Nintedanib diethanesulfonate salt crystal and preparation method and use thereof

The present invention relates to a nintedanib diethanesulfonate salt A-type crystal represented by formula (II), and also relates to a crystalline composition and pharmaceutical composition comprising the crystal, and preparation method and use thereof. An X-ray powder diffraction spectrum of the nintedanib diethanesulfonate salt A-type crystal of the present invention has a diffraction peak at about 14.64, 18.79, 19.31, 20.11, 21.20, 22.45 and 26.71° when represented via a 2θ value. The nintedanib diethanesulfonate salt A-type crystal of the present invention has a stable property, is non-hygroscopic and difficult to degrade, and is particularly suitable for medicine production.

MIXED CRYSTAL AGOMELATINE (FORM VIII), PREPARATION METHOD AND USE THEREOF AND PHARMACEUTICAL COMPOSITION CONTAINING SAME

The present invention provides a mixed crystalline form VIII of agomelatine, its method of preparation, application and pharmaceutical composition. The said mixed crystal consists mainly of crystalline form VI of agomelatine. The said mixed crystalline form is stable and has good reproducibility. Through stability tests, it has been found to be superior to the crystalline form VI in terms of stability. As a result, the crystalline form VIII of the present invention possesses advantages in pharmaceutical preparation. 114-. (canceled)17. The mixed crystalline form according to claim 15 , having the following DSC change-in-absorption diagram claim 15 , the onset value range being 97-98° C. claim 15 , the endothermic peak area being no lower than 90% claim 15 , with the preferable ratio being 95-99%.19. The preparation method according to claim 18 , wherein the molar ratio of agomelatine compounds of formula (II) and sodium acetate is from 1:1-1.5 claim 18 ,20. The preparation method according to claim 19 , wherein the molar ratio of agomelatine compounds of formula (II) and sodium acetate is from 1:1-1.1.21. The preparation method according to claim 18 , wherein the ratio of volume of acetic acid to water is 1:15-30.22. The preparation method according to claim 18 , wherein when the temperature of the resulting reaction mixture reaches 12-18° C. claim 18 , water is added dropwise in order to bring about crystallization.23. The preparation method according to claim 22 , wherein when the temperature of the resulting reaction mixture reaches 15° C. claim 22 , water is added dropwise in order to bring about crystallization.24. The preparation method according to claim 18 , wherein water is added dropwise to the resulting reaction mixture which is then agitated at a temperature of 10° C. in order to bring about crystallization.25. The preparation method according to claim 18 , wherein following the addition of the sodium acetate claim 18 , the reaction mixture is heated to ...

Display screen or portion thereof with a graphical user interface

METHOD AND APPARATUS FOR CONFIGURING DEVICES TO ENABLE DETERMINATION OF LOCATION INFORMATION

Aspects of the subject disclosure may include, for example, determining, according to a location of each of a plurality of devices, an arrangement of coverage areas of devices pairs of the plurality of devices to enable a determination of a mobile device location relative to one or more of the devices pairs within a demarcated area, and identifying a transmission schedule for each of the devices pairs to transmit a wireless signal that initiates a process to determine the mobile device location. Other embodiments are disclosed.

CRYSTAL FORM VII OF AGOMELATINE, PREPARATION METHOD AND USE THEREOF AND PHARMACEUTICAL COMPOSITION CONTAINING SAME

The present invention provides a new crystalline form VII of agomelatine, its method of preparation, application and pharmaceutical composition. This new crystalline form offers high purity, a stable crystalline structure and good reproducibility, while its method of production lends itself well to large scale production. In terms of stability and purity, it is superior to the numerous crystalline forms which have hitherto been reported. As a result, the crystalline form VII of the present invention possesses advantages in pharmaceutical preparation. 114-. (canceled)18. The preparation method according to claim 17 , wherein the molar ratio of the agomelatine compound of formula (II) or (III) and acetate is from 1:1-1.5.19. The preparation method according to claim 18 , wherein the molar ratio of the agomelatine compound of formula (II) or (III) and acetate is from 1:1-1.1.20. The preparation method according to claim 17 , wherein the ratio of volume of acetic acid to water is 1:10-30.21. The preparation method according to claim 17 , wherein the acetate is potassium acetate or ammonium acetate.22. The preparation method according to claim 17 , wherein when the temperature of the resulting reaction mixture reaches 19-25° C. claim 17 , water is added dropwise in order to bring about crystallization.23. The preparation method according to claim 22 , wherein when the temperature of the resulting reaction mixture reaches 22° C. or 23° C. claim 22 , water is added dropwise in order to bring about crystallization.24. The preparation method according to claim 17 , wherein water is added dropwise to the resulting reaction mixture which is then agitated at a temperature of 20° C. in order to bring about crystallization.25. The preparation method according to claim 17 , wherein following the addition of the acetate claim 17 , the reaction mixture is heated to 30-50° C. claim 17 , resulting in a clear solution; the solution is then left to cool on its own claim 17 , and water ...

DIHYDROINDOLINONE DERIVATIVES

Disclosed are dihydroindolone compounds which can modulate the activity of protein tyrosine kinases, a method for preparing the same, and pharmaceutical compositions comprising the same. Also disclosed are use of such compounds and pharmaceutical compositions thereof in the treatment and/or prophylaxis of protein tyrosine kinase associated diseases in an organism, particularly in the treatment and/or prophylaxis of tumors and fibroblast proliferation associated diseases.

Method and apparatus for configuring devices to enable determination of location information

Aspects of the subject disclosure may include, for example, determining, according to a location of each of a plurality of devices, an arrangement of coverage areas of devices pairs of the plurality of devices to enable a determination of a mobile device location relative to one or more of the devices pairs within a demarcated area, and identifying a transmission schedule for each of the devices pairs to transmit a wireless signal that initiates a process to determine the mobile device location. Other embodiments are disclosed.

AGOMELATINE HYDROCHLORIDE HYDRATE AND PREPARATION THEREOF

The present invention relates to an agomelatine hydrochloride hydrate of formula I, preparation and use thereof, and to pharmaceutical composition containing it. The agomelatine hydrohalide hydrate obtained through the present method has significant increased solubility than agomelatine, and therefore is more suitable for manufacturing pharmaceutical formulations. In addition, the product enjoys higher stability and purity. Using the present method, product of high purity can be obtained through a simple process, free of any complicated steps. wherein X is Cl.

Agomelatine hydrobromide hydrate and preparation thereof

The present invention relates to an agomelatine hydrobromide hydrate of formula I wherein X is Br, preparation and use thereof, and to pharmaceutical compositions containing it. The agomelatine hydrobromide hydrate obtained through the present method has significant increased solubility than agomelatine, and therefore is more suitable for manufacturing pharmaceutical formulations. In addition, the product enjoys higher stability and purity. Using the present method, product of high purity can be obtained through a simple process, free of any complicated steps.

SYNTHESIS PROCESS OF RUXOLITINIB

The present application falls within the field of drug synthesis, and in particular, the present application relates to a method for preparing ruxolitinib, and a method for preparing the intermediate and relevant intermediates used. The method comprises reacting a compound of formula II with a compound of formula IV or a salt thereof to obtain a compound of formula III, and then subjecting the compound of formula III to an acyl halogenation reaction, an amidation reaction, and a reaction dehydrating an amide to form a cyano group or removing the protecting group to prepare ruxolitinib. The method has the characteristics of brief steps, a high stereoselectivity, a high utilization ratio of atoms, mild reaction conditions and convenient post treatment. The method avoids using expensive asymmetric reaction catalysts, and is suitable for industrial production. 4. (canceled)78.-. (canceled)1014.-. (canceled)16. The process for preparing the compound of Formula III according to claim 15 , wherein the amino-protecting group is selected from benzyloxycarbonyl claim 15 , 2 claim 15 ,2 claim 15 ,2-trichloroethoxycarbonyl claim 15 , 2-(trimethylsilyl)ethoxycarbonyl claim 15 , 2-(4-trifluoromethylphenylsulfonyl)ethoxycarbonyl claim 15 , tert-butoxycarbonyl claim 15 , 1-adamantyloxycarbonyl claim 15 , 2-adamantylcarbonyl claim 15 , 2 claim 15 ,4-dimethylpent-3-yloxycarbonyl claim 15 , cyclohexyloxycarbonyl claim 15 , 1 claim 15 ,1-dimethyl-2 claim 15 ,2 claim 15 ,2-trichloroethoxycarbonyl claim 15 , vinyl claim 15 , 2-chloroethyl claim 15 , 2-phenylsulfonylethyl claim 15 , p-nitrophenylsulfonyl claim 15 , p-toluenesulfonyl claim 15 , phenylsulfonyl claim 15 , methanesulfonyl claim 15 , allyl claim 15 , benzyl claim 15 , 2-nitrobenzyl claim 15 , 4-nitrobenzyl claim 15 , diphenyl-4-pyridylmethyl claim 15 , N′ claim 15 ,N′-dimethylhydrazino claim 15 , methoxymethyl claim 15 , tert-butoxymethyl claim 15 , benzyloxymethyl claim 15 , 2-tetrahydropyranyl claim 15 , tri(Calkyl)silyl ...

Agomelatine hydrochloride hydrate and preparation thereof

The present invention relates to an agomelatine hydrochloride hydrate of formula I, preparation and use thereof, and to pharmaceutical composition containing it. The agomelatine hydrohalide hydrate obtained through the present method has significant increased solubility than agomelatine, and therefore is more suitable for manufacturing pharmaceutical formulations. In addition, the product enjoys higher stability and purity. Using the present method, product of high purity can be obtained through a simple process, free of any complicated steps. wherein X is Cl.

Method for preparing dabigatran etexilate intermediate, and intermediate compound

Disclosed are a method for preparing a dabigatran etexilate intermediate, and an intermediate compound. The method for preparing a dabigatran etexilate intermediate 4 comprises: reacting a compound 3 with a C1-C3alkyl alcohol solution of methylamine in an organic solvent, wherein, X=chlorine, bromine, or iodine. Also disclosed are an intermediate compound 3 and a preparation method thereof. The method for preparing a dabigatran etexilate intermediate of the present invention has the advantages of simple process, easy operation, high yield, and easy purification, thus being suitable for industrial production.

METHOD AND APPARATUS FOR CONFIGURING DEVICES TO ENABLE DETERMINATION OF LOCATION INFORMATION

Aspects of the subject disclosure may include, for example, determining, according to a location of each of a plurality of devices, an arrangement of coverage areas of devices pairs of the plurality of devices to enable a determination of a mobile device location relative to one or more of the devices pairs within a demarcated area, and identifying a transmission schedule for each of the devices pairs to transmit a wireless signal that initiates a process to determine the mobile device location. Other embodiments are disclosed.

AGOMELATINE HYDROBROMIDE HYDRATE AND PREPARATION THEREOF

The present invention relates to an agomelatine hydrobromide hydrate of formula I 113-. (canceled)15. The agomelatine hydrobromide hydrate according to claim 14 , wherein the agomelatine hydrobromide hydrate is in a crystalline form exhibiting the following crystal parameters: space group P2/c claim 14 , lattice parameters a=7.5943 (7) claim 14 , b=23.4046 (19) claim 14 , c=9.6438 (8) Å claim 14 , β=1613.9 (2)°.16. A method for the preparation of the agomelatine hydrobromide hydrate according to claim 14 , wherein agomelatine is reacted with HBr to produce the agomelatine hydrobromide hydrate.17. The method according to claim 16 , wherein agomelatine is reacted with HBr in an aqueous organic solvent to produce the agomelatine hydrobromide hydrate.18. The method according to claim 17 , wherein agomelatine is dissolved in an organic solvent before an aqueous HBr solution is added to precipitate a crystal of the product.19. The method according to claim 18 , wherein the aqueous HBr solution is added dropwise.20. The method according to claim 17 , wherein agomelatine is added to an aqueous organic solvent containing HBr to precipitate a crystal of the product.21. The method according to claim 18 , further comprising rinsing and drying the solid after crystallisation.22. The method according to claim 18 , wherein the reaction temperature is 0-20° C.23. The method according to claim 18 , wherein the organic solvent is ethyl acetate claim 18 , methyl acetate claim 18 , n-butyl acetate claim 18 , acetone or acetonitrile.24. The method according to claim 23 , wherein the organic solvent is ethyl acetate.25. The method according to claim 20 , further comprising rinsing and drying the solid after crystallisation.26. The method according to claim 20 , wherein the reaction temperature is 0-20° C.27. The method according to claim 20 , wherein the organic solvent is ethyl acetate claim 20 , methyl acetate claim 20 , n-butyl acetate claim 20 , acetone or acetonitrile.28. The method ...

NINTEDANIB DIETHANESULFONATE SALT CRYSTAL AND PREPARATION METHOD AND USE THEREOF

The present invention relates to a nintedanib diethanesulfonate salt A-type crystal represented by formula (II), and also relates to a crystalline composition and pharmaceutical composition comprising the crystal, and preparation method and use thereof. An X-ray powder diffraction spectrum of the nintedanib diethanesulfonate salt A-type crystal of the present invention has a diffraction peak at about 14.64, 18.79, 19.31, 20.11, 21.20, 22.45 and 26.71° when represented via a 2θ value. The nintedanib diethanesulfonate salt A-type crystal of the present invention has a stable property, is non-hygroscopic and difficult to degrade, and is particularly suitable for medicine production.

Method and apparatus for configuring devices to enable determination of location information

Aspects of the subject disclosure may include, for example, determining, according to a location of each of a plurality of devices, an arrangement of coverage areas of devices pairs of the plurality of devices to enable a determination of a mobile device location relative to one or more of the devices pairs within a demarcated area, and identifying a transmission schedule for each of the devices pairs to transmit a wireless signal that initiates a process to determine the mobile device location. Other embodiments are disclosed.

Dihydroindolinone derivatives

Disclosed are dihydroindolone compounds which can modulate the activity of protein tyrosine kinases, a method for preparing the same, and pharmaceutical compositions comprising the same. Also disclosed are use of such compounds and pharmaceutical compositions thereof in the treatment and/or prophylaxis of protein tyrosine kinase associated diseases in an organism, particularly in the treatment and/or prophylaxis of tumors and fibroblast proliferation associated diseases.

Synthesis process of ruxolitinib

The present application falls within the field of drug synthesis, and in particular, the present application relates to a method for preparing ruxolitinib, and a method for preparing the intermediate and relevant intermediates used. The method comprises reacting a compound of formula II with a compound of formula IV or a salt thereof to obtain a compound of formula III, and then subjecting the compound of formula III to an acyl halogenation reaction, an amidation reaction, and a reaction dehydrating an amide to form a cyano group or removing the protecting group to prepare ruxolitinib. The method has the characteristics of brief steps, a high stereoselectivity, a high utilization ratio of atoms, mild reaction conditions and convenient post treatment. The method avoids using expensive asymmetric reaction catalysts, and is suitable for industrial production.

METHOD FOR PREPARING DABIGATRAN ETEXILATE INTERMEDIATE, AND INTERMEDIATE COMPOUND

Disclosed are a method for preparing a dabigatran etexilate intermediate, and an intermediate compound. The method for preparing a dabigatran etexilate intermediate 4 comprises; reacting a compound 3 with a C-Calkyl alcohol solution of methylamine in an organic solvent, wherein, X=chlorine, bromine, or iodine. Also disclosed are an intermediate compound 3 and a preparation method thereof. The method for preparing a dabigatran etexilate intermediate of the present invention has the advantages of simple process, easy operation, high yield, and easy purification, thus being suitable for industrial production. 1. (canceled)2. (canceled)3. (canceled)4. (canceled)5. (canceled)6. (canceled)7. (canceled)8. (canceled)9. (canceled)10. (canceled)11. (canceled)12. (canceled)13. (canceled)14. (canceled)15. (canceled)17. The preparation method according to claim 16 , wherein the protic organic solvent is methanol and/or ethanol claim 16 , and the aprotic organic solvent is an aprotic polar organic solvent.18. The preparation method according to claim 17 , wherein the aprotic organic solvent is one or more of dimethyl sulfoxide claim 17 , N claim 17 ,N-dimethyl formamide claim 17 , N claim 17 ,N-dimethyl acetamide claim 17 , and N-methyl pyrrolidone.19. The preparation method according to claim 16 , wherein the C-Calkyl alcohol solution of methylamine is one or more of a methanol solution of methylamine claim 16 , an ethanol solution of methylamine claim 16 , and a propanol solution of methylamine; and the concentration claim 16 , of the C-Calkyl alcohol solution of methylamine is 27-32% by weight.20. The preparation method according to claim 16 , wherein the molar ratio of the compound 3 to methylamine is 1:1.98-1:2.35.21. The preparation method according to claim 16 , wherein the C-Calkyl alcohol solution of methylamine is added by dripping the C-alkyl alcohol solution of methylamine into a mixture of the compound 3 and the organic solvent.22. The preparation method according to ...

SORAFENIB HEMI-P-TOSYLATE MONOHYDRATE CRYSTAL AND PREPARATION PROCESS THEREOF

The present invention relates to the field of medicinal technology, and in particular, to sorafenib hemi-p-tosylate monohydrate crystal and preparation process thereof. The crystal has diffraction peaks occurring at 2θ angle of about 5.62, 6.67, 8.05, 9.06, 9.63, 9.91, 10.95, 11.25, 13.48, 14.00, 14.60, 15.08, 15.75, 16.20, 16.62, 16.80, 17.23, 18.40, 18.97, 19.32, 19.82, 20.49, 20.74, 21.51, 22.56, 22.86, 23.37, 23.71, 24.20, 24.71, 24.97, 25.54, 25.80, 26.18, 27.14, 27.48, and 28.29 degree in a X-ray powder diffraction pattern, and some advantages, such as a high stability, a low hygroscopicity and the like. 1. A sorafenib hemi-p-tosylate monohydrate crystal , characterized in that , in a X-ray powder diffraction pattern using Cu Kα irradiation , diffraction peaks occur at 2θ angle of 5.62 , 6.67 , 8.05 , 9.06 , 9.63 , 9.91 , 10.95 , 11.25 , 13.48 , 14.00 , 14.60 , 15.08 , 15.75 , 16.20 , 16.62 , 16.80 , 17.23 , 18.40 , 18.97 , 19.32 , 19.82 , 20.49 , 20.74 , 21.51 , 22.56 , 22.86 , 23.37 , 23.71 , 24.20 , 24.71 , 24.97 , 25.54 , 25.80 , 26.18 , 27.14 , 27.48 and 28.29 degree.2. The crystal of claim 1 , characterized in that claim 1 , in the X-ray powder diffraction pattern using Cu Kα irradiation claim 1 , the diffraction peaks occur at 2θ angle of 5.62 claim 1 , 6.67 claim 1 , 8.05 claim 1 , 9.06 claim 1 , 9.63 claim 1 , 9.91 claim 1 , 10.95 claim 1 , 11.25 claim 1 , 12.79 claim 1 , 13.48 claim 1 , 14.00 claim 1 , 14.60 claim 1 , 15.08 claim 1 , 15.75 claim 1 , 16.20 claim 1 , 16.62 claim 1 , 16.80 claim 1 , 17.23 claim 1 , 18.40 claim 1 , 18.97 claim 1 , 19.32 claim 1 , 19.82 claim 1 , 20.49 claim 1 , 20.74 claim 1 , 21.51 claim 1 , 22.06 claim 1 , 22.56 claim 1 , 22.86 claim 1 , 23.37 claim 1 , 23.71 claim 1 , 24.20 claim 1 , 24.71 claim 1 , 24.97 claim 1 , 25.54 claim 1 , 25.80 claim 1 , 26.18 claim 1 , 26.41 claim 1 , 27.14 claim 1 , 27.48 claim 1 , 28.29 claim 1 , 28.58 claim 1 , 29.15 and 29.88 degree.3. The crystal of claim 2 , characterized in that claim ...

Agomelatine hydrobromide hydrate and preparation thereof

An agomelatine hydrobromide hydrate of formula (I), in which X is Br, preparation method and use thereof as well as pharmaceutical composition containing it are provided. The solubility of the agomelatine hydrobromide hydrate obtained by the present method is significantly higher than that of agomelatine. Therefore, it is more suitable for manufacturing pharmaceutical formulations. In addition, the product has higher stability and purity. The present product of high purity can be obtained through a simple process, rather than process with complicated steps.

Agomelatine hydrochloride hydrate and preparation thereof

An agomelatine hydrochloride hydrate of formula (I), preparation, use, and pharmaceutical composition thereof are provided. Said hydrate obtained through the present method has significant increased solubi1ity than agomelatine, and therefore is more suitable for manufacturing pharmaceutical formulations. Using the present method, high purity can be obtained through a simple process, free of any complicated steps. Wherein X is Cl.

Agomelatine hydrobromide hydrate and preparation thereof

An agomelatine hydrobromide hydrate of formula (I), in which X is Br, preparation method and use thereof as well as pharmaceutical composition containing it are provided. The solubility of the agomelatine hydrobromide hydrate obtained by the present method is significantly higher than that of agomelatine. Therefore, it is more suitable for manufacturing pharmaceutical formulations. In addition, the product has higher stability and purity. The present product of high purity can be obtained through a simple process, rather than process with complicated steps.

AGOMELATIN HYDRATE BROMHYDRATE AND PREPARATION THEREOF

L'invention porte sur un bromhydrate d'agomélatine hydraté de formule (i), dans laquelle x représente br, sur son procédé de préparation et son utilisation ainsi que sur une composition pharmaceutique le contenant. La solubilité du bromhydrate d'agomélatine hydraté obtenu par le présent procédé est considérablement supérieure à celle de l'agomélatine. Par conséquent, il est plus approprié pour la fabrication de formulations pharmaceutiques. En outre, le produit a une stabilité et une pureté supérieures. Le présent produit de haute pureté peut être obtenu par un procédé simple, plutôt qu'un procédé comprenant des étapes compliquées.

Mixed crystal agomelatine (form-viii), preparation method and use thereof and pharmaceutical composition containing same.

La presente invención proporciona un cristal mixto de agomelatina (forma VIII), sus métodos de preparación, su aplicación y sus composiciones farmacéuticas en las que el cristal mixto es principalmente agomelatina de forma VI. La estabilidad del tipo mixto y la buena reproducibilidad y su método de preparación son mejores que en la mayoría de los informes existentes respecto de estabilidad y solubilidad del polimorfo VI. Por lo tanto, la presente invención proporciona una forma VIII que resulta ventajosa en la preparación.

Agomelatine hydrochloride hydrate and preparation thereof

New crystal form vii of agomelatine, preparation method and use thereof and pharmaceutical composition containing same

Dihydroindolone derivatives

Disclosed are dihydroindolone compounds of formula I, or pharmaceutically acceptable salts thereof, which can modulate the activity of protein tyrosine kinases. A method for preparing the same, and pharmaceutical compositions comprising the same are also disclosed. Also disclosed are use of such compounds and pharmaceutical compositions thereof in the treatment and/or prophylaxis of protein tyrosine kinase associated diseases in an organism, particularly in the treatment and/or prophylaxis of tumors and fibroblast proliferation associated diseases. (see formula I)

NEW CRYSTAL FORM VII OF AGOMELATIN, METHOD OF PREPARING AND USING THEREOF AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME

HYDROBROMIDE HYDROBROMIDE HYDROBROMIDE AND

Se proporciona un hidrato del hidrobromuro de agomelatina de fórmula (I), en la que X es Br, preparación, uso y composición farmacéutica del mismo. Dicho hidrato obtenido mediante el presente método tiene una solubilidad significativamente aumentada que la agomelatina, y por ello es más adecuada para fabricar formulaciones farmacéuticas. Usando el presente método, se puede obtener una pureza elevada mediante de un proceso simple, sin ninguna etapa complicada.

New crystalline form vii of agomelatine, preparation method and use thereof and pharmaceutical composition containing same

Disclosed herein is a new crystal form VII of agomelatine, the preparation method and use thereof and a pharmaceutical composition containing the same. Also disclosed is the method for the preparation of crystal form VII of agomelatine, which comprises dissolving form II or III agomelatine compounds in acetic acid, to which potassium acetate or ammonium acetate is then added, followed by the addition of water dropwise to this reaction mixture, which is then agitated at a temperature of 17-23°C in order to bring about crystallization, and the crystals are then separated from the solution. The new crystal form has a good purity, a stable crystal form and good reproducibility; the preparation method thereof is easy to amplify; and it is superior to most previously reported crystal forms in terms of stability and solubility. in acetic acid, to which potassium acetate or ammonium acetate is then added, followed by the addition of water dropwise to this reaction mixture, which is then agitated at a temperature of 17-23°C in order to bring about crystallization, and the crystals are then separated from the solution. The new crystal form has a good purity, a stable crystal form and good reproducibility; the preparation method thereof is easy to amplify; and it is superior to most previously reported crystal forms in terms of stability and solubility.

New crystal form vii of agomelatine, preparation method and use thereof and pharmaceutical composition containing same

New crystal form vii of agomelatine, preparation method and use thereof and pharmaceutical composition containing same

Mixed crystal agomelatine (form-viii), preparation method and use thereof and pharmaceutical composition containing same

mixed crystalline agomelatine (forma-viii), method of preparation and use thereof and pharmaceutical composition containing same

resumo patente de invenção: "agomelatina cristalina misturada (forma-viii), método de preparação e uso da mesma e composição farmacêutica contendo a mesma". a presente invenção refere-se a uma forma viii cristalina misturada da agomelatina, o seu método de preparação, aplicação e composição farmacêutica. o cristal misturado citado acima consiste principalmente na forma cristalina vi da agomelatina. a forma cristalina misturada citada acima é estável e tem a boa reprodutibilidade. através de testes de estabilidade, foi encontrado para ser superior à forma cristalina vi quanto a estabilidade. por conseguinte, a forma cristalina viii da presente invenção possui vantagens na preparação farmacêutica. 1/1 Patent Summary: "Mixed crystalline agomelatine (forma-viii), method of preparation and use thereof and pharmaceutical composition containing same". The present invention relates to a mixed crystalline form of agomelatine, its method of preparation, application and pharmaceutical composition. The above mixed crystal consists mainly of the crystalline form vi of agomelatine. The above mixed crystalline form is stable and has good reproducibility. through stability testing, was found to be superior to the crystalline form vi for stability. therefore, the crystalline form viii of the present invention has advantages in the pharmaceutical preparation. 1/1

Dihydroindolone derivatives

Disclosed are dihydroindolone compounds which can modulate the activity of protein tyrosine kinases, a method for preparing the same, and pharmaceutical compositions comprising the same. Also disclosed are use of such compounds and pharmaceutical compositions thereof in the treatment and/or prophylaxis of protein tyrosine kinase associated diseases in an organism, particularly in the treatment and/or prophylaxis of tumors and fibroblast proliferation associated diseases.

agomelatine hydrochloride hydrate and its preparation

HIDRATO DE CLORIDRATO DE AGOMELATINA E SUA PREPARAÇÃO. A presente invenção refere-se a um hidrato de cloridrato de agomelatina de fórmula (I), a preparação, o uso, e a composição farmacêutico do mesmo. O dito hidrato obtido através do presente método tem solubilidade aumentanda significativa do que a agomelatina, e, portanto, é mais adequado para a fabricação de formulações farmacêuticas. Usando o presente método, uma alta pureza pode ser obtida através de um processo simples, livre de quaisquer etapas complicadas. Onde X é CI. AGOMELATIN HYDRATE HYDRATE AND ITS PREPARATION. The present invention relates to an agomelatine hydrochloride hydrate of formula (I), the preparation, use, and pharmaceutical composition thereof. Said hydrate obtained by the present method has significantly increased solubility than agomelatine, and therefore is more suitable for the manufacture of pharmaceutical formulations. Using the present method, a high purity can be obtained through a simple process, free from any complicated steps. Where X is CI.

Agomelatine hydrobromide hydrate and preparation thereof

Agomelatine Hydrochloride Hydrate and its Preparation

AGOMELATINE HYDROCHLORIDE HYDROCHLORIDE AND PREPARATION OF THIS

Se proporciona un hidrato del hidrocloruro de agomelatina de fórmula (I), en la que X es CI, preparación, uso y composición farmacéutica del mismo. Dicho hidrato obtenido mediante el presente método tiene una solubilidad significativamente aumentada que la agomelatina, y por ello es más adecuada para fabricar formulaciones farmacéuticas. Usando el presente método, se puede obtener una pureza elevada mediante de un proceso simple, sin ninguna etapa complicada. An agomelatine hydrochloride hydrate of formula (I) is provided, wherein X is CI, preparation, use and pharmaceutical composition thereof. Said hydrate obtained by the present method has a significantly increased solubility than agomelatine, and is therefore more suitable for manufacturing pharmaceutical formulations. Using the present method, high purity can be obtained by a simple process, without any complicated stage.

New crystalline form vii of agomelatine, preparation method and use thereof and pharmaceutical composition containing same

The present invention provides a new crystal form VII of agomelatine, the preparation method and use thereof and a pharmaceutical composition containing the same. The new crystal form has a good purity, a stable crystal form and good reproducibility; the preparation method thereof is easy to amplify; and it is superior to most previously reported crystal forms in terms of stability and solubility. Therefore, the crystal form VII of the present invention has an advantage in terms of preparation.

AGOMELATIN, A CRYSTAL FORM VII, ITS PREPARATION METHODS, APPLICATIONS AND PHARMACEUTICAL COMPOSITIONS

Reivindicación 1: Un polimorfo de agomelatina de acuerdo con el modelo de difracción por rayos X, caracterizado por ángulo 2q:@@@@@@@@@ Claim 1: An agomelatine polymorph according to the X-ray diffraction model, characterized by angle 2q: @@@@@@@@@@

New crystal form vii of agomelatine, preparation method and use thereof and pharmaceutical composition containing same

AbstractNew crystalline form VII of agomelatine, preparation method and use thereof and pharmaceutical composition containing sameThe present invention provides a new crystalline form VII of agomelatine, its method of preparation, application and pharmaceutical composition. This new crystalline foim offers high purity, a stable crystalline structure and good reproducibility, while its method of production lends itself well to large scale production. In terms of stability and purity, it is superior to the numerous crystalline forms which have hitherto been reported. As a result, the crystalline form VII of the present invention possesses advantages in pharmaceutical preparation.

Agomelatine hydrochloride hydrate and preparation thereof

An agomelatine hydrochloride hydrate of formula (I), preparation, use, and pharmaceutical composition thereof are provided. Said hydrate obtained through the present method has significant increased solubi1ity than agomelatine, and therefore is more suitable for manufacturing pharmaceutical formulations. Using the present method, high purity can be obtained through a simple process, free of any complicated steps. Wherein X is Cl.

Agomelatine hydrobromide hydrate and preparation thereof.

The present invention relates to an agomelatine hydrochloride hydrate of formula I, preparation and use thereof, and to pharmaceutical composition containing it. The agomelatine hydrohalide hydrate obtained through the present method has significant increased solubility than that agomelatine, and therefore is more suitable for manufacturing pharmaceutical formulations. In addition, the product enjoys higher stability and purity. Using the present method, product of high purity can be obtained through a simple process, free of any complicated steps.

Agomelatine hydrochloride hydrate and preparation thereof

Disclosed is crystalline agomelatine hydrochloride monohydrate as represented by general formula (I), wherein X is Cl. Further disclosed is a method for the preparation of agomelatine hydrochloride monohydrate, wherein agomelatine is reacted with hydrochloric acid in an aqueous organic solvent to produce the agomelatine hydrochloride hydrate. Also disclosed is a pharmaceutical composition, comprising an agomelatine hydrochloride hydrate as defined above in associated with one or more pharmaceutically acceptable adjuvants or excipients.

HYDROBROMIDE HYDROBROMIDE HYDROBROMIDE AND PREPARATION OF THIS

LA PRESENTE INVENCIÓN PROPORCIONA UN HIDRATO DEL HIDROBROMURO DE AGOMELATINA, LA CUAL PRESENTA UNA SOLUBILIDAD, ESTABILIDAD Y PUREZA EXCELENTES, LO QUE LE HACE FAVORABLE PARA SU USO EN LA FABRICACIÓN DE FORMULACIONES FARMACÉUTICAS QUE CONTIENEN AGOMELATINA

Agomelatine hydrobromide hydrate and preparation thereof

An agomelatine hydrobromide hydrate of formula (I), in which X is Br, preparation method and use thereof as well as pharmaceutical composition containing it are provided. The solubility of the agomelatine hydrobromide hydrate obtained by the present method is significantly higher than that of agomelatine. Therefore, it is more suitable for manufacturing pharmaceutical formulations. In addition, the product has higher stability and purity. The present product of high purity can be obtained through a simple process, rather than process with complicated steps.

一种病患会阴护理包

本实用新型涉及一种病患会阴护理包，包括底布，所述底布包括前半部和后半部，其特征在于：所述底布的前半部的中间位置上设有一层吸水层，所述护理区的中间线转动连接一块中间垫布，所述中间垫布沿底布的后半部的中间线左右摆动，所述底布的后半部按中间线分为左护理区和右护理区，所述中间垫布摆动至左护理区上方时，中间垫布的背面朝上且中间垫布的背面上设有第一一次性手套，所述底布的右护理区上设有第二一次性手套，所述底布的左护理区上安装一个无菌操作盆。方便医护人员操作，节省准备备用物的时间，操作时用物归类清楚，方便初学者操作，避免操作者违反无菌操作，保持病人床单位整洁，便于使用后的用物整理。

Sorafenib hemi-p-tosylate monohydrate crystal and preparation process thereof

The present invention relates to the field of medicinal technology, and in particular, to sorafenib hemi-p-tosylate monohydrate crystal and preparation process thereof. The crystal has diffraction peaks occurring at 2θ angle of about 5.62, 6.67, 8.05, 9.06, 9.63, 9.91, 10.95, 11.25, 13.48, 14.00, 14.60, 15.08, 15.75, 16.20, 16.62, 16.80, 17.23, 18.40, 18.97, 19.32, 19.82, 20.49, 20.74, 21.51, 22.56, 22.86, 23.37, 23.71, 24.20, 24.71, 24.97, 25.54, 25.80, 26.18, 27.14, 27.48, and 28.29 degree in a X-ray powder diffraction pattern, and some advantages, such as a high stability, a low hygroscopicity and the like.

Crystal form VII of agomelatine, preparation method and use thereof and pharmaceutical composition containing same

The present invention provides a new crystalline form VII of agomelatine, its method of preparation, application and pharmaceutical composition. This new crystalline form offers high purity, a stable crystalline structure and good reproducibility, while its method of production lends itself well to large scale production. In terms of stability and purity, it is superior to the numerous crystalline forms which have hitherto been reported. As a result, the crystalline form VII of the present invention possesses advantages in pharmaceutical preparation.