1-acetyl-piperidine-4-carboxylic acid {2-[5-(1,3,3-trimethyl-6-aza-bicyclo-[3.2.1]octane-6-carbonyl)-benzoimidazol-1-yl]-ethyl}-amide | 936347-78-3

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 英文名称: 1-acetyl-piperidine-4-carboxylic acid {2-[5-(1,3,3-trimethyl-6-aza-bicyclo-[3.2.1]octane-6-carbonyl)-benzoimidazol-1-yl]-ethyl}-amide
• 英文别名: 1-acetyl-N-[2-[5-(1,3,3-trimethyl-6-azabicyclo[3.2.1]octane-6-carbonyl)benzimidazol-1-yl]ethyl]piperidine-4-carboxamide
• CAS: 936347-78-3
• 化学式: C₂₈H₃₉N₅O₃
• 分子量: 493.649
• InChiKey: VXNMWEDBVNNDGN-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.6
• 重原子数：
  36
• 可旋转键数：
  5
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.64
• 拓扑面积：
  87.5
• 氢给体数：
  1
• 氢受体数：
  4

文献信息

• PHARMACEUTICAL USE OF SUBSTITUTED AMIDES
  申请人：Kilburn John Paul

  公开号：US20090118259A1

  公开（公告）日：2009-05-07

  The use of substituted amides for modulating the activity of 11-hydroxysteroid dehydrogenase type 1 (11HSD1) 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 11HSD1 and may be useful in the treatment, prevention and/or prophylaxis of a range of medical disorders where a decreased intracellular concentration of active glucocorticoid is desirable.

  使用替代酰胺来调节11-羟基类固醇脱氢酶1（11HSD1）的活性以及将这些化合物用作药物组合物的用途被描述。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。这些化合物是11HSD1活性的调节剂，更具体地是抑制剂，可能在治疗、预防和/或预防一系列需要降低细胞内活性糖皮质激素浓度的医学疾病中有用。
• 11-BETA-HYDROXYSTEROID DEHYDROGENASE TYPE 1 (11BETA-HSD1) INHIBITORS AND USES THEREOF
  申请人：Jacobson Peer B.

  公开号：US20110159005A1

  公开（公告）日：2011-06-30

  A method for treating a patient suffering from inflammation, chronic inflammation, pain, rheumatoid arthritis (RA), osteoarthritis and osteoporosis, comprising administering an effective amount of a selective inhibitor of the 11-β-hydroxysteroid dehydrogenase Type 1 enzyme.
• US8053431B2
  申请人：——

  公开号：US8053431B2

  公开（公告）日：2011-11-08
• US8871208B2
  申请人：——

  公开号：US8871208B2

  公开（公告）日：2014-10-28
• [EN] PHARMACEUTICAL USE OF SUBSTITUTED AMIDES<br/>[FR] UTILISATION PHARMACEUTIQUE D'AMIDES SUBSTITUES
  申请人：NOVO NORDISK AS

  公开号：WO2007051811A2

  公开（公告）日：2007-05-10

  [EN] The use of substituted amides for modulating the activity of 11-hydroxysteroid dehydrogenase type 1 (11HSD1) 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 11HSD1 and may be useful in the treatment, prevention and/or prophylaxis of a range of medical disorders where a decreased intracellular concentration of active glucocorticoid is desirable.
  [FR] L'invention concerne l'utilisation d'amides substitués aux fins de modulation de l'activité de la 11-hydroxystéroïde déshydrogénase de type 1 (11HSD1) et l'utilisation de ces composés comme compositions pharmaceutiques. L'invention concerne également une classe d'amides substitués, l'utilisation de ceux-ci dans un traitement, des compositions pharmaceutiques comprenant les composés et l'utilisation de ceux-ci dans la fabrication de médicaments. Les composés selon l'invention sont des modulateurs et, plus précisément, des inhibiteurs de l'activité de la 11HSD1 et peuvent être utiles dans le traitement, la prévention et/ou la prophylaxie d'une palette de troubles médicaux pour lesquels une concentration intracellulaire diminuée de glucocorticoïde est souhaitée.