18-(3,9-Dihydroxy-4,8-dimethyl-5-oxododeca-6,10-dien-2-yl)-9-ethyl-8,10-dihydroxy-3,17-dimethoxy-5,7,11,13-tetramethyl-1-oxacyclooctadeca-3,5,13,15-tetraen-2-one

• 分子结构分类: 有机化合物 - 苯丙烷和聚酮 - 大环内酯类和类似物
• 英文名称: 18-(3,9-Dihydroxy-4,8-dimethyl-5-oxododeca-6,10-dien-2-yl)-9-ethyl-8,10-dihydroxy-3,17-dimethoxy-5,7,11,13-tetramethyl-1-oxacyclooctadeca-3,5,13,15-tetraen-2-one
• 化学式: C₃₉H₆₂O₉
• 分子量: 674.9
• InChiKey: GHUWJSVUOSYYER-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.9
• 重原子数：
  48
• 可旋转键数：
  11
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.64
• 拓扑面积：
  143
• 氢给体数：
  4
• 氢受体数：
  9

文献信息

• [EN] MACROCYCLIC LACTONE DERIVATIVES AND USES THEREOF<br/>[FR] DÉRIVÉS DE LACTONE MACROCYCLIQUE ET LEURS UTILISATIONS
  申请人：PIRAMAL ENTPR LTD

  公开号：WO2014118740A1

  公开（公告）日：2014-08-07

  The present invention provides compounds represented by Formula 1: wherein, R' is as defined in the specification, in all their stereoisomeric and tautomeric forms and mixtures thereof in all ratios, and their pharmaceutically acceptable salts, pharmaceutically acceptable solvates, pharmaceutically acceptable polymorphs and prodrugs. The invention also relates to processes for the preparation of the compounds of Formula and pharmaceutical compositions containing them. The compounds and the pharmaceutical compositions of the present invention are useful for the treatment of inflammatory disorders and/or viral infections. The compounds and the pharmaceutical compositions of the present invention are also useful for the treatment of cancer.

  本发明提供了由式1表示的化合物：其中，R'如规范中所定义，在其所有立体异构体和互变异构体形式以及它们在所有比例上的混合物中，以及它们的药学上可接受的盐、药学上可接受的溶剂合物、药学上可接受的多晶形和前药。本发明还涉及制备上述式化合物的方法以及含有它们的药物组合物。本发明的化合物和药物组合物可用于治疗炎症性疾病和/或病毒感染。本发明的化合物和药物组合物也可用于治疗癌症。
• MACROCYCLIC LACTONE DERIVATIVES FOR THE TREATMENT OF CANCER
  申请人：Mishra Prabhu Dutt

  公开号：US20120245183A1

  公开（公告）日：2012-09-27

  The present invention provides compounds represented by formula (1): wherein, R 1 , R 2 , R 3 and R 4 are as defined in the specification, in all their stereoisomeric and tautomeric forms and mixtures thereof in all ratios, and their pharmaceutically acceptable salts, pharmaceutically acceptable solvates, pharmaceutically acceptable polymorphs and prodrugs. The invention also relates to processes for the manufacture of compounds of formula (1) and pharmaceutical compositions containing them. The compounds and the pharmaceutical compositions of the present invention are useful for the treatment of cancer. The present invention further provides a method of treatment of cancer by administering a therapeutically effective amount of the said compound of formula (1) or its pharmaceutical composition, to a mammal in need thereof.

  本发明提供了由式（1）表示的化合物：其中，R1、R2、R3和R4如规范中所定义，在它们的立体异构体、互变异构体形式和所有比例的混合物中，以及它们的药学上可接受的盐、药学上可接受的溶剂化物、药学上可接受的多晶形和前药。本发明还涉及制备式（1）化合物和含有它们的制药组合物的过程。本发明的化合物和制药组合物对癌症的治疗有用。本发明还提供了一种通过向需要治疗的哺乳动物中给予所述式（1）化合物或其制药组合物的治疗有效量来治疗癌症的方法。
• USE OF MACROCYCLIC LACTONE DERIVATIVES FOR THE TREATMENT OF INFLAMMATORY DISORDERS
  申请人：Kulkarni-Almeida Asha

  公开号：US20120225889A1

  公开（公告）日：2012-09-06

  The present invention provides use of the compounds represented by formula (1): wherein, R 1 , R 2 , R 3 and R 4 are as defined in the specification, in all their stereo isomeric and tautomeric forms and mixtures thereof in all ratios, and their pharmaceutically acceptable salts, pharmaceutically acceptable solvates, pharmaceutically acceptable polymorphs and prodrugs and pharmaceutical compositions containing them for treatment of inflammatory disorders mediated by one or more cytokines selected from Tumor Necrosis Factor-alpha (TNF-α), interferon-γ (IFN-γ) and interleukins such as IL-1β, IL-2, IL-6, and IL-8. The present invention also relates to a pharmaceutical composition adapted for use in the treatment of inflammatory disorders. The present invention further provides a method of treatment of inflammatory disorders by administering a therapeutically effective amount of the said compound of formula (1) or its pharmaceutical composition, to a mammal in need thereof.

  本发明提供了使用由公式（1）表示的化合物的用途：其中，R1，R2，R3和R4如规范中所定义，在它们的所有立体异构体和互变异构体形式以及它们的所有比例的混合物中，以及它们的药学上可接受的盐，药学上可接受的溶剂合物，药学上可接受的多形体和前药以及含有它们的制剂，用于治疗由肿瘤坏死因子-α（TNF-α），干扰素-γ（IFN-γ）和白细胞介素如IL-1β，IL-2，IL-6和IL-8等选择性介导的炎症性疾病。本发明还涉及适用于治疗炎症性疾病的制药组合物。本发明还提供了一种治疗炎症性疾病的方法，通过向需要治疗的哺乳动物中给予公式（1）所述化合物或其制药组合物的治疗有效量。
• US8637683B2
  申请人：——

  公开号：US8637683B2

  公开（公告）日：2014-01-28