(2S,3R)-3-(4-fluorophenyl)-N-methoxy-N,8-dimethyl-8-azabicyclo[3.2.1]octane-2-carboxamide

• 分子结构分类: 有机化合物 - 生物碱及其衍生物 - 托烷生物碱
• 英文名称: (2S,3R)-3-(4-fluorophenyl)-N-methoxy-N,8-dimethyl-8-azabicyclo[3.2.1]octane-2-carboxamide
• 化学式: C₁₇H₂₃FN₂O₂
• 分子量: 306.37
• InChiKey: CZGFBAOBZNKZBU-GRAKBVBRSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.4
• 重原子数：
  22
• 可旋转键数：
  3
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.59
• 拓扑面积：
  32.8
• 氢给体数：
  0
• 氢受体数：
  4

文献信息

• Therapeutic tropane compounds
  申请人：——

  公开号：US20030125352A1

  公开（公告）日：2003-07-03

  This invention relates to therapeutic uses of boat tropane analogs, e.g, treatment of neurodegenerative disorders. More specifically the invention relates to a method of treating a neurological disorder in patient comprising administering to the patient an effective amount of a boat tropane compound.

  本发明涉及船形异钾烷类似物的治疗用途，例如治疗神经退行性疾病。更具体地，本发明涉及一种治疗患者神经系统疾病的方法，包括向患者施用有效量的船形异钾烷化合物。
• Intermediates for the synthesis of radiolabelled tropanes
  申请人：PRESIDENT AND FELLOWS OF HARVARD COLLEGE

  公开号：EP1238978A2

  公开（公告）日：2002-09-11

  The compounds of the present invention comprise a tropane compound or ligand that selectively binds to tropane recognition sites, e.g., neuron transporters such as that DAT. The tropane ligand is radiolabeled with a radioactive technetium or rhenium by a chelating ligand which is attached to the tropane ligand by a linker. Tropane compounds or ligands useful in the pratice of the present invention can generally be represented by formula II where R1 and R2 are defined as above and where R1 can also be substituted at the C4 position of the tropane ring: Any tropane compound of the general formula II is useful in the present invention so long as it binds to DAT. Useful tropane analogs have a 3α-group,i.e., are of the boat configuration. Intermediates for the synthesis of the radiolabeled tropanes are claimed.

  本发明的化合物包括一种选择性地结合到对氮杂环戊烷识别位点（如神经元转运体，如 DAT）的对氮杂环戊烷化合物或配体。通过螯合配体对托烷配体进行放射性锝或铼标记，螯合配体通过连接体连接到托烷配体上。 在本发明实践中有用的托烷化合物或配体一般可用式 II 表示，其中 R1 和 R2 的定义如上，R1 也可以在托烷环的 C4 位被取代： 只要能与 DAT 结合，通式 II 的任何托烷化合物在本发明中都是有用的。 有用的托烷类似物具有 3α 基团，即具有舟形构型。本发明要求合成放射性标记的托烷的中间体。
• Boat tropanes
  申请人：——

  公开号：US20020131931A1

  公开（公告）日：2002-09-19

  Radiopharmaceutical compounds are disclosed. A tropane compound is linked through the N atom at the 8-position to a chelating ligand capable of complexing technetium or rhenium to produce a neutral labeled complex that selectively binds to the dopamine transporter over the serotonin transporter with a ratio of 10 or more. These compounds can be prepared as separate diastereoisomers as well as a mixture of diastereoisomers. Also disclosed are radiopharmaceutical kits for preparing the labeled radiopharmaceutical compounds.

  本发明公开了放射性药物复合物。一种托烷化合物通过 8 位上的 N 原子与一种能与锝或铼络合的螯合配体相连，从而产生一种中性标记的复合物，该复合物能选择性地与多巴胺转运体结合，而与血清素转运体的结合比例为 10 或更高。这些化合物既可以制备成单独的非对映异构体，也可以制备成非对映异构体的混合物。还公开了用于制备标记放射性药物化合物的放射性药物试剂盒。
• Dopamine transporter imaging agents
  申请人：President and Fellows of Harvard College

  公开号：EP1051980B1

  公开（公告）日：2010-12-15
• US6548041B1
  申请人：——

  公开号：US6548041B1

  公开（公告）日：2003-04-15