4,6-二氨基-2-甲基-5-嘧啶甲腈 | 76587-28-5

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪类
• 中文名称: 4,6-二氨基-2-甲基-5-嘧啶甲腈
• 英文名称: 4,6-diamino-2-methyl-pyrimidine-5-carbonitrile
• 英文别名: 4,6-Diamino-2-methyl-pyrimidin-5-carbonitril；4,6-Diamino-2-methyl-5-cyan-pyrimidin；4,6-Diamino-2-methylpyrimidine-5-carbonitrile
• CAS: 76587-28-5
• 化学式: C₆H₇N₅
• mdl: MFCD07760828
• 分子量: 149.155
• InChiKey: AOOIPJVCCZPHBP-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.2
• 重原子数：
  11
• 可旋转键数：
  0
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.166
• 拓扑面积：
  102
• 氢给体数：
  2
• 氢受体数：
  5

安全信息

• 海关编码：
  2933599090

反应信息

• 作为反应物：
  描述：

  4,6-二氨基-2-甲基-5-嘧啶甲腈 在 镍 甲酸 、 氢气 、 sodium ethanolate 作用下， 以 乙醇 为溶剂， 25.0 ℃ 、344.73 kPa 条件下， 反应 10.0h， 生成 6-(2,6-Dichlorophenyl)-2-methylpyrido[2,3-d]pyrimidine-4,7-diamine
  参考文献：
  名称：

  Antihypertensive activity of 6-arylpyrido[2,3-d]pyrimidin-7-amine derivatives

  摘要：

  A series of 51 6-arylpyrido[2,3-d]pyrimidin-7-amine derivatives was prepared and evaluated for antihypertensive activity in the conscious spontaneously hypertensive rat. A number of these compounds, notably 6-(2,6-dichlorophenyl)-2-methylpyrido[2,3-d]pyrimidin-7-amine (36), lowered blood pressure in these rats in a gradual and sustained manner to normotensive levels at oral doses of 10-50 mg/kg. Normalized blood pressure levels could then be maintained by single daily oral doses. The effect of structural variation in the 6-aryl group and in the 2 and 4 positions of the pyridopyrimidine ring on activity is reported and discussed.

  DOI：

  10.1021/jm00136a006
• 作为产物：
  描述：

  4-hydroxy-2-methyl-6-oxo-1H-pyrimidine-5-carboxamide 在 氨 、 N,N-二甲基苯胺 、 三氯氧磷 作用下， 生成 4,6-二氨基-2-甲基-5-嘧啶甲腈
  参考文献：
  名称：

  Antihypertensive activity of 6-arylpyrido[2,3-d]pyrimidin-7-amine derivatives

  摘要：

  A series of 51 6-arylpyrido[2,3-d]pyrimidin-7-amine derivatives was prepared and evaluated for antihypertensive activity in the conscious spontaneously hypertensive rat. A number of these compounds, notably 6-(2,6-dichlorophenyl)-2-methylpyrido[2,3-d]pyrimidin-7-amine (36), lowered blood pressure in these rats in a gradual and sustained manner to normotensive levels at oral doses of 10-50 mg/kg. Normalized blood pressure levels could then be maintained by single daily oral doses. The effect of structural variation in the 6-aryl group and in the 2 and 4 positions of the pyridopyrimidine ring on activity is reported and discussed.

  DOI：

  10.1021/jm00136a006

文献信息

• NOVEL COMPOUNDS AS MODULATORS OF PROTEIN KINASES
  申请人：Rhizen Pharmaceuticals SA

  公开号：US20150320752A1

  公开（公告）日：2015-11-12

  The present invention provides PI3K protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of kinase mediated diseases or disorders with them.

  本发明提供PI3K蛋白激酶调节剂，制备方法，含有它们的制药组合物以及使用它们治疗、预防和/或改善激酶介导的疾病或障碍的方法。
• Substituted chromenones as modulators of protein kinases
  申请人：Rhizen Pharmaceuticals SA

  公开号：US10322130B2

  公开（公告）日：2019-06-18

  The present invention provides PI3K protein kinase modulators of formula wherein R, Cy1, R1, R2, L1 and Cy2 are as defined herein. The present invention also relates to methods of preparing compounds of formula (I) to pharmaceutical compositions containing them and to methods of treatment, prevention and/or amelioration of kinase mediated diseases or disorders with them.

  本发明提供式 PI3K 蛋白激酶调节剂，其中 R、Cy1、R1、R2、L1 和 Cy2 如本文所定义。 本发明还涉及制备式（I）化合物的方法、含有式（I）化合物的药物组合物以及用式（I）化合物治疗、预防和/或改善激酶介导的疾病或紊乱的方法。
• Budesinsky; Kopecky, Collection of Czechoslovak Chemical Communications, 1955, vol. 20, p. 52,56
  作者：Budesinsky、Kopecky

  DOI：——

  日期：——
• SUBSTITUTED CHROMENONES AS MODULATORS OF PROTEIN KINASES
  申请人：Rhizen Pharmaceuticals SA

  公开号：US20190105324A9

  公开（公告）日：2019-04-11

  The present invention provides PI3K protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of kinase mediated diseases or disorders with them.
• Antihypertensive activity of 6-arylpyrido[2,3-d]pyrimidin-7-amine derivatives
  作者：Lawrence R. Bennett、C. John Blankley、Robert W. Fleming、Ronald D. Smith、Deirdre K. Tessman

  DOI：10.1021/jm00136a006

  日期：1981.4

  A series of 51 6-arylpyrido[2,3-d]pyrimidin-7-amine derivatives was prepared and evaluated for antihypertensive activity in the conscious spontaneously hypertensive rat. A number of these compounds, notably 6-(2,6-dichlorophenyl)-2-methylpyrido[2,3-d]pyrimidin-7-amine (36), lowered blood pressure in these rats in a gradual and sustained manner to normotensive levels at oral doses of 10-50 mg/kg. Normalized blood pressure levels could then be maintained by single daily oral doses. The effect of structural variation in the 6-aryl group and in the 2 and 4 positions of the pyridopyrimidine ring on activity is reported and discussed.