Vanderbilt University

Kyle A Emmitte

Craig William Lindsley

P Jeffrey Conn

Andrew S Felts

Carrie K Jones

Alice L Rodriguez

Brittney S Bates

Julie L Engers

Charles David Weaver

Katrina A Bollinger

Brian A Chauder

Katrina A Smith

Yong-Jin Wu

Darren W Engers

Corey R Hopkins

Colleen M Niswender

Aaron M Bender

Changho Han

Joe Panarese

Joanne Bronson

Leah C Konkol

Jeffrey P Conn

Megan M Breiner

4,5-Substituted Picolinamide and picolinonitrile compounds of formula (I), where Ris CONHor CN and Ris an optionally substituted aryl or heteroaryl, are negative allosteric modulators of the metabotropic glutamate receptor 2 (mGlu). The compounds and pharmaceutical compositions including the compounds may be useful for treating depression, anxiety, obsessive-compulsive disorder, cognitive disorders, Alzheimer's disease, or autism spectrum disorders in a subject. 

4,5-substituted picolinamide and picolinonitrile metabotropic glutamate receptor 2 negative allosteric modulators

Described are negative allosteric modulators of metabotropic glutamate receptor 3 (mGlu3), pharmaceutical compositions including the compounds, and methods of using the compounds and compositions for treating depression, cognitive disorders, schizophrenia, Alzheimer's disease, or cancer in a subject.

Negative allosteric modulators of metabotropic glutamate receptor 3

Compounds which are useful as allosteric potentiators/positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4); pharmaceutical compositions comprising the compounds; and methods of using the compounds, for example, in treating neurological and psychiatric disorders or other disease state associated with glutamate dysfunction.

Isoquiniline and napthalene-substituted compounds as mGluR4 allosteric potentiators, compositions, and methods of treating neurological dysfunction

Substituted pyrrolopyridine, imidazopyridine and triazolopyridine compounds having a formula are positive allosteric modulators of the muscarinic acetylcholine receptor M(mAChR M) and the compounds and their pharmaceutical compositions may be useful in treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction. Compounds of the invention may be prepared in several steps from 2-halo-5,6-dihydro-7H-pyrrolo[3,4-b]pyridin-7-one intermediates.

Substituted pyrrolo[3,4-e]indolizines, imidazo[1,2-a]pyrrolo[3,4-e]pyridines, pyrrolo[3,4-e][1,2,4]triazolo[1,5-a]pyridines and pyrrolo[3,4-e][1,2,4]triazolo[4,3-a]pyridines as positive allosteric modulators of muscarinic acetylcholine receptor M1

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

Described are negative allosteric modulators of metabotropic glutamate receptor 3 (mGlu), pharmaceutical compositions including the compounds, and methods of using the compounds and compositions for treating depression, cognitive disorders, schizophrenia, Alzheimer's disease, or cancer in a subject. Exemplary negative allosteric modulators of metabotropic glutamate receptor 3 include pyrazolo[1,5-&#x3b1;]pyrazine compounds, such as those of the following formula: 

Substituted pyrazolo[1,5-a]pyrazines as negative allosteric modulators of metabotropic glutamate receptor 3

Substituted 6-aryl-imidazopyridine and 6-aryl-triazolopyridine carboxamide analogs as negative allosteric modulators of mGluR5

Substituted bicyclic heteroaryl carboxamide analogs as mGluR5 negative allosteric modulators

Described are negative allosteric modulators of metabotropic glutamate receptor 2 (mGlu), pharmaceutical compositions including the compounds, and methods of using the compounds and compositions for treating depression, anxiety, obsessive-compulsive disorder, cognitive disorders, Alzheimer's disease, or autism spectrum disorders in a subject.

Negative allosteric modulators of metabotropic glutamate receptor 2

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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

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Spring Hill, TN, United States of America

Kyle A Emmitte