Soft steroids having anti-inflammatory activity

A compound selected from the group consisting of:

• (a) a compound of the formula ##STR243## wherein:
• R.sub.1 is C.sub.1 -C.sub.10 alkyl;
• C.sub.2 -C.sub.10 (monohydroxy or polyhydroxy)alkyl;
• C.sub.1 -C.sub.10 (monohalo or polyhalo)alkyl;
• or --CH.sub.2 COOR.sub.6 wherein R.sub.6 is unsubstituted or substituted C.sub.1 -C.sub.10 alkyl;
• C.sub.3 -C.sub.8 cycloalkyl, C.sub.3 -C.sub.8 cycloalkenyl or C.sub.2 -C.sub.10 alkenyl, the substituents being selected from the group consisting of halo, lower alkoxy, lower alkylthio, lower alkylsulfinyl, lower alkylsulfonyl, ##STR244## or R.sub.6 is unsubstituted or substituted phenyl or benzyl, the substituents being selected from the group consisting of lower alkyl, lower alkoxy, halo, carabamoyl, lower alkoxycarbonyl, lower alkanoyloxy, lower haloalkyl, mono(lower alkyl)amino, di(lower alkyl)amino, mono(lower alkyl)carbamoyl, di(lower alkyl)carbamoyl, lower alkylthio, lower alkylsulfinyl and lower alkylsulfonyl;
• or R.sub.1 is --CH.sub.2 CONR.sub.7 R.sub.8 wherein R.sub.7 and R.sub.8, which can be the same or different, are each hydrogen, lower alkyl, C.sub.3 -C.sub.8 cycloalkyl, phenyl or benzyl, or R.sub.7 and R.sub.8 are combined such that --NR.sub.7 R.sub.8 represents the residue of a saturated monocyclic secondary amine;
• or R.sub.1 is unsubstituted or substituted phenyl or benzyl, the substituents being selected from the group of phenyl and benzyl substituents defined hereinabove with respect to R.sub.6 ;
• or R.sub.1 is ##STR245## wherein Y is --S--, --SO--, --SO.sub.2 -- or --O-- and R.sub.9 is hydrogen, lower alkyl or phenyl, or R.sub.9 and the lower alkyl group adjacent to Y are combined so that R.sub.1 is a cyclic system of the type ##STR246## wherein Y is defined as above and the alkylene group contains 3 to 10 carbon atoms, of which at least 3 and no more than 6 are ring atoms;
• or R.sub.1 is ##STR247## wherein R.sub.6 is defined as hereinabove and R.sub.10 is hydrogen, lower alkyl, phenyl or halophenyl;
• R.sub.2 is unsubstituted or substituted C.sub.1 -C.sub.10 alkyl, C.sub.3 -C.sub.8 cycloalkyl, C.sub.3 -C.sub.8 cycloalkenyl or C.sub.2 -C.sub.10 alkenyl, the substituents being selected from the group consisting of halo, lower alkoxy, lower alkylthio, lower alkylsulfinyl, lower alkylsulfonyl, ##STR248## or R.sub.2 is unsubstituted or substituted phenyl or benzyl, the substituents being selected from the group consisting of lower alkyl, lower alkoxy, halo, carbamoyl, lower alkoxycarbonyl, lower alkanoyloxy, lower haloalkyl, mono(lower alkyl)amino, di(lower alkyl)amino, mono(lower alkyl)carbamoyl, di(lower alkyl)carbamoyl, lower alkylthio, lower alkylsulfinyl and lower alkylsulfonyl;
• R.sub.3 is hydrogen, .alpha.-hydroxy, .beta.-hydroxy, .alpha.-methyl, .beta.-methyl, .dbd.CH.sub.2, or .alpha.- or ##STR249## wherein R.sub.2 is identical to R.sub.2 as defined hereinabove;
• R.sub.4 is hydrogen, fluoro or chloro;
• R.sub.5 is hydrogen, fluoro, chloro or methyl;
• X is --O-- or --S--;
• and the dotted line in ring A indicates that the 1,2 linkage is saturated or unsaturated;
• (b) a quaternary ammonium salt of a compound of formula (I) wherein at least one of R.sub.1 and R.sub.2 is a halo-substituted alkyl group;
• (c) a compound of the formula ##STR250## wherein R.sub.2, R.sub.4, R.sub.5, and the dotted line in ring A are as defined in (a) above, Z is carbonyl or .beta.-hydroxymethylene and R.sub.3 " is hydrogen, .alpha.-methyl, .beta.-methyl, .dbd.CH.sub.2 or .alpha.- or ##STR251## wherein R.sub.2 is identical to R.sub.2 above;
• (d) a compound of the formula ##STR252## wherein M is alkali metal, thallium, alkaline earth metal/2 or NH.sub.4 and R.sub.2, R.sub.3 ", R.sub.4, R.sub.5, Z and the dotted line in ring A are as defined in (a) and (c) above;
• (e) a compound of the formula ##STR253## wherein R.sub.3 "' is hydrogen, .alpha.-methyl, .beta.-methyl, .alpha.-OCOCl or .beta.-OCOCl, and R.sub.1, R.sub.4, R.sub.5, Z and the dotted line in ring A are as defined in (a) and (c) above;
• (f) a compound of the formula ##STR254## wherein R.sub.2, R.sub.3 ", R.sub.4, R.sub.5, Z and the dotted line in ring A are as defined in (a) and (c) above;
• and
• (g) a compound of the formula ##STR255## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, X and the dotted line in ring A are as defined in (a) above.