Infinity Pharmaceuticals, Inc.

Srx Cardio, LLC

Vesa Nevalainen

Alfredo C Castro

Stephane Peluso

Thomas T Tibbitts

Gregg F Keaney

Marta Nevalainen

Lawrence K Chan

Adilah Bahadoor

Daniel A Snyder

Thomas E Barta

Michael Mark Muehlemann

Jonathan William Bourne

Kyle D Monroe

Eric T Baldwin

Margaret Thompson Reece

This invention is related to the field of hypercholesterolemia. In particular, the invention provides compositions and methods to modulate circulating levels of low density lipoproteins by altering the conformation of the protein PCSK9 using synthetic ligands and/or synthetic ligand derivative sequences of 3-8 amino acids ranging between 350-2,000 Da. Altering the conformation of PCSK9 affects the interaction between PCSK9 and an endogenous low density lipoprotein receptor, and can lead to reduced or increased levels of circulating LDL-cholesterol. High LDL-cholesterol levels are associated with increased risk for heart disease. Low LDL-cholesterol levels may be problematic in other conditions, such as liver dysfunction; thus, there is also utility for ligands which can raise LDL levels.

Proprotein convertase subtilisin kexin type 9 (PCSK9) allosteric binding ligands to modulate serum low density lipoprotein (LDL) levels

Provided herein are tetrazolone FASN inhibitors of the formula (I): or a pharmaceutically acceptable form thereof; wherein the variables R, Rand Rare defined herein. Also provided herein are pharmaceutical compositions of the compounds provided herein as well as methods of their use for the treatment of various disorders such as hyperproliferative disorders, inflammatory disorders, obesity-related disorders and microbial infections.

Tetrazolones as inhibitors of fatty acid synthase

Provided herein are triazole FASN inhibitors of the formula (I): or a pharmaceutically acceptable form thereof; wherein the variables R, X, R, and Rare defined herein. Also provided herein are pharmaceutical compositions of the compounds provided herein as well as methods of their use for the treatment of various disorders such as hyperproliferative disorders, inflammatory disorders, obesity-related disorders and microbial infections.

Triazoles as inhibitors of fatty acid synthase

Growing community of inventors

Weymouth, MA, United States of America

Vesa Nevalainen