4-Chloro-2-(2-hydroxy-3-morpholin-4-ylpropyl)-5-phenyl-1,2-oxazol-3-one;hydrochloride

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 恶嗪烷类
• 英文名称: 4-Chloro-2-(2-hydroxy-3-morpholin-4-ylpropyl)-5-phenyl-1,2-oxazol-3-one;hydrochloride
• 化学式: C16H20Cl2N2O4
• 分子量: 375.2
• InChiKey: KIWUOCZHZROUNT-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.88
• 重原子数：
  24
• 可旋转键数：
  5
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.44
• 拓扑面积：
  62.2
• 氢给体数：
  2
• 氢受体数：
  5

文献信息

• Use of isoxazolinones as cerebro-active drugs
  申请人：Sankyo Company Limited

  公开号：EP0334674A2

  公开（公告）日：1989-09-27

  Isoxazolin-3-one derivatives of formula (I): [in which: R¹ is hydrogen or halogen; R² is C₁ - C₄ alkyl, optionally substituted phenyl or heterocyclic; or R¹ and R² together form a hydrocarbon ring; R³ is hydrogen or C₁ - C₄ alkyl; and R⁴ is C₁ - C₄ alkyl; or R³ and R⁴, together with the adjacent nitrogen, form a cycloaliphatic amino group] and pharmacoligically acceptable acid addition salts thereof have been found to have a direct effect on the cerebral circulation and/or metabolism, and they can be used in the treatment of cerebrovascular disorders.

  式(I)的异噁唑啉-3-酮衍生物： 其中R¹ 为氢或卤素；R² 为 C₁ - C₄ 烷基、任选取代的苯基或杂环；或 R¹ 和 R² 共同形成一个烃环；R³ 为氢或 C₁ - C₄ 烷基；R⁴ 为 C₁ - C₄ 烷基；或 R³ 和 R⁴ 与邻近的氮一起形成环脂族氨基]及其药理上可接受的酸加成盐已被发现对脑循环和/或新陈代谢有直接作用，可用于治疗脑血管疾病。
• Compositions and therapy for substance addiction
  申请人：——

  公开号：US20020168403A1

  公开（公告）日：2002-11-14

  Inhibitors of monoamine oxidase used in combination with an addictive substance, or a pharmacological derivative or analogue thereof, are useful for the treatment of substance addiction disorders. In particular, the invention discloses compositions, and methods of use thereof, comprising selegiline and nicotine for the treatment of cigarette smokers wishing to abstain. The compositions and methods of use thereof include oral, inhalant, parenteral and transdermal patch modes of therapy, whereby the subject benefits from the combined effects of a monoamine oxidase inhibitor in combination with an addicitive substance, or derivative thereof.

  单胺氧化酶抑制剂与成瘾物质或其药理衍生物或类似物结合使用，可用于治疗物质成瘾症。特别是，本发明公开了包含西格列汀和尼古丁的组合物及其使用方法，用于治疗希望戒烟的吸烟者。本发明的组合物及其使用方法包括口服、吸入、肠外和透皮贴剂治疗模式，受试者可从单胺氧化酶抑制剂与添加剂物质或其衍生物的联合作用中获益。
• METHODS AND COMPOSITIONS FOR TREATING PAIN
  申请人：Apkarian Technologies LLC

  公开号：EP3946302A1

  公开（公告）日：2022-02-09
• [EN] METHODS AND COMPOSITIONS FOR TREATING PAIN<br/>[FR] PROCÉDÉS ET COMPOSITIONS POUR LE TRAITEMENT DE LA DOULEUR
  申请人：APKARIAN TECH LLC

  公开号：WO2020227646A1

  公开（公告）日：2020-11-12

  The present disclosure features combinations of dopaminergic agents and analgesic agents useful for treating pain. In particular, the combinations feature a low ratio of dopaminergic agent to analgesic agent. The dopaminergic agent can be an agonist of the dopamine receptor D1 -like family or the dopamine receptor D2-like family. Such combinations potentiate analgesia to 1) alleviate acute pain, 2) prevent the transition from acute pain to chronic pain, and 3) manage chronic pain.