Glycine transporter-1 inhibitors: a patent review (2011-2016).

Mounting clinical failures with schizophrenic patients have blunted enthusiasm for GlyT-1 inhibition as an approach to treat the disease. However, research in the area remains quite active, as therapeutic potential for several additional indications has emerged. There are numerous and diverse GlyT-1 chemotypes now available that exhibit differentiating modes of binding and ligand-target binding kinetics, and this rich diversity of chemical matter may help further elucidate the target's pharmacological role in various indications and lead to the identification of a compound with optimal properties that may someday become a drug.