550 results about "Quinolizine" patented technology

The present invention discloses an infrared-shielding polyurethane glass film and a preparation method thereof, relating to the field of polymer materials technology. When preparing the infrared-shielding polyurethane glass film, the present invention comprises reacting an organic nickel complex and 3-imidazole-1-propionic acid to produce a functionalized crosslinker; sequentially reacting 4-aminophenylacetonitrile with 3-hydroxypropyl acrylate and quinoline-4-carboxaldehyde to produce a UV-absorbing monomer; reacting polypropylene glycol, a UV-absorbing monomer, 1,4-butanediol, and 4-chloromethyl-1,3-phenylenediisocyanate to polymerize to produce polyurethane; reacting tungsten-doped titanium dioxide and chloropropyltriethoxysilane to produce modified titanium dioxide; and uniformly mixing the polyurethane, modified titanium dioxide, the functionalized crosslinker, and acetone, followed by coating and curing to produce the infrared-shielding polyurethane glass film. The infrared-shielding polyurethane glass film prepared by the present invention has excellent infrared shielding, anti-aging, antibacterial, and mechanical properties.

The invention discloses a near-infrared dichroic dye, a liquid crystal composition and application of the near-infrared dichroic dye and the liquid crystal composition. The structural general formula of the disclosed dichroic dye is as shown in formula I in the specification. According to the invention, a hydrogenated quinoline ring, a hydrogenated benzopyran ring and a hydrogenated naphthalene ring are introduced into a molecular skeleton, so that the novel near-infrared dichroic dye with high light stability, high solubility, high order parameter and high light modulation capability is obtained. Compared with the near-infrared dichroic dye disclosed in the prior art, the absorption band is further subjected to red shift, and the light modulation capability is remarkably improved; ordering parameters are greatly improved, and the application bottleneck is solved.

Provided herein is the use of certain biomarkers, such as tryptophan and metabolites thereof for use in certain treatment methods. Suitable tryptophan metabolites that may serve as useful biomarkers include, for example, kynurenine (Kyn), kynurenic acid (KynA), and quinolinic acid. Such biomarkers may be used in identifying a subject who may benefit from treatment, predicting the responsiveness or monitoring the response of the subject to the treatment, or determining or adjusting the dosing or dosing regimen of the treatment to the subject.

The present application provides a therapeutic combination of a quinoline derivative and an antibody, which comprises an immune checkpoint inhibitor and a tyrosine kinase inhibitor, wherein the tyrosine kinase inhibitor is a compound of formula I or a pharmaceutically acceptable salt thereof. The therapeutic combination in the present application shows good activity against lung tumor and liver tumor.

Disclosed are a kinase inhibitor and a pharmaceutical composition comprising the kinase inhibitor. The kinase inhibitor comprises a compound as represented by formula (I) or a pharmaceutically acceptable salt, solvate, ester, acid, metabolite, or prodrug thereof. The compound and composition above can inhibit wild-type KIT and / or mutant KIT tyrosine kinase activity and treat, prevent, or alleviate diseases, disorders, or conditions associated with wild-type KIT and / or mutant KIT kinase activity.

The present application provides a therapeutic combination of a quinoline derivative and an antibody, which comprises an immune checkpoint inhibitor and a tyrosine kinase inhibitor, wherein the tyrosine kinase inhibitor is a compound of formula I or a pharmaceutically acceptable salt thereof. The therapeutic combination in the present application shows good activity against lung tumor and liver tumor.

The invention discloses a preparation method of a post-metallocene catalyst. The method comprises the following steps: by taking quinoline 2-formaldehyde and ortho-aminophenol as raw materials, carrying out reflux reaction on the raw materials and a first solvent to prepare a ligand; dispersing a metal chloride in a second solvent, adding a Grignard reagent, and carrying out a reaction at a low temperature to prepare a methylated metal reagent; and adding a ligand into the methylated metal reagent, reacting at room temperature for 10-12 hours, removing liquid in vacuum, adding part of the second solvent again, stirring, filtering after the product is dissolved, and recrystallizing the filtrate to obtain the product, the metallocene catalyst is obtained by firstly preparing the ligand, then preparing the methylated metal reagent, adding the ligand into the methylated metal reagent for reaction, then stirring by using the second solvent, filtering after the product is dissolved, and recrystallizing the filtrate, so that the operation steps are simple, and the preparation of the ligand does not need water-oxygen treatment operation, and is simple and easy to implement; the preparation cost of the post-metallocene catalyst is reduced, and the method is suitable for industrial large-scale production.

The invention relates to a manufacturing method of a photodynamic antibacterial fiber membrane for masks, which is characterized by comprising the following steps: step 1, preparing 1-methyl-5-(4-methoxyphenyl) quinoline; step 2, preparation of 1-methyl-5-(4-methoxyphenyl) quinolinium hexafluorophosphate; step 2, preparation of 2-methyl-5-(4-methoxyphenyl) quinolinium; and step 3, preparation of an electrostatic spinning fiber membrane: polylactic acid and polyethylene glycol are dissolved in a solvent, the target product is added to form a spinning solution, and the spinning solution is used for electrostatic spinning to form the electrostatic spinning fiber membrane. According to the invention, the photodynamic antibacterial fiber membrane with excellent stability, biodegradability, reusability and antibacterial efficiency can be prepared. Compared with a traditional non-woven fabric mask, the fiber membrane shows higher bacterium adsorption and killing capacity in air containing various bacteria by means of the high specific surface area of the fiber membrane and the synergistic effect of the high-activity antibacterial agent 5-MPQ-Me.

The present disclosure relates to a crystalline form of trans-4-[1-(3-Chloro-phenyl)-7-methoxy-2,4-dioxo-3,4-dihydro-2H-pyrimido[5,4-c]quinolin-3-yl]-cyclohexanecarboxylic acid hydrochloride, methods of preparation, and its use as a therapeutic agent to treat inflammatory diseases.

The present disclosure relates to a crystalline form of trans-4-[1-(3-Chloro-phenyl)-7-methoxy-2,4-dioxo-3,4-dihydro-2H-pyrimido[5,4-c]quinolin-3-yl]-cyclohexanecarboxylic acid hydrochloride, methods of preparation, and its use as a therapeutic agent to treat inflammatory diseases.

The application discloses an 8-hydroxyquinoline anticancer zinc (II) complex and a synthesis method and application thereof. The 8-hydroxyquinoline anticancer zinc (II) complex is synthesized by taking 5,7-diiodo-8-hydroxyquinoline, 5,7-dichloro-8-hydroxyquinoline, 5-chloro-7-iodo-8-hydroxyquinoline, 5,7-dibromo-8-hydroxyquinoline and 5-chloro-8-hydroxyquinoline as a first ligand and taking 4,4'-dimethoxy-2,2'-bipyridine, 4,4-di-tert-butyl-2,2-bipyridine, 5,5'-dimethyl-2,2-bipyridine, 2,2-bipyridine and 4,4'-dimethyl-2,2'-bipyridine as auxiliary ligands. The 8-hydroxyquinoline anticancer zinc (II) complex has good inhibiting effect on SK-OV-3CR cells of an ovarian cancer drug-resistant strain, is higher than that of cisplatin drugs, overcomes drug resistance of clinical drugs, has potential medicinal value and can be used for preparation of various antitumor drugs.

The invention relates to the technical field of semiconductor luminescent materials, in particular to a wide-band-gap semiconductor crystal luminescent material and a preparation method and application thereof. The chemical composition of the CdLCl < 2 >. H2O or the Cd2L2 (Ac) (H2O) is [CdLCl] < 2 >. H2O]. L represents a quinoline carboxylic acid ligand; ac represents an acetate ion; the crystal structure of the wide-band-gap semiconductor crystal luminescent material is a one-dimensional chain structure. The crystal complex is mainly formed by bridging cadmium ions with carboxyl of a quinoline carboxylic ligand, and the formed crystal complex emits light in a red region, is suitable for various light-emitting application scenes, and solves the problems that an existing wide-band-gap semiconductor light-emitting material is relatively low in light-emitting efficiency, light stability and heat stability, and the light-emitting efficiency is low. And the light-emitting wavelength is difficult to regulate and control.

Described is small molecule 6-methoxy-7-(3-(pyrrolidin-1-yl)propoxy)-4-(tetrahydro-2H-pyran-4-yl)quinolin-2-amine (MS152) that inhibits methyltransferases G9a / EHMT2. This inhibitor can be used for the treatment of patients with G9a / EHMT2 related diseases such as Prader-Willi Syndrome and Alzheimer's Disease. Formula (I).

The present invention discloses a method and kit for analyzing endotoxins in complex matrix samples based on liquid chromatography-mass spectrometry. 3-hydroxydecanoic acid, 3-hydroxydodecanoic acid, 3-hydroxytetradecanoic acid, 3-hydroxyhexadecanoic acid or 3-hydroxyoctadecanoic acid characteristic of endotoxins are released by KOH methanol solution for quantitative analysis of various types of endotoxin content; the hydrolyzate is derivatized with isoquinoline-1-carboxylic acid hydrazine to significantly improve the ionization efficiency of the hydrolyzate; using optimized liquid chromatography and mass spectrometry parameters, high stability, high sensitivity and broad spectrum detection of endotoxins from different bacterial sources are achieved. The method has strong anti-interference ability, is applicable to complex matrices, and solves the problem of high false negative rate caused by matrix interference in the prior art.

The invention provides a 1, 3, 4-oxadiazino tetrahydroisoquinoline compound as well as a preparation method and application thereof, and belongs to the technical field of heterocyclic compounds for medicines. The method comprises the following steps: by taking an azomethine imine substrate and a styrene oxide substrate as raw materials and cobalt perchlorate hexahydrate as a catalyst, adding the raw materials and the catalyst into a reaction solvent, reacting overnight at normal temperature, and performing column separation to obtain the 1, 3, 4-oxadiazino tetrahydroisoquinoline compound. According to the application, the reaction condition is mild, the selectivity is high, excellent cytotoxicity is shown on HeLa cervical cancer cells and A549 lung cancer cells, the half death inhibition ratio (IC50) value on tumor cells reaches the nanomole level, and the application has a good anti-cancer drug application prospect.

The invention discloses purslane isoquinoline alkaloid as well as a preparation method and application thereof. The purslane isoquinoline alkaloid is shown as a formula 1 or a formula 2, has GLP-1 receptor agonistic activity and can be used for preparing medicines and health-care foods for preventing and treating diabetes mellitus.

Disclosed herein is an isoquinoline-1 (2H)-one derivative of formula (I): or a stereoisomer, tautomer, or pharmaceutically acceptable salt thereof wherein the values of the variables (e.g., L2A, R1, R2A, R3, R4A, R4B, R4C, R4D, Q2, Q3, Q4) are as described herein. Also disclosed is a pharmaceutical composition comprising such derivatives, and a method of using such derivatives to treat or prevent a condition or disease responsive to inhibition of PI3K [alpha] activity in a subject.

This invention belongs to the field of medicinal chemistry, specifically relating to 2-[2-methyl-6-(quinoline-3-yl)nicotinyl]-N-phenylhydrazine-1-formamide derivatives, their preparation methods, and applications. This invention is the first to synthesize 2-[2-methyl-6-(quinoline-3-yl)nicotinyl]-N-phenylhydrazine-1-formamide derivatives. Furthermore, the preparation method for these derivatives features low raw material costs, high yield, and a simple and easily controllable reaction process, making it suitable for industrial production. Moreover, these derivatives exhibit high NR4A1 protein-level inhibitory activity and can be used to prepare anti-hepatocellular carcinoma drugs.

The present invention relates to a process for preparing the compound of Formula I in the form of a base or a salt thereof, and its use as an intermediate for the preparation of calcitonin gene- related peptide (CGRP) receptor antagonist active pharmaceutical ingredients, in particular zavegepant, where the compound of Formula I is the following: (I)

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.

The present invention relates to solid phase pharmaceutical compositions of 6′-fluoro-N-(4-fluorobenzyl)-4′-oxo-3′,4′-dihydro-1′H-spiro[piperidine-4,2′-quinoline]-1-carboxamide that is useful as a AKR1C3 dependent KARS inhibitor. The present invention also relates to processes for the preparation of said pharmaceutical compositions of said compound, methods of using said pharmaceutical compositions in the treatment of various diseases and disorders, and their use in diseases and disorders mediated by an AKR1C3 dependent KARS inhibitor.

The present invention relates to compound according to formula (I), (I) which is a positive allosteric modulator of D1 and accordingly of benefit as pharmaceutical agent for the treatment of diseases in which D1 receptors play a role.

The present application relates to the technical field of lithium ion battery, in particular to a kind of lithium ion battery electrolyte additive and its electrolyte and lithium ion battery, the additive structural formula is as follows: Wherein, Ar is selected from any one of phenyl, pyridyl or quinoline group;R1, R2 Same or different, R1 And R2 respectively independently selected from any one of hydrogen, fluorine, cyano, C1~C5 Alkyl, C1~C4 Alkoxy, fluorine-containing C1~C4 Alkoxy, x is selected from 1, 2 or 3;Y, z respectively selected from 1, 2, 3 or 4, x+y+z≤6, and Ar is phenyl, x=1, R1 And R2 are not hydrogen simultaneously.The additive can form stable SEI film on the negative electrode surface, reduce the impedance of battery, improve the low temperature performance of battery, and also have flame-retardant function.

The invention provides novel 5-membered heteroaryl derivatives of quinolinones that inhibit Werner Syndrome ATP dependent helicase enzyme (WRN) activity. The invention also provides pharmaceutical compositions comprising compounds of the invention and methods thereof for treating various diseases and disorders associated with or related to WRN activity, such as various types of cancer.

The present invention addresses the problem of providing a medicine that, despite of being a non-ergot dopamine agonist (DA), reduces the risk of the drowsiness side effect, and exhibits an excellent therapeutic effect on neurodegenerative disorders such as Parkinson's disease (PD). The present invention relates to a pharmaceutical composition for treating neurodegenerative diseases such as Parkinson's disease, the pharmaceutical composition comprising 1-{[(4aR,6R,8aR)-2-amino-3-cyano-8-methyl-4,4a,5,6,7,8,8a,9-octahydrothieno[3,2-g]quinolin-6-yl]carbonyl}-3-[2-(dimethylamino)ethyl]-1-propylurea or a pharmacologically acceptable salt thereof. The pharmaceutical composition is characterized by being orally administered at a daily dose of 0.25 mg to 2 mg in terms of free form.

The application discloses a quinolinone derivative compound, a pharmaceutical composition and application thereof. The quinolinone derivative compound can antagonize diarrhea induced by CGRP, and the compound has a good application prospect in preparation of a drug for treating irritable bowel syndrome.

The invention belongs to the technical field of pharmacy, and particularly relates to application of polycyclic alkaloid in preparation of an anti-breast cancer drug, and the polycyclic alkaloid is 1, 2a, 7-trimethyl-5-tosyl-1, 2, 2a, 3, 4, 5-hexahydropyrrolo [4, 3, 2-de] quinoline. The polycyclic alkaloid compound is applied to preparation of anti-breast cancer drugs, the effect of inhibiting growth of breast cancer cells is remarkable, and the efficacy of the polycyclic alkaloid compound is far better than that of a positive drug ML162 aiming at EC50 (mu M) + / -S.D = 9.04 + / -0.37 of HCC1937 human breast cancer cells.

This invention discloses a quinoline hydrazone ligand, its Fe(II) spin-crossover complex, and a method for synthesis. The quinoline hydrazone ligand is ( E )-4-bromo- N' -(quinoline-8-methylene)benzoylhydrazine, with the structural formula shown, and the complex structure shown. The ligands of this invention have sufficiently strong coordination ability with metals. The complex is not easily oxidized in air, does not easily dissociate in solution, and has good acid resistance. The complex is in a low-spin state and is suitable for photoacid switching in solution, making it applicable to fields such as spin-crossed molecular switches and acid-base stimulation sensors.

The present disclosure provides methods, pharmaceutical compositions, and kits for treating cancer in patients in need thereof. The methods comprise administering to a patient in need a small ubiquitin-like modifier (SUMO) activating enzyme (SAE) inhibitor, such as [(1R,2S,4R)-4-{[5-({4-[(1R)-7-chloro-1,2,3,4-tetrahydroisoquinolin-1-yl]-5-methyl-2-thienyl}carbonyl)pyrimidin-4-yl]amino}-2-hydroxy-cyclopentyl]methyl sulfamate (Compound I-263a) or a pharmaceutically acceptable salt, in combination with one or more anti-CD19 antibodies. Also provided are medicaments for use in treating cancer.

The present invention discloses a benzothiadiazine-1,1-diketo-quinoline derivative, a preparation method, and an application thereof, belonging to the technical field of chemical optical materials. A benzothiadiazine-1,1-diketo-quinoline derivative is provided. The structural formula of the benzothiadiazine-1,1-diketo-quinoline derivative is: wherein R is -N(CH2CH3)2 or -OCH3. The present invention introduces a benzothiadiazine-1,1-diketo heterocycle at the 2-aldehyde position of quinoline to prepare the benzothiadiazine-1,1-diketo-quinoline derivative. The preparation cost is low, the operation is simple, and the method is simple. The obtained benzothiadiazine-1,1-diketo-quinoline derivative exhibits fluorescent properties and can be used as a probe for the detection of heavy metal copper and / or mercury ions. At the same time, the synthesis method can be used for synthesis in fine organic chemical fields such as printing and dyeing technology and analytical detection.