7 results about "Gemfibrozil" patented technology

The invention discloses a gemfibrozil deuterated derivative as shown in a formula (I) as well as a preparation method and application thereof, and belongs to the field of organic and pharmaceutical synthesis. The method is simple in preparation process and low in cost. The gemfibrozil deuterated derivative synthesized by the method has the advantages of high purity and high deuterated rate. The invention also discloses an application of the gemfibrozil deuterated derivative in treatment of hyperlipidemia. The pharmacological action of the gemfibrozil deuterated derivative disclosed by the invention is obviously improved, and toxic metabolites of the gemfibrozil deuterated derivative are obviously reduced.

The invention provides a preparation method of a key intermediate of a gemfibrozil impurity A, and belongs to the technical field of chemical synthesis. According to the invention, a brand-new synthetic route of the gemfibrozil impurity A is designed firstly, and efficient preparation methods of three key intermediates are provided on the basis of the brand-new synthetic route. Specifically, the preparation method comprises the following steps: firstly, reacting with propionyl chloride in a 1, 2-dichloroethane environment under the catalysis of aluminum trichloride, and cooling, layering and drying a product to obtain a first intermediate; taking the first intermediate as a raw material, reacting with benzyl bromide in a DMF (Dimethyl Formamide) environment by taking potassium carbonate as an acid-binding agent, collecting an organic phase, dissolving with methanol, carrying out reduction reaction by using sodium borohydride under the catalysis of cerium chloride heptahydrate, and collecting to obtain a second intermediate; taking the second intermediate as a raw material, dissolving the second intermediate in methylbenzene, and performing dehydration reaction under the catalysis of TsOH.H2O to obtain a third intermediate; on the basis of the three intermediates, efficient synthesis of the gemfibrozil impurity A can be achieved, the synthesis route is short, and the process efficiency is high.

The invention provides a synthetic method of a gemfibrozil impurity A, and belongs to the technical field of chemical synthesis. According to the technical scheme, gemfibrozil is used as an initial raw material and firstly reacts with propionyl chloride in a 1, 2-dichloroethane environment under the catalysis of aluminum trichloride, a product reacts with benzyl bromide in a DMF environment by taking potassium carbonate as an acid-binding agent, an organic phase is collected and dissolved with methanol, and then reduction reaction is performed with sodium borohydride under the catalysis of cerium chloride heptahydrate to obtain gemfibrozil. Collecting to obtain an oily liquid compound, dissolving the oily liquid compound in toluene, carrying out a dehydration reaction under the catalysis of TsOH.H2O, carrying out a hydrolysis reaction on the reaction product in an isopropanol and sodium hydroxide system, carrying out reduced pressure distillation to remove isopropanol, carrying out acid adjustment, extracting with ethyl acetate, drying with sodium sulfate, filtering, concentrating to obtain a white solid, and finally refining and purifying to obtain the 2-(2, 4-dichlorophenyl)-1, 2, 3, 4, 5-tetramethyl-1, 3-pentanediol. A gemfibrozil impurity A finished product is obtained. The method is short in synthetic route, high in process efficiency, convenient to refine and purify and high in yield and purity, and has outstanding technical advantages.

The present disclosure generally relates to an improved pharmaceutical composition for the treatment of juvenile neuronal wax-like lipofuscia (JNCL) or juvenile Batton's disease, said disease being a deadly hereditary neurodegenerative disease in children caused by impairment of Cln3 gene function. The present disclosure also relates to a pharmaceutical composition for use in the treatment of juvenile neuronal wax-like lipofuscia (JNCL) or juvenile Batton's disease. More specifically, the present disclosure relates to a pharmaceutical composition comprising oral gemfibrozil for use in the treatment of juvenile neuronal wax-like lipofuscia (JNCL) or juvenile barton's disease.

In an aspect, the disclosure relates to a liquid pharmaceutical composition comprising, consisting essentially of, or consisting of gemfibrozil and an aqueous solvent. The disclosure also relates to methods of making the liquid pharmaceutical composition comprising gemfibrozil, uses thereof, and methods of treatment comprising administering the liquid pharmaceutical composition comprising gemfibrozil.

The application discloses a gemfibrozil deuterated derivative as shown in formula (I) and a preparation method and application thereof, and belongs to the field of organic and pharmaceutical synthesis. The method has simple preparation process and low cost. The gemfibrozil deuterated derivative synthesized by the method has the advantages of high purity and high deuterium substitution rate. The application also discloses application of the gemfibrozil deuterated derivative in treatment of hyperlipidemia. The gemfibrozil deuterated derivative has significantly improved pharmacological effect and significantly reduced toxic metabolites.

The present disclosure generally relates to improved pharmaceutical compositions useful for the treatment of juvenile neuronal ceroid lipofuscinosis (JNCL) or Juvenile Batten Disease which is a fatal inherited neurodegenerative disease of children caused by impairments in Cln3 gene function. More particularly, the disclosure relates to pharmaceutical compositions comprising oral gemfibrozil for the treatment of juvenile neuronal ceroid lipofuscinosis (JNCL) or Juvenile Batten Disease.