5-[(1R,2R,3S,5S)-3-(3,4-dichlorophenyl)-8-methyl-8-azabicyclo[3.2.1]octan-2-yl]-3-pyridin-4-yl-1,2,4-oxadiazole

• 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: 5-[(1R,2R,3S,5S)-3-(3,4-dichlorophenyl)-8-methyl-8-azabicyclo[3.2.1]octan-2-yl]-3-pyridin-4-yl-1,2,4-oxadiazole
• 化学式: C₂₁H₂₀Cl₂N₄O
• 分子量: 415.3
• InChiKey: QCMORAZUTMRXAN-OSGQAZFXSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.6
• 重原子数：
  28
• 可旋转键数：
  3
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  55
• 氢给体数：
  0
• 氢受体数：
  5

文献信息

• Aryl substituted heterocyclic compounds
  申请人：NEUROSEARCH A/S

  公开号：EP0604352A2

  公开（公告）日：1994-06-29

  The present invention discloses compounds of the formula any mixture thereof, or a pharmaceutically acceptable salt thereof; wherein R, R3, and R4 each have the meanings set forth in the specification. The compounds possess valuable pharmaceutical properties as dopamine reuptake inhibitors.

  本发明公开了如下式的化合物 其任何混合物或其药学上可接受的盐； 其中 R、R3 和 R4 各自具有说明书中规定的含义。 这些化合物作为多巴胺再摄取抑制剂具有宝贵的药用特性。
• Pharmaceutical composition comprising a monoamine neurotransmitter re-uptake inhibitor and an acetylcholinesterase inhibitor
  申请人：NeuroSearch AS

  公开号：EP2269608A2

  公开（公告）日：2011-01-05

  The invention relates to a pharmaceutical composition comprising a monoamine neurotransmitter re-uptake inhibitor comprising a 2,3-disubstituted tropane moiety, or a tautomer, a pharmaceutically acceptable salt, solvate, or physiologically functional derivative thereof (1), and at least one acetylcholinesterase inhibitor or a pharmaceutically acceptable salt, solvate, or physiologically functional derivative thereof (2), and a pharmaceutically acceptable carrier or excipient, and optionally one or more other therapeutic ingredients.

  本发明涉及一种药物组合物，该组合物包含一种单胺神经递质再摄取抑制剂，该抑制剂由 2,3-二取代的托烷分子或同系物、其药学上可接受的盐、溶液剂或生理功能衍生物 (1) 以及至少一种乙酰胆碱酯酶抑制剂或其药学上可接受的盐、溶液剂或生理功能衍生物 (2) 组成，还包含一种药学上可接受的载体或赋形剂，以及可选的一种或多种其他治疗成分。
• Tropane derivatives having dopamine reuptake inhibitor activity for the treatment of ischemic diseases
  申请人：Scheel-Kruger Jorgen

  公开号：US20050020621A1

  公开（公告）日：2005-01-27

  The present invention relates to the use of tropane derivatives having dopamine reuptake inhibitor activity for the treatment of diseases associated with reduced blood flow to the brain or with instances of a temporary break in blood supply to the brain, such as ischemic diseases.

  本发明涉及使用具有多巴胺再摄取抑制活性的托烷衍生物治疗与脑血流量减少或脑供血暂时中断有关的疾病，如缺血性疾病。
• Solid pharmaceutical preparation
  申请人：Brauns Ulrich

  公开号：US20050124651A1

  公开（公告）日：2005-06-09

  The invention relates to a solid pharmaceutical preparation containing one or more solid carriers and/or excipients and an active substance selected from among the Monoamine Neurotransmitter Re-uptake Inhibitors which have a 2,3-disubstituted tropane structure, the preparation thereof and use thereof for preparing a pharmaceutical composition for the treatment or prevention of central-nervous diseases or disorders.

  本发明涉及一种固体药物制剂，该制剂含有一种或多种固体载体和/或赋形剂以及一种选自具有 2,3-二取代托烷结构的单胺类神经递质再摄取抑制剂的活性物质，本发明还涉及其制备方法及其在制备治疗或预防中枢神经疾病或紊乱的药物组合物中的用途。
• Pharmaceutical composition comprising a monoamine neurotransmitter re-uptake inhibitor and an N-methyl-D-aspartate (NMDA) receptors antagonist
  申请人：Friedl Thomas

  公开号：US20050182089A1

  公开（公告）日：2005-08-18

  Accordingly, the invention relates to a pharmaceutical composition comprising a monoamine neurotransmitter re-uptake inhibitor comprising a 2,3-disubstituted tropane moiety, or a tautomer, a pharmaceutically acceptable salt, solvate, or physiologically functional derivative thereof, and at least one NMDA receptor antagonists or a pharmaceutically acceptable salt, solvate, or physiologically functional derivative thereof.

  因此，本发明涉及一种药物组合物，该药物组合物包含一种单胺神经递质再摄取抑制剂，该抑制剂由2,3-二取代的托烷分子或同系物、其药学上可接受的盐、溶液剂或生理功能衍生物以及至少一种NMDA受体拮抗剂或其药学上可接受的盐、溶液剂或生理功能衍生物组成。