(4-hydroxy-2,6-dimethyl-[3]pyridyl)-phenyl ketone

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: (4-hydroxy-2,6-dimethyl-[3]pyridyl)-phenyl ketone
• 英文别名: (4-Hydroxy-2,6-dimethyl-[3]pyridyl)-phenyl-keton；3-benzoyl-2,6-dimethyl-4(1H)-pyridone；3-benzoyl-2,6-dimethyl-1H-pyridin-4-one
• 化学式: C₁₄H₁₃NO₂
• 分子量: 227.263
• InChiKey: JERQPFAEAXCZPC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.4
• 重原子数：
  17
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.14
• 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：

  (4-hydroxy-2,6-dimethyl-[3]pyridyl)-phenyl ketone 在 三氯氧磷 、 sodium carbonate 作用下， 以 水 为溶剂， 反应 8.0h， 生成 (4-chloro-2,6-dimethyl-pyridin-3-yl)-phenyl-methanone
  参考文献：
  名称：

  WO2007/100295

  摘要：

  公开号：
• 作为产物：
  描述：

  2,6-二甲基-4-吡喃酮 在 乙醇 、 氨 、 水 、 三氟乙酸 作用下， 生成 (4-hydroxy-2,6-dimethyl-[3]pyridyl)-phenyl ketone
  参考文献：
  名称：

  Notes: Reactions of Several 4-Pyrones Catalyzed by Potassium Acetate and Trifluoroacetic Acid

  摘要：

  DOI：

  10.1021/jo01090a604

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。
• Pyridine compounds as angiotensin II antagonists, processes for their preparation and pharmaceutical compositions containing them
  申请人：ZENECA LIMITED

  公开号：EP0499416A2

  公开（公告）日：1992-08-19

  The invention concerns pharmaceutically useful compounds of formulae I-Ic, in which R1, R2, R3, R4, R5, R6, R7, X and Z have the various meanings defined herein, and their non-toxic salts, and pharmaceutical compositions containing them. The novel compounds are of value in treating conditions such as hypertension and congestive heart failure. The invention further concerns processes for the manufacture of the novel compounds and the use of the compounds in medical treatment.

  本发明涉及式 I-Ic 的药用化合物（其中 R1、R2、R3、R4、R5、R6、R7、X 和 Z 具有本文所定义的各种含义）及其无毒盐和含有它们的药物组合物。这些新型化合物具有治疗高血压和充血性心力衰竭等疾病的价值。本发明还涉及新型化合物的生产工艺以及这些化合物在医疗中的应用。
• Sato, Masayuki; Ogasawara, Hiromischi; Kato, Keiko, Chemical and pharmaceutical bulletin, 1983, vol. 31, # 12, p. 4300 - 4305
  作者：Sato, Masayuki、Ogasawara, Hiromischi、Kato, Keiko、Sakai, Masako、Kato, Tetsuzo

  DOI：——

  日期：——
• 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.
• SATO, MASAYUKI;OGASAWARA, HIROMICHI;KATO, KEIKO;SAKAI, MASAKO;KATO, TETSU+, CHEM. AND PHARM. BULL., 1983, 31, N 12, 4300-4305
  作者：SATO, MASAYUKI、OGASAWARA, HIROMICHI、KATO, KEIKO、SAKAI, MASAKO、KATO, TETSU+

  DOI：——

  日期：——