2-(4-(8-(2-aminobenzo[d]oxazol-5-yl)-3-methyl-2-oxo-2,3-dihydro-1H-imidazo[4,5-c]quinolin-1-yl)phenyl)-2-methylpropanenitril | 1395145-15-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 喹啉及其衍生物
• 英文名称: 2-(4-(8-(2-aminobenzo[d]oxazol-5-yl)-3-methyl-2-oxo-2,3-dihydro-1H-imidazo[4,5-c]quinolin-1-yl)phenyl)-2-methylpropanenitril
• 英文别名: 2-[4-[8-(2-Amino-1,3-benzoxazol-5-yl)-3-methyl-2-oxoimidazo[4,5-c]quinolin-1-yl]phenyl]-2-methylpropanenitrile
• CAS: 1395145-15-9
• 化学式: C₂₈H₂₂N₆O₂
• 分子量: 474.522
• InChiKey: HNFHHKPKXPNFKY-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.5
• 重原子数：
  36
• 可旋转键数：
  3
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.14
• 拓扑面积：
  112
• 氢给体数：
  1
• 氢受体数：
  6

反应信息

• 作为产物：
  描述：

  2-(4-(3-氨基-6-溴喹啉-4-基氨基)苯基)-2-甲基丙腈 在 四(三苯基膦)钯 、 sodium carbonate 、 三乙胺 作用下， 以 乙醇 、 二氯甲烷 、 水 、 N,N-二甲基甲酰胺 为溶剂， 反应 3.0h， 生成 2-(4-(8-(2-aminobenzo[d]oxazol-5-yl)-3-methyl-2-oxo-2,3-dihydro-1H-imidazo[4,5-c]quinolin-1-yl)phenyl)-2-methylpropanenitril
  参考文献：
  名称：

  COMBINATION OF KINASE INHIBITORS AND USES THEREOF

  摘要：

  本发明提供了一种治疗与PI3-激酶a和/或受体酪氨酸激酶（RTK）有关的疾病状况的方法。另一方面，该发明提供了一种治疗与PI3-激酶α和/或受体酪氨酸激酶（RTK）有关的疾病状况的方法。另一方面，提出了一种抑制细胞中Akt（S473）磷酸化的方法。

  公开号：

  US20150030588A1

文献信息

• [EN] COMBINATION OF KINASE INHIBITORS AND USES THEREOF<br/>[FR] COMBINAISON D'INHIBITEURS DE KINASE ET SES UTILISATIONS
  申请人：INTELLIKINE LLC

  公开号：WO2014151147A1

  公开（公告）日：2014-09-25

  The present invention provides for a method for treating a disease condition associated with PI3-kinase a and/or mTOR in a subject. In another aspect, the invention provides for a method for treating a disease condition associated with PI3-kinase a and/or mTOR in a subject. In yet another aspect, a method of inhibiting phosphorylation of both Akt (S473) and Akt (T308) in a cell is set forth. The present invention also provides a pharmaceutical kit effective for treating a disease condition associated with PI3 -kinase α and/or mTOR in a subject.

  本发明提供了一种治疗与受体内PI3-激酶α和/或mTOR相关的疾病状况的方法。另一方面，该发明提供了一种治疗与受体内PI3-激酶α和/或mTOR相关的疾病状况的方法。在另一个方面，提出了一种抑制细胞内Akt（S473）和Akt（T308）磷酸化的方法。本发明还提供了一种有效治疗与受体内PI3-激酶α和/或mTOR相关的疾病状况的药物套装。
• HETEROCYCLIC COMPOUNDS AND USES THEREOF
  申请人：Intellikine LLC

  公开号：US20150320727A1

  公开（公告）日：2015-11-12

  Heterocyclic entities that modulate PI3 kinase activity, pharmaceutical compositions containing the heterocyclic entities, and methods of using these chemical entities for treating diseases and conditions associated with PI3 kinase activity are described herein.

  本文描述了调节PI3激酶活性的杂环实体、含有这些杂环实体的药物组合物，以及利用这些化学实体治疗与PI3激酶活性相关的疾病和症状的方法。
• [EN] HETEROCYCLIC COMPOUNDS AND USES THEREOF<br/>[FR] COMPOSÉS HÉTÉROCYCLIQUES ET LEURS UTILISATIONS
  申请人：INTELLIKINE LLC

  公开号：WO2012116237A3

  公开（公告）日：2012-12-27
• Combination of Kinase Inhibitors and Uses Thereof
  申请人：INTELLIKINE, LLC

  公开号：US20160089371A1

  公开（公告）日：2016-03-31

  The present invention provides for a method for treating a disease condition associated with PI3-kinase a and/or mTOR in a subject. In another aspect, the invention provides for a method for treating a disease condition associated with PI3-kinase a and/or mTOR in a subject. In yet another aspect, a method of inhibiting phosphorylation of both Akt (S473) and Akt (T308) in a cell is set forth. The present invention also provides a pharmaceutical kit effective for treating a disease condition associated with PI3-kinase α and/or mTOR in a subject.
• COMBINATION OF MTOR INHIBITORS AND PI3-KINASE INHIBITORS, AND USES THEREOF
  申请人：Intellikine LLC

  公开号：US20160235758A1

  公开（公告）日：2016-08-18

  The present invention provides for a method for treating a disease condition associated with PI3-kinase α and/or mTOR in a subject. In another aspect, the invention provides for a method for treating a disease condition associated with PI3-kinase α and/or mTOR in a subject. In yet another aspect, a method of inhibiting phosphorylation of both Akt (S473) and Akt (T308) in a cell is set forth.