Trabanco-Suárez Andrés Avelino,Tresadern Gary John,Delgado-Jiménez Francisca,Vega Ramiro Juan Antonio,Gijsen Henricus Jacobus Maria,Oehlrich Daniel
申请号：
NZ61094811
公开号：
NZ610948A
申请日:
2011.12.21
申请国别(地区):
NZ
年份:
2014
代理人:
摘要：
The present invention relates to novel 5,6-dihydro-imidazo[1,2-a]pyrazin-8-ylamine derivatives as inhibitors of beta-secretase, also known as beta-site amyloid cleaving enzyme, BACE, BACE1, Asp2, or memapsin2. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which beta-secretase is involved, such as Alzheimer’s disease (AD), mild cognitive impairment, senility, dementia, dementia with Lewy bodies, cerebrovascular amyloid angiopathy, multi- infarct dementia, Down’s syndrome, dementia associated with stroke, dementia associated with Parkinson’s disease or dementia associated with beta-amyloid. Compounds of the disclosure include: (R)-N-{ 3-[8-amino-3-difluoromethyl-6-methyl-5,6-dihydroimidazo[1,2-a]pyrazin-6-yl]-4-fluorophenyl} -5-fluoropyridine-2-carboxamide, (R)-N-{ 3-[8-amino-2-chloro-3-cyano-6-methyl-5,6-dihydroimidazo[1,2-a]pyrazin-6-yl]-4-fluorophenyl} -5-fluoropyridine-2-carboxamide, (R)-5-methoxy-pyrazine-2-carboxylic acid [3-(8-amino-6-methyl-5,6-dihydro-imidazo[1,2-a]pyrazin-6-yI)-4-fluoro-phenyl]-amide, And (R)-tert-butyl [2-chloro-3-cyano-6-(2-fluoro-5-{ [(5-methoxypyrazin-2-yl)carbonyl]amino} phenyl)-6-methyl-5,6-dihydroimidazo[1,2-a]pyrazin-8-yl]carbamate
