4-Amino-2-(N-morpholino)-5-(3,5-dichlorophenyl)-6-methyl pyrimidine | 139256-32-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪类
• 英文名称: 4-Amino-2-(N-morpholino)-5-(3,5-dichlorophenyl)-6-methyl pyrimidine
• 英文别名: 5-(3,5-Dichlorophenyl)-6-methyl-2-morpholin-4-ylpyrimidin-4-amine
• CAS: 139256-32-9
• 化学式: C₁₅H₁₆Cl₂N₄O
• 分子量: 339.224
• InChiKey: XYAQXRWBALWEOU-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.2
• 重原子数：
  22
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  64.3
• 氢给体数：
  1
• 氢受体数：
  5

文献信息

• Pharmacologically active CNS compound
  申请人：THE WELLCOME FOUNDATION LIMITED

  公开号：EP0459819A2

  公开（公告）日：1991-12-04

  The invention provides a series of compounds of formula (I) and salts thereof, wherein for example, R¹ and R², which may be the same or different each represent -NR¹³R¹⁴ where R¹³ and R¹⁴ may each independently represent hydrogen or alkyl or, taken together with the nitrogen atom to which they are attached form a heterocyclic ring, optionally substituted by one or more alkyl or arylalkyl groups and optionally containing a further heteroatom; R³ is hydrogen, haloalkyl, alkoxymethyl or alkyl; R⁴ is hydrogen, nitro or halo; R⁵ is hydrogen or halo; R⁶ is hydrogen, halo, nitro, amino, alkylamino or dialkylamino; R⁷ is hydrogen or halo; R⁸ is hydrogen or halo; The compounds may be used for the treatment or prophylaxis of a neurodegenerative or other neurological disorder of the CNS, the aetiology or which includes excessive release of the neurotransmitter glutamate.

  本发明提供了一系列式 (I) 的化合物 及其盐类，其中例如 R¹和R²可以相同或不同，各自代表-NR¹³R¹⁴，其中R¹³和R¹⁴可以各自独立地代表氢或烷基，或与它们所连接的氮原子一起形成杂环，任选被一个或多个烷基或芳烷基取代，并任选含有另一个杂原子； R³ 是氢、卤代烷基、烷氧基甲基或烷基； R⁴ 是氢、硝基或卤代； R⁵ 是氢或卤素； R⁶ 是氢、卤素、硝基、氨基、烷基氨基或二烷基氨基； R⁷ 是氢或卤素； R⁸ 是氢或卤素； 这些化合物可用于治疗或预防中枢神经系统的神经退行性疾病或其他神经疾病，其病因或包括神经递质谷氨酸的过度释放。
• Pharmacologically active CNS pyridmidin compounds
  申请人：THE WELLCOME FOUNDATION LIMITED

  公开号：EP0679645A1

  公开（公告）日：1995-11-02

  A series of phenylpyrimidines and acid addition salts thereof are inhibitors of extracellular glutamate release. They have negligible effect against the enzyme dihydrofolate reductase. They are useful in the treatment or prophylaxis in a mammal of a neurodegenerative or other neurological disorder of the central nervous system, the aetiology of which includes excessive release of neurotransmitter glutamate.

  一系列苯基嘧啶及其酸加成盐是细胞外谷氨酸释放的抑制剂。 它们对二氢叶酸还原酶的作用微乎其微。 它们可用于治疗或预防哺乳动物中枢神经系统的神经退行性疾病或其他神经疾病，这些疾病的病因包括神经递质谷氨酸的过度释放。