Vanderbilt University

Thomas M Bridges

Craig William Lindsley

P Jeffrey Conn

Darren W Engers

James C Tarr

Julie L Engers

Madeline Long

Sean R Bollinger

Paul K Spearing

Michael R Wood

Andrew S Felts

Carrie K Jones

Aaron M Bender

Changho Han

Jeffrey P Conn

Disclosed herein are tricyclic compounds, including pyrimido[4',5&#x2032;:4,5]thieno[2,3-c]pyridazine-8-amine, pyrido[3&#x2032;,2&#x2032;:4,5]thieno[3,2-d]pyrimidine-4-amine, pyrazino[2&#x2032;,3&#x2032;:4,5]thieno[3,2-d]pyrimidin-4-amine, pyrido[3&#x2032;,2&#x2032;:4,5]furo[3,2-d]pyrimidin-4-amine, and pyrimido[4&#x2032;,5&#x2032;:4,5]furo[2,3-c]pyridazin-8-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 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.

In one aspect, the invention relates to indole compounds, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M(mAChR M); synthetic methods for 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. 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.

Indole compounds as positive allosteric modulators of the muscarinic receptor

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Nashville, TN, United States of America

Thomas M Bridges