androstane - 17 - beta - carbonsaeureester, procedures to their manufacture and pharmaceutical praeparate containing them.

摘要

The invention refers to compounds having anti-inflammatory activity characterized by the formula IMAGE or a stereoisomeric component thereof, in which formula X1 represents a hydrogen, chlorine, bromine or fluorine atom; X2 represents a hydrogen, chlorine, bromine or fluorine atom; R1 represents a beta -hydroxy group, a beta -chlorine atom or an oxo group; R2 represents a hydrogen atom, a methylene group or an alpha - or beta -methyl group; R3 represents a hydrogen atom or an acyl group of 1 through 8 carbon atoms; R4 represents a hydrogen atom, a (C1-C5) alkyl group or a phenyl group; R5 represents a hydrogen atom, a (C1-C5) alkyl group or a phenyl group; Y represents either CR7R8, O, S or NR9, where R7, R8 and R9 are selected from hydrogen or from straight or branched hydrocarbon chains having 1-8 carbon atoms or from a phenyl group. R6 represents a hydrogen; a methyl group; a phenyl or an alkenyl or cycloalkylene group optionally substituted by alkyl, nitro, carboxy, alkoxy, halogen, cyano, carbalkoxy and trifluoromethyl group(s); a (C1-C5) alkyl group substituted by at least one halogen atom; a saturated or unsaturated carbocyclic or heterocyclic (O, S, N) ring system containing 3-10 atoms in the ring system; a C1 alkyl group substituted by either one or two alicyclic or aromatic 3,4,5 or 6-numbered ring system(s) or one, two or three straight or branched alkyl or alkenyl group(s) of 1 through 18 carbon atoms; and represents a single or double bond. The invention also refers to a process and intermediates for the preparation of these compounds, a pharmaceutical preparation containing one of the compounds and a method for the treatment of inflammatory conditions.