3-(3-methoxyphenyl)-6-(4-methylpiperazine-1-carbonyl)-9H-carbazole-1-carboxamide | 1235463-13-4

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吲哚及其衍生物
• 英文名称: 3-(3-methoxyphenyl)-6-(4-methylpiperazine-1-carbonyl)-9H-carbazole-1-carboxamide
• CAS: 1235463-13-4
• 化学式: C₂₆H₂₆N₄O₃
• 分子量: 442.517
• InChiKey: YVYPLXQTNBRTDY-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.1
• 重原子数：
  33
• 可旋转键数：
  4
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.23
• 拓扑面积：
  91.7
• 氢给体数：
  2
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  4-[(4-甲基-1-哌嗪基)羰基]苯胺 在 四(三苯基膦)钯 、 potassium tert-butylate 、 palladium diacetate 、 sodium carbonate 作用下， 以 甲醇 、 溶剂黄146 、 二甲基亚砜 、 甲苯 为溶剂， 反应 3.0h， 生成 3-(3-methoxyphenyl)-6-(4-methylpiperazine-1-carbonyl)-9H-carbazole-1-carboxamide
  参考文献：
  名称：

  9H-Carbazole-1-carboxamides as potent and selective JAK2 inhibitors

  摘要：

  The discovery, synthesis, and characterization of 9H-carbazole-1-carboxamides as potent and selective ATP-competitive inhibitors of Janus kinase 2 (JAK2) are discussed. Optimization for JAK family selectivity led to compounds 14 and 21, with greater than 45-fold selectivity for JAK2 over all other members of the JAK kinase family. (C) 2015 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2015.04.101

文献信息

• [EN] CARBAZOLE AND CARBOLINE KINASE INHIBITORS<br/>[FR] CARBAZOLE ET INHIBITEURS DE LA CARBOLINE KINASE
  申请人：BRISTOL MYERS SQUIBB CO

  公开号：WO2010080474A1

  公开（公告）日：2010-07-15

  The present invention provides compounds of Formula (I) and pharmaceutically acceptable salts thereof. The Formula (I) compounds inhibit tyrosine kinase activity of Jak2, thereby making them useful as antiproliferative agents for the treatment of cancer and other diseases.

  本发明提供了式（I）的化合物及其药用可接受的盐。式（I）的化合物抑制Jak2的酪氨酸激酶活性，因此使它们在作为抗增殖剂治疗癌症和其他疾病方面有用。
• CARBAZOLE AND CARBOLINE KINASE INHIBITORS
  申请人：Purandare Ashok Vinayak

  公开号：US20120058988A1

  公开（公告）日：2012-03-08

  The present invention provides compounds of Formula (I) and pharmaceutically acceptable salts thereof The Formula (I) compounds inhibit tyrosine kinase activity of Jak2, thereby making them useful as antiproliferative agents for the treatment of cancer and other diseases.

  本发明提供了公式（I）的化合物及其药学上可接受的盐。公式（I）的化合物抑制Jak2的酪氨酸激酶活性，因此它们可用作抗增殖剂，用于治疗癌症和其他疾病。
• US8815840B2
  申请人：——

  公开号：US8815840B2

  公开（公告）日：2014-08-26
• 9H-Carbazole-1-carboxamides as potent and selective JAK2 inhibitors
  作者：Kurt Zimmermann、Xiaopeng Sang、Harold A. Mastalerz、Walter L. Johnson、Guifen Zhang、Qingjie Liu、Douglas Batt、Louis J. Lombardo、Dinesh Vyas、George L. Trainor、John S. Tokarski、Matthew V. Lorenzi、Dan You、Marco M. Gottardis、Jonathan Lippy、Javed Khan、John S. Sack、Ashok V. Purandare

  DOI：10.1016/j.bmcl.2015.04.101

  日期：2015.7

  The discovery, synthesis, and characterization of 9H-carbazole-1-carboxamides as potent and selective ATP-competitive inhibitors of Janus kinase 2 (JAK2) are discussed. Optimization for JAK family selectivity led to compounds 14 and 21, with greater than 45-fold selectivity for JAK2 over all other members of the JAK kinase family. (C) 2015 Elsevier Ltd. All rights reserved.