3results about How to "Reduce cardiotoxicity" patented technology

This invention provides a pharmaceutical composition containing hezemibrate and an HMG-CoA reductase inhibitor, and may further include one or more excipients selected from calcium carbonate, butylated hydroxyanisole, butylated hydroxytoluene, citric acid, sodium lauryl sulfate, polysorbate, croscarmellose sodium, crospovidone, microcrystalline cellulose, povidone, hydroxypropyl cellulose, lactose, pregelatinized starch, magnesium stearate, and talc. This composition can be formulated into various dosage forms, exhibiting good formulation stability and controllable quality.

This invention provides a benzothiadiazine 1,1-dioxide compound, its preparation method, and its applications. The general structural formula of the benzothiadiazine 1,1-dioxide compound is shown in Formula (I), or its isomers, or pharmaceutically acceptable salts, esters, or prodrugs thereof. The benzothiadiazine 1,1-dioxide compound of this invention has a novel structure, can selectively inhibit HDAC6 enzyme, has a strong protective effect on nerve cells, low toxicity, and low potential cardiotoxicity, and is expected to be used as a neuroprotective agent for the treatment of neurodegenerative diseases.

The application discloses an imiquimod prodrug and a preparation method and application thereof, and the structural formula of the imiquimod prodrug is shown in the following formula: the preparation method of the imiquimod prodrug comprises the following steps: step one, dissolving excessive imiquimod in anhydrous dioxane under a protective atmosphere, and dropping propargyl chloroformate dissolved in anhydrous dioxane under ice bath to obtain a mixture; step two, stirring the mixture obtained in the step one at 45-55 DEG C overnight; step three, filtering the product obtained in the step two, recovering excessive imiquimod, and purifying the filtrate after concentration and drying under reduced pressure to obtain the imiquimod prodrug. By using propargyloxy carbonyl to protect the amino group of the IMQ drug, the toxicity of the IMQ drug to cells is significantly reduced, and the systemic inflammatory response in mice is reduced; by using propargyloxy carbonyl to protect the amino group of the DOX drug, the toxicity of the DOX drug to cells is significantly reduced, and the cardiotoxicity in mice is reduced.