propan-2-yl (Z)-7-[(1R,2R,3R,5S)-3,5-dihydroxy-2-(3-hydroxy-5-phenylpentyl)cyclopentyl]hept-5-enoate

• 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: propan-2-yl (Z)-7-[(1R,2R,3R,5S)-3,5-dihydroxy-2-(3-hydroxy-5-phenylpentyl)cyclopentyl]hept-5-enoate
• 化学式: C₂₆H₄₀O₅
• 分子量: 432.6
• InChiKey: GGXICVAJURFBLW-ISHZQQPLSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.3
• 重原子数：
  31
• 可旋转键数：
  14
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.65
• 拓扑面积：
  87
• 氢给体数：
  3
• 氢受体数：
  5

文献信息

• [EN] A NOVEL PROCESS FOR THE PREPARATION OF PROSTAGLANDINS AND INTERMEDIATES THEREOF<br/>[FR] NOUVEAU PROCÉDÉ DE PRÉPARATION DE PROSTAGLANDINES ET DE LEURS INTERMÉDIAIRES
  申请人：BIOCON LTD

  公开号：WO2011055377A1

  公开（公告）日：2011-05-12

  This invention relates to novel process for the preparation of prostaglandin compounds having formula (K), wherein R is selected from the group consisting of C1-C7 alkyl; C7-C17 aralkyl wherein the aryl group is unsubstituted or substituted with one to three substituents selected from the group consisting of C1-C6 alkyl, halo and CF3; and (CH2)nOR2 wherein n is from 1 to 3 and R2 represents a C6-C10 aryl group which is unsubstituted or substituted with one to three substituents selected from the group consisting of C1-C6 alkyl, halo and CF3; and R1 is selected from OR3 and NHR3 wherein R3 is C1-C6 alkyl, H; and dashed lines represents a double bond or a single bond, is disclosed. Novel intermediates are also disclosed.

  本发明涉及一种制备公式（K）的前列腺素化合物的新工艺，其中R选自以下组中的一组：C1-C7烷基；C7-C17芳基烷基，其中芳基基团未取代或取代有1-3个取自C1-C6烷基，卤素和CF3的取代基；以及（CH2）nOR2，其中n为1-3，R2代表未取代或取代有1-3个取自C1-C6烷基，卤素和 的取代基的C6-C10芳基基团；R1选自OR3和NHR3，其中R3为C1-C6烷基，H；虚线表示双键或单键。本发明还揭示了新的中间体。
• NOVEL PROCESS FOR THE PREPARATION OF PROSTAGLANDINS AND INTERMEDIATES THEREOF
  申请人：Aswathanarayanappa Chandrashekar

  公开号：US20120209011A1

  公开（公告）日：2012-08-16

  This invention relates to novel process for the preparation of prostaglandin compounds having formula (K), wherein R is selected from the group consisting of C 1 -C 7 alkyl; C 7 -C 17 aralkyl wherein the aryl group is unsubstituted or substituted with one to three substituents selected from the group consisting of C 1 -C 6 alkyl, halo and CF 3 ; and (CH 2 ) n OR 2 wherein n is from 1 to 3 and R 2 represents a C 6 -C 10 aryl group which is unsubstituted or substituted with one to three substituents selected from the group consisting of C 1 -C 6 alkyl, halo and CF 3 ; and R 1 is selected from OR 3 and NHR 3 wherein R 3 is C 1 -C 6 alkyl, H; and dashed lines represents a double bond or a single bond, is disclosed. Novel intermediates are also disclosed.

  本发明涉及一种新型的制备具有式（K）的前列腺素化合物的方法，其中R选自以下组中的一种：C1-C7烷基；C7-C17芳基烷基，其中芳基基团未取代或取代有1至3个取代基，所述取代基选自C1-C6烷基，卤素和CF3；以及（CH2）nOR2，其中n为1至3，R2代表未取代或取代有1至3个取代基的C6-C10芳基基团，所述取代基选自C1-C6烷基，卤素和 ；R1选自OR3和NHR3，其中R3为C1-C6烷基，H；虚线表示双键或单键。本发明还公开了新型中间体。
• Pharmaceutical composition for treatment of increased intraocular pressure
  申请人：NOVALIQ GMBH

  公开号：US10555953B2

  公开（公告）日：2020-02-11

  The invention provides novel pharmaceutical compositions based on semifluorinated alkanes which are useful as carriers for a broad range of active ingredients. Preferred active ingredients include poorly water-soluble prostaglandin analogues. The invention further provides kits comprising such compositions.

  本发明提供了基于半氟化烷烃的新型药物组合物，可用作多种活性成分的载体。优选的活性成分包括水溶性差的前列腺素类似物。本发明进一步提供了包含此类组合物的试剂盒。
• Poly(ketals) and related compositions and methods
  申请人：Children's Medical Center Corporation

  公开号：US11071714B2

  公开（公告）日：2021-07-27

  Compositions comprising polymers comprising one or more ketal, monothioketal, and/or thioketal bonds are provided, as well as related methods and kits. In some embodiments, a polymer may comprise one or more repeat units comprising one or more ketal, monothioketal, and/or thioketal bonds and a precursor of a pharmaceutically active agent. The precursor of the pharmaceutically active agent may be located in the backbone or may be a pendant group. The polymer may degrade in certain environments (e.g., aqueous environments, acidic environments, in vivo, etc.) to produce the pharmaceutically active agent and other biocompatible degradation products, such as certain ketones, alcohols, and/or thiols. Regardless of the location of the precursor of the pharmaceutically active agent in the repeat unit(s), the polymer may have a prolonged degradation time and/or release of the pharmaceutically active agent in certain environments. Various compositions, described herein, may be particularly well suited for applications requiring extended release of pharmaceutically active agents, such as the treatment of ophthalmic disorders.

  本发明提供了由包含一个或多个酮键、单硫酮键和/或硫酮键的聚合物组成的组合物以及相关方法和试剂盒。在某些实施方案中，聚合物可包含一个或多个由一个或多个酮键、单硫酮键和/或硫酮键组成的重复单元和一种药用活性剂的前体。药用活性剂的前体可以位于骨架中，也可以是一个悬挂基团。聚合物可在特定环境（如水环境、酸性环境、体内等）中降解，产生药用活性剂和其他生物相容性降解产物，如某些酮、醇和/或硫醇。无论药用活性剂前体在重复单元中的位置如何，聚合物在某些环境中都可能会延长降解时间和/或释放药用活性剂。本文所述的各种组合物可能特别适用于需要延长药用活性剂释放时间的应用，如眼科疾病的治疗。
• OPHTHTALMIC COMPOSITIONS COMPRISING PROSTAGLANDIN F2 ALPHA DERIVATIVES AND HYALURONIC ACID
  申请人：Unither Pharmaceuticals

  公开号：EP2763654B1

  公开（公告）日：2020-04-29