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Expert Opin Ther Pat. 2013 Apr;23(4):393-408. doi: 10.1517/13543776.2013.760544. Epub 2013 Jan 22.

mGlu5 negative allosteric modulators: a patent review (2010-2012).

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Vanderbilt University Medical Center, Vanderbilt Center for Neuroscience Drug Discovery, Department of Chemistry, Nashville, TN 37232, USA.



The design and development of small molecule negative allosteric modulators (NAMs) of the metabotropic glutamate receptor subtype 5 (mGlu5) has been an area of intense interest for over a decade. Potential roles have been established for mGlu5 NAMs in the treatment of diseases such as pain, anxiety, gastroesophageal reflux disease (GERD), Parkinson's disease levodopa-induced dyskinesia (PD-LID), fragile X syndrome (FXS), autism, addiction, and depression.


This review begins with an update of the clinical trial efforts with mGlu5 NAMs. Following that update, the review summarizes small molecule mGlu5 NAM patent applications published between 2010 and 2012. These summaries are subdivided into three separate groups: inventions related to improvements in drug properties and/or developability, new chemical entities that contain a disubstituted alkyne, and new chemical entities that do not contain a disubstituted alkyne.


Given the abundant promise found within the mGlu5 NAM field, optimism remains that a drug will emerge from this therapeutic class. Still, the launch of a new drug is far from a certainty. It is encouraging to observe the ever-increasing chemical diversity among mGlu5 NAMs. Finally, in spite of the mature nature of this field, room remains for new advancements.

[Indexed for MEDLINE]

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