Norsk Hydro, A.s.

Bayer As

Thomas Ramdahl

John M Dornish

Erik O Pettersen

Reidar Oftebro

Rolf O Larsen

Bernt Borretzen

Bernt Bo Slashedrretzen

Vidar Moen

Rold O Larsen

Bernt Boorretzen

The present invention provides a tissue-targeting complex comprising a tissue targeting moiety, an octadentate hydroxypyridinone-containing ligand and the ion of an alpha-emitting thorium radionuclide. The invention additionally provides therapeutic methods employing such complexes, methods of their production and use, and kits and pharmaceutical compositions comprising such complexes.

Alpha-emitting complexes

Pharmaceutical compositions

New compounds having the general formula I ##STR1## wherein L may be H or D; Y may be CN or ##STR2## wherein A may be H, D, alkyl with 1-4 carbon atoms, OR wherein R is H or alkyl with 1-4 carbon atoms, or CR.sub.1 R.sub.2 R.sub.3 wherein R.sub.1, R.sub.2 and R.sub.3 are the same or different and are H or alkyl with 1-4 carbon atoms; Z is H, D, Y or alkyl with 1-4 C-atoms, halogen, nitro, amino, monoalkyl amino or dialkyl amino wherein the alkyl groups have 1-4 C atoms, or OR wherein R may be H or alkyl with 1-4 C-atoms, or CR.sub.4 R.sub.5 R.sub.6 wherein R.sub.4, R.sub.5 and R.sub.6 may be the same or different and may be H or F; X.sub.1 and X.sub.2 may be the same or different and may be OR, NR.sub.1 R.sub.2 or SR, wherein R, R.sub.1 and R.sub.2 may be the same or different and may be alkyl having 1-22 carbon atoms which may be branched or straight chained and/or may be further substituted; or X.sub.1 and X.sub.2 may together with the carbon atom to which they are bound form a cyclic acetal, thioacetal, dithiane, aminal, oxazolidine or thiazolidine; and pharmaceutically acceptable salts thereof. The compounds are useful as anti-cancer agents and as agents useful for the treatment of illnesses arising due to an abnormally elevated cell-proliferation.

Compounds

New compounds of formula I: ##STR1## wherein Y may be CN or ##STR2## wherein A may be H, D, alkyl with 1-4 carbon atoms, OR wherein R is H or alkyl with 1-4 carbon atoms, or --NR.sub.1 R.sub.2 or --CR.sub.1 R.sub.2 R.sub.3 wherein R.sub.1, R.sub.2 and R.sub.3 are the same or different and are H or alkyl with 1-4 carbon atoms;

Deuterated benzaldehydes

Growing community of inventors

Eiksmarka, Norway

Thomas Ramdahl