31results about "Secretins" patented technology

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 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.

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.

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 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 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 GIP / GLP1 dual agonist peptides.SOLUTION: Provided is, for example, a compound of SEQ ID NO:10 shown below or a pharmaceutically acceptable salt thereof, where the compound may be bonded to a resin, and one or more of the protecting groups Fmoc, Trt and / or Boc may be independently substituted with an alternative protecting group.SELECTED DRAWING: None

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.

A fusion protein having a triple activity and a use thereof are provided. More specifically, a fusion protein has a triple biological activity of glucagon-like peptide-1 (GLP-1), glucose-dependent insulinotropic polypeptide (GIP), and epidermal growth factor 21 (FGF21). It can be used for treating type 2 diabetes (T2D), obesity, and other diseases related to glucose and lipid metabolic abnormalities.

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.

A fusion protein having a triple activity and a use thereof are provided. More specifically, a fusion protein has a triple biological activity of glucagon-like peptide-1 (GLP-1), glucose-dependent insulinotropic polypeptide (GIP), and epidermal growth factor 21 (FGF21). It can be used for treating type 2 diabetes (T2D), obesity, and other diseases related to glucose and lipid metabolic abnormalities.

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

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

Hybrid polypeptides that stimulate GIP, GLP-1, and neuropeptide Y2 (NPY2) receptors and their pharmaceutical uses in the treatment of various diseases, conditions, or disorders, such as obesity, diabetes, and / or NASH, are disclosed. The polypeptides have the general structure Z1-Z2-Z3, where Z1 is a hybrid polypeptide that provides GIP and GLP1R agonism, Z2 is a linker, and Z3 is a polypeptide that provides NPY2R agonism.