43 results about "Growth hormone secretagogue receptor" patented technology

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.

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.

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.

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.

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.

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).

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.

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.

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.

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).

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.

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.

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 6 μmol / mL.