(2R)-6-[(4-甲氧基苯基)磺酰基甲基]-N,N-二丙基-1,2,3,4-四氢萘-2-胺 | 175442-95-2

• 分子结构分类: 有机化合物 - 苯类化合物 - 四氢化萘
• 中文名称: (2R)-6-[(4-甲氧基苯基)磺酰基甲基]-N,N-二丙基-1,2,3,4-四氢萘-2-胺
• 英文名称: GR 218231
• 英文别名: (2R)-6-[(4-methoxyphenyl)sulfonylmethyl]-N,N-dipropyl-1,2,3,4-tetrahydronaphthalen-2-amine
• CAS: 175442-95-2
• 化学式: C₂₄H₃₃NO₃S
• 分子量: 415.597
• InChiKey: HUXFXXWYIRBVJR-JOCHJYFZSA-N

物化性质

• 熔点：
  97 °C
• 沸点：
  585.0±50.0 °C(Predicted)
• 密度：
  1.16±0.1 g/cm3(Predicted)
• 溶解度：
  DMSO:~24 mg/mLat 60 °C,soluble

计算性质

• 辛醇/水分配系数(LogP)：
  5.2
• 重原子数：
  29
• 可旋转键数：
  9
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  55
• 氢给体数：
  0
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  6-溴-2-四氢萘酮 在 palladium on activated charcoal Oxone 、 氯化亚砜 、 甲酸铵 、 三乙酰氧基硼氢化钠 、 sodium carbonate 、 溶剂黄146 作用下， 以 二氯甲烷 、 水 、 异丙醇 为溶剂， 生成 (2R)-6-[(4-甲氧基苯基)磺酰基甲基]-N,N-二丙基-1,2,3,4-四氢萘-2-胺
  参考文献：
  名称：

  Novel 6-substituted 2-aminotetralins with potent and selective affinity for the dopamine D3 receptor

  摘要：

  Starting from (1S,2R)-5-methoxy-1-methyl-2-N,N-dipropylaminotetralin [(+)-UH-232] as a lead structure, a series of novel 6-substituted 2-aminotetralins have been discovered which show high affinity for dopamine D-3 receptors. One compound, GR218231, exhibits ca. 400 fold selectivity for the dopamine D-3 receptor over the D-2 receptor and ca. 10,000 fold selectivity with respect to D-1 and D-4 receptors.

  DOI：

  10.1016/0960-894x(96)00043-1

文献信息

• Novel D3 Dopamine Receptor Agonists to Treat Dyskinesia in Parkinson's Disease
  申请人：College of Medicine Philadelphia Health & Education Corporation d/b/a Drexel University

  公开号：US20140228355A1

  公开（公告）日：2014-08-14

  The present invention provides a method of inhibiting, suppressing or preventing levodopa-induced dyskinesia in a patient suffering from Parkinson's Disease, comprising the step of administering to the patient a pharmaceutical composition comprising at least one compound of the invention. The present invention further provides a method of inhibiting, suppressing or preventing Parkinson's Disease in a patient, comprising the step of administering to the patient a pharmaceutical composition comprising at least one compound of the invention.

  本发明提供了一种方法，用于抑制、抑制或预防帕金森病患者的左旋多巴诱发的运动障碍，包括向患者给予至少一种本发明化合物的药物组合物。本发明还提供了一种方法，用于抑制、抑制或预防帕金森病患者的病情，包括向患者给予至少一种本发明化合物的药物组合物。
• D3 dopamine receptor agonists to treat dyskinesia in Parkinson's disease
  申请人：DREXEL UNIVERSITY

  公开号：US10543180B2

  公开（公告）日：2020-01-28

  The present invention provides a method of inhibiting, suppressing or preventing levodopa-induced dyskinesia in a patient suffering from Parkinson's Disease, comprising the step of administering to the patient a pharmaceutical composition comprising at least one compound of the invention. The present invention further provides a method of inhibiting, suppressing or preventing Parkinson's Disease in a patient, comprising the step of administering to the patient a pharmaceutical composition comprising at least one compound of the invention.

  本发明提供了一种抑制、抑制或预防帕金森病患者左旋多巴诱发的运动障碍的方法，包括向患者施用包含至少一种本发明化合物的药物组合物的步骤。本发明进一步提供了一种抑制、抑制或预防患者帕金森病的方法，包括向患者施用包含至少一种本发明化合物的药物组合物的步骤。
• ARYLSULFONYLMETHYL OR ARYLSULFONAMIDE SUBSTITUTED AROMATIC COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MODULATION OF THE DOPAMINE D3 RECEPTOR
  申请人：Abbott GmbH & Co. KG

  公开号：EP1812416B1

  公开（公告）日：2013-08-21
• Arylsulfonylmethyl or arylsulfonamide substituted aromatic compounds suitable for treating disorders that respond to modulation of the dopamine D3 receptor
  申请人：AbbVie Deutschland GmbH & Co KG

  公开号：EP2439203B1

  公开（公告）日：2014-11-19
• NOVEL D3 DOPAMINE RECEPTOR AGONISTS TO TREAT DYSKINESIA IN PARKINSON'S DISEASE
  申请人：Philadelphia Health and Education Corporation

  公开号：EP2603215A2

  公开（公告）日：2013-06-19