Patent · US Expired

Androstane carbothioates

US4335121A · kind A · utility

128Cited by
4References
25Claims
0Family size

Assignee

Inventors

Key dates

Filing dateFeb 13, 1981
Grant dateJun 15, 1982
Priority date
Expiry dateFeb 13, 2001

Classification

  • Technology area (CPC C)Chemistry; Metallurgy
  • CPC primaryC07J71/0015
  • WIPO fieldOrganic fine chemistry
  • WIPO sectorChemistry

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.

Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.