Cancer targeting using carbonic anhydrase isoform ix inhibitors
AssigneesClaudiu Supuran, Stichting Maastricht Radiation Oncology “Maastro-Clinic”, Cnrs (Centre National De La Recherche Scientifique)
InventorsPhilippe Lambin, Jean-Yves Winum, Claudiu Supuran
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Abstract
The present invention concerns novel carbonic anhydrase IX inhibitors comprising a nitroimidazole moiety and their use in therapy of hypoxic conditions, in particular cancer treatment, especially chemotherapy and radiotherapy. The compounds of the invention have an increased specificity for the carbonic anhydrase IX enzyme compared to the art. The present invention relates to novel nitroimidazole derivates represented by formula (1).
Claims19
1-35. (canceled)
A compound of formula (1),
- wherein Z is Z1 with formula (2a):
- or Z is Z2 with formula (2b):
- (CH2)nCH2X
- or Z is Z3 with formula (2c):
- and R1 and R2 can be, each independently, H, alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclic, aryl, cyano or halogen atom;
- R3, R4, R6 and R7 can be, each independently H, alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclic, aryl, halogen atom, cyano, alkoxy, sulfonamide, sulfamate or sulfamide;
- R5 can be sulfonamide, sulfamate or sulfamide;
- X=sulfonamide, sulfamate or sulfamide;
- Y═O or S;
- n=0, 1, 2, 3, 4 or 5 and where if n=0, R2=2-CH3, Z═Z1, R3═R4═R6═R7═H and R5═SO2NH2 the NO2 is not on position 4, or a pharmaceutically acceptable salt thereof.
The compound or salt according to claim 1 wherein Y═S.
Dependencies are inferred from the claim text.