Methanesulfonic acid;2-(4-methylpiperazin-1-yl)-5-(2,3,5-trichlorophenyl)pyrimidin-4-amine

• 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: Methanesulfonic acid;2-(4-methylpiperazin-1-yl)-5-(2,3,5-trichlorophenyl)pyrimidin-4-amine
• 化学式: C16H20Cl3N5O3S
• 分子量: 468.8
• InChiKey: VQSWASDOWDBMFJ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.94
• 重原子数：
  28
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  121
• 氢给体数：
  2
• 氢受体数：
  8

文献信息

• Substituted phenylpyrimidine derivatives, useful in the treatment of prevention of CNS disorders
  申请人：THE WELLCOME FOUNDATION LIMITED

  公开号：EP0715851A2

  公开（公告）日：1996-06-12

  A class of substituted phenylpyrimidine compounds are disclosed which are potent inhibitors of the excitatory amino acid, glutamate. Such compounds are useful in the treatment or prevention of a range of CNS disorders including cerebral ischaemic damage and epilepsy.

  本研究公开了一类取代苯基嘧啶化合物，它们是兴奋性氨基酸谷氨酸的强效抑制剂。 此类化合物可用于治疗或预防一系列中枢神经系统疾病，包括脑缺血损伤和癫痫。
• Substituted phenylpyrimidine derivatives, useful in the treatment or prevention of CNS disorders
  申请人：THE WELLCOME FOUNDATION LIMITED

  公开号：EP0713703A2

  公开（公告）日：1996-05-29

  A class of substituted phenylpyrimidine compounds are disclosed which are potent inhibitors of the excitatory amino acid, glutamate. Such compounds are useful in the treatment or prevention of a range of CNS disorders including cerebral ischaemic damage and epilepsy.

  本研究公开了一类取代苯基嘧啶化合物，它们是兴奋性氨基酸谷氨酸的强效抑制剂。此类化合物可用于治疗或预防一系列中枢神经系统疾病，包括脑缺血损伤和癫痫。
• Piperazinyl-substituted phenyl pyrimidine derivatives useful in the treatment or prevention of disorders of the central nervous system
  申请人：THE WELLCOME FOUNDATION LIMITED

  公开号：EP1325916A1

  公开（公告）日：2003-07-09

  A class of substituted phenylpyrimidine compounds are disclosed which are potent inhibitors of the excitatory amino acid, glutamate. Such compounds are useful in the treatment or prevention of a range of CNS disorders including cerebral ischaemic damage and epilepsy. wherein: R1 is piperazinyl; R2 is amino; R3 is hydrogen, C1-C6 alkyl, trifluoromethyl, C1-C6 alkoxy, C1-C6 alkylthio, (C1-C6 alkyl)thio(C1-C6 alkyl), di[(C1-C6 alkyl)oxy] (C1-C6 alkyl), or CH2X wherein X is C1-C6 alkoxy, phenoxy or benzyloxy; each of R4, R5, R7 and R8 is the same or different and is selected from hydrogen and halo, or R4 and R5 together denote -CH=CH-CH=CH- in which case both R7 and R8 are hydrogen; R6 is hydrogen, halo, nitro or amino; and pharmaceutically acceptable acid addition salts thereof.

  本研究公开了一类取代苯基嘧啶化合物，它们是兴奋性氨基酸谷氨酸的强效抑制剂。此类化合物可用于治疗或预防一系列中枢神经系统疾病，包括脑缺血损伤和癫痫。 其中 R1 是哌嗪基 R2 是氨基 R3 是氢、C1-C6 烷基、三氟甲基、C1-C6 烷氧基、C1-C6 烷硫基、(C1-C6 烷基)硫(C1-C6 烷基)、二[(C1-C6 烷基)氧基](C1-C6 烷基)或 CH2X，其中 X 是 C1-C6 烷氧基、苯氧基或苄氧基； R4、R5、R7 和 R8 各自相同或不同，且选自氢和卤素，或 R4 和 R5 共同表示-CH=CH-CH=CH-，在这种情况下，R7 和 R8 都是氢； R6 是氢、卤素、硝基或氨基； 及其药学上可接受的酸加成盐。
• Pharmacologically active cns compounds
  申请人：THE WELLCOME FOUNDATION LIMITED

  公开号：EP1681058A2

  公开（公告）日：2006-07-19

  A class of substituted phenylpyrimidine compounds are disclosed which are potent inhibitors of the excitatory amino acid, glutamate. Such compounds are useful in the treatment or prevention of a range of CNS disorders including cerebral ischaemic damage and epilepsy.

  本研究公开了一类取代苯基嘧啶化合物，它们是兴奋性氨基酸谷氨酸的强效抑制剂。此类化合物可用于治疗或预防一系列中枢神经系统疾病，包括脑缺血损伤和癫痫。
• Pharmacologically active CNS compounds
  申请人：THE WELLCOME FOUNDATION LIMITED

  公开号：EP0372934B1

  公开（公告）日：1996-10-23