申请人:——
公开号:US20020032189A1
公开(公告)日:2002-03-14
A compound of the formula:
1
wherein Ar is an aromatic ring assembly group which may be substituted or a fused aromatic group which may be substituted; X is (i) a bond, (ii) —S—, —SO— or —SO
2
—, (iii) C
1-6
alkylene, C
2-6
alkenylene or C
2-6
alkynylene, etc., (iv) —CO—O— or (v) —(CH
2
)p-X
1
-, —(CH
2
)p-X
1
-(CH
2
)q-, —(CH
2
)r-CO-X
1
-, —SO
2
—NR
8
- or —(CH
2
)r-SO
2
—NR
8
- wherein X
1
is O or NR
8
, R
8
is H, a hydrocarbon group which may be substituted or an acyl, p is 0 to 5, q is 1 to 5, p+q is 1 to 5, and r is 1 to 4; Y is a divalent C
1-6
aliphatic hydrocarbon group optionally containing O or S, which may be substituted; R
1
and R
2
each is H or a lower alkyl which may be substituted, or R
1
and R
2
form a N-containing heterocyclic ring which may be substituted; Ring A is a benzene ring which may be further substituted; and Ring B is a 4- to 8-membered ring which may be further substituted, or a salt thereof has the effect of inhibiting amyloid-&bgr; protein production and/or secretion and is useful as a pharmaceutical composition for preventing and/or treating the neurodegenerative disease, etc.
该化合物的化学式为:1其中,Ar是芳香环组装基团,可以是取代的或融合的芳香基团,可以是取代的;X是(i)化学键,(ii)-S-,-SO-或-SO2-,(iii)C1-6烷基,C2-6烯基或C2-6炔基等,(iv)-CO-O-或(v)-(CH2)p-X1-,-(CH2)p-X1-(CH2)q-,-(CH2)r-CO-X1-,-SO2-NR8-或-(CH2)r-SO2-NR8-,其中X1是O或NR8,R8是氢,可以是取代的碳氢基团或酰基,p为0至5,q为1至5,p+q为1至5,r为1至4;Y是二价C1-6脂肪烃基团,可以选择性地含有O或S,可以是取代的;R1和R2分别是氢或可以取代的低烷基,或者R1和R2形成一个可以取代的含N的杂环;环A是苯环,可以进一步取代;环B是4-至8-成员环,可以进一步取代,或其盐具有抑制淀粉样蛋白β的产生和/或分泌的作用,可用作预防和/或治疗神经退行性疾病等的药物组成物。