56 results about "GLP-1 Analogue" patented technology

The invention relates to a derivative or pharmaceutically-acceptable salt of a GLP-1 analogue containing an amino acid sequence shown in a formula (I). The derivative of the GLP-1 analogue has the function of human GLP-1 analogue, and compared with the human GLP-1 analogue, the derivative has a longer half-life period in vivo. The derivative or pharmaceutically-acceptable salt of the GLP-1 analogue, or the pharmaceutical composition of derivatives containing the GLP-1 analogue or pharmaceutically-acceptable salts thereof can be widely used for treating non-insulin-dependent diabetes mellitus,insulin-dependent diabetes mellitus and obesity. The formula (1) is as follows: X1-X2-Glu-Gly-Thr-Phe-Thr-Ser-Asp-X10-Ser-X12-X13-X14-Glu-X16-X17-Ala-X19-X20-X21-Phe-Ile-X24-Trp-Leu-X27-X28-X29-X30-X31-X32-X33-X34-X35-X36-X37-X38-X39-Lys (I).

Provided are a glucagon-like peptide-1 (GLP-1) analogue monomer and dimmer, a preparation method thereof, and an application thereof. The GLP-1 analogue monomer comprises one cysteine; and the dimer is formed by two monomer molecules connected via an intermolecular disulfide bond formed by the cysteine. The GLP-1 monomer comprising cysteine has the following general formula: 7HAEX10TFTSX15VSSYLEX22X23AAKEFIX30WLX33KGRG37, wherein X10 is glycine or cysteine, X15 is aspartate or cysteine, X22 is glycine or cysteine, X23 is glutamine or cysteine, X30 is alanine or cysteine, and X33 is valine or cysteine; and only one of X10, X15, X22, X23, X30, and X33 is cysteine. The glucagon-like peptide-1 analogue dimer of the present invention has an in vivo half-life of more than 8 to 96 hours, thus facilitating clinical promotion and application.

The invention relates to new type GLP-1 analogues and a microwave promotive solid phase synthesis process of the same. GLP-1 analogues with longer pharmacological action time can be obtained by modifying 8, 9, 16, 22, 27 or 37 sites of natural GLP-1, the chemical synthesis is highly effectively and rapidly realized by microwave promotive solid phase synthesis process, the crude product is purified by highly effective liquid phase, and GLP-1 analogues is obtained after lyophilized.

Novel GLP-1 agonists which are protracted by coupling to a protraction protein.

The invention relates to truncated GLP-1 analogues, in particular a GLP-1 analogue which is a modified GLP-1(7-35) (SEQ ID No 1) having: i) a total of 2, 3, 4, 5 6, 7, 8, or 9 amino acid substitutions as compared to GLP-1(7-35), including a) a Glu residue at a position equivalent to position 22 of GLP-1(7-35), and b) an Arg residue at a position equivalent to position 26 of GLP-1(7-35); as well as derivatives thereof, and therapeutic uses and compositions. These analogues and derivatives are highly potent, have a good binding affinity to the GLP-1 receptor, also to the extracellular domain of the GLP-1 receptor, which is of potential relevance achieving long-acting, stable GLP-1 compounds with a potential for once weekly administration.

The invention provides a class of novel fusion protein of a GLP-1(glucagon like protein-1) analogue and a preparation method and application thereof. The fusion protein is composed of three ingredients: the GLP-1 analogue, connecting peptide and human serum albumin (HSA). The compound prepared by using the method has the advantages that the production cost is very low, the biological activity is higher, and the stability in vitro and vivo is better. The fusion protein can be used for treating diabetes, obesity and irritable bowel syndrome and other diseases which benefit from fasting plasma glucose reduction, stomach and / or bowel movement inhibition and stomach and / or bowel empty or food intake inhibition.

The invention discloses a glucagon-like peptide-1 analogue sustained release microsphere as well as a preparation method and an application thereof. The sustained release microsphere mainly includes 1-10 parts by weight of the glucagon-like peptide-1 analogue and 90-99 parts by weight of a polylactic acid-glycollic acid copolymer and is 0.5-100 [mu]m in range of average particle size. The invention also discloses the preparation method and the application of the sustained release microsphere and also inspects appearance, particle size, in-vitro releasing and in-vivo pharmacodynamic experimentof the microsphere. The sustained release microsphere supporting GLP-1 analogue has uniform particle size and has significant treatment effect on diabetes, can effectively control blood glucose for 14days and has the effect as a slow-effect preparation. The sustained release microsphere greatly reduces dosing frequency and increases compliance of patients, and also can inhibit food intake. The preparation method has simple process and gentle conditions, and is low in influence on activities of polypeptides.

A GLP-1 analogue composition for microneedle devices, which contains a GLP-1 analogue and at least one kind of solvent that is selected from the group consisting of water, glycerol, propylene glycol, ethylene glycol, 1,3-butylene glycol and polyethylene glycol.

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.

The invention relates to an Xenopus laevis GLP-1 analogue, a synthesis method and applications thereof. According to the present invention, the side chain and the C terminal of Xenopus laevis GLP-1 are subjected to structure modification to obtain the Xenopus laevis GLP-1 analogue with advantages of high blood glucose lowering activity and long pharmacological action time; and the Xenopus laevis GLP-1 analogue has significantly improved biological activity, and further has effects of strong long-acting blood glucose lowering and strong weight reducing.

The invention relates to a GLP-1 analogue and ziconotide composite slow-release microsphere preparation and a preparation method thereof. The slow-release microsphere preparation is prepared from a GLP-1 analogue, ziconotide, a biodegradable high polymer material with biocompatibility, a stabilizing agent and a freeze drying protection agent. The preparation method comprises the following steps of (1) adding water for preparing the GLP-1 analogue and the ziconotide into a medicine solution A; adding an organic solvent for preparing the biodegradable high polymer material with biocompatibility into a solution B; (2) mixing the solution A and the solution B; performing ultrasonic processing to form primary emulsion; adding the primary emulsion into a stabilizing agent water solution saturated by an organic mixed solvent; performing homogenizing emulsification to obtain secondary emulsion; (3) performing room-temperature stirring on the secondary emulsion for 1 hour; then, raising the temperature to 40 DEG C to 45 DEG C; maintaining the temperature for one hour; then, lowering the temperature to 10 DEG C; adding the freeze drying protection gent; screening and collecting particles; performing freeze drying; performing radiation sterilization. By using a related technology, the effect of treating diabetes and PDN (painful diabetic neuropathy) complications for a long time can be achieved; the pain of a patient is reduced; the medicine compliance of the patient is improved; the clinic practical significance is realized.

Provided herein are oral pharmaceutical compositions containing a GLP-1 analogue and / or insulin for treating and reducing the incidence of nonalcoholic fatty liver disease (NAFLD), hepatic steatosis, and sequelae thereof, and methods of utilizing same.