229 results about "Free base" patented technology

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.

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.

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.

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.

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 administration of a combination of: 1) about 100-110 mg, about 104-106 mg, or about 105 mg or less 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 or less of dextromethorphan hydrobromide, or a molar equivalent amount of the free base form or another salt form of dextromethorphan in human patients for treating neurological and psychiatric conditions, such as agitation associated Alzheimer's disease and / or reducing relapse of agitation in Alzheimer's disease.

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.

The present invention relates to a free base crystal form of a nitrogen-containing heterocyclic derivative, an acid salt and a crystal form thereof, a preparation method therefor, and a use thereof. In particular, the present invention relates to a free base crystal form of a compound represented by a general formula, an acid salt and a crystal form thereof, a preparation method therefor, a pharmaceutical composition containing a therapeutically effective amount of the salt or crystal form, and a use thereof as an inhibitor in the treatment of diseases such as cardiovascular disease and cerebrovascular disease.

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).

Disclosed herein are crystalline forms of the free base of 2-(4-(4-(aminomethyl)-1-oxo-1, 2-dihydrophthalazin-6-yl)-1-methyl-1H-pyrazol-5-yl)-4-chloro-6-cyclopropoxy-3-fluorobenzonitrile, pharmaceutically acceptable compositions comprising these crystalline forms, and methods of using these crystalline forms.

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.

To provide a crystalline form of a free base of a compound which is an ALK and ROS1 kinase inhibitor having deuterium atoms, or a pharmaceutically acceptable salt thereof.SOLUTION: The present invention provides a crystalline form I of the compound of formula (A), characterized in that its X-ray powder diffraction pattern obtained using CuKα radiation includes at least the characteristic peaks located at the following °2θ: 16.175±0.2, 17.299±0.2 and 21.218±0.2.SELECTED DRAWING: None

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.

The present invention provides freebase and salt forms useful for treating various SMARCA2-mediated disorders, such as cancer, by the administration of small molecule therapeutics that act as inhibitors of SMARCA2. Pharmaceutical compositions comprising the freebase and salt forms, as well as methods of their use and preparation, are also described.

The invention discloses a transdermal drug delivery patch with a five-layer structure and application thereof, and belongs to the technical field of pharmaceutical preparations. The patch comprises a backing film, a donepezil hydrochloride-containing reservoir layer, a controlled release film, an organic alkali-containing adhesion layer and a release film. The release rate of the donepezil hydrochloride is controlled through the controlled release film, the donepezil hydrochloride is isolated from organic alkali, the drug stability is improved, the drug release rate is regulated and controlled, the donepezil hydrochloride passes through the controlled release film and then is subjected to an in-situ reaction with the organic alkali in the adhesion layer, and the donepezil hydrochloride is converted into donepezil free alkali for transdermal delivery. According to the patch, the drug stability is improved, the preparation process is simple, the local safety is high, and the transdermal permeability of donepezil can be remarkably improved.

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

The present invention provides a new crystalline form of Cabozantinib free base, Formula (I), which is chemically known as N-(4-((6,7-dimethoxyquinolin-4-yl)oxy)phenyl)-N'-(4- fluorophenyl)cyclopropane-1,1-dicarboxamide and preparation of its novel crystalline polymorph Form E, Formula (II).

This disclosure relates to administration of a combination of: 1) about 100-110 mg, about 104-106 mg, or about 105 mg or less 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 or less 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.

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.