Vanderbilt University

La Jolla Pharmaceuticals Company

Darren W Engers

Craig William Lindsley

P Jeffrey Conn

Julie L Engers

Corey R Hopkins

Colleen M Niswender

Kayla J Temple

Madeline Long

Aaron M Bender

Alison R Gregro

Sean R Bollinger

Rocco D Gogliotti

Logan A Baker

James M Salovich

Paul K Spearing

Yiu-Yin Cheung

Charles David Weaver

Bruce J Melancon

Charles C Hong

Katrina A Bollinger

Thomas M Bridges

Anna E Ringuette

Joe Panarese

Yong-Jin Wu

Thomas Bachgaard Jensen

Michael R Wood

Michael Steven Poslusney

James C Tarr

Alexa E Richardson

Joanne Bronson

Andrew S Felts

Carrie K Jones

Kyle A Emmitte

Changho Han

Rory A Capstick

Anna L Blobaum

Jeffrey P Conn

Patrick R Gentry

Jerri M Rook

P Jeffery Conn

Matthew Ritter

Anish Vadukoot

Jason Guernon

Michael S Poslusney

PJeffrey Conn

Deuterium-labeled 4-((2,3-dihydrobenzo[b][1,4]dioxin-6-yl)oxy)piperidines substituted with pyrrolo[3,4-b]pyridin-5-one, furo[3,4-b]pyridin-5(7H)-one, or [1,2,4]triazolo[4,3-a]pyrimidin-3(2H)-one 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 modulators of the muscarinic acetylcholine receptor M4

Disclosed herein are analogues of 6-(4-((2,3-dihydrobenzo[b][1,4]dioxin-6-yl)oxy)piperidin-1-yl)-[1,2,4]triazolo[4,3-b]pyridazine, i.e. 7-(4-((phenyl or pyridin-3-yl)oxy)piperidin-1-yl)-4H-pyrimido[1,2-b]pyridazin-4-one derivatives of formula (I) 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.

Substituted pyrimido[1,2-b]pyridazines as positive allosteric modulators of the muscarinic acetylcholine receptor M4

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 M1 (mAChR M1), 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 M1

Disclosed herein are analogues of 6-(4-((2,3-dihydrobenzo[b][1,4]dioxin-6-yl)oxy)piperidin-1 -yl)-[1,2,4]triazolo[4,3-b]pyridazine of formula (Ib), 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.

Substituted pyrimido[1,2-b]pyridazines as positive allosteric modulators of the muscarinic acetylcholine receptor M

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.

Disclosed herein are substituted hexahydro-1H-cyclopenta[c]pyrrole compounds of formula (Ia), 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 substituted 2-azaspiro[3.3]heptane compounds of formula (I'), 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 M4

Disclosed herein are octahydropyrrolo[3,4-b]pyrrole compounds of formula (I), 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. 

Substituted octahydropyrrolo[3,4-b]pyrroles as 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.

Growing community of inventors

Brentwood, TN, United States of America

Darren W Engers