251 results about "Agomelatine" patented technology

The invention belongs to the technical field of medicines, and discloses a pharmaceutical composition for treating depression. The pharmaceutical composition is composed of a raw material agomelatine and auxiliary materials, wherein the raw material agomelatine is micronized agomelatine. Based on a deep research of the physical and chemical properties of agomelatine, the scientific researchers of the company accidentally find that agomelatine can be micronized for obtaining agomelatine with a certain particle size to produce a preparation, the invention has the advantages of uniform quality and good dissolution rate.

The invention discloses a crystalline Agomelatine ethylene glycol, acetic acid solvate and a preparation method thereof. The preparation method of the crystalline Agomelatine ethylene glycol solvate comprises the steps of: mixing Agomelatine with ethylene glycol according to the proportion of 1:2-5, heating the mixture to 100 to 130 DEG C, and melting and cooling the heated mixture to result in solids. The preparation method of the crystalline Agomelatine ethylene glycol solvate further comprises the steps of: dissolving Agomelatine in acetic acid to result in solution, and adding the solution into antisolvent, followed by standing still or constantly stirring or evaporating the solvent below 50 DEG C to result in crystal. The crystalline Agomelatine ethylene glycol, acetic acid solvate prepared according to the method has the advantages of: obviously reduced melting point of the solvate, high crystallization purity, good reproducibility, less amount of the solvent used, no need of protection from inert gas, low production cost, simple operation, mild reaction condition and easy control.

The invention provides a preparation method of agomelatine crystal form A which has a single endothermic peak at about 100 DEG C under the differential scanning calorimetry.

The invention provides a new preparation method of an important intermediate of the antidepressant agomelatine, i.e. 2-(7-methoxy-1-naphthyl) acetonitrile. In the method, a compound of formula III is subjected to a Wittig reaction so as to obtain a compound of formula XI, which then undergoes an aromatization reaction, so that 2-(7-methoxy-1-naphthyl) acetonitrile can be obtained. The preparation method of the invention has a short reaction route, the Wittig reaction and the aromatization reaction both have high yield. With mild reaction conditions and without anything to do with reagents and solvents etc. of high toxicity, the preparation method provided in the invention is suitable for industrial production.

The invention relates to new process for the synthesis of agomelatine. More particularly, the invention relates to a process for the industrial synthesis of the compound of formula (I).

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 relates to a coated solid orodispersible pharmaceutical composition for oral, oromucosal or sublingual administration of agomelatine.

The invention discloses a stable Agomelatine capsule medicine composition which is characterized in that 1000 capsules comprise the following components of 15-30g of Agomelatine, 70-140g of mannitol, 0.5-1g of superfine silica powder and a proper amount of 10 percent pre-gelatinized starch. The invention also relates to a preparation method of an Agomelatine capsule. The Agomelatine capsule prepared by adopting the formula and the preparation method provided in the invention has the advantages of good flowability, good dissolution rate, small content uniformity, high bioavailability and good treatment effect.

The present invention relates to a preparing method of agomelatine (N-[2-(7- anisyl-1- naphthyl) ethide] acetamide) of melatonin antidepressant drugs of commercial production. Firstly, 7- anisyl-1-tetralone is used as raw material, and is prepared into 2-(1,2,3,4- tetrahydrochysene-1- oxhydryl-7- methoxynaphthalene-1-base) acetonitrile in a cyanophoric way; then, 2-(1,2- dihydro-1-oxhydryl-7- methoxynaphthalene-1-base) acetonitrile is generated in an aromatization dehydrogenation way, and (7-- anisyl-1- naphthyl) acetonitrile is generated in a backflow reaction dehydrogenation way; finally, the agomelatine (N-[2-(7- anisyl-1- naphthyl) ethide] acetamide) is generated by reducing and acetylizing in a one-kettle way. The present invention has the advantages of high product purity, friendly environment, convenient operation and low cost, and is suitable for the commercial production.

The invention relates to a new crystal form of N-[2-(7-methoxyl-1-naphthyl)ethyl]acetamide (agomelatine), a preparation method of the new crystal form, a medicine including the new crystal form, and an application of the pharmaceutical composition in the medicine treating the depression.

The invention provides a preparation method of an agomelatine solid preparation. The preparation method comprises the steps of mixing agomelatine or pharmaceutically acceptable salts with polyvinylpolypyrrolidone; hot-melting the mixture to prepare particles; and mixing the particles with other pharmaceutically acceptable carriers to be tabletted or filled to form capsules. The agomelatine solid preparation prepared by the method is stable and controllable in quality and high in dissolution.