Substituted tetrahydrobenzopyrrolylfuranoic acid derivatives as

Details Substituted tetrahydrobenzopyrrolylfuranoic acid derivatives as Substituted tetrahydrobenzopyrrolylfuranoic acid derivatives as

1994-04-19

1995-09-19

Gerstl, Robert

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

548448, 548449, A61K 3140, C07D40706, C07D40712, C07D40702

Patent

active

054516005

ABSTRACT:
Compounds of the formula ##STR1## wherein R is hydrogen, alkyl.sub.1-8, geminal alkyl.sub.1-3, unsubstituted or substituted aryl; X is alkylene, --CR.sub.1 .dbd.CR.sub.2 -- (E and/or Z), carbonyl, oxygen or sulfur, wherein one of R.sub.1 and R.sub.2 is alkyl.sub.1-3 and the other is hydrogen; Y is unsubstituted alkyl.sub.1-12 or substituted by one or more alkyl.sub.1-3 groups, or unsubstituted or substituted phenylalkyl .sub.1-3 ; or a salt thereof with a pharmaceutically acceptable base, are described.
The compound of formula I are potent inhibitors of phospholipase A.sub.2 (PLA.sub.2) and are therefore useful in the treatment of inflammatory diseases, such as, psoriasis, inflammatory bowel disease, asthma, allergy, arthritis, dermatitis, gout, pulmonary, myocardial ischemia and trauma induced inflammation, such as, spinal cord injury.

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