Nycomed Amersham Plc

Amersham International Plc

Amersham Plc

Colin M Archer

Ian A Latham

Jonathan R Dilworth

Russell M Thompson

Panna Jobanputra

Lewis Reuben Canning

Anthony Leonard Riley

Harjit Kaur Gill

Anthony Eamon Storey

Gary Robert Bower

David Vaughan Griffiths

James Frederick Burke

Barbara Edwards

Adam Charles King

Cores for technetium radiopharmaceuticals

.sup.99m Tc complexes of formula L.sub.n Tc.dbd.NR, L.sub.n Tc--N.dbd.NY, or L.sub.n Tc--(N.dbd.NY).sub.2 wherein each L is independently a monodentate or multidentate ligand;

Ligands for radiopharmaceutical use are capable of chelating radiometal species and of being bound to biological targeting molecules. The ligands have formula (a) and (b), where A, A'=--SZ or Y, B.dbd.O or S, Y.dbd. (c), Z.dbd.H or a thiol protecting group, m=2 or 3, n=2 or 3, q=0 or 1, R.dbd.H or unsubstituted or substituted hydrocarbon and pharmaceutically acceptable salts, provided that at least one CR.sub.2 group represents CO and forms, together with an adjacent N atom, a --CONR-- amide group. ##STR1##

Metal chelating compounds having an SNNN donor set

A synth .sup.99m Tc complex which contains the moiety Tc.dbd.NR, Tc--N.dbd.NY or Tc(--N.dbd.NY).sub.2 and an organic ligand which confers biological target-seeking properties on the technetium complex, where R is an aryl group, a substituted or unsubstituted alkyl group or the group --NR.sup.1 R.sup.2 ; Y is an aryl group or a substituted or unsubstituted alkyl group; and R.sup.1 and R.sup.2 are H, aryl groups or substituted or unsubstituted aliphatic or cyclic alkyl groups, and are the same or different provided that both are not hydrogen. Radiopharmaceuticals comprising this complex are also described, together with methods for the preparation of the complex.

Radiometal complexes that localise in hypoxic tissue

Metal-oxime chelates for use as radiopharmaceutical agents

Ligands for radiopharmaceutical use are capable of chelating radiometal species and of being bound to biological targeting molecules. The ligands have the formula (a) and (b), where A, A'=--SZ or Y, B=O or S, Y=(c), Z=H or a thiol protecting group, m=2 or 3, n=2 or 3, q=0 or 1, R=H or unsubstituted or substituted hydrocarbon and pharmaceutically acceptable salts, provided that at least one CR.sub.2 group represents CO and forms, together with an adjacent N atom; a --CONR-- amide group. ##STR1##

Thioether-containing metal chelating compounds

Novel complexes of technetium (.sup.99 Tc or .sup.99m Tc) which contain the moiety Tc.dbd.NR, Tc--N.dbd.NY or Tc(--N.dbd.NY).sub.2, and a ligand which confers biological target-seeking properties on the complex, wherein R represents an aryl group, a substituted or unsubstituted alkyl group, or the grouping .dbd.NR.sup.1 R.sup.2 ; Y represents an aryl group or a substituted or unsubstituted alkyl group; and R.sup.1 and R.sup.2 are hydrogen, aryl groups or substituted or unsubstituted aliphatic or cyclic alkyl groups, and may be both the same or different, provided that both are not hydrogen. The complexes are suitable for use in radiopharmaceuticals for a variety of clinical applications. Methods for the preparation of these technetium complexes are also described.

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Buckinghamshire, United Kingdom

Colin M Archer