23 results about "Chloroquina" patented technology

The invention relates to a biological medicine technology, and discloses chloroquine lipid, a preparation method and application thereof, and lipid nanoparticles containing the chloroquine lipid. The chloroquine lipid is synthesized from chloroquine substances and alkylene oxide through a ring-opening reaction, and the chloroquine substances are selected from at least one of chloroquine, hydroxychloroquine, chloroquine derivatives and hydroxychloroquine derivatives. The lipid nanoparticles contain the chloroquine lipid, cationic lipid, phospholipid, PEG (polyethylene glycol) lipid and cholesterol. The chloroquine lipid can be used as a lipidated autophagy inhibitor, can endow the LNPs carrier with an autophagy inhibition function, and realizes the autophagy inhibition effect of'time-space synchronization ', so that the obstacle of'autophagy lysosome degradation' is broken through, and the gene delivery efficiency is enhanced.

The invention discloses an application of chloroquine in preparation of a medicine for treating glutamine deficiency type tumors, the chloroquine promotes IFN-gamma signal transduction by up-regulating IFNGR1 protein expression, so that the therapeutic effect of immunotherapy on the glutamine deficiency type tumors, ASCT2 low expression tumors or autophagy-lysosomal pathway active tumors is enhanced. The invention provides a new thought and an effective means for solving the problem of immunotherapy drug resistance caused by glutamine metabolism limitation, and has important theoretical significance and potential clinical application value.

The invention relates to the technical field of biological medicine, in particular to application of hordenine in preparation of a lysosome targeting preparation. The hordenine can be captured by the lysosome and accumulated in the lysosome, so that the hordenine has the characteristic of targeting the lysosome, and the hordenine can be used for preparing the lysosome targeting preparation. Hordenine is small in toxic and side effects and high in safety, and the problems that existing lysosomal targeted compounds such as chloroquine are high in toxicity and narrow in therapeutic window are effectively solved.

The application discloses a BN-g-C3N4 / Cs3Bi2Br9 composite photocatalyst for degrading chloroquine phosphate and a synthesis method thereof. The BN-g-C3N4 / Cs3Bi2Br9 composite photocatalyst is characterized by the fact that, as shown by a scanning electron microscope, Cs3Bi2Br9 is in-situ grown on the surface of BN-g-C3N4, and the two monomers form a composite material, and the size and morphology of the two are not obviously changed. The synthesis method of the composite photocatalyst is simple, the photocatalytic activity is high, the method is easy to enlarge, and the composite photocatalyst has good stability and reusability, and has a good engineering application prospect.

The invention discloses a chloroquine structure-containing compound, a composition containing the chloroquine structure-containing compound and application of the chloroquine structure-containing compound and the composition. The invention provides a compound as shown in a formula I or pharmaceutically acceptable salt thereof. The compound containing the chloroquine structure provided by the invention is a nano material synthesized from chloroquine and a derivative thereof and a lipid tail, and the nano material can be applied to gene therapy, drug delivery and the like. The LNP formed by the nano material and mRNA has a novel nano space structure different from that of the traditional LNP, and has better pharmaceutical properties compared with the traditional LNP. The LNP has an immunosuppression function, can avoid causing redundant inflammatory reactions, and has higher safety.

This invention belongs to the field of antitumor drug delivery technology, and discloses a dual-drug sequential delivery system, a composite hydrogel, its preparation method, and its applications. This invention achieves sequential release by encapsulating a cobalt (Co)-polyphenol coordination nanozyme (CoNZ) in a hydrogel and integrating it with microfibrils loaded with chloroquine (CQ). This invention provides a promising new approach to improving the treatment of CRPC by initially inducing ROS-mediated oxidative damage, subsequently inhibiting autophagy and blocking the TLR9 / NF-κB signaling pathway, synergistically disrupting the survival mechanisms of tumor cells.

This invention discloses the application of chloroquine in improving gene editing efficiency. Specifically, it provides a novel use for chloroquine: enhancing the gene editing efficiency of gene editing reagents on recipient biological materials. The gene editing reagent is a gene editing tool plasmid. No prior art studies have combined chloroquine with gene editing efficiency. The inventors of this invention have discovered that treating recipient biological materials with chloroquine before transfecting them with gene editing reagents can significantly improve gene editing efficiency. This invention is simple to operate, widely applicable, and opens up a new avenue for improving editing efficiency by introducing exogenous small molecules rather than directly modifying gene editing tools.

The application belongs to the technical field of pharmaceutical preparations, and particularly relates to a hydroxychloroquine sulfate medicament and a preparation method thereof. The hydroxychloroquine sulfate or / and a filler is granulated by using a granulating liquid with a specific composition, a thin film is covered on the surface of the raw material, and the granule particle size is controlled, so that the moisture absorption and sticking and collision problems which are prone to occur in the hydroxychloroquine sulfate tablet are effectively solved, and the hydroxychloroquine sulfate tablet has consistent dissolution effect with the raw material.

Provided herein are methods of treating inherited retinal degeneration in an eye of an individual, wherein the method comprises: administering: (i) hydroxychloroquine to the individual; and (ii) a Fas-inhibiting peptide to the eye, wherein the peptide comprises an amino acid sequence HHIYLGAVNYIY or variant sequence thereof, or a pharmaceutically acceptable salt thereof.

The present invention belongs to the field of chemical engineering, and particularly relates to a production method of high-quality 2,6-dichloroquinoxaline. In order to improve the quality of 2,6-dichloroquinoxaline and reduce the sulfur residue therein, this method specifically utilizes the characteristics of good water solubility and fast reaction rate of the reaction product of sulfur and sodium hydroxide to separate the residual sulfur in 2,6-dichloroquinoxaline, and a tubular reactor is used in combination to slow down the rate of formation of bis(6-chloroquinoxalin-2-yl)sulfide impurities by the reaction of 2,6-dichloroquinoxaline and S during the desulfurization process, so that the qualified rate of this impurity in the subsequent intermediate and quizalofop-P-ethyl reaches 100%, and the quality competitiveness of quizalofop-P-ethyl is improved.

This invention relates to the field of pharmaceutical biotechnology, providing the application of aminoquinoline compounds (such as hydroxychloroquine and chloroquine) in the preparation of drugs for treating hyperparathyroidism. These compounds restore the expression of calcium-sensitive receptors (CaSRs) on the cell membrane surface by inhibiting the lysosomal degradation pathway of CaSRs in parathyroid cells. Experiments have confirmed that 4-aminoquinoline compounds, used alone or in combination with calcimimetics (such as cinacalcet), significantly reduce serum PTH and calcium levels in a model of refractory secondary hyperparathyroidism (SHPT) and inhibit glandular hyperplasia. In particular, the combination therapy regimen exhibits a significant synergistic effect, effectively reversing calcimimetics resistance. This invention is the first to discover a novel use for the antimalarial / antirheumatic drug hydroxychloroquine in the treatment of hyperparathyroidism, realizing a new use for an existing drug; and providing a safe and effective new drug treatment strategy for clinically refractory SHPT.

The application discloses application of chrysin in preparation of a medicine for treating primary Sjogren's syndrome and belongs to the technical field of biological medicine. The application proves that chrysin can be specifically combined with TNFR2 protein and is a new type of TNFR2 inhibitor through molecular docking, molecular dynamics simulation, CETSA experiment and SPR experiment. Animal experiments show that chrysin can significantly increase the secretion amount of saliva and tear of a mouse model of primary Sjogren's syndrome, reduce the serum SSA and SSB antibody levels, reduce lymphocyte infiltration and acinus atrophy of submandibular glands and lacrimal glands, inhibit the expression of a cytokine INF-gamma, and the drug efficacy is equivalent to that of a positive medicine hydroxychloroquine; chrysin and gaoshunyujin have a synergistic effect, and the improvement effect on primary Sjogren's syndrome is better than that of hydroxychloroquine. The application provides a new medical use of chrysin, and provides a safe and effective prevention and treatment medicine for primary Sjogren's syndrome.

1. Name of the product of this design: Pharmaceutical packaging box (Hydroxychloroquine Sulfate Tablets). 2. Purpose of this design product: This design product is used for the outer packaging box of medicines. 3. The key design point of this design product lies in the combination of shape and pattern. 4. The picture or photo that best illustrates the design points: three-dimensional picture.

The invention discloses a method for synthesizing quinoxaline and derivatives thereof by using a chemical enzyme concerted catalysis system, which is characterized in that 2-(2-amino anilino) ethanol compounds are used as substrates, and the quinoxaline and the derivatives thereof are synthesized in a solvent through chemical enzyme concerted catalysis; wherein the chemical enzymes comprise alcohol dehydrogenase, catalase, natural cofactors and artificial cofactors. The quinoxaline compound disclosed by the invention is one of quinoxaline, 6-fluoroquinoxaline, 6-chloroquinoxaline, 6-bromoquinoxaline, 6-methylquinoxaline, 6-methoxyquinoxaline, 6-hydroxyquinoxaline and the like. The formula of the quinoxaline compound is shown in the description. According to the technical scheme provided by the invention, addition of additional cosubstrates and coenzymes is avoided, the highest substrate conversion rate can reach 95%, and excellent chemical selectivity is achieved. The product synthesized by the synthesis method is good in selectivity and relatively high in yield, and has a relatively good industrial application prospect in preparation of quinoxaline compounds through biological catalysis.

The application belongs to the field of pharmaceutical chemistry and particularly relates to a synthesis method of besuxidil mesylate. First, 2-chloroquinazoline-4-amine a is used as raw material, and then a nucleophilic substitution reaction with 5-bromoindazole b, a Suzuki coupling reaction with 3-hydroxyphenylboronic acid d, a Mitsunobu reaction with 2-hydroxy-N-isopropylacetamide f and a salt reaction with methanesulfonic acid are sequentially performed to obtain besuxidil mesylate. The main route of the application is short, and compared with the existing route, the yield is higher, and the industrial production is facilitated.

Disclosed are a chloroquine structure-containing compound, a composition containing same, and an application thereof. The present invention provides a compound as represented by formula (I) or a pharmaceutically acceptable salt thereof. The chloroquine structure-containing compound provided by the invention is a nano material obtained from the synthesis of chloroquine, a derivative thereof, and a lipid tail. The nano material can be applied to gene therapy, drug delivery, and the like. A lipid nanoparticle (LNP) formed from the nano material and mRNA has a novel nanoscale spatial structure different from that of a traditional LNP, and compared to a traditional LNP, the nano material has better pharmaceutical properties. The LNP exhibits an immunosuppressive function, avoids triggering an excessive inflammatory response, and has a higher safety profile.

The application discloses a kind of full continuous flow preparation methods of pyriproxyfen.The chloro o-nitroaniline solution and hydrogen are transported to fixed bed reactor to carry out continuous catalytic hydrogenation reaction, and the 4-chloro o-phenylenediamine reaction mixture obtained is transported to microchannel mixer and reactor with ethyl glyoxylic acid solution to carry out continuous cyclization reaction, and the 2-hydroxy-6-chloroquinoxaline suspension obtained is entered into continuous online filtering device, and the mixture is transported to micro-mixer and continuous flow reactor with phosphorus oxychloride by peristaltic pump, and the effluent reaction liquid and hydroquinone / catalyst mixture are transported to another fixed bed reactor to carry out continuous etherification;Reaction mixture and (S)-2-chloropropionic acid ethyl ester are entered into fixed bed reactor to carry out continuous etherification reaction;Product pyriproxyfen is obtained;Compared with traditional batch kettle type synthesis method, the method has short reaction time, high product yield, high degree of automation, high process continuous efficiency, high space-time yield, low energy consumption and easy industrial amplification application.

The invention discloses a device and method for preparing chloroquine nano-particle medicine, and relates to the technical field of chloroquine nano-particle medicine preparation, and the device comprises a nitrogen tank, a first storage tank, a first pipeline, a second pipeline, a third pipeline, a pressure flash tank, a spraying device, a condenser, a centrifugal machine, a dryer and a fourth pipeline; the nitrogen tank is communicated with the pressure flash tank while being communicated with the first storage tank; the first storage tank is used for placing a chloroquine acetone solution and is communicated with the pressure flash tank; the spraying device is arranged in the pressure flash tank, and the spraying device sprays and flashes the chloroqualinone solution to form flash gas; the pressure flash tank is communicated with the condenser, the condenser cools flash gas into a mixture of liquid acetone and chloroquine nanoparticles, the centrifugal machine can separate the mixture of liquid acetone and chloroquine nanoparticles, and the drying box can dry chloroquine nanoparticles. The preparation system has the advantages that the structure is simple, operation is convenient, cost is saved, and the preparation speed is effectively increased.

A subject is administered an amount of an active agent effective to treat and / or prevent a neurological disorder, wherein the active agent comprises S-hydroxychloroquine with an enantiomeric excess of at least 20% of the S-enantiomer of hydroxychloroquine. The active agent may further comprise tauroursodeoxycholic acid and / or 3,3'-diindolylmethane. The subject may be diagnosed with a neurological disorder or may be identified as being at risk of developing a neurological disorder. Administering the active agent may at least partially normalize an aberrant level of an indicator characteristic of the neurological disorder.

The present disclosure relates to an effect of inhibiting cancer metastasis by treatment of chlorphenesin and hydroxychloroquine alone or in combination. Chlorphenesin or hydroxychloroquine has the effect of inhibiting the metastasis and invasion of cancer cells. In particular, since it was identified that a combination thereof has a synergistic action, it is possible to effectively prevent or treat cancer metastasis by administering chlorphenesin and hydroxychloroquine respectively or in combination thereof.

The invention relates to the technical field of medicine synthesis, and particularly discloses a synthesis method of besudil mesylate. The besudil mesylate is prepared by taking 3-(4-chloroquinazoline-2-yl) phenyl acetate and 5-amino-1H-indazole-1-tert-butyl formate as initial raw materials through four-step reaction, compared with the traditional process, the reaction route is obviously simplified, the yield loss caused by accumulation of multi-step reaction can be effectively reduced, and the yield of besudil mesylate is increased. And the complexity and the operation difficulty of the synthesis process are reduced. Meanwhile, the intermediate compounds B, C and D all have Boc protecting groups, so that the reaction in each step has higher selectivity, and the purity of the target product is favorably improved. In addition, the synthetic route provided by the invention is mild in reaction condition, the safety of the process can be effectively improved, the reaction energy consumption is reduced, the adopted reagent is relatively environment-friendly, the treatment is relatively easy after the reaction is finished, serious pollution to the environment is avoided, and the industrial prospect is high.

The application discloses a novel coumarin derivative containing a quinazoline unit (as shown in structural formula I), and a preparation method thereof. The preparation method comprises the following steps: subjecting a coumarin molecule A treated by a sodium hydroxide solution to etherification reaction with a 4-chloroquinazoline molecule B in acetonitrile by heating, and then subjecting an intermediate product C obtained by the reaction to reaction with benzyl chloride or bromoethane in acetonitrile by heating, so as to obtain the novel coumarin derivative I containing the quinazoline unit. The novel coumarin derivative containing the quinazoline unit is a novel compound, has obvious inhibiting effect on human pancreatic cancer cells (PANC-1), human gastric cancer cells (SGC7901) and human breast cancer cells (MDA-MB-231), and can be developed as a novel anti-tumor drug candidate molecule.

The invention belongs to the field of medicines, and discloses a compound with a structure shown in a formula I. A preparation method of the compound comprises the following steps: carrying out cyclization reaction on methyl anthranilate containing substituent groups and formamide, and then carrying out chlorination reaction with thionyl chloride to obtain corresponding 4-chloroquinazoline; then, the coumarin molecules sequentially react with sodium hydroxide, 4-chloroquinazoline, TBTU and substituted amine, and the cinnamamide derivative containing the quinazoline unit is obtained. The cinnamamide derivative containing the quinazoline unit is a novel compound, has an inhibition effect on cell proliferation of cervical cancer, lung cancer, liver cancer, pancreatic cancer, gastric cancer or breast cancer, and can be used as a potential antitumor drug candidate molecule.