N-(3-{4-[4-(8-oxo-8H-[1,3]dioxolo[4,5-g]chromen-7-yl)butyl]piperazin-1-yl}phenyl)methanesulfonamide | 1268334-25-3

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪烷类
• 英文名称: N-(3-{4-[4-(8-oxo-8H-[1,3]dioxolo[4,5-g]chromen-7-yl)butyl]piperazin-1-yl}phenyl)methanesulfonamide
• 英文别名: F-17464 Free base；N-[3-[4-[4-(8-oxo-[1,3]dioxolo[4,5-g]chromen-7-yl)butyl]piperazin-1-yl]phenyl]methanesulfonamide
• CAS: 1268334-25-3
• 化学式: C₂₅H₂₉N₃O₆S
• 分子量: 499.588
• InChiKey: KLOYLPZTHLSRRB-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.9
• 重原子数：
  35
• 可旋转键数：
  8
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.4
• 拓扑面积：
  106
• 氢给体数：
  1
• 氢受体数：
  9

文献信息

• [EN] CHROMONE DERIVATIVES, A PROCESS FOR THEIR PREPARATION AND THEIR THERAPEUTIC APPLICATIONS<br/>[FR] DÉRIVÉS DE CHROMONE, LEUR PROCÉDÉ DE PRÉPARATION ET LEURS APPLICATIONS THÉRAPEUTIQUES
  申请人：PF MEDICAMENT

  公开号：WO2011027289A1

  公开（公告）日：2011-03-10

  The present invention relates to chromone derivatives, their preparation, their pharmaceutical compositions and their application as D3 dopaminergic ligands as a medicament for disorders of the central nervous system.

  本发明涉及香豆素衍生物，它们的制备、药物组合物以及它们作为D3多巴胺能受体配体在中枢神经系统疾病的药物应用。
• CHROMONE DERIVATIVES, A PROCESS FOR THEIR PREPARATION AND THEIR THERAPEUTIC APPLICATIONS
  申请人：Sokoloff Pierre

  公开号：US20120157463A1

  公开（公告）日：2012-06-21

  The present invention relates to chromone derivatives, their preparation, their pharmaceutical compositions and their application as D3 dopaminergic ligands as a medicament for disorders of the central nervous system.

  本发明涉及香豆素衍生物，其制备方法，其制药组合物以及作为D3多巴胺受体配体在中枢神经系统疾病的药物应用。
• Chromone derivative as a dopamine D3 receptor antagonist for its use for the treatment of autism spectrum disorder
  申请人：PIERRE FABRE MEDICAMENT

  公开号：US10028948B2

  公开（公告）日：2018-07-24

  The present invention claims a chromone derivative and pharmaceutical compositions and combinations comprising a least the said derivative, which is a dopamine D3 receptor antagonist, for their use for the treatment of autism spectrum disorder.

  本发明要求一种铬酮衍生物以及至少包含上述衍生物的药物组合物和组合物，该衍生物是一种多巴胺D3受体拮抗剂，用于治疗自闭症谱系障碍。
• Treatment of schizophrenia
  申请人：PIERRE FABRE MEDICAMENT

  公开号：US10842789B2

  公开（公告）日：2020-11-24

  The present invention relates to a method of treating schizophrenia in a subject in need thereof, the method comprising administering to the subject a therapeutically effective amount of a selective D3 antagonist, wherein said subject has at least one negative symptom (NS) among the following core negative symptoms in PANSS: Blunted Affect (N1), Emotional Withdrawal (N2), Poor Rapport (N3), Passive withdrawal (N4), and Lack of Spontaneity (N6); with moderate or higher severity. Methods for improving the probability of success and/or the effect of a treatment of schizophrenia in a subject in need thereof are also described.

  本发明涉及一种治疗有需要的受试者的精神分裂症的方法，该方法包括向受试者施用治疗有效量的选择性D3拮抗剂，其中所述受试者具有PANSS中以下核心阴性症状中的至少一种阴性症状（NS）：情感迟钝（N1）、情感退缩（N2）、亲和力差（N3）、被动退缩（N4）和缺乏自发性（N6）；且具有中等或更高的严重程度。此外，还介绍了提高需要治疗精神分裂症的受试者的成功概率和/或治疗效果的方法。
• A CHROMONE DERIVATIVE AS A DOPAMINE D3 RECEPTOR ANTAGONIST FOR ITS USE FOR THE TREATMENT OF AUTISM SPECTRUM DISORDER
  申请人：Pierre Fabre Médicament

  公开号：EP3079688A1

  公开（公告）日：2016-10-19