羟甲芬太尼 | 78995-14-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 中文名称: 羟甲芬太尼
• 中文别名: N-(3-氨基丙基)-N-甲基-环己胺
• 英文名称: Ohmefentanyl
• 英文别名: N-[1-(2-hydroxy-2-phenylethyl)-3-methylpiperidin-4-yl]-N-phenylpropanamide
• CAS: 78995-14-9
• 化学式: C₂₃H₃₀N₂O₂
• 分子量: 366.5
• InChiKey: FRPRNNRJTCONEC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.6
• 重原子数：
  27
• 可旋转键数：
  6
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.43
• 拓扑面积：
  43.8
• 氢给体数：
  1
• 氢受体数：
  3

文献信息

• Novel Therapeutic Compounds
  申请人：SESHA Ramesh

  公开号：US20120046272A1

  公开（公告）日：2012-02-23

  The present invention describes a series of therapeutically active compounds of formula I, X—Y—Z  (I) that are useful for treating a disorder in a mammal. In the formula I, X and Z, which may be same or different, are independently selected from substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted cycloalkylalkyl, substituted or unsubstituted aryl, substituted or unsubstituted arylalkyl, substituted or unsubstituted heteroaryl, substituted or unsubstituted heteroarylalkyl, substituted or unsubstituted heterocyclic group or substituted or unsubstituted heterocyclylalkyl; and Y is a linker selected from —O—, —S—, —NH—, —(CH 2 ) n —, —CO—, —CONR a —, —NR a CO—, —NR a COO—, —COO—, —CONR a CO—, —CONR a COO— and —COOCOO—. The compounds are useful to treat neurodegenerative disorders, depression, Alzheimer's disease, cognitive disorders, motor disorders, Parkinson's disease, drug addiction, behavioral disorders, inflammatory disorders, stomach disorders, cancers, acute pain, chronic pain and recurrent pain.

  本发明描述了一系列具有治疗活性的化合物，其化学式为I，X—Y—Z  (I)，适用于治疗哺乳动物中的某种疾病。在化学式I中，X和Z，可以相同也可以不同，独立地选择自取代或未取代的烷基、取代或未取代的烯基、取代或未取代的环烷基、取代或未取代的环烷基烷基、取代或未取代的芳基、取代或未取代的芳基烷基、取代或未取代的杂芳基、取代或未取代的杂芳基烷基、取代或未取代的杂环基团或取代或未取代的杂环烷基；Y是从—O—、—S—、—NH—、—(CH2)n—、—CO—、—CONRa—、—NRaCO—、—NRaCOO—、—COO—、—CONRaCO—、—CONRaCOO—和—COOCOO—中选择的连接基团。这些化合物适用于治疗神经退行性疾病、抑郁症、阿尔茨海默病、认知障碍、运动障碍、帕金森病、药物成瘾、行为障碍、炎症性疾病、胃病、癌症、急性疼痛、慢性疼痛和复发性疼痛。
• Methods and compositions for deterring abuse
  申请人：Acura Pharmaceuticals, Inc.

  公开号：US10155044B2

  公开（公告）日：2018-12-18

  Effective methods and compositions to deter abuse of pharmaceutical products (e.g., orally administered pharmaceutical products) including but not limited to immediate release, sustained or extended release and delayed release formulations for drugs subject to abuse comprising at least 10% by weight hydroxypropylcellulose; polyethylene oxide; and a disintegrant selected from the group consisting of crospovidone, sodium starch glycolate and croscarmellose sodium; wherein the ratio of hydroxypropylcellulose to polyethylene oxide on a weight basis is between about 10:1 and 1:10.

  阻止药物滥用的有效方法和组合物（如口服药物包括但不限于用于易滥用药物的速释、缓释和延释制剂，按重量计至少包含 10% 的羟丙基纤维素；聚氧化乙烯；以及选自由克罗波维酮、淀粉乙醇酸钠和克罗卡米洛糖钠组成的组的崩解剂；其中羟丙基纤维素与聚氧化乙烯的重量比约为 10:1 至 1:10。
• NASAL DRUG PRODUCTS AND METHODS OF THEIR USE
  申请人：Adapt Pharma Limited

  公开号：US20170071851A1

  公开（公告）日：2017-03-16

  Drug products adapted for nasal delivery, comprising a pre-primed device filled with a pharmaceutical composition comprising an opioid receptor antagonist, are provided. Methods of treating opioid overdose or its symptoms with the inventive drug products are also provided.
• PHARMACEUTICAL COMPOSITIONS AND METHODS FOR TREATMENT OF PAIN
  申请人：Board of Regents of the University of Texas System

  公开号：US20190117637A1

  公开（公告）日：2019-04-25

  Compositions and methods for treatment of acute and chronic pain are disclosed herein. These compositions include fixed dose oral formulations containing an atypical antipsychotic drug and an opioid. Also provided here are methods of treatment of pain, particularly chronic pain while attenuating the abuse-liability of prescription pain medications.
• MEDICATED SPRAY FOR TREATMENT OF SUBSTANCE ABUSE, OVERDOSE, ADDICTION AND IMPULSE CONTROL DISORDERS
  申请人：GOOBERMAN Lance L.

  公开号：US20200352917A1

  公开（公告）日：2020-11-12

  A method to treat carfentanyl overdose comprising administrating a pharmaceutical formulation in the form of liquid solution for spray administration by the nasal and/or buccal route containing naltrexone as active ingredient in amounts greater than 1%.