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    • 2. 发明专利
    • Compositions for protecting human skin and hair against the damaging effects of ultraviolet radiation, comprise new or known N-substituted anilinomethylene malonic acid derivatives
    • DE10063867A1
    • 2002-07-11
    • DE10063867
    • 2000-12-21
    • HAARMANN & REIMER GMBH
    • DILK ERICHJOHNCOCK WILLIAMLANGNER ROLAND
    • A61K8/04A61K8/41A61K8/42A61K8/44A61K8/49A61K8/58A61K8/891A61K8/898A61Q5/00A61Q17/04A61K7/42
    • Cosmetic and pharmaceutical compositions for protecting human skin and hair against the damaging effects of ultraviolet radiation, comprise N-substituted anilinomethylene malonic acid derivatives (I). Cosmetic and pharmaceutical compositions for protecting human skin and hair against the damaging effects of ultraviolet radiation comprise N-substituted anilinomethylene compounds of formula (I). R = 1-20C alkyl, 2-20C alkenyl, 3-15C cycloalkyl, 6-12C aryl, aralkyl (with 6-12C aryl and 1-6C alkyl components) or 5-12C heteroaryl, all optionally substituted by 1-6C alkyl, 1-16C alkoxy, 6-12C aryloxy, NH2, OH, COOR , CONR R and/or W or interrupted by ether oxygen; R = COOR , CONR R , CN or COR ; R = COOR , CONR R , CN or COR ; R -R = H, NH2, NO2 or R ; R -R = H or R , provided that R is not COOR ; W = a group of formula W1-W3; a, b = 0-3, provided that a+b = 3; A = a bond to the neighboring atom (sic); c = 1-10; and R = an aliphatic, araliphatic, alicyclic or optionally substituted aromatic group with up to 18C atoms. An Independent claim is also included for the following compounds: 2-(N-methylanilinomethylene)-propanedioic acid di-n-propyl, di-1-methylethyl, di-n-butyl, di-2-methylpropyl, di-n-pentyl, di-3-methylbutyl, di-4-methylpentyl and di-2-ethylhexyl esters; 2-(N-ethylanilinomethylene)-propanedioic acid di-n-propyl, di-1-methylethyl, di-n-butyl, di-2-methylpropyl, di-n-pentyl and di-3-methylbutyl esters; 2-(N-propylanilinomethylene)-propanedioic acid di-n-propyl, di-1-methylethyl, di-n-butyl, di-2-methylpropyl and di-3-methylbutyl esters; 2-cyano-2-(N-methylanilino)-2-propenoic acid n-propyl, methylethyl, n-butyl, 2-methylpropyl, n-pentyl, 3-methylbutyl, n-hexyl, 4-methylpentyl and 2-ethylhexyl esters; 2-cyano-2-(N-ethylanilino)-2-propenoic acid n-propyl, methylethyl, n-butyl, 2-methylpropyl, n-pentyl, 3-methylbutyl, n-hexyl, 4-methylpentyl, n-octyl and 2-ethylhexyl esters; and 2-cyano-2-(N-propylanilino)-2-propenoic acid n-propyl, methylethyl, n-butyl, 2-methylpropyl, n-pentyl, 3-methylbutyl, n-hexyl, 4-methylpentyl, n-octyl and 2-ethylhexyl esters.