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44 results about "Melanocortins" patented technology

Peptides derived from pro-opiomelanocortin (POMC) which can stimulate MELANOCYTES or CORTICOTROPHS. Melanocortins include ACTH; ALPHA-MSH; and other peptides such as BETA-MSH and GAMMA-MSH, derived from other fragments of POMC. These peptides act through a variety of MELANOCORTIN RECEPTORS to control different functions including steroidogenesis, energy homeostasis, feeding, and skin pigmentation.

Substituted melanocortin receptor-specific piperazine compounds

Melanocortin receptor-specific compounds of the general formulas and pharmaceutically acceptable salts thereof, where J is a substituted or unsubstituted monocyclic or bicyclic ring structure, L is a linker, W is a heteroatom unit with at least one cationic center, hydrogen bond donor or hydrogen bond acceptor, Q includes a substituted or unsubstituted aromatic carbocyclic ring, R6, R7, y and z are as defined in the specification, and the carbon atom marked with an asterisk can have any stereochemical configuration, and optionally with one or two additional ring substituents as defined, which compounds bind to one or more melanocortin receptors and are optionally an agonist, a partial agonist, an antagonist, an inverse agonist or an antagonist of an inverse agonist, and may be employed for treatment of one or more melanocortin receptor-associated conditions or disorders, and methods for the use of the compounds of the invention.
Owner:PALATIN TECH INC

Methods and reagents for discovering and using mammalian melanocortin receptor agonists and antagonists to modulate feeding behavior in animals

InactiveUS6476187B1Compound screeningApoptosis detectionScreening methodMelanocortin agonist
The present invention provides recombinant expression constructs comprising nucleic acid encoding mammalian melanocortin receptors, and mammalian cells into which said recombinant expression constructs have been introduced that express functional mammalian melanocortin receptors. The invention provides a panel of such transformed mammalian cells expressing melanocortin receptors for screening compounds for receptor agonist and antagonist activity. The invention also provides methods for using such panels of melanocortin receptor-expressing mammalian cells to specifically-detect and identify agonists and antagonists for each melanocortin receptor, as well as patterns of agonist and antagonist activity of said compounds for the class of melanocortin receptors. Such screening methods provide a means for identifying compounds with patterns of melanocortin agonist and antagonist activity which is associated with the capacity to influence or modify metabolism and behavior, particularly feeding behavior.
Owner:OREGON HEALTH & SCI UNIV

Compounds and Methods for Treating Obesity

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.
Owner:PALATIN TECH INC

Peptides with Efficacy in Rescuing Melanocortin-4 Receptor Polymorphic Agonist Signaling

InactiveUS20090176712A1Improved melanocortin receptor stimulationImprove the quality of lifeAntibody mimetics/scaffoldsMetabolism disorderMelanocortin agonistAgonist
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.
Owner:UNIV OF FLORIDA RES FOUNDATION INC

Use of Melanocortins to Treat Dyslipidemia

The present invention relates to peptide ligands of the melanocortin receptors, in particular the melancortin-4 receptor, and as such, are useful in the treatment of dyslipidemia and associated complications such as alcoholic and non-alcoholic fatty liver disease.
Owner:IPSEN PHARMA SAS

Method of treating men with testosterone supplement and 5alpha-reductase inhibitor

InactiveUS20090123571A1Minimizes unpleasantMinimizes potentially dangerous side effectBiocideOrganic active ingredientsDiseaseAviptadil
A method of treating Alzheimer's disease, Parkinson's disease, sexual dysfunction or erectile dysfunction in a man by administration of a 5alpha reductase inhibitor together with a testosterone supplement is described. The method is also concerned with the use of the 5alpha reductase inhibiting compound and the testosterone supplement together with another agent useful for treating erectile dysfunction, including PDE V inhibitors; AGE (advanced glycation end-product) breakers; alpha 1 blockers; alpha 1A antagonists; alpha 2 antagonists; dopamine agonists; dopamine D4 agonists; melanocortin agonists; oxytocin agonists; prostaglandin; radical scavengers; rotamase inhibitors; aviptadil; nitroglycerine; and GPCR agonists for treating male sexual dysfunction or erectile dysfunction.
Owner:MERCK SHARP & DOHME CORP

Substituted melanocortin receptor-specific piperazine compounds

A substituted piperazine compound having the structure I:or the structure IX:or an enantomeric, stereoisomeric or diastereomeric form of the foregoing, and pharmaceutically acceptable salts thereof, where J, L, Q, W, A, R6, R7, z and y are as defined in the specification, and the carbon atoms marked with an asterisk can have any stereochemical configuration, which compounds bind to one or more melanocortin receptors and may be employed in pharmaceutical preparations for treatment of one or more melanocortin receptor-associated conditions or disorders, and methods for the use of the compounds of the invention.
Owner:PALATIN TECH INC

Acylated spiropiperidine derivatives as melanocortin-4 receptor agonists

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.
Owner:MERCK SHARP & DOHME CORP

Adrenocorticotropic hormone analogs and related methods

ACTH analog compounds of the present invention include compounds comprising an ACTH peptide sequence with one or more structural modifications that can have one or more of the following preferred ACTH analog biological functions: (1) reduction of corticosteroid secretion by adrenal membrane in the presence of the ACTH analog compared to unmodified ACTH, (2) reduction of corticosteroid secretion by adrenal membrane in the presence of endogenous ACTH and (3) increased MC-2R binding affinity with reduced activation of the MC-2R receptor compared to unmodified ACTH binding to the MC-2R melanocortin. The ACTH analog compounds of the present invention are therefore useful for treatment or prevention of diseases and disorders related to ACTH, ACTH receptors or corticosteroid secretion, such as premature labor and Cushing's Disease.
Owner:UNIVERSITY OF DENVER +2

Method of treating men with testosterone supplement and 5alpha-reductase inhibitor

A method of treating Alzheimer's disease, Parkinson's disease, sexual dysfunction or erectile dysfunction in a man by administration of a 5alpha reductase inhibitor together with a testosterone supplement is described. The method is also concerned with the use of the 5alpha reductase inhibiting compound and the testosterone supplement together with another agent useful for treating erectile dysfunction, including PDE V inhibitors; AGE (advanced glycation end-product) breakers; alpha 1 blockers; alpha 1A antagonists; alpha 2 antagonists; dopamine agonists; dopamine D4 agonists; melanocortin agonists; oxytocin agonists; prostaglandin; radical scavengers; rotamase inhibitors; aviptadil; nitroglycerine; and GPCR agonists for treating male sexual dysfunction or erectile dysfunction.
Owner:MERCK & CO INC

Biomarkers for breast cancer and methods of use thereof

ActiveUS20170342502A1Microbiological testing/measurementFemale breast cancerSignaling network
Described herein is the use of Agouti Signaling Protein (ASIP), in addition to certain other melanocortin signaling network (MSN) genes, as prognostic and predictive biomarkers for the progression of breast cancer. In particular, the novel biomarkers can be used to determine if a female breast cancer patient is at risk of progressing to metastatic disease and thus also be used to direct treatment of the patient.
Owner:WISCONSIN ALUMNI RES FOUND

Auto-antibodies against the melanocortin-4 receptor

Disclosed are biological markers for obesity and methods for diagnosing and treating obesity and related conditions by detecting and modulating the activity of auto-antibodies against the melanocortin-4 receptor or a portion of the melanocortin-4 receptor. Also disclosed are methods for discovering new therapeutics which modulate the activity of auto-antibodies against the melanocortin-4 receptor or a portion of the melanocortin-4 receptor, in particular which prevent the binding of auto-antibodies against the melanocortin-4 receptor or a portion of the melanocortin-4 receptor.
Owner:UNIVERSITY OF BASEL

Monoclonal antibodies and binding fragments thereof directed to the melanocortin-4 receptor and their use in the treatment of cachexia and related conditions and diseases

Disclosed are monoclonal antibodies, binding fragments, and derivatives thereof directed to the human melanocortin-4 receptor, as well as pharmaceutical compositions including the same, and therapeutic uses, including methods for treating cachexia and related conditions and diseases, using such monoclonal antibodies, binding fragments, derivatives, and pharmaceutical compositions.
Owner:UNIVERSITY OF BASEL

Application of ML00253764 in preparation of medicine for treating obesity due to melanocortin receptors-4 mutant

InactiveCN104127411ARecovery capacityRestore cell membrane expressive abilityOrganic active ingredientsMetabolism disorderSignalling moleculesCell membrane
The invention relates to an application of ML00253764 in preparation of a medicine for treating obesity due to melanocortin receptors-4 mutant. The compound ML00253764 is taken as the medicine for treating obesity due to melanocortin receptors-4 mutant. The invention firstly found that ML00253764 (2-[2-(2-(5-bromine-2-methoxyphenyl)-ethyl]-3-fluorophenyl]-4,5-dihydro-1H-imidazoles) is taken as a pharmacy molecular chaperone of melanocortin receptor-4, and the ML00253764 has cell membrane expression capability of melanocortin receptor-4 for recovering cell membrane positioning defect and recovering generation capability of mutant signal molecules, and can be used for treating early obesity due to MC4R mutation.
Owner:TIANJIN UNIVERSITY OF SCIENCE AND TECHNOLOGY

Naphthalene-containing melanocortin receptor-specific small molecule

A melanocortin receptor-specific compound of the general formula of structure I: where X, R1, R2a, R2b, R3, R4a, R4b, R5a and R5b are as defined in the specification, which compound binds with high affinity to one or more melanocortin receptors and is optionally an agonist, an antagonist, an inverse agonist or an antagonist of an inverse agonist, and may be employed for treatment of one or melanocortin receptor-associated conditions or disorders, and methods for the use of the compounds of the invention.
Owner:PALATIN TECH INC

Acylated piperazine derivatives as melanocortin-4 receptor agonists

Certain novel N-acylated piperazine 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.
Owner:MERCK SHARP & DOHME CORP

RAAV vector-based pro-opiomelanocortin compositions and methods of use

Disclosed are methods for the use of pro-opiomelanocortin-encoding polynucleotides in the creation of transformed host cells and transgenic animals. In particular, the use of recombinant adeno-associated viral (rAAV) vector compositions, virions, and pluralities of virus particles that comprise a nucleic acid segment that expresses one or more mammalian pro-opiomelanocortin polypeptides in suitably transformed host cells is described. Also disclosed are methods for the treatment and amelioration of symptoms of a variety of conditions and disorders in an animal, including hyperinsulinemia, obesity, adiposity, overeating, and related eating disorders.
Owner:UNIV OF FLORIDA RES FOUNDATION INC
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