452350-33-3

Upstream product

• 124-63-0 methanesulfonyl chloride 
• 52727-57-8 5-bromo-2-aminobenzoic acid methyl ester 

Downstream Products

• 856898-38-9 N-[4-bromo-2-(hydroxymethyl)phenyl]methanesulfonamide 
• 1426683-30-8 C₂₀H₂₁N₃O₂S 
• 1353625-21-4 C₂₃H₂₇BrN₆O₄S 
• 1353629-38-5 C₂₀H₂₁BrClN₅O₃S 
• 1353623-66-1 C₂₃H₂₇BrN₆O₄S 
• 1353628-74-6 C₂₀H₂₁BrClN₅O₃S 
• 1353623-64-9 C₂₆H₃₂BrN₇O₅S 
• 1353623-63-8 C₂₆H₃₂BrN₇O₄S 
• 1225713-29-0 5-bromo-2-(methylsulfonamido)benzoic acid 
• 1353628-72-4 C₂₃H₂₆BrClN₆O₄S 
• 654682-76-5 methyl 5-bromo-2-[methyl(methylsulfonyl)amino]benzoate 
• 1426683-29-5 8-(4-ethylphenyl)-5-methyl-1,5-dihydropyrazolo[4,3-c][2,1]benzothiazine 4,4-dioxide 
• 1426683-47-7 C₁₇H₁₅FN₄O₂S 
• 1426683-46-6 C₁₈H₁₅FN₄O₃S 

Relevant academic research and scientific papers

Synthesis, characterization and biological activities of 2-[(methyl sulfonyl)]amino benzoic acid derivatives and their metal complexes

Sulfonamide derivatives and their metal complexes are acknowledged pharmaceutical moieties because this group has been played the key role as a functional part of the most of the drug structures due to constancy and for bearance in human beings. Sulfonamides have endowed great biological potential such as antibacterial, insulin releasing, carbonic anhydrase inhibitory, anti-inflammatory, antifungal and antitumor activities. In the present work, 2-[(methyl sulfonyl)] amino benzoic acid was N-alkylated using alkylating agent such as methyl. Due to the presence of electron donating groups like, -COOH, -SO2, N-, the above mentioned molecules act as an excellent chelating agent. These substituted N-alkylated sulfonamide ligands were treated with a number of outer and inner transition metals such as Co(II), Cu(II), Ce(II), Pr(II), Dy(II) and Nd(II) to form coordinate complexes. These newly synthesized sulfonamides and their metal complexes were characterized by melting points, solubility, colour, FTIR analysis and XRD. These products were subjected for antimicrobial activities as well as other accessible applications.

NOVEL SULFONYLAMINOBENZAMIDE COMPOUNDS AS ANTHELMINTICS

The present invention relates to a new compound of formula (I) wherein the variables have the meaning as indicated in the claims; or an enantiomer or salt thereof. The compounds of formula (I) are useful in the control of parasites, in particular endopara

Pyrazolo[1,5-A]pyrimidines as antiviral agents

The invention provides compounds and pharmaceutically acceptable salts and esters and compositions thereof, for treating viral infections. The compounds and compositions are useful for treating Pneumovirinae virus infection including Human respiratory syncytial virus infections.

Discovery of an oral respiratory syncytial virus (RSV) fusion inhibitor (GS-5806) and clinical proof of concept in a human RSV challenge study

GS-5806 is a novel, orally bioavailable RSV fusion inhibitor discovered following a lead optimization campaign on a screening hit. The oral absorption properties were optimized by converting to the pyrazolo[1,5-a]-pyrimidine heterocycle, while potency, metabolic, and physicochemical properties were optimized by introducing the para-chloro and aminopyrrolidine groups. A mean EC50 = 0.43 nM was found toward a panel of 75 RSV A and B clinical isolates and dose-dependent antiviral efficacy in the cotton rat model of RSV infection. Oral bioavailability in preclinical species ranged from 46 to 100%, with evidence of efficient penetration into lung tissue. In healthy human volunteers experimentally infected with RSV, a potent antiviral effect was observed with a mean 4.2 log10 reduction in peak viral load and a significant reduction in disease severity compared to placebo. In conclusion, a potent, once daily, oral RSV fusion inhibitor with the potential to treat RSV infection in infants and adults is reported.

New compounds

The present invention relates to a new compound of formula wherein the variables have the meaning as indicated in the claims; or an enantiomer or salt thereof. The compounds of formula (I) are useful in the control of parasites, in particular endoparasite

Discovery and characterization of novel allosteric FAK inhibitors

Focal adhesion kinase (FAK) regulates cell survival and proliferation pathways. Here we report the discovery of a highly selective series of 1,5-dihydropyrazolo[4,3-c][2,1]benzothiazines that demonstrate a novel mode of allosteric inhibition of FAK. These compounds showed slow dissociation from unphosphorylated FAK and were noncompetitive with ATP after long preincubation. Co-crystal structural analysis revealed that the compounds target a novel allosteric site within the C-lobe of the kinase domain, which induces disruption of ATP pocket formation leading to the inhibition of kinase activity. The potency of allosteric inhibition was reduced by phosphorylation of FAK. Coupled SAR analysis revealed that N-substitution of the fused pyrazole is critical to achieve allosteric binding and high selectivity among kinases.

TRICYCLIC INHIBITORS OF KINASES USEFUL FOR THE TREATMENT OF PROLIFERATIVE DISEASES

The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein R1, R2, R3, A, B, and n are defined in the description. The present invention relates also to compositions containing sa

Structure-based discovery of cellular-active allosteric inhibitors of FAK

In order to develop potent and selective focal adhesion kinase (FAK) inhibitors, synthetic studies on pyrazolo[4,3-c][2,1]benzothiazines targeted for the FAK allosteric site were carried out. Based on the X-ray structural analysis of the co-crystal of the lead compound, 8-(4-ethylphenyl)-5-methyl-1,5- dihydropyrazolo[4,3-c][2,1]benzothiazine 4,4-dioxide 1 with FAK, we designed and prepared 1,5-dimethyl-1,5-dihydropyrazolo[4,3-c][2,1]benzothiazin derivatives which selectively inhibited kinase activity of FAK without affecting seven other kinases. The optimized compound, N-(4-tert-butylbenzyl)-1,5-dimethyl-1,5- dihydropyrazolo[4,3-c][2,1]benzothiazin-8-amine 4,4-dioxide 30 possessed significant FAK kinase inhibitory activities both in cell-free (IC50 = 0.64 μM) and in cellular assays (IC50 = 7.1 μM). These results clearly demonstrated a potential of FAK allosteric inhibitors as antitumor agents.

PYRAZOLO[1,5-A]PYRIMIDINES AS ANTIVIRAL AGENTS

The invention provides compounds and pharmaceutically acceptable salts and esters and compositions thereof, for treating viral infections. The compounds and compositions are useful for treating Pneumovirinae virus infection including Human respiratory syncytial virus infections.

PYRAZOLO [1, 5 -A] PYRIMIDINES AS ANTIVIRAL AGENTS

The invention provides compounds of Formula I or Formula II: (I), (II) or a pharmaceutically acceptable salt or ester, thereof, as described herein. The compounds and compositions thereof are useful for treating Pneumovirinae virus infections. The compounds, compositions, and methods provided are particularly useful for the treatment of Human respiratory syncytial virus infections.