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Patent / Jan 01, 1983

Steroidal esters

  • Philip Page
EP 72200

Corticosteroid esters I and II (R = H, F, Cl; R1 = H, F, Cl, Me; R2 = halo, HO, oxo; R3 = H, Me; R4 = acyl; R5 = HO, H, halo, acyloxy) were prepd. as topical inflammation inhibitors and as agents in the treatment of psoriasis, eczema, neurodermatitis, seborrhea, contact dermatitis, and atopic dermatitis. Thus, 9.alpha.-fluoro-17-hydroxy-16.beta.-methyl- 11.beta.-(trifluoroacetoxy)pregna-1,4-diene-3,20-dione and 4-MeC6H4SO3H were added to a mixt. of [Me(CH2)5CO]2O and Cl3CCO2H at and reacted for 4 h at and then treated with 50% aq. Me2CHNH2 to give 21-deoxybetamethasone 17-heptanoate [II; R1 = R5 = H; R = F; R2 = HO; R3 = .beta.-Me; R4 = heptanoyl]. In the Mckenzie vasoconstriction test in humans, beclomethasone 17,21-diacetate possessed topical inflammation inhibiting activity equal to that of betamethasone 17-valerate and dexamethasone 17,21-dipropionate.