Vanderbilt University

Julie L Engers

Craig William Lindsley

P Jeffrey Conn

Darren W Engers

Aaron M Bender

Madeline Long

Kyle A Emmitte

Kayla J Temple

Sean R Bollinger

Paul K Spearing

Katrina A Bollinger

Corey R Hopkins

Colleen M Niswender

James C Tarr

Alison R Gregro

Logan A Baker

Thomas M Bridges

Joe Panarese

Yong-Jin Wu

Changho Han

Anna E Ringuette

Joanne Bronson

Anna L Blobaum

Megan M Breiner

Leah C Konkol

Jerri M Rook

6,7-Dihydrothiazolo[5,4-c]pyridines substituted in the 5-position with heterocyclic rings are positive allosteric modulators of the muscarinic acetylcholine receptor M(mAChR M) and may have use in treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction.

Positive allosteric modulators of the muscarinic acetylcholine receptor M4

Described are positive allosteric modulators of muscarinic acetylcholine receptor M(mAChR M), pharmaceutical compositions including the compounds, and methods of using the compounds and compositions for treating neurological disorders, psychiatric disorders, or a combination thereof.

Positive allosteric modulators of the muscarinic acetylcholine receptor M

Disclosed herein are substituted hexahydro-1H-cyclopenta[c]pyrrole compounds, which may be useful as antagonists 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 disorders using the compounds and compositions.

Antagonists of the muscarinic acetylcholine receptor M

Disclosed herein are 3-azabicyclo[3.1.0]hexan-6-amine compounds, which may be useful as antagonists 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 disorders using the compounds and compositions.

Disclosed herein are tricyclic compounds, including 3-(difluoromethyl)-4-methylpyrimido[4',5&#x2032;:4,5]thieno[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.

Antagonists of the muscarinic acetylcholine receptor M4

Disclosed herein are substituted 7-azaspiro[3.5]nonane compounds, which may be useful as antagonists 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 disorders using the compounds and compositions.

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.

Disclosed herein are pyrido[3',2&#x2032;:4,5]thieno[2,3-d]pyridazin-8-amine and thieno[2,3-c:4,5-d&#x2032;]dipyridazin-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.

Disclosed herein are 2,4-dimethylquinoline-6-carboxamide compounds and 3,4-dimethylcinnoline-6-carboxamide 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.

Disclosed herein are thieno[2,3-b:5,4-c']dipyridin-8-amine and pyrido[4&#x2032;,3&#x2032;:4,5]thieno[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 M1

Disclosed herein are tricyclic compounds, including thieno[2,3-d:4,5-d']dipyrimidin-4-amine and pyrido[4&#x2032;,3&#x2032;:4,5]thieno[2,3-d]pyrimidin-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.

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.

Growing community of inventors

Brentwood, TN, United States of America

Julie L Engers