| 摘要 |
<p>A class of selectively substituted fused tricyclic compounds based on a substituted pyridinone moiety are potent and functionally selective ligands for the α2/α3 subunit of the human GABA-A receptor and are thereby effective in the treatment of anxiety. The present invention provides a compound of formula (I), or a salt or N-oxide thereof: wherein E represents -(CH2)n-; n is 1, 2 or 3; R1 represents aryl, C¿3-7? heterocycloalkyl, C3-7 heterocycloalkenyl or heteroaryl, any of which groups may be optionally substituted; or halogen, -NHCOR?3, -COR3¿ or CO¿2R?3; R2 represents aryl or heteroaryl, either of which groups may be optionally substituted; and R3 represents C¿3-6? alkyl, hydroxy(C1-6)alkyl, C2-6 alkenyl, C3-7 cycloalkyl, aryl, aryl(C1-6)alkyl, heteroaryl or heteroaryl(C1-6)alkyl, any of which groups may be optionally substituted; said optional substitutents on R?1, R2 and R3¿ being independently selected from C¿1-6? alkyl, halo(C1-6)alkyl, C3-7 cycloalkyl, halogen, formyl and C2-6 alkylcarbonyl; excluding compounds in which R?1¿ represents methylthiazolyl or hydroxymethylthiazolyl.</p> |
