861905-19-3

Upstream product

• 1765-93-1 4-fluoroboronic acid 
• 53857-57-1 5-bromo-1H-indazole 
• 352-34-1 4-fluoro-1-iodobenzene 
• 1032650-26-2 N-[1-(5-bromo-2-fluorophenyl)meth-(E)-ylidene]-N'-(4-fluorophenyl)hydrazine 
• 1227795-68-7 5-bromo-2-fluorobenzaldehyde (4-fluorophenyl)hydrazone 

Downstream Products

• 917491-75-9 2,2,2-trifluoro-1-[1-(4-fluorophenyl)-1H-indazol-5-yl]-1-(1H-indol-3-yl)ethanol 
• 1032648-54-6 1-(5-chlorothiophen-2-yl)-2,2,2-trifluoro-1-[1-(4-fluorophenyl)-1H-indazol-5-yl]ethanol 
• 1032648-07-9 1-(7-chloro-1H-pyrrolo[2,3-c]pyridin-3-yl)-2,2,2-trifluoro-1-[1-(4-fluorophenyl)-1H-indazol-5-yl]ethanol 
• 1032648-80-8 1-(1-allyl-6-bromo-1H-indol-3-yl)-2,2,2-trifluoro-1-[1-(4-fluorophenyl)-1H-indazol-5-yl]ethanol 
• 1032649-10-7 1-allyl-4-{2,2,2-trifluoro-1-[1-(4-fluorophenyl)-1H-indazol-5-yl]-1-hydroxyethyl}-1H-pyrrole-2-carboxylic acid ethyl ester 
• 1032649-13-0 1-allyl-4-{2,2,2-trifluoro-1-[1-(4-fluorophenyl)-1H-indazol-5-yl]-1-hydroxyethyl}-1H-pyrrole-2-carbonitrile 
• 1032648-93-3 5-allyl-3-methyl-7-{2,2,2-trifluoro-1-[1-(4-fluorophenyl)-1H-indazol-5-yl]-1-hydroxyethyl}-3,5-dihydropyrrolo[3,2-d]pyrimidin-4-one 
• 1032648-13-7 3-{2,2,2-trifluoro-1-[1-(4-fluorophenyl)-1H-indazol-5-yl]-1-hydroxyethyl}pyrrolo[2,3-b]pyridine-1-sulfonic acid dimethylamide 
• 1032648-15-9 2,2,2-trifluoro-1-[1-(4-fluorophenyl)-1H-indazol-5-yl]-1-(1H-pyrrolo[2,3-b]pyridin-3-yl)ethanol 
• 1035342-80-3 tert-butyl N-[(E,2S)-4-[1-(4-fluorophenyl)indazol-5-yl]but-3-en-2-yl]carbamate 
• 1035342-23-4 N-[(2S)-1-[[1-(4-fluorophenyl)indazol-5-yl]amino]propan-2-yl]-2,4,6-trimethyl-benzenesulfonamide 
• 917494-83-8 1-(4-fluorophenyl)-1H-indazole-5-carbaldehyde 
• 1229095-98-0 4-[1-(4-fluorophenyl)-1H-indazol-5-yl]-3-(trifluoromethyl)-phenol 
• 1229095-95-7 4-[1-(4-fluorophenyl)-1H-indazol-5-yl]phenol 

Relevant academic research and scientific papers

Catalytic Enantioselective Arylboration of Alkenylarenes

A method for the catalytic enantioselective arylboration of alkenylarenes is disclosed. The reaction leads to the formation of 1,1-diarylalkanes that also incorporate an additional pinacol boronic ester which can be easily transformed to a variety of groups. The products are formed with excellent diastereoselectivities and enantioselectivities.

GLUCOSYLCERAMIDE SYNTHASE INHIBITORS FOR THE TREATMENT OF DISEASES

Described herein are compounds of Formula I, methods of making such compounds, pharmaceutical compositions and medicaments containing such compounds, and methods of using such compounds to treat or prevent diseases or conditions associated with the enzyme glucosylceramide synthase (GCS).

Structure guided design of 5-arylindazole glucocorticoid receptor agonists and antagonists

Glucocorticoid receptor (GR) agonists have been used for more than half a century as the most effective treatment of acute and chronic inflammatory conditions despite serious side effects that accompany their extended use that include glucose intolerance, muscle wasting, skin thinning, and osteoporosis. As a starting point for the identification of GR ligands with an improved therapeutic index, we wished to discover selective nonsteroidal GR agonists and antagonists with simplified structure compared to known GR ligands to serve as starting points for the optimization of dissociated GR modulators. To do so, we selected multiple chemical series by structure guided docking studies and evaluated GR agonist activity. From these efforts we identified 5-arylindazole compounds that showed moderate binding to the glucocorticoid receptor (GR) with clear opportunities for further development. Structure guided optimization was used to design arrays that led to potent GR agonists and antagonists. Several in vitro and in vivo experiments were utilized to demonstrate that GR agonist 23a (GSK9027) had a profile similar to that of a classical steroidal GR agonist.

5-Functionalized indazoles as glucocorticoid receptor agonists

An indazole based series of glucocorticoid receptor agonists is reported. The SAR exploration of this scaffold yielded compounds with nanomolar affinity for the glucocorticoid receptor with indications of selectivity for the preferred transrepression mech

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)

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

Compounds of Formula (IA) (IA), and Formula (IB) (IB), wherein R1, R2, R3, A, B, C, D, E, G, X, Y, and Z 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.