ethyl 2-(6-(6-chloropyrimidin-4-yl)-4-hydroxy-1-methyl-2-oxo-1,2-dihydroquinoline-3-carboxamido)acetate

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: ethyl 2-(6-(6-chloropyrimidin-4-yl)-4-hydroxy-1-methyl-2-oxo-1,2-dihydroquinoline-3-carboxamido)acetate
• 英文别名: ethyl 2-[[6-(6-chloropyrimidin-4-yl)-4-hydroxy-1-methyl-2-oxoquinoline-3-carbonyl]amino]acetate
• 化学式: C₁₉H₁₇ClN₄O₅
• 分子量: 416.821
• InChiKey: HXXBRVKJKANNBX-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.7
• 重原子数：
  29
• 可旋转键数：
  6
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.21
• 拓扑面积：
  122
• 氢给体数：
  2
• 氢受体数：
  7

反应信息

• 作为产物：
  描述：

  N-甲基蒽 在 四(三苯基膦)钯 、 1,1'-bis(diphenylphosphino)ferrocene-palladium dichloride 盐酸 、 potassium acetate 、 一氯化碘 、 sodium hydride 、 sodium carbonate 作用下， 以 1,4-二氧六环 、 水 、 N,N-二甲基甲酰胺 、 甲苯 、 mineral oil 为溶剂， 反应 57.5h， 生成 2-(6-(6-chloropyrimidin-4-yl)-4-hydroxy-1-methyl-2-oxo-1,2-dihydroquinoline-3-carboxamido)acetic acid 、 ethyl 2-(6-(6-chloropyrimidin-4-yl)-4-hydroxy-1-methyl-2-oxo-1,2-dihydroquinoline-3-carboxamido)acetate
  参考文献：
  名称：

  Quinolone based compounds exhibiting prolyl hydroxylase inhibitory activity, and compositions, and uses thereof

  摘要：

  这项发明涉及一类新型的喹诺酮类化合物，这些化合物显示出脯氨酰羟化酶抑制活性。该发明还涉及通过向受试者施用至少一种喹诺酮类化合物，来提高受试者中的HIF水平或活性，或治疗与受试者中HIF水平或活性相关的病症的方法。此外，该发明还涉及用于检测HIF分子中羟基脯氨酸残基的试验方法。

  公开号：

  US20070249605A1

文献信息

• QUINOLONE BASED COMPOUNDS EXHIBITING, PROLYL HYDROXYLASE INHIBITORY ACTIVITY, AND COMPOSITIONS, AND USES THEREOF
  申请人：Allen Jennifer R.

  公开号：US20100184763A1

  公开（公告）日：2010-07-22

  This invention relates to new quinolone based compounds that exhibit prolyl hydroxylase inhibitory activity. This invention also relates to methods of increasing HIF levels or activity in a subject or treating a condition associated with HIF levels or activity in a subject by administering to the subject at least one quinolone based compound. This invention further involves assays for the detection of a hydroxyproline residue in a HW molecule.

  本发明涉及一种新的基于喹诺酮的化合物，该化合物表现出脯氨酸羟化酶抑制活性。本发明还涉及通过向受试者施用至少一种基于喹诺酮的化合物来增加受试者中HIF水平或活性或治疗与HIF水平或活性相关的疾病的方法。本发明还涉及用于检测HW分子中羟基脯氨酸残基的测定方法。
• QUINOLONE BASED COMPOUNDS EXHIBITING PROLYL HYDROXYLASE INHIBITORY ACTIVITY, AND COMPOSITIONS, AND USES THEREOF
  申请人：ALLEN JENNIFER R.

  公开号：US20100240610A1

  公开（公告）日：2010-09-23

  This invention relates to new quinolone based compounds that exhibit prolyl hydroxylase inhibitory activity. This invention also relates to methods of increasing HIF levels or activity in a subject or treating a condition associated with HIF levels or activity in a subject by administering to the subject at least one quinolone based compound. This invention further involves assays for the detection of a hydroxyproline residue in a HIF molecule.

  本发明涉及一种新的基于喹诺酮的化合物，该化合物表现出丙氨酸羟化酶抑制活性。本发明还涉及通过向受试者施用至少一种基于喹诺酮的化合物来增加HIF水平或活性或治疗与HIF水平或活性相关的疾病的方法。本发明还涉及检测HIF分子中羟基脯氨酸残基的测定方法。
• Quinolone based compounds exhibiting, prolyl hydroxylase inhibitory activity, and compositions, and uses thereof
  申请人：Amgen Inc.

  公开号：US08017626B2

  公开（公告）日：2011-09-13

  This invention relates to new quinolone based compounds that exhibit prolyl hydroxylase inhibitory activity. This invention also relates to methods of increasing HIF levels or activity in a subject or treating a condition associated with HIF levels or activity in a subject by administering to the subject at least one quinolone based compound. This invention further involves assays for the detection of a hydroxyproline residue in a HIF molecule.

  本发明涉及一种新的喹诺酮基化合物，其具有脯氨酸羟化酶抑制活性。本发明还涉及通过向受试者投与至少一种喹诺酮基化合物来增加HIF水平或活性或治疗与HIF水平或活性相关的疾病的方法。此外，本发明还涉及用于检测HIF分子中羟基脯氨酸残基的检测方法。
• QUINOLONE BASED COMPOUNDS EXHIBITING PROLYL HYDROXYLASE INHIBITORY ACTIVITY, COMPOSITIONS AND USES THEREOF
  申请人：Amgen, Inc.

  公开号：EP1960363B1

  公开（公告）日：2014-01-22
• US7728130B2
  申请人：——

  公开号：US7728130B2

  公开（公告）日：2010-06-01