Vanderbilt University

Merck + Co., Inc.

Merck Sharp + Dohme Corp.

Eli Lilly and Company

Ono Pharmaceutical Co., Ltd.

La Jolla Pharmaceuticals Company

Craig William Lindsley

P Jeffrey Conn

Darren W Engers

Corey R Hopkins

Julie L Engers

Colleen M Niswender

Andrew S Felts

Carrie K Jones

Shaun R Stauffer

Kyle A Emmitte

Michael R Wood

Zhijian Zhao

Bruce J Melancon

Kayla J Temple

Aaron M Bender

Charles David Weaver

Madeline Long

Sean R Bollinger

Susana Conde-Ceide

José Manuel Bartolomé-Nebreda

Michael Steven Poslusney

James M Salovich

Alice L Rodriguez

Paul K Spearing

Mark E Duggan

James C Tarr

Rocco D Gogliotti

Richard Williams

Alison R Gregro

Gregor James MacDonald

Yiu-Yin Cheung

Katrina A Bollinger

Han Min Tong

Scott E Wolkenberg

Charles C Hong

Logan A Baker

Douglas J Sheffler

Brittney S Bates

Rory A Capstick

David James Hallett

William D Shipe

Thomas M Bridges

Mark T Bilodeau

José Ignacio Andrés-Gil

Zhicai Wu

Alex Gregory Waterson

Manuel Jesús Alcázar-Vaca

Changho Han

John C Hartnett

David Wisnoski

Ya Zhou

Joe Panarese

Christopher J Dinsmore

Yong-Jin Wu

Philip Arthur Hipskind

Thomas Bachgaard Jensen

Douglas C Beshore

Jeffrey M Bergman

Karen Lynn Lobb

Richard Todd Pickard

Robert Alan Gadski

Lisa Selsam Beavers

Haruto Kurata

George D Hartman

John M Schaus

Leslie Joseph Street

Jun Liang

James C Barrow

Richard Thomas Lewis

Mark E Layton

Wesley Peter Blackaby

Philip E Sanderson

Cynthia Darshini Jesudason

Peter J Manley

Brian Morgan Watson

Gary Allen Sulikowski

Cory R Theberge

Nicholas D P Cosford

James Arthur Nixon

Manuel Jesus Alcazar Vaca

Zhiqiang Yang

Jason Manka

Anna E Ringuette

Joseph David Panarese

Takahiro Mori

Kentaro Yashiro

R Daniel Beauchamp

Brian A Chauder

Heidi E Hamm

Jijun Hao

David D Wisnoski

Yoko Sekioka

Takako Takakuwa

María Luz Martín-Martín

Terence G Hamill

H Donald Burns

Andrew S Jennings

M Brad Nolt

Elizabeth Mary Naylor

Jaime Lynn Bunda

Disclosed herein are 1,2,3,4-tetrahydroisoquinolines and 4, 5, 6, 7-tetrahydrothieno [2, 3-cjpyridines, useful as antagonists of the muscarinic acetylcholine receptor M(mA·Ch·RM). 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

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

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.

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

Indazole compounds as mGluR4 allosteric potentiators, compositions, and methods of treating neurological dysfunction

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

Activator of TREK (TWIK RElated Kchannels) channels

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

Antagonists of the muscarinic acetylcholine receptor M

Indazole compounds as MGLUR4 allosteric potentiators, compositions, and methods of treating neurological dysfunction

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.

Growing community of inventors

Brentwood, TN, United States of America

Craig William Lindsley