2-ethyl-10-(4'-methyl-1'-piperazinyl)-4H-thieno[2,3-b][1,5]benzodiazepine

• 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: 2-ethyl-10-(4'-methyl-1'-piperazinyl)-4H-thieno[2,3-b][1,5]benzodiazepine
• 英文别名: 2-Ethyl-10-(4-methylpiperazin-1-yl)-4,5-dihydrothieno[3,2-c][1,5]benzodiazepine
• 化学式: C₁₈H₂₄N₄S
• 分子量: 328.481
• InChiKey: RBKZBBITAKTDCO-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4
• 重原子数：
  23
• 可旋转键数：
  2
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.44
• 拓扑面积：
  50
• 氢给体数：
  1
• 氢受体数：
  5

文献信息

• [EN] COMPOUND FOR THE TREATMENT OF CNS DISORDERS<br/>[FR] COMPOSE POUR LE TRAITEMENT DE TROUBLES DU SYSTEME NERVEUX CENTRAL (SNC)
  申请人：IVAX CORP

  公开号：WO2003104239A1

  公开（公告）日：2003-12-18

  The present invention relates to the compound 2-ethyl-10-(4-methyl-1-piperazinyl)-4H-thieno[2,3-b][1,5]benzodiazepine and its use as is or in substantially pure form in the treatment of CNS disorders including schizophrenia and bipolar disorder. The compound is prepared by reacting a substituted thiophene compound with 2-fluoronitrobenzene to form, after ring closure and reaction with N-methylpiperazine, the title compound. The compound is then purified to substantially pure form and is useful as an antipsychotic. The compound may also be combined with other active ingredients including HMG CoA reductase inhibitors such as lovastatin or simvastatin and/or antidepressants such as fluxoetine or other SSRIs to form medically useful combination products useful in treating psychotic conditions and depression while also preventing any rise beyond the normal range of cholesterol levels in any subset of patients that might develop such a condition.

  本发明涉及化合物2-乙基-10-(4-甲基-1-哌嗪基)-4H-噻吩[2,3-b] [1,5]苯二氮平及其作为治疗中枢神经系统疾病，包括精神分裂症和双相情感障碍的药物使用，可以是原样使用或在基本纯净形式下。该化合物通过将取代噻吩化合物与2-氟硝基苯反应，经环合和与N-甲基哌嗪反应后形成所述化合物。然后将该化合物纯化至基本纯净形式，并可用作抗精神病药物。该化合物还可以与其他活性成分结合，包括HMG CoA还原酶抑制剂，如洛伐他汀或辛伐他汀，以及抗抑郁药物，如氟西汀或其他SSRI，形成医学上有用的组合产品，用于治疗精神疾病和抑郁症，同时防止任何可能出现这种情况的患者胆固醇水平超出正常范围的上升。
• Compound useful for the treatment of CNS disorders
  申请人：——

  公开号：US20040063694A1

  公开（公告）日：2004-04-01

  The present invention relates to the compound 2-ethyl-10-(4-methyl-1-piperazinyl)-4H-thieno[2,3-b][l,5]benzodiazepine and its use as is or in substantially pure form in the treatment of CNS disorders including schizophrenia and bipolar disorder. The compound is prepared by reacting a substituted thiophene compound with 2-fluoronitrobenzene to form, after ring closure and reaction with N-methylpiperazine, the title compound. The compound is then purified to substantially pure form and is useful as an antipsychotic. The compound may also be combined with other active ingredients including HMG CoA reductase inhibitors such as lovastatin or simvastatin and/or antidepressants such as fluxoetine or other SSRIs to form medically useful combination products useful in treating psychotic conditions and depression while also preventing any rise beyond the normal range of cholesterol levels in any subset of patients that might develop such a condition.

  本发明涉及化合物 2-乙基-10-(4-甲基-1-哌嗪基)-4H-噻吩[2,3-b][l,5]苯并二氮杂卓及其在治疗中枢神经系统疾病（包括精神分裂症和躁狂症）中的原形或基本纯形用途。该化合物的制备方法是将取代的噻吩化合物与 2-氟硝基苯反应，在闭环并与 N-甲基哌嗪反应后形成标题化合物。该化合物随后被提纯为基本纯净的形式，可用作抗精神病药物。该化合物还可与其他活性成分结合使用，包括 HMG CoA 还原酶抑制剂，如洛伐他汀或辛伐他汀，和/或抗抑郁剂，如氟西汀或其他 SSRIs，以形成对治疗精神病和抑郁症有用的药物组合产品，同时还可防止任何可能出现此类病症的亚组患者的胆固醇水平升高超过正常范围。
• Pharmaceutical compounds
  申请人：LILLY INDUSTRIES LIMITED

  公开号：EP0454436B1

  公开（公告）日：1995-09-13
• US4115568A
  申请人：——

  公开号：US4115568A

  公开（公告）日：1978-09-19
• US4172831A
  申请人：——

  公开号：US4172831A

  公开（公告）日：1979-10-30