1-Phenyl-2-propanamine-D-glucaric acid (1:1) | 300666-46-0

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: 1-Phenyl-2-propanamine-D-glucaric acid (1:1)
• 英文别名: 1-phenylpropan-2-amine;(2S,3S,4S,5R)-2,3,4,5-tetrahydroxyhexanedioic acid
• CAS: 300666-46-0
• 化学式: C15H23NO8
• 分子量: 345.34
• InChiKey: VHKVKWTWHZUFIA-BHTRDKFFSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -1.82
• 重原子数：
  24
• 可旋转键数：
  7
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.47
• 拓扑面积：
  182
• 氢给体数：
  7
• 氢受体数：
  9

文献信息

• AMPHETAMINE CONTROLLED RELEASE, PRODRUG, AND ABUSE-DETERRENT DOSAGE FORMS
  申请人：CHEMAPOTHECA, LLC

  公开号：US20180243241A1

  公开（公告）日：2018-08-30

  The invention also relates to pharmaceutical compositions comprising highly pure amphetamine and amphetamine-class compounds resulting from the synthesis of chiral and racemic amphetamine derivatives by stereospecific, regioselective cuprate addition reaction with aziridine phosphoramidate compounds, and to methods of manufacturing, delivering, and using the amphetamine compounds resulting from the synthesis of chiral and racemic amphetamine derivatives by stereospecific, regioselective cuprate addition reaction with aziridine phosphoramidate compounds.

  这项发明还涉及包含高纯度苯丙胺和苯丙胺类化合物的药物组合物，这些化合物是通过对手性和消旋苯丙胺衍生物进行立体特异性、区域选择性的杯酸盐加成反应与环氧乙烷磷酰胺化合物合成而得到的，并且涉及通过对手性和消旋苯丙胺衍生物进行立体特异性、区域选择性的杯酸盐加成反应与环氧乙烷磷酰胺化合物合成而得到的苯丙胺化合物的制造、输送和使用方法。
• [EN] AMPHETAMINE CONTROLLED RELEASE, PRODRUG, AND ABUSE DETERRENT DOSAGE FORMS<br/>[FR] LIBÉRATION CONTRÔLÉE DE L'AMPHÉTAMINE, PROMÉDICAMENT ET FORMES POSOLOGIQUES DISSUASIVES DU MÉSUSAGE
  申请人：CHEMAPOTHECA LLC

  公开号：WO2017147375A1

  公开（公告）日：2017-08-31

  The invention also relates to pharmaceutical compositions comprising highly pure amphetamine and amphetamine-class compounds resulting from the synthesis of chiral and racemic amphetamine derivatives by stereospecific, regioselective cuprate addition reaction with aziridine phosphoramidate compounds, and to methods of manufacturing, delivering, and using the amphetamine compounds resulting from the synthesis of chiral and racemic amphetamine derivatives by stereospecific, regioselective cuprate addition reaction with aziridine phosphoramidate compounds.

  这项发明还涉及包含高纯度苯丙胺和苯丙胺类化合物的药物组合物，这些化合物是通过对手性和消旋苯丙胺衍生物进行立体特异性、区域选择性的杯酸盐加成反应与环氧乙烷磷酰胺化合物合成的，以及通过对手性和消旋苯丙胺衍生物进行立体特异性、区域选择性的杯酸盐加成反应与环氧乙烷磷酰胺化合物合成的苯丙胺化合物的制造、输送和使用方法。
• [EN] ABUSE RESISTANT AMPHETAMINE COMPOUNDS<br/>[FR] COMPOSES D'AMPHETAMINE RESISTANT AUX ABUS
  申请人：NEW RIVER PHARMACEUTICALS INC

  公开号：WO2005000334A1

  公开（公告）日：2005-01-06

  The invention describes compounds, compositions and methods of using the same comprising a chemical moiety covalently attached to amphetamine. These compounds and compositions are useful for reducing or preventing abuse and overdose of amphetamine. These compounds and compositions find particular use in providing an abuse-resistant alternative treatment for certain disorders, such as attention deficit hyperactivity disorder (ADHD), ADD, narcolepsy, and obesity. Oral bioavailability of amphetamine is maintained at therapeutically useful doses. At higher doses bioavailability is substantially reduced, thereby providing a method of reducing oral abuse liability. Further, compounds and compositions of the invention decrease the bioavailability of amphetamine by parenteral routes, such as intravenous or intranasal administration, further limiting their abuse liability.

  本发明涉及一种将化学基团共价连接到苯丙胺的化合物、组合物和使用方法。这些化合物和组合物可用于减少或预防苯丙胺的滥用和过量使用。这些化合物和组合物在为某些疾病提供抗滥用替代治疗方面具有特殊用途，例如注意力缺陷多动障碍（ADHD）、ADD、嗜睡症和肥胖症。在治疗上，苯丙胺的口服生物利用度保持在治疗上有用的剂量。在更高剂量下，生物利用度显著降低，从而提供了一种减少口服滥用风险的方法。此外，本发明的化合物和组合物通过静脉或鼻腔给药等肌肉注射途径进一步降低苯丙胺的生物利用度，从而进一步限制其滥用风险。
• Abuse resistant lysine amphetamine compounds
  申请人：Mickle Travis

  公开号：US20050038121A1

  公开（公告）日：2005-02-17

  The present invention describes compounds, compositions and methods of using the same comprising lysine covalently attached to amphetamine. These compounds and compositions are useful for reducing or preventing abuse and overdose of amphetamine. These compounds and compositions find particular use in providing an abuse-resistant alternative treatment for certain disorders, such as attention deficit hyperactivity disorder (ADHD), ADD, narcolepsy, and obesity. Oral bioavailability of amphetamine is maintained at therapeutically useful doses. At higher doses bioavailability is substantially reduced, thereby providing a method of reducing oral abuse liability. Further, compounds and compositions of the invention decrease the bioavailability of amphetamine by parenteral routes, such as intravenous or intranasal administration, further limiting their abuse liability.

  本发明描述了一种将赖氨酸共价连接到苯丙胺的化合物、组合物和使用方法。这些化合物和组合物有助于减少或预防苯丙胺的滥用和过量使用。这些化合物和组合物在提供一种抗滥用替代治疗某些疾病时特别有用，例如注意力缺陷多动障碍（ADHD）、ADD、嗜睡症和肥胖症。在治疗剂量下，苯丙胺的口服生物利用度得以维持。在更高剂量下，生物利用度显著降低，从而提供了一种减少口服滥用风险的方法。此外，本发明的化合物和组合物通过肌肉注射或鼻腔给药等静脉或鼻腔途径，进一步降低苯丙胺的生物利用度，从而限制了它们的滥用风险。
• ABUSE RESISTANT LYSINE AMPHETAMINE COMPOUNDS
  申请人：Mickle Travis

  公开号：US20100105781A1

  公开（公告）日：2010-04-29

  The present invention describes compounds, compositions and methods of using the same comprising lysine covalently attached to amphetamine. These compounds and compositions are useful for reducing or preventing abuse and overdose of amphetamine. These compounds and compositions find particular use in providing an abuse-resistant alternative treatment for certain disorders, such as attention deficit hyperactivity disorder (ADHD), ADD, narcolepsy, and obesity. Oral bioavailability of amphetamine is maintained at therapeutically useful doses. At higher doses bioavailability is substantially reduced, thereby providing a method of reducing oral abuse liability. Further, compounds and compositions of the invention decrease the bioavailability of amphetamine by parenteral routes, such as intravenous or intranasal administration, further limiting their abuse liability.

  本发明描述了化合物、组合物及其使用方法，其中赖氨酸共价连接到苯丙胺。这些化合物和组合物有助于减少或预防苯丙胺的滥用和过量使用。这些化合物和组合物在提供某些疾病的耐受性治疗方面特别有用，如注意力缺陷多动障碍（ADHD）、ADD、嗜睡病和肥胖症。在治疗剂量下，苯丙胺的口服生物利用度得以维持。在更高剂量下，生物利用度显著降低，从而提供了一种减少口服滥用风险的方法。此外，本发明的化合物和组合物通过肌肉注射或鼻腔给药等非口服途径降低苯丙胺的生物利用度，进一步限制了它们的滥用风险。