6-[3-(2-fluorophenyl)-4-[[[(1R)-1-naphthalen-1-ylethyl]amino]methyl]piperidin-1-yl]pyridine-3-carboxylic acid | 1027712-55-5

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡咯烷类
• 英文名称: 6-[3-(2-fluorophenyl)-4-[[[(1R)-1-naphthalen-1-ylethyl]amino]methyl]piperidin-1-yl]pyridine-3-carboxylic acid
• CAS: 1027712-55-5
• 化学式: C₃₀H₃₀FN₃O₂
• 分子量: 483.586
• InChiKey: QRAIIOMWHWOGIB-UNYPOBEMSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.5
• 重原子数：
  36
• 可旋转键数：
  7
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.27
• 拓扑面积：
  65.5
• 氢给体数：
  2
• 氢受体数：
  6

文献信息

• PIPERIDINE DERIVATIVE OR SALT THEREOF
  申请人：Hachiya Shunichiro

  公开号：US20100029687A1

  公开（公告）日：2010-02-04

  [Problem] To provide a compound which can be used for treating diseases in which a calcium sensing receptor (CaSR) participates, particularly hyperparathyroidism. [Means for Resolution] It was found that a novel piperidine derivative which is characterized in that one of a 3-position and a 4-position is substituted with an aminomethyl group substituted with an arylalkyl group or the like and the other position is substituted with aryl, heteroaryl or the like, or a salt thereof, has an excellent CaSR agonistic regulatory action, and also has excellent selectivity with a CYP2D6 inhibitory action having a possibility of causing drug interaction. Based on the above, this novel piperidine derivative is useful as a therapeutic agent for diseases in which CaSR participates (hyperparathyroidism, renal osteodystrophy, hypercalcemia, and the like).

  【问题】提供一种化合物，可用于治疗钙感受受体（CaSR）参与的疾病，特别是甲状旁腺功能亢进症。【解决方法】发现一种新的哌啶衍生物，其特征在于3位和4位中的一个位置被取代为含有芳基烷基等基团的氨甲基基团，另一个位置被取代为芳基、杂环芳基等，或其盐，具有出色的CaSR激动调节作用，并且具有出色的选择性，具有可能引起药物相互作用的CYP2D6抑制作用。基于以上发现，这种新的哌啶衍生物可用作治疗CaSR参与的疾病（甲状旁腺功能亢进症、肾性骨营养不良、高钙血症等）的治疗剂。
• PIPERIDINE DERIVATIVES OR SALTS THEREOF
  申请人：Astellas Pharma Inc.

  公开号：EP2085383A1

  公开（公告）日：2009-08-05

  [Problem] To provide a compound which can be used for treating diseases in which a calcium sensing receptor (CaSR) participates, particularly hyperparathyroidism. [Means for Resolution] It was found that a novel piperidine derivative which is characterized in that one of a 3-position and a 4-position is substituted with an aminomethyl group substituted with an arylalkyl group or the like and the other position is substituted with aryl, heteroaryl or the like, or a salt thereof, has an excellent CaSR agonistic regulatory action, and also has excellent selectivity with a CYP2D6 inhibitory action having a possibility of causing drug interaction. Based on the above, this novel piperidine derivative is useful as a therapeutic agent for diseases in which CaSR participates (hyperparathyroidism, renal osteodystrophy, hypercalcemia, and the like).

  [问题]提供一种可用于治疗钙传感受体（CaSR）参与的疾病，特别是甲状旁腺机能亢进的化合物。 [解决方法]发现一种新型哌啶衍生物，其特征在于 3 位和 4 位中的一个被氨甲基取代，另一个被芳基、杂芳基等取代，或其盐具有极好的 CaSR 激动调节作用，同时还具有极好的选择性，具有 CYP2D6 抑制作用，但有可能引起药物相互作用。基于以上所述，这种新型哌啶衍生物可作为治疗剂用于治疗 CaSR 参与的疾病（甲状旁腺功能亢进症、肾性骨营养不良症、高钙血症等）。
• US8153658B2
  申请人：——

  公开号：US8153658B2

  公开（公告）日：2012-04-10