Spofa, Spojene Podniky Pro Zdravotnickou Vyrobu

Vufb A.s

Milan Melka

Jiri Krepelka

Irena Kejhova

Milan Miko

Stanislava Pokorna

Ruzena Reichlova

Jaroslava Grimova

Karel Rezabek

Antonin Cerny

Vojtech Pujman

Milan Hruby

Anna Kargerova

Iva Vancurova

Slavjanka Cernochova

Alois Kolonicny

Josef Urbanec

Marta Beitova

Rzena Reichlova

Jiri Michalsky, Deceased

Jitka Sediva

Eva Skacelova

Jiri Hrbata

Milan Ferenc

##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

Basic ethers of 7-oxo-7H-benzo(c) fluorene have been shown to evidence a pronounced antineoplastic and immunosuppressive effect in mammals suffering from leukemia. The technique for preparing the described ethers and the addition salts thereof with pharmaceutically acceptable organic and inorganic acids involves the aminoalkylation of 5-hydroxy-7-oxo-7H-benzo(c) fluorene and its corresponding nuclear substituted derivatives on the hydroxylic oxygen atom.

Basic ethers of 7-oxo-7H-benzo(c) fluorene and a process for their

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Hradec Kralove, Czechia

Milan Melka