Amersham International Plc

Nycomed Amersham Plc

Amersham Plc

Ian A Latham

Colin M Archer

Jonathan R Dilworth

Panna Jobanputra

Russell M Thompson

James D Kelly

Kwok W Chiu

David V Griffiths

Peter Gerald Edwards

Joanne L Newman

John R Thornback

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;

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.

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.

Complexes useful as radiopharmaceuticals contain the .sup.99m Tc-NO moiety and up to four organic ligands which confer biological target-seeking properties on the complex. Preferred are mono-cationic complexes, particularly having the formula

Complexes of TC99m radiopharmaceuticals

This invention concerns novel bidentate ligands L having two phosphorus or arsenic atoms. Cationic complexes of the ligands with Technetium-99m, e.g. having the formula [TcO.sub.2 L.sub.2 ].sup.+, are useful for body imaging, particularly myocardial imaging. The ligands have the general formula

Ligands and cationic complexes thereof with technetium-99m

The invention concerns cationic complexes of Technetium-99m with bidentate ligands (L), including complexes having the formulae [Tc(NO) X L.sub.2 ].sup.+ and [Tc L.sub.3 ].sup.+, which are of interest as heart imaging agents. The ligands are characterized by having the formula Y.sub.2 QZQY.sub.2, where each Q is phosphorus or arsenic, Z is a 2 or 3 carbon atom linking group, and at least one of the groups Y and Z includes at least one --COC--ether group.

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Buckinghamshire, United Kingdom

Ian A Latham