Vanderbilt University

Alice L Rodriguez

P Jeffrey Conn

Carrie K Jones

Craig William Lindsley

Andrew S Felts

Charles David Weaver

Kyle A Emmitte

Brittney S Bates

Colleen M Niswender

Richard Williams

Brian A Chauder

Katrina A Smith

Jeffrey P Conn

Disclosed are negative allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

Substituted imidazopyridine and triazolopyridine compounds as negative allosteric modulators of mGluR5

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In one aspect, the invention relates to compounds, including phenylethynylbenzamide derivatives, cycloalkylethynylbenzamide derivatives, styrylbenzamide derivatives, 4-(3-phenyl-1,2,4-oxadiazol-5-yl)benzamide derivatives, 4-(pyridinylethynyl)benzamide derivatives, and N-phenylterephthalamide derivatives, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

Benzamide mGluR5 positive allosteric modulators and methods of making and using same

Substituted benzamide analogs as mGluR5 negative allosteric modulators and methods of making and using the same

Substituted heteroarylamide analogs as mGluR5 negative allosteric modulators and methods of making and using the same

Substituted heteroarylamine carboxamide analogs as mGluR5 negative allosteric modulators and methods of making and using the same

Substituted phenylamine carboxamide analogs as mGluR5 negative allosteric modulators and methods of making and using the same

In one aspect, the invention relates to bicyclic MGluR5 positive allosteric modulators, for example 6-(phenylethynyl)-3,4-dihydroisoquinolin-1(2H)-one, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

Bicyclic mGluR5 positive allosteric modulators and methods of making and using same

Provided is a method of treating conditions and disorders for which full mGluR5 antagonists are potentially effective, such as, e.g., anxiety, epilepsy, schizophrenia and other psychotic disorders, Parkinson's disease, addictive disorders, and the like in a subject in need of such treatment, comprising administration to such subject of a therapeutically effective amount of a partial, non-competitive mGluR5 antagonist compound of the invention. Specific examples of partial MgluR5 antagonists provided include those compounds having the formula: wherein:

Partial mGluR5 antagonists for treatment of anxiety and CNS disorders

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Nashville, TN, United States of America

Alice L Rodriguez