8-chloro-7-fluoroisoquinolin-3-yl trifluoromethanesulfonate | 1175272-64-6

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 异喹啉及其衍生物
• 英文名称: 8-chloro-7-fluoroisoquinolin-3-yl trifluoromethanesulfonate
• 英文别名: 8-Chloro-7-fluoroisoquinolin-3-yl trifluoromethanesulfonate；(8-chloro-7-fluoroisoquinolin-3-yl) trifluoromethanesulfonate
• CAS: 1175272-64-6
• 化学式: C₁₀H₄ClF₄NO₃S
• 分子量: 329.659
• InChiKey: SJLSJZODWXBRGY-UHFFFAOYSA-N

物化性质

• 沸点：
  405.2±45.0 °C(Predicted)
• 密度：
  1.696±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  3.9
• 重原子数：
  20
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.1
• 拓扑面积：
  64.6
• 氢给体数：
  0
• 氢受体数：
  8

反应信息

• 作为反应物：
  描述：

  8-chloro-7-fluoroisoquinolin-3-yl trifluoromethanesulfonate 在 (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride 、 tris-(dibenzylideneacetone)dipalladium(0) 、 potassium acetate 、 potassium carbonate 、 三环己基膦 作用下， 以 四氢呋喃 、 1,4-二氧六环 、 水 为溶剂， 反应 24.0h， 生成 5-(8-(7-acetyl-3-(tetrahydro-2H-pyran-4-yl)-5,6,7,8-tetrahydroimidazo[1,5-a]pyrazin-1-yl)-7-fluoroisoquinolin-3-yl)-N-methylpicolinamide
  参考文献：
  名称：

  [EN] IMIDAZOPIPERAZINE INHIBITORS OF TRANSCRIPTION ACTIVATING PROTEINS
  [FR] INHIBITEURS IMIDAZOPIPÉRAZINE DE PROTÉINES D'ACTIVATION DE LA TRANSCRIPTION

  摘要：

  本公开涉及杂环化合物和方法，这些方法可能作为转录激活蛋白（例如CBP和P300）的抑制剂，用于治疗或预防增生性疾病、炎症性疾病、自身免疫性疾病和纤维化疾病。

  公开号：

  WO2022072648A1
• 作为产物：
  描述：

  2-氯-3-氟苯甲胺 在 硫酸 、 三乙胺 作用下， 以 二氯甲烷 、 水 为溶剂， 反应 3.0h， 生成 8-chloro-7-fluoroisoquinolin-3-yl trifluoromethanesulfonate
  参考文献：
  名称：

  [EN] IMIDAZOPIPERAZINE INHIBITORS OF TRANSCRIPTION ACTIVATING PROTEINS
  [FR] INHIBITEURS IMIDAZOPIPÉRAZINE DE PROTÉINES D'ACTIVATION DE LA TRANSCRIPTION

  摘要：

  本公开涉及杂环化合物和方法，这些方法可能作为转录激活蛋白（例如CBP和P300）的抑制剂，用于治疗或预防增生性疾病、炎症性疾病、自身免疫性疾病和纤维化疾病。

  公开号：

  WO2022072648A1

文献信息

• IMIDAZOPIPERAZINE INHIBITORS OF TRANSCRIPTION ACTIVATING PROTEINS
  申请人：Board of Regents, The University of Texas System

  公开号：US20190298729A1

  公开（公告）日：2019-10-03

  The present disclosure relates to heterocyclic compounds and methods which may be useful as inhibitors of transcription activating proteins such as CBP and P300 for the treatment or prevention of diseases such as proliferative diseases, inflammatory disorders, autoimmune diseases, and fibrotic diseases.

  本公开涉及杂环化合物和方法，这些方法可能作为转录激活蛋白（如CBP和P300）的抑制剂，用于治疗或预防增殖性疾病、炎症性疾病、自身免疫疾病和纤维化疾病。
• IMIDAZOPIPERAZINONE INHIBITORS OF TRANSCRIPTION ACTIVATING PROTEINS
  申请人：Board of Regents, The University of Texas System

  公开号：US20190308978A1

  公开（公告）日：2019-10-10

  The present disclosure relates to heterocyclic compounds and methods which may be useful as inhibitors of transcription activating proteins such as CBP and P300 for the treatment or prevention of diseases such as proliferative diseases, inflammatory disorders, autoimmune diseases, and fibrotic diseases.

  本公开涉及可能用作转录激活蛋白如CBP和P300的抑制剂，用于治疗或预防诸如增殖性疾病、炎症性疾病、自身免疫疾病和纤维化疾病的异环化合物和方法。
• 2-AMINOPYRIDINE KINASE INHIBITORS
  申请人：Steinig Arno G.

  公开号：US20090197862A1

  公开（公告）日：2009-08-06

  2-Aminopyridine compounds having the structure of Formula I, and pharmaceutically acceptable salts of these compounds. Compounds of Formula I inhibit the activity of tyrosine kinase enzymes in animals, including humans, and are useful in the treatment and/or prevention of various diseases and conditions. In particular, compounds disclosed herein are inhibitors of kinases, in particular, but not limited to, KDR, Tie-2, Flt3, FGFR3, Ab1, Aurora A, c-Src, IGF-1R, ALK, c-MET, RON, PAK1, PAK2, and TAK1, and can be used in the treatment of proliferative diseases, such as, but not limited to, cancer. The present invention is also directed to a pharmaceutical composition comprising a therapeutically effective amount of a compound of Formula I, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier. The present invention is further directed to a method of treating a patient having a condition which is mediated by protein kinase activity by administering to the patient a therapeutically effective amount of the above-mentioned pharmaceutical composition.

  具有Formula I结构的2-氨基吡啶化合物，以及这些化合物的药用可接受的盐。Formula I的化合物抑制动物（包括人类）中的酪氨酸激酶酶活性，并可用于治疗和/或预防各种疾病和病况。特别地，本文披露的化合物是激酶抑制剂，特别是但不限于KDR、Tie-2、Flt3、FGFR3、Ab1、Aurora A、c-Src、IGF-1R、ALK、c-MET、RON、PAK1、PAK2和TAK1，并可用于治疗增生性疾病，如但不限于癌症。本发明还涉及一种包含Formula I化合物的药物组合物，或其药用可接受的盐，以及药用可接受的载体的药物组合物。本发明还涉及一种通过向患有由蛋白激酶活性介导的病症的患者投与上述药物组合物的治疗方法。
• Imidazopiperazinone inhibitors of transcription activating proteins
  申请人：Board of Regents, The University of Texas System

  公开号：US10899769B2

  公开（公告）日：2021-01-26

  The present disclosure relates to heterocyclic compounds and methods which may be useful as inhibitors of transcription activating proteins such as CBP and P300 for the treatment or prevention of diseases such as proliferative diseases, inflammatory disorders, autoimmune diseases, and fibrotic diseases.

  本公开涉及杂环化合物和方法，它们可用作转录激活蛋白（如 CBP 和 P300）的抑制剂，用于治疗或预防疾病，如增殖性疾病、炎症性疾病、自身免疫性疾病和纤维化疾病。
• Imidazopiperazine inhibitors of transcription activating proteins
  申请人：Board of Regents, The University of Texas System

  公开号：US11058688B2

  公开（公告）日：2021-07-13

  The present disclosure relates to heterocyclic compounds and methods which may be useful as inhibitors of transcription activating proteins such as CBP and P300 for the treatment or prevention of diseases such as proliferative diseases, inflammatory disorders, autoimmune diseases, and fibrotic diseases.

  本公开涉及杂环化合物和方法，它们可用作转录激活蛋白（如 CBP 和 P300）的抑制剂，用于治疗或预防疾病，如增殖性疾病、炎症性疾病、自身免疫性疾病和纤维化疾病。