Certain isoquinoline derivatives having anti-tumor properties
AssigneeLaboratoires Glaxo SA
InventorsBernard Andre Dumaitre, Nerina Dodic, Alain Claude-Marie Daugan, Pascal Maurice Charles Pianetti
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Abstract
Compounds are described of general formula (I) ##STR1## and salts and solvates thereof, including physiologically acceptable salts and solvates thereof, in which: Z represents either Het, ##STR2## Het represents an optionally substituted bicyclic or tricyclic ring selected from acricine isoquinolin-1-yl, isoquinolin-3-yl, The novel compounds of formula (I) can sensitize multi-drug resistant cancer cells to chemotherapeutic agents and may be formulated for use in therapy, particularly to improve or increase the efficacy of an anti-tumour drug.
Claims11
A compound of formula (Ia) ##STR13## wherein Z represents ##STR14## X represents an oxygen atom or NH;
- A represents an oxygen or a sulphur atom, a bond or a group (CH.sub.2).sub.1 NR.sup.7 where I represents zero or 1 and R.sup.7 represents a hydrogen atom or a methyl group;
- B represents a C.sub.1-4 alkylene chain optionally substituted by a hydroxyl group, except that the hydroxyl group and moiety A cannot be attached to the same carbon atom when A represents an oxygen or sulphur atom or a group (CH.sub.2).sub.1 NR.sup.7, or when A represents a bond B may also represent a C.sub.2-4 alkenylene chain;
- R.sup.2 represents a hydrogen or a halogen atom, or a C.sub.1-4 alkyl, C.sub.1-4 alkoxy or C.sub.1-4 alkylthio group;
- R.sup.3 represents a hydrogen atom or a C.sub.1-4 alkoxy group;
- R.sup.8 represents a hydrogen or halogen atom or a C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 akylthio or nitro group;
- R.sup.9 represents a hydrogen or halogen atom or a C.sub.1-4 alkyl, C.sub.1-4 alkoxy or C.sub.1-4 alkylthio group;
- R.sup.10 and R.sup.11 each represent a hydrogen atom or together form a bond or a linking atom selected from --O--, --S-- and NH;
- and physiologically acceptable salts and solvates thereof.
Dependencies are inferred from the claim text.