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454 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.

Pharmaceutical composition for preventing and / or treating pain and application thereof

The invention discloses a pharmaceutical composition for preventing and / or treating pain and application thereof.The pharmaceutical composition contains a Sigma-1 receptor antagonist and a histamine H3 receptor antagonist / inverse agonist and has a synergistic analgesic effect on various pains, the curative effect of the pharmaceutical composition is remarkably superior to that of a single drug, the use dosage of the single drug can be reduced, and therefore the side effect of single drug dosage dependence is reduced; good application prospects are realized.
Owner:JIANGSU OCEAN UNIV

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

(R)-3-(3-chloro-5-fluoro-2-((4-(1h-pyrazol-1-yl)-2-methylquinolin-8-yloxy)methyl)phenyl)morpholine derivatives and related compounds as bradykinin (BK) B2 receptor antagonist for treating skin diseases

The invention relates to a compound according to general formula (I), which acts as a bradykinin (BK) B2 receptor antagonist; to a pharmaceutical composition containing one or more of the compound(s) of the invention; to a combination preparation containing at least one compound of the invention and at least one further active pharmaceutical ingredient; and to said compound(s) for use as in a method of treating a skin disorder; eye disease; ear disease; mouth, throat and respiratory disease; gastrointestinal disease; liver, gallbladder and pancreatic disease; urinary tract and kidney disease; disease of male genitale organs and female genitale organs; disease of the hormone system; metabolic disease; cardiovascular disease; blood disease; lymphatic disease; disorder of the central nervous system; brain disorder; musculoskeletal system disease; allergy disorder; pain; infectious disease; inflammatory disorder; injury; immunology disorder; cancer; hereditary disease; or edema.
Owner:PHARVARIS GMBH

Compositions and methods for treating immune thrombocytopenia

PendingUS20250215090A1Pharmaceutical delivery mechanismAntibody ingredientsAgonistImmune thrombocytopenia
A method is disclosed for the treatment of human subjects diagnosed with immune thrombocytopenia (ITP). The method comprises administering to a human subject a human neonatal Fc receptor (hFcRn) antagonist, optionally in combination with standard-of-care ITP treatment. In certain embodiments, the hFcRn antagonist is efgartigimod (ARGX-113). Standard-of-care ITP treatment may comprise administration of corticosteroids, immunosuppressants, and / or thrombopoietin receptor (TPO-R) agonists.
Owner:ARGENX BVBA(BE)

Angiotensin ii type 2 receptor antagonist and use thereof for treating cancerous pain

An angiotensin II receptor antagonist and the use thereof for treating cancerous pain. Specifically, the present invention relates to a compound of formula (IV) or a pharmaceutically acceptable salt, ester, stereoisomer, polymorph, solvate, N-oxide, isotopic label, metabolite or prodrug thereof, and the use thereof for treating cancerous pain, preferably cancerous ostalgia.
Owner:BEIJING TIDE PHARMACEUTICAL CO LTD

Combination therapy of tyrosine kinase inhibitors and activin type 2 receptor antagonists for treatment of pulmonary arterial hypertension (PAH)

Disclosed herein are kits and methods for treating pulmonary arterial hypertension (PAH), the method 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: * an extracellular domain of activin type 2A (ACTR IIA) or activin type 2B receptor (ACTR IIB); and an Fc domain of human immunoglobulin G1 (IgG1). In some embodiments, the tyrosine kinase inhibitor is cellatinib or a pharmaceutically acceptable salt thereof, and the fusion protein is sotasercept.
Owner:GB002 CO LTD

Materials and methods for treating cancer

This document provides methods and materials involved in treating cancer. For example, methods and materials for modulating (e.g., increasing or decreasing) an interleukin-1 (IL-1) signaling pathway (e.g., an IL-1βsignaling pathway) during an adoptive cell therapy (e.g., a chimeric antigen receptor (CAR) T cell therapy) are provided. In some cases, one or more inhibitors of an interleukin-1 receptor antagonist (IL-1RA) polypeptide can be used to increasing IL-1 signaling (e.g., to reduce immunosuppression of the administered cells). In some cases, CAR T cells having a reduced level of an interleukin 1 receptor, type I (IL-1R1) polypeptide can have decreased IL-1 signaling (e.g., to reduce T cell toxicity associated with the administered cells).
Owner:MAYO FOUNDATION FOR MEDICAL EDUCATION & RESEARCH

Preparation method and application of impurity of beta 2 adrenal receptor agonist and M receptor antagonist bifunctional active compound

The invention belongs to the technical field of chemical pharmacy, and particularly relates to a preparation method and application of an impurity of a beta2 adrenal receptor stimulant and M receptor antagonist bifunctional active compound. According to the impurity preparation method of the beta2 adrenal receptor stimulant and M receptor antagonist bifunctional active compound, acetylation of amino is successfully realized by using acetylation reagents such as acetyl chloride and alkali accelerators such as N, N-diisopropylethylamine, then debenzylation is performed through hydrogenation reaction, and the compound shown in the formula I is successfully prepared. Then, through liquid chromatography purification, a high-purity compound as shown in the formula I is obtained, and the raw material medicine as shown in JKN2304 can meet the requirements of reference substances in the research and development process; the technical problem that in the prior art, an impurity synthesis process of a beta 2 adrenal gland receptor agonist and M receptor antagonist bifunctional active compound is lacked is solved.
Owner:XINXIANG HAIBIN PHARMA +1

Muscarinic acetylcholine m1 receptor antagonists

Provided herein, inter alia, are compounds which are useful as antagonists of the muscarinic acetylcholine receptor M1 (mAChR M1); synthetic methods for making the compounds, pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions.
Owner:CONTINEUM THERAPEUTICS INC

Combination of zibotentan and dapagliflozin for the treatment of endothelin related diseases

The present disclosure relates to the endothelin receptor antagonist (ERA) zibotentan in combination with the sodium-dependent glucose cotransporter 2 (SGLT-2) inhibitor dapagliflozin for use in the treatment of certain endothelin related diseases.
Owner:ASTRAZENECA AB

1-((S)-1-(3-chloro-5-fluoro-2-((4-(1h-pyrazol-1-yl)-2-methylquinolin-8-yloxy)methyl)phenyl)ethyl)-imidazolidine-2,4-dione derivatives and related compounds as bradykinin (BK) B2 receptor antagonist for treating skin diseases

The invention relates to a compound according to general formula (I), which acts as a bradykinin (BK) B2 receptor antagonist; to a pharmaceutical composition containing one or more of the compound(s) of the invention; to a combination preparation containing at least one compound of the invention and at least one further active pharmaceutical ingredient; and to said compound(s) for use as in a method of treating a skin disorder; eye disease; ear disease; mouth, throat and respiratory disease; gastrointestinal disease; liver, gallbladder and pancreatic disease; urinary tract and kidney disease; disease of male genitale organs and female genitale organs; disease of the hormone system; metabolic disease; cardiovascular disease; blood disease; lymphatic disease; disorder of the central nervous system; brain disorder; musculoskeletal system disease; allergy disorder; pain; infectious disease; inflammatory disorder; injury; immunology disorder; cancer; hereditary disease; or edema.
Owner:PHARVARIS GMBH

Compositions and methods for treating obesity and diabetes using 15-PGDH inhibitors

Provided herein are methods for treating obesity or diabetes by administering a 15- PGDH inhibitor to a subject. In some cases, the methods provided herein additionally involve administering to a subject an agent selected from the group consisting of: a glucagon- like peptide- 1 (GLP-1) receptor agonist, a glucose-dependent insulinotropic polypeptide (GIP) receptor agonist, a glucagon receptor agonist, a GLP-1 receptor / GIP receptor co- agonist, a GLP-1 receptor agonist / GIP receptor antagonist, a GLP-1 receptor / glucagon receptor co-agonist, a GLP-1 receptor / GIP receptor / glucagon receptor triple agonist, a GLP-1 receptor / GLP-2 receptor co-agonist, a combination of a GLP-1 receptor agonist and an amylin receptor agonist.
Owner:EPIRIUM BIO INC

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

Human growth hormone receptor antagonists and methods of use thereof

PCT designated stage expiredWO2025088605A2Peptide/protein ingredientsReceptors for hormonesDiseaseAcromegaly
Described herein are growth hormone receptor antagonists and modified growth hormone receptor antagonists. The growth hormone receptor antagonists and modified growth hormone receptor antagonists are useful in treating diseases or conditions, such as cancer and acromegaly, that are responsive to human growth hormone receptor antagonists.
Owner:OPKO BIOLOGICS LTD

Polymer conjugates of drugs with central nervous system (CNS) effects and peripheral nmdar blocking activity and / or immune system modulating effects

PendingUS20250302973A1Organic active ingredientsAntipyreticChemical MoietyNervous system
The present invention discloses novel molecules consisting of N-methyl-D-aspartate receptor (NMDAR) antagonists-polymer conjugates having a general structure D-(X-Poly-T)n, wherein D is an high affinity, i.e., (+)-, (−)-, or (±)-dizocilpine, or a low affinity, i.e., (+)-, (−)-, or (±)-methadone, CNS active NMDAR antagonist, n is an integer comprised between 1 and 6. X is a stable (enzymatically and / or hydrolytically under physiological conditions) linker comprising a covalent bond or a chain of atoms that covalently attaches a small molecule NMDAR antagonist drug moiety to the Poly derivative. Poly is a covalently bonded chain of repeating monomer units that form a polymer or an oligomer backbone of synthetic or natural origin. T, if present, is either another molecule of D, or a terminal group of Poly, represented by any suitable chemical group which, depending upon preference, is unreactive or reactive with other chemical moieties, or has a targeting property.
Owner:MGGM LLC

Crystal form of pyrimidine sulfonamide compound and preparation method therefor

Disclosed are a Crystal Form (I) of a pyrimidine sulfonamide compound and a preparation method therefor. The present disclosure relates to an application thereof in the preparation of a medicament for treating diseases related to ETA receptor antagonists.
Owner:WUXI BIOCITY BIOPHARMACEUTICS CO LTD

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

Adrenergic receptor ADRAC2 antagonists

The present application relates to adrenergic receptor ADRAC2 antagonists, to novel substituted heterocyclic carboxamides, to a method for the production thereof, to the use thereof alone or in combination for the treatment and / or prophylaxis of diseases and to the use thereof for producing medicaments for the treatment and / or prophylaxis of diseases, in particular for the treatment and / or prophylaxis of dyspnea, including sleep-induced dyspnea, including sleep-induced dyspnea, including sleep-induced dyspnea, including sleep-induced dyspnea, including sleep-induced dyspnea, including sleep-induced dyspnea. Such as central and obstructive sleep apnea, snoring (primary and obstructive snoring); dysphagia; peripheral and cardiovascular conditions, including diabetic microangiopathy; and peripheral and central nervous system disorders, including neurodegenerative and neuroinflammatory disorders.
Owner:BAYER AG

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

Therapeutic uses of bradykinin b2-receptor antagonists

The invention relates to the treatment of diseases or conditions that are responsive to bradykinin BK B2 receptor modulation. The treatment is preferably a prophylactic and / or chronic treatment and comprises the oral administration of a BK B2 receptor antagonist according to Formula (1), or a salt or solvate thereof, wherein R is deuterium or hydrogen: such as (S)-. / V-(1-deutero-1-(3-chloro-5-fluoro-2-((2-methyl-4-(1-methyl-1 / f-1,2,4-triazol-5-yl)quinolin-8-yloxy)methyl)phenyl)ethyl)-2-(difluoromethoxy)acetamide, by means of an extended-release composition that is adapted to release the BK B2 receptor antagonist over a period of at least 10 hours.
Owner:PHARVARIS GMBH

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

Solid extended-release composition comprising bradykinin b2-receptor antagonists

PendingUS20250228782A1Organic active ingredientsPowder deliveryBradykinin B2 Receptor AntagonistsEthyl group
The invention relates to pharmaceutical matrix tablets for oral administration comprising a bradykinin B2 receptor antagonist having a chemical structure according to Formula (1), or a salt or solvate thereof, wherein R is deuterium or hydrogen: Formula (1) such as (S)-1V-(1-deutero-1-(3-chloro-5-fluoro-2-((2-methyl-4-(1-methyl-1 / / -1,2,4-triazol-5-yl)quinolin-8-yloxy)methyl)phenyl)ethyl)-2-(difluoromethoxy)acetamide. The matrix tablets reliably provide extended release of the bradykinin B2 receptor antagonist which makes them particularly suitable for prophylactic and / or chronic therapies. Therapeutic uses of the matrix tablets are provided.
Owner:PHARVARIS GMBH