Novel androstane-17.beta.-carboxylic acid esters

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United States of America Patent

PATENT NO 4804656
SERIAL NO

06847933

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ATTORNEY / AGENT: (SPONSORED)

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Abstract

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The invention refers to compounds having anti-inflammatory activity characterized by the formula ##STR1## or a stereoisomeric component thereof, in which formula X.sub.1 represents a hydrogen, chlorine, bromine or fluorine atom; X.sub.2 represents a hydrogen, chlorine, bromine or fluorine atom; R.sub.1 represents a .beta.-hydroxy group, a .beta.-chlorine atom or an oxo group; R.sub.2 represents a hydrogen atom, a methylene group or an .alpha.- or .beta.-methyl group; R.sub.3 represents a hydrogen atom or an acyl group of 1 through 8 carbon atoms; R.sub.4 represents a hydrogen atom, a (C.sub.1 -C.sub.5) alkyl group or a phenyl group; R.sub.5 represents a hydrogen atom, a (C.sub.1 -C.sub.5) alkyl group or a phenyl group; Y represents either CR.sub.7 R.sub.8, O, S or NR.sub.9, where R.sub.7, R.sub.8 and R.sub.9 are selected from hydrogen or from straight or branched hydrocarbon chains having 1-8 carbon atoms or from a phenyl group. R.sub.6 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 (C.sub.1 -C.sub.5) 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 C.sub.1 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.

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Patent Owner(s)

Patent OwnerAddress
AKTIEBOLAGET DRACOSWEDEN'S LUND MAILBOX NO 34 LUND SKANE

International Classification(s)

Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Andersson, Paul H Sodra Sandby, SE 3 5
Andersson, Per T Lund, SE 3 5
Axelsson, Bengt I Genarp, SE 4 104
Thalen, Bror A Bjarred, SE 5 19
Trofast, Jan W Lund, SE 6 144

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