米芬太尼 | 117523-47-4

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 中文名称: 米芬太尼
• 英文名称: mirfentanil
• 英文别名: N-[1-(2-phenylethyl)piperidin-4-yl]-N-pyrazin-2-ylfuran-2-carboxamide
• CAS: 117523-47-4
• 化学式: C₂₂H₂₄N₄O₂
• 分子量: 376.458
• InChiKey: BJZZDOLVVLWFHN-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.1
• 重原子数：
  28
• 可旋转键数：
  6
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.32
• 拓扑面积：
  62.5
• 氢给体数：
  0
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  米芬太尼 、 甲醇 以72%的产率得到
  参考文献：
  名称：

  BAGLEY, JEROME R.;SPENCER, H. KENNETH

  摘要：

  DOI：
• 作为产物：
  描述：

  N-苯乙基-4-氨基哌啶 在 铜 、 三乙胺 作用下， 以 氯仿 为溶剂， 反应 6.5h， 生成 米芬太尼
  参考文献：
  名称：

  New 4-(heteroanilido)piperidines, structurally related to the pure opioidagonist fentanyl, with agonist and/or antagonist properties

  摘要：

  A research program based on certain heterocyclic modifications (12-50) of the fentanyl (1) molecule has generated a novel class of opioids. In the mouse hot-plate test, these compounds were weaker analgesics than 1. Two types of antagonists were observed in morphine-treated rabbits: those (e.g., 28) that reversed both respiratory depression and analgesia and those (e.g. 32) that selectively reversed respiratory depression. Evaluation of in vitro binding affinities to rat brain opioid receptors was inconclusive for a common locus of action for the agonist as well as the antagonist component. Further pharmacological evaluation of 32, N-(2-pyrazinyl)-N-(1-phenethyl-4-piperidinyl)-2-furamide, in the rat showed it to be a potent analgesic (ED50 = 0.07 mg/kg, tail-flick test) with little cardiovascular and respiratory depression when compared to fentanyl.

  DOI：

  10.1021/jm00123a028

文献信息

• [EN] NITROSATED BENZOPYRAN COMPOUNDS AS NOVEL CYCLOOXYGENASE-2 SELECTIVE INHIBITORS<br/>[FR] COMPOSES BENZOPYRANNE NITROSES EN TANT QUE NOUVEAUX INHIBITEURS SELECTIFS DE LA CYCLOOXYGENASE-2
  申请人：PHARMACIA & UPJOHN CO LLC

  公开号：WO2006040676A1

  公开（公告）日：2006-04-20

  This invention specifically relates to novel cyclooxygenase 2 (COX-2) selective inhibitor compounds that donate, transfer or release nitric oxide, stimulate endogenous synthesis of nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase. Compounds of particular interest and their analogs defined by formula (I) wherein Z, X, R1, R2, R3, and R4 are as described in the specification. This invention also relates to pharmaceutical compositions and methods for treating COX-2 mediated disorders, such as inflammation and inflammation related disorders.

  这项发明特指与新型环氧合酶2（COX-2）选择性抑制剂化合物有关，这些化合物可以提供、转移或释放一氧化氮，刺激内源性一氧化氮的合成，提高内源性内皮源性舒张因子的水平，或者是一氧化氮合酶的底物。特别感兴趣的化合物及其由式（I）中定义的类似物，其中Z、X、R1、R2、R3和R4如规范中所述。这项发明还涉及用于治疗COX-2介导的疾病，如炎症和与炎症相关的疾病的药物组合物和方法。
• [EN] CHROMENE DERIVATIVES AS ANTI-INFLAMMATORY AGENTS<br/>[FR] DERIVES DE CHROMENE A TITRE D'AGENTS ANTI-INFLAMMATOIRES
  申请人：PHARMACIA CORP

  公开号：WO2004087687A1

  公开（公告）日：2004-10-14

  The subject invention concerns methods and compounds that have utility in the treatment of a condition associated with cyclooxygenase-2 mediated disorders. Compounds of particular interest are benzopyrans and their analogs defined by formula (I). Wherein Z, X, R1, R2, R3, and R4 are as described in the specification.

  该发明涉及在治疗与环氧合酶-2介导的疾病相关的情况中具有效用的方法和化合物。特别感兴趣的化合物是由式(I)定义的苯并吡喃和它们的类似物。其中Z、X、R1、R2、R3和R4如规范中所述。
• [EN] PRODRUG COMPOSITIONS AND METHODS OF TREATMENT<br/>[FR] COMPOSITIONS DE PROMÉDICAMENT ET PROCÉDÉS DE TRAITEMENT
  申请人：AQUESTIVE THERAPEUTICS INC

  公开号：WO2021087359A1

  公开（公告）日：2021-05-06

  Pharmaceutical compositions include a prodrug of epinephrine are described.

  药物组合物包括表述的肾上腺素前药。
• Multi-functional ionic liquid compositions for overcoming polymorphism and imparting improved properties for active pharmaceutical, biological, nutritional, and energetic ingredients
  申请人：Rogers D. Robin

  公开号：US20070093462A1

  公开（公告）日：2007-04-26

  Disclosed are ionic liquids and methods of preparing ionic liquid compositions of active pharmaceutical, biological, nutritional, and energetic ingredients. Also disclosed are methods of using the compositions described herein to overcome polymorphism, overcome solubility and delivery problems, to control release rates, add functionality, enhance efficacy (synergy), and improve ease of use and manufacture.

  揭示了离子液体及制备活性药物、生物、营养和能量成分的离子液体组合物的方法。还揭示了利用本文描述的组合物的方法，以克服多型性、克服溶解度和输送问题、控制释放速率、增加功能性、增强功效（协同作用）以及改善易用性和制造工艺。
• Fluoro-substituted benzenesulfonyl compounds for the treatment of inflammation
  申请人：Pharmacia Corporation

  公开号：US20030032657A1

  公开（公告）日：2003-02-13

  Methods of treating cyclooxygenase-2 mediated disorders comprising administering to a subject a therapeutically effective amount of one or more fluoro-substituted benzenesulfonyl compounds corresponding to Formula I: 1 wherein A, X, n, R 1 , R 2 , and R 3 are as described in the specification, and novel fluoro-substituted benzenesulfonyl compounds within Formula I.

  治疗环氧合酶-2介导的疾病的方法包括向受试者施用与化学式I:1相对应的一种或多种氟代苯磺酰化合物的治疗有效剂量，其中化学式I中的A、X、n、R1、R2和R3如规范中所述，并且包括化学式I中的新型氟代苯磺酰化合物。