Class / Patent application number | Description | Number of patent applications / Date published |
514700200 | Glucagon, glucagon-like peptide (e.g., GLP-1, etc.) or derivative affecting or utilizing | 85 |
20100267629 | Enterostatin as Therapeutic Agent for Hypoglycemia - It has been discovered that enterostatin injections into mice caused an increase in blood glucose levels within 15 minutes of injection, and the glucose levels remained high for up to an hour after injection. In addition, mice injected with enterostatin showed less of an initial decrease in blood glucose following an insulin injection. Enterostatin was also shown to decrease AMPK activity in both mice and human tissues, which is additional support that glucose production is increased after enterostatin injection. This ability to enhance glucose production indicates that enterostatin could be used to treat hypoglycemia. | 10-21-2010 |
20100292143 | PYRROLE-2-CARBOXAMIDE DERIVATIVES AS GLUCOKINASE ACTIVATORS, THEIR PROCESS AND PHARMACEUTICAL APPLICATION - Pyrrole-2-carboxamide derivatives, their polymorphs, stereoisomers, prodrugs, solvates, pharmaceutically acceptable salts and formulations thereof, beneficial for prophylaxis, management, treatment, control of progression, or adjunct treatment of diseases and/or medical conditions where the activation of glucokinase would be beneficial, are disclosed. The disclosure also provides process of preparation of these pyrrole-2-carboxamides. | 11-18-2010 |
20100292144 | SUSTAINED DELIVERY OF EXENATIDE AND OTHER PEPTIDES - Described herein are implantable devices, formulations and methods of making implantable devices for the release of a polypeptide from an implantable device, and methods of use thereof. | 11-18-2010 |
20100305032 | Novel GLP-1 Derivatives - Novel polypeptide derivatives having protracted profile of action. | 12-02-2010 |
20100317576 | METHODS OF ENHANCING DIABETES RESOLUTION - Disclosed are compositions and methods for increasing diabetes resolution in a diabetic patient having undergone gastric restrictive surgery, entailing use of active agent that produces an incretin-like effect in the patient. | 12-16-2010 |
20100323956 | GLUCOSE-REGULATING POLYPEPTIDES AND METHODS OF MAKING AND USING SAME - The present invention relates to compositions comprising glucose regulating peptides linked to extended recombinant polypeptide (XTEN), isolated nucleic acids encoding the compositions and vectors and host cells containing the same, and methods of making and using such compositions in treatment of glucose regulating peptide-related diseases, disorders, and conditions. | 12-23-2010 |
20110009315 | LONG-ACTING TRANSIENT POLYMER CONJUGATES OF EXENDIN - Long-acting polymer exendin-4 or exendin agonist derivatives of the formula Pol-L-E are provided wherein Pol is a polymer, L is a releasing linker undergoing slow autohydrolysis and E is an exendin or exendin agonist. These exendin or exendin agonists are slowly released from Pol-L upon administration to a living organism. The derivatives are useful e.g. for the treatment of diabetes mellitus. | 01-13-2011 |
20110034380 | COMBINATION OF A SELECTIVE PPAR-GAMMA MODULATOR AND AN INCRETIN FOR THE TREATMENT OF DIABETES AND OBESITY - The present invention relates to pharmaceutical compositions and methods for the treatment of diabetes, obesity or disorders related to diabetes or obesity. The compositions comprise a combination of a selective PPARγ modulator and an incretin. The methods include the administration of the combination of a selective PPARγ modulator and an incretin. | 02-10-2011 |
20110053838 | PROCESS FOR SOLUBILIZING GLUCAGON-LIKE PEPTIDE 1 COMPOUNDS - Disclosed is a method of preparing a GLP-1 compound that is soluble in aqueous solution at pH 7.4 from a GLP-1 compound that is substantially insoluble in aqueous solution at pH 7.4. The insoluble GLP-1 compound is dissolved in aqueous base or in aqueous acid to form a GLP-1 solution. The GLP-1 solution is then neutralized to a pH at which substantially no amino acid racemization of the GLP-1 compounds occurs, after which the soluble GLP-1 compound is isolated from the neutralized solution. | 03-03-2011 |
20110053839 | GLP-1 Derivatives II - The present invention relates to a derivative of GLP-1(7-C), wherein C is 35 or 36 which derivative has just one lipophilic substituent which is attached to the C-terminal amino acid residue. | 03-03-2011 |
20110082079 | GLUCAGON-LIKE PEPTIDE-1 DERIVATIVES AND THEIR PHARMACEUTICAL USE - The invention relates to protracted Glucagon-Like Peptide-1 (GLP-1) derivatives and therapeutic uses thereof. The GLP-1 derivative of the invention comprises a modified GLP-1(7-37) sequence having a total of 2-12 amino acid modifications, including Glu22 and Arg26, and being derivatised with an albumin binding residue or pegylated in position 18, 20, 23, 30, 31, 34, 36, 37, or 39. These compounds are useful in the treatment or prevention of diabetes type 2 and related diseases. The compounds are potent, stable, have long half-lives, a high affinity of binding to albumin, and/or a high affinity of binding to the extracellular domain of the GLP-1 receptor (GLP-1R), all of which is of potential relevance for the overall aim of achieving long-acting, stable and active GLP-1 derivatives with a potential for once weekly administration. | 04-07-2011 |
20110136737 | DPP-IV Resistant GIP Hybrid Polypeptides with Selectable Properties - 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. | 06-09-2011 |
20110152186 | GLUCAGON-LIKE-PEPTIDE-2 (GLP-2) ANALOGUES - GLP-2 analogues are disclosed which comprise one of more substitutions as compared to [hGly2]GLP-2 and which improved biological activity in vivo and/or improved chemical stability, e.g., as assessed in in vitro stability assays. More particularly, preferred GLP-2 analogues disclosed herein comprise substitutions at one or more of positions 8, 16, 24 and/or 28 of the wild-type GLP-2 sequence, optionally in combination with further substitutions at position 2 (as mentioned in the introduction) and one or more of positions 3, 5, 7, 10 and 11, and/or a deletion of one or more of amino acids 31 to 33 and/or the addition of a N-terminal or C-terminal stabilizing peptide sequence. The analogues are particularly useful for the prophylaxis or treatment of stomach and bowel-related disorders and for ameliorating side effects of chemotherapy. Also disclosed are methods and kits for selecting a patient from populations suited for treatment with GLP-2 analogues. | 06-23-2011 |
20110172149 | Method of Regulating Glucose Metabolism, and Reagents Related Thereto - The present invention provides methods and compositions for modification and regulation of glucose and lipid metabolism, generally to reduce insulin resistance, hyperglycemia, hyperinsulinemia, obesity, hyperlipidemia, hyperlipoprotein-emia (such as chylomicrons, VLDL and LDL), and to regulate body fat and more generally lipid stores, and, more generally, for the improvement of metabolism disorders, especially those associated with diabetes, obesity and/or atherosclerosis. | 07-14-2011 |
20110195897 | GLYCOSYLATED GLP-1 PEPTIDE - Oligosaccharide chain added GLP-1 peptides are more stable in blood and more active in controlling blood-sugar levels than GLP-1 peptides without added oligosaccharides. Oligosaccharide chain added GLP-1 peptides having GLP-1 activity include at least one or at least two amino acids each substituted with an oligosaccharide chain added amino acid in GLP-1; a peptide having the amino acid sequence of GLP-1 with deletion, substitution or addition of one or several amino acids; or a GLP-1 analog. Oligosaccharide chain added GLP-1 peptides with at least one amino acid substituted with an oligosaccharide chain added amino acid include an oligosaccharide chain with oligo hyaluronic acid. Oligosaccharide chain added amino acids include oligosaccharide chains attached to amino acids via linkers. | 08-11-2011 |
20110212892 | AGENT FOR TREATMENT OF DIABETES - The present invention provides a hypoglycemic agent useful for treating diabetes or other similar diseases which has no adverse effects. Furthermore, the present invention provides a hypoglycemic agent comprising a combination of an antidiabetic drug and 2-methyl-2-[(4-{(1E)-3-[2-(4-methylbenzoyl)-1H-pyrrol-1-yl]prop-1-en-1-yl}benzyl)oxy]propanoic acid or a pharmaceutically acceptable salt thereof. | 09-01-2011 |
20110245166 | SUGAR CHAIN ADDED GLP-1 PEPTIDE - The present invention relates to an oligosaccharide chain added GLP-1 peptide that has higher stability in blood than that of GLP-1 and, preferably, exhibits higher activity of controlling blood-sugar levels than that of GLP-1. The present invention relates to an oligosaccharide chain added GLP-1 peptide having GLP-1 activity, wherein at least one amino acid is substituted with an oligosaccharide chain added amino acid, in: (a) GLP-1; (b) a peptide having the amino acid sequence of GLP-1 with deletion, substitution or addition of one or several amino acids; or (c) a GLP-1 analog. | 10-06-2011 |
20110257092 | GLUCAGON/GLP-1 RECEPTOR CO-AGONISTS - Modified glucagon peptides are disclosed having enhanced potency at the glucagon receptor relative to native glucagon. Further modification of the glucagon peptides by forming intramolecular bridges or the substitution of the terminal carboxylic acid with an amide group produces peptides exhibiting glucagon/GLP-1 receptor co-agonist activity. The solubility and stability of these high potency glucagon analogs can be further improved by modification of the polypeptides by pegylation, acylation, alkylation, substitution of carboxy terminal amino acids, C-terminal truncation, or the addition of a carboxy terminal peptide selected from the group consisting of SEQ ID NO: 26 (GPSSGAPPPS), SEQ ID NO: 27 (KRNRNNIA) and SEQ ID NO: 28 (KRNR). | 10-20-2011 |
20110269680 | GLP-1 ANALOGS AND USES THEREOF - The present invention relates to a peptide selected from a group comprising GLP-1 analogs, its truncated forms, or pharmaceutically acceptable salts and derivatives thereof. The present invention further relates to a peptide selected from a group comprising GLP-1 analogs, its truncated forms, or pharmaceutically acceptable salts and derivatives thereof, wherein one or more aminoacids are substituted with a non-coded aminoacid. | 11-03-2011 |
20110281797 | SITE-SPECIFIC MONOCONJUGATED INSULINOTROPIC GLP-1 PEPTIDES - The present invention is related to glucagon-like peptide-1 (GLP-1) and analogues insulinotropic peptides, monoconjugated to biocompatible polymeric molecules by enzymatic direct and site-specific transglutamination reaction as well as their pharmaceutical formulations and delivery systems for therapeutical application in dismetabolic pathologies such as type 2 diabetes. | 11-17-2011 |
20110281798 | Methods for Lowering Plasma Glucagon with Exendins and Exendin Agonist Analogs - Novel formulations containing exendins, exendin agonists and/or exendin analogs are provided. | 11-17-2011 |
20110301084 | Protracted Exendin-4 Compounds - Novel protracted exendin-4 compounds and therapeutic uses thereof. | 12-08-2011 |
20120004168 | EXENDINS AND EXENDIN AGONIST ANALOGS TO REGULATE GASTROINTESTINAL MOTILITY - Methods for reducing gastric motility and delaying gastric emptying for therapeutic and diagnostic purposes are disclosed which comprise administration of an effective amount of an exendin or an exendin agonist. Methods for treating conditions associated with elevated, inappropriate, or undesired post-prandial blood glucose levels are disclosed which comprise administration of an effective amount of an exendin or an exendin agonist alone or in conjunction with other anti-gastric emptying agents. | 01-05-2012 |
20120021980 | COMPOSITIONS FOR DRUG ADMINISTRATION - The present invention provides compositions and methods and for increasing the bioavailability of therapeutic agents in a subject. The compositions include at least one alkyl glycoside and at least one therapeutic agent, wherein the alkylglycoside has an alkyl chain length from about 10 to about 16 carbon atoms. In various aspects, the invention provides compositions and methods for oral delivery of glucagon-like peptide-1 analogs, such as exenatide, albiglutide, taspoglutide, liraglutide and lixisenatide. | 01-26-2012 |
20120040899 | Method for Treating Hyperglycemia with GLP-1 - A method for treating hyperglycemia and/or diabetes in a subject is provided. In particular, the method is directed for the treatment of patients with type 2 diabetes mellitus who have a fasting blood glucose concentration greater than about 8 mM, wherein the patient is administered a formulation comprising a GLP-1 molecule and a diketopiperazine by pulmonary inhalation with a dry powder inhalation system. | 02-16-2012 |
20120094905 | Method for Treating Hyperglycemia with GLP-1 - A method for treating hyperglycemia and/or diabetes in a subject is provided. In particular, the method is directed for the treatment of patients with type 2 diabetes mellitus who have a fasting blood glucose concentration greater than about 8 mM, wherein the patient is administered a formulation comprising a GLP-1 molecule and a diketopiperazine by pulmonary inhalation with a dry powder inhalation system. | 04-19-2012 |
20120101034 | PROCESS FOR SOLUBILIZING GLUCAGON-LIKE PEPTIDE 1 COMPOUNDS - Disclosed is a method of preparing a GLP-1 compound that is soluble in aqueous solution at pH 7.4 from a GLP-1 compound that is substantially insoluble in aqueous solution at pH 7.4. The insoluble GLP-1 compound is dissolved in aqueous base or in aqueous acid to form a GLP-1 solution. The GLP-1 solution is then neutralized to a pH at which substantially no amino acid racemization of the GLP-1 compounds occurs, after which the soluble GLP-1 compound is isolated from the neutralized solution. | 04-26-2012 |
20120108508 | METHOD FOR PROMOTING SECRETION OF GLUCAGON-LIKE PEPTIDE-1 BY ADMINISTERING K-CASEIN - The invention relates to a GLP-1 secretagogue and an inhibitor of postprandial rise in blood glucose, containing κ-casein as an active ingredient, and a food or drink for promoting GLP-1 secretion and an inhibitory food or drink of postprandial rise in blood glucose, containing a milk-derived casein protein wherein κ-casein accounts for 60% by mass or more of the milk-derived casein. | 05-03-2012 |
20120135922 | MODIFIED EXENDINS AND EXENDIN AGONISTS - Novel modified exendins and exendin agonists having an exendin or exendin agonist linked to one or more polyethylene glycol polymers, for example, and related formulations and dosages and methods of administration thereof are provided. These modified exendins and exendin agonists, compositions and methods are useful in treating diabetes and conditions that would be benefited by lowering plasma glucose or delaying and/or slowing gastric emptying or inhibiting food intake. | 05-31-2012 |
20120149639 | USE OF A DPP-IV INHIBITOR TO REDUCE HYPOGLYCEMIC EVENTS - The invention relates to a method to reduce the hypoglycemic events, especially severe hypoglycemic events resulting from insulin treatment, wherein the patient is treated with a Dipeptidyl peptidase IV inhibitor (DPP-IV inhibitor) or a pharmaceutically acceptable salt thereof. | 06-14-2012 |
20120157379 | Gastric Inhibitory Peptide Variants and Their Uses - Novel gastric inhibitory peptide (GIP) polypeptide compositions are provided. Human GIP alleles encode an extended peptide, referred to herein as GIP55S or GIP55G, which is resistant to serum degradation, relative to the known mature GIP peptide. GIP55S or GIP55G peptides find use where it is desirable to modulate insulin secretion. | 06-21-2012 |
20120172298 | GLP-1 AND FGF21 COMBINATIONS FOR TREATMENT OF DIABETES TYPE 2 - The invention relates to the use of a Fibroblast Growth Factor 21 (FGF21) compound and a Glucagon-Like Peptide 1 (GLP-1) compound in combination for the preparation of a medicament for the treatment of diabetes, more in particular type 2 diabetes, as well as pharmaceutical compositions comprising certain FGF21 and GLP-1 compounds in combination, together with a pharmaceutically acceptable carrier. The combination has a significant effect on parameters of relevance for diabetes type 2, viz. on the viability of beta cells ex vivo in the presence of free fatty acids, on caspase activity of beta cells ex vivo (a measure of cell apoptosis), and a blood glucose lowering effect on db/db mice in vivo. | 07-05-2012 |
20120196802 | MODIFIED EXENDINS AND USES THEREOF - The present invention discloses a modified exendin or pharmaceutically acceptable salts thereof, wherein the modified exendin comprises an amino acid sequence having at least 90% sequence identity to SEQ ID No. 17 and the amino acid sequence has a higher stability than the non-modified exendin of SEQ ID No. 4. These compounds are useful in treating type 2 diabetes as GLP-1 receptor agonists. | 08-02-2012 |
20120232003 | COMPOSITIONS AND METHODS FOR DIABETES TREATMENT - The present invention relates to methods and compositions for the treatment or prevention of type 2 diabetes by administering an effective amount of a melatonin receptor agonist to a human subject in need of such treatment or prevention. | 09-13-2012 |
20120264684 | Glycosylated Form of Antigenic GLP-1 Analogue - Disclosed is a glucagon-like peptide-1 (GLP-1) analogue which is obtained by ameliorating a highly antigenic GLP-1 analogue so that the GLP-1 analogue has reduced antigenicity without being lowered in the blood glucose suppressing activity. Specifically disclosed is a glycosylated form of an antigenic GLP-1 analogue, which has GLP-1 activity and is obtained by substituting at least one amino acid of an antigenic GLP-1 analogue with a glycosylated amino acid. | 10-18-2012 |
20120264685 | SHORT CHAIN PEPTIDOMIMETICS BASED ORALLY ACTIVE GLP 1 AGONIST AND GLUCAGON RECEPTOR ANTAGONIST - The present invention provides novel short chain peptidomimetics, which act as GLP-1 receptors agonist and glucagon receptor antagonist. These dual acting peptidomimetics exhibit increased stability to proteolytic cleavage, especially against DPP-IV (Dipeptidyl peptidase-IV) enzyme, GIT enzymes such as pepsin and acidic stomach pH and also against liver microsomes (in vitro). Due to increased metabolic stability, other than parenteral route of administration, these short chain peptidomimetics can be delivered by oral routes of administration, for the treatment or prevention of diabetes and related metabolic disorders, such as obesity, hyperlipidemia and eating disorders. | 10-18-2012 |
20120277151 | GLP-1 PHARMACEUTICAL COMPOSITIONS - The present invention is directed to peptide analogues of glucagon-like peptide-1, the pharmaceutically-acceptable salts thereof, to methods of using such analogues to treat mammals and to pharmaceutical compositions useful therefore comprising said analogues. | 11-01-2012 |
20120295847 | Acylated GLP-1 Compounds - Protracted GLP-1 compounds and therapeutic uses thereof. | 11-22-2012 |
20120322728 | PPAR-SPARING THIAZOLIDINEDIONES AND COMBINATIONS FOR THE TREATMENT OF DIABETES MELLITUS AND OTHER METABOLIC DISEASES - The present invention relates to thiazolidinedione analogues and pharmaceutical compositions that are useful for treating and/or preventing diabetes mellitis, optionally in combination with a second treatment. Furthermore, the present invention also provides methods of inducing remission of the symptoms of diabetes mellitis in a patient comprising administering a thiazolidinedione analogue and a GLP-1 agonist. | 12-20-2012 |
20120329711 | GLP-1 RECEPTOR AGONIST COMPOUNDS WITH A MODIFIED N-TERMINUS - The invention relates to GLP-1 receptor agonist compounds with a modified N-terminus. The compounds are of the formula Chem. 1: Y—Z—P, wherein P represents a fragment of a GLP-1 receptor agonist peptide lacking the two N-terminal amino acid residues; and Y—Z represents novel His-Ala mimetics. Examples of GLP-1 receptor agonist compounds are derived from human GLP-1 (7-37), exendin-4(1-39), or GLP-1 A (1-37). The invention also relates to derivatives of these compounds, in particular compounds with one or more albumin binding side chains capable of protracting the duration of action in vivo of these compounds. The peptides and derivatives of the invention have a good potency, a protracted pharmacokinetic profile, are stable against degradation by gastro intestinal enzymes, and/or have a high oral bioavailability. These properties are of importance in the development of GLP-1 receptor agonist compounds for subcutaneous, intravenous, and/or in particular oral administration. The invention also relates to intermediate products for use in the preparation of the GLP-1 receptor agonist compounds of the invention. | 12-27-2012 |
20130005652 | METHODS FOR ADMINISTERING LONG-LASTING HYPOGLYCEMIC AGENTS - The present invention relates to methods and pharmaceutical compositions relating to administering hypoglycemic agents and/or GLP-1 agonists wherein the mean maximum plasma concentration (Cmax) and/or Area Under the Curve (AUC) values of the hypoglycemic agent are increased and/or sustained. | 01-03-2013 |
20130040878 | PHARMACEUTICAL COMBINATION FOR USE IN THE TREATMENT OF DIABETES TYPE 2 PATIENTS - The present invention refers to a pharmaceutical combination for use in the treatment of diabetes type 2 patients. | 02-14-2013 |
20130059778 | Identification of a Genetic Risk Factor for Diabetes - Loss of function ankyrin-B variants have impaired function in pancreatic islets and are associated with type 2 diabetes. This finding provides the basis for methods of identifying at-risk individuals for type 2 diabetes and for personalized therapeutic strategies. | 03-07-2013 |
20130065828 | PHARMACEUTICAL COMBINATION FOR USE IN GLYCEMIC CONTROL IN DIABETES TYPE 2 PATIENTS - The present invention refers to a pharmaceutical combination for use in glycemic control in diabetes type 2 patients. | 03-14-2013 |
20130085102 | PREVENTION OF HYPOGLYCEMIA IN DIABETES MELLITUS TYPE 2 PATIENTS - A method for the prevention of hypoglycaemia in diabetes mellitus type 2 comprising administering
| 04-04-2013 |
20130130977 | POLYMER-BASED SUSTAINED RELEASE DEVICE - This invention relates to compositions for the sustained release of biologically active polypeptides, and methods of forming and using said compositions, for the sustained release of biologically active polypeptides. The sustained release compositions of this invention comprise a biocompatible polymer having dispersed therein, a biologically active polypeptide and a sugar. | 05-23-2013 |
20130157942 | STABILIZED INSULINOTROPIC PEPTIDES AND METHODS OF USE - The present invention provides stably cross-linked insulionotropic polypeptides having superior and un-expected benefits in the treatment of conditions involving abnormal glucose homeostasis, e.g., type 2 diabetes and conditions relating to type 2 diabetes. Such benefits include, but are not limited to, extended polypeptide half-life, enhanced alpha-helicity, improved thermal stability and protease resistance, increased functional activity and pharmacologic properties, improved bioavailability when administered by any route, and improved bioavailability and gastrointestinal absorption when delivered orally, as compared to the corresponding unmodified polypeptides. The invention also provides compositions for administering the polypeptides of the invention, as well as methods for pre-paring and evaluating the polypeptides of the invention. | 06-20-2013 |
20130165373 | THERAPEUTIC AGENT PREPARATIONS FOR DELIVERY INTO A LUMEN OF THE INTESTINAL TRACT USING A SWALLOWABLE DRUG DELIVERY DEVICE - Embodiments of the invention provide swallowable devices, preparations and methods for delivering drugs and other therapeutic agents within the GI tract. Many embodiments provide a swallowable device for delivering the agents. Particular embodiments provide a swallowable device such as a capsule for delivering drugs into the intestinal wall or other GI lumen. Embodiments also provide various drug preparations that are configured to be contained within the capsule, advanced from the capsule into the intestinal wall and degrade to release the drug into the bloodstream to produce a therapeutic effect. The preparation can be operably coupled to delivery means having a first configuration where the preparation is contained in the capsule and a second configuration where the preparation is advanced out of the capsule into the intestinal wall. Embodiments of the invention are particularly useful for the delivery of drugs which are poorly absorbed, tolerated and/or degraded within the GI tract. | 06-27-2013 |
20130178416 | FUSION PEPTIDE THERAPEUTIC COMPOSITIONS - Therapeutic compositions containing fusion proteins (FPs) including elastin-like peptides (ELPs) and peptide active therapeutic agents, and methods of making and using such compositions and fusion proteins. Therapeutic compositions of such type enable improved efficacy of the peptide active therapeutic agent to be achieved, in relation to the peptide active therapeutic agent alone. Enhanced efficacy of the peptide active therapeutic agent in the therapeutic composition may include improved solubility, bioavailability, bio-unavailability, half-life, etc., as compared to corresponding compositions containing the same peptide active therapeutic agent without associated ELPs. | 07-11-2013 |
20130203666 | PHARMACEUTICAL COMBINATION FOR USE IN GLYCEMIC CONTROL IN DIABETES TYPE 2 PATIENTS - The present invention refers to a pharmaceutical combination for use in glycemic control in diabetes type 2 patients. | 08-08-2013 |
20130210722 | METHODS FOR USING PEPTIDE AGONISTS HAVING GLP-1 ACTIVITY - Novel peptide agonists of GLP-1 activity useful for lowering blood glucose levels. The novel peptides comprise variants of the GLP-1 or the exendin-4 polypeptide sequence and are pharmacologically active and stable. These peptides are useful in the treatment of diseases that benefit from regulation of excess levels of blood glucose and/or regulation of gastric emptying, such as diabetes and eating disorders. | 08-15-2013 |
20130217622 | EXENDIN-4 ANALOGUE PEGYLATED WITH POLYETHYLENE GLYCOL OR DERIVATIVE THEREOF, PREPARATION METHOD THEREOF, AND PHARMACEUTICAL COMPOSTION FOR PREVENTING OR TREATING DIABETES, CONTAINING SAME AS ACTIVE INGREDIENT - 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. | 08-22-2013 |
20130281368 | Glucagon-Like Peptide-1 Glycopeptides - A stretching and exercise device has a first strap member having a pair of end portions, a second strap member having a pair of end portions, and a pair of resistance members connected between respective end portions of the first and second strap members. A third strap member has a pair of end portions attached to respective first and second surface portions of the second strap member. A fourth strap member is attached to a third surface portion of the second strap member different from the first and second surface portions thereof. | 10-24-2013 |
20130288960 | Double-Acylated GLP-1 Derivatives - The invention relates to a derivative of a GLP-1 analogue, which analogue comprises a first K residue at a position corresponding to position 18 of GLP-1 (7-37) (SEQ ID NO: 1), a second K residue at another position, and a maximum of twelve amino acid changes as compared to GLP-1 (7-37); which derivative comprises two protracting moieties attached to said first and second K residue, respectively, via a linker, wherein the protracting moiety is selected from Chem. 1, Chem. 2, and Chem. 3: Chem.: HOOC—(CH | 10-31-2013 |
20130310314 | SOLID PHASE SYNTHESIS OF H(GLY2)GLP-2 - The present invention relates to a method of preparing a peptide comprising the amino acid sequence His-Gly-Asp-Gly-Ser-Phe-Ser-Asp-Glu-Met-Asn-Thr-Ile-Leu-Asp-Asn-Leu-Ala-Ala-Arg-Asp-Phe-Ile-Asn-Trp-Leu-Ile-Gln-Thr-Lys-Ile-Thr-Asp (SEQ ID NO:1). In particular, the method comprises the steps of providing a first peptide fragment having a first protection group, which peptide fragment is conjugated to a support; providing a second peptide fragment having a second protection group; removing the first protection group from the first peptide fragment; and coupling the second peptide fragment to the N-terminally deprotected, support-conjugated first peptide fragment. The present invention further relates to a method of preparing a pharmaceutical composition containing said peptide. | 11-21-2013 |
20130331323 | GLP-1 POTENTIATORS FROM HEDYCHIUM CORONARIUM AND THEIR APPLICATIONS - A compound for controlling blood glucose level has a structure shown in Formula I: | 12-12-2013 |
20130338068 | DOUBLE-ACYLATED GLP-1 DERIVATIVES WITH A LINKER - The invention relates to a derivative of a GLP-1 analogue, which analogue comprises a first K residue at a position corresponding to position 18 of GLP-1(7-37) (SEQ ID NO: 1), a second K residue at another position, and a maximum of twelve amino acid changes as compared to GLP-1(7-37); which derivative comprises two protracting moieties attached to said first and second K residue, respectively, via a linker, wherein the protracting moiety is selected from | 12-19-2013 |
20130345129 | SUGAR CHAIN ADDED GLP-1 PEPTIDE - The present invention relates to an oligosaccharide chain added GLP-1 peptide that has higher stability in blood than that of GLP-1 and, preferably, exhibits higher activity of controlling blood-sugar levels than that of GLP-1. The present invention relates to an oligosaccharide chain added GLP-1 peptide having GLP-1 activity, wherein at least one amino acid is substituted with an oligosaccharide chain added amino acid, in: (a) GLP-1; (b) a peptide having the amino acid sequence of GLP-1 with deletion, substitution or addition of one or several amino acids; or (c) a GLP-1 analog. | 12-26-2013 |
20140024585 | Composition for the therapy of diabetes mellitus and adiposity - A composition containing at least two of the following active substances A, B, C, wherein:
| 01-23-2014 |
20140024586 | USE OF AN FGF-21 COMPOUND AND A GLP-1 COMPOUND FOR THE TREATMENT OF OBESITY - The present invention provides methods of lowering body weight by administering an FGF-21 compound in combination with a GLP- | 01-23-2014 |
20140031282 | FORMULATION FOR TREATMENT OF HYPERINSULINEMIC HYPOGLYCEMIA FOLLOWING GASTRIC BYPASS SURGERY - An effective combination of 6.25-100 mg of acarbose with a GLP-1 mimetic, such as 5-10 mg exenatide or 0.3-3.0 mg liraglutide. | 01-30-2014 |
20140038891 | MODIFIED EXENDINS AND EXENDIN AGONISTS - Novel modified exendins and exendin agonists having an exendin or exendin agonist linked to one or more polyethylene glycol polymers, for example, and related formulations and dosages and methods of administration thereof are provided. These modified exendins and exendin agonists, compositions and methods are useful in treating diabetes and conditions that would be benefited by lowering plasma glucose or delaying and/or slowing gastric emptying or inhibiting food intake. | 02-06-2014 |
20140066370 | Polypeptide Conjugate - The disclosure provides Polypeptide Conjugates with multiple improved pharmacological and pharmacokinetic properties and their use in treating various diseases and conditions, such as diabetes and/or obesity. | 03-06-2014 |
20140066371 | METHODS FOR ADMINISTERING LONG-LASTING HYPOGLYCEMIC AGENTS - The present invention relates to methods and pharmaceutical compositions relating to administering hypoglycemic agents and/or GLP-1 agonists wherein the mean maximum plasma concentration (Cmax) and/or Area Under the Curve (AUC) values of the hypoglycemic agent are increased and/or sustained. | 03-06-2014 |
20140066372 | Glucokinase Activator Compositions for the Treatment of Diabetes - The present invention relates to pharmaceutical compositions comprising {2-[3-cyclohexyl-3-(trans-4-propoxy-cyclohexyl)-ureido]-thiazol-5-ylsulfanyl}-acetic acid (FRI-1) in combination with an anti-diabetic drug selected from the group consisting of metformin, sitagliptin or exenatide. The present invention also relates to the use of the pharmaceutical compositions in restoring insulin sensitivity and treating type II diabetes, including reducing body weight in subjects undergoing type II diabetes treatment. | 03-06-2014 |
20140107028 | METHODS AND COMPOSITIONS FOR PREDICTING RESPONSE TO GLP-1 ANALOGS - Methods and compositions are provided for evaluating a diabetic patient for treatment with an incretin-based therapy. In certain embodiments, evaluation is ongoing and the patient is evaluated at multiple times. In additional embodiments, a diabetic patient is treated with an incretin-based therapy after the patient has been evaluated for expression levels of GLP-1R in a biological sample. In some aspects, the biological sample is specifically a blood sample that has been enriched for peripheral blood monocytes. | 04-17-2014 |
20140142037 | SITE-DIRECTED MONO-SUBSTITUTED PEGYLATED EXENDIN ANALOG AND PREPARATION METHOD THEREFOR - The invention discloses site-specific mono-PEGylated Exendin analogs in which any amino groups can be mono-PEGylated as well as their preparation method and use. The method of the present invention adopts a more stable protective group Dde (N-α-1-(4,4-dimethyl-2,6-dioxo-cyclohexylene)) to avoid multi-PEGylated side reactions rendered by unstable protecting groups, achieving mono-PEGylated Exendin analogs at a high recovery with a low reaction molar ratio. | 05-22-2014 |
20140148384 | USE OF AVE0010 FOR THE MANUFACTURE OF A MEDICAMENT FOR THE TREATMENT OF DIABETES MELLITUS TYPE 2 - The present invention refers to the use of Lixisenatide or/and a pharmaceutically acceptable salt thereof, for the manufacture of a medicament for the treatment of diabetes mellitus type 2, for inducing weight loss in diabetes type 2 patients or/and for preventing weight gain in diabetes type 2 patients. | 05-29-2014 |
20140187483 | GLP-1 AND METHODS FOR TREATING DIABETES - The present invention relates to use of GLP-1 or a related molecule having GLP-effect for the manufacture of a medicament for preventing or treating diabetes in a mammal. The amount and timing of administration of said medicament are subsequently reduced to produce a “drug holiday”. Practice of the invention achieves effective therapy without continuous drug exposure and without continuous presence of therapeutic levels of the drug. The invention also discloses a method of treating diabetes and related disorders in a mammal by administering glucagon like peptide (GLP-1) or a related molecule having GLP-1 like effect and thereby providing a therapeutically effective amount of endogenous insulin. | 07-03-2014 |
20140206613 | METHODS TO RESTORE GLYCEMIC CONTROL - Provided herein are methods and compositions to achieve a sustained delay in the progression of, or an amelioration of diabetes in a subject, or a delay in diabetes onset in a subject at risk for diabetes, comprising an abbreviated course of administration of a pharmaceutical composition comprising an exendin or an exendin agonist analog in an amount effective to induce β cell regeneration. | 07-24-2014 |
20140221288 | METHODS FOR RAPIDLY TREATING SEVERE HYPOGLYCEMIA - Disclosed is a method for treating or preventing hypoglycemia in a patient comprising administering an effective amount of a composition comprising a glucagon peptide which has been dried in a non-volatile buffer, and wherein the glucagon peptide has a pH memory that is about equal to the pH of the glucagon peptide in the non-volatile buffer, and an aprotic polar solvent, wherein the moisture content of the formulation is less than 5%, and wherein the dried glucagon peptide maintains the pH memory that is about equal to the pH of the glucagon peptide in the non-volatile buffer when the dried glucagon peptide is reconstituted in the aprotic polar solvent, wherein the patient has been diagnosed as having a blood glucose level between 0 mg/dL and less than 50 mg/dL or has an indication of impending hypoglycemia based on a blood glucose monitoring device before administration of the composition, and wherein the patient has a blood glucose level greater than 50 mg/dL to 180 mg/dL within 1 to 20 minutes after administration of the composition. | 08-07-2014 |
20140256626 | PEG CONJUGATES OF EXENATIDE - Slow release forms of exenatide wherein exenatide is releasably linked to polyethylene glycol carriers are disclosed. | 09-11-2014 |
20140287993 | AMINOTETRAHYDROPYRANS AS DIPEPTIDYL PEPTIDASE-IV INHIBITORS FOR THE TREATMENT OR PREVENTION OF DIABETES - The present invention is directed to novel substituted aminotetrahydropyrans of structural formula I which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved. | 09-25-2014 |
20140378374 | METHODS OF TREATMENT - The present invention provides methods of treating type 2 diabetes mellitus (T2DM) in human in need thereof comprising administering a pharmaceutical composition comprising a GLP-1 agonist to said human wherein said human has renal impairment. The present invention further provides methods of treating type 2 diabetes and/or providing glycemic control in a human wherein said human has renal impairment comprising administering to said human a subcutaneous injection of a pharmaceutical composition comprising albiglutide. | 12-25-2014 |
20140378375 | ALPHA/BETA-POLYPEPTIDE ANALOGS OF GLUCAGON-LIKE PEPTIDE 1 - Described herein are peptide analogs of glucagon-like peptide 1 (GLP-1) that retain agonist activity, but are more resistant to proteolytic degradation than native GLP-1. In the analogs, at least one α-amino acid found in the native GLP-1 is replaced with a β-amino acid residue, which may or may not be cyclically constrained. Pharmaceutical compositions containing the analogs are described, as are methods to treat diabetes, and methods to make proteolytically resistant GLP-1 analogs. | 12-25-2014 |
20150080298 | METHOD FOR TREATING HYPERGLYCEMIA - A method for treating hyperglycemia and/or diabetes in a subject is provided. In particular, the method is directed for the treatment of patients with type 2 diabetes mellitus who have a fasting blood glucose concentration greater than about 8 mM, wherein the patient is administered a formulation comprising a GLP-1 molecule and a diketopiperazine by pulmonary inhalation with a dry powder inhalation system. | 03-19-2015 |
20150105318 | ANTIDIABETIC MEDICATIONS - Methods of using antidiabetic medications which are suitable in the treatment or prevention of one or more conditions selected from type 1 diabetes mellitus, type 2 diabetes mellitus, impaired glucose tolerance, and hyperglycemia, among others. | 04-16-2015 |
20150133374 | Double-Acylated GLP-1 Derivatives - The invention relates to a derivative of a GLP-1 analogue, which analogue comprises a first K residue and a second K residue, at positions corresponding to position 26, and 37, respectively, of GLP-1(7-37) (SEQ ID NO: 1), and a maximum of eight amino acid changes as compared to GLP-1(7-37); which derivative comprises two protracting moieties attached to said first and second K residue, respectively, via a linker, wherein the protracting moiety is selected from Chem. 1: HOOC—(CH | 05-14-2015 |
20150299281 | GIP-GLP-1 DUAL AGONIST COMPOUNDS AND METHODS - The present invention relates to truncated GIP analogues which comprise one or more substitutions as compared to wild-type GIP and which may have the property of an altered, preferably increased GLP-1 activity, e.g. as assessed in in vitro efficacy assays. The invention provides GIP-GLP-1 dual agonist compounds and associated methods. | 10-22-2015 |
20160083447 | DOUBLE-ACYLATED GLP-1 DERIVATIVES - The invention relates to a derivative of a GLP-1 analogue, which analogue comprises a first K residue at a position corresponding to position 27 of GLP-1(7-37) (SEQ ID NO: 1); a second K residue at a position corresponding to position T of GLP-1(7-37), where T is an integer in the range of 7-37 except 18 and 27; and a maximum of ten amino acid changes as compared to GLP-1(7-37); wherein the first K residue is designated K | 03-24-2016 |
20160120951 | ACYLATED GLUCAGON ANALOGUES - The invention provides materials and methods for promoting weight loss or preventing weight gain, and in the treatment of diabetes and associated metabolic disorders. In particular, the invention provides novel acylated glucagon analogue peptides effective in such methods. The peptides may mediate their effect by having increased selectivity for the GLP-1 receptor as compared to human glucagon. | 05-05-2016 |
20160143998 | GLP-1 Derivatives and Uses Thereof - The invention relates to a derivative of a GLP-1 analogue, optionally C-terminally extended, which derivative comprises a first and a second protracting moiety in the form of a C20 or C22 diacid radical, a bis-amino branched linker, and a first and a second further linker each comprising an OEG-like linker element; wherein these elements are interconnected via amide bonds and attached to a Lys residue of the GLP-1 analogue. The invention also relates to intermediate products in the form of novel GLP-1 analogues incorporated in the derivatives of the invention, as well pharmaceutical compositions and medical uses of the derivatives. The derivatives have very long half-lives while maintaining a satisfactory potency, which makes them potentially suitable for once-monthly administration. | 05-26-2016 |
20160159876 | STABILIZED INSULINOTROPIC PEPTIDES AND METHODS OF USE - The present invention provides stably crosslinked insulinotropic polypeptides having superior and unexpected benefits in the treatment of conditions involving abnormal glucose homeostasis, e.g., type 2 diabetes and conditions relating to type 2 diabetes. Such benefits include, but are not limited to, extended polypeptide half-life, enhanced alpha-helicity, improved thermal stability and protease resistance, increased functional activity and pharmacologic properties, improved bioavailability when administered by any route, and improved bioavailability and gastrointestinal absorption when delivered orally, as compared to the corresponding unmodified polypeptides. The invention also provides compositions for administering the polypeptides of the invention, as well as methods for preparing and evaluating the polypeptides of the invention. | 06-09-2016 |
20160199438 | GIP AND GLP-1 CO-AGONIST COMPOUNDS | 07-14-2016 |
20190142904 | ACYLATED GLP-1/GLP-2 DUAL AGONISTS | 05-16-2019 |