48 results about "Receptor antagonist" patented technology

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.

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.

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.

Described herein are EphA4 receptor antagonists, pharmaceutical compositions containing EphA4 antagonists, and methods and uses of treating an EphA4-based disease, disorder or pathology in an individual using EphA4 receptor antagonists.

Provided herein include compounds, compositions, kits and methods for preventing and treating psychiatric disorders. The composition and methods described herein can prophylactically treat a subject prior to and / or after a stressor and / or prior to the recurrence of a stressor, thereby preventing or delaying a relapse of depression or depression-like and / or stress-induced behaviors and disorders. The composition can comprise a serotonin 4 receptor (S-HUR) agonist and an N- methyl-D-aspartate (NMDAR) antagonist and a pharmaceutically acceptable salt, analog, derivative or metabolite thereof.

The present disclosure provides methods of treating lung cancer by administering A2a receptor antagonists. In particular, these methods include monotherapy as well as combination therapy with checkpoint inhibitors and / or radiotherapy.

Provided is a compound represented by formula (1) or a pharmaceutically acceptable salt thereof (in formula (1), Ar is formula (Ar1) or (Ar2), and in these formulas, R1 and R2 each independently denote an alkyl, a haloalkyl, or a halogen, each R3 independently denotes an alkyl, a haloalkyl, a halogen, an alkoxy, or a haloalkoxy, and m is an integer of 0-3).

This invention relates to the application of AMPA receptor antagonists in the preparation of drugs for treating peritoneal metastases of gastric cancer, belonging to the field of biomedical technology. This invention discloses the application of GRIA2 as a drug target in the preparation of drugs for the prevention or treatment of peritoneal metastases of gastric cancer. It discloses the use of AMPA receptor antagonists NBQX and / or Selurampanel in the preparation of drugs for the prevention or treatment of peritoneal metastases of gastric cancer. NBQX and Selurampanel can significantly inhibit the migration, invasion, spheroidization ability, and adhesion to mesothelial cells of gastric cancer cells; in vivo experiments have confirmed that AMPA receptor antagonists can significantly reduce tumor burden and the number of metastatic nodules in a mouse model of peritoneal metastases of gastric cancer. Patient-derived organoid xenograft models further demonstrate that AMPA receptor antagonists have significant efficacy against peritoneal metastases of gastric cancer with high GRIA2 expression. This invention provides a new treatment strategy for peritoneal metastases of gastric cancer.

This invention provides a method for treating postoperative nausea and vomiting using buccal acupuncture combined with a triple antiemetic regimen. The method employs a combined intervention of buccal acupuncture and a triple antiemetic regimen. The triple regimen consists of a 5-HT3 receptor antagonist, a glucocorticoid, and a dopamine receptor antagonist, administered intravenously in two separate doses. The buccal acupuncture uses CA-2 (upper jiao), CA-3 (middle jiao), and CA-4 (lower jiao) as core acupoints, with auxiliary and reinforcing acupoints added based on the surgical site and high-risk groups. A standardized procedure of pecking stimulation is applied, along with a corresponding postoperative remedial antiemetic medication regimen. This invention organically combines multi-target drug blockade with buccal acupuncture's visceral regulation, synergistically enhancing the antiemetic effect, reducing the incidence of nausea and vomiting, and decreasing the need for remedial medication. The regimen is highly standardized, widely adaptable, and can meet the postoperative nausea and vomiting control needs of various surgeries and high-risk groups. It exhibits good safety, strong repeatability, and high clinical application value.

The present disclosure provides a compound of formula I or its pharma- ceutically acceptable salts, complexes, hydrates, solvates, tautomers, polymorphs, stereoisomers, racemates, and pharma- ceutically active derivatives thereof. The compound of formula I acts as an antagonist to adenosine receptors. The present disclosure also provides processes for the preparation of the compound of formula I and its pharmaceutical compositions. TIFF2024507022000440.tif50163

The present invention relates to a NMDA receptor antagonist and a use thereof. The NMDA receptor antagonist of the present invention is a compound of formulas II and III below, or a pharmaceutically acceptable salt, an enantiomer, a diastereomer, a tautomer, a solvate, an isotopic substituent, a polymorphic substance, a prodrug or a metabolite thereof. The present invention also provides a pharmaceutical composition comprising these compounds, and a use of these compounds in treating or preventing NMDA receptor-mediated diseases.

The present invention relates to adamantanyl-substituted benzamide compounds and their use as antagonists of the P2X7 purinoreceptor. The invention further relates to methods for the treatment of disease and conditions associated with the P2X7 purinoreceptor.

The disclosure relates generally to improvements in the treatment of pruritus, atopic dermatitis (AD), and associated symptoms with tradipitant. More particularly, it relates to a method for increasing the likelihood of achieving optimal therapeutic response in the treatment of an AD patient, where the AD patient is one for whom a potential therapy of choice may include the administration of an amount of an NK-1 antagonist, e.g. tradipitant effective to treat the patient's AD.

An N-formamidopyrazoline derivative is a compound having General Formula (I) or an enantiomer, a diastereomer, an epimer and a racemate thereof, or a pharmaceutically acceptable salt thereof. The compound is an antagonist of a ligand-gated non-selective cation channel receptor subtype P2X3, and can be used for treating or preventing various diseases mediated by the receptor P2X3.

A compound having the following formula (I): wherein groups R1 and R2 independently represent functional groups selected from hydrogen and aliphatic chains; R3 represents a functional group selected from hydrogen and methyl; R5 represents a functional group selected from hydrogen, methyl, and methylene; R6 represents a functional group selected from hydrogen, methyl, methylene, ethyl, and ethylene; and wherein group Q is a carborane substituent having the following molecular formula: C2B 10 H 11 R7; where R7 represents a functional group selected from hydrogen and aliphatic chains; or a pharmaceutically acceptable derivative thereof, which is used as a drug.

This application discloses a tissue fluid extraction device, relating to the field of health monitoring technology. The device includes an alternating current source and electrodes. The output terminal of the alternating current source is connected to the electrodes and is used to output a preset number of predetermined alternating current signals to the electrodes at preset time intervals. The preset time interval is greater than 0, and the preset number of signals is greater than or equal to 2. The electrodes are used to apply electrical stimulation corresponding to the alternating current signal output by the alternating current source to the tissue fluid extraction site, causing the tissue fluid to be released at the extraction site under electrical stimulation. This tissue fluid extraction device enables non-invasive tissue fluid extraction.

A tartrate salt of an ORL-1 receptor antagonist of the formula: wherein R1 is fluoro or chloro; R2a and R2b are each hydrogen or are each fluoro; R3 is hydrogen, methyl, hydroxymethyl, or (C-1-C3) alkoxymethyl; R4 is selected from the group consisting of fluoro, chloro, cyano, cyanomethyl, (C1-C3) alkyl, cyclopropyl, hydroxymethyl, methoxy, cyclopropylmethoxy, am inocarbonylmethoxy, (C1-C3) alkoxymethyl, cyclopropyloxymethyl, cyclopropylmethoxymethyl, 1-hydroxy-1-methylethyl, aminocarbonyloxymethyl, methylaminocarbonyloxymethyl, dimethylaminocarbonyloxymethyl, aminocarbonyl, aminocarbonylmethyl, -CH2-NR5R6, hydroxyimine, methoxyimine, morpholin-4-yl, morpholin-4-ylmethyl, Art, -CH2Ar1, tetrahydrofuran-2-yl, 3-oxomorpholin-4- ylmethyl, 2-oxopyrrolidin-1-ylmethyl, and 2-oxopiperidin-l-ylmethyl; R5 is hydrogen, C1-C3 alkyl, cyanomethyl, -C(O)CH3, or aminocarbonylmethyl; R6 is hydrogen or methyl; and Ar1 is a moiety selected from the group consisting of imidizol-l-yl, imidizol-2-yl, 2-methyl imidizol-1 -yl, pyrazol- 1 -yl, 1,2,3-triazol-1 -yl; 1,2,3-triazol-2-y1; 1,2,4 triazol-1 - yl, isoxazol-3-yl, oxazol-5-yl, and 3-methyl-1,2,4-oxadiazol-5-y1; and methods for its preparation are described.

The present application provides a combination product for the treatment and / or prevention of psychiatric and / or neurological disorders. The combination product comprises (i) a compound which promotes neurogenesis and has hallucinogenic and / or psychedelic side effects, and (ii) a 5-HT2A receptor antagonist which alleviates and / or removes the hallucinogenic and / or psychedelic side effects caused by the first compound.

The present invention relates to novel 1,4-substituted piperidine compounds of formula (I) having P2X7 receptor (P2X7) antagonistic properties, pharmaceutical compositions containing these compounds, chemical processes for preparing these compounds, and their use in the treatment or prevention of diseases associated with P2X7 receptor activity in animals, particularly humans.

The present invention provides fusion proteins comprising an interleukin-1 receptor antagonist (IL-1Ra) and an extracellular matrix (ECM)-binding peptide that specifically binds to one or more or all of the extracellular matrix proteins selected from the group consisting of fibrinogen, fibronectin, vitronectin, tenascin-C, and heparan sulfate, and uses of the fusion proteins to treat conditions in which IL-1Ra administration is beneficial or in which IL-1Ra signaling needs to be attenuated, to enhance tissue regeneration, in particular bone regeneration and / or wound repair, or to treat wounds, burns, and disorders of muscle, cartilage, tendon, and bone, to enhance the regenerative activity of growth factor administration, or to reduce inflammation or hyposensitivity of cells to growth factor stimulation.

The application discloses a method for preparing a pyrrole amide compound and an intermediate thereof. The pyrrole amide compound and / or the intermediate thereof can be used for preparing a pyrrole amide compound used as a salt corticoid receptor antagonist. In particular, the preparation method provided by the application is mild in conditions, simple in operation, safe and controllable, high in yield, and suitable for industrial production.

The application provides an application of an IL-36gamma inhibitor or a receptor antagonist thereof in preparation of a drug for treating osteoporosis. The application finds that, among inflammatory factors in the interleukin-1 family, IL-36gamma has an influence on osteoporosis, IL-36gamma secreted by bone marrow neutrophils in old diabetic mice is increased, binding with a surface receptor IL-36R of BMSC causes weakening of osteogenic differentiation of the BMSC, and leads to osteoporosis; and further, the effect is verified by designing an IL-36gamma inhibitor or a receptor IL-36R antagonist. Therefore, the application provides a new strategy for treating diabetes-related osteoporosis.

This invention belongs to the interdisciplinary field of tumor immunotherapy and gene delivery, specifically relating to an aromatic hydrocarbon receptor blocking functional lipid nanoparticle, its preparation method, and its application. The ionizable lipid derived from the aromatic hydrocarbon receptor antagonist has the structure shown in formula (1): Formula (1), where x is an integer between 10 and 16, X is -N(Me)2 or -OH, and n = 0 or 1. This invention designs and synthesizes aromatic ionizable lipids that combine AHR antagonistic activity and nucleic acid delivery capability, constructing a functionalized LNP vector integrating AHR antagonism, nucleic acid delivery, and macrophage targeting. This vector can efficiently transfect macrophages in vivo and express CAR, while simultaneously blocking the AHR pathway in situ to reverse immunosuppression, enhancing antigen presentation, and activating T cell immunity. This fundamentally solves the core problem of the limited efficacy of existing CAR-M in vivo editing technology in solid tumors, especially gliomas.

The invention relates to compositions and methods for treating cancer in a patient comprising subcutaneously administering a PD-1 antagonist, e.g., an anti-PD-1 antibody (e.g. pembrolizumab), or antigen binding fragment thereof, with or without hyaluronidase every six weeks, in specific amounts to the patient. In specific embodiments, the amount of anti-PD-1 antibody, or antigen binding fragment thereof, is about 600 mg to about 1000 mg. In specific embodiments, the administration occurs about every three weeks, and the amount of anti-PD-1 antibody, or antigen binding fragment thereof, is about 300 mg to about 500 mg. In certain embodiments, the PD-1 antagonist is pembrolizumab, or an antigen binding fragment thereof. Also provided are compositions and kits formulated for subcutaneous administration comprising a particular dosage of an anti-PD-1 antibody, or antigen-binding fragment thereof, and uses thereof for treating cancer.

Provided are an interleukin receptor antagonist and an application thereof, and specifically provided is a compound represented by formula (I) or a pharmaceutically acceptable salt thereof. The provided compound exhibits potent biological activity and good pharmacokinetic properties, or demonstrates good efficacy in animal pharmacodynamic studies. c[X4-X5-X6-X7-X8-X9]-X10-X11-X12-X13-X14-X15-X16 (I)

This invention relates to a compound containing an azobenzene structure or a pharmaceutically acceptable salt, cis-trans isomer, tautomer, solvate, polymorph, or prodrug thereof; the compound provided by this invention is based on the original adenosine A... 2A Based on the structure of receptor antagonists, an azobenzene structure is introduced, making adenosine A... 2A Receptor antagonists possess light-controlled switching properties, and the compounds of this invention can act as adenosine A. 2A Receptor antagonists applied to adenosine A 2A In receptor-mediated diseases, the light-controlled switching properties of the compounds provided by this invention enable them to achieve local efficacy through light irradiation after systemic administration. Some compounds provided by this invention exhibit a fourfold increase in antagonistic activity under specific wavelengths of light irradiation, while others exhibit a fourfold decrease in antagonistic activity under specific wavelengths of light irradiation. In in vivo animal experiments, compound 1 provided by this invention significantly increases the motor ability of mice after light irradiation.

Disclosed herein are compositions and methods for treating arthritis (e.g., osteoarthritis or rheumatoid arthritis) in a subject. The methods provided herein include intra-articular administration to a subject in need thereof using a composition comprising one or more nucleic acids that collectively encode an interleukin-1 receptor antagonist (IL-1Ra) polypeptide and an FGF18 polypeptide. Adeno-associated virus (AAV) viral genomes and particles carrying such nucleic acids and uses thereof are further described.

A pathway modulator, a pharmaceutical composition containing the same, uses thereof and a treatment method using the same. The pathway modulator (including one or more of dopamine beta-hydroxylase inhibitors, receptor agonists and receptor antagonists) can inhibit the occurrence and development of autoimmune diseases through immunomodulation, and thus can provide a potential therapeutic drug for the treatment of autoimmune diseases.

The present invention is directed to somatostatin receptor antagonist compounds having the structure of Formula I: RN I R11 NH *1 R9 O N R10 N *3 R3 *2 R8 L O o N NRR11 RO *7 O*8 N R6 R4 R15 ,N *5 N*6 N R13 n° R5 Formula I, , compositions comprising the same, and methods of using such compounds and compositions. The compounds may be useful in the prevention or treatment of hypoglycemia. 20 24 21 96 10 11 S ep 2 02 4 S O M A T O S T A T I N R E C E P T O R A N T A G O N I S T C O M P O U N D S A N D M E T H O D S O F U S I N G T H E S A M E A B S T R A C T 2 0 2 4 2 1 9 6 1 0 1 1 S e p 2 0 2 4 R N N H R O N N * 2 R ³ L O R O O * 7 N R O * 4 R 4 O N * 5 N R 1 2 O 1 3 R