N-(2-chloropyridin-4-yl)formamide | 1379164-31-4

• 分子结构分类: 有机化合物 - 有机氮化合物
• 英文名称: N-(2-chloropyridin-4-yl)formamide
• CAS: 1379164-31-4
• 化学式: C₆H₅ClN₂O
• 分子量: 156.572
• InChiKey: FUBNXHSCNKWXEC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1
• 重原子数：
  10
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  42
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  N-(2-chloropyridin-4-yl)formamide 、 4-氟溴苄 在 sodium hydride 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 生成 C₁₃H₁₀ClFN₂O
  参考文献：
  名称：

  Amide-based inhibitors of p38α MAP kinase. Part 1: Discovery of novel N-pyridyl amide lead molecules

  摘要：

  A novel series of N-pyridyl amides as potent p38 alpha kinase inhibitors is described. Based on the structural similarities between the initial hit and a well-known imidazole pyrimidine series of p38 alpha inhibitors, potencies within the newly discovered series were quickly improved by installation of an (S)-alpha-methylbenzyl moiety at the 2-position of the pyridine ring. The proposed binding modes of the new series to p38 alpha were evaluated against SAR findings and provided rationale for further development of this series of molecules. (C) 2010 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2010.02.088
• 作为产物：
  描述：

  2-氯-4-氨基吡啶 、 甲酰氯 在 三乙胺 作用下， 以 二氯甲烷 为溶剂， 生成 N-(2-chloropyridin-4-yl)formamide
  参考文献：
  名称：

  Amide-based inhibitors of p38α MAP kinase. Part 1: Discovery of novel N-pyridyl amide lead molecules

  摘要：

  A novel series of N-pyridyl amides as potent p38 alpha kinase inhibitors is described. Based on the structural similarities between the initial hit and a well-known imidazole pyrimidine series of p38 alpha inhibitors, potencies within the newly discovered series were quickly improved by installation of an (S)-alpha-methylbenzyl moiety at the 2-position of the pyridine ring. The proposed binding modes of the new series to p38 alpha were evaluated against SAR findings and provided rationale for further development of this series of molecules. (C) 2010 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2010.02.088

文献信息

• [EN] PHENYLALANINE DERIVATIVES AND THEIR USE AS NON-PEPTIDE GLP-1 RECEPTOR MODULATORS<br/>[FR] DÉRIVÉS PHÉNYLALANINES ET LEUR UTILISATION COMME MODULATEURS NON PEPTIDIQUES DU RÉCEPTEUR DE GLP-1
  申请人：ARGUSINA INC

  公开号：WO2011094890A1

  公开（公告）日：2011-08-11

  Provided herein are non-peptide GLP-1 receptor modulator compounds, for example, of Formula (I), pharmaceutical compositions comprising such compounds, and processes of preparation thereof. Also provided are methods of their use for the treatment of a metabolic disorder.

  本文提供了非肽类GLP-1受体调节剂化合物，例如，Formula (I)的化合物，包括这些化合物的药物组合物，以及其制备方法。还提供了这些化合物用于治疗代谢紊乱的方法。
• New Piperazine Compound and Use Thereof as a HCV Polymerase Inhibitor
  申请人：Abe Hiroyuki

  公开号：US20080081818A1

  公开（公告）日：2008-04-03

  The present invention relates to a compound represented by the following formula [I] wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof, or a solvate thereof and an anti-HCV agent and an HCV polymerase inhibitor containing this compound. The compound of the present invention shows an anti-HCV activity based on the HCV polymerase inhibitory activity, and useful as an agent for the prophylaxis or treatment of hepatitis C.

  本发明涉及一种由以下式[I]表示的化合物，其中每个符号如规范中定义，或其药学上可接受的盐，或其溶剂化合物，以及含有该化合物的抗HCV剂和HCV聚合酶抑制剂。本发明的化合物基于HCV聚合酶抑制活性显示出抗HCV活性，并且可用作预防或治疗丙型肝炎的药剂。
• NEW PIPERAZINE COMPOUND AND USE THEREOF AS A HCV POLYMERASE INHIBITOR
  申请人：Abe Hiroyuki

  公开号：US20120107273A1

  公开（公告）日：2012-05-03

  The present invention relates to a compound represented by the following formula [I] wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof, or a solvate thereof and an anti-HCV agent and an HCV polymerase inhibitor containing this compound. The compound of the present invention shows an anti-HCV activity based on the HCV polymerase inhibitory activity, and useful as an agent for the prophylaxis or treatment of hepatitis C.

  本发明涉及一种由下式[I]表示的化合物，其中每个符号如规范所定义，或其药学上可接受的盐，或其溶剂化物，以及含有该化合物的抗HCV剂和HCV聚合酶抑制剂。本发明的化合物基于HCV聚合酶抑制活性表现出抗HCV活性，可作为预防或治疗丙型肝炎的药剂。
• NOVEL PIPERAZINE COMPOUND, AND USE THEREOF AS HCV POLYMERASE INHIBITOR
  申请人：Japan Tobacco, Inc.

  公开号：EP2009004A1

  公开（公告）日：2008-12-31

  The present invention relates to a compound represented by the following formula [I] wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof, or a solvate thereof and an anti-HCV agent and an HCV polymerase inhibitor containing this compound. The compound of the present invention shows an anti-HCV activity based on the HCV polymerase inhibitory activity, and useful as an agent for the prophylaxis or treatment of hepatitis C.

  本发明涉及下式[I]所代表的化合物 其中各符号如说明书中所定义，或其药学上可接受的盐，或其溶液，以及含有该化合物的抗HCV药剂和HCV聚合酶抑制剂。本发明的化合物具有基于 HCV 聚合酶抑制活性的抗 HCV 活性，可用作丙型肝炎的预防或治疗剂。
• INHIBITORS OF HUMAN IMMUNODEFICIENCY VIRUS REPLICATION
  申请人：BOEHRINGER INGELHEIM INTERNATIONAL GMBH

  公开号：EP2429993B1

  公开（公告）日：2015-01-21