Asalhydromorphone | 1431529-94-0

• 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: Asalhydromorphone
• 英文别名: [(4R,4aR,7aR,12bS)-9-(2-acetyloxybenzoyl)oxy-3-methyl-2,4,4a,5,7a,13-hexahydro-1H-4,12-methanobenzofuro[3,2-e]isoquinolin-7-yl] 2-acetyloxybenzoate
• CAS: 1431529-94-0
• 化学式: C₃₅H₃₁NO₉
• 分子量: 609.632
• InChiKey: XPLFWDWDCNJVCV-ATPTVOOISA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5
• 重原子数：
  45
• 可旋转键数：
  10
• 环数：
  7.0
• sp3杂化的碳原子比例：
  0.31
• 拓扑面积：
  118
• 氢给体数：
  0
• 氢受体数：
  10

反应信息

• 作为产物：
  描述：

  氢吗啡酮 、 邻乙酰水杨酰氯 在 4-二甲氨基吡啶 、 三乙胺 作用下， 以 二氯甲烷 为溶剂， 生成 Asalhydromorphone
  参考文献：
  名称：

  [EN] IMMEDIATE-RELEASE ABUSE DETERRENT COMPOSITIONS OR MEDICAMENTS FOR TREATING PAIN, ADD, ADHD AND OTHER SYNDROMES OR DISORDERS
  [FR] COMPOSITIONS ANTI-ABUS À LIBÉRATION IMMÉDIATE OU MÉDICAMENTS DESTINÉS AU TRAITEMENT DE LA DOULEUR, DU DCA, DU TDAH, ET D'AUTRES SYNDROMES OU TROUBLES

  摘要：

  目前描述的技术提供了一种或多种组合物，最好是一种或多种立即释放剖面组合物，其中含有与羟考酮（吗啡-6-酮，4,5-α-环氧-3-甲氧基-17-甲基）或与羟吗啡（4,5,α-环氧-3-羟基-17-甲基吗啡-6-酮）化学结合的芳基羧酸，结合至少一种凝胶形成聚合物；至少一种崩解剂；和至少一种表面活性剂，以形成具有减少滥用潜力的新型组合物。羟考酮结合物还可以与镇痛剂（如对乙酰氨基酚）结合，形成包括至少一种凝胶形成聚合物；至少一种崩解剂；和至少一种表面活性剂的组合物。该技术还提供了药物配套组和合成本技术结合物的方法。

  公开号：

  WO2018071879A1

文献信息

• Benzoic acid, benzoic acid derivatives and heteroaryl carboxylic acid conjugates of hydromorphone, prodrugs, methods of making and use thereof
  申请人：KemPharm, Inc.

  公开号：US10441661B2

  公开（公告）日：2019-10-15

  The presently described technology provides compositions comprising aryl carboxylic acids chemically conjugated to hydromorphone (4,5-α-epoxy-3-hydroxy-17-methyl morphinan-6-one) to form novel prodrugs/compositions of hydromorphone. The hydromorphone prodrugs of the present technology have decreased side effects and decreased potential for abuse compared to unconjugated hydromorphone. The present technology also provides methods of treating patients, pharmaceutical kits and methods of synthesizing conjugates of the present technology.

  本技术提供的组合物包含与氢吗啡酮（4,5-α-环氧-3-羟基-17-甲基吗啡烷-6-酮）化学共轭的芳基羧酸，以形成新型的氢吗啡酮原药/组合物。与未结合的氢吗啡酮相比，本技术的氢吗啡酮原药具有更低的副作用和更低的滥用可能性。本技术还提供了治疗病人的方法、医药包和合成本技术共轭物的方法。
• BENZOIC ACID, BENZOIC ACID DERIVATIVES AND HETEROARYL CARBOXYLIC ACID CONJUGATES OF HYDROMORPHONE, PRODRUGS, METHODS OF MAKING AND USE THEREOF
  申请人：KemPharm, Inc.

  公开号：US20130150395A1

  公开（公告）日：2013-06-13

  The presently described technology provides compositions comprising aryl carboxylic acids chemically conjugated to hydromorphone (4,5-α-epoxy-3-hydroxy-17-methyl morphinan-6-one) to form novel prodrugs/compositions of hydromorphone. The hydromorphone prodrugs of the present technology have decreased side effects and decreased potential for abuse compared to unconjugated hydromorphone. The present technology also provides methods of treating patients, pharmaceutical kits and methods of synthesizing conjugates of the present technology.
• Benzoic Acid, Benzoic Acid Derivatives and Heteroaryl Carboxylic Acid Conjugates of Hydromorphone, Prodrugs, Methods of Making and Use Thereof
  申请人：KemPharm, Inc.

  公开号：US20140330021A1

  公开（公告）日：2014-11-06

  The presently described technology provides compositions comprising aryl carboxylic acids chemically conjugated to hydromorphone (4,5-α-epoxy-3-hydroxy-17-methyl morphinan-6-one) to form novel prodrugs/compositions of hydromorphone. The hydromorphone prodrugs of the present technology have decreased side effects and decreased potential for abuse compared to unconjugated hydromorphone. The present technology also provides methods of treating patients, pharmaceutical kits and methods of synthesizing conjugates of the present technology.
• US8816083B2
  申请人：——

  公开号：US8816083B2

  公开（公告）日：2014-08-26
• US9849185B2
  申请人：——

  公开号：US9849185B2

  公开（公告）日：2017-12-26