Androstane-17 beta-carboxylic acid esters

C - Chemistry – Metallurgy – 07 – J

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167/194, 260/81,

C07J 1/00 (2006.01) C07J 3/00 (2006.01) C07J 31/00 (2006.01) C07J 41/00 (2006.01) C07J 43/00 (2006.01)

Patent

CA 1278293

Abstract The invention refers to compounds havins anti-inflammatory activity characterized by the formula Image or a stereoisomer thereof, in which formula X1 represents a hydrogen, chlorine, bromine or fluorine atom; X2 represents a hydrogen, chlorine, bromine or fluorine atom; R1 represents .alpha. .beta.-hydroxy group, .alpha. .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 atom, a methyl group; a phenyl or an alkenyl or cycloalkenyl group option- ally substituted by alkyl, nitro, carboxy, alkoxy, halogen, cyano, carbalkoxy or trifluoromethyl group(s); a (C1-C5) alkyl group substituted by at least one halogen atom; a saturated or unsatur- ated 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-membered ring system(s) or one, two or three straight or branch- ed, saturated or unsaturated hydrocarbon chains having 1 through 18 carbon atoms; and Image represents a single or double bond. The invention also refers to a process and intermediates for the preparation of these compounds, a pharmaceutical preparation con- taining one of the compounds and a method for the treatment of inflammatory conditions.

505743

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