6-(2,4-Difluoro-phenoxy)-2-(3-hydroxy-1(R), 3-dimethyl-butylamino)-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one | 449811-96-5

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: 6-(2,4-Difluoro-phenoxy)-2-(3-hydroxy-1(R), 3-dimethyl-butylamino)-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one
• 英文别名: 6-(2,4-difluorophenoxy)-2-[[(2R)-4-hydroxy-4-methylpentan-2-yl]amino]-8-methylpyrido[2,3-d]pyrimidin-7-one
• CAS: 449811-96-5
• 化学式: C₂₀H₂₂F₂N₄O₃
• 分子量: 404.416
• InChiKey: CQBKXXDWVJIDMM-LLVKDONJSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.7
• 重原子数：
  29
• 可旋转键数：
  6
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.35
• 拓扑面积：
  87.6
• 氢给体数：
  2
• 氢受体数：
  8

文献信息

• 6-Substituted pyrido-pyrimidines
  申请人：——

  公开号：US20040116698A1

  公开（公告）日：2004-06-17

  The present invention provides compounds of the Formula I and II: 1 wherein R 1 , R 3 , W, Z, X 1 , X 2 , Ar 1 , R 8 and R 9 are as defined herein, and methods and intermediates for their preparation and uses thereof.

  本发明提供公式I和II的化合物：1其中R1、R3、W、Z、X1、X2、Ar1、R8和R9如本文所定义，以及其制备方法和中间体以及它们的用途。
• P38 kinase inhibitors reduce DUX4 and downstream gene expression for the treatment of FSHD
  申请人：Fulcrum Therapeutics, Inc.

  公开号：US10342786B2

  公开（公告）日：2019-07-09

  The disclosure relates to methods and compositions including p38 kinase inhibitors and agents that regulate expression of DUX4 and downstream genes including but not restricted to ZSCAN4, LEUTX, PRAMEF2, TRIM43, MBD3L2, KHDC1L, RFPL2, CCNA1, SLC34A2, TPRX1, PRAMEF20, TRIM49, PRAMEF4, PRAME6, PRAMEF15, or ZNF280A. Methods useful for treating a disease associated with abnormal DUX4 and downstream gene expression (e.g., Fascioscapulohumeral muscular dystrophy) are disclosed.

  本发明公开了包括 p38 激酶抑制剂和调节 DUX4 及下游基因（包括但不限于 ZSCAN4、LEUTX、PRAMEF2、TRIM43、MBD3L2、KHDC1L、RFPL2、CCNA1、SLC34A2、TPRX1、PRAMEF20、TRIM49、PRAMEF4、PRAME6、PRAMEF15 或 ZNF280A）表达的制剂在内的方法和组合物。本研究公开了用于治疗与 DUX4 及下游基因表达异常有关的疾病（如筋膜囊性肌营养不良症）的方法。
• 6-SUBSTITUTED PYRIDO-PYRIMIDINES
  申请人：F. HOFFMANN-LA ROCHE AG

  公开号：EP1361880A2

  公开（公告）日：2003-11-19
• P38 KINASE INHIBITORS REDUCE DUX4 AND DOWNSTREAM GENE EXPRESSION FOR THE TREATMENT OF FSHD
  申请人：Fulcrum Therapeutics, Inc.

  公开号：US20190105311A1

  公开（公告）日：2019-04-11

  The disclosure relates to methods and compositions including p38 kinase inhibitors and agents that regulate expression of DUX4 and downstream genes including but not restricted to ZSCAN4, LEUTX, PRAMEF2, TRIM43, MBD3L2, KHDC1L, RFPL2, CCNA1, SLC34A2, TPRX1, PRAMEF20, TRIM49, PRAMEF4, PRAME6, PRAMEF15, or ZNF280A. Methods useful for treating a disease associated with abnormal DUX4 and downstream gene expression (e.g., Facioscapulohumeral muscular dystrophy) are disclosed.
• US6696566B2
  申请人：——

  公开号：US6696566B2

  公开（公告）日：2004-02-24