3-benzyloxy-4,5α-epoxy-17-methyl-morphin-7-en-6α-ol | 14297-87-1

• 分子结构分类: 有机化合物 - 生物碱及其衍生物 - 吗啡烷
• 英文名称: 3-benzyloxy-4,5α-epoxy-17-methyl-morphin-7-en-6α-ol
• 英文别名: Benzylmorphin-Base；O³-benzyl-morphine；Morphinan-6-ol, 7,8-didehydro-4,5-epoxy-17-methyl-3-(phenylmethoxy)-, (5alpha,6alpha)-；3-methyl-9-phenylmethoxy-2,4,4a,7,7a,13-hexahydro-1H-4,12-methanobenzofuro[3,2-e]isoquinolin-7-ol
• CAS: 14297-87-1；135091-25-7
• 化学式: C₂₄H₂₅NO₃
• 分子量: 375.467
• InChiKey: RDJGWRFTDZZXSM-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.6
• 重原子数：
  28
• 可旋转键数：
  3
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.42
• 拓扑面积：
  41.9
• 氢给体数：
  1
• 氢受体数：
  4

文献信息

• FORMULATIONS OF NONOPIOID AND CONFINED OPIOID ANALGESICS
  申请人：AbbVie Deutschland GmbH & Co. KG

  公开号：US20130344143A1

  公开（公告）日：2013-12-26

  The preferred exemplary embodiments in the present application provide formulations and methods for the delivery of drugs, particularly drugs of abuse, having an abuse-relevant drug substantially confined in the core and a non-abuse relevant drug in a non-core region. These formulations have reduced potential for abuse. In the formulation, preferably the abuse relevant drug is an opioid and the non-abuse relevant drug is acetaminophen or ibuprofen. More preferably, the opioid is hydrocodone, and the non-abuse relevant analgesic is acetaminophen. In certain preferred embodiments, the dosage forms are characterized by resistance to solvent extraction; tampering, crushing or grinding. Certain embodiments of the inventions provide dosage forms that provide an initial burst of release of drug followed by a prolonged period of controllable drug release.

  本申请的首选示例实施方式提供了制剂和方法，用于输送药物，特别是滥用药物，其中滥用相关药物被实质上限制在核心中，而非滥用相关药物则在非核心区域。这些制剂具有减少滥用的潜力。在制剂中，首选的滥用相关药物是阿片类药物，而非滥用相关药物是对乙酰氨基酚或布洛芬。更优选的是，阿片类药物是羟考酮，非滥用相关的镇痛剂是对乙酰氨基酚。在某些首选实施方式中，剂型的特征是抗溶剂提取；防篡改，研磨或研磨。发明的某些实施方式提供剂型，其提供药物的初始释放突发，然后是可控的药物释放的长时间。
• Melt-extruded orally administrable opioid formulations
  申请人：Euro-Celtique, S.A.

  公开号：EP1449530A2

  公开（公告）日：2004-08-25

  Bioavailable sustained release oral opioid analgesic dosage forms, comprising a plurality of multiparticulates produced via melt extrusion techniques are disclosed.

  本发明公开了生物可利用的缓释口服阿片类镇痛剂剂型，包括通过熔融挤压技术生产的多种多微粒。
• Compositions and Methods for Prophylaxis and Treatment of Addictions
  申请人：Omeros Corporation

  公开号：EP2612553A1

  公开（公告）日：2013-07-10

  The present invention relates to methods of treating or preventing addiction and relapse use of addictive agents, and treating or preventing addictive or compulsive behaviour and relapse practice of an addictive behaviour or compulsion, by administering a peroxisome proliferator-activated receptor gamma (PPARγ) agonist, alone or in combination with another therapeutic agent, such as, for example, an opioid receptor antagonist or an antidepressant. The present invention also includes pharmaceutical compositions for treating or preventing addiction or relapse that include a PPARγ agonist and one or more other therapeutic agents, as well as unit dosage forms of such pharmaceutical compositions, which contain a dosage effective in treating or preventing addiction or relapse. The methods and compositions of the invention are useful in the treatment or prevention of addiction to any agent, including alcohol, nicotine, marijuana, cocaine, and amphetamines, as well as compulsive and addictive behaviours, including pathological gambling and pathological overeating.

  本发明涉及通过施用过氧化物酶体增殖激活受体γ(PPARγ)激动剂，单独或与另一种治疗剂，例如，阿片受体拮抗剂或抗抑郁剂联合使用，治疗或预防成瘾和复发使用成瘾制剂，以及治疗或预防成瘾或强迫行为和成瘾行为或强迫行为复发的方法。本发明还包括用于治疗或预防成瘾或复发的药物组合物，其中包括 PPARγ 激动剂和一种或多种其他治疗剂，以及这种药物组合物的单位剂型，其中含有对治疗或预防成瘾或复发有效的剂量。本发明的方法和组合物可用于治疗或预防对任何药物的成瘾，包括酒精、尼古丁、大麻、可卡因和苯丙胺，以及强迫性和成瘾性行为，包括病态赌博和病态暴饮暴食。
• Drug delivery devices and methods for controlled drug release through device orifice
  申请人：TARIS Biomedical LLC

  公开号：US10137287B2

  公开（公告）日：2018-11-27

  A drug delivery device is provided. In an embodiment, the device includes a device body having an elongated drug reservoir lumen, a drug positioned in the drug reservoir lumen, and at least one end plug positioned at an end of the device body, for example inserted in an end of the drug reservoir lumen. The end plug may include an aperture therethough, and the drug delivery device may be configured to release the drug from the drug reservoir lumen through the aperture.

  本文提供了一种给药装置。在一个实施例中，该装置包括具有细长储药腔的装置本体、位于储药腔中的药物以及位于装置本体端部的至少一个端塞，例如插入储药腔的端部。端塞可包括一个开孔，给药装置可配置为通过开孔从储药腔释放药物。
• Use of GABAA receptor reinforcing agent in preparation of sedative and anesthetic medicament
  申请人：Sichuan Haisco Pharmaceutical Co., Ltd.

  公开号：US10729666B2

  公开（公告）日：2020-08-04

  The present disclosure provides a pharmaceutical preparation of a compound of formula (I) or a stereoisomer, pharmaceutically acceptable salt, or prodrug thereof. The present disclosure further provides a method for general anesthesia or sedation for mammals. Also provided are kits and manufactured products of the medicament and the pharmaceutical composition and a method for using the medicament and the pharmaceutical composition.

  本公开提供了一种式（I）化合物或其立体异构体、药学上可接受的盐或原药的药物制剂。本公开进一步提供了一种用于哺乳动物全身麻醉或镇静的方法。还提供了该药物和药物组合物的试剂盒和制成品，以及使用该药物和药物组合物的方法。

表征谱图