2-[4-(1-Methyl)piperidinyl]benzothiazole | 51784-78-2

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并噻唑类
• 英文名称: 2-[4-(1-Methyl)piperidinyl]benzothiazole
• 英文别名: 2-(1-methyl-piperidin-4-yl)-benzothiazole；2-(1-Methylpiperidin-4-yl)benzothiazole；2-(1-methylpiperidin-4-yl)-1,3-benzothiazole
• CAS: 51784-78-2
• 化学式: C₁₃H₁₆N₂S
• 分子量: 232.349
• InChiKey: YZNCDFPIYXQYLF-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3
• 重原子数：
  16
• 可旋转键数：
  1
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.46
• 拓扑面积：
  44.4
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  2-(吡啶-4-基)苯并[d]噻唑 在 platinum(IV) oxide sodium tetrahydroborate 、 氢气 作用下， 以 乙醇 、 丙酮 为溶剂， 生成 2-[4-(1-Methyl)piperidinyl]benzothiazole
  参考文献：
  名称：

  Pyridinium salts

  摘要：

  DOI：

  10.1007/bf00475918

文献信息

• Non-Imidazole Histamine H3 Ligands, Part 2: New 2-Substituted Benzothiazoles as Histamine H3 Antagonists
  作者：Krzysztof Walczynski、Roman Guryn、Obbe P. Zuiderveld、Henk Timmerman

  DOI：10.1002/(sici)1521-4184(199911)332:11<389::aid-ardp389>3.0.co;2-u

  日期：1999.11

  New, non‐imidazole histamine H3 receptor antagonists were prepared and in vitro tested as H3 receptor antagonists measured as the electrically evoked contraction of the guinea‐pig jejunum. The 2‐(1‐piperidinyl)‐ and 2‐(1‐pyrrolidinyl)benzothiazoles show no or very poor activity; 2‐[1‐(4‐amino)piperidinyl]‐ and 2‐(1,2‐ethanediamino)‐ and 2‐(1,3‐propanediamino)derivatives of benzothiazole possess weak

  制备了新的非咪唑组胺 H3 受体拮抗剂，并作为 H3 受体拮抗剂进行了体外测试，测量结果为豚鼠空肠的电诱发收缩。2- (1-哌啶基) - 和 2- (1- 吡咯烷基) 苯并噻唑没有活性或活性很差；苯并噻唑的 2- [1- (4- 氨基) 哌啶基] - 和 2- (1,2- 乙二氨基) - 和 2- (1,3- 丙二氨基) 衍生物对 H3 受体具有弱活性，而 2- (4-哌啶基) 苯并噻唑和 2-[1- (4-哌嗪基)] 苯并噻唑表现出中等至良好的活性。亲脂性且不太笨重的替代品，如与哌嗪或哌啶环上的氮相连的正丙基，可产生有效的 H3 受体拮抗剂，其 pA2 值范围为 7.0 至 7.2。讨论了不同取代模式的构效关系。
• Novel Heterocyclic Substituted Carbonyl Derivatives and Their Use as Dopamine D3 Receptor Ligands
  申请人：Hendrix James A.

  公开号：US20090247509A1

  公开（公告）日：2009-10-01

  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，其表现出对多巴胺D3受体的选择性结合。另一方面，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、吉尔斯-德-拉-图雷综合症和亨廷顿病）、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方法以及将所述化合物作为多巴胺D3受体成像剂的制备和使用方法。
• Novel heterocyclic substituted carbonyl derivatives and their use as dopamine D3 receptor ligands
  申请人：Hendrix A. James

  公开号：US20070161641A1

  公开（公告）日：2007-07-12

  The invention relates to heterocyclic substituted carbonyl derivatives that display selective binding to dopamine D 3 receptors. In another aspect, the invention relates is 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，其具有选择性地与多巴胺D3受体结合。另一方面，本发明涉及一种治疗中枢神经系统疾病的方法，该疾病与多巴胺D3受体活性有关，包括对患者进行治疗，向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。本发明还涉及所述化合物的制备过程，以及将所述化合物作为多巴胺D3受体成像剂的制备和使用方法。
• Proline derivatives and use thereof as drugs
  申请人：Mitsubishi Tanabe Pharma Corporation

  公开号：EP1930319A1

  公开（公告）日：2008-06-11

  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.

  本发明旨在提供因具有 DPP-IV 抑制作用而具有治疗效果的化合物，并提供令人满意的药物产品。 本发明者发现，在式 (I) 所代表的脯氨酸的 γ 位上引入取代基的衍生物 其中各符号如说明书中所定义，具有强效的 DPP-IV 抑制活性，并通过提高稳定性完成了本发明。
• Heterocyclic substituted carbonyl derivatives and their use as dopamine D3 receptor ligands
  申请人：Aventis Pharmaceuticals Inc.

  公开号：EP1935887A1

  公开（公告）日：2008-06-25

  The invention relates to heterocyclic substituted carbonyl derivatives of the formula I that display selective binding to dopamine D3 receptors and are useful 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 D3 receptors.

  本发明涉及式 I 的杂环取代的羰基衍生物 本发明涉及式 I 的杂环取代羰基衍生物，该衍生物与多巴胺 D3 受体具有选择性结合，可用于治疗需要此类治疗的患者中与多巴胺 D3 受体活性相关的中枢神经系统紊乱，包括向受试者施用治疗有效量的所述化合物以缓解此类紊乱。可用这些化合物治疗的中枢神经系统疾病包括精神障碍、药物依赖、药物滥用、运动障碍（如帕金森病、帕金森氏症、神经抑制剂诱发的迟发性运动障碍、吉勒-德拉图雷特综合征和亨廷顿氏病）、痴呆、焦虑症、睡眠障碍、昼夜节律紊乱和情绪障碍。本发明还涉及本文所述化合物的制备过程以及将这些化合物用作多巴胺 D3 受体成像剂的制备和使用方法。