8-ethyl-7,7-difluoro-5,6-didehydro-9,10-dihydro-8H-benzo[8]annulene

• 分子结构分类: 有机化合物 - 苯类化合物
• 英文名称: 8-ethyl-7,7-difluoro-5,6-didehydro-9,10-dihydro-8H-benzo[8]annulene
• 化学式: C₁₄H₁₄F₂
• 分子量: 220.26
• InChiKey: GJYAYOUVAQZGQR-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.3
• 重原子数：
  16
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.43
• 拓扑面积：
  0
• 氢给体数：
  0
• 氢受体数：
  2

文献信息

• TARGETED IDURONATE-2-SULFATASE COMPOUNDS
  申请人：ANGIOCHEM INC.

  公开号：US20150290341A1

  公开（公告）日：2015-10-15

  The present invention is related to a compound that includes a lysosomal enzyme and a targeting moiety, for example, a compound that includes iduronate-2-sulfatase conjugated to Angiopep-2 through a linker formed by specific click chemistry reactions. In certain embodiments, these compounds, owing to the presence of the targeting moiety, can cross the blood-brain barrier or accumulate in the lysosome more effectively than the enzyme alone. The invention also features pharmaceutical compositions containing such compounds and methods for treating lysosomal storage disorders (e.g., mucopolysaccharidosis Type II) using such compounds.

  本发明涉及一种化合物，包括溶酶体酶和靶向基团，例如，包括通过特定点击化学反应形成的连接物将硫酸二糖醛酸酶与Angiopep-2结合在一起的化合物。在某些实施例中，由于存在靶向基团，这些化合物可以比单独的酶更有效地穿过血脑屏障或在溶酶体中积累。该发明还涉及含有这种化合物的药物组合物以及使用这种化合物治疗溶酶体贮积疾病（例如，粘多糖贮积症II型）的方法。
• [EN] TARGETED IDURONATE-2-SULFATASE COMPOUNDS<br/>[FR] COMPOSÉS D'IDURONATE-2-SULFATASE CIBLÉS
  申请人：ANGIOCHEM INC

  公开号：WO2014082184A1

  公开（公告）日：2014-06-05

  The present invention is related to a compound that includes a lysosomal enzyme and a targeting moiety, for example, a compound that includes iduronate-2-sulfatase conjugated to Angiopep-2 through a linker formed by specific click chemistry reactions. In certain embodiments, these compounds, owing to the presence of the targeting moiety, can cross the blood-brain barrier or accumulate in the lysosome more effectively than the enzyme alone. The invention also features pharmaceutical compositions containing such compounds and methods for treating lysosomal storage disorders (e.g., mucopolysaccharidosis Type II) using such compounds.