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1 PHENYLPYRROLIDIN 2 ONE DERIVATIVES AS PERK INHIBITORS
专利权人:
发明人:
AXTEN JEFFREY MICHAEL,FAUCHER NICOLAS ERIC,DAUGAN ALAIN CLAUDE MARIE,KETHIRI RAGHAVA REDDY,KRISTAM RAJENDRA,VENKATESHAPPA CHANDREGOWDA
申请号:
IN201817009508
公开号:
IN201817009508A
申请日:
2018.03.15
申请国别(地区):
IN
年份:
2018
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 Alzheimers disease neuropathic pain spinal cord injury traumatic brain injury ischemic stroke stroke Parkinsons disease diabetes metabolic syndrome metabolic disorders Huntingtons disease Creutzfeldt Jakob Disease fatal familial insomnia Gerstmann Strussler 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 Picks disease Neimann Picks 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.
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