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716 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.

Compositions and methods for treating immune thrombocytopenia

ActiveUS12202900B2Pharmaceutical 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)

Methods for treating bullous pemphigoid using fcrn antagonists

Provided herein are methods of treating bullous pemphigoid using an effective amount of a human neonatal Fc receptor (FcRn) antagonist. FcRn antagonists for use in the treatment of bullous pemphigoid and for use in the manufacture of a medicament for the treatment of bullous pemphigoid are also provided herein.
Owner:ARGENX BVBA(BE)

Small molecule prostaglandin f receptor antagonists

Disclosed herein are small molecule prostaglandin F (FP) receptor antagonists, methods of making them, and therapeutic methods using them.
Owner:FERRING BV

Treatment of hyperinsulinemic hypoglycemia with GLP-1 antagonist exendin(9-39)

ActiveUS12220444B2Metabolism disorderPeptide/protein ingredientsBlurred visionPostprandial Hypoglycemia
Treatment of hyperinsulinemic hypoglycemia comprises administration of an effective amount of a glucagon-like peptide-1 receptor antagonist (GLP1RA) alone or in combination with an amylinomimetic agent or any anti-gastric emptying agent. Patients suffering from hyperinsulinemic hypoglycemia after bariatric surgery experience particular benefit, as there is no current method effective for their treatment. Prevention or reduction of acute adverse effects of postprandial hypoglycemia, such as palpitations, tremor, weakness, sweating, confusion, fatigue, blurred vision, seizures, or loss of consciousness, and prevention of chronic adverse effects of hyperinsulinemic hypoglycemia, such as cognitive impairment, can be achieved by treatment with GLP1RA.
Owner:THE BOARD OF TRUSTEES OF THE LELAND STANFORD JUNIOR UNIV

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

Antagonists of the imidazoline-1 receptor for use in the prevention and / or treatment of an autoinflammatory or autoimmune disease

PCT designated stage expiredWO2025002914A1Amine active ingredientsCardiovascular disorderImidazoline receptorAutoimmune condition
The present invention refers to an antagonist of imidazoline-1 receptor (I1R) for use in the prevention and / or treatment of an autoinflammatory or autoimmune disease in a human subject, selected from the group consisting of (±)-2-endo-amino-3-exo- isopropylbicyclo[2.2.1]heptane (synonym: AGN192403), N-benzylguanidine, 2-(2- Fluoro-5-methylphenyl)-4,5-dihydro-1H-imidazole (synonym: S23757), 2-(2-chloro-4-iodo-phenylamino)-5-methyl-pyrroline (synonym: LNP911), 1-(4, 5-dihydro-1H-imidazol- 2-yl)isoquinoline (synonym: BU98008), 5-[2-bromophenoxy)methyl]-4,5-dihydro-1,3- oxazol-2-amine (synonym: S23515), 6-methylamino-2methylheptene (synonym: isometheptene), and 4-chloro-2,3-dihydro-2-oxo-1,3-benzothiazol-3-ylacetic acid (synonym: benazolin). Also, to the use of Imidazole propionate in the diagnosis of an autoinflammatory or autoimmune disease in a subject, and further to a method of diagnosis of atherosclerosis comprising assessing the level of ImP in a blood sample and determining whether said level is above or below a value of 41nM.
Owner:FUNDACION CENT NACIONAL DE INVESTIGACIONES CARDIOVASCULARES CARLOS III (CNIC)

Methods and compositions for treatment of glaucoma and related conditions

Methods, compositions and kits comprising alpha-adrenergic antagonists, such as phentolamine, for the treatment of glaucoma, ocular hypertension, and / or other ocular disorders, such as non-arteritic anterior ischemic optic neuropathy or keratoconus, are provided. Said methods, compositions and kits may further comprise additional therapeutic agents, including prostaglandin analogues such as latanoprost, beta-adrenergic antagonists, alpha-adrenergic agonists, carbonic anhydrase inhibitors, cholinergic agonists, NMDA receptor antagonist, adenosine receptor antagonists, 5-HT2a receptor agonists, or Rho kinase inhibitors.
Owner:OCUPHIRE PHARM INC

Muscarinic acetylcholine m1 receptor antagonists

Provided herein 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

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

Sterile inhalation suspension containing PDE-4 or PDE-3 / 4 inhibitor and preparation method and application thereof

The invention provides a preparation method and application of a suspension containing a PDE-4 or PDE-3 / 4 inhibitor for sterile inhalation. The preparation method comprises the following steps: dispersing a PDE-4 or PDE-3 / 4 inhibitor in injection water containing an excipient, and carrying out high-pressure moist heat sterilization to obtain a PDE-4 or PDE-3 / 4 inhibitor dispersion liquid; dissolving the long-acting beta2-receptor stimulant and / or the long-acting muscarinic receptor antagonist, sterilizing and filtering to obtain a mixed solution; and mixing the PDE-4 or PDE-3 / 4 inhibitor dispersion liquid with the mixed solution, dispersing, and carrying out sterile filling. The medicinal preparation prepared by the invention is a sterile inhalation suspension, and the sterile inhalation suspension containing the PDE-4 or PDE-3 / 4 inhibitor is high in bioavailability, good in patient medication compliance and good in preparation stability.
Owner:LEXENPHARM (SUZHOU) LTD

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)

Novel peptides as selective IL-23 receptor antagonists

The present disclosure relates to peptide IL23 receptor antagonists, pharmaceutical compositions thereof, and medical uses thereof, e.g., for the treatment of inflammatory bowel disease, such as Crohn's disease.
Owner:SANOFI SA(FR)

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

Treatment and management of augmentation in restless legs syndrome

ActiveUS12220404B2BiocidePharmaceutical delivery mechanismDopamine receptor antagonistDopamine
The present invention provides methods of treating Restless Legs Syndrome (RLS) including administering to a subject an effective amount of a dopamine D1 receptor antagonist. Compositions and kits useful for treating RLS are also provided.
Owner:EAST CAROLINA UNIVERSITY

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

Compositions and methods for treatment of chronic pain and depression

Described herein is a composition that includes an N-methyl-D-aspartate receptor (NMDAR) antagonist and a TAS2R receptor response mediating agent for treating neuropathic pain and depression. Methods for treating chronic pain with the described composition are also described.
Owner:JAVITT DANIEL C

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

Application of cannabidiol analogue CIAC001 in preparation of medicine for treating Alzheimer's disease

The invention discloses application of a cannabidiol analogue CIAC001 in preparation of a medicine for treating Alzheimer's disease, and relates to the technical field of medicine. The application comprises the following steps: step 1, medicine extraction: extracting CIAC001, an NMDA receptor antagonist and a cholinesterase inhibitor according to a ratio of 1: 5: 5 into a medicine carrying needle cylinder; 2, medicine heating, wherein a heating assembly is started to conduct pulse heating on the medicine in the medicine carrying needle cylinder; 3, nursing the patient: heating and nursing the injection part of the patient by using a nursing assembly; 4, medicine injection: pushing a pushing head, puncturing a needle into the injection part of the patient, and injecting the medicine into the body of the patient; and 5, observing and treating side reactions: taking down the injection device after the drug reaction is complete, observing the side reaction condition of the patient, and starting a temperature regulator to cool the patient. The medicine activity can be effectively improved, side effects of the medicine on patients are reduced, and therefore the treatment effect of the medicine is enhanced.
Owner:SHANGHAI KEXI PHARM TECH DEV CO LTD +2

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

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