38 results about "Istradefylline" patented technology

The present invention provides a method of treating behavioral disorders such as attention deficit hyperactivity disorder, comprising administering an effective amount of (E)-8-(3,4-dimethoxystyryl)-1,3-diethyl-7-methylxanthine or a pharmaceutically acceptable salt thereof to a patient in need thereof and the like.

The invention discloses a synthetic method of istradefylline, and belongs to the technical field of medicines. The synthesis method of the istradefylline mainly comprises the steps of acylation, ringclosing, methylation and the like. The method is high in yield, simple in step and single in solvent, wherein reaction selectivity can be effectively promoted and side reactions are reduced; after ring closing is finished, dimethyl sulfate is dropwise added for a methylation reaction by means of the alkalinity of dimethyl sulfate. The method can be more thorough and cleaner than a dimethyl carbonate reaction in the prior art. The whole process can be carried out in one reaction kettle, wherein the solvent only relates to ethanol and subsequently refined methanol and can be recycled, so that the synthesis method has advantages of high reaction selectivity and yield.

The invention relates to an istradefylline raw material drug and a preparation method thereof. Specifically, the invention relates to an istradefylline raw material drug. A compound shown in formula III is not higher than 0.5% and is a medicine preparation consisting of the istradefylline raw material drug and a pharmacologically acceptable carrier and / or diluent. The raw material drug and the preparation thereof have better safety, effectiveness and stability. The formula III is shown in the description.

The invention relates to a preparation method for Istradefylline represented by a formula (I) shown in the description. The method comprises the following steps: subjecting 6-amino-1,3-diethyl-5-nitroso-1H-pyrimid-2,4-dione represented by a formula (II) shown in the description, which serves as a raw material, to catalytic reduction and salt forming, so as to obtain 5,6-diamino-1,3-diethyl-1H-pyrimid-2,4-dione hydrochloride represented by a formula (III) shown in the description; then, carrying out acetylation on the compound (III), so as to obtain N-(6-amino-1,3-diethyl-2,4-dioxo-1,2,3,4-tetrahydropyrimid-5-yl)acetamide represented by a formula (IV) shown in the description; carrying out further ring closing, so as to obtain 1,3-diethyl-8-methyl-1H-purin-2,6(3H,7H)-dione represented by a formula (V) shown in the description; and carrying out methylation on the compound (V) firstly, and then, subjecting the methylation product to a condensation reaction with veratraldehyde represented by a formula (VII) shown in the description, thereby obtaining the end product Istradefylline. According to the novel preparation method for the Istradefylline, provided by the invention, raw materials, which are readily available industrially and are low in price, are used, the production process is more environmentally friendly, and the obtained product Istradefylline is high in yield and purity, thereby having a relatively high practical value.

The invention discloses a preparation method of an istradefylline impurity standard. Istradefylline is subjected as a raw material to Lewis acid catalysis [2+2] cycloaddition, the reaction product is then refined to obtain pure 8,8'-((1R,2R,3S,4S)-2,4-bis(3,4-dimethoxyphenyl)cyclobutane-1,3-diyl)bis(1,3-diethyl-7-methyl-1H-purine-2,6(3H,7H)-dione), and the content of the pure product is calibrated by conventional analytic means. The preparation method provided herein is simple and has a short preparation cycle, and the calibrated content is higher than 99.0%. Istradefylline impurity provided herein may act as an impurity standard, applied to the qualitative and quantitative study and detection on istradefylline material and its preparation impurities.

The invention discloses a high-performance liquid chromatography analytical method for istradefylline related substances. A reversed phase chromatographic column and an ultraviolet detector are adopted for isocratic elution with acetonitrile-phosphate buffer as a mobile phase. All known impurities in raw materials and preparations of istradefylline can be analyzed simultaneously, contents of the known impurities can be effectively controlled by a main component self contrast method with correction factors, a degree of separation between each impurity peak and a main peak is larger than 1.5, and purity of each impurity peak and the main peak is 1.0. The high-performance liquid chromatography analytical method for the istradefylline related substances is a high-specificity simple analytical method for quality control analysis of the raw materials and the preparations of the istradefylline.

Iguratimod, Repirinast, Lobenzarit, Actarit, Ifenprodil, Bemithyl, Bromantane, Emoxypine, Udenafil, and / or Istradefylline are used for the treatment or prophylaxis of renal fibrosis, kidney disease, or chronic kidney disease in a subject.