1-(1,3-dihydroxyprop-2-yl)-4-(4-fluorophenyl)-5-(2-phenoxypyrimidin-4-yl)imidazole | 219790-72-4

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: 1-(1,3-dihydroxyprop-2-yl)-4-(4-fluorophenyl)-5-(2-phenoxypyrimidin-4-yl)imidazole
• 英文别名: 2-[4-(4-Fluorophenyl)-5-(2-phenoxypyrimidin-4-yl)imidazol-1-yl]propane-1,3-diol
• CAS: 219790-72-4
• 化学式: C₂₂H₁₉FN₄O₃
• 分子量: 406.416
• InChiKey: ZDKIAVFEUPUCMR-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.2
• 重原子数：
  30
• 可旋转键数：
  7
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.14
• 拓扑面积：
  93.3
• 氢给体数：
  2
• 氢受体数：
  7

文献信息

• Novel substituted imidazole compounds
  申请人：SmithKline Beecham Corporation

  公开号：US20030114452A1

  公开（公告）日：2003-06-19

  Novel 1,4,5-substituted imidazole compounds and compositions for use in therapy as CSBP/p38 kinase inhibitors.

  小说1,4,5-取代咪唑化合物及其组合物，用于治疗作为CSBP / p38激酶抑制剂。
• Novel Substituted Imidazole Compounds
  申请人：Adams Jerry L.

  公开号：US20080114010A1

  公开（公告）日：2008-05-15

  Novel 1,4,5-substituted imidazole compounds and compositions for use in therapy as CSBP/p38 kinase inhibitors.

  小说1,4,5-取代咪唑化合物和用于治疗的组合物，作为CSBP/p38激酶抑制剂。
• DRUG FOR TREATING CORNEAL ENDOTHELIUM BY PROMOTING CELL PROLIFERATION OR INHIBITING CELL DAMAGE
  申请人：The Doshisha

  公开号：EP3069732A1

  公开（公告）日：2016-09-21

  Provided is an agent for treating or preventing a corneal endothelial disorder wherein cell proliferation is required. More specifically, provided is an agent for treating or preventing a corneal endothelial disorder, wherein cell proliferation is required, said agent comprising a p38MAP kinase inhibitor. In a preferred embodiment, the corneal endothelial disorder is a wound. In a preferred embodiment, the p38MAP kinase inhibitor is soluble in water. The p38MAP kinase inhibitor may comprise 4-[4-(4-fluorophenyl)-2-(4-methylsulfinylphenyl)-1H-imidazo le-5-yl]pyridine (SB203580) or a salt thereof.

  本发明提供了一种用于治疗或预防角膜内皮失调的制剂，其中需要细胞增殖。更具体地说，提供了一种用于治疗或预防角膜内皮紊乱的制剂，其中需要细胞增殖，所述制剂包括 p38MAP 激酶抑制剂。在一个优选的实施方案中，角膜内皮失调是一种伤口。在一个优选的实施方案中，p38MAP 激酶抑制剂可溶于水。p38MAP 激酶抑制剂可包括 4-[4-(4-氟苯基)-2-(4-甲亚磺酰基苯基)-1H-咪唑-5-基]吡啶 (SB203580) 或其盐。
• DRUG FOR TREATING OR PREVENTING DISORDER CAUSED BY TGF- SIGNALS, AND APPLICATION THEREOF
  申请人：The Doshisha

  公开号：EP3381472A1

  公开（公告）日：2018-10-03

  Provided is a drug or method for treating or preventing a condition, disorder, or disease of the corneal endothelium caused by transforming growth factor-β (TGF-β) signals, mitochondrial abnormalities, and/or endoplasmic reticulum (ER) associated stress in corneal endothelial cells, using p38 MAP kinase inhibitors. The present invention provides a drug which includes p38 MAP kinase inhibitors, and which is for treating or preventing a condition, disorder, or disease of the corneal endothelium caused by TGF-β signals and/or mitochondrial abnormalities in corneal endothelial cells. In the preferred embodiment, the condition, disorder, or disease of the corneal endothelium is Fuchs' corneal endothelial dystrophy.

  本发明提供了一种利用p38 MAP激酶抑制剂治疗或预防角膜内皮细胞中由转化生长因子-β（TGF-β）信号、线粒体异常和/或内质网（ER）相关应激引起的角膜内皮细胞状况、失调或疾病的药物或方法。本发明提供了一种药物，其中包括 p38 MAP 激酶抑制剂，用于治疗或预防由角膜内皮细胞中的 TGF-β 信号和/或线粒体异常引起的角膜内皮的状况、紊乱或疾病。在优选的实施方案中，角膜内皮的状况、失调或疾病是福氏角膜内皮营养不良症。
• Drug for treating corneal endothelium by promoting cell proliferation or inhibiting cell damage
  申请人：THE DOSHISHA

  公开号：US10813920B2

  公开（公告）日：2020-10-27

  Provided is an agent for treating or preventing a corneal endothelial disorder wherein cell proliferation is required. More specifically, provided is an agent for treating or preventing a corneal endothelial disorder, wherein cell proliferation is required, said agent comprising a p38MAP kinase inhibitor. In a preferred embodiment, the corneal endothelial disorder is a wound. In a preferred embodiment, the p38MAP kinase inhibitor is soluble in water. The p38MAP kinase inhibitor may comprise 4-(4-fluorophenyl)-2-(4-methylsulfinylphenyl)-5-(4-pyridyl)-1H-imidazole (SB203580) or a salt thereof.

  本发明提供了一种用于治疗或预防角膜内皮失调的制剂，其中需要细胞增殖。更具体地说，提供了一种用于治疗或预防角膜内皮紊乱的制剂，其中需要细胞增殖，所述制剂包括 p38MAP 激酶抑制剂。在一个优选的实施方案中，角膜内皮失调是一种伤口。在一个优选的实施方案中，p38MAP 激酶抑制剂可溶于水。p38MAP激酶抑制剂可包括4-(4-氟苯基)-2-(4-甲磺酰基苯基)-5-(4-吡啶基)-1H-咪唑(SB203580)或其盐。