161 results about "Cocrystal" patented technology

The present disclosure relates to pharmaceutically acceptable salts, cocrystals, and crystalline forms thereof, of a compound which is N—((S)-1-(3-(4-chloro-3-(methylsulfonamido)-1-(2,2,2-trifluoroethyl)-1H-indazol-7-yl)-6-(3-methyl-3-(methylsulfonyl)but-1-yn-1-yl)pyridin-2-yl)-2-(3,5-difluorophenyl)ethyl)-2- ((3bS,4aR)-5,5-difluoro-3-(trifluoromethyl)-3b,4,4a,5-tetrahydro-TH-cyclopropa[3,4]cyclopenta[1,2-c]pyrazol-1-yl)acetamide, which is useful in the treatment of a Retroviridae viral infection including an infection caused by the HIV virus.

Processes and methods of preparing Compound (I) are disclosed. Crystalline forms of Compound (I), pharmaceutically acceptable salts, solvates, hydrates, and cocrystals thereof, pharmaceutical compositions comprising the same, methods of treating cystic fibrosis using the same, and methods for making the same are also disclosed.

The invention relates to the technical field of pharmaceutical co-crystals, in particular to a co-crystal of p-aminosalicylic acid and proline and a preparation method and application of the co-crystal, the molecular formula of the co-crystal is C7H7NO3. 2C5H9NO2, Mo-K alpha radiation is used, the co-crystal has characteristic peaks at 8.521 + / -0.2 degrees, 9.828 + / -0.2 degrees, 15.584 + / -0.2 degrees, 17.002 + / -0.2 degrees, 22.387 + / -0.2 degrees and 24.087 + / -0.2 degrees through powder X-ray diffraction represented by the angle of 2 theta, and the characteristic peaks are different from the characteristic peaks at the same time. The eutectic crystal provided by the invention not only has very high purity and crystallinity, but also has the solubility obviously higher than that of an existing crystal form, has a relatively high dissolution rate, can be kept stable for a long time without deterioration, effectively avoids the problem of deterioration of a single drug, and keeps relatively good medication safety.

The invention relates to the technical field of eutectic crystals, in particular to a phloretin and nicotinamide eutectic crystal as well as a preparation method and application thereof, an XRD (X-Ray Diffraction) pattern of the eutectic crystal has characteristic diffraction peaks at least at positions where 2 theta angles are 14.54 degrees, 14.95 degrees, 15.28 degrees, 16.11 degrees, 16.71 degrees, 19.50 degrees, 23.14 degrees, 23.48 degrees, 26.00 degrees, 27.39 degrees and 32.66 degrees, and error tolerance of + / -0.2 degrees exists; in a DSC spectrum, characteristic endothermic peaks exist at 124.3 DEG C, 178.4 DEG C and 283.4 DEG C, and error tolerance of + / -0.2 DEG C exists. The preparation method comprises the following steps: dissolving nicotinamide and phloretin in water, and carrying out ultrasonic treatment, standing, crystallization, filtration, vacuum drying and grinding to obtain the eutectic crystal which can be applied to cosmetics, health care products, food and medicines. The eutectic crystal provided by the invention has the advantages of no irritation, high safety, easy absorption and good stability.

The present invention belongs to the field of biopharmaceuticals and specifically relates to a composition for detoxifying alcohol and preventing hangovers and its preparation method, comprising the following steps: 1) adding a portion of yeast extract to purified water to obtain solution A, adding curcumin to anhydrous ethanol to obtain solution B, and mixing solution A and solution B to obtain a mixed solution; 2) adjusting the pH of the mixed solution to 5-6; 3) placing the mixed solution in a -25°C cold trap and allowing it to stand for 16-32 hours until crystals precipitate; 4) filtering at 4°C to obtain a filter cake and a filtrate; 5) pulverizing the filter cake to obtain a crystalline powder; and 6) uniformly mixing the crystalline powder, another portion of yeast extract, dihydroquercetin, and excipients, and then tableting to obtain the composition for detoxifying alcohol and preventing hangovers. The present invention utilizes a complex formed by precipitating the yeast extract and curcumin cocrystals, which expands the application range of the composition and improves the solubility and bioavailability of curcumin.

This invention belongs to the technical field of medicinal chemistry and provides a milrinone-tartaric acid cocrystal. Using Cu-Kα radiation, its X-ray diffraction pattern (expressed as 2θ) exhibits characteristic peaks at at least 10.0±0.2°, 13.2±0.2°, 20.4±0.2°, 24.7±0.2°, 26.2±0.2°, 26.7±0.2°, and 34.3±0.2°. The cocrystal of this invention has high solubility and good stability. Using this cocrystal to prepare formulations avoids the use of large amounts of excipients and auxiliaries in existing technologies, reducing both production costs and clinical safety risks. The preparation method of the milrinone-tartaric acid cocrystal provided by this invention is simple to operate, the crystallization process is easy to control, and it has good reproducibility.

The present invention provides a neomycin-lactulose cocrystal and a preparation method thereof. The cocrystal is prepared from neomycin and lactulose. The powder X-ray diffraction pattern of the neomycin-lactulose cocrystal has diffraction angles 2θ=12.3°±0.2°, 13.9°±0.2°, 14.9°±0.2°, 16.2°±0.2°, 17.3°±0.2°, 18.1°±0.2°, 18.8° The neomycin-lactulose cocrystal of the present invention has characteristic peaks at 14.5°±0.2°, 19.5°±0.2°, 22.1°±0.2°, 23.2°±0.2°, 24.7°±0.2°, 25.4°±0.2°, 27.4°±0.2°, 28.0°±0.2°, 29.2°±0.2°, 29.8°±0.2°, 31.7°±0.2°, and 33.3°±0.2°. Compared with existing neomycin, the neomycin-lactulose cocrystal of the present invention has more stable physical properties and significantly improved bioavailability under the same conditions.

The invention discloses a eutectic of a compound as shown in a formula (I) and fumaric acid, a pharmaceutical composition and application of the eutectic. Specifically, the invention discloses a eutectic formed by a compound shown as a formula (I) and fumaric acid in a molar ratio of 1: 0.4-0.6, and the structure of the eutectic is shown as a formula (II), the invention also relates to a preparation method of the eutecticum of the compound as shown in the formula (I) and fumaric acid.

A cocrystal having the formula LiX·aM, or a solvate or hydrate thereof, wherein X is a conjugate base of an organic acid, M is a neutral organic molecule, and a is from 0.5 to 4, pharmaceutical compositions comprising such cocrystals, cocrystal solvates, or cocrystal hydrates, and methods of preparing such cocrystals, cocrystal solvates, or cocrystal hydrates, and such pharmaceutical compositions.

The invention relates to a method for producing a polymorphic or pseudo-polymorphic crystalline phase from a plurality of compounds (C, D, S1, S2), the method comprising steps of preparing (I) a supersaturated solution from the compounds, homogenizing (II) the supersaturated solution in an ultrasonic bath, transferring (III) the supersaturated solution into a plurality of heated tubes (54), aging (V) the solutions transferred into the tubes for a predetermined period of time, exposing the tubes (54) to a polarized pulsed laser beam before and / or during exposure, followed in situ by nucleation and then growing cocrystals inside the tubes (54), and filtering the exposed solutions in order to recover cocrystals having a size greater than a predetermined minimum size. This method is carried out in order to obtain cocrystallization from at least one active substance (D) and a coformer (C) in at least a first solvent (S1) and a second solvent (S2).

The invention relates to the technical field of eutectic crystals, in particular to an aesculin and mannitol eutectic crystal and a preparation method and application thereof.The XRD spectrum of the eutectic crystal at least has characteristic diffraction peaks at the positions where the angle 2 theta is 13.80 degrees, 17.41 degrees, 18.87 degrees, 19.99 degrees, 20.55 degrees, 21.46 degrees, 25.29 degrees, 27.15 degrees, 27.66 degrees, 28.30 degrees, 33.32 degrees, 34.13 degrees, 35.67 degrees, 36.33 degrees, 36.80 degrees and 44.06 degrees, and error tolerance of + / -0.2 degrees exists; characteristic endothermic peaks exist at 167.5 DEG C and 327 DEG C in a DSC spectrum, and error tolerance of + / -0.2 DEG C exists. The preparation method comprises the following steps: dissolving mannitol and escin in deionized water, heating and stirring, and carrying out high-temperature and high-pressure reaction, standing, crystallizing, filtering and drying to obtain the eutectic crystal which can be applied to cosmetics, health-care products, foods and medicines. The eutectic crystal provided by the invention has the advantages of no irritation, high safety, easy absorption and good stability.

New derivatives of 1-(4-methoxyphenyl)-7-oxo-6-[4-(2-oxopiperidin-1-yl) phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo [3,4c] pyridine-3-carboxamide (Apixaban) able to increase its water solubility. These derivatives are cocrystals derivatives ofApixaban of different acids, from which the most outstanding are the following: Apixaban Malonic Acid derivative, Apixaban-a-Ketoglutaric Acid derivative, Apixaban-Gallic Acid derivative, Apixaban-Maleic Acid derivative, Apixaban-L-Tartaric Acid derivative, and Apixaban Citric Acid derivative.

This application provides a phenethylresorcinol-proline cocrystal, its preparation method, and application, belonging to the field of cocrystal manufacturing technology. The structural formula of the phenethylresorcinol-proline cocrystal is shown in Formula I. The phenethylresorcinol-proline cocrystal has a good whitening effect, and also has the advantages of low irritation and high stability.

The disclosure is directed to cocrystals of fasoracetam, including R-fasoracetam, and various coformers. Crystalline materials comprising fasoracetam, including R-fasoracetam, are also provided. The disclosure further includes pharmaceutical compositions and methods of treatment of the cocrystals and crystalline materials of the disclosure.

The present disclosure relates to solid forms, such as salts, solvates, cocrystals and polymorphs, of Compound 1 as well as cocrystals of Compound 1 HO. Also disclosed are methods of preparing said solid forms, pharmaceutical compositions comprising the solid forms, and methods of treatment using said solid forms.

This invention discloses a nicotinamide-salicylic acid cocrystal, its preparation method, and its uses, relating to the field of cocrystal technology. The nicotinamide-salicylic acid cocrystal comprises nicotinamide and salicylic acid molecules, and the molecular formula of the nicotinamide-salicylic acid is C0. 13 H 12 N2O4, wherein the molar ratio of nicotinamide to salicylic acid is 1:1; the eutectic is monoclinic, space group P21 / n, with cell parameters a=11.080(2)Å, b=5.0000(10)Å, c=22.820(5)Å, α=90°, β=97.60(3)°, γ=90°, V=1253.1(4)Å. 3 The differential scanning calorimetry (DSC) spectrum of the eutectic showed a characteristic endothermic peak around 142.4 ± 2 °C. This invention addresses the problems of poor stability of nicotinamide, low solubility of salicylic acid, and strong irritation in existing technologies by optimizing intermolecular interactions to form a specific crystal form, thus providing a novel raw material with superior performance for the cosmetics industry. This is achieved through the preparation of a structurally stable, simple, and chemically superior nicotinamide-salicylic acid eutectic with excellent physicochemical properties.

To provide solid forms of a compound, drug substances comprising the same, pharmaceutical compositions comprising the same, methods of preparing the same, and treatment methods therewith.SOLUTION: The invention provides a crystalline form of a compound of formula (I), where the crystalline form has an X-ray powder diffraction pattern including peak positions, in degrees 2-theta (±0.2 degrees 2-theta), of 11.7, 17.8 and 21.8, and at least three peak positions selected from the group consisting of 12.8, 14.2, 19.8, 20.7, 22.2, and 25.0.SELECTED DRAWING: Figure 1

This invention discloses a circularly polarized room-temperature phosphorescent organic cocrystal, its preparation method, and its applications. The organic cocrystal is formed by the self-assembly of chiral donor and acceptor molecules. The chiral donor molecule is S / R-1-(1-naphthyl)ethanol, and the acceptor molecule is 1,2,4,5-benzenetetracarbonyl nitrile. The levorotatory or dextrorotatory chiral donor and acceptor molecules are dissolved in a good solvent, then a poor solvent is added. The mixture is sonicated until completely dissolved and allowed to stand until the solvent completely evaporates, yielding the organic cocrystal. Both the levorotatory and dextrorotatory chiral cocrystals exhibit green phosphorescence emission upon excitation. The lifetime of the levorotatory chiral cocrystal is 24.91 ms, and that of the dextrorotatory chiral cocrystal is 28.48 ms. The cocrystals exhibit excellent circularly polarized room-temperature phosphorescence performance, with the levorotatory chiral cocrystal achieving a phosphorescence efficiency of 22.43% per g. lum | is 0.03. The phosphorescence efficiency of the dextrorotatory chiral eutectic is 30.97%, | g lum | is 0.065.

Provided are co-crystals of Compound (I) and glutaric acid useful in the treatment of cancer and methods of preparing the same, pharmaceutical compositions thereof and uses for the treatment of cancer comprising administering the co-crystals described herein to a patient in need thereof.

Provided herein are crystalline forms of integrin inhibitors, compositions thereof, and methods of their uses. Crystalline forms of tartrate cocrystals of the inhibitors are also described, along with methods of preparing the crystalline forms. X-ray powder diffraction data, thermogravimetric analysis, and differential scanning calorimetry data are provided for the crystalline forms. The integrin inhibitors are useful for treatment of, inter alia, fibrotic diseases.

The presented invention relates to processes for preparation of Abemaciclib, compound of formula (1), or a salt or a solvate, preferably and N,N-dimethylformamide hemisolvate, or a cocrystal or solid forms thereof:

The present invention relates to cocrystals of N-{cis-3-[methyl(7H-pyrrolo[2,3-d]pyrimidin-4- yl)amino]cyclobutyl}propane-1-sulfonamide, to a method for obtaining said cocrystals, and to pharmaceutical compositions comprising said cocrystals, and to the medical uses thereof, particularly for the treatment or prevention of diseases that are known to improve by inhibiting the Janus kinase 1 enzyme.

This invention provides urolithin A cocrystals, their preparation methods, compositions, and applications. Specifically, this invention provides a urolithin A cocrystal with high bioavailability, wherein the urolithin A cocrystal is selected from the group consisting of: urolithin A-proline cocrystals, urolithin A-carnitine cocrystals, urolithin A-nicotinamide cocrystals, or urolithin A-creatine cocrystals. Compared to urolithin itself, the urolithin A cocrystals of this invention exhibit high stability, a significantly lower melting point, and significantly improved solubility and bioavailability. Furthermore, the preparation method is simple, easy to control, and has good reproducibility, allowing for stable acquisition of the target cocrystal. The composition containing the cocrystal, prepared by grinding, has high yield, low cost, and is suitable for large-scale production.

The disclosure generally relates to cocrystals of posaconazole and a coformer. The disclosure further relates to pharmaceutical compositions comprising the cocrystals, as well as methods of making the cocrystals, and methods of treating or preventing fungal, yeast, or dermatophyte infections using the cocrystals.

This invention belongs to the field of pharmaceutical chemistry technology, specifically relating to a monopravir-caprolactam cocrystal, its preparation method, and its applications. The monopravir-caprolactam cocrystal is composed of monopravir and caprolactam in a molar ratio of 1:1.9-2.1. X-ray powder diffraction was performed using Cu-Kα radiation, with angles expressed as 2θ±1, at 6.91, 7.09, 8.38, 11.24, 12.52, 13.26, 13.87, 14.24, 15.22, 16.82, 17.31, and 1... Characteristic peaks are observed at 9.73, 20.22, 20.53, 20.84, 21.90, 22.28, 22.52, 22.95, 23.51, 23.75, 24.00, 24.31, 24.86, 25.35, 26.44, 27.41, 28.02, 28.69, 29.22, 29.84, and 30.33. Monopravir-caprolactam cocrystals can be successfully prepared by grinding and / or solution methods, and grinding and / or melting methods. The preparation process is simple, and the obtained product has high purity. Characterization has confirmed it to be a new cocrystal. Powder flowability and tableting tests revealed that the monopravir-caprolactam cocrystals provided by this invention have better flowability and tableting properties compared to monopravir crystal form I, meeting the requirements of formulation and manufacturing processes.

The present disclosure relates to crystalline and amorphous forms of N2-(3-(2-(2H-1, 2, 3-triazol-2-yl) propan-2-yl)-1-cyclopropyl-1 / / -pyrazol-5-yl)- / V7-ethyl-5-(trifluoromethyl) pyrimidine-2, 4-diamine, co-crystals, pharmaceutical compositions, and formulations thereof.

This disclosure features chemical entities (e.g., a compound or a pharmaceutically acceptable salt, and / or hydrate, and / or cocrystal, and / or drug combination of the compound) that inhibit (e.g., antagonize) Stimulator of Interferon Genes (STING). Said chemical entities are useful, e.g., for treating a condition, disease or disorder in which increased (e.g., excessive) STING activation (e.g., STING signaling) contributes to the pathology and / or symptoms and / or progression of the condition, disease or disorder (e.g., cancer) in a subject (e.g., a human). This disclosure also features compositions containing the same as well as methods of using and making the same.

The present invention provides a co-crystal of adenosine dihydroxysuccinate, a preparation method thereof, and an application thereof. In the co-crystal of adenosine dihydroxysuccinate, the molar ratio of dihydroxysuccinic acid molecules to adenosine molecules is 1:(1-4). Without changing the structure of adenosine itself, dihydroxysuccinic acid is combined with adenosine to improve the water solubility of adenosine. Adenosine, which is hardly soluble in water, is prepared into a water-soluble co-crystal of adenosine dihydroxysuccinate, and the water solubility of the co-crystal of adenosine dihydroxysuccinate can reach 4%. It not only does not destroy the efficacy of dihydroxysuccinic acid and adenosine monomers, but also the two work synergistically to exert better effects, and has better effects than monomers and simple mixtures in many aspects such as antibacterial, antioxidant, anti-aging, hair care and anti-hair loss, and has good application prospects in skin care and hair care products.