The invention is directed to substituted indoline derivatives. Specifically, the invention is directed to compounds according to Formula 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, ocular diseases, 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, pancreatic, 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.本發明係關於經取代之吲哚啉衍生物。具體地說，本發明係關於根據式(I)之化合物：其中R1、R2及R3是在文中定義。本發明之化合物是PERK之抑制劑且可以用於治療癌症、眼疾及與活化未折疊的蛋白質反應路徑相關的疾病，例如阿茲海默氏症、中風、第1型糖尿病、巴金森氏症、漢丁頓氏舞蹈症、肌萎縮性側索硬化症、心肌梗塞、心血管疾病、動脈硬化及心律失調，且更特別是乳房、結腸、胰臟及肺之癌症。據此，本發明也關於包含本發明化合物之醫藥組成物。本發明還關於使用本發明化合物或包含本發明化合物之醫藥組成物抑制PERK活性及治療與其相關的疾病之方法。
