50 results about "Glucose-dependent insulinotropic polypeptide" patented technology

A GLP-1 / GIP dual-targeted polypeptide, containing a first polypeptide having the following amino acid sequence: X1X2X3GT FX4SDY SX5X6X7X8 X9X10X11X12X13 X14FX15X16W LX17X18X19. The GLP-1 / GIP dual-targeted polypeptide can effectively reduce the weight and blood sugar level.

Described herein is a method of treating a disease or condition, for example, obesity, weight gain, or diabetes, comprising administering to a subject in need thereof a glucose-dependent insulinotropic polypeptide receptor (GIPR) antagonist and a glucagon-like peptide 1 receptor (GLP-1R) agonist. Further described herein are pharmaceutical compositions comprising a GIPR antagonist and a GLP-1R agonist, which may be useful in the treatment of a disease or condition, for example, obesity, weight gain, or diabetes.

Described herein is a method of treating a disease or condition, for example, obesity, weight gain, or diabetes, comprising administering to a subject in need thereof a glucose-dependent insulinotropic polypeptide receptor (GIPR) antagonist and a glucagon-like peptide 1 receptor (GLP-1R) agonist. Further described herein are pharmaceutical compositions comprising a GIPR antagonist and a GLP-1R agonist, which may be useful in the treatment of a disease or condition, for example, obesity, weight gain, or diabetes.

Described herein is a method of treating a disease or condition, for example, obesity, weight gain, or diabetes, comprising administering to a subject in need thereof a glucose-dependent insulinotropic polypeptide receptor (GIPR) antagonist and a glucagon-like peptide 1 receptor (GLP-1R) agonist. Further described herein are pharmaceutical compositions comprising a GIPR antagonist and a GLP-1R agonist, which may be useful in the treatment of a disease or condition, for example, obesity, weight gain, or diabetes.

Incretin analogs are provided that have activity at each of the glucose-dependent insulinotropic polypeptide (GIP), glucagon-like peptide-1 (GLP-1) and glucagon (GCG) receptors. The incretin analogs have structural features resulting in balanced activity and extended duration of action at each of these receptors. Methods also are provided for treating diseases such as type 2 diabetes mellitus, dyslipidemia, metabolic syndrome, non-alcoholic fatty liver disease, non-alcoholic steatohepatitis and obesity.

The invention relates to the technical field of polypeptide drugs for metabolic diseases, in particular to a glucagon-like peptide (GLP-1), a glucose-dependent insulinotropic polypeptide (GIP) and a glucagon (GCG) triple receptor agonist (protein). According to the triple receptor agonist protein provided by the technical scheme, weight reduction is achieved, meanwhile, lower side effects are shown, and drug compliance is enhanced. The triple receptor stimulant researched and developed by the technical scheme can be applied to preparation of medicines with the effects of losing weight, reducing lipid or reducing blood sugar, solves the technical problem that the existing GLP-1, GIP and GCG triple receptor stimulants are difficult to reduce side effects while reducing body weight, and breaks through the weight loss mode that the traditional medicines depend on appetite suppression; due to the unique action mechanism and good safety, a safer and more effective treatment scheme is provided for patients, and the medicine has wide market prospects and social benefits.

The invention pertains to pharmaceutical compositions containing a GIP (glucose-dependent insulino-tropic polypeptide) and GLP-1 (Glucagon-like peptide-1) receptor agonist. In particular, the invention provides pharmaceutical compositions containing tirzepatide. The pharmaceutical compositions according to the invention are physically and chemically stable, are easy to manufacture and suitable for parenteral administration. The invention further provides methods for making the same as specified in the claims.

Described herein are compounds of Formula I:and their pharmaceutically acceptable salts, wherein R1, R2, R3, Rp, A1, L1, L2, T1, T2, T3, T4, n1, t1, t2, and t3 are defined herein; their use as GIPR antagonists; pharmaceutical compositions containing such compounds and salts; and the use of such compounds and salts to treat or prevent, for example, obesity, weight gain, and / or T2DM.

Described herein are compounds of Formula (I): I and their pharmaceutically acceptable salts, wherein R1, R2, R3, Rp, A1, L1, L2, T1, T2, T3, T4, n1, t1, t2, and t3 are defined herein; their use as GIPR antagonists; pharmaceutical compositions containing such compounds and salts; and the use of such compounds and salts to treat or prevent, for example, obesity, weight gain, and / or T2DM.

Provided herein are peptides and peptide conjugates comprising a dual glucose-dependent insulinotropic polypeptide (GIP) and GLP-1 receptor agonist. The peptides may be used for blood glucose management and treating conditions such as diabetes, obesity, non-alcoholic fatty liver disease (NAFLD), and non-alcoholic steatohepatitis (NASH).

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 relates to peptide compounds which are dual or tri-agonists of the human glucagon-like peptide-1 (GLP-1) receptor (GLP1R), the human glucose-dependent insulinotropic polypeptide (GIP) receptor (GIPR), and / or the human glucagon receptor (GCGR). The invention also relates to peptide compounds that are suitable for oral administration. These peptide compounds of the invention may be useful in the treatment of type 2 diabetes mellitus (T2DM) and obesity.

Described herein are compounds of Formula I: and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, L1, T1, T2, T3, T4, t1, and t2 are defined herein; the use thereof as a GIPR antagonist; pharmaceutical compositions containing such compounds and salts; and the use of such compounds and salts for the treatment or prevention of e.g. Obesity, weight gain and / or T2DM.

Doses and dosing regimens for incretin analogs are disclosed comprising determining and administering doses of long-acting incretin analogs suitable for once-weekly dosing, such as a glucose-dependent insulinotropic polypeptide (GIP), glucagon-like peptide-1 (GLP-1) and glucagon (GCG) (GGG) tri-receptor agonist.

The subject matter disclosed herein is generally directed to methods and compositions for preventing, suppressing or treating obesity and / or obesity-induced disorders, specifically, select piperidine urea-derived compounds as a monotherapy or a combination therapy with glucagon-like peptide 1 (GLP-1 – SEQ ID NO: 1) receptor agonist and / or dual GLP-1 (SEQ ID NO: 1) and glucose-dependent insulinotropic polypeptide GIP (SEQ ID NO: 8) receptor agonist for the treatment of obesity.

Provided is dual target agonist peptides, and more specifically to a series of dual target agonists that can simultaneously activate the human Glucagon like peptide-1 (GLP-1) receptor and the human glucose dependent insulinotropic polypeptide (GIP) receptor, as well as its pharmaceutical salts and pharmaceutical compositions. The peptides have dual agonist effect and can be used for the treatment of diabetes, obesity and other related diseases.

Doses and dosing regimens for incretin analogs are disclosed comprising determining and administering doses of long-acting incretin analogs suitable for once-weekly dosing, such as a glucose-dependent insulinotropic polypeptide (GIP), glucagon-like peptide-1 (GLP-1) and glucagon (GCG) (GGG) tri-receptor agonist.

The invention provides an insulinotropic polypeptide analogue and application thereof, and relates to the technical field of polypeptide preparation and application thereof. The intestinal insulinotropic polypeptide analogue comprises a co-agonist, the co-agonist is GLP-1, GIP and GCG three-receptor co-agonist polypeptide which is in acylation connection with a fatty acid side chain, and the amino acid sequence of the polypeptide or a salt thereof or a solvate thereof is shown as the following formula: Y (Aib) QGTFTSDX10SIX13LDX16X17AQ (Aib) X21FIX24X25LX27EGGPSSGAPPPS-NH2. In the present invention, it provides an enteric insulinotropic analogue having activity in each of a glucose-dependent insulinotropic polypeptide, a glucagon-like peptide-1, and a glucagon receptor, the polypeptide analogue can be used for treating and preventing metabolic disorders and other diseases including diabetes mellitus, obesity, metabolic syndromes and related diseases through various administration modes, and the polypeptide analogue can be used for treating and preventing metabolic disorders including diabetes mellitus, obesity, metabolic syndromes and related diseases through various administration modes.

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 invention provides compositions and methods for treating Postural orthostatic tachycardia syndrome (POTS). In some embodiments, the POTS is associated with hypermobility spectrum disorders / hypermobile Ehlers-Danlos syndrome (HSD / hEDS). In various embodiments, the invention relates to administering a composition comprising an effective amount of a molecular antagonist of Glucose-dependent Insulinotropic Polpeptide (GIP) to a patient in need thereof. In various embodiments, the molecular antagonist can be provided in a form for convenient self-administration upon the onset of symptoms or to prevent or reduce postprandial POTS symptoms, or in other embodiments, is administered at a set frequency.

This invention relates to a polypeptide compound and its applications, and more specifically, to a dual or triple agonist polypeptide drug that activates glucagon-like peptide-1 receptor and optionally glucose-dependent insulinotropic peptide receptor and glucagon receptor, and its application in the treatment of metabolic syndrome.

The present invention relates to novel peptides, which are derivatives of glucose-dependent insulinotropic polypeptide (GIP) analogs, having improved physical stability in solution and prolonged action curves. More specifically, the present invention relates to such peptides that are agonists for GIP receptors, and to their use in weight management or treatment of diseases such as obesity, diabetes or non-alcoholic steatohepatitis (NASH).

The present invention belongs to the field of polypeptide pharmaceuticals, and provides a dual agonist polypeptide compound and the pharmaceutical use thereof. An amino acid sequence of a GIP-R and GLP-1R dual agonist polypeptide compound is: Y1-X1-EGTFTSDYSI-X2-LDKI-X3-Q-Bn-X4-X5-VQWLI-X6-GGPSSG-X7-PPPS, and the C-terminal amino acid is amidated. The GIP-R and GLP-1R dual agonist polypeptide compound has a more significant dual agonistic effect on human glucose-dependent insulinotropic polypeptide (GIP) and human glucagon-like peptide-1 (GLP-1) receptors. The compound not only has the effects of lowering blood sugar and reducing weight, but also has a longer half-life and a higher bioavailability. The compound can avoid adverse reactions such as nausea and vomiting caused by the long-term use of existing drugs, and thus can be used as an effective raw material for the preparation of a drug for treating or preventing diabetes or an anti-obesity drug.

The invention relates to an engineering strain for intestinal delivery of a GLP-1 / GIP dual-receptor stimulant and application thereof, the strain takes uracil nutrition deletion type saccharomyces boulardii as a chassis strain, and a polypeptide expression module is integrated in a genome of the chassis strain; the polypeptide expression module comprises a secretory signal peptide coding sequence and a polypeptide coding sequence fused with the secretory signal peptide coding sequence, and the polypeptide coding sequence codes polypeptide formed by connecting a plurality of glucagon-like peptide-1 repetitive units and a plurality of glucose-dependent insulinotropic polypeptide repetitive units in series; restriction enzyme cutting sites which can be cut by yeast endogenous protease are arranged between the adjacent repeating units, so that the polypeptide is cut in a Golgi apparatus or a secretion processing process, and mature GLP-1 agonist and GIP agonist are released. The strain can be orally taken, can continuously control the delivery of GLP-1 / GIP dual agonists in an accurate dosage manner, so that the obesity and metabolic disorder are effectively improved, and the administration compliance and safety are improved.

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.

Described herein are compounds of Formula I:and their pharmaceutically acceptable salts, wherein R1, R2, R3, Rcy, L1, L2, T1, T2, T3, T4, n1, t1, t2, and t3 are defined herein; their use as GIPR antagonists; pharmaceutical compositions containing such compounds and salts; and the use of such compounds and salts to treat or prevent, for example, obesity, weight gain, and / or T2DM.

Described herein are compounds of Formula I: and their pharmaceutically acceptable salts, wherein R1, R2, R3, A1, L1, L2, T1, T2, T3, T4, n1, t1, and t2 are defined herein; their use as GIPR antagonists; pharmaceutical compositions containing such compounds and salts; and the use of such compounds and salts to treat or prevent, for example, obesity, weight gain, and / or T2DM.

The present invention relates to long acting glucagon-like peptide-1 and human glucose-dependent insulinotropic polypeptide (GIP) dual agonist polypeptide which may be useful for treating type 2 diabetes mellitus (T2D), diabetes with obesity, obesity and hyperlipidemia.

Described herein are compounds of Formula (I) and their pharmaceutically acceptable salts, wherein R1, R2, R3, Rcy, A1, L1, L2, T1, T2, T3, T4, n1, t1, t2, and t3 are defined herein; their use as GIPR antagonists; pharmaceutical compositions containing such compounds and salts; and the use of such compounds and salts to treat or prevent, for example, obesity, weight gain, and / or T2DM.

The present subject matter relates to a stable pharmaceutical compositions comprising an incretin analog with activity at glucose-dependent insulinotropic polypeptide (GIP) receptor and glucagon-like peptide- 1 (GLP-1) receptor. The present subject matter relates to a stable pharmaceutical composition, comprising tirzepatide or pharmaceutically acceptable salts thereof as an active ingredient and a suitable buffer. Further provided is a process for preparing the stable pharmaceutical composition comprising tirzepatide or pharmaceutically acceptable salts thereof.