77 results about "Zopiclone" 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.

A pharmaceutical composition with improved safety includes a selected amount of a vomit-inducing agent, wherein the selected amount is less than an amount needed to induce vomit in a user; and a therapeutic agent. The therapeutic agent may be selected from a sleeping pill, an anxiolytic, a hypnotic, a contraceptive agent. The therapeutic agent may also be selected from diazepam, flunitrazepam, alprazolam, triazolam, fludiazepam, midazolam, estazolam, zopiclone, and a combination thereof. The vomit-inducing agent may be selected from emetine, cephaeline, and a combination thereof.

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 is directed to racemic and stereomerically pure compounds of Formula 3: and to pharmaceutical compositions comprising them, methods of their use, and methods of their preparation.

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 invention relates to a preparation method of zopiclone for improving sleeping, belonging to the field of medicines. In the preparation process of 6-(5-chlro-2-pyridyl)-5, 7-dioxo-5, 6-dihydropyrrolo[3, 4-b] pyrazine, namely a compound 3, by taking DMAP (dimethylaminopyridine) as a catalyst, in the presence of triethylamine, cyclization is directly carried out to synthesize an intermediate 3. The crude product yield is 85%, the yield is improved, the operation is simplified, and irritant reagents such as acetic anhydride, thionyl chloride, ethyl chloroformate and the like are not used, thereby facilitating production, facilitating recovery of xylene as a solvent and reducing emission of three wastes. Zopiclone is further synthesized by the compound 3. The method is concise in whole line, simple and convenient to operate and more suitable for industrialized production.

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.

A preparation method of zopiclone uses 6-(5-chlorin-2-pyridyl)-5-hydroxy-7-oxo-5, 6-dihydropyrrole [3, 4-b] pyrazine and 1-chlorocarbonyl-4-methylpiperazine hydrochloride as material, in anhydrous organic solvent and alkali condition, uses 4-substituent pyridine as catalyst to prepare the product zopiclone. The inventive method uses the organic solvent with a little toxin and unease burning explosion, via special catalyst to process reaction completely, while the product has high purity and yield.

The invention provides a zopiclone tablet rapid identification method based on a near infrared spectrum. The zopiclone tablet rapid identification method comprises the following steps: firstly, acquiring an original graph and pre-processing the original graph; modeling by adopting two instruments, and identifying by one instrument, thus realizing modeling and identifying a spectrum by using the instruments; and carrying out a qualification test on near infrared diffuse reflection spectrums of a plurality of batches of dynamic production samples by using a model so as to judge whether medicines are counterfeited or not. After the model is established, a negative sample and a positive sample are used for testing the stability of the model respectively; and when the result is that the passing rate of the positive sample is 100% and the negative sample does not pass, the false positive rate and the false negative rate of the model are relatively low, the method is suitable for market rapid checking and the result is reliable. A rapid quality identification and evaluation method for zopiclone tablets which are produced by Qilu Pharmaceutical Co.,Ltd. and are packaged by an aluminum-plastic plate is established, the detected sample does not need to be subjected to complicated pre-treatment, and the sample is not damaged and polluted; and a lot of analysis time and cost can be saved, and the method is a convenient, rapid and lossless green analysis technology.

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.