39 results about "Phenylsulfonamide" patented technology

The application relates to a synthesis method of a phenothiazine derivative, and belongs to the technical field of synthesis in organic chemistry. A diaryl iodonium salt and N-(2-mercapto phenyl)-4-methyl benzene sulfonamide are used as starting materials, and chlorpromazine and perphenazine are obtained through a plurality of steps of substitution reaction, reduction reaction, addition reaction and deprotection reaction. In the application, the reaction raw materials are easy to obtain, the yield is high, and chlorpromazine and perphenazine can be successfully obtained.

The application discloses an amino benzene sulfonamide derivative and application thereof. The structural general formula of the amino benzene sulfonamide derivative is shown in the following formula. The amino benzene sulfonamide derivative has good pepsin inhibitory activity, can effectively block the adhesion and reactivation of pepsin in the pharyngeal mucosa, and has super high selectivity in the internal proteinase family compared with other non-specific protease inhibitors, thereby significantly reducing the off-target risk of normal physiological proteases in the human body. In addition, the compound is particularly suitable for local spray administration in the throat, can maintain a high concentration in the lesion site, and overcomes the defect of traditional oral antacid drugs in the insufficient effect on non-acid reflux, thereby providing a new solution for the treatment of throat reflux diseases.

The application belongs to the technical field of biomedicine, and particularly relates to a benzene sulfonamide derivative and application thereof in antidepressant drugs. The structural general formula of the compound is (I). The compound or a pharmaceutically acceptable salt thereof has agonistic activity on 5-hydroxytryptamine 2A type receptors. The compound is determined to have good antidepressant activity through a mouse tail suspension test model, an open field test model and a forced swimming test model, is a novel antidepressant compound with wide application prospect, has no hallucinogenic effect, and can be developed into an antidepressant therapeutic drug.

A method for preparing N-phenyl-N-trichloromethylthio phenyl sulfonamide by one-pot method, organic solvent, aniline and catalyst are added to phenylsulfonyl chloride, then slow addition of acid binding agent, incubation for 1-4 h to obtain a reaction solution containing intermediate N-phenyl phenyl sulfonamide; the system is cooled to 0-20℃, slow addition of per-chloromethylthio alcohol, after the end of feeding, continue to react for 1-4 h; then add water to separate the phases, add appropriate amount of water in the organic phase to distill the organic solvent, filter to obtain N-phenyl-N-trichloromethylthio phenyl sulfonamide. The method uses organic solvent as solvent, adopts two-step reaction one-pot method, the process is simple, improves the reaction conversion rate, effectively reduces the generation of by-products, the yield of the product is high, and the quality is good. The used organic solvent and acid binding agent can be recycled and used, which reduces the production cost and greatly reduces the three wastes, and is suitable for industrial production.

The application provides a 4-quinazolinone derivative containing a benzene sulfonamide piperazine ketone and a preparation method and application thereof. The derivative has the structure shown in the following general formula I. The application further relates to a preparation method of a compound containing the structure of formula I and application of the compound as an HIV-1 / HIV-2 capsid protein regulator in preparation of an anti-AIDS drug.

The invention provides a benzenesulfonamide derivative, a preparation method thereof and application of the benzenesulfonamide derivative in preparation of PARP1 inhibitors and antitumor drugs, and belongs to the technical field of medicines. The invention synthesizes a novel benzenesulfonamide derivative, namely a compound N, 4-dimethyl-N-(7H-pyrrolo [2, 3-d] pyrimidine-4-yl) benzenesulfonamide, and the benzenesulfonamide derivative provided by the invention can inhibit PARP1 enzyme activity in a targeted manner so as to inhibit DNA repair, activate a p53-mediated DDR signal channel, inhibit DNA repair and inhibit the expression of a p53-mediated DDR signal channel. The benzenesulfonamide derivative can induce apoptosis of lung cancer tumor cells and influence the cycle of the lung cancer tumor cells, has remarkable antitumor activity, and is simple in synthesis method, easy in raw material obtaining, high in synthesis route yield, environment-friendly and simple and convenient in operation process. The PARP1 inhibitor disclosed by the invention is simple in preparation process, high in drug purity, high in yield, stable in quality and easy for large-scale production. The compound disclosed by the invention has a wide prospect in the aspects of development and application of antitumor drugs.

The invention discloses a ruthenium complex of targeted carbonic anhydrase as well as a preparation method and application of the ruthenium complex. The complex takes ruthenium (Ru < 2 + >) as a central metal ion, is formed by coordinating a bidentate ligand (An-en) containing an anthracene structure, a pyridine derivative ligand (N-ABS) containing a benzenesulfonamide group and a ruthenium precursor, and has the capability of accurately targeting tumor cell carbonic anhydrase IX (CAIX); the complex is low in dark toxicity and excellent in curative effect in an anoxic environment, the defects that a traditional ruthenium complex is high in dark toxicity and poor in anoxic curative effect can be effectively overcome, and an efficient and low-toxicity new strategy is provided for anoxic tumor treatment.

The invention discloses an application of N-(4-methoxyphenyl)-4-(4-methoxyphenyl) benzenesulfonamide in preparation of drugs for treating allergic diseases, and belongs to the technical field of biological medicines. The invention discloses a new pharmaceutical application of N-(4-methoxyphenyl)-4-(4-methoxyphenyl) benzenesulfonamide for the first time, and the N-(4-methoxyphenyl)-4-(4-methoxyphenyl) benzenesulfonamide serving as an anti-allergic antagonist can effectively inhibit phospholipase C activity of stimulated cells and mediated calcium mobilization thereof in vitro. And the effective dose of the desloratadine, which is a positive drug, is lower in vivo to generate a comparable anti-allergic effect with the desloratadine. Meanwhile, in animal models of allergic rhinitis and atopic dermatitis, compared with a positive drug desloratadine, the compound can effectively inhibit the pathological progress of diseases at a lower dosage. Therefore, the compound has a definite effect of inhibiting in-vitro and in-vivo anaphylaxis, and can be effectively applied to the development of drugs for treating allergic diseases.

The invention provides an aggregation-induced emission (AIE) ionic probe (E)-4-(2-(5-(4-(diphenylamino) phenyl) thiophene-2-yl) vinyl)-1-(4-sulfanilamide acyl benzyl) quinoline-1-onium hexafluorophosphoric acid (V) salt of a targeted golf apparatus, namely a fluorescent probe TTQ-GA, a preparation method of the fluorescent probe TTQ-GA and application of the fluorescent probe TTQ-GA in the aspect of detection. The benzenesulfonamide group of the probe can be selectively combined with a Golgi apparatus protein cyclooxygenase 2 (COX-2) inhibitor SC-558 to realize Golgi apparatus targeting; due to the hydrophobic triphenylamine part and the hydrophilic quinoline cation part of the probe, the probe has amphipathy; the probe does not emit fluorescence in an aqueous solution, and can emit strong fluorescence when molecular movement is limited and excited, so that no-wash marking of the Golgi apparatus is realized; the probe generates a large amount of ROS under light excitation, promotes local lipid peroxidation increase of Golgi apparatus, and promotes cancer cell apoptosis.

The invention discloses a small-molecule inhibitor based on lactic dehydrogenase targeted design and application thereof, and belongs to the field of biological medicine, the small-molecule inhibitor is a benzenesulfonamide compound or pharmaceutically acceptable salt thereof, and the structure of the small-molecule inhibitor is shown in the specification. The lactic dehydrogenase inhibitor is suitable for treating and / or preventing diseases mediated by lactic dehydrogenase.

The application provides a benzene sulfonamide piperazine ketone glycine derivative and a preparation method and application thereof. The derivative has a structure shown in the following general formula I. The application also relates to a preparation method of a compound containing the structure of formula I and application of the compound as an HIV-1 / 2 capsid protein regulator in preparation of an anti-AIDS drug.

A compound of Formula (I) is provided: (I) Salts and crystalline forms of the compound of Formula (I) are also provided. The compound of Formula (I) and crystalline forms thereof can be used for the treatment of several conditions linked to the inhibition of SGK-1, such as a cardiovascular disease selected from the group consisting of Long QT syndrome, heart failure, arrhythmia, ischemic injury, ischemic infarction, inflammatory and fibrotic diseases, cardiac fibrosis, vascular proliferation, restenosis, dilated cardiomyopathy, and stent failure; cancer; epilepsy; Parkinson's disease; and Lafora disease.

The application discloses a series of 4-piperazine thiourea phenyl sulfonamide-1,8-naphthalimide derivatives with various structures and a preparation method of the derivatives. Test results show that some target compounds have good inhibitory activity on CA IX, and can be used for preparing drugs for inhibiting carbonic anhydrase IX enzyme activity and / or overexpression. Some target compounds have good antitumor activity on various tumor cell strains, and are expected to be used for preparing antitumor drugs.

This invention discloses a benzamide / benzenesulfonamide compound containing an aryl butanone structure, its preparation method, and its application, belonging to the field of medicinal chemistry. The structure of the benzamide compound containing the aryl butanone structure is as follows: R1 is hydrogen, halogen, alkyl, or alkoxy; R2 is tert-butyl, tert-pentyl, tert-octyl, adamantyl, or α,α-dimethylbenzyl; R3 is hydrogen, halogen, alkyl, alkoxy, fused ring, or aryl; R4 is hydrogen, alkyl, or aryl. The structure of the benzenesulfonamide compound containing the aryl butanone structure is as follows: R1 is hydrogen, halogen, or alkyl; R2 is tert-butyl, tert-pentyl, or tert-octyl; R3 is hydrogen, halogen, alkyl, or fused ring. The advantages of this invention are that some of the prepared compounds exhibit strong inhibitory effects on MCF-7 and HCT-116, and can be used as lead compounds for the subsequent preparation and development of antitumor drugs.

Compounds of Formulae I and II are disclosed: I II In compounds of formula I, R 1 is -OH or -NHC(=O)R10. The compounds of formula I are therefore benzenesulfonic acids or N-(phenylsulfonyl)carboxamides. The compounds of formula II are benzenesulfonamides. All of the compounds of formula I are MGAT2 inhibitors and are useful to treat obesity and metabolic dysfunction-associated steatotic liver disease (MASLD). All of the compounds of formula II are useful as intermediates in synthesizing N-(phenylsulfonyl)carboxamides of formula II, and a subset of compounds of formula II are also MGAT2 inhibitors and are useful to treat obesity and metabolic dysfunction-associated steatotic liver disease (MASLD).

Compounds are provided that act as potent antagonists of the CCR(9) receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR(9). The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR(9)-mediated diseases, and as controls in assays for the identification of CCR(9) antagonists.

The present disclosure relates to processes for the fluorination of molecules. One aspect provides a process for incorporating a fluorine atom into a molecule, said process comprising converting a compound of formula X-SG into a compound of formula X-F, wherein G is an optionally substituted C1-C6 alkyl group, an optionally substituted aryl group, or an optionally substituted heteroaryl group, and X is an organic group; and wherein the SG group is attached to a secondary or tertiary carbon atom in the organic group X; said process comprising treating said compound of formula X-SG with (i) an activator compound selected from the group consisting of N-halosuccinimides, N-halobenzenesulfonimides, N-halobenzenesulfonamides, dialkylaminodihalosulfinium salts, heterocyclylaminodihalosulfinium salts, dialkylaminosulfur trihalides, XeF2, difluoroiodotoluene, di- and tri-bromoisocyanuric acids, bromine, chlorine, hypervalent iodine compounds with I2; and other sources of Br+, Cl+, F+, I+, bromonium, iodonium, or chloronium; and (ii) a source of fluoride. Uses of the process in the preparation of various fluorinated molecules as well as uses of certain compounds as intermediates in the processes of the present disclosure are also provided.

The present disclosure provides a novel salt of 5-chloro-2-fluoro-4-((4-fluoro-2-(methyl(2-(methylamino)ethyl)amino)phenyl)amino)-N-(thiazol-4-yl)benzenesulfonamide and a method for preparing the same. The mesylate salt of 5-chloro-2-fluoro-4-((4-fluoro-2-(methyl(2-(methylamino)ethyl)amino)phenyl)amino)-N-(thiazol-4-yl)benzenesulfonamide, which may be prepared using methanesulfonic acid and, without wishing to be bound by theory, can exhibit reduced hygroscopicity and improved physicochemical stability and solubility. In some aspects, the present disclosure provides a pharmaceutical composition for preventing or treating a sodium channel blocker-related disease, comprising the mesylate salt of 5-chloro-2-fluoro-4-((4-fluoro-2-(methyl(2-(methylamino)ethyl)amino)phenyl)amino)-N-(thiazol-4-yl)benzenesulfonamide.

The invention discloses a benzenesulfonamide triazole derivative as well as a preparation method and application thereof, and is characterized in that the benzenesulfonamide triazole derivative has a structural formula shown as a formula I and a formula II or pharmaceutically acceptable salt, ester or solvate of the benzenesulfonamide triazole derivative with the structural formula shown as the formula I and the formula II, x is a carbonyl group, a sulfonyl group or a sulfuryl group; r1 is o-fluorophenyl, p-trifluoromethoxyphenyl, o-methoxyphenyl, o-methoxyanilino, p-methoxyphenyl, pyrimidine, thiazole, oxazole, methylthiophene, amino and methylamino, and the compound has the advantages that the compound can effectively inhibit CDK, the selectivity to CDK1 is higher than that of other subtype and / or eukaryotic tumor cell proliferation, and tumors are prevented and / or treated.

The invention belongs to the technical field of medicinal chemistry, and particularly relates to phenyl sulfanilamide para-triazole derivatives, a preparation method and application of the phenyl sulfanilamide para-triazole derivatives in resisting carbonic anhydrase. The structural general formula of the derivative is as shown in formula I, the invention provides a brand-new phenyl sulfanilamide para-triazole derivative and pharmaceutically acceptable salt, the inhibition activity of the derivative on human carbonic anhydrase is obviously superior to that of traditional inhibitors acetazolamide and methazolamide, and the derivative has selective binding capacity on different human carbonic anhydrase subtypes and has the potential to be developed into a novel carbonic anhydrase inhibition drug.

The invention is directed to the use of carbonic anhydrase V inhibitors for treatment of neurological and psychiatric disorders. In one aspect, the disclosure provides compositions for treating or preventing a neurological or psychiatric disease or disorder comprising a mitochondrial carbonic anhydrase V (CA-V) inhibitor. In various embodiments, the mitochondrial CA-V inhibitor selectively inhibits at least one or more of CA-VA and CA-VB. In some embodiments, the chemical compound is 4-phenylacetamidomethyl-benzenesulfonamide (4ITP), derivative, and analogs thereof.

The present invention relates to: phenylsulfonamide derivatives; a preparation method therefor; and a pharmaceutical composition containing same as an active ingredient for the prevention or treatment of cancer. The compound represented by chemical formula 1 disclosed in the present specification exhibited excellent inhibitory effects against kinases related to integrated stress response (ISR) and is thus expected to be useful as a treatment for cancer.

2-(3-(2-Methyl-6-(p-tolyl) pyridine-3-yl) ureido) benzenesulfonamide (formula I) compound and related pyridine based sulfonamide derivatives are disclosed. The compound of the invention is a carbonic anhydrase targeted small molecule and also an inhibitor of carbonic anhydrase activity and overexpression. Therefore, the compound is useful, as pharmaceutical agent, especially in the treatment and / or prevention of disorders associated with proliferative diseases, such as cancer.

Pharmaceutical compositions including a benzene sulfonamide thiazole compound according to formula (I):Also, the use of the pharmaceutical compositions including the benzene sulfonamide thiazole compound according to formula (I) as a medicament and in the prevention and / or treatment of cancers. The pharmaceutical compositions may be administered by various routes of administration.

The present application relates to the technical field of tumor treatment, and particularly relates to application of benzene sulfonamide compounds in preparation of chemical ablation drugs for treating solid tumors, and the benzene sulfonamide compounds provided by the present application have good application effects in preparation of the chemical ablation drugs for treating solid tumors, and the benzene sulfonamide compounds are selected from one or more of compounds shown in formula I, or stereoisomers, pharmaceutically acceptable salts, solvates or prodrugs thereof. The benzene sulfonamide compounds provided by the present application can significantly improve the anti-tumor activity and selectivity on various cancers (especially human non-small cell lung cancer), and a high-efficiency drug preparation without high-concentration ethanol dilution and ready-to-use is developed by taking the benzene sulfonamide compounds as raw materials, so that systematic breakthroughs are realized in three aspects of compound activity, action mechanism and clinical applicability, and an optimal solution is provided for developing a new generation of high-efficiency, low-toxicity and convenient-to-use tumor treatment drugs.

The invention discloses a 3, 5-dibromo-4-hydroxybenzenesulfonamide compound as well as a synthesis method and application thereof, the compound has the following structural general formula: R is one of the following: R1 is H, C1-C4 alkyl, trifluoromethyl or difluoromethyl, and R2 is H, C1-C4 alkyl or halogen. The 3, 5-dibromo-4-hydroxybenzenesulfonamide compound designed and synthesized by the invention is a novel compound and can be used for treating diseases related to gout.

Crystalline Forms of a compound of Formula I are provided: (I) Crystalline Form C is among the crystalline Forms identified. Form C has an X-ray powder diffraction (XRPD) pattern having characteristic peaks expressed in degrees 2Ɵ (±0.2° 2Ɵ) at 6.46, 15.88, 19.44 and 5.86, and a Differential Scanning Calorimetry (DSC) thermogram that exhibits an endotherm having an onset at 157.1°C.

The invention belongs to the technical field of organic synthesis, and particularly relates to a synthesis method of ester-substituted dibenzothiaza derivatives. The invention discloses a method for realizing intramolecular series aryl carboxylation cyclization reaction of an N-(2-ethynyl aryl)-N-alkyl benzene sulfonamide compound under visible light conditions by taking the N-(2-ethynyl aryl)-N-alkyl benzene sulfonamide compound as a substrate, sodium formate as a C1 source and alkali as an additive in the atmosphere of carbon dioxide (air exists and oxygen accounts for 21%). According to the reaction, under the conditions of room temperature and visible light, the ester-substituted dibenzothiaza derivative is synthesized at a medium yield. The method has the advantages of mild reaction conditions, good substrate compatibility, simple operation, cheap and easily available raw materials, simple preparation, stable structure and the like.

The invention provides a method for synthesizing N-phenyl-N-(trichloromethylthio) benzenesulfonamide by a green process, which belongs to the technical field of organic synthesis, and comprises the following steps: S1, adding solid alkali into an aniline organic solvent, using crown ether as an in-phase ion activator, dropwise adding benzenesulfonyl chloride, and reacting to obtain an organic phase containing N-phenyl benzenesulfonamide; and S2, dropwise adding perchloromethyl mercaptan into the organic phase containing N-phenyl benzenesulfonamide without water washing or phase inversion, carrying out a reaction, and carrying out cooling crystallization, filtration, re-washing and drying to obtain N-phenyl-N-(trichloromethylthio) benzenesulfonamide. The invention provides a method for synthesizing N-phenyl-N-(trichloromethylthio) benzenesulfonamide by a green process, which reduces side reactions, reduces the generation of three wastes, reduces the energy consumption of the process, and achieves the purposes of green and environment-friendly preparation process and obtaining of high-purity products.