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369 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

(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

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

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

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

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

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

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

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

CGRP receptor antagonists for treatment of chemotherapy-induced nausea and vomiting (CINV)

PendingCN120379667AOrganic active ingredientsInorganic active ingredientsCGRP receptorNeuropeptide AF
Nausea and vomiting are unpleasant events caused by a variety of triggering factors. Wherein medicines often cause nausea and vomiting. An anti-tumor chemotherapeutic agent is one of the most emetic drugs, and often causes chemotherapy-induced nausea and vomiting (CINV). The latter seriously impairs the therapeutic effect and the quality of life of the patient. It is of great interest in determining agents capable of preventing and combating drug-induced nausea and vomiting, including CINV. A calcitonin gene-related peptide (CGRP) is a neuropeptide having various effects in a human body. However, neuropeptide effects in the brain are still to be clarified. CGRP receptor antagonists (named as gezepam) have been recently approved for use in the treatment of migraine. The use of gezepams for the direct treatment of nausea and vomiting, including CINV, is described.
Owner:DRUGS MINERALS & GENERICS ITAL S R L IN FORMA ABBREVIATA D M G ITAL SRL

BRS-3 antagonist and application thereof in treating and / or preventing myocardial cell injury related diseases

The invention discloses a BRS-3 antagonist and application thereof in treating and / or preventing myocardial cell injury related diseases, and belongs to the field of biological medicine. It is found for the first time that licoflavone A and saikoside B2 can antagonize calcium ion (Ca < 2 + >) influx induced by a BRS-3 specific agonist MK5046 in a dose-dependent mode, and it is revealed that licoflavone A and saikoside B2 can serve as BRS-3 receptor antagonists to play a role. According to the application, an oxidative stress environment is simulated through hydrogen peroxide to explore the influence of licoflavone A of a BRS-3 receptor on myocardial cell activity, it is found for the first time that licoflavone A and bantag-1 can relieve myocardial cell injury caused by H2O2 by antagonizing BRS-3, it is revealed that the BRS-3 receptor possibly becomes a treatment target of myocardial injury caused by oxidative stress, and the application has a wide application prospect. The antagonist can be used for preparing medicines or health-care foods for treating or preventing myocardial cell injury related diseases.
Owner:SHANGHAI JIAOTONG UNIV

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

Quinazolinone 5-HT2A receptor antagonist as well as preparation method and medical application thereof

The invention discloses a quinazolinone 5-HT2A receptor antagonist or agonist compound as shown in a formula I, pharmaceutically acceptable salts of the quinazolinone 5-HT2A receptor antagonist or agonist compound as well as a preparation method and medical application of the quinazolinone 5-HT2A receptor antagonist or agonist compound and the pharmaceutically acceptable salts. The quinazolinone 5-HT2A receptor antagonist or agonist compound is a powerful 5-HT2A receptor antagonist and has potential anti-mental disease activity.
Owner:ACADEMY OF MILITARY MEDICAL SCIENCES

Human umbilical cord composition for treating Petroleum disease

A treated human umbilical cord composition for use in the treatment of Perony's disease by in vivo injection in a subject in need thereof using an effective amount of the composition. The composition comprises a water-based human umbilical cord filtrate, wherein endogenous hyaluronic acid (HA) and / or hyaluronic acid, fibronectin, insulin growth factor binding protein-1 (IGFBP-1), sulfated glycosaminoglycan (sGAG), exosomes, interleukin-1 receptor antagonist (IL-1ra), hepatocyte growth factor (HGF), transthyretin, metalloproteinase tissue inhibitor 1 (TIMP-1), and / or a pharmaceutically acceptable salt thereof in an amount effective to reduce the size of Pteroid disease plaques. The present invention relates to an aggregation glycan, or a combination thereof.
Owner:BIOSTEM TECHNOLOGIES INC

Method for synergistic enhancement of remyelination via modulation of RXR and a heterodimeric partner

PendingUS20250319078A1Nervous disorderAmide active ingredientsDiseaseRetinoid X receptor gamma
Disclosed herein are methods and compositions for treating a demyelinating disease, such as multiple sclerosis, by administering to a subject suffering from the disease at least one Retinoid X receptor gamma (RXRy) agonist and at least one member selected from a Liver X Receptor (LXR) antagonist, CYP51 inhibitor, TM7SF2 inhibitor, EBP inhibitor, and combinations thereof.
Owner:LAIRSON LUKE L +2

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