62473-92-1

Usage

Uses

Used in Pharmaceutical Industry:
6-Bromosaccharin is used as a pharmaceutical intermediate for the synthesis of various drugs, including anti-inflammatory and anti-neoplastic medications. Its role in drug production is crucial for the development of new therapeutic agents.
Used in Anticancer Research:
6-Bromosaccharin is used as a subject of research for its potential anti-cancer properties and antineoplastic activity. Its study contributes to the understanding of its effects on cancer cells and the development of novel cancer treatments.
Used in Antimicrobial Agent Development:
6-Bromosaccharin is used in the development of new antimicrobial agents due to its antimicrobial and antifungal properties. Its incorporation into these agents can potentially enhance their effectiveness against various pathogens.

Upstream product

• 56919-16-5 5-bromo-2-methylbenzene-1-sulfonamide 
• 135484-83-2 2-amino-4-bromo-benzoic acid methyl ester 
• 52727-57-8 5-bromo-2-aminobenzoic acid methyl ester 
• 5794-88-7 5-Bromo-2-aminobenzoic acid 
• 106-38-7 para-bromotoluene 
• 1242134-19-5 4-bromo-2-sulfamoylbenzoic acid 
• 69321-56-8 5-bromo-2-methyl-benzene-sulfonyl chloride 

Downstream Products

• 154607-01-9 4-bromo-2-chlorobenzonitrile 
• 1341040-15-0 6-bromo-2,3-dihydrobenzo[d]isothiazole 1,1-dioxide 
• 1414888-01-9 2-benzyl-6-bromobenzo[d]isothiazol-3(2H)-one 1,1-dioxide 
• 1414888-04-2 6,6'-((1,1' : 3',1''-terphenyl)-3,3''-diylbis(methylene))bis(2-benzylbenzo[d]isothiazol-3(2H)-one) 1,1-dioxide 
• 1414888-03-1 (2-benzyl-1,1-dioxido-3-oxo-2,3-dihydrobenzo[d]isothiazol-6-yl)boronic acid 
• 1414888-02-0 2-benzyl-6-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzo[d]isothiazol-3(2H)-one 1,1-dioxide 
• 1310719-85-7 C₂₉H₃₀N₆O₅S 
• 1310719-66-4 C₂₈H₃₀BrN₅O₅S 
• 612537-88-9 5-bromo-2-cyano-N-(5-isopropyl-4-methyl-3H-thiazol-2-ylidene)-benzenesulfonamide 

Relevant academic research and scientific papers

Preparation method and medical application of benzisothiazole and benzothiophene

The invention discloses a preparation method and medical application of benzisothiazole and benzothiophene, and telates to the field of pharmaceutical chemistry. According to the invention, benzisothiazole and benzothiophene are the first type of HIF-2 agonists; compared with a compound M1001 found by the applicant in the earlier stage, the invention has better HIF-2 agonist activity, and has remarkable enhancement activity on expression of mRNA and protein of EPO, VGEF, Glut1, NDRG1 and the like at the downstream of HIF-2, so that the invention can be used for preparing drugs for treating and/or preventing chronic kidney diseases/chronic renal anemia, dyslipidemia and high cholesterol caused by abnormal expression of HIF-2; and the method has a good industrialization prospect.

INHIBITORS OF THE YAP/TAZ-TEAD INTERACTION AND THEIR USE IN THE TREATMENT OF CANCER

The invention relates to compounds of formula (I): wherein R1; R2, R3, R4, R5 and are as defined in the description. The compounds of formula (I) are inhibitors of the YAP/TAZ-TEAD interaction and thu

O-Alkyl Hydroxamates Display Potent and Selective Antileishmanial Activity

Leishmania (L.) infantum causes visceral, cutaneous, and mucosal leishmaniasis in humans and canine leishmaniasis in dogs. Herein, we describe that O-alkyl hydroxamate derivatives displayed potent and selective in vitro activity against the amastigote stage of L. infantum while no activity was observed against promastigotes. Compound 5 showed potent in vivo activity against L. infantum. Moreover, the combination of compound 5 supported on gold nanoparticles and meglumine antimoniate was also effective in vivo and improved the activity of these compounds compared to that of the individual treatment. Docking studies showed that compound 5 did not reach highly conserved pocket C and established interactions with the semiconserved residues V44, A45, R242, and E243 in pocket A of LiSIR2rp1. The surface space determined by these four amino acids is not conserved in human sirtuins. Compound 5 represents a new class of selective ligands with antileishmanial activity.

A scaffold replacement approach towards new sirtuin 2 inhibitors

Sirtuins (SIRT1–SIRT7) are an evolutionary conserved family of NAD+-dependent protein deacylases regulating the acylation state of ε-N-lysine residues of proteins thereby controlling key biological processes. Numerous studies have found association of the aberrant enzymatic activity of SIRTs with various diseases like diabetes, cancer and neurodegenerative disorders. Previously, we have shown that substituted 2-alkyl-chroman-4-one/chromone derivatives can serve as selective inhibitors of SIRT2 possessing an antiproliferative effect in two human cancer cell lines. In this study, we have explored the bioisosteric replacement of the chroman-4-one/chromone core structure with different less lipophilic bicyclic scaffolds to overcome problems associated to poor physiochemical properties due to a highly lipophilic substitution pattern required for achieve a good inhibitory effect. Various new derivatives based on the quinolin-4(1H)-one scaffold, bicyclic secondary sulfonamides or saccharins were synthesized and evaluated for their SIRT inhibitory effect. Among the evaluated scaffolds, the benzothiadiazine-1,1-dioxide-based compounds showed the highest SIRT2 inhibitory activity. Molecular modeling studies gave insight into the binding mode of the new scaffold-replacement analogues.

Novel compounds that are inhibitors of YAP/TAZ-TEAD interaction and their use in the treatment of malignant mesothelioma

These compounds are useful as inhibitors of the YAP/TAZ-TEAD interaction.

Compositions for Treatment of Cystic Fibrosis and Other Chronic Diseases

The present invention relates to pharmaceutical compositions comprising an inhibitor of epithelial sodium channel activity in combination with at least one ABC Transporter modulator compound of Formula A, Formula B, Formula C, or Formula D. The invention also relates to pharmaceutical formulations thereof, and to methods of using such compositions in the treatment of CFTR mediated diseases, particularly cystic fibrosis using the pharmaceutical combination compositions.

SUBSTITUTED HETEROCYCLIC ACETAMIDES AS KAPPA OPIOID RECEPTOR (KOR) AGONISTS

The present invention relates to a series of substituted compounds having the general formula (I), including their ste reoisomers and/or their pharmaceutically acceptable salts, wherein R1, R2, R3. R4, R5, and R6 are as defined herein. This invention also relates to methods of making these compounds including intermediates. The compounds of this invention are effective at the kappa (κ) opioid receptor (KOR) site. Therefore, the compounds of this invention are useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of central nervous system disorders (CNS), including but not limited to acute and chronic pain, and associated disorders, particularly functioning peripherally at the CNS.

COMPOSITIONS FOR TREATMENT OF CYSTIC FIBROSIS AND OTHER CHRONIC DISEASES

The present invention relates to pharmaceutical compositions comprising an inhibitor of epithelial sodium channel activity in combination with at least one ABC Transporter modulator compound of Formula A, Formula B, Formula C, or Formula D. The invention also relates to pharmaceutical formulations thereof, and to methods of using such compositions in the treatment of CFTR mediated diseases, particularly cystic fibrosis using the pharmaceutical combination compositions.

DERIVATIVES OF BENZOTHIAZINES, PREPARATION THEREOF AND APPLICATION THEREOF AS DRUGS

The object of the present invention is benzothiazine derivatives having the capability of inhibiting 11β-HSD1 not only at an enzymatic level but also at a cell level. The compounds of the present invention are of general formula (I). Wherein notably R1 represents a hydrogen or OR1 represents an ester or an ether. R2 represents a naphthyl or a 1, 2, 3, 4-tetrahydro-naphthalene or a biphenyl or phenyl pyridine or a substituted phenyl. R3 represents a methyl or ethyl; R4 and R'4 represent a hydrogen.

Modulators of ATP-binding cassette transporters

Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.