trans-1-(3-cyclopentyloxy-6-fluoro-4-methoxyphenyl)-2-(2,6-difluorophenyl)ethene | 1349078-30-3

• 分子结构分类: 有机化合物 - 苯丙烷和聚酮 - 二苯乙烯类
• 英文名称: trans-1-(3-cyclopentyloxy-6-fluoro-4-methoxyphenyl)-2-(2,6-difluorophenyl)ethene
• 英文别名: 1-cyclopentyloxy-5-[(E)-2-(2,6-difluorophenyl)ethenyl]-4-fluoro-2-methoxybenzene
• CAS: 1349078-30-3
• 化学式: C₂₀H₁₉F₃O₂
• 分子量: 348.365
• InChiKey: NPDJVBYHXWFFAO-MDZDMXLPSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.7
• 重原子数：
  25
• 可旋转键数：
  5
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.3
• 拓扑面积：
  18.5
• 氢给体数：
  0
• 氢受体数：
  5

反应信息

• 作为产物：
  描述：

  (2,6-difluorobenzyl)triphenylphosphonium bromide 、 3-cyclopentyloxy-6-fluoro-4-methoxybenzaldehyde 生成 trans-1-(3-cyclopentyloxy-6-fluoro-4-methoxyphenyl)-2-(2,6-difluorophenyl)ethene
  参考文献：
  名称：

  Compounds as PDE IV and TNF inhibitors

  摘要：

  该发明涉及一种用于抑制肿瘤坏死因子（TNF）的产生或生理效应的化合物，或其N-氧化物或药用可接受的盐，该化合物适用于治疗患有与生理上有害的肿瘤坏死因子（TNF）过剩相关的疾病状态的患者。本发明范围内的化合物还抑制环状AMP磷酸二酯酶，并且适用于治疗与通过抑制环状AMP磷酸二酯酶调节的病理条件相关的疾病状态，这些疾病状态包括炎症和自身免疫性疾病，特别是第四型环状AMP磷酸二酯酶。因此，本发明涉及它们在药理上用于抑制TNF和/或环状AMP磷酸二酯酶的用途，包括含有这些化合物的药理组合物和其制备方法。

  公开号：

  US06472412B1

文献信息

• Compounds as PDE IV and TNF-inhibitors
  申请人：Fenton Garry

  公开号：US20060084809A1

  公开（公告）日：2006-04-20

  This invention is directed to a [di(ether or thioether)heteroaryl or fluoro substituted aryl] compound or an N-oxide thereof or a pharmaceutically acceptable salt thereof, which is useful for inhibiting the production or physiological effects of TNF in the treatment of a patient suffering from a disease state associated with a physiologically detrimental excess of tumor necrosis factor (TNF). Compounds within the scope of the present invention also inhibit cyclic AMP phosphodiesterase, and are useful in treating a disease state associated with pathological conditions that are modulated by inhibiting cyclic AMP phosphodiesterase, such disease states including inflammatory and autoimmune diseases, in particular type IV cyclic AMP phosphodiesterase. The present invention is therefore directed to their pharmacological use for inhibiting TNF and/or cyclic AMP phosphodiesterase, pharmacological compositions comprising the compounds and methods for their preparation.

  本发明涉及[含有(di(醚或硫醚)杂环或氟代芳基)化合物]或其N-氧化物或其药学上可接受的盐，该化合物在治疗患有与肿瘤坏死因子（TNF）生产或生理作用过量有害相关的疾病状态的患者中有用，能够抑制TNF的产生或生理作用。本发明范围内的化合物还抑制环磷酸腺苷磷酸二酯酶，并且在治疗与抑制环磷酸腺苷磷酸二酯酶相关的病理条件的疾病状态中有用，这些疾病状态包括炎症和自身免疫性疾病，特别是第四型环磷酸腺苷磷酸二酯酶。因此，本发明涉及它们在抑制TNF和/或环磷酸腺苷磷酸二酯酶方面的药理学用途，包括含有这些化合物的药理学组合物以及它们的制备方法。
• Compounds as PDE IV and TNF Inhibitors
  申请人：FENTON Garry

  公开号：US20080132706A1

  公开（公告）日：2008-06-05

  This invention is directed to a [di(ether or thioether)heteroaryl or fluoro substituted aryl] compound or an N-oxide thereof or a pharmaceutically acceptable salt thereof, which is useful for inhibiting the production or physiological effects of TNF in the treatment of a patient suffering from a disease state associated with a physiologically detrimental excess of tumor necrosis factor (TNF). Compounds within the scope of the present invention also inhibit cyclic AMP phosphodiesterase, and are useful in treating a disease state associated with pathological conditions that are modulated by inhibiting cyclic AMP phosphodiesterase, such disease states including inflammatory and autoimmune diseases, in particular type IV cyclic AMP phosphodiesterase. The present invention is therefore directed to their pharmacological use for inhibiting TNF and/or cyclic AMP phosphodiesterase, pharmacological compositions comprising the compounds and methods for their preparation.

  本发明涉及一种[含有(di(醚或硫醚)杂环或氟取代芳基)化合物或其N-氧化物或其药学上可接受的盐]，其在治疗患有与肿瘤坏死因子(TNF)生理有害过量相关的疾病状态的患者中，有用于抑制TNF的产生或生理效应。本发明范围内的化合物还抑制环磷酸腺苷磷酸二酯酶，并且在治疗与抑制环磷酸腺苷磷酸二酯酶相关的病理条件的疾病状态中有用，这些疾病状态包括炎症和自身免疫性疾病，特别是第四型环磷酸腺苷磷酸二酯酶。因此，本发明涉及它们的药理用途，用于抑制TNF和/或环磷酸腺苷磷酸二酯酶，包括含有这些化合物的药理组合物和其制备方法。
• COMPOUNDS AS PDE IV AND TNF INHIBITORS
  申请人：RHONE-POULENC RORER LIMITED

  公开号：EP0711282A1

  公开（公告）日：1996-05-15
• US6472412B1
  申请人：——

  公开号：US6472412B1

  公开（公告）日：2002-10-29
• US7045660B2
  申请人：——

  公开号：US7045660B2

  公开（公告）日：2006-05-16