Patent classifications
C07K14/605
BIOTIN MOIETY-CONJUGATED POLYPEPTIDE AND PHARMACEUTICAL COMPOSITION FOR ORAL ADMINISTRATION COMPRISING THE SAME
The present invention relates to a biotin moiety-conjugated polypeptide and a pharmaceutical composition for oral administration comprising the same, wherein the polypeptide according to the present invention has an excellent in vivo oral bioavailability.
METHOD FOR PREPARING LIRAGLUTIDE USING ENVIRONMENT-FRIENDLY SOLVENT
Proposed is a novel method for preparing liraglutide by means of an ionic liquid and a eutectic solvent, which are environment-friendly solvents. More specifically, the method is characterized in that fractionated peptide 1 represented by the following formula (1) and fractionated peptide 2 represented by the following formula (2) are subjected to a coupling reaction in the presence of an ionic liquid or a eutectic solvent. In preparing GLP-1 analogues such as liraglutide, the present method increases reactivity when producing liraglutide, which is an unprocessed reactant, by using an ionic liquid and a eutectic solvent as environment-friendly solvents instead of using organic solvents. Accordingly, through a relatively short and simple purification process, the present method has advantages of reducing the formation of related substances, improving purity, improving yields, shortening reaction times, reducing production cost, and lowering the manufacturing cost.
NOVEL PEPTIDE HORMONES
The present invention relates to peptides that are upregulated in response to nutritional cues, antibodies which bind to the peptides, nucleic acids encoding the peptides, vectors and host cells.
AN IMPROVED PROCESS FOR PREPARATION OF LIRAGLUTIDE
The present invention relates to an improved process for the preparation of Liraglutide. The present invention further related an improved process for the preparation of substantially pure material having a purity of greater than or equal to 99.5% by HPLC.
AN IMPROVED PROCESS FOR PREPARATION OF LIRAGLUTIDE
The present invention relates to an improved process for the preparation of Liraglutide. The present invention further related an improved process for the preparation of substantially pure material having a purity of greater than or equal to 99.5% by HPLC.
GLP-1 derivatives and uses thereof
The invention relates to a derivative of a GLP-1 analogue of a general Formula I, which derivative comprises a side chain attached to a Lys residue at position 34, 35, 36, 37, or 38 of the GLP-1 analogue, which side chain comprises a Branched linker, a 1.sup.st and a 2.sup.nd Protractor selected from C18 diacid, C20 diacid, and sulfonic acid C16, and at least one Linker element-1 incorporating ethylene glycol units. Linker element-1 may be incorporated in an optional Pre-linker, and/or in a 1.sup.st or 2.sup.nd Post-linker. The invention also relates to novel GLP-1 analogues, novel side chain intermediate products and their manufacture and use to prepare derivatives of biologically active peptides and proteins, as well as pharmaceutical compositions and medical uses of the analogues and 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 a derivative of a GLP-1 analogue of a general Formula I, which derivative comprises a side chain attached to a Lys residue at position 34, 35, 36, 37, or 38 of the GLP-1 analogue, which side chain comprises a Branched linker, a 1.sup.st and a 2.sup.nd Protractor selected from C18 diacid, C20 diacid, and sulfonic acid C16, and at least one Linker element-1 incorporating ethylene glycol units. Linker element-1 may be incorporated in an optional Pre-linker, and/or in a 1.sup.st or 2.sup.nd Post-linker. The invention also relates to novel GLP-1 analogues, novel side chain intermediate products and their manufacture and use to prepare derivatives of biologically active peptides and proteins, as well as pharmaceutical compositions and medical uses of the analogues and derivatives. The derivatives have very long half-lives while maintaining a satisfactory potency, which makes them potentially suitable for once-monthly administration.
GLUCAGON DERIVATIVES
The present invention relates to a novel peptide of a glucagon derivative and a composition for preventing or treating obesity comprising the peptide as an active ingredient. The glucagon derivative according to the present invention shows a more excellent activating effect with regard to both glucagon-like peptide-1 receptors and glucagon receptors compared to native glucagon, and thus can be widely used as an effective agent for treating obesity.
GLUCAGON DERIVATIVES
The present invention relates to a novel peptide of a glucagon derivative and a composition for preventing or treating obesity comprising the peptide as an active ingredient. The glucagon derivative according to the present invention shows a more excellent activating effect with regard to both glucagon-like peptide-1 receptors and glucagon receptors compared to native glucagon, and thus can be widely used as an effective agent for treating obesity.
Stable Pharmaceutical Solution Formulation of GLP-1R Antibody Fusion Protein
Disclosed is a stable pharmaceutical solution formulation of a GLP-1R antibody fusion protein, comprising a therapeutically effective amount of the GLP-1R antibody fusion protein, an amino acid, a surfactant and a buffer system. The final concentration of the amino acid is 1-500 mM, the final concentration of the surfactant is 0.01%-0.5%, and the pH value of the stable solution formulation is from 5.0 to 8.0. The stable solution formulation of the present invention can be used in the treatment of diabetes, obesity and conditions associated therewith.