Novo Nordisk A/s

Indiana University

Helmholtz Zentrum Munchen Deutsches Forschungszentrum Fur Gesundheit Und Umwelt

Brian Finan

Richard Dennis DiMarchi

Jesper F Lau

Henning Thoegersen

Steffen Reedtz-Runge

Bin Yang

Henning Thøgersen

Patrick J Knerr

Nicholas Cox

Fa Liu

Wouter Frederik Johan Hogendorf

Timo Dirk Mueller

Matthias Tschoep

Christoffer Clemmensen

Richard Dimarchi

Nicholas Raymond Cox

Richard D Dimarchi

Prodrug compounds of GLP-1/GIP receptor co-agonists are provided wherein the GLP-1/GIP receptor co-agonists have been modified by the linkage of a dipeptide to the GLP-1/GIP receptor co-agonist through an amide bond. The prodrugs disclosed herein have extended half-lives and are converted to the active GLP-1/GIP receptor co-agonist at physiological conditions through a non-enzymatic reaction driven by chemical instability.

Prodrugs and uses thereof

Peptide co-agonists of the human GLP-1 and GIP receptors suitable for oral delivery, including long-acting derivatives, and their medical use in treatment and/or prevention of obesity, diabetes, and/or liver diseases are described.

Co-agonists at GLP-1 and GIP receptors suitable for oral delivery

The present invention relates to novel peptides that are derivatives of glucose-dependent insulinotropic polypeptide (GIP) analogues having improved physical stability in solution and a protracted profile of action. More particular the invention relates to such peptides that are agonists at the GIP receptor and to their use in weight management or for treatment of diseases such as obesity, diabetes or non-alcoholic steatohepatitis (NASH).

GIP derivatives and uses thereof

The present invention relates to novel peptides that are derivatives of glucose-dependent insulinotropic polypeptide (GIP) analogues having improved physical stability in solution and a protracted profile of action. More particularly the invention relates to such peptides that are agonists at the GIP receptor and to their use in weight management or for treatment of diseases such as obesity, diabetes or non-alcoholic steatohepatitis (NASH). The peptides comprise a lysine residue at a position corresponding to position 24 of hGIP(1-31), and comprise a negatively charged modifying group attached to the epsilon amino group of the lysine residue.

The present invention relates to compositions comprising at least two different active compounds and the use of such combination compositions in medicine, in particular in methods for treating obesity and obesity-related disorders and/or in methods for inhibiting weight gain.

Combination compositions and their use in methods for treating obesity and obesity-related disorders

Provided herein are glucagon superfamily peptides conjugated with NHR ligands that are capable of acting at a nuclear hormone receptor. Also provided herein are pharmaceutical compositions and kits of the conjugates of the invention. Further provided herein are methods of treating a disease, e.g., a metabolic disorder, such as diabetes and obesity, comprising administering the conjugates of the invention.

Glucagon superfamily peptides exhibiting nuclear hormone receptor activity

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Indianapolis, IN, United States of America

Brian Finan