(S)-3-(4-fluorophenyl)pyrrolidine

• 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: (S)-3-(4-fluorophenyl)pyrrolidine
• 英文别名: (3S)-3-(4-fluorophenyl)pyrrolidine
• 化学式: C₁₀H₁₂FN
• 分子量: 165.21
• InChiKey: IWOQWISAVOSATC-SECBINFHSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.8
• 重原子数：
  12
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.4
• 拓扑面积：
  12
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  (S)-3-(4-fluorophenyl)pyrrolidine 、 3-(8-fluoro-5-methyl-1-oxo-1,2-dihydroisoquinolin-3-yl)propyl methanesulfonate 在 碳酸氢钠 、 sodium iodide 作用下， 以 乙腈 为溶剂， 生成 (S)-8-fluoro-3-(3-(3-(4-fluorophenyl)pyrrolidin-1-yl)propyl)-5-methylisoquinolin-1(2H)-one
  参考文献：
  名称：

  ISOQUINOLINONE DERIVATIVE, PREPARATION METHOD THEREFOR, AND PHARMACEUTICAL COMPOSITION, COMPRISING SAME AS ACTIVE INGREDIENT, FOR PREVENTION OR TREATMENT OF POLY(ADP-RIBOSE)POLYMERASE-1 (PARP-1)-ASSOCIATED DISEASE

  摘要：

  本发明涉及异喹啉酮衍生物、其制备方法以及用于预防或治疗与聚(ADP-核糖)聚合酶-1(PARP-1)有关的疾病的药物组合物，其中该异喹啉酮衍生物在纳摩尔单位浓度下表现出优异的PARP-1抑制作用，并在眼科疾病或障碍，特别是视网膜疾病方面表现出优异的细胞保护作用（凋亡抑制作用），因此可以有效地用作预防或治疗PARP-1相关疾病（例如眼科疾病或障碍）的药物组合物的活性成分。

  公开号：

  EP4053106A1

文献信息

• [EN] NOVEL COMPOUNDS FOR THE TREATMENT OF PARASITIC INFECTIONS<br/>[FR] NOUVEAUX COMPOSÉS POUR LE TRAITEMENT D'INFECTIONS PARASITAIRES
  申请人：GLAXOSMITHKLINE IP DEV LTD

  公开号：WO2019145360A1

  公开（公告）日：2019-08-01

  The present invention relates to novel compounds or pharmaceutically acceptable salts thereof, corresponding compositions, and methods and/or uses in therapy, for example in the treatment of parasitic infections such as malaria, in particular infection by Plasmodium falciparum. (I)

  本发明涉及新化合物或其药用盐，相应的组合物，以及在治疗中的方法和/或用途，例如在治疗寄生虫感染，如疟疾，特别是疟原虫感染方面的应用。
• [EN] 2,2-DIFLUORODIOXOLO A2A RECEPTOR ANTAGONISTS<br/>[FR] ANTAGONISTES 2,2-DIFLUORODIOXOLO DU RÉCEPTEUR A2A
  申请人：MERCK SHARP & DOHME

  公开号：WO2015027431A1

  公开（公告）日：2015-03-05

  The present invention is directed to 2,2-difluorodioxolo compounds that are antagonists of A2A receptor. The present invention is also directed to uses of the 2,2-difluorodioxolo compounds described herein in the potential treatment or prevention of neurological disorders and diseases in which A2A receptor are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds and to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which A2A receptors are involved.

  本发明涉及对A2A受体拮抗剂的2,2-二氟二氧杂环己烷化合物。本发明还涉及在潜在治疗或预防涉及A2A受体的神经系统疾病和疾病中使用本文所述的2,2-二氟二氧杂环己烷化合物。本发明还涉及包含这些化合物的药物组合物以及在预防或治疗涉及A2A受体的这些疾病中使用这些药物组合物的用途。
• [EN] 2,2-DIFLUORODIOXOLO A2A RECEPTOR ANTAGONISTS<br/>[FR] 2,2-DIFLUORODIOXOLO ANTAGONISTES DE RÉCEPTEURS A2A
  申请人：MERCK SHARP & DOHME

  公开号：WO2015031221A1

  公开（公告）日：2015-03-05

  The present invention is directed to 2,2-difluorodioxolo compounds that are antagonists of A2A receptor. The present invention is also directed to uses of the 2,2- difluorodioxolo compounds described herein in the potential treatment or prevention of 5 neurological disorders and diseases in which A2A receptor are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds and to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which A2A receptors are involved.

  本发明涉及2,2-二氟二氧杂环丁烷类化合物，其为A2A受体拮抗剂。本发明还涉及在潜在治疗或预防A2A受体参与的神经系统疾病和疾病中使用本文描述的2,2-二氟二氧杂环丁烷类化合物。本发明还涉及含有这些化合物的药物组合物以及这些药物组合物在预防或治疗A2A受体参与的相关疾病中的用途。
• PYRROLIDINE DERIVATIVES FOR THE TREATMENT OF A DISEASE DEPENDING ON THE ACTIVITY OF RENIN
  申请人：Breitenstein Werner

  公开号：US20100087427A1

  公开（公告）日：2010-04-08

  Novel 3-mono-, 3,4-di- and 3,4,4,-tri-substituted pyrrolidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on inappropriate activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on inappropriate activity of renin; the use of a compound of that class in the treatment of a disease that depends on inappropriate activity of renin; pharmaceutical formulations comprising a said substituted pyrrolidine compound, and/or a method of treatment comprising administering a said substituted pyrrolidine compound, a method for the manufacture of said substituted pyrrolidine compounds, and novel intermediates and partial steps for their synthesis are described. The substituted pyrrolidine compounds are especially of the formula I wherein the substituents are as described in the specification.

  小说3-单一、3,4-二和3,4,4-三取代吡咯烷化合物，这些化合物用于诊断和治疗温血动物，特别是用于治疗依赖于肾素不适当活性的疾病（=失调）；该类化合物用于制备用于治疗依赖于肾素不适当活性的疾病的制药配方；该类化合物用于治疗依赖于肾素不适当活性的疾病；包括所述取代吡咯烷化合物的制药配方和/或包括给予所述取代吡咯烷化合物的治疗方法，以及描述了制备所述取代吡咯烷化合物的新型中间体和部分步骤。所述取代吡咯烷化合物特别是公式I的取代基如说明书所述。
• 2,2-DIFLUORODIOXOLO A2A RECEPTOR ANTAGONISTS
  申请人：ALI Amjad

  公开号：US20160214997A1

  公开（公告）日：2016-07-28

  The present invention is directed to 2,2-difluorodioxolo compounds that are antagonists of A 2A receptor. The present invention is also directed to uses of the 2,2-difluorodioxolo compounds described herein in the potential treatment or prevention of neurological disorders and diseases in which A 2A receptor are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds and to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which A 2A receptors are involved.

  本发明涉及2,2-二氟二氧杂环己烷化合物，其为A2A受体拮抗剂。本发明还涉及使用本说明书中描述的2,2-二氟二氧杂环己烷化合物潜在地治疗或预防神经系统疾病和疾病，其中涉及A2A受体。本发明还涉及包含这些化合物的制药组合物以及使用这些制药组合物预防或治疗涉及A2A受体的这些疾病。