34 results about "Sulphonilamide" patented technology

This invention discloses 2'-hydroxy-4,4',6'-trimethoxychalcone and 5,7,4'-trimethoxyflavanone sulfonamide derivatives, their synthesis methods and applications, belonging to the field of pharmaceutical technology, and involving two series of compounds: 3-sulfonamido-2'-hydroxy-4,4',6'-trimethoxychalcone and 8,3'-disulfonamido-5,7,4'-trimethoxyflavanone, and their preparation methods. Starting with 2-hydroxy-4,6-dimethoxyacetophenone and p-anisaldehyde or 4-methoxy-3-nitrobenzaldehyde, 2'-hydroxy-4,4',6'-trimethoxychalcone or 3-amino-2'-hydroxy-4,4',6'-trimethoxychalcone intermediates were synthesized via the Claisen-Schmidt reaction. Then, through sulfonation and intramolecular Michael addition reactions, 2'-hydroxy-4,4',6'-trimethoxychalcone and 5,7,4'-trimethoxyflavanone sulfonamide derivatives were synthesized. The preparation method is simple, mild, and yields high results. In vitro and in vivo activity tests show that the derivatives disclosed in this invention have significant in vitro inhibitory activity against gastric cancer, esophageal cancer, colorectal cancer, and lung cancer cell lines, acting as inhibitors of the protein YBX1 / RPN1. Clinically, they can be applied to targeted therapy for cancers such as gastric cancer, esophageal cancer, colorectal cancer, and lung cancer.

The present application relates to the formula shown with BCA Tm agonist effect 2- (amino carbonyl) -1H-indole-5-carboxamide derivatives, its racemate or optical isomer, its solvate, or its pharmaceutically acceptable salt, and its use in the preparation of treating metabolic syndrome or obesity drugs and the use of pharmaceutical compositions containing them. Wherein, R1 is the following substituent group amide, methanol, methyl sulfonamide.

The application provides a preparation method of a pyrimidine sulfamide compound, and the method overcomes the defects of the prior art, such as the need of using an excessive strong base, low conversion efficiency, and more by-products, and the like, and the method is characterized in that the pyrimidine sulfamide is generated through the reaction of the combined action of a molecular sieve and a catalyst, the reaction condition is mild, the step is economical, the environment is friendly, the comprehensive production cost is low, the raw material is easy to obtain, the environment is friendly and economical, and the method is beneficial to the industrialized production of the pyrimidine sulfamide compound.

The application discloses a use of a benzene sulfonamide compound in preparation of a medicine for regulating sleep, and the benzene sulfonamide compound has the following structure: the application first proposes the use of the benzene sulfonamide compound in preparation of the medicine for regulating sleep, and animal experiments show that tail vein injection of the benzene sulfonamide compound into mice can promote sleep of the mice, can significantly reduce a proportion of wake time of the mice, and can increase proportions of non-rapid eye movement sleep time and rapid eye movement sleep time.

The application discloses a sulfonamide compound, a preparation method and application thereof. The compound can selectively antagonize a human and mouse NOD1 signal path, can inhibit secretion of inflammatory cytokines, and can be used for treating inflammatory diseases, in particular, gastritis caused by helicobacter pylori infection.

The present invention provides novel fluorinated cyclic derivatives of sulfonamides and sulfones useful in the treatment of various diseases and disorders associated with TRPML activity, such as neurodegenerative diseases, lysosomal storage diseases, muscular dystrophy, age-related common neurodegenerative diseases, oxidative stress or reactive oxygen substance (ROS)-related diseases, aging, etc. The invention also relates to a composition, a preparation method and application thereof.

The application discloses a 1, 2, 3-triazole sulfamide derivative, a preparation method and application thereof. The compound has a general formula (A). The synthesis method is as follows: sulfamide is used as a starting material, diazotization, azidation, and then coupling with ethyl acetoacetate to complete the docking of the triazole ring and the sulfamide, and an amide bond is introduced into the structure, and then a series of novel 1, 2, 3-triazole sulfamide derivatives are synthesized. The compounds have excellent bacteriostatic, insecticidal and fungicidal functions on escherichia coli, pseudomonas aeruginosa, salmonella typhi, staphylococcus aureus, bacillus subtilis, and fungi such as candida albicans and aspergillus niger, pests and plant pathogenic bacteria in forestry and other fields.

The present application relates to the technical field of environmental functional materials, and provides a polysulfamide-metal organic framework acid-resistant nanofiltration membrane as well as a preparation method and application thereof. The present application utilizes the metal organic framework MIL-101(Cr) to regulate the interfacial polymerization process of the polysulfamide selective layer, so that the polysulfamide-metal organic framework acid-resistant nanofiltration membrane with high permeability and good acid resistance is obtained. The polysulfamide-metal organic framework acid-resistant nanofiltration membrane prepared by the present application has good stability in a strong acid solution, can continuously work in acidic wastewater, has a relatively high permeation flux, can significantly improve the separation efficiency, can efficiently recover heavy metal ions in industrial acidic wastewater, and has a good application prospect in water treatment processes. Meanwhile, the preparation method provided by the present application is simple in process, controllable in cost, and suitable for large-scale production and application.

This invention discloses a novel chiral sulfinamide monophosphine ligand based on an oxanthracene skeleton, its preparation method, and its application. The preparation method includes the following steps: (1) oxanthracene is subjected to a substitution reaction with RBr in the presence of sodium hydride and a solvent to obtain intermediate 1; (2) intermediate 1 is subjected to lithium halide exchange with butyllithium in the presence of a solvent, followed by the addition of a halogen to obtain intermediate 2; (3) intermediate 2 is subjected to halogen-metal exchange with isopropylmagnesium chloride in the presence of a solvent, followed by the addition of diphenylphosphine chloride to undergo a substitution reaction to obtain intermediate 3; (4) intermediate 3 is subjected to lithium halide exchange with butyllithium in the presence of a solvent, followed by the addition of a compound to react in the presence of a Lewis acid to obtain the chiral sulfinamide monophosphine ligand. The chiral sulfinamide monophosphine ligand prepared by this invention can be used to prepare chiral α-alkyl-α-benzyltetrahydronaphthone compounds with high yield and ee value.

The application discloses a preparation method of a chiral sulfimine compound and belongs to the technical fields of visible light catalysis and organic synthesis. N -[(9 R )-6'-methoxyoctanosyl]-8-quinolinesulfonamide as a chiral ligand, fluorobenzene as a solvent, under the action of a copper salt and an oxidant, under visible light irradiation at room temperature in a protective atmosphere, the copper salt, the sulfenamide compound and N -[(9 R )-6'-methoxyoctanosyl]-8-quinolinesulfonamide form a copper complex, the copper complex enters an excited state under visible light irradiation, cleaves the oxidant through an energy transfer or single electron transfer process, generates a highly active free radical, the free radical activates an inert carbon-hydrogen bond to generate an alkyl free radical and reacts with the sulfenamide in the copper complex, asymmetric sulfuration of the inert carbon-hydrogen bond is realized, and the chiral sulfimine compound is obtained.

The present disclosure relates to use of a sultam compound in treating biliary tract cancer, and specifically relates to use of a compound represented by formula I or a pharmaceutically acceptable salt thereof in treating biliary tract cancer. The compound represented by formula I or the pharmaceutically acceptable salt thereof of the present disclosure has good safety and anti-tumor activity.

A rubber composition includes a chloroprene-based rubber, 5 to 80 parts by mass of silica, 0.5 to 15 parts by mass a silane coupling agent, and 0.5 to less than 20 parts by mass of a hydrate. The rubber composition satisfies at least one of (i) and (ii): (i) the rubber composition includes 0.1 to 3.0 parts by mass of 3-methyl-thiazolidine-2-thione; (ii) the rubber composition includes 0.1 to 3.0 parts by mass of compound A that is at least one of a thiourea-based compound, 3-methyl-thiazolidine-2-thione, and di(5-mercapto-1,3,4-thiadiazol-2-yl) disulfide; and 0.01 to 3.0 parts by mass of compound B that is at least one of a thiuram-based compound, a sulfenamide-based compound, a thiazole-based compound, a guanidine-based compound, a benzimidazole-based compound, N-phenyl-N-(trichloromethylthio)benzenesulfonamide, and a diazabicycloundecene-based compound.

The invention discloses a macromolecule capable of promoting intake of anticancer drugs, a composition and application of the macromolecule in preparation of the anticancer drugs. The macromolecule contains a plurality of guanidino groups and a plurality of sulfamide groups, the macromolecule has the average molecular weight smaller than or equal to 50,000 Da, and the zeta potential of the macromolecule is smaller than or equal to + 2 mV under the simulated normal physiological condition (pH 7.4) and larger than or equal to + 5 mV under the simulated tumor subacid environment (pH 6.5-6.8). The macromolecules can promote the aggregation and permeation of the anticancer drugs in tumor tissues and promote the anticancer drugs to enter cancer cells, and the anticancer effect of the anticancer drugs can be improved when the macromolecules are combined with the anticancer drugs, so that the anticancer effect is remarkably improved when the macromolecules are combined with the anticancer drugs under the same dosage of the anticancer drugs, and the anticancer effect of the anticancer drugs is improved. Or the toxic and side effects of the anticancer drugs are greatly reduced by combining with the macromolecules under the condition of lower dosage of the anticancer drugs.

Provided herein are compositions and methods for treating myelofibrosis in a subject. The methods comprise administering to the subject an effective amount of a compound, which is N-tert-butyl-3-[(5-methyl-2-{[4-(2-pyrrolidin-1-ylethoxy)phenyl]amino}pyrimidin-4-yl)amino]benzenesulfonamide or a pharmaceutical salt thereof or hydrate thereof.

The present disclosure relates to crystalline forms of sulfamide derivatives and methods for preparing same. Specifically, the present disclosure provides a novel crystalline form of the compound represented by Formula 1 and methods for preparing same. [Formula 1] TIFF2026505853000024.tif34168

Pharmaceutical formulations are provided that include a 4-((2-hydroxy-3-methoxybenzyl)amino)-benzenesulfonamide 12-LOX inhibitor with improved solubility for oral administration. Also provided are pharmaceutical formulations that include a selective 12-LOX inhibitor amorphously dispersed in a material selected from vinylpyrrolidone-vinyl acetate copolymer (Kollidon VA64), aminomethyl acrylate copolymer (Eudragit EPO), hydroxypropyl methylcellulose E3 (HPMC E3), or a combination thereof, and have a high drug load of 30% or more, comprising 40-80% of the total solid content of the formulation. Alternatively, the formulations contain additives, such as surfactants (sodium lauryl sulfate), crystallization inhibitors, or pH adjusters, in an amount of up to 20% of the total solid content of the formulation.

Provided is an industrial hose having excellent heat resistance and excellent adhesion between a plating wire layer 4 and an intermediate rubber layer 3. An industrial hose includes a layer structure in which an inner surface rubber layer 1, an organic fiber layer 2, an intermediate rubber layer 3, and a plating wire layer 4 are sequentially stacked, wherein the inner surface rubber layer 1 is formed from a rubber composition containing (A) to (D) components, the total content (B+C) of (B) and (C) components is 0.8 to 2.2 parts by mass with respect to 100 parts by mass of the (A) component, the mass ratio (B / C) of the (B) component to the (C) component is 1.8 to 18, (A) is a rubber component containing acrylonitrile butadiene rubber, (B) is at least one of a sulfenamide-based vulcanization accelerator and a thiazole-based vulcanization accelerator, (C) is a thiuram-based vulcanization accelerator, and (D) is N-phenyl-N-(trichloromethylthio)benzenesulfonamide.

The application provides a synthesis method of alogentan, and belongs to the technical field of heterocyclic compounds. Bromophenyldichloropyrimidine is used as a raw material, nucleophilic substitution is carried out between bromophenyldichloropyrimidine and excessive sulfonamide to prepare sulfanilamide, then the amino group is protected by using chloromethyl benzyl ether to form a sulfanilamide protector, the sulfanilamide protector is reacted with ethylene glycol under the condition of high temperature and strong base to form hydroxyethyl pyrimidine, the hydroxyethyl pyrimidine is reacted with 5-bromo-2-chloropyrimidine to form alogentan protector, and the chloromethyl benzyl protective group of the alogentan protector is hydrolyzed in acid to prepare alogentan. The application not only solves the problems of reactivity and selectivity of sulfonamide and pyrimidine ring, and the whole reaction process is simple, safe and high in product purity.

This invention provides a sulfadiazine amide compound having the structure shown in Formula (I), or a pharmaceutically acceptable salt thereof, or a stereoisomer thereof, and its use in the preparation of GPX4 inhibitors, as well as its use in drugs for the prevention and / or treatment of tumors. The sulfadiazine amide compound provided by this invention can act on targets including GPX4, exhibits strong inhibitory activity against GPX4, exerts antitumor effects through the ferroptosis pathway, and has strong inhibitory and therapeutic effects on various tumors, including pancreatic cancer.

The invention discloses a sulfonamide dehydrogenated curvulgarin derivative as well as a preparation method and medical application thereof. The specific structure of sulfonamide dehydrogenated curvulgarin is shown as a general formula (I). According to the preparation method, 10, 11-dehydrocurvularia is taken as an initial raw material, and a target compound is obtained through structural optimization. The compound has good anti-tumor activity and can be used as an anti-tumor drug.

The present invention relates to sulfamide derivatives of formula I, wherein the meaning of groups R1 and R2 is indicated in the description, for use to prevent and / or treat alcohol use disorder. The invention also relates to the administration of these derivatives in combination with other drugs and / or ligands. (I)

A system for synthesizing and evaluating chiral oxathiazolidine-2-oxides and chlorophosphoramidites, comprising: a synthesis module; a characterization module; a biological test module; an antibacterial assessment module; a computer-based docking module; and a control and data processing unit; wherein the synthesis module is configured to cyclize α-amino alcohols with halogenated derivatives under controlled stereoselective conditions to generate cyclic sulfamidites or phosphoramidites.

Provided are: a compound defined by chemical formula 1; a stereoisomer thereof; a tautomer thereof; and pharmaceutically acceptable salts of the compound, the stereoisomer, and the tautomer. The compound of the invention can inhibit the activity of topoisomerase I. [Chemical formula 1]

The invention relates to a new group of aromatic sulphonamides derivatives of formula (I) and their synthesis and use for modulation of the activity of protein disulfide isomerase (PDI). More particularly, the invention provides small molecule inhibitors of PDI A3 that display antiplatelet, antithrombotic and anticancer activities.

This specification provides novel sultam compound derivatives, compositions containing such compounds, methods for producing the sames, and uses thereof. The sultam compound derivatives are compounds of the following chemical formula I, or their tautomers, stereoisomers, prodrugs, crystalline forms, isotopic variants, pharmaceutically acceptable salts, hydrates, or solvates. The compounds and compositions of the present invention can be used to treat diseases or disorders mediated by polθ. TIFF2026513172000156.tif44149