3-[2-(trifluoromethyl)-4'-fluorobenzhydryloxy]-N-(tert-butyl)azetidine-1-carboxamide

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 3-[2-(trifluoromethyl)-4'-fluorobenzhydryloxy]-N-(tert-butyl)azetidine-1-carboxamide
• 英文别名: N-tert-butyl-3-[(4-fluorophenyl)-[2-(trifluoromethyl)phenyl]methoxy]azetidine-1-carboxamide
• 化学式: C₂₂H₂₄F₄N₂O₂
• 分子量: 424.438
• InChiKey: MBCVORKWWTUQEI-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.4
• 重原子数：
  30
• 可旋转键数：
  5
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.41
• 拓扑面积：
  41.6
• 氢给体数：
  1
• 氢受体数：
  6

反应信息

• 作为产物：
  描述：

  3-[2-(trifluoromethyl)-4'-fluorobenzhydryloxy]azetidine hydrochloride 、 叔丁基异氰酸酯 在 MP-carbonate 作用下， 以 二氯甲烷 为溶剂， 反应 16.0h， 以87%的产率得到3-[2-(trifluoromethyl)-4'-fluorobenzhydryloxy]-N-(tert-butyl)azetidine-1-carboxamide
  参考文献：
  名称：

  [EN] AZETIDINECARBOXAMIDE DERIVATIVES AND THEIR USE IN THE TREATMENT OF CB1 RECEPTOR MEDIATED DISORDERS
  [FR] DERIVES D'AZETIDINECARBOXAMIDE ET LEUR UTILISATION DANS LE TRAITEMENT DE TROUBLES MEDIES PAR LES RECEPTEUR CB1

  摘要：

  式(I)化合物及其在治疗中的应用，特别用于治疗由CB1受体介导的疾病，如肥胖症：式(I)中：R1和R2各自独立地选自芳基；R3为氢或烷基；或其药学上可接受的盐或前药，其中R1和R2中至少一个在相对于与[-CH-0-]基团连接点的邻位上具有非氢取代基。

  公开号：

  WO2004096763A1

文献信息

• Azetidinecarboxamide derivatives and their use in the treatment of cb1 receptor mediated disorders
  申请人：Davidson Edward Paul James

  公开号：US20070054891A1

  公开（公告）日：2007-03-08

  Compounds of formula (I) and their use in therapy, particularly for the treatment of a disorder mediated by CB 1 receptors such as obesity: Formula (I) wherein: R 1 and R 2 are independently selected from aryl; and R 3 is hydrogen or alkyl; or a pharmaceutically acceptable salt or prodrug thereof, wherein at least one of R 1 and R 2 has a non-hydrogen substituent in the ortho-position(s) thereof relative to the point of attachment to the [—CH-0-] group.

  公式（I）的化合物及其在治疗中的应用，特别是用于治疗由CB1受体介导的疾病，如肥胖症：公式（I）其中：R1和R2独立选择自芳基；R3为氢或烷基；或其药学上可接受的盐或前药，其中至少有一个R1和R2在其与[—CH-0-]基团连接点相对于邻位（ortho）位置上具有非氢取代基。
• Formulations and methods for treating acute cannabinoid overdose
  申请人：Anebulo Pharmaceuticals, Inc.

  公开号：US11141404B1

  公开（公告）日：2021-10-12

  Described herein are uses of the CB1 inhibitors (e.g., antagonists, neutral antagonists, inverse agonists) and various methods of using and administering a CB1 inhibitor to a patient, especially patients showing symptoms of drug overdose or suspected of a drug overdose. Further described herein are uses wherein the CB1 inhibitor is ANEB-001. Further described herein are treatments with a CB1 inhibitor for THC or synthetic cannabinoid overdose.

  本文描述了CB1抑制剂（如拮抗剂、中性拮抗剂、逆激动剂）的用途，以及向患者，特别是出现药物过量症状或疑似药物过量的患者使用和施用CB1抑制剂的各种方法。本文进一步描述了CB1抑制剂为ANEB-001的用途。本文还描述了使用 CB1 抑制剂治疗四氢大麻酚或合成大麻素过量的方法。
• AZETIDINECARBOXAMIDE DERIVATIVES AND THEIR USE IN THE TREATMENT OF CB1 RECEPTOR MEDIATED DISORDERS
  申请人：VERNALIS RESEARCH LIMITED

  公开号：EP1620395B1

  公开（公告）日：2009-12-30
• FORMULATIONS AND METHODS FOR TREATING ACUTE CANNABINOID OVERDOSE
  申请人：Anebulo Pharmaceuticals, Inc.

  公开号：US20220151990A1

  公开（公告）日：2022-05-19

  Described herein are uses of the CB1 inhibitors (e.g., antagonists, neutral antagonists, inverse agonists) and various methods of using and administering a CB1 inhibitor to a patient, especially patients showing symptoms of drug overdose or suspected of a drug overdose. Further described herein are uses wherein the CB1 inhibitor is ANEB-001. Further described herein are treatments with a CB1 inhibitor for THC or synthetic cannabinoid overdose.
• US7504522B2
  申请人：——

  公开号：US7504522B2

  公开（公告）日：2009-03-17