1028459-20-2

Upstream product

• 146137-76-0 2-Fluoro-5-iodo-benzaldehyde 
• 823-85-8 4-fluorophenyhydrazine hydrochloride 
• 113322-99-9 tert-butyl ((1R,2S)-1-hydroxy-1-phenylpropan-2-yl)carbamate 
• 108-86-1 bromobenzene 
• 492-41-1 (1R,2S)-norephedrine 
• 1025762-98-4 1-(4-fluorophenyl)-5-iodo-1H-indazole 

Downstream Products

• 1028458-64-1 N-[(1R,2S)-1-[1-(4-fluorophenyl)indazol-5-yl]oxy-1-phenyl-propan-2-yl]cyclopropanesulfonamide 
• 1028459-13-3 1-methylimidazole-4-sulfonic acid N-[(1R,2S)-1-[1-(4-fluorophenyl)indazol-5-yl]oxy-1-phenyl-propan-2-yl]amide 
• 1028459-14-4 3,5-dimethylisooxazole-4-sulfonic acid N-[(1R,2S)-1-[1-(4-fluorophenyl)indazol-5-yl]oxy-1-phenyl-propan-2-yl]amide 
• 1034147-99-3 N-((1S,2R)-2-{[1-(4-fluorophenyl)-1H-indazol-5-yl]oxy}-1-methyl-2-phenylethyl)cyclopropanecarboxamide 
• 1034149-16-0 l-{(1S,2R)-2-{[1-(4-fluorophenyl)-1H-indazole-5-yl]oxy}-1-methyl-2-phenylethyl}-3-(2-furylmethyl)thiourea 
• 1034149-08-0 1-(cyclopentyl)-3-{(1S,2R)-2-[1-(4-fluorophenyl)-1H-indazole-5-yloxy]-1-methyl-2-phenyl-ethyl}urea 
• 1034149-34-2 N-{(1R,2S)-1-[1-(4-fluorophenyl)indazol-5-yl]oxy-1-phenylpropan-2-yl}-5-methyl-[1,3,4]oxadiazol-2-carboxamide 
• 1034149-14-8 1-((R)-1,2-dimethylpropyl)-3-{(1S,2R)-2-[1-(4-fluorophenyl)-1H-indazole-5-yloxy]-1-methyl-2-phenylethyl}urea 
• 1034149-10-4 1-{(1S,2R)-2-{[1-(4-fluorophenyl)-1H-indazole-5-yl]oxy}-1-methyl-2-phenylethyl}-3-(2-furylmethyl)urea 
• 1034149-12-6 ethyl N-{[(1S,2R)-2-{[1-(4-fluorophenyl)-lH-indazole-5-yl]oxy}-1-methyl-2-phenylethyl]carbamoyl}glycinate 

Relevant academic research and scientific papers

Selective Nonsteroidal Glucocorticoid Receptor Modulators for the Inhaled Treatment of Pulmonary Diseases

A class of potent, nonsteroidal, selective indazole ether-based glucocorticoid receptor modulators (SGRMs) was developed for the inhaled treatment of respiratory diseases. Starting from an orally available compound with demonstrated anti-inflammatory activity in rat, a soft-drug strategy was implemented to ensure rapid elimination of drug candidates to minimize systemic GR activation. The first clinical candidate 1b (AZD5423) displayed a potent inhibition of lung edema in a rat model of allergic airway inflammation following dry powder inhalation combined with a moderate systemic GR-effect, assessed as thymic involution. Further optimization of inhaled drug properties provided a second, equally potent, candidate, 15m (AZD7594), that demonstrated an improved therapeutic ratio over the benchmark inhaled corticosteroid 3 (fluticasone propionate) and prolonged the inhibition of lung edema, indicating potential for once-daily treatment.

INDAZOLYL ESTER AND AMIDE DERIVATIVES FOR THE TREATMENT OF GLUCOCORTICOID RECEPTOR MEDIATED DISORDERS

Compounds of formula (I): The present invention relates to novel indazolyl ester or amide derivatives, to pharmaceutical compositions comprising such derivatives, to processes for preparing such novel derivatives and to the use of such derivatives as medicaments

INDOZALYL SULPHONAMIDE DERIVATIVES USEFUL AS GLUCOCORTICOID MODULATORS

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).