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DERIVES DE 1-PHENYLPYRROLIDIN-2-ONE COMME INHIBITEURS DE PERK
专利权人:
GLAXOSMITHKLINE INTELLECTUAL PROPERTY (NO.2) LIMITED
发明人:
AXTEN, JEFFREY MICHAEL,FAUCHER, NICOLAS ERIC,DAUGAN, ALAIN CLAUDE-MARIE,KETHIRI, RAGHAVA REDDY,KRISTAM, RAJENDRA,VENKATESHAPPA, CHANDREGOWDA
申请号:
CA2998705
公开号:
CA2998705A1
申请日:
2016.09.15
申请国别(地区):
CA
年份:
2017
代理人:
摘要:
The invention is directed to substituted pyrrolidinone and imidazolidinone derivatives. Specifically, the invention is directed to compounds according to Formula I: (I) wherein R1, R2, R3, R4, R5, R6, R7, X and Y are as defined herein. The compounds of the invention are inhibitors of PERK and can be useful in the treatment of cancer, pre-cancerous syndromes and diseases/injuries associated with activated unfolded protein response pathways, such as Alzheimer's disease, neuropathic pain, spinal cord injury, traumatic brain injury, ischemic stroke, stroke, Parkinson's disease, diabetes, metabolic syndrome, metabolic disorders, Huntington's disease, Creutzfeldt- Jakob Disease, fatal familial insomnia, Gerstmann-Sträussler-Scheinker syndrome, and related prion diseases, amyotrophic lateral sclerosis, progressive supranuclear palsy, myocardial infarction, cardiovascular disease, inflammation, organ fibrosis, chronic and acute diseases of the liver, fatty liver disease, liver steatosis, liver fibrosis, chronic and acute diseases of the lung, lung fibrosis, chronic and acute diseases of the kidney, kidney fibrosis, chronic traumatic encephalopathy (CTE), neurodegeneration, dementias, frontotemporal dementias, tauopathies, Pick's disease, Neimann-Pick's disease, amyloidosis, cognitive impairment, atherosclerosis, ocular diseases, arrhythmias, in organ transplantation and in the transportation of organs for transplantation. 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.
来源网站:
中国工程科技知识中心
来源网址:
http://www.ckcest.cn/home/

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