897380-82-4

Upstream product

• 897380-80-2 3,3,3-trifluoro-2-(2,4,6-trimethylbenzenesulfonylamino)propionic acid ethyl ester 
• 773-64-8 2-mesitylenesulphonyl chloride 
• 897380-81-3 2,4,6-trimethyl-N-(2,2,2-trifluoro-1-hydroxymethylethyl)benzenesulfonamide 
• 934986-94-4 2,2,2-trifluoro-1-{[(2,4,6-trimethylbenzenesulfonyl)amino]methyl}ethyl 2,4,6-trimethylbenzenesulfonate 

Downstream Products

• 1070749-82-4 2,4,6-trimethyl-N-(2,2,2-trifluoro-1-phenoxymethylethyl)-benzenesulfonamide 
• 1070749-80-2 2,4,6-trimethyl-N-(2,2,2-trifluoro-1-phenylsulfanylmethylethyl)benzene-sulfonamide 
• 1070749-90-4 2,4,6-trimethyl-N-(2,2,2-trifluoro-1-phenylaminomethylethyl)benzene-sulfonamide 
• 1070341-50-2 2,4,6-trimethyl-N-[2,2,2-trifluoro-1-(quinolin-4-yloxymethyl)ethyl]benzenesulfonamide 
• 1070341-30-8 2,4,6-trimethyl-N-[2,2,2-trifluoro-1-(quinolin-5-ylaminomethyl)ethyl]benzenesulfonamide 

Relevant academic research and scientific papers

The discovery of potent and selective non-steroidal glucocorticoid receptor modulators, suitable for inhalation

We report the discovery of highly potent and selective non-steroidal glucocorticoid receptor modulators with PK properties suitable for inhalation. A high throughput screen of the AstraZeneca compound collection identified sulfonamide 3 as a potent non-steroidal glucocorticoid receptor ligand. Further optimization of this lead generated indazoles 30 and 48 that were progressed to characterization in in vivo models. X-ray crystallography was used to gain further insight into the binding mode of selected ligands.

GLUCOCORTICOID MIMETICS, METHODS OF MAKING THEM, PHARMACEUTICAL COMPOSITIONS, AND USES THEREOF

Compounds of Formula (I) wherein R1, R2, R3, R4, R5, R6, X, R7, and R8 are as defined herein, or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.

NOVEL BICYCLIC SULFONAMIDES FOR USE AS GLUCOCORTICOID RECEPTOR MODULATORS IN THE TREATMENT OF INFLAMMATORY DISEASES

Compounds of formula (I): or a pharmaceutically acceptable salt thereof; compositions comprising them, processes for preparing them and their use in medical therapy (for example modulating the glucocorticoid receptor in a warm blooded animal).