Publication number: 20240216513
Abstract: Described herein are fatty acid-bifunctional degrader compounds, their various targets, their preparation, pharmaceutical compositions comprising them, and their use in the treatment of conditions, diseases, and disorders mediated by various target proteins.
Type:
Application
Filed:
March 10, 2022
Publication date:
July 4, 2024
Inventors:
Claire Adcock, Valerie Broennimann, Jiashun Cheng, Rohit Kumar Duvadie, Tanzina Fazal, Jinhai Gao, Fengfeng Guo, Robert Martin Grotzfeld, Christina Hebach, Gregory John Hollingworth, Darryl Brynley Jones, Alexei Karpov, Jialiang Li, Julien Lorber, Chester A. Metcalf, III, Walter Michael, Mark Gabriel Palermo, Scott Vaughan Plummer, James Harold Roache, Martin Sendzik, Ranny Mathew Thomas, Aimee Richardson Usera, Anna Vulpetti, Frederic Zecri, Liang Zhao, Thomas Zoller
Publication number: 20240066132
Abstract: The invention provides a conjugate comprising a biomolecule linked to a fatty acid via a linker wherein the fatty acid has the following Formulae A1, A2 or A3: wherein R1, R2, R3, R4, Ak, n, m and p are defined herein. The invention also relates to a method for manufacturing the conjugate of the invention such as GDF15 conjugate, and its therapeutic uses such as treatment or prevention of metabolic disorders or diseases, type 2 diabetes mellitus, obesity, pancreatitis, dyslipidemia, alcoholic and nonalcoholic fatty liver disease/steatohepatitis and other progressive liver diseases, insulin resistance, hyperinsulinemia, glucose intolerance, hyperglycemia, metabolic syndrome, hypertension, cardiovascular disease, atherosclerosis, peripheral arterial disease, stroke, heart failure, coronary heart disease, diabetic complications (including but not limited to chronic kidney disease), neuropathy, gastroparesis and other metabolic disorders.
Type:
Application
Filed:
July 14, 2023
Publication date:
February 29, 2024
Inventors:
David Weninger BARNES, Avirup BOSE, Alexandra Marshall BRUCE, Alokesh DUTTAROY, Chikwendu IBEBUNJO, Aaron KANTER, Louise Clare KIRMAN, Changgang LOU, Aimee Richardson USERA, Ken YAMADA, Jun YUAN, Frederic ZECRI
Publication number: 20210000964
Abstract: The invention provides a conjugate comprising a biomolecule linked to a fatty acid via a linker wherein the fatty acid has the following Formulae A1, A2 or A3: wherein R1, R2, R3, R4, Ak, n, m and p are defined herein. The invention also relates to a method for manufacturing the conjugate of the invention such as GDF15 conjugate, and its therapeutic uses such as treatment or prevention of metabolic disorders or diseases, type 2 diabetes mellitus, obesity, pancreatitis, dyslipidemia, alcoholic and nonalcoholic fatty liver disease/steatohepatitis and other progressive liver diseases, insulin resistance, hyperinsulinemia, glucose intolerance, hyperglycemia, metabolic syndrome, hypertension, cardiovascular disease, atherosclerosis, peripheral arterial disease, stroke, heart failure, coronary heart disease, diabetic complications (including but not limited to chronic kidney disease), neuropathy, gastroparesis and other metabolic disorders.
Type:
Application
Filed:
June 1, 2020
Publication date:
January 7, 2021
Inventors:
David Weninger BARNES, Avirup BOSE, Alexandra Marshall BRUCE, Alokesh DUTTAROY, Chikwendu IBEBUNJO, Aaron KANTER, Louise Clare KIRMAN, Changgang LOU, Aimee Richardson USERA, Ken YAMADA, Jun YUAN, Frederic ZECRI