(5Z)-7-[(1R,2R,3R,5S)-3,5-Dihydroxy-2-(3-oxodecyl)cyclopentyl]-5-heptenoic acid

• 分子结构分类: 有机化合物 - 脂质和类脂质分子 - 脂肪酰基
• 英文名称: (5Z)-7-[(1R,2R,3R,5S)-3,5-Dihydroxy-2-(3-oxodecyl)cyclopentyl]-5-heptenoic acid
• 英文别名: (E)-7-[(1R,2R,3R,5S)-3,5-dihydroxy-2-(3-oxodecyl)cyclopentyl]hept-5-enoic acid
• 化学式: C₂₂H₃₈O₅
• 分子量: 382.5
• InChiKey: TVHAZVBUYQMHBC-VLRWBWIZSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.7
• 重原子数：
  27
• 可旋转键数：
  15
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.82
• 拓扑面积：
  94.8
• 氢给体数：
  3
• 氢受体数：
  5

文献信息

• BIFUNCTIONAL RHO KINASE INHIBITOR COMPOUNDS, COMPOSITION AND USE
  申请人：INSPIRE PHARMACEUTICALS, INC.

  公开号：US20130131106A1

  公开（公告）日：2013-05-23

  This invention relates to synthetic bifunctional compounds comprising a first rho-associated kinase (ROCK) inhibiting compound and a second pharmaceutically active compound with complementary activity; the first and the second compounds are covalently linked by a biologically labile bond. This invention also relates to methods of making such compounds. The invention also relates to methods of using such bifunctional compounds in the prevention or treatment of diseases or conditions that are affected or can be assisted by altering the integrity or rearrangement of the cytoskeleton. Particularly, this invention relates to methods of treating ophthalmic diseases such as disorders in which intraocular pressure is elevated, for example primary open-angle glaucoma, using the bifunctional compounds.

  本发明涉及合成的双功能化合物，包括第一种抑制rho相关激酶(ROCK)的化合物和具有互补活性的第二种药物活性化合物；第一种和第二种化合物由生物可降解的化学键共价连接。本发明还涉及制备这种化合物的方法。本发明还涉及使用这种双功能化合物预防或治疗受到细胞骨架完整性或重组影响的疾病或病况的方法。特别地，本发明涉及使用这种双功能化合物治疗眼科疾病，例如原发性开角型青光眼等眼内压升高的疾病。
• HIGH PENETRATION COMPOSITIONS AND THEIR APPLICATIONS
  申请人：Yu, Chongxi

  公开号：EP2370406A1

  公开（公告）日：2011-10-05
• US7790905B2
  申请人：——

  公开号：US7790905B2

  公开（公告）日：2010-09-07
• [EN] HIGH PENETRATION COMPOSITIONS AND THEIR APPLICATIONS<br/>[FR] COMPOSITIONS À PÉNÉTRATION ÉLEVÉE ET LEURS APPLICATIONS
  申请人：YU CHONGXI

  公开号：WO2010065936A1

  公开（公告）日：2010-06-10

  High penetration compositions (HPC) of a parent compound, which are capable of crossing biological barriers with high penetration efficiency. The HPCs are capable of being converted to parent drugs or parent drug-related compounds such as metabolites after crossing one or more biological barriers and thus can render treatments for the conditions that the parent drugs or parent drug-related compounds can. Additionally, the HPCs are capable of reaching areas that their parent drugs or parent drug-related compounds may not be able to access or to render a sufficient concentration at the target areas HPCs of NSAIA, for example, have demonstrated indications such as treating hair loss. A HPC can be administered to a subject through various administration routes, e. g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.