OXOCOUMARIN AND BARBITURIC ACID DERIVATES, THEIR PREPARATION AND THEIR USE AS LIGAND INHIBITORS OF A CORTICOTROPIN-RELEASING FACTOR (CRF) AND/OR A CRF-BINDING PROTEIN COMPLEX

摘要

Ligand inhibitors for increasing levels of free corticotropin-releasing factor(CRF) in the brain are disclosed. Such ligand inhibitors cause release of CRFfrom the CRF/CRF-bind protein complex. Administration of the ligand inhibitorsprovide improvement in learning and memory, result in decreased food intakeand/or provide treatment for diseases associated with low levels of CRF in thebrain, notably Alzheimer's disease. In the practice of this invention, theligand inhibitor is one or more compounds having the structure (I), (II) or(III), including keto tautomers, stereoisomers and pharmaceutically acceptablesalts thereof, wherein R1, G and Xm of structure (I), R1', R2'R3', G and W ofstructure (II), and R1", R2", R3" and W of structure (III) are as disclosed inthe description.