Novo Nordisk A/s

Transtech Pharma, Inc.

Other

Leo-pharma A/s

Novo Nordick A/s

British Technology Group Intercorporate Licensing Limited

Noro Nordisk A/s

Vtv Therapeutics LLC

Lau, Jesper

Jesper F Lau

Anthony Murray

Thomas Kruse Hansen

Michael Ankersen

Lone Jeppesen

Patrick William Garibay

Thomas Kruse

Janos Tibor Kodra

Robert Carl Andrews

Dharma Rao Polisetti

Govindan Subramanian

Peter Madsen

Jacob Kofoed

Kalpathy Chidambareswaran Santhosh

Kjeld Madsen

Per Vedso

Henning Thoegersen

Marit Kristiansen

Jane Spetzler

Bernd Peschke

Daniel Peter Christen

Carsten Behrens

Adnan M M Mjalli

Jane Marie Lundbeck

Nils Langeland Johansen

Knud Erik Andersen

Mustafa Guzel

Lauge Schaeffer

Hans Petersen

Henrik Sune Andersen

Ole Hvilsted Olsen

Christian Klarner Sams

Anker S Jorgensen

Yu Ge

Daniel Dale Holsworth

Todd Kevin Jones

Ingrid Pettersson

Michael Bruno Plewe

Richard Dennis DiMarchi

Per Sauerberg

Min Teng

Lise Brown Christiansen

Jun Feng

Preben H Olesen

Yufeng Hong

Bapu Reddy Gaddam

Vlad Edward Gregor

Maria Carmen Valcarce Lopez

Svend Ludvigsen

Paw Bloch

Behrend Friedrich Lundt

Per Vedsø

Lars J Knutsen

Lars Linderoth

Steffen Reedtz-Runge

Ulrich Sensfuss

Jeremy T Cooper

Frank Urban Axe

Anthony Lai Ling

Inge Thoger Christensen

Brett Watson

Peter Kresten Nielsen

Luke Milburn Judge

Roy Teruyuki Uyeda

Maria Carmen Valcarce-Lopez

Shenghua Shi

Larry Kenneth Truesdale

Henning Thøgersen

Ulla Grove Sidelmann

Birgit Wieczorek

Anker Jon Hansen

Michael David Johnson

Henning Tho Slashedgersen

János Tibor Kodra

Patrick J Knerr

Farid Bakir

Florencio Zaragoza Dorwald

Simon Feldbæk Nielsen

Lars Naerum

Leif Hoejslet Christensen

Dilip Ramakant Bhumralkar

Michael James Newman

Anne Marie Horneman

Morten Schlein

Brian Finan

Javier Gonzalez

Liselotte Bjerre Knudsen

Lars Fogh Iversen

Asser Sloth Andersen

Claus Ulrich Jessen

Jianhe Chen

Jeppe Sturis

Per Olaf Huusfeldt

Florencio Zaragoza Dörwald

Soeren Oestergaard

Atsuo Kuki

Jens Christian Norrild

Christine Thomas

Christian Wenzel Tornoee

Henning Borge Petersen

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 construct comprising a compound targeting areas in the brain involved in the regulation of body weight and an allosteric ligand to a receptor located in the blood-brain barrier (BBB). The invention also relates to compositions and uses of such construct, for example in the prevention or treatment of overweight and obesity. Preferred compounds for regulation of body weight include GLP-1 receptor agonists (GLP-1RA), and preferred receptors located in the BBB include the transferrin receptor (TfR). Exemplary fusions and conjugates of GLP-1 RA's and anti TfR-Fab's exhibit an increased binding to brain regions expressing the GLP-1 receptor as compared to fusions or conjugates with inactive control Fab's, in particular in brain areas protected by the BBB. In vivo mice studies confirm increased reduction in food intake as well as weight loss for the active construct compared to the inactive one.

Compounds for treatment of obesity

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 invention relates to a derivative of a GLP-1 analogue, which analogue comprises a first K residue and a second K residue, at positions corresponding to position 26, and 37, respectively, of GLP-1(7-37) (SEQ ID NO: 1), and a maximum of eight amino acid changes as compared to GLP-1(7-37); which derivative comprises two protracting moieties attached to said first and second K residue, respectively, via a linker, wherein the protracting moiety is selected from Chem. 1: HOOC&#x2014;(CH)&#x2014;CO&#x2014;*, and Chem. 2: HOOC&#x2014;CH&#x2014;O&#x2014;(CH)&#x2014;CO&#x2014;*, in which x is an integer in the range of 8-16, and y is an integer in the range of 6-13; and the linker comprises Chem. 3: *&#x2014;NH&#x2014;(CH)&#x2014;CH[(CH)&#x2014;NRR]&#x2014;CO&#x2014;*, which is connected at its CO&#x2014;* end to the epsilon amino group of the first or the second K residue of the GLP-1 analogue, and wherein q is an integer in the range of 0-5, Rand Rindependently represent *&#x2014;H or *&#x2014;CH, and w is an integer in the range of 0-5; 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 peptide and linker intermediates. The derivatives are potent, stable, protracted, and suitable for oral administration.

Double-acylated GLP-1 derivatives

The invention relates to compounds derived from the EGF(A) domain of LDL-R, in particular compounds comprising a peptide analogue of the wild-type EGF(A) (LDL-R(293-332)) sequence and at least one substituent comprising at least one fatty acid group. The invention also relates to a pharmaceutical composition thereof and use a medicament. The novel EGF(A) compounds of the invention are useful as treatment e.g. in the field of cholesterol lowering, dyslipidaemia and cardiovascular disease.

EGF(A) analogues with fatty acid substituents

The invention relates to a derivative of a GLP-1 peptide, which peptide comprises a first Lys residue at a position corresponding to position 36 of GLP-1(7-37) (SEQ ID NO: 1), a second Lys residue at a position corresponding to position 37 of GLP-1(7-37) (SEQ ID NO: 1), and a maximum of seven amino acid changes as compared to GLP-1(7-37) (SEQ ID NO: 1); which derivative comprises two protractors attached to said first and second Lys residue, respectively, each via a linker; wherein the protractor is selected from:HOOC&#x2014;CH&#x2014;O&#x2014;(CH)&#x2014;CO&#x2014;*, and&#x2003;&#x2003;Chem. 1:HOOC&#x2014;(CH)&#x2014;CO&#x2014;*,&#x2003;&#x2003;Chem. 2:wherein y is an integer in the range of 8-11, and x is 12; and the linker comprises at least one of:*&#x2014;NH&#x2014;CH(COOH)&#x2014;(CH)&#x2014;CO&#x2014;*,&#x2003;&#x2003;Chem. 3:*&#x2014;NH&#x2014;CH((CH)&#x2014;COOH)&#x2014;CO&#x2014;*, and/or&#x2003;&#x2003;Chem. 4:*&#x2014;NH&#x2014;(CH)&#x2014;[O&#x2014;(CH)]&#x2014;O&#x2014;[CH]&#x2014;CO&#x2014;*,&#x2003;&#x2003;Chem. 5: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 uses thereof, such as for the treatment of diabetes and obesity, as well as to the GLP-1 peptides forming part of these derivatives which have Lys residues at positions 36 and 37 and no other Lys residues, and the GLP-1(9-37) fragments thereof. The invention furthermore relates to an intermediate product comprising 3-carboxyphenoxy-nonanoic acid with a protection group at the carboxy group of the nonanoic acid, optionally via a linker. The derivatives have a very good potency and a long half-life which makes them potentially useful for, e.g., oral administration.

Double-acylated GLP-1 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 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 invention relates to a derivative of a GLP-1 peptide, which peptide has two Lys residues, namely a first and a second Lys residue, and a maximum of eight amino acid changes as compared to GLP-1(7-37) (SEQ ID NO: 3), which derivative comprises two protracting moieties attached to the epsilon amino group of said first and second Lys residue, respectively, via a linker, wherein the protracting moiety is selected from Chem. 15: HOOC&#x2014;(CH)&#x2014;CO&#x2014;*, and Chem. 16: HOOC&#x2014;CH&#x2014;O&#x2014;(CH)&#x2014;CO&#x2014;*, in which x is an integer in the range of 10-16, and y is an integer in the range of 8-12; and the linker comprises a first linker element *&#x2014;NH&#x2014;CH(CHOH)&#x2014;CO&#x2014;*. A preferred linker is gGlu-Ser-Ser-Gly-Ser-Ser-Gly (SEQ ID NO: 2). The derivative of the invention has a very good potency, and a very good binding to the GLP-1 receptor. The invention also relates to the pharmaceutical use of the derivative, for example in the treatment and/or prevention of all forms of diabetes and related diseases.

GLP-1 derivatives

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

Novel GLP-1 compounds and their therapeutic use.

GLP-1 compounds

The invention relates to a derivative of a GLP-1 peptide, which peptide has two Lys residues, namely a first and a second Lys residue, and a maximum of eight amino acid changes as compared to GLP-1(7-37) (SEQ ID NO: 3), which derivative comprises two protracting moieties attached to the epsilon amino group of said first and second Lys residue, respectively, via a linker, wherein the protracting moiety is selected from Chem. 15: HOOC&#x2014;(CH2)x-CO&#x2014;*, and Chem. 16: HOOC&#x2014;C6H4-O&#x2014;(CH2)y-CO&#x2014;*, in which x is an integer in the range of 10-16, and y is an integer in the range of 8-12; and the linker comprises a first linker element *&#x2014;NH&#x2014;CH(CH2OH)&#x2014;CO&#x2014;*. A preferred linker is g Glu-Ser-Ser-Gly-Ser-Ser-Gly (SEQ ID NO: 2). The derivative of the invention has a very good potency, and a very good binding to the GLP-1 receptor. The invention also relates to the pharmaceutical use of the derivative, for example in the treatment and/or prevention of all forms of diabetes and related diseases.

Growing community of inventors

Farum, Denmark

Jesper F Lau