(R)-1-(1-((6-fluoronaphthalen-2-yl)methyl)pyrrolidin-3-yl)-3-(2-(2-hydroxyethoxy)phenyl)urea | 592551-93-4

• 分子结构分类: 有机化合物 - 苯类化合物 - 萘
• 英文名称: (R)-1-(1-((6-fluoronaphthalen-2-yl)methyl)pyrrolidin-3-yl)-3-(2-(2-hydroxyethoxy)phenyl)urea
• 英文别名: 1-[(3R)-1-[(6-fluoronaphthalen-2-yl)methyl]pyrrolidin-3-yl]-3-[2-(2-hydroxyethoxy)phenyl]urea
• CAS: 592551-93-4
• 化学式: C₂₄H₂₆FN₃O₃
• 分子量: 423.487
• InChiKey: SURDXQHAGDOKKM-OAQYLSRUSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.3
• 重原子数：
  31
• 可旋转键数：
  7
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.29
• 拓扑面积：
  73.8
• 氢给体数：
  3
• 氢受体数：
  5

反应信息

• 作为产物：
  描述：

  2-(2-硝基苯氧基)乙醇 在 咪唑 、 10% Pd/C 、 四丁基氟化铵 、 氢气 、 碳酸氢钠 作用下， 以 四氢呋喃 、 乙醇 、 乙腈 为溶剂， 生成 (R)-1-(1-((6-fluoronaphthalen-2-yl)methyl)pyrrolidin-3-yl)-3-(2-(2-hydroxyethoxy)phenyl)urea
  参考文献：
  名称：

  Pyrrolidinyl phenylurea derivatives as novel CCR3 antagonists

  摘要：

  Optimization starting with our lead compound 1 (IC50 = 4.9 nM) led to the identification of pyrrolidinyl phenylurea derivatives. Further modification toward improvement of the bioavailability provided (R)-1-(1-((6-fluoronaphthalen-2-yl)methyl)pyrrolidin-3-yl)-3-(2-(2-hydroxyethoxy)phenyl)urea 32 (IC50 = 1.7 nM), a potent and orally active CCR3 antagonist. (C) 2012 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2012.09.035

文献信息

• New compositions and methods of treating and/or preventing chronic obstructive pulmonary disease
  申请人：UNIVERSITE DE BORDEAUX

  公开号：EP3050574A1

  公开（公告）日：2016-08-03

  The present invention relates to a novel composition for the treatment and/or the prevention of chronic obstructive pulmonary disease (COPD) and acute exacerbations of chronic obstructive pulmonary disease (AECOPD).

  本发明涉及一种用于治疗和/或预防慢性阻塞性肺病（COPD）和慢性阻塞性肺病急性加重（AECOPD）的新型组合物。
• CHEMOKINE RECEPTOR CXCR4 INHIBITORS FOR TREATING AND/OR PREVENTING CHRONIC OBSTRUCTIVE PULMONARY DISEASE
  申请人：UNIVERSITE DE BORDEAUX

  公开号：EP3613435A1

  公开（公告）日：2020-02-26

  The present invention relates to a novel composition for the treatment and/or the prevention of chronic obstructive pulmonary disease (COPD) and acute exacerbations of chronic obstructive pulmonary disease (AECOPD).

  本发明涉及一种用于治疗和/或预防慢性阻塞性肺病（COPD）和慢性阻塞性肺病急性加重（AECOPD）的新型组合物。
• Inhibition of chemokine CCL7 or receptor CCR3 of same for the treatment and diagnosis of prostate cancer
  申请人：Universite Paul Sabatier (Toulouse III)

  公开号：US10401365B2

  公开（公告）日：2019-09-03

  The invention concerns an inhibitor of the expression of chemokine CCL7 or an inhibitor of the expression of the receptor CCR3 or an inhibitor of CCL7/CCR3 interaction for the use of same to prevent or treat the extension of prostate cancer outside the prostatic capsule in a subject. The invention also concerns a method for determining the degree of aggressiveness of a prostate cancer tumor in a subject suffering from prostate cancer, comprising a step of determining the concentration or level of expression of the receptor CCR3 in a sample of prostate tumor cells obtained from said subject.

  本发明涉及一种趋化因子CCL7表达抑制剂或受体CCR3表达抑制剂或CCL7/CCR3相互作用抑制剂，用于预防或治疗受试者的前列腺癌向前列腺囊外延伸。本发明还涉及一种确定前列腺癌患者前列腺癌肿瘤侵袭程度的方法，该方法包括一个步骤，即确定从所述患者处获得的前列腺肿瘤细胞样本中受体CCR3的浓度或表达水平。
• Methods of treating and/or preventing chronic obstructive pulmonary disease
  申请人：UNIVERSITE DE BORDEAUX

  公开号：US10813911B2

  公开（公告）日：2020-10-27

  The present invention relates to a novel composition or method of use for the treatment and/or the prevention of chronic obstructive pulmonary disease (COPD) and acute exacerbations of chronic obstructive pulmonary disease (AECOPDs).

  本发明涉及一种用于治疗和/或预防慢性阻塞性肺病（COPD）和慢性阻塞性肺病急性加重（AECOPDs）的新型组合物或使用方法。
• Use of plerixafor for treating and/or preventing acute exacerbations of chronic obstructive pulmonary disease
  申请人：UNIVERSITE DE BORDEAUX

  公开号：EP3050574B1

  公开（公告）日：2019-10-09