Substituted-4-thiazolidinone derivatives

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

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Details

514886, 514887, 548182, 548186, 548187, 548188, 548200, 548201, A61K 31425, C07D27704

Patent

active

050617206

ABSTRACT:
Disclosed are novel substituted 4-thiazolidinone derivatives having cyclooxygenase and 5-lipoxygenase inhibiting properties and which are topical antiinflammatory agents for inflammed conditions of the skin having the formula: ##STR1## wherein R is hydrogen or loweralkyl; R.sup.1 is loweralkyl or aryl; X is --(CH.sub.2)-aryl, --O--(CH.sub.2).sub.0-3 -aryl, --C(O)(CH.sub.2).sub.0-3 -aryl, --CH(OH)--(CH.sub.2).sub.0-3 -aryl or 3,4 ##STR2## (to form naphthyl ring); aryl is phenyl, substituted phenyl, or 2,3 or 4 pyridyl; W is oxygen; Q is -(alk.sup.1).sub.0-1 --(O).sub.0-1 --(B).sub.0-1 --(alk.sup.2).sub.0-1 --[C(O)Z].sub.0-1 ; B is ##STR3## Z is OR.sup.3 or NR.sup.4 R.sup.5 where R.sup.3 is hydrogen, loweralkyl, or a pharmaceutically acceptable metal cation, R.sup.4 and R.sup.5 are hydrogen or loweralkyl; alk.sup.1 and alk.sup.2 are lower alkylene or loweralkyleneloweralkyl, Y is hydrogen, loweralkyl, loweralkoxy, trifluoromethyl, nitro, or halo; and the stereoisomers and optical isomers thereof and pharmaceutically acceptable acid addition salts which form when a basic nitrogen is present.

REFERENCES:
patent: 2520178 (1950-08-01), Surrey
patent: 2623048 (1952-12-01), Long
patent: 3006919 (1961-10-01), Gaul et al.
patent: 4664694 (1987-05-01), Brouwer et al.

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