4-[4-(4-氟苯基)-1-[1-(3-异唑基甲基)-4-哌啶基]-1H-咪唑-5-基]-2-嘧啶胺 | 1293395-67-1

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 中文名称: 4-[4-(4-氟苯基)-1-[1-(3-异唑基甲基)-4-哌啶基]-1H-咪唑-5-基]-2-嘧啶胺
• 英文名称: 4-{4-(4-Fluorophenyl)-1-[1-(1,2-Oxazol-3-Ylmethyl)piperidin-4-Yl]-1h-Imidazol-5-Yl}pyrimidin-2-Amine
• 英文别名: 4-[5-(4-fluorophenyl)-3-[1-(1,2-oxazol-3-ylmethyl)piperidin-4-yl]imidazol-4-yl]pyrimidin-2-amine
• CAS: 1293395-67-1
• 化学式: C₂₂H₂₂FN₇O
• 分子量: 419.5
• InChiKey: XPWHRQHBPRSUAW-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.9
• 重原子数：
  31
• 可旋转键数：
  5
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.27
• 拓扑面积：
  98.9
• 氢给体数：
  1
• 氢受体数：
  8

文献信息

• Novel Compounds As Casein Kinase Inhibitors
  申请人：Subramanyam Chakrapani

  公开号：US20110098272A1

  公开（公告）日：2011-04-28

  Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

  所述化合物及其药用可接受盐已被披露，其中所述化合物具有规范中定义的Formula I结构。相应的药物组合物、治疗方法、合成方法和中间体也已被披露。
• COMPOUNDS FOR TREATMENT OF DISEASES RELATED TO DUX4 EXPRESSION
  申请人：Facio Intellectual Property B.V.

  公开号：EP3498278A1

  公开（公告）日：2019-06-19

  The present invention relates to compounds for the treatment of diseases related to DUX4 expression, such as muscular dystrophies, in this case facioscapulohumeral muscular dystrophy (FSHD). It also relates to use of such compounds, or to methods of use of such compounds.

  本发明涉及用于治疗与 DUX4 表达有关的疾病的化合物，例如肌肉萎缩症，在本例中为面肩肱肌萎缩症（FSHD）。本发明还涉及此类化合物的用途或使用方法。
• Treatment of respiratory diseases
  申请人：The University of Melbourne

  公开号：US10722513B2

  公开（公告）日：2020-07-28

  The present invention relates to compositions, methods and kits for the treatment of respiratory disease. In particular, the compositions, methods and kits are particularly useful, but not limited to, the treatment or prevention of exacerbations of asthma and chronic obstructive pulmonary disease. The present invention provides a method of treating or preventing a respiratory disease in a subject in need thereof, the method comprising administering to the subject a therapeutically effective amount of an inhibitor of casein kinase 1, thereby treating or preventing a respiratory disease in a subject. The present invention also provides a method of treating or preventing a respiratory disease in a subject in need thereof, the method comprising administering to the subject a therapeutically effective amount of an inhibitor of ALK5, thereby treating or preventing a respiratory disease in a subject, wherein the inhibitor is administered directly to the airway and/or lungs. The present invention also provides a method of treating or preventing a condition of the airway or lung involving fibrosis in a subject in need thereof, the method comprising administering to the subject a therapeutically effective amount of an inhibitor of casein kinase 1 or an inhibitor of ALK5, thereby treating or preventing a condition of the airway or lung involving fibrosis in a subject.

  本发明涉及治疗呼吸系统疾病的组合物、方法和试剂盒。特别是，本发明的组合物、方法和试剂盒特别有用，但不限于治疗或预防哮喘和慢性阻塞性肺病的恶化。本发明提供了一种治疗或预防有需要的受试者呼吸系统疾病的方法，该方法包括向受试者施用治疗有效量的酪蛋白激酶1抑制剂，从而治疗或预防受试者的呼吸系统疾病。本发明还提供了一种治疗或预防有需要的受试者的呼吸系统疾病的方法，该方法包括向受试者施用治疗有效量的ALK5抑制剂，从而治疗或预防受试者的呼吸系统疾病，其中抑制剂直接施用至气道和/或肺部。本发明还提供了一种治疗或预防有需要的受试者气道或肺部涉及纤维化的病症的方法，该方法包括向受试者施用治疗有效量的酪蛋白激酶1抑制剂或ALK5抑制剂，从而治疗或预防受试者气道或肺部涉及纤维化的病症。
• Compounds for treatment of diseases related to DUX4 expression
  申请人：Facio Intellectual Property B.V.

  公开号：US10973820B2

  公开（公告）日：2021-04-13

  The present invention relates to compounds for the treatment of diseases related to DUX4 expression, such as muscular dystrophies, wherein the disease is facioscapulohumeral muscular dystrophy (FSHD). It also relates to use of such compounds, or to methods of use of such compounds.

  本发明涉及用于治疗与DUX4表达有关的疾病的化合物，如肌肉萎缩症，其中该疾病为面肩肱肌营养不良症（FSHD）。本发明还涉及此类化合物的用途或使用方法。
• IMIDAZOLE DERIVATIVES AS CASEIN KINASE INHIBITORS
  申请人：Pfizer Inc.

  公开号：EP2493876B1

  公开（公告）日：2014-02-12