3-(4-phenoxyphenyl)imidazolidine-2,4-dione | 923039-29-6

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑烷类
• 英文名称: 3-(4-phenoxyphenyl)imidazolidine-2,4-dione
• CAS: 923039-29-6
• 化学式: C₁₅H₁₂N₂O₃
• 分子量: 268.272
• InChiKey: UHRZWZOMIKMALQ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.4
• 重原子数：
  20
• 可旋转键数：
  3
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.07
• 拓扑面积：
  58.6
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  3-(4-phenoxyphenyl)imidazolidine-2,4-dione 在 四氢吡咯 、 盐酸 、 magnesium sulfate 作用下， 以 乙醇 为溶剂， 反应 2.0h， 生成 (Z)-4-[2,5-Dioxo-1-(4-phenoxy-phenyl)-imidazolidin-4-ylidenemethyl]-benzaldehyde
  参考文献：
  名称：

  Design and synthesis of novel hydantoin-containing melanin-concentrating hormone receptor antagonists

  摘要：

  We report here new chemical series acting as antagonists of melanin-concentrating hormone receptor I (MCHR-1). Synthesis and structure-activity relationships are described leading to the identification of compounds with optimized in vitro pharmacological and in vitro ADME profiles. In vivo activity has been demonstrated in animal models of food intake and depression. (c) 2007 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2007.04.012
• 作为产物：
  描述：

  ethyl 2-[(4-phenoxyphenyl)carbamoylamino]acetate 在 盐酸 、 sodium hydroxide 作用下， 以 乙醇 为溶剂， 生成 3-(4-phenoxyphenyl)imidazolidine-2,4-dione
  参考文献：
  名称：

  Design and synthesis of novel hydantoin-containing melanin-concentrating hormone receptor antagonists

  摘要：

  We report here new chemical series acting as antagonists of melanin-concentrating hormone receptor I (MCHR-1). Synthesis and structure-activity relationships are described leading to the identification of compounds with optimized in vitro pharmacological and in vitro ADME profiles. In vivo activity has been demonstrated in animal models of food intake and depression. (c) 2007 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2007.04.012

文献信息

• A direct fixation of CO₂ for isotopic labelling of hydantoins using iodine–phosphine charge transfer complexes
  作者：John-Paul J. Bow、Valentina Adami、Agostino Marasco、Gaute Grønnevik、Dean A. Rivers、Guiseppe Alvaro、Patrick J. Riss

  DOI：10.1039/d2cc01754g

  日期：——

  Herein, we report a method for the isotopic labelling of hydantoins directly from CO2 by means of trimethyl-λ5-phosphine diiodide mediated carbonyl insertion. The method is suitable for 13C-labelling of diverse substrates and was implementated for 11C-labelling in PET-imaging facilities for the synthesis of radiotracers. Isolated yields of 90% and radiochemical yields of 89% were achieved for hydantoin

  在此，我们报道了一种通过三甲基-λ 5 -二碘化膦介导的羰基插入直接从 CO 2中同位素标记乙内酰脲的方法。该方法适用于不同底物的13 C-标记，并在 PET 成像设备中用于11 C-标记，用于合成放射性示踪剂。制剂中含有乙内酰脲的候选药物在 30 分钟内实现了 90% 的分离产率和 89% 的放射化学产率，具有高摩尔活性 (>400 MBq nmol -1 )。
• Imidazolidinedione derivatives
  申请人：AUTIFONY THERAPUTICS LIMITED

  公开号：US10632118B2

  公开（公告）日：2020-04-28

  The invention provides a compound of formula (Ia), and pharmaceutically acceptable salts thereof. The invention also provides use of the compounds or salts as modulators of Kv3.1 and/or Kv3.2, and in the treatment of diseases or disorders where a modulator of Kv3.1 and/or Kv3.2 is required, such as depression and mood disorders, hearing disorders, schizopherenea, substance abuse disorders, sleep disorders or epilepsy.

  本发明提供了一种式 (Ia) 的化合物、 及其药学上可接受的盐。本发明还提供了这些化合物或盐作为 Kv3.1 和/或 Kv3.2 调节剂的用途，以及在治疗需要 Kv3.1 和/或 Kv3.2 调节剂的疾病或紊乱中的用途，例如抑郁症和情绪紊乱、听力紊乱、精神分裂症、药物滥用紊乱、睡眠紊乱或癫痫。
• IMIDAZOLIDINEDIONE DERIVATIVES
  申请人：AUTIFONY THERAPEUTICS LIMITED

  公开号：US20170065585A1

  公开（公告）日：2017-03-09

  The invention provides a compound of formula (Ia), and pharmaceutically acceptable salts thereof. The invention also provides use of the compounds or salts as modulators of Kv3.1 and/or Kv3.2, and in the treatment of diseases or disorders where a modulator of Kv3.1 and/or Kv3.2 is required, such as depression and mood disorders, hearing disorders, schizopherenea, substance abuse disorders, sleep disorders or epilepsy.
• US9849131B2
  申请人：——

  公开号：US9849131B2

  公开（公告）日：2017-12-26
• [EN] COMPOUNDS DERIVED FROM 5-BENZYLIDENE IMIDAZOLIDINE 2,4-DIONE AND THEIR USE AS MCHR-1 ANTAGONISTS<br/>[FR] COMPOSES DERIVES DE 5-BENZYLIDENE IMIDAZOLIDINE 2,4-DIONE ET LEUR UTILISATION EN TANT QU'ANTAGONISTES DE MCHR-1
  申请人：CEREP

  公开号：WO2007012670A2

  公开（公告）日：2007-02-01

  [EN] The invention concerns the compounds of general formula (I), wherein: Ar¹, L¹, R¹, R², R³, R⁴ R⁵, R⁶, L², Q, and n are such as defined in the claims, and their preparation method. The invention also concerns the use of the compounds of formula (I) as medicine, and more particularly for preparing a medicine for treating obesity and related diseases, an anorexiant and/or a medicine for losing weight, a medicine for treating depression and/or anxiety, and more generally a medicine for treating a disease associated with MCH (melanin-concentrating hormone) receptors.
  [FR] La présente invention concerne les composés de formule générale (I) suivante :dans laquelle : Ar¹, L¹, R¹, R², R³, R⁴ R⁵, R⁶, L², Q, et n sont tels que définis dans les revendications, ainsi que leur procédé de préparation. L'invention concerne également l'utilisation des composés de formule (I)en tant que médicament, et plus particulièrement pour la préparation d'un médicament destiné au traitement de l'obésité et des maladies associées, d'un médicament coupe-faim et/ou d'un médicament entraînant une perte de poids, d'un médicament destiné au traitement de la dépression et/ou de l'anxiété, et plus généralement d'un médicament destiné au traitement d'une maladie associée aux récepteurs MCH (mélanine concentrating hormone).