3-(3H-benzimidazol-5-yl)-5-[3-(trifluoromethyl)-4-(1,1,1-trifluoropropan-2-yloxy)phenyl]-1,2,4-oxadiazole;hydrochloride | 952509-01-2

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: 3-(3H-benzimidazol-5-yl)-5-[3-(trifluoromethyl)-4-(1,1,1-trifluoropropan-2-yloxy)phenyl]-1,2,4-oxadiazole;hydrochloride
• CAS: 952509-01-2
• 化学式: C₁₉H₁₂F₆N₄O₂*ClH
• 分子量: 478.781
• InChiKey: KRUYZACYZSOZCV-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  6.05
• 重原子数：
  32
• 可旋转键数：
  4
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.21
• 拓扑面积：
  76.8
• 氢给体数：
  2
• 氢受体数：
  11

文献信息

• MEDICINE FOR PREVENTING OR TREATING OPHTHALMIC DISEASE ASSOCIATED WITH ENHANCED INTRAOCULAR NEOVASCULARIZATION AND/OR INTRAOCULAR VASCULAR PERMEABILITY
  申请人：Kyoto University

  公开号：EP3747471A1

  公开（公告）日：2020-12-09

  Provided is a pharmaceutical for preventing or treating an ophthalmic disease associated with intraocular neovascularization and/or increased intraocular vascular permeability. The inventors of the present invention have made investigations on a pharmaceutical for preventing or treating an ophthalmic disease associated with intraocular neovascularization and/or increased intraocular vascular permeability, and have confirmed that a selective S1P receptor agonist having agonist activity at an S1P1 receptor has an intraocular neovascularization-reducing action and an intraocular vascular permeability-reducing action, thus completing the present invention. A compound or a pharmaceutically acceptable salt thereof of the present invention, which serves as the selective S1P receptor agonist having agonist activity at the S1P1 receptor, has an intraocular neovascularization-reducing action and an intraocular vascular permeability-reducing action, and can be used as a preventive and/or therapeutic agent for, for example, exudative age-related macular degeneration, diabetic retinopathy, diabetic macular edema, myopic choroidal neovascularization, retinal artery occlusion, retinal vein occlusion, or neovascular glaucoma.

  本发明提供了一种用于预防或治疗与眼内新生血管和/或眼内血管通透性增加有关的眼科疾病的药物。本发明的发明者对一种用于预防或治疗与眼内新生血管化和/或眼内血管通透性增加相关的眼科疾病的药物进行了研究，并证实了一种对 S1P1 受体具有激动活性的选择性 S1P 受体激动剂具有降低眼内新生血管化作用和降低眼内血管通透性作用，从而完成了本发明。本发明的化合物或其药学上可接受的盐作为选择性 S1P 受体激动剂，在 S1P1 受体上具有激动活性，具有降低眼内新生血管作用和降低眼内血管通透性作用、本发明可用作渗出性老年性黄斑变性、糖尿病视网膜病变、糖尿病黄斑水肿、近视性脉络膜新生血管、视网膜动脉闭塞、视网膜静脉闭塞或新生血管性青光眼等疾病的预防和/或治疗药物。