4-ethyl-5-(1H-pyrazol-4-yl)pyrimidin-2-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: 4-ethyl-5-(1H-pyrazol-4-yl)pyrimidin-2-amine
• 化学式: C₉H₁₁N₅
• 分子量: 189.22
• InChiKey: VJFRKCFQFZUSID-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.6
• 重原子数：
  14
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.22
• 拓扑面积：
  80.5
• 氢给体数：
  2
• 氢受体数：
  4

文献信息

• 3-PYRIMIDIN-4-YL-OXAZOLIDIN-2-ONES AS INHIBITORS OF MUTANT IDH
  申请人：NOVARTIS AG

  公开号：US20150152093A1

  公开（公告）日：2015-06-04

  The invention is directed to a formula (I): or a pharmaceutically acceptable salt thereof, wherein R 1 , R 2a , R 2b and R 3 -R 7 are herein. The invention is also directed to compositions containing a compound of formula (I) and to the use of such compounds in the inhibition of mutant IDH proteins having a neomorphic activity. The invention is further directed to the use of a compound of formula (I) in the treatment of diseases or disorders associated with such mutant IDH proteins including, but not limited to, cell-proliferation disorders, such as cancer.

  该发明涉及一种公式(I)或其药学上可接受的盐，其中R1、R2a、R2b和R3-R7如下。该发明还涉及含有公式(I)化合物的组合物，并且涉及使用这些化合物来抑制具有新型活性的突变IDH蛋白质。该发明进一步涉及使用公式(I)化合物来治疗与这种突变IDH蛋白质相关的疾病或障碍，包括但不限于细胞增殖障碍，如癌症。
• 3-pyrimidin-4-yl-oxazolidin-2-ones as inhibitors of mutant IDH
  申请人：NOVARTIS AG

  公开号：US10112931B2

  公开（公告）日：2018-10-30

  The invention is directed to a formula (I): or a pharmaceutically acceptable salt thereof, wherein R1, R2a, R2b and R3-R7 are herein. The invention is also directed to compositions containing a compound of formula (I) and to the use of such compounds in the inhibition of mutant IDH proteins having a neomorphic activity. The invention is further directed to the use of a compound of formula (I) in the treatment of diseases or disorders associated with such mutant IDH proteins including, but not limited to, cell-proliferation disorders, such as cancer.

  本发明涉及式 (I)： 或其药学上可接受的盐，其中 R1、R2a、R2b 和 R3-R7 在此处。本发明还涉及含有式（I）化合物的组合物，以及此类化合物在抑制具有新变态活性的突变 IDH 蛋白中的用途。本发明进一步涉及式（I）化合物在治疗与此类突变IDH蛋白相关的疾病或紊乱中的用途，包括但不限于细胞增殖紊乱，如癌症。
• US20140275083A1
  申请人：——

  公开号：US20140275083A1

  公开（公告）日：2014-09-18