Vanderbilt University

Purdue Research Foundation

Changho Han

Shaun R Stauffer

Stephen W Fesik

Joseph R Alvarado

Craig William Lindsley

P Jeffrey Conn

Taekyu Lee

Rocco D Gogliotti

Kenneth M Meyers

Jonathan D Macdonald

Aaron M Bender

Jonathan J Mills

Jianhua Tian

Darren W Engers

Alex Gregory Waterson

Andrew S Felts

Carrie K Jones

Julie L Engers

Kyle A Emmitte

James M Salovich

Thomas M Bridges

KyuOk Jeon

William P Tansey

David A Colby

Mark V Riofski

Matthew Spock

Selena Chacon Simon

Kevin B Teuscher

Sameer S Nikhar

Alexey Kuznetsov

Substituted N-phenyl sulfonamide compounds inhibit WDR5-MYC interactions, and the compounds and their pharmaceutical compositions are useful for treating disorders and conditions in a subject, such as cancer cell proliferation.

WDR5-MYC inhibitors

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 M4

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

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.

Positive allosteric modulators of the muscarinic acetylcholine receptor M4

Substituted pyrrolopyridine, imidazopyridine and triazolopyridine compounds having a formula are positive allosteric modulators of the muscarinic acetylcholine receptor M(mAChR M) and the compounds and their pharmaceutical compositions may be useful in treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction. Compounds of the invention may be prepared in several steps from 2-halo-5,6-dihydro-7H-pyrrolo[3,4-b]pyridin-7-one intermediates.

Substituted pyrrolo[3,4-e]indolizines, imidazo[1,2-a]pyrrolo[3,4-e]pyridines, pyrrolo[3,4-e][1,2,4]triazolo[1,5-a]pyridines and pyrrolo[3,4-e][1,2,4]triazolo[4,3-a]pyridines as positive allosteric modulators of muscarinic acetylcholine receptor M1

The present invention relates to compositions, for example, the DBU/Hexafluoroacetone hydrate salt, and processes of preparing and using the same for the modification of chemical compounds via the release of trifluoroacetate. The DBU/Hexafluoroacetone hydrate salt can perform trifluoromethylation reactions on chemical compounds, such as carbonyl group-containing compounds.

Compositions and processes of preparing and using the same

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Nashville, TN, United States of America

Changho Han