University of Vermont

Boehringer Mannheim Italia

University of Vermont and State Agricultural College

A Paul Krapcho

Silvano Spinelli

Ernesto Menta

Ambrogio Oliva

Miles P Hacker

Ennio Cavalletti

Ferdinando C Giuliani

John J Landi, Jr

J J McCormack

Kenneth J Shaw

Pyrido-thiopyrandoinazoles with antitumor activity

This invention is directed to 2-aminoalkyl-5-aminoalkylamino substituted isoquino[8,7,6-cd]indazole-6-(2H)-ones and to 2-aminoalkyl-5-aminoalkylamino substituted-isoquino[5,6,7-cd]indazole-6(2H)-ones. These compounds have been shown to have antitumor activity.

2-aminoalkyl-5-aminoalkylamino substituted-isoquinoindazole-6(2H)-ones

This invention is directed to heteroannulated indazoles namely to 2,5-disubstituted quinolino-, isoquinolino-, phthalazino-, and quinoxalino- annulated indazole-6(2H)-ones and related mono N-oxides. These compounds have been shown to have antitumor activity.

Hetero-annulated indazoles

In the search for novel heteroanalogs of anthracenediones, 6,9-bis[(2-aminoethyl-amino]-benzo[g]isoquinoline-5,10-dione dimaleate (BBR 2778), was selected as the most promising compound. Toxicological studies indicate that BBR 2778 is not cardiotoxic.

6,9-bis[(2-aminoethyl) amino]benzo [g]isoquinoline-5,10- dione

This invention is directed to 2-aminoalkyl-5-aminoalkylamino substituted isoquino [8,7,6-cd]indazole-6-(2H)-ones and to 2-aminoalkyl-5-aminoalkylamino substituted-isoquino [5,6,7-cd] indazole-6(2H)-ones. These compounds have been shown to have antitumor activity.

The disclosure describes unsymmetrical 1,4-bis-(aminoalkylamino)-anthracene-9,10-diones useful in the treatment of neoplasms. Also described is a process of preparing same starting from 1,4-dimethoxyanthracene-9,10-dione which is reacted with an aminoalkylamine. The reaction product is treated with a dialkylaminoethylamine or a N-heteroethylamine to give the unsymmetrical compound.

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Shelburne, VT, United States of America

A Paul Krapcho