4-(3-Cyclopentyloxy-4-methoxyphenyl)-3-[(3-methoxy-4-phenylmethoxyphenyl)methyl]pyrrolidin-2-one

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡咯烷类
• 英文名称: 4-(3-Cyclopentyloxy-4-methoxyphenyl)-3-[(3-methoxy-4-phenylmethoxyphenyl)methyl]pyrrolidin-2-one
• 化学式: C₃₁H₃₅NO₅
• 分子量: 501.6
• InChiKey: BRIOCPYVAJSNNR-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.6
• 重原子数：
  37
• 可旋转键数：
  10
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.39
• 拓扑面积：
  66
• 氢给体数：
  1
• 氢受体数：
  5

文献信息

• BENZYLATED PDE4 INHIBITORS
  申请人：Lauener W. Ronald

  公开号：US20070208181A1

  公开（公告）日：2007-09-06

  The present invention is directed to a method for reducing the emetogenic effects of PDE inhibitors, and more particularly is directed to compounds having PDE4 inhibition activity with little or no emetogenic side-effects, and chemical methods including benzylation for preparing such compounds. A benzyl group may be attached to either a carbon or nitrogen atom of a PDE4 inhibitor. Suitable benzylation chemistry is to extract a hydrogen from a PDE4 inhibitor, preferably with a base, and then react the resulting nucleophilic PDE4 inhibitor with a benzylating agent, e.g., benzyl bromide or a derivative thereof.
• US7459479B2
  申请人：——

  公开号：US7459479B2

  公开（公告）日：2008-12-02
• [EN] COMBINATION OF PDE-V INHIBITORS AND NK1 ANTAGONISTS FOR THE TREATMENT OF DEPRESSION<br/>[FR] COMBINAISONS D'INHIBITEURS DE PDE-V ET D'ANTAGONISTES DE NK1 DANS LE TRAITEMENT DE LA DEPRESSION
  申请人：PFIZER PROD INC

  公开号：WO2003105815A1

  公开（公告）日：2003-12-24

  The present invention relates to a method of treating depression or anxiety in a mammal, including a human, by administering to the mammal a CNS-penetrant NK-1 receptor antagonist (e.g., a substance P receptor antagonist) in combination with a PDE IV inhibitor. It also relates to pharmaceutical compositions containing a pharmaceutically acceptable carrier, a CNS-penetrant NK-1 receptor antagonist and a PDE IV inhibitor.
• [EN] TREATMENT FOR DEPRESSION AND ANXIETY BY THE COMBINATION OF A PDE IV INHIBITOR AND AN ANTIDEPRESSANT OR AN ANXIOLYTIC AGENT<br/>[FR] TRAITEMENT DE LA DEPRESSION ET DE L'ANXIETE PAR LA COMBINAISON D'UN INHIBITEUR DE PDE IV ET D'UN ANTIDEPRESSEUR OU AGENT ANXIOLYTIQUE
  申请人：PFIZER PROD INC

  公开号：WO2003105902A1

  公开（公告）日：2003-12-24

  The present invention relates to a method of treating depression or anxiety in a mammal, including a human, by administering to the mammal a PDE IV inhibitor in combination with an antidepressant or an anxiolytic agent. It also relates to pharmaceutical compositions containing a pharmaceutically acceptable carrier, a PDE IV inhibitor and an anxiolytic agent or antidepressant.