Vanderbilt University

Carrie K Jones

P Jeffrey Conn

Craig William Lindsley

Alice L Rodriguez

Andrew S Felts

Shaun R Stauffer

Susana Conde-Ceide

Charles David Weaver

Kyle A Emmitte

Richard Williams

José Manuel Bartolomé-Nebreda

Brittney S Bates

Han Min Tong

Douglas J Sheffler

Gregor James MacDonald

Colleen M Niswender

Brian A Chauder

Darren W Engers

José Ignacio Andrés-Gil

Manuel Jesús Alcázar-Vaca

Manuel Jesus Alcazar Vaca

Changho Han

María Luz Martín-Martín

Thomas M Bridges

Jason Manka

Ya Zhou

Katrina A Smith

Gregor McDonald

José Manuel Bartolome-Nebreda

Jon Jacobs

Gregor Macdonald

Gregor James Macdonald

Jeffrey P Conn

Chrysa Malosh

Disclosed herein are thieno[3,2-e][1,2,4]triazolo[1,5-a]pyridin-6-amine, thieno[3,2-e][1,2,4]triazolo[4,3-a]pyridin-3-amine, and imidazo[1,2-a]thieno[3,2-e]pyridin-3-amine compounds, which may be useful as positive allosteric modulators of the muscarinic acetylcholine receptor M(mAChR M). Also disclosed herein are methods of making the compounds, pharmaceutical compositions comprising the compounds, and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions.

Positive allosteric modulators of the muscarinic acetylcholine receptor M4

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

In one aspect, the invention relates to substituted pyrazolo[1,5-a]pyrazines analogs, 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.

Substituted pyrazolo[1,5-a]pyrazines as mGluR5 receptor modulators

In one aspect, the invention relates to novel bicyclic oxazole and thiazole compounds which are positive allosteric modulators of the metabotropic glutamate receptor subtype 5 ('mGluR5'); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions; and methods for the treatment or prevention of disorders associated with glutamate dysfunction and diseases in which the mGluR5 subtype of receptors is involved. 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 oxazole and thiazole compounds and their use as allosteric modulators of mGluR5 receptors

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In one aspect, the invention relates to imidazopyrimidin-5(6H)-one analogs, 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.

Substituted imidazopyrimidin-5(6H)-ones as allosteric modulators of MGLUR5 receptors

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

In one aspect, the invention relates to naphthyridinone analogs, 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.

Naphthyridinone analogs as mGluR5 positive allosteric modulators

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

In one aspect, the invention relates to substituted pyrazolo[1,5-a]pyrazine compounds, 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.

Substituted pyrazolo[1,5-A]pyrazine compounds as allosteric modulators of mGluR5 receptors

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

In one aspect, the invention relates to bicyclic triazole and pyrazole lactams, 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 triazole and pyrazole lactams as allosteric modulators of mGluR5 receptors

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 compounds which are useful as inhibitors of glycine type 1 transporter (GlyT1) activity; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating disorders associated with glycine type 1 transporter (GlyT1) activity 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.

3.1.0 bicyclic GlyT1 inhibitors and methods of making and using same

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Nashville, TN, United States of America

Carrie K Jones