67 results about "Azacitidine" patented technology

Compounds and compositions of azacytosine analogs and derivatives are provided. In one aspect of the invention, analogs or derivatives of decitabine and azacitidine are provided with modification at the 4- and 6-position of the triazine ring, at the 1′-6′position of the ribose ring, or combinations thereof. Methods of synthesizing and manufacturing these analogs and derivatives are also provided. These compounds can be formulated into pharmaceutical compositions that can be used for treating any disease that is sensitive to the treatment with decitabine or azacitidine, such as hematological disorders and cancer.

Compounds and compositions of azacytosine analogs and derivatives are provided. In one aspect of the invention, analogs or derivatives of decitabine and azacitidine are provided with modification at the 4- and 6-position of the triazine ring, at the 1′–6′ position of the ribose ring, or combinations thereof. Methods of synthesizing and manufacturing these analogs and derivatives are also provided. These compounds can be formulated into pharmaceutical compositions that can be used for treating any disease that is sensitive to the treatment with decitabine or azacitidine, such as hematological disorders and cancer.

The invention discloses a phosphoryl N-fatty acyl nucleoside analogue for treating viral hepatitis and liver cancer. The phosphoryl N-fatty acyl nucleoside analogue is characterized in that a nucleoside analogue is modified by a cyclophosphoryl group and then is connected to aliphatic chains having different numbers of carbon atoms. The phosphoryl N-fatty acyl nucleoside analogue can be used for convenient preparation of a nanometer transmission system and has obvious hepatocyte and tumor targeting. The nanometer transmission system comprises liposome, nonionic surfactant niosomes, nanoparticles, nano-emulsion and a self-assembled transmission system. The nucleoside analogue is selected from lamivudine, adenine arabinoside, cidofovir, gemcitabine, cytosine arabinoside, azacitidine and fludarabine. After intravenous administration, the nanometer transmission system of the phosphoryl N-fatty acyl nucleoside analogue has effects of targeting treatment on viral hepatitis and liver cancer.

A process of synthesizing a 5-azacytosine nucleoside, such as azacitidine and decitabine, comprises coupling a silylated 5-azacytosine with a protected D-ribofuranose of formula in the presence of a sulfonic acid catalyst.

The invention belongs to the field of medical chemistry, and particularly relates to a preparation method of impurity component cyanurodiamide pentose of azacitidine. The method is characterized in that N2, N4-bi(trimethylsilyl)-6-trimethylsilyl-1,3,5,- triazine-2,4-diamine which is adopted as a raw material has condensation reaction with tetra-o-acetyl-d-ribose under the protection of trimethylsilyl and under the catalysis of aluminium trichloride, boron trifluoride, zinc chloride or titanium tetrachloride at the temperature of -10 to 20 DEG C, and then a protecting group on the sugar is removed to prepare the cyanurodiamide pentose.

The invention provides azacitidine lyophilized powder for injection. The azacitidine lyophilized powder is prepared from, by weight, 2-8 parts of azacitidine, 2-8 parts of mannitol, 100-300 parts of acetonitrile and 684-896 parts of water. The invention further provides a preparation method of the azacitidine lyophilized powder for injection. The preparation method comprises the steps that part ofthe water for injection is added into a liquid preparation tank; 100-300 parts by weight of acetonitrile is added, and stirring is conducted until the mixture is clear; 2-8 parts by weight of mannitol is added, stirring is conducted until the mixture is completely dissolved, and the temperature is lowered to be 0-4 DEG C; 2-8 parts by weight of a pre-micronized raw azacitidine material is weighed, washed with part of the remaining water for injection and then added into the liquid preparation tank, intensive stirring is conducted until the mixture is dissolved, and the water for injection isadded to reach the constant volume of 1000 parts; after sterile filtration, filling and freeze-drying, the preparation product is obtained. The particle size of the product and the total impurity level of the product can be effectively controlled, the stripping curve and other bioequivalence indexes of the product are equivalent to those of an original research product, and the total impurity level is lower than that of the original research product.

The invention discloses an impurity detection method, in particular to a detection method for tetraacetylribose in azacitidine. The method adopts high performance liquid chromatography, a octadecyl silane bonded silica gel chromatographic column is selected, and water-methanol is employed as the mobile phase to conduct isocratic elution, the flow rate is 0.8-1.2mL / min, the column temperature is 25-35DEG C, and the detection wavelength of the sample is 205nm-215nm. The mobile phase is employed to perform isocratic elution, wherein the volume percentage of methanol is 30-45%. The detection method has the advantages of high sensitivity, high accuracy, good impurity peak shape symmetry, and high column efficiency, etc.