3-Acetyl-6-ethyl-2-methyl-1H-pyridin4-one | 147330-28-7

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: 3-Acetyl-6-ethyl-2-methyl-1H-pyridin4-one
• 英文别名: 3-Acetyl-6-ethyl-2-methyl-1H-pyridin-4-one
• CAS: 147330-28-7
• 化学式: C₁₀H₁₃NO₂
• 分子量: 179.219
• InChiKey: VOCJVVWKAZSACI-UHFFFAOYSA-N

物化性质

• 沸点：
  316.4±42.0 °C(Predicted)
• 密度：
  1.064±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  1.2
• 重原子数：
  13
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.4
• 拓扑面积：
  46.2
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  3-Acetyl-6-ethyl-2-methyl-1H-pyridin4-one 在 三氯氧磷 、 碳酸氢钠 作用下， 以 水 为溶剂， 反应 8.0h， 生成 1-(4-Chloro-6-ethyl-2-methylpyridin-3-yl)ethanone
  参考文献：
  名称：

  WO2007/100295

  摘要：

  公开号：
• 作为产物：
  描述：

  4-氨基-3-戊烯-2-酮 、 5-(1-hydroxypropylidene)-2,2-dimethyl-[1,3]dioxane-4,6-dione 反应 2.0h， 生成 3-Acetyl-6-ethyl-2-methyl-1H-pyridin4-one
  参考文献：
  名称：

  WO2007/100295

  摘要：

  公开号：

文献信息

• Novel Dual Action Receptors Antagonists (Dara) at the Ati and Eta Receptors
  申请人：Gupta Ramesh Chandra

  公开号：US20100010035A1

  公开（公告）日：2010-01-14

  The present invention relates to new compounds of the formula [Chemical formula should be inserted here. Please see paper copy] wherein R1, R2, R3, and R31 are as specified herein. The invention also relates to a method for preparation thereof, as well as combinations of the new compounds with previously known agents. The invention also relates to the use of the above-mentioned compounds and combinations for the preparation of a medicament for treating hypertension of different kinds, alleviating organ damage of different kinds, treating or preventing diabetic nephropathy, treating endothelin and angiotensin mediated disorders, and treating prostate cancer.

  本发明涉及一种新的化合物，其化学式为[应在此处插入化学式。请参见纸质副本]，其中R1、R2、R3和R31如本文所述。本发明还涉及一种制备该化合物的方法，以及新化合物与先前已知药剂的组合。本发明还涉及上述化合物和组合物的用途，用于制备治疗不同类型的高血压、缓解不同类型的器官损伤、治疗或预防糖尿病肾病、治疗内皮素和血管紧张素介导的疾病以及治疗前列腺癌的药物。
• New nonpeptide angiotensin II receptor antagonists. 3. Synthesis, biological properties, and structure-activity relationships of 2-alkyl-4-(biphenylylmethoxy)pyridine derivatives
  作者：Robert H. Bradbury、Christopher P. Allott、Michael Dennis、J. Alan Girdwood、Peter W. Kenny、John S. Major、Alec A. Oldham、Arnold H. Ratcliffe、Janet E. Rivett

  DOI：10.1021/jm00061a016

  日期：1993.4

  A novel series of nonpeptide angiotensin II (AII) receptor antagonists is reported, derived from linkage of the biphenylyltetrazole moiety found in previously described antagonists via a methyleneoxy chain to the 4-position of a 3-substituted 2,6-dialkylpyridine. When evaluated in an in vitro binding assay using a guinea pig adrenal membrane preparation, compounds in this series generally gave IC50 values in the range 0.005-0.5 muM. A variety of substituents was found to be effective at the 3-position of the pyridine ring. On intravenous administration in a normotensive rat model, the more potent compounds inhibited the AII-induced pressor response with ED50 values in the range 0.1-1.0 mg/kg. One of the compounds, 2-ethyl-5,6,7,8-tetrahydro-4-[2'-(1H-tetrazol-5-yl)biphenyl-4-yl]methoxy}quinoline (26), demonstrated good oral activity in two rat models. At doses in the range 1-10 mg/kg po in AII-infused, conscious, normotensive rats, the compound exhibited a dose-related inhibition of the pressor response with a good duration of action at the higher doses. In a renal hypertensive rat model compound 26 showed a rapid and sustained lowering of blood pressure at a dose of 5 mg/kg po. Based on its profile, this compound, designated ICI D6888, has been selected for evaluation in volunteers.
• 4-BENZYLAMINOCHINOLINE KONJUGATE MIT GALLENSAEURE UND IHRE HETEROANALOGEN, VERFAHREN ZU IHRER HERSTELLUNG, DIESE VERBINDUNGEN ENTHALTENDE ARZNEIMITTEL UND DEREN ANWENDUNG
  申请人：Aventis Pharma Deutschland GmbH

  公开号：EP1218401A1

  公开（公告）日：2002-07-03
• NOVEL DUAL ACTION RECEPTORS ANTAGONISTS (DARA) AT THE ATI AND ETA RECEPTORS
  申请人：Torrent Pharmaceuticals Ltd

  公开号：EP1996588A1

  公开（公告）日：2008-12-03
• US6339077B1
  申请人：——

  公开号：US6339077B1

  公开（公告）日：2002-01-15