689 results about "Quinolizine" patented technology

The invention discloses a colorectal cancer radiotherapy sensitization medicine and application thereof, belongs to the field of biological medicine, and particularly relates to a colorectal cancer radiotherapy sensitization medicine which comprises active pharmaceutical ingredients and a solvent, the active pharmaceutical ingredients comprise doxorubicin and a nitrogen-containing compound, the nitrogen-containing compound comprises quinoline-6-carbohydrazide and N-benzyloxymethyl-4-nitroimidazole, and the nitrogen-containing compound comprises quinoline-6-carbohydrazide and The colorectal cancer radiotherapy sensitization medicine disclosed by the invention focuses on a key driving gene FOXP4 for colorectal cancer radiotherapy resistance, and FOXP4 protein is degraded through a ubiquitin-proteasome way, so that not only can the sensitivity of tumor cells to radiotherapy be remarkably improved and tumor growth be inhibited, but also damage to normal tissues is reduced; moreover, the problem of drug resistance easily generated by a traditional method is effectively avoided, the research and development cost is greatly reduced, clinical transformation is accelerated, and the method has a good clinical application prospect.

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 relates to a [NN] bidentate coordination metal catalyst based on a quinoline skeleton as well as a preparation method and application of the [NN] bidentate coordination metal catalyst. According to the preparation method, quinoline-8-formaldehyde and aniline are directly subjected to aldehyde-amine condensation under the catalysis of p-TsOH, and a quinoline-imino ligand is synthesized. The [NN] bidentate coordination metal catalyst based on the quinoline skeleton is prepared by carrying out one-pot reaction on the obtained ligand and in-situ synthesized MMe4 (M is Ti, Zr or Hf). The quinoline skeleton [NN] bidentate coordination metal catalyst is used for polyolefin synthesis. The preparation method has the advantages of simple synthesis process, easily available raw materials, high product yield and high temperature resistance, is suitable for high-temperature solution polymerization, and can be used for preparing high-performance polyolefin elastomers.

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 invention discloses a preparation and purification method and application of a quinoline derivative with biological activity, and belongs to the technical field of medicine synthesis. According to the key points of the technical scheme, the quinoline derivative molecule has a structure # imgabs0 #, wherein X is NH or empty (benzene rings are directly connected); r is an aromatic ring derivative or alkyl or other groups. The invention designs and synthesizes a quinoline derivative with a novel structure, and the compound has a relieving effect on LPS-induced microglial cell inflammation and has a certain inhibition effect on cervical cancer cells.

The invention discloses a demethylase ODM gene for synthesizing benzylisoquinoline alkaloids and application thereof, the demethylase ODM gene is an ODM1 gene or an ODM2 gene, the nucleotide sequence of the CDS region of the ODM1 gene is shown as SEQ ID NO: 1, and the nucleotide sequence of the CDS region of the ODM2 gene is shown as SEQ ID NO: 2. Aiming at the current situation that the research basis of a key gene for synthesizing corydalmine in rhizoma corydalis is weak, the ODM1 gene for catalyzing tetrahydropalmatine demethylation to specifically generate corydalmine and tetrahydrojatrorrhizine and the ODM2 gene for specifically generating tetrahydrojatrorrhizine are cloned from rhizoma corydalis for the first time. An important theoretical basis is provided for producing the corydalmine by utilizing a synthetic biological method in the future, and the corydalmine mutant has a wide application prospect and a great economic value.

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 silane modified polyether prepared from an ethoxyquin polymer, which is prepared by the following method: carrying out aminolysis reaction on the ethoxyquin polymer and epoxypropane to prepare amino alcohol; taking amino alcohol as an initiator, and carrying out polymerization reaction on the amino alcohol and epoxypropane to prepare ethyoxyl quinoline polyether polyol; the ethyoxyl quinoline polyether polyol, anhydride and epoxy organosiloxane are subjected to chemical modification, and the silane modified polyether is prepared. According to the method, resource utilization of the ethoxyquin distillation still residues is realized. Due to the introduction of a rigid nitrogen-containing heteroatom quinoline ring structure and an ester bond structure with high cohesive energy, the silane modified polyether prepared from the ethoxyquinoline polymer has the advantages of high strength, strong adhesion, moisture resistance, low odor, environmental protection, no solvent and the like after being cured, can be used for preparing glass cement, sealant, nail-free glue, ceramic tile adhesive and the like, and has wide application prospects. The method can be widely applied to building industry.

An object of the present invention is to provide a therapeutic or preventive agent for amyotrophic lateral sclerosis, the agent having inhibitory action against ferroptosis. The present invention provides a therapeutic or preventive agent for amyotrophic lateral sclerosis, the agent containing a tetrahydroquinoline derivative represented by the compound below or a pharmaceutically acceptable salt thereof as an active ingredient.

The invention discloses a small molecular proteasome agonist as well as a preparation method and application thereof. According to the invention, cyclohexylamine is used as an initial raw material, and 3-(1-(benzo [D] thiazole-2-carbonyl)-2-(furan-2-methylene) hydrazone group)-N-cyclohexylpropanamide and N-cyclohexyl-3-(2-(furan-2-methylene)-1-(quinoline-2-carbonyl) hydrazone group) propanamide are prepared through a five-step reaction. The two compounds provided by the invention have good 20S proteasome agonistic activity and ischemic injury myocardial cell protection activity, do not have obvious cytotoxicity, and are expected to become effective choices for ischemic cardiomyopathy and other proteotoxic diseases.

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 invention belongs to the field of cosmetics, and particularly discloses an ergothioneine anti-aging skin care composition and a preparation method thereof. According to the formula, each 100 g of the anti-allergy anti-inflammatory and anti-allergy anti-allergy anti-allergy anti-allergy anti-allergy anti-allergy anti-allergy anti-allergy anti-allergy anti-allergy anti-allergy anti-allergy anti-allergy anti-allergy anti-allergy anti-allergy anti-allergy anti-allergy anti-allergy anti-allergy anti-allergy anti-allergy anti-allergy anti-allergy anti-allergy anti-allergy anti-allergy anti-allergy anti-allergy anti-allergy anti-allergy anti-allergy anti-allergy anti-allergy anti-allergy anti-allergy anti-allergy anti-allergy anti-allergy anti The transdermal rate and the stability of the ergothioneine and the pyrroloquinoline quinone are improved by adopting a liposome encapsulation technology, an'enzymatic + non-enzymatic 'dual-mode antioxidant system is formed by combining the French muskmelon extract and the roxburgh rose extract, full-type free radical scavenging is covered, and cell autophagy is regulated and controlled through spermidine to delay senescence.

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 discloses a quinolinone derivative and a preparation method thereof, and the quinolinone derivative comprises a 3-phenyl-6, 7-dimethoxy isoquinolin-1 (2H)-one derivative and a 3-phenyl-6, 7-dimethoxy quinolin-2 (1H)-one derivative which are shown in the structural general formulas of formula (I) and formula (II). Wherein 4, 5-dimethoxy-2-methyl benzaldehyde is synthesized firstly, then the 4, 5-dimethoxy-2-methyl benzaldehyde and substituted cyanophenyl are subjected to cycloaddition reaction under the action of potassium tert-butoxide and LiHMDS, and the 4, 5-dimethoxy-2-methyl benzaldehyde is obtained; the preparation method of the 2-(substituted phenyl)-N-(2-formyl-4, 5-dimethoxyphenyl) acetamide comprises the following steps: synthesizing 2-amino-4, 5-dimethoxybenzaldehyde, carrying out acylation reaction on the 2-amino-4, 5-dimethoxybenzaldehyde and substituted phenylacetic acid under the action of HATU to obtain 2-(substituted phenyl)-N-(2-formyl-4, 5-dimethoxyphenyl) acetamide, and carrying out cyclization reaction on the 2-(substituted phenyl)-N-(2-formyl-4, 5-dimethoxyphenyl) acetamide under the action of K2CO3 to obtain the 2-(substituted phenyl)-N-(2-formyl-4, 5-dimethoxyphenyl) acetamide. The preparation method has the characteristics of mild reaction conditions, simplicity in operation, high efficiency, environment friendliness and the like.

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.

The present invention relates to imidazoquinoline or benzindazolone compounds, their pharmaceutically acceptable salts, hydrates, solvates, enantiomers, diastereoisomers, tautomers or prodrugs; their use in the prevention and treatment of inflammatory diseases; and intermediates for their preparation. By using the compounds of the present invention as substrates of NQO1 to activate the redox reaction of NQO1, the expression and activity of inflammatory cytokines can be inhibited, and thus they can be used for preventing or treating diseases related to NQO1 activity.

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.

A thermally-conductive silicone composition containing:(A) an organopolysiloxane having an alkenyl group bonded to at least two silicon atoms in one molecule;(B) an organohydrogenpolysiloxane having a hydrogen atom bonded to at least two silicon atoms in one molecule, wherein the silicon atom-bonded hydrogen atom amount in component (B) is 0.1-5.0 per one alkenyl group in component (A);(C) a thermally-conductive filler;(D) a complex of a metal and a 8-quinolinol, and(E) a platinum group metal catalyst.The thermally-conductive silicone composition provides a thermally-conductive silicone cured product enabling the suppression of the increase in hardness from an initial hardness during high temperature aging at 150° C.

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 disclosure relates to analogs of quinoxaline / quinoline cytotoxic agents, termed"Nupomycins" herein, linker-payloads, and protein-drug conjugates thereof, pharmaceutical compositions comprising same, and methods of treating disease therewith.