1-[4-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]octane-6-carbonyl)-phenyl]-pyrrolidine-3-carboxylic acid methyl ester | 1002097-79-1

• 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: 1-[4-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]octane-6-carbonyl)-phenyl]-pyrrolidine-3-carboxylic acid methyl ester
• 英文别名: methyl 1-[4-(1,3,3-trimethyl-6-azabicyclo[3.2.1]octane-6-carbonyl)phenyl]pyrrolidine-3-carboxylate
• CAS: 1002097-79-1
• 化学式: C₂₃H₃₂N₂O₃
• 分子量: 384.519
• InChiKey: URCFPFAWFJXPNY-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  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：
  0.65
• 拓扑面积：
  49.8
• 氢给体数：
  0
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  1-[4-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]octane-6-carbonyl)-phenyl]-pyrrolidine-3-carboxylic acid methyl ester 在 sodium hydroxide 、 水 、 盐酸 作用下， 以 乙醇 、 水 为溶剂， 反应 4.0h， 以73%的产率得到1-[4-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]octane-6-carbonyl)-phenyl]-pyrrolidine-3-carboxylic acid
  参考文献：
  名称：

  WO2008/6702

  摘要：

  公开号：
• 作为产物：
  描述：

  [4-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]-octane-6-carbonyl)-phenylamino]-acetic acid 、 丙烯酸甲酯（MA） 在 聚合甲醛 作用下， 以 甲苯 为溶剂， 反应 19.0h， 以52%的产率得到1-[4-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]octane-6-carbonyl)-phenyl]-pyrrolidine-3-carboxylic acid methyl ester
  参考文献：
  名称：

  WO2008/6702

  摘要：

  公开号：

文献信息

• 11BETA-HYDROXYSTEROID DEHYDROGENASE TYPE 1 ACTIVE COMPOUNDS
  申请人：Ebdrup Soren

  公开号：US20100009968A1

  公开（公告）日：2010-01-14

  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, of the general formula I. 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 11βHSDI and may be useful in the treatment of a range of medical disorders where a decreased intracellular concentration of active glucocorticoid 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）活性的方法，以及这些化合物作为药物组成物的用途。还介绍了一类新型的取代酰胺，其一般式为I。描述了它们在治疗中的应用、包含这些化合物的药物组成物，以及它们在制造药物方面的用途。这些化合物是11βHSDI活性的调节剂，更具体地说是抑制剂，可能在治疗需要降低细胞内活性糖皮质激素浓度的一系列医学疾病中有用。
• 11β-hydroxysteroid dehydrogenase type 1 active compounds
  申请人：High Point Pharmaceuticals, LLC

  公开号：US08048908B2

  公开（公告）日：2011-11-01

  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, of the general formula I. 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 11βHSDI and may be useful in the treatment of a range of medical disorders where a decreased intracellular concentration of active glucocorticoid 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）活性的方法，并将这些化合物用作制药组合物。同时，本文还描述了一类新型的取代酰胺，其一般式为I。这些化合物在治疗中的应用、制药组合物的含量以及它们在药物制造中的应用也被描述。这些化合物是11βHSDI活性的调节剂，更具体地说是抑制剂，它们可能在治疗需要降低细胞内活性糖皮质激素浓度的一系列医学疾病中有用。
• 11-Beta-Hydroxysteroid Dehydrogenase Type 1 Active Compounds
  申请人：Ebdrup Soren

  公开号：US20120010194A1

  公开（公告）日：2012-01-12

  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, of the general formula I. 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 11βHSDI and may be useful in the treatment of a range of medical disorders where a decreased intracellular concentration of active glucocorticoid is desirable.

  本文描述了使用取代酰胺来调节11β-羟化甾酮脱氢酶1型（11βHSD1）的活性，以及这些化合物作为药物组成物的用途。同时，还描述了一种新型的取代酰胺类化合物，其通式为I。本文还介绍了这些化合物在治疗中的应用、包含这些化合物的药物组成物，以及它们在制造药物方面的应用。这些化合物是11βHSDI的调节剂，更具体地说是抑制剂，并且在需要降低细胞内活性糖皮质激素浓度的一系列医学疾病的治疗中可能有用。
• 11-beta-hydroxysteroid dehydrogenase type 1 active compounds
  申请人：Ebdrup Soren

  公开号：US08383668B2

  公开（公告）日：2013-02-26

  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, of the general formula I. 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 11βHSDI and may be useful in the treatment of a range of medical disorders where a decreased intracellular concentration of active glucocorticoid 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）活性的方法，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，其通式为I。本文还描述了这些化合物在治疗中的应用、包含这些化合物的药物组合物，以及它们在药物制剂制造中的应用。这些化合物是11βHSDI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细胞内活性糖皮质激素浓度的医学疾病中有用。
• US8048908B2
  申请人：——

  公开号：US8048908B2

  公开（公告）日：2011-11-01