46 results about "Aminoquinolines" patented technology

The present invention is related to compounds of formula (I), or a therapeutically suitable salt or prodrug thereof, which antagonize the effects of melanin-concentrating hormone (MCH) through the melanin concentrating hormone receptor and are useful for the prevention or treatment of eating disorders, weight gain and obesity.

The invention relates to 3-cyan-6-aminoquinoline derivatives, a preparation method thereof and application thereof in medicines, in particular to new 3-cyan-6-aminoquinoline derivatives shown as a general formula (I) and medicinal salts thereof, and use thereof as a therapeutical agent, particularly a protein kinase inhibitor, wherein the definition of each substituent group in the general formula (I) is shown as the description. The formula (I) is shown in the description.

Disclosed is a rapid analysis method of the free amino acid content in a fresh tea sample. The rapid analysis method is characterized by comprising the steps of mincing and uniformly mixing the fresh tea sample, using ultrapure water as an extraction solvent, conducting digestion under the condition of 90 DEG C for 20 min, after centrifugal filtration is conducted, using 6-aminoquinoline-N-hydroxysuccinimdyl carbamate as a derivating agent to conduct pre-column derivatization, using an XBridge C18 chromatographic column to conduct gradient elution, and using a high performance liquid phase-fluorescence detector to conduct separation and detection. According to the rapid analysis method of the free amino acid content in the fresh tea sample, sample preparation is quick and simple, the cost is low, the degree of precision and the degree of accuracy are high, and the stability and linear relation are good, the whole analysis process is quick, sensitive and good in reproducibility, and thus the rapid analysis method is applicable to quick analysis of free amino acid in the fresh tea sample.

Compositions and methods are provided for preventing or treating the pre-clinical early-stages of inflammatory diseases, including autoimmune diseases, degenerative inflammatory diseases, metabolic inflammatory diseases, chronic infection associated with inflammation, cancer associated with inflammation, and other inflammatory diseases by administration to an individual of an effective dose of a synergistic combination of active agents comprising or consisting essentially of an aminoquinoline, e.g. hydroxychloroquine, and a statin, e.g. atorvastatin. Each or both of the active agents can be formulated in various ways, including without limitation a solid oral dosage form.

The invention relates to 4-aminoquinoline and a 4-aminoquinoline compound which are applied to the technical field of medicines and applications of the compound, compounds, configurational isomers and configurational isomer mixtures or pharmacologically acceptable salts and / or hydrates of the compound in the general formula I. The compound provided by the invention has the obvious antitumor activity and can be used for preparing the medicines for treating and / or preventing tumor diseases. In addition, the compound is light in molecular weight, simple to composite and small in toxic and side effects.

The invention discloses a quick analysis method of content of a theanine in fresh tea leaf sample. The quick analysis method is characterized by including: smashing and well mixing the fresh tea leaf sample, using ultrapure water as an extraction solvent, extracting at 90 DEG C for 20min, centrifugally filtering, using 6-aminoquinoline-N-hydroxysuccinimido carbamate as a derivating agent for pre-column derivatization, using an XBridge C18 chromatographic column for gradient elution, and using a high performance liquid chromatography-fluorescence detector for separating detection. The method is quick and simple in sample separation, low in cost, good in precision, accuracy, stability and linear relation, quick and sensitive in whole analysis process, high in repeatability and suitable for quick analysis of teanine in the fresh tea leaf sample.

The invention discloses surface-functionalized Fe3O4 nanoparticles and a preparation method thereof, and a method for applying the nanoparticles to enrich and detect Cu<2+>. The method comprises the steps of: carrying out surface modification on ferroferric oxide nanoparticles through chemical covalent coupling by adopting a chemosynthetic 8-chloracetyl aminoquinoline derivative, treating Cu<2+> aqueous solutions of different concentrations by utilizing surface-functionalized magnetic ferroferric oxide nanoparticles, and then detecting the enriching and adsorbing effect by atomic absorption. The detection result shows that the surface-functionalized Fe3O4 nanoparticles have very strong enriching action on trace Cu<2+>, and the enriching capability is 10-15 times that of surface-unfunctionalized Fe3O4 nanoparticles. The surface-functionalized Fe3O4 nanoparticles prepared by the preparation method have the characteristics of good enriching effect and high adsorption efficiency to Cu<2+>, simplicity and convenience in operation and easiness in analysis; and by utilizing the method, trace Cu<2+> in the solution can be effectively enriched and detected.

The invention relates to a preparation method for a benzotriazole Schiff base compound. A synthetic method comprises the steps of: (1) adding 5-carboxy benzotriazole, LiAlH4 and THF (tetrahydrofuran) into a flask, dripping TPAP / NMO (tetrapropylammonium perruthenate / N-morpholine oxide), CH2Cl2, THF and DMF (dimethyl formamide) after stirring for 2 hours, and reacting for 12 hours, so as to obtain white 5-aldehyde benzotriazole; (2) sequentially adding the product obtained in the step (1), formaldehyde, acetic acid and water into the flask, and carrying out stirring, standing and suction filtration, so as to obtain white 1-hydroxymethyl-5-aldehyde benzotriazole; (3) adding the product obtained in the step (2), CHCl3 and TBAB (tetrabutylammonium bromide) into the flask, dropwise adding CrO3 and a concentrated H2SO4 water solution after heating and dissolving the mixture, stirring until the solution becomes deep green, skimming, regulating the pH of an inorganic layer to be approximate to 8, and carrying out chloroform extraction, anhydrous sodium sulfate drying and rotary evaporation, so as to obtain orange red 1,5-dialdehyde benzotriazole; and (4) adding the product obtained in the step (3) into the flask, adding 6-aminoquinoline after dissolving the product by the ethanol, and carrying out backflow, filtering and recrystallization, so as to obtain a target compound of benzotriazole Schiff base. According to the target compound, the structure is novel, the corrosion inhibition performance is high, and the problem of acid washing of carbon steel can be effectively solved.

The invention relates to hydroxychloroquine or chloroquine, or a geometrical isomer thereof, or a pharmaceutically acceptable salt of the hydroxychloroquine or chloroquine, and / or a solvate of the hydroxychloroquine or chloroquine, and / or a hydrate of the hydroxychloroquine or chloroquine, a pharmaceutical composition containing the compound, and an application of the hydroxychloroquine or chloroquine to treatment of diseases or infection caused by SARS-CoV-2.

The present invention provides, among other things, new benzylamine compounds, compositions comprising benzylamine compounds, methods of making benzylamine compounds, and methods of using benzylamine compounds for treating or preventing a variety of conditions or diseases associated with lipoprotein metabolism.

The invention discloses a fluorescent cationic surface active agent and a preparation method and application thereof and relates to the cationic surface active agent and the preparation method and application thereof. The technical problems that an existing cationic surface active agent is single in function and performance is not regulated easily are solved. The chemical name of the fluorescent cationic surface active agent is N,N-dimethyl-N-alkyl-N-(N'-(5-quinolyl) aminoacyl methyl) ammonium halide, and the structural formula is shown in the description, wherein R is CnH2n+1, n is 8-22, and X is halogen. The preparation method comprises the steps that 5-chloracetyl-aminoquinoline and alkyl tertiary amine are dissolved in a solvent, heating and stirring are carried out, a coarse product is obtained, the solvent in the coarse product evaporates, and a solid product is obtained; furthermore, recrystallization is carried out on the solid product, and the fluorescent cationic surface active agent is obtained. The fluorescent cationic surface active agent can serve as a pH value indicator for a solution.

The invention discloses an adsorbing material with a function of removing oil spill pollutants in water. A controllable preparation process comprises the following steps: preparing 4-benzopyrone-2-carboxylic acid, oxotetrahydropyran, N,N-dimethylformamide, 2,5-dibromopyrimidine, 3-pyrimidine-5-benzaldehyde, 1-pyrimidine-2-piperidyl-4-one, 3-thiophenic acid and chloroform into mixed iquid D; preparing 4- pyrimidinecarboxylate, N,N-dimethylformamide, 5-pyrimidinemethanamine, 2-pyridine-4-pyrimidine-5-carboxylic acid, 3-pyrimidine-2-yl-benzaldehyde, 5-aminoquinoline and chloroform into mixed liquid H; fixing an injector absorbed with the mixed liquid D onto a track I of an electrostatic spinning instrument; fixing an injector absorbed with the mixed liquid H onto a track II of the electrostatic spinning instrument; and carrying out electrostatic spinning for 15 hours and drying for 24 hours in a vacuum drying box to obtain the adsorbing material with the function of removing oil spill pollutants in water.

The invention provides a composition prepared from artemisinin antimalarials and aminoquinoline antimalarials; the composition is suitable for treating the cancers, such as lung cancer, breast cancer and melanoma, has low side effect, and is effective in improving cancer treatment effect and reducing the development and progress of a patient's complications.

Disclosed are compositions, medical devices and methods for ameliorating sterile injury due object use in a subject in need thereof. More particularly, the present disclosure relates to compositions including N-Acetylcysteine and an aminoquinoline. The present disclosure also relates to compositions including an endonuclease and an aminoquinoline. The present disclosure also relates to medical devices including a coating comprising N-Acetyl-cysteine, an aminoquinoline, an endonuclease, and combinations thereof.

The present invention is concerned with the development of novel 8-aminoquinoline analogs in the treatment and prevention of malaria and the said compound has broad spectrum of activity against the blood as well as tissue stages of the human malaria parasites makes these compounds very attractive in the cure and prevention of malaria caused by drug-sensitive and multidrug resistant strains and also it is expected that development of these compounds as ideal antimalarial agents may lead to suppression as well as radical cure of the malaria infection with single drug therapy.

The invention discloses a preparation method and application of impurities of 4-aminoquinoline compounds, and concretely discloses a preparation method of 5-chloro-4-hydroxyl-3-quinolinecarboxylic acid (LKL-5 isomer). The preparation method is characterized in that the 5-chloro-4-hydroxyl-3-quinolinecarboxylic acid is separated from a mixture 1 containing the 5-chloro-4-hydroxyl-3-quinolinecarboxylic acid and 7-chloro-4-hydroxyl-3-quinolinecarboxylic acid by adopting a liquid phase method. Preferably, the mixture 1 is obtained by reacting diethyl m-chloroaniline methylene malonate (LKL-3) under the conditions of mineral oil and concentrated sulfuric acid, post-treating after the reaction is completed to obtain a mixture 2, hydrolyzing the mixture 2 under an alkaline condition, and post-treating to obtain the mixture 1. The purity of the 5-chloro-4-hydroxy-3-quinolinecarboxylic acid is greater than 99%, and preferably greater than 99.5%, the 5-chloro-4-hydroxy-3-quinolinecarboxylic acidcan be used for synthesizing subsequent products, and the 5-chloro-4-hydroxy-3-quinolinecarboxylic acid and the synthesized subsequent products can be used for impurity reference substances of 4-aminoquinoline compounds and can be used for quality control of related raw material medicines.

The invention discloses an application of a 4-aminoquinoline compound in preparation of a medicine for inhibiting exudative inflammation. The invention provides the application of the 4-aminoquinoline compound or a pharmaceutically acceptable salt thereof in preparation of the medicine or a pharmaceutical composition for treating and / or preventing exudative inflammation. The pharmaceutical composition comprises the 4-aminoquinoline compound or the pharmaceutically acceptable salt of the 4-aminoquinoline compound, and one or more pharmaceutically acceptable pharmaceutic adjuvants and / or one or more other active ingredients. The 4-aminoquinoline compound, such as chloroquine and hydroxychloroquine, has a good treatment effect on improvement of swelling of cells and exudation of blood vessels and intercellular fluid in an inflammatory state.

The present invention relates to 2-aminoquinolines of formula Iwherein R1, R2 and R3 are as defined in the specification, as 5-HT5A receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use for the treatment of CNS disorders.

The invention discloses a method for efficiently preparing an aza-acridine compound. The structural formula of the aza-acridine compound is shown as a formula I; the preparation method comprises the following steps: adding a 2-aminoquinoline-3-methanamide compound and a solvent under an air condition, and heating to reaction temperature; after the reaction is ended, separating and purifying to obtain multisubstituted acridine derivatives shown as the following formula, wherein the reaction temperature is 100 to 200DEG C, and the reaction time is 1 to 24 hours. A synthetic method of the aza-acridine compound, disclosed by the invention, has the advantages of scientificity, reasonability, simple and easily-operated synthesis process and high synthetic yield; a product is easy to purify. The invention also relates to the aza-acridine compound which can be used for inhibiting EGFR (Epidermal Growth Factor Receptor) and SrC, a preparation method of the aza-acridine compound, activity of a drug containing the aza-acridine compound and the application of the drug. The compound is shown in a formula II and can be used for preparing an EGFR and SrC activity inhibitor and a disease treatment medicine activated and mediated by the EGFR and the SrC.

Analgesic compositions comprise an aminoquinoline together with an opioid, a non-steroidal anti-inflammatory drug (NSAID), a NE / 5-HT reuptake inhibitor, or a combination thereof. The aminoquinoline potentiates bioactivity of opioids, NSAIDs and NE / 5-HT reuptake inhibitors.

According to the present invention, through a first-step metal-free halogenation reaction, a 5-site substituted arylated / heterocyclic 8-amidoquinoline compound is selectively obtained through a direct coupling reaction with a boric acid compound without separation; in the absence of the metal in the first step, the subsequent reaction is not affected; an aminoquinoline compound, a halide and a boric acid compound are adopted as raw materials, a common metal is adopted as a catalyst, and a common organic solvent is adopted as a reaction solvent; and halogenations, an arylation one-pot reaction, and column chromatography are sequentially performed to obtain the 5-site substituted arylated / heterocyclic 8-amidoquinoline compound.

The invention discloses a 5-cyano-8-acylaminoquinoline compound and a preparation method thereof, belonging to the technical field of quinoline compounds. The preparation method of the 5-cyano-8-acylaminoquinoline compound comprises the following steps: adding 8-acylaminoquinoline, tert-butylisonitrile, iodosobenzene, boric acid and hexafluoroisopropanol into a reactor, and then carrying out stirring and reacting at a temperature of 60 to 70 DEG C to obtain the 5-cyano-8-acylaminoquinoline compound. The invention further discloses the 5-cyano-8-acylaminoquinoline compound prepared by using the preparation method disclosed by the invention. The preparation method does not use any metal catalyst, so the use of the metal catalyst is avoided.

The invention discloses a synthesis method of a dihydropyrrolo2-aminoquinoline compound. The synthesis method comprises the following steps: in a reactor, dissolving high-alkyne propylamine, a catalyst, an oxidant and a ligand into an organic solvent, and then adding isocyanide; stirring and reacting at 80 to 100 DEG C; after reaction is finished, cooling a reaction solution to room temperature; separating and purifying the reaction solution to obtain the dihydropyrrolo2-aminoquinoline compound. The synthesis method disclosed by the invention takes the simple and easy-to-obtain high-alkyne propylamine as a raw material, and isocyanide migration and inserting serial cyclization reaction is carried out; common palladium salt is used as the catalyst, and cheap copper salt is used as an oxidant to construct the dihydropyrrolo2-aminoquinoline compound with extremely good medicinal value; the synthesis method has the advantages of simple and easy-to-obtain raw materials, simplicity and safety in operation, moderate conditions and high atom economy; the synthesis method has the characteristics of high efficiency, convenience, wide applicable range and the like in the synthesis of a targetproduct and has potential value in actual production and application.

The invention relates to the technical field of medicine, in particular to a class of aminoquinoline compounds, a preparation method thereof and an antifungal application thereof. The aminoquinoline compounds provided by the invention generally have good antifungal activity and have the potential to be developed into non-azole antifungal drugs.

The invention provides methods of preparing macrocycles including macrocycle stabilized peptides (MSPs). Macrocycles and MSPs are prepared according to nucleophilic capture of an iminoquinomethide type intermediate generated from a suitably substituted 2-amino-thiazol-5-yl carbinol. The preferred nucleophile may be selected from an electron rich aromatic moiety in the case of macrocycles and, in the case of MSPs, at least one amino acid comprises an electron rich aromatic moiety. In addition, the concept can be extended to other related 5-membered heterocyclic systems in place of the thiazole, such as imidazole or oxazole. The conditions for the generation of the corresponding iminoquinomethide type intermediates may be similar or different than the conditions used for the 2-amino-thiazol-5-yl carbinol.

The present invention relates to 2-aminoquinolines of formula Iwherein R1, R2 and R3 are as defined in the specification, as 5-HT5A receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use for the treatment of CNS disorders.

The invention discloses an alumina ceramic matrix composite for cutters, and a preparation method of the alumina ceramic matrix composite. The alumina ceramic matrix composite is prepared from the following main components: zirconium diboride, silicon carbide and titanium powder, and is prepared by adding carbon fibers, boron nitride, ammonium persulfate, a chitosan acetic acid solution, paraffin emulsion, hydroxypropyl acrylate, heavy calcium carbonate, sodium alginate, hesperiden, 7-aminoquinoline, a coupling agent, a sintering aids and deionized water, and carrying out the technologies such as ball milling, mixing, ultrasonic sound, molding, degumming, spraying, mould pressing, vacuum impregnation and hot pressed sintering. The alumina ceramic matrix composite has higher toughness, is excellent in wear resistance, bending resistance and hardness index, and can meet the requirements of the industry, thus having better application prospect.