72results about "Secretins" 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.

Disclosed are hybrid polypeptides that agonize GIP, GLP-1 and neuropeptide Y2 (NPY2) receptors and their medical use in the treatment of a variety of diseases, conditions or conditions, such as obesity, diabetes and / or NASH. The polypeptides have the general structure Z1-Z2-Z3 wherein Z1 is a hybrid polypeptide that provides GIPR and GLP1R agonism, Z2 is a linker, and Z3 is a polypeptide that provides hY2R agonism.

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.

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 present invention relates to triple agonists of the GLP1 / GIP / NPY2 receptor. Disclosed are hybrid polypeptides that agonize GIP, GLP-1 and neuropeptide Y2 (NPY2) receptors and their medical use in the treatment of a variety of diseases, conditions or conditions, such as obesity, diabetes and / or NASH. The polypeptides have the general structure Z1-Z2-Z3 wherein Z1 is a hybrid polypeptide that provides GIPR and GLP1R agonism, Z2 is a linker, and Z3 is a polypeptide that provides hY2R agonism.

The present disclosure relates to, inter alia, compositions and pharmaceutical composition s, including heterologous chimeric proteins that find use, inter alia, in the treatment of diabetes, obesity, or metabolic syndrome.

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 invention provides a fusion protein for treating metabolic diseases, and a preparation method and use thereof. The fusion protein has a general formula of R1-L-R2 or R2-L-R1, wherein R1 is FGF21 protein, an FGF21 protein analog, or a similar peptide with the biological function of FGF21 protein; R2 is GIP, mutant GIP or a similar peptide with the biological function of GIP; and L is a linker peptide. The fusion protein of the present invention is used as a therapeutic agent or a pharmaceutical composition in the treatment of diseases associated with hyperglycemia and hyperlipidemia, including diabetes, obesity, steatohepatitis or cardiovascular diseases,

This invention provides compounds suitable for oral administration that exhibit agonist activity at GIP and GLP-1 receptors. [Solution] The present invention provides compounds that are active in both the human glucose-dependent insulin-stimulating polypeptide (GIP) receptor and the glucagon-like peptide-1 (GLP-1) receptor. The present invention also relates to compounds that have a sustained action over a long period of time in each of these receptors. Furthermore, the present invention also relates to compounds that can be administered orally. These compounds may be useful in the treatment of type 2 diabetes mellitus ("T2DM"). These compounds may be useful in the treatment of obesity.

The present invention relates to glucose-dependent insulinotropic peptide (GIP) receptor (GIPR) antagonist GIP peptides in combination with glucagon-like peptide-1 (GLP-1) receptor agonists, such as GLP-1 peptides, for use in the treatment of obesity and obesity-related disorders, and GIPR antagonist GIP peptides for treating a subset of obesity-related disorders.

Disclosed is a method of modulating the Sct / SR axis in a mammalian subject in need thereof, including in a subject suffering from a liver disease, such as but not limited to, Early Stage PBC, Primary Sclerosing Cholangitis, Primary Biliary Cholangitis, Biliary Atresia, NASH, NAFLD, or Alcohol induced liver injury. A method of treating Late Stage PBC in a mammalian subject in need thereof is also disclosed; further disclosed is a method of ameliorating PBC-induced biliary damage in a mammalian subject in need thereof. Pharmaceutical compositions for modulating the Sct / SR axis, comprising a SR antagonist or a SR agonist, and a pharmaceutically acceptable carrier or excipient are also disclosed.

The present invention provides a process and intermediates for producing GIP / GLP1 dual agonist peptides, tilzepatide, or pharmaceutically acceptable salts thereof. [Solution] A process is provided for converting a depsipeptide isomer into a desired peptide, comprising: a. adjusting the pH of the depsipeptide isomer to approximately pH 7 to approximately pH 10; and b. incubating the depsipeptide isomer at pH 7 to pH 10 for at least 1 hour.

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 amino acid sequence: X1X2X3GTFX4SDYSX5X6X7X8X9X 10 X 11 X 12 X 13 X 14 FX 15 X 16 WLX 17 X 18 X 19 wherein X1 is Y or H, X2 is A or G or S, X3 is E or Q, X4 is I or T, X5 is I or K, X6 is A or Y or L or I, X7 is M or L, X8 is D or E, X9 is K or E, and X 10 is I or Q or K or E or L, and X 11 is H, A or R, and X 12 is A, Q, or V, and X 13 is K or Q or R or H, and X 14 is D or E or A or L, and X 15 is V or I, and X 16 is N or E or D or Q, and X 17 is L or I or K or V, and X 18 is A or E or K, and X 19 is Q or G, and X1 to X 13 X1 is Y, X2 is A, X3 is E, X4 is I, X5 is I, X6 is A, X7 is M, X8 is D, X9 is K, and X 10 is I and X 11 is H and X 12 is Q and X 13 is Q and X 14 is D and X 15 is V and X 16 is N and X 17 is L and X 18 is A and X 19 does not simultaneously satisfy Q. The GLP-1 / GIP dual targeting polypeptide can effectively reduce body weight and blood sugar level.

The present invention relates to long-acting glucagon-like peptide-1 and human glucose-dependent insulinotropic polypeptide (GIP) agonist polypeptides that may be useful in the treatment of type 2 diabetes (T2D), diabetes associated with obesity, obesity, and hyperlipidemia.

A GLP-1 / GIP dual-targeted polypeptide, containing a first polypeptide having the following amino acid sequence : X1X2X3GT FX4SDY SX5X6X7X8 X9X10X11X12X13 X14FX15X16W LX17X18X19, wherein X1 is Y or H, X2 is A or G or S, X3 is E or Q, X4 is I or T, X5 is I or K, X6 is A or Y or L or I, X7 is M or L, X8 is D or E, X9 is K or E, X10 is I or Q or K or E or L, X11 is H or A or R, X12 is A or Q or V, X13 is K or Q or R or H, X14 is D or E or A or L, X15 is V or I, X16 is N or E or D or Q, X17 is L or I or K or V, X18 is A or E or K, X19 is Q or G; X1~X13 do not satisfy at the same time that X1 is Y, X2 is A, X3 is E, X4 is I, X5 is I, X6 is A, X7 is M, X8 is D, X9 is K, X10 is I, X11 is H, X12 is Q, X13 is Q, X14 is D, X15 is V, X16 is N, X17 is L, X18 is A, X19 is Q. The GLP-1 / GIP dual-targeted polypeptide can effectively reduce the weight and blood sugar level.

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.

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.

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).