4-benzo[b]thiophenylpiperidine | 56838-93-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并噻吩类
• 英文名称: 4-benzo[b]thiophenylpiperidine
• 英文别名: 4-(benzo(b)thiophen-2-yl)pyperidine；4-(benzo[b]thien-2-yl)-piperidine；4-(benzo(b)thiophen-2-yl)piperidine；2-benzo(b)thiophene-piperidine；4-(1-Benzothiophen-2-yl)piperidine
• CAS: 56838-93-8
• 化学式: C₁₃H₁₅NS
• 分子量: 217.335
• InChiKey: KXPOMJGPFGAYEC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.1
• 重原子数：
  15
• 可旋转键数：
  1
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  40.3
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  (S)-2-(4-glycidyloxybenzo(b)furan-2-yl)-5-methyl-1,3,4-oxadiazole 、 4-benzo[b]thiophenylpiperidine 在 盐酸 作用下， 以 1,4-二氧六环 、 乙醇 为溶剂， 生成 (S)-1-(4-(benzo(b)thiophen-2-yl)pyperidino)-3-(2-(5-methyl-1,3,4-oxadiazol-2-yl)benzo(b)furan-4-yloxy)-2-propanol hydrochloride
  参考文献：
  名称：

  Phenoxypropylamine compounds

  摘要：

  本发明涉及一种公式（I）中的苯氧丙胺化合物： 1 其中每个符号如说明书中所定义，其光学活性化合物或其药物可接受的盐及水合物，同时显示出对5-HT 1A 受体的选择性亲和力和拮抗活性，以及5-HT再摄取抑制活性，并且可以用作快速表达抗抑郁效果的抗抑郁药。

  公开号：

  US20020111358A1
• 作为产物：
  描述：

  4-(benzo[b]thiophen-2-yl)-1,2,3,6-tetrahydropyridine 在 palladium 10% on activated carbon 氢气 作用下， 以 乙醇 为溶剂， 20.0 ℃ 、413.69 kPa 条件下， 生成 4-benzo[b]thiophenylpiperidine
  参考文献：
  名称：

  Piperidine derivatives as reuptake inhibitors

  摘要：

  本发明提供了式（I）的化合物以及一种抑制5-羟色胺再摄取和拮抗5-羟色胺受体的方法，包括向需要此类治疗的受试者施用式（I）的化合物的有效量。

  公开号：

  US06828332B1

文献信息

• Piperidine derivatives as reuptake inhibitors
  申请人：Eli Lilly and Company

  公开号：US06828332B1

  公开（公告）日：2004-12-07

  The present invention provides compounds of formula (I) and a method of inhibiting the reuptake of serotonin and antagonizing the serotonin receptor which comprises administering to a subject in need of such treatment an effective amount of a compound of formula (I).

  本发明提供了式（I）的化合物以及一种抑制5-羟色胺再摄取和拮抗5-羟色胺受体的方法，包括向需要此类治疗的受试者施用式（I）的化合物的有效量。
• [EN] HETEROCYCLIC SUBSTITUTED CARBONYL DERIVATIVES AND THEIR USE AS DOPAMINE D3 RECEPTOR LIGANDS<br/>[FR] DERIVES DE CARBONYLE SUBSTITUES HETEROCYCLIQUES ET UTILISATION DE CEUX-CI EN TANT QUE LIGANDS DU RECEPTEUR DE LA DOPAMINE D3
  申请人：AVENTIS PHARMA INC

  公开号：WO2002066446A1

  公开（公告）日：2002-08-29

  The invention relates to heterocyclic substituted carbonyl derivatives that display selective binding to dopamine D3 receptors. In another aspect, the invention relates to a method for treating central nervous system disorders associated with the dopamine D3 receptor activity in a patient in need of such treatment comprising administering to the subject a therapeutically effective amount of said compounds for alleviation of such disorder. The central nervous system disorders that may be treated with these compounds include Psychotic Disorders, Substance Dependence, Substance Abuse, Dyskinetic Disorders (e.g. Parkinson s Disease, Parkinsonism, Neuroleptic-Induced Tardive Dyskinesia, Gilles de la Tourette Syndrome and Huntington s Disease), Dementia, Anxiety Disorders, Sleep Disorders, Circadian Rhythm Disorders and Mood Disorders. The subject invention is also directed towards processes for the preparation of the compounds described herein as well as methods for making and using the compounds as imaging agents for dopamine D¿3 receptors.

  本发明涉及杂环取代羰基衍生物，其具有选择性地结合多巴胺D3受体。另一方面，本发明涉及一种用于治疗与多巴胺D3受体活性相关的中枢神经系统疾病的方法，包括向需要此类治疗的患者施用所述化合物的治疗有效量，以缓解此类疾病。这些化合物可以治疗的中枢神经系统疾病包括精神疾病、物质依赖、物质滥用、运动障碍（例如帕金森病、帕金森综合症、神经阻滞引起的迟发性运动障碍、吉尔·德·拉·图雷特综合症和亨廷顿病）、痴呆、焦虑症、睡眠障碍、昼夜节律紊乱和情绪障碍。本发明还涉及制备所述化合物的过程，以及将所述化合物用作多巴胺D3受体成像剂的方法。
• Proline derivatives and use thereof as drugs
  申请人：Kitajima Hiroshi

  公开号：US20050245538A1

  公开（公告）日：2005-11-03

  The present invention aims at providing compounds having therapeutic effects due to a DPP-IV inhibitory action, and satisfactory as pharmaceutical products. The present inventors have found that derivatives having a substituent introduced into the γ-position of proline represented by the formula (I) wherein each symbol is as defined in the specification, have a potent DPP-IV inhibitory activity, and completed the present invention by increasing the stability.

  本发明旨在提供具有治疗效果的化合物，其作用是通过DPP-IV的抑制作用，并且作为药物产品具有令人满意的效果。本发明人发现，在丙氨酸的γ位上引入取代基的衍生物具有强效的DPP-IV抑制活性，并通过增加稳定性完成了本发明。
• Novel heterocyclic substituted carbonyl derivatives and their use as dopamine D3 receptor
  申请人：Aventis Pharmaceutical Inc.

  公开号：US20040220173A1

  公开（公告）日：2004-11-04

  The invention relates to heterocyclic substituted carbonyl derivatives that display selective binding to dopamine D 3 receptors. In another aspect, the invention relates to a method for treating central nervous system disorders associated with the dopamine D 3 receptor activity in a patient in need of such treatment comprising administering to the subject a therapeutically effective amount of said compounds for alleviation of such disorder. The central nervous system disorders that may be treated with these compounds include Psychotic Disorders, Substance Dependence, Substance Abuse, Dyskinetic Disorders (e.g. Parkinson's Disease, Parkinsonism, Neuroleptic-Induced Tardive Dyskinesia, Gilles de la Tourette Syndrome and Huntington's Disease), Dementia, Anxiety Disorders, Sleep Disorders, Circadian Rhythm Disorders and Mood Disorders. The subject invention is also directed towards processes for the preparation of the compounds described herein as well as methods for making and using the compounds as imaging agents for dopamine D 3 receptors.

  本发明涉及杂环取代羰基衍生物，该衍生物显示出对多巴胺D3受体的选择性结合。在另一个方面，本发明涉及一种治疗与多巴胺D3受体活性相关的中枢神经系统疾病的方法，该方法包括向需要此类治疗的患者给予所述化合物的治疗有效量以缓解此类疾病。这些化合物可以治疗的中枢神经系统疾病包括精神病性障碍、物质依赖、物质滥用、运动障碍（例如帕金森病、帕金森综合症、神经阻滞剂引起的迟发性运动障碍、吉尔·德·拉·图雷特综合症和亨廷顿病）、痴呆、焦虑症、睡眠障碍、昼夜节律紊乱和情绪障碍。本发明还涉及制备上述化合物的过程以及将其作为多巴胺D3受体成像剂的方法。
• Proline derivatives and the use thereof as drugs
  申请人：——

  公开号：US20040106655A1

  公开（公告）日：2004-06-03

  The present invention aims at providing compounds having therapeutic effects due to a DPP-IV inhibitory action, and satisfactory as pharmaceutical products. The present inventors have found that derivatives having a substituent introduced into the &ggr;-position of proline represented by the formula (I) 1 wherein each symbol is as defined in the specification, have a potent DPP-IV inhibitory activity, and completed the present invention by increasing the stability.

  本发明旨在提供具有治疗作用的化合物，由于DPP-IV抑制作用而具有满意的药物产品。本发明人发现，具有引入取代基的脯氨酸γ-位置的衍生物，其化学式为(I)1，其中每个符号如规范中所定义，具有强效的DPP-IV抑制活性，并通过增加稳定性完成了本发明。