(3-phenylpyrrolidin-1-yl)-[5-(1H-pyrazol-4-yl)thiophen-3-yl]methanone | 1187467-34-0

• 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: (3-phenylpyrrolidin-1-yl)-[5-(1H-pyrazol-4-yl)thiophen-3-yl]methanone
• CAS: 1187467-34-0
• 化学式: C₁₈H₁₇N₃OS
• 分子量: 323.418
• InChiKey: TUJSOMCBXCTPBS-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.9
• 重原子数：
  23
• 可旋转键数：
  3
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.22
• 拓扑面积：
  77.2
• 氢给体数：
  1
• 氢受体数：
  3

文献信息

• Amido-Thiophene Compounds and Their Use
  申请人：Webster Scott Peter

  公开号：US20130012545A1

  公开（公告）日：2013-01-10

  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.

  本发明通常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，其在其他方面抑制11β-羟化固醇脱氢酶1型（11β-HSD1）。本发明还涉及包括这些化合物的制药组合物，并且在体内外使用这些化合物和组合物来抑制11β-羟化固醇脱氢酶1型；治疗通过抑制11β-羟化固醇脱氢酶1型改善的疾病；治疗代谢综合征，包括2型糖尿病和肥胖症等疾病，以及相关疾病，包括胰岛素抵抗、高血压、脂质代谢紊乱和缺血性（冠状动脉）心脏病等心血管疾病；治疗CNS疾病，如轻度认知障碍和早期痴呆，包括阿尔茨海默病等。
• AMIDO-THIOPHENE COMPOUNDS AND THEIR USE
  申请人：THE UNIVERSITY OF EDINBURGH

  公开号：EP2283004B1

  公开（公告）日：2015-05-27
• US8299063B2
  申请人：——

  公开号：US8299063B2

  公开（公告）日：2012-10-30