89 results about "MC4 Receptor" patented technology

Disclosed are compositions for affecting weight loss comprising bupropion and a second compound, where the second compound causes increased agonism of a melanocortin 3 receptor (MC3-R) or a melanocortin 4 receptor (MC4-R) compared to normal physiological conditions, antagonizes cannabinoid receptor activity, or is useful in the treatment of bipolar disorders. Also disclosed are methods of affecting weight loss, increasing energy expenditure, increasing satiety in an individual, or suppressing the appetite of an individual, comprising identifying an individual in need thereof and treating that individual with a combination of bupropion and a compound that enhances α-MSH activity, antagonizes cannabinoid receptor activity, or is useful in the treatment of bipolar disorders.

Disclosed are compositions for affecting weight loss comprising a first compound and a second compound, where the first compound is an opioid antagonist and the second compound causes increased agonism of a melanocortin 3 receptor (MC3-R) or a melanocortin 4 receptor (MC4-R) compared to normal physiological conditions. Also disclosed are methods of affecting weight loss, increasing energy expenditure, increasing satiety in an individual, or suppressing the appetite of an individual, comprising identifying an individual in need thereof and treating that individual to antagonize opioid receptor activity and to enhance α-MSH activity.

Certain novel bicyclic N-acylated piperidine derivatives are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-4R, such as obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.

Small cyclic peptides of the formula X1-X2-X3-X4-X5-X6-X7-R1 comprising 7-12 amino acid residues are provided. Said peptides are MC4 receptor agonists, and thus useful in the treatment of obesity and related diseases.

Methods for selection of compounds for treatment of obesity, compounds selected by the disclosed methods, and methods of treatment of obesity, wherein a selective melanocortin-4 receptor compound is identified, which compound is further characterized in that it attenuates the binding of both an agonist, including alpha-melanocyte stimulating hormone, and an inverse agonist, including agouti-related protein, to a melanocortin receptor, including melanocortin-4 receptor.

Peptides of formulae I, II and III that selectively activate melanocortin-4 (MC-4) receptor activity.

Certain novel N-acylated spiropiperidine derivatives are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-4R, such as obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.

The present invention relates to novel compounds, methods, and formulations useful for the oral delivery of a GLP-1 compound or an MC4 agonist peptide.

A highly selective melanocortin-4 receptor antagonist cyclic hexapeptide of the formula where R1, R2, R3a, R3b, R4, R5, x, y and z are as defined in the specification, and a method of treating body weight disorders, including cachexia, sarcopenia and wasting syndrome or disease, and treating inflammation and immune disorders.

There is provided novel diazepines that function as agonists at the melanocortin 4 receptor and as agonists at the melanocortin 1 receptor, pharmaceutical compositions containing them, methods for their use in treatment, and processes for their preparation.

An arginine derivative represented by the formula: [wherein Ar<1 >and Ar<2 >may be the same or different, and are each a phenyl group, a substituted phenyl group, a naphthyl group, a substituted naphthyl group or a heteroaromatic ring group containing one or more of nitrogen, oxygen and sulfur atoms; Y<1 >is a C1-5 alkylene group, a C2-5 alkenylene group or a single bond; and the C1-5 alkylene group optionally contains a carbon atom substituted with a phenyl group, a substituted phenyl group, a naphthyl group, a substituted naphthyl group or a C1-10 acylamino group; Q is a carbonyl group or a sulfonyl group; Y<2 >is a C1-5 alkylene group; the C1-5 alkylene group optionally contains a carbon atom substituted with a phenyl group, a substituted phenyl group, a naphthyl group, a substituted naphthyl group, a hydroxyl group, a carbamoyl group, a mono-C1-5 alkylamide group or a di-C1-5 alkylamide group], or a pharmaceutically acceptable salt thereof. There are provided peptidergic ligands which have the affinity and specificity to MC4 receptor.

A highly selective melanocortin-4 receptor antagonist cyclic peptide of the formula where R1, R2, R3, R4a, R4b, R5, R6, R7, x, y and z are as defined in the specification, and a method of treating body weight disorders, including cachexia, sarcopenia and wasting syndrome or disease, and treating inflammation and immune disorders.

The present invention relates to methods of treating and preventing obesity and obesity-related disorders in a subject comprising administering a neurokinin-1 antagonist and an anti-obesity agent, such as a melanocortin 4 receptor agonist, to said subject. The present invention further related to methods of treating or preventing sexual dysfunction, including male erectile dysfunction, in a subject comprising administering a neurokinin-1 antagonist and a sexual dysfunction therapeutic agent, such as a melanocortin 4 receptor agonist, to said subject. The present invention further provides for pharmaceutical compositions and medicaments useful in carrying out these methods.

A highly selective melanocortin-4 receptor antagonist cyclic hexapeptide of the formulawhere R1, R2, R3a, R3b, R4, R5, x, y and z are as defined in the specification, and a method of treating body weight disorders, including cachexia, sarcopenia and wasting syndrome or disease, and treating inflammation and immune disorders.

Small cyclic peptides of the formula X1-X2-X3-X4-X5-X6-X7-R1 comprising 7-12 amino acid residues are provided. Said peptides are MC4 receptor agonists, and thus useful in the treatment of obesity and related diseases.

Peptides cyclized via disulfide or lactam bridges are disclosed. The peptides exhibit melanocortin-4 receptor agonist activity and are useful for treating obesity.

A melanocortin-4 receptor agonist cyclic peptide of the formulawhere R1, R2, R3, R4a, R4b, R5, R6, R7a, R7b, x, y and z are as defined in the specification, and a method of treating sexual dysfunction, including male erectile dysfunction and female sexual dysfunction, and other melanocortin 4 receptor responsive conditions and disorders.

The present invention relates to drug screening assays, and diagnostic and therapeutic methods for the treatment of body weight disorders, such as obesity, anorexia and cachexia, utilizing the melanocortin 4-receptor (MC4-R) as the target for intervention. The invention also relates to compounds that modulate the activity or expression of the MC4-R, and the use of such compounds in the treatment of body weight disorders.

People who are on chronic steroids are known to have depressed levels of ACTH and thus should also have decreased levels of α-MSH. Recent data show that people with altered Melanocortin-4 (MC4) receptors (receptor for α-MSH) have strongly associated rates (100%) of Binge Eating Disorder diagnosable of DSM IV criteria. All patients who are on steroids and have low levels of ACTH, and thus low levels of α-MSH, could appear phenotypically identical to those with altered Melanocortin-4 receptors (MC4R). Patients with iatrogenically induced α-MSH deficiencies (including patients on chronic steroid therapy) could be expected to respond to exogenous α-MSH or MC4R agonist supplementation. Exogenous α-MSH or MC4R agonist treatment should also decrease serum leptin levels; therefore, the present invention provides a method of decreasing steroid induced weight gain by employing α-MSH agonists.

The subject invention provides novel peptides for use in treating mammals to control appetite and obesity. Disclosed is a peptide derivative having the formula:X1-Z-Q-arg-trp-NH12wherein: X1 is an acyl group, Z is amino-2-naphthyl-carboxylic acid or histidine, Q is (D)phenylalanine or p-iodo-(D)phenylalanine, or a pharmacologically acceptable salt, complex or derivative thereof, the peptide derivative having melanocortin-4 receptor agonist activity.

Disclosed are novel ligands based on an AGRP template that can rescue endogenous melanocortin agonist and / or antagonist dysfunction at MCR polymorphisms. In particular, the present invention provides novel synthetic ligands based on AGRP templates that can rescue endogenous melanocortin agonist dysfunction at MC4R polymorphisms to treat children and adults with these mutations and increase their quality of life.

Metallopeptides are provided for use in treatment of sexual dysfunction in mammals. The metallopeptides are agonists for at least one of melanocortin-3 or melanocortin-4 receptors. The metallopeptides are conformationally fixed on complexation of a metal ion-binding portion thereof with a metal ion. Also provided are metallopeptides that are antagonists for at least one of melanocortin-3 or melanocortin-4 receptors.

The subject invention provides novel peptides for use in treating mammals to control appetite and obesity. Disclosed is a peptide derivative having the formula: X1-Z-Q-arg-trp-NH2 wherein: X1 is an acyl group, Z is amino-2-naphthyl-carboxylic acid or histidine, Q is (D)phenylalanine or p-iodo-(D)phenylalanine, or a pharmacologically acceptable salt, complex or derivative thereof, the peptide derivative having melanocortin-4 receptor agonist activity.

The invention relates to methods of enhancing normal melanocortin-4 receptor (MC4R) activity, and to enhancing activity of an MC4R having a mutation which affects protein folding and / or processing of the MC4R. The invention provides a method of treating an individual having a condition in which increased activity of an MC4R at the cell surface would be beneficial, for example in obesity, by administering an effective amount of a pharmacological chaperone for the MC4R. The invention provides MC4R pharmacological chaperones which enhance the activity of MC4R. The invention further provides a method of screening to identify pharmacological chaperones which enhance folding of an MC4R in the endoplasmic reticulum (ER), in order to enhance the activity of the MC4R at the cell surface.

The invention relates to a method for breeding lean-type Chinese Huai pigs in a multi-gene pyramiding manner based on growth traits thereof. The method comprises the following operating steps: 1, carrying out DNA (deoxyribonucleic acid) extraction on the genome of the pig; 2, designing primers, more particularly, designing the PCR (polymerase chain reaction) amplification primers according to the gene sequences of insulin-like growth factor-I (IGF-I), pituitary specific transcription factor-I (PIT-I), liver X receptor alpha (LXR alpha) and melanocortin-4 receptor (MC4R); 3, carrying out the PCR; 4, carrying out restriction fragment length polymorphism (RFLP); and 5, carrying out the correlation analysis on the polymorphism and growth traits of genes. According to the analysis, the method can determine that the single growth rate of the pyramided gene with the gene type thereof being AADDGGFF is the highest one; the method can prevent the genes of other offsprings from being isolated after the selective reservation for breeding, thus achieving the optimal effect of the growth traits of the offsprings on the four gene types; and the method can stabilize the inheritance, particularly lead the genes of the growth traits to become homozygous within one generation, thus accelerating the cultivation of the lean-type Chinese Huai pigs.