.

Pharmaceutical Business Intelligence

  • Anticipate P&T budget requirements
  • Evaluate market entry opportunities
  • Find generic sources and suppliers
  • Predict branded drug patent expiration

► Plans and Pricing

Upgrade to enjoy subscriber-only features like email alerts and data export. See the Plans and Pricing

DrugPatentWatch Database Preview

Claims for Patent: 5,279,811

« Back to Dashboard

Claims for Patent: 5,279,811

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:07/143,561
Patent Claims: 1. A radiopharmaceutical comprising a lipophilic, charge neutral complex of a radionuclide and a diaminedithiol ligand wherein the diaminedithiol is selected from the following formula A and B; ##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, or (c) a 5- or 6-membered heterocyclic ring containing 1 or 2 heteroatoms selected from N, O or X, with the proviso that at lest one of R.sub.1 -R.sub.12 is --A--COOR,

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

2. A radiopharmaceutical of claim 1 wherein the radionuclide is a radioactive isotope of Tc, Ru, Cu, Co, Pt, Fe, Os, Ir, W, Re, Cr, Mo, Mn, Ni, Rh, Pd, Nb, or Ta.

3. A radiopharmaceutical of claim 1 wherein the radionuclide is technetium-99m.

4. A radiopharmaceutical to claim 1 wherein the diaminedithiol has the formula: ##STR13## wherein each of R.sup.1 -R.sup.12 individually is selected from the group consisting of H. alkyl of 1-6 carbon atoms and --A--COOR wherein A is a straight or branched chain alkylene of 0-6 carbon atoms, n, o and p are independently 1 or 2, and R is alkyl of 1-6 carbon atoms, with the proviso that at least one of R.sup.1 --R.sup.12 is --A--COOR.

5. A radiopharmaceutical of claim 4 wherein the radionuclide is a radioactive isotope of Tc, Ru, Cu, Co, Pt, Fe, Os, Jr, W, Re, Cr, Mo, Mn, Ni, Rh, Pd, Nb, or Ta.

6. A radiopharmaceutical of claim 4 wherein the radionuclide is technetium-99m.

7. A radiopharmaceutical of claim 6 wherein R and any alkyl in R.sup.1 -R.sup.12 is from 1-3 carbon atoms.

8. A radiopharmaceutical of claim 6 wherein A is a straight chain alkylene of 0-3 carbon atoms.

9. A radiopharmaceutical of claim 6 wherein n, o and p are 1. and 1-4 of R.sup.1 -R.sup.12 is --A--COOR.

10. A radiopharmaceutical of claim 9 wherein the diaminedithiol is non-aminated, and R and any alkyl in R.sup.1 -R.sup.12 is from 1-3 carbon atoms.

11. A radiopharmaceutical of claim 5 wherein R.sup.3 and R.sup.10 are --A--COOR and R.sup.4 and R.sup.9 are H and n, o and p are 1.

12. A radiopharmaceutical of claim 6 wherein A is a bond and R is ethyl.

13. A radiopharmaceutical of claim 6 wherein A is a bond and the stereochemistry at the position where that bond is attached to the diaminedithiol backbone is L.

14. A radiopharmaceutical of claim 6 wherein n, o and p are 1. and 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.

15. The radiopharmaceutical of claim 6 wherein the diaminedithiol is N,N'-1.2-ethylenedi-ylbis-L-cysteine, diethyl ester.

16. The radiopharmaceutical of claim 6 wherein the diaminedithiol is N,N'-1.2-ethylene-diylbis-L-cysteine, dimethylester, dihydrochloride.

17. The radiopharmaceutical of claim 6 wherein the diaminedithol is N,N'-1,2-ethylene-diylbis-L-cysteine, di-n-polyester, dihydrochloride.

18. A process of radioimaging comprising (i) administering parenterally to a mammal an effective amount of the composition of claim 1 in a pharmaceutically suitable carrier, and (ii) radioimaging the brain of the mammal after allowing sufficient time for the composition to localize in the brain.

19. A process of radioimaging comprising (i) administering parenterally to a mammal an effective amount of the composition of claim 2 in a pharmaceutically suitable carrier, and (ii) radioimaging the brain of the mammal after allowing sufficient time for the composition to localize in the brain.

20. A process of radioimaging comprising (i) administering parenterally to a mammal an effective amount of the composition of claim 3 in a pharmaceutically suitable carrier, and (ii) radioimaging the brain of the mammal after allowing sufficient time for the composition to localize in the brain.

21. A process of radioimaging comprising (i) administering parenterally to a mammal an effective amount of the composition of claim 4 in a pharmaceutically suitable carrier, and (ii) radioimaging the brain of the mammal after allowing sufficient time for the composition to localize in the brain.

22. A process of radioimaging comprising (i) administering parenterally to a mammal an effective amount of the composition of claim 5 in a pharmaceutically suitable carrier, and (ii) radioimaging the brain of the mammal after allowing sufficient time for the composition to localize in the brain.

23. A process of radioimaging comprising (i) administering parenterally to a mammal an effective amount of the composition of claim 6 in a pharmaceutically suitable carrier, and (ii) radioimaging the brain of the mammal after allowing sufficient time for the composition to localize in the brain.

24. A process of radioimaging comprising (i) administering parenterally to a mammal an effective amount of the composition of claim 7 in a pharmaceutically suitable carrier, and (ii) radioimaging the brain of the mammal after allowing sufficient time for the composition to localize in the brain.

25. A process of radioimaging comprising (i) administering parenterally to a mammal an effective amount of the composition of claim 8 in a pharmaceutically suitable carrier, and (ii) radioimaging the brain of the mammal after allowing sufficient time for the composition to localize in the brain.

26. A process of radioimaging comprising (i) administering parenterally to a mammal an effective amount of the composition of claim 9 in a pharmaceutically suitable carrier, and (ii) radioimaging the brain of the mammal after allowing sufficient time for the composition to localize in the brain.

27. A process of radioimaging comprising (i) administering parenterally to a mammal an effective amount of the composition of claim 6 in a pharmaceutically suitable carrier, and (ii) radioimaging the brain of the mammal after allowing sufficient time for the composition to localize in the brain.

28. A process of radioimaging comprising (i) administering parenterally to a mammal an effective amount of the composition of claim 11 in a pharmaceutically suitable carrier, and (ii) radioimaging the brain of the mammal after allowing sufficient time for the composition to localize in the brain.

29. A process of radioimaging comprising (i) administering parenterally to a mammal an effective amount of the composition of claim 12 in a pharmaceutically suitable carrier, and (ii) radioimaging the brain of the mammal after allowing sufficient time for the composition to localize in the brain.

30. A process of radioimaging comprising (i) administering parenterally to a mammal an effective amount of the composition of claim 13 in a pharmaceutically suitable carrier, and (ii) radioimaging the brain of the mammal after allowing sufficient time for the composition to localize in the brain.

31. A process of radioimaging comprising (i) administering parenterally to a mammal an effective amount of the composition of claim 14 in a pharmaceutically suitable carrier, and (ii) radioimaging the brain of the mammal after allowing sufficient time for the composition to localize in the brain.

32. A process of radioimaging comprising (i) administering parentally to a mammal an effective amount of the composition of claim 15 in a pharmaceutically suitable carrier, and (ii) radioimaging the brain of the mammal after allowing sufficient time for the composition to localize in the brain.

33. A process of radioimaging comprising (i) administering parenterally to a mammal an effective amount of the composition of claim 11 in a pharmaceutically suitable carrier, and (ii) radioimaging the brain of the mammal after allowing sufficient time for the composition to localize in the brain.

34. A process of radioimaging comprising (i) administering parenterally to a mammal an effective amount of the composition of claim 11 in a pharmaceutically suitable carrier, and (ii) radioimaging the brain of the mammal after allowing sufficient time for the composition to localize in the brain.
« Back to Dashboard

For more information try a trial or see the database preview and plans and pricing

How are People Using DrugPatentWatch?

Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verifification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.

`abc