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243 results about "Receptor antagonist" patented technology

A receptor antagonist is a type of receptor ligand or drug that blocks or dampens a biological response by binding to and blocking a receptor rather than activating it like an agonist. They are sometimes called blockers; examples include alpha blockers, beta blockers, and calcium channel blockers. In pharmacology, antagonists have affinity but no efficacy for their cognate receptors, and binding will disrupt the interaction and inhibit the function of an agonist or inverse agonist at receptors. Antagonists mediate their effects by binding to the active site or to the allosteric site on a receptor, or they may interact at unique binding sites not normally involved in the biological regulation of the receptor's activity. Antagonist activity may be reversible or irreversible depending on the longevity of the antagonist–receptor complex, which, in turn, depends on the nature of antagonist–receptor binding. The majority of drug antagonists achieve their potency by competing with endogenous ligands or substrates at structurally defined binding sites on receptors.

A process for the preparation of a CGRP receptor antagonist intermediate

The application discloses a method for preparing a CGRP receptor antagonistic intermediate, and belongs to the field of synthesis of medical intermediates. Compound 1 is used as a raw material, reacts with hydroxylamine hydrochloride in an organic solvent to generate an intermediate 2, and then reacts in the presence of a reducing agent to obtain a remikiren intermediate 3. The application is characterized in that a large steric hindrance silicon group is used as the R substituent in the compound 1, so that high stereoselectivity is ensured in the reduction reaction. The key intermediate obtained by using the method has high chiral purity, and the operation is simple, so that the industrial production of the product in the later stage can be realized.
Owner:CHEMVON BIOTECH CO LTD

Tyrosine kinase inhibitor and activin type 2 receptor antagonist combination therapy for treating pulmonary arterial hypertension (PAH)

Disclosed herein are kits and methods for treating pulmonary arterial hypertension (PAH), comprising administering to a subject in need thereof: •a therapeutically effective amount of a tyrosine kinase inhibitor or a pharmaceutically acceptable salt thereof; and•a therapeutically effective amount of a dimeric fusion protein comprising: •the extracellular domain of the activin type 2A (ACTR IIA) or the activin type 2B receptor (ACTR IIB); and the Fc domain of human immunoglobulin G1 (IgG1). In some embodiments, the tyrosine kinase inhibitor is Seralutinib or a pharmaceutically acceptable salt thereof and the fusion protein is Sotatercept.
Owner:GB002 INC

Peptidomimetic compound as well as preparation method and application thereof

The invention discloses a peptidomimetic compound as well as a preparation method and application thereof, and belongs to the technical field of medicinal chemistry. The peptidomimetic compound is shown as a formula I in the specification. The compound can act on the nerve center, has anti-epilepsy and anti-depression effects, can also act on the gastrointestinal tract, inhibits gastric acid secretion or tumor cell growth, is a novel cholecystokinin type 2 receptor antagonist, and has a great application prospect.
Owner:CENTRE FOR REGENERATIVE MEDICINE & HEALTH HONG KONG INSTITUTE OF SCIENCE & INNOVATION CHINESE ACADEMY OF SCIENCES +1

Use of glutamate 2B receptor antagonists and sigma receptor agonists as antitussives

The use of glutamate 2b receptor antagonists and sigma receptor agonists as antitussives to treat or prevent a cough is disclosed. In preferred embodiments, the glutamate 2b receptor antagonist is ifenprodil or radiprodil. Preferred sigma receptor agonists include fluvoxamine, fluoxetine, excitalpram, and donepezil.
Owner:SEYLTX INC

Ntsr1 receptor antagonists or drugs and uses thereof

PendingCN122124049AOrganic active ingredientsNervous disorderDiseaseAlcohol poison
This invention relates to the field of pharmaceutical technology, and discovers that the natural products boldinine and norboldinine can be used as NTSR1 (Neurotensin receptor-1, NTSR1) receptor antagonists and their applications. The compounds are boldinine and norboldinine ((+)-Laurolitsine), which have NTSR1 receptor antagonistic activity and are NTSR1 receptor antagonists that can prevent and treat alcohol poisoning, addiction, schizophrenia, autism spectrum disorder, and mood disorders. Accordingly, this invention can provide novel NTSR1 receptor antagonist prospective compounds with clear targets for the above-mentioned related diseases.
Owner:DALIAN INSTITUTE OF CHEMICAL PHYSICS CHINESE ACADEMY OF SCIENCES

3-((1H-pyrazol-4-yl)methyl)-6′-(phenyl)-2H-(1,2′-bipyridin)-2-one derivatives and related compounds as GPR139 antagonists for use in a method of treatment of e.g. depression

The present invention refers to compounds of formula (I). The present invention also relates to compounds of formula (I) for use as G Protein coupled Receptor 139 (GPR139) antagonists in methods of medical treatment of e.g. depression, Alzheimer's disease, schizophrenia, drug addiction, sleep disorders, pain, and attention deficit hyperactivity disorder. Exemplary compounds are e.g. 3-((1H-pyrazol-4-yl)methyl)-6′-(phenyl)-2H-(1,2′-bipyridin)-2-one derivatives and related compounds. The present description discloses the synthesis and characterisation of exemplary compounds, pharmacological data thereof, as well as exemplary tablet formulations comprising the compounds of the invention (e.g. page 83 to page 110; examples 1 to 33; reference example 1; test examples 1 and 2; tables 1 to 4).
Owner:TAKEDA PHARMA CO LTD

Sofalcone derivatives and pharmaceutical uses thereof

A series of sofalcone derivatives are provided.SOLUTION: A series of sofalcone derivatives provided by the present invention are, for example, compounds having a structure of formula (I), and have platelet aggregation inhibitory and antithrombotic effects. The sofalcone derivatives of the present invention are TxA2 receptor antagonists, have an inhibitory effect on platelet agglutination, and do not easily affect the hemostatic function. The present invention also provides a method for preparing the sofalcone derivative, and a method for using the sofalcone derivative for preventing or treating thrombotic diseases, or for inhibiting platelet aggregation.SELECTED DRAWING: None
Owner:KAOHSIUNG MEDICAL UNIVERSITY

Glp-1r antagonism to improve nutrition following gastrointestinal surgery

Methods of improving nutrition in subjects, including individuals who have undergone gastrointestinal surgery, by avexitide therapy are disclosed. Avexitide may be administered subcutaneously or intravenously as a part of a liquid pharmaceutical formulation. Avexitide therapy may improve weight and / or nutritional intake / status in subjects.
Owner:THE BOARD OF TRUSTEES OF THE LELAND STANFORD JUNIOR UNIV +1

Bicyclic aryl or heteroaryl derivative as Kappa receptor antagonist and composition and application thereof

The present invention relates to a pyridino aryl or heteroaryl derivative having a Kappa receptor antagonistic activity. In particular, the present invention relates to a compound represented by general formula (IV) or general formula (VII), a stereoisomer thereof, a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable salt of the stereoisomer. The invention also relates to a pharmaceutical composition containing the compound, a preparation method of the pharmaceutical composition, and a treatment method and application of diseases related to the antagonistic activity of the Kappa receptor, such as depression, depression with pleasant sensation deficiency, bipolar affective disorder, anxiety and other mental diseases. Wherein each substituent in the general formula (IV) or the general formula (VII) is as defined in the specification.
Owner:NHWA PHARMA CORPORATION

Application of 5-HT3 receptor antagonists in the preparation of antitumor drugs

This invention belongs to the field of medical technology, and specifically relates to the application of serotonin 3 receptor antagonists in the preparation of antitumor drugs. This invention, through research, demonstrates for the first time that serotonin 3 receptor antagonists can inhibit the activity of tumor cells resistant to third-generation EGFR-TKIs. More importantly, serotonin 3 receptor antagonists can not only reverse HER2 S310F mutation-mediated resistance to third-generation EGFR-TKIs, but also reverse secondary resistance to third-generation EGFR-TKIs, thus enabling their use as antitumor drugs for patients resistant to third-generation EGFR-TKIs. The combined use of serotonin 3 receptor antagonists and third-generation EGFR-TKIs exhibits a significant synergistic effect in inhibiting the proliferation of lung adenocarcinoma cells, with minimal toxic side effects on liver and kidney function, providing an effective treatment strategy for clinically reversing third-generation EGFR-TKI resistance and improving the treatment efficacy of NSCLC.
Owner:TIANJIN TUMOR HOSPITAL

C5ar inhibitor reduction of urinary scd163

PendingEP4671767A2Organic active ingredientsAntipyreticSoluble cd163Vasculitis
Provided herein are methods of treating ANCA-associated vasculitis (AAV) in individuals in need thereof comprising administering a complement component 5a receptor (C5aR) antagonist. Also provided herein are methods of treating a ANCA-associated vasculitis (AAV) with renal involvement in an individual in need thereof comprising administering a complement component 5a receptor (C5aR) antagonist to the individual if the individual exhibits an elevated urinary soluble CD163 (sCD163) to creatinine ratio compared to individuals without AAV. In some embodiments, the complement component 5a receptor (C5aR) antagonist is avacopan.
Owner:CHEMOCENTRYX INC

Therapeutic agent for autism spectrum disorder

To provide a more effective medicine for treating ASD.SOLUTION: A therapeutic agent for autism spectrum disorder, comprising an oxytocin receptor agonist as an active ingredient, wherein the therapeutic agent is administered in combination with a vasopressin 1a receptor antagonist. A therapeutic agent for autism spectrum disorder, comprising an oxytocin receptor agonist as an active ingredient, wherein the therapeutic agent is administered in combination with a vasopressin 30IU receptor antagonist. A therapeutic agent for autism spectrum disorder, wherein the oxytocin-receptor agonist is not agonistic to the vasopressin 1a receptor; a pharmaceutical composition for the treatment of autism spectrum disorder, wherein the pharmaceutical composition comprises an oxytocin-receptor agonist and a vasopressin 1a receptor antagonist as active ingredients; a pharmaceutical composition for the treatment of autism spectrum disorder, wherein the oxytocin-receptor agonist is not agonistic to the vasopressin 30IU receptor; and a pharmaceutical composition for the treatment of autism spectrum disorder, wherein the vasopressin-receptor antagonist is SR49059. 1a.SELECTED DRAWING: None
Owner:HAMAMATSU UNIV SCHOOL OF MEDICINE

Composition, cell culture and application of composition in differentiation of human pluripotent stem cells to myocardial cells and / or construction of human heart organoid

The invention provides a composition, cell culture and application of the composition in differentiation of human pluripotent stem cells to myocardial cells and / or construction of human-derived heart organoid, and belongs to the technical field of cell engineering. The invention provides a composition. The composition comprises a fatty acid receptor antagonist, a fatty acid synthetase inhibitor and a fatty acid oxidation activator. The composition provided by the invention can regulate cell metabolism, breaks through the contradiction that the proliferation capacity and the cell maturity cannot be obtained at the same time in the traditional technology, can maintain the myocardial cells in a proliferation stage, and obtains the myocardial cells with relatively mature structures and functions, and the contractility of 3D heart organs constructed by the myocardial cells is greatly improved. The invention provides a high-quality cell source for myocardial regeneration treatment, high-throughput drug cardiotoxicity screening and heart disease mechanism research, and has remarkable clinical application value and industrialization prospect.
Owner:HUBEI UNIV

Methods of using interleukin-23 receptor antagonists

The present invention relates to methods of administering a cyclic peptide inhibitor of the interleukin-23 receptor (IL-23R) or pharmaceutically acceptable salt or solvate forms thereof, corresponding compositions, assays, methods, and / or uses for treatment of psoriasis.
Owner:JANSSEN PHARMA NV

Special blood filtration replacement liquid for anticoagulation

The invention discloses blood filtration replacement liquid as well as a preparation method and application thereof. The displacement liquid comprises low molecular weight heparin calcium, prostaglandin E1, prostacyclin, electrolyte with specific concentration, glucose and an interleukin-1 receptor antagonist. The preparation method comprises the following steps: weighing the raw materials according to the proportion, dissolving to a constant volume, removing pyrogen and heat, and carrying out aseptic packaging. During clinical application, replacement liquid and blood are filtered according to the replacement rate of 1: 1-2: 1 according to the condition of a patient, 4-6 hours each time and 2-3 times each week, and related indexes are monitored. Animal tests show that the replacement liquid has good safety under the effective dosage, and has potential influence on part of organs under the high dosage. A stability test shows that the compound can be stably stored under a certain condition. The invention provides the replacement liquid which can achieve anticoagulation and blood vessel protection, maintain electrolyte balance and relieve inflammatory response, is expected to improve the prognosis of hemodialysis patients, and has important clinical significance and wide application prospects.
Owner:HUAREN PHARMACEUTICAL CO LTD +3

Use of glutamate 2B receptor antagonists and sigma receptor agonists as antitussives

The use of glutamate 2b receptor antagonists and sigma receptor agonists as antitussives to treat or prevent a cough is disclosed. In preferred embodiments, the glutamate 2b receptor antagonist is ifenprodil or radiprodil. Preferred sigma receptor agonists include fluvoxamine, fluoxetine, excitalpram, and donepezil.
Owner:SEYLTX INC

Small molecules as acaricidal kinin receptor antagonists or mosquitocidal agents

Methods and compositions for controlling, treating, preventing, or ameliorating arthropod infection are provided. Compositions can comprise one or more active agents of small molecules antagonists of arthropod kinin receptor. Methods of preventing disease development and infestation by arthropods are disclosed as well as methods of making, using, and producing such compositions.
Owner:TEXAS A&M UNIVERSITY

Peripheralization of centrally-acting cannabinoid-1 receptor antagonists by nanoparticles for the treatment metabolic related conditions

PendingUS20250367134A1Organic active ingredientsLiposomal deliverySelective modulationNanoparticle
The technology includes selective modulation of only a peripheral CB1R by using a CB1R antagonist contained in a peripherally restricted delivery system.
Owner:YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERUSALEM LTD

Method for synthesizing high-optical-purity five-membered lactam skeleton bulk drug through rhodium catalysis

The invention discloses a method for synthesizing a five-membered lactam skeleton bulk drug with high optical purity under the catalysis of rhodium, which is characterized in that racemic and cheap gamma-substituted alpha, beta-unsaturated gamma-lactam is used as a raw material, a dicyclooctene hydroxyl rhodium (I) dimer is used as a catalyst, a cheap chiral phosphine ligand is used as a ligand, and the raw material is synthesized by a one-step method. The high enantioselectivity arylation reaction with arylboronic acid is realized. According to the method, the optical purity limit of a traditional route is successfully broken through, the specific rotation of the obtained trans-beta, gamma-disubstituted gamma-lactams with three single configurations is remarkably higher than the highest value in the literature, and a high-enantioselectivity key synthesis building block is provided for synthesis of a protein kinase C regulator, a glutamate receptor antagonist and CGN-10100. The method provided by the invention is simple and easy to operate, mild in reaction condition, high in yield and strong in derivation ability, and provides a new method for efficient and high-enantioselectivity preparation of chiral bulk drugs.
Owner:YULIN UNIV

Seltorexant for use in treating major depressive disorder with insomnia symptoms

PCT designated stageWO2025242852A1Organic active ingredientsNervous disorderHuman patientRecurrent major depressive episodes
The disclosure provides methods for stratifying human patients with MDD in order to identify a human patient with MDD with insomnia symptoms (MDDIS) where such patients can benefit from treatment with an orexin-2 receptor antagonist, such as seltorexant.
Owner:JANSSEN PHARMA NV

Multicyclic TLR7 / 8 antagonists and their use in the treatment of immune disorders

The present invention relates to compounds of formula (I) and pharmaceutically acceptable compositions thereof useful as toll-like receptor 7 / 8 (TLR7 / 8) antagonists.SOLUTION: In Formula (I), ring A is aryl or heteroaryl; ring B is aryl or heteroaryl; and X is C (R4) 2, O, NR4, S, S (R4), or S (R4) 2.SELECTED DRAWING: None
Owner:MERCK PATENT GMBH

P2x7 receptor antagonists

Described herein are compounds of formula (I), where the substituents are disclosed herein, and exhibit antagonistic and / or inhibitory activity against the P2X7 receptor. These compounds, and their pharmaceutically acceptable salts, hydrates, solvates, and compositions thereof, are suitable for use in the prevention and treatment of diseases and conditions modulated by inhibition of the P2X7 receptor.
Owner:BREYE THERAPEUTICS APS

Application of growth hormone releasing peptide Ghrelin receptor in itching intervention

The invention relates to the technical field of medicines, in particular to application of a growth hormone releasing peptide Ghrelin receptor in itching intervention. By adjusting the activity of the receptor, the invention provides a new strategy for intervening pruritus: activation of the Ghrelin receptor can be used for inducing pruritus so as to construct a disease model; and inhibiting the Ghrelin receptor is used for preventing or treating pruritus, and the pruritus comprises acute pruritus and chronic pruritus. In specific implementation, the inhibition of the receptor is realized by applying the Ghrelin receptor antagonist, and the activation of the receptor is realized by applying the Ghrelin receptor agonist. Therefore, by targeting the Ghrelin receptor, controllable induction and efficient inhibition of pruritus are realized, mechanism innovation, treatment practicability and conversion feasibility are integrated, and a breakthrough strategy is provided for prevention and treatment of pruritus-related diseases.
Owner:FOURTH MILITARY MEDICAL UNIVERSITY

Nitrogen-containing spirocyclic compound, preparation method therefor and use thereof

Disclosed are an orexin receptor antagonist and the use thereof. Specifically disclosed are a compound represented by formula (I), and a stereoisomer, tautomer, crystal form, pharmaceutically acceptable salt, hydrate, solvate or prodrug thereof. The compound is an orexin receptor antagonist, and can be used for preparing a drug for treating and / or preventing orexin-related diseases.
Owner:AXTER THERAPEUTICS BIOPHARMACEUTICAL(TIANJIN) CO LTD

Compounds for use as apelin receptor antagonists

The present invention relates to synthetic polypeptide compounds which bind to a class A G-protein-coupled receptor, the Apelin receptor. These compounds may act as apelin receptor antagonists. These compounds and compositions comprising them may be useful in the treatment of diseases, such as cancer.
Owner:CAMBRIDGE ENTERPRISE LTD

Combination pharmacological interventions for multiple mechanisms of obstructive sleep apnea

PendingUS20260083709A1Organic active ingredientsPharmaceutical delivery mechanismNorepinephrine reuptake inhibitorPharmacological interventions
In general, the invention relates to pharmaceutical compositions comprising a norepinephrine reuptake inhibitor (NRI), muscarinic receptor antagonist, and carbonic anhydrase inhibitor and methods of treating Sleep Apnea comprising the administration of these pharmaceutical compositions.
Owner:THE BRIGHAM & WOMEN S HOSPITAL INC

Application of Vietnam ginseng saponin R18

The invention discloses an application of Vietnam ginseng saponin R18. According to the invention, a Ca < 2 + > biosensor is utilized to co-transfect Hela cells with MRGPRX4, the activation effect of Vietnam ginsenoside R18 on MRGPRX4 is detected, and the Vietnam ginsenoside R18 is confirmed to be an agonist of MRGRPX4. The Vietnam ginsenoside R18 acts on a mouse through subcutaneous injection to cause itching of the mouse, so that the Vietnam ginsenoside R18 can be used as a tool medicine for studying itching and is used for screening a G protein coupled receptor antagonist with an itching relieving effect or preparing an itching causing model; the traditional Chinese medicine quality is controlled, and the itching side effect of the traditional Chinese medicine is prevented.
Owner:JINAN UNIVERSITY