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Claims for Patent: 4,789,736

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Claims for Patent: 4,789,736

Title: Complexes of technetium-99m with propylene amine oximes
Abstract: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.
Inventor(s): Canning; Lewis R. (Herts, GB2), Nowotnik; David P. (Bucks, GB2), Neirinckx; Rudi D. (Bucks, GB2), Piper; Ian M. (Herts, GB2)
Assignee: Amersham International plc (Bucks, GB2)
Application Number:06/838,558
Patent Claims: 1. A lipophilic macrocyclic complex, useful as a diagnostic radiopharmaceutical, of technetium-99m with a propylene amine oxime ligand having the formula: ##STR9## said complex being in the form of a single stereoisomer or a mixture of stereoisomers.

2. The complex according to claim 1 wherein the ligand is the dl-diastereoisomer.

3. The complex according to claim 1 wherein the ligand is the l-enantiomer.

4. The complex according to claim 1 wherein the ligand is the d-enantiomer.

5. A propylene amine oxime ligand having the formula: ##STR10## said ligand being in the form of a single stereoisomer or a mixture of stereoisomers.

6. The ligand according to claim 5 which is the dl-diastereoisomer.

7. The ligand according to claim 5 which is the l-enantiomer.

8. The ligand as claimed in claim 5 which is the d-enantiomer.

9. The complex according to claim 1, having the formula: ##STR11##
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