Novo Nordisk A/s

Ziylo Limited

Thomas Kruse

Jesper F Lau

Henning Thoegersen

Lauge Schaeffer

Jane Spetzler

Ulrich Sensfuss

Patrick William Garibay

Jacob Kofoed

Per Sauerberg

Lars Linderoth

Thomas Hoeg-Jensen

Steffen Reedtz-Runge

Peter Kresten Nielsen

Kirsten Dahl

Carsten Behrens

Miroslav Havranek

Birgit Wieczorek

Mikael Kofod-Hansen

Martin Werner Borchsenius Muenzel

Ivan Snajdr

Ladislav Droz

Kirsten Raun

Michael Ankersen

Ingrid Pettersson

Janos Tibor Kodra

Bernd Peschke

Anthony Murray

Kjeld Madsen

Henning Thøgersen

Paw Bloch

Asser Sloth Andersen

Claus Ulrich Jessen

Soeren Oestergaard

Christian Poulsen

Jens Christian Norrild

János Tibor Kodra

Christian Wenzel Tornoee

Christine Bruun Schiødt

Vojtech Balsanek

Zuzana Drobnakova

Vladislav Kotek

Milan Stengl

Hana Drusanova

Lauge Schäffer

Jakob Ewald Rasmussen

Alice Ravn Madsen

Inga Sig Nielsen Nørby

Caspar Christensen

Anthony Davis

Jakob Ewald

Andrew Michael Chapman

Anette Sams Nielsen

Søren Østergaard

Jesper Færgeman Lau

Henning THØGERSEN

Cecilie Mia Joergensen

Cecilia Nilsson

Birgit Richter

Birgit Richter, Legal Representative

Steffen Runge

Birgit Wiezorek

Inga Sig Nielsen NØRBY

Christian Wenzel TORNØE

Lauge SCHÄFFER

Miroslav HAVRÁNEK

Hana VÁNOVÁ

Zuzana DROBNÁKOVÁ

Vojtech BALSÁNEK

Mikael Kofoed Hansen

Martin Werner Borchsenius MÜNZEL

Thomas HØEG-Jensen

Florencio Zaragoza Dörwald

This invention relates to glucose-sensitive albumin-binding diboron conjugates. More particularly the invention provides novel diboron compounds, and in particular diboronate or diboroxole compounds, useful as intermediate compounds for the synthesis of diboron conjugates.

Glucose-sensitive albumin-binding derivatives

The invention relates to a compound comprising an amylin receptor agonist. The invention also relates to a pharmaceutical composition, suitable for but not limited to oral administration, which comprises such a compound. The compound and pharmaceutical composition comprising it may be used for the medical treatment of subjects with overweight, obesity and associated co-morbidities.

Amylin receptor agonists

The invention relates to a compound comprising a GLP-1 receptor agonist and an amylin receptor agonist. The invention also relates to a pharmaceutical formulation, suitable for but not limited to oral administration, which comprises such a compound. The compound and pharmaceutical formulation comprising it may be used for the medical treatment of subjects with overweight, obesity and associated co-morbidities.

Co-agonists of the GLP-1 and amylin receptors

The present invention provides glucose sensitive insulin derivatives comprising a macrocycle, a glucose mimetic and human insulin or an analogue thereof, and their pharmaceutical use. Furthermore, the invention relates to pharmaceutical compositions comprising such glucose sensitive insulin derivatives, and to the use of such compounds for the treatment or prevention of medical conditions relating to diabetes.

Glucose sensitive insulins and uses thereof

This invention relates to glucose-sensitive albumin-binding diboron conjugates. More particularly the invention provides novel diboron compounds, and in particular diboronate or diboroxole compounds, useful as intermediate compounds for the synthesis of diboron conjugates. The diboron compounds are characterized by formula (I), which is: R1-X&#x2014;R2, and wherein 'X' is a mono- to multiatomic linker and where Rand R, which may be identical or different, each represents a group of Formula (11a) or (IIb) Also described are diboron conjugates represented by the general Formula (I'), which is: R1&#x2032;-X&#x2032;&#x2014;R2&#x2032;, in which either the moeities R1&#x2032; or R2&#x2032; or X&#x2032; carry a drug that is covalently attached to the diboron compound.

The invention relates to a derivative of a GLP-1 analogue, which analogue comprises a first K residue at a position corresponding to position 27 of GLP-1(7-37) (SEQ ID NO: 1); a second K residue at a position corresponding to position T of GLP-1(7-37), where T is an integer in the range of 7-37 except 18 and 27; and a maximum of ten amino acid changes as compared to GLP-1(7-37); wherein the first K residue is designated K, and the second K residue is designated K; which derivative comprises two albumin binding moieties attached to Kand K, respectively, via a linker, wherein the albumin binding moiety comprises a protracting moiety selected from HOOC&#x2014;(CH)&#x2014;CO&#x2014; and HOOC&#x2014;CH&#x2014;O&#x2014;(CH)&#x2014;CO&#x2014;; in which x is an integer in the range of 6-16, and y is an integer in the range of 3-17; wherein the linker comprises an element of the formula &#x2014;NH&#x2014;(CH)&#x2014;(O&#x2014;(CH))&#x2014;O&#x2014;(CH)&#x2014;CO&#x2014;, wherein k is an integer in the range of 1-5, and n is an integer in the range of 1-5; or a pharmaceutically acceptable salt, amide, or ester thereof. The invention also relates to the pharmaceutical use thereof, for example in the treatment and/or prevention of all forms of diabetes and related diseases, as well as to corresponding novel GLP-1 analogues. The derivatives are suitable for oral administration.

Double-acylated GLP-1 derivatives

The present invention relates to novel glucagon derivatives which are GLP-1/glucagon receptor co-agonists, and to the use of the glucagon derivatives in medicine, such as in the treatment of diabetes, obesity and related diseases and conditions.

GLP-1/glucagon receptor co-agonists for medical use

The present invention relates to peptides comprising an amino acid sequence SEQ ID NO: 1 (EASELSTAALGRLSAELHELATLPRTETGPESP), analogs and derivatives thereof and pharmaceutical compositions comprising such peptides and derivatives. This invention further regards the use of these peptides according to SEQ ID NO: 1, analogs and derivatives thereof as medicaments.

Amylin and calcitonin receptor agonist

The invention relates to a derivative of a GLP-1 analog, which analog comprises a first K residue at a position corresponding to position 27 of GLP-1(7-37) (SEQ ID NO: 1); a second K residue at a position corresponding to position T of GLP-1(7-37), where T is an integer in the range of 7-37 except 18 and 27; and a maximum of ten amino acid changes as compared to GLP-1(7-37); wherein the first K residue is designated K, and the second K residue is designated K; which derivative comprises two albumin binding moieties attached to Kand K, respectively, via a linker, wherein the albumin binding moiety comprises a protracting moiety selected from HOOC&#x2014;(CH)&#x2014;CO&#x2014; and HOOC&#x2014;CH&#x2014;O&#x2014;(CH)&#x2014;CO&#x2014;; in which x is an integer in the range of 6-16, and y is an integer in the range of 3-17; wherein the linker comprises an element of the formula &#x2014;NH&#x2014;(CH)&#x2014;(O&#x2014;(CH))&#x2014;O&#x2014;(CH)&#x2014;CO&#x2014;, wherein k is an integer in the range of 1-5, and n is an integer in the range of 1-5; or a pharmaceutically acceptable salt, amide, or ester thereof. The invention also relates to the pharmaceutical use thereof, for example in the treatment and/or prevention of all forms of diabetes and related diseases, as well as to corresponding novel GLP-1 analogs. The derivatives are suitable for oral administration.

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 derivatives of glucagon analogs comprising the substitutions Imp1 and His3, a substituent having three to ten negatively charged moieties covalently attached to a side chain of a lysine as well as intermediates and compositions thereof and their use in medicine.

Stable glucagon analogues and use for treatment of hypoglycaemia

The invention relates to novel stable and protracted GLP-1/glucagon receptor co-agonists, to the use of said peptides in therapy, to methods of treatment comprising administration of said peptides to patients, and to the use of said peptides in the manufacture of medicaments.

Stable, protracted GLP-1/glucagon receptor co-agonists for medical use

A semi-recombinant method for the production of GLP-1 analogues and derivatives with non-proteogenic amino acids in the N-terminal part combining the use of recombinant expression techniques and chemical peptide synthesis.

Semi-recombinant preparation of GLP-1 analogues

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Herlev, Denmark

Thomas Kruse