(R)-3-amino-2,3-dihydrothiophene 1,1-dioxide

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二氢噻吩类
• 英文名称: (R)-3-amino-2,3-dihydrothiophene 1,1-dioxide
• 英文别名: (3R)-1,1-dioxo-2,3-dihydrothiophen-3-amine
• 化学式: C₄H₇NO₂S
• 分子量: 133.171
• InChiKey: YQYVLIKFODWGAV-SCSAIBSYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -1.3
• 重原子数：
  8
• 可旋转键数：
  0
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  68.5
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  6-(4-cyclopropylphenyl)-2-oxo-1,2-dihydropyridine-3-carboxylic acid 、 (R)-3-amino-2,3-dihydrothiophene 1,1-dioxide 在 1-丙基磷酸酐 、 N,N-二异丙基乙胺 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 以33 %的产率得到(R)-6-(4-cyclopropylphenyl)-N-(1,1-dioxido-2,3-dihydrothiophen-3-yl)-2-oxo-1,2-dihydropyridine-3-carboxamide
  参考文献：
  名称：

  [EN] CYCLIC VINYL SULFONE COMPOUNDS AS WRN INHIBITORS
  [FR] COMPOSÉS DE SULFONE DE VINYLE CYCLIQUE UTILISÉS EN TANT QU'INHIBITEURS DE WRN

  摘要：

  Disclosed herein are certain succinamido derivatives of Formula (I): (I) that inhibit Wemer Syndrome ATP dependent helicase enzyme (WRN) activity, in particular inhibit WRN helicase domain activity and are thereofore useful in treating cancers treatable by inhibition of WRN, including cancers characterized by microsatellite instability (MSI) and/or defective DNA mismatch repair system (dMMR). Also, disclosed are pharmaceutical compositions comprising such compounds, methods of using such compounds, and methods making the same.

  公开号：

  WO2023062575A1

文献信息

• [EN] CYCLIC VINYL SULFONE COMPOUNDS AS WRN INHIBITORS<br/>[FR] COMPOSÉS DE SULFONE DE VINYLE CYCLIQUE UTILISÉS EN TANT QU'INHIBITEURS DE WRN
  申请人：[en]IDEAYA BIOSCIENCES, INC.

  公开号：WO2023062575A1

  公开（公告）日：2023-04-20

  Disclosed herein are certain succinamido derivatives of Formula (I): (I) that inhibit Wemer Syndrome ATP dependent helicase enzyme (WRN) activity, in particular inhibit WRN helicase domain activity and are thereofore useful in treating cancers treatable by inhibition of WRN, including cancers characterized by microsatellite instability (MSI) and/or defective DNA mismatch repair system (dMMR). Also, disclosed are pharmaceutical compositions comprising such compounds, methods of using such compounds, and methods making the same.