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43 results about "Mixed Opioid Agonist/Antagonist" patented technology
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An opioid modulator (or opioid receptor modulator) is a drug which has mixed agonist and antagonist actions at different opioid receptors and thus cannot clearly be described as either an opioid agonist or antagonist.
Novel compounds as opioid receptor modulators
ActiveUS20050203143A1Improved pharmacological profileImproved profileBiocideNervous disorderMixed Opioid Agonist/AntagonistOpioid receptor
The present invention is directed to novel opioid receptor modulators of Formula (I). The invention further relates to methods for preparing such compounds, pharmaceutical compositions containing them, and their use in the treatment of disorders that may be ameliorated or treated by the modulation of opioid receptors.
Owner:JANSSEN PHARMA NV
Compounds as opioid receptor modulators
ActiveUS7741356B2Improved profileBiocideOrganic active ingredientsDiseaseMixed Opioid Agonist/Antagonist
The present invention is directed to novel opioid receptor modulators of Formula (I).The invention further relates to methods for preparing such compounds, pharmaceutical compositions containing them, and their use in the treatment of disorders that may be ameliorated or treated by the modulation of opioid receptors.
Owner:JANSSEN PHARMA NV
Tricyclic opioid modulators
The invention is directed to compounds of Formula (I) useful as delta and mu opioid receptor modulators. Pharmaceutical and veterinary compositions and methods of treating mild to severe pain and various diseases using compounds of the invention are also described.
Owner:JANSSEN PHARMA NV
Heterodimeric opioid G-protein coupled receptors
InactiveUS6855807B1Effective treatmentAccurate identificationBacteriaBiological material analysisMu Opiate ReceptorHigh-throughput screening
Opioid receptors form functional heterodimers with each other and with other G-protein coupled receptors, such as dopamine receptors, adrenergic receptors, or chemokine receptors. These receptors can be exploited for high throughput screening of compounds to identify heterodimer opioid receptor modulators (agonists and antagonists). The invention also relates to identification of novel heterodimer receptor ligands and synergistic compositions, which can provide strategies for analgesia, narcotic addiction, hypertension, HIV infection, and immune system function.
Owner:NEW YORK UNIV
Opioid receptor modulator dosage formulations
ActiveUS20140271854A1Extended shelf lifeImprove stabilityBiocideOrganic active ingredientsBenzoic acidMixed Opioid Agonist/Antagonist
Abuse deterrent solid dosage formulations containing 5-({[2-Amino-3-(4-carbamoyl-2,6-dimethyl-phenyl)-propionyl]-[1-(4-phenyl-1H-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy-benzoic acid, and processes for the preparation and administration of these formulations.
Owner:ALLERGAN HLDG UNLTD
Opioid receptor modulator dosage formulations
ActiveUS9675587B2Prolong lifeImprove stabilityOrganic active ingredientsNervous disorderBenzoic acidMixed Opioid Agonist/Antagonist
Abuse deterrent solid dosage formulations containing 5-({[2-Amino-3-(4-carbamoyl-2,6-dimethyl-phenyl)-propionyl]-[1-(4-phenyl-1H-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy-benzoic acid, and processes for the preparation and administration of these formulations.
Owner:ALLERGAN HLDG UNLTD
Benzomorphan compounds as opioid receptors modulators
InactiveUS20150210646A1Reduce and prevent constipationReduction and prevention of constipationBiocideNervous disorderMixed Opioid Agonist/AntagonistBenzomorphan
The present invention is directed to Benzomorphan Analog compounds of the Formula (I), Formula (IA), Formula (IB), Formula (IC), or Formula (ID) as shown below, wherein R1, R2a, R2b, R3, R4, Z, and G are as defined herein. Compounds of the Invention are useful for treating pain, constipation, and other conditions modulated by activity of opioid and ORL-1 receptors.
Owner:PURDUE PHARMA LP
Preparation method of alanine derivatives
ActiveCN105693554AHigh yieldLow costCarbamic acid derivatives preparationCarboxylic acid nitrile preparationTyrosineMixed Opioid Agonist/Antagonist
The invention discloses a method for preparing alanine derivatives disclosed as Formula (I). The alanine derivatives can be used as a synthesis intermediate of an opioid receptor regulator, such as a synthesis intermediate of eluxadoline. By using the cheap and accessible chiral tyrosine as the initial raw material, the invention provides a brand-new synthesis route for preparing alanine derivatives. The whole reaction route has the advantages of high total yield, low cost and mild reaction conditions, is simple and safe for operation, and is suitable for large-scale industrial production.
Owner:四川伊诺达博医药科技有限公司
Piperdinyl-phenoxazine and phenothiazine derivatives as delta-opioid modulators
Owner:JANSSEN PHARMA NV
Tricyclic opioid modulators
The invention is directed to compounds of Formula (I) useful as delta and mu opioid receptor modulators. Pharmaceutical and veterinary compositions and methods of treating mild to severe pain and various diseases using compounds of the invention are also described.
Owner:JANSSEN PHARMA NV
4-substituted-2-phenoxy-phenylamine delta opioid receptor modulators
Owner:JANSSEN PHARMA NV
Pyrimidine compounds as delta opioid receptor modulators
ActiveUS20110105520A1Organic active ingredientsBiocideMixed Opioid Agonist/AntagonistOpioid receptor
Owner:JANSSEN PHARMA NV
4-substituted-2-phenoxy-phenylamine delta opioid receptor modulators
Owner:JANSSEN PHARMA NV
Mitragynine alkaloids as opioid receptor modulators
Owner:THE TRUSTEES OF COLUMBIA UNIV IN THE CITY OF NEW YORK
Polycyclic amines as opioid receptor modulators
ActiveUS20180258065A1Group 3/13 element organic compoundsMagnesiaAlcohol addictionNeurological disorder
The present invention provides a genus of polycyclic amines that are useful as opioid receptor modulators. The compounds of the invention are useful in both therapeutic and diagnostic methods, including for treating pain, neurological disorders, cardiac disorders, bowel disorders, drug and alcohol addiction, drug overdose, urinary disorders, respiratory disorders, sexual dysfunction, psoriasis, graft rejection or cancer.
Owner:ECSTASY LLC
Tricyclic delta-opioid modulators
Owner:JANSSEN PHARMA NV
Tricyclic delta-opioid modulators
Owner:JANSSEN PHARMA NV
Polycyclic amines as opioid receptor modulators
ActiveUS10676456B2Group 3/13 element organic compoundsMagnesiaAlcohol addictionNeurological disorder
The present invention provides a genus of polycyclic amines that are useful as opioid receptor modulators. The compounds of the invention are useful in both therapeutic and diagnostic methods, including for treating pain, neurological disorders, cardiac disorders, bowel disorders, drug and alcohol addiction, drug overdose, urinary disorders, respiratory disorders, sexual dysfunction, psoriasis, graft rejection or cancer.
Owner:ECSTASY LLC
Pyrimidine compounds as delta opioid receptor modulators
Owner:JANSSEN PHARMA NV
4-substituted-2-phenoxy-phenylamine delta opioid receptor modulators
Owner:JANSSEN PHARMA NV
Opioid receptor modulators and products and methods related thereto
InactiveUS20210147343A1Nervous disorderOrganic chemistry methodsMixed Opioid Agonist/AntagonistPharmaceutical medicine
Compounds are provided having the structure of Formula (I): or a pharmaceutically acceptable isomer, racemate, hydrate, solvate, isotope, or salt thereof, wherein A, B, L, R3, R4, R5, R6, R8, m and n are as defined herein. Such compounds modulate the opioid receptor, particulate the mu-opioid receptor (MOR) and / or the kappa-opioid receptor (KOR), and / or the delta-opioid receptor (DOR). Products containing such compounds, as well as methods for their use and preparation, are also provided.
Owner:EPIODYNE INC
Opioid receptor modulator dosage formulations
InactiveUS20220016034A1Extended shelf lifeImprove stabilityOrganic active ingredientsPill deliveryBenzoic acidMedicine
Abuse deterrent solid dosage formulations containing 5-({[2-Amino-3-(4-carbamoyl-2,6-dimethyl-phenyl)-propionyl]-[1-(4-phenyl-4,5-dihydro-1H-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy-benzoic acid, and processes for the preparation and administration of these formulations.
Owner:ALLERGAN HLDG UNLTD
Phenoxy-substituted pyrimidines as opioid receptor modulators
Owner:JANSSEN PHARMA NV
Mitragynine alkaloids as opioid receptor modulators
Owner:THE TRUSTEES OF COLUMBIA UNIV IN THE CITY OF NEW YORK
Opioid receptor modulators and products and methods related thereto
ActiveUS20210163402A1Nervous disorderOrganic chemistry methodsMedicineMixed Opioid Agonist/Antagonist
Compounds are provided having the structure of Formula (I):or a pharmaceutically acceptable isomer, racemate, hydrate, solvate, isotope, or salt thereof, wherein A, B, L, R3, R4, R5, R6, R8, m and n are as defined herein. Such compounds modulate the opioid receptor, particulare the mu-opioid receptor (MOR) and / or the kappa-opioid receptor (KOR), and / or the delta-opioid receptor (DOR). Products containing such compounds, as well as methods for their use and preparation, are also provided.
Owner:EPIODYNE INC
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