依他西平 | 88124-27-0

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯氮卓类
• 中文名称: 依他西平
• 英文名称: 5-methyl-11-ethoxy-5,6-dihydro-11H-dibenzo(b,e) azepine-6-one
• 英文别名: 5-methyl-11-ethoxy-5,6-dihydro-11H-dibenzo(b,e)-azepine-6-one；Etazepine；11-ethoxy-5-methyl-11H-benzo[c][1]benzazepin-6-one
• CAS: 88124-27-0
• 化学式: C₁₇H₁₇NO₂
• 分子量: 267.327
• InChiKey: BLGFGFHRMMDRPC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.7
• 重原子数：
  20
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.24
• 拓扑面积：
  29.5
• 氢给体数：
  0
• 氢受体数：
  2

安全信息

• 海关编码：
  2933990090

反应信息

• 作为产物：
  描述：

  11-hydroxy-5-methyl-5,11-dihydro-dibenzo[b,e]azepin-6-one 在 氯化亚砜 作用下， 生成 依他西平
  参考文献：
  名称：

  Alkoxy-11 dibenzo[b,e]azépinones-6 à activité anti-convulsivante

  摘要：

  DOI：

  10.1016/0223-5234(88)90145-6

文献信息

• Diagnostic/therapeutic agents
  申请人：Klaveness Jo

  公开号：US20050002865A1

  公开（公告）日：2005-01-06

  Targetable diagnostic and/or therapeutically active agents, e.g. ultrasound contrast agents, comprising a suspension in an aqueous carrier liquid of a reporter comprising gas-containing or gas-generating material, said agent being capable of forming at least two types of binding pairs with a target.

  可定位的诊断和/或治疗活性剂，例如超声对比剂，包括悬浮在水载体液中的报告物，该报告物包含含气体或生成气体的材料，该剂能够与目标形成至少两种结合对。
• Methods and compositions for treating cancer using P2RX2 inhibitors
  申请人：Flagship Pioneering Innovations V, Inc.

  公开号：US10457740B1

  公开（公告）日：2019-10-29

  The present invention provides methods for treating cancer using P2RX2 inhibitors, such as P2RX2 inhibitory antibodies, among others. The invention also features compositions containing P2RX2 inhibitors, methods of diagnosing patients with P2RX2-associated cancer, and methods of predicting the response of cancer in a subject to treatment with P2RX2 inhibitors.

  本发明提供了使用 P2RX2 抑制剂（如 P2RX2 抑制抗体等）治疗癌症的方法。本发明还包括含有 P2RX2 抑制剂的组合物、诊断 P2RX2 相关癌症患者的方法以及预测癌症对 P2RX2 抑制剂治疗的反应的方法。
• Controlled absorption water-soluble pharmaceutically active organic compound formulation for once-daily administration
  申请人：Counts David F.

  公开号：US10463611B2

  公开（公告）日：2019-11-05

  The present disclosure provides a once-daily water-soluble pharmaceutically active formulation for oral administration. In certain embodiments, the composition comprises a water-soluble pharmaceutically active organic compound incorporated into a small particulate, each particulate having a core of the water-soluble pharmaceutically active organic compound or an acceptable salt thereof in reversible association with a pharmaceutically acceptable drug-binding polymer. The core of the composition being surrounded by an insoluble water permeable membrane that is capable of delaying the dissolution of the pharmaceutically active compound therewithin and providing for extended release of the pharmaceutically active compound. In some embodiments, the formulation of the invention are designed to extend release of the pharmaceutically active organic compound for about 3 hours to about 8 hours, thereby enabling preparation of an extended release formulation for any pharmaceutically active compound with a half-life of from about 16 hours to about 21 hours.

  本公开提供了一种用于口服的每日一次水溶性药用活性制剂。在某些实施方案中，该组合物包括掺入小颗粒中的水溶性药用活性有机化合物，每个颗粒都有一个水溶性药用活性有机化合物或其可接受盐的核心，该核心与药学上可接受的药物结合聚合物可逆结合。组合物的核心由不溶性透水膜包围，该膜能够延迟其中的药用活性化合物的溶解，并延长药用活性化合物的释放时间。在某些实施方案中，本发明的制剂可将药用活性有机化合物的释放时间延长约 3 小时至约 8 小时，从而能够制备半衰期为约 16 小时至约 21 小时的任何药用活性化合物的缓释制剂。
• Methods for treating cancer using GRM8 inhibitors
  申请人：Flagship Pioneering Innovations V, Inc.

  公开号：US10683352B1

  公开（公告）日：2020-06-16

  The present invention provides methods for treating cancer using mGluR8 inhibitors, such as mGluR8 inhibitory antibodies and small molecules. The invention also features compositions containing mGluR8 inhibitors, methods of diagnosing patients with mGluR8-associated cancer, and methods of predicting the response of cancer in a subject to treatment with mGluR8 inhibitors.

  本发明提供了使用mGluR8抑制剂（如mGluR8抑制抗体和小分子）治疗癌症的方法。本发明还包括含有 mGluR8 抑制剂的组合物、诊断 mGluR8 相关癌症患者的方法以及预测癌症对 mGluR8 抑制剂治疗的反应的方法。
• Methods and compositions for treating cancer using SERCA pump inhibitors
  申请人：Flagship Pioneering Innovations V, Inc.

  公开号：US11013717B1

  公开（公告）日：2021-05-25

  The present invention provides methods for treating cancer using sarco/endoplasmic reticulum Ca2+-ATPase (SERCA) pump inhibitors, such as SERCA pump inhibitory antibodies, among others. The invention also features compositions containing SERCA pump inhibitors, methods of diagnosing patients with SERCA pump-associated cancer, and methods of predicting the response of cancer in a subject to treatment with SERCA pump inhibitors.

  本发明提供了使用肌浆/内质网Ca2+-ATP酶（SERCA）泵抑制剂（如SERCA泵抑制抗体等）治疗癌症的方法。本发明还包括含有 SERCA 泵抑制剂的组合物、诊断 SERCA 泵相关癌症患者的方法以及预测癌症对 SERCA 泵抑制剂治疗的反应的方法。