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32 results about "Partial agonist" patented technology

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.

Injectable formulations for non-naturally occurring melanocortin analogs for treating substance use disorders and / or modulating diabetes

PCT designated stageWO2026080392A2Metabolism disorderPharmaceutical delivery mechanismMelanocortin 3 receptorDiabetes mellitus
Provided herein are stable aqueous pharmaceutical compositions and formulation comprising non-naturally occurring melanocortin analogs. The non-naturally occurring melanocortin analogs may be partial agonists of the melanocortin 4 receptor with sub-micromolar or low-nanomolar binding activity. Certain non-naturally occurring melanocortin analogs may also be partial agonists or partial antagonists of the melanocortin 3 receptor.
Owner:ENDEVICA BIO INC

Non-naturally occurring melanocortin analogs with an extended c-terminus for modulating diabetes and / or treating substance use disorders

PCT designated stageWO2026039686A1Pharmaceutical delivery mechanismCyclic peptide ingredientsMelanocortin 3 receptorDiabetes mellitus
The present technology comprises non-naturally occurring melanocortin analogs or pharmaceutically acceptable salts, solvates, or stereoisomers thereof and compositions comprising the same. The non-naturally occurring melanocortin analogs may be partial agonists the melanocortin 4 receptor with sub-micromolar or low-nanomolar binding activity. Certain non-naturally occurring melanocortin analogs may also be partial agonists or partial antagonists of the melanocortin 3 receptor.
Owner:ENDEVICA BIO INC

V1a receptor partial agonists and methods of use

InactiveJP2026009187AOxytocins/vasopressinsPeptide/protein ingredientsPeritoneal fluidLiver fibrosis
V1a RECEPTOR PARTIAL AGONISTS AND METHODS OF USE SOLUTION: The present invention provides novel partial V1a agonists for partial activation of V1a receptors. The partial V1a agonists have therapeutic indices of at least 20 (e.g., at least 30, at least 40, at least 50, at least 60, at least 70, at least 80, at least 90, at least 100). Also provided is a method of treating liver fibrosis, hepatocirrhosis, portal hypertension, peritoneal fluid, esophageal varices, fundic varices, hemorrhage, arterial hypotension, and / or hepatorenal syndrome, comprising administering to a subject in need thereof a therapeutically effective dose of a composition comprising one or more of the disclosed partial V1a agonists, optionally in combination with a V2 antagonist.SELECTED DRAWING: None
Owner:PHARMAIN CORP

Non-naturally occurring melanocortin analogs with an n-terminal extension for modulating weight loss

PCT designated stageWO2026039662A1Metabolism disorderPharmaceutical delivery mechanismMelanocortin 3 receptorPharmaceutical medicine
The present technology comprises non-naturally occurring melanocortin analogs or pharmaceutically acceptable salts, solvates, or stereoisomers thereof and compositions comprising the same. The non-naturally occurring melanocortin analogs may be full agonists of the melanocortin 3 receptor and full or partial agonists of the melanocortin 4 receptor with sub-micromolar or low-nanomolar binding activity.
Owner:ENDEVICA BIO INC

Injectable formulations for non-naturally occurring melanocortin analogs for modulating weight loss

PCT designated stageWO2026080406A1Metabolism disorderPharmaceutical delivery mechanismMelanocortin 3 receptorPharmaceutical drug
The present technology comprises stable aqueous pharmaceutical compositions and formulation comprising non-naturally occurring melanocortin agonist analogs. In some embodiments, the non-naturally occurring melanocortin analogs may be full agonists of the melanocortin 3 receptor (MC3R) and full or partial agonists of the melanocortin 4 receptor (MC4R) with sub-micromolar and / or low-nanomolar binding activity.
Owner:ENDEVICA BIO INC

V1A Receptor Partial Agonist and Method of Use

PendingUS20260015389A1Oxytocins/vasopressinsPeptide/protein ingredientsLiver fibrosisHepatorenal syndrome
The present disclosure provides novel V1a partial agonists for partially activating a V1a receptor. The partial V1a agonist has a therapeutic index of at least 20 (e.g., at least 30, at least 40, at least 50, at least 60, at least 70, at least 80, at least 90, at least 100). Also provided are method of treating liver fibrosis, cirrhosis, portal hypertension, ascites, esophageal varices, fundal varices, bleeding, arterial hypotension, and / or hepatorenal syndrome, including administering to a subject in need thereof a therapeutically effective dose of a composition including the V1a partial agonist(s) of the present disclosure, optionally in combination with a V2 antagonist.
Owner:PHARMAIN CORP

Non-naturally occurring melanocortin analogs with various lactam cyclization types for modulating weight loss

PCT designated stageWO2026039648A1Peptide-nucleic acidsPharmaceutical delivery mechanismMelanocortin 3 receptorMC4 Receptor
The present technology comprises non-naturally occurring melanocortin analogs or pharmaceutically acceptable salts, solvates, or stereoisomers thereof and compositions comprising the same. The non-naturally occurring melanocortin analogs may be full agonists of the melanocortin 3 receptor and full or partial agonists of the melanocortin 4 receptor with sub-micromolar and / or low-nanomolar binding activity.
Owner:ENDEVICA BIO INC

Class of salt compounds of isosorbide mononitrate derivatives and use thereof

PCT designated stageWO2026061429A1Nervous disorderOrganic chemistryNR1 NMDA receptorPharmaceutical drug
The present invention belongs to the field of pharmaceuticals. Disclosed in the present invention are a class of salt compounds of isosorbide mononitrate derivatives and the use thereof. Salts formed by the isosorbide mononitrate derivatives of the present invention and D-cycloserine exhibit dual activities as a nitric oxide donor and a partial NMDA receptor agonist. The present invention further relates to the use of the salts formed by the isosorbide mononitrate derivatives and D-cycloserine in a drug for treating cerebral stroke or the recovery period of cerebral stroke.
Owner:NEURODAWN PHARM CO LTD

Non-naturally occurring melanocortin analogs with an n-terminal extension for modulating weight gain

PCT designated stageWO2026039674A1Pharmaceutical delivery mechanismCyclic peptide ingredientsMelanocortin 3 receptorMC4 Receptor
The present technology comprises non-naturally occurring melanocortin analogs or pharmaceutically acceptable salts, solvates, or stereoisomers thereof and compositions comprising the same. The non-naturally occurring melanocortin analogs may be full or partial antagonists of the melanocortin 3 receptor with sub-micromolar or low-nanomolar binding activity. Some of the non-naturally occurring melanocortin analogs may also be full or partial antagonists or partial agonists of the melanocortin 4 receptor with sub-micromolar or low-nanomolar binding activity.
Owner:ENDEVICA BIO INC

Selective opioid receptor agonists and antagonists

Compounds having opioid characteristics are provided that can be used for various therapeutic methods including the treatment of pain and opioid use disorders, and compounds having opioid antagonist properties that can be used to treat opioid overdoses. These compounds include agonists and antagonists having selective activity toward more one or more opioid receptors. Such compounds can be full or partial agonists, or can be antagonists lacking agonist properties toward delta and kappa opioid receptors. The partial agonists can diminish side effects associated with traditional opioid medications, and the antagonists can overcome respiratory depression caused by potent narcotics. Structurally these compounds include constrained piperidines with alkenyl or cyanoalkyl groups, as well as other substituents providing desired properties.
Owner:THE GOVERNMENT OF THE UNITED STATES OF AMERICA AS REPRESENTED BY THE SECRETARY DEPARTMENT OF HEALTH & HUMAN SERVICES

Intestine-specific partial agonists of farnesoid X receptor and uses thereof

ActiveUS12522562B2Organic chemistryDigestive systemDiseaseFarnesoid X receptor
An intestine-specific partial agonists of farnesoid X receptor (FXR) is disclosed, along with methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders associated with FXR activity.
Owner:EWHA DRUGDESIGNHOUSE CO LTD

Indazole derivatives as cannabinoid receptor partial agonists

ActiveUS12577207B2Organic chemistryMetabolism disorderDiseaseLiver disorder
The present disclosure includes peripheral partial agonists of one or more CB receptors, including modulation of CB1, both with and without CB2 selectivity. The compounds of the present disclosure may be useful in the treatment of diseases and disorders mediated by a CB-signaling pathway, including but not limited to pain, gastrointestinal disorders, metabolic disorders, and liver disorders, such as alcoholic steatohepatitis or nonalcoholic steatohepatitis (NASH).
Owner:RES TRIANGLE INST

Non-naturally occurring melanocortin analogs with halogenated dphe and various lactam cyclization types for modulating diabetes and / or treating substance use disorders

PCT designated stageWO2026039687A3Metabolism disorderPharmaceutical delivery mechanismMelanocortin 3 receptorDiabetes mellitus
The present technology comprises non-naturally occurring melanocortin analogs or pharmaceutically acceptable salts, solvates, or stereoisomers thereof and compositions comprising the same. The non-naturally occurring melanocortin analogs may be partial agonists of the melanocortin 4 receptor with sub-micromolar or low-nanomolar binding activity. Certain non-naturally occurring melanocortin analogs may also be partial agonists or partial antagonists of the melanocortin 3 receptor.
Owner:ENDEVICA BIO INC

Non-naturally occurring melanocortin analogs with an extended c-terminus for modulating weight gain

PCT designated stageWO2026039698A1Pharmaceutical delivery mechanismCyclic peptide ingredientsMelanocortin 3 receptorMC4 Receptor
The present technology comprises non-naturally occurring melanocortin analogs or pharmaceutically acceptable salts, solvates, or stereoisomers thereof and compositions comprising the same. The non-naturally occurring melanocortin analogs may be full or partial antagonists of the melanocortin 3 receptor with sub-micromolar or low-nanomolar binding activity. Some of the non-naturally occurring melanocortin analogs may also be full or partial antagonists or partial agonists of the melanocortin 4 receptor with sub-micromolar or low-nanomolar binding activity.
Owner:ENDEVICA BIO INC

Non-naturally occurring melanocortin analogs with an expanded cycle for modulating weight loss

PCT designated stageWO2026039611A1Pharmaceutical delivery mechanismCyclic peptide ingredientsMelanocortin 3 receptorPharmaceutical medicine
The present technology comprises non-naturally occurring melanocortin analogs or pharmaceutically acceptable salts, solvates, or stereoisomers thereof and compositions comprising the same. The non-naturally occurring melanocortin analogs may be full agonists of the melanocortin 3 receptor and full or partial agonists of the melanocortin 4 receptor with sub-micromolar or low-nanomolar binding activity.
Owner:ENDEVICA BIO INC

Non-naturally occurring melanocortin analogs with an expanded cycle for modulating diabetes or treating substance use disorders

PCT designated stageWO2026039612A1Pharmaceutical delivery mechanismCyclic peptide ingredientsMelanocortin 3 receptorDiabetes mellitus
The present technology comprises non-naturally occurring melanocortin analogs or pharmaceutically acceptable salts, solvates, or stereoisomers thereof and compositions comprising the same. The non-naturally occurring melanocortin analogs may be partial agonists the melanocortin 4 receptor with sub-micromolar or low-nanomolar binding activity. Certain non-naturally occurring melanocortin analogs may also be partial agonists or partial antagonists of the melanocortin 3 receptor.
Owner:ENDEVICA BIO INC

Cleavable conjugates of TLR7 / 8 agonist compounds, methods for their preparation and use.

Provided are Toll-like receptor 7 / 8 agonist compounds that facilitate local release and / or local retention of the bioactive form of a TLR7 / 8 agonist and reduce an unwanted systemic inflammatory cytokine response. 【Solution means】 Formula (I): F-[W-L 3 -L 2 -L 1 -D]x(I) [wherein, D is a TLR7 / 8 agonist moiety, L 1 is a linking or self-detachable linker, L 2 is a cleavable linker, L 3 is a conjugation linker, W is O, S or NR 10 wherein, R 10 is H or C1-C8 alkyl, x is an integer from 1 to 500, F is a conjugation moiety, and the TLR7 / 8 agonist moiety is a 1H-imidazo[4,5-c]quinoline derivative]. Compounds are provided.
Owner:DYNAVAX TECHNOLOGIES CORPORATION

Compositions and methods for treatment of fragile x syndrome

ActiveUS12527791B2Organic active ingredientsNervous systemCortical inhibition
Disclosed are methods of alleviating or preventing one or more symptoms associated with fragile X syndrome in an individual in need thereof via administration of a therapeutically effective amount of a GABA(A) alpha 2 and / or 3 partial agonist. The one or more symptoms may include impaired functional communication, anxiety, inattention, hyperactivity, sensory reactivity, autonomic nervous system dysregulation, aberrant eye gaze, self-injury, aggression, seizures, EEG abnormalities, including but not limited to, abnormal spectral analysis, event related potentials which may include auditory and visual responses, abnormalities in cortical responses as evoked by transcranial magnetic stimulation including resting and active motor thresholds and abnormal responses in measures of cortical inhibition and excitation, aberrant impaired cognitive function, compromised daily living skills, or a combination thereof.
Owner:CHILDRENS HOSPITAL MEDICAL CENT CINCINNATI

Discovery of a selective 5-HT2c agonist and 5-HT2a partial agonist by generative machine learning

PCT designated stageWO2026085333A1Organic active ingredientsNervous disorderDiseaseTryptamine Receptors
Disclosed are compounds having selectivity towards a serotonin 2 receptor (5-HT2), including 5-HT2A, 5-HT2B, and / or 5-HT2C, including a compound which is formula (I); (N-(2-(lH-indol-2-yl)ethyl)-2-(lH-indol-3-yl)-N-methylethan-1 -amine), or a pharmaceutically acceptable salts of the compounds. Methods and uses of the compounds in treating conditions treatable by agonism of 5-HT2A and / or 5-HT2C, the methods and uses comprising administering a disclosed compound to a subject in need thereof, are also disclosed.
Owner:COLLABORATIONS PHARMACEUTICALS INC

A quaternary ammonium salt type partial agonist of sphingosine-1-phosphate receptor subtype 1

PendingCN122301787AUlcerative colitisReceptor subtype
This invention pertains to the field of inflammatory bowel disease and relates to a quaternary ammonium salt-based locally acting sphingosine 1-phosphate receptor subtype 1 agonist. The compounds, their stereoisomers, and pharmaceutically acceptable salts of this application are locally acting S1PR1 agonists. These compounds exhibit good agonistic activity against sphingosine 1-phosphate receptor subtype 1, are almost not absorbed orally, and have low oral bioavailability. However, they still possess good in vivo anti-ulcerative colitis activity, improving intestinal inflammatory damage in mice with ulcerative colitis, increasing mouse weight, and increasing colon length. Therefore, these compounds, while maintaining in vivo anti-ulcerative colitis activity, can reduce the risk of infection caused by systemic immunosuppression. The structural formula of the sphingosine 1-phosphate receptor subtype 1 agonist is shown in Formula I.
Owner:NANJING YITENG PHARM RES INST CO LTD

Formulation for oral administration of non-naturally occurring melanocortin analogs for treating substance use disorders and / or modulating diabetes

PCT designated stageWO2026080395A1Pharmaceutical delivery mechanismPeptidesMelanocortin 3 receptorDiabetes mellitus
Provided herein are pharmaceutical compositions of non-naturally occurring melanocortin analogs formulated for oral administration. The non-naturally occurring melanocortin analogs may be partial agonists of the melanocortin 4 receptor with sub-micromolar or low-nanomolar binding activity. Certain non-naturally occurring melanocortin analogs may also be partial agonists or partial antagonists of the melanocortin 3 receptor.
Owner:ENDEVICA BIO INC

Non-naturally occurring melanocortin analogs with an n-terminal extension for modulating diabetes and / or treating substance use disorders

PCT designated stageWO2026039709A1Metabolism disorderPharmaceutical delivery mechanismMelanocortin 3 receptorDiabetes mellitus
The present technology comprises non-naturally occurring melanocortin analogs or pharmaceutically acceptable salts, solvates, or stereoisomers thereof and compositions comprising the same. The non-naturally occurring melanocortin analogs may be partial agonists the melanocortin 4 receptor with sub-micromolar or low-nanomolar binding activity. Certain non-naturally occurring melanocortin analogs may also be partial agonists or partial antagonists of the melanocortin 3 receptor.
Owner:ENDEVICA BIO INC

Il-2 muteins and their use

Novel recombinant interleukin-2 (IL-2) proteins are provided. In particular, provided are recombinant IL-2 proteins that are selectively mutated to be partial agonists of IL-2R-based signaling, or to increase IL-2R-based signaling, as compared to wild-type IL-2. The recombinant IL-2 proteins are useful, for example, in applications where fine-tuning one or more IL-2 functions is useful (e.g., in the treatment of autoimmune disease and cancer). Also provided are nucleic acids encoding the recombinant IL-2 proteins, methods of making the recombinant IL-2 proteins, pharmaceutical compositions that include the recombinant IL-2 proteins and methods of treatment using such pharmaceutical compositions.
Owner:THE GOVERNMENT OF THE UNITED STATES OF AMERICA AS REPRESENTED BY THE SECRETARY DEPARTMENT OF HEALTH & HUMAN SERVICES

Non-naturally occurring melanocortin analogs with expanded cycles and / or extended termini and associated uses

PCT designated stageWO2026039708A1Pharmaceutical delivery mechanismCyclic peptide ingredientsMelanocortin 3 receptorMC4 Receptor
Provided herein are non-naturally occurring melanocortin analogs or pharmaceutically acceptable salts, solvates, or stereoisomers thereof and compositions comprising the same. Some melanocortin analogs are full antagonists of the melanocortin 3 receptor and full agonists of the melanocortin 4 receptor with sub-micromolar or low- nanomolar binding activity. Other melanocortin analogs are full or partial antagonists of the melanocortin 4 receptor with no activity, partial agonist activity or full agonist activity on the melanocortin 3 receptor.
Owner:ENDEVICA BIO INC

Non-naturally occurring melanocortin analogs with halogenated DPHE and various lactam cyclization types for modulating diabetes and / or treating substance use disorders

PCT designated stageWO2026039687A2Metabolism disorderPeptide/protein ingredientsMelanocortin 3 receptorDiabetes mellitus
The present technology comprises non-naturally occurring melanocortin analogs or pharmaceutically acceptable salts, solvates, or stereoisomers thereof and compositions comprising the same. The non-naturally occurring melanocortin analogs may be partial agonists of the melanocortin 4 receptor with sub-micromolar or low-nanomolar binding activity. Certain non-naturally occurring melanocortin analogs may also be partial agonists or partial antagonists of the melanocortin 3 receptor.
Owner:ENDEVICA BIO INC

Non-naturally occurring melanocortin analogs with various lactam cyclization types for modulating weight gain

PCT designated stageWO2026039680A1Pharmaceutical delivery mechanismCyclic peptide ingredientsMelanocortin 3 receptorMC4 Receptor
The present technology comprises non-naturally occurring melanocortin analogs or pharmaceutically acceptable salts, solvates, or stereoisomers thereof and compositions comprising the same. The non-naturally occurring melanocortin analogs may be full or partial antagonists of the melanocortin 3 receptor with sub-micromolar or low-nanomolar binding activity. Some of the non-naturally occurring melanocortin analogs may also be full or partial antagonists or partial agonists of the melanocortin 4 receptor with sub-micromolar or low-nanomolar binding activity.
Owner:ENDEVICA BIO INC

Compound and application thereof in reducing risk of magical psychotropic drugs

The invention relates to a compound and application of the compound in reduction of magical risk caused by psychotropic drugs. The invention provides a compound, and a composition of pharmaceutically acceptable salt, racemate, enantiomer, solvate, hydrate, crystal form or eutectic of the compound. The compound is applied to preparation of a medicine for reducing the risk of magical risk caused by psychotropic drugs, and the psychotropic drugs are dimethoxytoluene propylamine. The invention synthesizes a compound which is used as a weak partial agonist of 5-HT2AR, can enhance the activation of DOM and 5-HT on a beta-arrestin2 pathway, has no influence on a G alpha q / 11 pathway, and shows special pharmacological properties.
Owner:ACADEMY OF MILITARY MEDICAL SCIENCES

FGF23 mutant and medicine for preventing or treating acute kidney injury

The invention relates to the technical field of biological medicine manufacturing, in particular to an FGF23 mutant capable of being used for preventing or treating acute kidney injury and a medicine. The FGF23 mutant is a novel FGF23 partial agonist designed by mutating the amino acid site of wild type FGF23. The FGF23 mutant disclosed by the invention can keep the AKI treatment activity and avoid adverse reaction on phosphate metabolism at the same time. Experiments prove that the FGF23 mutant disclosed by the invention shows excellent prevention and treatment effects on acute kidney injury in vivo and in vitro, and has a wide application prospect.
Owner:OUJIANG LAB