Spofa, Spojene Podniky Pro Zdravotnickou Vyrobu

Vufb A.s

Milan Miko

Jiri Krepelka

Milan Melka

Irena Kejhova

Jaroslava Grimova

Antonin Cerny

Stanislava Pokorna

Ruzena Reichlova

Milan Ferenc

Milan Hruby

Marta Beitova

Rzena Reichlova

Jiri Michalsky, Deceased

Anna Kargerova

Josef Urbanec

Alois Kolonicny

Eva Skacelova

Jiri Hrbata

Jitka Sediva

##STR1## New 6-[X-(2-hydroxyethyl)aminoalkyl]-5,11-dioxo-5,6-dihydro-11H-indeno[-1,2-c] isochinoline derivatives represented by general formula (I), in which X stands for the number of carbon atoms from 0 to 5 in aminoalkyl group situated on nitrogen atom in position 6 of the indenoisochinoline fundamental structure, their salts with inorganic and organic acids and their derivatives were described. Antitumorously effective indenoisochinoline derivatives are most preferably prepared by the process in which the indeno[1,2-c]isocoumarine and/or 1-methoxy-2-(2-methoxycarbonylphenyl)-1-inden-3-one, respectively, comprises reacting with N-(hydroxyethyl)alkylen diamine in a medium of suitable aprotic solvent, preferably dimethylformamide, and at increased temperature. Another process for the preparation comprises reacting 6-(X-chloroalkyl)-5,11-dioxo-5,6-dihydro-11H-indeno[1,2-c]isochinolines with 2-aminoethanol in suitable solvent, preferably dimethylformamide, in the presence of anhydrous potassium carbonate. New compounds, their derivatives and salts are useful for the preparation of drugs and compositions for the treatment of malignant neoplasias in mammals.

6-[X-(2-hydroxyethyl)

6-purinyl N-(2-chloroethyl) carbamate and thiocarbamate are disclosed of the general formula I, ##STR1## in which X stands for an oxygen or sulfur atom, and also a process for their preparation by reacting a purine derivative of the general formula II (hypoxanthine or 6-mercaptopurine, respectively) with 2-chloroethylisocyanate. The subject compounds of formula I show a remarkable antineoplastic effect in vitro and in vivo, and consequently have great potential for the treatment of malignant neoplastic diseases in mammals.

6-purinyl N-/2-chloroethyl/carbamate and thiocarbamate and process for

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Bratislava, Czechoslovakia

Milan Miko