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Claims for Patent: 5,431,900

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Claims for Patent: 5,431,900

Title: Ester-substituted diaminedithiols and radiolabeled complexes thereof
Abstract:Radiopharmaceuticals consisting essentially of a lipophilic, charge neutral radionuclide complex of a diaminedithiol ligand having 1-4 ester groups of the formula --A--COOR where A is a straight or branched chain alkylene of 0-10 carbon atoms and R is an alkyl group of 1-10 carbon atoms are useful in radioimaging brain perfusion in primates. Ester-substituted diaminedithiols in sterile, pharmaceutically acceptable form, and kits of the diaminedithiols and sterile, non-pyrogenic reducing agents for reducing preselected radionuclides are also provided. Technetium-99m is a preferred radionuclide.
Inventor(s): Bergstein; Paul L. (Norwood, MA), Cheesman; Edward H. (Townsend, MA), Watson; Alan D. (Andover, MA)
Assignee: The Du Pont Merck Pharmaceutical Company (Wilmington, DE)
Application Number:08/139,894
Patent Claims: 1. An ester-substituted diaminedithiol of the formula: ##STR12## or a pharmaceutically suitable salt thereof wherein: each of R.sub.1 -R.sub.12 individually is selected from the group consisting of H, alkyl of 1-10 carbon atoms and --A--COOR wherein A is a straight or branched chain alkylene of 0-10 carbon atoms, n, o, and p are independently 1 or 2, and R is (a) alkyl of 1-10 carbon atoms, (b) phenyl or benzyl optionally substituted with up to 5 ring substituents each selected from alkyl of 1-4 carbon atoms, fluoro, chloro, bromo, nitro, alkoxy of 1-4 carbon atoms, carboxyl, or a carboxylic acid ester of 1-4 carbon atoms,

said ester-substituted diaminedithiol in sterile, pharmaceutically acceptable form.

2. An ester-substituted diaminedithiol of the formula: ##STR13## or a pharmaceutically suitable salt thereof wherein: each of R.sup.1 -R.sup.12 individually is selected from the group consisting of H, alkyl of 1-10 carbon atoms and --A--COOR wherein A is a straight or branched chain alkylene of 1-10 carbon atoms, n, o, and p are independently 1 or 2, and R is (a) alkyl of 1-10 carbon atoms, with the proviso that at least on of R.sup.1 -R.sup.12 is --A--COOR,

said ester-substituted diaminedithiol in sterile, pharmaceutically acceptable form.

3. A diaminedithiol of claim 2 wherein R and any alkyl in R.sup.1 -R.sup.12 is from 1-3 carbon atoms.

4. A diaminedithiol of claim 2 wherein A is a straight chain alkylene of 0-3 carbon atoms.

5. A diaminedithiol of claim 2 wherein R.sup.3 and R.sup.10 are --A--COOR and R.sup.4 and R.sup.9 are H.

6. A diaminedithiol of claim 2 wherein A is a bond and R is ethyl.

7. A diaminedithiol of claim 2 wherein n, o and p are 1, R.sup.3 and R.sup.10 are --A--COOR where A is a straight chain alkylene of 0-3 carbon atoms and R is alkyl of 1-3 carbon atoms, R.sup.4 and R.sup.9 are H, and R.sup.1, R.sup.2, R.sup.5, R.sup.6, R.sup.7, R.sup.8, R.sup.11 and R.sup.12 individually are selected from the group consisting of H, and alkyl of 1-3 carbon atoms.

8. A diaminedithiol of claim 2 wherein 1-4 of R.sup.1 -R.sup.12 is --A--COOR.

9. A diaminedithiol of claim 2 wherein A is a bond and the stereochemistry at the position where that bond is attached to the diaminedithiol backbone is L.

10. The sterile, pharmaceutically acceptable diaminedithiol of claim 2 which is N,N'-1,2-ethylenediylbis-L-cysteine diethylester, dihydrochloride.

11. The sterile, pharmaceutically acceptable diaminedithiol of claim 2 which is N,N'-1,2-ethylenediylbis-L-cysteine, dimethylester, dihydrochloride.

12. The sterile pharmaceutically acceptable diaminedithiol of claim 2 which is N,N'-1,2-ethylenediylbis-L-cysteine, di-n-propylester, dihydrochloride.

13. A kit comprising a predetermined quantity of a sterile, pharmaceutically acceptable ester-substituted diaminedithiol of claim 1 and a predetermined quantity of a sterile, non-pyrogenic reducing agent for reducing a preselected radionuclide.

14. A kit comprising a predetermined quantity of a sterile, pharmaceutically acceptable ester-substituted diaminedithol of claim 2 and a predetermined quantity of a sterile, non-pyrogenic reducing agent for reducing a preselected radionuclide.

15. A kit of claim 14 wherein the reducing agent is a stannous salt for reducing technetium-99m.

16. A kit of claim 15 wherein the diaminedithiol is a diaminedithiol of claim 3.

17. A kit of claim 15 wherein the diaminedithiol is a diaminedithiol of claim 4.

18. A kit of claim 15 wherein the diaminedithiol is a diaminedithiol of claim 5.

19. A kit of claim 15 wherein the diaminedithiol is a diaminedithiol of claim 6.

20. A kit of claim 15 wherein the diaminedithiol is a diaminedithiol of claim 7.

21. A kit of claim 15 wherein the diaminedithiol is a diaminedithiol of claim 8.

22. A kit of claim 15 wherein the diaminedithiol is the diaminedithiol of claim 9.

23. A kit of claim 15 wherein the diaminedithiol is the diaminedithiol of claim 10.

24. A kit of claim 15 wherein the diaminedithiol is the diaminedithiol of claim 11.

25. A kit of claim 15 wherein the diaminedithiol is the diaminedithol of claim 12.
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