The Radiochemical Centre Limited

Amersham International Plc

Nycomed Amersham Plc

Anthony Leonard Riley

Reginald Monks

Anthony Eamon Storey

Colin M Archer

Lewis Reuben Canning

Gary Robert Bower

Harjit Kaur Gill

James D Kelly

David Vaughan Griffiths

Alan Michael Forster

Virginia Edith Chambers

Gavin Murray Cree

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

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

Biological targeting agents

Agents for the diagnosis or treatment of hypoxic cells comprise a bioreductive moiety such as 2-nitroimidazole, and a metal chelating moiety which is a bis-amine oxime of which a carbon atom adjacent a nitrogen atom is linked to the bioreductive moiety. A chelated metal atom or ion preferably Technetium-99m. The agent diffuses into cells where the 2-nitroimidazole is reduced thus trapping the chelated metal in the cell.

Metal complexes for hypoxic cells

Metal chelating ligands for hypoxic cells

Body function of a mammal is investigated using a .gamma.-emitting .sup.75 Se or .sup.123m Te labelled derivative of a bile acid or bile salt. Thus bowel function may be investigated by oral administration of the labelled compound followed, after a suitable period of time, by either a whole body count or a faecal count of radioactivity. Preferred bile acids and salts are substituted either at the 19-position or in the C-17 side chain.

Investigating body function

The present invention provides compounds having the general formula ##STR1## wherein R is ##STR2## and A is 0 or 1,

Labelled bile acids

Novel selenium derivatives of steroids have the formula I, ##STR1## where X is hydrogen or acyl, Y is hydrocarbon and n is 0 or 1, preferably 0. Such compounds, labelled with selenium-75 are of use for investigating body function, particularly for imaging the adrenal glands, and are claimed superior for the purpose to the 6.beta.- and 19- iodine derivatives of cholesterol.

Organ visualization

Novel selenium-75 derivatives of cholesterol have the formula ##STR1## (I) where X is hydrogen or acyl, Y is alkyl and n is 0 or 1. They are useful for visualizing the adrenal glands of mammals.

Novel dimeric and monomeric selenium-75 derivatives of steroids are made by reacting a keto steroid with selenium-75 dioxide or selenious acid-Se75. The resulting diselenide dimers can be converted into monomeric compounds by the use of a cleaving reagent followed by an alkylating agent. The compounds are useful in saturation analyses such as radioimmunoassays.

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Marlow, United Kingdom

Anthony Leonard Riley