F. HOFFMANN-LA ROCHE AG;GREEN, Luke;LIMBERG, Anja;BAUMANN, Karlheinz;LUEBBERS, Thomas;THOMAS, Andrew
发明人:
BAUMANN, Karlheinz,GREEN, Luke,LIMBERG, Anja,LUEBBERS, Thomas,THOMAS, Andrew
申请号：
EPEP2012/053301
公开号：
WO2012/116965A1
申请日:
2012.02.28
申请国别(地区):
EP
年份:
2012
代理人:
摘要：
The present invention relates to compounds of formula (l)； hetaryl I is a five or six membered heteroaryl group, containing 1 to 3 heteroatoms, selected from S or N； hetaryl II is a six membered heteroaryl group, containing 1 to 3 heteroatoms, selected from S or N, or is a two membered ring system containing 1 to 4 heteroatoms selected from S, or N, wherein at least one ring is aromatic in nature； R1 is lower alkyl, lower alkoxy, lower alkyl substituted by halogen or halogen； R2 is lower alkyl, lower alkyl substituted by halogen, halogen, lower alkoxy, cycloalkyl substituted by lower alkyl or lower alkyl substituted by halogen, or is lower alkyl substituted by hydroxy, or is furyl, or is O-benzyl, (CH2)p-phenyl, optionally substituted by halogen, lower alkoxy, lower alkyl substituted by halogen, lower alkyl or by cyano； R3 is hydrogen or lower alkyl； Y is (CH2)n-, -CH2OCH2-, -CH2O-, CH2S-, -CH2SCH2- and is bonded to two of the ring carbon atoms, bonding being to either the ring carbon atoms a and b or the ring carbon atoms c and d； p is 0 or 1； m is 0, 1 or 2； if m is 2 then R1 may be the same or different； -75- n is 2 or 3； o is 0, 1 or 2, if o is 2, then R2 may be the same or different； 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 cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica and Down syndrome.La présente invention porte sur des composés de formule (I), dans laquelle hétéroaryle I représente un groupe hétéroaryle à cinq ou six chaînons, contenant 1 à 3 hétéroatomes choisis entre S et N ； hétéroaryle II représente un groupe hétéroaryle à six chaînons, contenant 1 à 3 hétéroatomes choisis entre S et
