Certain 4-aminomethyl-2-substituted imidazole derivatives and 2-aminomethyl-4-substituted imidazole derivatives; new classes of dopamine receptor subtype specific ligands
申请人:Neurogen Corporation
公开号:US20020143044A1
公开(公告)日:2002-10-03
Disclosed are compounds of the formula:
1
wherein R
1
represents optionally substituted aryl, heteroaryl, arylalkyl, or cycloalkyl groups; X, Z, and Y are optionally substituted nitrogen or carbon atoms; R
3
and R
4
are organic or inorganic substitutents which may together form ring structutes; m is zero, one or two; and R
5
and R
6
are are organic or inorganic substituents;
and the pharmaceutically acceptable addition salts thereof,
which compounds are highly selective partial agonists or antagonists at brain dopamine receptor subtypes or prodrugs thereof and are useful in the diagnosis and treatment of affective disorders such as schizophrenia and depression as well as certain movement disorders such as Parkinsonism.
本发明涉及以下公式的化合物:1其中,R1代表可选取代的芳基,杂芳基,芳基烷基或环烷基基团;X,Z和Y是可选取代的氮或碳原子;R3和R4是有机或无机取代基,它们可以共同形成环结构;m为零,一或二;R5和R6是有机或无机取代基;以及其药学上可接受的盐。这些化合物是高度选择性的部分激动剂或拮抗剂,适用于诊断和治疗情感障碍,如精神分裂症和抑郁症以及某些运动障碍,如帕金森病。