5-amino-3-[5-[[2-(dimethylamino)ethyl-methylamino]methyl]-1H-indol-2-yl]-1H-pyridin-2-one

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吲哚及其衍生物
• 英文名称: 5-amino-3-[5-[[2-(dimethylamino)ethyl-methylamino]methyl]-1H-indol-2-yl]-1H-pyridin-2-one
• 化学式: C₁₉H₂₅N₅O
• 分子量: 339.4
• InChiKey: SCDWHZPXEWBFRL-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.9
• 重原子数：
  25
• 可旋转键数：
  6
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.32
• 拓扑面积：
  77.4
• 氢给体数：
  3
• 氢受体数：
  4

文献信息

• Indolyl-pyridone derivatives having checkpoint kinase 1 inhibitory activity
  申请人：Vernalis (R&D) Ltd.

  公开号：US10696652B2

  公开（公告）日：2020-06-30

  A method of treating a mammal suffering from a cancer responsive to inhibition of protein kinase activity, by administering to the mammal an amount of a compound of formula (I), or a pharmaceutically acceptable salt thereof, effective to inhibit protein kinase activity, wherein the compound of formula (I) is:

  一种治疗患有对蛋白激酶活性抑制有反应的癌症的哺乳动物的方法，向该哺乳动物施用一定量的式(I)化合物或其药学上可接受的盐，以有效抑制蛋白激酶活性，其中式(I)化合物是：
• INDOLYL-PYRIDONE DERIVATIVES HAVING CHECKPOINT KINASE 1 INHIBITORY ACTIVITY
  申请人：Vernalis (R&D) Ltd.

  公开号：EP2294065B1

  公开（公告）日：2014-03-19
• Indolyl-Pyridone Derivatives Having Checkpoint Kinase 1 Inhibitory Activity
  申请人：Vernalis (R&D) Ltd.

  公开号：US20170298043A1

  公开（公告）日：2017-10-19

  Compounds of formula (I) have checkpoint kinase 1 (CHK1) inhibitory activity: wherein R 1 , R 2 , R 5 and R 6 are independently selected from hydrogen, hydroxy, methyl, trifluoromethyl, hydroxymethyl, methoxy, trifluoromethoxy, methylamino and dimethylamino; R 3 , and R 4 are independently selected from hydrogen, hydroxy, C 1 -C 3 alkyl, fluoro-(C 1 -C 3 )-alkyl, hydroxy-(C 1 -C 3 )-alkyl, C 1 -C 3 alkoxy, fluoro-(C 1 -C 3 )-alkoxy, hydroxy-(C 1 -C 3 )-alkoxy, —N(R 11 )—R 12 , -Alk-N(R 11 )—R 12 , —O-Alk-N(R 11 )—R 12 , —C(═O)OH, carboxy-(C 1 -C 3 )-alkyl, or —C(═O)—NH—R 13 ; Alk is a straight or branched chain divalent C 1 -C 6 alkylene radical; R 7 and R 8 are independently selected from hydrogen, hydroxy, or C 1 -C 3 alkoxy; X is a straight chain divalent C 1 -C 3 alkylene radical, optionally substituted on one or more carbons by R 9 and/or R 10 ; W is selected from —C(═O)—N(—R 16 )— or —N(—R 17 )—C(═O)—; Y is hydrogen, C 1 -C 3 alkyl, C 1 -C 3 alkoxy, or halo; and Q is selected from optionally substituted phenyl, optionally substituted cyclohexyl, or an optionally substituted 6-membered monocyclic heteroaryl ring.
• US8916591B2
  申请人：——

  公开号：US8916591B2

  公开（公告）日：2014-12-23