- POTENT SOFT ANTI-INFLAMMATORY CORTICOSTEROID COMPOUNDS AND USES THEROF
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Potent soft corticosteroid pharmaceutical compositions comprising them and method for use as anti-inflammatory agents. Also, a method for softening fluticasone propionate and similar corticosteroids to arrive at potent but safer alternatives. The compound S-fluoromethyl 17α-dichloroacetoxy-6α,9α-difluoro-11β-hydroxy-16a- methyl-3-oxoandrosta-1,4-diene-17β-carbothioate, which is equally potent to but safer than fluticasone, is among those provided. Another compound of particular interest is 2-hydroxyethyl 17α-dichloroacetoxy-6α,9α-difluoro-11β-hydroxy-16β- methyl-3-oxoandrosta-1,4-diene-17β-carboxylate.
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Paragraph 0074; 0075; 0076
(2019/01/08)
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- Etiprednol dicloacetate, a new soft glucocorticoid drug candidate. Development of chemistry
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During development of chemistry of the soft drug candidate etiprednol dicloacetate (BNP-166) 1) optimization studies on the three-step chemical synthesis resulted in a process that could be scaled-up to the kg level, 2) the impurity profile was determined, 3) synthetic routes were developed for the preparation of the radiolabeled target compound, and 4) a series of hydroxylated metabolites was prepared.
- Csanadi,Horvath,Szekeres,Hasko,Ila,Ivanics,Patthy,Salat,Seres,Pallagi,Toth,Szederkenyi,Konya,Tegdes,Bodor,Zubovics, Zoltan
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p. 349 - 359
(2007/10/03)
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- ANDROSTENE DERIVATIVES
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The invention provides new androstene derivatives having anti-inflammatory activity, pharmaceutical compositions containing them, and methods of administering them to warm-blooded animals in the treatment of inflammation. The active compounds are alkyl 17 alpha -dichloroacetoxy-11 beta -hydroxyandrosta-1,4-dien-3-one-17 beta -carboxylates and related androstenes.
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- Androstene derivatives
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The invention provides new androstene derivatives having anti-inflammatory activity, pharmaceutical compositions containing them, and methods of administering them to warm-blooded animals in the treatment of inflammation. The active compounds are alkyl 17α-dichloroacetoxy-11β-hydroxyandrosta-1,4-dien-3-one-17β-carboxylates and related androstenes.
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