GIJSEN HENRICUS JACOBUS MARIA,VAN BRANDT SVEN FRANCISCUS ANNA
申请号：
NZ62385812
公开号：
NZ623858A
申请日:
2012.12.04
申请国别(地区):
NZ
年份:
2015
代理人:
摘要：
The disclosure relates to 5-(3-aminophenyl)-5-alkyl-5,6-dihydro-2-[1,4]oxazin-3-amine derivatives (formula I) as inhibitors of beta-secretase, also known as beta-site amyloid cleaving enzyme, BACE, BACE 1, Asp2, or memapsin2. The invention is also directed to pharmaceutical compositions comprising such compounds and the use of such compounds and compositions for the prevention and treatment of disorders in which beta-secretase is involved, such as Alzheimer&rsquos disease (AD), mild cognitive impairment, senility, dementia, dementia with Lewy bodies, cerebral amyloid angiopathy, multi-infarct dementia, Down&rsquos syndrome, dementia associated with stroke, dementia associated with Parkinson&rsquos disease and dementia associated with beta-amyloid. Example compounds include: (5R,6R*)-6-(Difluoromethyl)-5-{ 2-fluoro-5-[(3-methoxypyridin-2-yl)amino]phenyl} -5-methyl-5,6-dihydro-2H-1,4-oxazin-3-amine (5R,6R)-6-fluoro-5-[2-fluoro-S-(pyrimidin-2-ylamino)phenyl]-5-methyl-5,6-dihydro-2H-1,4-oxazin-3-amine (5R,6R)-5-{ 2-fluoro-5-[(3-methoxypyridin-2-yl)amino]phenyl} -5-methyl-6-(trifluoromethyl)-5,6-dihydro-2H-1,4-oxazin-3-amine (5R,6R)-5-[2-fluoro-5-(pyrimidin-2-ylamino)phenyl]-5-methyl-6-(trifluoromethyl)-5,6-dihydro-2H-1,4-oxazin-3-amine.
