36 results about "GIP receptor" patented technology

The invention provides novel compounds which are peptide hormone analogues, and which are useful in treating disorders such as diabetes and obesity. The compounds of the general sequence recited in the specification possess a tailored profile with regards5 to potency properties at the GIP receptor. With regard to in vivo properties, administration of example peptides of the invention have been shown, in animal models, to result in increased weight loss. Preferred compounds achieve this without reducing food intake significantly.

The present invention is entitled Triple Agonists at the Glucagon / GLP-1 / GIP Receptor. The present invention relates to triple agonists that are active at all of the glucagon, GLP-1 and GIP receptors and uses thereof.

Peptide conjugates comprising a peptide selected from a peptide that modulates the PYY receptor, a peptide that modulates both the GLP-1 receptor and the GCG receptor, a peptide that modulates both the GLP-1 receptor and the GIP receptor, and a peptide that modulates the GLP-1 receptor; and a staple attached to the peptide at a first amino acid and a second amino acid are disclosed herein. Also provided are peptide conjugates comprising prolactin-releasing peptide. The peptide conjugates may be used for treating conditions such as obesity. Further provided are stapled prolactin-releasing peptide.

The GIP receptor agonists of this disclosure have antiemetic properties and can therefore be used to reduce or inhibit the frequency or severity of episodes of nausea or vomiting in patients in need.

Disclosed are peptide analogs derived from glucose dependent insulinotropic peptide (GIP), which are antagonists of the GIP receptor. These GIP peptide analogs are modified by comprising one or more individual amino acid substitutions and are conjugated to fatty acids with / without linkers, thereby having improved antagonistic activity and improved pharmacokinetic profiles.

The present invention provides novel compounds that are peptide hormone analogs and are useful for treating disorders such as diabetes and obesity.The compounds of the general sequence listed herein have tailored profiles of potency at the GIP receptor.Regarding in vivo properties, administration of exemplary peptides of the present invention has been shown to result in improved weight loss in animal models.Preferred compounds achieve this without significantly reducing food intake.

The present disclosure provides methods of treating overweight or obese patients with or without type 2 diabetes mellitus. The treatment comprises administration of a dual GLP-1 receptor and GIP receptor agonist.

The present invention provides novel compounds which are peptide hormone analogs and are useful in the treatment of conditions such as diabetes and obesity. Compounds of the general sequence listed in the specification have a tailored profile with respect to potency characteristics for GIP receptors. Administration of example peptides of the invention has been demonstrated in animal models about in vivo characteristics to result in increased weight loss. Preferred compounds achieve this without significantly reducing food intake.

The present invention provides pharmaceutically acceptable controlled-release microparticle composition(s) and formulation(s) comprising said composition(s) for use in the treatment of obesity, diabetes, or both. The composition(s) and formulation(s) described herein comprise microparticles comprising API(s) and biodegradable polymer compounds. The API(s) of the composition(s) and formulation(s) described herein exhibit detectable or significant agonist activity for one or more of the melanocortin-1 receptor (MC1), melanocortin-2 receptor (MC2), melanocortin-3 receptor (MC3), melanocortin-4 receptor (MC4), and melanocortin-5 receptor (MC5), GLP-1 receptor, glucagon receptor, and GIP receptor, and generally have a molecular weight of at least about 1000 Da.

Disclosed are peptide analogs derived from glucose dependent insulinotropic peptide (GIP), which are antagonists of the GIP receptor. These GIP peptide analogs are modified by comprising one or more individual amino acid substitutions and are conjugated to fatty acids with / without linkers, thereby having improved antagonistic activity and improved pharmacokinetic profiles.

The present disclosure provides compounds of the formula:and their pharmaceutically acceptable salts, as well as pharmaceutical compositions comprising these compounds and their use in the treatment of type II diabetes mellitus and obesity.

The invention discloses a long-acting polypeptide analogue and application thereof.The polypeptide analogue can target a GLP-1 receptor, a GIP receptor and an NPY2 receptor at the same time and has multiple biological functions, the advantages of GLP-1 in diabetes treatment can be brought into play, the positive effects of GIP in glycometabolism and lipid metabolism regulation and appetite inhibition are achieved, and the polypeptide analogue can be used for treating diabetes mellitus and treating diabetes mellitus and treating diabetes mellitus and treating diabetes mellitus and treating diabetes mellitus and treating diabetes mellitus and treating diabetes mellitus and treating diabetes mellitus. The effect of the PYY3-36 on regulating and controlling the appetite is fused. The multi-target synergistic effect is beneficial to optimization of sugar, fat and energy balance. The polypeptide analogue shows a wider application prospect in the field of preparation of drugs for preventing and treating metabolic syndromes, such as diabetes, obesity and other diseases.

To provide a GIP receptor agonist peptide compound having an activating action on a GIP receptor.SOLUTION: To provide a new peptide compound containing an amino acid sequence represented by a specific sequence and having activation action on a GIP receptor, and to provide use of the peptide compound as a medicine.SELECTED DRAWING: None

The present disclosure provides methods of treating a steatotic liver disease associated with metabolic dysfunction, such as metabolic dysfunction-associated steatohepatitis (MASH), metabolic dysfunction-associated fatty livers disease (MAFLD), or metabolic dysfunction-associated steatotic liver disease (MASLD). The treatment comprises administration of a dual GLP-1 receptor and GIP receptor agonist.

The present invention relates to a composition comprising insulin and a triple agonist having activity on the glucagon receptor, the GLP-1 receptor and the GIP receptor, and to a combination preparation comprising the composition.

The present invention relates to an RNAi formulation for preventing or treating obesity and a combination therapy using the same, and more specifically to a pharmaceutical composition for preventing or treating obesity containing as an active ingredient an RNAi formulation comprising an antisense strand having sequence complementarity to the MARC1 mRNA sequence and a sense strand having sequence complementarity to the antisense strand, and a combination formulation with a GLP-1 receptor agonist or a GLP-1 / GIP receptor dual agonist.

Disclosed are glucose-dependent insulinotropic peptide (GIP) derived peptide analogs that are antagonists of the GIP receptor. These GIP peptide analogs are modified by inclusion of the amino acid substitutions A13Aib and / or N24E and conjugated with a fatty acid with or without a linker, resulting in improved solubility and / or physical stability.

This invention discloses a polypeptide analog with GLP-1 receptor agonist and GIP receptor antagonist activities and its applications. The sequence structure of the polypeptide analog is selected from any of the amino acid sequences shown in SEQ ID NO:1-2. This polypeptide compound achieves excellent hypoglycemic and sustained, superior weight loss effects by agonizing the GLP-1 receptor and antagonizing the GIP receptor. Therefore, this type of polypeptide compound has broad application prospects in the field of drug preparation for the prevention and treatment of metabolic syndromes, such as diabetes and obesity.

The present disclosure provides methods of treating a steatotic liver disease associated with metabolic dysfunction, such as metabolic dysfunction-associated steatohepatitis (MASH), metabolic dysfunction-associated fatty livers disease (MAFLD), or metabolic dysfunction-associated steatotic liver disease (MASLD). The treatment comprises administration of a dual GLP-1 receptor and GIP receptor agonist.

The present disclosure provides antibodies that specifically bind to and in some cases inhibit the human glucose-dependent insulinotropic polypeptide (GIP) receptor. The antibodies find use in a variety of treatment, diagnostic, and monitoring applications, which are also described. For example, the antibodies may be used to treat a metabolic disorder, such as a disorder of glucose metabolism. In some embodiments, the antibody may have CDRs that are selected from any of the antibodies set forth in FIG. 9 or 10.

To develop a stable liquid formulation of a persistent conjugate of a peptide active against all developed glucagon receptors, GLP-1 receptors, and GIP receptors, which can be stored for extended periods without concerns about viral contamination. [Solution] The present invention relates to a liquid formulation of a sustained-release conjugate of glucagon, GLP-1, and GIP triple-active compound, and a method for producing the same.

The present disclosure provides compounds of the formula: and their pharmaceutically acceptable salts, as well as pharmaceutical compositions comprising these compounds and their use in the treatment of type II diabetes mellitus and obesity.

Provided are a pharmaceutical composition of GLP-1 and GIP receptor dual agonist and the use thereof. The pharmaceutical composition has good dissolution characteristics and stability.

To provide a human glucose-dependentinsulinotropicpolypeptide (GIP) receptor agonist.SOLUTION: A compound of the following formula or a pharmaceutically acceptable salt thereof is provided: Wherein A is phenyl, 6-membered N-containing heteroaryl or thienyl, wherein said phenyl, heteroaryl or thienyl is optionally substituted with one or two substituents independently selected from halo, CF3, CHF2, CH3, cyclopropyl, OH and CN, or when R1 is an optionally substituted 8, 9 or 10 membered N-containing bicyclic heterocycle, A may be absent and X is O or S.SELECTED DRAWING: None

Provided herein are methods for treating obesity or diabetes by administering a 15- PGDH inhibitor to a subject. In some cases, the methods provided herein additionally involve administering to a subject an agent selected from the group consisting of: a glucagon- like peptide- 1 (GLP-1) receptor agonist, a glucose-dependent insulinotropic polypeptide (GIP) receptor agonist, a glucagon receptor agonist, a GLP-1 receptor / GIP receptor co- agonist, a GLP-1 receptor agonist / GIP receptor antagonist, a GLP-1 receptor / glucagon receptor co-agonist, a GLP-1 receptor / GIP receptor / glucagon receptor triple agonist, a GLP-1 receptor / GLP-2 receptor co-agonist, a combination of a GLP-1 receptor agonist and an amylin receptor agonist.

The present disclosure provides methods of treating an overweight or obese patient with or without type 2 diabetes. The treatment comprises administration of a dual GLP-1 receptor and a GIP receptor agonist.

The invention herein provides pharmaceutically acceptable, controlled-release particulate compositions and formulations comprising such compositions for the treatment of obesity, diabetes, or both. The compositions and formulations herein comprise particulates containing an API and a biodegradable polymer compound. The API of the compositions and formulations herein exhibits detectable or significant agonist activity against one or more of the following: melanocortin-1 receptor (MC1), melanocortin-2 receptor (MC2), melanocortin-3 receptor (MC3), melanocortin-4 receptor (MC4), and melanocortin-5 receptor (MC5), GLP-1 receptor, glucagon receptor, and GIP receptor, and generally has a molecular weight of at least about 1000 Da.

The present disclosure provides compounds of the formula: and their pharmaceutically acceptable salts, as well as pharmaceutical compositions comprising these compounds and their use in the treatment of type II diabetes mellitus and obesity.

This invention provides a novel protein. Experimental results have shown that the protein has agonist activity at three receptors, namely the glucagon-like peptide 1 (GLP-1) receptor, the glucose-dependent insulinotropic polypeptide (GIP) receptor, and the glucagon (Gcg) receptor, and has both blood glucose lowering and body weight reducing functions.

Development of therapeutic agents for the prevention or treatment of sequelae of respiratory infectious diseases. [Solution] The present invention relates to the preventive or therapeutic use of a triplicate and / or conjugate having activity against glucagon, GLP-1, and GIP receptor for the sequelae of respiratory infection diseases.