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43 results about "Growth hormone secretagogue receptor" patented technology

Growth hormone secretagogue receptor(GHS-R), also known as ghrelin receptor, is a G protein-coupled receptor that binds growth hormone secretagogues (GHSs), such as ghrelin, the "hunger hormone". The role of GHS-R is thought to be in regulating energy homeostasis and body weight. In the brain, they are most highly expressed in the hypothalamus, specifically the ventromedial nucleus and arcuate nucleus. GSH-Rs are also expressed in other areas of the brain, including the ventral tegmental area, hippocampus, and substantia nigra. Outside the central nervous system, too, GSH-Rs are also found in the liver, in skeletal muscle, and even in the heart.

Macrocyclic ghrelin receptor modulators and methods of using the same

ActiveUS20080194672A1Reduced and dysfunctional gastrointestinal motilityInhibit gastrointestinal motilityAntibacterial agentsOrganic active ingredientsSomatotropic hormonePharmaceutical Substances
The present invention provides novel conformationally-defined macrocyclic compounds that can function as selective modulators of the ghrelin receptor (growth hormone secretagogue receptor, GHS-R1a and subtypes, isoforms and variants thereof). Methods of synthesizing the novel compounds are also described herein. These compounds are useful as agonists of the ghrelin receptor and as medicaments for treatment and prevention of a range of medical conditions including, but not limited to, metabolic and / or endocrine disorders, gastrointestinal disorders, cardiovascular disorders, obesity and obesity-associated disorders, central nervous system disorders, bone disorders, genetic disorders, hyperproliferative disorders and inflammatory disorders.
Owner:OCERA THERAPEUTICS INC

Novel triazole derivatives as ghrelin analogue ligands of growth hormone secretagogue receptors

The present invention provides novel triazole derivatives as ghrelin analogue ligands of growth hormone secretagogue receptors according to formula (I) that are useful in the treatment or prophylaxis of physiological and / or pathophysiological conditions in mammals, preferably humans, that are mediated by GHS receptors. The present invention further provides GHS receptor antagonists and agonists that can be used for modulation of these receptors and are useful for treating above conditions, in particular growth retardation, cachexia, short-, medium- and / or long term regulation of energy balance; short-, medium- and / or long term regulation (stimulation and / or inhibition) of food intake; adipogenesis, adiposity and / or obesity; body weight gain and / or reduction; diabetes, diabetes type I, diabetes type II, tumor cell proliferation; inflammation, inflammatory effects, gastric postoperative ileus, postoperative ileus and / or gastrectomy (ghrelin replacement therapy).
Owner:ZENTARIS GMBH +3

Macrocyclic Ghrelin Receptor Antagonists and Inverse Agonists and Methods of Using the Same

InactiveUS20110105389A1Nervous disorderAntipyreticGrowth hormone-releasing peptideReceptor antagonist
The present invention provides novel conformationally-defined macrocyclic compounds that have been demonstrated to be selective modulators of the ghrelin receptor (GRLN, growth hormone secretagogue receptor, GHS-R1a and subtypes, isoforms and / or variants thereof). Methods of synthesizing the novel compounds are also described herein. These compounds are useful as antagonists or inverse agonists of the ghrelin receptor and as medicaments for treatment and prevention of a range of medical conditions including, but not limited to, metabolic and / or endocrine disorders, obesity and obesity-associated disorders, appetite or eating disorders, addictive disorders, cardiovascular disorders, gastrointestinal disorders, genetic disorders, hyperproliferative disorders, central nervous system disorders and inflammatory disorders.
Owner:OCERA THERAPEUTICS INC

Growth Hormone Secretagogue Receptor 1A Ligands

InactiveUS20080300180A1Good curative effectImprove the anchorage of the GHS-R1A ligandDipeptide ingredientsMetabolism disorderGrowth hormoneGH Receptor
The present invention relates to new growth hormone secretagogue receptor 1A (GHS-R 1A) ligands, and pharmaceutical compositions comprising any of the new GHS-R1 A ligands. The ligands are suitable for a wide range of applications, and thus the present invention also relates to use of the GHS-R1 A ligands according to the present invention in the manufacture of a medicament for the treatment of an individual in need thereof. In another aspect, the present invention relates to a method of treatment of an individual in need thereof, comprising administering to said individual one or more of the GHS-R1A ligands disclosed herein, such as e.g. for treatment of cancer cachexia.
Owner:GASTROTECH PHARMA AS

Methods of using macrocyclic agonists of the ghrelin receptor for treatment of gastrointestinal motility disorders

The present invention provides novel conformationally-defined macrocyclic compounds that have been demonstrated to be selective agonists of the ghrelin receptor (growth hormone secretagogue receptor, GHS-R1a and subtypes, isoforms and variants thereof). Such compounds are useful as medicaments for treatment and prevention of a range of medical conditions characterized by disturbed gastrointestinal motility including, but not limited to, post-surgical gastroparesis and post-operative ileus in combination with opioid-induced bowel dysfunction. These agents are effective for multiple disorders at dose levels equivalent to those required to treat a single disorder.
Owner:OCERA THERAPEUTICS INC

Macrocyclic Modulators of the Ghrelin Receptor

The present invention provides novel conformationally-defined macrocyclic compounds that have been demonstrated to be selective modulators of the ghrelin receptor (growth hormone secretagogue receptor, GHS-R1a and subtypes, isoforms and variants thereof). Methods of synthesizing the novel compounds are also described herein. These compounds are useful as agonists of the ghrelin receptor and as medicaments for treatment and prevention of a range of medical conditions including, but not limited to, metabolic and / or endocrine disorders, gastrointestinal disorders, cardiovascular disorders, obesity and obesity-associated disorders, central nervous system disorders, genetic disorders, hyperproliferative disorders and inflammatory disorders.
Owner:OCERA THERAPEUTICS INC

Methods of using macrocyclic modulators of the ghrelin receptor

InactiveUSRE42624E1Hormone peptidesDepsipeptidesGrowth hormone-releasing peptideInflammation
The present invention provides novel conformationally-defined macrocyclic compounds that have been demonstrated to be selective modulators of the ghrelin receptor (growth hormone secretagogue receptor, GHS-R1a and subtypes, isoforms and variants thereof). Methods of synthesizing the novel compounds are also described herein. These compounds are useful as agonists of the ghrelin receptor and as medicaments for treatment and prevention of a range of medical conditions including, but not limited to, metabolic and / or endocrine disorders, gastrointestinal disorders, cardiovascular disorders, obesity and obesity-associated disorders, central nervous system disorders, genetic disorders, hyperproliferative disorders and inflammatory disorders.
Owner:OCERA THERAPEUTICS INC

Novel triazole derivatives with improved receptor activity and bioavailability properties as ghrelin antagonists of growth hormone secretagogue receptors

ActiveUS20120083494A1Improved receptor antagonistic activityGood metabolic stabilityBiocideNervous disorderAdipogenesisTriazole derivatives
The present invention provides novel triazole derivatives with improved receptor activity and bioavailability properties as ghrelin analogue ligands of growth hormone secretagogue receptors according to formula (I) that are useful in the treatment or prophylaxis of physiological and / or pathophysiological conditions in mammals, preferably humans, that are mediated by GHS receptors. The present invention further provides GHS receptor antagonists and agonists that can be used for modulation of these receptors and are useful for treating above conditions, in particular alcohol disorder, drug abuse, growth retardation, cachexia, short-, medium-, and / or long term regulation of energy balance, short-, medium-, and / or long term regulation (stimulation and / or inhibition) of food intake, intake of rewarding food, adipogenesis, adiposity and / or obesity, body weight gain and / or reduction, diabetes, diabetes type I, diabetes type II, tumor cell proliferation, inflammation, inflammatory effects, gastric postoperative ileus, postoperative ileus and / or gastrectomy (ghrelin replacement therapy).
Owner:AETERNA ZENTARIS GMBH +3

Medical compositions containing ghrelin

It is provided a pharmaceutical composition stably containing ghrelin or its derivative, which is an endogenous growth hormone secretagogue (GHS) to a growth hormone secretagogue-receptor (GHS-R), comprising a aqueous solution containing the ghrelins having pH range of 2 to 7, wherein the aqueous solution having pH range of 2 to 7 is a buffer solution, especially, glycine hydrochloride buffer, acetate buffer, citrate buffer, lactate buffer, phosphate buffer, citric acid-phosphate buffer, phosphate-acetate-borate buffer or phthalate buffer, and the concentration of the ghrelins in the solution is from 0.03 nmol / mL to 61 μmol / mL.
Owner:ASUBIO PHARMA +1

Identification and Use of Growth Hormone Secretagogue Receptor Type 1A Antagonists

Compounds that are ligands for the growth hormone secretagogue receptor type 1A (GHS-R 1A), as well as pharmaceutically acceptable salts of such compounds, are useful for the manufacture of medicaments for the regulation of food intake.
Owner:NOVO NORDISK AS

Identification and use of growth hormone secretagogue receptor type 1A antagonists

Compounds that are ligands for the growth hormone secretagogue receptor type 1A (GHS-R 1A), as well as pharmaceutically acceptable salts of such compounds, are useful for the manufacture of medicaments for the regulation of food intake.
Owner:NOVO NORDISK AS

Macrocyclic Ghrelin Receptor Antagonists And Inverse Agonists And Methods Of Using The Same

The present invention provides novel conformationalIy- defined macrocyclic compounds of formula (I) that have been demonstrated to be selective modulators of the ghrelin receptor (GRLN, growth hormone secretagogue receptor, GHS-R1a and subtypes, isoforms and / or variants thereof). Methods of synthesizing the novel compounds are also described herein. These compounds are useful as antagonists or inverse agonists of the ghrelin receptor and as medicaments for treatment and prevention of a range of medical conditions including, but not limited to, metabolic and / or endocrine disorders, obesity and obesity- associated disorders, appetite or eating disorders, addictive disorders, cardiovascular disorders, gastrointestinal disorders, genetic disorders, hyperproliferative disorders, central nervous system disorders and inflammatory disorders.
Owner:OCERA THERAPEUTICS INC

Remedy for diabetes

The invention relates to a prophylactic or therapeutic for diabetes mellitus which comprises a growth-hormone secretagogue receptor (GHS-R) antagonist as an active ingredient, as well as a method of lowering the blood glucose level by administering a GHS-R antagonist. The invention further relates to a prophylactic or therapeutic which comprises a GHS-R antagonist as an active ingredient, as well as an appetite suppressant which comprises a GHS-R antagonist as an active ingredient.
Owner:CHUGAI PHARMA CO LTD

Ghrelin-containing sheep embryo in-vitro culture solution and culture method thereof

The invention provides a ghrelin-containing sheep embryo in-vitro culture solution. The sheep embryo in-vitro culture solution takes a TCM199 culture solution as a matrix; and the matrix also contains 400-800mg / mL ghrelin, 0.15mg / mL glutamine, 100IU / mL penicillin, 100mug / mL streptomycin and 5-10mg / mL bovine serum albumin. In the embryo in-vitro culture solution provided by the invention, ghrelin is used as the endogenous ligand of a growth hormone secretagogue receptor, and has the functions of regulating the secretion of reproductive hormone, promoting the growth of ovarian follicle and ovulation, adjusting the ovarian function, participating in the early developmental regulation of embryo and the like. By applying ghrelin to the sheep embryo in-vitro culture, the ectogenesis of the embryo can be effectively promoted, thus the problem of low ectogenesis rate of the sheep early embryo at present is solved. The sheep embryo in-vitro culture solution provided by the invention has relatively low economic cost, and is convenient to popularize and use in production.
Owner:ZHEJIANG UNIV

Preventives or Remedies for Hepatopathy

ActiveUS20070219114A1Preventing and alleviating progressionPromoting hepatocyte proliferationOrganic active ingredientsPeptide/protein ingredientsAdditive ingredientHepatectomy
The present invention relates to a preventive or a therapeutic agent for hepatopathy, comprising, as an effective ingredient, a polypeptide derivative having an activity of binding to growth hormone secretagogue receptor and thus elevating intracellular calcium ion concentration, and having one amino acid sequence selected from the group consisting of amino acid sequences represented by SEQ ID NOS: 1 to 22, or an amino acid sequence in which one to several amino acids are deleted, substituted or added at the amino acid residues other that the first to forth amino acid residues from the amino-terminus in the said amino acid sequence, or a pharmacologically acceptable salt thereof. The preventive or the therapeutic agent for hepatopathy in accordance with the present invention is useful as a drug suitable for treating or preventing hepatic diseases such as hepatitis, liver cirrhosis and hepatic insufficiency. Further, the preventive or the therapeutic agent for hepatopathy in accordance with the present invention is also useful as an agent of promoting hepatic regeneration and hepatic function recovery after hepatectomy.
Owner:KANGAWA KENJI

NMU-GHSR1b/NTSR1 oncogenic signaling pathway as a therapeutic target for lung cancer

The present invention relates to a method of and a kit for assessing the prognosis of lung cancer by detecting the expression level of the neuromedin U (NMU) gene in a patient-derived biological sample. The method and kit are particularly preferred for assessing the prognosis of non-small cell lung cancer (NSCLC). Furthermore, the present invention relates to a method of screening for a therapeutic agent for cancer, in particular, lung cancer, by detecting compounds that inhibit the binding of the NMU protein with the heterodimer of growth hormone secretagogue receptor 1b (GHSR1b) and neurotensin receptor 1 (NTSR1).
Owner:ONCOTHERAPY SCI INC

SPINAL NERVE REPAIR PROMOTING THERAPEUTICS CONTAINING GHRELIN OR ITS DERIVATIVES OR SUBSTANCES THAT ACT ON GHS-R1a AS AN ACTIVE INGREDIENT

The invention provides a spinal neuron damage treating agent for use in the treatment of spinal neuron damage, or an agent for promoting the proliferation of spinal neuronal precursor cells in the culture of spinal neuronal precursor cells, or an agent for promoting the regeneration of spinal nerves after transplantation of cultured spinal neuronal precursor cells, and the like.The invention provides an agent that contains a substance (e.g., ghrelin) that acts on the growth hormone secretagogue-receptor as an active ingredient, the agent being a spinal neuron damage treating agent for use in the treatment of spinal neuron damage, or an agent for promoting the proliferation of cultured spinal neuronal precursor cells in the culture of spinal neuronal precursor cells, or an agent for promoting the regeneration of spinal nerves after transplantation of cultured spinal neuronal precursor cells, and the like.
Owner:UNIVERSITY OF MIYAZAKI +2

Macrocyclic Modulators of the Ghrelin Receptor

The present invention provides novel conformationally-defined macrocyclic compounds that have been demonstrated to be selective modulators of the ghrelin receptor (growth hormone secretagogue receptor, GHS-R1a and subtypes, isoforms and variants thereof). Methods of synthesizing the novel compounds are also described herein. These compounds are useful as agonists of the ghrelin receptor and as medicaments for treatment and prevention of a range of medical conditions including, but not limited to, metabolic and / or endocrine disorders, gastrointestinal disorders, cardiovascular disorders, obesity and obesity-associated disorders, central nervous system disorders, genetic disorders, hyperproliferative disorders and inflammatory disorders.
Owner:OCERA THERAPEUTICS INC

Therapeutic agent for amyotrophic lateral sclerosis

The present invention provides a therapeutic agent for amyotrophic lateral sclerosis comprising a growth hormone secretagogue receptor (GHS-R) agonist or a pharmaceutically acceptable salt thereof as an active ingredient. An object of the present invention is to provide a pharmaceutical product for amyotrophic lateral sclerosis for which no effective drug exists. The therapeutic agent for amyotrophic lateral sclerosis of the present invention comprises a GHS-R agonist typified by ghrelin as an active ingredient and is administered to a recipient individual having amyotrophic lateral sclerosis with non-serious dysphagia. The individual may also be unresponsive or insufficiently responsive to an existing therapeutic agent for ALS.
Owner:DAIICHI SANKYO CO LTD

Polypeptide as agonist of growth hormone secretagogue receptor and use thereof

The invention provides a polypeptide as an agonist of a growth hormone secretagogue receptor (GHSR). The polypeptide has a structure as shown in formula I, or a stereoisomer, a mixture and a pharmaceutically acceptable salt thereof. Experimental results show that the provided polypeptide compound can effectively show relatively high agonistic activity on GHSR-1a, has a novel structure and small toxic and side effects, and has the potential of becoming a clinical candidate compound.
Owner:CHENGDU SINTANOVO BIOTECHNOLOGV CO LTD
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