2-(3-噻吩基甲基)-4,5-二氢-1H-咪唑 | 371122-32-6

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 亚胺内酰胺
• 中文名称: 2-(3-噻吩基甲基)-4,5-二氢-1H-咪唑
• 中文别名: 1,1-环丙烷二甲醇环硫酸酯
• 英文名称: 2-(3-thienyl)methyl-2-imidazoline
• 英文别名: 2-thiophen-3-ylmethyl-4,5-dihydro-1H-imidazole；2-(thiophen-3-ylmethyl)-4,5-dihydro-1H-imidazole
• CAS: 371122-32-6
• 化学式: C₈H₁₀N₂S
• 分子量: 166.247
• InChiKey: PFVPBXOWHUIDBN-UHFFFAOYSA-N

物化性质

• 沸点：
  353.6±25.0 °C(Predicted)
• 密度：
  1.29±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  0.5
• 重原子数：
  11
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  52.6
• 氢给体数：
  1
• 氢受体数：
  2

文献信息

• Method for the treatment of CNS disorders with substituted 2-imidazoles or imidazole derivatives
  申请人：Galley Guido

  公开号：US20070197621A1

  公开（公告）日：2007-08-23

  The present invention relates a method for treating depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder, stress-related disorders, psychotic disorders such as schizophrenia, neurological diseases such as Parkinson's disease, neurodegenerative disorders such as Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse and metabolic disorders such as eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders which comprises administering to an individual a therapeutically effective amount of a compound of formula I wherein R, R 1 , R 2 , A and n are as defined in the specification and to their pharmaceutically active salts. The invention also relates to novel compounds of formula I, pharmaceutical compositions containing them, and methods for their preparation.

  本发明涉及一种治疗抑郁症、焦虑症、双相情感障碍、注意力缺陷多动障碍、压力相关障碍、精神分裂症等精神障碍、帕金森病等神经系统疾病、阿尔茨海默病等神经退行性疾病、癫痫、偏头痛、高血压、物质滥用、进食障碍、糖尿病、糖尿病并发症、肥胖症、血脂异常、能量消耗和吸收障碍、体温稳态障碍、睡眠和昼夜节律障碍以及心血管疾病的方法，包括向个体施用化合物I的治疗有效量，其中R、R1、R2、A和n如规范中所定义，以及其药用活性盐。该发明还涉及化合物I的新颖化合物、含有它们的药物组合物以及它们的制备方法。
• Cyclic amidine compounds
  申请人：——

  公开号：US20030100769A1

  公开（公告）日：2003-05-29

  There is provided cyclic amidine compounds of the following formula (I): 1 wherein: A 1 and A 2 are hydrogen atom, optionally substituted alkyl group; optionally substituted aryl group; or optionally substituted heterocyclic group; and X is —C(R 1 ,R 2 )—C(R 3 ,R 4 )—, —C(R 5 )═C(R 6 )—, —C(R 7 ,R 8 )—C(R 9 ,R 10 )—C(R 11 ,R 12 )—, or —C(R 13 ,R 14 )—C(R 15 ,R 16 )—NH— (wherein, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , R 9 , R 10 , R 11 , R 12 , R 13 , R 14 , R 15 and R 16 are hydrogen atom; halogen atom; optionally substituted alkyl group; optionally substituted aryl group; or optionally substituted heterocyclic group; or pharmaceutically acceptable salts thereof. These compounds have good affinity for &agr;4&bgr;2 nicotinic acetylcholine receptors and activate the same to thereby exert a preventive or therapeutic effect on cerebral dysfunction.

  提供了以下式子（I）的环状腙类化合物：1其中：A1和A2为氢原子，可选取代烷基，可选取代芳基或可选取代杂环基；X为—C（R1，R2）—C（R3，R4）—，—C（R5）═C（R6）—，—C（R7，R8）—C（R9，R10）—C（R11，R12）—或—C（R13，R14）—C（R15，R16）—NH—（其中，R1、R2、R3、R4、R5、R6、R7、R8、R9、R10、R11、R12、R13、R14、R15和R16为氢原子，卤素原子，可选取代烷基，可选取代芳基或可选取代杂环基）或其药学上可接受的盐。这些化合物对α4β2型尼古丁乙酰胆碱受体具有良好的亲和力，并激活该受体，从而对脑功能障碍产生预防或治疗作用。
• CYCLIC AMIDINE COMPOUNDS AND THEIR USE AS ALPHA4BETA2 NICOTINIC ACETYLCHOLINE RECEPTOR LIGANDS
  申请人：SUNTORY LIMITED

  公开号：EP1280793A2

  公开（公告）日：2003-02-05
• EP1981497A2
  申请人：——

  公开号：EP1981497A2

  公开（公告）日：2008-10-22
• US7875645B2
  申请人：——

  公开号：US7875645B2

  公开（公告）日：2011-01-25