BAUMANN, KARLHEINZ,FLOHR, ALEXANDER,GOETSCHI, ERWIN,JACOBSEN, HELMUT,JOLIDON, SYNESE,LUEBBERS, THOMAS
申请号：
CA2703824
公开号：
CA2703824C
申请日:
2009.01.05
申请国别(地区):
CA
年份:
2016
代理人:
摘要：
The invention relates to compounds of formula (I) R1 is-C(O)O-lower alkyl, cyano or is hetaryl hetaryl is a five-or six memberedheteraryl group, optionally substituted by R R is halogen, lower alkyl,lower alkyl substituted by halogen, lower alkoxy or lower alkoxy substitutedby halogen R2 is hydrogen, lower alkoxy, lower alkyl, halogen or cyanoR3 is -(CH2)n-C(O)O-lower alkyl, lower alkyl, lower alkoxy, hydroxy,-O-Si(CH3)2-lower alkyl, -C(O)-N(lower alkyl)2, -O-S(O)2-lower alkyl,C3-7-cycloalkyl, S(O)2-aryl, heterocyclyl, -C(O)-heterocyclyl, or is aryl orhetaryl, which aryl or hetaryl rings are optionallysubstituted by one or more R R4 is hydrogen, lower alkyl, hydroxy or CH2CNX is S or -N=C(R5)- R5 is hydrogen, lower alkyl orhydroxy, is a bond, -O-, -CH2-, -CH2-CH2-, formula (II) or or -N(R)- R ishydrogen, lower alkyl, C(O)O-lower alkyl, C(O)-loweralkyl, S(O)2-lower alkyl, or benzyl n is 0 or 1 or to pharmaceutically activeacid addition salts. The compounds may be used forthe treatment of Alzheimers disease, cerebral amyloid angiopathy, hereditarycerebral hemorrhage with amyloidosis, Dutch-type(HCHWA-D), multi-infarct dementia, dementia pugilistica or Down syndrome.
