1,3-dimethyl-3-[4-(2-oxa-5-azabicyclo[2.2.1]heptane-5-carbonyl)-benzyl]-1-pyridin-2-yl-urea | 936019-62-4

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 恶嗪烷类
• 英文名称: 1,3-dimethyl-3-[4-(2-oxa-5-azabicyclo[2.2.1]heptane-5-carbonyl)-benzyl]-1-pyridin-2-yl-urea
• 英文别名: 1,3-Dimethyl-1-[[4-(2-oxa-5-azabicyclo[2.2.1]heptane-5-carbonyl)phenyl]methyl]-3-pyridin-2-ylurea
• CAS: 936019-62-4
• 化学式: C₂₁H₂₄N₄O₃
• 分子量: 380.447
• InChiKey: CIWQEPQIFKTSCH-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.4
• 重原子数：
  28
• 可旋转键数：
  4
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  66
• 氢给体数：
  0
• 氢受体数：
  4

文献信息

• PHARMACEUTICAL USE OF SUBSTITUTED AMIDES
  申请人：Andersen Henrik Sune

  公开号：US20090124598A1

  公开（公告）日：2009-05-14

  The use of substituted amides for modulating the activity of 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) and the use of these compounds as pharmaceutical compositions, are described. Also a novel class of substituted amides, their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments are described. The present compounds are modulators and more specifically inhibitors of the activity of 11βHSD1 and may be useful in the treatment of a range of medical disorders where a decreased intracellular concentration of active glucocorticoid is desirable.

  描述了使用替代酰胺来调节11β-羟基类固醇脱氢酶1（11βHSD1）活性以及将这些化合物用作药物组合物的用途。还描述了一类新型的替代酰胺，它们在治疗中的应用，包含这些化合物的药物组合物，以及它们在制造药物中的应用。目前的化合物是11βHSD1活性的调节剂，更具体地是抑制剂，并且可能在治疗一系列医学疾病中有用，其中降低细胞内活性糖皮质激素浓度是可取的。
• [EN] PHARMACEUTICAL USE OF SUBSTITUTED AMIDES<br/>[FR] UTILISATION PHARMACEUTIQUE D'AMIDES SUBSTITUES
  申请人：NOVO NORDISK AS

  公开号：WO2007051810A2

  公开（公告）日：2007-05-10

  [EN] The use of substituted amides for modulating the activity of 11ß-hydroxysteroid dehydrogenase type 1 (11ßHSD1) and the use of these compounds as pharmaceutical compositions, are described. Also a novel class of substituted amides, their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments are described. The present compounds are modulators and more specifically inhibitors of the activity of 11ßHSD1 and may be useful in the treatment of a range of medical disorders where a decreased intracellular concentration of active glucocorticoid is desirable.
  [FR] La présente invention concerne l'utilisation d'amides substitués pour moduler l'activité de la 11ß-hydroxystéroïde deshydrogénase de type 1 (11ßHSD1) et l'utilisation de ces composés en tant que compositions pharmaceutiques. Cette invention concerne également une nouvelle classe d'amides substitués, leur utilisation à des fins thérapeutiques, des compositions pharmaceutiques comprenant des composés, ainsi que leur utilisation dans la fabrication de médicaments. Les composés décrits dans cette invention sont des modulateurs et plus spécifiquement des inhibiteurs de l'activité de la 11ßHSD1 et ils peuvent être utilisés pour traiter un éventail de pathologies pour lesquelles une concentration intracellulaire réduite de glucocorticoïde actif est souhaitable.