4,4,6a,8a,11,11,14b-heptamethyl-2,3,4a,5,6,6b,7,8,9,10,12,12a,14,14a-tetradecahydro-1H-picen-3-ol

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: 4,4,6a,8a,11,11,14b-heptamethyl-2,3,4a,5,6,6b,7,8,9,10,12,12a,14,14a-tetradecahydro-1H-picen-3-ol
• 化学式: C₂₉H₄₈O
• 分子量: 412.7
• InChiKey: GLENULFUVDQXBU-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  8.6
• 重原子数：
  30
• 可旋转键数：
  0
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.93
• 拓扑面积：
  20.2
• 氢给体数：
  1
• 氢受体数：
  1

文献信息

• [EN] HYDROXAMATE TRITERPENOID DERIVATIVES<br/>[FR] DÉRIVÉS D'HYDROXAMATE TRITERPÉNOÏDE
  申请人：VIVACELL BIOTECHNOLOGY ESPANA S L

  公开号：WO2018069086A1

  公开（公告）日：2018-04-19

  Triterpenoid derivatives and compositions comprising said triterpenoids derivatives of Formula (I) are described, wherein R=-C(O)NHOH. Said triterpenoids and compositions show capacity to bind PHD2, stabilize HIF-1α and HIF-2α proteins, activate the HIF pathway in different cell types, induce angiogenesis in human endothelial vascular cell, show neuroprotective activity in vitro and in vivo, antidiabetic activity and reduce the levels of lipids in vivo, and increase the plasma levels of Erythropoietin in vivo. The triterpenoid derivatives described act also in a selective manner and do not induce Nrf2 activation, NF-κB inhibition, STAT3 inhibition, and TGR5 activation, which are known activities of the natural triterpenoid precursors. Said triterpenoid derivatives are useful in the treatment of conditions and diseases which are responsive to HIF activation such as stroke, cerebral palsy, traumatic injuries and neurodegenerative diseases; and also IBD, myocardial ischaemia–reperfusion injury, acute lung injury, diabetic and chronic wounds, organ transplantation, acute kidney injury or arterial diseases.

  本文描述了式（I）的三萜衍生物和包含该三萜衍生物的组合物，其中R=-C（O）NHOH。所述三萜衍生物和组合物表现出与PHD2结合的能力，稳定HIF-1α和HIF-2α蛋白，激活不同细胞类型中的HIF通路，诱导人类内皮细胞血管生成，显示体外和体内的神经保护作用，抗糖尿病活性并减少体内脂质水平，增加体内促红细胞生成素的血浆水平。所述三萜衍生物还具有选择性作用，不会诱导Nrf2激活、NF-κB抑制、STAT3抑制和TGR5激活，这是天然三萜衍生物前体的已知活性。所述三萜衍生物在治疗对HIF激活有反应的疾病和病症方面具有用途，例如中风、脑瘫、创伤性损伤和神经退行性疾病；以及炎症性肠病、心肌缺血再灌注损伤、急性肺损伤、糖尿病和慢性创口、器官移植、急性肾损伤或动脉疾病。
• US7517540B2
  申请人：——

  公开号：US7517540B2

  公开（公告）日：2009-04-14
• US8034389B2
  申请人：——

  公开号：US8034389B2

  公开（公告）日：2011-10-11