的有效量的给药。
• US8273749B2
  申请人：——

  公开号：US8273749B2

  公开（公告）日：2012-09-25