Patent ID: 7176327
Filing Date: 2007-02-13
Classification: A61K,A61P,C07F

Abstract:
1. A compound which is a Pt(IV) complex of the general formula I: wherein X 1 and X 2 are the same or different and each one represents a group of the general formula NR 1 R 2 R 3 wherein R 1 , R 2 and R 3 are the same or different and in each case each one may represent any one of H and optionally substituted alkyl, aryl, aralkyl, acyl, cycloalkyl, heterocyclyl, alkenyl, aralkenyl, alkinyl, cycloalkenyl, or X 1 and X 2 together represent a group of the general formula R 1 R 2 NR 4 NR 1 R 2 wherein R 1 and R 2 have the same meaning as hereinbefore, and R 4 represents an optionally substituted divalent, saturated or unsaturated, alkyl chain, an optionally substituted divalent, saturated or unsaturated cycloalkyl or an optionally substituted divalent aryl, or R 4 or two or more of R 1 , R 2 , R 3 and R 4 and the respective N atom(s) to which they are linked, represent an optionally substituted heterocyclyl having at least one ring containing said N atom(s); and Y 1 and Y 2 are the same or different or, when in a cis position, as a further alternative they may together represent a divalent moiety Y 3 , wherein at least one of Y 1 and Y 2 , or Y 3 , is a substantially labile ligand in the analogous Pt(II) complex corresponding to general formula (I) without the azide groups, whilst being substantially resistant, in vivo, to hydrolysis and physiological reducing agents, provided that one or more of R 1 , R 2 , R 3 and R 4 , may further represent a covalently bonded link to at least one further complex of formula I so as to form a dimmer or oligomer, or to a targeting moiety having affinity for a predetermined tissue or cell type, wherein said R 1 R 2 NR 4 NR 1 R 2 group is selected from bipyridyl, phenanthrolyl, 1,2-diaminophenyl and 1,2-diaminocyclohexyl.