Processing

Please wait...

Settings

Settings

Goto Application

1. WO2019057445 - MINIGASTRIN DERIVATES, IN PARTICULAR FOR USE IN CCK2 RECEPTOR POSITIVE TUMOUR DIAGNOSIS AND/OR TREATMENT

Publication Number WO/2019/057445
Publication Date 28.03.2019
International Application No. PCT/EP2018/073020
International Filing Date 27.08.2018
IPC
A61K 38/22 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
38Medicinal preparations containing peptides
16Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
17from animals; from humans
22Hormones
A61K 51/08 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
51Preparations containing radioactive substances for use in therapy or testing in vivo
02characterised by the carrier
04Organic compounds
08Peptides, e.g. proteins
C07K 14/595 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
14Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
435from animals; from humans
575Hormones
595Gastrins; Cholecystokinins (CCK)
G01N 33/574 2006.01
GPHYSICS
01MEASURING; TESTING
NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
33Investigating or analysing materials by specific methods not covered by groups G01N1/-G01N31/131
48Biological material, e.g. blood, urine; Haemocytometers
50Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
53Immunoassay; Biospecific binding assay; Materials therefor
574for cancer
CPC
A61K 38/2207
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
38Medicinal preparations containing peptides
16Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
17from animals; from humans
22Hormones
2207Gastrins; Cholecystokinins [CCK]
A61K 51/08
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
51Preparations containing radioactive substances for use in therapy or testing in vivo
02characterised by the carrier ; , i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
04Organic compounds
08Peptides, e.g. proteins ; , carriers being peptides, polyamino acids, proteins
A61K 51/088
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
51Preparations containing radioactive substances for use in therapy or testing in vivo
02characterised by the carrier ; , i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
04Organic compounds
08Peptides, e.g. proteins ; , carriers being peptides, polyamino acids, proteins
088conjugates with carriers being peptides, polyamino acids, proteins
C07K 14/595
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
14Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
435from animals; from humans
575Hormones
595Gastrins; Cholecystokinins [CCK]
G01N 2333/726
GPHYSICS
01MEASURING; TESTING
NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
2333Assays involving biological materials from specific organisms or of a specific nature
435from animals; from humans
705Assays involving receptors, cell surface antigens or cell surface determinants
72for hormones
726G protein coupled receptor, e.g. TSHR-thyrotropin-receptor, LH/hCG receptor, FSH
G01N 33/57484
GPHYSICS
01MEASURING; TESTING
NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
33Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
48Biological material, e.g. blood, urine
50Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
53Immunoassay; Biospecific binding assay; Materials therefor
574for cancer
57484involving compounds serving as markers for tumor, cancer, neoplasia, e.g. cellular determinants, receptors, heat shock/stress proteins, A-protein, oligosaccharides, metabolites
Applicants
  • PAUL SCHERRER INSTITUT [CH]/[CH]
Inventors
  • BEHE, Martin
  • MINDT, Thomas
  • GROB, Nathalie
  • SCHIBLI, Roger
Agents
  • FISCHER, Michael
Priority Data
17192428.521.09.2017EP
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) MINIGASTRIN DERIVATES, IN PARTICULAR FOR USE IN CCK2 RECEPTOR POSITIVE TUMOUR DIAGNOSIS AND/OR TREATMENT
(FR) DÉRIVÉS DE MINIGASTRINE DESTINÉS, EN PARTICULIER, À ÊTRE UTILISÉS DANS LE DIAGNOSTIC ET/OU LE TRAITEMENT DE TUMEURS POSITIVES POUR LE RÉCEPTEUR CCK2
Abstract
(EN)
It is therefore the objective of the present invention to provide minigastrin derivates which further improve the accumulation in CCK-2 receptor positive tumours by simultaneously very low accumulation in other organs, e.g. the kidneys. This objective is achieved according to the present invention by a minigastrin derivate having the formula: X-Z-Ala-Tyr-Gly-Trp-Met-Asp-Phe-NH2 (Y), wherein at least one of the connecting or terminal amide bonds between, before or after the amino acids of the sequence Z, Ala, Tyr, Gly, Trp, Met, Asp, Phe and NH2 or Y (C-terminal) is replaced by a 1,4-disubstituted or a 1,5-disubstituted 1,2,3-triazole, while X stands for a chemical group attached to the peptide for the purpose of diagnostic and/or therapeutic intervention at CCK-2 receptor relevant diseases, Y stands for C-terminal modifications of the peptide, such as amide, primary and secondary amides, free carboxylic acids and carboxylic ester derivatives including but not limited to amides and esters derived from linear or branched alkyl-,alkenyl-, alkynyl- aromatic-, and heterocyclic alcohols, and Z stands for a linker or DGlu* wherein DGlu* stands for a chain of DGlu having 1 to 6 repetitions (-DGlu-to -DGlu-DGlu-DGlu-DGlu-DGlu-DGlu-). These minigastrin derivates have a high specific internalization, excellent IC50 values and sufficient plasma stability.
(FR)
La présente invention concerne des dérivés de minigastrine qui améliorent encore l'accumulation dans les tumeurs positives pour le récepteur CCK-2 avec simultanément une très faible accumulation dans d'autres organes, par exemple les reins. La présente invention concerne un dérivé de minigastrine de formule : X-Z-Ala-Tyr-Gly-Trp-Met-Asp-Phe-NH2 (Y), dans laquelle au moins l'une des liaisons amide de liaison ou de terminaison entre, avant ou après les acides aminés de la séquence Z, Ala, Tyr, Gly, Trp, Met, Asp, Phe et NH2 ou Y (C-terminal) est remplacé par un groupe 1,2,3-triazole 1,4-disubstitué ou 1,5-disubstitué, tandis que X représente un groupe chimique attaché au peptide en vue d'une intervention diagnostique et/ou thérapeutique sur des maladies en rapport avec le récepteur CCK-2, Y représente des modifications C-terminales du peptide, tels qu'un amide, des amides primaires et secondaires, des acides carboxyliques libres et des dérivés d'ester carboxylique comprenant, mais sans s'y limiter, des amides et des esters dérivés d'alcools alkyliques, alcényliques, alcynyliques, aromatiques et hétérocycliques linéaires ou ramifiés et Z représente un lieur ou DGlu*, DGlu* représentant une chaîne DGlu comprenant 1 à 6 répétitions (-DGlu- à -DGlu-DGlu-DGlu-DGlu-DGlu-DGlu-). Ces dérivés de minigastrine présentent une internalisation spécifique élevée, d'excellentes valeurs de CI50 et une stabilité dans le plasma suffisante.
Also published as
JP2020516682
Latest bibliographic data on file with the International Bureau