Compsn. for dissipation of necrotic tissue and tumours - contains an oxazole-5-one deriv. of low toxicity

摘要

Compsn. which causes dissipation of (ecrotic) tissue and/or tumours contains >=1 oxazolone deriv. of formula (I). R1 = H or opt. substd. alkyl. R2 = aryl, 5-7 membersed heterocycle with 1 or 2 N, S or O atoms, alkyl, lower alkoxy, 4-7C cycloalkyl or cycloalkenyl, aralkyl or aralkenyl, all opt. substd.; or R1 + R2 together completel a 5-7C cycloalkylidene or cycloalkenylidene. R3 = alkyl, aryl, 4-7 membered heterocycle with 1 or 2 hetero atoms, aralkyl or aralkenyl, all opt. substd. (I) cause lysis of human or animals tissues and/or tumours, and have much lower toxicity than known cytostatics, e.g. an i, v, injection of 80 mg per day for 3 weeks caused no toxic manifestrations in rabbits. They are useful for treating tumours (including leukoses), scars ulcers, Hodgkin's disease, mycoses etc. A typical cpd, is 4-(3-chlorophenyl)-2-(1-acetamido-2-phenylethyl)-5(4H)-oxozolone, prepd. by reacting D, L-N-acetylphenylalanylglycine with 3-chlorobenzaldehyde.