| abstract |
A compound according to formula I: **(See formula)** the compound of formula I being characterized in that it is conjugated, in any of the R1 to R4 positions, with a compound selected from the group consisting of: a) al least one macromolecule of molecular weight and molecular diameter sufficient to substantially or completely prevent passage of the conjugate between said compound according to formula I and said macromolecule through the glomerular filter of the kidneys and passage into the primary urine, wherein said macromolecule is in covalent association with the compound of formula I and wherein the at least one macromolecule is a polyethylene glycol with an average molecular weight of 5 kDa to 100 kDa, and/or b) at least one alpha-emitting radionuclide; wherein R1, R2, R3 and/or R4 in formula I are selected from the group consisting of: hydrogen, amino, mercapto, carboxyl, phosphate and halo, including fluoro, chloro and bromo, C1-C6 alkyl, C1- alkenyl C6, C1-C6 alkynyl, C1-C6 alkanol, C1-C6 alkenol, C1-C6 alkoxy, C1-C6 alkenoxy, and wherein each of these is C1-C6 alkyl, C1-C6 alkenyl, C1-C6 alkynyl, alkanol C1-C6, C1-C6 alkenol, C1-C6 alkoxy, C1-C6 alkenoxy, may be further substituted with moieties selected from the group consisting of amino, mercapto, carboxyl, phosphate, and halo, including fluoro, chloro, and bromo or the equivalent molar amount of a pharmaceutically acceptable salt thereof, for use in the treatment of renal cell carcinoma. |