885266-19-3

Upstream product

• 773-64-8 2-mesitylenesulphonyl chloride 
• 2749-11-3 (S)-Alaninol 

Downstream Products

• 1609651-41-3 C₂₁H₂₅N₃O₂S 
• 1609651-40-2 C₂₁H₂₅N₃O₂S 
• 1609651-39-9 C₂₀H₂₇NO₃S 
• 1160376-85-1 N-cyclopropyl-4-{6-methyl-4-[((2S)-2-{[(2,4,6-trimethylphenyl)sulfonyl]amino}propyl)amino]-1H-indazol-1-yl}benzamide 
• 1274686-87-1 C₃₀H₃₇N₅O₃S 
• 1274686-86-0 C₂₈H₃₃N₅O₃S 
• 1274686-84-8 C₂₇H₃₂N₄O₃S 

Relevant academic research and scientific papers

Discovery of indazole ethers as novel, potent, non-steroidal glucocorticoid receptor modulators

A structure-based design approach led to the identification of a novel class of indazole ether based, non-steroidal glucocorticoid receptor (GR) modulators. Several examples were identified that displayed cell potency in the picomolar range, inhibiting LPS-induced TNF-α release by primary peripheral blood mononuclear cells (PBMCs). Additionally, an improved steroid hormone receptor binding selectivity profile, compared to classical steroidal GR agonists, was demonstrated. The indazole ether core tolerated a broad range of substituents allowing for modulation of the physiochemical parameters. A small sub-set of indazole ethers, with pharmacokinetic properties suitable for oral administration, was investigated in a rat antigen-induced joint inflammation model and demonstrated excellent anti-inflammatory efficacy.

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.

Discovery of a potent series of non-steroidal non α-trifluoromethyl carbinol glucocorticoid receptor agonists with reduced lipophilicity

A novel series of indazole non-steroidal glucocorticoid receptor agonist has been discovered. This series features a sulfonamide central core and meta amides which interact with the extended ligand binding domain. This series has produced some of the most potent and least lipophilic agonists of which we are aware such as 20a (NFκB pIC50 8.3 (100%), c log P 1.9). Certain analogues in this series also display evidence for modulated pharmacology.

N- (2 { [1-PHENYL-1H-INDAZ0L-4-YL] AMINO} PROPYL) -SULFONAMIDE DERIVATIVES AS NON-STEROIDAL GLUCOCORTICOID RECEPTOR LIGANDS FOR THE TREATMENT OF INFLAMMATIONS

The present invention provides compounds of formula (I): a process for their preparation, to pharmaceutical compositions comprising the compounds and the preparation of said compositions, to intermediates, and to use of the compounds for the manufacture o

INDAZOLYL SULPHONAMIDE DERIVATIVES FOR THE TREATMENT OF GLUCOCORTICOID RECEPTOR MEDIATED DISORDERS

Compounds of formula (I): [Chemical formula should be inserted here. Please see paper copy] 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)

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).

NOVEL SULPHONAMIDE DERIVATIVES AS GLUCOCORTICOID RECEPTOR MODULATORS FOR 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).