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44 results about "Melanocortins" patented technology
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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
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
InactiveUS20090076029A1Effective treatmentEfficacious is treating obesityCompound screeningOrganic active ingredientsMelanocytePhysiology
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
Acylated piperidine derivatives as melanocortin-4 receptor agonists
InactiveUS20040092501A1Minimize formationReduce appetiteBiocideMetabolism disorderDiseaseSexual dysfunction
Owner:MERCK SHARP & DOHME CORP
Selective cyclic peptides with melanocortin-4 receptor (MC4-R) agonist activity
Peptides cyclized via disulfide or lactam bridges are disclosed. The peptides exhibit melanocortin-4 receptor agonist activity and are useful for treating obesity.
Owner:F HOFFMANN LA ROCHE & CO AG
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
Compounds useful as modulators of melanocortin receptors and pharmaceutical compositions comprising same
InactiveUS6979691B2Improve the level ofGood effectBiocideSenses disorderMelanocortin receptorStereochemistry
Compounds having the formula (I), and pharmaceutically-acceptable salts, hydrates and prodrugs thereof,in which E is X is N or CH, W is —NR16R17, —NR16C(═O)R22, —NR16CO2R22, —OR23, or a heteroaryl or heterocyclo group as defined in the specification, and R1 through R12, R16, R17, R22, R23, x, y, and z are as defined in the specification, are useful as modulaters of melanocortin receptors, particularly MC-1R and MC-4R.
Owner:BRISTOL MYERS SQUIBB CO
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
ActiveUS7709484B1Impairment of energy homeostasisOrganic active ingredientsOrganic chemistryCompound aMelanocortin receptor
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
Novel Melanocortin Receptor Templates, Peptides, and Use Thereof
Owner:HASKELL LUEVANO CARRIE
Compounds, methods and formulations for the oral delivery of a glucagon-like peptide (GLP)-1 compound or a melanocortin-4 receptor (MC4) agonist peptide
Owner:NOVO NORDISK AS
Acylated spiropiperidine derivatives as melanocortin-4 receptor modulators
Certain novel N-acylated spiropiperidine derivatives are ligands of the human melanocortin receptor(s) and, in particular, are selective ligands 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 modulation of MC-4R, such as obesity, diabetes, nicotine addiction, alcoholism, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.
Owner:MERCK SHARP & DOHME LLC
Methods of modulating the activity of the MC1 receptor and treatment of conditions related to this receptor
InactiveUS20140128380A1Reduce formation rateBiocideCosmetic preparationsSolar urticariaHypopigmentation
The present invention provides compounds of Formula (I) that are useful for binding and / or modulating the biological activity of the melanocortin-1 receptor (MC1R). Compounds of this invention can be used to treat diseases and / or conditions in which modulation of MC1R is beneficial. Such diseases and / or conditions include, but are not limited to, hyperpigmentation (including melasma), hypopigmentation (including vitiligo), melanoma, basal cell carcinoma, squamous cell carcinoma, erythropoietic protoporphyria, polymorphous light eruption, solar urticaria, photosensitivity, sunburn, inflammatory diseases, aberrant fibroblast activity and pain.
Owner:MIMETICA PTY LTD
Process for the Synthesis of Ac-Arg-Cyclo(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-NH2
The present invention relates to a novel process for the synthesis of the melanocortin analog, Ac-Arg-cyclo(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-NH2, using solution-phase peptide chemistry.
Owner:IPSEN PHARMA SAS
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
Piperidine derivatives as melanocortin-4 receptor agonists
Certain novel 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.
Owner:MERCK SHARP & DOHME CORP
Adrenocorticotropic hormone analogs and related methods
InactiveCN101189022AMaintain healthPromote healthy growthPeptide/protein ingredientsCorticotropinSterolBiological activation
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
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
Melanocortin ligands and methods of use thereof
ActiveUS10899793B2Lower blood pressureInduce weight lossHormone peptidesTetrapeptide ingredientsOrganic chemistryMedicinal chemistry
Owner:TORREY PINES INST FOR MOLECULAR STUDIES +1
Auto-antibodies against the melanocortin-4 receptor
InactiveUS8008446B2Reduce appetiteInhibit bindingCompound screeningApoptosis detectionAutoantibodyMC4 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
InactiveUS7160886B2Reduce usageUseful in treatmentBiocideOrganic chemistrySexual dysfunctionMC4 Receptor
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
InactiveUS20050002905A1Reduce risk factorOvercome limitationsBiocideMetabolism disorderHyperinsulinemiaNucleotide
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
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
Compounds, Methods and Formulations for the Oral Delivery of a Glucagon-Like Peptide (Glp)-1 Compound or a Melanocortin-4 Receptor (Mc4) Agonist Peptide
Owner:NOVO NORDISK AS
Melanocortin Metallopeptode Combinatorial Libraries and Applications
InactiveUS20060240481A1Rapid and efficient complexationPeptide librariesIn-vivo radioactive preparationsCombinatorial chemistryMelanocortin receptor
Melanocortin receptor-specific peptide combinatorial libraries for forming metallopeptides and metallopeptide combinatorial libraries are provided for use in biological, pharmaceutical and related applications. The combinatorial libraries are constructed of peptides constructed from naturally occurring amino acids, stereoisomers and modifications of such amino acids, non-protein amino acids, post-translationally modified amino acids, enzymatically modified amino acids, or constructs or structures designed to mimic amino acids, in which the peptides are conformationally fixed on complexation of a metal ion-binding portion thereof with a metal ion.
Owner:PALATIN TECH INC
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