Photoreactive compounds and compositions

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...

Reexamination Certificate

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C546S012000

Reexamination Certificate

active

07928097

ABSTRACT:
The present invention provides a compound of formula (I): PtIV(N3)2X1X2Y1Y2, wherein X1and X2are the same or different and each one is a group NR1R2R3wherein R1, R2and R3are the same or different and each can be any one of H and optionally substituted alkyl, aryl, aralkyl, acyl, cycloalkyl, heterocyclyl, alkenyl, aralkenyl, alkinyl, cycloalkenyl, or X1and X2together represent a group R1R2NR4NR1R2wherein R1and R2have the same meaning as before, and R4represents an optionally substituted divalent, saturated or unsaturated, alkyl chain, an optionally substituted divalent, saturated or unsaturated cycloalkyl or an optionally substituted divalent aryl, or R4or two or more of R1, R2, R3and R4and 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 Y1and Y2are the same or different or when cis together represent a divalent moiety Y3, wherein at least one of Y1and Y2, or Y3, is a substantially labile ligand in the analogous Pt(II) complex without the azide groups, whilst being substantially resistant, in vivo, to hydrolysis and physiological reducing agents. One or more of R1, R2, R3and R4, may further represent a covalently bonded link to at least one further complex of formula (I) to form a dimer or oligomer, or to a targeting moiety having affinity for a predetermined tissue or cell type.

REFERENCES:
Mackay, F.S. et al.: A potent cytotoxic photoactivated platinum complex. PNAS, vol. 104, pp. 20743-20748, 2007.

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