申请人:——
公开号:US20010020035A1
公开(公告)日:2001-09-06
Disclosed are compounds of the formula
1
or the pharmaceutically acceptable non-toxic salts thereof wherein:
W represents substituted or unsubstituted aryl or heteroaryl;
T is hydrogen, halogen, hydroxyl, amino or alkyl;
X is hydrogen, hydroxy, or lower alkyl;
m is 0, 1, or 2;
n is 0, 1, or 2; and
R
3
and R
4
represent substituted or unsubstituted organic residues.
These compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAa brain receptors. These compounds are useful in the diagnosis and treatment of anxiety, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory.
揭示了以下化合物的化学式1或其药用可接受的非毒性盐,其中:W代表取代或未取代的芳基或杂环芳基;T为氢、卤素、羟基、氨基或烷基;X为氢、羟基或较低的烷基;m为0、1或2;n为0、1或2;R3和R4代表取代或未取代的有机残基。这些化合物是高度选择性的GABAa脑受体的激动剂、拮抗剂或逆拮抗剂,或者是GABAa脑受体的激动剂、拮抗剂或逆拮抗剂的前药。这些化合物在焦虑、睡眠和癫痫障碍的诊断和治疗、苯二氮卓类药物过量和增强记忆方面具有用途。