DERIVATIVES OF NITROGENOUS YPERITE BOUND WITH AMINO ACIDS THAT ARE PRODRUG SUBSTRATES FOR CARBOXYPEPTIDASE ENZYME, METHOD OF THEIR SYNTHESIS, PHARMACEUTICAL COMPOSITION AND BIOCOMPONENT SYSTEM FOR CYTOTOXIC DRUG DELIVERY Russian patent published in 1999 - IPC

FIELD: organic chemistry, biochemistry, pharmacy. SUBSTANCE: invention relates to new compounds of the formula (I) where R₁ and R₂ each independently means chlorine, bromine, iodine atoms or a group OSO₂Me; R^1a and R^2b - hydrogen atom; R₃ and R₄ - hydrogen atom; R^5a and R^5b - hydrogen atom, C_1-4-alkyl, haloid; R^5a and R^5b form -CH=CH-CH=CH-; R^5c and R^5d - hydrogen atom, cyano-group, haloid; X means O, NH, -CH₂-; Y means O; Z means -V-W where V means -CH₂T- where T means -CH₂- or -S-; W means COOH, -(C=O)NR₇R₈ where R₇ - hydrogen atom, C_1-6-alkyl and the others; R₈ - hydrogen atom and their salts. Method of synthesis of compounds of the formula (I) involves removal of protection in compound of the formula (Ia) . Invention proposes a pharmaceutical composition containing an effective amount of compound of the formula (I) and a bicomponent system for delivery of cytotoxic drug consisting of antibody or its fragment which are able to bind a definite antigen. Antigen or its fragment are conjugated with an enzyme CPG which is able to convert a compound of the formula (I) or its salt to a cytotoxic drug and has additionally a compound of the formula (I) or its salt which are converted to a cytotoxic drug by an enzyme CPG effect. EFFECT: improved method of synthesis and drug delivery. 16 cl, 12 dwg, 18 tbl, 46 ex