Vanderbilt University

Merck Sharp + Dohme Corp.

Merck + Co., Inc.

Sunesis Pharmaceuticals, Inc.

University of Michigan

Shaun R Stauffer

Craig William Lindsley

P Jeffrey Conn

Philippe G Nantermet

Susana Conde-Ceide

Harold G Selnick

Hemaka Anthony Rajapakse

Craig Alan Coburn

Gregor James MacDonald

Stephen W Fesik

José Manuel Bartolomé-Nebreda

Carrie K Jones

Han Min Tong

James C Barrow

Rocco D Gogliotti

Georgia B McGaughey

Shawn J Stachel

Changho Han

Joseph R Alvarado

José Ignacio Andrés-Gil

Manuel Jesús Alcázar-Vaca

Ya Zhou

Joseph David Panarese

Kenneth M Meyers

Jonathan D Macdonald

William P Tansey

Jason Manka

Joseph P Vacca

Matthew G Stanton

Samuel L Graham

Melissa S Egbertson

Wenjin Yang

James M Salovich

Edward T Olejniczak

Kayla J Temple

Keith P Moore

Jason Phan

KyuOk Jeon

Bruce Fahr

Wanli Lu

Ashley Nomland

Heidi E Hamm

Matthew T Duvernay

Miguel Angel Pena-Piñón

Gregor McDonald

Feng Wang

Jonathan J Mills

José Manuel Bartolome-Nebreda

Jianhua Tian

Jon Jacobs

Linghang Zhuang

Daniel Vincent Paone

Christopher S Burgey

Jolanta Grembecka

Tomasz Cierpicki

Alex Gregory Waterson

M Katharine Holloway

Zhengwu James Deng

Diem N Nguyen

Lou Anne Neilson

Manuel Jesus Alcazar Vaca

Kenneth E Rittle

Zhi-Qiang Yang

Melody McWherter

Craig M Potteiger

Jennifer R Davis

Mary Beth Young

John Jin Lim

Ivory D Hills

Sameer S Nikhar

Kevin B Teuscher

Alexey Kuznetsov

Selena Chacon Simon

Carolyn Segerdell

Gregor Macdonald

Wandong Wen

Sunil Kumar Upadhyay

Timothy J Senter

Gregor James Macdonald

Summer E Young

Mattahew G Stanton

Chrysa Malosh

Eric S Dawson

Zhengwu J Deng

Hemaka A Rajapakse

Georgia B Mcgaughey

John J Lim

Melody A Mcwherter

Shawn R Stachel

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

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 N-(6-(6,7-dihydro-5H-pyrrolo[1,2-a]imidazol-2-yl)-2,3-dihydro-1H-inden-1-yl)benzamide and acetamide-containing 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.

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.

Embodiments of the invention include compounds and compositions thereof to inhibit protease activated receptor-4. Also described are methods of preparation of compositions and methods for treating diseases related to thrombotic disorders by administration of the composition.

Substituted 5-membered heterocyclic analogs as protease activated receptor 4 (PAR-4) antagonists

In one aspect, the invention relates to N-substituted 3,4-dihydro-benzo[&#xa3;][1,4]oxazine-2-carboxamide analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M(mAChR M); synthesis methods for 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. 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.

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Embodiments of the invention include substituted indole compounds and compositions thereof to inhibit protease activated receptor-4. Also described are methods of preparation of compositions and methods for treating diseases related to thrombotic disorders by administration of the composition.

Substituted indoles as selective protease activated receptor 4 (PAR-4) antagonists

In one aspect, the invention relates to 3-benzylquinazolin-4(3H)-one analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M(mAChR M); synthesis methods for 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. 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. Exemplary 3-benzylquinazolin-4(3H)-one compounds include compounds of formula (I): 

Substituted quinazolin-4(3H)-ones, pyrido[3,4-d]pyrimidin-4(3H)-ones, pyrido[3,2-d]pyrimidin-4(3H)-ones and pyrido[2,3-d]pyrimidin-4(3H)-ones as positive allosteric modulators of muscarinic acetycholine receptor M1

The invention relates to substituted 1-benzylquinoxalin-2(1H)-one analogs, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M(mAChR M); methods for making the compounds; pharmaceutical compositions; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction. Exemplary 1-benzylquinoxalin-2(1H)-one compounds include compounds of the following formula: 

Substituted 1-benzylquinoxalin-2(1H)-one analogs as positive allosteric modulators of muscarinic acetylcholine receptor M1

In one aspect, the invention relates to substituted pyrazolo[1,5-a]pyrazines analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. 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.

Substituted pyrazolo[1,5-a]pyrazines as mGluR5 receptor modulators

The subject invention relates to novel P2X3 receptor antagonists that play a critical role in treating disease states associated with pain, in particular peripheral pain, inflammatory pain, or tissue injury pain that can be treated using a P2X3 receptor subunit modulator.

P2X3 receptor antagonists for treatment of pain

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

In one aspect, the invention relates to novel bicyclic oxazole and thiazole compounds which are positive allosteric modulators of the metabotropic glutamate receptor subtype 5 ('mGluR5'); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions; and methods for the treatment or prevention of disorders associated with glutamate dysfunction and diseases in which the mGluR5 subtype of receptors is involved. 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.

Bicyclic oxazole and thiazole compounds and their use as allosteric modulators of mGluR5 receptors

Growing community of inventors

Brentwood, TN, United States of America

Shaun R Stauffer