Vanderbilt University

University of Michigan

Rocco D Gogliotti

Craig William Lindsley

P Jeffrey Conn

Colleen M Niswender

Corey R Hopkins

Darren W Engers

Shaun R Stauffer

James M Salovich

Stephen W Fesik

Yiu-Yin Cheung

Taekyu Lee

Changho Han

Joseph R Alvarado

Kenneth M Meyers

Charles David Weaver

KyuOk Jeon

Jonathan D Macdonald

Jonathan J Mills

Jianhua Tian

Michael R Wood

Jolanta Grembecka

Tomasz Cierpicki

Edward T Olejniczak

Bruce J Melancon

Jason Phan

William P Tansey

Feng Wang

Sunil Kumar Upadhyay

Timothy J Senter

Patrick R Gentry

Evan P Lebois

Kevin B Teuscher

Isoquinolinone compounds and derivatives inhibit WDR5 and associated protein-protein interactions, and the compounds and their pharmaceutical compositions are useful for treating disorders and conditions in a subject, such as cancer cell proliferation.

WDR5 inhibitors and modulators

Described are imino-azacycle-benzamide compounds that inhibit WDR5 and associated protein-protein interactions, pharmaceutical compositions including the compounds, and methods of using the compounds and compositions for treating disorders and conditions in a subject.

Benzamides and picolinamides that are meta-substituted with imino-, guanidino-, or heterocycle-containing groups disrupt the WDR5-MLL1 protein-protein interaction, and have use in pharmaceutical compositions and in treating proliferative disorders and conditions in a subject, such as cancer.

WDR5-MLL1 inhibitors and modulators

Described are compounds that disrupt the WDR5-MLL1 protein-protein interaction, pharmaceutical compositions including the compounds, and methods of using the compounds and compositions for treating disorders and conditions in a subject.

The present invention relates generally to compounds that inhibit the binding of menin and MLL or MLL fusion proteins and methods of use thereof. In particular embodiments, the present invention provides compositions comprising piperidine-containing compounds and methods of use thereof to inhibit the interaction of menin with MLL oncoproteins (e.g., MLL1, MLL2, MLL-fusion oncoproteins), for example, for the treatment of leukemia, solid cancers, diabetes, and other diseases dependent on activity of MLL1, MLL2, MLL fusion proteins, MLL-PTD and/or menin.

Menin-MLL inhibitors and methods of use thereof

Heterocyclic sulfone compounds which are useful as allosteric potentiators/positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4); and methods of using the compounds, for example, in treating neurological and psychiatric disorders or other disease state associated with glutamate dysfunction.

Heterocyclic sulfone mGluR4 allosteric potentiators, compositions, and methods of treating neurological dysfunction

Pyrazole compounds 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 state associated with glutamate dysfunction.

mGluR4 allosteric potentiators, compositions, and methods of treating neurological dysfunction

Pyrazolopyridine, pyrazolopyrazine, pyrazolopyrimidine, pyrazolothiophene and pyrazolothiazole 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 state associated with glutamate dysfunction.

Pyrazolopyridine, pyrarolopyrazine, pyrazolopyrimidine, pyrazolothiophene and pyrazolothiazole compounds as MGLUR4 allosteric potentiators, compositions, and methods of treating neurological dysfunction

Pyrazolopyridine, pyrazolopyrazine, pyrazolopyrimidine, pyrazolothiophene and pyrazolothiazole compounds as MGLUR4 allosteric potentiators, compositions, and methods of treating neurological dysfunction

Compounds useful as allosteric potentiators/positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4) and use thereof.

MGLUR4 allosteric potentiators, compositions, and methods of treating neurological dysfunction

In one aspect, the invention relates to compounds having a general structure: which are useful as selective allosteric or bitopic agonists of the Mmuscarinic receptor; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds, for example, in treating neurodegenerative diseases, including Alzheimer's Disease. 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.

Alkyl 3-((2-amidoethyl)amino)-8-azabicyclo[3.2.1]octane-8-carboxylate analogs as selective M1 agonists and methods of making and using same

Compounds useful as allosteric potentiators/positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4) and methods of using the compounds.

Substituted 1,1,3,1-tetraoxidobenzo[D][1,3,2]dithiazoles as MGLUR4 allosteric potentiators, compositions, and methods of treating neurological dysfunction

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Kingston Springs, TN, United States of America

Rocco D Gogliotti