Substituted 1-aza-2-imino-heterocycles and their use as nicotinic acetylcholin receptors activators
申请人:——
公开号:US20030134848A1
公开(公告)日:2003-07-17
There is provided heterocyclic compounds of the following formula (I):
1
in which,
A is optionally substituted alkyl group, optionally substituted aryl group or optionally substituted heterocyclic group;
B
1
and B
2
are, hydrogen atom, alkyl group or hydroxyl group; or combined together to represent carbonyl group;
X is oxygen atom, sulfur atom, carbon atom or nitrogen atom;
dotted line shows either presence or absence of bond;
n is integer of 1 or 2; and
the group —X—Y— represents optionally substituted alkylene or cyclic alkenylene bond;
or a pharmaceutically acceptable salt thereof.
These compounds have good affinity for &agr;4&bgr;2 nicotinic acetylcholine receptors and activate the same to thereby exert a preventive or therapeutic effect on cerebral dysfunction.
提供以下式(I)的杂环化合物:1其中,A是可选取代烷基、可选取代芳基或可选取代杂环基;B1和B2是氢原子、烷基或羟基;或结合在一起表示羰基;X是氧原子、硫原子、碳原子或氮原子;虚线表示键的存在或不存在;n是1或2的整数;以及—X—Y—基团表示可选取代的烷基或环烯基键;或其药学上可接受的盐。这些化合物具有良好的对α4β2型尼古丁乙酰胆碱受体的亲和力,并激活它们,从而对脑功能障碍产生预防或治疗作用。