5 results about "Glimepiridum" patented technology

The application discloses a kind of screening and anti-myeloma application of targeting c-Maf small molecule inhibitor, especially provide the application of sorafenib or glimepiride in preparation anti-myeloma drug.Aspect.The application discloses a kind of method for screening targeting c-Maf small molecule inhibitor, it includes the steps based on molecular virtual screening docking.It is found that potential compound glimepiride and sorafenib can inhibit the activity of c-Maf by the method of the application through virtual screening, molecular dynamics (MD) simulation, molecular mechanics and MM / GBSA free energy calculation and experimental analysis, both can induce the cycle stagnation and cell apoptosis of myeloma cell.The method of the application can screen more targeting c-Maf small molecule inhibitor, it is also helpful to further structure optimization based on sorafenib and glimepiride in the future, and design c-Maf small molecule inhibitor with better activity.

The invention relates to a glimepiride derivative AX-134, which contains 5-aminovaleric acid methyl ester hydrochloride and pharmaceutically acceptable reaction materials, and is prepared by the following steps: dissolving the 5-aminovaleric acid methyl ester hydrochloride in an organic solvent, then adding phenyl chloroformate, then adding an alkali, reacting at room temperature for 0.5-6 hours, adding 1M diluted hydrochloric acid, extracting, and concentrating to obtain the glimepiride derivative AX-134. The preparation method comprises the following steps: dissolving 4-[2-(3-ethyl-4-methyl-2-oxo-3-pyrroline-1-formamido) ethyl]-benzenesulfonamide (CAS: 119018-29-0) in an organic solvent, adding an alkali, carrying out a reflux reaction for 2-12 hours, carrying out reduced pressure distillation to remove acetonitrile, adding ethyl acetate and a 1M sodium hydroxide aqueous solution (V / V = 1: 1), carrying out a reaction for 2-12 hours, and carrying out reduced pressure distillation to obtain the 4-[2-(3-ethyl-4-methyl-2-oxo-3-pyrroline-1-formamido) ethyl]-benzenesulfonamide compound, namely the 4-[2-(3-ethyl-4-methyl-2-oxo-3-pyrroline-1-formamido) ethyl]-benzenesulfonamide compound. Stirring reaction and liquid separation are performed, the pH value of a water phase is adjusted with concentrated hydrochloric acid, filtering is performed after stirring overnight, white solids are obtained and dried, and the glimepiride derivative AX-134 is obtained; the method can conveniently realize hectogram-level preparation in a laboratory, and is suitable for large-scale production.

The invention discloses a pharmaceutical composition for targeted activation of FSP1 and application of the pharmaceutical composition. The pharmaceutical composition comprises a medicine capable of activating ferroptosis inhibitory protein 1 and a reduced coenzyme I capable of enhancing the ferroptosis inhibitory protein 1 activation effect of the medicine. The medicine capable of activating the ferroptosis inhibition protein 1 comprises a second-generation sulfonylurea medicine; and the second generation sulfonylurea medicine is glimepiride or glibenclamide. The glimepiride, glibenclamide and other second-generation sulfonylurea drugs are combined with NADH, and the resistance of cells to ferroptosis can be remarkably improved by activating or improving the activity of FSP1, so that cell death after ischemia-reperfusion injury is inhibited; meanwhile, the invention provides new application of the glimepiride, the glibenclamide and other hypoglycemic drugs, the adaptation diseases of the glimepiride, the glibenclamide and other hypoglycemic drugs are expanded, and the glimepiride, the glibenclamide and other hypoglycemic drugs are combined with the NADH, so that the glimepiride, the glibenclamide and other hypoglycemic drugs can be used for treating ischemia reperfusion injury related diseases and organ preservation liquid to improve the protection effect on organs.

This invention relates to a glimepiride tablet and its preparation method. The glimepiride tablet, by weight, comprises: 2.0 parts glimepiride, 150-160 parts diluent, 8-15 parts disintegrant, 0.8-1.2 parts binder, and 0.8-1.2 parts lubricant. The diluent is selected from any one or more of the following: lactose, microcrystalline cellulose, or combinations thereof. This invention optimizes the product formulation and preparation process of glimepiride tablets, reducing the impurity content in the tablets and significantly improving the product's stability and dissolution performance.