165 results about "Ghrelin" patented technology

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 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:

wherein 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.

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.

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.

Weight loss can be promoted by introducing a microcatheter into the mid segment or distal portion of a human subject's left gastric artery and delivering, via the microcatheter, a plurality of particles with sizes between 300 and 500 μm into the distal portion of the subject's left gastric artery. The particles cause endovascular flow reduction or interruption in the distal portion of the subject's left gastric artery. The reduced or interrupted blood flow decreases the production of the hormone ghrelin, which reduces the subject's appetite, thereby promoting weight loss.