2-[1-(4-cyano-2-fluorophenyl)7-methoxy-3-methyl-2-oxo-2,3-dihydro-1H-imidazo[4,5-c]quinolin-8-yloxy]-2-phenyl-acetamide | 1360628-71-2

• 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-[1-(4-cyano-2-fluorophenyl)7-methoxy-3-methyl-2-oxo-2,3-dihydro-1H-imidazo[4,5-c]quinolin-8-yloxy]-2-phenyl-acetamide
• 英文别名: 2-[1-(4-Cyano-2-fluorophenyl)-7-methoxy-3-methyl-2-oxoimidazo[4,5-c]quinolin-8-yl]oxy-2-phenylacetamide
• CAS: 1360628-71-2
• 化学式: C₂₇H₂₀FN₅O₄
• 分子量: 497.485
• InChiKey: WSSRLEJNWLBFLX-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.2
• 重原子数：
  37
• 可旋转键数：
  6
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.11
• 拓扑面积：
  122
• 氢给体数：
  1
• 氢受体数：
  7

文献信息

• [EN] METHOD FOR TREATING CANCER USING A COMBINATION OF DNA-DAMAGING AGENTS AND DNA-PK INHIBITORS<br/>[FR] MÉTHODE DE TRAITEMENT DU CANCER UTILISANT UNE COMBINAISON D'AGENTS ENDOMMAGEANT L'ADN ET D'INHIBITEURS DE LA DNA-PK
  申请人：VERTEX PHARMA

  公开号：WO2018064092A1

  公开（公告）日：2018-04-05

  Described herein are methods of treating a proliferative disease in a subject by administering a DNA-damaging agent and between about 8 and about 48 hours later administering to the subject a DNA-PK inhibitor. Exemplary DNA-PK inhibitors are represented by Formula (B-I): and by pharmaceutically acceptable salts thereof, wherein R1, Q, Ring A, and Ring B are as defined herein.

  本文描述了一种治疗患者增殖性疾病的方法，包括向患者施用DNA损伤剂，然后在大约8到48小时后向患者施用DNA-PK抑制剂。示例的DNA-PK抑制剂由Formula（B-I）代表，并且其药用盐，其中R1、Q、环A和环B的定义如本文所述。
• Imidazo[4,5-c]quinolines as DNA-PK inhibitors
  申请人：Fuchss Thomas

  公开号：US20130172337A1

  公开（公告）日：2013-07-04

  The invention relates to compounds of the formulae (I) and (II) in which R1, R2, R3, R4, R5, R8, X and m have the meaning indicated in the claims, and/or physiologically acceptable salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios. The compounds of the formula (I) can be used for the inhibition of serine/threonine protein kinases and for the sensitisation of cancer cells to anticancer agents and/or ionising radiation. The invention also relates to the use of the compounds of the formula (I) in the prophylaxis, therapy or progress control of cancer, tumours, metastases or angiogenesis disorders, in combination with radiotherapy and/or an anticancer agent. The invention furthermore relates to a process for the preparation of the compounds of the formula (I).

  该发明涉及公式（I）和（II）中的化合物，其中R1、R2、R3、R4、R5、R8、X和m具有声明中指示的含义，及/或其生理上可接受的盐、互变异构体和立体异构体，包括所有比例的混合物。公式（I）的化合物可用于抑制丝氨酸/苏氨酸蛋白激酶，以及使癌细胞对抗癌药物和/或电离辐射敏感。该发明还涉及在预防、治疗或进展控制癌症、肿瘤、转移或血管生成障碍方面使用公式（I）的化合物，与放射治疗和/或抗癌药物结合。此外，该发明还涉及一种制备公式（I）化合物的方法。
• IMIDAZO[4,5-C]QUINOLINES AS DNA-PK INHIBITORS
  申请人：MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNG

  公开号：US20150203491A1

  公开（公告）日：2015-07-23

  The invention relates to compounds of the formulae (I) and (II) in which R1, R2, R3, R4, R5, R8, X and m have the meaning indicated in the claims, and/or physiologically acceptable salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios. The compounds of the formula (I) can be used for the inhibition of serine/threonine protein kinases and for the sensitisation of cancer cells to anticancer agents and/or ionising radiation. The invention also relates to the use of the compounds of the formula (I) in the prophylaxis, therapy or progress control of cancer, tumours, metastases or angiogenesis disorders, in combination with radiotherapy and/or an anticancer agent. The invention furthermore relates to a process for the preparation of the compounds of the formula (I).

  本发明涉及式（I）和（II）化合物，其中R1、R2、R3、R4、R5、R8、X和m具有所述权利要求中所示的含义，以及/或其生理上可接受的盐、互变异构体和立体异构体，包括所有比例的混合物。式（I）化合物可用于抑制丝氨酸/苏氨酸蛋白激酶，并使癌细胞对抗癌药物和/或电离辐射产生敏感性。本发明还涉及将式（I）化合物与放射治疗和/或抗癌药物结合在一起，在预防、治疗或进展控制癌症、肿瘤、转移或血管生成障碍方面使用该化合物。本发明还涉及制备式（I）化合物的方法。
• Method for treating cancer using a combination of DNA-damaging agents and DNA-PK inhibitors
  申请人：Vertex Pharmaceuticals Incorporated

  公开号：US11110108B2

  公开（公告）日：2021-09-07

  Described herein are methods of treating a proliferative disease in a subject by administering a DNA-damaging agent and between about 8 and about 48 hours later administering to the subject a DNA-PK inhibitor. Exemplary DNA-PK inhibitors are represented by Formula (B-I): and by pharmaceutically acceptable salts thereof, wherein R1, Q, Ring A, and Ring B are as defined herein.

  本文描述了通过给受试者施用 DNA 损伤剂并在约 8 至约 48 小时后给受试者施用 DNA-PK 抑制剂来治疗增殖性疾病的方法。示例性DNA-PK抑制剂由式（B-I）及其药学上可接受的盐表示，其中R1、Q、环A和环B如本文所定义。
• IMIDAZO[4,5-C]CHINOLINE ALS DNA-PK-INHIBITOREN
  申请人：Merck Patent GmbH

  公开号：EP2609082B1

  公开（公告）日：2015-02-18