5-HT2C receptor modulators: a patent survey.

IMPORTANCE OF THE FIELD

The 5-HT(2C) receptor is a GPCR and is one of the 14 subtypes that constitute the serotonin receptor family. The 5-HT₂(C) receptor is exclusively expressed in the CNS where it demonstrates a wide distribution and displays high-affinity interactions with a wide variety of psychiatric medications. Modulators of 5-HT₂(C) have been implicated as a potential treatment for diseases of significant unmet medical need, including obesity, schizophrenia, depression, anxiety, Parkinson's disease, drug addiction, erectile dysfunction and urinary incontinence. Thus, there is a great interest in developing potent and selective 5-HT₂(C) receptor modulators.

AREAS COVERED IN THIS REVIEW

This review article highlights the research progress in 5-HT₂(C) receptor modulators published in the patent literature between January 2003 and June 2010, giving emphasis to the medicinal chemist's standpoint.

WHAT THE READER WILL GAIN

Readers will rapidly gain an overview of the various 5-HT₂(C) receptor modulators reported in the patent literature in the past 8 years. Furthermore, the readers will learn which structure type can interact with the 5-HT₂(C) receptor. In addition, the readers will be aware of the pharmaceutical companies that have been the main players in the field.

TAKE HOME MESSAGE

There is substantial evidence supporting the concept that a selective 5-HT₂(C) receptor modulator should provide benefit in the treatment of a variety of CNS disorders. Although research efforts have identified several promising 5-HT₂(C) receptor modulators that display high functional selectivity, further clinical efficacy and safety data are needed to prove their actual clinical utility. Therefore, the query for selectively acting 5-HT₂(C) receptor modulators is still ongoing.