nicotinic acid 4,5α-epoxy-3-methoxy-17-methyl-morphinan-6α-yl ester | 808-24-2

• 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: nicotinic acid 4,5α-epoxy-3-methoxy-17-methyl-morphinan-6α-yl ester
• 英文别名: 4,5α-epoxy-3-methoxy-17-methyl-6α-nicotinoyloxy-morphinane；nicodicodine；[(4R,4aR,7S,7aR,12bS)-9-methoxy-3-methyl-2,4,4a,5,6,7,7a,13-octahydro-1H-4,12-methanobenzofuro[3,2-e]isoquinolin-7-yl] pyridine-3-carboxylate
• CAS: 808-24-2
• 化学式: C₂₄H₂₆N₂O₄
• 分子量: 406.481
• InChiKey: GTGRMWCOZHEYRL-MJFIPZRTSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.3
• 重原子数：
  30
• 可旋转键数：
  4
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  60.9
• 氢给体数：
  0
• 氢受体数：
  6

反应信息

• 作为产物：
  描述：

  烟酸 在 吡啶 、 氯化亚砜 作用下， 以 氯仿 为溶剂， 反应 22.0h， 生成 nicotinic acid 4,5α-epoxy-3-methoxy-17-methyl-morphinan-6α-yl ester
  参考文献：
  名称：

  Hosztafi; Kohegyi; Simon, Arzneimittel-Forschung/Drug Research, 1993, vol. 43, # 11, p. 1200 - 1203

  摘要：

  DOI：

文献信息

• METHODS AND COMPOSITIONS FOR PREVENTING OPIOID ABUSE
  申请人：Waterville Valley Technologies, Inc.

  公开号：US20160326182A1

  公开（公告）日：2016-11-10

  Abuse-resistant opioid compounds, drug delivery systems, pharmaceutical compositions comprising an opioid covalently bound to a chemical moiety are provided. Methods of delivering an active ingredient to a subject and methods of preventing opioid abuse are also provided.

  提供了耐滥用的阿片类化合物、药物输送系统、含有阿片类药物与化学基团共价结合的制药组合物。还提供了将活性成分输送给受试者的方法以及预防阿片类药物滥用的方法。
• Nitrate prodrugs able to release nitric oxide in a controlled and selective way and their use for prevention and treatment of inflammatory, ischemic and proliferative diseases
  申请人：Scaramuzzino, Giovanni

  公开号：EP1336602A1

  公开（公告）日：2003-08-20

  New pharmaceutical compounds of general formula (I): F-(X)q where q is an integer from 1 to 5, preferably 1; -F is chosen among drugs described in the text, -X is chosen among 4 groups -M, -T, -V and -Y as described in the text. The compounds of general formula (I) are nitrate prodrugs which can release nitric oxide in vivo in a controlled and selective way and without hypotensive side effects and for this reason they are useful for the preparation of medicines for prevention and treatment of inflammatory, ischemic, degenerative and proliferative diseases of musculoskeletal, tegumental, respiratory, gastrointestinal, genito-urinary and central nervous systems.

  通式（I）的新药物化合物：F-（X）q，其中q是1到5的整数，最好是1；-F是在文本中描述的药物中选择的，-X是在文本中描述的4个组-M，-T，-V和-Y中选择的。通式（I）的化合物是硝酸盐前药，可以在体内以受控和选择性的方式释放一氧化氮，而不会产生降压副作用，因此它们非常适用于制备用于预防和治疗肌肉骨骼，皮肤，呼吸，消化，泌尿和中枢神经系统的炎症，缺血，退行性和增生性疾病的药物。
• Diagnostic/therapeutic agents
  申请人：Klaveness Jo

  公开号：US20050002865A1

  公开（公告）日：2005-01-06

  Targetable diagnostic and/or therapeutically active agents, e.g. ultrasound contrast agents, comprising a suspension in an aqueous carrier liquid of a reporter comprising gas-containing or gas-generating material, said agent being capable of forming at least two types of binding pairs with a target.

  可定位的诊断和/或治疗活性剂，例如超声对比剂，包括悬浮在水载体液中的报告物，该报告物包含含气体或生成气体的材料，该剂能够与目标形成至少两种结合对。
• Breakthrough Pain Management
  申请人：LAB International SRL

  公开号：EP1964564A1

  公开（公告）日：2008-09-03

  The present invention is directed to a powdered formulation comprising an analgesic, preferably fentanyl, for use in pulmonary inhalation administration for the rapid analgesic titration of pain, in particular breakthrough pain. Upon administration, the powdered formulation is able to provide a narrower titration range in patients suffering from pain, as well as effective analgesic amounts of fentanyl in a shorter time and at lower dose levels of administered fentanyl when compared to fentanyl administered by an oral transmucosal route.

  本发明涉及一种粉末状制剂，包含一种镇痛剂，优选芬太尼，用于肺部吸入给药，以快速滴定镇痛剂，特别是突破性疼痛。与通过口腔黏膜给药途径给药的芬太尼相比，本发明的粉末制剂在给药后能够为疼痛患者提供更窄的滴定范围，并能在更短的时间内以更低的芬太尼剂量水平提供有效的芬太尼镇痛量。
• Methods and compositions for the treatment of heart failure and other disorders
  申请人：Ironwood Pharmaceuticals, Inc.

  公开号：EP2650303A1

  公开（公告）日：2013-10-16

  Peptides that act as GC-C receptor agonists and contain at least one D-Cys and are useful for the treatment of diuresis and heart disease as well as other disorders are described.

  本文介绍了作为 GC-C 受体激动剂并含有至少一种 D-Cys 的多肽，这些多肽可用于治疗利尿和心脏病以及其他疾病。