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Last Updated: December 22, 2024

Claims for Patent: 10,398,791


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Summary for Patent: 10,398,791
Title:Labeled inhibitors of prostate specific membrane antigen (PSMA), their use as imaging agents and pharmaceutical agents for the treatment of prostate cancer
Abstract: The present invention generally relates to the field of radiopharmaceuticals and their use in nuclear medicine as tracers, imaging agents and for the treatment of various disease states of prostate cancer. Thus, the present invention concerns compounds that are represented by the general Formulae (Ia) or (Ib).
Inventor(s): Eder; Matthias (Mannheim, DE), Kopka; Klaus (Dossenheim, DE), Schafer; Martin (Neckarsteinach, DE), Bauder-Wust; Ulrike (Schriesheim, DE), Haberkorn; Uwe (Schwetzingen, DE), Eisenhut; Michael (Heidelberg, DE), Mier; Walter (Bensheim, DE), Benesova; Martina (Heidelberg, DE)
Assignee: DEUTSCHES KREBSFORSCHUNGSZENTRUM (Heidelberg, DE) RUPRECHT-KARLS-UNIVERSITAT HEIDELBERG (Heidelberg, DE)
Application Number:16/114,988
Patent Claims: 1. A compound of the formula: ##STR00023## or a salt thereof.

2. The compound or salt thereof according to claim 1, wherein the compound or salt is lyophilized.

3. A composition comprising: (1) the compound and/or a salt thereof according to claim 1; and (2) optionally a pharmaceutically acceptable carrier.

4. The composition of claim 3, wherein the composition further comprises an excipient, and wherein the excipient is different from said pharmaceutically acceptable carrier.

5. The composition of claim 3, wherein the composition is a buffered solution.

6. The composition of claim 3, wherein the compound and/or a salt thereof, and optionally the pharmaceutically acceptable carrier, are lyophilized.

7. A compound of the formula: ##STR00024## or a salt thereof.

8. The compound or salt thereof according to claim 7, wherein the compound or salt is lyophilized.

9. A composition comprising: (1) the compound and/or a salt thereof according to claim 7; and (2) optionally a pharmaceutically acceptable carrier.

10. The composition of claim 9, wherein the composition further comprises an excipient, and wherein the excipient is different from said pharmaceutically acceptable carrier.

11. The composition of claim 9, wherein the composition is a buffered solution.

12. A compound of the formula: ##STR00025## or a salt thereof, wherein R' is a chelator of the formula: ##STR00026## wherein .sup.177Lu is complexed to the chelator.

13. A composition comprising: (1) the compound and/or a salt thereof according to claim 12; and (2) optionally a pharmaceutically acceptable carrier.

14. The composition of claim 13, wherein the composition further comprises an excipient, and wherein the excipient is different from said pharmaceutically acceptable carrier.

15. The composition of claim 13, wherein the composition is a buffered solution.

16. A compound of the formula: ##STR00027## or a salt thereof, wherein R' is a chelator of the formula: ##STR00028## wherein .sup.177Lu is complexed to the chelator.

17. A composition comprising: (1) the compound and/or a salt thereof according to claim 16; and (2) optionally a pharmaceutically acceptable carrier.

18. The composition of claim 17, wherein the composition further comprises an excipient, and wherein the excipient is different from said pharmaceutically acceptable carrier.

19. The composition of claim 17, wherein the composition is a buffered solution.

20. The composition of claim 9, wherein the compound and/or a salt thereof, and optionally the pharmaceutically acceptable carrier, are lyophilized.

21. The compound of claim 7 having the formula: ##STR00029## or a salt thereof.

22. The compound or salt thereof according to claim 21, wherein the compound or salt is lyophilized.

23. A composition comprising: (1) the compound and/or a salt thereof according to claims 21; and (2) optionally a pharmaceutically acceptable carrier.

24. The composition of claim 23, wherein the composition further comprises an excipient, and wherein the excipient is different from said pharmaceutically acceptable carrier.

25. The composition according to claim 23, wherein the composition is a buffered solution.

26. The composition of claim 23, wherein the compound and/or a salt thereof, and optionally the pharmaceutically acceptable carrier, are lyophilized.

27. The compound of claim 16 having the formula: ##STR00030## or a salt thereof, wherein R' is a chelator of the formula: ##STR00031## wherein .sup.177Lu is complexed to the chelator.

28. A composition comprising: (1) the compound and/or a salt thereof according to claims 27; and (2) optionally a pharmaceutically acceptable carrier.

29. The composition of claim 28, wherein the composition further comprises an excipient, and wherein the excipient is different from said pharmaceutically acceptable carrier.

30. The composition of claim 28, wherein the composition is a buffered solution.

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