540 results about "Insulin secretion" patented technology

The present invention relates to a therapeutic agent for diabetes with sulfonylurea secondary failure, which contains a GPR40 agonist. According to the present invention, a therapeutic agent for diabetes with sulfonylurea secondary failure that affords a superior insulin secretion effect and a superior hypoglycemic effect even in diabetic patients for whom a sulfonylurea compound or a fast-acting insulin secretagogue fails to provide an insulin secretion effect and therefore, fails to provide a sufficient hypoglycemic effect can be provided.

The present invention relates generally to novel GIP analogs and GIP hybrid polypeptides with selectable properties, useful as agents for the treatment and prevention of metabolic diseases and disorders, for example those which can be alleviated by control plasma glucose levels, insulin levels, and / or insulin secretion, positive inotropic effects, reduction of catabolic effects, slowing of gastric emptying. Such conditions and disorders include, but are not limited to, hypertension, dyslipidemia, cardiovascular disease, eating disorders, critical care, insulin-resistance, obesity, and diabetes mellitus of any kind, including type 1, type 2, and gestational diabetes.

The present invention relates generally to novel GIP analogs and GIP hybrid polypeptides with selectable properties, useful as agents for the treatment and prevention of metabolic diseases and disorders, for example those which can be alleviated by control plasma glucose levels, insulin levels, and / or insulin secretion, positive inotropic effects, reduction of catabolic effects, slowing of gastric emptying. Such conditions and disorders include, but are not limited to, hypertension, dyslipidemia, cardiovascular disease, eating disorders, critical care, insulin-resistance, obesity, and diabetes mellitus of any kind, including type 1, type 2, and gestational diabetes.

The present invention relates generally to novel, selectable hybrid polypeptides useful as agents for the treatment and prevention of metabolic diseases and disorders which can be alleviated by control plasma glucose levels, insulin levels, and / or insulin secretion, such as diabetes and diabetes-related conditions. Such conditions and disorders include, but are not limited to, hypertension, dyslipidemia, cardiovascular disease, eating disorders, insulin-resistance, obesity, and diabetes mellitus of any kind, including type 1, type 2, and gestational diabetes.

The present invention provides novel human glucagon-like peptide-1 (GLP-1) peptide mimics that mimic the biological activity of the native GLP-1 peptide and thus are useful for the treatment or prevention of diseases or disorders associated with GLP activity. Further, the present invention provides novel, chemically modified peptides that not only stimulate insulin secretion in type II diabetics, but also produce other beneficial insulinotropic responses. These synthetic peptide GLP-1 mimics exhibit increased stability to proteolytic cleavage making them ideal therapeutic candidates for oral or parenteral administration.

An agent for treating diabetes with sulfonylurea secondary failure which comprises a dipeptidyl peptidase IV inhibitor. The agent of the present invention is an agent for treating diabetes with sulfonylurea secondary failure showing excellent insulin-secreting and hypoglycemic effects on even diabetic patients on whom a sulfonylurea compound or a fast-acting insulin secretagogue has no insulin-secreting effect and therefore no sufficient hypoglycemic effect.

The present invention relates generally to novel GIP analogs and GIP hybrid polypeptides with selectable properties, useful as agents for the treatment and prevention of metabolic diseases and disorders, for example those which can be alleviated by control plasma glucose levels, insulin levels, and / or insulin secretion, positive inotropic effects, reduction of catabolic effects, slowing of gastric emptying. Such conditions and disorders include, but are not limited to, hypertension, dyslipidemia, cardiovascular disease, eating disorders, critical care, insulin-resistance, obesity, and diabetes mellitus of any kind, including type 1, type 2, and gestational diabetes.

In general this invention can be viewed as encompassing novel methods of treating diabetes and insulin resistance. The inventors have made the discovery that increasing secretion of endogenous glucagon-like peptide-1 (GLP-1) in combination with inhibiting the activity of dipeptidyl peptidase I (DPP-IV) can have a significant impact on hyperglycemia and insulin secretion in subjects suffering from diabetes and / or insulin resistance. Further the invention encompasses methods of identifying subjects having elevated secretion of GLP-1, methods of assessing sensitivity to a GLP-1 secretagogue, and methods of treating diabetes in these subjects by administering a GLP-1 secretagogue to alleviate at least one symptom of diabetes.

The present invention is directed to Nogo-A antagonists useful for the control of blood glucose or blood insulin levels in a subject and related use and formulation thereof. In particular, the invention is directed to Nogo-A antagonists useful for the prevention, repression or treatment insulin secretion deficiency and related methods and pharmaceutical formulations. In particular, the invention relates to Nogo-A antagonists useful in the treatment of diabetes mellitus.

The present invention provides novel human glucagon-like peptide-1 (GLP-1)-receptor modulators that have biological activity similar or superior to native GLP-1 peptide and thus are useful for the treatment or prevention of diseases or disorders associated with GLP activity. Further, the present invention provides novel, chemically modified compounds that not only stimulate insulin secretion in type II diabetics, but also produce other beneficial insulinotropic responses. These synthetic peptide GLP-1 receptor modulators exhibit increased stability to proteolytic cleavage making them ideal therapeutic candidates for oral or parenteral administration. The compounds of this invention show desirable pharmacokinetic properties and desirable potency in efficacy models of diabetes.

A compound represented by the formula (I) wherein one of R1 and R2 is a hydrogen atom or a substituent and the other is an optionally substituted cyclic group; W is a bond or a divalent aliphatic hydrocarbon group; Y is a group of the formula: —OR3 (wherein R3 is a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted heterocyclic group or an optionally substituted acyl group) or an optionally esterified or amidated carboxyl group, or a salt thereof or a prodrug thereof has a superior insulin secretion promoting action and a hypoglycemic action and shows low toxicity. Therefore, the compound is useful as a pharmaceutical agent, particularly as an agent for the prophylaxis or treatment of diabetes and diabetic complications, and the like.

A convenient screening tool and a convenient screening method for obtaining an agent for treating diabetes, a pharmaceutical composition for treating diabetes, and a process for manufacturing the pharmaceutical composition are disclosed. The screening tool is a G protein-coupled receptor, a variation functionally equivalent thereto, or a homologous polypeptide thereof which promotes insulin secretion under a high glucose concentration by activation, or cells transformed with an expression vector comprising a polynucleotide encoding the above polypeptide and expressing the polypeptide.

Methods for treating diabetes by increasing the insulin secretion by administration of a GLP-1 receptor agonist and / or a DPP-IV inhibitor in combination with a proton pump inhibitor and optionally a PPAR agonist are provided.

The present invention belongs to the technical field of biological pharmacy, and in particular relates to a preparation and purification method of tetra-hydroxyl xanthone mango aglycone (norathyriol), and an application thereof in hypoglycemic medicine. Based on biological experiments, mango glycoside is used as raw material; under the condition with phenol and hydroiodic acid, carbon-carbon bonds are broken to produce the crude product of mango aglycone; the crude product is separated and purified through silica gel column chromatography so that the mango aglycone is separated; the yield rate reaches 12 percent, the purity is higher than 95 percent, and the reproduction performance is good; the IGTT of C57BL / 6 normal mice is effectively improved with the norathyriol; and simultaneously the quantity of insulin secretion induced by glucose in vivo for the C57BL / 6 normal mice can be improved with the norathyriol. Therefore, the mango aglycone can be applied for preparation of hypoglycemic medicine.

The Present invention relates generally to novel GIP analogs and GIP hybrid polypeptides with selectable properties, useful as agents for the treatment and prevention of metabolic diseases and disorders, for example those which can be alleviated by control plasma glucose levels, insulin levels, and / or insulin secretion, positive inotropic effects, reduction of catabolic effects, slowing of gastric emptying. Such conditions and disorders include, but are not limited to, hypertension, dyslipidemia, cardiovascular disease, eating disorders, critical care, insulin-resistance, obesity, and diabetes mellitus of any kind, including type 1, type 2, and gestational diabetes.

The invention relates to an intelligent insulin pump system comprising an open-ring type insulin pump which is provided with an electric control unit, the electric control unit of the insulin pump is bidirectionally connected with an upper computer through a wireless module or a USB interface, insulin injecting management software is arranged in the upper computer which receives equipment information, setting information and insulin injection historical information from the insulin pump, and an insulin secretion curve model is generated by the insulin injecting management software and then is inputted to the electric control unit of the insulin pump to control the operation of the insulin pump. Because the insulin secretion curve model is automatically generated or manually established in the insulin injecting management software on the upper computer and is transmitted to the insulin pump by utilizing modules comprising Zigbee and the like in a wireless form or utilizing the USB interface in a wired form, the intelligent insulin pump system dispenses with the trouble of setting a large number of insulin outputting parameters in only several keys and LCD (Liquid Crystal Display) layering menus, thereby being convenient for the operation of users.

This invention relates to modified Vasoactive Intestinal Peptide (VIP) / Pituitary Adenylate Cyclase Activating Peptide (PACAP) Receptor 2 (VPAC2) agonists (VPAC2 agonists) comprising a VPAC2 agonist linked to a polyethylene glycol polymer, as well as related formulations, dosages, and methods of administration thereof for therapeutic purposes. These VPAC2 agonists, compositions, and methods are useful in providing a treatment option for those individuals afflicted with a metabolic disorder such as diabetes, impaired glucose tolerance, metabolic syndrome, or prediabetic states, by inducing glucose-dependent insulin secretion in the absence of the therapeutically limiting side effect of reducing or lowering blood pressure.

The present invention relates generally to novel GIP analogs and GIP hybrid polypeptides with selectable properties, useful as agents for the treatment and prevention of metabolic diseases and disorders, for example those which can be alleviated by control plasma glucose levels, insulin levels, and / or insulin secretion, positive inotropic effects, reduction of catabolic effects, slowing of gastric emptying. Such conditions and disorders include, but are not limited to, hypertension, dyslipidemia, cardiovascular disease, eating disorders, critical care, insulin-resistance, obesity, and diabetes mellitus of any kind, including type 1, type 2, and gestational diabetes.

There are provided novel pyrimidine derivatives which has been fused with an aromatic heterocycle selected from thiophene, thiazole and pyridine or pharmaceutically acceptable salts thereof; and a pharmaceutical composition comprising said compound as an active ingredient. These compounds exhibit excellent promoting activity on insulin secretion and activity against hyperglycemia. Hence, the pharmaceutical compositions comprising such compounds as active ingredients, based on these actions, are useful for treating and / or preventing insulin-dependent diabetes (type 1 diabetes), non-insulin-dependent diabetes (type 2 diabetes), insulin-resistant diseases, obesity, and the like.

This invention relates to a series of substituted cyclohexane containing analogues which are agonists of GPR119 intended to treat metabolic diseases mediated by GPR119 including Type I & II diabetes mellitus. Diabetes mellitus is an ever-increasing threat to human health causing various complications (blindness, kidney failure, neuropathy, heart attack, stroke, etc.). Recently it was found that activation of GPR119 which is highly expressed in pancreatic beta cells causes glucose dependent insulin secretion and GLP-1 release. Many pharmaceuticals are currently developing GPR119 agonists and herein we disclose alternative GPR119 agonists. Our invention describes GPR119 agonists having structural Formula (I), pharmaceutically acceptable salt or solvate of Formula (I), isomer or prodrug of Formula (I), and combination therapy of Formula (I) with other anti-diabetic drugs like DPP-IV inhibitors and / or insulin sensitizers.

The present invention relates to a mutant polypeptide of glucagon-like peptide-1 (GLP-1) and a modified compound thereof. In particular, a lysine is added in front of the end N of the glucagon-like peptide-1 to form the mutant polypeptide, and the glucagon-like peptide-1 includes natural GLP-1(7-36)amide or GLP-1(7-37) and a partial amino acid-subsituted derivative. Not only do the GLP-1 mutant polypeptide and the modified compound thereof show the effects of promoting insulin secretion and lowering blood sugar, but also, compared with the natural GLP-1, the stability and internal action time of the GLP-1 mutant polypeptide and the modified compound thereof are notably increased in respect to proteolytic enzyme, and the GLP-1 mutant polypeptide and the modified compound thereof can be used for the preparation of drugs treating diabetes or adiposity.

The present invention relates to methods and compositions for treating or ameliorating the effects of diabetes. In addition, the present invention relates to methods and compositions for treating or preventing hyperglycemia, as well as modulating monoamine levels, islet β-cell insulin secretion, insulin and / or glucagon levels in a patient. In certain preferred embodiments, such methods include administering to a patient an effective amount of a vesicular monoamine transporter type 2 (VMAT2) antagonist, such as tetrabenazine (TBZ), dihydrotetrabenazine (DTBZ), tetrahydroberberine (THB), reserpine, emetine, Compound 6, or enantiomers, optical isomers, diastereomers, N-oxides, crystalline forms, hydrates, metabolites or pharmaceutically acceptable salts thereof.

The present invention provides novel human glucagon-like peptide-1 (GLP-1) peptide mimics that mimic the biological activity of the native GLP-1 peptide and thus are useful for the treatment or prevention of diseases or disorders associated with GLP activity. Further, the present invention provides novel, chemically modified peptides that not only stimulate insulin secretion in type II diabetics, but also produce other beneficial insulinotropic responses. These synthetic peptide GLP-1 mimics exhibit increased stability to proteolytic cleavage making them ideal therapeutic candidates for oral or parenteral administration.

This invention uses placental alkaline phosphatase (“PALP”), and other members of the alkaline phosphatase family, to reduce the death and thereby maintain or enhance the viability and function of insulin-producing islet β-cells including insulin secretion. PALP may be administered to a patient that has received transplanted islet cells to protect the transplanted islets against ROS-mediated attacks by the patient's immune system. Transferrin and other promoters of islet survival may also be used to enhance the effects of PALP on islet viability both in vivo and in vitro.

Provided are a method for promoting insulin secretion, a method for suppressing the elevation of a blood glucose level, a method for ameliorating diabetes mellitus, a method for promoting growth of an animal, and a method for increasing an insulin level in breast milk. These methods comprising administering at least one member selected from the group consisting of a di- or a higher saccharide containing galactose, a derivative thereof, a saccharide containing N-acetylneuraminic acid, and a derivative thereof, to a patient in need thereof or an animal.

The present disclosure relates to an exendin-4 analogue PEGylated with polyethylene glycol or a derivative thereof, a preparation method, and a pharmaceutical composition for prevention or treatment of diabetes containing the same as an active ingredient. According to the present invention, the yield of an exendin-4 analogue can be increased via the selective PEGylation by using exendin-4 in which a cysteine is introduced into #40 site of the C-terminal, and treatment effect of medications can be increased, so that the exendin-4 analogue can be usefully applied as a composition for prevention or treatment of diseases caused by insulin hypersecretion.

The present invention provides novel human glucagon-like peptide-1 (GLP-1)-receptor modulators that have biological activity similar or superior to native GLP-1 peptide and thus are useful for the treatment or prevention of diseases or disorders associated with GLP activity. Further, the present invention provides novel, chemically modified peptides that not only stimulate insulin secretion in type II diabetics, but also produce other beneficial insulinotropic responses. These synthetic peptide GLP-1 receptor modulators exhibit increased stability to proteolytic cleavage making them ideal therapeutic candidates for oral or parenteral administration. The peptides of this invention show desirable pharmacokinetic properties and desirable potency in efficacy models of diabetes.

The present invention relates generally to novel GIP analogs and GIP hybrid polypeptides with selectable properties, useful as agents for the treatment and prevention of metabolic diseases and disorders, for example those which can be alleviated by control plasma glucose levels, insulin levels, and / or insulin secretion, positive inotropic effects, reduction of catabolic effects, slowing of gastric emptying. Such conditions and disorders include, but are not limited to, hypertension, dyslipidemia, cardiovascular disease, eating disorders, critical care, insulin-resistance, obesity, and diabetes mellitus of any kind, including type 1, type 2, and gestational diabetes.

The invention discloses a fusion protein of exendin-4 peptide and human serum albumin (HSA) and a preparation method thereof, belonging to the technical field of long-term recombination fusion protein medicine. The invention relates to a preparation method and a product of fusion protein of insulin secretion promoting peptide (Exendin-4) and human serum albumin (HSA). The fusion protein is characterized in that a genetic engineering method is adopted to directly fuse a single Exndin-4 peptide and HAS and without connecting peptide at the middle part to form stable and long half-life period Exendin-4-HAS fusion protein, and is applied in a treatment of non-insulin-dependent diabetes and obesity.