(1s,5s)-cyclooctane-1,5-diyl bis(4-methylbenzenesulfonate) | 6522-44-7

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: (1s,5s)-cyclooctane-1,5-diyl bis(4-methylbenzenesulfonate)
• 英文别名: cis-1,5-bis-(p-toluenesulfonyloxy)cyclooctane；cis-1,5-cyclooctanediol ditosylate；cis-Cyclooctan-1,5-diol-ditosylat
• CAS: 6522-44-7
• 化学式: C₂₂H₂₈O₆S₂
• 分子量: 452.593
• InChiKey: ZTCCFSKUCCLAPL-BGYRXZFFSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.51
• 重原子数：
  30.0
• 可旋转键数：
  6.0
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.45
• 拓扑面积：
  86.74
• 氢给体数：
  0.0
• 氢受体数：
  6.0

反应信息

• 作为反应物：
  描述：

  (1s,5s)-cyclooctane-1,5-diyl bis(4-methylbenzenesulfonate) 在 sodium azide 作用下， 以 二甲基亚砜 为溶剂， 生成
  参考文献：
  名称：

  cis-1,5-Diaminocyclooctane: the most basic gaseous primary amine?

  摘要：

  经测定，标题化合物的气相碱性大于腐胺，是迄今为止测得的碱性最强的原生二胺。

  DOI：

  10.1039/b305239g
• 作为产物：
  描述：

  cyclooctane-1,5-diol 、 对甲苯磺酰氯 在 吡啶 作用下， 反应 18.0h， 以68%的产率得到(1s,5s)-cyclooctane-1,5-diyl bis(4-methylbenzenesulfonate)
  参考文献：
  名称：

  Synthesis of New Chiral Amines, 2,6-Dimethyl-9-azabicyclo[3.3.1]nonane and Its Derivatives

  摘要：

  New chiral amines, 2,6-dimethyl-9-azabicyclo[3.3.1]nonane and its derivatives, were prepared starting from commercially available 1,5-dimethyl-1,5-cyclooctadiene followed by substitution reaction of the intermediate ditosylate with p-toluenesulfonamide under phase transfer conditions in 4 steps.

  DOI：

  10.3987/com-99-s71

文献信息

• Potassium channel blocking agents
  申请人：NeuroSearch A/S

  公开号：US20020049246A1

  公开（公告）日：2002-04-25

  This invention relates to novel potassium channel blocking agents, and their use in the preparation of pharmaceutical compositions. Moreover the invention is directed to pharmaceutical compositions useful for the treatment or alleviation of diseases or disorders associated with the activity of potassium channels, in particular asthma, cystic fibrosis, chronic obstructive pulmonary disease and rhinorrhea, convulsions, vascular spasms, coronary artery spasms, renal disorders, polycystic kidney disease, bladder spasms, urinary incontinence, bladder outflow obstruction, irritable bowel syndrome, gastrointestinal dysfunction, secretory diarrhoea, ischaemia, cerebral ischaemia, ischaemic hearth disease, angina pectoris, coronary hearth disease, traumatic brain injury, psychosis, anxiety, depression, dementia, memory and attention deficits, Alzheimer's disease, dysmenorrhea, narcolepsy, Reynaud's disease, intermittent claudication, Sjorgren's syndrome, migraine, arrhythmia, hypertension, absence seizures, myotonic muscle dystrophia, xerostomi, diabetes type II, hyperinsulinemia, premature labor, baldness, cancer, and immune suppression.

  本发明涉及新型钾通道阻滞剂及其在制备药物组合物中的应用。此外，本发明还涉及用于治疗或缓解与钾通道活性有关的疾病或疾病的药物组合物，特别是哮喘、囊性纤维化、慢性阻塞性肺疾病和流涕、惊厥、血管痉挛、冠状动脉痉挛、肾脏疾病、多囊肾病、膀胱痉挛、尿失禁、膀胱出流道梗阻、肠易激综合征、胃肠功能障碍、分泌性腹泻、缺血、脑缺血、缺血性心脏病、心绞痛、冠心病、创伤性脑损伤、精神病、焦虑、抑郁症、痴呆、记忆和注意力缺陷、阿尔茨海默病、痛经、嗜睡病、雷诺氏病、间歇性跛行、Sjorgren综合征、偏头痛、心律失常、高血压、失神发作、肌萎缩性肌肉营养不良、干口症、2型糖尿病、高胰岛素血症、早产、秃发、癌症和免疫抑制。
• Bis(benzimidazole) derivatives serving as potassium blocking agents
  申请人：Neurosearch A/S

  公开号：US06569880B2

  公开（公告）日：2003-05-27

  This invention relates to novel potassium channel blocking agents, and their use in the preparation of pharmaceutical compositions. Moreover the invention is directed to pharmaceutical compositions useful for the treatment or alleviation of diseases or disorders associated with the activity of potassium channels, in particular asthma, cystic fibrosis, chronic obstructive pulmonary disease and rhinorrhea, convulsions, vascular spasms, coronary artery spasms, renal disorders, polycystic kidney disease, bladder spasms, urinary incontinence, bladder outflow obstruction, irritable bowel syndrome, gastrointestinal dysfunction, secretory diarrhoea, ischaemia, cerebral ischaemia, ischaemic hearth disease, angina pectoris, coronary hearth disease, traumatic brain injury, psychosis, anxiety, depression, dementia, memory and attention deficits, Alzheimer's disease, dysmenorrhea, narcolepsy, Reynaud's disease, intermittent claudication, Sjorgren's syndrome, migraine, arrhythmia, hypertension, absence seizures, myotonic muscle dystrophia, xerostomi, diabetes type II, hyperinsulinemia, premature labor, baldness, cancer, and immune suppression.

  本发明涉及新型钾通道阻滞剂及其在制备药物组合物中的使用。此外，本发明针对与钾通道活动相关的疾病或障碍，特别是哮喘、囊性纤维化、慢性阻塞性肺疾病和流涕、惊厥、血管痉挛、冠状动脉痉挛、肾脏疾病、多囊肾病、膀胱痉挛、尿失禁、膀胱出口梗阻、肠易激综合征、胃肠功能障碍、分泌性腹泻、缺血、脑缺血、缺血性心脏病、心绞痛、冠心病、创伤性脑损伤、精神病、焦虑、抑郁、痴呆、记忆和注意力缺陷、阿尔茨海默病、痛经、嗜睡症、雷诺氏病、间歇性跛行、Sjorgren综合征、偏头痛、心律失常、高血压、失神发作、肌无力症、口干症、2型糖尿病、高胰岛素血症、早产、脱发、癌症和免疫抑制等疾病或障碍的治疗或缓解的药物组合物。
• Bis (benzimidazole) derivatives serving as potassium blocking agents
  申请人：Neurosearch A/S

  公开号：US06194447B1

  公开（公告）日：2001-02-27

  This invention relates to novel potassium channel blocking agents, and their use in the preparation of pharmaceutical compositions. Moreover the invention is directed to pharmaceutical compositions useful for the treatment or alleviation of diseases or disorders associated with the activity of potassium channels, in particular asthma, cystic fibrosis, chronic obstructive pulmonary disease and rhinorrhea, convulsions, vascular spasms, coronary artery spasms, renal disorders, polycystic kidney disease, bladder spasms, urinary incontinence, bladder outflow obstruction, irritable bowel syndrome, gastrointestinal dysfunction, secretory diarrhoea, ischaemia, cerebral ischaemia, ischaemic hearth disease, angina pectoris, coronary hearth disease, traumatic brain injury, psychosis, anxiety, depression, dementia, memory and attention deficits, Alzheimer's disease, dysmenorrhea, narcolepsy, Reynaud's disease, intermittent claudication, Sjorgren's syndrome, migraine, arrhythmia, hypertension, absence seizures, myotonic muscle dystrophia, xerostomi, diabetes type II, hyperinsulinemia, premature labor, baldness, cancer, and immune suppression.

  本发明涉及新型钾通道阻滞剂及其在制备制药组合物中的应用。此外，本发明针对与钾通道活动相关的疾病或疾病症状，特别是哮喘、囊性纤维化、慢性阻塞性肺病和鼻涕、抽搐、血管痉挛、冠状动脉痉挛、肾脏疾病、多囊肾病、膀胱痉挛、尿失禁、膀胱排出阻塞、肠易激综合症、胃肠功能障碍、分泌性腹泻、缺血、脑缺血、缺血性心脏病、心绞痛、冠心病、创伤性脑损伤、精神病、焦虑、抑郁、痴呆、记忆和注意力缺陷、阿尔茨海默病、痛经、嗜睡症、雷诺氏病、间歇性跛行、Sjorgren综合症、偏头痛、心律失常、高血压、失神发作、肌无力性肌萎缩症、干口症、2型糖尿病、高胰岛素血症、早产、脱发、癌症和免疫抑制等方面提供了有用的制药组合物。
• Bridged N-Bicyclic Sulfonamido Inhibitors of Gamma Secretase
  申请人：Konradi Andrei W.

  公开号：US20110178119A1

  公开（公告）日：2011-07-21

  The invention provides N-bicyclic sulfonamido compounds of Formula (I) wherein A is as described in the specification and R 1 and R 2 combine to form a [3.3.1] or a [3.2.1] ring system. Compounds of Formula I are useful in treating or preventing cognitive disorders, such as Alzheimer's Disease. The invention also encompasses pharmaceutical compositions comprising compounds of Formula (I) as well as methods of treating cognitive disorders, such as Alzheimer's disease.

  本发明提供了公式（I）的N-双环磺酰胺化合物，其中A如说明书所述，R1和R2结合形成[3.3.1]或[3.2.1]环系统。公式I的化合物在治疗或预防认知障碍，如阿尔茨海默病方面具有用途。本发明还包括含有公式（I）的药物组合物以及治疗认知障碍，如阿尔茨海默病的方法。
• Verbrugge,P.A. et al., Synthetic Communications, 1977, vol. 7, p. 1 - 11
  作者：Verbrugge,P.A. et al.

  DOI：——

  日期：——