HALL ADRIAN,FARTHING CHRISTOPHER NEIL,CASTRO PINEIRO JOSE LUIS
申请号：
NZ61136512
公开号：
NZ611365A
申请日:
2012.01.20
申请国别(地区):
NZ
年份:
2015
代理人:
摘要：
Disclosed are fused aminodihydrothiazine derivatives of formula (I): wherein X is hydrogen or fluorine； A is CH or N； Y is methyl, ethyl, monofluoromethyl, difluoromethyl, trifluoromethyl, difluoroethyl, methoxy, ethoxy, methoxymethyl or cyano； and pharmaceutically acceptable salts thereof； which compound has an A&bgr； production inhibitory effect or a BACE1 inhibitory effect and is useful as a prophylactic or therapeutic agent for a neurodegenerative disease caused by A&bgr； and typified by Alzheimer-type dementia. Examples of compounds of formula (I) are: N-(3-((4aS,5S,7aS)-2-amino-5-(trifluoromethyl)-4a,5,7,7a-tetrahydro-4H-furo[3,4-d][1,3]thiazin-7a-yl)-4-fluorophenyl)-5-cyanopicolinamide； N-(3-((4aS,5S,7aS)-2-amino-5-(trifluoromethyl)-4a,5,7,7a-tetrahydro-4H-furo[3,4-d] [1,3]thiazin-7a-yl)-4-fluorophenyl)-5-(difluoromethyl)pyrazine-2-carboxamide and N-(3-((4aS,5S,7aS)-2-amino-5-(trifluoromethyl)-4a,5,7,7a-tetrahydro-4H-furo[3,4-d][1,3]thiazin-7a-yl)-4-fluorophenyl)-5-methoxypyrazine-2-carboxamide.
