4-(1-piperazinyl)-1(2H)-phthalazinone | 464169-24-2

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪烷类
• 英文名称: 4-(1-piperazinyl)-1(2H)-phthalazinone
• 英文别名: 4-piperazin-1-yl-2H-phthalazin-1-one
• CAS: 464169-24-2
• 化学式: C₁₂H₁₄N₄O
• 分子量: 230.269
• InChiKey: BBCZHKSGWVHFKZ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0
• 重原子数：
  17
• 可旋转键数：
  1
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  56.7
• 氢给体数：
  2
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  1-氯-3-碘丙烷 、 4-(1-piperazinyl)-1(2H)-phthalazinone 在 sodium hydride 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 1.0h， 生成
  参考文献：
  名称：

  4-Aminophthalazin-1(2H)-one Derivatives as Melanin Concentrating Hormone Receptor 1 (MCH-R1) Antagonists

  摘要：

  DOI：

  10.5012/bkcs.2013.34.12.3851
• 作为产物：
  描述：

  1,4-二氯酞嗪 在 potassium carbonate 、 溶剂黄146 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 6.0h， 生成 4-(1-piperazinyl)-1(2H)-phthalazinone
  参考文献：
  名称：

  4-Aminophthalazin-1(2H)-one Derivatives as Melanin Concentrating Hormone Receptor 1 (MCH-R1) Antagonists

  摘要：

  DOI：

  10.5012/bkcs.2013.34.12.3851

文献信息

• Dna damage repair inhibitors for treatment of cancer
  申请人：Kudos Pharmaceuticals Limited

  公开号：EP2305221A1

  公开（公告）日：2011-04-06

  The present invention relates to the recognition that inhibition of the base excision repair pathway is selectively lethal in cells which are deficient in HR dependent DNA DSB repair. Methods and means relating to the treatment of cancers which are deficient in HR dependent DNA DSB repair using inhibitors which target base excision repair components, such as PARP, is provided herein.

  本发明涉及一种认识，即抑制碱基切除修复途径对缺乏 HR 依赖性 DNA DSB 修复的细胞具有选择性致死作用。本发明提供了使用靶向碱基切除修复成分（如 PARP）的抑制剂治疗缺乏 HR 依赖性 DNA DSB 修复的癌症的方法和手段。
• Use of a combination of Dbait molecule and PARP inhibitors to treat cancer
  申请人：INSTITUT CURIE

  公开号：US10563197B2

  公开（公告）日：2020-02-18

  The present invention relates to the combination of a PARP inhibitor with a Dbait molecule for treating cancer.

  本发明涉及 PARP 抑制剂与 Dbait 分子的组合，用于治疗癌症。
• Combination of an inhibitor of PARP with an inhibitor of GSK-3 or DOT1L
  申请人：King's College London

  公开号：US10799501B2

  公开（公告）日：2020-10-13

  Provided herein is a pharmaceutical combination comprising (a) a poly-(ADP-ribose)-polymerase (PARP) inhibitor and (b) a second agent comprising (i) an inhibitor of glycogen synthase kinase 3 (GSK-3) or (ii) an inhibitor of disrupter of telomeric silencing 1-like (DOT1L). Also provided is a method of treating a subject suffering from acute myeloid leukaemia, comprising administering to the subject a therapeutically effective amount of the pharmaceutical combination. There is also described herein a method for selecting a therapy for a subject suffering from acute myeloid leukaemia, comprising determining whether a chromosomal abnormality at 11q23 is present in a sample obtained from the subject; wherein if the chromosomal abnormality at 11q23 is present in the sample, a therapy comprising combined administration of (a) a poly-(ADP-ribose)-polymerase (PARP) inhibitor and (b) a second agent comprising (i) an inhibitor of glycogen synthase kinase 3 (GSK-3) or (ii) an inhibitor of disrupter of telomeric silencing 1-like (DOT1L) is selected for the subject.

  本文提供了一种药物组合，包括(a)聚（ADP-核糖）聚合酶（PARP）抑制剂和(b)第二种药物，包括(i)糖原合酶激酶 3（GSK-3）抑制剂或(ii)端粒沉默 1-样（DOT1L）干扰素抑制剂。还提供了一种治疗急性髓性白血病患者的方法，包括向患者施用治疗有效量的药物组合。本文还描述了一种为患有急性髓性白血病的受试者选择疗法的方法，包括确定从受试者处获得的样本中是否存在 11q23 染色体异常；其中，如果样本中存在 11q23 染色体异常，则为受试者选择一种疗法，该疗法包括联合给药(a)聚（ADP 核糖）聚合酶（PARP）抑制剂和(b)第二种药剂，第二种药剂包括(i)糖原合酶激酶 3（GSK-3）抑制剂或(ii)端粒沉默 1-样破坏者（DOT1L）抑制剂。
• DNA damage repair inhibitors for the treatment of cancer
  申请人：Ashworth Alan

  公开号：US20050227919A1

  公开（公告）日：2005-10-13

  The present invention relates to the recognition that inhibition of the base excision repair pathway is selectively lethal in cells which are deficient in HR dependent DNA DSB repair. Methods and means relating to the treatment of cancers which are deficient in HR dependent DNA DSB repair using inhibitors which target base excision repair components, such as PARP, is provided herein.

  本发明涉及一种认识，即抑制碱基切除修复途径对缺乏 HR 依赖性 DNA DSB 修复的细胞具有选择性致死作用。本发明提供了使用靶向碱基切除修复成分（如 PARP）的抑制剂治疗缺乏 HR 依赖性 DNA DSB 修复的癌症的方法和手段。
• DNA DAMAGE REPAIR INHIBITORS FOR TREATMENT OF CANCER
  申请人：Kudos Pharmaceuticals Limited

  公开号：EP1684736B1

  公开（公告）日：2011-08-24