Vanderbilt University

The Uab Research Foundation

National Institutes of Health, a Component of the US Dept. of Health & Human Services

University of Pennsylvania

Glaxosmithkline LLC

Boehringer Ingelheim International Gmbh

The United States of America,as Represented by the Secretary, Department of Health and Human Servic

Novartis Ag

Alex Gregory Waterson

Gary Allen Sulikowski

Kwangho Kim

Leonard M Neckers

Daniel Jason Urban

Victor M Darley-Usmar

Anton Simeonov

William J Moore

David Joseph Maloney

Ajit Jadhav

Xin Hu

Plamen P Christov

Laurence Zwiebel

Shyh Ming Yang

Kyle Ryan Brimacombe

Paul R Reid

Somnath Jana

Ian M Romaine

Chi V Dang

Bryan T Mott

Ganesh Rai Bantukallu

Jennifer L Kouznetsova

Robert William Taylor

Gregory M Pask

David C Rinker

Patrick L Jones

David Edward Uehling

Jason Phan

Qi Sun

Jason R Abbott

Craig William Lindsley

Stephen W Fesik

Matthew E Hall

Andrew Little

Scott Howard Dickerson

Matthias Treu

Andreas Gollner

Andreas Mantoulidis

Eric P Skaar

Michael C Burns

Joachim Broeker

Joseph Wendell Wilson

Kevin Kuntz

Kirk Stevens

Jianwen Cui

Robert Dale Hubbard

R Daniel Beauchamp

Brian Wilson

Ross P Holmes

Kimberly Petrov

Sam Ochieng

Kyle David Wood

John Knight

Tim Hodges

Christian Alan Paul Smethurst

Steve W Fesik

Jerry Leroy Adams

Mui Cheung

Shaun R Stauffer

Tobias Wunberg

Philip Anthony Harris

Neil W Johnson

Robert Anthony Mook

Juergen Ramharter

Xinrong Tian

James M Salovich

George Adjabeng

John Stellwagen

Changho Han

Kyle Allen Emmitte

Tara Renae Rheault

Jeffrey M Ralph

James Michael Salovich

Joseph R Alvarado

Douglas McCord Sammond

Jennifer Gabriel Badiang

John Brad Shotwell

Holly Kathleen Emerson

Jonathan D Macdonald

Kristen Elizabeth Nailor

William P Tansey

Ganesha Rai Bantukallu

Keith Hornberger

Stephon Cornell Smith

Neil Bifulco, Jr

Birgit Wilding

Julian Fuchs

Heinz Stadtmueller

Brendan Dutter

Gregory Schaaf

Erich W Baum

Ganesh Moorthy

J Phillip Kennedy

Pratiq Patel

Mul Cheung

Mariko Yamabe

Lorenz Herdeis

Kevin Sokol

Laura Anzaldi Mike

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

Provided is a compound of formula (I) in which Ar, R, U, V, W, X, and p are as described herein. Also provided are methods of using a compound of formula (I), including a method of treating cancer, a method of treating a patient with cancer cells resistant to an anti-cancer agent, and a method of inhibiting lactate dehydrogenase A (LDHA) and/or lactate dehydrogenase B (LDHB) activity in a cell.

Small molecule inhibitors of lactate dehydrogenase and methods of use thereof

The disclosure provides methods of treating a patient having primary hyperoxaluria or idiopathic hyperoxaluria comprising administering a therapeutically effective amount of compound of the formula and pharmaceutically acceptable salts, solvates, and hydrates thereof to the patient. The variables, e.g. ring A, n, R, R, R, X, Y, and Z are defined herein. These compounds act as lactate dehydrogenase inhibitors and are useful inhibiting the conversion of glyoxylate to oxalate. When administered to a patient having a disease or disorder associated with elevated oxalate levels, such as PH type 1, type 2, or type 3 or idiopathic hyperoxaluria the compounds prevent or substantially reduce the amount and buildup of oxalate the patient's kidneys, bladder, urinary tract and other parts of the patient's body.

Treating primary or idiopathic hyperoxaluria with small molecule inhibitors of lactate dehydrogenase

The present invention encompasses compounds of formula (I)

Annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer

The present invention encompasses compounds of formula (I) wherein R, R, R, R, Z, Rto R, A, p, U, V, W, L and E have the meanings given in the claims and specification, their use as inhibitors of mutant Ras family proteins, pharmaceutical compositions and preparations containing such compounds and their use as medicaments/medical uses, especially as agents for treatment and/or prevention of oncological diseases.

In one aspect, the invention relates to binary compositions that disrupt ORco-mediated odorant sensing. In particular, compounds and compositions are provided that can inhibit sensory (e.g., host targeting) functions in organisms that express ORco receptors such as airborne insects, e.g., mosquitos, and ticks. Methods of employing such agents, and articles incorporating the same, are also provided. 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.

Binary compositions as disruptors of Orco-mediated odorant sensing

The disclosure provides methods of treating a patient having primary hyperoxaluria or idiopathic hyperoxaluria comprising administering a therapeutically effective amound of compound of the formula and pharmaceutically acceptable salts, solvates, and hydrates thereof to the patient. The variables, e.g. ring A, n, R, R, R, X, Y, and Z are defined herein. These compounds act as lactate dehydrogenase inhibitors and are useful inhibiting the conversion of glyoxylate to oxalate. When administered to a patient having a disease or disorder associated with elevated oxalate levels, such as PH type 1, type 2, or type 3 or idiopathic hyperoxaluria the compounds prevent or substantially reduce the amount and buildup of oxalate the patient's kidneys, bladder, urinary tract and other parts of the patient's body.

In one aspect, the invention relates to chemical modulators of insect olfactory receptors. In particular, compounds and compositions are provided that can inhibit sensory (e.g., host targeting) functions in airborne insects such as mosquitos. Methods of employing such agents, and articles incorporating the same, are also provided. 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.

Compositions for inhibition of insect sensing

The present invention relates to quinazoline compounds and compositions that modulate Ras signaling. Compounds and compositions of the present invention are useful in the treatment of cancers and other disease states associated with Ras dysfunction (e.g., Ras-associated autoimmune leukoproliferative disorder, or certain types of mitochondrial dysfunction) in a subject, for example a mammal or a human.

Quinazoline compounds as modulators of Ras signaling

Provided is a compound of formula (I), in which Ar, R, U, V, W, X, and p are as described herein. Also provided are methods of using a compound of formula (I), including a method of treating cancer, a method of treating a patient with cancer cells resistant to an anti-cancer agent, and a method of inhibiting lactate dehydrogenase A (LDHA) and/or lactate dehydrogenase B (LDHB) activity in a cell.

The disclosure provides a compound of the formula (II) and pharmaceutically acceptable salts thereof. The variables, e.g. n, R, R, R, X, Y, and Z are defined herein. These compounds act as lactate dehydrogenase inhibitors and are useful for treating cancer and fibrosis. The compounds may be particularly useful for treating forms of cancer in which a metabolic switch from oxidative phosphorylation to glycolysis has occurred. The disclosure also provides pharmaceutical compositions containing a compound of this formula and method for treating patients having cancer, fibrosis, or other conditions in which a metabolic switch from oxidative phosphorylation to glycolysis has occurred. 

1 H-pyrazol-1-yl-thiazoles as inhibitors of lactate dehydrogenase and methods of use thereof

In one aspect, the invention relates to chemical modulators of insect olfactory receptors. In particular, compounds and compositions are provided that can inhibit sensory (e.g., host targeting) functions in airborne insects such as mosquitoes. Methods of employing such agents, and articles incorporating the same, are also provided. 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.

In one aspect, the invention relates to binary compositions that disrupt ORco-mediated odorant sensing. In particular, compounds and compositions are provided that can inhibit sensory (e.g., host targeting) functions in organisms that express ORco receptors such as airborne insects, e.g., mosquitoes, and ticks. Method of employing such agents, and articles incorporating the same, are also provided. 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.

Binary compositions as disruptors of orco-mediated odorant sensing

Growing community of inventors

Murfreesboro, TN, United States of America

Alex Gregory Waterson