171 results about "Mesylate" patented technology

The invention relates to the technical field of medicines, in particular to a sustained-release coating as well as a preparation method and application thereof. The coating adopts a three-layer gradient structure design and comprises an inner layer coating, a middle layer coating and an outer layer coating, and the layers are compounded and matched through ethyl cellulose and hydroxypropyl methylcellulose with different molecular weights and are combined with talcum powder filling amount with gradient decreasing and a triethyl citrate plasticizer, so that accurate regulation and control of drug release are realized. Through hierarchical swelling-diffusion dynamic balance, burst release is inhibited, the inner layer has high talcum powder content to resist initial swelling stress, the outer layer has low filling amount to maintain hydrophobic continuity, interface defects are reduced in combination with high-temperature curing, and the release stability and long-term storage performance of drugs such as dihydroergoline mesylate are remarkably improved; the problems of sudden release, damp-heat sensitivity, impurity generation and the like of a traditional single-layer coating are solved.

The present invention discloses a method for preparing a linker-drug conjugate and its intermediates. Specifically, a method for preparing compound LE14 is provided, which comprises subjecting an intermediate compound of formula II to an amide condensation reaction with a compound of formula III or its mesylate in the presence of a condensing agent, a base, and a solvent to obtain a compound of formula I. This method can produce a high-purity intermediate II, which is directly condensed with isotecan mesylate to obtain compound I, and then subjected to subsequent reactions to obtain the final product LE14. The preparation method of the present invention has one or more of the following advantages: using intermediate II as the starting material for the production process reduces process steps, facilitates product quality control, significantly reduces impurities in the final product, and improves purity. Furthermore, using the more economical isotecan for the condensation reaction significantly reduces production costs, making it more suitable for industrial production.

A drug combination of purinostat mesylate and an analog thereof for preventing and treating multiple myeloma, and the use thereof. Specifically, provided is a three-drug or four-drug combination of purinostat mesylate and an analog thereof, dexamethasone and other drug, which drug combination has significantly enhanced synergistic anti-tumor activity in vitro and in vivo, synergistically inhibits the expression of the key survival protein in multiple myeloma, is superior to existing clinical combination regimens, and has no significant toxic side effects. In addition, the drug combination significantly down-regulates the expression of CDK6, and overcomes the drug resistance to an immunomodulator. In particular, the three-drug combination of puisostat mesylate, a glucocorticoid and an immunomodulator has an excellent prevention and treatment effect on multiple myeloma, especially relapsed / refractory multiple myeloma.

Purinostat mesylate (PM) for preventing and treating diffuse large B-cell lymphoma (DLBCL), an analogue thereof, a drug for combined use, and the use. PM exhibits excellent in-vivo and in-vitro anti-tumor therapeutic effects on DLBCL (DEL and DHL) subtypes with poor prognosis, DLBCL subtypes having TP53 deletion and mutation combined with a plurality of poor prognosis gene mutations, and DLBCL having TP53 mutation with double expressors, which are superior to that of most existing DLBCL clinical therapy plans. A doublet or triplet therapy of PM with rituximab, R-CHOP, venetoclax and R-CHP also exhibits excellent in-vivo therapeutic effects against DLBCL and a plurality of subtypes. Thus, PM and the drug for combined use have an important clinical significance for the DLBCL and a plurality of subtypes.

The invention relates to the technical field of medicines, in particular to a dihydroergoline mesylate controlled release tablet and a preparation method thereof. The dihydroergoline mesylate controlled release tablet comprises a tablet core, an inner coating and an outer coating, wherein the tablet core is coated with the inner coating and the outer coating layer by layer; the weight ratio of the tablet core to the inner coating to the outer coating is 50: (6-8): (3-5); the dihydroergoline mesylate tablet solves the problem that the drug release rate of the existing dihydroergoline mesylate tablet is unstable, and realizes more uniform and predictable drug release characteristics. By optimizing preparation components and a preparation process, the controlled-release tablet disclosed by the invention can maintain stable drug concentration in vivo, and the treatment experience of a patient is improved.

The invention relates to the technical field of drug analysis, and particularly discloses an analysis method for measuring the content of a dihydroergoline mesylate bulk drug, which comprises the following steps: step S1, adding the dihydroergoline mesylate bulk drug into anhydrous acetonitrile to obtain a stock solution to be measured, precisely measuring 1mL of the stock solution, adding a cosolvent, uniformly shaking, and fixing the volume to obtain a solution to be measured; s2, taking a dihydroergoline mesylate raw material medicine, adding the dihydroergoline mesylate raw material medicine into anhydrous acetonitrile to obtain a control stock solution, precisely measuring 1mL of the control stock solution, adding a cosolvent, uniformly shaking, and fixing the volume to obtain a control solution; s3, measuring the content of the dihydroergoline mesylate raw material medicine by using a high performance liquid chromatography; according to the present invention, the cosolvent contains the 1-butyl-3-methylimidazole tosilate, the mobile phase of the high performance liquid chromatography contains the elution reinforcing agent, and through the reasonable ratio of the components, the solubility of the dihydroergoline mesylate can be improved, and the accuracy of the high performance liquid chromatography analysis can be improved.

The present invention relates to a process for the preparation of belumosudil mesylate and its crystalline form. Further, the present invention relates to a pharmaceutical composition comprising a therapeutically effective amount of the crystalline form of belumosudil mesylate obtained by the process of the present invention.

The present invention relates to the technical field of drug analysis, and is used to solve the problem that the existing quality method of pazufloxacin mesylate cannot separate photodegradable impurities, and provides a quality control method for pazufloxacin mesylate injection, comprising the following steps: (1) preparing a test solution; preparing a control solution; preparing a reference solution; (2) recording a chromatogram of the reference solution and the reference solution; (3) recording the chromatograms of the test solution and the reference solution; (4) calculating the content of pazufloxacin mesylate by peak area according to the external standard method. The present invention adjusts the ratio of two mobile phases in the gradient according to the polarity of each impurity, and changes isocratic elution to gradient elution, so that each impurity with different polarities can be well separated.

The invention relates to the technical field of pharmaceutical preparations, in particular to a solid dispersion-based sustained-release drug composite carrier as well as a preparation method and application thereof. The preparation method comprises the following steps: carrying out synergistic spray drying on double polymers (hydroxypropyl methylcellulose acetate succinate and polyvinylpyrrolidone-vinyl acetate copolymer) to form a solid dispersion; compounding with mesoporous silica and calcium silicate for localization, and spraying ethanol to activate pores; calcium stearate and magnesium stearate are sequentially added for lubrication; prefabricating a sustained-release skeleton master batch; and finally, mixing, rolling and forming. According to the method, through hierarchical structural design, the drug stability, the powder fluidity and the release controllability are remarkably improved, the method is suitable for industrial production of the dihydroergoline mesylate sustained release preparation, and a release curve is smooth and reliable.

The invention relates to a preparation method of rotigotine, which solves the technical problems of unreasonable reaction steps and higher production cost in the prior art, and comprises the following steps: carrying out chiral amination reduction reaction on 5-methoxy-2-tetralone, chiral phosphate, pinacol borane and p-methoxyaniline to obtain a compound 1; reacting the compound 1 with bromopropane to obtain a compound 2; reacting the compound 2 with ceric ammonium nitrate to obtain a compound 3; dissolving the compound 3 in hydrobromic acid, and reacting to obtain a compound 4; and carrying out a reaction on the compound 4 and 2-thiophene ethyl methanesulfonate to obtain a crude product rotigotine. The method can be applied to the field of preparation of rotigotine.

The present application provides methods of administering besudil mesylate to cGVHD patients.

The invention provides a preparation method of a key intermediate (3aR, 5S, 6aS)-5-(methylamino) hexahydrocyclopenta [c] pyrrol-2 (1H)-tert-butyl formate mesylate of a JAK kinase inhibitor, and belongs to the field of medical intermediates. The preparation method comprises the following steps: taking cis-5-oxohexahydrocyclopenta [C] pyrrol-2 (1H)-carboxylic acid tert-butyl ester as a raw material to react with methylamine equivalent to obtain an intermediate A; then carrying out reduction reaction in metal sodium and isopropanol to obtain a crude product, adding L-DBTA to form salt, removing isomers, and carrying out re-dissociation and salt formation with methanesulfonic acid to obtain a pure product. The method greatly shortens the reaction steps, reduces the raw material cost, is simple and reliable in process, and is easy for industrial production.

The invention discloses a deuterium-labeled stable isotope compound of everolimus and a preparation method thereof, the preparation method comprising: heating and heat-insulating a toluene solution of rapamycin, then adding dropwise a toluene solution containing 2-(tert-butyldimethylsilyloxy)ethyl trifluoromethanesulfonate-d4 and an organic base, stirring and heat-insulating the reaction and then cooling naturally, and post-processing to obtain tert-butyldimethylsilyloxy-everolimus-d4, wherein the organic base is one of N,N-diisopropylethylamine, triethylamine, pyridine and 2,6-lutidine; at 0°C and under nitrogen protection, hydrochloric acid solution is added to a methanol solution of tert-butyldimethylsilyloxy-everolimus-d4, and the reaction solution is reprocessed after the stirring reaction to obtain the product. The present invention ensures that the product does not contain other impurities and non-isotopic everolimus that are difficult to separate by adding an organic base and 2-(tert-butyldimethylsilyloxy)ethyl trifluoromethanesulfonate-d4 simultaneously.

The invention relates to a polymorphic form of an endopiroxostat addition salt as well as a preparation method and application of the polymorphic form. The acid addition salt is selected from the group consisting of hydrochloride, sulfate, phosphate, mesylate, benzene sulfonate, p-toluenesulfonate, hydrobromide, maleate, tartrate, citrate and fumarate, preferably hydrochloride. The endopiroxostat addition salt polymorph is high in stability, high in solubility, high in blood concentration, high in bioavailability and excellent in pharmacological action, so that the endopiroxostat addition salt is suitable for pharmaceutical preparations.

The invention provides a bromocriptine mesylate enteric-coated tablet and a preparation method thereof. Specifically, the bromocriptine mesylate enteric-coated tablet comprises a tablet core and an enteric coating layer wrapping the tablet core. The enteric-coated tablet disclosed by the invention is simple in process, good in stability and small in gastrointestinal side effect, the bioavailability of the enteric-coated tablet is more than two times that of a common tablet sold in the market, the dosage is expected to be reduced, the side effect is further reduced, and the enteric-coated tablet has excellent clinical value.

The invention belongs to the technical field of biological medicines, and particularly relates to a method for determining the contents of six elements in an amine silver mesylate lactone B powder injection preparation for injection. The method comprises the following steps: preparing a diluent, preparing a standard adding solution, preparing an element stock solution, preparing a standard curve solution, verifying linear parameters, verifying a limit of quantitation (LOQ), verifying specificity and verifying accuracy. Therefore, the content can be accurately measured, and clinical medication standards can be guided.

The invention discloses treatment of EGFR mutation positive non-small cell lung cancer brain metastasis by administering an effective dose of an EGFR inhibitor. The EGFR inhibitor is N-(2-((2-(dimethylamine) ethyl) (methyl) amine)-4-methoxy-5-((4-(1-deuterated methyl-1H-indol-3-yl) pyrimidine-N '-2-yl) amine) phenyl) acrylamide mesylate.

The invention belongs to the technical field of chemical analysis, and particularly relates to a method for separating and determining a rucotinib mesylate intermediate Z1 and related impurities thereof. The impurities comprise any one or more of an impurity SM2a, an impurity SM1d, an impurity Z1c, an impurity Z1b, an impurity Z1a, triphenylphosphine oxide, an impurity SM2, an impurity SM1 and an impurity Z1d. Octadecylsilane chemically bonded silica is adopted as a chromatographic column filling agent; a monopotassium phosphate buffer solution is used as a mobile phase A, a mixed solution of methanol and acetonitrile is used as a mobile phase B, and main components are separated from impurities through gradient elution; and detecting in a detector to obtain a chromatogram. The method is high in specificity, short in separation time, high in sensitivity and good in durability, and has important significance on quality control of rukotinib mesylate bulk drugs and preparation products.

The invention relates to the technical field of chemical pharmacy, and particularly discloses a preparation method of nafamostat mesylate. The preparation method comprises the following steps: adding 6-amidinyl-2-naphthol mesylate, 4-guanidinobenzoic acid hydrochloride and EDCI into a first solvent, and carrying out condensation reaction; adding a saturated sodium bicarbonate aqueous solution to obtain an intermediate; and adding the intermediate into a second solvent, adding methanesulfonic acid to form salt, and purifying to obtain the nafamostat mesylate. EDCI firstly reacts with a first solvent and is activated, nitrogen atoms with positive charges in EDCI after oxygen atoms on carbonyl carbon of carboxylic acid are activated are positively charged, the electrophilicity of carboxylic acid is increased, an active intermediate is formed, the active intermediate and alcohol are more easily subjected to nucleophilic substitution reaction, and dehydration condensation is performed to form an ester bond. EDCI is used as a condensing agent, so that the production efficiency and yield of the nafamostat mesylate are improved, the purity of the nafamostat mesylate is improved, the impurity content is reduced, the cost is low, and industrial production is easy.

Mesylates of heterocyclic cytokinins of general formula I:wherein R is selected from the group comprising C3-C15 cycloalkyl, furfuryl, allyl, 4-hydroxy-3-methylbut-2-en-1-yl, 3-methylbut-2-en-1-yl, 4-hydroxy-3-methylbutyl, 4-hydroxy-1,3-dimethylbut-2-en-1-yl, 4-hydroxy-1,3-dimethylbutyl, benzyl, wherein the cycloalkyl, allyl, benzyl and furfuryl may be unsubstituted or optionally substituted with 1 to 3 substituents selected from the group containing hydroxy, halogen, methyl, hydroxymethyl and methoxy, and salts, solvates and addition salts thereof. These compounds are particularly suitable for agricultural and biotechnological use, and their great advantage is increased water solubility as compared to the corresponding free bases of heterocyclic cytokinins.

The present disclosure provides methods of administering a Bruudil mesylate to certain subpopulations of patients suffering from cGVHD.

The invention provides a synthesis method of a pyridine salt compound. A 2-(trimethylsilyl) phenyl trifluoromethanesulfonate compound is used as a benzyne precursor, cesium fluoride is used as alkali, and the 2-(trimethylsilyl) phenyl trifluoromethanesulfonate compound reacts with 6-azaindole in acetonitrile without additional catalysts or under the protection of special conditions to prepare the pyridine salt compound. The reaction overcomes the defects of overlong route, harsh requirements on substrates and reaction conditions, limited expansion of substituted functional groups and the like in the previous reaction. According to the reaction, substrate synthesis is simple, reagents are cheap, the operation method is simple, and an efficient and practical novel method is provided for synthesis of pyridine salt compounds with important value in industrial production and bioactive compounds.

The invention discloses a salt form of a coronavirus 3CL protease inhibitor PLC-01 as well as a preparation method and application of the salt form, and belongs to the technical field of medicinal chemistry. Salt types of PLC-01 comprise inorganic acid salt, organic acid salt, sodium salt and a free state. According to the present invention, various organic acids, inorganic acids and solvents are mainly screened so as to obtain the PLC-01 hydrochloride Pattern A, the PLC-01 mesylate Pattern A, the PLC-01 sodium salt Pattern C and the PLC-01 free state Pattern A, wherein the PLC-01 hydrochloride Pattern A, the PLC-01 mesylate Pattern A, the PLC-01 sodium salt Pattern C and the PLC-01 free state Pattern A have characteristics of high purity and good stability; the invention also discloses a pharmaceutical composition of the salt form of the compound shown in the formula I. All salt forms of PLC-01 in the invention have strong inhibition efficacy on 3CL protease, and are expected to become novel active pharmaceutical ingredients for preventing or treating novel coronavirus infection.

The invention belongs to the technical field of biological medicines, and particularly relates to an application of Mitoquinone mesylate in resisting mycobacterium tuberculosis infection. According to the application disclosed by the invention, the biological effect of the Mitoquinone mesylate in resisting mycobacterium tuberculosis infection is found, the MIC of the Mitoquinone mesylate to a mycobacterium tuberculosis standard strain can reach 1.25 mu M, and the MIC of the Mitoquinone mesylate to a drug-resistant mycobacterium tuberculosis clinical isolated strain is more concentrated to be 1.25 mu M. In conclusion, the autophagy regulation effect of the Mitoquinone mesylate is remarkable, and the Mitoquinone mesylate can become a new treatment medicine in the anti-mycobacterium tuberculosis infection process. The clinical guiding significance is realized; moreover, the Mitoquinone mesylate is easy to obtain and low in cost, the prepared medicine takes effect quickly, and the Mitoquinone mesylate has actual production and application prospects. The Mitoquinone mesylate is high in safety, small in side effect and good in patient compliance.

The invention provides an inorganic perovskite solar cell based on a sulfonic ionic liquid additive. The perovskite solar cell comprises a flexible substrate, a hole transport layer, an inorganic perovskite thin film layer, an electron transport layer and an electrode layer. Wherein the additive is one or more of 1-propyl-3-methylimidazole mesylate ionic liquid, 1-propyl sulfonic acid-3-methylimidazole chlorine salt ionic liquid and 1-propyl sulfonic acid-3-methylimidazole hydrogen sulfate ionic liquid. The strong interaction between sulfonic acid groups in the additive and Cs ions in the inorganic perovskite reduces the phase transition energy barrier of the inorganic perovskite from a yellow phase to a black phase, the preparation temperature can be reduced to 100 DEG C or below, and finally device preparation is successfully carried out on a flexible substrate with limited heat resistance. And the flexible inorganic perovskite solar cell with relatively good performance and stability is realized. By reducing the preparation temperature of the black-phase inorganic perovskite thin film, the problem that the high preparation temperature of inorganic perovskite is incompatible with the heat resistance of the flexible substrate is solved.

The invention relates to mesylate of a heterocyclic substituted fused gamma-carboline derivative, a crystal form and a preparation method and application thereof. In particular, the present invention relates to a mesylate and a crystal form of a compound (6bR, 10aS)-8-(4-(4-fluorophenyl)-4-oxobutyl)-3, 6b-dimethyl-6b, 7, 8, 9, 10, 10a-hexahydro-1H-pyridine [3 ', 4': 4, 5] pyrrole [1, 2, 3-dequinoxaline-2 (3H)-one, a preparation method and application thereof, and a pharmaceutical composition containing a therapeutically effective amount of the mesylate and the crystal form of the compound, the invention also relates to application of the compound in preparation of medicines for preventing and / or treating neuropsychiatric diseases.

The present disclosure relates to a pharmaceutically acceptable salt and a crystal form of a fused pyridine ring derivative and a preparation method therefor. Specifically, the present disclosure relates to a choline salt, sodium salt, potassium salt, calcium salt, arginine salt, lysine salt, meglumine salt, ethanolamine salt, hydrosulfate, hydrochloride, tartrate, maleate, citrate, malate, p-toluenesulfonate, and mesylate, and a crystalline form of a compound as represented by formula (I).

1. Name of the designed product: packaging box (veterinary fleroxacin mesylate injection); 2. Use of the designed product: veterinary drug packaging; 3. Design points of the design: the pattern of the product; 4. Picture or photo best indicating the design points: front view.