4-hydroxy-1-methyl-2-oxo-1,2-dihydroquinoline-3-carboxamide | 92016-67-6

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 喹啉及其衍生物
• 英文名称: 4-hydroxy-1-methyl-2-oxo-1,2-dihydroquinoline-3-carboxamide
• 英文别名: 4-hydroxy-1-methyl-2-oxoquinoline-3-carboxamide
• CAS: 92016-67-6
• 化学式: C₁₁H₁₀N₂O₃
• 分子量: 218.212
• InChiKey: FCGOSOJMIHJZJB-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.1
• 重原子数：
  16
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.09
• 拓扑面积：
  83.6
• 氢给体数：
  2
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  4-hydroxy-1-methyl-N'-[(1E)-(2-nitrophenyl)methylene]-2-oxo-1,2-dihydroquinoline-3-carbohydrazide 在 溶剂黄146 、 锌 作用下， 反应 3.0h， 以80%的产率得到4-hydroxy-1-methyl-2-oxo-1,2-dihydroquinoline-3-carboxamide
  参考文献：
  名称：

  4-羟基-2-喹诺酮类化合物132. 1-R-4-羟基-2-氧-2-氧-1,2-二氢喹啉-3-羧酸2-硝基苄基肼的合成，化学和生物学性质

  摘要：

  DOI：

  10.1007/s10593-007-0221-8

文献信息

• [EN] 1,2-DIHYDRO-4-HYDROXY-2-OXO-QUINOLINE-3-CARBOXANILIDES AS AHR ACTIVATORS.<br/>[FR] 1,2-DIHYDRO-4-HYDROXY-2-OXO-QUINOLÉINE-3-CARBOXANILIDES EN TANT QU'ACTIVATEURS D'AHR
  申请人：PETTERSSON LARS

  公开号：WO2012050500A1

  公开（公告）日：2012-04-19

  The present invention relates to compounds which are 1, 2-dihydro-4- hydroxy-2-oxo-quinoline-3-carboxanilides, their thieno-pyridone analogs, and prodrugs thereof. This invention specifically relates to such derivatives containing an N-hydrogen in the carboxanilide moiety and which exhibit modulating activity towards the aromatic hydrocarbon receptor (AhR), and, specifically, also to prodrugs thereof. The present invention also relates to use of said compounds as a medicament, and for the treatment of cancer, autoimmune disorders and other disorders with an immunological component, and a pharmaceutical composition comprising one or more of said compounds and a method of treatment.

  本发明涉及化合物，其为1,2-二氢-4-羟基-2-氧基喹啉-3-羧酰苯胺，其噻吩-吡啶酮类似物及其前药。本发明具体涉及含有羧酰苯胺基团中N-氢的衍生物，具有对芳香烃受体（AhR）的调节活性，特别是还涉及其前药。本发明还涉及将所述化合物用作药物，用于治疗癌症、自身免疫性疾病和其他具有免疫成分的疾病，以及包含一种或多种所述化合物的药物组合物和治疗方法。
• NITROGEN-CONTAINING FUSED HETEROCYCLIC SHP2 INHIBITOR COMPOUND, PREPARATION METHOD, AND USE
  申请人：Shanghai Ringene BioPharma Co., Ltd.

  公开号：EP3878853A1

  公开（公告）日：2021-09-15

  Disclosed are a nitrogen-containing fused heterocyclic SHP2 inhibitor compound, a preparation method, and use. The nitrogen-containing fused heterocyclic SHP2 inhibitor compound is represented by formula I below. The compound has high inhibitory activity for an SHP2 enzyme and tumor cell proliferation, and has good druggability.

  本发明公开了一种含氮融合杂环 SHP2 抑制剂化合物、制备方法和用途。含氮融合杂环 SHP2 抑制剂化合物如下式 I 所示。该化合物对SHP2酶和肿瘤细胞增殖具有较高的抑制活性，且具有良好的可药用性。
• Heterocyclic carboxamides, compositions containing such compounds, processes for their preparation and methods of treatment therewith
  申请人：AB LEO

  公开号：EP0059698B1

  公开（公告）日：1985-09-25
• 1,2-DIHYDRO-4-HYDROXY-2-OXO-QUINOLINE-3-CARBOXANILIDES AS AHR ACTIVATORS.
  申请人：Immunahr AB

  公开号：EP2627638A1

  公开（公告）日：2013-08-21
• N-ETHYL-N-PHENYL-1,2-DIHYDRO-4,5-DI-HYDROXY-1-METHYL-2-OXO-3-QUINOLINE CARBOXAMIDE, PREPARATION AND USES THEREOF
  申请人：Teva Pharmaceutical Industries Ltd.

  公开号：EP2744498A1

  公开（公告）日：2014-06-25