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US 4,226,862 AGranted
Steroids and process for preparing the same
AssigneePierrel S.p.A.
InventorsMario Riva, Gaetano Palladino, Lucian Toscano
Life of this patent
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Abstract
Novel steroids are described together with processes of making them and pharmaceutical compositions containing them. The steroids have pharmaceutical activity, especially anti-inflammatory activity. They are all 2-Bromo-6.beta.-fluoro-pregna-1,4-diene-3,20-diones.
Claims41
Compounds having the formula:
- ##STR6## wherein X is Br, Cl or OQ;
- Y is Br, Cl, F or H;
- R.sub.1 is OQ or an alkyl orthoester;
- R.sub.2 is OQ;
- R.sub.3 is H, .alpha.OQ, .alpha.CH.sub.3 or .beta.CH.sub.3 ;
- and
- Q, which may be the same or different, is hydrogen or an acyl radical, or OQ in the 16, 17 or in the 17 and 21 positions may together form a cyclic ketal, cyclic acetal or cyclic alkyl orthoester;
- wherein at least one radical OQ is a carboxylic or an inorganic acid radical and pharmaceutically acceptable salts and esters thereof.
5 more elements
Compounds having the formula:
- ##STR7## wherein X is Br, Cl or OQ;
- Y is Br, Cl, F or H;
- R.sub.1 is OQ or an alkyl orthoester;
- R.sub.2 is OQ;
- R.sub.3 is H or .alpha.OQ;
- and
- Q which may be the same or different, is hydrogen or an acyl radical, or OQ in the 16, 17 or in the 17 and 21-positions may together form a cyclic ketal, cyclic acetal or cyclic alkyl orthoester;
- wherein at least one radical OQ is a carboxylic or an inorganic acid radical and pharmaceutically acceptable salts and esters thereof.
5 more elements
A process of making a compound of the formula:
- ##STR8## wherein R.sub.1 represents OQ or an orthoalkylester;
- R.sub.2 represents OQ;
- R.sub.3 represents H, .alpha.OQ, .alpha.CH.sub.3 or .alpha.CH.sub.3 ;
- and
- the radical Q, which may be the same or different, is H or acyl radicals, or the group OQ in the 16 and 17 positions or in the 17 and 21 positions may together form a cyclic ketal, cyclic acetal or cyclic alkyl orthoester, wherein at least one radical OQ is a carboxylic or an inorganic acid radical, which comprises reacting a compound of the formula:
- ##STR9## wherein R.sub.1 and R.sub.2 are as defined, and R.sub.3 is hydrogen, methyl or .alpha.OH;
- with a brominating agent to yield the 2.alpha.-brominated product.
4 more elements
A compound of the formula:
- ##STR10## wherein R.sub.1 is OH or Oacyl;
- R.sub.2 is OH, or Oacyl;
- R.sub.3 is H, CH.sub.3, .alpha. OH or .alpha. Oacyl, or R.sub.2 and R.sub.3 together may represent the group ##STR11## X is F, Cl or Br and Y is Cl or OH;
- or X and Y form 9, 11 epoxy or a 9, 11 double bond.
1 more element
Dependencies are inferred from the claim text.