5-Amino-3-[1-[2-(2,5-difluorophenyl)acetyl]-2,3-dihydroindol-5-yl]-1-ethylpyrazole-4-carboxamide

• 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-[1-[2-(2,5-difluorophenyl)acetyl]-2,3-dihydroindol-5-yl]-1-ethylpyrazole-4-carboxamide
• 英文别名: 5-amino-3-[1-[2-(2,5-difluorophenyl)acetyl]-2,3-dihydroindol-5-yl]-1-ethylpyrazole-4-carboxamide
• 化学式: C₂₂H₂₁F₂N₅O₂
• 分子量: 425.4
• InChiKey: IFKVREKEIPOOFD-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.5
• 重原子数：
  31
• 可旋转键数：
  5
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.23
• 拓扑面积：
  107
• 氢给体数：
  2
• 氢受体数：
  6

文献信息

• [EN] INDOLINE DERIVATIVES AS INHIBITORS OF PERK<br/>[FR] DÉRIVÉS D'INDOLINE UTILISÉS COMME INHIBITEURS DE PERK
  申请人：GLAXOSMITHKLINE IP NO 2 LTD

  公开号：WO2015056180A1

  公开（公告）日：2015-04-23

  The invention is directed to substituted indoline derivatives. Specifically, the invention is directed to compounds according to Formula I: (I) wherein R1, R2 and R3 are defined herein. The compounds of the invention are inhibitors of PERK and can be useful in the treatment of cancer and diseases associated with activated unfolded protein response pathways, such as Alzheimer's disease, stroke, Type 1 diabetes, Parkinson disease, Huntington's disease, amyotrophic lateral sclerosis, myocardial infarction, cardiovascular disease, atherosclerosis, and arrhythmias, and more specifically cancers of the breast, colon, pancreas and lung. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting PERK activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.