N-((2S,3R)-1-amino-3-hydroxy-1-oxobutan-2-yl)-5-methyl-1-oxo-2,5-diazaspiro[3.4]octane-6-carboxamide

• 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: N-((2S,3R)-1-amino-3-hydroxy-1-oxobutan-2-yl)-5-methyl-1-oxo-2,5-diazaspiro[3.4]octane-6-carboxamide
• 英文别名: N-[(2S,3R)-1-amino-3-hydroxy-1-oxobutan-2-yl]-5-methyl-3-oxo-2,5-diazaspiro[3.4]octane-6-carboxamide
• 化学式: C₁₂H₂₀N₄O₄
• 分子量: 284.315
• InChiKey: BQJQAMHDBMCTMK-CPONLOHJSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -2.2
• 重原子数：
  20
• 可旋转键数：
  4
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.75
• 拓扑面积：
  125
• 氢给体数：
  4
• 氢受体数：
  5

反应信息

• 作为产物：
  描述：

  benzyl 2-(benzyloxy)-1-oxo-2,5-diazaspiro[3.4]octane-6-carboxylate 在 氢气 、 溶剂黄146 、 Methanaminium,N-[(dimethylamino)(3H-1,2,3-triazolo[4,5-b]pyridin-3-yloxy)methylene]-N-methyl-, hexafluorophosphate(1-) 作用下， 以 甲醇 、 N,N-二甲基甲酰胺 为溶剂， 反应 50.17h， 生成 N-((2S,3R)-1-amino-3-hydroxy-1-oxobutan-2-yl)-5-methyl-1-oxo-2,5-diazaspiro[3.4]octane-6-carboxamide
  参考文献：
  名称：

  [EN] SPIRO-LACTAM AND BIS-SPIRO-LACTAM NMDA RECEPTOR MODULATORS AND USES THEREOF
  [FR] MODULATEURS SPIRO-LACTAMES ET BIS-SPIRO-LACTAMES DES RÉCEPTEURS NMDA ET LEURS UTILISATIONS

  摘要：

  揭示了具有调节NMDA受体活性潜力的化合物。这些化合物可用于治疗

  公开号：

  WO2018026792A1

文献信息

• Spiro-lactam and bis-spiro-lactam NMDA receptor modulators and uses thereof
  申请人：Aptinyx Inc.

  公开号：US11028095B2

  公开（公告）日：2021-06-08

  Disclosed are compounds having potency in the modulation of NMDA receptor activity. Such compounds can be used in the treatment of conditions such as depression and related disorders. Orally delivered formulations and other pharmaceutically acceptable delivery forms of the compounds, including intravenous formulations, are also disclosed.

  所公开的化合物具有调节 NMDA 受体活性的功效。此类化合物可用于治疗抑郁症及相关疾病。此外，还公开了口服制剂和其他药学上可接受的化合物给药形式，包括静脉注射制剂。
• SPIRO-LACTAM AND BIS-SPIRO-LACTAM NMDA RECEPTOR MODULATORS AND USES THEREOF
  申请人：Aptinyx Inc.

  公开号：EP3490994A1

  公开（公告）日：2019-06-05
• METHODS OF TREATING DISORDERS ASSOCIATED WITH ELEVATED LEVELS OF ANTIBODIES THAT INTERACT WITH THE NMDA RECEPTOR
  申请人：Aptinyx Inc.

  公开号：US20220273629A1

  公开（公告）日：2022-09-01

  Methods of treating a disorder associated with elevated NMDAR antibodies in a patient in need thereof are provided comprising, for example, administering to the patient an effective amount of a spiro-β-lactam compound.
• [EN] METHODS OF TREATING DISORDERS ASSOCIATED WITH ELEVATED LEVELS OF ANTIBODIES THAT INTERACT WITH THE NMDA RECEPTOR<br/>[FR] MÉTHODES DE TRAITEMENT DE TROUBLES ASSOCIÉS À DES TAUX ÉLEVÉS D'ANTICORPS EN INTERACTION AVEC LE RÉCEPTEUR NMDA
  申请人：APTINYX INC

  公开号：WO2021021996A1

  公开（公告）日：2021-02-04

  Methods of treating a disorder associated with elevated NMDAR antibodies in a patient in need thereof are provided comprising, for example, administering to the patient an effective amount of a spiro-β-lactam compound.
• [EN] SPIRO-LACTAM AND BIS-SPIRO-LACTAM NMDA RECEPTOR MODULATORS AND USES THEREOF<br/>[FR] MODULATEURS SPIRO-LACTAMES ET BIS-SPIRO-LACTAMES DES RÉCEPTEURS NMDA ET LEURS UTILISATIONS
  申请人：APTINYX INC

  公开号：WO2018026792A1

  公开（公告）日：2018-02-08

  Disclosed are compounds having potency in the modulation of NMDA receptor activity. Such compounds can be used in the treatment of conditions such as depression and related disorders. Orally delivered formulations and other pharmaceutically acceptable delivery forms of the compounds, including intravenous formulations, are also disclosed.

  揭示了具有调节NMDA受体活性潜力的化合物。这些化合物可用于治疗