Substituted spiro[isobenzofuran-1,4-piperidin]-3-ones and 3H-spiroisobenzofuran-1,4-piperidines
capable of modulating NPY5 receptor activity are provided. Such compounds may be
used to modulate ligand binding to NPY5 receptors in vivo or in vitro, and are
particularly useful in the treatment of a variety of disorders (e.g., eating disorders
such as obesity or bulimia, psychiatric disorders, diabetes and cardiovascular
disorders such as hypertension) in humans, domesticated companion animals and livestock
animals. Pharmaceutical compositions and methods for treating such disorders are
provided, as are methods for using such compounds for detecting NPY5 receptors.