2-(HET-)ARYL-4-(CYCLIC AMINO SUBSTITUTED) HETEROARYL FUSED PYRIDINE DERIVATIVES, THEIR PREPARATION AND THEIR USE AS (ANT-)AGONISTS FOR GABA (A) BRAIN RECEPTORS

摘要

Disclosed are compounds of formula (a) or the pharmaceutically acceptable non-toxic salts thereof wherein: n is an integer from 0 to 3; A and B are hydrogen or lower alkyl; the C ring represents a thiophene, pyridine or pyrimidine ring; and W is aryl, heteroaryl, 2- or 3-thienyl, or 2-, 3-, or 4-pyridyl, each of which may be substituted; X is CH, N, or O; Z represents an electron pair, hydrogen, or (un)substituted aryl, C(O)R or C(S)R; and R is as defined in the description, 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.