16,17-acetalsubstituted androstane-17.beta.-carboxylic acid esters prossessing high binding affinity to the glucocorticosteroid receptor

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United States of America Patent

PATENT NO 4950659
SERIAL NO

06843771

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Abstract

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The invention refers to compounds having anti-inflamatory activity characterized by the formula ##STR1## or a stereoisomeric component thereof, in which formula the 1,2-position is saturated or is a double bond X.sub.1 is selected from hydrogen, fluorine, chlorine and bromine X.sub.2 is selected from hydrogen, fluorine, chlorine and bromine R.sub.1 is selected from hydrogen or a straight or branched hydrocarbon chain having 1-4 carbon atoms R.sub.2 is selected from hydrogen or straight and branched hydrocarbon chains having 1-10 carbon atoms and R.sub.3 is selected from ##STR2## is O or S R.sub.4 is selected from hydrogen, straight or branched hydrocarbon chains having 1-10 carbon atoms or from phenyl R.sub.5 is selected from hydrogen or methyl and R.sub.6 is selected from hydrogen, straight or branched, saturated or unsaturated hydrocarbon chains having 1-10 carbon atoms, an alkyl group substituted by at least one halogen atom, a heterocyclic ring system containing 3-10 atoms in the ring system, ##STR3## (m=0,1,2; n=2,3,4,5,6), phenyl or benzyl groups which are unsubstituted or substituted by one or more alkyl, nitro, carboxy, alkoxy, halogen, cyano, carbalkoxy or trifluoromethyl group(s), provided that when R.sub.2 is hydrogen R.sub.1 is methyl. The invention also refers to a process and intermediates for the prearation of these compunds, a pharmaceutical preparation containing one of the compunds 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

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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 Bjaarred, SE 5 19
Trofast, Jan W Lund, SE 6 144

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