43 results about "Melanocortin 1 receptor" patented technology

A compound of general formula (1) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11 and R12 are H or methyl, R13, R14, R15 and R16 are H or alkyl, wherein L1 and L2 are linkers selected from single bond, methyl, ethyl, wherein R19, R20 and R21 are H or —CH₂X, NT is selected from H, hydroxyl, alkyl, aminoacid, aminoacid analogue, polypeptide and functional group, CT is selected from hydrogen, hydroxyl, alkyl, aminoacid, aminoacid analogue, polypeptide and functional group shows high selectivity and high affinity for MC1-receptors in combination with effective stimulation or inhibiton of cAMP formation in MC1-receptor expressing cells but low affinity for other subtypes of MC-receptors and may be used to treat a wide range of inflammatory conditions. Also disclosed is a DNA molecule and a corresponding vector encoding the compound, a fusion protein comprising a copy of it, a vector comprising DNA encoding the fusion protein, and a pharmaceutical composition comprising the compound.

A melanocortin receptor agonist cyclic peptide of the formula

where R, x and y are as defined in the specification, compositions and formulations including the peptide of the foregoing formula, and methods of preventing, ameliorating or treating melanocortin receptor-mediated diseases, indications, conditions and syndromes, including sexual dysfunction such as male erectile dysfunction and female sexual dysfunction.

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.

A method for inducing melanogenesis in a human subject having a melanocortin 1 receptor (MC1R) variant allele associated with loss of or diminished receptor function comprises administering to said subject an amount of an α-melanocyte stimulating hormone (α-MSH) analogue effective to induce melanogenesis by the melanocytes in the skin or other epidermal tissue of the subject.

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

The present invention relates to novel chimeric peptides and templates containing a combination of antagonist and agonist endogenous ligand residues. In particular, the present invention relates to novel chimeric peptides and templates thereof based upon melanocortin agonist peptides and agouti related protein (AGRP). The present invention provides multifunctional chimeric peptides having specific bioactivity at melanocortin receptors and their use as drugs to treat various diseases and conditions.

Provided are methods for selecting melanocortin receptor-specific compounds for attenuating food intake and for treatment of specific disease conditions, including treatment of obesity and related energy homeostasis or feeding disorders characterized by excess weight gain, without inducing a sexual response, and methods for selecting compounds for treatment of sexual dysfunction. Further provided are pharmaceutical preparations defined by such methods, and methods and preparations for attenuating food intake and treatment of said conditions.

A MC1R peptide ligand-elastic vesicle complex for preventing skin maladies. The MC1R peptide ligand is modified by coupling the melanocortin 1 receptor (MC1R) ligand to a functionality or linker, such as a click functionality, for conjugation to a surface or agent. The modified MC1R peptide ligand can be coupled, e.g., via a click reaction with a complementary click functionality attached, to a moiety to form an MC1R-targeted agent. Drugs, contrast agents, polymers, particles, micelles, elastic vesicles, surfaces of larger structures, or other moieties can be targeted to the MC1R. The MC1R peptide ligand-elastic vesicle complex is prepared as a patch or viscous emulsion that can be applied to human skin.

Linear peptides with a C-terminus —OH group that are specific for one or more melanocortin receptors, and which may be used in the treatment of melanocortin receptor-mediated disorders, including a variety of body weight disorders including cachexia, and for treatment of inflammation, immune disorders and other conditions, diseases and syndromes, and pharmaceutical compositions including such linear peptides.

The invention belongs to the technical fields of medicine preparation and applications, and in particular relates to an application of a non-peptide small-molecular compound as an MC4R (melanocortin-4 receptor) agonist and a specific mutant medicine mate thereof. According to the invention, the on-peptide small-molecular compound is discovered for the first time, wherein the on-peptide small-molecular compound is numbered as BMS470539, chemical name of the on-peptide small-molecular compound is 1-[1-(3-methyl-L-histidyl-O-methyl-D-tyrosyl)-4-phenyl-4-piperidyl]-1-butanone; and molecular weight of the compound is 559.697. The compound, as the melanocortin-4 receptor agonist, can function as the medicine mate to promote recovery of some MC4R defective mutants' capacities of generating signal molecules.