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343 results about "Inverse agonist" patented technology
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In pharmacology, an inverse agonist is a drug that binds to the same receptor as an agonist but induces a pharmacological response opposite to that of the agonist. A neutral antagonist has no activity in the absence of an agonist or inverse agonist but can block the activity of either. Inverse agonists have opposite actions to those of agonists but the effects of both of these can be blocked by antagonists.
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
Cannabinoid receptor antagonists/inverse agonists useful for treating obesity
The present invention provides novel pyrazoles that are useful as cannabinoid receptor antagonists and pharmaceutical compositions thereof and methods of using the same for treating obesity, diabetes, and / or cardiometabolic disorders.
Owner:JENRIN DISCOVERY
Compounds which modulate the CB2 receptor
Compounds are provided which bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, the compounds having the general formulawherein, R1, R2, A, Y, X, Ar1 and Ar2 have the meanings given in the specification, and the preparation and use thereof. The compounds are valuable CB2 receptor modulators.
Owner:BOEHRINGER INGELHEIM INT GMBH
Combinations of 5-ht2a inverse agonists and antagonists with antipsychotics
InactiveUS20090053329A1Achieve effectQuick effectCompounds screening/testingBiocideSide effectAntipsychotic drug therapy
Combinations of 5-HT2A inverse agonists or antagonists such as pimavanserin with antipsychotics such as risperidone are shown to induce a rapid onset of antipsychotic action and increase the number of responders when compared to therapy with the antipsychotic alone. These effects can be achieved at a low dose of the antipsychotic, thereby reducing the incidence of side effects. The combinations are also effective at decreases the incidence of weight gain and increased glucose or prolactin levels caused by the antipsychotic.
Owner:ACADIA PHARMA INC
Methods of identifying inverse agonists of the serotonin 2A receptor
InactiveUS20050148018A1Favorable side effect profileBroad efficacyCompound screeningHormone peptidesConstitutively activeSerotonin 2A Receptors
The present invention relates to a method of identifying compounds which act as inverse agonists of the 5-HT2A receptor, the method comprising contacting a constitutively active 5-HT2A receptor with at least one test compound and determining any decrease in the level of basal activity of the receptor so as to identify a test compound which is an inverse agonist of the 5-HT2A receptor. Such inverse agonists may be used in the treatment of schizophrenia and related psychoses.
Owner:WEINER DAVID +1
Selective serotonin 2A/2C receptor inverse agonists as therapeutics for neurodegenerative diseases
Behavioral pharmacological data with the compound of formula (I), a novel and selective 5HT2A / 2C receptor inverse agonist, demonstrate in vivo efficacy in models of psychosis and dyskinesias. This includes activity in reversing MK-801 induced locomotor behaviors, suggesting that this compound may be an efficacious anti-psychotic, and activity in an MPTP primate model of dyskinesias, suggesting efficacy as an anti-dyskinesia agent. These data support the hypothesis that 5HT2A / 2C receptor inverse agonism may confer antipsychotic and anti-dyskinetic efficacy in humans, and indicate a use of the compound of formula (I) and related agents as novel therapeutics for Parkinson's Disease, related human neurodegenerative diseases, and psychosis.
Owner:ACADIA PHARMA INC
Substituted aryl amides
Novel compounds of structural formula (I) are antagonists and / or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as psychotropic drugs in the treatment of psychosis, memory deficits, cognitive disorders, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, the treatment of obesity or eating disorders, as well as, the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, and cirrhosis of the liver.
Owner:MERCK & CO INC
Identification of ligands by selective amplification of cells transfected with receptors
InactiveUS20050244862A1Increase ratingsReduced responseCompound screeningApoptosis detectionConstitutively activeSerotonin 2A Receptors
Owner:ACADIA PHARMA INC
Selective serotonin 2A/2C receptor inverse agonists as therapeutics for neurodegenerative diseases
ActiveUS20060199842A1Inhibition of activationInhibition is effectiveBiocideNervous disorderMPTPNeuro-degenerative disease
Behavioral pharmacological data with the compound of formula (I), a novel and selective 5HT2A / 2C receptor inverse agonist, demonstrate in vivo efficacy in models of psychosis and dyskinesias. This includes activity in reversing MK-801 induced locomotor behaviors, suggesting that this compound may be an efficacious anti-psychotic, and activity in an MPTP primate model of dyskinesias, suggesting efficacy as an anti-dyskinesia agent. These data support the hypothesis that 5HT2A / 2C receptor inverse agonism may confer antipsychotic and anti-dyskinetic efficacy in humans, and indicate a use of the compound of formula (I) and related agents as novel therapeutics for Parkinson's Disease, related human neurodegenerative diseases, and psychosis.
Owner:ACADIA PHARMA INC
New pharmaceutical formulation comprising cannabidiol and tetrahydrocannabidivarin
InactiveUS20100317729A1Enhanced treatment optionGood for weight lossBiocideNervous disorderCannabinoidPharmaceutical formulation
The present invention relates to a novel pharmaceutical formulation comprising a ratioed mix of: (i) one or more compounds that acts as an inverse agonist of the CB1 and / or CB2 receptor; and (ii) one or more compounds that acts as a neutral antagonist of the CB1 and / or CB2 receptor. Preferably both the inverse agonist of the CB1 and / or CB2 receptor and the neutral antagonist of the CB1 and / or CB2 receptor are cannabinoids. Preferably the cannabinoids are tetrahydrocannabidivarin (THCV) and cannabidiol (CBD).
Owner:GW PHARMA LTD
Selective serotonin 2A/2C receptor inverse agonists as therapeutics for neurodegenerative diseases
Behavioral pharmacological data with the compound of formula (I), a novel and selective 5HT2A / 2C receptor inverse agonist, demonstrate in vivo efficacy in models of psychosis and dyskinesias. This includes activity in reversing MK-801 induced locomotor behaviors, suggesting that this compound may be an efficacious anti-psychotic, and activity in an MPTP primate model of dyskinesias, suggesting efficacy as an anti-dyskinesia agent. These data support the hypothesis that 5HT2A / 2C receptor inverse agonism may confer antipsychotic and anti-dyskinetic efficacy in humans, and indicate a use of the compound of formula (I) and related agents as novel therapeutics for Parkinson's Disease, related human neurodegenerative diseases, and psychosis.
Owner:ACADIA PHARMA INC
Use for Cannabinoid
InactiveUS20090306221A1High activityLess degree of activityBiocideNervous disorderDiseaseCannabinoid
The present invention relates to the use of one or more cannabinoids in the manufacture of medicaments for use in 0 the treatment of diseases and conditions benefiting from inverse agonism of the CB1 and / or the CB2 cannabinoid receptor. Preferably the cannabinoid is a cannabidiol (CBD) type compound or derivative thereof.
Owner:GW PHARMA LTD
Substituted amides
Novel compounds of the structural formula (I) are antagonists and / or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, the treatment of obesity or eating disorders, as well as the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, and cirrhosis of the liver.
Owner:MERCK SHARP & DOHME LLC
Glucagon antagonists/inverse agonists
A novel class of compounds, which act to antagonize the action of the glucagon hormone on the glucagon receptor. Owing to their antagonizing effect of the glucagon receptor the compounds may be suitable for the treatment and / or prevention of any glucagon-mediated conditions and diseases such as hyperglycemia, Type 1 diabetes, Type 2 diabetes and obesity.
Owner:PFIZER INC
Glucagon antagonists/inverse agonists
A novel class of compounds, which act to antagonize the action of the glucagon hormone on the glucagon receptor. Owing to their antagonizing effect of the glucagon receptor the compounds may be suitable for the treatment and / or prevention of any diseases and disorders, wherein a glucagon antagonistic action is beneficial, such as hyperglycemia, Type 1 diabetes, Type 2 diabetes, disorders of the lipid metabolism, such as dyslipidemia, and obesity.
Owner:PFIZER INC
Cannabinoid receptor antagonists/inverse agonists useful for treating metabolic disorders, including obesity and diabetes
The present invention provides novel pyrazoles that are useful as cannabinoid receptor antagonists and pharmaceutical compositions thereof and methods of using the same for treating obesity, diabetes, hepatic disorders, and / or cardiometabolic disorders.
Owner:JENRIN DISCOVERY
Methods for treating chemotherapy and radiation therapy side effects
ActiveUS20090176862A1Reduced hematopoietic functionDegraded immune functionAntibacterial agentsBiocideSide effectRadical radiotherapy
A method for treating chemo therapy or radiation therapy side effects in a mammal undergoing chemotherapy and / or radiation therapy, the method comprising a step of administering to the mammal a therapeutically effective amount of a RAR antagonist or RAR inverse agonist which binds to receptors of the RARα, RARβ and RARγ subtypes is disclosed. Such side effects include chemoradiotherapy-induced alopecia, chemoradiotherapy-induced thrombocytopenia, chemoradiotherapy-induced leucopenia and chemoradiotherapy-induced neutropenia.
Owner:IO THERAPEUTICS
Compounds Which Modulate The CB2 Receptor
Compounds are provided which bind to and are agonist, antagonists or inverse agonists of the CB2 receptor, the compounds having the general formula (I) wherein R1, R2, R3, X and Ar have the meanings given in the specification, and the preparation and use thereof. The compounds are valuable CB2 receptor modulators, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.
Owner:BOEHRINGER INGELHEIM INT GMBH
Compounds Which Modulate The CB2 Receptor
Compounds are provided which bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, the compounds having the general formula wherein, R1, R2, A, Y, X, Ar1 and Ar2 have the meanings given in the specification, and the preparation and use thereof. The compounds are valuable CB2 receptor modulators.
Owner:BOEHRINGER INGELHEIM INT GMBH
Compounds Which Modulate The CB2 Receptor
Compounds of formula (I) are disclosed. Compounds according to the invention are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.
Owner:BOEHRINGER INGELHEIM INT GMBH
Heterocyclic compounds as ligands of the GABAA receptor
Disclosed are heterocyclic compounds of the formula and the pharmaceutically acceptable salts thereof wherein the variables A, V, Y, J, E, X, T, G, Q, W, Z, b, n and m are defined herein. These compounds are highly selective agonists, antagonists or inverse agonists for GABAA brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAA brain receptor.
Owner:NEUROGEN +1
Histamine H3 Receptor Agents, Preparation and Therapeutic Uses
The present invention provides a novel compound of Formula (I) or a pharmaceutically acceptable salt thereof, having histamine-113 receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds. In another, embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula (I) as well as methods of using them to treat obesity, cognitive deficiencies, narcolepsy, and other histamine H3 receptor-related diseases.
Owner:FINLEY DON RICHARD +5
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
Methods of treating hyperlipidemia
The current invention relates to methods for treating hyperlipidemia in mammals, including humans. More specifically, the current invention relates to the use of retinoid or retinoid derivative that is able to act as an antagonist or inverse agonist of a retinoid receptor to treat hyperlipidemia.
Owner:ALLERGAN INC
Pyridine-3-carboxamide derivatives as CB1 inverse agonists
Owner:F HOFFMANN LA ROCHE INC
Diazepane Compounds Which Modulate The CB2 Receptor
Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.
Owner:BOEHRINGER INGELHEIM INT GMBH
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