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GAMMA SECRETASE MODULATERS
专利权人:
发明人:
申请号:
EP11702170.9
公开号:
EP2531503A1
申请日:
2011.01.28
申请国别(地区):
EP
年份:
2012
代理人:
摘要:
The invention relates to compounds of formula ( I ) wherein R1/R1 are independently from each other hydrogen, halogen, lower alkoxy or cyano R2 is lower alkyl, halogen, lower alkoxy, lower alkyl substituted by halogen, lower alkoxy substituted by halogen, lower alkyl substituted by OR, =0, -C(O)O-lower alkyl, -C(O)NH-lower alkyl, cyano, CH2-O-lower alkyl, cycloalkyl, NRRor is -O-(CH2)o-phenyl optionally substituted by halogen, or is -(CH2)o-phenyl optionally substituted by one, two or three substituents, selected from halogen, -(CH2)o-cyano, lower alkyl, lower alkyl substituted by halogen, lower alkyl substituted by hydroxy, C(O)H, -CH2-NH2-, -CH2-NH-C(O)O-lower alkyl, -CH2-NH-C(O)-lower alkyl, -CH2-NH-lower alkyl, -CH2-NH-S(O)2-lower alkyl, lower alkoxy or by lower alkoxy substituted by halogen, or is -(CH2)o-cycloalkyl, or is -(CH2)o-heterocycloalkyl which is optionally substituted by halogen, CF3, lower alkyl, -CH2CN, -C(O)-lower alkyl, -C(O)O-lower alkyl or S(O)2-lower alkyl, or is heteroaryl selected from the group consisting of furanyl, pyrazinyl, pyridinyl, benzooxazolyl or benzoimidazolyl which are optionally substituted by lower alkyl, or is 4-methyl-3,4-dihydro-2H-benzo[l,4]oxazine R and R are independently from each other hydrogen or lower alkyl, and o is 0 or 1 R3 may occur once or twice and is lower alkyl A is Formula a), b), c), d), e), f), h), i), j) and Formula k) R2 is hydrogen, lower alkyl, lower alkyl substituted by halogen, C(O)-lower alkyl, S(O)2-lower alkyl or phenyl optionally substituted by halogen hetaryl is a 5 or 6 membered N, S or O-containing heteroaryl group n is O, 1, 2 or 3 if n is 2 or 3, R2 may be the same or not or to pharmaceutically active acid addition salts thereof. The present compounds of formula ( I ) are modulators for amyloid beta and thus, they may be useful for the treatment or prevention of a disease associated with the deposition of β-amyloid in the brain, in particular Alzheimers disease, and other diseases such as c
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