Patent References 3636010 3828080 Pharmaceutical compositions of 6,9-difluoro-androst-4-ene-17ଲ-carboxylates and derivatives thereof Thioetianic acid derivatives Patent #: 4188385 InventorsAssigneeApplicationNo. 06/234113 filed on 02/13/1981US Classes:514/180, 9-position substituted514/179, Modified C-ring (except methyl in 13-position) (e.g., double bond containing, substituted, etc.)514/181, 21-position substituted552/528, The carbon is double bonded directly at the 16-position552/610Acyclic carbon bonded directly at the 17 beta-position of the cyclopentanohydrophenanthrene ring system (e.g., etiocholanic acids, 17 cyanoetiocholanes, 17-aldehydrostanes, etc.)ExaminersPrimary: Roberts, Elbert L.Attorney, Agent or FirmInternational ClassesC07J 41/00 (20060101)C07J 31/00 (20060101) C07J 71/00 (20060101) C07J 3/00 (20060101) Foreign Application Priority Data1980-02-15 GBAbstractCompounds of the formula ##STR1## wherein R1 represents a fluoro-, chloro- or bromo-methyl group or a 2'-fluoroethyl group, R2 represents a group COR6 where R6 is a C1-3 alkyl group or OR2 and R3 together form a 16,17-isopropylidenedioxy group; R3 represents a hydrogen atom, a methyl group (which may be in either the - or ଲ-configuration) or a methylene group; R4 represents a hydrogen, chlorine or fluorine atom; R5 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-halo-11ଲ-hydroxy grouping.Pharmaceutical compositions containing the compounds of formula I and methods for the use of the compounds are described and claimed. |
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