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1. WO2012062803 - DOUBLE-ACYLATED GLP-1 DERIVATIVES

Publication Number WO/2012/062803
Publication Date 18.05.2012
International Application No. PCT/EP2011/069738
International Filing Date 09.11.2011
IPC
A61K 47/48 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
48the non-active ingredient being chemically bound to the active ingredient, e.g. polymer drug conjugates
C07K 14/605 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
14Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
435from animals; from humans
575Hormones
605Glucagons
A61P 3/10 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
3Drugs for disorders of the metabolism
08for glucose homeostasis
10for hyperglycaemia, e.g. antidiabetics
CPC
A61K 38/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
38Medicinal preparations containing peptides
A61K 47/542
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
50the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
51the non-active ingredient being a modifying agent
54the modifying agent being an organic compound
542Carboxylic acids, e.g. a fatty acid or an amino acid
A61P 1/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
1Drugs for disorders of the alimentary tract or the digestive system
A61P 1/14
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
1Drugs for disorders of the alimentary tract or the digestive system
14Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
A61P 15/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
15Drugs for genital or sexual disorders
A61P 15/08
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
15Drugs for genital or sexual disorders
08for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
Applicants
  • NOVO NORDISK A/S [DK]/[DK] (AllExceptUS)
  • MADSEN, Alice Ravn [DK]/[DK] (UsOnly)
  • WIECZOREK, Birgit [DK]/[DK] (UsOnly)
  • KOFOED, Jacob [DK]/[DK] (UsOnly)
  • LAU, Jesper [DK]/[DK] (UsOnly)
  • SPETZLER, Jane [DK]/[DK] (UsOnly)
  • KODRA, János Tibor [DK]/[DK] (UsOnly)
  • LINDEROTH, Lars [DK]/[DK] (UsOnly)
  • GARIBAY, Patrick William [US]/[DK] (UsOnly)
  • SAUERBERG, Per [DK]/[DK] (UsOnly)
  • KRUSE, Thomas [DK]/[DK] (UsOnly)
Inventors
  • MADSEN, Alice Ravn
  • WIECZOREK, Birgit
  • KOFOED, Jacob
  • LAU, Jesper
  • SPETZLER, Jane
  • KODRA, János Tibor
  • LINDEROTH, Lars
  • GARIBAY, Patrick William
  • SAUERBERG, Per
  • KRUSE, Thomas
Common Representative
  • NOVO NORDISK A/S [DK]/[DK]
Priority Data
10190515.609.11.2010EP
11169276.009.06.2011EP
61/414,22116.11.2010US
61/497,12315.06.2011US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) DOUBLE-ACYLATED GLP-1 DERIVATIVES
(FR) DÉRIVÉS DE GLP-1 DOUBLEMENT ACYLÉS
Abstract
(EN)
The invention relates to a derivative of a GLP-1 analogue, which analogue comprises a first K residue at a position corresponding to position 18 of GLP-1 (7-37) (SEQ ID NO: 1 ), a second K residue at another position, and a maximum of twelve 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, Chem. 2, and Chem. 3: Chem. : HOOC-(CH2)x-CO-* Chem. 2: HOOC-C6H4-0-(CH2)y-CO-* Chem. 3: R2-C6H4-(CH2)z-CO-*, in which x is an integer in the range of 6-18, y is an integer in the range of 3-17, z is an integer in the range of 1 -5, and R2 is a group having a molar mass not higher than 150 Da; and the linker comprises Chem. 4: *-NH-(CH2)2-(0-(CH2)2)k-0-(CH2)n-CO-*. 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 peptides and side chain intermediates. The derivatives are suitable for oral administration.
(FR)
L'invention concerne un dérivé d'un analogue de GPL-1, ledit analogue comprenant un premier résidu K à une position correspondant à la position 18 de GLP-1 (7-37) (SEQ ID NO : 1), un second résidu K à une autre position, et un maximum de douze modifications d'acides aminés en comparaison à GLP-1 (7-37) ; le dérivé comprenant deux fractions étendues et fixées auxdits premier et second résidus K, respectivement, par l'intermédiaire d'un liant, la fraction étendue étant choisie parmi Chem. 1, Chem. 2 et Chem.3 : Chem. : HOOC-(CH2)x-CO-* Chem. 2: HOOC-C6H4-0-(CH2)y-CO-* Chem. 3: R2-C6H4-(CH2)z-CO-*, où x est un entier se situant dans la plage de 6-18, y est un entier se situant dans la plage de 3-17, z est un entier se situant dans la plage de 1-5, et R2 est un groupe ayant une masse molaire non supérieure à 150 Da ; et le liant comprenant Chem. 4: *-NH-(CH2)2-(0-(CH2)2)k-0-(CH2)n-CO-*, où k est un entier se situant dans la plage de 1-5, et n est un entier se situant dans la plage de 1-5 ; ou un sel, un amide ou un ester pharmaceutiquement acceptable de celui-ci. L'invention concerne également son utilisation pharmaceutique, par exemple dans le traitement et/ou la prévention de toutes formes de diabète et de maladie associées, ainsi que des nouveaux peptides et intermédiaires de chaîne latérale correspondants. Les dérivés sont adaptés à une administration par voie orale.
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