36 results about "Sulfamide" patented technology

Mcl-1 selective inhibitors, Bcl-2 selective inhibitors, and Mcl-1 / Bcl-2 dual inhibitors and methods of using the same for the treatment of disease are disclosed.

An endocyclic thiamidoamide-arylamide compound and a pharmaceutical composition comprising said compound are described, as well as the use of the same or of the pharmaceutical composition in the treatment of hepatitis B. In particular, a compound that can be used as an inhibitor of HBV replication and that has the structure shown in chemical formula (L), or a stereoisomer or tautomer thereof, or a pharmaceutically acceptable salt, hydrate, or solvate thereof, is described.

The invention discloses a pyrimidine derivative containing a thiosemicarbazide structure and application of the pyrimidine derivative, and relates to the technical field of medicines, the compound has good oxidation resistance and alpha-glucosidase resistance activity, and the compound is 2-(4, 4 '-difluorophenyl)-2-(4, 4'-difluorophenyl)-2-(4, 4 '-difluorophenyl)-2-(4, 4' The IC50 values of the compound 2-(4, 6-dimethyl pyrimidine-2-yl)-N-methylhydrazine-1-methylsulfamide on DPPH (1, 1-diphenyl-2-picrylhydrazyl) scavenging activity and ABTS (2, 2, 6-dimethyl pyrimidine-2-yl)-N-methylhydrazine-1-methylsulfamide are 3.96 mu g / mL and 2.01 mu g / mL respectively, the IC50 value of the compound 2-(4, 6-dimethyl pyrimidine-2-yl)-N-methylhydrazine-1-methylsulfamide on alpha-glucosidase inhibitory activity is 38.62 mu g / mL, the effect is best, and the compound 2-(4, 6-dimethyl pyrimidine-2-yl)-N-methylhydrazine-1 The pyrimidine derivative containing the thiosemicarbazide structure has a general formula shown in the specification, and is superior to control medicaments such as vitamin C, vitamin E and acarbose.

The invention discloses an industrial production method of a quinoline mercaptoacetic acid sulfonamide compound, which comprises the following steps: carrying out condensation reaction on an intermediate D-3 and methyl sulfonamide under the action of a condensing agent, concentrating under reduced pressure until no liquid flows out after the reaction is finished, adding acid, separating out a large amount of solid, filtering, pulping a filter cake with purified water, filtering and drying to obtain the quinoline mercaptoacetic acid sulfonamide compound. A compound D is obtained. The problems that in the prior art, the reaction yield is low, starting material impurities are contained, and the process is complex are solved, and the prepared compound D is low in cost, simple in process operation, high in yield, stable in quality and suitable for large-scale industrial production.

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 invention relates to an internal sulfonamide compound and a preparation method thereof. The invention relates to a preparation method of a sulfamide compound, which comprises the following steps: mixing an aminomalonic acid diethyl ester compound or an N-benzyl malonic acid monomethyl ester monoamide compound, a beta-aryl vinyl sulfonyl fluoride compound and MS, adding a solvent and a base catalyst, reacting at room temperature for 12-24 hours, separating and purifying to obtain the amide compound. The sulfamide compound and the preparation method thereof have the advantages of being simple in method, free of transition metal catalysis, wide in substrate range, mild in reaction condition, good in universality and the like.

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 invention relates to application of a sulfonamide compound or a pharmaceutical composition containing the sulfonamide compound in preparation of a medicine for treating pulmonary edema. The medicine has a prominent curative effect on pulmonary edema by inhibiting NKCC1 targets of lungs and is high in safety, so that adverse effects such as electrolyte disorder caused by potent diuretics are reduced, and the medicine is a better new medicine for clinically treating pulmonary edema.

The invention discloses a low-dielectric-loss chemical silver plating solution and a preparation method thereof. Each liter of the chemical silver plating solution comprises the following components: 0.2-10 g of soluble silver salt, 15-35 g of a complexing agent, 0.1-2 g of soluble nickel salt, 5-25 g of a reducing agent, 0.5-3 g of a stabilizer, 0.5-3 g of a brightener and the balance of water and a pH regulator. The complexing agent comprises at least one of carboxyl polyethylene glycol sulfamide and sodium 2, 3-dimercaptopropanesulfonate. The pH value of the prepared low-dielectric-loss chemical silver plating solution is weak acidity, the low-dielectric-loss chemical silver plating solution is good in compatibility and high in stability, very high stability can be kept after multi-period plating, and meanwhile a prepared silver plating layer is flat and uniform, has good thickness and white and bright metal luster and has high hardness and good wear resistance.

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 belongs to the field of carbon dioxide photocatalytic materials, and relates to a spin catalytic material for promoting CO2 photocatalysis and a preparation method thereof. The material is a high-activity metal grid supramolecule obtained by a volatilization method from a ligand 2,2'-pyrazine dihydrazine methanesulfamide (pbd) and a metal salt. As a photocatalyst, the material can adjust multiple spin states on a single Fe site in the metal grid supramolecule to effectively promote a visible light driven CO2 reduction reaction (CO2RR). After 1h of irradiation, the CO2 to CO yield can reach 6.26mmol g ‑1 , which shows an effective strategy of designing spin-based photocatalysts through supramolecular assembly to promote artificial photosynthesis.

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 invention belongs to the technical field of fracturing, and particularly relates to a temperature-resistant thickening agent for fracturing, and a preparation method of the temperature-resistant thickening agent comprises the following steps: modifying an aromatic ring on the surface of bentonite by using an aromatic ring silane coupling agent, reacting with chlorosulfonic acid to form a sulfonic acid group, and finally modifying a sulfonyl chloride group on the bentonite under the action of a chlorinating agent and a catalyst. Secondly, guar gum is modified with amino through an amino silane coupling agent, then under the catalytic action of triethylamine, the amino-modified guar gum and sulfonyl chloride groups on the modified bentonite are subjected to a nucleophilic substitution reaction to generate sulfonamide groups, and the modified guar gum / bentonite compound, namely the temperature-resistant thickening agent, is better in temperature resistance, salt resistance and anti-shearing effect, and can be used for preparing the high-temperature-resistant thickening agent. And the device can be suitable for more fracturing construction sites.

Provided herein are combinations of a methionine adenylyltransferase II alpha (MAT2A) inhibitor and a topoisomerase inhibitor, splicing inhibitor sulfonamide, or a KIF18 inhibitor. Also provided are methods of using such combinations to treat diseases or conditions, such as cancer.

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.

The invention relates to an exhaled air condensate metabolite composition, a kit and a method for predicting the risk of lung cancer. The exhaled air condensate metabolite composition for predicting the risk of the lung cancer comprises piperic acid, ethionamide, ethyl salicylate, hydroxy fatty acid branched chain fatty acid ester (2: 0 / 24: 4) (hereinafter abbreviated as FAHFA (2: 0 / 24: 4), glycine, indole-3-butyric acid, 4-hydroxyquinoline and methoxy indoleacetic acid. The kit for predicting the risk of the lung cancer comprises reagents required for detecting the contents of piperic acid, ethionamide, ethyl salicylate, FAHFA (2: 0 / 24: 4), glycine, indole-3-butyric acid, 4-hydroxyquinoline and methoxy indoleacetic acid in an exhaled gas condensate sample extraction solution. By means of the combined marker, a good prediction effect on the risk of the lung cancer can be achieved.

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

The raw materials for preparing a polymer self-cleaning coating spraying material include: silica, tetraethyl orthosilicate, hexadecyltrimethylsilane, polytetrafluoroethylene, aluminum tripolyphosphate, sodium silicate, modified MOF, and modified polysulfamide. The beneficial effects of this invention are: the self-cleaning coating prepared by this invention exhibits excellent performance in mesh testing, impact resistance testing, abrasion resistance testing, and cleanliness. In particular, after temperature rise treatment from -30℃ to 40℃, the performance of the self-cleaning coating prepared by this invention does not change significantly. The modified MOF and modified polysulfamide added in this invention ensure the coating's self-cleaning ability, flexibility, and adhesion.

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 invention provides a synthetic method of 4-piperidine sulfamide. The synthesis method of 4-piperidine sulfamide comprises the following step: in a solvent, in the presence of an iron source, a sulfur source and alkali, 4-piperidine sulfamide 2 is subjected to a reaction to obtain 4-piperidine sulfamide 1. The method has the advantages of easily available and stable raw materials, simple preparation method, easily realized reaction conditions, low cost, safety, environmental protection, high atom economy, few side reactions and high target product yield.

The present invention concerns the compound aprocitentan, {5-(4-bromo-phenyl)-6-[2-(5-bromo-pyrimidin-2-yloxy)-ethoxy]-pyrimidin-4-yl}-sulfamide: Formula (I) and its use as endothelin receptor antagonist in a method of treating hypertension including resistant hypertension in a subject in need thereof, said method comprising administering to the subject a pharmaceutical composition comprising a clinically proven effective amount of aprocitentan, or a pharmaceutically acceptable salt thereof.

The present invention provides indazolyl-piperidine sulfamides and related compounds, pharmaceutical compositions, their use for inhibiting mucosa-associated lymphoid tissue lymphoma translocation protein 1 (MALT1), and their use in treating diseases or conditions such as proliferative disorders, inflammatory disorders, or autoimmune disorders.

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)

The invention relates to the technical field of kaolin modification, in particular to modified kaolin with high viscosity concentration and a preparation method and application thereof. The preparation method of the modified kaolin with high viscosity concentration comprises the following steps: mixing kaolin and sulfamide, ball-milling, drying and modifying to obtain the modified kaolin. The invention provides a process for modifying the kaolin by combining dry ball milling and dry modification technologies and using sulfamide, so that the viscosity concentration of the kaolin can be improved, the structure of the kaolin is not changed, the original whiteness of the kaolin is maintained, the viscosity of a kaolin product is effectively reduced, and the comprehensive quality of the kaolin product is improved; and subsequent papermaking coating and other process applications are not influenced, so that the requirements of the papermaking industry are better met.

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 present application relates to a kind of dehydroabietylamine sulfamide derivatives and its preparation method, drilling fluid, the dehydroabietylamine sulfamide derivative can solve barite high-temperature settlement and system stability problem in drilling fluid system when being used as drilling fluid additive, the existence of the ternary phenanthrene skeleton structure and sulfamide group of dehydroabietyl sulfamide compound makes it can continuously maintain good emulsification and dispersion performance at higher temperature, ensures its efficient application in deep oil and gas exploration work.

The invention relates to the field of silicone rubber materials, and discloses high-temperature silicone rubber for an automobile ignition cable and a preparation method of the high-temperature silicone rubber. The invention discloses high-temperature silicone rubber for an automobile ignition cable. The high-temperature silicone rubber is prepared from the following raw materials in parts by weight: 100-120 parts of methyl vinyl silicone rubber, 12-20 parts of a heat-resistant additive, 10-20 parts of fumed silica, 5-10 parts of titanium dioxide, 5-8 parts of a flame retardant and 2-4 parts of a silane coupling agent, the heat-resistant additive is prepared by reacting a styrene monomer with acrylic ester containing fluorine and sulfamide. The silicone rubber material prepared by the invention is applied to an insulating protective layer of an automobile ignition cable, is not easy to generate surface precipitation and viscosity change in a long-term high-temperature environment, has relatively good anti-breakdown performance and high-temperature resistance, has relatively good flexibility and is not easy to crack.