Androstane carbothioates

Details Androstane carbothioates Androstane carbothioates

1981-02-13

1982-06-15

Roberts, Elbert L.

Drug, bio-affecting and body treating compositions

Antigen, epitope, or other immunospecific immunoeffector

Bacterium or component thereof or substance produced by said...

2603971, C07J 700, A61K 3156

Patent

active

043351212

ABSTRACT:
Compounds of the formula ##STR1## wherein R.sup.1 represents a fluoro-, chloro- or bromo-methyl group or a 2'-fluoroethyl group, R.sup.2 represents a group COR.sup.6 where R.sup.6 is a C.sub.1-3 alkyl group or OR.sup.2 and R.sup.3 together form a 16.alpha.,17.alpha.-isopropylidenedioxy group; R.sup.3 represents a hydrogen atom, a methyl group (which may be in either the .alpha.- or .beta.-configuration) or a methylene group; R.sup.4 represents a hydrogen, chlorine or fluorine atom; R.sup.5 represents a hydrogen or fluorine atom and symbol represents a single or double bond have good anti-inflammatory activity, particularly on topical applications.
The compounds of formula I are prepared by esterification, halogenation, reduction, deprotection and reaction at a 9,11-double bond to form a 9.alpha.-halo-11.beta.-hydroxy grouping.
Pharmaceutical compositions containing the compounds of formula I and methods for the use of the compounds are described and claimed.

REFERENCES:
patent: 3636010 (1972-01-01), Basel et al.
patent: 3828080 (1974-08-01), Phillipps et al.
patent: 4093721 (1978-06-01), Phillipps et al.
patent: 4188385 (1980-02-01), Edwards

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