[(1,3-dicyclohexyl-6-hydroxy-2,4-dioxo-1,2,3,4-tetrahydropyrimidine-5-carbonyl)amino]acetic acid

• 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: [(1,3-dicyclohexyl-6-hydroxy-2,4-dioxo-1,2,3,4-tetrahydropyrimidine-5-carbonyl)amino]acetic acid
• 英文别名: 2-(1,3-dicyclohexyl-6-hydroxy-2,4-dioxo-1,2,3,4-tetrahydropyrimidine-5-carboxamido)acetic acid；N-[(1,3-dicyclohexyl-6-hydroxy-2,4-dioxo-1,2,3,4-tetrahydro-5-pyrimidinyl)carbonyl]glycine；daprodustat；GSK1278863；2-[(1,3-dicyclohexyl-4-hydroxy-2,6-dioxopyrimidine-5-carbonyl)amino]acetic acid
• 化学式: C₁₉H₂₇N₃O₆
• 分子量: 393.44
• InChiKey: NVTKJBXOBFRPLQ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.1
• 重原子数：
  28
• 可旋转键数：
  5
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.68
• 拓扑面积：
  127
• 氢给体数：
  3
• 氢受体数：
  6

反应信息

• 作为产物：
  描述：

  N,N-二环己脲 在 sodium hydroxide 、 水 、 N,N-二异丙基乙胺 作用下， 以 乙醇 、 二氯甲烷 、 氯仿 为溶剂， 反应 7.0h， 生成 [(1,3-dicyclohexyl-6-hydroxy-2,4-dioxo-1,2,3,4-tetrahydropyrimidine-5-carbonyl)amino]acetic acid
  参考文献：
  名称：

  [EN] PROLYL HYDROXYLASE INHIBITORS
  [FR] INHIBITEURS DE PROLYLE HYDROXYLASE

  摘要：

  公开号：

  WO2007150011A3

文献信息

• PROLYL HYDROXYLASE INHIBITORS
  申请人：Duffy Kevin J.

  公开号：US20100113444A1

  公开（公告）日：2010-05-06

  The invention described herein relates to certain pyrimidinetrione N-substituted glycine derivatives of formula (I), (I) which are antagonists of HIF prolyl hydroxylases and are useful for treating diseases benefiting from the inhibition of this enzyme, anemia being one example.

  本发明涉及以下化学式（I）的某些嘧啶三酮N-取代甘氨酸衍生物，其为HIF脯氨酸羟化酶的拮抗剂，并且对于治疗受益于抑制该酶的疾病，贫血是其中之一的例子。
• PROLINE HYDROXYLASE INHIBITORS FOR USE IN THE SKELETAL MUSCLE REGENERATION
  申请人：Policlinico San Donato S.p.A.- Istituto di Ricovero e Cura a Carattere Scientifico

  公开号：EP3906926A1

  公开（公告）日：2021-11-10

  The present invention relates to proline hydroxylase (PHDs) inhibitors acting through pharmacological activation of hypoxia inducible factor-1a (HIF-1a), upregulation of Wnt7a expression and iron chelation for use in the skeletal muscle regeneration occurring after an hypoxic insult, and related pharmaceutical compositions for administration through systemic or topical route.

  本发明涉及通过药理学激活缺氧诱导因子-1a（HIF-1a）、上调 Wnt7a 表达和铁螯合作用的脯氨酸羟化酶（PHDs）抑制剂，用于缺氧损伤后的骨骼肌再生，以及通过全身或局部途径给药的相关药物组合物。
• Prolyl hydroxylase inhibitors
  申请人：GlaxoSmithKline, LLC

  公开号：US10035779B2

  公开（公告）日：2018-07-31

  The invention described herein relates to certain pyrimidinetrione N-substituted glycine derivatives of formula (I) which are antagonists of HIF prolyl hydroxylases and are useful for treating diseases benefiting from the inhibition of this enzyme, anemia being one example.

  本发明涉及式 (I) 的某些嘧啶三酮 N-取代甘氨酸衍生物 它们是 HIF 脯氨酰羟化酶的拮抗剂，可用于治疗因抑制该酶而获益的疾病，贫血就是其中一例。
• MOBILIZING AGENTS AND USES THEREFOR
  申请人：MATER MEDICAL RESEARCH INSTITUTE LIMITED

  公开号：US20160015786A1

  公开（公告）日：2016-01-21

  Disclosed is the use of a HIF-α potentiating agent and a mobilizer of hematopoietic stem cells and/or progenitor cells in methods and compositions for mobilizing hematopoietic stem cell and progenitor cells from the bone marrow into the peripheral blood. The compositions and methods are particularly useful for stem cell transplantation and for treating or preventing immune deficiencies.
• Prolyl Hydroxylase Inhibitors
  申请人：GlaxoSmithKline, LLC

  公开号：US20180305323A1

  公开（公告）日：2018-10-25

  The invention described herein relates to certain pyrimidinetrione N-substituted glycine derivatives of formula (I) which are antagonists of HIF prolyl hydroxylases and are useful for treating diseases benefiting from the inhibition of this enzyme, anemia being one example.