57 results about "GIP receptor" patented technology

To provide a pharmaceutical composition for prevention or treatment of metabolic syndrome.SOLUTION: The present invention provides a composition comprising: a glucagon derivative; and a GLP-1 receptor and GIP receptor dual agonist, and use thereof.SELECTED DRAWING: None

Methods and materials for treating mammals having cardiovascular and / or metabolic disease are provided herein. For example, methods and materials for treating mammals having cardiovascular and / or metabolic disease by administering (a) an analog of a natriuretic peptide (NP), such as atrial natriuretic peptide (ANP) or dendroaspis natriuretic peptide (DNP), and (b) a glucagon-like peptide-1 (GLP-1) receptor / glucose-dependent insulinotropic polypeptide (GIP) receptor agonist are provided herein. The NP analogs used in the methods provided herein can be less than 20 amino acids in length and, in some cases, can have one or more variations in their ring portion (as compared to wild type ANP or DNP) that affect the potency of the analog in activating the particulate guanylyl cyclase (GC-A) receptor.

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.

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

To provide glucose-dependent insulinotropic peptide (GIP)-derived peptide analogues which are antagonists of the GIP receptor.SOLUTION: The invention provides GIP-derived peptide analogues having specific sequences. The GIP peptide analogues are optimized by comprising amino acid substitutions A13Aib and / or N24E, and are fatty acid conjugated with / without a linker, thereby having improved solubility and / or physical stability.SELECTED DRAWING: None

The application discloses a GLP-1 / GIP receptor dual agonist and application thereof. The amino acid sequence general formula of the GLP-1 / GIP receptor dual agonist polypeptide compound is as follows: Tyr-Xaa1-Glu-Gly-Thr-Xaa2-Thr-Asn-Asp-Xaa3-Ser-Ile-Xaa4-Leu-Asp-Lys-Ile-Ala-Gln-Xaa5-Xaa6-Phe-Val-Gln-Trp-Leu-Xaa7-X aa8 -NH2. The application also relates to derivatives, long-acting compounds, pharmaceutically acceptable salts, pharmaceutical compositions and medicaments of the polypeptide compound. The GLP-1 / GIP receptor dual agonist polypeptide compound has more potential in preparation of drugs for treating metabolic syndrome and other diseases.

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 compounds of the Formula (IX), and their pharmaceutically acceptable salts, as well as pharmaceutical compositions comprising these compounds and their use as agonist at the human glucose-dependent insulinotropic polypeptide (GIP) in the treatment of type II diabetes mellitus and obesity.

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 present invention relates to GLP-1 receptor agonist compounds having an additional agonist activity over the GIP receptor and / or an agonist activity over the glucagon receptor and / or an antagonist activity over the GIP receptor for use in the treatment of joint diseases and / or joint pain and selected from the group comprising retatrutide, tirzepatide, orforglipron, mazdutide, efinopegdutide, froniglutide, maridebart cafraglutide, survodutide, efpeglenatide, ecnoglutide, efocipegtrutide and UBT251. The invention also relates to a pharmaceutical composition comprising at least one of the above mentioned GLP-1 receptor agonist compound, and a pharmaceutically acceptable excipient, for use in the treatment of joint diseases and / or joint pain.

Disclosed are glucose-dependent insulinotropic peptide (GIP)-derived peptide analogues which are antagonists of the GIP receptor. These GIP peptide analogues are optimized by comprising amino acid substitutions A13Aib and / or N24E, and are fatty acid conjugated with / without a linker, so to have improved solubility and / or physical stability.

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.

The GIP receptor agonists of the present disclosure have antiemetic properties and thus may be used to reduce or inhibit the frequency or severity of nausea or vomiting onset in a patient in need thereof.

Disclosed are glucose-dependent insulinotropic peptide (GIP)-derived peptide analogues which are antagonists of the GIP receptor. These GIP peptide analogues are modified by comprising one or more individual amino acid substitutions and are fatty acid conjugated with / without a linker, so to have improved antagonistic activity and improved pharmacokinetic profile.

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 an RNAi preparation for preventing or treating obesity and a combination therapy using the same, and more specifically, to a pharmaceutical composition for preventing or treating obesity and a combination preparation with a GLP-1 receptor agonist or a GLP-1 / GIP receptor dual agonist, which comprises an RNAi preparation as an active ingredient, the RNAi formulation comprises an antisense strand that is complementary to the MARC1mRNA sequence and a sense strand that is complementary to the antisense strand.

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.

Provided is a fusion protein, which can simultaneously target the GLP1 receptor or GLP1 / GCG receptors or GLP1 / GCG / GIP receptors, and the FGF21 receptor, can exhibit excellent effects of weight loss, improvement of NAS, etc., and can be used for treating related diseases.

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.