Non-steroidal glucocorticoid agonists

Abstract

New highly-selective glucocorticoid receptor agonists that are 3-bicyclyl-2-hydroxy-N-4-methyl-1-oxobenzoxazin-6-yl 2-trifluoromethylpropanamide derivatives are claimed. These compounds display reduced activity as trans-activators whilst retaining high affinity for the glucocorticoid receptor and good potency as transrepressors. They should thus produce fewer side effects than currently marketed corticosteroids and are claimed to provide methods of treating eczema, psoriasis, allergic dermatitis, neurodermatitis, pruritis and hypersensitivity reactions.

• 685698
• 799943
• β-adrenoceptor
• β₂-agonist
• asthma
• chronic obstructive pulmonary disease (COPD)
• corticosteroid
• glucocorticoid receptor