[5-[(4-Imidazol-1-ylphenoxy)methyl]thiophen-3-yl]-piperidin-1-ylmethanone | 1160718-60-4

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: [5-[(4-Imidazol-1-ylphenoxy)methyl]thiophen-3-yl]-piperidin-1-ylmethanone
• CAS: 1160718-60-4
• 化学式: C₂₀H₂₁N₃O₂S
• 分子量: 367.472
• InChiKey: NRDRBHMOESICLS-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.2
• 重原子数：
  26
• 可旋转键数：
  5
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.3
• 拓扑面积：
  75.6
• 氢给体数：
  0
• 氢受体数：
  4

文献信息

• Amido-Thiophene Compounds and Their Use as 11-Beta-HSD1 Inhibitors
  申请人：Webster Scott Peter

  公开号：US20100267696A1

  公开（公告）日：2010-10-21

  The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain amido-thiophene compounds that, inter alia, inhibit 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit 11β-hydroxysteroid dehydrogenase type 1; to treat disorders that are ameliorated by the inhibition of 11β-hydroxysteroid dehydrogenase type 1; to treat the metabolic syndrome, which includes disorders such as type 2 diabetes and obesity, and associated disorders including insulin resistance, hypertension, lipid disorders and cardiovascular disorders such as ischaemic (coronary) heart disease; to treat CNS disorders such as mild cognitive impairment and early dementia, including Alzheimer's disease; etc.

  本发明涉及治疗化合物领域。更具体地，本发明涉及某些酰胺噻吩化合物，其中包括抑制11β-羟基类固醇脱氢酶1型（11β-HSD1）的化合物。本发明还涉及包含这种化合物的制药组合物，以及在体内外使用这种化合物和组合物来抑制11β-羟基类固醇脱氢酶1型，治疗通过抑制11β-羟基类固醇脱氢酶1型改善的疾病，治疗代谢综合征，包括2型糖尿病和肥胖症，以及相关疾病，包括胰岛素抵抗、高血压、脂质异常和缺血性（冠状动脉）心脏病；治疗中枢神经系统疾病，如轻度认知障碍和早期痴呆，包括阿尔茨海默病等。
• US8362008B2
  申请人：——

  公开号：US8362008B2

  公开（公告）日：2013-01-29