5-Methoxy-2-methyl-4-(1,2,3,6-tetrahydro-4-pyridinyl)pyrimidine

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: 5-Methoxy-2-methyl-4-(1,2,3,6-tetrahydro-4-pyridinyl)pyrimidine
• 英文别名: 5-methoxy-2-methyl-4-(1,2,3,6-tetrahydropyridin-4-yl)pyrimidine
• 化学式: C₁₁H₁₅N₃O
• 分子量: 205.26
• InChiKey: XUNRJGPWAABQCL-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.4
• 重原子数：
  15
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.45
• 拓扑面积：
  47
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  5-Methoxy-2-methyl-4-(1,2,3,6-tetrahydro-4-pyridinyl)pyrimidine 、 氢气 在 钯 氢气 作用下， 以 甲醇 为溶剂， 25.0~40.0 ℃ 、266.64 MPa 条件下， 反应 6.0h， 以yielding 5-methoxy-2-methyl-4-(piperidin-4-yl)pyrimidine, Intermediate 11 (207 mg, 62%)的产率得到5-Methoxy-2-methyl-4-(4-piperidinyl)pyrimidine
  参考文献：
  名称：

  PIPERIDIN-1 -YL AND AZEPIN-1 -YL CARBOXYLATES AS MUSCARINIC M4 RECEPTOR AGONISTS

  摘要：

  本发明提供公式（I）及其药学上可接受的盐的毛果碱M4受体激动剂，其中m，n，p，q，R，R2和R3如规范中所定义，其制备过程，含有它们的药物组合物以及它们在治疗诸如精神分裂症，阿尔茨海默病和各种认知障碍以及治疗或缓解疼痛方面的用途。

  公开号：

  US20150376179A1

文献信息

• [EN] PIPERIDIN-1 -YL AND AZEPIN-1 -YL CARBOXYLATES AS MUSCARINIC M4 RECEPTOR AGONISTS<br/>[FR] CARBOXYLATES DE PIPÉRIDIN-1-YLE ET D'AZÉPIN-1-YLE À TITRE D'AGONISTES DU RÉCEPTEUR MUSCARINIQUE M4
  申请人：TAKEDA PHARMACEUTICAL

  公开号：WO2014122474A1

  公开（公告）日：2014-08-14

  The present invention provides muscarinic M4 receptor agonists of formula (I) and pharmaceutically acceptable salts thereof, wherein m, n, p, q, R, R2 and R3 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases such as schizophrenia, Alzheimer's disease and various cognitive disorders as well as in the treatment or alleviation of pain.

  本发明提供了式（I）的肌氨酸M4受体激动剂及其药用盐，其中m、n、p、q、R、R2和R3如规范中所定义，其制备方法，含有它们的药物组合物以及它们在治疗精神分裂症、阿尔茨海默病和各种认知障碍以及治疗或缓解疼痛中的用途。
• Piperidin-1-yl and azepin-1-yl carboxylates as muscarinic M4 receptor agonists
  申请人：Heptares Therapeutics Limited

  公开号：US10030012B2

  公开（公告）日：2018-07-24

  The present invention provides muscarinic M4 receptor agonists of formula (I) and pharmaceutically acceptable salts thereof, wherein m, n, p, q, R, R2 and R3 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases such as schizophrenia, Alzheimer's disease and various cognitive disorders as well as in the treatment or alleviation of pain.

  本发明提供了式 (I) 的毒蕈碱类 M4 受体激动剂及其药学上可接受的盐（其中 m、n、p、q、R、R2 和 R3 如说明书中所定义）、其制备工艺、含有它们的药物组合物以及它们在治疗诸如精神分裂症、阿尔茨海默病和各种认知障碍等疾病以及治疗或减轻疼痛中的用途。
• PIPERIDIN-1-YL AND AZEPIN-1-YL CARBOXYLATES AS MUSCARINIC M4 RECEPTOR AGONISTS
  申请人：Heptares Therapeutics Limited

  公开号：EP2953940B1

  公开（公告）日：2018-08-22
• US9593106B2
  申请人：——

  公开号：US9593106B2

  公开（公告）日：2017-03-14
• PIPERIDIN-1 -YL AND AZEPIN-1 -YL CARBOXYLATES AS MUSCARINIC M4 RECEPTOR AGONISTS
  申请人：TAKEDA PHARMACEUTICAL COMPANY LIMITED

  公开号：US20150376179A1

  公开（公告）日：2015-12-31

  The present invention provides muscarinic M4 receptor agonists of formula (I) and pharmaceutically acceptable salts thereof, wherein m, n, p, q, R, R 2 and R 3 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases such as schizophrenia, Alzheimer's disease and various cognitive disorders as well as in the treatment or alleviation of pain.

  本发明提供公式（I）及其药学上可接受的盐的毛果碱M4受体激动剂，其中m，n，p，q，R，R2和R3如规范中所定义，其制备过程，含有它们的药物组合物以及它们在治疗诸如精神分裂症，阿尔茨海默病和各种认知障碍以及治疗或缓解疼痛方面的用途。