Novo Nordisk A/s

Steffen Reedtz-Runge

Jesper F Lau

Henning Thoegersen

Jane Spetzler

Patrick William Garibay

Thomas Kruse

Ingrid Pettersson

Jacob Kofoed

Christian Wenzel Tornoee

Lauge Schaeffer

Richard Dennis DiMarchi

Per Sauerberg

Brian Finan

Patrick J Knerr

Nicholas Cox

Fa Liu

Wouter Frederik Johan Hogendorf

Janos Tibor Kodra

Kjeld Madsen

Ulrich Sensfuss

Henning Thøgersen

Soeren Oestergaard

Thomas Egebjerg

Jais Rose Bjelke

Philip Jonas Sassene

Lennart Lykke

Lauge Schäffer

Anne Louise Bank Kodal

Emma Balantic-Nielsen

Che Yang

Katharina Luise Maria Kopp

Nicholas Raymond Cox

Christian Wenzel Tornøe

Richard Dimarchi

Christian Wenzel TORNØE

Henning THØGERSEN

Christian Wenzel Tornoe

The present invention relates to compounds (e.g. ISVDs, polypeptides, polypeptide derivatives) capable of binding to Interleukin-6 (IL-6) and their use in the treatment of inflammatory diseases such as, e.g. cardiovascular disease (CVD).

Anti IL-6 domain antibodies with fatty acid substituents

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 application discloses compounds useful in treatment of diabetes, weight loss and/or reduction of cardiovascular risks. The compounds are bi-functional and therefore suitable as a simple treatment for patients that may benefit from treatment with both a GLP-1 receptor agonist and a PCSK9 inhibitor.

Bifunctional compounds

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 invention relates to a derivative of a GLP-1 analogue, optionally C-terminally extended, which derivative comprises a first and a second protracting moiety in the form of a C20 or C22 diacid radical, a bis-amino branched linker, and a first and a second further linker each comprising an OEG-like linker element; wherein these elements are interconnected via amide bonds and attached to a Lys residue of the GLP-1 analogue. The invention also relates to intermediate products in the form of novel GLP-1 analogues incorporated in the derivatives of the invention, as well pharmaceutical compositions and medical uses of the derivatives. The derivatives have very long half-lives while maintaining a satisfactory potency, which makes them potentially suitable for once-monthly administration.

GLP-1 derivatives and uses thereof

The invention relates to derivatives of GLP-1 like peptides which are C-terminally extended analogs of native GLP-1. The derivatives comprise two side chains, one at a position corresponding to position 42, and one at a position corresponding to position 18, 23, 27, 31, 36, or 38, wherein both positions are when compared to GLP-1(7-37). The side chains comprise a C19, C20, or C22 diacid protracting moiety and optionally a linker. The invention also relates to intermediate products in the form of novel GLP-1 analogs incorporated in the derivatives of the invention, as well as pharmaceutical compositions and medical uses of the derivatives. The derivatives have very long half-lives while maintaining a satisfactory potency, which makes them potentially suitable for once-monthly administration.

Derivatives of GLP-1 like peptides, and uses thereof

New GLP-1 derivatives, compositions thereof and their use in medicine.

Stable GLP-1 based GLP-1/glucagon receptor co-agonists

The invention relates to truncated GLP-1 analogs, in particular a GLP-1 analog which is a modified GLP-1(7-35) (SEQ ID No 1) having: i) a total of 2, 3, 4, 5 6, 7, 8, or 9 amino acid substitutions as compared to GLP-1(7-35), including a) a Glu residue at a position equivalent to position 22 of GLP-1(7-35), and b) an Arg residue at a position equivalent to position 26 of GLP-1(7-35); as well as derivatives thereof, and therapeutic uses and compositions. These analogs and derivatives are highly potent, have a good binding affinity to the GLP-1 receptor, also to the extracellular domain of the GLP-1 receptor, which is of potential relevance achieving long-acting, stable GLP-1 compounds with a potential for once weekly administration.

Truncated GLP-1 derivatives and their therapeutical use

The invention relates to protracted Glucagon-Like Peptide-1 (GLP-1) derivatives and therapeutic uses thereof. The GLP-1 derivative of the invention comprises a modified GLP-1(7-37) sequence having a total of 2-12 amino acid modifications, including Glu22 and Arg26, and being derivatised with an albumin binding residue or pegylated in position 18, 20, 23, 30, 31, 34, 36, 37, or 39. These compounds are useful in the treatment or prevention of diabetes type 2 and related diseases. The compounds are potent, stable, have long half-lives, a high affinity of binding to albumin, and/or a high affinity of binding to the extracellular domain of the GLP-1 receptor (GLP-1R), all of which is of potential relevance for the overall aim of achieving long-acting, stable and active GLP-1 derivatives with a potential for once weekly administration.

Glucagon-like peptide-1 derivatives and their pharmaceutical use

The invention relates to protracted peptide derivatives such as Glucagon-Like Peptide-1 (GLP-1), exendin-4, and analogs thereof, as well as therapeutic uses thereof. The peptide derivative of the invention comprises a peptide wherein at least one amino acid residue is derivatized with A-B-C-, or A-B-C-D-. These compounds are useful in the treatment or prevention of diabetes type 2 and related diseases. The compounds are potent, have a low ratio of binding affinity to the GLP-1 receptor in the presence of high/low albumin concentrations, have long half-lives, and have a high affinity of binding to albumin, all of which is of potential relevance for the overall aim of achieving long-acting, stable and active GLP-1 derivatives with a potential for once weekly administration.

Peptides derivatized with A-B-C-D- and their therapeutical use

Glucagon-Like Peptide-1 derivatives and their pharmaceutical use

Growing community of inventors

Bikeroed, Denmark

Steffen Reedtz-Runge