11 results about "Antagonists drugs" patented technology

The invention provides an ERalpha functionalized HEMT (High Electron Mobility Transistor) biosensor as well as a construction method and application thereof. The ERalpha functionalized HEMT biosensor comprises (1) an ERalpha functionalized HEMT biosensor; (2) a construction method of the ERalpha functionalized HEMT biosensor; and (3) application of the ERalpha functionalized HEMT biosensor in detection of an ERalpha potential antagonist. The biosensor provided by the invention takes an HEMT device as a carrier, is formed by functionally modifying ERalpha through chemical reaction, has the advantages of high sensitivity (the detection limit is as low as 1 fM), strong specificity, wide linear range (1 fM-100 nM) and the like, can efficiently and accurately identify the ERalpha potential antagonist, and provides a method or technical support for screening of ERalpha potential antagonist drugs.

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.

The present invention discloses novel molecules consisting of N-methyl-D-aspartate receptor (NMDAR) antagonist-polymer conjugates having the general structure D-(X-Poly-T) n wherein D is a high affinity, i.e. (+)-, (-)-or (+-)-dezocycline, or a low affinity, i.e. (+)-, (-)-or (+-)-methadone, CNS active NMDAR antagonist, n is an integer from 1 to 6. X is a stable (enzymatic and / or hydrolytic under physiological conditions) linker comprising a covalent bond or atomic chain covalently linking a small molecule NMDAR antagonist drug moiety to the Poly derivative. Poly is a covalently bonded chain of repeating monomer units forming a polymer backbone of synthetic or natural origin. T, if present, is another molecule of D, or an end group of Poly, represented by any suitable chemical group which, according to preference, does not react with or with other chemical moieties, or has targeting properties.

The present invention provides an ERα-functionalized HEMT biosensor and its construction method and application, including: (1) an ERα-functionalized HEMT biosensor; (2) a construction method of an ERα-functionalized HEMT biosensor; and (3) the application of the ERα-functionalized HEMT biosensor in the detection of potential ERα antagonists. The biosensor of the present invention uses a HEMT device as a carrier and is functionalized and modified with ERα through a chemical reaction. It has the advantages of high sensitivity (detection limit as low as 1 fM), strong specificity, and a wide linear range (1 fM-100 nM). It can efficiently and accurately identify potential ERα antagonists, providing a method or technical support for the screening of potential ERα antagonist drugs.

The present disclosure provides methods for preventing or treating a neurodegenerative disorder in a subject, where the neurodegenerative disorder is one characterized by a deposition of abnormal tau protein in the brain of the subject. The method generally includes administering to the subject a therapeutically effective amount of a drug that is a tau propagation antagonist.

The present disclosure relates to a crystal of a neurokinin-1 antagonist prodrug compound. Specifically, the present disclosure relates to a novel crystal and preparation method of the compound of formula I. The novel crystal of the present disclosure has good physicochemical properties and is more advantageous for clinical treatment. [Formula 1] TIFF2025502261000016.tif64168

The invention discloses a preparation method of a CXCR4 antagonist drug Mavorixfor and an isoquinoline derivative thereof, which comprises the following specific operation procedures: dissolving isoquinoline or benzimidazole in acetonitrile, adding methanol, a multi-bipyridine cobalt catalyst, electrolyte and a proton source, reacting under the conditions of visible light irradiation and constant voltage, and separating and purifying to obtain the CXCR4 antagonist drug Mavorixfor and the isoquinoline derivative thereof. And carrying out C-N coupling on the obtained hydroxymethylation product and a drug intermediate through a Mitsunobu reaction, so as to prepare the CXCR4 antagonist drug Mavorixfor and the isoquinoline derivative thereof. The method has the advantages of easily available and cheap raw materials, simple steps, high atom utilization rate, no need of additional addition of a stoichiometric oxidant, and good application prospects.

The invention belongs to the technical field of pharmaceutical preparations, and particularly relates to an MR (magnetic resonance) antagonist medicine and a preparation method thereof as well as an MR antagonist tablet and a preparation method thereof. By controlling the particle size of the fenerenone, tablets of different specifications are all dissolved out in vitro and are well fit with a reference preparation in dissolution, and in-vivo bioequivalence is better facilitated; the suspension is prepared from the raw material medicines and at least one of the adhesive and the surfactant, and a fluidized bed process and a liquid spraying adding mode are adopted, so that the flowability of the materials is improved, the mixing uniformity and the content uniformity can meet the requirements, and the content uniformity can be ensured to meet the requirements. And dissolution fitting and in-vivo bioequivalence of preparations with different specifications and an original reference preparation can be realized under various medium conditions.

Disclosed herein are methods of administering pharmaceutical formulations of a neurokinin-1 (NK-1) receptor antagonist to a subject in need of treatment of emesis.

The present invention provides a compound containing a polybrominated diphenyl ether structure, and the structure of the compound containing a polybrominated diphenyl ether structure is shown below: The present invention also provides a method for preparing the above-mentioned compound containing a polybrominated diphenyl ether structure, which is simple to prepare and easy to operate; the present invention also provides the use of the above-mentioned compound containing a polybrominated diphenyl ether structure in the preparation of NMDA receptor agonist or antagonist drugs and in the preparation of drugs for treating or preventing central nervous system diseases and / or mental disorders.

The present disclosure relates to the field of virtual screening and biotechnology, and particularly relates to a RAGE antagonist, a screening method and application in improving oocyte quality; through molecular docking and virtual screening technology, a candidate compound is successfully screened from a database, and from the candidate compound, the compound with the lowest binding free energy is selected as the final screened RAGE antagonist; the present disclosure uses virtual screening technology to quickly screen large food source compound library data, identifies the compound most likely to bind to the target, greatly speeds up the pace of RAGE antagonist drug discovery; a food source RAGE antagonist compound, millimetre wood acid, is successfully identified through virtual screening technology, which widens the clinical application scenario of millimetre wood acid, and clarifies the potential application of millimetre wood acid in preparing drugs for improving the decline of oocyte quality caused by the accumulation of AGEs, and provides a basis for the innovative development of new drugs for improving oocyte quality.