申请人:——
公开号:US20010044461A1
公开(公告)日:2001-11-22
Disclosed are compounds of the formula:
1
or the pharmaceutically acceptable acid addition salts thereof, wherein:
R
1
, R
2
, R
3
, R
4
are the same or different and represent hydrogen, C
1
-C
6
alkyl, halogen, hydroxy, amino, cyano, nitro, trifluoromethyl, trifluoromethoxy, C
1
-C
6
alkoxy, —O
2
CR′, —NHCOR′, —COR′, —SO
m
R′, where R′ is C
1
-C
6
alkyl and wherein m is 0, 1 or 2; or
R
1
, R
2
, R
3
, R
4
independently represent —CONR′R″, or —NR′R″ where R′ and R″ independently represent hydrogen or C
1
-C
6
alkyl;
R
5
is hydrogen or C
1
-C
6
alkyl; and
R represents an aminoalkyl group,
which compounds are useful in the treatment of affective disorders such as schizophrenia, depression, Alzheimer's disease, movement disorders such as Parkinsonism and dystonia, and other disorders which respond to dopaminergic blockade such as substance abuse and obsessive compulsive disorders. Further, compounds of this invention may be useful in treating the extrapyramidal side effects associated with the use of conventional neuroleptic agents.
本发明公开了以下式子的化合物
1
或其药学上可接受的酸加成盐,其中
R
1
, R
2
, R
3
, R
4
相同或不同,代表氢、C
1
-C
6
烷基、卤素、羟基、
氨基、
氰基、硝基、三
氟甲基、三
氟甲氧基、C
1
-C
6
烷氧基、-O
2
cr′、-nhcor′、-cor′、-so
m
R′,其中 R′是 C
1
-C
6
烷基,其中 m 为 0、1 或 2;或
R
1
, R
2
, R
3
, R
4
独立地代表-CONR′R″,或-NR′R″,其中 R′和 R″ 独立地代表氢或 C
1
-C
6
烷基;
R
5
是氢或 C
1
-C
6
烷基;以及
R 代表
氨基烷基、
这些化合物可用于治疗情感障碍,如精神分裂症、抑郁症、阿尔茨海默病、运动障碍,如帕
金森氏症和肌张力障碍,以及其他对
多巴胺能阻断反应的障碍,如药物滥用和强迫症。此外,本发明的化合物还可用于治疗与使用传统神经
安定剂相关的锥体外系副作用。