Abstract: Methods are provided for treatment or prophylaxis of liver or kidney dysfunction in individuals experiencing one or more of intestinal failure, short bowel syndrome or parenteral nutrition by the administration of GLP-2 or GLP-2 analogs.

Abstract: A liquid composition in an osmotic drug delivery system and a dosage form in an osmotic drug delivery system is disclosed comprising an amphiphilic molecule, a non-aqueous liquid solvent, and a pharmaceutically active agent.

Abstract: The present invention provides polypeptides that include an O-linked glycoconjugate in which a species such as a water-soluble polymer, a therapeutic agent of a biomolecule is covalently linked through an intact O-linked glycosyl residue to the polypeptide. The polypeptides of the invention include wild-type peptides and mutant peptides that include an O-linked glycosylation site that is not present in the wild-type peptide. Also provided are methods of making the peptides of the invention and methods, pharmaceutical compositions containing the peptides and methods of treating, ameliorating or preventing diseased in mammals by administering an amount of a peptide of the invention sufficient to achieve the desired response.

Abstract: The invention provides a method of treating a subject having, or at risk of developing, a condition in which functioning of the small or large intestine is impaired, enhancing functioning or preventing damage to the small or large intestine in a subject, or ameliorating inflammation of the small or large intestine in a subject, comprising administering to the subject a GLP-1 receptor agonist. A GLP-1 receptor agonist may also be provided in a pharmaceutically acceptable form in an amount effective to treat or prevent conditions of the small or large intestine. Further, pharmaceutical compositions are provided for the treatment or prevention of conditions of the small or large intestine comprising a GLP-1 receptor agonist, together with a pharmaceutically acceptable carrier, excipient or vehicle.

Abstract: The invention relates to a GLP-1 analogue which comprises a histidine (H) residue at a position corresponding to position 31 of GLP-1 (7-37) (SEQ ID NO: 1), a glutamine (Q) residue at a position corresponding to position 34 of GLP-1 (7-37) (SEQ ID NO: 1), and a maximum of ten amino acid modifications as compared to GLP-1 (7-37) (SEQ ID NO: 1); wherein the H residue is designated H31, and the Q residue is designated Q34; or a pharmaceutically acceptable salt, amide, or ester thereof. The invention also relates to derivatives thereof, as well as the pharmaceutical use of these analogues and derivatives, for example in the treatment and/or prevention of all forms of diabetes and related diseases. The invention furthermore relates to corresponding novel side chain intermediates. The derivatives are suitable for oral administration.

Abstract: The present invention provides methods for treating, preventing and/or ameliorating at least one cardiovascular disorder in a human in need thereof comprising administering to said human a pharmaceutical composition comprising at least one polypeptide having at least one GLP-1 activity and/or at least one GLP-1 agonist.

Abstract: The present invention relates to glucagon peptide agonists which have improved solubility and stability, to the use of the peptides in therapy, to methods of treatment comprising administration of the peptides to patients in need thereof, and to the use of the peptides in the manufacture of medicaments. The glucagon peptides of the invention are of particular interest in relation to the treatment of hypoglycemia, diabetes and obesity, as well as a variety of diseases or conditions associated with hypoglycemia, diabetes and obesity.

Abstract: Provided is a glucagon-like peptide-1 (GLP-1) analogue shown as the following formula, wherein X is selected from glycine and glycinamide. The GLP-1 analogue has a non-proteogenic amino acid residue in position 8 relative to the sequence GLP-1, and is acylated with a moiety comprising two acidic groups to the lysine residue in position 26. The GLP-1 analogue is resistant to dipeptidyl peptidase IV so as to have an extended half-life in vivo. Also provided is a use of the GLP-1 analogue in conquering blood sugar.

Abstract: Novel polypeptide derivatives having protracted profile of action.

Abstract: Novel polypeptide derivatives having protracted profile of action.

Abstract: The present invention relates to novel peptide compounds which have a protracted profile of action and improved solubility and stability, to the use of the compounds in therapy, to methods of treatment comprising administration of the compounds to patients in need thereof, and to the use of the compounds in the manufacture of medicaments. The compounds of the invention are of particular interest in relation to the treatment of hyperglycemia, diabetes and obesity, as well as a variety of diseases or conditions associated with hyperglycemia, diabetes and obesity.

Abstract: The invention relates to a pharmaceutical composition according to the claim 1 comprising an SGLT2 inhibitor and a GLP-1 receptor agonist which is suitable in the treatment or prevention of diabetes mellitus, impaired glucose tolerance, hyperglycemia or other conditions. In addition the present invention relates to methods for preventing or treating of metabolic disorders and related conditions.

Abstract: The present invention provides an Oxyntomodulin peptide analogue useful in the treatment of diabetes and/or obesity.

Abstract: Methods for treating conditions or disorders which can be alleviated by reducing food intake are disclosed which comprise administration of an effective amount of an exendin or an exendin agonist, alone or in conjunction with other compounds or compositions that affect satiety. The methods are useful for treating conditions or disorders, including obesity, Type II diabetes, eating disorders, and insulin-resistance syndrome. The methods are also useful for lowering the plasma glucose level, lowering the plasma lipid level, reducing the cardiac risk, reducing the appetite, and reducing the weight of subjects. Pharmaceutical compositions for use in the methods of the invention are also disclosed.

Abstract: Methods for treating abnormal glycosylated hemoglobin (HbA1c) levels in a patient in need thereof, wherein the provided methods comprise administering to a patient in need a therapeutically effective amount of an Interleukin-1? modulator. Also, the invention provides compositions comprising at least one lipid modifying agent and an IL-1? modulator.

Abstract: The invention provides a powdered composition for nasal administration, comprising a physiologically active peptide and cellulose acetate as the base, and having excellent nasal absorption for physiologically active peptides.

Abstract: The present invention provides heterocyclic derivatives of formula (I) that modulate the activity of stearoyl-CoA desaturase. Methods of using such derivatives to modulate the activity of stearoyl-CoA desaturase and pharmaceutical compositions comprising such derivatives are also encompassed.

Abstract: The present invention relates to compounds of the general formula: wherein ring A, ring B, R1, R3, Z, L1, and L2 are selected independently of each other and are as defined herein, to compositions comprising the compounds, and to methods of using the compounds as glucagon receptor antagonists and for the treatment or prevention of type 2 diabetes and conditions related thereto.

Abstract: 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.

Abstract: The invention relates to glucagon-related peptides and their use for the prevention or treatment of disorders involving the large intestine. In particular, it has now been demonstrated that GLP-2 and peptidic agonists of GLP-2 can cause proliferation of the tissue of large intestine. Thus, the invention provides methods of proliferating the large intestine in a subject in need thereof. Further, the methods of the invention are useful to treat or prevent inflammatory conditions of the large intestine, including inflammatory bowel diseases.

Abstract: The present invention provides methods and materials by which glycosylation of glycoproteins can be regulated. Methods include the monitoring and regulation of parameters such that a glycoprotein having a desired product quality is obtained.

Abstract: Drug delivery systems have been developed based on the formation of diketopiperazine carboxylate salts and microparticles containing the same. The systems may further comprise a bioactive agent. Related methods for making and using the biologically active agent delivery compositions are also provided. In certain embodiments, the pharmaceutically acceptable salts described can be formed by removal of solvent by methods including distillation, evaporation, spray drying or lyophilization.

Abstract: Provided herein are peptides and variant peptides that exhibit enhanced activity at the GLP-1 receptor, as compared to native glucagon.

Abstract: 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.

Abstract: The invention relates to novel polypeptide analogues of GLP-1 and exendin-4. The polypeptide, in a preferred embodiment, is insulinotropic and long-acting. Preferably, the polypeptide's insulinotropic effect is comparable to or exceeds the effect of an equimolar amount of GLP-1 or exendin-4. The invention also relates to a method of treating a subject with diabetes, comprising administering to the subject the polypeptide of the invention in an amount that has an insulinotropic effect. The invention also relates to methods of using GLP-1, exendin-4, and polypeptide analogues thereof for neuroprotective and neurotrophic effects.

Abstract: Provided herein are peptides and variant peptides that exhibit enhanced activity at the GLP-1 receptor, as compared to native glucagon.

Abstract: 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.

Abstract: Hibernating myocardium is characterized by viable myocardium with impaired function due to localized reduced perfusion. Hibernating myocytes retain cellular integrity, but cannot sustain high-energy requirements of contraction. High plasma levels of catecholamines, such as norepinepherine, are believed to be predictive of mortality from hibernating myocardium. Likewise, high levels of catecholamines lead to cardiomyopathy in patients with diabetes. GLP-1 reduces plasma norepinepherine levels, and it thus is useful in a method of treating hibernating myocardium or diabetic cardiomyopathy.

Abstract: Nanoparticles having a core and a corona of ligands covalently linked to the core, wherein differing species of peptides are bound to the nanoparticles and incorporated into various dosage forms.

Abstract: Compositions and methods are provided for mucosal delivery of peptides. The compositions include a stably hydrated peptide active agent complexed with a crown compound and/or a counter ion solubilized in a non-aqueous hydrophobic vehicle at a pH different from the pI of the peptide active agent. The methods include administering to a subject an effective amount of a composition of the disclosure. Other aspects include methods for the manufacture of the compositions of the disclosure. Also provided are compositions and kits that find use in practicing embodiments of the disclosure. The methods and compositions find use in a variety of applications, including the treatment of a variety of different disease conditions.

Abstract: The present invention provides methods for modification and regulation of glucagon-like peptide 1 (GLP-1) metabolism by administering therapeutically effective amounts of an inhibitor of dipeptidylpeptidase IV (DPIV) or a pharmaceutically acceptable salt thereof, where the inhibitor has a Ki for inhibition of DPIV of 10 nM or less; and the inhibitor is administered in an amount sufficient to inhibit DPIV proteolysis of GLP-1 but not sufficient to suppress the immune system of the animal.

Abstract: Protracted GLP-1 compounds and therapeutic uses thereof.

Abstract: The disclosure provides the use of GLP-1 receptor agonist compounds to treat pancreatitis (e.g., acute, chronic, hemorrhagic, necrotizing) in patients. The disclosure also provides the use of GLP-1 receptor agonist compounds to reduce elevated plasma amylase and/or lipase concentrations in patients. An exemplary GLP-1 receptor agonist compound is exenatide.

Abstract: The disclosure provides, among other things, the use of GLP-1 receptor agonist compounds to treat obstructive sleep apnea. The GLP-1 receptor agonist compounds may be exendins, exendin analogs, GLP-1(7-37), GLP-1 (7-37) analogs (e.g., GLP-1 (7-36)-NH2) and th like. The GLP-1 receptor agonist compound may be exenatide.

Abstract: The present invention describes the methods of using incretin mimetics such as GLP-1 receptor agonists, particularly exenatide, to treat short bowel syndrome and spastic or hyperactive esophageal motor disorders.

Abstract: Methods and uses for the treatment and prevention of cardiac and cardiovascular diseases comprising administration of a GLP-1 agonist.

Abstract: 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.

Abstract: Novel GLP-1 compounds and their therapeutic use.

Abstract: Provided herein are glucagon analogs comprising a modified amino acid sequence of native human glucagon (SEQ ID NO: 2) that exhibit activity at the glucagon receptor, activity at the GLP-I receptor, or activity at each of the glucagon receptor and the GLP-I receptor. In some embodiments, the glucagon analog exhibits at least 100% or more of the activity of native glucagon at the glucagon receptor and/or at least 100% or more of the activity of native GLP-I at the GLP-I receptor. In some embodiments, the glucagon analog has an EC50 at the GLP-I receptor which is within 50-fold or less than the EC50 at the glucagon receptor. In some embodiments, the glucagon analog has an EC50 at the GLP-I receptor which is two- to ten-fold greater than the EC50 at the glucagon receptor. Related conjugates, dimers and multimers, and pharmaceutical compositions, and uses thereof, are further provided.

Abstract: The present invention provides for compositions and methods for treating or preventing addictive and compulsive diseases and disorders, particular alcohol-related diseases and disorders, disclosed herein. The GLP activators of the present invention are effective against various alcohol and drug dependency diseases. In accordance with the invention, the present compositions and methods can be used to intercede upstream or downstream in the signal transduction cascade involved in GLP action to treat various alcohol and drug dependency diseases. In one embodiment, the synthesis or release of endogenous GLP can be stimulated. In another embodiment, the endogenous synthesis or release of another molecule active in the cascade downstream from GLP, (e.g., a molecule produced in response to GLP binding to a receptor), can be stimulated.

Abstract: A liquid composition comprising a GLP-1 agonist or/and a pharmacologically tolerable salt thereof and, optionally, at least one pharmaceutically acceptable excipient, wherein the composition comprises methionine, as add-on therapy with metformin and/or with long-acting insulin/insulin derivates where appropriate.

Abstract: The invention relates to a pharmaceutical composition comprising 1.a and/or 1.b according to claim 1 in combination with at least one second therapeutic agent 2 which is 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. In addition the present invention relates to methods for preventing or treating of metabolic disorders and related conditions.

Abstract: A method for the prevention of hypoglycaemia in diabetes mellitus type 2 comprising administering (a) desPro36Exendin-4(1-39)-Lys6-NH2 or/and a pharmaceutically acceptable salt thereof, and (b) a sulfonyl urea or/and a pharmaceutically acceptable salt thereof, to a subject in need thereof.

Abstract: 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.

Abstract: [Object] To provide a GPR40 activating agent containing, as an active ingredient, a novel compound having a GPR40 agonist action, a salt of the compound, a solvate of the compound or the salt, or the like, particularly, an insulin secretagogue and a prophylactic and/or therapeutic agent against diabetes, obesity, or other diseases. [Means of Solving the Problem] A compound of Formula (I): (where p is 0 to 4; j is 0 to 2; k is 0 to 1; a ring A is an aryl group, a heterocyclic group, a cycroalkyl group, a cycroalkenyl group, a spirocyclic group; a ring B is an aryl group, a heteroaryl group; X is 0 or —NR7—; and R1 to R7 and L are specific groups), a salt of the compound, or a solvate of the compound or the salt.

Abstract: Provided is a homodimer of insulinotropic peptide analogues and method for preparation thereof and use thereof, wherein the insulinotropic peptide analogue comprises GLP-1 and Exendin-4. The homodimer of insulinotropic peptide analogues of the invention is made by conjugating two identical insulinotropic peptide analogue molecules at the C-terminal Cys residues via disulfide bond or PEG molecule. The homodimer of insulinotropic peptide analogues of the invention has superior stability and biological activity in vivo, and prolonged half-life in the circulation, and can be used for the preparation of hypoglycemic drugs.

Abstract: The present invention generally relates to the field of nutrition and health. In particular, the present invention provides a composition that allows it to treat, limit or prevent muscle atrophy. Embodiments of the present invention are directed at GLP-2 containing compositions and to compositions that stimulate the secretion of GLP-2 in a body to treat or prevent muscle atrophy.

Abstract: The present invention relates to pre-formulations comprising low viscosity, non-liquid crystalline, mixtures of: a) at least one neutral diacyl lipid and/or at least one tocopherol; b) at least one phospholipid; c) at least one biocompatible, oxygen containing, low viscosity organic solvent; wherein at least one bioactive agent is dissolved or dispersed in the low viscosity mixture and wherein the pre-formulation forms, or is capable of forming, at least one liquid crystalline phase structure upon contact with an aqueous fluid. The preformulations are suitable for generating parenteral, non-parenteral and topical depot compositions for sustained release of active agents. The invention additionally relates to a method of delivery of an active agent comprising administration of a preformulation of the invention, a method of treatment comprising administration of a preformulation of the invention and the use of a preformulation of the invention in a method for the manufacture of a medicament.

Abstract: The present application refers to cells, e.g. mesenchymal stem cells or mesenchymal stromal cells, or any further suitable cell, encoding and secreting a neuroprotective factor, an anti-angiogenic factor and/or any other protein or protein-like substance suitable for (intraocular) treatment of eye diseases. Such eye diseases include glaucoma and other optic nerve disorders, retinal diseases, particularly retinitis pigmentosa (RP), age-related macular degeneration (AMD) and diabetic retinopathy, etc. The cells used herein are encapsulated in a (spherical) microcapsule, preferably comprising a core and at least one surface layer, to prevent a response of the immune system of the patient to be treated. The present application also refers to the use of these (spherical) microcapsule(s) or such factors for (intraocular) treatment of eye diseases as defined herein (for the preparation of a (pharmaceutical) composition) for the treatment of such eye diseases.

Abstract: 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.