166 results about "Ghrelin" patented technology

The present invention is related to a nucleic acid, preferably binding to ghrelin, whereby the nucleic acid comprises a first stretch Box A, and a second stretch Box B, whereby the first stretch Box A comprises about 25 consecutive nucleotides, the second stretch Box B comprises about six to eight consecutive nucleotides, whereby a 3′-terminal stretch of nucleotides of the first stretch Box A hybridises with the second stretch Box B, whereby upon hybridisation a first double-stranded structure is formed, whereby such first double-stranded structure comprises a bulge.

A method is provided for detecting a change in posture of a subject. An electrical impedance is measured between two or more sites on a stomach (20) of the subject, and an impedance signal is generated responsive thereto. The change in posture is detected by performing a posture analysis of the impedance signal. A method is also provided for treating a subject. The method includes applying an electrical signal to a site of the subject selected from the list consisting of: a colon (402) of the subject, and a distal small intestine (408) of the subject. The signal is configured to stimulate cells of the subject to increase secretion of glucagon-like-peptide-1 (GLP-1) or PYY, or to decrease secretion of ghrelin, in order to treat the subject.

A satiation device is described which includes a sheath or liner extending from the proximal or middle stomach to the distal antrum. Food ingested by the patient passes through the sheath or liner, thereby minimizing contact between the ingested food and the stomach. It is believed that over time, reduced contact between food and the stomach will result in decreased Ghrelin production by the patient and a consequent decrease in appetite. In some embodiments, the satiation device may also include a proximal pouch and / or a distal bypass tube.

The present invention is related to compounds of formula (I), or a therapeutically suitable salt or prodrug thereof, the preparation of the compounds, compositions containing the compounds and the use of the compounds in the prevention or treatment of disorders regulated by ghrelin including anorexia, cancer cachexia, eating disorders, age-related decline in body composition, weight gain, obesity, and diabetes mellitus.

The present invention provides a peptide-type compound which induces secretion of growth hormone and which has the activity of increasing the intracellular calcium ion concentration, wherein at least one amino acid is replaced by a modified amino acid and / or a non-amino acid compound, or a pharmaceutically acceptable salt thereof.

The invention comprises peptidyl analogs of ghrelin having greater stability which are active at the GHS receptor according to formulae depicted below:(R2)-A1-A2-A3-A4-A5-A6-A7-A8-A9-A10-A11-A12-A13-A14-A15-A16-A17-A18-A19-A20-A21-A22-A23-A24-A25-A26-A27-A28-R1 wherein the definitions of A1 to A28, R1 and R2 are provided for in the specification, with the exception that the N-terminal amino acid must be selected from the group consisting of Inp, 1-Apc and 4-Apc, the pharmaceutically acceptable salts thereof and pharmaceutical compositions comprising an effective amount of said compound together with therapeutic and non-therapeutic uses thereof.

The present invention is related to compounds of formula (I), or a therapeutically suitable salt or prodrug thereof, the preparation of the compounds, compositions containing the compounds and the use of the compounds in the prevention or treatment of disorders regulated by the action of ghrelin receptor, including Prader-Willi syndrome, eating disorder, weight gain, weight-loss maintainance following diet and exercise, obesity, and disorders associated with obesity such as noninsulin dependent diabetes mellitus.

The present invention relates, in one aspect, to the use of a secretagogue compound for the preparation of a medicament for the prophylaxis or treatment of cancer cachexia in an individual in need of such treatment. In another aspect, the present invention relates to the use of a ghrelin-like compound for the preparation of a medicament for prophylaxis or treatment of cachexia in an individual by administering a subcutaneous dosage of said medicament to the individual. In a further aspect, the present invention relates to the use of a ghrelin-like compound or a pharmaceutically acceptable salt thereof for the preparation of a medicament for stimulation of appetite in an individual by administering a subcutaneous dosage of said medicament to the individual. Furthermore, the present invention relates to a number of new ghrelin-like compounds and uses thereof, as well as to pharmaceutical compositions and medical packaging comprising the new ghrelin-like compounds.

The present invention relates to the use of a growth hormone (GH) secretagogue, such as a ghrelin-like compound, for the preparation of a medicament for the prophylaxis or treatment of ghrelin deficiency, and / or undesirable symptoms associated therewith, in an individual at risk of acquiring partial or complete ghrelin deficiency resulting from a medical treatment and / or from a pathological condition. The present invention also relates to use of a secretagogue compound for the preparation of a medicament for the prophylaxis or treatment of one or more of: loss of fat mass, loss of lean body mass, weight loss, cachexia, loss of appetite, immunological dysfunction, malnutrition, disrupted sleep pattern, sleepiness, reduction in intestinal absorption and / or intestinal mobility problems in an individual suffering from, or at risk of suffering from, ghrelin deficiency. Furthermore, the present invention relates to the use of a secretagogue, such as a ghrelin-like compound, for the production of a medicament for preventing weight increase in an individual either: a) being converted from a hyperthyroidic state to euthyroid state, or b) in remission from being converted from a hyperthyroidic state to euthyroid state.

Provided herein are methods of modulating hormone concentrations in a subject comprising the administration of a composition comprising a chemosensory receptor ligand, wherein the composition is adapted to deliver the ligand to one or more regions of the intestine of said subject. Also provided are methods directed to the modulation of circulating concentrations of one or more of GLP-1 (total), GLP-1 (active), GLP-2, oxyntomodulin, PYY (total), PYY 3-36, CCK, GIP, insulin, C-peptide, glycentin, uroguanylin amylin, and ghrelin (total), ghrelin (active) and glucagon.

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 loss of body weight and body fat, prophylaxis or treatment of cachexia, stimulation of appetite, stimulation of food intake, stimulation of weight gain, or increasing body fat mass, or increasing body lean mass. Another aspect relates to the use of a ghrelin splice variant-like compound for the preparation of a medicament for the prophylaxis or treatment of cancer cachexia in an individual in need of such treatment. Another aspect relates to the use of a ghrelin splice variant-like compound for the preparation of a medicament for prophylaxis or treatment of cachexia in an individual by administering a subcutaneous dosage of said medicament to the individual. A further aspect relates to the use of a ghrelin splice variant-like compound or a pharmaceutically acceptable salt thereof for the preparation of a medicament for stimulation of appetite in an individual by administering a subcutaneous dosage of said medicament to the individual. A further aspect relates to a number of new ghrelin splice variant-like compounds and uses thereof, as well as to pharmaceutical compositions and medical packaging comprising the new ghrelin splice variant-like compounds.

The present invention provides a method of stimulating the motility of the gastrointestinal system in a subject in need thereof, wherein the subject suffers from maladies (i.e., disorders, diseases, conditions, or drug- or surgery-induced dysfunction) of the gastrointestinal system, by administering to the subject a ghrelin mimetic, or pharmaceutically acceptable salt thereof. The invention also provides a method of treating a gastrointestinal malady by co-administering a ghrelin mimetic with a laxative, a H2 receptor antagonist, a serotonin receptor agonist, pure or mixed, an antacid, an opioid antagonist, a proton pump inhibitor, a motilin receptor agonist, dopamine antagonist, a cholinergic agonist, a cholinesterase inhibitor, somatostatin, octreotide, or any combination thereof.

The present invention is related to compounds of formula (I), or a therapeutically suitable salt or prodrug thereof, the preparation of the compounds, compositions containing the compounds and the use of the compounds in the prevention or treatment of disorders regulated by ghrelin including anorexia, cancer cachexia, eating disorders, age-related decline in body composition, weight gain, obesity, and diabetes mellitus.

The invention provides binding agents and assays for ghrelin signal peptide. The agents and assays are useful in methods for predicting, diagnosing, assessing or monitoring acute cardiac disorders, glucose handling disorders and diabetes in a subject. Also provided are nucleotides, polypeptides, and kits useful in the methods of the invention.

The invention comprises peptidyl analogs according to formulae (I) or (II) as depicted below:(R2R3)-A1-A2-A3-A4-A5-A6-A7-A8-A9-A10-A11-A12-A13-A14-A15-A16-A17-A18-A19-A20-A21-A22-A23-A24-A25-A-26-A27-A28-R1wherein the definitions of A1 to A28 and R1 to R3 are provided for in the specification for each of formulae (I) and (II), pharmaceutically acceptable salts thereof and pharmaceutical compositions comprising an effective amount of a compound of formula (I), that possess agonist or antagonist ghrelin activity, along with therapeutic and non-therapeutic uses thereof.

A method of treating neurodegeneration of substantia nigra pars compacta (SNpc) dopamine neurons and compositions therefor are provided.

Compounds of the invention act as inverse agonist ghrelin receptors. Some of the compounds of the invention may have both inverse agonistic and antagonistic properties as they both decrease or eliminate the constitutive activity of he ghrelin receptor and block the effect of ghrelin. Other preferred compounds of the invention have inverse agonistic properties but have little or no antagonistic activity. The compounds are suitable for medical and / or cosmetic use in connection with modulation of feeding behaviors, body composition and reduction of body mass. The invention also relates to methods for identifying inverse agonists for the ghrelin receptor and for monitoring the further development of such compounds.

The present invention relates to a method comprising administering to a patient diagnosed as being in need of treatment for nausea, emesis, or symptoms associated therewith comprising administering to a patient in need thereof a compound of formula (I) wherein: R1 is C6H5CH2OCH2—, C6H5(CH2)3— or indol-3-ylmethyl; Y is pyrrolidinyl, 4-methyl-piperidinyl or NR2R2; R2 are each independently C1-C6 alkyl; R3 is 2-napthyl or phenyl para-substituted by W; W is H, F, CF3, C1-C6 alkoxy or phenyl; and R4 is H or CH3; or a pharmaceutically acceptable salt or solvate thereof, in an amount that is effective in treating nausea, emesis, or symptoms associated therewith in said patient.

Novel spatially-defined macrocyclic compounds incorporating peptide bond surrogates are disclosed. Libraries of these macrocycles are then used to select one or more macrocycle species that exhibit a specific interaction with a particular biological target. In particular, compounds according to the invention are disclosed as agonists or antagonists of a mammalian motilin receptor and a mammalian ghrelin receptor.

The present invention provides ordered and repetitive antigen arrays comprising, inter alia, compositions comprising a virus-like particle (VLP) to which is linked at least one antigen, wherein said antigen is grehlin or peptides or fragments thereof. The invention also provides methods for producing the aforesaid compositions. The compositions and methods of the invention are useful in the production of vaccines and to efficiently induce self-specific immune responses, in particular antibody responses. The invention also provides for compositions and methods for the prevention and / or treatment of ghrelin-related conditions, disorders or diseases. For example, the compositions of the invention are useful in the production of vaccines for the prevention or treatment of obesity and other disease associated with increased food-uptake or increased body weight.

The invention features immunoconjugates for impeding weight gain and treating obesity in a subject. The immuno-conjugates comprise particular ghrelin polypeptides and a suitable carrier moiety.

Monoclonal antibodies and antigen-binding portions thereof that preferentially bind acetylated human ghrelin with respect to unacylated human ghrelin are disclosed. These molecules have high affinity for acylated human ghrelin, a slow off rate for acylated human ghrelin dissociation, and neutralize an acylated human ghrelin activity. These antibodies or antigen-binding portions thereof are useful for neutralizing ghrelin activity, e.g., in a human subject suffering from a disorder in which ghrelin activity is detrimental.

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, [Aib2, Glu3(NH-hexyl)]hGhrelin(1-28)-NH2 (SEQ ID NO:2) or other suitable ghrelin agonist, to counteract the catabolic effects of said dexamethasone and other natured glucocorticoids.

Disclosed is a method for refolding a protein or peptide that does not contain essential disulfides and that contains at least one free cysteine residue. Also disclosed are polymer IFN-γ conjugates that have been created by the chemical coupling of polymers such as polyethylene glycol moieties to IFN-γ, particularly via a free cysteine in the protein. Also disclosed are analogs of bioactive peptides that may be used to create longer acting versions of the peptides, including analogs of glucagon, glucagon-like peptide-1 (GLP-1), GLP-2, Gastric inhibitory peptide (GIP), PYY, exendin, ghrelin, gastrin, amylin, and oxyntomodulin.