12 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 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.

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.

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 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)

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

This invention relates to a method for preparing cyclic sulfonamide compounds. Specifically, the method involves: stirring a cyclic imine and a solvent at room temperature, then adding a nitrogen-containing heterocyclic carbene borane catalyst for reaction; after the reaction is complete, extraction is performed, and the residual crude product is purified to obtain the amine compound; the reaction equation is as follows: R in the cyclic imine and the amine compound... 1 Including hydrogen atoms, ester groups, C1-C4 alkyl or aryl groups, X 1 Including oxygen atoms or carbon and sulfur atoms directly connected at both ends, R 2 and X 2 Choose one of the connections, R 2 Including hydrogen atoms, methoxy groups, C1-C4 alkyl or aryl groups, X 2 It is a halogen; the molecular structure of the nitrogen-containing heterocyclic carbene borane is: R in the nitrogen-containing heterocyclic carbene borane 3 Including C1-C4 alkyl or aryl groups. Compared with the prior art, the cyclic imine compounds of the present invention exhibit rapid reduction under mild reaction conditions, a simple and efficient process, and a high overall yield.

The present disclosures relates to deuterated anti-cancer compounds that can be useful as modulators of splicing factor RBM39. Also disclosed herein are pharmaceutical compositions that can include a compound of Formula (I), the use and preparation thereof.

The invention discloses a green synthesis method of an accelerator N, N-dicyclohexyl-2-benzothiazole sulfenamide, which comprises the following steps: reacting dibenzothiazyl disulfide (MBTS) as a sulfur source with dicyclohexylamine in a solvent in the presence of iodine / iodide ions (I / I <->) in an air or oxygen atmosphere under a weakly alkaline condition to generate DCBS (N, N-dicyclohexyl-2-benzothiazole sulfenamide). Compared with an existing oxidation system, the method has the advantages that the process is simplified, salt load and waste liquid are remarkably reduced, operation safety is improved, product purity is high, yield is stable, and the method is suitable for large-scale industrial production.