140 results about "Free base" patented technology

This disclosure relates to administration of a combination of: 1) about 100-110 mg, about 104-106 mg, or about 105 mg of bupropion hydrochloride, or a molar equivalent amount of the free base form or another salt form of bupropion; and 2) about 40-50 mg, about 44-46 mg, or about 45 mg of dextromethorphan hydrobromide, or a molar equivalent amount of the free base form or another salt form of dextromethorphan in certain patient populations, such as patients having moderate renal impairment, patients receiving a concomitant strong CYP2D6 inhibitor, patients who are known CYP2D6 poor metabolizers, those in need of an NMDA antagonist that does not cause dissociation, and those at risk of QT prolongation.

This disclosure relates to dosage forms comprising bupropion hydrochloride, another salt form of bupropion, or the free base form of bupropion; dextromethorphan hydrobromide, another salt form of dextromethorphan, or the free base form of dextromethorphan, and a polymer. In some embodiments, the dosage form has no significant dose dumping of bupropion in the presence of ethanol in vitro. In some embodiments, the dosage form does not have a food effect for bupropion or dextromethorphan when taken with a high-fat meal in human subjects. Some embodiments include a method of treating a nervous system condition (such as depression, e.g., major depressive disorder, including treatment-resistant depression, agitation associated with Alzheimer's disease (or agitation associated with dementia of the Alzheimer's type), agitation associated with dementia, anxiety (or generalized anxiety disorder), neuropathic pain, or peripheral diabetic neuropathic pain) comprising, administering a dosage form described herein to a human being in need thereof.

The invention relates to the technical field of mineral processing, and particularly provides a combined reagent system for flotation and magnesium reduction of talc-containing copper-molybdenum ore and application of the combined reagent system. The combined reagent system comprises a flotation collecting agent (faint yellow to orange transparent liquid, 40%-50% of active ingredients and less than or equal to 3% of free alkali) with active ingredients in the formula 1 and a flotation depressing agent (light yellow powder, extracellular polysaccharide extract of xanthomonas, the weight-average molecular weight of 1000-1500000 Daltons and rich in hydroxyl, carboxyl and pyruvic acid groups) with a structural formula in the formula 2, and the flotation depressing agent comprises extracellular polysaccharide extract of xanthomonas, the weight-average molecular weight of xanthomonas and the weight-average molecular weight of xanthomonas and is rich in hydroxyl, carboxyl and pyruvic acid groups. Through the synergistic adsorption effect of the combined reagent, the flotation grade and the recovery rate of the copper sulfide molybdenum ore are remarkably improved under the condition that the pH is 8-11. The combined reagent system has the advantages of being high in flotation efficiency, high in selectivity, low in reagent cost, environmentally friendly, high in industrial applicability and the like.

The present invention belongs to the field of biotechnology. Disclosed is a dosage composition of a complement factor B inhibitor. Specifically, the present invention provides a pharmaceutical composition comprising a compound represented by formula I, an isomer thereof, or a pharmaceutically acceptable salt thereof in a unit dosage form, wherein the mass of the compound or the pharmaceutically acceptable salt thereof is 5-1500 mg based on the free base.

The compound cis)-N—((S)-1-(6-(4-fluoro-1H-pyrazol-1-yl)pyridin-3-yl)ethyl)-1-methoxy-4-(4 methyl-6-(5-methyl-1H-pyrazol-3-ylamino)pyrimidin-2-yl)cyclohexanecarboxamide can be prepared as a free base in various crystalline solid forms, and in various salt forms each having one or more solid forms.

The salt, such as adipate salt Form A, and freebase forms of Compound A are WEE1 inhibitors. Such salts and / or forms and freebase forms, as well as pharmaceutically acceptable salts and compositions thereof, are useful for treating diseases or conditions, including conditions characterized by excessive cellular proliferation, such as breast cancer.

Provided herein are crystalline salt and free base forms and amorphous forms of a compound having the following formula (I): (I) Compound 1. Also provided are pharmaceutical compositions comprising such crystalline and amorphous forms, processes for their manufacture and their use for the treatment of various conditions such as hemolytic anemia, sickle cell disease and MDS (very low risk MDS, low risk MDS, lower risk MDS and / or moderate risk MDS).

The present disclosure relates to solid state forms of Compound (1) freebase. The present disclosure also relates to processes for the preparation of the solid state forms, the pharmaceutical compositions comprising the forms, and the use thereof, e.g., in the treatment and prevention of disorders in which NLRP3 activity is implicated.

The subject of the invention is N-substituted derivatives of l-(l-phenyl-3-aryl)-lH-pyrazol-4-yl)methanamine with the general formula 1, where ¥ represents CH or N, R1 represents hydrogen, R2 represents no substituent, R3 represents hydrogen, while R4 represents N-propylbenzamide, benzo[b]furan, dihydrobenzo [b] furan, methylenedioxybenzene, ethyl benzoate, or propyl benzoate, substituted accordingly, their method of production and application, and the method of obtaining and application of N-substituted derivatives of l-(l-phenyl-3-aryl)-IH-pyrazol-4-yl)methanamine with the general formula 1, where Y represents C, CH, or N, R1 represents hydrogen or a methyl group, R2 represents a methyl group or no substituent, R3 represents hydrogen or a methyl group, while R4 represents dimethylpyrazole, methylpyrazole, dimethylimidazo[l,2-a]pyrimidine, or isopropoxybenzene, substituted accordingly. The compounds that are the subject of the invention are obtained through reductive amination using borohydride derivatives as the reducing agent, advantageously sodium triacetoxyborohydride, in the amount of 1.4-2.0 eq, amine in the amount of 1.0-1.1 eq, advantageously in slight excess, base, advantageously triethylamine in the amount of 1.0-1.1 eq (in the case of using amine in the form of hydrochloride), and the starting aldehyde. The reaction is conducted in a nonpolar solvent environment, advantageously dichloroethane at a concentration of about 0.1 M. The crude product is purified by column chromatography on silica gel using a methanol in dichloromethane mixture as the eluent, in concentration ranges from 2% to 5%. In order to obtain a solid form and improve the physicochemical parameters, the free bases are converted into hydrochloride form, and then crystallized from a polar solvent, advantageously ethanol or propanol.

The present invention discloses a series of phenylurea derivative compounds, specifically relating to the compounds as free base, or isomer, or solvate, or pharmaceutically acceptable salt forms; methods of preparing medicaments; compounds composition, and therapeutic uses thereof. The present invention has developed a series of structurally novel compounds based on histamine H3 receptor ligands, and a series of relevant biological tests have been performed on the compounds. The results of the tests all indicate that the compounds have significant H3 receptor antagonistic activity and can be used as lead compounds for the prevention or treatment of H3 receptor-related diseases.

The present invention relates to inhalable formulations, and kits and methods suitable for the preparation of such inhalable formulations. The inhalable formulations comprise a freebase of a deuterium-substituted dimethyltryptamine compound. The inhalable formulations also comprise a biocompatible excipient. Such formulations are suitable for inhalation and have uses in the treatment of psychiatric or neurological disorders. Deuterium-substituted dimethyltryptamine compounds may be metabolised more slowly than their protio analogues, allowing for a longer lasting therapeutic effect.

A method of treating moderate to severe chronic hand eczema in a human patient comprises administering to the skin of the human patient in need thereof an acidified aqueous topical composition comprising 20 mg / g of free base-based digotinib, or a pharmaceutically acceptable salt thereof, twice a day.

This disclosure relates to administration of a combination of: 1) about 100-110 mg, about 104-106 mg, or about 105 mg of bupropion hydrochloride, or a molar equivalent amount of a free base form or another salt form of bupropion; and 2) about 40-50 mg, about 44-46 mg, or about 45 mg of dextromethorphan hydrobromide, or a molar equivalent amount of a free base form or another salt form of dextromethorphan in certain patient populations, such as patients having moderate renal impairment, patients receiving a concomitant strong CYP2D6 inhibitor, patients who are known CYP2D6 poor metabolizers, those in need of an NMDA antagonist that does not cause dissociation, and those at risk of QT prolongation.

Various salt forms and free bases of compound (I) represented by the following chemical formula are disclosed (I).

Heterocyclic compound drugs with a nitrogen atom as a heterocyclic atom may be used as a kinase inhibitor. The preparation of a free base crystal form of the compound is also provided. The compound used as a kinase inhibitor is a compound as shown in formula I, or a deuterated compound thereof, or a pharmaceutically acceptable salt, solvate or prodrug. Biological activity experiments prove that the compound has a good inhibitory activity on exon 20 insertion mutations in EGFR and HER2, exon 19 deletion in EGFR and exon 21 point mutation in EGFR, and can be used as the bulk drug in relevant drugs.

This invention relates to the crystalline form (form 7) of the free base of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-5-oxo-10,15,16,17-tetrahydro-2H-8,4-(methiminated bridged)pyrazolo[4,3-h][2,5,11]benzoxazadiazetatetracycline-3-carboxynitrile (lorlatinib). The invention also relates to pharmaceutical compositions comprising form 7 and to methods of treating abnormal cell growth in mammals, such as cancer, using form 7 and such compositions.

Mesylates of heterocyclic cytokinins of general formula I:wherein R is selected from the group comprising C3-C15 cycloalkyl, furfuryl, allyl, 4-hydroxy-3-methylbut-2-en-1-yl, 3-methylbut-2-en-1-yl, 4-hydroxy-3-methylbutyl, 4-hydroxy-1,3-dimethylbut-2-en-1-yl, 4-hydroxy-1,3-dimethylbutyl, benzyl, wherein the cycloalkyl, allyl, benzyl and furfuryl may be unsubstituted or optionally substituted with 1 to 3 substituents selected from the group containing hydroxy, halogen, methyl, hydroxymethyl and methoxy, and salts, solvates and addition salts thereof. These compounds are particularly suitable for agricultural and biotechnological use, and their great advantage is increased water solubility as compared to the corresponding free bases of heterocyclic cytokinins.

The application belongs to the field of medicine production, and particularly relates to a preparation method of melphalan hydrochloride for removing melphalan-D-isomer impurities, which comprises the following steps: synthesizing N,N-o-phthaloyl-4-(dihydroxyethylamino)-L-phenylalanine ethyl ester, synthesizing N,N-o-phthaloyl melphalan ethyl ester, preparing melphalan free base, crystallizing melphalan hydrochloride and drying, and adding a tartaric acid aqueous solution into a hydrochloric acid-isopropyl alcohol crystallization system, which can effectively remove melphalan-D-isomer impurities, solve the problem of the isomer impurities, and significantly improve the product quality of melphalan hydrochloride and reduce the safety risk.

The application provides a method for preparing alvocidib maleate, wherein crude alvocidib free base is refined, and the refined product is salted with maleic acid to obtain alvocidib maleate; the method is simple in process and convenient for industrialized mass production.

Provided is a type I crystal of a free base of 4-(4-(3-((2-(tert-butylamino)ethyl)amino)-6-(5-(trifluoromethyl)-1,3,4-oxadiazol-2-yl)pyridin-2-yl)piperidin-1-yl)-5,5-dimethyl-5H-pyrrolo[2,3-d]pyrimidin-6(7H)-one, which has peaks at, at least, 2 diffraction angles (2θ±0.2°) selected from the following (a), and at, at least, 2 diffraction angles (2θ±0.2°) selected from the following (b), in a powder X-ray diffraction spectrum (CuKα):(a) 6.2°, 9.3°, 9.7°, 11.1°, 15.4° and 25.1°; and(b) 6.7°, 8.3°, 8.7°, 13.0°, 13.7°, 16.3°, 16.9°, 17.7°, 18.7°, 19.4°, 20.3°, 25.9° and 26.5°.

The contact lens treatment solution comprises: (a) one or more potassium salts selected from the group consisting of potassium chloride, potassium citrate, potassium hydroxide, potassium borate, potassium ethylenediaminetetraacetate, and potassium phosphate; (b) an antimicrobial agent comprising alexidine or a salt or free base thereof; and (c) optionally, one or more sodium salts selected from the group consisting of sodium chloride, sodium citrate, sodium hydroxide, sodium phosphate, sodium ethylenediaminetetraacetate, and sodium borate, wherein, when one or more sodium salts are present, the one or more potassium salts are present in an amount greater than the amount of the one or more sodium salts.

The present invention relates to the field of pharmaceutical crystal forms, and specifically relates to crystal forms of 2-(4,4-difluoroazepin-1-yl)-N-(2-sulfamoylpyridin-4-yl)quinoline-3-carboxamide and a salt thereof, a pharmaceutical composition, and a use. The crystal forms of a compound of formula (I) and a salt thereof which are obtained in the present invention have excellent physical stability and chemical stability, and compared with free base crystal form K1 of the compound of formula (I), have significantly improved solubility, hygroscopicity and bioavailability, and are more conducive to clinical applications. Also disclosed in the present invention is a use of the crystal forms of the compound of formula (I) and the salt thereof as sodium ion channel Nav1.8 inhibitors for treating a wide range of pain.

Provided herein are formulations, processes, solid forms and methods of use (e.g., methods of treating a hematological malignancy) relating to salts of and solid forms comprising free base or salts of (S)-2-(2,6-dioxopiperidin-3-yl)-4-((2-fluoro-4-((3-morpholinoazetidin-1-yl)methyl)benzyl)amino)isoindoline-1,3-dione.

The application provides oseltamivir tablets and a preparation method, the oseltamivir tablets comprising, in terms of weight fractions, 230-250 parts of sustained-release granules, 45-65 parts of immediate-release granules, 10-20 parts of a glidant, and 20-30 parts of a binder, wherein the sustained-release granules contain 110-130 parts of oseltamivir free base, and the immediate-release granules contain 25-35 parts of oseltamivir free base.The oseltamivir tablets have a small single tablet weight and good sustained-release effect, and the patient's medication compliance is strong; by optimizing the particle size and preparation process of the immediate-release granules to reduce the deviation of the initial dissolution rate, the drug quality is controllable and the drug efficacy is stable.

The present invention relates to combinations comprising a checkpoint inhibitor and a c-Met inhibitor, Compound 1. The invention also relates to crystalline forms of the free base of Compound 1, as well as crystalline forms of salts of Compound 1, in combination with a checkpoint inhibitor. The invention further relates to methods of treating cancer by administering Compound 1 as a single agent or a combination described herein.

This disclosure relates to a phosphate salt of 1-((3S,4R)-3-((2-((1-ethyl-1H-pyrazol-4-yl)amino)-7H-pyrrolo[2,3-d]pyrimidin-4-yl)oxy)-4-fluoropiperidin-1-yl)prop-2-en-1-one, a crystalline form thereof, and a method for its preparation. The phosphate salt and crystalline form have low hygroscopicity compared to the free base and improved stability and solubility, making them suitable for pharmaceutical use. Furthermore, the method for preparing the phosphate salt and crystalline form according to this disclosure has the advantage of enabling mass production and improving the safety of the preparation procedure by using safer materials than the reactants used in conventional preparation methods.

Provided is a method for purifying an organic solvent and a device for purifying an organic solvent, with which it is possible to reduce the amount of impurities such as metal impurities of as many kinds as possible from the organic solvent. The method for purifying an organic solvent includes an anion exchanger contact step for bringing an organic solvent to be purified into contact with an anion exchanger A and an anion exchanger B, wherein: the anion exchanger A is an anion exchanger having at least one ionic form that is selected from the group consisting of an OH form, a free base form, a carbonate form, and a bicarbonate form; and the anion exchanger B is a chelate resin that contains a glucamine-type ion exchange group.

The disclosure is in part directed to crystalline free base forms of N-(4-((2-methoxy-3-(1-(methyl-d / 3)-1H,2,4-triazol-3-yl)phenyl) amino)-5-(propanoyl-3,3,3-d / 3)pyridin-2-yl) cyclopropane carboxamide, pharmaceutical compositions thereof, and methods of use.

A sensor to detect solid particles of a target salt can include a support substrate, an adsorption layer, a sensing layer oriented between the support substrate and the adsorption layer, and an electrode pair in contact with the sensing layer and separated by the sensing layer. The adsorption layer can include an ion exchange medium formed of a first porous structured material functionalized with basic or acidic functional groups. The basic or acidic functional groups can remove an acid or base component from the target salt to form a free base or free acid, respectively, of the target salt. The sensing layer can include a second porous structured material functionalized to detect the free base or acid of the target salt by a change in conductivity.