N-(1-oxo-2,3-dihydroisoindol-4-yl)formamide

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 异吲哚及其衍生物
• 英文名称: N-(1-oxo-2,3-dihydroisoindol-4-yl)formamide
• 化学式: C₉H₈N₂O₂
• 分子量: 176.17
• InChiKey: MAMFTRGYGLRHSW-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0
• 重原子数：
  13
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.11
• 拓扑面积：
  58.2
• 氢给体数：
  2
• 氢受体数：
  2

文献信息

• [EN] 4-CARBOXAMIDO-ISOINDOLINONE DERIVATIVES AS SELECTIVE PARP-1 INHIBITORS<br/>[FR] DÉRIVÉS DE 4-CARBOXAMIDO-ISOINDOLINONE EN TANT QU'INHIBITEURS SÉLECTIFS DE PARP-1
  申请人：NERVIANO MEDICAL SCIENCES SRL

  公开号：WO2014064149A1

  公开（公告）日：2014-05-01

  There are provided substituted 4-carboxamido-isoindolinone derivatives which selectively inhibit the activity of poly (ADP-ribose) polymerase PARP-1 with respect to poly (ADP-ribose) polymerase PARP-2. The compounds of this invention are therefore useful in treating diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing pharmaceutical compositions comprising these compounds.

  提供了替代的4-羧胺基异吲哚啉酮衍生物，可以选择性地抑制与PARP-2相比的聚(ADP-核糖)聚合酶PARP-1的活性。因此，本发明的化合物在治疗癌症、心血管疾病、中枢神经系统损伤和不同形式的炎症等疾病方面是有用的。本发明还提供了制备这些化合物的方法、包含这些化合物的药物组合物以及利用包含这些化合物的药物组合物治疗疾病的方法。
• 4-CARBOXAMIDO-ISOINDOLINONE DERIVATIVES AS SELECTIVE PARP-1 INHIBITORS
  申请人：NERVIANO MEDICAL SCIENCES S.R.L.

  公开号：US20150274662A1

  公开（公告）日：2015-10-01

  There are provided substituted 4-carboxamido-isoindolinone derivatives which selectively inhibit the activity of poly (ADP-ribose) polymerase PARP-1 with respect to poly (ADP-ribose) polymerase PARP-2. The compounds of this invention are therefore useful in treating diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing pharmaceutical compositions comprising these compounds.

  本发明提供了替代4-羧酰胺基异吲哚酮衍生物，其选择性地抑制聚(ADP-核糖)聚合酶PARP-1的活性，相对于聚(ADP-核糖)聚合酶PARP-2。因此，本发明的化合物可用于治疗癌症、心血管疾病、中枢神经系统损伤和不同形式的炎症等疾病。本发明还提供了制备这些化合物的方法、包含这些化合物的制药组合物以及利用包含这些化合物的制药组合物治疗疾病的方法。
• PARP genomic variants conferring resistance and sensitization to chemotherapy under inhibition
  申请人：University of Pittsburgh—Of the Commonwealth System of Higher Education

  公开号：US10260108B2

  公开（公告）日：2019-04-16

  A method is provided for selecting a subject diagnosed with cancer as a candidate for treatment with a PARP1 inhibitor, or both a PARP1 inhibitor and a chemotherapeutic agent such as an alkylating agent. The method includes detecting the presence or absence of a mutation in a non-coding region of a PARP1 gene, wherein the presence of a mutation in the PARP1 gene indicates that the cancer can be treated with the PARP1 inhibitor, optionally in conjunction with the chemotherapeutic agent. In a specific, non-limiting example, the PARP1 inhibitor is verliparib (ABT-888).

  本发明提供了一种方法，用于选择诊断为癌症的受试者作为 PARP1 抑制剂或 PARP1 抑制剂和化疗剂（如烷化剂）的候选治疗对象。该方法包括检测 PARP1 基因非编码区中是否存在突变，其中 PARP1 基因中突变的存在表明癌症可以用 PARP1 抑制剂治疗，可以选择与化疗剂一起使用。在一个具体的、非限制性的例子中，PARP1 抑制剂是 verliPARib（ABT-888）。
• 4-carboxamido-isoindolinone derivatives as selective PARP-1 inhibitors
  申请人：NERVIANO MEDICAL SCIENCES S.r.l

  公开号：US10385018B2

  公开（公告）日：2019-08-20

  There are provided substituted 4-carboxamido-isoindolinone derivatives which selectively inhibit the activity of poly (ADP-ribose) polymerase PARP-1 with respect to poly (ADP-ribose) polymerase PARP-2. The compounds of this invention are therefore useful in treating diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing pharmaceutical compositions comprising these compounds.

  本发明提供了取代的 4-甲酰胺基异吲哚啉酮衍生物，相对于多（ADP-核糖）聚合酶 PARP-2 而言，它们能选择性地抑制多（ADP-核糖）聚合酶 PARP-1 的活性。因此，本发明的化合物可用于治疗癌症、心血管疾病、中枢神经系统损伤和不同形式的炎症等疾病。本发明还提供了制备这些化合物的方法、包含这些化合物的药物组合物，以及利用包含这些化合物的药物组合物治疗疾病的方法。
• CDK MODULATORS AND METHODS FOR THE TREATMENT OF CANCER
  申请人：Salk Institute for Biological Studies

  公开号：US20170157212A1

  公开（公告）日：2017-06-08

  Disclosed is a polypeptide that includes amino acids 183-222 of CRIF, wherein the polypeptide does not include the full length CRIF1 amino acid sequence. Also disclosed is a nucleic acid molecule encoding this polypeptide, vectors including this nucleic acid molecule, and host cells transformed with these vectors. In some embodiments, methods are disclosed for treating a subject with cancer, comprising administering to the subject a therapeutically effective amount of an inhibitor of CDK12/CRIF1 interaction, thereby treating the cancer in the subject. In specific non-limiting examples, these methods can utilize CRIF1 polypeptides, nucleic acids encoding these polypeptides, and vectors including these nucleic acids.