Amersham International Plc

Nycomed Amersham Plc

Lewis Reuben Canning

Colin M Archer

Anthony Leonard Riley

Harjit Kaur Gill

Anthony Eamon Storey

Gary Robert Bower

David P Nowotnik

David Vaughan Griffiths

Barbara Edwards

Adam Charles King

Ian M Piper

Rudi D Neirinckx

James Frederick Burke

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

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 propylene amine oxime ligands have the formula ##STR1## where each of R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7 or R.sub.8 may be hydrogen, hydrocarbon, carboxyl, amine, amide or nitrile, provided that, if R.sub.1 is the same as R.sub.9 and R.sub.2 is the same as R.sub.7, then R.sub.8 is not H. These unsymmetrical ligands form complexes with Technetium-99m which are capable, on injection into mammals, of crossing the blood-brain barrier and of being retained in the brain for a time to permit diagnosis.

Complexes of Technetium 99m with propylene amine oximes

A family of propylene amine oxime ligands has the formula 2 ##STR1## wherein preferably R.sup.1 is Cl-C4 alkyl or phenyl and each of R, R.sup.2, R.sup.3 and R.sup.4 is H or Cl-C4 alkyl. The technetium-99m complexes of these ligands are lipophilic neutral complexes useful as diagnostic radiopharmaceuticals and particularly for brain scanning. The ligands show stereoisomerism. The preparation and properties of the dl- and meso-stereoisomers, and of the d- and l-enantiomers, are described. The l-enantiomer and the dl-stereoisomer of the preferred compound (2, R=R.sup.1 =R.sup.2 =CH.sub.3, R.sup.3 =R.sup.4 =H) show good retention in the brain.

Complexes of technetium-99m with propylene amine oximes

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Chesham, United Kingdom

Lewis Reuben Canning