(2R,3S,4R,5R,8R,10R,11R,12S,13S,14R)-2-ethyl-3,4,10-trihydroxy-13-[(2R,4R,5S,6S)-5-hydroxy-4-methoxy-4,6-dimethyloxan-2-yl]oxy-11-[(2S,3R,6R)-3-hydroxy-6-methyloxan-2-yl]oxy-3,5,6,8,10,12,14-heptamethyl-1-oxa-6-azacyclopentadecan-15-one | 688002-51-9

• 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: (2R,3S,4R,5R,8R,10R,11R,12S,13S,14R)-2-ethyl-3,4,10-trihydroxy-13-[(2R,4R,5S,6S)-5-hydroxy-4-methoxy-4,6-dimethyloxan-2-yl]oxy-11-[(2S,3R,6R)-3-hydroxy-6-methyloxan-2-yl]oxy-3,5,6,8,10,12,14-heptamethyl-1-oxa-6-azacyclopentadecan-15-one
• CAS: 688002-51-9
• 化学式: C₃₆H₆₇NO₁₂
• 分子量: 705.927
• InChiKey: CJGVZUQEIDFEQQ-FHFBNANVSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.3
• 重原子数：
  49
• 可旋转键数：
  6
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.97
• 拓扑面积：
  177
• 氢给体数：
  5
• 氢受体数：
  13

反应信息

• 作为产物：
  描述：

  、 聚合甲醛 在 甲酸 作用下， 以 氯仿 为溶剂， 反应 4.0h， 以77%的产率得到(2R,3S,4R,5R,8R,10R,11R,12S,13S,14R)-2-ethyl-3,4,10-trihydroxy-13-[(2R,4R,5S,6S)-5-hydroxy-4-methoxy-4,6-dimethyloxan-2-yl]oxy-11-[(2S,3R,6R)-3-hydroxy-6-methyloxan-2-yl]oxy-3,5,6,8,10,12,14-heptamethyl-1-oxa-6-azacyclopentadecan-15-one
  参考文献：
  名称：

  [EN] 9A-AZALIDES WITH ANTI-INFLAMMATORY ACTIVITY
  [FR] 9A-AZALIDES AYANT UNE ACTIVITE ANTI-INFLAMMATOIRE

  摘要：

  描述了具有抗炎活性的大环内酯类药物，尤其是在位置3没有克拉迪诺糖的9a-氮杂大环内酯类药物，它们的药用盐和包含它们作为活性成分的药物组合物。

  公开号：

  WO2004039821A1

文献信息

• [EN] IMMUNOMODULATING IMINE-OXAZOLINE AZALIDES<br/>[FR] AZALIDES IMMUNOMODULATEURS D'IMINE-OXAZOLINE
  申请人：ZOETIS SERVICES LLC

  公开号：WO2021183759A1

  公开（公告）日：2021-09-16

  Defined herein are immunemodulating Formula (1) compounds wherein R1, R2, R3, and W are as defined herein, stereoisomers thereof, and pharmaceutically acceptable salts thereof; and compositions comprising said compounds. The invention also includes methods for treating an inflammatory and/or immunological disease or disorder in an animal by administering a therapeutically effective amount of a Formula (1) compound, stereoisomer thereof, and a pharmaceutically acceptable salt thereof; or use of said compound of Formula (1 ) to prepare a medicament for treating an inflammatory and/or immunological disease or disorder in an animal.

  本发明定义了免疫调节式(1)化合物，其中R1、R2、R3和W如本文所定义，其立体异构体，以及药学上可接受的盐；以及包含这些化合物的组合物。本发明还包括通过给予动物治疗有效量的式(1)化合物、其立体异构体及药学上可接受的盐，来治疗炎症和/或免疫性疾病或障碍的方法；以及使用式(1)化合物制备用于治疗动物炎症和/或免疫性疾病或障碍的药物的用途。
• Azithromycin derivatives with epithelial barrier enhancement properties
  申请人：EpiEndo Pharmaceuticals ehf

  公开号：US10723752B2

  公开（公告）日：2020-07-28

  The invention provides novel compounds that are derivatives of Azithromycin and that have been found by the current inventors to have low antimicrobial activity but significant epithelial barrier enhancement properties. The invention further provides use of the compounds as a medicament, in particular in the treatment or prophylaxis of a disease or condition that is caused by a defect in epithelial cells or tissue, or a disease or condition that benefits from enhancement or restoration of epithelial barrier function, for example diseases of the respiratory tract.

  本发明提供了新型化合物，它们是阿奇霉素的衍生物，本发明人发现它们具有较低的抗菌活性，但具有显著的上皮屏障增强特性。本发明进一步提供了这些化合物作为药物的用途，特别是用于治疗或预防由上皮细胞或组织缺陷引起的疾病或病症，或受益于上皮屏障功能增强或恢复的疾病或病症，例如呼吸道疾病。
• [EN] IMMUNOMODULATING O-HET-ARYL AZALIDES<br/>[FR] AZALIDES IMMUNOMODULATEURS O-HET-ARYLE
  申请人：ZOETIS SERVICES LLC

  公开号：WO2021183762A1

  公开（公告）日：2021-09-16

  Defined herein are immunomodulating Formula (1) compounds stereoisomers thereof, and pharmaceutically acceptable salts thereof; wherein R0, R1, R2, R10, W, Ring C and n are as defined herein, stereoisomers thereof, and pharmaceutically acceptable salts thereof; and compositions comprising said compounds. The invention also includes methods for treating an inflammatory and/or immunological disease or disorder in an animal by administering a therapeutically effective amount of a Formula (1) compound, stereoisomer thereof, and a pharmaceutically acceptable salt thereof; or use of said compound of Formula (1) to prepare a medicament for treating an inflammatory and/or immunological disease or disorder in an animal.
• [EN] IMMUNOMODULATING TRIFLUOROMETHYL-AMINAL AZALIDES<br/>[FR] AZALIDES IMMUNOMODULATEURS DE TRIFLUOROMÉTHYL-AMINAL
  申请人：ZOETIS SERVICES LLC

  公开号：WO2021183754A1

  公开（公告）日：2021-09-16

  Defined herein are immunomodulating Formula (1) compounds, wherein R1, R2 and W are as defined herein, stereoisomers thereof, and pharmaceutically acceptable salts thereof; and compositions comprising said compounds. The invention also includes methods for treating an inflammatory and/or immunological disease or disorder in an animal by administering a therapeutically effective amount of a Formula (1) compound, stereoisomer thereof, and a pharmaceutically acceptable salt thereof; or use of said compound of Formula (1) to prepare a medicament for treating an inflammatory and/or immunological disease or disorder in an animal.
• [EN] IMMUNOMODULATING UREA AZALIDES<br/>[FR] AZALIDES D'URÉE IMMUNOMODULATEURS
  申请人：ZOETIS SERVICES LLC

  公开号：WO2021183758A1

  公开（公告）日：2021-09-16

  Defined herein are immunomodulating Formula (1) compounds wherein R, R0, R1, R2,R3 and W are as defined herein, stereoisomers thereof, and pharmaceutically acceptable salts thereof; and compositions comprising said compounds. The invention also includes methods for treating an inflammatory and/or immunological disease or disorder in an animal by administering a therapeutically effective amount of a Formula (1) compound, stereoisomer thereof, and a pharmaceutically acceptable salt thereof; or use of said compound of Formula (1) to prepare a medicament for treating an inflammatory and/or immunological disease or disorder in an animal.