Entries |
Document | Title | Date |
20100317572 | PHARMACEUTICAL COMPOSITION COMPRISING TESOFENSINE OR ITS ANALOGUE AND AN ANTI-OBESITY COMPOUND - This invention relates to novel pharmaceutical compositions comprising a therapeutically effective combination of a compound of Formula I and an anti-obesity compound. The pharmaceutical compositions for use according to the invention are contemplated particularly useful for combating obesity or an obesity associated disease. | 12-16-2010 |
20110003737 | AZABICYCLOALKANE-INDOLE AND AZABICYCLOALKANE-PYRROLO-PYRIDINE MCH-1 ANTAGONISTS, METHODS OF MAKING, AND USE THEREOF - Novel MCH-1 receptor antagonists are disclosed. These compounds are used in the treatment of various disorders, including obesity, anxiety, depression, non-alcoholic fatty liver disease, and psychiatric disorders. Methods of making these compounds are also described in the present invention. | 01-06-2011 |
20110034373 | 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-1 compound. In addition, the present invention also provides methods to treat obesity by administering an FGF-21 compound in combination with a GLP-1 compound. The present invention also discloses combinations useful in the methods of the present invention. | 02-10-2011 |
20110034374 | Oxyntomodulin for Preventing or Treating Excess Weight - Compositions and methods for use in the prevention or treatment of excess weight in a mammal have been developed. The compositions comprise oxyntomodulin which is shown to reduce food intake. | 02-10-2011 |
20110034375 | NON-BASIC MELANIN CONCENTRATING HORMONE RECEPTOR-1 ANTAGONISTS - The present application provides compounds, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula I. Additionally, the present application provides pharmaceutical compositions containing at least one compound according to Formula I and optionally at least one additional therapeutic agent. Finally, the present application provides methods for treating a patient suffering from an MCHR-1 modulated disease or disorder such as, for example, obesity, diabetes, depression or anxiety by administration of a therapeutically effective dose of a compound according to Formula I. | 02-10-2011 |
20110092417 | LEPTIN FUSION PROTEINS - The disclosure relates to leptin fusion polypeptides; nucleic acid molecules encoding said polypeptides and methods of treatment that use said polypeptides. | 04-21-2011 |
20110130329 | Glp-1 Fusion Peptides, Their Production and Use - The present invention provides fusion peptides having GLP-1 activity and enhanced stability in vivo, in particular resistancy to dipeptidyl peptidase IV. The fusion peptide comprises as component (I) N-terminally a GLP-1(7-35, 7-36 or 7-37) sequence and as component (II) C-terminally a peptide sequence of at least 9 amino acids or a functional fragment, variant or derivative thereof. Component (II) is preferably a full or partial version of IP2 (intervening peptide 2). A preferred embodiment comprises the sequence GLP-1(7-35, 36 or 37)/IP2/GLP-1(7-35, 36 or 37) or GLP-2. The fusion peptide may be produced in engineered cells or synthetically and may be used for the preparation of a medicament for treating various diseases or disorders, e.g. diabetes type 1 or 2, apoptosis related diseases or neurodegenerative disorders. | 06-02-2011 |
20110136733 | ANALOGUES OF GLUCOSE-DEPENDENT INSULINOTROPIC POLYPEPTIDE - There is provided a novel series of analogues of glucose-dependent insulinotropic polypeptide compounds, pharmaceutical compositions containing said compounds, and the use of said compounds as GIP-receptor agonists or antagonists for treatment of GIP-receptor mediated conditions, such as non-insulin dependent diabetes mellitus and obesity. | 06-09-2011 |
20110144008 | PEPTIDE AGONISTS OF 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. | 06-16-2011 |
20110152182 | OXYNTOMODULIN PEPTIDE ANALOGUE - The present invention provides an Oxyntomodulin peptide analogue useful in the treatment of diabetes and/or obesity. | 06-23-2011 |
20110152183 | DERIVATISED HYBRID PEPTIDES OF AMYLIN AND SALMON CALCITONIN - Described are derivatives of hybrid peptides and pharmaceutical compositions comprising such, wherein said hybrid peptides comprise the C-terminal end of the human amylin peptide sequence, the middle portion of the salmon calcitonin peptide sequence and the N-terminal end of the human amylin peptide sequence, and wherein an albumin binding moiety is attached to the hybrid peptide, optionally via a linker. | 06-23-2011 |
20110166062 | GIP-BASED MIXED AGONISTS FOR TREATMENT OF METABOLIC DISORDERS AND OBESITY - Glucagon peptides that exhibit GIP agonist activity in addition to glucagon and/or GLP-I activity are provided. Pharmaceutical compositions comprising such glucagon peptides and therapeutic methods of using such peptides are also provided. | 07-07-2011 |
20110178006 | METHOD FOR ADMINISTERING GLP-1 MOLECULES - The invention relates to formulations that demonstrate the feasibility of oral absorption comprising glucose-like peptide-1 compounds and specified delivery agents, and to methods of stimulating GLP-1 receptor in a subject in need of such stimulation, by administration of the formulation of the present invention. | 07-21-2011 |
20110183899 | METHODS AND COMPOSITIONS FOR THE TREATMENT OF OBESITY - The invention relates to methods and compositions for the treatment of obesity. The methods and compositions relate to the use of an agent that reduces or prevents endoplasmic reticulum stress in conjunction with leptin. | 07-28-2011 |
20110207661 | BENZYLBENZENE DERIVATIVES AND METHODS OF USE - Provided are compounds having an inhibitory effect on sodium-dependent glucose cotransporter SGLT. The invention also provides pharmaceutical compositions, methods of preparing the compounds, synthetic intermediates, and methods of using the compounds, independently or in combination with other therapeutic agents, for treating diseases and conditions which are affected by SGLT inhibition. | 08-25-2011 |
20110237503 | NOVEL PEPTIDES AND METHODS FOR THEIR PREPARATION AND USE - The present invention is in the field of treatment of diabetes and relates to peptides that exhibit activity for both glucose-dependent insulinotropic peptide receptor (GIP-R) and glucagon-like peptide-1 receptor (GLP-1-R) and are selective over glucagon receptor (Gluc-R). Specifically provided are GIP analogs with amino acid substitutions introduced to modulate activity for both GIP-R and GLP-1-R and maintain selectivity over Gluc-R. | 09-29-2011 |
20110245161 | Use of Ghrelin Splice Variant for Treating Hypercholesterolemia and/or High Cholesterol and/or High Cholesterol Complication and/or Lipemia and/or Lipemia Complication and/or Coronary Heart Disease and/or Weight Management and/or Diabetes and/or Hyperglycemia - The present disclosure relates, in one aspect, to use of ghrelin splice variant or an analogue thereof for the preparation of a medicament for one or more of: treatment and/or prevention of hypercholesterolemia and/or high cholesterol and/or high cholesterol complication and/or lipemia and/or lipemia complication and/or CHD and/or weight management and/or diabetes and/or hyperglycemia. | 10-06-2011 |
20110245162 | METHODS FOR TREATING DIABETES AND REDUCING BODY WEIGHT - Methods for reducing body weight, altering body composition, treating diabetes, reducing HbA | 10-06-2011 |
20110288011 | PEPTIDE THERAPEUTIC CONJUGATES AND USES THEREOF - The present invention features a compound having the formula A-X-B, where A is peptide vector capable of enhancing transport of the compound across the blood-brain barrier or into particular cell types, X is a linker, and B is a peptide therapeutic. The compounds of the invention can be used to treat any disease for which the peptide therapeutic is useful. | 11-24-2011 |
20110301080 | PHARMACEUTICAL COMPOSITIONS - The present invention provides pharmaceutical compositions comprising at least one polypeptide having GLP-1 activity wherein an effective dose of said pharmaceutical composition comprises 15 mg, 30 mg, 50 mg or 100 mg of said polypeptide having GLP-1 activity. Also provided are methods of administering the pharmaceutical compositions of the invention. | 12-08-2011 |
20120021976 | BICYCLIC PIPERIDINE AND PIPERAZINE DERIVATIVES AS GPCR MODULATORS FOR THE TREATMENT OF OBESITY, DIABETES AND OTHER METABOLIC DISORDERS - The present invention relates to Bicyclic Piperidine and piperazine Derivatives, compositions comprising a Bicyclic Piperidine and piperazine Derivative, and methods of using the Bicyclic Piperidine and piperazine Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of a GPCR in a patient. | 01-26-2012 |
20120046222 | N-TERMINUS CONFORMATIONALLY CONSTRAINED GLP-1 RECEPTOR AGONIST COMPOUNDS - The disclosure provides N-terminus conformationally constrained compounds, which may comprise peptide mimetics and/or amino acid substitutions, which may be used in peptides, such as GLP-1 receptor agonist compounds, to induce a β-turn secondary structure at the N-terminus. The N-terminus conformationally constrained compounds may be used for research purposes; to produce GLP-1 receptor agonist compounds having improved GLP-1 receptor binding activity, enzymatic stability, or in vivo glucose lowering activity; and to develop GLP-1 receptor agonist compounds which have fewer amino acid residues. The disclosure also provides GLP-1 receptor agonist compounds, such as exendins, exendin analogs, GLP-1 (7-37), GLP-1 (7-37) analogs, comprising the N-terminus conformationally constrained compounds. The compounds are useful for treating various diseases, such as diabetes and obesity. The disclosure also provides methods for chemically synthesizing the N-terminus conformationally constrained compounds. | 02-23-2012 |
20120058939 | AZABICYCLOALKANE-INDOLE AND AZABICYCLOALKANE-PYRROLO-PYRIDINE MCH-1 ANTAGONISTS, METHODS OF MAKING, AND USE THEREOF - Novel MCH-1 receptor antagonists are disclosed. These compounds are used in the treatment of various disorders, including obesity, anxiety, depression, non-alcoholic fatty liver disease, and psychiatric disorders. Methods of making these compounds are also described in the present invention. | 03-08-2012 |
20120071401 | AMYLIN AGONIST COMPOUNDS FOR ESTROGEN-DEFICIENT MAMMALS - Provided herein are methods to treat estrogen deficiency in mammals by administering amylin agonist compounds. Also provided herein are methods to treat obesity and overweight in estrogen-deficient mammals; methods to reduce or maintain body weight and/or body fat in estrogen-deficient mammals; and methods to increase Bdnf levels in mammals by administering effective amounts of amylin agonist compounds. The estrogen deficiency may be caused by menopause, perimenopause, post-menopause, ovarian dysfunction, an overectomy, a hysterectomy, and the like. The amylin agonist compounds may be any known in the art or described herein, such as pramlintide, davalintide, or SEQ ID NO: 142. | 03-22-2012 |
20120071402 | Protease Stabilized, Pegylated Insulin Analogues - Novel PEGylated insulin analogues exhibiting resistance towards proteases can, effectively, be administered pulmonary or orally. The insulin analogues contain B25H and A14E or A14H. The PEGylation is at B29K. | 03-22-2012 |
20120071403 | Methods for Treating Type 2 Diabetes in Patients Resistant to Previous Treatment with other Anti-Diabetic Drugs Employing an SGLT2 Inhibitor and Compositions Thereof - The invention provides methods for treating a patient having type 2 diabetes who has failed on previous regimens of one or more oral and/or injectable anti-diabetic agents, which include the step of administering a therapeutically effective amount of an SGLT2 inhibitor alone or in combination with another anti-diabetic agent and/or other therapeutic agent to such patient. A pharmaceutical composition containing dapagliflozin or dapagliflozin-S-propylene glycol solvate and one or more diabetic agents and/or other therapeutic agents for use in the methods of the invention is also provided. | 03-22-2012 |
20120115777 | Use of Ultrarapid Acting Insulin - Disclosed herein are improved methods of treating hyperglycemia with a combination of an ultrarapid acting insulin and insulin glargine comprising prandial administration of the ultrarapid insulin, and administration of a first dose of insulin glargine within 6 hours of waking for a day. | 05-10-2012 |
20120115778 | Methods of Suppressing Appetite by the Administration of Antagonists of the Serotonin HTR1a or HTR2b Receptors or Inhibitors of TPH2 - Methods for treating eating disorders associated with excessive weight gain, suppressing appetite, reducing body weight, or treating obesity in an animal by administering one or more antagonists of the serotonin Htr1a or Htr2b receptor, or a Tph2 inhibitor are provided, or combinations thereof. | 05-10-2012 |
20120129767 | USE OF A GHRELIN AGONIST TO IMPROVE THE CATABOLIC EFFECTS OF GLUCOCORTICOID TREATMENT - A method and pharmaceutical composition for inhibiting the effect of glucocorticoids, particularly dexamethasone, which suppress growth hormone secretion, by administering ghrelin or a ghrelin analogue, for example, [Aib | 05-24-2012 |
20120129768 | GLP-1 ANALOGUES AND THEIR PHARMACEUTICAL SALTS AND USES - This invention discloses GLP-1 analogues and their pharmaceutical salts, wherein the GLP-1 analogue comprises an amino acid sequence of general formula (I), wherein Lys represents a modified lysine with a lipophilic acid. The GLP-1 analogues provided by this invention have the function of human GLP-1, and a longer half-life in vivo compared with the human GLP-1. Uses of such compounds and compositions include treating non-insulin-dependent diabetes, insulin-dependent diabetes, and obesity. | 05-24-2012 |
20120172295 | GIP RECEPTOR-ACTIVE GLUCAGON COMPOUNDS - Glucagon peptides with increased GIP activity are provided, optionally with GLP-I and/or glucagon activity. In some embodiments, C-terminally extended glucagon peptides comprising an amino acid sequence substantially similar to native glucagon are provided herein. | 07-05-2012 |
20120190616 | Analogues of Insulin-Like Growth Factor-1 (IGF-1) Having Amino Acid Substitution at Position 59 - The present invention relates to novel analogues of insulin-like growth factor-1 (IGF-1), pharmaceutical compositions containing said analogues, and the use of said analogues for treatment of IGF-1-receptor mediated conditions, such as short stature, diabetes therapy, neurodegenerative disease treatment, and cartilage repair. More particularly, the present invention relates to novel analogues of IGF-1 having an amino acid substitution at position 59, e.g., (Asn | 07-26-2012 |
20120196798 | GLP-1 ANALOGUES AND THEIR PHARMACEUTICAL SALTS AND USES - This invention discloses GLP-1 analogues and their pharmaceutical salts, wherein the GLP-1 analogue comprises an amino acid sequence of general formula (I), wherein Lys represents a modified lysine with a lipophilic acid. The GLP-1 analogues provided by this invention have the function of human GLP-1, and a longer half-life in vivo compared with the human GLP-1. Uses of such compounds and compositions include treating non-insulin-dependent diabetes, insulin-dependent diabetes, and obesity. | 08-02-2012 |
20120196799 | Amylin Family Peptides and Methods for Making and Using Them - Methods for treating obesity are disclosed which comprise administration of a therapeutically effective amount of an amylin or an amylin agonist alone or in conjunction with another obesity relief agent. Additionally, methods for reducing insulin-induced weight gain are disclosed which comprise administration of a therapeutically effective amount of an amylin or an amylin agonist. | 08-02-2012 |
20120238493 | GLUCAGON ANALOGS EXHIBITING GIP RECEPTOR ACTIVITY - Provided herein are glucagon analogs which exhibit potent activity at the GIP receptor, and, as such are contemplated for use in treating diabetes and obesity. In exemplary embodiments, the glucagon analog of the present disclosures exhibit an EC50 at the GIP receptor which is within the nanomolar or picomolar range. | 09-20-2012 |
20120245083 | Derivatives of CGRP - Acylated CGRP compounds with a linker have prolonged action and are valuable as medicaments. | 09-27-2012 |
20120277147 | PREVENTION OF HYPOGLYCAEMIA IN DIABETES MELLITUS TYPE 2 PATIENTS - A method for the prevention of hypoglycaemia in diabetes mellitus type 2 comprising administering (a) desPro | 11-01-2012 |
20120283179 | PHARMACEUTICAL COMPOSITION COMPRISING A GLP-1 AGONIST AND METHIONINE - 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. | 11-08-2012 |
20120329707 | GLUCAGON/GLP-1 RECEPTOR CO-AGONISTS - Provided herein are peptides and variant peptides that exhibit enhanced activity at the GLP-1 receptor, as compared to native glucagon. | 12-27-2012 |
20120329708 | GLUCAGON/GLP-1 RECEPTOR CO-AGONISTS - Provided herein are peptides and variant peptides that exhibit enhanced activity at the GLP-1 receptor, as compared to native glucagon. | 12-27-2012 |
20130005649 | PHARMACEUTICAL COMBINATION FOR IMPROVING GLYCEMIC CONTROL AS ADD-ON THERAPY TO BASAL INSULIN - The present invention refers to a pharmaceutical combination for use in glycemic control in diabetes type 2 patients. | 01-03-2013 |
20130023467 | PHARMACEUTICAL COMBINATION FOR USE IN INDUCING WEIGHT LOSS IN DIABETES TYPE 2 PATIENTS OR/AND FOR PREVENTING WEIGHT GAIN IN DIABETES TYPE 2 PATIENTS - The present invention refers to a pharmaceutical combination for use in inducing weight loss in diabetes type 2 patients or/and for preventing weight gain in diabetes type 2 patients. | 01-24-2013 |
20130035285 | NOVEL GLUCAGON ANALOGUES - 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. | 02-07-2013 |
20130053307 | METHOD FOR WEIGHT LOSS AIDED BY ADMINISTRATION OF HUMAN CHORIONIC GONADOTROPIN - Methods are provided for increased rates of weight loss while reducing the discomfort caused by dieting. An initial daily dose of HCG of 200 IU or greater is administered to a patient on a reduced calorie diet plan for weight loss. The reduced calorie diet plan includes limits on the amounts of protein, vegetables and fruits that may be eaten based upon caloric content and sugar levels in the vegetables and fruit. In one embodiment, the reduced calorie diet plan limits caloric intake to 500-800 calories per day. The patient is monitored and the daily HCG dose may be adjusted upward as needed to control hunger and maintain patient comfort. | 02-28-2013 |
20130079277 | THERAPEUTIC AGENTS COMPRISING ELASTIN-LIKE PEPTIDES - The present invention provides therapeutic agents and compositions comprising elastin-like peptides (ELPs) and therapeutic proteins. In some embodiments, the therapeutic protein is a GLP-1 receptor agonist, insulin, or Factor VII/VIIa, including functional analogs. The present invention further provides encoding polynucleotides, as well as methods of making and using the therapeutic agents. The therapeutic agents have improvements in relation to their use as therapeutics, including, inter alia, one or more of half-life, clearance and/or persistance in the body, solubility, and bioavailability. | 03-28-2013 |
20130079278 | Novel Glucagon Analogues - The present invention relates to novel glucagon peptides, to the use of said glucagon peptides in therapy, to methods of treatment comprising administration of said glucagon peptides to patients in need thereof, and to the use of said glucagon peptides in the manufacture of medicaments. The glucagon peptides of the present 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. | 03-28-2013 |
20130085099 | THERAPEUTIC AGENTS COMPRISING ELASTIN-LIKE PEPTIDES - The present invention provides therapeutic agents and compositions comprising elastin-like peptides (ELPs) and therapeutic proteins. In some embodiments, the therapeutic protein is a GLP-1 receptor agonist, insulin, or Factor VII/VIIa, including functional analogs. The present invention further provides encoding polynucleotides, as well as methods of making and using the therapeutic agents. The therapeutic agents have improvements in relation to their use as therapeutics, including, inter alia, one or more of half-life, clearance and/or persistence in the body, solubility, and bioavailability. | 04-04-2013 |
20130085100 | New Uses of Oxytocin-Like Molecules and Related Methods - The present invention is directed to a derivative selected from oxytocin, an oxytocin derivative, and an oxytocin agonist useful for the treatment of a disorder selected from obesity and insulin resistance and related methods and pharmaceutical formulations. In particular, the invention relates to a derivative selected from oxytocin, an oxytocin derivative, and an oxytocin agonist useful in the treatment of metabolic syndrome. | 04-04-2013 |
20130090285 | METHODS OF TREATMENT WITH GLP-1 RECEPTOR AGONISTS - The invention provides methods for treating diabetes or obesity, as well as methods for inducing weight loss, preventing weight gain, or controlling weight in a patient in need thereof. The methods comprise administering to the patient at least one effective dose of a GLP-1 receptor agonist, or a regimen of GLP-1 receptor agonist comprising a plurality of substantially evenly spaced doses. The effective dose or regimen does not induce substantial nausea or appetite suppression in the patient. | 04-11-2013 |
20130090286 | 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). | 04-11-2013 |
20130090287 | Devices, Formulations, and Methods for Delivery of Multiple Beneficial Agents - The present invention relates to osmotic delivery devices, formulations, and methods for delivery of two or more beneficial agents. In one aspect, the present invention provides osmotic delivery devices useful for substantially concurrent administration of two or more beneficial agents. In another aspect, the present invention provides beneficial agent formulations for use in the osmotic delivery devices. The formulations include formulations wherein beneficial agents are soluble in the vehicle, suspension formulations comprising particle formulations of one or more beneficial agent, and combinations thereof. Further, methods for treatment of a variety of diseases or conditions using two or more beneficial agents are disclosed, wherein the methods are preferably practiced using the osmotic delivery devices and/or formulations of the invention. | 04-11-2013 |
20130102528 | Methods and Pharmaceutical Composition for the Treatment of a Feeding Disorder with Early-Onset in a Patient - The present invention relates to a compound which is an agonist of the oxytocin receptor o for use in the treatment of a feeding disorder with early-onset. In a particular embodiment, the agonist of the oxytocin receptor is the oxytocin or an active fragment thereof. | 04-25-2013 |
20130116172 | GLUCAGON SUPERFAMILY PEPTIDES EXHBITING G PROTEIN COUPLED RECEPTOR ACTIVITY - Provided herein are glucagon superfamily peptides conjugated with GPCR ligands that are capable of acting at a G protein-coupled receptor. Also provided herein are pharmaceutical compositions and kits of the conjugates of the invention. Further provided herein are methods of treating a disease, e.g., a metabolic disorder, such as diabetes and obesity, comprising administering the conjugates of the invention. | 05-09-2013 |
20130116173 | Glucagon Analogs Exhibiting GIP Receptor Activity - Provided herein are glucagon analogs which exhibit potent activity at the GIP receptor, and, as such are contemplated for use in treating diabetes and obesity. In exemplary embodiments, the glucagon analog of the present disclosures exhibit an EC50 at the GIP receptor which is within the nanomolar or picomolar range. | 05-09-2013 |
20130123169 | PEPTIDOMIMETIC MACROCYCLES - The present invention provides peptidomimetic macrocycles capable of modulating growth hormone levels and methods of using such macrocycles for the treatment of disease. | 05-16-2013 |
20130123170 | Growth Hormone Releasing Peptides - Disclosed are peptide and peptidomimetic compounds generally according to formula (I) that are useful as GHRP analogs: | 05-16-2013 |
20130137631 | GIP ANALOG AND 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. | 05-30-2013 |
20130143798 | NOVEL GLUCAGON ANALOGUES - The present invention relates to novel peptide compounds which have an improved physical stability in solution and improved solubility at neutral pH, 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. | 06-06-2013 |
20130157933 | ALBUMIN FUSION PROTEINS - The present invention encompasses albumin fusion proteins. Nucleic acid molecules encoding the albumin fusion proteins of the invention are also encompassed by the invention, as are vectors containing these nucleic acids, host cells transformed with these nucleic acids vectors, and methods of making the albumin fusion proteins of the invention and using these nucleic acids, vectors, and/or host cells. Additionally the present invention encompasses pharmaceutical compositions comprising albumin fusion proteins and methods of treating or preventing diseases, disorders or conditions related to diabetes mellitus using albumin fusion proteins of the invention. | 06-20-2013 |
20130157934 | Glucagon Superfamily Peptides Exhibiting Glucocorticoid Receptor Activity - Provided herein are glucagon superfamily peptides conjugated with GR ligands that are capable of acting at a glucocorticoid receptor. Also provided herein are pharmaceutical compositions and kits of the conjugates of the invention. Further provided herein are methods of treating a disease, e.g., a metabolic disorder, such as diabetes and obesity, comprising administering the conjugates of the invention. | 06-20-2013 |
20130157935 | GLUCAGON ANALOGUES - The invention provides materials and methods for promoting weight loss or preventing weight gain without affecting glycemic control. In particular, the invention provides novel 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. | 06-20-2013 |
20130157936 | MODULATION OF GHRELIN LEVELS AND GHRELIN/UNACYLATED GHRELIN RATIO USING UNACYLATED GHRELIN - A method and a composition for decreasing ghrelin levels and/or decreasing ghrelin/unacylated ghrelin ratio in a subject, the method comprising administering an effective amount of unacylated ghrelin, a fragment thereof, an analog thereof and/or pharmaceutically acceptable salts thereof to the subject wherein a reduction in ghrelin levels and/or a reduction in ghrelin/unacylated ghrelin ratio is beneficial to the subject. Also, use of ghrelin level and/or ghrelin/unacylated ghrelin ratio as biomarkers for determining a subject's likelihood of responding to and/or benefiting from administration of unacylated ghrelin. | 06-20-2013 |
20130172243 | Methods for Treating Diabetes and Reducing Body Weight - Methods for reducing body weight, altering body composition, treating diabetes, reducing HbA | 07-04-2013 |
20130172244 | SUBCUTANEOUS THERAPEUTIC USE OF DPP-4 INHIBITOR - The present invention relates to methods for treating and/or preventing metabolic diseases comprising the subcutaneous or transdermal administration of a therapeutically effective amount of a certain DPP-4 inhibitor. The invention further relates to a subcutaneous combination of a certain DPP-4 inhibitor and GLP-1 having a short half life, particularly for reducing weight. | 07-04-2013 |
20130184203 | GLP-1 RECEPTOR AGONIST COMPOUNDS HAVING STABILIZED REGIONS - The disclosure provides GLP-1 receptor agonist compounds having stabilized regions corresponding to alpha-helical regions of the natural peptide compounds. The disclosure also provides benzamide-containing exendin-4 analogs and alkene-constrained exendin-4 analogs, both of which have stabilized regions corresponding to alpha-helical regions of exendin-4. | 07-18-2013 |
20130203659 | GLP-1 COMPOUNDS - GLP-1 compounds comprising GLP-1 analogs and methods of using the GLP-1 compounds for treating metabolic disorders, enhancing insulin expression, and promoting insulin secretion in a patient are provided. | 08-08-2013 |
20130203660 | 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 lactam 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, substitution of carboxy terminal amino acids, 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). | 08-08-2013 |
20130203661 | HIGHLY SOLUBLE LEPTINS - The disclosure provides chimeric polypeptides and nucleic acid molecules encoding chimeric polypeptides. Also provided are pharmaceutical compositions and methods of treatment for diseases and disorders including lipodystrophy, dyslipidemia, hyperlipidemia, overweight, obesity, hypothalamic amenorrhea, Alzheimer's disease, leptin deficiency, fatty liver disease or diabetes (including type I and type II). Additional diseases and disorders which can be treated by the compounds and methods described herein include nonalcoholic steatohepatitis (NASH) and nonalcoholic fatty liver disease (NAFLD), metabolic syndrome X and Huntington's Disease. | 08-08-2013 |
20130231279 | OXYTOCIN TREATMENT TO IMPROVE MEMORY AND MODIFY BLOOD GLUCOSE - The disclosure provides a method for enhancing memory of a subject, lowering blood glucose levels in a subject, and treating schizophrenia, the methods comprise intranasally administering to the subject an amount of a oxytocin peptide or analogue thereof having a beneficial effect. | 09-05-2013 |
20130274182 | ENGINEERED POLYPEPTIDES HAVING ENHANCED DURATION OF ACTION - Compounds are provided having inter alia good duration of action, high potency and/or convenient dosing regimens including once weekly administration. The compounds are engineered polypeptides which incorporate an albumin binding domain in combination with one or more biologically active polypeptides. Also provided are pharmaceutical compositions and methods of treatment for diseases and disorders including lipodystrophy, dyslipidemia, hyperlipidemia, overweight, obesity, hypothalamic amenorrhea, Alzheimer's disease, leptin deficiency, fatty liver disease or diabetes (including type I and type II). Additional diseases and disorders which can be treated by the compounds and methods described herein include nonalcoholic steatohepatitis (NASH) and nonalcoholic fatty liver disease (NAFLD), metabolic syndrome X and Huntington's Disease. | 10-17-2013 |
20130288958 | Novel Glucagon Analogues - The present invention relates to novel glucagon peptides, to the use of said glucagon peptides in therapy, to methods of treatment comprising administration of said glucagon peptides to patients in need thereof, and to the use of said glucagon peptides in the manufacture of medicaments. The glucagon peptides of the present 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. | 10-31-2013 |
20130324463 | USE OF A DPP-4 INHIBITOR FOR MODIFYING FOOD INTAKE AND REGULATING FOOD PREFERENCE - The present invention relates to the use of a certain DPP-4 inhibitor for modifying food intake and regulating food preference. | 12-05-2013 |
20130331316 | CHIMERIC FIBROBLAST GROWTH FACTOR 21 PROTEINS AND METHODS OF USE - The present invention relates to a chimeric protein that includes an N-terminus coupled to a C-terminus, where the N-terminus includes a portion of a paracrine fibroblast growth factor (“FGF”) and the C-terminus includes a C-terminal portion of an FGF21 molecule. The portion of the paracrine FGF is modified to decrease binding affinity for heparin and/or heparan sulfate compared to the portion without the modification. The present invention also relates to pharmaceutical compositions including chimeric proteins according to the present invention, methods for treating a subject suffering from diabetes, obesity, or metabolic syndrome, and methods of screening for compounds with enhanced binding affinity for the βKlotho-FGF receptor complex involving the use of chimeric proteins of the present invention. | 12-12-2013 |
20130331317 | CHIMERIC FIBROBLAST GROWTH FACTOR 19 PROTEINS AND METHODS OF USE - The present invention relates to a chimeric protein that includes an N-terminus coupled to a C-terminus, where the N-terminus includes a portion of a paracrine fibroblast growth factor (“FGF”) and the C-terminus includes a C-terminal portion of an FGF19 molecule. The portion of the paracrine FGF is modified to decrease binding affinity for heparin and/or heparan sulfate compared to the portion without the modification. The present invention also relates to pharmaceutical compositions including chimeric proteins according to the present invention, methods for treating a subject suffering from diabetes, obesity, or metabolic syndrome, and methods of screening for compounds with enhanced binding affinity for the βKlotho-FGF receptor complex involving the use of chimeric proteins of the present invention. | 12-12-2013 |
20140005106 | METHOD FOR ADMINISTERING GLP-1 MOLECULES | 01-02-2014 |
20140018290 | LEPTIN DERIVATIVES - The invention relates to Leptin derivatives, compositions and therapeutic use there-of. | 01-16-2014 |
20140018291 | METHODS FOR TREATING METABOLIC DISORDERS AND OBESITY WITH GIP AND GLP-1 RECEPTOR-ACTIVE GLUCAGON-BASED PEPTIDES - Methods are provided for administering an extended half-life GLP-1/GIP coagonist peptide to a patient in need thereof for reducing weight gain, inducing weight loss, treating hyperglycemia, reducing blood glucose levels, or normalizing blood glucose levels in said patient. | 01-16-2014 |
20140031278 | Novel Glucagon Analogues - The present invention relates to novel glucagon peptides with improved stability and solubility at neutral pH, 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 glucagon peptides 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. | 01-30-2014 |
20140057839 | FORMULATIONS AND METHODS FOR WEIGHT LOSS AND BODY CONTOURING - Formulations and methods for weight loss and body contouring are disclosed. An illustrative formulation comprises human chorionic gonadotrophin (hCG) and resveratrol. An illustrative method for weight loss and body contouring comprises administering hCG and resveratrol sublingually. | 02-27-2014 |
20140073563 | FUSION PROTEINS FOR TREATING A METABOLIC SYNDROME - The invention is directed to a fusion protein comprising at least one FGF-21 (fibroblast growth factor-21) compound and at least one GLP-1R (glucagon-like peptide-1 receptor) agonist as well as to pharmaceutical compositions, medical uses and methods of treatment involving the fusion protein, particularly in the field of diabetes, dyslipidemia, obesity and/or adipositas. | 03-13-2014 |
20140094406 | CHIMERIC FIBROBLAST GROWTH FACTOR 21 PROTEINS AND METHODS OF USE - The present invention relates to a chimeric protein that includes an N-terminus coupled to a C-terminus, where the N-terminus includes a portion of a paracrine fibroblast growth factor (“FGF”) and the C-terminus includes a C-terminal portion of an FGF21 molecule. The portion of the paracrine FGF is modified to decrease binding affinity for heparin and/or heparan sulfate compared to the portion without the modification. The present invention also relates to pharmaceutical compositions including chimeric proteins according to the present invention, methods for treating a subject suffering from diabetes, obesity, or metabolic syndrome, and methods of screening for compounds with enhanced binding affinity for the βKlotho-FGF receptor complex involving the use of chimeric proteins of the present invention. | 04-03-2014 |
20140107021 | GLUCAGON ANTAGONIST-GIP AGONIST CONJUGATES AND COMPOSITIONS FOR THE TREATMENT OF METABOLIC DISORDERS AND OBESITY - Provided herein are peptide combinations comprising a GIP agonist peptide and a glucagon antagonist peptide. In some embodiments, the peptide combination is provided as a composition, e.g., a pharmaceutical composition, while in other embodiments, the peptide combination is provided as a kit. In yet other embodiments, the peptide combination is provided as a conjugate, e.g., a fusion peptide, a heterodimer. In specific aspects, the GIP agonist peptide is an analog of native human glucagon. In specific aspects, the glucagon antagonist peptide is an analog of native human glucagon. In some embodiments, the GIP agonist peptide is covalently attached to the glucagon antagonist peptide via a linker. Method of treating a disease, e.g., a metabolic disorder, such as diabetes and obesity, comprising administering the peptide compositions described herein are further provided. | 04-17-2014 |
20140107022 | CHIMERIC FIBROBLAST GROWTH FACTOR 19 PROTEINS AND METHODS OF USE - The present invention relates to a chimeric protein that includes an N-terminus coupled to a C-terminus, where the N-terminus includes a portion of a paracrine fibroblast growth factor (“FGF”) and the C-terminus includes a C-terminal portion of an FGF19 molecule. The portion of the paracrine FGF is modified to decrease binding affinity for heparin and/or heparan sulfate compared to the portion without the modification. The present invention also relates to pharmaceutical compositions including chimeric proteins according to the present invention, methods for treating a subject suffering from diabetes, obesity, or metabolic syndrome, and methods of screening for compounds with enhanced binding affinity for the βKlotho-FGF receptor complex involving the use of chimeric proteins of the present invention. | 04-17-2014 |
20140121154 | Compositions Comprising Glucagon Analogs And Methods Of Making And Using The Same - This invention relates to novel compositions comprising analogs of glucagon, wherein the analog comprises an α-amino acid and at least one β-amino acid. Administration of the compositions may be used for effecting treatment or prevention of a plurality of disease states caused by dysfunctional biochemical or biological pathways, including diabetes and other metabolic disorders. The compositions and methods of this invention are particularly useful to identify novel therapeutic modulators of in-vivo receptor activity with extended half-lives and relevant bioactivity as compared to the naturally translated polypeptides upon which the analogs are derived. | 05-01-2014 |
20140121155 | Crystal Forms of Saxagliptin and Processes for Preparing Same - Physical crystal structures of a compound of the formula I: | 05-01-2014 |
20140148383 | Entacapone for prevention and treatment of obesity and related metabolic diseases - Obesity is inhibited by administering to a person in need thereof an effective amount of entacapone ((2E)-2-cyano-3-(3,4-dihydroxy-5-nitrophenyl)-N,N-diethylprop-2-enamide), or a pharmaceutically-acceptable salt thereof, particularly in conjunction with a second, different anti-obesity medicament. Pharmaceutical compositions comprise entacapone copackaged or coformulated with a second, different anti-obesity medicament. | 05-29-2014 |
20140162944 | CONTROLLED RELEASE PEPTIDE FORMULATIONS - The present invention relates to compositions forming a low viscosity mixture of: a) 20-80 wt. % of at least one diacyl glycerol and/or a tocopherol; b) 20-80 wt. % of at least one phosphatidyl choline (PC); c) 5-20 wt. % of at least one biocompatible, organic mono-alcoholic solvent; d) up to 20 wt. % polar solvent e) at least one peptide active agent; f) optionally at least one antioxidant; wherein the ratio of components a:b is in the range 40:60 to 54:46; wherein the pre-formulation forms, or is capable of forming, at least one liquid crystalline phase structure upon contact with excess aqueous fluid. The invention further relates to methods of treatment comprising administration of such compositions, and to pre-filled administration devices and kits containing the formulations. | 06-12-2014 |
20140162945 | GLUCOSE DEPENDENT INSULINOTROPIC POLYPEPTIDE ANALOGS, PHARMACEUTICAL COMPOSITIONS AND USE THEREOF - The present invention provides a GIP analog, which is derived from GIP (1-29, SEQ ID NO: 1), has both GLP-1 agonist activity and GIPR stimulation activity, and comprises an amino acid sequence represented by the following formula I: Tyr-A2-A3-Gly-Thr-Phe-A7-Ser-Asp-Tyr-Ser-A12-A13-A14-A15-Lys-A17-A18-A19-A20-A21-A22-A23-A24-Trp-Leu-A27-A28-A29-Y. The present invention also provides a pharmaceutical composition comprising the GIP analog and use thereof. | 06-12-2014 |
20140162946 | FORMULATIONS AND METHODS FOR WEIGHT LOSS AND BODY CONTOURING - Formulations and methods for weight loss and body contouring are disclosed. An illustrative formulation comprises human chorionic gonadotrophin (hCG) and resveratrol. An illustrative method for weight loss and body contouring comprises administering hCG and resveratrol sublingually. | 06-12-2014 |
20140206607 | GLUCAGON/GLP-1 RECEPTOR CO-AGONISTS - Provided herein are peptides and variant peptides that exhibit enhanced activity at the GLP-1 receptor, as compared to native glucagon. | 07-24-2014 |
20140206608 | Exendin-4 Derivatives - The present invention relates to exendin-4 derivatives and their medical use, for example in the treatment of disorders of the metabolic syndrome, including diabetes and obesity, as well as reduction of excess food intake. | 07-24-2014 |
20140206609 | Functionalized Exendin-4 Derivatives - The present invention relates to exendin-4 derivatives and their medical use, for example in the treatment of disorders of the metabolic syndrome, including diabetes and obesity, as well as reduction of excess food intake. | 07-24-2014 |
20140221282 | LONG DURATION DUAL HORMONE CONJUGATES - There are provided compounds having two peptide hormones bound to a central water-soluble polymeric spacer and methods of use thereof. | 08-07-2014 |
20140221283 | GLUCAGON/GLP-1 RECEPTOR CO-AGONISTS - Provided herein are peptides and variant peptides that exhibit enhanced activity at the GLP-1 receptor, as compared to native glucagon. | 08-07-2014 |
20140235535 | ENGINEERED POLYPEPTIDES HAVING ENHANCED DURATION OF ACTION WITH REDUCED IMMUNOGENICITY - Compounds are provided having inter alia good duration of action, high potency and/or convenient dosing regimens including oral administration, and reduced immunogenicity. The compounds are engineered polypeptides which incorporate an albumin binding domain in combination with one or more biologically active polypeptides. Also provided are pharmaceutical compositions and methods of treatment for diseases and disorders including obesity and overweight, diabetes, dyslipidemia, hyperlipidemia, Alzheimer's disease, fatty liver disease, Short Bowel Syndrome, Parkinson's disease, and cardiovascular disease. | 08-21-2014 |
20140243260 | CHIMERIC FIBROBLAST GROWTH FACTOR 23 PROTEINS AND METHODS OF USE - The present invention relates to an isolated chimeric protein. The isolated chimeric protein includes an N-terminus coupled to a C-terminus, where the N-terminus includes an N-terminal portion from a fibroblast growth factor (“FGF”) 23 molecule and the C-terminus includes a C-terminal portion from an FGF19 molecule. The present invention also relates to a pharmaceutical composition including an isolated chimeric protein and a pharmaceutically acceptable carrier. The isolated chimeric protein includes an N-terminus coupled to a C-terminus, where the N-terminus includes an N-terminal portion from a fibroblast growth factor (“FGF”) 23 molecule and the C-terminus includes a C-terminal portion from an FGF19 molecule, and a pharmaceutically-acceptable carrier. Yet another aspect of the present invention relates to a method for treating a subject suffering from a disorder. This method includes selecting a subject suffering from the disorder and administering to the subject a therapeutically effective amount of a chimeric protein according to the present invention. | 08-28-2014 |
20140249077 | GEL COMPOSITIONS - The present invention is directed to compositions and methods of preparation of phospholipid gels. | 09-04-2014 |
20140256621 | ENGINEERED POYPEPTIDES HAVING ENHANCED DURATION OF ACTION AND REDUCED IMMUNOGENICITY - Compounds are provided having inter alia good duration of action, high potency and/or convenient dosing regimens including once weekly administration. The compounds are engineered polypeptides which incorporate an albumin binding domain in combination with one or more biologically active polypeptides. Also provided are pharmaceutical compositions and methods of treatment for diseases and disorders including lipodystrophy, dyslipidemia, hyperlipidemia, overweight, obesity, hypothalamic amenorrhea, Alzheimer's disease, leptin deficiency, fatty liver disease or diabetes (including type I and type II). Additional diseases and disorders which can be treated by the compounds and methods described herein include nonalcoholic steatohepatitis (NASH) and nonalcoholic fatty liver disease (NAFLD), metabolic syndrome X and Huntington's Disease. | 09-11-2014 |
20140323397 | TREATMENTS FOR GASTROINTESTINAL DISORDERS - The present invention provides new uroguanylin derivatives that are useful for the treatment of gastrointestinal disorders. The present invention also provides compositions and methods of treating gastrointestinal disorders and pharmaceutical compositions for accomplishing the same. In some embodiments, these pharmaceutical compositions include oral dosage forms. | 10-30-2014 |
20140329743 | Method of Treating Melanocortin-4 Receptor-Associated Disorders in Heterozygous Carriers - A method of treating a disorder in a subject. The method comprises administering to said subject an effective amount of an agonist of the melanocortin-4 receptor (MC4R). The subject is a heterozygous carrier of an MC4R mutation, and the disorder results from an attenuated response of MC4R to a-melanocortin stimulating hormone (a-MSH). | 11-06-2014 |
20140336109 | MODULATION OF GHRELIN LEVELS AND GHRELIN/UNACYLATED GHRELIN RATIO USING UNACYLATED GHRELIN - A method and a composition for decreasing ghrelin levels and/or decreasing ghrelin/unacylated ghrelin ratio in a subject, the method comprising administering an effective amount of unacylated ghrelin, a fragment thereof, an analog thereof and/or pharmaceutically acceptable salts thereof to the subject wherein a reduction in ghrelin levels and/or a reduction in ghrelin/unacylated ghrelin ratio is beneficial to the subject. Also, use of ghrelin level and/or ghrelin/unacylated ghrelin ratio as biomarkers for determining a subject's likelihood of responding to and/or benefiting from administration of unacylated ghrelin. | 11-13-2014 |
20140349923 | Compositions And Methods For Treating Diabetes And/Or Obesity - Compositions are disclosed which comprise one or more of the following; an anthocyanin, an oligosaccharide, a pectin, or a long-chain fatty acid. Such compositions are useful for treating diabetes or obesity. | 11-27-2014 |
20140357552 | PEPTIDE COMPOUND - The present invention provides a novel peptide compound having an activating action on GLP-1 receptors and GIP receptors and use of the peptide compound as a medicament. Specifically, a peptide containing a partial sequence represented by the formula (I) or a salt thereof and a medicament comprising the same are provided. | 12-04-2014 |
20150025002 | PEPTIDES AND PEPTIDE DERIVATIVES BASED ON XENIN - The invention relates to peptides and peptide derivatives based on the naturally occurring peptide xenin. The invention provides a peptide of SEQ ID No. 1 or an analogue thereof which is able to stimulate insulin secretion and which has no more than 7 amino acid substitutions or deletions as compared to the native sequence, the peptide having one or more lysine residues substituted with a lipophilic substituent of 840 carbon atoms, optionally via a spacer. The present invention also provides a peptide of SEQ ID No. 1 or an analogue thereof which is able to stimulate insulin secretion and which has no more than 7 amino acid substitutions or deletions as compared to the native sequence and in which one or more of Lys | 01-22-2015 |
20150025003 | 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. | 01-22-2015 |
20150031606 | Compositions comprising a delivery agent and preparation thereof - The invention relates to granules and pharmaceutical compositions comprising a salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid and a lubricant obtained by mixing hereof for more than 5 minutes prior to granulation as well as processes for their preparation and use thereof in medicine. | 01-29-2015 |
20150045293 | MELANOCORTIN ANALOGS HAVING ENHANCED ACTIVITY AND TRANSPORT - Described herein are melanocortin analogs having enhanced activity and transport. | 02-12-2015 |
20150051141 | Compositions Comprising Glucagon Analogs And Methods Of Making And Using The Same - This invention relates to novel compositions comprising analogs of glucagon, wherein the analog comprises an α-amino acid and at least one β-amino acid. Administration of the compositions may be used for effecting treatment or prevention of a plurality of disease states caused by dysfunctional biochemical or biological pathways, including diabetes and other metabolic disorders. The compositions and methods of this invention are particularly useful to identify novel therapeutic modulators of in-vivo receptor activity with extended half-lives and relevant bioactivity as compared to the naturally translated polypeptides upon which the analogs are derived. | 02-19-2015 |
20150072926 | COMPOSITIONS OF GLP-1 PEPTIDES AND PREPARATION THEREOF - The invention relates to pharmaceutical compositions comprising a first type of granules and a second type of granules, wherein said first type of granules comprises a salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid and no GLP-1 peptide, and wherein said second type of granules comprises a GLP-1 peptide and no salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid, as well as the intermediate granules, processes for the preparation of the granules and compositions, and use thereof in medicine. | 03-12-2015 |
20150080295 | GLUCAGON ANALOGUES - The invention provides materials and methods for promoting weight loss or preventing weight gain, and in the treatment of diabetes, metabolic syndrome and associated disorders. In particular, the invention provides novel 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. | 03-19-2015 |
20150111816 | METHODS AND TREATMENT WITH GLP-1 RECEPTOR AGONISTS - The invention provides methods for treating diabetes or obesity, as well as methods for inducing weight loss, preventing weight gain, or controlling weight in a patient in need thereof. The methods comprise administering to the patient at least one effective dose of a GLP-1 receptor agonist, or a regimen of GLP-1 receptor agonist comprising a plurality of substantially evenly spaced doses. The effective dose or regimen does not induce substantial nausea or appetite suppression in the patient. | 04-23-2015 |
20150111817 | GLUCAGON ANALOGUES - The invention provides materials and methods for the treatment of obesity and excess weight, diabetes, and other associated metabolic disorders. In particular, the invention provides novel 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. | 04-23-2015 |
20150111818 | DEVICES, FORMULATIONS, AND METHODS FOR DELIVERY OF MULTIPLE BENEFICIAL AGENTS - The present invention relates to osmotic delivery devices, formulations, and methods for delivery of two or more beneficial agents. In one aspect, the present invention provides osmotic delivery devices useful for substantially concurrent administration of two or more beneficial agents. In another aspect, the present invention provides beneficial agent formulations for use in the osmotic delivery devices. The formulations include formulations wherein beneficial agents are soluble in the vehicle, suspension formulations comprising particle formulations of one or more beneficial agent, and combinations thereof. Further, methods for treatment of a variety of diseases or conditions using two or more beneficial agents are disclosed, wherein the methods are preferably practiced using the osmotic delivery devices and/or formulations of the invention. | 04-23-2015 |
20150119321 | System and Method of Losing Weight - A unique combination of weight loss modalities that produce 20-40 pounds of weigh loss in a six week treatment period. Treatment includes a meal plan chosen to provide adequate protein and nutrition during dieting and to assist metabolism of toxins created from the release of stored fat, high amounts of fiber to assist in collecting toxins and fat in the elimination system and to encourage peristaltic action in the bowel, a bowel toner to further increase peristaltic action in the bowel, stimulating liver functions of fat and toxins. The weight loss portion of the treatment is limited to six week segments, and added to the plurality of modalities comprising the invention, to further support the body during weight loss. By supporting the body during weight loss, his invention(s) avoids the “plateau” routinely experienced by existing weight loss systems, when the metabolism slows to avoid further damage from ultra-low calories, medications, bariatric surgeries, and other stressful programs. A stabilization period is used to maintain the weight lost, and dramatically reduce the incidence of rebound weight gain. | 04-30-2015 |
20150126439 | PHARMACEUTICAL COMPOSITION - A combination comprising at least a first insulin-like compound and a second insulin-like compound for treating a condition or a disease in a subject in need thereof where administration of insulin would be of benefit to said subject is described. The combination is administered in an amount to achieve a beneficial glycaemic control in said subject as determined by the levels of HbA | 05-07-2015 |
20150126440 | 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 lactam 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, substitution of carboxy terminal amino acids, 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). | 05-07-2015 |
20150148289 | PEGYLATED OXM VARIANTS - A composition which includes oxyntomodulin and polyethylene glycol polymer (PEG polymer) linked via a reversible linker such as 9-fluorenylmethoxycarbonyl (Fmoc) or 2-sulfo-9-fluorenylmethoxycarbonyl (FMS) is disclosed. Pharmaceutical compositions comprising the reverse pegylated oxyntomodulin and methods of using same are also disclosed. | 05-28-2015 |
20150290334 | PEPTIDE PHARMACEUTICALS FOR INSULIN RESISTANCE - Described herein are methods of syntheses and therapeutic uses of covalently modified peptides and/or proteins. The covalently modified peptides and/or proteins allow for improved pharmaceutical properties of peptide and protein-based therapeutics. | 10-15-2015 |
20150291679 | NOVEL OXYNTOMODULIN DERIVATIVES AND PHARMACEUTICAL COMPOSITION FOR TREATING OBESITY COMPRISING THE SAME - The present invention relates to a novel peptide showing more excellent activities on a glucagon like peptide-1 receptor and a glucagon receptor than native oxyntomodulin, and a composition for the prevention or treatment of obesity comprising the peptide as an active ingredient. Unlike native oxyntomodulin, the novel peptide of the present invention reduces food intake, suppresses gastric emptying, and facilitates lipolysis with reduced side-effects, and also shows excellent receptor-activating effects. Thus, it can be widely used in the treatment of obesity with safety and efficacy. | 10-15-2015 |
20150306181 | DELIVERY OF BIOTHERAPEUTICS TO THE BRAIN - Compositions and methods for delivering therapeutic compounds to the brain are provided. | 10-29-2015 |
20150307579 | Glucagon/GLP-1 Agonists For The Treatment Of Obesity - This disclosure provides GLP-1/glue agon agonist peptides for the treatment of metabolic diseases, e.g., obesity. | 10-29-2015 |
20150322130 | GIP-BASED MIXED AGONISTS FOR TREATMENT OF METABOLIC DISORDERS AND OBESITY - Glucagon peptides that exhibit GIP agonist activity in addition to glucagon and/or GLP-1 activity are provided. Pharmaceutical compositions comprising such glucagon peptides and therapeutic methods of using such peptides are also provided. | 11-12-2015 |
20150366983 | MODIFIED CANINE LEPTIN POLYPEPTIDES - Modified canine leptin polypeptides and formulations and uses thereof, are provided including polyethylene glycol (PEG) modified canine leptin polypeptides, wherein the PEG moiety is covalently attached to a para-acetyl-phenylalanine (pAF) residue of the polypeptide, and related compositions and methods useful in treating companion animal obesity and other leptin-related disorders. | 12-24-2015 |
20150368311 | Exendin-4 Derivatives as Selective Glucagon Receptor Agonists - The present invention relates to glucagon receptor agonists and their medical use, for example in the treatment of severe hypoglycemia. | 12-24-2015 |
20150368313 | Novel Glucagon Analogues - The present invention relates to novel glucagon peptides with improved stability and solubility at neutral pH, 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 glucagon peptides 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. | 12-24-2015 |
20150374792 | COMPOSITIONS AND METHODS FOR TREATING COGNITIVE DEFICITS - A method of treating or preventing cognitive impairment deficits in subjects with age-associated cognitive decline or a dementing illness includes administering to the subject a therapeutically effective amount of amylin, an amylin agonist, or an amylin derivative to treat the cognitive impairment or deficit. | 12-31-2015 |
20150376256 | GLUCAGON/GLP-1 RECEPTOR CO-AGONISTS - Provided herein are peptides and variant peptides that exhibit enhanced activity at the GLP-1 receptor, as compared to native glucagon. | 12-31-2015 |
20150376257 | GLUCAGON ANALOGUES - The invention provides materials and methods for promoting weight loss or preventing weight gain and for treating diabetes and associated metabolic disorders. In particular, the invention provides novel glucagon analogue peptide compounds effective in such methods. The compounds may mediate their effect by having, for example, increased selectivity for the GLP-1 receptor compared to human glucagon. | 12-31-2015 |
20160002311 | Novel Glucagon Analogues - 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. | 01-07-2016 |
20160017016 | PEGYLATED GLUCAGON AND GLP-1 CO-AGONISTS FOR THE TREATMENT OF OBESITY - This disclosure provides pegylated GLP-1/glucagon agonist peptides for the treatment of metabolic diseases, e.g., obesity. | 01-21-2016 |
20160051628 | METHODS OF TREATING FGF21-ASSOCIATED DISORDERS - The invention relates to the identification of new polypeptide and protein variants of fibroblast growth factor 21 (FGF21) that have improved pharmaceutical properties. Also disclosed are methods for treating FGF21-associated disorders, including metabolic conditions. | 02-25-2016 |
20160051688 | GLUCAGON SUPERFAMILY PEPTIDES EXHIBITING G PROTEIN-COUPLED RECEPTOR ACTIVITY - Provided herein are glucagon superfamily peptides conjugated with GPCR ligands that are capable of acting at a G protein-coupled receptor. Also provided herein are pharmaceutical compositions and kits of the conjugates of the invention. Further provided herein are methods of treating a disease, e.g., a metabolic disorder, such as diabetes and obesity, comprising administering the conjugates of the invention. | 02-25-2016 |
20160052988 | PEPTIDE COMPOUND - The present invention provides a novel peptide compound having an activating action on GLP-1 receptors and GIP receptors and use of the peptide compound as a medicament. Specifically, a peptide containing a partial sequence represented by the formula (I) or a salt thereof and a medicament comprising the same are provided. P | 02-25-2016 |
20160052989 | GIP RECEPTOR-ACTIVE GLUCAGON COMPOUNDS - Glucagon peptides with increased GIP activity are provided, optionally with GLP-1 and/or glucagon activity. In some embodiments, C-terminally extended glucagon peptides comprising an amino acid sequence substantially similar to native glucagon are provided herein. | 02-25-2016 |
20160067184 | Oral Dosing of GLP-1 Compounds - The present invention relates to improved uses of GLP-1 peptides in oral therapy. | 03-10-2016 |
20160083446 | HIGHLY SOLUBLE LEPTINS - The disclosure provides chimeric polypeptides and nucleic acid molecules encoding chimeric polypeptides. Also provided are pharmaceutical compositions and methods of treatment for diseases and disorders including lipodystrophy, dyslipidemia, hyperlipidemia, overweight, obesity, hypothalamic amenorrhea, Alzheimer's disease, leptin deficiency, fatty liver disease or diabetes (including type I and type II). Additional diseases and disorders which can be treated by the compounds and methods described herein include nonalcoholic steatohepatitis (NASH) and nonalcoholic fatty liver disease (NAFLD), metabolic syndrome X and Huntington's Disease. | 03-24-2016 |
20160095905 | Compositions and Methods for Induced Brown Fat Differentiation - The invention provides methods and compositions for inducing brown fat cell differentiation through modulation of both Prdm1β and C/EBPβ activity and/or expression. Also provided are methods for preventing or treating obesity or an obesity related disorder in a subject through stimulation of both Prdm1β and C/EBPβ expression and/or activity. Further provided are methods for identifying compounds that are capable of modulating both Prdm1β and C/EBPβ expression and/or activity. | 04-07-2016 |
20160102129 | Stable GLP-1 Based GLP-1/Glucagon Receptor Co-Agonists - New GLP-1 derivatives, compositions thereof and their use in medicine. | 04-14-2016 |
20160108102 | Novel GLP-1 Derivatives - Novel polypeptide derivatives having protracted profile of action. | 04-21-2016 |
20160115215 | Glucagon Analogs Exhibiting GIP Receptor Activity - Provided herein are glucagon analogs which exhibit potent activity at the GIP receptor, and, as such are contemplated for use in treating diabetes and obesity. In exemplary embodiments, the glucagon analog of the present disclosures exhibit an EC50 at the GIP receptor which is within the nanomolar or picomolar range. | 04-28-2016 |
20160128985 | Methods and Compositions for the Treatment of Body Weight Related Disorders - The present invention relates to methods for reducing body weight in an animal in need thereof via administration of a therapeutically effective amount of a compound having a general tripartite structure A-B-C. In the tripartite structure A, B, and C are identical or non-identical structures, for example, but not limited to, heterocyclic, phenyl or benzyl ring structures with or without substitutions and are described in detail herein. The methods may utilize particular compounds, for example, having a piperidinyl, a pyrrolinyl or pyridinyl A ring, a thiazole B ring, and a phenyl C ring which may be further substituted independently. Also provided are methods for increasing thermogenesis without reducing lean body mass during weight loss in an animal by administering of a therapeutically effective amount of the compounds described. | 05-12-2016 |
20160137709 | ENGINEERED POLYPEPTIDES HAVING ENHANCED DURATION OF ACTION - Compounds are provided having inter alia good duration of action, high potency and/or convenient dosing regimens including once weekly administration. The compounds are engineered polypeptides which incorporate an albumin binding domain in combination with one or more biologically active polypeptides. Also provided are pharmaceutical compositions and methods of treatment for diseases and disorders including lipodystrophy, dyslipidemia, hyperlipidemia, overweight, obesity, hypothalamic amenorrhea, Alzheimer's disease, leptin deficiency, fatty liver disease or diabetes (including type I and type II). Additional diseases and disorders which can be treated by the compounds and methods described herein include nonalcoholic steatohepatitis (NASH) and nonalcoholic fatty liver disease (NAFLD), metabolic syndrome X and Huntington's Disease. | 05-19-2016 |
20160137710 | PEPTIDOMIMETIC MACROCYCLES - The present invention provides peptidomimetic macrocycles capable of modulating growth hormone levels and methods of using such macrocycles for the treatment of disease. | 05-19-2016 |
20160151459 | THERAPEUTIC METHOD OF TREATING METABOLIC DISORDERS | 06-02-2016 |
20160184401 | NON-AGGLOMERATING BIOCONJUGATES OF AMYLIN AND AMYLIN-MIMETIC COMPOUNDS, COMPOSITIONS COMPRISING THE SAME, AND MAKING AND USE THEREOF - The present disclosure concerns new non-agglomerating bioconjugates of amylin, amylin-mimetic compounds, and combinations comprising the same. Methodology of making and using are provided herein. In some embodiments, an instant non-agglomerating amylin bioconjugate can be used for treating a disease associated with a lack of natural production of amylin and/or deposition or accumulation of extracellular amyloid fibers, which contribute to the dysfunction or failure of systemic organs such as the pancreas or the brain. | 06-30-2016 |
20160375039 | COMPOUNDS FOR THE TREATMENT OF OBESITY AND METHODS OF USE THEREOF - Weight loss agents include compounds defined by Formula I or a pharmaceutically acceptable salt or prodrug thereof, compositions containing the same, and methods of use thereof are described herein. In some embodiments, the compound is Withaferin A. In other embodiments, the compound is Michael addition product of Withaferin A. The compounds can be administered to induce weight loss in a pre-obese, obese, or morbidly obese patient, reduce body fat in a pre-obese, obese, or morbidly obese patient, reduce food intake in a pre-obese, obese, or morbidly obese patient, improve glucose homeostasis in a pre-obese, obese, or morbidly obese patient, or combinations thereof. | 12-29-2016 |
20190142747 | Pharmaceutical Composition Comprising a GLP-1-Agonist and Methionine | 05-16-2019 |
20190142906 | INSULIN RECEPTOR PARTIAL AGONISTS AND GLP-1 ANALOGUES | 05-16-2019 |