6-(dimethylamino)-4-[(methylamino)methyl]-2-{6-[4-(propan-2-yl)-4H-1,2,4-triazol-3-yl]pyridin-2-yl}-2,3-dihydro-1H-pyrrolo[3,4-c]pyridin-1-one | 2421198-78-7

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡咯并吡啶类
• 英文名称: 6-(dimethylamino)-4-[(methylamino)methyl]-2-{6-[4-(propan-2-yl)-4H-1,2,4-triazol-3-yl]pyridin-2-yl}-2,3-dihydro-1H-pyrrolo[3,4-c]pyridin-1-one
• 英文别名: US11142525, Example 1；6-(dimethylamino)-4-(methylaminomethyl)-2-[6-(4-propan-2-yl-1,2,4-triazol-3-yl)pyridin-2-yl]-3H-pyrrolo[3,4-c]pyridin-1-one
• CAS: 2421198-78-7
• 化学式: C₂₁H₂₆N₈O
• 分子量: 406.49
• InChiKey: YTUDJKCCACKHLG-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.5
• 重原子数：
  30
• 可旋转键数：
  6
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  92.1
• 氢给体数：
  1
• 氢受体数：
  7

反应信息

• 作为产物：
  描述：

  tert-butyl {[6-(dimethylamino)-1-oxo-2-{6-[4-(propan-2-yl)-4H-1,2,4-triazol-3-yl]pyridin-2-yl}-2,3-dihydro-1H-pyrrolo[3,4-c]pyridin-4-yl]methyl}methylcarbamate 在 盐酸 作用下， 以 乙酸乙酯 为溶剂， 反应 1.0h， 以93%的产率得到6-(dimethylamino)-4-[(methylamino)methyl]-2-{6-[4-(propan-2-yl)-4H-1,2,4-triazol-3-yl]pyridin-2-yl}-2,3-dihydro-1H-pyrrolo[3,4-c]pyridin-1-one
  参考文献：
  名称：

  WO2020100027A5

  摘要：

  公开号：

  WO2020100027A5

文献信息

• Azalactam compounds as HPK1 inhibitors
  申请人：Pfizer Inc.

  公开号：US11142525B2

  公开（公告）日：2021-10-12

  This invention relates to compounds of general Formula (I) and pharmaceutically acceptable salts thereof, in which R1, R1a, R2, R3, R4, and (R5)a are as defined herein, to pharmaceutical compositions comprising such compounds and pharmaceutically acceptable salts thereof, and to methods of using such compounds, pharmaceutically acceptable salts and compositions for the treatment of abnormal cell growth, including cancer.

  本发明涉及通式 (I) 的化合物 及其药学上可接受的盐，其中 R1、R1a、R2、R3、R4 和 (R5)a 如本文所定义；包含此类化合物及其药学上可接受的盐的药物组合物；以及使用此类化合物、药学上可接受的盐和组合物治疗异常细胞生长（包括癌症）的方法。
• 2,3-DIHYDRO-1H-PYRROLO[3,4-C]PYRIDIN-1-ONE DERIVATIVES AS HPK1 INHIBITORS FOR THE TREATMENT OF CANCER
  申请人：Pfizer Inc.

  公开号：EP3880676A1

  公开（公告）日：2021-09-22
• Azalactam Compounds as HPK1 Inhibitors
  申请人：Pfizer Inc.

  公开号：US20200172539A1

  公开（公告）日：2020-06-04

  This invention relates to compounds of general Formula (I) and pharmaceutically acceptable salts thereof, in which R 1 , R 1a , R 2 , R 3 , R 4 , and (R 5 ) a are as defined herein, to pharmaceutical compositions comprising such compounds and pharmaceutically acceptable salts thereof, and to methods of using such compounds, pharmaceutically acceptable salts and compositions for the treatment of abnormal cell growth, including cancer.
• [EN] 2,3-DIHYDRO-1H-PYRROLO[3,4-C]PYRIDIN-1-ONE DERIVATIVES AS HPK1 INHIBITORS FOR THE TREATMENT OF CANCER<br/>[FR] DÉRIVÉS DE 2,3-DIHYDRO-1H-PYRROLO[3,4-C]PYRIDIN-1-ONE SERVANT D'INHIBITEURS DE HPK1 POUR LE TRAITEMENT DU CANCER
  申请人：PFIZER

  公开号：WO2020100027A1

  公开（公告）日：2020-05-22

  This invention relates to 2,3-dihydro-1H-pyrrolo[3,4-c]pyridin-1-one derivatives of general Formula (I) and pharmaceutically acceptable salts thereof, as hematopoietic progenitor kinase 1 (HPK1) inhibitors, in which R1, R1a, R2, R3, R4, and (R5)a are as defined herein, to pharmaceutical compositions comprising such compounds and and to compositions for the treatment of abnormal cell growth, including cancer. A specific exemplary compound is e.g. 4-[(methylamino)methyl]-6- [methyl(propan-2-yl)amino]-2-[6-(4-propyl-4H-l,2,4-triazol-3-yl) pyridin-2-yl]-2,3-dihydro-lH-pyrrolo[3,4-c]pyridin-l-one. The present description discloses the preparation of exemplary compounds as well as pharmacological data thereof (e.g. pages 82 to 211; examples 1 to 188; tables 1 to 5).