69 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 regards 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.

Provided are a GLP1 analogue and GLP1 / GIP receptor co-agonist analogues, a fusion protein comprising the GLP1 analogue or the GLP1 / GIP receptor co-agonist analogue, and methods of use thereof. In various embodiments, the fusion protein comprises the GLP1 analogue or the GLP1 / GIP receptor co-agonist analogue fused to a protecting antibody or further fused to a stabilizing domain. In some embodiments, the fusion proteins are useful for treating or ameliorating a symptom or indication of a disorder such as obesity and diabetes.

Provided is a tri-agonist polypeptide compound targeting a GLP-1 receptor, a glucagon receptor and a GIP receptor, wherein the polypeptide compound can selectively act on the GLP-1 receptor, the glucagon receptor and the GIP receptor, so as to exert the activities of GLP-1, glucagon and GIP at the same time, and the polypeptide compound has a unique agonistic activity proportion for the three receptors, thus achieving better glucose reduction, weight reduction and lipid regulation effects.

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.

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.

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

The present disclosure provides GIP receptor agonist peptide compounds suitable for once per day dosing (QD), said peptide compounds having an activating action on GIP receptors and use of the GIP receptor agonist peptide as a medicament for the treatment and / or prevention of emesis, or a symptom or condition associated with emesis while having an improved profile.

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 invention herein provides pharmaceutically acceptable, controlled-release microparticle composition(s) and formulation(s) comprising such composition(s) for use in the treatment of obesity, diabetes, or both. Composition(s) and formulation(s) herein comprise microparticles comprising API(s) and biodegradable polymer compound(s). API(s) of composition(s) and formulation(s) herein demonstrate detectable or significant agonist activity against one or more of 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 typically have a molecular weight of at least about 1000 Da.

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 invention discloses a long-acting GLP-1 / GIP / Y2 receptor triple agonist as well as a preparation method and application thereof, the amino acid sequence of the receptor triple agonist is as shown in the following general formula (I), and the receptor triple agonist can act on a GLP-1 receptor, a GIP receptor and a Y2 receptor at the same time and can play the activities of GLP-1, GIP and PYY at the same time. The GLP-1 / GIP / Y2 receptor triple agonist disclosed by the invention has the effects of effectively reducing blood sugar and weight and regulating lipid. The compound has greater potential when being applied to medicines for treating metabolic syndromes, such as diabetes, obesity, non-alcoholic fatty liver diseases, non-alcoholic steatohepatitis, dyslipidemia and other diseases. # imgabs0 #

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.