[5-(2-Methylphenyl)thiophen-3-yl]-piperidin-1-ylmethanone | 1187466-45-0

• 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: [5-(2-Methylphenyl)thiophen-3-yl]-piperidin-1-ylmethanone
• CAS: 1187466-45-0
• 化学式: C₁₇H₁₉NOS
• 分子量: 285.41
• InChiKey: NGMXDEGZIOBCOG-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.9
• 重原子数：
  20
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.35
• 拓扑面积：
  48.6
• 氢给体数：
  0
• 氢受体数：
  2

文献信息

• [EN] AMIDO-THIOPHENE COMPOUNDS AND THEIR USE<br/>[FR] COMPOSÉS AMIDO-THIOPHÈNE ET LEUR UTILISATION
  申请人：UNIV EDINBURGH

  公开号：WO2009112845A1

  公开（公告）日：2009-09-17

  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 11 β-hydroxysteroid dehydrogenase type 1 (11 β-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 11 β-hydroxysteroid dehydrogenase type 1; to treat disorders that are ameliorated by the inhibition of 11 β-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.

  本发明一般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（11β-HSD1）的作用。本发明还涉及包含这些化合物的药物组合物，以及使用这些化合物和组合物，在体内和体外，抑制11β-羟基类固醇脱氢酶1；治疗通过抑制11β-羟基类固醇脱氢酶1而得到改善的疾病；治疗代谢综合征，其中包括糖尿病和肥胖等疾病，以及相关疾病，包括胰岛素抵抗、高血压、脂质紊乱和心血管疾病，如缺血性（冠状）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。
• 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
• [EN] A CELLULAR DRUG SCREENING METHOD USING FACS AND LC-MS.<br/>[FR] PROCÉDÉ CELLULAIRE DE CRIBLAGE DE MÉDICAMENTS À L'AIDE DU TRI DE CELLULES ACTIVÉES PAR FLUORESCENCE ET DU COUPLAGE CHROMATOGRAPHIE LIQUIDE-SPECTROMÉTRIE DE MASSE
  申请人：UNIV EDINBURGH

  公开号：WO2015082900A1

  公开（公告）日：2015-06-11

  Described herein are new methods for the rapid screening of compounds for a multiplicity of parameters in a single stage. More particularly, there is provided a novel screening method for the assessment of protein binding, cellular permeability and cytotoxicity of compounds in a single stage.