4-bromo-2-(((2-hydroxypropyl)amino)methyl)phenol

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 4-bromo-2-(((2-hydroxypropyl)amino)methyl)phenol
• 英文别名: 4-Bromo-2-[(2-hydroxypropylamino)methyl]phenol；4-bromo-2-[(2-hydroxypropylamino)methyl]phenol
• 化学式: C₁₀H₁₄BrNO₂
• 分子量: 260.131
• InChiKey: RHKJYEOKGPJIFH-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.7
• 重原子数：
  14
• 可旋转键数：
  4
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.4
• 拓扑面积：
  52.5
• 氢给体数：
  3
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  4-bromo-2-(((2-hydroxypropyl)amino)methyl)phenol 在 偶氮二甲酸二异丙酯 、 dichloro[1,3-bis(2,6-di-3-pentylphenyl)imidazol-2-ylidene](3-chloropyridyl)palladium(II) 、 水 、 三苯基膦 、 sodium hydroxide 、 sodium t-butanolate 作用下， 以 四氢呋喃 、 1,4-二氧六环 、 甲醇 为溶剂， 反应 30.0h， 生成 tert-butyl 7-(7-(difluoromethyl)-6-(1-methyl-1H-pyrazol-4-yl)-3,4-dihydroquinolin-1(2H)-yl)-2-methyl-2,3-dihydrobenzo[f][1,4]oxazepine-4(5H)-carboxylate
  参考文献：
  名称：

  [EN] HETEROCYCLIC INHIBITORS OF CBP/EP300 AND THEIR USE IN THE TREATMENT OF CANCER
  [FR] COMPOSÉS THÉRAPEUTIQUES ET LEURS UTILISATIONS

  摘要：

  公开号：

  WO2017205536A3
• 作为产物：
  描述：

  异丙醇胺 、 5-溴水杨醛 在 甲醇 、 sodium tetrahydroborate 作用下， 以 甲醇 为溶剂， 生成 4-bromo-2-(((2-hydroxypropyl)amino)methyl)phenol
  参考文献：
  名称：

  [EN] HETEROCYCLIC INHIBITORS OF CBP/EP300 AND THEIR USE IN THE TREATMENT OF CANCER
  [FR] COMPOSÉS THÉRAPEUTIQUES ET LEURS UTILISATIONS

  摘要：

  公开号：

  WO2017205536A3

文献信息

• Therapeutic compounds and uses thereof
  申请人：GENENTECH, INC.

  公开号：US10696655B2

  公开（公告）日：2020-06-30

  The present invention relates to compounds of formula (I) and formula (II): and to salts thereof, wherein R1-R4 of formula (I) and R5-R6 of formula (II) have any of the values defined herein, and compositions and uses thereof. The compounds are useful as inhibitors of CBP and/or EP300. Also included are pharmaceutical compositions comprising a compound of formula (I) of formula (II), or a pharmaceutically acceptable salt thereof, and methods of using such compounds and salts in the treatment of various CBP and/or EP300-mediated disorders.

  本发明涉及式（I）和式（II）化合物： 及其盐，其中式(I)的 R1-R4 和式(II)的 R5-R6 具有本文定义的任一值，以及其组合物和用途。这些化合物可用作 CBP 和/或 EP300 的抑制剂。还包括包含式(I)的式(II)的化合物或其药学上可接受的盐的药物组合物，以及使用这种化合物和盐治疗各种CBP和/或EP300介导的疾病的方法。
• HETEROCYCLIC INHIBITORS OF CBP/EP300 AND THEIR USE IN THE TREATMENT OF CANCER
  申请人：Genentech, Inc.

  公开号：EP3464270A2

  公开（公告）日：2019-04-10
• THERAPEUTIC COMPOUNDS AND USES THEREOF
  申请人：GENENTECH, INC.

  公开号：US20190152949A1

  公开（公告）日：2019-05-23

  The present invention relates to compounds of formula (I) and formula (II): and to salts thereof, wherein R 1 -R 4 of formula (I) and R 5 -R 6 of formula (II) have any of the values defined herein, and compositions and uses thereof. The compounds are useful as inhibitors of CBP and/or EP300. Also included are pharmaceutical compositions comprising a compound of formula (I) of formula (II), or a pharmaceutically acceptable salt thereof, and methods of using such compounds and salts in the treatment of various CBP and/or EP300-mediated disorders.
• [EN] THERAPEUTIC COMPOUNDS AND USES THEREOF<br/>[FR] COMPOSÉS THÉRAPEUTIQUES ET LEURS UTILISATIONS
  申请人：GENENTECH INC

  公开号：WO2017205536A2

  公开（公告）日：2017-11-30

  The present invention relates to compounds of formula (I) and formula (II): and to salts thereof, wherein R1-R4 of formula (I) and R5-R6 of formula (II) have any of the values defined herein, and compositions and uses thereof. The compounds are useful as inhibitors of CBP and/or EP300. Also included are pharmaceutical compositions comprising a compound of formula (I) of formula (II), or a pharmaceutically acceptable salt thereof, and methods of using such compounds and salts in the treatment of various CBP and/or EP300-mediated disorders.
• [EN] HETEROCYCLIC INHIBITORS OF CBP/EP300 AND THEIR USE IN THE TREATMENT OF CANCER<br/>[FR] COMPOSÉS THÉRAPEUTIQUES ET LEURS UTILISATIONS
  申请人：GENENTECH INC

  公开号：WO2017205536A3

  公开（公告）日：2018-01-04