申请人:Neurogen Corporation, Corporation of the State of Delaware
公开号:US20020156280A1
公开(公告)日:2002-10-24
The present invention encompasses structures of the Formula
1
or the pharmaceutically acceptable non-toxic salts thereof wherein:
X is hydrogen, halogen, (un)substituted alkyl, (un)substituted alkoxy or amino; and
Y is (un)substituted alkyl, aryl, or heteroaryl,
which 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, Down Syndrome, sleep, cognitive and seizure disorders, and overdose with benzodiazepine drugs and for enhancement of alertness.
本发明涵盖了Formula1的结构或其药学上可接受的非毒性盐,其中:X为氢、卤素、(未)取代烷基、(未)取代烷氧基或氨基;Y为(未)取代烷基、芳基或杂环芳基,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。这些化合物在焦虑、唐氏综合症、睡眠、认知和癫痫障碍、苯二氮平类药物过量和警觉性增强的诊断和治疗中有用。