235 results about "Cocrystal" patented technology

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 invention discloses a glabridin-nicotinamide eutectic crystal and a preparation method and application thereof, and belongs to the technical field of eutectic crystals, the eutectic crystal comprises nicotinamide and glabridin molecules, the molecular formula of nicotinamide-glabridin is C26H26N2O5, and the molar ratio of nicotinamide to glabridin is 1: 1. According to the invention, the cocrystal is used as a raw material, complete characterization is carried out on the cocrystal to prove that the cocrystal has certain physical and chemical stability, the stability of nicotinamide is improved after the cocrystal is prepared, and no irritant substance nicotinic acid is generated in cosmetics in a cocrystal stability experiment. And the eutectic crystal is generally neutral, mild, non-irritant, natural and suitable for cosmetics or health care products.

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.

Disclosed is a novel quercetin-hexahydric alcohol cocrystal. These cocrystals have been developed as innovative pharmaceutical formulations. The present invention encompasses methods for producing these cocrystal materials, as well as their application as bioenhancers for active pharmaceutical ingredients, phytochemicals, vitamins, and minerals. The disclosed process for preparing quercetin-hexahydric alcohol cocrystals involves the formation of the cocrystal through a kinetic-controlled co crystallization process, enhancing the bioavailability and efficacy of bioactive compounds.

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.

Compositions comprising cocrystals of acetylsalicylic acid and theanine that have been formulated with tromethamine are provided. Methods of preparing the compositions and methods of using the compositions with optional zinc or dipyridamole treatments are also provided.

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.

This present application discloses a chemical entity of formula (I), a pharmaceutically acceptable salt and / or hydrate and / or cocrystal and / or drug combination thereof that inhibits epidermal growth factor receptor (EGFR, ERBB1) and / or Human epidermal growth factor receptor 2 (HER2, ERBB2). The chemical entity of formula (I) is useful, e.g., for treating a condition, disease or disorder in which increased (e.g., excessive) EGFR and / or HER2 activation 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 application also provides compositions containing the same as well as methods of using and making the same.

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 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 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-((36S,4aR)-5,5-difluoro-3-(trifluoromethyl)-3b,4,4a,5-tetrahydro-1H-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.

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.

The invention discloses a cocrystal of rhein and sophocarpine, a preparation method thereof, and a composition and use thereof. The invention belongs to the field of medical technology. Specifically, the invention discloses a cocrystal of rhein and sophocarpine with a lead compound rhein as a pharmaceutical active ingredient and sophocarpine as a cocrystal ligand; a preparation method of the cocrystal of rhein and sophocarpine; and the use of the cocrystal of rhein and sophocarpine as a pharmaceutical active ingredient in the preparation of anti-inflammatory, anti-infective, anti-osteoarthritis and other drugs.

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 invention discloses a eutectic of omeprazole and 3, 5-dinitrobenzoic acid, the molar ratio of omeprazole to 3, 5-dinitrobenzoic acid is 1: 1, and compared with omeprazole, the eutectic has higher stability, in-vivo absorption speed and onset speed.

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.

The invention relates to two sitagliptin pharmaceutical co-crystals as well as a preparation method and application thereof. The sitagliptin pharmaceutical co-crystal 1 (sitagliptin-CaCl2 co-crystal) is formed by combining the sitagliptin pharmaceutical co-crystal 1 (sitagliptin-CaCl2 co-crystal) according to the molar ratio of 2: 1, and the molecular formula of the sitagliptin pharmaceutical co-crystal 1 is C32H30CaCl2F12N10O2; the sitagliptin pharmaceutical co-crystal 2 (sitagliptin-ZnBr2 co-crystal) is formed by combining the sitagliptin pharmaceutical co-crystal 2 (sitagliptin-ZnBr2 co-crystal) according to the molar ratio of 1: 1, and the molecular formula of the sitagliptin pharmaceutical co-crystal 2 is C16H15ZnBr2F6N5O. The two Sitagliptin pharmaceutical co-crystals prepared by the invention are characterized by means of X-ray powder diffraction (PXRD), single crystal X-ray powder diffraction (SCXRD), differential scanning calorimetry (DSC), thermogravimetric analyzer (TGA) and the like. Compared with the prior art, the sitagliptin pharmaceutical co-crystal prepared by the invention has one or more improved characteristics compared with the existing compound, and has important value for optimization and development of the medicine in the future.

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.

The invention provides an IWV / MFI cocrystallization molecular sieve and a preparation method and application thereof. The chemical composition of the cocrystallization molecular sieve is mSiO2.nGeO2.xXO1.5, X is a framework trivalent element, the molar ratio m: n of SiO2 to GeO2 is (2.5-10): 1, and the ratio (m + n): x of the sum of the molar numbers of SiO2 and GeO2 to the molar number of XO1.5 is (35-80): 1. The IWV / MFI co-crystallization molecular sieve is prepared through a single template agent, the process is simple, the proportion of the IWV molecular sieve and the MFI molecular sieve in the co-crystal is adjustable, and different use requirements can be met.

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 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.