1-(3-fluoro-5-thiophen-3-yl-phenyl)-piperazine

• 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: 1-(3-fluoro-5-thiophen-3-yl-phenyl)-piperazine
• 英文别名: 1-(3-fluoro-5-thiophen-3-ylphenyl)piperazine
• 化学式: C₁₄H₁₅FN₂S
• 分子量: 262.351
• InChiKey: BAJVCQQBZLAKTP-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.8
• 重原子数：
  18
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.29
• 拓扑面积：
  43.5
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  3-(3-bromo-5-fluoro-phenyl)-thiophene 、 N-Boc-哌嗪 在 tris-(dibenzylideneacetone)dipalladium(0) 三叔丁基膦 、 sodium t-butanolate 作用下， 以 正己烷 、 甲苯 为溶剂， 反应 5.0h， 生成 1-(3-fluoro-5-thiophen-3-yl-phenyl)-piperazine
  参考文献：
  名称：

  WO2006/65600

  摘要：

  公开号：

文献信息

• N-Biaryl and N-Arylheteroaryl Piperazine Derivatives as Modulators of the 5Ht2c Receptor Useful For the Treatment of Disorders Related Thereto
  申请人：Smith Brian M.

  公开号：US20080119477A1

  公开（公告）日：2008-05-22

  The present invention relates to certain biarylz and arylheteroaryl piperazine derivatives of Formula (Ia) that are modulators of the 5HT 2c receptor. Accordingly, compounds of the present invention are useful for the treatment of 5HT 2c receptor associated diseases or disorders, such as, obesity, Alzheimer Disease, erectile dysfunction and related disorders.

  本发明涉及公式(Ia)中的某些双芳基和芳基杂芳基哌嗪衍生物，它们是5HT2c受体的调节剂。因此，本发明的化合物对于治疗与5HT2c受体相关的疾病或障碍，如肥胖症、阿尔茨海默病、勃起功能障碍和相关疾病是有用的。
• THERAPEUTIC AGENT FOR STRESS URINARY INCONTINENCE AND FECAL INCONTINENCE
  申请人：Takeda Pharmaceutical Company Limited

  公开号：EP3733204A1

  公开（公告）日：2020-11-04

  The present invention provides a medicament for use in treating stress urinary incontinence with fewer adverse effects including a body weight lowering effect. The present invention also provides a medicament for use in treating a disease such as incontinence of feces and further provide a medicament for use in treating a disease such as incontinence of feces with fewer adverse effects including a body weight lowering effect. A medicament for use in treating stress urinary incontinence, comprising a 5-HT2C receptor agonist, wherein the medicament is administered at a dosage lower than the minimum dosage of the agonist as an anti-obesity drug. A medicament for use in treating incontinence of feces, etc., comprising a 5-HT2C receptor agonist. A medicament for use in treating incontinence of feces, comprising a 5-HT2C receptor agonist, wherein the medicament is administered at a dosage lower than the minimum dosage of the agonist as an anti-obesity drug.

  本发明提供了一种用于治疗压力性尿失禁的药物，其不良反应较少，包括降低体重的效果。本发明还提供了一种用于治疗大便失禁等疾病的药物，并进一步提供了一种用于治疗大便失禁等疾病的药物，其不良反应较少，包括有降低体重的作用。 一种用于治疗压力性尿失禁的药物，包含一种5-HT2C受体激动剂，其中该药物的给药剂量低于作为抗肥胖药物的激动剂的最小剂量。一种用于治疗大便失禁等的药物，包含一种 5-HT2C 受体激动剂。一种用于治疗大便失禁等的药物，包含一种5-HT2C受体激动剂，其中该药物作为抗肥胖药物以低于该激动剂最小剂量的剂量给药。
• N-BIARYL AND N-ARYLHETEROARYL PIPERAZINE DERIVATIVES AS MODULATORS OF THE 5HT2C RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO
  申请人：Arena Pharmaceuticals, Inc.

  公开号：EP1828156A2

  公开（公告）日：2007-09-05
• AGENT FOR TREATING FIBROMYALGIA
  申请人：Nagakura Yukinori

  公开号：US20120253036A1

  公开（公告）日：2012-10-04

  An agent for treating fibromyalgia containing a 5-HT 2C receptor agonist as an active ingredient
• THERAPEUTIC AGENTS FOR STRESS URINARY INCONTINENCE AND INCOTINENCE OF FECES
  申请人：Takeda Pharmaceutical Company Limited

  公开号：US20210052600A1

  公开（公告）日：2021-02-25

  The present invention provides a medicament for use in treating stress urinary incontinence with fewer adverse effects including a body weight lowering effect. The present invention also provides a medicament for use in treating a disease such as incontinence of feces and further provide a medicament for use in treating a disease such as incontinence of feces with fewer adverse effects including a body weight lowering effect. A medicament for use in treating stress urinary incontinence, comprising a 5-HT 2C receptor agonist, wherein the medicament is administered at a dosage lower than the minimum dosage of the agonist as an anti-obesity drug. A medicament for use in treating incontinence of feces, etc., comprising a 5-HT 2C receptor agonist. A medicament for use in treating incontinence of feces, comprising a 5-HT 2C receptor agonist, wherein the medicament is administered at a dosage lower than the minimum dosage of the agonist as an anti-obesity drug.