N-cyclopropyl-N-(2,3,4,5,6,7-hexahydro-1H-indazol-5-yl)-4-pyrimidin-5-ylbenzamide

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪类
• 英文名称: N-cyclopropyl-N-(2,3,4,5,6,7-hexahydro-1H-indazol-5-yl)-4-pyrimidin-5-ylbenzamide
• 化学式: C₂₁H₂₃N₅O
• 分子量: 361.4
• InChiKey: WBZXZZHLAIZSIV-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2
• 重原子数：
  27
• 可旋转键数：
  4
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  70.2
• 氢给体数：
  2
• 氢受体数：
  5

文献信息

• BICYCLIC HETEROCYCLIC COMPOUND
  申请人：Astellas Pharma Inc.

  公开号：EP2772484A1

  公开（公告）日：2014-09-03

  [Problem] To provide a compound useful as an active ingredient of a pharmaceutical composition for treating 11β-hydroxysteroid dehydrogenase type 1-related diseases such as dementia, schizophrenia, depression, pain (particularly, neuropathic pain or fibromyalgia), diabetes (particularly, type II diabetes mellitus), insulin resistance and the like. [Means for Solution] A bicyclic heterocyclic compound (the bicyclic heterocycle is formed when a cyclohexane ring is fused with a 5- to 6-membered monocyclic heterocycle that has only a nitrogen atom as a hetero atom) substituted with an acylamino group such as a (hetero)aroylamino group or the like or a pharmaceutically acceptable salt thereof was found to have an excellent selective inhibitory action against 11β-HSD1. Accordingly, the bicyclic heterocyclic compound of the present invention can be used for treating dementia, schizophrenia, depression, pain (particularly, neuropathic pain or fibromyalgia), diabetes (particularly, type II diabetes mellitus), insulin resistance, and the like.

  [问题]提供一种化合物，作为药物组合物的有效成分，用于治疗与11β-羟基类固醇脱氢酶1型相关的疾病，如痴呆症、精神分裂症、抑郁症、疼痛（尤其是神经性疼痛或纤维肌痛）、糖尿病（尤其是II型糖尿病）、胰岛素抵抗等。 [解决方法]研究发现，一种被酰氨基如（杂）酰氨基或类似基团取代的双环杂环化合物（双环杂环由环己烷环与仅有一个氮原子作为杂原子的 5 至 6 元单环杂环融合而成）或其药学上可接受的盐对 11β-HSD1 具有极好的选择性抑制作用。因此，本发明的双环杂环化合物可用于治疗痴呆症、精神分裂症、抑郁症、疼痛（尤其是神经性疼痛或纤维肌痛）、糖尿病（尤其是II型糖尿病）、胰岛素抵抗等。