N-{(R)-4-[1-(3-Cyclopentyloxy-4-methoxyphenyl)-2-(4-pyridyl)ethyl]phenylacetyl}trifluoromethanesulfonamide | 192766-97-5

• 分子结构分类: 有机化合物 - 苯丙烷和聚酮 - 二芳基庚烷
• 英文名称: N-{(R)-4-[1-(3-Cyclopentyloxy-4-methoxyphenyl)-2-(4-pyridyl)ethyl]phenylacetyl}trifluoromethanesulfonamide
• 英文别名: N-{(R)-4-[1-(3-Cyclopentyloxy-4-methoxyphenyl)-2-(pyridin-4-yl)ethyl]phenylacetyl}trifluoromethanesulfonamide；2-[4-[(1R)-1-(3-cyclopentyloxy-4-methoxyphenyl)-2-pyridin-4-ylethyl]phenyl]-N-(trifluoromethylsulfonyl)acetamide
• CAS: 192766-97-5
• 化学式: C₂₈H₂₉F₃N₂O₅S
• 分子量: 562.61
• InChiKey: XIYFYVVGWRXISN-XMMPIXPASA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.7
• 重原子数：
  39
• 可旋转键数：
  10
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.36
• 拓扑面积：
  103
• 氢给体数：
  1
• 氢受体数：
  9

文献信息

• [EN] TRI-ARYL ETHANE DERIVATIVES AS PDE IV INHIBITORS<br/>[FR] DERIVES D'ETHANE TRI-ARYLE UTILISES COMME INHIBITEURS DE PDE IV
  申请人：MERCK FROSST CANADA INC.

  公开号：WO1997022586A1

  公开（公告）日：1997-06-26

  (EN) The invention encompasses the novel compound of formula (I), useful in the treatment of diseases, including asthma, by raising the level of cyclic adenosine-3',5'-monophosphate (cAMP) through the inhibition of phosphodiesterase IV (PDE IV). The invention also encompasses certain pharmaceutical compositions and methods for treatment of diseases by inhibition of PDE IV, resulting in an elevation of cAMP, comprising the use of compounds of Formula (I).(FR) Nouveau composé de formule (I) utilisé pour traiter des maladies, y compris l'asthme, par augmentation du niveau d'adénosine-3',5'-monophosphate cyclique (cAMP), cette augmentation étant obtenue par l'inhibition de la phosphodiestérase IV (PDE IV). L'invention se rapporte également à certaines compositions pharmaceutiques et à des méthodes de traitement des maladies par inhibition de la PDE IV, entraînant une augmentation de cAMP, ces méthodes consistant à utiliser des composés de la formule (I).

  该发明涵盖了化合物(I)的新颖结构，通过抑制磷酸二酯酶IV（PDE IV）提高环磷酸腺苷-3'，5'-单磷酸（cAMP）水平，用于治疗包括哮喘在内的疾病。该发明还涵盖了某些药物组合物和通过抑制PDE IV治疗疾病的方法，导致cAMP升高，包括使用化合物(I)的方法。
• TRI-ARYL ETHANE DERIVATIVES AS PDE IV INHIBITORS
  申请人：MERCK FROSST CANADA INC.

  公开号：EP0873311A1

  公开（公告）日：1998-10-28
• BETA-CELL REPLICATION PROMOTING COMPOUNDS AND METHODS OF THEIR USE
  申请人：President and Fellows of Harvard College

  公开号：EP2804603A1

  公开（公告）日：2014-11-26
• [EN] BETA-CELL REPLICATION PROMOTING COMPOUNDS AND METHODS OF THEIR USE<br/>[FR] COMPOSÉS PROMOTEURS DE RÉPLICATION DES CELLULES BÊTA ET LEURS PROCÉDÉS D'UTILISATION
  申请人：HARVARD COLLEGE

  公开号：WO2013106547A1

  公开（公告）日：2013-07-18

  Disclosed are methods for stimulating or increasing β-cell replication or growthdisclosed or increasing insulin secretion, and methods of treating disorders such as diabetes, as well as related compositions and formulations.