5-methyl-1-(3'-trifluoromethylphenyl)-2(1H)pyridone | 53427-79-5

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 5-methyl-1-(3'-trifluoromethylphenyl)-2(1H)pyridone
• 英文别名: 5-methyl-1(3'-trifluoromethylphenyl)-2-(1H)-pyridone；5-methyl-1-[3-(trifluoromethyl)phenyl]pyridin-2-one
• CAS: 53427-79-5
• 化学式: C₁₃H₁₀F₃NO
• 分子量: 253.224
• InChiKey: PLMQFHAKZKHJAT-UHFFFAOYSA-N

物化性质

• 沸点：
  345.2±42.0 °C(Predicted)
• 密度：
  1.290±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  2.7
• 重原子数：
  18
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.15
• 拓扑面积：
  20.3
• 氢给体数：
  0
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  草酰氯 、 5-methyl-1-(3'-trifluoromethylphenyl)-2(1H)pyridone 、 1,2-二氯乙烷 、 N,N-二甲基甲酰胺 生成 2-chloro-5-methyl-1-(3-trifluoromethyl-phenyl)-pyridinium chloride
  参考文献：
  名称：

  Substituted iminoazines

  摘要：

  这项发明涉及一种新型的通式（I）中的取代亚胺嘧啶化合物，其中R1、R2、R3、R4、Z1、Z2和Z3分别如描述中所定义，以及它们的制备过程和中间体的多种方法，以及它们作为除草剂的用途。

  公开号：

  US20040029881A1
• 作为产物：
  描述：

  2-羟基-5-甲基嘧啶 、 3-碘三氟甲苯 以gives a 78% yield of 5-methyl-1-(3'-trifluoromethylphenyl)-2-(1H)-pyridone的产率得到5-methyl-1-(3'-trifluoromethylphenyl)-2(1H)pyridone
  参考文献：
  名称：

  5-Methyl-1-phenyl-2-(1H)-pyridone compositions and methods of use

  摘要：

  本发明涉及一种新型的镇痛、退热、消炎组合物，其活性成分为5-甲基-1-苯基-2-(1H)-吡啶酮。这种组合物还被发现可以显著降低血清尿酸和葡萄糖水平，并且能够有效治疗人类和其他哺乳动物的许多上呼吸道疾病。此外，这种成分还可以缓解皮肤病如皮炎和毒葛引起的过敏反应。含有5-甲基-1-苯基-2-(1H)-吡啶酮的组合物在口服或涂抹到特定的目标组织时不会引起刺激或其他不良反应。

  公开号：

  US03974281A1

文献信息

• COMPOUNDS AND METHODS FOR TREATING INFLAMMATORY AND FIBROTIC DISORDERS
  申请人：Kossen Karl

  公开号：US20090318455A1

  公开（公告）日：2009-12-24

  Disclosed are compounds and methods for treating inflammatory and fibrotic disorders, including methods of modulating a stress activated protein kinase (SAPK) system with an active compound, wherein the active compound exhibits low potency for inhibition of the p38 MAPK; and wherein the contacting is conducted at a SAPK-modulating concentration that is at a low percentage inhibitory concentration for inhibition of the p38 MAPK by the compound. Also disclosed are derivatives and analogs of pirfenidone, useful for modulating a stress activated protein kinase (SAPK) system.

  公开了用于治疗炎症和纤维化疾病的化合物和方法，包括用活性化合物调节应激活化蛋白激酶（SAPK）系统的方法，其中活性化合物对p38 MAPK的抑制效力较低；并且其中接触是在SAPK调节浓度下进行的，该浓度对化合物抑制p38 MAPK的抑制浓度百分比较低。还公开了吡非尼酮的衍生物和类似物，它们可用于调节应激活化蛋白激酶（SAPK）系统。
• Method for reducing serum glucose levels
  申请人：Affiliated Medical Research, Inc.

  公开号：US04042699A1

  公开（公告）日：1977-08-16

  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 glucose 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.

  本发明涉及一种含有化合物5-甲基-1-苯基-2-(1H)-吡啶酮作为活性成分的新型药物组合物。发现这种组合物具有代谢特性，可以显著降低人类和其他哺乳动物的血清葡萄糖水平。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，在应用于特定目标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。
• MACROCYCLIC COMPOUNDS AS INHIBITORS OF VIRAL REPLICATION
  申请人：BLATT LAWRENCE M.

  公开号：US20090286843A1

  公开（公告）日：2009-11-19

  The embodiments provide compounds of the general formulas I-XIX, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating flaviviral infection, including hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition.

  该实施例提供了一般式I-XIX的化合物，以及包括药物组合物在内的组合物。该实施例还提供了治疗方法，包括治疗黄热病毒感染的方法，包括丙型肝炎病毒感染的方法和治疗肝纤维化的方法，通常涉及向需要治疗的个体施用所述化合物或组合物的有效量。
• Hyperglycosylated variants of interferon alfacon-1
  申请人：Alios Biopharma Inc.

  公开号：EP2093235A1

  公开（公告）日：2009-08-26

  The present invention provides synthetic Type I interferon receptor polypeptide agonists comprising consensus or hybrid Type I interferon receptor polypeptide agonists, containing one or more native or non-native glycosylation sites. The present invention provides synthetic Type I interferon receptor polypeptide agonists comprising consensus or hybrid Type I interferon receptor polypeptide agonists, containing one or more native or nonnative glycosylation sites, as well as erythropoietin and darbepoetin alfa, each of which are linked to a penetrating peptide that facilitates translocation of a substance across a biological barrier as well as pharmaceutical compositions, including oral formulations, of the same. The present invention further provides oral formulations of hyperglycosylated or protease-resistant, hyperglycosylated polypeptide variants, which polypeptide variants lack at least one protease cleavage site found in a parent polypeptide, and thus exhibit increased protease resistance compared to the parent polypeptide, which polypeptide variants further include (1) a carbohydrate moiety covalently linked to at least one non-native glycosylation site not found in the parent protein therapeutic or (2) a carbohydrate moiety covalently linked to at least one native glycosylation site found but not glycosylated in the parent protein therapeutic. The present invention further provides compositions, including oral pharmaceutical compositions, comprising the synthetic Type I interferon receptor polypeptide agonist, the hyperglycosylated polypeptide variant, or the hyperglycosylated, protease-resistant polypeptide variant. The present invention further provides containers, devices, and kits comprising the synthetic Type I interferon receptor polypeptide agonist, the hyperglycosylated polypeptide variant, or the hyperglycosylated, protease-resistant polypeptide variant. The present invention further provides therapeutic methods involving administering an effective amount of an oral pharmaceutical composition comprising a synthetic Type I interferon receptor polypeptide agonist, a hyperglycosylated polypeptide variant, or a hyperglycosylated, protease-resistant polypeptide variant to an individual in need thereof.

  本发明提供合成的I型干扰素受体多肽激动剂，包括共识或混合I型干扰素受体多肽激动剂，含有一个或多个原生或非原生糖基化位点。本发明提供合成的 I 型干扰素受体多肽激动剂，包括共识或混合 I 型干扰素受体多肽激动剂，含有一个或多个原生或非原生糖基化位点，以及促红细胞生成素和达贝胎素α，其中每一种都与促进物质通过生物屏障转运的穿透肽相连，以及药物组合物，包括其口服制剂。本发明进一步提供了高糖基化或抗蛋白酶的高糖基化多肽变体的口服制剂，这些多肽变体缺乏母体多肽中的至少一个蛋白酶裂解位点，因此与母体多肽相比表现出更强的抗蛋白酶能力、多肽变体进一步包括(1)与至少一个非原生糖基化位点共价连接的碳水化合物分子，该糖基化位点在母体蛋白治疗剂中未发现；或(2)与至少一个原生糖基化位点共价连接的碳水化合物分子，该糖基化位点在母体蛋白治疗剂中发现但未糖基化。本发明进一步提供了包含合成的 I 型干扰素受体多肽激动剂、高糖基化多肽变体或高糖基化、抗蛋白酶多肽变体的组合物，包括口服药物组合物。本发明进一步提供了包含合成 I 型干扰素受体多肽激动剂、高糖基化多肽变体或高糖基化、抗蛋白酶多肽变体的容器、装置和试剂盒。本发明进一步提供了治疗方法，包括向有需要的个体施用有效量的口服药物组合物，该组合物包含合成的I型干扰素受体多肽激动剂、高糖基化多肽变体或高糖基化、抗蛋白酶多肽变体。