申请人:Hoffmann-LaRoche Inc.
公开号:US05164387A1
公开(公告)日:1992-11-17
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.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)=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 prophylaxix of neoplasms, dermatoses and ageing of the skin.
该发明涉及以下结构的化合物:##STR1##
其中R.sup.1为氢、酰基、较低烷基或--CHO、--CH.sub.2 OR.sup.10、--COR.sup.7或OR.sup.13;R.sup.2、R.sup.3和R.sup.4独立地为氢、较低烷基、较低烷氧基或卤素;R.sup.5和R.sup.6独立地为氢或较低烷基;R.sup.7为羟基、较低烷氧基或NR.sup.8 R.sup.9;R.sup.8和R.sup.9独立地为氢或较低烷基;X和Y独立地为>CR.sup.14 R.sup.15、--O--、--S--、>SO.sub.2或>NR.sup.18;R.sup.10和R.sup.18独立地为氢、较低烷基或酰基;M为--C(R.sup.11)=C(R.sup.12)--、--CONH--或--NH--CO--;R.sup.11、R.sup.12、R.sup.14和R.sup.15独立地为氢或较低烷基;R.sup.13为氢、较低烷氧羰基或较低烷基,可以被
氨基、单烷基
氨基、双烷基
氨基、吗啉基、噻吗
吡啉基或
哌嗪基取代;n为1、2、3或4;但要求至少一个X和Y含有杂原子,并且当X含有杂原子时,n为1、3或4,Y为>C(CH.sub.3).sub.2且R.sup.1为较低烷基或--CH.sub.2 OR.sup.10或--COR.sup.7,或者当R.sup.1为羧基时,为公式I化合物的盐。公式I化合物在肿瘤、皮肤病和皮肤衰老的治疗和预防中有用。