N-[2-(diethylamino)ethyl]-2-[2-[2-(2,3-difluorophenyl)ethyl]-4-oxo-6,7-dihydro-5H-cyclopenta[d]pyrimidin-1-yl]-3-[4-[4-(trifluoromethyl)phenyl]phenyl]propanamide

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: N-[2-(diethylamino)ethyl]-2-[2-[2-(2,3-difluorophenyl)ethyl]-4-oxo-6,7-dihydro-5H-cyclopenta[d]pyrimidin-1-yl]-3-[4-[4-(trifluoromethyl)phenyl]phenyl]propanamide
• 化学式: C₃₇H₃₉F₅N₄O₂
• 分子量: 666.7
• InChiKey: TWVVMAOQVWVEDS-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  6.8
• 重原子数：
  48
• 可旋转键数：
  13
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  65
• 氢给体数：
  1
• 氢受体数：
  8

文献信息

• [EN] PLA2G7/LP-PLA2 AS BIOMARKER AND THERAPEUTIC TARGET IN THE PREVENTION AND TREATMENT OF CALCIFIC AORTIC VALVE DISEASE<br/>[FR] PLA2G7/LP-PLA2 EN TANT QUE BIOMARQUEUR ET CIBLE THÉRAPEUTIQUE DANS LA PRÉVENTION ET LE TRAITEMENT D'UNE MALADIE DE VALVE AORTIQUE CALCIFIÉE
  申请人：UNIV LAVAL

  公开号：WO2013185214A1

  公开（公告）日：2013-12-19

  The present invention relates to the treatment and/or prevention of calcific aortic vascular disease (CAVD) and valve calcification. Particularly, the invention provides a target for intervention in the treatment or prevention of CAVD through the administration of an of inhibitor PLA2G7 expression or Lp-PLA2 enzymatic activity. Also, the invention provides 5 means to treat hypertension related to decreased arterial compliance and vascular calcification. The invention also relates to the use of inhibitors of Lp-PLA2 to prevent structural valve degeneration (SVD) as the major cause of bioprosthetic valve failure leading to bioprostheses (BPs) stenosis or regurgitation.