101 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.

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 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.

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).

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 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.

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.

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 invention relates to GABAA positive allosteric modulator compounds, methods of preparation and uses thereof. Described herein are polymorphs comprising 2 ', 6-difluoro-5'-[3-(1-hydroxy-1-methylethyl)-imidazo [1, 2-b] [1, 2, 4] triazin-7-yl] biphenyl-2-carbonitrile (TPA023B) or a salt thereof. In one aspect, crystalline polymorphic salts or co-crystals of TPA023B with phosphoric acid are disclosed herein, Methods of making and using the same are also described herein.

A cocrystal of a compound useful for treating cancer and a process for its preparation, pharmaceutical compositions thereof, and use for cancer treatment comprising administering the cocrystal described herein to a patient in need are provided.

A pharmaceutical use of a pharmaceutical composition containing platinum drugs or platinum drug co-crystals as main active substances in preventing or treating immunological diseases such as rheumatoid arthritis, and other diseases. The platinum drugs mainly refer to oxaliplatin, and the platinum drug co-crystals mainly refer to carboplatin co-crystals or oxaliplatin co-crystals. Further disclosed is a method using platinum drugs or platinum drug co-crystals, either alone or in combination with at least one additional therapeutic agent or adjuvant therapy agent.

The invention provides a 3, 5-dihydroxy-4 '-pentylbiphenyl-betaine eutectic as well as a preparation method and application thereof, and belongs to the technical field of pesticide preparation. The invention provides a 3, 5-dihydroxy-4 '-pentylbiphenyl-betaine eutectic which is formed by combining 3, 5-dihydroxy-4'-pentylbiphenyl and betaine through an intermolecular hydrogen bond, and a preparation method of the 3, 5-dihydroxy-4 '-pentylbiphenyl-betaine eutectic. According to the 3, 5-dihydroxyl-4 '-pentylbiphenyl-betaine eutectic and the preparation method thereof, the eutectic is formed by BP and BET, the solubility and the dissolution rate of BP are improved, the application amount of pesticide molecules is reduced, and the 3, 5-dihydroxyl-4'-pentylbiphenyl-betaine eutectic is applied to various plant pathogenic fungi. Results of the embodiment show that the co-crystals formed by BP and BET are combined through hydrogen bonds in a molar ratio of 1: 1, the dissolution effect of the co-crystals is superior to that of the medicine, and the dissolution effect is not affected by the pH environment. Compared with drugs with the same concentration and the drug eutecticum, the drug eutecticum shows the antibacterial activity advantage superior to that of original drug molecules.

The invention belongs to the technical field of pharmaceutical chemical crystallization, and particularly relates to tripterine, a crystal form of a solvate of the tripterine, a preparation method and application of the tripterine. The crystal form is a co-crystal of the tripterine and a solvent, and the ratio of the tripterine to the solvent is (45-200) mg: (1-30) mL. And the solvent is selected from C1-C4 alcohol solvents, C3-C5 ester solvents and non-polar solvents. 22 solvates and one novel polymorphic form are prepared by slurry conversion and solvent evaporation methods. The solvate is of a unique channel type structure, and solvent molecules are embedded into a three-dimensional framework constructed by a tripterine hydrogen bond network through hydrogen bonds and Van der Waals interaction. The stability of the crystal obtained by the polar solvent is obviously superior to that of the non-polar solvent, the structure-function relationship among the solvent polarity, the crystal structure and the thermal stability is clarified, and a theoretical basis and experimental guidance are provided for the preparation design of the tripterine medicine.

The invention discloses an upatinib eutectic crystal form as well as a preparation method and application thereof, and belongs to the technical field of medicinal chemistry. The invention provides an eutectic crystal form I formed by upatinib and vanillic acid and an eutectic crystal form G formed by upatinib and syringic acid, which have definite and reproducible characteristic X-ray powder diffraction pattern and melting point, have excellent solubility in an aqueous medium, do not generate crystal form transformation after being stored for 1 month under the condition of relative humidity of 40 DEG C / 75%, and can be used for preparing a crystal form of upatinib. And the stability is good. The preparation process route is short, the operation condition is mild, the used solvent is conventional, the target eutectic can be efficiently and repeatedly obtained, the defects that some existing eutectic preparation processes are complex, long in period or harsh in condition are overcome, and the method has good process amplification and industrialization prospects.

This disclosure relates to solid forms of (2S)-2-[(10S,17E)-16-ethoxy-6,8,10,12,20-pentamethyl-2,8,10,11,12,13-hexahydro-14H-5,3-(azenometheno)tripyrazolo[3,4-f:3',4'-j:4'',3''-n][1,4]oxazacyclopentadecin-14-yl]propan-1-ol that are useful in the treatment of disease, such as cancer, in mammals. This disclosure also relates to the preparation of such solid forms, including polymorphs, salts, cocrystals, solvates, hydrates, or a combination thereof. This disclosure also relates to compositions including such solid forms, and to methods of using such compositions in the treatment of diseases, such as cancer, in mammals, especially in humans.

The invention belongs to the technical field of pharmaceutical co-crystals, and particularly relates to a synthetic method and application of an amantadine-butylphthalide co-crystal. Butylphthalide reacts to obtain butylphthalide salt or butylphenyltitanic acid, the butylphthalide salt or butylphenyltitanic acid reacts with different substituted amantadine or hydrochloride thereof to synthesize the pharmaceutical co-crystal, and the co-crystal structure can adjust the crystal lattice energy of the pharmaceutical, improve the solubility of the pharmaceutical in water or physiological media, promote the rapid dissolution and absorption of the pharmaceutical in vivo, improve the bioavailability and improve the bioavailability of the pharmaceutical. According to the eutecticum, the problem of solubility of butylphthalide is solved, the formed eutecticum shows certain neuroprotective activity, the biological activity of the eutecticum is remarkably superior to that of a monomer drug, the clinical medication dosage can be reduced while the same treatment effect is achieved, and the eutecticum has certain scientific research value and industrial popularization significance.

The present disclosure relates to co-crystals of sacubitril (or a salt of sacubitril, in particular an alkaline earth metal salt or alkali metal salt) and melsartan (or a salt of melsartan, in particular an alkaline earth metal salt or alkali metal salt) and methods of preparation thereof, pharmaceutical compositions containing the co-crystals and uses of the co-crystals, in particular for the treatment of cardiovascular system diseases.

The application relates to a pharmaceutical cocrystal of cytarabine and 5-fluorouracil and a preparation method thereof, and relates to the technical field of pharmaceutical cocrystals. The pharmaceutical cocrystal is composed of one cytarabine molecule and one 5-fluorouracil molecule as a basic structural unit, and has a chemical formula of [C9H 13 N3O5.C4H3N2O2F]; the pharmaceutical cocrystal belongs to an orthorhombic system and has a space group of P212121. The pharmaceutical cocrystal prepared by a solvent evaporation method and a cooling method improves the permeability of cytarabine, appropriately reduces the solubility of cytarabine, and significantly improves the antitumor activity of cytarabine; through the complementary advantages of the properties and the pharmacodynamic effects of two components, the synergistic antitumor effects of cytarabine and 5-fluorouracil are realized, and a new idea is provided for developing synergistic antitumor pharmaceutical cocrystals. The pharmaceutical cocrystal can keep the skeleton structure of the crystal unchanged after long-term placement at room temperature, the preparation method is simple and easy to implement, the cost is low, and the pharmaceutical cocrystal is convenient for large-scale production.