61 results about "Eszopiclone" patented technology

One aspect of the present invention relates to pharmaceutical compositions comprising a sedative agent; and melatonin or a melatonin analog, collectively referred to as “melatonin agents.” In a preferred embodiment, the sedative agent is eszopiclone. The pharmaceutical compositions of the invention are useful in the treatment of various sleep disorders. In addition, the present invention also relates to a method of treating a patient suffering from a sleep abnormality or insomnia comprising administering a therapeutically effective amount of a pharmaceutical composition of the invention.

One aspect of the present invention relates to pharmaceutical compositions containing two or more active agents that when taken together can be used to treat, e.g., menopause, mood disorders, anxiety disorders, or cognitive disorders. The first component of the pharmaceutical composition is a sedative eszopiclone. The second component of the pharmaceutical composition is trans 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-N-methyl-1-napthalenamine or trans 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-napthalenamine. The present invention also relates to a method of treating menopause, perimenopause, mood disorders, anxiety disorders, and cognitive disorders.

One aspect of the present invention relates to pharmaceutical compositions containing two or more active agents that when taken together can be used to treat, e.g., menopause, mood disorders, anxiety disorders, or cognitive disorders. The first component of the pharmaceutical composition is a sedative eszopiclone. The second component of the pharmaceutical composition is an antidepressant. The present invention also relates to a method of treating menopause, perimenopause, mood disorders, anxiety disorders, and cognitive disorders.

The present disclosure provides a unit dosage form with an anxiolytic dosage of zopiclone particularly eszopiclone. Also provided is a method for treatment or prophylaxis of anxiety using a subsedative dosage of zopiclone particularly eszopiclone.

One aspect of the present invention relates to pharmaceutical compositions containing two or more active agents that when taken together can be used to treat, e.g., menopause, mood disorders, anxiety disorders, or cognitive disorders. The first component of the pharmaceutical composition is a sedative eszopiclone. The second component of the pharmaceutical composition is O-desmethylvenlafaxine. The present invention also relates to a method of treating menopause, perimenopause, mood disorders, anxiety disorders, and cognitive disorders.

The invention relates to an eszopiclone preparation method comprising main steps that: zopiclone is subjected to a reaction with D-dibenzoyltartaric acid or a hydrate thereof, such that dextral zopiclone-D-dibenzoyltartrate is produced; and the salt is dissociated, such that eszopiclone is obtained. According to the method, D-dibenzoyltartaric acid with a substance amount of a quarter to a half of that of zopiclone is adopted. The reaction conditions are mild, operation is convenient, product yield is high, and product purity is high. The method is suitable for large-scale industrialized productions.

The present invention provides methods for preparing eszopiclone Form A, substantially chemically pure eszopiclone, or eszopiclone with low level(s) of residual solvent(s). The present invention also provides eszopiclone with low level(s) of residual solvent(s). The present invention also provides a process for optical enrichment of eszopiclone free base. For instance, one of the embodiments of the invention is directed to a method of preparing eszopiclone Form A, wherein the method comprises crystallizing eszopiclone free base from a solvent selected from the group consisting of isopropanol (IPA), methyl isobutyl ketone (MIBK), acetone, n-butanol, i-butanolisobutanol, 2-butanol, tetrahydrofuran (THF), dimethyl carbonate, methanol, ethanol, ethyl lactate, dimethylformamide (DMF), carbon tetrachloride, toluene, iso-butyl acetate and mixtures thereof.

The invention relates to an eszopiclone-containing particle and its preparation method. The particle can cover the bitter taste of eszopiclone, has no obvious sandy feeling, has uniform contents and high dissolution rate, and can be used for preparing solid dosage forms such as orally disintegrating tablets, dispersing tablets, suspension granules and the like.

The invention discloses a medicinal composition containing Esopiclone and a preparation method thereof. The Esopiclone-containing medicinal composition consists of a main medicine and auxiliary materials. In the invention, by controlling the particle size of the main medicine, a pre-mixing method and the auxiliary materials, the medicinal composition which has high dissolution rate and high content uniformity can be obtained. The preparation method adopts a modern preparation technique, the quality of the product is stable, and an Esopiclone-containing solid oral preparation which is safe, effective, quick in absorption, high in bioavailability and accurate in dosage is provided for patients.

The invention discloses a making method of 6-(5-chlorine-2-pyridine)-5,7-dioxy-6,7-dihydrogen-5H-pyrrole [3,4-b] pyrazine (I) as intermediate of right-adjuvant clone, which comprises the following steps: dissolving 3-(5-chloropyridine-2-amino)formyl morpholine pyrazine-2-carboxyl acid (II) into the composite liquid of organic solvent/amine; adding chloroformate in the reacting liquid; obtaining the product I.

The present invention relates to a process for optically resolving eszopiclone, comprising chiral chromatography. Preferably the process comprises a multi-column continuous process or a simulated moving bed process. Preferably the stationary phase used in the chiral chromatography process comprises an amylose or cellulose derivative of tris(3,5-dimethylphenyl carbamate), or an amylose derivative of tris-α-methylbenzylcarbamate. The process of the present invention has the advantage that it is high yielding and can be carried out on an industrial scale.

The present invention also provides eszopiclone, or a pharmaceutically acceptable salt thereof, obtained by the chiral chromatography process. The eszopiclone or salt thereof is suitable for use as a medicament, for example, for the treatment of anxiety or insomnia.

The invention relates to a chiral synthesis method for Eszopiclone and belongs to the technical field of medicine. The chiral synthesis method for Eszopiclone comprises the following two steps of reaction: (1), reducing under the action of a 6-(5-chlorine-2-pyridyl)-5,6-dioxo-6,7-dihydro-5H-pyrrol(3,4-b)pyrazine chiral reagent to obtain 6-(5-chlorine-2-pyridyl)-5(S)-hydroxyl-7-oxo-6,7-dihydro-5H-pyrrol(3,4-b)pyrazine; and (2), reacting the 6-(5-chlorine-2-pyridyl)-5(S)-hydroxyl-7-oxo-6,7- dihydro-5H-pyrrol(3,4-b)pyrazine with 1-chloroformyl-4-methylpiperazine hydrochloride under the action of organic base to obtain the Eszopiclone. The chiral synthesis method for the Eszopiclone has the advantages of high atom utilization ratio, short steps and advanced technology.

The invention relates to a racemization method of eszopiclone. According to the invention, tetramethylguanidine which is cheap and easily available is used as a racemization agent. The method provided by the invention is simple to operate, is safe and stable, has advantages of high yield and good product quality, and is suitable for industrial production.

Disclosed herein is the process for preparation of 6-(5-chloro-pyrid-2-yl)-5-[(4-methyl-1-piperazinyl)carbonyloxy]-7-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyrazine (Zopiclone), its resolution to get the dextrorotatory isomer of formula (I) substantially free of R(−) enantiomer and recovery of key raw material i.e. 6-(5-chloro pyrid-2-yl)-5-hydroxy-7-oxo-5,6-dihydropyrrolo[3,4-b]pyrazine from the R-isomer of Zopiclone followed by conversion of the recovered compound to get pure Eszopiclone (I) in high yield and high purity.

The invention relates to a pharmaceutical composition containing a dexzopiclone tablet, belonging to the technical field of medicine. Commercially available dexzopiclone tablets are of three specifications, i.e., 1 mg, 2 mg and 3 mg. Due to small specifications of the dexzopiclone tablets, content uniformity of prepared tablets can hardly achieve standards; and since the dexzopiclone is hardly soluble in water, reproducibility of the dissolution data of tablets of different batches is poor. The technical scheme of the invention is as follows: the dexzopiclone tablet is characterized by containing, by mass, 1% of dexzopiclone with D90 of below 30 mu m, 0 to 77.5% of dicalcium phosphate dihydrate, 20 to 97.5% of microcrystalline cellulose, 1% of croscarmellose sodium and 0.5% of magnesium stearate. The technical scheme of the invention overcomes the above-mentioned problems in the prior art.

The invention relates to an eszopiclone composition and a preparation method thereof and belongs to the technical field of pharmaceutical preparations. According to the eszopiclone composition provided by the invention, the unit dose of the composition is prepared from 1 to 3mg of eszopiclone, 40 to 87mg of microcrystalline cellulose, 8 to 12mg of dicalcium phosphate, 3 to 5mg of croscarmellose sodium, 10 to 30mg of colloidal silicon dioxide, 10 to 20mg of oily auxiliary material and 1.4 to 2mg of magnesium stearate. According to the technical scheme provided by the invention, the stable and safe eszopiclone tablet composition is obtained.

The invention relates to the technical filed of a medicine, and discloses an eszopiclone oral disintegrating tablet and a preparation method thereof. The eszopiclone oral disintegrating tablet is prepared by a bulk drug and excipients, wherein the weight percentage of the bulk drug to the excipients is 1-5%:95-99%, the eszopiclone oral disintegrating tablet comprises the following components by weight percentage: 1-5% of eszopiclone, 5-20% of a disintegrating agent, 70-90% of a filler, 1-5% of a flavouring, and 0.5-2.5% of a lubricant; wherein the sum of the weight percentage of the raw materials is 100%. By aiming at the disadvantages of difficult dissolution of eszopiclone in water, slow dissolution speed, and poor mouthfeel of eszopiclone, various excipients capable of promoting disintegration of the bulk drug eszopiclone and effectively covering the adverse smell of eszopiclone can be selected from many drugs, the obtained eszopiclone oral disintegrating tablet has the advantages of fast disintegration speed, short disintegration time, good palatability, smooth and clean surface, and no spot and the like. The oral disintegrating tablet is prepared by a direct tabletting method,the process is simple, and the economic benefit is good.