7-fluoro-3-methyl-8-[6-[3-(1-piperidyl)propoxy]-3-pyridyl]-1-tetrahydropyran-4-yl-imidazo[4,5-c]quinolin-2-one

• 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: 7-fluoro-3-methyl-8-[6-[3-(1-piperidyl)propoxy]-3-pyridyl]-1-tetrahydropyran-4-yl-imidazo[4,5-c]quinolin-2-one
• 英文别名: 7-Fluoro-3-methyl-8-[6-[3-(1-piperidyl)propoxy]-3-pyridyl]-1-tetrahydropyran-4-yl-imidazo[4,5-c]quinolin-2-one；7-fluoro-3-methyl-1-(oxan-4-yl)-8-[6-(3-piperidin-1-ylpropoxy)pyridin-3-yl]imidazo[4,5-c]quinolin-2-one
• 化学式: C₂₉H₃₄FN₅O₃
• 分子量: 519.619
• InChiKey: QHRPXFUAYFWEPQ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.8
• 重原子数：
  38
• 可旋转键数：
  7
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.48
• 拓扑面积：
  71
• 氢给体数：
  0
• 氢受体数：
  7

反应信息

• 作为产物：
  描述：

  1-哌啶丙醇 、 7-fluoro-8-(6-fluoro-3-pyridyl)-3-methyl-1-tetrahydropyran-4-yl-imidazo[4,5-c]quinolin-2-one 在 sodium hydride 作用下， 以 四氢呋喃 为溶剂， 反应 24.52h， 以56%的产率得到7-fluoro-3-methyl-8-[6-[3-(1-piperidyl)propoxy]-3-pyridyl]-1-tetrahydropyran-4-yl-imidazo[4,5-c]quinolin-2-one
  参考文献：
  名称：

  [EN] IMIDAZO[4,5-C]QUINOLIN-2-ONE COMPOUNDS AND THEIR USE IN TREATING CANCER
  [FR] COMPOSÉS IMIDAZO[4,5C]QUINOLINE-2-ONE ET LEUR UTILISATION DANS LE TRAITEMENT DU CANCER

  摘要：

  该规范通常涉及式(I)的化合物及其药用盐，其中Q、R1、R2、R3、R4和R5具有本规范中定义的任何含义。该规范还涉及使用这些化合物和其盐来治疗或预防ATM激酶介导的疾病，包括癌症。该规范还涉及咪唑并[4,5- c]喹啉-2-酮化合物的结晶形式及其药用盐；包含这些化合物和盐的药物组合物；包含这些化合物和盐的试剂盒；这些化合物和盐的制造方法；用于制造这些化合物和盐的中间体；以及使用这些化合物和盐治疗ATM激酶介导的疾病，包括癌症的方法。

  公开号：

  WO2015170081A1

文献信息

• Imidazo[4,5-c]quinolin-2-one Compounds and Their Use in Treating Cancer
  申请人：AstraZeneca AB

  公开号：US20150336952A1

  公开（公告）日：2015-11-26

  The specification generally relates to compounds of Formula (I): and pharmaceutically acceptable salts thereof, where Q, R 1 , R 2 , R 3 , R 4 and R 5 have any of the meanings defined herein. The specification also relates to the use of such compounds and salts thereof to treat or prevent ATM kinase mediated disease, including cancer. The specification further relates to crystalline forms of compounds of imidazo[4,5-c]quinolin-2-one compounds and pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising such compounds and salts; kits comprising such compounds and salts; methods of manufacture of such compounds and salts; intermediates useful in the manufacture of such compounds and salts; and to methods of treating ATM kinase mediated disease, including cancer, using such compounds and salts.

  本规范一般涉及公式（I）的化合物及其药学上可接受的盐，其中Q、R1、R2、R3、R4和R5具有此处定义的任何含义。本规范还涉及使用这些化合物及其盐来治疗或预防ATM激酶介导的疾病，包括癌症。本规范还涉及咪唑并[4,5-c]喹啉-2-酮化合物的晶体形式及其药学上可接受的盐；包含这些化合物和盐的药物组合物；包含这些化合物和盐的试剂盒；制造这些化合物和盐的方法；在制造这些化合物和盐的中间体中有用的中间体；以及使用这些化合物和盐治疗ATM激酶介导的疾病，包括癌症的方法。
• Imidazo[4,5-c]quinolin-2-one compounds and their use in treating Cancer
  申请人：AstraZeneca AB

  公开号：US09428503B2

  公开（公告）日：2016-08-30

  The specification generally relates to compounds of Formula (I): and pharmaceutically acceptable salts thereof, where Q, R1, R2, R3, R4 and R5 have any of the meanings defined herein. The specification also relates to the use of such compounds and salts thereof to treat or prevent ATM kinase mediated disease, including cancer. The specification further relates to crystalline forms of compounds of imidazo[4,5-c]quinolin-2-one compounds and pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising such compounds and salts; kits comprising such compounds and salts; methods of manufacture of such compounds and salts; intermediates useful in the manufacture of such compounds and salts; and to methods of treating ATM kinase mediated disease, including cancer, using such compounds and salts.

  该规范通常涉及公式（I）的化合物及其药学上可接受的盐，其中Q，R1，R2，R3，R4和R5具有本文所定义的任何含义。该规范还涉及使用这些化合物及其盐来治疗或预防ATM激酶介导的疾病，包括癌症。该规范进一步涉及咪唑[4,5-c]喹啉-2-酮化合物的晶体形式及其药学上可接受的盐；包含这些化合物和盐的制药组合物；包含这些化合物和盐的工具包；制造这些化合物和盐的方法；在制造这些化合物和盐的中间体；以及使用这些化合物和盐治疗ATM激酶介导的疾病，包括癌症的方法。
• Imidazo[4,5-c]quinolin-2-one compounds and their use in treating cancer
  申请人：AstraZeneca AB

  公开号：US10189834B2

  公开（公告）日：2019-01-29

  The specification generally relates to compounds of Formula (I): and pharmaceutically acceptable salts thereof, where Q, R1, R2, R3, R4 and R5 have any of the meanings defined herein. The specification also relates to the use of such compounds and salts thereof to treat or prevent ATM kinase mediated disease, including cancer. The specification further relates to crystalline forms of compounds of imidazo[4,5-c]quinolin-2-one compounds and pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising such compounds and salts; kits comprising such compounds and salts; methods of manufacture of such compounds and salts; intermediates useful in the manufacture of such compounds and salts; and to methods of treating ATM kinase mediated disease, including cancer, using such compounds and salts.

  本说明书一般涉及式 (I) 化合物： 及其药学上可接受的盐，其中 Q、R1、R2、R3、R4 和 R5 具有本文定义的任何含义。本说明书还涉及使用此类化合物及其盐治疗或预防 ATM 激酶介导的疾病，包括癌症。本说明书进一步涉及咪唑并[4,5-c]喹啉-2-酮化合物的结晶形式及其药学上可接受的盐；包含此类化合物和盐的药物组合物；包含此类化合物和盐的试剂盒；制造此类化合物和盐的方法；制造此类化合物和盐有用的中间体；以及使用此类化合物和盐治疗ATM激酶介导的疾病（包括癌症）的方法。
• IMIDAZO[4,5-C]QUINOLIN-2-ONE COMPOUNDS AND THEIR USE IN TREATING CANCER
  申请人：Astrazeneca AB

  公开号：EP3140303B1

  公开（公告）日：2018-03-28
• US9428503B2
  申请人：——

  公开号：US9428503B2

  公开（公告）日：2016-08-30