申请人:——
公开号:US20020035121A1
公开(公告)日:2002-03-21
Disclosed are compounds of the formula:
1
wherein X, Q, W and
2
are as defined herein. These compounds are agonists, antagonists or inverse agonists for GABA
A
brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABA
A
brain receptors and are therefore useful in the diagnosis and treatment of anxiety, depression, Down Syndrome, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory. Pharmaceutical compositions, including packaged pharmaceutical compositions, are further provided. Compounds of the invention are also useful as probes for the localization of GABA
A
receptors in tissue samples.
本发明揭示了化合物的公式:1,其中X,Q,W和2如定义所述。这些化合物是GABAA脑受体的激动剂,拮抗剂或反向激动剂,或者是GABAA脑受体激动剂,拮抗剂或反向激动剂的前药,因此在焦虑,抑郁,唐氏综合症,睡眠和癫痫障碍,苯二氮卓类药物过量和记忆增强的诊断和治疗中有用。此外,还提供了包括包装的制药组合物在内的制药组合物。本发明的化合物还可用作组织样本中GABAA受体定位的探针。