5-Methyl-3-phenyl-2-(1H)-pyridone | 53428-05-0

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶及其衍生物
• 英文名称: 5-Methyl-3-phenyl-2-(1H)-pyridone
• 英文别名: 5-Methyl-3-phenylpyridin-2(1H)-one；5-methyl-3-phenyl-1H-pyridin-2-one
• CAS: 53428-05-0
• 化学式: C₁₂H₁₁NO
• 分子量: 185.225
• InChiKey: UWADCDHQKKDQEL-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.8
• 重原子数：
  14
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.08
• 拓扑面积：
  29.1
• 氢给体数：
  1
• 氢受体数：
  1

反应信息

• 作为反应物：
  描述：

  5-Methyl-3-phenyl-2-(1H)-pyridone 、 碘苯 以to give 1,3-Diphenyl-5-methyl-2-(1H)-pyridone in 77% yield的产率得到1,3-Diphenyl-5-methyl-2-(1H) pyridone
  参考文献：
  名称：

  Method for reducing serum uric acid levels

  摘要：

  本发明涉及一种新型药物组合物，其活性成分为5-甲基-1-苯基-2-(1H)-吡啶酮化合物。已发现这种组合物具有代谢特性，能显著降低人类和其他哺乳动物的血清尿酸水平。含有5-甲基-1-苯基-2-(1H)-吡啶酮的组合物在口服时不会引起刺激，应用于特定目标组织时也不会出现明显的刺激或其他后遗症。

  公开号：

  US04052509A1

文献信息

• 5-Methyl-1-phenyl-2-(1H)-pyridone compositions and methods of use
  申请人：Affiliated Medical Research, Inc.

  公开号：US03974281A1

  公开（公告）日：1976-08-10

  Novel analgesic, anti-pyretic, anti-inflammatory compositions containing as the active ingredient the compound, 5-methyl-1-phenyl-2-(1H)-pyridone are described. Such compositions have also been found to cause significant lowering of serum uric acid and glucose levels and to be effective in the treatment of a number of upper respiratory ailments in humans and other mammals. Skin conditions such as dermatitis and poison ivy are also alleviated by this agent. The compositions containing 5-methyl-1-phenyl-2-(1H)-pyridone caused no irritation on oral administration or when applied to specific target tissues showed no significant irritation or other sequelae.

  描述了一种含有活性成分5-甲基-1-苯基-2-(1H)-吡啶酮的新型镇痛、退烧、抗炎组合物。这种组合物还被发现能显著降低血清尿酸和葡萄糖水平，并对人类和其他哺乳动物的多种上呼吸道疾病治疗有效。皮肤状况如皮炎和毒葛也可以通过这种药物缓解。含有5-甲基-1-苯基-2-(1H)-吡啶酮的组合物在口服时不引起刺激，在应用于特定靶组织时也没有显著的刺激或其他后遗症。
• Method for reducing serum uric acid levels
  申请人：Affiliated Medical Research, Inc.

  公开号：US04052509A1

  公开（公告）日：1977-10-04

  Novel pharmaceutical compositions containing as the active ingredient the compound 5-methyl-1-phenyl-2-(1H)-pyridone are described. Such compositions have been found to have a metabolic property which causes significant lowering of serum uric acid levels in humans and other mammals. The compositions containing 5-methyl-1-phenyl-2-(1H)-pyridone caused no irritation on oral administration or when applied to specific target tissues showed no significant irritation or other sequelae.

  本发明涉及一种新型药物组合物，其活性成分为5-甲基-1-苯基-2-(1H)-吡啶酮化合物。已发现这种组合物具有代谢特性，能显著降低人类和其他哺乳动物的血清尿酸水平。含有5-甲基-1-苯基-2-(1H)-吡啶酮的组合物在口服时不会引起刺激，应用于特定目标组织时也不会出现明显的刺激或其他后遗症。
• GRANULATE FORMULATION OF 5-METHYL-1-PHENYL-2(1H)-PYRIDONE AND METHOD OF MAKING THE SAME
  申请人：F. Hoffmann-La Roche AG

  公开号：EP3895696A1

  公开（公告）日：2021-10-20

  The disclosure relates to granulate formulations of pirfenidone and methods of making such formulations

  本公开涉及吡非尼酮的颗粒制剂和制造这种制剂的方法
• Methods of using a pharmaceutical composition containing pirfenidone in sustained-release tablet form
  申请人：CELL THERAPY AND TECHNOLOGY S.A. DE C.V.

  公开号：US10383862B2

  公开（公告）日：2019-08-20

  The instant invention relates to a process for the preparation of a pharmaceutical composition in sustained-release tablet form comprising from 600 milligrams to 2400 milligrams of Pirfenidone (PFD), in such a way that the drug is bioavailable during an extended period of time of 12 hours from its administration. In this way, the anti-fibrotic and anti-inflammatory action of the drug Pirfenidone is optimized. Moreover, the instant invention offers advantages and a higher therapeutic efficacy compared to other pharmaceutical forms of Pirfenidone for oral administration and its therapeutic application in the regression of chronic renal failure secondary to primary glomerulosclerosis; it shows a better activity with regard to the reduction and/or regression of deleterious effects in breast capsular contracture observed after the surgical implantation of breast implants in humans and has an important anti-TNF-α and anti-TGF-β1 action for the treatment of hepatic fibrosis.

  本发明涉及一种制备缓释片剂型药物组合物的工艺，该组合物含有 600 毫克至 2400 毫克的吡非尼酮（PFD），在给药后的 12 小时延长期内，该药物可被生物利用。这样，药物吡非尼酮的抗纤维化和抗炎作用就得到了优化。此外，与其他口服吡非尼酮药剂相比，本发明具有优势和更高的疗效，可用于治疗原发性肾小球硬化症继发的慢性肾功能衰竭；在减少和/或消除乳房植入物手术后观察到的乳房包膜挛缩的有害影响方面，本发明显示出更好的活性；在治疗肝纤维化方面，本发明具有重要的抗肿瘤坏死因子-α和抗肿瘤坏死因子-β1作用。
• Use of 5-methyl-1-phenyl-2-(1H)-pyridone in the prevention of fibrotic lesions
  申请人：Yamauchi, Shitotomo

  公开号：EP0383591B1

  公开（公告）日：2001-11-21