4-(5-fluoro-pyrimidin-2-yloxy)-N-(5-hydroxy-adamantan-2-yl)-butyramide | 1076238-72-6

• 分子结构分类: 有机化合物 - 有机氮化合物
• 英文名称: 4-(5-fluoro-pyrimidin-2-yloxy)-N-(5-hydroxy-adamantan-2-yl)-butyramide
• 英文别名: 4-(5-fluoropyrimidin-2-yl)oxy-N-(5-hydroxy-2-adamantyl)butanamide
• CAS: 1076238-72-6
• 化学式: C₁₈H₂₄FN₃O₃
• 分子量: 349.405
• InChiKey: SMCMBUHCBSBVAG-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.4
• 重原子数：
  25
• 可旋转键数：
  6
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.72
• 拓扑面积：
  84.3
• 氢给体数：
  2
• 氢受体数：
  6

文献信息

• PHARMACEUTICAL USE OF SUBSTITUTED AMIDES
  申请人：Ebdrup Soren

  公开号：US20100087543A1

  公开（公告）日：2010-04-08

  The use of substituted amides for modulating the activity of 11β-hydroxysteroid dehydro-genase type 1 (11βHSD1) and the use of these compounds as pharmaceutical composi-tions, are described. Also a novel class of substituted amides, their use in therapy, phar-maceutical compositions comprising the compounds, as well as their use in the manufac-ture 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 gluco-corticoid is desirable.

  本文描述了使用取代酰胺来调节11β-羟基类固醇脱氢酶1型（11βHSD1）的活性以及这些化合物作为药物组合物的用途。还描述了一类新型的取代酰胺，它们在治疗中的用途，包括这些化合物的药物组合物以及它们在制造药物方面的用途。这些化合物是11βHSD1活性的调节剂，更具体地说是抑制剂，可能在治疗一系列需要降低活性糖皮质激素细胞内浓度的医学疾病中有用。
• US8383683B2
  申请人：——

  公开号：US8383683B2

  公开（公告）日：2013-02-26
• [EN] PHARMACEUTICAL USE OF SUBSTITUTED AMIDES<br/>[FR] UTILISATION PHARMACEUTIQUE D'AMIDES SUBSTITUÉS
  申请人：TRANSTECH PHARMA INC

  公开号：WO2008134221A1

  公开（公告）日：2008-11-06

  [EN] The use of substituted amides for modulating the activity of 11ß-hydroxysteroid dehydro-genase type 1 (11ßHSD1) and the use of these compounds as pharmaceutical composi-tions, are described. Also a novel class of substituted amides, their use in therapy, phar-maceutical compositions comprising the compounds, as well as their use in the manufac-ture 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 gluco-corticoid is desirable.
  [FR] L'invention concerne l'utilisation d'amides substitués dans la modulation de l'activité de la 11ß-hydroxystéroïde déshydrogénase de type 1 (11ßHSD1) et l'utilisation desdits composés comme compositions pharmaceutiques. L'invention se rapporte également à une nouvelle classe d'amides substitués, à leur utilisation en thérapie, à des compositions pharmaceutiques comprenant lesdits composés et à l'utilisation de ces derniers dans la fabrication de médicaments. Les composés de l'invention sont des modulateurs et, en particulier, des inhibiteurs de l'activité de 11ßHSD1 et peuvent être utilisés dans le traitement d'une variété de troubles médicaux dans lesquels il est souhaitable d'obtenir une concentration intracellulaire réduite de gluco-corticoïde actif.