249 results about "Agomelatine" patented technology

The crystalline form V of a compound of formula (I) is characterised by the X diffraction diagram thereof on a powder.

The crystalline form IV of a compound of formula (I) is characterised by the X diffraction diagram thereof on a powder.

The crystalline form III of a compound of formula (I) is characterised by the X diffraction diagram thereof on a powder, and the drugs contains it.

A process for the industrial synthesis and a new crystalline form of the compound of formula (I):

Medicinal products containing the same which are useful in treating disorders of the melatoninergic system.

The invention discloses a preparation method of an agomelatine I type crystal which is an anti-depressant. The preparation method comprises the following steps of: dissolving crude agomelatine in a hydrophily organic solvent, filtering, dropping the filtrate into water under stirring, separating out solids and drying; wherein the weight part ratio of the hydrophily organic solvent to the water is 1:2-50. The agomelatine I type crystal prepared by the invention has excellent quality, good reproducibility, and high purity of HPLC normalization method to be above 99 percent, and is more suitable for large-scale industrialization production.

The invention relates to a novel dispersible tablet which is prepared from a certain amount of antipsychotic medicines or pharmaceutically acceptable salt or ester thereof or mixture thereof, a certain amount of selective serotonin reuptake inhibitors (SSRIs) and at least one of pharmaceutically acceptable carriers, wherein the antipsychotic medicines are aripiprazole, fluvoxamine, escitalopram, olanzapine, mirtazapine, clozapine, ziprasidone, mianserin, agomelatine, lurasidone, iloperidone, blonanserin, moclobemide, timiperone, palipeddone, trimipramine, carpipramine, lofepramine or mosapramine. The novel dispersible tablet is used for preventing, delaying or treating depression or schizophrenia of patients. Compared with common tablets or capsules, the novel dispersible tablet has the characteristics of quick and uniform dispersion, short disintegration time, quick medicine absorption, high bioavailability and good stability, and is convenient to take.

The invention discloses a preparation method of an agomelatine I crystal form, which comprises the steps of: adding agomelatine into a mixed solvent of amide and water, heating for dissolving, then reducing the temperature and separating out crystals, and drying to obtain a solid. The agomelatine is dissolved in the heated mixed solvent of the amide and water, and separated out slowly in a cooled mixed solvent of the amide and water, and the high-purity I crystal form can be stably obtained. The method has the advantages of high purity of reaching above 99 percent of the single crystal form, simple operation and good repeatability, and the like and is suitable for industrialized production.

The invention relates to agomelatine benzenesulfonic acid compound of a formula I and a preparation method thereof; the agomelatine benzenesulfonic acid compound obtained by the invention is good in product stability, high in purity and is suitable for application demand when finished drug is prepared; preparation technology is also very simple; and a high-purity product can be obtained without special operation, wherein in the formula (I), R=CH3, H.

The invention provides a copolymer containing amorphous agomelatine. The detection of a sample of the copolymer by Differential Scanning Calorimetry (DSC) and X-ray powder diffraction shows that the sample has stable properties. The copolymer mainly comprises agomelatine raw material, carrier and solvent. The invention also provides a preparation method of the copolymer containing amorphous agomelatine, and the method has good reproducibility. The invention further provides a pharmaceutical composition containing the copolymer containing amorphous agomelatine and an application of the copolymer containing amorphous agomelatine in preparing medicines for treating depression.

The invention provides an agomelatine-containing orally disintegrating tablet, which is characterized in that the inclusion technology is adopted to prepare the agomelatine-containing orally disintegrating tablet. The invention effectively covers up the tingling of agomelatine, improves the dissolution of the agomelatine, and is suitable for industrial production.

The invention relates to an agomelatine crystal form B, a preparation method thereof and a medicinal composition containing the same.

The invention provides an agomelatine solid preparation. Agomelatine and a carrier are subjected to hot melt extrusion to form solid dispersoid of agomelatine, and the solid dispersoid of agomelatine can be further prepared into the solid preparation. A product can be dissolved out well and is controllable in quality.

Crystalline form V of the compound of formula (I):

characterised by its powder X-ray diffraction diagram. Medicinal products containing the same which are useful in the treatment of melatoninergic disorders.

The invention aims at providing a preparation method of 2-(7-anisyl-1- naphthyl) ethylamine (II) which is an important midbody of agomelatine. The preparation method uses 2- (7-anisyl-1-naphthyl) acetamide (VII) as an initiative raw material, only needs one reaction step, has higher yield, abolishes high-voltage hydrogenation, has mild conditions and does not need special devices.

The invention relates to an agomelatine sulfuric acid composition shown in the formula I and a preparation method of the agomelatine sulfuric acid composition. The agomelatine sulfuric acid composition obtained by using the preparation method is good in stability and high in purity, and is suitable for application in finished-product medicinal preparations. The preparation process is also quite simple, so that the product with high purity can be obtained without special operations.

The invention discloses agomelatine-isonicotine eutectic crystal which has the chemical formula (I). The diffraction angles 2theta can be 10.20 DEG, 14.43 DEG, 15.97 DEG, 17.64 DEG, 18.57 DEG, 19.22 DEG, 19.91 DEG, 20.68 DEG, 21.39 DEG, 21.66 DEG, 21.94 DEG, 23.16 DEG, 24.28 DEG, 24.75 DEG, 25.42 DEG, 29.54 DEG, 29.90 DEG and 30.39 DEG. The agomelatine-isonicotine eutectic crystal is prepared by melting agomelatine and isonicotine and cooling. The agomelatine-isonicotine eutectic crystal is easy to prepare and has low preparation cost.

The invention relates to a preparation method for an intermediate compound for preparing agomelatine. The agomelatine intermediate 2-(7-methoxyl-1-naphthyl) acetamide is directly obtained by the ammonolysis of (7-methoxyl-1-naphthyl) ethyl acetate. The method has high reaction yield; reagents used have low cost; the method also has relatively mild reaction condition, safe operation and good controllability. Besides, the whole reaction process is not added with highly toxic reagent or solvent, thus meeting the requirement of environmental protection and being very suitable for industrialized production application.

The invention belongs to the technical field of medicine, and discloses a medicine composition containing agomelatine prepared form components of, by weight: 11% to 25% of agomelatine, 30% to 65% of lactose, 11% to 40% of starch, 8% to 15% of carboxymethylstarch sodium, 0.5 to 5% of stearic acid, 0.6% to 2% of magnesium stearate, and 0.5% to 5% of silicon dioxide. As a result of experiments, preparations prepared with the medicine composition provided by the invention provide a better dissolution rate.