11-(1-哌嗪)-二苯并[b,f][1,4]硫氮杂革-7-醇 | 232597-73-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并硫氮卓类
• 中文名称: 11-(1-哌嗪)-二苯并[b,f][1,4]硫氮杂革-7-醇
• 中文别名: 喹硫平杂质
• 英文名称: 6-Piperazin-1-ylbenzo[b][1,4]benzothiazepin-2-ol
• CAS: 232597-73-8
• 化学式: C₁₇H₁₇N₃OS
• 分子量: 311.4
• InChiKey: CAWOJGJDGLXKTF-UHFFFAOYSA-N

物化性质

• 熔点：
  213-216°C
• 沸点：
  530.5±60.0 °C(Predicted)
• 密度：
  1.38±0.1 g/cm3(Predicted)
• 溶解度：
  甲醇（微溶）、水（微溶）

计算性质

• 辛醇/水分配系数(LogP)：
  2.2
• 重原子数：
  22
• 可旋转键数：
  1
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.24
• 拓扑面积：
  73.2
• 氢给体数：
  2
• 氢受体数：
  4

文献信息

• [EN] AMINO ACID CONJUGATES OF QUETIAPINE, PROCESS FOR MAKING AND USING THE SAME<br/>[FR] CONJUGUÉS D'ACIDES AMINÉS DE QUÉTIAPINE, PROCÉDÉ DE FABRICATION ET D'UTILISATION DE CEUX-CI
  申请人：KEMPHARM INC

  公开号：WO2011082076A1

  公开（公告）日：2011-07-07

  The presently described technology provides a novel class of prodrugs of quetiapine that can be synthesized by chemically conjugating amino acids to quetiapine. The present technology also provides methods of treating patients, pharmaceutical compositions and methods of synthesizing conjugates of the present technology.

  目前描述的技术提供了一种新型的奎哌齐平前药类，可以通过将氨基酸与奎哌齐平进行化学偶联来合成。目前的技术还提供了治疗患者的方法、制药组合物和合成本技术的结合物的方法。
• FATTY ACID CONJUGATES OF QUETIAPINE, PROCESS FOR MAKING AND USING THE SAME
  申请人：KemPharm, Inc.

  公开号：US20170247368A1

  公开（公告）日：2017-08-31

  The presently described technology provides a novel class of prodrugs of quetiapine that can be synthesized by chemically conjugating fatty acids to quetiapine. Pharmaceutical compositions and methods of synthesizing conjugates of the present technology are also provided. Methods of treating patients with the compositions of the present technology are also provided.

  目前所描述的技术提供了一种新型的奎硫平前药类，可以通过将脂肪酸与奎硫平进行化学共轭来合成。同时，还提供了制备本技术共轭物的药物组合物和方法。还提供了使用本技术组合物治疗患者的方法。
• Amino acid conjugates of quetiapine, process for making and using the same
  申请人：KemPharm, Inc.

  公开号：US10010615B2

  公开（公告）日：2018-07-03

  The presently described technology provides a novel class of prodrugs of quetiapine that can be synthesized by chemically conjugating amino acids. The present technology also provides methods of treating patients, pharmaceutical compositions and methods of synthesizing conjugates of the present technology.

  本技术提供了一类新型的喹硫平原药，可以通过化学合成氨基酸的方法合成。本技术还提供了治疗病人的方法、药物组合物和合成本技术共轭物的方法。
• Metabolite
  申请人：Goldstein Jeffrey

  公开号：US20050026899A1

  公开（公告）日：2005-02-03

  A method of treating anxiety, agitation, hostility, panic, eating disorders, affective symptoms, mood symptoms, negative and positive psychotic symptoms commonly associated with schizophrenia, dementia, anxiety, depression, mood disorders, bipolar disorders, bipolar mania, bipolar depression, cognitive disorders and neurodegenerative disorders comprising administering an effective amount of Formula I or its pharmaceutically acceptable salt. In another aspect of the invention a pharmaceutical composition is provided comprising an effective amount of Formula I or its pharmaceutically acceptable salt and at least on pharmaceutically acceptable carrier or diluent.

  一种治疗焦虑、激动、敌意、恐慌、进食障碍、情感症状、情绪症状、阴性和阳性精神症状的方法，这些症状通常与精神分裂症、痴呆症、焦虑症、抑郁症、情绪障碍、双相情感障碍、双相躁狂症、双相抑郁症、认知障碍和神经退行性疾病有关。 或其药学上可接受的盐。在本发明的另一方面，提供了一种药物组合物，其中包含有效量的式Ⅰ或其药学上可接受的盐和至少一种药学上可接受的载体或稀释剂。
• AMINO ACID CONJUGATES OF QUETIAPINE, PROCESS FOR MAKING AND USING THE SAME
  申请人：Kempharm, Inc.

  公开号：EP2519101A1

  公开（公告）日：2012-11-07