Sarizotan dihydrochloride | 177976-12-4

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶及其衍生物
• 英文名称: Sarizotan dihydrochloride
• 英文别名: 1-[(2R)-3,4-dihydro-2H-chromen-2-yl]-N-[[5-(4-fluorophenyl)pyridin-3-yl]methyl]methanamine;dihydrochloride
• CAS: 177976-12-4
• 化学式: C22H23Cl2FN2O
• 分子量: 421.3
• InChiKey: ANXOJXYTTDGHAJ-GHVWMZMZSA-N

物化性质

• 熔点：
  234-235°
• 比旋光度：
  20 -65° (c = 1 in methanol)

计算性质

• 辛醇/水分配系数(LogP)：
  5.21
• 重原子数：
  28
• 可旋转键数：
  5
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.23
• 拓扑面积：
  34.2
• 氢给体数：
  3
• 氢受体数：
  4

文献信息

• Method for producing-2[-5-(4-fluorophenyl)-3-pyridylmethylaminomethyl]-chromane
  申请人：——

  公开号：US20040138266A1

  公开（公告）日：2004-07-15

  The present invention relates to a process for the preparation of 2-[5-(4-fluorophenyl)-3-pyridylmethylaminomethyl]chroman, the enantiomers and its salts, characterised in that 5-(4-fluorophenyl)pyridine-3-carbaldehyde is reacted directly with aminomethylchroman or its salts under reducing conditions to give 2-[5-(4-fluorophenyl)-3-pyridylmethylaminomethyl]chroman, and the latter is, if desired, converted into one of its physiologically acceptable salts by treatment with an acid.

  本发明涉及一种制备2 - [5-（4-氟苯基）-3-吡啶甲基氨甲基] 色满及其对映体和其盐的方法，其特征在于，5-（4-氟苯基）吡啶-3-甲醛在还原条件下直接与氨甲基色满或其盐反应，得到2 - [5-（4-氟苯基）-3-吡啶甲基氨甲基] 色满，如有需要，可以通过酸处理将其转化为其生理上可接受的盐之一。
• AGENT FOR IMPROVING MOTOR COMPLICATIONS OR PSYCHIATRIC SYMPTOMS IN PARKINSON'S DISEASE
  申请人：Asubio Pharma Co., Ltd.

  公开号：EP2213290A1

  公开（公告）日：2010-08-04

  A drug containing a compound having the formula (I): or a pharmacologically acceptable salt thereof or their hydrates, which alleviates motor complications associated with a treatment with levodopa for Parkinson's disease, delays the onset of motor complications associated with a treatment with levodopa, and inhibiting or delaying the advance of symptoms of Parkinson's disease is provided. The compound having the formula (I) has a serotonin 1A receptor partial agonist action, does not have an antagonist action against dopamine D2 receptors, has an agonist action against dopamine D3 receptors, has an effect of alleviation and delay of onset of motor complications associated with repeated doses of levodopa and, further, is also effective against associated with psychiatric symptoms in advanced stage Parkinson's disease patients.

  一种含有式(I)化合物的药物： 或其药理学上可接受的盐或它们的水合物的药物，该药物可减轻与左旋多巴治疗帕金森病相关的运动并发症，延缓与左旋多巴治疗相关的运动并发症的发生，抑制或延缓帕金森病症状的发展。具有式（I）的化合物具有5-羟色胺1A受体部分激动作用，对多巴胺D2受体无拮抗作用，对多巴胺D3受体有激动作用，具有缓解和延迟与重复剂量左旋多巴治疗相关的运动并发症发作的作用，此外，还对晚期帕金森病患者的相关精神症状有效。
• VERFAHREN ZUR HERSTELLUNG VON 2- -5-(4-FLUORPHENYL)-3-PYRIDYLMETHYLAMINOMETHYL -CHROMANE
  申请人：Merck Patent GmbH

  公开号：EP1383763A2

  公开（公告）日：2004-01-28
• VERFAHREN ZUR HERSTELLUNG VON 2-(-5-(4-FLUORPHENYL)-3-PYRIDYLMETHYLAMINOMETHYL)-CHROMAN
  申请人：Merck Patent GmbH

  公开号：EP1383763B1

  公开（公告）日：2005-10-12
• DRUG FOR ALLEVIATING MOTOR COMPLICATIONS OR PSYCHIATRIC SYMPTOMS OF PARKINSON'S DISEASE
  申请人：Tani Yoshihiro

  公开号：US20100204202A1

  公开（公告）日：2010-08-12

  A drug containing a compound having the formula (I): or a pharmacologically acceptable salt thereof or their hydrates, which alleviates motor complications associated with a treatment with levodopa for Parkinson's disease, delays the onset of motor complications associated with a treatment with levodopa, and inhibiting or delaying the advance of symptoms of Parkinson's disease is provided. The compound having the formula (I) has a serotonin 1A receptor partial agonist action, does not have an antagonist action against dopamine D2 receptors, has an agonist action against dopamine D3 receptors, has an effect of alleviation and delay of onset of motor complications associated with repeated doses of levodopa and, further, is also effective against associated with psychiatric symptoms in advanced stage Parkinson's disease patients.