Condensed heterocyclic compounds and pharmaceutical use thereof

Details Condensed heterocyclic compounds and pharmaceutical use thereof Condensed heterocyclic compounds and pharmaceutical use thereof

1992-08-18

1994-04-05

Raymond, Richard L.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

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

5142282, 5142335, 514255, 514456, 514469, 544 587, 544 62, 544147, 544151, 544153, 544376, 549355, 549398, 549404, 549405, 549408, 549409, 549462, A61K 3134, A61K 3135, C07D30780, C07D31158

Patent

active

053005228

ABSTRACT:
The invention relates to compounds of the formula ##STR1## wherein R.sup.1 is hydrogen. acyl, lower-alkyl or --CHO, --CH.sub.2 OR.sup.10, --COR.sup.7 or OR.sup.13 ; R.sup.2, R.sup.3 and R.sup.4 are, independently, hydrogen, lower-alkyl, lower-alkoxy or halogen; R.sup.5 and R.sup.5 are, independently, hydrogen or lower-alkyl; R.sup.7 is hydroxy, lower-alkoxy or NR.sup.8 R.sup.9 ; R.sup.8 and R.sup.9 are, independently, hydrogen or lower-alkyl; X and Y are, independently, >CR.sup.14 R.sup.15, --O--, --S--, >SO, >SO.sub.2 or >NR.sup.18 ; R.sup.10 and R.sup.18 are, independently, hydrogen, lower-alkyl or acyl; M is --C(R.sup.11).dbd.C(R.sup.12)--, --CONH-- or --NH--CO--; R.sup.11, R.sup.12, R.sup.14 and R.sup.15 are, independently, hydrogen or lower-alkyl, R.sup.13 is hydrogen, lower-alkoxycarbonyl or lower- alkyl, which can be substituted by amino, mono-alkylamino, di-alkylamino, morpholino, thiomorpholino or piperazino; and n is 1, 2, 3 or 4; with the proviso that at least one of X and Y comprises a hetero atom and that n is 1, 3 or 4 when X contains a hetero atom, Y is >C(CH.sub.3).sub.2 and R.sup.1 is lower-alkyl or --CH.sub.2 OR.sup.10 or --COR.sup.7, or a salt of a compound of formula I, when R.sup.1 is carboxy.
The compounds of formula I are useful in the treatment and prophylaxis of neoplasms, dermatoses and ageing of the skin.

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