Topical and systemic antiinflammatory steroid cpds. - are 21-salicylate or acetyl-salicylate ester cpds. of hydroxy-pregnane cpds

Topical and systemic antiinflammatory steroid cpds. - are 21-salicylate or acetyl-salicylate ester cpds. of hydroxy-pregnane cpds

Steroid salicylates of formula (I) are new. In (I), R is H or acetyl. X is H, F or Cl. Y is OH, O, Cl or F. X1 is H, halo or CH3. Z is H, OH, alpha- or beta-methyl or a gp. (II). They are prepd. from the 21-hydroxy cpd. by reacting with a suitable deriv. of acetylsalicylic acid, then opt. hydrolysis...

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Bibliographische Detailangaben
Hauptverfasser: CASTELLI,PIERPAOLO, L.G. MELI,ALBERT, PALLADINO,GAETANO, DA COL,MARCO
Format: Patent
Sprache:eng ; ger
Schlagworte:
CHEMISTRY
METALLURGY
ORGANIC CHEMISTRY
STEROIDS
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Zusammenfassung:Steroid salicylates of formula (I) are new. In (I), R is H or acetyl. X is H, F or Cl. Y is OH, O, Cl or F. X1 is H, halo or CH3. Z is H, OH, alpha- or beta-methyl or a gp. (II). They are prepd. from the 21-hydroxy cpd. by reacting with a suitable deriv. of acetylsalicylic acid, then opt. hydrolysis to convert R is acetyl to H. In an example 9 alpha-fluoro-prednisolone-21-acetylsalicylate was prepd. by reacting 9 alpha-fluoro-prednisolone with acetylsalicyloyl chloride. Cpds. are useful in human and veterinary medicine for treating e.g. conjunctivitis, dermatitis, eczema, allergies rheumatoid arthritis etc.