1-(4-fIuorophenyl)-2-(4-(imidazo[1,2-α]pyridine-8-carbonyl)piperazin-1-yl)ethanone | 1116690-52-8

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: 1-(4-fIuorophenyl)-2-(4-(imidazo[1,2-α]pyridine-8-carbonyl)piperazin-1-yl)ethanone
• 英文别名: 1-(4-Fluorophenyl)-2-(4-(imidazo[1,2-alpha]pyridine-8-carbonyl)piperazin-1-yl)ethanone；1-(4-fluorophenyl)-2-[4-(imidazo[1,2-a]pyridine-8-carbonyl)piperazin-1-yl]ethanone
• CAS: 1116690-52-8
• 化学式: C₂₀H₁₉FN₄O₂
• 分子量: 366.395
• InChiKey: PENJSKTXKZICAN-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.5
• 重原子数：
  27
• 可旋转键数：
  4
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.25
• 拓扑面积：
  57.9
• 氢给体数：
  0
• 氢受体数：
  5

反应信息

• 作为产物：
  描述：

  8-羧酸咪唑并[1,2-A]吡啶 、 1-(4-fluorophenyl)-2-(piperazin-1-yl)ethanone hydrochloride 以to afford a brown oil (28.2 mg)的产率得到
  参考文献：
  名称：

  IMIDAZO[1,2-A]PYRIDINE DERIVATIVES AS MODULATORS OF THE 5-HT2A SEROTONIN RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO

  摘要：

  公式（Ia）的咪唑[1,2-α]吡啶衍生物及其制药组合物，可调节5-HT2A 5-羟色胺受体的活性。该化合物及其制药组合物适用于治疗失眠、睡眠障碍、血小板聚集、冠状动脉疾病、心肌梗死、短暂性脑缺血发作、心绞痛、中风、心房颤动、血栓形成、哮喘或其症状、烦躁或其症状、行为障碍、药物诱导的精神病、兴奋性精神病、Gilles de Ia Tourette综合症、躁狂障碍、器质性或NOS精神病、精神病性障碍、急性精神分裂症、慢性精神分裂症、NOS精神分裂症及相关疾病、糖尿病相关疾病、进行性多灶性白质脑病等治疗方法。本发明还涉及与其他药物分别或联合使用治疗5-HT2A 5-羟色胺受体介导的疾病的方法。

  公开号：

  US20110263592A1

文献信息

• Imidazo[1,2-α]pyridine derivatives as modulators of the 5-HT2A serotonin receptor useful for the treatment of disorders related thereto
  申请人：Arena Pharmaceuticals, Inc.

  公开号：US10058549B2

  公开（公告）日：2018-08-28

  rmidazo[1,2-α]pyridine derivatives of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of insomnia, dyssomnia, parasomnia and related sleep disorders, platelet aggregation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, thrombosis, asthma or symptoms thereof, agitation or symptoms thereof, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de Ia Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorders, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, diabetic- related disorders, progressive multifocal leukoencephalopathy and the like. The present invention also relates to methods for the treatment of 5-HT2A serotonin receptor mediated disorders in combination with other pharmaceutical agents administered separately or together.

  式（Ia）的咪唑并[1,2-α]吡啶衍生物及其药物组合物，可调节 5-HT2A 血清素受体的活性。其化合物和药物组合物用于治疗失眠、失眠症、副失眠和相关睡眠障碍、血小板聚集、冠状动脉疾病、心肌梗塞、短暂性脑缺血发作、心绞痛、中风、心房颤动、血栓形成、哮喘或其症状、躁动或其症状、行为障碍、药物性精神病、兴奋性精神病、Gilles de Ia Tourette 综合征、躁狂症、器质性或非器质性精神病、精神障碍、精神病、急性精神分裂症、慢性精神分裂症、非器质性精神分裂症及相关疾病、糖尿病相关疾病、进行性多灶性白质脑病等。本发明还涉及与其他药剂单独或联合给药治疗 5-HT2A 血清素受体介导的疾病的方法。
• US9567327B2
  申请人：——

  公开号：US9567327B2

  公开（公告）日：2017-02-14
• [EN] IMIDAZO[L,2-a]PYRIDINE DERIVATIVES AS MODULATORS OF THE 5-HT2A SEROTONIN RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO<br/>[FR] DÉRIVÉS D'IMIDAZO[L,2-?]PYRIDINE UTILISÉS COMME MODULATEURS DU RÉCEPTEUR SÉROTONINERGIQUE 5-HT2A DANS LE TRAITEMENT DES TROUBLES QUI LUI SONT ASSOCIÉS
  申请人：ARENA PHARM INC

  公开号：WO2009023253A2

  公开（公告）日：2009-02-19

  rmidazo[l,2-α]pyridine derivatives of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of insomnia, dyssomnia, parasomnia and related sleep disorders, platelet aggregation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, thrombosis, asthma or symptoms thereof, agitation or symptoms thereof, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de Ia Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorders, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, diabetic- related disorders, progressive multifocal leukoencephalopathy and the like. The present invention also relates to methods for the treatment of 5-HT2A serotonin receptor mediated disorders in combination with other pharmaceutical agents administered separately or together.