University of Michigan

Metabolic Solutions Development Company, LLC

Michigan State University

The United States Government As Represented by the Department of Veterans Affairs

University of Missouri

Indiana University

Wayne State University

The University of Bath

Cirius Therapeutics, Inc.

Octeta Therapeutics, LLC

Scott D Larsen

Steven Paul Tanis

Hollis Showalter

Alan Robert Saltiel

Timothy Parker

James A Shayman

Michael William Wilson

James Robert Zeller

Richard Neubig

Kim Hutchings

Gerald D Artman, Iii

Robert C Gadwood

David Ginsburg

Gerard R Colca

Akira Abe

Ronald J Buckanovich

Hongmin Sun

John J G Tesmer

Bryan Yestrepsky

Kun Yang

Helen Waldschmidt

Kristoff Homan

Liming Shu

Richard F Keep

Erika Mathes Lisabeth

Gerald D Artman

James R Zeller

Neil Moss

Duxin Sun

Emily Elizabeth Freeman

Qin Jiang

David J Miller

Stephen Husbands

Daniel H Teitelbaum

Nicholas James Mayhew

Rolf F Kletzien

Arun Rishi

Levi Lynn Blazer

Hiroyuki Koga

Walajapet Rajeswaran

Dinesh Khanna

John Traynor

Janice Sindac

Scott Barraza

Peter Lucas

Hollis D Showalter

Brandt C Huddle

Thomas Hurley

Dylan Kahl

Zohreh Sajjadi Hashemi

Andrew Haak

John JG Tesmer

Gerald D Iii Artman

This invention is in the field of medicinal chemistry. In particular, the invention relates to a new class of small-molecules having a thiopyrimidinone structure which function as inhibitors of ALDH protein, and their use as therapeutics for the treatment of cancer and other diseases.

Small molecule inhibitors of ALDH and uses thereof

Glucosylceramide synthase inhibitors and compositions containing the same are disclosed. Methods of using the glucosylceramide synthase inhibitors in the treatment of diseases and conditions wherein inhibition of glucosylceramide synthase provides a benefit, like Gaucher disease and Fabry disease, also are disclosed.

Glucosylceramide synthase inhibitors and therapeutic methods using the same

Disclosed herein are inhibitors of Rho/MRTF/SRF-mediated gene transcription, and methods for their use in treating or preventing diseases such as cancer and fibrosis. In particular, disclosed herein are compounds of Formula (I) and pharmaceutically acceptable salts thereof: wherein the substituents are as described.

Inhibitors of Rho/MRTF/SRF-mediated gene transcription and methods for use of the same

Disclosed herein are inhibitors of gene transcription mediated by myocardin-related transcription factor and serum response factor, or both myocardin-related transcription factor and serum response factor ('MRTF/SRF'), and methods for their use in treating or preventing cancer and fibrosis. In particular, disclosed herein are compounds of Formula (I) and Formula (II), and pharmaceutically acceptable salts thereof: wherein the substituents are as described.

Inhibitors of myocardin-related transcription factor and serum response factor (MRTF/SRF)-mediated gene transcription and methods for use of the same

Provided herein is technology relating to deuterated amlexanox and particularly, but not exclusively, to compositions comprising deuterated amlexanox, methods of producing deuterated amlexanox, and uses of deuterated amlexanox.

Deuterated amlexanox

Disclosed herein are novel GRK inhibitors and methods for their use in treating or preventing heart disease, such as cardiac failure, cardiac hypertrophy, and hypertension. In particular, disclosed herein are compounds of Formula (I) and pharmaceutically acceptable salt thereof, wherein the substituents are as described. 

G protein-coupled receptor kinase inhibitors and methods for use of the same

Disclosed herein are novel GRK2 inhibitors and methods for their use in treating or preventing heart disease, such as cardiac failure, cardiac hypertrophy, and hypertension. In particular, disclosed herein are compounds of Formula (I) and pharmaceutically acceptable salt thereof: wherein the substituents are as described. 

G protein-coupled receptor kinase 2 inhibitors and methods for use of the same

The invention provides compounds of formula I: and salts thereof. The invention also provides pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I and therapeutic methods for treating cancer using compounds of formula I. 

Therapeutic compounds and methods

The present invention relates to hydroxamate compounds and pharmaceutical compositions that are useful for treating and/or preventing metabolic inflammation mediated diseases such as diabetes, obesity, hypertension, dyslipidemia, a neurodegenerative disorder (e.g., Alzheimer's disease, Parkinson's disease, or Huntington's disease), or any combination thereof. Moreover, the present invention also provides methods of treatment for these diseases or disorders.

PPAR-sparing compounds for the treatment of metabolic diseases

The present invention relates to chemical compounds, methods for their discovery, and their therapeutic and research use. In particular, the present invention provides compounds as therapeutic agents against bacterial infections (e.g., biofilms).

Methods and compositions for treating bacterial infection

The present invention relates to chemical compounds, methods for their discovery, and their therapeutic and research use. In particular, the present invention provides compounds as therapeutic agents against cancer stem cells.

Methods and compositions for targeting cancer stem cells

Provided herein is technology relating to deuterated amiexanox and particularly, but not exclusively, to compositions comprising deuterated amiexanox, methods of producing deuterated amiexanox, and uses of deuterated amiexanox. Provided herein are deuteratecl amiexanox compounds for the treatment of obesity, insulin resistance, diabetes, and steatosis. In addition, the deuterated compounds are anti-inflammatory antiallergic immunomodulators. e.g., for the treatment of diseases associated with inflammation. The deuterium kinetic isotope effect associated with placing deuterium at the site of metabolic derivatization slows metabolic derivatization and thus increases the lifetime of the active drug in vivo.

The present invention relates to novel salts of thiazolidinediones and other pharmaceutical agents that are useful for treating and/or preventing metabolic diseases (e.g., diabetes, or neurodegenerative diseases (e.g., Alzheimer's Disease).

PPAR-sparing thiazolidinedione salts for the treatment of metabolic diseases

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South Lyon, MI, United States of America

Scott D Larsen