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282 results about "Partial agonist" patented technology
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In pharmacology, partial agonists are drugs that bind to and activate a given receptor, but have only partial efficacy at the receptor relative to a full agonist. They may also be considered ligands which display both agonistic and antagonistic effects—when both a full agonist and partial agonist are present, the partial agonist actually acts as a competitive antagonist, competing with the full agonist for receptor occupancy and producing a net decrease in the receptor activation observed with the full agonist alone. Clinically, partial agonists can be used to activate receptors to give a desired submaximal response when inadequate amounts of the endogenous ligand are present, or they can reduce the overstimulation of receptors when excess amounts of the endogenous ligand are present.
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 for treating idiopathic hyperhidrosis and associated conditions
InactiveUS20040192754A1Reduced activityAlleviate and treat symptomBiocideAnimal repellantsAllosteric modulatorMianserin Hydrochloride
The subject invention provides methods for treating symptoms and / or conditions associated with idiopathic hyperhidrosis by using compounds that decrease the activity of serotonin 5-HT2C receptors. Compounds that can ameliorate symptoms of idiopathic hyperhidrosis and associated conditions include 5-HT2C receptor antagonists (i.e., ketanserin, ritanserin, mianserin, mesulergine, cyproheptadine, fluoxetine, mirtazapine, olanzapine, and ziprasidone) as well as 5-HT2C receptor modulators (i.e., inverse agonists, partial agonists, and allosteric modulators).
Owner:SHAPIRA NATHAN ANDREW +2
Combination therapy for depression
InactiveUS20090023744A1Good curative effectEliminate side effectsOrganic active ingredientsNervous disorderSerotoninMetabolite
A combination therapy for treating depressive disorders is provided herein. The combination therapy comprises administering an effective amount of bupropion or its metabolites together with at least one serotonin 5-HT1A partial agonist or its metabolites to a patient in need of treatment of the depressive disorder. Pharmaceutical formulations, including packaged pharmaceutical formulations, comprising this combination are also provided herein.
Owner:THE GENERAL HOSPITAL CORP
Benzodioxane and benzodioxolane derivatives and uses thereof
Compounds of formula I or pharmaceutically acceptable salts thereof are provided: wherein each of R1, R2, R3, R4, y, n, m, and Ar are as defined, and described in classes and subclasses herein, which are agonists or partial agonists of the 2C subtype of brain serotonin receptors. The compounds, and compositions containing the compounds, can be used to treat a variety of central nervous system disorders such as schizophrenia.
Owner:WYETH LLC
Tricyclic quinolinone and tricyclic quinoline androgen receptor modulator compounds and methods
Owner:LIGAND PHARMA INC
Chromane and chromene derivatives and uses thereof
Compounds of formula I or pharmaceutically acceptable salts thereof are provided: wherein each of R1, R2, R3, R4, y, m, n, and Ar are as defined, and described in classes and subclasses herein, which are agonists or partial agonists of the 2C subtype of brain serotonin receptors. The compounds, and compositions containing the compounds, can be used to treat a variety of central nervous system disorders such as schizophrenia.
Owner:WYETH
Dihydrobenzofuran derivatives and uses therof
The present invention provides a composition comprising a compound of formula I: or a pharmaceutically acceptable salt thereof, wherein each of R1, R2, R3, y, n, and Ar are as defined, and described in classes and subclasses herein, which are agonists or partial agonists of the 2C subtype of brain serotonin receptors. Such compounds, and compositions thereof, are useful for treating a variety of central nervous system disorders such as schizophrenia.
Owner:WYETH LLC
Benzofuranyl alkanamine derivatives and uses thereof
InactiveUS20060247276A1Increase body weightUseful in treatmentBiocideNervous disorderSerotoninMedicine
Compounds of formula I or pharmaceutically acceptable salts thereof are provided: wherein each of R1, R1′, R2, R3, R4, n, and Ar are as defined, and described in classes and subclasses herein, which are agonists or partial agonists of the 2C subtype of brain serotonin receptors. The compounds, and compositions containing the compounds, can be used to treat a variety of central nervous system disorders such as schizophrenia.
Owner:WYETH LLC
Dihydrobenzofuranyl alkanamine derivatives and methods for using same
Compounds of formula 2 or pharmaceutically acceptable salts thereof are provided: wherein each of R1a, R2a, R3a, Ar, y, and m are as defined herein, which are agonists or partial agonists of the 2C subtype of brain serotonin receptors. The compounds, and compositions containing the compounds, are used to treat a variety of central nervous system disorders such as schizophrenia.
Owner:WYETH LLC
Composition for the administration of a D1-agonists
Owner:WEST PHARMA SERVICES DRUG DELIVERY & CLINICAL RES CENT
Method of treating mental disorders using D4 and 5-HT2A antagonists, inverse agonists or partial agonists
InactiveUS20050119248A1Good treatment effectRapid onsetBiocideOrganic chemistryDissociativeDrug compound
The present invention relates to methods of treating of the underlying dysregulation of the emotional functionality of mental disorders (i.e. affect instability-hypersensitivity-hyperaesthesia-dissociative phenomena- . . . ) using compounds and compositions of compounds having D4 and / or 5-HT2A antagonistic, partial agonistic or inverse agonistic activity for. The invention also relates to methods comprising administering to a patient diagnosed as having a neuropsychiatric disorder a pharmaceutical composition containing (i) compounds having D4 antagonistic, partial agonistic or inverse agonistic activity and / or (ii) compounds having 5-HT2A antagonistic, partial agonistic or inverse agonistic, and / or (iii) any known medicinal compound and compositions of said compounds. The combined D4 and 5-HT2A antagonistic, partial agonistic or inverse agonistic effects may reside within the same chemical or biological compound or in two different chemical and / or biological compounds.
Owner:PHARMANEUROBOOST
Acyl sulfamides for treatment of obesity, diabetes and lipid disorders
A class of acyl sulfamides comprises compounds that are potent ligands for PPAR gamma and generally have antagonist or partial agonist activity. The compounds may be useful in the treatment, control or prevention of obesity, non-insulin dependent diabetes mellitus (NIDDM), hyperglycemia, dyslipidemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, atherosclerosis, vascular restenosis, inflammation, and other PPAR gamma mediated diseases, disorders and conditions.
Owner:MERCK SHARP & DOHME CORP
Methods of treating alzheimer's disease, huntington's disease, autism, or other disorders
The disclosure relates, at least in part, to methods of treating autism in a patient in need thereof by administering an effective amount of a disclosed compound, e.g., a NMDA receptor glycine site partial agonist.
Owner:NORTHWEST UNIV
FXR receptor modulator, and preparation method and application thereof
ActiveCN106946867AFXR agonistic activity is goodOrganic chemistryAntipyreticChronic cholestasisChronic hepatitis
The invention discloses an FXR receptor modulator, and a preparation method and an application thereof, belonging to the field of medicinal chemistry. The FXR receptor modulator with a structure characteristic as shown in a formula I in the specification or pharmaceutically-acceptable salts or stereoisomers or solvates or prodrugs thereof can bind with an FXR (i.e., NR1H4) receptor and is used as an agonist or a partial agonist of the FXR receptor, thereby being able to be applied to prevention and treatment of FXR mediated diseases, such as chronic intrahepatic or extrahepatic cholestasis, hepatic fibrosis caused by chronic cholestasis or acute intrahepatic cholestasis, or chronic hepatitis B, or gallstone, or liver cancer, or colon cancer, or inflammatory bowel diseases, etc., wherein a part of compounds specifically can reach an FXR-excited EC<50> of 100 nM or below, show good FXR agonist activity, have excellent application prospects, and provide a new medicine choice for clinical treatment of the FXR mediated diseases.
Owner:GUANGZHOU HENOVCOM BIOSCI CO LTD
Compounds, their preparation and use
Novel compounds of general formula (I), the use of these compounds as medicaments, pharmaceuticaly compositions comprising the compounds and methods of treatment employing these compounds and compostiones. The present compounds may be useful in the treatment and / or prevention of conditions mediated by nuclear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR). The compounds exert their effects by modulating the PPARγ response in a partial agonist manner.
Owner:HIGH POINT PHARMA
Composition, synthesis and therapeutic applications of polyamines
InactiveUS20050085555A1Chromium concentration were decreasedIncrease excretionBiocideGroup 5/15 element organic compoundsAntidoteRisk stroke
This invention relates to a process of synthesis and composition of open chain (ring), closed ring, linear branched and or substituted polyamines, polyamine derived tyrosine phosphatase inhibitors and PPAR partial agonists / partial antagonists via a series of substitution reactions and optimizing the bioavailability and biological activities of the compounds. Polyamines prevent the toxicty of neutoxins and diabetogenic toxins including paraquat, methyphenyl pyridine radical, rotenone, diazoxide, streptozotocin and alloxan. These polyamines can be to treat neurological, cardiovascular, endocrine acquired and inherited mitochondrial DNA damage diseases and other disorders in mammalian subjects, and more specifically to the therapy of Parkinson's disease, Alzheimer's disease, Lou Gehrig's disease, Binswanger's disease, Olivopontine Cerebellar Degeneration, Lewy Body disease, Diabetes, Stroke, Atherosclerosis, Myocardial Ischemia, Cardiomyopathy, Nephropathy, Ischemia, Glaucoma, Presbycussis, Cancer, Osteoporosis, Rheumatoid Arthritis, Inflammatory Bowel Disease, Multiple Sclerosis and as Antidotes to Toxin Exposure.
Owner:MURPHY MICHAEL A
Use of D4 and 5-HT2A antagonists, inverse agonists or partial agonists
InactiveUS20110207776A1Good treatment effectRapid onsetBiocideNervous disorderDrug compoundInstability
The present invention relates to the use of compounds and compositions of compounds having D4 and 5-HT2A antagonistic, partial agonistic or inverse agonistic activity for the treatment of the underlying dysregulation of the emotional functionality of mental disorders (i.e. affect instability—hypersensitivity—hyperaesthesia—dissociative phenomena—etc). The invention also relates to methods comprising administering to a patient diagnosed as having a neuropsychiatric disorder a pharmaceutical composition containing (i) compounds having D4 antagonistic, partial agonistic or inverse agonistic activity and (ii) compounds having 5-HT2A antagonistic, partial agonistic or inverse agonistic, and (iii) any known medicinal compound and compositions of said compounds. The combined D4 and 5-HT2A antagonistic, partial agonistic or inverse agonistic effects may reside within the same chemical or biological compound or in two different chemical and / or biological compounds.
Owner:BUNTINX ERIK
MHC complexes and uses thereof
InactiveUS7074904B2Improve stabilityEasy affinity purificationBiocideVirusesMajor histocompatibility complex proteinFusion Complex
The present invention relates to novel complexes of major histocompability complex (MHC) molecules and uses of such complexes. In particular, the invention relates to MHC fusion complexes that contain a MHC molecule with a peptide-binding groove and a presenting peptide covalently linked to the MHC protein. Fusion complexes of the invention are useful for a variety of applications including in vitro screens for identification and isolation of peptides that modulate activity of selected T cells, including peptides that are T cell receptor antagonists and partial agonists, methods of suppressing an immune response of a mammal and methods for inducing an immune response in a mammal.
Owner:ALTOR BIOSCIENCE CORP
Serotonergic compositions and methods for treatment of mild cognitive impairment
A method of treating Mild Cognitive Impairment has been discovered. The treatment method comprises administering an effective amount of a serotonergic agent, including, but not limited to dexnorfenfluramine. The agent can be any serotonergic agonist, partial agonist, serotonin reuptake inhibitor, or combinations of these agents. The treatment method also encompasses combinations of serotonergic agents and non-steroidal anti-inflammatory agents. The treatment method may also delay the onset of Mild Cognitive Impairment, dementia, or both.
Owner:WURTMAN RICHARD J +1
Dopamine D3 acceptor portion agonist and its application
InactiveCN1948298AReduce the number of jumpsReduce weight lossOrganic active ingredientsNervous disorderChemical structureNervous system
The present invention relates to a dopamine D3 receptor portion excitant or its pharmaceutically acceptable salt and its application for curing diseases of central nervous system. Said invention also provides its chemical structure general formula, and provides detailed description.
Owner:SOUTHEAST UNIV
Melanocortin receptor-specific piperazine compounds with diamine groups
Melanocortin receptor-specific compounds with diamine groups of the general formulaand pharmaceutically acceptable salts thereof, where W is a diamine heteroatom unit with at least one cationic center, hydrogen bond donor or hydrogen bond acceptor, J, Q, L1, L2, L3, R1a, R1b, R2a, R2b and X are as defined in the specification, and the carbon atom marked with an asterisk can have any stereochemical configuration. Compounds disclosed herein bind to one or more melanocortin receptors and may be an agonist, a partial agonist, an antagonist, an inverse agonist or an antagonist of an inverse agonist as to one or more melanocortin receptors, and may be employed for treatment of one or more melanocortin receptor-associated conditions or disorders, including specifically treatment of obesity and related conditions.
Owner:PALATIN TECH INC
Dihydrobenzofuranyl alkanamines and methods for using same as cns agents
Compounds of formula 1 or pharmaceutically acceptable salts thereof are provided: which are agonists and partial agonists of the 2c subtype of brain serotonin receptors. The compounds, and compositions containing the compounds, can be used to treat a variety of central nervous system disorders such as schizophrenia.
Owner:WYETH LLC
Use of N-desmethylclozapine and related compounds as dopamine stabilizing agents
InactiveUS20060252744A1Reduce exposureMany symptomBiocideNervous disorderPsychosis drugNeuropsychiatric disease
Disclosed herein is the use of N-desmethylclozapine (NDMC) and related compounds to treat a variety of neuropsychiatric diseases including psychosis. It is shown that NDMC and related compounds are agonists or partial agonists at D2 and D3 dopamine receptors and thus may be effective as a dopamine stabilizing agent, allowing it to be used to treat or provide reduced incidence of Extrapyramidal symptoms (EPS) and / or tardive dyskinesias (TD). Also disclosed is administering NDMC and related compounds in combination with other anti-psychotic agents.
Owner:ACADIA PHARMA INC
[1,4]Diazepino[6,7,1-ij]quinoline derivatives as antipsychotic and antiobesity agents
![[1,4]Diazepino[6,7,1-ij]quinoline derivatives as antipsychotic and antiobesity agents](https://images-eureka-patsnap-com.libproxy1.nus.edu.sg/patent_img/a3c445cf-2707-4780-9b76-409cd765be12/US07129237-C00001.png "[1,4]Diazepino[6,7,1-ij]quinoline derivatives as antipsychotic and antiobesity agents")
![[1,4]Diazepino[6,7,1-ij]quinoline derivatives as antipsychotic and antiobesity agents](https://images-eureka-patsnap-com.libproxy1.nus.edu.sg/patent_img/a3c445cf-2707-4780-9b76-409cd765be12/US07129237-C00002.png "[1,4]Diazepino[6,7,1-ij]quinoline derivatives as antipsychotic and antiobesity agents")
![[1,4]Diazepino[6,7,1-ij]quinoline derivatives as antipsychotic and antiobesity agents](https://images-eureka-patsnap-com.libproxy1.nus.edu.sg/patent_img/a3c445cf-2707-4780-9b76-409cd765be12/US07129237-C00003.png "[1,4]Diazepino[6,7,1-ij]quinoline derivatives as antipsychotic and antiobesity agents")
Owner:WYETH LLC
A3 adenosine receptor antagonists and partial agonists
InactiveUS20110171130A1High potencyHighly selectiveBiocideSenses disorderHypersensitive responseArthritis
Disclosed are A3 adenosine receptor antagonists and / or partial agonists of formula (I): wherein R1 to R5 are as described herein, as well as pharmaceutical compositions thereof and methods of use thereof. The antagonists or partial agonists find use in treating a number of diseases including cancer, glaucoma, inflammatory diseases, asthma, stroke, myocardial infarction, allergic reactions, rhinitis, poison ivy induced responses, urticaria, scleroderma, arthritis, brain arteriole diameter constriction, bronchoconstriction, and myocardial ischemia, as well as in preventing cardiac ischemia. Also disclosed are radiolabeled compounds of formula (I) and the use thereof in diagnostic imaging of tissues and organs.
Owner:UNITED STATES OF AMERICA
Biosensors for monitoring receptor-mediated g-protein activation
ActiveUS20090298162A1Easy to useCompound screeningBioreactor/fermenter combinationsBiological activationQuantitative assay
The present invention relates to novel biosensors that are based on bioluminescence resonance energy transfer (BRET). These biosensors may be used to monitor rapid interaction and conformational changes within G protein-coupled receptor / G protein complexes and, in this way, reflect the activation status of the receptor. Advantageously, the biosensors may be used as a highly sensitive and quantitative assay for the identification of ligands (agonists, antagonists, inverse agonists, partial agonists, etc.) targeting G protein-coupled receptors (GPCRs) as well as for the analysis of the activation status of these receptors. Moreover, multiplexing different biosensors within receptors / G protein complexes allows for mapping ligand textures. Additionally, the biosensors permit the direct, real-time examination of interactions between receptors and G protein in their natural environment, the living cell.
Owner:UNIV DE MONTREAL
Substituted Melanocortin Receptor-Specific Single Acyl Piperazine Compounds
ActiveUS20060287330A1Impairment of energy homeostasisOrganic active ingredientsOrganic chemistryAcyl groupHeteroatom
Melanocortin receptor-specific compounds of the general formula and pharmaceutically acceptable salts thereof, where J is a substituted or unsubstituted monocyclic or bicyclic ring structure, W is a heteroatom unit with at least one cationic center, hydrogen bond donor or hydrogen bond acceptor, Q is a substituted or unsubstituted aromatic carbocyclic ring group, L, R2a, R2b, R3a, R3b, r, x and y are as defined in the specification, and the carbon atoms marked with an asterisk can have any stereochemical configuration. Compounds disclosed herein bind to one or more melanocortin receptors and may be an agonist, a partial agonist, an antagonist, an inverse agonist or an antagonist of an inverse agonist as to one or more melanocortin receptors, and may be employed for treatment of one or more melanocortin receptor-associated conditions or disorders, including specifically treatment of obesity and related conditions.
Owner:PALATIN TECH INC
Method for enhancing learning and memory impaired by neurodegenerative disorders and compounds and compositions for effecting the same
InactiveUS20130096126A1Easy to learnEnhance memoryOrganic active ingredientsBiocideAdrenergicAdrenergic receptor agonists
A method for enhancing learning or memory of both in a mammal having impaired learning or emory of both from a neuro-degenerative disorder, which entails the step of administering at least one compound or a salt thereof which is a β1-adrenergic receptor agonist, partial agonist or receptor ligand in an amount effective to improve the learning or memory or both of said mammal.
Owner:THE BOARD OF TRUSTEES OF THE LELAND STANFORD JUNIOR UNIV
Methods and compositions for treating and preventing trigeminal autonomic cephalgias, migraine, and vascular conditions
The present invention relates to, among other things, methods for treating trigeminal cephalgias such as migraine and migraine like headaches and other cerebrovascular conditions associated with pain and or inflammation. When non-steroidal anti inflammatory drugs (NSAIDs), such as ketoprofen, are applied locally using specific topical formulations immediate relief of pain is obtained. Intense pain is typically reduced to mild pain or no pain within 30 minutes of application of the topical formulation. The NSAID may be given in combination with other pharmacological agents, such as vasoconstrictors, opioids, decongestants and / or non-opioid migraine drugs, such as triptans and ergots and agents that affect serotonin receptors as agonists, antagonists or partial agonists.
Owner:ACHELIOS THERAPEUTICS
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