47 results about "Glucagon-Like Peptide Receptors" patented technology

A composition including a compound which binds to a receptor for glucagon-like peptide-1 and a pharmaceutical carrier. The amount of the compound present is effective to control appetite in a human. Also disclosed is a method for controlling appetite and for reducing food intake in a human by administering to the human a composition comprising a compound which binds to a receptor for glucagon-like peptide-1 and a pharmaceutical carrier.

A composition for the treatment of impaired glucose tolerance (IGT) including a compound which binds to a receptor for glucagon-like peptide-1, and a pharmaceutical carrier. The amount of the compound present is an effective amount to improve pancreatic β-cell sensitivity to blood glucose levels in a human with IGT. Also, a method for improving the pattern of insulin secretory responses in a human with IGT by administering to the human a composition comprising a compound which binds to a receptor for glucagon-like peptide-1 and a pharmaceutical carrier.

The present invention provides novel human glucagon-like peptide-1 (GLP-1)-receptor modulators that have biological activity similar or superior to native GLP-1 peptide and thus are useful for the treatment or prevention of diseases or disorders associated with GLP activity. Further, the present invention provides novel, chemically modified compounds that not only stimulate insulin secretion in type II diabetics, but also produce other beneficial insulinotropic responses. These synthetic peptide GLP-1 receptor modulators exhibit increased stability to proteolytic cleavage making them ideal therapeutic candidates for oral or parenteral administration. The compounds of this invention show desirable pharmacokinetic properties and desirable potency in efficacy models of diabetes.

The invention relates to a cell strain for measuring the bioactivity of GLP-1 and functional analogue thereof and an application of the cell strain and belongs to the technical field of measurement of drug bioactivity. The GLP-1R / HEK293 cell strain is preserved in the common microorganism center of China microorganism culture preservation management committee and the preservation number is CGMCCNo.5909. The invention relates to a measuring method for establishing express glucagon peptide-1 receptor (GLP-1R) genetic engineering cell strain GLP-1R / HEK293 and measuring the bioactivity of GLP-1 and analogue thereof in external stimulation on the basis of the change in the cAMP level in the cell after the GLP-1R / HEK293 cell strain is stimulated by the glucagon peptide-1 receptor (GLP-1R) and the functional analogue thereof. The measuring method is easily standardized, is excellent in repeatability and has the characteristics of low cost, convenience and accuracy, thereby being excellent in application prospect.

The subject matter described herein provides novel human glucagon-like peptide-1 (GLP-1) receptor modulators that have biological activity similar or superior to native GLP-1 peptide and thus are useful for the treatment or prevention of diseases or disorders associated with GLP activity. The described compounds include chemically modified peptides that not only stimulate insulin secretion in type II diabetics, but also produce other beneficial insulinotropic responses. These synthetic peptide GLP-1 receptor modulators exhibit increased stability to proteolytic cleavage making them ideal therapeutic candidates for oral or parenteral administration. The disclosed and claimed peptides show desirable pharmacokinetic properties and desirable potency in efficacy models of diabetes.

The present invention relates to combinations, pharmaceutical compositions and fusion molecules comprising an FGF21 (fibroblast growth factor 21) compound and a GLP-1R (glucagon-like peptide-1 receptor) agonist with optimized GLP-1R agonist / FGF21 compound activity ratio. It further relates to their use as medicaments, in particular for the treatment of obesity, being overweight, metabolic syndrome, diabetes mellitus, diabetic retinopathy, hyperglycemia, dyslipidemia, Non-Alcoholic SteatoHepatitis (NASH) and / or atherosclerosis.

Combination treatment of obesity and its complications with seladelpar or a salt thereof and a glucagon-like peptide-1 (GLP-1) receptor agonist.

Combination treatment of NAFLD, including NASH, with seladelpar or a salt thereof and a glucagon-like peptide-1 (GLP-1) receptor agonist.

Described are antibody peptide conjugates (APCs) comprising an antibody conjugated to a peptide analog of glucagon, which have been modified to be resistant to cleavage and inactivation by dipeptidyl peptidase IV (DPP-IV) and to increase in vivo half-life of the peptide analog while enabling the peptide analog to have agonist activity at the glucagon (GCG) receptor and the glucagon-like peptide 1 (GLP-1) receptor and the use of such APCs for treatment of metabolic disorders such as diabetes, non-alcoholic fatty liver disease (NAFLD), non-alcoholic steatohepatitis (NASH), and obesity.

The invention relates to application of a polypeptide compound having a double activation effect on a glucagons-like peptide-1 receptor (GLP-1R) and a glucagons receptor (GCCR). The degree of BDL-induced rat cholestasis-induced liver fibrosis can be obviously decreased, and the effect of treating biliary cirrhosis and other diseases is remarkable. The double-target-point agonist polypeptide can beused for preventing or treating biliary cirrhosis and related liver fibrosis diseases.

The invention relates to a pharmaceutical composition of recombinant glucagon-like peptide-1 receptor stimulant for injection; wherein the recombinant glucagon-like peptide-1 receptor stimulant is prepared by escherichia coli expression and purification and has a sequence represented by the SEQ ID No.2. The pharmaceutical composition for injection comprises a recombinant glucagon-like peptide-1 receptor stimulant, critic acid-sodium citrate buffering salts, and polyol. The invention further relates to an injection liquid and freeze-dried powder injection containing the recombinant glucagon-like peptide-1 receptor stimulant. The pharmaceutical composition of recombinant glucagon-like peptide-1 receptor stimulant for injection has the advantages of safety, stability, convenience in transportation and storage, and suitability for industrial production.

The invention relates to an exendin-4 radioactive probe targeting a glucagon-like peptide-1 receptor, and a preparation method thereof, and belongs to the field of radiopharmaceutical chemistry. The structural formula of the radioactive probe is shown in the specification. The marking time of the radioactive probe is 8 min, and the marking yield is more than 99%, the radiochemical purity the product, determined by radio-HPLC is more than 99%. The product shows high affinity and high specificity to the glucagon-like peptide-1 receptor, meanwhile, has better in-vivo biological metabolism property, and is a potential PET imaging agent for the glucagon-like peptide-1 receptor.

The invention discloses a fusion protein. The fusion protein includes a protein therapeutic agent and a receptor binding agent. The protein therapeutic agent is a GLP-1 peptide or an analogue thereof. The receptor binding agent is a cholera toxin B subunit or an analogue thereof. The fusion protein can be used for treating diabetes, and the like through oral administration.

The present invention provides modified glucagon-like peptide 1 (GLP1) polypeptides, fusion proteins comprising modified GLP1 polypeptides, and methods of use thereof. In various embodiments of the invention, the fusion proteins are GLP1 receptor agonists that comprise a modified GLP1 fused to a stabilizing domain. In some embodiments, the fusion proteins comprising modified GLP1 are useful for treating or ameliorating a symptom or indication of a disorder such as obesity and diabetes.

The invention relates to methods, uses, compositions and formulations including a melanocortin receptor-4 agonist and a glucagon-like peptide-1 receptor agonist for treatment of obesity, diabetes, metabolic syndrome and related indications, diseases or disorders.

The invention relates to a composition of a micro-array drug delivery system of a glucagon-like peptide-1 receptor stimulating agent and belongs to the technical field of pharmacy. The composition disclosed by the invention at least comprises two parts, i.e., a part A and a part B, wherein the A is a micro-array film, and the B is the glucagon-like peptide-1 receptor stimulating agent. The composition has the advantages that preparation materials, morphologies and use performance of the existing micro-array systems are broken through by researching interaction between the system and drugs based on morphologies of the existing micro-arrays, and thus, the composition is more applicable to drug delivery. The final-provided composition of the micro-array drug delivery system for delivering the GLP-1 receptor stimulating agent is stable in process, high in drug load amount and uniform in drug distribution, and the problem of the existing micro-array preparation materials that the GLP-1 receptor stimulating agent cannot be delivered is solved.

The disclosures herein relate to novel compounds of formula (1): and salts thereof, wherein R1, AA1, AA2, LysR, X and Y are defined herein, and their use in treating, preventing, ameliorating, controlling or reducing the risk of disorders associated with Glucagon-like peptide-1 (GLP-1) receptors.

The invention relates to a human glucagon-like peptide-1 receptor (GLP-1R) activator and application thereof. The human glucagon-like peptide-1 receptor activator comprises a compound shown in a formula I which is described in the specification or a pharmaceutically acceptable salt of a compound, and R1, R2, R3, R4, R5 and R6 are respectively and independently selected from any one of H, C1-C4 alkyl, sulfydryl, phosphate group, vinyl or acetyl. It is found for the first time that the compound shown in the formula I or the pharmaceutically acceptable salt thereof can improve glycolipid metabolism of whole-body tissue cells, enhance oxidative degradation of lipid molecules, inhibit expression of adipogenic genes, inhibit activity of acetyl coenzyme A synthetase and reduce synthesis of triglyceride, glucose-induced insulin synthesis and secretion are improved, insulin antagonism is relieved, compensatory amplification of pancreatic beta cells is relieved, and the survival rate and functions of pancreatic cells in the II-type diabetes mellitus-like state are improved.

The present disclosure relates to an analog of glucagon-like peptide-1 (glp-1) receptor agonist. The present disclosure provides analogs of glucagon-like peptide-1 (glp-1) receptor agonist wherein, the amino acid at position 2 of the glucagon-like peptide-1 (glp-1) receptor agonist is replaced with D-Alanine. The analogs of glucagon-like peptide-1 (glp-1) have one or more properties of prolonged half-life, better pharmacokinetic profile, retained biological activity, and being advantageous for relieving the patient's burden by reducing the dosing frequency and dose. The present disclosure further provides processes for preparing synthetic glucagon-like peptide-1 (glp-1) analogs.

The invention provides a multifunctional variant protein and a fusion protein thereof, and the multifunctional variant protein comprises Fibroblast growth factor 21(FGF21) protein or a mutant protein thereof and a Glucagon-like peptide-1 (GLP-1) receptor or a mutant protein thereof, wherein the pharmaceutical composition of the fusion protein can be used for treating diabetes, obesity, dyslipidemia, metabolic syndrome, nonalcoholic fatty liver disease, nonalcoholic fatty hepatitis and other related diseases.

The invention discloses a long-acting fusion protein with dual activation activity on a glucagon-like peptide-1 (GLP-1) receptor (GLP-1R) and a glucose-dependent insulinotropic polypeptide (GIP) receptor (GIPR), as well as a preparation method and application of the long-acting fusion protein. The fusion protein is formed by sequentially connecting three structural functional domains, namely exendin-4 or a mutant thereof, human glucose-dependent insulinotropic polypeptide (GIP) or a mutant thereof and an Fc fragment of human immunoglobulin IgG through a linker or directly connecting the three structural functional domains from an N-terminal to a C terminal. The invention also provides a genetic engineering preparation method for soluble expression of the fusion protein in escherichia coli. The method is simple in process, and protein products with biological activity can be conveniently and directly obtained from cell wall breaking liquid through purification. The fusion protein disclosed by the invention has remarkable dual agonist activity on GLP-1R and GIPR, and can be applied to preparation of medicines for treating diabetes, obesity, hyperlipidemia and other related diseases.

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.

The invention discloses a pharmaceutical composition for controlling glucose fluctuation. The composition is composed of one or more of levocarnitine, a levocarnitine derivative, a pharmaceutically acceptable salt of levocarnitine or the derivative thereof, a metabolic regulation drug, insulin and analogues thereof, a sulfonylurea promotor, metformin, an alpha-glucosidase inhibitor, a thiazolidinedione derivative sensitizer, a phenanthroid derivative promotor, a glucagon-like peptide-1 (GLP-1) receptor stimulant, a dipeptidyl peptidase 4 (DPP-4) inhibitor and a pancreatic amyloid polypeptide analogue, and has the effect of controlling glucose fluctuation.