发明名称 2-aminoalkyl-5-aminoalkylamino substituted isoquinoindazole-6-(2h)-ones with antitumour activity
摘要 Compounds of formula (I) wherein R is hydrogen or hydroxy; one of X and Y is a carbon atom and the other is a nitrogen atom, with the proviso that when Y is nitrogen, R is hydrogen; A and B are the same or different and are selected from the group of C1-C10 alkyl or phenylalkyl; C2-C10 alkyl having one or two substituents selected from the group consisting of OR1 and NR2R3; C2-C10 alkyl interrupted by one or two oxygen atoms or by one -NR4- group, and being said C2-C10 alkyl optionally substituted by one or two hydroxy (OH) or NR2R3 groups; R1 is selected from the group consisting of hydrogen, C1-C6 alkyl, phenyl, phenylalkyl, -S(O2)R5, C2-C6 alkyl optionally substituted by NR2R3; R2 and R3 may be the same or different and are selected from the group consisting of hydrogen, C1-C10 alkyl, phenylalkyl, phenyl, C2-C10 alkyl substituted with one or two hydroxy (OH) groups, or R2 and R3 taken together with the nitrogen atom to which they are attached form an ethyleneimine ring or a 5- or 6-member aromatic or non-aromatic heterocyclic ring which optionally contains another heteroatom such as sulfur, oxygen or nitrogen; R4 is selected from the group consisting of hydrogen, C1-C10 alkyl, C2-C10 hydroxylalkyl, C2-C10 alkyl substituted by NR2R3, phenylalkyl, phenyl; R5 is selected from the group consisting of C1-C10 alkyl, phenylalkyl; as free bases and their salts with pharmaceutically acceptable acids. These compounds have been shown to have antitumor activity.
申请公布号 AU4844193(A) 申请公布日期 1994.04.12
申请号 AU19930048441 申请日期 1993.09.08
申请人 UNIV VERMONT;BOEHRINGER MANNHEIM ITALIA 发明人 KRAPCHO A PAUL;MENTA ERNESTO;OLIVA AMBROGIO;SPINELLI SILVANO
分类号 A61K31/416;A61K31/435;A61K31/437;A61K31/4745;A61P35/00;C07D221/08;C07D471/06 主分类号 A61K31/416
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