Organic compounds -- part of the class 532-570 series – Organic compounds – Four or more ring nitrogens in the bicyclo ring system
Patent
1993-12-23
1995-05-30
Raymond, Richard L.
Organic compounds -- part of the class 532-570 series
Organic compounds
Four or more ring nitrogens in the bicyclo ring system
544 587, 544377, 549350, 549365, 549434, 549436, 549437, 549438, 549439, 549440, 549443, 549444, 549445, 549446, 549447, C07D41312, C07D31758, C07D31760, C07D31918
Patent
active
054202736
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.6 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 hereto 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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Klaus Michael
Mohr Peter
Weiss Ekkehard
Epstein William H.
Gould George M.
Hoffman-La Roche Inc.
Pokras Bruce A.
Raymond Richard L.
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